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1. 发明授权

US06773724B2 Stable salts of O-acetylsalicylic acid with basic amino acids 有权
标题翻译： O-乙酰水杨酸与碱性氨基酸的稳定盐
公开(公告)号：US06773724B2
公开(公告)日：2004-08-10
申请号：US09906497
申请日：2001-07-16
申请人： Gerhard Franckowiak , Hubert Appolt , Gregor Leifker , Hans-Peter Wirges , Wolfram Ledwoch
发明人： Gerhard Franckowiak , Hubert Appolt , Gregor Leifker , Hans-Peter Wirges , Wolfram Ledwoch
IPC分类号： A61K914
CPC分类号： A61K31/616 , C07C229/26
摘要： The present invention relates to stable salts of O-acetylsalicylic acid with basic amino acids, a process for their preparation and their use as medicaments.
摘要翻译：本发明涉及O-乙酰水杨酸与碱性氨基酸的稳定盐，其制备方法及其作为药物的用途。

2. 发明授权

US4645775A Positive inotropic 3-nitro-5-substituted ester and thioester-1,4-dihydropyridines 失效
标题翻译：正性收缩性3-硝基-5-取代酯和硫酯-1,4-二氢吡啶
公开(公告)号：US4645775A
公开(公告)日：1987-02-24
申请号：US734502
申请日：1985-05-15
申请人： Jurgen Stoltefuss , Fred R. Heiker , Gerhard Franckowiak , Matthias Schramm , Gunter Thomas , Rainer Gross
发明人： Jurgen Stoltefuss , Fred R. Heiker , Gerhard Franckowiak , Matthias Schramm , Gunter Thomas , Rainer Gross
IPC分类号： A61K31/4427 , A61K31/455 , A61P9/04 , A61P9/12 , C07D211/90 , C07D401/12 , C07D413/04
CPC分类号： C07D401/12 , C07D211/90 , C07D413/04
摘要： Novel 3-nitro-dihydropyridine derivatives of the formula ##STR1## in which R.sub.1 and R.sub.2 each independently is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.12 -alkoxy, C.sub.1 -C.sub.4 -halogenoalkoxy, halogen, nitro, C.sub.1 -C.sub.4 -halogenoalkyl, C.sub.1 -C.sub.4 -halogenoalkylmercapto, ##STR2## Z is oxygen or sulphur, R.sub.4 and R.sub.5 each independently is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, C.sub.1 -C.sub.4 -halogenoalkyl, C.sub.1 -C.sub.4 -halogenoalkoxy or nitro, orR.sub.1 and R.sub.2, together with 2 C atoms of the phenyl ring form the ring ##STR3## X is oxygen or sulphur, A is a hydrocarbon radical with up to 12 C atoms which optionally contains one or two identical or different chain members from the group comprising O, S and CO and/or which is optionally substituted by hydroxyl or aliphatic acyloxy with up to 4 C atoms,R.sub.3 is --O--COR.sub.6, --S--CO--R.sub.6, SH, OH , NH.sub.2, ##STR4## NH--COR.sub.6, COOR.sub.6, NR.sub.7 R.sub.8 or CONR.sub.7 R.sub.8, R.sub.6 is hydrogen or an aliphatic radical with up to 6 C atoms or a phenyl radical, andR.sub.7 and R.sub.8 each independently is hydrogen or an aliphatic radical with up to 6 C atoms or a phenyl radical,or a physiologically acceptable salts thereof, which are active in circulation and exhibit positive inotropic activity.
摘要翻译：其中R 1和R 2各自独立地为氢，C 1 -C 4 - 烷基，C 1 -C 12 - 烷氧基，C 1 -C 4 - 卤代烷氧基，卤素，硝基，C 1 -C 4 - 卤代烷基的新颖的3-硝基 - 二氢吡啶衍生物，C 1 -C 4卤代烷基巯基，Z为氧或硫，R 4和R 5各自独立地为氢，C 1 -C 4 - 烷基，C 1 -C 6 - 烷氧基，卤素，C 1 -C 4 - 卤代烷基，C 1 -C 4卤代烷氧基或硝基或R1和R2与苯环的2 C原子一起形成环，X是氧或硫，A是具有至多12个C原子的烃基，其任选地含有一个或两个相同或不同的链成员由包含O，S和CO的基团和/或其任选被具有至多4个C原子的羟基或脂族酰氧基取代，R 3是-O-COR 6，-S-CO-R 6，SH，OH，NH 2， > NH-COR 6，COOR 6，NR 7 R 8或CONR 7 R 8，R 6是氢或具有至多6个C原子或苯基的脂族基团，并且R 7和R 8各自独立地为氢或至多6个碳原子的脂族基团 oms或苯基或其生理上可接受的盐，其在循环中具有活性并表现出正性肌力活性。

