Biologically active molecules, conjugates thereof, and therapeutic uses

Patent metadata

Field	Value
Publication number	US-12378258-B2
Application number	US-202217733974-A
Country	US
Kind code	B2
Filing date	Apr 29, 2022
Priority date	Mar 15, 2013
Publication date	Aug 5, 2025
Grant date	Aug 5, 2025

Abstract

The present disclosure relates to linker compounds that are useful in covalently linking biologically active molecules with Ligands. The disclosed compounds also relate to biologically active molecules and Ligand conjugates, wherein the biologically active molecule is linked to the Ligand through a linker. The disclosure further provides compositions comprising biologically active molecule-ligand conjugates, methods of modifying abnormal cell growth and methods of treatment using the conjugates or the compositions.

First claim

What is claimed is:

1. A method for reducing, retarding, or stopping an abnormal cell growth comprising contacting one or more cells growing abnormally with a compound, in an amount sufficient to retard, reduce, or stop the abnormal cell growth, and wherein the compound has the following formula

wherein A 3a is —CH 2 —, —CH 2 CH 2 —, or —CH 2 CH 2 CH 2 CH 2 —; and
R 4a is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, heteroaryl, or heterocyclyl.

2. The method of claim 1 , wherein A 3a is —CH 2 CH 2 —.

3. The method of claim 2 , wherein R 4a is a substituted or unsubstituted alkyl.

4. The method of claim 3 , wherein the compound is

5. The method of claim 1 , wherein the one or more cells growing abnormally is within a mammal.

6. The method of claim 1 , wherein the one or more cells growing abnormally comprise a tumor cell.

7. The method of claim 1 , wherein the one or more cells growing abnormally comprise a colon cancer cell.

8. The method of claim 1 , wherein the one or more cells growing abnormally comprise a lung cancer cell.

9. The method of claim 1 , wherein A 3 is —CH 2 CH 2 —.

10. The method of claim 1 , further comprising administering sequentially or consecutively an additional therapy.

11. The method of claim 10 , wherein the additional therapy is radiation therapy, chemotherapy, or a combination of both.

12. The method of claim 1 , further comprising administering at least one additional therapeutic agent.

Assignees

• Regeneron Pharma

Inventors

• Nittoli Thomas

Classifications

• A61K31/5365

  ortho- or peri-condensed with heterocyclic ring systems · CPC title

• A61K47/68033

  the drug being a maytansine · CPC title

• A61K47/6849

  the antibody targeting a receptor, a cell surface antigen or a cell surface determinant · CPC title

• A61K47/6869

  the tumour determinant being from a cell of the reproductive system: ovaria, uterus, testes, prostate · CPC title

• A61K47/6855

  the tumour determinant being from breast cancer cell · CPC title