发明授权
- 专利标题: Methods and compounds
- 专利标题(中): 方法和化合物
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申请号: US654154申请日: 1991-02-12
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公开(公告)号: US5190946A公开(公告)日: 1993-03-02
- 发明人: Avner Ramu , Karel Valter
- 申请人: Avner Ramu , Karel Valter
- 申请人地址: NJ Nutley
- 专利权人: Hoffmann-La Roche Inc.
- 当前专利权人: Hoffmann-La Roche Inc.
- 当前专利权人地址: NJ Nutley
- 优先权: GBX9004099 19900223; GBX9004100 19900223; GBX9007144 19900330
- 主分类号: A61K31/13
- IPC分类号: A61K31/13 ; A61K31/135 ; A61K31/165 ; A61K31/22 ; A61K31/235 ; A61K31/475 ; A61K31/495 ; A61K31/675 ; A61P23/02 ; A61P25/02 ; A61P35/00 ; C07C217/06 ; C07C219/10 ; C07C219/14 ; C07C229/04 ; C07C229/34 ; C07C233/36 ; C07C233/78 ; C07C235/10 ; C07C235/50 ; C07C237/10 ; C07C237/20 ; C07C237/34 ; C07D295/088 ; C07D295/108 ; C07D295/13 ; C07D295/14 ; C07D295/15 ; C07D295/18 ; C07D295/185
摘要:
Compounds of formula ##STR1## wherein R and R.sup.3, which may be the same or different, each is hydrogen, an alkyl group containing 1 to 5 carbon atoms, or an optionally substituted aryl or aralkyl group, substituents being selected from the group consisting of halogen, alkoxy and alkyl groups containing 1 to 5 carbon atoms, said alkyl groups in turn being optionally halo-substituted; R.sup.1 and R.sup.2, which may be the same or different, each is hydrogen, an alkyl group containing 1 to 5 carbon atoms, or an optionally substituted aryl or aralkyl group, substituents being as indicated above or R.sup.1 and R.sup.2 taken together are an alkylene group containing 2 or 3 carbon atoms; m and p, which may be the same or different each is a number from 0 to 3; n is the number 2 or 3; and X is a group of the formula R.sub.x.sup.4 --CO--, R.sub.x.sup.4 --COO--, R.sub.x.sup.4 --CONH--, R.sub.x.sup.4 --NHCO--, or R.sub.x.sup.4 --O-- and Y is a group of formula R.sub.y.sup.4 --CO--, R.sub.y.sup.4 --COO--, R.sub.y.sup.4 --CONH--, R.sub.y.sup.4 --NHCO--, or R.sub.y.sup.4 --O-- which R.sub.y.sup.4 and R.sub.x.sup.4, which may be the same of different, each is an optionally substituted aryl, aralkyl or aryloxyalkyl group, substitutents being as indicated above, and the alkyl moiety in the aralkyl and aryloxyalkyl groups containing 1 to 5 carbon atoms and can be optionally substituted by a cyloalkyl group containing 3 to 8 carbon atoms; and physiologically acceptable acid addition salts thereof, have been found to be active in restoring drug-sensitivity to cancer cells that have become multidrug-resistant. They can, therefore, be used as adjuvants in oncology, and they can be administered simultaneously, separately or at intervals in combination with one or more conventional anti-cancer agents for treating malignant tumors and corresponding metastases.Compounds and salts which have not been previously described in British Patent Specification No. 883013 as well as their preparation and pharmaceutical compositions containing them are also disclosed.
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