摘要:
The present invention relates to the use of adenosine receptor agonists, preferably A3 receptor agonists, either alone or in combination with other agents for the treatment, prevention and/or management of diseases or disorders associated with under-expression of HIF-1α and/or decreased HIF-1 α activity (e.g., ischemic related disorders). The methods of the invention are directed to methods of reducing tissue damage (e.g., substantially prevention tissue damage, inducing tissue protection) resulting from ischemia orhypoxia. The invention provides methods for treating, preventing and/or ameliorating one or more symptoms of hypoxic or HIF-1α related disorders by administering an A3 receptor agonist either alone or in combination with other agents.
摘要翻译:本发明涉及腺苷受体激动剂,优选A 3 N 3受体激动剂,单独使用或与其它药剂组合用于治疗,预防和/或控制与低血糖相关的疾病或病症, HIF-1α的表达和/或降低的HIF-1α活性(例如缺血性相关疾病)。 本发明的方法涉及减少由局部缺血或缺氧引起的组织损伤(例如,基本上预防组织损伤,诱导组织保护)的方法。 本发明提供了通过单独或与其它药剂组合施用A 3 O 3受体激动剂来治疗,预防和/或改善一种或多种缺氧或HIF-1α相关疾病症状的方法。
摘要:
The present invention relates to the use of adenosine receptor antagonists, preferably A3 receptor antagonists, either alone or in combination with other agents for the treatment, prevention and/or management of diseases or disorders associated with overexpression of HIF-1α and/or increased HIF-1α activity (e.g., cancer, respiratory disease). The methods and compositions of the invention are particularly useful for preventing, treating, or ameliorating symptoms associated with a cancer, disease or disorder associated with hypoxia-inducible factor 1α (HIF-1α) using the A3 receptor antagonists of the invention. The present invention provides methods to inhibit the growth of tumors, particularly solid tumors and more particularly hypoxic tumors.
摘要:
The present invention discloses the use of high affinity adenosine A3 receptor antagonists for enhancing chemotherapeutic treatment of cancers expressing adenosine A3 receptors and cancers expressing P-glycoprotein or MRP. In preferred embodiments, adenosine A3 receptor antagonists are administered before or during administration of a taxane family, vinca alkaloid, camptothecin or antibiotic chemotherapeutic agent.
摘要翻译:本发明公开了高亲和力腺苷A 3 N 3受体拮抗剂用于增强表达腺苷A 3 N受体和表达P-糖蛋白或MRP的癌症的癌症的化学治疗的用途。 在优选的实施方案中,腺苷A 3受体拮抗剂在紫杉烷类家族,长春花生物碱,喜树碱或抗生素化学治疗剂施用之前或期间施用。
摘要:
The invention relates to the diagnosis and prognosis of solid tumors and melanoma by detecting increased cellular levels of A3 receptors in tissue and/or leukocytes obtained from patients with cancer or patients at risk for developing cancer.
摘要:
Tumor growth and metastasis can be inhibited by administration of adenosine A1 and/or A3 antagonists, preferably A3 antagonists, to a patient. The antagonists can be, and preferably are, administered in combination with other anti-tumor agents, such as anti-angiogenic agents (including adenosine A2a antagonists) and/or cytotoxic agents. Because the cytotoxic agents attack the tumor cells themselves, and the anti-angiogenic agents prevent the growth of vasculature which would otherwise support the growth of the tumor cells.
摘要:
A method of and a formulation for treating hyper-excited sensory nerve functions are provided. The method comprises administering to a patient in need of treatment thereof a pharmaceutical composition comprising an effective amount of 2-Amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)(4-chlorophenyl) methanone or a pharmaceutically acceptable salt thereof. The disorder treated include hyperesthesia, dysesthesia, allodynia, hyperalgesia, tinnitus, ganglionic dysfunction and combinations thereof. The co-administration of adenosine is not needed. The pharmaceutical preparation is suitable for oral administration. The pharmaceutical preparation is useful in the reduction of neuropathic pain in a conscious human. The use of the pharmaceutical preparation does not result in medically adverse cardiovascular symptoms associated with administration of adenosine.
摘要:
The present invention discloses the use of high affinity adenosine A3 receptor antagonists for enhancing chemotherapeutic treatment of cancers expressing adenosine A3 receptors and cancers expressing P-glycoprotein or MRP. In preferred embodiments, adenosine A3 receptor antagonists are administered before or during administration of a taxane family, vinca alkaloid, camptothecin or antibiotic chemotherapeutic agent.
摘要:
Provided is a method for the synthesis of an aralkyloxyadenosine or an alkoxyadenosine. The method includes protecting the hydroxyl sugar groups with a protecting group to produce a protected halogenated adenosine. The protected halogenated adenosine is alkoxylated, and the hydroxyl sugar groups of the protected halogenated adenosine are deprotected to provide the aralkyloxyadenosine or alkoxyadenosine.
摘要:
The present invention relates to pharmaceutical compositions and methods for promoting wound healing. The invention also relates to methods of making pharmaceutical compositions disclosed herein. Pharmaceutical compositions are disclosed comprising an effective amount of a 2-alkoxyadenosine or 2-aralkoxyadenosine, about 10% to about 70% w/w propylene glycol and a thickening agent.
摘要:
The present invention relates to adenosine A3 receptor antagonists and their use for the prevention and treatment of atherosclerosis by administering to a mammal, in need thereof, a therapeutically effective amount of an adenosine A3 receptor antagonist, or a pharmaceutically acceptable salt thereof, alone or in combination with other anti-atherosclerotic agents.