Antipsychotic indolyl derivatives

A pharmaceutical composition comprising a therapeutically effective amount of a compound according to the formula:

• wherein
• R1 and R2 are each independently selected from H, OH, F, Cl, Br, I, 1 to 6 carbon alkyl or alkenyl, 1 to 6 carbon alkoxy, aryl, OR5, nitro, amino, CF3 and when R1 and R2 are taken together, form a fused ring at the 2,3- or 3,4- positions providing a fused phenyl group or a benzodioxane group, or a 4- or 7-substituted indole group, or a 5- or 8-substituted quinoline group;
• the group formed by the fusion of R1 and R2 being taken together is further optionally substituted by from 1 to 3 groups selected from H, COOH or the C1 to C6 alkyl esters thereof, OH, F, Cl, Br, I, 1 to 6 carbon alkyl or alkenyl, 1 to 6 carbon alkoxy, OR5, —C(O)NR6R7, nitro, amino, or CF3;
• R3 represents a group selected from hydrogen, a 1 to 6 carbon alkyl, a 1 to 4 carbon alkoxy or a halogen;
• R4 represents a group selected from hydrogen, 1 to 6 carbon alkyl or R5;
• R5 is CH2Ph in which the phenyl ring can be optionally substituted by a group selected from OMe, halogen, CF3;
• R6 and R7 are independently selected from H or C1 to C6 alkyl;
• X is N;
• A is selected from a group represented by N, CH and CH2;
• and
• B is selected from a group represented by ═O, H and H2;
• such that the moiety in formula (1) represented by the formula:
• with the proviso that when R1 and R2 taken together with the ring to which they are attached form a 4- or 7-substituted indole group, then B is ═O;
• or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient.

A method of treating a patient suffering from schizophrenia, comprising providing to a patient in need thereof, a therapeutically effective amount of a compound according to the formula:

• wherein
• R1 and R2 are each independently selected from H, OH, F, Cl, Br, I, 1 to 6 carbon alkyl or alkenyl, 1 to 6 carbon alkoxy, aryl, OR5, nitro, amino, CF3 and when R1 and R2 are taken together, form a fused ring at the 2,3- or 3,4- positions providing a fused phenyl group or a benzodioxane group, or a 4- or 7-substituted indole group, or a 5- or 8-substituted quinoline group;
• the group formed by the fusion of R1 and R2 being taken together is further optionally substituted by from 1 to 3 groups selected from H, COOH or the C1 to C6 alkyl esters thereof, OH, F, Cl, Br, I, 1 to 6 carbon alkyl or alkenyl, 1 to 6 carbon alkoxy, OR5, —C(O)NR6R7, nitro, amino, or CF3;
• R3 represents a group selected from hydrogen, a 1 to 6 carbon alkyl, a 1 to 4 carbon alkoxy or a halogen;
• R4 represents a group selected from hydrogen, 1 to 6 carbon alkyl or R5;
• R5 is CH2Ph in which the phenyl ring can be optionally substituted by a group selected from OMe, halogen, CF3;
• R6 and R7 are independently selected from H or C1 to C6 alkyl;
• X is N;
• A is selected from a group represented by N, CH and CH2;
• and
• B is selected from a group represented by ═O, H and H2;
• such that the moiety in formula (1) represented by the formula:
• with the proviso that when R1 and R2 taken together with the ring to which they are attached form a 4- or 7-substituted indole group, then B is ═O;
• or a pharmaceutically acceptable salt thereof.