Carbonyl derivatives as histamine h-2 receptor antagonists

Details Carbonyl derivatives as histamine h-2 receptor antagonists Carbonyl derivatives as histamine h-2 receptor antagonists

C - Chemistry, Metallurgy

07

D

260/259, 260/308

C07D 231/38 (2006.01) C07D 239/42 (2006.01) C07D 239/46 (2006.01) C07D 249/04 (2006.01) C07D 251/16 (2006.01) C07D 277/48 (2006.01)

Patent

CA 1209999

ABSTRACT The invention relates to carbonyl derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where is provided a guanidine derivative of the formula I:- Image I in which R1 and R2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkyl- alkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R1 and R2 is halogen substituted, or R2 is hydrogen and R1 is R5-E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO, SO2 or NR6 in which R6 is H or 1-6C alkyl, R5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R5 and R6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R2 is H and R1 is H, 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; ring X is a heterocyclic ring as defined in the speci- fication; 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; R4 is H or 1-6C alkyl; R3 is H 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.

397102

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