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101. 发明授权

US08034933B2 Piperidine derivatives useful as CCR5 antagonists 失效
标题翻译：哌啶衍生物可用作CCR5拮抗剂
公开(公告)号：US08034933B2
公开(公告)日：2011-10-11
申请号：US12104914
申请日：2008-04-17
申请人： Anandan Palani , Michael W. Miller , Jack D. Scott
发明人： Anandan Palani , Michael W. Miller , Jack D. Scott
IPC分类号： C07D401/14 , C07D239/02
CPC分类号： C07D401/14
摘要： The present invention provides a compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R9, R10, A and B are as defined in the specification. The present invention also provides pharmaceutical compositions containing the compound of this invention, and methods of treatment using the compound of this invention. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.
摘要翻译：本发明提供下式化合物或其药学上可接受的盐或溶剂化物，其中R1，R2，R3，R9，R10，A和B如说明书中所定义。本发明还提供含有本发明化合物的药物组合物和使用本发明化合物的治疗方法。本发明还涉及本发明化合物与一种或多种可用于治疗人类免疫缺陷病毒（HIV）的抗病毒剂或其它药剂的组合的用途。本发明还涉及本发明化合物单独或与另一种药剂组合用于治疗实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化。

102. 发明授权

US07442703B2 Piperidine derivatives useful as CCR5 antagonists 失效
公开(公告)号：US07442703B2
公开(公告)日：2008-10-28
申请号：US10629466
申请日：2003-07-29
申请人： Anandan Palani , Michael W. Miller , Jack D. Scott
发明人： Anandan Palani , Michael W. Miller , Jack D. Scott
IPC分类号： A61K31/505 , C07D401/14
CPC分类号： C07D401/14
摘要： The present invention provides a compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R9, R10, A and B are as defined in the specification. The present invention also provides pharmaceutical compositions containing the compound of this invention, and methods of treatment using the compound of this invention. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.

103. 发明申请

US20050004121A1 MCH antagonists for the treatment of obesity 失效
标题翻译： MCH拮抗剂用于治疗肥胖
公开(公告)号：US20050004121A1
公开(公告)日：2005-01-06
申请号：US10878788
申请日：2004-06-28
申请人： Anandan Palani , Sherry Shapiro , Hubert Josien , Thomas Bara , John Clader , Pradeep Pushpavanam , Shengjian Li , Mark McBriar
发明人： Anandan Palani , Sherry Shapiro , Hubert Josien , Thomas Bara , John Clader , Pradeep Pushpavanam , Shengjian Li , Mark McBriar
IPC分类号： C07D409/14 , A61K31/5377 , A61K31/496
CPC分类号： C07D409/14
摘要： The present invention discloses methods of using antagonists for melanin-concentrating hormone (MCH), to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes, as well as novel compounds which are antagonists for melanin-concentrating hormone (MCH). In other aspects, the invention is directed to pharmaceutical compositions comprising such MCH antagonists as well as methods for preparing such compounds. Compounds of the invention generally have the structure: where the substituents are as defined herein.
摘要翻译：本发明公开了使用拮抗剂用于黑色素浓缩激素（MCH），治疗肥胖症，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法，以及作为黑色素浓缩激素（MCH）拮抗剂的新化合物。在其它方面，本发明涉及包含这种MCH拮抗剂的药物组合物以及制备这些化合物的方法。本发明的化合物通常具有以下结构：其中取代基如本文所定义。

104. 发明公开

US20230257371A1 CYCLIC CYANOENONE DERIVATIVES AS MODULATORS OF KEAP1 审中-公开
公开(公告)号：US20230257371A1
公开(公告)日：2023-08-17
申请号：US18015671
申请日：2021-07-15
申请人： Michael ALTMAN , David A. CANDITO , Alec H. CHRISTIAN , Ornella DI PIETRO , Min LU , Umar Faruk MANSOOR , Katrina Marie MENNIE , Andrew J. MUSACCHIO , Anandan PALANI , Michael H. REUTERSHAN , David Matthew SHAW , MERCK SHARP & DOHME LLC , MSD R&D INNOVATION CENTRE LIMITED
发明人： Michael D. Altman , David A. Canditio , Alec H. Christian , Ornella Di Pietro , Min Lu , Umar Faruk Mansoor , Katrina Marie Mennie , Andrew J. Musacchio , Anandan Palani , Michael H. Reutershan , David Matthew Shaw , Ping Lui , Stephen St-Gallay
IPC分类号： C07D413/04 , C07D403/06 , C07D265/36 , C07D401/06 , C07D491/048 , C07D471/04 , C07D209/96 , C07D487/04 , C07D307/94
CPC分类号： C07D413/04 , C07D403/06 , C07D265/36 , C07D401/06 , C07D491/048 , C07D471/04 , C07D209/96 , C07D487/04 , C07D307/94
摘要： The present invention relates to cyclic cyanoenone derivatives of Formula (I) or pharmaceutically acceptable salts or solvates thereof, wherein R1, R2, R3, R4 and m are as defined herein. The present invention also relates to pharmaceutical compositions comprising the cyclic cyanoenone derivatives of Formula (I) and to their use in therapy.

