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1. 发明申请

US20060223819A1 Quinoline Derivatives as NK-3 Antagonists 审中-公开
标题翻译：喹啉衍生物作为NK-3拮抗剂
公开(公告)号：US20060223819A1
公开(公告)日：2006-10-05
申请号：US11425508
申请日：2006-06-21
申请人： Carlo Farina , Stefania Gagliardi , Giuseppe Giardina , Mario Grugni , Marisa Martinelli , Guy Marguerite Nadler
发明人： Carlo Farina , Stefania Gagliardi , Giuseppe Giardina , Mario Grugni , Marisa Martinelli , Guy Marguerite Nadler
IPC分类号： A61K31/496 , C07D403/02
CPC分类号： C07D401/06 , A61K31/495 , C07D215/52 , C07D409/14 , C07D493/04
摘要： Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: 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：某些下面的式（I）化合物或其药学上可接受的盐或水合物：制备此类化合物的方法，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医药中的用途。

2. 发明申请

WO2002083664A1 3-SUBSTITUTED QUINOLINE-4-CARBOXAMIDE DERIVATIVES AS NK-3 AND NK-2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 3-取代的喹啉-4-羧酰胺衍生物作为NK-3和NK-2受体拮抗剂
公开(公告)号：WO2002083664A1
公开(公告)日：2002-10-24
申请号：PCT/EP2002/004070
申请日：2002-04-11
申请人： GLAXOSMITHKLINE S.P.A. , FARINA, Carlo , GAGLIARDI, Stefania , GIARDINA, Giuseppe, Arnaldo, Maria , MARTINELLI, Marisa
发明人： FARINA, Carlo , GAGLIARDI, Stefania , GIARDINA, Giuseppe, Arnaldo, Maria , MARTINELLI, Marisa
IPC分类号： C07D401/06
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 R 1 is H or alkyl; R 2 is aryl or cycloalkyl or heteroaryl; R 3 is H or alkyl, wherein the alkyl group may be optionally substituted by one or more fluorine atoms; R 4 is H, hydroxyalkyl, dihydroxyalkyl or hydroxyalkoxyalkyl; R 5 is branched or linear alkyl, cycloalkyl, cycloalkylalkyl, aryl, or a single or fused ring aromatic heterocyclic group; R 6 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; R 7 is H or halo; R¿8= is H or =O; and any of R 2 and R 5 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.
摘要翻译：下面的化合物（I）或其药学上可接受的盐或溶剂合物：其中R1是H或烷基; R2是芳基或环烷基或杂芳基; R3是H或烷基，其中烷基可以任选被一个或多个氟原子取代; R4是H，羟基烷基，二羟基烷基或羟基烷氧基烷基; R5是支链或直链烷基，环烷基，环烷基烷基，芳基或单或稠环芳族杂环基; R6代表H或至多三个独立地选自烷基，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，三氟甲基或氨基或单或二烷基氨基的取代基的取代基。 R7是H或卤素; R8 =是H或= O; 羟基，氨基，氰基，硝基，羧基，氧代，烷基，烯基，芳基，烷氧基，甲酰氨基，磺酰氨基，三氟甲基或单或二烷基氨基取代一次或多次 ; 条件是所述式（I）化合物不是选自根据权利要求1的列表的化合物。

