US4362870A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Selective opioid receptor alkylating agents
Assignee: University of Minnesota System
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Filing: 1981-03-19
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Granted: 1982-12-07
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Expires: 2001-03-19
Abstract
Abstract A selective opioid receptor, site-directed alkylating agent useful as a narcotic antagonist and non-addictive analgesic having the formula: <IMAGE> wherein R is a Michael acceptor, a haloacetamide or isothiocyanate and R' is cyclopropylmethyl, allyl or substituted allyl. The Michael acceptors may be acrylamides or esters: <IMAGE> wherein R2 is alkyl or aralkyl, and salts thereof. The preparation of the compounds is described, along with experiments involving the use of the compounds.
Inventors
- 👤 Philip S. Portoghese
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 10:05
CPC Classifications
C; C07; C07D; C07D489/00; C07D489/06; C07D489/08
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
89 words
A selective opioid receptor alkylating agent having the formula: ##STR15## wherein R is an ester having the general formula: ##STR16## wherein R 2 is (CH 2 ) n H or (CH 2 ) n Ar and n is 1 to 5, wherein Ar is phenyl, furane, naphthyl, thiophene or substituted phenyl, the substituent being halogen, hydroxy, nitro, methoxy, methyl, trifluoromethyl or amino, and R' is selected from the group consisting of cyclopropylmethyl, allyl and substituted allyl, the substituent being methyl, ethyl, propyl or halogen, and pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
89 words
A selective opioid receptor alkylating agent having the formula: ##STR15## wherein R is an ester having the general formula: ##STR16## wherein R 2 is (CH 2 ) n H or (CH 2 ) n Ar and n is 1 to 5, wherein Ar is phenyl, furane, naphthyl, thiophene or substituted phenyl, the substituent being halogen, hydroxy, nitro, methoxy, methyl, trifluoromethyl or amino, and R' is selected from the group consisting of cyclopropylmethyl, allyl and substituted allyl, the substituent being methyl, ethyl, propyl or halogen, and pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
15 words
The alkylating agent of claim 1 wherein R' is cyclopropylmethyl and R 2 is methyl.
Claim 4
Dependent Claim
11 words
The hydrogen chloride salt of the alkylating agent of claim 2.
Claim 5
Dependent Claim
41 words
A selective opioid receptor alkylating agent having the formula: ##STR17## wherein R is isothiocyanate, and R' is selected from the group consisting of cyclopropylmethyl, allyl and substituted allyl, the substituent being methyl, ethyl, propyl or halogen, and pharmaceutically acceptable salts thereof.
Claim 6
Dependent Claim
41 words
A selective opioid receptor alkylating agent having the formula: ##STR17## wherein R is isothiocyanate, and R' is selected from the group consisting of cyclopropylmethyl, allyl and substituted allyl, the substituent being methyl, ethyl, propyl or halogen, and pharmaceutically acceptable salts thereof.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1985-12-06 | 1986-06-07 | 1986-12-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-12-06 | 1990-06-07 | 1990-12-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-12-06 | 1994-06-07 | 1994-12-07 | $7700.00 | Window Closed / Lapsed |