公开(公告)号：US10301260B2

公开(公告)日：2019-05-28

申请号：US15308459

申请日：2015-05-06

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Xiang-Yang Ye ,  Bruce A. Ellsworth ,  Elizabeth A. Jurica

IPC: C07D207/08 ,  C07D401/04 ,  C07D413/04 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  A61K45/06 ,  A61K31/40 ,  A61K31/422 ,  A61K31/4439

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.

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：US20160280680A1

公开(公告)日：2016-09-29

申请号：US14442642

申请日：2013-11-15

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Bruce A. Ellsworth ,  Elizabeth A. Jurica ,  Jun Shi ,  William R. Ewing ,  Xiang-Yang Ye ,  Ximao Wu ,  Zhu Yeheng ,  Sun Chongqing

IPC: C07D401/12 ,  C07D207/08 ,  A61K31/4025 ,  C07D207/12 ,  A61K45/06 ,  C07D401/14 ,  A61K31/4545 ,  A61K31/506 ,  C07D487/04 ,  A61K31/5025 ,  A61K31/454 ,  C07D401/10

CPC classification number: C07D401/12 ,  A61K31/4025 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/5025 ,  A61K31/506 ,  A61K45/06 ,  C07D207/08 ,  C07D207/12 ,  C07D401/10 ,  C07D401/14 ,  C07D487/04

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.

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：US11028071B2

公开(公告)日：2021-06-08

申请号：US16924346

申请日：2020-07-09

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Xiang-Yang Ye ,  Christian L. Morales ,  Mendi A. Higgins ,  Eric Mull

IPC: C07D401/14 ,  A61P35/00 ,  C07D471/04 ,  C07D498/04

Abstract: The present invention provides compounds of Formula (Ia) or (Ib): 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：US20190256496A1

公开(公告)日：2019-08-22

申请号：US16347831

申请日：2017-11-07

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Xiang-Yang Ye ,  Christian L. Morales ,  Mendi Higgins ,  Eric Mull

IPC: C07D401/14 ,  C07D471/04 ,  C07D498/04 ,  A61P35/00

Abstract: The present invention provides compounds of Formula (Ia) or (Ib): 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：US20200339540A1

公开(公告)日：2020-10-29

申请号：US16924346

申请日：2020-07-09

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Xiang-Yang Ye ,  Christian L. Morales ,  Mendi A. Higgins ,  Eric Mull

IPC: C07D401/14 ,  A61P35/00 ,  C07D471/04 ,  C07D498/04

Abstract: The present invention provides compounds of Formula (Ia) or (Ib): 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：US10745384B2

公开(公告)日：2020-08-18

申请号：US16347831

申请日：2017-11-07

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Xiang-Yang Ye ,  Christian L. Morales ,  Mendi A. Higgins ,  Eric Mull

IPC: C07D401/14 ,  A61P35/00 ,  C07D471/04 ,  C07D498/04 ,  A61K31/404

Abstract: The present invention provides compounds of Formula (Ia) or (Ib): 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：US09714231B2

公开(公告)日：2017-07-25

申请号：US14442642

申请日：2013-11-15

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Bruce A. Ellsworth ,  Elizabeth A. Jurica ,  Jun Shi ,  William R. Ewing ,  Xiang-Yang Ye ,  Ximao Wu ,  Zhu Yeheng ,  Sun Chongqing

IPC: A61K31/4025 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/5025 ,  A61K31/506 ,  C07D401/12 ,  C07D401/14 ,  C07D487/04 ,  A61K45/06 ,  C07D207/08 ,  C07D207/12 ,  C07D401/10

CPC classification number: C07D401/12 ,  A61K31/4025 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/5025 ,  A61K31/506 ,  A61K45/06 ,  C07D207/08 ,  C07D207/12 ,  C07D401/10 ,  C07D401/14 ,  C07D487/04

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.