Biarylamide derivatives and their use as pkmyt1 inhibitors

Abstract

The present invention is generally in the field of therapeutic compounds. More specifically, the present invention relates to specific biaryl amide compounds of the structural formula (also referred to herein as' BAA compounds') capable of inhibiting protein kinases, membrane associated tyrosine / threonine 1 (PKMYT1). The invention also relates to: pharmaceutical compositions comprising such compounds, and to the inhibition of PKMYT1 kinase in vitro and in vivo using such compounds and compositions; treating conditions (e.g., diseases) that can be ameliorated by inhibition of PKMYT1 kinase; and treating proliferative conditions, cancers and the like. Formula (I)

Description

(19) State Intellectual Property Office (12) Invention Patent Application (10) Application Publication Number (43) Application Publication Date (21) Application Number 202480030955.3 (22) Application Date 2024.03.08 (30) Priority Data 23386018.8 2023.03.09 EP (85) PCT International Application Entering National Phase Date 2025.11.06 (86) PCT International Application Application Data PCT / EP2024 / 056305 2024.03.08 (87) PCT International Application Publication Data WO2024 / 184550 EN 2024.09.12 (71) Applicant Cancer Research Technology Co., Ltd. Address London, UK Applicant M-T Bio Ltd. (72) Inventors Ali Rauf Evsimios Spirizon-Gavrieldan Nigulescu-Duwaz Michael Branddeborah Smithson Christopher Fitzpatrick Aleksandar Griez Amhammed Aljala Monica Lisas Kate Ryan Birkin Christopher Stephen Kscholio Leon Ian Hagen Richard Mare Caroline Springer (74) Patent Agency Beijing Tianhao United Intellectual Property Agency Co., Ltd. 11112 Patent Attorney Zhang Keke Zhu Wen (51) Int.Cl. C07D 413 / 12 (2006.01) C07D 417 / 12 (2006.01) C07D 417 / 14 (2006.01) C07D 487 / 04(2006.01) C07D 513 / 04(2006.01) A61P 35 / 00(2006.01) A61K 31 / 381(2006.01) (54) Invention Title: Biarylamide Derivatives and Their Use as PKMYT1 Inhibitors (57) Abstract: This invention generally belongs to the field of therapeutic compounds. More specifically, this invention relates to specific biarylamide compounds (also referred to herein as “BAA compounds”) with the following structural formulas that are capable of inhibiting protein kinase, membrane-associated tyrosine / threonine 1 (PKMYT1). This invention also relates to: pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions to inhibit PKMYT1 kinase in vitro and in vivo; treatment of conditions (e.g., diseases) that can be improved by inhibiting PKMYT1 kinase; treatment of proliferative conditions, cancer, etc. Formula (I) Claims 15 pages Description 530 pages CN 121568936 A 2026.02.24 CN 1 21 56 89 36 A 1. A compound represented by the following formula: or a pharmaceutically acceptable salt or solvate thereof; wherein: Ring A is: wherein:-RA1 is -RA11; -RA11 is -RA111, -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A111, -OCF3, -NH2, -NHR A111, -NRA1112, -CN, -C(=O)RA111, -C(=O)OH, -C(=O)ORA111, -C(=O)NH2, -C(=O)NHRA111, -C(=O)NRA1112 or -S(=O)2R A111; each -RA111 is independently a straight-chain or branched saturated C1-4 alkyl group; -RA2 is -RA22; -RA22 is -RA222, -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A222, -OCF3, -NH2, -NHR A222, -NRA2222, -CN, -C(=O)RA222, -C(=O)OH, -C(=O)ORA222, -C(=O)NH2, -C(=O)NHRA222, -C(=O)NRA2222 or -S(=O)2R A222; each -RA222 is independently a straight-chain or branched saturated C1-4 alkyl group; -RA3 is -H or -RA33; -RA33 is -RA333, -F, -Cl, -Br, -I, -CF3, -OH, -OR A333 or -OCF3; each -RA333 is independently a straight-chain or branched saturated C1-4 alkyl group; -RA4 is -H or -RA44; -RA44 is -RA444, -F, -Cl, -Br, -I, -CF3, -OH, -ORA444, or -OCF3; each -RA444 is independently a straight-chain or branched saturated C1-4 alkyl group; and: ring B is selected from: wherein: Y1 is S, O, NH, or NRY1; Y2 is CH, CRY2, or N; Y3 is N, CH, or CRY3; claims 1 / 15 page 2 CN 121568936 A Y4 is N, CH, or CRY4; Y5 is S, O, NH, or NRY5; Y6 is N, CH, or CRY6; Y7 is N, CH, or CRY7; Y8 is N, CH, or CRY8; Y9 is S, O, NH, or NRY9; wherein: Each of -RY2, -RY3, -RY4, -RY6, -RY7, and -RY8 is independently -H, -F, -Cl, -Br, -I, -RYY, -CF3, -OH, -ORYY, -OCF3, -NH2, -NHRYY, or -NRYY2; each of -RYY is independently a straight-chain or branched saturated C1-4 alkyl group; and wherein: each of -RY1, -RY5, and -RY9 is independently -RYYN, -C(=O)RYYN, -C(=O)ORYYN, -C(=O)NH2, -C(=O)NHRYYN, -C(=O)NRYYN2, or -S(=O)2RYYN; each -RYYN is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; and wherein: -Q can be -Q1, -LQ1-Q1, -Q2, -LQ2-Q2, -Q3, -LQ3-Q3, -Q4, -LQ4-Q4, -Q5, or -H; wherein: Q1 is a C5-10 heteroaryl group; and: the carbon atom is optionally substituted with one or more -RQ1C groups; and the secondary nitrogen atom, if present, is optionally substituted with one or more -RQ1N groups; -LQ1- is a straight-chain or branched saturated C1-4 alkylene group; Q2 is a C3-10 heterocyclic group; and: the sulfur atom, if present, is optionally substituted with one or two =O groups; the carbon atom is optionally substituted with one or more -RQ2C groups; and the secondary nitrogen atom, if present, is optionally substituted with one or more -RQ2N groups; -LQ2- is a straight-chain or branched saturated C1-4 alkylene group; Q3 is phenyl or naphthyl; And optionally substituted with one or more -RQ3C groups; -LQ3- is a straight-chain or branched saturated C1-4 alkylene group; Q4 is a C3-10 carbocyclic group; and optionally substituted with one or more -RQ4C groups; -LQ4- is a straight-chain or branched saturated C1-4 alkylene group; Q5 is a straight-chain or branched saturated C1-6 alkyl group; and optionally substituted with one or more -RQ5C groups; Claims 2 / 15 page 3 CN 121568936 A and wherein: each -RQ1C is independently: -F, -Cl, -Br, -I, -RQ1CC, -RQ1CX, -ORQ1CX, -OH, -ORQ1CC, -LQ1C-OH, -LQ1C-ORQ1CC, -NH2, -NHR Q1CC, -NRQ1CC2, -R Q1CM, ‑LQ1C‑NH2, ‑L Q1C ‑NHRQ1CC, ‑LQ1C‑NRQ1CC2, ‑L Q1C ‑RQ1CM, ‑NHC(=O)RQ1CC, ‑N(RQ1CC)C(=O)RQ1CC, ‑NHC(=O)ORQ1CC, ‑LQ1C‑NHC(=O)RQ1CC、‑LQ1C‑NHC(=O)ORQ1CC、‑C(=O)NH2、‑C(=O)NHRQ1CC、‑C(=O)NRQ1CC2、‑C(=O)RQ1CM、=O、‑NHC(=O)NH2、‑NHC(=O)NHRQ1CC、‑NHC(=O)NRQ1CC2、‑NHC(=O)RQ1CM、‑LQ1C‑C(=O)NH2、‑L Q1C ‑C(=O)NHRQ1CC、‑LQ1C‑C(=O)NRQ1CC2、‑L Q1C ‑C(=O)RQ1CM、‑C(=O)OH、‑C(=O)ORQ1CC、‑OC(=O)RQ1CC、 ‑OC(=O)NH2、‑OC(=O)NHRQ1CC、‑OC(=O)NRQ1CC2、‑OC(=O)RQ1CM、 -S(=O)2R Q1CC, -S(=O)2R Q1CX, -S(=O)2NH2, -S(=O)2 NHRQ`CC, -S(=O)2 NRQ1CC2, -S(=O)2 RQ1CM, -NHS(=O)RQ1CC, -NHS(=O)2 RQ1CC, -CN, -C≡CH or -NO2; and two adjacent -RQ1C, if present, can jointly form -(CH2)n1-O-(CH2)m1- or -O-(CH2)p1-O-, where: n1 is 0, 1, 2 or 3; m1 is 0, 1, 2 or 3; and p1 is 1 or 2; provided that m1+n1 is 2 or 3; where: Each -RQ1CC is independently a straight-chain or branched saturated C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, C3-7 heterocyclic, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-6 alkyl is optionally substituted with -OH, -CN, or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -C1-4 alkyl, -CHF2, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; each -RQ1CX is independently a straight-chain or branched saturated C1-4 haloalkyl; each -LQ1C- is independently a straight-chain or branched saturated C1-4 alkylene. Each -RQ1CM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and linked through that N-ring atom; and: the carbon atom is optionally substituted by one or more -RQ1CMM groups; the sulfur atom, if present, is optionally substituted by one or two =O groups; and the secondary nitrogen atom, if present, is optionally substituted by groups selected from: -RQ1CMM, -C(=O)RQ1CMM, -C(=O)ORQ1CMM, -C(=O)NH2, -C(=O)NHRQ1CMM, -C(=O)NRQ1CMM2 and -S(=O)2RQ1CMM; and each -RQ1CMM is independently -F, -NH2, straight-chain or branched saturated C1-4 alkyl, C1-4 alkylOC(=O)NH-, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl is optionally replaced by one or more of the following claims 3 / 15 page 4 CN 121568936 A Group substitutions: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; and wherein: each -RQ1N independently is: -RQ1NC, -LQ1N-RQ1NC, -RQINX, -RQ1Nhet, -LQ1N-RQ1Nhet, -LQ1N-OH, -LQ1N-ORQ1NC, -LQ1N-C(=O))RQ1NC, -S(=O)2RQ1NC, -LQ1N-C(=O)OH, -LQ1N-C(=O)ORQ1NC, -LQ1N-C(=O)NH2, -LQ1N-C(=O)NHRQ1NK, -LQ1N-C(=O)NRQ1NC2, -LQ1N -C(=O)RQ1NP, -LQ1N-NH2, -LQ1N-NHRQ1NC, -LQ1N-NRQ1NC2, -LQ1N-RQ1NM, or -LQ1N-NHC(=O)ORQ1NC; wherein: each -RQ1NC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein each C1-4 alkyl is optionally converted by -F, -OH, -C≡N, - SO2-CH3 or -OCH3 is substituted, wherein each cycloalkyl, phenyl, and heteroaryl group is optionally substituted by one or more groups selected from the following: -F, -Cl, -Br, straight-chain or branched saturated C1-4 alkyl, -CHF2, -CF3, -OH, -OCH3, -CH2-O-CH3, -OCH2CH3, -C(=O)-NH-phenyl, -NH2, -NH(CH3), and -N(CH3)2; wherein the C1-4 alkyl and phenyl groups are independently and optionally substituted by -CH3 or -OH; each -RQ1NX is independently a straight-chain or branched saturated C1-4 haloalkyl group;Each -LQ1N- is independently a straight-chain or branched saturated C1-4 alkylene group; wherein the C1-4 alkylene group is optionally substituted with -OH or -OMe; each -RQ1NM is independently a non-aromatic C3-7 heterocyclic group having at least one N-ring atom and being linked through that N-ring atom; and: the carbon atom is optionally substituted with one or more -RQ1NMM groups; the sulfur atom, if present, is optionally substituted with one or two =O groups; and the secondary nitrogen atom, if present, is optionally substituted with a group selected from: -RQ1NMM, -C(=O)RQ1NMM, -C(=O)ORQ1NMM, -C(=O)NH2, -C(=O)NHRQ1NMM, -C(=O)NRQ1NMM2 and -S(=O)2RQ1NMM ; and each -RQ1NMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; and wherein: each -RQ1Nhet is independently a non-aromatic C3-7 heterocyclic group, and: the sulfur atom, if present, is optionally substituted with one or two =O groups; The carbon atom is optionally substituted with one or more -RQ1NHH groups or =O groups; and the secondary nitrogen atom, if present, is optionally substituted with a group selected from the following: -RQ1NHH, -C(=O)RQ1NJJ, -C(=O)ORQ1NHH, -C(=O)NH2, -C(=O)NHRQ1NHH, -C(=O)NRQ1NHH2 and -S(=O)2RQ1NHH; Claims 4 / 15 pages 5 CN 121568936 A Wherein: Each -RQ1NHH is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, C3-7 heterocyclic, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or - OCH3 is substituted, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted by one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; and wherein: -RQ1NJJ is -RJ1, -RJ2, -LJ-RJ2, -RJ3, -LJ-RJ3, -RJ4, -LJ-RJ4, -RJ5 or -LJ-RJ5;-RJ1 is a straight-chain or branched saturated C1-6 alkyl group; and optionally substituted with one or more groups selected from the following: -F, -OH, -ORJJ, -O-phenyl, -C(=O)OH, -C(=O)ORJJ, -NH2, -NHRJJ, and -NRJJ2; each -RJ2 is independently a C3-6 cycloalkyl group; and optionally substituted with one or more groups selected from the following: -F, -RJJ, -CF3, -OH, -ORJJ, -NH2, -NHRJJ, and -NRJJ2; each -RJ3 is independently a non-aromatic C3-7 heterocyclic group; and: the sulfur atom, if present, is optionally substituted with one or two =O groups; the carbon atom is optionally substituted with one or more groups selected from -F, -RJJ, -CF3, -OH, -ORJJ, -NH2, and -NHRJJ. The -RJ4 group is substituted with a group selected from -NRJJ2; and the secondary nitrogen atom, if present, is optionally substituted with a group selected from -RJJ, -C(=O)RJJ, -C(=O)ORJJ and -S(=O)2RJJ; each -RJ4 is phenyl; and is optionally substituted with one or more groups selected from -F, -Cl, -RJJ, -CF3, -OH, -ORJJ, -NH2, -NHRJJ and -NRJJ2; each -RJ5 is independently a C5-6 heteroaryl group; and: the carbon atom is optionally substituted with one or more groups selected from -F, -RJJ, -CF3, -OH, -ORJJ, -NH2, -NHRJJ and -NRJJ2; and the secondary nitrogen atom, if present, is optionally substituted with a group selected from -RJJ, -C(=O)RJJ, -C(=O) ORJJ and -S(=O)2RJJ; each -LJ- is independently a straight-chain or branched saturated C1-4 alkylene group, and optionally substituted with one or more -F groups; each -RJJ is a straight-chain or branched saturated C1-4 alkyl group; and wherein: -RQ1NK is -RK1, -RK2, -LK-RK2, -RK3, -LK-RK3, -RK4, -LK-RK4, -RK5 or -LK-RK5; -RK1 is a straight-chain or branched saturated C1-7 alkyl group; and optionally substituted with one or more groups selected from the following: -F, -OH, -ORKK, -OCH2CH2OCH3, -O-phenyl, -C(=O)OH, -C(=O)ORKK, -NH2, -NHRKK and -NRKK2; Each -RK2 group is independently a C3-6 cycloalkyl group; and optionally substituted with one or more groups selected from the following: -F, -RKK, -CF3, -OH, -ORKK, -NH2, -NHRKK, and -NRKK2; each -RK3 group is independently a non-aromatic C3-7 heterocyclic group; and:The carbon atom is optionally substituted with one or more groups selected from -F, -RKK, -CF3, -OH, -ORKK, -NH2, -NHRKK, and -NRKK2; and the secondary nitrogen atom, if present, is optionally substituted with groups selected from -RKK, -C(=O)RKK, -C(=O)ORKK, and -S(=O)2RKK; each -RK4 is phenyl; and is optionally substituted with one or more groups selected from -F, -Cl, -RKK, -CF3, -OH, -ORKK, -NH2, -NHRKK, and -NRKK2; each -RK5 is independently a C5-6 heteroaryl; and: the carbon atom is optionally substituted with one or more groups selected from -F, -RKK, -CF3, -OH, -ORKK, -NH2, -NHRKK, and -NRKK2. The groups KK and -NRKK2 are substituted; and the secondary nitrogen atom, if present, is optionally substituted with a group selected from: -RKK, -C(=O)RKK, -C(=O)ORKK and -S(=O)2RKK; each -LK- is a straight-chain or branched saturated C1-4 alkylene group, and is optionally substituted with one or more -F groups; each -RKK is a straight-chain or branched saturated C1-4 alkyl group; and wherein: -RQ1NP is a non-aromatic C3-11 heterocyclic group having at least one N ring atom and being linked by the N ring atom; and: the sulfur atom, if present, is optionally substituted with one or two =O groups; The carbon atom is optionally substituted with one or more groups selected from -RQ1NPP, -F, -OH, -ORQ1NPP, and =O; and the secondary nitrogen atom, if present, is optionally substituted with groups selected from: -RQ1NPP, -RQ1NPPX, -C(=O)RQ1NPP, -C(=O)ORQ1NPP, -C(=O)NH2, -C(=O)NHRQ1NPP, -C(=O)NRQ1NPP2, and -S(=O)2RQ1NPP; each -RQ1NPP is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -F, -OH, or -OCH3. Furthermore, each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; -RQ1NPPX is a straight-chain or branched saturated C1-4 haloalkyl group; and wherein: each -RQ2C is independently: -F, -RQ2CC, -RQ2CX,-OH, -ORQ2CC, -ORQ2CX, -NH2, -NHRQ2CC, -NRQ2CC2, -RQ2CM, -NHC(=O)RQ2CC, -NHC(=O)ORQ2CC, -C(=O)NH2, -C(=O)NHRQ2CC, -C(=O)NRQ2CC2, -C(=O)RQ2CM, -C(=O)OH, -C(=O)ORQ2CC, -OC(=O)RQ2CC, -OC(=O)NH2, -OC(=O)NHRQ2CC, -OC(=O)NRQ2CC2, -OC(=O)RQ2CM or =O; wherein: each -RQ2CC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, C3-7 Heterocyclic, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; each -RQ2CX is independently a straight-chain or branched saturated C1-4 haloalkyl; each -RQ2CM is independently a non-aromatic C3-11 heterocyclic group having at least one N ring atom and linked by that N ring atom; and: carbon atoms are optionally substituted with one or more -RQ2CMM groups; sulfur atoms, if present, are optionally substituted with one or two =O groups; and claims 6 / 15 page 7 CN 121568936 A The secondary nitrogen atom, if present, is optionally substituted with a group selected from the following: -RQ2CMM, -C(=O)RQ2CMM, -C(=O)ORQ2CMM, -C(=O)NH2, -C(=O)NHRQ2CMM, -C(=O)NRQ2CMM2, and -S(=O)2RQ2CMM; and each -RQ2CMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, - OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; and wherein: each -RQ2N is independently: -RQ2NC, =O, -C(=O)RQ2NC, -C(=O)-LQ2N-OH, -C(=O)-LQ2N-ORQ2NC,‑C(=O)‑LQ2N‑NH2, ‑C(=O)‑LQ2N‑NHRQ2NC, ‑C(=O)‑LQ2N‑NRQ2NC2, ‑C(=O)‑LQ2N‑RQ2NM, ‑C(=O)ORQ2NC, ‑LQ2N‑NH2, ‑L Q2N ‑NHRQ2NC, ‑LQ2N‑NRQ2NC2, ‑L Q2N ‑RQ2NM, ‑C(=O)NH2, ‑C(=O)NHRQ2NC, ‑C(=O)NRQ2NC2, ‑C(=O)RQ2NM, ‑LQ2N‑C(=O)NH2, ‑L Q2N ‑C(=O)NHRQ2NC、‑LQ2N‑C(=O)NRQ2NC2、‑L Q2N -C(=O)RQ2NM or -S(=O)2RQ2NC; wherein: each -RQ2NC is independently a straight-chain or branched saturated C1-6 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-6 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl is optionally substituted with one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; each -LQ2N- is independently a straight-chain or branched saturated C1-4 alkylene; each -RQ2NM is independently a non-aromatic C3-11 heterocyclic group having at least one N ring atom and connected through that N ring atom; and: The carbon atom is optionally substituted with one or more -RQ2NMM groups; the sulfur atom, if present, is optionally substituted with one or two =O groups; and the secondary nitrogen atom, if present, is optionally substituted with groups selected from: -RQ2NMM, -C(=O)RQ2NMM, -C(=O)ORQ2NMM, -C(=O)NH2, -C(=O)NHRQ2NMM, -C(=O)NRQ2NMM2 and -S(=O)2RQ2NMM Furthermore, each -RQ2NMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl group, wherein the C1-4 alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; and wherein: each -RQ3C is independently: -F, -Cl, -Br, -I, -RQ3CC, -RQ3CX, -ORQ3CX,-OH, -ORQ3CC, Claims 7 / 15 Page 8 CN 121568936 A -LQ3C-OH, -LQ3C-ORQ3CC, -NH2, -NHRQ3CC, -NRQ3CC2, -RQ3CM, -LQ3C-NH2, -LQ3C -NHRQ3CC, -LQ3C-NRQ3CC2, -LQ3C -RQ3CM, -NHC(=O)RQ3CC, -NHC(=O)ORQ3CC, -LQ3C-NHC(=O)RQ3CC, -LQ3C-NHC(=O)ORQ3CC, -C(=O)NH2, -C(=O)NHRQ3CC, -C(=O)NRQ3CC2, -C(=O)RQ3CM, -LQ3C-C(=O)NH2, -L Q3C -C(=O)NHRQ3CC, -LQ3C-C(=O)NRQ3CC2, -L Q3C -C(=O)RQ3CM, -C(=O)OH, -C(=O)ORQ3CC, -OC(=O)RQ3CC, -OC(=O)NH2, -OC(=O)NHRQ3CC, -OC(=O)NRQ3CC2, -OC(=O)RQ3CM, -S(=O)2R Q3CC, S(=O)2R Q3CM; -CN or -NO2; and two adjacent -RQ3C, if present, can together form -(CH2)n3-O-(CH2)m3-, -(CH2)n3-NH- (CH2)m3-, -(CH2)q3(C(O))-NH-(CH2)v3-, -NH-(CH2)q3C(O)(CH2)v3-O-, -NH-(CH2)p3-NH- or -O-(CH2)p3-O-, wherein: n3 is 0, 1, 2 or 3; m3 is 0, 1, 2 or 3; p3 is 1 or 2; q3 is 0, 1, 2 or 3; v3 is 0, 1, 2 or 3, provided that m3+n3 is 2 or 3; wherein: each -RQ3CC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, C3-7 heterocyclic, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally divided by -F, -OH Or -OCH3 substitution, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted by one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; each -RQ3CX is independently a straight-chain or branched saturated C1-4 haloalkyl; each -LQ3C- is independently a straight-chain or branched saturated C1-4 alkylene;Each -RQ3CM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and connected through that N-ring atom; and: the carbon atom is optionally substituted by one or more -RQ3CMM groups; the sulfur atom, if present, is optionally substituted by one or two =O groups; and the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ3CMM, -C(=O)RQ3CMM, -C(=O)ORQ3CMM, -C(=O)NH2, -C(=O)NHRQ3CMM, -C(=O)NRQ3CMM2 and -S(=O)2RQ3CMM; and each -RQ3CMM is independently a straight-chain or branched saturated -F, C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, Phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; and wherein each -RQ4C is independently: -F, -RQ4CC, -RQ4CX, -OH, -ORQ4CC, -ORQ4CX, -NH2, -NHRQ4CC, -NRQ4CC2, -RQ4CM, -NHC(=O)RQ4CC, -NHC(=O)ORQ4CC, -C(=O)NH2, -C(=O)NHRQ4CC, -C(=O)NRQ4CC2, -C(=O)RQ4CM, -C(=O)OH, -C(=O)ORQ4CC, -OC(=O)RQ4CC, -OC(=O)NH2, -OC(=O)NHRQ4CC, -OC(=O)NRQ4CC2, -OC(=O)RQ4CM or =O; wherein: each -RQ4CC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, C3-7 heterocyclic, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally surrounded by -OH or - OCH3 is substituted, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted by one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; each -RQ4CX is independently a straight-chain or branched saturated C1-4 haloalkyl group;Each -RQ4CM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and being linked by that N-ring atom; and: the carbon atom is optionally substituted by one or more -RQ4CMM groups; the sulfur atom, if present, is optionally substituted by one or two =O groups; and the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ4CMM, -C(=O)RQ4CMM, -C(=O)ORQ4CMM, -C(=O)NH2, -C(=O)NHRQ4CMM, -C(=O)NRQ4CMM2 and -S(=O)2RQ4CMM; Each -RQ4CMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl group, wherein the C1-4 alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; and wherein: each -RQ5C is independently: -F, -OH, -ORQ5CC, -OCF3, -NH2, -NHRQ5CC, -NRQ5CC2, -RQ5CM, -NHC(=O)RQ5CC, -NHC(=O)ORQ5CC, -C(=O)NH2, -C(=O)NHRQ5CC, -C(=O)NRQ5CC2, -C(=O)RQ5CM, -C(=O)OH, -C(=O)ORQ5CC, -OC(=O)RQ5CC, -OC(=O)NH2, -OC(=O)NHRQ5CC, -OC(=O)NRQ5CC2 or -OC(=O)RQ5CM; wherein: each -RQ5CC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, C3-7 heterocyclic, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally surrounded by -OH or - OCH3 is substituted, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2; each -RQ5CM is independently a non-aromatic C3-11 heterocyclic group having at least one N ring atom and being linked through that N ring atom; and: carbon atoms are optionally substituted with one or more -RQ5CMM groups; sulfur atoms, if present, are optionally substituted with one or two =O groups; and claims 9 / 15, page 10CN 121568936 A Secondary nitrogen atom, if present, optionally substituted with a group selected from the following: -RQ5CMM, -C(=O)RQ5CMM, -C(=O)ORQ5CMM, -C(=O)NH2, -C(=O)NHRQ5CMM, -C(=O)NRQ5CMM2 and -S(=O)2RQ5CMM; each -RQ5CMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, - 1. OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2. 2. The compound according to claim 1 or a pharmaceutically acceptable salt or solvate thereof, wherein: -RA1 is -RA11; and -RA11 is -RA111, -F, -Cl or -Br; and each -RA111 is independently a straight-chain or branched saturated C1-4 alkyl group. 3. The compound according to any one of the preceding claims or a pharmaceutically acceptable salt or solvate thereof, wherein: -RA2 is -RA22; -RA22 is -RA222, -F, -Cl or -Br; and each -RA222 is independently a straight-chain or branched saturated C1-4 alkyl group. 4. The compound according to any one of the preceding claims or a pharmaceutically acceptable salt or solvate thereof, wherein: -RA3 is -H or -RA33; and -RA33 is -Br. 5. A compound according to any one of the preceding claims, or a pharmaceutically acceptable salt or solvate thereof, wherein: -RA4 is -H or -RA44; -RA44 is -RA444, -Cl, or -Br; and each -RA444 is independently a straight-chain or branched saturated C1-4 alkyl group. 6. A compound according to any one of the preceding claims, or a pharmaceutically acceptable salt or solvate thereof, wherein: ring B is selected from: wherein: Y1 is S or O; Y2 is CH, CRY2, or N; Y3 is N; and each -RY2 is independently -NH2. 7. The compound according to any one of the preceding claims, or a pharmaceutically acceptable salt or solvate thereof, wherein: -Q is -Q1, or -LQ1-Q1; wherein: Q1 is a C5-10 heteroaryl group; and: the carbon atom is optionally substituted with one or more -RQ1C groups; and the secondary nitrogen atom, if present, is optionally substituted with one or more -RQ1N groups; and-LQ1- is a straight-chain or branched saturated C1-4 alkylene group; wherein each -RQ1C is independently: -F, -Cl, -Br, -RQ1CC, -RQ1CX, -ORQ1CX, -OH, -ORQ1CC, -NH2, -NHRQ1CC, -NRQ1CC2, -RQ1CM, -LQ1C-RQ1CM, -NHC(=O)RQ1CC, -N(RQ1CC)C(=O)RQ1CC, -NHC(=O)ORQ1CC, -C(=O)NH2, -C(=O)NHRQ1CC, -C(=O)NRQ1CC2, -C(=O)RQ1CM, =O, -NHC(=O)NHRQ1CC, -LQ1C-C(=O)NRQ1CC2, -C(=O)OH, -C(=O)ORQ1CC, -OC(=O)NH2, -S(=O)2RQ1CX, -S(=O)2RQ1CM, -NHS(=O)RQ1CC, -NHS(=O)2RQ1CC, -CN or -C≡CH; wherein: each -RQ1CC is independently a straight-chain or branched saturated C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, C3-7 heterocyclic, phenyl or C5-6 heteroaryl, wherein the C1-6 alkyl is optionally substituted by -OH, -CN or -OCH3, and each phenyl and heteroaryl is optionally substituted by one or more groups selected from the following: -F, -Cl, -CH3, -CHF2, -CF3, -OCH3; each -RQ1CX is independently a straight-chain or branched saturated C1-4 haloalkyl; Each -LQ1C- is independently a straight-chain or branched saturated C1-4 alkylene group; each -RQ1CM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and connected through that N-ring atom; and: the carbon atom is optionally substituted by one or more -RQ1CMM groups; the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ1CMM; and each -RQ1CMM is independently -F, -NH2, straight-chain or branched saturated C1-4 alkyl, C1-4 alkylOC(=O)NH-, C3-6 cycloalkyl, wherein the C1-4 alkyl is optionally substituted by -OH; and wherein: each -RQ1N is independently: -RQ1NC, -LQ1N-RQ1NC, -RQ1NX, -RQ1Nhet, -LQ1N-RQ1Nhet, (Claims 11 / 15, page 12, CN) 121568936 A ‑LQ1N‑OH, ‑LQ1N‑ORQ1NC, ‑S(=O)2R Q1NC, ‑LQ1N‑C(=O)OH, ‑LQ1N‑C(=O)ORQ1NC, ‑LQ1N‑C(=O)NH2, ‑L Q1N-C(=O)NHRQ1NK, -LQ1N-C(=O)NRQ1NC2, -LQ1N-C(=O)RQ1NP, -LQ1N-NH2, -LQ1N-NRQ1NC2, or -LQ1N-NHC(=O)ORQ1NC; wherein: each -RQ1NC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, phenyl, or C5-6 heteroaryl group, wherein each C1-4 alkyl group is optionally substituted with -F, -OH, -C≡N, -SO2-CH3, or -OCH3, wherein each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -Br, straight-chain or branched saturated C1-4 alkyl, -CHF2, -CF3, -CH2-O- CH3, -OCH2CH3, -C(=O)-NH-phenyl, wherein the C1-4 alkyl and phenyl groups are optionally substituted with -CH3 or -OH; each -RQ1NX is independently a straight-chain or branched saturated C1-4 haloalkyl group; each -LQ1N- is independently a straight-chain or branched saturated C1-4 alkylene group; wherein the C1-4 alkylene group is optionally substituted with -OH or -OMe; and wherein: each -RQ1Nhet is independently a non-aromatic C3-7 heterocyclic group, and: the carbon atom is optionally substituted with one or more =O groups; and the secondary nitrogen atom, if present, is optionally substituted with a group selected from the following: -RQ1NHH, -C(=O)RQINJJ, -C(=O)ORQ1NHH, -C(=O)NHRQ1NHH, -C(=O)NRQ1NHH2; wherein: Each -RQ1NHH is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, or phenyl-C1-3 alkyl group; and wherein: -RQ1NJJ is -RJ1, -LJ-RJ2, -RJ3, -LJ-RJ3, -RJ4, -LJ-RJ4, or -LJ-RJ5; -RJ1 is a straight-chain or branched saturated C1-6 alkyl group; and is optionally substituted by one or more groups selected from the following: -F, -OH, -ORJJ, -O-phenyl, -C(=O)ORJJ; each -RJ2 is independently a C3-6 cycloalkyl group; each -RJ3 is independently a non-aromatic C3-7 heterocyclic group; each -RJ4 is phenyl; and is optionally substituted by one or more groups selected from the following: -F, -ORJJ, -NH2, and -NRJJ2; Each -RJ5 is independently a C5-6 heteroaryl group; each -LJ- is independently a straight-chain or branched saturated C1-4 alkylene group, and optionally substituted with one or more -F groups; each -RJJ is a straight-chain or branched saturated C1-4 alkyl group; and wherein: -RQ1NK is -RK1, -RK2, -RK3, -LK-RK3; -RK1 is a straight-chain or branched saturated C1-7 alkyl group; and optionally substituted with one or more groups selected from the following: -F, -OH, -ORKK, -OCH2CH2OCH3, and -NRKK2; each -RK2 is independently a C3-6 cycloalkyl group; each -RK3 is independently a non-aromatic C3-7 heterocyclic group; and: the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RKK and -C(=O)ORKK; each -LK- is a straight-chain or branched saturated C1-4 alkylene group, and each -RKK is a straight-chain or branched saturated C1-4 alkyl group; and wherein: -RQ1NP is a non-aromatic C3-11 heterocyclic group having at least one N ring atom and connected through the N ring atom; and: The carbon atom is optionally substituted with one or more groups selected from -RQ1NPP, -F, -OH, -ORQ1NPP and =O; and the secondary nitrogen atom, if present, is optionally substituted with groups selected from: -RQ1NPP, -RQ1NPPX, -C(=O)RQ1NPP, -C(=O)ORQ1NPP, -C(=O)NRQ1NPP2 and -S(=O)2RQ1NPP; each -RQ1NPP is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, or phenyl group, wherein the C1-4 alkyl group is optionally substituted with -F, -OH or -OCH3; -RQ1NPPX is a straight-chain or branched saturated C1-4 haloalkyl group. 8. The compound or its pharmaceutically acceptable salt or solvate according to any one of claims 1-6, wherein: -Q is -Q2 or -LQ2-Q2; wherein: Q2 is a C3-10 heterocyclic group; and: the sulfur atom, if present, is optionally substituted by one or two =O groups; the secondary nitrogen atom, if present, is optionally substituted by one or more -RQ2N groups; and -LQ2- is a straight-chain or branched saturated C1-4 alkylene group; wherein each -RQ2N is independently: -RQ2NC, =O, -C(=O)RQ2NC, -C(=O)-LQ2N-RQ2NM, -C(=O)ORQ2NC, -LQ2N-C(=O)NRQ2NC2 or -S(=O)2RQ2NC; wherein: Each -RQ2NC is independently a straight-chain or branched saturated C1-6 alkyl, phenyl-C1-3 alkyl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-6 alkyl is optionally substituted with -OH, and each phenyl and heteroaryl is optionally substituted with one or more groups selected from -Cl and -OCH3; each -LQ2N- is independently a straight-chain or branched saturated C1-4 alkylene; each -RQ2NM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and being linked through that N-ring atom.9. The compound or its pharmaceutically acceptable salt or solvate according to any one of claims 1-6, wherein: -Q is -Q3 or -LQ3-Q3; Q3 is phenyl; and optionally substituted by one or more -RQ3C groups; and -LQ3- is a straight-chain or branched saturated C1-4 alkylene group; and wherein: each -RQ3C is independently: -F, -RQ3CC, -RQ3CX, -OH, -ORQ3CC, -NHC(=O)RQ3CC, -C(=O)NHRQ3CC, -C(=O)RQ3CM, -S(=O)2RQ3CC, S(=O)2RQ3CM; Furthermore, two adjacent -RQ3C groups, if present, can collectively form -NH-(CH2)q3C(O)(CH2)v3-O-, where q3 is 0 and v3 is 1; wherein: each -RQ3CC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, or C3-7 heterocyclic group, wherein the C1-4 alkyl group is optionally substituted with -F; each -RQ3CX is independently a straight-chain or branched saturated C1-4 haloalkyl group; each -RQ3CM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and being linked through that N-ring atom; and: carbon atoms are optionally substituted with one or more -RQ3CMM groups; each -RQ3CMM is independently -F. 10. The compound or a pharmaceutically acceptable salt or solvate thereof according to any one of claims 1-6, wherein: -Q is -Q4 or -LQ4-Q4, Q4 is a C3-10 carbocyclic group; and -LQ4- is a straight-chain or branched saturated C1-4 alkylene group. 11. The compound according to any one of claims 1-6, or a pharmaceutically acceptable salt or solvate thereof, wherein: -Q is -Q5 or -H; Q5 is a straight-chain or branched saturated C1-6 alkyl group; and optionally substituted with one or more -RQ5C groups; wherein each -RQ5C is independently: -OH, -ORQ5CC, -NHC(=O)RQ5CC, -NHC(=O)ORQ5CC, -C(=O)NH2, -C(=O)NHRQ5CC, -C(=O)RQ5CM, wherein: each -RQ5CC is independently a straight-chain or branched saturated C1-4 alkyl group; each -RQ5CM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and linked by said N-ring atom. 12. A pharmaceutical composition comprising: the compound according to any one of claims 1-11, or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier or diluent. Claims, pages 14 / 15, CN 121568936 A13. Use of the compound of any one of claims 1-11 or a pharmaceutically acceptable salt or solvate thereof in a method of treating a human or animal body by means of treatment. 14. Use of the compound of any one of claims 1-11 or a pharmaceutically acceptable salt or solvate thereof in the preparation of a medicament for treating proliferative diseases. 15. A method of treating a proliferative disease in a human or animal body, comprising administering to a subject requiring treatment a therapeutically effective amount of the compound of any one of claims 1-11 or a pharmaceutically acceptable salt or solvate thereof. 16. Use of the compound, salt, or solvate of claim 14, or the method of claim 15, wherein the proliferative disease is cancer. 17. Use of the compound, salt, or solvate of claim 14, or the method of claim 15, wherein the proliferative disease is: endometrial cancer, uterine cancer, ovarian cancer, breast cancer, gastric cancer, bladder cancer, pancreatic cancer, mesothelioma, renal cancer, gastric cancer, esophageal cancer, colorectal cancer, glioblastoma, or lung cancer. Claims 15 / 15 Page 16 CN 121568936 A Biarylamide Derivatives and Their Use as PKMYT1 Inhibitors Technical Field

[0001] This invention generally belongs to the field of therapeutic compounds. More specifically, this invention relates to specific biarylamide compounds (also referred to herein as “BAA compounds”) that are capable of inhibiting protein kinase membrane-associated tyrosine / threonine 1 (PKMYT1). This invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds and compositions to inhibit PKMYT1 kinase in vitro and in vivo; to the treatment of conditions (e.g., diseases) that can be improved by inhibiting PKMYT1 kinase; to the treatment of proliferative conditions, cancer, etc. Background Art

[0002] Related publications are cited herein to provide a more complete description of the current state of the art to which this invention pertains. Each reference is incorporated herein by reference in its entirety to the same extent as each individual reference is expressly and individually incorporated by reference.

[0003] In this specification, including the appended claims, unless the context otherwise requires, the word "comprising" and similar expressions (such as "containing" and "including") should be understood to mean including the whole or steps or groups thereof, but not to exclude any other whole or steps or groups thereof.

[0004] It must be noted that, as used in the specification and the appended claims, the singular forms "a," "an," or "the" cover the plural objects referred to, unless the context clearly states otherwise. Thus, for example, when referring to "a drug carrier," it includes a mixture of two or more such carriers, and similar cases.

[0005] Typically, ranges herein are expressed as from “about” a particular value and / or to “about” another particular value. When expressed as such a range, another implementation includes from said particular value and / or to said other particular value. Similarly, when a numerical value is expressed as an approximation (by using the prefix “about”), it should be understood that the particular value constitutes another implementation.

[0006] This disclosure includes information that may help in understanding the invention. However, this does not mean that any information provided herein is prior art or related to the invention currently claimed, nor does it mean that any publication explicitly or implicitly referenced is prior art.

[0007] Protein kinase membrane-associated tyrosine / threonine 1 (PKMYT1)

[0008] A key feature of cancer is that cancer cells break through the control of the cell cycle, which prevents entry into the dividing state until suitable conditions are met. Once conditions are suitable, the cell enters the cell division cycle through a decision point called the “restriction point” under the action of the Cdk4 / 6-cyclin D complex. Once this point of no return is reached, the cell activates Cdk2-cyclin E to drive DNA replication, subsequently separating the DNA into two daughter cells in later stages of the cell cycle (via Cdk1-cyclin B).

[0009] In order to proliferate illegally, cancer cells inappropriately enhance the kinase activity of the Cdk4 / 6-cyclin D complex, or bypass the need to activate Cdk4 / 6-cyclin D by activating the downstream Cdk2-cyclin E complex, thus becoming independent of any input signals to Cdk4 / 6-cyclin D. The execution of both pathways allows cancer to evade normal controls that maintain homeostasis and growth in the body. Thus, cancer proliferation is uncontrolled.

[0010] Drugs that inhibit the Cdk4 / 6-cyclin D complex have had a significant therapeutic impact in hormone-responsive HER2-negative breast cancer (HER2-ER+) and are being tested in a variety of other cancers. Instructions 1 / 530 pages 17 CN 121568936 A

[0011] In contrast, antagonism against the hyperactivation of Cdk2-cyclin E was considered untreatable until a recent study reported that a WEE1 family kinase called PKMYT1 is only required when cyclin E levels are abnormally high (Gallo et al., 2022). Importantly, they found that eliminating PKMYT1 did not kill normal cells.

[0012] The same study showed that eliminating PKMYT1 in the presence of cyclin E (CCNE1) overexpression is synthetically lethal; while CCNE1 overexpression promotes the transcription of cyclin B, thereby reducing cyclin B levels.The production of CCNE1 is increased to such an extent that all available Cdk1 inhibitory activity requires the inhibition of this Cdk1-cyclin B and the prevention of catastrophic mitosis. Therefore, excessive CCNE1 production leads to dependence on PKMYT1.

[0013] FBXW7 is a gene encoding an E3 ligase that degrades cyclin E. The loss of FBXW7 in the presence of PKMYT1 inhibition has been found to be synthetically lethal (Durocher et al., 2021), suggesting the potential of PKMYT1 drugs as first-line therapy in various cancers. CCNE1 amplification has been reported in several cancer types, including endometrial cancer, ovarian cancer, breast cancer, and gastric cancer, with a frequency ranging from 5% to 40%. CCNE1 amplification and / or FBXW7 mutations occur in more than 60% of uterine carcinosarcomas, more than 20% of uterine cancers, approximately 20% of ovarian cancers, approximately 18% of gastric cancers, approximately 14% of colorectal cancers, approximately 12% of bladder cancers, 11.5% of esophageal cancers, approximately 11% of cervical cancers, 7.5% of sarcomas, and approximately 7% of squamous cell carcinomas of the lung (Durocher et al., 2021). CCNE1 is also found at lower levels in other cancers, such as adenoid cystic carcinoma, pancreatic cancer, mesothelioma, lung adenocarcinoma, head and neck cancer, diffuse large B-cell lymphoma, and hepatocellular carcinoma (Gorski et al., 2020). Furthermore, ovarian cancers with CCNE1 overexpression are a 50% recombinant group and therefore cannot benefit from PARP inhibitors (Gorski et al., 2020), highlighting the unmet need in these indications.

