Biologically active molecules, conjugates thereof, and therapeutic uses

Patent metadata

Field	Value
Publication number	US-11345715-B2
Application number	US-202016740312-A
Country	US
Kind code	B2
Filing date	Jan 10, 2020
Priority date	Mar 15, 2013
Publication date	May 31, 2022
Grant date	May 31, 2022

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

3. The compound of claim 2 , wherein R 4a is an unsubstituted alkyl.

4. The compound of claim 3 , having the structure

5. A compound having a structure selected from the group consisting of

6. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable carriers, diluents, or excipients.

7. A pharmaceutical composition comprising the compound of claim 4 , or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable carriers, diluents, or excipients.

8. A pharmaceutical composition comprising the compound of claim 5 , or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable carriers, diluents, or excipients.

Assignees

• Regeneron Pharma

Inventors

• Nittoli Thomas

Classifications

• A61K47/68033

  the drug being a maytansine · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61K47/6849

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

• C07D507/00 Primary

  Heterocyclic compounds containing a condensed beta-lactam ring system, not provided for by groups C07D463/00, C07D477/00 or C07D499/00 - C07D505/00; Such ring systems being further condensed · CPC title

• A61K47/6855

  the tumour determinant being from breast cancer cell · CPC title