发明名称 BI-PYRROLIDINYLVINL (CARBA) CEPHALOSPORINS
摘要 <p>The present invention relates to cephalosporin derivatives of general formula (I), wherein R is R<4> -Ys-(CR<5>R<6>)m- or (formula a) R<1>, R<2> are each independently hydrogen or lower alkyl; R<3> is hydrogen, hydroxy-lower alkyl or carbamoylmethyl; Z is phenylene, heterocyclylen or naphthylene; R<4> is halogen, phenyl, benzyl, naphthyl or heterocyclyl, the phenyl, benzyl, naphthyl or heterocyclyl being optionally substituted by at least one of halogen, hydroxy, optionally substituted lower alkyl, lower alkoxy, amino, lower alkylamino, di-lower alkylamino, carboxy, lower alkoxycarbonyl or carbamoyl; Q is S or CH2; Y is S, O, NH or CH2; M is 0 or 1; s is 0 or 1; R<5>, R<6> are each independently hydrogen or lower alkyl; X is CR<8> or N; R<7> is hydrogen, lower alkyl, lower cycloalkyl, formyl, acetyl or pivaloyl; R<8> is hydrogen or halogen; and 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 WO0032605(A1) 申请公布日期 2000.06.08
申请号 WO1999EP09120 申请日期 1999.11.25
申请人 F. HOFFMANN-LA ROCHE AG 发明人 HEBEISEN, PAUL;HEINZE-KRAUSS, INGRID;RICHTER, HANS
分类号 A61P31/00;C07D463/00;C07D501/00;C07D501/52;C07D501/56;(IPC1-7):C07D501/52;A61K31/545 主分类号 A61P31/00
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