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1. 发明申请

US20190135825A1 Quinazoline and Indole Compounds to Treat Medical Disorders 审中-公开
公开(公告)号：US20190135825A1
公开(公告)日：2019-05-09
申请号：US16226378
申请日：2018-12-19
申请人： Achillion Pharmaceuticals, Inc.
发明人： Jason Allan Wiles , Avinash Phadke
IPC分类号： C07D491/056 , C07D239/94 , C07D403/14 , C07D401/06 , C07D401/04 , C07D401/14 , C07D417/14 , C07D451/02 , C07D471/02
摘要： Compounds, methods of use, and processes for making inhibitors of Complement Factor B are provided.

2. 发明申请

US20190085005A1 PHOSPHONATE COMPOUNDS FOR TREATMENT OF COMPLEMENT MEDIATED DISORDERS 审中-公开
公开(公告)号：US20190085005A1
公开(公告)日：2019-03-21
申请号：US16162162
申请日：2018-10-16
申请人： Achillion Pharmaceuticals, Inc.
发明人： Jason Allan Wiles , Akihiro Hashimoto , Venkat Rao Gadhachanda , Godwin Pais , Qiuping wang , Dawei Chen , Xiangzhu Wang , Atul Agarwal , Milind Deshpande , Avinash Phadke
IPC分类号： C07F9/572 , C07D417/06 , C07F7/08 , C07D401/14 , C07D403/14 , C07D403/12 , C07D209/42 , C07D471/08 , C07D209/30 , C07D209/44 , C07D209/88 , C07D209/12 , A61K31/519 , A61K31/501 , A61K9/00 , A61K31/4045 , A61K31/444 , A61K31/675 , A61K31/404 , A61K31/407 , A61K31/4162 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/549 , A61K31/55 , A61K31/683 , C07F9/6558 , C07F9/6561 , C07D513/04 , C07B59/00 , C07D209/14 , C07D209/40 , C07D405/12 , C07D417/12 , C07D487/14 , C07D491/113 , C07D495/04 , C07D413/06 , C07D403/08 , C07D405/14 , C07D487/04 , C07D413/14 , C07D417/14 , C07D403/06 , C07F5/02 , C07D471/04
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 a phosphonate (R32) 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.

3. 发明授权

US10100072B2 Phosphonate compounds for treatment of complement mediated disorders 有权
公开(公告)号：US10100072B2
公开(公告)日：2018-10-16
申请号：US15607120
申请日：2017-05-26
申请人： Achillion Pharmaceuticals, Inc.
发明人： Jason Allan Wiles , Akihiro Hashimoto , Venkat Rao Gadhachanda , Godwin Pais , Qiuping Wang , Dawei Chen , Xiangzhu Wang , Atul Agarwal , Milind Deshpande , Avinash Phadke
IPC分类号： C07F9/6561 , C07F9/6558 , C07F9/572 , C07F7/08 , C07F5/02 , C07B59/00 , C07D495/04 , A61K31/683 , A61K31/55 , A61K31/506 , A61K31/496 , A61K31/4439
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 a phosphonate (R32) 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.

4. 发明申请

US20180055824A1 SUBSTITUTED ALIPHANES, CYCLOPHANES, HETERAPHANES, HETEROPHANES, HETERO-HETERAPHANES AND METALLOCENES USEFUL FOR TREATING HCV INFECTIONS 审中-公开
公开(公告)号：US20180055824A1
公开(公告)日：2018-03-01
申请号：US15804842
申请日：2017-11-06
申请人： Achillion Pharmaceuticals, Inc.
发明人： Jason Allan Wiles , Qiuping Wang , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Venkat Gadhachanda , Avinash Phadke , Milind Deshpande , Dawei Chen
IPC分类号： A61K31/4184 , C07F17/02 , C07D401/14 , C07D209/42 , C07D403/04 , A61K9/20 , A61K9/00 , C07F15/02 , A61K31/427 , A61K31/454 , C07D453/06 , C07D491/113 , A61K31/422 , C07F5/02 , C07D403/14 , C07D413/14 , C07D417/14 , C07D471/08 , C07D491/10 , C07D519/00 , A61K45/06 , A61K31/4178 , A61K31/555 , A61K31/496 , A61K31/439
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： The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D (Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.

5. 发明授权

US09468629B2 Substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes useful for treating HCV infections 有权
公开(公告)号：US09468629B2
公开(公告)日：2016-10-18
申请号：US14972827
申请日：2015-12-17
申请人： Achillion Pharmaceuticals, Inc
发明人： Jason Allan Wiles , Qiuping Wang , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Venkat Gadhachanda , Avinash Phadke , Milind Deshpande , Dawei Chen
IPC分类号： C07D403/14 , C07D403/04 , C07F5/02 , C07D209/42 , A61K31/4184 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/08 , C07D491/10 , C07D519/00 , A61K45/06 , A61K31/4178 , A61K31/439 , A61K31/496 , A61K31/555 , C07F17/02 , A61K31/422 , A61K31/427 , A61K31/454 , C07D453/06 , C07D491/113 , C07F15/02 , A61K9/00 , A61K9/20
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： The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D (Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.

6. 发明申请

US20160115157A1 SUBSTITUTED ALIPHANES, CYCLOPHANES, HETERAPHANES, HETEROPHANES, HETERO-HETERAPHANES AND METALLOCENES USEFUL FOR TREATING HCV INFECTIONS 有权
公开(公告)号：US20160115157A1
公开(公告)日：2016-04-28
申请号：US14972827
申请日：2015-12-17
申请人： Achillion Pharmaceuticals, Inc
发明人： Jason Allan Wiles , Qiuping Wang , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Venkat Gadhachanda , Avinash Phadke , Milind Deshpande , Dawei Chen
IPC分类号： C07D403/14 , C07D403/04 , C07F5/02 , C07D209/42
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： The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D (Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.

