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    • 2. 发明申请
    • N-SUBSTITUTE-2-OXODIHYDROPYRIDINE DERIVATES
    • N-取代-2-氧代二氢吡啶衍生物
    • WO2004031175A2
    • 2004-04-15
    • PCT/JP2003/012290
    • 2003-09-25
    • BANYU PHARMACEUTICAL CO., LTD.SATO, NagaakiANDO, MakotoISHIKAWA, ShihoNAGASE, TsuyoshiNAGAI, KeitaKANATANI, Akio
    • SATO, NagaakiANDO, MakotoISHIKAWA, ShihoNAGASE, TsuyoshiNAGAI, KeitaKANATANI, Akio
    • C07D401/14
    • C07D213/80C07D401/04C07D401/14
    • A compound of the formula (I): (wherein Ar 1l and Ar 2 are independently aryl or heteroaryl, any of which is optionally substituted by a substituent selected from the group consisting of cyano, halogen, nitro, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl) -lower alkyl, lower alkenyl, lower alkylamino, di-lower alkylamino, lower alkanoylamino, lower alkylsulfonylamino, arylsulfonylamino, hydroxy, lower alkoxy, halo-lower alkoxy, aryloxy, heteroaryloxy, lower alkylthio, carboxyl, formyl, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, di-lower alkylcarbamoyl, lower alkylsulfonyl, arylsulfonyl, aryl and heteroaryl; R 1 and R 2 are independently lower alkyl, cyclo-lower alkyl, cyclo(lower alkyl)-lower alkyl or lower alkoxy, any of which is optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di-lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, f ormyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl; R 1 , R 4 and R 5 are independently hydrogen, cyano, halogen hydroxy, or lower alkyl, lower alkoxy or lower alkylthio, the last three groups being optionally substituted by a substituent selected from the group consisting of halogen, lower alkylamino, di -lower alkylamino, lower alkanoylamino, hydroxy, lower alkoxy, formyl, lower alkoxycarbonyl, lower alkylcarbamoyl and di-lower alkylcarbamoyl), or a salt or ester thereof is useful as a neuropeptide Y receptor antagonist agent and is also useful as an agent for the treatment of bulimia, obesity or diabetes.
    • 式(I)的化合物:其中Ar 11和Ar 2独立地为芳基或杂芳基,其中任何一个任选被选自氰基,卤素,硝基,低级烷基, 卤代低级烷基,羟基 - 低级烷基,环 - 低级烷基,环(低级烷基) - 低级烷基,低级烯基,低级烷基氨基,二低级烷基氨基,低级烷酰基氨基,低级烷基磺酰基氨基,芳基磺酰基氨基,羟基,低级烷氧基, 低级烷氧基,芳氧基,杂芳氧基,低级烷硫基,羧基,甲酰基,低级烷酰基,低级烷氧基羰基,氨基甲酰基,低级烷基氨基甲酰基,二低级烷基氨基甲酰基,低级烷基磺酰基,芳基磺酰基,芳基和杂芳基; R 1和R 2独立地为 低级烷基,环 - 低级烷基,环(低级烷基) - 低级烷基或低级烷氧基,其中任何一个任选被选自卤素,低级烷基氨基,二低级烷基氨基,低级烷酰氨基,羟基, 低级烷氧基,芳基,低级 低级烷基氨基甲酰基和二低级烷基氨基甲酰基; R 1,R 4和R 5独立地是氢,氰基,卤素羟基或低级烷基,低级烷氧基或低级烷硫基,最后三个基团任选被选自以下的取代基取代:卤素 低级烷基氨基,二低级烷基氨基,低级烷酰基氨基,羟基,低级烷氧基,甲酰基,低级烷氧基羰基,低级烷基氨基甲酰基和二低级烷基氨基甲酰基)或其盐或酯可用作神经肽Y受体拮抗剂,也可用 作为治疗贪食症,肥胖症或糖尿病的药物。
    • 5. 发明公开
    • PYRIDONE COMPOUND
    • 吡啶酮化合物
    • EP1916239A1
    • 2008-04-30
    • EP06782591.9
    • 2006-08-03
    • BANYU PHARMACEUTICAL CO., LTD.
    • ANDO, MakotoSEKINO, EtsukoHAGA, YujiOTAKE, NorikazuMORIYA, Minoru
    • C07D213/64A61P1/16
    • C07D213/69C07D213/64C07D213/89C07D239/52C07D401/10C07D401/14C07D405/10C07D487/08
    • An active ingredient is a compound represented by the general formula [I]:

      [wherein R 1 and R 2 represent a lower alkyl group, a C 3-6 cycloalkyl group or the like, X 1 and X 2 represent methine, an Ar-Y 1 -Y 2 -Y 3 -substituted methine or the like, however either of them is an Ar-Y 1 -Y 2 -Y 3 -substituted methine, X 3 to X 8 represent methine, -N- or the like, Y 1 and Y 3 represent a single bond, -O- or the like, Y 2 represent a single bond, a lower alkylene group or the like, W represent -(O)-(CH 2 )n-(O)- or the like, n represents an integer of 1 to 4, L and Z 2 represent a single bond or a methylene group, Z 1 represents a single bond, a C 1-4 alkylene group or the like, and Ar represents an aromatic carbocyclic group or the like]. The compound acts as a melanin-concentrating hormone receptor antagonist and useful as a therapeutic agent for obesity or the like.
    • 活性成分是由通式[I]表示的化合物:[其中R1和R2代表低级烷基,C3-6环烷基等,X1和X2代表次甲基,Ar-Y1-Y2-Y3 取代的次甲基等,然而它们中的任一个都是Ar-Y1-Y2-Y3-取代的次甲基,X3至X8代表次甲基,N-等,Y1和Y3代表单键,-O-或 Y 2表示单键,低级亚烷基等,W表示 - (O) - (CH 2)n - (O) - 等,n表示1至4的整数,L和Z 2表示 单键或亚甲基,Z 1表示单键,C 1-4亚烷基等,Ar表示芳香族碳环基等]。 该化合物作为黑色素浓缩激素受体拮抗剂发挥作用,可用作肥胖症等的治疗剂。