Patent US3932644A successfully refreshed from Google Patents.
US3932644A
Expired / Lapsed
US
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H2 histamine receptor inhibitors
Assignee: GlaxoSmithKline LLC
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Filing: 1974-04-24
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Granted: 1976-01-13
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Expires: 1994-04-24
Abstract
Abstract Heterocyclic compounds which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A specific compound of this invention is 2-[2-(4-methyl-5-imidazolylmethylthio)ethylamino]-4-pyrimidone.
Inventors
- 👤 Graham John Durant
- 👤 John Colin Emmett
- 👤 Charon Robin Ganellin
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 21:58
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/56; A; A61; A61P; A61P1/00; A61P1/04; A61P43/00; C07D233/00; C07D233/54; C07D233/66; C07D233/86; C07D233/88; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
132 words
A pharmaceutical composition to inhibit H-2 histamine receptors, said H-2 histamine receptors being those histamine receptors which are not inhibited by mepyramine but are inhibited by burimamide, comprising a pharmaceutical carrier and in an effective amount to inhibit said receptors a heterocyclic compound of the formula: ##SPC4## wherein A taken together with the nitrogen and carbon atoms shown forms a pyridine ring, said ring having a keto or thione group and optionally substituted by one or two lower alkyl, phenyl or benzyl groups; R is a grouping of the formula: Het--CH.sub.2 Z(CH.sub.2).sub.n -- wherein Het is an imidazole ring, said ring being optionally substituted by lower alkyl, amino, hydroxy or halogen; Z is sulphur or a methylene group and n is 2 or 3 or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
132 words
A pharmaceutical composition to inhibit H-2 histamine receptors, said H-2 histamine receptors being those histamine receptors which are not inhibited by mepyramine but are inhibited by burimamide, comprising a pharmaceutical carrier and in an effective amount to inhibit said receptors a heterocyclic compound of the formula: ##SPC4## wherein A taken together with the nitrogen and carbon atoms shown forms a pyridine ring, said ring having a keto or thione group and optionally substituted by one or two lower alkyl, phenyl or benzyl groups; R is a grouping of the formula: Het--CH.sub.2 Z(CH.sub.2).sub.n -- wherein Het is an imidazole ring, said ring being optionally substituted by lower alkyl, amino, hydroxy or halogen; Z is sulphur or a methylene group and n is 2 or 3 or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
52 words
A pharmaceutical composition of claim 1 in which the heterocyclic compound is of the formula: ##SPC5## wherein R has the same significance as in claim 1; X is oxygen or sulphur and Y 1 and Y 2 , which may be the same or different, are hydrogen, lower alkyl, phenyl or benzyl.
Claim 4
Dependent Claim
13 words
A pharmaceutical composition of claim 1 in which the heterocyclic compound is 2-[2-(4-methyl-5-imidazolylmethylthio)ethylamino]-(1H)-pyrid-4-one.
Claim 5
Independent Claim
139 words
A method of inhibiting H-2 histamine receptors, said H-2 histamine receptors being those histamine receptors which are not inhibited by mepyramine but are inhibited by burimamide, which comprises administering to an animal in need of inhibition of said receptors in an effective amount to inhibit said receptors a heterocyclic compound of the formula: ##SPC6## wherein A taken together with the nitrogen and carbon atoms shown forms a pyridine ring, said ring having a keto or thione group and optionally substituted by one or two lower alkyl, phenyl or benzyl groups; R is a grouping of the formula: Het--CH.sub.2 Z(CH.sub.2).sub.n -- wherein Het is an imidazole ring, said ring being optionally substituted by lower alkyl, amino, hydroxy or halogen; Z is sulphur or a methylene group and n is 2 or 3 or a pharmaceutically acceptable acid addition salt thereof.
Claim 6
Independent Claim
139 words
A method of inhibiting H-2 histamine receptors, said H-2 histamine receptors being those histamine receptors which are not inhibited by mepyramine but are inhibited by burimamide, which comprises administering to an animal in need of inhibition of said receptors in an effective amount to inhibit said receptors a heterocyclic compound of the formula: ##SPC6## wherein A taken together with the nitrogen and carbon atoms shown forms a pyridine ring, said ring having a keto or thione group and optionally substituted by one or two lower alkyl, phenyl or benzyl groups; R is a grouping of the formula: Het--CH.sub.2 Z(CH.sub.2).sub.n -- wherein Het is an imidazole ring, said ring being optionally substituted by lower alkyl, amino, hydroxy or halogen; Z is sulphur or a methylene group and n is 2 or 3 or a pharmaceutically acceptable acid addition salt thereof.
Claim 7
Dependent Claim
50 words
A method of claim 4 wherein the heterocyclic compound is of the formula ##SPC7## wherein R has the same significance as in claim 4; X is oxygen or sulphur and Y 1 and Y 2 , which may be the same or different, are hydrogen, lower alkyl, phenyl or benzyl.
Claim 8
Dependent Claim
12 words
A method of claim 4 in which the heterocyclic compound is 2-[2-(4-methyl-5-imidazolylmethylthio)ethylamino]-(1H)-pyrid-4-one.
Claim 9
Independent Claim
123 words
A method of inhibiting gastric acid secretion which comprises administering internally to an animal in need of inhibition of gastric acid secretion in an effective amount to inhibit gastric acid secretion a heterocyclic compound of the formula: ##SPC8## wherein A taken together with the nitrogen and carbon atoms shown forms a pyridine ring, said ring having a keto or thione group and optionally substituted by one or two lower alkyl, phenyl or benzyl groups; R is a grouping of the formula: Het--CH.sub.2 Z(CH.sub.2).sub.n -- wherein Het is an imidazole ring, said ring being optionally substituted by lower alkyl, amino, hydroxy or halogen; Z is sulphur or a methylene group and n is 2 or 3 or a pharmaceutically acceptable acid addition salt thereof.
Claim 10
Independent Claim
123 words
A method of inhibiting gastric acid secretion which comprises administering internally to an animal in need of inhibition of gastric acid secretion in an effective amount to inhibit gastric acid secretion a heterocyclic compound of the formula: ##SPC8## wherein A taken together with the nitrogen and carbon atoms shown forms a pyridine ring, said ring having a keto or thione group and optionally substituted by one or two lower alkyl, phenyl or benzyl groups; R is a grouping of the formula: Het--CH.sub.2 Z(CH.sub.2).sub.n -- wherein Het is an imidazole ring, said ring being optionally substituted by lower alkyl, amino, hydroxy or halogen; Z is sulphur or a methylene group and n is 2 or 3 or a pharmaceutically acceptable acid addition salt thereof.
References Cited (Backward Citations)
US3654291A
Cited
US3853897A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1979-01-12 | 1979-07-14 | 1980-01-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-01-12 | 1983-07-14 | 1984-01-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-01-12 | 1987-07-14 | 1988-01-13 | $7700.00 | Window Closed / Lapsed |