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:US-3929840-A 优先权日:1972-07-14 标题 :Labile esters of ({31 )(cis-1,2-epoxypropyl)phosphonic 发明人:CHRISTENSEN BURTON G; LEANZA WILLIAM J; ALBERS-SCHONBERG GEORG 权利人:MERCK & CO INC 摘要:Labile esters of (-)(cis-1,2-epoxypropyl)phosphonic acid are prepared from the free acid or salts thereof by reaction with an alcohol or a hydrocarbyl halide. In addition to their utility as intermediates in the synthesis of antibacterially active salts of (-)(cis-1,2-epoxypropyl)phosphonic acid, those esters have significant antibacterial activity.
专利号:US-9907796-B2 优先权日:2012-10-04 标题:Methods of treating tumoral diseases, or bacterial or viral infections 发明人:DEOKAR RHUSHIKESH CHANDRABHAN; DUGAR SUNDEEP; MAHAJAN DINESH; WERNER MILTON HENRY 权利人:DEOKAR RHUSHIKESH CHANDRABHAN; DUGAR SUNDEEP; MAHAJAN DINESH; WERNER MILTON HENRY; INHIBIKASE THERAPEUTICS INC 摘要:Novel compounds and their synthesis are described. Methods for using these compounds in the prevention or treatment of cancer, a bacterial infection or a viral infection in a subject are also described.
专利号:US-9359376-B2 优先权日:2011-04-08 标题:Substituted methylformyl reagents and method of using same to modify physicochemical and/or pharmacokinetic properties of compounds 发明人:DUGAR SUNDEEP; MAHAJAN DINESH; HOLLINGER FRANK PETER 权利人:DUGAR SUNDEEP; MAHAJAN DINESH; HOLLINGER FRANK PETER; SPHAERA PHARMA PTE LTD 摘要:The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.
专利号:US-9802975-B2 优先权日:2014-06-10 标题:Protecting groups for “Z nucleotide†and methods thereof 发明人:LUNSTAD BENJAMIN D; DELLINGER DOUGLAS J 权利人:AGILENT TECHNOLOGIES INC 摘要:The present disclosure provides nucleoside compounds and oligonucleotides including an unnatural 6-amino-2-pyridone heterocyclic base where the 6-amino and 2-positions are protected. The 2-position of the heterocyclic base can be protected with an acyl-oxy-methyl protecting group. In some embodiments, the protected heterocyclic base has the following structure where AcOM is an acetyl-oxy-methyl group and R is a ribose or deoxyribose sugar: n n n n n n n n n n Methods for synthesizing an oligonucleotide are provided in which the subject compounds find use. The method can include protecting an unnatural (e.g., Z) nucleotide with an acetyl-oxy-methyl group; incorporating the protected unnatural nucleotide into a nucleotide sequence on a solid support; and removing the acetyl-oxy-methyl group from the unnatural nucleotide incorporated into the nucleotide sequence. The compounds and methods find use in the synthesis of long oligonucleotides including Z nucleotides.