IP Library Patent Application 16903566
Patent Application
App. No. 16/903,566

AROMATIC-CATIONIC PEPTIDES AND USES OF SAME

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Patent No.
US None
App. No.
16/903,566
Abstract

The disclosure provides compositions and methods relating to aromatic-cationic peptides. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof. For example, the peptides may be administered to subjects in need of a mitochondrial-targeted antioxidant.

Claims (114)

1 . An aromatic-cationic peptide selected from the group consisting of:

D-Arg-Tyr-Lys-Phe-NH 2

D-Arg-Dmt-D-Lys-Phe-NH 2

D-Arg-Dmt-Lys-D-Phe-NH 2

Phe-D-Arg-D-Phe-Lys-NH 2

Phe-D-Arg-Phe-D-Lys-NH 2

D-Phe-D-Arg-D-Phe-D-Lys-NH 2

Lys-D-Phe-Arg-Dmt-NH 2

D-Arg-Arg-Dmt-Phe-NH 2

Dmt-D-Phe-Arg-Lys-NH 2

Phe-D-Dmt-Arg-Lys-NH 2

D-Arg-Dmt-Lys-NH 2

Arg-D-Dmt-Lys-NH 2

D-Arg-Dmt-Phe-NH 2

Arg-D-Dmt-Arg-NH 2

Dmt-D-Arg-NH 2

D-Arg-Dmt-NH 2

D-Dmt-Arg-NH 2

Arg-D-Dmt-NH 2

D-Arg-D-Dmt-NH 2

D-Arg-D-Tyr-Lys-Phe-NH 2

D-Arg-Tyr-D-Lys-Phe-NH 2

D-Arg-Tyr-Lys-D-Phe-NH 2

D-Arg-D-Tyr-D-Lys-D-Phe-NH 2

Lys-D-Phe-Arg-Tyr-NH 2

D-Arg-Arg-Tyr-Phe-NH 2

Tyr-D-Phe-Arg-Lys-NH 2

Phe-D-Tyr-Arg-Lys-NH 2

D-Arg-Tyr-Lys-NH 2

Arg-D-Tyr-Lys-NH 2

D-Aig-Tyr-Phe-NH 2

Arg-D-Tyr-Arg-NH 2

Tyr-D-Arg-NH 2

D-Arg-Tyr-NH 2

D-Tyr-Arg-NH 2

Arg-D-Tyr-NH 2

D-Arg-D-Tyr-NH 2

Dmt-Lys-Phe-NH 2

Lys-Dmt-D-Arg-NH 2

Phe-Lys-Dmt-NH 2

D-Arg-Phe-Lys-NH 2

D-Arg-Cha-Lys-NH 2

D-Arg-Trp-Lys-NH 2

Dmt-Lys-D-Phe-NH 2

Dmt-Lys-NH 2

Lys-Phe-NH 2

D-Arg-Cha-Lys-Cha-NH 2

D-Nle-Dmt-Ahe-Phe-NH 2

D-Nle-Cha-Ahe-Cha-NH 2

wherein Cha is cyclohexyl alanine, Nle is norleucine, and Ahe is 2-amino-heptanoic acid.

2 . A pharmaceutical composition comprising one or more aromatic-cationic peptides of claim 1 and pharmaceutically acceptable salts thereof.

3 . The pharmaceutical composition of claim 2 further comprising a pharmaceutically acceptable carrier.

4 . A method of reducing the number of mitochondria undergoing mitochondrial permeability transition (MPT), or preventing mitochondrial permeability transitioning in a mammal in need thereof, the method comprising administering to the mammal an effective amount of one or more aromatic-cationic peptides of claim 1 .

5 . A method for reducing oxidative damage in a mammal in need thereof, the method comprising administering to the mammal an effective amount of one or more aromatic-cationic peptides of claim 1 .

6 . A method for increasing the ATP synthesis rate in a mammal in need thereof, the method comprising administering to the mammal an effective amount of one or more aromatic-cationic peptides of claim 1 .

