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1. 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。

2. 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。

3. 发明授权

US06613770B1 Quinoline derivatives as NK-2 and NK-3 receptor ligands 失效
标题翻译：喹啉衍生物作为NK-2和NK-3受体配体
公开(公告)号：US06613770B1
公开(公告)日：2003-09-02
申请号：US09856385
申请日：2001-09-28
申请人： Carlo Farina , Giuseppe Giardina , Mario Grugni , Guy Marguerite Marie Gerard Nadler , Luca Francesco Raveglia
发明人： Carlo Farina , Giuseppe Giardina , Mario Grugni , Guy Marguerite Marie Gerard Nadler , Luca Francesco Raveglia
IPC分类号： A61K314725
CPC分类号： C07D401/06 , C07D215/52 , C07D401/14
摘要： A compound, or a solvate or a salt thereof, of formula (I): wherein R is linear or branched alkyl; 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 alkyl or R4 and R together with the carbon atom to which they are attached form an optionally substituted C3-12 cycloalkyl group; 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：式（I）的化合物或其溶剂化物或其盐：其中R是直链或支链烷基; R1代表氢或最多四个选自下列的任选取代基：C 1-6烷基，C 1-6烯基芳基，C 1-6烷氧基，羟基，卤素，硝基，氰基，羧基，甲酰胺基，磺酰氨基，C 1-6烷氧基羰基，三氟甲基，酰氧基，苯二甲酰亚氨基，氨基或单-C2和二-C6烷基氨基; R2代表 - （CH2）n-NY1Y2其中n是1至9的整数，Y1和Y2独立地选自氢; C 1-6 - 烷基; 被羟基，C 1-6烷基氨基或双（C 1-6烷基）氨基取代的C 1-6烷基; C 1-6 - 烯基; 芳基或芳基-C 1-6 - 烷基或Y1和Y2与它们所连接的氮原子一起表示任选取代的N-连接的单或稠环杂环基; R 3是支链或直链C 1-6烷基，C 3-7 环烷基，C 4-7环烷基烷基，任选取代的芳基或任选取代的单环或稠环芳族杂环基; R 4表示氢或烷基或R 4，R与它们所连接的碳原子一起形成任选取代的C 3-12环烷基; 制备这种化合物的方法，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。

4. 发明申请

US20060161004A1 Novel compounds 审中-公开
标题翻译：新型化合物
公开(公告)号：US20060161004A1
公开(公告)日：2006-07-20
申请号：US11331623
申请日：2006-01-13
申请人： Carlo Farina , Giuseppe Giardina , Mario Grugni , Guy Marguerite Nadler
发明人： Carlo Farina , Giuseppe Giardina , Mario Grugni , Guy Marguerite Nadler
IPC分类号： A61K31/4709 , C07D401/02
CPC分类号： C07D401/06 , C07D401/14
摘要： Certain compounds of formula (I): 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。

5. 发明授权

US06780875B2 Quinoline-4-carboxamide derivatives as NK-3 and NK-2 receptor antagonists 失效
标题翻译：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：US06780875B2
公开(公告)日：2004-08-24
申请号：US10358938
申请日：2003-02-05
申请人： Carlo Farina , Giuseppe Giardina , Mario Grugni , Marcel Morvan , Guy Marguerite Marie Gérard Nadler , Luca Francesco Raveglia
发明人： Carlo Farina , Giuseppe Giardina , Mario Grugni , Marcel Morvan , Guy Marguerite Marie Gérard Nadler , Luca Francesco Raveglia
IPC分类号： A61K314709
CPC分类号： C07D401/06 , C07D215/52 , C07D401/12 , C07D401/14 , C07D413/10 , C07D417/12 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/10
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 C5-7 cycloalkyl group, or an optionally substituted single or fused ring aromatic heterocyclic group; R is hydrogen, linear or branched C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl; R1 represents hydrogen or up to three 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, amino or mono- and di-C1-6 alkylamino, R2 represents a moiety —(CH2)n—NYY2 wherein n is an integer in the range of from 1 to 9, Y1 and Y2 are independently selected from C1-6-alkyl; C1-6 alkyl substituted with hydroxy, alkoxy, C1-6 alkylamino or bis (C1-6 alkyl) amino; C3-6 cycloalkyl; C4-6 azacycloalkyl; 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, R5 represents hydrogen or halogen; 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：式（I）的化合物或其溶剂化物或其盐：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C 5-7环烷基，或任选取代的单或稠合环芳族杂环基团; R是氢，直链或支链C 1-6烷基，C 3-7环烷基，C 3-7环烷基烷基; R 1代表氢或最多三个选自下列的任选取代基：C 1-6烷基， 6-烯基，芳基，C 1-6烷氧基，羟基，卤素，硝基，氰基，羧基，甲酰氨基，磺酰氨基，C 1-6烷氧基羰基，三氟甲基，酰氧基，氨基或单-C 1-6烷基氨基，（CH 2）n -NYY 2，其中n是1至9的整数，Y 1和Y 2独立地选自C 1-6 - 烷基; 被羟基，烷氧基，C 1-6烷基氨基或双（C 1-6烷基）氨基取代的C 1-6烷基; C3-6环烷基; C4-6氮杂环烷基; C 1-6 - 烯基; 芳基或芳基-C 1-6 - 烷基或Y1和Y2与它们所连接的氮原子一起表示任选取代的N-连接的单或稠环杂环基; R 3是支链或直链C 1-6烷基，C 3-7 环烷基，C 4-7环烷基烷基，任选取代的芳基或任选取代的单环或稠环芳族杂环基; R 4表示氢或C 1-6烷基，R 5表示氢或卤素; 制备这种化合物的方法，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。

