公开(公告)号：US20230167131A1

公开(公告)日：2023-06-01

申请号：US17799028

申请日：2021-02-11

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Kumaravel Selvakumar ,  Venkatram Paidi ,  Srinivasan Thangathirupathy ,  Vijaya Kumar Cm ,  Tirupathi Rao Alajangi ,  Mallikarjun Reddy Sura ,  Krishna Mahadevu ,  Ramesh Kumar Sistla ,  Piyush Agarwal ,  Arul Mozhi Subbiah Karuppiah ,  Jalathi S. Nair ,  Ooha Morampudi ,  Manoranjan Panda ,  Joseph A. Tino ,  Robert J. Cherney ,  John V. Duncia ,  Daniel S. Gardner ,  T. G. Murali Dhar ,  Audrey Graham Ross ,  Paul E. Gormisky ,  Xiao Zhu ,  Boris M. Seletsky ,  Alyssa H. Antropow ,  Deqiang Niu ,  Zhengdong Zhu ,  Guobin Miao ,  Julio Herman Cuervo

IPC: C07D519/00 ,  C07D471/04 ,  C07D487/04 ,  C07D409/14 ,  C07D405/14 ,  C07D413/14

CPC classification number: C07D519/00 ,  C07D471/04 ,  C07D487/04 ,  C07D409/14 ,  C07D405/14 ,  C07D413/14

Abstract: The disclosure generally relates to substituted heterocyclic compounds of Formula (Ia), which are inhibitors of PAD4, method for preparing these compounds, pharmaceutical compositions comprising these compounds and use of these compounds in the treatment of a disease or a disorder associated with PAD4 enzyme activity.

公开(公告)号：US10294256B2

公开(公告)日：2019-05-21

申请号：US15838434

申请日：2017-12-12

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Michael G. Yang ,  Zili Xiao ,  John V. Duncia ,  David S. Weinstein

IPC: C07D401/00 ,  C07F9/6558 ,  A61P29/00 ,  A61P37/00 ,  C07F9/6509 ,  A61K31/50 ,  A61K31/501 ,  C07D401/12 ,  C07D237/24

Abstract: Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where all substituents are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.

公开(公告)号：US20180370956A1

公开(公告)日：2018-12-27

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 K. 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 ,  C07D405/14 ,  C07D405/12 ,  C07D213/74 ,  C07D401/14 ,  C07D417/14 ,  C07D401/12

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：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：US20150191464A1

公开(公告)日：2015-07-09

申请号：US14588470

申请日：2015-01-02

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Joseph B. Santella ,  Sreekantha Ratna Kumar ,  John V. Duncia ,  Daniel S. Gardner ,  Venkatram Reddy Paidi ,  Satheesh Kesavan Nair ,  John Hynes ,  Hong Wu ,  Natesan Murugesan ,  Kandhasamy Sarkunam ,  Piramanayagam Arunachalam

IPC: C07D471/04 ,  C07D519/00 ,  C07D401/14 ,  C07F9/6561 ,  C07D401/04 ,  C07D487/04

CPC classification number: C07D471/04 ,  C07D401/04 ,  C07D401/14 ,  C07D487/04 ,  C07D519/00 ,  C07F9/65616

Abstract: Disclosed are compounds of Formula (I) or salts thereof, wherein: HET is a heteroaryl selected from pyrazolyl, indolyl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-d]pyrimidinyl, pyrazolo[3,4-b]pyridinyl, pyrazolo[3,4-d]pyrimidinyl, 2,3-dihydro-1H-pyrrolo[2,3-b]pyridinyl, imidazo[4,5-b]pyridinyl, and purinyl, wherein said heteroaryl is substituted with Ra and Rb; and R1 and R2 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.

Abstract translation: 公开了式（I）的化合物或其盐，其中：HET是选自吡唑基，吲哚基，吡咯并[2,3-b]吡啶基，吡咯并[2,3-d]嘧啶基，吡唑并[3,4- b]吡啶基，吡唑并[3,4-d]嘧啶基，2,3-二氢-1H-吡咯并[2,3-b]吡啶基，咪唑并[4,5-b]吡啶基和嘌呤基，其中所述杂芳基被取代 与Ra和Rb; 并且R1和R2在本文中定义。 还公开了使用这样的化合物作为IRAK4的调节剂的方法和包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓炎症和自身免疫性疾病。