US4497812A
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US
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2-Amino-5-aminomethyl-2-oxazolines, compositions and use
Assignee: Cortial SA
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Filing: 1983-10-05
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Granted: 1985-02-05
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Expires: 2003-10-05
Abstract
Abstract This invention relates to new 2-amino-5-aminomethyl-2-oxazolines, the method of preparing them, and their pharmacological properties making possible their application in cardiovascular, psychotropic, antiinflammatory antiallergic, antihistamine, antiH 2 therapy. These new products have the general formula: ##STR1## wherein R 1 and R 2 independently represent an alkyl radical of C 1 to C 4 , or a carbocyclic alkyl radical having less than 4 rings, or a carbocyclic radical having less than 4 rings; R 1 and R 2 can form, with the nitrogen atom to which they are attached, a 4 to 7 member heterocycle containing 1 or 2 nitrogen atoms, and either 1 or 0 oxygen atoms. This heterocycle can be substituted by R with R being a lower alkyl, allyl, benzyl, pyridyl, phenyl substituted or not by one or more substituents such as halogen, trifluoromethyl, methyl, methoxy, hydroxy.
Inventors
- 👤 Marie-Helene Creuzet
- 👤 Claude Feniou
- 👤 Christian Jarry
- 👤 Gisele Prat
- 👤 Henri Pontagnier
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 15:31
CPC Classifications
C; C07; C07D; C07D303/00; C07D303/02; C07D303/36; A; A61; A61P; A61P1/00; A61P1/04; A61P25/00; A61P25/18; A61P25/20; A61P25/24; A61P25/26; A61P29/00; A61P3/00; A61P3/06; A61P37/00; A61P37/08; A61P43/00; A61P7/00; A61P7/10; A61P9/00; A61P9/08; A61P9/10; A61P9/12; C07D263/00; C07D263/02; C07D263/08; C07D263/16; C07D263/28
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
157 words
A compound having the general formula: ##STR15## wherein R 1 and R 2 independently represent an alkyl radical of C 1 to C 4 , or a carbocyclic alkyl radical having less than 4 rings, or a carbocyclic radical having less than 4 rings; R 1 and R 2 can form, with the nitrogen atom to which they are attached, a 4 to 7 member heterocycle containing 1 or 2 nitrogen atoms, and either 1 or 0 oxygen atoms, said heterocycle can be substituted by R with R being an alkyl radical of C 1 to C 4 , a carbocyclic alkyl radical having less than 4 rings, allyl, a 5 or 6 member heterocycle containing 1 nitrogen, or a carbocyclic radical having less than 4 rings substituted or not by one or more substituents such as halogen, trihalomethyl alkyl of C 1 to C 4 , alkyloxy of C 1 to C 4 , or hydroxy.
Claim 2
Dependent Claim
157 words
A compound having the general formula: ##STR15## wherein R 1 and R 2 independently represent an alkyl radical of C 1 to C 4 , or a carbocyclic alkyl radical having less than 4 rings, or a carbocyclic radical having less than 4 rings; R 1 and R 2 can form, with the nitrogen atom to which they are attached, a 4 to 7 member heterocycle containing 1 or 2 nitrogen atoms, and either 1 or 0 oxygen atoms, said heterocycle can be substituted by R with R being an alkyl radical of C 1 to C 4 , a carbocyclic alkyl radical having less than 4 rings, allyl, a 5 or 6 member heterocycle containing 1 nitrogen, or a carbocyclic radical having less than 4 rings substituted or not by one or more substituents such as halogen, trihalomethyl alkyl of C 1 to C 4 , alkyloxy of C 1 to C 4 , or hydroxy.
Claim 3
Dependent Claim
30 words
The compound of claim 1, wherein R 1 and R 2 are independently chosen from the group consisting of methyl, ethyl, n-propyl, iso-propyl, n-butyl, sec-butyl, iso-butyl, tert-butyl, benzyl, and phenyl.
Claim 4
Dependent Claim
28 words
The compound of claim 1, wherein said heterocycle formed by R 1 and R 2 is chosen from the group consisting of piperidine, pyrrolidone, morpholine, tetrahydroisoquinoline, and piperazine.
Claim 5
Dependent Claim
30 words
A pharmaceutical or veterinary composition characterized in that it contains as active principle at least a product as in claim 1 in association with a pharmaceutical vehicle or suitable excipient.
Claim 6
Dependent Claim
18 words
A method for cardiovascular therapy which comprises administration of an effective amount of a compound of claim 1.
Claim 7
Dependent Claim
18 words
A method for allergology therapy which comprises administration of an effective amount of a compound of claim 1.
Claim 8
Dependent Claim
19 words
A method for gastroduodenal ulcer therapy which comprises administration of an effective amount of a compound of claim 1.
Claim 9
Dependent Claim
18 words
A method for psychotropic therapy which comprises administration of an effective amount of a compound of claim 1.
References Cited (Backward Citations)
US3299089A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-02-05 | 1988-08-06 | 1989-02-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-02-05 | 1992-08-06 | 1993-02-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-02-05 | 1996-08-06 | 1997-02-05 | $7700.00 | Window Closed / Lapsed |