US4440904A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Nonapeptide anti-secretory agents
Assignee: Wyeth LLC
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Filing: 1983-01-31
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Granted: 1984-04-03
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Expires: 2003-01-31
Abstract
Abstract The nonapeptides ##STR1## in which X 1 is either L- or D- His, Lys or Arg; X 2 is either L- or D- Phe, Tyr, Trp, Leu, Met, His, Glu or Asp; X 3 is Phe, Tyr, Trp, Leu or Met; X 4 is L- or D-Trp; X 5 is Thr, Val or Abu; and, X 6 is either L- or D- Phe, Tyr, Trp, Leu, Met, Ser or Thr; the linear precursor intermediates and pharmaceutically acceptable salts and amides thereof are inhibitors of growth hormone release and are anti-secretory agents which act as H 2 -receptor antagonists.
Inventors
- 👤 Dimitrios Sarantakis
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 20:03
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; Y10S930/26
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
81 words
A compound of the formula: ##STR7## in which X 1 is either L- or D-His, Lys or Arg; X 2 is either L- or D-Phe, Tyr, Trp, Leu, Met, His, Glu or Asp; X 3 is Phe, Tyr, Trp, Leu or Met; X 4 is L- or D-Trp; X 5 is Thr, Val or Abu; and, X 6 is either L- or D-Phe, Tyr, Trp, Leu, Met, Ser or Thr; the linear precursor intermediates thereof, pharmaceutically acceptable salts and amides thereof.
Claim 2
Dependent Claim
81 words
A compound of the formula: ##STR7## in which X 1 is either L- or D-His, Lys or Arg; X 2 is either L- or D-Phe, Tyr, Trp, Leu, Met, His, Glu or Asp; X 3 is Phe, Tyr, Trp, Leu or Met; X 4 is L- or D-Trp; X 5 is Thr, Val or Abu; and, X 6 is either L- or D-Phe, Tyr, Trp, Leu, Met, Ser or Thr; the linear precursor intermediates thereof, pharmaceutically acceptable salts and amides thereof.
Claim 3
Dependent Claim
11 words
The compound of claim 1 which is L-Histidyl-L-tyrosyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-L-cysteinyl-L-phenylalanine cyclic (3-8) disulfide.
Claim 4
Dependent Claim
198 words
A compound of claim 1 of the formula: ##STR8## in which X 1 is either L- or D-His, Lys or Arg; X 2 is either L- or D-Phe, Tyr, Trp, Leu, Met, His, Glu or Asp; X 3 is Phe, Tyr, Trp, Leu or Met; X 4 is L- or D-Trp; X 5 is Thr, Val or Abu; X 6 is either L- or D-Phe, Tyr, Trp, Leu, Met, Ser or Thr; and, R is hydrogen or an alpha amino protecting group; R 1 is hydrogen or an amino protecting group; R 2 is hydrogen, a phenolic hydroxy protecting group for tyrosine, an amino protecting group for histidine or a carboxy protecting group for glutamic or aspartic acid; R 3 is hydrogen or a phenolic hydroxy protecting group; R 5 is hydrogen or a hydroxyl protecting group; R 6 is hydrogen or a hydroxyl protecting group; R 8 is --NHR 10 , in which R 10 is alkyl of 2 to 4 carbon atoms, or --OR 11 , in which R 11 is hydrogen or alkyl of 1 to 6 carbon atoms or --OCH 2 (resin support); R 9 and R 10 are hydrogen or sulfhydryl protecting groups.
Claim 5
Dependent Claim
12 words
The compound which is N.sup.α -tert-Butyloxycarbonyl-N im -benzyloxycarbonyl-L-histidyl-O-2,6-dichloro-benzyl-L-tyrosyl-S-4-methylbenzyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-N.sup.ε -2-chlorobenzyloxycarbonyl-L-lysyl-O-benzyl-L-threonyl-S-4-methylbenzyl-L-cysteinyl-L-phenylalanine hydroxymethyl polystyrene ester.
Claim 6
Dependent Claim
12 words
The compound which is N.sup.α -tert-Butyloxycarbonyl-N im -benzyloxycarbonyl-L-histidyl-O-2,6-dichloro-benzyl-L-tyrosyl-S-4-methylbenzyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-N.sup.ε -2-chlorobenzyloxycarbonyl-L-lysyl-O-benzyl-L-threonyl-S-4-methylbenzyl-L-cysteinyl-L-phenylalanine hydroxymethyl polystyrene ester.
References Cited (Backward Citations)
US4282143A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-04-03 | 1987-10-03 | 1988-04-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-04-03 | 1991-10-03 | 1992-04-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-04-03 | 1995-10-03 | 1996-04-03 | $7700.00 | Window Closed / Lapsed |