C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 487/04 (2006.01) A61K 31/4985 (2006.01) A61K 31/551 (2006.01) A61P 25/00 (2006.01) C07D 207/36 (2006.01) C07D 241/06 (2006.01) C07D 241/08 (2006.01) C07D 243/08 (2006.01)
Patent
CA 2694288
The invention relates to 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-6-carboxamide and 2,3,4,5-tetrahydropyrrolo[1,2-a][1,4]-diazépine-7-carboxamide derivatives of general formula (I), where R1 = H, C1-C10alkyl, C3-C7 cycloalkyl, (CH2)n-(C1-C6)alkenyl, (CH2)n-(C1-C6)alkynyl, C1-C6alkyl-Z-(C1-C6)alkyl, where Z = a heteroatom chosen from O, N and S(O)m, or R1 = a group COOR, S(O)mR, aryl or aralkyl; R2 = one or more groups from H, halogen, C1-C6alkyl, C3-C7cycloalkyl, C1-C6alkenyl, C1-C6alkynyl, C1-C6alkyl-Z-(C1-C6)alkyl, where Z = a heteroatom from O, N and S(O)m, or R2 = halo(C1-C6)alkyl, halo(C1-C6)alkoxy, hydroxy, C1-C6alkoxy, nitro, cyano, amino, NR7R8, COOR, C(O)NR7R8, O-C(O)(C1-C6)alkyl, S(O)m-NR7R8, aryl; R3 = trifluoromethyl; R4 and R5 independently = H, or R4 and R5 form a saturated ring with the carbon to which they are attached with 3 to 6 C optionally containing 0 to 1 heteroatoms from O, N or S; R6 = H, halogen, C1-C6alkyl, C3-C7cycloalkyl, nitro, amino, NR7R8, COOR, aryl, NR7(SO2)R8 or C(O)NR7R8; W = methylene or C(O); m = a whole number between 0 and 2, n = a whole number between 1 and 6, p= 2 or 3. Method for production and therapeutic application.
L'invention concerne les dérivés de 1, 2,3,4-tétrahydropyrrolo-[1,2-a]- pyrazine-6-carboxamides et de 2, 3, 4, 5-tétrahydropyrrolo [1, 2-a] [1, 4]-diazépine-7-carboxamides, de formule générale (I) selon la revendication 1 ayant une activité inhibitrice vis-à-vis de l'activité .beta.-secrétax.
Baudoin Bernard
Evers Michel
Genevois-Borella Arielle
Karlsson Andreas
Malleron Jean-Luc
Robic
Sanofi-Aventis
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