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：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.

公开(公告)号：US09682980B2

公开(公告)日：2017-06-20

申请号：US14406029

申请日：2013-06-19

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ronald J. Mattson ,  Zhaoxing Meng ,  Leatte R. Guernon

IPC: C07D491/107 ,  C07D487/04

CPC classification number: C07D487/04 ,  C07D491/107

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 modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system. Formula (I):

公开(公告)号：US20150152113A1

公开(公告)日：2015-06-04

申请号：US14406029

申请日：2013-06-19

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Ronald J. Mattson ,  Zhaoxing Meng ,  Leatte R. Guernon

IPC: C07D487/04 ,  C07D491/107

CPC classification number: C07D487/04 ,  C07D491/107

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 modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system. Formula (I):

Abstract translation: 本公开内容通常涉及式I化合物，包括其盐，以及使用该化合物的组合物和方法。 该化合物调节mGluR2受体并且可用于治疗中枢神经系统的各种疾病。 式（I）：