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    Piperazine-substituted aryl and aralkyl carboxylic acids useful for treating infirmaties caused by excess lipids or thrombocyte
    2.
    发明授权
    Piperazine-substituted aryl and aralkyl carboxylic acids useful for treating infirmaties caused by excess lipids or thrombocyte 失效
    哌嗪取代的芳基和芳烷基羧酸，可用于治疗由过量脂质或血小板细胞引起的体温

    公开(公告)号：US4616086A

    公开(公告)日：1986-10-07

    申请号：US657032

    申请日：1984-10-01

    申请人： Ernst-Christian Witte ,  Hans P. Wolff ,  Bernd Hagenbruch ,  Karlheinz Stegmeir ,  Johannes Pill

    发明人： Ernst-Christian Witte ,  Hans P. Wolff ,  Bernd Hagenbruch ,  Karlheinz Stegmeir ,  Johannes Pill

    IPC分类号： C07D295/02 ,  A61K31/495 ,  A61P7/00 ,  C07D295/06 ,  C07D295/08 ,  C07D295/096 ,  C07D295/112 ,  C07D295/14 ,  C07D295/15 ,  C07D295/155 ,  C07D295/185 ,  C07D295/192 ,  C07D295/194 ,  C07D295/20 ,  C07D295/205 ,  C07D295/26 ,  C07D241/04

    CPC分类号： C07D295/185 ,  C07D295/096 ,  C07D295/112 ,  C07D295/15 ,  C07D295/155 ,  C07D295/192 ,  C07D295/194 ,  C07D295/205 ,  C07D295/26

    摘要： The present invention is concerned with new carboxylic acid derivatives, with processes for the preparation thereof and with pharmaceutical compositions for lipid depression and thrombocyte aggregation, containing them, and to methods for treating infirmaties caused by excess lipids or thrombocyte aggregation.The new carboxylic acid derivatives according to the present invention are compounds of the general formula: ##STR1## wherein A is a valency bond or a lower alkylene chain, B is a valency bond or a saturated or unsaturated lower alkylene chain, R is hydrogen, an alkyl group which can be substituted by hydroxyl, carboxyl, sulphonic acid or optionally substituted phenoxy group, or R is an aralkyl radical, the aryl moiety of which can be substituted and the alkyl moiety of which is optionally unsaturated and can contain up to 4 carbon atoms, or R is a phenacyl radical, the phenyl moiety optionally substituted, or R is an acyl radical derived from aliphatic, araliphatic or aromatic carboxylic or sulphonic acid, or R is an aryl radical optionally substituted with the proviso that when A is a valency bond, R cannot be hydrogen, methyl, ethyl, hydroxyethyl, benzyl or phenyl, and the physiologically acceptable salts, esters and amides thereof.

    摘要翻译： 本发明涉及新的羧酸衍生物，其制备方法和含有它们的脂质抑制和血小板聚集的药物组合物，以及用于治疗由过量脂质或凝血细胞聚集引起的不孕症的方法。 根据本发明的新的羧酸衍生物是下列通式的化合物：其中A是价键或低级亚烷基链，B是价键或饱和或不饱和的低级亚烷基链，R 是氢，可以被羟基，羧基，磺酸或任选取代的苯氧基取代的烷基，或R是芳烷基，其芳基部分可以被取代，并且其烷基部分任选是不饱和的并且可以含有 最多4个碳原子，或R是苯甲酰基，苯基部分任选被取代，或R是衍生自脂族，芳脂族或芳族羧酸或磺酸的酰基，或R是任选被取代的芳基，条件是当 A是价键，R不能是氢，甲基，乙基，羟乙基，苄基或苯基，以及它们的生理上可接受的盐，酯和酰胺。

    .alpha., .omega.-dicarboxylic acids and medicaments which contain these compounds
    3.
    发明授权
    .alpha., .omega.-dicarboxylic acids and medicaments which contain these compounds 失效
    α，ω-二羧酸和含有这些化合物的药物

    公开(公告)号：US4711896A

    公开(公告)日：1987-12-08

    申请号：US840563

    申请日：1986-02-21

    申请人： Jacob Bar-Tana ,  Ernst-Christian Witte ,  Bernd Hagenbruch ,  Johannes Pill ,  Karlheinz Stegmeier

