Bicyclic cinnamide compound

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 471/04 (2006.01) A61K 31/4178 (2006.01) A61K 31/437 (2006.01) A61K 31/4375 (2006.01) A61K 31/55 (2006.01) A61P 25/28 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2629512

A bicyclic cinnamide compound represented by the formula (I) [wherein (II) indicates a single bond or double bond; Ar1 represents phenyl or pyridinyl optionally substituted by one to three substituents; R1 and R2 each represents C1-6 alkyl, hydroxy, etc.; Z1 represents optionally substituted methylene or vinylene, oxygen, or imino optionally substituted by C1-6 alkyl or C1-6 acyl; and p, q, and r each is an integer of 0-2]. It functions to reduce the production of A.beta.40 and A.beta.42. It is hence useful especially as a preventive or remedy for neurodegenerative diseases of which A.beta. is causative, such as Alzheimer's disease and Down's syndrome.

L'invention concerne un composé cinnamide bicyclique représenté par la formule (I) : (I) [dans laquelle (II) représente une liaison simple ou double ; Ar1 représente un phényle ou un pyridinyle éventuellement substitué par un à trois susbtituants ; R1 et R2 représentent chacun C1-6 alkyle, hydroxy, etc. ; Z1 représente un méthylène ou un vinylène éventuellement substitué, oxygène ou imino éventuellement substitué par C1-6 alkyle ou C1-6 acyle ; et p, q et r sont chacun un entier compris entre 0 et 2.] Ce composé agit en réduisant la production de A.beta.40 et de A.beta.42. Il convient donc tout particulièrement par son action préventive ou curative pour des maladies neurodégénératives, telles que la maladie d'Alzheimer ou le syndrome de Down, dont l'agent responsable est A.beta..

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