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US 10,766,903 B2Granted
Piperidine derivatives as inhibitors of ubiquitin specific protease 7
AssigneeAlmac Discovery Limited
InventorsColin O'Dowd, Tim Harrison, Peter Hewitt, Shane Rountree, Miel Hugues, Frank Burkamp, Linda Duncan Jordan, Matthew Helm, Fabio Broccatelli, James John Crawford, Lewis Gazzard, Ingrid Wertz, Wendy Lee
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Abstract
The present invention concerns the identification of inhibitors of ubiquitin specific protease 7 (USP7), and methods of use thereof.
Claims22
A compound of formula (I):
- or a pharmaceutically acceptable salt, tautomer, stereoisomer or N-oxide derivative thereof, wherein:
- R1 is H, OH or an optionally substituted alkyl group;
- R2 is an optionally substituted C1-C6 alkyl, optionally substituted C2-C6 alkenyl, optionally substituted C2-C6 alkynyl, optionally substituted C3-C6 cycloalkyl, optionally substituted C4-C6 alkylcycloalkyl, optionally substituted C4-C6 aryl, optionally substituted C3-C6 heteroaryl, optionally substituted C4-C8 aryloxy, optionally substituted C7-C10 arylalkyl or optionally substituted C5-C10 heteroarylalkyl group;
- and
- Q is selected from the group consisting of:
- wherein:
- R5a is H, halo, optionally substituted C1-C6 alkyl, or optionally substituted amino;
- R5b is H, halo, optionally substituted C1-C6 alkyl, optionally substituted C2-C6 alkynyl, benzyl, optionally monosubstituted C3-C6 heteroaryl, optionally substituted C3-C6 heterocycloalkyl, optionally substituted C1-C6 alkoxy, NR′R″, or RaNR′R″,
- wherein Ra is C1-C6 alkyl or C2-C6 alkenyl;
- and
- wherein R′ and R″ are each independently selected from H, oxo-substituted C1-C6 alkyl, hydroxy-substituted C1-C6 alkyl, optionally substituted C1-C6 alkoxy, optionally substituted C3-C6 cycloalkyl, optionally substituted C1-C7 alkylamine, optionally substituted C2-C7 alkenylamine, optionally substituted C3-C10 heterocycloalkyl, optionally substituted C4-C10 aryl, optionally substituted C3-C10 heteroaryl, optionally substituted C5-C10 alkylaryl, optionally substituted C4-C10 alkylheterocycloalkyl, and C4-C6 alkylheteroaryl, or wherein R′ and R″ together form an optionally substituted C3-C8 heterocycloalkyl including the N to which they are attached;
- R6a is H, optionally substituted C1-C6 alkyl, optionally substituted amino, optionally substituted C4-C6 aryl, optionally substituted C1-C6 sulfide, optionally substituted C1-C6 sulfonyl, or optionally substituted amino;
- R6b is H, cyano, halo, optionally substituted C1-C6 alkyl, optionally substituted C2-C6 alkenyl, optionally substituted C2-C6 alkynyl, optionally substituted C3-C6 cycloalkyl, optionally substituted C4-C6 cycloalkenyl, optionally substituted C2-C6 ynol, optionally substituted C4-C6 aryl, optionally substituted C3-C6 heteroaryl, optionally substituted amino;
- R7a is H;
- R7b is H or optionally substituted C4-C6 aryl;
- or wherein R7a and R7b together form an optionally substituted C1-C6 aryl group together with the carbons to which they are attached;
- R8a is H or is optionally substituted C4-C6 aryl;
- R9a is Cl, F, Br, I, or cyano;
- and
- R9b is H, optionally substituted C1-C6 alkyl, optionally substituted C4-C6 aryl, optionally substituted C3-C8 heteroaryl, C1-C6 alkoxy.
17 more elements
Dependencies are inferred from the claim text.