Compounds and preparations having antiviral effect
    1.
    发明申请
    Compounds and preparations having antiviral effect 有权
    具有抗病毒作用的化合物和制剂

    公开(公告)号:US20070066684A1

    公开(公告)日:2007-03-22

    申请号:US10557922

    申请日:2003-05-22

    IPC分类号: A61K31/19 A61K31/12

    CPC分类号: A61K31/235

    摘要: An antiviral preparation comprising as an active ingredient, a phorbol derivative of formula 1: wherein is R1 —(CH2)aX(CH2)bCH3, —(CH2)cX(CH2)dYCH3, —CO(CH2)eCH3 or —(CH2)fCH3 R2 is —CO(CH2)nCH3, R3, R4 and R5 are hydrogen atom, or an aliphatic or aromatic carboxylic acid residue, X and Y are O or S, and each of a-f and n is a number, and having a specific safety index S.I.=CC50/EC50 of 10 or more wherein EC50 means a concentration at which HIV-1 induced cytopathogenic effect (CPE) in MT-4 cell is inhibited by 50%, and CC50 means a concentration at which survival of MT-4 cell in a cell proliferation test is reduced by 50%. These preparations are particularly effective for human immuno-deficiency virus (HIV).

    摘要翻译: 一种抗病毒制剂,其包含作为活性成分的式1的佛波醇衍生物:其中R 1 - (CH 2)2 X(CH (CH 2)2 CH 3, - (CH 2)2 C(CH 3) C(CH 2)2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 或者 - (CH 2)2 CH 3 R 2是-CO( CH 2,R 3,R 3,R 3,R 3,R 3, 或者脂族或芳族羧酸残基,X和Y分别是O或S,并且各af和n都是数,并且具有特定的安全指数SI = CC < 50或更高,其中EC 50是指在MT-4细胞中HIV-1诱导细胞致病作用(CPE)被抑制的浓度 50%,CC 50是指细胞增殖试验中MT-4细胞的存活率降低50%的浓度。 这些制剂对人免疫缺陷病毒(HIV)特别有效。

    Compounds and preparations having antiviral effect
    2.
    发明授权
    Compounds and preparations having antiviral effect 有权
    具有抗病毒作用的化合物和制剂

    公开(公告)号:US07662852B2

    公开(公告)日:2010-02-16

    申请号:US10557922

    申请日:2003-05-22

    CPC分类号: A61K31/235

    摘要: An antiviral preparation comprising as an active ingredient, a phorbol derivative of formula 1: wherein is R1 is —(CH2)aX(CH2)bCH3, —(CH2)cX(CH2)dYCH3, —CO(CH2)eCH3 or —(CH2)fCH3 R2 is —CO(CH2)nCH3, R3, R4 and R5 are hydrogen atom, or an aliphatic or aromatic carboxylic acid residue, X and Y are O or S, and each of a-f and n is a number, and having a specific safety index S.I.=CC50/EC50 of 10 or more wherein EC50 means a concentration at which HIV-1 induced cytopathogenic effect (CPE) in MT-4 cell is inhibited by 50%, and CC50 means a concentration at which survival of MT-4 cell in a cell proliferation test is reduced by 50%. These preparations are particularly effective for human immuno-deficiency virus (HIV).

    摘要翻译: 包含作为活性成分的式1的佛波醇衍生物的抗病毒制剂:其中R1是 - (CH2)aX(CH2)bCH3, - (CH2)cX(CH2)dYCH3,-CO(CH2)eCH3或 - (CH2 )fCH 3 R 2是-CO(CH 2)n CH 3,R 3,R 4和R 5是氢原子,或脂族或芳族羧酸残基,X和Y是O或S,并且af和n各自是数, 特异性安全性指数SI = CC50 / EC50为10以上,其中EC 50是指MT-4细胞中HIV-1诱导的细胞致病作用(CPE)的抑制浓度为50%,CC50是指MT- 4细胞在细胞增殖试验中减少了50%。 这些制剂对人免疫缺陷病毒(HIV)特别有效。

    Ultraviolet absorber
    3.
    发明授权
    Ultraviolet absorber 有权
    紫外吸收剂

    公开(公告)号:US08252273B2

    公开(公告)日:2012-08-28

    申请号:US12677900

    申请日:2008-04-02

    IPC分类号: A61K8/49 A61K8/00 C07C69/76

    CPC分类号: C07C69/734 A61K8/37 A61Q17/04

    摘要: There is provided an ultraviolet absorber having a strong absorptive capacity in the UVA range and an absorptive capacity in the UVB range to have an ultraviolet inhibitory effect in a wide range of wavelength, increasing in an ultraviolet absorptive capacity over the course of ultraviolet irradiation time in both the UVA and the UVB ranges and having an excellent solubility. An ultraviolet absorber comprising, as an active ingredient, a compound of General Formula I: (where —OA is an alkoxy group) that exhibits an ultraviolet A wave absorptive capacity which increases over time and that has an ultraviolet B wave absorptive capacity.

