A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/495 (2006.01) A61K 31/13 (2006.01) A61K 31/135 (2006.01) A61K 31/215 (2006.01) A61K 31/22 (2006.01) A61K 31/475 (2006.01) A61K 31/675 (2006.01) C07C 219/10 (2006.01) C07D 295/088 (2006.01) C07D 295/108 (2006.01) C07D 295/13 (2006.01) C07D 295/15 (2006.01) C07D 295/185 (2006.01)
Patent
CA 2036912
RAN 4060/156k Abstract Compounds of formula Image wherein R and R3, which may be the same or different, each represents a hydrogen atom, an alkyl group containing 1 to 5 carbon atoms, or an optionally substituted aryl or aralkyl group, substituents being selected from halogen atoms, alkoxy and alkyl groups containing 1 to 5 carbon atoms, said alkyl groups in turn being optionally halo-substituted; R1 and R2, which may be the same or different, each represents a hydrogen atom, an alkyl group containing 1 to 5 carbon atoms, or an optionally substituted aryl or aralkyl group, substi-tuents being as indicated above, or R1 and R2 together represent an alkylene group containing 2 or 3 carbon atoms; m and p, which may be the same or different each represents a number from 0 to 3; n represents the number 2 or 3; and X represents a group of formula R?-CO-, R?-CONH-, R?-NHCO-, or R?-O- and Y represents a group of formula R?,-CO-, R?-COO-,R?-CONH-, R?-NHCO or R?-O- in which groups R?, and R?, which may be the same or different, each represents an optionally substituted aryl, aralkyl or aryloxyalkyl group, substituents being as indicated above, and the alkyl moiety in the aralkyl and aryloxyalkyl groups containing 1 to 5 carbon atoms and being optionally substituted by a cycloalkyl group containing 3 to 8 carbon atoms; andphysiologically 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 tumours and corresponding metastases. Some of these compounds and salts which have not been previously described as well as their manufacture and pharmaceutical compositions containing them are also disclosed.
Ramu Avner
Valter Karel
F. Hoffmann-La Roche Ag
Gowling Lafleur Henderson Llp
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