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公开(公告)号:US20050085414A1
公开(公告)日:2005-04-21
申请号:US10990462
申请日:2004-11-18
申请人: Russell Hagan , Keith Bunce , Alan Naylor , Mark Ladlow , Andrew McElroy , Andrew Whittington , Barry Coomber
发明人: Russell Hagan , Keith Bunce , Alan Naylor , Mark Ladlow , Andrew McElroy , Andrew Whittington , Barry Coomber
IPC分类号: A61K31/40 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/57 , A61K38/00 , A61K45/06 , A61P1/08 , A61P25/24 , A61P43/00 , C07D453/02 , C07D487/08 , A61K38/16 , A61K31/573 , A61K31/557 , A61K31/7072 , A61K31/4184
CPC分类号: C07D487/08 , A61K31/44 , A61K31/445 , A61K31/57 , A61K45/06 , Y10S514/872 , A61K31/435 , A61K31/415 , A61K31/165 , A61K2300/00
摘要: The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. wherein R represents the ring A or 2-pyridinyl or 2-pyridinyl-N-oxide; R1 is selected from halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl, and S(O)nC1-4alkyl groups; R2 and R3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C1-4alkyl, C1-4alkoxy, trifluoromethyl and cyano groups; n represents zero, 1 or 2; and pharmaceutically acceptable salts and solvates thereof.
摘要翻译: 本发明涉及速激肽拮抗剂(包括P物质拮抗剂和其他神经激肽拮抗剂)在治疗呕吐中的用途。 还描述了式(I)的新型速激肽拮抗剂,其制备方法,含有它们的药物组合物及其医疗用途。 其中R表示环A或2-吡啶基或2-吡啶基-N-氧化物; R 1选自卤素原子和C 1-4烷基,C 1-4烷氧基,三氟甲基和S(O) C 1-4烷基; R 2和R 3可以相同或不同,各自独立地选自氢和卤素原子和C 1-4烷基 C 1-4烷氧基,三氟甲基和氰基; n表示0,1或2; 及其药学上可接受的盐和溶剂化物。
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公开(公告)号:US5360820A
公开(公告)日:1994-11-01
申请号:US946635
申请日:1992-09-18
申请人: Russell M. Hagan , Keith T. Bunce , Alan Naylor , Mark Ladlow , Andrew B. McElroy , Andrew R. Whittington , Barry A. Coomber
发明人: Russell M. Hagan , Keith T. Bunce , Alan Naylor , Mark Ladlow , Andrew B. McElroy , Andrew R. Whittington , Barry A. Coomber
IPC分类号: A61K31/40 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/57 , A61K38/00 , A61K45/06 , A61P1/08 , A61P25/24 , A61P43/00 , C07D453/02 , C07D487/08 , A61K31/20 , A61K31/55 , A61K31/135 , A61K31/19
CPC分类号: C07D487/08 , A61K31/44 , A61K31/445 , A61K31/57 , A61K45/06 , Y10S514/872
摘要: The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. ##STR1## wherein R represents the ring A ##STR2## or 2-pyridinyl or 2-pyridinyl-N-oxide; R.sup.1 is selected from halogen atoms and C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, and S(O).sub.n C.sub.1-4 alkyl groups;R.sup.2 and R.sup.3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl and cyano groups;n represents zero, 1 or 2;and pharmaceutically acceptable salts and solvates thereof.
摘要翻译: 本发明涉及速激肽拮抗剂(包括P物质拮抗剂和其他神经激肽拮抗剂)在治疗呕吐中的用途。 还描述了式(I)的新型速激肽拮抗剂,其制备方法,含有它们的药物组合物及其医疗用途。 (I)其中R表示环A或2-吡啶基或2-吡啶基-N-氧化物; R 1选自卤素原子和C 1-4烷基,C 1-4烷氧基,三氟甲基和S(O)n C 1-4烷基; R 2和R 3可以相同或不同,各自独立地选自氢和卤素原子和C 1-4烷基,C 1-4烷氧基,三氟甲基和氰基; n表示0,1或2; 及其药学上可接受的盐和溶剂化物。
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公开(公告)号:US20070129367A1
公开(公告)日:2007-06-07
申请号:US10528592
申请日:2003-09-25
申请人: Andrew Eatherton , Gerard Giblin , Richard Green , Jennifer Doughty , Karamjit Jandu , William Mitchell , Alan Naylor , Giovanni Palombi , Derek Rawlings , Brian Slingsby , Andrew Whittington
发明人: Andrew Eatherton , Gerard Giblin , Richard Green , Jennifer Doughty , Karamjit Jandu , William Mitchell , Alan Naylor , Giovanni Palombi , Derek Rawlings , Brian Slingsby , Andrew Whittington
IPC分类号: A61K31/53 , A61K31/501 , A61K31/506 , A61K31/497 , A61K31/4439 , C07D417/02 , C07D413/02 , C07D403/02 , C07D401/02
CPC分类号: C07D213/82 , C07D401/12 , C07D413/12
摘要: The present invention relates to novel pyridine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor.
