Title:
BISPHOSPHONIC ACID DERIVATIVES
Document Type and Number:
WIPO Patent Application WO/1996/030378
Kind Code:
A1
Abstract:
Bisphosphonic acid derivatives having a partial structure of epoxysuccinic acid and showing the activity of inhibiting a cysteine protease, in particular, one represented by general formula (I) or its salt (wherein R1 represents hydrogen, alkyl or aralkyl; X1 represents -O-, -NR6- or a divalent heterocyclic residue; A1 represents a single bond or an amino acid or dipeptide residue having the N-terminus on the right side; A2 represents a single bond or an amino acid or dipeptide residue having the N-terminus on the left side; L1 represents a divalent leaving group; and R2, R3, R4, R5 and R6 independently represent each hydrogen, alkyl or aralkyl) which are useful as a remedy for bone diseases and in the treatment or prevention of diseases in association with the hyperfunction of cathepsins L and B.
Inventors:
NOMURA YUTAKA (JP)
TAKAHASHI TOSHIHIRO (JP)
HARA KAORU (JP)
YOSHINO KOH (JP)
MASAKI MITSUO (JP)
TAKAHASHI TOSHIHIRO (JP)
HARA KAORU (JP)
YOSHINO KOH (JP)
MASAKI MITSUO (JP)
Application Number:
PCT/JP1996/000888
Publication Date:
October 03, 1996
Filing Date:
April 01, 1996
Export Citation:
Assignee:
NIPPON CHEMIPHAR CO (JP)
NOMURA YUTAKA (JP)
TAKAHASHI TOSHIHIRO (JP)
HARA KAORU (JP)
YOSHINO KOH (JP)
MASAKI MITSUO (JP)
NOMURA YUTAKA (JP)
TAKAHASHI TOSHIHIRO (JP)
HARA KAORU (JP)
YOSHINO KOH (JP)
MASAKI MITSUO (JP)
International Classes:
C07F9/655; C07K5/06; A61K38/00; (IPC1-7): C07F9/655; A61K31/665; A61K31/675; A61K38/55; C07K5/062
Foreign References:
| US3579570A | 1971-05-18 | |||
| US3822296A | 1974-07-02 | |||
| JPS63284127A | 1988-11-21 | |||
| JPH02218610A | 1990-08-31 | |||
| JPH02268190A | 1990-11-01 | |||
| JPH05230086A | 1993-09-07 |
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