Patent ID: 7091227
Filing Date: 2006-08-15
Classification: A61P,C07D

Abstract:
1. A compound of formula (I), racemic-diastereomeric mixtures thereof, optical isomers thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, and isotopes, wherein, Q is H Y is O or S; W is H, Cl, Br, I, NO 2 , CN, SCN, OCF 3 , —X q —(C(R 10 ) 2 ) a —Y 1 q —(C(R 10 ) 2 ) a —Z 1 q , or an optionally substituted group selected from the group consisting of alkyl, alkenyl and alkynyl; Y NR q for each occurrence is independently 0 or 1; a for each occurrence is independently 0 or an integer from 1 to 5; R Z X 1 is hydrogen, alkyl or hydroxyalkyl; R 1 and R 2 are each independently hydrogen, halogen, hydroxy, nitro, cyano, COOH, COOX 3 , SX 3 , SO 2 X 3 , SOX 3 , C(O)X 3 , NHC(O)X 3 , C(O)NHX 3 , NHSO 2 X 3 or selected from an optionally substituted group consisting of alkyl, alkenyl, alkynyl, alkoxy, amino, —NHX 3 , —NX 3 X 3 , alkylamino, arylamino, alkylthio, alkylsulfonato, aryl, aryloxy, arylalkyl, arylalkenyl, arylalkynyl, arylalkyloxy, cycloalkyl, —(CH 2 ) m —(CHX 2 )CN, —(CH 2 ) m —(CHX 2 )COOH, —(CH 2 ) m —(CHX 2 )COOX 3 , —(CH 2 ) m —(CHX 2 )SO 2 X 3 , —(CH 2 ) m —(CHX 2 )C(O)X 3 , —(CH 2 ) m —(CHX 2 )C(O)NHX 3 and —(CH 2 ) m —(CHX 2 )NHSO 2 X 3 provided that the alkylamino and arylamino are attached to the phenyl ring via the nitrogen of the amino group; where m is 0 to 4; X for each occurrence is independently H or an optionally substituted moiety selected from the group consisting of alkyl, alkenyl, alkynyl, carbonyl, S(O) X R 3 is hydrogen, or an optionally substituted moiety selected from the group consisting of carbonyl, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, amino, alkylamino, arylamino, alkoxy; and acyl; where each of the optionally substituted moieties described hereinabove is optionally substituted by one or more substituents each independently selected from the group consisting of oxo, amino, nitro, mono- or bi-(C 1 –C 6 )alkylamino, hydroxy, nitrile, chloro, fluoro, bromo, iodo, CF 3 , (C 1 –C 6 )alkyl, —C(O)(C 1 –C 6 )alkyl, —COOH, —COO(C 1 –C 6 )alkyl, —S—(C 1 –C 6 )alkyl, —S-aryl, (C 1 –C 6 )alkoxy, —SO 2 NH 2 , phenyl, phenyl(C 1 –C 6 )alkyl, —O—(C 1 –C 6 )alkyl-OH, —O—(C 1 –C 6 )alkyl-O—(C 1 —C 6 )alkyl, —O—(C 2 –C 6 )alkyl-N—((C 1 –C 6 )alkyl) n , —N—(C 1 –C 6 )alkyl-OH, —N—(C 1 –C 6 )alkyl-O—(C 1 –C 6 )alkyl, —C(O)NH 2 , —C(O)N((C 1 –C 6 )alkyl) n , , —S(O) n (C 1 –C 6 )alkyl; and —S(O) n aryl—where the alkyl groups mentioned herein optionally have one or more unsaturated bonds in the alkyl portion; n is 0, 1 or 2; provided that 1) when Q is H; Y is O; R 1 and R 2 are each hydrogen, halogen, alkyl, alkoxy, alkylthio, carboxyalkyl or optionally substituted phenyl; and X 1 is hydrogen or alkyl; then R 3 is not alkyl, alkenyl, alkoxy, cycloalkyl or optionally substituted phenyl; 2) when Q is H; Y is O; R 1 and R 2 are each hydrogen, halogen, alkyl, alkoxy, alkylthio, carboxyalkyl or optionally substituted phenyl; then X 1 and R 3 are not taken together to form 3) when W is Cl, Br or I; Q is hydrogen; Y is O; X 1 is H; then R 3 is not or phenyl optionally substituted by 1 to 3 substituents independently selected from the group consisting of amino, mono- or bi-(C 1 –C 6 )alkylamino, hydroxy, chloro, fluoro, bromo, iodo, (C 1 –C 6 )alkyl, (C 1 –C 6 )alkoxy and —SO 2 NH 2 ; 4) when W is Cl, Br or I; Q is H; R 1 is 7-Cl; R 2 is H; and X 1 is alkyl; then R 3 is not alkyl, alkoxy or cycloalkyl; 5) when W is Cl, Br or I; Q is H; R 1 is 7-Cl; R 2 is H; and X 1 is H; then R 3 is not alkyl or cycloalkylamino; 6) when W is Cl, Br, I or NO 2 ; Q is H; Y is O; X 1 is H; R 1 is OH; R 2 is NO 2 , amino, alkyl, alkoxy, hydroxy lower alkyl or dialkylamino; then R 3 is not H or alkyl; 7) when W is Cl, Br or I; Q is H; Y is O; R 1 is CF 3 , CH 2 F, NO 2 , alkyl or alkoxy; R 2 is H; X 1 is H; then R 3 is not naphthyl or phenyl optionally substituted with halo, CF 3 , alkyl or alkoxy; 8) when W is Cl, Br or I; Q is H; R 1 is alkyl; R 2 is H; X 1 is H or alkyl; then R 3 is not alkyl or alkoxy; 9) when W is Cl; Q is H; Y is S; R 1 and R 2 are each H; X 1 is H; then R 3 is not ethyl; 10) when W is Cl; Q is H; Y is O; R 1 and R 2 are each H; X 1 is H; then R 3 is not n-butyl; 11) when W is H, then R 1 and R 2 are not H at the same time. 12) the compound is not