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1. 发明授权

US4258058A Phenoxyalkylcarboxylic acid compounds and thrombocyte-aggregation inhibition 失效
标题翻译：苯氧基烷基羧酸化合物和血小板聚集抑制作用
公开(公告)号：US4258058A
公开(公告)日：1981-03-24
申请号：US15536
申请日：1979-02-26
申请人： Ernst-Christian Witte , Hans P. Wolff , Max Thiel , Karlheinz Stegmeier , Egon Roesch
发明人： Ernst-Christian Witte , Hans P. Wolff , Max Thiel , Karlheinz Stegmeier , Egon Roesch
IPC分类号： A61K31/19 , A61K31/165 , A61K31/195 , A61K31/22 , A61P3/06 , A61P7/02 , C07C67/00 , C07C301/00 , C07C303/38 , C07C303/40 , C07C311/03 , C07C311/04 , C07C311/06 , C07C311/14 , C07C311/16 , C07C311/17 , C07C311/29 , C07D209/48 , C07C143/78 , A61K31/24
CPC分类号： C07D209/48
摘要： Phenoxyalkylcarboxylic acid compounds of the formula ##STR1## wherein R is hydrogen or lower alkylR.sub.1 is alkyl or aryl, aralkyl or aralkenyl radical, the aryl moiety of which can be substituted one or more times by halogen, hydroxyl, trifluoromethyl or lower alkyl, alkoxy or acylR.sub.2 and R.sub.3 are individually selected from hydrogen or lower alkyl, andn is 0, 1, 2 or 3and the physiologically acceptable salts, esters and amides thereof; are outstandingly effective in inhibiting thrombocyte aggregation.
摘要翻译：其中R为氢或低级烷基R 1的苯氧基烷基羧酸化合物为烷基或芳基，芳烷基或芳烯基，其芳基部分可被卤素，羟基，三氟甲基或低级烷基烷氧基取代一次或多次或酰基R2和R3分别选自氢或低级烷基，n为0,1,2或3及其生理上可接受的盐，酯和酰胺; 在抑制血小板聚集方面效果显着。

2. 发明授权

US4153728A Phenoxyalkylcarboxylic acid compounds and therapeutic compositions 失效
标题翻译：苯氧基烷基羧酸化合物和治疗组合物
公开(公告)号：US4153728A
公开(公告)日：1979-05-08
申请号：US733542
申请日：1976-10-18
申请人： Hans P. Wolff , Ernst-Christian Witte , Max Thiel , Harald Stork , Egon Roesch
发明人： Hans P. Wolff , Ernst-Christian Witte , Max Thiel , Harald Stork , Egon Roesch
IPC分类号： A61K31/215 , A61K20060101 , A61K31/16 , A61K31/19 , A61K31/22 , A61P3/06 , A61P7/02 , C07C20060101 , C07C51/00 , C07C59/68 , C07C67/00 , C07C69/734 , C07C69/76 , C07C231/00 , C07C231/02 , C07C231/12 , C07C235/34 , C07C235/48 , C07C101/42 , A01N9/20
CPC分类号： C07C2101/14 , Y10S514/824
摘要： Novel phenoxyalkylcarboxylic acid compounds of the formula ##STR1## wherein B is a valency bond or a straight-chained or branched, saturated or unsaturated hydrocarbon radical containing up to 3 carbon atoms;N is 1 or 2 andR.sub.1, r.sub.2 and R.sub.3 are hydrogen or lower alkyl; and the pharmacologically compatible salts thereof; have been found to be outstandingly effective in lowering the serum lipid level and the cholesterol level in mammals without inducing undesired side effects and to possess excellent thrombocyte-aggregation inhibiting activity.
摘要翻译：式（I）的新型苯氧基烷基羧酸化合物，其中B是含有至多3个碳原子的价键或直链或支链，饱和或不饱和的烃基; N 1 OR 2，R 1，R 2和R 3为氢或低级烷基; 和其药理学上相容的盐; 已被发现在降低哺乳动物血清脂质水平和胆固醇水平而没有诱导不期望的副作用并且具有优异的血小板聚集抑制活性方面是非常有效的。

