Pyrimidine compounds as jak kinase inhibitors
AssigneeTheravance Biopharma R&D IP, LLC
InventorsRyan Hudson, Jennifer Kozak, Melissa Fleury, Paul R. Fatheree, Anne-Marie Beausoleil, Dante D. Podesto, Xiaojun Huang
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Abstract
The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of JAK kinases. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.
Claims23
1-22. (canceled)
A method of treating a gastrointestinal inflammatory disease in a mammal the method comprising administering to the mammal a compound of formula (I):
- wherein
- R1 is selected from:
- (a) —S(O)2R4, wherein R4 is selected from:
- C1-4alkyl, wherein C1-4alkyl is optionally substituted with —CN, —OC1-3alkyl, or C3-6cycloalkyl,
- heterocyclyl containing 4 to 6 ring atoms including one nitrogen atom, wherein any heterocyclyl is optionally substituted with —CN,
- C3-6cycloalkyl,
- pyridinyl, wherein pyridinyl is optionally substituted with fluoro, and
- phenyl,
- (b) C1-4alkyl, wherein C1-4alkyl is optionally substituted with —CN,
- or
- pyridinyl, wherein pyridinyl is optionally substituted with —CN;
- and
- (c) —C(O)R5, wherein R5 is selected from:
- C1-4alkyl, wherein C1-4alkyl is optionally substituted with C3-6cycloalkyl, or with one or two fluoro,
- —OC1-4alkyl,
- C3-6cycloalkyl, and
- morpholinyl;
- R2 is hydrogen or methyl;
- R3 is C1-3alkyl and
- n is 1 or 2;
- or a pharmaceutically-acceptable salt thereof.
A method of treating an inflammatory disease of the skin in a mammal, the method comprising applying a pharmaceutical composition comprising a compound of formula (I):
- wherein
- R1 is selected from:
- (a) —S(O)2R4, wherein R4 is selected from:
- C1-4alkyl, wherein C1-4alkyl is optionally substituted with —CN, —OC1-3alkyl, or C3-6cycloalkyl,
- heterocyclyl containing 4 to 6 ring atoms including one nitrogen atom, wherein any heterocyclyl is optionally substituted with —CN,
- C3-6cycloalkyl,
- pyridinyl, wherein pyridinyl is optionally substituted with fluoro, and
- phenyl;
- (b) C1-4alkyl, wherein C1-4alkyl is optionally substituted with —CN,
- or
- pyridinyl, wherein pyridinyl is optionally substituted with —CN;
- and
- (c) —C(O)R5, wherein R5 is selected from:
- C1-4alkyl, wherein C1-4alkyl is optionally substituted with C3-6cycloalkyl, or with one or two fluoro,
- —OC1-4alkyl,
- C3-6cycloalkyl, and
- morpholinyl;
- R2 is hydrogen or methyl;
- R3 is C1-3alkyl and
- n is 1 or 2;
- or a pharmaceutically-acceptable salt thereof to the skin of the mammal.
A method of treating a gastrointestinal inflammatory disease in a mammal, the method comprising administering to the mammal a compound of formula:
- or a pharmaceutically-acceptable salt thereof.
Dependencies are inferred from the claim text.