US4250087A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Carboxyl terminus analogs of β-endorphin
Assignee: University of California Berkeley
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Filing: 1979-12-10
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Granted: 1981-02-10
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Expires: 1999-12-10
Abstract
Abstract Novel carboxyl terminus analogs of beta -endorphin are described. The carboxyl terminus of such analogs is selected from lower alkyl amide, glycine, glycinamide, or polyglycine. These analogs exhibit either greater analgesic activity than the parent beta -endorphin and/or increased binding activity in an opiate binding assay.
Inventors
- 👤 Choh H. Li
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 18:54
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/665; C07K14/675; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
63 words
Analogs of endorphin of the formula H-Tyr-Gly-Gly-Phe-Met.sup.5 -Thr-Ser-B-Lys-Ser.sup.10 -Gln-Thr-Pro-Leu-Val.sup.15 -Thr-Leu-Phe-Lys-Asn.sup.20 -Ala-Ile-X-Lys-Asn.sup.25 -Ala-Y-Lys-Lys-Gly.sup.30 -Q I wherein B is Glu or Gln, X is Ile or Val; Y is His or Tyr and Q is --NH--lower alkyl or (Gly) n --A where n is an integer from 1 to 5 and A is --OH or --NH 2 and the pharmaceutically acceptable acid addition salts thereof.
Claim 2
Dependent Claim
63 words
Analogs of endorphin of the formula H-Tyr-Gly-Gly-Phe-Met.sup.5 -Thr-Ser-B-Lys-Ser.sup.10 -Gln-Thr-Pro-Leu-Val.sup.15 -Thr-Leu-Phe-Lys-Asn.sup.20 -Ala-Ile-X-Lys-Asn.sup.25 -Ala-Y-Lys-Lys-Gly.sup.30 -Q I wherein B is Glu or Gln, X is Ile or Val; Y is His or Tyr and Q is --NH--lower alkyl or (Gly) n --A where n is an integer from 1 to 5 and A is --OH or --NH 2 and the pharmaceutically acceptable acid addition salts thereof.
Claim 3
Dependent Claim
13 words
The compounds of claim 1 wherein X is Ile and Y is Tyr.
Claim 4
Dependent Claim
11 words
The compounds of claim 2 wherein Q is (Gly) n -A.
Claim 5
Dependent Claim
12 words
The compound of claim 3 which is [Gly 31 ]-β h -endorphin.
Claim 6
Dependent Claim
12 words
The compound of claim 3 which is [Gly 31 ]-β h -endorphinamide.
Claim 7
Dependent Claim
13 words
The compound of claim 3 which is [Gly 31 ]-β h -endorphinyl glycine.
Claim 8
Dependent Claim
14 words
The compound of claim 3 which is [Gly 31 ]-β h -EP-Gly-NH 2 .
Claim 9
Dependent Claim
14 words
The compound of claim 3 which is [Gly 31 ]-β h -EP-Gly-Gly-NH 2 .
Claim 10
Dependent Claim
17 words
The compound of claim 3 which is [Gln 8 , Gly 31 ]-β h -EP-Gly-Gly-NH 2 .
Claim 11
Dependent Claim
10 words
The compounds of claim 2 wherein Q is --NH--lower alkyl.
Claim 12
Dependent Claim
21 words
The compound of claim 10 which is [CH 3 (CH 2 ) 4 --NH 2 31 ]-β h -EP-Gly-Gly-NH 2 .
References Cited (Backward Citations)
US4038222A
Cited
US4116950A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-02-10 | 1984-08-11 | 1985-02-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-02-10 | 1988-08-11 | 1989-02-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-02-10 | 1992-08-11 | 1993-02-10 | $7700.00 | Window Closed / Lapsed |