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PHARMACEUTICALLY ACTIVE PYRAZINE DERIVATIVES
专利权人:
SENTINEL ONCOLOGY LIMITED
发明人:
Robert George Boyle,Richard Justin Boyce
申请号:
US15461268
公开号:
US20170247341A1
申请日:
2017.03.16
申请国别(地区):
US
年份:
2017
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 R8.Also provided are pharmaceutical compositions containing the compounds and methods for making the compounds.
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