Substituted aralkyl derivatives
AssigneeCadila Healthcare Limited
InventorsBraj Lohray, Vidya Lohray, Mukul Jain, Sujay Basu, Harikishore Pingali, Saurin Raval, Preeti Raval
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Abstract
The present invention relates to novel substituted aralkyl derivatives of the general formula (I) and (IIIa), their derivatives, their analogs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, pharmaceutical compositions containing them, use of these compounds in medicine and the intermediates involved in their preparation.
Claims30
A compound of the general formula (I),
- , their analogs, their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, wherein
- ‘A’ represents a substituted or unsubstituted, group selected from aryl, heteroaryl, heterocyclyl groups;
- ‘n’ is an integer from 1-3, with the proviso that when A is substituted or unsubstituted phenyl group, then Ar does not represent a divalent phenyl group;
- ‘X’ represents oxygen or sulfur;
- ‘Ar’ represents a substituted or unsubstituted single or fused divalent aromatic, heteroaromatic or a heterocyclic group;
- G1 represents OR1, SR1, S(O)R3, S(O)2R3, N3, CN, COOH, tetrazolyl groups;
- G2 represents OR1, NR1R2, SR1, S(O)R3, S(O)2R3, N3, CN, COOH, tetrazolyl groups;
- R1, R2 represents hydrogen, substituted or unsubstituted groups selected from linear or branched (C1-C8)alkyl, (C3-C7)cycloalkyl, acyl, aryl, heteroaryl, heterocyclyl, aminocarbonyl, aralkyl, alkylaminocarbonyl, arylaminocarbonyl, aralkylaminocarbonyl, heteroarylaminocarbonyl, heteroaralkylaminocarbonyl, heterocyclylaminocarbonyl, alkoxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl, heteroaryloxycarbonyl, heteroaraloxycarbonyl, heterocycloxycarbonyl groups;
- R3 represents substituted or unsubstituted groups selected from alkyl, aryl, polyhaloalkyl, heterocyclyl, heteroaryl groups;
- with the proviso that, when G2 represents NR1R2, G1 does not represent —OH group;
- G3 represents hydrogen or (C1-C8)alkyl or (C3-C7)cycloalkyl groups.
Novel compounds of formula (IIIa), their analogs, their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, wherein ‘A’ represents 4-oxazolyl group substituted with one or two substitutents selected from substituted or unsubstituted linear or branched (C1-C12)alkyl, substituted or unsubstituted single or fused heteroaryl or heterocyclic groups with the proviso that one of the substituents on “A” is always a heteroaryl or heterocyclic group and with the further proviso that when the heteroaryl is pyridyl group, such group is unsubstituted;
- ‘Ar’ represents unsubstituted phenyl;
- G1 represents OR1 or SR, where R1 represents hydrogen, perfluoro(C1-C12)alkyl, substituted or unsubstituted groups selected from linear or branched (C1-C12)alkyl, cyclo(C1-C12)alkyl, aryl, ar(C1-C12)alkyl, heteroaryl, heteroar(C1-C12)alkyl, heterocyclyl, alkoxyalkyl, aryloxyalkyl, alkoxycarbonyl, aryloxycarbonyl, cycloalkyloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl or acyl groups;
- R4 represents OH, alkoxy or aryloxy, aralkoxy or NR1R2 groups, where R1 & R2 may be same or different and independently represent hydrogen, substituted or unsubstituted groups selected from linear or branched (C1-C8)alkyl, (C3-C7)cycloalkyl, acyl, aryl, heteroaryl, heterocyclyl, aminocarbonyl, aralkyl, alkylaminocarbonyl, arylaminocarbonyl, aralkylaminocarbonyl, heteroarylaminocarbonyl, heteroaralkylaminocarbonyl, heterocyclylaminocarbonyl, alkoxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl, heteroaryloxycarbonyl, heteroaraloxycarbonyl, heterocycloxycarbonyl groups or SO2R3 wherein R3 represents substituted or unsubstituted groups selected from alkyl, aryl, polyhaloalkyl, heterocyclyl, heteroaryl groups;
- ‘n’ is an integer from 1-3;
- X represents O or S,
Dependencies are inferred from the claim text.