US4148786A
Expired / Lapsed
US
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Analgesic polypeptide
Assignee: Wyeth LLC
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Filing: 1978-06-26
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Granted: 1979-04-10
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Expires: 1998-06-26
Abstract
Abstract The polypeptides of the formula: ##STR1## in which R 1 is hydrogen, lower alkyl, allyl, 2-isopentenyl, 3-isopentenyl, cyclopropylmethyl, cyclobutylmethyl, phenethyl or arginyl; R 2 is hydrogen or lower alkyl; R 3 is hydrogen or lower alkyl; R 4 is hydrogen, hydroxymethyl, carbo(lower)alkoxy, carbamyl or carboxy; and X is hydrogen, chloro, fluoro, bromo or iodo, the linear precursors thereof or a pharmaceutically acceptable salt thereof, Exert an analgesic effect in warm-blooded animals when peripherally administered.
Inventors
- 👤 Dimitrois Sarantakis
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 04:33
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/665; C07K14/70; C07K14/702; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/28
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
64 words
A polypeptide of the formula: ##STR4## in which R 1 is hydrogen, lower alkyl, allyl, 2-isopentenyl, 3-isopentenyl, cyclopropylmethyl, cyclobutylmethyl, phenethyl or arginyl; R 2 is hydrogen or lower alkyl; R 3 is hydrogen or lower alkyl; R 4 is hydrogen, hydroxymethyl, carbo(lower)alkoxy, carbamyl or carboxy; and X is hydrogen, chloro, fluoro, bromo or iodo; the linear precursors thereof or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
64 words
A polypeptide of the formula: ##STR4## in which R 1 is hydrogen, lower alkyl, allyl, 2-isopentenyl, 3-isopentenyl, cyclopropylmethyl, cyclobutylmethyl, phenethyl or arginyl; R 2 is hydrogen or lower alkyl; R 3 is hydrogen or lower alkyl; R 4 is hydrogen, hydroxymethyl, carbo(lower)alkoxy, carbamyl or carboxy; and X is hydrogen, chloro, fluoro, bromo or iodo; the linear precursors thereof or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
21 words
A compound of claim 1 which is Tyr-D-Cys-Gly-Phe-D-Cys-NH 2 cyclic (2-5) disulfide, its linear precursor or a pharmaceuticaly acceptable salt thereof.
Claim 4
Dependent Claim
21 words
A compound of claim 1 which is Tyr-D-Cys-Gly-Phe-Cys-NH 2 cyclic (2-5) disulfide, its linear precursor or a pharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim
21 words
A compound of claim 1 which is Tyr-D-Cys-Gly-N-methyl-Phe-D-Cys-NH 2 cyclic (2-5) disulfide, its linear precursor or a pharmaceutically acceptable salt thereof.
Claim 6
Dependent Claim
21 words
A compound of claim 1 which is Arg-Tyr-D-Cys-Gly-Phe-D-Cys-NH 2 cyclic (3-6) disulfide, its linear precursor or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
21 words
A compound of claim 1 which is N-methyl-Tyr-D-Cys-Gly-Phe-D-Cys-NH 2 cyclic (2-5) disulfide, its linear precursor or a pharmaceutically acceptable salt thereof.
Claim 8
Dependent Claim
63 words
A compound of the formula: ##STR5## in which R 2 is hydrogen or lower alkyl; R 3 is hydrogen or lower alkyl; X is hydrogen, chloro, bromo, fluoro or iodo; A is hydrogen, an α-amino protecting group or α-amino protected, N-guanyl protected arginyl; F is a phenolic hydroxy protecting group; D is a mercapto protecting group; and E is a mercapto protecting group.
Claim 9
Dependent Claim
63 words
A compound of the formula: ##STR5## in which R 2 is hydrogen or lower alkyl; R 3 is hydrogen or lower alkyl; X is hydrogen, chloro, bromo, fluoro or iodo; A is hydrogen, an α-amino protecting group or α-amino protected, N-guanyl protected arginyl; F is a phenolic hydroxy protecting group; D is a mercapto protecting group; and E is a mercapto protecting group.
Claim 10
Dependent Claim
24 words
A compound of claim 7 in which A is tert-butyloxycarbonyl-(N g -NO 2 )Arg, F is 2,6-dichlorobenzyl, D is p-methoxybenzyl and E is p-methoxybenzyl.
Claim 11
Dependent Claim
20 words
A compound of claim 7 in which A is tert-butyloxycarbonyl, F is 2,6-dichlorobenzyl, D is p-methoxybenzyl and E is p-methoxybenzyl.
References Cited (Backward Citations)
US4028319A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-04-09 | 1982-10-09 | 1983-04-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-04-09 | 1986-10-09 | 1987-04-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-04-09 | 1990-10-09 | 1991-04-10 | $7700.00 | Window Closed / Lapsed |