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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. 发明授权

US06903117B2 Indole derivatives for the treatment of osteoporosis 失效
标题翻译：吲哚衍生物用于治疗骨质疏松症
公开(公告)号：US06903117B2
公开(公告)日：2005-06-07
申请号：US10300332
申请日：2002-11-20
申请人： Carlo Farina , Stefania Gagliardi , Guy Marguerite Marie Gerard Nadler
发明人： Carlo Farina , Stefania Gagliardi , Guy Marguerite Marie Gerard Nadler
IPC分类号： B82B1/00 , C07D209/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D451/02 , C07D451/04 , C07D455/02 , C07D471/04 , C07D471/08 , C07D471/16 , A61K31/454
CPC分类号： C07D451/02 , C07D209/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D451/04 , C07D455/02 , C07D471/04 , C07D471/08
摘要： A compound of formula (I): or a salt thereof, or a solvate thereof, wherein Ra represents a group R5 which is hydrogen, alkyl or optionally substituted aryl and Rb represents a moiety of formula (a): wherein X represents a hydroxy or an alkoxy group wherein the alkyl group may be substitued or unsubstituted or X represents a group NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, an optionally substituted heterocyclic group or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclic group; R1 represents an alkyl or a substituted or unsubstituted aryl group; and R2, R3 and R4 each independently represent hydrogen, alkyl, aryl or substituted aryl; R6 and R7 each independently represent hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R6 and R7 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; and R8 represents hydrogen, hydroxy, alkynoyl, alkyl, aminoalkyl, hydroxyalkyl, carboxyalky, carbalkoxyalkyl, carbamoyl or aminosulphonyl; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound in medicine.
摘要翻译：式（I）化合物或其盐或其溶剂合物，其中R a表示R 5基团，其为氢，烷基或任选取代的芳基，R b表示式（a ）：其中X表示羟基或烷氧基，其中烷基可以被取代或未被取代，或X表示基团NR 1 R t R 3和R 3各自独立地表示氢，烷基，取代的烷基，任选取代的烯基，任选取代的芳基，任选取代的芳烷基，任选取代的杂环基或任选取代的杂环基烷基，和它们所连接的氮一起形成杂环基; R 1表示烷基或取代或未取代的芳基; 和R 2，R 3和R 4各自独立地表示氢，烷基，芳基或取代的芳基; R 6和R 7各自独立地表示氢，羟基，氨基，烷氧基，任选取代的芳氧基，任选取代的苄氧基，烷基氨基，二烷基氨基，卤素，三氟甲基，三氟甲氧基，硝基，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基或R 6和R 7一起代表亚甲二氧基，羰基二氧基或羰基二氨基; R 8表示氢，羟基，炔酰基，烷基，氨基烷基，羟基烷基，羧基，烷氧基烷基，氨基甲酰基或氨基磺酰基; 制备这种化合物的方法，含有这种化合物的药物组合物和这种化合物在医药中的用途。