    摘要翻译: 提供了在UVA范围内具有强吸收能力的紫外线吸收剂和在UVB范围内的吸收能力,在宽波长范围内具有紫外线抑制作用,在紫外线照射时间内增加紫外线吸收能力 UVA和UVB两者都具有优异的溶解性。 一种紫外线吸收剂,其特征在于,含有通式I的化合物(其中-OA为烷氧基),其表现出随时间而增加并具有紫外线B吸收能力的紫外线A吸收能力。

    Stereoisomeric indole compounds, process for the preparation of the same, and use thereof
    4.
    发明授权
    Stereoisomeric indole compounds, process for the preparation of the same, and use thereof 有权
    立体异吲哚化合物,其制备方法及其用途

    公开(公告)号:US06348484B1

    公开(公告)日:2002-02-19

    申请号:US09486318

    申请日:2000-02-25

    IPC分类号: A61K31422

    CPC分类号: C07D413/04

    摘要: Novel stereoisomeric indole compounds of the formula (1), a process for the preparation the same, and use thereof wherein, Y represents the group wherein, X represents alkyl group having 1-5 carbon atom(s) (the alkyl group may be substituted with hydroxyl group, carboxyl group, amino group, methylthio group, mercapto group, guanidyl group, imidazolyl group or benzyl group), and R1 and R2 represent each independently hydrogen atom, alkyl group, aralkyl group, cycloalkyl group or aryl group;R represents hydrogen atom, alkyl group, aralkyl group, cycloalkyl group, aryl group, monovalent metal, amine or ammonium; and the symbol ‘*’ represents a position of an asymmetric carbon atom. The above-mentioned compounds can be prepared by condensing tryptophan with a stereoisomeric &agr;-amino acid or carboxylic acid to form an amide form and subjecting or carboxylic acid to form an amide form and subjecting the amide form to oxidative cyclization to form an oxazole ring at once. The compounds exhibit; physiological activities such as inhibitory action against lipid peroxidation, and can be therefore utilized in the form of lipid peroxidation inhibitors containing the same as the active ingredient.

    摘要翻译: 式(1)的新型立体异构吲哚化合物及其制备方法及其用途,其中Y表示基团,其中X表示具有1-5个碳原子的烷基(该烷基可被羟基取代 基团,羧基,氨基,甲硫基,巯基,胍基,咪唑基或苄基),R1和R2各自独立地表示氢原子,烷基,芳烷基,环烷基或芳基; R表示氢原子 烷基,芳烷基,环烷基,芳基,一价金属,胺或铵; 并且符号“*”表示不对称碳原子的位置,上述化合物可以通过将色氨酸与立体异构的α-氨基酸或羧酸缩合形成酰胺形式并使其经受或羧酸形成酰胺来制备 形成并使酰胺形式进行氧化环化以形成恶唑环,化合物表现出生理活性,例如对脂质过氧化作用的抑制作用,因此可以以含有与活性成分相同的脂质过氧化抑制剂的形式使用 。

    ULTRAVIOLET ABSORBER
    5.
    发明申请
    ULTRAVIOLET ABSORBER 有权
    超紫外线吸收剂

    公开(公告)号:US20100239508A1

    公开(公告)日:2010-09-23

    申请号:US12677900

    申请日:2008-04-02

    CPC分类号: C07C69/734 A61K8/37 A61Q17/04

    摘要: There is provided an ultraviolet absorber having a strong absorptive capacity in the UVA range and an absorptive capacity in the UVB range to have an ultraviolet inhibitory effect in a wide range of wavelength, increasing in an ultraviolet absorptive capacity over the course of ultraviolet irradiation time in both the UVA and the UVB ranges and having an excellent solubility. An ultraviolet absorber comprising, as an active ingredient, a compound of General Formula I: (where —OA is an alkoxy group) that exhibits an ultraviolet A wave absorptive capacity which increases over time and that has an ultraviolet B wave absorptive capacity.

    摘要翻译: 提供了在UVA范围内具有强吸收能力的紫外线吸收剂和在UVB范围内的吸收能力,在宽波长范围内具有紫外线抑制作用,在紫外线照射时间内增加紫外线吸收能力 UVA和UVB两者都具有优异的溶解性。 一种紫外线吸收剂,其特征在于,含有通式I的化合物(其中-OA为烷氧基),其表现出随时间而增加并具有紫外线B吸收能力的紫外线A吸收能力。

    Compound protecting against ultraviolet rays
    6.
    发明授权
    Compound protecting against ultraviolet rays 有权
    化合物防紫外线

    公开(公告)号:US07361785B2

    公开(公告)日:2008-04-22

    申请号:US10533202

    申请日:2002-11-05

    IPC分类号: C07C63/36 C07C205/06

    摘要: An ultraviolet ray protection agent including a compound having an ultraviolet ray protection effect as an active ingredient. The compound is expressed by general formula I′: wherein X represents NH or O; Y′ represents a vinyl group substituted by a methyl group or a phenyl group, or a phenyl group substituted by a methoxy group or a fluorine atom, or a naphthyl group; and Z represents a phenyl group substituted by a methyl group, a carboxyl group or a nitro group, or a naphthyl group. The compound represented by the general formula I′ includes both novel compounds of the present invention and known compounds. The ultraviolet ray protection agent of the present invention offers outstanding ultraviolet ray protection effectiveness and is very safe.

