Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1991-04-23
1992-06-09
Chan, Nicky
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
549362, 549435, 549444, 549462, 549484, 549486, 560152, 560187, 560250, 560 25, 514466, 514469, 514471, 514550, 514546, A61K 31335, A61K 3136, C07D31918, C07D31448
Patent
active
051207591
ABSTRACT:
Novel compounds of the formula ##STR1## wherein R.sup.1 is lower-alkyl, lower-alkoxy-lower-alkyl, lower-alkylthio-lower-alkyl or furyl, R.sup.2 is lower-alkyl, phenyl-lower-alkyl or cyclohexyl-lower-alkyl, each of R.sup.3 and R.sup.6 independently is hydrogen or fluorine, each of R.sup.4 and R.sup.5 independently is hydrogen or lower-alkoxy or together are methylenedioxy, ethylenedioxy or ethylenoxy and n is an integer from 1 to 3, have a pronounced activity in counteracting cerebral insufficiency or improving cognitive functions and also reduce the multiple-resistance towards cytostatics in the treatment of tumors or of chloroquine resistance in the treatment of malaria. They can accordingly be used as medicaments, especially for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions. The novel compounds of formula I can be manufactured by O-acylating a likewise novel compound of the formula ##STR2## wherein R.sup.2 is lower-alkyl, phenyl-lower-alkyl or cyclohexyl-lower-alkyl, each of R.sup.3 and R.sup.6 independently is hydrogen or fluorine, each of R.sup.4 and R.sup.5 independently is hydrogen or lower-alkoxy or together are methylenedioxy, ethylendioxy or ethylenoxy and n is an integer from 1 to 3.
REFERENCES:
patent: 4680310 (1987-07-01), Hengartner et al.
patent: 4808605 (1989-02-01), Branca et al.
Chemical Abstracts, 111:442f (1989).
J. Cardio. Pharm. 13(5) 754 (1989).
Hengartner Urs
Ramuz Henri
Chan Nicky
Gould George M.
Hoffmann-La Roche Inc.
Isgro William G.
Krovatin William
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