Acetamido-phenyltetrazole derivatives and methods of use thereof
Acetamido-phenyltetrazole derivatives modulate P-glycoprotein and cytochrome P450 enzymes to enhance the bioavailability and delivery of anticancer drugs to tumor cells and the brain, addressing multidrug resistance and adverse effects.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Filing Date
- 2021-10-07
- Publication Date
- 2026-03-03
AI Technical Summary
Existing anticancer drugs face challenges due to multidrug resistance caused by overexpression of P-glycoprotein and cytochrome P450 enzymes, leading to reduced efficacy and bioavailability, particularly in tumor cells and the brain, with conventional modulators causing significant adverse effects.
Development of acetamido-phenyltetrazole derivatives that modulate P-glycoprotein and cytochrome P450 enzymes to enhance the bioavailability and delivery of therapeutic agents to tumor cells and the brain, while minimizing side effects.
The acetamido-phenyltetrazole derivatives improve the sensitivity of tumor cells to anticancer drugs and increase their delivery to the brain, overcoming multidrug resistance and enhancing therapeutic efficacy with reduced adverse effects.
Smart Images

Figure 0007823036000001 
Figure 0007823036000002 
Figure 0007823036000003
Abstract
Description
[Technical Field]
[0001] Related Applications This application claims priority to and benefit of U.S. Provisional Application No. 63 / 088,778, filed October 7, 2020, the entire contents of which are incorporated herein by reference.
[0002] Field of Disclosure The present disclosure relates to acetamido-phenyltetrazole derivatives that have P-glycoprotein-modulating activity and / or modulating activity against the drug-metabolizing enzyme cytochrome P450 (e.g., CYP3A4 and / or CYP3A5 isoforms) and are useful for treating the human or animal body. The present disclosure also relates to methods for preparing these compounds, pharmaceutical compositions containing them, and their use in treating disorders in which the expression of P-glycoprotein and / or cytochrome P450 isoforms (e.g., CYP3A4 or CYP3A5) is modulated (e.g., multidrug-resistant cancers). The present disclosure also relates to the use of compounds of the present disclosure to improve the oral bioavailability of therapeutic agents that are substrates of P-glycoprotein and / or cytochrome P450. The present disclosure also relates to the use of compounds of the present disclosure to increase the brain distribution of therapeutic agents that are substrates of P-glycoprotein and / or cytochrome P450. [Background technology]
[0003] background Many anticancer drugs (e.g., vinca alkaloids, anthracyclines, epipodophyllotoxins, paclitaxel, and docetaxel) are ineffective when administered to patients with multidrug resistance (MDR) caused by overexpression of P-glycoprotein. P-glycoprotein regulates the intracellular accumulation of administered anticancer drugs by extruding them from tumor cells. Expression of the drug-metabolizing CYP3A4 protein in breast, colorectal, and esophageal tumors, and Ewing's sarcoma, can suppress the intracellular concentration of anticancer drugs by forming metabolites with reduced antitumor activity. This action of CYP3A4 limits the efficacy of anticancer drugs or contributes to the development of resistance to these drugs. Modulation of P-glycoprotein and / or cytochrome P450 enzymes (e.g., CYP3A4) in tumor cells can increase the sensitivity of these cells to anticancer drugs.
[0004] P-glycoprotein is also expressed in normal healthy tissues, such as the small intestine. Intestinal P-glycoprotein does not allow its substrates to pass through the epithelial cells that line the intestinal wall, thus reducing the oral bioavailability of these substrates. In addition, anticancer drugs may also undergo first-pass metabolism by cytochrome P450 enzymes (e.g., CYP3A4 and / or CYP3A5 isoforms) present in the small intestine and liver, further reducing oral bioavailability. Therefore, it is necessary to improve the bioavailability of anticancer drugs by dual targeting and regulating P-glycoprotein and cytochrome P450 enzymes (e.g., CYP3A4 and / or CYP3A5 isoforms).
[0005] Furthermore, the localization of P-glycoprotein in the endothelial cells of the blood-brain barrier significantly restricts the transport of P-glycoprotein substrates from the blood to the brain. Modulation of P-glycoprotein at the blood-brain barrier may be beneficial in the treatment of several central nervous system (CNS) disorders, such as brain tumors such as glioblastoma.
[0006] Conventional P-glycoprotein modulators, such as verapamil and cyclosporine A, cause significant adverse effects (e.g., hypotension and immunosuppression). Therefore, several novel P-glycoprotein modulators, such as piperidine-2-carboxylate, acridine, piperazine-2,5-dione, anthranilic acid, and methanodibenzosuberane derivatives, have been developed. However, these newly introduced P-glycoprotein modulators have been reported to exhibit toxicity and other adverse effects. The present disclosure arises from a need to provide additional compounds for modulating P-glycoprotein and cytochrome P450 (e.g., CYP3A4 and CYP3A5 isoforms) enzymes that a) significantly improve the bioavailability of substrates for these enzymes, including anticancer drugs, b) overcome multidrug resistance in tumors, and c) improve the delivery of P-glycoprotein substrates to the brain while reducing significant side effects. Summary of the Invention
[0007] overview In one aspect, the disclosure provides a compound of formula (IA), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823036000001.tif39128In formula, A is C 3~10 cycloalkyl, 3- to 14-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-14 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said cycloalkyl or heterocyclyl is optionally substituted with oxo; R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6alkoxy, halogen, -CN, -OH, -NH2, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R1 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R2 and R3 are each independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11 )2, or -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein neither R2 nor R3 is H, and wherein said -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently oxo, halogen, -OH, -NH2, -CN, or -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R 10 may be substituted with; R8 is -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9; Each R9 independently represents -(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein said heteroaryl or aryl may be optionally substituted with one or more halogen, —CN, —OH, or —NH; Each R 10 are independently halogen, -OH, -NH2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl may be substituted with one or more C 3~10cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2; 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, halogen, -CN, -OH, or -NH; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, where R5 and R6 together with the atoms to which they are attached form a heterocyclyl or heteroaryl substituted with two R7 and both R7 are -O-methyl, (a) one of R2 and R3 is not -O-methyl; or (b) R x or R y is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0008] In one aspect, the disclosure provides compounds of formula (I), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823036000002.tif39128In formula, A is C 3~10cycloalkyl, 3- to 14-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-14 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said cycloalkyl or heterocyclyl is optionally substituted with oxo; R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, -CN, -OH, -NH2, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R1 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R2 and R3 are each independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11 )2, or -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein neither R2 nor R3 is H, and wherein said -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently oxo, halogen, -OH, -NH2, -CN, or -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R 10 may be substituted with; R8 is -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9; Each R9 independently represents -(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein said heteroaryl or aryl may be optionally substituted with one or more halogen, —CN, —OH, or —NH; Each R 10 are independently halogen, -OH, -NH2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl may be substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2; 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, halogen, -CN, -OH, or -NH; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, wherein when R5 and R6 together with the atom to which they are attached form a heterocyclyl or heteroaryl substituted with two R7, one R7 is not -O-methyl.
[0009] In one aspect, the disclosure provides a compound of formula (I'), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823036000003.tif39128In formula, A is TIFF0007823036000004.tif21162; R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, -CN, -OH, -NH2, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R1 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R2 and R3 are each independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11 )2, or -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein neither R2 nor R3 is H, and wherein said -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently oxo, halogen, -OH, -NH2, -CN, or -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R 10 may be substituted with; R8 is -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9; Each R9 independently represents -(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein said heteroaryl or aryl may be optionally substituted with one or more halogen, —CN, —OH, or —NH; Each R 10 are independently halogen, -OH, -NH2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl may be substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2; 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, halogen, -CN, -OH, or -NH; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, wherein when R5 and R6 together with the atom to which they are attached form a heterocyclyl or heteroaryl substituted with two R7, one R7 is not -O-methyl.
[0010] In one aspect, the disclosure provides a compound of formula (II), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823036000005.tif39128In formula, R x is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, -CN, -OH, -NH2, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R1 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R2 and R3 are each independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11 )2, or -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein neither R2 nor R3 is H, and wherein said -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently oxo, halogen, -OH, -NH2, -CN, or -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R 10 may be substituted with; R8 is -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9; Each R9 independently represents -(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein said heteroaryl or aryl may be optionally substituted with one or more halogen, —CN, —OH, or —NH; Each R 10 are independently halogen, -OH, -NH2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl may be substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2; 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, halogen, -CN, -OH, or -NH; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, wherein when R5 and R6 together with the atom to which they are attached form a heterocyclyl or heteroaryl substituted with two R7, one R7 is not -O-methyl.
[0011] In one aspect, the disclosure provides a compound of formula (IA'), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823036000006.tif39128In formula, A is C 3~10cycloalkyl, 3- to 14-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-14 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said cycloalkyl or heterocyclyl is optionally substituted with oxo; R x and R y are each independently H or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R1 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R2 and R3 each independently represent H, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 alkynyl, or -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein neither R2 nor R3 is H, and wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently 1~6 is alkoxy; n, m, and p are each independently 0 or 1; where (a) one of R2 and R3 is not —O-methyl; or (b) R x or R yis a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0012] In one aspect, the disclosure provides compounds obtainable or obtainable by a method for preparing a compound described herein (e.g., a method comprising one or more steps described in Schemes 1-6).
[0013] In one aspect, the present disclosure provides a pharmaceutical composition comprising a compound of the present disclosure, or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof, and a pharmaceutically acceptable diluent or carrier.
[0014] In one aspect, the present disclosure provides intermediates described herein that are suitable for use in the methods for preparing the compounds described herein (e.g., the intermediates are selected from the intermediates described in Examples 1-16).
[0015] In one aspect, the present disclosure provides a method of modulating P-glycoprotein activity (e.g., in vitro or in vivo) and / or cytochrome P450 activity (e.g., in vitro or in vivo), comprising contacting a cell with an effective amount of a compound of the present disclosure, or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof.
[0016] In one aspect, the present disclosure provides a method of treating or preventing a disease or disorder disclosed herein in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of the present disclosure, or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof, or a pharmaceutical composition of the present disclosure.
[0017] In one aspect, the present disclosure provides compounds of the present disclosure, or pharmaceutically acceptable prodrugs, solvates, enantiomers, stereoisomers, tautomers, or salts thereof, for use in modulating P-glycoprotein activity (e.g., in vitro or in vivo) and / or cytochrome P450 activity (e.g., in vitro or in vivo).
[0018] In one aspect, the present disclosure provides a compound of the present disclosure, or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof, for use in treating or preventing a disease or disorder disclosed herein.
[0019] In one aspect, the present disclosure provides the use of a compound of the present disclosure, or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof, in the manufacture of a medicament for modulating P-glycoprotein activity (e.g., in vitro or in vivo) and / or cytochrome P450 activity (e.g., in vitro or in vivo).
[0020] In one aspect, the disclosure provides the use of a compound of the disclosure, or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof, in the manufacture of a medicament for treating or preventing a disease or disorder disclosed herein.
[0021] In one aspect, the disclosure provides methods of preparing the compounds of the disclosure.
[0022] In one aspect, the disclosure provides a method of preparing a compound, comprising one or more steps described herein.
[0023] Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this disclosure belongs. As used herein, the singular also includes the plural unless the context clearly dictates otherwise. Although methods and materials similar or equivalent to those described herein can be used in the practice or testing of this disclosure, suitable methods and materials are described below. All publications, patent applications, patents, and other references mentioned herein are incorporated by reference. References cited herein are not admitted to be prior art to this disclosure. In case of conflict, the present specification, including definitions, will prevail. Furthermore, the materials, methods, and examples are illustrative only and are not intended to be limiting. In the event of a conflict between a chemical structure and the name of a compound disclosed herein, the chemical structure will prevail.
