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31. 发明授权

US4555512A Circulation-active novel chromone- and thiochromone-substituted 1,4-dihydropyridine-lactones 失效
标题翻译：循环活性新型色酮和硫色酮取代的1,4-二氢吡啶内酯
公开(公告)号：US4555512A
公开(公告)日：1985-11-26
申请号：US589614
申请日：1984-03-14
申请人： Siegfried Goldmann , Friedrich Bossert , Matthias Schramm , Gunter Thomas , Rainer Gross
发明人： Siegfried Goldmann , Friedrich Bossert , Matthias Schramm , Gunter Thomas , Rainer Gross
IPC分类号： A61K31/435 , A61K31/44 , A61P3/00 , A61P3/08 , A61P9/02 , A61P9/04 , C07D307/66 , C07D491/04 , C07D491/048 , C07F7/08
CPC分类号： C07D491/04 , C07D307/66 , C07F7/0812
摘要： Dihydropyridines of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.5 and R.sup.6 can be hydrogen or various halogen or organic radicals,R.sup.4 is an optionally substituted hydrocarbon radical,A is a direct bond, a C.sub.1 -C.sub.20 -alkylene chain or a C.sub.2 -C.sub.20 -alkenylene chain, which chains are optionally interrupted by O or SX is O or S, andY is a direct bond, O, S, --NH--or--N-alkyl with 1 to 8 C atomsor a pharmaceutically acceptable salt,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/or liquid balance.
摘要翻译：其中R 1，R 2，R 5和R 6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，C 1 -C 20亚烷基链或C 2 -C 20亚烷基链 -C 20亚烯基链，其任选地被O或SX中断，是O或S，Y是直接键，具有1至8个C原子的O，S，-NH-或N-烷基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/或液体平衡。

32. 发明授权

US4762853A 1-oxo-1,3,4,7-tetrahydrobenzo[C]furans 失效
标题翻译： 1-氧代-1,3,4,7-四氢苯并[C]呋喃
公开(公告)号：US4762853A
公开(公告)日：1988-08-09
申请号：US917875
申请日：1986-10-10
申请人： Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
发明人： Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
IPC分类号： A61K31/365 , A61K31/38 , A61K31/381 , A61K31/382 , A61K31/44 , A61K31/443 , A61K31/4433 , A61P3/00 , A61P3/08 , A61P9/00 , A61P9/02 , A61P9/04 , C07D307/88 , C07D333/72 , C07D335/00 , C07D405/04 , C07D409/04 , C07D407/02 , A61K31/35
CPC分类号： C07D405/04 , C07D307/88 , C07D409/04
摘要： 1-Oxo-1,3,4,7-tetrahydrobenzofuranes of the formula ##STR1## in which X is O or S,R is optionally substituted phenyl or heteroaryl,R.sup.1 is OH, monoalkylamino or dialkylamino, andR.sup.2 is an acyl or esterified carboxy radical,or pharmacologically acceptable salts thereof, which are active in circulation, e.g. they increase myocardial contractility, increase the flow of Ca.sup.2+ into the cell, increase blood pressure, reduce blood sugar, reduce swelling of mucous membranes and affect the salt and/or fluid balance.
摘要翻译：其中X为O或S，R为任选取代的苯基或杂芳基，R 1为OH，单烷基氨基或二烷基氨基，R 2为酰基或酯化的式羧基或其药理学上可接受的盐，其在循环中是有活性的，例如它们增加心肌收缩力，增加Ca2 +流入细胞，增加血压，降低血糖，减少粘膜肿胀并影响盐和/或液体平衡。

33. 发明授权

US4642310A Circulation-active tetrahydrothienopyridines 失效
标题翻译：循环活性四氢噻吩并吡啶
公开(公告)号：US4642310A
公开(公告)日：1987-02-10
申请号：US716876
申请日：1985-03-28
申请人： Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
发明人： Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
IPC分类号： A61K31/435 , A61K31/44 , A61K31/535 , A61P9/00 , C07D211/90 , C07D409/04 , C07D493/04 , C07D495/04 , C07D495/06 , A61K31/38 , C07D417/02 , C07D513/04
CPC分类号： C07D409/04 , C07C327/00 , C07D211/90 , C07D495/04
摘要： Tetrahydrothienopyridines of the formula ##STR1## in which R is optionally substituted aryl or heterocyclyl,R.sup.1 is an organic radical, andR.sup.2, R.sup.3 and R.sup.4 each independently is hydrogen or an organic radical, or pharmaceutically acceptable salts thereof, which are coronary active, hypotensive, anti-diabetic and salt balance restoring.
摘要翻译：其中R是任选取代的芳基或杂环基，R 1是有机基团，并且R 2，R 3和R 4各自独立地是氢或有机基团或其药学上可接受的盐，它们是冠状动脉，低血压的四氢噻吩并吡啶，抗糖尿病和盐平衡恢复。

