US4185010A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Nonapeptides
Assignee: Wyeth LLC
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Filing: 1978-12-12
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Granted: 1980-01-22
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Expires: 1998-12-12
Abstract
Abstract (des-Ala 1 , Gly 2 , Asn 5 , Thr 12 , Ser 13 )-His 4 -D-Trp 8 -Abu 10 -Somatostatin and analogues thereof selectively inhibit glucagon release without materially altering blood serum growth hormone and insulin levels.
Inventors
- 👤 Dimitrios Sarantakis
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 10:12
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/575; C07K14/655; C07K14/6555; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/16; Y10S930/28
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
62 words
A common of the formula: ##STR3## in which the A groups are hydrogen or a direct bond between the two sulfur atoms; X is hydrogen or Nh 2 ; X 1 is L-Trp or D-Trp; X 2 is L-Abu, L-Val, L-Phe or L-Thr; and the two cysteinyl moieties are of L- or D-configuration, the linear precursor intermediates or pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
62 words
A common of the formula: ##STR3## in which the A groups are hydrogen or a direct bond between the two sulfur atoms; X is hydrogen or Nh 2 ; X 1 is L-Trp or D-Trp; X 2 is L-Abu, L-Val, L-Phe or L-Thr; and the two cysteinyl moieties are of L- or D-configuration, the linear precursor intermediates or pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
17 words
A compound of claim 1 which is L-Cys-LHis-L-Phe-L-Phe-D-Trp-L-Lys-L-Abu-L-Phe-L-Cys cyclic (1-9) disulfide or a pharmaceutically acceptable salt thereof.
Claim 4
Dependent Claim
73 words
A compound of the formula: R-Cys(R.sup.1)-His(R.sup.2)-Phe-Phe-X.sub.1 -Lys-X.sub.2 -Phe-Cys(R.sup.3)-O-CH.sub.2 -polystyrene resin) in which R is an α-amino protecting group; R 1 is a sulfhydryl protecting group; R 2 is amino protecting group; X 1 is L-Trp or D-Trp; X 2 is L-Abu, L-Val, L-Phe or L-Thr(R 4 ) where R 4 is a hydroxyl protecting group; R 3 is a sulfhydryl protecting group; and the two cysteinyl moieties are of L- or D- configuration.
Claim 5
Dependent Claim
73 words
A compound of the formula: R-Cys(R.sup.1)-His(R.sup.2)-Phe-Phe-X.sub.1 -Lys-X.sub.2 -Phe-Cys(R.sup.3)-O-CH.sub.2 -polystyrene resin) in which R is an α-amino protecting group; R 1 is a sulfhydryl protecting group; R 2 is amino protecting group; X 1 is L-Trp or D-Trp; X 2 is L-Abu, L-Val, L-Phe or L-Thr(R 4 ) where R 4 is a hydroxyl protecting group; R 3 is a sulfhydryl protecting group; and the two cysteinyl moieties are of L- or D- configuration.
Claim 6
Dependent Claim
31 words
A compound of claim 3 in which R is t-butyloxycarbonyl; R 1 is p-methoxybenzyl; R 2 is tosyl; X 1 is D-Trp; X 2 is α-aminobutyryl and R 3 is p-methoxybenzyl.
References Cited (Backward Citations)
US4105603A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-01-21 | 1983-07-23 | 1984-01-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-01-21 | 1987-07-23 | 1988-01-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-01-21 | 1991-07-23 | 1992-01-22 | $7700.00 | Window Closed / Lapsed |