[0024] [The present invention 1001] A compound of formula (IA) or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823036000007.tif39128 During the ceremony, A is C 3~10 cycloalkyl, 3- to 14-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-14 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said cycloalkyl or heterocyclyl is optionally substituted with oxo; R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, halogen, -CN, -OH, -NH 2 , a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R 1 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R 2 and R 3 are independently H, C 2~6 Alkenyl, C2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 ) 2 , -C(O)NR 11 -S(O) 2 R 11 , -C(O)NR 11 -S(O) 2 -OR 11 , -C(O)NR 11 -S(O) 2 -N(R 11 ) 2 or —O—(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), where R 2 MoR 3 Here, the -OC is not H. 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R 5 and R 6 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or -C(O)R 7 wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 7 or R 5 and R 6 together with the atoms to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more R 7 may be substituted with; Each R 7 are independently oxo, halogen, -OH, -NH 2 , -CN, -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 ) 2 、C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl) 2 , -O-(CH 2 ) t -R 8 , -NH-(CH 2 ) t -R 8 、C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R 10 may be substituted with; R 8 -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH 2 , -NH(C 1~6 alkyl), -N(C 1~6 alkyl) 2 , -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 9 may be substituted with; Each R 9 are independently -(CH 2 ) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH 2 ) u -(C 6~10 aryl), wherein the heteroaryl or aryl is selected from one or more halogen, —CN, —OH, or —NH 2 may be substituted with; Each R 10 are independently halogen, -OH, -NH 2 , -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl may be substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, oxo, halogen, -CN, -OH, or -NH 2 or 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, halogen, -CN, -OH, or -NH 2 may be substituted with; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, where R 5 and R 6 together with the atoms to which they are attached, form two R 7 and forming a heterocyclyl or heteroaryl substituted with both R 7 is -O-methyl, (a) R 2 and R 3 one of which is not -O-methyl; or (b) R x or R y is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. [The present invention 1002] A compound of formula (I) or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823036000008.tif39128 During the ceremony, A is C 3~10 cycloalkyl, 3- to 14-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-14 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said cycloalkyl or heterocyclyl is optionally substituted with oxo; R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, halogen, -CN, -OH, -NH 2 , a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R 1 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R 2 and R 3 are independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 ) 2 , -C(O)NR 11 -S(O) 2 R 11 , -C(O)NR 11 -S(O) 2 -OR 11 , -C(O)NR 11 -S(O) 2 -N(R 11 ) 2 or —O—(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), where R 2 MoR 3 Here, the -OC is not H. 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R 5 and R 6 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C6~10 aryl, 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or -C(O)R 7 wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 7 or R 5 and R 6 together with the atoms to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more R 7 may be substituted with; Each R 7 are independently oxo, halogen, -OH, -NH 2 , -CN, -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 ) 2 、C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl) 2 , -O-(CH 2 ) t -R 8 , -NH-(CH 2 ) t -R 8 、C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R 10 may be substituted with; R 8 -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH 2 , -NH(C 1~6 alkyl), -N(C 1~6 alkyl) 2 , -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 9 may be substituted with; Each R 9 are independently -(CH 2 ) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH 2 ) u-(C 6~10 aryl), wherein the heteroaryl or aryl is selected from one or more halogen, —CN, —OH, or —NH 2 may be substituted with; Each R 10 are independently halogen, -OH, -NH 2 , -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl may be substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, oxo, halogen, -CN, -OH, or -NH 2 or 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, halogen, -CN, -OH, or -NH 2 may be substituted with; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, where R 5 and R 6 together with the atoms to which they are attached, form two R 7 When forming a heterocyclyl or heteroaryl substituted with one R 7 is not -O-methyl. [The present invention 1003] A compound of formula (I') or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823036000009.tif39128 During the ceremony, A is TIFF0007823036000010.tif23164 and; R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, halogen, -CN, -OH, -NH 2 , a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R 1 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R 2 and R 3 are independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 ) 2 , -C(O)NR 11 -S(O) 2 R 11 , -C(O)NR 11 -S(O) 2 -OR 11 , -C(O)NR 11 -S(O) 2 -N(R 11 ) 2 or —O—(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), where R 2 MoR 3 Here, the -OC is not H. 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C6~10 optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R 5 and R 6 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or -C(O)R 7 wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 7 or R 5 and R 6 together with the atoms to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more R 7 may be substituted with; Each R 7 are independently oxo, halogen, -OH, -NH 2 , -CN, -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 ) 2 、C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl) 2 , -O-(CH 2 ) t -R 8 , -NH-(CH 2 ) t -R 8 、C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R 10 may be substituted with; R 8 -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH 2 , -NH(C 1~6 alkyl), -N(C 1~6 alkyl) 2 , -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 9 may be substituted with; Each R 9 are independently -(CH 2 ) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH 2 ) u -(C 6~10 aryl), wherein the heteroaryl or aryl is selected from one or more halogen, —CN, —OH, or —NH 2 may be substituted with; Each R 10 are independently halogen, -OH, -NH 2 , -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl may be substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, oxo, halogen, -CN, -OH, or -NH 2 or 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, halogen, -CN, -OH, or -NH 2 may be substituted with; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, where R 5 and R 6 together with the atoms to which they are attached, form two R 7 When forming a heterocyclyl or heteroaryl substituted with one R 7 is not -O-methyl. [The present invention 1004] A compound of formula (II) or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823036000011.tif40128 During the ceremony, R x is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, halogen, -CN, -OH, -NH 2 , a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R 1 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R 2 and R 3 are independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 ) 2 , -C(O)NR 11 -S(O) 2 R 11 , -C(O)NR 11 -S(O) 2 -OR 11 , -C(O)NR 11 -S(O) 2 -N(R 11 ) 2 or —O—(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), where R 2 MoR 3 Here, the -OC is not H. 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R 5 and R 6 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or -C(O)R 7 wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 7 or R 5 and R 6 together with the atoms to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more R 7 may be substituted with; Each R 7 are independently oxo, halogen, -OH, -NH 2 , -CN, -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 ) 2 、C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl) 2 , -O-(CH 2 ) t -R 8 , -NH-(CH 2 ) t -R 8 、C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R 10 may be substituted with; R 8 -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH 2 , -NH(C1~6 alkyl), -N(C 1~6 alkyl) 2 , -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 9 may be substituted with; Each R 9 are independently -(CH 2 ) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH 2 ) u -(C 6~10 aryl), wherein the heteroaryl or aryl is selected from one or more halogen, —CN, —OH, or —NH 2 may be substituted with; Each R 10 are independently halogen, -OH, -NH 2 , -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl may be substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, oxo, halogen, -CN, -OH, or -NH 2 or 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, halogen, -CN, -OH, or -NH 2 may be substituted with; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, where R 5 and R 6 together with the atoms to which they are attached, form two R 7 When forming a heterocyclyl or heteroaryl substituted with one R 7 is not -O-methyl. [The present invention 1005] A compound of formula (IA') or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823036000012.tif39128 During the ceremony, A is C 3~10 cycloalkyl, 3- to 14-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-14 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said cycloalkyl or heterocyclyl is optionally substituted with oxo; R x and R y are each independently H or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R 1 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R 2 and R 3 are independently H, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 alkynyl, or -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), where R 2 MoR 3 Here, the -OC is not H. 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R 5 and R 6 together with the atoms to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more R 7 may be substituted with; Each R 7 independently, C 1~6 is alkoxy; n, m, and p are each independently 0 or 1; where (a) R2 and R 3 is not -O-methyl; or (b) R x or R y is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. [The present invention 1006] R x and R y are independently H, C 1~6 Any of the compounds of the present invention described above, wherein the aryl group is alkyl, or -OH. [The present invention 1007] R 1 is H or C 1~6 Any of the compounds of the present invention above, wherein the compound is alkyl. [The present invention 1008] R 2 and R 3 are each independently, -OC 1~6 Alkyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 ) 2 , or -C(O)NR 11 -S(O) 2 R 11 Any of the compounds of the present invention, wherein [The present invention 1009] R 5 and R 6 are independently H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or -C(O)R 7 wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 7 Any of the compounds of the present invention described above, optionally substituted with [The present invention 1010] R 5 and R 6 are independently H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 7 Any of the compounds of the present invention described above, optionally substituted with [The present invention 1011] R 5 and R 6 are independently H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 7 Any of the compounds of the present invention substituted with: [The present invention 1012] R 5 and R 6 together with the atoms to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more R 7 Any of the compounds of the present invention substituted with: [The present invention 1013] Each R 7 are independently oxo, halogen, -OH, -NH 2 , -CN, -C(O)R 10 、C 1~3 Alkyl, C 2~6 Alkynyl, -O-(CH 2 ) t -R 8 、C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkynyl, alkoxy, aryl, or heteroaryl is selected from one or more R 10 Any of the compounds of the present invention described above, optionally substituted with [The present invention 1014] Each R 7 are independently oxo, halogen, -OH, -NH 2 , -CN, -C(O)R 10 、C 1~3 Alkyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -O-(CH 2 ) t -R 8 、C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkynyl, alkoxy, aryl, or heteroaryl is selected from one or more R 10 Any of the compounds of the present invention substituted with: [The present invention 1015] R 8 -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH 2 , -N(C 1~6 alkyl) 2 , -S(C 1~6 alkyl), 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkoxy, alkyl, heterocyclyl, or heteroaryl is selected from one or more R 9 Any of the compounds of the present invention described above, optionally substituted with [The present invention 1016] R 8 -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH 2 , -N(C 1~6 alkyl) 2 , -S(C 1~6 alkyl), 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkoxy, alkyl, heterocyclyl, or heteroaryl is selected from one or more R 9 Any of the compounds of the present invention substituted with: [The present invention 1017] Each R 9 are independent, -(CH 2 ) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH 2 ) u -(C 6~10 Any of the preceding compounds of the present invention wherein said heteroaryl or aryl is optionally substituted with one or more halogen or -OH. [The present invention 1018] Each R 9 are independent, -(CH 2 ) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH 2 ) u -(C 6~10 Any of the preceding compounds of the present invention is a heteroaryl or aryl), wherein said heteroaryl or aryl is substituted with one or more halogen or -OH. [The present invention 1019] Each R 10 independently, C 1~6 Alkyl, C 1~6 Any of the compounds of the present invention which is haloalkyl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. [The present invention 1020] Each R 11 became independent, H; One or more 3- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 Aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S optionally substituted with C 1~6 Alkyl wherein the heterocyclyl, aryl, or heteroaryl is a 5-10 membered heteroaryl containing one or more heteroatoms selected from N, O, and S; C 1~6 Any of the compounds of the present invention described above may be substituted with alkyl or oxo. [The present invention 1021] Each R 11 became independent, H; One or more 3- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 Aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S optionally substituted with C 1~6 Alkyl wherein the heterocyclyl, aryl, or heteroaryl is a 5-10 membered heteroaryl containing one or more heteroatoms selected from N, O, and S; C 1~6 Any of the compounds of the present invention substituted with alkyl, or oxo. [The present invention 1022] Each R 11 became independent, H; One or more 3- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 Aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S Replaced by C 1~6 Alkyl wherein the heterocyclyl, aryl, or heteroaryl is a 5-10 membered heteroaryl containing one or more heteroatoms selected from N, O, and S; C 1~6 Any of the compounds of the present invention described above may be substituted with alkyl or oxo. [The present invention 1023] 2 R's 11 together with the atoms to which they are bonded, One or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, halogen, -CN, -OH, or -NH 2 4- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with Any of the compounds of the present invention which form: [The present invention 1024] 2 R's 11 together with the atoms to which they are bonded, One or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, halogen, -CN, -OH, or -NH 2 4- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, substituted with Any of the compounds of the present invention which form: [The present invention 1025] Any of the compounds of the present invention wherein each n is 0. [The present invention 1026] Any of the compounds of the present invention wherein each n is 1. [The present invention 1027] Any of the preceding compounds of the present invention wherein each m is 0. [The present invention 1028] Any of the preceding compounds of the present invention wherein each m is 1. [The present invention 1029] Any of the compounds of the present invention wherein each p is 0. [The present invention 1030] Any of the compounds of the present invention wherein each p is 1. [The present invention 1031] R 2 MoR 3 or H. [The present invention 1032] R 5 and R 6 together with the atoms to which they are attached, form two R 7 When forming a heterocyclyl or heteroaryl substituted with one R 7 Any of the preceding compounds of the present invention, wherein is not -O-methyl. [The present invention 1033] Compounds of formula (Ia) or (Ib): TIFF0007823036000013.tif77128 or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof. [The present invention 1034] A compound of formula (Ic), (Id), (Ie), or (If): TIFF0007823036000014.tif164128 or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof. [This invention 1035] Compounds of formula (I-a') or (I-b'): TIFF0007823036000015.tif77128 or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof. [The present invention 1036] Compound of formula (II-a): TIFF0007823036000016.tif42128 5. The compound of any one of claims 1001 to 1004, which is a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof. [This invention 1037] Compound of formula (II-a'): TIFF0007823036000017.tif42128 5. The compound of any one of claims 1001 to 1004, which is a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof. [The present invention 1038] Any of compounds 1001 to 1005 of the present invention selected from Table 1. [This invention 1039] A compound of the present invention 1001 or 1005 selected from Table 2. [The present invention 1040] A pharmaceutical composition comprising any one of the compounds of the present invention 1001 to 1039, or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof, and a pharmaceutically acceptable diluent or carrier. [This invention 1041] A method for regulating P-glycoprotein activity and / or cytochrome P450 activity, comprising contacting a cell with an effective amount of any of the compounds of the present inventions 1001 to 1039 or the pharmaceutical composition of the present invention 1040. [The present invention 1042] A method for treating or preventing cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of any of the compounds of present inventions 1001 to 1039 or the pharmaceutical composition of present invention 1040. [This invention 1043] A compound of any of claims 1001 to 1039 or a pharmaceutical composition of claim 1040 for use in modulating P-glycoprotein activity and / or cytochrome P450 activity. [This invention 1044] A compound of any of claims 1001 to 1039 or a pharmaceutical composition of claim 1040 for use in treating or preventing a disease or disorder disclosed herein. [This invention 1045] Use of any of the compounds of inventions 1001 to 1039 or the pharmaceutical composition of invention 1040 in the manufacture of a medicament for modulating P-glycoprotein activity and / or cytochrome P450 activity. [The present invention 1046] Use of any of the compounds of inventions 1001 to 1039 or the pharmaceutical composition of invention 1040 in the manufacture of a medicament for treating or preventing a disease or disorder disclosed herein. Other features and advantages of the present disclosure will be apparent from the following detailed description and claims. DETAILED DESCRIPTION OF THE INVENTION
[0025] Detailed Description Compounds of the Disclosure In one aspect, the disclosure provides a compound of formula (IA), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823036000018.tif39128In formula, A is C 3~10 cycloalkyl, 3- to 14-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10aryl or 5-14 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said cycloalkyl or heterocyclyl is optionally substituted with oxo; R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, -CN, -OH, -NH2, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R1 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R2 and R3 are each independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11 )2, or -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein neither R2 nor R3 is H, and wherein said -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R5 and R6 are each independently H, C1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently oxo, halogen, -OH, -NH2, -CN, or -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R 10 may be substituted with; R8 is -OH, C 1~6 Alkoxy, C1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9; Each R9 independently represents -(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein said heteroaryl or aryl may be optionally substituted with one or more halogen, —CN, —OH, or —NH; Each R 10 are independently halogen, -OH, -NH2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl may be substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2; 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, halogen, -CN, -OH, or -NH; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, where R5 and R6 together with the atoms to which they are attached form a heterocyclyl or heteroaryl substituted with two R7 and both R7 are -O-methyl, (a) one of R2 and R3 is not -O-methyl; or (b) R x or R y is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0026] In one aspect, the disclosure provides compounds of formula (I), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823036000019.tif39128In formula, A is C 3~10 cycloalkyl, 3- to 14-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-14 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said cycloalkyl or heterocyclyl is optionally substituted with oxo; R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, -CN, -OH, -NH2, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R1 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R2 and R3 are each independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11)2, or -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein neither R2 nor R3 is H, and wherein said -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently oxo, halogen, -OH, -NH2, -CN, or -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R 10 may be substituted with; R8 is -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9; Each R9 independently represents -(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein said heteroaryl or aryl may be optionally substituted with one or more halogen, —CN, —OH, or —NH; Each R 10 are independently halogen, -OH, -NH2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl may be substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2; 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, halogen, -CN, -OH, or -NH; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, wherein when R5 and R6 together with the atom to which they are attached form a heterocyclyl or heteroaryl substituted with two R7, one R7 is not -O-methyl.
[0027] In one aspect, the disclosure provides a compound of formula (I'), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823036000020.tif39128In formula, A is TIFF0007823036000021.tif21162; R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, -CN, -OH, -NH2, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R1 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R2 and R3 are each independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11)2, or -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein neither R2 nor R3 is H, and wherein said -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently oxo, halogen, -OH, -NH2, -CN, or -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R 10 may be substituted with; R8 is -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9; Each R9 independently represents -(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein said heteroaryl or aryl may be optionally substituted with one or more halogen, —CN, —OH, or —NH; Each R 10 are independently halogen, -OH, -NH2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl may be substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2; 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, halogen, -CN, -OH, or -NH; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, wherein when R5 and R6 together with the atom to which they are attached form a heterocyclyl or heteroaryl substituted with two R7, one R7 is not -O-methyl.
[0028] In one aspect, the disclosure provides a compound of formula (II), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823036000022.tif39128In formula, R x is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, -CN, -OH, -NH2, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R1 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R2 and R3 are each independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11 )2, or -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein neither R2 nor R3 is H, and wherein said -OC 1~6 Alkyl, -OC 2~6Alkenyl, or -OC 2~6 Alkynyl is C 6~10 optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently oxo, halogen, -OH, -NH2, -CN, or -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R 10 may be substituted with; R8 is -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9; Each R9 independently represents -(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein said heteroaryl or aryl may be optionally substituted with one or more halogen, —CN, —OH, or —NH; Each R 10 are independently halogen, -OH, -NH2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl may be substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2; 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, halogen, -CN, -OH, or -NH; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, wherein when R5 and R6 together with the atom to which they are attached form a heterocyclyl or heteroaryl substituted with two R7, one R7 is not -O-methyl.
[0029] In one aspect, the disclosure provides a compound of formula (IA'), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823036000023.tif39128In formula, A is C 3~10 cycloalkyl, 3- to 14-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-14 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said cycloalkyl or heterocyclyl is optionally substituted with oxo; R x and R y are each independently H or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R1 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R2 and R3 each independently represent H, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 alkynyl, or -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein neither R2 nor R3 is H, and wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently 1~6 is alkoxy; n, m, and p are each independently 0 or 1; where (a) one of R2 and R3 is not —O-methyl; or (b) R x or R y is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0030] For compounds of formula (IA), (I), (I'), (II), or (IA'), A, R x、 R y , R1, R2, R3, R5, R6, R7, R8, R9, R 10 , R 11 , n, m, p, t, and u can be appropriately selected from the groups described herein; A, R x、 R y , R1, R2, R3, R5, R6, R7, R8, R9, R 10 , R 11 , n, m, p, t, and u may be any group described herein in A, R x、 R y , R1, R2, R3, R5, R6, R7, R8, R9, R 10 , R 11 , n, m, p, t, and u may be combined with any of the groups described herein, as appropriate.