34. 发明授权

US4647568A Circulation-active hydroxy-tetra-hydropyridinelactones 失效
公开(公告)号：US4647568A
公开(公告)日：1987-03-03
申请号：US673296
申请日：1984-11-20
申请人： Klaus Gorlitzer , Ulrich Bartke , Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
发明人： Klaus Gorlitzer , Ulrich Bartke , Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
IPC分类号： A61K31/435 , A61K31/47 , A61K31/505 , A61P3/00 , A61P3/08 , A61P9/04 , C07D211/90 , C07D491/04 , C07D491/048 , C07F7/10 , A61K31/455 , A61K31/535 , A61K31/695
CPC分类号： C07D491/04 , C07D211/90
摘要： Hydroxytetrahydropyridinelactones of the formula ##STR1## in which R represents a phenyl, naphthyl, thienyl, furyl, pyrryl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyridazinyl, pyrimidyl, pyrazinyl, quinolyl, isoquinolyl, indolyl, benzimidazolyl, quinazolyl, quinoxalyl, thionaphthenyl, isothionaphthenyl, chromonyl, thiochromonyl, chromenyl, thiochromenyl, benzoxadiazolyl or benzthiadiazolyl radical, and the stated radicals may carry 1 to 3 identical or different substituents from the group comprising C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, C.sub.2 -C.sub.20 -alkinyl, C.sub.1 -C.sub.20 -alkoxy, fluorine, chlorine, bromine, iodine, trifluoromethyl, monofluoro-C.sub.1 -C.sub.10 -alkoxy, polyfluoro-C.sub.1 -C.sub.10 -alkoxy, hydroxyl, amino, mono-C.sub.1 -C.sub.10 -alkylamino, di-C.sub.1 -C.sub.10 -alkylamino, nitro, cyano, azido, carboxyl, carb-C.sub.1 -C.sub.10 -alkoxy, carboxamido, sulphonamido, SO.sub.m -alkyl (m=0 to 2, 1 to 20 C atoms), phenyl, benzyl, benzyloxy or benzylthio, it being possible for the 4 last-mentioned substituents to carry 1 to 3 radicals from the group comprising C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, C.sub.1 -C.sub.5 -alkylthio, fluorine, chlorine, bromine, iodine, cyano, nitro, azido, hydroxyl, trifluoromethyl, amino, C.sub.1 -C.sub.6 -alkylamino or di-C.sub.1 -C.sub.6 -alkylamino,R.sup.1 represents a straight-chain, branched or cyclic saturated or unsaturated hydrocarbon radical which has 1-20 C atoms, may be interrupted in the chain by 1 or 2 oxygen or sulphur atoms and may be optionally substituted by one or more fluorine atoms, NO.sub.2, C.sub.3 -C.sub.12 -trialkyl-silyl, hydroxyl, chlorine, bromine, iodine or cyano,R.sup.2 represents hydrogen, --NH.sub.2, --CHO, cyano, --CH.sub.2 OH or a straight-chain or branched saturated or unsaturated hydrocarbon radical having 1 to 8 C atoms,R.sup.3 represents hydrogen or a straight-chain or branched C.sub.1 -C.sub.10 -alkyl radical which may be interrupted in the alkyl chain by one or two oxygen atoms and may be optionally substituted by fluorine, chlorine, bromine, iodine, --CN, --NH.sub.2, --OH or morpholino, which can be used as cardiotonics for improving the contractility of the heart. Moveover, they increase the flow of Ca.sup.++ into the cells and can therefore be employed as antihypotonics, for lowering the blood sugar level, for reducing the swelling of mucous membranes and for influencing the salt balance and/or fluid balance.