3. 发明授权

US4540684A 3-Nitro-5-amide-1,4-dihydropyridines with positive inotropic activity 失效
标题翻译：具有正性肌力活性的3-硝基-5-酰胺-1,4-二氢吡啶
公开(公告)号：US4540684A
公开(公告)日：1985-09-10
申请号：US612093
申请日：1984-05-18
申请人： Jurgen Stoltefuss , Gerhard Franckowiak , Horst Boshagen , Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
发明人： Jurgen Stoltefuss , Gerhard Franckowiak , Horst Boshagen , Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
IPC分类号： A61K31/455 , A61P3/08 , A61P9/02 , A61P9/04 , C07D211/90 , C07D211/98 , A61K31/70 , C07D405/12
CPC分类号： C07D211/90
摘要： A 1,4-dihydropyridine derivative of the formula ##STR1## in which R and R.sub.1 each independently is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 to C.sub.12 -alkoxy, C.sub.1 -C.sub.4 -halogenoalkoxy, halogen, nitro, trifluoromethyl, ##STR2## X is oxygen or sulphur, R.sub.4 and R.sub.5 each independently is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, trifluoromethyl, amino or nitro, andR.sub.2 and R.sub.3 each independently is hydrogen, a C.sub.1 -C.sub.10 -alkyl, C.sub.2 -C.sub.10 -alkenyl or C.sub.3 -C.sub.10 -alkinyl radical which is optionally substituted by halogen, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, amino, mono- and di-C.sub.1 -C.sub.4 -alkylamino, carbo-C.sub.1 -C.sub.6 -alkoxy and/or nitro, a C.sub.3 to C.sub.6 -membered cycloalkyl radical, a phenyl radical which is optionally substituted by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, amino and/or nitro, or a phenyl-C.sub.1 -C.sub.3 -alkyl radical, or a carbohydrate radical which is optionally bonded via a C.sub.1 -C.sub.8 -alkyl chain to the amide nitrogen atomor a pharmaceutically acceptable acid addition salt thereof, which improves the contractility of the heart, raises the blood pressure, lowers the blood sugar, reduces the swelling of mucous membranes and affects the salt and fluid balances of a patient.
摘要翻译：其中R和R 1各自独立地为氢，C 1 -C 4 - 烷基，C 1 -C 12 - 烷氧基，C 1 -C 4卤代烷氧基，卤素，硝基，三氟甲基， X是氧或硫，R4和R5各自独立地是氢，C1-C4-烷基，C1-C6-烷氧基，卤素，三氟甲基，氨基或硝基，R2和R3各自独立地是氢，C1-C10 - 烷基，C 2 -C 10 - 烯基或C 3 -C 10 - 炔基，其任选被卤素，羟基，C 1 -C 4 - 烷氧基，氨基，单 - 和二-C 1 -C 4 - 烷基氨基，C 1 -C 6 - 和/或硝基，C3至C6元环烷基，任选被C 1 -C 4 - 烷基，C 1 -C 6 - 烷氧基，卤素，氨基和/或硝基取代的苯基，或苯基-C 1 -C 3 - 烷基或通过C1-C8烷基链任选与酰胺氮原子键合的碳水化合物基团或其药学上可接受的酸加成盐，其改善心脏的收缩力，使血压升高 ure，降低血糖，减少粘膜肿胀，影响患者的盐和液体平衡。

