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Pharmaceutically Active Pyrazine Derivatives
专利权人:
发明人:
Robert George Boyle,Richard Justin Boyce
申请号:
US14358678
公开号:
US20140323484A1
申请日:
2012.11.16
申请国别(地区):
US
年份:
2014
代理人:
摘要:
The invention provides compounds which inhibit or modulate the activity of Chk-1 kinase and which are useful in the treatment of cancer. The compounds have the general formula (1):and salts, N-oxides and tautomers thereof, wherein m is 2, 3 or 4 n is 0 or 1 Q1 is selected from a bond C(═O) S(O) SO2 and an alkylene chain of 1 to 4 carbon atoms in length between the moiety R4 and the nitrogen atom. N, wherein (a) one or more of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with one or two C1-4 alkyl groups and/or (b) one carbon atom of the 1 to 4 carbon atoms of the alkylene chain may optionally be replaced by a cyclopropane-1,1-diyl or 1,1-cyclobutanediyl group and/or (c) one carbon atom of the 1 to 4 carbon atoms of the alkylene chain may optionally be replaced by C(═O), S(O), or SO2, provided that Q1 contains no more than one C(═O), S(O), or SO2 moiety R1 is selected from hydrogen, methyl, chlorine and bromine R2 is selected from hydrogen, methyl, methoxy and a group —(O)p-Q2-R5 R3 is selected from hydrogen, a group Hyd1, a group —O-Hyd1 and a group —(O)p-Q2-R5 provided that when one of R2 and R3 is —(O)p-Q2-R5, the other is selected from hydrogen, methoxy and methyl and R4 is selected from amino, NH-Hyd2, N(Hyd2)2 and a non-aromatic carbocyclic or heterocyclic ring of 4 to 7 ring members containing 0, 1, 2 or 3 heteroatom ring members selected from O, N and S and oxidised forms thereof the carbocyclic or heterocyclic ring being optionally substituted with one or two substituents R9.Also provided are pharmaceutical compositions containing the compounds and methods for making the compounds.
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