6. 发明申请

US20050070574A1 Novel compounds 审中-公开
公开(公告)号：US20050070574A1
公开(公告)日：2005-03-31
申请号：US10949185
申请日：2004-09-24
申请人： Carlo Farina , Giuseppe Giardina , Mario Grugni , Guy Marguerite Nadler
发明人： Carlo Farina , Giuseppe Giardina , Mario Grugni , Guy Marguerite Nadler
IPC分类号： A61K31/4709 , A61P1/04 , A61P7/04 , A61P7/12 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/10 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P27/02 , A61P27/16 , A61P29/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D401/06 , C07D401/14 , C07D409/14 , C07D41/02
CPC分类号： C07D401/06 , C07D401/14
摘要： Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: wherein: R1 is H or alkyl; R2 is —R8R9; R8 is a single bond or alkyl, optionally substituted one or more times by hydroxy; R9 is aryl or cycloalkyl or heteroaryl, optionally substituted one or more times by hydroxy, alkoxy, or alkoxyalkyl; R3 is H or alkyl or cycloalkyl or cycloalkylalkyl, optionally substituted one or more times by hydroxy or by one or more fluorines; R4 is —NR10R11; R10 and R11 are independently selected from H or alkyl, or R10 and R11 together with the nitrogen atom to which they are attached form a saturated or unsaturated heterocyclic ring comprising 3-8 ring members, which heterocyclic ring is unsubstituted or is substituted one or more times by one or more substituents R12; R12 is oxo or —R13R14R15, wherein R13 is a single bond or alkyl, R14 is OC(O) or C(O)O, and R15 is H or alkyl; R5 is an alkyl, cycloalkyl, cycloalkylalkyl, aryl, or single or fused ring aromatic heterocyclic group, which group is unsubstituted or is substituted one or more times by one or more substituents selected from halo such as fluoro, alkyl or haloalkyl such as fluoroalkyl; R6 represents H or up to three substituents independently selected from the list consisting of: alkyl, alkenyl, aryl, alkoxy or a hydroxylated derivative thereof, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, alkoxycarbonyl, haloalkyl such as trifluoromethyl, acyloxy, amino, mono- or di-alkylamino, alkoxyamido, alkoxycarboxylate or an esterified derivative thereof; R7 is H or halo; a is 1-6; and any of R1, R3, R5, R8, R9, 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.

7. 发明申请

US20060235026A1 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.

8. 发明申请

US20060160846A1 Quinoline derivatives 失效
标题翻译：喹啉衍生物
公开(公告)号：US20060160846A1
公开(公告)日：2006-07-20
申请号：US11385461
申请日：2006-03-21
申请人： Carlo Farina , Giuseppe Giardina , Mario Grugni , Luca Raveglia
发明人： Carlo Farina , Giuseppe Giardina , Mario Grugni , Luca Raveglia
IPC分类号： A61K31/4709 , C07D401/02
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): are useful in treating inter alia pulmonary disorders, CNS disorders and neurodegenerative disorders.
摘要翻译：式（I）的NK 3受体拮抗剂：可用于治疗肺功能紊乱，中枢神经系统疾病和神经变性疾病。

9. 发明申请

US20050182093A1 Novel compounds 审中-公开
标题翻译：新型化合物
公开(公告)号：US20050182093A1
公开(公告)日：2005-08-18
申请号：US11102943
申请日：2005-04-11
申请人： Carlo Farina , Giuseppe Giardina , Mario Grugni , Lorenzo Perugini
发明人： Carlo Farina , Giuseppe Giardina , Mario Grugni , Lorenzo Perugini
IPC分类号： C07D491/056 , A61K31/4709 , A61K31/4741 , A61P1/04 , A61P11/00 , A61P11/06 , A61P13/02 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/04 , A61P25/02 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/02 , A61P29/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D215/52 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , A61K31/55 , C07D41/14
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和这些化合物在医药中的用途。

10. 发明申请

US20050096316A1 Quinoline derivatives(2) 审中-公开
标题翻译：喹啉衍生物（2）
公开(公告)号：US20050096316A1
公开(公告)日：2005-05-05
申请号：US10999180
申请日：2004-11-29
申请人： Carlo Farina , Giuseppe Giardina , Mario Grugni , Luca Raveglia
发明人： Carlo Farina , Giuseppe Giardina , Mario Grugni , Luca Raveglia
IPC分类号： A61K31/00 , A61K31/47 , A61K31/4709 , A61K31/473 , A61K45/00 , A61P1/00 , A61P1/14 , A61P1/16 , A61P3/00 , A61P3/04 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/00 , A61P13/02 , A61P13/12 , A61P17/00 , A61P17/06 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/00 , A61P27/02 , A61P27/16 , A61P29/00 , A61P37/08 , A61P43/00 , C07D215/52 , C07D221/18 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/04 , C07D417/02 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D413/02 , C07D43/02
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): are useful in treating inter alia pulmonary disorders, CNS disorders and neurodegenerative disorders.
摘要翻译：式（I）的NK 3受体拮抗剂：可用于治疗肺功能紊乱，中枢神经系统疾病和神经变性疾病。

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