Title:
1-OXO-ISOINDOLINE-4-CARBOXAMIDE AND 1-OXO-1,2,3,4-TETRAHYDROISOQUINOLINE-5-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2009/044019
Kind Code:
A9
Abstract:
The invention relates to 1-oxo-isoindoline-4-carboxamide and 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamide derivatives of general formula (I) where: R1 = H, C1-C10alkyl, C3-C7cycloalkyl, (CH2)n-(C1-C6)alkenyl, (CH2)n-(C1-C6)alkynyl, (C1-C6)alkyl-Z-(C1-C6)alkyl, where Z = a heteroatom chosen from O, N and S(O)m, or R1 = COOR, S(O)mR, aryl or aralkyl, R2 = one or more of H, halogen, C1-C6alkyl, C3-C7cycloalkyl, C1-C6alkenyl, C1-C6alkynyl, C1-C6alkyl-Z-(C1-C6)alkyl, where Z = a heteroatom chosen from O, N and S(O)m, or R2 = halo(C1-C6)alkyl, C1-C6alkoxy, halo(C1-C6)alkoxy, hydroxy, nitro, cyano, amino, NR7R8, COOR, CONR7R8, O- CO(C1-C6)alkyl, S(O)m-NR7R8, aryl; R3 = trifluoromethyl;R4 and R5 independently = H, or R4 and R5 together with the carbon to which they are attached form a saturated ring with 3 to 6 C and optionally containing O to 1 heteroatoms chosen from O, N or S; R6 = H,halogen, C1- C6alkyl, C3-C7cycloalkyl, C3-C7cycloalkyl-(C1-C6)alkyl, halo(C1-C6)alkyl, nitro, amino, NR7R8, COOR, NR7(SO2)R8, CONR7R8, aryl or heterocycle; X = C1-C2alkylene; m = a whole number from O to 2 and n = a whole number from1 to 6. The invention further relates to a method for preparation and therapeutic application thereof as ß-secretase inhibitors for the treatment of neurodegenerative disorders such as Alzheimers.
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Inventors:
BAUDOIN BERNARD (FR)
EVERS MICHEL (FR)
GENEVOIS-BORELLA ARIELLE (FR)
KARLSSON ANDREAS (FR)
MALLERON JEAN-LUC (FR)
MATHIEU MAGALI (FR)
EVERS MICHEL (FR)
GENEVOIS-BORELLA ARIELLE (FR)
KARLSSON ANDREAS (FR)
MALLERON JEAN-LUC (FR)
MATHIEU MAGALI (FR)
Application Number:
PCT/FR2008/001110
Publication Date:
October 14, 2010
Filing Date:
July 25, 2008
Export Citation:
Assignee:
SANOFI AVENTIS (FR)
BAUDOIN BERNARD (FR)
EVERS MICHEL (FR)
GENEVOIS-BORELLA ARIELLE (FR)
KARLSSON ANDREAS (FR)
MALLERON JEAN-LUC (FR)
MATHIEU MAGALI (FR)
BAUDOIN BERNARD (FR)
EVERS MICHEL (FR)
GENEVOIS-BORELLA ARIELLE (FR)
KARLSSON ANDREAS (FR)
MALLERON JEAN-LUC (FR)
MATHIEU MAGALI (FR)
International Classes:
C07D209/46; A61K31/4035; A61K31/472; A61P25/00; C07D217/24; C07D413/12
Attorney, Agent or Firm:
MOREL-PECHEUX, Muriel (Département Brevets174 avenue de France, Paris, FR)
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