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23 条记录 (耗时 0.018 秒)

    Substituted sulphonamides, pharmaceuticals thereof and methods of using them
    1.
    发明授权
    Substituted sulphonamides, pharmaceuticals thereof and methods of using them 失效
    取代的磺酰胺，其药物和使用它们的方法

    公开(公告)号：US4981873A

    公开(公告)日：1991-01-01

    申请号：US370455

    申请日：1989-06-23

    申请人： Ernst-Christian Witte ,  Karlheinz Stegmeier ,  Liesel Doerge ,  Robert A. Slater

    发明人： Ernst-Christian Witte ,  Karlheinz Stegmeier ,  Liesel Doerge ,  Robert A. Slater

    IPC分类号： A61K31/18 ,  A61K31/19 ,  A61K31/22 ,  A61K31/41 ,  A61K31/655 ,  A61P1/04 ,  A61P7/02 ,  A61P9/00 ,  A61P11/00 ,  A61P43/00 ,  C07C311/04 ,  C07C311/05 ,  C07C311/14 ,  C07C311/17 ,  C07C311/18 ,  C07C311/29 ,  C07C311/40 ,  C07C317/14 ,  C07C317/28 ,  C07C317/44 ,  C07C323/49 ,  C07C323/52 ,  C07C323/60 ,  C07C323/67 ,  C07D257/04

    CPC分类号： C07C317/14 ,  C07C323/52

    摘要： The present invention concerns compounds of the formula: ##STR1## where R.sub.1 is an alkyl or alkenyl radical containing up to 6 carbon atoms, a cycloalkyl radical containing 3 to 7 carbon atoms, an aralkyl, aralkenyl or aryl radical in which the aryl radical or moiety can be substituted one or more times by halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 -alkylamino, C.sub.2 -C.sub.12 -dialkylamino, C.sub.1 -C.sub.6 -acylamino, C.sub.1 -C.sub.16 -acyl, C.sub.1 -C.sub.6 -alkylsulphenyl, -sulphinyl or -sulphonyl or by azido, R.sub.2 is hydrogen atom or a C.sub.1 -C.sub.6 -alkyl, aralkyl, aralkenyl or acyl radical, A and B are saturated or unsaturated alkylene chains containing up to 10 carbon atoms which can be substituted one or more times by C.sub.1 -C.sub.3 -alkyl radicals, the sum of carbon atoms in chains A and B being at least 4 and at most 11, Q is an oxygen or sulphur atom, a sulphonyl or sulphinyl group or an amino group --N(R.sub.2)--, R.sub.2 having the same meaning as above, and Y is a free carboxylic acid group or a carboxylic acid ester, carboxylic acid amide, hydroxymethyl or tetrazolyl radical; the pharmacologically acceptable salts thereof and the optically active and E-Z isomers thereof, as well as mixtures thereof.These compounds are useful as they have an antagonistic action towards thromboxane A.sub.2 as well as against prostaglandin endoperoxide. They inhibit the aggregation of blood platelets and prevent the constriction of the smooth musculature as well as bronchoconstriction.

    摘要翻译： 本发明涉及下式的化合物：其中R1是含有至多6个碳原子的烷基或烯基，含有3-7个碳原子的环烷基，芳烷基，芳烯基或芳基，其中芳基或 C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，羟基，三氟甲基，氰基，硝基，氨基，C 1 -C 6 - 烷基氨基，C 2 -C 12 - 二烷基氨基，C 1 -C 6酰基氨基 ，C 1 -C 16 - 酰基，C 1 -C 6 - 烷基亚磺酰基， - 亚磺酰基或 - 磺酰基或叠氮基，R 2是氢原子或C 1 -C 6烷基，芳烷基，芳烯基或酰基，A和B是饱和或不饱和亚烷基链 含有多至10个可被C 1 -C 3 - 烷基取代一次或多次的碳原子，链A和B中的碳原子总数至少为4且至多为11，Q是氧或硫原子， 磺酰基或亚磺酰基或氨基-N（R2） - ，R2具有与上述相同的含义，Y是游离羧酸基或羧基 C酸酯，羧酸酰胺，羟甲基或四唑基; 其药理学上可接受的盐及其光学活性和E-Z异构体，以及它们的混合物。 这些化合物是有用的，因为它们对血栓素A2以及前列腺素过氧化物具有拮抗作用。 它们抑制血小板聚集，防止平滑肌肉收缩以及支气管收缩。

