Title:
HYDRAZIDE COMPOUND AS KAPPA AGONIST
Document Type and Number:
Japanese Patent JP3233276
Kind Code:
B2
Abstract:
PROBLEM TO BE SOLVED: To obtain the subject new compound having agonist activity against opioid kappa receptor, useful as an analgesic, an anesthetic, an anti- inflammatory agent and a neuroprotective agent and also in arthritis, stroke or functional bowel disease.
SOLUTION: This compound is represented by formula I [R1 and R2 are each H, an (alkyl)-CO group or the like; R3 is H, hydroxy or the like; R4 is a (substituted)phenyl or a heterocyclic group], e.g. N'-tert.- butoxycarbonylamino-2-(3,4-dichlorophenyl)-N-[2-(3-(S)- methoxymethoxypyrrolidin-1-yl)-1-(S)phenylethyl]acetamide. The compound of formula I is produced by reacting, e.g. a compound of formula II with N- protected carbazate (e.g. NH2NHBOC) to afford a compound of formula III, reacting the compound of formula III with a desired phenylacetate, subjecting the resultant compound to normal hydrolysis to remove N-protecting group (e.g. BOC) and obtaining an unsubstituted hydrazide compound.
Inventors:
Fumitaka Ito
Application Number:
JP16283798A
Publication Date:
November 26, 2001
Filing Date:
May 28, 1998
Export Citation:
Assignee:
Pfizer Pharmaceuticals Co., Ltd.
International Classes:
C07D401/12; A61K31/40; A61K31/4025; A61K31/44; A61K31/4427; A61K31/443; A61K31/4433; A61P1/00; A61P23/00; A61P23/02; A61P25/00; A61P25/02; A61P25/04; A61P25/28; A61P29/00; A61P43/00; C07D207/06; C07D207/12; C07D405/12; C07D409/12; (IPC1-7): C07D207/12; A61K31/40; A61K31/44; A61P23/00; A61P25/04; A61P25/28; A61P29/00; C07D207/06; C07D401/12; C07D405/12; C07D409/12
Attorney, Agent or Firm:
Hiroshi Kobayashi