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    • 1. 发明申请
    • TREATMENT OF INFLAMMATORY DISORDERS
    • 治疗炎症性疾病
    • WO2006074192A2
    • 2006-07-13
    • PCT/US2006000132
    • 2006-01-03
    • BIONAUT PHARMACEUTICALS INCAN WENQIAN FRANKPARK JUN YOUNGKHODADOUST MEHRANHESS HANS-JURGENHUSSOIN MD SAJJAT
    • AN WENQIAN FRANKPARK JUN YOUNGKHODADOUST MEHRANHESS HANS-JURGENHUSSOIN MD SAJJAT
    • A61K31/203A61K31/05A61K31/09A61K31/165A61K31/19A61K31/343A61K31/365A61K31/366A61K31/37A61K31/415A61K31/428A61K31/498A61K31/517A61K31/56A61K31/57C07F9/12
    • Methods of treating an inflammatory disorder include administering an effective amount of a compound represented by Structural Formula (I). Ring A is optionally substituted, contains zero, one, two, or three double bonds, and is optionally fused to an aliphatic, aryl or heteroaryl ring; X is an optionally substituted 1 to 3 carbon aliphatic chain that is optionally fused to a monocyclic, optionally substituted, aliphatic, heterocyclic, aryl, or heteroaryl ring, wherein one or two carbons in X are optionally replaced with -O-, -S-, or -NR e -; Y is carbon or nitrogen; R 1 and R 2 are independently -H, -OH, -CN, -NO 2 , -NR f R g , halogen, optionally substituted alkyl, or optionally substituted alkoxy; or R 1 and R 2 together link the carbons to which they are bonded with a bond, -O-, -S-, or -NR h -; R 3 and R 4 are independently -H, -OH, -CN, -NO 2 , -NR i R j , halogen, optionally substituted alkyl, or optionally substituted alkoxy, or R 4 is =0; or R 3 and R 4 , taken together with the atoms to which they are bonded, form a monocyclic, optionally substituted, aliphatic, heterocyclic, aryl, or heteroaryl ring that is optionally fused to a monocyclic or bicyclic, optionally substituted, aliphatic, heterocyclic, aryl, or heteroaryl ring; R e -R j are independently -H or optionally substituted alkyl; and each of the OSM signaling inhibitor compounds has at least one hydrogen atom bonded to an oxygen, nitrogen, or sulfur atom. The OSM signaling inhibitor compounds also include pharmaceutically acceptable salt or solvates of the compounds represented by Structural Formula (I).
    • 治疗炎性病症的方法包括施用有效量的结构式(I)表示的化合物。 环A任选被取代,含有0,1,2或3个双键,并且任选地与脂族,芳基或杂芳基环稠合; X是任选被1至3个碳的脂族链,其任选地与单环,任选取代的脂族,杂环,芳基或杂芳基环稠合,其中X中的一个或两个碳任选被-O-,-S- ,或-NR e - Y是碳或氮; R 1和R 2独立地是-H,-OH,-CN,-NO 2,-NR f, 卤素,任选取代的烷基或任选取代的烷氧基; 或R 1和R 2 2一起连接与它们键合的碳键,-O-,-S-或-NR“ SUP> - ; R 3和R 4独立地是-H,-OH,-CN,-NO 2,-NR O, 卤素,任选取代的烷基或任选取代的烷氧基,或R 4是= O; 或R 3和R 4与它们所键合的原子一起形成单环,任选取代的脂族,杂环,芳基或杂芳基环,其是 任选地与单环或双环,任选取代的脂族,杂环,芳基或杂芳基环稠合; R e独立地是-H或任选取代的烷基; 并且每个OSM信号传导抑制剂化合物具有至少一个与氧,氮或硫原子键合的氢原子。 OSM信号传导抑制剂化合物还包括由结构式(I)表示的化合物的药学上可接受的盐或溶剂合物。
    • 4. 发明申请
    • USE OF NA+/ K+-ATPASE INHIBITORS AND ANTAGONISTS THEREOF
    • 使用NA + / K + -ATPASE抑制剂及其拮抗剂
    • WO2006044916A3
    • 2007-01-04
    • PCT/US2005037486
    • 2005-10-18
    • BIONAUT PHARMACEUTICALS INCKHODADOUST MEHRANSHARMA AJAY
    • KHODADOUST MEHRANSHARMA AJAY
    • A61K31/56
    • A61K31/56A61K31/58A61K31/704A61K31/7048
    • The reagent, pharmaceutical formulation, kit, and methods of the invention provides a new approach for treating hypoxia-related pathological conditions, such as Alzheimer's Disease, and those involving excessive angiogenesis, especially those non-­cancer pathological conditions. The invention provides the use of Na + /K + -ATPase inhibitors, such as cardiac glycosides (e.g. ouabain and proscillaridin, etc.), either alone or in combination with other standard therapeutic agents for treating such conditions. The invention also relates to the use of cardiac glycoside inhibitors / antagonists as reagents, pharmaceutical formulations, or in kits and methods for treating conditions arising from excessive amount of cardiac glycosides, including all symptoms of digitalis poisoning, depression, hypertension, etc. The pharmaceutical formulation of the invention may be delivered to a patient either systemically or locally, or both. The pharmaceutical formulations of the invention may be delivered either in one dose, or continuously over a sustained period of time using, for example, sustained drug delivery devices.
    • 本发明的试剂,药物制剂,试剂盒和方法提供了治疗缺氧相关病理状况(例如阿尔茨海默病)和涉及过度血管生成的那些的新方法,特别是那些非癌症病理状况。 本发明提供单独使用或与其它组合使用的Na + + / K + + / - ATP酶抑制剂,例如强心苷(例如哇巴因和前列腺素等) 用于治疗这些病症的标准治疗剂。 本发明还涉及使用强心苷抑制剂/拮抗剂作为试剂,药物制剂,或用于治疗由过量的强心苷引起的病症的试剂盒和方法,包括洋地黄中毒,抑郁症,高血压等所有症状。药物 本发明的制剂可以全身或局部地递送到患者,或两者。 本发明的药物制剂可以使用例如持续的药物递送装置以一个剂量或持续的时间段连续递送。