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    • 8. 发明公开
    • Novel piperidine derivatives and pharmaceutical compositions containing same
    • 新型哌啶衍生物和含有其的药物组合物
    • EP0092391A3
    • 1984-09-26
    • EP83302123
    • 1983-04-14
    • KYOWA HAKKO KOGYO CO., LTD
    • Teranishi, MasayukiObase, HiroyukiNomoto, YujiShuto, KatsuichiKarasawa, AkiraKasuya, Yutaka
    • C07D401/06C07D401/04A61K31/445C07D211/58C07D211/26
    • C07D401/04C07D211/26C07D211/58C07D401/06
    • Novel piperidine derivatives are disclosed having hypotensive activity, as well as pharmaceutical preparations containing them. The novel compounds are of the formula
      wherein A is a hydroxyl group, a halogen atom, a C,-C 5 alkyl group, a C 1 -C 5 alkoxy group, a C 2 -C 5 alkenyloxy group, a C 1 -C 5 alkinyloxy group, a C 1 -C 5 alkylthio group, a carboxyl group, a C 1 -C 5 alkoxycarbonyl group, a nitro group, an amino group, a C 1 -C 5 alkylamino group, a C,-C 5 alkanoylamino group, a sulfamoyl group, a mono- or di- (C 1 -C 5 alkyl) aminosulfonyl group, a C 1 -C 5 alkylsulfonyl group, a carbamoyl group, a cyano group or a trifluoromethyl group; when m is 2 or more, A may be the same or different groups, or two A groups may combine to form a C,-C 5 alkylenedioxy group; m is 0 or an integer of 1-5; Q is a carbonyl group or a hydroxymethylene group; R is a hydrogen atom or an alkyl group having 1-4 carbon atoms; X and Y are defined as follows: i) when Y = H, X represents
      ii) when Y = CH 3 , X represents
      and when
      X represents a hydrogen atom and their pharmacologically acceptable acid addition salts.
    • 公开了具有降血压活性的新型哌啶衍生物,以及含有它们的药物制剂。 该新化合物具有式CHEM,其中A为羟基,卤原子,C1-C5烷基,C1-C5烷氧基,C7-C5链烯氧基,C1-C5烷氧基, C1-C5烷硫基,羧基,C1-C5烷氧基羰基,硝基,氨基,C1-C5烷基氨基,C1-C5烷酰基氨基,氨磺酰基,一或二( C1-C5烷基)氨基磺酰基,C1-C5烷基磺酰基,氨基甲酰基,氰基或三氟甲基; 当m为2以上时,A可以相同或不同,或两个A基团可以结合形成C1-C5亚烷基二氧基; m为0或1-5的整数; Q是羰基或羟基亚甲基; R是氢原子或具有1-4个碳原子的醇酸基; X和Y定义如下:i)当Y = H时,X表示 ii)当Y = CH 3时,X表示,当Y = CHEM时,X表示氢原子及其药理学上可接受的酸加成盐 。