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US 10,851,102 B2Granted
Imidazole and triazole containing bicyclic compounds as JAK inhibitors
AssigneeTheravance Biopharma R&D IP, LLC
InventorsRobert Murray McKinnell, Erik Fenster, Tom M. Lam, Anthony Francesco Palermo
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Abstract
The invention provides compounds of formula (I): or a pharmaceutically-acceptable salt thereof, wherein the variables are defined in the specification, that are inhibitors of JAK kinases, particularly JAK3. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat gastrointestinal and other inflammatory diseases.
Claims19
A compound of formula (I):
- or a pharmaceutically acceptable salt thereof, wherein
- X1 and X2 are each independently selected from N and CH;
- is selected from the group consisting of
- Ra, Rb, Rc, and Rf are each independently selected from the group consisting of H and C1-3 alkyl;
- Rd, Re, Rg, Rh, Ri, Rj, Rl, Rm, Rn and Ro are each independently selected from the group consisting of H and C1-3 alkyl wherein the C1-3 alkyl group may be optionally substituted with 1 to 3 halogens;
- A is selected from the group consisting of
- (a) a 4 to 8 membered monocyclic heterocyclic group containing one nitrogen atom and optionally containing one additional heteroatom selected from N, S, S(O)2 and O, and
- (b) a 6 to 10 membered multicyclic heterocyclic group containing one nitrogen atom and optionally containing one additional heteroatom selected from N, S, S(O)2 and O,
- wherein L is linked to a carbon atom in A and A is optionally substituted with 1 to 3 Rk groups;
- each Rk is independently selected from the group consisting of F, CN, C1-3 alkoxy, and C1-3 alkyl, wherein the C1-3 alkyl group may be optionally substituted with OH, OMe or 1 to 3 halogens;
- R1 is selected from the group consisting of:
- wherein Rp and Rq are each independently selected from the group consisting of H, C3-5 cycloalkyl and C1-6 alkyl;
- R2 is selected from the group consisting of H, Cl, OMe, Me and F;
- R3 is selected from the group consisting of H, Me, Et, CF3, OMe, and F;
- R4 is selected from the group consisting of H, Me, OMe, Cl, and F;
- and
- R5 is selected from the group consisting of H, Me, Et, and F.
14 more elements
A compound of formula:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.