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：US20190127358A1

公开(公告)日：2019-05-02

申请号：US16175895

申请日：2018-10-31

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： David S. Yoon ,  Rushith Kumar Anumula ,  Srinivas Cheruku ,  Yanting Huang ,  Elizabeth Anne Jurica ,  Wei Meng ,  Susheel Jethanand Nara ,  Rishikesh Narayan ,  Ramesh Kumar Sistla ,  Ximao Wu ,  Guohua Zhao

IPC: C07D413/14 ,  C07D413/04 ,  A61P35/00 ,  A61P29/00 ,  A61P13/12 ,  A61P1/16 ,  A61P1/18

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 modulate the activity of farnesoid 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：US10202390B2

公开(公告)日：2019-02-12

申请号：US15738435

申请日：2016-06-23

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: C07D487/04

Abstract: Disclosed are compounds of Formula (I) or salts thereof, wherein: HET is a heteroaryl selected from imidazo[1,2-b]pyridazinyl and pyrazolo[1,5-a]pyrimidinyl, 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; A is pyrazolyl, imidazolyl, or triazolyl, each substituted with zero or 1 Ra; and R3, Ra, 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：US20180346440A1

公开(公告)日：2018-12-06

申请号：US15763280

申请日：2016-09-29

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Joanne J. Bronson ,  Ling Chen ,  Jonathan L. Ditta ,  Carolyn Diane Dzierba ,  Prasada Rao Jalagam ,  Guanglin Luo ,  John E. Macor ,  Tarun Kumar Maishal ,  Susheel Jethanand Nara ,  Ramkumar Rajamani ,  Ramesh Kumar Sistla ,  Soodamani Thangavel

IPC: C07D401/04 ,  C07D413/14 ,  A61P25/16 ,  A61P25/28 ,  A61P25/18 ,  A61P25/02

Abstract: The present disclosure is directed to biaryl compounds of formula (I) which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds and their use for treating e.g. pain, Alzheimer's disease, Parkinson's disease and schizophrenia.

公开(公告)号：US20160122358A1

公开(公告)日：2016-05-05

申请号：US14994346

申请日：2016-01-13

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Upender Velaparthi ,  Chetan Padmakar Darne ,  Peiying Liu ,  Mark D. Wittman ,  Bradley C. Pearce ,  Erika M. V. Araujo ,  Bireshwar Dasgupta ,  Jalathi Surendran Nair ,  Sakthi Kumaran Janakiraman ,  Chandrasekhar Reddy Rachamreddy ,  Mallikarjuna Rao Mettu ,  Arul Mozhi Subbiah Karuppiah ,  Subba Reddy Bandreddy ,  Nagalakshmi Pulicharla ,  Rajesh Onkardas Bora ,  Shilpa Maheshwarappa Holehatti ,  Selvakumar Kumaravel ,  Dibakar Mullick ,  Ramesh Kumar Sistla

IPC: C07D487/04 ,  C07D487/20 ,  C07D491/20 ,  C07D487/10 ,  C07D491/147

CPC classification number: C07D487/04 ,  C07D487/10 ,  C07D487/20 ,  C07D491/147 ,  C07D491/20 ,  C07D519/00

Abstract: The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.