Process for the manufacture of bi-2h-pyrroli(di)nediones

C - Chemistry – Metallurgy – 07 – D

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C07D 401/14 (2006.01) C07D 207/273 (2006.01) C07D 207/38 (2006.01) C07D 403/00 (2006.01) C07D 413/14 (2006.01)

Patent

CA 1331756

- 1 - Process for the Manufacture of Bi-2H-Pyrroli(di)nediones Abstract Novel substituted tetrahydro-, hexahydro- and octahydro- [3,4'-bi-2H-pyrrolo]-2,2'-diones of the formula Image (I) in which each of R1 and R2 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-C3-C7- alkyleneamino-lower alkyl which is unsubstituted or substi- tuted (in the alkyleneamino radical) by lower alkoxycarbonyl and by oxo or hydroxy, or N,N-C3-C7-alkenyleneamino-lower alkyl which is unsubstituted or substituted (in the alken- yleneamino radical) by lower alkoxycarbonyl or by lower alkoxycarbonyl and hydroxy, or N,N-(aza-, N'-lower alkylaza- or N'-lower alkanoylaza-, oxa- or thia)C3-C7-alkyleneamino- lower alkyl, 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 - 2 - which is unsubstituted or substituted in the phenyl moiety by one or more groups selected from lower alkyl, lower alkoxy, halogen and trifluoromethyl, or represents a car- bamoyl-lower alkyl radical which is disubstituted by C3-C7- alkylene which is unsubstituted or substituted by lower alkoxycarbonyl and by oxo or hydroxy, or by C3-C7-alkenylene which is unsubstituted or substituted by lower alkoxycar- bonyl or by lower alkoxycarbonyl and hydroxy, or by aza-, N'-lower alkylaza- or N'-lower alkanoylaza-, oxa- or thia- C3-C7-alkylene, each of R3, R4, R5 and R6 represents hydrogen or lower alkyl, or R3 and R4 together and R5 and R6 together represent a 4- to 8-membered alkylene radical, and each of R7, R8, R9 and R10 represents hydrogen, or R7 together with R8 and R9 together with R10 represent in each case an additional bond, and their salts. The compounds of the invention possess valuable nontropic properties and can be used for the treatment of cerebral insufficiency, especially memory disorders, such as senile dementia or dementia of the Alzheimer type.

502393

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