Dipeptide nitriles

C - Chemistry – Metallurgy – 07 – C

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C07C 255/29 (2006.01) A61K 31/275 (2006.01) A61K 31/33 (2006.01) C07C 255/44 (2006.01) C07C 271/22 (2006.01) C07C 317/44 (2006.01) C07C 323/52 (2006.01) C07C 323/62 (2006.01) C07D 207/32 (2006.01) C07D 207/327 (2006.01) C07D 209/18 (2006.01) C07D 209/42 (2006.01) C07D 211/06 (2006.01) C07D 213/64 (2006.01) C07D 213/81 (2006.01) C07D 213/82 (2006.01) C07D 215/48 (2006.01) C07D 233/54 (2006.01) C07D 241/44 (2006.01) C07D 249/06 (2006.01) C07D 295/08 (2006.01) C07D 295/092 (2006.01) C07D 295/14 (2006.01) C07D

Patent

CA 2306313

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.

L'invention concerne des nitriles de dipeptides à substitution de l'extrémité N-terminale qui sont de puissants inhibiteurs des cathepsines de cystéine, par exemple, les cathepsines B, K, L et S et peuvent être utilisés pour traiter les maladies et les états dépendants de la cathepsine de cystéine, y compris, l'inflammation, la polyarthrite rhumatoïde, l'arthrose, l'ostéoporose, les tumeurs (en particulier, l'invasion tumorale et les métastases tumorales), les maladies coronaires, l'athérosclérose (y compris la rupture et la déstabilisation des plaques d'athérosclérose). En particulier, les nitriles de dipeptides sont des composés de la formule (I) ou des esters physiologiquement acceptables ou pouvant être scindés ou des sels de ces derniers. Dans la formule, les symboles sont tels que définis. On a constaté qu'un choix approprié des groupes R, R2, R3, R4, R5, X1, Y et L permettait de modifier la sélectivité relative des composés comme inhibiteurs des divers types de cathepsine de cystéine, par exemple, les cathepsines B, K, L et S pour obtenir des inhibiteurs qui inhibent, de manière sélective, un type de cathepsine particulier ou des combinaisons de types de cathepsines.

LandOfFree

Say what you really think

Search LandOfFree.com for Canadian inventors and patents. Rate them and share your experience with other people.

Rating

Dipeptide nitriles does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Dipeptide nitriles, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Dipeptide nitriles will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFCA-PAI-O-2074609

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.