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1.发明授权Specific 1,4-dihydropyridine-3,5-dicarboxylic acid ester and its pharmaceutical use 失效具体的1,4-二氢吡啶-3,5-二羧酸酯及其药物用途
公开(公告)号：US5342847A
公开(公告)日：1994-08-30
申请号：US1017
申请日：1993-01-16
IPC分类号： A61K31/445 , A61K31/44 , A61K31/451 , A61P9/00 , A61P9/10 , C07D211/90 , C07D211/86 , A61K31/455
CPC分类号： C07D211/90
摘要： The invention relates to the new dimethyl 2,6-dimethyl-1-n-propyl-4-(trifluoro-methylphenyl)-1,4-dihydropyridine-3-dicarboxylate, a process for its preparation and its use as a medicament in ischaemic diseases which are associated with disorders of the microcirculation. This action can occur both in the peripheral and in the cerebral vascular system.
摘要翻译： 本发明涉及新的2,6-二甲基-1-正丙基-4-（三氟 - 甲基苯基）-1,4-二氢吡啶-3-甲酸二甲酯，其制备方法及其作为缺血性药物的用途 与微循环障碍相关的疾病。 这种作用可能发生在外周和脑血管系统中。
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2.发明授权Specific 1,4-dihydropyridine-3,5-dicarboxylic acid ester, and its pharmaceutical use 失效特定的1,4-二氢吡啶-3,5-二羧酸酯及其药物用途
公开(公告)号：US5559139A
公开(公告)日：1996-09-24
申请号：US90722
申请日：1993-07-13
IPC分类号： A61K31/455 , A61K31/44 , A61P9/08 , A61P9/10 , C07D211/90 , C07D211/86
CPC分类号： C07D211/90
摘要： The invention relates to the new dimethyl 4-(4-chloro-3-trifluoromethylphenyl) -1-cyclopropyl-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, a process for its preparation and its use as a medicament in ischaemic diseases which are associated with disorders of the microcirculation. This action can occur both in the peripheral and in the cerebral vascular system.
摘要翻译： 本发明涉及新的4-（4-氯-3-三氟甲基苯基）-1-环丙基-2,6-二甲基-1,4-二氢吡啶-3,5-二甲酸二甲酯，其制备方法及其用途 与微循环障碍相关的缺血性疾病的药物。 这种作用可能发生在外周和脑血管系统中。
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3.发明授权Haemorheological use of N-alkylated 1,4-dihydropyridine-dicarboxylic acid esters, and some new compounds 失效N-烷基化1,4-二氢吡啶 - 二羧酸酯的血液流变学研究，以及一些新的化合物
公开(公告)号：US5432185A
公开(公告)日：1995-07-11
申请号：US65503
申请日：1993-05-21
IPC分类号： A61K31/445 , A61K31/44 , A61K31/451 , A61P9/08 , A61P9/10 , C07D211/90 , A61K31/455
CPC分类号： C07D211/90
摘要： Improving circulation, with minimal effect on blood pressure, using N-alkylated 1,4-dihydropyridines of the formula ##STR1## in which R.sup.1 represents hydrogen, nitro, cyano, trifluoromethyl, trifluoromethoxy, halogen or methyl,R.sup.2 represents hydrogen, halogen, nitro, hydroxyl, trifluoromethyl or methyl,R.sup.3 represents hydrogen or cyano, orR.sup.2 and R.sup.3 together form a fused benzo ring,R.sup.4 and R.sup.5 are identical or different and represent straight-chain or branched alkyl having up to 8 carbon atoms, which is optionally substituted by alkoxy having up to 4 carbon atoms, andR.sup.6 represents straight-chain or branched alkyl having up to 10 carbon atoms or represents cycloalkyl having 3 to 7 carbon atoms.Many of the compounds are new.
