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51. 发明公开

EP2041156A1 4-AMINO-4-OXOBUTANOYL PEPTIDES AS INHIBITORS OF VIRAL REPLICATION 有权
标题翻译： 4-氨基-4-氧代哌嗪代谢物ALS HEMMER VIRALER REPLIKATION
公开(公告)号：EP2041156A1
公开(公告)日：2009-04-01
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 rovides 4-amino-4-oxobutanoyl peptide compounds of Formula I (I) and the pharmaceutically salts and hydrates thereof. The variables R1-R9, R16, R18 R19, 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.
摘要翻译：本发明提供式I的4-氨基-4-氧代丁酰基肽化合物及其药用盐和水合物。变量R 1 -R 9，R 16，R 18，R 19，n，M，，n，M，和Z在本文中定义。某些式I的化合物可用作抗病毒剂。本文公开的某些4-氨基-4-氧代丁酰肽化合物是病毒复制的有效和/或选择性抑制剂，特别是丙型肝炎病毒复制。本发明还提供含有一种或多种4-氨基-4-氧代丁酰基肽化合物和一种或多种药学上可接受的载体的药物组合物。这样的药物组合物可以含有4-氨基-4-氧代丁酰基肽化合物作为唯一的活性剂，或者可以含有含有肽化合物的4-氨基-4-氧代丁酰肽与一种或多种其它药物活性剂的组合。本发明还提供了用于治疗哺乳动物中的病毒感染（包括丙型肝炎感染）的方法。

52. 发明公开

EP3623367A1 ARYL, HETEROARYL, AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF COMPLEMENT MEDIATED DISORDERS 有权转让
公开(公告)号：EP3623367A1
公开(公告)日：2020-03-18
申请号：EP19206925.0
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, Avisash, S.
IPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , A61P37/00 , A61K31/416 , A61K31/401
摘要： Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula II, 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.

53. 发明授权

EP3059241B1 INTERMEDIATES IN THE PREPARATION OF A BIS(BENZIMIDAZOLE)CYCLOPHANE DERIVATIVE 有权
标题翻译：中间体在制备双（苯并咪唑）环烷基衍生物
公开(公告)号：EP3059241B1
公开(公告)日：2017-11-01
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

54. 发明公开

EP3110806A1 PHOSPHONATE COMPOUNDS FOR TREATMENT OF COMPLEMENT MEDIATED DISORDERS 审中-公开
标题翻译： PHOSPHONATVERBINDUNGEN ZUR BEHANDLUNG VON KOMPLEMENTVERMITTELTEN ERKRANKUNGEN
公开(公告)号：EP3110806A1
公开(公告)日：2017-01-04
申请号：EP15755701.8
申请日：2015-02-25
申请人： Achillion Pharmaceuticals, Inc.
发明人： WILES, Jason, Allan , HASHIMOTO, Akihiro , GADHACHANDA, Venkat, Rao , PAIS, Godwin , WANG, Qiuping , CHEN, Dawei , WANG, Xiangzhu , AGARWAL, Atul , DESHPANDE, Milind , PHADKE, Avinash, S.
IPC分类号： C07D401/14 , C07D403/14 , C07D471/04
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。

55. 发明公开

EP3110804A1 CARBAMATE, ESTER, AND KETONE COMPOUNDS FOR TREATMENT OF COMPLEMENT MEDIATED DISORDERS 审中-公开
标题翻译： CARBAMAT-，ESTER- UND KETONVERBINDUNGEN ZUR BEHANDLUNG VON KOMPLEMENTVERMITTELTEN ERKRANKUNGEN
公开(公告)号：EP3110804A1
公开(公告)日：2017-01-04
申请号：EP15755090.6
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： C07D401/14 , C07D403/14 , C07D471/04
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。

56. 发明公开

EP2364310A2 4-AMINO-4-OXOBUTANOYL PEPTIDE CYCLIC ANALOGUES, INHIBITORS OF VIRAL REPLICATION 有权
标题翻译：例如病毒复制抑制剂4-氨基-4-氧丁肽环状类似物
公开(公告)号：EP2364310A2
公开(公告)日：2011-09-14
申请号：EP09832542.6
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 , C07D403/12 , C07D417/14
CPC分类号： C07K5/12 , A61K38/00 , C07K5/06165
摘要： The invention provides 4-amino-4-oxobutanoyl peptides and cyclic analogues thereof of Formula I and the pharmaceutically salts thereof. The variables are defined herein. Certain compounds of Formula I are useful as antiviral agents. 4-amino-4-oxobutanoyl peptide cyclic analogues as 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 cyclic analogues and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptide cyclic analogue as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptide cyclic analogue and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in patients.

