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21. 发明授权

US5703240A Piperidine derivatives 失效
标题翻译：哌啶衍生物
公开(公告)号：US5703240A
公开(公告)日：1997-12-30
申请号：US612843
申请日：1996-03-21
申请人： Duncan Robert Armour , Brian Evans , David Middlemiss , Alan Naylor , Neil Anthony Pegg , Maria Victoria Vinader , Gerard Martin Paul Giblin , Tania Hubbard , Michael Menteith Hann , Xiao-Qing Lewell , Stephen Paul Watson
发明人： Duncan Robert Armour , Brian Evans , David Middlemiss , Alan Naylor , Neil Anthony Pegg , Maria Victoria Vinader , Gerard Martin Paul Giblin , Tania Hubbard , Michael Menteith Hann , Xiao-Qing Lewell , Stephen Paul Watson
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4523 , A61K31/454 , A61P1/00 , A61P1/08 , A61P25/04 , A61P29/00 , A61P43/00 , C07D20060101 , C07D211/56 , C07D401/10 , C07D401/12
CPC分类号： C07D401/12
摘要： The present invention relates to piperidine derivatives of formula (I) ##STR1## wherein R.sup.1 is a C.sub.1-4 alkoxy group; R.sup.2 is ##STR2## R.sup.3 is a hydrogen or halogen atom; R.sup.4 and R.sup.5 may each independently represent a hydrogen or halogen atom, or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethyl group; R.sup.6 is a hydrogen atom, a C.sub.1-4 alkyl, (CH.sub.2).sub.m cyclopropyl, --S(O).sub.n C.sub.1-4 alkyl, phenyl, NR.sup.7 R.sup.8, CH.sub.2 C(O)CF.sub.3 or trifluoromethyl group; R.sup.7 and R.sup.8 may each independently represent a hydrogen atom, or a C.sub.1-4 alkyl or acyl group; x represents zero or 1; n represents zero, 1 or 2; m represents zero or 1; and pharmaceutically acceptable salts and solvates thereof; to processes for their preparation; and their use in the treatment of conditions mediated by tachykinins.
摘要翻译： PCT No.PCT / EP94 / 03129 Sec。 371日期1996年3月21日 102（e）1996年3月21日PCT PCT 1994年9月20日PCT公布。第WO95 / 08549号公报日期：1995年3月30日本发明涉及式（I）的哌啶衍生物其中R 1为C 1-4烷氧基; R 2是氢或卤素原子; R 4和R 5可各自独立地表示氢或卤素原子，或C 1-4烷基，C 1-4烷氧基或三氟甲基; R6是氢原子，C1-4烷基，（CH2）环丙基，-S（O）nC1-4烷基，苯基，NR7R8，CH2C（O）CF3或三氟甲基; R 7和R 8可各自独立地表示氢原子或C 1-4烷基或酰基; x表示零或1; n表示0，1或2; m表示0或1; 及其药学上可接受的盐和溶剂合物; 进行准备; 及其用于治疗由速激肽介导的病症。

22. 发明申请

US20060211678A1 Aryl-amino substituted pyrrolopyrimidine multi-kinase inhibiting compounds 失效
标题翻译：芳基 - 氨基取代的吡咯并嘧啶多激酶抑制化合物
公开(公告)号：US20060211678A1
公开(公告)日：2006-09-21
申请号：US11194158
申请日：2005-08-01
申请人： Saleh Ahmed , Oscar Barba , Jason Bloxham , Graham Dawson , Wiliam Gattrell , John Kitchin , Neil Anthony Pegg , Imaad Saba , Shazia Sadiq , Colin Peter Sambrook Smith , Don Smyth , Amo Steing , Robin Wilkes , Bijoy Panicker , Paula Tavares , Matthew Cox , An-Hu Li , Hanqing Dong , Lifu Ma , Kenneth Foreman , Qinghua Weng , Kathryn Stolz
发明人： Saleh Ahmed , Oscar Barba , Jason Bloxham , Graham Dawson , Wiliam Gattrell , John Kitchin , Neil Anthony Pegg , Imaad Saba , Shazia Sadiq , Colin Peter Sambrook Smith , Don Smyth , Amo Steing , Robin Wilkes , Bijoy Panicker , Paula Tavares , Matthew Cox , An-Hu Li , Hanqing Dong , Lifu Ma , Kenneth Foreman , Qinghua Weng , Kathryn Stolz
IPC分类号： A61K31/5377 , A61K31/519 , A61K31/496 , A61K31/4745 , C07D487/02 , C07D471/02
CPC分类号： C07D471/02 , C07D487/02 , C07D487/04
摘要： Compounds represented by Formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, are inhibitors of least two of the Abl, Aurora-A, Blk, c-Raf, cSRC, Src, PRK2, FGFR3, Flt3, Lck, Mek1, PDK-1, GSK3β, EGFR, p70S6K, BMX, SGK, CaMKII, Tie-2, IGF-1R, Ron, Ret, and KDR kinases in animals, including humans, for the treatment and/or prevention of various diseases and conditions such as cancer.
摘要翻译：由式（I）表示的化合物或其立体异构体或其药学上可接受的盐是Abl，Aurora-A，Blk，c-Raf，cSRC，Src，PRK2，FGFR3，Flt3，Lck，Mek1，PDK中的至少两种的抑制剂 -1，GSK3beta，EGFR，p70S6K，BMX，SGK，CaMKII，Tie-2，IGF-1R，Ron，Ret和KDR激酶，用于治疗和/或预防各种疾病和病症，癌症。

