Patent ID: 6608083
Filing Date: 2003-08-19
Classification: A61K,A61P,C04B,C07D

Abstract:
A compound, or solvate or salt thereof, of formula (I): in which: Ar is an optionally substituted phenyl group, or a naphthyl or C5-7 cycloalkdienyl group, or an optionally substituted single or fused ring heterocyclic group, having aromatic character, containing from 5 to 12 ring atoms and comprising up to four hetero-atoms in the or each ring selected from S, O, N; R is linear or branched C1-8 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, an optionally substituted phenyl group or a phenyl C1-6 alkyl group, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C1-6 alkyl, amino C1-6 alkyl, C1-6 alkylaminoalkyl, di C1-6 alkylaminoalkyl, C1-6 acylaminoalkyl, C1-6 alkoxyalkyl, C1-6 alkylcarbonyl, carboxy, C1-6 alkoxyxcarbonyl, C1-6 alkoxycarbonyl C1-6 alkyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di C1-6 alkylaminocarbonyl, halogeno C1-6 alkyl; or is a group â€”(CH2)pâ€” when cyclized onto Ar, where p is 2 or 3; R1 is hydrogen or C1-6 linear or branched alkyl, or together with R2 form a â€”(CH2)nâ€” group in which n represents 3, 4, or 5; R1 together with R forms a group â€”(CH2)qâ€”, in which q is 2, 3, 4 or 5; R2 is hydrogen; R3 is hydrogen, C1-6 linear or branched alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino, mono- and di-C1-6 alkylamino, â€”O(CH2)râ€”NT2, in which r is 2, 3, or 4 and T is hydrogen or C1-6 alkyl or it forms with the adjacent nitrogen a group â€ƒin which V and V1 are independently hydrogen or oxygen and u is 0,1 or 2; â€”O(CH2)sâ€”OW2 in which s is 2, 3, or 4 and W is hydrogen or C1-6 alkyl; hydroxyalkyl, aminoalkyl, mono-or di-alkylaminoalkyl, acylamino, alkylsulphonylamino, aminoacylamino, mono- or di-alkylaminoacylamino; with up to four R3 substituents being present in the quinoline nucleus; R4 is C1-6 linear or branched alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino, mono- and di-C1-6 alkylamino, â€”O(CH2)râ€”NT2, in which r is 2, 3, or 4 and T is hydrogen or C1-6 alkyl or it forms with the adjacent nitrogen a group â€ƒin which V and V1 are independently hydrogen or oxygen and u is 0,1 or 2; â€”O(CH2)sâ€”OW2 in which s is 2, 3, or 4 and W is hydrogen or C1-6 alkyl; hydroxyalkyl, aminoalkyl, mono-or di-alkylaminoalkyl, acylamino, alkylsulphonylamino, aminoacylamino, mono- or di-alkylaminoacylamino; with up to four R3 substituents being present in the quinoline nucleus; or R4 is a group â€”(CH2)tâ€” when cyclized onto R5 as aryl, in which t is 1, 2, or 3; R5 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, wherein an optional substituent is hydroxy, halogen, C1-6 alkoxy or C1-6 alkyl, or an optionally substituted single or fused ring heterocyclic group, having aromatic character, containing from 5 to 12 ring atoms and comprising up to four hetero-atoms in the or each ring selected from S, O, N; X is O, S, or Nâ€”Câ‰¡N.