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    BROMFENAC ORGANIC SALTS AND PREPARATION METHOD, COMPOSITION AND USE THEREOF
    4.
    发明申请
    BROMFENAC ORGANIC SALTS AND PREPARATION METHOD, COMPOSITION AND USE THEREOF 审中-公开
    BROMFENAC有机盐及其制备方法，组合物及其用途

    公开(公告)号：US20140039056A1

    公开(公告)日：2014-02-06

    申请号：US13994587

    申请日：2011-12-13

    申请人： Jidong Liu ,  Yuchun Yang ,  Jiuliang Wang ,  Hai Tang

    发明人： Jidong Liu ,  Yuchun Yang ,  Jiuliang Wang ,  Hai Tang

    IPC分类号： C07C229/40 ,  C07C227/14 ,  C07C213/08 ,  C07C215/40

    CPC分类号： C07C229/40 ,  A61K31/13 ,  A61K31/131 ,  A61K31/196 ,  C07C213/08 ,  C07C215/40 ,  C07C227/14

    摘要： Provided are bromfenac organic salts and preparation method, composition and use thereof. The bromfenac organic salt has the structure as shown in the following Formula I, wherein A represents an organic base. Also provided are a method for the preparation of the bromfenac organic salt, a composition comprising the bromfenac organic salts, a use of the bromfenac organic salts or the composition thereof in manufacture of a medicament for treatment and/or prophylaxis of an inflammation or for analgesia, and a method for treatment and/or prophylaxis of an inflammation or for analgesia.

    摘要翻译： 提供溴芬酸有机盐及其制备方法，组合物和用途。 溴芬酸有机盐具有如下式I所示的结构，其中A表示有机碱。 还提供了制备溴芬酸有机盐的方法，包含溴芬酸有机盐的组合物，溴芬酸有机盐或其组合物在制备用于治疗和/或预防炎症或镇痛的药物中的用途 ，以及治疗和/或预防炎症或镇痛的方法。

    SITAGLIPTIN INTERMEDIATE COMPOUNDS, PREPARATION METHODS AND USES THEREOF
    5.
    发明申请
    SITAGLIPTIN INTERMEDIATE COMPOUNDS, PREPARATION METHODS AND USES THEREOF 有权
    SITAGLIPTIN中间体化合物，其制备方法及其用途

    公开(公告)号：US20130012735A1

    公开(公告)日：2013-01-10

    申请号：US13636486

    申请日：2011-03-22

    申请人： Hongjun Gao ,  Min Li

    发明人： Hongjun Gao ,  Min Li

    IPC分类号： C07C227/16 ,  C07C229/40 ,  C07C69/96

    CPC分类号： C07C68/06 ,  C07C68/065 ,  C07C69/96 ,  C07C227/18 ,  C07C229/24 ,  C07C229/34 ,  C07C269/04 ,  C07D487/04 ,  Y02P20/55 ,  C07C271/22

    摘要： Sitagliptin intermediate compounds of formula (f) and methods of preparation and use thereof are disclosed. Compounds of formula (f) are prepared by the following steps: compounds of formula (a) are subjected to electrophilic reaction with benzyl halides to form compounds of formula (b), which then react with compounds of formula (i) to form novel compounds of formula (e). Gignard agents formed from 2,4,5-trifluoro brmobenzene and magnesium metal react with compounds of formula (e) to afford compounds of formula (f), which are novel intermediates for the preparation of Sitagliptin intermediates of formula (g). Compounds of formula (f) are subjected to reduction by Pd/C, debenzylation, substitution of protecting group to form compounds of formula (g). Compounds of formula (a), (b), (i), (e), (f), and (g) have the following structures, in which R is protecting group of carboxyl and R2 is (substituted) hydrocarbyl.

