EPOXYSUCCINAMIDE DERIVATIVES OR SALTS THEREOF, AND DRUGS CONTAINING THE SAME

Title:

EPOXYSUCCINAMIDE DERIVATIVES OR SALTS THEREOF, AND DRUGS CONTAINING THE SAME

Document Type and Number:

WIPO Patent Application WO/1997/021694

Kind Code:

A1

Abstract:

Epoxysuccinamide derivatives represented by general formula (1) or salts thereof and drugs comprising the same as the active ingredient, wherein R1 and R2 are the same or different and each represents H or optionally substituted aromatic hydrocarbyl or aralkyl, or R1 and R2 may form a nitrogenous heterocycle in cooperation with the adjacent nitrogen atom; R3 represents H or acyl; R4 represents H or aralkyl; and R5 represents optionally substituted aromatic hydrocarbyl or aralkyl or may form an optionally protected amino acid residue in cooperation with the adjacent nitrogen atom. These compounds have a cathepsin inhibitory activity, in particular a specific inhibitory activity against cathepsin L, and are hence effective in the prophylaxis and therapy of bone diseases such as osteoporosis.

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Inventors:

YAMASHITA TOMOHIRO (JP)
SUDA YOSHIMITSU (JP)
TADA YUKIO (JP)
KATSUNUMA NOBUHIKO (JP)
ASAO TETSUJI (JP)

Application Number:

PCT/JP1996/003603

Publication Date:

June 19, 1997

Filing Date:

December 10, 1996

Export Citation:

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Assignee:

TAIHO PHARMACEUTICAL CO LTD (JP)
YAMASHITA TOMOHIRO (JP)
SUDA YOSHIMITSU (JP)
TADA YUKIO (JP)
KATSUNUMA NOBUHIKO (JP)
ASAO TETSUJI (JP)

International Classes:

C07D303/48; (IPC1-7): C07D303/48; A61K31/335

Foreign References:

EP0665447A2

1995-08-02

Other References: