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    • 8. 发明授权
    • &mgr;-Selective opioid peptides
    • mu-选择性阿片肽
    • US06337319B1
    • 2002-01-08
    • US08718585
    • 1996-10-02
    • Wuyi Wang
    • Wuyi Wang
    • A61K3807
    • C07K5/1027A61K38/00C07K5/1016
    • This invention relates to novel opioid peptides for the treatment of pain as well as a method for the preparation thereof and pharmaceutically acceptable compositions comprising these peptides. The invention also relates to methods for controlling pain in patients using compositions of the invention and the use of said compounds in the preparation of formulations effective in pain treatment. The peptides of this invention have a high degree of selectivity for the &mgr;-opioid receptor. The peptides of the present invention are particularly well-suited as analgesic agents acting substantially on peripheral &mgr;-opioid receptors. Because these peptides act peripherally, they substantially avoid producing side effects normally associated with central analgesic action.
    • 本发明涉及用于治疗疼痛的新型阿片类肽以及其制备方法和包含这些肽的药学上可接受的组合物。 本发明还涉及使用本发明组合物治疗患者疼痛的方法以及所述化合物在制备有效治疗疼痛的配方中的用途。 本发明的肽对μ-阿片受体具有高度的选择性。 本发明的肽特别适合作为基本上作用于外周mu-阿片受体的止痛剂。 因为这些肽在外周作用,它们基本上避免产生通常与中枢镇痛作用相关的副作用。
    • 9. 发明授权
    • Method and apparatus for rapidly cooling a gem, including two stage cooling
    • 用于快速冷却宝石的方法和装置,包括两级冷却
    • US08477293B2
    • 2013-07-02
    • US12380445
    • 2009-02-27
    • Matt HallRen LuWuyi Wang
    • Matt HallRen LuWuyi Wang
    • G01N21/00
    • F25B19/005F25D3/10F25D19/006G01N21/0332G01N21/31G01N21/3563G01N21/87G01N2021/0335G01N2021/3155G01N2201/065
    • A cooling apparatus includes a container configured to contain a coolant within a space. The apparatus further includes a cooling block positioned substantially within the space and having a high heat capacity such that the space not occupied by the cooling block is filled with a coolant to a level at or below the top of the cooling block, and a placement structure having high thermal conductivity positioned on top of the cooling block and outside of the space. A method for cooling an object is also provided, which includes inserting a coolant into a container configured to contain the coolant within a space, and placing the object on a placement structure outside the space. For this method, the placement structure has a high thermal conductivity and is coupled to a cooling block, the cooling block having a high heat capacity and positioned substantially within the space. A two-stage cooling apparatus and method is also described.
    • 一种冷却装置包括:容器,其构造成在空间内容纳冷却剂。 该装置还包括基本上位于该空间内并且具有高热容量的冷却块,使得未被冷却块占据的空间用冷却剂填充到冷却块的顶部或下方的水平面,以及放置结构 具有高的导热性位于冷却块的顶部并且位于空间外部。 还提供了一种用于冷却物体的方法,其包括将冷却剂插入构造成在空间内容纳冷却剂的容器中,并将物体放置在空间外部的放置结构上。 对于该方法,放置结构具有高导热性并且耦合到冷却块,该冷却块具有高的热容并且基本位于该空间内。 还描述了两级​​冷却装置和方法。
    • 10. 发明申请
    • Process for preparation of pentostatin (R)-3-(2-Deoxy-beta-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidaz[4,5-d][1,3] diazepin-8-ol
    • 制备喷他他汀(R)-3-(2-脱氧-β-D-赤型 - 呋喃戊糖基)-3,6,7,8-四氢咪唑并[4,5-d] [1,3]二氮杂-8- ol
    • US20090012288A1
    • 2009-01-08
    • US11822177
    • 2007-07-03
    • Hai-Ren ZhangWuyi Wang
    • Hai-Ren ZhangWuyi Wang
    • C07D473/00
    • C07D487/04
    • In a process for preparing pentostatin, the improvement wherein reduction is performed on ketone prior to deprotection, comprising: a) reacting 3-(2-deoxy-3,5-di-O-p-toluoyl-b-D-erythro-pentofuranosyl)-6,7-dihydroimidazol [4,5-d][1,3] diazepin-8 (3H)-one with a ruthenium catalyst formed by the reaction of di-μ-chlorobis[(p-cymene) chlororuthenium (II) and N-(arylsulfonyl)-1,2-diarylethylene diamine in a solvent; b) stopping the reaction in step a) by making the reaction medium alkaline; c) separating the mixture from step b) into combined organic layers and washing the reaction product from the combined organic layers with water, filtering, and evaporating solvent to provide a crude product, wherein the ratio of 8R vs 8S isomeric alcohol >100; d) purifying said crude product by chromatography; e) deprotecting the keto nucleoside in the crude product in methanol/sodium methoxide to obtain pentostatin; and f) purifying by recrystallizing pentostatin from methanol to remove inorganic and isomeric impurities.
    • 在制备喷司他丁的方法中,其改进在于在脱保护之前还原在酮上进行,包括:a)使3-(2-脱氧-3,5-二 - 对甲苯酰基-bD-赤型 - 戊呋喃糖基) 通过二氯双[(对甲基异丙基苯)氯钌(II)和N-甲基苯甲酰胺反应形成的钌催化剂,将7-二氢咪唑并[4,5-d] [1,3]二氮杂-8(3H) (芳基磺酰基)-1,2-二亚乙基二胺在溶剂中; b)在步骤a)中停止反应,使反应介质呈碱性; c)将步骤b)中的混合物分离成合并的有机层,并从合并的有机层中用水,过滤和蒸发溶剂洗涤反应产物,得到粗产物,其中8R与8S异构醇的比> 100; d)通过色谱纯化所述粗产物; e)将甲醇/甲醇钠中的粗产物中的酮基核苷脱保护,得到喷司他丁; 和f)通过从甲醇中重结晶pentostatin来除去无机和异构杂质的纯化。