US4083983A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Alkoxy pyridine compounds
Assignee: Smith Kline & French Laboratories Ltd
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Filing: 1976-07-13
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Granted: 1978-04-11
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Expires: 1996-07-13
Abstract
Abstract The compounds are alkoxypyridine compounds which are histamine H2-antagonists. Two specific compounds of the present invention are N-cyano-N'-methyl-N''-[2-((3-methoxy-2-pyridyl)methylthio)ethyl]guanidine and 1-methylamino-1-[2-(3-methoxy-2-pyridyl)methylthio)ethylamino]-2-nitro ethylene.
Inventors
- 👤 Graham John Durant
- 👤 Charon Robin Ganellin
- 👤 George Sidney Sach
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 23:50
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/78; C07D213/79; A; A61; A61P; A61P1/00; A61P1/04; A61P29/00; A61P43/00; C07D213/62; C07D213/63; C07D213/65; C07D213/68
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
113 words
A compound of the formula: ##STR6## wherein Het is a grouping of the formula: ##STR7## wherein R' is lower alkyl or --(CH 2 ) p A where p is 2 to 4 and A is hydroxy, lower alkoxy or dimethylamino; R 2 is hydrogen, lower alkyl, lower alkoxy, amino, halogen or methylamino; or --OR' and R 2 can together form a --O(CH 2 ) q O-- group attached to adjacent carbon atoms on the pyridine ring, where q is 1 to 4; Z is sulphur or methylene; n is 2 or 3; X is NH, NCN or NOH; Y is hydrogen, lower alkyl or 2-hydroxyethyl; or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
113 words
A compound of the formula: ##STR6## wherein Het is a grouping of the formula: ##STR7## wherein R' is lower alkyl or --(CH 2 ) p A where p is 2 to 4 and A is hydroxy, lower alkoxy or dimethylamino; R 2 is hydrogen, lower alkyl, lower alkoxy, amino, halogen or methylamino; or --OR' and R 2 can together form a --O(CH 2 ) q O-- group attached to adjacent carbon atoms on the pyridine ring, where q is 1 to 4; Z is sulphur or methylene; n is 2 or 3; X is NH, NCN or NOH; Y is hydrogen, lower alkyl or 2-hydroxyethyl; or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
14 words
A compound of claim 1 wherein the 6-position of the pyridine ring is unsubstituted.
Claim 4
Dependent Claim
23 words
A compound of claim 1 wherein --OR' and R 2 are in the 3 and 4 position of the pyridine ring comprising Het.
Claim 5
Dependent Claim
10 words
A compound of claim 1 wherein R 2 is hydrogen.
Claim 6
Dependent Claim
18 words
A compound of claim 4 wherein --OR' is in the 3 position of the pyridine ring comprising Het.
Claim 7
Dependent Claim
10 words
A compound of claim 1 wherein R' is lower alkyl.
Claim 8
Dependent Claim
9 words
A compound of claim 6 wherein R' is methyl.
Claim 9
Dependent Claim
9 words
A compound of claim 1 wherein Z is sulphur.
Claim 10
Dependent Claim
9 words
A compound of claim 1 wherein n is 2.
Claim 11
Dependent Claim
9 words
A compound of claim 1 wherein X is NCN.
Claim 12
Dependent Claim
10 words
A compound of claim 1 wherein Y is lower alkyl.
Claim 13
Dependent Claim
9 words
A compound of claim 1 wherein Y is methyl.
Claim 14
Dependent Claim
9 words
A compound of claim 1, said compound being N-cyano-N'-methyl-N"-[2-(3-methoxy-2-pyridylmethylthio)ethyl]guanidine.
Claim 15
Dependent Claim
9 words
A compound of claim 1, said compound being N-cyano-N'-methyl-N"-[2-(3-ethoxy-2-pyridylmethylthio)ethyl]guanidine.
Claim 16
Dependent Claim
9 words
A compound of claim 1, said compound being N-cyano-N'-methyl-N"-[2-(4-methoxy-2-pyridylmethylthio)ethyl]guanidine.
Claim 17
Dependent Claim
9 words
A compound of claim 1, said compound being N-cyano-N'-methyl-N"-[2-(3,4-dimethoxy-2-pyridylmethylthio)ethyl]guanidine
Claim 18
Dependent Claim
9 words
A compound of claim 1, said compound being N-cyano-N'-methyl-N"-[2-(3-chloro-4-methoxy-2-pyridylmethylthio)ethyl]guanidine.
Claim 19
Dependent Claim
9 words
A compound of claim 1, said compound being N-cyano-N'-methyl-N"-[4-(3-methoxy-2-pyridyl)butyl]guanidine.
Claim 20
Dependent Claim
32 words
A pharmaceutical composition to block histamine H 2 -receptors comprising in an effective amount to block said receptors a compound of claim 1 in combination with a pharmaceutically acceptable diluent or carrier.
Claim 21
Dependent Claim
37 words
A method of blocking histamine H 2 -receptors which comprises administering orally or parenterally to an animal in need of blocking of said receptors in an effective amount to block said receptors, a compound of claim 1.
References Cited (Backward Citations)
US3950333A
Cited
US3876647A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-04-10 | 1981-10-10 | 1982-04-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-04-10 | 1985-10-10 | 1986-04-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-04-10 | 1989-10-10 | 1990-04-11 | $7700.00 | Window Closed / Lapsed |