    Sulphonamidocycloalkane compounds, pharmaceutical compositions containing them, and methods of use thereof
    2.
    发明授权
    Sulphonamidocycloalkane compounds, pharmaceutical compositions containing them, and methods of use thereof 失效
    磺酰胺环糊精化合物，含有它们的药物组合物及其使用方法

    公开(公告)号：US5140038A

    公开(公告)日：1992-08-18

    申请号：US401254

    申请日：1989-08-31

    申请人： Ernst-Christian Witte ,  Karlheinz Stegmeier ,  Liesel Doerge

    发明人： Ernst-Christian Witte ,  Karlheinz Stegmeier ,  Liesel Doerge

    IPC分类号： A61K31/18 ,  A61K31/195 ,  A61K31/22 ,  A61K31/41 ,  A61P1/04 ,  A61P3/00 ,  A61P7/02 ,  A61P9/00 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/28 ,  C07C311/19 ,  C07C323/65 ,  C07D257/04 ,  C07D257/06

    CPC分类号： C07D257/04 ,  C07C311/19 ,  C07D257/06 ,  C07C2101/14

    摘要： The present invention provides sulphonamides of the general formula: ##STR1## wherein R.sup.1 and R.sup.2, which can be the same or different, are hydrogen or halogen atoms or C.sub.1 -C.sub.6 -alkyl, trifluoro-methyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, N-alkylaminocarbonyl or N,N-dialkylaminocarbonyl radicals or, when R.sup.1 and R.sup.2 are alkyl radicals ortho to one another, R.sup.1 and R.sup.2, together with the carbon atoms to which they are attached, form a saturated or unsaturated C.sub.5 -C.sub.7 -alkylene ring, R.sup.3 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical, a phenylalkyl or phenylalkenyl radical, the phenyl moiety of which can be substituted by halogen, alkyl or trifluoromethyl, C is a --(CH.sub.2).sub.m -- radical, in which m is 0, 1, 2 or 3, or a branched C.sub.2 -C.sub.5 alkylene radical, whereby a methylene radical --CH.sub.2 -- of the group C can be replaced by an oxygen or sulphur atom or by a hydroxymethylene radical --CHOH-- or carbonyl group --CO--, B is a 1,2-, 1,3-, 1,4-cyclohexylidene or 1,2- or 1,3-cyclopentylidene radical.

    摘要翻译： 本发明提供通式如下的磺酰胺：其中R 1和R 2可以相同或不同，为氢或卤素原子或C 1 -C 6烷基，三氟甲基，氰基，羧基，烷氧基羰基 ，氨基羰基，N-烷基氨基羰基或N，N-二烷基氨基羰基，或者当R 1和R 2是彼此相邻的烷基时，R 1和R 2与它们连接的碳原子一起形成饱和或不饱和的C5-C7 - 亚烷基环，R3是氢原子，含有至多6个碳原子的烷基，酰基，苯基烷基或苯基烯基，其苯基部分可以被卤素，烷基或三氟甲基取代，C是 - （ CH 2）m - 基，其中m为0,1,2或3，或支链C 2 -C 5亚烷基，其中基团C的亚甲基-CH 2可以被氧或硫原子或羟基亚甲基 基团-CHOH-或羰基-CO-，B是1,2-，1,3-，1,4-亚环己基或1,2-或 1,3-亚环戊基。

    Sulphonamidocycloalkane compounds, pharmaceutical compositions containing them, and methods of use thereof
    3.
    发明授权
    Sulphonamidocycloalkane compounds, pharmaceutical compositions containing them, and methods of use thereof 失效
    磺酰氨基环烷烃化合物，含有它们的药物组合物及其使用方法

    公开(公告)号：US5407951A

    公开(公告)日：1995-04-18

    申请号：US906339

    申请日：1992-06-30

    申请人： Ernst-Christian Witte ,  Karlheinz Stegmeier ,  Liesel Doerge

    发明人： Ernst-Christian Witte ,  Karlheinz Stegmeier ,  Liesel Doerge

    IPC分类号： A61K31/18 ,  A61K31/195 ,  A61K31/22 ,  A61K31/41 ,  A61P1/04 ,  A61P3/00 ,  A61P7/02 ,  A61P9/00 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/28 ,  C07C311/19 ,  C07C323/65 ,  C07D257/04 ,  C07D257/06 ,  C07C311/16 ,  C07C311/17

