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Patent US4492651A successfully refreshed from Google Patents.
US4492651A
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Cyclic hexapeptides
Assignee: Wyeth LLC
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Filing: 1983-11-23
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Granted: 1985-01-08
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Expires: 2003-11-23
Abstract
Abstract Cyclic hexapeptides of the formula: ##STR1## in which X 1 is Thr, Val or Abu; X 2 is Phe, Trp or Tyr; n is one of the integers 2, 3 or 4; m is one of the integers 1, 2, 3 or 4; R 1 is hydrogen or a hydroxyl protecting group for Thr; R 2 is hydrogen or a hydroxyl protecting group for Tyr; R 3 is hydrogen or a N.sup.ε protecting group for Lys; R 4 is hydrogen, alkanoyl, aroyl or an amino protecting group; or pharmaceutically acceptable salts thereof, are inhibitors of growth hormone secretion useful in the treatment of acromegaly and diabetes.
Inventors
- 👤 Dimitrios Sarantakis
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 04:45
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/575; C07K14/655; C07K14/6555; A; A61; A61K; A61K38/00; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/16; Y10S930/27
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
105 words
A compound of the formula: ##STR6## in which X 1 is Thr, Val or Abu; X 2 is Phe, Trp or Tyr; n is one of the integers 2, 3 or 4; m is one of the integers 1, 2, 3 or 4; R 1 is hydrogen or a hydroxyl protecting group for Thr; R 2 is hydrogen or a hydroxyl protecting group for Tyr; R 3 is hydrogen or a N.sup.ε protecting group for Lys; R 4 is hydrogen, alkanoyl of 2 to 6 carbon atoms, aroyl of 7 to 10 carbon atoms or an amino protecting group, or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
105 words
A compound of the formula: ##STR6## in which X 1 is Thr, Val or Abu; X 2 is Phe, Trp or Tyr; n is one of the integers 2, 3 or 4; m is one of the integers 1, 2, 3 or 4; R 1 is hydrogen or a hydroxyl protecting group for Thr; R 2 is hydrogen or a hydroxyl protecting group for Tyr; R 3 is hydrogen or a N.sup.ε protecting group for Lys; R 4 is hydrogen, alkanoyl of 2 to 6 carbon atoms, aroyl of 7 to 10 carbon atoms or an amino protecting group, or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
8 words
The compound of claim 1 which is cyclo(D-tryptophyl-L-lysyl-L-threonyl-L-phenylalanyl-D,L-2-piperazinocarboxyl-L-phenylalanyl).
Claim 4
Dependent Claim
113 words
A compound of the formula ##STR7## in which X 1 is Thr, Val or Abu; X 2 is Phe, Trp or Tyr; n is one of the integers 2, 3 or 4; m is one of the integers 1, 2, 3 or 4; R is hydrogen or an α-amino protecting group; R 1 is a hydroxyl protecting group for Thr; R 2 is a hydroxyl protecting group for Tyr; R 3 is an N.sup.ε protecting group for Lys; R 4 is alkanoyl of 2 to 6 carbon atoms, aroyl of 7 to 10 carbon atoms or an amino protecting group; and R 5 is --NHNH 2 or the residue of an oxypolystyrene resin.
Claim 5
Dependent Claim
113 words
A compound of the formula ##STR7## in which X 1 is Thr, Val or Abu; X 2 is Phe, Trp or Tyr; n is one of the integers 2, 3 or 4; m is one of the integers 1, 2, 3 or 4; R is hydrogen or an α-amino protecting group; R 1 is a hydroxyl protecting group for Thr; R 2 is a hydroxyl protecting group for Tyr; R 3 is an N.sup.ε protecting group for Lys; R 4 is alkanoyl of 2 to 6 carbon atoms, aroyl of 7 to 10 carbon atoms or an amino protecting group; and R 5 is --NHNH 2 or the residue of an oxypolystyrene resin.
Claim 6
Dependent Claim
11 words
The compound of claim 3 which is tert-butyloxycarbonyl-D-tryptophyl-N-2-chlorobenzyloxycarbonyl-L-lysyl-O-benzyl-L-threonyl-L-phenylalanyl-DL-4-benzyloxycarbonyl-2-piperazinocarboxyl-L-phenylalanine hydroxymethyl polystyrene ester.
Claim 7
Dependent Claim
10 words
The compound of claim 3 which is D-tryptophyl-N 2-chlorobenzyloxycarbonyl-L-lysyl-O-benzyl-L-threonyl-L-phenylalanyl-4-benzyloxy-carbonyl-2-piperazinocarboxyl-L-phenylalanyl hydrazide.
References Cited (Backward Citations)
US4089958A
Cited
US4427661A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-01-08 | 1988-07-09 | 1989-01-08 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-01-08 | 1992-07-09 | 1993-01-08 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-01-08 | 1996-07-09 | 1997-01-08 | $7700.00 | Window Closed / Lapsed |