US4051256A
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Guanidine derivatives
Assignee: Imperial Chemical Industries Ltd
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Filing: 1976-09-19
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Granted: 1977-09-27
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Expires: 1996-09-19
Abstract
Abstract Guanidine derivatives of the formula: ##STR1## in which R 1 is a cyclohexyl, adamantyl, bicycloheptanyl, bicycloheptenyl, tricycloheptanyl or tetracyclononanyl radical and R 2 is a phenyl or pyridyl radical optionally substituted by 1 or 2 halogen atoms, or alkyl, cyanoalkyl, alkoxycarbonyl or amino radicals, and the pharmaceutically-acceptable acid-addition salts thereof, active against rhinoviruses, are disclosed, along with processes for their manufacture, compositions containing them, a method of combatting rhinoviral infections and a method of selectively killing rhinoviruses in a mixed virus population.
Inventors
- 👤 Douglas Lintin Swallow
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 12:19
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/13; A61K31/155
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
75 words
A compound of the formula: ##STR13## wherein R 1 is selected from the group consisting of adamantyl, bicyclo[2,2,1]heptanyl, bicyclo[2,2,1]hept-5-enyl, tricyclo[2,2,1,0 2 ,6 ]heptanyl and tetracyclo[4,3,0,0 2 ,4,0 3 ,7 ]-nonanyl and R 2 is selected from the group consisting of phenyl optionally substituted by a substituent selected from the group consisting of halogen, alkyl and cyanoalkyl of 1 to 6 carbons, alkoxycarbonyl of 2 to 6 carbons and amino, and the pharmaceutically-acceptable acid-addition salts thereof.
Claim 2
Dependent Claim
75 words
A compound of the formula: ##STR13## wherein R 1 is selected from the group consisting of adamantyl, bicyclo[2,2,1]heptanyl, bicyclo[2,2,1]hept-5-enyl, tricyclo[2,2,1,0 2 ,6 ]heptanyl and tetracyclo[4,3,0,0 2 ,4,0 3 ,7 ]-nonanyl and R 2 is selected from the group consisting of phenyl optionally substituted by a substituent selected from the group consisting of halogen, alkyl and cyanoalkyl of 1 to 6 carbons, alkoxycarbonyl of 2 to 6 carbons and amino, and the pharmaceutically-acceptable acid-addition salts thereof.
Claim 3
Dependent Claim
56 words
The compound of claim 1 wherein R 1 is selected from the group consisting of adamant-1-yl, exo-bicyclo[2,2,1]heptan-2-yl, endo-bicyclo[2,2,1]heptan-2-yl, exo-bicyclo[2,2,1]hept-5-en-2-yl, tricyclo[2,2,1,0 2 ,6 ]heptan-3-yl and tetracyclo[4,3,0,0 2 ,4,0 3 ,7 ]nonan-8-yl and R 2 is selected from the group consisting of phenyl optionally substituted selected from chlorine, bromine, methyl, cyanomethyl, methoxycarbonyl, amino and 1 or 2 fluorines.
Claim 4
Dependent Claim
20 words
The compound of claim 1 wherein R 1 is in the exo-configuration and R 2 carries a single optional substituent.
Claim 5
Dependent Claim
31 words
The compound of claim 1 wherein R 1 is selected from the group consisting of exo-bicyclo[2,2,1]hept-5-en-2-yl and exo-bicyclo[2,2,1]heptan-2-yl and R 2 is a phenyl radical which bears a single optional substituent.
Claim 6
Dependent Claim
26 words
The compound of claim 1 wherein R 1 is exo-bicyclo[2,2,1]hept-5-en-2-yl and R 2 is a phenyl radical which bears a single optional substituent in the 4-position.
Claim 7
Dependent Claim
20 words
The compound of claim 5 wherein the single optional substituent in R 2 is selected from fluorine, chlorine and bromine.
Claim 8
Dependent Claim
7 words
2-Exo-[3-(p-chlorophenyl)guanidino]bicyclo[2,2,1]hept-5-ene and the pharmaceutically-acceptable acid-addition salts thereof.
Claim 9
Dependent Claim
7 words
2-Exo-[3-(p-chlorophenyl)guanidino]bicyclo[2,2,1]hept-5-ene and the pharmaceutically-acceptable acid-addition salts thereof.
Claim 10
Dependent Claim
7 words
2-Exo-[3-(p-fluorophenyl)guanidino]bicyclo[2,2,1]-hept-5-ene and the pharmaceutically-acceptable acid-addition salts thereof.
Claim 11
Dependent Claim
7 words
2-Exo-[3-(p-fluorophenyl)guanidino]bicyclo[2,2,1]-hept-5-ene and the pharmaceutically-acceptable acid-addition salts thereof.
Claim 12
Dependent Claim
27 words
A pharmaceutical composition for combatting or preventing a rhinoviral infection in man comprising an effective amount of the compound of claim 1 together with a pharmaceutically-acceptable carrier.
Claim 13
Dependent Claim
23 words
A method of combatting or preventing a rhinoviral infection in man which comprises administering an anti-rhinovirally-effective amount of the 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) | 1980-09-26 | 1981-03-28 | 1981-09-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-09-26 | 1985-03-28 | 1985-09-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-09-26 | 1989-03-28 | 1989-09-27 | $7700.00 | Window Closed / Lapsed |