Patent NZ-520521-A (NZ)
Title: Compounds having antitumor activity: process for their preparation and pharmaceutical compositions containing them
Inventor: NANDURI SRINIVAS
IPC: A61P33/06
Filed: 2001-02-02
Abstract: A compound of formula (1) and its stereoisomers, polymorphs and pharmaceutically acceptable salts are described wherein: R1, R2 and R3 are the same or different and independently represent hydrogen or substituted or unsubstituted groups selected from linear or branched (C1-C8) alkyl group, phenyl, heteroaryl group selected from pyridyl, furyl or thiophenyl; aralkyl selected from benzyl or phenethyl; heteroaralkyl group selected from pyridylmethyl, pyridylethyl, furanmethyl or furanethyl; (C2-C8) alkanoyl, (C3-C8) alkenoyl, benzoyl, heteroaroyl group selected from pyridyl carbonyl or furyl carbonyl; sulfonyl group selected from methanesulfonyl, benzenesulfonyl or p-toluenesulfonyl; or a group -(CO)-W-R4 where W represents O, S or NR5, wherein R5 represents hydrogen or( C1-C6)alkyl group, R4 represents substituted or unsubstituted groups selected from (C1-C8)alkyl, phenyl, benzoyl, or aralkyl selected from benzyl or phenethyl, when the group represented by R4 is substituted the substituent is selected from halogen atom, amino, cyano, hydroxy, nitro, trifluorethyl, (C1-C8)alkyl or (C1-C6) alkoxy; Or R2 and R3 together form a substituted or unsubstituted 5 to 7 membered cyclic structure containing carbon and oxygen atoms; wherein the substituents on R1, R2 and R3 are selected from cyano, hydroxy, nitro, halogen atom, amino, alkanoyl, aroyl, acyloxy (C1-C6) alkoxy, substituted or unsubstituted (C1-C8) alkyl, wherein when the alkyl group is substituted the substituent is selected from halogen, hydroxy, nitro, cyano, amino, phenyl or (C1-C6) alkoxy; substituted of unsubstituted aryl group selected from phenyl or napthyl wherein when the aryl group is substituted the substituent is selected from (C1-C6) alkyl, halogen atom, amino, cyano, hydroxy, nitro, trifluoroethyl or (C1-C6) alkoxy; and wherein the aryl group is disubstituted, the two substituents on the adjacent carbon atoms form a linking group selected from -X-CH2-Y-, -X-CH2-CH2-Y-, where X and Y may be same or different and independently represent O, N, S or CH2; thio, thioalkyl, alkylthio, heteroaryl selected from pyridyl, furyl or thienyl; mono(C1-C6) alkylamino, di(C1-C6)alkylamino, acylamino, arylamino, aralkylamino,alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, or COOR, where R represents hydrogen or(C1-C6)alkyl groups; wherein when the groups represented by R1, R2 or R3 are multisubstituted, the substituents present on the two adjacent carbons may form a linking group -X-(CR6R7)n-Y- where R6 and R7 represent (C1-C8)alkyl, X and Y may be same or different and independently represent CH,O, S or NH; and n = 1 or 2. Also described is a process of preparing the compounds of formula (1). The compounds are useful in preparing a medicament fro treating cancer, psoriasis, HSV, HIV, restenosis, atherosclerosis, viral infections, malaria, bacterial infections, immunomodulation, liver disorders, cardiovascular disorders, diabetes, dyslipidemia, other metabolic disorders, insulin resistance (type II diabetes), leptin resistance, impaired glucose tolerance, dyslipidemia, body weight reduction or disorders related to syndrome X.