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US 2017/0362229 A1Published application
Crystalline solid forms of a bet inhibitor
AssigneeIncyte Corporation
InventorsShili Chen, Zhongjiang Jia, Pingli Liu, Lei Qiao, Yongzhong Wu, Jiacheng Zhou, Qun Li
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Abstract
The present application relates to crystalline solid forms of an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of diseases such as cancer.
Claims53
A solid form of a compound having the formula:
- wherein the solid form is crystalline.
A process of preparing Form I of Compound 1:
- comprising precipitating Form I from a solution comprising Compound 1 and a solvent.
A process of preparing Form II of Compound 1:
- comprising precipitating Form II from a solution comprising Compound I and a solvent.
A process of preparing Compound 8:
- comprising reacting Compound 7:
- with Compound 9:
- in the presence of P2 and B2, wherein P2 is a transition metal catalyst and B2 is a base.
A process of preparing Compound 7:
- comprising reacting Compound 6:
- with 4,4,4′,4′,5,5,5′,5′-octamethyl-2,2′-bi(1,3,2-dioxaborolane) in the presence of P3 and B3, wherein P3 is a transition metal catalyst and B3 is a base.
A compound which is
- or a salt thereof.
Dependencies are inferred from the claim text.