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    CB.sub.2 Receptor agonist compounds
    1.
    发明授权
    CB.sub.2 Receptor agonist compounds 失效

    公开(公告)号：US6013648A

    公开(公告)日：2000-01-11

    申请号：US995902

    申请日：1997-12-22

    申请人： Murielle Rinaldi ,  Francis Barth ,  Pierre Casellas ,  Christian Congy ,  Didier Oustric ,  Malcolm R. Bell ,  Thomas E. D'Ambra ,  Richard E. Philion

    发明人： Murielle Rinaldi ,  Francis Barth ,  Pierre Casellas ,  Christian Congy ,  Didier Oustric ,  Malcolm R. Bell ,  Thomas E. D'Ambra ,  Richard E. Philion

    IPC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 ,  A61K31/405

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

    摘要： The use of human CB.sub.2 receptor-specific agonists of formula (I) or (I') for preparing immunomodulating drugs is disclosed. In formulae (I) and (I'), R.sub.1 is a group selected from --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11, --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11, --CHR.sub.9 CH.sub.2 NR'.sub.6 R'.sub.11, --(CH.sub.2).sub.n Z and --COR.sub.8 ; R'.sub.1 is a --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11 or --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11 group; R.sub.2 and R'.sub.2 are hydrogen, halogen or C.sub.1-4 alkyl; R.sub.3 is hydrogen, C.sub.1-4 alkyl or a group selected from --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11, --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11 and --COR.sub.8 ; R'.sub.3 is a .dbd.CR.sub.6 R.sub.8 group; R.sub.4 has one of the meanings given for R.sub.5 or is a --COR.sub.8 group; R.sub.5 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, a halogen atom, a CF.sub.3 group, an OCF.sub.3 group or C.sub.1-4 alkylthio; R'.sub.5 has one of the meanings given for R.sub.5 and is in the 5 or 6 position of the indene ring; R.sub.6 is hydrogen or C.sub.1-4 alkyl; R'.sub.6 is C.sub.1-4 alkyl; R.sub.7 has one of the meanings given for R.sub.5 or R.sub.7 and R.sub.9 together form a --Y--CH.sub.2 -- group attached to the indole ring in the 7 position by a group Y; R.sub.8 is phenyl substituted one to four times by a substituent selected from halogen, C.sub.1-4 alkyl or C.sub.1-4 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 C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen, cyano, hydroxyl, trifluoromethyl and imidazol-1-yl; R.sub.10 and R.sub.11 together are a group selected from --CH.sub.2 --O--CH.sub.2 --CR.sub.12 R.sub.13 -- and --(CH.sub.2).sub.p --CR.sub.12 R.sub.13 --, wherein the carbon atom substituted by R.sub.12 and R.sub.13 is attached to the nitrogen atom; R'.sub.11 is C.sub.1-4 alkyl; or R'.sub.11 and R'.sub.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 pyrrolidin-1-yl; each of R.sub.12 and R.sub.13 is independently hydrogen or C.sub.1-4 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.