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1-oxo-isoindoline-4-carboxamides and 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamides derivatives, their preparation and their therapeutic application.
专利权人:
Sanofi-Aventis
发明人:
Andreas Karlsson,Arielle Genevois-Borella,Bernard Baudoin,Jean-Luc Malleron,MAGALI MATHIEU,Michel Evers
申请号:
BRPI0813624
公开号:
BRPI0813624A2
申请日:
2008.07.25
申请国别(地区):
BR
年份:
2019
代理人:
摘要:
1-Oxo-isoindoline-4-carboxamide and 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamide compounds (I) and their base or acid addition salts, hydrates or solvates are new. 1-Oxo-isoindoline-4-carboxamide and 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamide compounds of formula (I) and their base or acid addition salts, hydrates or solvates are new. R 1>;H, 1-10C alkyl, 3-7C cycloalkyl, (CH 2) n-(1-6C)alkenyl, (CH 2) n-(1-6C)alkynyl, 1-6C alkyl-Z-(1-6C alkyl), aryl or aralkyl (all optionally substituted by halo, 1-6C alkyl, 3-7C cycloalkyl, halo(1-6C)alkyl, 1-6C alkoxy, halo(1-6C)alkoxy, NR 7>;R 8>;, nitro, cyano, OR, COOR, CONR 7>;R 8>;or S(O) mNR 7>;R 8>;), COOR or S(O) mR; Z : heteroatom comprising O, N or S(O) m; R 2>;halo(1-6C)alkyl, halo(1-6C)alkoxy, OH, 1-6C alkoxy, NO 2, CN, NH 2, NR 7>;R 8>;, COOR, CONR 7>;R 8>;, OCO(1-6C)alkyl, S(O) mNR 7>;R 8>;or aryl (all optionally substituted by one or more halo, 1-6C alkyl, 3-7C cycloalkyl, halo(1-6C)alkyl, (1-6C)alkoxy, halo(1-6C)alkoxy, NR 7>;R 8>;, NO 2, CN, OR, COOR, CONR 7>;R 8>;or S(O) mNR 7>;R 8>;), H (preferred), halo, 1-6C alkyl, 3-7C cycloalkyl, (1-6C)alkenyl, (1-6C)alkynyl or 1-6C alkyl-Z-(1-6C alkyl); R 3>;CF 3; either R 4>;, R 5>;H; or CR 4>;R 5>;ring containing 3-6 carbon atoms (optionally saturated and optionally containing 0 or 1 heteroatom comprising O, N or S); R 6>;H (preferred), halo, 1-6C alkyl, 3-7C cycloalkyl, 3-7C cycloalkyl-1-6C alkyl, NO 2, NH 2, NR 7>;R 8>;, COOR, NR 7>;(SO 2)R 8>;, CONR 7>;R 8>;or aryl; either R 7>;, R 8>;, R : H, 1-6C alkyl, 3-7C cycloalkyl, 3-7C cycloalkyl-1-6C alkyl, aryl, aryl(1-6C)alkylene or COR; or R 7>;R 8>;ring containing 5-7 carbon atoms (optionally saturated and substituted by heteroatom of O, N or S(O) m); X : 1-2C alkylene (optionally substituted by one or more 1-6C alkyl group); m : 0-2; and n : 1-6. Where the carbon carrying the benzyl substituted by R2 is absolute configuration S and the
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