Maytansinoids, pharmaceutical compositions thereof and method of use thereof
AssigneeTakeda Chemical Industries, Ltd.
InventorsOsamu Miyashita, Hiroshi Akimoto
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Abstract
Novel maytansinoid compounds of the formula: ##STR1## wherein X is H or Cl, R.sup.1 is an alkyl group of 2 to 4 carbon atoms and R.sup.2 is a lower alkyl group or an unsubstituted or substituted phenyl or aralkyl group, have antimitotic, antitumor and antimicrobial activities.
Claims13
A compound of the formula:
- ##STR6## wherein X is H or Cl, R.sup.1 is C.sub.2-4 alkyl and R.sup.2 is C.sub.1-4 alkyl, phenyl or phenyl-C.sub.1-3 alkyl, said phenyl or phenyl-C.sub.1-3 alkyl being unsubstituted or substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro, amino, mono or di-C.sub.1-4 alkylamino, mono- or di-C.sub.1-4 alkanoylamino, halogenated mono- or di-C.sub.1-4 alkanoylamino, halogen or halogenated C.sub.1-4 alkyl.
A pharmaceutical composition suitable for inhibiting the growth of tumor cells and prolonging the survival time of a tumor-bearing warm-blooded animal, which comprises as an active ingredient an effective amount of a compound of the formula:
- ##STR7## wherein X is H or Cl, R.sup.1 is C.sub.2-4 alkyl and R.sup.2 is C.sub.1-4 alkyl, phenyl or phenyl-C.sub.1-3 alkyl, said phenyl or phenyl-C.sub.1-3 alkyl being unsubstituted or substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro, amino, mono- or di-C.sub.1-4 alkylamino, mono- or di-C.sub.1-4 alkanoylamino, halogenated mono- or di-C.sub.1-4 alkanoylamino, halogen or halogenated C.sub.1-4 alkyl, and a pharmaceutically acceptable carrier or diluent therefor.
A method for inhibiting the growth of tumor cells and prolonging the survival time of a tumor-bearing warm-blooded animal, which comprises administering to said animal an effective amount of a compound of the formula:
- ##STR8## wherein X is H or Cl, R.sup.1 is C.sub.2-4 alkyl and R.sup.2 is C.sub.1-4 alkyl, phenyl or phenyl-C.sub.1-3 alkyl, said phenyl or phenyl-C.sub.1-3 alkyl being unsubstituted or substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, nitro, amino, mono- or di-C.sub.1-4 alkylamino, mono- or di-C.sub.1-4 alkanoylamino, halogenated mono- or di-C.sub.1-4 alkanoylamino, halogen or halogenated C.sub.1-4 alkyl.
Dependencies are inferred from the claim text.