Piperidinyl piperidine derivatives useful as inhibitors of chemokine receptors
    1.
    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

    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。

    2'-Hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols,
methods for their manufacture, method for their use as antibacterial
agents, and compositions useful therefor
    5.
    发明授权
    2'-Hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols, methods for their manufacture, method for their use as antibacterial agents, and compositions useful therefor 失效
    2'-脱氧-2'-脱氨基-4,6-二-O-(氨基糖基)-1,3-二氨基环糊精,其制备方法,其用作抗菌剂的方法和可用于其的组合物

    公开(公告)号:US4212859A

    公开(公告)日:1980-07-15

    申请号:US912603

    申请日:1978-06-05

    CPC分类号: C07H15/234 Y02P20/55

    摘要: 2'-Hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols having a 6'-amino function exhibit antibacterial activity and are prepared by reaction of the corresponding N-protected (except the 2'-amino)-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitol with hydrogen peroxide in the presence of tungstate ion, followed by cleavage of the thereby formed 2'-oximino derivative, thence reduction of the resulting 2'-oxo derivative and removal of the N-protecting groups.Preferred compounds are 1-N-(.omega.-amino-.alpha.-hydroxyalkanoyl)-2'-hydroxy-2'-desamino-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols which exhibit antibacterial activity against bacteria resistant to the parent aminoglycoside.

    摘要翻译: 具有6'-氨基功能的2'-羟基-2'-脱氨基-4,6-二-O-(氨基糖基)-1,3-二氨基二醇具有抗菌活性,并通过相应的N-保护(除 2'-氨基)-4,6-二-O-(氨基糖基)-1,3-二氨基环糊精与过氧化氢在钨酸根离子存在下,然后裂解由此形成的2'-肟基衍生物,从而减少 得到的2'-氧代衍生物和N-保护基团的除去。 优选的化合物是对细菌具有抗菌活性的1-N-(ω-氨基-α-羟基烷酰基)-2'-羟基-2'-脱氨基-4,6-二-O-(氨基糖基)-1,3-二氨基二醇 对母体氨基糖苷类具有抗性。

    Piperidinyl piperazine derivatives useful as inhibitors of chemokine receptors
    9.
    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

    IPC分类号: A61K31/496 C07D403/14

    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。