发明名称 3-[2-OXO-PYRROLIDINYL-3-YLIDENE]METHYLENE SUBSTITUTED 7-[2-(5-AMINO-[1,2,4]THIADIAZOL-3-YL)2-HYDROXYIMINO-ACETYLAMINO ]-CEPHALOSPORIN DERIVATIVES AND MEDICAMENTS
摘要 <p>The present invention relates to cephalosporin derivatives of the general formula <CHEM> wherein X is CH or N; R<1> is hydrogen or cyclopentyl; R<2> is a group of formula <CHEM> R<3> is hydrogen, an alkalimetal ion or a tertiary ammonium group; R<4> is hydrogen, an amino protecting group, pyrrolidin-2-ylmethyl, azetidin-3-ylmethyl, iminomethyl, 1-carbamimidoyl; R<5> is hydrogen, dialkylcarbamoyl, omega -hydroxyalkyl, omega -aminoalkyl, pyridinium-1-ylmethyl, 1-hydroxy-3-aminomethyl-propyl or (hydroxy)-(pyrrolidin-2-yl)methyl; R<6> is hydrogen, trifluoromethyl or hydroxy; and R<7> is alkyl, omega -hydroxy-alkyl, cycloalkyl, 3-pyrrolidinyl, 3-azetidinyl, iminomethyl or 1-carbamimidoyl; as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts; the invention is further concerned with the manufacture of compounds of formula I; with their use as pharmaceutically active substances, particularly for the treatment and prophylaxis of infectious diseases, and with pharmaceutical preparations containing a compound of formula I for the treatment and prophylaxis of infectious diseases.</p>
申请公布号 NZ329363(A) 申请公布日期 1999.01.28
申请号 NZ19970329363 申请日期 1997.12.09
申请人 F HOFFMANN-LA ROCHE AG 发明人 ANGEHRN, PETER;HEBEISEN, PAUL;HEINZE-KRAUSS, INGRID;PAGE, MALCOLM;RUNTZ, VALERIE
分类号 A61K31/545;A61K31/546;A61P31/04;C07D417/12;C07D501/00;C07D501/04;C07D501/06;C07D501/24;C07D501/34;C07D501/56;C07F9/572;C07F9/6558;(IPC1-7):C07D501/48 主分类号 A61K31/545
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