US4100117A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Somatostatin analogs and intermediates thereto
Assignee: Eli Lilly and Co
•
Filing: 1977-04-21
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Granted: 1978-07-11
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Expires: 1997-04-21
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 exhibit various activities including inhibition of the release of gastric acid and reduction of gut motility.
Inventors
- 👤 James E. Shields
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 04:40
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: 11
Claim 1
Independent Claim
153 words
A compound selected from those of the formula ##STR8## and its pharmaceutically acceptable non-toxic acid addition salts, and intermediates to said compounds, said intermediates having the formula R-D-Val-Gly-L-Cys(R 1 )-L-Lys(R 2 )-L-Asn-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 ##STR9## in which the resin is polystyrene; with the proviso that, when X is hydroxy, each of R, R 1 , R 2 , R 3 , R 4 , and R 5 is hydrogen, and, when X is ##STR10## each of R, R 1 , R 2 , R 3 , and R 4 is other than hydrogen.
Claim 2
Dependent Claim
153 words
A compound selected from those of the formula ##STR8## and its pharmaceutically acceptable non-toxic acid addition salts, and intermediates to said compounds, said intermediates having the formula R-D-Val-Gly-L-Cys(R 1 )-L-Lys(R 2 )-L-Asn-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 ##STR9## in which the resin is polystyrene; with the proviso that, when X is hydroxy, each of R, R 1 , R 2 , R 3 , R 4 , and R 5 is hydrogen, and, when X is ##STR10## each of R, R 1 , R 2 , R 3 , and R 4 is other than hydrogen.
Claim 3
Dependent Claim
16 words
Compound of claim 1, having the formula ##STR11## and pharmaceutically acceptable non-toxic acid addition salts thereof.
Claim 4
Dependent Claim
22 words
Compound of claim 1, having the formula R-D-Val-Gly-L-Cys(R 1 )-L-Lys(R 2 )-L-Asn-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.
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 X is ##STR12##
Claim 7
Dependent Claim
9 words
Compound of claim 5, in which R is t-butyloxy-carbonyl.
Claim 8
Dependent Claim
10 words
Compound of claim 5, in which R 1 is p-methoxybenzyl.
Claim 9
Dependent Claim
10 words
Compound of claim 5, in which R 2 is o-chloro-benzyloxycarbonyl.
Claim 10
Dependent Claim
13 words
Compound of claim 5, in which R 3 and R 4 are benzyl.
Claim 11
Dependent Claim
8 words
Compound of claim 5, having the formula ##STR13##
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) | 1981-07-10 | 1982-01-09 | 1982-07-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-07-10 | 1986-01-09 | 1986-07-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-07-10 | 1990-01-09 | 1990-07-11 | $7700.00 | Window Closed / Lapsed |