Apoptosis-inducing agents for treatment of cancer and immune and autoimmune diseases
Patent Information
- Application Number
- JP2025019817
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2009-05-26
- Filing Date
- 2025-02-10
- Publication Date
- 2025-05-09
- Estimated Expiration
- Not applicable · inactive patent
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Figure 2025072583000001 
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Abstract
Description
[Technical Field]
[0001] This application claims priority to U.S. Provisional Patent Application No. 61 / 181,203, filed May 26, 2009, which is incorporated herein by reference in its entirety.
[0002] FIELD OF THE INVENTION The present invention relates to compounds that inhibit the activity of the Bcl-2 anti-apoptotic protein, compositions containing the compounds, and methods for treating diseases in which the anti-apoptotic Bcl-2 protein is expressed. [Background technology]
[0003] Background of the Invention Anti-apoptotic Bcl-2 proteins have been implicated in many diseases, and therefore there is an ongoing need in the therapeutic field for compounds that inhibit the activity of anti-apoptotic Bcl-2 proteins.
[0004] Overexpression of Bcl-2 protein correlates with resistance to chemotherapy, clinical outcome, disease progression, overall prognosis, or a combination thereof, in various cancers and disorders of the immune system.
[0005] The involvement of Bcl-2 protein in bladder cancer, brain cancer, breast cancer, bone marrow cancer, cervical cancer, chronic lymphocytic leukemia, colorectal cancer, esophageal cancer, hepatocellular carcinoma, lymphoblastic leukemia, follicular lymphoma, lymphoid malignancies of T-cell or B-cell origin, melanoma, myeloid leukemia, myeloma, oral cancer, ovarian cancer, non-small cell lung cancer, prostate cancer, small cell lung cancer, pancreatic cancer, and the like, is described in commonly owned PCTUS2004 / 36770, published as WO2005 / 049593, and PCTUS2004 / 37911, published as WO2005 / 024636.
[0006] The involvement of Bcl-2 proteins in immune and autoimmune diseases has been described in Current Allergy and Asthma Reports 2003, 3, 378-384; British Journal of Haematology 2000, 110(3), 584-90; Blood 2000, 95(4), 1283-92; and New England Journal of Medicine 2004, 351(14), 1409-1418. The involvement of Bcl-2 proteins in arthritis has been disclosed in commonly owned U.S. Provisional Patent Application No. 60 / 988,479. The involvement of Bcl-2 proteins in bone marrow transplant rejection has been disclosed in commonly owned U.S. Provisional Patent Application No. 11 / 941,196. [Prior art documents] [Patent documents]
[0007] [Patent Document 1] International Publication No. 2005 / 049593 [Patent Document 2] International Publication No. 2005 / 024636 [Patent Document 3] U.S. Provisional Patent Application No. 60 / 988479 [Patent Document 4] U.S. Provisional Patent Application No. 11 / 941196 [Non-patent literature]
[0008] [Non-Patent Document 1] Current Allergy and Asthma Reports 2003, 3, 378-384 [Non-patent document 2] British Journal of Haematology 2000, 110(3), 584-90 [Non-patent document 3] Blood 2000, 95(4), 1283-92 [Non-patent document 4] New England Journal of Medicine 2004, 351(14), 1409-1418. Summary of the Invention
[0009] Summary of the Invention Accordingly, one embodiment of the present invention relates to compounds or therapeutically acceptable salts that are useful as inhibitors of anti-apoptotic Bcl-2 proteins, which compounds have the following formula (I):
[0010] [ka] During the ceremony, A 1 is N or C(A 2 ) and; A 2 H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; B 1 は、H、R 1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; D 1 は、H、R 1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; IN 1 は、H、R 1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1, NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A and; Y 1 are H, CN, NO2, C(O)OH, F, Cl, Br, I, CF3, OCF3, CF2CF3, OCF2CF3, R 17 , OR 17 , C(O)R 17 , C(O)OR 17 , S.R. 17 , SO2R 17 , NH2, NHR 17 , N(R 17 )2, NHC(O)R 17 , C(O)NH2, C(O)NHR 17 , C(O)N(R 17 )2, NHS(O)R 17 or NHSO2R 17 is; or E 1 and Y 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; A 2 , B 1 and D 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A is; or Y 1 and B 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; A 2 、D 1 and E 1 are independently selected from H, R 1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 [[ID=3l]])2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 ?、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR [[ID=*]] 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1 ?、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CHs)R 1 、N(CH3)SO2N(CH3)R 1 It should be noted that there may be some unclear or potentially incorrect notations in the original text, such as "C(NH)NH2" which might be more accurately written as "C(NH2)NH2" in a more standard chemical context. This translation attempts to maintain the integrity of the original text as much as possible while converting it to English., F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A is; or A 2 and B 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; D 1 , E 1 and Y 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1, C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A is; or A 2 and D 1 together with the atoms to which they are attached are benzene, naphthalene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; B 1 , E 1 and Y 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A and; G 1 is H or C(O)OR; R is alkyl; R 1 is R 2 , R 3 , R 4 or R 5 and; R 1A is cycloalkyl, cycloalkenyl or cycloalkynyl; R 2 is uncondensed or R 2A is a phenyl fused to R 2A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 3 is uncondensed or R 3A is a heteroaryl fused to R 3A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 4 are uncondensed or R 4A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to4A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 5 are each unsubstituted or one, two, or three independently selected R 6 , NC(R 6A )(R 6B ), R 7 , OR 7 , S.R. 7 , S(O)R 7 , SO2R 7 , NHR 7 , N(R 7 )2, C(O)R 7 , C(O)NH2, C(O)NHR 7 , C(O)N(R 7 )2, NHC(O)R 7 , N.R. 7 C(O)R 7 , NHSO2R 7 , NHC(O)OR 7 , SO2NH2, SO2NHR 7 , SO2N(R 7 )2, NHC(O)NH2, NHC(O)NHR 7 , NHC(O)CH(CH3)NHC(O)CH(CH3)NH2, NHC(O)CH(CH3)NHC(O)CH(CH3)NHR 7 , OH, (O), C(O)OH, N3, CN, NH2, CF3, CF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 6 is a C2-C5 spiroalkyl, each unsubstituted or substituted with OH, (O), N3, CN, CF3, CF2CF3, F, Cl, Br, I, NH2, NH(CH3), or N(CH3)2; R 6A and R 6B are independently selected alkyls or together with the N to which they are attached form R 6C and; R 6Cis aziridin-1-yl, azetidin-1-yl, pyrrolidin-1-yl or piperidin-1-yl, each of which has one CH moiety that is unsubstituted or replaced by O, C(O), CNOH, CNOCH3, S, S(O), SO2 or NH; R 7 is R 8 , R 9 , R 10 or R 11 and; R 8 is not condensed or R 8A is a phenyl fused to R 8A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 9 is uncondensed or R 9A is a heteroaryl fused to R 9A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 10 are uncondensed or R 10A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 10A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 11 are each unsubstituted or one, two, or three independently selected R 12 , OR 12 , S.R. 12 , S(O)R 12 , SO2R 12 , C(O)R 12 , CO(O)R 12 ,OC(O)R 12 ,OC(O)OR 12 , NH2, NHR 12 , N(R 12 )2, NHC(O)R 12 , N.R. 12 C(O)R 12 , NHS(O)2R 12 , N.R.12 S(O)2R 12 , NHC(O)OR 12 , N.R. 12 C(O)OR 12 , NHC(O)NH2, NHC(O)NHR 12 , NHC(O)N(R 12 )2, NR 12 C(O)NHR 12 , N.R. 12 C(O)N(R 12 )2, C(O)NH2, C(O)NHR 12 , C(O)N(R 12 )2, C(O)NHOH, C(O)NHOR 12 , C(O)NHSO2R 12 , C(O)NR 12 SO2R 12 , SO2NH2, SO2NHR 12 , SO2N(R 12 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 12 , C(N)N(R 12 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 12 is R 13 , R 14 , R 15 or R 16 and; R 13 is uncondensed or R 13A is a phenyl fused to R 13A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 14 is uncondensed or R 14A is a heteroaryl fused to R 14A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 15 are uncondensed or R 15Aa cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene fused with R 15A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 16 is alkyl, alkenyl, or alkynyl; R 17 is R 18 , R 19 , R 20 or R 21 and; R 18 is not condensed or R 18A is a phenyl fused to R 18A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 19 is not condensed or R 19A is a heteroaryl fused to R 19A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 20 are uncondensed or R 20A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 20A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 21 are each unsubstituted or one, two, or three independently selected R 22 , OR 22 , S.R. 22 , S(O)R 22 , SO2R 22 , C(O)R 22 , CO(O)R 22 ,OC(O)R 22 ,OC(O)OR 22 , NH2, NHR 22 , N(R 22 )2, NHC(O)R 22 , N.R. 22 C(O)R22 , NHS(O)2R 22 , N.R. 22 S(O)2R 22 , NHC(O)OR 22 , N.R. 22 C(O)OR 22 , NHC(O)NH2, NHC(O)NHR 22 , NHC(O)N(R 22 )2, NR 22 C(O)NHR 22 , N.R. 22 C(O)N(R 22 )2, C(O)NH2, C(O)NHR 22 , C(O)N(R 22 )2, C(O)NHOH, C(O)NHOR 22 , C(O)NHSO2R 22 , C(O)NR 22 SO2R 22 , SO2NH2, SO2NHR 22 , SO2N(R 22 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 22 , C(N)N(R 22 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 22 is R 23 , R 24 or R 25 and; R 23 is uncondensed or R 23A is a phenyl fused to R 23A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 24 is uncondensed or R 24A is a heteroarene fused to; R 24A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 25 are uncondensed or R25A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 25A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; Z 1 is R 26 or R 27 and; Z 2 is R 28 , R 29 or R 30 and; Z 1A and Z 2A are both absent or together are CH2, CH2CH2 or Z 12A It forms; Z 12A is C2-C6-alkylene with one or two CH2 moieties replaced by NH, N(CH3), S, S(O) or SO2; L 1 is R 37 , OR 37 , S.R. 37 , S(O)R 37 , SO2R 37 , C(O)R 37 , CO(O)R 37 ,OC(O)R 37 ,OC(O)OR 37 , NHR 37 , C(O)NH, C(O)NR 37 , C(O)NHOR 37 , C(O)NHSO2R 37 , SO2NH, SO2NHR 37 , C(N)NH, C(N)NHR 37 and; R 26 is uncondensed or R 26A is a phenylene fused to R 26A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 27 is uncondensed or R 27A is a heteroarylene fused to R27A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 28 is uncondensed or R 28A is a phenylene fused to R 28A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 29 is uncondensed or R 29A is a heteroarylene fused to R 29A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 30 are uncondensed or R 30A a cycloalkylene, cycloalkenylene, heterocyclic alkylene, or heterocyclic alkenylene fused with R 30A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 37 is a bond or R 37A and; R 37A are each unsubstituted or one, two, or three independently selected R 37B , OR 37B , S.R. 37B , S(O)R 37B , SO2R 37B , C(O)R 37B , CO(O)R 37B ,OC(O)R 37B ,OC(O)OR 37B , NH2, NHR 37B , N(R 37B )2, NHC(O)R 37B , N.R. 37B C(O)R 37B , NHS(O)2R 37B , N.R. 37B S(O)2R 37B , NHC(O)OR 37B , N.R. 37B C(O)OR 37B, NHC(O)NH2, NHC(O)NHR 37B , NHC(O)N(R 37B )2, NR 37B C(O)NHR 37B , N.R. 37B C(O)N(R 37B )2, C(O)NH2, C(O)NHR 37B , C(O)N(R 37B )2, C(O)NHOH, C(O)NHOR 37B , C(O)NHSO2R 37B , C(O)NR 37B SO2R 37B , SO2NH2, SO2NHR 37B , SO2N(R 37B )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 37B , C(N)N(R 37B )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, alkylene, alkenylene or alkynylene substituted with F, Cl, Br and I substituents; R 37B is alkyl, alkenyl, alkynyl or R 37C and; R 37C is phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; Z 3 is R 38 , R 39 or R 40 and; R 38 is not condensed or R 38A is a phenyl fused to R 38A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 39 is not condensed or R 39A is a heteroaryl fused to R 39A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 40are uncondensed or R 40A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 40A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 26 and R 27 The part represented by R 41 , OR 41 , S.R. 41 , S(O)R 41 , SO2R 41 , C(O)R 41 , CO(O)R 41 ,OC(O)R 41 ,OC(O)OR 41 , NHR 41 , N(R 41 )2, NHC(O)R 41 , N.R. 41 C(O)R 41 , NHS(O)2R 41 , N.R. 41 S(O)2R 41 , NHC(O)OR 41 , N.R. 41 C(O)OR 41 , NHC(O)NHR 41 , NHC(O)N(R 41 )2, NR 41 C(O)NHR 41 , N.R. 41 C(O)N(R 41 )2, C(O)NHR 41 , C(O)N(R 41 )2, C(O)NHOR 41 , C(O)NHSO2R 41 , C(O)NR 41 SO2R 41 , SO2NHR 41 , SO2N(R 41 )2, C(N)NHR 41 or C(N)N(R 41 )2 (i.e., Z 1A and Z 2A is absent) or further substituted (i.e., Z 1A and Z2A if exists); R 41 is R 43A is a heteroaryl fused to R 43A is unfused or benzene, heteroarene or R 43B benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene fused with; R 43B is a cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; E 1 and Y 1 is one, Y 1 and B 1 is one, A 2 and B 1 is one, A 2 and D 1 is one, R 1A , R 2 , R 2A , R 3 , R 3A , R 4 , R 4A , R 6 , R 6C , R 8 , R 8A , R 9 , R 9A , R 10 , R 10A , R 13 , R 13A , R 14 , R 14A , R 15 , R 15A , R 18 , R 18A , R 19 , R 19A , R 20 , R 20A , R 23 , R 23A , R 24 , R 24A , R 25 , R 25A , R 26 , R 26A , R 27 , R 27A , R 28 , R 28A , R 29 , R29A , R 30 , R 30A , R 37B , R 38 , R 38A , R 39 , R 39A , R 40 and R 40A is independently unsubstituted, further unsubstituted, or contains 1 or 2 or 3 or 4 or 5 independently selected R 57A , R 57 , OR 57 , S.R. 57 , S(O)R 57 , SO2R 57 , C(O)R 57 , CO(O)R 57 ,OC(O)R 57 ,OC(O)OR 57 , NH2, NHR 57 , N(R 57 )2, NHC(O)R 57 , N.R. 57 C(O)R 57 , NHS(O)2R 57 , N.R. 57 S(O)2R 57 , NHC(O)OR 57 , N.R. 57 C(O)OR 57 , NHC(O)NH2, NHC(O)NHR 57 , NHC(O)N(R 57 )2, NR 57 C(O)NHR 57 , N.R. 57 C(O)N(R 57 )2, C(O)NH2, C(O)NHR 57 , C(O)N(R 57 )2, C(O)NHOH, C(O)NHOR 57 , C(O)NHSO2R 57 , C(O)NR 57 SO2R 57 , SO2NH2, SO2NHR 57 , SO2N(R 57 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 57 , C(N)N(R 57)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, substituted or further substituted with F, Cl, Br or I; R 57A is spiroalkyl or spiroheteroalkyl; R 57 is R 58 , R 59 , R 60 or R 61 and; R 58 is not condensed or R 58A is a phenyl fused to R 58A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 59 is not condensed or R 59A is a heteroaryl fused to R 59A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 60 are uncondensed or R 60A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 60A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 61 are each unsubstituted or one, two, or three independently selected R 62 , OR 62 , S.R. 62 , S(O)R 62 , SO2R 62 , C(O)R 62 , CO(O)R 62 ,OC(O)R 62 ,OC(O)OR 62 , NH2, NHR 62 , N(R 62 )2, NHC(O)R 62 , N.R. 62 C(O)R 62 , NHS(O)2R62 , N.R. 62 S(O)2R 62 , NHC(O)OR 62 , N.R. 62 C(O)OR 62 , NHC(O)NH2, NHC(O)NHR 62 , NHC(O)N(R 62 )2, NR 62 C(O)NHR 62 , N.R. 62 C(O)N(R 62 )2, C(O)NH2, C(O)NHR 62 , C(O)N(R 62 )2, NHC(O)N(R 57 )2, NR 57 C(O)NHR 57 , N.R. 57 C(O)N(R 57 )2, C(O)NH2, C(O)NHR 57 , C(O)N(R 57 )2, C(O)NHOH, C(O)NHOR 57 , C(O)NHSO2R 57 , C(O)NR 57 SO2R 57 , SO2NH2, SO2NHR 57 , SO2N(R 57 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 57 , C(N)N(R 57 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 57A is spiroalkyl or spiroheteroalkyl; R 57 is R 58 , R 59 , R 60 or R 61 and; R 58 is not condensed or R 58A is a phenyl fused to R 58Ais benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 59 is not condensed or R 59A is a heteroaryl fused to R 59A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 60 are uncondensed or R 60A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 60A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 61 are each unsubstituted or one, two, or three independently selected R 62 , OR 62 , S.R. 62 , S(O)R 62 , SO2R 62 , C(O)R 62 , CO(O)R 62 ,OC(O)R 62 ,OC(O)OR 62 , NH2, NHR 62 , N(R 62 )2, NHC(O)R 62 , N.R. 62 C(O)R 62 , NHS(O)2R 62 , N.R. 62 S(O)2R 62 , NHC(O)OR 62 , N.R. 62 C(O)OR 62 , NHC(O)NH2, NHC(O)NHR 62 , NHC(O)N(R 62 )2, NR 62 C(O)NHR 62 , N.R. 62 C(O)N(R 62 )2, C(O)NH2, C(O)NHR 62 , C(O)N(R 62 )2, C(O)NHOH, C(O)NHOR 62, C(O)NHSO2R 62 , C(O)NR 62 SO2R 62 , SO2NH2, SO2NHR 62 , SO2N(R 62 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 62 , C(N)N(R 62 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 62 is R 63 , R 64 , R 65 or R 66 and; R 63 is not condensed or R 63A is a phenyl fused to R 63A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 64 is not condensed or R 64A is a heteroaryl fused to R 64A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 65 are uncondensed or R 65A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 65A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 66 are each unsubstituted or one, two, or three independently selected R 67 , OR 67 , S.R. 67 , S(O)R 67 , SO2R 67 , C(O)R 67 , CO(O)R 67 ,OC(O)R 67,OC(O)OR 67 , NH2, NHR 67 , N(R 67 )2, NHC(O)R 67 , N.R. 67 C(O)R 67 , NHS(O)2R 67 , N.R. 67 S(O)2R 67 , NHC(O)OR 67 , N.R. 67 C(O)OR 67 , NHC(O)NH2, NHC(O)NHR 67 , NHC(O)N(R 67 )2, NR 67 C(O)NHR 67 , N.R. 67 C(O)N(R 67 )2, C(O)NH2, C(O)NHR 67 , C(O)N(R 67 )2, C(O)NHOH, C(O)NHOR 67 , C(O)NHSO2R 67 , C(O)NR 67 SO2R 67 , SO2NH2, SO2NHR 67 , SO2N(R 67 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 67 , C(N)N(R 67 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br, or I substituent substituted alkyl, alkenyl, or alkynyl; R 67 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 57A , R 58 , R 59 , R 60 , R 63 , R 64 , R 65 and R 67The cyclic moiety represented by the formula (I) is unsubstituted or is substituted with 1 or 2 or 3 or 4 independently selected R 68 , OR 68 , S.R. 68 , S(O)R 68 , SO2R 68 , C(O)R 68 , CO(O)R 68 ,OC(O)R 68 ,OC(O)OR 68 , NH2, NHR 68 , N(R 68 )2, NHC(O)R 68 , N.R. 68 C(O)R 68 , NHS(O)2R 68 , N.R. 68 S(O)2R 68 , NHC(O)OR 68 , N.R. 68 C(O)OR 68 , NHC(O)NH2, NHC(O)NHR 68 , NHC(O)N(R 68 )2, NR 68 C(O)NHR 68 , N.R. 68 C(O)N(R 68 )2, C(O)NH2, C(O)NHR 68 , C(O)N(R 68 )2, C(O)NHOH, C(O)NHOR 68 , C(O)NHSO2R 68 , C(O)NR 68 SO2R 68 , SO2NH2, SO2NHR 68 , SO2N(R 68 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 68 , C(N)N(R 68 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I; R 68 is R 69 , R 70 , R 71 or R 72 and; R69 is not condensed or R 69A is a phenyl fused to R 69A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 70 is uncondensed or R 70A is a heteroaryl fused to R 70A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 71 are uncondensed or R 71A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 71A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 72 are each unsubstituted or one, two, or three independently selected R 73 , OR 73 , S.R. 73 , S(O)R 73 , SO2R 73 , C(O)R 73 , CO(O)R 73 ,OC(O)R 73 ,OC(O)OR 73 , NH2, NHR 73 , N(R 73 )2, NHC(O)R 73 , N.R. 73 C(O)R 73 , NHS(O)2R 73 , N.R. 73 S(O)2R 73 , NHC(O)OR 73 , N.R. 73 C(O)OR 73 , NHC(O)NH2, NHC(O)NHR 73 , NHC(O)N(R 73 )2, NR 73 C(O)NHR 73 , N.R. 73 C(O)N(R 73 )2, C(O)NH2, C(O)NHR73 , C(O)N(R 73 )2, C(O)NHOH, C(O)NHOR 73 , C(O)NHSO2R 73 , C(O)NR 73 SO2R 73 , SO2NH2, SO2NHR 73 , SO2N(R 73 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 73 , C(N)N(R 73 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 73 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 69 , R 70 and R 71 is unsubstituted or substituted with one or two or three or four independently selected NH, C(O)NH, C(O)NHOH, SONH, CF, CFCF, C(O)H, C(O)OH, C(N)NH, OH, (O), CN, N, NO, CF, CFCF, OCF, OCFCF, F, Cl, Br, or I.
[0011] Another embodiment of the present invention relates to compounds or therapeutically acceptable salts useful as inhibitors of anti-apoptotic Bcl-2 proteins, which compounds have the following formula (II) or a therapeutically acceptable salt thereof:
[0012] [ka] During the ceremony, R 100 is R 26 as described for the substituents above; n is 0, 1, 2 or 3; A1 はNまたはC(A 2 )であり; WHOSE 2 は、H、R 1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1, F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A and; E 1 and Y 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; A 2 , B 1 and D 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1, C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A is; or Y 1 and B 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; A 2 , D 1 and E 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A is; or A 2 and B 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; D 1 , E 1 and Y 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A is; or A 2 and D 1 together with the atoms to which they are attached are benzene, naphthalene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; B 1 , E 1 and Y 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A and; R 1 is R 2 , R 3 , R 4 or R 5 and; R 1A is cycloalkyl, cycloalkenyl or cycloalkynyl; R 2 is uncondensed or R 2A is a phenyl fused to R 2Ais benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 3 is uncondensed or R 3A is a heteroaryl fused to R 3A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 4 are uncondensed or R 4A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 4A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 5 are each unsubstituted or one, two, or three independently selected R 6 , NC(R 6A )(R 6B ), R 7 , OR 7 , S.R. 7 , S(O)R 7 , SO2R 7 , NHR 7 , N(R 7 )2, C(O)R 7 , C(O)NH2, C(O)NHR 7 , C(O)N(R 7 )2, NHC(O)R 7 , N.R. 7 C(O)R 7 , NHSO2R 7 , NHC(O)OR 7 , SO2NH2, SO2NHR 7 , SO2N(R 7 )2, NHC(O)NH2, NHC(O)NHR 7 , NHC(O)CH(CH3)NHC(O)CH(CH3)NH2, NHC(O)CH(CH3)NHC(O)CH(CH3)NHR 7 , OH, (O), C(O)OH, N3, CN, NH2, CF3, CF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R6 is a C2-C5 spiroalkyl, each unsubstituted or substituted with OH, (O), N3, CN, CF3, CF2CF3, F, Cl, Br, I, NH2, NH(CH3), or N(CH3)2; R 6A and R 6B are independently selected alkyls or together with the N to which they are attached form R 6C and; R 6C is aziridin-1-yl, azetidin-1-yl, pyrrolidin-1-yl or piperidin-1-yl, each of which has one CH moiety that is unsubstituted or replaced by O, C(O), CNOH, CNOCH3, S, S(O), SO2 or NH; R 7 is R 8 , R 9 , R 10 or R 11 and; R 8 is not condensed or R 8A is a phenyl fused to R 8A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 9 is uncondensed or R 9A is a heteroaryl fused to R 9A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 10 are uncondensed or R 10A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 10A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 11 are each unsubstituted or one, two, or three independently selected R 12 , OR 12 , S.R. 12 , S(O)R12 , SO2R 12 , C(O)R 12 , CO(O)R 12 ,OC(O)R 12 ,OC(O)OR 12 , NH2, NHR 12 , N(R 12 )2, NHC(O)R 12 , N.R. 12 C(O)R 12 , NHS(O)2R 12 , N.R. 12 S(O)2R 12 , NHC(O)OR 12 , N.R. 12 C(O)OR 12 , NHC(O)NH2, NHC(O)NHR 12 , NHC(O)N(R 12 )2, NR 12 C(O)NHR 12 , N.R. 12 C(O)N(R 12 )2, C(O)NH2, C(O)NHR 12 , C(O)N(R 12 )2, C(O)NHOH, C(O)NHOR 12 , C(O)NHSO2R 12 , C(O)NR 12 SO2R 12 , SO2NH2, SO2NHR 12 , SO2N(R 12 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 12 , C(N)N(R 12 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 12 is R 13 , R 14 , R 15 or R 16 and; R 13 is uncondensed or R 13A is a phenyl fused to R 13Ais benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 14 is uncondensed or R 14A is a heteroaryl fused to R 14A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 15 are uncondensed or R 15A a cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene fused with R 15A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 16 is alkyl, alkenyl, or alkynyl; R 17 is R 18 , R 19 , R 20 or R 21 and; R 18 is not condensed or R 18A is a phenyl fused to R 18A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 19 is not condensed or R 19A is a heteroaryl fused to R 19A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 20 are uncondensed or R 20A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 20A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 21 are each unsubstituted or one, two, or three independently selected R 22, OR 22 , S.R. 22 , S(O)R 22 , SO2R 22 , C(O)R 22 , CO(O)R 22 ,OC(O)R 22 ,OC(O)OR 22 , NH2, NHR 22 , N(R 22 )2, NHC(O)R 22 , N.R. 22 C(O)R 22 , NHS(O)2R 22 , N.R. 22 S(O)2R 22 , NHC(O)OR 22 , N.R. 22 C(O)OR 22 , NHC(O)NH2, NHC(O)NHR 22 , NHC(O)N(R 22 )2, NR 22 C(O)NHR 22 , N.R. 22 C(O)N(R 22 )2, C(O)NH2, C(O)NHR 22 , C(O)N(R 22 )2, C(O)NHOH, C(O)NHOR 22 , C(O)NHSO2R 22 , C(O)NR 22 SO2R 22 , SO2NH2, SO2NHR 22 , SO2N(R 22 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 22 , C(N)N(R 22 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 22 is R 23 , R 24 or R 25 and; R 23 is uncondensed or R 23A is a phenyl fused to R 23Ais benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 24 is uncondensed or R 24A is a heteroarene fused to; R 24A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 25 are uncondensed or R 25A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 25A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; Z 2 is R 28 , R 29 or R 30 and; L 1 is R 37 , OR 37 , S.R. 37 , S(O)R 37 , SO2R 37 , C(O)R 37 , CO(O)R 37 ,OC(O)R 37 ,OC(O)OR 37 , NHR 37 , C(O)NH, C(O)NR 37 , C(O)NHOR 37 , C(O)NHSO2R 37 , SO2NH, SO2NHR 37 , C(N)NH, C(N)NHR 37 and; R 28 is uncondensed or R 28A is a phenylene fused to R 28A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 29 is uncondensed or R 29A is a heteroarylene fused to R 29Ais benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 30 are uncondensed or R 30A a cycloalkylene, cycloalkenylene, heterocyclic alkylene, or heterocyclic alkenylene fused with R 30A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 37 is a bond or R 37A and; R 37A are each unsubstituted or one, two, or three independently selected R 37B , OR 37B , S.R. 37B , S(O)R 37B , SO2R 37B , C(O)R 37B , CO(O)R 37B ,OC(O)R 37B ,OC(O)OR 37B , NH2, NHR 37B , N(R 37B )2, NHC(O)R 37B , N.R. 37B C(O)R 37B , NHS(O)2R 37B , N.R. 37B S(O)2R 37B , NHC(O)OR 37B , N.R. 37B C(O)OR 37B , NHC(O)NH2, NHC(O)NHR 37B , NHC(O)N(R 37B )2, NR 37B C(O)NHR 37B , N.R. 37B C(O)N(R 37B )2, C(O)NH2, C(O)NHR 37B , C(O)N(R 37B )2, C(O)NHOH, C(O)NHOR 37B , C(O)NHSO2R 37B , C(O)NR 37B SO2R 37B , SO2NH2, SO2NHR37B , SO2N(R 37B )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 37B , C(N)N(R 37B )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br and I substituents substituted alkylene, alkenylene or alkynylene; R 37B is alkyl, alkenyl, alkynyl or R 37C and; R 37C is phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; Z 3 is R 38 , R 39 or R 40 and; R 38 is not condensed or R 38A is a phenyl fused to R 38A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 39 is not condensed or R 39A is a heteroaryl fused to R 39A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 40 are uncondensed or R 40A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 40A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; E 1 and Y 1 is one, Y 1 and B 1 is one, A 2 and B 1 is one, A 2 and D 1 is one, R1A , R 2 , R 2A , R 3 , R 3A , R 4 , R 4A , R 6 , R 6C , R 8 , R 8A , R 9 , R 9A , R 10 , R 10A , R 13 , R 13A , R 14 , R 14A , R 15 , R 15A , R 18 , R 18A , R 19 , R 19A , R 20 , R 20A , R 23 , R 23A , R 24 , R 24A , R 25 , R 25A , R 26 , R 26A , R 27 , R 27A , R 28 , R 28A , R 29 , R 29A , R 30 , R 30A , R 37B , R 38 , R 38A , R 39 , R 39A , R 40 and R 40A is independently unsubstituted, further unsubstituted, or contains 1 or 2 or 3 or 4 or 5 independently selected R 57A , R 57 , OR 57 , S.R. 57 , S(O)R 57 , SO2R 57 , C(O)R 57 , CO(O)R 57 ,OC(O)R 57 ,OC(O)OR 57, NH2, NHR 57 , N(R 57 )2, NHC(O)R 57 , N.R. 57 C(O)R 57 , NHS(O)2R 57 , N.R. 57 S(O)2R 57 , NHC(O)OR 57 , N.R. 57 C(O)OR 57 , NHC(O)NH2, NHC(O)NHR 57 , NHC(O)N(R 57 )2, NR 57 C(O)NHR 57 , N.R. 57 C(O)N(R 57 )2, C(O)NH2, C(O)NHR 57 , C(O)N(R 57 )2, C(O)NHOH, C(O)NHOR 57 , C(O)NHSO2R 57 , C(O)NR 57 SO2R 57 , SO2NH2, SO2NHR 57 , SO2N(R 57 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 57 , C(N)N(R 57 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, substituted or further substituted with F, Cl, Br or I; R 57A is spiroalkyl or heterospiroalkyl; R 57 is R 58 , R 59 , R 60 or R 61 and; R 58 is not condensed or R 58A is a phenyl fused to R 58A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 59 is not condensed or R59A is a heteroaryl fused to R 59A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 60 are uncondensed or R 60A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 60A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 61 are each unsubstituted or one, two, or three independently selected R 62 , OR 62 , S.R. 62 , S(O)R 62 , SO2R 62 , C(O)R 62 , CO(O)R 62 ,OC(O)R 62 ,OC(O)OR 62 , NH2, NHR 62 , N(R 62 )2, NHC(O)R 62 , N.R. 62 C(O)R 62 , NHS(O)2R 62 , N.R. 62 S(O)2R 62 , NHC(O)OR 62 , N.R. 62 C(O)OR 62 , NHC(O)NH2, NHC(O)NHR 62 , NHC(O)N(R 62 )2, NR 62 C(O)NHR 62 , N.R. 62 C(O)N(R 62 )2, C(O)NH2, C(O)NHR 62 , C(O)N(R 62 )2, C(O)NHOH, C(O)NHOR 62 , C(O)NHSO2R 62 , C(O)NR 62 SO2R 62 , SO2NH2, SO2NHR 62, SO2N(R 62 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 62 , C(N)N(R 62 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 62 is R 63 , R 64 , R 65 or R 66 and; R 63 is not condensed or R 63A is a phenyl fused to R 63A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 64 is not condensed or R 64A is a heteroaryl fused to R 64A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 65 are uncondensed or R 65A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 65A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 66 are each unsubstituted or one, two, or three independently selected R 67 , OR 67 , S.R. 67 , S(O)R 67 , SO2R 67 , C(O)R 67 , CO(O)R 67 ,OC(O)R 67 ,OC(O)OR 67 , NH2, NHR 67 , N(R 67 )2, NHC(O)R 67 , N.R.67 C(O)R 67 , NHS(O)2R 67 , N.R. 67 S(O)2R 67 , NHC(O)OR 67 , N.R. 67 C(O)OR 67 , NHC(O)NH2, NHC(O)NHR 67 , NHC(O)N(R 67 )2, NR 67 C(O)NHR 67 , N.R. 67 C(O)N(R 67 )2, C(O)NH2, C(O)NHR 67 , C(O)N(R 67 )2, C(O)NHOH, C(O)NHOR 67 , C(O)NHSO2R 67 , C(O)NR 67 SO2R 67 , SO2NH2, SO2NHR 67 , SO2N(R 67 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 67 , C(N)N(R 67 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br, or I substituent substituted alkyl, alkenyl, or alkynyl; R 67 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 57A , R 58 , R 59 , R 60 , R 63 , R 64 , R 65 and R 67 The cyclic moiety represented by the formula (I) is unsubstituted or is substituted with 1 or 2 or 3 or 4 independently selected R 68 , OR 68 , S.R. 68 , S(O)R 68 , SO2R 68, C(O)R 68 , CO(O)R 68 ,OC(O)R 68 ,OC(O)OR 68 , NH2, NHR 68 , N(R 68 )2, NHC(O)R 68 , N.R. 68 C(O)R 68 , NHS(O)2R 68 , N.R. 68 S(O)2R 68 , NHC(O)OR 68 , N.R. 68 C(O)OR 68 , NHC(O)NH2, NHC(O)NHR 68 , NHC(O)N(R 68 )2, NR 68 C(O)NHR 68 is replaced by; R 60 are uncondensed or R 60A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 60A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 61 are each unsubstituted or one, two, or three independently selected R 62 , OR 62 , S.R. 62 , S(O)R 62 , SO2R 62 , C(O)R 62 , CO(O)R 62 ,OC(O)R 62 ,OC(O)OR 62 , NH2, NHR 62 , N(R 62 )2, NHC(O)R 62 , N.R. 62 C(O)R 62 , NHS(O)2R 62 , N.R. 62 S(O)2R 62 , NHC(O)OR 62 , N.R. 62 C(O)OR 62, NHC(O)NH2, NHC(O)NHR 62 , NHC(O)N(R 62 )2, NR 62 C(O)NHR 62 , N.R. 62 C(O)N(R 62 )2, C(O)NH2, C(O)NHR 62 , C(O)N(R 62 )2, C(O)NHOH, C(O)NHOR 62 , C(O)NHSO2R 62 , C(O)NR 62 SO2R 62 , SO2NH2, SO2NHR 62 , SO2N(R 62 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 62 , C(N)N(R 62 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 62 is R 63 , R 64 , R 65 or R 66 and; R 63 is not condensed or R 63A is a phenyl fused to R 63A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 64 is not condensed or R 64A is a heteroaryl fused to R 64A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 65 are uncondensed or R 65A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 65Ais benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 66 are each unsubstituted or one, two, or three independently selected R 67 , OR 67 , S.R. 67 , S(O)R 67 , SO2R 67 , C(O)R 67 , CO(O)R 67 ,OC(O)R 67 ,OC(O)OR 67 , NH2, NHR 67 , N(R 67 )2, NHC(O)R 67 , N.R. 67 C(O)R 67 , NHS(O)2R 67 , N.R. 67 S(O)2R 67 , NHC(O)OR 67 , N.R. 67 C(O)OR 67 , NHC(O)NH2, NHC(O)NHR 67 , NHC(O)N(R 67 )2, NR 67 C(O)NHR 67 , N.R. 67 C(O)N(R 67 )2, C(O)NH2, C(O)NHR 67 , C(O)N(R 67 )2, C(O)NHOH, C(O)NHOR 67 , C(O)NHSO2R 67 , C(O)NR 67 SO2R 67 , SO2NH2, SO2NHR 67 , SO2N(R 67 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 67 , C(N)N(R 67 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br, or I substituent substituted alkyl, alkenyl, or alkynyl; R 67is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 57A , R 58 , R 59 , R 60 , R 63 , R 64 , R 65 and R 67 The cyclic moiety represented by the formula (I) is unsubstituted or is substituted with 1 or 2 or 3 or 4 independently selected R 68 , OR 68 , S.R. 68 , S(O)R 68 , SO2R 68 , C(O)R 68 , CO(O)R 68 ,OC(O)R 68 ,OC(O)OR 68 , NH2, NHR 68 , N(R 68 )2, NHC(O)R 68 , N.R. 68 C(O)R 68 , NHS(O)2R 68 , N.R. 68 S(O)2R 68 , NHC(O)OR 68 , N.R. 68 C(O)OR 68 , NHC(O)NH2, NHC(O)NHR 68 , NHC(O)N(R 68 )2, NR 68 C(O)NHR 68 , N.R. 68 C(O)N(R 68 )2, C(O)NH2, C(O)NHR 68 , C(O)N(R 68 )2, C(O)NHOH, C(O)NHOR 68 , C(O)NHSO2R 68 , C(O)NR 68 SO2R 68 , SO2NH2, SO2NHR 68 , SO2N(R 68 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 68, C(N)N(R 68 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I; R 68 is R 69 , R 70 , R 71 or R 72 and; R 69 is not condensed or R 69A is a phenyl fused to R 69A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 70 is uncondensed or R 70A is a heteroaryl fused to R 70A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 71 are uncondensed or R 71A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 71A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 72 are each unsubstituted or one, two, or three independently selected R 73 , OR 73 , S.R. 73 , S(O)R 73 , SO2R 73 , C(O)R 73 , CO(O)R 73 ,OC(O)R 73 ,OC(O)OR 73 , NH2, NHR 73 , N(R 73 )2, NHC(O)R 73 , N.R. 73 C(O)R 73 , NHS(O)2R 73 , N.R. 73 S(O)2R 73, NHC(O)OR 73 , N.R. 73 C(O)OR 73 , NHC(O)NH2, NHC(O)NHR 73 , NHC(O)N(R 73 )2, NR 73 C(O)NHR 73 , N.R. 73 C(O)N(R 73 )2, C(O)NH2, C(O)NHR 73 , C(O)N(R 73 )2, C(O)NHOH, C(O)NHOR 73 , C(O)NHSO2R 73 , C(O)NR 73 SO2R 73 , SO2NH2, SO2NHR 73 , SO2N(R 73 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 73 , C(N)N(R 73 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 73 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 69 , R 70 and R 71 is unsubstituted or substituted with one or two or three or four independently selected NH, C(O)NH, C(O)NHOH, SONH, CF, CFCF, C(O)H, C(O)OH, C(N)NH, OH, (O), CN, N, NO, CF, CFCF, OCF, OCFCF, F, Cl, Br, or I.
