Anti-SRSA quinoline carboxylic acid derivatives
    5.
    发明授权
    Anti-SRSA quinoline carboxylic acid derivatives 失效
    抗SRSA喹啉羧酸衍生物

    公开(公告)号:US4474788A

    公开(公告)日:1984-10-02

    申请号:US438163

    申请日:1982-11-01

    申请人: John R. Bantick

    发明人: John R. Bantick

    摘要: There are described compounds of formula I, ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.7, which may be the same or different, each represent hydrogen, hydroxy, alkyl Cl to 6, alkoxy C1 to 6, amino, acyl C2 to 6, acylamino C2 to 6, alkenyl C2 to 6, halogen, or alkoxy C1 to 6 substituted by phenyl,X is a hydrocarbon chain of 1 to 10 carbon atoms optionally substituted by a hydroxy group,A is --Q--COOH,Q is absent or represents a straight or branched alkylene, alkenylene or alkynylene group of up to and including 6 carbon atoms,R.sub.8 and R.sub.9, which may be the same or different, each represent hydrogen or alkyl C1 to 6 or together form a single bond,D, Y and Z, which may be th same or different, each represent sulphur, oxygen or --NR.sub.10 --, andR.sub.10 is hydrogen or alkyl C1-C6,provided that(i) when D, Z and Y are all oxygen, R.sub.8 and R.sub.9 do not together form a single bond,(ii) when D is oxygen, R.sub.8 and R.sub.9 together form a single bond, X is (CH.sub.2).sub.5, A is --COOH, one of Y and Z is sulphur and the other is oxygen, at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.7 is other than hydrogen,and pharmaceutically acceptable salts, esters and amides thereof.There are also described processes to these compounds, and pharmaceutical, e.g. anti-allergic, compositions containing them.

    摘要翻译: 描述了式I的化合物,其中可以相同或不同的R 1,R 2,R 3,R 4,R 5和R 7各自表示氢,羟基,C 1-6烷基,烷氧基C1至6, 氨基,酰基C2至6,酰基氨基C2至6,烯基C2至6,卤素或被苯基取代的烷氧基C1至6,X为任选被羟基取代的1至10个碳原子的烃链,A为-Q -COOH,Q不存在或表示直至并包括6个碳原子的直链或支链亚烷基,亚烯基或亚炔基,R8和R9可以相同或不同,各自表示氢或C1至6的烷基或一起形成 单键,D,Y和Z可以相同或不同,各自表示硫,氧或-NR 10 - ,R 10是氢或C 1 -C 6烷基,条件是(ⅰ)当D,Z和Y为 (ⅱ)当D为氧时,R 8和R 9一起形成单键,X为(CH 2)5,A为-COOH,Y和Z之一为硫 和另一个 是氧,R 1,R 2,R 3,R 4,R 5和R 7中的至少一个不是氢,及其药学上可接受的盐,酯和酰胺。 还描述了这些化合物的方法,以及药物,例如, 抗过敏,含有它们的组合物。

    Pharmaceutical heterocyclic compounds and compositions
    6.
    发明授权
    Pharmaceutical heterocyclic compounds and compositions 失效
    药物杂环化合物和组合物

    公开(公告)号:US4281008A

    公开(公告)日:1981-07-28

    申请号:US127832

    申请日:1980-03-06

    摘要: The compounds of the formula: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.7, which may be the same or different, each represent hydrogen, hydroxy, alkyl or alkoxy of 1 to 6 carbon atoms, amino, acyl or acylamino of 2 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, halogen, or alkoxy of 1 to 6 carbon atoms substituted by phenyl,X is a hydrocarbon chain of 1 to 10 carbon atoms optionally substituted by a hydroxy group,A is oxygen or is absent,Q represents a straight or branched alkylene, alkenylene or alkynylene group of 2 to 6 carbon atoms, andD represents carboxy, 5-tetrazolyl or carboxamido-5-tetrazolyl,and pharmaceutically acceptable salts, esters and amides thereof,are pharmaceutically active, being antagonists of the slow reacting substance of anaphylaxis (SRS-A) or its pathological effects.Pharmaceutical compositions containing the compounds are also described, as well as processes for preparing the compounds.

    摘要翻译: 下式的化合物:其中:R 1,R 2,R 3,R 4,R 5和R 7可以相同或不同,分别表示1至6个碳原子的氢,羟基,烷基或烷氧基, 2至6个碳原子的氨基,酰基或酰基氨基,2至6个碳原子的烯基,卤素或被苯基取代的1至6个碳原子的烷氧基,X是任选被羟基取代的1至10个碳原子的烃链 基团,A为氧或不存在,Q表示2至6个碳原子的直链或支链亚烷基,亚烯基或亚炔基,D表示羧基,5-四唑基或甲酰胺基-5-四唑基,以及药学上可接受的盐,酯和 其酰胺是药学活性的,是过敏反应缓慢反应物质(SRS-A)或其病理作用的拮抗剂。 还描述了含有这些化合物的药物组合物,以及制备化合物的方法。