# US 2014/0155329 A1 · Long-Acting Peptide Analogs

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- Number: US 2014/0155329 A1
- Document ID: US20140155329A1
- Status: Published application
- Kind: A1
- Application number: 14/110,098
- Filed: 2012-04-05
- Published: 2014-06-05
- Earliest claimed: 2011-04-07
- Assignees: The Board of Trustees of the Leland Stanford Junior University
- Inventors: Sheau Yu Hsu; Chia Lin Chang
- Web page: https://patentgrep.com/patent/US20140155329A1

## CPC

- A61K 38/22: Hormones (derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin A61K38/33, e.g. corticotropin A61K38/35)
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/02: Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/12: Antihypertensives
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 14/575: Hormones (derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin C07K14/665, e.g. corticotropin C07K14/695)
- A61K 47/50: the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- C07K 16/28: against receptors, cell surface antigens or cell surface determinants
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)

## Abstract

Long-acting agonistic analogs for CLR/RAMP receptors are provided that have an extended half-live in vivo.

## Claims

### Claim 1

A biologically active intermedin or adrenomedullin peptide having a serum half-life of greater than 1.5 hours.

### Claim 2 (depends on 1)

The peptide of claim 1, wherein the peptide is modified by conjugation of a polymer to the amino terminus of the peptide.

### Claim 3 (depends on 2)

The peptide of claim 2, wherein said peptide has the structure:
where R1 is a linear or branched C3-C100 alkyl; preferably a C4-C30 alkyl optionally substituted with halo, hydroxy, alkoxy, amino, alkylamino, dialkylamino, sulfate, or phosphate, and which may by saturated, or mono- or di-unsaturated.

### Claim 4 (depends on 3)

The peptide of claim 3, wherein R1 is selected from palmitate; stearate; arachidic acid; lauric acid; myristic acid; myristoleic acid; palmitoleic acid; sapienic acid; oleic acid; linoleic acid; α-linolenic acid; arachidonic acid; eicosapentaenoic acid; erucic acid; and docosahexaenoic acid.

### Claim 5 (depends on 1)

The peptide of claim 1, wherein the peptide comprises or consists of the amino acid sequence set forth as SEQ ID NO:3; SEQ ID NO:4; or SEQ ID NO:7.

### Claim 6 (depends on 1)

The peptide of claim 1, wherein the peptide comprises or consists of the amino acid sequence set forth as SEQ ID NO:6.

### Claim 7 (depends on 1)

A pharmaceutical composition comprising a therapeutically effective dose of the peptide of claim 1, and a pharmaceutically acceptable derivative.

### Claim 8 (depends on 7)

A method of delivering a long-acting agonist for CLR/RAMP receptors activity to a host animal for an extended period of time, the method comprising administering to said animal a pharmaceutical composition according to claim 7.

### Claim 9 (depends on 7)

A method of reducing peripheral blood pressure in an individual while increasing cardiac output, the method comprising:
administering to said individual a pharmaceutical composition according to claim 7, wherein the peptide is delivered at a time interval greater than once every four hours.

### Claim 10 (depends on 9)

The method of claim 9, wherein the peptide is delivered at a time interval greater than once every 12 hours.