Patent ID: 6342502
Filing Date: 2002-01-29
Classification: A61P,C07D

Abstract:
A method of treating, or reducing the risk of, asthma in a patient suffering from, or at risk of, said disease, which comprises administering to the patient a therapeutically effective amount of a compound of formula (I): wherein:R is â€”C(O)Ar1, â€”C(R4)(R5)Ar1, or Ar2; Ar1 is naphthyl, quinolyl, isoquinolyl, indolyl, benzofuranyl or benzothienyl, each of which can be optionally substituted by one or more substituents selected from C1-4 alkyl, C1-4 alkoxy, halogen or trifluoromethyl, or Ar1 is phenyl optionally substituted by one or more substituents selected from C1-4 alkyl, C1-4 alkoxy, halogen, trifluoromethyl, amino, nitro, cyano, trifluoromethoxy, phenoxy, â€”CH2N(R6)2, â€”NHSO2CF3, C1-4 alkylsulphonylamino, â€”NHC(O)R6a, CO2R7 or â€”C(O)NR8R8a; R4 represents H or C1-4 alkyl; R5 represents H or OH; each R6 independently represents H or C1-4 alkyl; R6a represents H, C1-6 alkyl, aryl or arC1-4 alkyl, wherein the aryl group or aryl moiety in the aralkyl group is phenyl or pyridyl, each of which may be optionally substituted by one or more substituents selected from C1-4 alkyl, C1-4 alkoxy, C1-4 alkylcarbonylamino, halogen or trifluoromethyl; R7 represents H or C1-4 alkyl; R8 and R8a each independently represent H, C1-4 alkyl, phenyl or pyridyl; Ar2 is acenaphthenyl, indanyl, iminodihydrobenzofuranyl or fluorenyl, each of which can be optionally substituted by one or more substituents selected from OH, C1-4 alkyl, C1-4 alkoxy, halogen, or trifluoromethyl; R1 and R2 are independently H, C1-6 alkyl, C3-6 alkenyl, CH2CH3-5 cycloalkyl or C3-6 cycloalkyl; R3 represents H, Xâ€”R9 or Xâ€”Ar3; X represents S(O)n, C(O)NR10, C(O)O, NH(CO)NR10, NH(CO)O or SO2NR10; n is 0, 1 or 2; R9 represents a methyl group optionally substituted by one or more substituents selected from CN, CO2H, C1-5 alkoxycarbonyl, 5-tetrazolyl, SO2NH2 or C(O)NR11R12, or represents C2-6 alkyl or C3-6 alkenyl, each of which may be optionally substituted by one or more substituents selected from OH, CN, CO2H, C1-5 alkoxy, C1-5 alkoxycarbonyl, 5-tetrazolyl, azide, phthalimido, SO2NH2, C(O)NR11R12, NR13R14, NHC(O)R15 or NHSO2R16 where R11, R12, R13 and R14 each independently represent H or C1-4 alkyl, R15 represents C1-4 alkyl, C1-4 alkoxy, di(C1-4alkyl)amino, or alkoxyalkylene containing up to 6 carbon atoms, and R16 represents C1-4 alkyl or trifluoromethyl; or, additionally, in the case where X represents C(O)NR10, NH(CO)NR10 or SO2NR10, R9 and R10 together with the nitrogen atom to which they are attached may form a 4- to 7-membered heterocyclic ring which may be optionally substituted by one or more OH groups; R10 represents H, C1-6 alkyl or is linked to as defined above; and Ar3 is phenyl, pyridyl or pyridine N-oxide, each of which may be optionally substituted by one or more substituents selected from OH, NO2, NH2, NHSO2CF3, C1-4 alkoxy, bis C1-4 alkanesulphonylamino, C1-4 alkylcarbonylamino or alkoxycarbonylamino; or a pharmaceutically-acceptable salt or solvate thereof.