Patent ReferencesDerivatives of 5,5-diphenylhydantoin exhibiting enhanced solubility and the therapeutic use thereof Prodrugs of rapamycin Patent #: 4650803 InventorsAssigneeApplicationNo. 321152 filed on 03/09/1989US Classes:514/449, Oxygen containing hetero ring514/320, Hetero ring in the polycyclo ring system514/422, Additional hetero ring514/908, LEUKEMIA546/196, Hetero ring in the polycyclo ring system548/525, Polycyclo ring system which includes ring chalcogen549/510The hetero ring is four-memberedExaminersPrimary: Raymond, Richard L.Assistant: Russell, Mark W. Attorney, Agent or FirmInternational ClassesA61K 031/335C07D 305/14 AbstractDerivatives 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 R2 and R3 are each hydrogen on an alkyl radical having from one to three carbon atoms or wherein R2 and R3 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 R1 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.Other References
Field of SearchThe hetero ring is four-memberedSulfur or halogen attached directly or indirectly to the hetero ring by nonionic bonding Oxygen containing hetero ring LEUKEMIA Hetero ring in the polycyclo ring system Additional hetero ring Polycyclo ring system which includes ring chalcogen Hetero ring in the polycyclo ring system |
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