公开(公告)号：US10781215B2

公开(公告)日：2020-09-22

申请号：US16344459

申请日：2017-10-27

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Stephen T. Wrobleski ,  David S. Weinstein ,  Michael G. Yang

IPC分类号： C07D487/04 ,  C07D471/04 ,  C07D473/34

摘要： 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：US10294256B2

公开(公告)日：2019-05-21

申请号：US15838434

申请日：2017-12-12

申请人： BRISTOL-MYERS SQUIBB COMPANY

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

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

摘要： 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：US20160304524A1

公开(公告)日：2016-10-20

申请号：US15102991

申请日：2014-12-10

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Chunjian Liu ,  James Lin ,  Ryan M. Moslin ,  David S. Weinstein ,  John S. Tokarski

IPC分类号： C07D487/04 ,  C07D498/14

CPC分类号： C07D487/04 ,  C07D487/14 ,  C07D498/14

摘要： 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.

公开(公告)号：US20220356180A1

公开(公告)日：2022-11-10

申请号：US17244938

申请日：2021-04-29

申请人： Bristol-Myers Squibb Company

发明人： Ryan M. Moslin ,  David S. Weinstein ,  Stephen T. Wrobleski ,  John S. Tokarski ,  Amit Kumar ,  Douglas G. Batt ,  Shuqun Lin ,  Chunjian Liu ,  Steven H. Spergel ,  Yanlei Zhang ,  Qingjie Liu

IPC分类号： C07D417/14 ,  C07D403/12 ,  C07D401/14 ,  C07D413/14 ,  C07D401/12 ,  C07D237/24 ,  C07D403/14 ,  C07D413/12 ,  C07D417/12 ,  C07B59/00

摘要： 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.

公开(公告)号：US20180325899A1

公开(公告)日：2018-11-15

申请号：US15776094

申请日：2016-11-17

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： David S. Weinstein ,  Ryan M. Moslin ,  Yanlei Zhang ,  Daniel S. Gardner ,  Joseph B. Santella ,  Charles M. Langevine ,  Sylwia Stachura

IPC分类号： A61K31/5025 ,  A61K31/53 ,  A61K31/5377 ,  A61P29/00 ,  A61P37/02

CPC分类号： A61K31/5025 ,  A61K31/53 ,  A61K31/5377 ,  A61P29/00 ,  A61P37/02 ,  C07D487/04

摘要： Compounds of formula I or a stereoisomer or pharmaceutically-acceptable salt thereof, 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：US20180162889A1

公开(公告)日：2018-06-14

申请号：US15838434

申请日：2017-12-12

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Michael G. YANG ,  Zili Xiao ,  John V. Duncia ,  David S. Weinstein

IPC分类号： C07F9/6558 ,  C07F9/6509 ,  A61P37/00 ,  A61P29/00

CPC分类号： C07F9/65583 ,  A61K31/50 ,  A61K31/501 ,  A61P29/00 ,  A61P37/00 ,  C07D237/24 ,  C07D401/12 ,  C07F9/650905

摘要： 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：US09725443B2

公开(公告)日：2017-08-08

申请号：US15022673

申请日：2014-09-18

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： T. G. Murali Dhar ,  Jingwu Duan ,  Hua Gong ,  Bin Jiang ,  Zhonghui Lu ,  David S. Weinstein

IPC分类号： A61K31/47 ,  C07D417/06 ,  C07D401/06 ,  C07D401/12 ,  C07D413/14 ,  C07D215/58 ,  C07D413/06

CPC分类号： C07D417/06 ,  C07D215/58 ,  C07D401/06 ,  C07D401/12 ,  C07D413/06 ,  C07D413/14

摘要： Described are RORγ modulators of the formula (I), or pharmaceutically acceptable salts thereof, wherein all substituents are defined herein. The invention includes stereoisomeric forms of the compounds of formula I, including stereoisomerically-pure, scalemic and racemic form, as well as tautomers thereof. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

公开(公告)号：US09663469B2

公开(公告)日：2017-05-30

申请号：US14917420

申请日：2014-09-08

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： T. G. Murali Dhar ,  Jingwu Duan ,  Hua Gong ,  Bin Jiang ,  Zhonghui Lu ,  David S. Weinstein

IPC分类号： C07D279/16 ,  C07D401/06 ,  C07D417/06 ,  C07D215/58 ,  C07D401/14 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/04 ,  C07D491/10 ,  C07D405/14 ,  C07D409/12 ,  C07D471/10 ,  C07D487/10 ,  C07D491/044

CPC分类号： C07D215/58 ,  C07D279/16 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07D471/10 ,  C07D487/10 ,  C07D491/04 ,  C07D491/044 ,  C07D491/10

摘要： Described are RORγ modulators of the formula (I), or pharmaceutically acceptable salts thereof, wherein all substituents are defined herein. The invention includes stereoisomeric forms of the compounds of formula I, including stereoisomerically-pure, scalemic and racemic form, as well as tautomers thereof. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

公开(公告)号：US20160185776A1

公开(公告)日：2016-06-30

申请号：US14911485

申请日：2014-08-21

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： David S. Weinstein ,  Hua Gong ,  Michael G Yang ,  Zili Xiao

IPC分类号： C07D471/04 ,  C07D311/90

CPC分类号： C07D471/04 ,  C07D311/80 ,  C07D311/90 ,  C07D491/04

摘要： Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-KB activity, including metabolic and inflammatory and immune diseases or disorders, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a pharmaceutically-acceptable salt thereof, in which the variables are as defined in the specification.

摘要翻译： 提供了新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病或病症，所述疾病或病症包括代谢和炎症和免疫疾病或病症，其具有式 （I）：其对映异构体，非对映异构体或其互变异构体或其药学上可接受的盐，其中变量如说明书中所定义。

公开(公告)号：US20150299139A1

公开(公告)日：2015-10-22

申请号：US14441213

申请日：2013-11-07

申请人： Bristol-Myers Squibb Company

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

IPC分类号： C07D239/48

CPC分类号： C07D239/48 ,  C07D239/95

摘要： 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.

摘要翻译： 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。