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1. 发明授权

US4590291A Thrombin inhibitory new dihydroxybenzene ether derivatives 失效
标题翻译：凝血酶抑制新二羟基苯醚衍生物
公开(公告)号：US4590291A
公开(公告)日：1986-05-20
申请号：US385355
申请日：1982-06-07
申请人： Horst Boshagen , Ulrich Horlein , Gerd Reinhardt , Friedel Seuter , Elisabeth Perzborn
发明人： Horst Boshagen , Ulrich Horlein , Gerd Reinhardt , Friedel Seuter , Elisabeth Perzborn
IPC分类号： C07C69/92 , A61K31/085 , A61P7/02 , A61P9/08 , A61P9/10 , C07C41/00 , C07C43/17 , C07C43/20 , C07C43/225 , C07C51/00 , C07C59/31 , C07C59/64 , C07C59/68 , C07C59/90 , C07C65/24 , C07C65/40 , C07C67/00 , C07C69/736 , C07C69/76 , C07C313/00 , C07C323/20
CPC分类号： C07C65/24 , C07C59/68 , C07C59/90 , C07C65/40
摘要： An ether derivative of a dihydroxybenzene of the formula ##STR1## in which R.sup.1 is 1 to 3 identical or different substituents selected from hydrogen, halogen, trifluoromethyl, carboxyl, alkyl, alkoxy, alkylmercapto and carbalkoxy, with in each case 1 to 4 carbon atoms in the alkyl and alkoxy groups, andR.sup.2 and R.sup.3 are different and each is an alkyl or alkenyl chain in which 1 or 2 CH.sub.2 chain members are optionally replaced by O, S, CO or a phenylene group, and/or in which the chain is optionally substituted by 1 to 3 identical or different substituents selected from hydroxyl, halogen, trifluoromethyl, phenyl, carboxyl, alkyl, alkoxy, alkylmercapto, carbalkoxy, and acyl, the phenyl radical in turn optionally being substituted by halogen, trifluoromethyl, carboxyl, alkyl, alkoxy, alkylmercapto or carbaloxy, and the abovementioned alkyl, alkoxy and acyl groups in each case containing 1 to 4 carbon atoms, and in which at least one of the radicals R.sup.2 or R.sup.3 is substituted and/or in at least one of the radicals R.sup.2 or R.sup.3 1 or 2 chain members are replaced by 1 or 2 identical or different radicals selected from O, S, CO and phenylene, is effective in combating cardiac infarcations, angina pectoric, thromboembolic illnesses, in venous and arterial regions and arteriosclerosis.
摘要翻译：其中R 1是1至3个相同或不同的选自氢，卤素，三氟甲基，羧基，烷基，烷氧基，烷基巯基和烷氧基的取代基的式“IMAGE”的二羟基苯的醚衍生物，在每种情况下为1至4个碳原子在烷基和烷氧基中，且R 2和R 3不同，并且各自为烷基或烯基链，其中1或2个CH 2链成员任选被O，S，CO或亚苯基取代，和/或其中链任选地被1至3个相同或不同的选自羟基，卤素，三氟甲基，苯基，羧基，烷基，烷氧基，烷基巯基，烷氧基和酰基的取代基取代，苯基依次任选被卤素，三氟甲基，羧基，烷基，烷氧基，烷基巯基或卡巴氧基，以及上述烷基，烷氧基和酰基，每种情况下含有1至4个碳原子，并且其中至少一个基团R 2或R 3被取代和/或至少一个o 基团R 2或R 3 1或2链成员被选自O，S，CO和亚苯基的1或2个相同或不同的基团取代，有效地对抗静脉和动脉区域的心脏梗塞，心绞痛，血栓栓塞性疾病，以及动脉硬化。

2. 发明授权

US4904797A Process of preparing cycloalkano(1,2-B)indole-sulphonamides 失效
标题翻译：制备环烷（1,2-B）吲哚磺酰胺的方法
公开(公告)号：US4904797A
公开(公告)日：1990-02-27
申请号：US308152
申请日：1989-02-08
申请人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
发明人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
IPC分类号： A61K31/40 , A61K31/403 , A61P7/02 , A61P11/00 , A61P37/08 , C07D209/80 , C07D209/86 , C07D209/88 , C07D209/94 , C07D491/10
CPC分类号： C07D209/80 , C07D209/86 , C07D209/88 , C07D491/10
摘要： Cycloalkano[1,2-b]indole-sulphonamides of the formula ##STR1## where appropriate in an isomeric form, and their salts are disclosed. These compounds are useful to inhibit platelet aggregation and to antagonize thromboxane A.sub.2.

