公开(公告)号：US20240317769A1

公开(公告)日：2024-09-26

申请号：US18550234

申请日：2022-03-14

Applicant: Bristol-Myers Squibb Company

Inventor： Brian Edward FINK ,  Robert Joseph CHERNEY ,  Khehyong NGU ,  Upender VELAPARTHI ,  Wayne David VACCARO ,  Zheming RUAN ,  Lan-Ying QIN ,  Pravin S. SHIRUDE ,  Hasibur RAHAMAN

IPC: C07D487/08 ,  A61K31/517 ,  C07D471/08 ,  C07D519/00

CPC classification number: C07D487/08 ,  A61K31/517 ,  C07D471/08 ,  C07D519/00

Abstract: The present disclosure relates to KRAS inhibitors. Methods of treating cancers using the compounds are also provided.

公开(公告)号：US20240316161A1

公开(公告)日：2024-09-26

申请号：US18482248

申请日：2023-10-06

Applicant: Bristol-Myers Squibb Company

Inventor： Sharon CLOAD ,  Linda ENGLE ,  Dasa LIPOVSEK ,  Malavi MADIREDDI ,  Ginger Chao RAKESTRAW ,  Joanna SWAIN ,  Wenjun ZHAO ,  Hui WEI ,  Aaron P. YAMNIUK ,  Vidhyashankar RAMAMURTHY ,  Alexander T. KOZHICH ,  Martin J. CORBETT ,  Stanley Richard KRYSTEK, JR.

IPC: A61K38/39 ,  A61K38/00 ,  A61K38/17 ,  A61K45/06 ,  A61K47/60 ,  A61K47/64 ,  C07K14/435 ,  C07K14/765 ,  C07K14/78 ,  C07K14/79 ,  C07K16/18 ,  C07K16/46 ,  G01N33/74

CPC classification number: A61K38/39 ,  A61K38/17 ,  A61K38/1709 ,  A61K45/06 ,  A61K47/60 ,  A61K47/642 ,  C07K14/435 ,  C07K14/765 ,  C07K14/78 ,  C07K14/79 ,  C07K16/18 ,  C07K16/46 ,  G01N33/74 ,  A61K38/00 ,  C07K2319/30 ,  C07K2319/31

Abstract: The present invention relates to fibronectin-based scaffold domain proteins that bind to myostatin. The invention also relates to the use of these proteins in therapeutic applications to treat muscular dystrophy, cachexia, sarcopenia, osteoarthritis, osteoporosis, diabetes, obesity, COPD, chronic kidney disease, heart failure, myocardial infarction, and fibrosis. The invention further relates to cells comprising such proteins, polynucleotides encoding such proteins or fragments thereof, and to vectors comprising the polynucleotides encoding the proteins.

公开(公告)号：US12097241B2

公开(公告)日：2024-09-24

申请号：US17573238

申请日：2022-01-11

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Gene M. Dubowchik ,  Olafur S. Gudmundsson ,  Xiaojun Han ,  R. Michael Lawrence ,  Dasa Lipovsek ,  Cort S. Madsen ,  Claudio Mapelli ,  Paul E. Morin ,  Michael C. Myers

IPC: A61K38/18 ,  A61K38/22 ,  C07K1/107 ,  C07K14/64 ,  A61K38/00 ,  A61K45/06 ,  A61K47/64 ,  A61P9/00

CPC classification number: A61K38/18 ,  A61K38/2221 ,  C07K1/1077 ,  C07K14/64 ,  A61K38/00 ,  A61K45/06 ,  A61K47/64 ,  A61P9/00

Abstract: The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.

公开(公告)号：US20240309019A1

公开(公告)日：2024-09-19

申请号：US18530405

申请日：2023-12-06

Applicant: Bristol-Myers Squibb Company

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

IPC: C07D519/00 ,  A61P7/02 ,  C07D515/14

CPC classification number: C07D519/00 ,  A61P7/02 ,  C07D515/14

Abstract: 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 R1, 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：US12060341B2

公开(公告)日：2024-08-13

申请号：US17888600

申请日：2022-08-16

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Benjamin P. Vokits ,  Scott A. Shaw

IPC: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D471/04

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D471/04

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




or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

公开(公告)号：US20240261367A1

公开(公告)日：2024-08-08

申请号：US18554675

申请日：2022-04-12

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： TAO WANG

IPC: A61K38/12 ,  A61K47/54 ,  A61K47/60

CPC classification number: A61K38/12 ,  A61K47/543 ,  A61K47/545 ,  A61K47/60

Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PDL1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.