    CPC分类号： C07D257/04 ,  C07C311/19 ,  C07D257/06 ,  C07C2101/14

    摘要： The present invention provides sulphonamides of the general formula: ##STR1## wherein R.sup.1 and R.sup.2, which can be the same or different, are hydrogen or halogen atoms or C.sub.1 -C.sub.6 -alkyl, trifluoro-methyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, N-alkylaminocarbonyl or N,N-dialkylaminocarbonyl radicals or, when R.sup.1 and R.sup.2 are alkyl radicals ortho to one another, R.sup.1 and R.sup.2 together with the carbon atoms to which they are attached, form a saturated or unsaturated C.sub.5-C.sub.7 -alkylene ring, R.sup.3 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical, a phenylalkyl or phenylalkenyl radical, the phenyl moiety of which can be substituted by halogen, alkyl or trifluoromethyl, C is a --(CH.sub.2).sub.m --radical, in which m is 0, 1, 2 or 3, or a branched C.sub.2 -C.sub.5 -alkylene radical, whereby a methylene radical --CH.sub.2 --of the group C can be replaced by an oxygen or sulphur atom or by a hydroxymethylene radical --CHOH--or carbonyl group --CO--, B is a 1,2-, 1,3-, 1,4-cyclohexylidene or 1,2- or 1,3-cyclopentylidene radical.

    摘要翻译： 本发明提供通式如下的磺酰胺：其中R 1和R 2可以相同或不同，为氢或卤素原子或C 1 -C 6烷基，三氟甲基，氰基，羧基，烷氧基羰基 ，氨基羰基，N-烷基氨基羰基或N，N-二烷基氨基羰基，或者当R 1和R 2是彼此邻位的烷基时，R 1和R 2与它们所连接的碳原子一起形成饱和或不饱和的C 5 -C 7 - 亚烷基环，R 3是氢原子，含有至多6个碳原子的烷基，酰基，苯基烷基或苯基烯基，其苯基部分可以被卤素，烷基或三氟甲基取代，C是 - （CH 2 ）m-基，其中m为0,1,2或3，或支链C 2 -C 5 - 亚烷基，其中基团C的亚甲基-CH 2可以被氧或硫原子替代，或由 羟基亚甲基-CHOH-或羰基-CO-，B是1,2-，1,3-，1,4-亚环己基或1,2-或1， 3-环戊基。

    Sulfonamides of phenylalkylamines or phenoxyalkylamines processes for their preparation and medicaments containing these compounds
    4.
    发明授权
    Sulfonamides of phenylalkylamines or phenoxyalkylamines processes for their preparation and medicaments containing these compounds 失效
    苯基烷基胺或苯氧基烷基胺的磺酰胺用于制备它们和含有这些化合物的药物

    公开(公告)号：US5446065A

    公开(公告)日：1995-08-29

    申请号：US75489

    申请日：1993-06-21

    申请人： Ernst-Christian Witte ,  Hansjorg Beckh ,  Karlheinz Stegmeier ,  Liesel Doerge

    发明人： Ernst-Christian Witte ,  Hansjorg Beckh ,  Karlheinz Stegmeier ,  Liesel Doerge