4. 发明授权

US4537881A 5-Nitro 1,4-dihydropyridines having a positive inotropic effect 失效
标题翻译：具有正性肌力作用的5-硝基1,4-二氢吡啶类
公开(公告)号：US4537881A
公开(公告)日：1985-08-27
申请号：US627596
申请日：1984-07-03
申请人： Fred R. Heiker , Jurgen Stoltefuss , Gerhard Franckowiak , Matthias Schramm , Gunter Thomas , Rainer Gross
发明人： Fred R. Heiker , Jurgen Stoltefuss , Gerhard Franckowiak , Matthias Schramm , Gunter Thomas , Rainer Gross
IPC分类号： A61K31/70 , A61K31/7028 , A61P3/08 , A61P9/04 , A61P9/12 , C07H15/04 , C07H15/06 , C07H15/12 , C07H15/14 , C07H15/26 , A61K31/41 , A61K31/395 , C07D405/12
CPC分类号： C07H15/06 , C07H15/04 , C07H15/14 , C07H15/26
摘要： Novel 1,4-dihydropyridines of the fomula ##STR1## in which R.sub.1 and R.sub.2 each independently is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.12 -alkoxy, C.sub.1 -C.sub.4 -halogenoalkoxy, halogen, nitro, C.sub.1 -C.sub.4 -halogenoalkyl, C.sub.1 -C.sub.4 -halogenoalkylmercapto, ##STR2## in which Z is oxygen or sulphur, andR.sub.4 and R.sub.5 each independently is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, C.sub.1 -C.sub.4 -halogenoalkyl, C.sub.1 -C.sub.4 -halogenoalkoxy or nitro, orR.sub.1 and R.sub.2, together with 2 C atoms of the phenyl ring, form the ring ##STR3## X is oxygen, sulphur or the radical NR.sub.6, R.sub.6 is a C.sub.1 -C.sub.6 -alkyl group,A is a C.sub.2 -C.sub.10 -alkylene group, it being necessary that at least two C atoms are located in the alkylene chain which connects the carbonyloxy group to X, andR.sub.3 is a monosaccharide or disaccharide moiety or a protected monosaccharide or disaccharide moiety,or pharmaceutically acceptable addition salts thereof, which exhibit positive inotropic activity and are useful in treating circulatory disorders.
摘要翻译： R1和R2各自独立地为氢，C1-C4-烷基，C1-C12-烷氧基，C1-C4-卤代烷氧基，卤素，硝基，C1-C4-卤代烷基， C1-C4卤代烷基巯基，其中Z是氧或硫，R4和R5各自独立地是氢，C1-C4-烷基，C1-C6-烷氧基，卤素，C1-C4-卤代烷基，C1-C4-卤代烷基，卤代烷氧基或硝基，或R 1和R 2与苯环的2 C原子一起形成环，X为氧，硫或基团NR 6，R 6为C 1 -C 6 - 烷基，A为C 2 - C10亚烷基，必须至少两个C原子位于将羰氧基连接到X的亚烷基链中，R3是单糖或二糖部分或受保护的单糖或二糖部分，或其药学上可接受的加成盐，其表现出正性肌力活性并且可用于治疗循环障碍。

5. 发明申请

US20050171070A1 Stable salts of o-acetylsalicylic acid containing basic amino acids II 审中-公开
标题翻译：含有碱性氨基酸的邻乙酰水杨酸的稳定盐II
公开(公告)号：US20050171070A1
公开(公告)日：2005-08-04
申请号：US10501677
申请日：2003-01-07
申请人： Felix Ecker , Ralf Bullesbach , Wolfram Ledwoch , Gerhard Franckowiak , Marianne Petersen-Braun
发明人： Felix Ecker , Ralf Bullesbach , Wolfram Ledwoch , Gerhard Franckowiak , Marianne Petersen-Braun
IPC分类号： A61K9/00 , A61K9/16 , A61K9/20 , A61K9/48 , A61K31/192 , A61K45/00 , A61K47/10 , A61K47/18 , A61K47/26 , A61K47/46 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/10 , A61P19/02 , A61P21/00 , A61P25/04 , A61P25/06 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/18 , A61P35/00 , C07C69/157 , C07C229/26 , A61K31/60 , A61K31/198
CPC分类号： A61K9/1688 , A61K9/0056 , A61K9/2018 , C07C229/26
摘要： The present invention relates to improved compositions comprising stable salts of O-acetylsalicylic acid with basic amino acids, to pharmaceuticals comprising them and to their use for preparing pharmaceuticals.
摘要翻译：本发明涉及包含O-乙酰水杨酸与碱性氨基酸的稳定盐的改进组合物，包括它们的药物及其制备药物的用途。

