IP Library Patent Application 12085221
Patent Application
App. No. 12/085,221

Skin Repair Accelerating Therapeutic Agent Containing Ghrelin and Derivatives Thereof or Substance Acting On GHS-R1a as Active Ingredient

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Quick Facts
Patent No.
US None
App. No.
12/085,221
Abstract

The present invention provides a novel therapeutic agent for skin injuries and a skin regeneration accelerator. The therapeutic agent for skin injuries and the skin regeneration accelerator containing a substance acting on a growth hormone secretagogue receptor or a pharmaceutically acceptable salt thereof as an active ingredient.

Claims (35)

1 . A therapeutic agent for skin injuries, comprising a substance acting on a growth hormone secretagogue receptor or a pharmaceutically acceptable salt thereof as an active ingredient.

2 . The therapeutic agent according to claim 1 , wherein the substance is a peptide selected from the group consisting of (i) a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a third amino acid residue from the amino terminus is a modified amino acid residue in which fatty acid is introduced into the side chain of the amino acid residue and (ii) a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which one or several of 5 th to 28 th amino acids from the amino terminus are deleted, substituted and/or added, and the 3 rd amino acid residue from the amino terminus is a modified amino acid residue having fatty acid introduced into the side chain of the amino acid residue, or a pharmaceutically acceptable salt thereof.

3 . The therapeutic agent according to claim 2 , wherein the substance is a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a serine residue at the 3 rd position from the amino terminus is a modified amino acid residue having fatty acid introduced into the side chain hydroxyl group of the amino acid residue.

4 . The therapeutic agent according to claim 3 , wherein the substance is a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a serine residue at the 3 rd position from the amino terminus has a side chain hydroxyl group acylated with an n-octanoyl group.

5 . The therapeutic agent according to claim 1 , containing the active ingredient in an amount of 0.001 mg to 100 mg per unit formulation.

6 . A skin regeneration accelerator, comprising a substance acting on the growth hormone secretagogue receptor, or a pharmaceutically acceptable salt thereof, as an active ingredient.

7 . The accelerator according to claim 6 , wherein the substance is a peptide selected from the group consisting of (i) a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a third amino acid residue from the amino terminus is a modified amino acid residue in which fatty acid is introduced into the side chain of the amino acid residue and (ii) a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which one or several of 5 th to 28 th amino acids from the amino terminus are deleted, substituted and/or added, and the 3 rd amino acid residue from the amino terminus is a modified amino acid residue having fatty acid introduced into the side chain of the amino acid residue, or a pharmaceutically acceptable salt thereof.

8 . The accelerator according to claim 7 , wherein the substance is a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a serine residue at the 3rd position from the amino terminus is a modified amino acid residue having fatty acid introduced into the side chain hydroxyl group of the amino acid residue.

9 . The accelerator according to claim 8 , wherein the substance is a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a serine residue at the 3 rd position from the amino terminus has a side chain hydroxyl group acylated with an n-octanoyl group.

10 . The accelerator according to claim 6 , containing the active ingredient in an amount of 0.001 mg to 100 mg per unit formulation.

11 . A method for accelerating proliferation of a cultured skin cell, using a substance acting on the growth hormone secretagogue receptor or a pharmaceutically acceptable salt thereof as an active ingredient.

12 . The method according to claim 11 , wherein the substance is a peptide selected from the group consisting of (i) a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a third amino acid residue from the amino terminus is a modified amino acid residue in which fatty acid is introduced into the side chain of the amino acid residue and (ii) a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which one or several of 5 th to 28 th amino acids from the amino terminus are deleted, substituted and/or added, and the 3 rd amino acid residue from the amino terminus is a modified amino acid residue having fatty acid introduced into the side chain of the amino acid residue, or a pharmaceutically acceptable salt thereof.

13 . The method according to claim 12 , wherein the substance is a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a serine residue at the 3 rd position from the amino terminus is a modified amino acid residue having fatty acid introduced into the side chain hydroxyl group of the amino acid residue.

14 . The method according to claim 13 , wherein the substance is a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a serine residue at the 3 rd position from the amino terminus has a side chain hydroxyl group acylated with an n-octanoyl group.

15 . The method according to claim 11 , wherein proliferation of the cultured skin cell is performed in a medium containing the active ingredient in an amount of 0.0000001 mg/mL to 0.1 mg/mL.

16 . A treatment method of skin injuries, comprising administration of a substance acting on a growth hormone secretagogue receptor or a pharmaceutically acceptable salt thereof as an active ingredient to a mammal requiring treatment of skin injuries.

17 . The method according to claim 16 , wherein the substance is a peptide selected from the group consisting of (i) a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a third amino acid residue from the amino terminus is a modified amino acid residue in which fatty acid is introduced into the side chain of the amino acid residue and (ii) a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which one or several of 5 th to 28 th amino acids from the amino terminus are deleted, substituted and/or added, and the 3 rd amino acid residue from the amino terminus is a modified amino acid residue having fatty acid introduced into the side chain of the amino acid residue, or a pharmaceutically acceptable salt thereof.

18 . The method according to claim 17 , wherein the substance is a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a serine residue at the 3 rd position from the amino terminus is a modified amino acid residue having fatty acid introduced into the side chain hydroxyl group of the amino acid residue.

