发明名称 The use of human Cb2 receptor agonists for preparing immunomodulating compounds
摘要 <p>The use of human CB2 receptor-specific agonists of formula (I) or (I') in the prepartion of medicaments for controlling immunomodulation. R1 is selected from -CH2CHR10NR6R11, -(CH2)2NR'6R'11, -CHR9CH2NR'6R'11, -(CH2)nZ and -COR8; R'1 is a -CH2CHR10NR6R11 or -(CH2)2NR'6R'11; 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 =CR6R8; R4 is R5 or -COR8; R5 is hydrogen, C1-4 alkyl, C1-4 alkoxy, a halogen atom, a CF3 group, an OCF3 group or C1-4 alkylthio; R'5 is 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 is 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.</p>
申请公布号 NZ312161(A) 申请公布日期 2000.08.25
申请号 NZ19960312161 申请日期 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
分类号 C07D295/08;A61K31/135;A61K31/40;A61K31/403;A61K31/404;A61K31/435;A61K31/47;A61K31/535;A61K31/5355;A61K31/5375;A61K31/538;A61K45/00;A61P29/00;A61P37/00;A61P37/02;A61P37/08;A61P43/00;C07D209/08;C07D209/12;C07D209/14;C07D209/16;C07D413/06;C07D471/04;C07D471/06;C07D487/06;C07D491/06;C07D498/06;(IPC1-7):A61K31/40 主分类号 C07D295/08
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