公开(公告)号：EP3589628A1

公开(公告)日：2020-01-08

申请号：EP18761960.6

申请日：2018-03-01

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 ,  BARRISH, Joel, Charles ,  GREENLEE, William ,  EASTMAN, Kyle, J.

IPC分类号： C07D403/08 ,  C07F9/572

公开(公告)号：EP3110418B1

公开(公告)日：2019-11-06

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： C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  A61K31/416 ,  A61K31/401 ,  A61P37/00

公开(公告)号：EP2970195B1

公开(公告)日：2017-08-02

申请号：EP14722457.0

申请日：2014-03-14

申请人： Achillion Pharmaceuticals, Inc.

发明人： PHADKE, Avinash ,  HASHIMOTO, Akihiro ,  GADHACHANDA, Venkat

IPC分类号： C07D401/12

CPC分类号： C07K5/06139 ,  C07B2200/13 ,  C07D207/16 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07K5/0821

公开(公告)号：EP3059241A1

公开(公告)日：2016-08-24

申请号：EP16157270.6

申请日：2012-05-29

申请人： Achillion Pharmaceuticals, Inc.

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

IPC分类号： C07F17/02 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D471/14 ,  C07D491/10 ,  C07D519/00 ,  A61K31/4178 ,  A61K31/4164 ,  A61P31/00 ,  A61P31/12

CPC分类号： A61K31/4184 ,  A61K9/0053 ,  A61K9/20 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/555 ,  A61K45/06 ,  A61K2300/00 ,  C07D209/42 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D453/06 ,  C07D471/08 ,  C07D491/10 ,  C07D491/113 ,  C07D519/00 ,  C07F5/025 ,  C07F15/02 ,  C07F17/02

摘要： Provided is a compound having a structure selected from the group consisting of:




which are intermediates in the preparation of Carbamic acid,
N,N'-[tricyclo[8.2.2.24,7]hexadeca-4,6,10,12,13,15-hexaene-5,11-diyl bis [1H-benzimidazole-6,2-diyl[(2S,3aS,7aS)-octahydro-1H-indole-2,1-diyl][(1S)-1-(1-methylethyl)-2-oxo-2,1-ethane diyl]]] bis-, C,C'-dimethyl ester, which is a Hepatitis C virus NS5a (HCV NS5a) protease replication inhibitor

摘要翻译： 本发明提供具有选自以下的结构的化合物：其为制备氨基甲酸的N，N' - [三环[8.2.2.24,7]十六氢-4,6,10,12,13， （2S，3aS，7aS） - 八氢-1H-吲哚-2,1-二基] [（1S）-1-（1（1H-苯并咪唑） - 甲基乙基）-2-氧代-2,1-乙烷二基]]]双 - ，C，C'-二甲基酯，其为丙型肝炎病毒NS5a（HCV NS5a）蛋白酶复制抑制剂

公开(公告)号：EP2041156B1

公开(公告)日：2013-11-20

申请号：EP07810457.7

申请日：2007-07-13

申请人： Achillion Pharmaceuticals, Inc.

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

IPC分类号： C07K5/02 ,  C07K5/06 ,  A61K38/00 ,  C07K5/08

CPC分类号： A61K38/05 ,  A61K38/00 ,  A61K38/12 ,  A61K45/06 ,  C07K5/02 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191 ,  C07K5/0808 ,  C07K5/12

摘要： The invention provides 4-amino-4-oxobutanoyl peptide compounds of Formula I and the pharmaceutically salts and hydrates thereof. The variables R 1 -R 9 , R 16 , R 18 , R 19 , n, M, , n, M, , and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain 4-amino-4-oxobutanoyl peptide compounds disclosed herein are potent and/ or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide compounds and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain 4-amino-4-oxobutanoyl peptide compound as the only active agent or may contain a combination of 4-amino-4-oxobutanoyl peptide containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.

公开(公告)号：EP2364310A4

公开(公告)日：2012-05-16

申请号：EP09832542

申请日：2009-12-10

申请人： ACHILLION PHARMACEUTICALS INC

发明人： PHADKE AVINASH ,  WANG XIANGZHU ,  PAIS GODWIN ,  HASHIMOTO AKIHIRO ,  GADHACHANDA VENKAT ,  CHEN DAWEI ,  AGARWAL ATUL ,  ZHANG SUOMING ,  LIU CUIXIAN ,  LI SHOUMING ,  DESHPANDE MILIND

IPC分类号： C07D403/14 ,  A61K38/05 ,  C07D403/12 ,  C07D417/14 ,  C07K5/06

CPC分类号： C07K5/12 ,  A61K38/00 ,  C07K5/06165

公开(公告)号：EP2414368A2

公开(公告)日：2012-02-08

申请号：EP10759532.4

申请日：2010-04-05

申请人： Achillion Pharmaceuticals, Inc.

