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1. 发明授权

US5008279A Circulation-active fluoromethoxyphenyl dihydropyridine compounds 失效
标题翻译：循环活性氟甲氧基苯基二氢吡啶化合物
公开(公告)号：US5008279A
公开(公告)日：1991-04-16
申请号：US263671
申请日：1988-10-27
申请人： Gerhard Franckowiak , Jurgen Stoltefuss , Martin Bechem , Rainer Gross , Michael Kayser , Siegbert Hebisch , Matthias Schramm
发明人： Gerhard Franckowiak , Jurgen Stoltefuss , Martin Bechem , Rainer Gross , Michael Kayser , Siegbert Hebisch , Matthias Schramm
IPC分类号： A61K31/445 , A61K31/451 , A61P9/08 , C07D211/90 , C07D401/12
CPC分类号： C07D401/12 , C07D211/90
摘要： Circulation-active fluoromethoxyphenyldihydropyridines of the formula ##STR1## in which X stands for hydrogen or fluorine andR stands for straight-chain, branched or cyclic alkyl or alkenyl having 2 to 12 carbon atoms which can be interrupted by 1 to 2 oxygen and/or sulphur atoms in the chain, and which can be monosubstituted or polysubstituted(a) by hydroxyl, aryl having 6 to 12 carbon atoms, aryloxy having 6 to 12 carbon atoms, where the aryl radical is again substituted by alkyl having up to 4 carbon atoms, alkoxy having up to 4 carbon atoms or halogen, the substituents being identical or different, or(b) by carboxyl, alkoxycarbonyl having up to 6 carbon atoms, pyridyl, piperidyl, pyrimidyl, acyloxy having up to 7 carbon atoms, sulphamoyl, carbamoyl, halogen or cyano, the substituents being identical or different, or(c) by an amino group, where the amino group can carry one or two identical or different substituents from the group consisting of alkyl having up to 6 carbon atoms, benzyl, phenyl or acyl having up to 7 carbon atoms,and salts thereof.
摘要翻译：式（I）的循环活性氟甲氧基苯基二氢吡啶，其中X代表氢或氟，R代表可被1至2个氧中断的具有2至12个碳原子的直链，支链或环状烷基或链烯基和/或链中的硫原子，并且其可以被羟基，具有6至12个碳原子的芳基，具有6至12个碳原子的芳氧基单取代或多取代（a），其中芳基再次被具有至多 4个碳原子，具有至多4个碳原子的烷氧基或卤素，取代基相同或不同，或（b）由羧基，具有至多6个碳原子的烷氧基羰基，吡啶基，哌啶基，嘧啶基，具有至多7个碳原子的酰氧基，氨基甲酰基，氨基甲酰基，卤素或氰基，取代基相同或不同，或（c）氨基，其中氨基可以带有一个或两个相同或不同的取代基，由至多6个碳原子的烷基 ms，苄基，苯基或具有至多7个碳原子的酰基及其盐。

2. 发明授权

US5420142A Certain 3-formyl-1, 4-dihydropyridines and their pharmaceutical composition and use 失效
标题翻译：某些3-甲酰基-1,4-二氢吡啶及其药物组成和用途
公开(公告)号：US5420142A
公开(公告)日：1995-05-30
申请号：US166671
申请日：1993-12-14
申请人： Jurgen Stoltefuss , Gerhard Franckowiak , Horst Boshagen , Martin Bechem , Rainer Gross , Siegbert Hebisch , Joachim Hutter , Howard-Paul Rounding , Matthias Schramm
发明人： Jurgen Stoltefuss , Gerhard Franckowiak , Horst Boshagen , Martin Bechem , Rainer Gross , Siegbert Hebisch , Joachim Hutter , Howard-Paul Rounding , Matthias Schramm
IPC分类号： A61K31/435 , A61K31/47 , A61P9/00 , A61P9/12 , C07D211/90 , C07D401/04
CPC分类号： C07D401/04 , C07D211/90
摘要： The present invention relates to the use of 3-formyl-1,4-dihydropyridine derivatives as medicaments for the control of cardiovascular diseases, in particular of pathologically changed blood pressure and of cardiac insufficiency, new compounds and a process for their preparation.
摘要翻译：本发明涉及3-甲酰基-1,4-二氢吡啶衍生物作为药物用于控制心血管疾病，特别是病理改变的血压和心功能不全的新用途及其制备方法。