[0014] CCNE1 amplification has been observed in more aggressive subtypes, including uterine carcinosarcoma (UCS; approximately 40%), uterine serous carcinoma (USC; approximately 25%), high-grade serous ovarian carcinoma (HGSOC; approximately 20%), and triple-negative breast cancer (TNBC; approximately 8%). Overexpression of CCNE1 in tumor biopsies is associated with lower overall survival compared to patients with normal cyclin E1 levels. HGSOC patients with CCNE1 overexpression have a lower response rate to cisplatin, which is currently the standard of care.

[0015] Similarly, FBXW7 is frequently mutated in several cancer types, including uterine carcinosarcoma, endometrial cancer, colorectal cancer, cervical cancer, bladder cancer, head and neck cancer, gastric cancer, and squamous cell carcinoma of the lung, with a frequency ranging from 5% to 39%. Similar to CCNE1 overexpression, FBXW7 driver mutations have been observed in more aggressive endometrial cancer subtypes, including UCS and USC.

[0016] Increased Cdk2-cyclin E activity through multiple pathways is also associated with resistance to Cdk4 / 6 inhibitors (Fassl et al., 2022); this suggests that inhibiting PKMYT1 will also produce [resistance] approximately 2 years after treatment with Cdk4 / 6 inhibitors.It has become an effective second-line treatment option in the population of HER2-ER+ breast cancer patients with drug resistance. The recently discovered PKMYT1 inhibitor RP-6306 (Szychowski et al., 2022) has shown efficacy in vivo in breast and ovarian cancer models overexpressing CCNE1, as well as in pancreatic PDX models with increased CCNE1 expression, when used alone or in combination with gemcitabine (Gallo et al., 2022).

[0017] It has been reported that in cancer cells, PKMYT1 inhibition is associated with synthetic lethality with protein phosphatase 2 (PP2A) deficiency, particularly the regulatory subunit Bα (PPP2R2A) deficiency (Yost et al., 2021). Inactivation of PPP2R2A is present in 15% of prostate adenocarcinomas and in more than 5% of ovarian serous cystadenocarcinomas, rectal adenocarcinomas, bladder urothelial carcinomas, colorectal adenocarcinomas, invasive breast cancers, endometrial cancers of the uterine corpus, uterine carcinosarcomas, hepatocellular carcinomas, squamous cell carcinomas of the lungs, and lung adenocarcinomas.

[0018] PKMYT1 is a cell cycle-regulated kinase belonging to the WEE1 family of kinases, which includes WEE1 and WEE2. WEE2 is restricted to the gonads because it regulates meiosis. In contrast, both PKMYT1 and WEE1 are widely expressed. PKMYT1 is mainly located in the endoplasmic reticulum and Golgi apparatus, while WEE1 is mainly located in nucleoproteins. PKMYT1 is involved in the negative regulation of the CDK1-cyclin B complex, which promotes the transition of cells from the G2 phase of the cell cycle to the mitotic phase (M phase). The biological processes of cyclin E overproduction create a demand for PKMYT1, which is not normally essential. Cyclin E accumulation promotes the transcription of cyclin B1; CCNE1 overexpression greatly enhances the potential for forming active Cdk1-cyclin B. This leads to a far greater demand for the Cdk1-cyclin B repressive activity of WEE1 and PKMYT1, making PKMYT1 essential. Furthermore, CCNE1 overproduction stimulates abnormally high levels of DNA replication, depleting the nucleotide pool and causing DNA damage (Jones et al., 2013). The DNA damage resulting from cyclin E accumulation is not inherently lethal because cells possess G2 / M checkpoints that prevent genome segregation during mitosis until all damage is repaired. These checkpoint pathways enhance the activity of Wee1 family kinases WEE1 and PKMYT1, which inhibit division by phosphorylating Cdk1 kinases, thereby blocking Cdk1-cyclin B activity. With persistent damage, WEE1 and PKMYT1 remain highly active, preventing cell division. Therefore, inhibiting WEE1 or PKMYT1 will still affect the DNA of damaged cells.Damaged and / or non-replicating cells kill them by forcing them to divide. This leads to a greater need for the ability of WEE1 and PKMYT1 to limit CDK1-cyclin B activity to maintain cell survival.

[0019] PKMYT1 can be removed from untransformed cells because WEE1 alone is sufficient to meet the need to inhibit CDK1-cyclin B1 activity. PKMYT1 activity only becomes critical when abnormally high levels of DNA damage create a greater need for CDK1-cyclin B1 inhibition.

[0020] The WEE1 inhibitor adavorcetebucil has been clinically tested in various solid tumors (clinicaltrials.gov) but has shown significant toxicity. The toxicity of WEE1 inhibition likely stems from its ability to inhibit the CDK2 and CDK1 complex. CDK2-cyclin E and CDK2-cyclin A regulate the initiation and development of DNA replication. The release of excessive levels of CDK2-cyclin activity results in DNA damage, a phenomenon known as oncogene-induced replicative senescence. PKMYT1 inhibition is unlikely to exhibit similar S-phase toxicity because, unlike WEE1, PKMYT1 phosphorylates CDK1 (Booher et al., 1997; Liu et al., 1997).

[0021] In general, the dependence on PKMYT1 due to excessive Cdk2-cyclin E activity in cancer cells, and the significantly reduced toxicity in normal tissues due to PKMYT1 inhibition of CDK1 regulation, make PKMYT1 a highly attractive inhibitory target for patients with abnormal tumor proliferation due to enhanced Cdk2-cyclin E activity.

[0022] Overexpression of PKMYT1 (compared to normal tissues) has been observed in a variety of cancers, including squamous cell carcinoma of the lung, lung adenocarcinoma, endometrial cancer of the uterine corpus, invasive breast cancer, hepatocellular carcinoma, clear cell renal cell carcinoma, chromophobe renal cell carcinoma, papillary renal cell carcinoma, squamous cell carcinoma of the head and neck, colonic adenocarcinoma, gastric adenocarcinoma, thyroid cancer, and prostate adenocarcinoma. High expression of PKMYT1 protein is associated with poor prognosis in adrenocortical carcinoma, chromophobe renal cell carcinoma, clear cell renal cell carcinoma, papillary renal cell carcinoma, low-grade glioma, hepatocellular carcinoma, lung adenocarcinoma, mesothelioma, pancreatic adenocarcinoma, prostate adenocarcinoma, cutaneous melanoma, uveal melanoma (Shao et al., 2021), and breast cancer (Liu et al., 2020).

[0023] PKMYT1 is involved in the development, invasion, and / or metastasis of many solid tumors, such as non-small cell lung cancer (Zhang et al., 2020).(References: He et al., 2022; He et al., 2021; Sun et al., 2019), osteosarcoma (Luo et al., 2022), clear cell renal cell carcinoma (Chen et al., 2020; Chen et al., 2021), oral squamous cell carcinoma (Cai et al., 2022), gastric cancer (Hu et al., 2022; Zhang et al., 2020), prostate cancer (Wang et al., 2020), esophageal squamous cell carcinoma (Zhang et al., 2019), colorectal cancer (Jeong et al., 2018), hepatocellular carcinoma (Liu et al., 2017), ovarian cancer (Xuan et al., 2020), neuroblastoma (especially with MYCN amplification) (Chayka et al., 2015), glioblastoma (Toledo et al., 2015). PKMYT1 is crucial for survival in some hematologic malignancies, such as acute lymphoblastic leukemia and multiple myeloma (Ghelli Luserna di Rora et al., 2020).

[0024] PKMYT1 can be used to address treatment resistance or to enhance the efficacy of cancer therapies. Elevated PKMYT1 levels have been reported as a resistance mechanism to persistent WEE1 inhibition (Lewis et al., 2019). PKMYT1 inhibitors may also be a useful second-line treatment to complement emerging WEE1-based therapies.

[0025] Knockdown of PKMYT1 eliminates radiation-induced G2 / M stagnation, leading to reduced survival of radiotreated cells, and is therefore a promising target for improving radiosensitivity in lung adenocarcinoma (Long et al., 2020). PKMYT1 may also be shown to enhance the efficacy of anti-microtubule cancer drugs (Visconti et al., 2017).

[0026] PKMYT1 also plays a role in viral infection. During the S phase of the cell cycle, knockdown of PKMYT1 reduces the number of cells supporting lytic infection by Kaposi's sarcoma herpesvirus (KSHV) (Bryan et al., 2006). KSHV is a precipitant for plasmablastic variants of Kaposi's sarcoma, primary exudative lymphoma (PEL), and multicentric Castleman's disease.

[0027] There is currently a clear need for selective inhibitors of PKMYT1 that have good pharmacokinetic properties, are suitable for oral administration, and have very low or no toxicity.

[0028] This disclosure provides compounds and compositions capable of selectively inhibiting PKMYT1 to treat cancer. Summary of the Invention

[0029] One aspect of the invention relates to specific biarylamide compounds (also referred to herein as "BAA compounds") as described herein, which are capable of inhibiting protein kinase membrane-associated tyrosine / threonine 1 (PKMYT1).

[0030] Another aspect of the invention relates to compositions (e.g., pharmaceutical compositions) comprising a BAA compound as described herein and a pharmaceutically acceptable carrier or diluent.

[0031] Another aspect of the invention relates to a method of preparing a composition (e.g., a pharmaceutical composition) comprising the step of mixing a BAA compound as described herein with a pharmaceutically acceptable carrier or diluent.

[0032] Another aspect of the invention relates to a method of inhibiting PKMYT1 in vitro or in vivo (e.g., inhibiting, reducing, or blocking the activity or function of PKMYT1), comprising contacting PKMYT1 with an effective amount of a BAA compound as described herein.

[0033] Another aspect of the invention relates to a method of inhibiting PKMYT1 in cells in vitro or in vivo (e.g., inhibiting, reducing, or blocking the activity or function of PKMYT1), comprising contacting cells with an effective amount of a BAA compound as described herein.

[0034] Another aspect of the invention relates to a method of using a BAA compound as described herein for treating a human or animal body by means of therapy, for example, a method of treating a condition (e.g., a disease) as described herein.

[0035] Another aspect of the invention relates to the use of the BAA compounds described herein in methods of treating a human or animal body by means of treatment, for example, in methods of treating a condition (e.g., a disease) as described herein.

[0036] Another aspect of the invention relates to the use of the BAA compounds described herein in the preparation of a medicament, for example, for a treatment method, for example, a method of treating a condition (e.g., a disease) as described herein.

[0037] Another aspect of the invention relates to a treatment method, for example, a method of treating a condition (e.g., a disease) as described herein, comprising administering a therapeutically effective amount of the BAA compound described herein to a subject requiring treatment, the BAA compound preferably being in the form of a pharmaceutical composition.

[0038] In one embodiment, the condition is one that is improved by inhibiting PKMYT1 (e.g., inhibiting or reducing or blocking the activity or function of PKMYT1).

[0039] In one embodiment, the condition is, for example, a proliferative condition, cancer, etc. as described herein.

[0040] Another aspect of the invention relates to a kit comprising (a) a BAA compound as described herein, preferably as a composition (e.g., a pharmaceutical composition) and provided in a suitable container and / or suitable packaging; and (b) instructions for use, for example, in treating a condition (e.g., a disease) as described herein, such as a written instruction on how to administer the compound.

[0041] Another aspect of the invention relates to a BAA compound obtainable by synthetic methods as described herein, or by methods including synthetic methods as described herein.

[0042] Another aspect of the invention relates to BAA compounds obtained by synthetic methods as described herein, or methods including synthetic methods as described herein.

[0043] Another aspect of the invention relates to novel intermediates as described herein, which are suitable for use in the synthetic methods described herein.

[0044] Another aspect of the invention relates to the use of such novel intermediates as described herein in the synthetic methods described herein.

[0045] Those skilled in the art will understand that features and preferred embodiments of one aspect of the invention will also apply to other aspects of the invention. Detailed Description of Embodiments

[0046] Compounds

[0047] One aspect of the present invention is a compound represented by the following formula, or a pharmaceutically acceptable salt or solvation thereof, wherein ring A and ring B are as described herein (for convenience, they are collectively referred to herein as "biarylamide compounds" or "BAA compounds"):

[0048]

[0049] Some embodiments include the following:

[0050] (1) A compound represented by the following formula:

[0051]

[0052] or a pharmaceutically acceptable salt or solvation thereof;

[0053] wherein:

[0054] Ring A is:

[0055]

[0056] wherein:

[0057] -RA1 is -RA11;

[0058] -RA11 is -RA111, -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A111, -OCF3, -NH2, -NHR A111, - NRA1112, -CN, -C(=O)RA111, -C(=O)OH, -C(=O)ORA111, -C(=O)NH2, -C(=O)NHRA111, -C(=O)NRA1112 or -S(=O)2RA111;

[0059] Each -RA111 is independently a straight-chain or branched saturated C1-4 alkyl group; Specification 5 / 530 page 21 CN 121568936 A

[0060] -RA2 is -RA22;

[0061] -RA22 is -RA222, -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A222, -OCF3, -NH2, -NHR A222, - NRA2222, -CN, -C(=O)RA222, -C(=O)OH, -C(=O)ORA222, -C(=O)NH2, -C(=O)NHRA222, -C(=O)NRA2222 or -S(=O)2RA222;

[0062] Each -RA222 is independently a straight-chain or branched saturated C1-4 alkyl group;

[0063] -RA3 is -H or -RA33;

[0064] -RA33 is -RA333, -F, -Cl, -Br, -I, -CF3, -OH, -ORA333Or -OCF3;

[0065] Each -RA333 is independently a straight-chain or branched saturated C1-4 alkyl;

[0066] -RA4 is -H or -RA44;

[0067] -RA44 is -RA444, -F, -Cl, -Br, -I, -CF3, -OH, -OR A444 or -OCF3;

[0068] Each -RA444 is independently a straight-chain or branched saturated C1-4 alkyl;

[0069] and:

[0070] Ring B is selected from:

[0071]

[0072] wherein:

[0073] Y1 is S, O, NH or NRY1;

[0074] Y2 is CH, CRY2 or N;

[0075] Y3 is N, CH or CRY3;

[0076] Y4 is N, CH or CRY4;

[0077] Y5 is S, O, NH, or NRY5;

[0078] Y6 is N, CH, or CRY6;

[0079] Y7 is N, CH, or CRY7;

[0080] Y8 is N, CH, or CRY8;

[0081] Y9 is S, O, NH, or NRY9;

[0082] Wherein:

[0083] Each -RY2, -RY3, -RY4, -RY6, -RY7, and -RY8 is independently -H, -F, -Cl, -Br, -I, -RYY, -CF3, -OH, -ORYY, -OCF3, -NH2, -NHRYY, or -NRYY2;

[0084] Each -RYY is independently a straight-chain or branched saturated C1-4 alkyl group;

[0085] And wherein:

[0086] Each -RY1, -RY5, and -RY9 is independently -RYYN, -C(=O)RYYN, -C(=O)ORYYN, -C(=O)NH2, -C(=O)NHRYYN, -C(=O)NRYYN2, or -S(=O)2RYYN;

[0087] Each -RYYN is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, - CF3, -OH, -OCH3, -NH2, -NH(CH3)2 and -N(CH3)2;

[0088] and wherein:

[0089] -Q is -Q1, -LQ1-Q1, -Q2, -LQ2-Q2, -Q3, -LQ3-Q3, -Q4, -LQ4-Q4, -Q5 or -H; Specification 6 / 530 page 22 CN 121568936 A

[0090] wherein:

[0091] Q1 is a C5-10 heteroaryl group;

[0092] and:

[0093] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[0094] the secondary nitrogen atom, if present, is optionally substituted with one or more -RQ1N groups;

[0095] -LQ1- is a straight-chain or branched saturated C1-4 alkylene group;

[0096] Q2 is a C3-10 heterocyclic group;

[0097] and:

[0098] the sulfur atom, if present, is optionally substituted with one or two =O groups;

[0099] the carbon atom is optionally substituted with one or more -RQ2C groups; and

[0100] the secondary nitrogen atom, if present, is optionally substituted with one or more -RQ2N groups;

[0101] -LQ2- is a straight-chain or branched saturated C1-4 alkylene group;

[0102] Q3 is a phenyl or naphthyl group;

[0103] and optionally substituted with one or more -RQ3C groups;

[0104] -LQ3- is a straight-chain or branched saturated C1-4 alkylene group;

[0105] Q4 is a C3-10 carbocyclic group;

[0106] and optionally substituted with one or more -RQ4C groups;

[0107] -LQ4- is a straight-chain or branched saturated C1-4 alkylene group;

[0108] Q5 is a straight-chain or branched saturated C1-6 alkyl group;

[0109] and optionally substituted with one or more -RQ5C groups;

[0110] and wherein:

[0111] Each -RQ1C is independently:

[0112] -F, -Cl, -Br, -I,

[0113] -RQ1CC,

[0114] -RQ1CX, -ORQ1CX,

[0115] -OH, -ORQ1CC,

[0116] -LQ1C-OH, -LQ1C-ORQ1CC,

[0117] -NH2, -NHR Q1CC, -NRQ1CC2, -R Q1CM,

[0118] -LQ1C-NH2, -L Q1C -NHRQ1CC, -LQ1C-NRQ1CC2, -L Q1C -RQ1CM,

[0119] -NHC(=O)RQ1CC, -N(RQ1CC)C(=O)RQ1CC, -NHC(=O)ORQ1CC,

[0120] -LQ1C-NHC(=O)RQ1CC, -LQ1C-NHC(=O)ORQ1CC,

[0121] -C(=O)NH2, -C(=O)NHRQ1CC, -C(=O)NRQ1CC2, -C(=O)RQ1CM, =O

[0122] -NHC(=O)NH2, -NHC(=O)NHRQ1CC, -NHC(O)NRQ1CC2, -NHC(=O)RQ1CM,

[0123] ‑LQ1C‑C(=O)NH2、‑L Q1C-C(=O)NHRQ1CC, -LQ1C-C(=O)NRQ1CC2, -L Q1C -C(=O)RQ1CM,

[0124] -C(=O)OH, -C(=O)ORQ1CC,

[0125] -OC(=O)RQ1CC,

[0126] -OC(=O)NH2, -OC(=O)NHRQ1CC, -OC(=O)NRQ1CC2, -OC(=O)RQ1CM,

[0127] -S(=O)2R Q1CC, -S(=O)2R Q1CX,

[0128] -S(=O)2NH2, -S(=O)2NHR Q1CC, -S(=O)2NR Q1CC 2, -S(=O)2R Q1CM, Specification 7 / 530 Page 23 CN 121568936 A

[0129] -NHS(=O)RQ1CC, -NHS(=O)2RQ1CC,

[0130] -CN, -C≡CH or -NO2;

[0131] and two adjacent -RQ1C, if present, can jointly form -(CH2)n1-O-(CH2)ml- or -O-(CH2)p1-O-, wherein: n1 is 0, 1, 2 or 3; m1 is 0, 1, 2 or 3; and p1 is 1 or 2; provided that m1+n1 is 2 or 3;

[0132] wherein:

[0133] each -RQ1CC is independently a straight-chain or branched saturated C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 Alkyl, C3-7 heterocyclic, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-6 alkyl is optionally substituted with -OH, -CN, or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from: -F, -Cl, -C1-4 alkyl, -CHF2, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2;

[0134] Each -RQ1CX is independently a straight-chain or branched saturated C1-4 haloalkyl;

[0135] Each -LQ1C is independently a straight-chain or branched saturated C1-4 alkylene;

[0136] Each -RQ1CM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and connected through the N-ring atom; and:

[0137] The carbon atom is optionally substituted with one or more -RQ1CMM groups;

[0138] the sulfur atom, if present, is optionally substituted with one or two =O groups; and

[0139] the secondary nitrogen atom, if present, is optionally substituted with groups selected from: -RQ1CMM, -C(=O).RQ1CMM, -C(=O)ORQ1CMM, -C(=O)NH2, -C(=O)NHRQ1CMM, -C(=O)NRQ1CMM2 and -S(=O)2RQ1CMM; and

[0140] each -RQ1CMM is independently -F, -NH2, straight-chain or branched saturated C1-4 alkyl, C1-4 alkylOC(=O)NH-, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein C1-4 The alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0141] and wherein:

[0142] each -RQ1N is independently:

[0143] -RQ1NC, -LQ1N-RQ1NC,

[0144] -RQ1NX,

[0145] -RQ1Nhet, -LQ1N-RQ1Nhet,

[0146] -LQ1N-OH, -LQ1N-ORQ1NC,

[0147] -LQ1N-C(=O)RQ1NC,

[0148] -S(=O)2RQ1NC,

[0149] -LQ1N-C(=O)OH, -LQ1N-C(=O)ORQ1NC,

[0150] -LQ1N-C(=O)NH2, -LQ1N-C(=O)NHRQ1NK, -LQ1N-C(=O)NRQ1NC2, -LQ1N-C(=O)RQ1NP,

[0151] -LQ1N-NH2, -LQ1N-NHRQ1NC, -LQ1N-NRQ1NC2, -LQ1N-RQ1NM,

[0152] or -LQ1N-NHC(=O)ORQ1NC:

[0153] Wherein:

[0154] Each -RQ1NC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl group, wherein each C1-4 alkyl group is optionally substituted with -F, -OH, -C≡N, -SO₂-CH₃, or -OCH₃, wherein each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -Br, straight-chain or branched saturated C1-4 alkyl, -CHF₂, -CF₃, -OH, -OCH₃, -CH₂-O-CH₃, -OCH2CH3, -C(=O)-NH-phenyl, -NH2, -NH(CH3) and -N(CH3)2; wherein the C1-4 alkyl and phenyl groups are independently and optionally substituted with -CH3 or -OH;

[0155] Each -RQ1NX is independently a straight-chain or branched saturated C1-4 haloalkyl;

[0156] Each -LQ1N- is independently a straight-chain or branched saturated C1-4 alkylene; wherein the C1-4 alkylene is optionally substituted with -OH or -OMe

[0157] Each -RQ1NM is independently a non-aromatic C3-7 heterocyclic group having at least one N ring atom and connected by the N ring atom; and:

[0158] The carbon atom is optionally substituted with one or more -RQ1NMM groups;

[0159] The sulfur atom, if present, is optionally substituted with one or two =O groups; and

[0160] the secondary nitrogen atom, if present, is optionally substituted with a group selected from: -RQ1NMM, -C(=O)RQ1NMM, -C(=O)ORQ1NMM, -C(=O)NH2, -C(=O)NHRQ1NMM, -C(=O)NRQ1NMM2 and -S(=O)2RQ1NMM; and

[0161] Each -RQ1NMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0162] and wherein:

[0163] Each -RQ1Nhet is independently a non-aromatic C3-7 heterocyclic group, and:

[0164] a sulfur atom, if present, is optionally substituted with one or two =O groups;

[0165] The carbon atom is optionally substituted with one or more -RQ1NHH groups or =O groups; and

[0166] the secondary nitrogen atom, if present, is optionally substituted with a group selected from: -RQ1NHH, -C(=O)RQ1NJJ, -C(=O)ORQ1NHH, -C(=O)NH2, -C(=O)NHRQ1NHH, -C(=O)NRQ1NHH2 and -S(=O)2RQ1NHH;

[0167] wherein:

[0168] each -RQ1NHH is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, C3-7Heterocyclic, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0169] and wherein:

[0170] -RQ1NJJ is -RJ1, -RJ2, -LJ-RJ2, -RJ3, -LJ-RJ3, -RJ4, -LJ-RJ4, -RJ5 or -LJ-RJ5;

[0171] -RJ1 is a straight-chain or branched saturated C1-6 alkyl; and is optionally substituted with one or more groups selected from the following: - F, -OH, -ORJJ, -O-phenyl, -C(=O)OH, -C(=O)ORJJ, -NH2, -NHRJJ and -NRJJ2;

[0172] Each -RJ2 is independently a C3-6 cycloalkyl group; and optionally substituted with one or more groups selected from: -F, -RJJ, -CF3, -OH, -ORJJ, -NH2, -NHRJJ and -NRJJ2;

[0173] Each -RJ3 is independently a non-aromatic C3-7 heterocyclic group; and:

[0174] The sulfur atom, if present, is optionally substituted with one or two =O groups;

[0175] The carbon atom is optionally substituted with one or more groups selected from -F, -RJJ, -CF3, -OH, -ORJJ, -NH2, -NHRJJ and -NRJJ2; and

[0176] The secondary nitrogen atom, if present, is optionally substituted with a group selected from the following: -RJJ, -C(=O)RJJ, -C(=O)ORJJ and -S(=O)2RJJ;

[0177] Each -RJ4 is phenyl; and is optionally substituted with one or more groups selected from the following: -F, -Cl, -RJJ, -CF3, -OH, -ORJJ, -NH2, -NHRJJ and -NRJJ2; Specification 9 / 530 page 25 CN 121568936 A

[0178] Each -RJ5 is independently a C5-6 heteroaryl; and:

[0179] The carbon atom is optionally substituted with one or more groups selected from -F, -RJJ, -CF3, -OH, -ORJJ, -NH2, -NHRJJ and -NRJJ2; and

[0180] Secondary nitrogen atoms, if present, are optionally substituted with groups selected from the following: -RJJ, -C(=O)RJJ, -C(=O)ORJJ and -S(=O)2RJJ;

[0181] Each -LJ- is independently a straight-chain or branched saturated C1-4 alkylene group, and is optionally substituted with one or more -F groups;

[0182] Each -RJJ is a straight-chain or branched saturated C1-4 alkyl group;

[0183] and wherein:

[0184] -RQ1NK is -RK1, -RK2, -LK-RK2, -RK3, -LK-RK3, -RK4, -LK-RK4, -RK5 or -LK-RK5;

[0185] -RK1 is a straight-chain or branched saturated C1-7 alkyl group; and optionally substituted with one or more groups selected from the following: -F, -OH, -ORKK, -OCH2CH2OCH3, -O-phenyl, -C(=O)OH, -C(=O)ORKK, -NH2, -NHRKK and -NRKK2;

[0186] Each -RK2 is independently a C3-6 cycloalkyl group; and optionally substituted with one or more groups selected from the following: -F, - RKK, -CF3, -OH, -ORKK, -NH2, -NHRKK and -NRKK2;

[0187] Each -RK3 is independently a non-aromatic C3-7 heterocyclic group; and:

[0188] The carbon atom is optionally substituted by one or more groups selected from -F, -RKK, -CF3, -OH, -ORKK, -NH2, -NHRKK and -NRKK2; and

[0189] The secondary nitrogen atom, if present, is optionally substituted by groups selected from: -RKK, -C(=O)RKK, -C(=O)ORKK and -S(=O)2RKK;

[0190] Each -RK4 is a phenyl group; and is optionally substituted by one or more groups selected from: -F, -Cl, -RKK, -CF3, -OH, -ORKK, -NH2, -NHRKK And -NRKK2;

[0191] Each -RK5 is independently a C5-6 heteroaryl; and:

[0192] The carbon atom is optionally substituted with one or more groups selected from -F, -RKK, -CF3, -OH, -ORKK, -NH2, -NHRKK and -NRKK2; and

[0193] The secondary nitrogen atom, if present, is optionally substituted with a group selected from: -RKK, -C(=O)RKK, -C(=O)ORKK and -S(=O)2RKK;

[0194] Each -LK- is a straight-chain or branched saturated C1-4 alkylene group, and is optionally substituted with one or more -F;

[0195] Each -RKK is a straight-chain or branched saturated C1-4 alkyl group;

[0196] and wherein:

[0197] -RQ1NP is a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and being linked by that N-ring atom; and:

[0198] the sulfur atom, if present, is optionally substituted with one or two =O groups;

[0199] The carbon atom is optionally substituted with one or more groups selected from -RQ1NPP, -F, -OH, -ORQ1NPP and =O; and

[0200] the secondary nitrogen atom, if present, is optionally substituted with groups selected from: -RQ1NPP, -RQ1NPPX, -C(=O)RQ1NPP, -C(=O)ORQ1NPP, -C(=O)NH2, -C(=O)NHRQ1NPP, -C(=O)NRQ1NPP2 and -S(=O)2RQ1NPP;

[0201] Each -RQ1NPP is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -F, -OH, or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2;

[0202] -RQ1NPPX is a straight-chain or branched saturated C1-4 haloalkyl; Specification 10 / 530 page 26 CN 121568936 A

[0203] and wherein:

[0204] Each -RQ2C is independently:

[0205] -F,

[0206] -RQ2CC, -RQ2CX,

[0207] -OH, -ORQ2CC, -ORQ2CX,

[0208] -NH2, -NHR Q2CC, -NRQ2CC2, -R Q2CM,

[0209] -NHC(=O)RQ2CC, -NHC(=O)ORQ2CC,

[0210] -C(=O)NH2, -C(=O)NHRQ2CC, -C(=O)NRQ2CC2, -C(=O)RQ2CM,

[0211] -C(=O)OH, -C(=O)ORQ2CC,

[0212] -OC(=O)RQ2CC,

[0213] -OC(=O)NH2, -OC(=O)NHRQ2CC, -OC(=O)NRQ2CC2, -OC(=O)RQ2CM or

[0214] =O;

[0215] wherein:

[0216] each -RQ2CC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, C3-7 heterocyclic, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0217] Each -RQ2CX is independently a straight-chain or branched saturated C1-4 haloalkyl group;

[0218] Each -RQ2CM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and connected by the N-ring atom; and:

[0219] The carbon atom is optionally substituted by one or more -RQ2CMM groups;

[0220] The sulfur atom, if present, is optionally substituted by one or two =O groups; and

[0221] The secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ2CMM, -C(=O). RQ2CMM, -C(=O)ORQ2CMM, -C(=O)NH2, -C(=O)NHRQ2CMM, -C(=O)NRQ2CMM2 and -S(=O)2RQ2CMM; and

[0222] each -RQ2CMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0223] and wherein:

[0224] Each -RQ2N is independently:

[0225] -RQ2NC,

[0226] =O, -C(=O)RQ2NC,

[0227] -C(=O)-LQ2N-OH, -C(=O)-LQ2N-ORQ2NC,

[0228] -C(=O)-LQ2N-NH2, -C(=O)-LQ2N-NHRQ2NC, -C(=O)-LQ2N-NRQ2NC2, -C(=O)-LQ2N-RQ2NM,

[0229] -C(=O)ORQ2NC,

[0230] -LQ2N-NH2, -LQ2N-NHRQ2NC, -LQ2N-NRQ2NC2, -LQ2N-RQ2NM,

[0231] -C(=O)NH2, -C(=O)NHRQ2NC, -C(=O)NRQ2NC2, -C(=O)RQ2NM,

[0232] -LQ2N-C(=O)NH2, -L Q2N -C(=O)NHRQ2NC, -LQ2N-C(=O)NRQ2NC2, -L Q2N -C(=O)RQ2NM or

[0233] -S(=O)2R Q2NC; Instruction manual 11 / 530 page 27CN 121568936 A

[0234] Wherein:

[0235] Each -RQ2NC is independently a straight-chain or branched saturated C1-6 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-6 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0236] Each -LQ2N- is independently a straight-chain or branched saturated C1-4 alkylene;

[0237] Each -RQ2NM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and linked by that N-ring atom; and:

[0238] the carbon atom is optionally substituted with one or more -RQ2NMM groups;

[0239] the sulfur atom, if present, is optionally substituted with one or two =O groups; and

[0240] the secondary nitrogen atom, if present, is optionally substituted with a group selected from: -RQ2NMM, -C(=O)RQ2NMM, -C(=O)ORQ2NMM, -C(=O)NH2, -C(=O)NHRQ2NMM, -C(=O)NRQ2NMM2 and -S(=O)2RQ2NMM; and

[0241] Each -RQ2NMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0242] and wherein:

[0243] Each -RQ3C is independently:

[0244] -F, -Cl, -Br, -I,

[0245] -RQ3CC,

[0246] -RQ3CX, -ORQ3CX,

[0247] -OH, -ORQ3CC,

[0248] -LQ3C-OH, -LQ3C-ORQ3CC,

[0249] -NH2, -NHR Q3CC, -NRQ3CC2, -R Q3CM,

[0250] -LQ3C-NH2, -L Q3C -NHRQ3CC, -LQ3C-NRQ3CC2, -L Q3C -RQ3CM,

[0251] -NHC(=O)RQ3CC, -NHC(=O)ORQ3CC,-LQ3C-NHC(=O)RQ3CC, -LQ3C-NHC(=O)ORQ3CC,

[0253] -C(=O)NH2, -C(=O)NHRQ3CC, -C(=O)NRQ3CC2, -C(=O)RQ3CM,

[0254] -LQ3C-C(=O)NH2, -L Q3C ‑C(=O)NHRQ3CC,‑LQ3C‑C(=O)NRQ3CC2,‑L Q3C‑C(=O)RQ3CM,

[0255] ‑C(=O)OH,‑C(=O)ORQ3CC,

[0256] ‑OC(=O)RQ3CC,

[0257] -OC(=O)NH2, -OC(=O)NHRQ3CC, -OC(=O)NRQ3CC2, -OC(=O)RQ3CM,

[0258] -S(=O)2RQ3CC, S(=O)2RQ3CM;

[0259] -CN or -NO2;

[0260] and two adjacent -RQ3C, if present, can jointly form -(CH2)n3-O-(CH2)m3-, -(CH2)n3-NH-(CH2)m3-, -(CH2)q3(C(O))-NH-(CH2)v3-, -NH-(CH2)q3C(O)(CH2)v3-O-, -NH-(CH2)p3-NH- or - O-(CH2)p3-O-, wherein: n3 is 0, 1, 2 or 3; m3 is 0, 1, 2 or 3; p3 is 1 or 2; q3 is 0, 1, 2 or 3; v3 is 0, 1, 2 or 3, provided that m3+n3 is 2 or 3;

[0261] wherein: Specification 12 / 530 page 28 CN 121568936 A

[0262] Each -RQ3CC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, C3-7 heterocyclic, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted by -F, -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl is optionally substituted by one or more groups selected from the following: - F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0263] Each -RQ3CX is independently a straight-chain or branched saturated C1-4 haloalkyl group;

[0264] Each -LQ3C is independently a straight-chain or branched saturated C1-4 alkylene group;

[0265] Each -RQ3CM is independently a non-aromatic C3-11 heterocyclic group having at least one N ring atom and being linked by the N ring atom; and:

[0266] The carbon atom is optionally substituted by one or more -RQ3CMM groups;

[0267] The sulfur atom, if present, is optionally substituted with one or two =O groups; and

[0268] The secondary nitrogen atom, if present, is optionally substituted with a group selected from: -RQ3CMM, -C(=O)RQ3CMM, -C(=O)ORQ3CMM, -C(=O)NH2, -C(=O)NHRQ3CMM, -C(=O)NRQ3CMM2 and -S(=O)2RQ3CMM; and

[0269] Each -RQ3CMM is independently a straight-chain or branched saturated -F, C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3. Substitution, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted by one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0270] and wherein:

[0271] Each -RQ4C is independently:

[0272] -F,

[0273] -RQ4CC, -RQ4CX,

[0274] -OH, -ORQ4CC, -ORQ4CX,

[0275] -NH2, -NHRQ4CC, -NRQ4CC2, -RQ4CM,

[0276] -NHC(=O)RQ4CC, -NHC(=O)ORQ4CC,

[0277] -C(=O)NH2, -C(=O)NHRQ4CC, -C(=O)NRQ4CC2, -C(=O)RQ4CM,

[0278] -C(=O)OH, -C(=O)ORQ4CC,

[0279] -OC(=O)RQ4CC,

[0280] -OC(=O)NH2, -OC(=O)NHRQ4CC, -OC(=O)NRQ4CC2, -OC(=O)RQ4CM or

[0281] =O;

[0282] Wherein:

[0283] Each -RQ4CC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, C3-7 Heterocyclic, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2;

[0284] Each -RQ4CX is independently a straight-chain or branched saturated C1-4 haloalkyl;

[0285] Each -RQ4CM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and connected through that N-ring atom; and:

[0286] the carbon atom is optionally substituted with one or more -RQ4CMM groups;

[0287] the sulfur atom, if present, is optionally substituted with one or two =O groups; and

[0288] the secondary nitrogen atom, if present, is optionally substituted with a group selected from: -RQ4CMM, -C(=O)ORQ4CMM, -C(=O)NH2, -C(=O)NHRQ4CMM, -C(=O)NRQ4CMM2 and -S(=O)2RQ4CMM;

[0289] Each -RQ4CMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0290] and wherein:

[0291] Each -RQ5C is independently:

[0292] -F, -OH, -ORQ5CC, -OCF3,

[0293] -NH2, -NHRQ5CC, -NRQ5CC2, -RQ5CM,

[0294] -NHC(=O)RQ5CC, -NHC(=O)ORQ5CC,

[0295] -C(=O)NH2, -C(=O)NHRQ5CC, -C(=O)NRQ5CC2, -C(=O)RQ5CM,

[0296] -C(=O)OH, -C(=O)ORQ5CC,

[0297] -OC(=O)RQ5CC,

[0298] -OC(=O)NH2, -OC(=O)NHRQ5CC, -OC(=O)NRQ5CC2 or -OC(=O)RQ5CM;

[0299] Wherein:

[0300] Each -RQ5CC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, C3-7 Heterocyclic, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from the following:F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0301] Each -RQ5CM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and connected by that N-ring atom; and:

[0302] The carbon atom is optionally substituted by one or more -RQ5CMM groups;

[0303] The sulfur atom, if present, is optionally substituted by one or two =O groups; and

[0304] The secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ5CMM, -C(=O)RQ5CMM, -C(=O)ORQ5CMM, -C(=O)NH2, -C(=O)NHRQ5CMM, -C(=O)NRQ5CMM2 and -S(=O)2RQ5CMM;

[0305] Each -RQ5CMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or Cs-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0306] (2) A compound represented by the following formula:

[0307]

[0308] or a pharmaceutically acceptable salt or solvate thereof (e.g., a pharmaceutically acceptable salt thereof);

[0309] wherein:

[0310] ring A is: Specification 14 / 530 pages 30 CN 121568936 A

[0311]

[0312] wherein:

[0313] -RA1 is -RA11;

[0314] -RA11 is -RA111, -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A111, -OCF3, -NH2, -NHR A111, - NRA1112, -CN, -C(=O)RA111, -C(=O)OH, -C(=O)ORA111, -C(=O)NH2, -C(=O)NHRA111, -C(=O)NRA1112 or -S(=O)2RA111;

[0315] Each -RA111 is independently a straight-chain or branched saturated C1-4 alkyl group;

[0316] -RA2 is -RA22;

[0317] -RA22 is -RA222, -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -ORA222, -OCF3, -NH2, -NHRA222, -NRA2222, -CN, -C(=O)RA222, -C(=O)OH, -C(=O)ORA222, -C(=O)NH2, -C(=O)NHRA222, -C(=O)NRA2222 or -S(=O)2RA222;

[0318] Each -RA222 is independently a straight-chain or branched saturated C1-4 alkyl group;

[0319] -RA3 is -H or -RA33;

[0320] -RA33 is -RA333, -F, -Cl, -Br, -I, -CF3, -OH, -ORA333 or -OCF3;

[0321] Each -RA333 is independently a straight-chain or branched saturated C1-4 alkyl group;

[0322] -RA4 is -H or -RA44;

[0323] -RA44 is -RA444, -F, -Cl, -Br, -I, -CF3, -OH, -OR A444 or -OCF3;

[0324] Each -RA444 is independently a straight-chain or branched saturated C1-4 alkyl group;

[0325] and:

[0326] Ring B is selected from:

[0327]

[0328] wherein:

[0329] Y1 is S, O, NH, NRY1;

[0330] Y2 is CH, CRY2 or N;

[0331] Y3 is N, CH or CRY3;

[0332] Y4 is N, CH or CRY4;

[0333] Y5 is S, O, NH, NRY5;

[0334] Y6 is N, CH or CRY6;

[0335] Y7 is N, CH or CRY7;

[0336] Y8 is N, CH or CRY8;

[0337] Y9 is S, O, NH, NRY9;

[0338] Wherein:

[0339] Each -RY2, -RY3, -RY4, -RY6, -RY7 and -RY8 is independently -H, -F, -Cl, -Br, -I, -RYY, -CF3, -OH, -ORYY, -OCF3, -NH2, -NHRYY or -NRYY2;

[0340] Each -RYY is independently a straight-chain or branched saturated C1-4 alkyl group;

[0341] And wherein:

[0342] Each -RY1, -RY5 and -RY9 is independently -RYYN, -C(=O)RYYN, -C(=O)ORYYN, -C(=O)NH2, -C(=O) NHRYYN, -C(=O)NRYYN2 or -S(=O)2RYYN;

[0343] Each -RYYN is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl,Phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0344] and wherein:

[0345] -Q is -Q1, -LQ1-Q1, -Q2, -LQ2-Q2, -Q3, -LQ3-Q3, -Q4, -LQ4-Q4, -Q5

[0346] or -H;

[0347] wherein:

[0348] Q1 is C5-10 heteroaryl;

[0349] and:

[0350] The carbon atom is optionally substituted with one or more -RQ1C groups; and

[0351] the secondary nitrogen atom, if present, is optionally substituted with one or more -RQ1N groups;

[0352] -LQ1- is a straight-chain or branched saturated C1-4 alkylene group;

[0353] Q2 is a non-aromatic C3-7 heterocyclic group;

[0354] and:

[0355] the sulfur atom, if present, is optionally substituted with one or two =O groups;

[0356] the carbon atom is optionally substituted with one or more -RQ2C groups; and

[0357] the secondary nitrogen atom, if present, is optionally substituted with one or more -RQ2N groups;

[0358] -LQ2- is a straight-chain or branched saturated C1-4 alkylene group;

[0359] Q3 is a phenyl or naphthyl group;

[0360] and is optionally substituted with one or more -RQ3C groups;

[0361] -LQ3- is a straight-chain or branched saturated C1-4 alkylene group;

[0362] Q4 is a C3-7 cycloalkyl group;

[0363] and optionally substituted with one or more -RQ4C groups;

[0364] -LQ4- is a straight-chain or branched saturated C1-4 alkylene group;

[0365] Q5 is a straight-chain or branched saturated C1-6 alkyl group;

[0366] and optionally substituted with one or more -RQ5C groups;

[0367] and wherein:

[0368] Each -RQ1C is independently:

[0369] -F, -Cl, -Br, -I,

[0370] -RQ1CC,

[0371] -RQ1CX, -ORQ1CX,

[0372] -OH, -ORQ1CC,

[0373] -LQ1C-OH, -LQ1C-ORQ1CC, Specification 16 / 530 pages 32 CN 121568936 A

[0374] -NH2, -NHR Q1CC, -NRQ1CC2, -R Q1CM,

[0375] -LQ1C-NH2, -L Q1C‑NHRQ1CC, ‑LQ1C‑NRQ1CC2, ‑L Q1C ‑RQ1CM,

[0376] ‑NHC(=O)RQ1CC, ‑NHC(=O)ORQ1CC,

[0377] ‑LQ1C‑NHC(=O)RQ1CC, ‑LQ1C‑NHC(=O)ORQ1CC,

[0378] -C(=O)NH2, -C(=O)NHRQ1CC, -C(=O)NRQ1CC2, -C(=O)RQ1CM

[0380] -C(=O)OH, -C(=O)ORQ1CC,

[0381] -OC(=O)RQ1CC,

[0382] -OC(=O)NH2, -OC(=O)NHRQ1CC, -OC(=O)NRQ1CC2, -OC(=O)RQ1CM,

[0383] -S(=O)2RQ1CC,

[0384] -S(=O)2NH2, -S(=O)2NHRQ1CC, -S(=O)2NRQ1CC2, -S(=O)2NRQ1CM,

[0385] -CN or -NO2;

