US4608376A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Opiate agonists and antagonists
Assignee: Memorial Sloan Kettering Cancer Center
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Filing: 1982-09-30
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Granted: 1986-08-26
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Expires: 2002-09-30
Abstract
Abstract Dihydromorphinone compound of the general formula HDM=N-R wherein HDM is <IMAGE> where * indicates binding carbon R1 is an optionally substituted alkyl, alkylene, cycloalkyl, or cycloalkylene R2 is OH or H R3 is OH or OCH3 and R is N=R4, N-R4, <IMAGE> R4 is an optionally substituted alkyl, alkylene, cycloalkyl, cycloalkylene, aryl, heterocycloalkyl, heterocycloalkylene, or alkenyl, and n is 1-10, and use thereof as an opiate receptor blocker.
Inventors
- 👤 Gavril W. Pasternak
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 10:22
CPC Classifications
C; C07; C07D; C07D489/00; C07D489/06; C07D489/08
Claims Analysis
Total Claims: 5
Claim 1
Independent Claim
89 words
Dihydromorphinone compound of the general formula HDM═N--R wherein ##STR10## R1 is alkyl with 1 to 10 carbon atoms or alkenyl of 2 to 10 carbon atoms, R2 is OH or H, R3 is OH, ##STR11## R4 is HDM, alkenylidene with 2 to 10 carbon atoms, or cycloalkenylidene of up to 6 carbon atoms, R5 is phenyl, alkyl of 1 to 4 carbon atoms, alkenyl with 2 to 10 carbon atoms, cycloalkyl of up to 6 carbon atoms, or cycloalkenyl of up to 6 carbon atoms and n is 1-10.
Claim 2
Dependent Claim
89 words
Dihydromorphinone compound of the general formula HDM═N--R wherein ##STR10## R1 is alkyl with 1 to 10 carbon atoms or alkenyl of 2 to 10 carbon atoms, R2 is OH or H, R3 is OH, ##STR11## R4 is HDM, alkenylidene with 2 to 10 carbon atoms, or cycloalkenylidene of up to 6 carbon atoms, R5 is phenyl, alkyl of 1 to 4 carbon atoms, alkenyl with 2 to 10 carbon atoms, cycloalkyl of up to 6 carbon atoms, or cycloalkenyl of up to 6 carbon atoms and n is 1-10.
Claim 3
Dependent Claim
117 words
Method of controlling appetite comprising selectively and/or irreversibly blocking the mu1 opiate receptors by administering an effective amount of a dihydromorphinone compound of the formula HDM═N--R wherein ##STR12## wherein * indicates binding carbon R1 is alkyl with 1 to 10 carbon atoms or alkenyl of 2 to 10 carbon atoms, R2 is OH or H R3 is OH or OCH 3 and ##STR13## R4 is HDM, alkenylidene with 2 to 10 carbon atoms, or cycloalkenylidene of up to 6 carbon atoms, R5 is phenyl, alkyl of 1 to 4 carbon atoms, alkenyl with 2 to 10 carbon atoms, cycloalkyl of up to 6 carbon atoms, or cycloalkenyl of up to 6 carbon atoms and n is 1-10.
Claim 4
Dependent Claim
117 words
Method of controlling appetite comprising selectively and/or irreversibly blocking the mu1 opiate receptors by administering an effective amount of a dihydromorphinone compound of the formula HDM═N--R wherein ##STR12## wherein * indicates binding carbon R1 is alkyl with 1 to 10 carbon atoms or alkenyl of 2 to 10 carbon atoms, R2 is OH or H R3 is OH or OCH 3 and ##STR13## R4 is HDM, alkenylidene with 2 to 10 carbon atoms, or cycloalkenylidene of up to 6 carbon atoms, R5 is phenyl, alkyl of 1 to 4 carbon atoms, alkenyl with 2 to 10 carbon atoms, cycloalkyl of up to 6 carbon atoms, or cycloalkenyl of up to 6 carbon atoms and n is 1-10.
Claim 5
Dependent Claim
19 words
Method of reducing opiate dependency in an addict comprising administering an effective amount of the compound of claim 1.
References Cited (Backward Citations)
US2797221A
Cited
US4362870A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1989-08-25 | 1990-02-24 | 1990-08-26 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-08-25 | 1994-02-24 | 1994-08-26 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-08-25 | 1998-02-24 | 1998-08-26 | $7700.00 | Window Closed / Lapsed |