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    5-Carbamoylthieno (2,3-B)thiophene-2-sulfon-amides as topically active carbonic anhydrase inhibitors
    1.
    发明公开
    5-Carbamoylthieno (2,3-B)thiophene-2-sulfon-amides as topically active carbonic anhydrase inhibitors 失效
    5-氨基甲酰噻吩并（2,3-B）噻吩-2-磺酰胺的制备方法Kohlensäureanhydraseinhibitoren。

    公开(公告)号：EP0382537A1

    公开(公告)日：1990-08-16

    申请号：EP90301352.2

    申请日：1990-02-08

    申请人： Merck & Co., Inc.

    发明人： Hartman, George D. ,  Prugh, John D.

    IPC分类号： C07D495/04 ,  A61K31/38

    CPC分类号： C07D495/04

    摘要： Novel 5-carbamoylthieno[2,3-b]thiophene-2-sulfonamides of formula (I) and derivatives thereof are prepared in
    reactions of 5-methoxycarbonylthieno[2,3-b]thiophene-2-sulfonamide with alkylamines, alkoxyalkylamines and hydroxyalkylamines. These compounds are useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.

    摘要翻译： 在5-甲氧基羰基噻吩并[2,3-b]噻吩-2-磺酰胺与烷基胺的反应中制备式（I）的新型5-氨基甲酰噻吩并[2,3-b]噻吩-2-磺酰胺及其衍生物， 烷氧基烷基胺和羟烷基胺。 这些化合物可用于治疗组合物中升高的眼内压，包括滴眼剂和插入物。

    5-Thiaalkanoic acid derivatives having antihypercholesterolemic activity
    2.
    发明公开
    5-Thiaalkanoic acid derivatives having antihypercholesterolemic activity 失效
    具有抗高胆固醇血症活性的5-硫杂链烷酸衍生物

    公开(公告)号：EP0127848A2

    公开(公告)日：1984-12-12

    申请号：EP84105921.5

    申请日：1984-05-24

    申请人： Merck & Co., Inc.

    发明人： Prugh, John D.

    IPC分类号： C07C149/00 ,  C07C147/14 ,  C07C147/00 ,  A61K31/19

    CPC分类号： C07C323/00 ,  A01N37/36 ,  A01N37/38 ,  A01N41/10 ,  C07C17/093 ,  C07C33/46 ,  C07C33/486 ,  C07C43/225 ,  C07C43/23 ,  C07C309/00 ,  C07C317/00 ,  C07C25/18

    摘要： Derivatives of 3-hydroxy-5-thia-ω-aryl-alkanoic acids are disclosed having the structural formula:
    wherein Z is:


    n is 0, 1 or 2;
    E is -CH 2 - -CH 2 -CH 2 -, -CH 2 -CH 2 -CH 2 -, -CH=CH-CH 2 -: or -CH 2 -CH=CH-;
    R,, R 2 and R 3 are, e.g.. hydrogen, chloro, bromo, fluoro, C 1-4 alkyl, phenyl, substituted phenyl or OR 7 in which R 7 is, e.g., hydrogen,
    C 2-8 alkanoyl, benzoyl, phenyl,
    substituted phenyl, C 1-9 alkyl,
    annamyl, C 1-4 haloalkyl, allyl,
    cycloalkyl-C 1-3 -alkyl, adamantyl-C 1-3 -atkyl.
    or phenyl Ci-3 alkyl;
    R 4 , R 5 and R 6 are gydrogen, chloro, bromo, fluoro or C 1-3 alkyl; and
    X is, e.g., hydrogen, C 1-3 alkyl, a cation derived from an alkali metal, or is ammonium.

    Those compounds have antihypercholesterolemic activity by virtue of their ability to inhibit 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase and antifungal acticity.

    摘要翻译： 公开了具有以下结构式的3-羟基-5-硫杂-ω-芳基 - 链烷酸的衍生物：其中Z是：n是0,1或2; E是-CH 2 -CH 2 -CH 2 - ， - CH 2 -CH 2 -CH 2 - ， - CH = CH-CH 2 - 或-CH 2 -CH = CH-; R 1，R 2和R 3是例如氢，氯，溴，氟，C 1-4烷基，苯基，取代的苯基或OR 7，其中R 7是例如氢，C 2-8烷酰基，苯甲酰基，苯基，取代的苯基， 茚基，C1-4卤代烷基，烯丙基，环烷基-C1-3-烷基，金刚烷基-C1-3-烷基。 或苯基C 1-3烷基; R4，R5和R6是氢，氯，溴，氟或C1-3烷基; X是例如氢，C1-3烷基，衍生自碱金属的阳离子或铵。 这些化合物凭借其抑制3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶和抗真菌活性的能力而具有抗高胆固醇血症活性。

    Substituted thieno(3,2-B) thiophene-2-sulfonamides as topically active carbonic anhydrase inhibitors
    6.
    发明公开
    Substituted thieno(3,2-B) thiophene-2-sulfonamides as topically active carbonic anhydrase inhibitors 失效
    噻吩并（3,2-B）噻吩-2-磺酰胺衍生物替代物（Kohlensäureanhydraseinhibitoren）。

    公开(公告)号：EP0375320A1

    公开(公告)日：1990-06-27

    申请号：EP89313201.9

    申请日：1989-12-18

    申请人： Merck & Co., Inc.

    发明人： Hartman, George D. ,  Prugh, John D.