[0031] In some embodiments, the N atom of the compound is an N-oxide.
[0032] In some embodiments, the N-oxide has the formula TIFF0007823036000024.tif16128, wherein TIFF0007823036000025.tif9128 shows the bond for a compound of formula (IA), (I), (I'), (II), or (IA').
[0033] In some embodiments, the N-oxide has the formula TIFF0007823036000026.tif14128, wherein TIFF0007823036000027.tif9128 shows the bond for a compound of formula (IA), (I), (I'), (II), or (IA').
[0034] In some embodiments, the N-oxide has the formula TIFF0007823036000028.tif15128, wherein TIFF0007823036000029.tif9128 shows the bond for a compound of formula (IA), (I), (I'), (II), or (IA').
[0035] In some embodiments, A is C 3~10 cycloalkyl, 3- to 14-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or 5-14 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl or heterocyclyl is optionally substituted with oxo.
[0036] In some embodiments, A is C 3~10 cycloalkyl, 3- to 14-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-14 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0037] In some embodiments, A is C 3~10 cycloalkyl or 3- to 14-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl or heterocyclyl is optionally substituted with oxo.
[0038] In some embodiments, A is C 3~10 cycloalkyl, or a 3- to 14-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S.
[0039] In some embodiments, A is C optionally substituted with oxo. 3~10 It is cycloalkyl.
[0040] In some embodiments, A is C3 cycloalkyl. In some embodiments, A is C4 cycloalkyl. In some embodiments, A is C5 cycloalkyl. In some embodiments, A is C6 cycloalkyl. In some embodiments, A is C7 cycloalkyl. In some embodiments, A is C8 cycloalkyl. In some embodiments, A is C9 cycloalkyl. In some embodiments, A is C 10 It is cycloalkyl.
[0041] In some embodiments, A is a C3 cycloalkyl optionally substituted with oxo. In some embodiments, A is a C4 cycloalkyl optionally substituted with oxo. In some embodiments, A is a C5 cycloalkyl optionally substituted with oxo. In some embodiments, A is a C6 cycloalkyl optionally substituted with oxo. In some embodiments, A is a C7 cycloalkyl optionally substituted with oxo. In some embodiments, A is a C8 cycloalkyl optionally substituted with oxo. In some embodiments, A is a C9 cycloalkyl optionally substituted with oxo. In some embodiments, A is a C6 cycloalkyl optionally substituted with oxo. 10 It is cycloalkyl.
[0042] In some embodiments, A is a C3-C7 monocyclic cycloalkyl. In some embodiments, A is a C3-C7 monocyclic saturated cycloalkyl. In some embodiments, A is a C3-C7 monocyclic partially saturated cycloalkyl. In some embodiments, A is a C9-C 10 In some embodiments, A is a C-C 10 In some embodiments, A is a C-C bicyclic saturated cycloalkyl. 10 In some embodiments, A is a C-C bicyclic partially saturated cycloalkyl. 10It is a polycyclic cycloalkyl.
[0043] In some embodiments, A is a C3-C7 monocyclic cycloalkyl optionally substituted with oxo. In some embodiments, A is a C3-C7 monocyclic saturated cycloalkyl optionally substituted with oxo. In some embodiments, A is a C3-C7 monocyclic partially saturated cycloalkyl optionally substituted with oxo. In some embodiments, A is a C9-C monocyclic partially saturated cycloalkyl optionally substituted with oxo. 10 In some embodiments, A is a C9-C cycloalkyl optionally substituted with oxo. 10 In some embodiments, A is a C9-C10 alkyl group optionally substituted with oxo. 10 In some embodiments, A is a C8-C10 alkyl group optionally substituted with oxo. 10 It is a polycyclic cycloalkyl.
[0044] In some embodiments, A is a 3-14 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0045] In some embodiments, A is a 3-14 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with oxo.
[0046] In some embodiments, A is a 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0047] In some embodiments, A is a 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with oxo.
[0048] In some embodiments, A is a 3-membered heterocyclyl containing one heteroatom selected from N, O, and S. In some embodiments, A is a 4-membered heterocyclyl containing one to two heteroatoms selected from N, O, and S. In some embodiments, A is a 5-membered heterocyclyl containing one to three heteroatoms selected from N, O, and S. In some embodiments, A is a 6-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S. In some embodiments, A is a 7-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S. In some embodiments, A is an 8-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S. In some embodiments, A is a 9-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S. In some embodiments, A is a 10-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S. In some embodiments, A is an 11-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is a 14-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0049] In some embodiments, A is a 3-membered heterocyclyl containing one heteroatom selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 4-membered heterocyclyl containing one to two heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 5-membered heterocyclyl containing one to three heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 6-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 7-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is an 8-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 9-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is an 11-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 12-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 14-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo.
[0050] In some embodiments, A is a 7-10 membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0051] In some embodiments, A is a 7-10 membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with oxo.
[0052] In some embodiments, A is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0053] In some embodiments, A is a 7-membered bicyclic heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is an 8-membered bicyclic heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 9-membered bicyclic heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 10-membered bicyclic heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo.
[0054] In some embodiments, A is an 8-14 membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0055] In some embodiments, A is an 8-14 membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with oxo.
[0056] In some embodiments, A is an 8-10 membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0057] In some embodiments, A is an 8-10 membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with oxo.
[0058] In some embodiments, A is a 14-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0059] In some embodiments, A is a 14-membered polycyclic heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo.
[0060] In some embodiments, A is a 14-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with oxo.
[0061] In some embodiments, A is C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0062] In some embodiments, A is C 6~10 In some embodiments, A is aryl. In some embodiments, A is C5-C6 aryl. In some embodiments, A is phenyl.
[0063] In some embodiments, A is a 5-14 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0064] In some embodiments, A is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0065] In some embodiments, A is a 5-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, A is a 6-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, A is a 7-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, A is an 8-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, A is a 9-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, A is a 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, A is an 11-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, A is a 12-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, A is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is a 14-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0066] In some embodiments, A is a 9-10 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0067] In some embodiments, A is a 9-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is a 10-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0068] In some embodiments, A is a 9-10 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0069] In some embodiments, A is The file is TIFF0007823036000030.tif23164.
[0070] In some embodiments, A is The file is TIFF0007823036000031.tif22128.
[0071] In some embodiments, A is The file is TIFF0007823036000032.tif21128.
[0072] In some embodiments, A is The file is TIFF0007823036000033.tif15128.
[0073] In some embodiments, A is The file is TIFF0007823036000034.tif15128.
[0074] In some embodiments, A is The file is TIFF0007823036000035.tif22128.
[0075] In some embodiments, R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, —CN, —OH, —NH2, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0076] In some embodiments, R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 It is alkoxy, halogen, -CN, -OH, or -NH2.
[0077] In some embodiments, R x and R y are H respectively.
[0078] In some embodiments, R x and R y are each independently, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, —CN, —OH, —NH2, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0079] In some embodiments, R x and R y are each independently, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 It is alkoxy, halogen, -CN, -OH, or -NH2.
[0080] In some embodiments, R x and R y are each independently a 3- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S.
[0081] In some embodiments, R x and R y are independently H, C 1~6 alkyl, or -OH.
[0082] In some embodiments, R x is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6alkoxy, halogen, —CN, —OH, —NH2, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0083] In some embodiments, R x is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 It is alkoxy, halogen, -CN, -OH, or -NH2.
[0084] In some embodiments, R x is H.
[0085] In some embodiments, R x is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, —CN, —OH, —NH2, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0086] In some embodiments, R x is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 It is alkoxy, halogen, -CN, -OH, or -NH2.
[0087] In some embodiments, R x is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, or C 1~6 It is an alkoxy.
[0088] In some embodiments, R x is C 1~6 Alkyl, C2~6 Alkenyl, or C 2~6 It is alkynyl.
[0089] In some embodiments, R x is C 1~6 In some embodiments, R x is methyl. In some embodiments, R x is ethyl. In some embodiments, R x is propyl. In some embodiments, R x is butyl. In some embodiments, R x is pentyl. In some embodiments, R x is hexyl. In some embodiments, R x is isopropyl. In some embodiments, R x is isobutyl. In some embodiments, R x is isopentyl. In some embodiments, R x is isohexyl. In some embodiments, R x is sec butyl. In some embodiments, R x is sec pentyl. In some embodiments, R x is sec hexyl. In some embodiments, R x is tert butyl.
[0090] In some embodiments, R x is C 2~6 In some embodiments, R is alkenyl. x is C alkenyl. In some embodiments, R x is C alkenyl. In some embodiments, R x is C4 alkenyl. In some embodiments, R x is C5 alkenyl. In some embodiments, R x is a C6 alkenyl.
[0091] In some embodiments, R x is C 2~6 In some embodiments, R is alkynyl. xis C alkynyl. In some embodiments, R x is C alkynyl. In some embodiments, R x is C4 alkynyl. In some embodiments, R x is C5 alkynyl. In some embodiments, R x is a C6 alkynyl.
[0092] In some embodiments, R x is C 1~6 In some embodiments, R is alkoxy. x is methoxy. In some embodiments, R x is ethoxy. In some embodiments, R x is propoxy. In some embodiments, R x is butoxy. In some embodiments, R x is pentoxy. In some embodiments, R x is hexoxy.
[0093] In some embodiments, R x is a halogen, -CN, -OH, or -NH2.
[0094] In some embodiments, R x is a halogen. In some embodiments, R x is F, Cl, Br, or I. In some embodiments, R x is F, Cl, or Br. In some embodiments, R x is F. In some embodiments, R x is Cl. In some embodiments, R x is Br. In some embodiments, R x is I.
[0095] In some embodiments, R x is -CN. In some embodiments, R x is —OH. In some embodiments, R x is -NH2.
[0096] In some embodiments, Rx is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0097] In some embodiments, R x is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0098] In some embodiments, R x is a 3-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R x is a 4-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R x is a 5-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R x is a 6-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R x is a 7-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R x is an 8-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R x is a 9-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R x is a 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S.
[0099] In some embodiments, R x is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0100] In some embodiments, R xis a 5-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R x is a 6-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R x is a 7-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R x is an 8-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R x is a 9-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R x is a 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S.
[0101] In some embodiments, each R x is H, C 1~6 alkyl, or -OH.
[0102] In some embodiments, R y is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, —CN, —OH, —NH2, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0103] In some embodiments, R y is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 It is alkoxy, halogen, -CN, -OH, or -NH2.
[0104] In some embodiments, R y is H.
[0105] In some embodiments, R y is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, —CN, —OH, —NH2, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0106] In some embodiments, R y is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 It is alkoxy, halogen, -CN, -OH, or -NH2.
[0107] In some embodiments, R y is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, or C 1~6 It is an alkoxy.
[0108] In some embodiments, R y is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0109] In some embodiments, R y is C 1~6 In some embodiments, R y is methyl. In some embodiments, R y is ethyl. In some embodiments, R y is propyl. In some embodiments, R y is butyl. In some embodiments, R y is pentyl. In some embodiments, R y is hexyl. In some embodiments, R y is isopropyl. In some embodiments, R yis isobutyl. In some embodiments, R y is isopentyl. In some embodiments, R y is isohexyl. In some embodiments, R y is sec butyl. In some embodiments, R y is sec pentyl. In some embodiments, R y is sec hexyl. In some embodiments, R y is tert butyl.
[0110] In some embodiments, R y is C 2~6 In some embodiments, R is alkenyl. y is C alkenyl. In some embodiments, R y is C alkenyl. In some embodiments, R y is C4 alkenyl. In some embodiments, R y is C5 alkenyl. In some embodiments, R y is a C6 alkenyl.
[0111] In some embodiments, R y is C 2~6 In some embodiments, R is alkynyl. y is C alkynyl. In some embodiments, R y is C alkynyl. In some embodiments, R y is C4 alkynyl. In some embodiments, R y is C5 alkynyl. In some embodiments, R y is a C6 alkynyl.
[0112] In some embodiments, R y is C 1~6 In some embodiments, R is alkoxy. y is methoxy. In some embodiments, R y is ethoxy. In some embodiments, R y is propoxy. In some embodiments, R y is butoxy. In some embodiments, R yis pentoxy. In some embodiments, R y is hexoxy.
[0113] In some embodiments, R y is a halogen, -CN, -OH, or -NH2.
[0114] In some embodiments, R y is a halogen. In some embodiments, R y is F, Cl, Br, or I. In some embodiments, R y is F, Cl, or Br. In some embodiments, R y is F. In some embodiments, R y is Cl. In some embodiments, R y is Br. In some embodiments, R y is I.
[0115] In some embodiments, R y is -CN. In some embodiments, R y is —OH. In some embodiments, R y is -NH2.
[0116] In some embodiments, R y is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0117] In some embodiments, R y is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0118] In some embodiments, R y is a 3-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R y is a 4-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R yis a 5-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R y is a 6-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R y is a 7-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R y is an 8-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R y is a 9-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R y is a 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S.
[0119] In some embodiments, R y is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0120] In some embodiments, R y is a 5-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R y is a 6-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R y is a 7-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R y is an 8-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R y is a 9-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R y is a 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S.
[0121] In some embodiments, each R y is H, C1~6 alkyl, or -OH.
[0122] In some embodiments, R is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0123] In some embodiments, R1 is H.
[0124] In some embodiments, R is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0125] In some embodiments, R is C 1~6 In some embodiments, R1 is alkyl. In some embodiments, R1 is methyl. In some embodiments, R1 is ethyl. In some embodiments, R1 is propyl. In some embodiments, R1 is butyl. In some embodiments, R1 is pentyl. In some embodiments, R1 is hexyl. In some embodiments, R1 is isopropyl. In some embodiments, R1 is isobutyl. In some embodiments, R1 is isopentyl. In some embodiments, R1 is isohexyl. In some embodiments, R1 is secbutyl. In some embodiments, R1 is secpentyl. In some embodiments, R1 is sechexyl. In some embodiments, R1 is tertbutyl.
[0126] In some embodiments, R is C 2~6 In some embodiments, R1 is C2 alkenyl. In some embodiments, R1 is C3 alkenyl. In some embodiments, R1 is C4 alkenyl. In some embodiments, R1 is C5 alkenyl. In some embodiments, R1 is C6 alkenyl.
[0127] In some embodiments, R is C 2~6In some embodiments, R1 is C2 alkynyl. In some embodiments, R1 is C3 alkynyl. In some embodiments, R1 is C4 alkynyl. In some embodiments, R1 is C5 alkynyl. In some embodiments, R1 is C6 alkynyl.
[0128] In some embodiments, each R is H or C 1~6 It is alkyl.
[0129] In some embodiments, R2 and R3 are each independently selected from H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11 )2, or -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein neither R2 nor R3 is H, and wherein said -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 It may be substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O and S.
[0130] In some embodiments, R2 and R3 are each independently selected from H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2, wherein neither R2 nor R3 is H, and wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 It may be substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O and S.
[0131] In some embodiments, R2 and R3 are each independently selected from H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11 )2, or —O—(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S).
[0132] In some embodiments, R2 and R3 are each independently selected from H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11)2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2, where neither R2 nor R3 is H.
[0133] In some embodiments, R2 and R3 are each independently C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11 )2, or —O—(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S).
