C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 303/48 (2006.01) A61K 31/335 (2006.01)
Patent
CA 2217051
An epoxysuccinic acid derivative having the following formula: (see formula I) [wherein R1 is hydrogen, alkyl, aryl, or aralkyl; each of R2 and R3 independently is aryl, aralkyl or alkyl; X is -O- or -NR4-; and R4 is hydrogen, alkyl, or aralkyl] is useful for prevention and treatment of bone diseases such as osteoporosis, malignant hypercalcemia and Paget's syndrome, and further useful for treatment of osteoarthritis and rheumatoid arthritis which are accompanied by abnormal enhancement of cathepsin L activity, and furthermore useful as a medicine for treating diseases in which cathepsin B and L participate, such as muscular dystrophy and muscular atrophy.
La présente invention concerne des dérivés d'acide époxysuccinique représentés par la formule générale (I). Dans cette formule, R<1> est hydrogène, alkyle, aryle ou aralkyle. R<2> et R<3> sont chacun indépendamment aryle, aralkyle ou alkyle. X est -O- ou -NR<4>-, R<4> étant hydrogène, alkyle ou aralkyle. Ces dérivés conviennent avantageusement à la prévention ou au traitement des affections osseuses telles que l'ostéoporose, l'hypercalcémie maligne, et le syndrome osseux de Behcet. Ces dérivés conviennent avantageusement également au traitement de l'arthrose et de la polyarthrite rhumatoïde liée à l'hypergasie de la cathepsine L, ainsi que comme remède contre les affections, telles que la dystrophie musculaire et l'amyotrophie, dans lesquelles interviennent les cathepsines L et B.
Hara Kaoru
Masaki Mitsuo
Nomura Yutaka
Takahashi Toshihiro
Yoshino Yasushi
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Nippon Chemiphar Co. Ltd.
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