| abstract |
The present invention relates to b-carboline derivatives of formula (I) wherein the substituents have the following meanings: R1 is independently halogen, nitro, hydroxy, C1-C8 alkyl, C1-C8 alkoxy; , -NH2, -NHRA, -N (RA) 2, -O-RA, -C (O) NH2, -C (O) NHRA, -C (O) N (RA) 2, -NC (O) - RA, -SO2NHRA, -SO2N (RA) 2 phenyl (optionally substituted with 1-3 RB groups) or heteroaryl (optionally substituted with 1-3 RB groups); n is an integer from 0 to 4; X is oxygen, sulfur or -NRD; R2 is (C5-C10) alkyl (optionally substituted with 1-3 RB), aryl (optionally substituted with 1-3 RB), heteroaryl (optionally 1-3). RB) or heterocycloalkyl (optionally substituted with 1-3 RB); a is 0 or 1; Y is -CH 2 -, -C (O) -, -C (O) O -, -C (O) -NH- or -SO 2 -; m is an integer from 0 to 2; R3 is independently halogen, nitro, (C1-C8) alkyl, (C1-C8) alkoxy, trifluoromethyl, trifluoromethoxy, phenyl (optionally substituted with 1-3 RB), phenylsulfonyl, naphthyl - (C 1 -C 8) araralkyl, heteroaryl (optionally substituted with 1 to 3 RB groups), -NH 2, -NHRA, -N (R A) 2; Z is -CH 2 -, -CHOH- or -C (O) -; provided that when Z is -CHOH- or -C (O) - then X is NH; R 4 is hydrogen, hydroxy, carboxy, C 1-6 alkylcarbonyl, C 1-6 alkylalkoxycarbonyl, di (C 1-8 alkyl) aminoalkoxycarbonyl, di (C 1-8 alkyl) -amino- (C1-C8-alkyl) -aminocarbonyl or -CORF. The present invention also provides the use of the disclosed derivatives for the manufacture of a medicament for the treatment of PDE-related diseases and conditions, such as male erectile dysfunction. HE |