US4062816A
Expired / Lapsed
US
⏱️ 0.0 years remaining
D-Ala5 -somatostatin and intermediates thereto
Assignee: Eli Lilly and Co
•
Filing: 1976-03-11
•
Granted: 1977-12-13
•
Expires: 1996-03-11
Abstract
Abstract The tetradecapeptide ##STR1## is described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptide. This tetradecapeptide as well as its pharmaceutically acceptable acid addition salts inhibit the secretion of gastric acid.
Inventors
- 👤 James E. Shields
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 15:52
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: 10
Claim 1
Independent Claim
148 words
A compound of the formula ##STR9## and its pharmaceutically acceptable non-toxic acid addition salts, and intermediates to said compound, said intermediates having the formula R-L-Ala-Gly-L-Cys(R 1 )-L-Lys(R 2 )-D-Ala-L-Phe-L-Phe-L-Trp(R 5 )-L-Lys(R 2 )-L-Thr(R 3 )-L-Phe-L-Thr(R 3 )-L-Ser(R 4 )-L-Cys(R.sub.1)-X; in which R is hydrogen or an α-amino protecting group; R 1 is hydrogen or a thio protecting group; R 2 is hydrogen or an ε-amino protecting group; R 3 and R 4 each are hydrogen or a hydroxy protecting group; R 5 is hydrogen or formyl; and X is hydroxy or ##STR10## in which the resin is polystyrene; with the proviso that, when X is hydroxy, R, R 1 , R 2 , R 3 , R 4 , and R 5 each are hydrogen, and, when X is ##STR11## R, R 1 , R 2 , R 3 , and R 4 each are other than hydrogen.
Claim 2
Dependent Claim
148 words
A compound of the formula ##STR9## and its pharmaceutically acceptable non-toxic acid addition salts, and intermediates to said compound, said intermediates having the formula R-L-Ala-Gly-L-Cys(R 1 )-L-Lys(R 2 )-D-Ala-L-Phe-L-Phe-L-Trp(R 5 )-L-Lys(R 2 )-L-Thr(R 3 )-L-Phe-L-Thr(R 3 )-L-Ser(R 4 )-L-Cys(R.sub.1)-X; in which R is hydrogen or an α-amino protecting group; R 1 is hydrogen or a thio protecting group; R 2 is hydrogen or an ε-amino protecting group; R 3 and R 4 each are hydrogen or a hydroxy protecting group; R 5 is hydrogen or formyl; and X is hydroxy or ##STR10## in which the resin is polystyrene; with the proviso that, when X is hydroxy, R, R 1 , R 2 , R 3 , R 4 , and R 5 each are hydrogen, and, when X is ##STR11## R, R 1 , R 2 , R 3 , and R 4 each are other than hydrogen.
Claim 3
Dependent Claim
16 words
Compound of claim 1, having the formula ##STR12## and pharmaceutically acceptable non-toxic acid addition salts thereof.
Claim 4
Dependent Claim
24 words
Compound of claim 1, having the formula R-L-Ala-Gly-L-Cys(R 1 )-L-Lys(R 2 )-D-Ala-L-Phe-L-Phe-L-Trp(R 5 )-L-Lys(R 2 )-L-Thr(R 3 )-L-Phe-L-Thr-(R 3 )-L-Ser(R 4 )-L-Cys(R 1 )-X.
Claim 5
Dependent Claim
9 words
Compound of claim 3, in which X is hydroxy.
Claim 6
Dependent Claim
9 words
Compound of claim 3, in which R is t-butyloxycarbonyl.
Claim 7
Dependent Claim
10 words
Compound of claim 3, in which R 1 is p-methoxybenzyl.
Claim 8
Dependent Claim
10 words
Compound of claim 3, in which R 2 is cyclopentyloxycarbonyl.
Claim 9
Dependent Claim
13 words
Compound of claim 3, in which R 3 and R 4 are benzyl.
Claim 10
Dependent Claim
8 words
Compound of claim 3, having the formula ##STR13##
References Cited (Backward Citations)
US3933784A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-12-12 | 1981-06-13 | 1981-12-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-12-12 | 1985-06-13 | 1985-12-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-12-12 | 1989-06-13 | 1989-12-13 | $7700.00 | Window Closed / Lapsed |