US3968216A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Method of inhibiting histamine activity with guanidine compounds
Assignee: Smith Kline & French Laboratories Ltd
•
Filing: 1974-11-25
•
Granted: 1976-07-06
•
Expires: 1994-11-25
Abstract
Abstract A method of inhibiting histamine activity in particular inhibiting H-2 histamine receptors, by administering heterocyclicalkylguanidines.
Inventors
- 👤 James Whyte Black
- 👤 Graham John Durant
- 👤 John Colin Emmett
- 👤 Charon Robin Ganellin
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 09:56
CPC Classifications
C; C07; C07D; C07D277/00; C07D277/02; C07D277/20; C07D277/22; C07D277/28; C07D209/00; C07D209/02; C07D209/44; C07D209/48; C07D213/00; C07D213/02; C07D213/04; C07D213/24; C07D213/36; C07D213/40; C07D231/00; C07D231/02; C07D231/10; C07D231/12; C07D233/00; C07D233/04; C07D233/20; C07D233/24; C07D233/26; C07D233/54; C07D233/64; C07D249/00; C07D249/02; C07D249/08
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
148 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 internally to an animal requiring inhibition of said H-2 histamine receptors in an amount sufficient to inhibit said H-2 histamine receptors a compound of the formula: ##SPC5## in which: n is 2 to 5; A taken together with the carbon and nitrogen atoms to which it is attached forms a pyridine ring; R 1 is hydrogen, alkyl having 1 to 4 carbon atoms or benzyl; R 2 is hydrogen, alkyl having 1 to 4 carbon atoms, benzyl, imidazolylethyl or amino or R 1 and R 2 together form an ethylene bridge and R 3 is hydrogen, alkyl having 1 to 4 carbon atoms, alkylthio having 1 to 4 carbon atoms or amino or pharmaceutically acceptable acid addition salts thereof.
Claim 2
Independent Claim
148 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 internally to an animal requiring inhibition of said H-2 histamine receptors in an amount sufficient to inhibit said H-2 histamine receptors a compound of the formula: ##SPC5## in which: n is 2 to 5; A taken together with the carbon and nitrogen atoms to which it is attached forms a pyridine ring; R 1 is hydrogen, alkyl having 1 to 4 carbon atoms or benzyl; R 2 is hydrogen, alkyl having 1 to 4 carbon atoms, benzyl, imidazolylethyl or amino or R 1 and R 2 together form an ethylene bridge and R 3 is hydrogen, alkyl having 1 to 4 carbon atoms, alkylthio having 1 to 4 carbon atoms or amino or pharmaceutically acceptable acid addition salts thereof.
Claim 3
Dependent Claim
12 words
A method according to claim 1 in which the compound is 3-(2-pyridyl)propylguanidine.
Claim 4
Dependent Claim
12 words
A method according to claim 1 in which the compound is 2-(2-pyridyl)ethylguanidine.
Claim 5
Independent Claim
127 words
A method of inhibiting gastric acid secretion which comprises administering internally to an animal requiring inhibition of gastric acid secretion in an amount sufficient to inhibit gastric acid secretion a compound of the formula ##SPC6## in which: n is 2 to 5 A taken together with the carbon and nitrogen atoms to which it is attached forms a pyridine ring; R 1 is hydrogen, alkyl having 1 to 4 carbon atoms or benzyl; R 2 is hydrogen, alkyl having 1 to 4 carbon atoms, benzyl, imidazolylethyl or amino or R 1 and R 2 together form an ethylene bridge and R 3 is hydrogen, alkyl having 1 to 4 carbon atoms, alkylthio having 1 to 4 carbon atoms or amino or pharmaceutically acceptable acid addition salts thereof.
Claim 6
Independent Claim
127 words
A method of inhibiting gastric acid secretion which comprises administering internally to an animal requiring inhibition of gastric acid secretion in an amount sufficient to inhibit gastric acid secretion a compound of the formula ##SPC6## in which: n is 2 to 5 A taken together with the carbon and nitrogen atoms to which it is attached forms a pyridine ring; R 1 is hydrogen, alkyl having 1 to 4 carbon atoms or benzyl; R 2 is hydrogen, alkyl having 1 to 4 carbon atoms, benzyl, imidazolylethyl or amino or R 1 and R 2 together form an ethylene bridge and R 3 is hydrogen, alkyl having 1 to 4 carbon atoms, alkylthio having 1 to 4 carbon atoms or amino or pharmaceutically acceptable acid addition salts thereof.
Claim 7
Independent Claim
121 words
A method of producing anti-inflammatory activity which comprises administering to an animal requiring said activity in an amount sufficient to produce said activity a compound of the formula: ##SPC7## in which: n is 2 to 5; A taken together with the carbon and nitrogen atoms to which it is attached forms a pyridine ring; R 1 is hyrogen, alkyl having 1 to 4 carbon atoms or benzyl; R 2 is hydrogen, alkyl having 1 to 4 carbon atoms, benzyl, imidazolylethyl or amino or R 1 and R 2 together form an ethylene bridge and R 3 is hydrogen, alkyl having 1 to 4 carbon atoms, alkylthio having 1 to 4 carbon atoms or amino or pharmaceutically acceptable acid addition salts thereof.
Claim 8
Independent Claim
121 words
A method of producing anti-inflammatory activity which comprises administering to an animal requiring said activity in an amount sufficient to produce said activity a compound of the formula: ##SPC7## in which: n is 2 to 5; A taken together with the carbon and nitrogen atoms to which it is attached forms a pyridine ring; R 1 is hyrogen, alkyl having 1 to 4 carbon atoms or benzyl; R 2 is hydrogen, alkyl having 1 to 4 carbon atoms, benzyl, imidazolylethyl or amino or R 1 and R 2 together form an ethylene bridge and R 3 is hydrogen, alkyl having 1 to 4 carbon atoms, alkylthio having 1 to 4 carbon atoms or amino or pharmaceutically acceptable acid addition salts thereof.
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) | 1979-07-06 | 1980-01-05 | 1980-07-06 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-07-06 | 1984-01-05 | 1984-07-06 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-07-06 | 1988-01-05 | 1988-07-06 | $7700.00 | Window Closed / Lapsed |