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US 11,691,962 B2Granted
Therapeutic compounds and compositions
AssigneeeXIthera Pharmaceuticals, Inc.
InventorsBertrand L. Chenard, Yuelian Xu, Frans L. Stassen, Neil J. Hayward, Zhiyao Teng
Life of this patent
Estimating the term…
Abstract
The present invention provides compounds that inhibit Factor XIa or kallikrein and pharmaceutically acceptable salts thereof and compositions thereof. The present invention also provides methods of using these compounds and compositions.
Claims14
A compound of formula (II):
- or a pharmaceutically acceptable salt thereof, wherein
- R1 is hydrogen or —NR8R9;
- Ra is C1-6 alkyl, C1-6 haloalkyl, halo, cyano, or —OR6;
- Rb is hydrogen or C1-6 alkyl;
- R2 is optionally substituted 5-membered heteroaryl or optionally substituted 5-membered heterocyclyl;
- R3 is hydrogen, C1-6 alkyl, or C1-6 haloalkyl;
- R4 is C1-6 alkyl, C1-6 haloalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one, two, or three independent occurrences of halo, C1-6 alkyl, C1-6 haloalkyl, cyano, or —OR6;
- R5 is hydrogen, C1-6 alkyl, C1-6 haloalkyl, cycloalkyl, or aryl, wherein the cycloalkyl or aryl is optionally substituted with one, two, or three independent occurrences of halo, C1-6 alkyl, C1-6 haloalkyl, cyano, or —OR6 or
- R4 and R5, taken together with the carbon atom to which they are attached form a ring;
- R6 is hydrogen, C1-6 alkyl, or C1-6 haloalkyl;
- each R8 and R9 is independently hydrogen, C1-6 alkyl, —C(O)R10, or —C(O)OR10;
- R10 is C1-6 alkyl or C1-6 haloalkyl;
- Rx is —O or absent, wherein when Rx is —O, the nitrogen atom of the pyridyl ring is positively charged and Rx is negatively charged, thereby forming a pyridyl N-oxide;
- m is 0, 1, 2, or, 3;
- and
- n is 0 or 1, wherein if n is 0, then R5 is hydrogen and R4 is absent.
13 more elements
Dependencies are inferred from the claim text.