C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/314, 260/314
C07D 233/06 (2006.01) C07D 233/08 (2006.01) C07D 233/54 (2006.01) C07D 233/56 (2006.01)
Patent
CA 1183544
ABSTRACT OF THE DISCLOSURE Novel 2-substituted imidazole and imidazoline derivatives and their non-toxic pharmaceutically acceptable acid addition salts and the preparation thereof are provided herein. The novel compounds have the formula or Image (I) Image (II) wherein each of R1, R2 and R3, which can be the same or different, is hydrogen, chloro, bromo, fluoro, methyl, ethyl, methoxy, amino, hydroxy or nitro; R4 and R5, which can be the same or different, are hydrogen, an alkyl radical of 1 to 7 carbon atoms, hydroxymethyl or Image R6 is hydrogen, an alkyl radical of 1 to 7 carbon atoms or Abstract-2 Image R7 and R8 are hydrogen, chloro or methyl; X is -CH=CH- or -CH2-; n is 0-7 and m is 0-6; and their non-toxic pharmaceutically acceptable acid addition salts and mixtures thereof. The compounds of formulae I and II are novel provided that, in general formula I a) when n = 0 and R1 and R2 are both hydrogen then R3 is not hydrogen, methoxy or 4-chloro, b) when n = 0, X = -CH=CH-, and R1 and R2 are hydrogen, R3 is not nitro, amino, or hydroxy, c) when n is 1 and R1, R2, R3 and R5 are all hydrogen, then if X is CH2 and R6 is hydrogen, R4 is other than hydroxymethyl, d) when n is 2 and X is CH2 then R1, R2, R3, R4, R5 and R6 are not all hydrogen, and e) in general formula (II), when m is 0 or 1, R1, R2 and R3 are not all hydrogen. The compounds 2-(2-phenylethyl)-4-hydroxymethyl- imidazole, 2-(3-phenylpropyl)-imidazole, and 2-(2-phenyl-1-hydroxyethyl)- 1-methyl-imidazole are excluded. The compounds and their non-toxic salts exhibit valuable pharmacological activity and are useful in the treatment of mammals, especially as antihypertensives and also as antithrombotic and antimycotic agents. The most effective compounds of the invention are 2-[2-(2,6-dimethylphenyl)-ethyl]-imidazole and 2-[2-(2,6-dimethyl- phenyl)ethyl]-4-methyl-imidazole.
400252
Karjalainen Arto J.
Kurkela Kauko O. A.
Borden Ladner Gervais Llp
Farmos - Yhtyma Oy
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