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51. 发明申请

US20050192306A1 Pyrimidine derivatives as selective inhibitors of COX-2 审中-公开
标题翻译：嘧啶衍生物作为COX-2的选择性抑制剂
公开(公告)号：US20050192306A1
公开(公告)日：2005-09-01
申请号：US11119653
申请日：2005-05-02
申请人： Jennifer Doughty , Richard Green , Charles Hartley , Alan Naylor , Jeremy Payne , Neil Pegg
发明人： Jennifer Doughty , Richard 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
CPC分类号： C07D239/42
摘要： Methods of treating a subject suffering from a condition which is mediated by COX-2.
摘要翻译：治疗患有COX-2介导的病症的受试者的方法。

52. 发明授权

US06451794B1 2,3-Diaryl-pyrazolo[1,5-b]pyridazines derivatives, their preparation and their use as cyclooxygenase 2(COX-2) inhibitors 失效
标题翻译： 2,3-二芳基 - 吡唑并[1,5-b]哒嗪衍生物，其制备及其作为环氧合酶2（COX-2）抑制剂的用途
公开(公告)号：US06451794B1
公开(公告)日：2002-09-17
申请号：US09508029
申请日：2000-06-13
申请人： Paul John Beswick , Ian Baxter Campbell , Neil Mathews , Alan Naylor
发明人： Paul John Beswick , Ian Baxter Campbell , Neil Mathews , Alan Naylor
IPC分类号： A61K314985
CPC分类号： C07D487/04 , A61K31/50 , Y02P20/55
摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof in which: R0 is halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxy substituted by one or more fluorine atoms, or O(CH2)nNR4R5; R1 and R2 are independently selected from H, C1-6alkyl, C1-6alkyl, substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5, (CH2)nSC1-6alkyl or C(O)NR4R5; with the proviso that when R0 is at the 4-position and is halogen, at least one of R1 and R2 is C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5 or (CH2)nSC1-6alkyl, C(O)NR4R5; R3 is C1-6alkyl or NH2; R4 and R5 are independently selected from H, or C1-6alkyl or, together with the nitrogen atom to which they are attached, form a 4-8 membered saturated ring; and n is 1-4. 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）化合物及其药学上可接受的衍生物，其中：R 0是卤素，C 1-6烷基，C 1-6烷氧基，被一个或多个氟原子取代的C 1-6烷氧基或O（CH 2）n NR 4 R 5; R 1和R 2独立地选自被一个或多个氟原子取代的H，C 1-6烷基，C 1-6烷基，C 1-6烷氧基，C 1-6羟烷基，SC 1-6烷基，C（O）H，C（O）C 1-6烷基（C 1-6烷基磺酰基），被一个或多个氟原子取代的C 1-6烷氧基，O（CH 2）n CO 2 C 1-6烷基，O（CH 2）nSC 1-6烷基，（CH 2）n NR 4 R 5，（CH 2）nSC 1-6烷基或C（O）NR 4 R 5; 条件是当R 0在4-位且是卤素时，R 1和R 2中的至少一个是C 1-6烷基磺酰基，被一个或多个氟原子取代的C 1-6烷氧基，O（CH 2）n CO 2 C 1-6烷基，O（CH 2））nSC1-6烷基，（CH2）nNR4R5或（CH2）nSC1-6烷基，C（O）NR4R5; R3是C1-6烷基或NH2; R 4和R 5独立地选自H或C 1-6烷基，或与它们所连接的氮原子一起形成4-8元饱和环; n为1-4。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。

