公开(公告)号：US07384948B2

公开(公告)日：2008-06-10

申请号：US10628933

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.

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。

公开(公告)号：US07045636B2

公开(公告)日：2006-05-16

申请号：US10278468

申请日：2002-10-23

申请人： Anandan Palani ,  Sherry A. Shapiro ,  Mark D. McBriar ,  Jing Su

发明人： Anandan Palani ,  Sherry A. Shapiro ,  Mark D. McBriar ,  Jing Su

IPC分类号： C07D207/00 ,  C07D213/00 ,  A01N43/40 ,  A61K31/435

CPC分类号： C07D295/13 ,  A61K38/00 ,  C07C255/60 ,  C07C2601/02 ,  C07C2601/08 ,  C07D205/04 ,  C07D207/12 ,  C07D207/14 ,  C07D295/15 ,  C07K5/06026 ,  C07K5/06139 ,  C07K5/06191

摘要： The present invention discloses compounds, which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

公开(公告)号：US06689765B2

公开(公告)日：2004-02-10

申请号：US10061011

申请日：2002-01-30

申请人： Bahige M. Baroudy ,  John W. Clader ,  Hubert B. Josien ,  Stuart W. McCombie ,  Brian A. McKittrick ,  Michael W. Miller ,  Bernard R. Neustadt ,  Anandan Palani ,  Elizabeth M. Smith ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin ,  Eric Gilbert ,  Marc A. Labroli

发明人： Bahige M. Baroudy ,  John W. Clader ,  Hubert B. Josien ,  Stuart W. McCombie ,  Brian A. McKittrick ,  Michael W. Miller ,  Bernard R. Neustadt ,  Anandan Palani ,  Elizabeth M. Smith ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin ,  Eric Gilbert ,  Marc A. Labroli

IPC分类号： A61K31695

CPC分类号： C07D401/06 ,  A61K31/496 ,  A61K45/06 ,  C07D211/58 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D409/06 ,  C07D413/06 ,  A61K2300/00

摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v, host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.

摘要翻译： 使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基， 苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R 4，R 5，R 5和R 5独立地选自氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基， R 7为氢或烷基; R 6为氢，烷基或烯基;用于治疗HIV，实体器官移植排斥，移植物v，宿主病，关节炎，类风湿性关节炎，炎性肠病，特应性皮炎， 公开了牛皮癣，哮喘，过敏或多发性硬化，以及新化合物，包含它们的药物组合物，以及本发明的CCR5拮抗剂与用于治疗 可用于治疗炎性疾病的HIV或药物。

公开(公告)号：US20230285514A1

公开(公告)日：2023-09-14

申请号：US17785279

申请日：2020-12-18

申请人： Elisabetta BIANCHI ,  Paul E. CARRINGTON ,  Qiaolin DENG ,  Songnian LIN ,  Federica ORVIETO ,  Anandan PALANI ,  Antonello PESSI ,  Tomi K. SAWYER ,  Merck Sharp & Dohme LLC

发明人： Elisabetta Bianchi ,  Paul E. Carrington ,  Qiaolin Deng ,  Songnian Lin ,  Federica Orvieto ,  Anandan Palani ,  Antonello Pessi ,  Tomi K. Sawyer

IPC分类号： A61K38/26 ,  A61K38/28 ,  C07K14/605

CPC分类号： A61K38/26 ,  A61K38/28 ,  C07K14/605

摘要： The stapled peptides of the present invention, and pharmaceutically acceptable salts thereof, are co-agonists of the glucagon and GLP-1 receptors, and may be useful in the treatment, prevention and suppression of diseases mediated by the glucagon receptor and the GLP-1 receptor, including but not limited to, metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.

