Title:
BONE RESORPTION INHIBITORS
Document Type and Number:
WIPO Patent Application WO/1998/001133
Kind Code:
A1
Abstract:
Drugs, in particular, bone resorption inhibitors containing as the active ingredient compounds having selective cathepsin K inhibitory effects, among all, proline derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof, wherein each symbol has the meaning as specified below: X: a moiety (except for the C-terminal carbonyl group) of an amino acid residue with its side chain optionally protected; R?1�: an amino-protective group; G: a glycine residue; n: 0 or 1; R?3�: a group inhibiting the activity of the SH group of cysteine protease; and R?4�: hydrogen, hydroxy or phenyl.
Inventors:
AIBE KAZUHIKO (JP)
TAKEBAYASHI YUKIHIRO (JP)
ISHII YASUTAKA (JP)
NOSHIRO OSAMU (JP)
NODA ICHIO (JP)
IGARASHI SUSUMU (JP)
TAKEBAYASHI YUKIHIRO (JP)
ISHII YASUTAKA (JP)
NOSHIRO OSAMU (JP)
NODA ICHIO (JP)
IGARASHI SUSUMU (JP)
Application Number:
PCT/JP1997/002357
Publication Date:
January 15, 1998
Filing Date:
July 08, 1997
Export Citation:
Assignee:
YAMANOUCHI PHARMA CO LTD (JP)
AIBE KAZUHIKO (JP)
TAKEBAYASHI YUKIHIRO (JP)
ISHII YASUTAKA (JP)
NOSHIRO OSAMU (JP)
NODA ICHIO (JP)
IGARASHI SUSUMU (JP)
AIBE KAZUHIKO (JP)
TAKEBAYASHI YUKIHIRO (JP)
ISHII YASUTAKA (JP)
NOSHIRO OSAMU (JP)
NODA ICHIO (JP)
IGARASHI SUSUMU (JP)
International Classes:
C07D207/16; C07K5/078; (IPC1-7): A61K31/40; A61K31/415; A61K31/42; A61K31/425; A61K31/445; A61K31/495; A61K31/505; A61K31/535; A61K35/06; A61K35/55; C07D207/16; C07D405/12; C07D413/12; C07D417/12; C07K5/078; C07K5/083
Domestic Patent References:
| WO1997020856A1 | 1997-06-12 |
Foreign References:
| JPS63253061A | 1988-10-20 | |||
| JPS62129297A | 1987-06-11 | |||
| JPH08104698A | 1996-04-23 | |||
| JPS58140026A | 1983-08-19 |
Other References:
J. BIOL. CHEM., Vol. 271, No. 21, (1996), MARY J. BOSSARD et al., "Proteolytic Activity of Human Osteoclast Cathepsin K", p. 12517-12524.
J. BIOL. CHEM., Vol. 271, No. 21, (1996), FRED H. DRAKE et al., "Cathepsin K, but Not Cathepsin B,L, or S, is Abundantly Expressed in Human Osteoclasts", p. 12511-12516.
BIOCHEM. BIOPHYS. RES. COMMUN., Vol. 206, No. 1, (1995), TETSUYA INAOKA et al., "Molecular Cloning of Human cDNA for Cathepisin K: Novel Cysteine Proteinase Predominantly Expressed in Bone", p. 89-96.
J. BIOL. CHEM., Vol. 271, No. 21, (1996), FRED H. DRAKE et al., "Cathepsin K, but Not Cathepsin B,L, or S, is Abundantly Expressed in Human Osteoclasts", p. 12511-12516.
BIOCHEM. BIOPHYS. RES. COMMUN., Vol. 206, No. 1, (1995), TETSUYA INAOKA et al., "Molecular Cloning of Human cDNA for Cathepisin K: Novel Cysteine Proteinase Predominantly Expressed in Bone", p. 89-96.
Attorney, Agent or Firm:
Nagai, Shozo (Patent & Information Dept., 17-1, Hasune 3-chom, Itabashi-ku Tokyo, JP)
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