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    SUBSTITUTED QUINAZOLINES (OPEN RING)
    3.
    发明申请
    SUBSTITUTED QUINAZOLINES (OPEN RING) 审中-公开
    取代藜芦醇（OPEN RING）

    公开(公告)号：WO2011114163A1

    公开(公告)日：2011-09-22

    申请号：PCT/GB2011/050531

    申请日：2011-03-17

    申请人： SHIRE LLC ,  FRANKLIN, Richard ,  GOLDING, Bernard

    发明人： FRANKLIN, Richard ,  GOLDING, Bernard

    IPC分类号： C07D239/72

    CPC分类号： C07D239/84 ,  C07D239/86

    摘要： This invention relates to the discovery of prodrugs of 5-substituted analogues of the selective platelet lowering agent anagrelide which are extremely potent inhibitors of phosphodiesterase III (PDE III). The prodrug compounds are potentially useful agents for the treatment of conditions in which the inhibition of PDE III in beneficial.

    摘要翻译： 本发明涉及作为磷酸二酯酶III（PDE III）的非常有效的抑制剂的选择性血小板降低剂阿那格雷的5-取代的类似物的前药的发现。 前药化合物是用于治疗PDE III抑制有益的病症的潜在有用的药剂。

    SUBSTITUTED QUINAZOLINES AS BLOOD PLATELET LOWERING AGENTS
    4.
    发明申请
    SUBSTITUTED QUINAZOLINES AS BLOOD PLATELET LOWERING AGENTS 审中-公开
    作为血液平板降低剂的替代品

    公开(公告)号：WO2009138793A1

    公开(公告)日：2009-11-19

    申请号：PCT/GB2009/050513

    申请日：2009-05-13

    申请人： SHIRE LLC ,  GOLDING, Bernard ,  FRANKLIN, Richard

    发明人： GOLDING, Bernard ,  FRANKLIN, Richard

    IPC分类号： C07D487/04 ,  C07D513/04 ,  A61K31/519 ,  A61P7/00

    CPC分类号： C07D487/04 ,  C07D513/04

    摘要： This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim (I): and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

    摘要翻译： 本发明涉及具有降低心血管副作用潜力的选择性血小板降低剂阿那格雷的取代类似物的发现，其应该导致改善的患者依从性和治疗骨髓增生性疾病的安全性。 更具体地，本发明涉及具有下面通式的某些咪唑并喹唑啉衍生物，其中取代基具有权利要求（I）中定义的含义：并且其在人体中具有作为血小板降低剂的效用。 本发明的化合物通过抑制巨核细胞吞噬作用并因此起血小板的形成的作用。

    SUBSTITUTED QUINAZOLINES
    5.
    发明申请
    SUBSTITUTED QUINAZOLINES 审中-公开
    取代的喹唑啉

    公开(公告)号：WO2009138792A1

    公开(公告)日：2009-11-19

    申请号：PCT/GB2009/050512

    申请日：2009-05-13

    申请人： SHIRE LLC ,  GOLDING, Bernard ,  CICALA, Peter ,  FRANKLIN, Richard ,  HIRST, Kim

    发明人： GOLDING, Bernard ,  CICALA, Peter ,  FRANKLIN, Richard ,  HIRST, Kim

    IPC分类号： C07D471/04 ,  C07D475/04 ,  C07D491/048 ,  C07D495/04 ,  A61K31/519 ,  A61P7/02

    CPC分类号： C07D471/04 ,  C07D475/04 ,  C07D491/048 ,  C07D495/04

    摘要： This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

    摘要翻译： 本发明涉及降低心血管副作用潜力的选择性血小板降低剂阿那格雷的3-取代类似物和5-取代的类似物的发现，其应该导致改善的患者依从性和治疗骨髓增生性疾病的安全性。 更具体地，本发明涉及具有以下通式的某些咪唑并喹唑啉衍生物，其中取代基具有权利要求1中定义的含义，并且其在人体中可用作血小板降低剂。 本发明的化合物通过抑制巨核细胞吞噬作用并因此起血小板的形成的作用。

    SUBSTITUTED QUINAZOLINES
    7.
    发明申请
    SUBSTITUTED QUINAZOLINES 审中-公开
    取代的喹唑啉