[0134] In some embodiments, R2 and R3 are each independently C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0135] In some embodiments, R2 and R3 are each independently -OC 1~6 Alkyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, or -C(O)NR 11 -S(O)2R 11 is.
[0136] In some embodiments, neither R2 nor R3 is H.
[0137] In some embodiments, R2 is not H.
[0138] In some embodiments, R3 is not H.
[0139] In some embodiments, R2 is H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11 )2, or -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein neither R2 nor R3 is H, and wherein said -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 It may be substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O and S.
[0140] In some embodiments, R2 is H, C 2~6 Alkenyl, C 2~6Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2, wherein neither R2 nor R3 is H, and wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 It may be substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O and S.
[0141] In some embodiments, R2 is H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11 )2, or —O—(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S).
[0142] In some embodiments, R2 is H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0143] In some embodiments, R2 is H.
[0144] In some embodiments, R2 is C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11 )2, or —O—(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S).
[0145] In some embodiments, R2 is C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR11 -S(O)2-N(R 11 )2.
[0146] In some embodiments, R2 is C 2~6 Alkenyl or C 2~6 It is alkynyl.
[0147] In some embodiments, R2 is C 2~6 In some embodiments, R2 is C2 alkenyl. In some embodiments, R2 is C3 alkenyl. In some embodiments, R2 is C4 alkenyl. In some embodiments, R2 is C5 alkenyl. In some embodiments, R2 is C6 alkenyl.
[0148] In some embodiments, R2 is C 2~6 In some embodiments, R2 is C2 alkynyl. In some embodiments, R2 is C3 alkynyl. In some embodiments, R2 is C4 alkynyl. In some embodiments, R2 is C5 alkynyl. In some embodiments, R2 is C6 alkynyl.
[0149] In some embodiments, R2 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0150] In some embodiments, R2 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 alkynyl, wherein the -OC 1~6Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 It may be substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O and S.
[0151] In some embodiments, R2 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 alkynyl, wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 It may be substituted with aryl.
[0152] In some embodiments, R2 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 alkynyl, wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 The alkynyl may be substituted with a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0153] In some embodiments, R2 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 alkynyl, wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S;
[0154] In some embodiments, R2 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC2~6 alkynyl, wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 It is substituted with aryl.
[0155] In some embodiments, R2 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 alkynyl, wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 The alkynyl is substituted with a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0156] In some embodiments, R2 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 It is alkynyl.
[0157] In some embodiments, R2 is C 6~10 -OC, optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; 1~6 It is alkyl.
[0158] In some embodiments, R2 is C 6~10 -OC optionally substituted with aryl 1~6 It is alkyl.
[0159] In some embodiments, R2 is -OC optionally substituted with phenyl. 1~6 It is alkyl.
[0160] In some embodiments, R2 is -O-methyl optionally substituted with phenyl.
[0161] In some embodiments, R2 is -OC substituted with phenyl.1~6 It is alkyl.
[0162] In some embodiments, R2 is -O-methyl substituted with phenyl.
[0163] In some embodiments, R2 is an optionally substituted 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, -OC 1~6 It is alkyl.
[0164] In some embodiments, R2 is C 6~10 -OC substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; 1~6 It is alkyl.
[0165] In some embodiments, R2 is C 6~10 Aryl-substituted -OC 1~6 It is alkyl.
[0166] In some embodiments, R2 is -OC substituted with a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. 1~6 It is alkyl.
[0167] In some embodiments, R2 is -OC 1~6In some embodiments, R2 is -O-methyl. In some embodiments, R2 is -O-ethyl. In some embodiments, R2 is -O-propyl. In some embodiments, R2 is -O-butyl. In some embodiments, R2 is -O-pentyl. In some embodiments, R2 is -O-hexyl. In some embodiments, R2 is -O-isopropyl. In some embodiments, R2 is -O-isobutyl. In some embodiments, R2 is -O-isopentyl. In some embodiments, R2 is -O-isohexyl. In some embodiments, R2 is -O-secbutyl. In some embodiments, R2 is -O-secpentyl. In some embodiments, R2 is -O-sechexyl. In some embodiments, R2 is -O-tertbutyl.
[0168] In some embodiments, R2 is C 6~10 -OC, optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; 2~6 It is alkenyl.
[0169] In some embodiments, R2 is C 6~10 -OC optionally substituted with aryl 2~6 It is alkenyl.
[0170] In some embodiments, R2 is an optionally substituted 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, -OC 2~6 It is alkenyl.
[0171] In some embodiments, R2 is C 6~10 -OC substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; 2~6 It is alkenyl.
[0172] In some embodiments, R2 is C 6~10 Aryl-substituted -OC 2~6It is alkenyl.
[0173] In some embodiments, R2 is -OC substituted with a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. 2~6 It is alkenyl.
[0174] In some embodiments, R2 is -OC 2~6 In some embodiments, R2 is -O-C2 alkenyl. In some embodiments, R2 is -O-C3 alkenyl. In some embodiments, R2 is -O-C4 alkenyl. In some embodiments, R2 is -O-C5 alkenyl. In some embodiments, R2 is -O-C6 alkenyl.
[0175] In some embodiments, R2 is C 6~10 -OC, optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; 2~6 It is alkynyl.
[0176] In some embodiments, R2 is C 6~10 -OC optionally substituted with aryl 2~6 It is alkynyl.
[0177] In some embodiments, R2 is an optionally substituted 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, -OC 2~6 It is alkynyl.
[0178] In some embodiments, R2 is C 6~10 -OC substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; 2~6 It is alkynyl.
[0179] In some embodiments, R2 is C 6~10 Aryl-substituted -OC 2~6 It is alkynyl.
[0180] In some embodiments, R2 is -OC substituted with a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. 2~6 It is alkynyl.
[0181] In some embodiments, R2 is -OC 2~6 In some embodiments, R2 is -O-C2 alkynyl. In some embodiments, R2 is -O-C3 alkynyl. In some embodiments, R2 is -O-C4 alkynyl. In some embodiments, R2 is -O-C5 alkynyl. In some embodiments, R2 is -O-C6 alkynyl.
[0182] In some embodiments, R2 is -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0183] In some embodiments, R2 is -C(O)R 11 , -C(O)OR 11 , or -C(O)N(R 11 )2.
[0184] In some embodiments, R2 is -C(O)R 11 In some embodiments, R2 is -C(O)OR 11 In some embodiments, R2 is —C(O)N(R 11 )2.
[0185] In some embodiments, R2 is -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11, or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0186] In some embodiments, R2 is -C(O)NR 11 -S(O)2R 11 In some embodiments, R2 is -C(O)NR 11 -S(O)2-OR 11 In some embodiments, R2 is -C(O)NR 11 -S(O)2-N(R 11 )2.
[0187] In some embodiments, R2 is -OC 1~6 Alkyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, or -C(O)NR 11 -S(O)2R 11 is.
[0188] In some embodiments, R2 is -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S).
[0189] In some embodiments, R2 is -O-(5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S). In some embodiments, R2 is -O-(6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S). In some embodiments, R2 is -O-(7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S). In some embodiments, R2 is -O-(8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S). In some embodiments, R2 is -O-(9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S). In some embodiments, R2 is -O-(10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S).
[0190] In some embodiments, R2 is -O-methyl, -O-methyl substituted with phenyl, or -C(O)2CH3.
[0191] In some embodiments, R2 is -O-methyl or -O-methyl substituted with phenyl.
[0192] In some embodiments, R3 is H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11 )2, or -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein neither R2 nor R3 is H, and wherein said -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 It may be substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O and S.
[0193] In some embodiments, R3 is H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11-S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2, wherein neither R2 nor R3 is H, and wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 It may be substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O and S.
[0194] In some embodiments, R3 is H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11 )2, or —O—(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S).
[0195] In some embodiments, R3 is H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R11 )2.
[0196] In some embodiments, R3 is H.
[0197] In some embodiments, R3 is C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , -C(O)NR 11 -S(O)2-N(R 11 )2, or —O—(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S).
[0198] In some embodiments, R3 is C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0199] In some embodiments, R3 is C 2~6 Alkenyl or C 2~6 It is alkynyl.
[0200] In some embodiments, R3 is C2~6 In some embodiments, R3 is C2 alkenyl. In some embodiments, R3 is C3 alkenyl. In some embodiments, R3 is C4 alkenyl. In some embodiments, R3 is C5 alkenyl. In some embodiments, R3 is C6 alkenyl.
[0201] In some embodiments, R3 is C 2~6 In some embodiments, R3 is C2 alkynyl. In some embodiments, R3 is C3 alkynyl. In some embodiments, R3 is C4 alkynyl. In some embodiments, R3 is C5 alkynyl. In some embodiments, R3 is C6 alkynyl.
[0202] In some embodiments, R3 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0203] In some embodiments, R3 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 alkynyl, wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 It may be substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O and S.
[0204] In some embodiments, R3 is -OC 1~6Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 alkynyl, wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 It may be substituted with aryl.
[0205] In some embodiments, R3 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 alkynyl, wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 The alkynyl may be substituted with a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0206] In some embodiments, R3 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 alkynyl, wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S;
[0207] In some embodiments, R3 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 alkynyl, wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 Alkynyl is C 6~10 It is substituted with aryl.
[0208] In some embodiments, R3 is -OC 1~6 Alkyl, -OC2~6 Alkenyl, or -OC 2~6 alkynyl, wherein the -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 The alkynyl is substituted with a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0209] In some embodiments, R3 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 It is alkynyl.
[0210] In some embodiments, R3 is C 6~10 -OC, optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; 1~6 It is alkyl.
[0211] In some embodiments, R3 is C 6~10 -OC optionally substituted with aryl 1~6 It is alkyl.
[0212] In some embodiments, R3 is -OC optionally substituted with phenyl. 1~6 It is alkyl.
[0213] In some embodiments, R3 is -O-methyl optionally substituted with phenyl.
[0214] In some embodiments, R3 is -OC substituted with phenyl. 1~6 It is alkyl.
[0215] In some embodiments, R3 is -O-methyl substituted with phenyl.
[0216] In some embodiments, R3 is an optionally substituted 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, -OC1~6 It is alkyl.
[0217] In some embodiments, R3 is C 6~10 -OC substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; 1~6 It is alkyl.
[0218] In some embodiments, R3 is C 6~10 Aryl-substituted -OC 1~6 It is alkyl.
[0219] In some embodiments, R3 is -OC substituted with a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. 1~6 It is alkyl.
[0220] In some embodiments, R3 is -OC 1~6 In some embodiments, R3 is -O-methyl. In some embodiments, R3 is -O-ethyl. In some embodiments, R3 is -O-propyl. In some embodiments, R3 is -O-butyl. In some embodiments, R3 is -O-pentyl. In some embodiments, R3 is -O-hexyl. In some embodiments, R3 is -O-isopropyl. In some embodiments, R3 is -O-isobutyl. In some embodiments, R3 is -O-isopentyl. In some embodiments, R3 is -O-isohexyl. In some embodiments, R3 is -O-secbutyl. In some embodiments, R3 is -O-secpentyl. In some embodiments, R3 is -O-sechexyl. In some embodiments, R3 is -O-tertbutyl.
[0221] In some embodiments, R3 is C 6~10 -OC, optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; 2~6 It is alkenyl.
[0222] In some embodiments, R3 is C 6~10 -OC optionally substituted with aryl 2~6 It is alkenyl.
[0223] In some embodiments, R3 is an optionally substituted 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, -OC 2~6 It is alkenyl.
[0224] In some embodiments, R3 is C 6~10 -OC substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; 2~6 It is alkenyl.
[0225] In some embodiments, R3 is C 6~10 Aryl-substituted -OC 2~6 It is alkenyl.
[0226] In some embodiments, R3 is -OC substituted with a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. 2~6 It is alkenyl.
[0227] In some embodiments, R3 is -OC 2~6 In some embodiments, R3 is -O-C2 alkenyl. In some embodiments, R3 is -O-C3 alkenyl. In some embodiments, R3 is -O-C4 alkenyl. In some embodiments, R3 is -O-C5 alkenyl. In some embodiments, R3 is -O-C6 alkenyl.
[0228] In some embodiments, R3 is C 6~10 -OC, optionally substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; 2~6 It is alkynyl.
[0229] In some embodiments, R3 is C 6~10 -OC optionally substituted with aryl 2~6 It is alkynyl.
[0230] In some embodiments, R3 is an optionally substituted 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, -OC 2~6 It is alkynyl.
[0231] In some embodiments, R3 is C 6~10 -OC substituted with aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; 2~6 It is alkynyl.
[0232] In some embodiments, R3 is C 6~10 Aryl-substituted -OC 2~6 It is alkynyl.
[0233] In some embodiments, R3 is -OC substituted with a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. 2~6 It is alkynyl.
[0234] In some embodiments, R3 is -OC 2~6 In some embodiments, R3 is -O-C2 alkynyl. In some embodiments, R3 is -O-C3 alkynyl. In some embodiments, R3 is -O-C4 alkynyl. In some embodiments, R3 is -O-C5 alkynyl. In some embodiments, R3 is -O-C6 alkynyl.
[0235] In some embodiments, R3 is -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11, or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0236] In some embodiments, R3 is -C(O)R 11 , -C(O)OR 11 , or -C(O)N(R 11 )2.
[0237] In some embodiments, R3 is -C(O)R 11 In some embodiments, R3 is -C(O)OR 11 In some embodiments, R3 is —C(O)N(R 11 )2.
[0238] In some embodiments, R3 is -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0239] In some embodiments, R3 is -C(O)NR 11 -S(O)2R 11 In some embodiments, R3 is -C(O)NR 11 -S(O)2-OR 11 In some embodiments, R3 is -C(O)NR 11 -S(O)2-N(R 11 )2.
[0240] In some embodiments, R3 is -OC 1~6 Alkyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, or -C(O)NR 11 -S(O)2R 11 is.
[0241] In some embodiments, R3 is -O-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S).
[0242] In some embodiments, R3 is -O-(5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S). In some embodiments, R3 is -O-(6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S). In some embodiments, R3 is -O-(7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S). In some embodiments, R3 is -O-(8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S). In some embodiments, R3 is -O-(9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S). In some embodiments, R3 is -O-(10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S).
[0243] In some embodiments, R3 is -O-methyl, -O-methyl substituted with phenyl, or -C(O)2CH3.
[0244] In some embodiments, R3 is -O-methyl or -O-methyl substituted with phenyl.
[0245] In some embodiments, R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7.
[0246] In some embodiments, R5 and R6 are each independently C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7.
[0247] In some embodiments, R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0248] In some embodiments, R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0249] In some embodiments, R5 and R6 are each independently H.
[0250] In some embodiments, R5 and R6 are each independently C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0251] In some embodiments, R5 and R6 are each independently C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0252] In some embodiments, R5 and R6 are each independently H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5- to 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0253] In some embodiments, R5 and R6 are each independently H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0254] In some embodiments, R5 and R6 are each independently H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is substituted with one or more R7.
[0255] In some embodiments, R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is substituted with one or more R7.
[0256] In some embodiments, R5 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0257] In some embodiments, R5 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0258] In some embodiments, R5 is H.
[0259] In some embodiments, R5 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0260] In some embodiments, R5 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0261] In some embodiments, R5 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynyl, wherein said alkyl, alkenyl, or alkynyl is optionally substituted with one or more R7.
