US4918055A
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Method of stimulating melanocytes by topical application of analogs of alpha-MSH, and compositions for use in same
Assignee: Individual
•
Filing: 1988-02-11
•
Granted: 1990-04-17
•
Expires: 2008-02-11
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
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 01:15
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
203 words
A method for stimulating melanin production in a vertebrate which comprises administrating 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-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.sub.1 -W-X-Y-Z-R.sub.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-Try, 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
203 words
A method for stimulating melanin production in a vertebrate which comprises administrating 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-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.sub.1 -W-X-Y-Z-R.sub.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-Try, 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
12 words
The method of claim 1 wherein the compound is Ac-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trg-Gly-Lys-Pro-Val-NH 2 .
Claim 9
Dependent Claim
12 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 in which R 1 is Ac-Nle-Glu, and X is D-Phe.
Claim 13
Independent Claim
207 words
A method for the stimulation of integumental melancytes 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.sub.1 -W-X-Y-Z-R.sub.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 RH 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 melancytes 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.sub.1 -W-X-Y-Z-R.sub.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 RH 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
12 words
The method of claim 12 wherein the compound is Ac-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH 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-Pro-Val-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 in which R 1 is Ac-Nle-Glu, and X is D-Phe.
References Cited (Backward Citations)
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