IP Library › Patent Application 18782621
Patent Application
App. No. 18/782,621

CDK9 Inhibitors and Polymorphs Thereof For Use As Agents For Treatment of Cancer

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Quick Facts
Patent No.
US None
App. No.
18/782,621
Abstract

A crystalline form and/or polymorph of a compound having the following structure (I), including tautomeric and zwitterionic forms thereof, are provided: Methods associated with preparation and use of the polymorphs, and pharmaceutical compositions comprising the same are also provided. Also provided are methods for preparing a compound having formula (I), or a salt, tautomer or zwitterionic form thereof.

Claims (19)

1 . (canceled)

2 . A method for preparing crystalline Form B of a compound having the following structure (II):

the method comprising:

contacting a compound having the following structure (V):

or a tautomer, salt or zwitterionic form thereof, with an acid in a solvent, thereby preparing the crystalline Form B of the compound having structure (II).

3 . The method of claim 2 , wherein the acid has at least one pK a value that is less than about 5.

4 . The method of claim 2 , wherein the acid has a pK a value of greater than about 1.

5 . The method of claim 2 , wherein the acid is an organic acid.

6 . The method of claim 5 , wherein the organic acid is selected from maleic acid, acetic acid, citric acid and propionic acid.

7 . The method of claim 6 , wherein the organic acid is maleic acid.

8 . The method of claim 2 , wherein the solvent is tetrahydrofuran, methanol, ethanol, butanol, methyl ethyl ketone, acetone, diisopropylether, ethyl acetate or water, or a combination of any of the foregoing.

9 . The method of claim 2 , wherein the solvent is an organic solvent.

10 . The method of claim 2 , wherein the solvent comprises tetrahydrofuran or wherein the solvent is a mixture of methanol and acetone.

11 . A method for preparing crystalline Form B of a compound having the following structure (II):

the method comprising:

(a) contacting a compound having the following structure (IV):

or a tautomer or salt thereof, with di-tert-butylhalophosphonate in the presence of an amine base, thereby forming a compound having the following structure (V):

or a tautomer or salt thereof; and

(b) contacting the compound having structure (V), or a tautomer or salt thereof, in an organic solvent, with an acid having at least one pK a value that is less than about 5 and a pK a value of greater than about 1 in an organic solvent, thereby preparing crystalline Form B of a compound having structure (II).