Carboxylic acid derivatives

C - Chemistry – Metallurgy – 07 – F

Patent

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C07F 9/94 (2006.01) A61K 31/34 (2006.01) A61K 31/41 (2006.01) C07D 307/38 (2006.01) C07D 307/52 (2006.01) C07D 405/12 (2006.01)

Patent

CA 2041175

A B S T R A C T CARBOXYLIC ACID DERIVATIVES The invention relates to a salt of a basic histamine H2-receptor antagonist of formula (I) Image (I) and a complex of bismuth with a carboxylic acid selected from tartaric acid, citric acid and alkyl citric acids, or a solvate of such a salt, wherein R1 represents a group of formula or Image Image where R3 represents methyl or the group (CH2)2CONR4R5 in which R4 and R5 both represent ethyl groups; R2 represents a hydrogen atom or, when R1 is the group -C(=CHNO2)NHCH3, R2 may also represent a methyl group; and n is 3 and X is oxygen, or n is 2 and X is CH2 or sulphur; with the provisos that (i) when R1 represents 6877/ABS Image or Image then X is sulphur and n is 2; (ii) when R1 represents -C(=CHNO2)NHCH3 and R2 is hydrogen, then X is oxygen and n is 3 or X is CH2 and n is 2; and (iii) when R1 represents -C(=CHNO2)NHCH3 and R2 is methyl, then X is oxygen and n is 3 or X is sulphur and n is 2. The salts and solvates thereof are useful in the treatment of gastro-intestinal disorders, such as peptic ulcer disease, gastritis and non-ulcer dyspepsia. 6877/ABS

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