.alpha.-oxopyrrolo[2,3-b]indole acetic acids, esters, amides...

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) A61K 31/40 (2006.01) A61K 31/44 (2006.01) A61K 31/495 (2006.01)

Patent

CA 2042737

ABSTRACT HOE 90/S 010 .alpha.-Oxopyrrolo[2,3-b]indole acetic acids, esters, amides and related analogs, a process for their preparation and their use as medicaments This invention relates to compounds of the formula Image where X is -NH, oxygen, N-loweralkyl, or N-arylloweralkyl; R1 is hydrogen, loweralkyl, cycloalkyl, aryl, arylloweralkyl, loweralkylene, haloloweralkyl, heteroaryl selected from the group consisting of thienyl, furanyl, pyrrolyl and pyridinyl; heteroarylloweralkyl, heterocyclic selected from piperidinyl, piperazinyl, pyrrolidinyl; or heterocyclicloweralkyl; R2 is hydrogen or loweralkyl; R3 is loweralkyl or arylloweralkyl; R4 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, arylloweralkyl, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl or loweralkoxycarbonyl; Y is hydrogen, halogen, loweralkyl or loweralkoxy, and the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention are useful for alleviating various memory dysfunctions characterized by a cholinergic defect such as Alzheimer's disease.

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