3. 发明授权

US4443477A Sulphonamidophenylcarboxylic acid compounds and pharmaceutical compositions containing them 失效
标题翻译：磺酰氨基苯基羧酸化合物和含有它们的药物组合物
公开(公告)号：US4443477A
公开(公告)日：1984-04-17
申请号：US395882
申请日：1982-07-07
申请人： Ernst-Christian Witte , Hans P. Wolfe , Karlheinz Stegmeier , Egon Roesch
发明人： Ernst-Christian Witte , Hans P. Wolfe , Karlheinz Stegmeier , Egon Roesch
IPC分类号： A61K31/18 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/235 , A61P3/06 , A61P7/02 , A61P9/10 , C07C67/00 , C07C301/00 , C07C303/38 , C07C303/40 , C07C311/00 , C07C311/06 , C07C311/19 , C07C143/78
CPC分类号： C07C311/00
摘要： The invention provides sulphonamides of the formula ##STR1## wherein R is a hydrogen atom or a lower alkyl radical;R.sub.1 is alkyl, aryl, aralkyl or aralkenyl, the aryl moiety of which in each case can be optionally substituted one or more times by hydroxyl, halogen, trifluoromethyl, lower alkyl or alkoxy or by acyl, carboxy or alkoxycarbonyl;n is 1, 2 or 3; andW is a valence bond or a divalent aliphatic hydrocarbon linkageand the physiologically acceptable salts, esters and amides of such compound. These compounds have excellent pharmacological lipid depressing activity and inhibit thrombocyte aggregation.
摘要翻译：本发明提供了式（I）的磺酰胺，其中R是氢原子或低级烷基; R 1是烷基，芳基，芳烷基或芳烯基，其芳基部分可以任选被羟基，卤素，三氟甲基，低级烷基或烷氧基取代或被酰基，羧基或烷氧基羰基取代一次或多次; n为1,2或3; W是这种化合物的价键或二价脂族烃键和生理上可接受的盐，酯和酰胺。这些化合物具有优异的药理学抑郁活性和抑制血小板聚集。

4. 发明授权

US4151303A Phenoxyalkylcarboxylic acid compounds and serum-lipid and triglyceride depressing therapeutic compositions 失效
标题翻译：苯氧基烷基羧酸化合物和血清 - 脂质和甘油三酯抑制治疗组合物
公开(公告)号：US4151303A
公开(公告)日：1979-04-24
申请号：US719878
申请日：1976-09-01
申请人： Ernst-Christian Witte , Hans P. Wolff , Kurt Stach, deceased , Wolfgang Schaumann , Karlheinz Stegmeier
发明人： Ernst-Christian Witte , Hans P. Wolff , Kurt Stach, deceased , Wolfgang Schaumann , Karlheinz Stegmeier
IPC分类号： A61K31/22 , A61K31/19 , A61P3/06 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C233/12 , C07C233/19 , C07C233/22 , C07C235/20 , C07C101/42 , A01N9/20
CPC分类号： C07C233/12
摘要： Novel phenoxyalkylcarboxylic acid compounds of the formula ##STR1## wherein A is aryl, aryloxy, substituted aryl or substituted aryloxy, wherein the substituents are selected from lower alkyl, lower alkoxy, halogen and haloalkyl;B is a straight-chained or branched, saturated or unsaturated hydrocarbyl containing up to 5 carbon atoms;N is 1, 2 or 3 andR.sub.1, r.sub.2 and R.sub.3, which may be the same or different, are hydrogen or lower alkyl;And the pharmacologically compatible salts thereof; have been found to be outstandingly effective in depressing serum-lipid and triglycerides in the serum of mammals.
摘要翻译：式（I）的新型苯氧基烷基羧酸化合物，其中A是芳基，芳氧基，取代的芳基或取代的芳氧基，其中取代基选自低级烷基，低级烷氧基，卤素和卤代烷基; B是含有至多5个碳原子的直链或支链饱和或不饱和烃基; N IS 1，2 OR 3，R 1，R 2和R 3可以相同或不同，为氢或低级烷基; 及其药理学兼容性; 已被认为是非常有效地抑制血清中的血清和血清中的血清脂蛋白。

