Maytansinoids, their use and pharmaceutical compositions thereof
First Claim
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1. A compound of the formula:
- ##STR4## wherein Y is H or Cl, and R is phenyl-C1-4 alkyl, pyridyl-C1-4 alkyl, imidazolyl-C1-4 alkyl, indolyl-C1-4 alkyl, furyl-C1-4 alkyl or thienyl-C1-4 alkyl, each of said groups being substituted at either or both α
- and β
-positions by hydroxyl, halogen or C1-5 alkanoyloxy.
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Abstract
Novel maytansinoids of the formula: ##STR1## wherein Y is H or Cl, and R is C2-15 alkyl, phenyl-C1-4 alkyl, pyridyl-C1-4 alkyl, imidazolyl-C1-4 alkyl, indolyl-C1-4 alkyl, furyl-C1-4 alkyl or thienyl-C1-4 alkyl, said R group being substituted by hydroxyl, halogen or C1-5 alkanoyloxy at its α- and/or β-position, have antimitotic, antitumor and antimicrobial activities.
163 Citations
12 Claims
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1. A compound of the formula:
- ##STR4## wherein Y is H or Cl, and R is phenyl-C1-4 alkyl, pyridyl-C1-4 alkyl, imidazolyl-C1-4 alkyl, indolyl-C1-4 alkyl, furyl-C1-4 alkyl or thienyl-C1-4 alkyl, each of said groups being substituted at either or both α
- and β
-positions by hydroxyl, halogen or C1-5 alkanoyloxy. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8)
- ##STR4## wherein Y is H or Cl, and R is phenyl-C1-4 alkyl, pyridyl-C1-4 alkyl, imidazolyl-C1-4 alkyl, indolyl-C1-4 alkyl, furyl-C1-4 alkyl or thienyl-C1-4 alkyl, each of said groups being substituted at either or both α
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9. Maytansinol 3-(2,2-dimethyl)-1,3-dioxolan-4-carboxylate.
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10. Maytansinol 3-α
- -acetoxyphenylacetate.
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11. 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-C1-4 alkyl, pyridyl-C1-4 alkyl, imidazolyl-C1-4 alkyl, indolyl-C1-4 alkyl, furyl-C1-4 alkyl or thienyl-C1-4 alkyl, each of said groups being substituted at either or both α
- and β
-positions by hydroxyl, halogen or C1-5 alkanoyloxy.
- ##STR5## wherein Y is H or Cl, and R is phenyl-C1-4 alkyl, pyridyl-C1-4 alkyl, imidazolyl-C1-4 alkyl, indolyl-C1-4 alkyl, furyl-C1-4 alkyl or thienyl-C1-4 alkyl, each of said groups being substituted at either or both α
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12. 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-C1-4 alkyl, pyridyl-C1-4 alkyl, imidazolyl-C1-4 alkyl, indolyl-C1-4 alkyl, furyl-C1-4 alkyl or thienyl-C1-4 alkyl, each of said groups being substituted at either or both α
- and β
-positions by hydroxyl, halogen or C1-5 alkanoyloxy.
- ##STR6## wherein Y is H or Cl, and R is phenyl-C1-4 alkyl, pyridyl-C1-4 alkyl, imidazolyl-C1-4 alkyl, indolyl-C1-4 alkyl, furyl-C1-4 alkyl or thienyl-C1-4 alkyl, each of said groups being substituted at either or both α
Specification
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Current AssigneeTakeda Chemical Industries, Ltd. (Takeda Pharmaceutical Company Limited)
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Original AssigneeTakeda Chemical Industries, Ltd. (Takeda Pharmaceutical Company Limited)
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InventorsAkimoto, Hiroshi, Miyashita, Osamu
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Primary Examiner(s)BOND, ROBERT
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Application NumberUS06/152,392Time in Patent Office649 DaysField of Search260/239.3 P, 424/248.54US Class Current514/229.5CPC Class CodesA61P 35/00 Antineoplastic agentsC07D 498/18 Bridged systems
