US4496521A
Expired / Lapsed
US
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Insulin-potentiating peptides
Assignee: Whittier Institute for Diabetes and Endocrinology
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Filing: 1983-07-15
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Granted: 1985-01-29
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Expires: 2003-07-15
Abstract
Abstract hGH(1-43) having the formula: H--Phe--Pro--Thr--Ile--Pro--Leu--Ser--Arg--Leu--Phe--Asp--Asn--Ala--Met--Leu--Arg--Ala--His--Arg--Leu--His--Gln--Leu--Ala--Phe--Asp--Thr--Try--Gln--Glu--Phe--Glu--Glu--Ala--Try--Ile--Pro--Lys--Glu--Gln--Lys--Tyr--Ser--OH has been found to have remarkable insulin-potentiating action, as has the fragment hGH (17-43). Pharmaceutical compositions in accordance with the invention include hGH(1-43), hGH(17-43) or a biologically active intermediate fragment, or a nontoxic salt thereof, dispersed in a pharmaceutically acceptable carrier. Such peptides or pharmaceutically acceptable salts thereof may be administered to mammals to promote the action of insulin. Such a peptide can be synthesized by exclusively solid-phase techniques, by partial solid-phase techniques, by fragment condensation, by classical solution addition or by recently developed recombinant DNA techniques.
Inventors
- 👤 U. James Lewis
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 14:17
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/575; C07K14/61; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/12
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
39 words
A composition of matter in the form of a synthetic peptide having the formula: H--Phe--Pro--Thr--Ile--Pro--Leu--Ser--Arg--Leu--Phe--Asp--Asn--Ala--Met--Leu--Arg--Ala--His--Arg--Leu--His--Gln--Leu--Ala--Phe--Asp--Thr--Tyr--Gln--Glu--Phe--Glu--Glu--Ala--Tyr--Ile--Pro--Lys--Glu--Gln--Lys--Tyr--Ser--OH wherein one or more residues can be deleted beginning at the N-terminus and extending through Arg in the 16-position, or a nontoxic salt thereof.
Claim 2
Dependent Claim
39 words
A composition of matter in the form of a synthetic peptide having the formula: H--Phe--Pro--Thr--Ile--Pro--Leu--Ser--Arg--Leu--Phe--Asp--Asn--Ala--Met--Leu--Arg--Ala--His--Arg--Leu--His--Gln--Leu--Ala--Phe--Asp--Thr--Tyr--Gln--Glu--Phe--Glu--Glu--Ala--Tyr--Ile--Pro--Lys--Glu--Gln--Lys--Tyr--Ser--OH wherein one or more residues can be deleted beginning at the N-terminus and extending through Arg in the 16-position, or a nontoxic salt thereof.
Claim 3
Dependent Claim
11 words
A composition in accordance with claim 1 having the formula: H--Phe--Pro--Thr--Ile--Pro--Leu--Ser--Arg--Leu--Phe--Asp--Asn--Ala--Met--Leu--Arg--Ala--His--Arg--Leu--His--Gln--Leu--Ala--Phe--Asp--Thr--Tyr--Gln--Glu--Phe--Glu--Glu--Ala--Tyr--Ile--Pro--Lys--Glu--Gln--Lys--Tyr--Ser--OH.
Claim 4
Dependent Claim
11 words
A composition in accordance with claim 1 having the formula: H--Ala--His--Arg--Leu--His--Gln--Leu--Ala--Phe--Asp--Thr--Tyr--Gln--Glu--Phe--Glu--Glu--Ala--Tyr--Ile--Pro--Lys--Glu--Gln--Lys--Tyr--Ser--OH.
Claim 5
Dependent Claim
54 words
A pharmaceutical composition for potentiating the action of insulin in mammals which composition comprises an effective amount of a peptide having the formula: H--Phe--Pro--Thr--Ile--Pro--Leu--Ser--Arg--Leu--Phe--Asp--Asn--Ala--Met--Leu--Arg--Ala--His--Arg--Leu--His--Gln--Leu--Ala--Phe--Asp--Thr--Tyr--Gln--Glu--Phe--Glu--Glu--Ala--Tyr--Ile--Pro--Lys--Glu--Gln--Lys--Tyr--Ser--OH wherein one or more residues can be deleted beginning at the N-terminus and extending through Arg in the 16-position, or a nontoxic salt thereof; and a pharmaceutically acceptable carrier therefor.