摘要翻译： 使用其中R 1表示氢，硝基，氰基，三氟甲基，三氟甲氧基，卤素或甲基的式（I）的N-烷基化1,4-二氢吡啶，改善循环，对血压影响最小，R 2表示氢， 卤素，硝基，羟基，三氟甲基或甲基，R 3表示氢或氰基，或R 2和R 3一起形成稠合的苯并环，R 4和R 5相同或不同，表示具有至多8个碳原子的直链或支链烷基， 任选被具有至多4个碳原子的烷氧基取代，R6代表具有至多10个碳原子的直链或支链烷基或代表具有3至7个碳原子的环烷基。 许多化合物是新的。
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公开(公告)号：US5234935A
公开(公告)日：1993-08-10
申请号：US680454
申请日：1991-04-04
IPC分类号： A61K31/445 , A61K31/44 , A61K31/451 , A61P9/08 , A61P9/10 , C07D211/90
CPC分类号： C07D211/90
摘要： Improving circulation, with minimal effect on blood pressure, using N-alkylated 1,4-dihydropyridines of the formula ##STR1## in which R.sup.1 represents hydrogen, nitro, cyano, trifluoromethyl, trifluoromethoxy, halogen or methyl,R.sup.2 represents hydrogen, halogen, nitro, hydroxyl, trifluoromethyl or methyl,R.sup.3 represents hydrogen or cyano, orR.sup.2 and R.sup.3 together form a fused benzo ring,R.sup.4 and R.sup.5 are identical or different and represent straight-chain or branched alkyl having up to 8 carbon atoms, which is optionally substituted by alkoxy having up to 4 carbon atoms, andR.sup.6 represents straight-chain or branched alkyl having up to 10 carbon atoms or represents cycloalkyl having 3 to 7 carbon atoms.Many of the compounds are new.
摘要翻译： 使用其中R 1表示氢，硝基，氰基，三氟甲基，三氟甲氧基，卤素或甲基的式（I）的N-烷基化1,4-二氢吡啶，改善循环，对血压影响最小，R 2表示氢， 卤素，硝基，羟基，三氟甲基或甲基，R 3表示氢或氰基，或R 2和R 3一起形成稠合的苯并环，R 4和R 5相同或不同，表示具有至多8个碳原子的直链或支链烷基， 任选被具有至多4个碳原子的烷氧基取代，R6代表具有至多10个碳原子的直链或支链烷基或代表具有3至7个碳原子的环烷基。 许多化合物是新的。
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公开(公告)号：US5328931A
公开(公告)日：1994-07-12
申请号：US917565
申请日：1992-07-21
IPC分类号： A61K31/435 , A61K31/44 , A61P25/18 , A61P25/28 , C07D211/90 , C07D213/55 , A61K31/455
CPC分类号： C07D211/90
摘要： N-alkylated 1,4-dihydropyridinedicarboxylic acid esters can be prepared either by reaction of aldehydes with acetoacetic esters and amines, optionally with isolation of the corresponding ylidene compounds, or by reaction of aminocrotonic acid esters with ylidene compounds and subsequent alkylation of the NH function. The N-alkylated 1,4-dihydropyridinedicarboxylic acid esters can be employed as active compounds in medicaments, in particular as cerebral therapeutics.