3. 发明授权

US5344944A Circulation-active dioxyalkylenearyl-dihydropyridines 失效
标题翻译：循环活性二氧杂环己烯基 - 二氢吡啶
公开(公告)号：US5344944A
公开(公告)日：1994-09-06
申请号：US116414
申请日：1993-09-03
申请人： Gerhard Franckowiak , Albrecht Marhold , Martin Bechem , Rainer Gross , Michael Kayser , Matthias Schramm , Gunther Thomas
发明人： Gerhard Franckowiak , Albrecht Marhold , Martin Bechem , Rainer Gross , Michael Kayser , Matthias Schramm , Gunther Thomas
IPC分类号： C07D317/46 , A61K31/335 , A61K31/357 , A61K31/36 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/455 , A61K31/50 , A61P3/08 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , C07D319/20 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/04 , C07D491/044 , C07D491/048 , C07D317/62
CPC分类号： C07D405/04 , C07D405/14 , C07D491/04
摘要： Circulation-active dihydropyridines of the formula ##STR1## in which R.sup.1 is H, CN, NO.sub.2 or --COOR.sup.7,R.sup.7 is H, alkyl or various other radicals,R.sup.2 and R.sup.4 each independently is alkyl or other radicals,R.sup.3 is H or optionally substituted alkyl, andR.sup.5 completes a keto or ester group,and physiologically acceptable salts thereof. Also the aldehyde intermediate therefor of the formula ##STR2##
摘要翻译：其中R 1是H，CN，NO 2或-COOR 7，R 7是H，烷基或各种其它基团，R 2和R 4各自独立地是烷基或其它基团，R 3是H或任选被取代的具有通式“IMAGE”的循环活性二氢吡啶烷基和R 5完成酮基或酯基团及其生理上可接受的盐。也可以使用式为“IMAGE”的醛中间体

4. 发明授权

US4753936A Circulation-active substituted 1,4-dihydropyridine-3-carboxylic acid piperazides 失效
标题翻译：循环活性的取代的1,4-二氢吡啶-3-羧酸哌嗪
公开(公告)号：US4753936A
公开(公告)日：1988-06-28
申请号：US002094
申请日：1987-01-12
申请人： Gerhard Franckowiak , Gunther Thomas , Matthias Schramm , Michael Kayser , Rainer Gross , Martin Bechem
发明人： Gerhard Franckowiak , Gunther Thomas , Matthias Schramm , Michael Kayser , Rainer Gross , Martin Bechem
IPC分类号： C07D335/00 , A61K31/4433 , A61K31/455 , A61P3/08 , A61P7/02 , A61P9/08 , A61P9/10 , A61P9/12 , C07D211/90 , C07D409/04 , C07D413/04 , A61K31/495 , C07D401/06 , C07D401/14 , C07D413/14
CPC分类号： C07D413/04 , C07D211/90
摘要： 1,4-Dihydropyridine-3-carboxylic acid piperazides of the formula ##STR1## in which R.sup.1 is CN or alkyl, preferably methyl,R.sup.2 is H, CN, NO.sub.2 or preferably carboxyalkyl,R.sup.3 is aryl or heterocyclic, andR.sup.4 is alkyl, cycloalkyl, aryl or an acyl radical,and physiologically acceptable salts thereof, are circulation active. Novel intermediates are also provided.
摘要翻译：其中R1是CN或烷基，优选甲基，R2是H，CN，NO2或优选羧基烷基，R3是芳基或杂环，R4是烷基，环烷基，环烷基，芳基或酰基及其生理上可接受的盐是循环活性的。还提供了新的中间体。