3. 发明授权

US6025390A Heteroaromatic pentadienoic acid derivatives useful as inhibitors of bone resorption 失效
标题翻译：可用作骨吸收抑制剂的杂芳族戊二烯酸衍生物
公开(公告)号：US6025390A
公开(公告)日：2000-02-15
申请号：US214689
申请日：1999-06-23
申请人： Carlo Farina , Stefania Gagliardi , Guy Marguerite Marie Gerard Nadler , Michel Jean Roger Martin
发明人： Carlo Farina , Stefania Gagliardi , Guy Marguerite Marie Gerard Nadler , Michel Jean Roger Martin
IPC分类号： A61K31/343 , A61K31/381 , A61K31/4525 , A61K31/4535 , A61K31/47 , A61P19/10 , C07D215/12 , C07D307/80 , C07D333/60 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , A61K31/34 , A61K31/38 , A61K31/445 , C07D215/00 , C07D401/00
CPC分类号： C07D405/06 , C07D215/12 , C07D307/80 , C07D333/60 , C07D409/06
摘要： A compound of formula (I) or a salt thereof, or a solvate thereof, ##STR1## wherein: R.sub.1 represents an alkyl group or a substituted or unsubstituted aryl group; R.sub.2, R.sub.3 and R.sub.4 each independently represent hydrogen, alkyl, aryl or substituted aryl; R.sub.5 and R.sub.6 each independently represent hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R.sub.5 and R.sub.6 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; X represents a hydroxy or an alkoxy group wherein the alkyl group may be substituted or unsubstituted or X represents a group NR.sub.S R.sub.t wherein R.sub.S and R.sub.t each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, an optionally substituted heterocyclic group or an optionally substituted heterocyclylalkyl group, or R.sub.S and R.sub.t together with the nitrogen to which they are attached form a heterocyclic group; and Y represents O or S and Z represents CH, CH.dbd.CH or N; or Y represents NR.sub.7 wherein R.sub.7 represents hydrogen, hydroxy, alkanoyl, alkyl, aminoalkyl, hydroxyalkyl, carboxyalkyl, carbalkoxyalkyl, carbamoyl or aminosulphonyl and Z represents CH.dbd.CH or N; a pharmaceutical composition containing such a compound, a process for preparing such a compound and the use of such a compound in medicine.
摘要翻译： PCT No.PCT / EP97 / 03709 Sec。 371日期1999年6月23日第 102（e）1999年6月23日PCT 1997年7月7日PCT公布。出版物WO98 / 01436 日期1998年1月15日A式（I）化合物或其盐或其溶剂化物，其中：R1表示烷基或取代或未取代的芳基; R2，R3和R4各自独立地表示氢，烷基，芳基或取代的芳基; R5和R6各自独立地表示氢，羟基，氨基，烷氧基，任选取代的芳氧基，任选取代的苄氧基，烷基氨基，二烷基氨基，卤素，三氟甲基，三氟甲氧基，硝基，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基或R5和R6一起代表亚甲二氧基，羰基二氧基或羰基二氨基; X表示羟基或烷氧基，其中烷基可以是取代或未取代的或X表示NRSRt基团，其中RS和Rt各自独立地表示氢，烷基，取代的烷基，任选取代的烯基，任选取代的芳基，任选取代的芳基烷基，任选取代的杂环基或任选取代的杂环基烷基，或RS和R R与它们所连接的氮一起形成杂环基; Y表示O或S，Z表示CH，CH = CH或N; 或Y表示NR 7，其中R 7表示氢，羟基，烷酰基，烷基，氨基烷基，羟基烷基，羧基烷基，烷氧基烷基，氨基甲酰基或氨基磺酰基，Z表示CH = CH或N; 含有这种化合物的药物组合物，这种化合物的制备方法和这种化合物在医药中的应用。

