Amine compounds, their production and use

Details Amine compounds, their production and use Amine compounds, their production and use

C - Chemistry, Metallurgy

07

C

C07C 217/74 (2006.01) A61K 31/135 (2006.01) A61K 31/36 (2006.01) A61P 25/28 (2006.01) C07D 317/54 (2006.01)

Patent

CA 2276278

A compound of formula (I) wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) -S-, -SO- or -SO2-, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc., (iv) -CO-O-- or (v) -(CH2)p-x1-, -(CH2)p-X1-(CH2)q-, -(CH2)r-CO-X1-, -SO2-NR8- or - (CH2)r-SO2-NR8- wherein X1 is O or NR8, R8 is H, a hydrocarbon group which may be substituted or an acyl, p is 0 to 5, q is 1 to 5, p+q is 1 to 5, and r is 1 to 4; Y is a divalent C1-6 aliphatic hydrocarbon group optionally containing O or S, which may be substituted; R1 and R2 each is H or a lower alkyl which may be substituted, or R1 and R2 form an N-containing heterocyclic ring which may be substituted; Ring A is a benzene ring which may be further substituted; and Ring B is a 4- to 8-membered ring which may be further substituted, or a salt thereof has the effect of inhibiting amyloid-.beta. protein production and/or secretion and is useful as a pharmaceutical composition for preventing and/or treating the neurodegenerative disease, etc.

L'invention porte sur des composés de formule (I) dans laquelle: Ar est un groupe aromatique cyclique, facultativement substitué ou un groupe aromatique fondu facultativement substitué, X est: (i) une liaison, (ii) -S-, -SO-, ou -SO2-, (iii) C1-6 alkylène, C2-6 alcénylène, ou C2-6 alkynylène, etc., (iv) -CO-O, ou (v) -(CH2)p-X<1>-, -(CH2)p-X<1>-(CH2)q-, -(CH2)r-CO-X<1>-, -SO2-NR<8>-, ou -(CH2)r-SO2-NR<8>-, ou X<1> est O ou NR<8>, R<8> est H, un groupe hydrocarbure facultativement substitué ou acyle, p est 0 à 5, q est 1 à 5, p + q est 1 à 5, et r est 1 à 4; Y est un groupe hydrocarbure aliphatique C1-6 divalent facultativement substitué contenant O ou S; R<1> et R<2> sont chacun H ou alkyle inférieur facultativement substitué, ou R<1> et R<2> forment ensemble un cycle hétérocyclique contenant N facultativement substitué; le cycle A est un cycle benzénique pouvant être substitué ultérieurement, le cycle B est un cycle à 4- à 8- éléments. Ledit composé ou l'un de ses sels ont pour effet d'inhiber la production et/ou la sécrétion de la protéine amyloïde beta et servent, sous forme de composition pharmaceutique, à la prévention et au traitement des troubles neurodégénératifs.

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