23. 发明授权

US07026327B2 Pyrimidine derivatives useful as selective COX-2 inhibitors 失效
公开(公告)号：US07026327B2
公开(公告)日：2006-04-11
申请号：US10477547
申请日：2002-05-23
申请人： Alan Naylor , Jeremy John Payne , Neil Anthony Pegg
发明人： Alan Naylor , Jeremy John Payne , Neil Anthony Pegg
IPC分类号： C07D239/34 , C07D401/12 , A61K31/505
CPC分类号： C07D239/34 , A61K31/505 , C07D401/12
摘要： The invention provides the compounds of formula (I) in which: R1 is selected from the group consisting of H, C1-6alkyl, C1-2alkyl substituted by one to five fluorine atoms, C3-6alkenyl, C3-6alkynyl, C3-10cycloalkylC0-6alkyl, C4-12bridged cycloalkyl, A(CR4R5)n and B(CR4R5)n; R2 is C1-2alkyl substituted by one to five fluorine atoms; R3 is selected from the group consisting of C1-6alkyl, NH2 and R7CONH; R4 and R5 are independently selected from H or C1-6alkyl; A is an unsubstituted 5- or 6-membered heteroaryl or an unsubstituted 6-membered aryl, or a 5- or 6-membered heteroaryl or a 6-membered aryl substituted by one or more R6; R6 is selected from the group consisting of halogen, C1-6alkyl, C1-6alkyl substituted by one more fluorine atoms, C1-6alkoxy, C1-6alkoxy substituted by one or more F, NH2SO2 and C1-6alkylSO2; B is selected from the group consisting of where defines the point of attachment of the ring; R7 is selected from the group consisting of H, C1-6alkyl, C1-6alkoxy, C1-6alkylOC1-6alkyl, phenyl, HO2CC1-6alkyl, C1-6alkylOCOC1-6alkyl, C1-6alkylOCO, H2NC1-6alkyl, C1-6alkylOCONHC1-6alkyl and C1-6alkylCONHC1-6alkyl; and n is 0 to 4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of variety of conditions and diseases.

24. 发明授权

US06780869B1 Pyrimidine derivatives 失效
标题翻译：嘧啶衍生物
公开(公告)号：US06780869B1
公开(公告)日：2004-08-24
申请号：US10130516
申请日：2002-05-16
申请人： Richard Howard Green , Charles David Hartley , Alan Naylor , Jeremy John Payne , Neil Anthony Pegg
发明人： Richard Howard Green , Charles David Hartley , Alan Naylor , Jeremy John Payne , Neil Anthony Pegg
IPC分类号： C07D23942
CPC分类号： C07D239/42
摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof, in which: R1 and R2 are independently selected from H, C1-6 alkyl, C2-6alkenyl, C3-6alkynyl, C3-10cycloalkylC0-6alkyl or C4-12bridged cycloalkane; and R3 is C1-6alkyl or NH2. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of pain, fever, inflammation and a variety of conditions and diseases.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的衍生物，其中：R 1和R 2独立地选自H，C 1-6烷基，C 2-6烯基，C 3-6炔基，C 3-10环烷基C 0 C6烷基或C4-12桥连环烷烃; 和R 3是C 1-6烷基或NH 2。式（I）的化合物是COX-2的有效和选择性抑制剂，并且可用于治疗疼痛，发烧，炎症和多种病症和疾病。

