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11. 发明授权

US07115616B2 Pyrimidinone compounds 有权
标题翻译：嘧啶酮化合物
公开(公告)号：US07115616B2
公开(公告)日：2006-10-03
申请号：US10776876
申请日：2004-02-11
申请人： Ashley Edward Fenwick , Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith
发明人： Ashley Edward Fenwick , Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith
IPC分类号： C07D473/00 , C07D239/02 , A61K31/505 , A61P9/10
CPC分类号： C07D239/56 , C07D401/14 , C07D403/06
摘要： Pyrimidinone compounds of formula (10 are inhibitors of the enzyme Lp-PLA2 and of use in therapy, in particular for treating atherosclerosis.
摘要翻译：式（10）的嘧啶酮化合物是Lp-PLA 2酶的抑制剂，并且在治疗中尤其用于治疗动脉粥样硬化。

12. 发明授权

US07462620B2 Pyrimidinone derivatives and their use in the treatment of atherosclerosis 失效
标题翻译：嘧啶酮衍生物及其在治疗动脉粥样硬化中的应用
公开(公告)号：US07462620B2
公开(公告)日：2008-12-09
申请号：US11456129
申请日：2006-07-07
申请人： Deirdre Mary Bernadette Hickey , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith
发明人： Deirdre Mary Bernadette Hickey , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith
IPC分类号： C07D239/70 , A61K31/517
CPC分类号： C07D239/36 , C07D239/70 , C07D239/91 , C07D401/12 , C07D403/12 , C07D409/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis.
摘要翻译：式（I）化合物：是Lp-PLA2酶的抑制剂，可用于治疗，特别是治疗动脉粥样硬化。

13. 发明授权

US06953803B1 Pyrimidine compounds 有权
标题翻译：嘧啶化合物
公开(公告)号：US06953803B1
公开(公告)日：2005-10-11
申请号：US10030661
申请日：2000-04-25
申请人： Deirdre Mary Bernadette Hickey , Colin Andrew Leach , Stephen Allan Smith
发明人： Deirdre Mary Bernadette Hickey , Colin Andrew Leach , Stephen Allan Smith
IPC分类号： A61K31/00 , A61K31/506 , A61K31/513 , A61K31/5377 , A61P3/10 , A61P9/08 , A61P9/10 , A61P9/12 , A61P19/02 , A61P25/18 , A61P25/28 , A61P29/00 , A61P43/00 , C07D239/26 , C07D239/34 , C07D239/42 , C07D239/56 , C07D401/14 , C07D403/06 , C07D403/08 , C07D409/14 , A01N43/54 , A61K31/497 , A61K31/535 , C07D403/00 , C07D413/00
CPC分类号： C07D239/56 , C07D401/14 , C07D403/06
摘要： Pyrmidinone compounds of formula (I) are inhibitors of the enzyme Lp-PLA2 and of use in therapy, in particular for treating atherosclerosis.
摘要翻译：式（I）的嘧啶酮化合物是Lp-PLA 2酶的抑制剂，并且用于治疗，特别是用于治疗动脉粥样硬化。

14. 发明授权

US07153861B2 5,6 -Trimethylenepyrimidin-4-one compounds 有权
标题翻译： 5,6-三甲基嘧啶-4-酮化合物
公开(公告)号：US07153861B2
公开(公告)日：2006-12-26
申请号：US10694561
申请日：2003-10-27
申请人： Colin Andrew Leach , Stephen Allan Smith , Steven James Stanway
发明人： Colin Andrew Leach , Stephen Allan Smith , Steven James Stanway
IPC分类号： C07D239/70 , A61K31/517 , C07D401/12
CPC分类号： C07D239/56 , C07D239/60 , C07D239/70 , C07D239/95 , C07D401/12 , C07D403/12 , C07D495/04
摘要： Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use is treating atheroscelerosis.
摘要翻译：式（I）的嘧啶酮化合物：是Lp-PLA 2酶的抑制剂，并且可用于治疗动脉粥样硬化。

15. 发明授权

US07470694B2 5,6-trimethylenepyrimidin-4-one compounds 有权
标题翻译： 5,6-三亚甲基嘧啶-4-酮化合物
公开(公告)号：US07470694B2
公开(公告)日：2008-12-30
申请号：US11561035
申请日：2006-11-17
申请人： Colin Andrew Leach , Stephen Allan Smith , Steven James Stanway
发明人： Colin Andrew Leach , Stephen Allan Smith , Steven James Stanway
IPC分类号： A61K31/517
CPC分类号： C07D239/56 , C07D239/60 , C07D239/70 , C07D239/95 , C07D401/12 , C07D403/12 , C07D495/04
摘要： Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atheroscelerosis.
摘要翻译：式（I）的嘧啶酮化合物：是Lp-PLA2酶的抑制剂，可用于治疗动脉粥样硬化。

