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US4866038A
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Method of stimulating integumental melanocytes by topical application of analogs of alpha-msh
Assignee: University Patents Inc
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Filing: 1988-07-22
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Granted: 1989-09-12
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Expires: 2008-07-22
Abstract
Abstract A method for stimulating integumental melanocytes by the topical application of alpha-MSH analogs, and compositions comprising said analogs for use in the method are described.
Inventors
- 👤 Victor J. Hruby
- 👤 Mac E. Hadley
- 👤 Robert Dorr
- 👤 Norman Levine
- 👤 Elizabeth Sugg
- 👤 Wayne L. Cody
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 23:19
CPC Classifications
A; A61; A61K; A61K38/00; A61Q; A61Q19/00; A61Q19/04; A61K38/16; A61K38/17; A61K38/33; A61K38/34; A61K8/00; A61K8/18; A61K8/30; A61K8/64; A61P; A61P17/00; A61P43/00
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
206 words
A method of stimulating melanin production in a vertebrate which comprises administering to said vertebrate in an amount sufficient to cause stimulation of melanocytes a compound of the group: (1) alpha-MSH having the amino acid formula: Ac--Ser--Tyr--Ser--Met--Glu--His--Phe--Arg--Trp--Gly--Lys--Pro--Val--NH.sub.2 ; (2) Alpha-MSH analogues having the formula: Ac--Ser--Tyr--Ser--M--Glu--His--D--Phe--Arg--Trp--Gly--Lys--ProVal--NH.sub.2 wherein M is selected from the group consisting of Met, Nle, and Cys; (3) analogues of alpha-MSH having the formula: R 1 --W--X--Y--Z--R 2 wherein R 1 is selected from the group consisting of Ac--Gly, Ac--Met--Glu, Ac--Nle--Glu and Ac--Tyr--Glu; wherein W is selected from the group consisting of His, and D--His; wherein X is selected from the group consisting of Phe, D--Phe, Tyr, D--Tyr, and (pNO 2 )D--Phe; wherein Y is selected from the group consisting of Arg and D--Arg; wherein Z is selected from the group consisting of Trp and D--Trp; and wherein R 2 is selected from the group consisting of NH 2 , Gly--NH 2 , and Gly--Lys--NH 2 ; and (4) alpha-MSH analogues selected from the group consisting of [Nle 4 , D--Phe 7 ]--alpha--MSH [Nle 4 , D--Phe 7 ]--alpha--MSH 4-10 [Nle 4 , D--Phe 7 ]--alpha MSH 4-11 [Nle 4 , D--Phe 7 , D--Trp 9 ]--alpha--MSH 4-11 [Nle 4 , D--Phe 7 ]--alpha--MSH 4-9
Claim 2
Independent Claim
206 words
A method of stimulating melanin production in a vertebrate which comprises administering to said vertebrate in an amount sufficient to cause stimulation of melanocytes a compound of the group: (1) alpha-MSH having the amino acid formula: Ac--Ser--Tyr--Ser--Met--Glu--His--Phe--Arg--Trp--Gly--Lys--Pro--Val--NH.sub.2 ; (2) Alpha-MSH analogues having the formula: Ac--Ser--Tyr--Ser--M--Glu--His--D--Phe--Arg--Trp--Gly--Lys--ProVal--NH.sub.2 wherein M is selected from the group consisting of Met, Nle, and Cys; (3) analogues of alpha-MSH having the formula: R 1 --W--X--Y--Z--R 2 wherein R 1 is selected from the group consisting of Ac--Gly, Ac--Met--Glu, Ac--Nle--Glu and Ac--Tyr--Glu; wherein W is selected from the group consisting of His, and D--His; wherein X is selected from the group consisting of Phe, D--Phe, Tyr, D--Tyr, and (pNO 2 )D--Phe; wherein Y is selected from the group consisting of Arg and D--Arg; wherein Z is selected from the group consisting of Trp and D--Trp; and wherein R 2 is selected from the group consisting of NH 2 , Gly--NH 2 , and Gly--Lys--NH 2 ; and (4) alpha-MSH analogues selected from the group consisting of [Nle 4 , D--Phe 7 ]--alpha--MSH [Nle 4 , D--Phe 7 ]--alpha--MSH 4-10 [Nle 4 , D--Phe 7 ]--alpha MSH 4-11 [Nle 4 , D--Phe 7 , D--Trp 9 ]--alpha--MSH 4-11 [Nle 4 , D--Phe 7 ]--alpha--MSH 4-9
Claim 3
Dependent Claim
15 words
The method of claim 1 wherein the compound is [Nle 4 , D--Phe 7 ]--alpha--MSH.