3. 发明授权

US4774240A N-indolylethyl-sulphonic acid amides and their use 失效
标题翻译： N-吲哚基乙磺酸酰胺及其用途
公开(公告)号：US4774240A
公开(公告)日：1988-09-27
申请号：US852475
申请日：1986-04-14
申请人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
发明人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/41 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/47 , A61K31/64 , A61P7/02 , A61P11/00 , A61P37/08 , C07D209/14 , C07D209/16 , C07D209/34 , C07D333/00 , C07D401/12 , C07D409/12 , C07D417/12 , C07D521/00
CPC分类号： C07D401/12 , C07D209/16 , C07D409/12 , C07D417/12
摘要： The invention relates to N-indolylethyl-sulphonic acid amides of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are defined in the specification and X is carboxyl, alkoxycarbonyl, cyano or carboxamido. These active compounds are useful in medicaments in combating thromboses, thromboembolisms, allergies or asthmatic disorders.
摘要翻译：本发明涉及式（I）所示的N-吲哚基乙磺酸酰胺，其中R 1，R 2，R 3，R 4和R 5在本说明书中定义，X为羧基，烷氧基羰基，氰基或甲酰胺基。这些活性化合物可用于对抗血栓形成，血栓栓塞，过敏或哮喘性疾病的药物中。

4. 发明授权

US4882353A Chroman derivatives for combating thrombosis and asthma 失效
标题翻译：用于对抗血栓形成和哮喘的色甘衍生物
公开(公告)号：US4882353A
公开(公告)日：1989-11-21
申请号：US263143
申请日：1988-10-26
申请人： Ulrich Niewohner , Franz-Peter Hoever , Folker Lieb , Hermann Oediger , Ulrich Rosentreter , Horst Boshagen , Elisabeth Perzborn , Volker-Bernd Fiedler , Friedel Seuter
发明人： Ulrich Niewohner , Franz-Peter Hoever , Folker Lieb , Hermann Oediger , Ulrich Rosentreter , Horst Boshagen , Elisabeth Perzborn , Volker-Bernd Fiedler , Friedel Seuter
IPC分类号： A61K31/35 , A61K31/352 , A61P7/02 , C07D311/58 , C07D311/60 , C07D311/64 , C07D311/68 , C07D311/96
CPC分类号： C07D311/96 , C07D311/58 , C07D311/60 , C07D311/64 , C07D311/68
摘要： For inhibiting thombocyte aggregation, vasodilating and bronchodilating, the new chroman derivatives of the formula ##STR1## in which R.sup.1 stands for hydrogen, halogen, alkyl, hydroxyl, alkoxy, trifluoromethyl or cyano,R.sup.2 and R.sup.3 are identical or different and stand for hydrogen, alkyl, cycloalkyl or aryl,R.sup.4 stands for hydroxyl, alkoxy, aryloxy, aralkoxy or for a group of the formula --NR.sup.5 R.sup.6, whereR.sup.5 and R.sup.6 are identical or different and in each case denote hydrogen, alkyl, aryl or aralkyl,X denotes a direct bond or an oxygen or sulphur atom, NH or N-alkyl, andn denotes 0 or 1,and their physiologically tolerable salts. Also new intermediates of the formulas ##STR2##
摘要翻译：为了抑制血管细胞聚集，血管扩张和支气管扩张，式（Ⅰ）中R1代表氢，卤素，烷基，羟基，烷氧基，三氟甲基或氰基，R2和R3的新的苯并二氢吡喃衍生物是相同或不同的，对于氢，烷基，环烷基或芳基，R4代表羟基，烷氧基，芳氧基，芳烷氧基或式-NR5R6基团，其中R5和R6相同或不同，并且在每种情况下都表示氢，烷基，芳基或芳烷基， X表示直接键或氧或硫原子，NH或N-烷基，n表示0或1，以及它们的生理上可耐受的盐。（IMA）>（IV）的新中间体