19 . The method according to claim 18 , wherein the substance is a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a serine residue at the 3 rd position from the amino terminus has a side chain hydroxyl group acylated with an n-octanoyl group.

20 . The method according to claim 16 , wherein the active ingredient is administered in an amount of 0.001 mg to 100 mg per administration.

21 . A method for accelerating skin regeneration, comprising administration of a substance acting on a growth hormone secretagogue receptor or a pharmaceutically acceptable salt thereof as an active ingredient to a mammal requiring acceleration of skin regeneration.

22 . The method according to claim 21 , wherein the substance is a peptide selected from the group consisting of (i) a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a third amino acid residue from the amino terminus is a modified amino acid residue in which fatty acid is introduced into the side chain of the amino acid residue and (ii) a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which one or several of 5 th to 28 th amino acids from the amino terminus are deleted, substituted and/or added, and the 3 rd amino acid residue from the amino terminus is a modified amino acid residue having fatty acid introduced into the side chain of the amino acid residue, or a pharmaceutically acceptable salt thereof.

23 . The method according to claim 22 , wherein the substance is a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a serine residue at the 3 rd position from the amino terminus is a modified amino acid residue having fatty acid introduced into the side chain hydroxyl group of the amino acid residue.

24 . The method according to claim 23 , wherein the substance is a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a serine residue at the 3 rd position from the amino terminus has a side chain hydroxyl group acylated with an n-octanoyl group.

25 . The method according to claim 21 , wherein the active ingredient is administered in an amount of 0.001 mg to 100 mg per administration.

26 . Use of a substance acting on a growth hormone secretagogue receptor or a pharmaceutically acceptable salt thereof as an active ingredient for production of a pharmaceutical composition for treatment of skin injuries.

27 . The use according to claim 26 , wherein the substance is a peptide selected from the group consisting of (i) a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a third amino acid residue from the amino terminus is a modified amino acid residue in which fatty acid is introduced into the side chain of the amino acid residue and (ii) a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which one or several of 5 th to 28 th amino acids from the amino terminus are deleted, substituted and/or added, and the 3 rd amino acid residue from the amino terminus is a modified amino acid residue having fatty acid introduced into the side chain of the amino acid residue, or a pharmaceutically acceptable salt thereof.

28 . The use according to claim 27 , wherein the substance is a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a serine residue at the 3 rd position from the amino terminus is a modified amino acid residue having fatty acid introduced into the side chain hydroxyl group of the amino acid residue.

29 . The use according to claim 28 , wherein the substance is a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a serine residue at the 3 rd position from the amino terminus has a side chain hydroxyl group acylated with an n-octanoyl group.

30 . The use according to claim 26 , wherein the pharmaceutical composition for treatment of skin injuries contains the active ingredient in an amount of 0.001 mg to 100 mg per unit formulation.

31 . Use of a substance acting on a growth hormone secretagogue receptor or a pharmaceutically acceptable salt thereof as an active ingredient for production of a pharmaceutical composition for acceleration of skin regeneration.

32 . The use according to claim 3 l, wherein the substance is a peptide selected from the group consisting of (i) a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a third amino acid residue from the amino terminus is a modified amino acid residue in which fatty acid is introduced into the side chain of the amino acid residue and (ii) a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which one or several of 5 th to 28 th amino acids from the amino terminus are deleted, substituted and/or added, and the 3 rd amino acid residue from the amino terminus is a modified amino acid residue having fatty acid introduced into the side chain of the amino acid residue, or a pharmaceutically acceptable salt thereof.

33 . The use according to claim 32 , wherein the substance is a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a serine residue at the 3 rd position from the amino terminus is a modified amino acid residue having fatty acid introduced into the side chain hydroxyl group of the amino acid residue.

34 . The use according to claim 33 , wherein the substance is a peptide having an amino acid sequence represented by SEQ ID NO: 1, in which a serine residue at the 3 rd position from the amino terminus has a side chain hydroxyl group acylated with an n-octanoyl group.

35 . The use according to claim 31 , wherein the pharmaceutical composition for acceleration of skin regeneration contains the active ingredient in an amount of 0.001 mg to 100 mg per unit formulation.

Assignments (3)
MERGER Recorded Nov 3, 2010
From: JAPAN AS REPRESENTED BY PRESIDENT OF NATIONAL CARDIOVASCULAR CENTER
To: NATIONAL CEREBRAL AND CARDIOVASCULAR CENTER
Reel/Frame 025243/0123 →
MERGER Recorded Jul 13, 2010
From: ASUBIO PHARMA CO., LTD.
To: DAIICHI SANKYO COMPANY, LIMITED
Reel/Frame 024674/0910 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 10, 2008
From: MURAKAMI, NOBORU; NAKAHARA, KEIKO; KANGAWA, KENJI; HAYASHI, YUJIRO
To: UNIVERSITY OF MIYAZAKI; JAPAN AS REPRESENTED BY PRESIDENT OF NATIONAL CARDIOVASCULAR CENTER; ASUBIO PHARMA CO., LTD.
Reel/Frame 021532/0849 →