公开(公告)号：US09549917B2

公开(公告)日：2017-01-24

申请号：US14343448

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 ,  Zhong Lai ,  Qun Dang ,  Nicolas Zorn

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 ,  Zhong Lai ,  Qun Dang ,  Nicolas Zorn

IPC分类号： A61K45/06 ,  A61K31/506 ,  A61K31/444 ,  A61K31/443 ,  A61K31/497 ,  A61K31/501 ,  A61K31/695 ,  A61K31/424 ,  A61K31/4245 ,  A61K31/4439 ,  C07D405/14 ,  C07D413/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/433 ,  A61K31/5365 ,  A61K31/5377 ,  A61K31/5383 ,  C07F7/10

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。

公开(公告)号：US09290453B2

公开(公告)日：2016-03-22

申请号：US13996371

申请日：2011-12-19

申请人： Christopher W. Boyce ,  Salem Fevrier ,  Kevin D. McCormick ,  Anandan Palani ,  Robert G. Aslanian ,  Phieng Siliphaivanh ,  Joey L. Methot ,  William Colby Brown ,  Henry Vaccaro

发明人： Christopher W. Boyce ,  Salem Fevrier ,  Kevin D. McCormick ,  Anandan Palani ,  Robert G. Aslanian ,  Phieng Siliphaivanh ,  Joey L. Methot ,  William Colby Brown ,  Henry Vaccaro

IPC分类号： A61K31/47 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/4375 ,  C07D215/48 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D491/107 ,  C07D405/12 ,  A61K45/06

CPC分类号： C07D215/48 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/496 ,  A61K45/06 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D471/04 ,  C07D491/107

摘要： The invention provides certain quinolines and aza-quinolines of the Formula (I), and their pharmaceutically acceptable salts, wherein E, J1, Ja, Jb, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.

摘要翻译： 本发明提供了式（I）的某些喹啉和氮杂喹啉及其药学上可接受的盐，其中E，J1，Ja，Jb，R2，R3，R22，Ra，Rb，Rc，Rd，X，Y，b ，n和q如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗与不受控制或不适当刺激CRTH2功能相关的疾病或病症的方法。

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。

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.

公开(公告)号：US20080188485A1

公开(公告)日：2008-08-07

申请号：US12055900

申请日：2008-03-26

申请人： Bahige M. Baroudy ,  John W. Clader ,  Hubert B. Josien ,  Stuart W. McCombie ,  Brian A. McKittrick ,  Michael W. Miller ,  Bernard R. Neustadt ,  Anandan Palani ,  Elizabeth M. Smith ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin ,  Eric Gilbert ,  Marc A. Labroli

发明人： Bahige M. Baroudy ,  John W. Clader ,  Hubert B. Josien ,  Stuart W. McCombie ,  Brian A. McKittrick ,  Michael W. Miller ,  Bernard R. Neustadt ,  Anandan Palani ,  Elizabeth M. Smith ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin ,  Eric Gilbert ,  Marc A. Labroli

IPC分类号： A61K31/496 ,  A61P1/00 ,  A61P19/02

CPC分类号： C07D401/06 ,  A61K31/496 ,  A61K45/06 ,  C07D211/58 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D409/06 ,  C07D413/06 ,  A61K2300/00

摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroarylalkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.

摘要翻译： 使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，芴基，二苯甲基或任选取代的苯基或杂芳基烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R 4，R 5和R 7是氢或烷基; R 6是氢，烷基或链烯基; 公开了用于治疗HIV，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，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物 ，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

公开(公告)号：US07348328B2

公开(公告)日：2008-03-25

申请号：US10308782

申请日：2002-12-03

申请人： John W. Clader ,  Anandan Palani ,  Ruo Xu ,  Mark D. McBriar ,  Jing Su ,  Haiqun Tang

发明人： John W. Clader ,  Anandan Palani ,  Ruo Xu ,  Mark D. McBriar ,  Jing Su ,  Haiqun Tang

IPC分类号： A61K31/497 ,  C07D237/02 ,  C07D265/30

CPC分类号： C07D207/08 ,  C07C275/30 ,  C07C2601/14 ,  C07C2602/18 ,  C07C2602/20 ,  C07D205/04 ,  C07D207/06 ,  C07D207/10 ,  C07D207/12 ,  C07D207/14 ,  C07D209/52 ,  C07D211/26 ,  C07D211/34 ,  C07D211/96 ,  C07D213/75 ,  C07D213/89 ,  C07D233/24 ,  C07D295/13 ,  C07D333/36 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D413/06

摘要： The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

摘要翻译： 本发明公开了作为黑色素浓缩激素（MCH）的新型拮抗剂的化合物以及这些化合物的制备方法。 在另一个实施方案中，本发明公开了包含这样的MCH拮抗剂的药物组合物以及使用它们治疗肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。