Derrick L Jones

US Patent:

41653777, Aug 21, 1979

Filed:

Apr 19, 1978

Appl. No.:

5/897910

Inventors:

Derrick F. Jones - Wilmington DE
Tobias O. Yellin - Wallingford PA

Assignee:

ICI Americas Inc. - Wilmington DE

International Classification:

C07D27738
C07D23388
A61K 31425
A61K 31415

US Classification:

424270

Abstract:

The invention relates to guanidine derivatives of imidazoles and thiazoles which are histamine H-2 antagonists and which inhibit the secretion of gastric acid, to methods for their manufacture, to pharmaceutical compositions containing them and to methods of using such guanidine derivatives and compositions. The guanidine derivatives are of the general formula I: ##STR1## in which X is S or NH, Y is CH. sub. 2, a direct bond or a vinylene radical, m is 0 to 4 and n is 1 to 4, R. sup. 1 is hydrogen, halogen or alkyl, R. sup. 2 is hydrogen, alkyl, alkanoyl or aroyl, A is a 3,4-dioxocyclobuten-1,2-diyl radical or C. dbd. Z in which Z is O, S, NCN, NNO. sub. 2, CHNO. sub. 2, NCONH. sub. 2, C(CN). sub. 2, NCOR. sup. 3, NCO. sub. 2 R. sup. 3, NSO. sub. 2 R. sup. 3 or NR. sup. 4 in which R. sup. 3 is alkyl or aryl and R. sup.

US Patent:

42347351, Nov 18, 1980

Filed:

Aug 13, 1979

Appl. No.:

6/065801

Inventors:

Derrick F. Jones - Wilmington DE
Tobias O. Yellin - Wallingford PA

Assignee:

Imperial Chemical Industries Limited - London
ICI Americas Inc. - Wilmington DE

International Classification:

C07D27738
C07D23388
A61K 31425
A61K 31415

US Classification:

548198

Abstract:

The invention relates to guanidine derivatives of imidazoles and thiazoles which are histamine H-2 antagonists and which inhibit the secretion of gastric acid, to methods for their manufacture, to pharmaceutical compositions containing them and to methods of using such guanidine derivatives and compositions. The guanidine derivatives are of the general formula I: ##STR1## in which X is S or NH, Y is CH. sub. 2, a direct bond or a vinylene radical, m is 0 to 4 and n is 1 to 4, R. sup. 1 is hydrogen, halogen or alkyl, R. sup. 2 is hydrogen, alkyl, alkanoyl or aroyl, A is a 3,4-dioxocyclobuten-1,2-diyl radical or C. dbd. Z in which Z is O, S, NCN, NNO. sub. 2, CHNO. sub. 2, NCONH. sub. 2, C(CN). sub. 2, NCOR. sup. 3, NCO. sub. 2 R. sup. 3, NSO. sub. 2 R. sup. 3 or NR. sup. 4 in which R. sup. 3 is alkyl or aryl and R. sup.