公开(公告)号：US12129250B2

公开(公告)日：2024-10-29

申请号：US18372417

申请日：2023-09-25

申请人： LYNK PHARMACEUTICALS CO. LTD.

发明人： Zhaokui Wan ,  Michael Lawrence Vazquez ,  Gurmit Grewal ,  Xiaodong Li ,  Lin Su ,  Jingyu Wu

IPC分类号： C07D471/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D471/18 ,  C07D487/04 ,  C07D487/08 ,  C07D491/04 ,  C07D495/04 ,  C07D498/08 ,  C07D498/18

CPC分类号： C07D471/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D471/18 ,  C07D487/04 ,  C07D487/08 ,  C07D491/04 ,  C07D495/04 ,  C07D498/08 ,  C07D498/18

摘要： The invention provides a novel class of therapeutic agents that are safe and effective TYK2 inhibitors and pharmaceutical compositions of these compounds and methods of preparation and use thereof against various TYK2-mediated diseases and disorders.

公开(公告)号：US12084455B2

公开(公告)日：2024-09-10

申请号：US17224557

申请日：2021-04-07

申请人： Gilead Sciences, Inc.

发明人： Elizabeth M. Bacon ,  Elbert Chin ,  Jeromy J. Cottell ,  Ashley Anne Katana ,  Darryl Kato ,  John O. Link ,  Nathan Shapiro ,  Teresa Alejandra Trejo Martin ,  Zheng-Yu Yang

IPC分类号： C07D405/14 ,  A61K31/52 ,  A61K31/55 ,  A61K31/553 ,  A61K31/685 ,  A61K31/688 ,  A61K45/06 ,  A61P31/18 ,  C07C243/28 ,  C07C275/16 ,  C07D401/12 ,  C07D403/12 ,  C07D471/08 ,  C07D487/08 ,  C07D487/10 ,  C07D491/04

CPC分类号： C07D487/08 ,  A61K31/52 ,  A61K31/55 ,  A61K31/553 ,  A61K31/685 ,  A61K31/688 ,  A61K45/06 ,  A61P31/18 ,  C07C243/28 ,  C07C275/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D471/08 ,  C07D487/10 ,  C07D491/04

摘要： The invention provides a compound of Formula I:






or a pharmaceutically acceptable salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS symptoms in a mammal using compounds of Formula I.

公开(公告)号：US12006322B2

公开(公告)日：2024-06-11

申请号：US18471250

申请日：2023-09-20

申请人： Xinthera, Inc.

发明人： Robert L. Hoffman ,  Porino Jinjo Va ,  Joseph Robert Pinchman ,  Qing Dong ,  Stephen W. Kaldor

IPC分类号： A61K31/444 ,  C07D213/81 ,  C07D487/04 ,  C07D491/04

CPC分类号： C07D487/04 ,  C07D491/04

摘要： Described herein are tricyclic PARP1 inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of cancer and are of Formula (Ip):

公开(公告)号：US20240158364A1

公开(公告)日：2024-05-16

申请号：US18511612

申请日：2023-11-16

申请人： Vandria SA

发明人： Christopher L. Rinsch ,  Penelope Andreux ,  Jonathan Mark Sutton ,  Eileen Mary Seward ,  Jamie D. Knight ,  Ian Linney ,  Peter C. Sennhen ,  Said Oumouch ,  Florent Beaufils ,  Thomas Christian Fessard

IPC分类号： C07D311/80 ,  C07D217/24 ,  C07D279/02 ,  C07D407/12 ,  C07D491/04 ,  C07D491/107 ,  C07D493/04 ,  C07D493/10

CPC分类号： C07D311/80 ,  C07D217/24 ,  C07D279/02 ,  C07D407/12 ,  C07D491/04 ,  C07D491/107 ,  C07D493/04 ,  C07D493/10

摘要： Disclosed are compounds, compositions, and methods useful for treating neuronal and mitochondrial diseases.

