Patent US4034101A successfully refreshed from Google Patents.
US4034101A
Expired / Lapsed
US
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N-Oxy and N-amino guanidines
Assignee: Smith Kline & French Laboratories Ltd
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Filing: 1975-06-11
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Granted: 1977-07-05
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Expires: 1995-06-11
Abstract
Abstract The compounds are N-oxy and N-amino guanidines which are histamine H2-antagonists. A compound of this invention is N-hydroxy-N'methyl-N''-[2-((4-methyl-5-imidazolyl)methylthio)-ethyl]gu anidine.
Inventors
- 👤 Graham John Durant
- 👤 Charon Robin Ganellin
- 👤 Geoffrey Robert Owen
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 16:47
CPC Classifications
C; C07; C07D; C07D233/00; C07D233/54; C07D233/64; A; A61; A61P; A61P43/00; C07C; C07C281/00; C07C281/16; C07C281/18; C07D213/00; C07D213/02; C07D213/04; C07D213/24; C07D213/28; C07D213/32; C07D277/00; C07D277/02; C07D277/20; C07D277/22; C07D277/26; C07D277/28
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
124 words
A compound of the formula: ##STR5## wherein R 1 represents a grouping of the structure shown in the formula: Het-- (CH.sub.2).sub.m Z(CH.sub.2).sub.n FORMULA II wherein Het is imidazole which is attached at a ring carbon and which is optionally substituted by lower alkyl, chlorine or bromine; Z is sulphur or a methylene group; m is 0, 1 or 2 and n is 2 or 3 provided that the sum of m and n is 3 or 4; R 2 is hydrogen, lower alkyl or a grouping of the structure shown in Formula II wherein Het, m, n and Z are as defined above; X is oxygen and R 3 is hydrogen, lower alkyl, phenyl or benzyl, or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
124 words
A compound of the formula: ##STR5## wherein R 1 represents a grouping of the structure shown in the formula: Het-- (CH.sub.2).sub.m Z(CH.sub.2).sub.n FORMULA II wherein Het is imidazole which is attached at a ring carbon and which is optionally substituted by lower alkyl, chlorine or bromine; Z is sulphur or a methylene group; m is 0, 1 or 2 and n is 2 or 3 provided that the sum of m and n is 3 or 4; R 2 is hydrogen, lower alkyl or a grouping of the structure shown in Formula II wherein Het, m, n and Z are as defined above; X is oxygen and R 3 is hydrogen, lower alkyl, phenyl or benzyl, or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
10 words
A compound of claim 1 wherein R 3 is hydrogen.
Claim 4
Dependent Claim
11 words
A compound of claim 1 wherein R 2 is lower alkyl.
Claim 5
Dependent Claim
15 words
A compound of claim 1 wherein R 2 is the same as R 1 .
Claim 6
Dependent Claim
13 words
A compound of claim 1 wherein m is 1 and n is 2.
Claim 7
Dependent Claim
9 words
A compound of claim 1 wherein Z is sulphur.
Claim 8
Dependent Claim
26 words
A compound of claim 1 wherein Het is imidazole which is attached at a ring carbon and which is optionally substituted by methyl, chlorine or bromine.
Claim 9
Dependent Claim
9 words
A compound of claim 1, said compound being N-hydroxy-N'-methyl-N"-[2-((4-methyl-5-imidazolyl)methylthio)ethyl]guanidine.
Claim 10
Dependent Claim
10 words
A compound of claim 1, said compound being N-hydroxy-N', N"-bis[2-((4-methyl-5-imidazolyl)methylthio)ethyl]guanidine.
Claim 11
Dependent Claim
9 words
A compound of claim 1, said compound being N-methoxy-N'-methyl-N"-[2-((4-methyl-5-imidazolyl)methylthio)ethyl]guanidine.
Claim 12
Dependent Claim
10 words
A compound of claim 1, said compound being N-methoxy-N', N"-bis[2-((4-methyl-5-imidazolyl)methylthio)ethyl]guanidine.
Claim 13
Dependent Claim
32 words
A pharmaceutical composition to block histamine H 2 -receptors comprising a pharmaceutically acceptable diluent or carrier and, in an effective amount to block histamine H 2 -receptors, a compound of claim 1.
Claim 14
Dependent Claim
38 words
A method of blocking histamine H 2 -receptors which comprises administering to an animal in need of blocking of histamine H 2 -receptors in an effective amount to block histamine H 2 -receptors a compound of claim 1.
Claim 15
Dependent Claim
30 words
A method of inhibiting gastric acid secretion which comprises administering to an animal in need thereof in an effective amount to inhibit gastric acid secretion a compound of claim 1.
Claim 16
Dependent Claim
50 words
A compound of the formula: ##STR6## wherein Het is imidazole which is attached at a ring carbon and which is optionally substituted by lower alkyl, chlorine or bromine; X is oxygen or NH; and R is hydrogen, lower alkyl, phenyl or benzyl, or a pharmaceutically acceptable acid addition salt thereof.
Claim 17
Dependent Claim
50 words
A compound of the formula: ##STR6## wherein Het is imidazole which is attached at a ring carbon and which is optionally substituted by lower alkyl, chlorine or bromine; X is oxygen or NH; and R is hydrogen, lower alkyl, phenyl or benzyl, or a pharmaceutically acceptable acid addition salt thereof.
Claim 18
Dependent Claim
10 words
A compound of claim 15, said compound being N-amino-N',N" -bis[2-((4-methyl-5-imidazolyl)methylthio)ethyl]guanidine.
Claim 19
Dependent Claim
32 words
A pharmaceutical composition to block histamine H 2 -receptors comprising a pharmaceutically acceptable diluent or carrier and, in an effective amount to block histamine H 2 -receptors, a compound of claim 15.
Claim 20
Dependent Claim
38 words
A method of blocking histamine H 2 -receptors which comprises administering to an animal in need of blocking of histamine H 2 -receptors in an effective amount to block histamine H 2 -receptors a compound of claim 15.
Claim 21
Dependent Claim
30 words
A method of inhibiting gastric acid secretion which comprises administering to an animal in need thereof in an effective amount to inhibit gastric acid secretion a compound of claim 15.
References Cited (Backward Citations)
DE2053175A1
Cited
DE2211454A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-07-04 | 1981-01-03 | 1981-07-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-07-04 | 1985-01-03 | 1985-07-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-07-04 | 1989-01-03 | 1989-07-05 | $7700.00 | Window Closed / Lapsed |