IP Library › Patent Application 13412148
Patent Application
App. No. 13/412,148

PROCESSES FOR INTERMEDIATES FOR MACROCYCLIC COMPOUNDS

Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US None
App. No.
13/412,148
Abstract

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 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.

Claims (19)

1 - 39 . (canceled)

40 . A compound of formula (IV):

wherein R 1 is C 1 -C 4 alkyl; PG 5 is hydrogen or an amine protecting group; and PG 6 is hydrogen or a hydroxy protecting group.

41 . The compound of claim 40 , wherein R 1 is methyl.

42 . The compound of claim 40 , wherein PG 5 is hydrogen.

43 . The compound of claim 40 , wherein PG 5 is a carbamate protecting group.

44 . The compound of claim 40 , wherein PG 5 is selected from the group consisting of tert-butoxycarbonyl (Boc), benzyloxycarbonyl (Cbz), 9-fluorenylmethoxycarbonyl (Fmoc), α,α-dimethyl-3,5-dimethoxybenzyloxycarbonyl (Ddz) and allyloxycarbonyl (Alloc).

45 . The compound of claim 40 , wherein PG 6 is hydrogen.

46 . The compound of claim 40 represented by the following structures:

wherein PG 5 is hydrogen or an amine protecting group; and PG 6 is hydrogen or a hydroxy protecting group.

47 . The compound of claim 44 , wherein PG 5 is α,α-dimethyl-3,5-dimethoxybenzyloxy-carbonyl (Ddz).

48 . The compound of claim 46 , wherein PG 5 is α,α-dimethyl-3,5-dimethoxybenzyloxy-carbonyl (Ddz).

49 . The compound of claim 47 represented by the following structures:

50 . The compound of claim 44 , wherein PG 5 is tert-butoxycarbonyl (Boc).

51 . The compound of claim 50 represented by the following structures:

52 . A process of using a compound of claim 40 to make a compound of formula (I);

wherein R 1 is C 1 -C 4 alkyl.

53 . A process of using a compound of claim 40 to make a compound of formula (G);

wherein R 1 is C 1 -C 4 alkyl and PG 1 is an amine protecting group.