2024年3月21日发(作者：云嘉木)
专利内容由知识产权出版社提供
专利名称：QUINOLINE-4-CARBOXAMIDE DERIVATIVES
AS NK-3 AND NK-2 RECEPTOR
ANTAGONISTS
发明人：FARINA, Carlo,Nikem Research
S.r.l.,GIARDINA, Giuseppe,Nikem Research
S.r.l.,GRUGNI, Mario,Nikem Research
S.r.l.,NADLER, Guy Margue. Marie
Gerard,Glaxosmithkline
申请号：EP01983584.2
申请日：20011112
公开号：EP1334088A1
公开日：20030813
摘要：Certain compounds of formula (I) below or a pharmaceutically acceptable salt
or hydrate thereof: (I) 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 N R11R12; 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: C¿1-6? 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.
申请人：GlaxoSmithKline S.p.A.,Laboratoire Glaxosmithkline S.A.S.
地址：Via Alessandro Fleming, 2 37135 Verona IT,100, route de Versailles 78163 Marly-
le-Roi Cedex FR
国籍：IT,FR
代理机构：Rutter, Keith
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2024年3月21日发(作者：云嘉木)
专利内容由知识产权出版社提供
专利名称：QUINOLINE-4-CARBOXAMIDE DERIVATIVES
AS NK-3 AND NK-2 RECEPTOR
ANTAGONISTS
发明人：FARINA, Carlo,Nikem Research
S.r.l.,GIARDINA, Giuseppe,Nikem Research
S.r.l.,GRUGNI, Mario,Nikem Research
S.r.l.,NADLER, Guy Margue. Marie
Gerard,Glaxosmithkline
申请号：EP01983584.2
申请日：20011112
公开号：EP1334088A1
公开日：20030813
摘要：Certain compounds of formula (I) below or a pharmaceutically acceptable salt
or hydrate thereof: (I) 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 N R11R12; 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: C¿1-6? 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.
申请人：GlaxoSmithKline S.p.A.,Laboratoire Glaxosmithkline S.A.S.
地址：Via Alessandro Fleming, 2 37135 Verona IT,100, route de Versailles 78163 Marly-
le-Roi Cedex FR
国籍：IT,FR
代理机构：Rutter, Keith
更多信息请下载全文后查看