[0386] and two adjacent -RQ1C, if present, can together form -(CH2)n1-O-(CH2)m1- or -O- (CH2)p1-O-, wherein: n1 is 0, 1, 2 or 3; m1 is 0, 1, 2 or 3; and p1 is 1 or 2; provided that m1+n1 is 2 or 3;

[0387] wherein:

[0388] each -RQ1CC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, C3-7 heterocyclic, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0389] Each -RQ1CX is independently a straight-chain or branched saturated C1-4 haloalkyl group;

[0390] Each -LQ1C is independently a straight-chain or branched saturated C1-4 alkylene group;

[0391] Each -RQ1CM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and being linked by the N-ring atom; and:

[0392] The carbon atom is optionally substituted by one or more -RQ1CMM groups;

[0393] The sulfur atom, if present, is optionally substituted with one or two =O groups; and

[0394] the secondary nitrogen atom, if present, is optionally substituted with a group selected from: -RQ1CMM, -C(=O)RQ1CMM, -C(=O)ORQ1CMM, -C(=O)NH2, -C(=O)NHRQ1CMM, -C(=O)NRQ1CMM2 and -S(=O)2RQ1CMM; and

[0395] Each -RQ1CMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0396] and wherein:

[0397] Each -RQ1N is independently:

[0398] -RQ1NC,

[0399] -RQ1NX,

[0400] -RQ1Nhet, -LQ1N-RQ1Nhet,

[0401] -LQ1N-OH, -LQ1N-ORQ1NC,

[0402] -LQ1N-C(=O)RQ1NC,

[0403] -LQ1N-C(=O)OH, -LQ1N-C(=O)ORQ1NC, Specification 17 / 530 Page 33 CN 121568936 A

[0404] -LQ1N-C(=O)NH2, -LQ1N-C(=O)NHRQ1NK, -LQ1N-C(=O)NRQ1NC2, -LQ1N-C(=O)RQ1NP,

[0405] -LQ1N-NH2, -LQ1N-NHRQ1NC, -LQ1N-NRQ1NC2, -LQ1N-RQ1NM,

[0406] Or -RQ1N-NHC(=O)ORQ1NC;

[0407] wherein:

[0408] each -RQ1NC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein each cycloalkyl, phenyl and heteroaryl is optionally substituted by one or more groups selected from the following: -F, -Cl, -CH3-CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0409] each -RQ1NX is independently a straight-chain or branched saturated C1-4 haloalkyl;

[0410] Each -LQ1N- is independently a straight-chain or branched saturated C1-4 alkylene group;

[0411] Each -RQ1NM is independently a non-aromatic C3-7 heterocyclic group having at least one N-ring atom and connected by the N-ring atom; and:

[0412] The carbon atom is optionally substituted with one or more -RQ1CMM groups;

[0413] The sulfur atom, if present, is optionally substituted with one or two =O groups; and

[0414] The secondary nitrogen atom, if present, is optionally substituted with a group selected from: -RQ1NMM, -C(=O)RQ1NMM, -C(=O)ORQ1NMM, -C(=O)NH2, -C(=O)NHRQ1NMM, -C(=O)NRQ1NMM2 and -S(=O)2RQ1NMM; and

[0415] Each -RQ1NMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0416] and wherein:

[0417] Each -RQ1Nhet is independently a non-aromatic C3-7 heterocyclic group, and:

[0418] a sulfur atom, if present, is optionally substituted with one or two =O groups;

[0419] The carbon atom is optionally substituted with one or more -RQ1NHH groups or =O groups; and

[0420] the secondary nitrogen atom, if present, is optionally substituted with a group selected from the following: -RQ1NHH, -C(=O)RQ1NJJ, -C(=O)ORQ1NHH, -C(=O)NH2, -C(=O)NHRQ1NHH, -C(=O)NRQ1NHH2 and -S(=O)2RQ1NHH;

[0421] wherein:

[0422] each -RQ1NHH is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, C3-7 heterocyclic, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH Or -OCH3 substitution, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0423] and wherein:

[0424] -RQ1NJJ is -RJ1, -RJ2, -LJ-RJ2, -RJ3, -LJ-RJ3, -RJ4, -LJ-RJ4, -RJ5, or -LJ-RJ5;

[0425] -RJ1 is a straight-chain or branched saturated C1-6 alkyl group; and optionally substituted with one or more groups selected from the following: -F, -OH, -ORJJ, -O-phenyl, -C(=O)OH, -C(=O)ORJJ, -NH2, -NHRJJ, and -NRJJ2;

[0426] Each -RJ2 is independently a C3-6 cycloalkyl group; and optionally substituted with one or more groups selected from the following: -F, -RJJ, -CF3, -OH, -ORJJ, -NH2, -NHRJJ, and -NRJJ2;

[0427] Each -RJ3 is independently a non-aromatic C3-7 heterocyclic group; and:

[0428] the sulfur atom, if present, is optionally substituted with one or two =O groups; Specification 18 / 530 page 34 CN 121568936 A

[0429] the carbon atom is optionally substituted with one or more groups selected from -F, -RJJ, -CF3, -OH, -ORJJ, -NH2, -NHRJJ and -NRJJ2; and

[0430] the secondary nitrogen atom, if present, is optionally substituted with groups selected from: -RJJ, -C(=O)RJJ, -C(=O)ORJJ and -S(=O)2RJJ;

[0431] each -RJ4 is a phenyl group; and is optionally substituted with one or more groups selected from: -F, -Cl, -RJJ, -CF3, -OH, -OR JJ, -NH2, -NHR JJ and -NRJJ2;

[0432] Each -RJ5 is independently a C5-6 heteroaryl; and:

[0433] The carbon atom is optionally substituted by one or more groups selected from -F, -RJJ, -CF3, -OH, -OR JJ, -NH2, -NHR JJ and -NRJJ2; and

[0434] The secondary nitrogen atom, if present, is optionally substituted by groups selected from: -RJJ, -C(=O)RJJ, -C(=O)ORJJ and -S(=O)2RJJ;

[0435] Each -LJ- is independently a straight-chain or branched saturated C1-4 alkylene group, and is optionally substituted by one or more -F;

[0436] Each -RJJ is a straight-chain or branched saturated C1-4 alkyl group;

[0437] and wherein:

[0438] -RQ1NK is -RK1, -RK2, -LK-RK2, -RK3, -LK-RK3, -RK4, -LK-RK4, -RK5, or -LK-RK5;

[0439] -RK1 is a straight-chain or branched saturated C1-7 alkyl group; and optionally substituted by one or more groups selected from the following:F, -OH, -ORKK, -OCH2CH2OCH3, -O-phenyl, -C(=O)OH, -C(=O)ORKK, -NH2, -NHR KK and -NRKK2;

[0440] Each -RK2 is independently a C3-6 cycloalkyl group; and optionally substituted with one or more groups selected from: -F, -RKK, -CF3, -OH, -OR KK, -NH2, -NHR KK and -NRKK2;

[0441] Each -RK3 is independently a non-aromatic C3-7 heterocyclic group; and:

[0442] The carbon atom is optionally substituted with one or more groups selected from -F, -RKK, -CF3, -OH, -OR KK, -NH2, -NHR KK and -NRKK2; and

[0443] The secondary nitrogen atom, if present, is optionally substituted with a group selected from the following groups: -RKK, -C(=O)RKK, -C(=O)ORKK, and -S(=O)2RKK;

[0444] Each -RK4 is phenyl; and is optionally substituted with one or more groups selected from the following groups: -F, -Cl, -RKK, -CF3, -OH, -ORKK, -NH2, -NHRKK, and -NRKK2;

[0445] Each -RK5 is independently a C5-6 heteroaryl; and:

[0446] The carbon atom is optionally substituted with one or more groups selected from -F, -RKK, -CF3, -OH, -ORKK, -NH2, -NHRKK, and -NRKK2; and

[0447] Secondary nitrogen atoms, if present, are optionally substituted with groups selected from: -RKK, -C(=O)RKK, -C(=O)ORKK, and -S(=O)2RKK;

[0448] Each -LK- is a straight-chain or branched saturated C1-4 alkylene group, and is optionally substituted with one or more -F groups;

[0449] Each -RKK is a straight-chain or branched saturated C1-4 alkyl group;

[0450] and wherein:

[0451] -RQ1NP is a non-aromatic C3-11 heterocyclic group having at least one N-ring atom, and is linked by the N-ring atom; and:

[0452] Sulfur atoms, if present, are optionally substituted with one or two =O groups;

[0453] Carbon atoms are optionally substituted with one or more groups selected from -RQ1NPP, -F, -OH, -ORQ1NPP, and =O; and

[0454] The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -RQ1NPP, -RQ1NPPX, -C (= ... [Specification 19 / 530, page 35, CN 121568936 A])-RQ1NPP, -C(=O)ORQ1NPP, -C(=O)NH2, -C(=O)NHRQ1NPP, -C(=O)NRQ1NPP2 and -S(=O)2RQ1NPP;

[0455] Each -RQ1NPP is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0456] -RQ1NPPX is a straight-chain or branched saturated C1-4 haloalkyl group;

[0457] and wherein:

[0458] Each -RQ2C is independently:

[0459] -F,

[0460] -RQ2CC, -RQ2CX,

[0461] -OH, -ORQ2CC, -ORQ2CX,

[0462] -NH2, -NHRQ2CC, -NRQ2CC2, -RQ2CM,

[0463] -NHC(=O)RQ2CC, -NHC(=O)ORQ2CC,

[0464] -C(=O)NH2, -C(=O)NHRQ2CC, -C(=O)NRQ2CC2, -C(=O)RQ2CM,

[0465] -C(=O)OH, -C(=O)ORQ2CC,

[0466] -OC(=O)RQ2CC,

[0467] -OC(=O)NH2, -OC(=O)NHRQ2CC, -OC(=O)NRQ2CC2, -OC(=O)RQ2CM or

[0468] =O;

[0469] wherein:

[0470] each -RQ2CC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, C3-7 heterocyclic, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl is optionally substituted with one or more groups selected from the following: - F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0471] Each -RQ2CX is independently a straight-chain or branched saturated C1-4 haloalkyl group;

[0472] Each -RQ2CM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and connected through this N-ring atom; and:

[0473] The carbon atom is optionally substituted with one or more -RQ2CMM groups;

[0474] the sulfur atom, if present, is optionally substituted with one or two =O groups; and

[0475] the secondary nitrogen atom, if present, is optionally substituted with a group selected from: -RQ2CMM, -C(=O)RQ2CMM, -C(=O)ORQ2CMM, -C(=O)NH2, -C(=O)NHRQ2CMM, -C(=O)NRQ2CMM2 and -S(=O)2RQ2CMM; and

[0476] Each -RQ2CMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0477] and wherein:

[0478] Each -RQ2N is independently:

[0479] -RQ2NC,

[0480] -C(=O)RQ2NC,

[0481] -C(=O)-LQ2N-OH, -C(=O)-LQ2N-ORQ2NC, Specification 20 / 530 Page 36 CN 121568936 A

[0482] -C(=O)-LQ2N-NH2, -C(=O)-LQ2N-NHRQ2NC, -C(=O)-LQ2N-NRQ2NC2, -C(=O)-LQ2N-RQ2NM,

[0483] -C(=O)ORQ2NC,

[0484] -LQ2N-NH2, -LQ2N-NHRQ2NC, -LQ2N-NRQ2NC2, -LQ2N-RQ2NM,

[0485] -C(=O)NH2, -C(=O)NHRQ2NC, -C(=O)NRQ2NC2, -C(=O)RQ2NM,

[0486] -LQ2N-C(=O)NH2, -L Q2N-C(=O)NHRQ2NC, -LQ2N-C(=O)NRQ2NC2, -L Q2N-C(=O)RQ2NM or

[0487] -S(=O)2R Q2NC;

[0488] wherein:

[0489] each -RQ2NC is independently a straight-chain or branched saturated C1-6 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-6 alkyl is optionally replaced by -OH or -OCH3.The cycloalkyl, phenyl, and heteroaryl groups are optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0490] Each -LQ2N- is independently a straight-chain or branched saturated C1-4 alkylene group;

[0491] Each -RQ2NM is independently a non-aromatic C3-11 heterocyclic group having at least one N ring atom and being linked by the N ring atom; and:

[0492] The carbon atom is optionally substituted with one or more -RQ2NMM groups;

[0493] The sulfur atom, if present, is optionally substituted with one or two =O groups; and

[0494] The secondary nitrogen atom, if present, is optionally substituted with a group selected from the following: -RQ2NMM, -C(=O) RQ2NMM, -C(=O)ORQ2NMM, -C(=O)NH2, -C(=O)NHRQ2NMM, -C(=O)NRQ2NMM2 and -S(=O)2RQ2NMM; and

[0495] each -RQ2NMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0496] and wherein:

[0497] Each -RQ3C is independently:

[0498] -F, -Cl, -Br, -I,

[0499] -RQ3CC,

[0500] -RQ3CX, -ORQ3CX,

[0501] -OH, -ORQ3CC,

[0502] -LQ3C-OH, -LQ3C-ORQ3CC,

[0503] -NH2, -NHRQ3CC, -NRQ3CC2, -RQ3CM,

[0504] -LQ3C-NH2, -LQ3C-NHRQ3CC, -LQ3C-NRQ3CC2, -LQ3C-RQ3CM,

[0505] -NHC(=O)RQ3CC, -NHC(=O)ORQ3CC,

[0506] -LQ3C-NHC(=O)RQ3CC, -LQ3C-NHC(=O)ORQ3CC,

[0507] -C(=O)NH2, -C(=O)NHRQ3CC, -C(=O)NRQ3CC2, -C(=O)RQ3CM,

[0508] -LQ3C-C(=O)NH2, -L Q3C-C(=O)NHRQ3CC, -LQ3C-C(=O)NRQ3CC2, -LQ3C-C(=O)RQ3CM,

[0509] -C(=O)OH, -C(=O)ORQ3CC,

[0510] -OC(=O)RQ3CC,

[0511] -OC(=O)NH2, -OC(=O)NHRQ3CC, -OC(=O)NRQ3CC2, -OC(=O)RQ3CM,

[0512] -CN or -NO2; Specification 21 / 530 page 37 CN 121568936 A

[0513] and two adjacent -RQ3C, if present, can together form -(CH2)n3-O-(CH2)m3- or -O- (CH2)p3-O-, wherein: n3 is 0, 1, 2 or 3; m3 is 0, 1, 2 or 3; and p3 is 1 or 2; provided that m3+n3 is 2 or 3;

[0514] wherein:

[0515] each -RQ3CC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, C3-7 heterocyclic, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0516] Each -RQ3CX is independently a straight-chain or branched saturated C1-4 haloalkyl group;

[0517] Each -LQ3C is independently a straight-chain or branched saturated C1-4 alkylene group;

[0518] Each -RQ3CM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and being linked by the N-ring atom; and:

[0519] The carbon atom is optionally substituted by one or more -RQ3CMM groups;

[0520] The sulfur atom, if present, is optionally substituted by one or two =O groups; and

[0521] The secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ3CMM, -C(=O)RQ3CMM, -C(=O)ORQ3CMM, -C(=O)NH2, -C(=O)NHRQ3CMM, -C(=O)NRQ3CMM2 and -S(=O)2R Q3CMM; and

[0522] each -RQ3CMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally replaced by -OH or -OCH3.The cycloalkyl, phenyl, and heteroaryl groups are optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0523] and wherein:

[0524] Each -RQ4C is independently:

[0525] -F,

[0526] -RQ4CC, -RQ4CX,

[0527] -OH, -ORQ4CC, -ORQ4CX,

[0528] -NH2, -NHRQ4CC, -NRQ4CC2, -RQ4CM,

[0529] -NHC(=O)RQ4CC, -NHC(=O)ORQ4CC,

[0530] -C(=O)NH2, -C(=O)NHRQ4CC, -C(=O)NRQ4CC2, -C(=O)RQ4CM,

[0531] -C(=O)OH, -C(=O)ORQ4CC,

[0532] -OC(=O)RQ4CC,

[0533] -OC(=O)NH2, -OC(=O)NHRQ4CC, -OC(=O)NRQ4CC2, -OC(=O)RQ4CM or

[0534] =O;

[0535] Wherein:

[0536] Each -RQ4CC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, C3-7 Heterocyclic, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2;

[0537] Each -RQ4CX is independently a straight-chain or branched saturated C1-4 haloalkyl;

[0538] Each -RQ4CM is independently a non-aromatic C3-11 heterocyclic group having at least one N ring atom and linked by the N ring atom; and: Specification 22 / 530 page 38 CN 121568936 A

[0539] The carbon atom is optionally substituted with one or more -RQ4CMM groups;

[0540] The sulfur atom, if present, is optionally substituted with one or two =O groups; and

[0541] the secondary nitrogen atom, if present, is optionally substituted with a group selected from: -RQ4CMM, -C(=O)RQ4CMM, -C(=O)ORQ4CMM, -C(=O)NH2, -C(=O)NHRQ4CMM, -C(=O)NRQ4CMM2 and -S(=O)2RQ4CMM;

[0542] Each -RQ4CMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2;

[0543] and wherein:

[0544] Each -RQ5C is independently:

[0545] -F, -OH, -ORQ5CC, -OCF3,

[0546] -NH2, -NHRQ5CC, -NRQ5CC2, -RQ5CM,

[0547] -NHC(=O)RQ5CC, -NHC(=O)ORQ5CC,

[0548] -C(=O)NH2, -C(=O)NHRQ5CC, -C(=O)NRQ5CC2, -C(=O)RQ5CM,

[0549] -C(=O)OH, -C(=O)ORQ5CC,

[0550] -OC(=O)RQ5CC,

[0551] -OC(=O)NH2, -OC(=O)NHRQ5CC, -OC(=O)NRQ5CC2 or -OC(=O)RQ5CM;

[0552] Wherein:

[0553] Each -RQ5CC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, C3-7 Heterocyclic groups, phenyl groups, phenyl-C1-3 alkyl groups, C5-6 heteroaryl groups, or C5-6 heteroaryl-C1-3 alkyl groups, wherein the C1-4 alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from the group consisting of -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2;

[0554] Each -RQ5CM is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and being linked by the N-ring atom; and:

[0555] The carbon atom is optionally substituted with one or more -RQ5CMM groups;

[0556] The sulfur atom, if present, is optionally substituted with one or two =O groups; and

[0557] The secondary nitrogen atom, if present, is optionally substituted with a group selected from the following: -RQ5CMM, -C(=O)RQ5CMM, -C(=O)ORQ5CMM, -C(=O)NH2, -C(=O)NHRQ5CMM, -C(=O)NRQ5CMM2 and -S(=O)2RQ5CMM;

[0558] Each -RQ5CMM is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl, or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl, and heteroaryl is optionally substituted with one or more groups selected from the group consisting of -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3), and -N(CH3)2.

[0559] To avoid ambiguity:

[0560] The nitrogen atom in the central amide group (-NH-C(=O)- linking ring A and ring B) is intended to be unsubstituted.

[0561] The meta-OH substituent on ring A is intended to be unsubstituted.

[0562] Ring B is intended not to fuse with any other ring.

[0563] In terms such as “C9-10 heteroaryl” and “C3-7 heterocyclic group”, the index “Cx-y” refers to the number of ring atoms, which can be carbon atoms or heteroatoms (e.g., N, O, S, as the case may be). For example, pyridyl is an example of a C6 heteroaryl, and piperidinyl is an example of a C6 heterocyclic group. Specification 23 / 530 pages 39 CN 121568936 A

[0564] The term “heteroaryl” refers to a group that is attached to the rest of the molecule by an atom that is part of an aromatic ring system having one or more heteroatoms (e.g., N, O, S, as the case may be). Unless otherwise stated, heteroaryl groups can be attached by a ring carbon atom or a ring nitrogen atom. For example, pyridyl is an example of a C6 heteroaryl, and quinolinyl (e.g., quinolin-2-yl, quinolin-7-yl, etc.) is an example of a C10 heteroaryl. Furthermore, the aromatic ring system may optionally be fused with one or more non-aromatic rings, which may contain one or more heteroatoms (e.g., N, O, S, as the case may be) or contain only carbon atoms. For example, 4,5,6,7-tetrahydro-1H-indol-2-yl is an example of a C9 heteroaryl; 4,5,6,7-tetrahydro-1H-pyrrolo[2,3-b]pyridin-2-yl is an example of a C9 heteroaryl. Pyridinyl and furan are examples of C5-6 heteroaryl.

[0565] The term "heterocyclic group" refers to a group comprising at least one non-aromatic ring system (comprising one or more heteroatoms (e.g., N, O, S, as the case may be)) which is connected to the remainder of the molecule by an atom belonging to a portion of the non-aromatic ring system (comprising one or more heteroatoms (e.g., N, O, S, as the case may be)). Unless otherwise stated, heterocyclic groups may be connected by cyclic carbon atoms or cyclic nitrogen atoms. In one implementation, the term "heterocyclic group" refers to a group belonging to the class of heterocyclic groups.A group in which an atom of a non-aromatic ring is attached to the remainder of the molecule, wherein the non-aromatic ring is part of a non-aromatic ring system having one or more heteroatoms (e.g., N, O, S, as the case may be). Unless otherwise stated, the sulfide ring atom may be substituted with one or two oxygen (=O) groups (e.g., as in 1,1-dioxo-1,4-thiazinyl-4-yl). Unless otherwise stated, "heterocyclic group" includes monocyclic heterocyclic groups (e.g., piperidinyl, an example of a monocyclic C6 heterocyclic group), fused heterocyclic groups (e.g., 3-azabicyclo[3.1.0]hexyl, an example of a fused C6 heterocyclic group; decahydroquinolinyl, an example of a fused C10 heterocyclic group), and bridged heterocyclic groups (e.g., 6-azabicyclo[3.1.1]heptyl and 2,5-diazabicyclo[2.2.1]heptane, both examples of bridged C7 heterocyclic groups; 3,8-diazabicyclo[3.2.1]octyl, Examples of bridged C8 heterocyclic groups include spirocyclic heterocyclic groups (2,6-diazaspiro[3.3]heptane, an example of a spirocyclic C7 heterocyclic group; 7-azaspiro[3.5]nonyl, an example of a spirocyclic C9 heterocyclic group; and 2,8-diazaspiro[4.5]decane, an example of a spirocyclic C10 heterocyclic group). Tetrahydropyran and pyrrolidine are examples of C3-7 heterocyclic groups. Furthermore, non-aromatic ring systems may optionally be fused with one or more aromatic rings, which may contain one or more heteroatoms (e.g., N, O, S, as the case may be) or only carbon atoms. For example, 4,5,6,7-tetrahydro-1H-pyrrolo[2,3-b]pyridin-5-yl is an example of a C9 heterocyclic group; and 1,2,3,4-tetrahydroisoquinoline-3-yl is an example of a C10 heterocyclic group. 2,3-Dihydro-1-benzofuran is an example of a C9 heterocyclic group in which the non-aromatic ring system is fused with an aromatic ring. 3,4-Dihydro-2H-1,4-benzoxazine and 2,3-Dihydro-1,4-benzodioxane are examples of C10 heterocyclic groups in which the non-aromatic ring system is fused with an aromatic ring. Some examples of “non-aromatic C3-7 heterocyclic groups” include oxobutane, piperidine, pyrrolidine, tetrahydrofuran, tetrahydropyran, pyrrolidine, morpholinyl, azabutane, and tetrahydrothiophene.

[0566] “Non-aromatic C3-11 heterocyclic group having at least one N ring atom and being connected by that N ring atom” comprises at least one non-aromatic ring system containing at least one nitrogen ring atom and being connected to the rest of the molecule by that ring nitrogen atom, and may optionally contain one or more additional heteroatoms (e.g., N, O, S, as appropriate). Furthermore, the non-aromatic ring system may optionally be fused with one or more aromatic rings, which may contain one or more heteroatoms (e.g., N, O, S, as appropriate) or only carbon atoms. In one embodiment, the term "having at least one N ring" is used."A non-aromatic C3-11 heterocyclic group with an N-ring atom" refers to a heterocyclic group connected by an N-ring atom, but it may have an additional N-ring atom. Examples include: azaheterocyclic, azaheterocyclic butyl, pyrrolidinyl, piperidinyl, piperazine, morpholinyl, thiomorpholinyl, azaheptanyl, and diazaheptanyl.

[0567] The term "carbocyclic" refers to a ring system containing at least one non-aromatic carbocyclic ring and containing only carbon atoms. Unless otherwise stated, "carbocyclic" includes monocyclic carbocyclic groups (e.g., cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl), bicyclic carbocyclic, and bicyclic carbocyclic groups. (See specification 24 / 530 pages 40 CN 121568936 A) Cyclocyclic groups (e.g., 2,3-dihydro-1H-indene), fused carbocyclic groups (e.g., 7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopentadien[a]phenanthrene, estradiol core skeleton), bridged carbocyclic groups (e.g., 1,2,3,4-tetrahydro-1,4-methylenenaphthalene), and spirocyclic carbocyclic groups (e.g., 3′,4′-dihydro-2′H-spiro[cyclopentane-1,1′-naphthalene]).

[0568] The term “haloalkyl” refers to an alkyl group substituted with one or more halogen groups (e.g., -F, -Cl, -Br, -I). The term “fluoroalkyl” refers to an alkyl group substituted with one or more -F groups. For example, -CF3 and -CHF2 are examples of C1 fluoroalkyl groups; -CH2CF3 and -CH2CHF2 are examples of C2 fluoroalkyl groups.

[0569] The term "C1-4 alkylene" refers to an alkyl group having two connection points. For example, -CH2- is an example of a C1 alkylene; -CH2CH2- and -CH(CH3)- are examples of C2 alkylene; -CH2CH2CH2- and -CH(CH3)2- are examples of C3 alkylene.

[0570] Examples of C1-7 alkyl, C1-6 alkyl, and C1-4 alkyl include methyl, ethyl, propyl, isopropyl, and butyl. Examples of C3-6 cycloalkyl include cyclopropyl and cyclohexyl. Examples of C3-6 cycloalkyl-C1-3 alkyl include cyclopropylmethyl and cyclohexylethyl. Examples of phenyl-C1-3 alkyl include benzyl and 2-phenylpropyl. Examples of C5-6 heteroaryl-C1-3 alkyl include pyrimidin-2-ylmethyl and thiazolyl-4-ylethyl. Examples of C2-6 alkenyl include vinyl and propenyl.

[0571] In the context of optional substituents (e.g., "one or more RAR1C groups"), the phrase "one or more groups" is necessarily limited by the body moiety and the number of suitable substitution positions thereon. In some body moiety (e.g., tetrazolium), only one position can be used for substitution. However, for other body moiety, there can be multiple positions (e.g., phenyl has five). In addition to being limited by the body moiety, "one or more groups" can be, for example, 1, 2, 3, 4, etc., but more preferably 1, 2, or 3.One, more preferably one or two, and even more preferably one.

[0572] The phrase “substituent on carbon” is intended to refer to a substituent attached to a carbon ring atom. Similarly, the phrase “substituent on secondary nitrogen” is intended to refer to a substituent attached to a nitrogen ring atom, in the absence of which the nitrogen ring atom would be a secondary nitrogen ring atom (i.e., -NH-). Thus, pyridyl can have only “substituent on carbon”, while 1H pyrrole can have both “substituent on carbon” and “substituent on secondary nitrogen”, as shown below.

[0573]

[0574] Similarly, piperidinyl can have only “substituent on carbon”, while piperazine can have both “substituent on carbon” and “substituent on secondary nitrogen”, as shown below.

[0575]

[0576] Some compounds, although containing a carbon ring atom, may not have any substituted carbon ring atoms. For example, in specification 25 / 530, page 41, CN 121568936 A, the tetrazolium group may only allow "substituents on carbon" or only "substituents on secondary nitrogen," as shown below.

[0577]

[0578] Unless otherwise stated, when a compound is shown or described as having one or more chiral centers and may have two or more stereoisomers, all such stereoisomers are disclosed and covered, including those existing alone (e.g., isolated from other stereoisomers) and those existing as mixtures (e.g., as equimolar or non-equimolar mixtures of two or more stereoisomers). For example, unless otherwise stated, when a compound has only one chiral center, each (R) and (S) enantiomer is disclosed and covered, including those existing alone (e.g., isolated from other enantiomers) and those existing as mixtures (e.g., as equimolar or non-equimolar mixtures of two or more enantiomers). For example, the initial carbon atom of the pendant sec-butyl-CH(CH3)CH2CH3 is usually chiral, thus producing stereoisomers, for example, if it is the only chiral center, then it has (R) and (S) enantiomers, both of which are disclosed and covered.

[0579] RA11 group

[0580] (3) The compound according to (1) or (2), wherein:

[0581] -RA11 is -RA111, -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A111, -OCF3 or -CN.

[0582] (4) The compound according to (1) or (2), wherein:

[0583] -RA11 is -RA111, -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A111 or -OCF3.

[0584] (5) The compound according to (1) or (2), wherein:

[0585] -RA11 is -RA111, -F, -Cl, -Br, -I, -CF3, -OH, -ORA111 or -OCF3.

[0586] (6) The compound according to (1) or (2), wherein:

[0587] -RA11 is -RA111, -F, -Cl, -Br, -I, -OH or -ORA111.

[0588] (7) The compound according to (1) or (2), wherein:

[0589] -RA11 is -RA111, -F, -Cl, -Br, -I or -OH.

[0590] (8) The compound according to (1) or (2), wherein:

[0591] -RA11 is -RA111, -F, -Cl or -OH.

[0592] (9) The compound according to (1) or (2), wherein:

[0593] -RA11 is -RA111, -F or -Cl.

[0594] (10) The compound according to (1) or (2), wherein:

[0595] -RA11 is -RA111.

[0596] (11) The compound according to (1) or (2), wherein:

[0597] -RA11 is -RA111, -F, -Cl or -Br.

[0598] (12) The compound according to (1) or (2), wherein:

[0599] -RA11 is -F.

[0600] (13) The compound according to (1) or (2), wherein: Specification 26 / 530 pages 42 CN 121568936 A

[0601] -RA11 is -Cl.

[0602] (14) The compound according to (1) or (2), wherein:

[0603] -RA11 is -Br.

[0604] (15) The compound according to (1) or (2), wherein:

[0605] -RA11 is -RA111 or -Br.

[0606] -RA111 group

[0607] (16) The compound according to any one of (1) to (15), wherein: -RA111 is -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[0608] (17) The compound according to any one of (1) to (15), wherein:

[0609] -RA111 is -Me, -Et, -nPr or -iPr.

[0610] (18) The compound according to any one of (1) to (15), wherein:

[0611] -RA111 is -Me or -Et.

[0612] (19) The compound according to any one of (1) to (15), wherein:

[0613] -RA111 is -Me.

[0614] (20) The compound according to any one of (1) to (15), wherein:

[0615] -RA111 is -Et.

[0616] -RA22 group

[0617] (21) The compound according to any one of (1) to (20), wherein:

[0618] -RA22 is -RA222, -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A222, -OCF3 or -CN.

[0619] (22) The compound according to any one of (1) to (20), wherein:

[0620] -RA22 is -RA222, -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A222 or -OCF3.

[0621] (23) The compound according to any one of (1) to (20), wherein:

[0622] -RA22 is -RA222, -F, -Cl, -Br, -I, -CF3, -OH, -OR A222 or -OCF3.

[0623] (24) The compound according to any one of (1) to (20), wherein:

[0624] -RA22 is -RA222, -F, -Cl, -Br, -I, -OH or -ORA222.

[0625] (25) The compound according to any one of (1) to (20), wherein:

[0626] -RA22 is -RA222, -F, -Cl, -Br, -I or -OH.

[0627] (26) The compound according to any one of (1) to (20), wherein:

[0628] -RA22 is -RA222, -F, -Cl or -OH.

[0629] (27) The compound according to any one of (1) to (20), wherein:

[0630] -RA22 is -RA222, -F or -Cl.

[0631] (28) The compound according to any one of (1) to (20), wherein:

[0632] -RA22 is -RA222.

[0633] (29) The compound according to any one of (1) to (20), wherein:

[0634] -RA22 is -Cl.

[0635] (30) The compound according to any one of (1) to (20), wherein:

[0636] -RA22 is -RA222, -F, -Cl or -Br.

[0637] (31) The compound according to any one of (1) to (20), wherein:

[0638] -RA22 is -F. Specification 27 / 530 pages 43 CN 121568936 A

[0639] (32) The compound according to any one of (1) to (20), wherein:

[0640] -RA22 is -Br.

[0641] -RA222 group

[0642] (33) The compound according to any one of (1) to (32), wherein:

[0643] Each -RA222, if present, is a straight-chain saturated C1-4 alkyl group.

[0644] (34) The compound according to any one of (1) to (32), wherein:

[0645] Each -RA222, if present, is -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[0646] (35) The compound according to any one of (1) to (32), wherein:

[0647] Each -RA222, if present, is -Me, -Et, -nPr or -iPr.

[0648] (36) The compound according to any one of (1) to (32), wherein:

[0649] Each -RA222, if present, is -Me or -Et.

[0650] (37) The compound according to any one of (1) to (32), wherein:

[0651] Each -RA222, if present, is -Me.

[0652] -RA3 group

[0653] (38) The compound according to any one of (1) to (37), wherein:

[0654] -RA3 is -H.

[0655] (39) The compound according to any one of (1) to (37), wherein: -RA3 is -RA33.

[0656] -RA33 group

[0657] (40) The compound according to any one of (1) to (37), wherein:

[0658] -RA33, if present, is:

[0659] -RA333, -F, -Cl, -Br, -I, -OH or -ORA333.

[0660] (41) The compound according to any one of (1) to (37), wherein:

[0661] -RA33, if present, is:

[0662] -RA333, -F, -Cl, -Br, -I or -OH.

[0663] (42) The compound according to any one of (1) to (37), wherein:

[0664] -RA33, if present, is:

[0665] -RA333, -F, -Cl or -OH.

[0666] (43) The compound according to any one of (1) to (37), wherein:

[0667] -RA33, if present, is:

[0668] -RA333, -F or -Cl.

[0669] (44) The compound according to any one of (1) to (37), wherein:

[0670] -RA33, if present, is:

[0671] -RA333.

[0672] (45) The compound according to any one of (1) to (37), wherein:

[0673] -RA33, if present, is:

[0674] -Cl.

[0675] (46) The compound according to any one of (1) to (37), wherein:

[0676] -RA33, if present, is:

[0677] -Br. Specification 28 / 530 page 44 CN 121568936 A

[0678] -RA333 group

[0679] (47) The compound according to any one of (1) to (37), wherein:

[0680] Each -RA333, if present, is -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[0681] (48) The compound according to any one of (1) to (37), wherein:

[0682] Each -RA333, if present, is -Me, -Et, -nPr or -iPr.

[0683] (49) The compound according to any one of (1) to (37), wherein:

[0684] Each -RA333, if present, is -Me or -Et.

[0685] (50) The compound according to any one of (1) to (37), wherein:

[0686] each -RA333, if present, is -Me.

[0687] -RA4 group

[0688] (51) The compound according to any one of (1) to (50), wherein:

[0689] -RA4 is -H.

[0690] (52) The compound according to any one of (1) to (50), wherein:

[0691] -RA4 is -RA44.

[0692] -RA44 group

[0693] (53) The compound according to any one of (1) to (52), wherein:

[0694] -RA44, if present, is:

[0695] -RA444, -F, -Cl, -Br, -I, -OH or -ORA444.

[0696] (54) The compound according to any one of (1) to (52), wherein:

[0697] -RA44, if present, is:

[0698] -RA444, -F, -Cl, -Br, -I or -OH.

[0699] (55) The compound according to any one of (1) to (52), wherein: -RA44, if present, is:

[0700] -RA444, -F, -Cl or -OH.

[0701] (56) The compound according to any one of (1) to (52), wherein:

[0702] -RA44, if present, is:

[0703] -RA444, -F or -Cl.

[0704] (57) The compound according to any one of (1) to (52), wherein:

[0705] -RA44, if present, is:

[0706] -RA444.

[0707] (58) The compound according to any one of (1) to (52), wherein:

[0708] -RA44, if present, is:

[0709] -Cl.

[0710] (59) The compound according to any one of (1) to (52), wherein:

[0711] -RA44, if present, is:

[0712] -RA444, -Cl or -Br.

[0713] -RA444 group

[0714] (60) The compound according to any one of (1) to (59), wherein:

[0715] Each -RA444, if present, is a straight-chain saturated C1-4 alkyl group.

[0716] (61) The compound according to any one of (1) to (59), wherein: Specification 29 / 530 pages 45 CN 121568936 A

[0717] Each -RA444, if present, is -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[0718] (62) The compound according to any one of (1) to (59), wherein:

[0719] each -RA444, if present, is -Me, -Et, -nPr or -iPr.

[0720] (63) The compound according to any one of (1) to (59), wherein:

[0721] each -RA444, if present, is -Me or -Et.

[0722] (64) The compound according to any one of (1) to (59), wherein:

[0723] each -RA444, if present, is -Me.

[0724] Ring B

[0725] (65) The compound according to any one of (1) to (64), wherein:

[0726] Ring B is:

[0727]

[0728] (66) The compound according to any one of (1) to (64), wherein:

[0729] Ring B is:

[0730]

[0731] (67) The compound according to any one of (1) to (64), wherein:

[0732] Ring B is:

[0733] ​​

[0734] (68) The compound according to any one of (1) to (64), wherein:

[0735] Y1 is S, O, or NH if present;

[0736] Y2 is CH or N if present;

[0737] Y3 is N or CH if present;

[0738] Y4 is N or CH if present;

[0739] Y5 is S, O, or NH if present;

[0740] Y6 is N or CH if present;

[0741] Y7 is N or CH if present;

[0742] Y8 is N or CH if present; and

[0743] Y9 is S, O, or NH if present.

[0744] For example, ring B is selected from: Specification 30 / 530, page 46, CN 121568936 A

[0745]

[0746]

[0747] (69) The compound according to any one of (1) to (64), wherein:

[0748] Y1 is S if present;

[0749] Y2 is CH, CRY2 or N if present;

[0750] Y3 is N, CH or CRY3 if present;

[0751] Y4 is N, CH or CRY4 if present;

[0752] Y5 is S if present; Specification 31 / 530 Page 47 CN 121568936 A

[0753] Y6 is N, CH or CRY6 if present;

[0754] Y7 is N, CH or CRY7 if present;

[0755] Y8 is N, CH or CRY8 if present; and

[0756] Y9 is S if present.

[0757] (70) The compound according to any one of (1) to (64), wherein:

[0758] Y1 is S if present;

[0759] Y2 is CH or N if present;

[0760] Y3 is N or CH if present;

[0761] Y4 is N or CH if present;

[0762] Y5 is S if present;

[0763] Y6 is N or CH if present;

[0764] Y7 is N or CH if present;

[0765] Y8 is N or CH if present; and

[0766] Y9 is S if present.

[0767] (71) The compound according to any one of (1) to (64), wherein:

[0768] Y1 is S if present;

[0769] Y2 is CH, CRY2 or N if present;

[0770] Y3 is N, CH or CRY3 if present;

[0771] wherein exactly one of Y2 and Y3 is N;

[0772] Y4 is N, CH or CRY4 if present;

[0773] Y5 is S if present;

[0774] Y6 is N, CH or CRY6 if present;

[0775] wherein exactly one of Y4 and Y6 is N;

[0776] Y7 is N, CH or CRY7 if present;

[0777] Y8 is N, CH or CRY8 if present;

[0778] Y9 is S if present; and

[0779] wherein exactly one of Y7 and Y8 is N.

[0780] (72) The compound according to any one of (1) to (64), wherein ring B is:

[0781]

[0782] (73) The compound according to any one of (1) to (64), wherein:

[0783] Y1 is S if present;

[0784] Y2 is CH, CRY2 or N if present;

[0785] Y3 is N, CH or CRY3 if present;

[0786] Among them, exactly one of Y2 and Y3 is N; Specification 32 / 530 page 48 CN 121568936 A

[0787] Y4 is N if it exists;

[0788] Y5 is S if it exists;

[0789] Y6 is CH or CRY6 if it exists;

[0790] Y7 is N if it exists;

[0791] Y8 is CH or CRY8 if it exists; and

[0792] Y9 is S if it exists.

[0793] (74) The compound according to any one of (1) to (64), wherein ring B is:

[0794]

[0795] (75) The compound according to any one of (1) to (64), wherein:

[0796] Y1 is S if present;

[0797] Y2 is CH, CRY2 or N if present;

[0798] Y3 is N, CH or CRY3 if present; and

[0799] wherein exactly one of Y2 and Y3 is N.

[0800] (76) The compound according to any one of (1) to (64), wherein ring B is:

[0801]

[0802] (77) The compound according to any one of (1) to (64), wherein:

[0803] Y1 is S if present;

[0804] Y2 is CH or CRY2 if present;

[0805] Y3 is N if present.

[0806] (78) The compound according to any one of (1) to (64), wherein ring B is:

[0807]

[0808] (79) The compound according to any one of (1) to (64), wherein:

[0809] Ring B is:

[0810]

[0811] wherein:

[0812] Y1 is S or O;

[0813] Y2 is CH, CRY2 or N;

[0814] Y3 is N. Specification 33 / 530 Page 49 CN 121568936 A

[0815] (80) The compound according to any one of (1) to (64), wherein:

[0816] Ring B is:

[0817]

[0818] wherein:

[0819] Y1 is S or O;

[0820] Y2 is CH or N;

[0821] Y3 is N.

[0822] -RY2, -RY3 and other groups

[0823] (81) A compound according to any one of (1) to (80), wherein:

[0824] Each of -RY2, -RY3, -RY4, -RY6, -RY7 and -RY8, if present, is independently:

[0825] -F, -Cl, -Br, -I, -RYY, -CF3, -OH, -ORYY, -OCF3 or -NH2.

[0826] (82) The compound according to any one of (1) to (80), wherein:

[0827] each of -RY2, -RY3, -RY4, -RY6, -RY7 and -RY8, if present, is independently:

[0828] -F, -Cl, -Br, -I, -RYY or -NH2.

[0829] (83) The compound according to any one of (1) to (80), wherein:

[0830] each of -RY2, -RY3, -RY4, -RY6, -RY7 and -RY8, if present, is independently:

[0831] -F, -Cl, -RYY or -NH2.

[0832] (84) The compound according to any one of (1) to (80), wherein:

[0833] each of -RY2, -RY3, -RY4, -RY6, -RY7 and -RY8, if present, is independently:

[0834] -H.

