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US 2014/0350006 A1Published application
Pyrazolopyridine Derivatives, Preparation Process Therefor And Therapeutic Use Thereof
AssigneeSanofi
InventorsChantal Alcouffe, Kirsten Bjegarde, Jacques Mauger
Life of this patent
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Abstract
The invention relates to FGF-inhibiting pyrazolopyrimidine derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.
Claims21
Compound corresponding to formula (I):
- in which:
- the representation of the pyrazole ring indicates that the substituent R4 may be borne either by the nitrogen alpha to the pyridine ring (I′) or by the nitrogen alpha to the carbon bearing a substituent R3 (I″) such that:
- wherein
- R1 represents an aryl, pyridyl or pyrazolyl group optionally substituted with one or more substituents chosen from:
- a halogen atom,
- a group —CF3,
- a cyano group,
- a group —NR6R6′ in which R6 and R6′ are as defined below,
- a group —NR10R11 such that R10 and R11 form, together with the nitrogen atom to which they are attached, a saturated or unsaturated heterocycle comprising one or more heteroatoms chosen from a nitrogen atom and an oxygen atom, optionally substituted with one or more substituents chosen from a halogen atom and a linear or branched alkyl group,
- a group —CH2NR10R11 such that R10 and R11 form, together with the nitrogen atom to which they are attached, a saturated or unsaturated heterocycle comprising one or more heteroatoms chosen from a nitrogen atom and an oxygen atom,
- a group —COR12 in which R12 represents a hydroxyl group or a group —NR6R6′, in which R6 and R6′ are as defined below,
- a group —CONR7R7′ such that R7 and R7′ form, together with the nitrogen atom to which they are attached, a heterocycloalkyl comprising one or more heteroatoms chosen from a nitrogen atom and an oxygen atom,
- a group —(CH2)pNHSO2CH3 in which p represents 0 or 1,
- a group —OR13 in which R13 represents a linear group (C1-C3)alkyl,
- a group (C1-C3)alkyl,
- or R1 represents a bicyclic group of formula A below:
- in which R8 and R9 form, together with the carbon atoms to which they are attached, a saturated or unsaturated heterocycle comprising one or more heteroatoms chosen from a nitrogen atom, an oxygen atom and a sulfur atom, optionally substituted with one or more linear alkyl groups,
- R2 represents a group:
- —CF3,
- —CHF2,
- —COOH, or
- —CONHR5, in which R5 is as defined below,
- R3 represents:
- a hydrogen atom,
- an aryl group, optionally substituted with an alkoxymethyl group,
- a cycloalkyl group, or
- a heteroaryl group chosen from thienyl and pyridyl groups,
- R4 represents:
- a hydrogen atom,
- a linear group (C1-C3)alkyl, optionally substituted with a group —NR6R6′ in which R6 and R′6 are as defined below or a group —NR7R7′′ such that R7 and R7′ form, together with the nitrogen atom to which they are attached, a heterocycloalkyl comprising one or more heteroatoms chosen from a nitrogen atom and an oxygen atom,
- R5 represents:
- a hydrogen atom,
- a linear group (C1-C3)alkyl, optionally substituted with a pyridyl group, or
- an aromatic group chosen from aryl and pyridyl,
- R6 and R′6, which may be identical or different, represent a hydrogen atom or a linear alkyl group,
- in the form of the base or of an acid-addition or base-addition salt.
33 more elements
(canceled)
15-17. (canceled)
Dependencies are inferred from the claim text.