摘要翻译: 本发明涉及新颖的吡啶衍生物,含有这些化合物的药物组合物及其在治疗疾病尤其是疼痛中的用途,该疾病通过大麻素受体的活性的增加或减少直接或间接引起。
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公开(公告)号:US20060247261A1
公开(公告)日:2006-11-02
申请号:US10524469
申请日:2003-08-19
申请人: Andrew Eatherton , Gerard Giblin , Richard Green , Jennifer Doughty , William Mitchell , Alan Naylor , Derek Rawlings , Brian Slingsby , Andrew Whittington
发明人: Andrew Eatherton , Gerard Giblin , Richard Green , Jennifer Doughty , William Mitchell , Alan Naylor , Derek Rawlings , Brian Slingsby , Andrew Whittington
IPC分类号: A61K31/506 , A61K31/505 , C07D403/02
CPC分类号: C07D239/42 , C07D401/12
摘要: The present invention relates to novel pyrimidine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor.
摘要翻译: 本发明涉及新颖的嘧啶衍生物,含有这些化合物的药物组合物及其在治疗疾病尤其是疼痛中的用途,该疾病是由大麻素受体的活性的增加或减少直接或间接引起的。
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公开(公告)号:US20060240048A1
公开(公告)日:2006-10-26
申请号:US10528613
申请日:2003-09-25
申请人: Andrew Eatherton , Gerard Martin Giblin , Richard Green , Jennifer Doughty , Karamjit Jandu , William Mitchell , Alan Naylor , Giovanni Palombi , Derek Rawlings , Brian Slingsby , Andrew Whittington
发明人: Andrew Eatherton , Gerard Martin Giblin , Richard Green , Jennifer Doughty , Karamjit Jandu , William Mitchell , Alan Naylor , Giovanni Palombi , Derek Rawlings , Brian Slingsby , Andrew Whittington
IPC分类号: A61K47/00
CPC分类号: C07D213/82 , C07D401/06 , C07D403/06 , C07D405/12 , C07D409/12
摘要: The present invention relates to novel pyridine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor.
摘要翻译: 本发明涉及新颖的吡啶衍生物,含有这些化合物的药物组合物及其在治疗疾病尤其是疼痛中的用途,所述疾病通过大麻素受体的活性的增加或减少而直接或间接引起。
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公开(公告)号:US20080280868A1
公开(公告)日:2008-11-13
申请号:US10597524
申请日:2005-02-22
IPC分类号: A61K31/4418 , C07D213/74 , C07D401/04 , A61P29/00 , A61P37/00
CPC分类号: C07D213/74 , C07D401/06 , C07D405/12 , C07D409/12
摘要: The present invention relates to novel pyridine derivatives such as compounds of the formula (I): and the use of such compounds or pharmaceutical compositions thereof in the treatment of diseases, particularly pain, which are mediated by the activity of the cannabinoid 2 receptor.
摘要翻译: 本发明涉及新的吡啶衍生物,例如式(I)的化合物:以及这些化合物或其药物组合物在治疗由大麻素2受体的活性介导的疾病,特别是疼痛中的用途。
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公开(公告)号:US20050282845A1
公开(公告)日:2005-12-22
申请号:US11165073
申请日:2005-06-23
申请人: Malcolm Carter , Alan Naylor , Martin Pass , Jeremy Payne , Neil Pegg
发明人: Malcolm Carter , Alan Naylor , Martin Pass , Jeremy Payne , Neil Pegg
IPC分类号: A61K31/506 , A61P29/00 , A61P43/00 , C07D405/12
CPC分类号: C07D405/12
摘要: Methods for the treatment of pain, fever, inflammation of a variety of conditions and diseases.
