Title:
DIPEPTIDE NITRILES
Document Type and Number:
WIPO Patent Application WO1999024460
Kind Code:
B1
Abstract:
N-terminal substituted dipeptide nitriles as defined are useful as inhibitors of cysteine cathepsins, e.g. cathepsins B, K, L and S, and can be used for the treatment of cysteine cathepsin dependent diseases and conditions, including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, tumors (especially tumor invasion and tumor metastasis), coronary disease, atherosclerosis (including atherosclerotic plaque rupture and destabilization). Particular dipeptide nitriles are compounds of formula (I), or physiologically-acceptable and -cleavable esters or salts thereof, wherein: the symbols are as defined. In particular it has been found that by appropriate choice of groups R, R2, R3, R4, R5, X1, Y and L, the relative selectivity of the compounds as inhibitors of the various cysteine cathepsin types, e.g. cathepsins B, K, L and S, may be altered, e.g. to obtain inhibitors which selectively inhibit a particular cathepsin type or combination of cathepsin types.
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Inventors:
ALTMANN EVA (CH)
BETSCHART CLAUDIA (JP)
GOHDA KEIGO (JP)
HORIUCHI MIYUKI (JP)
LATTMANN RENE (CH)
MISSBACH MARTIN (CH)
SAKAKI JUNICHI (JP)
TAKAI MICHIHIRO (JP)
TENO NAOKI (JP)
COWEN SCOTT DOUGLAS (US)
GREENSPAN PAUL DAVID (US)
MCQUIRE LESLIE WIGHTON (US)
TOMMASI RUBEN ALBERTO (US)
VAN DUZER JOHN HENRY (US)
BETSCHART CLAUDIA (JP)
GOHDA KEIGO (JP)
HORIUCHI MIYUKI (JP)
LATTMANN RENE (CH)
MISSBACH MARTIN (CH)
SAKAKI JUNICHI (JP)
TAKAI MICHIHIRO (JP)
TENO NAOKI (JP)
COWEN SCOTT DOUGLAS (US)
GREENSPAN PAUL DAVID (US)
MCQUIRE LESLIE WIGHTON (US)
TOMMASI RUBEN ALBERTO (US)
VAN DUZER JOHN HENRY (US)
Application Number:
PCT/EP1998/006937
Publication Date:
October 28, 1999
Filing Date:
November 03, 1998
Export Citation:
Assignee:
NOVARTIS AG (CH)
NOVARTIS ERFIND VERWALT GMBH (AT)
ALTMANN EVA (CH)
BETSCHART CLAUDIA (JP)
GOHDA KEIGO (JP)
HORIUCHI MIYUKI (JP)
LATTMANN RENE (CH)
MISSBACH MARTIN (CH)
SAKAKI JUNICHI (JP)
TAKAI MICHIHIRO (JP)
TENO NAOKI (JP)
COWEN SCOTT DOUGLAS (US)
GREENSPAN PAUL DAVID (US)
MCQUIRE LESLIE WIGHTON (US)
TOMMASI RUBEN ALBERTO (US)
DUZER JOHN HENRY VAN (US)
NOVARTIS ERFIND VERWALT GMBH (AT)
ALTMANN EVA (CH)
BETSCHART CLAUDIA (JP)
GOHDA KEIGO (JP)
HORIUCHI MIYUKI (JP)
LATTMANN RENE (CH)
MISSBACH MARTIN (CH)
SAKAKI JUNICHI (JP)
TAKAI MICHIHIRO (JP)
TENO NAOKI (JP)
COWEN SCOTT DOUGLAS (US)
GREENSPAN PAUL DAVID (US)
MCQUIRE LESLIE WIGHTON (US)
TOMMASI RUBEN ALBERTO (US)
DUZER JOHN HENRY VAN (US)
International Classes:
A61K31/275; A61K31/341; A61K31/343; A61K31/352; A61K31/357; A61K31/36; A61K31/381; A61K31/40; A61K31/4015; A61K31/403; A61K31/404; A61K31/415; A61K31/4155; A61K31/4164; A61K31/4192; A61K31/426; A61K31/44; A61K31/4406; A61K31/4409; A61K31/4418; A61K31/443; A61K31/4433; A61K31/4453; A61K31/451; A61K31/47; A61K31/495; A61K31/4965; C07D249/04; A61K31/519; A61K31/5375; A61K38/00; A61P9/10; A61P19/02; A61P19/10; A61P29/00; A61P35/00; A61P35/04; C07C255/29; C07C255/44; C07C271/22; C07C317/44; C07C323/52; C07C323/62; C07D207/327; C07D207/416; C07D209/08; C07D209/18; C07D209/42; C07D211/06; C07D211/14; C07D213/56; C07D213/64; C07D213/81; C07D213/82; C07D215/48; C07D231/14; C07D233/54; C07D233/64; C07D241/44; C07D249/06; C07D277/20; C07D277/56; C07D295/092; C07D295/14; C07D295/15; C07D295/155; C07D295/18; C07D307/54; C07D307/68; C07D307/79; C07D307/84; C07D307/85; C07D317/68; C07D333/24; C07D333/40; C07D333/48; C07D403/12; C07D405/12; C07D409/12; C07D487/04; C07K5/06; C07K5/062; C07D207/32; (IPC1-7): C07C255/29; A61K31/275; A61K31/33; C07D209/42; C07D215/48; C07D241/44; C07D333/24; C07D295/14; C07D233/54; C07D209/18; C07C255/44; C07D207/32; C07D307/85; C07D295/08; C07C271/22; C07K5/062; C07D213/64; C07C323/52; C07C317/44; C07C323/62; C07D249/06; C07D211/06; C07D307/68; C07D333/40; C07D213/81; C07D213/82; C07D307/54
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