825622-13-7

Upstream product

• 825622-12-6 4-(2,6-difluoro-benzoylamino)-1-(tetrahydro-pyran-2-yl)-1H-pyrazole-3-carboxylic acid methyl ester 

Downstream Products

• 825619-56-5 2,6-difluoro-N-[3-formyl-1-(tetrahydro-pyran-2-yl)-1H-pyrazol-4-yl]-benzamide 

Relevant academic research and scientific papers

PYRAZOLE DERIVATIVES AS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES

The invention provides a compound of the formula (I): for use in medicine: or salts or tautomers or N-oxides or solvates thereof; wherein R1 is an optionally substituted heterocyclic group having from 3 to 12 ring members provided that the cyclic group joined to the pyrazole contains at least one heteroatom selected from N, O or S; A is a bond or -Y-(B)n-; B is C=O, NRg(C=O) or O(C=O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; n is 0 or 1; Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from optionally substituted carbocyclic and heterocyclic groups having from 3 to 12 ring members or an optionally substituted C1-8 hydrocarbyl group; with the proviso that R1 is not formula (II): where X, R3’ and R4’ are defined in the claims.

3,4-DISUBSTITUTED PYRAZOLES AS CYCLIN DEPENDENT KINASES (CDK) OR AURORA KINASE OR GLYCOGEN SYNTHASE 3 (GSK-3) INHIBITORS

The invention provides compounds of the formula (I); or salts or solvates or N-oxides thereof; wherein: Rq is selected from groups (a), (b) and (c); the asterisk denoting the point of attachment to the pyrazole ring; X is N or CR5; X" is NR4', O, S or S(O); A is a bond or -(CH2)m-(B)n-; B is C=O, NRg(C=O) or O(C=O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R0 is hydrogen or, together with NRg when present, forms a group -(CH2)p- wherein p is 2 to 4; and R1 to R6b are as defined in the description. Compounds of the formula (I) have activity as inhibitors of CDK, aurora and GSK-3 kinases are useful in treating or preventing diseases such as cancers that are mediated by the said kinases.