    公开(公告)号：WO2008065444A2

    公开(公告)日：2008-06-05

    申请号：PCT/GB2007/050697

    申请日：2007-11-19

    申请人： SHIRE LLC ,  FRANKLIN, Richard ,  GOLDING, Bernard

    发明人： FRANKLIN, Richard ,  GOLDING, Bernard

    CPC分类号： C07D487/04

    摘要： This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

    摘要翻译： 本发明涉及降低心血管副作用潜力的选择性血小板降低剂阿那格雷的3-取代类似物和5-取代的类似物的发现，其应该导致改善的患者依从性和治疗骨髓增生性疾病的安全性。 更具体地，本发明涉及某些在人体中作为血小板降低剂具有效用的咪唑并喹唑啉衍生物。 本发明的化合物通过抑制巨核细胞吞噬作用并因此起血小板的形成的作用。

    OIL BASED FORMULATIONS
    8.
    发明申请
    OIL BASED FORMULATIONS 审中-公开
    基于油的配方

    公开(公告)号：WO2012066347A1

    公开(公告)日：2012-05-24

    申请号：PCT/GB2011/052262

    申请日：2011-11-18

    申请人： SHIRE, LLC ,  FRANKLIN, Richard ,  GOLDING, Bernard

    发明人： FRANKLIN, Richard ,  GOLDING, Bernard

    IPC分类号： A61K9/50 ,  A61K31/485 ,  A61K9/51

    CPC分类号： A61K31/485 ,  A61K9/4825 ,  A61K9/4875 ,  A61K31/55 ,  A61K47/44

    摘要： The present invention relates to the use of oil based delivery vehicles to prevent undesirable premature hydrolysis of phenolic amino benzoic acid carbamate prodrugs, while resident in the gut lumen. Preclusion of water and hydrolytic enzymes prior to prodrug absorption ensures that such compounds can be fully absorbed intact without undergoing unintended premature hydrolysis in the gastrointestinal tract so maximizing the benefit of improved systemic availability afforded by the prodrug. Furthermore judicious selection of oil and prodrug salt form can result in a sustained release plasma PK profile. The avoidance of premature degradation and release of active drug into the gut lumen minimizes any potential for a direct adverse interaction within the gut lumen.

    摘要翻译： 本发明涉及油基递送载体的用途，以防止苯胺氨基苯甲酸氨基甲酸酯前药在居住在肠腔中时不期望的过早水解。 在前药吸收之前排除水和水解酶确保这样的化合物完全被完全吸收，而不会在胃肠道中经历不期望的过早水解，从而最大化由前体药物提供的改善的全身可用性的益处。 此外，明智地选择油和前药盐形式可导致持续释放血浆PK谱。 避免过早降解和将活性药物释放到肠腔中，可以最大限度地减少肠腔内直接不良相互作用的潜力。

    ANAGRELIDE DERIVATIVES (IMIDAZO [2, 1-B] QUINAZOLIN - 2 - ONES ) AS PDE III INHIBITORS USEFUL AS ANTITHROMBOTIC AGENTS
    9.
    发明申请
    ANAGRELIDE DERIVATIVES (IMIDAZO [2, 1-B] QUINAZOLIN - 2 - ONES ) AS PDE III INHIBITORS USEFUL AS ANTITHROMBOTIC AGENTS 审中-公开
    抗生素衍生物（IMIDAZO [2,1-B]喹唑啉-2 - ONES）作为PDE III抑制剂有效用作抗生素

    公开(公告)号：WO2011114160A1

    公开(公告)日：2011-09-22

    申请号：PCT/GB2011/050528

    申请日：2011-03-17

    申请人： SHIRE LLC ,  FRANKLIN, Richard ,  GOLDING, Bernard

    发明人： FRANKLIN, Richard ,  GOLDING, Bernard

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P7/02

    CPC分类号： C07D487/04

    摘要： This invention relates to the discovery of 5-substituted analogues of the selective platelet lowering agent anagrelide, which are extremely potent inhibitors of phosphodiesterase III (PDE III). The compounds are potentially useful agents for the treatment of conditions in which the inhibition of PDE III in beneficial. Formula (I): wherein: R 1 is independently selected form C 1-6 alkyl or C 1-6 haloalkyl; R 2 is selected from hydrogen, C 1-6 alkyl or C 1-6 haloalkyl; and X 1 and X 2 are each independently halo.

    摘要翻译： 本发明涉及选择性血小板降低剂阿那格雷的5-取代类似物的发现，其是磷酸二酯酶III（PDE III）的非常有效的抑制剂。 这些化合物是用于治疗有益于其中抑制PDE III的病症的潜在有用的药剂。 式（I）：其中：R 1独立地选自C 1-6烷基或C 1-6卤代烷基; R2选自氢，C 1-6烷基或C 1-6卤代烷基; X1和X2各自独立地为卤素。