5. 发明授权

US3997667A 1-[3-(Naphth-1-yloxy)-propyl]-piperazine compounds and therapeutic compositions 失效
标题翻译： 1- {8- 3-（萘-1-基氧基） - 丙基{9-哌嗪化合物和治疗组合物
公开(公告)号：US3997667A
公开(公告)日：1976-12-14
申请号：US544721
申请日：1975-01-28
申请人： Ernst-Christian Witte , Kurt Stach , Max Thiel , Gisbert Sponer , Egon Roesch
发明人： Ernst-Christian Witte , Kurt Stach , Max Thiel , Gisbert Sponer , Egon Roesch
IPC分类号： C07D295/08 , C07D295/088 , C07D295/092 , C07D295/096
CPC分类号： C07D295/088
摘要： New 1-[3-naphth-1-yloxy)-propyl]-piperazine compounds of the formula: ##STR1## wherein X is hydrogen or methoxy;And the pharmacologically compatible salts thereof;Are outstandingly effective in lowering blood pressure and are thus useful as anti-hypertensive agents.
摘要翻译：新的1- [3-萘-1-基氧基） - 丙基] - 哌嗪化合物，其结构式如下：其中X是氢或甲氧基; 及其药理学兼容性; 在降低血液压力方面非常有效，并且有效地作为抗高血压药物。

6. 发明授权

US3997666A 1-[3-(Naphth-1-yloxy)-2-hydroxypropvl]-piperazine compounds and therapeutic compositions 失效
标题翻译： 1- {8- 3-（萘-1-基氧基）-2-羟基丙基{9-哌嗪化合物和治疗组合物
公开(公告)号：US3997666A
公开(公告)日：1976-12-14
申请号：US544719
申请日：1975-01-28
申请人： Ernst-Christian Witte , Kurt Stach , Max Thiel , Gisbert Sponer , Egon Roesch
发明人： Ernst-Christian Witte , Kurt Stach , Max Thiel , Gisbert Sponer , Egon Roesch
IPC分类号： C07D295/08 , A61K31/495 , A61P9/12 , C07D295/088 , C07D295/092 , C07D295/096
CPC分类号： C07D295/088
摘要： New 1-[3-(naphth-1-yloxy)-2-hydroxypropyl]-piperazine compounds of the formula: ##STR1## and the pharmacologically compatible salts thereof are outstandingly effective in lowering blood pressure and are thus useful as anti-hypertensive agents.
摘要翻译：具有下式的新的1- [3-（萘-1-基氧基）-2-羟丙基] - 哌嗪化合物及其药理学相容的盐在降低血压方面显着有效，因此可用作抗 - 高血压药物

7. 发明授权

US5446065A Sulfonamides of phenylalkylamines or phenoxyalkylamines processes for their preparation and medicaments containing these compounds 失效
标题翻译：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。

8. 发明授权

US4981873A Substituted sulphonamides, pharmaceuticals thereof and methods of using them 失效
标题翻译：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。

9. 发明授权

US5140038A Sulphonamidocycloalkane compounds, pharmaceutical compositions containing them, and methods of use thereof 失效
标题翻译：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。

10. 发明授权

US4997847A Biologically active compounds 失效
标题翻译：生物活性化合物
公开(公告)号：US4997847A
公开(公告)日：1991-03-05
申请号：US235061
申请日：1988-08-22
申请人： Robert J. Ife , David G. Cooper , Robert A. Slater , Karlheinz Stegmeier , Ernst-Christian Witte
发明人： Robert J. Ife , David G. Cooper , Robert A. Slater , Karlheinz Stegmeier , Ernst-Christian Witte
IPC分类号： A61K31/195 , A61K31/19 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/63 , A61P7/02 , C07C303/36 , C07C311/19 , C07C311/29 , C07D307/64 , C07D333/34
CPC分类号： A61K31/19 , A61K31/34 , A61K31/38 , A61K31/63 , C07D307/64 , C07D333/34
摘要： The invention relates to phenylsulphonamidolkanoic acids which have thromboxane A.sub.2 receptor antagonist activity.

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