Sulphonamide derivatives, process for their preparation, and their use as medicaments

A process for the preparation of a compound of formula (I) or a salt thereof.

• 13
• wherein:
• P is phenyl, naphthyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulphur;
• A is a single bond, a C1-6alkylene or a C1-6alkenylene group;
• R1 is halogen, C1-6alkyl optionally substituted by one or more halogen atoms, C3-6cycloalkyl, COC1-6alkyl, C1-6alkoxy, OCF3, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, acyl, nitro, amino, alkylamino or dialkylamino, cyano or R1 is phenyl, naphthyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulphur;
• n is 0,1,2,3,4, 5 or 6:
• R2 is hydrogen, C1-6 alkyl or aryl C1-6 alkyl;
• R3 is a group R5 or together with R5 forms a group (CH2)2O or (CH2)3O or R3 is linked to R2 to form a group (CH2)2 or (CH2)3;
• R4 is —X(CH2)p—R6 where X is a single bond, CH2, O, NH or N—C1-6-alkyl and p is 0 to 6 and R6 is an optionally substituted 5- to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from nitrogen, sulphur or oxygen, or R6 is NR7R8 where R7 and R8 are independently hydrogen, C1-6 alkyl or aryl C1-6alkyl;
• and
• R5 is hydrogen, halogen, C1-6alkyl, C3-6cycloalkyl, COC1-6alkyl, C1-6alkoxy, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, acyl, nitro, trifluoromethyl, cyano or aryl,
• which process comprises the coupling of a compound of formula (II):
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• in which R1, n, P, and A are as defined in formula (I) or protected derivatives thereof and L is a leaving group with a compound of formula (III):
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• in which R2, R3, R4 and R5 are as defined in formula (I) or protected derivatives thereof and optionally thereafter:
• removing any protecting groups,
• forming a pharmaceutically acceptable salt.