4. 发明授权

US5981525A Indole derivatives useful in the treatment of osteoporosis 失效
标题翻译：吲哚衍生物可用于治疗骨质疏松症
公开(公告)号：US5981525A
公开(公告)日：1999-11-09
申请号：US860760
申请日：1997-10-09
申请人： Carlo Farina , Stefania Gagliardi , Carlo Parini , Mario Pinza , Guy Marguerite Marie Gerard Nadler , Marcel Jean-Marie Morvan
发明人： Carlo Farina , Stefania Gagliardi , Carlo Parini , Mario Pinza , Guy Marguerite Marie Gerard Nadler , Marcel Jean-Marie Morvan
IPC分类号： C07D487/04 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/475 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/535 , A61P3/06 , A61P7/00 , A61P19/10 , A61P25/28 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/04 , A61P43/00 , C07D209/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , C07D451/04 , C07D453/02 , C07D471/04 , C07D473/34 , C07D521/00 , C07F9/572 , C07D209/14 , C07D209/12
CPC分类号： C07D231/12 , C07D209/18 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , C07D451/04 , C07D453/02 , C07D471/04 , C07D473/34 , C07F9/5728
摘要： A compound of formula (I) or a salt thereof, or a solvate thereof, wherein either (i) Ra represents a group R.sub.5 which is hydrogen, alkyl or optionally substituted aryl and R.sub.5 represents a moiety of formula (a); wherein X represents a hydroxy or an alkoxy group wherein the alkyl group may be substituted or unsubstituted or X represents a group NR.sub.s R.sub.t wherein R.sub.s and R.sub.t each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, an optionally substituted heterocyclic group or an optionally substituted heterocyclylalkyl group, or R.sub.s and R.sub.t together may form a heterocyclic group; R.sub.1 represents an alkyl or a substituted or unsubstituted aryl group; and R.sub.2, R.sub.3 and R.sub.4 each independently represent hydrogen, alkyl, aryl or substituted aryl or (ii) R.sub.a represents a moiety of the above defined formula (a) and R.sub.b represents the above defined R.sub.5 ; R.sub.6 and R.sub.7 each independently represents hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R.sub.6 and R.sub.7 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; and R.sub.8 represents hydrogen, hydroxy, allanoyl, alkyl, aminoalkyl, hydroxyalkyl, carboxyalkyl, carbalkoxyalkyl, carbamoyl or aminosulphonyl; a process for the preparation of such a compound, a pharmaceutical composition comprising such a compound and the use of such a compound in medicine.
摘要翻译： PCT No.PCT / EP96 / 00157 Sec。 371 1997年10月9日第 102（e）1997年10月9日PCT PCT 1996年1月8日PCT公布。公开号WO96 / 21644 日期：1996年7月18日一种式（I）化合物或其盐或其溶剂合物，其中（i）Ra表示氢，烷基或任选取代的芳基的基团R 5，R 5表示式（a ）; 其中X表示羟基或烷氧基，其中烷基可以是取代或未取代的或X表示基团NRsRt，其中R 5和R t各自独立地表示氢，烷基，取代的烷基，任选取代的烯基，任选取代的芳基，任选取代的芳基烷基，任选取代的杂环基或任选取代的杂环基烷基，或者R 1和R 2一起可以形成杂环基; R1表示烷基或取代或未取代的芳基; 并且R 2，R 3和R 4各自独立地表示氢，烷基，芳基或取代的芳基或（ii）R a表示上述定义的式（a）的部分，R b表示上述定义的R 5; R6和R7各自独立地表示氢，羟基，氨基，烷氧基，任选取代的芳氧基，任选取代的苄氧基，烷基氨基，二烷基氨基，卤素，三氟甲基，三氟甲氧基，硝基，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基或R6和R7一起表示亚甲二氧基，羰基二氧基或羰基二氨基; 羟基，烷酰基，氨基烷基，羟基烷基，羧基烷基，碳烷氧基烷基，氨基甲酰基或氨基磺酰基; 制备这种化合物的方法，包含这种化合物的药物组合物和这种化合物在医药中的用途。

5. 发明授权

US06506758B2 Indole derivatives useful A.O. for the treatment of osteoporosis 失效
标题翻译：吲哚衍生物有用A.O. 用于治疗骨质疏松症
公开(公告)号：US06506758B2
公开(公告)日：2003-01-14
申请号：US09975347
申请日：2001-10-11
申请人： Stefania Gagliardi , Guy Marguerite Marie Gerard Nadler , Pietro A T Novella
发明人： Stefania Gagliardi , Guy Marguerite Marie Gerard Nadler , Pietro A T Novella
IPC分类号： C07D40112
CPC分类号： C07D401/12 , C07D209/18
摘要： A compound of formula (I): or a salt thereof, or a solvate thereof, wherein: A represents an optionally substituted aryl group or an optionally substituted heterocyclyl group; Ra represents —CO—NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heterocyclyl or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclyl group; R1 and R2 each independently represents hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R1 and R2 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; and R3 represents hydrogen, alkanoyl, alkyl, aminoalkyl, hydroxyalkyl, carboxyalkyl, carbalkoxyalkyl, carbamoyl or alkylsulphonyl and arylsulphonyl; a process for the preparation of such a compound, a pharmaceutical composition containing such a compound and the use of such a compound or composition in medicine.
摘要翻译：式（I）化合物或其盐或其溶剂化物，其中：A表示任选取代的芳基或任选取代的杂环基; Ra表示-CO-NRsRt，其中R 5和R 5各自独立地表示氢，烷基取代的烷基，任选取代的烯基，任选取代的芳基，任选取代的芳基烷基，任选取代的杂环基或任选取代的杂环基烷基，或R 5和R 5与它们所连接的氮一起形成杂环基; R 1和R 2各自独立地表示氢，羟基，氨基，烷氧基，任选取代的芳氧基，任选取代的苄氧基，烷基氨基，二烷基氨基，卤素，三氟甲基，三氟甲氧基，硝基，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基，或R1和R2一起代表亚甲二氧基，羰基二氧基或羰基二氨基; 烷基，氨基烷基，羟基烷基，羧基烷基，烷氧基烷基，氨基甲酰基或烷基磺酰基和芳基磺酰基; 制备这种化合物的方法，含有这种化合物的药物组合物和这种化合物或组合物在医药中的用途。

