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公开(公告)号：US20080275053A1
公开(公告)日：2008-11-06
申请号：US10575072
申请日：2004-10-06
申请人： Gerard Martin Paul Giblin , Adrian Hall , Ian Reginald Kilford , Xiao Qing Lewell , Neil Derek Miller , Alan Naylor
发明人： Gerard Martin Paul Giblin , Adrian Hall , Ian Reginald Kilford , Xiao Qing Lewell , Neil Derek Miller , Alan Naylor
IPC分类号： A61K31/4965 , A61P25/00 , A61P29/00 , A61P37/00 , C07D207/337 , C07D231/12 , C07D241/12 , A61K31/4418 , A61K31/4439 , A61K31/365 , C07D307/58 , C07D213/55 , C07D471/04 , A61K31/40 , A61K31/415
CPC分类号： C07D207/337 , C07D213/55 , C07D213/56 , C07D231/12 , C07D241/12 , C07D307/46 , C07D401/04
摘要： Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, B, D, Z, R1, R2a, R2b, and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译： 式（I）化合物或其药学上可接受的衍生物：其中A，B，D，Z，R 1，R 2a，R 2b， >和R x x如本说明书中所定义，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。
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公开(公告)号：US07446222B2
公开(公告)日：2008-11-04
申请号：US10533036
申请日：2003-10-30
申请人： Rino Antonio Bit , Gerard Martin Paul Giblin , Adrian Hall , David Nigel Hurst , Ian Reginald Kilford , Neil Derek Miller , Tiziana Scoccitti
发明人： Rino Antonio Bit , Gerard Martin Paul Giblin , Adrian Hall , David Nigel Hurst , Ian Reginald Kilford , Neil Derek Miller , Tiziana Scoccitti
IPC分类号： C07C63/331 , C07C63/33 , C07C233/54 , C07C229/64 , C07D257/06 , C07D213/30
CPC分类号： C07D333/38 , C07C65/03 , C07C65/24 , C07C69/734 , C07C69/94 , C07C229/64 , C07C233/54 , C07C235/42 , C07C311/08 , C07C311/51 , C07D211/60 , C07D211/62 , C07D213/30 , C07D213/38 , C07D213/61 , C07D213/64 , C07D213/79 , C07D213/80 , C07D241/24 , C07D241/26 , C07D257/04 , C07D261/18 , C07D333/16
摘要： Compounds of formula (I) or derivatives thereof: wherein A, B, Z, R1, R2a, R2b, Rx, R8, and R9 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译： 式（I）化合物或其衍生物：其中A，B，Z，R 1，R 2a，R 2b，R SUP R 8，R 8和R 9如说明书中所定义，制备这些化合物的方法，包含这些化合物的药物组合物和 在药物中使用这些化合物。
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公开(公告)号：US20090030061A1
公开(公告)日：2009-01-29
申请号：US12278979
申请日：2007-02-12
IPC分类号： A61K31/403 , C07D209/62 , A61P29/00
CPC分类号： C07D209/66 , C07D209/64
摘要： A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein R1 to R8, X, and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
摘要翻译： 式（I）化合物或其药学上可接受的衍生物，其中R 1至R 8，X和Y如说明书中所定义; 制备这种化合物的方法; 包含这些化合物的药物组合物; 并在药物中使用这些化合物。
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公开(公告)号：US20080234358A1
公开(公告)日：2008-09-25
申请号：US12111989
申请日：2008-04-30
申请人： Miles Stuart Congreve , Gerard Martin, Paul Giblin , Andrew McMurtrie Mason , Neil Derek Miller , Susan Roomans , Ann Louise Walker
