US4277485A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Oxazole or isoxazole alkylamino ethylene compounds as inhibitors of H-2 histamine receptors
Assignee: Smith Kline & French Laboratories Ltd
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Filing: 1980-02-04
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Granted: 1981-07-07
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Expires: 2000-02-04
Abstract
Abstract The compounds are ethylene derivatives which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A compound of this invention is 1-nitro-2-methylamino-2-[2-((4-methyl-5-imidazolyl)methylthio)-ethylam ino]ethylene.
Inventors
- 👤 Graham J. Durant
- 👤 John C. Emmett
- 👤 Charon F. Ganellin
- 👤 Hunter D. Prain
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 10:07
CPC Classifications
C; C07; C07D; C07D275/00; C07D275/02; C07D213/00; C07D213/02; C07D213/04; C07D213/24; C07D213/28; C07D213/32; C07D249/00; C07D249/02; C07D249/08; C07D261/00; C07D261/02; C07D261/06; C07D261/08; C07D285/00; C07D285/01; C07D285/02; C07D285/04; C07D285/08
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
148 words
A compound of the formula: ##STR8## wherein X and Y, which may be the same or different, are hydrogen, nitro, cyano or SO 2 Ar but are not both hydrogen; Het' is an oxazole or isoxazole ring which ring is attached at a ring carbon and is unsubstituted or substituted by lower alkyl, hydroxyl, halogen or amino; R is hydrogen, lower alkyl or Het-(CH 2 ) m Z(CH 2 ) n ; Z is sulphur or methylene; m is 0, 1 or 2 and n is 2 or 3 provided that the sum of m and n is 3 or 4; Het is an oxazole, isoxazole or triazole ring which ring is attached at a ring carbon and is unsubstituted or substituted by lower alkyl, hydroxyl, halogen or amino; and Ar is phenyl unsubstituted or substituted by halogen or methyl or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
148 words
A compound of the formula: ##STR8## wherein X and Y, which may be the same or different, are hydrogen, nitro, cyano or SO 2 Ar but are not both hydrogen; Het' is an oxazole or isoxazole ring which ring is attached at a ring carbon and is unsubstituted or substituted by lower alkyl, hydroxyl, halogen or amino; R is hydrogen, lower alkyl or Het-(CH 2 ) m Z(CH 2 ) n ; Z is sulphur or methylene; m is 0, 1 or 2 and n is 2 or 3 provided that the sum of m and n is 3 or 4; Het is an oxazole, isoxazole or triazole ring which ring is attached at a ring carbon and is unsubstituted or substituted by lower alkyl, hydroxyl, halogen or amino; and Ar is phenyl unsubstituted or substituted by halogen or methyl or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
26 words
A compound of claim 1 wherein X and Y are hydrogen, nitro or cyano, but are not both hydrogen; and R is hydrogen or lower alkyl.
Claim 4
Dependent Claim
27 words
A compound of claim 1 wherein R is methyl or Het-CH 2 SCH 2 CH 2 : Z is sulphur: m is 1 and n is 2.
Claim 5
Dependent Claim
13 words
A compound of claim 1 wherein X is nitro and Y is hydrogen.
Claim 6
Dependent Claim
26 words
A pharmaceutical composition to inhibit H-2 histamine receptors comprising a pharmaceutical carrier and in an effective amount to inhibit said receptors a compound of claim 1.
Claim 7
Dependent Claim
29 words
A method of inhibiting H-2 histamine receptors which comprises administering to an animal in need thereof in an effective amount to inhibit said receptors a compound of claim 1.
References Cited (Backward Citations)
US4154844A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-07-06 | 1985-01-05 | 1985-07-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-07-06 | 1989-01-05 | 1989-07-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-07-06 | 1993-01-05 | 1993-07-07 | $7700.00 | Window Closed / Lapsed |