5. 发明授权

US4853406A Polyhydrobenzi[c,d]indolesulphonamides 失效
标题翻译：聚氢化苯并[c，d]吲哚磺酰胺
公开(公告)号：US4853406A
公开(公告)日：1989-08-01
申请号：US200342
申请日：1988-05-31
申请人： Ulrich Rosentreter , Horst Boshagen , Folker Lieb , Hermann Oediger , Ulrich Niewohner , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
发明人： Ulrich Rosentreter , Horst Boshagen , Folker Lieb , Hermann Oediger , Ulrich Niewohner , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
IPC分类号： A61K31/40 , A61K31/403 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/08 , A61P37/08 , C07D209/90
CPC分类号： C07D209/90
摘要： Thrombocyte aggregation-inhibiting polyhydrobenz[c,d]indolesulphonamide of the formula ##STR1## in which R.sup.1 is hydrogen, aryl or alkyl,R.sup.2 is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, hydroxyl, aralkoxy ora group of the formula ##STR2## R.sup.3 and R.sup.4 each independently is hydrogen, alkyl, aryl, aralkyl or acyl andX is cyano or carboxyl, and salts thereof. Intermediates therefor of the formula ##STR3## are also new.
摘要翻译： R 1为氢，芳基或烷基，R 2为氢，卤素，烷基，烷氧基，三氟甲基，三氟甲氧基，羟基，芳烷氧基或基团的式（I）的血小板聚集抑制性多羟基苯并[c，d]吲哚磺酰胺式R 3和R 4各自独立地为氢，烷基，芳基，芳烷基或酰基，X为氰基或羧基，及其盐。具有公式（II）的中间体也是新的。

6. 发明授权

US4965258A Cycloalkano(1,2-B)indole-sulphonamides, pharmaceutical compositions and use 失效
标题翻译：环烯烃（1,2-B）吲哚磺酰胺，药物组合物和用途
公开(公告)号：US4965258A
公开(公告)日：1990-10-23
申请号：US442043
申请日：1989-11-28
申请人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
发明人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
IPC分类号： A61K31/40 , A61K31/403 , A61P7/02 , A61P11/00 , A61P37/08 , C07D209/80 , C07D209/86 , C07D209/88 , C07D209/94 , C07D491/10
CPC分类号： C07D209/80 , C07D209/86 , C07D209/88 , C07D491/10
摘要： Cycloalkano[1,2-b]indole-sulphonamides of the formula ##STR1## where appropriate in an isomeric form, and their salts are disclosed. These compounds are useful to inhibit platelet aggregation and to antoganize thromboxane A.sub.2.

7. 发明授权

US4988820A Cycloalkano(1,2-B) indole-sulponamides 失效
标题翻译：环咯烷（1,2-B）吲哚磺胺
公开(公告)号：US4988820A
公开(公告)日：1991-01-29
申请号：US556592
申请日：1990-07-20
申请人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
发明人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
IPC分类号： C07D209/80 , C07D209/86 , C07D209/88 , C07D491/10
CPC分类号： C07D209/80 , C07D209/86 , C07D209/88 , C07D491/10
摘要： Cycloalkano[1,2-b]indole-sulphonamides of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, trifluoromethyl, carboxyl or alkoxycarbonyl, represents a group of the formula --S(O).sub.m R.sup.3, in which R.sup.3 denotes alkyl or aryl, and m denotes one of the numbers 0, 1 or 2, represents a group of the formula ##STR2## in which R.sup.4 and R.sup.5 are identical or different and represent hydrogen, alkyl, aryl, aralkyl or acetyl, represents a group of the formula --OR.sup.6, in which R.sup.6 denotes hydrogen, alkyl, aryl, aralkyl, alkyl-SO.sub.2 --, aryl--SO.sub.2 --, aralkyl--SO.sub.2 -- or trifluoromethyl, or represents alkyl, alkenyl or cycloalkyl, each of which is optionally substituted by carboxyl, alkoxycarbonyl, halogen, hydroxyl, alkoxy, alkylthio or cyano, R.sup.2 represents aryl which is optionally substituted up to 5 times by halogen, cyano, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, alkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxy, alkylthio, hydroxyl, carboxyl, alkoxycarbonyl, phenyl, phenoxy, benzyloxy, benzylthio or a group of the formula ##STR3## in which R.sup.4 and R.sup.5 have the abovementioned meaning, x represents the number 1, 2 or 3, and y represents the number 0 or 1, where appropriate in an isomeric form, and their salts are disclosed. These compounds are useful to inhibit platelet aggregation and to antagonize thromboxane A.sub.2.
摘要翻译：其中R 1表示氢，卤素，三氟甲基，羧基或烷氧基羰基的式[IMAGE]的环烷基[1,2-b]吲哚磺酰胺代表式-S（O）m R 3的基团，其中R 3表示烷基或芳基，m表示数字0,1或2中的一个，表示其中R 4和R 5相同或不同并且表示氢，烷基，芳基，芳烷基或乙酰基的式“IMAGE”的基团，表示其中R 6表示氢，烷基，芳基，芳烷基，烷基-SO 2 - ，芳基-SO 2 - ，芳烷基-SO 2 - 或三氟甲基，或表示烷基，烯基或环烷基，其各自任选被羧基，氰基，三氟甲基，三氟甲氧基，三氟甲硫基，烷基，羧基烷基，烷氧基羰基烷基，烷氧基，烷硫基，羟基，羧基，烷氧基羰基，烷氧基羰基，烷硫基，苯基，苯氧基，苄氧基，苄硫基或其中R 4和R 5具有上述含义的式“IMAGE”的基团，x表示数字1,2或3，并且y代表数字0或1，其中适当的是异构体形式，并且其公开的盐。这些化合物可用于抑制血小板聚集和拮抗血栓素A2。

