公开(公告)号：US10023562B2

公开(公告)日：2018-07-17

申请号：US15480682

申请日：2017-04-06

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

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：US20180000788A1

公开(公告)日：2018-01-04

申请号：US15541725

申请日：2016-01-08

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

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

CPC classification number: A61K31/4178 ,  A61K31/422 ,  A61K31/498 ,  C07D401/10 ,  C07D401/14 ,  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：US20170210730A1

公开(公告)日：2017-07-27

申请号：US15480682

申请日：2017-04-06

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: C07D407/14 ,  C07D213/74 ,  C07D417/14 ,  C07D405/14 ,  C07D401/14 ,  C07D405/12 ,  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: 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：US09546153B2

公开(公告)日：2017-01-17

申请号：US14441698

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: C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D513/04 ,  C07D417/14 ,  C07D471/04

CPC classification number: C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

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

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是双环杂环，并且R 1，R 3，R 4，R 5和R 6如本文所定义，其可用作激酶调节剂，包括IRAK -4调制。

公开(公告)号：US08987311B2

公开(公告)日：2015-03-24

申请号：US14371281

申请日：2013-01-11

Applicant: Bristol-Myers Squibb Company

Inventor： Dharmpal S. Dodd ,  Christopher P. Mussari ,  Rajeev S. Bhide ,  Satheesh Kesavan Nair ,  Venkatram Reddy Paidi ,  Sreekantha Ratna Kumar ,  Abhisek Banerjee ,  Ramesh Sistla ,  William J. Pitts ,  John Hynes

IPC: C07D401/04 ,  A61K31/44 ,  C07D471/10 ,  C07D417/14

CPC classification number: C07D471/10 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

Abstract: Compounds having the following formula: (I) wherein: A is an optionally substituted triazole, or a stereoisomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.

Abstract translation: 具有下式的化合物：（I）其中：A是任选取代的三唑或其立体异构体或其药学上可接受的盐，可用作激酶调节剂，包括IRAK-4调节。

公开(公告)号：US20230124468A1

公开(公告)日：2023-04-20

申请号：US17960199

申请日：2022-10-05

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.

公开(公告)号：US10723723B2

公开(公告)日：2020-07-28

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 ,  A61P13/02 ,  A61P9/00 ,  A61P9/12 ,  A61P9/04 ,  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：US10214537B2

公开(公告)日：2019-02-26

申请号：US15521202

申请日：2015-10-21

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Rajeev S. Bhide ,  Douglas G. Batt ,  Robert J. Cherney ,  Lyndon A. M. Cornelius ,  Qingjie Liu ,  David Marcoux ,  James Neels ,  Michael A. Poss ,  Zheming Ruan ,  Qing Shi ,  Anurag S. Srivastava ,  Lan-ying Qin ,  Joseph A. Tino ,  Scott Hunter Watterson

IPC: C07D487/04 ,  C07D491/08 ,  A61K31/53 ,  A61K31/541 ,  A61P29/00

Abstract: Disclosed are compounds of Formula (I) or a salt thereof; wherein: X is N or CH; Q1 is: (i) Cl, Br, I, —CN, —CH3, or —CF3; (ii) a 5-membered heteroaryl selected from pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, oxadiazolyl, and thiadiazolyl; (iii) a 6?membered heteroaryl selected from pyridinyl, pyridazinyl, and pyrimidinyl; or (iv) a bicyclic heteroaryl selected from indolyl, pyrrolopyridinyl, pyrazolopyridinyl and benzo[d]oxazolyl; wherein each of said 5-membered, 6-membered, and bicyclic heteroaryl is substituted with zero to 1 Ra and zero to 1 Rb; and R1, R2, R3, R4, R5, R6, Ra, and Rb 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：US20170355707A1

公开(公告)日：2017-12-14

申请号：US15521202

申请日：2015-10-21

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Rajeev S. Bhide ,  Douglas G. Batt ,  Robert J Cherney ,  Lyndon A.M. Cornelius ,  Qingjie Liu ,  David Marcoux ,  James Neels ,  Michael A. Poss ,  Zheming Ruan ,  Qing Shi ,  Anurag S. Srivastava ,  Lan-ying Qin ,  Joseph A. Tino ,  Scott Hunter Watterson

IPC: C07D491/08 ,  C07D487/04

CPC classification number: C07D491/08 ,  C07D487/04

Abstract: Disclosed are compounds of Formula (I) or a salt thereof; wherein: X is N or CH; Q1 is: (i) Cl, Br, I, —CN, —CH3, or —CF3; (ii) a 5-membered heteroaryl selected from pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, oxadiazolyl, and thiadiazolyl; (iii) a 6?membered heteroaryl selected from pyridinyl, pyridazinyl, and pyrimidinyl; or (iv) a bicyclic heteroaryl selected from indolyl, pyrrolopyridinyl, pyrazolopyridinyl and benzo[d]oxazolyl; wherein each of said 5-membered, 6-membered, and bicyclic heteroaryl is substituted with zero to 1 Ra and zero to 1 Rb; and R1, R2, R3, R4, R5, R6, Ra, and Rb 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：USRE49700E1

公开(公告)日：2023-10-17

申请号：US17183286

申请日：2021-02-23

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.