专利号:US-8895747-B2 优先权日:2009-07-27 标 题 :Method and substances for preparation of N-substituted pyridinium compounds 发明人:HEINDL DIETER; MAERZ HERIBERT; SCHMIDT AXEL 权利人:HEINDL DIETER; MAERZ HERIBERT; SCHMIDT AXEL; ROCHE DIAGNOSTICS OPERATIONS 摘要:Methods for the synthesis of N-substituted pyridinium compounds by using an N-heteroaryl substituted pyridinium salt (Zincke salt) and reacting it with a nucleophilic amine are provided. Novel purine-substituted pyridyl compounds, which may be useful reagents in the above reaction, are also disclosed.
专利号:JP-6038111-B2 优先权日:2014-12-27 标 题:2,6-Dichloro-8-iodo-7-deazapurine for the synthesis of polysubstituted 7-deazapurine derivatives
专利号:US-2013123498-A1 优先权日:2011-10-19 标 题 :Process for the preparation of etravirine and intermediates in the synthesis thereof 发明人:MAJER MAJA SEPELJ; KRIZMANIC IRENA; VRBANEC GORDANA 权利人:MAJER MAJA SEPELJ; KRIZMANIC IRENA; VRBANEC GORDANA 摘要:The present invention includes compounds of Formula 1 of the following structure: n n n n n n n n n n or salts thereof, wherein X is a halogen or a tosyl group. Processes for preparing the compounds of Formula 1 are disclosed in the patent application. The compounds of Formula 1 are useful as intermediates for preparation of Etravirine. The present invention is also directed toward processes for preparing Etravirine.
专利号:WO-2012170647-A1 优先权日:2011-06-09 标题 :Process for the preparation of etravirine and intermediates in the synthesis thereof 发明人:SEPELJ MAJER MAJA; KRIZMANIC IRENA; SEPAC DRAGAN 权利人:ASSIA CHEM IND LTD; TEVA PHARMA; SEPELJ MAJER MAJA; KRIZMANIC IRENA; SEPAC DRAGAN 摘要:The present patent application provides intermediates, e.g., 4-(6-(acetylamino)-2- chloropyrimidin-4-yloxy)-3,5-dimethylbenzonitrile, for preparing Etravirine or the salts of Etravirine, and processes for preparing Etravirine or its salts as disclosed in the specification herein. The application also provides processes for preparing 4-(6-(acetylamino)-2- chloropyrimidin-4-yloxy)-3,5-dimethylbenzonitrile.
专利号:US-6472403-B2 优先权日:2000-01-20 标 题 :αV integrin receptor antagonists 发明人:DUGGAN MARK E; HALCZENKO WASYL; HUTCHINSON JOHN H; LI AIWEN; MEISSNER ROBERT S; PERKINS JAMES J; STEELE THOMAS G; WANG JIABING; PATANE MICHAEL A 权利人:MERCK & CO INC 摘要:The present invention relates to novel imidazolidinone derivatives thereof, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3 and/or αvβ5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.