摘要翻译: 治疗疼痛,发烧,炎症的各种病症和疾病的方法。
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公开(公告)号:US20050032823A1
公开(公告)日:2005-02-10
申请号:US10477819
申请日:2002-05-23
申请人: Richard Doughty , Jennifer Doughty Green , Charles Hartley , Alan Naylor , Jeremy Payne , Neil Pegg
发明人: Richard Doughty , Jennifer Doughty Green , Charles Hartley , Alan Naylor , Jeremy Payne , Neil Pegg
IPC分类号: A61K31/505 , A61P1/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P9/00 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/06 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P29/00 , A61P31/12 , A61P31/16 , A61P35/00 , A61P43/00 , C07D239/42 , C07D239/02
CPC分类号: C07D239/42
摘要: The invention thus provides the compounds of formula (I) and pharmaceutically acceptable salts thereof, in which: R1 and R2 are independently selected from the group consisting of H, C1-6alkyl, C2-6alkenyl, C3-4alkynyl, C3-10cycloalkylC0-6alkyl and C4-12bridged cycloalkyl; R3 is selected from the group consisting of C1-6alkyl, NH2 and R5CONH; R4 is selected from the group consisting of CH2F, CHF2, CF3CH2, CF3CHF and CF3CF2; and R5 is selected from the group consisting of H, C1-6alkyl, C1-6alkoxy, C1-6alkylOC1-6alkyl, phenyl, HO 2cc1-6?alkyl, C1-6alkylOCOC1-6alkyl, C1-4alkylOCO, H2NC1-6alkyl, C1-6alkylOCONHC1-6alkyl and C1-6alkylCONHC1-6alkyl. 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: 因此,本发明提供式(I)化合物及其药学上可接受的盐,其中:R 1和R 2独立地选自H,C 1-6烷基,C 2-6烯基,C 3-4炔基 ,C 3-10环烷基C 1-6烷基和C 4-12桥环烷基; R 3选自C 1-6烷基,NH 2和R 5 CONH; R 4选自CH 2 F,CHF 2,CF 3 CH 2,CF 3 CHF和CF 3 CF 2; 并且R 5选自H,C 1-6烷基,C 1-6烷氧基,C 1-6烷基C 1-6烷基,苯基,HO
2 C 1-6烷基,C 1-6烷基COC 1-6烷基,C 1-4烷基COO,H 2 NC 1-6烷基,C 1-6烷基OCONHC 1-6烷基和C 1-6烷基CONHC -6-烷基。 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,各种病症和疾病的炎症。 -
公开(公告)号:US06780870B2
公开(公告)日:2004-08-24
申请号:US10182788
申请日:2002-07-31
IPC分类号: C07D23942
CPC分类号: C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
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, or C1-6alkyl; R3 is C1-6alkyl or NH2; R4 is H or C1-6alkyl; A is a 5- or 6-membered aryl, or a 5- or 6-membered aryl substituted by one or more R5; R5 is halogen, C1-6alkyl, C1-6alkyl substituted by one ore more F, C1-6alkoxy, C1-6alkoxy substituted by one or more F, SO2NH2 or SO2C1-6alkyl; and n is 1 to 4.
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或C 1-6烷基; R 3是C 1-6烷基或NH 2; R 4是H或C 1-6烷基; A是5或6元芳基或被一个或多个R 5取代的5或6元芳基; R 5是卤素,C 1 -C 6烷基, 被一个或多个F,C 1-6烷氧基,被一个或多个F,SO 2 NH 2或SO 2 C 1-6烷基取代的C 1-6烷氧基取代的C 1-6烷基; andn是1到4。
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公开(公告)号:US5023255A
公开(公告)日:1991-06-11
申请号:US493250
申请日:1990-03-14
IPC分类号: C12N9/99 , A61K31/53 , A61P29/00 , A61P37/08 , A61P43/00 , C07C281/02 , C07C281/06 , C07D233/64 , C07D253/06 , C07D281/02 , C07D401/12 , C07D413/12 , C07D417/12
CPC分类号: C07D253/06
摘要: Triazine derivatives of formula (I) ##STR1## or salts thereof, whereinR.sup.1 represents a halogen atom or a group selected from hydroxy; C.sub.1-8 alkyl C.sub.1-6 alkoxy; C.sub.1-3 alkoxy C.sub.1-3 alkoxy; phenoxy or phenyl C.sub.1-3 alkoxy, wherein the phenyl group is optionally substituted by a halogen atom or a group selected from C.sub.1-3 alkyl, C.sub.1-3 alkoxy, or hydroxy; fluoro C.sub.1-3 alkyl; cyano; --CO.sub.2 R.sup.3, wherein R.sup.3 represents a hydrogen atom or a C.sub.1-4 alkyl group; --CONR.sup.4 R.sup.5, wherein R.sup.4 and R.sup.5 each independently represents a hydrogen atom or a C.sub.1-4 alkyl group, or, together with the nitrogen atom to which they are attached, form a saturated 5- to 7- membered ring, which ring optionally contains one or more atoms selected from an oxygen or a sulphur atom, or a group selected from --NH-- or --N(CH.sub.3)--; andR.sup.2 represents a hydrogen or halogen atom, or a group selected from hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;are inhibitors of the enzyme 5-lipoxygenase.Processes for preparing the triazine derivatives of formula (I) and compositions containing them are also described.
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