Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1989-03-09
1990-10-02
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546196, 548525, 549510, 514320, 514422, 514908, A61K 31335, C07D30514
Patent
active
049607901
ABSTRACT:
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.
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Mathew Abraham E.
Stella Valentino J.
Raymond Richard L.
Russell Mark W.
University of Kansas
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