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    Metabolites of tricyclic amides useful for inhibition of G-protein function and methods of treatment of proliferative diseases
    1.
    发明授权
    Metabolites of tricyclic amides useful for inhibition of G-protein function and methods of treatment of proliferative diseases 失效
    用于抑制G蛋白功能的三环酰胺的代谢物和治疗增殖性疾病的方法

    公开(公告)号：US07271174B2

    公开(公告)日：2007-09-18

    申请号：US10874556

    申请日：2004-06-23

    申请人： Swapan K. Chowdhury ,  Anima Ghosal ,  Robert M. Iannucci ,  Wenqing Feng ,  Tze-Ming Chan ,  Shmuel Zbaida ,  Kevin B. Alton ,  Ronald J. Doll ,  Keith P. Minor

    发明人： Swapan K. Chowdhury ,  Anima Ghosal ,  Robert M. Iannucci ,  Wenqing Feng ,  Tze-Ming Chan ,  Shmuel Zbaida ,  Kevin B. Alton ,  Ronald J. Doll ,  Keith P. Minor

    IPC分类号： C07D221/06 ,  A61K31/435

    CPC分类号： C07D401/14

    摘要： The present invention relates to metabolites of tricyclic amides, and structurally related compounds, represented by the structural formula (I): and pharmaceutically acceptable isomers, salts, solvates or esters of the compound of formula (I), wherein: R1 is selected from the group consisting of H and ═O; R2-R5 can be the same or different, each being independently selected from the group consisting of H, —OH, halide, —NH2 and ═O; and, the combination solid-dashed lines independently represent either single bonds or double bonds, wherein the number of combination solid-dashed lines that are double bonds is not greater than 2, and when, the double bonds are not adjacent, and when 0, one of R1-R5 is not H. Also disclosed are methods of treatment of proliferative diseases and methods for inhibiting the abnormal growth of cells, and for inhibiting farnesyl protein transferase using the novel compounds.

    摘要翻译： 本发明涉及由结构式（I）表示的三环酰胺的代谢物和结构相关的化合物：和式（I）化合物的药学上可接受的异构体，盐，溶剂化物或酯，其中：R 1 选自H和-O; R 2 -R 5可以相同或不同，各自独立地选自H，-OH，卤化物，-NH 2， SUB>和-O; 并且，组合虚线独立地表示单键或双键，其中双键的组合实线的数目不大于2，当双键不相邻时，当为0时， R 1〜R 5之一不是H.还公开了治疗增殖性疾病的方法和抑制细胞异常生长的方法，以及用于抑制法呢基蛋白转移酶 使用新型化合物。

    Piperidinyl piperazine derivatives useful as inhibitors of chemokine receptors
    3.
    发明申请
    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：US20060223821A1

    公开(公告)日：2006-10-05

    申请号：US11358520

    申请日：2006-02-21

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

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

    IPC分类号： A61K31/496 ,  C07D403/14

    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至R 8如本文所公开的CCR5受体的抑制剂 制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物，制备包含一种或多种这类化合物的药物制剂的方法，以及使用这种化合物治疗，预防，抑制或改善与CCR5相关的一种或多种疾病的方法 或药物组合物。 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。

    Piperidinyl piperidine derivatives useful as inhibitors of chemokine receptors
    4.
    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。

    Piperidinyl piperazine derivatives useful as inhibitors of chemokine receptors
    5.
    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
    6.
    发明申请
    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：US20060223856A1

    公开(公告)日：2006-10-05

    申请号：US11358248

    申请日：2006-02-21

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

    发明人： Tze-Ming Chan ,  Kathleen Cox ,  Wenqing Feng ,  Michael Miller ,  Daniel Weston ,  Stuart 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至R 8如本文所公开的CCR5受体的抑制剂 制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物，制备包含一种或多种这类化合物的药物制剂的方法，以及使用这种化合物治疗，预防，抑制或改善与CCR5相关的一种或多种疾病的方法 或药物组合物。 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。