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    3-ACYLINDOLES COMME AGONISTES DU RECEPTEUR CB2
    3.
    发明授权
    3-ACYLINDOLES COMME AGONISTES DU RECEPTEUR CB2 失效

    公开(公告)号：EP0833818B1

    公开(公告)日：2001-10-17

    申请号：EP96922962.4

    申请日：1996-06-20

    申请人： SANOFI-SYNTHELABO

    发明人： RINALDI, Murielle ,  BARTH, Francis ,  CASELLAS, Pierre ,  CONGY, Christian ,  OUSTRIC, Didier ,  BELL, Malcolm, R. ,  D'AMBRA, Thomas, E. ,  PHILION, Richard, E.

    IPC分类号： C07D209/12 ,  A61K31/40 ,  C07D209/16 ,  C07D498/06 ,  C07D471/06 ,  C07D209/08

    CPC分类号： A61K31/404 ,  A61K31/5355 ,  A61K31/538

    摘要： The use of human CB2 receptor-specific agonists of formula (I) or (I') for preparing immunomodulating drugs is disclosed. In formulae (I) and (I'), R1 is a group selected from -CH2CHR10NR6R11, -(CH2)2NR'6R'11, -CHR9CH2NR'6R'11, -(CH2)nZ and -COR8; R'1 is a -CH2CHR10NR6R11 or -(CH2)2NR'6R'11 group; R2 and R'2 are hydrogen, halogen or C1-4 alkyl; R3 is hydrogen, C1-4 alkyl or a group selected from -CH2CHR10NR6R11, -(CH2)2NR'6R'11 and -COR8; R'3 is a =CR6R8 group; R4 has one of the meanings given for R5 or is a -COR8 group; R5 is hydrogen, C1-4 alkyl, C1-4 alkoxy, a halogen atom, a CF3 group, an OCF3 group or C1-4 alkylthio; R'5 has one of the meanings given for R5 and is in the 5 or 6 position of the indene ring; R6 is hydrogen or C1-4 alkyl; R'6 is C1-4 alkyl; R7 has one of the meanings given for R5 or R7 and R9 together form a -Y-CH2- group attached to the indole ring in the 7 position by a group Y; R8 is phenyl substituted one to four times by a substituent selected from halogen, C1-4 alkyl or C1-4 alkoxy; a polycyclic ring selected from naphth-1-yl, naphth-2-yl, 1,2,3,4-tetrahydronaphth-1-yl, 1,2,3,4-tetrahydronaphth-5-yl, anthryl, benzofuryl, benzothien-2-yl, benzothien-3-yl, 2-, 3-, 4- or 8-quinolyl, said polycyclic rings optionally being substituted once or twice by a substituent selected from C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, halogen, cyano, hydroxyl, trifluoromethyl and imidazol-1-yl; R10 and R11 together are a group selected from -CH2-O-CH2-CR12R13- and -(CH2)p-CR12R13-, wherein the carbon atom substituted by R12 and R13 is attached to the nitrogen atom; R'11 is C1-4 alkyl; or R'11 and R'6, taken together with the nitrogen atom to which they are attached, form a group selected from morpholin-4-yl, thiomorpholin-4-yl, piperidin-1-yl and pyrolidin-1-yl; each of R12 and R13 is independently hydrogen or C1-4 alkyl; n is 2, 3, 4 or 5; p is 2 or 3; Z is a methyl group or a halogen atom; and Y is a methylene group or an oxygen atom.

    摘要翻译： 公开了式（I）或（I'）的人CB 2受体特异性激动剂用于制备免疫调节药物的用途。 在式（I）和（I'）中，R1是选自-CH2CHR10NR6R11， - （CH2）2NR'6R'11，-CHR9CH2NR'6R'11， - （CH2）nZ和-COR8的基团; R'1是-CH2CHR10NR6R11或 - （CH2）2NR'6R'11; R2和R'2是氢，卤素或C1-4烷基; R3是氢，C1-4烷基或选自-CH2CHR10NR6R11， - （CH2）2NR'6R'11和-COR8的基团; R'3是a = CR6R8基团; R4具有对R5给出的含义之一或是-COR8基团; R5是氢，C1-4烷基，C1-4烷氧基，卤原子，CF3基，OCF3基或C1-4烷硫基; R'5具有R5给出的含义之一并且在茚环的5或6位; R6是氢或C1-4烷基; R'6是C1-4烷基; R7具有R5给出的含义之一，或者R7和R9一起形成连接至吲哚环的-Y-CH2-基团在7位被基团Y连接; R8为被选自卤素，C1-4烷基或C1-4烷氧基的取代基取代1至4次的苯基; 选自萘-1-基，萘-2-基，1,2,3,4-四氢萘-1-基，1,2,3,4-四氢萘-5-基，蒽基，苯并呋喃基，苯并噻吩基的多环 苯并噻吩-3-基，2-，3-，4-或8-喹啉基，所述多环任选地被选自以下的取代基取代一次或两次：C 1-4烷基，C 1-4烷氧基， 烷硫基，卤素，氰基，羟基，三氟甲基和咪唑-1-基; R10和R11一起为选自-CH2-O-CH2-CR12R13-和 - （CH2）p-CR12R13-的基团，其中被R12和R13取代的碳原子与氮原子连接; R'11是C1-4烷基; 或R'11和R'6与它们所连接的氮原子一起形成选自吗啉-4-基，硫代吗啉-4-基，哌啶-1-基和吡咯烷-1-基的基团; R 12和R 13中的每一个独立地为氢或C 1-4烷基; n是2,3,4或5; p是2或3; Z是甲基或卤素原子; Y是亚甲基或氧原子。