6. 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。

7. 发明授权

US5985905A Indole derivatives for the treatment of osteoporosis 失效
标题翻译：吲哚衍生物用于治疗骨质疏松症
公开(公告)号：US5985905A
公开(公告)日：1999-11-16
申请号：US214648
申请日：1999-05-05
申请人： Carlo Farina , Guy Marguerite Marie Gerard Nadler , Pierfausto Seneci
发明人： Carlo Farina , Guy Marguerite Marie Gerard Nadler , Pierfausto Seneci
IPC分类号： A61K31/404 , A61K31/427 , A61P19/10 , A61P31/12 , A61P35/00 , C07D403/06 , C07D405/06 , C07D417/06 , A61K31/405 , A61K31/425
CPC分类号： C07D403/06 , C07D405/06 , C07D417/06
摘要： The invention relates to indole compounds, a process for preparing, pharmaceutical compositions containing the compounds and treating diseases associated with over activity of osteoclasts.
摘要翻译： PCT No.PCT / EP97 / 03711 Sec。 371日期1999年5月5日 102（e）日期1999年5月5日PCT 1997年7月7日PCT公布。第WO98 / 01445号公报日本1998年1月15日本发明涉及吲哚化合物，一种制备含有该化合物的药物组合物和治疗与破骨细胞的过度活性相关的疾病的方法。

