Benzoxazines and related nitrogen-containing heterobicyclic...

C - Chemistry – Metallurgy – 07 – D

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C07D 265/36 (2006.01) A61K 31/538 (2006.01) A61K 31/5415 (2006.01) A61P 9/12 (2006.01) C07D 279/16 (2006.01) C07D 413/04 (2006.01)

Patent

CA 2636985

The present invention relates to a compound, useful as a mineralocorticoid receptor-modulating agent, of the following formula [I]: (see formula I) wherein Ring A is a benzene ring optionally having a substituent(s) other than R1 or a nitrogen-containing 6-membered aromatic heterocyclic ring optionally having a substituent(s) other than R1, R1 is a group of the formula: R a SO2NH-, R a SO2NH-CH2- or (R b)(R c)NSO2-, R a is an alkyl group, a cycloalkyl group, an amino group optionally substituted by an alkyl group(s), an optionally substituted aryl group, or an optionally substituted heteroaryl group, R b and R c are the same or different and are each a hydrogen atom, an alkyl group or a cycloalkyl group, R2 and R3 are the same or different and are each a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an alkenyl group, a carboxyl group, an alkoxycarbonyl group, an optionally substituted carbamoyl group or an optionally substituted aryl group, or both R2 and R3 combine together with the adjacent carbon atom to form a saturated or unsaturated cyclic group (said cyclic group optionally containing the same or different one or two heteroatom(s) selected from an oxygen atom, a sulfur atom and a nitrogen atom), X is an oxygen atom, a sulfur atom, a methylene group or a group of the formula: - NR4-, R4 is a hydrogen atom, an alkyl group, an optionally substituted aralkyl group or an acyl group, Y is a group of the formula: -C(=O)-, -C(=S)- or -CH(R5)-, R5 is a hydrogen atom, an alkyl group or an optionally substituted aryl group, Ar is an optionally substituted aryl group or an optionally substituted heteroaryl group, and Q is a single bond, an alkylene group or an alkenylene group, or a pharmaceutically acceptable salt thereof excluding certain specified compounds.

La présente invention concerne un composé utile en tant qu'agent de modulation de récepteurs de minéralocorticoïdes, de formule (I); dans laquelle: le noyau A est un noyau benzène ayant éventuellement un/des substituant(s) autre(s) que R1; R1 est un groupe de formule RaSO2NH-; Ra est un groupe alkyle; R2 et R3 sont chacun un atome d'hydrogène, un groupe phényle, un groupe alkyle éventuellement substitué; X est un atome d'oxygène; Y est un groupe de formule -C(=O)- ; Ar est un groupe aryle éventuellement substitué ou un groupe hétéroaryle éventuellement substitué; Q est une liaison simple, un groupe alkylène; ou un sel pharmaceutiquement acceptable dudit composé.

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