摘要翻译： N-烷基化的1,4-二氢吡啶二羧酸酯可以通过醛与乙酰乙酸酯和胺的反应制备，任选地分离相应的亚基化合物，或通过氨基巴豆酸酯与亚基化合物的反应和随后NH官能团的烷基化 。 N-烷基化的1,4-二氢吡啶二羧酸酯可以用作药物中的活性化合物，特别是作为脑治疗剂。
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公开(公告)号：US5407948A
公开(公告)日：1995-04-18
申请号：US239197
申请日：1994-05-06
申请人： Peter Fey , Walter Hubsch , Jurgen Dressel , Rudolf Hanko , Thomas Kramer , Ulrich Muller , Matthias Muller-Gliemann , Martin Beuck , Hilmar Bischoff , Stefan Wohlfeil , Dirk Denzer , Stanislav Kazda , Johannes-Peter Stasch , Andreas Knorr , Siegfried Zaiss
发明人： Peter Fey , Walter Hubsch , Jurgen Dressel , Rudolf Hanko , Thomas Kramer , Ulrich Muller , Matthias Muller-Gliemann , Martin Beuck , Hilmar Bischoff , Stefan Wohlfeil , Dirk Denzer , Stanislav Kazda , Johannes-Peter Stasch , Andreas Knorr , Siegfried Zaiss
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/4427 , A61K31/50 , A61K31/53 , A61P9/10 , A61P9/12 , A61P43/00 , C07D213/60 , C07D213/64 , C07D213/71 , C07D213/76 , C07D213/78 , C07D213/79 , C07D401/10 , C07D401/14
CPC分类号： C07D401/14
摘要： Substituted mono- and bipyridylmethylpyridones are prepared either by reaction of pyridones with mono- or bipyridylmethylhalogen compounds or by reaction of pyridone-substituted halogenopyridines with tetrazolylphenylboronic acids. The substituted mono- and bipyridylmethylpyridones can be employed as active compounds in medicaments, in particular for the treatment of arterial hypertension and atherosclerosis.
摘要翻译： 取代的单 - 和二吡啶基甲基吡啶酮通过吡啶酮与单吡啶基或联吡啶甲基卤化合物的反应或通过吡啶酮取代的卤代吡啶与四唑基苯基硼酸的反应来制备。 取代的单吡啶基和联吡啶基甲基吡啶酮可用作药物中的活性化合物，特别是用于治疗动脉高血压和动脉粥样硬化。
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7.发明申请Use of microsomal triglyceride transfer protein (MTP) inhibitors for reducing the number of postprandial triglyceride-rich lipoprotein particles (PPTRL) 审中-公开使用微粒体甘油三酯转运蛋白（MTP）抑制剂减少餐后富含甘油三酯的脂蛋白颗粒（PPTRL）公开(公告)号：US20060166999A1
公开(公告)日：2006-07-27
申请号：US11388810
申请日：2006-03-24
IPC分类号： A61K31/517 , A61K31/502 , A61K31/4745 , C07D487/02 , C07D471/02
CPC分类号： A61K31/437
摘要： The invention relates to the use of inhibitors of the microsomal triglyceride transfer protein (MTP) for reducing the number of postprandial triglyceride-rich lipoprotein particles (ppTRL) or for reducing their decomposition products i.e. the cholesterol-rich ‘small remnant particle’ (remnants). Said particles are associated with apolipoprotein B-48 (ApoB-48) and are designated as ‘ppTRL’ in the further course of events.
摘要翻译： 本发明涉及微粒体甘油三酯转运蛋白（MTP）的抑制剂用于减少餐后富含甘油三酯的脂蛋白颗粒数（ppTRL）或降低其分解产物的应用，即富含胆固醇的“小残余颗粒”（残留物） 。 所述颗粒与载脂蛋白B-48（ApoB-48）相关，并且在进一步的事件中被指定为“ppTRL”。
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公开(公告)号：US5935983A
公开(公告)日：1999-08-10
申请号：US960075
申请日：1997-10-24
申请人： Matthias Muller-Gliemann , Ulrich Muller , Martin Beuck , Siegfried Zaiss , Christoph Gerdes , Anke Domdey-Bette , Rudi Grutzmann , Stefan Lohmer , Stefan Wohlfeil , Ozkan Yalkinoglu , James Elting , Dirk Denzer
发明人： Matthias Muller-Gliemann , Ulrich Muller , Martin Beuck , Siegfried Zaiss , Christoph Gerdes , Anke Domdey-Bette , Rudi Grutzmann , Stefan Lohmer , Stefan Wohlfeil , Ozkan Yalkinoglu , James Elting , Dirk Denzer
IPC分类号： C07D235/16 , A61K31/415 , A61K31/4184 , A61K31/4188 , A61K31/435 , A61K31/437 , A61K31/44 , A61P9/00 , A61P9/10 , C07D235/08 , C07D235/18 , C07D471/04
CPC分类号： C07D471/04 , A61K31/4184 , A61K31/437 , C07D235/08 , C07D235/18
摘要： The phenylcyclohexylcarboxamides, some of which are known, are suitable as active compounds in medicaments, in particular in medicaments for the treatment of restenosis.
