Mitomycin derivatives as antileukemia agents
AssigneeKyowa Hakko Kogyo Co., Ltd.
InventorsTokuyuki Kuroda, Koji Hisamura, Tohru Sugaya, Yutaka Ohsawa, Hideo Ueno, Makoto Morimoto, Tadashi Ashizawa
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AssigneeKyowa Hakko Kogyo Co., Ltd.
InventorsTokuyuki Kuroda, Koji Hisamura, Tohru Sugaya, Yutaka Ohsawa, Hideo Ueno, Makoto Morimoto, Tadashi Ashizawa
Estimating the term…
Mitomycin derivatives having potent antitumor activity having the formula: ##STR1## wherein A is ON--or R.sub.4 N.dbd.N--[wherein R.sub.4 is selected from ##STR2## and optionally substituted heterocyclic groups (wherein R.sub.5 and R.sub.8 are each independently selected from hydrogen, lower alkyl and lower cycloalkyl; R.sub.6 is selected from hydrogen, halogen, hydroxy, lower alkoxy, amino and nitro; R.sub.7 is selected from lower alkyl and lower cycloalkyl; and X is selected from oxygen, sulphur and imino)]; R.sub.1 and R.sub.2 are each independently selected from hydrogen, lower alkyl, lower cycloalkyl, optionally substituted aralkyl, optionally substituted alkanoyl, optionally substituted arylcarbonyl, optionally substituted alkanesulfonyl, arylsulfonyl and aralkylsulfonyl; R.sub.3 is hydrogen or carbamoyl; Y is hydrogen or methyl; Z is selected from hydrogen, methyl and acetyl; and is an .alpha. or .beta. bond.
Mitomycin compounds represented by the formula:
(1aS-(1a.alpha.,8.beta.,8a.alpha.,8b.alpha.))-4,7-d ihydroxy-1,1a,2,8,8a,8b-hexahydro-8-hydroxymethyl-8a-methoxy-5-methyl-6-nit roso-azirino[2',3':3,4]pyrrolo[1,2-a]indole.
(1aS-(1a.alpha.,8.beta.,8a.alpha.,8b.alph a.))-8-{[(aminocarbonyl)oxy]methyl}-4,8a-dimethoxy-1,1a,2,8,8a,8b-hexahydro -7-hydroxy-5-methyl-6-nitroso-azirino[2',3':3,4]pyrrolo[1,2-a]indole.
(1aS-(1a.alpha.,8.beta.,8a.alpha.,8b.alpha.))-8-{[(aminocarbonyl) oxy]methyl}-1,1a,2,8,8a,8b-hexahydro-5-methyl-6-nitroso-4,7,8a-trimethoxy-a zirino[2',3':3,4]pyrrolo[1,2-a]indole.
(1aS-(1a.alpha.,8.beta.,8a.alpha., 8b.alpha.))-1-acetyl-4-acetyloxy-8-{[(aminocarbonyl)oxy]methyl}-1,1a,2,8,8a ,8b-hexahydro-7-hydroxy-8a-methoxy-5-methyl-6-nitroso-azirino(2',3':3,4)pyr rolo(1,2-a)indole.
(1aS-(1a.alpha .,8.beta.,8a.alpha.,8b.alpha.))-8-{(aminocarbonyl)oxy)methyl}-1,1a,2,8-8a,8 b-hexahydro-7-hydroxy-8a-methoxy-5-methyl-6-nitroso-4-(p-toluenesulfonyl)ox y)azirino(2',3':3,4)pyrrolo(1,2-a)indole.
(1aS-(1a.alpha.,8.beta.,8a.alpha.,8b. alpha.)-8-{(aminocarbonyl)oxy)methyl}-4,7-dihydroxy-1,1a,2,8,8a,8b-hexahydr o-8a-methoxy-5-methyl-6-{((methylthio)thiocarbonyl)azo}azirino(2',3':3,4)py rrolo(1,2-a)indole.
Dependencies are inferred from the claim text.