专利号:US-5656634-A 优先权日:1991-03-21 标题 :N-aryl and N-heteroarylamide and urea derivatives as inhibitors of acyl coenzyme A: cholesterol acyl transferase (ACAT) 发明人:CHANG GEORGE; HAMANAKA ERNEST S; MCCARTHY PETER A; TRUONG THIEN V; WALKER FREDERICK J 权利人:PFIZER 摘要:Compounds of the formula ##STR1## the pharmaceutically acceptable salts thereof, wherein Q and R 1 are as defined below, and novel carboxylic acid and acid halide intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.
专利号:US-5869676-A 优先权日:1997-05-15 标题:Process for the synthesis of ribonucleotide reductase inhibitors 3-AP and 3-AMP 发明人:NIU CHUANSHENG; LI JUN; LI XIUYAN; DOYLE TERRENCE W; CHEN SHU-HUI 权利人:VION PHARMACEUTICALS INC 摘要:The present invention relates to improved, efficient chemical syntheses of 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP) and 3-amino-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP).
专利号:US-6514997-B2 优先权日:1999-12-03 标题:Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis 发明人:DRAGOVICH PETER S; PRINS THOMAS J; ZHOU RU; JOHNNSON JR THEODORE O 权利人:AGOURON PHARMA 摘要:Compounds of the formula: n where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the picornaviral 3C protease. Also disclosed are compounds of the formula: n where the formula variables are as defined herein that advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as rhinovirus 3C proteases. Intermediates and synthetic methods for preparing such compounds are also described.
专利号:RU-2198875-C2 优先权日:1997-05-15 标 题:Methods of synthesis of pyridine-2-carboxaldehyde thiosemicarbazones and intermediate pyridine-2-carboxaldehydes
专利号:US-5596001-A 优先权日:1993-10-25 标题 :4-aryl-3-(heteroarylureido)quinoline derivatves 发明人:HAMANAKA ERNEST S 权利人:PFIZER 摘要:Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , m, X and Q are as defined below, and novel intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and natiatherosclerosis agents.
专利号:EP-0984932-A4 优先权日:1997-05-15 标题:METHOD FOR THE SYNTHESIS OF THE RIBONUCLEOTIDE REDUCTASE INHIBITORS 3-AP AND 3-AMP