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US4104382A
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Pharmaceutical compositions and methods of inhibiting H-1 and H-2 histamine receptors
Assignee: Smith Kline & French Laboratories Ltd
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Filing: 1976-09-27
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Granted: 1978-08-01
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Expires: 1996-09-27
Abstract
Abstract Pharmaceutical compositions and methods of inhibiting H-1 and H-2 histamine receptors by administering an antihistamine and an H-2 histamine receptor inhibitor. Exemplary of the antihistamine in the compositions and methods of this invention is mepyramine and exemplary of the H-2 histamine receptor inhibitor is N-cyano-N'-methyl-N''-[2-((4-methyl-5-imidazolyl)-methylthio)ethyl]gua nidine.
Inventors
- 👤 James Whyte Black
- 👤 Michael Edward Parsons
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 23:48
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/24; C07D213/36; C07D213/40; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/40; A61K31/41; A61K31/415; A61K31/42; A61K31/425; A61K31/435; A61K31/44; A61K31/445; A61K31/495; A61K31/50; A61K31/54; C07D249/00; C07D249/02; C07D249/08; C07D275/00; C07D275/02
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
158 words
A pharmaceutical composition having H-1 and H-2 histamine receptor inhibiting activity which comprises about 30 mg. to about 250 mg. of an antihistamine, said antihistamine being a compound which inhibits those histamine receptors inhibited by mepyramine, about 50 mg. to about 500 mg. of an H-2 histamine receptor inhibitor, H-2 histamine receptors being those histamine receptors which are not inhibited by mepyramine but are inhibited by burimamide, and a pharmaceutically acceptable diluent or carrier, wherein said H-2 histamine receptor inhibitor is a compound of the formula: ##STR15## wherein A is such that there is formed together with the carbon atom shown a thiazole, isothiazole or pyridine ring; X 1 is hydrogen, lower alkyl, halogen, amino or hydroxyl; X 2 is hydrogen; k is 1; m is 2; Y is sulphur; E is NR 2 ; R 1 is hydrogen or lower alkyl; and R 2 is hydrogen, nitro or cyano, or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
158 words
A pharmaceutical composition having H-1 and H-2 histamine receptor inhibiting activity which comprises about 30 mg. to about 250 mg. of an antihistamine, said antihistamine being a compound which inhibits those histamine receptors inhibited by mepyramine, about 50 mg. to about 500 mg. of an H-2 histamine receptor inhibitor, H-2 histamine receptors being those histamine receptors which are not inhibited by mepyramine but are inhibited by burimamide, and a pharmaceutically acceptable diluent or carrier, wherein said H-2 histamine receptor inhibitor is a compound of the formula: ##STR15## wherein A is such that there is formed together with the carbon atom shown a thiazole, isothiazole or pyridine ring; X 1 is hydrogen, lower alkyl, halogen, amino or hydroxyl; X 2 is hydrogen; k is 1; m is 2; Y is sulphur; E is NR 2 ; R 1 is hydrogen or lower alkyl; and R 2 is hydrogen, nitro or cyano, or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
43 words
A pharmaceutical composition according to claim 1 wherein the antihistamine is a compound selected from the group consisting of mepyramine, mebrophenhydramine, promethazine, diphenhydramine, chlorpheniramine, triprolidene, antazoline, bromodiphenydramine, parabromodylamine, carbinoxamine, cyproheptadine, chlorcyclizine, dimethindene, diphenylpyraline, dimethothiazine, methdilazine, trimeprazine, mebhydroline, methapyrilene, phenindamine, pheniramine, phenyltoloxamine and pyrrobutamine.
Claim 4
Independent Claim
167 words
A method of inhibiting H-1 and H-2 histamine receptors which comprises administering to an animal in need thereof, in amounts sufficient to inhibit both H-1 and H-2 histamine receptors, an antihistamine, said antihistamine being a compound which inhibits those histamine receptors inhibited by mepyramine, and an H-2 histamine receptor inhibitor, said H-1 histamine receptors being those histamine receptors which are inhibited by mepyramine and said H-2 histamine receptors being those histamine receptors which are not inhibited by mepyramine but are inhibited by burimamide, wherein said H-2 histamine receptor inhibitor is a compound of the formula: ##STR16## wherein A is such that there is formed together with the carbon atom shown a thiazole, isothiazole or pyridine ring; X 1 is hydrogen, lower alkyl, halogen, amino or hydroxyl; X 2 is hydrogen, k is 1; m is 2; Y is sulphur; E is NR 2 ; R 1 is hydrogen or lower alkyl; and R 2 is hydrogen, nitro or cyano, or a pharmaceutically acceptable acid addition salt thereof.
