专利号:US-9802934-B2 优先权日:2013-10-17 标 题 :Process for the synthesis of (R)-praziquantel 发明人:QIAN MINGXIN 权利人:TONGLI BIOMEDICAL CO LTD 摘要:The present disclosure relates to a process and new intermediates for the synthesis of (R)-praziquantel, which is obtained through four steps in proper order, that is, condensation reaction, reduction reaction, acylation reaction and ring-closing reaction, using (1R)-2-substituted-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid as starting material. Overall, the present disclosure provides a (R)-praziquantel product with higher optical purity through a process route that is more cost effective and environmentally friendly.
专利号:US-6608196-B2 优先权日:2001-05-03 标题 :Process for solid supported synthesis of pyruvate-derived compounds 发明人:WANG BING; JANAGANI SATYANARAYANA; CALLAWAY WYETH B; SESSLER JONATHAN L 权利人:GALILEO PHARMACEUTICALS INC 摘要:Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.
专利号:US-2007015798-A1 优先权日:2005-02-25 标 题 :Efficient and stereoselective process for large scale synthesis of (3R)-3-(2,3-dihydrobenzofuran-5-yl)-1,2,3,4-tetrahydropyrrolo[3,4-b]quinolin-9-one derivatives 发明人:LI XUN; LEMAIRE SEBASTIEN; MARKO ISTVAN; WILLEMSENS ALBERT 权利人:LI XUN; LEMAIRE SEBASTIEN; MARKO ISTVAN; WILLEMSENS ALBERT 摘要:This invention relates to an efficient process for large scale stereoselective production of (3R)-3-(2,3-dihydrobenzofuran-5-yl)-1,2,3,4-tetrahydropyrrolo[3,4-b]quinolin-9-ones and key intermediates used for the preparation of benzofuranyl pyrroloquinolones as potent and selective PDE5 inhibitors for the treatment of erectile dysfunction, as well as pharmaceutical compositions and methods of treatment utilizing these compounds.
专利号:US-5712269-A 优先权日:1993-04-05 标题 :M2 receptor ligand for the treatment of neurological disorders 发明人:MCCABE R TYLER; WILSON BRYAN R; RHODES CHRISTOPHER A 权利人:PHARMACEUTICAL DISCOVERY CORP 摘要:Muscarinic M2 receptor ligands are described which are suitable for the treatment of neurological disorders, and which may be administered with minimal side-effects. A method of synthesis of these compounds is also described.
专利号:US-11091445-B2 优先权日:2016-10-24 标题 :Compounds, process for obtaining the compounds, pharmaceutical composition, use of the compounds and method for treating psychiatric disorders and/or sleep disorders 发明人:RUCH WERNECK GUIMARÃES CRISTIANO; FELYPE ZANETI DE AZEVEDO HATYLAS; MASCARELLO ALESSANDRA; WATANABE DA COSTA RENATA; FREIRE TORRES RUSSO VALTER; MANNOCHIO DE SOUZA RUSSO ELISA 权利人:ACHE LABORATORIOS FARMACEUTICOS SA 摘要:The present disclosure relates to novel and inventive pharmacologically active benzimidazole derivative compounds, which surprisingly have high affinity for melatonin MT1 and MT2 receptors and low affinity for CYP450 complex enzymes, specially CYP1A2. The present invention also relates to novel and inventive routes of synthesis of these compounds, pharmaceutical compositions comprising the compounds and the use of these compounds in the treatment of individuals affected by psychiatric disorders and/or sleep disorders related to these receptors (specially depression, anxiety, circadian cycle disorders), in addition to a process for producing the composition.
专利号:US-4620009-A 优先权日:1980-03-17 标 题 :Synthesis of intermediates for tetramisole, levamisole and their derivatives 发明人:RAGHU SIVARAMAN; HOFFMANN ARTHUR K; SINGH BALWANT 权利人:CYANAMID AGRICULTURAL DE PUERT 摘要:A process for the manufacture of 1-(2-alkoxyethyl)-4-phenyl-4-imidazolin-2-ones, 1-(2-alkoxyethyl)-4-phenyl-2-imidazolidones, 1-(2-alkoxyethyl)-4-phenyl-imidazolidine-2-thiones, certain of the corresponding 1-(2-hydroxyethyl) derivatives and their 3-acylated derivatives, and certain related compounds which are all useful as intermediates in a new process for the manufacture of tetramisole, dl-2,3,5,6-tetrahydro-6-phenylimidazo-[2,1-b]thiazole, and its derivatives. The compound tetramisole is useful as an anthelmintic.
[参考文献]: Shigeo Hayashi, Et Al. Design, Synthesis And Structure-Activity Relationship Studies Of Novel And Diverse Cyclooxygenase-2 Inhibitors As Anti-Inflammatory Drugs. J Enzyme Inhib Med Chem. 2014 Dec;29(6):846-67.
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