专利号:US-2012115907-A1 优先权日:2009-04-24 标题 :Novel compounds as inhibitors of renin 发明人:THOMBARE PRAVAIN; DESAI JIGAR; JAIN MUKUL R 权利人:THOMBARE PRAVAIN; DESAI JIGAR; JAIN MUKUL R; CADILA HEALTHCARE LTD 摘要:The present invention relates to novel renin inhibitors of general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (1), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
专利号:EP-0830136-B1 优先权日:1995-03-07 标 题:New cryptophycins from synthesis 发明人:MOORE RICHARD E; TIUS MARCUS A; BARROW RUSSELL A; LIANG JIAN; CORBETT THOMAS H; VALERIOTE FREDERICK A; HEMSCHEIDT THOMAS K; GOLAKOTI TRIMURTULU 权利人:UNIV HAWAII; UNIV WAYNE STATE 摘要:Novel cryptophycin compounds are disclosed, together with methods of producing cryptophycins by total synthesis and methods for the use of such cryptophycins in pharmaceuticals to inhibit the proliferation of mammalian cells and to treat neoplasia.
专利号:US-6013626-A 优先权日:1993-12-21 标题 :Cryptophycins from synthesis 发明人:MOORE RICHARD E; TIUS MARCUS A; BARROW RUSSELL A; LIANG JIAN; CORBETT THOMAS H; VALERIOTE FREDERICK A; GOLAKOTI TRIMURTULU; HEMSCHEIDT THOMAS K 权利人:UNIV HAWAII; UNIV WAYNE STATE 摘要:A cryptophycin compound is provided having the structure: ##STR1## Further provided are methods of producing cryptophycins by total synthesis and methods of using cryptophycins in pharmaceuticals. It is a further object of this invention to use cryptophycins to inhibit the proliferation of mammalian cells. Moreover, methods of using cryptophycins to treat neoplasia is also provided.
专利号:US-4086423-A 优先权日:1973-10-12 标题 :Process for cephem synthesis 发明人:FIRESTONE RAYMOND A; RATCLIFFE RONALD W; CHRISTENSEN BURTON G 权利人:MERCK & CO INC 摘要:Cephalosporin antibiotics of the formula: ##STR1## are produced by cycloaddition of a glycine derivative of the formula ##STR2## with a thiazine derivative of the formula ##STR3##
专利号:US-4051132-A 优先权日:1974-01-23 标 题 :Process for epimerizing beta-lactam antibiotic compounds by means of an acid quench 发明人:FIRESTONE RAYMOND A 权利人:MERCK & CO INC 摘要:Total synthesis methods employ 7-amino (6-amino in the case of a penicillin derivative) group in the alpha configuration. The instant invention provides a general route for preparing the 7β-amino (or 6β-amino) compound, through the formation of an imino-containing intermediate, followed by hydrolysis to the desired epimer. Novel intermediate products are provided. The compounds having the desired beta epimer can be converted to acylamino-antibiotics.
专利号:US-4167630-A 优先权日:1975-12-24 标 题 :Process for epimerizing beta-lactam antibiotic compounds, and related products 发明人:FIRESTONE RAYMOND A 权利人:MERCK & CO INC 摘要:Through total synthesis methods developed in the assignee's laboratories, new as well as old penicillin and cephalosporin compounds (all containing the beta-lactam functional group) have been prepared. One of the key intermediates prepared by total synthesis has the 7-amino (6-amino in the case of a penicillin derivative) group in the alpha configuration. The instant invention provides a general route for preparing the 7β-amino (or 6β-amino) compound, through the formation of an imino-containing intermediate, followed by hydrolysis to the desired epimer. Novel intermediate products are provided. The compounds having the desired beta epimer can be converted to acylaminoantibiotics.