8. 发明授权

US4843091A Indolylpropionic acids, compositions of, and use thereof to inhibit thrombocyte aggregation 失效
标题翻译：吲哚丙酸，其组合物及其用途，用于抑制血小板聚集
公开(公告)号：US4843091A
公开(公告)日：1989-06-27
申请号：US58489
申请日：1987-06-05
申请人： Ulrich Rosentreter , Horst Boshagen , Folker Lieb , Hermann Oediger , Volker-Bernd Fiedler , Elisabeth Perzborn , Friedel Seuter
发明人： Ulrich Rosentreter , Horst Boshagen , Folker Lieb , Hermann Oediger , Volker-Bernd Fiedler , Elisabeth Perzborn , Friedel Seuter
IPC分类号： A61K31/403 , A61K31/404 , A61K31/405 , A61P7/02 , C07D209/08 , C07D209/18 , C07D209/24 , C07D401/04 , C07D405/04 , C07D409/04
CPC分类号： C07D401/04 , C07D209/08 , C07D209/24 , C07D405/04 , C07D409/04
摘要： An N-sulphonamidoethyl-indole of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl, alkoxy, alkylthio, halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, difluoromethoxy, aryl, arylthio, aralkyl, aralkoxy, aralkylthio, acyl or a group of the formula ##STR2## in which R.sup.5 and R.sup.6 are identical or different and denote hydrogen, alkyl, aryl, aralkyl or acyl, andR.sup.3 represents hydrogen, alkyl, aryl, pyridyl, thienyl or furyl, andR.sup.4 represents hydrogen, alkyl, alkoxy, alkylthio, halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, aryl, aryloxy, arylthio, aralkyl, aralkoxy, aralkylthio, acl or a group of the formula ##STR3## in which R.sup.7 and R.sup.8 are identical or different and denote hydrogen, alkyl, aryl, aralkyl or acyl,R.sup.5 represents hydrogen, ##STR4## or a pharmacologically acceptable salt of ##STR5## and R.sup.2 represents hydrogen, alkyl or aryl.The compounds were R.sup.5 is ##STR6## or a salt thereof inhibit the aggregation of thrombocytes.
摘要翻译：其中R 1表示氢，烷基，烷氧基，烷硫基，卤素，三氟甲基，三氟甲氧基，三氟甲硫基，二氟甲氧基，芳基，芳硫基，芳烷基，芳烷氧基，芳烷硫基，酰基或一组基团的N-磺酰氨基乙基 - 吲哚式中，R 5和R 6相同或不同，表示氢，烷基，芳基，芳烷基或酰基，R 3表示氢，烷基，芳基，吡啶基，噻吩基或呋喃基，R 4表示氢，烷基，烷氧基，烷硫基卤素，三氟甲基，三氟甲氧基，三氟甲硫基，芳基，芳氧基，芳硫基，芳烷基，芳烷氧基，芳烷硫基，acl或其中R 7和R 8相同或不同并表示氢，烷基，芳基，芳烷基或酰基，R 5表示氢，或者是IMA IMA的药理学上可接受的盐，R 2表示氢，烷基或芳基。化合物是R5是抑制凝血细胞聚集的盐或其盐。