发明人： Miles Stuart Congreve , Gerard Martin, Paul Giblin , Andrew McMurtrie Mason , Neil Derek Miller , Susan Roomans , Ann Louise Walker
IPC分类号： A61K31/4035 , C07D209/44 , A61P29/00
CPC分类号： C07D209/66 , C07D209/64
摘要： A compound of formula (I) wherein R1 and R3 are the same or different and represent ═O, hydrogen, C1-6alkyl, C1-6dialkyl, ═CHC1-C5alkyl, ═S, or a 5- or 6-membered aryl; R4 to R9 are the same or different and represent hydrogen, C1-6alkoxy, OCF3, OCH2CF3, O-cyclopropyl, OCH2-cyclopropyl, C1-C6alkyl, S-alkyl, NR210 where R10 is hydrogen or C1-6alkyl, halogen, NO2, OH, CH2OC1-C6alkyl, CH2OH, or CF3; Q1 is hydrogen, C1-6alkyl, C1-6dialkyl, C1-6alkoxy, NHAc, NR210 where R10 is hydrogen or C1-6alkyl, difluoro, fluoro, ═O, or OH; Q2, Q3, Q4 and Q5 are the same or different and represent hydrogen, C1-6alkoxy, OCF3, OCH2CF3, O-cyclopropyl, OCH2-cyclopropyl, C1-C6alkyl, S-alkyl, NR210 where R10 is hydrogen or C1-6alkyl, halogen, NO2, OH, CH2OC1-C6alkyl, CH2OH, or a 5- or 6-membered aryl; with the proviso that the compounds [4-(1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]-2-propionic acid, sodium salt and [4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetic acid are excluded; and pharmaceutically acceptable derivatives thereof.
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公开(公告)号：US07732622B2
公开(公告)日：2010-06-08
申请号：US12111989
申请日：2008-04-30
申请人： Miles Stuart Congreve , Gerard Martin Paul Giblin , Andrew McMurtrie Mason , Neil Derek Miller , Susan Roomans , Ann Louise Walker
发明人： Miles Stuart Congreve , Gerard Martin Paul Giblin , Andrew McMurtrie Mason , Neil Derek Miller , Susan Roomans , Ann Louise Walker
IPC分类号： C07D209/60 , A61K31/40
CPC分类号： C07D209/66 , C07D209/64
摘要： A compound of formula (I) wherein R1 and R3 are the same or different and represent ═O, hydrogen, C1-6alkyl, C1-6dialkyl, ═CHC1-C5alkyl, ═S, or a 5- or 6-membered aryl; R4 to R9 are the same or different and represent hydrogen, C1-6alkoxy, OCF3, OCH2CF3, O-cyclopropyl, OCH2-cyclopropyl, C1-C6alkyl, S-alkyl, NR210 where R10 is hydrogen or C1-6alkyl, halogen, NO2, OH, CH2OC1-C6alkyl, CH2OH, or CF3; Q1 is hydrogen, C1-6alkyl, C1-6dialkyl, C1-6alkoxy, NHAc, NR210 where R10 is hydrogen or C1-6alkyl, difluoro, fluoro, ═O, or OH; Q2, Q3, Q4 and Q5 are the same or different and represent hydrogen, C1-6alkoxy, OCF3, OCH2CF3, O-cyclopropyl, OCH2-cyclopropyl, C1-C6alkyl, S-alkyl, NR210 where R10 is hydrogen or C1-6alkyl, halogen, NO2, OH, CH2OC1-C6alkyl, CH2OH, or a 5- or 6-membered aryl; with the proviso that the compounds [4-(1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]-2-propionic acid, sodium salt and [4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetic acid are excluded; and pharmaceutically acceptable derivatives thereof.
