Indoloylguanidine derivatives as inhibitors of sodium-hydrogen exchange.

摘要

Novel indoloylguanidine derivatives of the following formula (I), and pharmaceutically acceptable salts thereof, inhibit the Na<+>/H<+> exchanger activity and are therefore useful in the treatment and prevention of disease caused by increased Na<+>/H<+> exchanger activity. <CHEM> wherein each R1, which may be the same or different, is independently selected from hydrogen, an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a halogen, a nitro group, an acyl group, a carboxyl group, an alkoxycarbonyl group, an aromatic group, and a group of formula: -OR3, -NR6R7, -SO2NR6R7 or -S(O)nR40; R2 is a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, a hydroxy group, an alkoxy group or a group of formula -CH2R20; R3 is hydrogen, an alkyl group, a substituted alkyl group, a cycloalkyl group or a group shown by formula: -CH2R30, wherein R30 represents an alkenyl group or an alkynyl group; each of R6 and R7, which may be the same or different, is independently selected from hydrogen, an alkyl group, a substituted alkyl group, a cycloalkyl group, an acyl group and a group of formula: -CH2R60, wherein R60 represents an alkenyl group or an alkynyl group; or R6 and R7, together with the nitrogen atom to which they are attached, form a saturated 5- to 7- membered cyclic amino group which optionally includes at least one other hetero atom in the ring; R40 is an alkyl group or a substituted alkyl group; n is 0, 1 or 2; and, R20 is an alkenyl group or an alkynyl group; and wherein the substituents R1 and the guanidinocarbonyl group -C(=O)-N=C(NH2)2 are each, independently, attached to any one of the 5- and 6- membered rings of the indole nucleus; or a pharmaceutically acceptable acid addition salt thereof.