# US 8,465,724 B2 · Multi-drug ligand conjugates

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- Number: US 8,465,724 B2
- Document ID: US8465724B2
- Status: Granted
- Kind: B2
- Application number: 12/064,191
- Filed: 2006-08-18
- Published: 2008-10-09
- Granted: 2013-06-18
- Earliest claimed: 2005-08-19
- Assignees: Endocyte, Inc.
- Applicants: Iontcho Radoslavov Vlahov; Christopher Paul Leamon
- Inventors: Iontcho Radoslavov Vlahov; Christopher Paul Leamon
- Web page: https://patentgrep.com/patent/US8465724B2

## CPC

- A61K 47/65: Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
- A61K 47/551: {one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic 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)
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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

## Abstract

Described herein are compounds, pharmaceutical compositions and methods for treating pathogenic cell populations in a patient. The compounds described herein include conjugates of a plurality of cytotoxic drugs and vitamin receptor binding ligands. The plurality of drugs may be the same or different. Similarly, the vitamin receptor binding ligands may be the same or different. The conjugates also include a linker that is formed from one or more spacer linkers, heteroatom linkers, and releasable linkers.

## Claims

### Claim 1

A compound of the formula
or a pharmaceutically acceptable salt thereof, wherein q is an integer from 0 to 8; or
or a pharmaceutically acceptable salt thereof, wherein AA forms an amino acid; and n is an integer from 0 to 8.

### Claim 2 (depends on 1)

The compound of claim 1 wherein q is 1 to 8.

### Claim 3 (depends on 1)

The compound of claim 1 wherein n is 1 to 8.

### Claim 4

A compound of the formula
or
or
or a pharmaceutically acceptable salt thereof.

### Claim 5 (depends on 4)

The compound of claim 4 the formula
or a pharmaceutically acceptable salt thereof.

### Claim 6 (depends on 4)

The compound of claim 4 the formula
or a pharmaceutically acceptable salt thereof.

### Claim 7 (depends on 4)

The compound of claim 4 the formula
or a pharmaceutically acceptable salt thereof.

### Claim 8 (depends on 4)

A pharmaceutical composition comprising a drug delivery conjugate of claim 4, and a pharmaceutically acceptable carrier, diluent, or excipient therefor.

### Claim 9 (depends on 1)

A pharmaceutical composition comprising the compound of claim 1, and a pharmaceutically acceptable carrier, diluent, or excipient therefor.