Maytansinoids and use
AssigneeTakeda Chemical Industries, Ltd.
InventorsOsamu Miyashita, Hiroshi Akimoto
Life of this patent
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Abstract
Novel maytansinoids of the formula: ##STR1## wherein R is an alicyclic hydrocarbon group of 3 to 10 carbon atoms, phenyl or heterocyclic group, which may optionally be substituted, and A is an alkylene group of 1 to 4 carbon atoms or a bond, provided that A means said alkylene group when attached to a N atom in said heterocyclic group R, have antimicrobial, antimitotic and antitumor activities.
Claims13
A compound of the formula:
- ##STR4## wherein R is C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, phenyl or a heterocyclic group selected from the class consisting of pyridyl, pyrrolidinyl, tetrazolyl, furyl and thienyl, said cycloalkyl, cycloalkenyl, phenyl and heterocyclic group being unsubstituted or substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.2-4 alkanoyl, C.sub.2-4 alkanoyloxy, C.sub.2-4 alkoxycarbonyl, halogen, nitro, cyano, trifluoromethyl, di-C.sub.1-4 alkylamino, C.sub.1-4 alkylthio, methylsulfinyl, methylsulfonyl, oxo, thioxo or C.sub.1-4 alkanoylamido, and
- A is C.sub.1-4 alkylene or a bond, provided that A means said alkylene when attached to a N atom in said heterocyclic group R.
A pharmaceutical composition suitable for inhibiting the growth of tumour cells and prolonging the survival time of a warm-blooded animal which comprises as an active ingredient an effective amount of a compound of the following formula (I) and a pharmaceutically acceptable carrier or diluent therefor:
- ##STR5## wherein R is C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, phenyl or a heterocyclic group selected from the class consisting of pyridinyl, pyrrolidinyl, tetrazolyl, furyl and thienyl, said cycloalkyl, cycloalkenyl, phenyl and heterocyclic group being unsubstituted or substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.2-4 alkanoyl, C.sub.2-4 alkanoyloxy, C.sub.2-4 alkoxycarbonyl, halogen, nitro, cyano, trifluoromethyl, di-C.sub.1-4 alkylamino, C.sub.1-4 alkylthio, methylsulfinyl, methylsulfonyl, oxo, thioxo or C.sub.1-4 alkanoylamido, and
- A is C.sub.1-4 alkylene or a bond, provided that A means said alkylene when attached to a N atom in said heterocyclic group R.
A method for inhibiting the growth of tumour cells and prolonging the survival time of a tumour-bearing warm-blooded animal, which comprises administering to said animal an effective amount of a compound of the formula:
- ##STR6## wherein R is C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, phenyl or heterocyclic group selected from the class consisting of pyridyl, pyrrodinyl, tetrazolyl, furyl and thienyl, said cycloalkyl, cycloalkenyl, phenyl and heterocyclic group being unsubstituted or substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.2-4 alkanoyl, C.sub.2-4 alkanoyloxy, C.sub.2-4 alkoxycarbonyl, halogen, nitro, cyano trifluoromethyl, di-C.sub.1-4 alkylamino, C.sub.1-4 alkylthio, methylsulfinyl, methylsulfonyl, oxo, thioxo or C.sub.1-4 alkanoylamido, and
- A is C.sub.1-4 alkylene or a bond, provided that A means said alkylene when attached to a N atom in said heterocyclic group R.
Dependencies are inferred from the claim text.