JAK inhibitors containing a 4-membered heterocyclic amide
AssigneeTheravance Biopharma R&D IP, LLC
InventorsPaul R. Fatheree, Gary E. L. Brandt, Cameron Smith, Steven D. E. Sullivan, Lori Jean Van Orden
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Abstract
The invention provides compounds of formula (I): which contain a 4-membered heterocyclic amide, where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.
Claims20
A method of inhibiting a Janus kinase in a mammal comprising administering to the mammal a compound of formula (I):
- wherein:
- R1 is selected from hydrogen, C1-3alkyl, and C3-6cycloalkyl, and X is —C(O)R2,
- wherein
- R2 is —NR13R14, wherein
- R13 and R14, taken together with the nitrogen atom to which they are attached, form a 4-membered heterocyclyl, wherein the heterocyclyl is optionally substituted with —NR5R6 and R7,
- R5 and R6 are independently C1-3alkyl or R5 and R6, taken together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclyl optionally including an oxygen atom, and
- R7 is C1-3alkyl, optionally substituted with a 5- or 6-membered heterocyclyl containing one nitrogen atom,
- or a pharmaceutically-acceptable salt thereof.
A method of inhibiting a Janus kinase in a mammal comprising administering to the mammal a compound of formula (II):
- wherein:
- R1 is C1-3alkyl, and
- R2 is
- wherein
- R5 and R6 are independently C1-3alkyl or R5 and R6, taken together, form —(CH2)4-5—, and R7 is hydrogen or C1-3alkyl,
- or a pharmaceutically-acceptable salt thereof.
Dependencies are inferred from the claim text.