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1. 发明授权

US07169924B2 Pyrimidinone derivatives and their use in the treatment of atherosclerosis 失效
公开(公告)号：US07169924B2
公开(公告)日：2007-01-30
申请号：US10398977
申请日：2001-10-05
申请人： Richard Leonard Elliott , Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith
发明人： Richard Leonard Elliott , Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith
IPC分类号： C07D239/70 , A61K31/517 , A61P9/01
CPC分类号： C07D239/36 , C07D239/70 , C07D239/91 , C07D401/12 , C07D403/12 , C07D409/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Compound of formula (I): are disclosed in which: R1 is an aryl group, optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from C(1-6)alkyl, C(1-6)alkoxy, C(1-6)alkylthio, hydroxy, halogen, CN, and mono to perfluoro-C(1-4)alkyl; R2 is halogen, C(1-3)alkyl, C(1-3)alkoxy, hydroxyC(1-3)alkyl, C(1-3)alkylthio, C(1-3)alkylsulphinyl, aminoC(1-3)alkyl, mono- or di-C(1-3)alkylaminoC(1-3)alkyl, C(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkoxyC(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkylsulphonylaminoC(1-3)alkyl, C(1-3)alkylcarboxy, C(1-3)alkylcarboxyC(1-3)alkyl, and R3 is hydrogen, halogen, C(1-3)alkyl, or hydroxyC(1-3)alkcyl; or R2 and R3 together with the pyrimidone ring carbon atoms to which they are attached form a fused 5-or 6-membered carbocyclic ring; or R2 and R3 together with the pyrimidone ring carbon atoms to which they are attached form a fused benzo or heteroaryl ring ring optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from halogen, C(1-4)alkyl, cyano, C(1-6)alkoxy, C(1-6)alkylthio or mono to perfluoro-C(1-4)alkyl; R4 is hydrogen, C(1-6)alkyl which may be unsubstituted or substituted by 1, 2 or 3 substituents selected from hydroxy, halogen, OR7, COR7, carboxy, COOR7, CONR9R10, NR9R10, NR7COR8, mono- or di-(hydroxyC(1-6)alkyl) amino and N-hydroxyC(1-6)alkyl-N—C(1-6)allkylamino; or R4 is Het-C(0-4)alkyl in which Het is a 5- to 7- membered heterocyclyl ring comprising N and optionally O or S, and in which N may be substituted by COR7, COOR7, CONR9R10, or C(1-6)alkyl optionally substituted by 1, 2 or 3 substituents selected from hydroxy, halogen, OR7, COR7, carboxy, COOR7, CONR9R10 or NR9R10, for instance, piperidinyl-4-yl, pyrrolidin-3-yl; R5 is an aryl or a heteroaryl ring optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selectd from C(1-6)alkyl, C(1-6)alkoxy, C(1-6)alkylthio, arylC(1-6)alkoxy, hydroxy, halogen, CN, COR7, carboxy, COOR7, NR7COR8, CONR9R10, SO2NR9R10, NR7SO2R8, NR9R10, mono to perfluoro-C(1-4)alkyl and mono to perfluoro-C(1-4)alkoxy; R6 is an aryl or a heteroaryl ring which is further optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from C(1-18)alkyl, C(1-18)alkoxy, C(1-6)alkylthio, C(1-6)alkylsulfonyl, arylC(1-6)alkoxy, hydroxy, halogen, CN, COR7, carboxy, COOR7, CONR9R10, NR7COR8, SO2NR9R10, NR7SO2R8, NR9R10, mono to perfluoro-C(1-4)alkyl and mono to perfluoro-C(1-4)alkoxy, or C(5-10)alkyl; These compound are useful for treating diseases associated with abnormal activity of the phospholipase A2 enzyme, for example athereosclosis.

