US 11,236,059 B2 · Targeted cytotoxic ratjadone derivatives and conjugates thereof

Abstract

The present invention is directed to novel natural product-derived ratjadone-based compounds useful as payloads (or toxins) in drug-conjugates constructs with cell target binding moieties (CTBM) and payload-linker compounds useful in connection with drug conjugates. The present invention further relates to new ratjadone compositions including the aforementioned payloads, payload-linkers and drug conjugates, and methods for using these payloads, payload-linkers and drug conjugates, to treat pathological conditions including cancer, inflammatory and infectious diseases.

Claims16

Dependent claims

A compound according to Formula I

wherein:
one of R1 and R2 is NHR9 and one is selected from H and OH;
R3, R4 and R5 are independently of one another selected from the group that consists of H, CH3 and C2H5;
R6 is CH3 or C2H5;
R7 and OR are independently of one another selected from the group that consists of H, CH3, C2H5, n-C3H7,
and
R9 is H.

4 more elements

Dependencies are inferred from the claim text.

Facts

Application

16/637,257Filed 8 Aug 2018

Priority

EP 171855989 Aug 2017

Published

US 2020/0239426 A130 Jul 2020

Granted

1 Feb 2022

Term ends

Not estimatedThe source records don’t support an estimate.

Classification11 codes

C07D 309/30
With hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals,…:…
C07D 309/32
Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings: having…
A61K 47/551
The modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug: one of the codrug's…
A61K 47/64
The modifying agent being a protein, peptide or polyamino acid: drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying…

Targeted cytotoxic ratjadone derivatives and conjugates thereof

Life of this patent

Targeted cytotoxic ratjadone derivatives and conjugates thereof

Life of this patent

Abstract

Claims16