摘要翻译： 其中一些已知的苯基环己基甲酰胺适合作为药物中的活性化合物，特别是用于治疗再狭窄的药物。
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公开(公告)号：US5599823A
公开(公告)日：1997-02-04
申请号：US268903
申请日：1994-06-29
申请人： Matthias M uller-Gliemann , Martin Beuck , Stanislav Kazda , Johannes-Peter Stasch , Andreas Knorr , Stefan Wohlfeil , Walter H ubsch , J urgen Dressel , Peter Fey , Rudolf Hanko , Thomas Kr amer , Ulrich M uller , Siegfried Zaiss
发明人： Matthias M uller-Gliemann , Martin Beuck , Stanislav Kazda , Johannes-Peter Stasch , Andreas Knorr , Stefan Wohlfeil , Walter H ubsch , J urgen Dressel , Peter Fey , Rudolf Hanko , Thomas Kr amer , Ulrich M uller , Siegfried Zaiss
IPC分类号： A61K31/41 , A61K31/44 , A61K31/4412 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/4433 , A61K31/455 , A61P9/10 , A61P9/12 , C07D213/64 , C07D213/79 , C07D213/80 , C07D401/10 , C07D401/14 , C07D409/14
CPC分类号： C07D401/10
摘要： Substituted biphenylpyridones can be prepared by alkylating pyridones on the nitrogen. The substituted biphenylpyridones are suitable as active substances in medicaments, in particular in hypotensive and anti-atherosclerotic medicaments.
摘要翻译： 取代的联苯基吡啶酮可以通过在氮上烷基化吡啶酮来制备。 取代的联苯吡啶适合作为药物中的活性物质，特别是低血压和抗动脉粥样硬化药物。
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10.发明授权
公开(公告)号：US5395840A
公开(公告)日：1995-03-07
申请号：US193835
申请日：1994-02-08
申请人： Ulrich E. Muller , Jurgen Dressel , Peter Fey , Rudolf H. Hanko , Walter Hubsch , Thomas Kramer , Matthias Muller-Gliemann , Martin Beuck , Stanisiav Kazda , Stefan Wohlfeil , Andreas Knorr , Johannes-Peter Stasch , Siegfried Zaiss
发明人： Ulrich E. Muller , Jurgen Dressel , Peter Fey , Rudolf H. Hanko , Walter Hubsch , Thomas Kramer , Matthias Muller-Gliemann , Martin Beuck , Stanisiav Kazda , Stefan Wohlfeil , Andreas Knorr , Johannes-Peter Stasch , Siegfried Zaiss
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/4188 , A61K31/435 , A61P9/00 , A61P9/10 , A61P9/12 , A61P43/00 , C07D209/02 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/30 , C07D235/08 , C07D235/10 , C07D235/18 , C07D403/10 , C07D471/04
CPC分类号： C07D471/04
摘要： Heterocyclically substituted phenyl-cyclohexanecarboxylic acid derivatives are prepared by reacting appropriate heterocyclic compounds with cyclohexanebenzyl halides.The compounds can be employed as active compounds in medicaments for the treatment of arterial hypertension and atherosclerosis.
摘要翻译： 通过使适当的杂环化合物与环己烷苄基卤化物反应来制备杂环取代的苯基 - 环己烷羧酸衍生物。 该化合物可用作用于治疗动脉高血压和动脉粥样硬化的药物中的活性化合物。
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