3. 发明申请

WO2003040099A1 PREPARATION OF BENZOSUBERONYLPIPERIDINE COMPOUNDS 审中-公开
标题翻译：苯并噻唑啉化合物的制备
公开(公告)号：WO2003040099A1
公开(公告)日：2003-05-15
申请号：PCT/EP2002/012356
申请日：2002-11-05
申请人： GLAXOSMITHKLINE S.P.A. , PALOMBI, Giovanni , RONZONI, Silvano
发明人： PALOMBI, Giovanni , RONZONI, Silvano
IPC分类号： C07D211/22
CPC分类号： C07D211/22
摘要： Diastereoselective and enantioselective synthetic routes for the preparation of compounds of formula (I) or derivatives thereof, wherein: R is C 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkoxy, hydroxy, halo, C 1-6 alkenyl, C 1-6 alkynyl, amino, C 1-6 alkylamino, di(C 1-6 alkyl)amino, hydroxyC 1-6 alkyl, C 1-6 alkoxyC 1-6 alkyl, arylC 1-6 alkoxy, heteroarylC 1-6 alkoxy, aminoC 1-6 alkyl, (C 1-6 alkyl)aminoC 1-6 alkyl, di(C 1-6 alkyl)aminoC 1-6 alkyl, arylC 1-6 alkylamino, heteroarylC 1-6 alkylamino; R 1 is hydrogen or R; R 2 is hydroxy, C 1-6 alkoxy, amino, C 1-6 alkylamino, di(C 1-6 alkyl)amino; R 3 and R 4 are each independently selected from the list consisting of perhaloC 1-6 alkyl, hydrogen, halo, C 1-6 alkyl, C 1-6 alkoxy, hydroxy, amino, C 1-6 alkylamino, di(C 1-6 alkyl)amino, hydroxyC 1-6 alkyl, C 1-6 alkoxyC 1-6 alkyl, aminoC 1-6 alkyl, (C 1-6 alkyl)aminoC 1-6 alkyl, di(C 1-6 alkyl)aminoC 1-6 alkyl, aryl, and COX wherein X may be hydroxy, C 1-6 alkoxy, C 1-6 alkyl, amino, C 1-6 alkylamino, or di(C 1-6 alkyl)amino; andwherein any alkyl group or the alkyl moiety of any group containing such a moiety may be substituted one or more times by halo.
摘要翻译：用于制备式（I）化合物或其衍生物的非对映选择性和对映选择性合成路线，其中：R为C 1-6烷基，C 3-7环烷基，C 1-6烷氧基，羟基，卤素，C 1-6烯基，C 1-6炔基，氨基，C 1 （C 1-6烷基）氨基，C 1-6烷基氨基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，芳基C 1-6烷氧基，杂芳基C 1-6烷氧基，氨基C 1-6烷基，（C 1-6烷基）氨基C 1-6烷基， C 1-6烷基，芳基C 1-6烷基氨基，杂芳基C 1-6烷基氨基; R 1是氢或R; R 2是羟基，C 1-6烷氧基，氨基，C 1-6烷基氨基，二（C 1-6烷基）氨基; R 3和R 4各自独立地选自全卤代C 1-6烷基，氢，卤素，C 1-6烷基，C 1-6烷氧基，羟基，氨基，C 1-6烷基氨基，二（C 1-6烷基）氨基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，氨基C 1-6烷基，（C 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基）氨基C 1-6烷基，芳基和COX，其中X可以是羟基，C 1-6烷氧基，C 1-6烷基，氨基，C 1-6烷基氨基或二（C 1-6烷基）氨基; 并且任何烷基或含有该部分的任何基团的烷基部分可以被卤素取代一次或多次。

4. 发明申请

WO2005005411A1 SUBSTITUTED INDOLE LIGANDS FOR THE ORL-1 RECEPTOR 审中-公开
标题翻译：替代ORL-1受体的替代配体
公开(公告)号：WO2005005411A1
公开(公告)日：2005-01-20
申请号：PCT/EP2004/007294
申请日：2004-07-01
申请人： GLAXOSMITHKLINE S.P.A. , CONSONNI, Alessandra , DEL SORDO, Simone , FARINA, Carlo , GAGLIARDI, Stefania , RONZONI, Silvano , VALLESE, Stefania
发明人： CONSONNI, Alessandra , DEL SORDO, Simone , FARINA, Carlo , GAGLIARDI, Stefania , RONZONI, Silvano , VALLESE, Stefania
IPC分类号： C07D401/06
CPC分类号： C07D409/14 , C07D401/06 , C07D401/14 , C07D405/14
摘要： New ligands for the ORL-1 receptor are described, useful for modulating the activity of said receptors in a patient in need thereof, and for preventing and treating illnesses dependent on the stimulation of this receptor. The new compounds conform to structural formula (I), wherein Q is a moiety of formula (II) and R, R 0 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 are further defined in the description.
摘要翻译：描述了ORL-1受体的新配体，可用于调节有需要的患者中所述受体的活性，以及用于预防和治疗依赖于该受体刺激的疾病。新化合物符合结构式（I），其中Q是式（II）的部分，R 1，R 2，R 1，R 2，R 3，R 4，R 4， <5>，R 6在说明书中进一步限定。

5. 发明申请

WO2002083663A1 QUINOLINE-4-CARBOXAMIDE DERIVATIVES AS NK-3 AND NK-2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：喹啉-4-羧酰胺衍生物作为NK-3和NK-2受体拮抗剂
公开(公告)号：WO2002083663A1
公开(公告)日：2002-10-24
申请号：PCT/EP2002/004066
申请日：2002-04-11
申请人： GLAXOSMITHKLINE S.P.A. , FARINA, Carlo , GAGLIARDI, Stefania , GIARDINA, Giuseppe, Arnaldo, Maria , MARTINELLI, Marisa
发明人： FARINA, Carlo , GAGLIARDI, Stefania , GIARDINA, Giuseppe, Arnaldo, Maria , MARTINELLI, Marisa
IPC分类号： C07D401/06
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 of formula (I) as detailed in the specification or a pharmaceutically acceptable salt or solvate thereof, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine. Figure (I) wherein: R 1 is H or alkyl; R 2 is aryl or cycloalkyl or heteroaryl; R 3 is H or alkyl, wherein the group may be optionally substituted by one or more fluorine atoms; R 4 is NR 8 R 9 ; R 8 is H, lakyl or R 11 R 12 and R 9 is H, alkyl or R 13 R 14 ; or R 8 and R 9 together with the N atom to wich they are attached form a heterocyclic ring comprising 4-8 ring members, said ring members optionally including in addition to said N atom one or more further heteroatoms selected from N, O or S; and further detailed in the specification.
摘要翻译：说明书或其药学上可接受的盐或溶剂合物中详述的式（I）化合物，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在医药中的用途。图（I）其中：R1是H或烷基; R2是芳基或环烷基或杂芳基; R3是H或烷基，其中基团可以任选被一个或多个氟原子取代; R4是NR8R9; R8是H，烷基或R11R12，R9是H，烷基或R13R14; 或R 8和R 9与它们所连接的N原子一起形成包含4-8个环成员的杂环，所述环成员除了所述N原子之外任选地还包括一个或多个另外的选自N，O或S的杂原子; 并在说明书中进一步详细描述。

