利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

32 条记录 (耗时 0.04 秒)

    Quinoline-4-Carboxamide Derivatives as NK-3 and NK-2 Receptor Antagonists
    13.
    发明申请
    Quinoline-4-Carboxamide Derivatives as NK-3 and NK-2 Receptor Antagonists 审中-公开

    公开(公告)号：US20060235026A1

    公开(公告)日：2006-10-19

    申请号：US11425434

    申请日：2006-06-21

    申请人： Carlo Farina ,  Giuseppe Giardina ,  Mario Grugni ,  Guy Gerard Nadler

    发明人： Carlo Farina ,  Giuseppe Giardina ,  Mario Grugni ,  Guy Gerard Nadler

    IPC分类号： A61K31/496 ,  C07D403/02

    CPC分类号： C07D215/52

    摘要： Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: wherein: R1 is H or C1-6 alkyl; R2 is aryl or C3-7 cycloalkyl or heteroaryl; R3 is H or C1-3 alkyl, optionally substituted by one or more fluorines; R4 is R8R9; R8 is a single bond, C1-6 alkyl, or aryl; R9 is H, COO R10, or NR11R12; R10 is H or C1-6 alkyl; R11 and R12 are independently selected from H and C1-6 alkyl; R5 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, aryl, or a single or fused ring aromatic heterocyclic group; R6 represents H or up to three substituents independently selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, amino or mono- or di-C1-6 alkylamino; R7 is H or halo; a is 1-6; and any of R2, R5, R8, R10, R11 and R12 may optionally be substituted one or more times by halo, hydroxy, amino, cyano, nitro, carboxy or oxo; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.

    Benzosuberonylpiperdine compounds as analgesics
    17.
    发明授权
    Benzosuberonylpiperdine compounds as analgesics 失效

    公开(公告)号：US07115633B2

    公开(公告)日：2006-10-03

    申请号：US10275242

    申请日：2001-05-01

    申请人： Daniela Barlocco ,  Giorgio Cignarella ,  Giuseppe Giardina ,  Mario Grugni ,  Silvano Ronzoni

    发明人： Daniela Barlocco ,  Giorgio Cignarella ,  Giuseppe Giardina ,  Mario Grugni ,  Silvano Ronzoni

    IPC分类号： A61K31/445 ,  C07D211/14

    CPC分类号： C07D211/14 ,  C07D211/18 ,  C07D211/22

    摘要： Compounds of formula (I) or a derivative thereof, wherein; R is C1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, hydroxy, halo, C1-6alkenyl, C1-6alkynyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl; R1 is hydrogen or R; R2 is hydroxy, C1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino; R3 is hydrogen or C1-6alkyl; R4 and R5 are each independently selected from the list consisting of perhaloC1-6alkyl, hydrogen, halo, C1-6alkyl, C1-6alkoxy, hydroxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl, and COX wherein X may be hydroxy, C1-6alkoxy, C1-6alkyl, amino, C1-6alkylamino, or di(C1-6alkyl)amino; with the proviso that, when R3 is hydrogen, then R4 and R5 are not both hydrogen; and wherein any alkyl group or the alkyl moiety of any group containing such a moiety may be substituted one or more times by halo; are ligands of the ORL-1 receptor and are useful in therapy.

    QUINOLINE-4-CARBOXAMIDE AS NK-2 AND NK-3 RECEPTOR ANTAGONISTS
    18.
    发明申请
    QUINOLINE-4-CARBOXAMIDE AS NK-2 AND NK-3 RECEPTOR ANTAGONISTS 审中-公开

    公开(公告)号：US20070197546A1

    公开(公告)日：2007-08-23

    申请号：US11691899

    申请日：2007-03-27

    申请人： Giuseppe Giardina ,  Mario Grugni ,  Davide Graziani ,  Luca Raveglia

    发明人： Giuseppe Giardina ,  Mario Grugni ,  Davide Graziani ,  Luca Raveglia

    IPC分类号： A61K31/4709 ,  A61K31/496 ,  C07D401/02

    CPC分类号： C07D401/06 ,  C07D215/50 ,  C07D215/52 ,  C07D251/52 ,  C07D491/10 ,  C07D491/113

    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 a C5-7 cycloalkyl group or an optionally substituted single or fused ring aromatic heterocyclic group,; R is C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, optionally substituted phenyl or phenyl C1-6 alkyl, 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 alkoxycarbonyl, C1-6 alkoxycarbonyl C1-6 alkyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di C1-6 alkylaminocarbonyl, halogeno C1-6 alkyl; or R is a group —(CH2)p— wherein p is 2 or 3 which group forms a ring with a carbon atom of Ar; R1 represents hydrogen or up to four optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino or mono- and di-C1-6 alkylamino; R2 represents a moiety —(CH2)n—NY1Y2 wherein n is an integer in the range of from 1 to 9, Y1 and Y2 are independently selected from hydrogen; C1-6-alkyl; C1-6 alkyl substituted with hydroxy, C1-6 alkylamino or bis (C1-6 alkyl) amino; C1-6-alkenyl; aryl or aryl-C1-6-alkyl or Y1 and Y2 together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group; R3 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R4 represents hydrogen or C1-6 alkyl; a pharmaceutical composition comprising such a compound, process for preparing such a compound and the use of such a compound in medicine.