Heterocyclic guanidine derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 233/54 (2006.01) C07C 281/18 (2006.01) C07C 337/08 (2006.01) C07D 213/65 (2006.01) C07D 231/12 (2006.01) C07D 231/18 (2006.01) C07D 233/08 (2006.01) C07D 241/12 (2006.01) C07D 249/08 (2006.01) C07D 261/08 (2006.01) C07D 263/32 (2006.01) C07D 275/02 (2006.01) C07D 277/26 (2006.01) C07D 285/135 (2006.01)

Patent

CA 1053242

ABSTRACT OF THE DISCLOSURE Pharmacologically active guanidines are disclosed having the structural formula Image wherein R1 is hydrogen or lower alkyl; R2 is a grouping of the formula Het - (CH2)mZ (CH2)n - wherein Het is an imidazole ring which is optionally substituted by lower alkyl, trifluoromethyl, hydroxy, halogen or amino; Z is sulphur, oxygen, NH or a methylene group: m and n are integers from 0 to 4 such that their sum is from 2 to 4; X is COR3, CSR3, SO2R4, N=CHR5 or when Z is methylene, nitro; R3 is lower alkyl, lower alkoxy, or amino; R4 is lower alkyl, phenyl substituted by lower alkyl, halogen or amino, phenyl, trifluoromethyl or amino; and R5 is phenyl. These compounds have utility in inhibiting certain actions of histamine which are not inhibited by other antihistamines such as mepyramine as well as being useful as inhibitors of certain actions of gastrin.

177944

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