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New tropane derivatives, useful to treat e.g. retrovirus infections, inflammatory diseases, multiple sclerosis, rheumatoid arthritis and graft rejection, are chemokine-5 receptor modulators
New tropane derivatives, useful to treat e.g. retrovirus infections, inflammatory diseases, multiple sclerosis, rheumatoid arthritis and graft rejection, are chemokine-5 receptor modulators
Tropane derivatives (I) are new. Tropane derivatives of formula (I) and their salts, solvates and derivatives are new. [Image] R 11-6C alkyl; and R 21-6C alkyl or 3-7C cycloalkyl (alkyl is optionally substituted by CF 3). Independent claims are included for: (1) preparation of (I); and (2) intermediates of formulae (II), (IV), (VI), (VII), (XVI), (XVII), (XVIII), (XX) and (XXIII). [Image] ACTIVITY : Anti-HIV; Virucide; Antiinflammatory; Neuroprotective; Antiarthritic; Antirheumatic; Immunosuppressive; Gastrointestinal-Gen.; Cytostatic; Gynecological; Antidiabetic; Nephrotropic; Respiratory-Gen.; Cardiant; Antipsoriatic; Cerebroprotective; Vasotropic; Anorectic; CNS-Gen.; Antiarteriosclerotic; Dermatological; Analgesic; Tranquilizer; Antimicrobial; Hepatotropic; Antibacterial. MECHANISM OF ACTION : Chemokine-5 (CCR-5) receptor modulator. (I) were tested for its chemokine-5 receptor modulatory activity in chinese hamster ovary cells using intracellular calcium mobilization assay. The results showed that the median inhibitory concentration of tert-butyl-3-endo-[(3-nitro-4-pyridinyl)amino]-8-azabicyclo[3.2.1]octane-8-carboxylate was 2.7 nM.
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机译：Tropane衍生物（I）是新的。式（I）的Tropane衍生物及其盐，溶剂化物和衍生物是新的。 [图像] R 1> 1-6C烷基; R 2＞ 1-6C烷基或3-7C环烷基（烷基任选地被CF 3取代）。包括以下方面的独立权利要求：（1）制备（I）; （2）式（II），（IV），（VI），（VII），（XVI），（XVII），（XVIII），（XX）和（XXIII）的中间体。活动：抗艾滋病毒;杀病毒剂;消炎（药;具有神经保护作用;抗关节炎抗风湿;免疫抑制胃肠源细胞抑制妇科抗糖尿病嗜肾呼吸器;卡迪恩对牛皮癣;脑保护变压性厌食的; CNS-Gen .;抗动脉硬化;皮肤;止痛药镇静剂;抗菌;肝抗菌。作用机理：趋化因子5（CCR-5）受体调节剂。 （I）使用细胞内钙动员试验测试了其在中国仓鼠卵巢细胞中的趋化因子5受体调节活性。结果表明，叔丁基-3-内基-[[（3-硝基-4-吡啶基）氨基] -8-氮杂双环[3.2.1]辛烷-8-羧酸盐的抑制浓度中值为2.7 nM。
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