US4485039A
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Synthetic analogues of α-melanotropin
Assignee: University Patents Inc
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Filing: 1982-06-11
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Granted: 1984-11-27
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Expires: 2002-06-11
Abstract
Abstract Cyclic analogues of the tridecapeptide hormone, α-melanotropin. (α-melanocyte stimulating hormone, α-MSH), wherein a physiologically stable intramolecular interaction exists (1) between the amino acid residue at position 4 and an amino acid residue at position 10 or 11, and/or (2) between the amino acid residue at position 5 and an amino acid residue at position 10 or 11. Preferred analogues, e.g., [half-Cys 4 , half-Cys 10 ]-α-MSH display greatly increased in vitro potency, prolongation, and resistance to enzymatic degradation.
Inventors
- 👤 Victor J. Hruby
- 👤 Mac E. Hadley
- 👤 Tomi K. Sawyer
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 13:42
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/665; C07K14/695; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/29
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
51 words
Cyclic α-melanotropin stimulating hormone analogues wherein a physiologically stable intramolecular interaction exists (1) between the amino acid residue at position 4 and an amino acid residue at position 10 or 11, and/or (2) between the amino acid residue at position 5 and an amino acid residue at position 10 or 11.
Claim 2
Dependent Claim
51 words
Cyclic α-melanotropin stimulating hormone analogues wherein a physiologically stable intramolecular interaction exists (1) between the amino acid residue at position 4 and an amino acid residue at position 10 or 11, and/or (2) between the amino acid residue at position 5 and an amino acid residue at position 10 or 11.
Claim 3
Dependent Claim
17 words
Cyclic analogues according to claim 1 wherein a physiologically stable intramolecular interaction present is a covalent bond.
Claim 4
Dependent Claim
14 words
Cyclic analogues according to claim 2 wherein the covalent bond is a disulfide bond.
Claim 5
Dependent Claim
14 words
Cyclic analogues according to claim 2 wherein the covalent bond is a carba bond.
Claim 6
Dependent Claim
14 words
Cyclic analogues according to claim 2 wherein the covalent bond is a dicarba bond.
Claim 7
Dependent Claim
111 words
Cyclic α-melanotropin stimulating hormones of the formula: [half-Cys 4 , half-Cys 10 ]-α-MSH acetyl-[half-Cys 4 , half-Cys 10 ]-α-MSH 4-13NH .sbsb.2 [half-Cys 4 , half-Cys 11 ]-α-MSH acetyl-[half-Cys 4 , half-Cys 11 ]-α-MSH 4-13NH .sbsb.2 [half-Cys 5 , half-Cys 10 ]-α-MSH acetyl-[half-Cys 5 , half-Cys 10 ]-α-MSH 5-13NH .sbsb.2 [half-Cys 5 , half-Cys 11 ]-α-MSH acetyl-[half-Cys 5 , half-Cys 11 ]-α-MSH 5-13NH .sbsb.2 [half-Cys 4 , half-Cys 10 ][half-Cys 5 , half-Cys 11 ]-α-MSH acetyl-[half-Cys 4 , half-Cys 10 ][half-Cys 5 , half-Cys 11 ]-α-MSH 4-13NH .sbsb.2 [half-Cys 4 , half-Cys 11 ][half-Cys 5 , half-Cys 10 ]-α-MSH acetyl-[half-Cys 4 , half-Cys 11 ][half-Cys 5 , half-Cys 10 ]-α-MSH 4-13NH .sbsb.2.
Claim 8
Dependent Claim
111 words
Cyclic α-melanotropin stimulating hormones of the formula: [half-Cys 4 , half-Cys 10 ]-α-MSH acetyl-[half-Cys 4 , half-Cys 10 ]-α-MSH 4-13NH .sbsb.2 [half-Cys 4 , half-Cys 11 ]-α-MSH acetyl-[half-Cys 4 , half-Cys 11 ]-α-MSH 4-13NH .sbsb.2 [half-Cys 5 , half-Cys 10 ]-α-MSH acetyl-[half-Cys 5 , half-Cys 10 ]-α-MSH 5-13NH .sbsb.2 [half-Cys 5 , half-Cys 11 ]-α-MSH acetyl-[half-Cys 5 , half-Cys 11 ]-α-MSH 5-13NH .sbsb.2 [half-Cys 4 , half-Cys 10 ][half-Cys 5 , half-Cys 11 ]-α-MSH acetyl-[half-Cys 4 , half-Cys 10 ][half-Cys 5 , half-Cys 11 ]-α-MSH 4-13NH .sbsb.2 [half-Cys 4 , half-Cys 11 ][half-Cys 5 , half-Cys 10 ]-α-MSH acetyl-[half-Cys 4 , half-Cys 11 ][half-Cys 5 , half-Cys 10 ]-α-MSH 4-13NH .sbsb.2.
Claim 9
Dependent Claim
55 words
Cyclic α-melanotropin stimulating hormones of the formula: [half-Cys 4 , carba-half-Cys 10 ]-α-MSH [half-Cys 4 , carba-half-Cys 11 ]-α-MSH [half-Cys 5 , carba-half-Cys 10 ]-α-MSH [half-Cys 5 , carba-half-Cys 11 ]-α-MSH [carba-half-Cys 4 , half-Cys 10 ]-α-MSH [carba-half-Cys 4 , half-Cys 11 ]-α-MSH [carba-half-Cys 5 , half-Cys 10 ]-α-MSH [carba-half-Cys 5 , half-Cys 11 ]-α-MSH.
Claim 10
Dependent Claim
55 words
Cyclic α-melanotropin stimulating hormones of the formula: [half-Cys 4 , carba-half-Cys 10 ]-α-MSH [half-Cys 4 , carba-half-Cys 11 ]-α-MSH [half-Cys 5 , carba-half-Cys 10 ]-α-MSH [half-Cys 5 , carba-half-Cys 11 ]-α-MSH [carba-half-Cys 4 , half-Cys 10 ]-α-MSH [carba-half-Cys 4 , half-Cys 11 ]-α-MSH [carba-half-Cys 5 , half-Cys 10 ]-α-MSH [carba-half-Cys 5 , half-Cys 11 ]-α-MSH.
Claim 11
Dependent Claim
53 words
Cyclic analogues according to claim 5, namely [carba-half-Cys 4 , carba-half-Cys 10 ]-α-MSH [carba-half-Cys 4 , carba-half-Cys 11 ]-α-MSH [carba-half-Cys 5 , carba-half-Cys 10 ]-α-MSH [carba-half-Cys 5 , carba-half-Cys 11 ]-α-MSH [carba-half-Cys 4 , carba-half-Cys 10 ][carba-half-Cys 5 , carba-half-Cys 11 ]-α-MSH [carba-half-Cys 4 , carba-half-Cys 11 ][carba-half-Cys 5 , carba-half-Cys 10 ]-α-MSH.
References Cited (Backward Citations)
No citation records indexed.
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