[0262] In some embodiments, R5 is a C optionally substituted with one or more R7 1~6In some embodiments, R5 is alkyl. In some embodiments, R5 is methyl, optionally substituted with one or more R7. In some embodiments, R5 is ethyl, optionally substituted with one or more R7. In some embodiments, R5 is propyl, optionally substituted with one or more R7. In some embodiments, R5 is butyl, optionally substituted with one or more R7. In some embodiments, R5 is pentyl, optionally substituted with one or more R7. In some embodiments, R5 is hexyl, optionally substituted with one or more R7. In some embodiments, R5 is isopropyl, optionally substituted with one or more R7. In some embodiments, R5 is isobutyl, optionally substituted with one or more R7. In some embodiments, R5 is isopentyl, optionally substituted with one or more R7. In some embodiments, R5 is isohexyl, optionally substituted with one or more R7. In some embodiments, R5 is secbutyl, optionally substituted with one or more R7. In some embodiments, R5 is sec-pentyl, optionally substituted with one or more R7. In some embodiments, R5 is sec-hexyl, optionally substituted with one or more R7. In some embodiments, R5 is tert-butyl, optionally substituted with one or more R7.
[0263] In some embodiments, R5 is a C optionally substituted with one or more R7 2~6 In some embodiments, R5 is C2 alkenyl optionally substituted with one or more R7. In some embodiments, R5 is C3 alkenyl optionally substituted with one or more R7. In some embodiments, R5 is C4 alkenyl optionally substituted with one or more R7. In some embodiments, R5 is C5 alkenyl optionally substituted with one or more R7. In some embodiments, R5 is C6 alkenyl optionally substituted with one or more R7.
[0264] In some embodiments, R5 is a C optionally substituted with one or more R7 2~6 In some embodiments, R5 is C2 alkynyl optionally substituted with one or more R7. In some embodiments, R5 is C3 alkynyl optionally substituted with one or more R7. In some embodiments, R5 is C4 alkynyl optionally substituted with one or more R7. In some embodiments, R5 is C5 alkynyl optionally substituted with one or more R7. In some embodiments, R5 is C6 alkynyl optionally substituted with one or more R7.
[0265] In some embodiments, R5 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynyl, wherein said alkyl, alkenyl, or alkynyl is substituted with one or more R7.
[0266] In some embodiments, R5 is a C substituted with one or more R7 1~6In some embodiments, R5 is alkyl. In some embodiments, R5 is methyl substituted with one or more R7. In some embodiments, R5 is ethyl substituted with one or more R7. In some embodiments, R5 is propyl substituted with one or more R7. In some embodiments, R5 is butyl substituted with one or more R7. In some embodiments, R5 is pentyl substituted with one or more R7. In some embodiments, R5 is hexyl substituted with one or more R7. In some embodiments, R5 is isopropyl substituted with one or more R7. In some embodiments, R5 is isobutyl substituted with one or more R7. In some embodiments, R5 is isopentyl substituted with one or more R7. In some embodiments, R5 is isohexyl substituted with one or more R7. In some embodiments, R5 is secbutyl substituted with one or more R7. In some embodiments, R5 is sec-pentyl substituted with one or more R7. In some embodiments, R5 is sec-hexyl substituted with one or more R7. In some embodiments, R5 is tert-butyl substituted with one or more R7.
[0267] In some embodiments, R5 is a C substituted with one or more R7 2~6 In some embodiments, R5 is C2 alkenyl substituted with one or more R7. In some embodiments, R5 is C3 alkenyl substituted with one or more R7. In some embodiments, R5 is C4 alkenyl substituted with one or more R7. In some embodiments, R5 is C5 alkenyl substituted with one or more R7. In some embodiments, R5 is C6 alkenyl substituted with one or more R7.
[0268] In some embodiments, R5 is a C substituted with one or more R7 2~6In some embodiments, R5 is a C2 alkynyl substituted with one or more R7. In some embodiments, R5 is a C3 alkynyl substituted with one or more R7. In some embodiments, R5 is a C4 alkynyl substituted with one or more R7. In some embodiments, R5 is a C5 alkynyl substituted with one or more R7. In some embodiments, R5 is a C6 alkynyl substituted with one or more R7.
[0269] In some embodiments, R5 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynyl, wherein said alkyl, alkenyl, or alkynyl is substituted with one R7.
[0270] In some embodiments, R5 is C substituted with 1 R7 1~6 In some embodiments, R5 is alkyl. In some embodiments, R5 is methyl substituted with one R7. In some embodiments, R5 is ethyl substituted with one R7. In some embodiments, R5 is propyl substituted with one R7. In some embodiments, R5 is butyl substituted with one R7. In some embodiments, R5 is pentyl substituted with one R7. In some embodiments, R5 is hexyl substituted with one R7. In some embodiments, R5 is isopropyl substituted with one R7. In some embodiments, R5 is isobutyl substituted with one R7. In some embodiments, R5 is isopentyl substituted with one R7. In some embodiments, R5 is isohexyl substituted with one R7. In some embodiments, R5 is secbutyl substituted with one R7. In some embodiments, R5 is secpentyl substituted with one R7. In some embodiments, R5 is sechexyl substituted with 1 R7. In some embodiments, R5 is tertbutyl substituted with 1 R7.
[0271] In some embodiments, R5 is C substituted with 1 R72~6 In some embodiments, R5 is C2 alkenyl substituted with 1 R7. In some embodiments, R5 is C3 alkenyl substituted with 1 R7. In some embodiments, R5 is C4 alkenyl substituted with 1 R7. In some embodiments, R5 is C5 alkenyl substituted with 1 R7. In some embodiments, R5 is C6 alkenyl substituted with 1 R7.
[0272] In some embodiments, R5 is C substituted with 1 R7 2~6 In some embodiments, R5 is C2 alkynyl substituted with 1 R7. In some embodiments, R5 is C3 alkynyl substituted with 1 R7. In some embodiments, R5 is C4 alkynyl substituted with 1 R7. In some embodiments, R5 is C5 alkynyl substituted with 1 R7. In some embodiments, R5 is C6 alkynyl substituted with 1 R7.
[0273] In some embodiments, R5 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0274] In some embodiments, R5 is C 1~6 In some embodiments, R5 is alkyl. In some embodiments, R5 is methyl. In some embodiments, R5 is ethyl. In some embodiments, R5 is propyl. In some embodiments, R5 is butyl. In some embodiments, R5 is pentyl. In some embodiments, R5 is hexyl. In some embodiments, R5 is isopropyl. In some embodiments, R5 is isobutyl. In some embodiments, R5 is isopentyl. In some embodiments, R5 is isohexyl. In some embodiments, R5 is secbutyl. In some embodiments, R5 is secpentyl. In some embodiments, R5 is sechexyl. In some embodiments, R5 is tertbutyl.
[0275] In some embodiments, R5 is C 2~6 In some embodiments, R5 is C2 alkenyl. In some embodiments, R5 is C3 alkenyl. In some embodiments, R5 is C4 alkenyl. In some embodiments, R5 is C5 alkenyl. In some embodiments, R5 is C6 alkenyl.
[0276] In some embodiments, R5 is C 2~6 In some embodiments, R5 is C2 alkynyl. In some embodiments, R5 is C3 alkynyl. In some embodiments, R5 is C4 alkynyl. In some embodiments, R5 is C5 alkynyl. In some embodiments, R5 is C6 alkynyl.
[0277] In some embodiments, R5 is C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0278] In some embodiments, R5 is C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0279] In some embodiments, R5 is C 3~10 cycloalkyl or 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl or heterocyclyl is optionally substituted with one or more R7.
[0280] In some embodiments, R5 is C 3~10 cycloalkyl or a 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S.
[0281] In some embodiments, R5 is a C optionally substituted with one or more R7 3~10 It is cycloalkyl.
[0282] In some embodiments, R5 is a C3 cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C4 cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C5 cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C6 cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C7 cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C8 cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C9 cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C6 cycloalkyl optionally substituted with one or more R7. 10 It is cycloalkyl.
[0283] In some embodiments, R5 is a C3-C7 monocyclic cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C3-C7 monocyclic saturated cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C3-C7 monocyclic partially saturated cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C9-C7 monocyclic partially saturated cycloalkyl optionally substituted with one or more R7. 10 In some embodiments, R5 is a C9-C cycloalkyl optionally substituted with one or more R7. 10 In some embodiments, R5 is a C9-C cycloalkyl group optionally substituted with one or more R7.10 In some embodiments, R5 is a C8-C6 bicyclic partially saturated cycloalkyl optionally substituted with one or more R7. 10 It is a polycyclic cycloalkyl.
[0284] In some embodiments, R5 is a C substituted with one or more R7 3~10 It is cycloalkyl.
[0285] In some embodiments, R5 is a C3 cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C4 cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C5 cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C6 cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C7 cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C8 cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C9 cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C6 cycloalkyl substituted with one or more R7. 10 It is cycloalkyl.
[0286] In some embodiments, R5 is a C3-C7 monocyclic cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C3-C7 monocyclic saturated cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C9-C7 monocyclic partially saturated cycloalkyl substituted with one or more R7. 10 In some embodiments, R5 is a C9-C substituted with one or more R7. 10 In some embodiments, R5 is a C9-C substituted bicyclic saturated cycloalkyl. 10 In some embodiments, R5 is a C8-C substituted with one or more R7.10 It is a polycyclic cycloalkyl.
[0287] In some embodiments, R5 is C substituted with 1 R7 3~10 It is cycloalkyl.
[0288] In some embodiments, R5 is C3 cycloalkyl substituted with one R7. In some embodiments, R5 is C4 cycloalkyl substituted with one R7. In some embodiments, R5 is C5 cycloalkyl substituted with one R7. In some embodiments, R5 is C6 cycloalkyl substituted with one R7. In some embodiments, R5 is C7 cycloalkyl substituted with one R7. In some embodiments, R5 is C8 cycloalkyl substituted with one R7. In some embodiments, R5 is C9 cycloalkyl substituted with one R7. In some embodiments, R5 is C6 cycloalkyl substituted with one R7. In some embodiments, R5 is C7 cycloalkyl substituted with one R7. 10 It is cycloalkyl.
[0289] In some embodiments, R5 is a C3-C7 monocyclic cycloalkyl substituted with one R7. In some embodiments, R5 is a C3-C7 monocyclic saturated cycloalkyl substituted with one R7. In some embodiments, R5 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one R7. In some embodiments, R5 is a C9-C1 monocyclic partially saturated cycloalkyl substituted with one R7. 10 In some embodiments, R5 is a C9-C cycloalkyl substituted with one R7. 10 In some embodiments, R5 is a C9-C substituted with one R7. 10 In some embodiments, R5 is a C8-C substituted with one R7. 10 It is a polycyclic cycloalkyl.
[0290] In some embodiments, R5 is C 3~10 It is cycloalkyl.
[0291] In some embodiments, R5 is C3 cycloalkyl. In some embodiments, R5 is C4 cycloalkyl. In some embodiments, R5 is C5 cycloalkyl. In some embodiments, R5 is C6 cycloalkyl. In some embodiments, R5 is C7 cycloalkyl. In some embodiments, R5 is C8 cycloalkyl. In some embodiments, R5 is C9 cycloalkyl. In some embodiments, R5 is C 10 It is cycloalkyl.
[0292] In some embodiments, R5 is a C3-C7 monocyclic cycloalkyl. In some embodiments, R5 is a C3-C7 monocyclic saturated cycloalkyl. In some embodiments, R5 is a C3-C7 monocyclic partially saturated cycloalkyl. In some embodiments, R5 is a C9-C 10 In some embodiments, R5 is a C9-C 10 In some embodiments, R5 is a C9-C 10 In some embodiments, R5 is a C8-C 10 It is a polycyclic cycloalkyl.
[0293] In some embodiments, R5 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 11-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0294] In some embodiments, R5 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 11-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0295] In some embodiments, R5 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 11-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0296] In some embodiments, R5 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 11-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0297] In some embodiments, R5 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0298] In some embodiments, R5 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0299] In some embodiments, R5 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0300] In some embodiments, R5 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0301] In some embodiments, R5 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 13-membered polycyclic heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0302] In some embodiments, R5 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0303] In some embodiments, R5 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0304] In some embodiments, R5 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0305] In some embodiments, R5 is C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the aryl or heteroaryl is optionally substituted with one or more R7.
[0306] In some embodiments, R5 is C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0307] In some embodiments, R5 is a C optionally substituted with one or more R7 6~10 It is aryl.
[0308] In some embodiments, R5 is a C optionally substituted with one or more R7 6~8 In some embodiments, R5 is phenyl optionally substituted with one or more R7.
[0309] In some embodiments, R5 is a C substituted with one or more R7 6~8 In some embodiments, R5 is phenyl substituted with one or more R7.
[0310] In some embodiments, R5 is C substituted with 1 R7 6~8 In some embodiments, R5 is phenyl substituted with 1 R7.
[0311] In some embodiments, R5 is C 6~10 It is aryl.
[0312] In some embodiments, R5 is C 6~8 In some embodiments, R5 is phenyl.
[0313] In some embodiments, R5 is a 5- to 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 11-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0314] In some embodiments, R5 is a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 11-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0315] In some embodiments, R5 is a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 11-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0316] In some embodiments, R5 is a 5- to 13-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 5-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 6-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 7-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 8-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 9-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 11-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0317] In some embodiments, R5 is a 9- to 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 9-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 10-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 11-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 12-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0318] In some embodiments, R5 is a 9-13 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 9 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 10 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 11 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 12 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0319] In some embodiments, R5 is a 9-13 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 9 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 10 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 11 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 12 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0320] In some embodiments, R5 is a 9- to 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 9-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 10-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 11-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 12-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0321] In some embodiments, R5 is a 9- to 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 9-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 10-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 11-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 12-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 13-membered polycyclic heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0322] In some embodiments, R5 is a 9-13 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 9 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 10 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 11 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 12 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0323] In some embodiments, R5 is a 9-13 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 9 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 10 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 11 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 12 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0324] In some embodiments, R5 is a 9- to 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 9-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 10-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 11-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 12-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0325] In some embodiments, R5 is H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10aryl, a 5- to 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0326] In some embodiments, R5 is H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0327] In some embodiments, R5 is H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is substituted with one or more R7.
[0328] In some embodiments, R5 is cyclopropyl, piperidine, tetrahydropyran, morpholine, phenyl, pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0329] In some embodiments, R5 is cyclopropyl, piperidine, tetrahydropyran, or morpholine.
[0330] In some embodiments, R5 is phenyl, pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0331] In some embodiments, R5 is pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0332] In some embodiments, R5 is pyridine, pyrimidine, or indazole.
[0333] In some embodiments, R5 is indazole.
[0334] In some embodiments, R5 is tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0335] In some embodiments, R5 is tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, or imidazole.
[0336] In some embodiments, R5 is 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0337] In some embodiments, R5 is 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, or benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole.
[0338] In some embodiments, R5 is 9H-carbazole.
[0339] In some embodiments, R6 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0340] In some embodiments, R6 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0341] In some embodiments, R6 is H.
[0342] In some embodiments, R6 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0343] In some embodiments, R6 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0344] In some embodiments, R6 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynyl, wherein said alkyl, alkenyl, or alkynyl is optionally substituted with one or more R7.
