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1. 发明申请

WO2009138792A1 SUBSTITUTED QUINAZOLINES 审中-公开
标题翻译：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。

2. 发明申请

WO2009147418A1 SUBSTITUTED QUINAZOLINES 审中-公开
标题翻译：取代的喹唑啉
公开(公告)号：WO2009147418A1
公开(公告)日：2009-12-10
申请号：PCT/GB2009/050516
申请日：2009-05-13
申请人： SHIRE LLC , GOLDING, Bernard , FRANKLIN, Richard , CICALA, Peter
发明人： GOLDING, Bernard , FRANKLIN, Richard , CICALA, Peter
IPC分类号： C07D239/84 , A61K31/517 , A61P7/02
CPC分类号： C07D239/84
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 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：本发明涉及选择性血小板降低剂阿那格雷的取代类似物的发现，其降低了心血管副作用的可能性，这将导致改善的患者依从性和治疗骨髓增殖性疾病的安全性。更具体地说，本发明涉及具有如下所示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，并且其在人类中具有作为血小板降低剂的用途。本发明的化合物通过抑制巨核细胞生成并因此形成血小板起作用。

3. 发明申请

WO2009138796A2 SUBSTITUTED QUINAZOLINES 审中-公开
标题翻译：取代的喹唑啉
公开(公告)号：WO2009138796A2
公开(公告)日：2009-11-19
申请号：PCT/GB2009/050517
申请日：2009-05-13
申请人： SHIRE LLC , GOLDING, Bernard, T. , FRANKLIN, Richard , MACLEOD, Angus , CICALA, Peter
发明人： GOLDING, Bernard, T. , FRANKLIN, Richard , MACLEOD, Angus , CICALA, Peter
IPC分类号： C07D487/04 , A61K31/5025 , A61P7/02
CPC分类号： C07D487/04
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 where 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。更具体地说，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（I）中所定义的含义：并且它们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。

4. 发明申请

WO2009138788A1 SUBSTITUTED QUINAZOLINES 审中-公开
标题翻译：取代的喹唑啉
公开(公告)号：WO2009138788A1
公开(公告)日：2009-11-19
申请号：PCT/GB2009/050508
申请日：2009-05-13
申请人： SHIRE LLC , GOLDING, Bernard , CICALA, Peter , FRANKLIN, Richard , MACLEOD, Angus
发明人： GOLDING, Bernard , CICALA, Peter , FRANKLIN, Richard , MACLEOD, Angus
IPC分类号： C07D239/84 , A61K31/517 , A61P7/02
CPC分类号： C07D239/84
摘要： This invention relates to the discovery of prodrugs of substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have the general formula (I) 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 the formation of blood platelets.
摘要翻译：本发明涉及降低选择性血小板降低剂阿那格雷的取代类似物的前药，其具有降低心血管副作用的潜力，因此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（I）的某些咪唑并喹唑啉衍生物的前药，其中取代基具有权利要求1中定义的含义，并且其可用作人血小板降低剂。本发明化合物通过抑制血小板的形成起作用。

5. 发明申请

WO2008022128A2 TRANSDERMAL DELIVERY OF MEPTAZINOL 审中-公开
标题翻译： MTATAZINOL的透皮递送
公开(公告)号：WO2008022128A2
公开(公告)日：2008-02-21
申请号：PCT/US2007/075902
申请日：2007-08-14
申请人： SHIRE PHARMACEUTICALS, INC. , FRANKLIN, Richard , CICALA, Peter
发明人： FRANKLIN, Richard , CICALA, Peter
IPC分类号： A61K9/70 , A61K31/55 , A61K9/00
CPC分类号： A61K9/7084
摘要： A delivery system for the delivery of a salt of meptazinol which increases the bioavailability of meptanizol by an effective amount to provide analgesic relief is disclosed. One embodiment of the delivery system is a transdermal device which increases the skin flux of meptazinol by an effective amount to provide analgesic relief. Also disclosed are methods of providing analgesic relief.
摘要翻译：公开了一种用于递送美普他酚盐的递送系统，该递送系统将美普唑醇的生物利用度提高了有效量以提供镇痛药缓解。递送系统的一个实施方案是透皮装置，其将美普他酚的皮肤通量增加有效量以提供止痛缓解。还公开了提供止痛缓解的方法。

