Patent US4180501A successfully refreshed from Google Patents.
US4180501A
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Bis (polypeptide) derivatives of enkephalin
Assignee: VETERANS ADMINISTRATION United States, AS REPRESENTED
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Filing: 1978-06-16
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Granted: 1979-12-25
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Expires: 1998-06-16
Abstract
Abstract Bis-(polypeptide) derivatives represented by the formulae: ##STR1## wherein: X is glycine or a chiral residue of a D-amino acid selected from the group consisting of D-alanine, D-leucine, D-isoleucine, D-valine, D-norvaline, D-phenylalanine, D-tyrosine, D-tryptophan, D-serine, D-threonine, D-methionine, D-glutamic acid, D-glutamine, D-aspartic acid, D-asparagine, D-lysine, D-proline, D-histidine and D-arginine; Y a residue of methionine or leucine and Z is selected from the group consisting of hydroxy, amino, loweralkylamine, diloweralkylamino and loweralkoxy; each R 1 is hydrogen or fluorine and the pharmaceutically acceptable salts thereof; intermediates useful in making the novel pentapeptides and pharmaceutical compositions and methods employing them.
Inventors
- 👤 David H. Coy
- 👤 Abba J. Kastin
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 03:24
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/665; C07K14/67; C07K14/672; C07K14/70; C07K14/702; C07K5/00; C07K5/04; C07K5/10; C07K5/1002; C07K5/1016; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/12
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
76 words
A polypeptide of the formulae ##STR4## wherein: X is a chiral residue of a D-amino acid selected from the group consisting of D-alanine, D-leucine, D-isoleucine, D-valine, D-norvaline, D-phenylalanine, D-tyrosine, D-tryptophan, D-serine, D-threonine, D-methionine, D-glutamic acid, D-glutamine, D-aspartic acid, D-asparagine, D-lysine, D-proline, D-histidine and D-arginine; Y is methionine or leucine and Z is selected from the group consisting of hydroxy, amino, loweralkylamino, diloweralkylamino and loweralkoxy; and the pharmaceutically acceptable salts thereof; R 1 is hydrogen or fluorine.
Claim 2
Dependent Claim
76 words
A polypeptide of the formulae ##STR4## wherein: X is a chiral residue of a D-amino acid selected from the group consisting of D-alanine, D-leucine, D-isoleucine, D-valine, D-norvaline, D-phenylalanine, D-tyrosine, D-tryptophan, D-serine, D-threonine, D-methionine, D-glutamic acid, D-glutamine, D-aspartic acid, D-asparagine, D-lysine, D-proline, D-histidine and D-arginine; Y is methionine or leucine and Z is selected from the group consisting of hydroxy, amino, loweralkylamino, diloweralkylamino and loweralkoxy; and the pharmaceutically acceptable salts thereof; R 1 is hydrogen or fluorine.
Claim 3
Dependent Claim
9 words
A compound of claim 1 wherein Y is methionine.
Claim 4
Dependent Claim
9 words
A compound of claim 2 wherein Z is hydroxy.
Claim 5
Dependent Claim
9 words
A compound of claim 2 wherein Z is amino.
Claim 6
Dependent Claim
9 words
A compound of claim 2 wherein Z is loweralkylamino.
Claim 7
Dependent Claim
9 words
A compound of claim 2 wherein Z is diloweralkylamino.
Claim 8
Dependent Claim
9 words
A compound of claim 1 wherein Z is loweralkoxy.
Claim 9
Dependent Claim
14 words
A compound of claim 4: N.sup.α,N.sup.ε -bis(Tyr-D-Ala-Gly-Phe-Met)lysine amide or a pharmaceutically acceptable salt thereof.
Claim 10
Dependent Claim
9 words
A compound of claim 1 wherein Y is leucine.
Claim 11
Dependent Claim
9 words
A compound of claim 9 wherein X is hydroxy.
Claim 12
Dependent Claim
9 words
A compound of claim 10 wherein X is amino.
Claim 13
Dependent Claim
9 words
A compound of claim 10 wherein X is loweralkylamino.
Claim 14
Dependent Claim
9 words
A compound of claim 10 wherein X is diloweralkylamino.
Claim 15
Dependent Claim
9 words
A compound of claim 10 wherein X is loweralkoxy.
Claim 16
Dependent Claim
21 words
A pharmaceutical composition comprising administering an effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier or diluent.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-12-24 | 1983-06-25 | 1983-12-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-12-24 | 1987-06-25 | 1987-12-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-12-24 | 1991-06-25 | 1991-12-25 | $7700.00 | Window Closed / Lapsed |