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US 2011/0237641 A1Published application
Substituted pyrazoles, compositions containing these, method of production and use
AssigneeSanofi-Aventis
InventorsKirsten BJERGARDE, Mark DODSON, Jacques MAUGER, Anil NAIR, Marcel PATEK, Michel TABART
Life of this patent
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Abstract
The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.
Claims23
A compound of formula (I):
- wherein:
- 1) A and Ar are independently selected from the group consisting of:
- aryl, heteroaryl, substituted aryl, and substituted heteroaryl;
- 2) L is O—CO—NH;
- 3) R1 is selected from the group consisting of:
- H, R6, COR6, SO2R6, in which R6 is chosen from H, OR7, NR8R9, alkyl, cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl, in which R7 is chosen from H, phenyl and alkyl, and in which R9 and R9 are independently selected from the group consisting of H, alkyl, cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl, or alternatively R9 and R9 are linked together to form a saturated 5- to 8-membered ring containing from 0 to 3 heteroatoms chosen from O, S and N;
- 4) X is selected from the group consisting of:
- O and NH;
- 5) R3 is selected from the group consisting of:
- H, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl;
- 6) R4a is selected from the group consisting of:
- H and (C1-C4)alkyl;
- 7) R4b is selected from the group consisting of:
- H and (C1-C4)alkyl;
- 8) R5 is selected from the group consisting of:
- H, halogen, R10, CN, O(R10), OC(O)(R10), OC(O)N(R10)(R11), OS(O2)(R10), N(R10)(R11), N═C(R10)(R11), N(R10)C(O)(R11), N(R10)C(O)O(R11), N(R12)C(O)N(R10)(R11), N(R12)C(S)N(R10)(R11), N(R10)S(O2)(R11), C(O)(R10), C(O)O(R10), C(O)N(R10)(R11), C(═N(R11))(R10), C(═N(OR11))(R10), S(R10), S(O)(R10), S(O2)(R10), S(O2)O(R10), S(O2)N(R10)(R11);
- in which each R10, R11, R12 is independently selected from the group consisting of H, alkyl, alkylene, alkynyl, aryl, heteroaryl, cycloalkyl, heterocyclyl, substituted alkyl, substituted alkylene, substituted alkynyl, substituted aryl, substituted heteroaryl, substituted cycloalkyl and substituted heterocyclyl.
14 more elements
Dependencies are inferred from the claim text.