US4113729A
Expired / Lapsed
US
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3-Phenoxymorphinans and derivatives thereof
Assignee: Hoffmann La Roche Inc
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Filing: 1977-06-29
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Granted: 1978-09-12
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Expires: 1997-06-29
Abstract
Abstract Levo-rotary 3-phenoxy N-substituted morphinans and derivatives thereof useful as analgesics and/or narcotic antagonists and their preparation form (-)-3-hydroxy-N-lower alkyl morphinan including intermediates in this preparation.
Inventors
- 👤 Ernest Mohacsi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 11:46
CPC Classifications
C; C07; C07D; C07D221/00; C07D221/02; C07D221/22; C07D221/28; C07D217/00; C07D217/12; C07D217/18
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
114 words
A compound of the formula ##STR17## wherein R is halo, lower alkyl, lower alkoxy, hydroxy, nitro or hydrogen; R 1 is hydrogen, lower alkenyl containing from 2 to 7 carbon atoms, --CH 2 --(CH 2 ) p R 2 , and ##STR18## R 2 is phenyl, cyclo-lower alkyl containing from 3 to 6 carbon atoms, or a 5 or 6 membered heteroaromatic ring containing a hetero atom selected from the group consisting of oxygen, nitrogen and sulfur; p is an integer from 0 to 3; and n is an integer from 1 to 5; and the lower alkoxy and lower alkyl substituents contain from 1 to 7 carbon atoms and pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
114 words
A compound of the formula ##STR17## wherein R is halo, lower alkyl, lower alkoxy, hydroxy, nitro or hydrogen; R 1 is hydrogen, lower alkenyl containing from 2 to 7 carbon atoms, --CH 2 --(CH 2 ) p R 2 , and ##STR18## R 2 is phenyl, cyclo-lower alkyl containing from 3 to 6 carbon atoms, or a 5 or 6 membered heteroaromatic ring containing a hetero atom selected from the group consisting of oxygen, nitrogen and sulfur; p is an integer from 0 to 3; and n is an integer from 1 to 5; and the lower alkoxy and lower alkyl substituents contain from 1 to 7 carbon atoms and pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
11 words
The compound of claim 1 wherein R 1 is lower alkyl.
Claim 4
Dependent Claim
10 words
The compound of claim 2 wherein said compound is (-)-3-phenoxy-N-methylmorphinan.
Claim 5
Dependent Claim
9 words
The compound of claim 2 wherein R is halo.
Claim 6
Dependent Claim
10 words
The compound of claim 4 wherein said compound is (-)-3-pentafluorophenoxy-N-methylmorphinan.
Claim 7
Dependent Claim
9 words
The compound of claim 4 wherein said compound is(-)-3-(p-fluoro)phenoxy-N-methylmorphinan.
Claim 8
Dependent Claim
9 words
The compound of claim 2 wherein R is nitro.
Claim 9
Dependent Claim
10 words
The compound of claim 7 wherein said compound is (-)-3-(o-nitro)-phenoxy-N-methyl-morphinan.
Claim 10
Dependent Claim
9 words
The compound of claim 2 wherein R is hydroxy.
Claim 11
Dependent Claim
10 words
The compound of claim 9 wherein said compound is (-)-3-(p-hydroxy)phenoxy-N-methylmorphinan.
Claim 12
Dependent Claim
10 words
The compound of claim 2 wherein R is lower alkoxy.
Claim 13
Dependent Claim
10 words
The compound of claim 11 wherein said compound is (-)-3-(o-methoxy)phenoxy-N-methylmorphinan.
Claim 14
Dependent Claim
18 words
The compound of claim 1 wherein R 1 is --CH 2 --(CH 2 ) p --R 2 .
Claim 15
Dependent Claim
10 words
The compound of claim 13 wherein said compound is (-)-3phenoxy-N-cyclopropylmethylmorphinan.
Claim 16
Dependent Claim
10 words
The compound of claim 13 wherein R 1 is ##STR19##
Claim 17
Dependent Claim
10 words
The compound of claim 13 wherein said compound is (-)-3-phenoxy17-cyclopropylcarbonylmorphinan.
Claim 18
Dependent Claim
27 words
A compound of the formula ##STR20## wherein R is halo, nitro, lower alkyl, lower alkoxy, hydroxy or hydrogen and n is an integer from 1 to 5.
Claim 19
Dependent Claim
27 words
A compound of the formula ##STR20## wherein R is halo, nitro, lower alkyl, lower alkoxy, hydroxy or hydrogen and n is an integer from 1 to 5.
Claim 20
Dependent Claim
10 words
The compound of claim 17 wherein said compound is (-)-3-phenoxyN-trichlorocarbethoxymorphinan.
References Cited (Backward Citations)
DE2030981A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-09-11 | 1982-03-13 | 1982-09-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-09-11 | 1986-03-13 | 1986-09-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-09-11 | 1990-03-13 | 1990-09-12 | $7700.00 | Window Closed / Lapsed |