Small molecule drug conjugates

Patent metadata

Field	Value
Publication number	US-10016511-B2
Application number	US-201715431310-A
Country	US
Kind code	B2
Filing date	Feb 13, 2017
Priority date	Feb 3, 2014
Publication date	Jul 10, 2018
Grant date	Jul 10, 2018

Abstract

A binding moiety (B) for Carbonic Anhydrase IX (CAIX), the binding moiety comprising:

The binding moiety is univalent, bivalent, or multivalent. A targeted therapeutic agent may comprise the binding moiety. The invention also includes a method for treating a disease expressing elevated levels of CAIX by administering the targeted therapeutic agent.

First claim

The invention claimed is:

1. A binding moiety (B) for Carbonic Anhydrase IX (CAIX), wherein the binding moiety comprises:

wherein R is selected from the group consisting of:

wherein R′ is H or C1-C7 alkyl, C1-C7 alkenyl, or C1-C7 heteroalkyl, optionally substituted with one, two or three substituents, and preferably R′ is methyl.

2. The binding moiety (B) according to claim 1 , wherein the binding moiety is univalent, bivalent or multivalent.

3. A targeted therapeutic agent comprising the binding moiety according to claim 1 or 2 .

4. The targeted therapeutic agent of claim 3 , wherein said binding moiety further comprises a drug moiety.

5. The targeted therapeutic agent of claim 4 , wherein the drug moiety is a cytotoxic agent.

6. A method of treating a disease expressing elevated levels of CAIX, the method comprising administering the targeted therapeutic agent of claim 4 .

7. A method of treating a disease expressing elevated levels of CAIX, the method comprising administering the targeted therapeutic agent of claim 5 .

8. The method of claim 6 , wherein the disease is renal cell carcinoma.

9. The targeted therapeutic agent of claim 3 , wherein said binding moiety further comprises a label.

10. A method of diagnosing a disease displaying elevated levels of CAIX, the method comprising administering the targeted therapeutic agent of claim 9 .

Assignees

• Philochem Ag
• Eth Zuerich

Inventors

• Krall Nikolaus
• Decurtins Willy
• Neri Dario
• Scheuermann Jörg
• Wichert Moreno

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• C07B2200/05

  Isotopically modified compounds, e.g. labelled · CPC title

• A61K38/05

  Dipeptides · CPC title

• A61K51/08

  Peptides, e.g. proteins {, carriers being peptides, polyamino acids, proteins} · CPC title

• A61K31/535

  having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines · CPC title