US4000296A
Expired / Lapsed
US
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Imidazole alkylguanidine compounds
Assignee: Smith Kline & French Laboratories Ltd
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Filing: 1975-03-21
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Granted: 1976-12-28
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Expires: 1995-03-21
Abstract
Abstract The compounds are guanidines, for example N-benzenesulphonyl-N'-[2-((4-methyl-5-imidazolyl)-methylthio)ethyl]gua nidine, which are inhibitors of histamine activity.
Inventors
- 👤 Graham John Durant
- 👤 John Colin Emmett
- 👤 Charon Robin Ganellin
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 11:00
CPC Classifications
C; C07; C07C; C07C281/00; C07C281/16; C07C281/18; C07D; C07D233/00; C07D233/04; C07D233/06; C07D233/08
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
122 words
A compound of the formula: ##STR6## wherein R 1 is hydrogen or lower alkyl; R 2 is a grouping of the formula Het - (CH 2 ) m Z(CH 2 ) n - wherein Het is imidazole which is optionally substituted by lower alkyl, trifluoromethyl or halogen; Z is sulphur, oxygen, NH or a methylene group; m is 0, 1 or 2 and n is 2 or 3, the sum of m and n being from 2 to 4; X is COR 3 , CSR 3 or SO 2 R 4 ; R 3 is amino and R 4 is lower alkyl, trifluoromethyl, amino or phenyl optionally substituted by halogen, lower alkyl or amino; or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
122 words
A compound of the formula: ##STR6## wherein R 1 is hydrogen or lower alkyl; R 2 is a grouping of the formula Het - (CH 2 ) m Z(CH 2 ) n - wherein Het is imidazole which is optionally substituted by lower alkyl, trifluoromethyl or halogen; Z is sulphur, oxygen, NH or a methylene group; m is 0, 1 or 2 and n is 2 or 3, the sum of m and n being from 2 to 4; X is COR 3 , CSR 3 or SO 2 R 4 ; R 3 is amino and R 4 is lower alkyl, trifluoromethyl, amino or phenyl optionally substituted by halogen, lower alkyl or amino; or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
30 words
A compound according to claim 1 wherein X is COR 3 or SO 2 R 4 and R 3 and R 4 have the same significance as in claim 1.
Claim 4
Dependent Claim
11 words
A compound according to claim 1 wherein R 1 is methyl.
Claim 5
Dependent Claim
17 words
A compound according to claim 1 wherein Z is sulphur, m is 1 and n is 2.
Claim 6
Dependent Claim
21 words
A compound according to claim 1 wherein Het is an imidazolyl, ring which ring is optionally substituted by methyl or halogen.
Claim 7
Dependent Claim
13 words
A compound according to claim 1 wherein X is phenylsulphonyl, aminosulphonyl or aminocarbonyl.
Claim 8
Dependent Claim
10 words
A compound according to claim 1, said compound being N-benzenesulphonyl-N'-[2-((4-methyl-5-imidazolyl)methylthio)ethyl]guanidine.
Claim 9
Dependent Claim
50 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 in an effective amount to inhibit said receptors a compound according to claim 1 and a non-toxic pharmaceutically acceptable diluent or carrier.
Claim 10
Dependent Claim
52 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 compound of claim 1.
Claim 11
Dependent Claim
36 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 compound of claim 1.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1979-12-28 | 1980-06-28 | 1980-12-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-12-28 | 1984-06-28 | 1984-12-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-12-28 | 1988-06-28 | 1988-12-28 | $7700.00 | Window Closed / Lapsed |