[0835] (85) The compound according to any one of (1) to (80), wherein:

[0836] each of -RY2, -RY3, -RY4, -RY6, -RY7 and -RY8, if present, is independently:

[0837] -F, -Cl or -RYY.

[0838] (86) The compound according to any one of (1) to (80), wherein:

[0839] each of -RY2 is -NH2.

[0840] -RYY group

[0841] (87) The compound according to any one of (1) to (86), wherein:

[0842] each of -RYY, if present, is:

[0843] -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[0844] (88) The compound according to any one of (1) to (86), wherein:

[0845] each -RYY, if present, is:

[0846] -Me, -Et, -nPr or -iPr.

[0847] (89) The compound according to any one of (1) to (86), wherein:

[0848] each -RYY, if present, is:

[0849] -Me or -Et.

[0850] (90) The compound according to any one of (1) to (86), wherein:

[0851] each -RYY, if present, is: Specification 34 / 530 pages 50 CN 121568936 A

[0852] -Me.

[0853] -RY1, -RY5 and -RY9 groups

[0854] (91) The compound according to any one of (1) to (90), wherein:

[0855] Each -RY1, -RY5 and -RY9, if present, is independently:

[0856] -RYYN or -C(=O)RYYN.

[0857] (92) The compound according to any one of (1) to (90), wherein:

[0858] each of -RY1, -RY5 and -RY9, if present, is independently:

[0859] -RYYN.

[0860] -RYYN group

[0861] (93) The compound according to any one of (1) to (92), wherein:

[0862] each of -RYYN, if present, is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, wherein each phenyl is optionally substituted by one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[0863] (94) The compound according to any one of (1) to (92), wherein:

[0864] each -RYYN, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-, wherein each phenyl is optionally substituted by one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[0865] (95) The compound according to any one of (1) to (92), wherein:

[0866] each -RYYN, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or benzyl.

[0867] (96) The compound according to any one of (1) to (92), wherein:

[0868] each -RYYN, if present, is independently a straight-chain or branched saturated C1-4 alkyl.

[0869] (97) The compound according to any one of (1) to (92), wherein:

[0870] each -RYYN is -Me if present.

[0871] -Q group

[0872] (98) The compound according to any one of (1) to (97), wherein:

[0873] -Q is -Q1, -LQ1-Q1, -Q2, -LQ2-Q2, -Q3, -LQ3-Q3, -Q4, -LQ4-Q4 or -Q5.

[0874] (99) The compound according to any one of (1) to (97), wherein:

[0875] -Q is -Q1, -LQ1-Q1, -Q2 or -LQ2-Q2.

[0876] (100) The compound according to any one of (1) to (97), wherein:

[0877] -Q is -Q1 or -LQ2-Q2.

[0878] (101) The compound according to any one of (1) to (97), wherein:

[0879] -Q is -Q1.

[0880] (102) The compound according to any one of (1) to (97), wherein:

[0881] -Q is -LQ1-Q1.

[0882] (103) The compound according to any one of (1) to (97), wherein:

[0883] -Q is -Q2.

[0884] (104) (84) The compound according to any one of (1) to (97), wherein:

[0885] -Q is -LQ2-Q2.

[0886] (105) The compound according to any one of (1) to (97), wherein: Specification 35 / 530 pages 51 CN 121568936 A

[0887] -Q is -Q3.

[0888] (106) The compound according to any one of (1) to (97), wherein:

[0889] -Q is -LQ3-Q3.

[0890] (107) The compound according to any one of (1) to (97), wherein:

[0891] -Q is -Q4.

[0892] (108) The compound according to any one of (1) to (97), wherein:

[0893] -Q is -LQ4-Q4.

[0894] (109) The compound according to any one of (1) to (97), wherein:

[0895] -Q is -Q5.

[0896] (110) The compound according to any one of (1) to (97), wherein:

[0897] -Q is -H.

[0898] -Q1 group

[0899] (111) The compound according to any one of (1) to (110), wherein:

[0900] -Q1 is a C5-9 heteroaryl if present;

[0901] and:

[0902] The carbon atom is optionally substituted by one or more -RQ1C groups; and

[0903] The secondary nitrogen atom, if present, is optionally substituted by a -RQ1N group.

[0904] (112) The compound according to any one of (1) to (110), wherein:

[0905] -Q1 is a C5-6 heteroaryl if present;

[0906] and:

[0907] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[0908] the secondary nitrogen atom is optionally substituted with a -RQ1N group if present.

[0909] (113) The compound according to any one of (1) to (110), wherein:

[0910] -Q1 is a C5 heteroaryl if present;

[0911] and:

[0912] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[0913] the secondary nitrogen atom is optionally substituted with a -RQ1N group if present.

[0914] (114) The compound according to any one of (1) to (110), wherein:

[0915] -Q1 is, if present, pyrazolyl, pyrroleyl, imidazolyl, triazolyl, tetrazolyl, furanyl, thiophene, oxoAzolium, isoxazolium, thiazolyl, isothiazolium, oxadiazolium, or thiadiazolium;

[0916] and:

[0917] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[0918] the secondary nitrogen atom, if present, is optionally substituted with a -RQ1N group.

[0919] (115) the compound according to any one of (1) to (110), wherein:

[0920] -Q1, if present, is pyrazolium, pyrroleium, imidazolyl, furanyl, oxazolium, isoxazolium, thiazolyl, isothiazolium, oxadiazolium, or thiadiazolium;

[0921] and:

[0922] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[0923] the secondary nitrogen atom, if present, is optionally substituted with a -RQ1N group. Specification 36 / 530 pages 52 CN 121568936 A

[0924] (116) The compound according to any one of (1) to (110), wherein:

[0925] -Q1, if present, is pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, oxadiazolyl or thiadiazolyl;

[0926] and:

[0927] the carbon atom is optionally substituted by one or more -RQ1C groups; and

[0928] the secondary nitrogen atom, if present, is optionally substituted by -RQ1N groups.

[0929] (117) The compound according to any one of (1) to (110), wherein:

[0930] -Q1 is a pyrazolyl group (e.g., 1H-pyrazol-3-yl, 1H-pyrazol-4-yl, 1H-pyrazol-5-yl or pyrazol-1-yl) if present;

[0931] and:

[0932] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[0933] the secondary nitrogen atom is optionally substituted with a -RQ1N group if present.

[0934]

[0935] (118) The compound according to any one of (1) to (110), wherein:

[0936] -Q1 is a pyrazol-1-yl group if present;

[0937] and the carbon atom is optionally substituted with one or more -RQ1C groups.

[0938] (119) The compound according to any one of (1) to (110), wherein:

[0939] -Q1, if present, is 1H-pyrazole-3-yl;

[0940] and:

[0941] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[0942] the secondary nitrogen atom is optionally substituted with -RQ1N groups.

[0943] (120) The compound according to any one of (1) to (110), wherein:

[0944] -Q1, if present, is 1H-pyrazole-4-yl;

[0945] and:

[0946] The carbon atom is optionally substituted with one or more -RQ1C groups; and

[0947] the secondary nitrogen atom is optionally substituted with a -RQ1N group.

[0948] (121) The compound according to any one of (1) to (110), wherein:

[0949] -Q1 is 1H-pyrazole-5-yl if present;

[0950] and:

[0951] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[0952] the secondary nitrogen atom is optionally substituted with a -RQ1N group.

[0953] (122) The compound according to any one of (1) to (110), wherein:

[0954] -Q1 is a C9 heteroaryl if present;

[0955] and:

[0956] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[0957] the secondary nitrogen atom, if present, is optionally substituted with a -RQ1N group.

[0958] (123) The compound according to any one of (1) to (81105), wherein: Specification 37 / 530 pages 53 CN 121568936 A

[0959] -Q1 is a C9 heteroaryl if present;

[0960] wherein the C9 heteroaryl is a 5:6 fused heteroaryl;

[0961] and:

[0962] the carbon atom is optionally substituted by one or more -RQ1C groups; and

[0963] the secondary nitrogen atom, if present, is optionally substituted by a -RQ1N group.

[0964] (124) The compound according to any one of (1) to (110), wherein:

[0965] -Q1 is, if present, indole, inzolyl, benzimidazolyl, benzoxazolyl, pyrazolopyridyl, pyrazolopyrimidinyl, imidazopyridyl, or pyrrolopyridyl;

[0966] and:

[0967] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[0968] the secondary nitrogen atom is optionally substituted with -RQ1N groups.

[0969] (125) The compound according to any one of (1) to (110), wherein:

[0970] -Q1 is indole-2-yl or indole-3-yl if present;

[0971] and:

[0972] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[0973] the secondary nitrogen atom is optionally substituted with a -RQ1N group.

[0974]

[0975] (126) The compound according to any one of (1) to (110), wherein:

[0976] -Q1 is 2H-indazole-3-yl or 1H-indazole-3-yl if present;

[0977] and:

[0978] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[0979] the secondary nitrogen atom is optionally substituted with a -RQ1N group.

[0980]

[0981] (127) The compound according to any one of (1) to (110), wherein:

[0982] -Q1 is benzimidazole-2-yl if present;

[0983] and:

[0984] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[0985] the secondary nitrogen atom is optionally substituted with -RQ1N groups.

[0986] Specification 38 / 530 pages 54 CN 121568936 A

[0987] (128) The compound according to any one of (1) to (110), wherein:

[0988] -Q1 is benzimidazole-2-yl if present;

[0989] and:

[0990] the carbon atom is optionally substituted with one or more -RQ1C groups.

[0991]

[0992] (129) The compound according to any one of (1) to (110), wherein:

[0993] -Q1 is pyrazolo[1,5-a]pyridin-2-yl or pyrazolo[1,5-a]pyridin-3-yl if present;

[0994] and:

[0995] the carbon atom is optionally substituted by one or more -RQ1C groups.

[0996]

[0997] (130) The compound according to any one of (1) to (110), wherein:

[0998] -Q1, if present, is 1H-pyrazolo[3,4-b]pyridin-3-yl, 1H-pyrazolo[3,4-c]pyridin-3-yl, 1H-pyrazolo[4,3-c]pyridin-3-yl or 1H-pyrazolo[4,3-b]pyridin-3-yl;

[0999] and:

[1000] The carbon atom is optionally substituted with one or more -RQ1C groups; and

[1001] The secondary nitrogen atom is optionally substituted with -RQ1N groups.

[1002]

[1003] (131) The compound according to any one of (1) to (110), wherein:

[1004] -Q1 is imidazo[1,2-a]pyridin-2-yl or imidazo[1,2-a]pyridin-3-yl if present;

[1005] and:

[1006] the carbon atom is optionally substituted by one or more -RQ1C groups.

[1007]

[1008] (132) The compound according to any one of (1) to (110), wherein:

[1009] -Q1, if present, is 1H-pyrrolo[3,2-b]pyridin-2-yl or 1H-pyrrolo[3,2-b]pyridin-3-yl;

[1010] and:

[1011] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[1012] the secondary nitrogen atom is optionally substituted with -RQ1N groups.

[1013]

[1014] (133) The compound according to any one of (1) to (110), wherein:

[1015] -Q1 is 1H-pyrrolo[3,2-c]pyridin-2-yl or 1H-pyrrolo[3,2-c]pyridin-3-yl if present;

[1016] and:

[1017] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[1018] the secondary nitrogen atom is optionally substituted with -RQ1N groups.

[1019]

[1020] (134) The compound according to any one of (1) to (110), wherein:

[1021] -Q1 is 1H-pyrrolo[2,3-c]pyridin-2-yl or 1H-pyrrolo[2,3-c]pyridin-3-yl if present;

[1022] and:

[1023] the carbon atom is optionally substituted with one or more -RQ1C groups; and

[1024] the secondary nitrogen atom is optionally substituted with -RQ1N groups.

[1025]

[1026] (135) The compound according to any one of (1) to (110), wherein:

[1027] -Q1, if present, is pyrazolo[1,5-c]pyrimidin-2-yl, pyrazolo[1,5-c]pyrimidin-3-yl, pyrazolo[1,5-a]pyrimidin-2-yl or pyrazolo[1,5-a]pyrimidin-3-yl;

[1028] and:

[1029] The carbon atom is optionally substituted by one or more -RQ1C groups. Specification 40 / 530 pages 56 CN 121568936 A

[1030]

[1031] (136) the compound according to any one of (1) to (110), wherein:

[1032] -Q1 is, if present, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, thiophene, 1,3,4-oxadiazolyl, 1,2,4-oxadiazolyl, 1,3,4-thiadiazolyl, 6,7-dihydro-4H-pyrano[4,3-d]thiazolyl, imidazolyl, 1,3-benzoxazolyl, pyrazolo[1,5-a]pyridyl, indazole, pyrazolo[4,3-b]pyridyl, pyrimidinyl, pyrazolo[3,4-b]pyridyl, pyrazolo[3,4-c]pyridyl, 4,5,6,7-tetrahydro-1H-indazole, 1,4,5,6-tetrahydrocyclopentano[c]pyrazolyl, Pyrazolo[4,3-c]pyridyl, 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazinyl, 1,2,4-triazolyl, pyridyl, pyrimidinyl, quinolinyl, isoquinolinyl, quinazolinyl, 1,8-naphthidyl, pyridazinyl, indoleyl, 7H-pyrrolo[2,3-d]pyrimidinyl, 1,3-benzothiazolyl, thieno[2,3-d]pyrimidinyl, pyrrolo[2,1-f][1,2,4]triazinyl, benzofuranyl, 1,5-naphthidyl, 1,7-naphthidyl, 2,7-naphthidyl or 1,6-naphthidyl;

[1033] and:

[1034] The carbon atom is optionally substituted with one or more -RQ1C groups; and

[1035] The secondary nitrogen atom, if present, is optionally substituted with one or more -RQ1N groups.

[1036] -LQ1- group

[1037] (137) The compound according to any one of (1) to (136), wherein:

[1038] -LQ1- is -CH2-, -C(CH3)2-, -CH2CH2- or -CH2CH2CH2- if present.

[1039] (138) The compound according to any one of (1) to (136), wherein:

[1040] -LQ1- is -CH2-, -CH2CH2- or -CH2CH2CH2- if present.

[1041] (139) The compound according to any one of (1) to (136), wherein:

[1042] -LQ1- is -CH2- if present.

[1043] (140) The compound according to any one of (1) to (136), wherein:

[1044] -LQ1- is -CH2CH2- if present.

[1045] (141) The compound according to any one of (1) to (136), wherein:

[1046] -LQ1- is -CH2CH2CH2- if present.

[1047] -Q2 group

[1048] (142) The compound according to any one of (1) to (141), wherein:

[1049] -Q2, if present, is aziridine, pyrrolidinyl, piperidinyl, piperazine, morpholinyl, thiomorpholinyl, aziridine-heptyl or diaziridine-heptyl;

[1050] and:

[1051] the sulfur atom, if present, is optionally substituted with one or two =O groups;

[1052] the carbon atom is optionally substituted with one or more -RQ2C groups; and

[1053] the secondary nitrogen atom, if present, is optionally substituted with one or more -RQ2N groups.

[1054] (143) The compound according to any one of (1) to (141), wherein:

[1055] -Q2, if present, is pyrrolidinyl, piperidinyl, piperazineyl, morpholinyl, or thiomorpholinyl;

[1056] and: Specification 41 / 530 pages 57 CN 121568936 A

[1057] Sulfur atom, if present, is optionally substituted by one or two =O groups;

[1058] Carbon atom is optionally substituted by one or more -RQ2C groups; and

[1059] Secondary nitrogen atom, if present, is optionally substituted by -RQ2N groups.

[1060] (144) The compound according to any one of (1) to (141), wherein:

[1061] -Q2, if present, is piperidinyl or piperazineyl;

[1062] and:

[1063] The carbon atom is optionally substituted with one or more -RQ2C groups; and

[1064] the secondary nitrogen atom, if present, is optionally substituted with a -RQ2N group.

[1065] (145) The compound according to any one of (1) to (141), wherein:

[1066] -Q2, if present, is piperidinyl (e.g., piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl);

[1067] and:

[1068] the carbon atom is optionally substituted with one or more -RQ2C groups; and

[1069] the secondary nitrogen atom, if present, is optionally substituted with a -RQ2N group.

[1070]

[1071] (146) The compound according to any one of (1) to (141), wherein:

[1072] -Q2 is piperidin-4-yl if present;

[1073] and:

[1074] the carbon atom is optionally substituted with one or more -RQ2C groups; and

[1075] the secondary nitrogen atom is optionally substituted with a -RQ2N group.

[1076] (147) The compound according to any one of (1) to (141), wherein:

[1077] -Q2 is piperazine (e.g., piperazine-1-yl, piperazine-2-yl) if present;

[1078] and:

[1079] the carbon atom is optionally substituted with one or more -RQ2C groups; and

[1080] the secondary nitrogen atom is optionally substituted with a -RQ2N group.

[1081]

[1082] (148) The compound according to any one of (1) to (141), wherein:

[1083] -Q2 is piperazine-1-yl if present;

[1084] and:

[1085] the carbon atom is optionally substituted with one or more -RQ2C groups; and

[1086] the secondary nitrogen atom is optionally substituted with -RQ2N groups. Specification 42 / 530 pages 58 CN 121568936 A

[1087]

[1088] (149) The compound according to any one of (1) to (141), wherein:

[1089] -Q2, if present, is pyrrolidinyl, morpholinyl, piperidinyl, thiomorpholinyl, piperazine, 2,3-dihydro-1,4-benzodioxane, 3,4-dihydro-2H-1,4-benzooxazine or 2,3-dihydro-1-benzofuranyl;

[1090] and:

[1091] a sulfur atom, if present, optionally substituted with one or two =O groups;

[1092] a secondary nitrogen atom, if present, optionally substituted with one or more -RQ2N groups.

[1093] -LQ2- group

[1094] (150) The compound according to any one of (1) to (149), wherein:

[1095] -LQ2- is -CH2-, -C(CH3)2-, -CH2CH2- or -CH2CH2CH2- if present.

[1096] (151) The compound according to any one of (1) to (149), wherein:

[1097] -LQ2- is -CH2-, -CH2CH2- or -CH2CH2CH2- if present.

[1098] (152) The compound according to any one of (1) to (149), wherein:

[1099] -LQ2- is -CH2- or -CH2CH2CH2- if present.

[1100] (153) The compound according to any one of (1) to (149), wherein:

[1101] -LQ2- is -CH2- if present.

[1102] (154) The compound according to any one of (1) to (149), wherein:

[1103] -LQ2- is -CH2CH2- if present.

[1104] (155) The compound according to any one of (1) to (149), wherein:

[1105] -LQ2- is -CH2CH2CH2- if present.

[1106] -Q3 group

[1107] (156) The compound according to any one of (1) to (155), wherein:

[1108] -Q3 is phenyl if present;

[1109] and optionally substituted with one or more -RQ3C groups.

[1110] (157) The compound according to any one of (1) to (155), wherein:

[1111] -Q3 is naphthyl if present;

[1112] and optionally substituted with one or more -RQ3C groups.

[1113] -LQ3- group

[1114] (158) The compound according to any one of (1) to (157), wherein:

[1115] -LQ3- is -CH2-, -C(CH3)2-, -CH2CH2- or -CH2CH2CH2- if present.

[1116] (159) The compound according to any one of (1) to (157), wherein:

[1117] -LQ3- is -CH2-, -CH2CH2- or -CH2CH2CH2- if present.

[1118] (160) The compound according to any one of (1) to (157), wherein:

[1119] -LQ3- is -CH2- or -CH2CH2- if present. Specification page 43 / 530 59 CN 121568936 A

[1120] (161) The compound according to any one of (1) to (157), wherein:

[1121] -LQ3- is -CH2- if present.

[1122] (162) The compound according to any one of (1) to (157), wherein:

[1123] -LQ3- is -CH2CH2- if present.

[1124] (163) The compound according to any one of (1) to (157), wherein:

[1125] -LQ3- is -CH2CH2CH2- if present.

[1126] -Q4 group

[1127] (164) The compound according to any one of (1) to (163), wherein:

[1128] -Q4 is cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl if present;

[1129] and optionally substituted by one or more -RQ4C groups.

[1130] (165) The compound according to any one of (1) to (163), wherein:

[1131] -Q4 is cyclopropyl if present;

[1132] and optionally substituted with one or more -RQ4C groups.

[1133] (166) The compound according to any one of (1) to (163), wherein:

[1134] -Q4 is cyclobutyl if present;

[1135] and optionally substituted with one or more -RQ4C groups.

[1136] (167) The compound according to any one of (1) to (163), wherein:

[1137] -Q4 is cyclopentyl if present;

[1138] and optionally substituted with one or more -RQ4C groups.

[1139] (168) The compound according to any one of (1) to (163), wherein:

[1140] -Q4 is cyclohexyl if present;

[1141] and optionally substituted with one or more -RQ4C groups.

[1142] (169) The compound according to any one of (1) to (163), wherein:

[1143] -Q4 is cyclopropyl or cyclohexyl if present;

[1144] and optionally substituted with one or more -RQ4C groups.

[1145] -LQ4- group

[1146] (170) The compound according to any one of (1) to (169), wherein:

[1147] -LQ4- is -CH2-, -C(CH3)2-, -CH2CH2- or -CH2CH2CH2- if present.

[1148] (171) The compound according to any one of (1) to (169), wherein:

[1149] -LQ4- is -CH2-, -CH2CH2- or -CH2CH2CH2- if present.

[1150] (172) The compound according to any one of (1) to (169), wherein:

[1151] -LQ4- is -CH2- if present.

[1152] (173) The compound according to any one of (1) to (169), wherein:

[1153] -LQ4- is -CH2CH2- if present.

[1154] (174) The compound according to any one of (1) to (169), wherein:

[1155] -LQ4- is -CH2CH2CH2- if present.

[1156] -Q5 group

[1157] (175) The compound according to any one of (1) to (174), wherein:

[1158] -Q5 is -Me, -Et, -nPr, -iPr, -nBu, -iBu, -sBu, -tBu, n-pentyl, isopentyl, neopentyl, n-hexyl, isohexyl or 3,3-dimethylbutyl if present;

[1159] and optionally substituted by one or more -RQ5C groups.

[1160] (176) The compound according to any one of (1) to (174), wherein:

[1161] -Q5, if present, is a straight-chain or branched saturated C1-4 alkyl group;

[1162] and optionally substituted with one or more -RQ5C groups.

[1163] (177) The compound according to any one of (1) to (174), wherein:

[1164] -Q5, if present, is -Me, -Et or -nPr;

[1165] and optionally substituted with one or more -RQ5C groups.

[1166] (178) The compound according to any one of (1) to (174), wherein:

[1167] -Q5, if present, is -CH2-RQ5C, -CH2CH2-RQ5C, or -CH2CH2CH2-RQ5C.

[1168] (179) The compound according to any one of (1) to (174), wherein:

[1169] -Q5 is -CH2-RQ5C if present.

[1170] (180) The compound according to any one of (1) to (174), wherein:

[1171] -Q5 is -CH2CH2-RQ5C if present.

[1172] (181) The compound according to any one of (1) to (174), wherein:

[1173] -Q5 is -CH2CH2CH2-RQ5C if present.

[1174] (182) The compound according to any one of (1) to (174), wherein:

[1175] -Q5 is -Me, -Et, -nPr or 3,3-dimethylbutyl if present.

[1176] And optionally substituted with one or more -RQ5C groups.

[1177] -RQ1C group

[1178] (183) The compound according to any one of (1) to (182), wherein:

[1179] Each -RQ1C, if present, is independently:

[1180] ‑F, ‑Cl, ‑Br, ‑I,

[1181] ‑RQ1CC,

[1182] ‑RQ1CX, ‑ORQ1CX,

[1183] ‑OH, ‑ORQ1CC,

[1184] ‑LQ1C‑OH, ‑LQ1C‑ORQ1CC,

[1185] ‑NH2, ‑NHR Q1CC, ‑NRQ1CC2, ‑R Q1CM,

[1186] -LQ1C-NH2, -L Q1C -NHRQ1CC, -LQ1C-NRQ1CC2, -L Q1C -RQ1CM,

[1187] -C(=O)NH2, -C(=O)NHRQ1CC, -C(=O)NRQ1CC2, -C(=O)RQ1CM,

[1188] -C(=O)OH or -C(=O)ORQ1CC,

[1189] -S(=O)2RQ1CC or -CN;

[1190] and two adjacent -RQ1C, if present, can together form -(CH2)n1-O-(CH2)m1- or -O-(CH2)p1-O-.

[1191] (184) The compound according to any one of (1) to (182), wherein:

[1192] each -RQ1C, if present, is independently:

[1193] -F, -Cl, -Br, -I,

[1194] -RQ1CC,

[1195] -RQ1CX, -ORQ1CX,

[1196] -OH, -ORQ1CC,

[1197] -NH2, -NHRQ1CC, -NRQ1CC2, -RQ1CM,

[1198] -C(=O)NH2, -C(=O)NHRQ1CC, -C(=O)NRQ1CC2, -C(=O)RQ1CM,

[1199] -C(=O)OH or -C(=O)ORQ1CC.

[1200] (185) The compound according to any one of (1) to (182), wherein:

[1201] each -RQ1C, if present, is independently:

[1202] -RQ1CC,

[1203] -RQ1CX,

[1204] -NH2, -MHRQ1CC, -NRQ1CC2, -RQ1CM,

[1205] -C(=O)NH2, -C(=O)NHRQ1CC, -C(=O)NRQ1CC2, -C(=O)RQ1CM,

[1206] -C(=O)OH or -C(=O)ORQ1CC.

[1207] (186) The compound according to any one of (1) to (182), wherein:

[1208] each -RQ1C, if present, is independently:

[1209] -RQ1CC,

[1210] -RQ1CX, or

[1211] -C(=O)ORQ1CC.

[1212] (187) The compound according to any one of (1) to (182), wherein:

[1213] each -RQ1C is:

[1214] -RQ1CC if present.

[1215] (188) The compound according to any one of (1) to (182), wherein:

[1216] each -RQ1C, if present, is independently:

[1217] -F, -Cl, -Br,

[1218] -RQ1CC,

[1219] -RQ1CX, -ORQ1CX,

[1220] -OH, -ORQ1CC,

[1221] -NH2, -NHRQ1CC, -NRQ1CC2, -RQ1CM,

[1222] -LQ1C-RQ1CM,

[1223] -NHC(=O)RQ1CC, -N(RQ1CC)C(=O)RQ1CC, -NHC(=O)ORQ1CC,

[1224] ‑C(=O)NH2、‑C(=O)NHRQ1CC、‑C(=O)NRQ1CC2、‑C(=O)RQ1CM、=O,

[1225] ‑NHC(=O)NHRQ1CC、

[1226] ‑LQ1C‑C(=O)NRQ1CC2

[1227] ‑C(=O)OH、‑C(=O)ORQ1CC、

[1228] -OC(=O)NH2,

[1229] -S(=O)2R Q1CX,

[1230] -S(=O)2R Q1CM,

[1231] -NHS(=O)RQ1CC, -NHS(=O)2R Q1CC,

[1232] -CN or -C≡CH.

[1233] (189) The compound according to any one of (1) to (182), wherein:

[1234] each -RQ1C, if present, is independently: Specification 46 / 530 pages 62 CN 121568936 A

[1235] -F, -Cl,

[1236] -RQ1CC,

[1237] -RQ1CX,

[1238] -ORQ1CC,

[1239] -NRQ1CC2, -R Q1CM,

[1240] -NHC(=O)RQ1CC, or

[1241] -LQ1C-C(=O)NRQ1CC2.

[1242] -RQ1CC group

[1243] (190) The compound according to any one of (1) to (189), wherein:

[1244] Each -RQ1CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, or C3-6 cycloalkane.alkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, wherein each phenyl group is optionally substituted with one or more groups selected from the group consisting of: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[1245] (191) The compound according to any one of (1) to (189), wherein:

[1246] each -RQ1CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl or phenyl-CH2-, wherein each phenyl group is optionally substituted with one or more groups selected from the group consisting of: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[1247] (192) The compound according to any one of (1) to (189), wherein:

[1248] each -RQ1CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or benzyl.

[1249] (193) The compound according to any one of (1) to (189), wherein:

[1250] each -RQ1CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl.

[1251] (194) The compound according to any one of (1) to (189), wherein:

[1252] each -RQ1CC, if present, is independently -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[1253] (195) The compound according to any one of (1) to (189), wherein:

[1254] each -RQ1CC, if present, is independently -Me, -Et, -nPr or -iPr.

[1255] (196) The compound according to any one of (1) to (189), wherein:

[1256] each -RQ1CC, if present, is independently -Me or -Et.

[1257] (197) The compound according to any one of (1) to (189), wherein:

[1258] each -RQ1CC, if present, is -Me.

[1259] (198) The compound according to any one of (1) to (189), wherein:

[1260] each -RQ1CC, if present, is independently a straight-chain or branched saturated C1-6 alkyl, C2-6 alkylene, C3-6 cycloalkyl, C3-7 heterocyclic, phenyl, or Cs-6 heteroaryl group, wherein the C1-6 alkyl group is optionally substituted with -OH, -CN, or -OCH3, and each phenyl and heteroaryl group is optionally substituted with one or more groups selected from the group consisting of -F, -Cl, -CH3, -CHF2, -CF3, and -OCH3.

[1261] (199) The compound according to any one of (1) to (189), wherein:

[1262] Each -RQ1CC, if present, is independently -Me, -Et, -iPr, -iBu, -t-Bu, -heptyl, C2-6 alkylene, cyclopropyl, tetrahydropyran, phenyl, or pyrazolyl, pyrimidinyl, wherein -Me, -Et, -iPr, -iBu, -t-Bu or -heptyl is optionally substituted with -OH, -CN or -OCH3, and each phenyl, pyrazolyl and pyrimidinyl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CHF2, -CF3 and -OCH3.

[1263] (200) The compound according to any one of (1) to (189), wherein:

[1264] each -RQ1CC, if present, is independently a straight-chain C1-6 alkyl, C3-6 cycloalkyl, phenyl or C5-6 heteroaryl, wherein each cycloalkyl, phenyl and heteroaryl in the specification 47 / 530 pages 63 CN 121568936 A is optionally substituted by one or more groups selected from the group consisting of -F, -Cl, -C1-4 alkyl, -CHF2, -CF3 and -OCH3.

[1265] The indices “n1” and “m1” in -(CH2)n1-O-(CH2)m1-

[1266] (201) The compound according to any one of (1) to (200), wherein:

[1267] n1 is 0, 1, 2 or 3 if present;

[1268] m1 is 0, 1, 2 or 3 if present;

[1269] provided that m1+n1 is 2 or 3.

[1270] (202) The compound according to any one of (1) to (200), wherein:

[1271] n1 is 0, 1 or 2 if present;

[1272] m1 is 0, 1 or 2 if present;

[1273] provided that m1+n1 is 2 or 3.

[1274] (203) The compound according to any one of (1) to (200), wherein:

[1275] n1 is 1 or 2 if present;

[1276] m1 is 1 or 2 if present;

[1277] provided that m1+n1 is 2 or 3.

[1278] The index “p1” in -O-(CH2)p1-O-

[1279] (204) The compound according to any one of (1) to (203), wherein:

[1280] p1 is 1 if present.

[1281] (205) The compound according to any one of (1) to (203), wherein:

[1282] p1 is 2 if present.

[1283] -RQ1CX group

[1284] (206) The compound according to any one of (1) to (203), wherein:

[1285] each -RQ1CX, if present, is independently a straight-chain or branched saturated C1-4 fluoroalkyl group.

[1286] (207) The compound according to any one of (1) to (203), wherein:

[1287] each -RQ1CX, if present, is independently -CF3, -CHF2, -CH2CF3 or -CH2CHF2.

[1288] (208) The compound according to any one of (1) to (203), wherein:

[1289] each -RQ1CX, if present, is -CF3.

[1290] (209) The compound according to any one of (1) to (203), wherein:

[1291] each -RQ1CX, if present, is independently -CF3 or -CH2CF3.

[1292] -LQ1C- group

[1293] (210) The compound according to any one of (1) to (209), wherein:

[1294] Each -LQ1C- is independently -CH2-, -C(CH3)2-, -CH2CH2- or -CH2CH2CH2- if present.

[1295] (211) The compound according to any one of (1) to (209), wherein:

[1296] Each -LQ1C- is independently -CH2-, -CH2CH2- or -CH2CH2CH2- if present.

[1297] (212) The compound according to any one of (1) to (209), wherein:

[1298] Each -LQ1C- is -CH2- if present.

[1299] (213) The compound according to any one of (1) to (209), wherein:

[1300] each -LQ1C- is -CH2CH2- if present.

[1301] (214) The compound according to any one of (1) to (209), wherein: Specification 48 / 530 pages 64 CN 121568936 A

[1302] each -LQ1C- is -CH2CH2CH2- if present.

[1303] -RQ1CM group

[1304] (215) The compound according to any one of (1) to (214), wherein:

[1305] each -RQ1CM, if present, is independently an azircyclic butyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, azircyclic heptyl or diazircyclic heptyl, and:

[1306] the carbon atom is optionally substituted by one or more -RQ1CMM groups; and

[1307] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ1CMM, -C(=O)RQ1CMM, -C(=O)ORQ1CMM, -C(=O)NH2, -C(=O)NHRQ1CMM, -C(=O)NRQ1CMM2 and -S(=O)2RQ1CMM.

[1308] (216) The compound according to any one of (1) to (214), wherein:

[1309] each -RQ1CM is independently pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl if present, and:

[1310] the carbon atom is optionally substituted by one or more -RQ1CMM groups; and

[1311] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ1CMM, -C(=O)RQ1CMM, -C(=O)ORQ1CMM, -C(=O)NH2, -C(=O)NHRQ1CMM, -C(=O)NRQ1CMM2 and -S(=O)2RQ1CMM.

[1312] (217) The compound according to any one of (1) to (214), wherein:

[1313] each -RQ1CM is independently pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl if present, and:

[1314] the carbon atom is optionally substituted by one or more -RQ1CMM groups; and

[1315] the secondary nitrogen atom, if present, is optionally substituted by a group selected from -RQ1CMM, -C(=O)RQ1CMM and -C(=O)ORQ1CMM.

[1316] (218) The compound according to any one of (1) to (214), wherein:

[1317] each -RQ1CM, if present, is independently a non-aromatic C3-11 heterocyclic group having at least one N ring atom and connected by the N ring atom, and:

[1318] the carbon atom is optionally substituted by one or more -RQ1CMM groups; and

[1319] the secondary nitrogen atom, if present, is optionally substituted by a group selected from -RQ1CMM.

[1320] (219) The compound according to any one of (1) to (214), wherein:

[1321] each -RQ1CM, if present, is independently piperazine, piperidinyl, pyrrolidinyl, or morpholinyl linked by an N-ring atom; and:

[1322] the carbon atom is optionally substituted by one or more -RQ1CMM groups; and

[1323] the secondary nitrogen atom, if present, is optionally substituted by a group selected from -RQ1CMM.

[1324] (220) The compound according to any one of (1) to (214), wherein:

[1325] each -RQ1CM, if present, has its secondary nitrogen atom, if present, optionally substituted by a group selected from -RQ1CMM.

[1326] -RQ1CMM group

[1327] (221) The compound according to any one of (1) to (220), wherein:

[1328] Each -RQ1CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, or C3-6 cycloalkyl group.C1-3 alkyl, phenyl or phenyl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl or phenyl is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[1329] (222) The compound according to any one of (1) to (220), wherein:

[1330] each -RQ1CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl or phenyl-C1-3 alkyl, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3, and each cycloalkyl and phenyl is optionally substituted with one or more groups selected from the group consisting of -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[1331] (223) The compound according to any one of (1) to (220), wherein:

[1332] each -RQ1CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-, wherein the C1-4 alkyl is optionally substituted with -OH or -OCH3.

[1333] (224) The compound according to any one of (1) to (220), wherein:

[1334] each -RQ1CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or benzyl.

[1335] (225) The compound according to any one of (1) to (220), wherein:

[1336] each -RQ1CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, and is optionally substituted with -OH or -OCH3.

[1337] (226) The compound according to any one of (1) to (220), wherein:

[1338] each -RQ1CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl group.

[1339] (227) The compound according to any one of (1) to (220), wherein:

[1340] each -RQ1CMM, if present, is independently -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[1341] (228) The compound according to any one of (1) to (220), wherein:

[1342] each -RQ1CMM, if present, is independently -Me, -Et, -nPr or -iPr.

[1343] (229) The compound according to any one of (1) to (220), wherein:

[1344] each -RQ1CMM, if present, is independently -Me or -Et.

[1345] (230) The compound according to any one of (1) to (220), wherein:

[1346] each -RQ1CMM is -Me if present.

[1347] (231) The compound according to any one of (1) to (220), wherein:

[1348] each -RQ1CMM is independently -F, -NH2, straight-chain saturated C1-4 alkyl, C1-4 alkylOC(=O)NH- or C3-6 cycloalkyl, wherein the C1-4 alkyl is optionally substituted with -OH.

[1349] (232) The compound according to any one of (1) to (220), wherein:

[1350] each -RQ1CMM is independently -F, -NH2, -Me, -Et, EtOC(=O)NH- or cyclopropyl, wherein -Me or -Et is optionally substituted with -OH.

[1351] (233) The compound according to any one of (1) to (220), wherein:

[1352] each -RQ1CMM is independently -F, or straight-chain or branched saturated C1-4 alkyl, if present.

[1353] -RQ1N group

[1354] (234) The compound according to any one of (1) to (233), wherein:

[1355] Each -RQ1N, if present, is independently:

[1356] -RQ1NC,

[1357] -RQ1NX,

[1358] -RQ1Nhet, -LQ1N-RQ1Nhet,

[1359] -LQ1N-OH, -LQ1N-ORQ1NC,

[1360] -LQ1N-C(=O)OH, -LQ1N-C(=O)ORQ1NC,

[1361] -LQ1N-C(=O)NH2, -LQ1N-C(O)NHRQ1NK, -LQ1N-C(=O)NRQ1NC2, -LQ1N -C(=O)RQ1NP,

[1362] -LQ1N-NH2, -LQ1N-NHRQ1NC, -LQ1N-NRQ1NC2, -LQ1N-RQ1NM,

[1363] -LQ1N-NHC(=O)ORQ1NC. Specification 50 / 530 pages 66 CN 121568936 A

[1364] (235) The compound according to any one of (1) to (233), wherein:

[1365] Each -RQ1N, if present, is independently:

[1366] -RQ1NC,

[1367] -LQ1N-C(=O)NRQ1NC2 or -LQ1N-C(=O)RQ1NP.

[1368] (236) The compound according to any one of (1) to (233), wherein:

[1369] each -RQ1N, if present, is independently:

[1370] -RQ1Nhet or -LQ1N-RQ1Nhet.

[1371] (237) The compound according to any one of (1) to (233), wherein:

[1372] each -RQ1N, if present, is:

[1373] -RQ1Nhet.

[1374] (238) The compound according to any one of (1) to (233), wherein:

[1375] each -RQ1N, if present, is:

[1376] -LQ1N-C(=O)NH2, -LQ1N-C(=O)NHRQ1NK, -LQ1N-C(=O)NRQ1NC2 or -LQ1N-C(=O)RQ1NP.

[1377] (239) The compound according to any one of (1) to (233), wherein:

[1378] each -RQ1N, if present, is:

[1379] -LQ1N-C(=O)NHRQ1NK, -LQ1N-C(=O)NRQ1NC2 or -LQ1N-C(=O)RQ1NP.

[1380] (240) The compound according to any one of (1) to (233), wherein:

[1381] each -RQ1N, if present, is:

[1382] -LQ1N-C(=O)NHRQ1NK.

[1383] (241) The compound according to any one of (1) to (233), wherein:

[1384] each -RQ1N, if present, is:

[1385] -LQ1N-C(=O)RQ1NP.

[1386] (242) The compound according to any one of (1) to (233), wherein:

[1387] each -RQ1N, if present, is:

[1388] -RQ1NC.

[1389] (243) The compound according to any one of (1) to (233), wherein:

[1390] each -RQ1N, if present, is independently:

[1391] -LQ1N-OH or -LQ1N-ORQ1NC.

[1392] (244) The compound according to any one of (1) to (233), wherein:

[1393] each -RQ1N, if present, is independently:

[1394] -LQ1N-NH2, -LQ1N-NHRQ1NC, -LQ1N-NRQ1NC2 or -LQ1N-RQ1NM.

[1395] (245) The compound according to any one of (1) to (233), wherein:

[1396] each -RQ1N, if present, is independently:

[1397] -RQ1NC, -LQ1N-RQ1NC,

[1398] -RQ1NX,

[1399] -RQ1Nhet, -LQ1N-RQ1Nhet,

[1400] -LQ1N-OH, -LQ1N-ORQ1NC,

[1401] -S(=O)2R Q1NC,

[1402] -LQ1N-C(=O)OH, -LQ1N-C(=O)ORQ1NC, Specification 51 / 530 pages 67 CN 121568936 A

[1403] -LQ1N-C(=O)NH2, -L Q1N-C(=O)NHRQ1NK, -LQ1N-C(=O)NRQ1NC2, -L Q1N-C(=O)RQ1NP,

[1404] -LQ1N-NH2, -L Q1N-NRQ1NC2,

[1405] or -LQ1N-NHC(=O)ORQ1NC;

[1406] (246) The compound according to any one of (1) to (233), wherein:

[1407] Each -RQ1N, if present, is independently:

[1408] -RQ1NC,

[1409] -RQ1NX,

[1410] -RQ1Nhet, -LQ1N-RQ1Nhet,

[1411] -S(=O)2R Q1NC,

[1412] -LQ1N-C(=O)NRQ1NC2 or -LQ1N-C(=O)RQ1NP.

[1413] -RQ1NC group

[1414] (247) The compound according to any one of (1) to (246), wherein:

[1415] Each -RQ1NC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, wherein each phenyl is optionally substituted by one or more groups selected from the group consisting of -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[1416] (248) The compound according to any one of (1) to (246), wherein:

[1417] each -RQ1NC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-, wherein each phenyl is optionally substituted by one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[1418] (249) The compound according to any one of (1) to (246), wherein:

[1419] each -RQ1NC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or benzyl.

[1420] (250) The compound according to any one of (1) to (246), wherein:

[1421] each -RQ1NC, if present, is independently a straight-chain or branched saturated C1-4 alkyl.

[1422] (251) The compound according to any one of (1) to (246), wherein:

[1423] Each -RQ1NC, if present, is independently -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[1424] (252) The compound according to any one of (1) to (246), wherein:

[1425] Each -RQ1NC, if present, is independently -Me, -Et, -nPr, or -iPr.

[1426] (253) The compound according to any one of (1) to (246), wherein:

[1427] Each -RQ1NC, if present, is independently -Me or -Et.

[1428] (254) The compound according to any one of (1) to (246), wherein:

[1429] Each -RQ1NC, if present, is -Me.

[1430] (255) The compound according to any one of (1) to (246), wherein:

[1431] each -RQ1NC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, phenyl or C5-6 heteroaryl, wherein each C1-4 alkyl is optionally substituted with -F, -OH, -C≡N, -SO2-CH3 or -OCH3, wherein each cycloalkyl, phenyl and heteroaryl is optionally substituted with one or more groups selected from: -F, -Cl, -Br, straight-chain or branched saturated C1-4 alkyl, -CHF2, -CF3, -CH2-O-CH3, -OCH2CH3 and -C(=O)-NH-phenyl, wherein the C1-4 alkyl and phenyl are independently optionally substituted with -CH3 or -OH.

