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。

公开(公告)号：US5173500A

公开(公告)日：1992-12-22

申请号：US700976

申请日：1991-05-16

申请人： Hansjorg Beckh

发明人： Hansjorg Beckh

IPC分类号： C07D257/04 ,  C07D257/06

CPC分类号： C07D257/04 ,  C07D257/06 ,  Y10S514/822

摘要： The present invention provides sulphonamides of the general formula: ##STR1## wherein R is a hydrogen or halogen atom, 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： 本发明提供了通式如下的磺酰胺：其中R是氢或卤素原子，氰基或C 1 -C 6烷基或三氟甲基，n是1,2或3，m是0 或1至5，X是价键，氧原子，羰基或-CHOH-基团，A是价键或羰基，B是价键或-NH-基团; 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。

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。