5. 发明授权

US4898865A [4-(6-Oxo-1,4,5,6-tetrahydro-3-pyridazinyl) anilino hexyl 1,4-dihydro-2,6 Di methyl 5 nitro 4 aryl pyridine 3-carboxylates 失效
标题翻译： [4-（6-氧代-1,4,5,6-四氢-3-哒嗪基）苯胺基己基1,4-二氢-2,6-二甲基-5-硝基4芳基吡啶3-羧酸酯
公开(公告)号：US4898865A
公开(公告)日：1990-02-06
申请号：US218759
申请日：1988-07-13
申请人： Gerhard Franckowiak , Martin Bechem , Michael Kayser , Rainer Gross , Matthias Schramm , Friedel Seuter , Elisabeth Perzborn , Gunther Thomas
发明人： Gerhard Franckowiak , Martin Bechem , Michael Kayser , Rainer Gross , Matthias Schramm , Friedel Seuter , Elisabeth Perzborn , Gunther Thomas
IPC分类号： A61K31/50 , A61P3/00 , A61P3/08 , A61P9/00 , C07D237/04 , C07D401/12 , C07D409/14 , C07D413/14 , C07D417/14
CPC分类号： C07D401/12 , C07D237/04
摘要： Circulation active nitrodihydropyridines of the formula ##STR1## in which R represents aryl which has 6 to 12 carbon atoms and can be substituted up to 4 times, identically or differently, by halogen, nitro, cyano, alkyl, alkoxy, alkylthio, in each case having up to 6 carbon atoms, trifluoromethyl, trifluoromethoxy, difluoromethoxy, trifluoromethylthio, difluoromethylenedioxy, trifluoroethylenedioxy or tetrafluoroethylenedioxy or by benzyl, benzyloxy or benzylthio, each of which is optionally substituted by halogen, nitro, cyano, trifuoromethyl, alkyl having up to 4 carbon atoms or alkoxy having up to 4 carbon atoms, or represents a heterocycle which is optionally substituted by halogen, phenyl or alkyl having up to 4 carbon atoms and is from the group consisting of pyrryl, thienyl, furyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, pyridyl, pyrimidyl, pyridazinyl, quinolyl, benzoxadiazolyl, chromenyl or thiochromenyl, andn represents a number from 1 to 12,and physiologically acceptable salts thereof.
摘要翻译：具有式“IMAGE”的循环活性硝基二氢吡啶，其中R表示具有6至12个碳原子并且可以相同或不同地被卤素，硝基，氰基，烷基，烷氧基，烷硫基取代至多4次的芳基，具有至多6个碳原子，三氟甲基，三氟甲氧基，二氟甲氧基，三氟甲硫基，二氟亚甲二氧基，三氟亚乙二氧基或四氟亚乙二氧基或苄基，苄氧基或苄硫基，其各自任选被卤素，硝基，氰基，三氟甲基，具有至多4个碳原子的烷基或具有至多4个碳原子的烷氧基，或表示任选被卤素，苯基或具有至多4个碳原子的烷基取代的杂环，并且是由吡咯基，噻吩基，呋喃基，吡唑基，咪唑基，恶唑基，噻唑基，吡啶基，嘧啶基，哒嗪基，喹啉基，苯并二唑基，苯并二唑基，色烯基或硫代色烯基，n表示1〜12的数，生理学上可接受的其盐。

6. 发明授权

US4886816A Circulation-active dioxyalkylenearyl-dihydropyridines 失效
标题翻译：循环活性二氧杂环己烯基 - 二氢吡啶
公开(公告)号：US4886816A
公开(公告)日：1989-12-12
申请号：US190748
申请日：1988-05-05
申请人： Gerhard Franckowiak , Albrecht Marhold , Martin Bechem , Rainer Gross , Michael Kayser , Matthias Schramm , Gunther Thomas
发明人： Gerhard Franckowiak , Albrecht Marhold , Martin Bechem , Rainer Gross , Michael Kayser , Matthias Schramm , Gunther Thomas
IPC分类号： C07D317/46 , A61K31/335 , A61K31/357 , A61K31/36 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/455 , A61K31/50 , A61P3/08 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , C07D319/20 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/04 , C07D491/044 , C07D491/048
CPC分类号： C07D405/04 , C07D405/14 , C07D491/04
摘要： Circulation-active dihydropyridines of the formula ##STR1## in which R.sup.1 is H, CN, NO.sub.2 or --COOR.sup.7,R.sup.7 is H, alkyl or various other radicals,R.sup.2 and R.sup.4 each independently is alkyl or other radicals,R.sup.3 is H or optionally substituted alkyl,R.sup.5 completes a keto or ester group, andR.sup.6 is a direct bond or --CF.sub.2 -- or --CHF--,and physiologically acceptable salts thereof.
摘要翻译：其中R 1是H，CN，NO 2或-COOR 7，R 7是H，烷基或各种其它基团，R 2和R 4各自独立地是烷基或其它基团，R 3是H或任选被取代的具有通式“IMAGE”的循环活性二氢吡啶烷基，R5完成酮基或酯基团，并且R 6是直接键或-CF2-或-CHF-，及其生理上可接受的盐。