35. 发明授权

US5721238A 2,8-disubstituted quinazolinones 失效
标题翻译： 2,8-二取代喹唑啉酮
公开(公告)号：US5721238A
公开(公告)日：1998-02-24
申请号：US584865
申请日：1996-01-11
申请人： Fred Robert Heiker , Ulrich Niewohner , Wolfgang Hartwig , Helmuth Schutz , Erwin Bischoff , Elisabeth Perzborn , Matthias Schramm
发明人： Fred Robert Heiker , Ulrich Niewohner , Wolfgang Hartwig , Helmuth Schutz , Erwin Bischoff , Elisabeth Perzborn , Matthias Schramm
IPC分类号： A61K31/505 , A61K31/517 , A61K31/535 , A61K31/655 , A61P7/02 , A61P9/06 , A61P9/08 , A61P9/10 , A61P13/08 , A61P29/00 , A61P43/00 , C07D239/91 , C07D405/04 , C07D413/12 , C07D413/14 , C07D239/80
CPC分类号： C07D405/04 , C07D239/91
摘要： 2,8-Disubstituted quinazolinones are prepared by first subjecting the quinazolinone basic skeleton to condensation by customary reactions and then introducing the desired substituents into the 8-position. The compounds are suitable as active compounds in medicaments, in particular for the treatment of inflammations, thromboembolic diseases and cardiovascular diseases.
摘要翻译：通过首先使喹唑啉酮碱性骨架通过常规反应冷凝，然后将所需的取代基引入8-位来制备2,8-二取代喹唑啉酮。该化合物适合作为药物中的活性化合物，特别是用于治疗炎症，血栓栓塞性疾病和心血管疾病。

36. 发明授权

US5272161A Indolesulphonamide-substituted dihydropyridines 失效
标题翻译：吲哚磺酰胺取代的二氢吡啶
公开(公告)号：US5272161A
公开(公告)日：1993-12-21
申请号：US942550
申请日：1992-09-09
申请人： Ulrich Niewohner , Siegfried Goldmann , Ulrich Muller , Andreas Knorr , Elisabeth Perzborn , Matthias Schramm , Bernhard Beckermann
发明人： Ulrich Niewohner , Siegfried Goldmann , Ulrich Muller , Andreas Knorr , Elisabeth Perzborn , Matthias Schramm , Bernhard Beckermann
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/455 , A61K31/505 , A61P7/02 , A61P9/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14
CPC分类号： C07D401/12 , C07D401/14
摘要： Indolesulphonamide-substituted dihydropyridines can be prepared by reaction of dihydropyridinecarboxylic acids with hydroxy-substituted indolesulphonamides, or by reaction of amino- or hydroxy-substituted dihydropyridines with indolesulphonamidecarboxylic acids. The indolesulphonamide-substituted dihydropyridines can be employed as active substances in medicaments for the treatment of cardiac, circulatory and thromboedabolic disorders.
摘要翻译：吲哚磺酰胺取代的二氢吡啶可以通过二氢吡啶羧酸与羟基取代的吲哚磺酰胺的反应或通过氨基或羟基取代的二氢吡啶与吲哚磺酰胺羧酸的反应来制备。吲哚磺酰胺取代的二氢吡啶可用作用于治疗心脏，循环和血栓代谢紊乱的药物中的活性物质。

37. 发明授权

US5866571A 9-substituted 2-(2-n-alkoxyphenyl)-purin-6-ones 失效
标题翻译： 9-取代的2-（2-n-烷氧基苯基） - 嘌呤-6-酮
公开(公告)号：US5866571A
公开(公告)日：1999-02-02
申请号：US585996
申请日：1996-01-16
申请人： Ulrich Niewohner , Erwin Bischoff , Helmuth Schutz , Elisabeth Perzborn , Matthias Schramm
发明人： Ulrich Niewohner , Erwin Bischoff , Helmuth Schutz , Elisabeth Perzborn , Matthias Schramm
IPC分类号： C07D473/34 , A61K31/52 , A61K31/522 , A61K31/535 , A61K31/63 , A61K31/655 , A61P7/02 , A61P9/00 , A61P13/02 , A61P15/00 , A61P29/00 , A61P43/00 , C07D295/26 , C07D473/00 , C07D473/30
CPC分类号： C07D473/00 , C07D473/30
摘要： 9-Substituted 2-(2-n-alkoxyphenyl)purin-6-ones are prepared by cyclizing correspondingly substituted imidazoles and derivatizing the purines thus obtained. The 9-substituted .sup.2 -(2-n-alkoxyphenyl)purin-6-ones can be employed as active compounds in medicaments, in particular in medicarnents for treatment of inflammations, thromboembolic diseases and cardiovascular diseases.
摘要翻译： 9-取代的2-（2-正烷氧基苯基）嘌呤-6-酮通过环化相应取代的咪唑并衍生得到的嘌呤来制备。 9-取代的2-（2-正烷氧基苯基）嘌呤-6-酮可用作药物中的活性化合物，特别是用于治疗炎症，血栓栓塞性疾病和心血管疾病的药物。