25. 发明授权

US06498166B1 Pyrazolopyridines 失效
标题翻译：吡唑并吡啶类
公开(公告)号：US06498166B1
公开(公告)日：2002-12-24
申请号：US09890925
申请日：2001-08-30
申请人： Ian Baxter Campbell , Paul Francis Lambeth , Alan Naylor , Neil Anthony Pegg
发明人： Ian Baxter Campbell , Paul Francis Lambeth , Alan Naylor , Neil Anthony Pegg
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： The invention provides the compounds of formula (I) wherein: R0 and R1 are independently selected from H, halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms; R2 is halogen, CN, CONR4R5, CO2H, CO2C1-6alkyl, or NHSO2R4; R3 is C1-6alkyl or NH2; and R4 and R5 are independently selected from H, C1-6alkyl, phenyl, phenyl substituted by one or more atoms or groups (selected from halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms), or together with the nitrogen atom to which they are attached form a saturated 4 to 8 membered ring; and pharmaceutically acceptable derivatives thereof. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.
摘要翻译：本发明提供式（I）化合物，其中：R 0和R 1独立地选自H，卤素，C 1-6烷基，C 1-6烷氧基或被一个或多个氟原子取代的C 1-6烷氧基; R 2是卤素，CN，CONR 4 R 5 ，CO 2 H，CO 2 C 1-6烷基或NHSO 2 R 4; R 3是C 1-6烷基或NH 2; R 4和R 5独立地选自H，C 1-6烷基，苯基，被一个或多个原子或基团取代的苯基（选自卤素，C 1-6烷基，C 1-6烷氧基或被一个或多个氟原子取代的C 1-6烷氧基），或与它们所连接的氮原子一起形成饱和的4至8元环; 其药学上可接受的衍生物。式（I）化合物是COX-2的有效和选择性抑制剂，可用于治疗疼痛，发热，多种病症和疾病的炎症。

26. 发明授权

US5843966A Piperidine derivatives 失效
标题翻译：哌啶衍生物
公开(公告)号：US5843966A
公开(公告)日：1998-12-01
申请号：US899190
申请日：1997-07-23
申请人： Duncan Robert Armour , Brian Evans , David Middlemiss , Tania Hubbard , Michael Menteith Hann , Xiao-Qing Lewell , Stephen Paul Watson , Alan Naylor , Neil Anthony Pegg , Maria Victoria Vinader , Gerard Martin Paul Giblin
发明人： Duncan Robert Armour , Brian Evans , David Middlemiss , Tania Hubbard , Michael Menteith Hann , Xiao-Qing Lewell , Stephen Paul Watson , Alan Naylor , Neil Anthony Pegg , Maria Victoria Vinader , Gerard Martin Paul Giblin
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4523 , A61K31/454 , A61P1/00 , A61P1/08 , A61P25/04 , A61P29/00 , A61P43/00 , C07D20060101 , C07D211/56 , C07D401/10 , C07D401/12
CPC分类号： C07D401/12
摘要： The present invention relates to piperidine derivatives of formula (I) ##STR1## wherein R.sup.1 is a C.sub.1-4 alkoxy group; R.sup.2 is ##STR2## R.sup.3 is a hydrogen or halogen atom; R.sup.4 and R.sup.5 may each independently represent a hydrogen or halogen atom, or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethyl group; R.sup.6 is a hydrogen atom, a C.sub.1-4 alkyl, (CH.sub.2).sub.m cyclopropyl, --S(O).sub.n C.sub.1-4 alkyl, phenyl, NR.sup.7 R.sub.8, CH.sub.2 C(O)CF.sub.3 or trifluoromethyl group; R.sup.7 and R.sup.8 may each independently represent a hydrogen atom, or a C.sub.1-4 alkyl or acyl group; x represents zero or 1; n represents zero, 1 or 2; m represents zero or 1; and pharmaceutically acceptable salts and solvates thereof; to processes for their preparation; and their use in the treatment of conditions mediated by tachykinins.
摘要翻译：本发明涉及式（I）的哌啶衍生物其中R 1为C 1-4烷氧基; R 2是氢或卤素原子; R 4和R 5可各自独立地表示氢或卤素原子，或C 1-4烷基，C 1-4烷氧基或三氟甲基; R6是氢原子，C1-4烷基，（CH2）环丙基，-S（O）nC1-4烷基，苯基，NR7R8，CH2C（O）CF3或三氟甲基; R 7和R 8可各自独立地表示氢原子或C 1-4烷基或酰基; x表示零或1; n表示0，1或2; m表示0或1; 及其药学上可接受的盐和溶剂合物; 进行准备; 及其用于治疗由速激肽介导的病症。

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