105. 发明授权

US10793615B2 Long-acting co-agonists of the glucagon and GLP-1 receptors 有权
公开(公告)号：US10793615B2
公开(公告)日：2020-10-06
申请号：US15759911
申请日：2016-10-21
申请人： Merck Sharp & Dohme Corp. , Anandan Palani , Ravi Nargund , Paul E. Carrington , Tomi Sawyer , Qiaolin Deng , Antonello Pessi , Elisabetta Bianchi , Federica Orvieto
发明人： Anandan Palani , Ravi Nargund , Paul E. Carrington , Tomi Sawyer , Qiaolin Deng , Antonello Pessi , Elisabetta Bianchi , Federica Orvieto
IPC分类号： A61K38/00 , A61K38/28 , A61P3/04 , A61P7/12 , A61P3/10 , C07K14/435 , C07K14/605
摘要： Long-acting co-agonists of the glucagon and GLP-1 receptors are described.

106. 发明申请

US20170037056A1 Iminothiadiazepane Dioxide Compounds as BACE Inhibitors, Compositions, and Their Use 有权
标题翻译：作为BACE抑制剂，组合物及其用途的伊马替西二酮二氧化物化合物
公开(公告)号：US20170037056A1
公开(公告)日：2017-02-09
申请号：US15104257
申请日：2014-12-16
申请人： Xing DAI , Jared N. CUMMING , Jack D. SCOTT , Hong LIU , Anandan PALANI , MERCK SHARP & DOHME CORP.
发明人： Xing Dai , Jared N. Cumming , Jack D. Scott , Hong Liu , Anandan Palani
IPC分类号： C07D513/04 , C07D471/04 , C07D285/36 , C07D417/12
CPC分类号： C07D513/04 , C07D285/36 , C07D417/12 , C07D471/04
摘要： In its many embodiments, the present invention provides certain iminothiadiazepane dioxide compounds, including compounds Formula (I): or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1A, R1B, R2, R3, R4, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
摘要翻译：或其互变异构体和所述化合物和所述互变异构体的药学上可接受的盐，其中RN，R1A，R1B，R2，R3，R4，环A，RA，m，-L1-和RL如本文所定义。本发明的新化合物可用作BACE抑制剂，并且可用于治疗和预防与其相关的各种病症。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括用于治疗阿尔茨海默氏病的药物组合物。

107. 发明申请

US20150246902A1 SUBSTITUED BENZOFURAN COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 有权
标题翻译：替代苯并呋喃化合物及其用于治疗病毒性疾病的方法
公开(公告)号：US20150246902A1
公开(公告)日：2015-09-03
申请号：US14343462
申请日：2012-08-16
申请人： Casey C. McComas , Nigel J. Liverton , Joerg Habermann , Uwe Koch , Frank Narjes , Peng Li , Xuanjia Peng , Richard Soll , Hao Wu , Anandan Palani , Xing Dai , Hong Liu , Shuwen He , Qun Dang
发明人： Casey C. McComas , Nigel J. Liverton , Joerg Habermann , Uwe Koch , Frank Narjes , Peng Li , Xuanjia Peng , Richard Soll , Hao Wu , Anandan Palani , Xing Dai , Hong Liu , Shuwen He , Qun Dang
IPC分类号： C07D405/04 , C07D473/00 , A61K31/52 , A61K45/06 , A61K31/437 , C07D487/04 , A61K31/4985 , A61K31/5025 , A61K31/4184 , C07D471/04
CPC分类号： C07D405/04 , A61K31/4045 , A61K31/416 , A61K31/4184 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/4985 , A61K31/5025 , A61K31/52 , A61K45/06 , C07D405/14 , C07D471/04 , C07D473/00 , C07D487/04 , C07D498/04 , Y02A50/387 , Y02A50/389 , Y02A50/395 , A61K2300/00
摘要： The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
摘要翻译：本发明涉及可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂，这种化合物的合成以及这些化合物用于抑制HCV NS5B聚合酶活性用于治疗或预防HCV感染的式（I）化合物并用于在基于细胞的系统中抑制HCV病毒复制和/或病毒生产。

