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：US09809573B2

公开(公告)日：2017-11-07

申请号：US15033770

申请日：2014-11-03

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Guanglin Luo ,  Ling Chen ,  Gene M. Dubowchik ,  Swanee E. Jacutin-Porte ,  Prasanna Sivaprakasam ,  John E. Macor

IPC: C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/08 ,  C07D513/04 ,  C07D213/81 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04

CPC classification number: C07D401/12 ,  C07D213/81 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D487/08 ,  C07D513/04

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, antagonists of the NR2B 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：US20230322695A1

公开(公告)日：2023-10-12

申请号：US18161184

申请日：2023-01-30

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Haibo Liu ,  Laura Akullian D′Agostino ,  Shoshana L. Posy ,  Annapurna Pendri ,  Swanee E. Jacutin-Porte

IPC: C07D285/06 ,  A61K45/06 ,  A61P35/00 ,  C07D417/12 ,  C07D417/10

CPC classification number: C07D285/06 ,  A61K45/06 ,  A61P35/00 ,  C07D417/10 ,  C07D417/12

Abstract: Disclosed are compounds of Formula (I)





pharmaceutically acceptable salts thereof are defined herein, and pharmaceutical compositions thereof and combinations thereof, and methods of using the same as inhibitors of protein tyrosine phosphatases (PTPN2). These compounds are useful in treating cancer and diseases susceptible to PNPT2 inhibition.

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：US10752609B2

公开(公告)日：2020-08-25

申请号：US16463467

申请日：2017-11-27

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Richard A. Hartz ,  Vijay T. Ahuja ,  Guanglin Luo ,  Ling Chen ,  Prasanna Sivaprakasam ,  Gene M. Dubowchik ,  Swanee E. Jacutin-Porte ,  John E. Macor

IPC: C07D401/12 ,  A61P25/28 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D417/14

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.

公开(公告)号：US12162848B2

公开(公告)日：2024-12-10

申请号：US18161184

申请日：2023-01-30

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Haibo Liu ,  Laura Akullian D'Agostino ,  Shoshana L. Posy ,  Annapurna Pendri ,  Swanee E. Jacutin-Porte

IPC: C07D285/06 ,  A61K45/06 ,  A61P35/00 ,  C07D417/10 ,  C07D417/12

Abstract: Disclosed are compounds of Formula (I) pharmaceutically acceptable salts thereof are defined herein, and pharmaceutical compositions thereof and combinations thereof, and methods of using the same as inhibitors of protein tyrosine phosphatases (PTPN2). These compounds are useful in treating cancer and diseases susceptible to PNPT2 inhibition.

公开(公告)号：US09718804B2

公开(公告)日：2017-08-01

申请号：US15033813

申请日：2014-11-03

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Guanglin Luo ,  Ling Chen ,  Gene M. Dubowchik ,  Swanee E. Jacutin-Porte ,  Vivekananda M. Vrudhula ,  Senliang Pan ,  Prasanna Sivaprakasam ,  John E. Macor

IPC: C07D213/02 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D471/04

CPC classification number: C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.

公开(公告)号：US20160289210A1

公开(公告)日：2016-10-06

申请号：US15033770

申请日：2014-11-03

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Guanglin Luo ,  Ling Chen ,  Gene M. Dubowchik ,  Swanee E. Jacutin-Porte ,  Prasanna Sivaprakasam ,  John E. Macor

IPC: C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D513/04 ,  C07D487/08 ,  C07D417/12 ,  C07D417/14 ,  C07D409/14 ,  C07D413/14

CPC classification number: C07D401/12 ,  C07D213/81 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D487/08 ,  C07D513/04

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, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.

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。 这些化合物是NR2B受体的配体，拮抗剂，可用于治疗中枢神经系统的各种疾病。

公开(公告)号：US20160272621A1

公开(公告)日：2016-09-22

申请号：US15033813

申请日：2014-11-03

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Guanglin Luo ,  Ling Chen ,  Gene M. Dubowchik ,  Swanee E. Jacutin-Porte ,  Vivekananda M. Vrudhula ,  Senliang Pan ,  Prasanna Sivaprakasam ,  John E. Macor

IPC: C07D401/14 ,  C07D487/04 ,  C07D471/04 ,  C07D413/14 ,  C07D405/14

CPC classification number: C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.