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1. 发明申请

WO2022229615A1 COMPOUNDS 审中-公开
公开(公告)号：WO2022229615A1
公开(公告)日：2022-11-03
申请号：PCT/GB2022/051042
申请日：2022-04-25
申请人： PATHIOS THERAPEUTICS LIMITED
发明人： MILLER, David , MCCARTHY, Tom , NAYLOR, Alan , MILNE, Gavin
IPC分类号： C07D471/18 , A61P11/00 , A61P35/00 , A61P37/00 , A61K31/46 , 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.

2. 发明申请

WO2021245427A1 N-PHENYLAMINOCARBONYL PYRIDINO-, PYRIMIDINO AND BENZO-TROPANES AS MODULATORS OF GPR65 审中-公开
公开(公告)号：WO2021245427A1
公开(公告)日：2021-12-09
申请号：PCT/GB2021/051397
申请日：2021-06-04
申请人： PATHIOS THERAPEUTICS LIMITED
发明人： MCCARTHY, Tom , MILNE, Gavin , MOECHEL, Tobias , NAYLOR, Alan , MILLER, David
IPC分类号： A61P9/10 , A61P11/06 , A61P35/00 , A61P37/02 , C07D451/00 , C07D471/08 , C07D487/04 , A61K31/46
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' are each independently selected from H, alkyl, haloalkyl, COR12, and SO2R13, 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.

3. 发明申请

WO2021245426A1 N-(PHENYLAMINOCARBONYL) TETRAHYDRO-ISOQUINOLINES AND RELATED COMPOUNDS AS MODULATORS OF GPR65 审中-公开
公开(公告)号：WO2021245426A1
公开(公告)日：2021-12-09
申请号：PCT/GB2021/051396
申请日：2021-06-04
申请人： PATHIOS THERAPEUTICS LIMITED
发明人： MCCARTHY, Tom , MILNE, Gavin , MOECHEL, Tobias , NAYLOR, Alan
IPC分类号： A61P9/10 , A61P11/06 , A61P35/00 , A61P37/02 , C07D217/02 , C07D217/24 , C07D413/04 , C07D471/04 , C07D487/04 , C07D487/14 , C07D498/04 , A61K31/47 , A61K31/5365 , A61K31/4738 , C07D217/06 , C07D409/04 , C07D471/14
摘要： The present invention relates to a compound of formula (Ia), or a pharmaceutically acceptable salt or solvate thereof, (I) wherein: ring A is a 5- or 6-membered monocyclic aromatic or heteroaromatic ring, or a 9- or 10-membered bicyclic aromatic or heteroaromatic ring, each of which is optionally substituted with one or more substituents selected from F, Cl, Br, I, CN, alkoxy, NR11R11', OH, SO2-alkyl, CO2-alkyl, 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 and Z are each independently 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, I and haloalkyl; R2 and R3 are each independently selected from H, F, Cl, Br, I, CN, and haloalkyl; wherein at least two of R2, R3 and R4 are other than H; and R11 and R11' are each independently selected from H, alkyl, haloalkyl, COR12, and SO2R13, wherein R12 and R13 are both alkyl; wherein the compound is other than: N-(3,4-Dichlorophenyl)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxamide; N-(3,4-Dichlorophenyl)-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-carboxamide; N-(4-Chloro-3-(trifluoromethyl)phenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide; N-(3,4-dichlorophenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide; N-(3,4-Dichlorophenyl)-6,7-dihydroisoxazolo[4,5-c]pyridine-5(4H)-carboxamide; and N-(3,4-Dichlorophenyl)-4-methyl-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-carboxamide. Further aspects of the invention relate to such compounds for use in the field of immunooncology, immunology, and related applications.

4. 发明申请

WO2023067322A1 TRICYCLIC GPR65 MODULATORS 审中-公开
公开(公告)号：WO2023067322A1
公开(公告)日：2023-04-27
申请号：PCT/GB2022/052644
申请日：2022-10-17
申请人： PATHIOS THERAPEUTICS LIMITED
发明人： MCCARTHY, Tom , NAYLOR, Alan , MILLER, David , MILNE, Gavin , IEVA, Maria , MOCHEL, Tobias , ESVAN, Yannick , FEUTRILL, John
IPC分类号： A61P11/00 , A61P11/06 , A61P35/00 , A61P43/00 , C07D471/18 , A61K31/439
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 B is: a monocyclic aromatic group; or a monocyclic or bicyclic heteroaromatic group, each of which is optionally substituted by halo, CN, OH, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, hydroxycycloalkyl, O-cycloalkyl, alkoxy, haloalkoxy, heterocycloalkyl, O- heterocycloalkyl, aryl, heteroaryl, O-aryl, NHCO-alkenyl, NHCO-aryl, -(CH2)q-O-heteroaryl, CONH-aryl, aryloxy-alkyl, O-aralkyl, and CO2-alkyl, wherein said aryl, heteroaryl, heterocycloalkyl, O-cycloalkyl, NHCO-aryl, -(CH2)q-O-heteroaryl, CONH-aryl, aryloxy-alkyl, O-aralkyl, and O-aryl groups are each optionally further substituted by one or more groups independently selected from halo, alkyl, haloalkyl, alkoxy, NHCO-alkyl, NR13R13', SO2-alkyl, CN, hydroxyalkyl, CONR14R14', alkyl-NR15R15', heterocycloalkyl, alkyl-heterocycloalkyl, alkyl- cycloalkyl, aryl, (CH2)m-NHSO2-alkyl, CO2R16, alkoxy-alkyl, haloalkoxy, O-heterocycloalkyl, heteroaryl, alkoxy-alkoxy, and O-(CH2)p-cycloalkyl, where in the latter group, said cycloalkyl group is optionally further substituted by one or more halo, haloalkyl, alkyl or alkoxy groups; m is an integer from 0 to 3; p and q are each independently 0 to 3; Z is CR12; Y is CR10 R10', wherein R10 and R10' are each independently selected from H, F, alkyl, and haloalkyl; Ra and Rb are each independently selected from H and alkyl; R6 is selected from H, alkyl, cycloalkyl and hydroxyalkyl; R12 is selected from H, alkyl, haloalkyl, halo, OH and O-alkyl; and R13, R13', R14, R14', R15, R15', and R16 are each independently selected from H, alkyl, and alkoxyalkyl. Further aspects of the invention relate to compounds of formula (I) for use as a medicament, particularly in the field of immuno-oncology, immunology, and related applications.

5. 发明申请

WO2022136844A1 N-(PYRIDIN-2-YL)-6,7,8,9-TETRAHYDRO-5H-5,8-EPIMINOCYCLOHEPTA[C]PYRIDINE-10-CARBOXAMIDE DERIVATIVES AND SIMILAR COMPOUNDS AS GPR65 MODULATORS FOR THE TREATMENT OF CANCER 审中-公开
公开(公告)号：WO2022136844A1
公开(公告)日：2022-06-30
申请号：PCT/GB2021/053354
申请日：2021-12-17
申请人： PATHIOS THERAPEUTICS LIMITED
发明人： MCCARTHY, Tom , NAYLOR, Alan , MILNE, Gavin , MILLER, David , LEVA, Maria
IPC分类号： C07D471/18 , C07D487/18 , C07D471/04 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/00 , A61P37/02 , A61P37/04 , A61P37/06 , A61P37/08 , A61P11/00 , A61P11/06 , A61P11/08 , A61P11/10
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)-l-fluoro-6,7,8,9- tetrahydro-5H-5,8-epiminocyclohepta[c]pyridine-10-carboxamide (compound 1)

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