公开(公告)号：EP3110417A1

公开(公告)日：2017-01-04

申请号：EP15754663.1

申请日：2015-02-25

申请人： Achillion Pharmaceuticals, Inc.

发明人： GADHACHANDA, Venkat Rao ,  HASHIMOTO, Akihiro ,  PAIS, Godwin ,  WANG, Qiuping ,  CHEN, Dawei ,  WANG, Xiangzhu ,  AGARWAL, Atul ,  DESHPANDE, Milind ,  WILES, Jason Allan ,  PHADKE, Avinash S.

IPC分类号： A61K31/401 ,  A61P37/00 ,  A61K31/416

CPC分类号： C07F9/5728 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0048 ,  A61K9/0053 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/549 ,  A61K31/55 ,  A61K31/675 ,  A61K31/683 ,  C07B59/002 ,  C07B2200/05 ,  C07D209/12 ,  C07D209/14 ,  C07D209/30 ,  C07D209/40 ,  C07D209/42 ,  C07D209/44 ,  C07D209/88 ,  C07D401/14 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/14 ,  C07D491/113 ,  C07D495/04 ,  C07D513/04 ,  C07F5/025 ,  C07F5/027 ,  C07F7/0812 ,  C07F9/65583 ,  C07F9/6561 ,  C07F9/65616

摘要： Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

摘要翻译： 提供化合物，使用方法以及制备包含式I的补体因子D的抑制剂的方法或其药学上可接受的盐或组合物。 本文描述的抑制剂靶向因子D并且在替代补体途径的早期和必需点抑制或调节补体级联，并降低D因子调节经典和凝集素补体途径的能力。 本文所述的因子D的抑制剂能够减少与某些自身免疫性，炎性和神经变性疾病以及缺血 - 再灌注损伤和癌症相关的补体的过度活化。

公开(公告)号：EP4053117A1

公开(公告)日：2022-09-07

申请号：EP22166051.7

申请日：2016-08-25

申请人： Achillion Pharmaceuticals, Inc.

发明人： WILES, Jason Allan ,  PHADKE, Avinash S. ,  DESHPANDE, Milind ,  AGARWAL, Atul ,  CHEN, Dawei ,  GADHACHANDA, Venkat Rao ,  HASHIMOTO, Akihiro ,  PAIS, Godwin ,  WANG, Qiuping ,  WANG, Xiangzhu

IPC分类号： C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  C07D493/04 ,  C07D495/04 ,  A61P1/16

摘要： Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R 12 or R 13 on the A group is an aryl, heteroaryl or heterocycle (R 32 ) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.

公开(公告)号：EP4129407A1

公开(公告)日：2023-02-08

申请号：EP22193148.8

申请日：2015-02-25

申请人： Achillion Pharmaceuticals, Inc.

发明人： GADHACHANDA, Venkat Rao ,  WANG, Qiuping ,  PAIS, Godwin ,  HASHIMOTO, Akihiro ,  CHEN, Dawei ,  WANG, Xiangzhu ,  ARARWAL, Atul ,  DESHPANDE, Milind ,  WILES, Jason Allan ,  PHADKE, Avinash S.

IPC分类号： A61P37/00 ,  A61K31/416 ,  A61K31/401 ,  C07D401/14 ,  C07D403/14

摘要： Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formulae X or VI, or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.