16. 发明授权

US06559155B1 Pyrimidinone derivatives for the treatment of atherosclerosis 失效
标题翻译：嘧啶酮衍生物用于治疗动脉粥样硬化
公开(公告)号：US06559155B1
公开(公告)日：2003-05-06
申请号：US09763492
申请日：2001-02-21
申请人： Colin Andrew Leach , Stephen Allan Smith
发明人： Colin Andrew Leach , Stephen Allan Smith
IPC分类号： A61K31505
CPC分类号： C07D239/56 , C07D401/14
摘要： Pyrimidones of formula (I) are inhibitors of the enzyme LpPLA2 and thereof use in treating inter alia atherosclerosis, in which: R1 is COOH or a salt thereof, COOR10, CONR11R12, CN or CH2OH; R2 is a mono- or bicyclic aromatic ring system or a mono- or bicyclic heteroaromatic ring system; R3 is C1-20alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-5alkyl, C1-10alkoxyC1-10alkyl, or an aromatic or heteroaromatic ring system; W is SO2 or a bond; X is O or S; and Y is a group of the formula A1—A2—A3 in which A1 and A3 each represent a bond or a straight chain or branched alkylene group, said alkylene group(s) containing a total of 1 to 10 carbon atoms and A2 represents a bond or O, S, SO, SO2, CO, C═CH2, CONH, NHCO, CR15R16, CH═CH or C═C, providing that when A2 is O, S, SO, SO2 or CONH, A3 contains at least two carbon atoms linking the A2 group and the CH2 group in formula (I).
摘要翻译：式（I）的嘧啶酮是LpPLA2酶的抑制剂，其用于治疗特别是动脉粥样硬化，其中：R1是COOH或其盐，COOR10，CONR11R12，CN或CH2OH; R2是单环或双环芳环体系或单环或双环杂芳环系; R 3为C 1-20烷基，C 3-6环烷基，C 3-6环烷基C 1-5烷基，C 1-10烷氧基C 1-10烷基或芳族或杂芳环系; W为SO 2或键; X为O 或S; 和Y是式A1-A2-A3的基团，其中A1和A3各自表示键或直链或支链亚烷基，所述亚烷基含有总共1至10个碳原子，A2表示键或O，S，SO，SO2，CO，C = CH2，CONH，NHCO，CR15R16，CH = CH或C = C，条件是当A2为O，S，SO，SO2或CONH时，A3含有至少两个碳连接式（I）中的A2基团和CH2基团的原子。

17. 发明授权

US08765772B2 Purine derivatives for use in the treatment of allergic, inflammatory and infectious diseases 有权
标题翻译：嘌呤衍生物用于治疗过敏性，炎性和感染性疾病
公开(公告)号：US08765772B2
公开(公告)日：2014-07-01
申请号：US13058470
申请日：2009-08-07
申请人： Keith Biggadike , Diane Mary Coe , Xiao Qing Lewell , Charlotte Jane Mitchell , Stephen Allan Smith , Naimisha Trivedi
发明人： Keith Biggadike , Diane Mary Coe , Xiao Qing Lewell , Charlotte Jane Mitchell , Stephen Allan Smith , Naimisha Trivedi
IPC分类号： A61K31/522 , C07D473/34
CPC分类号： A61K31/522 , A61K9/0043 , A61K31/55 , A61K45/06 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00 , C07D473/16 , C07D473/18
摘要： The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
摘要翻译：本发明涉及式（I）的化合物：其中R 1是C 1-6烷基氨基，C 1-6烷氧基或C 3-7环烷氧基; m为3〜6的整数， n为0〜4的整数，其盐是人类干扰素的诱导剂。诱导人类干扰素的化合物可用于治疗各种疾病，例如治疗过敏性疾病和其它炎性病症，例如过敏性鼻炎和哮喘，治疗感染性疾病和癌症，并且也可用作疫苗佐剂。