108. 发明申请

US20140199263A1 HETEROCYCLIC-SUBSTITUTED BENZOFURAN DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 有权
标题翻译：杂环取代的苯唑嘌呤衍生物及其用于治疗病毒性疾病的方法
公开(公告)号：US20140199263A1
公开(公告)日：2014-07-17
申请号：US14343448
申请日：2012-08-16
申请人： Casey Cameron McComas , Nigel J. Liverton , Joerg Habermann , Uwe Koch , Frank Narjes , Peng Li , Xuanjia Peng , Richard Soll , Hao Wu , Anandan Palani , Xing Dai , Hong Liu , Shuwen He , Zhong Lai , Qun Dang , Nicolas Zorn
发明人： Casey Cameron McComas , Nigel J. Liverton , Joerg Habermann , Uwe Koch , Frank Narjes , Peng Li , Xuanjia Peng , Richard Soll , Hao Wu , Anandan Palani , Xing Dai , Hong Liu , Shuwen He , Zhong Lai , Qun Dang , Nicolas Zorn
IPC分类号： C07D513/04 , A61K31/497 , C07D405/14 , A61K31/4439 , C07D413/14 , A61K31/4245 , A61K31/444 , A61K31/506 , C07D498/04 , C07D417/14 , A61K31/5377 , A61K31/501 , A61K31/433 , C07D409/14 , A61K31/5365 , A61K31/5383 , C07F7/10 , A61K31/695 , A61K45/06 , C07D471/04
CPC分类号： A61K31/4245 , A61K31/433 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5365 , A61K31/5377 , A61K31/5383 , A61K31/695 , A61K45/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04 , C07D513/04 , C07F7/10 , Y02A50/385 , Y02A50/387 , Y02A50/389 , A61K31/424 , A61K2300/00
摘要： The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
摘要翻译：本发明涉及可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂，这种化合物的合成以及这些化合物用于抑制HCV NS5B聚合酶活性用于治疗或预防HCV感染的式（I）化合物并用于在基于细胞的系统中抑制HCV病毒复制和/或病毒生产。

109. 发明申请

US20110224187A1 PYRROLIDINE, PIPERIDINE AND PIPERAZINE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译：吡咯啉，哌啶和哌嗪衍生物及其使用方法
公开(公告)号：US20110224187A1
公开(公告)日：2011-09-15
申请号：US13124020
申请日：2009-10-14
申请人： Anandan Palani , Michael Y. Berlin , Aslanian G. Robert , Vaccaro M. Henry , Chan Tin-Yau , Xiao Dong , Degrado Sylvia , Rao U. Ashwin , Chen Xiao , Lee Yoon Joo , Sofolarides J. Michael , Shao Ning , Huang R. Ying , Liu Zhidan , Wang Li Yuan , Pu Haiyan
发明人： Anandan Palani , Michael Y. Berlin , Aslanian G. Robert , Vaccaro M. Henry , Chan Tin-Yau , Xiao Dong , Degrado Sylvia , Rao U. Ashwin , Chen Xiao , Lee Yoon Joo , Sofolarides J. Michael , Shao Ning , Huang R. Ying , Liu Zhidan , Wang Li Yuan , Pu Haiyan
IPC分类号： A61K31/438 , C07D417/04 , A61K31/496 , C07D487/04 , A61K31/4985 , C07D471/10 , A61K31/5377 , A61K31/454 , A61K31/541 , C07D417/14 , A61K31/4545 , A61P37/08 , A61P11/00 , A61P9/00 , A61P29/00 , A61P1/00 , A61P25/00 , A61P3/00 , A61P3/04 , A61P3/10 , A61P3/08
CPC分类号： C07D285/135 , C07D271/113 , C07D417/04 , C07D417/14 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/107
摘要： The present invention relates to novel Pyrrolidine, Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Pyrrolidine, Piperidine and Piperazine Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity, an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
摘要翻译：本发明涉及新颖的吡咯烷，哌啶和哌嗪衍生物，包含吡咯烷，哌啶和哌嗪衍生物的药物组合物以及这些化合物用于治疗或预防治疗过敏，使用过敏引起的气道反应，充血，心血管疾病，炎性疾病，胃肠道疾病，神经障碍，代谢障碍，肥胖症，肥胖相关病症，糖尿病，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。

110. 发明申请

US20080214575A1 PIPERIDINE DERIVATIVES USEFUL AS CCR5 ANTAGONISTS 失效
标题翻译：哌啶衍生物作为CCR5拮抗剂有用
公开(公告)号：US20080214575A1
公开(公告)日：2008-09-04
申请号：US12104914
申请日：2008-04-17
申请人： Anandan Palani , Michael W. Miller , Jack D. Scott
发明人： Anandan Palani , Michael W. Miller , Jack D. Scott
IPC分类号： A61K31/506 , C07D401/14 , A61P31/12
CPC分类号： C07D401/14
摘要： The present invention provides a compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R9, R10, A and B are as defined in the specification. The present invention also provides pharmaceutical compositions containing the compound of this invention, and methods of treatment using the compound of this invention. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.
摘要翻译：本发明提供下式的化合物或其药学上可接受的盐或溶剂化物，其中R 1，R 2，R 3，R 3， A，B和B如本说明书中所定义。本发明还提供含有本发明化合物的药物组合物和使用本发明化合物的治疗方法。本发明还涉及本发明化合物与一种或多种可用于治疗人类免疫缺陷病毒（HIV）的抗病毒剂或其它药剂的组合的用途。本发明还涉及本发明化合物单独或与另一种药剂组合用于治疗实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化。

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