9. 发明授权

US4827032A Cycloalkyl-one-containing benzenesulphonamides 失效
标题翻译：含环烷基一的苯磺酰胺
公开(公告)号：US4827032A
公开(公告)日：1989-05-02
申请号：US212840
申请日：1988-06-29
申请人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
发明人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Friedel Seuter , Elisabeth Perzborn , Volker-Bernd Fiedler
IPC分类号： A61K31/40 , A61K31/403 , A61P7/02 , A61P11/00 , A61P37/08 , C07D209/80 , C07D209/86 , C07D209/88 , C07D209/94 , C07D491/10 , C07C143/78
CPC分类号： C07D209/80 , C07D209/86 , C07D209/88 , C07D491/10
摘要： Cycloalkanol[1,2-b]indole-sulphonamides of the formula ##STR1## where appropriate in an isomeric form, and their salts are disclosed. These compounds are useful to inhibit platelet aggregation and to antagonize thromboxane A.sub.2.
摘要翻译：公开了具有异构体形式的合适的式“IMAGE”的环烷醇[1,2-b]吲哚磺酰胺及其盐。这些化合物可用于抑制血小板聚集和拮抗血栓素A2。

10. 发明授权

US4806551A N-dihydroindolylethyl-sulphonamides 失效
标题翻译： N-二氢吲哚基乙基磺酰胺
公开(公告)号：US4806551A
公开(公告)日：1989-02-21
申请号：US39395
申请日：1987-04-16
申请人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Volker-Bernd Fiedler , Elisabeth Perzborn , Friedel Seuter
发明人： Horst Boshagen , Ulrich Rosentreter , Folker Lieb , Hermann Oediger , Volker-Bernd Fiedler , Elisabeth Perzborn , Friedel Seuter
IPC分类号： C07D209/14 , A61K31/40 , A61K31/403 , A61K31/404 , A61P7/02 , C07D209/16 , C07D209/34
CPC分类号： C07D209/16
摘要： New N-dihydroindolylethyl-sulphonamides are prepared from the corresponding N-indolylethyl-sulphonamides by oxidation or hydrogenation and are useful as active compounds in medicaments. These compounds exhibit a platelet aggregation-inhibiting and thromboxan A.sub.2 -antagonistic action.The N-dihydroindolylethyl-sulphonamides have the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, trifluoromethyl, carboxyl or alkoxycarbonyl, or represents a group of the formula --S(O).sub.m R.sup.5,whereinR.sup.5 denotes alkyl or aryl andm denotes one of the numbers 0, 1 or 2, orR.sup.1 represents a group of the formula ##STR2## or R.sup.1 represents a group of the formula --OR.sup.8, orR.sup.1 represents optionally substituted alkyl, alkenyl or cycloalkyl,R.sup.2 represents aryl, which is optionally substituted by up to 5 substituents,R.sup.3 represents hydrogenor alkyl andR.sup.4 represents hydrogen, orR.sup.3 and R.sup.4 together bond a carbonyl oxygen.
摘要翻译：通过氧化或氢化由相应的N-吲哚基乙基磺酰胺制备新的N-二氢吲哚基乙基磺酰胺，并且可用作药物中的活性化合物。这些化合物表现出血小板聚集抑制和血栓素A2拮抗作用。 N-二氢吲哚基乙基磺酰胺具有式“IMAGE”，其中R 1表示氢，卤素，三氟甲基，羧基或烷氧基羰基，或表示式-S（O）m R 5的基团，其中R 5表示烷基或芳基，m表示一个数字0,1或2，或者R1表示式“IMAGE”或R1表示式-OR8的基团，或R1表示任选取代的烷基，烯基或环烷基，R 2表示芳基，其任选被取代最多5个取代基，R 3表示氢或烷基，R 4表示氢，或者R 3和R 4一起键合羰基氧。

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