Thiazole compound and use thereof

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 277/24 (2006.01) A61K 31/426 (2006.01) A61K 31/427 (2006.01) A61K 31/4439 (2006.01) A61K 31/4709 (2006.01) A61K 31/496 (2006.01) A61K 31/497 (2006.01) A61K 31/498 (2006.01) A61K 31/506 (2006.01) A61K 31/5377 (2006.01) A61P 17/00 (2006.01) A61P 43/00 (2006.01) C07D 277/20 (2006.01) C07D 277/30 (2006.01) C07D 417/06 (2006.01) C07D 495/04 (2006.01)

Patent

CA 2566625

A novel thiazole compound represented by the general formula (1), an optical isomer thereof, or a salt of either. They have specific inhibitory activity against phosphodiesterase 4. [Chemical formula 1] (1) In the formula, R1 represents di(C1-6 alkoxy)phenyl; R2 represents any of the following groups (a) to (t): (a) phenyl, (b) naphthyl, (c) pyridyl, (d) furyl, (e) thienyl, (f) isoxazolyl, (g) thizolyl, (h) pyrrolyl, (i) imidazolyl, (j) tetrazolyl, (k) pyrazinyl, (l) thienothienyl, (m) benzothienyl, (n) indolyl, (o) benzimidazolyl, (p) indazolyl, (q) quinolyl, (r) 1,2,3,4-tetrahydroquinolyl, (s) quinoxanyl, and (t) 1,3-benzodioxolyl; and A represents any of the following groups (i) to (vi): (i) -CO-B (B represents C1-6 alkylene), (ii) -CO- Ba- (Ba represents C2-6 alkenylene), (iii) -CH(OH)-B-, (iv) -COCH(COOR3)-Bb- (R3 represents C1-6 alkyl and Bb represents C1-6 alkylene), and (v) -Bc- (Bc represents C2-6 alkylene).

Nouveau composé thiazole représenté par la formule générale (1), isomère optique de celui-ci ou sel de l'un ou l'autre. Ils ont une activité d'inhibition spécifique vis-à-vis de la phosphodiestérase 4. [Formule chimique 1] (1) Dans la formule, R1 représente un di(alcoxy en C¿1-6?)phényle ; R2 représente l'un quelconque des groupes (a) à (t) suivants : (a) phényle, (b) naphtyle, (c) pyridyle, (d) furyle, (e) thiényle, (f) isoxazolyle, (g) thizolyle, (h) pyrrolyle, (i) imidazolyle, (j) tétrazolyle, (k) pyrazinyle, (l) thiénothiényle, (m) benzothiényle, (n) indolyle, (o) benzimidazolyle, (p) indazolyle, (q) quinolyle, (r) 1,2,3,4-tétrahydroquinolyle, (s) quinoxanyle et (t) 1,3-benzodioxolyle ; et A représente l'un quelconque des groupes (i) à (vi) suivants : (i) -CO-B (B représente un alkylène en C¿1-6?), (ii) -CO-Ba- (Ba représente un alcénylène en C¿2-6?), (iii) -CH(OH)-B-, (iv) -COCH(COOR3)-Bb- (R3 représente un alkyle en C¿1-6? et Bb représente un alkylène en C¿1-6?) et (v) -Bc- (Bc représente un alkylène en C¿2-6?).

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