公开(公告)号：EP3340981A1

公开(公告)日：2018-07-04

申请号：EP16840121.4

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： A61K31/40 ,  A61K31/167 ,  A61K31/395 ,  C07D401/14 ,  C07D403/14 ,  C07D471/04

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

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 R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.

公开(公告)号：EP3110423A2

公开(公告)日：2017-01-04

申请号：EP15755233.2

申请日：2015-02-25

申请人： Achillion Pharmaceuticals, Inc.

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

IPC分类号： A61K31/519

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，使用方法和制备包含式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，其中A组中的R 12或R 13是膦酸酯（R32）。 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：EP3110418A1

公开(公告)日：2017-01-04

申请号：EP15755617.6

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 ,  AGARWAL, Atul ,  DESHPANDE, Milind ,  WILES, Jason, Allan ,  PHADKE, Avinash, S.

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

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：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：EP2125113A2

公开(公告)日：2009-12-02

申请号：EP08726107.9

申请日：2008-02-26

申请人： Achillion Pharmaceuticals, Inc.

发明人： AGARWAL, Atul ,  WANG, Xiangzhu ,  CHEN, Dawei ,  ZHANG, Suoming ,  PHADKE, Avinash

IPC分类号： A61P31/14 ,  A61K38/06 ,  C07K5/08

CPC分类号： C07K5/06078 ,  A61K38/00 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/0812

摘要： The present invention provides tertiary amine substituted peptides of Formula (I) useful as inhibitors of HCV replication. The variables R and R1-R12 in Formula I are described herein. The invention also includes methods for preparing such compounds. The present invention further includes pharmaceutical compositions containing tertiary amine substituted peptides and methods for using such compounds, including methods for using the compounds to treat hepatitis C infection.