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1. 发明公开

US20240228494A1 COMPOUNDS 审中-公开
公开(公告)号：US20240228494A1
公开(公告)日：2024-07-11
申请号：US18556260
申请日：2022-04-25
申请人： PATHIOS THERAPEUTICS LIMITED
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.

2. 发明公开

US20240190821A1 SULFONAMIDE SUBSTITUTED N-(1H-INDOL-7-YL)BENZENESULFONAMIDES AND USES THEREOF 审中-公开
公开(公告)号：US20240190821A1
公开(公告)日：2024-06-13
申请号：US18275382
申请日：2022-02-01
申请人： Triana Biomedicines, Inc.
发明人： William J. Greenlee , Nicholas Calandra , Soumya Ray , Arthur F. Kluge
IPC分类号： C07D209/40 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04 , C07D471/18 , C07D487/04 , C07D487/10 , C07D498/10
CPC分类号： C07D209/40 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04 , C07D471/18 , C07D487/04 , C07D487/10 , C07D498/10
摘要： The present application discloses novel compounds of formula (I), pharmaceutical compositions containing these compounds and methods of inducing degradation of a protein, comprising contacting the protein with an effective amount of a compound of the disclosure. Methods of treating disease and disorders that results from abnormal activity of a target protein in a subject, are also disclosed.

3. 发明公开

US20240051961A1 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：US20240051961A1
公开(公告)日：2024-02-15
申请号：US18257540
申请日：2021-12-17
申请人： PATHIOS THERAPEUTICS LIMITED
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)

4. 发明公开

US20240043382A1 MODIFIED INDOLE ALKALOIDS FOR THERAPEUTIC USES 审中-公开
公开(公告)号：US20240043382A1
公开(公告)日：2024-02-08
申请号：US18267827
申请日：2021-12-17
申请人： COMPASS PATHFINDER LIMITED
发明人： Ryan PROTZKO
IPC分类号： C07D209/16 , C07D471/14 , C07D471/18 , C12P19/60 , C12P17/18 , C12P17/10 , C12P11/00 , C12P9/00 , C07F9/572 , C07H17/02 , C12N9/12 , C12N9/10 , C12N9/88
CPC分类号： C07D209/16 , C07D471/14 , C07D471/18 , C12P19/60 , C12P17/182 , C12P17/10 , C12P11/00 , C12P9/00 , C07F9/5728 , C07H17/02 , C12N9/1205 , C12N9/1007 , C12N9/13 , C12N9/1033 , C12N9/1051 , C12N9/88 , C12Y201/01049 , C12Y201/01004 , C12Y203/01084 , C12Y204/01017 , C12Y402/0102
摘要： Disclosed herein are enzymatic and modified host cell methods for prepared modified indole alkaloids. Also disclosed herein are modified indole alkaloids and their therapeutic use for treating diseases and disorders.

5. 发明授权

US11814386B2 Fused pyrrolines which act as ubiquitin-specific protease 30 (USP30) inhibitors 有权
公开(公告)号：US11814386B2
公开(公告)日：2023-11-14
申请号：US18048079
申请日：2022-10-20
申请人： FORMA Therapeutics, Inc.
发明人： Alex J. Buckmelter , Justin Andrew Caravella , Hongbin Li , Matthew W. Martin , Steven Mischke , David James Richard , Angela V. West
IPC分类号： C07D471/18 , C07D403/12 , C07D471/08 , C07D487/08 , C07D487/18 , C07D491/107
CPC分类号： C07D471/18 , C07D403/12 , C07D471/08 , C07D487/08 , C07D487/18 , C07D491/107
摘要： The disclosure relates to USP30 Inhibitor Compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, and medical uses involving same.

