公开(公告)号：US11554120B2

公开(公告)日：2023-01-17

申请号：US16527802

申请日：2019-07-31

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Yam B. Poudel ,  Sanjeev Gangwar ,  Liqi He ,  Prasanna Sivaprakasam ,  Matthias Broekema ,  Matthew Cox ,  Christine M. Tarby ,  Qian Zhang ,  Naidu S. Chowdari

IPC: C07D487/04 ,  A61K31/519 ,  A61K47/60 ,  A61K39/395 ,  A61P35/00 ,  A61K31/395

Abstract: Compounds according to formula I are useful as agonists of Toll-like receptor 7 (TLR7). Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.

公开(公告)号：US11168079B2

公开(公告)日：2021-11-09

申请号：US16759660

申请日：2018-10-31

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Joseph E. Carpenter ,  Matthias Broekema ,  Jianxin Feng ,  Chunjian Liu ,  Wei Wang ,  Ying Wang

IPC: C07D401/14 ,  A61K31/4545 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D519/00

Abstract: The present invention provides compounds of Formula (I): Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of famesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

公开(公告)号：US20150133479A1

公开(公告)日：2015-05-14

申请号：US14400758

申请日：2013-05-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Matthias Broekema ,  Gang Wu ,  Dean A. Wacker

IPC: C07D401/14 ,  A61K31/403 ,  A61K31/506

CPC classification number: C07D401/14 ,  A61K31/403 ,  A61K31/506

Abstract: Novel compounds of structure Formula I: (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.

Abstract translation: 提供结构式I的新型化合物：其中R1，R2和R3在本文中定义的是GPR119G蛋白偶联受体调节剂，其中R 1，R 2和R 3在本文中定义，所述化合物是式（I）或其对映异构体，非对映异构体或其药学上可接受的盐。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。 因此，本公开还涉及包含这些新化合物的组合物以及通过使用任何这些新化合物或包含任何这些新化合物的组合物来治疗与GPR119G蛋白偶联受体的活性有关的疾病或病症的方法。

公开(公告)号：US20200283430A1

公开(公告)日：2020-09-10

申请号：US16759660

申请日：2018-10-31

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Joseph E. Carpenter ,  Matthias Broekema ,  Jianxin Feng ,  Chunjian Liu ,  Wei Wang ,  Ying Wang

IPC: C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D487/04 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention provides compounds of Formula (I): Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of famesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

公开(公告)号：US12037323B2

公开(公告)日：2024-07-16

申请号：US17052232

申请日：2019-05-02

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Christine M. Tarby ,  Derek J. Norris ,  Julian C. Lo ,  Vijay T. Ahuja ,  Steven P. Seitz ,  Ashvinikumar V. Gavai ,  John S. Tokarski ,  Mohini Rajasagi ,  Michael Wichroski ,  Matthias Broekema

IPC: C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

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

Abstract: The invention relates generally to compounds that are Mer-Ax1 inhibitors, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.

公开(公告)号：US20230339891A1

公开(公告)日：2023-10-26

申请号：US17052232

申请日：2019-05-02

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Christine M. Tarby ,  Derek J. Norris ,  Julian C. Lo ,  Vijay T. Ahuja ,  Steven P. Seitz ,  Ashvinikumar V. Gavai ,  John S. Tokarski ,  Mohini Rajasagi ,  Michael Wichroski ,  Matthias Broekema

IPC: C07D401/14 ,  C07D417/14 ,  C07D471/04 ,  C07D405/14

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

Abstract: The invention relates generally to compounds that are Mer-Ax1 inhibitors, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.

公开(公告)号：US09174965B2

公开(公告)日：2015-11-03

申请号：US14400758

申请日：2013-05-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Matthias Broekema ,  Gang Wu ,  Dean A. Wacker

IPC: C07D401/14 ,  A61K31/506 ,  A61K31/403

CPC classification number: C07D401/14 ,  A61K31/403 ,  A61K31/506

Abstract: Novel compounds of structure Formula I: (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.

Abstract translation: 提供结构式I的新型化合物：其中R1，R2和R3在本文中定义的是GPR119G蛋白偶联受体调节剂，其中R 1，R 2和R 3在本文中定义，所述化合物是式（I）或其对映异构体，非对映异构体或其药学上可接受的盐。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。 因此，本公开还涉及包含这些新化合物的组合物以及通过使用任何这些新化合物或包含任何这些新化合物的组合物来治疗与GPR119G蛋白偶联受体的活性有关的疾病或病症的方法。