6. 发明申请

US20050009791A1 Stable salts of O-acetylsalicylic acid with basic amino acids 失效
标题翻译： O-乙酰水杨酸与碱性氨基酸的稳定盐
公开(公告)号：US20050009791A1
公开(公告)日：2005-01-13
申请号：US10915652
申请日：2004-08-09
申请人： Gerhard Franckowiak , Hubert Appolt , Gregor Leifker , Hans-Peter Wirges , Wolfram Ledwoch
发明人： Gerhard Franckowiak , Hubert Appolt , Gregor Leifker , Hans-Peter Wirges , Wolfram Ledwoch
IPC分类号： A61K9/16 , A61K31/616 , A61K45/00 , A61K47/18 , A61P9/10 , A61P19/00 , A61P19/02 , A61P25/00 , A61P25/04 , A61P25/06 , A61P29/00 , C07C69/157 , C07C229/26 , C07D233/64 , A61K31/60
CPC分类号： A61K31/616 , C07C229/26
摘要： The present invention relates to stable salts of O-acetylsalicylic acid with basic amino acids, a process for their preparation and their use as medicaments.
摘要翻译：本发明涉及O-乙酰水杨酸与碱性氨基酸的稳定盐，其制备方法及其作为药物的用途。

7. 发明授权

US4876255A Substituted 1,4-dihydropyridines for control of circulation and thromboses 失效
标题翻译：用于控制循环和血栓形成的取代的1,4-二氢吡啶
公开(公告)号：US4876255A
公开(公告)日：1989-10-24
申请号：US178710
申请日：1988-04-07
申请人： Gerhard Franckowiak , Ulrich Rosentreter , Elisabeth Perzborn , Friedel Seuter , Michael Kayser , Gunther Thomas
发明人： Gerhard Franckowiak , Ulrich Rosentreter , Elisabeth Perzborn , Friedel Seuter , Michael Kayser , Gunther Thomas
IPC分类号： A61K31/50 , A61K31/505 , A61P7/02 , A61P9/00 , C07D211/90 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
CPC分类号： C07D401/12 , C07D211/90 , C07D401/14 , C07D409/14 , C07D413/14
摘要： For the control of coronary diseases and thromboses there are provided the novel compounds ##STR1## in which R.sup.1 is an optionally substituted phenyl or heterocyclic radical,R.sup.2 is a cyano, keto, carboxy, ester or amide group, andX is from 0 to 6,and physiologically acceptable salts thereof.
摘要翻译：为了控制冠状动脉疾病和血栓形成，提供了新的化合物（I），其中R 1是任选取代的苯基或杂环基，R 2是氰基，酮基，羧基，酯或酰胺基，X是 0至6，及其生理上可接受的盐。

8. 发明授权

US4772612A Circulation-active 1,4-dihydropyridines 失效
标题翻译：循环活性1,4-二氢吡啶类
公开(公告)号：US4772612A
公开(公告)日：1988-09-20
申请号：US870042
申请日：1986-06-03
申请人： Siegfried Goldmann , Jurgen Stoltefuss , Gerhard Franckowiak , Rainer Gross , Matthias Schramm , Gunter Thomas
发明人： Siegfried Goldmann , Jurgen Stoltefuss , Gerhard Franckowiak , Rainer Gross , Matthias Schramm , Gunter Thomas
IPC分类号： A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/455 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/12 , C07D211/90 , C07D333/00 , C07D401/12 , C07D405/12 , C07D409/12 , C07D491/04 , C07D491/048
CPC分类号： C07D409/12 , C07D211/90 , C07D491/04
摘要： Novel circulation active dihydropyridines of the formula ##STR1## in which X is CO, SO.sub.2 or CONH,R.sup.4 is H, OH, alkyl, halogen, acyloxy, alkoxyalkoxy, aralkyloxy, or together with R.sup.5 forms a heterocyclic ring, andthe other radicals are conventional in the dihydropyridine art,and pharmaceutically acceptable salts thereof.
摘要翻译：其中X为CO，SO 2或CONH，R 4为H，OH，烷基，卤素，酰氧基，烷氧基烷氧基，芳烷氧基或与R 5一起形成杂环的新型循环活性二氢吡啶类化合物，其中X为CO，SO2或CONH，在二氢吡啶领域中是常规的，及其药学上可接受的盐。