    IPC分类号： C07C311/13 ,  C07C311/17 ,  C07C311/18 ,  C07C311/21 ,  C07C311/29 ,  C07C323/67 ,  C07D295/185 ,  A61K31/18

    CPC分类号： C07D295/185 ,  C07C311/17 ,  C07C311/18 ,  C07C2101/14

    摘要： Compounds of the formula I ##STR1## in which R.sub.1 signifies an aryl, aralkyl or an aralkenyl group, the aryl radical of which can, in each case, be substituted one or more times by halogen, cyano, alkyl, trifluoromethyl, alkoxy, alkylthio, trifluoromethoxy, hydroxyl or carboxyl, m a whole number from 1 to 3, n a whole number from 1 to 5, R.sub.2 hydrogen, an alkyl, aralkyl or acyl group, Q a bond or an oxygen atom, R.sub.3 hydrogen or a lower alkyl radical which is possibly terminally substituted by carboxyl or by a hydroxyl group and R.sub.4 hydrogen, a lower alkyl group with 1-4 C-atoms, which is possibly terminally substituted by carboxyl or hydroxyl, a possibly substituted phenyl, heteroaryl, cycloalkyl or acyl group or a group ##STR2## in which R.sub.5 represents a straight-chained or branched alkyl chain with 1-4 C-atoms which is possibly terminally substituted by carboxyl, alkoxycarbonyl, aminocarbonyl, hydroxyl, mercapto, alkylthio or imidazolyl and Y a carboxyl, an alkoxycarbonyl, aminocarbonyl or cyano, formyl, hydroxymethyl, aminomethyl or ortho ester group, whereby R.sub.3 and R.sub.4 can also be component of a 5- or 6-membered saturated or unsaturated possibly substituted heterocycle with 1-4 heteroatoms which can be annellated with further ring compounds via one or more bonds, as well as their salts, esters and amides, processes for their preparation and medicaments with thromboxane-antagonistic action which contain these compounds.

    摘要翻译： PCT No.PCT / EP91 / 02456 Sec。 371日期：1993年6月21日 102（e）日期1993年6月21日PCT 1991年12月19日PCT公布。 出版物WO92 / 日期：1992年7月9日。式Ⅰ化合物（Ⅰ）其中R1表示芳基，芳烷基或芳烯基，其芳基可以在每种情况下被卤素取代一次或多次 氰基，烷基，三氟甲基，烷氧基，烷硫基，三氟甲氧基，羟基或羧基，整数为1至3，na整数1至5，R 2氢，烷基，芳烷基或酰基，Q a键或氧 原子，R3氢或可能被羧基或羟基末端取代的低级烷基，R4为氢原子，可被羧基或羟基末端取代的具有1-4个C原子的低级烷基，可能被取代 苯基，杂芳基，环烷基或酰基或基团，其中R 5表示具有1-4个C原子的直链或支链烷基链，其可以被羧基末端取代，烷氧基羰基，氨基羰基，羟基，巯基，烷硫基 或咪唑基，Y是羧基，烷氧基羰基 1，氨基羰基或氰基，甲酰基，羟甲基，氨基甲基或原酸酯基，其中R3和R4也可以是具有1-4个杂原子的5或6元饱和或不饱和可能取代的杂环的组分，其可以与另外的环 通过一个或多个键的化合物，以及它们的盐，酯和酰胺，其制备方法和含有这些化合物的血栓烷拮抗作用的药物。

    Sulphonamides containing a tetrazolyl radical
    9.
    发明授权
    Sulphonamides containing a tetrazolyl radical 失效
    含有四唑基的磺酰胺

    公开(公告)号：US5037990A

    公开(公告)日：1991-08-06

    申请号：US401317

    申请日：1989-08-31

    申请人： Hansjorg Beckh ,  Ernst-Christian Witte ,  Karlheinz Stegmeier ,  Leisel Doerge

    发明人： Hansjorg Beckh ,  Ernst-Christian Witte ,  Karlheinz Stegmeier ,  Leisel Doerge

    IPC分类号： A61K31/41 ,  A61P7/02 ,  A61P43/00 ,  C07D257/04 ,  C07D257/06

    CPC分类号： C07D257/04 ,  C07D257/06

    摘要： The present invention provides sulphonamides of the general formula: ##STR1## wherein R is a hydrogen or halogen arom, a cyano group or a C.sub.1 -C.sub.6 -alkyl or trifluoromethyl radical, n is 1, 2 or 3, m is 0 or 1 to 5, X is a valency bond, an oxygen atom, a carbonyl group or a --CHOH-- group, A is a valency bond or a carbonyl group and B is a valency bond or an --NH-- group; the physiologically acceptable salts thereof with inorganic and organic acids, as well as the optical isomers thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.

