专利号:US-3962217-A 优先权日:1969-10-24 标 题 :Process for the manufacture of Δ16 -steroid-14β,18,20-triols and -14β,20-diol-18-ols of the pregnane series 发明人:WEHRLI HANSULI; JEGER OSKAR 权利人:CIBA GEIGY CORP 摘要:The invention is for a selective reduction of the 20- oxo group in Δ 16 -steroid-14β,18-diol-20-ones of the pregnane series to form the two epimeric 20-alcohols having the 20 S and 20 R configuration. The process is especially intended for the manufacture of alkaloids of the batrachotoxin type, particularly for batrachotoxinine A, which is a pregnane derivative having a 20 S alcohol grouping, and epimers and derivatives, such as epi-batrachotixinine A or 7,8-dihydrobatrachotoxinine A. The process is characterized by reducing the said Δ 16 -steroid-14β,18-diol-20-ones in form of their 14,18-ketals, for instance the 14,18 acetonides and using appropriate complex light metal hydrides and operating at appropriate temperatures. The separation of the two isomers is easy and can be effected by the usual physical operations, such as crystallization or chromatography. In the 14β,18,20-triols obtained the 18-hydroxy group can be dehydrogenated to the corresponding 18-aldehydes, which are intermediates necessary in the synthesis of the said pharmacological interesting substances, such as batrachotoxin, by treatment with a sulphoxide in the presence of a carboxylic acid anhydride.
专利号:US-4713383-A 优先权日:1984-10-01 标 题:Triazoloquinazoline compounds, and their methods of preparation, pharmaceutical compositions, and uses 发明人:FRANCIS JOHN E; GELOTTE KARL O 权利人:CIBA GEIGY CORP 摘要:[1,2,4]triazolo[1,5-c]quinazoline compounds of the formula wherein R1 is optionally substituted phenyl, pyridyl, furyl thienyl, dihydro or tetrahydro furanyl or thienyl, pyranyl, or 0-ribofuranosyl; R2 is hydrogen or lower alkyl; X is oxygen or NR3, R3 is as defined in the claims, and ring A is unsubstituted or substituted as set forth in the claims. The compounds wherein X is N-R3 are especially useful as adenosine antagonists and for the treatment of asthma. The compounds wherein X is oxygen are useful as benzodiazepine antagonists and as intermediates in the synthesis of the compounds wherein X is N-R3.
专利号:US-8598166-B2 优先权日:2008-03-21 标 题:Polysubstituted derivatives of 6-heteroarylimidazo[1,2-a]pyridines, and preparation and therapeutic use thereof 发明人:DE PERETTI DANIELLE; EVANNO YANNICK; MACHNIK DAVID; RAKOTOARISOA NATHALIE 权利人:DE PERETTI DANIELLE; EVANNO YANNICK; MACHNIK DAVID; RAKOTOARISOA NATHALIE; SANOFI SA 摘要:Compounds of formula (I): n nwherein R 1 , R 2 , R 3 , R 4 , Het and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
专利号:US-12180188-B2 优先权日:2020-05-19 标题:Antifibrotic compounds and related methods 发明人:STEFANOVIC BRANKO; NEFZI ADEL 权利人:UNIV FLORIDA STATE RES FOUND; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:This discloses that compounds of Formula 1 have antifibrotic properties. In particular, this discloses a pharmaceutical composition including one or more compounds of Formula 1 and methods of using compounds of Formula 1 in fibrosis treatment and inhibiting type 1 collagen synthesis.
专利号:WO-2005082899-A1 优先权日:2004-01-28 标 题:Oxazolidinone derivatives as antimicrobials 发明人:SALMAN MOHAMMAD; BISWAJIT DAS; RUDRA SONALI; YADAV AJAY SINGH; RATTAN ASHOK 权利人:RANBAXY LAB LTD; SALMAN MOHAMMAD; BISWAJIT DAS; RUDRA SONALI; YADAV AJAY SINGH; RATTAN ASHOK 摘要:The present invention relates to certain substituted phenyl oxazolidinones of formula (I) and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing such compounds as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacterioides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
专利号:WO-2006043121-A1 优先权日:2004-10-20 标 题:Oxazolidinone derivatives as antimicrobials 发明人:MEHTA ANITA; DAS BISWAJIT; RUDRA SONALI; YADAV AJAY SINGH; KUMARI SANGITA; SALMAN MOHAMMAD; RATTAN ASHOK 权利人:RANBAXY LAB LTD; MEHTA ANITA; DAS BISWAJIT; RUDRA SONALI; YADAV AJAY SINGH; KUMARI SANGITA; SALMAN MOHAMMAD; RATTAN ASHOK 摘要:The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
摘要:Littke, A., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 215. 摘要:Andersson, C.-M.; Andersson, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 42. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026).