US4038408A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Certain thiazolyl and isothiazolyl compounds and compositions and methods which employ them
Assignee: Smith Kline & French Laboratories Ltd
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Filing: 1976-07-13
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Granted: 1977-07-26
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Expires: 1996-07-13
Abstract
Abstract The compounds are heterocyclomethylsulphinylethyl derivatives of N-cyanoguanidines, thioureas and 2-amino-1-nitroethylene which are histamine H 2 -antagonists or are converted into histamine H 2 -antagonists in the animal body. Two specific compounds of the present invention are 1-nitro-2-[2-((2-thiazolyl)methylsulphinyl)ethylamino]-2-[2-((2-thiazolyl)methylthio)ethylamino]ethylene and 1-nitro-2,2-bis-[2-((2-thiazolyl)methylsulphinyl)ethylamino]ethylene.
Inventors
- 👤 Graham John Durant
- 👤 Charon Robin Ganellin
- 👤 Torben Hesselbo
- 👤 George Raymond White
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 12:45
CPC Classifications
C; C07; C07D; C07D277/00; C07D277/02; C07D277/20; C07D277/22; C07D277/26; A; A61; A61P; A61P37/00; A61P37/08; A61P9/00
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
50 words
A compound of the formula: ##STR6## wherein Het and Het' are each selected from imidazole optionally substituted by methyl or bromo, thiazole, and isothiazole, provided that at least one of Het and Het' is thiazole or isothiazole; Z is sulphur, SO or methylene; X is sulphur, CHNO 2 or NCN.
Claim 2
Dependent Claim
50 words
A compound of the formula: ##STR6## wherein Het and Het' are each selected from imidazole optionally substituted by methyl or bromo, thiazole, and isothiazole, provided that at least one of Het and Het' is thiazole or isothiazole; Z is sulphur, SO or methylene; X is sulphur, CHNO 2 or NCN.
Claim 3
Dependent Claim
32 words
A compound according to claim 1 wherein Het and Het' are each selected from 5-methyl-4-imidazolyl, 5-bromo-4-imidazolyl, 2-thiazolyl and 3-isothiazolyl, provided that at least one of Het and Het' is 2-thiazolyl or 3-isothiazolyl.
Claim 4
Dependent Claim
11 words
A compound of claim 1 wherein Het and Het' are identical.
Claim 5
Dependent Claim
11 words
A compound of claim 1 wherein Z is sulphur or methylene.
Claim 6
Dependent Claim
9 words
A compound of claim 1 wherein Z is sulphur.
Claim 7
Dependent Claim
12 words
A compound of claim 1 wherein X is CHNO 2 or NCN.
Claim 8
Dependent Claim
9 words
A compound of claim 1, said compound being 1-nitro-2-[2-((2-thiazolyl)methylsulphinyl)ethylamino]-2-[2-((thiazolyl)methylthio)ethylamino]ethylene.
Claim 9
Dependent Claim
9 words
A compound of claim 1, said compound being 1-nitro-2,2-bis-[2-((thiazolyl)methylsulphinyl)ethylamino]ethylene.
Claim 10
Dependent Claim
35 words
A pharmaceutical composition for oral administration to block histamine H 2 -receptors comprising in an amount effective to block said receptors a compound of claim 1 in combination with a pharmaceutically acceptable diluent or carrier.
Claim 11
Dependent Claim
32 words
A pharmaceutical composition to block histamine H 2 -receptors comprising in an amount effective to block said receptors a compound of claim 4 in combination with a pharmaceutically acceptable diluent or carrier.
Claim 12
Dependent Claim
27 words
A method of blocking histamine H 2 -receptors which comprises administering in an amount effective to block said receptors to an animal a compound of claim 1.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-07-25 | 1981-01-24 | 1981-07-26 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-07-25 | 1985-01-24 | 1985-07-26 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-07-25 | 1989-01-24 | 1989-07-26 | $7700.00 | Window Closed / Lapsed |