[0013] Another embodiment is A 1 is N or C(A 2 ) and;A 2 is H and G 1is H.
[0014] 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3R)-tetrahydro-2H-pyran-3-ylmethyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-(2-naphthylsulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2-methoxyethyl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-({4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-(tetrahydro-2H-pyran-4-ylmethoxy)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1,4-dioxan-2-ylmethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(2,2,2-trifluoroethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(3,3,3-trifluoropropyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2S)-1,4-dioxan-2-ylmethoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; cis-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2R)-1,4-dioxan-2-ylmethoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(1,4-dioxan-2-ylmethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-{[4-(1,4-dioxan-2-ylmethoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-{[5-cyano-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-cyano-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-{[3-(aminocarbonyl)-4-(tetrahydro-2H-pyran-4-ylmethoxy)phenyl]sulfonyl}-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; cis-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-chloro-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-{[5-chloro-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-{[4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]-3-(trifluoromethyl)phenyl]sulfonyl}benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-({4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)benzamide; trans-4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(1-methylpiperidin-4-yl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 5-({[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]amino}sulfonyl)-2-(tetrahydro-2H-pyran-4-ylmethoxy)nicotinamide; N-({5-bromo-6-[(1-methylpiperidin-4-yl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-methylpiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-cyano-6-(1,4-dioxan-2-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-{[5-bromo-6-(1,4-dioxan-2-ylmethoxy)pyridin-3-yl]sulfonyl}-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2,2-dimethyltetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-5-cyano-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({4-[(1-acetylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({2-chloro-5-fluoro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(3-morpholin-4-ylpropyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-cyano-6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-cyano-6-(2-morpholin-4-ylethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[2-(2-methoxyethoxy)ethyl]sulfonyl}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[2-(2-methoxyethoxy)ethyl]sulfonyl}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)oxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-bromo-6-[(1-tetrahydro-2H-pyran-4-ylpiperidin-4-yl)amino]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2-cyanoethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; cis-4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-N-{[4-({4-[bis(cyclopropylmethyl)amino]cyclohexyl}amino)-3-nitrophenyl]sulfonyl}-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1-methylpiperidin-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(morpholin-3-ylmethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(4-methylpiperazin-1-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylbut-2-ynyl)oxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-ethynyl-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-oxo-3,4-dihydroquinazolin-6-yl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[8-(4-chlorophenyl)spiro[4.5]dec-7-en-7-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; cis-4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[8-(4-chlorophenyl)spiro[4.5]dec-7-en-7-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[8-(4-chlorophenyl)spiro[4.5]dec-7-en-7-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-cyano-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; tert-butyl 3-{[4-({[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]amino}sulfonyl)-2-nitrophenoxy]methyl}morpholine-4-carboxylate; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-(morpholin-3-ylmethoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[8-(4-chlorophenyl)spiro[4.5]dec-7-en-7-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[1-(methylsulfonyl)piperidin-4-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1,1-dioxidetetrahydro-2H-thiopyran-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-chloro-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[1-(2,2,2-trifluoroethyl)piperidin-4-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-cyano-6-[(1-tetrahydro-2H-pyran-4-ylpiperidin-4-yl)oxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-isopropyl-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-5-fluoro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; and therapeutically acceptable salts and metabolites thereof.
[0015] 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({1-[2-fluoro-1-(fluoromethyl)ethyl]piperidin-4-yl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[1-(2,2-difluoroethyl)piperidin-4-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-cyclopropylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1-morpholin-4-ylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-(dicyclopropylamino)cyclohexyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-6,6-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-bromo-6-[(4-ethylmorpholin-3-yl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-ethylmorpholin-3-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(4-tetrahydro-2H-pyran-4-ylmorpholin-3-yl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-1-tetrahydro-2H-pyran-4-ylpiperidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-cyano-6-[(tetrahydro-2H-pyran-4-ylmethyl)amino]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1,1-dioxidothiomorpholin-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(4-aminotetrahydro-2H-pyran-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-cyano-6-[(4-morpholin-4-ylcyclohexyl)amino]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-cyano-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1S,3R)-3-morpholin-4-ylcyclopentyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1R,3S)-3-morpholin-4-ylcyclopentyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(morpholin-2-ylmethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydrofuran-3-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({1-[cis-3-fluorotetrahydro-2H-pyran-4-yl]piperidin-4-yl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-tetrahydro-2H-pyran-4-ylazetidin-3-yl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-tetrahydrofuran-3-ylazetidin-3-yl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3R)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4- [(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)-N-(4-((trans-4-hydroxycyclohexyl)methoxy)-3-nitrophenylsulfonyl)benzamide; 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)-N-(4-((cis-4-methoxycyclohexyl)methoxy)-3-nitrophenylsulfonyl)benzamide; cis-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-(cyclopropylamino)cyclohexyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[4-(tetrahydro-2H-pyran-4-ylamino)cyclohexyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-N-({5-bromo-6-[(4-morpholin-4-ylcyclohexyl)oxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methoxycyclohexyl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; tert-butyl 4-{[4-({[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]amino}sulfonyl)-2-nitrophenoxy]methyl}-4-fluoropiperidine-1-carboxylate; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluoropiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[4-(4-tetrahydro-2H-pyran-4-ylpiperazin-1-yl)cyclohexyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({1-[2-fluoro-1-(fluoromethyl)ethyl]piperidin-4-yl}methoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3R)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(2,2-dimethyltetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3S)-1-(2,2-dimethyltetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methylmorpholin-2-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(2-methoxyethyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(4-acetylmorpholin-2-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[trans-4-(fluoromethyl)-1-oxetan-3-ylpyrrolidin-3-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-oxetan-3-ylpiperidin-4-yl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-cyclobutylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[1-(2,2-dimethyltetrahydro-2H-pyran-4-yl)piperidin-4-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3S)-1-cyclopropylpyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-tetrahydrofuran-3-ylpiperidin-4-yl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-cyclopropylpyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3S)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(3-hydroxy-2,2-dimethylpropyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[1-(methylsulfonyl)piperidin-3-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(1-acetylpiperidin-3-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(methylsulfonyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-3,3-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({1-[2-fluoro-1-(fluoromethyl)ethyl]azetidin-3-yl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[1-(methylsulfonyl)pyrrolidin-3-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(1-acetylpyrrolidin-3-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(3R)-1-acetylpyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(3-methoxy-2,2-dimethylpropyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(1R,3R)-3-hydroxycyclopentyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(1S,3S)-3-hydroxycyclopentyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(1S,3R)-3-hydroxycyclopentyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(1R,3S)-3-hydroxycyclopentyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-2-oxopiperidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[({1-[2-fluoro-1-(fluoromethyl)ethyl]azetidin-3-yl}methyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(1-oxetan-3-ylazetidin-3-yl)methyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(1-oxetan-3-ylpiperidin-4-yl)methyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1-cyclopropylpiperidin-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(2-fluoroethyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(2,2-difluoroethyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluoro-1-oxetan-3-ylpiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(2S)-4,4-difluoro-1-oxetan-3-ylpyrrolidin-2-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(4-tetrahydro-2H-pyran-4-ylmorpholin-3-yl)methyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-cyclobutylmorpholin-3-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(4-tetrahydrofuran-3-ylmorpholin-3-yl)methyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[({1-[2-fluoro-1-(fluoromethyl)ethyl]piperidin-4-yl}methyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-cyclopropyl-4-fluoropiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methoxybenzyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[3-(trifluoromethoxy)benzyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(3-methoxybenzyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-(difluoromethoxy)benzyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-(1,4-dioxaspiro[4.5]dec-8-ylamino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-N-[(4-{[4-(acetylamino)cyclohexyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(2,2-difluoroethyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3S)-1-(2-fluoroethyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3S)-1-(2,2-difluoroethyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(2-fluoroethyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-1-oxetan-3-ylpyrrolidin-3-yl]methoxy}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-hydroxybenzyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(3-hydroxybenzyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[3-(difluoromethoxy)benzyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[cis-3-morpholin-4-ylcyclopentyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({4-[(methylsulfonyl)amino]cyclohexyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-cyclopropylpiperidin-4-yl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-oxetan-3-ylpiperidin-4-yl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluoro-1-tetrahydro-2H-pyran-4-ylpiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluoro-1-tetrahydrofuran-3-ylpiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-fluoro-1-(methylsulfonyl)piperidin-4-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3R)-1-oxetan-3-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-hydroxycyclohexyl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({4-[3-(dimethylamino)propoxy]benzyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-(2-morpholin-4-ylethoxy)benzyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(E)-4-hydroxy-1-adamantyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(Z)-4-hydroxy-1-adamantyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({4-[(1S,4S)-bicyclo[2.2.1]hept-5-en-2-ylmethoxy]-3-nitrophenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-methyl-5-oxopyrrolidin-3-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1R,4R,5R,6S)-5,6-dihydroxybicyclo[2.2.1]hept-2-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1R,4R,5S,6R)-5,6-dihydroxybicyclo[2.2.1]hept-2-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(3-oxocyclohexyl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohexa-1,3-dien-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({(3R)-1-[2-fluoro-1-(fluoromethyl)ethyl]pyrrolidin-3-yl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-5-(trifluoromethyl)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3S)-1-oxetan-3-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-N-({5-chloro-6-[(4-methoxycyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; cis-N-({5-chloro-6-[(4-methoxycyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-1-oxetan-3-ylpyrrolidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[({4-[2-(2-methoxyethoxy)ethyl]morpholin-2-yl}methyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(cyanomethyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(N,N-dimethylglycyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; (2-{[(4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}-2-nitrophenyl)amino]methyl}morpholin-4-yl)acetic acid; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[4-(oxetan-3-yl)morpholin-2-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-cyclopropylmorpholin-2-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-(methylsulfonyl)-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methyltetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; Ethyl 4-(4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}-2-nitrophenyl)piperazine-1-carboxylate; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[4-(morpholin-4-yl)piperidin-1-yl]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3R)-1-(oxetan-3-yl)pyrrolidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(1,3-difluoropropan-2-yl)pyrrolidin-3-yl]amino}-3-[(trifluoromethyl)sulfonyl]phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-isopropylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({4-[(1-tert-butylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[1-(2-methoxyethyl)piperidin-3-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[1-(cyanomethyl)piperidin-3-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluoro-1-methylpiperidin-4-yl)methoxy]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(3R)-1-(1,3-difluoropropan-2-yl)pyrrolidin-3-yl]amino}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; tert-Butyl 4-[(4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}-2-nitrophenyl)amino]piperazine-1-carboxylate; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-(pentafluoro-λ 6-sulfanyl)-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methoxytetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(1,3-difluoropropan-2-yl)pyrrolidin-3-yl]oxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[4-(oxetan-3-yl)piperazin-1-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(3R)-tetrahydrofuran-3-ylamino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4,4-difluorocyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({4-[(1-tert-butylpiperidin-4-yl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-({[4-(oxetan-3-yl)morpholin-2-yl]methyl}amino)-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]amino}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(1-cyclopropylpiperidin-4-yl)amino]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(2S)-4-(cyanomethyl)morpholin-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(2S)-4-(N,N-dimethylglycyl)morpholin-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(2R)-4-(cyanomethyl)morpholin-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(2R)-4-(N,N-dimethylglycyl)morpholin-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-fluoro-6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[3-hydroxy-2-(hydroxymethyl)-2-methylpropoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(1,3-difluoropropan-2-yl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(cyanomethyl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({(3R)-1-[2-(2-methoxyethoxy)ethyl]pyrrolidin-3-yl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(N,N-dimethylglycyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[1-(oxetan-3-yl)azetidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(cyanomethyl)-4-fluoropiperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(2R)-4-(N,N-dimethylglycyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(2S)-4-(N,N-dimethylglycyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(N,N-dimethylglycyl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(3R)-1-(2,2-difluoroethyl)pyrrolidin-3-yl]oxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(cyanomethyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-{4-[(4′-chlorobiphenyl-2-yl)methyl]-4-methoxypiperidin-1-yl}-N-({5-chloro-6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-{4-[(4′-chlorobiphenyl-2-yl)methyl]-4-methoxypiperidin-1-yl}-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[9-(4-chlorophenyl)-3-(1,3-difluoropropan-2-yl)-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[9-(4-chlorophenyl)-3-isopropyl-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[9-(4-chlorophenyl)-3-(1,3-difluoropropan-2-yl)-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-N-{[5-chloro-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[9-(4-chlorophenyl)-3-isopropyl-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-N-{[5-chloro-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(4-fluoro-1-methylpiperidin-4-yl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(N,N-dimethylglycyl)-4-fluoropiperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-{4-[(4′-chlorobiphenyl-2-yl)methyl]-4-fluoropiperidin-1-yl}-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-{4-[(4′-chlorobiphenyl-2-yl)methyl]-4-fluoropiperidin-1-yl}-N-({5-chloro-6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[9-(4-chlorophenyl)-3-isopropyl-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-({4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]-3-(trifluoromethyl)phenyl}sulfonyl)benzamide; N-[(5-chloro-6-{[(3R)-1-(1,3-difluoropropan-2-yl)pyrrolidin-3-yl]oxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[2-(tetrahydrofuran-3-yloxy)ethoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-cyanocyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[4-fluoro-1-(oxetan-3-yl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-cyano-6-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-(3-furylmethoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(3R)-1-(1,3-difluoropropan-2-yl)pyrrolidin-3-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(3R)-1-(2,2-difluoroethyl)pyrrolidin-3-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(1,3-difluoropropan-2-yl)-4-fluoropiperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-4-[(4-fluoro-1-methylpiperidin-4-yl)methoxy]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-cyano-4-(tetrahydro-2H-pyran-4-ylmethoxy)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(2,2-difluoroethyl)-4-fluoropiperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(4,4-difluorocyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[6-{[1-(1,3-difluoropropan-2-yl)-4-fluoropiperidin-4-yl]methoxy}-5-(trifluoromethyl)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-chloro-6-[2-(tetrahydrofuran-2-yl)ethoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}-3-methylpiperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[3-(cyclopropylamino)propyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-{[5-chloro-6-(2-methoxyethoxy)pyridin-3-yl]sulfonyl}-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-fluoro-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[1-(methoxyacetyl)piperidin-4-yl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[1-(N,N-dimethylglycyl)piperidin-4-yl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohexyl]methyl}piperidin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-{[6-(tetrahydro-2H-pyran-4-ylmethoxy)-5-(trifluoromethyl)pyridin-3-yl]sulfonyl}benzamide; N-({5-chloro-6-[(trans-4-hydroxycyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-cyano-4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({6-[(trans-4-methoxycyclohexyl)methoxy]-5-(trifluoromethyl)pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({6-[(cis-4-methoxycyclohexyl)methoxy]-5-(trifluoromethyl)pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(4,4-difluoro-1-hydroxycyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperidin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[trans-4-(morpholin-4-yl)cyclohexyl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(1,3-thiazol-5-ylmethyl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-4-[(trans-4-hydroxycyclohexyl)methoxy]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-chloro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-(trifluoromethyl)phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(2,2,2-trifluoroethyl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[1-(oxetan-3-yl)piperidin-4-yl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3,5-difluoro-4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(oxetan-3-yl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[1-(1-methyl-L-prolyl)piperidin-4-yl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3,4-difluoro-5-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(2S)-4-cyclopropylmorpholin-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperidin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperidin-1-yl)-N-{[3-chloro-4-(tetrahydro-2H-pyran-4-ylmethoxy)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 2-{[(4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}-2-nitrophenyl)amino]methyl}morpholine-4-carboxylate; 2-{[(4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}-2-nitrophenyl)amino]methyl}-N-ethyl-N-methylmorpholine-4-carboxamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(methylsulfonyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclobutyl(cyclopropyl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-difluorocyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[4-fluoro-1-(oxetan-3-yl)piperidin-4-yl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-chloro-4-(tetrahydrofuran-3-ylmethoxy)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-difluorocyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-hydroxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]phenyl}sulfonyl)-4-(4-{[9-(4-chlorophenyl)-3-(oxetan-3-yl)-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(2R)-4-cyclopropylmorpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(2S)-4-cyclopropylmorpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[5-(4-chlorophenyl)spiro[2.5]oct-5-en-6-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-{[5-chloro-6-({4-[cyclopropyl(oxetan-3-yl)amino]cyclohexyl}methoxy)pyridin-3-yl]sulfonyl}-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[5-(4-chlorophenyl)spiro[2.5]oct-5-en-6-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-cyclopropylmorpholin-2-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-4-[(4-cyclopropylmorpholin-2-yl)methoxy]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[(4-cyclopropylmorpholin-2-yl)methyl]amino}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 2-{[(2-chloro-4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}phenyl)amino]methyl}-N-ethyl-N-methylmorpholine-4-carboxamide; (2S)-2-{[(3-chloro-5-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}pyridin-2-yl)oxy]methyl}-N-ethyl-N-methylmorpholine-4-carboxamide; N-[(5-chloro-6-{[(4-cyclopropylmorpholin-2-yl)methyl]amino}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 2-{[(3-chloro-5-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}pyridin-2-yl)amino]methyl}-N-ethyl-N-methylmorpholine-4-carboxamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(cis-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(1R,2R,4R,5R)-5-hydroxy-5-methylbicyclo[2.2.1]hept-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({4-[(2-cyanoethyl)(cyclopropyl)amino]cyclohexyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(trans-4-hydroxy-4-methylcyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[5-(4-chlorophenyl)spiro[2.5]oct-5-en-6-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-chloro-6-(5,6,7,8-tetrahydroimidazo[1,2-a]pyridin-6-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(1R,2S,4R,5R)-5-hydroxy-5-methylbicyclo[2.2.1]hept-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(cis-4-hydroxy-4-methylcyclohexyl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[4-fluoro-1-(oxetan-3-yl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[5-(4-chlorophenyl)spiro[2.5]oct-5-en-6-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-(3,3-difluoropyrrolidin-1-yl)cyclohexyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(trans-4-hydroxy-4-methylcyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(cis-4-hydroxy-4-methylcyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({4-[(2,2-difluorocyclopropyl)amino]cyclohexyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(cis-1-fluoro-4-hydroxycyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-(2-oxaspiro[3.5]non-7-ylmethoxy)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(trans-4-hydroxy-4-methylcyclohexyl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-bis(fluoromethyl)cyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-cyclopropylmorpholin-2-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(trans-1-fluoro-4-hydroxy-4-methylcyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(cis-1-fluoro-4-hydroxy-4-methylcyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-cyano-4-{[4-fluoro-1-(oxetan-3-yl)piperidin-4-yl]methoxy}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-ethyl-4-hydroxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(cis-4-ethyl-4-hydroxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5-(methoxymethyl)-5-methylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(2S)-4-(oxetan-3-yl)morpholin-2-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-4-[(trans-4-hydroxy-4-methylcyclohexyl)methoxy]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({4-[(2-cyanoethyl)(cyclopropyl)amino]-1-fluorocyclohexyl}methoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-nitro-6-[(tetrahydro-2H-pyran-4-ylmethyl)amino]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(2-oxaspiro[3.5]non-7-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-cyano-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; Pivalic acid {[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)amino}methyl; butyrate {[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)amino}methyl; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-{[3-(tetrahydro-2H-pyran-4-ylmethyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-6-yl]sulfonyl}benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(6-{[(trans-4-hydroxy-4-methylcyclohexyl)methyl]amino}-5-nitropyridin-3-yl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(5-cyano-6-{[4-fluoro-1-(oxetan-3-yl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-(4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}-2-nitrophenyl)morpholine-4-carboxamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(methoxymethyl)cyclohexyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(5-chloro-6-{[1-(1,3-thiazol-2-yl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(6-{[(cis-4-hydroxy-4-methylcyclohexyl)methyl]amino}-5-nitropyridin-3-yl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5-methoxy-5-methylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5-methoxy-5-methylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; and therapeutically acceptable salts and metabolites thereof.
[0016] Another embodiment relates to the compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharmaceutically acceptable salt thereof.
[0017] Another embodiment relates to the compound trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharmaceutically acceptable salt thereof.
[0018] Another embodiment relates to the compound cis-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharmaceutically acceptable salt thereof.
[0019] Another embodiment relates to the compound trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharmaceutically acceptable salt thereof.
[0020] Another embodiment relates to the compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharmaceutically acceptable salt thereof.
[0021] Another embodiment relates to the compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharmaceutically acceptable salt thereof.
[0022] Another embodiment relates to the compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(cis-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharmaceutically acceptable salt thereof.
[0023] Another embodiment relates to the compound N-[(5-chloro-6-{[4-fluoro-1-(oxetan-3-yl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharmaceutically acceptable salt thereof.
[0024] Another embodiment relates to the compound N-({5-bromo-6-[(1-tetrahydro-2H-pyran-4-ylpiperidin-4-yl)amino]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharmaceutically acceptable salt thereof.
[0025] Another embodiment relates to the compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(methylsulfonyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharmaceutically acceptable salt thereof.
[0026] Another embodiment relates to the compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(oxetan-3-yl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharmaceutically acceptable salt thereof.
[0027] Another embodiment relates to the compound 4-(4-{[2-(4-chlorophenyl)-5-methoxy-5-methylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; or a pharmaceutically acceptable salt thereof.
[0028] Yet another embodiment is 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(methylsulfonyl)pyrrolidine-3- or a pharmaceutically acceptable salt thereof.
[0029] Yet another embodiment is N-[(5-chloro-6-{[1-(cyanomethyl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl )-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(oxetan-3-yl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharmaceutically acceptable salt thereof.
[0030] Yet another embodiment is 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; ... or a pharmaceutically acceptable salt thereof.
[0031] Another embodiment relates to the compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(oxetan-3-yl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; or a pharmaceutically acceptable salt thereof.
[0032] Yet another embodiment is 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3R)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[ The present invention relates to a compound having formula (I) or (II) which is 2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methylmorpholin-2-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide, or a pharmaceutically acceptable salt thereof.
[0033] Yet another embodiment comprises: 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-tetrahydro-2H-pyran-3-ylmethyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-(1,4-dioxan-2-ylmethoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-bromo-6-[(1-tetrahydro-2H-pyran-4-ylpiperidin-4-yl)amino]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(4-aminotetrahydro-2H-pyran-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3R)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methylmorpholin-2-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(methylsulfonyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methoxytetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(cyanomethyl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(oxetan-3-yl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(1R,2S,4R,5R)-5-hydroxy-5-methylbicyclo[2.2.1]hept-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(6-{[(cis-4-hydroxy-4-methylcyclohexyl)methyl]amino}-5-nitropyridin-3-yl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; The present invention relates to a compound having formula (I) or (II) which is 4-(4-{[2-(4-chlorophenyl)-5-methoxy-5-methylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide, or a pharmaceutically acceptable salt thereof.
[0034] Another embodiment relates to the compound N-[(5-chloro-6-{[1-(cyanomethyl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; or a pharmaceutically acceptable salt thereof.
[0035] Yet another embodiment is N-[(4-{[(4-aminotetrahydro-2H-pyran-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; or a pharmaceutically acceptable salt thereof.
[0036] Another embodiment relates to the compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methoxytetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharmaceutically acceptable salt thereof.
[0037] Another embodiment relates to a composition for treating bladder cancer, brain cancer, breast cancer, bone marrow cancer, cervical cancer, chronic lymphocytic leukemia, colorectal cancer, esophageal cancer, hepatocellular carcinoma, lymphoblastic leukemia, follicular lymphoma, lymphoid malignancies of T-cell or B-cell origin, melanoma, myeloid leukemia, myeloma, oral cancer, ovarian cancer, non-small cell lung cancer, chronic lymphocytic leukemia, myeloma, prostate cancer, small cell lung cancer, or splenic cancer, comprising an excipient and a therapeutically effective amount of a compound of Formula (I) or Formula (II).
[0038] Another embodiment relates to a method of treating bladder cancer, brain cancer, breast cancer, bone marrow cancer, cervical cancer, chronic lymphocytic leukemia, colorectal cancer, esophageal cancer, hepatocellular carcinoma, lymphoblastic leukemia, follicular lymphoma, lymphoid malignancies of T-cell or B-cell origin, melanoma, myeloid leukemia, myeloma, oral cancer, ovarian cancer, non-small cell lung cancer, chronic lymphocytic leukemia, myeloma, prostate cancer, small cell lung cancer, or splenic cancer in a patient, comprising administering to the patient a therapeutically effective amount of a compound of Formula (I) or Formula (II).
[0039] Another embodiment relates to a method of treating bladder cancer, brain cancer, breast cancer, bone marrow cancer, cervical cancer, chronic lymphocytic leukemia, colorectal cancer, esophageal cancer, hepatocellular carcinoma, lymphoblastic leukemia, follicular lymphoma, lymphoid malignancies of T-cell or B-cell origin, melanoma, myeloid leukemia, myeloma, oral cancer, ovarian cancer, non-small cell lung cancer, chronic lymphocytic leukemia, myeloma, prostate cancer, small cell lung cancer, or splenic cancer in a patient, comprising administering to the patient a therapeutically effective amount of a compound of Formula (I) or Formula (II) and therapeutically effective amounts of one or more additional therapeutic agents. DETAILED DESCRIPTION OF THE INVENTION
[0040] Detailed Description of the Invention Variables herein are designated and can be embodied by identifiers (capital letters with superscript numbers and / or superscript letters).