6. 发明申请

WO2002083645A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2002083645A1
公开(公告)日：2002-10-24
申请号：PCT/EP2002/004069
申请日：2002-04-11
申请人： GLAXOSMITHKLINE S.P.A. , FARINA, Carlo , GIARDINA, Giuseppe, Arnaldo, Maria , GRUGNI, Mario , PERUGINI, Lorenzo
发明人： FARINA, Carlo , GIARDINA, Giuseppe, Arnaldo, Maria , GRUGNI, Mario , PERUGINI, Lorenzo
IPC分类号： C07D215/52
CPC分类号： C07D401/14 , C07D215/52
摘要： A compound of formula (I) as detailed in the specification or a pharmaceutically acceptable salt or solvate thereof, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine.
摘要翻译：说明书或其药学上可接受的盐或溶剂合物中详述的式（I）化合物，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在医药中的用途。

7. 发明申请

US20070015766A1 Quinoline Derivatives as NK-3 and NK-2 Antagonists 审中-公开
标题翻译：喹啉衍生物作为NK-3和NK-2拮抗剂
公开(公告)号：US20070015766A1
公开(公告)日：2007-01-18
申请号：US11426414
申请日：2006-06-26
申请人： Carlo Farina , Stefania Gagliardi , Giuseppe Giardina , Mario Grugni , Marisa Martinelli , Guy Marguerite Marie Gerard Nadler
发明人： Carlo Farina , Stefania Gagliardi , Giuseppe Giardina , Mario Grugni , Marisa Martinelli , Guy Marguerite Marie Gerard Nadler
IPC分类号： A61K31/496 , C07D403/02
CPC分类号： C07D401/12 , C07D215/52
摘要： Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: wherein: R1 is H or alkyl; R2 is aryl, cycloalkyl or heteroaryl; R3 is H or C1-3 alkyl, optionally substituted by one or more fluorines; R4 is H, R8NR9R10, R11R13 or R11R12R13; or R5 is branched or linear alkyl, cycloalkyl, aryl, arylalkyl, or a single or fused ring aromatic heterocyclic group; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and the use of such compounds and composition in medicine.
摘要翻译：某些下式（I）化合物或其药学上可接受的盐或水合物：其中：R 1是H或烷基; R 2是芳基，环烷基或杂芳基; R 3是H或C 1-3烷基，任选被一个或多个氟取代; R 4是H，R 8 NR 9 R 10，R 11 R 13或13个R 12 R 13 13; 或R 5是支链或直链烷基，环烷基，芳基，芳烷基或单或稠环芳族杂环基; 制备这些化合物的方法，包含这些化合物的药物组合物和这些化合物的用途以及这些化合物和组合物在医药中的用途。

8. 发明申请

US20070161647A1 QUINOLINE-4-CARBOXAMIDE DERIVATIVES AS NK-3 and NK-2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：喹啉-4-羧酰胺衍生物作为NK-3和NK-2受体拮抗剂
公开(公告)号：US20070161647A1
公开(公告)日：2007-07-12
申请号：US11685380
申请日：2007-03-13
申请人： Carlo Farina , Stefania Gagliardi , Giuseppe Giardina , Marisa Martinelli
发明人： Carlo Farina , Stefania Gagliardi , Giuseppe Giardina , Marisa Martinelli
IPC分类号： A61K31/496 , A61K31/4747 , C07D403/02 , C07D471/10
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 of formula (I) as detailed in the specification or a pharmaceutically acceptable salt or solvate thereof, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine.
摘要翻译：说明书或其药学上可接受的盐或溶剂合物中详述的式（I）化合物，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在医药中的用途。

9. 发明授权

US07115633B2 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.

10. 发明授权

US07223867B2 Preparation of benzosuberonylpiperidine compounds 失效
公开(公告)号：US07223867B2
公开(公告)日：2007-05-29
申请号：US10494838
申请日：2002-11-05
申请人： Giovanni Palombi , Silvano Ronzoni
发明人： Giovanni Palombi , Silvano Ronzoni
IPC分类号： C07D211/06
CPC分类号： C07D211/22
摘要： Diastereoselective and enantioselective synthetic routes for the preparation of compounds of formula (I): or derivatives 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, arylC1-6alkoxy, heteroarylC1-6alkoxy, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, arylC1-6alkylamino, heteroarylC1-6alkyamino; R1 is hydrogen or R; R2 is hydroxy, C1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino; R3 and R4 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, C1-6 alkoxy, C1-6alkyl, amino, C1-6alkylamino, or di(C1-6alkyl)amino; 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.

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