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US 11,958,856 B2Granted
Substituted 1,2,3,8,9,9a-hexahydro-5H-pyrrolo[1,2-a]azepin-5-ones as factor XIa inhibitors
AssigneeJanssen Pharmaceutica NV
InventorsGuozhang Xu, Zhijie Liu
Life of this patent
Estimating the term…
Abstract
A compound of formula (I) or a pharmaceutically acceptable salt or stereoisomer thereof: Pharmaceutical compositions containing said compounds, and the use of said compounds in the treatment and/or prophylaxis of thromboembolic disorders, inflammatory disorders and diseases or conditions in which plasma kallikrein activity is implicated.
Claims16
A compound of formula (I):
- or a pharmaceutically acceptable salt or stereoisomer thereof,
- wherein:
- Q is C(O)NHR6 or
- R′ is halogen, CN, NO2, C1-4 alkyl, C1-4 fluoroalkyl, C(O)C1-4 alkyl, NRARB, OH, OC1-4 alkyl, OC1-4 fluoroalkyl, C3-6 cycloalkyl, phenyl, or 5- or 6-membered heterocyclyl, wherein the C3-6 cycloalkyl, phenyl, or 5- or 6-membered heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, C1-4 alkyl, C1-4 fluoroalkyl, C1-4 alkylene-NRARB, C(O)OH, C(O)OC1-4 alkyl, NRARB, OH, OC1-4 alkyl, OC1-4 fluoroalkyl, C3-7 cycloalkyl, and 5- or 6-membered heterocyclyl;
- each R2 is independently F, Cl, CH3, or OCH3;
- R4 is H or halogen;
- R5 is phenyl or 5- or 6-membered heteroaryl, wherein the phenyl or 5- or 6-membered heteroaryl is optionally substituted with one or two substituents independently selected from the group consisting of halogen, C1-4 alkyl, C1-2, fluoroalkyl, C1-2, hydroxyalkyl, C(O)NRCRD, C(O)OH, C(O)OC1-4 alkyl, NRARB, and NRCC(O)C1-2 alkyl;
- R6 is phenyl or 9- or 10-membered heteroaryl, wherein the phenyl or 9- or 10-membered heteroaryl is optionally substituted with one or two substituents independently selected from the group consisting of halogen, C1-4 alkyl, C1-2, fluoroalkyl, C1-2, hydroxyalkyl, C(O)NRERF, C(O)OH, C(O)OC1-4 alkyl, Nine, and NRCC(O)C1-2 alkyl;
- each RA is independently H or C1-4 alkyl;
- each RB is independently H or C1-4 alkyl;
- each RC is independently H, C1-2 alkyl, or C1-4 hydroxyalkyl;
- each RD is independently H, C1-2 alkyl, or C1-4 hydroxyalkyl;
- each RE is independently H or C1-4 alkyl;
- each RF is independently H or C1-4 alkyl;
- and
- a is 0, 1, 2, or 3.
13 more elements
Dependencies are inferred from the claim text.