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1. 发明公开

EP1857443A2 Therapeutic morpholino-substituted compounds 有权
标题翻译：治疗吗啉取代物Verbindungen
公开(公告)号：EP1857443A2
公开(公告)日：2007-11-21
申请号：EP07009194.7
申请日：2001-01-24
申请人： AstraZeneca AB
发明人： Robertson, Alan D. , Jackson, Shaun , Kenche, Vijaya , Yaip, Cindy , Parbaharan, Hishani , Thompson, Phil
IPC分类号： C07D215/38 , C07D311/58 , C07D471/04 , A61K31/352 , A61K31/473 , A61K31/505 , A61P9/00 , A61P11/00 , A61P11/06 , A61P35/00 , C07D311/64
CPC分类号： C07D215/38 , C07D311/22 , C07D311/58 , C07D311/64 , C07D471/04
摘要： Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a cansequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation. The compounds are useful in treating PI 3-kinase-dependent conditions including cardiovascular diseases such as coronary artery occlusion, stroke, acute coronary syndrome, acute myocardial infarction, vascular restenasis, atherosclerosis, and unstable angina; respiratory diseases such as asthma, chronic obstructive pulmonary diseases (COPD), and bronchitis; inflammatory disorders; neoplasms including cancers such as glioma, prostate cancer, small cell lung cancer, and breast cancer; and diseases linked to disordered white blood cell function, such as autoimmune and inflammatory diseases.
摘要翻译：吗啉代取代的吡啶并嘧啶，喹诺酮和苯并吡喃酮衍生物抑制磷酸肌醇（PI）3-激酶，其是调节血小板粘附过程的酶。作为可能的结果，所讨论的化合物具有抗血栓形成活性以及其它药物性质。 PI 3激酶产生在血液流动条件下刺激血小板粘附的3-磷酸化PI第二信使。由于血小板粘附是形成血栓的必要步骤，所以这些条件下这些PI3-激酶化合物的抑制可抑制或预防血栓形成。该化合物可用于治疗PI 3激酶依赖性疾病，包括心血管疾病如冠状动脉闭塞，中风，急性冠状动脉综合征，急性心肌梗塞，血管再狭窄，动脉粥样硬化和不稳定性心绞痛; 呼吸系统疾病如哮喘，慢性阻塞性肺疾病（COPD）和支气管炎; 炎症性疾病; 肿瘤包括癌症如胶质瘤，前列腺癌，小细胞肺癌和乳腺癌; 以及与无序白细胞功能相关的疾病，如自身免疫性疾病和炎性疾病。

2. 发明授权

EP1857443B1 Therapeutic morpholino-substituted compounds 有权
标题翻译：治疗性吗啉代取代的化合物
公开(公告)号：EP1857443B1
公开(公告)日：2012-03-28
申请号：EP07009194.7
申请日：2001-01-24
申请人： AstraZeneca AB
发明人： Robertson, Alan D. , Jackson, Shaun, Australian Centre for Blood Diseases, Monash University , Kenche, Vijaya , Yaip, Cindy , Parbaharan, Hishani , Thompson, Phil
IPC分类号： C07D215/38 , C07D311/58 , C07D471/04 , A61K31/352 , A61K31/473 , A61K31/505 , A61P9/00 , A61P11/00 , A61P11/06 , A61P35/00 , C07D311/64
CPC分类号： C07D215/38 , C07D311/22 , C07D311/58 , C07D311/64 , C07D471/04

3. 发明公开

EP1857443A3 Therapeutic morpholino-substituted compounds 有权
标题翻译：治疗性吗啉代取代的化合物
公开(公告)号：EP1857443A3
公开(公告)日：2007-12-26
申请号：EP07009194.7
申请日：2001-01-24
申请人： AstraZeneca AB
发明人： Robertson, Alan D. , Jackson, Shaun, Australian Centre for Blood Diseases, Monash University , Kenche, Vijaya , Yaip, Cindy , Parbaharan, Hishani , Thompson, Phil
IPC分类号： C07D215/38 , C07D311/58 , C07D471/04 , A61K31/352 , A61K31/473 , A61K31/505 , A61P9/00 , A61P11/00 , A61P11/06 , A61P35/00 , C07D311/64
CPC分类号： C07D215/38 , C07D311/22 , C07D311/58 , C07D311/64 , C07D471/04
摘要： Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a cansequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation. The compounds are useful in treating PI 3-kinase-dependent conditions including cardiovascular diseases such as coronary artery occlusion, stroke, acute coronary syndrome, acute myocardial infarction, vascular restenasis, atherosclerosis, and unstable angina; respiratory diseases such as asthma, chronic obstructive pulmonary diseases (COPD), and bronchitis; inflammatory disorders; neoplasms including cancers such as glioma, prostate cancer, small cell lung cancer, and breast cancer; and diseases linked to disordered white blood cell function, such as autoimmune and inflammatory diseases.

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