Claim 4
Dependent Claim
17 words
The method of claim 1 wherein the compound is [Nle 4 , D--Phe 7 ]--alpha--MSH 4-10 .
Claim 5
Dependent Claim
17 words
The method of claim 1 wherein the compound is [Nle 4 , D--Phe 7 ]--alpha--MSH 4-11 .
Claim 6
Dependent Claim
20 words
The method of claim 1 wherein the compound is [Nle 4 , D--Phe 7 , D--Trp 9 ]--alpha--MSH 4-11 .
Claim 7
Dependent Claim
17 words
The method of claim 1 wherein the compound is [Nle 4 , D--Phe 7 ]--alpha--MSH 4-9 .
Claim 8
Dependent Claim
11 words
The method of claim 1 wherein the compound is Ac--Ser--Tyr--Ser--Met--Glu--His--Phe--Arg--Trp--Gly--Lys--Pro--Val--NH.sub.2 ;
Claim 9
Dependent Claim
11 words
The method of claim 1 wherein the compound is Ac--Ser--Tyr--Ser--Cys--Glu--His--D--Phe--Arg--Trp--Gly--Lys--Pro--Val--NH 2
Claim 10
Dependent Claim
18 words
A method of claim 1 wherein the compound is an analogue of alpha-MSH in which X is D-Phe.
Claim 11
Dependent Claim
19 words
A method of claim 1 wherein the compound is an analogue of alpha-MSH in which R 1 is Ac--Nle--Glu.
Claim 12
Dependent Claim
23 words
A method of claim 1 wherein the compound is an analogue of alpha-MSH is which R 1 is Ac--Nle--Glue, and X is D--Phe.
Claim 13
Independent Claim
207 words
A method for the stimulation of integumental melanocytes in a vertebrate which comprises administrating topically to the epidermal tissue of said vertebrate in an amount sufficient to cause stimulation, a compound of the group: (1) alpha-MSH having the amino acid formula: Ac--Ser--Tyr--Ser--Met--Glu--His--Phe--Arg--Trp--Gly--Lys--Pro--Val--NH.sub.2 ; (2) alpha--MSH analogues having the formula: Ac--Ser--Tyr--Ser--M--Glu--His--D--Phe--Arg--Trp--Gly--Lys--Pro--Val--NH.sub.2 wherein M is selected from the group consisting of Met, Nle and Cys; (3) analogues of alpha--MSH having the formula: R 1 --W--X--Y--Z--R 2 wherein R 1 is selected from the group consisting of Ac--Gly, Ac--Met--Glu,Ac--Nle--Glu, and Ac--Tyr--Glu' wherein W is selected from the group consisting of His and D--His; wherein X is selected from the group consisting of Phe, D--Phe--Tyr, D--Tyr, and (pNO 2 )D--Phe; wherein Y is selected from the group consisting of Arg and D--Arg; wherein Z is selected from the group consisting of Trp and D--Trp; and wherein R 2 is selected from the group consisting of NH 2 , Gly--N 2 and Gly--Lys--NH 2 ; and (4) alpha--MSH analogues selected from the group consisting of [Nle 4 , D--Phe 7 ]--alpha--MSH [Nle 4 , D--Phe 7 ]--alpha--MSH 4-10 [Nle 4 , D--Phe 7 ]--alpha--MSH 4-11 [Nle 4 , D--Phe 7 , D--Trp 9 [--alpha--MSH 4-11 [Nle 4 , D--Phe 7 ]--alpha--MSH 4-9
Claim 14
Independent Claim
207 words