[0041] It is understood that proper valency is maintained in all moieties and combinations herein, with monovalent moieties having multiple atoms being depicted left to right and attached at the left end, and divalent moieties also being depicted left to right.
[0042] It is also clear that a specific embodiment of a variable moiety herein may be the same or different from another specific embodiment having the same identifying expression.
[0043] The term "alkenyl" as used herein means a straight or branched hydrocarbon chain containing from 2 to 10 carbons and containing at least one carbon-carbon double bond. x -C y The term "alkenyl" means a straight or branched hydrocarbon chain containing x to y carbon atoms and having at least one carbon-carbon double bond. The term "C3-C6 alkenyl" means an alkenyl group containing from 3 to 6 carbon atoms. Representative examples of alkenyl include, but are not limited to, buta-2,3-dienyl, ethenyl, 2-propenyl, 2-methyl-2-propenyl, 3-butenyl, 4-pentenyl, 5-hexenyl, 2-heptenyl, 2-methyl-1-heptenyl, and 3-decenyl.
[0044] The term "alkenylene" means a divalent group derived from a straight or branched chain hydrocarbon of from 2 to 4 carbon atoms and containing at least one carbon-carbon double bond. x -C yThe term "alkenylene" means a divalent group derived from a straight or branched hydrocarbon chain containing at least one carbon-carbon double bond and containing from x to y carbon atoms. Representative examples of alkenylene include, but are not limited to, -CH=CH- and -CHCH=CH-.
[0045] The term "alkyl" as used herein means a straight or branched saturated hydrocarbon chain containing from 1 to 10 carbon atoms. x -C y The term "alkyl" means a straight or branched chain saturated hydrocarbon containing from x to y carbon atoms. For example, "C1-C6 alkyl" means a straight or branched chain saturated hydrocarbon containing from 2 to 6 carbon atoms. Representative examples of alkyl include, but are not limited to, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, n-hexyl, 3-methylhexyl, 2,2-dimethylpentyl, 2,3-dimethylpentyl, n-heptyl, n-octyl, n-nonyl, and n-decyl.
[0046] The term "alkylene" means a divalent group derived from a straight or branched saturated hydrocarbon chain of 1 to 10 carbon atoms, for example, 1 to 4 carbon atoms. x -C y "Alkylene" means a divalent group derived from a straight or branched chain saturated hydrocarbon containing from x to y carbon atoms. For example, "C2-C6 alkylene" means a straight or branched chain saturated hydrocarbon containing from 2 to 6 carbon atoms. Representative examples of alkylene include, but are not limited to, -CH2-, -CH2CH2-, -CH2CH2CH2-, -CH2CH2CH2CH2-, and -CH2CH(CH3)CH2-.
[0047] The term "alkynyl" as used herein means a straight or branched chain hydrocarbon group containing from 2 to 10 carbon atoms and containing at least one carbon-carbon triple bond.x -C y The term "alkynyl" refers to a straight or branched chain hydrocarbon group containing from x to y carbon atoms. For example, "C3-C6 alkynyl" refers to a straight or branched chain hydrocarbon group containing from 3 to 6 carbon atoms and containing at least one carbon-carbon triple bond. Representative examples of alkynyl include, but are not limited to, acetylenyl, 1-propynyl, 2-propynyl, 3-butynyl, 2-pentynyl, and 1-butynyl.
[0048] The term "alkynylene," as used herein, means a divalent group derived from a straight or branched chain hydrocarbon group containing from 2 to 10 carbon atoms and containing at least one carbon-carbon triple bond.
[0049] The term "aryl" as used herein means phenyl.
[0050] The term "cyclic moiety," as used herein, means benzene, phenyl, phenylene, cycloalkane, cycloalkyl, cycloalkylene, cycloalkene, cycloalkenyl, cycloalkenylene, cycloalkyne, cycloalkynyl, cycloalkynylene, heteroarene, heteroaryl, heterocycloalkane, heterocycloalkyl, heterocycloalkene, heterocycloalkenyl, and spiroalkyl.
[0051] As used herein, the terms "cycloalkylene" or "cycloalkyl" or "cycloalkane" refer to a monocyclic or bridged hydrocarbon ring system. A monocyclic cycloalkyl is a carbocyclic ring system containing 3 to 10 carbon atoms, 0 heteroatoms, and 0 double bonds. Examples of monocyclic ring systems include cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, and cyclooctyl. A monocyclic ring can contain one or two alkylene bridges, each consisting of 1, 2, or 3 carbon atoms, respectively, connecting two non-adjacent carbon atoms of the ring system. Representative examples of such bridged cycloalkyl ring systems include bicyclo[3.1.1]heptane, bicyclo[2.2.1]heptane, bicyclo[2.2.2]octane, bicyclo[3.2.2]nonane, bicyclo[3.3.1]nonane, bicyclo[4.2.1]nonane, tricyclo[3.3.1.0]nonane, and tricyclo[3.3.1.0]nonane. 3,7 ]nonane (octahydro-2,5-methanopentalene or noradamantane) and tricyclo[3.3.1.1 3,7 ]decane (adamantane), etc. Monocyclic and bridged cycloalkyls can be attached to the parent molecular moiety through any substitutable atom contained within the ring system.
[0052] As used herein, the term "cycloalkenylene" or "cycloalkenyl" or "cycloalkene" refers to a monocyclic or bridged hydrocarbon ring system. Monocyclic cycloalkenyls have 4 to 10 carbon atoms and zero heteroatoms. A 4-membered ring system has one double bond, a 5- or 6-membered ring system has one or two double bonds, a 7- or 8-membered ring system has one, two, or three double bonds, and a 9- or 10-membered ring has one, two, three, or four double bonds. Representative examples of monocyclic cycloalkenyl groups include, but are not limited to, cyclobutenyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, and cyclooctenyl. A monocyclic cycloalkenyl ring can contain one or two alkylene bridges, each consisting of one, two, or three carbon atoms, connecting two non-adjacent carbon atoms of the ring system. Representative examples of bridged cycloalkenyl groups include, but are not limited to, 4,5,6,7-tetrahydro-3aH-indene, octahydronaphthalenyl, and 1,6-dihydro-pentalene. Monocyclic and bridged cycloalkenyls can be attached to the parent molecular moiety through any substitutable atom contained within the ring system.
[0053] As used herein, the term "cycloalkyne" or "cycloalkynyl" or "cycloalkynylene" refers to a monocyclic or bridged hydrocarbon ring system. A monocyclic cycloalkynyl has 8 or more carbon atoms, 0 heteroatoms, and 1 or more triple bonds. A monocyclic cycloalkynyl ring can contain one or two alkylene bridges, each consisting of 1, 2, or 3 carbon atoms, connecting two non-adjacent carbon atoms of the ring system. A monocyclic or bridged cycloalkynyl can be attached to the parent molecular moiety through any substitutable atom contained within the ring system.
[0054] As used herein, the term "heteroarene" or "heteroaryl" or "heteroarylene" refers to a 5- or 6-membered aromatic ring having at least one carbon atom and one or more independently selected nitrogen, oxygen, or sulfur atoms. The heteroarenes of the present invention are connected through any adjacent atom in the ring, provided that appropriate valence is maintained. Representative examples of heteroaryl include, but are not limited to, furanyl (including but not limited to furan-2-yl), imidazolyl (including but not limited to 1H-imidazol-1-yl), isoxazolyl, isothiazolyl, oxadiazolyl, 1,3-oxazolyl, pyridinyl (e.g., pyridin-4-yl, pyridin-2-yl, pyridin-3-yl), pyridazinyl, pyrimidinyl, pyrazinyl, pyrazolyl, pyrrolyl, tetrazolyl, thiadiazolyl, 1,3-thiazolyl, thienyl (including but not limited to thien-2-yl, thien-3-yl), triazolyl, and triazinyl.
[0055] The term "heterocycloalkane" or "heterocycloalkyl" or "heterocycloalkylene," as used herein, refers to a monocyclic or bridged 3-, 4-, 5-, 6-, 7-, or 8-membered ring containing at least one heteroatom independently selected from the group consisting of O, N, and S, and zero double bonds. Monocyclic and bridged heterocyclic alkanes are connected to the parent molecular moiety through any substitutable carbon atom or any substitutable nitrogen atom contained within the ring. The nitrogen and sulfur heteroatoms in the heterocycle may be optionally oxidized, and the nitrogen atom may be optionally quaternized. Representative examples of heterocyclic alkane groups include, but are not limited to, morpholinyl, tetrahydropyranyl, pyrrolidinyl, piperidinyl, dioxolanyl, tetrahydrofuranyl, thiomorpholinyl, 1,4-dioxanyl, tetrahydrothienyl, tetrahydrothiopyranyl, oxetanyl, piperazinyl, imidazolidinyl, azetidine, azepanyl, aziridinyl, diazepanyl, dithiolanyl, dithianyl, isoxazolidinyl, isothiazolidinyl, oxadiazolidinyl, oxazolidinyl, pyrazolidinyl, tetrahydrothienyl, thiadiazolidinyl, thiazolidinyl, thiomorpholinyl, trithianyl, and trithianyl.
[0056] The terms "heterocyclic alkene" or "heterocyclic alkenyl" or "heterocyclic alkenylene," as used herein, refer to a monocyclic or bridged 3-, 4-, 5-, 6-, 7-, or 8-membered ring containing at least one heteroatom independently selected from the group consisting of O, N, and S, and one or more double bonds. Monocyclic and bridged heterocyclic alkenes are connected to the parent molecular moiety through any substitutable carbon atom or any substitutable nitrogen atom contained within the ring. The nitrogen and sulfur heteroatoms in the heterocycle may be optionally oxidized, and the nitrogen atom may be optionally quaternized. Representative examples of heterocyclic alkene groups include, but are not limited to, 1,4,5,6-tetrahydropyridazinyl, 1,2,3,6-tetrahydropyridinyl, dihydropyranyl, imidazolinyl, isothiazolinyl, oxadiazolinyl, isoxazolinyl, oxazolinyl, pyranyl, pyrazolinyl, pyrrolinyl, thiadiazolinyl, thiazolinyl, and thiopyranyl.
[0057] As used herein, the term "phenyl" refers to a monovalent group formed by removal of a hydrogen atom from benzene.
[0058] As used herein, the term "phenylene" refers to a divalent group formed by removal of a hydrogen atom from a phenyl.
[0059] The term "spiroalkyl" as used herein means an alkylene group bonded to the same carbon atom at both ends, examples being C2-spiroalkyl, C3-spiroalkyl, C4-spiroalkyl, C5-spiroalkyl, C6-spiroalkyl, C7-spiroalkyl, C8-spiroalkyl, and C9-spiroalkyl.
[0060] As used herein, the term "spiroheteroalkyl" refers to a spiroalkyl having one or two CH moieties replaced by independently selected O, C(O), CNOH, CNOCH, S, S(O), SO, or NH and one or two CH moieties that are unreplaced or replaced by N.
[0061] The term "spiroheteroalkenyl," as used herein, means a spiroalkenyl having one or two CH moieties replaced by independently selected O, C(O), CNOH, CNOCH, S, S(O), SO, or NH and one or two CH moieties that are unreplaced or replaced by N, and means a spiroalkenyl having one or two CH moieties that are unreplaced or replaced by independently selected O, C(O), CNOH, CNOCH, S, S(O), SO, or NH and one or two CH moieties that are replaced by N.
[0062] The term "C2-C5-spiroalkyl" as used herein means C2-spiroalkyl, C3-spiroalkyl, C4-spiroalkyl, and C5-spiroalkyl.
[0063] A therapeutically effective amount of a compound of formula (I) or formula (II) is administered to the patient.
[0064] Another embodiment relates to a method of treating bladder cancer, brain cancer, breast cancer, bone marrow cancer, cervical cancer, chronic lymphocytic leukemia, colorectal cancer, esophageal cancer, hepatocellular carcinoma, lymphoblastic leukemia, follicular lymphoma, lymphoid malignancies of T-cell or B-cell origin, melanoma, myeloid leukemia, myeloma, oral cancer, ovarian cancer, non-small cell lung cancer, chronic lymphocytic leukemia, myeloma, prostate cancer, small cell lung cancer, or splenic cancer in a patient, comprising administering to the patient a therapeutically effective amount of a compound of Formula (I) or Formula (II) and therapeutically effective amounts of one or more additional therapeutic agents.
[0065] Detailed Description of the Invention Variables herein are designated and can be embodied by identifiers (capital letters with superscript numbers and / or superscript letters).
[0066] It is understood that proper valency is maintained in all moieties and combinations herein, with monovalent moieties having multiple atoms being depicted left to right and attached at the left end, and divalent moieties also being depicted left to right.
[0067] It is also clear that a specific embodiment of a variable moiety herein may be the same or different from another specific embodiment having the same identifying expression.
[0068] The term "alkenyl" as used herein means a straight or branched hydrocarbon chain containing from 2 to 10 carbons and containing at least one carbon-carbon double bond. x -C yThe term "alkenyl" means a straight or branched hydrocarbon chain containing x to y carbon atoms and having at least one carbon-carbon double bond. The term "C3-C6 alkenyl" means an alkenyl group containing from 3 to 6 carbon atoms. Representative examples of alkenyl include, but are not limited to, buta-2,3-dienyl, ethenyl, 2-propenyl, 2-methyl-2-propenyl, 3-butenyl, 4-pentenyl, 5-hexenyl, 2-heptenyl, 2-methyl-1-heptenyl, and 3-decenyl.
[0069] The term "alkenylene" means a divalent group derived from a straight or branched chain hydrocarbon of from 2 to 4 carbon atoms and containing at least one carbon-carbon double bond. x -C y The term "alkylene" refers to the divalent groups methoxymethyl, methoxyethoxymethyl, 2-(trimethylsilyl)ethoxymethyl, benzyloxymethyl, methylthiomethyl, 2-methylthioethyl, phenylthiomethyl, 1,1-dimethyl-2-propenyl, 3-methyl-3-butenyl, allyl, trimethylsilyl, triethylsilyl, triisopropylsilyl, diethylisopropylsilyl, tert-butyldimethylsilyl, tert-butyldiphenylsilyl, diphenylmethylsilyl, and tert-butylmethoxyphenylsilyl, which contain at least one carbon-carbon double bond and are derived from a straight or branched hydrocarbon chain containing x through y.
[0070] As used herein, the term "OH or SH protecting group" means any of benzyloxycarbonyl, 4-nitrobenzyloxycarbonyl, 4-bromobenzyloxycarbonyl, 4-methoxybenzyloxycarbonyl, 3,4-dimethoxybenzyloxycarbonyl, methoxycarbonyl, ethoxycarbonyl, tert-butoxycarbonyl, 1,1-dimethylpropoxycarbonyl, isopropoxycarbonyl, isobutyloxycarbonyl, diphenylmethoxycarbonyl, 2,2,2-trichloroethoxy ... oxycarbonyl, 2,2,2-tribromoethoxycarbonyl, 2-(trimethylsilyl)ethoxycarbonyl, 2-(phenylsulfonyl)ethoxycarbonyl, 2-(triphenylphosphonio)ethoxycarbonyl, 2-furfuryloxycarbonyl, 1-adamantyloxycarbonyl, vinyloxycarbonyl, allyloxycarbonyl, S-benzylthiocarbonyl, 4-ethoxy-1-naphthyloxycarbonyl, 8-quinolyloxycarbonyl, acetyl, formyl, chloroacetyl, dichloro
[0033] Means paraacetyl, trichloroacetyl, trifluoroacetyl, methoxyacetyl, phenoxyacetyl, pivaloyl, benzoyl, methyl, tert-butyl, 2,2,2-trichloroethyl, 2-trimethylsilylethyl, 1,1-dimethyl-2-propenyl, 3-methyl-3-butenyl, allyl, benzyl (phenylmethyl), para-methoxybenzyl, 3,4-dimethoxybenzyl, diphenylmethyl, triphenylmethyl, tetrahydrofuryl, tetrahydropyranyl, tetrahydrothiopyranyl, methoxymethyl, methylthiomethyl, benzyloxymethyl, 2-methoxyethoxymethyl, 2,2,2-trichloroethoxymethyl, 2-(trimethylsilyl)ethoxymethyl, 1-ethoxyethyl, methanesulfonyl, para-toluenesulfonyl, trimethylsilyl, triethylsilyl, triisopropylsilyl, diethylisopropylsilyl, tert-butyldimethylsilyl, tert-butyldiphenylsilyl, diphenylmethylsilyl and tert-butylmethoxyphenylsilyl.
[0071] compound Geometric isomers of the compounds of the present invention may exist. The compounds of the present invention may contain carbon-carbon or carbon-nitrogen double bonds in the E or Z configuration, where the term "E" denotes two relatively more prominent substituents on opposite sides of the carbon-carbon or carbon-nitrogen double bond, and the term "Z" denotes two relatively more prominent substituents on the same side of the carbon-carbon or carbon-nitrogen double bond, as determined by the Cahn-Ingold-Prelog precedence rules. The compounds of the present invention may also exist as a mixture of "E" and "Z" isomers. Substituents around a cycloalkyl or heterocycloalkyl are designated as being in the cis or trans configuration. The present invention also contemplates various isomers and mixtures thereof resulting from the arrangement of substituents around the adamantane ring system. Two substituents around a single ring within the adamantane ring system are designated as being in the Z or E relative configuration. See, for example, CD Jones, M. Kaselj, RN Salvatore, WJ le Noble J. Org. Chem. 1998, 63, 2758-2760.
[0072] The compounds of the present invention can contain asymmetrically substituted carbon atoms in the R or S configuration, where the terms "R" and "S" are as defined by IUPAC 1974 Recommendations for Section E, Fundamental Stereochemistry, Pure Appl. Chem. (1976) 45, 13-10. Compounds with asymmetrically substituted carbon atoms in equal amounts of R and S configuration are racemic at those carbon atoms. Atoms in which one configuration is in excess over the other are assigned to the configuration that is present in the greater amount, preferably about 85% to 90% excess, more preferably about 95% to 99% excess, and even more preferably greater than about 99% excess. Thus, the present invention includes racemic mixtures, relative and absolute stereoisomers, and mixtures of relative and absolute stereoisomers.
[0073] Isotopically enriched or labeled compounds The compounds of the present invention can exist in isotopically labeled or isotopically enriched forms containing one or more atoms having an atomic mass or mass number different from the atomic mass or mass number most abundantly found in nature. The isotopes can be radioactive or non-radioactive. Isotopes of atoms such as hydrogen, carbon, phosphorus, sulfur, fluorine, chlorine, and iodine include: 2 H, 3 H, 13 C. 14 C. 15 N, 18 O. 32 P, 35 S, 18 F, 36 Cl and 125 These include, but are not limited to, I. Compounds that contain other isotopes of these atoms and / or other atoms are within the scope of this invention.
[0074] In another embodiment, the isotope-labeled compound is deuterium ( 2 H), tritium ( 3 H) or 14The isotopically labeled compounds of the present invention include a C isotope. The isotopically labeled compounds of the present invention can be prepared by general methods known to those skilled in the art. Such isotopically labeled compounds can be readily prepared by carrying out the procedures disclosed in the examples and schemes disclosed herein, substituting a readily available isotopically labeled reagent for the unlabeled reagent. Optionally, a compound can be treated with an isotopically labeled reagent to exchange a normal atom for its isotope. For example, hydrogen can be exchanged for deuterium by the action of a deuterated acid such as D2SO4 / D2O. In addition to the above, relevant procedures and intermediates can be found, for example, in Lizondo, J et al., Drugs Fut, 21(11), 1116(1996); Brickner, SJ et al., J Med Chem, 39(3), 673(1996); Mallesham, B et al., Org Lett, 5(7), 963 (2003); PCT Publication Nos. WO1997010223, WO2005099353, WO1995007271, WO2006008754; U.S. Patent Nos. 7,538,189; 7,534,814; 7,531,685; 7,528,131; 7,521,421; 7,514,068; 7,511,013; and U.S. Patent Application Publication Nos. 20090137457; 20090 Nos. 131485; 20090131363; 20090118238; 20090111840; 20090105338; 20090105307; 20090105147; 20090093422; 20090088416; and 20090082471 (these methods are incorporated herein by reference).
[0075] The isotopically labeled compounds of the present invention can be used as standards to determine the efficacy of Bcl-2 inhibitors in binding assays. Isotopically labeled compounds have been used in pharmaceutical research to determine the in vivo metabolic fate of a compound by evaluating its mechanism of action and metabolic pathway with the non-isotopically labeled parent compound (Blake et al. J. Pharm. Sci. 64, 3, 367-391(1975)). Such metabolic studies are important in the design of safe and effective therapeutic agents, either because in vivo active compounds are administered to patients or because metabolites produced from the parent compound are identified as toxic or carcinogenic (Foster et al., Advances in Drug Research Vol. 14, pp. 2-36, Academic Press, London, 1985; Kato et al., J. Labeled Comp. Radiopharmaceut., 36(10):927-932 (1995); Kushner et al., Can. J. Physiol. Pharmacol., 77, 79-88 (1999)).
[0076] Additionally, drugs containing non-radioactive isotopes, such as deuterated drugs, referred to as "heavy drugs," can be used to treat diseases and conditions associated with Bcl-2 activity. Increasing the amount of isotope present in the compound is referred to as enrichment. Examples of enrichment amounts include about 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16, 21, 25, 29, 33, 37, 42, 46, 50, 54, 58, 63, 67, 71, 75, 79, 84, 88, 92, 96 to about 100 mol %. Substitution of approximately 15% of normal atoms with heavy isotopes has been performed and maintained in mammals, such as rodents and dogs, for periods of days to weeks with minimal adverse effects (Czajka DM and Finkel AJ, Ann. NY Acad. Sci. 1960 84:770; Thomson JF, Ann. New York Acad. Sci 1960 84:736; Czakja DM et al., Am. J. Physiol. 1961 201:357). Acute substitution of deuterium at levels as high as 15% to 23% in human body fluids has been shown to produce no toxicity (Blagojevic N et al. "Dosimetry & Treatment Planning for Neutron Capture Therapy", Zamenhof R, Solares G and Harling O Eds. 1994. Advanced Medical Publishing, Madison Wis. pp. 125-134; Diabetes Metab. 23:251(1997)).
[0077] Stable isotope labeling of drugs can alter their physico-chemical properties, such as pKa and lipid solubility. If the isotope substitution affects regions involved in ligand-receptor interactions, these effects and changes can affect the pharmacodynamic response of the drug molecule. Although some physical properties of stable isotope-labeled molecules differ from those of their unlabeled counterparts, their chemical and physiological properties are the same, with one exception: due to the increased mass of the heavy isotope, bonds involving the heavy isotope and another atom become stronger than the same bond between the heavy isotope and that atom with a light isotope. Therefore, isotope incorporation at sites of metabolic or enzymatic transformation can slow these reactions and alter the pharmacokinetic profile and potency compared to the unlabeled compound.
[0078] A in the compound of formula (I) 1 , B 1 , D 1 , E 1 , G 1 , Y 1 , L 1 , Z 1A , Z 2A , Z 1 , Z 2 and Z 3 Suitable groups for A are independently selected. The described embodiments of the present invention can be combined. Such combinations are contemplated and are within the scope of the present invention. For example, A 1 , B 1 , D 1 , E 1 , G 1 , Y 1 , L 1 , Z 1A , Z 2A , Z 1 , Z 2 and Z 3 Any of the embodiments of A 1 , B 1 , D 1 , E 1 , G 1 , Y 1 , L 1 , Z 1A , Z 2A , Z 1 , Z 2 and Z3 It is contemplated that any of the above may be combined with any other of the defined embodiments.
[0079] Accordingly, one embodiment of the present invention relates to compounds or therapeutically acceptable salts useful as inhibitors of anti-apoptotic Bcl-2 proteins, which compounds have the following formula (I):
[0080] [ka] During the ceremony, A 1 is N or C(A 2 ) and; A 2 H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; B 1 は、H、R 1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; D 1 は、H、R 1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; IN 1 は、H、R 1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A and; Y 1 are H, CN, NO2, C(O)OH, F, Cl, Br, I, CF3, OCF3, CF2CF3, OCF2CF3, R 17 , OR 17 , C(O)R 17 , C(O)OR 17 , S.R. 17 , SO2R 17 , NH2, NHR 17 , N(R 17 )2, NHC(O)R 17 , C(O)NH2, C(O)NHR 17 , C(O)N(R 17 )2, NHS(O)R 17 or NHSO2R 17 is; or E 1 and Y 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; A 2 , B 1 and D 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A is; or Y 1 and B 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; A 2 , D 1and E 1 is independently selected from H, R 1 , OR 1 , SR 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 , OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , NR 1 C(O)R 1 , NHC(O)OR 1 , NR 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , NR 1 C(O)N(R 1 [[ID=5)]])2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , NR 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , NR 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A ; or A 2 and B 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; D 1 , E 1 and Y 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A is; or A 2 and D 1 together with the atoms to which they are attached are benzene, naphthalene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; B 1 , E 1 and Y 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1, N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A and; G 1 is H or C(O)OR; R is alkyl; R 1 is R 2 , R 3 , R 4 or R 5 and; R 1A is cycloalkyl, cycloalkenyl or cycloalkynyl; R 2 is uncondensed or R 2A is a phenyl fused to R 2A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 3 is uncondensed or R 3A is a heteroaryl fused to R 3A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 4 are uncondensed or R 4A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 4A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 5are each unsubstituted or one, two, or three independently selected R 6 , NC(R 6A )(R 6B ), R 7 , OR 7 , S.R. 7 , S(O)R 7 , SO2R 7 , NHR 7 , N(R 7 )2, C(O)R 7 , C(O)NH2, C(O)NHR 7 , C(O)N(R 7 )2, NHC(O)R 7 , N.R. 7 C(O)R 7 , NHSO2R 7 , NHC(O)OR 7 , SO2NH2, SO2NHR 7 , SO2N(R 7 )2, NHC(O)NH2, NHC(O)NHR 7 , NHC(O)CH(CH3)NHC(O)CH(CH3)NH2, NHC(O)CH(CH3)NHC(O)CH(CH3)NHR 7 , OH, (O), C(O)OH, N3, CN, NH2, CF3, CF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 6 is a C2-C5 spiroalkyl, each unsubstituted or substituted with OH, (O), N3, CN, CF3, CF2CF3, F, Cl, Br, I, NH2, NH(CH3), or N(CH3)2; R 6A and R 6B are independently selected alkyls or together with the N to which they are attached form R 6C and; R 6C is aziridin-1-yl, azetidin-1-yl, pyrrolidin-1-yl or piperidin-1-yl, each of which has one CH moiety that is unsubstituted or replaced by O, C(O), CNOH, CNOCH3, S, S(O), SO2 or NH; R7 is R 8 , R 9 , R 10 or R 11 and; R 8 is not condensed or R 8A is a phenyl fused to R 8A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 9 is uncondensed or R 9A is a heteroaryl fused to R 9A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 10 are uncondensed or R 10A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 10A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 11 are each unsubstituted or one, two, or three independently selected R 12 , OR 12 , S.R. 12 , S(O)R 12 , SO2R 12 , C(O)R 12 , CO(O)R 12 ,OC(O)R 12 ,OC(O)OR 12 , NH2, NHR 12 , N(R 12 )2, NHC(O)R 12 , N.R. 12 C(O)R 12 , NHS(O)2R 12 , N.R. 12 S(O)2R 12 , NHC(O)OR 12 , N.R. 12 C(O)OR 12 , NHC(O)NH2, NHC(O)NHR 12 , NHC(O)N(R 12)2, NR 12 C(O)NHR 12 , N.R. 12 C(O)N(R 12 )2, C(O)NH2, C(O)NHR 12 , C(O)N(R 12 )2, C(O)NHOH, C(O)NHOR 12 , C(O)NHSO2R 12 , C(O)NR 12 SO2R 12 , SO2NH2, SO2NHR 12 , SO2N(R 12 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 12 , C(N)N(R 12 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 12 is R 13 , R 14 , R 15 or R 16 and; R 13 is uncondensed or R 13A is a phenyl fused to R 13A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 14 is uncondensed or R 14A is a heteroaryl fused to R 14A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 15 are uncondensed or R 15A a cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene fused with R 15A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 16is alkyl, alkenyl, or alkynyl; R 17 is R 18 , R 19 , R 20 or R 21 and; R 18 is not condensed or R 18A is a phenyl fused to R 18A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 19 is not condensed or R 19A is a heteroaryl fused to R 19A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 20 are uncondensed or R 20A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 20A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 21 are each unsubstituted or one, two, or three independently selected R 22 , OR 22 , S.R. 22 , S(O)R 22 , SO2R 22 , C(O)R 22 , CO(O)R 22 ,OC(O)R 22 ,OC(O)OR 22 , NH2, NHR 22 , N(R 22 )2, NHC(O)R 22 , N.R. 22 C(O)R 22 , NHS(O)2R 22 , N.R. 22 S(O)2R 22 , NHC(O)OR 22 , N.R. 22 C(O)OR 22, NHC(O)NH2, NHC(O)NHR 22 , NHC(O)N(R 22 )2, NR 22 C(O)NHR 22 , N.R. 22 C(O)N(R 22 )2, C(O)NH2, C(O)NHR 22 , C(O)N(R 22 )2, C(O)NHOH, C(O)NHOR 22 , C(O)NHSO2R 22 , C(O)NR 22 SO2R 22 , SO2NH2, SO2NHR 22 , SO2N(R 22 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 22 , C(N)N(R 22 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 22 is R 23 , R 24 or R 25 and; R 23 is uncondensed or R 23A is a phenyl fused to R 23A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 24 is uncondensed or R 24A is a heteroarene fused to; R 24A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 25 are uncondensed or R 25A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 25A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; Z 1 is R 26 or R 27 and; Z 2 is R 28 , R 29 or R 30 and; Z 1A and Z 2A are both absent or together are CH2, CH2CH2 or Z 12A It forms; Z 12A is C2-C6-alkylene with one or two CH2 moieties replaced by NH, N(CH3), S, S(O) or SO2; L 1 is R 37 , OR 37 , S.R. 37 , S(O)R 37 , SO2R 37 , C(O)R 37 , CO(O)R 37 ,OC(O)R 37 ,OC(O)OR 37 , NHR 37 , C(O)NH, C(O)NR 37 , C(O)NHOR 37 , C(O)NHSO2R 37 , SO2NH, SO2NHR 37 , C(N)NH, C(N)NHR 37 and; R 26 is uncondensed or R 26A is a phenylene fused to R 26A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 27 is uncondensed or R 27A is a heteroarylene fused to R 27A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 28 is uncondensed or R 28Ais a phenylene fused to R 28A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 29 is uncondensed or R 29A is a heteroarylene fused to R 29A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 30 are uncondensed or R 30A a cycloalkylene, cycloalkenylene, heterocyclic alkylene, or heterocyclic alkenylene fused with R 30A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 37 is a bond or R 37A and; R 37A are each unsubstituted or one, two, or three independently selected R 37B , OR 37B , S.R. 37B , S(O)R 37B , SO2R 37B , C(O)R 37B , CO(O)R 37B ,OC(O)R 37B ,OC(O)OR 37B , NH2, NHR 37B , N(R 37B )2, NHC(O)R 37B , N.R. 37B C(O)R 37B , NHS(O)2R 37B , N.R. 37B S(O)2R 37B , NHC(O)OR 37B , N.R. 37B C(O)OR 37B , NHC(O)NH2, NHC(O)NHR 37B , NHC(O)N(R 37B )2, NR 37B C(O)NHR 37B , N.R. 37B C(O)N(R37B )2, C(O)NH2, C(O)NHR 37B , C(O)N(R 37B )2, C(O)NHOH, C(O)NHOR 37B , C(O)NHSO2R 37B , C(O)NR 37B SO2R 37B , SO2NH2, SO2NHR 37B , SO2N(R 37B )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 37B , C(N)N(R 37B )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, alkylene, alkenylene or alkynylene substituted with F, Cl, Br and I substituents; R 37B is alkyl, alkenyl, alkynyl or R 37C and; R 37C is phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; Z 3 is R 38 , R 39 or R 40 and; R 38 is not condensed or R 38A is a phenyl fused to R 38A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 39 is not condensed or R 39A is a heteroaryl fused to R 39A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 40 are uncondensed or R 40A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 40Ais benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 26 and R 27 The part represented by R 41 , OR 41 , S.R. 41 , S(O)R 41 , SO2R 41 , C(O)R 41 , CO(O)R 41 ,OC(O)R 41 ,OC(O)OR 41 , NHR 41 , N(R 41 )2, NHC(O)R 41 , N.R. 41 C(O)R 41 , NHS(O)2R 41 , N.R. 41 S(O)2R 41 , NHC(O)OR 41 , N.R. 41 C(O)OR 41 , NHC(O)NHR 41 , NHC(O)N(R 41 )2, NR 41 C(O)NHR 41 , N.R. 41 C(O)N(R 41 )2, C(O)NHR 41 , C(O)N(R 41 )2, C(O)NHOR 41 , C(O)NHSO2R 41 , C(O)NR 41 SO2R 41 , SO2NHR 41 , SO2N(R 41 )2, C(N)NHR 41 or C(N)N(R 41 )2 (i.e., Z 1A and Z 2A is absent) or further substituted (i.e., Z 1A and Z 2A if exists); R 41 is R 43A is a heteroaryl fused to R 43Ais unfused or benzene, heteroarene or R 43B benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene fused with; R 43B is a cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; E 1 and Y 1 is one, Y 1 and B 1 is one, A 2 and B 1 is one, A 2 and D 1 is one, R 1A , R 2 , R 2A , R 3 , R 3A , R 4 , R 4A , R 6 , R 6C , R 8 , R 8A , R 9 , R 9A , R 10 , R 10A , R 13 , R 13A , R 14 , R 14A , R 15 , R 15A , R 18 , R 18A , R 19 , R 19A , R 20 , R 20A , R 23 , R 23A , R 24 , R 24A , R 25 , R 25A , R 26 , R 26A , R 27 , R 27A , R 28 , R 28A , R 29 , R 29A , R 30 , R 30A , R 37B , R 38 , R 38A , R39 , R 39A , R 40 and R 40A is independently unsubstituted, further unsubstituted, or contains 1 or 2 or 3 or 4 or 5 independently selected R 57A , R 57 , OR 57 , S.R. 57 , S(O)R 57 , SO2R 57 , C(O)R 57 , CO(O)R 57 ,OC(O)R 57 ,OC(O)OR 57 , NH2, NHR 57 , N(R 57 )2, NHC(O)R 57 , N.R. 57 C(O)R 57 , NHS(O)2R 57 , N.R. 57 S(O)2R 57 , NHC(O)OR 57 , N.R. 57 C(O)OR 57 , NHC(O)NH2, NHC(O)NHR 57 , NHC(O)N(R 57 )2, NR 57 C(O)NHR 57 , N.R. 57 C(O)N(R 57 )2, C(O)NH2, C(O)NHR 57 , C(O)N(R 57 )2, C(O)NHOH, C(O)NHOR 57 , C(O)NHSO2R 57 , C(O)NR 57 SO2R 57 , SO2NH2, SO2NHR 57 , SO2N(R 57 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 57 , C(N)N(R 57 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, substituted or further substituted with F, Cl, Br or I; R 57A is spiroalkyl or spiroheteroalkyl; R 57 is R 58 , R 59 , R 60 or R 61 and; R 58 is not condensed or R 58A is a phenyl fused to R 58A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 59 is not condensed or R 59A is a heteroaryl fused to R 59A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 60 are uncondensed or R 60A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 60A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 61 are each unsubstituted or one, two, or three independently selected R 62 , OR 62 , S.R. 62 , S(O)R 62 , SO2R 62 , C(O)R 62 , CO(O)R 62 ,OC(O)R 62 ,OC(O)OR 62 , NH2, NHR 62 , N(R 62 )2, NHC(O)R 62 , N.R. 62 C(O)R 62 , NHS(O)2R 62 , N.R. 62 S(O)2R 62 , NHC(O)OR 62 , N.R. 62 C(O)OR62 , NHC(O)NH2, NHC(O)NHR 62 , NHC(O)N(R 62 )2, NR 62 C(O)NHR 62 , N.R. 62 C(O)N(R 62 )2, C(O)NH2, C(O)NHR 62 , C(O)N(R 62 )2, C(O)NHOH, C(O)NHOR 62 , C(O)NHSO2R 62 , C(O)NR 62 SO2R 62 , SO2NH2, SO2NHR 62 , SO2N(R 62 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 62 , C(N)N(R 62 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 62 is R 63 , R 64 , R 65 or R 66 and; R 63 is not condensed or R 63A is a phenyl fused to R 63A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 64 is not condensed or R 64A is a heteroaryl fused to R 64A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 65 are uncondensed or R 65A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 65Ais benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 66 are each unsubstituted or one, two, or three independently selected R 67 , OR 67 , S.R. 67 , S(O)R 67 , SO2R 67 , C(O)R 67 , CO(O)R 67 ,OC(O)R 67 ,OC(O)OR 67 , NH2, NHR 67 , N(R 67 )2, NHC(O)R 67 , N.R. 67 C(O)R 67 , NHS(O)2R 67 , N.R. 67 S(O)2R 67 , NHC(O)OR 67 , N.R. 67 C(O)OR 67 , NHC(O)NH2, NHC(O)NHR 67 , NHC(O)N(R 67 )2, NR 67 C(O)NHR 67 , N.R. 67 C(O)N(R 67 )2, C(O)NH2, C(O)NHR 67 , C(O)N(R 67 )2, C(O)NHOH, C(O)NHOR 67 , C(O)NHSO2R 67 , C(O)NR 67 SO2R 67 , SO2NH2, SO2NHR 67 , SO2N(R 67 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 67 , C(N)N(R 67 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br, or I substituent substituted alkyl, alkenyl, or alkynyl; R 67is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 57A , R 58 , R 59 , R 60 , R 63 , R 64 , R 65 and R 67 The cyclic moiety represented by the formula (I) is unsubstituted or is substituted with 1 or 2 or 3 or 4 independently selected R 68 , OR 68 , S.R. 68 , S(O)R 68 , SO2R 68 , C(O)R 68 , CO(O)R 68 ,OC(O)R 68 ,OC(O)OR 68 , NH2, NHR 68 , N(R 68 )2, NHC(O)R 68 , N.R. 68 C(O)R 68 , NHS(O)2R 68 , N.R. 68 S(O)2R 68 , NHC(O)OR 68 , N.R. 68 C(O)OR 68 , NHC(O)NH2, NHC(O)NHR 68 , NHC(O)N(R 68 )2, NR 68 C(O)NHR 68 , N.R. 68 C(O)N(R 68 )2, C(O)NH2, C(O)NHR 68 , C(O)N(R 68 )2, C(O)NHOH, C(O)NHOR 68 , C(O)NHSO2R 68 , C(O)NR 68 SO2R 68 , SO2NH2, SO2NHR 68 , SO2N(R 68 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 68, C(N)N(R 68 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I; R 68 is R 69 , R 70 , R 71 or R 72 and; R 69 is not condensed or R 69A is a phenyl fused to R 69A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 70 is uncondensed or R 70A is a heteroaryl fused to R 70A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 71 are uncondensed or R 71A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 71A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 72 are each unsubstituted or one, two, or three independently selected R 73 , OR 73 , S.R. 73 , S(O)R 73 , SO2R 73 , C(O)R 73 , CO(O)R 73 ,OC(O)R 73 ,OC(O)OR 73 , NH2, NHR 73 , N(R 73 )2, NHC(O)R 73 , N.R. 73 C(O)R 73 , NHS(O)2R 73 , N.R. 73 S(O)2R 73, NHC(O)OR 73 , N.R. 73 C(O)OR 73 , NHC(O)NH2, NHC(O)NHR 73 , NHC(O)N(R 73 )2, NR 73 C(O)NHR 73 , N.R. 73 C(O)N(R 73 )2, C(O)NH2, C(O)NHR 73 , C(O)N(R 73 )2, C(O)NHOH, C(O)NHOR 73 , C(O)NHSO2R 73 , C(O)NR 73 SO2R 73 , SO2NH2, SO2NHR 73 , SO2N(R 73 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 73 , C(N)N(R 73 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 73 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 69 , R 70 and R 71 is unsubstituted or substituted with one or two or three or four independently selected NH, C(O)NH, C(O)NHOH, SONH, CF, CFCF, C(O)H, C(O)OH, C(N)NH, OH, (O), CN, N, NO, CF, CFCF, OCF, OCFCF, F, Cl, Br, or I.
