# US 2008/0187493 A1 · Peptide-Based Compounds

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- Number: US 2008/0187493 A1
- Document ID: US20080187493A1
- Status: Published application
- Kind: A1
- Application number: 12/053,829
- Filed: 2008-03-24
- Published: 2008-08-07
- Earliest claimed: 2000-04-12
- Assignees: Ge Healthcare Limited
- Inventors: Alan Cuthbertson; Bard Indrevoll
- Web page: https://patentgrep.com/patent/US20080187493A1

## CPC

- A61K 51/082: {the peptide being a RGD-containing peptide}
- A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
- A61K 47/62: the modifying agent being a protein, peptide or polyamino acid
- A61K 47/64: Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent (peptidic linkers A61K47/65)
- A61K 51/088: {conjugates with carriers being peptides, polyamino acids or proteins (antibodies A61K51/10)}
- A61P 9/00: Drugs for disorders of the cardiovascular system
- 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 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 35/04: specific for metastasis
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 7/02: Linear peptides containing at least one abnormal peptide link
- C07K 7/06: having 5 to 11 amino acids
- C07K 14/78: Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin or cold insoluble globulin [CIG]
- 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

The invention relates to new peptide-based compounds for use as diagnostic imaging agents or as therapeutic agents wherein the agents comprise a targeting vector which binds to receptors associated with integrin receptors.

## Claims

### Claim at position 1

1-20. (canceled)

### Claim 21

A compound of formula I representing a vector (V)
wherein
G represents glycine, and
D represents aspartic acid, and
R1 represents —(CH2)n— or —(CH2)n—C6H4— wherein
n represents a positive integer 1 to 10, and
h represents a positive integer 1 or 2, and
X1 represents a bond or 1 to 5 amino acid residues wherein each amino acid residue independently optionally can be derivatized with a functional side-chain suitable for modifying the pharmacokinetics or blood clearance rates of the said agents, and
X2 and X4 represent independently an amino acid residue capable of forming a disulfide bond,
X3 represents arginine, N-methylarginine or an arginine mimetic,
X5 represents a hydrophobic amino acid or derivatives thereof, and
X6 represents a thiol-containing amino acid residue,
and k represents a positive integer 1 to 10, and
X7 represents 1 to 10 amino acid residues or is absent,
and X8 is absent.

### Claim 22

A pharmaceutical composition comprising an effective amount of a compound of general formula (I) or a salt thereof, together with one or more pharmaceutically acceptable adjuvants, excipients or diluents for use in enhancing image contrast in in vivo imaging or for treatment of a disease.

### Claim 23

A process for the preparation of a contrast agent comprising the moieties vector (V), linker (L) and reporter (R), said process comprising the conjugation of the vector V, optionally via the linker (L) to a compound detectable in a diagnostic imaging procedure or to a chelating agent and if necessary metallating the chelant groups in the resultant conjugate with a metal ion detectable in a diagnostic imaging procedure.

### Claim 24 (depends on 21)

A compound as claimed in claim 21 for the manufacture of a contrast medium for use in a method of diagnosis involving administration of said contrast medium to an animate subject and generation of an image of at least part of said subject.

### Claim 25 (depends on 21)

A method of generating an image of an human or non-human animal subject involving administering a contrast agent to said subject, and generating an image of at least a part of said subject to which said contrast agent has distributed, characterised in that said contrast agent comprises a compound of claim 21.

### Claim 26 (depends on 21)

A method of generating enhanced images of a human or non-human animal subject previously administered with a contrast agent composition comprising a compound as claimed in claim 21, which method comprises generating an image of at least part of said subject.

### Claim 27 (depends on 21)

A method of monitoring the effect of treatment of a human or non-human animal subject with a drug to combat a condition associated with cancer, said method involving administering to said subject a compound of claim 21 and detecting the uptake of said agent by cell receptors, said administration and detection optionally but preferably being effected repeatedly.

### Claim 28 (depends on 21)

A method of treating cancer or a related disease in a human or non-human body which comprises the administration of an effective amount of a compound of claim 21.

### Claim 29 (depends on 21)

A compound according to claim 21 for the manufacture of a medicament for the therapeutic or prophylactic treatment of cancer or a related disease in a human or non-human.