[1432] (256) The compound according to any one of (1) to (246), wherein:

[1433] each -RQ1NC, if present, is independently methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl, pyrimidinyl, oxazolyl, pyridinyl, thiazolyl, imidazole, or pyrazolyl, wherein each methyl, ethyl, propyl, isopropyl, butyl, isobutyl, or tert-butyl is optionally substituted with F, -OH, -C≡N, -SO2-CH3, or -OCH3; wherein each cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl, pyrimidinyl, oxazolyl, pyridinyl, thiazolyl, cyclopropyl, cyclohexyl, phenyl, pyrimidinyl, oxazolyl, pyridinyl, thiazolyl, cyclopropyl, cyclobutyl ...cyclobutyl, cyclopropyl, cyclobutyl, cyclohexyl, phenyl, pyrimidinyl, oxazolyl, pyridinyl, cyclobutyl, cyclopropyl, cyclobutyl, cyclobutyl, cyclohexyl, phenyl, py The imidazolyl or pyrazolyl group is optionally substituted with one or more groups selected from the group consisting of: F, Cl, Br, straight-chain or branched saturated C1-4 alkyl, -CHF2, -CF3, -CH2-O-CH3, -OCH2CH3, and -C=O-NH-phenyl, wherein the C1-4 alkyl and phenyl groups are optionally substituted independently with -CH3 or -OH.

[1434] (257) The compound according to any one of (1) to (246), wherein:

[1435] Each -RQ1NC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, phenyl, or C5-6 heteroaryl group, wherein each C1-4 alkyl group is optionally substituted with -F, -OH, -C≡N, -SO2-CH3, or -OCH3, wherein each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from the group consisting of -F, -Cl, -CF3, and -OCH3.

[1436] -RQ1NX group

[1437] (258) The compound according to any one of (1) to (257), wherein:

[1438] Each -RQ1NX, if present, is independently a straight-chain or branched saturated C1-4 fluoroalkyl group.

[1439] (259) The compound according to any one of (1) to (257), wherein:

[1440] each -RQ1NX is independently -CF3, -CHF2, -CH2CF3 or -CH2CHF2 if present.

[1441] (260) The compound according to any one of (1) to (257), wherein:

[1442] each -RQ1NX is -CHF2 if present.

[1443] (261) The compound according to any one of (1) to (257), wherein:

[1444] each -RQ1NX is -CH2CH2F, -CH2CHF2, -CH2CF3 and -CH2CH2Br if present.

[1445] -LQ1N- group

[1446] (262) The compound according to any one of (1) to (261), wherein:

[1447] Each -LQ1N- is independently -CH2-, -C(CH3)2-, -CH2CH2- or -CH2CH2CH2- if present.

[1448] (263) The compound according to any one of (1) to (261), wherein:

[1449] Each -LQ1N- is independently -CH2-, -CH2CH2- or -CH2CH2CH2- if present.

[1450] (264) The compound according to any one of (1) to (261), wherein:

[1451] Each -LQ1N- is -CH2- if present.

[1452] (265) The compound according to any one of (1) to (261), wherein:

[1453] each -LQ1N- is -CH2CH2- if present.

[1454] (266) The compound according to any one of (1) to (261), wherein:

[1455] each -LQ1N- is -CH2CH2CH2- if present.

[1456] (267) The compound according to any one of (1) to (261), wherein:

[1457] Each -LQ1N-, if present, is -CH2-, -C(CH3)2CH2-, -CH2CH2-, or -CH2CH2CH2-, wherein -CH2-, -C(CH3)2CH2-, -CH2CH2-, or -CH2CH2CH2- is optionally replaced by -OH or -OMe.

[1458] -RQ1NM group

[1459] (268) The compound according to any one of (1) to (267), wherein:

[1460] Each -RQ1NM, if present, is independently an aziridine, pyrrolidinyl, piperidinyl, piperazine, morpholinyl, thiomorpholinyl, aziridine-heptyl or diaziridine-heptyl, and:

[1461] The carbon atom is optionally substituted by one or more -RQ1NMM groups; and

[1462] The secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ1NMM, -C(=O) Specification 53 / 530 pages 69 CN 121568936 A RQ1NMM, -C(=O)ORQ1NMM, -C(=O)NH2, -C(=O)NHRQ1NMM, -C(=O)NRQ1NMM2 and -S(=O)2R Q1NMM.

[1463] (269) The compound according to any one of (1) to (267), wherein:

[1464] each -RQ1NM is independently pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl if present, and:

[1465] the carbon atom is optionally substituted by one or more -RQ1NMM groups; and

[1466] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ1NMM, -C(=O)RQ1NMM, -C(=O)ORQ1NMM, -C(=O)NH2, -C(=O)NHRQ1NMM, -C(=O)NRQ1NMM2 and -S(=O)2RQ1NMM.

[1467] (270) The compound according to any one of (1) to (267), wherein:

[1468] each -RQ1NM, if present, is independently pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl, and:

[1469] the carbon atom is optionally substituted by one or more -RQ1NMM groups; and

[1470] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ1NMM, -C(=O)RQ1NMM and -C(=O)ORQ1NMM.

[1471] -RQ1NMM group

[1472] (271) The compound according to any one of (1) to (270), wherein:

[1473] each -RQ1NMM, if present, is independently straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, wherein each phenyl group is optionally substituted with one or more groups selected from the group consisting of: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[1474] (272) The compound according to any one of (1) to (270), wherein:

[1475] each -RQ1NMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl or phenyl-CH2-, wherein each phenyl group is optionally substituted with one or more groups selected from the group consisting of: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[1476] (273) The compound according to any one of (1) to (270), wherein:

[1477] each -RQ1NMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or benzyl.

[1478] (274) The compound according to any one of (1) to (270), wherein:

[1479] each -RQ1NMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl.

[1480] (275) The compound according to any one of (1) to (270), wherein:

[1481] each -RQ1NMM, if present, is -Me.

[1482] -RQ1Nhet group

[1483] (276) The compound according to any one of (1) to (275), wherein:

[1484] Each -RQ1Nhet, if present, is independently an azircyclic butyl, oxacyclic butyl, pyrrolidinyl, tetrahydrofuranyl, piperidinyl, piperazinyl, tetrahydropyranyl, morpholinyl, thiomorpholinyl, azircyclic heptyl or diazircyclic heptyl;

[1485] and:

[1486] The sulfur atom, if present, is optionally substituted with one or two =O groups;

[1487] The carbon atom is optionally substituted with one or more -RQ1NHH or =O groups; and

[1488] The secondary nitrogen atom, if present, is optionally substituted with a group selected from: -RQ1NHH, -C(=O). RQ1NJJ, -C(=O)ORQ1NHH, -C(=O)NH2, -C(=O)NHRQ1NHH, C(=O)NRQ1NHH2 and -S(=O)2RQ1NHH.

[1489] (277) The compound according to any one of (1) to (275), wherein:

[1490] each -RQ1Nhet, if present, is independently an oxetane, pyrrolidinyl, tetrahydrofuranyl, piperidinyl, piperazinyl, tetrahydropyranyl or morpholinyl;

[1491] and: Specification 54 / 530 pages 70 CN 121568936 A

[1492] The carbon atom is optionally substituted with one or more -RQ1NHH or =O groups; and

[1493] the secondary nitrogen atom, if present, is optionally substituted with groups selected from: -RQ1NHH, -C(=O)RQ1NJJ, -C(=O)ORQ1NHH, -C(=O)NH2, -C(=O)NHRQ1NHH, C(=O)NRQ1NHH2 and -S(=O)2RQ1NHH.

[1494] (278) The compound according to any one of (1) to (275), wherein:

[1495] each -RQ1Nhet is independently pyrrolidinyl, piperidinyl or piperazineyl if present;

[1496] and:

[1497] the carbon atom is optionally substituted by one or more -RQ1NHH or =O groups; and

[1498] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ1NHH, -C(=O)RQ1NJJ, -C(=O)ORQ1NHH, -C(=O)NH2, -C(=O)NHRQ1NHH, C(=O)NRQ1NHH2 and -S(=O)2RQ1NHH.

[1499] (279) The compound according to any one of (1) to (275), wherein:

[1500] each -RQ1Nhet is independently pyrrolidinyl or piperidinyl if present;

[1501] and:

[1502] the carbon atom is optionally substituted by one or more -RQ1NHH or =O groups; and

[1503] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ1NHH, -C(=O)RQ1NJJ, -C(=O)ORQ1NHH, -C(=O)NH2, -C(=O)NHRQ1NHH, C(=O)NRQ1NHH2 and -S(=O)2RQ1NHH.

[1504] (280) The compound according to any one of (1) to (275), wherein:

[1505] each -RQ1Nhet is pyrrolidinyl if present;

[1506] and:

[1507] the carbon atom is optionally substituted by one or more -RQ1NHH or =O groups; and

[1508] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ1NHH, -C(=O)RQ1NJJ, -C(=O)ORQ1NHH, -C(=O)NH2, -C(=O)NHRQ1NHH, C(=O)NRQ1NHH2 and -S(=O)2RQ1NHH.

[1509] (281) The compound according to any one of (1) to (275), wherein:

[1510] each -RQ1Nhet is independently a non-aromatic C3-7 heterocyclic group if present;

[1511] and:

[1512] The carbon atom is optionally substituted with one or more =O groups; and

[1513] the secondary nitrogen atom, if present, is optionally substituted with a group selected from the group: -RQ1NHH, -C(=O)RQ1NJJ, -C(=O)ORQ1NHH, -C(=O)NHRQ1NHH and C(=O)NRQ1NHH2.

[1514] (282) The compound according to any one of (1) to (275), wherein:

[1515] each -RQ1Nhet is independently oxobutyryl, piperidinyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydropyranyl, morpholinyl, aziroxybutyryl or tetrahydrothiophene;

[1516] and:

[1517] the carbon atom is optionally substituted by one or more =O groups; and

[1518] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ1NHH, -C(=O)RQ1NJJ, -C(=O)ORQ1NHH, -C(=O)NHRQ1NHH and C(=O)NRQ1NHH2.

[1519] -RQ1NHH group

[1520] (283) The compound according to any one of (1) to (283), wherein:

[1521] Each -RQ1NHH, if present, is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, wherein each phenyl is optionally substituted by one or more groups selected from the group consisting of: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2. Specification 55 / 530 pages 71 CN 121568936 A

[1522] (284) The compound according to any one of (1) to (283), wherein:

[1523] each -RQ1NHH, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl or phenyl-CH2-, wherein each phenyl is optionally substituted by one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[1524] (285) The compound according to any one of (1) to (283), wherein:

[1525] each -RQ1NHH, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl or benzyl.

[1526] (286) The compound according to any one of (1) to (283), wherein:

[1527] each -RQ1NHH, if present, is independently a straight-chain or branched saturated C1-4 alkyl group.

[1528] (287) The compound according to any one of (1) to (283), wherein:

[1529] Each -RQ1NHH, if present, is independently -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[1530] (288) The compound according to any one of (1) to (283), wherein:

[1531] Each -RQ1NHH, if present, is independently -Me, -Et, -nPr, or -iPr.

[1532] (289) The compound according to any one of (1) to (283), wherein:

[1533] Each -RQ1NHH, if present, is independently -Me or -Et.

[1534] (290) The compound according to any one of (1) to (283), wherein:

[1535] Each -RQ1NHH, if present, is -Me.

[1536] (291) The compound according to any one of (1) to (283), wherein:

[1537] each -RQ1NHH, if present, is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl or phenyl-C1-3 alkyl.

[1538] (292) The compound according to any one of (1) to (283), wherein:

[1539] each -RQ1NHH, if present, is independently -Me, -Et, -tBu, cyclopropyl, benzyl or phenethyl.

[1540] -RQ1NJJ group

[1541] (293) The compound according to any one of (1) to (292), wherein:

[1542] -RQ1NJJ is -RJ1, -LJ-RJ2, -RJ3, -LJ-RJ3, -RJ4, -LJ-RJ4 or -LJ-RJ5 if present.

[1543] (294) The compound according to any one of (1) to (292), wherein:

[1544] -RQ1NJJ is -RJ1, -LJ-RJ2, -LJ-RJ3, -LJ-RJ4 or -LJ-RJ5 if present.

[1545] (295) The compound according to any one of (1) to (292), wherein:

[1546] -RQ1NJJ is -RJ1, -LJ-RJ3, -LJ-RJ4 or -LJ-RJ5 if present.

[1547] (296) The compound according to any one of (1) to (292), wherein:

[1548] -RQ1NJJ is -RJ1, -LJ-RJ4 or -LJ-RJ5 if present.

[1549] (297) The compound according to any one of (1) to (292), wherein:

[1550] -RQ1NJJ is -RJ1 or -LJ-RJ4 if present.

[1551] (298) The compound according to any one of (1) to (292), wherein:

[1552] -RQ1NJJ is -LJ-RJ2, -LJ-RJ3, -LJ-RJ4 or -LJ-RJ5 if present.

[1553] (299) The compound according to any one of (1) to (292), wherein:

[1554] -RQ1NJJ is -LJ-RJ3, -LJ-RJ4 or -LJ-RJ5 if present.

[1555] (300) The compound according to any one of (1) to (292), wherein:

[1556] -RQ1NJJ is -LJ-RJ4 or -LJ-RJ5 if present.

[1557] (301) The compound according to any one of (1) to (292), wherein: Specification 56 / 530 pages 72 CN 121568936 A

[1558] -RQINJJ is -LJ-RJ4 if present.

[1559] -RJ1 group

[1560] (302) The compound according to any one of (1) to (301), wherein:

[1561] -RJ1, if present, is a straight-chain or branched saturated C1-6 alkyl; and optionally substituted by one or more groups selected from the group consisting of: -F, -OH, -ORJJ, -O-phenyl, -C(=O)OH, -C(=O)ORJJ, -NH2, -NHRJJ and -NRJJ2.

[1562] (303) The compound according to any one of (1) to (301), wherein:

[1563] -RJ1, if present, is a straight-chain or branched saturated C1-4 alkyl; and optionally substituted by one or more groups selected from the group consisting of: -F, -OH, -ORJJ, -O-phenyl, -C(=O)OH, -C(=O)ORJJ, -NH2, -NHRJJ and -NRJJ2.

[1564] (304) The compound according to any one of (1) to (301), wherein:

[1565] -RJ1, if present, is a straight-chain or branched saturated C1-4 alkyl group; and optionally substituted by one or more groups selected from -F, -OH or -ORJJ.

[1566] (305) The compound according to any one of (1) to (301), wherein:

[1567] -RJ1, if present, is a straight-chain or branched saturated C1-4 alkyl group.

[1568] (306) The compound according to any one of (1) to (301), wherein:

[1569] -RJ1, if present, is -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[1570] (307) The compound according to any one of (1) to (301), wherein:

[1571] -RJ1 is -Me, -Et, -nPr or -iPr if present.

[1572] (308) The compound according to any one of (1) to (301), wherein:

[1573] -RJ1 is -Me or -Et if present.

[1574] (309) The compound according to any one of (1) to (301), wherein:

[1575] -RJ1 is -Me if present.

[1576] (310) The compound according to any one of (1) to (301), wherein:

[1577] -RJ1 is a straight-chain or branched saturated C1-6 alkyl if present; and optionally substituted with one or more groups selected from the group consisting of -F, -ORJJ, -O-phenyl and -C(=O)ORJJ.

[1578] (311) The compound according to any one of (1) to (301), wherein:

[1579] -RJ1 is -Me, -Et, -iPr, -iBu if present; and optionally substituted by one or more groups selected from -F, -ORJJ, -O-phenyl and -C(=O)ORJJ.

[1580] -RJ2 group

[1581] (312) The compound according to any one of (1) to (311), wherein:

[1582] Each -RJ2 is independently cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl if present.

[1583] (313) The compound according to any one of (1) to (311), wherein:

[1584] Each -RJ2 is cyclopropyl if present.

[1585] (314) The compound according to any one of (1) to (311), wherein:

[1586] each -RJ2 is independently cyclobutyl if present.

[1587] (315) The compound according to any one of (1) to (311), wherein:

[1588] each -RJ2 is independently cyclopentyl if present.

[1589] (316) The compound according to any one of (1) to (311), wherein:

[1590] each -RJ2 is independently cyclohexyl if present.

[1591] -RJ3 group specification 57 / 530 pages 73 CN 121568936 A

[1592] (317) The compound according to any one of (1) to (316), wherein:

[1593] each -RJ3 is independently non-aromatic C3-7 heteroaryl if present.

[1594] (318) The compound according to any one of (1) to (316), wherein:

[1595] each -RJ3, if present, is independently an azirrobutyl, oxacyclobutyl, pyrrolithyl, tetrahydrofuranyl, piperidinyl, piperazinyl, tetrahydropyranyl, morpholinyl, thiomorpholinyl, azirroheptyl or diazirroheptyl;

[1596] and:

[1597] the sulfur atom, if present, is optionally substituted with one or two =O groups;

[1598] The carbon atom is optionally substituted by one or more groups selected from the group consisting of -F, -RJJ, -CF3, -OH, -ORJJ, -NH2, -NHRJJ and -NRJJ2; and

[1599] the secondary nitrogen atom, if present, is optionally substituted by a group selected from the group consisting of -RJJ, -C(=O)RJJ, -C(=O)ORJJ and -S(=O)2RJJ.

[1600] (319) The compound according to any one of (1) to (316), wherein:

[1601] each -RJ3, if present, is independently pyrrolidinyl, tetrahydrofuranyl, piperidinyl, piperazinyl, tetrahydropyranyl or morpholinyl;

[1602] and:

[1603] the carbon atom is optionally substituted by one or more groups selected from the group consisting of -F, -RJJ, -CF3, -OH, -ORJJ, -NH2, -NHRJJ and -NRJJ2; and

[1604] the secondary nitrogen atom, if present, is optionally substituted by a group selected from the group consisting of -RJJ, -C(=O)RJJ, -C(=O)ORJJ and -S(=O)2RJJ.

[1605] (320) The compound according to any one of (1) to (316), wherein:

[1606] each -RJ3, if present, is independently pyrrolidinyl, tetrahydrofuranyl, piperidinyl, piperazinyl, tetrahydropyranyl or morpholinyl;

[1607] and:

[1608] the carbon atom is optionally substituted by one or more groups selected from -F and -RJJ; and

[1609] the secondary nitrogen atom, if present, is optionally substituted by groups selected from -RJJ, -C(=O)RJJ, -C(=O)ORJJ and -S(=O)2RJJ.

[1610] (321) The compound according to any one of (1) to (316), wherein:

[1611] each -RJ3, if present, is independently pyrrolyl, tetrahydrofuranyl, piperidinyl, piperazinyl, tetrahydropyranyl or morpholinyl;

[1612] and:

[1613] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RJJ, -C(=O)RJJ, -C(=O)ORJJ and -S(=O)2RJJ.

[1614] (322) The compound according to any one of (1) to (316), wherein:

[1615] each -RJ3, if present, is independently tetrahydropyranyl or piperidinyl.

[1616] -RJ4 group

[1617] (323) The compound according to any one of (1) to (322), wherein:

[1618] each -RJ4 is phenyl if present; and optionally substituted by one or more groups selected from: -F, -Cl, -RJJ, -OH, -NH2, -NHRJJAnd -NRJJ.

[1619] (324) The compound according to any one of (1) to (322), wherein: Specification 58 / 530 pages 74 CN 121568936 A

[1620] Each -RJ4 is phenyl if present.

[1621] (325) The compound according to any one of (1) to (322), wherein:

[1622] Each -RJ4 is phenyl if present; and optionally substituted by one or more groups selected from: -F, -ORJJ, -NH2 and -NRJJ2.

[1623] -RJ5 group

[1624] (326) The compound according to any one of (1) to (325), wherein:

[1625] Each -RJ5 is independently C5-6 heteroaryl if present.

[1626] (327) The compound according to any one of (1) to (325), wherein:

[1627] each -RJ5 is independently pyrroleyl, furanyl, thiophenyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridinyl, pyrimidinyl or pyridazinyl if present; and:

[1628] the carbon atom is optionally substituted by one or more groups selected from the group: -F, -RJJ, -CF3, -OH, -ORJJ, -NH2, -NHRJJ and -NRJJ2; and

[1629] the secondary nitrogen atom, if present, is optionally substituted by a group selected from the group: -RJJ, -C(=O)RJJ, -C(=O)ORJJ and -S(=O)2RJJ.

[1630] (328) The compound according to any one of (1) to (325), wherein:

[1631] each -RJ5 is independently pyrrole, furanyl, thiophene, pyrazolyl, pyridinyl, pyrimidinyl or pyridazinyl if present; and:

[1632] the carbon atom is optionally substituted by one or more groups selected from the group consisting of -F, -RJJ, -CF3, -OH, -ORJJ, -NH2, -NHRJJ and -NRJJ2; and

[1633] the secondary nitrogen atom, if present, is optionally substituted by a group selected from the group consisting of -RJJ, -C(=O)RJJ, -C(=O)ORJJ and -S(=O)2RJJ.

[1634] (329) The compound according to any one of (1) to (325), wherein:

[1635] each -RJ5 is independently thiophene, pyrazolyl or pyridinyl if present; and:

[1636] the carbon atom is optionally substituted by one or more groups selected from: -F, -RJJ, -CF3, -OH, -ORJJ, -NH2, -NHRJJ and -NRJJ2; and

[1637] The secondary nitrogen atom, if present, is optionally substituted with a group selected from the following: -RJJ, -C(=O)RJJ, -C(=O)ORJJ and -S(=O)2RJJ.

[1638] (330) The compound according to any one of (1) to (325), wherein:

[1639] Each -RJ5, if present, is independently thiophene, pyrazol, or pyridinyl.

[1640] -LJ- group

[1641] (331) The compound according to any one of (1) to (330), wherein:

[1642] Each -LJ-, if present, is independently -CH2-, -CF2-, -C(CH3)2-, -CH2CH2- or -CH2CH2CH2-.

[1643] (332) The compound according to any one of (1) to (330), wherein:

[1644] each -LJ- is independently a straight-chain or branched saturated C1-4 alkylene group if present.

[1645] (333) The compound according to any one of (1) to (330), wherein:

[1646] each -LJ- is independently -CH2-, -C(CH3)2-, -CH2CH2- or -CH2CH2CH2- if present.

[1647] (334) The compound according to any one of (1) to (330), wherein:

[1648] each -LJ- is independently -CH2-, -CH2CH2- or -CH2CH2CH2- if present.

[1649] (335) The compound according to any one of (1) to (330), wherein:

[1650] Each -LJ- is -CH2- if present.

[1651] (336) The compound according to any one of (1) to (330), wherein:

[1652] Each -LJ- is -CH2CH2- if present.

[1653] (337) The compound according to any one of (1) to (330), wherein:

[1654] Each -LJ- is -CH2CH2CH2- if present.

[1655] (338) The compound according to any one of (1) to (330), wherein:

[1656] Each -LJ- is independently -CH2- or -CH2CH2- if present, and optionally substituted with one or more -F.

[1657] -RJJ group

[1658] (339) The compound according to any one of (1) to (338), wherein:

[1659] each -RJJ, if present, is:

[1660] -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[1661] (340) The compound according to any one of (1) to (338), wherein:

[1662] If any -RJJ is present, it is:

[1663] -Me, -Et, -nPr or -iPr.

[1664] (341) The compound according to any one of (1) to (338), wherein:

[1665] If any -RJJ is present, it is:

[1666] -Me or -Et.

[1667] (342) The compound according to any one of (1) to (338), wherein:

[1668] If any -RJJ is present, it is:

[1669] -Me.

[1670] -RQ1NK group

[1671] (343) The compound according to any one of (1) to (342), wherein:

[1672] -RQ1NK is -RK1, -RK2, -LK-RK2, -RK3 or -LK-RK3 if present;

[1673] (344) The compound according to any one of (1) to (342), wherein:

[1674] -RQ1NK is -RK1, -RK2, -RK3 or -LK-RK3 if present;

[1675] (345) The compound according to any one of (1) to (342), wherein:

[1676] -RQ1NK is -RK1 if present.

[1677] (346) The compound according to any one of (1) to (342), wherein:

[1678] -RQ1NK is -RK2 if present.

[1679] (347) The compound according to any one of (1) to (342), wherein:

[1680] -RQINK is -RK3 if present.

[1681] (348) The compound according to any one of (1) to (342), wherein:

[1682] -RQ1NK is -LK-RK3 if present.

[1683] -RK1 group

[1684] (349) The compound according to any one of (1) to (348), wherein:

[1685] -RK1 is a straight-chain or branched saturated C1-6 alkyl group if present; and optionally substituted by one or more groups selected from: -F, -OH, -ORKK, -O-phenyl, -C(=O)OH, -C(=O)ORKK, -NH2, -NHRKK and -NRKK2.

[1686] (350) The compound according to any one of (1) to (348), wherein:

[1687] -RK1 is a straight-chain or branched saturated C1-4 alkyl group if present; and optionally substituted with one or more groups selected from: -F, -OH, -ORKK, -O-phenyl, -C(=O)OH, -C(=O)ORKK, -NH2, -NHRKK and -NRKK2.

[1688] (351) The compound according to any one of (1) to (348), wherein:

[1689] -RK1, if present, is a straight-chain or branched saturated C1-4 alkyl group; and optionally substituted by one or more groups selected from -F, -OH or -ORKK.

[1690] (352) The compound according to any one of (1) to (348), wherein:

[1691] -RK1, if present, is a straight-chain or branched saturated C1-4 alkyl group.

[1692] (353) The compound according to any one of (1) to (348), wherein:

[1693] -RK1, if present, is -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[1694] (354) The compound according to any one of (1) to (348), wherein:

[1695] -RK1 is -Me, -Et, -nPr or -iPr if present.

[1696] (355) The compound according to any one of (1) to (348), wherein:

[1697] -RK1 is -Me or -Et if present.

[1698] (356) The compound according to any one of (1) to (348), wherein:

[1699] -RK1 is -Me if present.

[1700] (357) The compound according to any one of (1) to (348), wherein:

[1701] -RK1 is a straight-chain or branched saturated C1-7 alkyl group if present; and optionally substituted with one or more groups selected from -OH, -ORKK, -OCH2CH2OCH3 and -NRKK2.

[1702] (358) The compound according to any one of (1) to (348), wherein:

[1703] -RK1 is -Me, -Et, -nPr, -iPr, -tBu or heptane if present; and optionally substituted by one or more groups selected from -OH, -ORKK, -OCH2CH2OCH3 and -NRKK2.

[1704] -RK2 group

[1705] (359) The compound according to any one of (1) to (358), wherein:

[1706] Each -RK2 is independently C3-6 cycloalkyl if present.

[1707] (360) The compound according to any one of (1) to (358), wherein:

[1708] Each -RK2 is independently cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl if present.

[1709] (361) The compound according to any one of (1) to (358), wherein:

[1710] each -RK2 is cyclopropyl if present.

[1711] (362) The compound according to any one of (1) to (358), wherein:

[1712] each -RK2 is independently cyclobutyl if present.

[1713] (363) The compound according to any one of (1) to (358), wherein:

[1714] each -RK2 is independently cyclopentyl if present.

[1715] (364) The compound according to any one of (1) to (358), wherein:

[1716] each -RK2 is independently cyclohexyl if present.

[1717] -RK3 group

[1718] (365) The compound according to any one of (1) to (364), wherein:

[1719] each -RK3 is independently non-aromatic C3-7 heterocyclic group if present; and:

[1720] a secondary nitrogen atom, if present, optionally substituted with a group selected from -RKK and -C(=O)ORKK.

[1721] (366) The compound according to any one of (1) to (364), wherein: Specification 61 / 530 pages 77 CN 121568936 A

[1722] Each -RK3, if present, is independently morpholino, piperidino, piperazino, pyrrolidinyl or tetrahydropyrrolidinyl; and:

[1723] The secondary nitrogen atom, if present, is optionally substituted by a group selected from -RKK and -C(=O)ORKK.

[1724] (367) The compound according to any one of (1) to (364), wherein:

[1725] each -RK3, if present, is independently an aziridine, oxadiidine, pyrrolidinyl, tetrahydrofuranyl, piperidinyl, piperazinyl, tetrahydropyranyl, morpholinyl, thiomorpholinyl, aziridine-heptyl or diaziridine-heptyl;

[1726] and:

[1727] the sulfur atom, if present, is optionally substituted by one or two =O groups;

[1728] the carbon atom is optionally substituted by one or more groups selected from: -F, -RKK, -CF3, -OH, -ORKK, -NH2, -NHRKK and -NRKK2; and

[1729] the secondary nitrogen atom, if present, is optionally substituted by groups selected from: -RKK, -C(=O)RKK, -C (=O)ORKK and -S(=O)2R KK.

[1730] (368) The compound according to any one of (1) to (364), wherein:

[1731] each -RK3, if present, is independently pyrrolidinyl, tetrahydrofuranyl, piperidinyl, piperazinyl, tetrahydropyranyl or morpholinyl;

[1732] and:

[1733] the carbon atom is optionally substituted by one or more groups selected from: -F, -RKK, -CF3, -OH, -OR KK, -NH2, -NHR KK and -NRKK2; and

[1734] the secondary nitrogen atom, if present, is optionally substituted by groups selected from: -RKK, -C(=O)RKK, -C(=O)ORKK and -S(=O)2R KK.

[1735] (369) The compound according to any one of (1) to (364), wherein:

[1736] each -RK3, if present, is independently pyrrolidinyl, tetrahydrofuranyl, piperidinyl, piperazinyl, tetrahydropyranyl or morpholinyl;

[1737] and:

[1738] the carbon atom is optionally substituted by one or more groups selected from: -F and -RKK; and

[1739] the secondary nitrogen atom, if present, is optionally substituted by groups selected from: -RKK, -C(=O)RKK, -C(=O)ORKK and -S(=O)2R KK.

[1740] (370) The compound according to any one of (1) to (364), wherein:

[1741] each -RK3, if present, is independently pyrrolidinyl, tetrahydrofuranyl, piperidinyl, piperazinyl, tetrahydropyranyl or morpholinyl;

[1742] and:

[1743] a secondary nitrogen atom, if present, optionally substituted with a group selected from: -RKK, -C(=O)RKK, -C(=O)ORKK and -S(=O)2RKK.

[1744] -RK4 group

[1745] (371) The compound according to any one of (1) to (370), wherein:

[1746] each -RK4, if present, is phenyl; and optionally substituted with one or more groups selected from: -F, -Cl, -RKK, -CF3, -OH and -ORKK.

[1747] (372) The compound according to any one of (1) to (370), wherein:

[1748] each -RK4 is phenyl if present. Specification 62 / 530 pages 78 CN 121568936 A

[1749] -RK5 group

[1750] (373) The compound according to any one of (1) to (372), wherein:

[1751] Each -RK5, if present, is independently pyrroleyl, furanyl, thiopheneyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyridinyl, pyrimidinyl or pyridazinyl; and:

[1752] The carbon atom is optionally substituted by one or more groups selected from: -F, -RKK, -CF3, -OH, -ORKK, -NH2, -NHRKK and -NRKK2; and

[1753] The secondary nitrogen atom, if present, is optionally substituted by groups selected from: -RKK, -C(=O)RKK, -C(=O)ORKK and -S(=O)2R KK.

[1754] (374) The compound according to any one of (1) to (372), wherein:

[1755] each -RK5 is independently pyrroleyl, furanyl, thiopheneyl, pyrazolyl, pyridyl, pyrimidinyl orPyridazinyl; and:

[1756] The carbon atom is optionally substituted by one or more groups selected from the group consisting of -F, -RKK, -CF3, -OH, -ORKK, -NH2, -NHRKK and -NRKK2; and

[1757] The secondary nitrogen atom, if present, is optionally substituted by a group selected from the group consisting of -RKK, -C(=O)RKK, -C(=O)ORKK and -S(=O)2RKK.

[1758] (375) The compound according to any one of (1) to (372), wherein:

[1759] Each -RK5, if present, is independently pyrroloyl, furanyl, thiophenyl, pyrazolyl, pyridinyl, pyrimidinyl or pyridazinyl.

[1760] -LK- group

[1761] (376) The compound according to any one of (1) to (375), wherein:

[1762] Each -LK- is independently a straight-chain or branched saturated C1-4 alkylene group if present.

[1763] (377) The compound according to any one of (1) to (375), wherein:

[1764] Each -LK- is independently -CH2-, -C(CH3)2-, -CH2CH2- or -CH2CH2CH2- if present.

[1765] (378) The compound according to any one of (1) to (375), wherein:

[1766] Each -LK- is independently -CH2-, -CH2CH2- or -CH2CH2CH2- if present.

[1767] (379) The compound according to any one of (1) to (375), wherein:

[1768] each -LK- is independently -CH2- or -CH2CH2- if present.

[1769] (380) The compound according to any one of (1) to (375), wherein:

[1770] each -LK- is -CH2- if present.

[1771] (381) The compound according to any one of (1) to (375), wherein:

[1772] each -LK- is -CH2CH2- if present.

[1773] (382) The compound according to any one of (1) to (375), wherein:

[1774] each -LK- is -CH2CH2CH2- if present.

[1775] -RKK group

[1776] (383) The compound according to any one of (1) to (382), wherein:

[1777] Each -RKK, if present, is:

[1778] -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[1779] (384) The compound according to any one of (1) to (382), wherein:

[1780] Each -RKK, if present, is: Specification 63 / 530 pages 79 CN121568936 A

[1781] -Me, -Et, -nPr or -iPr.

[1782] (385) The compound according to any one of (1) to (382), wherein:

[1783] each -RKK, if present, is:

[1784] -Me or -tBu.

[1785] (386) The compound according to any one of (1) to (382), wherein:

[1786] each -RKK, if present, is:

[1787] -Me or -Et.

[1788] (387) The compound according to any one of (1) to (382), wherein:

[1789] each -RKK, if present, is:

[1790] -Me.

[1791] -RQ1NP group

[1792] (388) The compound according to any one of (1) to (387), wherein:

[1793] -RQ1NP, if present, is independently a non-aromatic C3-11 heterocyclic group having at least one N ring atom and connected by the N ring atom; and:

[1794] The carbon atom is optionally substituted by one or more groups selected from the group: -RQ1NPP, -F, -OH, -ORQ1NPP and =O; and

[1795] The secondary nitrogen atom, if present, is optionally substituted by a group selected from the group: -RQ1NPP, -RQ1NPPX, -C(=O)RQ1NPP, -C(=O)ORQ1NPP, -C(=O)NRQ1NPP2 and -S(=O)2RQ1NPP.

[1796] (389) The compound according to any one of (1) to (387), wherein:

[1797] -RQ1NP, if present, is independently a morpholino, piperazino, piperidino, pyrrolyl, 2,5-diazabicyclo[2.2.1]heptyl, 2,6-diazabicyclo[3.3]heptyl, 2,8-diazabicyclo[4.5]decyl, 1,4-diazapentyl, aziridine, 3,8-diazabicyclo[3.2.1]octyl, 3-azibicyclo[3.1.0]hexyl, aziridine, 2-azispiro[3.3]heptyl or 2,6-azispiro[3.3]heptyl; and:

[1798] The carbon atom is optionally substituted with one or more groups selected from the group consisting of -RQ1NPP, -F, -OH, -ORQ1NPP and =O; and

[1799] the secondary nitrogen atom, if present, is optionally substituted with groups selected from the group consisting of -RQ1NPP, -RQ1NPPX, -C(=O)RQ1NPP, -C(=O)ORQ1NPP, -C(=O)NRQ1NPP2 and -S(=O)2RQ1NPP.

[1800] (390) the compound according to any one of (1) to (387), wherein:

[1801] If present, the carbon atom of -RQ1NP is optionally substituted independently by one or more groups selected from -RQ1NPP; and

[1802] the secondary nitrogen atom, if present, is optionally substituted by a group selected from -RQ1NPP.

[1803] (391) The compound according to any one of (1) to (387), wherein:

[1804] -RQ1NP is independently:

[1805] aziridine, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, aziridine heptane, diaziridine heptane, 3-azibicyclo[3.1.0]hexyl, 3,6-diazabicyclo[3.1.1]heptyl, 3-azibicyclo[3.1.1]heptyl, 2,5-diazabicyclo[2.2.1]heptyl, 2-azibicyclo[2.2.1]heptyl, 3,8-diazabicyclo[3.2.1]octyl, 3-azibicyclo[3.2.1]octyl, 2-azibicyclo[3.3]heptyl, 2,6-azibicyclo[3.4]hepyl, 3.5-diazabicyclo[3.5]octyl, 2-azibicyclo[3.6]hepyl, 2,6-azibicyclo[3.5]hepyl, 3.6-azibicyclo[3.6]hepyl, 3.7]octyl, 2-azibicyclo[3.6]hepyl, 3.7]hepyl, 3.8-diazabicyclo[3.2.1]octyl, 3.7]octyl, 2-azibicyclo[3.6]hepyl, 3.7]hepyl, 3.8-azibicyclo[3.6]octyl, 3.7]hepyl, 3.8-azibicyclo[3.6]hep ...8 .3]Heptyl, 6-azaspirocyclic[3.4]octyl, 2-azaspirocyclic[3.4]octyl, 2,7-azaspirocyclic[3.4]octyl, 7-azaspirocyclic[3.5]nonyl, 2-azaspirocyclic[3.5]nonyl, 2,7-diazaspirocyclic[3.5]nonyl, 2,7-diazaspirocyclic[4.4]nonyl, 2,8-diazaspirocyclic[4.5]decyl or 3,9-diazaspirocyclic[5.5]undecyl;

[1806] and linked by an N-ring atom;

[1807] and:

[1808] a sulfur atom, if present, optionally substituted by one or two =O groups;

[1809] The carbon atom is optionally substituted by one or more groups selected from the following: -RQ1NPP, -F, -OH, -ORQ1NPP and =O; and

[1810] the secondary nitrogen atom, if present, is optionally substituted by groups selected from the following: -RQ1NPP, -RQ1NPPX, -C(=O)RQ1NPP, -C(=O)ORQ1NPP, -C(=O)NH2, -C(=O)NHRQ1NPP, -C(=O)NRQ1NPP2 and -S(=O)2RQ1NPP.

[1811] Specification 65 / 530 pages 81 CN 121568936 A

[1812]

[1813] (392) The compound according to any one of (1) to (387), wherein:

[1814] -RQ1NP, if present, is independently:

[1815] azahexacyclic butyl, pyrrolidinyl, piperidinyl, piperazinyl, 2-azaspiro[3.3]heptyl, morpholinyl, thiomorpholinyl, azahexacyclic heptyl, or diazaheptyl;

[1816] and linked by an N-ring atom;

[1817] And:

[1818] Sulfur atoms, if present, are optionally substituted with one or two =O groups;

[1819] Carbon atoms are optionally substituted with one or more groups selected from the group consisting of -RQ1NPP, -F, -OH, -ORQ1NPP and =O; and

[1820] Secondary nitrogen atoms, if present, are optionally substituted with groups selected from the group consisting of -RQ1NPP, -RQ1NPPX, -C(=O)RQ1NPP, -C(=O)ORQ1NPP, -C(=O)NH2, -C(=O)NHRQ1NPP, -C(=O)NRQ1NPP2 and -S(=O)2RQ1NPP.

[1821] (393) The compound according to any one of (1) to (387), wherein:

[1822] -RQ1NP, if present, is independently:

[1823] azahexacyclic butyl, pyrrolidinyl, piperidinyl, piperazinyl, or morpholinyl;

[1824] and linked by an N-ring atom;

[1825] and:

[1826] the carbon atom is optionally substituted by one or more groups selected from: -RQ1NPP, -F, -OH, -ORQ1NPP and =O; Specification 66 / 530 pages 82 CN 121568936 A and

[1827] the secondary nitrogen atom, if present, is optionally substituted by groups selected from: -RQ1NPP, -RQ1NPPX, -C(= O)RQ1NPP, -C(=O)ORQ1NPP, -C(=O)NH2, -C(=O)NHRQ1NPP, -C(=O)NRQ1NPP2 and -S(=O)2RQ1NPP.

[1828] -RQ1NPP group

[1829] (394) The compound according to any one of (1) to (393), wherein:

[1830] Each -RQ1NPP, if present, is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-C1-3 alkyl or phenyl, wherein the C1-4 alkyl is optionally substituted with -F, -OH or -OCH3.

[1831] (395) The compound according to any one of (1) to (393), wherein:

[1832] each -RQ1NPP, if present, is independently -Me, -Et, -iPr, -iBu, -tBu, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl or phenyl, wherein -Me, -Et, -iPr, -iBu or -tBu is optionally substituted with -F, -OH or -OCH3.

[1833] (396) The compound according to any one of (1) to (393), wherein:

[1834] each -RQ1NPP, if present, is independently a straight-chain or branched saturated C1-4 alkyl or phenyl, wherein the C1-4 alkyl is independently...Optionally substituted with -F, -OH or -OCH3.

[1835] (397) The compound according to any one of (1) to (393), wherein:

[1836] each -RQ1NPP, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl or phenyl-CH2-, wherein each phenyl is optionally substituted with one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[1837] (398) The compound according to any one of (1) to (393), wherein:

[1838] each -RQ1NPP, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl or phenyl-CH2-.

[1839] (399) The compound according to any one of (1) to (393), wherein:

[1840] each -RQ1NPP, if present, is independently a straight-chain or branched saturated C1-4 alkyl group.

[1841] (400) The compound according to any one of (1) to (393), wherein:

[1842] each -RQ1NPP, if present, is:

[1843] -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[1844] (401) The compound according to any one of (1) to (393), wherein:

[1845] each -RQ1NPP, if present, is:

[1846] -Me, -Et, -nPr or -iPr.

[1847] (402) The compound according to any one of (1) to (393), wherein:

[1848] each -RQ1NPP, if present, is:

[1849] -Me or -Et.

[1850] (403) The compound according to any one of (1) to (393), wherein:

[1851] each -RQ1NPP, if present, is:

[1852] -Me.

[1853] -RQ1NPPX group

[1854] (404) The compound according to any one of (1) to (403), wherein:

[1855] -RQ1NPPX, if present, is independently a straight-chain or branched saturated C1-4 fluoroalkyl group.

[1856] (405) The compound according to any one of (1) to (403), wherein:

[1857] -RQ1NPPX is independently -CF3, -CHF2, -CH2CF3 or -CH2CHF2 if present. Specification 67 / 530 pages 83 CN 121568936 A

[1858] (406) The compound according to any one of (1) to (403), wherein:

[1859] -RQ1NPPX is -CH2CF3 if present.

[1860] -RQ2C group

[1861] (407) The compound according to any one of (1) to (406), wherein:

[1862] each -RQ2C is independently:

[1863] -F,

[1864] -RQ2CC, -RQ2CX,

[1865] -OH, -ORQ2CC, -ORQ2CX,

[1866] -NH2, -NHRQ2CC, -NRQ2CC2, -RQ2CM,

[1867] -NHC(=O)RQ2CC, -NHC(=O)ORQ2CC or

[1868] =O.

