Conjugates for treating diseases caused by PSMA expressing cells

Patent metadata

Field	Value
Publication number	US-10912840-B2
Application number	US-201815977640-A
Country	US
Kind code	B2
Filing date	May 11, 2018
Priority date	Nov 15, 2012
Publication date	Feb 9, 2021
Grant date	Feb 9, 2021

Abstract

The invention described herein pertains to the diagnosis, imaging, and/or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and/or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using compounds capable of targeting PSMA expressing cells.

First claim

What is claimed is:

1. A conjugate having a formula B-L-(D) n , or a pharmaceutically acceptable salt thereof;
wherein B is a radical of a prostate-specific membrane antigen (PSMA) binding ligand having the formula

wherein * is the point of attachment to L;
L is a polyvalent linker comprising an aminomethylphenylacetic acid diradical; an alkylene substituted with one or more substituents X 1 selected from the group consisting of aryl, substituted aryl, arylalkyl, and substituted arylalkyl; and a cyclic structure selected from the group consisting of a cyclic ether, a cyclic amine, a heterocycle, an arylene, and a heteroarylene;
wherein D is a positron emission tomography (PET) imaging agent; and
wherein n is 1 .

2. The conjugate or a pharmaceutically acceptable salt thereof of claim 1 , wherein the linker further comprises one or more amino acids.

3. The conjugate or a pharmaceutically acceptable salt thereof of claim 1 , wherein the positron emission tomography (PET) imaging agent is an 18 F group covalently attached to the polyvalent linker.

4. The conjugate or a pharmaceutically acceptable salt thereof of claim 1 , wherein the conjugate comprises a fluoroaryl group selected from the group consisting of fluorophenyl, difluorophenyl, and fluoronitrophenyl.

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

Assignees

• Endocyte Inc

Inventors

• Vlahov Iontcho Radoslavov
• Reddy Joseph Anand
• Bloomfield Alicia
• Dorton Ryan
• Nelson Melissa
• Vetzel Marilynn
• Leamon Christopher Paul

Classifications

• A61K47/64 Primary

  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) · CPC title

• A61K49/0002 Primary

  General or multifunctional contrast agents, e.g. chelated agents · CPC title

• C07K5/1019

  with the first amino acid being basic · CPC title

• C07K5/06113

  Asp- or Asn-amino acid · CPC title

• C07K5/021

  containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds · CPC title