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1. 发明授权

US08143264B2 Xanthine derivatives as selective HM74A agonists 失效
标题翻译：黄嘌呤衍生物作为选择性HM74A激动剂
公开(公告)号：US08143264B2
公开(公告)日：2012-03-27
申请号：US12063434
申请日：2006-08-08
申请人： Richard Jonathan Daniel Hatley , Andrew McMurtrie Mason , Ivan Leo Pinto
发明人： Richard Jonathan Daniel Hatley , Andrew McMurtrie Mason , Ivan Leo Pinto
IPC分类号： C07D473/04 , C07D473/06 , A61K31/522 , A61P9/10 , A61P9/00 , A61P13/12 , A61P3/10
CPC分类号： C07D473/04 , C07D473/06
摘要： The present invention relates to a xanthine compound derivative which is 3-butyl-8-chloro-1-(3-{5-[(4-fluorophenyl)methyl]-2H-tetrazol-2-yl}propyl)-3,7-dihydro-1H-purine-2,6-dione: a pharmaceutically acceptable salt thereof, corresponding pharmaceutical formulations, combinations, preparation methods and methods or uses in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.
摘要翻译：本发明涉及3-丁基-8-氯-1-（3- {5 - [（4-氟苯基）甲基] -2H-四唑-2-基}丙基）-3,7 - 二氢-1H-嘌呤-2,6-二酮：其药学上可接受的盐，相应的药物制剂，组合，制备方法和方法或用途，用于治疗HM74A受体的未激活有助于疾病或其中激活的疾病的受体将是有益的。

2. 发明申请

US20100168122A1 XANTHINE DERIVATIVES AS SELECTIVE HM74A AGONISTS 失效
标题翻译： XANTHINE衍生物作为选择性HM74A激动剂
公开(公告)号：US20100168122A1
公开(公告)日：2010-07-01
申请号：US12063434
申请日：2006-08-08
申请人： Richard Jonathan Daniel Hatley , Andrew McMurtrie Mason , Ivan Leo Pinto
发明人： Richard Jonathan Daniel Hatley , Andrew McMurtrie Mason , Ivan Leo Pinto
IPC分类号： C07D473/04 , A61K31/522
CPC分类号： C07D473/04 , C07D473/06
摘要： The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for manufacture of said derivatives, pharmaceutical formulations containing these compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial
摘要翻译：本发明涉及作为黄嘌呤衍生物的式（I）化合物，所述衍生物的制备方法，含有这些化合物的药物制剂以及该化合物在治疗中的用途，例如治疗未激活的疾病 HM74A受体有助于该疾病或受体活化将是有益的

3. 发明申请

US20080221108A1 Anthranilic Acid Derivatives As Hm74A Receptor Agonists 审中-公开
标题翻译：邻氨基苯甲酸衍生物作为Hm74A受体激动剂
公开(公告)号：US20080221108A1
公开(公告)日：2008-09-11
申请号：US11815350
申请日：2006-02-14
申请人： Richard Hatley , Andrew McMurtrie Mason , Ivan Leo Pinto , Ian Edward David Smith
发明人： Richard Hatley , Andrew McMurtrie Mason , Ivan Leo Pinto , Ian Edward David Smith
IPC分类号： A61K31/196 , C07D271/06 , C07D253/10 , A61K31/4245 , A61P3/00 , A61P9/10 , A61K31/53 , C07C63/06
CPC分类号： C07C235/24 , C07D253/10 , C07D271/06 , C07D401/04
摘要： Therapeutically active anthranilic acid derivatives of Formula (I) wherein R1, R2 and W, are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.
摘要翻译：其中R 1，R 2和W的式（I）的治疗活性的邻氨基苯甲酸衍生物如说明书中所定义，用于制备所述衍生物，药物制剂含有活性化合物和化合物在治疗中的用途，特别是在治疗其中HM74A受体的活化不足有助于疾病或其中受体的活化将是有益的疾病方面。

4. 发明申请

US20080214638A1 Anthranilic Acid Derivatives Active as the Hm74a Receptor 审中-公开
标题翻译：活性为Hm74a受体的邻氨基苯甲酸衍生物
公开(公告)号：US20080214638A1
公开(公告)日：2008-09-04
申请号：US11815402
申请日：2006-02-14
申请人： Andrew McMurtrie Mason , Ivan Leo Pinto , Shahzad Sharooq Rahman
发明人： Andrew McMurtrie Mason , Ivan Leo Pinto , Shahzad Sharooq Rahman
IPC分类号： A61K31/41 , C07C229/00 , A61K31/19 , A61P29/00 , A61P9/00 , C07D257/04
CPC分类号： C07D257/04 , C07C235/24
摘要： Therapeutically active anthranilic acid derivatives of Formula (I) or of Formula (Ia) wherein R, R1, R2 and Z are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.
摘要翻译：式（I）或式（Ia）的其中R，R 1，R 2和Z如本说明书中所定义的式（I）或式（Ia）的治疗活性的邻氨基苯甲酸衍生物所述衍生物的制备，含有活性化合物的药物制剂和该化合物在治疗中的用途，特别是用于治疗HM74A受体的未激活有助于疾病或受体激活将是有益的疾病，被披露。

5. 发明申请

US20080200468A1 2-Substituted 5-Membered Heteroaryl Carboxylates as Hm74a Receptor Agonists 审中-公开
标题翻译： 2-取代的5元杂芳基羧酸盐作为Hm74a受体激动剂
公开(公告)号：US20080200468A1
公开(公告)日：2008-08-21
申请号：US11815389
申请日：2006-02-14
申请人： Juliet Kay Simpson , Ivan Leo Pinto
发明人： Juliet Kay Simpson , Ivan Leo Pinto
IPC分类号： A61K31/53 , C07D333/36 , C07D401/14 , A61P3/06 , A61P3/00 , A61K31/381
CPC分类号： C07D333/40 , C07D307/68 , C07D409/12
摘要： Therapeutically active heteroaryl carboxylic acid derivatives of Formula (I) wherein R1, R2, W, X, Y and Z are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.
摘要翻译：其中R 1，R 2，W，X，Y和Z的式（I）的治疗活性的杂芳基羧酸衍生物如说明书中所定义，制备方法的所述衍生物，含有活性化合物的药物制剂以及该药物在治疗中的用途，特别是用于治疗其中HM74A受体的未激活有助于该疾病或受体活化将有益的疾病。披露

6. 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。

7. 发明申请

US20100160354A1 NOVEL COMPOUNDS 有权
标题翻译：新型化合物
公开(公告)号：US20100160354A1
公开(公告)日：2010-06-24
申请号：US12717349
申请日：2010-03-04
申请人： Ivan Leo Pinto , Shahzad Sharooq Rahman , Neville Hubert Nicholson
发明人： Ivan Leo Pinto , Shahzad Sharooq Rahman , Neville Hubert Nicholson
IPC分类号： A61K31/522 , A61P9/00 , A61P7/12 , A61P3/04 , A61P3/06
CPC分类号： C07D473/06 , C07D473/04
摘要： The present invention relates to therapeutically active xanthine derivative compounds of Formula (I): corresponding processes for manufacture of said derivatives, pharmaceutical formulations containing and uses of such compounds in therapy, particularly in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.
摘要翻译：本发明涉及式（I）的治疗活性黄嘌呤衍生物化合物：用于制备所述衍生物的相应方法，含有这些化合物在治疗中的药物制剂，以及其用途，特别是治疗HM74A受体活化不足的疾病该疾病或受体的激活将是有益的。

8. 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。

9. 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。

10. 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.

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