Dr. Reddy's Laboratories, Incorporated

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Dr. Reddy's Research Foundation

Subrahmanyam Duvvuri

Venkateswarlu Akella

Sriram K Rajagopal

Shanavas Alikunju

Sharma Manohara Vedula

Raju Sirisilla

Ajaya Kumar Reka

Ramesh Mullangi

Sairam Pothukuchi

Vamsee Krishna Chintakunta

Archana Prabhakar Kulakarni

Rao Venkateswara Kalla

Srinivas Ssv Akella

Raghavendra Madhva Sattegeri

Sastry V R S Thungathurthi

Shobha Madabhushi

Sharma Manohar Vedula

Ramachandra Puranik

A 5(S)-(2'-hydroxyethoxy)-20(S)-camptothecin diasterisomer is described which is a better inhibitor of topoisomerase I than either the diastereoisomeric mixture 5(RS)-(2&#x2032;-hydroxyethoxy)-20(S)-camptothecin, or the 5(R)-(2&#x2032;-hydroxyethoxy)-20(S)-camptothecin diastereoisomer. Pharmaceutical compositions of the 5(S)-(2&#x2032;-hydroxyethoxy)-20(S)-camptothecin diastereoisomer are also described as are methods of using the compound for the inhibition of topoisomerase I and for the treatment of cancer.

5(S)-(2'-hydroxyethoxy)-20(S)-camptothecin and its preparation and use for the treatment of cancer

A crystalline form of 5(S)-(2'-hydroxyethoxy)-20(S)-camptothecin diastereoisomer of 5(RS)-(2&#x2032;-hydroxyethoxy)-20(S)-camptothecin is described that is characterized by having an X-ray powder diffraction pattern comprising one or more peak intensities expressed in degrees 2&#x3b8; that are selected from the group consisting of 7.2&#xb1;0.1, 9.4&#xb1;0.1, 11.02&#xb1;0.1, 12.00&#xb1;0.1, 14.54&#xb1;0.1, 15.2&#xb1;0.1, 18.92&#xb1;0.1, 21.86&#xb1;0.1, 22.74&#xb1;0.1 and 26.42&#xb1;0.1. Methods of making and using the compound are also described.

Crystalline form of 5(S)-(2-hydroxyethoxy)-20(S)-camptothecin

Described are pharmaceutically acceptable salts of a compound of formula (I) its tautomeric forms, its stereoisomers or its polymorphs, which is obtained by treating the compound of formula (I) with an acid selected from the group consisting of hydrohalo acid selected from the group consisting of hydrochloric acid or hydrobromic acid, acetic acid; sulfuric acid, nitric acid, phosphoric acid, boric acid, perchloric acid, tartaric acid, maleic acid, citric acid, methanesulfonic acid, benzoic acid, ascorbic acid, salicylic acid and benzene sulfonic acid wherein Rrepresents substituted (C&#x2013;C) alkyl wherein the substituent(s) is selected from mono (C&#x2013;C) alkylamino or di (C&#x2013;C) alkylamino; Rrepresents hydroxy;

Pharmaceutically acceptable salts of 20(s)-camptothecins

Novel water soluble C-ring analogues of 20(S)-camptothecin having the general formula 1.

Water soluble analogues of 20(S)-camptothecin

Novel water soluble C-ring analogues of 20(S)-camptothecin having the general formula 1,

Novel water soluble C-ring analogs of 20(S)-camptothecin having the formula 1. ##STR1## The compounds of the formula 1 are prepared from the compounds of the formula 12 having C-20(S) chiral carbon. The compounds of the formula 1 possess potent anti-cancer and anti-viral properties.

Water soluble C-ring analogues of 20(S)-camptothecin

Novel taxane derivatives and intermediates having the formula 1. ##STR1## and a process for the preparation of the compounds of the formula 1 from 14-.beta.-hydroxy-10-deacetylbaccatin III of formula 2 ##STR2## and pharmaceutically acceptable compositions containing the taxane derivatives and intermediates of formula 1.

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Hyderabad Telangana, India

Subrahmanyam Duvvuri