[0081] Another embodiment of the present invention is A 1 is N or C(A 2 ) and A 2がH、R 1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; B 1 が、H、R1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; D 1 が、H、R1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; IN 1 が、H、R1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 ,EVENT 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 EVENT 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 C(F)Cl,Br, I, CN, NO2, N3, OH, C(O)H, CF3, C(O)OH, C(O)NH 1A であり; THE 1, H, CN, NO2, C(O)OH, F, Cl, Br, I, CF3, OCF3, CF2CF3, OCF2CF3, R 17 , OR 17 , C(O)R 17 , C(O)OR 17 , S.R. 17 , SO2R 17 , NH2, NHR 17 , N(R 17 )2, NHC(O)R 17 , C(O)NH2, C(O)NHR 17 , C(O)N(R 17 )2, NHS(O)R 17 or NHSO2R 17 is; or E 1 and Y 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; A 2 , B 1 and D 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1, SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A is; or Y 1 and B 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; A 2 , D 1 and E 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1, NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A is; or A 2 and B 1 together with the atom to which they are attached are benzene, naphthylene, a heteroarene, a cycloalkane, a cycloalkene, a heterocyclic alkane, or a heterocyclic alkene; D 1 , E 1 and Y 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1)2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A is; or A 2 and D 1 together with the atoms to which they are attached are benzene, naphthalene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; B 1 , E 1 and Y 1 are independently selected H, R 1 , OR1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; G 1 がHまたはC(O)ORであり; R is alkyl; R 1 R 2 , R 3 , R 4 or R 5 and; R 1A is cycloalkyl, cycloalkenyl, or cycloalkynyl; R 2 Is not condensed or R 2A is a phenyl fused to R 2A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 3 Is not condensed or R 3A is a heteroaryl fused to R 3A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 4 However, each is not condensed or R 4A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 4A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 5 are each unsubstituted or one, two, or three independently selected R 6 , NC(R 6A )(R 6B ), R 7 , OR 7 , S.R. 7 , S(O)R 7 , SO2R 7 , NHR 7 , N(R 7 )2, C(O)R 7 , C(O)NH2, C(O)NHR 7 , C(O)N(R 7 )2, NHC(O)R 7 , N.R. 7 C(O)R 7 , NHSO2R 7 , NHC(O)OR 7, SO2NH2, SO2NHR 7 , SO2N(R 7 )2, NHC(O)NH2, NHC(O)NHR 7 , NHC(O)CH(CH3)NHC(O)CH(CH3)NH2, NHC(O)CH(CH3)NHC(O)CH(CH3)NHR 7 , OH, (O), C(O)OH, N3, CN, NH2, CF3, CF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 6 is a C2-C5 spiroalkyl, each unsubstituted or substituted with OH, (O), N3, CN, CF3, CF2CF3, F, Cl, Br, I, NH2, NH(CH3), or N(CH3)2; R 6A and R 6B are independently selected alkyls or, together with the N to which they are attached, R 6C and; R 6C is aziridin-1-yl, azetidin-1-yl, pyrrolidin-1-yl or piperidin-1-yl, each having one CH moiety that is unsubstituted or replaced by O, C(O), CNOH, CNOCH3, S, S(O), SO2 or NH; R 7 R 8 , R 9 , R 10 or R 11 and; R 8 But it is not condensed or R 8A is a phenyl fused to R 8A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 9 But it is not condensed or R 9A is a heteroaryl fused to R 9A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 10 However, each is not condensed or R10A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 10A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 11 are each unsubstituted or one, two, or three independently selected R 12 , OR 12 , S.R. 12 , S(O)R 12 , SO2R 12 , C(O)R 12 , CO(O)R 12 ,OC(O)R 12 ,OC(O)OR 12 , NH2, NHR 12 , N(R 12 )2, NHC(O)R 12 , N.R. 12 C(O)R 12 , NHS(O)2R 12 , N.R. 12 S(O)2R 12 , NHC(O)OR 12 , N.R. 12 C(O)OR 12 , NHC(O)NH2, NHC(O)NHR 12 , NHC(O)N(R 12 )2, NR 12 C(O)NHR 12 , N.R. 12 C(O)N(R 12 )2, C(O)NH2, C(O)NHR 12 , C(O)N(R 12 )2, C(O)NHOH, C(O)NHOR 12 , C(O)NHSO2R 12 , C(O)NR 12 SO2R 12 , SO2NH2, SO2NHR 12 , SO2N(R 12 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 12 , C(N)N(R 12)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 12 But R 13 , R 14 , R 15 or R 16 and; R 13 But it is not condensed or R 13A is a phenyl fused to R 13A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 14 But it is not condensed or R 14A is a heteroaryl fused to R 14A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 15 However, each is not condensed or R 15A a cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene fused with R 15A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 16 is alkyl, alkenyl, or alkynyl; R 17 R 18 , R 19 , R 20 or R 21 and; R 18 But it is not condensed or R 18A is a phenyl fused to R 18A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 19 But it is not condensed or R 19A is a heteroaryl fused to R 19Ais benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 20 However, each is not condensed or R 20A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 20A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 21 are each unsubstituted or one, two, or three independently selected R 22 , OR 22 , S.R. 22 , S(O)R 22 , SO2R 22 , C(O)R 22 , CO(O)R 22 ,OC(O)R 22 ,OC(O)OR 22 , NH2, NHR 22 , N(R 22 )2, NHC(O)R 22 , N.R. 22 C(O)R 22 , NHS(O)2R 22 , N.R. 22 S(O)2R 22 , NHC(O)OR 22 , N.R. 22 C(O)OR 22 , NHC(O)NH2, NHC(O)NHR 22 , NHC(O)N(R 22 )2, NR 22 C(O)NHR 22 , N.R. 22 C(O)N(R 22 )2, C(O)NH2, C(O)NHR 22 , C(O)N(R 22 )2, C(O)NHOH, C(O)NHOR 22 , C(O)NHSO2R 22 , C(O)NR 22 SO2R 22 , SO2NH2, SO2NHR 22 , SO2N(R 22)2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 22 , C(N)N(R 22 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 22 R 23 , R 24 or R 25 and; R 64 Is not condensed or R 64A is a heteroaryl fused to R 64A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 65 are not condensed or R 65A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 65A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 66 are each unsubstituted or 1, 2, or 3 independently selected R 67 , OR 67 , S.R. 67 , S(O)R 67 , SO2R 67 , C(O)R 67 , CO(O)R 67 ,OC(O)R 67 ,OC(O)OR 67 , NH2, NHR 67 , N(R 67 )2, NHC(O)R 67 , N.R. 67 C(O)R 67 , NHS(O)2R 67 , N.R. 67 S(O)2R 67 , NHC(O)OR 67 , N.R. 67 C(O)OR 67 , NHC(O)NH2, NHC(O)NHR67 , NHC(O)N(R 67 )2, NR 67 C(O)NHR 67 , N.R. 67 C(O)N(R 67 )2, C(O)NH2, C(O)NHR 67 , C(O)N(R 67 )2, C(O)NHOH, C(O)NHOR 67 , C(O)NHSO2R 67 , C(O)NR 67 SO2R 67 , SO2NH2, SO2NHR 67 , SO2N(R 67 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 67 , C(N)N(R 67 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br, or I substituent substituted alkyl, alkenyl, or alkynyl; R 67 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 57A , R 58 , R 59 , R 60 , R 63 , R 64 , R 65 and R 67 is unsubstituted or is substituted with 1 or 2 or 3 or 4 independently selected R 68 , OR 68 , S.R. 68 , S(O)R 68 , SO2R 68 , C(O)R 68 , CO(O)R 68 ,OC(O)R 68 ,OC(O)OR 68 , NH2, NHR 68 , N(R 68 )2, NHC(O)R 68 , N.R. 68 C(O)R68 , NHS(O)2R 68 , N.R. 68 S(O)2R 68 , NHC(O)OR 68 , N.R. 68 C(O)OR 68 , NHC(O)NH2, NHC(O)NHR 68 , NHC(O)N(R 68 )2, NR 68 C(O)NHR 68 , N.R. 68 C(O)N(R 68 )2, C(O)NH2, C(O)NHR 68 , C(O)N(R 68 )2, C(O)NHOH, C(O)NHOR 68 , C(O)NHSO2R 68 , C(O)NR 68 SO2R 68 , SO2NH2, SO2NHR 68 , SO2N(R 68 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 68 , C(N)N(R 68 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I; R 68 R 69 , R 70 , R 71 or R 72 and; R 69 Is not condensed or R 69A is a phenyl fused to R 69A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 70 But it is not condensed or R 70A is a heteroaryl fused to R 70A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 71 However, each is not condensed or R 71Ais a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 71A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 72 are each unsubstituted or 1, 2, or 3 independently selected R 73 , OR 73 , S.R. 73 , S(O)R 73 , SO2R 73 , C(O)R 73 , CO(O)R 73 ,OC(O)R 73 ,OC(O)OR 73 , NH2, NHR 73 , N(R 73 )2, NHC(O)R 73 , N.R. 73 C(O)R 73 , NHS(O)2R 73 , N.R. 73 S(O)2R 73 , NHC(O)OR 73 , N.R. 73 C(O)OR 73 , NHC(O)NH2, NHC(O)NHR 73 , NHC(O)N(R 73 )2, NR 73 C(O)NHR 73 , N.R. 73 C(O)N(R 73 )2, C(O)NH2, C(O)NHR 73 , C(O)N(R 73 )2, C(O)NHOH, C(O)NHOR 73 , C(O)NHSO2R 73 , C(O)NR 73 SO2R 73 , SO2NH2, SO2NHR 73 , SO2N(R 73 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 73 , C(N)N(R 73)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 73 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 69 , R 70 and R 71 is unsubstituted or substituted with 1 or 2 or 3 or 4 independently selected NH, C(O)NH, C(O)NHOH, SONH, CF, CFCF, C(O)H, C(O)OH, C(N)NH, OH, (O), CN, N, NO, CF, CFCF, OCF, OCFCF, F, Cl, Br or I.
[0082] Another embodiment of the present invention is A 1 is N or C(A 2 ) and A 2 H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; B 1 が、H、R 1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A ;C(N)NHR 57 , C(N)N(R 57 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I; R 57A is spiroalkyl or spiroheteroalkyl; R 57 R 58 , R 59 , R 60 or R 61 and; R 58 Is not condensed or R 58A is a phenyl fused to R 58A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 59 Is not condensed or R 59A is a heteroaryl fused to R 59Ais benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 60 are not condensed or R 60A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 60A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 61 are each unsubstituted or 1, 2, or 3 independently selected R 62 , OR 62 , S.R. 62 , S(O)R 62 , SO2R 62 , C(O)R 62 , CO(O)R 62 ,OC(O)R 62 ,OC(O)OR 62 , NH2, NHR 62 , N(R 62 )2, NHC(O)R 62 , N.R. 62 C(O)R 62 , NHS(O)2R 62 , N.R. 62 S(O)2R 62 , NHC(O)OR 62 , N.R. 62 C(O)OR 62 , NHC(O)NH2, NHC(O)NHR 62 , NHC(O)N(R 62 )2, NR 62 C(O)NHR 62 , N.R. 62 C(O)N(R 62 )2, C(O)NH2, C(O)NHR 62 , C(O)N(R 62 )2, C(O)NHOH, C(O)NHOR 62 , C(O)NHSO2R 62 , C(O)NR 62 SO2R 62 , SO2NH2, SO2NHR 62 , SO2N(R 62)2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 62 , C(N)N(R 62 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 62 R 63 , R 64 , R 65 or R 66 and; R 63 Is not condensed or R 63A is a phenyl fused to R 63A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 64 Is not condensed or R 64A is a heteroaryl fused to R 64A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 65 are not condensed or R 65A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 65A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 66 are each unsubstituted or 1, 2, or 3 independently selected R 67 , OR 67 , S.R. 67 , S(O)R 67 , SO2R 67 , C(O)R 67 , CO(O)R 67 ,OC(O)R 67 ,OC(O)OR 67 , NH2, NHR 67 , N(R 67 )2, NHC(O)R 67 , N.R. 67 C(O)R67 , NHS(O)2R 67 , N.R. 67 S(O)2R 67 , NHC(O)OR 67 , N.R. 67 C(O)OR 67 , NHC(O)NH2, NHC(O)NHR 67 , NHC(O)N(R 67 )2, NR 67 C(O)NHR 67 , N.R. 67 C(O)N(R 67 )2, C(O)NH2, C(O)NHR 67 , C(O)N(R 67 )2, C(O)NHOH, C(O)NHOR 67 , C(O)NHSO2R 67 , C(O)NR 67 SO2R 67 , SO2NH2, SO2NHR 67 , SO2N(R 67 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 67 , C(N)N(R 67 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br, or I substituent substituted alkyl, alkenyl, or alkynyl; R 67 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 57A , R 58 , R 59 , R 60 , R 63 , R 64 , R 65 and R 67 is unsubstituted or is substituted with 1 or 2 or 3 or 4 independently selected R 68 , OR 68 , S.R. 68 , S(O)R 68 , SO2R 68 , C(O)R 68, CO(O)R 68 ,OC(O)R 68 ,OC(O)OR 68 , NH2, NHR 68 , N(R 68 )2, NHC(O)R 68 , N.R. 68 C(O)R 68 , NHS(O)2R 68 , N.R. 68 S(O)2R 68 , NHC(O)OR 68 , N.R. 68 C(O)OR 68 , NHC(O)NH2, NHC(O)NHR 68 , NHC(O)N(R 68 )2, NR 68 C(O)NHR 68 , N.R. 68 C(O)N(R 68 )2, C(O)NH2, C(O)NHR 68 , C(O)N(R 68 )2, C(O)NHOH, C(O)NHOR 68 , C(O)NHSO2R 68 , C(O)NR 68 SO2R 68 , SO2NH2, SO2NHR 68 , SO2N(R 68 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 68 , C(N)N(R 68 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I; R 68 R 69 , R 70 , R 71 or R 72 and; R 69 Is not condensed or R 69A is a phenyl fused to R 69A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 70 But it is not condensed or R70A is a heteroaryl fused to R 70A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 71 However, each is not condensed or R 71A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 71A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 72 are each unsubstituted or 1, 2, or 3 independently selected R 73 , OR 73 , S.R. 73 , S(O)R 73 , SO2R 73 , C(O)R 73 , CO(O)R 73 ,OC(O)R 73 ,OC(O)OR 73 , NH2, NHR 73 , N(R 73 )2, NHC(O)R 73 , N.R. 73 C(O)R 73 , NHS(O)2R 73 , N.R. 73 S(O)2R 73 , NHC(O)OR 73 , N.R. 73 C(O)OR 73 , NHC(O)NH2, NHC(O)NHR 73 , NHC(O)N(R 73 )2, NR 73 C(O)NHR 73 , N.R. 73 C(O)N(R 73 )2, C(O)NH2, C(O)NHR 73 , C(O)N(R 73 )2, C(O)NHOH, C(O)NHOR 73 , C(O)NHSO2R 73 , C(O)NR 73 SO2R 73 , SO2NH2, SO2NHR 73, SO2N(R 73 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 73 , C(N)N(R 73 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 73 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 69 , R 70 and R 71 is unsubstituted or substituted with 1 or 2 or 3 or 4 independently selected NH, C(O)NH, C(O)NHOH, SONH, CF, CFCF, C(O)H, C(O)OH, C(N)NH, OH, (O), CN, N, NO, CF, CFCF, OCF, OCFCF, F, Cl, Br or I.
[0083] Another embodiment of the present invention is A 1 is N or C(A 2 ) and; A 2 But, H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; B 1 が、H、R 1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; D 1 が、H、R 1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; IN 1 が、H、R 1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R 1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; Y 1 が、H、CN、NO2、C(O)OH、F、Cl、Br、I、CF3、OCF3、CF2CF3、OCF2CF3、R 17 、OR 17 、C(O)R 17 、C(O)OR 17 、SR 17 、SO2R 17 、NH2、NHR 17 、N(R 17 )2、NHC(O)R 17 、C(O)NH2、C(O)NHR 17 、C(O)N(R 17 )2、NHS(O)R 17 またはNHSO2R 17 であり;または IN 1and Y 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; A 2 , B 1 and D 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A is; or Y 1 and B 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; A 2 , D 1 and E 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A is; or A 2 and B 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; D 1 , E 1 and Y 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1)2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A is; or A 2 and D 1 together with the atoms to which they are attached are benzene, naphthalene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; B 1 , E 1 and Y 1 are independently selected H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1 SO2R 1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 , C(NH)N(R 1 )2NHSO2NHR 1 , NHSO2N(CH3)R 1 , N(CH3)SO2N(CH3)R 1 , F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O)NH2 or C(O)OR 1A and; G 1 is H or C(O)OR; R is alkyl; R 1 R 2 , R 3 , R 4 or R 5 and; R 1A is cycloalkyl, cycloalkenyl, or cycloalkynyl; R 2 But it is not condensed or R 2A is a phenyl fused to R 2A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 3 But it is not condensed or R3A is a heteroaryl fused to R 3A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 4 However, each is not condensed or R 4A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 4A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 5 are each unsubstituted or one, two, or three independently selected R 6 , NC(R 6A )(R 6B ), R 7 , OR 7 , S.R. 7 , S(O)R 7 , SO2R 7 , NHR 7 , N(R 7 )2, C(O)R 7 , C(O)NH2, C(O)NHR 7 , C(O)N(R 7 )2, NHC(O)R 7 , N.R. 7 C(O)R 7 , NHSO2R 7 , NHC(O)OR 7 , SO2NH2, SO2NHR 7 , SO2N(R 7 )2, NHC(O)NH2, NHC(O)NHR 7 , NHC(O)CH(CH3)NHC(O)CH(CH3)NH2, NHC(O)CH(CH3)NHC(O)CH(CH3)NHR 7 , OH, (O), C(O)OH, N3, CN, NH2, CF3, CF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 6is a C2-C5 spiroalkyl, each unsubstituted or substituted with OH, (O), N3, CN, CF3, CF2CF3, F, Cl, Br, I, NH2, NH(CH3), or N(CH3)2; R 6A and R 6B are independently selected alkyls or together with the N to which they are attached form R 6C and; R 6C is aziridin-1-yl, azetidin-1-yl, pyrrolidin-1-yl, or piperidin-1-yl, each of which has one CH moiety that is unsubstituted or replaced by O, C(O), CNOH, CNOCH3, S, S(O), SO2, or NH; R 7 But R 8 , R 9 , R 10 or R 11 and; R 8 Is not condensed or R 8A is a phenyl fused to R 8A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 9 But it is not condensed or R 9A is a heteroaryl fused to R 9A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 10 However, each is not condensed or R 10A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 10A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 11 are each unsubstituted or one, two, or three independently selected R 12 , OR 12 , S.R. 12 , S(O)R 12, SO2R 12 , C(O)R 12 , CO(O)R 12 ,OC(O)R 12 ,OC(O)OR 12 , NH2, NHR 12 , N(R 12 )2, NHC(O)R 12 , N.R. 12 C(O)R 12 , NHS(O)2R 12 , N.R. 12 S(O)2R 12 , NHC(O)OR 12 , N.R. 12 C(O)OR 12 , NHC(O)NH2, NHC(O)NHR 12 , NHC(O)N(R 12 )2, NR 12 C(O)NHR 12 , N.R. 12 C(O)N(R 12 )2, C(O)NH2, C(O)NHR 12 , C(O)N(R 12 )2, C(O)NHOH, C(O)NHOR 12 , C(O)NHSO2R 12 , C(O)NR 12 SO2R 12 , SO2NH2, SO2NHR 12 , SO2N(R 12 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 12 , C(N)N(R 12 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 12 But R 13 , R 14 , R 15 or R 16 and; R 13 But it is not condensed or R 13A is a phenyl fused to R 13Ais benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 14 But it is not condensed or R 14A is a heteroaryl fused to R 14A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 15 However, each is not condensed or R 15A a cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene fused with R 15A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 16 is alkyl, alkenyl, or alkynyl; R 17 R 18 , R 19 , R 20 or R 21 and; R 18 is not condensed or R 18A is a phenyl fused to R 18A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 19 Is not condensed or R 19A is a heteroaryl fused to R 19A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 20 However, each is not condensed or R 20A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 20A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 21 are each unsubstituted or one, two, or three independently selected R 22, OR 22 , S.R. 22 , S(O)R 22 , SO2R 22 , C(O)R 22 , CO(O)R 22 ,OC(O)R 22 ,OC(O)OR 22 , NH2, NHR 22 , N(R 22 )2, NHC(O)R 22 , N.R. 22 C(O)R 22 , NHS(O)2R 22 , N.R. 22 S(O)2R 22 , NHC(O)OR 22 , N.R. 22 C(O)OR 22 , NHC(O)NH2, NHC(O)NHR 22 , NHC(O)N(R 22 )2, NR 22 C(O)NHR 22 , N.R. 22 C(O)N(R 22 )2, C(O)NH2, C(O)NHR 22 , C(O)N(R 22 )2, C(O)NHOH, C(O)NHOR 22 , C(O)NHSO2R 22 , C(O)NR 22 SO2R 22 , SO2NH2, SO2NHR 22 , SO2N(R 22 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 22 , C(N)N(R 22 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 22 But R 23 , R 24 or R 25 and; R 23 But it is not condensed or R 23A is a phenyl fused to R 23Ais benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 24 But it is not condensed or R 24A is a heteroarene fused to; R 24A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 25 However, each is not condensed or R 25A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 25A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; Z 1 R 26 or R 27 and; Z 2 R 28 , R 29 or R 30 and; Z 1A and Z 2A are both absent or together are CH2, CH2CH2 or Z 12A It forms; Z 12A is C2-C6-alkylene with one or two CH2 moieties replaced by NH, N(CH3), S, S(O) or SO2; L 1 But R 37 , OR 37 , S.R. 37 , S(O)R 37 , SO2R 37 , C(O)R 37 , CO(O)R 37 ,OC(O)R 37 ,OC(O)OR 37 , NHR 37 , C(O)NH, C(O)NR 37 , C(O)NHOR 37 , C(O)NHSO2R 37 , SO2NH, SO2NHR 37, C(N)NH, C(N)NHR 37 and; R 26 But it is not condensed or R 26A is a phenylene fused to R 26A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 27 But it is not condensed or R 27A is a heteroarylene fused to R 27A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 28 But it is not condensed or R 28A is a phenylene fused to R 28A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 66 are each unsubstituted or 1, 2, or 3 independently selected R 67 , OR 67 , S.R. 67 , S(O)R 67 , SO2R 67 , C(O)R 67 , CO(O)R 67 ,OC(O)R 67 ,OC(O)OR 67 , NH2, NHR 67 , N(R 67 )2, NHC(O)R 67 , N.R. 67 C(O)R 67 , NHS(O)2R 67 , N.R. 67 S(O)2R 67 , NHC(O)OR 67 , N.R. 67 C(O)OR 67 , NHC(O)NH2, NHC(O)NHR 67 , NHC(O)N(R 67 )2, NR 67 C(O)NHR 67 , N.R. 67 C(O)N(R 67)2, C(O)NH2, C(O)NHR 67 , C(O)N(R 67 )2, C(O)NHOH, C(O)NHOR 67 , C(O)NHSO2R 67 , C(O)NR 67 SO2R 67 , SO2NH2, SO2NHR 67 , SO2N(R 67 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 67 , C(N)N(R 67 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br, or I substituent substituted alkyl, alkenyl, or alkynyl; R 67 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 57A , R 58 , R 59 , R 60 , R 63 , R 64 , R 65 and R 67 is unsubstituted or is substituted with 1 or 2 or 3 or 4 independently selected R 68 , OR 68 , S.R. 68 , S(O)R 68 , SO2R 68 , C(O)R 68 , CO(O)R 68 ,OC(O)R 68 ,OC(O)OR 68 , NH2, NHR 68 , N(R 68 )2, NHC(O)R 68 , N.R. 68 C(O)R 68 , NHS(O)2R 68 , N.R. 68 S(O)2R 68 , NHC(O)OR 68 , N.R. 68 C(O)OR68 , NHC(O)NH2, NHC(O)NHR 68 , NHC(O)N(R 68 )2, NR 68 C(O)NHR 68 , N.R. 68 C(O)N(R 68 )2, C(O)NH2, C(O)NHR 68 , C(O)N(R 68 )2, C(O)NHOH, C(O)NHOR 68 , C(O)NHSO2R 68 , C(O)NR 68 SO2R 68 , SO2NH2, SO2NHR 68 , SO2N(R 68 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 68 , C(N)N(R 68 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I; R 68 R 69 , R 70 , R 71 or R 72 and; R 69 Is not condensed or R 69A is a phenyl fused to R 69A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 70 But it is not condensed or R 70A is a heteroaryl fused to R 70A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 71 However, each is not condensed or R 71A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 71A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 72 are each unsubstituted or 1, 2, or 3 independently selected R 73 , OR 73 , S.R. 73 , S(O)R 73 , SO2R 73 , C(O)R 73 , CO(O)R 73 ,OC(O)R 73 ,OC(O)OR 73 , NH2, NHR 73 , N(R 73 )2, NHC(O)R 73 , N.R. 73 C(O)R 73 , NHS(O)2R 73 , N.R. 73 S(O)2R 73 , NHC(O)OR 73 , N.R. 73 C(O)OR 73 , NHC(O)NH2, NHC(O)NHR 73 , NHC(O)N(R 73 )2, NR 73 C(O)NHR 73 , N.R. 73 C(O)N(R 73 )2, C(O)NH2, C(O)NHR 73 , C(O)N(R 73 )2, C(O)NHOH, C(O)NHOR 73 , C(O)NHSO2R 73 , C(O)NR 73 SO2R 73 , SO2NH2, SO2NHR 73 , SO2N(R 73 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 73 , C(N)N(R 73 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 73is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 69 , R 70 and R 71 is unsubstituted or substituted with 1 or 2 or 3 or 4 independently selected NH, C(O)NH, C(O)NHOH, SONH, CF, CFCF, C(O)H, C(O)OH, C(N)NH, OH, (O), CN, N, NO, CF, CFCF, OCF, OCFCF, F, Cl, Br or I.
