Piperazine-substituted aryl and aralkyl carboxylic acids useful for
treating infirmaties caused by excess lipids or thrombocyte
    9.
    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

    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。

    Sulfonamides of phenylalkylamines or phenoxyalkylamines processes for
their preparation and medicaments containing these compounds
    10.
    发明授权
    Sulfonamides of phenylalkylamines or phenoxyalkylamines processes for their preparation and medicaments containing these compounds 失效
    苯基烷基胺或苯氧基烷基胺的磺酰胺用于制备它们和含有这些化合物的药物

    公开(公告)号:US5446065A

    公开(公告)日:1995-08-29

    申请号:US75489

    申请日:1993-06-21

    摘要: Compounds of the formula I ##STR1## in which R.sub.1 signifies an aryl, aralkyl or an aralkenyl group, the aryl radical of which can, in each case, be substituted one or more times by halogen, cyano, alkyl, trifluoromethyl, alkoxy, alkylthio, trifluoromethoxy, hydroxyl or carboxyl, m a whole number from 1 to 3, n a whole number from 1 to 5, R.sub.2 hydrogen, an alkyl, aralkyl or acyl group, Q a bond or an oxygen atom, R.sub.3 hydrogen or a lower alkyl radical which is possibly terminally substituted by carboxyl or by a hydroxyl group and R.sub.4 hydrogen, a lower alkyl group with 1-4 C-atoms, which is possibly terminally substituted by carboxyl or hydroxyl, a possibly substituted phenyl, heteroaryl, cycloalkyl or acyl group or a group ##STR2## in which R.sub.5 represents a straight-chained or branched alkyl chain with 1-4 C-atoms which is possibly terminally substituted by carboxyl, alkoxycarbonyl, aminocarbonyl, hydroxyl, mercapto, alkylthio or imidazolyl and Y a carboxyl, an alkoxycarbonyl, aminocarbonyl or cyano, formyl, hydroxymethyl, aminomethyl or ortho ester group, whereby R.sub.3 and R.sub.4 can also be component of a 5- or 6-membered saturated or unsaturated possibly substituted heterocycle with 1-4 heteroatoms which can be annellated with further ring compounds via one or more bonds, as well as their salts, esters and amides, processes for their preparation and medicaments with thromboxane-antagonistic action which contain these compounds.

    摘要翻译: PCT No.PCT / EP91 / 02456 Sec。 371日期:1993年6月21日 102(e)日期1993年6月21日PCT 1991年12月19日PCT公布。 出版物WO92 / 日期:1992年7月9日。式Ⅰ化合物(Ⅰ)其中R1表示芳基,芳烷基或芳烯基,其芳基可以在每种情况下被卤素取代一次或多次 氰基,烷基,三氟甲基,烷氧基,烷硫基,三氟甲氧基,羟基或羧基,整数为1至3,na整数1至5,R 2氢,烷基,芳烷基或酰基,Q a键或氧 原子,R3氢或可能被羧基或羟基末端取代的低级烷基,R4为氢原子,可被羧基或羟基末端取代的具有1-4个C原子的低级烷基,可能被取代 苯基,杂芳基,环烷基或酰基或基团,其中R 5表示具有1-4个C原子的直链或支链烷基链,其可以被羧基末端取代,烷氧基羰基,氨基羰基,羟基,巯基,烷硫基 或咪唑基,Y是羧基,烷氧基羰基 1,氨基羰基或氰基,甲酰基,羟甲基,氨基甲基或原酸酯基,其中R3和R4也可以是具有1-4个杂原子的5或6元饱和或不饱和可能取代的杂环的组分,其可以与另外的环 通过一个或多个键的化合物,以及它们的盐,酯和酰胺,其制备方法和含有这些化合物的血栓烷拮抗作用的药物。