Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1987-06-24
1988-12-06
Brust, Joseph Paul
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514252, 514333, 514422, 514316, 5142322, 544 585, 544141, 544357, 544372, 546256, 546187, 548519, A61K 3140, C07D29518, C07D20726
Patent
active
047896744
ABSTRACT:
Novel Substituted tetrahydro-, hexahydro- and octahydro-[3,4'-bi-2H-pyrrolel]-2,2'-diones of the formula ##STR1## in which each of R.sub.1 and R.sub.2 represents a carboxy-lower alkyl radical, or an unsubstituted carbamoyl-lower alkyl radical or a carbamoyl-lower alkyl radical which is N-mono- or N,N-di-substituted by lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, amino-lower alkyl, N-mono- or N,N-di-lower alkylamino-lower alkyl, or by N,N-alkyleneamino-lower alkyl optionally substituted (in the alkyleneamino radical) by lower alkoxycarbonyl and by oxo or hydroxy, or N,N-alkenylene-amino-lower alkyl optionally substituted (in the alkenyleneamino radical) by lower alkoxycarbonyl and optionally additionally by hydroxy, or N,N-(aza-, N'-lower alkylaza- or N'-lower alkanoylaza-, oxa- or thia)alkyleneamino-lower alkyl, each of which has from 4 to 8 ring members, carbamoyl-lower alkyl, N-mono- or N,N-di-lower alkylcarbamoyl-lower alkyl, 3- to 8-membered cycloalkyl, dicycloalkyl or tricycloalkyl, or by phenyl-lower alkyl which is unsubstituted or substituted in the phenyl moiety by lower alkyl, lower alkoxy, halogen and/or trifluoromethyl, or represents a carbomoyl-lower alkyl radical which is disubstituted by alkylene optionally substituted by lower alkoxycarbonyl and by oxo or hydroxy, or by alkenylene optionally substituted by lower alkoxycarbonyl and optionally additionally by hydroxy, or by aza-, N'-lower alkylaza- or N'-lower alkanoylaza-, oxa- or thia-alkylene, each of which has from 3 to 7 chain members, each of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 represents hydrogen or lower alkyl, or R.sub.3 and R.sub.4 together and/or R.sub.5 and R.sub.6 together represent a 4- to 8-membered alkylene radical, and each of R.sub.7, R.sub.8, R.sub.9 and R.sub.10 represents hydrogen, or R.sub.7 together with R.sub.8 and/or R.sub.9 together with R.sub.10 represent in each case an additional bond, and their salts, have nootropic activity and can be used as active ingredients in medicaments. They are manufactured, for example, as follows: in a compound of the formula ##STR2## in which R'.sub.1 represents a group that can be converted into a radical R.sub.1 and R'.sub.2 represents a radical R.sub.2 or a group that can be converted into the radical R.sub.2, or in a salt thereof, R'.sub.1 is converted into a group R.sub.1 and, optionally, a radical R'.sub.2 that can be converted into R.sub.2 is converted into a group R.sub.2.
REFERENCES:
patent: 3459738 (1969-08-01), Morren et al.
patent: 4144246 (1949-06-01), L'Italien
Mulholland, et al., J. Chem. Soc., Perkin Trans., 1:2121-2128, (1972).
Lee, et al., J. Am. Chem. Soc., 100:4225-4236, (1978).
Pifferi et al., Il Farmaco, 32:602-613, (1977).
Brust Joseph Paul
Ciba-Geigy Corporation
Fishman Irving M.
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