2-aminothiazoline derivatives and their use as no-synthase...

C - Chemistry – Metallurgy – 07 – D

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C07D 277/18 (2006.01) A61K 31/426 (2006.01) A61K 31/427 (2006.01) A61K 31/4439 (2006.01) A61K 31/497 (2006.01) A61P 25/00 (2006.01) C07C 215/00 (2006.01) C07C 229/00 (2006.01) C07C 233/00 (2006.01) C07C 271/00 (2006.01) C07C 333/00 (2006.01) C07C 335/06 (2006.01) C07D 213/38 (2006.01) C07D 213/40 (2006.01) C07D 213/70 (2006.01) C07D 213/89 (2006.01) C07D 241/12 (2006.01) C07D 277/28 (2006.01) C07D 333/20 (2006.01) C07D 417/06 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2411760

The invention concerns 2-aminithiazoline derivatives of formula (I) wherein: either R¿1? is a hydrogen atom or an alkyl radical and R¿2? is an alkyl, -alk-NH¿2?, -CH-R¿3?, -CH¿2?-S-R¿4? or phenyl radical substituted by a nitro or NH-C(=NH)CH¿3? radical; or R¿1? is an alkyl radical and R¿2? is a hydrogen atom; R¿3? is a cycloalkyl (3-6C), pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl, phenyl or phenyl radical substituted by a nitro, hydroxy or carboxy radical; R¿4? represents a pyridyl or pyridyl N-oxide radical; alk represents an alkylene radical or their pharmaceutically acceptable salts excluding some known compounds, and the use of said derivatives as inducible NO-synthase inhibitors.

La présente invention concerne les dérivés de 2-aminothiazoline de formule (I) dans laquelle soit R1 est un atome d'hydrogène ou un radical alkyle et R2 est un radical alkyle, -alk-NH2, -CH2-R3, -CH2-S-R4 ou phényle substitué par un radical nitro ou -NH-C(=NH)CH3, soit R1 est un radical alkyle et R2 est un atome d'hydrogène, R3 est un radical cycloalkyle (3-6C), pyridyle, N-oxyde de pyridyle, thiényle, thiazolyle, imidazolyle, pyrazinyle, triazolyle, phényle ou phényle substitué par un radical nitro, hydroxy ou carboxy, R4 représente un radical pyridyle ou N-oxyde de pyridyle, alk représente un radical alkylène ou leurs sels pharmaceutiquement acceptables, à l'exclusion de certains composés connus, ainsi que l'utilisation de ces dérivés comme inhibiteurs de NO-synthase inductible.

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