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农业专利-农业专业知识服务系统

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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

专利权人:: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE - CNRS -;CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE - CNRS -

发明人:: BACH STEPHANE,STEPHANE BACH,COUTURIER CYRIL,CYRIL COUTURIER,CORBEL CAROLINE,CAROLINE CORBEL,GUERITTE FRANCOISE,FRANCOISE GUERITTE,ZHU WANG QIAN,QIAN ZHU WANG,BOUSSEROUEL HADJIRA,HADJIRA BOUSSEROUEL

申请号：: FR1004627

公开号：: FR2967914A1

申请日:: 2010.11.29

申请国别(地区):: FR

年份:: 2012

代理人:

摘要：: 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 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-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 3>；1-3C-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.L'invention concerne des dérivés d'androstane pour une utilisation pour le traitement de troubles du système nerveux central par inhibition des interactions entre les protéines CDK5 et p25, ces dérivés répondant à la formule (I), dans laquelle R1 = - NH - NH-(R3)； -N(R3) ou -N (R3) ； -NH-CO-R3 ； - N(R3)- CO-R3 ； -OH ； = O ； tetrazolyle ； -O-CO-R3 ； R2 représente - CO-R3； - CH -OH ； -C(R3) =N-OH ； -C(R3) = N - NH -C (=NH)- NH ； -C - (R3)= N-NH ； alkyle en C1-C8； - CH(OH)-R3； =CH-R3； - CH(R3) -NH-R