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    • 2. 发明授权
    • Vented, flexible, thin chemiluminescent device
    • 通风,灵活,薄化学发光装置
    • US5226710A
    • 1993-07-13
    • US922432
    • 1992-07-30
    • Robert D. GigliaWilliam E. BayKevin Nolan
    • Robert D. GigliaWilliam E. BayKevin Nolan
    • F21K2/06
    • F21K2/06
    • There is provided a flexible, thin, chemiluminescent device comprised of a back sheet having sealed thereto at its edges a windowed front sheet, separation means to divide the internal cavity into a larger and a smaller compartment, the larger compartment containing a contents-releasable receptacle for one part of a two-part chemiluminescent composition and an absorbent material in the larger compartment containing the second part of the composition external to the receptacle, the smaller compartment forming an exit passageway for gases, being in open communication with the larger compartment at its upstream end, and open to the atmosphere through a vent at its downstream end, whereby gases generated during storage and use can exit harmlessly without distorting or inflating the device. The smaller compartment may contain a gas porous component which acts to separate residual liquid from escaping gas thereby preventing unwanted liquid leakage from the chemiluminescent device.
    • 提供了一种柔性,薄的化学发光装置,其包括在其边缘处密封有窗口的前片的背片,将内腔分成更大和更小的隔室的分离装置,较大的隔间含有可释放内容物的容器 对于两部分化学发光组合物的一部分和在容纳在容器外部的组合物的第二部分的较大隔间中的吸收材料,较小的隔室形成用于气体的出口通道, 上游端,并通过其下游端的通风口向大气敞开,由此在储存和使用期间产生的气体可以无害地退出,而不会使设备变形或膨胀。 较小的隔室可以包含气体多孔组分,其用于将残留液体与逸出气体分离,从而防止不希望的液体从化学发光装置泄漏。
    • 4. 发明申请
    • DISODIUM SALTS, MONOHYDRATES, AND ETHANOL SOLVATES FOR DELIVERING ACTIVE AGENTS
    • 用于递送活性剂的二盐,单酯和乙醇溶剂
    • US20110251125A1
    • 2011-10-13
    • US13053641
    • 2011-03-22
    • William E. BayRajesh K. AgarwalKiran ChaudharyShingai MajuruMichael M. GoldbergJoanne P. CorvinoMoise AzriaJoseph M. AultSimon D. BatemanSubash PatelJoseph SikoraRebecca F. YangJoseph L. Zielinski
    • William E. BayRajesh K. AgarwalKiran ChaudharyShingai MajuruMichael M. GoldbergJoanne P. CorvinoMoise AzriaJoseph M. AultSimon D. BatemanSubash PatelJoseph SikoraRebecca F. YangJoseph L. Zielinski
    • A61K38/23
    • C07C231/00A61K9/2013A61K47/183C07C235/60C07D265/26C07C235/58
    • The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substituted or unsubstituted C2-C16alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above. The invention also provides a hydrate of a disodium salt of a delivery agent of the formula above. Preferred delivery agents include, but are not limited to, N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC), N-(10-[2-hydroxybenzoyl]amino)decanoic acid (SNAD), and sodium N-(8-[2-hydroxybenzoyl]amino)caprylate (SNAC). The invention also provides methods of preparing the disodium salt, ethanol solvate, and hydrate and compositions containing the disodium salt, ethanol solvate, and/or hydrate.
    • 发明人已经发现,某些递送剂的二钠盐比相应的单钠盐具有惊人的更大的递送活性剂的功效。 此外,本发明人已经发现,这些递送剂的二钠盐与乙醇形成溶剂合物并与水合。 递送剂具有下式:其中R 1,R 2,R 3和R 4独立地是氢,卤素,C 1 -C 4烷基或C 1 -C 4烷氧基; 取代或未取代的C 2 -C 16亚烷基,取代或未取代的C 1 -C 12烷基(亚芳基)或取代或未取代的芳基(C 1 -C 12亚烷基)。 本发明的水合物和溶剂合物对于递送活性剂(例如肝素和降钙素)比其相应的单钠盐和游离酸具有惊人的更大的功效。 本发明提供了一种醇溶剂合物,例如乙醇溶剂化物,其具有上式的递送剂的二钠盐。 本发明还提供了上式的递送剂的二钠盐的水合物。 优选的递送剂包括但不限于N-(5-氯水杨酰基)-8-氨基辛酸(5-CNAC),N-(10- [2-羟基苯甲酰基]氨基)癸酸(SNAD)和N - (8- [2-羟基苯甲酰基]氨基)辛酸酯(SNAC)。 本发明还提供了制备二钠盐,乙醇溶剂合物和水合物的方法以及含有二钠盐,乙醇溶剂化物和/或水合物的组合物。
    • 10. 发明授权
    • Method of preparing salicylamides
    • 制备水杨酰胺的方法
    • US07262325B2
    • 2007-08-28
    • US10297156
    • 2001-06-04
    • William E. BayJoAnne P. Corvino
    • William E. BayJoAnne P. Corvino
    • C07C231/02C07C233/65
    • C07C231/02C07C231/08C07C235/60
    • The present invention provides a fast, high yield method for preparing salicylamide intermediates. The method comprises reacting a C4 or higher alkyl ester of salicylic acid or derivative thereof with at least one amine selected from the group consisting of monoalkylamines, dialkylamines, ammonia, and any combination of any of the foregoing in alcohol to yield the salicylamide. The C4 or higher alkyl ester of salicylic acid or a derivative thereof is preferably prepared by reacting salicylic acid or a derivative thereof with a C4 or higher alcohol in presence of at least one of sulfuric acid, a sulfonic acid, and a mineral acid. This process for preparing salicylamide intermediates from salicylic acid or derivative thereof generally has a cycle time of about 2 days, and yields about 95% of a 99% pure material. In comparison, when a C3 or lower alkyl ester is used in lieu of the C4 or higher alkyl ester, the process generally has a cycle time of 7–9 days and yields about 60% of a 95% pure material. Methods of preparing an alkylated salicylamide are also provided.
    • 本发明提供了制备水杨酰胺中间体的快速,高产率的方法。 该方法包括使水杨酸或其衍生物的C 4或更高级烷基酯与选自单烷基胺,二烷基胺,氨的至少一种胺和上述任何一种的任何组合 酒精产生水杨酰胺。 水杨酸的C 4或更高级烷基酯或其衍生物优选通过使水杨酸或其衍生物与C 4或更高级醇在at 硫酸,磺酸和无机酸中的至少一种。 从水杨酸或其衍生物制备水杨酰胺中间体的方法通常具有约2天的循环时间,并且产生约95%的纯度为99%的物质。 相比之下,当使用C 3或低级烷基酯代替C 4或更高级烷基酯时,该方法通常具有7-9天的循环时间 并产生约60%的95%纯物质。 还提供了制备烷基化水杨酰胺的方法。