US4451394A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Dodecapeptides preventing glucose and triglyceride assimilation
Assignee: Wyeth LLC
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Filing: 1982-10-25
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Granted: 1984-05-29
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Expires: 2002-10-25
Abstract
Abstract Polypeptides of the formula: ##STR1## where X 1 is either D- or L- Lys, Arg, His or Orn; X 2 is either D- or L- Asn, His, Glu, Asp, Tyr, Trp or Phe; X 3 is either D- or L- Trp; the linear precursor intermediates thereof and pharmaceutically acceptable salts and amides thereof are inhibitors of growth hormone release, active for periods of two hour and more. In addition, the compounds of this invention normalize post-prandial glucose and triglyceride levels in diabetics. The compounds are useful for treatment of patients suffering from diabetes mellitus and excessive growth hormone secretion (acromegaly).
Inventors
- 👤 Dimitrios Sarantakis
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 12:12
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; Y10S930/26
Claims Analysis
Total Claims: 5
Claim 1
Independent Claim
54 words
A compound of the formula: ##STR5## where X 1 is either D- or L- Lys, Arg, His or Orn; X 2 is either D- or L- Asn, His, Glu, Asp, Tyr, Trp or Phe; X 3 is either D- or L- Trp; the linear precursor intermediates thereof and pharmaceutically acceptable salts and amides thereof.
Claim 2
Dependent Claim
54 words
A compound of the formula: ##STR5## where X 1 is either D- or L- Lys, Arg, His or Orn; X 2 is either D- or L- Asn, His, Glu, Asp, Tyr, Trp or Phe; X 3 is either D- or L- Trp; the linear precursor intermediates thereof and pharmaceutically acceptable salts and amides thereof.
Claim 3
Dependent Claim
11 words
The compound of claim 1 which is L-phenylalanyl-L-arginyl-L-glutamyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-L-cysteinyl-L-threonyl-L-seryl-L-phenylalanine cyclic (4-9) disulfide.
Claim 4
Dependent Claim
163 words
The compound of claim 1 which is ##STR6## where X 1 is either D- or L- Lys, Arg, His or Orn; X 2 is either D- or L- Asn, His, Glu, Asp, Tyr, Trp or Phe; X 3 is either D- or L- Trp; and R is hydrogen or an alpha amino protecting group; R 1 is hydrogen or an amino protecting group; R 2 is hydrogen or an imino protecting group for D- or L- His or a phenolic hydroxyl protecting group for D- or L- Tyr; R 3 is hydrogen or an amino protecting group; R 4 , R 5 and R 6 are hydrogen or hydroxy protecting groups; R 7 is --NHR 10 ; in which R 10 is alkyl of 2 to 4 carbon atoms or --OR 10 , in which R 11 is hydrogen or alkyl of 1 to 6 carbon atoms or --OCH 2 (resin support); R 8 and R 9 are hydrogen or sulfhydryl protecting groups.
Claim 5
Dependent Claim
13 words
The compound of claim 1 which is N-tert-Butyloxycarbonyl-L-phenylalanyl-N g -tosyl-L-arginyl-γ-benzyl-L-glutamyl-S-p-methoxybenzyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-N.sup.ε -2-chloro-benzyloxycarbonyl-L-lysyl-O-benzyl-L-threonyl-S-p-methoxybenzyl-L-cysteinyl-O-benzyl-L-threonyl-O-benzyl-L-seryl-L-phenylalanyl-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) | 1987-05-29 | 1987-11-28 | 1988-05-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-05-29 | 1991-11-28 | 1992-05-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-05-29 | 1995-11-28 | 1996-05-29 | $7700.00 | Window Closed / Lapsed |