公开(公告)号：US10654860B2

公开(公告)日：2020-05-19

申请号：US16461029

申请日：2017-11-29

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Wu Yang ,  Peter W. Glunz ,  Rajeev S. Bhide ,  Kamalraj Thiyagarajan

IPC: C07D487/10 ,  C07D403/10 ,  C07D471/04 ,  C07D491/052 ,  C07D491/147 ,  C07D231/54 ,  C07D487/04 ,  C07D403/04 ,  A61K31/436

Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

公开(公告)号：US20190276466A1

公开(公告)日：2019-09-12

申请号：US16461029

申请日：2017-11-29

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Wu Yang ,  Peter W. Glunz ,  Rajeev S. Bhide ,  Kamalraj Thiyagarajan

IPC: C07D487/10 ,  C07D403/10 ,  C07D491/147 ,  C07D471/04 ,  C07D491/052

Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

公开(公告)号：US10123993B2

公开(公告)日：2018-11-13

申请号：US15541725

申请日：2016-01-08

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Peter W. Glunz ,  Doree F. Sitkoff ,  Navnath Dnyanoba Yadav ,  Mandar Shrikrishna Bodas ,  Rajeev S. Bhide ,  Sharanabasappa Patil ,  Kumaresan Chinnakotti ,  Prasanna Savanor Maddu Rao ,  Jeevan Prakash Shetty

IPC: A61K31/4178 ,  A61K31/422 ,  A61K31/498 ,  C07D401/14 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

公开(公告)号：US20150284382A1

公开(公告)日：2015-10-08

申请号：US14441705

申请日：2013-11-07

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Rajeev S. Bhide ,  John V. Duncia ,  John Hynes ,  Satheesh K. Nair ,  William J. Pitts ,  Sreekantha R. Kumar ,  Daniel S. Gardner ,  Natesan Murugesan ,  Venkatram Reddy Paidi ,  Joseph B. Santella ,  Ramesh Sistla ,  Hong Wu

IPC: C07D417/14 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D213/74 ,  C07D401/12

CPC classification number: C07D407/14 ,  C07D213/74 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/14

Abstract: Compounds having the following formula (I) or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R2 is a monocyclic heteroaryl group, and R1, R3, R4, R5 and R6 are as defined herein, are useful as kinase modulators, including IRAK-4 inhibition.

Abstract translation: 具有下式（I）的化合物或其立体异构体或其药学上可接受的盐，其中R 2是单环杂芳基，且R 1，R 3，R 4，R 5和R 6如本文所定义，可用作激酶调节剂，包括IRAK -4抑制。

公开(公告)号：US20240327390A1

公开(公告)日：2024-10-03

申请号：US18659052

申请日：2024-05-09

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Navnath Dnyanoba Yadav ,  Rajeev S. Bhide ,  Rajesh Onkardas Bora ,  Prashantha Gunaga ,  Manoranjan Panda ,  Eldon Scott Priestley ,  Jeremy Richter

IPC: C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

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

Abstract: Disclosed are compounds of Formula (I)




or a salt thereof,

wherein R1 is:





each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3a, R3b, L1, B, V, Y, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.

公开(公告)号：US10544133B2

公开(公告)日：2020-01-28

申请号：US16009389

申请日：2018-06-15

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Rajeev S. Bhide ,  John V. Duncia ,  John Hynes ,  Satheesh Kesavan Nair ,  William J. Pitts ,  Sreekantha Ratna Kumar ,  Daniel S. Gardner ,  Natesan Murugesan ,  Venkatram Reddy Paidi ,  Joseph B. Santella ,  Ramesh Kumar Sistla ,  Hong Wu

IPC: C07D407/14 ,  C07D401/14 ,  C07D401/12 ,  C07D417/14 ,  C07D213/74 ,  C07D405/12 ,  C07D405/14

Abstract: Compounds having the following formula: or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R2 is a monocyclic heteroaryl group, and R1, R3, R4, R5 and R6 are as defined herein, are useful as kinase modulators, including IRAK-4 inhibition.

公开(公告)号：US20190248769A1

公开(公告)日：2019-08-15

申请号：US16344823

申请日：2017-11-02

Applicant: Bristol-Myers Squibb Company

Inventor： Prashantha Gunaga ,  Rajeev S. Bhide ,  Rajesh Onkardas Bora ,  Manoranjan Panda ,  Navnath Dnyanoba Yadav ,  Eldon Scott Priestley ,  Jeremy Richter

IPC: C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  A61P9/12 ,  A61P9/04 ,  A61P13/02 ,  C07D471/04

Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein R1 is (II) or (III); each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3, L1, L2, R1a, R1b, R1c, and n are define herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.

公开(公告)号：US20180346453A1

公开(公告)日：2018-12-06

申请号：US15993683

申请日：2018-05-31

Applicant: Bristol-Myers Squibb Company

Inventor： Navnath Dnyanoba Yadav ,  Rajeev S. Bhide ,  Rajesh Onkardas Bora ,  Prashantha Gunaga ,  Manoranjan Panda ,  Eldon Scott Priestley ,  Jeremy Richter

IPC: C07D405/14 ,  C07D417/14 ,  C07D413/14

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

Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein R1 is: each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3a, R3b, L1, B, V, Y, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.

公开(公告)号：US10023576B2

公开(公告)日：2018-07-17

申请号：US15521199

申请日：2015-10-21

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Rajeev S. Bhide ,  Zheming Ruan ,  Robert J. Cherney ,  Lyndon A. M. Cornelius ,  T. G. Murali Dhar ,  Hua Gong ,  David Marcoux ,  Michael A. Poss ,  Lan-ying Qin ,  Qing Shi ,  Joseph A. Tino

IPC: C07D487/04

Abstract: Disclosed are compounds of Formula (I); or a salt thereof; wherein Qi is (i) Cl, Br, I, —CN, —CH3, or —CF3; or (ii) pyrazole, triazole, or pyridinyl, each substituted with R1; Q2 is pyridinyl, indazolyl, isoquinolinyl, or benzo[d]imidazolyl substituted with R2 and R3; and R1, R2, and R3 are defined herein. Also disclosed are methods of using such compounds as modulators of PI3K, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases.

公开(公告)号：US20200339550A1

公开(公告)日：2020-10-29

申请号：US16928079

申请日：2020-07-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Navnath Dnyanoba Yadav ,  Rajeev S. Bhide ,  Rajesh Onkardas Bora ,  Prashantha Gunaga ,  Manoranjan Panda ,  Eldon Scott Priestley ,  Jeremy Richter

IPC: C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein R1 is: each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3a, R3b, L1, B, V, Y, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.