ALCOHOL OR ALDEHYDE DERIVATIVE AND ITS USE

Title:

ALCOHOL OR ALDEHYDE DERIVATIVE AND ITS USE

Document Type and Number:

Japanese Patent JP2848232

Kind Code:

B2

Abstract:

PURPOSE: To provide an alcohol or aldehyde derivative having selective inhibitory action on cathepsin, directly acting to the bones to suppress the bone resorption and useful for the prevention and treatment of osteoporosis.
CONSTITUTION: A compound of the formula I [R1 is H or arylalkyl, heterocyclic- alkyl or lower alkyl which may have substituent; R2 and R3 are H or (substituted) hydrocarbon residue; R4 is (substituted) alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl; X is CHO or CH2OB (B is H or hydroxyl-protecting group); m and n are 0 or 1], e.g. N-(1-naphthylsulfonyl)-(L)- isoleucyl-(L)-tryptophanal. Some of the compounds of the formula I can be produced by reacting a compound of the formula II [R4' is (substituted) alkanoyl, sulfonyl or carbonyloxy] or its reactive derivative with a compound of the formula III and optionally subjecting the reaction product to oxidation reaction or hydroxyl-protection reaction.

Inventors:

SODA TAKASHI
FUJISAWA YUKIO
YASUMA TSUNEO
MIZOGUCHI JUNJI
KOORI MASAKI
TAKIZAWA MASAYUKI

Application Number:

JP1108194A

Publication Date:

January 20, 1999

Filing Date:

February 02, 1994

Export Citation:

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Assignee:

TAKEDA YAKUHIN KOGYO KK

International Classes:

A61K31/16; A61K38/55; A61K31/165; A61K31/18; A61K31/27; A61P3/00; A61P3/02; A61P43/00; C07C231/12; C07C233/18; C07C233/22; C07C233/31; C07C237/10; C07C237/22; C07C271/16; C07C271/18; C07C271/22; C07C303/40; C07C311/19; C07C337/02; C07D209/14; C07D209/16; C07K1/113; C07K5/06; C07K5/062; C07K14/81; A61K38/00; (IPC1-7): C07D209/14

Domestic Patent References:

JP5155764A
JP5178758A
JP6506921A

Attorney, Agent or Firm:

Tadao Asahina (1 person outside)

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