53. 发明授权

US5243076A Phenethanolamine derivatives 失效
标题翻译：苯乙醇胺衍生物
公开(公告)号：US5243076A
公开(公告)日：1993-09-07
申请号：US810183
申请日：1991-12-19
申请人： Ian F. Skidmore , Lawrence H. C. Lunts , Harry Finch , Alan Naylor
发明人： Ian F. Skidmore , Lawrence H. C. Lunts , Harry Finch , Alan Naylor
IPC分类号： C07C217/48 , A61K31/135 , A61K31/335 , A61K31/357 , A61K31/36 , A61P11/00 , A61P25/02 , C07C33/46 , C07C43/174 , C07C43/178 , C07C43/225 , C07C45/00 , C07C45/30 , C07C47/277 , C07C49/255 , C07C59/13 , C07C59/66 , C07C67/00 , C07C213/00 , C07C213/02 , C07C217/10 , C07C217/14 , C07C217/28 , C07C217/64 , C07C229/38 , C07D303/40 , C07D309/12 , C07D309/18 , C07D317/54 , C07D317/58 , C07D319/06 , C07D319/08 , C07D319/18
CPC分类号： C07C45/004 , C07C229/38 , C07C309/00 , C07C33/46 , C07C43/174 , C07C43/1742 , C07C43/1782 , C07C43/225 , C07C45/30 , C07C47/277 , C07C49/255 , C07C59/66 , C07D303/40 , C07D309/12 , C07D317/54 , C07D319/06 , Y02P20/55 , Y10S514/826 , Y10S514/863 , Y10S514/886 , Y10S514/887 , Y10S514/906 , Y10S514/913 , Y10S514/925 , Y10S514/926 , Y10S514/927 , Y10S514/928
摘要： Phenethanolamine derivatives are disclosed of formula ##STR1## wherein m is 2 to 8; n is 1 to 7 provided that m+n is 4 to 12;Ar is phenyl or phenyl substituted by one or two halogen atoms, alkyl or alkoxy groups or by an alkylenedioxy group;R.sup.1 and R.sup.2 are hydrogen or alkyl provided that the sum total of carbon atoms in R.sup.1 and R.sup.2 is not more than 4;and the physiologically acceptable salts and solvates thereof.The compounds have a selective stimulant action at .beta..sub.2 -adrenoreceptors and may be used inter alia in the treatment of diseases associated with reversible airways obstructions such as asthma and chronic bronchitis. The compounds may be formulated in conventional manner as pharmaceutical compositions with physiologically acceptable carriers or excipients.The compounds may be prepared, for example by alkylation of an amine: ##STR2## where R.sup.3, R.sup.5 and R.sup.6 is hydrogen or a protecting group, followed by removal of any protecting group.
摘要翻译：公开了苯甲醇胺衍生物，其中m为2至8; n为1〜7，条件是m + n为4〜12; Ar是被一个或两个卤素原子，烷基或烷氧基或亚烷基二氧基取代的苯基或苯基; R1和R2是氢或烷基，条件是R1和R2中碳原子的总和不大于4; 及其生理上可接受的盐和溶剂化物。所述化合物在β2肾上腺素受体具有选择性兴奋剂作用，并且可以特别用于治疗与可逆气道阻塞物如哮喘和慢性支气管炎相关的疾病。化合物可以以常规方式配制成具有生理上可接受的载体或赋形剂的药物组合物。化合物可以例如通过烷基化胺制备：其中R 3，R 5和R 6是氢或保护基，然后除去任何保护基。

