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COMPOSÉS PHARMACEUTIQUES
专利权人:
SAREUM LIMITED
发明人:
READER, John Charles
申请号:
EPEP2013/068198
公开号:
WO2015/032423A1
申请日:
2013.09.03
申请国别(地区):
EP
年份:
2015
代理人:
摘要:
The invention provides a compound which is an amide of the formula (2): or a salt or stereoisomer thereof; wherein: R7 is selected from chlorine and fluorine; R3, R4, R5 and R6 are each independently selected from hydrogen, fluorine and chlorine; n is 0, 1 or 2; Q1 is selected from C(=O), S(=O) and SO2; A is absent or is NR2; R1 is selected from: - hydrogen; - an optionally substituted C1-6 non-aromatic hydrocarbon group; and - 3- to 7-membered non-aromatic carbocyclic and heterocyclic rings containing one or two heteroatom ring members selected from O, N and S, and bridged bicyclic heterocyclic rings of seven to nine ring members of which one or two are nitrogen atoms, the carbocyclic and heterocyclic rings and bridged bicyclic heterocyclic rings being optionally substituted; R2 is selected from hydrogen and C1-4 alkyl; or NR1R2 forms an optionally substituted 4- to 7-membered non-aromatic nitrogen- containing heterocyclic ring optionally containing a second heteroatom ring member selected from nitrogen and oxygen; with the provisos that: (i) no more than two of R3 to R6 are other than hydrogen; and (ii) when R7 and R6 are both fluorine, then one of R3 to R5 is chlorine or fluorine and/or R1-A-Q1 is selected from ethylsulfonyl and isopropylsulfonyl. Also provided are pharmaceutical compositions containing the compounds and their therapeutic uses.L'invention concerne un composé qui est un amide de la formule (2) : ou un sel ou un stéréoisomère de celui-ci; où : R7 est choisi parmi chlore et fluor; R3, R4, R5 et R6 sont chacun indépendamment choisis parmi hydrogène, fluor et chlore; n est 0, 1 ou 2; Q1 est choisi parmi C(=O), S(=O) et SO2; A est absent ou représente NR2; R1 est choisi parmi : -hydrogène, -un groupe hydrocarboné non aromatique en C1-6 facultativement substitué; et -des noyaux carbocycliques et hétérocycliques non aromatiques à 3 à 7 chaînons contenant un ou deux chaînons de cycle hétéroatomes choisis parmi O, N et S, et des noyaux hétérocycliques bicy
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