18. 发明授权

US08067426B2 6-amino-purin-8-one compounds 有权
标题翻译： 6-氨基 - 嘌呤-8-酮化合物
公开(公告)号：US08067426B2
公开(公告)日：2011-11-29
申请号：US12537392
申请日：2009-08-07
申请人： Keith Biggadike , Diane Mary Coe , Xiao Qing Lewell , Charlotte Jane Mitchell , Stephen Allan Smith , Naimisha Trivedi
发明人： Keith Biggadike , Diane Mary Coe , Xiao Qing Lewell , Charlotte Jane Mitchell , Stephen Allan Smith , Naimisha Trivedi
IPC分类号： C07D473/18 , A61K31/522 , C07D473/40 , C07D473/16 , A61P37/08 , A61P11/06
CPC分类号： A61K31/522 , A61K9/0043 , A61K31/55 , A61K45/06 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00 , C07D473/16 , C07D473/18
摘要： Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
摘要翻译：式（I）化合物：其中R 1是C 1-6烷基氨基，C 1-6烷氧基或C 3-7环烷氧基; m为3〜6的整数， n为0〜4的整数，其盐是人类干扰素的诱导剂。诱导人类干扰素的化合物可用于治疗各种疾病，例如治疗过敏性疾病和其它炎性病症，例如过敏性鼻炎和哮喘，治疗感染性疾病和癌症，并且也可用作疫苗佐剂。

19. 发明申请

US20110229500A1 PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES 有权
标题翻译：用于治疗过敏，炎性和感染性疾病的药物衍生物
公开(公告)号：US20110229500A1
公开(公告)日：2011-09-22
申请号：US13058470
申请日：2009-08-07
申请人： Keith Biggadike , Diane Mary Coe , Xiao Qing Lewell , Charlotte Jane Mitchell , Stephen Allan Smith , Naimisha Trivedi
发明人： Keith Biggadike , Diane Mary Coe , Xiao Qing Lewell , Charlotte Jane Mitchell , Stephen Allan Smith , Naimisha Trivedi
IPC分类号： A61K31/522 , C07D473/34 , A61K31/55 , A61K39/00 , A61P37/00 , A61P11/06 , A61P37/08 , A61P29/00
CPC分类号： A61K31/522 , A61K9/0043 , A61K31/55 , A61K45/06 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00 , C07D473/16 , C07D473/18
摘要： The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
摘要翻译：本发明涉及式（I）的化合物：其中R 1是C 1-6烷基氨基，C 1-6烷氧基或C 3-7环烷氧基; m为3〜6的整数， n为0〜4的整数，其盐是人类干扰素的诱导剂。诱导人类干扰素的化合物可用于治疗各种疾病，例如治疗过敏性疾病和其它炎性病症，例如过敏性鼻炎和哮喘，治疗感染性疾病和癌症，并且也可用作疫苗佐剂。

20. 发明申请

US20090227600A1 4-(PYRAZINE-2-YL) -PYRROLIDINE -2-CARBOXYLIC ACID COMPOUNDS AND DERIVATIVES THEREOF AS HEPATITIS C VIRUS INHIBITORS 审中-公开
标题翻译： 4-（吡嗪-2-基） - 吡咯烷-2-羧酸化合物及其作为丙型肝炎病毒抑制剂的衍生物
公开(公告)号：US20090227600A1
公开(公告)日：2009-09-10
申请号：US11577940
申请日：2005-10-24
申请人： Rossella Guidetti , David Haigh , Charles David Hartley , Peter David Howes , Fabrizio Nerozzi , Stephen Allan Smith
发明人： Rossella Guidetti , David Haigh , Charles David Hartley , Peter David Howes , Fabrizio Nerozzi , Stephen Allan Smith
IPC分类号： A61K31/497 , C07D417/14 , A61P31/12
CPC分类号： C07D417/14
摘要： Anti-viral agents of Formula (Ia) wherein: A represents hydroxy; B represents C(O)R3 wherein R3 is 4-tert-butyl-3-methoxyphenyl; D represents 1,3-thiazol-2-yl or 5-methyl-1,3-thiazol-2-yl; E represents pyrazin-2-yl; G represents 1,3-thiazol-2-ylmethyl, 1,3-thiazol-4-ylmethyl, 1,2-thiazol-3-ylmethyl, or 1H-pyrazol-1-ylmethyl; and salts, solvates and esters thereof; provided that when A is esterified to form —OR where R is selected from straight or branched chain alkyl, aralkyl, aryloxyalkyl, or aryl, then R is other than tert-butyl, processes for their preparation and their use in HCV treatment are provided.
摘要翻译：式（Ia）的抗病毒剂，其中：A表示羟基; B表示C（O）R 3，其中R 3是4-叔丁基-3-甲氧基苯基; D代表1,3-噻唑-2-基或5-甲基-1,3-噻唑-2-基; E表示吡嗪-2-基; G表示1,3-噻唑-2-基甲基，1,3-噻唑-4-基甲基，1,2-噻唑-3-基甲基或1H-吡唑-1-基甲基; 及其盐，溶剂化物和酯; 条件是当A被酯化形成-OR时，其中R选自直链或支链烷基，芳烷基，芳氧基烷基或芳基，则R不是叔丁基，提供其制备方法及其在HCV治疗中的用途。

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