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US 2009/0275585 A1Published application
Novel Compounds and Therapeutic Use Thereof for Protein Kinase Inhibition
OwnerZhanggui Wuinventor
Life of this patent
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Abstract
Novel compound having the following formula: Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same. The novel compounds of the present invention are found to inhibit protein kinases, especially Checkpoint kinase Chk1/Chk2.
Claims17
A compound of formula I.
- in the form of a racemate, a pure stereoisomer, or in the form of a mixtures of stereoisomers in any mixing ratio, in the illustrated form or in the form of an acid, a base or in the form of a salt or a solvate,
- wherein,
- X═CH;
- N;
- S, O
- Y═CH;
- S;
- N, O
- W═CH, N, CR20
- L=Ch, N, CR20,
- where R20 is selected from —OR21;
- —NR21R22;
- —CN;
- —SR21;
- —S(O)R21;
- —S(O)2R21;
- —S(O)2NR21R22;
- —C(O)NR21R22;
- —N(R21)C(O)R22;
- —N(R21)S(O)2R22;
- N(R21)C(O)N(R22R23);
- —N(R21)C(O)OR22;
- heteroatom including F, Cl, Br, and I;
- alkyl (C1-C8);
- cycloalkyl (C3-C8) without and with substitutions by alkyls (C1-C8), cycloalkyls (C3-C8), aryls, heteroaryls;
- aryl with or without substitution;
- heteroaryl with or without substitution;
- aryalkyl with or without substitution;
- heterocyclyl with or without substitution;
- heteterocyclylalkyl with or without substitution;
- alkenyl with or without substitution;
- alkynyl with or without substitution;
- wherein R21, R22 and R22 is independently chosen from H, alkyl (C1-C8), cycloalkyls (C3-C8), aryl with or without substitution, alkylaryl with or without substitutions, heteroaryl with or without substitution;
- R1 is selected from following groups:
- where X CH2, NH, S, or O;
- R8—H, —NH2, —OH, —N(R4, R5), —C(R4R5)1-7NR6R7, —C(R4R5)1-7OR6, —N(R4)NR5R6
- R4, R5, R6, R7═H, alkyls (C1-C6), cycloalkyls (C3-C8) with or without nuclear heteroatoms such as O, S, N, aryls (selected from unsubstituted and substituted aromatics), or heteroaromatics (selected from unsubstituted and substituted heteroaromatics),
- R9, R10, R11, R12, R13H, alkyls (C1—C6), cycloalkyls (C3-C8) with or without nuclear heteroatoms such as O, S, N, unsubstituted or substituted aryls, or unsubstituted or substituted heteroaromatics,
- R2 is selected from a group consisting of H, OH, NH2, OR4, NR14R15, alkyl, aryl, heteroaryl, cycloalkyl, arylalkyl, heterocyclyl, heterocyclylalkyl, alkenyl, alkynyl,
- where R14, R15 and R16 are selected from:
- H;
- heteroatom such as F, Cl, Br, I;
- alkyl (C1-C8);
- cycloalkyl (C3-C8) without and with substitutions:
- substitutions are selected from alkyls (C1-C8), cycloalkyls (C3-C8), aryls, heteroaryls;
- —OR17;
- —SR17;
- —NR17R18;
- —S(O)R17;
- —S(O)2R17;
- —S(O)2NR17R18;
- —C(O)NR17R18;
- —N(R17)C(O)R18;
- —N(R17)S(O)2R18;
- —N(R17)C(O)N(R18R19);
- —N(R17)C(O)OR18;
- Aryl with or without substitution, heteroaryl with or without substitution, aryalkyl with or without substitution, heterocyclyl with or without substitution, heteterocyclylalkyl with or without substitution, alkenyl with or without substitution, alkynyl with or without substitution;
- where R17, R18 and R17 chosen from H, alkyl (C1-C8), cycloalkyls (C3-C8), aryl with or without substitution, alkylaryl with or without substitutions, heteroaryl with or without substitution;
- or R14, R15 and R16 can be part of ring which is fused containing 0-3 heteroatoms selected from N, O, and S.
- and
- R3 is selected from a group consisting of H, alkyl, aryl, heteroaryl, cycloalkyl, arylalkyl, heterocyclyl, heterocyclylalkyl, alkenyl, alkynyl.
58 more elements
Dependencies are inferred from the claim text.