Claim 5
Independent Claim
167 words
A method of inhibiting H-1 and H-2 histamine receptors which comprises administering to an animal in need thereof, in amounts sufficient to inhibit both H-1 and H-2 histamine receptors, an antihistamine, said antihistamine being a compound which inhibits those histamine receptors inhibited by mepyramine, and an H-2 histamine receptor inhibitor, said H-1 histamine receptors being those histamine receptors which are inhibited by mepyramine and said H-2 histamine receptors being those histamine receptors which are not inhibited by mepyramine but are inhibited by burimamide, wherein said H-2 histamine receptor inhibitor is a compound of the formula: ##STR16## wherein A is such that there is formed together with the carbon atom shown a thiazole, isothiazole or pyridine ring; X 1 is hydrogen, lower alkyl, halogen, amino or hydroxyl; X 2 is hydrogen, k is 1; m is 2; Y is sulphur; E is NR 2 ; R 1 is hydrogen or lower alkyl; and R 2 is hydrogen, nitro or cyano, or a pharmaceutically acceptable acid addition salt thereof.
Claim 6
Dependent Claim
41 words
A method of claim 3 wherein the antihistamine is a compound selected from the group consisting of mepyramine, mebrophenhydramine, promethazine, diphenhydramine, chlorpheniramine, triprolidene, antazoline, bromodiphenydramine, parabromdylamine, carbinoxamine, cyproheptadine, chlorcyclizine, dimethindene, diphenylpyraline, dimethothiazine, methdilazine, trimeprazine, mebhydroline, methapyrilene, phenindamine, pheniramine, phenyltoloxamine and pyrrobutamine.
Claim 7
Independent Claim
146 words
A method of producing anti-inflammatory activity which comprises administering to an animal in need thereof, in amounts sufficient to produce said activity, an antihistamine, said antihistamine being a compound which inhibits those histamine receptors inhibited by mepyramine, and an H-2 histamine receptor inhibitor, said H-2 histamine receptors being those histamine receptors which are not inhibited by mepyramine but are inhibited by burimamide, wherein said H-2 histamine receptor inhibitor is a compound of the formula: ##STR17## wherein A is such that there is formed together with the carbon atom shown a thiazole, isothiazole or pyridine ring; X 1 is hydrogen, lower alkyl, halogen, amino or hydroxyl; X 2 is hydrogen; k is 1; m is 2; Y is sulphur; E is NR 2 ; R 1 is hydrogen or lower alkyl; and R 2 is hydrogen, nitro or cyano, or a pharmaceutically acceptable acid addition salt thereof.
Claim 8
Independent Claim
146 words
A method of producing anti-inflammatory activity which comprises administering to an animal in need thereof, in amounts sufficient to produce said activity, an antihistamine, said antihistamine being a compound which inhibits those histamine receptors inhibited by mepyramine, and an H-2 histamine receptor inhibitor, said H-2 histamine receptors being those histamine receptors which are not inhibited by mepyramine but are inhibited by burimamide, wherein said H-2 histamine receptor inhibitor is a compound of the formula: ##STR17## wherein A is such that there is formed together with the carbon atom shown a thiazole, isothiazole or pyridine ring; X 1 is hydrogen, lower alkyl, halogen, amino or hydroxyl; X 2 is hydrogen; k is 1; m is 2; Y is sulphur; E is NR 2 ; R 1 is hydrogen or lower alkyl; and R 2 is hydrogen, nitro or cyano, or a pharmaceutically acceptable acid addition salt thereof.
Claim 9
Dependent Claim
42 words
A method of claim 5 in which the antihistamine is a compound selected from the group consisting of mepyramine, mebrophenhydramine, promethazine, diphenhydramine, chlorpheniramine, triprolidene, antazoline, bromodiphenhydramine, parabromdylamine, carbinoxamine, cyproheptadine, chlorcyclizine, dimethindene, diphenylpyraline, dimethothiazine, methdilazine, trimeprazine, mebhydroline, methapyrilene, phenindamine, pheniramine, phenyltoloxamine and pyrrobutamine.
References Cited (Backward Citations)
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