US4022797A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Certain thiazole, isothiazole, oxazole, and isoxazole compounds
Assignee: Smith Kline & French Laboratories Ltd
•
Filing: 1975-12-04
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Granted: 1977-05-10
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Expires: 1995-12-04
Abstract
Abstract The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-guanidines 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
2026-11-04 13:41
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/62; C07D213/70; A; A61; A61P; A61P29/00; C07D213/24; C07D213/28; C07D213/32; C07D213/36; C07D213/38; C07D213/63; C07D213/65; C07D213/72; C07D213/74; C07D231/00; C07D231/02; C07D231/10; C07D231/12; C07D233/00; C07D233/54; C07D233/66; C07D233/84; C07D233/90; C07D235/00; C07D235/02; C07D235/04; C07D235/06; C07D249/00; C07D249/02; C07D249/08; C07D249/10; C07D249/12; C07D261/00; C07D261/02; C07D261/06; C07D261/08; C07D263/00; C07D263/02; C07D263/30; C07D263/34; C07D263/46; C07D275/00; C07D275/02; C07D275/03; C07D277/00; C07D277/02; C07D277/20; C07D277/22; C07D277/26; C07D285/00; C07D285/01; C07D285/02; C07D285/04; C07D285/12; C07D285/125; C07D285/135; C07D471/00; C07D471/02; C07D471/04
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
122 words
A compound of the formula: ##STR15## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being a thiazole, isothiazole, oxazole or isoxazole ring; X 1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl, halogen, amino or ##STR16## X 2 hydrogen or when X 1 is lower alkyl, lower alkyl or halogen; k is 0 to 2 and m is 2 or 3, provided that the sum of k and m is 3 or 4; Y is oxygen, sulphur or NH; E is NR 2 ; R 1 is hydrogen, lower alkyl or di-lower alkylamino-lower alkyl; and R 2 is hydrogen, nitro or cyano, or a pharmaceutically acceptable addition salt thereof.
Claim 2
Dependent Claim
122 words
A compound of the formula: ##STR15## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being a thiazole, isothiazole, oxazole or isoxazole ring; X 1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl, halogen, amino or ##STR16## X 2 hydrogen or when X 1 is lower alkyl, lower alkyl or halogen; k is 0 to 2 and m is 2 or 3, provided that the sum of k and m is 3 or 4; Y is oxygen, sulphur or NH; E is NR 2 ; R 1 is hydrogen, lower alkyl or di-lower alkylamino-lower alkyl; and R 2 is hydrogen, nitro or cyano, or a pharmaceutically acceptable addition salt thereof.
Claim 3
Dependent Claim
11 words
A compound of claim 1 wherein Y is oxygen or sulphur.
Claim 4
Dependent Claim
9 words
A compound of claim 1 wherein Y is NH.
Claim 5
Dependent Claim
21 words
A compound of claim 1 wherein said unsaturated heterocyclic nucleus is thiazole or oxazole and R 2 is hydrogen or nitro.
Claim 6
Dependent Claim
13 words
A compound of claim 4 wherein k is 1 and m is 2.
Claim 7
Dependent Claim
12 words
A compound of claim 1 wherein said unsaturated heterocyclic nucleus is thiazole.
Claim 8
Dependent Claim
28 words
A compound of claim 6 wherein X 1 is hydrogen, methyl, bromo, hydroxyl or amino and X 2 is hydrogen; Y is sulphur and R 1 is methyl.
Claim 9
Dependent Claim
9 words
A compound of claim 1, said compound being N-cyano-N'-methyl-N"-[2-(2-thiazolylmethylthio)ethyl]guanidine.
Claim 10
Dependent Claim
9 words
A compound of claim 1, said compound being N-cyano-N'-[2-(3-isothiazolylmethylthio)ethyl]-N"-methylguanidine.
Claim 11
Dependent Claim
9 words
A compound of claim 1, said compound being N-cyano-N-[2-(3-isoxazolylmethylthio)ethyl]-N"-methylguanidine.
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) | 1980-05-09 | 1980-11-08 | 1981-05-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-05-09 | 1984-11-08 | 1985-05-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-05-09 | 1988-11-08 | 1989-05-10 | $7700.00 | Window Closed / Lapsed |