    摘要翻译: 包含具有紫外线保护作用的化合物作为有效成分的紫外线防护剂。 该化合物由通式I'表示:其中X表示NH或O; Y'表示被甲基或苯基取代的乙烯基或被甲氧基或氟原子取代的苯基或萘基; Z表示被甲基,羧基或硝基取代的苯基或萘基。 由通式I'表示的化合物包括本发明的新化合物和已知化合物。 本发明的紫外线防护剂提供优异的紫外线防护效果,且非常安全。

    Receptor linked protein tyrosine phosphatases
    8.
    发明授权
    Receptor linked protein tyrosine phosphatases 失效
    受体连接蛋白酪氨酸磷酸酶

    公开(公告)号:US07220309B2

    公开(公告)日:2007-05-22

    申请号:US10385206

    申请日:2003-03-10

    IPC分类号: C30B29/14

    摘要: The crystal structures of CD45 and LAR, described herein, provide a basis for kinetic and functional studies. Identification of the crystal structures of cellular molecules is important in to determine functional roles in immunity, phosphorylation events, disease initiation mechanism. The isolated crystals and methods for crystallization thereof, are also important in identifying small molecule interactions with cellular molecules for new drug discovery.

    摘要翻译: 本文所述的CD45和LAR的晶体结构为动力学和功能研究提供了基础。 鉴定细胞分子的晶体结构对于确定免疫,磷酸化事件,疾病发病机制中的功能作用是重要的。 分离的晶体及其结晶方法在识别与细胞分子相互作用的新型药物发现方面也很重要。

    Nozzle vane driving control apparatus of variable nozzle turbocharger
    9.
    发明授权
    Nozzle vane driving control apparatus of variable nozzle turbocharger 有权
    可变喷嘴涡轮增压器喷嘴叶片驱动控制装置

    公开(公告)号:US06895750B2

    公开(公告)日:2005-05-24

    申请号:US10780910

    申请日:2004-02-19

    摘要: In a nozzle vane driving control apparatus of a variable nozzle turbocharger including an actuator for carrying out a driving operation for opening and closing a nozzle vane of a variable nozzle and an ECU for controlling the opening degree of the nozzle vane which is obtained by the actuator, an actuator cover for covering a pinion and reduction gears by interposing a base provided integrally with a motor case portion therebetween, a unit body accommodating each of control boards, a position sensor for detecting the rotating position of an output shaft and a connector having a terminal connecting a motor and each of the control boards, and a unit cover for covering the unit body are removably fastened and fixed with a bolt and are thus integrated with each other.

    摘要翻译: 一种可变喷嘴涡轮增压器的喷嘴叶片驱动控制装置,包括用于执行用于打开和关闭可变喷嘴的喷嘴叶片的驱动操作的致动器和用于控制由致动器获得的喷嘴叶片的开度的ECU ,用于通过将与其间的电动机壳体部分整体设置的基座相互覆盖小齿轮和减速齿轮的致动器盖,容纳每个控制板的单元体,用于检测输出轴的旋转位置的位置传感器和具有 连接电动机和每个控制板的端子和用于覆盖单元主体的单元盖可拆卸地用螺栓紧固和固定,并因此彼此一体化。

    Heterodimeric T lymphocyte receptor subunit
    10.
    发明授权
    Heterodimeric T lymphocyte receptor subunit 失效
    异二聚体T淋巴细胞受体亚单位

    公开(公告)号:US5977321A

    公开(公告)日:1999-11-02

    申请号:US742539

    申请日:1991-08-08

    IPC分类号: C07K14/725 C07K16/28

    CPC分类号: C07K16/2809 C07K14/7051

    摘要: Disclosed is a heterodimeric T lymphocyte receptor subunit. The subunit consists of variable, joining, constant, transmembrane, and cytoplasmic regions.The structure, amino acid, and nucleotide sequence of the lymphocyte receptor subunit were determined using cDNA clones derived from a functional murine cytotoxic T lymphocyte clone. The genes corresponding to these cDNA are expressed and rearranged specifically in T cells and have significant sequence homologies to immunoglobulin V and C genes.T cell receptor subunits may be produced from the cDNA clones. The protein molecules may be further used for the production of T-cell clone specific antibodies.

    摘要翻译: 公开了异二聚体T淋巴细胞受体亚基。 亚基由可变,连接,恒定,跨膜和胞质区组成。 使用衍生自功能性鼠细胞毒性T淋巴细胞克隆的cDNA克隆测定淋巴细胞受体亚基的结构,氨基酸和核苷酸序列。 与这些cDNA相对应的基因在T细胞中特异性表达和重排,并且与免疫球蛋白V和C基因具有显着的序列同源性。 T细胞受体亚基可以从cDNA克隆产生。 蛋白质分子可以进一步用于生产T细胞克隆特异性抗体。