[0345] In some embodiments, R6 is a C optionally substituted with one or more R7 1~6In some embodiments, R6 is alkyl. In some embodiments, R6 is methyl, optionally substituted with one or more R7. In some embodiments, R6 is ethyl, optionally substituted with one or more R7. In some embodiments, R6 is propyl, optionally substituted with one or more R7. In some embodiments, R6 is butyl, optionally substituted with one or more R7. In some embodiments, R6 is pentyl, optionally substituted with one or more R7. In some embodiments, R6 is hexyl, optionally substituted with one or more R7. In some embodiments, R6 is isopropyl, optionally substituted with one or more R7. In some embodiments, R6 is isobutyl, optionally substituted with one or more R7. In some embodiments, R6 is isopentyl, optionally substituted with one or more R7. In some embodiments, R6 is isohexyl, optionally substituted with one or more R7. In some embodiments, R6 is secbutyl, optionally substituted with one or more R7. In some embodiments, R6 is sec-pentyl, optionally substituted with one or more R7. In some embodiments, R6 is sec-hexyl, optionally substituted with one or more R7. In some embodiments, R6 is tert-butyl, optionally substituted with one or more R7.
[0346] In some embodiments, R6 is a C optionally substituted with one or more R7 2~6 In some embodiments, R6 is C2 alkenyl optionally substituted with one or more R7. In some embodiments, R6 is C3 alkenyl optionally substituted with one or more R7. In some embodiments, R6 is C4 alkenyl optionally substituted with one or more R7. In some embodiments, R6 is C5 alkenyl optionally substituted with one or more R7. In some embodiments, R6 is C6 alkenyl optionally substituted with one or more R7.
[0347] In some embodiments, R6 is a C optionally substituted with one or more R7 2~6 In some embodiments, R6 is C2 alkynyl optionally substituted with one or more R7. In some embodiments, R6 is C3 alkynyl optionally substituted with one or more R7. In some embodiments, R6 is C4 alkynyl optionally substituted with one or more R7. In some embodiments, R6 is C5 alkynyl optionally substituted with one or more R7. In some embodiments, R6 is C6 alkynyl optionally substituted with one or more R7.
[0348] In some embodiments, R6 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynyl, wherein said alkyl, alkenyl, or alkynyl is substituted with one or more R7.
[0349] In some embodiments, R6 is a C substituted with one or more R7 1~6In some embodiments, R6 is alkyl. In some embodiments, R6 is methyl substituted with one or more R7. In some embodiments, R6 is ethyl substituted with one or more R7. In some embodiments, R6 is propyl substituted with one or more R7. In some embodiments, R6 is butyl substituted with one or more R7. In some embodiments, R6 is pentyl substituted with one or more R7. In some embodiments, R6 is hexyl substituted with one or more R7. In some embodiments, R6 is isopropyl substituted with one or more R7. In some embodiments, R6 is isobutyl substituted with one or more R7. In some embodiments, R6 is isopentyl substituted with one or more R7. In some embodiments, R6 is isohexyl substituted with one or more R7. In some embodiments, R6 is secbutyl substituted with one or more R7. In some embodiments, R6 is sec-pentyl substituted with one or more R7. In some embodiments, R6 is sec-hexyl substituted with one or more R7. In some embodiments, R6 is tert-butyl substituted with one or more R7.
[0350] In some embodiments, R6 is a C substituted with one or more R7 2~6 In some embodiments, R6 is C2 alkenyl substituted with one or more R7. In some embodiments, R6 is C3 alkenyl substituted with one or more R7. In some embodiments, R6 is C4 alkenyl substituted with one or more R7. In some embodiments, R6 is C5 alkenyl substituted with one or more R7. In some embodiments, R6 is C6 alkenyl substituted with one or more R7.
[0351] In some embodiments, R6 is a C substituted with one or more R7 2~6In some embodiments, R6 is a C2 alkynyl substituted with one or more R7. In some embodiments, R6 is a C3 alkynyl substituted with one or more R7. In some embodiments, R6 is a C4 alkynyl substituted with one or more R7. In some embodiments, R6 is a C5 alkynyl substituted with one or more R7. In some embodiments, R6 is a C6 alkynyl substituted with one or more R7.
[0352] In some embodiments, R6 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynyl, wherein said alkyl, alkenyl, or alkynyl is substituted with one R7.
[0353] In some embodiments, R6 is C substituted with 1 R7 1~6 In some embodiments, R6 is alkyl. In some embodiments, R6 is methyl substituted with one R7. In some embodiments, R6 is ethyl substituted with one R7. In some embodiments, R6 is propyl substituted with one R7. In some embodiments, R6 is butyl substituted with one R7. In some embodiments, R6 is pentyl substituted with one R7. In some embodiments, R6 is hexyl substituted with one R7. In some embodiments, R6 is isopropyl substituted with one R7. In some embodiments, R6 is isobutyl substituted with one R7. In some embodiments, R6 is isopentyl substituted with one R7. In some embodiments, R6 is isohexyl substituted with one R7. In some embodiments, R6 is secbutyl substituted with one R7. In some embodiments, R6 is secpentyl substituted with one R7. In some embodiments, R6 is sechexyl substituted with 1 R7. In some embodiments, R6 is tertbutyl substituted with 1 R7.
[0354] In some embodiments, R6 is C substituted with 1 R72~6 In some embodiments, R6 is C2 alkenyl substituted with 1 R7. In some embodiments, R6 is C3 alkenyl substituted with 1 R7. In some embodiments, R6 is C4 alkenyl substituted with 1 R7. In some embodiments, R6 is C5 alkenyl substituted with 1 R7. In some embodiments, R6 is C6 alkenyl substituted with 1 R7.
[0355] In some embodiments, R6 is C substituted with 1 R7 2~6 In some embodiments, R6 is a C2 alkynyl substituted with 1 R7. In some embodiments, R6 is a C3 alkynyl substituted with 1 R7. In some embodiments, R6 is a C4 alkynyl substituted with 1 R7. In some embodiments, R6 is a C5 alkynyl substituted with 1 R7. In some embodiments, R6 is a C6 alkynyl substituted with 1 R7.
[0356] In some embodiments, R6 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0357] In some embodiments, R6 is C 1~6 In some embodiments, R6 is alkyl. In some embodiments, R6 is methyl. In some embodiments, R6 is ethyl. In some embodiments, R6 is propyl. In some embodiments, R6 is butyl. In some embodiments, R6 is pentyl. In some embodiments, R6 is hexyl. In some embodiments, R6 is isopropyl. In some embodiments, R6 is isobutyl. In some embodiments, R6 is isopentyl. In some embodiments, R6 is isohexyl. In some embodiments, R6 is secbutyl. In some embodiments, R6 is secpentyl. In some embodiments, R6 is sechexyl. In some embodiments, R6 is tertbutyl.
[0358] In some embodiments, R6 is C 2~6 In some embodiments, R6 is C2 alkenyl. In some embodiments, R6 is C3 alkenyl. In some embodiments, R6 is C4 alkenyl. In some embodiments, R6 is C5 alkenyl. In some embodiments, R6 is C6 alkenyl.
[0359] In some embodiments, R6 is C 2~6 In some embodiments, R6 is C2 alkynyl. In some embodiments, R6 is C3 alkynyl. In some embodiments, R6 is C4 alkynyl. In some embodiments, R6 is C5 alkynyl. In some embodiments, R6 is C6 alkynyl.
[0360] In some embodiments, R6 is C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0361] In some embodiments, R6 is C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0362] In some embodiments, R6 is C 3~10 cycloalkyl or 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl or heterocyclyl is optionally substituted with one or more R7.
[0363] In some embodiments, R6 is C 3~10 cycloalkyl or a 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S.
[0364] In some embodiments, R6 is a C optionally substituted with one or more R7 3~10 It is cycloalkyl.
[0365] In some embodiments, R6 is a C3 cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C4 cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C5 cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C6 cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C7 cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C8 cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C9 cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C6 cycloalkyl optionally substituted with one or more R7. 10 It is cycloalkyl.
[0366] In some embodiments, R6 is a C3-C7 monocyclic cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C3-C7 monocyclic saturated cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C3-C7 monocyclic partially saturated cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C9-C7 monocyclic partially saturated cycloalkyl optionally substituted with one or more R7. 10 In some embodiments, R6 is a C9-C cycloalkyl optionally substituted with one or more R7. 10 In some embodiments, R6 is a C9-C cycloalkyl group optionally substituted with one or more R7.10 In some embodiments, R6 is a C8-C6 bicyclic partially saturated cycloalkyl optionally substituted with one or more R7. 10 It is a polycyclic cycloalkyl.
[0367] In some embodiments, R6 is a C substituted with one or more R7 3~10 It is cycloalkyl.
[0368] In some embodiments, R6 is a C3 cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C4 cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C5 cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C6 cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C7 cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C8 cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C9 cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C6 cycloalkyl substituted with one or more R7. 10 It is cycloalkyl.
[0369] In some embodiments, R6 is a C3-C7 monocyclic cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C3-C7 monocyclic saturated cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C9-C7 monocyclic partially saturated cycloalkyl substituted with one or more R7. 10 In some embodiments, R6 is a C9-C substituted with one or more R7. 10 In some embodiments, R6 is a C9-C substituted bicyclic saturated cycloalkyl. 10 In some embodiments, R6 is a C8-C substituted bicyclic partially saturated cycloalkyl.10 It is a polycyclic cycloalkyl.
[0370] In some embodiments, R6 is C substituted with 1 R7 3~10 It is cycloalkyl.
[0371] In some embodiments, R6 is a C3 cycloalkyl substituted with one R7. In some embodiments, R6 is a C4 cycloalkyl substituted with one R7. In some embodiments, R6 is a C5 cycloalkyl substituted with one R7. In some embodiments, R6 is a C6 cycloalkyl substituted with one R7. In some embodiments, R6 is a C7 cycloalkyl substituted with one R7. In some embodiments, R6 is a C8 cycloalkyl substituted with one R7. In some embodiments, R6 is a C9 cycloalkyl substituted with one R7. In some embodiments, R6 is a C6 cycloalkyl substituted with one R7. 10 It is cycloalkyl.
[0372] In some embodiments, R6 is a C3-C7 monocyclic cycloalkyl substituted with one R7. In some embodiments, R6 is a C3-C7 monocyclic saturated cycloalkyl substituted with one R7. In some embodiments, R6 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one R7. In some embodiments, R6 is a C9-C monocyclic partially saturated cycloalkyl substituted with one R7. 10 In some embodiments, R6 is a C9-C cycloalkyl substituted with one R7. 10 In some embodiments, R6 is a C9-C substituted with one R7. 10 In some embodiments, R6 is a C8-C substituted with one R7. 10 It is a polycyclic cycloalkyl.
[0373] In some embodiments, R6 is C 3~10 It is cycloalkyl.
[0374] In some embodiments, R6 is C3 cycloalkyl. In some embodiments, R6 is C4 cycloalkyl. In some embodiments, R6 is C5 cycloalkyl. In some embodiments, R6 is C6 cycloalkyl. In some embodiments, R6 is C7 cycloalkyl. In some embodiments, R6 is C8 cycloalkyl. In some embodiments, R6 is C9 cycloalkyl. In some embodiments, R6 is C 10 It is cycloalkyl.
[0375] In some embodiments, R6 is a C3-C7 monocyclic cycloalkyl. In some embodiments, R6 is a C3-C7 monocyclic saturated cycloalkyl. In some embodiments, R6 is a C3-C7 monocyclic partially saturated cycloalkyl. In some embodiments, R6 is a C9-C 10 In some embodiments, R6 is a C9-C 10 In some embodiments, R6 is a C9-C 10 In some embodiments, R6 is a C8-C 10 It is a polycyclic cycloalkyl.
[0376] In some embodiments, R6 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 7-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 8-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 9-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 11-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0377] In some embodiments, R6 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 11-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0378] In some embodiments, R6 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 11-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0379] In some embodiments, R6 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 11-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0380] In some embodiments, R6 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0381] In some embodiments, R6 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0382] In some embodiments, R6 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0383] In some embodiments, R6 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0384] In some embodiments, R6 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 13-membered polycyclic heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0385] In some embodiments, R6 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0386] In some embodiments, R6 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0387] In some embodiments, R6 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0388] In some embodiments, R6 is C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the aryl or heteroaryl is optionally substituted with one or more R7.
[0389] In some embodiments, R6 is C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0390] In some embodiments, R6 is a C optionally substituted with one or more R7 6~10 It is aryl.
[0391] In some embodiments, R6 is a C optionally substituted with one or more R7 6~8 In some embodiments, R6 is phenyl optionally substituted with one or more R7.
[0392] In some embodiments, R6 is a C substituted with one or more R7 6~8 In some embodiments, R6 is phenyl substituted with one or more R7.
[0393] In some embodiments, R6 is C substituted with 1 R7 6~8 In some embodiments, R6 is phenyl substituted with 1 R7.
[0394] In some embodiments, R6 is C 6~10 It is aryl.
[0395] In some embodiments, R6 is C 6~8 In some embodiments, R6 is phenyl.
[0396] In some embodiments, R6 is a 5- to 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 11-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0397] In some embodiments, R6 is a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 11-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0398] In some embodiments, R6 is a 5- to 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 11-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0399] In some embodiments, R6 is a 5- to 13-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 5-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 6-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 7-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 8-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 9-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 11-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0400] In some embodiments, R6 is a 9- to 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 9-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 10-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 11-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 12-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0401] In some embodiments, R6 is a 9-13 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 9 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 10 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 11 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 12 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0402] In some embodiments, R6 is a 9-13 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 9 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 10 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 11 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 12 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0403] In some embodiments, R6 is a 9- to 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 9-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 10-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 11-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 12-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0404] In some embodiments, R6 is a 9- to 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 9-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 10-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 11-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 12-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 13-membered polycyclic heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0405] In some embodiments, R6 is a 9-13 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 9 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 10 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 11 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 12 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0406] In some embodiments, R6 is a 9-13 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 9 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 10 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 11 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 12 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0407] In some embodiments, R6 is a 9- to 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 9-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 10-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 11-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 12-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0408] In some embodiments, R6 is H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10aryl, a 5- to 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0409] In some embodiments, R6 is H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0410] In some embodiments, R6 is H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is substituted with one or more R7.
[0411] In some embodiments, R6 is cyclopropyl, piperidine, tetrahydropyran, morpholine, phenyl, pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0412] In some embodiments, R6 is cyclopropyl, piperidine, tetrahydropyran, or morpholine.
[0413] In some embodiments, R6 is phenyl, pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0414] In some embodiments, R6 is pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0415] In some embodiments, R6 is pyridine, pyrimidine, or indazole.
[0416] In some embodiments, R6 is indazole.
[0417] In some embodiments, R6 is tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0418] In some embodiments, R6 is tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, or imidazole.
[0419] In some embodiments, R6 is 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0420] In some embodiments, R6 is 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, or benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole.
[0421] In some embodiments, R6 is 9H-carbazole.
[0422] In some embodiments, R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7.
[0423] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0424] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0425] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0426] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0427] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0428] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0429] In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0430] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 9-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0431] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0432] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0433] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0434] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0435] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0436] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0437] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0438] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0439] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0440] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0441] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0442] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atoms to which they are attached, form a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atoms to which they are attached, form a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0443] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0444] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0445] In some embodiments, R5 and R6 together with the atoms to which they are attached form a piperidine optionally substituted with one or more R7.
[0446] In some embodiments, R5 and R6 together with the atoms to which they are attached form a piperidine substituted with one or more R7.
[0447] In some embodiments, R5 and R6 together with the atom to which they are attached form a piperidine substituted with one R7.
[0448] In some embodiments, R5 and R6 together with the atom to which they are attached form a piperidine.
[0449] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydroquinoline optionally substituted with one or more R7.
[0450] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydroquinoline substituted with one or more R7.
