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    Piperidine derivatives useful as CCR5 antagonists
    5.
    发明授权
    Piperidine derivatives useful as CCR5 antagonists 有权
    哌啶衍生物可用作CCR5拮抗剂

    公开(公告)号：US06387930B1

    公开(公告)日：2002-05-14

    申请号：US09562815

    申请日：2000-05-01

    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 ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin

    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 ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin

    IPC分类号： C07D40104

    CPC分类号： C07D401/14 ,  C07D211/58 ,  C07D413/14 ,  C07D417/14

    摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein X is —C(R13)2—, —C(R13)(R19)—, —C(O)—, —O—, —NH—, —N(alkyl)—, R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is H, alkyl or alkenyl; R2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl; R3 is optionally substituted phenyl, heteroaryl or naphthyl; R4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, —CH2CH2OH, —CH2CH2—O-alkyl, —CH2C(O)—O-alkyl, —CH2C(O)NH2, —CH2C(O)—NHalkyl or —CH2C(O)—N(alkyl)2; R19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and R5, R13, R14, R15 and R16 are hydrogen or alkyl 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X是-C（R 13）2 - ， - C（R 13）（R 19） - ， - C（O） - ， - O - N（烷基） - ，R是任选取代的苯基，吡啶基，噻吩基或萘基; R1是H，烷基或烯基; R2是任选取代的苯基，苯基烷基，杂芳基或杂芳基烷基，萘基，芴基或二苯基甲基; R 3是任选取代的苯基， 杂芳基或萘基; R4是H，烷基，氟代烷基，环丙基甲基，-CH2CH2OH，-CH2CH2-O-烷基，-CH2C（O）-O-烷基，-CH2C（O）NH2，-CH2C（O） 或-CH 2 C（O）-N（烷基）2; R 19是任选取代的苯基，杂芳基或萘基，环烷基，环烷基烷基或烷氧基烷基; 和R 5，R 13，R 14，R 15和R 16是氢或烷基，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，炎性肠病，特应性皮炎，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。

    Piperidine derivatives useful as CCR5 antagonists
    6.
    发明授权
    Piperidine derivatives useful as CCR5 antagonists 有权
    哌啶衍生物可用作CCR5拮抗剂

    公开(公告)号：US06602885B2

    公开(公告)日：2003-08-05

    申请号：US10010481

    申请日：2001-11-08

    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 ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin

    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 ,  Ruo Steensma ,  Jayaram R. Tagat ,  Susan F. Vice ,  Mark A. Laughlin

    IPC分类号： A61K314545

    CPC分类号： C07D401/14 ,  C07D211/58 ,  C07D413/14 ,  C07D417/14

    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 H, alkyl or alkenyl; R2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl; R3 is optionally substituted phenyl, heteroaryl or naphthyl; R4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, —CH2CH2OH, —CH2CH2—O-alkyl, —CH2C(O)—O-alkyl, —CH2C(O)NH2, —CH2C(O)—NHalkyl or —CH2C(O)—N(alkyl)2; R19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and R5, R13, R14, R15 and R16 are hydrogen or alkyl 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H，烷基或烯基; R 2是任选取代的苯基，苯基烷基，杂芳基或杂芳基烷基，萘基，芴基或 二苯基甲基; R3是任选取代的苯基，杂芳基或萘基; R 4是H，烷基，氟代烷基，环丙基甲基，-CH 2 CH 2 OH，-CH 2 CH 2 -O-烷基，-CH 2 C（O）-O-烷基，-CH 2 C（O） ，-CH 2 C（O）-NH烷基或-CH 2 C（O）-N（烷基）2; R 19是任选取代的苯基，杂芳基或萘基，环烷基，环烷基烷基或烷氧基烷基; 和R 5，R 13，R 14，R 15和R 16是氢或烷基，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，炎性肠病，特应性皮炎，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。

    FUSED TRICYCLIC COMPOUNDS WITH ADENOSINE A2a RECEPTOR ANTAGONIST ACTIVITY
    8.
    发明申请
    FUSED TRICYCLIC COMPOUNDS WITH ADENOSINE A2a RECEPTOR ANTAGONIST ACTIVITY 有权
    具有腺苷A2a受体拮抗剂活性的融合三聚体化合物

    公开(公告)号：US20120232086A1

    公开(公告)日：2012-09-13

    申请号：US13510094

    申请日：2010-11-12

    申请人： Joel M. Harris ,  Bernard R. Neustadt ,  Andrew W. Stampford

    发明人： Joel M. Harris ,  Bernard R. Neustadt ,  Andrew W. Stampford

    IPC分类号： A61K31/4985 ,  A61K31/519 ,  A61P25/00 ,  C07D487/04 ,  A61P25/16 ,  A61P25/24

    CPC分类号： C07D487/04 ,  C07D471/14

    摘要： The present invention relates to certain fused tricyclic heteroaryl rings compounds of the Formula (I) (also referred to herein as the “Fused Tricyclic Compounds”), wherein M, Q, U, W, X, Y, Z, R1, R2, and R3, and rings C and D are as herein described. The present invention also provides compositions comprising at least one Fused Tricyclic Compound, and use of such compounds in the treatment of central nervous system diseases or disorders such as Parkinson's disease.

    摘要翻译： 本发明涉及式（I）（本文中也称为“熔融三环化合物”）的某些稠合三环杂芳基环化合物，其中M，Q，U，W，X，Y，Z，R 1，R 2， 和R 3，环C和D如本文所述。 本发明还提供了包含至少一种熔融三环化合物的组合物，以及这些化合物在治疗中枢神经系统疾病或障碍如帕金森病中的用途。