- 专利标题: Carbamates of rapamycin
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申请号: US54655申请日: 1993-04-23
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公开(公告)号: US5302584A公开(公告)日: 1994-04-12
- 发明人: Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
- 申请人: Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
- 申请人地址: NJ Madison
- 专利权人: American Home Products Corporation
- 当前专利权人: American Home Products Corporation
- 当前专利权人地址: NJ Madison
- 主分类号: A61K31/435
- IPC分类号: A61K31/435 ; A61K31/395 ; A61K31/436 ; A61K31/44 ; A61K31/675 ; A61K31/70 ; A61P9/00 ; A61P29/00 ; A61P37/06 ; C07D20060101 ; C07D221/00 ; C07D273/00 ; C07D311/00 ; C07D487/18 ; C07D491/06 ; C07D498/18 ; C07H19/01 ; C07J1/00
摘要:
A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONH--[(CR.sup.3 R.sup.4).sub.m (--A--(CR.sup.5 R.sup.6).sub.n).sub.p ].sub.q --B; ##STR2## R.sup.3, R.sup.4, R.sup.5, R.sup.6, and B are each, independently, hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, cycloalkyl, --OR.sup.7, --SR.sup.7, halogen, --CN, --NO.sub.2, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, --OSO.sub.3 R.sup.7, --NR.sup.7 R.sup.8, --NHCOR.sup.7, --NHSO.sub.2 R.sup.7, or Ar;R.sup.7 and R.sup.8 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl;R.sup.9 and R.sup.10 are each, independently, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, or Ar;A is --CH.sub.2 --, --NR.sup.7 --, --O--, --S--, --SO--, --SO.sub.2 --, --PR.sup.7 --, --CO--, --NHCO--, --NHSO--, or --P(O)(R.sup.7)--;Ar is phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, quinoxalyl, thienyl, thionaphthyl, furyl, benzofuryl, benzodioxyl, benzoxazolyl, benzoisoxazolyl, indolyl, thiazolyl, isoxazolyl, pyrimidinyl, pyrazinyl, imidazolyl, benzopyranyl, benz[b]thiophenolyl, benzimidazolyl, benzthiazolyl, benzodioxolyl, piperidinyl, morpholinyl, piperazinyl, tetrahydrofuranyl, or pyrrolidinyl; wherein the Ar group may be optionally mono-, di-, or tri- substituted; ##STR3## is a nitrogen containing heterocycle that may be saturated, unsaturated, or partially unsaturated, and may be optionally mono-, di-, or tri- substituted; with the proviso that R.sup.1 and R.sup.2 are not both hydrogen;m=0-6;n=0-6;p=0-1;q=0-1;or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
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