[0451] In some embodiments, R5 and R6 together with the atom to which they are attached form a tetrahydroquinoline substituted with one R7.
[0452] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydroquinoline.
[0453] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydroisoquinoline optionally substituted with one or more R7.
[0454] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydroisoquinoline substituted with one or more R7.
[0455] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydroisoquinoline substituted with one R7.
[0456] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydroisoquinoline.
[0457] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydroimidazopyrazine optionally substituted with one or more R7.
[0458] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydroimidazopyrazine substituted with one or more R7.
[0459] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydroimidazopyrazine substituted with one R7.
[0460] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydroimidazopyrazine.
[0461] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydronaphthyridine optionally substituted with one or more R7.
[0462] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydronaphthyridine substituted with one or more R7.
[0463] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydronaphthyridine substituted with one R7.
[0464] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydronaphthyridine.
[0465] In some embodiments, each R7 is independently oxo, halogen, -OH, -NH2, -CN, -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2)t -R8, -NH-(CH2) t -R8, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R 10 may be substituted with.
[0466] In some embodiments, each R7 is independently oxo, halogen, -OH, -NH2, -CN, -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0467] In some embodiments, R7 is oxo, halogen, —OH, —NH2, —CN, —C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, -O-(CH2) t -R8, or -NH-(CH2) t -R8.
[0468] In some embodiments, R7 is oxo, halogen, -OH, -NH2, or -CN.
[0469] In some embodiments, R7 is oxo.
[0470] In some embodiments, R7 is halogen. In some embodiments, R7 is F, Cl, Br, or I. In some embodiments, R7 is F, Cl, or Br. In some embodiments, R7 is F. In some embodiments, R7 is Cl. In some embodiments, R7 is Br. In some embodiments, R7 is I.
[0471] In some embodiments, R7 is -OH. In some embodiments, R7 is -NH2. In some embodiments, R7 is -CN.
[0472] In some embodiments, R7 is -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, -O-(CH2) t -R8, or -NH-(CH2) t -R8.
[0473] In some embodiments, R7 is -C(O)R 10 In some embodiments, R7 is -C(O)OR 10 In some embodiments, R7 is —C(O)N(R 10 )2. In some embodiments, R7 is -O-(CH2) t In some embodiments, R7 is -NH-(CH2) t -R8.
[0474] In some embodiments, R7 is C 1~6 Alkoxy, -NH(C 1~6 alkyl), or -N(C 1~6 alkyl)2.
[0475] In some embodiments, R7 is one or more R 10 C optionally substituted with 1~6 It is an alkoxy.
[0476] In some embodiments, R7 is one or more R 10 C replaced with 1~6 It is an alkoxy.
[0477] In some embodiments, R7 is selected from the group consisting of 1 R 10 C replaced with 1~6 In some embodiments, R7 is alkoxy. 10 C replaced with 1~6 It is an alkoxy.
[0478] In some embodiments, R7 is C 1~6 In some embodiments, R7 is alkoxy. In some embodiments, R7 is methoxy. In some embodiments, R7 is ethoxy. In some embodiments, R7 is propoxy. In some embodiments, R7 is butoxy. In some embodiments, R7 is pentoxy. In some embodiments, R7 is hexoxy. In some embodiments, R7 is isopropoxy. In some embodiments, R7 is isobutoxy. In some embodiments, R7 is isopentoxy. In some embodiments, R7 is isohexoxy. In some embodiments, R7 is secbutoxy. In some embodiments, R7 is secpentoxy. In some embodiments, R7 is sechexoxy. In some embodiments, R7 is tertbutoxy.
[0479] In some embodiments, R7 is —NH(C 1~6 alkyl) or -N(C 1~6 In some embodiments, R7 is -NH(C 1~6 In some embodiments, R7 is -N(C alkyl). 1~6 alkyl)2.
[0480] In some embodiments, R7 is C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R 10 may be substituted with.
[0481] In some embodiments, R7 is C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0482] In some embodiments, R7 is C 1~3 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more R 10 may be substituted with.
[0483] In some embodiments, R7 is one or more R 10 C optionally substituted with 1~3 In some embodiments, R7 is one or more R 10 In some embodiments, R7 is methyl optionally substituted with one or more R 10 In some embodiments, R7 is ethyl optionally substituted with one or more R 10 In some embodiments, R7 is propyl optionally substituted with one or more R 10 isopropyl which may be substituted with
[0484] In some embodiments, R7 is one or more R 10 C optionally substituted with 2~6 In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a C2 alkenyl optionally substituted with one or more R 10 In some embodiments, R7 is a C3 alkenyl optionally substituted with one or more R 10 In some embodiments, R7 is a C4 alkenyl optionally substituted with one or more R 10 In some embodiments, R7 is a C5 alkenyl optionally substituted with one or more R 10 and C6 alkenyl optionally substituted with.
[0485] In some embodiments, R7 is one or more R 10 C optionally substituted with 2~6 In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a C2 alkynyl optionally substituted with one or more R 10 In some embodiments, R7 is a C3 alkynyl optionally substituted with one or more R 10 In some embodiments, R7 is a C4 alkynyl optionally substituted with one or more R 10 In some embodiments, R7 is a C5 alkynyl optionally substituted with one or more R 10 and C6 alkynyl optionally substituted with.
[0486] In some embodiments, R7 is C 1~3 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more R 10 is replaced by .
[0487] In some embodiments, R7 is one or more R10 C replaced with 1~3 In some embodiments, R7 is one or more R 10 In some embodiments, R7 is methyl substituted with one or more R 10 In some embodiments, R7 is ethyl substituted with one or more R 10 In some embodiments, R7 is propyl substituted with one or more R 10 isopropyl substituted with
[0488] In some embodiments, R7 is one or more R 10 C replaced with 2~6 In some embodiments, R7 is one or more R 10 In some embodiments, R is a C alkenyl substituted with one or more R 10 In some embodiments, R is a C alkenyl substituted with one or more R 10 In some embodiments, R7 is a C4 alkenyl substituted with one or more R 10 In some embodiments, R7 is a C5 alkenyl substituted with one or more R 10 and C6 alkenyl substituted with
[0489] In some embodiments, R7 is one or more R 10 C replaced with 2~6 In some embodiments, R7 is one or more R 10 In some embodiments, R is a C alkynyl substituted with one or more R 10 In some embodiments, R is a C alkynyl substituted with one or more R 10 In some embodiments, R7 is a C4 alkynyl substituted with one or more R 10 In some embodiments, R7 is a C5 alkynyl substituted with one or more R 10 is a C6 alkynyl substituted with
[0490] In some embodiments, R7 is C 1~3 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one R 10 is replaced by .
[0491] In some embodiments, R7 is selected from the group consisting of 1 R 10 C replaced with 1~3 In some embodiments, R7 is an alkyl group. 10 In some embodiments, R7 is methyl substituted with one R 10 In some embodiments, R7 is ethyl substituted with one R 10 In some embodiments, R7 is propyl substituted with one R 10 isopropyl substituted with
[0492] In some embodiments, R7 is selected from the group consisting of 1 R 10 C replaced with 2~6 In some embodiments, R7 is an alkenyl. 10 In some embodiments, R is a C alkenyl substituted with one R 10 In some embodiments, R is a C alkenyl substituted with one R 10 In some embodiments, R7 is a C4 alkenyl substituted with one R 10 In some embodiments, R7 is a C5 alkenyl substituted with one R 10 and C6 alkenyl substituted with
[0493] In some embodiments, R7 is selected from the group consisting of 1 R 10 C replaced with 2~6 In some embodiments, R7 is alkynyl. 10 In some embodiments, R7 is a C2 alkynyl substituted with one R 10 In some embodiments, R is a C alkynyl substituted with one R 10In some embodiments, R is a C alkynyl substituted with one R 10 In some embodiments, R7 is a C5 alkynyl substituted with one R 10 is a C6 alkynyl substituted with
[0494] In some embodiments, R7 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0495] In some embodiments, R7 is C 1~3 In some embodiments, R7 is alkyl. In some embodiments, R7 is methyl. In some embodiments, R7 is ethyl. In some embodiments, R7 is propyl. In some embodiments, R7 is isopropyl.
[0496] In some embodiments, R7 is C 2~6 In some embodiments, R7 is C2 alkenyl. In some embodiments, R7 is C3 alkenyl. In some embodiments, R7 is C4 alkenyl. In some embodiments, R7 is C5 alkenyl. In some embodiments, R7 is C6 alkenyl.
[0497] In some embodiments, R7 is C 2~6 In some embodiments, R7 is C2 alkynyl. In some embodiments, R7 is C3 alkynyl. In some embodiments, R7 is C4 alkynyl. In some embodiments, R7 is C5 alkynyl. In some embodiments, R7 is C6 alkynyl.
[0498] In some embodiments, R7 is C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 10 may be substituted with.
[0499] In some embodiments, R7 is C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0500] In some embodiments, R7 is C 3~10 cycloalkyl or 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl or heterocyclyl is selected from one or more R 10 may be substituted with.
[0501] In some embodiments, R7 is C 3~10 cycloalkyl, or a 3- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S.
[0502] In some embodiments, R7 is one or more R 10 C optionally substituted with 3~10 It is cycloalkyl.
[0503] In some embodiments, R7 is one or more R 10 In some embodiments, R is a C cycloalkyl optionally substituted with one or more R 10 In some embodiments, R7 is a C4 cycloalkyl optionally substituted with one or more R 10 In some embodiments, R7 is a C5 cycloalkyl optionally substituted with one or more R 10In some embodiments, R is a C cycloalkyl optionally substituted with one or more R 10 In some embodiments, R is a C cycloalkyl optionally substituted with one or more R 10 In some embodiments, R is a C cycloalkyl optionally substituted with one or more R 10 In some embodiments, R7 is a C9 cycloalkyl optionally substituted with one or more R 10 C optionally substituted with 10 It is cycloalkyl.
[0504] In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a C3-C7 monocyclic cycloalkyl optionally substituted with one or more R 10 In some embodiments, R7 is a C3-C7 monocyclic saturated cycloalkyl optionally substituted with one or more R 10 In some embodiments, R7 is a C3-C7 monocyclic partially saturated cycloalkyl optionally substituted with one or more R 10 C9 to C optionally substituted 10 In some embodiments, R7 is a bicyclic cycloalkyl. In some embodiments, R7 is one or more R 10 C9 to C optionally substituted 10 In some embodiments, R7 is a bicyclic saturated cycloalkyl. 10 C9 to C optionally substituted 10 In some embodiments, R7 is a bicyclic partially saturated cycloalkyl. 10 C8 to C optionally substituted 10 It is a polycyclic cycloalkyl.
[0505] In some embodiments, R7 is one or more R 10 C replaced with 3~10 It is cycloalkyl.
[0506] In some embodiments, R7 is one or more R 10 In some embodiments, R is a C cycloalkyl substituted with one or more R 10 In some embodiments, R is a C cycloalkyl substituted with one or more R 10 In some embodiments, R is a C cycloalkyl substituted with one or more R 10 In some embodiments, R is a C cycloalkyl substituted with one or more R 10 In some embodiments, R is a C cycloalkyl substituted with one or more R 10 In some embodiments, R is a C cycloalkyl substituted with one or more R 10 In some embodiments, R is a C cycloalkyl substituted with one or more R 10 C replaced with 10 It is cycloalkyl.
[0507] In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a C3-C7 monocyclic cycloalkyl substituted with one or more R 10 In some embodiments, R7 is a C3-C7 monocyclic saturated cycloalkyl substituted with one or more R 10 In some embodiments, R7 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one or more R 10 C9~C substituted with 10 In some embodiments, R7 is a bicyclic cycloalkyl. In some embodiments, R7 is one or more R 10 C9~C substituted with 10 In some embodiments, R7 is a bicyclic saturated cycloalkyl. 10 C9~C substituted with 10 In some embodiments, R7 is a bicyclic partially saturated cycloalkyl. 10 C8~C substituted with 10 It is a polycyclic cycloalkyl.
[0508] In some embodiments, R7 is selected from the group consisting of 1 R 10 C replaced with 3~10 It is cycloalkyl.
[0509] In some embodiments, R7 is selected from the group consisting of 1 R 10 In some embodiments, R is a C cycloalkyl substituted with one R 10 In some embodiments, R is a C cycloalkyl substituted with one R 10 In some embodiments, R is a C cycloalkyl substituted with one R 10 In some embodiments, R is a C cycloalkyl substituted with one R 10 In some embodiments, R is a C cycloalkyl substituted with one R 10 In some embodiments, R is a C cycloalkyl substituted with one R 10 In some embodiments, R is a C cycloalkyl substituted with one R 10 C replaced with 10 It is cycloalkyl.
[0510] In some embodiments, R7 is selected from the group consisting of 1 R 10 In some embodiments, R7 is a C3-C7 monocyclic cycloalkyl substituted with one R 10 In some embodiments, R7 is a C3-C7 monocyclic saturated cycloalkyl substituted with one R 10 In some embodiments, R7 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one R 10 C9~C substituted with 10 In some embodiments, R7 is a bicyclic cycloalkyl. 10 C9~C substituted with 10 In some embodiments, R7 is a bicyclic saturated cycloalkyl. 10 C9~C substituted with 10 In some embodiments, R7 is a bicyclic partially saturated cycloalkyl. 10 C8~C substituted with10 It is a polycyclic cycloalkyl.
[0511] In some embodiments, R7 is C 3~10 It is cycloalkyl.
[0512] In some embodiments, R7 is C3 cycloalkyl. In some embodiments, R7 is C4 cycloalkyl. In some embodiments, R7 is C5 cycloalkyl. In some embodiments, R7 is C6 cycloalkyl. In some embodiments, R7 is C7 cycloalkyl. In some embodiments, R7 is C8 cycloalkyl. In some embodiments, R7 is C9 cycloalkyl. In some embodiments, R7 is C 10 It is cycloalkyl.
[0513] In some embodiments, R7 is a C3-C7 monocyclic cycloalkyl. In some embodiments, R7 is a C3-C7 monocyclic saturated cycloalkyl. In some embodiments, R7 is a C3-C7 monocyclic partially saturated cycloalkyl. In some embodiments, R7 is a C9-C 10 In some embodiments, R7 is a C9-C 10 In some embodiments, R7 is a C9-C 10 In some embodiments, R7 is a C8-C 10 It is a polycyclic cycloalkyl.
[0514] In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 3-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10In some embodiments, R7 is a 4-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 5-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 6-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 7-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is an 8-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 9-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 and 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with
[0515] In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10In some embodiments, R7 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 and a 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, substituted with
[0516] In some embodiments, R7 is selected from the group consisting of 1 R 10 In some embodiments, R7 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R10 In some embodiments, R7 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 and a 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, substituted with
[0517] In some embodiments, R7 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0518] In some embodiments, R7 is C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the aryl or heteroaryl is selected from one or more R 10 may be substituted with.
[0519] In some embodiments, R7 is C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0520] In some embodiments, R7 is one or more R 10 C optionally substituted with 6~10 It is aryl.
[0521] In some embodiments, R7 is one or more R 10 C optionally substituted with 6~8 In some embodiments, R7 is one or more R 10 and phenyl optionally substituted with .
[0522] In some embodiments, R7 is one or more R 10 C replaced with 6~8 In some embodiments, R7 is one or more R 10 is a phenyl substituted with
[0523] In some embodiments, R7 is selected from the group consisting of 1 R 10 C replaced with 6~8 In some embodiments, R7 is aryl. 10 is a phenyl substituted with
[0524] In some embodiments, R7 is C 6~10 It is aryl.
