C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 17/02 (2006.01) A61K 31/706 (2006.01) A61P 35/00 (2006.01)
Patent
CA 2361624
Novel compounds represented by the general formula (I) or salts thereof, which are reduced in toxicity and improved in anticancer activity as compared with known carcinostatic anthracycline derivatives (I), (wherein A is methyl or CF3; B is hydrogen or an electron-withdrawing group such as halogeno, provided that when A is CF3, B is hydrogen, while when A is methyl, B is an electron- withdrawing group; and R1 and R2 are each hydroxyl or the like). Novel water- soluble carcinostatic compounds, represented by general formula (V), (wherein A and B are each as defined above; and R5, R6 and R7 are each hydrogen or an .omega.-amino acid residue, with the proviso that the cases wherein all of R5, R6 and R7 are hydrogen are excepted).
L'invention concerne des composés représentés par la formule (I), y compris leurs sels, dont la toxicité est réduite et qui ont un effet anticancéreux amélioré par rapport aux dérivés carcinostatiques connus d'anthracycline. Dans ladite formule, A est méthyle ou CF¿3?; B est hydrogène ou un groupe suppresseur d'électrons du type halogéno, à condition que, lorsque A est CF¿3?, B soit hydrogène, et que, lorsque A est méthyle, B soit un groupe suppresseur d'électrons; et R?1¿ et R?2¿ sont chacun hydroxyle ou autre. L'invention concerne en outre des composés carcinostatiques hydrosolubles représentés par la formule (V). Dans ladite formule, A et B sont tels que définis ci-dessus; et R?5¿, R?6¿ et R?7¿ sont chacun hydrogène ou un résidu d'acide aminé .omega., à condition que R?5¿, R?6¿ et R?7¿ ne soient pas tous hydrogène.
Sohtome Hiromi
Takagi Yasushi
Takeuchi Tomio
Tsuchiya Tsutomu
Umezawa Sumio
Macrae & Co.
Sohtome Hiromi
Takagi Yasushi
Takeuchi Tomio
Tsuchiya Tsutomu
LandOfFree
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