发明授权
- 专利标题: Rapamycin oximes
- 专利标题(中): 雷帕霉素肟
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申请号: US134237申请日: 1993-10-08
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公开(公告)号: US5373014A公开(公告)日: 1994-12-13
- 发明人: Amedeo A. Failli , Robert J. Steffan , Craig E. Caufield , David C. Hu , Alexander A. Grinfeld
- 申请人: Amedeo A. Failli , Robert J. Steffan , Craig E. Caufield , David C. Hu , Alexander A. Grinfeld
- 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: C07D498/18
- IPC分类号: C07D498/18 ; A61K31/395 ; C07D491/16
摘要:
A compound of the structure ##STR1## wherein R.sup.1 is ##STR2## R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.3 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or --CO.sub.2 R.sup.8 ;R.sup.4 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, Ar, aminoalkyl, thioalkyl, alkylthioalkyl, hydroxyalkyl, or --CO.sub.2 R.sup.8 ;R.sup.5 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, At, or --CO.sub.2 R.sup.8 ;R.sup.6 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.7 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, fluorenylmethyl, orAr;Y is O or S;X is .dbd.N--O--(CH.sub.2).sub.f --Z or .dbd.N--O--Ar;Z is hydrogen, alkenyl, alkynyl, alkoxy, cyano, fluoro, trifluoromethyl, --NR.sup.5 R.sup.6, aryloxy, or Ar;Ar is aryl which may be optionally mono-, di-, or tri- substituted;a=0-4;b=0-1;c=0-4;d=0-6;e=0-6; andf=0-6;or a pharmaceutically acceptable salt thereof, with the proviso that when f is 0, Z is hydrogen and further provided that when R.sup.3 or R.sup.5 is --CO.sub.2 R.sup.8, R.sup.8 is not hydrogen which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
公开/授权文献
- US6000859A Camera and flash unit positioning device 公开/授权日:1999-12-14
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