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    • 11. 发明授权
    • .alpha., .omega.-dicarboxylic acids and medicaments which contain these
compounds
    • α,ω-二羧酸和含有这些化合物的药物
    • US4711896A
    • 1987-12-08
    • US840563
    • 1986-02-21
    • Jacob Bar-TanaErnst-Christian WitteBernd HagenbruchJohannes PillKarlheinz Stegmeier
    • Jacob Bar-TanaErnst-Christian WitteBernd HagenbruchJohannes PillKarlheinz Stegmeier
    • C07C55/02A61K31/19A61P3/06A61P3/08C07C51/00C07C55/28C07C55/32C07C57/13C07C57/30C07C57/34C07C57/38C07C57/42C07C57/52C07C59/245C07C59/305C07C59/84C07C67/00C07C121/48C07C121/50
    • C07C57/42C07C55/28C07C55/32C07C57/13C07C57/34C07C57/38C07C59/245C07C59/305C07C59/84
    • ##STR1## α, ω-dicarboxylic acids having the general formula (I') in which: R
      1 and R
      2 , which may be different or the same, represent a lower alkyl group which can be substituted by hydroxy, lower alkoxy, halogen or phenyl, the phenyl being capable of substitution one or several times by hydroxy, lower alkoxy, lower alkyl or halogen; a lower alkenyl or alkinyl group; a C
      3 -C
      7 -cyclo-alkyl group or a phenyl group possibly substituted by hydroxy, halogen, lower alkyl or lower alkoxy, and X and Y, which may be different or the same, represent hydrogen, lower alkyl, lower alkoxy, hydroxy, cyano, halogen, carboxyl, lower alkoxycarbonyl or carbamoyl, and Q represents non-ramified, saturated or unsaturated alkyl chain with 8-14 C atoms, which can be substituted, interrupted by hetero-atoms, and form part of a cyclic system, as well as their carboxylic acid derivatives in vivo, provided that when Q represents an unramified, saturated alkyl chain with 8-14 C atoms, and R
      1 and R
      2 represent methyl and Y represents hydrogen, X may not represent hydrogen, ethoxy-carbonyl, bromine, cyano or methyl, and if R
      1 and R
      2 represent methyl and X and Y hydrogen, then Q may not represent any formula (II) group. Process for their preparation and medicines containing these compounds, which have an anti-diabetic action and lower the level of lipids.
    • PCT No.PCT / EP85 / 00288 Sec。 371日期1986年2月21日 102(e)日期1986年2月21日PCT归档1985年6月15日PCT公布。 公开号WO86 / 00298 日本1月16日,1986年1月16日,具有通式(I')的α,ω-二羧酸,其中:R1和R2可以不同或相同,表示 可被羟基,低级烷氧基,卤素或苯基取代的低级烷基,苯基能够被羟基,低级烷氧基,低级烷基或卤素取代一次或几次; 低级烯基或炔基; 可以被羟基,卤素,低级烷基或低级烷氧基取代的C 3 -C 7 - 环烷基或苯基,X和Y可以不同或相同,表示氢,低级烷基,低级烷氧基,羟基, 氰基,卤素,羧基,低级烷氧基羰基或氨基甲酰基,Q表示具有8-14个C原子的非分支,饱和或不饱和的烷基链,其可被取代,被杂原子间隔并形成环系的一部分,如 以及它们的体内羧酸衍生物,条件是当Q表示具有8-14个C原子的未饱和的饱和烷基链时,R 1和R 2表示甲基且Y表示氢,X可以不表示氢,乙氧羰基,溴, 氰基或甲基,并且如果R 1和R 2表示甲基且X和Y氢,则Q可以不表示任何式(II)基团。 其制备方法和含有这些化合物的药物,其具有抗糖尿病作用并降低脂质水平。
    • 14. 发明授权
    • 2H-1-benzopyran-2-one derivatives, processes for the preparation thereof
and pharmaceutical compositions containing them
    • 2H-1-苯并吡喃-2-酮衍生物,其制备方法和含有它们的药物组合物
    • US4670439A
    • 1987-06-02
    • US755496
    • 1985-07-16
    • Ernst-Christian WittePeter NeubertAndroniki Roesch
    • Ernst-Christian WittePeter NeubertAndroniki Roesch
    • A61K31/495A61P37/08C07D311/16C07D311/18C07D311/54C07D405/12
    • C07D311/18C07D311/16C07D311/54
    • The present invention provides 2H-1-benzopyran-2-one derivatives of the general formula: ##STR1## wherein either R.sub.1 is a lower alkyl radical, optionally substituted by phenyl, which can be substituted by lower alkyl, lower alkoxy, hydroxyl or halogen, and R.sub.2 is trifluoromethyl, cyano, hydroxymethyl, alkoxymethyl, acyloxymethyl, halogenomethyl, aminomethyl, mono- or dialkylaminomethyl, acyl, carboxyl, alkoxycarbonyl or carbamoyl, which can be mono- or disubstituted by lower alkyl; or R.sub.1 is trifluoromethyl, cyano, hydroxymethyl, alkoxymethyl, acyloxymethyl, halogenomethyl, aminomethyl, mono- or dialkylaminomethyl, acyl, carboxyl, alkoxycarbonyl or carbamoyl, which can be mono- or disubstituted by lower alkyl, and R.sub.2 is a lower alkyl radical, optionally substituted by phenyl, which can be substituted by lower alkyl, lower alkoxy, hydroxyl or halogen, and R.sub.3 is a phenyl or benzyl radical which can be substituted by lower alkyl, lower alkoxy, hydroxyl or halogen; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these 2H-1-benzopyran-2-one derivatives and pharmaceutical compositions containing them.
    • 本发明提供通式如下的1H-1-苯并吡喃-2-酮衍生物:其中R 1是任选被苯基取代的低级烷基,其可以被低级烷基,低级烷氧基, 羟基或卤素,R2是三氟甲基,氰基,羟甲基,烷氧基甲基,酰氧基甲基,卤代甲基,氨基甲基,一烷基氨基甲基或二烷基氨基甲基,酰基,羧基,烷氧基羰基或氨基甲酰基,其可以被低级烷基单取代或二取代; 或R 1是三氟甲基,氰基,羟甲基,烷氧基甲基,酰氧基甲基,卤代甲基,氨基甲基,一烷基氨基甲基或二烷基氨基甲基,酰基,羧基,烷氧基羰基或氨基甲酰基,其可以被低级烷基单或二取代,并且R 2是低级烷基, 被苯基取代,其可以被低级烷基,低级烷氧基,羟基或卤素取代,R3是可被低级烷基,低级烷氧基,羟基或卤素取代的苯基或苄基; 及其药理学上可接受的盐。 本发明还提供制备这些2H-1-苯并吡喃-2-酮衍生物的方法和含有它们的药物组合物。