Conjugates for treating diseases caused by PSMA expressing cells

• US 9,636,413 B2
• Filed: 11/14/2013
• Issued: 05/02/2017
• Est. Priority Date: 11/15/2012
• Status: Active Grant

• Current Assignee: Endocyte, Inc. (Novartis Ag)
• Original Assignee: Endocyte, Inc. (Novartis Ag)
• Inventors: Vlahov, Iontcho Radoslavov, Reddy, Joseph Anand, Leamon, Christopher Paul, Bloomfield, Alicia, Dorton, Ryan, Nelson, Melissa, Vetzel, Marilynn
• Primary Examiner(s): Ha, Julie
• Assistant Examiner(s): KOMATSU, LI N
• Application Number:
  US14/443,212
• Publication Number:
  US 20150297735A1
• Time in Patent Office: 1,265 Days
• CPC Class Codes: A61K 38/00 Medicinal preparations containing peptides peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00
• CPC Class Codes: A61K 38/05 Dipeptides
• CPC Class Codes: A61K 38/06 Tripeptides
• CPC Class Codes: A61K 38/07 Tetrapeptides
• CPC Class Codes: A61K 38/08 Peptides having 5 to 11 amino acids A61K38/043 - A61K38/046 take precedence
• CPC Class Codes: A61K 47/542 Carboxylic acids, e.g. a fatty acid or an amino acid
• CPC Class Codes: A61K 47/547 Chelates, e.g. Gd-DOTA or Zinc-amino acid chelates; Chelate-forming compounds, e.g. DOTA or ethylenediamine being covalently linked or complexed to the pharmacologically- or therapeutically-active agent
• CPC Class Codes: 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
• CPC Class Codes: A61K 49/0002 General or multifunctional contrast agents, e.g. chelated agents
• CPC Class Codes: A61K 51/04 Organic compounds
• CPC Class Codes: A61P 13/08 of the prostate
• CPC Class Codes: A61P 13/10 of the bladder
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: C07K 5/021 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 Class Codes: C07K 5/06113 Asp- or Asn-amino acid
• CPC Class Codes: C07K 5/10 Tetrapeptides
• CPC Class Codes: C07K 5/1019 with the first amino acid being basic

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.

Claims

1. A conjugate having the formula

2. A pharmaceutical composition comprising a conjugate having a formula

3. The pharmaceutical composition of claim 2, wherein the conjugate or the pharmaceutically acceptable salt thereof is present in a therapeutically effective amount for treating a disease in a host animal caused by a pathogenic population of cells, said cells expressing prostate-specific membrane antigen (PSMA).

4. The pharmaceutical composition of claim 2, further comprising one or a plurality of additional therapeutically active compounds.

5. The pharmaceutical composition of claim 2, further comprising one or a plurality of pharmaceutically acceptable carriers.

6. The pharmaceutical composition of claim 2, further comprising one or a plurality of pharmaceutically acceptable diluents.

7. The pharmaceutical composition of claim 2, further comprising one or a plurality of pharmaceutically acceptable excipients.

8. The pharmaceutical composition of claim 2, further comprising a component selected from the group consisting of an additional therapeutically active compound, a pharmaceutically acceptable carrier, a pharmaceutically acceptable diluent, a pharmaceutically acceptable excipient, and a combination thereof.

9. The pharmaceutical composition of claim 2, wherein the pharmaceutical composition is in bulk form.

10. The pharmaceutical composition of claim 2, e pharmaceutical composition is a unit dose.