[0525] In some embodiments, R7 is C 6~8 In some embodiments, R7 is phenyl.
[0526] In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 5-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10In some embodiments, R7 is a 6-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 7-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is an 8-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 9-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 and 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with
[0527] In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10and 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, substituted with
[0528] In some embodiments, R7 is selected from the group consisting of 1 R 10 In some embodiments, R7 is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 and 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, substituted with
[0529] In some embodiments, R7 is a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0530] In some embodiments, R7 is cyclopropyl, piperidine, tetrahydropyran, morpholine, phenyl, pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0531] In some embodiments, R7 is cyclopropyl, piperidine, tetrahydropyran, or morpholine.
[0532] In some embodiments, R7 is phenyl, pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0533] In some embodiments, R7 is pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0534] In some embodiments, R7 is pyridine or pyrimidine.
[0535] In some embodiments, R7 is tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0536] In some embodiments, R7 is tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, or imidazole.
[0537] In some embodiments, R7 is 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0538] In some embodiments, R7 is 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, or benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole.
[0539] In some embodiments, R7 is 9H-carbazole.
[0540] In some embodiments, R7 is oxo, halogen, —OH, —NH2, —CN, —C(O)R 10 , C 1~6 Alkyl, C 2~6 Alkynyl, -O-(CH2) t -R8, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkynyl, aryl, or heteroaryl is selected from one or more R 10 may be substituted with.
[0541] In some embodiments, R7 is oxo, halogen, —OH, —NH2, —CN, —C(O)R 10 , C 1~6 Alkyl, C 2~6 Alkynyl, -O-(CH2) t -R8, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkynyl, aryl, or heteroaryl is selected from one or more R 10 is replaced by .
[0542] In some embodiments, R8 is —OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9.
[0543] In some embodiments, R8 is —OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0544] In some embodiments, R8 is —OH, C1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, or -S(C 1~6 alkyl), wherein the alkoxy or alkyl is optionally substituted with one or more R9.
[0545] In some embodiments, R8 is —OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, or -S(C 1~6 alkyl), wherein the alkoxy or alkyl is substituted with one or more R9.
[0546] In some embodiments, R8 is —OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, or -S(C 1~6 alkyl), wherein the alkoxy or alkyl is substituted with one R9.
[0547] In some embodiments, R8 is a C optionally substituted with one or more R9 1~6 It is an alkoxy.
[0548] In some embodiments, R8 is C 1~6 Alkoxy-OH, wherein the alkoxy is optionally substituted with one or more R9.
[0549] In some embodiments, R8 is C substituted with one or more R9 1~6 It is an alkoxy.
[0550] In some embodiments, R8 is C 1~6Alkoxy-OH, wherein the alkoxy is substituted with one or more R9.
[0551] In some embodiments, R8 is C substituted with 1 R9 1~6 It is an alkoxy.
[0552] In some embodiments, R8 is C 1~6 Alkoxy-OH, wherein the alkoxy is substituted with one R9.
[0553] In some embodiments, R8 is —NH(C 1~6 alkyl), wherein the alkyl is optionally substituted with one or more R9.
[0554] In some embodiments, R8 is —N(C 1~6 alkyl)2, wherein the alkyl is optionally substituted with one or more R9.
[0555] In some embodiments, R8 is —NH(C 1~6 alkyl), wherein the alkyl is substituted with one or more R9.
[0556] In some embodiments, R8 is —N(C 1~6 alkyl)2, wherein the alkyl is substituted with one or more R9.
[0557] In some embodiments, R8 is —NH(C 1~6 alkyl), wherein the alkyl is substituted with one R9.
[0558] In some embodiments, R8 is —N(C 1~6 alkyl)2, wherein the alkyl is substituted with one R9.
[0559] In some embodiments, R8 is -S(C 1~6 alkyl)2, wherein the alkyl is optionally substituted with one or more R9.
[0560] In some embodiments, R8 is -S(C 1~6 alkyl)2, wherein the alkyl is substituted with one or more R9.
[0561] In some embodiments, R8 is -S(C 1~6 alkyl)2, wherein the alkyl is substituted with one R9.
[0562] In some embodiments, R8 is —OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl).
[0563] In some embodiments, R8 is —OH, C 1~6 Alkoxy, or C 1~6 It is alkoxy-OH.
[0564] In some embodiments, R8 is -OH.
[0565] In some embodiments, R8 is C 1~6 In some embodiments, R is alkoxy. In some embodiments, R is methoxy. In some embodiments, R is ethoxy. In some embodiments, R is propoxy. In some embodiments, R is butoxy. In some embodiments, R is pentoxy. In some embodiments, R is hexoxy. In some embodiments, R is isopropoxy. In some embodiments, R is isobutoxy. In some embodiments, R is isopentoxy. In some embodiments, R is isohexoxy. In some embodiments, R is secbutoxy. In some embodiments, R is secpentoxy. In some embodiments, R is sechexoxy. In some embodiments, R is tertbutoxy.
[0566] In some embodiments, R8 is C1~6 In some embodiments, R is alkoxy-OH. In some embodiments, R is methoxy-OH. In some embodiments, R is ethoxy-OH. In some embodiments, R is propoxy-OH. In some embodiments, R is butoxy-OH. In some embodiments, R is pentoxy-OH. In some embodiments, R is hexoxy-OH. In some embodiments, R is isopropoxy-OH. In some embodiments, R is isobutoxy-OH. In some embodiments, R is isopentoxy-OH. In some embodiments, R is isohexoxy-OH. In some embodiments, R is sec-butoxy-OH. In some embodiments, R is sec-pentoxy-OH. In some embodiments, R is sec-hexoxy-OH. In some embodiments, R is tert-butoxy-OH.
[0567] In some embodiments, R is —NH, —NH(C 1~6 alkyl), or -N(C 1~6 alkyl)2.
[0568] In some embodiments, R8 is -NH2.
[0569] In some embodiments, R8 is —NH(C 1~6In some embodiments, R is -NH(methyl). In some embodiments, R is -NH(ethyl). In some embodiments, R is -NH(propyl). In some embodiments, R is -NH(butyl). In some embodiments, R is -NH(pentyl). In some embodiments, R is -NH(hexyl). In some embodiments, R is -NH(isopropyl). In some embodiments, R is -NH(isobutyl). In some embodiments, R is -NH(isopentyl). In some embodiments, R is -NH(isohexyl). In some embodiments, R is -NH(secbutyl). In some embodiments, R is -NH(secpentyl). In some embodiments, R is -NH(sechexyl). In some embodiments, R is -NH(tertbutyl).
[0570] In some embodiments, R8 is —N(C 1~6 In some embodiments, R is -N(methyl) . In some embodiments, R is -N(ethyl) . In some embodiments, R is -N(propyl) . In some embodiments, R is -N(butyl) . In some embodiments, R is -N(pentyl) . In some embodiments, R is -N(hexyl) . In some embodiments, R is -N(isopropyl) . In some embodiments, R is -N(isobutyl) . In some embodiments, R is -N(isopentyl) . In some embodiments, R is -N(isohexyl) . In some embodiments, R is -N(secbutyl) . In some embodiments, R is -N(secpentyl) . In some embodiments, R is -N(sechexyl) . In some embodiments, R is -N(tertbutyl) .
[0571] In some embodiments, R8 is -SH or -S(C 1~6 alkyl).
[0572] In some embodiments, R8 is -SH.
[0573] In some embodiments, R8 is -S(C 1~6 alkyl)2.
[0574] In some embodiments, R8 is -S(methyl). In some embodiments, R8 is -S(ethyl). In some embodiments, R8 is -S(propyl). In some embodiments, R8 is -S(butyl). In some embodiments, R8 is -S(pentyl). In some embodiments, R8 is -S(hexyl). In some embodiments, R8 is -S(isopropyl). In some embodiments, R8 is -S(isobutyl). In some embodiments, R8 is -S(isopentyl). In some embodiments, R8 is -S(isohexyl). In some embodiments, R8 is -S(secbutyl). In some embodiments, R8 is -S(secpentyl). In some embodiments, R8 is -S(sechexyl). In some embodiments, R8 is -S(tertbutyl).
[0575] In some embodiments, R8 is C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9.
[0576] In some embodiments, R8 is C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0577] In some embodiments, R8 is C 3~10cycloalkyl or 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl or heterocyclyl is optionally substituted with one or more R9.
[0578] In some embodiments, R8 is C 3~10 cycloalkyl, or a 3- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S.
[0579] In some embodiments, R8 is a C optionally substituted with one or more R9 3~10 It is cycloalkyl.
[0580] In some embodiments, R8 is a C3 cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C4 cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C5 cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C6 cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C7 cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C8 cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C9 cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C6 cycloalkyl optionally substituted with one or more R9. 10 It is cycloalkyl.
[0581] In some embodiments, R8 is a C3-C7 monocyclic cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C3-C7 monocyclic saturated cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C3-C7 monocyclic partially saturated cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C9-C7 monocyclic partially saturated cycloalkyl optionally substituted with one or more R9.10 In some embodiments, R is a C-C alkyl group optionally substituted with one or more R. 10 In some embodiments, R8 is a C9-C10 alkyl group optionally substituted with one or more R9. 10 In some embodiments, R is a C-C bicyclic partially saturated cycloalkyl optionally substituted with one or more R. 10 It is a polycyclic cycloalkyl.
[0582] In some embodiments, R8 is C substituted with one or more R9 3~10 It is cycloalkyl.
[0583] In some embodiments, R8 is a C3 cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C4 cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C5 cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C6 cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C7 cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C8 cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C9 cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C6 cycloalkyl substituted with one or more R9. 10 It is cycloalkyl.
[0584] In some embodiments, R8 is a C3-C7 monocyclic cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C3-C7 monocyclic saturated cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C9-C7 monocyclic partially saturated cycloalkyl substituted with one or more R9. 10In some embodiments, R is a C-C alkyl group substituted with one or more R. 10 In some embodiments, R is a C-C alkyl group substituted with one or more R. 10 In some embodiments, R is a C-C bicyclic partially saturated cycloalkyl substituted with one or more R. 10 It is a polycyclic cycloalkyl.
[0585] In some embodiments, R8 is C substituted with 1 R9 3~10 It is cycloalkyl.
[0586] In some embodiments, R8 is a C3 cycloalkyl substituted with one R9. In some embodiments, R8 is a C4 cycloalkyl substituted with one R9. In some embodiments, R8 is a C5 cycloalkyl substituted with one R9. In some embodiments, R8 is a C6 cycloalkyl substituted with one R9. In some embodiments, R8 is a C7 cycloalkyl substituted with one R9. In some embodiments, R8 is a C8 cycloalkyl substituted with one R9. In some embodiments, R8 is a C9 cycloalkyl substituted with one R9. In some embodiments, R8 is a C6 cycloalkyl substituted with one R9. In some embodiments, R8 is a C7 cycloalkyl substituted with one R9. In some embodiments, R8 is a C8 cycloalkyl substituted with one R9. In some embodiments, R8 is a C9 cycloalkyl substituted with one R9. In some embodiments, R8 is a C8 cycloalkyl substituted with one R9. 10 It is cycloalkyl.
[0587] In some embodiments, R8 is a C3-C7 monocyclic cycloalkyl substituted with one R9. In some embodiments, R8 is a C3-C7 monocyclic saturated cycloalkyl substituted with one R9. In some embodiments, R8 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one R9. In some embodiments, R8 is a C9-C7 monocyclic partially saturated cycloalkyl substituted with one R9. 10 In some embodiments, R is a C-C substituted with one R. 10 In some embodiments, R8 is a C9-C substituted with one R9. 10In some embodiments, R is a C-C bicyclic partially saturated cycloalkyl substituted with one R. 10 It is a polycyclic cycloalkyl.
[0588] In some embodiments, R8 is C 3~10 It is cycloalkyl.
[0589] In some embodiments, R8 is C3 cycloalkyl. In some embodiments, R8 is C4 cycloalkyl. In some embodiments, R8 is C5 cycloalkyl. In some embodiments, R8 is C6 cycloalkyl. In some embodiments, R8 is C7 cycloalkyl. In some embodiments, R8 is C8 cycloalkyl. In some embodiments, R8 is C9 cycloalkyl. In some embodiments, R8 is C 10 It is cycloalkyl.
[0590] In some embodiments, R8 is a C3-C7 monocyclic cycloalkyl. In some embodiments, R8 is a C3-C7 monocyclic saturated cycloalkyl. In some embodiments, R8 is a C3-C7 monocyclic partially saturated cycloalkyl. In some embodiments, R8 is a C9-C 10 In some embodiments, R is a C-C 10 In some embodiments, R is a C-C bicyclic saturated cycloalkyl. 10 In some embodiments, R is a C-C bicyclic partially saturated cycloalkyl. 10 It is a polycyclic cycloalkyl.
[0591] In some embodiments, R8 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9.
[0592] In some embodiments, R8 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9.
[0593] In some embodiments, R8 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with 1 R9. In some embodiments, R8 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with 1 R9. In some embodiments, R8 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with 1 R9.
[0594] In some embodiments, R8 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0595] In some embodiments, R8 is C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the aryl or heteroaryl is optionally substituted with one or more R9.
[0596] In some embodiments, R8 is C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0597] In some embodiments, R8 is a C optionally substituted with one or more R9 6~10 It is aryl.
[0598] In some embodiments, R8 is a C optionally substituted with one or more R9 6~8In some embodiments, R8 is phenyl optionally substituted with one or more R9.
[0599] In some embodiments, R8 is C substituted with one or more R9 6~8 In some embodiments, R8 is phenyl substituted with one or more R9.
[0600] In some embodiments, R8 is C substituted with 1 R9 6~8 In some embodiments, R8 is phenyl substituted with 1 R9.
[0601] In some embodiments, R8 is C 6~10 It is aryl.
[0602] In some embodiments, R8 is C 6~8 In some embodiments, R8 is phenyl.
[0603] In some embodiments, R8 is a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiment...
Claims
1. The following:
1. A compound selected from the group consisting of: or a pharmaceutically acceptable solvate, enantiomer, stereoisomer, tautomer, or salt thereof.
2. 10. A pharmaceutical composition comprising the compound of claim 1, or a pharmaceutically acceptable solvate, enantiomer, stereoisomer, tautomer, or salt thereof, and a pharmaceutically acceptable diluent or carrier.
3. 3. The pharmaceutical composition of claim 2 for use in treating cancer sensitive to modulation of P-glycoprotein activity and / or cytochrome P450 activity.
4. 3. The pharmaceutical composition of claim 2 for use in the treatment or prevention of a disease or disorder sensitive to inhibition of P-glycoprotein activity or cytochrome P450 activity.
5. 10. Use of the compound of claim 1, or a pharmaceutically acceptable solvate, enantiomer, stereoisomer, tautomer, or salt thereof, in the manufacture of a medicament for treating cancer sensitive to modulation of P-glycoprotein activity and / or cytochrome P450 activity.
6. 10. Use of the compound of claim 1, or a pharmaceutically acceptable solvate, enantiomer, stereoisomer, tautomer, or salt thereof, in the manufacture of a medicament for treating or preventing a disease or disorder sensitive to inhibition of P-glycoprotein activity or cytochrome P450 activity.
Citation Information
Patent Citations
Method for producing tetrazolmethanesulfonate and novel compounds used therein
JP2013517267A
JPP2007-597493A