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    • 3. 发明专利
    • DERIVATIVES OF QUINOLINE-4-CARBOXAMIDES, METHOD FOR THEIR PREPARATION AND APPLICATION AS NEUROKININ 3(NK-3) AND NEUROKININ 2(NK-2) RECEPTOR ANTAGONISTS
    • BG102557A
    • 1999-03-31
    • BG10255798
    • 1998-06-18
    • GIARDINA GIUSEPPE AGRUGNI MARIORAVEGLIA LUCA FFARINA CARLO
    • GIARDINA GIUSEPPE AGRUGNI MARIORAVEGLIA LUCA FFARINA CARLO
    • A61K31/47C07D215/52C07D401/06C07D401/12C07D487/04C07D521/00
    • The invention relates to compounds with the formulawhere Ar means optionally a substituted aryl or C5-7cycloalkyldienyl group, or optionally substituted aromaticheterocyclic group containing one ring or condensed rings; R meansC1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, optionallysubstituted phenyl or phenyl C1-6 alkyl, optionally substituted5-atom heteroaromatic ring containing up to 4 heteroatoms selectedfrom 0 and N, hydroxy C1-6 alkyl, amino C1-6 alkyl, C1-6alkylaminoalkyl, di C1-6 alkylaminoalkyl, C1-6 acylaminoalkyl,C1-6 alkoxyalkyl, C1-6 alkylcarbonyl, carboxy, C1-6alkoxacyrbonyl, C1-6 alkoxycarbonyl-C1-6 alkyl, aminocarbonyl,C1-6 alkylaminocarbonyl, di C1-6 alkylaminocarbonyl, halogeno C1-6alkyl or R is a group - (CH2)p where p has the value of 2 or 3 andwhich forms a ring with a carbon atom from Ar; R1 is hydrogen oroptionally up to four subsituents selected from C1-6 alkyl, C1-6alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano,carboxy, carboxyanido, sulphonamido, C1-6 alkoxycarbonyl,trifluoromethyl, acyloxy, phthalimido, amino or mono- and di C1-6alkylamino; R2 means hydrogen, C1-6 alkyl, hydroxy, halogen,cyano, amino, mono- or di C1-6 alkylamino, alkylsulphonylamino,mono- or di C1-6 alkanoylamino where each alkyl group isoptionally substituted by an aminogroup or by mono- ordialkylaminogroup, or R2 is a residue - X-(CH2)n-Y, where X is abond or -O- and n has the value of 1 to 5, provided that when X is-O-, n has the value of only 2 to 5, and Y means a NY1Y2 groupwhere Y1 and Y2 are separately selected from hydrogen, C1-6 alkyl,C1-6 alkenyl, aryl or aryl C1-6 alkyl or Y is hydroxy, halogen oroptionally substituted N-bound single or condensed ringheterocyclic group; R3 means a straight or branching chain C1-6alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionallysubstituted aryl or substituted single or condensed aromaticheterocyclic group, and R4 means hydrogen or C1-6 alkyl. Theinvention also relates to solvates or salts of the compound withformula I.20 claims