    UTILISATION DE DERIVES DE LA TETRAHYDROPYRIDINE POUR LA PREPARATION DE MEDICAMENTS POUR LE TRAITEMENT DES MALADIES ENTRAINANT UNE DEMYELINISATION
    10.
    发明授权
    UTILISATION DE DERIVES DE LA TETRAHYDROPYRIDINE POUR LA PREPARATION DE MEDICAMENTS POUR LE TRAITEMENT DES MALADIES ENTRAINANT UNE DEMYELINISATION 失效
    TETRAHYDROPYRIDINDERIVATEN的药物来治疗疾病脱髓鞘的生产中使用

    公开(公告)号：EP0979079B1

    公开(公告)日：2004-06-16

    申请号：EP98921552.0

    申请日：1998-04-17

    申请人： SANOFI-SYNTHELABO

    发明人： BOURRIE, Bernard ,  CASELLAS, Pierre ,  MAFFRAND, Jean-Pierre

    IPC分类号： A61K31/44

    CPC分类号： A61K31/444 ,  A61K31/4418

    摘要： The invention concerns the use of tetrahydropyridine derivatives of formula (I) in which: R1 represents a halogen or a CF3, (C1-C4) alkyl or (C1-C4)alkoxy group; Y represents a nitrogen atom or a CH group; Z' and Z" represent each hydrogen or a (C1-C3) alkyl group, or one represents hydrogen and the other a hydroxy group, or both together represent an oxo group; Z represents a phenyl radical; a phenyl radical monosubstituted by a substituent X, X being (a) a (C1-C6)alkyl, (C1-C6)alkoxy (C3-C7)carboxyalkyl, (C1-C4)alkoxycarbonyl(C1-C6)alkyl, (C3-C7)carboxyalkoxy or (C1-C4)-alkoxycarbonyl(C1-C6) alkoxy group; (b) a group selected among a (C3-C7)cycloalkyl, (C3-C7)cycloalkoxy, (C3-C7)cycloalkylmethyl, (C3-C7)cycloalkylamino and cyclohexenyl group, said group capable of being substituted by a halogen, hydroxy, (C1-C4)alkoxy, carboxy, (C1-C4)alkoxycarbonyl, amino, mono- or di-(C1-C4)alkylamino; or (c) a group selected among a phenyl, phenoxy, phenylamino, N-(C1-C3)alkylphenylamino, phenylmethyl, phenylethyl, phenylcarbonyl, phenylthio, phenylsulphonyl, phenylsulphinyl or styryl group, said group can be mono- or polysubstituted on the phenyl group by a halogen, CF3, (C1-C4)alkyl, (C1-C4)alkoxy, cyano, amino, mono- or di-(C1-C4)alkylamino, (C1-C4)acylamino, carboxy, (C1-C4)alkoxycarbonyl, aminocarbonyl, mono- or di-(C1-C4)alkylaminocarbonyl, amino(C1-C4)alkyl hydroxy(C1-C4)alkyl or halogeno(C1-C4)alkyl; a phenyl radical disubstituted by a substituent R2, R2 being a halogen or a hydroxy, methyl, ethyl, (C3-C6)alkyl, (C1-C4)alkoxy or trifuoromethyl group and by a substituent X, X being as defined above; a 1-naphthyl or 2-naphthyl radical; a 1-naphthyl or 2-naphthyl radical, substituted in positions 5, 6, 7 and/or 8 by one or two hydroxyl groups, one or two (C1-C4) alkoxy groups, or a 6,7-methylenedioxy group; or Z" is hydrogen and Z and Z' represent, each independently, a phenyl group non-substituted or mono-, di- or trisubstituted; or one of its pharmaceutically acceptable salts or solvates, for preparing pharmaceutical compositions to fight against diseases causing demyelination.