2 results about "Morphine derivatives" patented technology

To provide a spirocyclic morphine derivative having κ-opioid receptor agonist activity. 【Solution means】 A compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: TIFF2026086955000362.tif5071 (In the formula, R 1 ~R 5 , R 7 ~R 1 3 represents a hydrogen atom, a C 1-6 alkyl group, etc., R 6 represents a hydrogen atom, a hydroxy group, etc., A represents a heterocycle which may contain at least one heteroatom selected from N, O and S as ring-constituting atoms, etc., W represents a C 1-6 alkylene group, etc., X represents a C 1-6 alkylene group, etc., Y represents a C 1-6 alkylene, etc., Z represents a C 3-7 saturated hydrocarbon ring, etc.).

This application relates to a 7α-substituted piperazine morphine derivative, its preparation method, and its uses. Specifically, it relates to 7α-(N-substituted piperazine)-tetrahydrothebaine derivatives as shown in general formula (I) or pharmaceutically acceptable salts thereof, and their preparation methods. Furthermore, it relates to the use of such derivatives in the preparation of analgesic, anti-irritable bowel syndrome, antipruritic, anti-addictive, and antidepressant drugs. The derivatives described in this invention exhibit significantly enhanced κ-receptor agonist activity and κ-receptor subtype selectivity.