[0084] Another embodiment of the present invention is A 1 is N or C(A 2 ) and; A 2 H, R 1 , OR 1 , S.R. 1 , S(O)R 1 , SO2R 1 , C(O)R 1 , C(O)OR 1 ,OC(O)R 1 , NHR 1 , N(R 1 )2, C(O)NHR 1 , C(O)N(R 1 )2, NHC(O)R 1 , N.R. 1 C(O)R 1 , NHC(O)OR 1 , N.R. 1 C(O)OR 1 , NHC(O)NH2, NHC(O)NHR 1 , NHC(O)N(R 1 )2, NR 1 C(O)NHR 1 , N.R. 1 C(O)N(R 1 )2, SO2NH2, SO2NHR 1 , SO2N(R 1 )2, NHSO2R 1 , N.R. 1SO2R 1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; B 1 が、H、R 1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R1 、NHSO2NHR 1 、NHSO2N(R 1 )2、NR 1 SO2NHR 1 、NR 1 SO2N(R 1 )2、C(O)NHNOH、C(O)NHNOR 1 、C(O)NHSO2R 1 、C(NH)NH2、C(NH)NHR 1 、C(NH)N(R 1 )2NHSO2NHR 1 、NHSO2N(CH3)R 1 、N(CH3)SO2N(CH3)R 1 F, Cl, Br, I, CN, NO2, N3, OH, C(O)H, CHNOH, CH(NOCH3), CF3, C(O)OH, C(O) NH2, C(O)OR 1A であり; D 1 が、H、R 1 、OR 1 、SR 1 、S(O)R 1 、SO2R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 )2、C(O)NHR 1 、C(O)N(R 1 )2、NHC(O)R 1 、NR 1 C(O)R 1 、NHC(O)OR 1 、NR 1 C(O)OR 1 、NHC(O)NH2、NHC(O)NHR 1 、NHC(O)N(R 1 )2、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 )2、SO2NH2、SO2NHR 1 、SO2N(R 1 )2、NHSO2R 1 、NR 1 SO2R1 , NHSO2NHR 1 , NHSO2N(R 1 )2, NR 1 SO2NHR 1 , N.R. 1 SO2N(R 1 )2, C(O)NHNOH, C(O)NHNOR 1 , C(O)NHSO2R 1 , C(NH)NH2, C(NH)NHR 1 and; R 62 R 63 , R 64 , R 65 or R 66 and; R 63 Is not condensed or R 63A is a phenyl fused to R 63A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 64 Is not condensed or R 64A is a heteroaryl fused to R 64A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 65 are not condensed or R 65A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 65A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 66 are each unsubstituted or 1, 2, or 3 independently selected R 67 , OR 67 , S.R. 67 , S(O)R 67 , SO2R 67 , C(O)R 67 , CO(O)R 67 ,OC(O)R 67 ,OC(O)OR 67 , NH2, NHR 67 , N(R67 )2, NHC(O)R 67 , N.R. 67 C(O)R 67 , NHS(O)2R 67 , N.R. 67 S(O)2R 67 , NHC(O)OR 67 , N.R. 67 C(O)OR 67 , NHC(O)NH2, NHC(O)NHR 67 , NHC(O)N(R 67 )2, NR 67 C(O)NHR 67 , N.R. 67 C(O)N(R 67 )2, C(O)NH2, C(O)NHR 67 , C(O)N(R 67 )2, C(O)NHOH, C(O)NHOR 67 , C(O)NHSO2R 67 , C(O)NR 67 SO2R 67 , SO2NH2, SO2NHR 67 , SO2N(R 67 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 67 , C(N)N(R 67 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br, or I substituent substituted alkyl, alkenyl, or alkynyl; R 67 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 57A , R 58 , R 59 , R 60 , R 63 , R 64 , R 65 and R 67 is unsubstituted or is substituted with 1 or 2 or 3 or 4 independently selected R 68 , OR 68 , S.R. 68, S(O)R 68 , SO2R 68 , C(O)R 68 , CO(O)R 68 ,OC(O)R 68 ,OC(O)OR 68 , NH2, NHR 68 , N(R 68 )2, NHC(O)R 68 , N.R. 68 C(O)R 68 , NHS(O)2R 68 , N.R. 68 S(O)2R 68 , NHC(O)OR 68 , N.R. 68 C(O)OR 68 , NHC(O)NH2, NHC(O)NHR 68 , NHC(O)N(R 68 )2, NR 68 C(O)NHR 68 , N.R. 68 C(O)N(R 68 )2, C(O)NH2, C(O)NHR 68 , C(O)N(R 68 )2, C(O)NHOH, C(O)NHOR 68 , C(O)NHSO2R 68 , C(O)NR 68 SO2R 68 , SO2NH2, SO2NHR 68 , SO2N(R 68 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 68 , C(N)N(R 68 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I; R 68 R 69 , R 70 , R 71 or R 72 and; R 69 Is not condensed or R 69A is a phenyl fused to R 69Ais benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 70 But it is not condensed or R 70A is a heteroaryl fused to R 70A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 71 However, each is not condensed or R 71A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 71A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 72 are each unsubstituted or 1, 2, or 3 independently selected R 73 , OR 73 , S.R. 73 , S(O)R 73 , SO2R 73 , C(O)R 73 , CO(O)R 73 ,OC(O)R 73 ,OC(O)OR 73 , NH2, NHR 73 , N(R 73 )2, NHC(O)R 73 , N.R. 73 C(O)R 73 , NHS(O)2R 73 , N.R. 73 S(O)2R 73 , NHC(O)OR 73 , N.R. 73 C(O)OR 73 , NHC(O)NH2, NHC(O)NHR 73 , NHC(O)N(R 73 )2, NR 73 C(O)NHR 73 , N.R. 73 C(O)N(R 73 )2, C(O)NH2, C(O)NHR 73 , C(O)N(R 73 )2, C(O)NHOH, C(O)NHOR 73, C(O)NHSO2R 73 , C(O)NR 73 SO2R 73 , SO2NH2, SO2NHR 73 , SO2N(R 73 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 73 , C(N)N(R 73 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 73 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 69 , R 70 and R 71 is unsubstituted or substituted with 1 or 2 or 3 or 4 independently selected NH, C(O)NH, C(O)NHOH, SONH, CF, CFCF, C(O)H, C(O)OH, C(N)NH, OH, (O), CN, N, NO, CF, CFCF, OCF, OCFCF, F, Cl, Br or I.
[0085] In one embodiment of formula (I), A 1 is N and G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H, F, Cl, Br or I; G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;G 1 is H.
[0086] In one embodiment of formula (I), B 1 is R 1 , OR 1 , NHR 1 , NHC(O)R 1 , F, Cl, Br or I. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is NHR 1 and;G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is OR 1 and;G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is Cl; G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is R 1 and;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is NHR 1 and;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is OR 1 and;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is Cl; G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is R 1 and;G 1 is H.
[0087] In one embodiment of Formula (I), D 1 is H or Cl. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is NHR 1 And ;D 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is NHR 1 And ;D 1 is Cl; G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is OR 1 And ;D 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is Cl;D 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is R 1 And ;D 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is NHR 1 And ;D 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is NHR 1 And ;D 1 is Cl; G 1 is H. In another embodiment of formula (I), A1 is N;B 1 is OR 1 And ;D 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is Cl;D 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is R 1 And ;D 1 is H;G 1 is H.
[0088] In one embodiment of Formula (I), E 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is NHR 1 And ;D 1 is H;E 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is NHR 1 and;E 1 is H;D 1 is Cl; G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is OR 1 And ;D 1 is H;E 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is Cl;D 1 is H;E 1is H;G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is R 1 And ;D 1 is H;E 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is NHR 1 And ;D 1 is H;E 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is NHR 1 and;E 1 is H;D 1 is Cl and G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is OR 1 And ;D 1 is H;E 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is Cl;D 1 is H;E 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is R 1 And ;D 1 is H;E 1 is H;G 1 is H.
[0089] In one embodiment of Formula (I), Y 1 are H, CN, NO2, F, Cl, Br, I, CF3, and R 17 , OR 17 , S.R. 17 , SO2R 17or C(O)NH2. In another embodiment of formula (I), Y 1 is H. In another embodiment of formula (I), Y 1 In another embodiment of formula (I), Y 1 is F, Cl, Br or I. In another embodiment of formula (I), Y 1 is CF3. In another embodiment of formula (I), Y 1 is SR 17 In another embodiment of formula (I), Y 1 is OR 17 In another embodiment of formula (I), Y 1 is NO2. In another embodiment of formula (I), Y 1 is SO2R 17 and;R 17 is as defined herein. In another embodiment of formula (I), Y 1 is SO2R 17 and;R 17 is alkyl. In another embodiment of formula (I), Y 1 is R 17 and;R 17 is alkynyl. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is NHR 1 And ;D 1 is H;E 1 is H;G 1 is H;Y 1 is NO2 or SO2R 17 and;R 17 is alkyl or alkynyl. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is NHR 1 And ;D 1 is H;E 1 is H;G 1 is H;Y 1 In another embodiment of formula (I), A 1 is C(A2 ) and;A 2 is H;B 1 is NHR 1 And ;D 1 is H;E 1 is H;G 1 is H;Y 1 is SO2R 17 and;R 17 is alkyl substituted with 3 F. In another embodiment of formula (I), A 1 is N;B 1 is NHR 1 And ;D 1 is H;E 1 is H;G 1 is H;Y 1 is NO2 or SO2R 17 and;R 17 is alkyl or alkynyl. In another embodiment of formula (I), A 1 is N;B 1 is NHR 1 And ;D 1 is H;E 1 is H;G 1 is H;Y 1 In another embodiment of formula (I), A 1 is N;B 1 is NHR 1 And ;D 1 is H;E 1 is H;G 1 is H;Y 1 is SO2R 17 and;R 17 is alkyl substituted with three F's.
[0090] In one embodiment of Formula (I), G 1 is H;A 1 is N or C(A 2 ) and;A 2 is H. In another embodiment of formula (I), G 1 is H;A 1 is N or C(A 2 ) and;A 2 is H;B 1is NHR 1 In another embodiment of formula (I), G 1 is H;A 1 is N or C(A 2 ) and;A 2 is H;B 1 is NHR 1 And ;D 1 is H. In another embodiment of formula (I), G 1 is H;A 1 is N or C(A 2 ) and;A 2 is H;B 1 is NHR 1 And ;D 1 is H;E 1 is H. In another embodiment of formula (I), G 1 is H;A 1 is N or C(A 2 ) and;A 2 is H;B 1 is NHR 1 And ;D 1 is H;E 1 is H;Y 1 is NO2.
[0091] In one embodiment of Formula (I), Y 1 and B 1 together with the atom to which they are attached is benzene. In another embodiment of formula (I), Y 1 and B 1 together with the atoms to which they are attached is a heteroarene. 1 is C(A 2 ) and;A 2 , G 1 , E 1 and D 1 are independently selected H; Y 1 and B 1 together with the atom to which they are attached is benzene. 1 is C(A 2 ) and;A 2 , G 1 , E1 and D 1 are independently selected H; Y 1 and B 1 together with the atoms to which they are attached form a heteroarene.
[0092] In one embodiment of Formula (I), R 1 is R 4 or R 5 In one embodiment of formula (I), R 1 is R 4 In one embodiment of formula (I), R 1 is R 5 In one embodiment of formula (I), R 1 is R 4 and;R 4 is cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl. In one embodiment of Formula (I), R 1 is R 4 and;R 4 is cycloalkyl or heterocycloalkyl. In one embodiment of Formula (I), R 1 is R 4 and;R 4 is cycloalkyl. In one embodiment of Formula (I), R 1 is R 4 and;R 4 is heterocyclic alkyl.
[0093] In one embodiment of Formula (I), R 1 is R 4 and;R 4 is cycloalkyl; R 4 is unsubstituted or substituted as defined herein. In another embodiment of formula (I), R 1 is R 4 and;R 4 is cycloalkyl; and the cycloalkyl ring is substituted as defined herein. In another embodiment of formula (I), R 1 is R 4 and;R 4 is cycloalkyl; the cycloalkyl ring is R 57or N(R 57 In another embodiment of formula (I), R 1 is R 4 and;R 4 is cycloalkyl; the cycloalkyl ring is cyclohexyl; the cyclohexyl ring is R 57 is substituted with;R 57 is R 60 In another embodiment of formula (I), R 1 is R 4 and;R 4 is cycloalkyl; the cycloalkyl ring is cyclohexyl; the cyclohexyl ring is R 57 is substituted with;R 57 is R 60 and;R 60 is heterocycloalkyl. In another embodiment of Formula (I), R 1 is R 4 and;R 4 is cycloalkyl; the cycloalkyl ring is cyclohexyl; the cyclohexyl ring is R 57 is substituted with;R 57 is R 60 and;R 60 is heterocycloalkyl; and the heterocycloalkyl ring is morpholinyl. In another embodiment of formula (I), R 1 is R 4 and;R 4 is cycloalkyl; the cycloalkyl ring is N(R 57 In another embodiment of formula (I), R 1 is R 4 and;R 4 is cycloalkyl; the cycloalkyl ring is cyclohexyl; the cyclohexyl ring is N(R 7 In another embodiment of formula (I), R 1 is R 4 and;R 4 is cycloalkyl; the cycloalkyl ring is cyclohexyl; the cyclohexyl ring is N(R 57 )2 and substituted with R 57 is R61 and;R 61 is not substituted or R 62 In another embodiment of formula (I), R 1 is R 4 and;R 4 is cycloalkyl; the cycloalkyl ring is cyclohexyl; the cyclohexyl ring is R 57 is substituted with;R 57 is R 61 and;R 61 is not substituted or R 62 is alkyl substituted with; R 62 is R 65 and;R 65 is cycloalkyl. In another embodiment of formula (I), R 1 is R 4 and;R 4 is cycloalkyl; the cycloalkyl ring is cyclohexyl; the cyclohexyl ring is R 57 is substituted with;R 57 is R 61 and;R 61 is R 62 is alkyl substituted with; R 62 is R 65 and;R 65 is cyclopropyl.
[0094] In one embodiment of Formula (I), R 1 is R 4 and;R 4 is heterocyclic alkyl; R 4 is unsubstituted or substituted as defined herein. In another embodiment of formula (I), R 1 is R 4 and;R 4 is heterocycloalkyl; and the heterocycloalkyl ring is substituted as defined herein. In another embodiment of formula (I), R 1 is R 4 and;R 4 is a heterocyclic alkyl; the heterocyclic alkyl ring is R 57 In another embodiment of formula (I), R1 is R 4 and;R 4 is heterocyclic alkyl; the heterocyclic alkyl ring is piperdinyl or piperidinyl; the heterocyclic alkyl ring is R 57 is substituted with;R 57 is R 60 or R 61 In another embodiment of formula (I), R 1 is R 4 and;R 4 is heterocyclic alkyl; the heterocyclic alkyl is piperdinyl or piperidinyl; the piperdinyl or piperidinyl ring is R 57 is substituted with;R 57 is R 60 or R 61 and;R 60 is heterocyclic alkyl; R 61 is alkyl. In another embodiment of formula (I), R 1 is R 4 and;R 4 is heterocyclic alkyl; the heterocyclic alkyl is piperdinyl or piperidinyl; the piperdinyl or piperidinyl ring is R 57 is substituted with;R 57 is R 60 and;R 60 is heterocycloalkyl; and the heterocycloalkyl is tetrahydropyranyl. In another embodiment of formula (I), R 1 is R 4 and;R 4 is heterocyclic alkyl; the heterocyclic alkyl is piperdinyl or piperidinyl; the piperdinyl or piperidinyl ring is R 57 is substituted with;R 57 is R 61 and;R 61 is alkyl; and the alkyl is methyl. In another embodiment of formula (I), R 1 is R 4 and;R 4 is heterocycloalkyl; the heterocycloalkyl is piperdinyl or piperidinyl; the piperdinyl or piperidinyl ring is C(O)OR57 is substituted with;R 57 is R 61 and;R 61 is alkyl; and the alkyl is methyl.
[0095] In one embodiment of Formula (I), R 1 is R 5 and;R 5 is unsubstituted or substituted alkyl. In one embodiment of Formula (I), R 1 is R 5 and;R 5 is not substituted or R 7 , OR 7 , OH, CN, or F. In another embodiment of formula (I), R 1 is R 5 and;R 5 is R 7 , OR 7 , NHR 7 or N(R 7 ) alkyl substituted with 2.
[0096] In one embodiment of Formula (I), R 7 is unsubstituted or substituted as defined herein; 8 , R 9 , R 10 or R 11 In another embodiment of formula (I), R 7 is unsubstituted or substituted as defined herein; 8 In another embodiment of formula (I), R 7 is unsubstituted or substituted as defined herein; 9 In another embodiment of formula (I), R 7 is unsubstituted or substituted as defined herein; 10 In another embodiment of formula (I), R 7 is unsubstituted or substituted as defined herein; 11 is.
[0097] In one embodiment of Formula (I), R 8 is phenyl, unsubstituted or substituted as defined herein.
[0098] In one embodiment of Formula (I), R 9 is heteroaryl, unsubstituted or substituted as defined herein. In another embodiment of formula (I), R 9 is furanyl, unsubstituted or substituted as defined herein. In another embodiment of formula (I), R 9 is a substituted furanyl.
[0099] In one embodiment of Formula (I), R 10 is cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl, wherein heterocycloalkyl is unsubstituted or substituted as defined herein. In another embodiment of formula (I), R 10 is heterocycloalkyl, unsubstituted or substituted as defined herein. In another embodiment of formula (I), R 10 is tetrahydrofuranyl, tetrahydropyranyl, morpholinyl, dioxanyl, oxetanyl, piperdinyl or pyrrolidinyl, which are unsubstituted or substituted as defined herein. In another embodiment of formula (I), R 10 is tetrahydropyranyl, unsubstituted or substituted as defined herein. In another embodiment of formula (I), R 10 is morpholinyl, unsubstituted or substituted as defined herein. In another embodiment of formula (I), R 10 is cycloalkyl, unsubstituted or substituted as defined herein. In another embodiment of formula (I), R 10 is cycloalkyl, unsubstituted or substituted as defined herein. In another embodiment of formula (I), R 10is cyclohexyl, cyclopropyl, cyclobutyl, or bicyclo[2.2.1]heptanyl, which is unsubstituted or substituted as defined herein. In another embodiment of formula (I), R 10 is R 10A and R 10A is a heteroarene. In another embodiment of Formula (I), R 10 is 5,6,7,8-tetrahydroimidazo[1,2-a]pyridinyl.
[0100] In one embodiment of Formula (I), R 11 is alkyl, alkenyl, or alkynyl, unsubstituted or substituted as defined herein. In another embodiment of formula (I), R 11 is alkyl. In another embodiment of formula (I), R 11 is methyl, unsubstituted or substituted as defined herein. In another embodiment of formula (I), R 11 is alkyl substituted as defined herein. In another embodiment of formula (I), R 11 is R 12 , OR 12 or alkyl substituted with CF. In another embodiment of formula (I), R 11 is OR 12 is alkyl substituted with; R 12 is R 16 and;R 16 is alkyl. In another embodiment of formula (I), C(O)NHOH, C(O)NHOR 57 , C(O)NHSO2R 57 , C(O)NR 57 SO2R 57 , SO2NH2, SO2NHR 57 , SO2N(R 57 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 57 , C(N)N(R 57)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I; R 57A is spiroalkyl or spiroheteroalkyl; R 57 is R 58 , R 59 , R 60 or R 61 and; R 58 is not condensed or R 58A is a phenyl fused to R 58A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 59 is not condensed or R 59A is a heteroaryl fused to R 59A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 60 are uncondensed or R 60A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 60A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 61 are each unsubstituted or one, two, or three independently selected R 62 , OR 62 , S.R. 62 , S(O)R 62 , SO2R 62 , C(O)R 62 , CO(O)R 62 ,OC(O)R 62 ,OC(O)OR 62 , NH2, NHR 62 , N(R 62 )2, NHC(O)R 62 , N.R. 62 C(O)R 62 , NHS(O)2R 62 , N.R.62 S(O)2R 62 , NHC(O)OR 62 , N.R. 62 C(O)OR 62 , NHC(O)NH2, NHC(O)NHR 62 , NHC(O)N(R 62 )2, NR 62 C(O)NHR 62 , N.R. 62 C(O)N(R 62 )2, C(O)NH2, C(O)NHR 62 , C(O)N(R 62 )2, C(O)NHOH, C(O)NHOR 62 , C(O)NHSO2R 62 , C(O)NR 62 SO2R 62 , SO2NH2, SO2NHR 62 , SO2N(R 62 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 62 , C(N)N(R 62 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I substituted alkyl, alkenyl or alkynyl; R 62 is R 63 , R 64 , R 65 or R 66 and; R 63 is not condensed or R 63A is a phenyl fused to R 63A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 64 is not condensed or R 64A is a heteroaryl fused to R 64A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 65 are uncondensed or R 65Ais a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 65A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 66 are each unsubstituted or one, two, or three independently selected R 67 , OR 67 , S.R. 67 , S(O)R 67 , SO2R 67 , C(O)R 67 , CO(O)R 67 ,OC(O)R 67 ,OC(O)OR 67 , NH2, NHR 67 , N(R 67 )2, NHC(O)R 67 , N.R. 67 C(O)R 67 , NHS(O)2R 67 , N.R. 67 S(O)2R 67 , NHC(O)OR 67 , N.R. 67 C(O)OR 67 , NHC(O)NH2, NHC(O)NHR 67 , NHC(O)N(R 67 )2, NR 67 C(O)NHR 67 , N.R. 67 C(O)N(R 67 )2, C(O)NH2, C(O)NHR 67 , C(O)N(R 67 )2, C(O)NHOH, C(O)NHOR 67 , C(O)NHSO2R 67 , C(O)NR 67 SO2R 67 , SO2NH2, SO2NHR 67 , SO2N(R 67 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 67 , C(N)N(R 67)2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br, or I substituent substituted alkyl, alkenyl, or alkynyl; R 67 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 57A , R 58 , R 59 , R 60 , R 63 , R 64 , R 65 and R 67 The cyclic moiety represented by the formula (I) is unsubstituted or is substituted with 1 or 2 or 3 or 4 independently selected R 68 , OR 68 , S.R. 68 , S(O)R 68 , SO2R 68 , C(O)R 68 , CO(O)R 68 ,OC(O)R 68 ,OC(O)OR 68 , NH2, NHR 68 , N(R 68 )2, NHC(O)R 68 , N.R. 68 C(O)R 68 , NHS(O)2R 68 , N.R. 68 S(O)2R 68 , NHC(O)OR 68 , N.R. 68 C(O)OR 68 , NHC(O)NH2, NHC(O)NHR 68 , NHC(O)N(R 68 )2, NR 68 C(O)NHR 68 , N.R. 68 C(O)N(R 68 )2, C(O)NH2, C(O)NHR 68 , C(O)N(R 68 )2, C(O)NHOH, C(O)NHOR 68 , C(O)NHSO2R 68 , C(O)NR68 SO2R 68 , SO2NH2, SO2NHR 68 , SO2N(R 68 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 68 , C(N)N(R 68 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, F, Cl, Br or I; R 68 is R 69 , R 70 , R 71 or R 72 and; R 69 is not condensed or R 69A is a phenyl fused to R 69A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 70 is uncondensed or R 70A is a heteroaryl fused to R 70A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 71 are uncondensed or R 71A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 71A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 72 are each unsubstituted or one, two, or three independently selected R 73 , OR 73 , S.R. 73 , S(O)R 73 , SO2R 73 , C(O)R 73 , CO(O)R 73 ,OC(O)R 73 ,OC(O)OR 73 , NH2, NHR 73 , N(R73 )2, NHC(O)R 73 , N.R. 73 C(O)R 73 , NHS(O)2R 73 , N.R. 73 S(O)2R 73 , NHC(O)OR 73 , N.R. 73 C(O)OR 73 , NHC(O)NH2, NHC(O)NHR 73 , NHC(O)N(R 73 )2, NR 73 C(O)NHR 73 , N.R. 73 C(O)N(R 73 )2, C(O)NH2, C(O)NHR 73 , C(O)N(R 73 )2, C(O)NHOH, C(O)NHOR 73 , C(O)NHSO2R 73 , C(O)NR 73 SO2R 73 , SO2NH2, SO2NHR 73 , SO2N(R 73 )2, C(O)H, C(O)OH, C(N)NH2, C(N)NHR 73 , C(N)N(R 73 )2, CNOH, CNOCH3, OH, (O), CN, N3, NO2, CF3, CF2CF3, OCF3, OCF2CF3, alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 73 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 69 , R 70 and R 71 is unsubstituted or substituted with one or two or three or four independently selected NH, C(O)NH, C(O)NHOH, SONH, CF, CFCF, C(O)H, C(O)OH, C(N)NH, OH, (O), CN, N, NO, CF, CFCF, OCF, OCFCF, F, Cl, Br, or I.
[0101] In one embodiment of formula (I), A 1 is N and G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H, F, Cl, Br or I; G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;G 1 is H.
[0102] In one embodiment of formula (I), B 1 is R 1 , OR 1 , NHR 1 , NHC(O)R 1 , F, Cl, Br or I. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is NHR 1 and;G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is OR 1 and;G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is Cl; G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is R 1 and;G 1is H. In another embodiment of formula (I), A 1 is N;B 1 is NHR 1 and;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is OR 1 and;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is Cl; G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is R 1 and;G 1 is H.
[0103] In one embodiment of Formula (I), D 1 is H or Cl. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is NHR 1 And ;D 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is NHR 1 And ;D 1 is Cl; G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is OR 1 And ;D 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is Cl;D 1 is H;G 1is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is R 1 And ;D 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is NHR 1 And ;D 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is NHR 1 And ;D 1 is Cl; G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is OR 1 And ;D 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is Cl;D 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is N;B 1 is R 1 And ;D 1 is H;G 1 is H.
[0104] In one embodiment of Formula (I), E 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2 is H;B 1 is NHR 1 And ;D 1 is H;E 1 is H;G 1 is H. In another embodiment of formula (I), A 1 is C(A 2 ) and;A 2is H;B 1 is NHR 1 and;E 1 is H;D 1 is Cl; G 1 is H. In another embodiment, 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3R)-tetrahydro-2H-pyran-3-ylmethyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-(2-naphthylsulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2-methoxyethyl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-({4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-(tetrahydro-2H-pyran-4-ylmethoxy)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1,4-dioxan-2-ylmethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(2,2,2-trifluoroethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(3,3,3-trifluoropropyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2S)-1,4-dioxan-2-ylmethoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; cis-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2R)-1,4-dioxan-2-ylmethoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(1,4-dioxan-2-ylmethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-{[4-(1,4-dioxan-2-ylmethoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-{[5-cyano-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-cyano-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-{[3-(aminocarbonyl)-4-(tetrahydro-2H-pyran-4-ylmethoxy)phenyl]sulfonyl}-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; cis-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-chloro-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-{[5-chloro-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-{[4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]-3-(trifluoromethyl)phenyl]sulfonyl}benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-({4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)benzamide; trans-4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(1-methylpiperidin-4-yl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 5-({[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]amino}sulfonyl)-2-(tetrahydro-2H-pyran-4-ylmethoxy)nicotinamide; N-({5-bromo-6-[(1-methylpiperidin-4-yl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-methylpiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-cyano-6-(1,4-dioxan-2-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-{[5-bromo-6-(1,4-dioxan-2-ylmethoxy)pyridin-3-yl]sulfonyl}-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2,2-dimethyltetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-5-cyano-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({4-[(1-acetylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({2-chloro-5-fluoro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(3-morpholin-4-ylpropyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-cyano-6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-cyano-6-(2-morpholin-4-ylethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[2-(2-methoxyethoxy)ethyl]sulfonyl}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[2-(2-methoxyethoxy)ethyl]sulfonyl}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)oxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-bromo-6-[(1-tetrahydro-2H-pyran-4-ylpiperidin-4-yl)amino]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2-cyanoethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; cis-4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-N-{[4-({4-[bis(cyclopropylmethyl)amino]cyclohexyl}amino)-3-nitrophenyl]sulfonyl}-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1-methylpiperidin-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(morpholin-3-ylmethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(4-methylpiperazin-1-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylbut-2-ynyl)oxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-ethynyl-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-oxo-3,4-dihydroquinazolin-6-yl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[8-(4-chlorophenyl)spiro[4.5]dec-7-en-7-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; cis-4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[8-(4-chlorophenyl)spiro[4.5]dec-7-en-7-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[8-(4-chlorophenyl)spiro[4.5]dec-7-en-7-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-cyano-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; tert-butyl 3-{[4-({[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]amino}sulfonyl)-2-nitrophenoxy]methyl}morpholine-4-carboxylate; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-(morpholin-3-ylmethoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[8-(4-chlorophenyl)spiro[4.5]dec-7-en-7-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[1-(methylsulfonyl)piperidin-4-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1,1-dioxidetetrahydro-2H-thiopyran-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-chloro-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[1-(2,2,2-trifluoroethyl)piperidin-4-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-cyano-6-[(1-tetrahydro-2H-pyran-4-ylpiperidin-4-yl)oxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-isopropyl-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-5-fluoro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; and therapeutically acceptable salts and metabolites thereof.
