公开(公告)号：US09657009B2

公开(公告)日：2017-05-23

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

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.

公开(公告)号：US09540333B2

公开(公告)日：2017-01-10

申请号：US14441213

申请日：2013-11-07

Applicant: Bristol-Myers Squibb Company

Inventor： Joseph B. Santella ,  Ryan M. Moslin ,  David S. Weinstein ,  Stephen T. Wrobleski ,  John S. Tokarski

IPC: C07D239/48 ,  C07D239/95

CPC classification number: C07D239/48 ,  C07D239/95

Abstract: Compounds having the following formula (I): or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 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.

Abstract translation: 具有下式（I）的化合物或其立体异构体或药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5如本文所定义，可用于调节IL-12，IL-23和/ 或通过作用于Tyk-2引起信号转导抑制的IFNα。

公开(公告)号：US09169252B2

公开(公告)日：2015-10-27

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: C07D213/02 ,  C07D519/00 ,  C07D401/14 ,  C07D471/04 ,  C07D401/04 ,  C07D487/04 ,  C07F9/6561

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。

公开(公告)号：US20150274696A1

公开(公告)日：2015-10-01

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

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：US20130178444A1

公开(公告)日：2013-07-11

申请号：US13785039

申请日：2013-03-05

Applicant: Bristol-Myers Squibb Company

Inventor： John Hynes ,  Percy H. Carter ,  Lyndon A.M. Cornelius ,  T.G. Murali Dhar ,  John V. Duncia ,  Satheesh K. Nair ,  Joseph B. Santella ,  Jayakumar S. Warrier ,  Hong Wu

IPC: C07D211/60 ,  C07F9/59

CPC classification number: C07D211/60 ,  C07D211/52 ,  C07F9/59

Abstract: The present application describes prodrugs of the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis using the prodrug compounds of the invention are disclosed.

Abstract translation: 本申请描述了式（I）化合物的前药或其立体异构体或其药学上可接受的盐。 此外，公开了使用本发明的前药化合物治疗和预防炎症性疾病如哮喘和过敏性疾病以及自身免疫性病症如类风湿性关节炎的方法。