发明授权
- 专利标题: Carbamates of rapaycin
- 专利标题(中): 高分子化合物的氨基甲酸酯
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申请号: US449593申请日: 1995-05-24
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公开(公告)号: US5559227A公开(公告)日: 1996-09-24
- 发明人: Amedeo A. Failli , Oleg I. Bleyman , Wenling Kao , Magid A. Abou-Gharbia
- 申请人: Amedeo A. Failli , Oleg I. Bleyman , Wenling Kao , Magid A. Abou-Gharbia
- 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: A61K31/395
- IPC分类号: A61K31/395 ; A61K31/44 ; A61K31/675 ; C07D491/06 ; C07D498/04 ; C07D498/16
摘要:
A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONR.sup.3 (CR.sup.4 R.sup.5).sub.m (CR.sup.6 R.sup.7).sub.n (CR.sup.8 R.sup.9).sub.p NR.sup.10 R.sup.11, or ##STR2## or --CONR.sup.3 R.sup.13 ; R.sup.3 is hydrogen, alkyl, or arylalkyl;R.sup.4, R.sup.5, R.sup.8, and R.sup.9 are each, independently, hydrogen, alkyl, --OH, --CF.sub.3, or --F;R.sup.6 is hydrogen or --OR.sup.13 ;R.sup.7 is hydrogen or alkyl;R.sup.10 is hydrogen, alkyl, or arylalkyl;R.sup.11, R.sup.12 and R.sup.13 are each, independently, --(CR.sup.15 R.sup.16).sub.r R.sup.17 ;R.sup.14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl;R.sup.15 and R.sup.16 are each, independently, hydrogen or alkyl;R.sup.17 is ##STR3## or --C.tbd.C--R.sup.21 ; R.sup.18, R.sup.19, R.sup.20, and R.sup.21 are each, independently, hydrogen, alkyl, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted; ##STR4## is a 5-7 membered saturated or partially unsaturated heterocyclic radical containing at least 2 ring nitrogens, wherein the heterocyclic ting may optionally contain NR.sup.22 in the heterocyclic ring, and the ring carbons may optionally be substituted by alkyl, arylalkyl, halogen, --CF.sub.3, --OR.sup.14, or --CO.sub.2 R.sup.10 ;R.sup.22 is hydrogen, alkyl, or arylalkyl;m=0-6;n=1-6;p=0-6; andr=1-6with the proviso that R.sup.1 and R.sup.2 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
公开/授权文献
- US4445637A Air register with automatic zone control 公开/授权日:1984-05-01
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