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公开(公告)号:US20240228494A1
公开(公告)日:2024-07-11
申请号:US18556260
申请日:2022-04-25
发明人: David MILLER , Tom MCCARTHY , Alan NAYLOR , Gavin MILNE
IPC分类号: C07D471/18 , A61K31/4353 , A61K31/519
CPC分类号: C07D471/18 , A61K31/4353 , A61K31/519
摘要: One aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, (I) ring A is an is optionally substituted 5 or 6 membered aromatic or heteroaromatic ring; Y is selected from CH2, C═N—OH, and CR10R10′; Ra and Rb are each independently selected from H and alkyl; Z is selected from O, S, NR17 and CR18; X is selected from O and NH; p is 0, 1 or 2; q is 0 or 1; and r is 0 or 1; wherein at least one of p, q and r is other than zero, and with the proviso that: (i) when r is 0, p is 1 and q is 1, when X is NH, Z is other than O; (ii) when r and q are both 0, and p is 1, Z is not O; R1, R4, and R5 are each independently selected from H, alkyl, alkoxy, OH, F, Cl, Br, and I; R2 and R3 are each independently selected from H, F, Cl, Br, I, CN, methoxy, haloalkyl, haloalkoxy and CO2-alkyl; R10 and R10′ are each independently selected from H, F, alkyl, and haloalkyl; R15 and R16 are each independently selected from H, alkoxy, alkyl and OH; R17 is selected from H, CN, OH, alkoxy and alkyl; R18 is NO2 or CN; and wherein the compound is other than: (6S,9R)-10-benzyl-4-chloro-6,7,8,9-tetrahydro-5H-6,9-epiminocyclohepta[d]-pyrimidine; (6S,9R)-10-benzyl-1,5,6,7,8,9-hexahydro-4H-6,9-epiminocyclohepta[d]pyrimidin-4-one; (6R,9S)-10-benzyl-1,5,6,7,8,9-hexahydro-4H-6,9-epiminocyclohepta[d]pyrimidin-4-one; 10-benzyl-1,5,6,7,8,9-hexahydro-4H-6,9-epiminocyclohepta[d]pyrimidin-4-one; 10-(2,4,6-trimethoxybenzyl)-6,7,8,9-tetrahydro-5H-5,8-epiminocyclohepta[d]-pyrimidine; and 2-methoxy-5-((6,7,8,9-tetrahydro-5H-5,8-epiminocyclohepta[d]pyrimidin-10-yl)methyl)-benzonitrile. Further aspects of the invention relate to compounds of formula (I) for use in the field of immuno-oncology, immunology, and related applications.
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公开(公告)号:US20240051961A1
公开(公告)日:2024-02-15
申请号:US18257540
申请日:2021-12-17
发明人: Tom MCCARTHY , Alan NAYLOR , Gavin MILNE , David MILLER , Maria IEVA
IPC分类号: C07D471/18 , C07D519/00
CPC分类号: C07D471/18 , C07D519/00
摘要: The present invention relates to compounds of formula (I) as GPR65 modulators for the treatment of a proliferative disorder, such as e.g. cancer, an immune disorder, asthma, chronic obstructive pulmonary disease (CORD) or acute respiratory distress syndrome (ARDS). Preferred compounds are e.g. N-(Pyridin-2-yl)-6,7,8,9-tetrahydro-5H-5,8-epiminocyclohepta[c]pyridine-10-carboxamide derivatives and similar compounds, such as e.g. (5R,8S)—N-(4-chloro-5-(trifluoromethyl)pyridin-2-yl)-1-fluoro-6,7,8,9-tetrahydro-5H-5,8-epiminocyclohepta[c]pyridine-10-carboxamide (compound 1)
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公开(公告)号:US20230373989A1
公开(公告)日:2023-11-23
申请号:US17999008
申请日:2021-06-04
发明人: Tom MCCARTHY , Gavin MILNE , Tobias MOECHEL , Alan NAYLOR , David MILLER
IPC分类号: C07D451/00 , C07D451/02
CPC分类号: C07D451/00 , C07D451/02
摘要: One aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, (I) wherein: ring A is a 5 or 6 membered aromatic or heteroaromatic ring, wherein said aromatic or heteroaromatic ring is optionally substituted with one or more substituents selected from F, Cl, Br, I, CN, alkoxy, NR11R11′, OH, alkyl, haloalkyl, aralkyl, aryl, and heteroaryl, and wherein said aryl and heteroaryl substituents are in turn optionally substituted with one or more substituents each independently selected from F, Cl, Br, I, CN, alkoxy, NR11R11′, OH, alkyl, haloalkyl, and aralkyl; Y is selected from C═N—OH and CR10R10′, wherein R10 and R10′, are each independently selected from H, F, alkyl, and haloalkyl; R1, R4, and R5 are each independently selected from H, F, Cl, Br, and I; R2 and R3 are each independently selected from H, F, Cl, Br, I, CN, methoxy, and haloalkyl; and R11 and R11′ wherein R12 and R13 are both alkyl; for use as a medicament. Further aspects of the invention relate to compounds of formula (I) for use in the field of immuno-oncology, immunology, and related applications, and compounds of formula (I) per se.
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