A method for the stimulation of integumental melanocytes in a vertebrate which comprises administrating topically to the epidermal tissue of said vertebrate in an amount sufficient to cause stimulation, a compound of the group: (1) alpha-MSH having the amino acid formula: Ac--Ser--Tyr--Ser--Met--Glu--His--Phe--Arg--Trp--Gly--Lys--Pro--Val--NH.sub.2 ; (2) alpha--MSH analogues having the formula: Ac--Ser--Tyr--Ser--M--Glu--His--D--Phe--Arg--Trp--Gly--Lys--Pro--Val--NH.sub.2 wherein M is selected from the group consisting of Met, Nle and Cys; (3) analogues of alpha--MSH having the formula: R 1 --W--X--Y--Z--R 2 wherein R 1 is selected from the group consisting of Ac--Gly, Ac--Met--Glu,Ac--Nle--Glu, and Ac--Tyr--Glu' wherein W is selected from the group consisting of His and D--His; wherein X is selected from the group consisting of Phe, D--Phe--Tyr, D--Tyr, and (pNO 2 )D--Phe; wherein Y is selected from the group consisting of Arg and D--Arg; wherein Z is selected from the group consisting of Trp and D--Trp; and wherein R 2 is selected from the group consisting of NH 2 , Gly--N 2 and Gly--Lys--NH 2 ; and (4) alpha--MSH analogues selected from the group consisting of [Nle 4 , D--Phe 7 ]--alpha--MSH [Nle 4 , D--Phe 7 ]--alpha--MSH 4-10 [Nle 4 , D--Phe 7 ]--alpha--MSH 4-11 [Nle 4 , D--Phe 7 , D--Trp 9 [--alpha--MSH 4-11 [Nle 4 , D--Phe 7 ]--alpha--MSH 4-9
Claim 15
Dependent Claim
17 words
The method of claim 12 wherein the compound is [Nle 4 , D--Phe 7 ]--alpha--MSH 4-10 .
Claim 16
Dependent Claim
17 words
The method of claim 12 wherein the compound is [Nle 4 , D--Phe 7 ]--alpha--MSH 4-11 .
Claim 17
Dependent Claim
20 words
The method of claim 12 wherein the compound is [Nle 4 , D--Phe 7 , D--Trp 9 ]--alpha--MSH 4-11 .
Claim 18
Dependent Claim
17 words
The method of claim 12 wherein the compound is [Nle 4 , D--Phe 7 ]--alpha--MSH 4-9 .
Claim 19
Dependent Claim
11 words
The method of claim 12 wherein the compound is Ac--Ser--Tyr--Ser--Met--Glu--His--Phe--Arg--Trp--Gly--Lys--ProVal--NH.sub.2 ;
Claim 20
Dependent Claim
10 words
The method of claim 12 wherein the compound is Ac--Ser--Tyr--Ser--Cys--Glu--His--D--Phe--Arg--Trp--Gly--Lys--ProVal--NH.sub.2
Claim 21
Dependent Claim
18 words
A method of claim 12 wherein the compound is an analogue of alpha--MSH in which X is D--Phe.
Claim 22
Dependent Claim
19 words
A method of claim 12 wherein the compound is an analogue of alpha--MSH in which R 1 is Ac--Nle--Glu.
Claim 23
Dependent Claim
23 words
A method of claim 12 wherein the compound is an analogue of alpha--MSH is which R 1 is Ac--Nle--Glu, and X is D--Phe.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-09-11 | 1993-03-13 | 1993-09-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-09-11 | 1997-03-13 | 1997-09-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-09-11 | 2001-03-13 | 2001-09-12 | $7700.00 | Window Closed / Lapsed |