C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 225/06 (2006.01) A61K 31/395 (2006.01)
Patent
CA 2651557
The present invention relates to 17-oxymacbecin analogues according to the formula (IA) or (IB) below, or a pharmaceutically acceptable salt thereof, wherein: R1 represents H, OH or OCH3; R2 represents H or CH3 R3 represents H or CONH2 R4 and R5 either both represent H or together they represent a bond (i.e. C4 to C5 is a double bond); and R6 represents H or OH; and R7 represents H or CH3. that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and / or prophylaxis of cancer or B-cell malignancies.
L'invention concerne des analogues de 17-oxymacbécine selon la formule (IA) ou (IB), ou un sel de ceux-ci pharmaceutiquement acceptables. R1 représente H, OH ou OCH3; R2 représente H ou CH3; R3 représente H ou CONH2; R4 et R5 représentent tous deux H ou ensemble une liaison (c'est-à-dire C4 à C5 est une liaison double); et R6 représente H ou OH; et R7 représente H ou CH3; on les utilise, par exemple, dans le traitement du cancer, des malignités touchant les lymphocytes B, du paludisme, d'infection fongique, des maladies du système nerveux central et des maladies neurodégénératives, des maladies dépendant de l'angiogenèse, des maladies auto-immunes et/ou comme prétraitement prophylactique du cancer. L'invention concerne en outre des procédés de production de ces composés et leur utilisation en médecine, notamment dans le traitement et/ou la prophylaxie du cancer ou de malignités touchant les lymphocytes B.
Coates Nigel
Gaisser Sabine
Martin Christine
Zhang Ming
Biotica Technology Limited
Norton Rose Or S.e.n.c.r.l. S.r.l./llp
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