发明名称 Trypsin-like serine protease inhibitors, and their preparation and use
摘要 Glycylglycine derivatives with a benzylsulfonylamido group at one end of the chain and an amidino-organylamido group at the other end are new, including their racemates, crystal forms, hydrates and salts. Compounds (I) of the formula shown are new, and also their racemates, crystal forms, hydrates and salts with organic or inorganic acids. i : 0 or 1, preferably 0; R4H or OH, preferably H; A : 1,4-phenylene, 1,4-cyclohexylene, pyridine-2,5- or -3,6-diyl, or thiophene-2,5-diyl, preferably phenylene; R1H, COOH, COOR5, aminomethyl, halogen or pseudohalogen, preferably COOH; R5 : methyl or ethyl; R33-aminophenyl, 4-pyridylmethyl, 4-amidinophenylmethyl or 4-aminomethylphenylmethyl; R23-12C alkyl (optionally cycloalkyl-substituted), 6-14C aryl or aralkyl, heteroaryl or as 6-12C heteroarylalkyl with 1-3 hetero-atoms, -CH2-(CH2)p-phenylene-R6, -CH2-(CH2)p-cyclohexyl, -(CH2)p-(1- or 2-naphthyl) or -CH2-(CH2)p-CH2-NHCOO-CH2-phenyl; R6halogen or pseudohalogen; p : 0, 1 or 2 . [Image]
申请公布号 AU2007308421(A1) 申请公布日期 2008.05.02
申请号 AU20070308421 申请日期 2007.10.24
申请人 THE MEDICINES COMPANY (LEIPZIG) GMBH 发明人 MOHAMMED DAGHISCH;ANETT SOFFING;ANDREA SCHWEINITZ;JORG STURZEBECHER;CLAUDIA REICHELT;PETER STEINMETZER;ANDREAS VAN DE LOCHT;SILKE NICKLISCH;TORSTEN STEINMETZER;ALEXANDER SCHULZE;JOCHEN HEINICKE;FRIEDRICH-ALEXANDER LUDWIG
分类号 C07C311/33;A61K31/18;A61K31/44;A61P7/02;C07D213/56;C07D213/89;C07D233/64 主分类号 C07C311/33
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