公开(公告)号：US10968219B2

公开(公告)日：2021-04-06

申请号：US16347844

申请日：2017-11-07

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： 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: C07D471/04 ,  C07D491/04 ,  C07D519/00 ,  A61P11/00 ,  A61P19/10 ,  A61P35/00 ,  A61P37/06

Abstract: 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 ay-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：USRE49735E1

公开(公告)日：2023-11-28

申请号：US17481947

申请日：2021-09-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Andrew P. Degnan ,  Hong Huang ,  Lawrence B. Snyder ,  Fukang Yang ,  Kevin W. Gillman ,  Michael Frederick Parker

IPC: C07D413/04 ,  C07D263/18 ,  C07D413/10 ,  C07D413/14

CPC classification number: C07D413/04 ,  C07D263/18 ,  C07D413/10 ,  C07D413/14

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.

公开(公告)号：US11884661B2

公开(公告)日：2024-01-30

申请号：US17184179

申请日：2021-02-24

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： 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: C07D471/04 ,  C07D491/04 ,  C07D519/00 ,  A61P11/00 ,  A61P19/10 ,  A61P35/00 ,  A61P37/06

CPC classification number: C07D471/04 ,  A61P11/00 ,  A61P19/10 ,  A61P35/00 ,  A61P37/06 ,  C07D491/04 ,  C07D519/00

Abstract: 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：US20210188847A1

公开(公告)日：2021-06-24

申请号：US17184179

申请日：2021-02-24

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： 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: C07D471/04 ,  A61P37/06 ,  A61P11/00 ,  A61P19/10 ,  A61P35/00 ,  C07D519/00 ,  C07D491/04

Abstract: 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.