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10 条记录 (耗时 0.04 秒)

    Pyridyl substituted alkenoic acid derivatives
    1.
    发明授权
    Pyridyl substituted alkenoic acid derivatives 失效
    吡啶基取代的烯酸衍生物

    公开(公告)号：US5248780A

    公开(公告)日：1993-09-28

    申请号：US951760

    申请日：1992-09-25

    申请人： Andrew G. Brewster ,  George R. Brown ,  Alan W. Faull ,  Reginald Jessup ,  Michael J. Smithers

    发明人： Andrew G. Brewster ,  George R. Brown ,  Alan W. Faull ,  Reginald Jessup ,  Michael J. Smithers

    IPC分类号： C07D405/04 ,  C07D405/14

    CPC分类号： C07D405/04 ,  C07D405/14

    摘要： The invention concerns novel, pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of the formula I containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A.sup.1 is alkylene, R.sup.1 is a variety of substituents defined hereinafter, and R.sup.2 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.

    摘要翻译： 本发明涉及式I的新型药学上有用的1,3-二烷基链烯酸衍生物，其在二恶烷环的第4位含有吡啶基部分，其中第2,4和5位的基团具有顺式相对立体化学，X是 氢，烷氧基或羟基，Y是亚乙烯基，n是1或2，A1是亚烷基，R1是下文定义的各种取代基，R2是羟基，生理上可接受的醇残基或烷基磺酰氨基，及其药学上可接受的盐。 本发明还包括用于制备和使用酸衍生物的方法以及用于治疗用于一种或多种疾病如缺血性心脏病，脑血管疾病，哮喘病和/或炎性疾病的药物组合物。

    4-pyridyl-1,3-dioxane derivatives
    3.
    发明授权
    4-pyridyl-1,3-dioxane derivatives 失效
    4-吡啶基-1,3-二恶烷衍生物

    公开(公告)号：US5401849A

    公开(公告)日：1995-03-28

    申请号：US78658

    申请日：1993-06-21

    申请人： Andrew G. Brewster ,  George R. Brown ,  Alan W. Faull ,  Reginald Jessup ,  Michael J. Smithers

    发明人： Andrew G. Brewster ,  George R. Brown ,  Alan W. Faull ,  Reginald Jessup ,  Michael J. Smithers

    IPC分类号： C07D405/04 ,  C07D405/14

    CPC分类号： C07D405/04 ,  C07D405/14

    摘要： The invention concerns pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of formula VII and formula XI containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, wherein X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A.sup.1 is alkylene, R.sup.1 is a variety of substituents defined hereinafter, Ra and Rb are independently methyl or ethyl, R.sup.2 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及式VII和式XI的药学上有用的1,3-二恶烷烯酸衍生物，其在二恶烷环的4位含有吡啶基部分，其中2,4和5位的基团具有顺式相对立体化学，其中X 是氢，烷氧基或羟基，Y是亚乙烯基，n是1或2，A1是亚烷基，R1是下文定义的各种取代基，R a和R b独立地是甲基或乙基，R 2是羟基，生理上可接受的醇残基或烷基磺酰胺 ，及其药学上可接受的盐。

    Heterocyclic acids
    9.
    发明授权
    Heterocyclic acids 失效
    杂环酸

    公开(公告)号：US5410064A

    公开(公告)日：1995-04-25

    申请号：US36304

    申请日：1993-03-24

    申请人： Alan W. Faull ,  Keith Russell ,  William J. Watkins

    发明人： Alan W. Faull ,  Keith Russell ,  William J. Watkins

    IPC分类号： A61K31/415 ,  A61K31/425 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  C07D263/26 ,  C07D403/04 ,  C07D405/04 ,  C07D417/04 ,  C07D263/38

    CPC分类号： C07D403/04 ,  C07D263/26 ,  C07D417/04

    摘要： The invention concerns novel 1,3-dioxane alkenoic acid derivatives of the formula I ##STR1## wherein: n is the integer 1 or 2; Y is methyleneoxy, vinylene or ethylene;A.sup.1 is (1-6C)alkylene;R.sup.1 is a group of the formula R.sup.2.A.sup.2 -, in which:R.sup.2 is phenyl unsubstituted or bearing up to three substituents which are independently selected from (1-6C)alkyl, (1-6C)alkoxy, (2-6C)alkanoyl, (1-6C)alkylthio, (1-6C)alkylsulphonyl, halogeno, trifluoromethyl, nitro and cyano;A.sup.2 is a direct bond to R.sup.2 or a group of the formula --W--C(R.sup.4)(R.sup.5)-- wherein W is oxygen, methylene or a direct bond to R.sup.2, and R.sup.4 and R.sup.5 are independently (1-4C)alkyl;Q is a heterocyclyl group selected from thiazol-5-yl and imidazol-5-yl, the latter being unsubstituted or bearing a (1-12C)alkyl group at the 1-position of the imidazole ring; andR.sup.3 is hydroxy, a physiologically acceptable alcohol residue, or (1-4C)alkanesulphonamido;or a pharmaceutically acceptable salt thereof. The compounds are thromboxane A.sub.2 antagonists and inhibitors of thromboxane A.sub.2 synthase, and are useful on the treatment of a variety of diseases in which thromboxane A.sub.2 is involved, such as is ischaemic heart disease, cerebrovascular disease and peripheral vascular disease. The invention also includes processes for the manufacture and use of the compounds, and pharmaceutical compositions containing them.