[0105] 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({1-[2-fluoro-1-(fluoromethyl)ethyl]piperidin-4-yl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[1-(2,2-difluoroethyl)piperidin-4-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-cyclopropylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1-morpholin-4-ylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-(dicyclopropylamino)cyclohexyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-6,6-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-bromo-6-[(4-ethylmorpholin-3-yl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-ethylmorpholin-3-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(4-tetrahydro-2H-pyran-4-ylmorpholin-3-yl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-1-tetrahydro-2H-pyran-4-ylpiperidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-cyano-6-[(tetrahydro-2H-pyran-4-ylmethyl)amino]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1,1-dioxidothiomorpholin-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(4-aminotetrahydro-2H-pyran-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-cyano-6-[(4-morpholin-4-ylcyclohexyl)amino]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-cyano-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1S,3R)-3-morpholin-4-ylcyclopentyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1R,3S)-3-morpholin-4-ylcyclopentyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(morpholin-2-ylmethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydrofuran-3-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({1-[cis-3-fluorotetrahydro-2H-pyran-4-yl]piperidin-4-yl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-tetrahydro-2H-pyran-4-ylazetidin-3-yl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-tetrahydrofuran-3-ylazetidin-3-yl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3R)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4- [(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)-N-(4-((trans-4-hydroxycyclohexyl)methoxy)-3-nitrophenylsulfonyl)benzamide; 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)-N-(4-((cis-4-methoxycyclohexyl)methoxy)-3-nitrophenylsulfonyl)benzamide; cis-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-(cyclopropylamino)cyclohexyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[4-(tetrahydro-2H-pyran-4-ylamino)cyclohexyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-N-({5-bromo-6-[(4-morpholin-4-ylcyclohexyl)oxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methoxycyclohexyl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; tert-butyl 4-{[4-({[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]amino}sulfonyl)-2-nitrophenoxy]methyl}-4-fluoropiperidine-1-carboxylate; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluoropiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[4-(4-tetrahydro-2H-pyran-4-ylpiperazin-1-yl)cyclohexyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({1-[2-fluoro-1-(fluoromethyl)ethyl]piperidin-4-yl}methoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3R)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(2,2-dimethyltetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3S)-1-(2,2-dimethyltetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methylmorpholin-2-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(2-methoxyethyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(4-acetylmorpholin-2-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[trans-4-(fluoromethyl)-1-oxetan-3-ylpyrrolidin-3-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-oxetan-3-ylpiperidin-4-yl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-cyclobutylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[1-(2,2-dimethyltetrahydro-2H-pyran-4-yl)piperidin-4-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3S)-1-cyclopropylpyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-tetrahydrofuran-3-ylpiperidin-4-yl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-cyclopropylpyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3S)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(3-hydroxy-2,2-dimethylpropyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[1-(methylsulfonyl)piperidin-3-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(1-acetylpiperidin-3-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(methylsulfonyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-3,3-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({1-[2-fluoro-1-(fluoromethyl)ethyl]azetidin-3-yl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[1-(methylsulfonyl)pyrrolidin-3-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(1-acetylpyrrolidin-3-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(3R)-1-acetylpyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(3-methoxy-2,2-dimethylpropyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(1R,3R)-3-hydroxycyclopentyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(1S,3S)-3-hydroxycyclopentyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(1S,3R)-3-hydroxycyclopentyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(1R,3S)-3-hydroxycyclopentyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-2-oxopiperidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[({1-[2-fluoro-1-(fluoromethyl)ethyl]azetidin-3-yl}methyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(1-oxetan-3-ylazetidin-3-yl)methyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(1-oxetan-3-ylpiperidin-4-yl)methyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1-cyclopropylpiperidin-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(2-fluoroethyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(2,2-difluoroethyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluoro-1-oxetan-3-ylpiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(2S)-4,4-difluoro-1-oxetan-3-ylpyrrolidin-2-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(4-tetrahydro-2H-pyran-4-ylmorpholin-3-yl)methyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-cyclobutylmorpholin-3-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(4-tetrahydrofuran-3-ylmorpholin-3-yl)methyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[({1-[2-fluoro-1-(fluoromethyl)ethyl]piperidin-4-yl}methyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-cyclopropyl-4-fluoropiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methoxybenzyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[3-(trifluoromethoxy)benzyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(3-methoxybenzyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-(difluoromethoxy)benzyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-(1,4-dioxaspiro[4.5]dec-8-ylamino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-N-[(4-{[4-(acetylamino)cyclohexyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(2,2-difluoroethyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3S)-1-(2-fluoroethyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3S)-1-(2,2-difluoroethyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(2-fluoroethyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-1-oxetan-3-ylpyrrolidin-3-yl]methoxy}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-hydroxybenzyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(3-hydroxybenzyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[3-(difluoromethoxy)benzyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[cis-3-morpholin-4-ylcyclopentyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({4-[(methylsulfonyl)amino]cyclohexyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-cyclopropylpiperidin-4-yl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-oxetan-3-ylpiperidin-4-yl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluoro-1-tetrahydro-2H-pyran-4-ylpiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluoro-1-tetrahydrofuran-3-ylpiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-fluoro-1-(methylsulfonyl)piperidin-4-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3R)-1-oxetan-3-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-hydroxycyclohexyl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({4-[3-(dimethylamino)propoxy]benzyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-(2-morpholin-4-ylethoxy)benzyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(E)-4-hydroxy-1-adamantyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(Z)-4-hydroxy-1-adamantyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({4-[(1S,4S)-bicyclo[2.2.1]hept-5-en-2-ylmethoxy]-3-nitrophenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-methyl-5-oxopyrrolidin-3-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1R,4R,5R,6S)-5,6-dihydroxybicyclo[2.2.1]hept-2-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1R,4R,5S,6R)-5,6-dihydroxybicyclo[2.2.1]hept-2-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(3-oxocyclohexyl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohexa-1,3-dien-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({(3R)-1-[2-fluoro-1-(fluoromethyl)ethyl]pyrrolidin-3-yl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-5-(trifluoromethyl)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3S)-1-oxetan-3-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-N-({5-chloro-6-[(4-methoxycyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; cis-N-({5-chloro-6-[(4-methoxycyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-1-oxetan-3-ylpyrrolidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[({4-[2-(2-methoxyethoxy)ethyl]morpholin-2-yl}methyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(cyanomethyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(N,N-dimethylglycyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; (2-{[(4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}-2-nitrophenyl)amino]methyl}morpholin-4-yl)acetic acid; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[4-(oxetan-3-yl)morpholin-2-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-cyclopropylmorpholin-2-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-(methylsulfonyl)-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methyltetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; Ethyl 4-(4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}-2-nitrophenyl)piperazine-1-carboxylate; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[4-(morpholin-4-yl)piperidin-1-yl]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3R)-1-(oxetan-3-yl)pyrrolidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(1,3-difluoropropan-2-yl)pyrrolidin-3-yl]amino}-3-[(trifluoromethyl)sulfonyl]phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-isopropylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({4-[(1-tert-butylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[1-(2-methoxyethyl)piperidin-3-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[1-(cyanomethyl)piperidin-3-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluoro-1-methylpiperidin-4-yl)methoxy]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(3R)-1-(1,3-difluoropropan-2-yl)pyrrolidin-3-yl]amino}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; tert-Butyl 4-[(4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}-2-nitrophenyl)amino]piperazine-1-carboxylate; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-(pentafluoro-λ 6-sulfanyl)-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methoxytetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(1,3-difluoropropan-2-yl)pyrrolidin-3-yl]oxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[4-(oxetan-3-yl)piperazin-1-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(3R)-tetrahydrofuran-3-ylamino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4,4-difluorocyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({4-[(1-tert-butylpiperidin-4-yl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-({[4-(oxetan-3-yl)morpholin-2-yl]methyl}amino)-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]amino}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(1-cyclopropylpiperidin-4-yl)amino]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(2S)-4-(cyanomethyl)morpholin-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(2S)-4-(N,N-dimethylglycyl)morpholin-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(2R)-4-(cyanomethyl)morpholin-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(2R)-4-(N,N-dimethylglycyl)morpholin-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-fluoro-6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[3-hydroxy-2-(hydroxymethyl)-2-methylpropoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(1,3-difluoropropan-2-yl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(cyanomethyl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({(3R)-1-[2-(2-methoxyethoxy)ethyl]pyrrolidin-3-yl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(N,N-dimethylglycyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[1-(oxetan-3-yl)azetidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(cyanomethyl)-4-fluoropiperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(2R)-4-(N,N-dimethylglycyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(2S)-4-(N,N-dimethylglycyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(N,N-dimethylglycyl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(3R)-1-(2,2-difluoroethyl)pyrrolidin-3-yl]oxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(cyanomethyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-{4-[(4′-chlorobiphenyl-2-yl)methyl]-4-methoxypiperidin-1-yl}-N-({5-chloro-6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-{4-[(4′-chlorobiphenyl-2-yl)methyl]-4-methoxypiperidin-1-yl}-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[9-(4-chlorophenyl)-3-(1,3-difluoropropan-2-yl)-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[9-(4-chlorophenyl)-3-isopropyl-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[9-(4-chlorophenyl)-3-(1,3-difluoropropan-2-yl)-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-N-{[5-chloro-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[9-(4-chlorophenyl)-3-isopropyl-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-N-{[5-chloro-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(4-fluoro-1-methylpiperidin-4-yl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(N,N-dimethylglycyl)-4-fluoropiperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-{4-[(4′-chlorobiphenyl-2-yl)methyl]-4-fluoropiperidin-1-yl}-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-{4-[(4′-chlorobiphenyl-2-yl)methyl]-4-fluoropiperidin-1-yl}-N-({5-chloro-6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[9-(4-chlorophenyl)-3-isopropyl-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-({4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]-3-(trifluoromethyl)phenyl}sulfonyl)benzamide; N-[(5-chloro-6-{[(3R)-1-(1,3-difluoropropan-2-yl)pyrrolidin-3-yl]oxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[2-(tetrahydrofuran-3-yloxy)ethoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-cyanocyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[4-fluoro-1-(oxetan-3-yl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-cyano-6-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-(3-furylmethoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(3R)-1-(1,3-difluoropropan-2-yl)pyrrolidin-3-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(3R)-1-(2,2-difluoroethyl)pyrrolidin-3-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(1,3-difluoropropan-2-yl)-4-fluoropiperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-4-[(4-fluoro-1-methylpiperidin-4-yl)methoxy]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-cyano-4-(tetrahydro-2H-pyran-4-ylmethoxy)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(2,2-difluoroethyl)-4-fluoropiperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(4,4-difluorocyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[6-{[1-(1,3-difluoropropan-2-yl)-4-fluoropiperidin-4-yl]methoxy}-5-(trifluoromethyl)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-chloro-6-[2-(tetrahydrofuran-2-yl)ethoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}-3-methylpiperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[3-(cyclopropylamino)propyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-{[5-chloro-6-(2-methoxyethoxy)pyridin-3-yl]sulfonyl}-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-fluoro-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[1-(methoxyacetyl)piperidin-4-yl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[1-(N,N-dimethylglycyl)piperidin-4-yl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohexyl]methyl}piperidin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-{[6-(tetrahydro-2H-pyran-4-ylmethoxy)-5-(trifluoromethyl)pyridin-3-yl]sulfonyl}benzamide; N-({5-chloro-6-[(trans-4-hydroxycyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-cyano-4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({6-[(trans-4-methoxycyclohexyl)methoxy]-5-(trifluoromethyl)pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({6-[(cis-4-methoxycyclohexyl)methoxy]-5-(trifluoromethyl)pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(4,4-difluoro-1-hydroxycyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperidin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[trans-4-(morpholin-4-yl)cyclohexyl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(1,3-thiazol-5-ylmethyl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-4-[(trans-4-hydroxycyclohexyl)methoxy]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-chloro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-(trifluoromethyl)phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(2,2,2-trifluoroethyl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[1-(oxetan-3-yl)piperidin-4-yl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimet...
Claims
1. A compound having the following formula (I) or a therapeutically acceptable salt of said compound: 【Chemistry 1】 [In the formula, A 1 is N or C (A 2 ) and A 2 は、H、R 1 , OR 1 ,SR 1 ,S(O)R 1 、SO 2 R 1 , C (O) R 1 ,C(O)OR 1 ,OC(O)R 1 ,NHR 1 ,N (R) 1 ) 2 ,C(O)NHR 1 , C (O) N (R 1 ) 2 ,NHC (O)R 1 ,NR 1 C(O)R 1 ,NHC (O)O 1 ,NR 1 C(O)OR 1 ,NHC(O)NH 2 、NXC(O)NXR 1 、NFC(O)N(R 1 ) 2 ,NR 1 C(O)NHR 1 ,NR 1 C(O)N(R 1 ) 2 、SO 2 NH 2 、SO 2 NHR 1 、SO 2 N (R) 1 ) 2 、NHSO 2 R 1 ,NR 1 SO 2 R 1 、NHSO 2 NHR 1 、NHSO 2 N (R) 1 ) 2 ,NR 1 SO 2 NHR 1 ,NR 1 SO 2 N (R) 1 ) 2 、C(O)NXNOH、C(O)NXNOR 1 ,C(O)NHSO 2 R 1 <h2 style=";text-align:left;direction:ltr">、C(NH)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)N(R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> )<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )SO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、F、Cl、Br、I、CN、NO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、N<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、OH、C(O)H、CHNOH、CH(NOCH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )、CF<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、C(O)OH、C(O)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr">またはC(O)OR<h2 style=";text-align:left;direction:ltr"> 1A <h2 style=";text-align:left;direction:ltr">であり; B 1 は、H、R 1 , OR 1 ,SR 1 ,S(O)R 1 、SO 2 R 1 , C (O) R 1 ,C(O)OR 1 ,OC(O)R 1 ,NHR 1 ,N (R) 1 ) 2 ,C(O)NHR 1 , C (O) N (R 1 ) 2 ,NHC (O)R 1 ,NR 1 C(O)R 1 ,NHC (O)O 1 ,NR 1 C(O)OR 1 ,NHC(O)NH 2 、NXC(O)NXR 1 、NFC(O)N(R 1 ) 2 ,NR 1 C(O)NHR 1 ,NR 1 C(O)N(R 1 ) 2 、SO 2 NH 2 、SO 2 NHR 1 、SO 2 N (R) 1 ) 2 、NHSO 2 R 1 ,NR 1 SO 2 R 1 、NHSO 2 NHR 1 、NHSO 2 N (R) 1 ) 2 ,NR 1 SO 2 NHR 1 ,NR 1 SO 2 N (R) 1 ) 2 、C(O)NXNOH、C(O)NXNOR 1 ,C(O)NHSO 2 R 1 <h2 style=";text-align:left;direction:ltr">、C(NH)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)N(R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> )<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )SO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、F、Cl、Br、I、CN、NO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、N<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、OH、C(O)H、CHNOH、CH(NOCH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )、CF<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、C(O)OH、C(O)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr">またはC(O)OR<h2 style=";text-align:left;direction:ltr"> 1A <h2 style=";text-align:left;direction:ltr">であり; D 1 は、H、R 1 , OR 1 ,SR 1 ,S(O)R 1 、SO 2 R 1 , C (O) R 1 ,C(O)OR 1 ,OC(O)R 1 ,NHR 1 ,N (R) 1 ) 2 ,C(O)NHR 1 , C (O) N (R 1 ) 2 ,NHC (O)R 1 ,NR 1 C(O)R 1 ,NHC (O)O 1 ,NR 1 C(O)OR 1 ,NHC(O)NH 2 、NXC(O)NXR 1 、NFC(O)N(R 1 ) 2 ,NR 1 C(O)NHR 1 ,NR 1 C(O)N(R 1 ) 2 、SO 2 NH 2 、SO 2 NHR 1 、SO 2 N (R) 1 ) 2 、NHSO 2 R 1 ,NR 1 SO 2 R 1 、NHSO 2 NHR 1 、NHSO 2 N (R) 1 ) 2 ,NR 1 SO 2 NHR 1 ,NR 1 SO 2 N (R) 1 ) 2 、C(O)NXNOH、C(O)NXNOR 1 ,C(O)NHSO 2 R 1 <h2 style=";text-align:left;direction:ltr">、C(NH)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)N(R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> )<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )SO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、F、Cl、Br、I、CN、NO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、N<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、OH、C(O)H、CHNOH、CH(NOCH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )、CF<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、C(O)OH、C(O)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr">またはC(O)OR<h2 style=";text-align:left;direction:ltr"> 1A <h2 style=";text-align:left;direction:ltr">であり; E 1 は、H、R 1 , OR 1 ,SR 1 ,S(O)R 1 、SO 2 R 1 , C (O) R 1 ,C(O)OR 1 ,OC(O)R 1 ,NHR 1 ,N (R) 1 ) 2 ,C(O)NHR 1 , C (O) N (R 1 ) 2 ,NHC (O)R 1 ,NR 1 C(O)R 1 ,NHC (O)O 1 ,NR 1 C(O)OR 1 ,NHC(O)NH 2 、NXC(O)NXR 1 、NFC(O)N(R 1 ) 2 ,NR 1 C(O)NHR 1 ,NR 1 C(O)N(R 1 ) 2 、SO 2 NH 2 、SO 2 NHR 1 、SO 2 N (R) 1 ) 2 、NHSO 2 R 1 ,NR 1 SO 2 R 1 、NHSO 2 NHR 1 、NHSO 2 N (R) 1 ) 2 ,NR 1 SO 2 NHR 1 ,NR 1 SO 2 N (R) 1 ) 2 、C(O)NXNOH、C(O)NXNOR 1 ,C(O)NHSO 2 R 1 , C(NH)NH 2 , C(NH)NH 1 , C(NH)N(R 1 ) 2 N.H.S.O. 2 NHR 1 , N.H.S.O. 2 N (CH 3 ) R 1 , N(CH 3 ) S.O. 2 N (CH 3 ) R 1 , F, Cl, Br, I, CN, NO 2 , N 3 , OH, C(O)H, CHNOH, CH(NOCH 3 ), C.F. 3 , C(O)OH, C(O)NH 2 or C(O)OR 1A and Y 1 H, CN, NO 2 , C(O)OH, F, Cl, Br, I, CF 3 , O.C.F. 3 , C.F. 2 CF 3 , O.C.F. 2 CF 3 , R 17 , OR 17 , C(O)R 17 , C(O)OR 17 , S.R. 17 , S.O. 2 R 17 , N.H. 2 , N.H.R. 17 , N(R 17 ) 2 , NHC(O)R 17 , C(O)NH 2 , C(O)NHR 17 , C(O)N(R 17 ) 2 , N.H.S.(O)R. 17 or NHSO 2 R 17 or E 1 and Y 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; and A 2 、B 1 and D 1 are independently selected from H, R 1 , OR 1 , SR 1 , S(O)R 1 , SO 2 R 1 , C(O)R 1 , C(O)OR 1 , OC(O)R 1 , NHR 1 , N(R 1 ) 2 , C(O)NHR 1 , C(O)N(R 1 ) 2 , NHCO)R 1 , NR 1 C(O)R 1 , NHCO)OR 1 , NR 1 C(O)OR 1 , NHCONH 2 , NHCONHR 1 , NHCON(R 1 ) 2 , NR 1 C(O)NHR 1 , NR 1 C(O)N(R 1 ) 2 , SO 2 NH 2 , SO 2 NHR 1 , SO 2 N(R 1 ) 2 , NHSO 2 R 1 , NR 1 SO 2 R 1 , NHSO 2 NHR 1 , NHSO 2 N(R 1 ) 2 , NR 1 SO 2 NHR 1 , NR 1 SO 2 N(R 1 ) 2 , C(O)NHNOH, C(O)NHNOR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(O)NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 1<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)N(R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> )<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )SO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、F、Cl、Br、I、CN、NO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、N<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、OH、C(O)H、CHNOH、CH(NOCH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )、CF<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、C(O)OH、C(O)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr">またはC(O)OR<h2 style=";text-align:left;direction:ltr"> 1A <h2 style=";text-align:left;direction:ltr">であり;または Y 1 and B 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; and A 2 、 D 1 and E 1 are independently selected from H, R 1 , OR 1 , SR 1 , S(O)R 1 , SO 2 R 1 , C(O)R 1 , C(O)OR 1 , OC(O)R 1 , NHR 1 , N(R 1 ) 2 , C(O)NHR 1 , C(O)N(R 1 ) 2 , NHCO)R 1 , NR 1 C(O)R 1 , NHCO)OR 1 , NR 1 C(O)OR 1 , NHCONH 2 , NHCONHR 1 , NHCON(R 1 ) 2 , NR 1 C(O)NHR 1 , NR 1 C(O)N(R 1 ) 2 , SO 2 NH 2 , SO 2 NH 1 , SO 2 N(R 1 ) 2 , NHSO 2 R 1 , NR 1 SO 2 R 1 , NHSO 2 NH 1 , NHSO 2 N(R 1 ) 2 , NR 1 SO 2 NH 1 , NR 1 SO 2 N(R 1 ) 2 , C(O)NHNOH, C(O)NHNOR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(O)NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 1<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)N(R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> )<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )SO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、F、Cl、Br、I、CN、NO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、N<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、OH、C(O)H、CHNOH、CH(NOCH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )、CF<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、C(O)OH、C(O)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr">またはC(O)OR<h2 style=";text-align:left;direction:ltr"> 1A <h2 style=";text-align:left;direction:ltr">であり;または A 2 and B 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; and D 1 、E 1 and Y 1 are independently selected from H, R 1 、OR 1 、SR 1 、S(O)R 1 、SO 2 R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 ) 2 、C(O)NHR 1 、C(O)N(R 1 ) 2 、NHCO)R 1 、NR 1 C(O)R 1 、NHCO)OR 1 、NR 1 C(O)OR 1 、NHCONH 2 、NHCONHR 1 、NHCON(R 1 ) 2 、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 ) 2 、SO 2 NH 2 、SO 2 NHR 1 、SO 2 N(R 1 ) 2 、NHSO 2 R 1 、NR 1 SO 2 R 1 、NHSO 2 NHR 1 、NHSO 2 N(R 1 ) 2 、NR 1 SO 2 NHR 1 、NR 1 SO 2 N(R 1 ) 2 、C(O)NHNOH, C(O)NHNOR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(O)NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 1<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)N(R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> )<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )SO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、F、Cl、Br、I、CN、NO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、N<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、OH、C(O)H、CHNOH、CH(NOCH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )、CF<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、C(O)OH、C(O)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr">またはC(O)OR<h2 style=";text-align:left;direction:ltr"> 1A <h2 style=";text-align:left;direction:ltr">であり;または A 2 and D. 1 together with the atoms to which they are attached are benzene, naphthalene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; and B 1 、E 1 and Y 1 are independently selected from H, R 1 、OR 1 、SR 1 、S(O)R 1 、SO 2 R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 ) 2 、C(O)NHR 1 、C(O)N(R 1 ) 2 、NHCO 1 、NR 1 COR 1 、NHCOOR 1 、NR 1 COOR 1 、NHCONH 2 、NHCONHR 1 、NHCON(R 1 ) 2 、NR 1 CONHR 1 、NR 1 CON(R 1 ) 2 、SO 2 NH 2 、SO 2 NHR 1 、SO 2 N(R 1 ) 2 、NHSO 2 R 1 、NR 1 SO 2 R 1 、NHSO 2 NHR 1 、NHSO 2 N(R 1 ) 2 、NR 1 SO 2 NHR 1 、NR 1 SO 2 N(R 1 ) 2 、C(O)NHNOH, C(O)NHNOR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(O)NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 1<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)N(R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> )<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )SO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、F、Cl、Br、I、CN、NO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、N<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、OH、C(O)H、CHNOH、CH(NOCH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )、CF<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、C(O)OH、C(O)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr">またはC(O)OR<h2 style=";text-align:left;direction:ltr"> 1A <h2 style=";text-align:left;direction:ltr">であり; G 1 is H or C(O)OR; R is alkyl; R 1 is R 2 , R 3 , R 4 Or R 5 and R 1A is cycloalkyl, cycloalkenyl, or cycloalkynyl; R 2 is not condensed or R 2A is a phenyl fused to 2A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 3 is not condensed or R 3A is a heteroaryl fused to 3A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 4 are either uncondensed or R 4A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 4A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 5 each is unsubstituted or represents one, two, or three independently selected R 6 , N.C. 6A ) (R 6B ), R 7 , OR 7 , S.R. 7 , S(O)R 7 , S.O. 2 R 7 , N.H.R. 7 , N(R 7 ) 2 , C(O)R 7 , C(O)NH 2 , C(O)NHR 7 , C(O)N(R 7 ) 2 , NHC(O)R 7 , N.R. 7 C(O)R 7 , N.H.S.O. 2 R 7 , NHC(O)OR 7 , S.O. 2 N.H. 2 , S.O. 2 NHR 7 , S.O. 2 N (R 7 ) 2 , NHC(O)NH 2 ,NHC(O)NHR 7 ,NHC(O)CH(CH 3 )NHC(O)CH(CH 3 ) N.H. 2 ,NHC(O)CH(CH 3 )NHC(O)CH(CH 3 ) N.H.R. 7 , OH, (O), C(O)OH, N 3 , C.N., N.H. 2 , C.F. 3 , C.F. 2 CF 3 , alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 6 are unsubstituted or OH, (O), N 3 , C.N., C.F. 3 , C.F. 2 CF 3 , F, Cl, Br, I, NH 2 , NH(CH 3 ) or N(CH 3 ) 2 C substituted with 2 -C 5 is a spiroalkyl; R 6A and R 6B are independently selected alkyl or together with the N to which they are attached represent R 6C and R 6C is aziridin-1-yl, azetidin-1-yl, pyrrolidin-1-yl or piperidin-1-yl, each of which is unsubstituted or O, C(O), CNOH, CNOCH 3 ,S,S(O),SO 2 or one CH replaced by NH 2 portion; R 7 is R 8 , R 9 , R 10 Or R 11 and R 8 Is not condensed or R 8A is a phenyl fused to 8A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 9 is not condensed or R 9A is a heteroaryl fused to 9A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 10 are either uncondensed or R 10A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 10A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 11 each is unsubstituted or represents one, two, or three independently selected R 12 , OR 12 , S.R. 12 , S(O)R 12 , S.O. 2 R 12 , C(O)R 12 , CO(O)R 12 , O.C.(O)R 12 , O C (O) O R 12 , N.H. 2 , N.H.R. 12 , N(R 12 ) 2 , NHC(O)R 12 , N.R. 12 C(O)R 12 , N.H.S. (O) 2 R 12 , N.R. 12 S (O) 2 R 12 , NHC(O)OR 12 , N.R. 12 C(O)OR 12 , NHC(O)NH 2 ,NHC(O)NHR 12 ,NHC(O)N(R 12 ) 2 , N.R. 12 C(O)NHR 12 , N.R. 12 C(O)N(R 12 ) 2 , C(O)NH 2 , C(O)NHR 12 , C(O)N(R 12 ) 2 , C(O)NHOH, C(O)NHOR 12 , C(O)NHSO 2 R 12 , C(O)NR 12 SO 2 R 12 , S.O. 2 N.H. 2 , S.O. 2 NHR 12 , S.O. 2 N (R 12 ) 2 , C(O)H, C(O)OH, C(N)NH 2 , C(N)NHR 12 , C(N)N(R 12 ) 2 ,CNOH,CNOCH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 12 is R 13 , R 14 , R 15 Or R 16 and R 13 is not condensed or R 13A is a phenyl fused to 13A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 14 is not condensed or R 14A is a heteroaryl fused to 14A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 15 are either uncondensed or R 15A is a cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene fused with 15A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 16 is alkyl, alkenyl or alkynyl; R 17 is R 18 , R 19 , R 20 Or R 21 and R 18 Is not condensed or R 18A is a phenyl fused to 18A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 19 Is not condensed or R 19A is a heteroaryl fused to 19A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 20 are either uncondensed or R 20A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 20A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 21 each is unsubstituted or represents one, two, or three independently selected R 22 , OR 22 , S.R. 22 , S(O)R 22 , S.O. 2 R 22 , C(O)R 22 , CO(O)R 22 , O.C.(O)R 22 , O C (O) O R 22 , N.H. 2 , N.H.R. 22 , N(R 22 ) 2 , NHC(O)R 22 , N.R. 22 C(O)R 22 , N.H.S. (O) 2 R 22 , N.R. 22 S (O) 2 R 22 , NHC(O)OR 22 , N.R. 22 C(O)OR 22 , NHC(O)NH 2 ,NHC(O)NHR 22 ,NHC(O)N(R 22 ) 2 , N.R. 22 C(O)NHR 22 , N.R. 22 C(O)N(R 22 ) 2 , C(O)NH 2 , C(O)NHR 22 , C(O)N(R 22 ) 2 , C(O)NHOH, C(O)NHOR 22 , C(O)NHSO 2 R 22 , C(O)NR 22 SO 2 R 22 , S.O. 2 N.H. 2 , S.O. 2 NHR 22 , S.O. 2 N (R 22 ) 2 , C(O)H, C(O)OH, C(N)NH 2 , C(N)NHR 22 , C(N)N(R 22 ) 2 ,CNOH,CNOCH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 22 is R 23 , R 24 Or R 25 and R 23 is not condensed or R 23A is a phenyl fused to 23A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 24 is not condensed or R 24A R is a heteroarene fused to 24A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 25 are either uncondensed or R 25A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 25A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; Z 1 is R 26 Or R 27 and Z 2 is R 28 , R 29 Or R 30 and Z 1A and Z 2A are both non-existent or together are CH 2 , C.H. 2 CH 2 Or Z 12A forming Z 12A is NH, N(CH 3 ), S, S(O) or SO 2 One or two CH replaced by 2 C having a moiety 2 -C 6 - alkylene; L 1 は、R 37 、OR 37 、S 37 、S(O)R 37 、SO 2 R 37 、C(O)R 37 、CO(O)R 37 、OC(O)R 37 、OC(O)OR 37 、NHYR 37 、C(O)NH、C(O)NR 37 、C(O)NHOR 37 、C(O)NHSO 2 R 37 、SO 2 NH、SO 2 NER 37 、C(N)NH、C(N)NHR 37 ; R 26 is not condensed or R 26A R is a phenylene fused to 26A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 27 is not condensed or R 27A R is a heteroarylene fused to 27A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 28 is not condensed or R 28A R is a phenylene fused to 28A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 29 is not condensed or R 29A R is a heteroarylene fused to 29A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 30 are either uncondensed or R 30A is a cycloalkylene, cycloalkenylene, heterocyclic alkylene, or heterocyclic alkenylene fused with 30A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 37 is a bond or R 37A and R 37A each is unsubstituted or represents one, two, or three independently selected R 37B , OR 37B , S.R. 37B , S(O)R 37B , S.O. 2 R 37B , C(O)R 37B , CO(O)R 37B , O.C.(O)R 37B , O C (O) O R 37B , N.H. 2 , N.H.R. 37B , N(R 37B ) 2 , NHC(O)R 37B , N.R. 37B C(O)R 37B , N.H.S. (O) 2 R 37B , N.R. 37B S (O) 2 R 37B , NHC(O)OR 37B , N.R. 37B C(O)OR 37B , NHC(O)NH 2 ,NHC(O)NHR 37B ,NHC(O)N(R 37B ) 2 , N.R. 37B C(O)NHR 37B , N.R. 37B C(O)N(R 37B ) 2 , C(O)NH 2 , C(O)NHR 37B , C(O)N(R 37B ) 2 , C(O)NHOH, C(O)NHOR 37B , C(O)NHSO 2 R 37B , C(O)NR 37B SO 2 R 37B , S.O. 2 N.H. 2 , S.O. 2 NHR 37B , S.O. 2 N (R 37B ) 2 , C(O)H, C(O)OH, C(N)NH 2 , C(N)NHR 37B , C(N)N(R 37B ) 2 ,CNOH,CNOCH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , alkylene, alkenylene or alkynylene substituted with F, Cl, Br and I substituents; R 37B is alkyl, alkenyl, alkynyl or R 37C and R 37C is phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; Z 3 is R 38 , R 39 Or R 40 and R 38 Is not condensed or R 38A is a phenyl fused to 38A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 39 Is not condensed or R 39A is a heteroaryl fused to 39A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 40 are either uncondensed or R 40A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 40A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 26 and R 27 The moiety represented by R 41 , OR 41 , S.R. 41 , S(O)R 41 , S.O. 2 R 41 , C(O)R 41 , CO(O)R 41 , O.C.(O)R 41 , O C (O) O R 41 , N.H.R. 41 , N(R 41 ) 2 , NHC(O)R 41 , N.R. 41 C(O)R 41 , N.H.S. (O) 2 R 41 , N.R. 41 S (O) 2 R 41 , NHC(O)OR 41 , N.R. 41 C(O)OR 41 ,NHC(O)NHR 41 ,NHC(O)N(R 41 ) 2 , N.R. 41 C(O)NHR 41 , N.R. 41 C(O)N(R 41 ) 2 , C(O)NHR 41 , C(O)N(R 41 ) 2 , C(O)NHOR 41 , C(O)NHSO 2 R 41 , C(O)NR 41 SO 2 R 41 , S.O. 2 NHR 41 , S.O. 2 N (R 41 ) 2 , C(N)NHR 41 or C(N)N(R 41 ) 2 (i.e., Z 1A and Z 2A is absent) or further substituted (i.e., Z 1A and Z 2A exists); R 41 is R 43A is a heteroaryl fused to 43A is unfused or is benzene, heteroarene or R 43B R is a benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene fused with 43B is a cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; E 1 and Y 1 is one, Y 1 and B 1 is one, A 2 and B 1 is one, A 2 and D. 1 is one, R 1A , R 2 , R 2A , R 3 , R 3A , R 4 , R 4A , R 6 , R 6C , R 8 , R 8A , R 9 , R 9A , R 10 , R 10A , R 13 , R 13A , R 14 , R 14A , R 15 , R 15A , R 18 , R 18A , R 19 , R 19A , R 20 , R 20A , R 23 , R 23A , R 24 , R 24A , R 25 , R 25A , R 26 , R 26A , R 27 , R 27A , R 28 , R 28A , R 29 , R 29A , R 30 , R 30A , R 37B , R 38 , R 38A , R 39 , R 39A , R 40 and R 40A The cyclic moiety represented by is independently unsubstituted, further unsubstituted, or contains 1 or 2 or 3 or 4 or 5 independently selected R 57A , R 57 , OR 57 ,SR 57 ,S(O)R 57 、SO 2 R 57 , C (O) R 57 ,CO(O)R 57 ,OC(O)R 57 ,OC(O)CR 57 ,NH 2 ,NHR 57 ,N (R) 57 ) 2 ,NHC (O)R 57 ,NR 57 C(O)R 57 ,NHS (O) 2 R 57 ,NR 57 S (O) 2 R 57 ,NHC (O)O 57 ,NR 57 C(O)OR 57 ,NHC(O)NH 2 、NXC(O)NXR 57 、NFC(O)N(R 57 ) 2 ,NR 57 C(O)NHR 57 ,NR 57 C(O)N(R 57 ) 2 ,C(O)NH 2 ,C(O)NHR 57 , C (O) N (R 57 ) 2 、C(O)NHOH、C(O)NHOR 57 ,C(O)NHSO 2 R 57 ,C(O)NR 57 SO 2 R 57 、SO 2 NH 2 、SO 2 NHR 57 、SO 2 N (R) 57 ) 2 、C(O)H、C(O)OH、C(N)NH 2 ,C(N)NHR 57 , C (N) N (R 57 ) 2 ,CNOH,CNOH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , substituted or further substituted with F, Cl, Br or I; R 57A is spiroalkyl or spiroheteroalkyl; R 57 is R 58 , R 59 , R 60 Or R 61 and R 58 Is not condensed or R 58A is a phenyl fused to 58A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 59 Is not condensed or R 59A is a heteroaryl fused to 59A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 60 Each is either uncondensed or R 60A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 60A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 61 each is unsubstituted or represents one, two, or three independently selected R 62 , OR 62 , S.R. 62 , S(O)R 62 , S.O. 2 R 62 , C(O)R 62 , CO(O)R 62 , O.C.(O)R 62 , O C (O) O R 62 , N.H. 2 , N.H.R. 62 , N(R 62 ) 2 , NHC(O)R 62 , N.R. 62 C(O)R 62 , N.H.S. (O) 2 R 62 , N.R. 62 S (O) 2 R 62 , NHC(O)OR 62 , N.R. 62 C(O)OR 62 , NHC(O)NH 2 ,NHC(O)NHR 62 ,NHC(O)N(R 62 ) 2 , N.R. 62 C(O)NHR 62 , N.R. 62 C(O)N(R 62 ) 2 , C(O)NH 2 , C(O)NHR 62 , C(O)N(R 62 ) 2 , C(O)NHOH, C(O)NHOR 62 , C(O)NHSO 2 R 62 , C(O)NR 62 SO 2 R 62 , S.O. 2 N.H. 2 , S.O. 2 NHR 62 , S.O. 2 N (R 62 ) 2 , C(O)H, C(O)OH, C(N)NH 2 , C(N)NHR 62 , C(N)N(R 62 ) 2 ,CNOH,CNOCH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 62 is R 63 , R 64 , R 65 Or R 66 and R 63 Is not condensed or R 63A is a phenyl fused to 63A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 64 Is not condensed or R 64A is a heteroaryl fused to 64A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 65 Each is either uncondensed or R 65A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 65A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 66 each is unsubstituted or represents one, two, or three independently selected R 67 , OR 67 , S.R. 67 , S(O)R 67 , S.O. 2 R 67 , C(O)R 67 , CO(O)R 67 , O.C.(O)R 67 , O C (O) O R 67 , N.H. 2 , N.H.R. 67 , N(R 67 ) 2 , NHC(O)R 67 , N.R. 67 C(O)R 67 , N.H.S. (O) 2 R 67 , N.R. 67 S (O) 2 R 67 , NHC(O)OR 67 , N.R. 67 C(O)OR 67 , NHC(O)NH 2 ,NHC(O)NHR 67 ,NHC(O)N(R 67 ) 2 , N.R. 67 C(O)NHR 67 , N.R. 67 C(O)N(R 67 ) 2 , C(O)NH 2 , C(O)NHR 67 , C(O)N(R 67 ) 2 , C(O)NHOH, C(O)NHOR 67 , C(O)NHSO 2 R 67 , C(O)NR 67 SO 2 R 67 , S.O. 2 N.H. 2 , S.O. 2 NHR 67 , S.O. 2 N (R 67 ) 2 , C(O)H, C(O)OH, C(N)NH 2 , C(N)NHR 67 , C(N)N(R 67 ) 2 ,CNOH,CNOCH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I substituents; R 67 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 57A , R 58 , R 59 , R 60 , R 63 , R 64 , R 65 and R 67 The cyclic moiety represented by the formula (I) is unsubstituted or contains one or two or three or four independently selected R 68 , OR 68 , S.R. 68 , S(O)R 68 , S.O. 2 R 68 , C(O)R 68 , CO(O)R 68 , O.C.(O)R 68 , O C (O) O R 68 , N.H. 2 , N.H.R. 68 , N(R 68 ) 2 , NHC(O)R 68 , N.R. 68 C(O)R 68 , N.H.S. (O) 2 R 68 , N.R. 68 S (O) 2 R 68 , NHC(O)OR 68 , N.R. 68 C(O)OR 68 , NHC(O)NH 2 ,NHC(O)NHR 68 ,NHC(O)N(R 68 ) 2 , N.R. 68 C(O)NHR 68 , N.R. 68 C(O)N(R 68 ) 2 , C(O)NH 2 , C(O)NHR 68 , C(O)N(R 68 ) 2 , C(O)NHOH, C(O)NHOR 68 , C(O)NHSO 2 R 68 , C(O)NR 68 SO 2 R 68 , S.O. 2 N.H. 2 , S.O. 2 NHR 68 , S.O. 2 N (R 68 ) 2 , C(O)H, C(O)OH, C(N)NH 2 , C(N)NHR 68 , C(N)N(R 68 ) 2 ,CNOH,CNOCH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , substituted with F, Cl, Br or I; R 68 is R 69 , R 70 , R 71 Or R 72 and R 69 Is not condensed or R 69A is a phenyl fused to 69A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 70 is not condensed or R 70A is a heteroaryl fused to 70A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 71 are either uncondensed or R 71A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 71A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 72 each is unsubstituted or represents one, two, or three independently selected R 73 , OR 73 , S.R. 73 , S(O)R 73 , S.O. 2 R 73 , C(O)R 73 , CO(O)R 73 , O.C.(O)R 73 , O C (O) O R 73 , N.H. 2 , N.H.R. 73 , N(R 73 ) 2 , NHC(O)R 73 , N.R. 73 C(O)R 73 , N.H.S. (O) 2 R 73 , N.R. 73 S (O) 2 R 73 , NHC(O)OR 73 , N.R. 73 C(O)OR 73 , NHC(O)NH 2 ,NHC(O)NHR 73 ,NHC(O)N(R 73 ) 2 , N.R. 73 C(O)NHR 73 , N.R. 73 C(O)N(R 73 ) 2 , C(O)NH 2 , C(O)NHR 73 , C(O)N(R 73 ) 2 , C(O)NHOH, C(O)NHOR 73 , C(O)NHSO 2 R 73 , C(O)NR 73 SO 2 R 73 , S.O. 2 N.H. 2 , S.O. 2 NHR 73 , S.O. 2 N (R 73 ) 2 , C(O)H, C(O)OH, C(N)NH 2 , C(N)NHR 73 , C(N)N(R 73 ) 2 ,CNOH,CNOCH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 73 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; and R 69 , R 70 and R 71 is unsubstituted or is substituted with 1 or 2 or 3 or 4 independently selected NH 2 , C(O)NH 2 ,C(O)NHOH,SO 2 N.H. 2 , C.F. 3 , C.F. 2 CF 3 , C(O)H, C(O)OH, C(N)NH 2 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , substituted with F, Cl, Br or I.
