AMINOBORANE ACID DERIVATIVE AND PROTEASOME INHIBITORY DRUG CONTAINING THE SAME

• Main Authors: NAKAMARU, KOICHI, TACHIBANA, YOJI, KOJIMA, RYOTARO, SATOH, HIROAKI, UENO, MASAHIRO
• Format: Patent
• Language: English; French; Japanese
• Published: 24.04.2003
• Edition: 7
• Subjects: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

A novel aminoborane acid derivative represented by the general formula (1): (1) (wherein X is a group of the general formula (2), (3), or (4); (2) (3) (4) Y is the group of the formula (5) or (6); (5) (6) R1 and R2 are the same or different and each is C3−6 alkyl or C1−6 alkyl substituted by phenyl; Z1 is oxygen or sulfur; Z2 is hydrogen, methoxy, or halogeno; and m is 1 or 2), which has proteasome inhibitory activity. The compound having proteasome inhibitory activity is useful as an immunosuppressant, anti−inflammatory agent, antiallergic, remedy for autoimmune diseases, remedy for chronic inflammatory diseases such as inflammatory bowel diseases (ulcerative colitis and Crohn's disease), anticancer agent, or remedy for nerve degeneration diseases. A novel aminoborane acid derivative represented by the general formula 1: 1 wherein X is a group of the general formula 2, 3, or 4 2 3 4 Y is the group of the formula 5 or 6 5 6 R1 and R2 are the same or different and each is C3-6 alkyl or C1-6 alkyl substituted by phenyl Z1 is oxygen or sulfur Z2 is hydrogen, methoxy, or halogeno and m is 1 or 2, which has proteasome inhibitory activity. The compound having proteasome inhibitory activity is useful as an immunosuppressant, anti-inflammatory agent, antiallergic, remedy for autoimmune diseases, remedy for chronic inflammatory diseases such as inflammatory bowel diseases ulcerative colitis and Crohn's disease, anticancer agent, or remedy for nerve degeneration diseases. La présente invention concerne un nouveau dérivé d'acide d'aminoborane représenté par la formule générale (1) (où x représente un groupe de formule générale (2), (3) ou (4) ; Y représente le groupe de formule (5) ou (6) ; R1 et R2 sont identiques ou différents et chacun représente alkyle C3-6 ou alkyle C1-6 substitué par du phényle ; Z-1 représente oxygène ou soufre ; Z2 représente hydrogène, méthoxy ou halogène ; et m représente 1 ou 2), qui présente une activité inhibitrice de protéasomes. Ledit composé à activité inhibitrice de protéasomes est utile en tant qu'immunosuppresseur, agent anti-inflammatoire, antiallergique, remède contre les maladies auto-immunes, remède contre les maladies inflammatoires chroniques telles que les maladies entériques inflammatoires (colite ulcéreuse et maladie de Crohn), agent anticancéreux ou remède contre les maladies de dégénérescence nerveuse.