Plant extract and the process for treating hepatic fibrosis and liver cancer
    34.
    发明授权
    Plant extract and the process for treating hepatic fibrosis and liver cancer 有权
    植物提取物和治疗肝纤维化和肝癌的过程

    公开(公告)号:US09474777B2

    公开(公告)日:2016-10-25

    申请号:US14144264

    申请日:2013-12-30

    CPC classification number: A61K36/41 A61K2236/00

    Abstract: An extract of Graptopetalum paraguayense prepared by a method that includes: extracting a Graptopetalum paraguayense (GP) starting material with an alcoholic solvent to produce an alcoholic extract and a residue; separating the residue from the alcoholic extract; extracting the residue with an aqueous dimethyl sulfoxide (DMSO) solvent to produce a DMSO extract; subjecting the DMSO extract to ultrafiltration using a filter having a selected molecular weight cutoff; drying a fraction retained by the filter to obtain the extract of Graptopetalum paraguayense. Uses of an extract of Graptopetalum paraguayense for the treatment or prevention of liver fibrosis, hepatic cirrhosis, liver cancer, recurrence of liver fibrosis after surgery, or recurrence of liver cancer after surgery.

    Abstract translation: 通过包括以下方法制备的Graptopetalum巴拉圭的提取物包括:用醇溶剂萃取Graptopetalum巴拉圭(GP)起始原料以产生醇提取物和残余物; 从酒精提取物中分离残留物; 用二甲基亚砜(DMSO)水溶液萃取残余物,得到DMSO提取物; 使用具有选择的分子量截止值的过滤器对DMSO提取物进行超滤; 干燥由过滤器保留的部分,以获得格拉菲叶醋巴拉圭的提取物。 Graptopetalum paraguayense的提取物用于治疗或预防肝纤维化,肝硬化,肝癌,手术后肝纤维化复发或手术后肝癌复发。

    QUINAZOLINE COMPOUNDS, METHOD FOR PREPARING THE SAME AND USE THEREOF
    36.
    发明申请
    QUINAZOLINE COMPOUNDS, METHOD FOR PREPARING THE SAME AND USE THEREOF 有权
    喹唑啉化合物,其制备方法和用途

    公开(公告)号:US20150158854A1

    公开(公告)日:2015-06-11

    申请号:US14103662

    申请日:2013-12-11

    CPC classification number: C07D417/14 C07D239/94 C07D401/04 C07D403/04

    Abstract: A compound for treating a protein kinase-related disease or disorder having a structure of formula (I) wherein G is a heteroaryl, heterocyclic or alkyne; X is N or CH; L1 is —N(R7)—, —O—, —C(S)—, —C(O)—, or —S—; L2 is —N(R8)— or —O—; R1 and R2 are independently hydrogen, halogen, hydroxyl, amino, cyano, nitro, carboxy, C1-C4 alkoxy, C1-C4 alkoxy C1-C4 alkoxy, N,N—(C1-C4 dialkyl)amino C1-C4 alkoxy, N—(C1-C4 alkyl)amino C1-C4 alkoxy, C1-C4 alkanoyl, C1-C4 alkanoyloxy, N—(C1-C4 alkyl)amino, N,N—(C1-C4 dialkyl)amino, C1-C4 alkanoyl amino, or heterocyclyl, wherein C1-C4 alkyl is optionally substituted with one or more substituents selected from fluorine and chlorine; R3, R4 and R5 are independently hydrogen, fluorine or chlorine; R6 is C1-C4 alkyl or aryl, which is optionally substituted with one or more substituents selected from halogen, hydroxyl, amino, cyano, nitro; or R6 and R8 form a 5-6 membered cyclyl or heterocyclyl.

    Abstract translation: 一种用于治疗具有式(I)结构的蛋白激酶相关疾病或病症的化合物,其中G是杂芳基,杂环或炔基; X为N或CH; L 1是-N(R 7) - , - O - , - C(S) - , - C(O) - 或-S-; L2是-N(R8) - 或-O-; R1和R2独立地是氢,卤素,羟基,氨基,氰基,硝基,羧基,C1-C4烷氧基,C1-C4烷氧基C1-C4烷氧基,N,N-(C1-C4二烷基)氨基C1-C4烷氧基,N - (C 1 -C 4烷基)氨基C 1 -C 4烷氧基,C 1 -C 4烷酰基,C 1 -C 4烷酰氧基,N-(C 1 -C 4烷基)氨基,N,N-(C 1 -C 4二烷基)氨基,C 1 -C 4烷酰基氨基 或杂环基,其中C 1 -C 4烷基任选被一个或多个选自氟和氯的取代基取代; R3,R4和R5独立地是氢,氟或氯; R6是C1-C4烷基或芳基,其任选被一个或多个选自卤素,羟基,氨基,氰基,硝基的取代基取代; 或R6和R8形成5-6元环基或杂环基。

    BISPECIFIC T-CELL ACTIVATOR ANTIBODY
    37.
    发明申请
    BISPECIFIC T-CELL ACTIVATOR ANTIBODY 有权
    双重T细胞激活剂抗体

    公开(公告)号:US20130165629A1

    公开(公告)日:2013-06-27

    申请号:US13720573

    申请日:2012-12-19

    Abstract: This invention relates to bispecific antibodies having combinations of linker and hinge sequences to create linker-hinge interface domains with biological significance. Such linker-hinge interface domains covalently join two molecules, maintain the biological activities of linked molecules (target binding), stabilize the biological characteristics of new molecule (solubility and 4° C. stability), maintain the chemical, biochemical and physical properties (cytotoxicity) of the linked molecules, and modulate the biological characteristics of the linked molecules (activating T-lymphocytes without significant sign of proliferations). Both linker (GGGGS) and hinge (CPPCP) sequences are required to establish functional linker-hinge interface domains as deletion of any of the component resulted in significant lost of T-lymphocyte mediated activity.

    Abstract translation: 本发明涉及具有接头和铰链序列组合的双特异性抗体以产生具有生物学意义的接头 - 铰链界面结构域。 这种接头 - 铰链界面域共价连接两个分子,保持连接分子的生物活性(靶结合),稳定新分子的生物学特性(溶解度和4℃稳定性),保持化学,生化和物理性质(细胞毒性 ),并调节连接分子的生物学特性(活化T淋巴细胞而没有显着增殖迹象)。 需要两种接头(GGGGS)和铰链(CPPCP)序列来建立功能性接头 - 铰链界面区域,因为任何组分的缺失导致T淋巴细胞介导的活性的显着丧失。

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