54. 发明授权

US5225445A Phenethanolamine derivatives having .beta..sub.2 -adrenoreceptor selective stimulant action 失效
标题翻译：具有（BETA）2-ADRENORECEPTOR选择性STIMULANT行动的苯乙醇胺衍生物
公开(公告)号：US5225445A
公开(公告)日：1993-07-06
申请号：US837783
申请日：1992-02-19
申请人： Ian F. Skidmore , Lawrence H. C. Lunts , Harry Finch , Alan Naylor
发明人： Ian F. Skidmore , Lawrence H. C. Lunts , Harry Finch , Alan Naylor
IPC分类号： C07C217/48 , A61K31/135 , A61K31/335 , A61K31/357 , A61K31/36 , A61P11/00 , A61P25/02 , C07C33/46 , C07C43/174 , C07C43/178 , C07C43/225 , C07C45/00 , C07C45/30 , C07C47/277 , C07C49/255 , C07C59/13 , C07C59/66 , C07C67/00 , C07C213/00 , C07C213/02 , C07C217/10 , C07C217/14 , C07C217/28 , C07C217/64 , C07C229/38 , C07D303/40 , C07D309/12 , C07D309/18 , C07D317/54 , C07D317/58 , C07D319/06 , C07D319/08 , C07D319/18
CPC分类号： C07C45/004 , C07C229/38 , C07C309/00 , C07C33/46 , C07C43/174 , C07C43/1742 , C07C43/1782 , C07C43/225 , C07C45/30 , C07C47/277 , C07C49/255 , C07C59/66 , C07D303/40 , C07D309/12 , C07D317/54 , C07D319/06 , Y02P20/55 , Y10S514/826 , Y10S514/863 , Y10S514/886 , Y10S514/887 , Y10S514/906 , Y10S514/913 , Y10S514/925 , Y10S514/926 , Y10S514/927 , Y10S514/928
摘要： Phenethanolamine derivatives are disclosed of formula ##STR1## wherein m is 2 to 8; n is 1 to 7 provided that m+n is 4 to 12;Ar is phenyl or phenyl substituted by one or two halogen atoms, alkyl or alkoxy groups or by an alkylenedioxy group;R.sup.1 and R.sup.2 are hydrogen or alkyl provided that the sum total of carbon atoms in R.sup.1 and R.sup.2 is not more than 4;and the physiologically acceptable salts and solvates thereof.The compounds have a selective stimulant action at .beta..sub.2 -adrenoreceptors and may be used inter alia in the treatment of diseases associated with reversible airways obstructions such as asthma and chronic bronchitis. The compounds may be formulated in conventional manner as pharmaceutical compositions with physiologically acceptable carriers or excipients.The compounds may be prepared, for example by alkylation of an amine: ##STR2## where R.sup.3, R.sup.5 and R.sup.6 is hydrogen or a protecting group, followed by removal of any protecting group.
摘要翻译：公开了苯甲醇胺衍生物，其中m为2至8; n为1〜7，条件是m + n为4〜12; Ar是被一个或两个卤素原子，烷基或烷氧基或亚烷基二氧基取代的苯基或苯基; R1和R2是氢或烷基，条件是R1和R2中碳原子的总和不大于4; 及其生理上可接受的盐和溶剂化物。所述化合物在β2肾上腺素受体具有选择性兴奋剂作用，并且可以特别用于治疗与可逆气道阻塞物如哮喘和慢性支气管炎相关的疾病。化合物可以以常规方式配制成具有生理上可接受的载体或赋形剂的药物组合物。化合物可以例如通过烷基化胺制备：其中R 3，R 5和R 6是氢或保护基，然后除去任何保护基。

55. 发明授权

US5109023A Phenethanolamine derivatives 失效
公开(公告)号：US5109023A
公开(公告)日：1992-04-28
申请号：US622505
申请日：1990-12-05
申请人： William L. Mitchell , Ian F. Skidmore , Lawrence H. C. Lunts , Harry Finch , Alan Naylor , David Hartley
发明人： William L. Mitchell , Ian F. Skidmore , Lawrence H. C. Lunts , Harry Finch , Alan Naylor , David Hartley
IPC分类号： C07C307/10 , C07C65/11 , C07C217/08 , C07C231/12 , C07C233/43 , C07C275/34 , C07C311/08 , C07C323/12 , C07C323/16 , C07C323/25
CPC分类号： C07C65/11 , Y10S514/819 , Y10S514/826 , Y10S514/886 , Y10S514/887 , Y10S514/913 , Y10S514/925 , Y10S514/927
摘要： The invention provides a method of treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis, utilizing the compounds of the formula ##STR1## or a physiological acceptable salt or solvate thereof, wherein Q represents a 1- or 2- naphthalenyl group.

56. 发明授权

US4943578A Piperazine compounds 失效
标题翻译：哌嗪化合物
公开(公告)号：US4943578A
公开(公告)日：1990-07-24
申请号：US355335
申请日：1989-05-23
申请人： Alan Naylor , Duncan B. Judd , Dearg S. Brown
发明人： Alan Naylor , Duncan B. Judd , Dearg S. Brown
IPC分类号： A61K31/495 , A61P9/00 , A61P9/10 , A61P25/04 , A61P25/28 , C07D241/04 , C07D401/06
CPC分类号： C07D401/06 , C07D241/04
摘要： Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents --COR.sub.4, --CO.sub.2 R.sub.4 or --COCO.sub.2 R.sub.4 (where R.sub.4 represents a hydrogen atom or an unsubstituted or substituted C.sub.1-10 hydrocarbon moiety);R.sub.2 and R.sub.3 are the same or different and are C.sub.1-6 alkyl or C.sub.3-6 alkenyl; or --NR.sub.2 R.sub.3 forms a 5-membered (optionally containing an oxygen atom adjacent to the nitrogen) or 6-membered ring, which ring optionally contains one unit of unsaturation and which is unsubstituted or substituted by optionally substituted methylidene, --COR.sub.5 (where R.sub.5 represents C.sub.1-6 alkyl, --OR.sub.6 or --NHR.sub.6 and R.sub.6 represents hydrogen, C.sub.1-6 alkyl, aryl, or ar(C.sub.1-6)alkyl, or N.dbd.NOR.sub.7 (where R.sub.7 represents C.sub.1-6 alkyl);X represents a direct bond, --CH.sub.2 -- or --CH.sub.2 O--;Ar represents a substituted phenyl moiety;and physiologically acceptable salts thereof.The compounds are indicated as useful in the treatment of pain and cerebral ischaemia.Processes and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.

