Patent US4038414A successfully refreshed from Google Patents.
US4038414A
Expired / Lapsed
US
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Amines and processes for their manufacture
Assignee: Novartis Corp
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Filing: 1975-12-19
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Granted: 1977-07-26
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Expires: 1995-12-19
Abstract
Abstract Amines of the formula ##STR1## wherein R 1 is lower alkyl, lower alkoxy or amino, R 2 is hydrogen or lower alkyl, R 3 is hydrogen, lower alkyl, carboxyl or lower alkoxycarbonyl, R 4 is hydrogen or lower alkyl, R 5 is lower alkyl, aryl-lower alkyl or optionally functionally modified carboxy-lower alkyl and R 6 denotes halogen, trifluoromethyl, lower alkyl, lower alkenyl, lower alkoxy, lower alkenyloxy, nitro, lower alkoxymethyl, carbamoyl, N-lower alkylcarbamoyl, nitrile, lower alkinyloxy or hydrogen, and their salts block cardiac and vascular β-receptors the are useful in the treatment of arrhythenias and angina pectoris and as intermediates for, especially for pharmaceutically active substances.
Inventors
- 👤 Knut Alfred Jaeggi
- 👤 Franz Ostermayer
- 👤 Herbert Schroter
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 10:55
CPC Classifications
C; C07; C07D; C07D263/00; C07D263/02; C07D263/30; C07D263/34; C07D263/36; C07D263/42; C07C; C07C45/00; C07C45/51; C07C45/511; C07C45/512; C07D263/04; C07D263/06
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
87 words
An amine of the formula I ##STR15## wherein R 1 is lower alkyl, R 2 is hydrogen or lower alkyl, R 3 is hydrogen or lower alkyl, R 4 is hydrogen or lower alkyl, R 5 is lower alkyl, phenyl-lower alkyl, or phenyl lower alkyl substituted by lower alkyl, lower alkoxy, halogen and/or trifluoromethyl and R 6 denotes halogeno, trifluoromethyl, lower alkyl, lower alkenyl, lower alkoxy, lower alkenyloxy, nitro, lower alkoxymethyl, carbamoyl, N-lower alkylcarbamoyl, cyano, lower alkinyloxy or hydrogen, or a therapeutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
87 words
An amine of the formula I ##STR15## wherein R 1 is lower alkyl, R 2 is hydrogen or lower alkyl, R 3 is hydrogen or lower alkyl, R 4 is hydrogen or lower alkyl, R 5 is lower alkyl, phenyl-lower alkyl, or phenyl lower alkyl substituted by lower alkyl, lower alkoxy, halogen and/or trifluoromethyl and R 6 denotes halogeno, trifluoromethyl, lower alkyl, lower alkenyl, lower alkoxy, lower alkenyloxy, nitro, lower alkoxymethyl, carbamoyl, N-lower alkylcarbamoyl, cyano, lower alkinyloxy or hydrogen, or a therapeutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
95 words
An amine as claimed in claim 1 and having the formula I, wherein R 1 is lower alkyl, R 2 is hydrogen or lower alkyl, R 3 is hydrogen, R 4 is hydrogen or lower alkyl with up to 4 carbon atoms, R 5 is α-branched lower alkyl or a group of the formula ##STR16## wherein n is 0, 1 or 2 and R is phenyl or phenyl substituted by halogen or lower alkoxy and R 6 is hydrogen, halogeno, lower alkoxy, lower alkenyl or lower alkenyloxy, or a therapeutically acceptable acid addition salt thereof.
Claim 4
Dependent Claim
120 words
An amine as claimed in claim 1 and having the formula I, wherein R 1 is lower alkyl with up to 4 carbon atoms, R 2 is hydrogen, R 3 is hydrogen, R 4 is hydrogen, R 5 is α-branched lower alkyl with 3 to 6 carbon atoms or a group of the formula ##STR17## wherein n' is 1 or 2 and R' is phenyl or phenyl substituted by chloro, bromo or lower alkoxy with up to 4 carbon atoms, and R 6 is hydrogen, chloro, bromo, lower alkoxy with up to 4 carbon atoms, lower alkenyl with 2 to 5 carbon atoms or lower alkenyloxy with 3 to 5 carbon atoms, or a therapeutically acceptable acid addition salt thereof.
Claim 5
Dependent Claim
89 words
An amine as claimed in claim 1 and having the formula I, wherein R 1 denotes ethyl or methyl, R 2 is hydrogen R 3 is hydrogen, R 4 is hydrogen, R 5 is α-branched lower alkyl with 3 or 4 carbon atoms or a group of the formula ##STR18## wherein n' is 1 or 2 and R" is phenyl or phenyl substituted by methoxy, ethoxy or chloro, and R 6 denotes hydrogen, methoxy, ethoxy, chloro, allyl, methallyl, 1-propenyl, allyloxy or methallyloxy, and therapeutically acceptable acid addition salts thereof.
Claim 6
Dependent Claim
53 words
An amine as claimed in claim 1 and having the formula I, wherein R 1 is methyl, R 2 is hydrogen, R 3 is hydrogen, R 4 is hydrogen, R 5 is isopropyl, tert.-butyl or 2-(3-phenyl)-butyl and R 6 is hydrogen, methoxy, chloro, allyloxy or allyl, or a therapeutically acceptable addition salt thereof.
Claim 7
Dependent Claim
14 words
1-[4-(2-Acetylaminovinyl)-2-allyl-phenoxy]-2-hydroxy-3-isopropylamino-propane as claimed in claim 1, or a therapeutically acceptable acid addition salt thereof.
Claim 8
Dependent Claim
29 words
A pharmaceutical composition useful in the treatment of arrhythmias and angina pectoris comprising a therapeutically effective amount of a compound of claim 1 together with a pharmaceutically acceptable excipient.
References Cited (Backward Citations)
US3852468A
Cited
US3634511A
Cited
US3712927A
Cited
US3872147A
Cited
US3755413A
Cited
US3864398A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-07-25 | 1981-01-24 | 1981-07-26 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-07-25 | 1985-01-24 | 1985-07-26 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-07-25 | 1989-01-24 | 1989-07-26 | $7700.00 | Window Closed / Lapsed |