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1. 发明授权

EP1385839B1 3-SUBSTITUTED QUINOLINE-4-CARBOXAMIDE DERIVATIVES AS NK-3 AND NK-2 RECEPTOR ANTAGONISTS 有权
标题翻译： 3-取代的喹啉-4-甲酰胺衍生物作为NK-3和NK-2受体拮抗剂
公开(公告)号：EP1385839B1
公开(公告)日：2006-02-22
申请号：EP02761911.3
申请日：2002-04-11
申请人： GlaxoSmithKline S.p.A.
发明人： FARINA, Carlo , GAGLIARDI, Stefania , GIARDINA, Giuseppe, Arnaldo, Maria , MARTINELLI, Marisa
IPC分类号： C07D401/06 , C07D409/14 , C07D215/16 , C07D215/52 , A61K31/47 , A61K31/4709 , A61P11/00 , A61P25/00 , C07D241/00 , C07D215/00 , C07D333/00
CPC分类号： C07D215/50 , C07D215/16 , C07D215/52 , C07D401/04 , C07D401/06 , C07D401/14 , C07D409/04 , C07D409/14 , C07D417/06 , C07D487/04
摘要： A compound forula (I) below or a pharmaceuticaly acceptable salt or solvate thereof: wherein R1 is H or alkyl; R2 is aryl or cycloalkyl or heteroaryl; R3 is H or alkyl, wherein the alkyl group may be optionally substituted by one or more fluorine atoms; R4 is H, hydroxyalkyl, dihydroxyalkyl or hydroxyalkoxyalkyl; R5 is branched or linear alkyl, cycloalkyl, 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: alkyl, alkenyl, aryl, alkoxy, hydroxy, halo, nitro, cyano, carboxy, carboxamido, sulphonamido, trifluoromethyl, or amino or mono- or di-alkylamino; R7 is H or halo; R¿8= is H or =O; and any of R¿2? and R5 may optionally be substituted one or more times by halo, hydroxy, amino, cyano, nitro, carboxy, oxo, alkyl, alkenyl, aryl, alkoxy, carboxamido, sulphonamido, trifluoromethyl, or mono- or di- alkylamino; with the proviso that said compound of formula (I) is not a compound selected from the list according to claim 1.

2. 发明授权

EP0876348B1 SALTS OF QUINOLINE DERIVATIVES AS NK3 ANTAGONISTS 失效
标题翻译：喹啉作为NK3拮抗剂的盐类
公开(公告)号：EP0876348B1
公开(公告)日：2003-02-26
申请号：EP96941026.5
申请日：1996-11-22
申请人： GlaxoSmithKline S.p.A.
发明人： GIARDINA, Giuseppe, Arnaldo, Maria , FARINA, Carlo , GRUGNI, Mario , RAVEGLIA, Luca, Francesco
IPC分类号： C07D215/52 , A61K31/47
CPC分类号： C07D215/52 , C07D215/50
摘要： A compound of formula (I) or a solvate thereof, characterised in that salt comprises a compound of formula (I) in anionic form and a salting cation; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound in medicine.

