会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 5. 发明申请
    • SITAGLIPTIN INTERMEDIATE COMPOUNDS, PREPARATION METHODS AND USES THEREOF
    • SITAGLIPTIN中间体化合物,其制备方法及其用途
    • US20130012735A1
    • 2013-01-10
    • US13636486
    • 2011-03-22
    • Hongjun GaoMin Li
    • Hongjun GaoMin Li
    • C07C227/16C07C229/40C07C69/96
    • C07C68/06C07C68/065C07C69/96C07C227/18C07C229/24C07C229/34C07C269/04C07D487/04Y02P20/55C07C271/22
    • 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.
    • 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。
    • 8. 发明申请
    • FUNCTIONALIZED PHENOLIC ESTERS AND AMIDES AND POLYMERS THEREFROM
    • 功能化的酚醛和乳酸和聚合物
    • US20110130448A1
    • 2011-06-02
    • US12962195
    • 2010-12-07
    • Rao S. Bezwada
    • Rao S. Bezwada
    • A61K31/353C07C69/773C07C235/56C07C229/40C07C69/732C07D311/36A61K31/235A61K31/167A61K31/216A61P39/06A61P31/00A61P3/02A23L1/30A23L1/302
    • A61K31/192A61K31/353A61K31/405C07C69/734C07C69/92
    • 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.
    • 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。