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US3976643A
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US
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Guanidines
Assignee: William H Rorer Inc
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Filing: 1975-02-20
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Granted: 1976-08-24
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Expires: 1995-02-20
Abstract
Abstract Novel substituted phenylquanidine compounds and processes for their preparation are disclosed. Their use as anti-hypertensive agents is also revealed.
Inventors
- 👤 Julius Diamond
- 👤 George H. Douglas
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 19:30
CPC Classifications
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Claims Analysis
Total Claims: 3
Claim 1
Independent Claim
174 words
A process for the preparations of a guanidine compound of the formula: ##EQU9## where: R 2 , R 3 , R 4 ,R 5 and R 6 may be the same or different and are hydrogen, provided at least one of R 2 , R 3 , R 4 , R 5 and R 6 is other than hydrogen, halo, haloloweralkyl, nitro, cyano, loweralkylsulfonyl, loweralkoxy or loweralkyl, R, r' and R" are hydrogen, loweralkyl, intermediate alkyl, loweralkenyl, cycloalkyl, cycloalkylloweralkyl, aralkyl, cycloalkenyl, acyl, aroyl or aryl; R' and R" together are loweralkylidenyl or heteroloweralkylidenyl; and the non-toxic acid addition salts thereof; which comprises: intimately contacting a substituted aniline of the formula: ##SPC3## where R 2 , r 3 , r 4 , r 5 and R 6 are as described above and HX' is the salt of a mineral acid; with a cyanamide of the formula: ##EQU10## in the presence of a phenolic solvent selected from the group consisting of: phenol, cresol and xylenol; at temperatures from about 25°C to 150°C and isolating said guanidine.
Claim 2
Dependent Claim
174 words
A process for the preparations of a guanidine compound of the formula: ##EQU9## where: R 2 , R 3 , R 4 ,R 5 and R 6 may be the same or different and are hydrogen, provided at least one of R 2 , R 3 , R 4 , R 5 and R 6 is other than hydrogen, halo, haloloweralkyl, nitro, cyano, loweralkylsulfonyl, loweralkoxy or loweralkyl, R, r' and R" are hydrogen, loweralkyl, intermediate alkyl, loweralkenyl, cycloalkyl, cycloalkylloweralkyl, aralkyl, cycloalkenyl, acyl, aroyl or aryl; R' and R" together are loweralkylidenyl or heteroloweralkylidenyl; and the non-toxic acid addition salts thereof; which comprises: intimately contacting a substituted aniline of the formula: ##SPC3## where R 2 , r 3 , r 4 , r 5 and R 6 are as described above and HX' is the salt of a mineral acid; with a cyanamide of the formula: ##EQU10## in the presence of a phenolic solvent selected from the group consisting of: phenol, cresol and xylenol; at temperatures from about 25°C to 150°C and isolating said guanidine.
Claim 3
Dependent Claim
18 words
A process according to claim 1 where the reaction is carried out at temperatures between 60°C to 100°C.
References Cited (Backward Citations)
US3860648A
Cited
US3830933A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1979-08-24 | 1980-02-23 | 1980-08-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-08-24 | 1984-02-23 | 1984-08-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-08-24 | 1988-02-23 | 1988-08-24 | $7700.00 | Window Closed / Lapsed |