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1.发明公开DERIVES D'AMINO-TROPANE, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 有权AMINOTROPANDERIVATE，其制备方法及其食疗
公开(公告)号：EP1773829A1
公开(公告)日：2007-04-18
申请号：EP05790816.2
申请日：2005-07-20
申请人： Sanofi-Aventis
CPC分类号： C07D451/04
摘要： The invention concerns amino-tropane derivatives of general formula (I), wherein: Ra R a' et R5 represent hydrogen atoms or alkyl groups; R1 represents a hydrogen atom or an alkyl, cycloalkyl, heterocycloalkyl or aryl group; R2 represents a group of formula -(CH2)x-(CO)y-Y or -(CO)y-(CH2)x-Y, wherein Y represents a hydrogen atom or a hydroxy, alkyl, cycloalkyl, alkoxy, aryl, heteroaryl group or NR11R12; R3 represents 1 to 3 groups selected among halogen atoms and alkyl, cycloalkyl OR, -NRR', -CO-NRR', -NR-CO-R', -NR-CO-NRR', -NR-COOR', -NO2, -CN and -COOR groups; R4 is selected among a group of formula (a), (b), (c) or (d): or a group of formula -A-R18, -A-CH=N-R19, -A-N(R20)-A'-R19, -A-CO-N(R2O)-A'-R19, -A-CH(NH2)-R19, -A-N(R20)-COO-A' or -(CH2)r-heteroaryl. The invention also concerns a method for preparing said derivatives and the therapeutic use thereof.
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2.发明公开DERIVES D'AMINO-PIPERIDINE, LEUR PREPARATION ET LEUR APPLICATION EN TANT QU'AGONISTES DES RECEPTEURS AUX MELANOCORTINES 审中-公开AMINOPIPERIDINDERIVATE，及其制备方法和用途作为黑皮素受体激动剂
公开(公告)号：EP1786809A2
公开(公告)日：2007-05-23
申请号：EP05790800.6
申请日：2005-07-20
申请人： Sanofi-Aventis
发明人： BRAUN, Alain , CORNET, Bruno , COURTEMANCHE, Gilles , CRESPIN, Olivier , FETT, Eykmar , PASCAL, Cécile
IPC分类号： C07D451/04 , C07D453/02 , A61K31/4468 , A61K31/439 , C07D401/12 , C07D405/12 , C07D401/14 , A61P15/10 , C07D211/58
CPC分类号： C07D211/58 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D451/04 , C07D453/02
摘要： The invention concerns aminopiperidine derivatives of general formula (I) wherein: Ra, Ra' and R5 represent hydrogen atoms or alkyl groups; R1 represent a hydrogen atom and an alkyl, cycloalkyl, heterocycloalkyl or aryl group; R2 represents a group of formula -(CH2)x-(CO)y-Y or -(CO)y-(CH2)x-Y, wherein Y represents a hydrogen atom or a hydroxy, alkyl, cycloalkyl, alkoxy, aryl, heteroaryl or NR 11R12 group, Y being other than a hydrogen atom when x = y = 0; R3 represents 1 to 3 groups selected among halogen atoms and alkyl, cycloalkyl, -OR, -NRR', -CO-NRR', -NR-CO-R', -NR-CO-NRR', -NR-COOR', -NO2, -CN and COOR groups; R4 is selected among groups of formula (a), (b) and (c), wherein p = 0, 1, 2 or 3, m = 0, 1 or 2; X represents an oxygen or sulphur atom or a -C(R 6)(R7)- or -N(R10)- member. The invention also concerns a method for preparing said derivatives and their therapeutic use as melanocortin receptor agonists for treating obesity, diabetes, sexual dysfunction.
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3.发明授权DERIVES D'AMINO-TROPANE, LEUR PREPARATION ET LEURS APPLICATIONS EN THERAPEUTIQUE 有权AMINOTROPANDERIVATE，其制备方法及其食疗
公开(公告)号：EP1773829B1
公开(公告)日：2008-12-17
申请号：EP05790816.2
申请日：2005-07-20
申请人： Sanofi-Aventis
CPC分类号： C07D451/04
摘要： The invention concerns amino-tropane derivatives of general formula (I), wherein: Ra R a' et R5 represent hydrogen atoms or alkyl groups; R1 represents a hydrogen atom or an alkyl, cycloalkyl, heterocycloalkyl or aryl group; R2 represents a group of formula -(CH2)x-(CO)y-Y or -(CO)y-(CH2)x-Y, wherein Y represents a hydrogen atom or a hydroxy, alkyl, cycloalkyl, alkoxy, aryl, heteroaryl group or NR11R12; R3 represents 1 to 3 groups selected among halogen atoms and alkyl, cycloalkyl OR, -NRR', -CO-NRR', -NR-CO-R', -NR-CO-NRR', -NR-COOR', -NO2, -CN and -COOR groups; R4 is selected among a group of formula (a), (b), (c) or (d): or a group of formula -A-R18, -A-CH=N-R19, -A-N(R20)-A'-R19, -A-CO-N(R2O)-A'-R19, -A-CH(NH2)-R19, -A-N(R20)-COO-A' or -(CH2)r-heteroaryl. The invention also concerns a method for preparing said derivatives and the therapeutic use thereof.
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