2. A compound having the following formula (II): or a therapeutically acceptable salt of said compound: 【Chemistry 2】 [In the formula, R 100 is R 26 As described above for the substituents; n is 0, 1, 2 or 3; A 1 is N or C (A 2 ) and A 2 は、H、R 1 , OR 1 ,SR 1 ,S(O)R 1 、SO 2 R 1 , C (O) R 1 ,C(O)OR 1 ,OC(O)R 1 ,NHR 1 ,N (R) 1 ) 2 ,C(O)NHR 1 , C (O) N (R 1 ) 2 ,NHC (O)R 1 ,NR 1 C(O)R 1 ,NHC (O)O 1 ,NR 1 C(O)OR 1 ,NHC(O)NH 2 、NXC(O)NXR 1 、NFC(O)N(R 1 ) 2 ,NR 1 C(O)NHR 1 ,NR 1 C(O)N(R 1 ) 2 、SO 2 NH 2 、SO 2 NHR 1 、SO 2 N (R) 1 ) 2 、NHSO 2 R 1 ,NR 1 SO 2 R 1 、NHSO 2 NHR 1 、NHSO 2 N (R) 1 ) 2 ,NR 1 SO 2 NHR 1 ,NR 1 SO 2 N (R) 1 ) 2 、C(O)NXNOH、C(O)NXNOR 1 ,C(O)NHSO 2 R 1 <h2 style=";text-align:left;direction:ltr">、C(NH)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)N(R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> )<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )SO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、F、Cl、Br、I、CN、NO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、N<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、OH、C(O)H、CHNOH、CH(NOCH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )、CF<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、C(O)OH、C(O)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr">またはC(O)OR<h2 style=";text-align:left;direction:ltr"> 1A <h2 style=";text-align:left;direction:ltr">であり; B 1 は、H、R 1 , OR 1 ,SR 1 ,S(O)R 1 、SO 2 R 1 , C (O) R 1 ,C(O)OR 1 ,OC(O)R 1 ,NHR 1 ,N (R) 1 ) 2 ,C(O)NHR 1 , C (O) N (R 1 ) 2 ,NHC (O)R 1 ,NR 1 C(O)R 1 ,NHC (O)O 1 ,NR 1 C(O)OR 1 ,NHC(O)NH 2 、NXC(O)NXR 1 、NFC(O)N(R 1 ) 2 ,NR 1 C(O)NHR 1 ,NR 1 C(O)N(R 1 ) 2 、SO 2 NH 2 、SO 2 NHR 1 、SO 2 N (R) 1 ) 2 、NHSO 2 R 1 ,NR 1 SO 2 R 1 、NHSO 2 NHR 1 、NHSO 2 N (R) 1 ) 2 ,NR 1 SO 2 NHR 1 ,NR 1 SO 2 N (R) 1 ) 2 、C(O)NXNOH、C(O)NXNOR 1 ,C(O)NHSO 2 R 1 <h2 style=";text-align:left;direction:ltr">、C(NH)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)N(R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> )<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )SO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、F、Cl、Br、I、CN、NO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、N<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、OH、C(O)H、CHNOH、CH(NOCH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )、CF<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、C(O)OH、C(O)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr">またはC(O)OR<h2 style=";text-align:left;direction:ltr"> 1A <h2 style=";text-align:left;direction:ltr">であり; D 1 は、H、R 1 , OR 1 ,SR 1 ,S(O)R 1 、SO 2 R 1 , C (O) R 1 ,C(O)OR 1 ,OC(O)R 1 ,NHR 1 ,N (R) 1 ) 2 ,C(O)NHR 1 , C (O) N (R 1 ) 2 ,NHC (O)R 1 ,NR 1 C(O)R 1 ,NHC (O)O 1 ,NR 1 C(O)OR 1 ,NHC(O)NH 2 、NXC(O)NXR 1 、NFC(O)N(R 1 ) 2 ,NR 1 C(O)NHR 1 ,NR 1 C(O)N(R 1 ) 2 、SO 2 NH 2 、SO 2 NHR 1 、SO 2 N (R) 1 ) 2 、NHSO 2 R 1 ,NR 1 SO 2 R 1 、NHSO 2 NHR 1 、NHSO 2 N (R) 1 ) 2 ,NR 1 SO 2 NHR 1 ,NR 1 SO 2 N (R) 1 ) 2 、C(O)NXNOH、C(O)NXNOR 1 ,C(O)NHSO 2 R 1 <h2 style=";text-align:left;direction:ltr">、C(NH)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)N(R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> )<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )SO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、F、Cl、Br、I、CN、NO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、N<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、OH、C(O)H、CHNOH、CH(NOCH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )、CF<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、C(O)OH、C(O)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr">またはC(O)OR<h2 style=";text-align:left;direction:ltr"> 1A <h2 style=";text-align:left;direction:ltr">であり; E 1 は、H、R 1 , OR 1 ,SR 1 ,S(O)R 1 、SO 2 R 1 , C (O) R 1 ,C(O)OR 1 ,OC(O)R 1 ,NHR 1 ,N (R) 1 ) 2 ,C(O)NHR 1 , C (O) N (R 1 ) 2 ,NHC (O)R 1 ,NR 1 C(O)R 1 ,NHC (O)O 1 ,NR 1 C(O)OR 1 ,NHC(O)NH 2 、NXC(O)NXR 1 、NFC(O)N(R 1 ) 2 ,NR 1 C(O)NHR 1 ,NR 1 C(O)N(R 1 ) 2 、SO 2 NH 2 、SO 2 NHR 1 、SO 2 N (R) 1 ) 2 、NHSO 2 R 1 ,NR 1 SO 2 R 1 、NHSO 2 NHR 1 、NHSO 2 N (R) 1 ) 2 ,NR 1 SO 2 NHR 1 ,NR 1 SO 2 N (R) 1 ) 2 、C(O)NXNOH、C(O)NXNOR 1 ,C(O)NHSO 2 R 1 , C(NH)NH 2 , C(NH)NH 1 , C(NH)N(R 1 ) 2 N.H.S.O. 2 NHR 1 , N.H.S.O. 2 N (CH 3 ) R 1 , N(CH 3 ) S.O. 2 N (CH 3 ) R 1 , F, Cl, Br, I, CN, NO 2 , N 3 , OH, C(O)H, CHNOH, CH(NOCH 3 ), C.F. 3 , C(O)OH, C(O)NH 2 or C(O)OR 1A and Y 1 H, CN, NO 2 , C(O)OH, F, Cl, Br, I, CF 3 , O.C.F. 3 , C.F. 2 CF 3 , O.C.F. 2 CF 3 , R 17 , OR 17 , C(O)R 17 , C(O)OR 17 , S.R. 17 , S.O. 2 R 17 , N.H. 2 , N.H.R. 17 , N(R 17 ) 2 , NHC(O)R 17 , C(O)NH 2 , C(O)NHR 17 , C(O)N(R 17 ) 2 , N.H.S.(O)R. 17 or NHSO 2 R 17 or E 1 and Y 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; and A 2 、B 1 and D 1 are independently selected from H, R 1 、OR 1 、SR 1 、S(O)R 1 、SO 2 R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 ) 2 、C(O)NHR 1 、C(O)N(R 1 ) 2 、NHCO 1 、NR 1 C(O)R 1 、NHCOOR 1 、NR 1 C(O)OR 1 、NHCONH 2 、NHCONHR 1 、NHCON(R 1 ) 2 、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 ) 2 、SO 2 NH 2 、SO 2 NHR 1 、SO 2 N(R 1 ) 2 、NHSO 2 R 1 、NR 1 SO 2 R 1 、NHSO 2 NHR 1 、NHSO 2 N(R 1 ) 2 、NR 1 SO 2 NHR 1 、NR 1 SO 2 N(R 1 ) 2 、C(O)NHNOH, C(O)NHNOR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(O)NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 1<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)N(R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> )<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )SO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、F、Cl、Br、I、CN、NO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、N<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、OH、C(O)H、CHNOH、CH(NOCH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )、CF<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、C(O)OH、C(O)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr">またはC(O)OR<h2 style=";text-align:left;direction:ltr"> 1A <h2 style=";text-align:left;direction:ltr">であり;または Y 1 and B 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; and A 2 、 D 1 and E 1 are independently selected from H, R 1 , OR 1 , SR 1 , S(O)R 1 , SO 2 R 1 , C(O)R 1 , C(O)OR 1 , OC(O)R 1 , NHR 1 , N(R 1 ), 2 , C(O)NHR 1 , C(O)N(R 1 ), 2 , NHCO)R 1 , NR 1 C(O)R 1 , NHCO)OR 1 , NR 1 C(O)OR 1 , NHCO)NH 2 , NHCO)NHR 1 , NHCO)N(R 1 ), 2 , NR 1 C(O)NHR 1 , NR 1 C(O)N(R 1 ), 2 , SO 2 NH 2 , SO 2 NHR 1 , SO 2 N(R 1 ), 2 , NHSO 2 R 1 , NR 1 SO 2 R 1 , NHSO 2 NHR 1 , NHSO 2 N(R 1 ), 2 , NR 1 SO 2 NHR 1 , NR 1 SO 2 N(R 1 ), 2 , C(O)NHNOH, C(O)NHNOR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(O)NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 1<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)N(R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> )<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )SO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、F、Cl、Br、I、CN、NO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、N<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、OH、C(O)H、CHNOH、CH(NOCH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )、CF<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、C(O)OH、C(O)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr">またはC(O)OR<h2 style=";text-align:left;direction:ltr"> 1A <h2 style=";text-align:left;direction:ltr">であり;または A 2 and B 1 together with the atoms to which they are attached are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; and D 1 、E 1 and Y 1 are independently selected from H, R 1 、OR 1 、SR 1 、S(O)R 1 、SO 2 R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 ) 2 、C(O)NHR 1 、C(O)N(R 1 ) 2 、NH C(O)R 1 、NR 1 C(O)R 1 、NH C(O)OR 1 、NR 1 C(O)OR 1 、NH C(O)NH 2 、NH C(O)NHR 1 、NH C(O)N(R 1 ) 2 、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 ) 2 、SO 2 NH 2 、SO 2 NH R 1 、SO 2 N(R 1 ) 2 、NH SO 2 R 1 、NR 1 SO 2 R 1 、NH SO 2 NH R 1 、NH SO 2 N(R 1 ) 2 、NR 1 SO 2 NH R 1 、NR 1 SO 2 N(R 1 ) 2 、C(O)NHNOH, C(O)NHNOR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(O)NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 1<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)N(R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> )<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )SO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、F、Cl、Br、I、CN、NO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、N<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、OH、C(O)H、CHNOH、CH(NOCH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )、CF<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、C(O)OH、C(O)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr">またはC(O)OR<h2 style=";text-align:left;direction:ltr"> 1A <h2 style=";text-align:left;direction:ltr">であり;または A 2 and D. 1 together with the atoms to which they are attached are benzene, naphthalene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; and B 1 、E 1 and Y 1 are independently selected from H, R 1 、OR 1 、SR 1 、S(O)R 1 、SO 2 R 1 、C(O)R 1 、C(O)OR 1 、OC(O)R 1 、NHR 1 、N(R 1 ) 2 、C(O)NHR 1 、C(O)N(R 1 ) 2 、NH C(O)R 1 、NR 1 C(O)R 1 、NH C(O)OR 1 、NR 1 C(O)OR 1 、NH C(O)NH 2 、NH C(O)NHR 1 、NH C(O)N(R 1 ) 2 、NR 1 C(O)NHR 1 、NR 1 C(O)N(R 1 ) 2 、SO 2 NH 2 、SO 2 NH R 1 、SO 2 N(R 1 ) 2 、NH SO 2 R 1 、NR 1 SO 2 R 1 、NH SO 2 NH R 1 、NH SO 2 N(R 1 ) 2 、NR 1 SO 2 NH R 1 、NR 1 SO 2 N(R 1 ) 2 、C(O)NHNOH, C(O)NHNOR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(O)NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 1<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、C(NH)NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、C(NH)N(R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> )<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> NHR<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、NHSO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )SO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> N(CH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )R<h2 style=";text-align:left;direction:ltr"> 1 <h2 style=";text-align:left;direction:ltr"> 、F、Cl、Br、I、CN、NO<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr"> 、N<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、OH、C(O)H、CHNOH、CH(NOCH<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> )、CF<h2 style=";text-align:left;direction:ltr"> 3 <h2 style=";text-align:left;direction:ltr"> 、C(O)OH、C(O)NH<h2 style=";text-align:left;direction:ltr"> 2 <h2 style=";text-align:left;direction:ltr">またはC(O)OR<h2 style=";text-align:left;direction:ltr"> 1A <h2 style=";text-align:left;direction:ltr">であり; R 1 is R 2 , R 3 , R 4 Or R 5 and R 1A is cycloalkyl, cycloalkenyl, or cycloalkynyl; R 2 is not condensed or R 2A is a phenyl fused to 2A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 3 is not condensed or R 3A is a heteroaryl fused to 3A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 4 are either uncondensed or R 4A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 4A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 5 each is unsubstituted or represents one, two, or three independently selected R 6 , N.C. 6A ) (R 6B ), R 7 , OR 7 , S.R. 7 , S(O)R 7 , S.O. 2 R 7 , N.H.R. 7 , N(R 7 ) 2 , C(O)R 7 , C(O)NH 2 , C(O)NHR 7 , C(O)N(R 7 ) 2 , NHC(O)R 7 , N.R. 7 C(O)R 7 , N.H.S.O. 2 R 7 , NHC(O)OR 7 , S.O. 2 N.H. 2 , S.O. 2 NHR 7 , S.O. 2 N (R 7 ) 2 , NHC(O)NH 2 ,NHC(O)NHR 7 ,NHC(O)CH(CH 3 )NHC(O)CH(CH 3 ) N.H. 2 ,NHC(O)CH(CH 3 )NHC(O)CH(CH 3 ) N.H.R. 7 , OH, (O), C(O)OH, N 3 , C.N., N.H. 2 , C.F. 3 , C.F. 2 CF 3 , alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 6 are unsubstituted or OH, (O), N 3 , C.N., C.F. 3 , C.F. 2 CF 3 , F, Cl, Br, I, NH 2 , NH(CH 3 ) or N(CH 3 ) 2 C substituted with 2 -C 5 is a spiroalkyl; R 6A and R 6B are independently selected alkyl or together with the N to which they are attached represent R 6C and R 6C is aziridin-1-yl, azetidin-1-yl, pyrrolidin-1-yl or piperidin-1-yl, each of which is unsubstituted or O, C(O), CNOH, CNOCH 3 ,S,S(O),SO 2 or one CH replaced by NH 2 portion; R 7 is R 8 , R 9 , R 10 Or R 11 and R 8 Is not condensed or R 8A is a phenyl fused to 8A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 9 is not condensed or R 9A is a heteroaryl fused to 9A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 10 are either uncondensed or R 10A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 10A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 11 each is unsubstituted or represents one, two, or three independently selected R 12 , OR 12 , S.R. 12 , S(O)R 12 , S.O. 2 R 12 , C(O)R 12 , CO(O)R 12 , O.C.(O)R 12 , O C (O) O R 12 , N.H. 2 , N.H.R. 12 , N(R 12 ) 2 , NHC(O)R 12 , N.R. 12 C(O)R 12 , N.H.S. (O) 2 R 12 , N.R. 12 S (O) 2 R 12 , NHC(O)OR 12 , N.R. 12 C(O)OR 12 , NHC(O)NH 2 ,NHC(O)NHR 12 ,NHC(O)N(R 12 ) 2 , N.R. 12 C(O)NHR 12 , N.R. 12 C(O)N(R 12 ) 2 , C(O)NH 2 , C(O)NHR 12 , C(O)N(R 12 ) 2 , C(O)NHOH, C(O)NHOR 12 , C(O)NHSO 2 R 12 , C(O)NR 12 SO 2 R 12 , S.O. 2 N.H. 2 , S.O. 2 NHR 12 , S.O. 2 N (R 12 ) 2 , C(O)H, C(O)OH, C(N)NH 2 , C(N)NHR 12 , C(N)N(R 12 ) 2 ,CNOH,CNOCH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 12 is R 13 , R 14 , R 15 Or R 16 and R 13 is not condensed or R 13A is a phenyl fused to 13A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 14 is not condensed or R 14A is a heteroaryl fused to 14A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 15 are either uncondensed or R 15A is a cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene fused with 15A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 16 is alkyl, alkenyl or alkynyl; R 17 is R 18 , R 19 , R 20 Or R 21 and R 18 Is not condensed or R 18A is a phenyl fused to 18A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 19 Is not condensed or R 19A is a heteroaryl fused to 19A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 20 are either uncondensed or R 20A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 20A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 21 each is unsubstituted or represents one, two, or three independently selected R 22 , OR 22 , S.R. 22 , S(O)R 22 , S.O. 2 R 22 , C(O)R 22 , CO(O)R 22 , O.C.(O)R 22 , O C (O) O R 22 , N.H. 2 , N.H.R. 22 , N(R 22 ) 2 , NHC(O)R 22 , N.R. 22 C(O)R 22 , N.H.S. (O) 2 R 22 , N.R. 22 S (O) 2 R 22 , NHC(O)OR 22 , N.R. 22 C(O)OR 22 , NHC(O)NH 2 ,NHC(O)NHR 22 ,NHC(O)N(R 22 ) 2 , N.R. 22 C(O)NHR 22 , N.R. 22 C(O)N(R 22 ) 2 , C(O)NH 2 , C(O)NHR 22 , C(O)N(R 22 ) 2 , C(O)NHOH, C(O)NHOR 22 , C(O)NHSO 2 R 22 , C(O)NR 22 SO 2 R 22 , S.O. 2 N.H. 2 , S.O. 2 NHR 22 , S.O. 2 N (R 22 ) 2 , C(O)H, C(O)OH, C(N)NH 2 , C(N)NHR 22 , C(N)N(R 22 ) 2 ,CNOH,CNOCH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 22 is R 23 , R 24 Or R 25 and R 23 is not condensed or R 23A is a phenyl fused to 23A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 24 is not condensed or R 24A R is a heteroarene fused to 24A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 25 are either uncondensed or R 25A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 25A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; Z 2 is R 28 , R 29 Or R 30 and L 1 は、R 37 、OR 37 、S 37 、S(O)R 37 、SO 2 R 37 、C(O)R 37 、CO(O)R 37 、OC(O)R 37 、OC(O)OR 37 、NHYR 37 、C(O)NH、C(O)NR 37 、C(O)NHOR 37 、C(O)NHSO 2 R 37 、SO 2 NH、SO 2 NER 37 、C(N)NH、C(N)NHR 37 ; R 28 is not condensed or R 28A R is a phenylene fused to 28A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 29 is not condensed or R 29A R is a heteroarylene fused to 29A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 30 are either uncondensed or R 30A is a cycloalkylene, cycloalkenylene, heterocyclic alkylene, or heterocyclic alkenylene fused with 30A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 37 is a bond or R 37A and R 37A each is unsubstituted or represents one, two, or three independently selected R 37B , OR 37B , S.R. 37B , S(O)R 37B , S.O. 2 R 37B , C(O)R 37B , CO(O)R 37B , O.C.(O)R 37B , O C (O) O R 37B , N.H. 2 , N.H.R. 37B , N(R 37B ) 2 , NHC(O)R 37B , N.R. 37B C(O)R 37B , N.H.S. (O) 2 R 37B , N.R. 37B S (O) 2 R 37B , NHC(O)OR 37B , N.R. 37B C(O)OR 37B , NHC(O)NH 2 ,NHC(O)NHR 37B ,NHC(O)N(R 37B ) 2 , N.R. 37B C(O)NHR 37B , N.R. 37B C(O)N(R 37B ) 2 , C(O)NH 2 , C(O)NHR 37B , C(O)N(R 37B ) 2 , C(O)NHOH, C(O)NHOR 37B , C(O)NHSO 2 R 37B , C(O)NR 37B SO 2 R 37B , S.O. 2 N.H. 2 , S.O. 2 NHR 37B , S.O. 2 N (R 37B ) 2 , C(O)H, C(O)OH, C(N)NH 2 , C(N)NHR 37B , C(N)N(R 37B ) 2 ,CNOH,CNOCH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , alkylene, alkenylene or alkynylene substituted with F, Cl, Br and I substituents; R 37B is alkyl, alkenyl, alkynyl or R 37C and R 37C is phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; Z 3 is R 38 , R 39 Or R 40 and R 38 Is not condensed or R 38A is a phenyl fused to 38A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 39 Is not condensed or R 39A is a heteroaryl fused to 39A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 40 are either uncondensed or R 40A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 40A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; E 1 and Y 1 is one, Y 1 and B 1 is one, A 2 and B 1 is one, A 2 and D. 1 is one, R 1A , R 2 , R 2A , R 3 , R 3A , R 4 , R 4A , R 6 , R 6C , R 8 , R 8A , R 9 , R 9A , R 10 , R 10A , R 13 , R 13A , R 14 , R 14A , R 15 , R 15A , R 18 , R 18A , R 19 , R 19A , R 20 , R 20A , R 23 , R 23A , R 24 , R 24A , R 25 , R 25A , R 26 , R 26A , R 27 , R 27A , R 28 , R 28A , R 29 , R 29A , R 30 , R 30A , R 37B , R 38 , R 38A , R 39 , R 39A , R 40 and R 40A The cyclic moiety represented by is independently unsubstituted, further unsubstituted, or contains 1 or 2 or 3 or 4 or 5 independently selected R 57A , R 57 , OR 57 ,SR 57 ,S(O)R 57 、SO 2 R 57 , C (O) R 57 ,CO(O)R 57 ,OC(O)R 57 ,OC(O)OR 57 ,NH 2 ,NHR 57 ,N (R) 57 ) 2 ,NHC (O)R 57 ,NR 57 C(O)R 57 ,NHS (O) 2 R 57 ,NR 57 S (O) 2 R 57 ,NHC (O)O 57 ,NR 57 C(O)OR 57 ,NHC(O)NH 2 、NXC(O)NXR 57 、NFC(O)N(R 57 ) 2 ,NR 57 C(O)NHR 57 ,NR 57 C(O)N(R 57 ) 2 ,C(O)NH 2 ,C(O)NHR 57 , C (O) N (R 57 ) 2 、C(O)NHOH、C(O)NHOR 57 ,C(O)NHSO 2 R 57 ,C(O)NR 57 SO 2 R 57 、SO 2 NH 2 、SO 2 NHR 57 、SO 2 N (R) 57 ) 2 、C(O)H、C(O)OH、C(N)NH 2 ,C(N)NHR 57 , C (N) N (R 57 ) 2 ,CNOH,CNOH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , substituted or further substituted with F, Cl, Br or I; R 57A is spiroalkyl or heterospiroalkyl; R 57 is R 58 , R 59 , R 60 Or R 61 and R 58 Is not condensed or R 58A is a phenyl fused to 58A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 59 Is not condensed or R 59A is a heteroaryl fused to 59A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 60 Each is either uncondensed or R 60A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 60A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 61 each is unsubstituted or represents one, two, or three independently selected R 62 , OR 62 , S.R. 62 , S(O)R 62 , S.O. 2 R 62 , C(O)R 62 , CO(O)R 62 , O.C.(O)R 62 , O C (O) O R 62 , N.H. 2 , N.H.R. 62 , N(R 62 ) 2 , NHC(O)R 62 , N.R. 62 C(O)R 62 , N.H.S. (O) 2 R 62 , N.R. 62 S (O) 2 R 62 , NHC(O)OR 62 , N.R. 62 C(O)OR 62 , NHC(O)NH 2 ,NHC(O)NHR 62 ,NHC(O)N(R 62 ) 2 , N.R. 62 C(O)NHR 62 , N.R. 62 C(O)N(R 62 ) 2 , C(O)NH 2 , C(O)NHR 62 , C(O)N(R 62 ) 2 , C(O)NHOH, C(O)NHOR 62 , C(O)NHSO 2 R 62 , C(O)NR 62 SO 2 R 62 , S.O. 2 N.H. 2 , S.O. 2 NHR 62 , S.O. 2 N (R 62 ) 2 , C(O)H, C(O)OH, C(N)NH 2 , C(N)NHR 62 , C(N)N(R 62 ) 2 ,CNOH,CNOCH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 62 is R 63 , R 64 , R 65 Or R 66 and R 63 Is not condensed or R 63A is a phenyl fused to 63A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 64 Is not condensed or R 64A is a heteroaryl fused to 64A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 65 Each is either uncondensed or R 65A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 65A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 66 each is unsubstituted or represents one, two, or three independently selected R 67 , OR 67 , S.R. 67 , S(O)R 67 , S.O. 2 R 67 , C(O)R 67 , CO(O)R 67 , O.C.(O)R 67 , O C (O) O R 67 , N.H. 2 , N.H.R. 67 , N(R 67 ) 2 , NHC(O)R 67 , N.R. 67 C(O)R 67 , N.H.S. (O) 2 R 67 , N.R. 67 S (O) 2 R 67 , NHC(O)OR 67 , N.R. 67 C(O)OR 67 , NHC(O)NH 2 ,NHC(O)NHR 67 ,NHC(O)N(R 67 ) 2 , N.R. 67 C(O)NHR 67 , N.R. 67 C(O)N(R 67 ) 2 , C(O)NH 2 , C(O)NHR 67 , C(O)N(R 67 ) 2 , C(O)NHOH, C(O)NHOR 67 , C(O)NHSO 2 R 67 , C(O)NR 67 SO 2 R 67 , S.O. 2 N.H. 2 , S.O. 2 NHR 67 , S.O. 2 N (R 67 ) 2 , C(O)H, C(O)OH, C(N)NH 2 , C(N)NHR 67 , C(N)N(R 67 ) 2 ,CNOH,CNOCH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I substituents; R 67 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; R 57A , R 58 , R 59 , R 60 , R 63 , R 64 , R 65 and R 67 The cyclic moiety represented by the formula (I) is unsubstituted or contains one or two or three or four independently selected R 68 , OR 68 , S.R. 68 , S(O)R 68 , S.O. 2 R 68 , C(O)R 68 , CO(O)R 68 , O.C.(O)R 68 , O C (O) O R 68 , N.H. 2 , N.H.R. 68 , N(R 68 ) 2 , NHC(O)R 68 , N.R. 68 C(O)R 68 , N.H.S. (O) 2 R 68 , N.R. 68 S (O) 2 R 68 , NHC(O)OR 68 , N.R. 68 C(O)OR 68 , NHC(O)NH 2 ,NHC(O)NHR 68 ,NHC(O)N(R 68 ) 2 , N.R. 68 C(O)NHR 68 , N.R. 68 C(O)N(R 68 ) 2 , C(O)NH 2 , C(O)NHR 68 , C(O)N(R 68 ) 2 , C(O)NHOH, C(O)NHOR 68 , C(O)NHSO 2 R 68 , C(O)NR 68 SO 2 R 68 , S.O. 2 N.H. 2 , S.O. 2 NHR 68 , S.O. 2 N (R 68 ) 2 , C(O)H, C(O)OH, C(N)NH 2 , C(N)NHR 68 , C(N)N(R 68 ) 2 ,CNOH,CNOCH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , substituted with F, Cl, Br or I; R 68 is R 69 , R 70 , R 71 Or R 72 and R 69 Is not condensed or R 69A is a phenyl fused to 69A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 70 is not condensed or R 70A is a heteroaryl fused to 70A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 71 are either uncondensed or R 71A is a cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl fused to 71A is benzene, heteroarene, cycloalkane, cycloalkene, heterocyclic alkane, or heterocyclic alkene; R 72 each is unsubstituted or represents one, two, or three independently selected R 73 , OR 73 , S.R. 73 , S(O)R 73 , S.O. 2 R 73 , C(O)R 73 , CO(O)R 73 , O.C.(O)R 73 , O C (O) O R 73 , N.H. 2 , N.H.R. 73 , N(R 73 ) 2 , NHC(O)R 73 , N.R. 73 C(O)R 73 , N.H.S. (O) 2 R 73 , N.R. 73 S (O) 2 R 73 , NHC(O)OR 73 , N.R. 73 C(O)OR 73 , NHC(O)NH 2 ,NHC(O)NHR 73 ,NHC(O)N(R 73 ) 2 , N.R. 73 C(O)NHR 73 , N.R. 73 C(O)N(R 73 ) 2 , C(O)NH 2 , C(O)NHR 73 , C(O)N(R 73 ) 2 , C(O)NHOH, C(O)NHOR 73 , C(O)NHSO 2 R 73 , C(O)NR 73 SO 2 R 73 , S.O. 2 N.H. 2 , S.O. 2 NHR 73 , S.O. 2 N (R 73 ) 2 , C(O)H, C(O)OH, C(N)NH 2 , C(N)NHR 73 , C(N)N(R 73 ) 2 ,CNOH,CNOCH 3 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , alkyl, alkenyl or alkynyl substituted with F, Cl, Br or I; R 73 is alkyl, alkenyl, alkynyl, phenyl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or heterocycloalkenyl; and R 69 , R 70 and R 71 is unsubstituted or is substituted with 1 or 2 or 3 or 4 independently selected NH 2 , C(O)NH 2 ,C(O)NHOH,SO 2 N.H. 2 , C.F. 3 , C.F. 2 CF 3 , C(O)H, C(O)OH, C(N)NH 2 , OH, (O), CN, N 3 , NO 2 , C.F. 3 , C.F. 2 CF 3 , O.C.F. 3 , O.C.F. 2 CF 3 , substituted with F, Cl, Br or I.