[1869] (408) The compound according to any one of (1) to (406), wherein:

[1870] each -RQ2C, if present, is independently:

[1871] -F,

[1872] -RQ2CC, -RQ2CX,

[1873] -OH, -ORQ2CC, -ORQ2CX,

[1874] -NH2, -NHRQ2CC, -NRQ2CC2 or -RQ2CM.

[1875] (409) The compound according to any one of (1) to (406), wherein:

[1876] each -RQ2C, if present, is independently:

[1877] -F,

[1878] -RQ2CC, -RQ2CX,

[1879] -OH, -ORQ2CC or -ORQ2CX.

[1880] -RQ2CC group

[1881] (410) The compound according to any one of (1) to (409), wherein:

[1882] Each -RQ2CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-, wherein each phenyl is optionally substituted by one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[1883] (411) The compound according to any one of (1) to (409), wherein:

[1884] Each -RQ2CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-.

[1885] (412) The compound according to any one of (1) to (409), wherein:

[1886] each -RQ2CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl group.

[1887] (413) The compound according to any one of (1) to (409), wherein:

[1888] each -RQ2CC, if present, is:

[1889] -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[1890] (414) The compound according to any one of (1) to (409), wherein:

[1891] each -RQ2CC, if present, is:

[1892] -Me, -Et, -nPr or -iPr.

[1893] (415) The compound according to any one of (1) to (409), wherein:

[1894] Each -RQ2CC, if present, is: Specification 68 / 530 pages 84 CN 121568936 A

[1895] -Me or -Et.

[1896] (416) The compound according to any one of (1) to (409), wherein:

[1897] Each -RQ2CC, if present, is:

[1898] -Me.

[1899] -RQ2CX group

[1900] (417) The compound according to any one of (1) to (416), wherein:

[1901] Each -RQ2CX, if present, is independently a straight-chain or branched saturated C1-4 fluoroalkyl group.

[1902] (418) The compound according to any one of (1) to (341), wherein:

[1903] each -RQ2CX is independently -CF3, -CHF2, -CH2CF3 or -CH2CHF2 if present.

[1904] (419) The compound according to any one of (1) to (416), wherein:

[1905] each -RQ2CX is -CF3 if present.

[1906] -RQ2CM group

[1907] (420) The compound according to any one of (1) to (419), wherein:

[1908] Each -RQ2CM, if present, is independently an azircyclic butyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, azircyclic heptyl or diazircyclic heptyl, and:

[1909] The carbon atom is optionally substituted by one or more -RQ2CMM groups; and

[1910] The secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ2CMM, -C(=O)RQ2CMM, -C(=O)ORQ2CMM, -C(=O)NH2, -C(=O)NHRQ2CMM, -C(=O)NRQ2CMM2 and -S(=O)2RQ2CMM.

[1911] (421) The compound according to any one of (1) to (419), wherein:

[1912] each -RQ2CM, if present, is independently pyrrolidinyl, piperidinyl, piperazinyl, or morpholinyl, and:

[1913] the carbon atom is optionally substituted by one or more -RQ2CMM groups; and

[1914] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ2CMM, -C(=O)RQ2CMM, -C(=O)ORQ2CMM, -C(=O)NH2, -C(=O)NHRQ2CMM, -C(=O)NRQ2CMM2, and -S(=O)2RQ2CMM.

[1915] (422) The compound according to any one of (1) to (419), wherein:

[1916] each -RQ2CM is independently pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl if present, and:

[1917] the carbon atom is optionally substituted by one or more -RQ2CMM groups; and

[1918] the secondary nitrogen atom, if present, is optionally substituted by a group selected from -RQ2CMM, -C(=O)RQ2CMM and -C(=O)ORQ2CMM.

[1919] -RQ2CMM group

[1920] (423) The compound according to any one of (1) to (422), wherein:

[1921] Each -RQ2CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-, wherein each phenyl is optionally substituted by one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[1922] (424) The compound according to any one of (1) to (422), wherein:

[1923] Each -RQ2CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-.

[1924] (425) The compound according to any one of (1) to (422), wherein:

[1925] each -RQ2CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl group.

[1926] (426) The compound according to any one of (1) to (422), wherein:

[1927] each -RQ2CMM, if present, is: Specification 69 / 530 pages 85 CN 121568936 A

[1928] -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[1929] (427) The compound according to any one of (1) to (422), wherein:

[1930] each -RQ2CMM, if present, is:

[1931] -Me, -Et, -nPr or -iPr.

[1932] (428) The compound according to any one of (1) to (422), wherein:

[1933] each -RQ2CMM, if present, is:

[1934] -Me or -Et.

[1935] (429) The compound according to any one of (1) to (422), wherein:

[1936] each -RQ2CMM, if present, is:

[1937] -Me.

[1938] -RQ2N group

[1939] (430) The compound according to any one of (1) to (429), wherein:

[1940] each -RQ2N, if present, is independently:

[1941] -RQ2NC,

[1942] =O, -C(=O)RQ2NC,

[1943] C(=O)-LQ2N-RQ2NM,

[1944] -C(=O)ORQ2NC,

[1945] -LQ2N-C(=O)NRQ2NC2 or

[1946] -S(=O)2R Q2NC.

[1947] (431) The compound according to any one of (1) to (429), wherein:

[1948] each -RQ2N, if present, is independently:

[1949] -RQ2NC,

[1950] -C(=O)RQ2NC,

[1951] -C(=O)-LQ2N-OH, -C(=O)-LQ2N-ORQ2NC,

[1952] -C(=O)-LQ2N-NH2, -C(=O)-LQ2N-NHRQ2NC, -C(=O)-LQ2N-NRQ2NC2, -C(=O)-LQ2N-RQ2NM,

[1953] -C(=O)ORQ2NC,

[1954] -C(=O)NH2, -C(=O)NHRQ2NC, -C(=O)NRQ2NC2, -C(=O)RQ2NM,

[1955] -LQ2N-C(=O)NH2, -L Q2N -C(=O)NHRQ2NC, -LQ2N-C(=O)NRQ2NC2 or -LQ2N-C(=O)RQ2NM.

[1956] (432) The compound according to any one of (1) to (429), wherein:

[1957] each -RQ2N is independently:

[1958] -RQ2NC,

[1959] -C(=O)RQ2NC,

[1960] -C(=O)-LQ2N-OH, -C(=O)-LQ2N-ORQ2NC,

[1961] -C(=O)-LQ2N-NH2, -C(=O)-LQ2N-NHRQ2NC, -C(=O)-LQ2N-NRQ2NC2, -C(=O)-LQ2N-RQ2NM,

[1962] -C(=O)NH2, -C(=O)NHRQ2NC, -C(=O)NRQ2NC2 or -C(=O)RQ2NM.

[1963] (433) The compound according to any one of (1) to (429), wherein:

[1964] each -RQ2N, if present, is independently:

[1965] -RQ2NC or

[1966] -C(=O)RQ2NC. Specification 70 / 530 pages 86 CN 121568936 A

[1967] (434) The compound according to any one of (1) to (429), wherein:

[1968] each -RQ2N, if present, is:

[1969] -C(=O)RQ2NC.

[1970] -RQ2NC group

[1971] (435) A compound according to any one of (1) to (434), wherein:

[1972] Each -RQ2NC, if present, is independently a straight-chain or branched saturated C1-6 alkyl, phenyl-C1-3 alkyl or C5-6 heteroaryl-C1-3 alkyl, wherein the C1-6 alkyl is optionally substituted with -OH, and each phenyl and heteroaryl is optionally substituted with one or more groups selected from -Cl and -OCH3.

[1973] (436) A compound according to any one of (1) to (434), wherein:

[1974] Each -RQ2NC, if present, is independently -Me, -Et, -t-Bu, t-pentyl, benzyl or pyridinylmethyl, wherein -Me, -Et, -t-Bu, t-pentyl is optionally substituted with -OH, and each phenyl and pyridinyl is optionally substituted with one or more groups selected from -Cl and -OCH3.

[1975] (437) The compound according to any one of (1) to (434), wherein:

[1976] each -RQ2NC, if present, is independently a straight-chain or branched saturated C1-6 alkyl, phenyl, phenyl-CH2-, pyridyl or pyridyl-CH2-, wherein the C1-6 alkyl is optionally substituted with -OH or -OCH3, and each phenyl and pyridyl is optionally substituted with one or more groups selected from the group consisting of -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[1977] (438) The compound according to any one of (1) to (434), wherein:

[1978] each -RQ2NC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-, wherein each phenyl is optionally substituted by one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[1979] (439) The compound according to any one of (1) to (434), wherein:

[1980] each -RQ2NC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-.

[1981] (440) The compound according to any one of (1) to (434), wherein:

[1982] each -RQ2NC, if present, is independently a straight-chain or branched saturated C1-4 alkyl.

[1983] (441) The compound according to any one of (1) to (434), wherein:

[1984] each -RQ2NC, if present, is:

[1985] -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[1986] (442) The compound according to any one of (1) to (434), wherein:

[1987] Each -RQ2NC, if present, is:

[1988] -Me, -Et, -nPr or -iPr.

[1989] (443) The compound according to any one of (1) to (434), wherein:

[1990] Each -RQ2NC, if present, is:

[1991] -Me or -Et.

[1992] (444) The compound according to any one of (1) to (434), wherein:

[1993] Each -RQ2NC, if present, is:

[1994] -Me.

[1995] -LQ2N- group

[1996] (445) The compound according to any one of (1) to (444), wherein:

[1997] Each -LQ2N-, if present, is independently -CH2-, -C(CH3)2-, -CH2CH2- or -CH2CH2CH2-. Specification 71 / 530 pages 87 CN 121568936 A

[1998] (446) The compound according to any one of (1) to (444), wherein:

[1999] each -LQ2N- is independently -CH2-, -CH2CH2- or -CH2CH2CH2- if present.

[2000] (447) The compound according to any one of (1) to (444), wherein:

[2001] each -LQ2N- is -CH2- if present.

[2002] (448) The compound according to any one of (1) to (444), wherein:

[2003] each -LQ2N- is -CH2CH2- if present.

[2004] (449) The compound according to any one of (1) to (444), wherein:

[2005] each -LQ2N- is -CH2CH2CH2- if present.

[2006] -RQ2NM group

[2007] (450) The compound according to any one of (1) to (449), wherein:

[2008] Each -RQ2NM, if present, is independently a non-aromatic C3-11 heterocyclic group having at least one N-ring atom and connected by said N-ring atom.

[2009] (451) The compound according to any one of (1) to (449), wherein:

[2010] Each -RQ2NM, if present, is independently a pyrrolidinyl or morpholinyl group connected by an N-ring atom.

[2011] (452) The compound according to any one of (1) to (449), wherein:

[2012] each -RQ2NM, if present, is independently an azircyclic butyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, azircyclic heptyl, or diazircyclic heptyl, and:

[2013] the carbon atom is optionally substituted by one or more -RQ2NMM groups; and

[2014] The secondary nitrogen atom, if present, is optionally substituted with a group selected from the following: -RQ2NMM, -C(=O)RQ2NMM, -C(=O)ORQ2NMM, -C(=O)NH2, -C(=O)NHRQ2NMM, -C(=O)NRQ2NMM2 and -S(=O)2RQ2NMM.

[2015] (453) The compound according to any one of (1) to (449), wherein:

[2016] each -RQ2NM is independently pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl if present, and:

[2017] the carbon atom is optionally substituted by one or more -RQ2NMM groups; and

[2018] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ2NMM, -C(=O)RQ2NMM, -C(=O)ORQ2NMM, -C(=O)NH2, -C(=O)NHRQ2NMM, -C(=O)NRQ2NMM2 and -S(=O)2RQ2NMM.

[2019] (454) The compound according to any one of (1) to (449), wherein:

[2020] each -RQ2NM is independently pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl if present, and:

[2021] the carbon atom is optionally substituted by one or more -RQ2NMM groups; and

[2022] the secondary nitrogen atom, if present, is optionally substituted by a group selected from -RQ2NMM, -C(=O)RQ2NMM and -C(=O)ORQ2NMM.

[2023] -RQ2NMM group

[2024] (455) The compound according to any one of (1) to (454), wherein:

[2025] Each -RQ2NMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-, wherein each phenyl is optionally substituted by one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[2026] (456) The compound according to any one of (1) to (454), wherein:

[2027] Each -RQ2NMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-.

[2028] (457) The compound according to any one of (1) to (454), wherein:

[2029] each -RQ2NMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl group. Specification 72 / 530 pages 88 CN 121568936 A

[2030] (458) The compound according to any one of (1) to (454), wherein:

[2031] each -RQ2NMM, if present, is:

[2032] -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[2033] (459) The compound according to any one of (1) to (454), wherein:

[2034] each -RQ2NMM, if present, is:

[2035] -Me, -Et, -nPr or -iPr.

[2036] (460) The compound according to any one of (1) to (454), wherein:

[2037] each -RQ2NMM, if present, is:

[2038] -Me or -Et.

[2039] (461) The compound according to any one of (1) to (454), wherein:

[2040] each -RQ2NMM, if present, is:

[2041] -Me.

[2042] -RQ3C group

[2043] (462) The compound according to any one of (1) to (461), wherein:

[2044] Each -RQ3C, if present, is independently:

[2045] -F,

[2046] -RQ3CC,

[2047] -RQ3CX,

[2048] -OH, -ORQ3CC,

[2049] -NHC(=O)RQ3CC,

[2050] -C(=O)NHRQ3CC, -C(=O)RQ3CM,

[2051] -S(=O)2RQ3CC or -S(=O)2RQ3CM;

[2052] and two adjacent -RQ3Cs, if present, can together form -NH-(CH2)q3C(O)(CH2)v3-O-, Wherein: q3 is 0 and v3 is 1.

[2053] (463) The compound according to any one of (1) to (461), wherein:

[2054] each -RQ3C, if present, is independently:

[2055] -F, -Cl, -Br, -I,

[2056] -RQ3CC,

[2057] -RQ3CX, -ORQ3CX,

[2058] -OH, -ORQ3CC,

[2059] -NH2, -NHRQ3CC, -NRQ3CC2, -RQ3CM,

[2060] -NHC(=O)RQ3CC, -NHC(=O)ORQ3CC,

[2061] -C(=O)NH2, -C(=O)NHRQ3CC, -C(=O)NRQ3CC2, -C(=O)RQ3CM,

[2062] ‑C(=O)OH, ‑C(=O)ORQ3CC,

[2063] ‑OC(=O)RQ3CC,

[2064] ‑OC(=O)NH2, ‑OC(=O)NHRQ3CC, ‑OC(=O)NRQ3CC2, ‑OC(=O)RQ3CM,

[2065] ‑CN or‑NO2;

[2066] Furthermore, two adjacent -RQ3C, if present, can together form -(CH2)n3-O-(CH2)m3- or -O-(CH2)p3-O. Specification 73 / 530 pages 89 CN 121568936 A

[2067] (464) The compound according to any one of (1) to (461), wherein:

[2068] Each -RQ3C, if present, is independently:

[2069] -F, -Cl, -Br, -I,

[2070] -RQ3CC,

[2071] -RQ3CX, -ORQ3CX,

[2072] -OH, -ORQ3CC,

[2073] -NH2, -NHRQ3CC, -NRQ3CC2 or -RQ3CM;

[2074] and two adjacent -RQ3Cs, if present, can together form -(CH2)n3-O-(CH2)m3- or -O-(CH2)p3-O.

[2075] (465) The compound according to any one of (1) to (461), wherein:

[2076] each -RQ3C, if present, is independently:

[2077] -F, -Cl, -Br, -I,

[2078] -RQ3CC,

[2079] -RQ3CX, -ORQ3CX,

[2080] -OH or -ORQ3CC.

[2081] The index "q3" in -(CH2)q3(C(O))-NH-(CH2)v3- and -NH-(CH2)q3C(O)(CH2)v3-O-.

[2082] (466) The compound according to any one of (1) to (465), wherein:

[2083] q3 is 0 if present.

[2084] (467) The compound according to any one of (1) to (465), wherein:

[2085] q3 is 1 if present.

[2086] (468) The compound according to any one of (1) to (465), wherein:

[2087] q3 is 2 if present.

[2088] (469) The compound according to any one of (1) to (465), wherein:

[2089] q3 is 3 if present.

[2090] The index “v3” in -(CH2)g3(C(O))-NH-(CH2)v3- and -NH-(CH2)q3C(O)(CH2)v3-O-.

[2091] (470) The compound according to any one of (1) to (469), wherein:

[2092] v3 is 0 if present.

[2093] (471) The compound according to any one of (1) to (469), wherein:

[2094] v3 is 1 if present.

[2095] (472) The compound according to any one of (1) to (469), wherein:

[2096] v3 is 2 if present.

[2097] (473) The compound according to any one of (1) to (469), wherein:

[2098] v3 is 3 if present.

[2099] -RQ3CC group

[2100] (474) The compound according to any one of (1) to (473), wherein:

[2101] Each -RQ3CC is independently a straight-chain or branched saturated C1-4 alkyl, C3-6 cycloalkyl or C3-7 heteroaryl if present, wherein the C1-4 alkyl is optionally substituted with -F.

[2102] (475) The compound according to any one of (1) to (473), wherein:

[2103] each -RQ3CC is independently -Me, -Et, -iPr-iBu, cyclopropyl or 4,5-dihydro-1,3-oxazolyl, if present, wherein -Me, -Et, -iPr or -iBu is optionally substituted with -F.

[2104] (476) The compound according to any one of (1) to (473), wherein:

[2105] each -RQ3CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-, wherein each phenyl is optionally substituted by one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[2106] (477) The compound according to any one of (1) to (473), wherein:

[2107] each -RQ3CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-.

[2108] (478) The compound according to any one of (1) to (473), wherein:

[2109] each -RQ3CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl.

[2110] (479) The compound according to any one of (1) to (473), wherein:

[2111] each -RQ3CC, if present, is:

[2112] -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[2113] (480) The compound according to any one of (1) to (473), wherein:

[2114] each -RQ3CC, if present, is:

[2115] -Me, -Et, -nPr or -iPr.

[2116] (481) The compound according to any one of (1) to (473), wherein:

[2117] each -RQ3CC, if present, is:

[2118] -Me or -Et.

[2119] (482) The compound according to any one of (1) to (473), wherein:

[2120] each -RQ3CC, if present, is:

[2121] -Me.

[2122] -RQ3CX group

[2123] (483) The compound according to any one of (1) to (482), wherein:

[2124] each -RQ3CX, if present, is independently a straight-chain or branched saturated C1-4 fluoroalkyl group.

[2125] (484) The compound according to any one of (1) to (482), wherein:

[2126] each -RQ3CX, if present, is independently -CF3, -CHF2, -CH2CF3 or -CH2CHF2.

[2127] (485) The compound according to any one of (1) to (482), wherein:

[2128] each -RQ3CX, if present, is -CF3.

[2129] -LQ3C- group

[2130] (486) The compound according to any one of (1) to (485), wherein:

[2131] Each -LQ3C- is independently -CH2-, -C(CH3)2-, -CH2CH2- or -CH2CH2CH2- if present.

[2132] (487) The compound according to any one of (1) to (485), wherein:

[2133] Each -LQ3C- is independently -CH2-, -CH2CH2- or -CH2CH2CH2- if present.

[2134] (488) The compound according to any one of (1) to (485), wherein:

[2135] Each -LQ3C- is -CH2- if present.

[2136] (489) The compound according to any one of (1) to (485), wherein:

[2137] each -LQ3C- is -CH2CH2- if present.

[2138] (490) The compound according to any one of (1) to (485), wherein:

[2139] each -LQ3C- is -CH2CH2CH2- if present. Specification 75 / 530 pages 91 CN 121568936 A

[2140] -RQ3CM group

[2141] (491) The compound according to any one of (1) to (490), wherein:

[2142] each -RQ3CM, if present, is independently a non-aromatic C3-11 heterocyclic group having at least one N ring atom and connected by the N ring atom; and:

[2143] the carbon atom is optionally substituted by one or more -RQ3CMM groups.

[2144] (492) The compound according to any one of (1) to (490), wherein:

[2145] each -RQ3CM, if present, is independently pyrrolidinyl or 2-azabicyclo[2.2.1]heptyl, and via NThe ring atoms are linked; and:

[2146] the carbon atoms are optionally substituted with one or more -RQ3CMM groups.

[2147] (493) The compound according to any one of (1) to (490), wherein:

[2148] each -RQ3CM is independently an azacyclobutane, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, azacycloheptane or diazacycloheptane, and:

[2149] the carbon atom is optionally substituted by one or more -RQ3CMM groups; and

[2150] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ3CMM, -C(=O)RQ3CMM, -C(=O)ORQ3CMM, -C(=O)NH2, -C(=O)NHRQ3CMM, -C(=O)NRQ3CMM2 and -S(=O)2RQ3CMM.

[2151] (494) The compound according to any one of (1) to (490), wherein:

[2152] each -RQ3CM, if present, is independently pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl, and:

[2153] the carbon atom is optionally substituted by one or more -RQ3CMM groups; and

[2154] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ3CMM, -C(=O)RQ3CMM, -C(=O)ORQ3CMM, -C(=O)NH2, -C(=O)NHRQ3CMM, -C(=O)NRQ3CMM2 and -S(=O)2RQ3CMM.

[2155] (495) The compound according to any one of (1) to (490), wherein:

[2156] each -RQ3CM is independently pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl if present, and:

[2157] the carbon atom is optionally substituted by one or more -RQ3CMM groups; and

[2158] the secondary nitrogen atom, if present, is optionally substituted by a group selected from -RQ3CMM, -C(=O)RQ3CMM and -C(=O)ORQ3CMM.

[2159] -RQ3CMM group

[2160] (496) The compound according to any one of (1) to (495), wherein:

[2161] Each -RQ3CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-, wherein each phenyl is optionally substituted by one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[2162] (497) The compound according to any one of (1) to (495), wherein:

[2163] Each -RQ3CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-.

[2164] (498) The compound according to any one of (1) to (495), wherein:

[2165] Each -RQ3CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl.

[2166] (499) The compound according to any one of (1) to (495), wherein:

[2167] Each -RQ3CMM, if present, is:

[2168] -Me, -Et, -nPr, -iPr, -nBu, or -tBu.

[2169] (500) The compound according to any one of (1) to (495), wherein:

[2170] each -RQ3CMM, if present, is: Specification 76 / 530 pages 92 CN 121568936 A

[2171] -Me, -Et, -nPr or -iPr.

[2172] (501) The compound according to any one of (1) to (495), wherein:

[2173] each -RQ3CMM, if present, is:

[2174] -Me or -Et.

[2175] (502) The compound according to any one of (1) to (495), wherein:

[2176] each -RQ3CMM, if present, is:

[2177] -Me.

[2178] (503) The compound according to any one of (1) to (495), wherein:

[2179] each of -RQ3CMM, if present, is:

[2180] -F.

[2181] (504) The indices “n3” and “m3” in -(CH2)n3-O-(CH2)m3- and -(CH2)n3-NH-(CH2)m3-

[2182] The compound according to any one of (1) to (503), wherein:

[2183] n3, if present, is 0, 1, 2 or 3;

[2184] m3, if present, is 0, 1, 2 or 3;

[2185] provided that m3+n3 is 2 or 3.

[2186] (505) The compound according to any one of (1) to (503), wherein:

[2187] n3 is 0, 1 or 2 if present;

[2188] m3 is 0, 1 or 2 if present;

[2189] provided that m3+n3 is 2 or 3.

[2190] (506) The compound according to any one of (1) to (503), wherein:

[2191] n3 is 1 or 2 if present;

[2192] m3 is 1 or 2 if present;

[2193] provided that m3+n3 is 2 or 3.

[2194] The index “p3” in -O-(CH2)p3-O- and -NH-(CH2)p3-NH-

[2195] (507) The compound according to any one of (1) to (503), wherein:

[2196] p3 is 1 if present.

[2197] (508) The compound according to any one of (1) to (503), wherein:

[2198] p3 is 2 if present.

[2199] -RQ4C group

[2200] (509) The compound according to any one of (1) to (508), wherein:

[2201] Each -RQ4C is independently:

[2202] -F,

[2203] -RQ4CC, -RQ4CX,

[2204] -OH, -ORQ4CC, -ORQ4CX,

[2205] -NH2, -NHRQ4CC, -NRQ4CC2 or -RQ4CM.

[2206] (510) The compound according to any one of (1) to (508), wherein:

[2207] each -RQ4C, if present, is independently:

[2208] -RQ4CC, -RQ4CX,

[2209] -OH, -ORQ4CC or -ORQ4CX. Specification 77 / 530 pages 93 CN 121568936 A

[2210] (511) The compound according to any one of (1) to (508), wherein:

[2211] each -RQ4C, if present, is independently:

[2212] -RQ4CC,

[2213] -OH or -ORQ4CC.

[2214] -RQ4CC group

[2215] (512) The compound according to any one of (1) to (511), wherein:

[2216] Each -RQ4CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, phenyl-C1-3 alkyl, C5-6 heteroaryl or C5-6 heteroaryl-C1-3 alkyl, wherein each phenyl and heteroaryl is optionally substituted by one or more groups selected from the group consisting of -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[2217] (513) The compound according to any one of (1) to (511), wherein:

[2218] each -RQ4CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-, wherein each phenyl is optionally substituted by one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[2219] (514) The compound according to any one of (1) to (511), wherein:

[2220] each -RQ4CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-.

[2221] (515) The compound according to any one of (1) to (511), wherein:

[2222] each -RQ4CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl group.

[2223] (516) The compound according to any one of (1) to (511), wherein:

[2224] each -RQ4CC, if present, is:

[2225] -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[2226] (517) The compound according to any one of (1) to (511), wherein:

[2227] each -RQ4CC, if present, is:

[2228] -Me, -Et, -nPr or -iPr.

[2229] (518) The compound according to any one of (1) to (511), wherein:

[2230] each -RQ4CC, if present, is:

[2231] -Me or -Et.

[2232] (519) The compound according to any one of (1) to (511), wherein:

[2233] each -RQ4CC, if present, is:

[2234] -Me.

[2235] -RQ4CX group

[2236] (520) The compound according to any one of (1) to (519), wherein:

[2237] each -RQ4CX, if present, is independently a straight-chain or branched saturated C1-4 fluoroalkyl group.

[2238] (521) The compound according to any one of (1) to (519), wherein:

[2239] each -RQ4CX is independently -CF3, -CHF2, -CH2CF3 or -CH2CHF2 if present.

[2240] (522) The compound according to any one of (1) to (519), wherein:

[2241] each -RQ4CX is -CF3 if present.

[2242] -RQ4CM group

[2243] (523) The compound according to any one of (1) to (522), wherein:

[2244] Each -RQ4CM, if present, is independently an azircyclic butyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, azircyclic heptyl or diazircyclic heptyl, and:

[2245] The carbon atom is optionally substituted by one or more -RQ4CMM groups; and

[2246] The secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ4CMM, -C(=O). RQ4CMM, ‑C(=O)ORQ4CMM, ‑C(=O)NH2, ‑C(=O)NHRQ4CMM, ‑C(=O)NRQ4CMM2 and ‑S(=O)2R Q4CMM.

[2247] (524) The compound according to any one of (1) to (522), wherein:

[2248] each -RQ4CM, if present, is independently pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl, and:

[2249] the carbon atom is optionally substituted by one or more -RQ4CMM groups; and

[2250] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ4CMM, -C(=O)RQ4CMM, -C(=O)ORQ4CMM, -C(=O)NH2, -C(=O)NHRQ4CMM, -C(=O)NRQ4CMM2 and -S(=O)2RQ4CMM.

[2251] (525) The compound according to any one of (1) to (522), wherein:

[2252] each -RQ4CM is independently pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl if present, and:

[2253] the carbon atom is optionally substituted by one or more -RQ4CMM groups; and

[2254] the secondary nitrogen atom, if present, is optionally substituted by a group selected from -RQ4CMM, -C(=O)RQ4CMM and -C(=O)ORQ4CMM.

[2255] -RQ4CMM group

[2256] (526) The compound according to any one of (1) to (522), wherein:

[2257] Each -RQ4CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-, wherein each phenyl is optionally substituted by one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[2258] (527) The compound according to any one of (1) to (522), wherein:

[2259] Each -RQ4CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-.

[2260] (528) The compound according to any one of (1) to (522), wherein:

[2261] each -RQ4CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl group.

[2262] (529) The compound according to any one of (1) to (522), wherein:

[2263] each -RQ4CMM, if present, is:

[2264] -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[2265] (530) The compound according to any one of (1) to (522), wherein:

[2266] each -RQ4CMM, if present, is:

[2267] -Me, -Et, -nPr or -iPr.

[2268] (531) The compound according to any one of (1) to (522), wherein:

[2269] Each -RQ4CMM, if present, is:

[2270] -Me or -Et.

[2271] (532) The compound according to any one of (1) to (522), wherein:

[2272] Each -RQ4CMM, if present, is:

[2273] -Me.

[2274] -RQ5C group

[2275] (533) The compound according to any one of (1) to (532), wherein:

[2276] Each -RQ5C, if present, is independently:

[2277] -OH, -ORQ5CC,

[2278] -NHC(=O)RQ5CC, -NHC(=O)ORQ5CC,

[2279] -C(=O)NH2, -C(=O)NHRQ5CC or -C(=O)RQ5CM.

[2280] (534) The compound according to any one of (1) to (532), wherein:

[2281] each -RQ5C, if present, is independently:

[2282] -OH, -ORQ5CC,

[2283] -NH2, -NHRQ5CC, -NRQ5CC2, -RQ5CM,

[2284] -NHC(=O)RQ5CC, -NHC(=O)ORQ5CC,

[2285] -C(=O)NH2, -C(=O)NHRQ5CC, -C(=O)NRQ5CC2, -C(=O)RQ5CM,

[2286] -OC(=O)NH2, -OC(=O)NHRQ5CC, -OC(=O)NRQ5CC2 or -OC(=O)RQ5CM.

[2287] (535) The compound according to any one of (1) to (532), wherein:

[2288] each -RQ5C, if present, is independently:

[2289] -OH, -ORQ5CC,

[2290] -NH2, -NHR Q5CC, -NRQ5CC2, -R Q5CM,

[2291] -NHC(=O)RQ5CC or -NHC(=O)ORQ5CC.

[2292] (536) The compound according to any one of (1) to (532), wherein:

[2293] each -RQ5C, if present, is independently:

[2294] -NH2, -NHR Q5CC, -NRQ5CC2, -R Q5CM,

[2295] -NHC(=O)RQ5CC or -NHC(=O)ORQ5CC.

[2296] (537) The compound according to any one of (1) to (532), wherein:

[2297] each -RQ5C, if present, is independently:

[2298] -NHC(=O)RQ5CC or -NHC(=O)ORQ5CC.

[2299] -RQ5CC group

[2300] (538) The compound according to any one of (1) to (537), wherein:

[2301] Each -RQ5CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl or phenyl-CH2-, wherein each phenyl is optionally substituted by one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[2302] (539) The compound according to any one of (1) to (537), wherein:

[2303] Each -RQ5CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl or phenyl-CH2-.

[2304] (540) The compound according to any one of (1) to (537), wherein:

[2305] each -RQ5CC, if present, is independently a straight-chain or branched saturated C1-4 alkyl group.

[2306] (541) The compound according to any one of (1) to (537), wherein:

[2307] each -RQ5CC, if present, is:

[2308] -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[2309] (542) The compound according to any one of (1) to (537), wherein:

[2310] each -RQ5CC, if present, is:

[2311] -Me, -Et or -tBu.

[2312] (543) The compound according to any one of (1) to (537), wherein:

[2313] each -RQ5CC, if present, is:

[2314] -Me, -Et, -nPr or -iPr. Specification 80 / 530 pages 96 CN 121568936 A

[2315] (544) The compound according to any one of (1) to (537), wherein:

[2316] each -RQ5CC, if present, is:

[2317] -Me or -Et.

[2318] (545) The compound according to any one of (1) to (537), wherein:

[2319] each -RQ5CC, if present, is:

[2320] -Me.

[2321] -RQ5CM group

[2322] (546) The compound according to any one of (1) to (545), wherein:

[2323] Each -RQ5CM, if present, is independently a non-aromatic C3-11 heterocyclic group having at least one N ring atom and connected by the N ring atom; and:

[2324] (547) The compound according to any one of (1) to (545), wherein:

[2325] Each -RQ5CMIf present, it is independently azacyclobutane, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, azacycloheptane, or diazacycloheptane, and:

[2326] the carbon atom is optionally substituted by one or more -RQ5CMM groups; and

[2327] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ5CMM, -C(=O)RQ5CMM, -C(=O)ORQ5CMM, -C(=O)NH2, -C(=O)NHRQ5CMM, -C(=O)NRQ5CMM2, and -S(=O)2RQ5CMM.

[2328] (548) The compound according to any one of (1) to (545), wherein:

[2329] each -RQ5CM is independently pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl if present, and:

[2330] the carbon atom is optionally substituted by one or more -RQ5CMM groups; and

[2331] the secondary nitrogen atom, if present, is optionally substituted by a group selected from: -RQ5CMM, -C(=O)RQ5CMM, -C(=O)ORQ5CMM, -C(=O)NH2, -C(=O)NHRQ5CMM, -C(=O)NRQ5CMM2 and -S(=O)2RQ5CMM.

[2332] (549) The compound according to any one of (1) to (545), wherein:

[2333] each -RQ5CM, if present, is independently pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl, and:

[2334] the carbon atom is optionally substituted by one or more -RQ5CMM groups; and

[2335] the secondary nitrogen atom, if present, is optionally substituted by a group selected from -RQ5CMM, -C(=O)RQ5CMM and -C(=O)ORQ5CMM.

[2336] (550) The compound according to any one of (1) to (545), wherein:

[2337] each -RQ5CM, if present, is independently morpholinyl.

[2338] -RQ5CMM group

[2339] (551) The compound according to any one of (1) to (550), wherein:

[2340] Each -RQ5CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-, wherein each phenyl is optionally substituted by one or more groups selected from: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

[2341] (552) The compound according to any one of (1) to (550), wherein:

[2342] Each -RQ5CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl, phenyl, or phenyl-CH2-.

[2343] (553) The compound according to any one of (1) to (550), wherein:

[2344] each -RQ5CMM, if present, is independently a straight-chain or branched saturated C1-4 alkyl group.

[2345] (554) The compound according to any one of (1) to (550), wherein:

[2346] each -RQ5CMM, if present, is: Specification 81 / 530 pages 97 CN 121568936 A

[2347] -Me, -Et, -nPr, -iPr, -nBu or -tBu.

[2348] (555) The compound according to any one of (1) to (550), wherein:

[2349] each -RQ5CMM, if present, is:

[2350] -Me, -Et, -nPr or -iPr.

[2351] (556) The compound according to any one of (1) to (550), wherein:

[2352] each -RQ5CMM, if present, is:

[2353] -Me or -Et.

[2354] (557) The compound according to any one of (1) to (550), wherein:

[2355] each -RQ5CMM, if present, is:

[2356] -Me.

[2357] Some preferred combinations

[2358] (558) The compound according to any one of (1) to (557), if applicable, wherein:

[2359] -RA3 is -H; and

[2360] -RA4 is -H.

[2361] For example, ring A is:

[2362]

[2363] (559) the compound according to any one of (1) to (557), wherein, if applicable,:

[2364] -RA1 is -RA11, -RA11 is -RA111 and -RA111 is -Me;

[2365] -RA2 is -RA22, -RA22 is -RA222 and -RA222 is -Me;

[2366] -RA3 is -H; and

[2367] -RA4 is -H.

[2368] For example, ring A is:

[2369]

[2370] (560) the compound according to any one of (1) to (557), wherein, if applicable, ring B is:

[2371] Y1 is S;

[2372] Y2 is CH or CRY2;

[2373] Y3 is N;

[2374] -RA1 is -RA11, -RA11 is -RA111 and -RA111 is -Me;

[2375] -RA2 is -RA22, -RA22 is -RA222 and -RA222 is -Me; Specification 82 / 530 pages 98 CN 121568936 A

[2376] -RA3 is -H; and

[2377] -RA4 is -H.

[2378] For example, the compound is a compound having the following structural formula:

[2379]

[2380] (561) the compound according to any one of (1) to (557), wherein, if applicable, the following is true:

[2381] ring B is

[2382] -RA1 is -RA11, -RA11 is -RA111 and -RA111 is -Me;

[2383] -RA2 is -RA22, -RA22 is -RA222 and -RA222 is -Me;

[2384] -RA3 is -H;

[2385] -RA4 is -H; and

[2386] -Q is -Q1.

[2387] For example, the compound is a compound having the following structural formula:

[2388]

[2389] (562) The compound according to any one of (1) to (557), wherein, if applicable, the following is true:

[2390] Ring B is

[2391] -RA1 is -RA11, -RA11 is -RA111 and -RA111 is -Me;

[2392] -RA2 is -RA22, -RA22 is -RA222 and -RA222 is -Me;

[2393] -RA3 is -H;

[2394] -RA4 is -H;

[2395] -Q is -Q1; and

[2396] -Q1 is pyrazolyl and:

[2397] The carbon atom is optionally substituted by one or more -RQ1C groups; and

[2398] The secondary nitrogen atom is optionally substituted by -RQ1N if present.

[2399] (563) The compound according to any one of (1) to (557), wherein, if applicable,:

[2400] Ring B is specified in the specification 83 / 530 page 99 CN 121568936 A

[2401] -RA1 is -RA11, -RA11 is -RA111 and -RA111 is -Me;

[2402] -RA2 is -RA22, -RA22 is -RA222 and -RA222 is -Me;

[2403] -RA3 is -H;

[2404] -RA4 is -H;

[2405] -Q is -Q1; and

[2406] -Q1 is 1H-pyrazole-3-yl, and:

[2407] The carbon atom is optionally substituted by one or more -RQ1C groups; and

[2408] The secondary nitrogen atom is substituted by -RQ1N.

[2409] For example, the compound is a compound having the following structural formula:

[2410]

[2411] (564) the compound according to any one of (1) to (557), wherein, if applicable,:

[2412] ring B is

[2413] -Q is -Q1; and

[2414] -Q1 is pyridyl and:

[2415] carbon atoms are optionally substituted by one or more -RQ1C groups; and

[2416] The secondary nitrogen atom is replaced by -RQ1N.

[2417] (565) The compound according to any one of (1) to (557), wherein, if applicable,:

[2418] ring B is

[2419] -RA1 is -RA11, -RA11 is -RA111 and -RA111 is -Me;

[2420] -RA2 is -RA22, -RA22 is -RA222 and -RA222 is -Me;

[2421] -RA3 is -H;

[2422] -RA4 is -H;

[2423] -Q is -Q1; and

[2424] -Q1 is 1H-pyrazole-3-yl, and:

[2425] carbon atoms are optionally substituted by one or more -RQ1C groups; and

[2426] secondary nitrogen atoms are substituted by -RQ1N;

[2427] wherein:

[2428] -RQ1N is -RQ1NC, -RQ1Nhet, -LQ1N-C(=O)RQ1NP or -LQ1N-C(=O)NRQ1NC2.

[2429] (566) The compound according to any one of (1) to (557), wherein, if applicable, the following are provided:

[2430] Ring B is

[2431] -RA1 is -RA11, -RA11 is -RA111 and -RA111 is -Me;

[2432] -RA2 is -RA22, -RA22 is -RA222 and -RA222 is -Me;

[2433] -RA3 is -H;

[2434] -RA4 is -H;

[2435] -Q is -Q1; and

[2436] -Q1 is 1H-pyrazole-3-yl, and:

[2437] The carbon atom is optionally substituted by one or more -RQ1C groups; and

[2438] The secondary nitrogen atom is substituted by -RQ1N;

[2439] Wherein:

[2440] -RQ1N is -LQ1N-C(=O)RQ1NP; and

[2441] -LQ1N- is -CH2-.

[2442] For example, the compound is a compound having the following structural formula:

[2443]

[2444] (567) The compound according to any one of (1) to (557), wherein, if applicable,:

[2445] Ring B is

[2446] -RA1 is -RA11, -RA11 is -RA111 and -RA111 is -Me;

[2447] -RA2 is -RA22, -RA22 is -RA222 and -RA222 is -Me;

[2448] -RA3 is -H;

[2449] -RA4 is -H;

[2450] -Q is -Q1; and

[2451] -Q1 is 1H-pyrazole-3-yl, and:

[2452] The carbon atom is optionally substituted with one or more -RQ1C groups; and

[2453] the secondary nitrogen atom is substituted with -RQ1N;

[2454] wherein:

[2455] -RQ1N is -RQ1NC.

[2456] For example, the compound is a compound having the following structural formula: Specification 85 / 530 pages 101 CN 121568936 A

[2457]

[2458] (568) The compound according to any one of (1) to (557), wherein, if applicable, ring B is

[2459] -RA1 is -RA11, -RA11 is -RA111 and -RA111 is -Me;

[2460] -RA2 is -RA22, -RA22 is -RA222 and -RA222 is -Me;

[2461] -RA3 is -H;

[2462] -RA4-H;

[2463] -Q is -Q1; and

[2464] -Q1 is 1H-pyrazol-3-yl, and:

[2465] The secondary nitrogen atom is substituted by -RQ1N;

[2466] wherein:

[2467] -RQ1N is -RQ1Nhet.

[2468] For example, the compound is a compound having the following structural formula:

[2469]

[2470] Some specific examples

[2471] (569) According to the compound of (1), selected from compounds represented by the following formula and their pharmaceutically acceptable salts and solvates (e.g., their pharmaceutically acceptable salts):

[2472] Specification 86 / 530 pages 102 CN 121568936 A

[2473] Specification 87 / 530 pages 103 CN 121568936 A

[2474] Specification 88 / 530 pages 104 CN 121568936 A

[2475] Specification 89 / 530 pages 105 CN 121568936 A

[2476] Specification 90 / 530 pages 106 CN 121568936 A

[2477] Specification 91 / 530 pages 107 CN 121568936 A

[2478] Specification 92 / 530 pages 108 CN 121568936 A

[2479] Specification 93 / 530 pages 109 CN 121568936 A

[2480] Specification 94 / 530 pages 110 CN 121568936 A

[2481] Specification 95 / 530 pages 111 CN 121568936 A

[2482] Specification 96 / 530 pages 112 CN 121568936 A

[2483] Specification97 / 530 pages, 113 CN 121568936 A

[2484] Specification 98 / 530 pages, 114 CN 121568936 A

[2485] Specification 99 / 530 pages, 115 CN 121568936 A

[2486] Specification 100 / 530 pages, 116 CN 121568936 A

[2487] Specification 101 / 530 pages, 117 CN 121568936 A

[2488] Specification 102 / 530 pages, 118 CN 121568936 A

[2489] Specification 103 / 530 pages, 119 CN 121568936 A

[2490] Specification 104 / 530 pages, 120 CN 121568936 A

[2491] Instruction manual 105 / 530 pages 121 CN 121568936 A

[2492] Instruction manual 106 / 530 pages 122 CN 121568936 A

[2493] Instruction manual 107 / 530 pages 123 CN 121568936 A

[2494] Instruction manual 108 / 530 pages 124 CN 121568936 A

[2495] Instruction manual 109 / 530 pages 125 CN 121568936 A

[2496] Instruction manual 110 / 530 pages 126 CN 121568936 A

[2497] Instruction manual 111 / 530 pages 127 CN 121568936 A

[2498] Instruction manual 112 / 530 pages 128 CN 121568936 A

[2499] Specification 113 / 530 pages 129 CN 121568936 A

[2500] Specification 114 / 530 pages 130 CN 121568936 A

[2501] Specification 115 / 530 pages 131 CN 121568936 A

[2502] Specification 116 / 530 pages 132 CN 121568936 A

[2503] Specification 117 / 530 pages 133 CN 121568936 A

[2504]

[2505] In one embodiment, the BAA compound can be obtained (or acquired) by the methods described in the following experimental section.

