US 8,940,784 B2 · Water-soluble CC-1065 analogs and their conjugates

Abstract

This invention relates to novel analogs of the DNA-binding alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.

Claims2

Dependent claims

A compound which is

or the (1R,10S) isomer, the (1R,10R) isomer, or the (1S,10S) isomer of one of these, or a mixture of two or more of said isomers.

Dependencies are inferred from the claim text.

Facts

Application

12/223,682Filed 2 Feb 2007

Priority

WO PCT/NL2006/0500202 Feb 2006

Published

US 2009/0318668 A124 Dec 2009

Granted

27 Jan 2015

Term ends

Not estimatedThe source records don’t support an estimate.

Classification14 codes

C07D 209/60
[b]- or [c]-condensed: naphtho [b] pyrroles; Hydrogenated naphtho [b] pyrroles
A61K 31/404
Condensed with carbocyclic rings, e.g. carbazole: indoles, e.g. pindolol
A61K 31/454
Containing further heterocyclic ring systems: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/5377
1,4-Oxazines, e.g. morpholine: not condensed and containing further heterocyclic rings, e.g. timolol

Water-soluble CC-1065 analogs and their conjugates

Life of this patent

Water-soluble CC-1065 analogs and their conjugates

Life of this patent

Abstract

Claims2