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    Piperidinyl piperazine derivatives useful as inhibitors of chemokine receptors
    1.
    发明授权
    Piperidinyl piperazine derivatives useful as inhibitors of chemokine receptors 失效
    可用作趋化因子受体抑制剂的哌啶基哌嗪衍生物

    公开(公告)号：US07659275B2

    公开(公告)日：2010-02-09

    申请号：US11358520

    申请日：2006-02-21

    申请人： Tze-Ming Chan ,  Kathleen Kox ,  Wenqing Feng ,  Michael W. Miller ,  Daniel Weston ,  Stuart W. McCombie

    发明人： Tze-Ming Chan ,  Kathleen Kox ,  Wenqing Feng ,  Michael W. Miller ,  Daniel Weston ,  Stuart W. McCombie

    IPC分类号： A61K31/497 ,  C07D401/00

    CPC分类号： C07D211/96 ,  C07D401/06 ,  C07D401/14

    摘要： In its many embodiments, the present invention provides a novel class of compounds of structural formula IA or IB where R1-R8 are as disclosed herein as inhibitors of the CCR5 receptors, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with CCR5 using such compounds or pharmaceutical compositions. 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： 在其许多实施方案中，本发明提供了一类新颖结构式IA或IB的化合物，其中R 1 -R 8如本文所公开的CCR5受体的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物， 制备包含一种或多种此类化合物的药物制剂的方法，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CCR5相关的一种或多种疾病的方法。 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。

    Piperidinyl piperidine derivatives useful as inhibitors of chemokine receptors
    2.
    发明授权
    Piperidinyl piperidine derivatives useful as inhibitors of chemokine receptors 失效
    可用作趋化因子受体抑制剂的哌啶基哌啶衍生物

    公开(公告)号：US07705019B2

    公开(公告)日：2010-04-27

    申请号：US11358248

    申请日：2006-02-21

    申请人： Tze-Ming Chan ,  Kathleen Cox ,  Wenqing Feng ,  Michael W. Miller ,  Daniel Weston ,  Stuart W. McCombie

    发明人： Tze-Ming Chan ,  Kathleen Cox ,  Wenqing Feng ,  Michael W. Miller ,  Daniel Weston ,  Stuart W. McCombie

    IPC分类号： A61K31/4545 ,  C07D403/14

    CPC分类号： C07D401/14

    摘要： In its many embodiments, the present invention provides a novel class of compounds of structural formula IA or IB where R1-R8 are as disclosed herein as inhibitors of the CCR5 receptors, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with CCR5 using such compounds or pharmaceutical compositions. 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： 在其许多实施方案中，本发明提供了一类新颖结构式IA或IB的化合物，其中R 1 -R 8如本文所公开的CCR5受体的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物， 制备包含一种或多种此类化合物的药物制剂的方法，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CCR5相关的一种或多种疾病的方法。 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。

    Piperidine derivatives useful as CCR5 antagonists
    4.
    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
    8.
    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。

    Muscarinic antagonists
    10.
    发明授权
    Muscarinic antagonists 有权
    毒蕈碱拮抗剂

    公开(公告)号：US06294554B1

    公开(公告)日：2001-09-25

    申请号：US09651652

    申请日：2000-08-30

    申请人： John W. Clader ,  Joseph A. Kozlowski ,  Stuart W. McCombie ,  Michael W. Miller ,  Susan F. Vice

    发明人： John W. Clader ,  Joseph A. Kozlowski ,  Stuart W. McCombie ,  Michael W. Miller ,  Susan F. Vice

    IPC分类号： A61K31445

    CPC分类号： C07D401/14 ,  C07D211/58 ,  C07D405/14

    摘要： Amide derivatives of 1,4 di-substituted piperidine compounds of the formula or a pharmaceutically acceptable salt, ester or solvate thereof, wherein Q and Q1 are each —CH═, or one of Q and Q1 is —CH═ and the other is —N═; X is —CH2— or Y and Z are —C(R5)═, or one of Y and Z is —C(R5)═ and the other is —N═; R1 is 1 to 3 substituents selected from H, halogen and alkoxy; R2 and R5 are 1 to 3 substituents selected from H, halogen, alkyl and alkoxy; and R3 and R4 are H or (C1-C6)alkyl are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed.

    摘要翻译： 式II的1,4-二取代哌啶化合物的酰胺衍生物或其药学上可接受的盐，酯或溶剂化物，其中Q和Q1各自为-CH =，或Q和Q1中的一个为-CH =，另一个为-N = ; X是-CH 2 - 或Y，Z是-C（R 5）=，或Y和Z之一是-C（R 5）=，另一个是-N =; R 1是1至3个选自H，卤素和 烷氧基; R2和R5是1至3个选自H，卤素，烷基和烷氧基的取代基; 和R 3和R 4是H或（C 1 -C 6）烷基是用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。 还公开了药物组合物和制备方法。