titleOfInvention |
1,2,3,4-tetrahydropyrrolo [1,2-A] pyrazine-6-carboxamide and 2,3,4,5-tetrahydropyrrolo [1,2-A] [1,4 ] -Diazepine-7-carboxamide derivatives, their preparation and therapeutic uses |
abstract |
The present invention relates to 1,2,3,4-tetrahydropyrrolo [1,2-a] pyrazine-6-carboxamide of formula (I) and 2,3,4,5-tetrahydropyrrolo [1 , 2-a] [1,4] diazepine-7-carboxamide derivatives, methods for their preparation and therapeutic uses: <Formula I> Where R 1 = H, C 1 -C 10 alkyl, C 3 -C 7 cycloalkyl, (CH 2 ) n- (C 1 -C 6 ) alkenyl, (CH 2 ) n- (C 1 -C 6 ) alkynyl , C 1 -C 6 alkyl-Z- (C 1 -C 6 ) alkyl, wherein Z = 0, heteroatoms selected from N, and S (O) m , or R1 = COOR, S (O) m R, aryl Or aralkyl groups; R 2 = H, halogen, C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 1 -C 6 alkenyl, C 1 -C 6 alkynyl, C 1 -C 6 alkyl-Z- (C 1- C 6) one or more alkyl groups of from heteroatoms selected from (wherein Z = O, N and S (O) m), or R2 = halo (C 1 -C 6) alkyl, halo (C 1 -C 6) alkoxy , Hydroxy, C 1 -C 6 alkoxy, nitro, cyano, amino, NR7R8, COOR, C (O) NR7R8, OC (O) (C 1 -C 6 ) alkyl, S (O) m -NR7R8, aryl ; R3 = trifluoromethyl; R 4 and R 5 are independently H or R 4 and R 5 together with the carbon to which they are attached form a saturated ring containing 3 to 6 carbons and optionally containing 0 to 1 heteroatom selected from O, N or S and ; R 6 = H, halogen, C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, nitro, amino, NR 7 R 8, COOR, aryl, NR 7 (SO 2 ) R 8 or C (O) NR 7 R 8; W = methylene or C (O); m = an integer of 0 to 2, n = an integer of 1 to 6, p = 2 or 3. |