- Identification of 3-amido-4-anilinoquinolines as potent and selective inhibitors of CSF-1R kinase
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3-Amido-4-anilinoquinolines are potent and highly selective inhibitors of CSF-1R. Their synthesis and SAR is reported, along with initial efforts to optimize the physical properties and PK through modifications at the quinoline 6- and 7-positions.
- Scott, David A.,Balliet, Carrie L.,Cook, Donald J.,Davies, Audrey M.,Gero, Thomas W.,Omer, Charles A.,Poondru, Srinivasu,Theoclitou, Maria-Elena,Tyurin, Boris,Zinda, Michael J.
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scheme or table
p. 697 - 700
(2009/08/15)
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- Derivatives of quinoline as inhibitors for MEK
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1. A compound of formula (I) or a pharmaceutically acceptable salt thereof. wherein: n is 0-1; X and Y are independently selected from -NH-, -O-, -S-, or -NR8- where R8 is alkyl of 1-6 carbon atoms and X may additionally comprise a CH2 group; R7 is a group (CH2)mR9 where m is 0,or an integer of from 1-3 and R9 is a substituted aryl group, an optionally substituted cycloalkyl ring of up to 10 carbon atoms, or an optionally substituted heterocyclic ring or an N-oxide of any nitrogen containing ring; R6 is a divalent cycloalkyl of 3 to 7 carbon atoms, which may be optionally further substituted with one or more alkyl of 1 to 6 carbon atom groups; or is a divalent pyridinyl, pyimidinyl, or phenyl ring; wherein the pyridinyl, pyrimidinyl, or phenyl ring may be optionally further substituted with one or more specified groups; R1, R2, R3 and R4 are each independently selected from hydrogen or various specified organic groups. Compounds are useful as pharmaceuticals for the inhibition of MEK activity.
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Page/Page column 41
(2010/02/14)
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