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US 2010/0249108 A1Published application
Substituted dipyrido-pyrimido-diazepine and benzo-pyrido-pyrimido compounds
AssigneeArQule, Inc.
InventorsManish Tandon, Yanbin Liu, Nivedita Namdev, Mark A. Ashwell, Rocio Palma
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Abstract
The present invention relates to substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
Claims21
A compound having formula I:
- or a pharmaceutically acceptable salt or ester thereof, wherein:
- X is R or NR2R3;
- X1 is N or CRX1;
- X2 is N or CRX2;
- X3 is N or CRX3,
- provided that at least one of X1, X2 and X3 is N;
- R is H, hydroxyl, or -QR-TR;
- RX1, RX2 and RX3 are each independently H or unsubstituted or substituted C1-C6 alkyl;
- R1 is H or -Q-T;
- R2 and R3 are each independently H or -Q-T, or R2 and R3, together with the atom to which they attach, form a 5-, 6- or 7-membered ring which optionally comprises 1-4 heteroatoms selected from N, O and S and is optionally substituted;
- Q and QR are each independently a bond or unsubstituted or substituted C1-C6 alkyl linker;
- T 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 C6-C10 aryl-C1-C6 alkyl, 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;
- TR 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 C6-C10 aryl-C1-C6 alkyl, 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;
- p and q are each independently 0, 1, 2 or 3;
- each R4 is independently unsubstituted or substituted C1-C6 alkyl;
- each R5 is independently unsubstituted or substituted C1-C6 alkyl;
- and
- R6 is H or unsubstituted or substituted C1-C6 alkyl.
15 more elements
Dependencies are inferred from the claim text.