7. 发明授权

US09115175B2 Processes for Producing sovaprevir 有权
标题翻译：生产sovaprevir的方法
公开(公告)号：US09115175B2
公开(公告)日：2015-08-25
申请号：US14211510
申请日：2014-03-14
申请人： Achillion Pharmaceuticals, Inc.
发明人： Avinash Phadke , Akihiro Hashimoto , Venkat Gadhachanda
IPC分类号： C07K5/097 , C07D401/12 , C07D207/16 , C07D401/06
CPC分类号： C07K5/06139 , C07B2200/13 , C07D207/16 , C07D401/06 , C07D401/12 , C07D401/14 , C07K5/0821
摘要： The disclosure includes novel processes for producing Sovaprevir comprising adding compound E to F-1 to provide Sovaprevir. The disclosure further includes intermediates useful for producing Sovaprevir. The disclosure also include a novel crystalline form of Sovaprevir, Form F, and a method for preparing spray-dried amorphous Sovaprevir from crystalline Form F.
摘要翻译：本公开内容包括用于生产索普伐维尔的新方法，其包括向F-1中加入化合物E以提供索伐他韦。本公开还包括可用于生产索维普韦的中间体。本公开还包括新型结晶形式的Sovaprevir，Form F，以及从晶型F制备喷雾干燥的无定形Sovaprevir的方法。

8. 发明申请

US20140328796A1 4-AMINO-4-OXOBUTANOYL PEPTIDES AS INHIBITORS OF VIRAL REPLICATION 有权
标题翻译：作为病毒复制抑制剂的4-氨基-4-氧代哌啶
公开(公告)号：US20140328796A1
公开(公告)日：2014-11-06
申请号：US14336427
申请日：2014-07-21
申请人： ACHILLION PHARMACEUTICALS, INC.
发明人： Avinash Phadke , Xiangzhu Wang , Suoming Zhang , Atul Agarwal
IPC分类号： A61K38/05 , A61K38/12 , C07K5/12 , C07K5/078 , A61K45/06
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 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：本发明提供了式I的4-氨基-4-氧代丁酰基肽化合物及其药学上可接受的盐和水合物。变量R1-R9，R16，R18，R19，n，M，n，M和Z在本文中定义。某些式I化合物可用作抗病毒剂。本文公开的某些4-氨基-4-氧代丁酰基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4-氨基-4-氧代丁酰基肽的肽化合物和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。

9. 发明申请

US20140271855A1 SOVAPREVIR TABLETS 审中-公开
标题翻译： SOVAPREVIR平板电脑
公开(公告)号：US20140271855A1
公开(公告)日：2014-09-18
申请号：US14208195
申请日：2014-03-13
申请人： Achillion Pharmaceuticals Inc.
发明人： Jennifer Hsing-Chung Chu , Gautam Shah , Avinash Phadke
IPC分类号： A61K9/28 , A61K9/20 , A61K38/05
CPC分类号： A61K9/28 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2059 , A61K31/4709 , A61K38/05
摘要： The disclosure includes tablet cores comprising Sovaprevir and a crystal growth inhibitor selected from hydroxypropyl methyl cellulose (HPMC), HPC (hydroxypropyl cellulose), hypromellose acetate succinate (HPMCAS), polyvinyl pyrrolidone (PVP), copovidone (PVP-VA), a copolymer of methacrylic acid and ethyl acrylate, or any combination of the foregoing, wherein ratio of Sovaprevir to crystal growth inhibitor is from about 40:60 (w/w) to about 60:40 (w/w). The disclosure further includes film coated tables. The disclosure also includes methods of treating HCV with the tablets described herein.
摘要翻译：本发明包括包含索伐他汀的片芯和选自羟丙基甲基纤维素（HPMC），HPC（羟丙基纤维素），乙酸琥珀酸羟丙甲纤维素（HPMCAS），聚乙烯吡咯烷酮（PVP），共聚维酮（PVP-VA））的结晶生长抑制剂，甲基丙烯酸和丙烯酸乙酯，或上述的任何组合，其中索普伐维尔与晶体生长抑制剂的比例为约40:60（w / w）至约60:40（w / w）。本公开还包括薄膜包衣桌。本公开还包括用本文所述的片剂治疗HCV的方法。

10. 发明授权

US10092547B2 Substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero- heteraphanes and metallocenes useful for treating HCV infections 有权
公开(公告)号：US10092547B2
公开(公告)日：2018-10-09
申请号：US15804842
申请日：2017-11-06
申请人： Achillion Pharmaceuticals, Inc.
发明人： Jason Allan Wiles , Qiuping Wang , Akihiro Hashimoto , Godwin Pais , Xiangzhu Wang , Venkat Gadhachanda , Avinash Phadke , Milind Deshpande , Dawei Chen
IPC分类号： A61K31/4184 , C07F17/02 , C07D401/14 , C07D209/42 , C07D403/04 , A61K9/20 , A61K9/00 , C07F15/02 , A61K31/427 , A61K31/454 , C07D453/06 , C07D491/113 , A61K31/422 , C07F5/02 , C07D403/14 , C07D413/14 , C07D417/14 , C07D471/08 , C07D491/10 , C07D519/00 , A61K45/06 , A61K31/4178 , A61K31/555 , A61K31/496 , A61K31/439
摘要： The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D (Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.

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