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    • 41. 发明公开
    • 신규 2,5-피리딘디카복실산 유도체
    • 新的2,5-吡啶二羧酸
    • KR1020000031735A
    • 2000-06-05
    • KR1019980047918
    • 1998-11-10
    • 동화약품주식회사
    • 윤성준이상욱심형수박용균양왕용김종우박상진
    • C07D401/14
    • PURPOSE: 2,5-pyrimidinedicarboxylic acids and the method for manufacturing it are provided, which have effect on restraining the proliferation of HBV(Hepatitis B Virus) and HIV(Human Immunodeficiency Virus). CONSTITUTION: In the formula 1, R1 represents hydrogen, alkyl group, hydroxy alkyl group, alkoxy alkyl group, dihydroxy alkyl group and dialkoxy alkyl group and R2 represents hydrogen and alkyl group. 2,5-pyridinedicarboxylic acids(formula 1) can form organic or inorganic salt such as chloric acid, phosphoric acid, oxalic acid, maleic acid and tartaric acid which is admitted pharmaceutically. 2,5-pyridinedicarboxylic acids are prepared from following reaction(reaction 1). Piperazines are piperazine(R1=hydrogen), 1-methylpiperazine(R1=methyl group), 1-ethylpiperazine(R1=ethyl group), 1-(2-hydroxyethyl)piperazine(R1=2-hydroxyethyl group. Nicotinic acids(formula 2) are reacted with acyl chloride, product of this reaction is reacted with piperazine compounds and 2,5-pyrimidinedicarboxylic acids are prepared from this reaction.
    • 目的:提供2,5-嘧啶二羧酸及其制备方法,其具有抑制HBV(乙型肝炎病毒)和HIV(人类免疫缺陷病毒)增殖的作用。 构成:在式1中,R 1表示氢,烷基,羟基烷基,烷氧基烷基,二羟基烷基和二烷氧基烷基,R 2表示氢和烷基。 2,5-吡啶二羧酸(式1)可以形成有机或无机盐,例如药学上允许的氯酸,磷酸,草酸,马来酸和酒石酸。 从以下反应制备2,5-吡啶二羧酸(反应1)。 哌嗪是哌嗪(R1 =氢),1-甲基哌嗪(R1 =甲基),1-乙基哌嗪(R1 =乙基),1-(2-羟乙基)哌嗪(R1 = 2-羟乙基)烟酸(式2 )与酰氯反应,将该反应产物与哌嗪化合物反应,并从该反应制备2,5-嘧啶二羧酸。
    • 42. 发明公开
    • 세포수용체와HIV의상호작용을저해하는항AIDS펩타이드
    • 抗艾滋病肽抑制细胞受体与人类免疫缺陷病毒(HIV)之间的相互作用
    • KR1020000021557A
    • 2000-04-25
    • KR1019980040708
    • 1998-09-30
    • 동화약품주식회사학교법인 포항공과대학교
    • 윤성준김종우성영철이경재신동혁김남두최요한박상진장환봉한진희
    • C07K7/08
    • C07K7/08C07K7/64
    • PURPOSE: Provided is a peptide inhibiting an interaction between gp120 that is outer membrane protein of HIV and a cell receptor, CD4 on a stage of cell infection of HIV CONSTITUTION: A peptide consists of 12 amino acids. each amino acid comprises especially, proline and phenylalanine on the fourth and sixth position from amino-ends respectively and random amino acids. Peptide inhibits interaction between cell receptor, CD4 and outer membrane of HIV-1, gp120 on an early step of virus infection so it can be provided as a new AIDS treatment and used for combination therapy. To select a peptide which can be used for AIDS therapy, panning method which is characterized by using agarose bead as matrix and phage-displayed peptide library, is provided. In the panning method, peptide is obtained by using phosphate-buffered saline, competitive binding, and E.coli used as a host cell of phage.
    • 目的:提供抑制HIV的外膜蛋白的gp120与细胞受体之间的相互作用的肽,HIV在细胞感染阶段的CD4组成:肽由12个氨基酸组成。 每个氨基酸分别特别包括氨基末端的第四和第六位上的脯氨酸和苯丙氨酸以及随机氨基酸。 肽在病毒感染的早期阶段抑制细胞受体,CD4和HIV-1外膜之间的相互作用,因此可以作为新的AIDS治疗提供并用于联合治疗。 为了选择可用于AIDS治疗的肽,提供以使用琼脂糖珠作为基质和噬菌体展示肽文库的淘选方法。 在淘选方法中,通过使用磷酸盐缓冲盐水,竞争性结合和用作噬菌体宿主细胞的大肠杆菌获得肽。