9. 发明授权

US4540789A Circulation-active novel chromone-and thiochromone-substituted 1,4-dihydropyridines 失效
标题翻译：循环活性新型色酮和硫色酮取代的1,4-二氢吡啶
公开(公告)号：US4540789A
公开(公告)日：1985-09-10
申请号：US589436
申请日：1984-03-14
申请人： Siegfried Goldmann , Gerhard Franckowiak , Matthias Schramm , Gunter Thomas , Rainer Gross
发明人： Siegfried Goldmann , Gerhard Franckowiak , Matthias Schramm , Gunter Thomas , Rainer Gross
IPC分类号： A61K31/435 , A61K31/443 , A61K31/4433 , A61K31/455 , A61P3/08 , A61P9/02 , A61P9/04 , A61P27/16 , C07D211/90 , C07D405/04 , C07D409/04 , C07D409/14 , C07D405/06
CPC分类号： C07D405/04 , C07D211/90 , C07D409/04 , C07D409/14
摘要： Dihydropyridines of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 can be hydrogen or various halogen or organic radicals,R.sup.4 is an optionally substituted hydrocarbon radical,A is a direct bond, an alkylene chain with 1 to 20 C atoms or an alkenylene chain with 2 to 20 atoms, the chains being optionally interrupted by O or S,X is O or S andY is a direct bond, O, S, -NH- or -N- alkyl with 1 to 8 C atoms,or a pharmaceutically acceptable salt thereof, are useful as cardiotonic agents for improving heart contractility, antihypotonic agents, for lowering the blood sugar level, for detumescing mucous membranes and for influencing the salt and liquid balance.
摘要翻译：其中R 1，R 2，R 5，R 6，R 7和R 8可以是氢或各种卤素或有机基团，R 4是任选取代的烃基，A是直接键，具有1至 20个C原子或具有2至20个原子的亚链烯基，链任选地被O或S间隔，X是O或S，Y是直接键，O，S，-NH-或-N-烷基，具有1至 8 C原子或其药学上可接受的盐可用作改善心脏收缩力的强心剂，抗低血糖剂，降低血糖水平，用于消肿粘膜和影响盐和液体平衡。

10. 发明授权

US4360520A 1,4-Dihydropyridazine compounds, and their medicinal use 失效
标题翻译： 1,4-二氢哒嗪化合物及其药用
公开(公告)号：US4360520A
公开(公告)日：1982-11-23
申请号：US941527
申请日：1978-09-11
申请人： Horst Meyer , Gerhard Franckowiak , Friedrich Bossert , Arend Heise , Stanislav Kazda , Kurt Stoepel , Robertson Towart , Egbert Wehinger
发明人： Horst Meyer , Gerhard Franckowiak , Friedrich Bossert , Arend Heise , Stanislav Kazda , Kurt Stoepel , Robertson Towart , Egbert Wehinger
IPC分类号： A61K31/50 , A61P9/08 , A61P9/10 , A61P9/12 , C07D237/00 , C07D237/04 , C07D333/00 , C07D405/04 , C07D409/04 , C07D409/14 , A61K31/495
CPC分类号： C07D237/04
摘要： The invention includes new 1,4-dihydropyridazine compounds, compositions containing said 1,4-dihydropyridazine compounds and methods for the use of said compounds and compositions. Also included in the invention are methods for preparing the new 1,4-dihydropyridazine compounds.
摘要翻译：本发明包括新的1,4-二氢哒嗪化合物，含有所述1,4-二氢哒嗪化合物的组合物和使用所述化合物和组合物的方法。本发明还包括制备新的1,4-二氢哒嗪化合物的方法。

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