    发明人： Jacob Bar-Tana ,  Ernst-Christian Witte ,  Bernd Hagenbruch ,  Johannes Pill ,  Karlheinz Stegmeier

    IPC分类号： C07C55/02 ,  A61K31/19 ,  A61P3/06 ,  A61P3/08 ,  C07C51/00 ,  C07C55/28 ,  C07C55/32 ,  C07C57/13 ,  C07C57/30 ,  C07C57/34 ,  C07C57/38 ,  C07C57/42 ,  C07C57/52 ,  C07C59/245 ,  C07C59/305 ,  C07C59/84 ,  C07C67/00 ,  C07C121/48 ,  C07C121/50

    CPC分类号： C07C57/42 ,  C07C55/28 ,  C07C55/32 ,  C07C57/13 ,  C07C57/34 ,  C07C57/38 ,  C07C59/245 ,  C07C59/305 ,  C07C59/84

    摘要： ##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.

    摘要翻译： 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。

    Carboxylic acid derivatives, processes for the preparation thereof and pharmaceutical compositions containing them
    4.
    发明授权
    Carboxylic acid derivatives, processes for the preparation thereof and pharmaceutical compositions containing them 失效
    羧酸衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：US4609673A

    公开(公告)日：1986-09-02

    申请号：US682935

    申请日：1984-12-18

    申请人： Hermann Eggerer ,  Bernd Hagenbruch ,  Tran G. Nguyen ,  Karlheinz Stegmeier ,  Johannes Pill

    发明人： Hermann Eggerer ,  Bernd Hagenbruch ,  Tran G. Nguyen ,  Karlheinz Stegmeier ,  Johannes Pill

    IPC分类号： A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K31/23 ,  A61P3/06 ,  C07C67/00 ,  C07C301/00 ,  C07C313/00 ,  C07C315/04 ,  C07C317/44 ,  C07C317/46 ,  C07C323/51 ,  C07C149/20 ,  C07C147/05

    CPC分类号： A61K31/23

    摘要： The present invention provides carboxylic acid derivatives of the general formula: ##STR1## wherein R is a hydrogen atom, alkyl, a metal cation or an ammonium or alkylammonium ion, R.sub.1 is a hydrogen atom, a hydroxyl group or an alkyl, O-alkyl,O-benzyl or O-acyl radical, R.sub.2 is a hydrogen atom or an alkyl, aryl or aralkyl radical, n is 0, 1 or 2 and R.sub.3 is an acyl radical, this radical being(a) a straight-chained or branched, saturated or unsaturated alkanoyl radical containing 2 to 11 carbon atoms; or(b) the radical ##STR2## in which A is a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon radical containing up to 4 carbon atoms, which is optionally substituted by hydroxyl, and B is a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon radical containing up to 8 carbon atoms, which is optionally substituted one or more times by hydroxyl, carboxyl or phenyl, or B is a phenyl or cycloalkyl radical; or(c) the radical ##STR3## in which A and B have the same meanings as in (b) and R.sub.4 is a hydrogen atom or an alkyl or aralkyl radical; as well as the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions containing them.

    摘要翻译： 本发明提供以下通式的羧酸衍生物：其中R是氢原子，烷基，金属阳离子或铵或烷基铵离子，R1是氢原子，羟基或烷基， O-烷基，O-苄基或O-酰基，R2是氢原子或烷基，芳基或芳烷基，n是0,1或2，R3是酰基，该基团是（a） 含有2至11个碳原子的链或支链，饱和或不饱和烷酰基; 或（b）其中A是含有至多4个碳原子的直链或支链，饱和或不饱和的脂族烃基的基团，其任选被羟基取代，B是直链或支链的， 含有至多8个碳原子的饱和或不饱和脂族烃基，其任选被羟基，羧基或苯基取代一次或多次，或B是苯基或环烷基; 或（c）其中A和B具有与（b）中相同含义的基团，R4为氢原子或烷基或芳烷基; 以及其药理学上可接受的盐。 本发明还提供了制备这些化合物的方法，以及含有它们的药物组合物。