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1. 发明授权

US5079258A Tetrahydro-1-benz-(C,D)-indolepropionic acid sulphonamides as thrombocyte aggregation inhibitors 失效
标题翻译：四氢叶酸1-苄基 - （C，D） - 亚磷酸磺酰胺作为血栓聚集抑制剂
公开(公告)号：US5079258A
公开(公告)日：1992-01-07
申请号：US384531
申请日：1989-07-24
申请人： Horst Boshagen , Ulrich Rosentreter , Elisabeth Perzborn , Volker-Bernd Fiedler
发明人： Horst Boshagen , Ulrich Rosentreter , Elisabeth Perzborn , Volker-Bernd Fiedler
IPC分类号： A61K31/403 , A61K31/405 , A61P7/02 , C07D209/90 , C07D405/04
CPC分类号： C07D209/90
摘要： Tetrahydro-1-benz-[c,d],indolepropionic acid sulphonamides of the formula ##STR1## can be prepared by reaction of tetrahydro-1-benz-[c,d]-indolesulphonamides with acrylonitrile and subsequent hydrolysis. The new compounds can be employed inhibiting thrombocyte aggregation.
摘要翻译：四氢-1-苯并[c，d]吲哚丙酸磺酰胺可以通过四氢-1-苯并[c，d] - 吲哚磺酰胺与丙烯腈和随后的水解反应来制备。新化合物可用于抑制血小板聚集。

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

US5039670A Antithrombotic substituted cycloalkano(B)dihydroindole- and -indole-sulphonamides and use 失效
标题翻译：抗血栓取代环烷（B）二氢吲哚 - 和吲哚磺酰胺和用途
公开(公告)号：US5039670A
公开(公告)日：1991-08-13
申请号：US599321
申请日：1990-10-17
申请人： Horst Boshagen , Ulrich Muller , Ulrich Rosentreter , Erwin Bischoff , Volker-Bernd Fiedler , Elisabeth Perzborn , Joachim Hutter , Peter Norman , Nigel J. Cuthbert , Hilary P. Francis , Marie G. McKenniff
发明人： Horst Boshagen , Ulrich Muller , Ulrich Rosentreter , Erwin Bischoff , Volker-Bernd Fiedler , Elisabeth Perzborn , Joachim Hutter , Peter Norman , Nigel J. Cuthbert , Hilary P. Francis , Marie G. McKenniff
IPC分类号： C07D209/86 , A61K31/40 , A61K31/403 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/00 , A61P37/08 , C07D209/88 , C07D209/94
CPC分类号： C07D209/88
摘要： Substituted antithrombotic substituted cycloalkano[b]-dihydroindole- and -indole-sulphonamides for treatment of thromboses, thromboembolisms, ischemias, asthma and allergies, of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen or other radicals,X is aryl, alkyl or CF.sub.3,m and Z each is 1,2,3 or 4,n is 0, 1 or 2,A is a bond or --NH--, andY is OH, alkoxy, aryloxy, amino or sulphonylamine, with the proviso that, in all cases, two of the substituents R.sup.1 -R.sup.4 are other than hydrogen in the event that m represents the number 2 and Y represents the hydroxyl group,or a salt thereof.
摘要翻译：用于治疗式（I）的血栓形成，血栓栓塞，缺血，哮喘和过敏的取代的抗血栓形成取代的环烷基[b] - 二氢吲哚和吲哚磺酰胺，其中R 1，R 2，R 3和R 4是氢或其它基团，X是芳基，烷基或CF 3，m和Z各自为1,2,3或4，n为0,1或2，A为键或-NH-，Y为OH，烷氧基，芳氧基，氨基或磺酰胺，条件是在所有情况下，在m表示数2且Y表示羟基的情况下，两个取代基R 1 -R 4不同于氢，或其盐。

5. 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.