摘要翻译： 式（I）的化合物，其中R 1和R 3相同或不同并且表示≡O，氢，C 1-6烷基，C 1-6二烷基，= CHCl-C 5烷基，= S或5或6元芳基; R4至R9相同或不同，表示氢，C1-6烷氧基，OCF3，OCH2CF3，O-环丙基，OCH2-环丙基，C1-C6烷基，S-烷基，NR210，其中R10为氢或C1-6烷基，卤素， OH，CH 2 OC 1 -C 6烷基，CH 2 OH或CF 3; Q1是氢，C1-6烷基，C1-6二烷基，C1-6烷氧基，NHAc，NR210，其中R10是氢或C1-6烷基，二氟，氟，= O或OH; Q2，Q3，Q4和Q5相同或不同，表示氢，C1-6烷氧基，OCF3，OCH2CF3，O-环丙基，OCH2-环丙基，C1-C6烷基，S-烷基，NR210，其中R10是氢或C1-6烷基， 卤素，NO 2，OH，CH 2 OC 1 -C 6烷基，CH 2 OH或5或6元芳基; 条件是化合物[4-（1-氧代-1,3-二氢-2H-苯并[f]异吲哚-2-基）苯基] -2-丙酸钠盐和[4-（4,9 - 二乙氧基-1-氧代-1,3-二氢-2H-苯并[f]异吲哚-2-基）苯基]乙酸; 和它们的药用衍生物。
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公开(公告)号：US06924297B2
公开(公告)日：2005-08-02
申请号：US10450891
申请日：2001-12-20
申请人： Gerard Martin Paul Giblin , Haydn Terence Jones , Andrew McMurtrie Mason , Neil Derek Miller , Susan Roomans , Stephen Edward Shanahan , Ann Louise Walker
发明人： Gerard Martin Paul Giblin , Haydn Terence Jones , Andrew McMurtrie Mason , Neil Derek Miller , Susan Roomans , Stephen Edward Shanahan , Ann Louise Walker
IPC分类号： C07D401/12 , A61K31/403 , A61K31/42 , A61K31/427 , A61K31/4439 , A61P1/00 , A61P1/02 , A61P1/04 , A61P1/12 , A61P1/16 , A61P3/00 , A61P3/02 , A61P3/10 , A61P3/14 , A61P5/10 , A61P5/18 , A61P7/02 , A61P7/06 , A61P7/12 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/04 , A61P13/12 , A61P15/10 , A61P17/00 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/04 , A61P19/06 , A61P19/08 , A61P19/10 , A61P21/00 , A61P21/04 , A61P25/02 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P27/02 , A61P27/06 , A61P27/14 , A61P29/00 , A61P31/00 , A61P31/12 , A61P31/16 , A61P31/18 , A61P35/00 , A61P37/06 , A61P39/02 , A61P43/00 , C07D209/64 , C07D209/66 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D209/60
CPC分类号： C07D209/64 , C07D209/66
摘要： Compounds of formula (I) and pharmaceutically acceptable derivatives thereof bind with high affinity to the EP4 receptor and are of use in the treatment or prevention of conditions such as a pain, inflammatory, immunological, bone, neurodegenerative or renal disorder.
摘要翻译： 式（I）化合物及其药学上可接受的衍生物以高亲和力结合EP4受体，并且可用于治疗或预防诸如疼痛，炎症，免疫学，骨骼，神经变性或肾脏疾病的病症。
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7.发明申请Quinoline Compounds Capable of Binding the Cb2 and/or the 5-Ht6 Receptor 审中-公开能够结合Cb2和/或5-Ht6受体的喹啉化合物公开(公告)号：US20090012056A1
公开(公告)日：2009-01-08
申请号：US12088502
申请日：2006-09-26
申请人： Mahmood Ahmed , Gerard Martin Paul Giblin , Christopher Norbert Johnson , David George Hubert Livermore , Neil Derek Miller , Stephen Frederick Moss , David R. Witty
发明人： Mahmood Ahmed , Gerard Martin Paul Giblin , Christopher Norbert Johnson , David George Hubert Livermore , Neil Derek Miller , Stephen Frederick Moss , David R. Witty
IPC分类号： A61K31/4709 , C07D401/10 , A61P25/24
CPC分类号： C07D491/10 , C07D215/36 , C07D401/06
摘要： The present invention relates to novel quinoline derivatives such as compounds of the formula (I) which possess antagonist potency for the 5-HT6 receptor and/or are capable of selectively modulating the cannabinoid 2 receptor: and the use of such compounds or pharmaceutical compositions thereof in the treatment of CNS disorders.