3. G 1 is H; A 1 is N or C (A 2 ) and A 2 is H 2. The compound of claim 1.
4. G 1 is H; A 1 is N or C (A 2 ) and A 2 is H; and B 1 NHR 1 is 2. The compound of claim 1.
5. G 1 is H; A 1 is N or C (A 2 ) and A 2 is H; B 1 NHR 1 and D 1 is H 2. The compound of claim 1.
6. G 1 is H; A 1 is N or C (A 2 ) and A 2 is H; B 1 NHR 1 and D 1 is H; and E 1 is H 2. The compound of claim 1.
7. G 1 is H; A 1 is N or C (A 2 ) and A 2 is H; B 1 NHR 1 and D 1 is H; E 1 is H; and Y 1 No 2 is 2. The compound of claim 1.
8. The compound is 4-{4-[(4'-chloro-1,1'-biphenyl-2-yl)methyl]piperazin-1-yl}-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-{4-[(4'-chloro-1,1'-biphenyl-2-yl)methyl]piperazin-1-yl}-N-({4-[(3-morpholin-4-ylpropyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-tetrahydro-2H-pyran-4-ylpiperidin-4-yl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-methylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methylpiperazin-1-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2-methoxyethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-tetrahydro-2H-pyran-3-ylmethyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-(1,4-dioxan-2-ylmethoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3R)-tetrahydro-2H-pyran-3-ylmethyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-(2-naphthylsulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2-methoxyethyl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-({4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-(tetrahydro-2H-pyran-4-ylmethoxy)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1,4-dioxan-2-ylmethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(2,2,2-trifluoroethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(3,3,3-trifluoropropyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2S)-1,4-dioxan-2-ylmethoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; cis-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2R)-1,4-dioxan-2-ylmethoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(1,4-dioxan-2-ylmethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-{[4-(1,4-dioxan-2-ylmethoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-{[5-cyano-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-cyano-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-{[3-(aminocarbonyl)-4-(tetrahydro-2H-pyran-4-ylmethoxy)phenyl]sulfonyl}-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; cis-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-chloro-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-{[5-chloro-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-{[4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]-3-(trifluoromethyl)phenyl]sulfonyl}benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-({4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)benzamide; trans-4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(1-methylpiperidin-4-yl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 5-({[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]amino}sulfonyl)-2-(tetrahydro-2H-pyran-4-ylmethoxy)nicotinamide; N-({5-bromo-6-[(1-methylpiperidin-4-yl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-methylpiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-cyano-6-(1,4-dioxan-2-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-{[5-bromo-6-(1,4-dioxan-2-ylmethoxy)pyridin-3-yl]sulfonyl}-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2,2-dimethyltetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-5-cyano-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({4-[(1-acetylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({2-chloro-5-fluoro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(3-morpholin-4-ylpropyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-cyano-6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-cyano-6-(2-morpholin-4-ylethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[2-(2-methoxyethoxy)ethyl]sulfonyl}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[2-(2-methoxyethoxy)ethyl]sulfonyl}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)oxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-bromo-6-[(1-tetrahydro-2H-pyran-4-ylpiperidin-4-yl)amino]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(2-cyanoethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; cis-4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-N-{[4-({4-[bis(cyclopropylmethyl)amino]cyclohexyl}amino)-3-nitrophenyl]sulfonyl}-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1-methylpiperidin-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(morpholin-3-ylmethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-({4-[(4-methylpiperazin-1-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylbut-2-ynyl)oxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-ethynyl-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-oxo-3,4-dihydroquinazolin-6-yl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[8-(4-chlorophenyl)spiro[4.5]dec-7-en-7-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; cis-4-(4-{[4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[8-(4-chlorophenyl)spiro[4.5]dec-7-en-7-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[8-(4-chlorophenyl)spiro[4.5]dec-7-en-7-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-cyano-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 3-{[4-({[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]amino}sulfonyl)-2-nitrophenoxy]methyl}morpholine-4-carboxylate tert-butyl; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-(morpholin-3-ylmethoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[8-(4-chlorophenyl)spiro[4.5]dec-7-en-7-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[1-(methylsulfonyl)piperidin-4-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1,1-dioxidetetrahydro-2H-thiopyran-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-chloro-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[1-(2,2,2-trifluoroethyl)piperidin-4-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-cyano-6-[(1-tetrahydro-2H-pyran-4-ylpiperidin-4-yl)oxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-isopropyl-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-5-fluoro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; and therapeutically acceptable salts and metabolites thereof; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({1-[2-fluoro-1-(fluoromethyl)ethyl]piperidin-4-yl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[1-(2,2-difluoroethyl)piperidin-4-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-cyclopropylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1-morpholin-4-ylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-(dicyclopropylamino)cyclohexyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-6,6-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-bromo-6-[(4-ethylmorpholin-3-yl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-ethylmorpholin-3-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(4-tetrahydro-2H-pyran-4-ylmorpholin-3-yl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-1-tetrahydro-2H-pyran-4-ylpiperidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-cyano-6-[(tetrahydro-2H-pyran-4-ylmethyl)amino]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1,1-dioxidothiomorpholin-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(4-aminotetrahydro-2H-pyran-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-cyano-6-[(4-morpholin-4-ylcyclohexyl)amino]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-cyano-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1S,3R)-3-morpholin-4-ylcyclopentyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1R,3S)-3-morpholin-4-ylcyclopentyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(morpholin-2-ylmethyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydrofuran-3-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({1-[cis-3-fluorotetrahydro-2H-pyran-4-yl]piperidin-4-yl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-tetrahydro-2H-pyran-4-ylazetidin-3-yl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-tetrahydrofuran-3-ylazetidin-3-yl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3R)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4- [(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)-N-(4-((trans-4-hydroxycyclohexyl)methoxy)-3-nitrophenylsulfonyl)benzamide; 2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)-N-(4-((cis-4-methoxycyclohexyl)methoxy)-3-nitrophenylsulfonyl)benzamide; cis-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-(cyclopropylamino)cyclohexyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[4-(tetrahydro-2H-pyran-4-ylamino)cyclohexyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-N-({5-bromo-6-[(4-morpholin-4-ylcyclohexyl)oxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methoxycyclohexyl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-{[4-({[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]amino}sulfonyl)-2-nitrophenoxy]methyl}-4-fluoropiperidine-1-carboxylate tert-butyl; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluoropiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[4-(4-tetrahydro-2H-pyran-4-ylpiperazin-1-yl)cyclohexyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({1-[2-fluoro-1-(fluoromethyl)ethyl]piperidin-4-yl}methoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3R)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(2,2-dimethyltetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3S)-1-(2,2-dimethyltetrahydro-2H-pyran-4-yl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methylmorpholin-2-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(2-methoxyethyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(4-acetylmorpholin-2-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[trans-4-(fluoromethyl)-1-oxetan-3-ylpyrrolidin-3-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-oxetan-3-ylpiperidin-4-yl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-cyclobutylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[1-(2,2-dimethyltetrahydro-2H-pyran-4-yl)piperidin-4-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3S)-1-cyclopropylpyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-tetrahydrofuran-3-ylpiperidin-4-yl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-cyclopropylpyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3S)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(3-hydroxy-2,2-dimethylpropyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[1-(methylsulfonyl)piperidin-3-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(1-acetylpiperidin-3-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(methylsulfonyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-3,3-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({1-[2-fluoro-1-(fluoromethyl)ethyl]azetidin-3-yl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[1-(methylsulfonyl)pyrrolidin-3-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(1-acetylpyrrolidin-3-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(3R)-1-acetylpyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(3-methoxy-2,2-dimethylpropyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(1R,3R)-3-hydroxycyclopentyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(1S,3S)-3-hydroxycyclopentyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(1S,3R)-3-hydroxycyclopentyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(1R,3S)-3-hydroxycyclopentyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-2-oxopiperidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[({1-[2-fluoro-1-(fluoromethyl)ethyl]azetidin-3-yl}methyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(1-oxetan-3-ylazetidin-3-yl)methyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(1-oxetan-3-ylpiperidin-4-yl)methyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1-cyclopropylpiperidin-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(2-fluoroethyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(2,2-difluoroethyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluoro-1-oxetan-3-ylpiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(2S)-4,4-difluoro-1-oxetan-3-ylpyrrolidin-2-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(4-tetrahydro-2H-pyran-4-ylmorpholin-3-yl)methyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-cyclobutylmorpholin-3-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(4-tetrahydrofuran-3-ylmorpholin-3-yl)methyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[({1-[2-fluoro-1-(fluoromethyl)ethyl]piperidin-4-yl}methyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-cyclopropyl-4-fluoropiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methoxybenzyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[3-(trifluoromethoxy)benzyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(3-methoxybenzyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-(difluoromethoxy)benzyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-(1,4-dioxaspiro[4.5]dec-8-ylamino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-N-[(4-{[4-(acetylamino)cyclohexyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(2,2-difluoroethyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3S)-1-(2-fluoroethyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3S)-1-(2,2-difluoroethyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(2-fluoroethyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-1-oxetan-3-ylpyrrolidin-3-yl]methoxy}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-hydroxybenzyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(3-hydroxybenzyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[3-(difluoromethoxy)benzyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[cis-3-morpholin-4-ylcyclopentyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({4-[(methylsulfonyl)amino]cyclohexyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-cyclopropylpiperidin-4-yl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(1-oxetan-3-ylpiperidin-4-yl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluoro-1-tetrahydro-2H-pyran-4-ylpiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluoro-1-tetrahydrofuran-3-ylpiperidin-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-fluoro-1-(methylsulfonyl)piperidin-4-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3R)-1-oxetan-3-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-hydroxycyclohexyl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({4-[3-(dimethylamino)propoxy]benzyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-(2-morpholin-4-ylethoxy)benzyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(E)-4-hydroxy-1-adamantyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(Z)-4-hydroxy-1-adamantyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({4-[(1S,4S)-bicyclo[2.2.1]hept-5-en-2-ylmethoxy]-3-nitrophenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-methyl-5-oxopyrrolidin-3-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1R,4R,5R,6S)-5,6-dihydroxybicyclo[2.2.1]hept-2-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1R,4R,5S,6R)-5,6-dihydroxybicyclo[2.2.1]hept-2-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(3-oxocyclohexyl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohexa-1,3-dien-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({(3R)-1-[2-fluoro-1-(fluoromethyl)ethyl]pyrrolidin-3-yl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-5-(trifluoromethyl)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3S)-1-oxetan-3-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-N-({5-chloro-6-[(4-methoxycyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; cis-N-({5-chloro-6-[(4-methoxycyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-1-oxetan-3-ylpyrrolidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[({4-[2-(2-methoxyethoxy)ethyl]morpholin-2-yl}methyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(cyanomethyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(N,N-dimethylglycyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; (2-{[(4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}-2-nitrophenyl)amino]methyl}morpholin-4-yl)acetic acid; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[4-(oxetan-3-yl)morpholin-2-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-cyclopropylmorpholin-2-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-(methylsulfonyl)-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methyltetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; Ethyl 4-(4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}-2-nitrophenyl)piperazine-1-carboxylate; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[4-(morpholin-4-yl)piperidin-1-yl]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3R)-1-(oxetan-3-yl)pyrrolidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(1,3-difluoropropan-2-yl)pyrrolidin-3-yl]amino}-3-[(trifluoromethyl)sulfonyl]phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(1-isopropylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({4-[(1-tert-butylpiperidin-4-yl)amino]-3-nitrophenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[1-(2-methoxyethyl)piperidin-3-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[1-(cyanomethyl)piperidin-3-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluoro-1-methylpiperidin-4-yl)methoxy]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(3R)-1-(1,3-difluoropropan-2-yl)pyrrolidin-3-yl]amino}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; tert-butyl 4-[(4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}-2-nitrophenyl)amino]piperazine-1-carboxylate; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-(pentafluoro-λ 6 -sulfanyl)-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methoxytetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(1,3-difluoropropan-2-yl)pyrrolidin-3-yl]oxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[4-(oxetan-3-yl)piperazin-1-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(3R)-tetrahydrofuran-3-ylamino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4,4-difluorocyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({4-[(1-tert-butylpiperidin-4-yl)amino]-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-({[4-(oxetan-3-yl)morpholin-2-yl]methyl}amino)-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(4-fluorotetrahydro-2H-pyran-4-yl)methyl]amino}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(1-cyclopropylpiperidin-4-yl)amino]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(2S)-4-(cyanomethyl)morpholin-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(2S)-4-(N,N-dimethylglycyl)morpholin-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(2R)-4-(cyanomethyl)morpholin-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(2R)-4-(N,N-dimethylglycyl)morpholin-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-fluoro-6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[3-hydroxy-2-(hydroxymethyl)-2-methylpropoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(1,3-difluoropropan-2-yl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(cyanomethyl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({(3R)-1-[2-(2-methoxyethoxy)ethyl]pyrrolidin-3-yl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(N,N-dimethylglycyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[1-(oxetan-3-yl)azetidin-3-yl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(cyanomethyl)-4-fluoropiperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(2R)-4-(N,N-dimethylglycyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(2S)-4-(N,N-dimethylglycyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(N,N-dimethylglycyl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(3R)-1-(2,2-difluoroethyl)pyrrolidin-3-yl]oxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(cyanomethyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-{4-[(4'-chlorobiphenyl-2-yl)methyl]-4-methoxypiperidin-1-yl}-N-({5-chloro-6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-{4-[(4'-chlorobiphenyl-2-yl)methyl]-4-methoxypiperidin-1-yl}-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[9-(4-chlorophenyl)-3-(1,3-difluoropropan-2-yl)-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[9-(4-chlorophenyl)-3-isopropyl-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[9-(4-chlorophenyl)-3-(1,3-difluoropropan-2-yl)-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-N-{[5-chloro-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[9-(4-chlorophenyl)-3-isopropyl-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-N-{[5-chloro-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(4-fluoro-1-methylpiperidin-4-yl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(N,N-dimethylglycyl)-4-fluoropiperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-{4-[(4'-chlorobiphenyl-2-yl)methyl]-4-fluoropiperidin-1-yl}-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-{4-[(4'-chlorobiphenyl-2-yl)methyl]-4-fluoropiperidin-1-yl}-N-({5-chloro-6-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[9-(4-chlorophenyl)-3-isopropyl-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-({4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]-3-(trifluoromethyl)phenyl}sulfonyl)benzamide; N-[(5-chloro-6-{[(3R)-1-(1,3-difluoropropan-2-yl)pyrrolidin-3-yl]oxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[2-(tetrahydrofuran-3-yloxy)ethoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-cyanocyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[4-fluoro-1-(oxetan-3-yl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-cyano-6-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-(3-furylmethoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(3R)-1-(1,3-difluoropropan-2-yl)pyrrolidin-3-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(3R)-1-(2,2-difluoroethyl)pyrrolidin-3-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(1,3-difluoropropan-2-yl)-4-fluoropiperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-4-[(4-fluoro-1-methylpiperidin-4-yl)methoxy]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-cyano-4-(tetrahydro-2H-pyran-4-ylmethoxy)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(2,2-difluoroethyl)-4-fluoropiperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(4,4-difluorocyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[6-{[1-(1,3-difluoropropan-2-yl)-4-fluoropiperidin-4-yl]methoxy}-5-(trifluoromethyl)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-chloro-6-[2-(tetrahydrofuran-2-yl)ethoxy]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}-3-methylpiperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[3-(cyclopropylamino)propyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-{[5-chloro-6-(2-methoxyethoxy)pyridin-3-yl]sulfonyl}-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-fluoro-6-(tetrahydro-2H-pyran-4-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[1-(methoxyacetyl)piperidin-4-yl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[1-(N,N-dimethylglycyl)piperidin-4-yl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohexyl]methyl}piperidin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-{[6-(tetrahydro-2H-pyran-4-ylmethoxy)-5-(trifluoromethyl)pyridin-3-yl]sulfonyl}benzamide; N-({5-chloro-6-[(trans-4-hydroxycyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-cyano-4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({6-[(trans-4-methoxycyclohexyl)methoxy]-5-(trifluoromethyl)pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({6-[(cis-4-methoxycyclohexyl)methoxy]-5-(trifluoromethyl)pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(4,4-difluoro-1-hydroxycyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperidin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[trans-4-(morpholin-4-yl)cyclohexyl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(1,3-thiazol-5-ylmethyl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-4-[(trans-4-hydroxycyclohexyl)methoxy]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-chloro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-(trifluoromethyl)phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(2,2,2-trifluoroethyl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[1-(oxetan-3-yl)piperidin-4-yl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3,5-difluoro-4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(oxetan-3-yl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[1-(1-methyl-L-prolyl)piperidin-4-yl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3,4-difluoro-5-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(2S)-4-cyclopropylmorpholin-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperidin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperidin-1-yl)-N-{[3-chloro-4-(tetrahydro-2H-pyran-4-ylmethoxy)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 2-{[(4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}-2-nitrophenyl)amino]methyl}morpholine-4-carboxylate methyl; 2-{[(4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}-2-nitrophenyl)amino]methyl}-N-ethyl-N-methylmorpholine-4-carboxamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(methylsulfonyl)morpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclobutyl(cyclopropyl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-difluorocyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[4-fluoro-1-(oxetan-3-yl)piperidin-4-yl]methoxy}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-chloro-4-(tetrahydrofuran-3-ylmethoxy)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-difluorocyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-hydroxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]phenyl}sulfonyl)-4-(4-{[9-(4-chlorophenyl)-3-(oxetan-3-yl)-3-azaspiro[5.5]undec-8-en-8-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(2R)-4-cyclopropylmorpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[(2S)-4-cyclopropylmorpholin-2-yl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[5-(4-chlorophenyl)spiro[2.5]oct-5-en-6-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-{[5-chloro-6-({4-[cyclopropyl(oxetan-3-yl)amino]cyclohexyl}methoxy)pyridin-3-yl]sulfonyl}-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[5-(4-chlorophenyl)spiro[2.5]oct-5-en-6-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-cyclopropylmorpholin-2-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-4-[(4-cyclopropylmorpholin-2-yl)methoxy]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(3-chloro-4-{[(4-cyclopropylmorpholin-2-yl)methyl]amino}phenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 2-{[(2-chloro-4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}phenyl)amino]methyl}-N-ethyl-N-methylmorpholine-4-carboxamide; (2S)-2-{[(3-chloro-5-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}pyridin-2-yl)oxy]methyl}-N-ethyl-N-methylmorpholine-4-carboxamide; N-[(5-chloro-6-{[(4-cyclopropylmorpholin-2-yl)methyl]amino}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 2-{[(3-chloro-5-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}pyridin-2-yl)amino]methyl}-N-ethyl-N-methylmorpholine-4-carboxamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(cis-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(1R,2R,4R,5R)-5-hydroxy-5-methylbicyclo[2.2.1]hept-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({4-[(2-cyanoethyl)(cyclopropyl)amino]cyclohexyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(trans-4-hydroxy-4-methylcyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[5-(4-chlorophenyl)spiro[2.5]oct-5-en-6-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-chloro-6-(5,6,7,8-tetrahydroimidazo[1,2-a]pyridin-6-ylmethoxy)pyridin-3-yl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(1R,2S,4R,5R)-5-hydroxy-5-methylbicyclo[2.2.1]hept-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(cis-4-hydroxy-4-methylcyclohexyl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[4-fluoro-1-(oxetan-3-yl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[5-(4-chlorophenyl)spiro[2.5]oct-5-en-6-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[4-(3,3-difluoropyrrolidin-1-yl)cyclohexyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(trans-4-hydroxy-4-methylcyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(cis-4-hydroxy-4-methylcyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({4-[(2,2-difluorocyclopropyl)amino]cyclohexyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(cis-1-fluoro-4-hydroxycyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-(2-oxaspiro[3.5]non-7-ylmethoxy)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(trans-4-hydroxy-4-methylcyclohexyl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5,5-bis(fluoromethyl)cyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-cyclopropylmorpholin-2-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(trans-1-fluoro-4-hydroxy-4-methylcyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-chloro-6-[(cis-1-fluoro-4-hydroxy-4-methylcyclohexyl)methoxy]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-cyano-4-{[4-fluoro-1-(oxetan-3-yl)piperidin-4-yl]methoxy}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-ethyl-4-hydroxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(cis-4-ethyl-4-hydroxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5-(methoxymethyl)-5-methylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(2S)-4-(oxetan-3-yl)morpholin-2-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({3-chloro-4-[(trans-4-hydroxy-4-methylcyclohexyl)methoxy]phenyl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({4-[(2-cyanoethyl)(cyclopropyl)amino]-1-fluorocyclohexyl}methoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({5-nitro-6-[(tetrahydro-2H-pyran-4-ylmethyl)amino]pyridin-3-yl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(2-oxaspiro[3.5]non-7-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-cyano-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; Pivalic acid {[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)amino}methyl; Butyric acid {[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)amino}methyl; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-N-{[3-(tetrahydro-2H-pyran-4-ylmethyl)-3H-[1,2,3]triazolo[4,5-b]pyridin-6-yl]sulfonyl}benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(6-{[(trans-4-hydroxy-4-methylcyclohexyl)methyl]amino}-5-nitropyridin-3-yl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(5-cyano-6-{[4-fluoro-1-(oxetan-3-yl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-(4-{[4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl}-2-nitrophenyl)morpholine-4-carboxamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({[4-(methoxymethyl)cyclohexyl]methyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(5-chloro-6-{[1-(1,3-thiazol-2-yl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(6-{[(cis-4-hydroxy-4-methylcyclohexyl)methyl]amino}-5-nitropyridin-3-yl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5-methoxy-5-methylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5-methoxy-5-methylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; and therapeutically acceptable salts and metabolites thereof.
3. The compound of claim 1 or claim 2 selected from:
9. The compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharma- ceutically acceptable salt thereof.
10. The compound trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-morpholin-4-ylcyclohexyl)amino]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharma- ceutically acceptable salt thereof.
11. The compound cis-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharma- ceutically acceptable salt thereof.
12. The compound trans-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methoxycyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharma- ceutically acceptable salt thereof.
13. The compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-fluorotetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharma- ceutically acceptable salt thereof.
14. The compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharma- ceutically acceptable salt thereof.
15. The compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(cis-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharma- ceutically acceptable salt thereof.
16. The compound N-[(5-chloro-6-{[4-fluoro-1-(oxetan-3-yl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharma- ceutically acceptable salt thereof.
17. The compound N-({5-bromo-6-[(1-tetrahydro-2H-pyran-4-ylpiperidin-4-yl)amino]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; or a pharma- ceutically acceptable salt thereof.
18. The compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(methylsulfonyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; or a pharma- ceutically acceptable salt thereof.
19. The compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(oxetan-3-yl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; or a pharma- ceutically acceptable salt thereof.
20. The compound 4-(4-{[2-(4-chlorophenyl)-5-methoxy-5-methylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; or a pharma- ceutically acceptable salt thereof.
21. The compound is 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(methylsulfonyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(oxetan-3-yl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 3. The compound of claim 1 or claim 2, selected from:
22. The compound is N-[(5-chloro-6-{[1-(cyanomethyl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(oxetan-3-yl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 3. The compound of claim 1 or claim 2, selected from:
23. The compound is 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(trans-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(cis-4-hydroxy-4-methylcyclohexyl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide 3. The compound of claim 1 or claim 2, selected from:
24. The compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(oxetan-3-yl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; or a pharma- ceutically acceptable salt thereof.
25. The compound is 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3R)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 3. The compound of claim 1 or claim 2 selected from 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methylmorpholin-2-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; or a pharma- ceutically acceptable salt thereof.
26. The compound is 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(3-nitro-4-{[(3S)-tetrahydro-2H-pyran-3-ylmethyl]amino}phenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-(1,4-dioxan-2-ylmethoxy)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-({5-bromo-6-[(1-tetrahydro-2H-pyran-4-ylpiperidin-4-yl)amino]pyridin-3-yl}sulfonyl)-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(4-{[(4-aminotetrahydro-2H-pyran-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[3-nitro-4-({[(3R)-1-tetrahydro-2H-pyran-4-ylpyrrolidin-3-yl]methyl}amino)phenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(4-methylmorpholin-2-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(3R)-1-(methylsulfonyl)pyrrolidin-3-yl]amino}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methoxytetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[1-(cyanomethyl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[4-({3-[cyclopropyl(oxetan-3-yl)amino]propyl}amino)-3-nitrophenyl]sulfonyl}-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; N-[(5-chloro-6-{[(1R,2S,4R,5R)-5-hydroxy-5-methylbicyclo[2.2.1]hept-2-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(6-{[(cis-4-hydroxy-4-methylcyclohexyl)methyl]amino}-5-nitropyridin-3-yl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-5-methoxy-5-methylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; or a pharma- ceutical acceptable salt thereof 3. The compound of claim 1 or claim 2 selected from:
27. The compound N-[(5-chloro-6-{[1-(cyanomethyl)piperidin-4-yl]methoxy}pyridin-3-yl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; or a pharma- ceutically acceptable salt thereof.
28. The compound is N-[(4-{[(4-aminotetrahydro-2H-pyran-4-yl)methyl]amino}-3-nitrophenyl)sulfonyl]-4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methoxytetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide; or a pharma- ceutical acceptable salt thereof 3. The compound of claim 1 or claim 2 selected from:
29. The compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-[(4-methoxytetrahydro-2H-pyran-4-yl)methoxy]-3-nitrophenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide or a pharma- ceutically acceptable salt thereof.
30. A composition for treating bladder cancer, brain cancer, breast cancer, bone marrow cancer, cervical cancer, chronic lymphocytic leukemia, colorectal cancer, esophageal cancer, hepatocellular carcinoma, lymphoblastic leukemia, follicular lymphoma, lymphoid malignancies of T-cell or B-cell origin, melanoma, myeloid leukemia, myeloma, oral cancer, ovarian cancer, non-small cell lung cancer, chronic lymphocytic leukemia, myeloma, prostate cancer, small cell lung cancer or splenic cancer comprising an excipient and a therapeutically effective amount of a compound of claim 1 or claim 2.
31. A method of treating bladder cancer, brain cancer, breast cancer, bone marrow cancer, cervical cancer, chronic lymphocytic leukemia, colorectal cancer, esophageal cancer, hepatocellular carcinoma, lymphoblastic leukemia, follicular lymphoma, lymphoid malignancies of T-cell or B-cell origin, melanoma, myeloid leukemia, myeloma, oral cancer, ovarian cancer, non-small cell lung cancer, chronic lymphocytic leukemia, myeloma, prostate cancer, small cell lung cancer or splenic cancer in a patient, comprising administering to the patient a therapeutically effective amount of a compound of claim 1 or claim 2.
32. A method of treating bladder cancer, brain cancer, breast cancer, bone marrow cancer, cervical cancer, chronic lymphocytic leukemia, colorectal cancer, esophageal cancer, hepatocellular carcinoma, lymphoblastic leukemia, follicular lymphoma, lymphoid malignancies of T-cell or B-cell origin, melanoma, myeloid leukemia, myeloma, oral cancer, ovarian cancer, non-small cell lung cancer, chronic lymphocytic leukemia, myeloma, prostate cancer, small cell lung cancer or splenic cancer in a patient, comprising administering to the patient a therapeutically effective amount of a compound of claim 1 or claim 2 and a therapeutically effective amount of one or more additional therapeutic agents.
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