Heterocyclyl-3-sulfonylindazoles as 5-hydroxytryptamine-6 ligands

A method for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor in a patient in need thereof which comprises providing to said patient a therapeutically effective amount of a compound of formula I

• 55
• wherein
• A is C, CR8 or N;
• R1 is H, halogen, CN, COR9, OCO2R10, CO2R11, CONR12R13, SOxR14, NR15R16, OR17 or a C1-C6alkyl, C3-C7cycloalkyl, aryl or heteroaryl group each optionally substituted;
• R2 is an optionally substituted C1-C6alkyl, C3-C7cycloalkyl, aryl, or heteroaryl group or an optionally substituted 8- to 13-membered bicyclic or tricyclic ring system having a N atom at the bridgehead and optionally containing 1, 2 or 3 additional heteroatoms selected from N, O or S;
• R3 is H or a C1-C6alkyl, C3-C7cycloalkyl, aryl or heteroaryl group each optionally substituted;
• R4 is H or a C1-C6alkyl or C3-C7cycloalkyl group each optionally substituted;
• R5, R6 and R7 are each independently H or a C1-C6alkyl or C3-C7cycloalkyl group each optionally substituted;
• m and p are each independently an integer of 1, 2 or 3;
• n is an integer of 1 or 2;
• R8 is H, OH or an optionally substituted C1-C6alkoxy group;
• R9, R10, R11, and R17 are each independently H or a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, cycloheteroalkyl, aryl or heteroaryl group each optionally substituted;
• R12, R13, R15 and R16 are each independently H or an optionally substituted C1-C4alkyl group or R12 and R13 or R15 and R16 may be taken together with the atom to which they are attached to form a 5- to 7-membered ring optionally containing another heteroatom selected from O, NR18 or SOx;
• R14 is a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, cycloheteroalkyl, aryl or heteroaryl group each optionally substituted;
• R18 is H or a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C7cycloalkyl, cycloheteroalkyl, aryl or heteraryl group each optionally substituted;
• x is 0 or an integer of 1 or 2;
• and
• represents a single bond or a double bond;
• or the stereoisomes thereof or the pharmaceutically acceptable salts thereof.

A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and an effective amount of a compound of formula I

• 56
• wherein
• A is C, CR8 or N;
• R1 is H, halogen, CN, COR9, OCO2R10, CO2R11, CONR12R13, SOxR14, NR15R16, OR17 or a C1-C6alkyl, C3-C7cycloalkyl, aryl or heteroaryl group each optionally substituted;
• R2 is an optionally substituted C1-C6alkyl, C3-C7cycloalkyl, aryl, or heteroaryl group or an optionally substituted 8- to 13-membered bicyclic or tricyclic ring system having a N atom at the bridgehead and optionally containing 1, 2 or 3 additional heteroatoms selected from N, O or S;
• R3 is H or a C1-C6alkyl, C3-C7cycloalkyl, aryl or heteroaryl group each optionally substituted;
• R4 is H or a C1-C6alkyl or C3-C7cycloalkyl group each optionally substituted;
• R5, R6 and R7 are each independently H or a C1-C6alkyl or C3-C7cycloalkyl group each optionally substituted;
• m and p are each independently an integer of 1, 2 or 3;
• n is an integer of 1 or 2;
• R8 is H, OH or an optionally substituted C1-C6alkoxy group;
• R9, R10, R11, and R17 are each independently H or a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, cycloheteroalkyl, aryl or heteroaryl group each optionally substituted;
• R12, R13, R15 and R16 are each independently H or an optionally substituted C1-C4alkyl group or R12 and R13 or R15 and R16 may be taken together with the atom to which they are attached to form a 5- to 7-membered ring optionally containing another heteroatom selected from O, NR18 or SOx;
• R14 is a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, cycloheteroalkyl, aryl or heteroaryl group each optionally substituted;
• R18 is H or a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C7cycloalkyl, cycloheteroalkyl, aryl or heteraryl group each optionally substituted;
• x is 0 or an integer of 1 or 2;
• and
• represents a single bond or a double bond;
• or the stereoisomes thereof or the pharmaceutically acceptable salts thereof.