2. 发明授权

US07638520B2 Pyrimidine compounds 有权
标题翻译：嘧啶化合物
公开(公告)号：US07638520B2
公开(公告)日：2009-12-29
申请号：US11561926
申请日：2006-11-21
申请人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
发明人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
IPC分类号： C07D239/70 , 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。

3. 发明申请

US20090170877A1 5,6-Trimethylenepyrimidin-4-one compounds 审中-公开
标题翻译： 5,6-三甲基嘧啶-4-酮化合物
公开(公告)号：US20090170877A1
公开(公告)日：2009-07-02
申请号：US12372837
申请日：2009-02-18
申请人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
发明人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
IPC分类号： A61K31/506 , A61K31/517 , A61K31/513 , A61P29/00 , A61P25/00 , A61P25/28
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 atherosclerosis.
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。

4. 发明申请

US20120172378A1 NOVEL COMPOUNDS 有权
标题翻译：新型化合物
公开(公告)号：US20120172378A1
公开(公告)日：2012-07-05
申请号：US13309941
申请日：2011-12-02
申请人： Deirdre Mary Bernadette HICKEY , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
发明人： Deirdre Mary Bernadette HICKEY , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
IPC分类号： A61K31/517 , C07D239/70 , A61P9/10 , C07D401/12 , C07D239/56 , A61K31/513 , C07D403/12
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 in treating atherosclerosis.
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。

5. 发明授权

US06417192B1 Pyrimidinone compounds and pharmaceutical compositions containing them 失效
公开(公告)号：US06417192B1
公开(公告)日：2002-07-09
申请号：US09530713
申请日：2000-06-28
申请人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Roderick Alan Porter , Stephen Allan Smith
发明人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Roderick Alan Porter , Stephen Allan Smith
IPC分类号： C07D23954
CPC分类号： C07D239/56 , C07D231/12 , C07D233/56 , C07D239/52 , C07D249/08 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D407/14 , C07D409/14 , C07D417/06 , C07D417/14
摘要： A group of novel pyrimidone compounds are inhibitors of the enzyme LDL PLA2 and therefore of use in treating atherosclerosis.

6. 发明授权

US07652019B2 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：US07652019B2
公开(公告)日：2010-01-26
申请号：US12349086
申请日：2009-01-06
申请人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
发明人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
IPC分类号： A61K31/517 , C07D239/70
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 atherosclerosis.
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。

7. 发明授权

US07235566B2 Pyridinone derivatives for treatment of atherosclerosis 有权
标题翻译：用于治疗动脉粥样硬化的吡啶酮衍生物
公开(公告)号：US07235566B2
公开(公告)日：2007-06-26
申请号：US10900489
申请日：2004-07-28
申请人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , John Liddle , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
发明人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , John Liddle , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
IPC分类号： C07D215/36 , C07D401/02 , A61K31/47
CPC分类号： C07D221/04 , C04B35/632 , C07D211/74 , C07D215/36 , C07D401/12 , C07D471/04 , C07D495/04 , C07D513/04
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-PLA 2酶的抑制剂，可用于治疗，特别是用于治疗动脉粥样硬化。

8. 发明授权

US06649619B1 Compounds 有权
标题翻译：化合物
公开(公告)号：US06649619B1
公开(公告)日：2003-11-18
申请号：US10357238
申请日：2003-02-03
申请人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
发明人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
IPC分类号： C07D23970
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。

9. 发明授权

US08871775B2 Compounds 有权
标题翻译：化合物
公开(公告)号：US08871775B2
公开(公告)日：2014-10-28
申请号：US13309941
申请日：2011-12-02
申请人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
发明人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
IPC分类号： A61K31/519 , C07D473/00 , C07D239/02 , C07D239/95 , C07D239/56 , C07D239/60 , C07D403/12 , C07D495/04 , C07D239/70 , 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 in treating atherosclerosis.
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。

10. 发明申请

US20090118313A1 Novel Compounds 有权
标题翻译：新型化合物
公开(公告)号：US20090118313A1
公开(公告)日：2009-05-07
申请号：US12349086
申请日：2009-01-06
申请人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
发明人： Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith , Steven James Stanway
IPC分类号： A61K31/519 , A61K31/506 , A61K31/513 , A61P9/10 , A61K31/505 , 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 atherosclerosis.
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。

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