公开(公告)号：EP2545045A1

公开(公告)日：2013-01-16

申请号：EP11711709.3

申请日：2011-03-09

申请人： Incyte Corporation

发明人： HUANG, Taisheng ,  XUE, Chu-Biao ,  WANG, Anlai ,  KONG, Ling ,  YE, Hai Fen ,  YAO, Wenqing ,  RODGERS, James D. ,  SHEPARD, Stacey ,  WANG, Haisheng ,  SHAO, Lixin ,  LI, Hui-Yin ,  LI, Qun

IPC分类号： C07D401/14 ,  C07D405/14 ,  A61K31/4155 ,  A61K31/437 ,  A61K31/4468 ,  A61P29/00

CPC分类号： A61K31/4545 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0024 ,  A61K9/0048 ,  A61K31/519 ,  A61P1/00 ,  A61P11/00 ,  A61P11/06 ,  A61P27/02 ,  A61P35/00 ,  C07B2200/13 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00

摘要： The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

公开(公告)号：EP3036238A1

公开(公告)日：2016-06-29

申请号：EP14766267.0

申请日：2014-08-22

申请人： Incyte Corporation

发明人： LI, Yun-Long ,  BURNS, David M. ,  FENG, Hao ,  HUANG, Taisheng ,  MEI, Song ,  PAN, Jun ,  VECHORKIN, Oleg ,  YE, Hai Fen ,  ZHU, Wenyu ,  RAFALSKI, Maria ,  WANG, Anlai ,  XUE, Chu-Biao

IPC分类号： C07D491/048 ,  C07D495/04 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/5025 ,  A61P35/00 ,  A61P37/02 ,  A61P37/08 ,  A61P9/10

CPC分类号： C07D495/04 ,  C07D491/048

摘要： The present disclosure describes furo-and thieno-pyridine carboxamide compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: X is S or 0; A
5 is N or C-R
5 . Cy
A is a 5 to 6 membered monocyclic heteroaryl group, wherein the ring atoms of the heteroaryl group forming Cy
A consist of carbon atoms and 1, 2, or 3 heteroatoms selected from N, 0 and S, and wherein the 5 to 6 membered monocyclic heteroaryl group forming Cy
A is unsubstituted or substituted with 1, 2, or 3 R
A ; Cy
B is C
6-10 aryl, C
3-7 cycloalkyl, 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl wherein the ring atoms of the ring atoms of the heteroaryl or heterocycloalkyl forming Cy
B consist of carbon atoms and 1, 2 or 3 heteroatoms selected from 0, N and S, and wherein each of said C
6-10 aryl, C
3-7 cycloalkyl, 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl forming Cy
B is unsubstituted or substituted with 1, 2, 3, 4 or 5 R
B ; R
2 is H, halogen or NH
2 ; and R
5 , R
6 and R
7 are as defined in claim 1; The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

摘要翻译： 本公开描述了呋喃和噻吩并吡啶甲酰胺化合物，以及它们的组合物和使用方法。 该化合物抑制Pim激酶的活性，并且可用于治疗与Pim激酶活性相关的疾病，包括例如癌症和其它疾病。