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    • 1. 发明申请
    • N-SUBSTITUTED-2-OXODIHYDROPYRIDINE DERIVATIVES AS NPY ANTAGONISTS
    • N-取代的2-氧代二氢吡啶衍生物作为NPY拮抗剂
    • WO2004031175A3
    • 2005-02-24
    • PCT/JP0312290
    • 2003-09-25
    • BANYU PHARMA CO LTDSATO NAGAAKIANDO MAKOTOISHIKAWA SHIHONAGASE TSUYOSHINAGAI KEITAKANATANI AKIO
    • SATO NAGAAKIANDO MAKOTOISHIKAWA SHIHONAGASE TSUYOSHINAGAI KEITAKANATANI AKIO
    • A61P3/04C07D213/80C07D401/04C07D401/14A61K31/444
    • C07D213/80C07D401/04C07D401/14
    • A compound of the formula (I): (wherein Ar and Ar 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 and R 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 , R and R 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。
    • 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。