C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 5/062 (2006.01) A61K 38/05 (2006.01) A61P 7/02 (2006.01) C07K 5/065 (2006.01) C07K 5/068 (2006.01) C07K 5/072 (2006.01)
Patent
CA 2529938
The present invention relates to novel compounds of Formula (I) wherein ~X~ represents an amino acid group, ~n~ is an integer between 1 and 4, ~R1~ represents benzyl, t-butyl or 9-fluorenylmethyl and ~R2~ represents a tetramethylmercaptoimidazole derivative or -S+R3R4, wherein R3 and R4 each independently represent lower alkyl, or a pharmaceutically and/or veterinarily acceptable derivative thereof. The present invention further relates to pharmaceutical formulations of said compound and the use thereof in the preparation of a medicament for inhibiting diseases in which transglutaminase has been implicated. Advantageously, the medicament is for treating fibrosis, scarring and/or cancer. Additionally, the invention relates to a method of inhibiting autoimmune diseases such as coeliac disease, neurodegeneration and chronic inflammatory diseases (e.g. of the joints including rheumatoid arthritis and osteoarthritis in a subject). The invention further relates to a method for preventing or treating rejection of a transplanted organ.
L'invention concerne des composés de formule <I>I</I>. X' est un groupe aminoacide, n' est un entier compris entre 1 et 4, R¿1? est benzyle, t-butyle ou 9-fluorénylméthyle et R¿2? est un dérivé tétraméthylmercaptoimidazole ou -S?+¿R¿3?R¿4?, sachant que R¿3? et R¿4? sont chacun indépendamment alkyle inférieur, ou bien un dérivé correspondant acceptable du point de vue pharmaceutique et/ou vétérinaire. L'invention concerne également des formulations pharmaceutiques correspondantes et leur utilisation dans la préparation d'un médicament inhibant les maladies dans lesquelles intervient la transglutaminase. Ledit médicament présente un intérêt dans le traitement de la fibrose, de la cicatrisation et/ou du cancer. L'invention concerne en outre un procédé relatif à l'inhibition des maladies auto-immunes du type maladie coeliaque, neurodégénérescence et maladies inflammatoires chroniques (concernant par exemple les articulations, y compris la polyarthrite rhumatoïde et l'ostéoarthrose). L'invention concerne enfin un procédé de prévention ou de traitement du rejet d'organe transplanté.
Coutts Ian George
Griffin Martin
Saint Robert Edward
Aston University
Borden Ladner Gervais Llp
The Nottingham Trent University
LandOfFree
Dipeptide transglutaminase inhibitors and methods of using... 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 transglutaminase inhibitors and methods of using..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Dipeptide transglutaminase inhibitors and methods of using... will most certainly appreciate the feedback.
Profile ID: LFCA-PAI-O-1866103