Patent ID: 6342601
Filing Date: 2002-01-29
Classification: A61P,C07D

Abstract:
A compound of formula whereinB represents a sulfur (S) or oxygen (O) atom; D represents a carbon (C) atom; E represents a group CR3; R1 represents a group NRâ€²Râ€³ where Râ€² represent a hydrogen atom or a C1-C6 alkyl group, Râ€³ represents a C1-C6 alkyl group, or Râ€² and Râ€³ together with the nitrogen atom to which they are attached form a 3- to 7-membered saturated heterocyclic ring, or R1 represents a C1-C6 alkyl, C1-C6 alkoxy, C1-C3-alkyloxyC1-C3 alkyl, C3-C6-cycloalkyloxyC1-C3-alkyl, C3-C6 alkenyl, phenyl, C3-C7 cycloalkyl, C3-C5 cycloalkylmethyl or C3-C7 cycloalkenyl group, each of which may be unsubstituted or substituted by one or more halogen atoms; R2 represents a methyl group, or a C2-C6 alkyl group which may be unsubstituted or substituted by a C1-C6 alkoxy group other than in the 1-position; R3 represents a hydrogen atom or a group Xâ€”R5 or Xâ€”Ar1; X represents a group â€”Oâ€”, S(O)n, SO2N(R6) or C(O)N(R6); n is 0, 1 or 2; R5 represents an alkyl or alkenyl group which may be unsubstituted or substituted by amido, amino, carboxyl, cyano, hydroxyl, C1-C6 alkoxy, C1-C6 alkylthio, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, C3C7 cycloalkyl, (di) C1-C6 alkylamino, C2-C6 acylamino, C1-C6 alkylsulfonamido, tetrahydrofuranyl, dioxolanyl, imidazolyl, haloC1-C6alkylsulfonamido or tetrazolyl, or, additionally, in the case where X represents SO2N(R6) or C(&boxH;O)N(R6), R5 and R6 together with the nitrogen atom to which they are attached may form a 3- to 7-membered heterocyclic ring which may be unsubstituted or substituted by amido, amino, carboxyl, cyano, hydroxyl, C1-C6 alkoxy, C1-C6 alkylthio, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, C3-C7 cycloalkyl, (di) C1-C6 alkylamino, C2-C6 acylamino, C1-C6 alkylsulfonamido, tetrahydrofuranyl, dioxolanyl, imidazolyl, haloC1-C6alkylsulfonamido or tetrazolyl; Ar1 represents a phenyl or pyridyl group each of which may be unsubstituted or substituted by one or more substituents independently selected from carboxyl, hydroxyl, C2-C6 acylamino, C1-C6 alkylamido, C1-C6 alkylsulfonamido and (di) C1-C6, alkylsulfamoyl; R6 represents a hydrogen atom, C1-C6 alkyl or is linked to R5 as defined above; R4 represents a group CHR7Ar2, Ar3, C(O)Ar1 or CR7(OH)Ar2; Ar2 represents an aryl or heteroaryl group which may be unsubstituted or substituted by one or more substituent groups independently selected from halogen, trifluoromethyl, trifluoromethoxy, amino, cyano, carboxyl, nitro, C1-C6 alkyl, C1-C6 alkoxy, (di)C1-C6 alkylamino, C2-C6 acylamino, C1-C6 alkylsulfonamido, CONHâ€”(C1-C6 alkyl) and C1-C6 alkoxycarbonyl; Ar3 represents an acenaphthenyl, indanyl or fluorenyl group, each of which may be unsubstituted or substituted by one or more substituent groups independently selected from halogen, trifluoromethyl, trifluoromethoxy, amino, cyano, carboxyl, nitro, C1-C6 alkyl, C1-C6 alkoxy, (di)C1-C6 alkylamino, C2-C6 acylamino, C1-C6 alkylsulfonamido, CONHâ€”(C1-C6 alkyl) and C1-C6 alkoxycarbonyl; and R7 represents a hydrogen atom or a C1-C4 alkyl group; or a pharmaceutically-acceptable salt or solvate thereof.