公开(公告)号：US11939337B2

公开(公告)日：2024-03-26

申请号：US17864198

申请日：2022-07-13

申请人： UNIVERSITY OF PUERTO RICO

发明人： Cornelis P. Vlaar ,  Suranganie Dharmawardhane Flanagan ,  Eliud Hernandez-O'Farrill ,  Linette Castillo-Pichardo

IPC分类号： C07D491/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14 ,  C07D491/048

CPC分类号： C07D491/048 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/14

摘要： Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.

公开(公告)号：US11932658B2

公开(公告)日：2024-03-19

申请号：US17142288

申请日：2021-01-06

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Xiaojun Zhang ,  Eldon Scott Priestley ,  Oz Scott Halpern ,  Wen Jiang ,  Samuel Kaye Reznik ,  Jeremy M. Richter

IPC分类号： C07D491/04 ,  A61K31/498 ,  A61P7/02 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D515/14 ,  C07D519/00

CPC分类号： C07D519/00 ,  A61P7/02 ,  C07D515/14

摘要： Disclosed are compounds of Formula (I) to (VIII):




or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R3 is a tricyclic heteroaryl group substituted with R3a and zero to 2 R3b; and Ri, R2, R3a, R3b, R4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.

公开(公告)号：US11884661B2

公开(公告)日：2024-01-30

申请号：US17184179

申请日：2021-02-24

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Guohua Zhao ,  Pratik Devasthale ,  Xiang-Yang Ye ,  Kumaravel Selvakumar ,  Suresh Dhanusu ,  Palanikumar Balasubramanian ,  Leatte R. Guernon ,  Rita Civiello ,  Xiaojun Han ,  Michael Frederick Parker ,  Swanee E. Jacutin-Porte

IPC分类号： C07D471/04 ,  C07D491/04 ,  C07D519/00 ,  A61P11/00 ,  A61P19/10 ,  A61P35/00 ,  A61P37/06

CPC分类号： C07D471/04 ,  A61P11/00 ,  A61P19/10 ,  A61P35/00 ,  A61P37/06 ,  C07D491/04 ,  C07D519/00

摘要： The present invention provides compounds of Formula (I):




or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to αV-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of αv-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

公开(公告)号：US11858943B2

公开(公告)日：2024-01-02

申请号：US17500780

申请日：2021-10-13

申请人： Neumora Therapeutics, Inc.

发明人： Robert M. Jones ,  Mariangela Urbano ,  Gary Brandt ,  David Hardick ,  Chris Knight ,  Jason Tierney

IPC分类号： C07D487/04 ,  A61P15/08 ,  A61P15/10 ,  A61P25/20 ,  C07D498/04 ,  A61P9/06 ,  A61P25/18 ,  A61P25/22 ,  C07D491/04 ,  A61P25/24

CPC分类号： C07D487/04 ,  A61P9/06 ,  A61P15/08 ,  A61P15/10 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  C07D491/04 ,  C07D498/04

摘要： Compounds are provided that antagonize vasopressin receptors, particularly the V1a receptor products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof:




wherein A, B, G, R1, R1b, R1c, R2 and X are as defined herein.

公开(公告)号：US20230348473A1

公开(公告)日：2023-11-02

申请号：US18140370

申请日：2023-04-27

申请人： Xinthera, Inc.

发明人： Robert L. HOFFMAN ,  Porino Jinjo VA ,  Joseph Robert PINCHMAN ,  Qing DONG ,  Stephen W. KALDOR

IPC分类号： C07D487/04 ,  C07D491/04

CPC分类号： C07D487/04 ,  C07D491/04

摘要： Described herein are tricyclic PARP1 inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of cancer.

公开(公告)号：US20230348416A1

公开(公告)日：2023-11-02

申请号：US18023411

申请日：2021-08-31

申请人： Heptares Therapeutics Limited

发明人： Sarah Joanne BUCKNELL ,  Stephen Paul WATSON ,  Michael Alistair O'BRIEN

IPC分类号： C07D401/04 ,  C07D405/14 ,  C07D491/04

CPC分类号： C07D401/04 ,  C07D405/14 ,  C07D491/04

摘要： The disclosures herein relate to novel compounds of Formula (1): or a salt thereof, wherein Q, V, L, W, R1 and R2 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with GPR52 receptors.