6. 发明公开

EP2297159A2 SUBSTITUTED QUINAZOLINES 有权
标题翻译：取代的喹唑啉
公开(公告)号：EP2297159A2
公开(公告)日：2011-03-23
申请号：EP09746113.1
申请日：2009-05-13
申请人： Shire LLC
发明人： GOLDING, Bernard, T. , FRANKLIN, Richard , MACLEOD, Angus , CICALA, Peter
IPC分类号： C07D487/04 , A61K31/5025 , A61P7/02
CPC分类号： C07D487/04
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 where 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：本发明涉及选择性血小板降低剂阿那格雷的取代类似物的发现，其降低了心血管副作用的可能性，这将导致改善的患者依从性和治疗骨髓增殖性疾病的安全性。更具体地说，本发明涉及具有如下所示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）中定义的含义并且在人类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生成并因此形成血小板起作用。

7. 发明授权

EP2297159B1 SUBSTITUTED QUINAZOLINES 有权
标题翻译：取代Chinazolines
公开(公告)号：EP2297159B1
公开(公告)日：2012-08-15
申请号：EP09746113.1
申请日：2009-05-13
申请人： Shire LLC
发明人： GOLDING, Bernard, T. , FRANKLIN, Richard , MACLEOD, Angus , CICALA, Peter
IPC分类号： C07D487/04 , A61K31/5025 , A61P7/02
CPC分类号： C07D487/04
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 where 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.

8. 发明公开

EP2303849A1 SUBSTITUTED QUINAZOLINES 审中-公开
标题翻译：取代的喹唑啉
公开(公告)号：EP2303849A1
公开(公告)日：2011-04-06
申请号：EP09757790.2
申请日：2009-05-13
申请人： Shire LLC
发明人： GOLDING, Bernard , FRANKLIN, Richard , CICALA, Peter
IPC分类号： C07D239/84 , A61K31/517 , A61P7/02
CPC分类号： C07D239/84
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 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：本发明涉及选择性血小板降低剂阿那格雷的取代类似物的发现，其降低了心血管副作用的可能性，这将导致改善的患者依从性和治疗骨髓增殖性疾病的安全性。更具体地说，本发明涉及具有如下所示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，并且其在人类中具有作为血小板降低剂的用途。本发明的化合物通过抑制巨核细胞生成并因此形成血小板起作用。

9. 发明公开

EP2297146A1 SUBSTITUTED QUINAZOLINES 审中-公开
标题翻译：取代的喹唑啉
公开(公告)号：EP2297146A1
公开(公告)日：2011-03-23
申请号：EP09746109.9
申请日：2009-05-13
申请人： Shire LLC
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：本发明涉及选择性血小板降低剂阿那格雷的3-和5-取代类似物的发现，其降低了心血管副作用的可能性，这将导致改善的患者依从性和治疗骨髓增殖性疾病的安全性。更具体地说，本发明涉及具有如下所示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，并且其在人类中具有作为血小板降低剂的用途。本发明的化合物通过抑制巨核细胞生成并因此形成血小板起作用。

10. 发明公开

EP2297116A1 SUBSTITUTED QUINAZOLINES 审中-公开
标题翻译：取代的喹唑啉
公开(公告)号：EP2297116A1
公开(公告)日：2011-03-23
申请号：EP09746105.7
申请日：2009-05-13
申请人： Shire LLC
发明人： GOLDING, Bernard , CICALA, Peter , FRANKLIN, Richard , MACLEOD, Angus
IPC分类号： C07D239/84 , A61K31/517 , A61P7/02
CPC分类号： C07D239/84
摘要： This invention relates to the discovery of prodrugs of substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have the general formula (I) 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 the formation of blood platelets.
摘要翻译：本发明涉及选择性血小板降低剂阿那格雷的取代类似物的前体药物的发现，其降低了心血管副作用的可能性并且因此应该导致改善的患者依从性和治疗骨髓增殖性疾病的安全性。更具体地说，本发明涉及具有如下所示的通式（I）的某些咪唑并喹唑啉衍生物的前体药物，其中取代基具有权利要求1中定义的含义并且可用作人类血小板降低剂。本发明的化合物通过抑制血小板的形成起作用。

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