US3894151A
Expired / Lapsed
US
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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: 1973-04-09
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Granted: 1975-07-08
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Expires: 1993-04-09
Abstract
Abstract Pharmaceutical compositions and methods of inhibiting H-1 and H2 histamine receptors by administering an antihistamine and an H2 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-methyl-N''(4-(5)-imidazolyl)butyl)thiourea.
Inventors
- 👤 James Whyte Black
- 👤 Michael Edward Parsons
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 11:37
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; A61K31/505; A61K31/54; C07D233/00; C07D233/54; C07D233/64; C07D249/00; C07D249/02; C07D249/08; C07D275/00; C07D275/02
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
98 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 ANTHIHISTAMINE, 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 BUTIMAMIDE, AND A PHARMACEUTICALLY ACCEPABLE DILUENT OR CARRIER, WHEREIN SAID H-2 HISTAMINE RECEPTOR INHIBITOR IS A COMPOUND SELECTED ROM THE GROUP CONSISTING OF N-METHYL-N''-(4-(4(5)-IMIDAZOLYL)BUTYL) THIOUREA, N-(4-(4(5)-IMIDAZOLYL)BUTYL)THIOUREA, N-METHYL-N''(4-(4-BROMO-5-IMIDAZOLYL)BUTYL)THIOUREA, N-METHYL-N''-(2((4-METHYL-5-IMIDAZOLYL)METHYLTHIO)ETHYL)THIOUREA AND NMETHYL-N''-(2-((4-IMIDAZOLYL) METHYLTHIO) ETHYL)THIOUREA.
Claim 2
Dependent Claim
98 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 ANTHIHISTAMINE, 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 BUTIMAMIDE, AND A PHARMACEUTICALLY ACCEPABLE DILUENT OR CARRIER, WHEREIN SAID H-2 HISTAMINE RECEPTOR INHIBITOR IS A COMPOUND SELECTED ROM THE GROUP CONSISTING OF N-METHYL-N''-(4-(4(5)-IMIDAZOLYL)BUTYL) THIOUREA, N-(4-(4(5)-IMIDAZOLYL)BUTYL)THIOUREA, N-METHYL-N''(4-(4-BROMO-5-IMIDAZOLYL)BUTYL)THIOUREA, N-METHYL-N''-(2((4-METHYL-5-IMIDAZOLYL)METHYLTHIO)ETHYL)THIOUREA AND NMETHYL-N''-(2-((4-IMIDAZOLYL) METHYLTHIO) ETHYL)THIOUREA.
Claim 3
Dependent Claim
44 words
A pharmaceutical composition according to claim 1 in which 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, phenytoloxamine and pyrrobutamine.
Claim 4
Dependent Claim
17 words
A pharmaceutical composition according to claim 1 in which the H-2 histamine receptor inhibitor is N-methyl-N''-(4(4(5) -imidazolyl)butyl)thiourea.
Claim 5
Dependent Claim
16 words
A pharmaceutical composition according to claim 1 in which the H-2 histamine receptor inhibitor is N-methyl-N''-(2-((4-methyl-5-imidazolyl)methylthio)ethyl)thiourea.
Claim 6
Dependent Claim
20 words
A pharmaceutical composition according to claim 2 wherein the antihistamine is mepyramine and the H-2 histamine receptor inhibitor is N-methyl-N''-(4-(4(5)-imidazolyl)butyll-thiourea.
Claim 7
Dependent Claim
20 words
A pharmaceutical composition according to claim 2 wherein the antihistamine is mepyramine and the H-2 histamine receptor inhibitor is N-methyl-N''-(2-((4-methyl-5-imidazolyl)methylthio)ethyl)thiourea.
Claim 8
Dependent Claim
20 words
A pharmaceutical composition according to claim 2 wherein the antihistamine is promethazine and the H-2 histamine receptor inhibitor is N-methyl-N''(2-((4-methyl-5-imidazolyl)methylthio)ethyl)thiourea.
Claim 9
Dependent Claim
95 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-2histamine receptor inhibitor, said H-2histamine receptor inhibitor being selected from those set out in claim 1, 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.
Claim 10
Dependent Claim
42 words
A method of claim 8 in which 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 11
Dependent Claim
15 words
A method of claim 8 in which the H-2 histamine receptor inhibitor is N-methyl-N''-(4-(4(5) -imidazolyl)butyl)thiourea.
Claim 12
Dependent Claim
15 words
A method of claim 8 in which the H-2 histamine receptor inhibitor is N-methyl-N''-(2-((4-methyl-5-imidazolylmethylthio)ethyl)thiourea. -imidazolyl)methylthio)ethyl)
Claim 13
Dependent Claim
19 words
A method of claim 9 in which the antihistamine is mepyramine and the H-2 histamine receptor inhibitor is N-methyl-N''-(4-(4(5)-imidazolyl)butyl)thiourea.
Claim 14
Dependent Claim
19 words
A method of claim 9 in which the antihistamine is mepyramine and the H-2 histamine receptor inhibitor is N-methyl-N''-(2-((4-methyl-5-imidazolyl)methylthio)ethyl)thiourea.
Claim 15
Dependent Claim
70 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 selected from those set out in claim 1 said H-2 histamine receptors being those histamine recetors which are not inhibited by mepyramine but are inhibited by burimamide.
Claim 16
Dependent Claim
42 words
A method of claim 14 in which 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 17
Dependent Claim
15 words
A method of claim 14 in which the H-2 histamine receptor inhibitor is N-methyl-N''-(4-(4(5) -imidazolyl)butyl)thiourea.
Claim 18
Dependent Claim
14 words
A method of claim 14 in which the H-2 histamine receptor inhibitor is N-methyl-N''-(2-((4-methyl-5-imidazolyl)-methylthio)ethyl)thiourea.
Claim 19
Dependent Claim
19 words
A method of claim 15 in which the antihistamine is mepyramine and the H-2 histamine receptor inhibitor is N-methyl-N''-(4-(4(5)-imidazolyl)butyl)thiourea.
Claim 20
Dependent Claim
20 words
A method of claim 15 in which the antihistamine is mepyramine and the H-2 histamine receptor inhibitor is N-methyl-N''(2- ((4-methyl-5-imidazolyl)methylthio)ethyl)thiourea.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1978-07-07 | 1979-01-06 | 1979-07-08 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1982-07-07 | 1983-01-06 | 1983-07-08 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1986-07-07 | 1987-01-06 | 1987-07-08 | $7700.00 | Window Closed / Lapsed |