Heterocyclic derivatives as histamine h-2 receptor antagonists

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

C - Chemistry, Metallurgy

07

D

260/259, 260/300

C07D 239/28 (2006.01) C07D 213/73 (2006.01) C07D 213/75 (2006.01) C07D 231/16 (2006.01) C07D 231/40 (2006.01) C07D 239/42 (2006.01) C07D 239/46 (2006.01) C07D 239/545 (2006.01) C07D 249/04 (2006.01) C07D 249/08 (2006.01) C07D 249/14 (2006.01) C07D 257/06 (2006.01) C07D 403/02 (2006.01)

Patent

CA 1200549

ABSTRACT HETEROCYCLIC DERIVATIVES This invention relates to heterocyclic 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 in which R1 and R2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, 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 2-6 alkylene optionally substituted by 1or2 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; ring Xis 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; and R3 and R4 are a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.

398640

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