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AssigneeUniversity of Kansas
InventorsValentino J. Stella, Abraham E. Mathew
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Derivatives of taxol represented by the formula ##STR1## wherein R and R' are each H or the residue of an amino acid selected from the group consisting of alanine, leucine, isoleucine, saline, phenylalanine, proline, lysine and arginine or a group of the formula ##STR2## wherein n is an integer of 1 to 3 and R.sup.2 and R.sup.3 are each hydrogen on an alkyl radical having from one to three carbon atoms or wherein R.sup.2 and R.sup.3 together with the nitrogen atom to which they are attached form a saturated heterocyclic ring having four to five carbon atoms, with the proviso that at least one of R and R.sup.1 is not hydrogen, are provided together with pharmaceutical compositions of such derivatives. The taxol derivatives have increased water solubility as compared to taxol, and have excellent antitumor activity.
A compound of the formula ##STR19## wherein R and R' are each H or the residue of an amino acid selected from the group consisting of alanine, leucine, isoleucine, valine, phenylalanine, proline, lysine and arginine or a group of the formula ##STR20## wherein n is an integer of 1 to 3 and R.sup.2 and R.sup.3 are each hydrogen or an alkyl radical having from one to three carbon atoms or wherein R.sup.2 and R.sup.3 together with the nitrogen atom to which they are attached form a saturated heterocyclic ring having four or five carbon atoms or an acid addition salt thereof, with the proviso that at least one of R and R.sup.1 is not hydrogen, and with the second proviso that said compound is not 2'-(.beta.-alanyl)taxol.
A pharmaceutical composition comprising an effective antitumor amount of at least one compound of the formula ##STR22## wherein R and R' are each H or the residue of an amino acid selected from the group consisting of alanine, leucine, isoleucine, valine, phenylalanine, proline, lysine and arginine or a group of the formula ##STR23## wherein n is an integer of 1 to 3 and R.sup.2 and R.sup.3 are each hydrogen or an alkyl radical having from one to three carbon atoms or wherein R.sup.2 and R.sup.3 together with the nitrogen atom to which they are attached form a saturated heterocyclic ring having four to five carbon atoms, with the proviso that at least one of R and R.sup.1 is not hydrogen, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent or excipient.
A taxol derivative selected from the group consisting of
Dependencies are inferred from the claim text.