Androgen receptor PROTACS
AssigneeGlaxoSmithKline Intellectual Property Development Limited
InventorsChristopher Patrick Tinworth, Laura Trulli
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Abstract
Certain Androgen receptor PROTAC (PROteolysis TArgeting Chimera) compounds contain a series of 2,4-dioxotetrahydropyrimidinyl derivatives that bind cereblon. The PROTAC compounds may be viewed as being comprised of an androgen receptor binding moieties, a linker and a cereblon binding moiety or degron. Medical uses of these PROTAC compounds are also disclosed.
Claims28
A compound of formula (V), a tautomer of a compound of formula (V), or a salt thereof
- wherein:
- X1 is N or C—R1 wherein R1 is selected from the group consisting of H, halo, and C1-4haloalkyl;
- X4 is C—R2 or N wherein R2 is selected from the group consisting of H, halo and C1-3haloalkyl;
- X2 and X3 are independently selected from N or CH;
- X6 and X5 are independently selected from N or C, wherein when X6 is N, X5 is C;
- p and q are independently 0 or 1;
- X7 is CR6;
- R6, R7, R8, R9, R10, R11, R12, R13, R14 and R17 are independently selected from H or halo;
- R16 is H, OH or halo;
- R18, R19 and R20 are independently H, halo or C1-3haloalkyl;
- R22 is selected from the group consisting of halo and OR23
- R21 is independently H or methyl, and
- R23 is C1-3alkyl.
A compound that is N-((1r,3r)-3-(4-cyano-3-methoxyphenoxy)-2,2,4,4-tetramethylcyclobutyl)-4-(4-((4-(4-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-1H-pyrazolo[4,3-c]pyridin-1-yl)piperidin-1-yl)methyl)piperidin-1-yl)-3-fluorobenzamide or a tautomer, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.