US 10,537,645 B2Granted

Protein-polymer-drug conjugates

AssigneeMersana Therapeutics, Inc.

InventorsAleksandr V. Yurkovetskiy, Mao Yin, Timothy B. Lowinger, Joshua D. Thomas, Charles E. Hammond, Cheri A. Stevenson, Natalya D. Bodyak, Patrick R. Conlon, Dmitry R. Gumerov

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Abstract

Auristatin compounds and conjugates thereof are provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently an Auristatin compound. LD and LP are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

Claims20

Dependent claims

A polymeric scaffold of Formula (Ia) useful to conjugate with an antibody:

wherein:
the scaffold comprises poly(l-hydroxymethylethylene hydroxymethyl-formal) (PHF) having a molecular weight ranging from 2 kDa to 40 kDa;
each occurrence of D is independently a KSP inhibitor;
LD1 is a carbonyl-containing moiety;
each occurrence of
in
is independently a first linker that contains a biodegradable bond so that when the bond is broken, D is released in an active form for its intended therapeutic effect;
and the
in
between LD1 and D denotes direct or indirect attachment of D to LD1;
each occurrence of
is independently a second linker not yet connected to an antibody, in which LP2 is a moiety containing a functional group that is yet to form a covalent bond with a functional group of the antibody, and the
between LD1 and LP2 denotes direct or indirect attachment of LP2 to LD1, and each occurrence of the second linker is distinct from each occurrence of the first linker;
m is an integer from 1 to 300,
m1 is an integer from 1 to 140,
m2 is an integer from 1 to 40,
m3 is an integer from 1 to 18, and
the sum of m, m1, m2 and m3 ranges from 15 to about 300.

15 more elements

Dependencies are inferred from the claim text.

Facts

Application: 15/902,540Filed 22 Feb 2018 · continuation
Priority: 10 Jun 2011
Published: US 2018/0243428 A130 Aug 2018
Granted: 21 Jan 2020
Term ends: Not estimatedThe source records don’t support an estimate.

Classification17 codes

A61K 47/59
The modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule: obtained otherwise than by…
A61K 31/4745
Ortho- or peri-condensed with heterocyclic ring systems: condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
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…
A61K 47/6803
Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent: drugs conjugated to an antibody or…

Family

Application61/495,771Us provisional application · filed 10 Jun 2011
Application61/501,000Us provisional application · filed 24 Jun 2011
Application61/513,234Us provisional application · filed 29 Jul 2011
Application61/566,935Us provisional application · filed 5 Dec 2011
Application61/605,618Us provisional application · filed 1 Mar 2012
Application61/618,499Us provisional application · filed 30 Mar 2012
Application13/493,899Parent of this division · filed 11 Jun 2012
Application13/944,561Parent of this continuation · filed 17 Jul 2013
US 8,685,383 B2Parent of this division · filed 1 Apr 2014
Application14/457,955Parent of this continuation · filed 12 Aug 2014
US 8,808,679 B2Parent of this continuation · filed 19 Aug 2014
Application15/001,119Parent of this continuation · filed 19 Jan 2016
US 9,254,339 B2Parent of this continuation · filed 9 Feb 2016
US 2018/0243428 A1Pre-grant publication · published 30 Aug 2018
US 9,943,609 B2Parent of this continuation
Application13/944,561Parent of this division
US 2012/0321583 A1Published application
US 2013/0309192 A1Published application
US 2015/0064130 A1Published application
US 2016/0220696 A1Published application
US 10,537,645 B2This patent

From the US filing history. Foreign family members aren’t listed.