6. 发明授权

US11680066B2 Ibogaine-related compounds and corresponding methods 有权
公开(公告)号：US11680066B2
公开(公告)日：2023-06-20
申请号：US17300293
申请日：2021-05-13
申请人： Jeffrey Alan McKinney
发明人： Jeffrey Alan McKinney
IPC分类号： A61K31/55 , A61P25/22 , A61P25/30 , C07D471/18
CPC分类号： C07D471/18 , C07B2200/05
摘要： The present invention relates to Ibogaine derivatives and related methods. It more specifically relates to deutero- and fluoro-derivatives of Ibogaine and related methods. In one aspect, the present invention provides a compound. The structure of the compound is shown as compound 1 in FIG. 1. In another aspect, the present invention provides a method of treating an addiction disorder. The method comprises administration of compound 1. In another aspect, the present invention provides a method of treating an anxiety-related disorder or impulse control disorder. The method comprises administration of compound 1.

7. 发明公开

US20230183258A1 NLRP3 MODULATORS 审中-公开
公开(公告)号：US20230183258A1
公开(公告)日：2023-06-15
申请号：US18163680
申请日：2023-02-02
申请人： Zomagen Biosciences Ltd
发明人： Raju MOHAN , John NUSS , Jason HARRIS , Shendong YUAN
IPC分类号： C07D491/18 , C07D513/18 , C07D471/18 , C07D495/18 , A61P29/00 , A61P25/28 , A61P3/10 , A61P9/10
CPC分类号： C07D491/18 , C07D513/18 , C07D471/18 , C07D495/18 , A61P29/00 , A61P25/28 , A61P3/10 , A61P9/10
摘要： Described herein are NLRP3 modulators and methods of utilizing NLRP3 modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

8. 发明公开

US20230151010A1 CRYSTALLINE FORMS OF (9R, 135S)-13- {4-[5-CHLORO-2-(4-CHLORO-1H,2,3- TRIAZOL- 1 -YL)PHENYL] -6-OXO- 1,6-DIHYDROPYRIMIDIN- 1-YL}-3-(DIFLUOROMETHYL)-9-METHYL-3,4,7,15- TETRAAZATRICYCLO [ 12.3.1.0 2·6] OCTADECA- 1(18), 2(6), 4, 14, 16-PENTAEN-8-ONE 审中-公开
公开(公告)号：US20230151010A1
公开(公告)日：2023-05-18
申请号：US17995848
申请日：2021-04-09
申请人： Bristol-Myers Squibb Company , Janssen Pharmaceutica NV
发明人： Andrew K. Dilger , Michael A. Galella , Daniel Smith , Theresa M. Ziemba , David Lüdeker , Christos XIOURAS , Dipali AHUJA , Dirk Angelina J. CLEEREN
IPC分类号： C07D471/18
CPC分类号： C07D471/18 , C07B2200/13
摘要： Disclosed are crystalline forms of Compound (I). Compound (I) is useful as an anti-thromboembolic agent in the treatment of cardiovascular diseases.

9. 发明申请

US20230126252A1 FUSED PYRROLINES WHICH ACT AS UBIQUITIN-SPECIFIC PROTEASE 30 (USP30) INHIBITORS 有权
公开(公告)号：US20230126252A1
公开(公告)日：2023-04-27
申请号：US18048079
申请日：2022-10-20
申请人： FORMA Therapeutics, Inc.
发明人： Alex J. Buckmelter , Justin Andrew Caravella , Hongbin Li , Matthew W. Martin , Steven Mischke , David James Richard , Angela V. West
IPC分类号： C07D471/18 , C07D403/12 , C07D471/08 , C07D487/08 , C07D487/18 , C07D491/107
摘要： The disclosure relates to USP30 Inhibitor Compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, and medical uses involving same.

10. 发明申请

US20230058729A1 MACROCYCLES AS FACTOR XIA INHIBITORS 有权
公开(公告)号：US20230058729A1
公开(公告)日：2023-02-23
申请号：US17493516
申请日：2021-10-04
申请人： Bristol-Myers Squibb Company
发明人： James R. CORTE , Tianan FANG , Carl P. DECICCO , Donald J.P. PINTO , Karen A. ROSSI , Zilun HU , Yoon JEON , Mimi L. QUAN , Joanne M. SMALLHEER , Yufeng WANG , Wu YANG
IPC分类号： C07D487/04 , C07D487/08 , C07D498/08 , C07D487/06 , C07D487/16 , C07D498/06 , C07D471/18 , C07D487/18 , C07D471/14 , C07D487/14 , C07D498/04
摘要： The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

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