Amide derivatives as histamine h-2 receptor antagonists

C - Chemistry – Metallurgy – 07 – D

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C07D 231/38 (2006.01) C07D 213/76 (2006.01) C07D 239/42 (2006.01) C07D 239/46 (2006.01) C07D 241/40 (2006.01) C07D 249/04 (2006.01) C07D 277/48 (2006.01)

Patent

CA 1209998

-47- ABSTRACT AMIDE DERIVATIVES The invention relates to amide derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I:- Image I in which R1 is a hydrogen or 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C aralkyl or 7-11C aroyl, the aryl, aralkyl and aroyl radical being optionally substituted; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene, or a 1-8C alkylene into which is optionally inserted one or two groups; D is O or S; and R2 and R3 are hydrogen or a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.

397033

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