Claim 6
Dependent Claim
54 words
A pharmaceutical composition for potentiating the action of insulin in mammals which composition comprises an effective amount of a peptide having the formula: H--Phe--Pro--Thr--Ile--Pro--Leu--Ser--Arg--Leu--Phe--Asp--Asn--Ala--Met--Leu--Arg--Ala--His--Arg--Leu--His--Gln--Leu--Ala--Phe--Asp--Thr--Tyr--Gln--Glu--Phe--Glu--Glu--Ala--Tyr--Ile--Pro--Lys--Glu--Gln--Lys--Tyr--Ser--OH wherein one or more residues can be deleted beginning at the N-terminus and extending through Arg in the 16-position, or a nontoxic salt thereof; and a pharmaceutically acceptable carrier therefor.
Claim 7
Dependent Claim
16 words
A pharmaceutical composition in accordance with claim 4 in combination with an effective amount of insulin.
Claim 8
Dependent Claim
14 words
A composition in accordance with claim 4 wherein said peptide has the formula: H--Phe--Pro--Thr--Ile--Pro--Leu--Ser--Arg--Leu--Phe--Asp--Asn--Ala--Met--Leu--Arg--Ala--His--Arg--Leu--His--Gln--Leu--Ala--Phe--Asp--Thr--Tyr--Gln--Glu--Phe--Glu--Glu--Ala--Tyr--Ile--Pro--Lys--Glu--Gln--Lys--Tyr--Ser--OH.
Claim 9
Dependent Claim
14 words
A composition in accordance with claim 4 wherein said peptide has the formula: H--Ala--His--Arg--Leu--His--Gln--Leu--Ala--Phe--Asp--Thr--Tyr--Gln--Glu--Phe--Glu--Glu--Ala--Tyr--Ile--Pro--Lys--Glu--Gln--Lys--Tyr--Ser--OH.
Claim 10
Independent Claim
68 words
A method for controlling the oxidation of sugar in mammals and the storage of sugar in the form of glycogen, which method comprises administering to said mammal an effective amount of a peptide having the formula: H--Phe--Pro--Thr--Ile--Pro--Leu--Ser--Arg--Leu--Phe--Asp--Asn--Ala--Met--Leu--Arg--Ala--His--Arg--Leu--His--Gln--Leu--Ala--Phe--Asp--Thr--Tyr--Gln--Glu--Phe--Glu--Glu--Ala--Tyr--Ile--Pro--Lys--Glu--Gln--Lys--Tyr--Ser--OH wherein one or more residues can be deleted beginning at the N-terminus and extending through Arg in the 16-position or a biologically active N-terminal fragment thereof, or a nontoxic salt thereof.
Claim 11
Independent Claim
68 words
A method for controlling the oxidation of sugar in mammals and the storage of sugar in the form of glycogen, which method comprises administering to said mammal an effective amount of a peptide having the formula: H--Phe--Pro--Thr--Ile--Pro--Leu--Ser--Arg--Leu--Phe--Asp--Asn--Ala--Met--Leu--Arg--Ala--His--Arg--Leu--His--Gln--Leu--Ala--Phe--Asp--Thr--Tyr--Gln--Glu--Phe--Glu--Glu--Ala--Tyr--Ile--Pro--Lys--Glu--Gln--Lys--Tyr--Ser--OH wherein one or more residues can be deleted beginning at the N-terminus and extending through Arg in the 16-position or a biologically active N-terminal fragment thereof, or a nontoxic salt thereof.
Claim 12
Dependent Claim
14 words
The method in accordance with claim 8 wherein the peptide has the formula: H--Phe--Pro--Thr--Ile--Pro--Leu--Ser--Arg--Leu--Phe--Asp--Asn--Ala--Met--Leu--Arg--Ala--His--Arg--Leu--His--Gln--Leu--Ala--Phe--Asp--Thr--Tyr--Gln--Glu--Phe--Glu--Glu--Ala--Tyr--Ile--Pro--Lys--Glu--Gln--Lys--Tyr--Ser--OH.
Claim 13
Dependent Claim
14 words
The method in accordance with claim 8 wherein the peptide has the formula: H--Ala--His--Arg--Leu--His--Gln--Leu--Ala--Phe--Asp--Thr--Try--Gln--Glu--Phe--Glu--Glu--Ala--Tyr--Ile--Pro--Lys--Glu--Gln--Lys--Tyr--Ser--OH.
Claim 14
Dependent Claim
18 words
The method in accordance with claim 8 wherein said administering is carried out intravenously, subcutaneously, percutaneously or intramuscularly.
Claim 15
Dependent Claim
24 words
The method of claim 11 wherein said administration is at a level between about 1 and about 200 micrograms per kilogram of body weight.
Claim 16
Dependent Claim
24 words
The method in accordance with claim 11 wherein said administration is carried out in combination with the administration of an effective amount of insulin.
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) | 1988-01-29 | 1988-07-30 | 1989-01-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-01-29 | 1992-07-30 | 1993-01-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-01-29 | 1996-07-30 | 1997-01-29 | $7700.00 | Window Closed / Lapsed |