US4192879A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Imidazolyl alkylamino nitroethylene compounds
Assignee: Smith Kline & French Laboratories Ltd
•
Filing: 1978-03-31
•
Granted: 1980-03-11
•
Expires: 1998-03-31
Abstract
Abstract The compounds are novel N-substituted-N'-heterocyclic alkylthioureas, guanidines and 1-nitro-2,2-diaminoethylene compounds which are histamine H2-antagonists.
Inventors
- 👤 Graham J. Durant
- 👤 Charon R. Ganellin
- 👤 Geoffrey R. Owen
- 👤 Rodney C. Young
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 04:10
CPC Classifications
C; C07; C07D; C07D233/00; C07D233/54; C07D233/64; C07D277/00; C07D277/02; C07D277/20; C07D277/22; C07D277/26
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
85 words
A compound of the formula: ##STR19## wherein X is CHNO 2 ; Y is amino, lower alkylamino, di(lower alkyl)amino, lower alkoxy, phenylethyl, imidazolylethyl, allyl, 2,2,2-trifluoroethyl, or (CH 2 ) n R; Z is sulphur or methylene; Het is an imidazole ring which is attached at a ring carbon and which ring is optionally substituted by lower alkyl or halogen; n is an integer from 1 to 12; and R is hydroxy, lower alkoxy, amino or lower alkylamino; or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
85 words
A compound of the formula: ##STR19## wherein X is CHNO 2 ; Y is amino, lower alkylamino, di(lower alkyl)amino, lower alkoxy, phenylethyl, imidazolylethyl, allyl, 2,2,2-trifluoroethyl, or (CH 2 ) n R; Z is sulphur or methylene; Het is an imidazole ring which is attached at a ring carbon and which ring is optionally substituted by lower alkyl or halogen; n is an integer from 1 to 12; and R is hydroxy, lower alkoxy, amino or lower alkylamino; or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
17 words
A compound according to claim 1 wherein Het is imidazole optionally substituted by methyl, chloro or bromo.
Claim 4
Dependent Claim
10 words
A compound according to claim 2 wherein Het is 4-methyl-5-imidazolyl.
Claim 5
Dependent Claim
24 words
A compound according to claim 1 wherein Y is amino, 2,2,2-trifluoroethyl, (CH 2 ) n OH or (CH 2 ) n NH 2 .
Claim 6
Dependent Claim
37 words
A compound according to claim 1 wherein Y is amino, lower alkoxy, phenylethyl, imidazolylethyl, 2,2,2-trifluoroethyl or (CH 2 ) n R; n is an integer from 1 to 11 and R is hydroxy, lower alkoxy or amino.
Claim 7
Dependent Claim
22 words
A compound according to claim 5 wherein n is an integer from 1 to 7 and R is hydroxy or lower alkoxy.
Claim 8
Dependent Claim
9 words
A compound of claim 1, said compound being 1-nitro-2-hydrazino-2-[2-((4-methyl-5-imidazolyl)methylthio)ethylamino]ethylene.
Claim 9
Dependent Claim
9 words
A compound of claim 1, said compound being 1-nitro-2-(2,2,2-trifluoroethylamino)-2-[2-((4-methyl-5-imidazolyl)methylthio)ethylamino]ethylene.
Claim 10
Dependent Claim
30 words
A pharmaceutical composition to block histamine H 2 -receptors comprising in an effective amount to block said receptors a compound according to claim 1 and a pharmaceutical diluent or carrier.
Claim 11
Dependent Claim
30 words
A method of blocking histamine H 2 -receptors which comprises administering to an animal in need thereof in an effective amount to block said receptors a compound of claim 1.
References Cited (Backward Citations)
GB1305549A
Cited
US3868457A
Cited
US3968216A
Cited
US3808336A
Cited
DE2211454A1
Cited
US3950333A
Cited
US4000296A
Cited
US3953460A
Cited
US4046907A
Cited
US4124717A
Cited
US4109003A
Cited
US4034101A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-03-11 | 1983-09-10 | 1984-03-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-03-11 | 1987-09-10 | 1988-03-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-03-11 | 1991-09-10 | 1992-03-11 | $7700.00 | Window Closed / Lapsed |