公开(公告)号：US20220259205A1

公开(公告)日：2022-08-18

申请号：US17627915

申请日：2020-07-16

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Satheesh Kesavan Nair ,  Venkatram Reddy Paidi ,  Kandhasamy Sarkunam ,  Ramesh Kumar Sistla ,  John Hynes ,  Natesan Murugesan

IPC: C07D471/04 ,  C07D471/14 ,  C07D491/048

Abstract: Disclosed are compounds of Formula (I) or a salt or prodrug thereof, wherein: X1 and X2 are independently C or N, provided that zero or one of X1 and X2 is N; Ring A represented by the structure is: or; and Q, R1, R2, R3, R4, R6, and p are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.

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：US20190292191A1

公开(公告)日：2019-09-26

申请号：US16314574

申请日：2016-06-23

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： John V. Duncia ,  Daniel S. Gardner ,  John Hynes ,  John E. Macor ,  Natesan Murugesan ,  Joseph B. Santella ,  Hong Wu ,  Durgarao Kantheti ,  Satheesh Kesavan Nair ,  Venkatram Reddy Paidi ,  Sreekantha Ratna Kumar ,  Kandhasamy Sarkunam ,  Ramesh Kumar Sistla ,  Subba Rao Polimera

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

Abstract: Disclosed are compounds of Formula (I) Formula (I) or salts thereof, wherein HET is a heteroaryl selected from oxazolyl, pyrazolyl, imidazo[1,2-b]pyridazin-3-yl, and pyrazolo[1,5-a]pyrimidin-3-yl, wherein said heteroaryl is attached to the pyridinyl group in the compound of Formula (I) by a carbon ring atom in the heteroaryl and wherein said heteroaryl is substituted with zero to 2 Rb; and R1, R3, and Rb are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.

公开(公告)号：US10167254B2

公开(公告)日：2019-01-01

申请号：US15584818

申请日：2017-05-02

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： James Aaron Balog ,  Emily Charlotte Cherney ,  Weiwei Guo ,  Audris Huang ,  Jay A. Markwalder ,  Steven P. Seitz ,  Weifang Shan ,  David K. Williams ,  Natesan Murugesan ,  Susheel Jethanand Nara ,  Saumya Roy ,  Soodamani Thangavel ,  Ramesh Kumar Sistla ,  Srinivas Cheruku ,  Srinivasan Thangathirupathy ,  Yadagiri Kanyaboina ,  Nagalakshmi Pulicharla

IPC: A61K31/17 ,  C07C275/40 ,  A61K31/196 ,  A61K31/277 ,  A61K31/351 ,  A61K31/382 ,  A61K31/397 ,  A61K31/428 ,  A61K31/437 ,  A61K31/445 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/538 ,  A61K39/395 ,  C07C229/42 ,  C07C255/58 ,  C07D205/04 ,  C07D211/14 ,  C07D239/47 ,  C07D265/36 ,  C07D277/64 ,  C07D295/155 ,  C07D309/04 ,  C07D335/02 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D309/14 ,  C07D407/12 ,  C07D487/08 ,  C07D265/30 ,  C07D207/08 ,  C07D211/08 ,  C07D307/22 ,  C07C255/57 ,  C07C235/38 ,  C07C235/56 ,  C07C233/81 ,  C07C275/42 ,  C07D207/12 ,  C07D239/34 ,  C07D317/46 ,  C07D413/14 ,  C07D471/08 ,  C07C275/30 ,  A61K45/06

Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

公开(公告)号：US20220144818A1

公开(公告)日：2022-05-12

申请号：US17601942

申请日：2020-04-08

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Chunjian Liu ,  Jianxin Feng ,  Pratik Devasthale ,  Natesan Murugesan ,  Bruce A. Ellsworth ,  Alicia Regueiro-Ren ,  Susheel Jethanand Nara ,  Prasada Rao Jalagam ,  Manoranjan Panda

IPC: C07D417/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14

Abstract: The present disclosure relates to compounds of Formula (I) or (II), which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions.

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：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：US10562887B2

公开(公告)日：2020-02-18

申请号：US16098978

申请日：2017-05-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Natesan Murugesan ,  Peter W. Glunz ,  Mandar Shrikrishna Bodas ,  Navnath Dnyanoba Yadav ,  Venu Alla

IPC: C07D403/10 ,  C07D401/10 ,  C07D403/14 ,  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：US20190152956A1

公开(公告)日：2019-05-23

申请号：US16098978

申请日：2017-05-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Natesan Murugesan ,  Peter W. Glunz ,  Mandar Shrikrishna Bodas ,  Navnath Dnyanoba Yadav ,  Venu Alla

IPC: C07D403/10 ,  C07D403/14 ,  C07D401/10 ,  C07D487/04 ,  C07D471/04

CPC classification number: C07D403/10 ,  C07D401/10 ,  C07D403/14 ,  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.