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    Quinoline derivatives(2)
    2.
    发明授权
    Quinoline derivatives(2) 失效

    公开(公告)号：US06608083B1

    公开(公告)日：2003-08-19

    申请号：US08450437

    申请日：1995-05-25

    申请人： Carlo Farina ,  Giuseppe Arnaldo Maria Giardina ,  Mario Grugni ,  Luca Francesco Raveglia

    发明人： Carlo Farina ,  Giuseppe Arnaldo Maria Giardina ,  Mario Grugni ,  Luca Francesco Raveglia

    IPC分类号： C07D21500

    CPC分类号： C04B35/632 ,  A61K31/00 ,  A61K31/4709 ,  C07D215/52 ,  C07D221/18 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04

    摘要： NK3 receptor antagonists 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 —(CH2)p— when cyclized onto Ar, where p is 2 or 3; R1 and R2, which may be the same or different, are independently hydrogen or C1-6 linear or branched alkyl, or together form a —(CH2)n— group in which n represents 3, 4, or 5; or R1 together with R forms a group —(CH2)q—, in which q is 2, 3, 4 or 5; R3 and R4, which may be the same or different are independently 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, —O(CH2)r—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  in which V and V1 are independently hydrogen or oxygen and u is 0,1 or 2; —O(CH2)s—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 —(CH2)t— 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; in which inter alia, Ar is phenyl, optionally substituted by C1-6 alkyl or halogen; thienyl or a C5-7 cycloalkdienyl group; R is C1-6 alkyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyl or hydroxy C1-6 alkyl; R1 and R2 are each hydrogen or C1-6 alkyl; R3 is hydrogen, hydroxy, halogen, C1-6 alkoxy or C1-6 alkyl; R4 is hydrogen, C1-6 alkyl, C1-6 alkoxy, hydroxy, anino, halogen, aminoalkoxy, mono- or di-alkylaminoalkoxy, mono- or di-alkylaminoalkyl, phthaloylalkoxy, mono- or di-alkylaminoacylarnino or acylamino; R5 is phenyl, thienyl, furyl, pyrryl or thiazolyl, and X is oxygen. X is O, S, or N—C≡N.

    Quinoline derivatives
    3.
    发明授权
    Quinoline derivatives 失效
    喹啉衍生物

    公开(公告)号：US06277862B1

    公开(公告)日：2001-08-21

    申请号：US09077151

    申请日：1998-05-22

    申请人： Giuseppe Arnaldo Maria Giardina ,  Mario Grugni ,  Luca Francesco Raveglia ,  Carlo Farina

    发明人： Giuseppe Arnaldo Maria Giardina ,  Mario Grugni ,  Luca Francesco Raveglia ,  Carlo Farina

    IPC分类号： A61K3147

    CPC分类号： C07D215/52

    摘要： A compound, or a solvate or a salt thereof, of formula (I), wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or an optionally substituted single or fused ring aromatic heterocyclic group; R, R1, R2 and R3 are as defined in the description; a process for the preparation of such a compound, a pharmaceutical composition containing such a compound or composition in medicine.

    摘要翻译： 式（I）的化合物或其溶剂合物或其盐，其中Ar为任选取代的芳基或C 5-7环二烯基，或任选取代的单环或稠环芳族杂环基; R，R1，R2和R3如说明书中所定义; 制备这种化合物的方法，在药物中含有这种化合物或组合物的药物组合物。