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US 2022/0017538 A1Published application
Thioester prodrugs of macrocycles as inhibitors of histone deacetylases
AssigneeOnKure, Inc.
InventorAnthony D. Piscopio
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Abstract
The present invention provides a novel macrocyclic prodrug compound of general Formula (I), a pharmaceutical composition comprising a compound of Formula (I), and a method for treating diseases mediated by HDAC enzymes by administering a compound of Formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, A and Z are defined herein.
Claims21
-17. (canceled)
A method for preparing a thiol compound of formula 6
- comprising reacting a chloride compound of formula 1
- with a thioacid,
- followed by hydrolysis of the resulting thioester with a reducing agent to provide the compound of formula 6.
A method for preparing a compound of formula 4
- wherein:
- Ra and Rb are H;
- Rx is H or lower alkyl;
- and
- Ry is H or lower alkyl,
- the method comprising reacting a chloride compound 1
- with a thioacid of formula 2
- to provide a compound of formula 3
- wherein:
- Ra is Boc;
- Rb is H;
- Rx is H or lower alkyl;
- and
- Ry is H or lower alkyl,
- followed by deprotection of the compound of formula 3 to provide the compound of formula 4.
12 more elements
Dependencies are inferred from the claim text.