C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/299
C07D 487/04 (2006.01) C07D 487/14 (2006.01) C07F 9/24 (2006.01) C07F 9/6561 (2006.01)
Patent
CA 1239645
ABSTRACT 7-Acylamino-9a-methoxymitosanes having enhanced capacity to inhibit animal tumors in vivo relative to mitomycin C are produced by N7-acylation of 7-amino-9a-methoxymitosane, or N1a,N7-diacylation thereof. Carboxamide, thiocarboxamide, urea, thiourea, urethane, thiophosphoramide, phosphoramide, and sulfonamide derivatives are disclosed. These compounds conform to the following formula: Image Formula III wherein R1 is selected from H, C1-6 alkyl, and R7, R7 is selected from Image wherein Ra is selected from H, C1-6 alkyl, A-substituted C1-6 alkyl, C6-10 aryl, A-substituted C6-10 aryl, C7-17 aralkyl, A-substituted C7-17 aralkyl, C2-6 alkenyl, A-substituted C2-6 alkenyl, C2-6 alkynyl, A-substituted C2-6 alkynyl, C3-8 cycloalkyl, C4-10 cycloalkylalkyl, Rb is selected from the group consisting of C1-6 alkyl, A-substituted C1-6 alkyl, C6-10 aryl, A-substituted C6-10 aryl, C7-17 aralkyl and A-substituted C7-17 aralkyl, wherein said A substituent is selected from the group consisting of chlorine, bromine, fluorine, iodine, amino, protected amino, C1-6 alkoxy, C1-6 alkylamino, di(C1-6)alkylamino, C3-8 cycloalkylamino, C4-14 cycloalkylamino, thiol, C1-6 alkylthio, C1-6 alkyldithio, C6-10 arylthio, and C7-17 aralkylthio.
469874
Doyle Terrence W.
Kaneko Takushi
Wong Henry S.l.
Bristol-Myers Company
Gowling Lafleur Henderson Llp
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