摘要:
The present invention relates to selective inhibitors of phosphoinositide (PI) 3-kinase β, use of the selective inhibitors in anti-thrombotic therapy, and a method for screening compounds useful for the new anti-thrombotic therapy by detecting selective inhibitory activity of PI 3-kinase β of the compound. The invention also relates to novel compounds that are inhibitors of PI 3-kinase.
摘要:
Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). 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 restenosis, 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。 因此,所讨论的化合物具有抗血栓形成活性以及其它药物性质。 所要求的化合物由式(I),(II)和(III)表示。 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。 因为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型心绞痛; 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,包括癌症如神经胶质瘤,前列腺癌,小细胞肺癌和乳腺癌的肿瘤,以及与无序白细胞功能如自身免疫性和炎性疾病相关的疾病。
摘要:
Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). 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 restenosis, 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:
Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). 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 restenosis, 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:
Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). 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 restenosis, 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:
Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). 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 restenosis, 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。 因此,所讨论的化合物具有抗血栓形成活性以及其它药物性质。 所要求的化合物由式(I),(II)和(III)表示。 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。 因为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型心绞痛; 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,包括癌症如神经胶质瘤,前列腺癌,小细胞肺癌和乳腺癌的肿瘤,以及与无序白细胞功能如自身免疫性和炎性疾病相关的疾病。
摘要:
Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). 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 restenosis, 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:
The present invention relates to enantiomerically pure (−) 2-[1-(7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl)ethylamino]benzoic acid or pharmaceutically acceptable salts thereof, it being in a solid state, its use in medical therapy, pharmaceutical composition comprising it, its use in the preparation of a medicament for use in a method for preventing or treating diseases, and its use in method for preventing or treating disease. The present invention relates to a selective inhibitor of phosphoinositide (PI) 3-kinase β and use of the selective inhibitor in e.g. anti-thrombotic therapy.
摘要:
A case configured to enclose a portable electronic device includes a plurality of externally accessible electrical contacts, enabling electrical current to flow to or from the device while enclosed in the case. The invention is applicable to all types of portable devices, including laptop, notebook and palm-top computers, as well as telecommunications devices, video players and music players. Typically the electrical contacts allow a battery in the case or in the device to be recharged while device is enclosed. An adaptor cable may be provided between the device and the electrical contacts so that the same or similar case may be used with different model devices from different manufacturers. For greater ‘universality,’ a voltage-changing adaptor cable may be provided within the case between the device and the electrical contacts. The system may further include a docking bay to receive the case, the docking bay having a set of electrical contacts configured to electrically engage with the contacts on the case. Such a docking bay may take the form of a charging stand, a cart with one or more slots or compartments, or a locker with a door and a storage compartment.
摘要:
The field of the invention relates to methods for dissolving a thrombus using inhibitors of platelet contractility. More particularly, the present invention relates to the use of an inhibitor of platelet contractility in combination with one or more thrombolytic agents and optionally one or more anticoagulants for inhibiting platelet contraction and consolidation in the developing thrombus.