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US 2007/0167469 A1Published application
Pyrido-pyrimidine derivatives, preparation thereof, and therapeutic use thereof
AssigneeSanofi-Aventis
InventorsBernard Bourrie, Pierre Casellas, Samir Jegham, Pierre Perreaut
Life of this patent
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Abstract
The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I) and acid addition salts, hydrates and solvates thereof, as well as in the form of enantiomers, diastereoisomers and mixtures thereof. The disclosure also concerns methods for preparing said derivatives, pharmaceutical compositions containing a compound of general formula (I), and their therapeutic use.
Claims19
A compound of formula (I):
- wherein:
- R1 is selected from the group consisting of (C1-C6)alkyl, (C3-C7)cycloalkyl, CH2COR4, phenyl and phenyl substituted with one or more substituents independently selected from hydroxy, halogen, or (C1-C6)alkyl;
- R4 represents a hydroxyl, (C1-C4)alkoxy, amino, (C1-C4)alkylamino or di(C1-C4)alkylamino group;
- Ar1 represents a radical selected from:
- R5 represents a cyano, hydroxy(C1-C4)alkyl, (C1-C6)alkoxy(C1-C4)alkyl group or a (CH2)nNR7R8, CO2R7, CONHNR7R8, CONR7R8, CONR8OR9, (CH2)nNR7COR8 or (CH2)nNR7COOR8 group;
- R6 represents a hydrogen atom, a (C1-C4)alkyl group or one of the values given for R5;
- or R5 and R6 are bonded together to form a cycle comprising 0 to 2 heteroatoms selected from N and O, said cycle containing 4 to 7 chain links optionally being substituted with one or more substituents independently selected from halogen, (C1-C4)alkyl, halogenated (C1-C4)alkyl, hydroxy(C1-C4)alkyl, (C1-C4)alkoxy(C1-C4)alkyl, (CH2)mNR7R8, or a tert-butoxycarbonyl group;
- R7 and R8 each independently represent a substituent selected from H, phenyl, (C1-C4)alkyl, (C1-C4)alkyl-OH, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-NH2, (C1-C4)alkyl-(C3-C7)cycloalkyl, C(═NH)NH2, SO2(C1-C6)alkyl, and SO2-phenyl;
- R8 may also represent a tert-butoxycarbonyl or benzyloxycarbonyl group;
- or R7 and R8 together with the nitrogen atom to which they are bonded constitute an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl radical, said radical being unsubstituted or substituted one or more times with a (C1-C6)alkyl, (C1-C4)alkyl-OH, COO(C1-C6)alkyl or F group;
- R9 represents a hydrogen atom or a (C1-C4)alkyl group;
- Ar2 represents a phenyl group which is unsubstituted or substituted 1 to 5 times with substituents independently selected from a halogen atom or a (C1-C4)alkyl, trifluoromethyl or (C1-C4)alkoxy group;
- n represents 1, 2 or 3;
- m represents 0, 1, 2 or 3;
- or an acid addition salt thereof, or a hydrate or solvate of said compound or said salt.
12 more elements
Dependencies are inferred from the claim text.