    摘要翻译： 本发明提供了下列通式的磺酰胺：其中R是氢或卤素芳基，氰基或C 1 -C 6烷基或三氟甲基，n是1,2或3， m为0或1〜5，X为价键，氧原子，羰基或-CHOH-基，A为价键或羰基，B为价键或-NH-基; 其与无机和有机酸的生理上可接受的盐以及其旋光异构体。 本发明还提供了制备这些化合物的方法和含有它们的药物组合物。

    Sulphonylalkylamines, processes for the preparation thereof and pharmaceutical compositions containing them
    10.
    发明授权
    Sulphonylalkylamines, processes for the preparation thereof and pharmaceutical compositions containing them 失效
    磺酰基烷基胺，其制备方法和含有它们的药物组合物

    公开(公告)号：US4948809A

    公开(公告)日：1990-08-14

    申请号：US281955

    申请日：1988-12-05

    申请人： Ernst-Christian Witte ,  Hans-Peter Wolff ,  Karlheinz Stegmeier ,  Johannes Pill

    发明人： Ernst-Christian Witte ,  Hans-Peter Wolff ,  Karlheinz Stegmeier ,  Johannes Pill

    IPC分类号： A61K31/655 ,  A61K31/18 ,  A61K31/185 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K31/275 ,  A61P1/04 ,  A61P7/02 ,  A61P9/00 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P43/00 ,  C07C67/00 ,  C07C301/00 ,  C07C303/38 ,  C07C303/40 ,  C07C311/00 ,  C07C311/15 ,  C07C311/16 ,  C07C311/17 ,  C07C311/29 ,  C07C311/39 ,  C07D307/33

    CPC分类号： C07D307/33 ,  C07C309/00

    摘要： The present invention provides sulphonylphenylalkylamines of the general formula: ##STR1## wherein R.sub.1 is an alkyl radical containing up to 6 carbon atoms, a cycloalkyl radical containing 3-7 carbon atoms or an aralkyl, aralkenyl or aryl radical, the aryl moiety, in each case, being optionally substituted one or more times by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino, C.sub.1 -C.sub.6 acylamino, C.sub.1 -C.sub.16 acyl or azide, R.sub.2 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical or an aralkyl or aralkenyl radical, the aryl moiety, in each case, optionally being substituted one or more times by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, trifluoromethyl, cyano, nitro, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.1 -C.sub.12 dialkylamino, C.sub.1 -C.sub.6 acylamino, C.sub.1 -C.sub.16 acyl or azide, B is an unbranched or branched alkylene chain with a maximum of 4 carbon atoms and A an alkyl or alkenyl radical containing up to 6 carbon atoms, a C.sub.1 -C.sub.6 formylalkyl radical, a C.sub.1 -C.sub.6 hydroxy-alkyl group or a radical --D--R.sub.3, in which D is a ##STR2## and R.sub.3 is a hydrogen atom, a C.sub.1 -C.sub.5 alkyl, a C.sub.1 -C.sub.5 hydroxyalkyl or a C.sub.1 -C.sub.5 alkylcarboxylic acid radical, as well as the pharmacologically acceptable salts thereof, the esters and amides thereof and the lactones of those compounds which contain a hydroxyl and a carboxyl group, with the exception of the compound benzene-sulphonic acid-(4-acetylphenethylamide).The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.

    摘要翻译： 本发明提供通式如下的磺酰基苯基烷基胺：其中R 1是含有至多6个碳原子的烷基，含有3-7个碳原子的环烷基或芳烷基，芳烯基或芳基，芳基部分 任选被卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，三氟甲基，氰基，硝基，氨基，C 1 -C 6烷基氨基，C 2 -C 12二烷基氨基，C 1 -C 6酰基氨基， C1-C16酰基或叠氮化物，R2是氢原子，含有至多6个碳原子的烷基，酰基或芳烷基或芳烯基，芳基部分，在每种情况下，任选被卤素取代一次或多次 ，C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，三氟甲基，氰基，硝基，氨基，C 1 -C 6烷基氨基，C 1 -C 12二烷基氨基，C 1 -C 6酰氨基，C 1 -C 16酰基或叠氮基，B是无支链或支链亚烷基 具有最多4个碳原子的链，A是含有至多6个碳的烷基或烯基 原子，C 1 -C 6甲酰基烷基，C 1 -C 6羟基烷基或基团-D-R 3，其中D是R 3，R 3是氢原子，C 1 -C 5烷基，C 1 -C 5 羟基烷基或C1-C5烷基羧酸基团，以及其药理学上可接受的盐，其中含有羟基和羧基的那些化合物的酯和酰胺和内酯，除了化合物苯磺酸 - （4-乙酰苯乙胺）。 本发明还提供了制备这些化合物的方法和含有它们的药物组合物。