57. 发明公开

EP1879575A2 THIAZOLE COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：噻唑和其使用方法
公开(公告)号：EP1879575A2
公开(公告)日：2008-01-23
申请号：EP06770077.3
申请日：2006-05-09
申请人： Achillion Pharmaceuticals, Inc.
发明人： ZHANG, Suoming , PHADKE, Avinash , LIU, Cuixian , WANG, Xiangzhu , QUINN, Jesse , CHEN, Dawei , GADHACHANDA, Venkat , LI, Shouming , DESHPANDE, Milind
IPC分类号： A61K31/426 , A61K31/427 , A61P31/12 , C07D487/04
CPC分类号： C07D487/04 , C07D277/38 , C07D277/42 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/ or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.

58. 发明公开

EP1562895A1 SUBSTITUTED ARYL ACYLTHIOUREAS AND RELATED COMPOUNDS; INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：维多利亚州立大学抑制剂维生素修复
公开(公告)号：EP1562895A1
公开(公告)日：2005-08-17
申请号：EP03786803.1
申请日：2003-11-18
申请人： Achillion Pharmaceuticals, Inc.
发明人： CHEN, Dawei , DESHPANDE, Milind , THURKAUF, Andrew , PHADKE, Avinash , WANG, Xiangzhu , SHEN, Yiping , LIU, Cuixian , QUINN, Jesse , OHKANDA, Junko , LI, Shouming
IPC分类号： C07C335/26 , C07D207/16 , C07D207/34 , C07D209/48 , C07D211/62 , C07D211/70 , C07D211/86 , C07D213/65 , C07D213/81 , C07D215/06 , C07D217/04 , C07D233/90 , C07D239/26 , C07D257/04 , C07D261/18
CPC分类号： C07D209/48 , C07C335/26 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/12 , C07D207/16 , C07D207/34 , C07D207/416 , C07D209/42 , C07D211/14 , C07D211/62 , C07D211/70 , C07D211/86 , C07D213/64 , C07D213/65 , C07D213/81 , C07D215/06 , C07D215/48 , C07D217/04 , C07D231/14 , C07D233/42 , C07D233/90 , C07D239/26 , C07D241/24 , C07D241/44 , C07D249/06 , C07D257/04 , C07D261/18 , C07D263/34 , C07D263/57 , C07D271/08 , C07D271/12 , C07D277/56 , C07D277/66 , C07D277/68 , C07D285/06 , C07D295/135 , C07D295/15 , C07D307/52 , C07D307/68 , C07D307/85 , C07D311/24 , C07D311/66 , C07D317/66 , C07D319/20 , C07D333/20 , C07D333/34 , C07D333/38 , C07D333/70 , C07D405/04 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D487/04 , C07D495/04
摘要： The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/ or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.
摘要翻译：本发明提供式I的化合物和药学上可接受的盐，其中变量A1，A2，R1，R2，V，W，X，Y和Z在本文中定义。本文所述的某些具有强的抗病毒活性的式I化合物。本发明特别提供了作为丙型肝炎病毒复制的有效和/或选择性抑制剂的式I化合物。本发明还提供含有一种或多种式I化合物或这些化合物的盐，溶剂化物或酰化前药以及一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。本发明还包括通过向所述患者施用一定量的有效降低疾病或病症的体征或症状的式I化合物来治疗患有某些感染性疾病的患者的方法。这些传染病包括病毒感染，特别是HCV感染。本发明特别包括治疗患有感染性疾病的人类患者的方法，还包括治疗患有感染性疾病的其它动物，包括牲畜和驯养的伴侣动物的方法。治疗方法包括给予式I化合物作为单一活性剂或给予式I化合物与一种或多种其它治疗剂的组合。

59. 发明公开

EP3340982A1 COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS 有权转让
公开(公告)号：EP3340982A1
公开(公告)日：2018-07-04
申请号：EP16840164.4
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 , GREENLEE, William
IPC分类号： A61K31/40 , A61K31/167 , A61K31/395 , C07D401/14 , C07D403/14 , C07D471/04
CPC分类号： C07D209/12 , A61K45/06 , A61P1/16 , C07D207/16 , C07D231/56 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I′″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

60. 发明公开

EP3340981A1 ARYL, HETEROARYL, AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS 有权转让
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.

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