7. 发明授权

US4769375A Circulation-active 1,4-dihydropyridine derivatives and use thereas 失效
标题翻译：循环活性的1,4-二氢吡啶衍生物并用于其中
公开(公告)号：US4769375A
公开(公告)日：1988-09-06
申请号：US890998
申请日：1986-07-25
申请人： Horst Meyer , Gerhard Franckowiak , Gunther Thomas , Matthias Schramm , Michael Kayser , Martin Bechem , Rainer Gross
发明人： Horst Meyer , Gerhard Franckowiak , Gunther Thomas , Matthias Schramm , Michael Kayser , Martin Bechem , Rainer Gross
IPC分类号： A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/473 , A61P3/08 , A61P9/00 , A61P9/08 , A61P9/10 , C07D215/06 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/24 , C07D215/36 , C07D215/54 , C07D221/04 , C07D311/74 , C07D311/94 , C07D335/00 , C07D401/04 , C07D405/04 , C07D409/04
CPC分类号： C07D221/04 , C07D215/14 , C07D215/18 , C07D215/24 , C07D215/36 , C07D215/54 , C07D311/74 , C07D311/94 , C07D401/04 , C07D405/04 , C07D409/04
摘要： Circulation-active dihydropyridines of the formula ##STR1## in which R.sup.1 is optionally substituted aryl or heterocyclic,R.sup.2 is H, NO.sub.2, CN, C.sub.1 -C.sub.8 -alkylsulphonyl, aryl or carboalkoxy,R.sup.3 is alkyl or aryl,R.sup.4 is H or alkyl,X is C.dbd.O or a direct bond, andn is a number from 1 to 20,or physiologically acceptable salts thereof. A synthesis using morpholines or thiomorpholines is also disclosed.
摘要翻译： R 1为任选取代的芳基或杂环，R 2为H，NO 2，CN，C 1 -C 8 - 烷基磺酰基，芳基或烷氧羰基，R 3为烷基或芳基，R 4为H或烷基， X为C = O或直接键，n为1〜20的数，或其生理上可接受的盐。还公开了使用吗啉或硫代吗啉的合成。

8. 发明授权

US4710501A Circulation active pyrimidinyl-dihydropyridines 失效
标题翻译：循环活性嘧啶基 - 二氢吡啶
公开(公告)号：US4710501A
公开(公告)日：1987-12-01
申请号：US862869
申请日：1986-05-13
申请人： Gerhard Franckowiak , Martin Bechem , Rainer Gross , Michael Kayser , Matthias Schramm , Gunter Thomas
发明人： Gerhard Franckowiak , Martin Bechem , Rainer Gross , Michael Kayser , Matthias Schramm , Gunter Thomas
IPC分类号： A61K31/505 , A61K31/70 , A61K31/7028 , A61P9/02 , A61P9/04 , A61P9/08 , C07D401/04 , C07D401/14 , C07H15/06 , C07H15/26 , A61K31/44 , C07D239/24
CPC分类号： C07D401/04 , C07D401/14 , C07H15/26
摘要： Novel compounds of the formula ##STR1## in which R.sup.2 is hydrogen or a substituent, andR.sup.1 is optionally substituted alkyl or alkenyl,exhibit positive inotropic activity on the cardiac muscle, intensifying the contraction power.
摘要翻译：式中，R 2为氢或取代基，R 1为任选取代的烷基或烯基的新颖化合物“IMAGE”表现出对心肌的正性肌力活性，增强收缩力。

9. 发明授权

US4707479A Circulation active dihydropyridine-3-carboxamides 失效
标题翻译：循环活性二氢吡啶-3-甲酰胺
公开(公告)号：US4707479A
公开(公告)日：1987-11-17
申请号：US806057
申请日：1985-12-05
申请人： Horst Meyer , Gerhard Franckowiak , Ulrich Rosentreter , Rainer Gross , Gunter Thomas , Matthias Schramm , Michael Kayser , Friedel Seuter , Elisabeth Perzborn , Martin Bechem
发明人： Horst Meyer , Gerhard Franckowiak , Ulrich Rosentreter , Rainer Gross , Gunter Thomas , Matthias Schramm , Michael Kayser , Friedel Seuter , Elisabeth Perzborn , Martin Bechem
IPC分类号： A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/50 , A61P3/08 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/08 , A61P9/10 , C07D211/90 , C07D237/00 , C07D237/04 , C07D333/00 , C07D335/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/04 , C07D491/048 , C07D495/04 , C07D401/06
CPC分类号： C07D401/12 , C07D211/90 , C07D237/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D491/04
摘要： 1,4-Dihyropyridinecarboxamides of the formula ##STR1## and salts thereof, are effective for treating cardiac insufficiency, thromboses, thromboembolisms and ischaemias, for influencing the blood-sugar level and the circulation and as coronary therapeutic agents and anti-arrhythmic agents.
摘要翻译：具有式“IMAGE”及其盐的1,4-二氢吡啶甲酰胺及其盐对于治疗心功能不全，血栓形成，血栓栓塞和间皮瘤有效，用于影响血糖水平和循环以及作为冠状动脉治疗剂和抗心律不齐剂。

10. 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。

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