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专利信息
专利号:WO-2011130852-A1
优先权日:2010-04-21
标题:Preparation of intermediates for the synthesis of dihydropyridine calcium channel blockers
发明人:SOUZA FABIO; PAN MING
权利人:ALPHORA RES INC; SOUZA FABIO; PAN MING
摘要:4- (2,3- dichlorophenyl) -1,4- dihydro- 2,6- dimethyl- 5- methoxycarbonyl- 3- pyridinecarboxylic acid, a key intermediate in the synthesis of the cardiovascular calcium channel blocker drug 3-butanoyloxymethoxycarbonyl-5- methoxycarbonyl-4- (2,3-dichlorophenyl) -2,6- dimethyl-1,4- dihydropyridine, of purity greater than 97% and essentially free of the corresponding diacid, is prepared by a process involving selective precipitation of its carboxylate via addition of concentrated solutions of alkali metal salts. Similar intermediate mono-carboxylic acids useful in the synthesis of other unsymmetrically substituted dihydropyrine drugs such as nisoldipine, nitrendipine and nimodipine can be similarly prepared and purified.
专利号:US-8455655-B2
优先权日:2010-05-07
标题:Preparation of dihydropyridines
发明人:VISHNU NEWADKAR RAVINDRANATH; PURUSHOTTAM JOSHI ANIL; KUMAR SINGH SANTOSH
权利人:VISHNU NEWADKAR RAVINDRANATH; PURUSHOTTAM JOSHI ANIL; KUMAR SINGH SANTOSH; LESVI LABORATORIOS SL
摘要:The invention relates to a method and compounds for the preparation of clevidipine butyrate, a very short acting hypertensive calcium antagonist, as well as the synthesis of these compounds useful for the preparation of clevidipine (also known as clevidipine butyrate). Moreover the invention also discloses polymorphic forms of clevidipine butyrate, useful for the preparation of pharmaceutical compositions, and processes to prepare them.
专利号:CA-2701272-A1
优先权日:2010-04-21
标 题 :Preparation of intermediates for the synthesis of dihydropyridine calcium channel blockers
专利号:US-5258519-A
优先权日:1990-11-13
标 题:Dihydropyridine vasodilators agents
发明人:WHEELER THOMAS N; KENAKIN TERRENCE P
权利人:GLAXO INC
摘要:Compounds of the following formula (I): (I) where R1 and R2 are alkyl or cycloalkyl, which may be substituted, R4 is aryl such as phenyl which may be substituted, L is a direct bond or an oxygen containing linking group, R is a hydrogen, alkyloxy, alkyl, halogen or haloalkyl and Het is a pyridinyl or pyridazinyl group. The compounds can be used antihypertensives or myocardial relaxants. Also part of the invention are pharmaceutical compositions, intermediates and methods of synthesis.
专利号:US-5100892-A
优先权日:1990-11-13
标 题 :Dihydropyridine vasodilator agents
发明人:WHEELER THOMAS N; KENAKIN TERRENCE P
权利人:GLAXO INC
摘要:Compounds of the following formula (I): (I) where R1 and R2 are alkyl or cycloalkyl, which may be substituted, R4 is aryl such as phenyl which may be substituted, L is a direct bond or an oxygen containing linking group, R is a hydrogen, alkyloxy, alkyl, halogen or haloalkyl and Het is a pyridinyl or pyridazinyl group. The compounds can be used antihypertensives or myocardial relaxants. Also part of the invention are pharmaceutical compositions, intermediates and methods of synthesis.