[2506] In one embodiment, according to any of the embodiments described herein (e.g., embodiments (1), (2) or(3); or claim 1) provides a BAA compound, provided that any specific example is excluded individually. For example, a further feature is any embodiment described herein (e.g., embodiment (1), (2), or (3); or claim 1), provided that any (e.g., any one, any two, or any three) compounds in the foregoing table are excluded individually.

[2507] In one embodiment, a BAA compound is provided according to any embodiment described herein (e.g., embodiment (1), (2), or (3); or claim 1), provided that any other embodiment described herein is specifically excluded.

[2508] Combination

[2509] It will be understood that some features of the invention (which are described in separate embodiments for clarity) may also be provided in combination in a single embodiment. Conversely, various features of the invention (described in the content of a single embodiment for brevity) may also be provided separately or in any suitable sub-combination. This invention specifically covers all combinations of embodiments relating to the chemical groups (e.g., ring A, ring B, etc.) represented by the variables, and is disclosed herein as each and each combination is disclosed individually and explicitly, such that the compounds covered by these combinations are stable compounds (i.e., compounds that can be isolated, characterized and tested for their biological activity). In this case, it will be readily understood by those skilled in the art that combinations of some groups (e.g., substituents) may produce compounds that are difficult to synthesize and / or chemically unstable. Furthermore, all sub-combinations of the chemical groups listed in the embodiments describing such variables are also specifically covered by this invention and are disclosed herein as each and each sub-combination of such chemical groups is disclosed herein as each and each sub-combination of such chemical groups is disclosed herein as each and each sub-combination of such chemical groups is disclosed individually and explicitly.

[2510] Substantially Purified Form

[2511] One aspect of this invention relates to BAA compounds as described herein, which are present in a substantially purified form and / or in a substantially impurity-free form.

[2512] In one embodiment, the substantially purified form is at least 50% by weight, for example at least 60% by weight, for example at least 70% by weight, for example at least 80% by weight, for example at least 90% by weight, for example at least 95% by weight, for example at least 97% by weight, for example at least 98% by weight, for example at least 99% by weight.

[2513] Unless otherwise stated, the substantially purified form refers to a compound existing in any stereoisomer or enantiomer form. For example, in one embodiment, the substantially purified form refers to a mixture of stereoisomers, i.e., purified relative to other compounds. In one embodiment, the substantially purified form refers to a stereoisomer. (Specification 118 / 530 pages 134 CN 121568936 A)Isomers, such as optically pure stereoisomers. In one embodiment, substantially purified form refers to a mixture of enantiomers. In one embodiment, substantially purified form refers to an equimolar mixture of enantiomers (i.e., a racemic mixture, a racemic mixture). In one embodiment, substantially purified form refers to one enantiomer, such as an optically pure enantiomer.

[2514] In one embodiment, the contaminant is equivalent to no more than 50% by weight, for example, no more than 40% by weight, for example, no more than 30% by weight, for example, no more than 20% by weight, for example, no more than 10% by weight, for example, no more than 5% by weight, for example, no more than 3% by weight, for example, no more than 2% by weight, for example, no more than 1% by weight.

[2515] Unless otherwise stated, contaminant refers to other compounds, i.e., compounds other than stereoisomers or enantiomers. In one embodiment, contaminant refers to other compounds and other stereoisomers. In one embodiment, contaminant refers to other compounds and other enantiomers.

[2516] In one embodiment, the substantially purified form is at least 60% optically pure (i.e., based on 1 mole, 60% of the compound is the desired stereoisomer or enantiomer and 40% is the undesirable stereoisomer or enantiomer), for example at least 70% optically pure, for example at least 80% optically pure, for example at least 90% optically pure, for example at least 95% optically pure, for example at least 97% optically pure, for example at least 98% optically pure, for example at least 99% optically pure.

[2517] Isomers

[2518] Some compounds may exist in one or more specific geometric, optical, enantiomers, diastereomers, epimers, steatomers, tautomers, conformational isomers or anomers, including but not limited to cis and trans forms; E- and Z-forms; c-, t- and r-forms; endogenous and exogenous forms; R-, S- and intermediate forms; D- and L-forms; d- and 1-forms; (+) and (-) forms; ketone, enol and enolate forms; cis and trans forms; synclinal and anticline forms; α- and β-forms; axial and latitudinal forms; boat-, chair-, torsion boat-, envelope- and half-chair-forms; and combinations thereof, hereinafter collectively referred to as “isomers” (or “isomeric forms”).

[2519] When referring to a class of structures, structural isomers belonging to that class are usually also included (e.g., C1-6 alkyl includes n-propyl and isopropyl; butyl includes n-butyl, isobutyl, sec-butyl, and tert-butyl; methoxyphenyl includes ortho, meta, and para-methoxyphenyl).

[2520] However, when referring to a particular group or substitution form, it is not intended to include other structures (or structural isomers) that differ in the connection between atoms rather than in spatial position. For example, methoxy(-OCH3) is mentioned.When referring to a chlorophenyl, it does not mean that it refers to its structural isomer, hydroxymethyl (CH2OH). Similarly, when explicitly mentioned, ortho-chlorophenyl does not mean that it refers to its structural isomer, meta-chlorophenyl.

[2521] The above exclusions do not apply to tautomeric forms, such as ketone, enol, and enolate forms, as in, for example, the following tautomeric pairs: ketone / enol (as shown below), imine / enamine, amide / imino alcohol, amidine / amidinium, nitroso / oxime, thione / ethanethiol, N-nitroso / hydroxyazo, and nitro / isonitroso. When one tautomeric form is mentioned herein, it is intended to cover both tautomeric forms.

[2522]

[2523] For example, 1H-pyridin-2-one-5-yl and 2-hydroxy-pyridin-5-yl (as shown below) are tautomeric forms of each other. When one is mentioned herein, it is intended to cover both structures. Specification 119 / 530 pages 135 CN 121568936 A

[2524]

[2525] Note that the term “isomer” specifically includes compounds having one or more isotopic substitutions. For example, H can exist in any isotopic form, including 1H, 2H(D), and 3H(T); C can exist in any isotopic form, including 12C, 13C, and 14C; O can exist in any isotopic form, including 16O and 18O; and so on.

[2526] Unless otherwise stated, references to a particular compound include all such isomer forms, including mixtures thereof (e.g., racemic mixtures). Methods for the preparation (e.g., asymmetric synthesis) and separation (e.g., fractional crystallization and chromatographic means) of such isomer forms are known in the art or readily obtained in a known manner by applying the methods taught herein or known methods.

[2527] Unless otherwise stated, references to a particular compound include all such isomer forms, including mixtures thereof (e.g., racemic mixtures). Methods for the preparation (e.g., asymmetric synthesis) and separation (e.g., fractional distillation crystallization and chromatographic means) of such isomer forms are known in the art or readily obtained in a known manner by applying the methods taught herein or known methods.

[2528] Salts

[2529] Relevant salts of the said compounds, such as pharmaceutically acceptable salts, can be readily prepared, purified, and / or treated as needed. The term "salt" as used herein refers to a solid complex comprising a first co-forming entity (e.g., a compound such as a BAA compound) and a second co-forming entity (e.g., a suitable Brønsted acid or base), wherein a proton is completely transferred from one entity to the other. Examples of pharmaceutically acceptable salts are found in the literature "Berge et al., 1977," Pharmaceutically AcceptableSalts, “J. Pharm. Sci., Vol. 66, pp. 1–19”, are discussed.

[2530] For example, if the compound is anionic or has a functional group that can be anionic (e.g., -COOH can be -COO-), then it can form a salt with a suitable cation. Examples of suitable inorganic cations include, but are not limited to, alkali metal ions (such as Na+ and K+), alkaline earth metal cations (such as Ca2+ and Mg2+) and other cations (such as Al3+) and ammonium ions (i.e., NH4+). Examples of suitable organic cations include, but are not limited to, substituted ammonium ions (e.g., NH3R+, NH2R2+, NHR3+, NR4+), wherein each R is independently a straight-chain or branched saturated C1–18 alkyl, C3–8 cycloalkyl, C3–8 cycloalkyl-C1–6-alkyl, and phenyl-C1–6 alkyl, wherein the phenyl is optionally substituted. Examples of suitable substituted ammonium ions are those derived from: ethylamine, diethylamine, dicyclohexylamine, triethylamine, butylamine, ethylenediamine, ethanolamine, diethanolamine, piperazine, benzylamine, phenylbenzylamine, choline, meglumine, and tromethamine, as well as amino acids such as lysine and arginine. A common example of a quaternary ammonium ion is N(CH3)4+.

[2531] If the compound is cationic, or has a functional group that becomes a cation upon protonation (e.g., -NH2 can become -NH3+), then it can form a salt with a suitable anion.

[2532] For example, if the bulk structure contains a cationic group (e.g., -NMe2+), or has a functional group that becomes a cation upon protonation (e.g., -NH2+ can become -NH3+), then it can form a salt with a suitable anion. In the case of quaternary ammonium compounds, an anti-anion is usually always present to balance the positive charge. If, in addition to cationic groups (e.g., -NMe2+, -NH3+), the compound also contains groups capable of forming anions (e.g., -COOH), then an inner salt (also called a zwitterion) can be formed.

[2533] Examples of suitable inorganic anions include, but are not limited to, anions derived from the following inorganic acids: hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, sulfurous acid, nitric acid, nitrous acid, phosphoric acid, and phosphorous acid.

[2534] Examples of suitable organic anions include, but are not limited to, anions derived from the following organic acids: 2-acetoxybenzoic acid, acetic acid, trifluoroacetic acid, ascorbic acid, aspartic acid, benzoic acid, camphor sulfonic acid, cinnamic acid, citric acid, edetate, 1,2-ethanedisulfonic acid, ethyl sulfonic acid, fumaric acid, glucoheptanoic acid, gluconic acid, glutamic acid, glycolic acid, hydroxymaleic acid, hydroxyl...Naphthalenecarboxylic acid, hydroxyethanesulfonic acid, lactic acid, lactobionic acid, lauric acid, maleic acid, malic acid, methanesulfonic acid, viscous acid, oleic acid, oxalic acid, palmitic acid, pamoic acid, pantothenic acid, phenylacetic acid, benzenesulfonic acid, propionic acid, pyruvic acid, salicylic acid, stearic acid, succinic acid, sulfanilic acid, tartaric acid, toluenesulfonic acid, and valeric acid. Examples of suitable polymeric organic anions include, but are not limited to, those derived from the following polymeric acids: tannic acid, carboxymethyl cellulose.

[2535] Examples of suitable counterions, especially those suitable for quaternary ammonium compounds (e.g., those with -NMe2+ groups), include 1-adamantanesulfonate, benzenesulfonate, hydrogen sulfate, bromide, chloride, iodide, methanesulfonate, methyl sulfate, 1,5-naphthalenedisulfonate, 4-nitrobenzenesulfonate, formate, tartrate, toluenesulfonate, trifluoroacetate, trifluoromethanesulfonate, and sulfate. Furthermore, if the compound also contains a group capable of forming an anion (e.g., -COOH), an inner salt may be formed.

[2536] Unless otherwise stated, references to a particular compound also include its salt form.

[2537] In one embodiment, the BAA compound is provided in the form of a salt.

[2538] In one embodiment, the BAA compound is provided in a neutral form (e.g., as a free acid, free base, or zwitterion).

[2539] Solvates and Hydrates

[2540] The corresponding solvates of the compound can be conveniently prepared, purified, and / or treated as needed. The term "solvate" as used herein refers to a complex of a solute (e.g., a compound, a salt of a compound) and a solvent in its conventional sense. If the solvent is water, the solvate may be conveniently referred to as a hydrate, such as a monohydrate, dihydrate, trihydrate, etc.

[2541] Unless otherwise stated, references to a particular compound also include its solvate and hydrate forms.

[2542] In one embodiment, the BAA compound is provided in the form of a solvate.

[2543] In one embodiment, the BAA compound is provided as a hydrate.

[2544] In one embodiment, the BAA compound is provided as a non-solventized form.

[2545] Chemically Protected Form

[2546] A chemically protected form of the compound can be readily prepared, purified, and / or treated as needed. The term "chemically protected form" as used herein, understood in a conventional chemical context, refers to a compound in which one or more reactive functional groups are protected from undesirable chemical reactions under specific conditions (such as pH, temperature, radiation, solvent, reactive chemical reagents, etc.). In practice, well-known chemical methods are used to reversibly render otherwise reactive functional groups non-reactive under specific conditions. In a chemically protected form, one or more reactive functional groups are present as protected or protecting groups (or masked or shielding groups, blocked or blocking groups). By protecting the reactive functional groups…Protecting groups can undergo reactions involving other unprotected reactive functional groups without affecting the protected group; protecting groups can be removed, or masking groups can be transformed, usually in subsequent steps, with little effect on the rest of the molecule. See, for example, Protecting Groups in Organic Synthesis (T. Green and P. Wuts; 4th ed.; John Wiley, 2006).

[2547] In organic synthesis, a wide variety of such “protection,” “blocking,” or “masking” methods are widely used and known to the public. For example, a compound containing two unequal reactive functional groups that are reactive under certain conditions can be derivatized so that one of the functional groups is “protected” and thus not reactive under certain conditions; thus, the compound can be used as a reactant with only one reactive functional group. After the desired reaction (involving the other functional group) is completed, the protecting group can be “deprotected” to restore its original function.

[2548] For example, the hydroxyl group can be protected as an ether (OR) or an ester (OC(=O)R), such as: tert-butyl ether; benzyl ether, diphenylmethyl (diphenylmethyl) ether or triphenylmethyl (triphenylmethyl) ether; trimethylsilyl or tert-butyldimethylsilyl ether; or acetyl ester (-OC(=O)CH3, OAc).

[2549] For example, the aldehyde or ketone group can be protected as an acetal (R-CH(OR)2) or a ketal (R2C(OR)2), respectively, wherein the carbonyl group (>C=O) is converted to a 1,1-diether (>C(OR)2) by reacting with, for example, a primary alcohol in the presence of an acid. The aldehyde or ketone group can be readily regenerated, for example, by hydrolysis with water in the presence of an acid.

[2550] For example, the amino group can be protected, for example, in the form of an amide (NRCO-R), such as acetamide (-NHCO-CH3); or in the form of a carbamate (-NRCO-OR), such as benzyloxycarbamate (-NHCO-OCH2C6H5, - NH-Cbz), tert-butoxycarbamate (-NHCO-OC(CH3)3, -NH-Boc); 2-biphenyl-2-propoxycarbamate (-NHCO-OC(CH3)2C6H4C6H5, NH-Bpoc), 9-fluorenylmethoxycarbamate (-NH-Fmoc), 6-nitrocinnamoxycarbamate (-NH-Nvoc), 2-trimethylsilylethoxycarbamate (-NH-Teoc), 2,2,2-trichloroethoxycarbamate (-NH-Troc), allyloxyamide (-NH-Alloc), or 2-(benzenesulfonyl)ethoxycarbamate.Ester (-NH-Psec); or, in suitable cases (e.g., cyclic amines), in the form of nitrooxy radical (>N-O·); or, in suitable cases (e.g., heterocyclic nitrogen), in the form of 2-trimethylsilylethoxymethyl (N-SEM).

[2551] For example, the carboxylic acid group can be protected in the form of an ester, such as: C1-7 alkyl ester (e.g., methyl ester; tert-butyl ester); C1-7 haloalkyl ester (e.g., 2,2,2-trihaloethyl ester); 2-tris(C1-7 alkyl)silyl-ethyl ester; or C5-20 aryl-C1-7 alkyl ester (e.g., benzyl ester; nitrobenzyl ester); or protected in the form of an amide or hydrazide, such as acetamide or N,N,N′-trimethylhydrazide.

[2552] For example, the thiol group can be protected in the form of a thioether (-SR), such as: benzyl thioether; acetamidomethyl ether (-S-CH2NHC(=O)CH3).

[2553] Prodrugs

[2554] The compounds described herein can be conveniently prepared, purified, and / or processed as needed. As used herein, the term "prodrug" refers to a compound that can produce the desired activity in vivo. Typically, prodrugs are inactive or have less activity than the desired activity of the compound, but can provide advantageous treatment, administration, or metabolic properties.

[2555] For example, some prodrugs are esters of active compounds (e.g., physiologically acceptable and metabolically unstable esters). During metabolism, the ester group (-C(=O)OR) is broken down, resulting in the active drug. Such esters can be formed by esterification reactions, for example, by pre-protecting any carboxylic acid groups (-C(=O)OH) in the bulk compound using any other active groups present in the bulk compound, and then deprotecting them as needed.

[2556] In addition, some prodrugs are activated by an enzymatic process to produce an active compound, or the compound produces an active compound through a further chemical reaction (e.g., as in antibody-guided enzyme prodrug therapy (ADEPT), gene-guided enzyme prodrug therapy (GDEPT), ligand-guided enzyme prodrug therapy (LIDEPT), etc.). For example, the prodrug can be a sugar derivative or other glycoside conjugate, or an amino acid ester derivative.

[2557] Composition

[2558] A composition (e.g., a pharmaceutical composition) comprising a BAA compound as described herein and a pharmaceutically acceptable carrier, diluent, or excipient is also described herein. Specification 122 / 530 pages 138 CN 121568936 A

[2559] A method for preparing a composition (e.g., a pharmaceutical composition) is also described herein, comprising mixing a BAA compound as described herein with a pharmaceutically acceptable carrier, diluent, or excipient.

[2560] Use

[2561] As described herein, BAA compounds are capable of inhibiting PKMYT1 (e.g., inhibiting or reducing or blocking the activity or function of PKMYT1).

[2562] Therefore, BAA compounds as described herein can be used, for example, to treat conditions (e.g., diseases) that can be improved by inhibiting PKMYT1 (e.g., by inhibiting or reducing or blocking the activity or function of PKMYT1).

[2563] Use in methods of inhibiting PKMYT1

[2564] A method of inhibiting PKMYT1 (e.g., inhibiting or reducing or blocking the activity or function of PKMYT1) in vitro or in vivo is also described herein, the method comprising contacting PKMYT1 with an effective amount of the BAA compound described herein.

[2565] A method of inhibiting PKMYT1 (e.g., inhibiting or reducing or blocking the activity or function of PKMYT1) in cells (in vitro or in vivo) is also described herein, the method comprising contacting cells with an effective amount of the BAA compound described herein.

[2566] In one embodiment, the method is carried out in vitro.

[2567] In one embodiment, the method is carried out in vivo.

[2568] In one embodiment, the BAA compound is provided in the form of a pharmaceutically acceptable composition.

[2569] Those skilled in the art can readily determine whether a candidate compound inhibits PKMYT1 (e.g., inhibits or reduces or blocks the activity or function of PKMYT1). For example, suitable assays are described herein, and / or such methods are known in the art.

[2570] Those skilled in the art can readily determine whether a candidate compound inhibits PKMYT1 in cells (e.g., inhibits or reduces or blocks or inhibits the activity or function of PKMYT1). For example, cell samples can be grown in vitro, and the compound can be contacted with these cells, and the effect of the compound on these cells can be observed. As an example of “effect,” the morphological state of the cells (e.g., survival or death, etc.) can be determined. If the compound is found to have an effect on the cells, this can serve as a prognostic or diagnostic marker of the efficacy of the compound in a method of treating a subject (e.g., a patient) carrying the same cell type. As another example of “effect,” the direct interaction between the compound and an intracellular target can be measured using, for example, colorimetric, fluorescence, or luminescent readings (e.g., “target binding assay”).

[2571] Use in methods such as inhibiting cell proliferation

[2572] The BAA compounds described herein can, for example: (a) regulate (e.g., inhibit) cell proliferation; (b) inhibit cell cycle progression; (c) promote apoptosis; (d) reduce colony formation; (e) slow the growth or self-renewal of tumor spheroids; (f) enhance the cytotoxic effect of DNA damaging agents; or (g) a combination of one or more of the above.

[2573] Therefore, the text also describes a method for regulating (e.g., inhibiting) cell proliferation, inhibiting cell cycle progression, promoting apoptosis, reducing colony formation, reducing tumor spheroid growth or self-renewal, or a combination of one or more of the above, in vitro or in vivo, the method comprising contacting cells with an effective amount of the BAA compound described herein.

[2574] In one embodiment, the method is performed in vitro.

[2575] In one embodiment, the method is performed in vivo.

[2576] In one embodiment, the BAA compound is provided in the form of a pharmaceutically acceptable composition.

[2577] Any type of cell can be treated or targeted, including, for example, blood cells (including, for example, neutrophils, eosinophils, basophils, lymphocytes, monocytes, erythrocytes, platelets), lung cells, gastrointestinal cells (including, for example, intestinal cells, colon cells), mammary cells (breast cells), ovarian cells, prostate cells, liver cells (hepatocytes), kidney cells (kidney cells), bladder cells, pancreatic cells, brain cells, and skin cells.

[2578] Those skilled in the art can readily determine whether a candidate compound can regulate (e.g., inhibit) cell proliferation, etc. For example, assays that can be conveniently used to assess the activity of a particular compound are described herein, and / or such methods are known in the art.

[2579] The BAA compounds described herein can inhibit cell migration and invasion, for example, inhibit metastasis.

[2580] The BAA compounds described herein can restore the sensitivity of drug-resistant cell populations to another agent.

[2581] The BAA compounds described herein can prevent cell populations from developing resistance to another agent.

[2582] The BAA compounds described herein can enhance the effects of other agents on DNA damage and subsequent cell killing. These agents can be therapeutic compounds that produce DNA damage or interfere with DNA damage responses.

[2583] Use in Treatment Methods

[2584] The use of the BAA compounds described herein in methods of treating human or animal bodies by means of treatment, such as methods of treating conditions (e.g., diseases) as described herein, is also described herein.

[2585] The use of the BAA compounds described herein in methods of treating human or animal bodies by means of treatment, such as methods of treating conditions (e.g., diseases) as described herein, is also described herein.

[2586] Use in Pharmaceutical Manufacturing

[2587] The use of the BAA compounds described herein in manufacturing pharmaceuticals for treatment methods, such as methods of treating conditions (e.g., diseases) as described herein, is also described herein.

[2588] In one embodiment, the pharmaceuticals comprise the BAA compound.

[2589] Treatment Methods

[2590] A treatment method is also described herein, for example, a method for treating a condition (e.g., a disease) as described herein, comprising administering to a subject requiring treatment a therapeutically effective amount of a BAA compound as described herein, preferably in the form of a pharmaceutical composition.

[2591] Condition treated - a condition improved by inhibiting PKMYT1

[2592] In one embodiment (e.g., a compound for use in a treatment method, use in a treatment method, use in pharmaceutical manufacturing, a treatment method), the treatment is a condition (e.g., a disease) that can be improved by inhibiting PKMYT1 (e.g., by inhibiting or reducing or blocking the activity or function of PKMYT1).

[2593] Condition treated

[2594] In one embodiment (e.g., a compound for use in a treatment method, use in a treatment method, use in pharmaceutical manufacturing, a treatment method), the treatment is a condition (e.g., a disease), such as a proliferative condition, cancer, etc. as described herein.

[2595] Proliferative condition

[2596] In one embodiment, the condition is: a proliferative condition.

[2597] As used herein, the term “proliferative disorder” refers to an undesirable or uncontrolled proliferation of cells, such as neoplastic or proliferative growth.

[2598] In one embodiment, a proliferative disorder is characterized by benign, precancerous, malignant, pre-metastatic, metastatic, or non-metastatic cell proliferation, including, for example: vegetations, hyperplasia, tumors (e.g., histiocytoma, glioma, astrocytoma, osteoma), cancer, psoriasis, bone diseases, fibroproliferative disorders (e.g., connective tissue), pulmonary fibrosis, atherosclerosis, and smooth muscle cell proliferation in blood vessels, such as stenosis or restenosis following angioplasty. Specification 124 / 530 pages 140 CN 121568936 A

[2599] Disorders Treated – Proliferative Disorders

[2600] In one embodiment (e.g., use in a method of therapy, use in pharmaceutical manufacturing, treatment method), the treatment is a treatment of a proliferative disorder.

[2601] As used herein, the term "proliferative disorder" refers to an undesirable or uncontrolled proliferation of cells, such as neoplastic or proliferative growth, due to excessive or abnormal cell proliferation.

[2602] In one embodiment, the treatment is to treat a proliferative disorder having benign, precancerous, or malignant cell proliferation characteristics.

[2603] In one embodiment, the treatment is to treat a proliferative disorder having or further having the following characteristics: inappropriate activity and / or expression of PKMYT1, CCNE1, FBXW7, or PPP2A or one subunit thereof.

[2604] In one embodiment, the treatment is to treat a proliferative disorder having or further having the following characteristics:Treatment: PKMYT1 or CCNE1 overexpression.

[2605] In one embodiment, the treatment is for a proliferative disease having or further having the following characteristics: PKMYT1 overexpression.

[2606] In one embodiment, the treatment is for a proliferative disease having or further having the following characteristics: CCNE1 overexpression.

[2607] In one embodiment, the treatment is for a proliferative disease having or further having the following characteristics: FBXW7 inactivation, reduced activity, or reduced expression level.

[2608] In one embodiment, the treatment is for a proliferative disease having or further having the following characteristics: FBXW7 inactivation.

[2609] In one embodiment, the treatment is for a proliferative disease having or further having the following characteristics: reduced PPP2R2A activity or reduced expression level.

[2610] In one embodiment, the treatment is a cancer treatment.

[2611] Disease treated - Cancer

[2612] In one embodiment (e.g., use in a therapeutic method, use in pharmaceutical manufacturing, treatment method), the treatment is a cancer treatment.

[2613] Cancers include:

[2614] (1) Carcinomas, including tumors originating from layered squamous epithelium (squamous cell carcinoma) and tumors arising in organs or glands (adenocarcinoma). Examples include the breast, colon, lung, prostate, and ovary.

[2615] (2) Sarcomas, including: osteosarcoma and osteogenic sarcoma (bone); chondrosarcoma (cartilage); leiomyosarcoma (smooth muscle); rhabdomyosarcoma (skeletal muscle); mesothelioma and mesothelioma (membranous lining of body cavities); fibrosarcoma (fibrous tissue); angiosarcoma and angioendothelioma (vascular); liposarcoma (adipose tissue); glioma and astrocytoma (neurogenic connective tissue found in the brain); myxosarcoma (primordial embryonic connective tissue); mesenchymal and mixed mesodermal tumors (mixed connective tissue types).

[2616] (3) Myeloma.

[2617] (4) Hematopoietic system tumors, including: myeloid and granulocytic leukemias (malignant tumors of the bone marrow and granulocytic leukocyte series), such as chronic myeloid leukemia (CML), acute myeloid leukemia (AML); lymphocytic, lymphoblastic and lymphoblastic leukemias (malignant tumors of the lymphocyte and lymphoblastic blood cell series), such as acute lymphoblastic leukemia (ALL), chronic lymphocytic leukemia (CLL); polycythemia vera (malignant tumors of various blood cell products, but mainly red blood cells). Specification 125 / 530 pages 141 CN 121568936 A

[2618] (5) Lymphomas, including: Hodgkin lymphoma and non-Hodgkin lymphoma.

[2619] (6) Mixed tumors, including, for example: adenosquamous carcinoma; mixed mesodermal tumors; carcinosarcoma; teratoma.

[2620] In one embodiment, the cancer is:

[2621] Bone or muscle sarcoma, such as: bone cancer; osteosarcoma; chondrosarcoma; Ewing's sarcoma; cardiac cancer; leiomyosarcoma; malignant fibrous histiocytoma of bone; osteosarcoma; or rhabdomyosarcoma;

[2622] Cancers of the brain and nervous system, such as:

[2623] Astrocytoma; brain cancer; brainstem glioma; cerebellar astrocytoma; cerebral astrocytoma; ependymoma; glioblastoma; glioma; medulloblastoma; neuroblastoma; oligodendroglioma; fibrous astrocytoma; pineal astrocytoma; pituitary adenoma; primitive neuroectodermal tumor; schwannoma; or optic pathway and hypothalamic glioma;

[2624] Breast cancer, such as: breast cancer; invasive cribriform carcinoma; inflammatory breast cancer; invasive lobular carcinoma; medullary carcinoma; male breast cancer: phyllodes tumor; or tubular carcinoma;

[2625] Cancers of the endocrine system, such as: adrenal carcinoma; adrenocortical carcinoma; papillary thyroid carcinoma; follicular thyroid carcinoma; islet cell carcinoma; polyendocrine adenoma syndrome; parathyroid carcinoma; pheochromocytoma; thyroid cancer; or thyroid gland cancer;

[2626] Ocular cancers, such as: retinoblastoma; or uveal melanoma;

[2627] Gastrointestinal cancers, such as:

[2628] Anal cancer; appendix cancer; biliary tract cancer; intestinal cancer; bile duct cancer; colonic adenocarcinoma; colonic adenoma; colon cancer; exocrine pancreatic cancer; extrahepatic bile duct cancer; gallbladder cancer; stomach (gastric) cancer; gastrointestinal cancer; gastrointestinal carcinoid tumors; gastrointestinal carcinoid tumors; gastrointestinal stromal tumors (GIST); hepatocellular carcinoma; hepatoblastoma; kidney cancer; colorectal cancer; liver cancer; colorectal cancer; pancreatic cancer; rectal cancer; or small bowel cancer;

[2629] Urogenital or gynecological cancers, such as: bladder cancer; cervical cancer; endometrial cancer; gonadal germ cell tumors; urogenital cancers; gestational trophoblastic tumors; gynecological cancers; ovarian cancer; ovarian epithelial cancer; ovarian germ cell tumors; penile cancer; prostate cancer; renal cell carcinoma; transitional cell carcinoma of the renal pelvis and ureter; seminoma; teratoma; testicular cancer; transitional cell carcinoma of the ureter and renal pelvis; urethral cancer; uterine sarcoma; vaginal cancer; vulvar cancer; or Wilms' tumor;

[2630] Head and neck cancers, such as: esophageal cancer; head and neck cancer; head and neck squamous cell carcinoma; hypopharyngeal cancer; nasopharyngeal carcinoma; nasopharyngeal tumor; oral cancer; oropharyngeal cancer; sinus and nasal cavity cancer; pharyngeal cancer; or salivary gland cancer;

[2631] Hematopoietic system cancers, such as:

[2632] plasma cell tumors, such as plasmacytoma or multiple myeloma;

[2633] Leukemia, such as: acute biphenotypic leukemia; acute eosinophilic leukemia; acute lymphoblastic leukemia; acute myeloid dendritic cell leukemia; acute myeloid leukemia; acute promyelocytic leukemia; B-cell prolymphocytic leukemia; chronic lymphocytic leukemia; chronic myeloid leukemia; hairy cell leukemia; large granular lymphocytic leukemia;Mast cell leukemia; precursor B-cell lymphoblastic leukemia; T-cell prolymphoblastic leukemia;

[2634] Lymphoma, for example: AIDS-related lymphoma; anaplastic large cell lymphoma; angioimmunoblastic T-cell lymphoma; Burkitt lymphoma; cutaneous T-cell lymphoma; diffuse large B-cell lymphoma; follicular lymphoma; hepatosplenic T-cell lymphoma; Hodgkin lymphoma; intravascular large B-cell lymphoma; lymphomatoid granulomatosis; lymphoplasmacytic lymphoma; mantle cell lymphoma; marginal zone B-cell lymphoma; mediastinal large B-cell lymphoma; mucosa-associated lymphoid tissue lymphoma; mycosis fungoides; nodular marginal zone B-cell lymphoma; non-Hodgkin lymphoma; plasmablastic lymphoma; Primary central nervous system lymphoma; primary cutaneous follicular lymphoma; primary cutaneous immunocytoma; primary exudative lymphoma; Cezari syndrome; or marginal zone lymphoma of the spleen; or

[2635] myelodyplastic syndrome;

[2636] skin cancer, such as: basal cell carcinoma; dermatofibrosarcoma protuberans; fibrosarcoma; keratoacanthoma; malignant melanoma; melanoma; Merkel cell carcinoma; sebaceous gland carcinoma; or squamous cell carcinoma;

[2637] thoracic and respiratory system cancers, such as: adenocarcinoma; bronchial adenoma; bronchial carcinoid; laryngeal carcinoma; lung cancer; mediastinal carcinoma; mesothelioma; non-small cell lung cancer; peritoneal carcinoma; pleural pulmonary blastoma; small cell lung cancer; thymic carcinoma; or thymoma carcinoma;

[2638] Cancers associated with HIV / AIDS, such as Kaposi's sarcoma;

[2639] or other cancers, such as epithelioid hemangioendothelioma; myxoid small round cell tumor; or liposarcoma.

[2640] In one embodiment, the cancer is:

[2641] endometrial cancer, uterine cancer, ovarian cancer, breast cancer, gastric cancer, bladder cancer, pancreatic cancer, mesothelioma, renal cancer, stomach cancer, esophageal cancer, colorectal cancer, glioblastoma, lung cancer, or squamous cell carcinoma of the lung.

[2642] In one embodiment, the cancer is endometrial cancer.

[2643] In one embodiment, the cancer is uterine cancer.

[2644] In one embodiment, the cancer is ovarian cancer.

[2645] In one embodiment, the cancer is breast cancer.

[2646] In one embodiment, the cancer is gastric cancer.

[2647] In one embodiment, the cancer is bladder cancer.

[2648] In one embodiment, the cancer is pancreatic cancer.

[2649] In one embodiment, the cancer is mesothelioma.

[2650] In one embodiment, the cancer is kidney cancer.

[2651] In one embodiment, the cancer is stomach cancer.

[2652] In one embodiment, the cancer is esophageal cancer.

[2653] In one embodiment, the cancer is colorectal cancer.

[2654] In one embodiment, the cancer is glioblastoma.

[2655] In one embodiment, the cancer is lung cancer.

[2656] In one embodiment, the cancer is squamous cell carcinoma of the lung.

[2657] In one embodiment, the cancer is characterized, or further characterized, by inappropriate activity of PKMYT1 (e.g., overexpression). For example, in one embodiment, the cancer is:

[2658] squamous cell carcinoma of the lung, lung adenocarcinoma, endometrial cancer of the uterine corpus, breast cancer, invasive breast cancer, hepatocellular carcinoma, clear cell renal cell carcinoma, chromophobe renal cell carcinoma, papillary renal cell carcinoma, squamous cell carcinoma of the head and neck, colonic adenocarcinoma, gastric adenocarcinoma, thyroid cancer, prostate adenocarcinoma, adrenocortical carcinoma, low-grade glioma, mesothelioma, pancreatic adenocarcinoma, cutaneous melanoma of the skin, uveal melanoma.

[2659] In one embodiment, the cancer is characterized, or further characterized, by PKMYT1 involvement in development, invasion, and / or metastasis. For example, in one embodiment, the cancer is:

[2660] non-small cell lung cancer, osteosarcoma, clear cell renal cell carcinoma, oral squamous cell carcinoma, gastric cancer, prostate cancer, esophageal squamous cell carcinoma, colorectal cancer, hepatocellular carcinoma, ovarian cancer, neuroblastoma (especially the type with MYCN amplification), glioblastoma, acute lymphoblastic leukemia, multiple myeloma, Kaposi's sarcoma, primary exudative lymphoma (PEL), or plasmacytic variant of multicentric Castleman's disease. Specification 127 / 530 pages 143 CN 121568936 A

[2661] In one embodiment, the cancer is characterized, or further characterized, by inappropriate activity of CCNE1 (e.g., overexpression). For example, in one embodiment, the cancer is:

[2662] uterine carcinosarcoma, uterine cancer, endometrial cancer, breast cancer, ovarian cancer, gastric cancer, colorectal cancer, bladder cancer, esophageal cancer, cervical cancer, sarcoma, squamous cell carcinoma of the lung, adenoid cystic carcinoma, pancreatic cancer, mesothelioma, lung adenocarcinoma, head and neck cancer, diffuse large B-cell lymphoma, or liver cancer.

[2663] In one embodiment, the cancer is characterized, or further characterized, by inappropriate activity of CCNE1 (e.g., overexpression). For example, in one embodiment, the cancer is:

[2664] uterine carcinosarcoma, uterine cancer, endometrial cancer, breast cancer, ovarian cancer, gastric cancer, colorectal cancer, bladder cancer, esophageal cancer, cervical cancer, sarcoma, or squamous cell carcinoma of the lung.

[2665] In one embodiment, the cancer is uterine carcinosarcoma (UCS) or uterine serous carcinoma (USC).

[2666] In one embodiment, the cancer is high-grade serous ovarian cancer (HGSOC).

[2667] In one embodiment, the cancer is high-grade serous ovarian cancer with CCNE1 amplification.

[2668] In one embodiment, the cancer is triple-negative breast cancer (TNBC).

[2669] In one embodiment, the cancer is characterized, or further characterized, by inappropriate activity of FBXW7 (e.g., inactivation). For example, in one embodiment, the cancer is:

[2670] uterine carcinosarcoma, uterine cancer, endometrial cancer, breast cancer, ovarian cancer, gastric cancer, colorectal cancer, bladder cancer, esophageal cancer, cervical cancer, sarcoma, squamous cell carcinoma of the lung, or head and neck cancer.

[2671] In one embodiment, the cancer is characterized, or further characterized, by inappropriate activity of FBXW7 (e.g., inactivation). For example, in one embodiment, the cancer is:

[2672] uterine carcinosarcoma, endometrial cancer, colorectal cancer, cervical cancer, bladder cancer, head and neck cancer, gastric cancer, or squamous cell carcinoma of the lung.

[2673] In one embodiment, the cancer is uterine carcinosarcoma (UCS) or uterine serous carcinoma (USC).

[2674] In one embodiment, the cancer is characterized, or further characterized, by inappropriate activity of PPP2R2A (e.g., inactivation, reduced activity, reduced expression). For example, in one embodiment, the cancer is:

[2675] prostate adenocarcinoma, ovarian serous cystadenocarcinoma, rectal adenocarcinoma, bladder urothelial carcinoma, colorectal adenocarcinoma, invasive breast cancer, endometrial cancer of the uterine corpus, uterine carcinosarcoma, hepatocellular carcinoma, squamous cell carcinoma of the lung, or lung adenocarcinoma.

[2676] In one embodiment, the cancer (e.g., as described above) is characterized, or further characterized, as treatment-resistant cancer, such as chemotherapy-resistant cancer, radiation-resistant cancer, and / or immunotherapy-resistant cancer.

[2677] In one embodiment, the treatment-resistant cancer is resistant to standard care treatment.

[2678] In one embodiment, the treatment-resistant cancer is resistant to one or more of PARP inhibitors, cisplatin, WEE1 inhibitors, and Cdk4 / 6 inhibitors.

[2679] In one embodiment, the cancer being treated is ovarian cancer with strong recombination ability.

[2680] In one embodiment, the cancer being treated is HER2-ER+ breast cancer with CdK4 / 6 resistance.

[2681] In one embodiment, the cancer (e.g., as described above) is characterized, or further characterized, as metastatic cancer.

[2682] The anticancer effect can be produced through one or more mechanisms, including but not limited to: regulation of cell proliferation, inhibition of cell cycle progression, inhibition of angiogenesis (formation of new blood vessels), inhibition of metastasis (spread of tumor from its origin), inhibition of cell migration (spread of cancer cells to other parts of the body), inhibition of invasion (spread of tumor cells to adjacent normal tissues), promotion of apoptosis (programmed cell death), necrosis-induced death, or induction of autophagic death. The chemical reactions described hereinThe compound can be used to treat the cancer described herein, without being limited to the mechanisms discussed herein. Specification 128 / 530 pages 144 CN 121568936 A

[2683] Treatment

[2684] The term “treatment” as used herein in the context of treating a condition (e.g., disease) generally refers to treatment on a human or animal (e.g., in veterinary use) in which some desired therapeutic effect is achieved, such as inhibiting the development of the condition (including, for example, slowing the rate of development, stopping the rate of development), alleviating the symptoms of the condition, improving the condition, and curing the condition. Treatment as a preventive measure (i.e., prevention) is also included. For example, the treatment of subjects (e.g., patients) who have not yet developed the condition but are at risk of developing the condition is also covered by the term “treatment”.

[2685] For example, the treatment of cancer includes slowing the development of cancer, alleviating the symptoms of cancer, reducing the incidence of cancer, preventing cancer, etc.

[2686] As used herein, the term “therapeuticly effective amount” refers to an amount of compound or material, composition, or form of administration containing the compound that, when administered according to a desired treatment regimen, is effective in producing some expected therapeutic effect and has a reasonable benefit / risk ratio.

[2687] Combination Therapy

[2688] As used herein, the term “treatment” includes combination treatment and therapy, wherein two or more treatments or therapies are combined together, for example, sequentially or simultaneously. For example, the BAA compounds described herein may also be used in combination therapy, for example, in combination with other drugs.

[2689] Thus, the use of BAA compounds as described herein in combination with one or more other therapeutic agents (e.g., 1, 2, 3, 4, etc.) is also described herein.

[2690] For example, methods of treating a human or animal body with BAA compounds as described herein by means of treatment, such as methods of treating a condition (e.g., disease) as described herein, wherein the BAA compound is administered in combination with one or more other therapeutic agents (e.g., 1, 2, 3, 4, etc.).

[2691] This document also describes the use of BAA compounds as described herein in methods of treating human or animal bodies, such as in methods of treating conditions (e.g., diseases) as described herein, wherein the BAA compound is administered in combination with one or more (e.g., 1, 2, 3, 4, etc.) other therapeutic agents.

[2692] This document also describes the use of BAA compounds as described herein in methods of treating human or animal bodies, such as in methods of treating conditions (e.g., diseases) as described herein, wherein the BAA compound is administered in combination with one or more (e.g., 1, 2, 3, 4, etc.) other therapeutic agents.

[2693] This document also describes the use of BAA compounds as described herein in the manufacture of medicaments for use in treatment methods, such as...As in a method of treating a condition (e.g., a disease) as described herein, the BAA compound is administered in combination with one or more other therapeutic agents (e.g., 1, 2, 3, 4, etc.).

[2694] In one embodiment, the medicament comprises a BAA compound.

[2695] A treatment method, such as a method of treating a condition (e.g., a disease) as described herein, is also described herein, comprising administering to a subject requiring treatment a therapeutically effective amount of the BAA compound described herein, preferably in the form of a pharmaceutical composition, wherein the BAA compound is administered in combination with one or more other therapeutic agents (e.g., 1, 2, 3, 4, etc.).

