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    Tyrosine derivatives, a process for preparing the same and a pharmaceutical composition containing the same for treating hypertension
    5.
    发明公开
    Tyrosine derivatives, a process for preparing the same and a pharmaceutical composition containing the same for treating hypertension 失效
    酪氨酸衍生物，它们的制备方法和用于治疗高血压的药物组合物。

    公开(公告)号：EP0030734A1

    公开(公告)日：1981-06-24

    申请号：EP80107927.8

    申请日：1980-12-16

    申请人： Merck & Co., Inc.

    发明人： Baldwin, John J. ,  Ponticello, Gerald S. ,  Denny, George H. ,  Stone, Clement A.

    IPC分类号： C07C101/72 ,  C07D521/00 ,  A61K31/195

    CPC分类号： C07D233/64 ,  C07D213/51 ,  C07D231/12 ,  C07D233/56 ,  C07D239/26 ,  C07D241/24 ,  C07D249/08 ,  C07D261/18 ,  C07D285/08 ,  C07D307/54

    摘要： Tyrosine derivatives having the formula:
    wherein

    A is H, C 2 -C 4 -alkanoyl, benzoyl, substituted benzoyl, phen-C 2 -C 4 alkanoyl or substituted phen-C 2 -C4- alkanoyl,
    R 1 is H, C 1 -C 4 alkyl, phenyl, substituted phenyl, phen-C 1 -C 4 -alkyl, substituted phen-C 1 -C 4 -alkyl and substituted or unsubstituted heteroaryl group having 5-6 ring members and 1-3 hetero atoms selected from 0, N and S,
    X is O or S and
    R 2 is an acyl radical of the formula
    wherein R 3 is C 1 -C 17 alkyl, phenyl, substituted phenyl, phen-C 1 -C 4 -alkyl, substituted phen-C 1 -C 4 -alkyl, heteroaryl having 5-6 ring members and 1-3 hetero atoms selected from 0, S and N or said heteroaryl-C 1 -C 4 -alkyl, a process for their preparation and a pharmaceutical composition containing those tyrosine derivatives for treating hypertension are disclosed.

    摘要翻译： 具有下式的酪氨酸衍生物：其中A是H，C 2 -C 4烷酰基，苯甲酰基，取代的苯甲酰基，苯-C2 -C 4烷酰基或苯substituiertem-C2 -C 4烷酰基，R 1是H，C 1 -C 4烷基的苯基，取代 苯基，苯基-C1-C4-烷基，取代的选自O，N和S中的苯基-C 1 -C 4烷基和具有5-6个环成员和1-3个杂原子substituiertem奥德unsubstituiertem杂芳基，X是O或S，并且 R 2是下式基团 worin R3的酰基是C1-C17烷基，苯基，苯基substituiertem，苯-C1-C4烷基，substituiertem苯-C1-C4烷基，杂芳基具有5-6个环成员和1 -3杂原子选自O，S和N或所述杂芳基C1-C4烷基，一个其制备方法和包含用于治疗高血压的那些酪氨酸衍生物的药物组合物是游离缺失光盘。

    Substituted dihydrothieno-thiophene-2-sulfonamides and dioxides thereof
    8.
    发明公开
    Substituted dihydrothieno-thiophene-2-sulfonamides and dioxides thereof 失效
    取代基二氢噻吩并噻吩-2-磺酰胺和二氧化物。

    公开(公告)号：EP0480745A2

    公开(公告)日：1992-04-15

    申请号：EP91309372.0

    申请日：1991-10-11

    申请人： MERCK & CO. INC.

    发明人： Baldwin, John J. ,  Selnick, Harold G. ,  Ponticello, Gerald S. ,  Radzilowski, Ellen M.

    IPC分类号： C07D495/04 ,  C07D333/34 ,  A61K31/38

    CPC分类号： C07D495/04 ,  C07D333/34

    摘要： Substituted 4,5-dihydrothieno[2,3-b]thiophene-2-sulfonamides and 6,6-oxides and dioxides thereof of formula I and the isomeric 5,6-dihydrothieno[3,2-b]thiophene-2-sulfonamides and 4,4-dioxides thereof of formula II are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.

    摘要翻译： 取代的式I的4,5-二氢噻吩并[2,3-b]噻吩-2-磺酰胺及其6,6-氧化物和二氧化物和异构的5,6-二氢噻吩并[3,2-b]噻吩-2-磺酰胺 和式II的4,4-二氧化物是可用于治疗与其相关的高眼压症和青光眼的局部有效的碳酸酐酶抑制剂。 -