YU30891A

YU30891A - DIAMINO DERIVATIVES, THEIR MIXTURES AND THE PROCESS FOR THEIR PRODUCTION

Info

Publication number: YU30891A
Application number: YU30891A
Authority: YU
Inventors: A. Ramu; K. Valter
Original assignee: F. Hoffmann-La Roche Ag.
Priority date: 1990-02-23
Filing date: 1991-02-21
Publication date: 1994-04-05
Also published as: TW197411B; KR910021239A

Abstract

DIAMINSKI DERIVATI, NJIHOVE SMESE I POSTUPAK ZA NJIHOVU PROIZVODNJU, jedinjenje formule gde R i R3, koji mogu da budu isti ili razliciti, predstavljaju atom vodonika, neku alkil grupu koja sadrzi 1 do 5 ugljenikovih atoma, ili neku po potrebi supstituisanu aril ili aralkil grupu, pri cemu su supstituenti odabrani od halogenih atoma, alkoksi i alkil grupu koje sadrze 1 do 5 ugljenikovih atoma, pri cemu su te grupe po potrebi sa svoje strane halo-supstituisane; R1 i R2, koji mogu da budu isti ili razliciti, predstavljaju atom vodonika, neku alkil grupu koja sadrzi 1 do 5 ugljenikovih atoma, ili po potrebi supstituisanu aril ili aralkil grupu, pri cemu su supstituenti vec navedeni, ili R1 i R2 zajedno predstavljaju alkilen grupu koja sadrzi 2 ili 3 ugljenikova atoma; m i p, koji mogu da budu isti ili razliciti, predstavljaju broj od O do 3; n predstavlja broj 2 ili 3; i X predstavlja grupu formule Rx4-CO-, Rx4-COO-, Rx4-CONH-, Rx4-NHCO-, ili Rx4-O- i Y predstavlja grupu formule Ry4-CO-, Ry4-COO-, Ry4-CONH-, Ry4-NHCO-, ili Ry4-O- u kojima grupe Ry4 i Rx4, koje mogu da budu iste ili razlicite, predstavljaju po potrebi supstituisanu aril, aralkil ili ariloksialkil grupu, ciji su supstituenti vec definisani, a alkil jezgro u aralkil i ariloksialkil grupama sadrze 1 do 5 ugljenikovih atoma i po potrebi su supstituisani cikloalkil grupom koja sadrzi 3 do 8 ugljenikovih atoma; i njihove fizioloski prihvatljive soli za adiranje kiselina, pronadjeno je da su aktivne kod uspostavljanja osetljivosti celija raka koje su postale otporne na mnoge lekove. Ona, prema tome mogu da se koriste kao pomocna sredstva u onkologiji i mogu da se daju simultano, odvojeno ili u intervalima u kombinaciji sa jednim ili vise konvencionalnih antikancerogenih agenasa za lecenje malignih tumova i odgovarajucih metastaza. Takodje su sadrzana i neka od ovih jedinjenja i soli koje prethodno nisu bila opisana, kao i njihova proizvodnja i farmaceutski sastavi koji ih sadrze.DIAMINE DERIVATIVES, THEIR MIXTURES AND THE PROCESS FOR THEIR PRODUCTION, a compound of the formula wherein R and R3, which may be the same or different, represent a hydrogen atom, an alkyl group containing 1 to 5 carbon atoms, or an optionally substituted aryl or aralkyl group. , wherein the substituents are selected from halogen atoms, alkoxy and alkyl groups containing 1 to 5 carbon atoms, these groups being optionally halo-substituted; R 1 and R 2, which may be the same or different, represent a hydrogen atom, an alkyl group containing 1 to 5 carbon atoms, or an optionally substituted aryl or aralkyl group, the substituents already mentioned, or R 1 and R 2 together represent alkylene a group containing 2 or 3 carbon atoms; m and p, which may be the same or different, represent a number from O to 3; n represents the number 2 or 3; and X represents a group of formula Rx4-CO-, Rx4-COO-, Rx4-CONH-, Rx4-NHCO-, or Rx4-O- and Y represents a group of formula Ry4-CO-, Ry4-COO-, Ry4-CONH-, Ry4-NHCO-, or Ry4-O- in which the groups Ry4 and Rx4, which may be the same or different, represent an optionally substituted aryl, aralkyl or aryloxyalkyl group, the substituents of which are already defined, and the alkyl nucleus in the aralkyl and aryloxyalkyl groups containing 1 to 5 carbon atoms and optionally substituted by a cycloalkyl group containing 3 to 8 carbon atoms; and their physiologically acceptable acid addition salts, have been found to be active in establishing the sensitivity of cancer cells that have become resistant to many drugs. They can therefore be used as adjuvants in oncology and may be administered simultaneously, separately or at intervals in combination with one or more conventional anticancer agents for the treatment of malignant tumors and corresponding metastases. Also contained are some of these compounds and salts not previously described, as well as their manufacture and pharmaceutical compositions containing them.