Maytansinoids, their use and pharmaceutical compositions thereof
AssigneeTakeda Chemical Industries, Ltd.
InventorsOsamu Miyashita, Hiroshi Akimoto
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Abstract
Novel maytansinoids of the formula: ##STR1## wherein Y is H or Cl, and R is C.sub.2-15 alkyl, phenyl-C.sub.1-4 alkyl, pyridyl-C.sub.1-4 alkyl, imidazolyl-C.sub.1-4 alkyl, indolyl-C.sub.1-4 alkyl, furyl-C.sub.1-4 alkyl or thienyl-C.sub.1-4 alkyl, said R group being substituted by hydroxyl, halogen or C.sub.1-5 alkanoyloxy at its .alpha.- and/or .beta.-position, have antimitotic, antitumor and antimicrobial activities.
Claims12
A compound of the formula:
- ##STR4## wherein Y is H or Cl, and R is phenyl-C.sub.1-4 alkyl, pyridyl-C.sub.1-4 alkyl, imidazolyl-C.sub.1-4 alkyl, indolyl-C.sub.1-4 alkyl, furyl-C.sub.1-4 alkyl or thienyl-C.sub.1-4 alkyl, each of said groups being substituted at either or both .alpha.- and .beta.-positions by hydroxyl, halogen or C.sub.1-5 alkanoyloxy.
Maytansinol 3-(2,2-dimethyl)-1,3-dioxolan-4-carboxylate.
Maytansinol 3-.alpha.-acetoxyphenylacetate.
A pharmaceutical composition 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:
- ##STR5## wherein Y is H or Cl, and R is phenyl-C.sub.1-4 alkyl, pyridyl-C.sub.1-4 alkyl, imidazolyl-C.sub.1-4 alkyl, indolyl-C.sub.1-4 alkyl, furyl-C.sub.1-4 alkyl or thienyl-C.sub.1-4 alkyl, each of said groups being substituted at either or both .alpha.- and .beta.-positions by hydroxyl, halogen or C.sub.1-5 alkanoyloxy.
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:
- ##STR6## wherein Y is H or Cl, and R is phenyl-C.sub.1-4 alkyl, pyridyl-C.sub.1-4 alkyl, imidazolyl-C.sub.1-4 alkyl, indolyl-C.sub.1-4 alkyl, furyl-C.sub.1-4 alkyl or thienyl-C.sub.1-4 alkyl, each of said groups being substituted at either or both .alpha.- and .beta.-positions by hydroxyl, halogen or C.sub.1-5 alkanoyloxy.
Dependencies are inferred from the claim text.