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US 2007/0191380 A1Published application
Kinase inhibitor scaffolds and methods for their preparation
AssigneeIrm LLC
InventorsSheng Ding, Qiang Ding, Nathanael Gray
Life of this patent
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Abstract
General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.
Claims16
A compound having the following Formula:
- wherein
- R is selected from the group consisting of a 5- or 6-membered heteroaryl and a 9- or 10-membered 6,5- or 6,6-fused heteroaryl, containing from 1-4 nitrogen atoms, optionally substituted with 1-2 groups independently selected from the group consisting of hydrogen, C1-6alkyl, aryl, C1-6alkylaryl, C3-8cycloalkyl, heterocycle, heteroaryl, C1-6alkylhydroxy, C1-6alkoxy and NR4R4;
- R1 is a member selected from the group consisting of phenyl and benzyl, substituted on the aromatic ring with from 1-4 substituents independently selected from the group consisting of C1-6alkyl, C1-6alkoxy, C1-6alkylhydroxy, C1-6alkylamine, C1-6aminoalkyl, halo and heterocycle;
- L is selected from the group consisting of —O—, —NR2— and a bond;
- each R2 is independently a member selected from the group consisting of hydrogen and C1-4alkyl;
- R3 is independently a member selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted heteroalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocycloalkyl, halogen and alkoxy groups;
- or
- R2 and R3 taken together form a 3-8 membered heterocyclic ring containing from 1-2 heteroatoms selected from the group consisting of N and O, optionally substituted with 1-2 members independently selected from the group consisting of C1-4alkyl, C1-4alkylhydroxy, C1-4alkoxy and C1-4alkylamine;
- R4, if present, is a member selected from the group consisting of optionally substituted alkyl, optionally substituted heteroalkyl and acyl groups;
- and
- all pharmaceutically acceptable salts, hydrates, solvates, isomers and prodrugs thereof.
8 more elements
Dependencies are inferred from the claim text.