38. 发明授权

US5861404A 2,9-disubstituted purin-6-ones 失效
标题翻译： 2,9-二取代的嘌呤-6-酮
公开(公告)号：US5861404A
公开(公告)日：1999-01-19
申请号：US587321
申请日：1996-01-12
申请人： Ulrich Niewohner , Erwin Bischoff , Helmuth Schutz , Elisabeth Perzborn , Matthias Schramm
发明人： Ulrich Niewohner , Erwin Bischoff , Helmuth Schutz , Elisabeth Perzborn , Matthias Schramm
IPC分类号： A61K31/52 , A61K31/522 , A61P7/02 , A61P9/00 , A61P13/02 , A61P15/00 , A61P29/00 , A61P43/00 , C07D233/90 , C07D473/00 , C07D473/30
CPC分类号： C07D473/00
摘要： 2,9-Disubstituted purin-6-ones are prepared by acylating correspondingly substituted aminoimidazoles in a first step and then cyclizing the product to the purine. The new 2,9-disubstituted purin-6-ones can be employed as active compounds in medicaments, in particular for the treatment of inflammations, thromboembolic and cardiovascular diseases and diseases of the urogenital system.
摘要翻译： 2,9-二取代的嘌呤-6-酮通过在第一步中酰化相应的取代的氨基咪唑然后将产物环化成嘌呤来制备。新的2,9-二取代的嘌呤-6-酮可以用作药物中的活性化合物，特别是用于治疗炎症，血栓栓塞和心血管疾病以及泌尿生殖系统的疾病。

39. 发明授权

US4886820A Dihydropyridine combination product comprising a dihydropyridine compound and a cardioactive nitrate 失效
标题翻译：包含二氢吡啶化合物和心脏活性硝酸盐的二氢吡啶组合产物
公开(公告)号：US4886820A
公开(公告)日：1989-12-12
申请号：US274182
申请日：1988-11-03
申请人： Rainer Gross , Matthias Schramm
发明人： Rainer Gross , Matthias Schramm
IPC分类号： A61K31/34 , A61K31/04 , A61K31/44 , A61K31/455 , A61P9/08 , A61P9/10
CPC分类号： A61K31/44
摘要： A solid medicament formulation which can be administered orally, comprising 1 to 40 mg of a dihydropyridine of the formula ##STR1## in which R.sup.1 and R.sup.3 are always different from one another and represent alkyl which has 1 to 12 carbon atoms and which is optionally substituted once or several times by fluorine or chlorine or which is optionally interrupted by an oxygen atom in the chain, andA represents the radical ##STR2## R.sup.2 representing one or two substituents from the group consisting of nitro, chlorine and trifluoromethyl, or represents and 0.1 to 100 mg of a cardioactive nitrate. The composition is cardio-active and the patient's tendency toward nitrate tolerance is reduced.
摘要翻译：可以口服给药的固体药物制剂，其包含1至40mg式“IMAGE”的二氢吡啶，其中R 1和R 3总是彼此不同，并且表示具有1至12个碳原子并且任选被取代的烷基一次或几次用氟或氯或任选地被链中的氧原子中断，并且A代表表示一个或两个来自硝基，氯和三氟甲基的取代基的基团，或表示和0.1至100mg的心脏活性硝酸盐。该组合物是有活力的，并且患者对耐硝酸盐耐受性的倾向降低。

40. 发明授权

US4749714A Nifedipine isosorbide 5-monoitrate combination product 失效
标题翻译：硝苯地平异山梨醇5-单硝酸酯组合产品
公开(公告)号：US4749714A
公开(公告)日：1988-06-07
申请号：US98334
申请日：1987-09-18
申请人： Rainer Gross , Matthias Schramm
发明人： Rainer Gross , Matthias Schramm
IPC分类号： A61K31/34 , A61K31/44 , A61K31/455 , A61P9/00 , A61P9/08 , A61P9/10
CPC分类号： A61K31/44
摘要： A solid medicament formulation which can be administered orally comprising 5 to 30 mg of nifedipine and 10 to 40 mg of isosorbide 5-mononitrate. Oral administration of such cardioactive formulation reduces the time tolerance to the isosorbide 5-mononitrate alone.
摘要翻译：可以口服给药的固体药物制剂，包含5至30mg硝苯地平和10至40mg 5-硝酸异山梨酯。这种心脏制剂的口服给药减少了单独使用异山梨醇5-单硝酸盐的时间耐受性。

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