发明授权
US4681938A Novel polycyclic hydrazones of rifamycins, their manufacture, and their pharmaceutical compositions for treating tuberculosis 失效
利福霉素的新型多环腙,其制造及其用于治疗结核病的药物组合物

  • 专利标题: Novel polycyclic hydrazones of rifamycins, their manufacture, and their pharmaceutical compositions for treating tuberculosis
  • 专利标题(中): 利福霉素的新型多环腙,其制造及其用于治疗结核病的药物组合物
  • 申请号: US763725
    申请日: 1985-08-08
  • 公开(公告)号: US4681938A
    公开(公告)日: 1987-07-21
  • 发明人: Peter Traxler
  • 申请人: Peter Traxler
  • 申请人地址: NY Ardsley
  • 专利权人: Ciba-Geigy Corporation
  • 当前专利权人: Ciba-Geigy Corporation
  • 当前专利权人地址: NY Ardsley
  • 主分类号: C07D498/08
  • IPC分类号: C07D498/08 C07D519/00 A61K31/395 A61K31/495
Novel polycyclic hydrazones of rifamycins, their manufacture, and their
pharmaceutical compositions for treating tuberculosis
摘要:
Novel hydrazones derived from 3-formylrifamycin S or SV as the aldehydo component and a bi- or tri-cyclic N-aminopiperazine as the hydrazino component and having the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6, independently of one another, each represents a hydrogen atom or C.sub.1-4 -alkyl,m and n, independently of one another, each represents an integer from 0 to 5,X represents C.sub.1-5 -alkylidene, benzylidene or C.sub.1-4 -alkoxymethylene,Y represents C.sub.1-5 -alkylidene, C.sub.1-4 -alkoxymethylene, oxy, thio or optionally substituted imino of the formula --N(R)-- wherein R represents hydrogen, C.sub.1-4 -alkyl, C.sub.3-5 -alkenyl, C.sub.3-12 -cycloalkyl or phenyl, orX and Y together represent 1,2-cycloalkylene or o-phenylene each of which can be substituted by from one to three C.sub.1-4 -alkyl radicals, andRif represents a radical of rifamycin S or SV that is bonded in the 3-position by the free valency,are distinguished by a high and long-lasting antituberculotic activity. They are manufactured in conventional manner, for example by condensation of their components.
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