    IPC分类号： C07D495/04 ,  A61K31/38

    CPC分类号： C07D495/04

    摘要： Novel substituted thieno[3,2-b]thiophene-2-­sulfonamides of formula (I) are prepared by novel synthetic processes. These compounds are useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.

    摘要翻译： 式（I）的新型取代的噻吩并[3,2-b]噻吩-2-磺酰胺通过新的合成方法制备。 这些化合物可用于治疗组合物中升高的眼内压，包括滴眼剂和插入物。

    5-[N-methoxyethyl-N-methoxyethoxyethyl)aminomethyl]thieno [2,3-b] thiophene-2-sulfonamide as antiglaucoma agents
    7.
    发明公开
    5-[N-methoxyethyl-N-methoxyethoxyethyl)aminomethyl]thieno [2,3-b] thiophene-2-sulfonamide as antiglaucoma agents 失效
    噻吩并[2,3-b]噻吩-2-磺酰胺的N- [N-甲氧基乙基 - 正 - 甲氧基乙氧基乙基]氨基甲基酯。

    公开(公告)号：EP0366178A1

    公开(公告)日：1990-05-02

    申请号：EP89202589.1

    申请日：1989-10-13

    申请人： Merck & Co., Inc.

    发明人： Hartman, George D. ,  Prugh, John D.

    IPC分类号： C07D495/04 ,  A61K31/38

    CPC分类号： C07D495/04

    摘要： This invention relates to novel aromatic sulfonamides useful in the treatment of elevated intraocular pressure. More particularly this invention relates to the compounds having the structural formula:
    as well as the pharmaceutically and ophthalmo­logically acceptable salts thereof. This invention also relates to pharmaceutical compositions and the use thereof for systemic and ophthalmic use employing the novel compound of this invention as active ingredient for the treatment of elevated intraocular pressure, especially when accompanied by pathological damage such as in the disease known as glaucoma. The invention also relates to processes for preparation of the novel compound.

    摘要翻译： 本发明涉及可用于治疗眼内压升高的新型芳族磺酰胺。 更具体地说，本发明涉及具有以下结构式的化合物：以及其药学和眼科学上可接受的盐。 本发明还涉及用于全身和眼用途的药物组合物及其用途，其使用本发明的新化合物作为治疗眼内压升高的活性成分，特别是伴有诸如称为青光眼的疾病的病理损伤时。 本发明还涉及新型化合物的制备方法。

    5-Thiaalkanoic acid derivatives having antihypercholesterolemic activity
    9.
    发明公开
    5-Thiaalkanoic acid derivatives having antihypercholesterolemic activity 失效
    具有抗胆固醇活性的5-硫代酸衍生物

    公开(公告)号：EP0127848A3

    公开(公告)日：1985-04-17

    申请号：EP84105921

    申请日：1984-05-24

    申请人： MERCK & CO. INC.

    发明人： Prugh, John D.

    IPC分类号： C07C149/00 ,  C07C147/14 ,  C07C147/00 ,  A61K31/19

    CPC分类号： C07C323/00 ,  A01N37/36 ,  A01N37/38 ,  A01N41/10 ,  C07C17/093 ,  C07C33/46 ,  C07C33/486 ,  C07C43/225 ,  C07C43/23 ,  C07C309/00 ,  C07C317/00 ,  C07C25/18

    摘要： Derivatives of 3-hydroxy-5-thia-ω-aryl-alkanoic acids are disclosed having the structural formula:
    wherein Z is:
    n is 0, 1 or 2; E is -CH 2 - -CH 2 -CH 2 -, -CH 2 -CH 2 -CH 2 -, -CH=CH-CH 2 -: or -CH 2 -CH=CH-; R,, R 2 and R 3 are, e.g.. hydrogen, chloro, bromo, fluoro, C 1-4 alkyl, phenyl, substituted phenyl or OR 7 in which R 7 is, e.g., hydrogen, C 2-8 alkanoyl, benzoyl, phenyl, substituted phenyl, C 1-9 alkyl, annamyl, C 1-4 haloalkyl, allyl, cycloalkyl-C 1-3 -alkyl, adamantyl-C 1-3 -atkyl. or phenyl Ci-3 alkyl; R 4 , R 5 and R 6 are gydrogen, chloro, bromo, fluoro or C 1-3 alkyl; and X is, e.g., hydrogen, C 1-3 alkyl, a cation derived from an alkali metal, or is ammonium. Those compounds have antihypercholesterolemic activity by virtue of their ability to inhibit 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase and antifungal acticity.

    摘要翻译： 公开了具有以下结构式的3-羟基-5-硫杂 - ω-芳基 - 链烷酸的衍生物： n为0,1或2; E是-CH 2 - ， - CH 2 -CH 2 - ， - CH 2 -CH 2 -CH 2 - ， - CH = CH-CH 2 - 。 或-CH 2 -CH = CH-; R1，R2和R3是例如氢，氯，溴，氟，C1-4烷基，苯基，取代的苯基或OR7，其中R7是例如氢，C2-8烷酰基，苯甲酰基，苯基，取代的苯基，C1-9烷基 ，肉桂基，C 1-4卤代烷基，烯丙基，环烷基-C 1-3 - 烷基，金刚烷基-C 1-3 - 烷基或苯基C 1-3烷基; R 4，R 5和R 6是氢，氯，溴，氟或C 1-3烷基; X是例如氢，C 1-3烷基，衍生自碱金属的阳离子，或是铵。 这些化合物由于其抑制3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶和抗真菌活性的能力而具有抗高胆固醇血症活性。