摘要翻译： 本发明涉及新颖的喹啉衍生物，例如具有5-HT 6受体的拮抗剂效能和/或能够选择性调节大麻素2受体的式（I）化合物，以及这些化合物或其药物组合物的用途 在治疗中枢神经系统疾病。
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公开(公告)号：US07718689B2
公开(公告)日：2010-05-18
申请号：US12278979
申请日：2007-02-12
IPC分类号： A61K31/4035 , C07D209/60
CPC分类号： C07D209/66 , C07D209/64
摘要： A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein R1 to R8, X, and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
摘要翻译： 式（I）化合物或其药学上可接受的衍生物，其中R 1至R 8，X和Y如说明书中所定义; 制备这种化合物的方法; 包含这些化合物的药物组合物; 并在药物中使用这些化合物。
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公开(公告)号：US07514437B2
公开(公告)日：2009-04-07
申请号：US10499177
申请日：2002-12-20
申请人： Alan David Borthwick , Richard Jonathan Hatley , Deirdre Mary Bernadette Hickey , John Liddle , David George Hubert Livermore , Andrew McMurtrie Mason , Neil Derek Miller , Fabrizio Nerozzi , Steven Leslie Sollis , Anna Katrin Szardenings , Paul Graham Wyatt
发明人： Alan David Borthwick , Richard Jonathan Hatley , Deirdre Mary Bernadette Hickey , John Liddle , David George Hubert Livermore , Andrew McMurtrie Mason , Neil Derek Miller , Fabrizio Nerozzi , Steven Leslie Sollis , Anna Katrin Szardenings , Paul Graham Wyatt
IPC分类号： A61K31/497 , A61K31/4965 , C07D241/00 , C07D241/02
CPC分类号： C07D241/08 , A61K38/00 , C07D401/10 , C07D403/06 , C07D413/10 , C07D417/06 , C07K5/06078 , C07K5/06191
摘要： A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a mammal in need thereof of an effective amount of a compound of the formula (I) and/or a physiologically acceptable derivative thereof, wherein the substituents have the meaning given in the description. Disclosed are also novel compounds of formula (I) and processes for their preparation.
摘要翻译： 一种治疗或预防通过催产素作用介导的疾病或病症的方法，其包括向有需要的哺乳动物施用有效量的式（I）化合物和/或其生理上可接受的衍生物，其中所述取代基具有 说明中给出的含义。 公开了式（I）的新化合物及其制备方法。
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10.发明申请5-Sulfonyl-1-Piperidinyl Substituted Indole Derivatives as 5-Ht6 Receptor Antagonists for the Treatment of Cns Disorders 审中-公开5-磺基-1-哌啶基取代的吲哚衍生物作为治疗Cns病的5-Ht6受体拮抗剂公开(公告)号：US20080318933A1
公开(公告)日：2008-12-25
申请号：US11576070
申请日：2005-10-05
申请人： Mahmood Ahmed , Christopher Norbert Johnson , Neil Derek Miller , Peter Henry Milner , Dean Andrew Rivers , David R Witty
发明人： Mahmood Ahmed , Christopher Norbert Johnson , Neil Derek Miller , Peter Henry Milner , Dean Andrew Rivers , David R Witty
IPC分类号： A61K31/55 , C07D401/04 , A61K31/454 , A61P3/00 , A61P25/00 , C07D403/04 , A61K31/403
CPC分类号： C07D401/14 , C07D401/04 , C07D417/14
摘要： The present invention relates to novel indole derivatives such as compounds of the formula (I): which possess antagonist potency at the 5-HT6 receptor and the use of such compounds or pharmaceutically acceptable salts or solvates thereof in the treatment of Alzheimer's disease and other CNS disorders.
摘要翻译： 本发明涉及新的吲哚衍生物，例如式（I）的化合物：其具有5-HT 6受体的拮抗剂效力，以及这些化合物或其药学上可接受的盐或溶剂化物在治疗阿尔茨海默病和其它CNS中的用途 疾病
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