# US 10,500,286 B2 · CCK2R-drug conjugates

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- Number: US 10,500,286 B2
- Document ID: US10500286B2
- Status: Granted
- Kind: B2
- Application number: 15/751,633
- Filed: 2016-08-10
- Published: 2018-08-16
- Granted: 2019-12-10
- Earliest claimed: 2015-08-14
- Assignees: Endocyte, Inc.
- Applicants: Endocyte, Inc.
- Inventors: Garth L. Parham; Melissa Nelson; Marilynn Vetzel; Christina M. Dircksen; Joseph Anand Reddy; Christopher Paul Leamon; Iontcho Radoslavov Vlahov
- Web page: https://patentgrep.com/patent/US10500286B2

## CPC

- 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 31/5513: 1,4-Benzodiazepines, e.g. diazepam {or clozapine}
- A61K 38/03: Peptides having up to 20 amino acids in an undefined or only partially defined sequence; Derivatives thereof
- A61K 38/07: Tetrapeptides
- A61K 47/545: {Heterocyclic compounds (A61K47/558 takes precedence)}
- A61K 49/00: Preparations for testing in vivo
- A61K 51/088: {conjugates with carriers being peptides, polyamino acids or proteins (antibodies A61K51/10)}
- A61P 35/00: Antineoplastic agents
- C07D 209/20: substituted additionally by nitrogen atoms, e.g. tryptophane
- C07D 243/12: 1,5-Benzodiazepines; Hydrogenated 1,5-benzodiazepines
- C07D 405/14: containing three or more hetero rings
- C07D 417/14: containing three or more hetero rings
- A61K 38/14: Peptides containing saccharide radicals; Derivatives thereof {, e.g. bleomycin, phleomycin, muramylpeptides or vancomycin}
- 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
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The disclosure provided herein pertains to CCK2R-drug conjugates. In particular, the disclosure pertains to CCK2R-drug conjugates that target the delivery of drugs to a mammalian recipient. Also described are methods of making and using CCK2R-drug conjugates.

## Claims

### Claim 1

A conjugate of the formula A-L-B, or a pharmaceutically acceptable salt thereof, wherein A is an imaging agent (I), L is a linker, and B is a binding ligand of CCK2R,
wherein the conjugate has the formula
wherein R is H, SO3− or SO3M, wherein M is a counter-ion, L is a linker, and I is an imaging agent, and
wherein L is of the formula
wherein AA is an amino acid, R′ is selected from the group consisting of H, C1-C6 alkyl, and —C(O)R″, R″ is selected from the group consisting of H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl C3-C6 cycloalkyl and C6-C10 aryl, m is an integer between 1 and 50, and * is a covalent bond.

### Claim 2 (depends on 1)

The conjugate of claim 1, or a pharmaceutically acceptable salt thereof, wherein each amino acid is independently selected from the group consisting of L-asparagine, L-arginine, L-glycine, L-aspartic acid, L-glutamic acid, L-glutamine, L-cysteine, L-alanine, L-valine, L-leucine, L-isoleucine, 3-amino-L-alanine, D-asparagine, D-arginine, D-glycine, D-aspartic acid, D-glutamic acid, D-glutamine, D-cysteine, D-alanine, D-valine, D-leucine, D-isoleucine and 3-amino-D-alanine.

### Claim 3 (depends on 1)

The conjugate of claim 1, or a pharmaceutically acceptable salt thereof, wherein each amino acid is independently selected from the group consisting of L-asparagine, L-arginine, L-glycine, L-aspartic acid, L-glutamic acid, L-glutamine, L-cysteine, L-alanine, L-valine, L-leucine, L-isoleucine and 3-amino-L-alanine.

### Claim 4 (depends on 1)

The conjugate of claim 1, or a pharmaceutically acceptable salt thereof, of the formula

### Claim 5 (depends on 1)

A pharmaceutical composition, comprising a conjugate of claim 1, or a pharmaceutically acceptable salt thereof, and optionally at least one excipient.