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US 8,283,359 B2Granted
Thieno-pyridine derivatives as MEK inhibitors
AssigneeUCB Pharma S.A.
InventorsMartin Clive Hutchings, Sarah Catherine Archibald, Daniel Christopher Brookings, Jeremy Martin Davis, James Andrew Johnson, Barry John Langham, Judi Charlotte Neuss
Life of this patent
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Abstract
A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.
Claims16
A compound of Formula (I), or a pharmaceutically acceptable salt or N-oxide thereof:
- wherein
- R1 is hydrogen, halogen or C1-6 alkyl;
- R2 is halogen or C1-6 alkyl;
- R3 is hydrogen, cyano, —CO2Ra, —CONRbRc or —CON(ORb)Rc;
- Ra is C1-6 alkyl;
- Rb is hydrogen, optionally substituted C1-6 alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted C3-7 cycloalkyl(C1-6)alkyl, optionally substituted aryl, optionally substituted aryl(C1-6)alkyl, optionally substituted C3-7 heterocycloalkyl, optionally substituted C3-7 heterocycloalkyl(C1-6)alkyl, optionally substituted heteroaryl or optionally substituted heteroaryl(C1-6)alkyl;
- Rc is hydrogen or C1-6 alkyl optionally substituted with one or more hydroxyl groups;
- or
- Rb and Rc are taken together with the nitrogen atom to which they are attached to form a cyclic group selected from optionally substituted azetidinyl, optionally substituted pyrrolidinyl, optionally substituted piperidinyl, optionally substituted morpholinyl, optionally substituted thiomorpholinyl, optionally substituted piperazinyl, optionally substituted homopiperidinyl, optionally substituted homomorpholinyl and optionally substituted homopiperazinyl.
6 more elements
Dependencies are inferred from the claim text.