8. 发明授权

US5712284A Azalicyclooctane derivatives as anti-arrhythmic agents 失效
标题翻译：作为抗心律失常剂的氮杂环辛烷衍生物
公开(公告)号：US5712284A
公开(公告)日：1998-01-27
申请号：US578667
申请日：1996-02-14
申请人： Guy Marguerite Marie Gerard Nadler , Michel Louis Souchet
发明人： Guy Marguerite Marie Gerard Nadler , Michel Louis Souchet
IPC分类号： C07D453/02 , A61K31/435 , A61K31/44 , A61P9/06 , A61P9/08 , A61P9/10 , C07D451/04 , C07D453/06
CPC分类号： C07D451/04
摘要： A compound of formula (I) or a salt thereof, or a solvate thereof: ##STR1## wherein B represents a C.sub.1-4 n-alkylene group wherein each carbon is optionally substituted by a C.sub.1-6 alkyl group; Z represents a bond, CH.sub.2, (CH.sub.2).sub.2 or X--CH.sub.2 --CH.sub.2 wherein X represents O or S; D represents CO, SO.sub.2, NH--CO or NH--SO.sub.2 ; T represents a bond and U represents CH.sub.2 or T represents CH.sub.2 and U represents a bond; Q represents aryl, aralkyl, aralkenyl or aralkynyl, wherein the aryl moiety may be unsubstituted or substituted with 1 to 5 substituents selected from the list consisting of nitre, halogen, alkylsulfonamido, acylamido, 1H-imidazolyl, alkyl or haloalkyl, or Q represents substituted or unsubstituted: furanyl, pyranyl, thienyl, thiazolyI, imidazolyl, triazolyl or the benzo fused equivalents or furanyl, pyranyl, thienyl, thiazolyl, 1H-imidazolyl, or triazolyl, indolyl, oxoindolyl, indenyl, isoindenyl, indazolyl, indolizinyl or pyridinyl or cycloalkyl optionally fused to an aryl group; R.sub.1, R.sub.2, and R.sub.3 each independently represents H, alkyl, OH or alkoxy or, if attached to adjacent carbon atoms, any two of R.sub.1, R.sub.2, and R.sub.3 together with the carbon atoms to which they are attached may form a fused heterocyclic ring of five or six atoms wherein one, two or three of the said atoms are oxygen or nitrogen; Ar represents substituted or unsubstituted aryl, wherein the optional substituents are the above defined R.sub.1, R.sub.2, and R.sub.3 or Ar represents a substituted or unsubstituted heteroaryl group; a process for the preparation of such a compound and the use of such a compound in medicine.
摘要翻译： PCT No.PCT / EP94 / 02299 Sec。 371日期：1996年2月14日 102（e）1996年2月14日PCT PCT 1994年7月11日PCT公布。公开号WO95 / 03301 日期：1995年2月2日一种式（I）化合物或其盐或其溶剂合物：其中B表示C 1-4正亚烷基，其中每个碳任选被C 1-6取代烷基; Z表示键，CH 2，（CH 2）2或X-CH 2 -CH 2，其中X表示O或S; D表示CO，SO2，NH-CO或NH-SO2; T表示键，U表示CH 2或T表示CH 2，U表示键; Q表示芳基，芳烷基，芳烯基或芳炔基，其中芳基部分可以是未取代的或被1至5个选自硝基，卤素，烷基磺酰氨基，酰基酰氨基，1H-咪唑基，烷基或卤代烷基的取代基取代，或Q表示取代的或未取代的：呋喃基，吡喃基，噻吩基，噻唑基，咪唑基，三唑基或苯并稠合的等价物或呋喃基，吡喃基，噻吩基，噻唑基，1H-咪唑基或三唑基，吲哚基，氧代吲哚基，茚基，异茚基，吲唑基，吲嗪基或吡啶基或环烷基任选地与芳基稠合; R 1，R 2和R 3各自独立地表示H，烷基，OH或烷氧基，或者如果连接到相邻碳原子上，则R 1，R 2和R 3中的任何两个与它们所连接的碳原子一起可以形成稠合杂环其中一个，两个或三个所述原子是氧或氮; Ar表示取代或未取代的芳基，其中任选取代基为上述定义的R 1，R 2和R 3或Ar表示取代或未取代的杂芳基; 制备这种化合物的方法和这种化合物在医药中的用途。

9. 发明授权

US07186730B2 Bicyclic nitrogen-containing heterocyclic derivatives for use as antibacterials 失效
标题翻译：用作抗菌剂的双环含氮杂环衍生物
公开(公告)号：US07186730B2
公开(公告)日：2007-03-06
申请号：US10477900
申请日：2002-05-24
申请人： Catherine Genevieve Yvette Dartois , Roger Edward Markwell , Guy Marguerite Marie Gerard Nadler , Neil David Pearson
发明人： Catherine Genevieve Yvette Dartois , Roger Edward Markwell , Guy Marguerite Marie Gerard Nadler , Neil David Pearson
IPC分类号： A61K31/4375 , C07D471/02
CPC分类号： C07D471/04
摘要： Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
摘要翻译：哌啶衍生物及其药学上可接受的衍生物可用于哺乳动物，特别是人的细菌感染治疗方法。

10. 发明授权

US07491714B2 Quinolines and nitrogenated derivatives thereof and their use as antibacterial agents 失效
标题翻译：喹啉和其氮化衍生物及其作为抗菌剂的用途
公开(公告)号：US07491714B2
公开(公告)日：2009-02-17
申请号：US10537034
申请日：2003-12-03
申请人： Jeffrey Michael Axten , Catherine Genevieve Yvette Dartois , Guy Marguerite Marie Gerard Nadler , Neil David Pearson
发明人： Jeffrey Michael Axten , Catherine Genevieve Yvette Dartois , Guy Marguerite Marie Gerard Nadler , Neil David Pearson
IPC分类号： C07D413/02 , A61K31/421
CPC分类号： C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D513/04
摘要： Quinoline and naphthridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans.
摘要翻译：喹啉和萘啶衍生物可用于治疗哺乳动物，特别是人的细菌感染。

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