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    Piperidine derivatives useful as CCR5 antagonists
    3.
    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。

    Pegylated interferon alfa-CCR5 antagonist combination HIV therapy
    7.
    发明授权
    Pegylated interferon alfa-CCR5 antagonist combination HIV therapy 失效
    聚乙二醇化干扰素α-CCR5拮抗剂组合HIV治疗

    公开(公告)号：US06635646B1

    公开(公告)日：2003-10-21

    申请号：US09562729

    申请日：2000-05-01

    申请人： Mark A. Laughlin

    发明人： Mark A. Laughlin

    IPC分类号： A61K3150

    CPC分类号： A61K31/497 ,  A61K31/50

    摘要： Methods for treating treatment-naive as well as treatment-experienced adult and pediatric patients having HIV-1 infections as well as patients co-infected with HIV-1 and HCV involving administering a therapeutically effective amount of pegylated interferon-alfa, e.g., pegylated interferon alfa-2b, in association with a therapeutically effective amount of a CCR5 antagonist or preferably further in association with a therapeutically effective amount of at least one of ribavirin, IL-2, IL-12, pentafuside alone or in combination with a therapeutically effective amount of an anti-HIV-1 drug therapy, e.g., HAART are disclosed.

    摘要翻译： 治疗初治者以及具有HIV-1感染的治疗经验的成人和儿科患者以及共同感染HIV-1和HCV的患者的方法包括施用治疗有效量的聚乙二醇化干扰素-α，例如聚乙二醇化干扰素 α-2b与治疗有效量的CCR5拮抗剂相关联，或优选与治疗有效量的单独的或与治疗有效量的组合的病毒素，IL-2，IL-12，五 的抗HIV-1药物疗法，例如，HAART被公开。

    Pegylated interferon alfa-CCR5 antagonist combination HIV therapy
    8.
    发明授权
    Pegylated interferon alfa-CCR5 antagonist combination HIV therapy 失效
    聚乙二醇化干扰素α-CCR5拮抗剂组合HIV治疗

    公开(公告)号：US07247631B2

    公开(公告)日：2007-07-24

    申请号：US10430370

    申请日：2003-05-06

    申请人： Mark A. Laughlin

    发明人： Mark A. Laughlin

    IPC分类号： A61K31/50 ,  A61K31/501 ,  A61K31/497 ,  A01N43/40

    CPC分类号： A61K31/497 ,  A61K31/50

    摘要： Methods for treating treatment-naive as well as treatment-experienced adult and pediatric patients having HIV-1 infections as well as patients co-infected with HIV-1 and HCV involving administering a therapeutically effective amount of pegylated interferon-alfa, e.g., pegylated interferon alfa-2b, in association with a therapeutically effective amount of a CCR5 antagonist or preferably further in association with a therapeutically effective amount of at least one of ribavirin, IL-2, IL-12, pentafuside alone or in combination with a therapeutically effective amount of an anti-HIV-1 drug therapy, e.g., HAART are disclosed.

    摘要翻译： 治疗初治者以及具有HIV-1感染的治疗经验的成人和儿科患者以及共同感染HIV-1和HCV的患者的方法包括施用治疗有效量的聚乙二醇化干扰素-α，例如聚乙二醇化干扰素 α-2b与治疗有效量的CCR5拮抗剂相关联，或优选与治疗有效量的单独的或与治疗有效量的组合的病毒素，IL-2，IL-12，五 的抗HIV-1药物疗法，例如，HAART被公开。