6. 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

7. 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。

8. 发明授权

US5096897A Antithrombotic substituted cycloalkano(b)dihydroindole- and -indole-sulphonamides 失效
标题翻译：抗生素替代环孢素（B）二氢吲哚并 - 亚磺酰胺
公开(公告)号：US5096897A
公开(公告)日：1992-03-17
申请号：US678563
申请日：1991-03-28
申请人： Horst Boshagen , Ulrich Muller , Ulrich Rosentreter , Erwin Bischoff , Volker-Bernd Fiedler , Elisabeth Perzborn , Joachim Hutter , Peter Norman , Nigel J. Cuthbert , Hilary P. Francis , Marie G. McKenniff
发明人： Horst Boshagen , Ulrich Muller , Ulrich Rosentreter , Erwin Bischoff , Volker-Bernd Fiedler , Elisabeth Perzborn , Joachim Hutter , Peter Norman , Nigel J. Cuthbert , Hilary P. Francis , Marie G. McKenniff
IPC分类号： C07D209/86 , A61K31/40 , A61K31/403 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/00 , A61P37/08 , C07D209/88 , C07D209/94
CPC分类号： C07D209/88
摘要： Substituted antithrombotic substituted cycloalkano[b]-dihydroindole- and -indole-sulphonamides for treatment of thromboses, thromboembolisms, ischaemias, asthma and allergies, of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are hydrogen or other radicals,X is aryl, alkyl or CF.sub.3,m and Z each is 1, 2, 3 or 4,n is 0, 1 or 2,A is a bond or --NH--, andY is OH, alkoxy, aryloxy, amino or sulphonylamine, with the proviso that, in all cases, two of the substituents R.sup.1 -R.sup.4 are other than hydrogen in the event that m represents the number 2 and Y represents the hydroxyl group,or a salt thereof.

9. 发明授权

US5015657A 2-halogen-substituted N-indolylethyl-sulphonamides and inhibiting platelet aggregation and antagonizing thromboxane A.sub.2 therewith 失效
标题翻译： 2-卤素取代的N-吲哚基乙基磺酰胺，并且抑制血小板聚集并拮抗血栓素A2
公开(公告)号：US5015657A
公开(公告)日：1991-05-14
申请号：US436858
申请日：1989-11-15
申请人： Horst Boshagen , Elisabeth Perzborn , Volker-Bernd Fiedler
发明人： Horst Boshagen , Elisabeth Perzborn , Volker-Bernd Fiedler
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P7/02 , C07D209/30
CPC分类号： C07D209/30
摘要： Inhibiting platelet aggregation and antagonizing thromboxane A.sub.2 with new 2-halogen-substituted N-indolyethyl-sulphonamides of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, trifluoromethyl, carboxyl or alkoxycarbonyl having up to 8 carbon atoms, orrepresents straight-chain or branched alkyl having up to 8 carbon atoms, or represents cycloalkyl having 3 to 8 carbon atoms, which is optionally substituted by carboxyl, halogen, alkoxy or alkoxycarbonyl having in each case up to 8 carbon atoms, cyano or hydroxyl, orrepresents a group of the formula --S(O).sub.n --R.sup.5,--NR.sup.6 R.sup.7 or --OR.sup.8represents straight-chain or branched alkyl having up to 10 carbon atoms, which is optionally substituted by halogen, phenyl, hydroxyl or cyano, orrepresents aryl having 6 to 10 carbon atoms, which is optionally substituted by up to 5 identical or different substituents from the group comprising halogen, cyano, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, alkyl, alkoxy, alkoxycarbonyl or alkylthio having in each case up to 8 carbon atoms, hydroxyl, carboxyl, phenyl, phenoxy, benzyloxy and benzylthio, or by a group of the formula --NR.sup.6 R.sup.7,R.sup.3 represents halogen,R.sup.4 represents hydrogen or straight-chain or branched alkyl having up to 8 carbon atoms, or represents phenylandm represents one of the numbers 2, 3 or 4, and salts thereof.
摘要翻译：抑制血小板聚集和拮抗血栓素A2与新的2-卤素取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N- 具有至多8个碳原子的直链或支链烷基，或代表具有3-8个碳原子的环烷基，其任选被羧基，卤素，烷氧基或烷氧基羰基所取代，每种情况下最多具有8个碳原子，氰基或羟基，或表示式-S（O）n -R 5，-NR 6 R 7或-OR 8表示具有至多10个碳原子的直链或支链烷基，其任选被卤素，苯基，羟基或氰基取代，或表示芳基具有6至10个碳原子，其任选被至多5个相同或不同的取代基取代，所述取代基包括卤素，氰基，三氟甲基，三氟甲氧基，三氟甲硫基，烷基，烷氧基，烷氧基羰基或具有至多8个碳原子的烷硫基，羟基，羧基，苯基，苯氧基，苄氧基和苄硫基，或由-NR 6 R 7基团，R 3表示卤素，R 4表示氢或具有直链或支链烷基的直链或支链烷基 8个碳原子，或表示苯基，m表示数2，3或4中的一个，及其盐。

10. 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。

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