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37 条记录 (耗时 0.023 秒)

    4-pyridyl-1,3-dioxane derivatives
    31.
    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。

    Ingestible hydrophilic polymeric amines useful for lowering blood cholesterol
    32.
    发明授权
    Ingestible hydrophilic polymeric amines useful for lowering blood cholesterol 失效
    可用的亲水性聚合胺可用于降低血液胆固醇

    公开(公告)号：US5236701A

    公开(公告)日：1993-08-17

    申请号：US381988

    申请日：1989-07-19

    申请人： Leon E. St. Pierre ,  George R. Brown ,  Gaoming Wu

    发明人： Leon E. St. Pierre ,  George R. Brown ,  Gaoming Wu

    IPC分类号： A61K31/785

    CPC分类号： A61K31/785

    摘要： The invention is concerned with novel ingestible cross-linked homopolymers having functional groups consisting of linear or branched amines, of the formula: ##STR1## and their pharmaceutically acceptable salts of the formulae: ##STR2## wherein P represents a hydrophilic, cross-linked and non-digestible homopolymer backbone; R is a hydrogen atom or a lower alkyl radical; X.sup.- is a pharmaceutically acceptable anion; m is an integer varying from 1 to 10 inclusive; and n, o and p are, independently, integers varying from 2 to 12 inclusive. The amine functionalized and cross-linked homopolymers of the invention are highly efficient adsorbents for bile acids and salts and can thus be used for reducing hypercholesterolemia in affected humans.

    摘要翻译： 本发明涉及具有下列通式的直链或支链胺官能团的新颖可摄取的交联均聚物：其[P（（CH 2）n NRR）m R（Ia）或者（Ib））及其药学上可接受的盐 式：P [（CH2）nN +（R）2] mR.mX-（Ic）和（IMA）其中P表示亲水的，交联和不消化的均聚物主链; R是氢原子或低级烷基; X-是药学上可接受的阴离子; m为1〜10的整数， 并且n，o和p独立地为从2到12的整数。 本发明的胺官能化和交联的均聚物是胆汁酸和盐的高效吸附剂，因此可用于降低受影响人体的高胆固醇血症。

    N-[4-o-hydroxyphenyl-1,3-dioxan-5-ylhexenoyl]sulphonamides
    35.
    发明授权
    N-[4-o-hydroxyphenyl-1,3-dioxan-5-ylhexenoyl]sulphonamides 失效
    N- [4-邻羟基苯基-1,3-二恶烷-5-基己烯酰基]磺酰胺

    公开(公告)号：US4845120A

    公开(公告)日：1989-07-04

    申请号：US40153

    申请日：1987-04-20

    申请人： George R. Brown ,  Michael J. Smithers

    发明人： George R. Brown ,  Michael J. Smithers

    IPC分类号： A61K31/335 ,  A61K31/357 ,  A61P9/00 ,  A61P9/12 ,  A61P11/08 ,  C07D319/06 ,  C07F7/18

    CPC分类号： C07D319/06

    摘要： The invention concerns novel N-[4(Z)-2-substituted-6-(4-o-hydroxyphenyl-1,3 dioxan-cis-5-yl)hexenoyl]sulphonamide derivatives of formula I of value as therapeutic agents. Typically R.sup.1 is a branched (3-6C)alkyl, trifluoromethyl or phenyl radical as defined hereinafter and R.sup.2 is alkyl, benzyl or phenyl.The invention also discloses salts of the formula I compounds as well as pharmaceutical compositions containing the compounds and processes for the production of the compounds.

    摘要翻译： 本发明涉及价值为治疗剂的式I的新型N- [4（Z）-2-取代-6-（4-邻羟基苯基-1,3-二烷 - 顺式-5-基）己烯酰基]磺酰胺衍生物。 通常R 1是如下文所定义的支链（3-6C）烷基，三氟甲基或苯基，R 2是烷基，苄基或苯基。 本发明还公开了式I化合物的盐以及含有化合物的药物组合物和用于制备化合物的方法。

    1,3-Dioxolane-5-yl-hexenoic acid derivatives
    36.
    发明授权
    1,3-Dioxolane-5-yl-hexenoic acid derivatives 失效
    1,3-二氧戊环-5-基 - 己烯酸衍生物

    公开(公告)号：US4824858A

    公开(公告)日：1989-04-25

    申请号：US861335

    申请日：1986-05-09

    申请人： George R. Brown ,  Michael J. Smithers

    发明人： George R. Brown ,  Michael J. Smithers

    IPC分类号： C07D319/06 ,  A61K31/335

    CPC分类号： C07D319/06

    摘要： The invention describes novel (2-styryl-, 2-naphthyl- and 2-phenethyl-4-o-hydroxyphenyl-1,3-dioxan-5-yl)alkenoic acids and related tetrazoles and sulphonamides, of the formula I wherein Q completes a benzene or pyridine ring, Y is vinylene, Z is carboxy, 1 (H)-tetrazol-5-yl or a group of the formula --CO.NHSO.sub.2 R.sup.6, and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, A.sup.1, A.sup.2, n and m have the meanings defined in the specification, and pharmaceutically acceptable salts thereof, for use in conjunction with their pharmaceutical compositions in treating certain pulmonary and/or vascular disorders. The invention also describes various processes and intermediates for the manufacture of the novel compounds.

    摘要翻译： 本发明描述了式I中的新型（2-苯乙烯基，2-萘基 - 和2-苯乙基-4-邻羟基苯基-1,3-二恶烷-5-基）链烯酸和相关的四唑和磺酰胺，其中Q完成 苯或吡啶环，Y是亚乙烯基，Z是羧基，1（H） - 四唑-5-基或式-CO.NHSO 2 R 6，R1，R2，R3，R4，R5，R6，A1， A2，n和m具有本说明书中定义的含义及其药学上可接受的盐，用于与其药物组合物联合用于治疗某些肺和/或血管疾病。 本发明还描述了用于制备新化合物的各种方法和中间体。