- INDAZOLES AS WNT/B-CATENIN SIGNALING PATHWAY INHIBITORS AND THERAPEUTIC USES THEREOF
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Described herein are methods of treating a disorder or disease in which aberrant Wnt signaling is implicated, with a variety of compounds, including Wnt inhibitor compounds. More particularly, it concerns the use of an indazole compound or analogs thereof
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- IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES
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The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+-O- or CR3; Y is N, N+-O- or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
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Page/Page column 121-122
(2010/11/17)
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- Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents
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A series of 3,5-disubstituted pyrazolo[3,4-b]pyridine cyclin-dependent kinase (CDK) inhibitors was synthesized. These compounds showed potent and selective CDK inhibitory activities and inhibited in vitro cellular proliferation in cultured human tumor cel
- Lin, Ronghui,Connolly, Peter J.,Lu, Yanhua,Chiu, George,Li, Shengjian,Yu, Yang,Huang, Shenlin,Li, Xun,Emanuel, Stuart L.,Middleton, Steven A.,Gruninger, Robert H.,Adams, Mary,Fuentes-Pesquera, Angel R.,Greenberger, Lee M.
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p. 4297 - 4302
(2008/02/11)
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- Indazolecarboxamide derivatives, preparation and use thereof as CDK1, CDK2 and CDK4 inhibitors
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Compound corresponding to general formula (I): [image] in which, R1 represents a hydrogen or halogen atom, an NH2, NHR2, NHCOR2, NO2, CN, CH2NH2 and CH2NHR2; or alternatively R1 represents an optionally substituted phenyl or an optionally substituted heteroaromatic group; Ar represents an optionally substituted phenyl group or an optionally substituted heteroaromatic group; n represents 0, 1, 2 or 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. Application in therapy.
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Page/Page column 15
(2008/06/13)
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- SYNTHESIS OF 5-BROMO-4-METHYL-PYRIDIN-3-YLMETHYL)-ETHYL-CARBAMIC ACID TERT-BUTYL ESTER
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The present invention relates to novel synthetic methods for the preparation of intermediates of 3{5-[3-(4,6-Difluoro-1H-benzoimidazol-2-yl)-1H-indazol-5-yl]-4-methyl-pyridin-3-ylmethyl}-ethyl-amine.
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Page/Page column 8
(2010/11/08)
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