3. 发明公开

EP1385839A1 3-SUBSTITUTED QUINOLINE-4-CARBOXAMIDE DERIVATIVES AS NK-3 AND NK-2 RECEPTOR ANTAGONISTS 有权
标题翻译： 3-取代的喹啉-4-甲酰胺衍生物作为NK-3和NK-2受体拮抗剂
公开(公告)号：EP1385839A1
公开(公告)日：2004-02-04
申请号：EP02761911.3
申请日：2002-04-11
申请人： GlaxoSmithKline S.p.A.
发明人： FARINA, Carlo , GAGLIARDI, Stefania , GIARDINA, Giuseppe, Arnaldo, Maria , MARTINELLI, Marisa
IPC分类号： C07D401/06 , C07D409/14 , C07D215/16 , C07D215/52 , A61K31/47 , A61K31/4709 , A61P11/00 , A61P25/00
CPC分类号： C07D215/50 , C07D215/16 , C07D215/52 , C07D401/04 , C07D401/06 , C07D401/14 , C07D409/04 , C07D409/14 , C07D417/06 , C07D487/04
摘要： A compound forula (I) below or a pharmaceuticaly acceptable salt or solvate thereof: wherein R1 is H or alkyl; R2 is aryl or cycloalkyl or heteroaryl; R3 is H or alkyl, wherein the alkyl group may be optionally substituted by one or more fluorine atoms; R4 is H, hydroxyalkyl, dihydroxyalkyl or hydroxyalkoxyalkyl; R5 is branched or linear alkyl, cycloalkyl, 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: alkyl, alkenyl, aryl, alkoxy, hydroxy, halo, nitro, cyano, carboxy, carboxamido, sulphonamido, trifluoromethyl, or amino or mono- or di-alkylamino; R7 is H or halo; R¿8= is H or =O; and any of R¿2? and R5 may optionally be substituted one or more times by halo, hydroxy, amino, cyano, nitro, carboxy, oxo, alkyl, alkenyl, aryl, alkoxy, carboxamido, sulphonamido, trifluoromethyl, or mono- or di- alkylamino; with the proviso that said compound of formula (I) is not a compound selected from the list according to claim 1.

4. 发明公开

EP1337253A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：EP1337253A1
公开(公告)日：2003-08-27
申请号：EP01998350.1
申请日：2001-11-27
申请人： GlaxoSmithKline S.p.A. , Laboratoire Glaxosmithkline S.A.S.
发明人： FARINA, Carlo , GIARDINA, Giuseppe , GRUGNI, Mario,NiKem Research srl , NADLER, Guy, Marguerite, Marie, Gerard
IPC分类号： A61K31/47
CPC分类号： C07D401/06 , C07D401/14
摘要： Certain compounds of formula (I) or a pharmaceutically acceptable salts or hydrate thereof wherein R1 is H or alkyl; R2 is aryl or cycloalkyl or heteroaryl; R3 is H or alkyl, optionally substituted by one or more fluorines; R4 is -NR8R9 or R12; r8 is H or methyl; R9 is H, alkyl, aryl, cycloalkyl or R10R11; or R8 and R9 together form a heterocyclic ring comprising 3-8 ringe members, which heterocyclic ring is optionally unsubstituted or is substituted one or more times by R11; R10 is alkyl, aryl or cycloalkyl; R11 is carboxy or alkylcarboxy; R12 is R13 or OR13; R13 is H or alkyl or aryl, optionally substituted by one or more fluorines; R5 is branched or linear alkyl, cycloalkyl, 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: alkyl, alkenyl, aryl, alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, alkoxycarbonyl, trifluoromethyl, acyloxy, amino or mono or di-alkylamino; R7 is H or halo; a is 1-6; and any of R2, R5, R9, and R10 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.
摘要翻译：某些式（I）化合物或其药学上可接受的盐或水合物，其中R 1为H或烷基; R2是芳基或环烷基或杂芳基; R3是H或烷基，任选被一个或多个氟取代; R4是-NR8R9或R12; r8是H或甲基; R9是H，烷基，芳基，环烷基或R10R11; 或R 8和R 9一起形成包含3-8个环部分的杂环，所述杂环任选未被取代或被R 11取代一次或多次; R10是烷基，芳基或环烷基; R11是羧基或烷基羧基; R12是R13或OR13; R13是H或烷基或芳基，任选被一个或多个氟取代; R5是支链或直链烷基，环烷基，环烷基烷基，芳基或单环或稠环芳族杂环基团; R6代表H或至多三个独立地选自下列的取代基：烷基，烯基，芳基，烷氧基，羟基，卤素，硝基，氰基，羧基，甲酰氨基，磺酰氨基，烷氧羰基，三氟甲基，酰氧基，氨基或单或二 - 烷基; R7是H或卤素; a是1-6; 并且R 2，R 5，R 9和R 10中的任一个可任选地被卤素，羟基，氨基，氰基，硝基，羧基或氧代取代一次或多次; 制备这些化合物的方法，包含这些化合物的药物组合物以及这些化合物和组合物在药物中的用途。

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