57. 发明申请

US20090239845A1 PYRAZOLE COMPOUNDS AS PROSTAGLANDIN RECEPTORS LIGANDS 审中-公开
标题翻译：作为PROSTAGLANDIN受体配体的吡咯化合物
公开(公告)号：US20090239845A1
公开(公告)日：2009-09-24
申请号：US11912402
申请日：2006-04-24
申请人： Elizabeth Ann Conway , Gerard Martin Paul Giblin , Mairi Gibson , Adrian Hall , Thomas George Christopher Hayhow , Mark Patrick Healy , David Nigel Hurst , Ian Reginald Kilford , Stephen Carl McKeown , Alan Naylor , Helen Susanne Price , Derek Anthony Rawlings
发明人： Elizabeth Ann Conway , Gerard Martin Paul Giblin , Mairi Gibson , Adrian Hall , Thomas George Christopher Hayhow , Mark Patrick Healy , David Nigel Hurst , Ian Reginald Kilford , Stephen Carl McKeown , Alan Naylor , Helen Susanne Price , Derek Anthony Rawlings
IPC分类号： A61K31/55 , C07D231/40 , A61K31/415 , A61K31/5377 , C07D413/12 , C07D403/12 , A61P9/00
CPC分类号： C07D231/40 , C07D231/14 , C07D231/20 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein Z, R1, R2a, R2b, R10, R11 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Z，R1，R2a，R2b，R10，R11和Rx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。

58. 发明申请

US20090227591A1 Cyclopentene compounds 审中-公开
标题翻译：环戊烯化合物
公开(公告)号：US20090227591A1
公开(公告)日：2009-09-10
申请号：US10574901
申请日：2004-10-06
申请人： Gerard Martin Paul Giblin , Adrian Hall , David Nigel Hurst , Ian Reginald Kilford , Xiao Qing Lewell , Alan Naylor , Riccardo Novelli
发明人： Gerard Martin Paul Giblin , Adrian Hall , David Nigel Hurst , Ian Reginald Kilford , Xiao Qing Lewell , Alan Naylor , Riccardo Novelli
IPC分类号： A61K31/501 , A61K31/44 , C07D401/02 , C07D213/62
CPC分类号： C07C65/28 , C07C229/56 , C07C233/54 , C07C2601/10 , C07D213/55 , C07D213/61 , C07D213/64 , C07D237/24 , C07D239/28 , C07D241/24 , C07D401/08
摘要： Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, B, Z, R1, R2a, R2b, R8, R9, 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，Z，R1，R2a，R2b，R8，R9和Rx如本说明书中所定义，制备这些化合物的方法，药物组合物包括这些化合物和这些化合物在医药中的用途。

59. 发明申请

US20080275053A1 Heterocyclyl Compounds 审中-公开
标题翻译：杂环化合物
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。

60. 发明申请

US20080261977A1 Pyrimidine Derivatives as Cannabinoid Receptor Modulators 审中-公开
标题翻译：嘧啶衍生物作为大麻类受体调节剂
公开(公告)号：US20080261977A1
公开(公告)日：2008-10-23
申请号：US10597521
申请日：2005-02-21
申请人： Andrew John Eatherton , Gerard Martin Paul Giblin , William Leonard Mitchell , Alan Naylor
发明人： Andrew John Eatherton , Gerard Martin Paul Giblin , William Leonard Mitchell , Alan Naylor
IPC分类号： A61K31/5377 , C07D239/42 , A61K31/505 , A61P29/00 , A61P37/00 , C07D413/06
CPC分类号： C07D239/42 , C07D401/12
摘要： The present invention relates to novel pyrimidine 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：本发明涉及新颖的嘧啶衍生物，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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