7 . A method for determining the presence or amount of an administered aromatic-cationic peptide in a subject, the method comprising: detecting the administered aromatic-cationic peptide in a biological sample from the subject, wherein the aromatic-cationic peptide is selected from the group consisting of:

D-Arg-Tyr-Lys-Phe-NH 2

D-Arg-Dmt-D-Lys-Phe-NH 2

D-Arg-Dmt-Lys-D-Phe-NH 2

Phe-D-Arg-D-Phe-Lys-NH 2

Phe-D-Arg-Phe-D-Lys-NH 2

D-Phe-D-Arg-D-Phe-D-Lys-NH 2

Lys-D-Phe-Arg-Dmt-NH 2

D-Arg-Arg-Dmt-Phe-NH 2

Dmt-D-Phe-Arg-Lys-NH 2

Phe-D-Dmt-Arg-Lys-NH 2

D-Arg-Dmt-Lys-NH 2

Arg-D-Dmt-Lys-NH 2

D-Arg-Dmt-Phe-NH 2

Arg-D-Dmt-Arg-NH 2

Dmt-D-Arg-NH 2

D-Arg-Dmt-NH 2

D-Dmt-Arg-NH 2

Arg-D-Dmt-NH 2

D-Arg-D-Dmt-NH 2

D-Arg-D-Tyr-Lys-Phe-NH 2

D-Arg-Tyr-D-Lys-Phe-NH 2

D-Arg-Tyr-Lys-D-Phe-NH 2

D-Arg-D-Tyr-D-Lys-D-Phe-NH 2

Lys-D-Phe-Arg-Tyr-NH 2

D-Arg-Arg-Tyr-Phe-NH 2

Tyr-D-Phe-Arg-Lys-NH 2

Phe-D-Tyr-Arg-Lys-NH 2

D-Arg-Tyr-Lys-NH 2

Arg-D-Tyr-Lys-NH 2

D-Arg-Tyr-Phe-NH 2

Arg-D-Tyr-Arg-NH 2

Tyr-D-Arg-NH 2

D-Arg-Tyr-NH 2

D-Tyr-Arg-NH 2

Arg-D-Tyr-NH 2

D-Arg-D-Tyr-NH 2

Dmt-Lys-Phe-NH 2

Lys-Dmt-D-Arg-NH 2

Phe-Lys-Dmt-NH 2

D-Arg-Phe-Lys-NH 2

D-Arg-Cha-Lys-NH 2

D-Arg-Trp-Lys-NH 2

Dmt-Lys-D-Phe-NH 2

Dmt-Lys-NH 2

Lys-Phe-NH 2

D-Arg-Cha-Lys-Cha-NH 2

D-Nle-Dmt-Ahe-Phe-NH 2 and

D-Nle-Cha-Ahe-Cha-NH 2 .

8 . The method of claim 7 , wherein detecting is performed during administration of the peptide.

9 . The method of claim 7 , wherein detecting is performed after administration of the peptide.

10 . The method of any one of claim 7 , wherein detecting comprises HPLC.

11 . The method of claim 10 , wherein the HPLC comprises reverse phase HPLC.

12 . The method of claim 10 , wherein the HPLC comprises ion exchange HPLC.

13 . The method of claim 7 , wherein detecting comprises mass spectrometry.

14 . The method of claim 7 , wherein the biological sample comprises a fluid.

15 . The method of claim 7 , wherein the biological sample comprises a cell.

16 . The method of claim 7 , wherein the biological sample comprises a tissue.

17 . The method of any one of claim 7 , wherein the biological sample comprises a biopsy.

Assignments (5)
CHANGE OF ADDRESS Recorded Nov 11, 2022
From: STEALTH BIOTHERAPEUTICS INC.
To: STEALTH BIOTHERAPEUTICS INC.
Reel/Frame 061925/0092 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2021
From: STEALTH BIOTHERAPEUTICS CORP
To: STEALTH BIOTHERAPEUTICS INC.
Reel/Frame 058164/0305 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 19, 2021
From: GU, LAWRENCE
To: STEALTH PEPTIDES INTERNATIONAL, INC.
Reel/Frame 056897/0807 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 19, 2021
From: LIU, LIPING
To: STEALTH PEPTIDES INTERNATIONAL, INC.
Reel/Frame 056901/0202 →
CHANGE OF NAME Recorded Jul 19, 2021
From: STEALTH PEPTIDES INTERNATIONAL, INC.
To: STEALTH BIOTHERAPEUTICS CORP
Reel/Frame 056999/0278 →