Patent ID: 6498190
Filing Date: 2002-12-24
Classification: A61K,A61P,C07C,C07D,C07F

Abstract:
A compound of the formula (Ia): whereinA is alkylene which optionally is intercalated by a hetero atom or phenylene, contains an oxo group, and/or has an unsaturated bond; B is hydrogen, alkyl, aralkyl or acyl; R is COOR1, CH2OR2 or CON(R3)R4; R1 is hydrogen or alkyl; R2 is hydrogen or alkyl; R3 and R4 are independently hydrogen, alkyl, hydroxy or alkylsulfonyl; X1 is a single bond, phenylene, naphthylene, thiophenediyl, indolediyl, or oxazolediyl; X2 is a single bond, â€”N&boxH;Nâ€”, â€”N&boxH;CHâ€”, â€”CH&boxH;Nâ€”, â€”CH&boxH;Nâ€”Nâ€”, â€”CH&boxH;Nâ€”Oâ€”, â€”C&boxH;NNHCSNHâ€”, â€”C&boxH;NNHCONHâ€”, â€”CH&boxH;CHâ€”, â€”CH(OH)â€”, â€”C(Cl)&boxH;C(Cl)â€”, â€”(CH2)nâ€”, ethynylene, â€”N(R5)â€”, â€”N(R51)COâ€”, â€”N(R52)SO2â€”, â€”N(R53)CON(R54)â€”, â€”CON(R55)â€”, â€”SO2N(R56)â€”, â€”Oâ€”, â€”Sâ€”, â€”SOâ€”, â€”SO2â€”, â€”COâ€”, oxadiazolediyl, thiadiazolediyl or tetrazolediyl; X3 is alkyl, alkenyl, alkynyl, aryl, aralkyl, heterocyclic group, cycloalkyl, cycloalkenyl, thiazolinylidenemethyl, thiazolidinylidenemethyl, â€”CH&boxH;NR6 or â€”N&boxH;C(R7)R8; R5, R51, R52, R53, R54, R55 and R56 each are hydrogen or alkyl; R6 is hydrogen, alkyl, hydroxy, alkoxy, carbamoyloxy, thiocarbamoyloxy, ureido or thioureido; R7 and R8 each are independently alkyl, alkyoxy or aryl; and n is 1 or 2; wherein a cyclic substituent may have one to three substituents selected from the group consisting of nitro, alkoxy, sulfamoyl, substituted- or unsubstituted-amino, acyl, acyloxy, hydroxy, halogen, alkyl, alkynyl, carboxy, alkoxycarbonyl, aralkoxycarbonyl, aryloxycarbonyl, mesyloxy, cyano, alkenyloxy, hydroxyalkyl, trifluoromethyl, alkylthio, â€”N&boxH;PPh3, oxo, thioxo, hydroxyimino, alkoxyimino, phenyl and alkylenedioxy or its salt or hydrate thereof, provided that compounds wherein (1) X1 and X2 are a single bond, and X3 is substituted- or unsubstituted-phenyl, or naphthyl; and (2) A is 5-heptenylene, R is COOR1 (R1 is hydrogen or methyl), X1 is 1,4-phenylene, X2 is a single bond, and X3 is unsubstituted phenyl; (3) X1 and X2 are a single bond, X3 is methyl, n-hexyl, 2-cyclohexylethyl, benzyl, phenethyl, or substituted- or unsubstituted-alkenyl; (4) X1 and X2 are a single bond, and X3 is pyridyl; and (5) X1 is a single bond, X2 is â€”CH&boxH;CHâ€”, and X3 is phenyl are excluded.