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US 2010/0249110 A1Published application
Substituted pyrazolo-pyrimidine compounds
AssigneeArQule, Inc.
InventorsManish Tandon, Jianqiang Wang, Nivedita Namdev
Life of this patent
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Abstract
The present invention relates to substituted pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.
Claims31
A compound having formula I or Ia:
- or a pharmaceutically acceptable salt or ester thereof, wherein:
- n is 1 or 2;
- R1 is H, unsubstituted or substituted C1-C6 alkyl, C(O)R11, C(O)OR11 or C(O)NR11R12;
- R11 and R12 are each independently H or -Q1-Ti;
- R2 is H or -Q2-T2;
- R3 is H or -Q3-T3;
- R4 is NRN1RN2, SRs or S(O)2RS;
- RN1 and RN2 are each independently H or -Q41-T41, or RN1 and RN2, together with the nitrogen atom they attach to, form a 5- or 6-member ring which optionally comprises 1-4 heteroatoms selected from N, O and S and is optionally substituted with 1-5 Rf;
- each Rf is independently H or -Q42-T42, or any two adjacent Rf, together with the atoms they attach to, form a 5- or 6-member ring which optionally comprises 1-4 heteroatoms selected from N, O and S and is optionally substituted;
- RS is H or unsubstituted or substituted C1-C6 alkyl;
- Q1, Q2, Q3, Q41 and Q42 are each independently a bond or unsubstituted or substituted C1-C6 alkyl linker;
- T1 is H, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C1-C6 alkoxy, unsubstituted or substituted C6-C10 aryl, unsubstituted or substituted C6-C10 aryloxy, unsubstituted or substituted heteroaryl comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S, unsubstituted or substituted C3-C10 carbocycle or unsubstituted or substituted heterocycle comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S;
- T2 is H, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C6-C10 aryl, unsubstituted or substituted heteroaryl comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S, unsubstituted or substituted C3-C10 carbocycle or unsubstituted or substituted heterocycle comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S;
- T3 is H, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C6-C10 aryl, unsubstituted or substituted heteroaryl comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S, unsubstituted or substituted C3-C10 carbocycle, unsubstituted or substituted heterocycle comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S, C(O)R31 or C(O)OR31;
- T41 is H, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C1-C6 alkoxy, unsubstituted or substituted amino, unsubstituted or substituted C1-C6 alkylamino, unsubstituted or substituted di-C1-C6 alkylamino, unsubstituted or substituted C6-C10 aryl, unsubstituted or substituted C6-C10 aryloxy, unsubstituted or substituted heteroaryl comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S, unsubstituted or substituted C3-C10 carbocycle or unsubstituted or substituted heterocycle comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S;
- T42 is H, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C6-C10 aryl, unsubstituted or substituted heteroaryl comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S, unsubstituted or substituted C3-C10 carbocycle, unsubstituted or substituted heterocycle comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S, C(O)R42 or C(O)OR42;
- R31 is H or unsubstituted or substituted C1-C6 alkyl;
- and
- R42 is H, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C6-C10 aryl, unsubstituted or substituted heteroaryl comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S, unsubstituted or substituted C3-C10 carbocycle or unsubstituted or substituted heterocycle comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S.
16 more elements
Dependencies are inferred from the claim text.