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    • 9. 发明申请
    • 1,5-DIARYL-PYRROLE-3-CARBOXAMIDE DERIVATIVES AND THEIR USE AS CANNABINOID RECEPTOR MODULATORS
    • 1,5-二氨基-3-吡啶酰胺衍生物及其作为CANNABINOID受体调节剂的用途
    • WO2004058249A1
    • 2004-07-15
    • PCT/GB2003/005569
    • 2003-12-18
    • ASTRAZENECA ABASTRAZENECA UK LIMITEDBERGGREN, Anna, Ingrid, KristinaBOSTROM, Stig, JonasCHENG, LeifengELEBRING, Stig, ThomasGREASLEY, PeterNAGARD, MatsWILSTERMANN, Johan, MichaelTERRICABRAS, Emma
    • BERGGREN, Anna, Ingrid, KristinaBOSTROM, Stig, JonasCHENG, LeifengELEBRING, Stig, ThomasGREASLEY, PeterNAGARD, MatsWILSTERMANN, Johan, MichaelTERRICABRAS, Emma
    • A61K31/402
    • C07D401/04A61K31/402A61K31/4025A61K31/454C07D207/34C07D401/06
    • The present invention relates to a compound of formula (I) (A chemical formula should be inserted here - please see paper copy enclosed herewith) in which R 1 and R 2 independently represent phenyl, thienyl or pyridyl each of which is optionally substituted by one, two or three groups represented by Z; and R 3 is H, a C 1-3 alkyl group, a C 1-3 alkoxymethyl group, trifluoromethyl, a hydroxyC 1-3 alkyl group, an aminoC 1-3 alkyl group, C 1-3 alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C 1-3 alkylcarbamoyl, acetyl, or hydrazinocarbonyl of formula -CONHNR a R b wherein R a and R b are as defined for R 4 and R 5 respectively; X is CO or SO 2 ; Y is absent or represents NH optionally substituted by a C 1-3 alkyl group; R 4 and R 5 independently represent: a C 1-6 alkyl group; an (amino)C 1-4 alkyl- group in which the amino is optionally substituted by one or more C 1-3 alkyl groups; an optionally substituted non-aromatic C 3-15 carbocyclic group; a (C 3-12 cycloalkyl)C 1-3 alkyl- group; a group -(CH 2 ) r (phenyl ) s ; naphthyl; anthracenyl; a saturated 5 to 8 membered heterocyclic group containing one nitrogen and optionally one of the following: oxygen, sulphur or an additional nitrogen wherein the heterocyclic group is optionally substituted ;1-adamantylmethyl; a group - (CH 2 ) t Het where Het represents an aromatic heterocycle optionally substituted; or R 4 represents H and R 5 is as defined above; or R 4 and R 5 together with the nitrogen atom to which they are attached represent a saturated 5 to 8 membered heterocyclic group; R 6 is H, a C 1-3 alkyl group, a C 1-3 alkoxymethyl group, trifluoromethyl, a hydroxyC 1-3 alkyl group, C 1-3 alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C 1-3 alkylcarbamoyl, acetyl, or hydrazinocarbonyl of formula -CONHNR a R b ; with provisos; to processes for preparing such compounds, to their use in the treatment of obesity, psychiatric and neurological disorders particularly obesity, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    • 本发明涉及式(I)化合物(此处应插入化学式 - 请参见随附的纸质复制品),其中R 1和R 2独立地表示苯基,噻吩基或吡啶基,其各自为 任选被一个,两个或三个由Z表示的基团取代; R 3为H,C 1-3烷基,C 1-3烷氧基甲基,三氟甲基,羟基C 1-3烷基,氨基C 1-3烷基,C 1-3烷氧基羰基,羧基,氰基,氨基甲酰基,一或二C 1-3烷基氨基甲酰基 ,乙酰基或肼基羰基,其中R a和R b分别如R 4和R 5所定义; X是CO或SO2; Y不存在或表示任选被C 1-3烷基取代的NH; R 4和R 5独立地表示:C 1-6烷基; 氨基被一个或多个C 1-3烷基任选取代的(氨基)C 1-4烷基 - 基团; 任选取代的非芳族C 3-15碳环基团; (C3-12环烷基)C1-3烷基; 基团 - (CH 2)r(苯基)s; 萘; 蒽; 含有一个氮的饱和5至8元杂环基和任选的以下之一:氧,硫或另外的氮,其中杂环基任选被取代; 1-金刚烷基甲基; 基团 - (CH 2)t Het,其中Het表示任选取代的芳族杂环; 或R 4表示H且R 5如上所定义; 或R 4和R 5与它们所连接的氮原子一起表示饱和的5至8元杂环基; R 6是H,C 1-3烷基,C 1-3烷氧基甲基,三氟甲基,羟基C 1-3烷基,C 1-3烷氧基羰基,羧基,氰基,氨基甲酰基,一或二C 1-3烷基氨基甲酰基,乙酰基或肼基羰基 -CONHNR