发明人： BRADBURY, Barton James ,  DESHPANDE, Milind ,  HASHIMOTO, Akihiro ,  KIM, Ha Young ,  LUCIEN, Edlaine ,  PAIS, Godwin ,  PUCCI, Michael ,  WANG, Qiuping ,  WILES, Jason Allan ,  PHADKE, Avinash

IPC分类号： C07D495/04 ,  C07D495/16 ,  C07D495/14 ,  A61P29/00

CPC分类号： A61K31/4743 ,  A61K31/496 ,  C07D495/04 ,  C07D498/16 ,  C07D519/00

摘要： Disclosed herein are hydroxythienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula (I) in which the variables R
2 , R
6 , and R
7 are defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The invention also provides pharmaceutical compositions, pharmaceutical compositions containing a hydroxythienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a hydroxythienoquinolone or related compound to an animal suffering from a microbial infection.

摘要翻译： 本文公开了羟基噻吩并喹啉酮和相关化合物及其药学上可接受的盐，其可用作抗病毒剂且具有通式（I），其中变量R 2，R 6和R 7如本文所定义。 本文提供的某些化合物具有有效的抗菌，抗原生动物或抗真菌活性，并且对于治疗MRSA感染特别有效。 本发明还提供药物组合物，包含羟基噻吩并喹诺酮与一种或多种其他活性剂的组合的药物组合物，以及通过将有效量的羟基噻吩并喹诺酮或相关化合物给予患有微生物感染的动物来治疗动物中的微生物感染的方法。

公开(公告)号：EP2374812A2

公开(公告)日：2011-10-12

申请号：EP11169378.4

申请日：2007-07-13

申请人： Achillion Pharmaceuticals, Inc.

发明人： Phadke, Avinash ,  Zhang, Suoming ,  Wang, Xiangzhu ,  Agarwal, Atul

IPC分类号： C07K5/02 ,  C07K5/06 ,  A61K38/00 ,  C07K5/08

CPC分类号： A61K38/05 ,  A61K38/00 ,  A61K38/12 ,  A61K45/06 ,  C07K5/02 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191 ,  C07K5/0808 ,  C07K5/12

摘要： The invention provides 4-amino-4-oxobutanoyl peptide compounds of Formula I

and the pharmaceutically salts and hydrates thereof.
The variables R 1 -R 9 , R 16 , R 18 , R 19 , n, M, , n, M, , and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain 4-amino-4-oxobutanoyl peptide compounds disclosed herein are potent and/ or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide compounds and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain 4-amino-4-oxobutanoyl peptide compound as the only active agent or may contain a combination of 4-amino-4-oxobutanoyl peptide containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.

公开(公告)号：EP2297143A1

公开(公告)日：2011-03-23

申请号：EP09759594.6

申请日：2009-06-08

申请人： Achillion Pharmaceuticals, Inc.

发明人： LIU, Cuixan ,  PHADKE, Avinash ,  WANG, Xiangzhu ,  ZHANG, Suoming

IPC分类号： C07D417/04 ,  C07D417/14 ,  A61K31/4436 ,  A61P1/00

CPC分类号： C07D417/04 ,  C07D417/14

摘要： The invention provides amino-substituted aminothiazole compounds of Formula (I) and Formula (II) where A is a group of the formula: and the variables X, Y, R, and R
1 to R
7 are described herein. These compounds are prodrugs of compounds useful as inhibitors of viral replication. Compositions containing such compounds, and methods of treating viral infections with these compounds, as well as to processes and intermediates useful for preparing such compounds are also provided by the invention.

公开(公告)号：EP2266579A1

公开(公告)日：2010-12-29

申请号：EP10177224.2

申请日：2005-10-18

申请人： Achillion Pharmaceuticals, Inc.

发明人： Pottage, John

IPC分类号： A61K31/70 ,  A61K31/55 ,  A61K31/535 ,  A61P31/14 ,  A61P31/18 ,  A61K9/00

CPC分类号： A61K31/535 ,  A61K9/2022 ,  A61K9/2027 ,  A61K31/513 ,  A61K31/522 ,  A61K31/55 ,  A61K31/551 ,  A61K31/70 ,  A61K31/7072 ,  A61K45/06 ,  A61K2300/00

摘要： A pharmaceutical composition comprising elvucitabine, lactose monohydrate, and anhydrous lactose, in which the lactose monohydrate and anhydrous lactose taken together comprise about 60 percent to about 90 percent of the pharmaceutical composition by weight.

摘要翻译： 一种药物组合物，其包含一次性水溶液和无水乳糖，其中乳糖一水合物和无水乳糖组合在一起包含按重量计约60％至约90％的药物组合物。