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首页> 外国专利> New 3alpha-amino-5alpha-androstane derivatives are protein cyclin-dependent kinase 5/p25 interaction inhibitors useful to treat e.g. stroke, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis and diabetes

New 3alpha-amino-5alpha-androstane derivatives are protein cyclin-dependent kinase 5/p25 interaction inhibitors useful to treat e.g. stroke, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis and diabetes

机译：新的3α-氨基-5α-雄甾烷衍生物是蛋白质细胞周期蛋白依赖性激酶5 / p25相互作用抑制剂，可用于治疗例如糖尿病。中风，阿尔茨海默氏病，帕金森氏病，肌萎缩性侧索硬化症和糖尿病

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3alpha -Amino-5alpha -androstane derivatives (I) or their salts, racemates, and/or geometrical or optical isomers are new. 3alpha -Amino-5alpha -androstane derivatives of formula (I) or their salts, racemates, and/or geometrical or optical isomers are new. R 1-NH 2-NH-(R 3), -N(R 3) 2, -N +(R 3) 3, -NH-COR 3, -N(R 3)-CO-R 3, OH, =O, tetrazolyl or -O-CO-R 3, preferably NH 2; R 2CO-R 3, -CH 2-OH, -C(R3)=N-OH, -C(R 3)-N-NH-C(=NH)-NH 2, -C-(R 3)=N-NH 2, 1-8C-alkyl, -CH(OH)-R 3, =CH-R 3, -CH(R 3)-NH-R 3, OH, -CH-(R 3)-NH-CO-R 3, -CH(R 3)-N(R 3) 2, -CH(R 3)-NH 2, -CH(R 3)-N(R 3)-CO-R 3, -CH(R 3)-N +(R 3) 3, -CH(R 3)-NH-CO-R 3, oxazolonyl, H-(CH 2) n-P-(C 6H 5) 3, chain type polyalkylene glycol with a terminal group, such as -NH 2(which is capable of forming a bond on activated sepharose beads), or a biotinylated group; and R 31-3C-alkyl or H. ACTIVITY : CNS-Gen.; Cerebroprotective; Vasotropic; Neuroprotective; Nootropic; Antiparkinsonian; Analgesic; Cytostatic; Antidiabetic; Virucide. MECHANISM OF ACTION : Protein cyclin-dependent kinase 5/p25 interaction inhibitor. The ability of (I) to inhibit protein cyclin-dependent kinase 5/p25 interaction was tested using bioluminescence resonance energy transfer technique. The results showed that (3R,5S,8S,9S,10S,13S,14S)-10,13-dimethyl-hexadecahydro-cyclopenta[a]phenanthren-3-ylamine exhibited an IC 50value of 4 mu m.
机译：3α-氨基-5α-雄甾烷衍生物（I）或其盐，外消旋物和/或几何或光学异构体是新的。式（I）的3α-氨基-5α-雄甾烷衍生物或其盐，外消旋物和/或几何或光学异构体是新的。 R 1> -NH 2-NH-（R 3>），-N（R 3>）2，-N +>（R 3>）3，-NH-COR 3>，-N（R 3>）- CO-R 3>，OH，＝ O，四唑基或-O-CO-R 3>，优选NH 2; R 2> CO-R 3>，-CH 2 -OH，-C（R3）= N-OH，-C（R 3>）-N-NH-C（= NH）-NH 2，-C-（ R 3>）= N-NH 2，1-8C-烷基，-CH（OH）-R 3>，= CH-R 3>，-CH（R 3>）-NH-R 3>，OH，- CH-（R 3>）-NH-CO-R 3>，-CH（R 3>）-N（R 3>）2，-CH（R 3>）-NH 2，-CH（R 3>） -N（R 3>）-CO-R 3>，-CH（R 3>）-N +>（R 3>）3，-CH（R 3>）-NH-CO-R 3>，恶唑酮基， H-（CH 2）nP-（C 6H 5）3，具有端基的链型聚亚烷基二醇，例如-NH 2（能够在活化的琼脂糖珠上形成键）或生物素化基团;活性：CNS-Gen .;和R 3＞ 1-3C-烷基或H。脑保护变压性具有神经保护作用;促智;反帕金森病;止痛药细胞抑制抗糖尿病杀病毒剂。作用机理：蛋白细胞周期蛋白依赖性激酶5 / p25相互作用抑制剂。使用生物发光共振能量转移技术测试了（I）抑制蛋白质细胞周期蛋白依赖性激酶5 / p25相互作用的能力。结果表明，（3R，5S，8S，9S，10S，13S，14S）-10，13-二甲基-十六氢-环戊[a]菲基-3-基胺的IC 50值为4μm。

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