Intermediates for macrocyclic compounds
View Patent ↗The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , n 1 , m, p Z 1 , Z 2 , and Z 3 are as describe in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.
1. A compound of formula W-T-Y, wherein W and Y are independently selected from the group consisting of —OH, —NH 2 and —NHR 60 , wherein R 60 is lower alkyl, and T is the following structure:
wherein
L 5 is CH or N;
L 6 is CR 52 R 53 or O, wherein R 52 and R 53 are independently selected from the group consisting of hydrogen and lower alkyl;
R 54 and R 55 are independently lower alkyl; and, when L 6 is CR 52 R 53 , R 55 is also selected from hydroxy;
R 56 is hydrogen or lower alkyl, and R 57 is selected from the group consisting of hydrogen and lower alkyl, and, when no double bond is present between the carbon atoms to which R 56 and R 57 are bonded, R 56 and R 57 are also independently selected from hydroxy; and
(W) indicates the point of attachment of T to W; and (Y) indicates the point of attachment of T to Y;
with the proviso that T is not the following:
further comprising one or more protecting groups.
2. A compound of formula W-T-Y, wherein W and Y are independently selected from the group consisting of —OH, —NH 2 and —NHR 60 , wherein R 60 is lower alkyl, and T is the following structure:
wherein
L 5 is CH or N;
L 6 is CR 52 R 53 or O, wherein R 52 and R 53 are independently selected from the group consisting of hydrogen and lower alkyl;
R 54 and R 55 is lower alkyl; and, when L 6 is CR 52 R 53 , R 55 is also selected from hydroxy;
R 56 and R 57 are independently selected from the group consisting of hydrogen and lower alkyl, and, when no double bond is present between the carbon atoms to which R 56 and R 57 are bonded, R 56 and R 57 are also independently selected from hydroxy; and
(W) indicates the point of attachment of T to W; and (Y) indicates the point of attachment of T to Y;
with the proviso that T is not the following:
3. The compound of claim 2 , further comprising one or more protecting groups.