    摘要翻译： 本发明涉及式I的新型1,3-二恶烷烯酸衍生物，其中：n是整数1或2; Y是亚甲氧基，亚乙烯基或亚乙基; A1为（1-6C）亚烷基; R1是式R2.A2-的基团，其中：R2是未取代的或最多带有三个独立地选自（1-6C）烷基，（1-6C）烷氧基，（2-6C）烷酰基的取代基的苯基 ，（1-6C）烷硫基，（1-6C）烷基磺酰基，卤代，三氟甲基，硝基和氰基; A2是与R2或式-W-C（R4）（R5） - 的基团的直接键合，其中W是氧，亚甲基或与R2的直接键合，R4和R5独立地是（1-4C）烷基; Q是选自噻唑-5-基和咪唑-5-基的杂环基，后者是未取代的或在咪唑环的1位带有（1-12C）烷基; 和R3是羟基，生理上可接受的醇残基或（1-4C）烷基磺酰胺基; 或其药学上可接受的盐。 化合物是凝血恶烷A2拮抗剂和凝血恶烷A2合酶抑制剂，可用于治疗血栓素A2涉及的多种疾病，例如缺血性心脏病，脑血管病和外周血管病。 本发明还包括用于制备和使用化合物的方法以及含有它们的药物组合物。

    Heterocyclic acids
    10.
    发明授权
    Heterocyclic acids 失效
    杂环酸

    公开(公告)号：US5219874A

    公开(公告)日：1993-06-15

    申请号：US763304

    申请日：1991-09-20

    申请人： Alan W. Faull ,  Keith Russell ,  Williams J. Watkins

    发明人： Alan W. Faull ,  Keith Russell ,  Williams J. Watkins

    IPC分类号： A61K31/415 ,  A61K31/425 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  C07D263/26 ,  C07D403/04 ,  C07D405/04 ,  C07D417/04

    CPC分类号： C07D403/04 ,  C07D263/26 ,  C07D417/04

    摘要： The invention concerns novel 1,3-dioxane alkenoic acid derivatives of the formula I ##STR1## wherein: n is the integer 1 or 2;Y is methyleneoxy, vinylene or ethylene;A.sup.1 is (1-6C)alkylene;R.sup.1 is a group of the formula R.sup.2.A.sup.2 --, in which:R.sup.2 is phenyl unsubstituted or bearing up to three substituents which are independently selected from (1-6C)alkyl, (1-6C)alkoxy, (2-6C)alkanoyl, (1-6C)alkylthio, (1-6C)alkylsulphonyl, halogeno, trifluoromethyl, nitro and cyano;A.sup.2 is a direct bond to R.sup.2 or a group of the formula --W--C(R.sup.4)(R.sup.5)-- wherein W is oxygen, methylene or a direct bond to R.sup.2, and R.sup.4 and R.sup.5 are independently (1-4C)alkyl;Q is a heterocyclyl group selected from thiazol-5-yl and imidazol-5-yl, the latter being unsubstituted or bearing a (1-12C)alkyl group at the 1-position of the imidazole ring; andR.sup.3 is hydroxy, a physiologically acceptable alcohol residue, or (1-4C)alkanesulphonamido;or a pharmaceutically acceptable salt thereof. The compounds are thromboxane A.sub.2 antagonists and inhibitors of thromboxane A.sub.2 synthase.

    摘要翻译： 本发明涉及式I的新型1,3-二恶烷烯酸衍生物，其中：n是整数1或2; Y是亚甲氧基，亚乙烯基或亚乙基; A1为（1-6C）亚烷基; R1是式R2.A2-的基团，其中：R2是未取代的或最多带有三个独立地选自（1-6C）烷基，（1-6C）烷氧基，（2-6C）烷酰基的取代基的苯基 ，（1-6C）烷硫基，（1-6C）烷基磺酰基，卤代，三氟甲基，硝基和氰基; A2是与R2或式-W-C（R4）（R5） - 的基团的直接键合，其中W是氧，亚甲基或与R2的直接键合，R4和R5独立地是（1-4C）烷基; Q是选自噻唑-5-基和咪唑-5-基的杂环基，后者是未取代的或在咪唑环的1位带有（1-12C）烷基; 和R3是羟基，生理上可接受的醇残基或（1-4C）烷基磺酰胺基; 或其药学上可接受的盐。 化合物是凝血恶烷A2拮抗剂和血栓烷A2合酶抑制剂。