[2696] The specific combination will be determined by the physician, who will select the dosage based on their general knowledge and dosing regimens known to skilled practitioners.

[2697] The agents (e.g., the BAA compound described herein, plus one or more other agents) may be administered simultaneously or sequentially, and may be administered via different routes according to their respective dosage regimens. For example, when administered sequentially, the agent can be administered at close intervals (e.g., within 5 to 10 minutes) or at longer intervals (e.g., 1, 2, 3, 4 or more hours apart, or even longer intervals as needed), with the precise dosing regimen adapted to the specific characteristics of the therapeutic agent.

[2698] The agent (e.g., the BAA compound described herein, plus one or more other agents) can be formulated in a single dosage form, or the individual agents can be formulated separately and optionally provided together in a kit, optionally with their instructions for use.

[2699] In one embodiment, the other agents (e.g., additional therapeutic agents) are immunotherapeutic agents, such as immune checkpoint inhibitors.

[2700] In one implementation, the other agents (e.g., additional therapeutic agents, such as additional anticancer drugs) are immunotherapeutic agents, such as monoclonal antibodies (e.g., trastuzumab, bevacizumab, cetuximab, daratumumab or nachitamumab, nesetuzumab, octotuzumab, oflamumab, panitumumab, pertuzumab, ramucirumab or rituximab), bispecific antibodies (e.g., bonatetumab), immune checkpoint inhibitors (e.g., boratumab). Examples of treatments include ipilimumab, nivolumab, pembrolizumab, sempulimab, atezolizumab, durvalumab, avelumab, dostalimumab, or trimemumab; immunomodulators (e.g., imiquimod, thalidomide, lenalidomide, or propiconazole); cytokines such as interleukins (e.g., IL-2 adeleukin); interferons (e.g., IFNa); oncolytic viruses (e.g., talimogene laherparepvec); or T-cell therapy.

[2701] In one embodiment, other agents are antibody-drug conjugates (i.e., "ADCs"), such as brentuximab vedotin, ovatuzumab, somituximab, trastuzumab emtansine, trastuzumab emtansine, gemtuzumab oxazomicin, enrofloxacin, polotuzumab, tisotumab vedotin-tftv, goxatocillin, rontoxicin, or vedictitumab.

[2702] In one embodiment, other agents are DNA damaging agents, such as alkylating agents (e.g., cisplatin, oxaliplatin, ...). Carboplatin, cyclophosphamide, melphalan, levofloxacin, bendamustine, temozolomide, terabetin, mitomycin C, or dacarbazine; antimetabolites (e.g., capecitabine, gemcitabine, 5-fluorouracil, fluorouracil, trifluorouridine, telpiracillin, cytarabine, or methotrexate); DNA intercalating agents (e.g., anthracyclines such as doxorubicin, epirubicin, or daunorubicin); antibiotics (e.g., bleomycin, actinomycin, or styraxicin); topoisomerase 1 inhibitors (e.g., camptothecin, such as irinotecan or topotecan); topoisomerase 2 inhibitors (e.g., etoposide); microtubule-targeting agents (e.g., taxanes such as paclitaxel; or vinca alkaloids such as vincristine, vinblastine, vinorelbine, or eribulin); or antibiotics (e.g., bleomycin or mitomycin-C).

[2703] In one embodiment, the other agent is a topoisomerase I inhibitor (e.g., irinotecan or topotecan), a topoisomerase II inhibitor (e.g., etoposide), or an antimetabolite (e.g., gemcitabine).

[2704] In one embodiment, the other agent is an alkylating agent (e.g., cisplatin).

[2705] In one embodiment, the other agent is a topoisomerase I inhibitor (e.g., irinotecan or topotecan).

[2706] In one embodiment, the other agent is a topoisomerase II inhibitor (e.g., etoposide).

[2707] In one embodiment, the other agent is an antimetabolite (e.g., gemcitabine).

[2708] In one embodiment, the other agent is a DNA damage repair inhibitor (e.g., a PARP inhibitor, such as olaparib, rucapranib, niraparib, or talapopanib; or a PARG inhibitor; or a USP1 inhibitor).

[2709] In one embodiment, the other agent is a double-strand break repair inhibitor (e.g., a Polθ inhibitor, or a RAD51 inhibitor).

[2710] In one embodiment, the other agent is a signaling pathway inhibitor, such as a kinase inhibitor (e.g., abexicinib, acalatinib, afatinib, alectinib, avatinib, axitinib, baricitinib, besudil, bumitinib, bosutinib, brigatinib, cabozantinib, capiprinib, ceritinib, cobitinib, rizotinib, dabrafenib, dacomitant). (Instructions for use 130 / 530, page 146, CN 121568936 A)Dasatinib, Cannafinib, Entecavir, Erdatinib, Elotinib, Everolimus, Fedratinib, Fastamatinib, Gefitinib, Gefitinib, Ibrutinib, Imatinib, Ifatinib, Lapatinib, Larotrectinib, Lenvatinib, Lorlatinib, Midostinib, Mobocitinib, Lenatinib, Netoxutinib, Nilotinib, Nintedanib, Osimertinib, Palbocicib Pazopanib, Pemitinib, Pericidatinib, Panatinib, Peracetinib, Regorafenib, Rebocicib, Ripretinib, Ruxotinib, Serpatinib, Celumitinib, Sirolimus, Sorafenib, Sunitinib, Tesseirolimus, Terpotinib, Tivozambique, Tofacitinib, Trametinib, Triraciab, Tucatinib, Upatinib, Vandertanib, Vemurafenib, or Zanubrutinib.

[2711] In one embodiment, the other agent is a cell cycle targeting inhibitor, such as a CDK4 / 6 inhibitor (e.g., Pazopanib, Abecilib, or Rebocicib).

[2712] In one embodiment, the other agent is an agent that targets DNA damage checkpoints, such as an ATR inhibitor (e.g., celal-setebuprofen, gatisetebuprofen, tevosetebuprofen, elimuxertebuprofen, or carmustib), an ATM inhibitor (e.g., AZD0156), a CHK1 inhibitor (e.g., prezal-setebuprofen), a CHK2 inhibitor, a WEE1 inhibitor (e.g., adavoratebuprofen or azenoxetebuprofen), a PLK1 inhibitor (e.g., onivozetibuprofen), or an AUR-A inhibitor (e.g., JAB-2485).

[2713] In one embodiment, the other agent is an ATR inhibitor (e.g., celal-setebuprofen, gatisetebuprofen, tevosetebuprofen, elimuxertebuprofen, or carmustib), a CHK1 inhibitor (e.g., prezal-setebuprofen), or a WEE1 inhibitor (e.g., adavoratebuprofen or azenoxetebuprofen).

[2714] In one embodiment, the other agent is an ATR inhibitor (e.g., celal-celtib, gaticeltib, tevoceltib, or ...

Claims

1. A compound represented by the following formula: Or its pharmaceutically acceptable salts or solvates; in: Ring A is: in: -R A1 -R A11 ; -R A11 is -R A111 、-F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A111 、-OCF3, -NH2, -NHR A111 、-NR A111 2, -CN, -C(=O)R A111 、-C(=O)OH, -C(=O)OR A111 、-C(=O)NH2, -C(=O)NHR A111 、-C(=O)NR A111 2 or -S(=O)2R A111 ; Each -R A111 Independently saturated C for straight or branched chains 1-4 alkyl; -R A2 -R A22 ; -R A22 is -R A222 , -F, -Cl, -Br, -I, -CF3, -CHF2, -OH, -OR A222 , -OCF3, -NH2, -NHR A222 , -NR A222 2, -CN, -C(=O)R A222 , -C(=O)OH, -C(=O)OR A222 , -C(=O)NH2, -C(=O)NHR A222 , -C(=O)NR A222 2 or -S(=O)2R A222 ; Each -R A222 Independently saturated C for straight or branched chains 1-4 alkyl; -R A3 -H or -R A33 ; -R A33 -R A333 , -F, -Cl, -Br, -I, -CF3, -OH, -OR A333 Or -OCF3; Each -R A333 Independently saturated C for straight or branched chains 1-4 alkyl; -R A4 -H or -R A44 ; -R A44 -R A444 , -F, -Cl, -Br, -I, -CF3, -OH, -OR A444 Or -OCF3; Each -R A444 Independently saturated C for straight or branched chains 1-4 alkyl; and: Ring B is selected from: in: Y 1 For S, O, NH or NR Y1 ; Y 2 For CH, CR Y2 Or N; Y 3 For N, CH or CR Y3 ; Y 4 For N, CH or CR Y4 ; Y 5 For S, O, NH or NR Y5 ; Y 6 For N, CH or CR Y6 ; Y 7 For N, CH or CR Y7 ; Y 8 For N, CH or CR Y8 ; Y 9 For S, O, NH or NR Y9 ; in: Each -R Y2 -R Y3 -R Y4 -R Y6 -R Y7 and -R Y8 Independently -H, -F, -Cl, -Br, -I, -R YY -CF3, -OH, -OR YY -OCF3, -NH2, -NHR YY or -NR YY 2; Each -R YY Independently saturated C for straight or branched chains 1-4 alkyl; And among them: Each -R Y1 -R Y5 and -R Y9 Independently for -R YYN -C(=O)R YYN -C(=O)OR YYN -C(=O)NH2, -C(=O)NHR YYN -C(=O)NR YYN 2 or -S(=O)2R YYN ; Each -R YYN Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-4 The alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; And among them: -Q is -Q 1 -L Q1 -Q 1 -Q 2 -L Q2 -Q 2 -Q 3 -L Q3 -Q 3 -Q 4 -L Q4 -Q 4 -Q 5 Or -H; in: Q 1 C 5-10 Mixed aromatics; and: Carbon atoms are optionally surrounded by one or more -R Q1C Group substitution; and Secondary nitrogen atoms, if present, are optionally surrounded by one or more -R atoms. Q1N Group substitution; -L Q1 - For straight-chain or branched saturation C 1-4 Alkylene; Q 2 C 3-10 Heterocyclic groups; and: The sulfur atom, if present, may optionally be replaced by one or two =O groups; Carbon atoms are optionally surrounded by one or more -R Q2C Group substitution; and Secondary nitrogen atoms, if present, are optionally surrounded by one or more -R atoms. Q2N Group substitution; -L Q2 - For straight-chain or branched saturation C 1-4 Alkylene; Q 3 It is phenyl or naphthyl; And optionally by one or more -R Q3C Group substitution; -L Q3 - For straight-chain or branched saturation C 1-4 Alkylene; Q 4 C 3-10 carbon cyclo group; And optionally by one or more -R Q4C Group substitution; -L Q4 - For straight-chain or branched saturation C 1-4 Alkylene; Q 5 For straight-chain or branched saturated C 1-6 alkyl; And optionally by one or more -R Q5C Group substitution; And among them: Each -R Q1C Independently: -F, -Cl, -Br, -I, -R Q1CC 、 -R Q1CX 、-OR Q1CX 、 -OH、-OR Q1CC 、 -L Q1C -OH、-L Q1C -OR Q1CC 、 -NH2, -NHR Q1CC 、-NR Q1CC 2.-R Q1CM 、 -L Q1C -NH2, -L Q1C -NHR Q1CC -L Q1C -NR Q1CC 2.-L Q1C -R Q1CM 、 -NHC(=O)R Q1CC 、-N(R Q1CC )C(=O)R Q1CC 、-NHC(=O)OR Q1CC 、 -L Q1C -NHC(=O)R Q1CC 、-L Q1C -NHC(=O)OR Q1CC 、 -C(=O)NH2, -C(=O)NHR Q1CC -C(=O)NR Q1CC 2. -C(=O)R Q1CM 、=O、-NHC(=O)NH2、-NHC(=O)NHR Q1CC -NHC(=O)NR Q1CC 2. -NHC(=O)R Q1CM 、 -L Q1C -C(=O)NH2、-L Q1C -C(=O)NHR Q1CC -L Q1C -C(=O)NR Q1CC 2.-L Q1C -C(=O)R Q1CM 、 -C(=O)OH、-C(=O)OR Q1CC 、 -OC(=O)R Q1CC 、 -OC(=O)NH2、-OC(=O)NHR Q1CC -OC(=O)NR Q1CC 2、-OC(=O)R Q1CM 、 -S(=O)2R Q1CC 、-S(=O)2R Q1CX 、 -S(=O)2NH2、-S(=O)2 N HR Q`CC 、-S(=O)2 N R Q1CC 2、-S(=O)2 RQ1CM 、 -NHS(=O)R Q1CC 、-NHS(=O)2 RQ1CC 、 -CN, -C≡CH, or -NO2; And two adjacent -R Q1C If present, they can co-form -(CH2). n1 -O-(CH2) m1 -or -O-(CH2) p1 -O-, where: n1 is 0, 1, 2 or 3; m1 is 0, 1, 2 or 3; and p1 is 1 or 2; provided that m1+n1 is 2 or 3; in: Each -R Q1CC Independently saturated C for straight or branched chains 1-6 Alkyl, C 2-6 alkenyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, C 3-7 Heterocyclic group, phenyl, phenyl-C 1-3 Alkyl, C5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-6 The alkyl group is optionally substituted with -OH, -CN, or -OCH3, and each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -C 1-4 Alkyl groups, -CHF2, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; Each -R Q1CX Independently saturated C for straight or branched chains 1-4 Halogenated alkyl groups; Each -L Q1C - Independently saturate C for straight or branched chains 1-4 Alkylene; Each -R Q1CM Independently a non-aromatic C having at least one N ring atom 3-11 Heterocyclic group, and connected through the N-ring atom; and: Carbon atoms are optionally surrounded by one or more -R Q1CMM Group substitution; The sulfur atom, if present, may optionally be replaced by one or two =O groups; and The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R Q1CMM -C(=O)R Q1CMM -C(=O)OR Q1CMM -C(=O)NH2, -C(=O)NHR Q1CMM -C(=O)NR Q1CMM 2 and -S(=O)2R Q1CMM ;and Each -R Q1CMM Independently saturated C with -F, -NH2, straight or branched chains 1-4 Alkyl, C 1-4 Alkyl OC(=O)NH-, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-4 The alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; And among them: Each -R Q1N Independently: -R Q1NC 、-L Q1N -R Q1NC 、 -R QINX 、 -R Q1Nhet 、-L Q1N -R Q1Nhet 、 -L Q1N -OH、-L Q1N -OR Q1NC 、 -L Q1N -C(=O))R Q1NC 、 -S(=O)2R Q1NC 、 -L Q1N -C(=O)OH、-L Q1N -C(=O)OR Q1NC 、 -L Q1N -C(=O)NH2、-L Q1N -C(=O)NHR Q1NK -L Q1N -C(=O)NR Q1NC 2.-L Q1N -C(=O)R Q1NP 、 -L Q1N -NH2, -L Q1N -NHR Q1NC -L Q1N -NR Q1NC 2.-L Q1N -R Q1NM 、 or -L Q1N -NHC(=O)OR Q1NC ; in: Each -R Q1NC Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl groups, wherein each C 1-4 The alkyl group is optionally substituted with -F, -OH, -C≡N, -SO₂-CH₃, or -OCH₃, wherein each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -Br, straight-chain or branched saturated C 1-4 Alkyl, -CHF2, -CF3, -OH, -OCH3, -CH2-O-CH3, -OCH2CH3, -C(=O)-NH-phenyl, -NH2, -NH(CH3) and -N(CH3)2; wherein C 1-4 Alkyl and phenyl groups are optionally substituted with -CH3 or -OH independently; Each -R Q1NX Independently saturated C for straight or branched chains 1-4 Halogenated alkyl groups; Each -L Q1N - Independently saturate C for straight or branched chains 1-4 Alkylene; wherein C 1-4 The alkylene group may optionally be replaced by -OH or -OMe; Each -R Q1NM Independently a non-aromatic C having at least one N ring atom 3-7 Heterocyclic group, and connected through the N-ring atom; and: Carbon atoms are optionally surrounded by one or more -R Q1NMM Group substitution; The sulfur atom, if present, may optionally be replaced by one or two =O groups; and The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R Q1NMM -C(=O)R Q1NMM -C(=O)OR Q1NMM -C(=O)NH2, -C(=O)NHR Q1NMM -C(=O)NR Q1NMM 2 and -S(=O)2R Q1NMM ;and Each -R Q1NMM Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, C 3-6 Cycloalkyl-C1-3 alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-4 The alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; And among them: Each -R Q1Nhet Independently non-aromatic C 3-7 Heterocyclic group, and: The sulfur atom, if present, may optionally be replaced by one or two =O groups; Carbon atoms are optionally surrounded by one or more -R Q1NHH Substitution of groups or =O groups; and The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R Q1NHH -C(=O)R Q1NJJ -C(=O)OR Q1NHH -C(=O)NH2, -C(=O)NHR Q1NHH -C(=O)NR Q1NHH 2 and -S(=O)2R Q1NHH ; in: Each -R Q1NHH Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, C 3-7 Heterocyclic group, phenyl, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-4 The alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; And among them: -R Q1NJJ is -R J1 、-R J2 、-L J -R J2 、-R J3 、-L J -R J3 、-RJ 4 、-L J -R J4 、-R J5 or -L J -R J5 ; -R J1 For straight-chain or branched saturated C 1-6 Alkyl group; and optionally substituted with one or more groups selected from the following: -F, -OH, -OR JJ -O-phenyl, -C(=O)OH, -C(=O)OR JJ -NH2, -NHR JJ and -NR JJ 2; Each -R J2 Independently for C 3-6 Cycloalkyl; and optionally substituted with one or more groups selected from the following: -F, -R JJ -CF3, -OH, -OR JJ -NH2, -NHR JJ and -NR JJ 2; Each -R J3 Independently non-aromatic C 3-7 Heterocyclic group; and: The sulfur atom, if present, may optionally be replaced by one or two =O groups; Carbon atoms are optionally surrounded by one or more atoms selected from -F, -R JJ -CF3, -OH, -OR JJ -NH2, -NHR JJ and -NR JJ Substitution of the group of 2; and The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R JJ -C(=O)R JJ -C(=O)OR JJ and -S(=O)2R JJ ; Each -R J4 It is phenyl; and optionally substituted with one or more groups selected from the following: -F, -Cl, -R JJ -CF3, -OH, -OR JJ -NH2, -NHR JJ and -NR JJ 2; Each -R J5 Independently for C 5-6 heteroaryl; and: Carbon atoms are optionally surrounded by one or more atoms selected from -F, -R JJ -CF3, -OH, -OR JJ -NH2, -NHR JJ and -NR JJ Substitution of the group of 2; and The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R JJ -C(=O)R JJ -C(=O)OR JJ and -S(=O)2R JJ ; Each -L J - Independently saturate C for straight or branched chains 1-4 Alkylene, and optionally substituted with one or more -F; Each -R JJ For straight-chain or branched saturated C 1-4 alkyl; And among them: -R Q1NK -R K1 -R K2 -L K -R K2 -R K3 -L K -R K3 -R K4 -L K -R K4 -R K5 or -L K -R K5 ; -R K1 For straight-chain or branched saturated C 1-7 Alkyl group; and optionally substituted with one or more groups selected from the following: -F, -OH, -OR KK -OCH2CH2OCH3, -O-phenyl, -C(=O)OH, -C(=O)OR KK -NH2, -NHR KK and -NR KK 2; Each -R K2 Independently for C 3-6 Cycloalkyl; and optionally substituted with one or more groups selected from the following: -F, -R KK -CF3, -OH, -OR KK -NH2, -NHR KK and -NR KK 2; Each -R K3 Independently non-aromatic C 3-7 Heterocyclic group; and: Carbon atoms are optionally surrounded by one or more atoms selected from -F, -R KK -CF3, -OH, -OR KK -NH2, -NHR KK and -NR KK Substitution of the group of 2; and The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R KK -C(=O)R KK -C(=O)OR KK and -S(=O)2R KK ; Each -R K4 It is phenyl; and optionally substituted with one or more groups selected from the following: -F, -Cl, -R KK -CF3, -OH, -OR KK -NH2, -NHR KK and -NR KK 2; Each -R K5 Independently for C 5-6 heteroaryl; and: Carbon atoms are optionally surrounded by one or more atoms selected from -F, -R KK -CF3, -OH, -OR KK -NH2, -NHR KK and -NR KK Substitution of the group of 2; and The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R KK -C(=O)R KK -C(=O)OR KK and -S(=O)2R KK ; Each -L K - For straight-chain or branched saturation C 1-4 Alkylene, and optionally substituted with one or more -F; Each -R KK For straight-chain or branched saturated C 1-4 alkyl; And among them: -R Q1NP A non-aromatic C having at least one N-ring atom 3-11 Heterocyclic group, and connected through the N-ring atom; and: The sulfur atom, if present, may optionally be replaced by one or two =O groups; Carbon atoms are optionally surrounded by one or more atoms selected from -R Q1NPP -F, -OH, -OR Q1NPP Substitution of groups with =O; and The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R Q1NPP -R Q1NPPX -C(=O)R Q1NPP -C(=O)OR Q1NPP -C(=O)NH2, -C(=O)NHR Q1NPP -C(=O)NR Q1NPP 2 and -S(=O)2RQ 1NPP ; Each -R Q1NPP Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-4 The alkyl group is optionally substituted with -F, -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; -R Q1NPPX For straight-chain or branched saturated C 1-4 Halogenated alkyl groups; And among them: Each -R Q2C Independently: -F， -R Q2CC 、-R Q2CX 、 -OH、-OR Q2CC 、-OR Q2CX 、 -NH2, -NHR Q2CC 、-NR Q2CC 2.-R Q2CM 、 -NHC(=O)R Q2CC 、-NHC(=O)OR Q2CC 、 -C(=O)NH2、-C(=O)NHR Q2CC 、-C(=O)NR Q2CC 2、-C(=O)R Q2CM 、 -C(=O)OH、-C(=O)OR Q2CC 、 -OC(=O)R Q2CC 、 -OC(=O)NH2, -OC(=O)NHR Q2CC , -OC(=O)NR Q2CC 2, -OC(=O)R Q2CM or =O; in: Each -R Q2CC Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, phenyl, C 3-7 Heterocyclic group, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-4 The alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; Each -R Q2CX Independently saturated C for straight or branched chains 1-4 Halogenated alkyl groups; Each -R Q2CM Independently a non-aromatic C having at least one N ring atom 3-11 Heterocyclic group, and connected through the N-ring atom; and: Carbon atoms are optionally surrounded by one or more -R Q2CMM Group substitution; The sulfur atom, if present, may optionally be replaced by one or two =O groups; and The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R Q2CMM -C(=O)R Q2CMM -C(=O)OR Q2CMM -C(=O)NH2, -C(=O)NHR Q2CMM -C(=O)NR Q2CMM 2 and -S(=O)2 RQ2CMM ;and Each -R Q2CMM Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-4 The alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; And among them: Each -R Q2N Independently: -R Q2NC 、 =O、-C(=O)R Q2NC , -C(=O)-L Q2N -OH、-C(=O)-L Q2N -OR Q2NC 、 -C(=O)-L Q2N -NH2, -C(=O)-L Q2N -NHR Q2NC -C(=O)-L Q2N -NR Q2NC 2. -C(=O)-L Q2N -R Q2NM 、 -C(=O)OR Q2NC 、 -L Q2N -NH2, -L Q2N -NHR Q2NC -L Q2N -NR Q2NC 2.-L Q2N -R Q2NM 、 -C(=O)NH2、-C(=O)NHR Q2NC 、-C(=O)NR Q2NC 2、-C(=O)R Q2NM 、 -L Q2N -C(=O)NH2、-L Q2N -C(=O)NHR Q2NC -L Q2N -C(=O)NR Q2NC 2. -L Q2N -C(=O)R Q2NM or -S(=O)2R Q2NC ; in: Each -R Q2NC Independently saturated C for straight or branched chains 1-6 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-6 The alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; Each -L Q2N - Independently saturate C for straight or branched chains 1-4 Alkylene; Each -R Q2NM Independently a non-aromatic C having at least one N ring atom 3-11 Heterocyclic group, and connected through the N-ring atom; and: Carbon atoms are optionally surrounded by one or more -R Q2NMM Group substitution; The sulfur atom, if present, may optionally be replaced by one or two =O groups; and The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R Q2NMM -C(=O)R Q2NMM -C(=O)OR Q2NMM -C(=O)NH2, -C(=O)NHR Q2NMM -C(=O)NR Q2NMM 2 and -S(=O)2R Q2NMM ;and Each -R Q2NMM Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-4 The alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; And among them: Each -R Q3C Independently: -F, -Cl, -Br, -I, -R Q3CC 、 -R Q3CX 、-OR Q3CX 、 -OH、-OR Q3CC 、 -L Q3C -OH、-L Q3C -OR Q3CC 、 -NH2, -NHR Q3CC 、-NR Q3CC 2.-R Q3CM 、 -L Q3C -NH2, -L Q3C -NHR Q3CC -L Q3C -NR Q3CC 2.-L Q3C -R Q3CM 、 -NHC(=O)R Q3CC 、-NHC(=O)OR Q3CC 、 -L Q3C -NHC(=O)R Q3CC 、-L Q3C -NHC(=O)OR Q3CC 、 -C(=O)NH2、-C(=O)NHR Q3CC 、-C(=O)NR Q3CC 2、-C(=O)R Q3CM 、 -L Q3C -C(=O)NH2、-L Q3C -C(=O)NHR Q3CC -L Q3C -C(=O)NR Q3CC 2.-L Q3C -C(=O)R Q3CM 、 -C(=O)OH、-C(=O)OR Q3CC 、 -OC(=O)R Q3CC 、 -OC(=O)NH2、-OC(=O)NHR Q3CC -OC(=O)NR Q3CC 2、-OC(=O)R Q3CM 、 -S(=O)2R Q3CC 、S(=O)2R Q3CM ; -CN or -NO2; And two adjacent -R Q3C If present, they can co-form -(CH2). n3 -O-(CH2) m3 -、-(CH2) n3 -NH-(CH2) m3 -、-(CH2) q3 (C(O))-NH-(CH2) v3 -、-NH-(CH2) q3 C(O)(CH2) v3 -O-, -NH-(CH2) p3 -NH- or -O-(CH2) p3 -O-, where: n3 is 0, 1, 2 or 3; m3 is 0, 1, 2 or 3; p3 is 1 or 2; q3 is 0, 1, 2 or 3; v3 is 0, 1, 2 or 3, provided that m3+n3 is 2 or 3; in: Each -R Q3CC Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, C 3-7 Heterocyclic group, phenyl, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-4 The alkyl group is optionally substituted with -F, -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; Each -R Q3CX Independently saturated C for straight or branched chains 1-4 Halogenated alkyl groups; Each -L Q3C - Independently saturate C for straight or branched chains 1-4 Alkylene; Each -R Q3CM Independently a non-aromatic C having at least one N ring atom 3-11 Heterocyclic group, and connected through the N-ring atom; and: Carbon atoms are optionally surrounded by one or more -R Q3CMM Group substitution; The sulfur atom, if present, may optionally be replaced by one or two =O groups; and The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R Q3CMM -C(=O)R Q3CMM -C(=O)OR Q3CMM -C(=O)NH2, -C(=O)NHR Q3CMM -C(=O)NR Q3CMM 2 and -S(=O)2R Q3CMM ;and Each -R Q3CMM Independently saturated with linear or branched -F, C 1-4 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-4 The alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; And among them: Each -R Q4C Independently: -F、 -R Q4CC 、-R Q4CX 、 -OH、-OR Q4CC 、-OR Q4CX 、 -NH2, -NHR Q4CC 、-NR Q4CC 2.-R Q4CM 、 -NHC(=O)R Q4CC 、-NHC(=O)OR Q4CC 、 -C(=O)NH2、-C(=O)NHR Q4CC 、-C(=O)NR Q4CC 2、-C(=O)R Q4CM 、 -C(=O)OH、-C(=O)OR Q4CC 、 -OC(=O)R Q4CC 、 -OC(=O)NH2, -OC(=O)NHR Q4CC , -OC(=O)NR Q4CC 2, -OC(=O)R Q4CM or =O; in: Each -R Q4CC Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, C 3-7 Heterocyclic group, phenyl, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-4 The alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; Each -R Q4CX Independently saturated C for straight or branched chains 1-4 Halogenated alkyl groups; Each -R Q4CM Independently a non-aromatic C having at least one N ring atom 3-11 Heterocyclic group, and connected through the N-ring atom; and: Carbon atoms are optionally surrounded by one or more -R Q4CMM Group substitution; The sulfur atom, if present, may optionally be replaced by one or two =O groups; and The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R Q4CMM -C(=O)R Q4CMM -C(=O)OR Q4CMM -C(=O)NH2, -C(=O)NHR Q4CMM -C(=O)NR Q4CMM 2 and -S(=O)2R Q4CMM ; Each -R Q4CMM Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-4 The alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; And among them: Each -R Q5C Independently: -F、-OH、-OR Q5CC 、-OCF3、 -NH2, -NHR Q5CC 、-NR Q5CC 2.-R Q5CM 、 -NHC(=O)R Q5CC 、-NHC(=O)OR Q5CC 、 -C(=O)NH2、-C(=O)NHR Q5CC 、-C(=O)NR Q5CC 2、-C(=O)R Q5CM 、 -C(=O)OH、-C(=O)OR Q5CC 、 -OC(=O)R Q5CC 、 -OC(=O)NH2, -OC(=O)NHR Q5CC , -OC(=O)NR Q5CC 2 or -OC(=O)R Q5CM ; in: Each -R Q5CC Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, C 3-7 Heterocyclic group, phenyl, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-4 The alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2; Each -R Q5CM Independently a non-aromatic C having at least one N ring atom 3-11 Heterocyclic group, and connected through the N-ring atom; and: Carbon atoms are optionally surrounded by one or more -R Q5CMM Group substitution; The sulfur atom, if present, may optionally be replaced by one or two =O groups; and The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R Q5CMM -C(=O)R Q5CMM -C(=O)OR Q5CMM -C(=O)NH2, -C(=O)NHR Q5CMM -C(=O)NR Q5CMM 2 and -S(=O)2R Q5CMM ; Each -R Q5CMM Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, phenyl, phenyl-C 1-3 Alkyl, C 5-6 heteroaryl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-4 The alkyl group is optionally substituted with -OH or -OCH3, and each cycloalkyl, phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CF3, -OH, -OCH3, -NH2, -NH(CH3) and -N(CH3)2.

2. The compound according to claim 1, or a pharmaceutically acceptable salt or solvate thereof, wherein: -R A1 -R A11 ;and -R A11 -R A111 -F, -Cl, or -Br; and Each -R A111 Independently saturated C for straight or branched chains 1-4 alkyl.

3. The compound according to any one of the preceding claims, or a pharmaceutically acceptable salt or solvate thereof, wherein: -R A2 -R A22 ; -R A22 -R A222 -F, -Cl, or -Br; and Each -R A222 Independently saturated C for straight or branched chains 1-4 alkyl.

4. The compound according to any one of the preceding claims, or a pharmaceutically acceptable salt or solvate thereof, wherein: -R A3 -H or -R A33 ;and -R A33 It is -Br.

5. The compound according to any one of the preceding claims, or a pharmaceutically acceptable salt or solvate thereof, wherein: -R A4 -H or -R A44 ; -R A44 -R A444 -Cl or -Br; and Each -R A444 Independently saturated C for straight or branched chains 1-4 alkyl.

6. The compound according to any one of the preceding claims, or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring B is selected from: in: Y 1 For S or O; Y 2 For CH, CR Y2 Or N; Y 3 Let N be N; and Each -R Y2 Independently -NH2.

7. The compound according to any one of the preceding claims, or a pharmaceutically acceptable salt or solvation thereof, wherein: -Q is -Q 1 、or -L Q1 -Q 1 ;in: Q 1 C 5-10 Mixed aromatics; and: Carbon atoms are optionally surrounded by one or more -R Q1C Group substitution; and Secondary nitrogen atoms, if present, are optionally surrounded by one or more -R atoms. Q1N Group substitution; and -L Q1 - For straight-chain or branched saturation C 1-4 Alkylene; in Each -R Q1C Independently: -F, -Cl, -Br -R Q1CC 、 -R Q1CX 、-OR Q1CX 、 -OH、-OR Q1CC 、 -NH2, -NHR Q1CC 、-NR Q1CC 2.-R Q1CM 、 -L Q1C -R Q1CM 、 -NHC(=O)R Q1CC 、-N(R Q1CC )C(=O)R Q1CC 、-NHC(=O)OR Q1CC 、 -C(=O)NH2、-C(=O)NHR Q1CC 、-C(=O)NR Q1CC 2、-C(=O)R Q1CM 、=O、 -NHC(=O)NHR Q1CC 、 -L Q1C -C(=O)NR Q1CC 2、 -C(=O)OH、-C(=O)OR Q1CC 、 -OC(=O)NH2、 -S(=O)2R Q1CX 、 -S(=O)2R Q1CM 、 -NHS(=O)R Q1CC ,-NHS(=O)2R Q1CC 、 -CN or -C≡CH; in: Each -R Q1CC Independently saturated C for straight or branched chains 1-6 Alkyl, C 2-6 alkenyl, C 3-6 cycloalkyl, C 3-7 Heterocyclic, phenyl or C 5-6 heteroaryl, of which C 1-6 The alkyl group is optionally substituted with -OH, -CN or -OCH3, and each phenyl and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -CH3, -CHF2, -CF3, -OCH3; Each -R Q1CX Independently saturated C for straight or branched chains 1-4 Halogenated alkyl groups; Each -L Q1C - Independently saturate C for straight or branched chains 1-4 Alkylene; Each -R Q1CM Independently a non-aromatic C having at least one N ring atom 3-11 Heterocyclic group, and connected through the N-ring atom; and: Carbon atoms are optionally surrounded by one or more -R Q1CMM Group substitution; The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R Q1CMM ;and Each -R Q1CMM Independently saturated C with -F, -NH2, straight or branched chains 1-4 Alkyl, C 1-4 Alkyl OC(=O)NH-, C 3-6 cycloalkyl, wherein C 1-4 Alkyl groups may optionally be substituted with -OH; And among them: Each -R Q1N Independently: -R Q1NC 、-L Q1N -R Q1NC 、 -R Q1NX 、 -R Q1Nhet 、-L Q1N -RQ 1Nhet 、 -L Q1N -OH、-L Q1N -OR Q1NC 、 -S(=O)2R Q1NC 、 -L Q1N -C(=O)OH、-L Q1N -C(=O)OR Q1NC 、 -L Q1N -C(=O)NH2、-L Q1N -C(=O)NHR Q1NK -L Q1N -C(=O)NR Q1NC 2.-L Q1N -C(=O)R Q1NP 、 -L Q1N -NH2, -L Q1N -NR Q1NC 2. or -L Q1N -NHC(=O)OR Q1NC ; in: Each -R Q1NC Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, phenyl or C 5-6 heteroaryl, wherein each C 1-4 The alkyl group is optionally substituted with -F, -OH, -C≡N, -SO₂-CH₃, or -OCH₃, wherein each cycloalkyl, phenyl, and heteroaryl group is optionally substituted with one or more groups selected from the following: -F, -Cl, -Br, straight-chain or branched saturated C 1-4 Alkyl, -CHF2, -CF3, -CH2-O-CH3, -OCH2CH3, -C(=O)-NH-phenyl, wherein C 1-4 Alkyl and phenyl groups may optionally be substituted with -CH3 or -OH; Each -R Q1NX Independently saturated C for straight or branched chains 1-4 Halogenated alkyl groups; Each -L Q1N - Independently saturate C for straight or branched chains 1-4 Alkylene; wherein C 1-4 The alkylene group may optionally be replaced by -OH or -OMe; And among them: Each -R Q1Nhet Independently non-aromatic C 3-7 Heterocyclic group, and: Carbon atoms are optionally replaced by one or more =O atoms; and The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R Q1NHH -C(=O)R QINJJ -C(=O)OR Q1NHH -C(=O)NHR Q1NHH -C(=O)NR Q1NHH 2; in: Each -R Q1NHH Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, phenyl-C 1-3 alkyl; And among them: -R Q1NJJ -R J1 -L J -R J2 -R J3 -L J -R J3 -R J4 -L J -R J4 or -L J -R J5 ; -R J1 For straight-chain or branched saturated C 1-6 Alkyl group; and optionally substituted with one or more groups selected from the following: -F, -OH, -OR JJ -O-phenyl, -C(=O)OR JJ ; Each -R J2 Independently for C 3-6 cycloalkyl; Each -R J3 Independently non-aromatic C 3-7 Heterocyclic groups; Each -R J4 It is phenyl; and optionally substituted with one or more groups selected from the following: -F, -OR JJ -NH2 and -NR JJ 2; Each -R J5 Independently for C 5-6 Mixed aromatics; Each -L J - Independently saturate C for straight or branched chains 1-4 Alkylene, and optionally substituted with one or more -F; Each -R JJ For straight-chain or branched saturated C 1-4 alkyl; And among them: -R Q1NK -R K1 -R K2 -R K3 -L K -R K3 ; -R K1 For straight-chain or branched saturated C 1-7 Alkyl group; and optionally substituted with one or more groups selected from the following: -F, -OH, -OR KK -OCH2CH2OCH3 and -NR KK 2; Each -R K2 Independently for C 3-6 cycloalkyl; Each -R K3 Independently non-aromatic C 3-7 Heterocyclic group; and: The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R KK and -C(=O)OR KK ; Each -L K - For straight-chain or branched saturation C 1-4 Alkylene Each -R KK For straight-chain or branched saturated C 1-4 alkyl; And among them: -R Q1NP A non-aromatic C having at least one N-ring atom 3-11 Heterocyclic group, and connected through the N-ring atom; and: Carbon atoms are optionally surrounded by one or more atoms selected from -R Q1NPP -F, -OH, -OR Q1NPP Substitution of groups with =O; and The secondary nitrogen atom, if present, may optionally be substituted with a group selected from the following: -R Q1NPP -R Q1NPPX -C(=O)R Q1NPP -C(=O)OR Q1NPP -C(=O)NR Q1NPP 2 and -S(=O)2R Q1NPP ; Each -R Q1NPP Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, phenyl, of which C 1-4 The alkyl group may optionally be substituted with -F, -OH or -OCH3; -R Q1NPPX For straight-chain or branched saturated C 1-4 Halogenated alkyl groups.

8. The compound according to any one of claims 1-6, or a pharmaceutically acceptable salt or solvate thereof, wherein: -Q is -Q 2 、or -L Q2 -Q 2 ;in: Q 2 C 3-10 Heterocyclic groups; and: The sulfur atom, if present, may optionally be replaced by one or two =O groups; Secondary nitrogen atoms, if present, are optionally surrounded by one or more -R atoms. Q2N Group substitution; and -L Q2 - For straight-chain or branched saturation C 1-4 Alkylene; in Each -R Q2N Independently: -R Q2NC 、 =O、-C(=O)R Q2NC 、 -C(=O)-L Q2N -R Q2NM 、 -C(=O)OR Q2NC 、 -L Q2N -C(=O)NR Q2NC 2 or -S(=O)2R Q2NC ; in: Each -R Q2NC Independently saturated C for straight or branched chains 1-6 Alkyl, phenyl-C 1-3 Alkyl or C 5-6 heteroaryl-C 1-3 Alkyl, wherein C 1-6 The alkyl group is optionally substituted with -OH, and each phenyl and heteroaryl group is optionally substituted with one or more groups selected from -Cl and -OCH3; Each -L Q2N - Independently saturate C for straight or branched chains 1-4 Alkylene; Each -R Q2NM Independently a non-aromatic C having at least one N ring atom 3-11 Heterocyclic groups, and connected through the N-ring atoms.

9. The compound according to any one of claims 1-6, or a pharmaceutically acceptable salt or solvate thereof, wherein: -Q is -Q 3 or -L Q3 -Q 3 ; Q 3 It is phenyl; And optionally by one or more -R Q3C Group substitution; and -L Q3 - For straight-chain or branched saturation C 1-4 Alkylene; And among them: Each -R Q3C Independently: -F、 -R Q3CC 、 -R Q3CX 、 -OH、-OR Q3CC 、 -NHC(=O)R Q3CC 、 -C(=O)NHR Q3CC -C(=O)R Q3CM 、 -S(=O)2R Q3CC 、S(=O)2R Q3CM ; And two adjacent -R Q3C If present, they can co-form -NH-(CH2). q3 C(O)(CH2) v3 -O-, where q3 is 0 and v3 is 1; in: Each -R Q3CC Independently saturated C for straight or branched chains 1-4 Alkyl, C 3-6 cycloalkyl, C 3-7 Heterocyclic groups, where C 1-4 Alkyl groups are optionally substituted with -F; Each -R Q3CX Independently saturated C for straight or branched chains 1-4 Halogenated alkyl groups; Each -R Q3CM Independently a non-aromatic C having at least one N ring atom 3-11 Heterocyclic group, and connected through the N-ring atom; and: Carbon atoms are optionally surrounded by one or more -R Q3CMM Group substitution; Each -R Q3CMM Independently -F.

10. The compound according to any one of claims 1-6, or a pharmaceutically acceptable salt or solvate thereof, wherein: -Q is -Q 4 、or -L Q4 -Q 4 , Q 4 C 3-10 Carbocyclic group; and -L Q4 - For straight-chain or branched saturation C 1-4 Alkylene.

11. The compound according to any one of claims 1-6, or a pharmaceutically acceptable salt or solvate thereof, wherein: -Q is -Q 5 、 or -H; Q 5 For straight-chain or branched saturated C 1-6 alkyl; And optionally by one or more -R Q5C Group substitution; in Each -R Q5C Independently: -OH、-OR Q5CC 、 -NHC(=O)R Q5CC 、-NHC(=O)OR Q5CC 、 -C(=O)NH2、-C(=O)NHR Q5CC 、-C(=O)R Q5CM , in: Each -R Q5CC Independently saturated C for straight or branched chains 1-4 alkyl; Each -R Q5CM Independently a non-aromatic C having at least one N ring atom 3-11 Heterocyclic groups, and connected through the N-ring atoms.

12. A pharmaceutical composition comprising: The compound according to any one of claims 1-11, or Its pharmaceutically acceptable salts or solvates, and Pharmaceutically acceptable carriers or diluents.

13. Use of the compound or a pharmaceutically acceptable salt or solvate thereof according to any one of claims 1-11 in a method of treating a human or animal body by means of treatment.

14. Use of the compound or a pharmaceutically acceptable salt or solvate thereof according to any one of claims 1-11 in the preparation of a medicament for treating proliferative diseases.

15. A method of treating a proliferative disease in a human or animal body, comprising administering to a subject requiring treatment a therapeutically effective amount of the compound according to any one of claims 1-11 or a pharmaceutically acceptable salt or solvate thereof.

16. Use of the compound, salt, or solvate according to claim 14, or the method according to claim 15, The proliferative disease mentioned above is cancer.

17. Use of the compound, salt, or solvate according to claim 14, or the method according to claim 15. The proliferative diseases mentioned above are: endometrial cancer, uterine cancer, ovarian cancer, breast cancer, gastric cancer, bladder cancer, pancreatic cancer, mesothelioma, kidney cancer, stomach cancer, esophageal cancer, colorectal cancer, glioblastoma, or lung cancer.