    摘要翻译： 公开了式（f）的西格列汀中间体化合物及其制备和使用方法。 通过以下步骤制备式（f）化合物：使式（a）化合物与苄基卤进行亲电子反应，形成式（b）化合物，然后与式（ⅰ）化合物反应形成新化合物 的式（e）。 由2,4,5-三氟Brmobenzene和镁金属形成的Gignard试剂与式（e）化合物反应，得到式（f）化合物，它们是制备式（g）的西他列汀中间体的新型中间体。 式（f）的化合物通过Pd / C进行还原，脱苄基，保护基的取代形成式（g）的化合物。 式（a），（b），（i），（e），（f）和（g）的化合物具有以下结构，其中R是保护基团的羧基，R 2是（取代的）烃基。

    FUNCTIONALIZED PHENOLIC ESTERS AND AMIDES AND POLYMERS THEREFROM
    8.
    发明申请
    FUNCTIONALIZED PHENOLIC ESTERS AND AMIDES AND POLYMERS THEREFROM 有权
    功能化的酚醛和乳酸和聚合物

    公开(公告)号：US20110130448A1

    公开(公告)日：2011-06-02

    申请号：US12962195

    申请日：2010-12-07

    申请人： Rao S. Bezwada

    发明人： Rao S. Bezwada

    IPC分类号： A61K31/353 ,  C07C69/773 ,  C07C235/56 ,  C07C229/40 ,  C07C69/732 ,  C07D311/36 ,  A61K31/235 ,  A61K31/167 ,  A61K31/216 ,  A61P39/06 ,  A61P31/00 ,  A61P3/02 ,  A23L1/30 ,  A23L1/302

    CPC分类号： A61K31/192 ,  A61K31/353 ,  A61K31/405 ,  C07C69/734 ,  C07C69/92

    摘要： The present invention relates to a compound of the formula: R-AR—O—Y—R′ Wherein R represents one or more members selected from H, alkoxy, benzyloxy, aldehyde, halogen, carboxylic acid, —NO2, —NH2, —NHCOCH3, and —NH—Y—R′, which is attached directly to AR or attached through an aliphatic chain. The carboxylic acid moiety in R includes but is not limited to the following carboxylic acids: benzoic acids, cinnamic acids, ferulic acid, caffeic acid, syringic acid, salicyclic acid, vanillic acid, phenylacetic acids, phenylpropionic acids, and sinapinic acid. -AR—O— is a biologically active phenolic moiety comprising 1 to 6 substituted or unsubstituted aryl rings that are directly bonded to each other, fused together, or joined through a linking group. Y represents a member selected from: —COCH2O— (glycolic ester moiety) —COCH(CH3)O— (lactic ester moiety) —COCH2OCH2CH2O— (dioxanone ester moiety) —COCH2CH2CH2CH2CH2O— (caprolactone ester moiety) —CO(CH2)mO— where m is an integer between 2-4 and 6-24 inclusive —COCH2—O—(CH2CH2O)n— where n is an integer between 2 and 24, inclusive; and R′ is either hydrogen or a benzyl or an alkyl group, the alkyl group being either straight-chained or branched. The resultant functionalized phenolic compounds, used singly or in combinations, and their polymers have controllable degradation profiles, releasing the active component over a desired time range. The polymers are useful for biomaterials and biomedical devices, wherein said biologically active phenolic moiety is a residue of a phenolic compound.

    摘要翻译： 本发明涉及式R-AR-O-Y-R'的化合物，其中R代表一个或多个选自H，烷氧基，苄氧基，醛，卤素，羧酸，-NO 2，-NH 2， NHCOCH 3和-NH-Y-R'，其直接连接到AR或通过脂族链连接。 R中的羧酸部分包括但不限于以下羧酸：苯甲酸，肉桂酸，阿魏酸，咖啡酸，丁香酸，水杨酸，香草酸，苯乙酸，苯基丙酸和芥子酸。 -AR-O-是包含1至6个取代或未取代的芳环的生物活性酚部分，其直接键合，稠合在一起或通过连接基团连接。 Y表示选自-COCH 2 O-（乙醇酸酯部分）-COCH（CH 3）O-（乳酸酯部分）-COCH 2 OCH 2 CH 2 O-（二氧杂环己酮酯部分）-COCH 2 CH 2 CH 2 CH 2 CH 2 O-（己内酯部分）-CO（CH 2）m O- 其中m是2-4和6-24之间的整数，包括-COCH 2 -O-（CH 2 CH 2 O）n - ，其中n是2和24之间的整数，包括端值; 并且R'是氢或苄基或烷基，烷基是直链或支链的。 所得到的单独或组合使用的官能化酚类化合物及其聚合物具有可控的降解特征，在期望的时间范围内释放活性组分。 聚合物可用于生物材料和生物医学装置，其中所述生物活性酚部分是酚类化合物的残基。