公开(公告)号：US20240218022A1

公开(公告)日：2024-07-04

申请号：US18509844

申请日：2023-11-15

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： JENNIFER X. QIAO ,  YUNHUI ZHANG ,  KENNETH M. BOY ,  MICHAEL A. POSS

IPC: C07K7/64

CPC classification number: C07K7/64

Abstract: This invention relates to novel anti-VISTA macrocyclic peptides and their related analogs with appended pharmacokinetic-enhancing tails (PKEs) with general structure of formula (I), which can be used as VISTA inhibitors.

公开(公告)号：US12012374B2

公开(公告)日：2024-06-18

申请号：US17610548

申请日：2020-05-07

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Lalgudi S. Harikrishnan ,  Muthoni G. Kamau ,  Brian E. Fink

IPC: C07D207/12 ,  C07C317/22 ,  C07D401/06 ,  C07D403/06 ,  C07D407/06 ,  C07D409/06 ,  C07D417/06

CPC classification number: C07C317/22 ,  C07D207/12 ,  C07D401/06 ,  C07D403/06 ,  C07D407/06 ,  C07D409/06 ,  C07D417/06

Abstract: The present invention is directed to compounds of the formula wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

公开(公告)号：US20240190829A1

公开(公告)日：2024-06-13

申请号：US18524426

申请日：2023-11-30

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Steven H. Spergel ,  Ryan M. Moslin ,  Michael Edward Mertzman ,  Joseph A. Tino ,  Shoshana L. Posy ,  Sirish Kaushik Lakkaraju ,  Zili Xiao ,  James Kempson

IPC: C07D249/04 ,  A61K31/501 ,  A61P25/16 ,  A61P25/28

CPC classification number: C07D249/04 ,  A61K31/501 ,  A61P25/16 ,  A61P25/28

Abstract: There are disclosed compounds of the following formula I:




or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.

公开(公告)号：US11981734B2

公开(公告)日：2024-05-14

申请号：US17668807

申请日：2022-02-10

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Natalie Bezman ,  Alan J. Korman ,  Shrikant Deshpande ,  Amy D. Jhatakia ,  Richard Y. Huang ,  Guodong Chen ,  Ginger C. Rakestraw ,  Karla Ann Henning ,  Vangipuram S. Rangan ,  Christine Bee ,  Xiang Shao

IPC: C07K16/28 ,  A61K39/395 ,  A61K47/68 ,  A61P35/00 ,  C07K1/22 ,  C12N5/071 ,  C12N15/85 ,  C12P21/00 ,  G01N33/68 ,  A61K39/00

CPC classification number: C07K16/2803 ,  A61K39/3955 ,  A61K47/6849 ,  A61P35/00 ,  C07K1/22 ,  C12N5/0682 ,  C12N15/85 ,  C12P21/005 ,  G01N33/68 ,  A61K2039/505 ,  A61K2039/507 ,  C07K2317/21 ,  C07K2317/24 ,  C07K2317/31 ,  C07K2317/33 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/76 ,  C07K2317/77 ,  C07K2317/92 ,  C07K2317/94 ,  C12N2510/02 ,  C12N2800/107

Abstract: The present disclosure provides isolated monoclonal antibodies (e.g., humanized and human monoclonal antibodies), or antigen-binding fragments thereof, that specifically bind to human natural killer cell inhibitory receptor group 2A (NKG2A) protein with high affinity and exhibit therapeutically desirable functional properties, such as for the treatment of, for example, cancer. Immunoconjugates, bispecific molecules, and pharmaceutical compositions comprising the anti-NKG2A antibodies of the invention are also provided. Nucleic acid molecules encoding the antibodies, expression vectors, host cells, and methods of treatment of, for example, cancer using the antibodies are further provided. Combination therapy, in which an anti-NKG2A antibody in the present disclosure is co-administered with at least one additional agent such as another antibody (e.g., anti-PD-1, anti-PD-L1, and/or anti-CTLA-4 antibodies), is also provided.