HIV-1 protease inhibitors
    3.
    发明授权
    HIV-1 protease inhibitors 失效
    HIV-1蛋白酶抑制剂

    公开(公告)号:US5827827A

    公开(公告)日:1998-10-27

    申请号:US667001

    申请日:1996-06-20

    CPC分类号: C07K7/02 C07K5/021 A61K38/00

    摘要: A series of novel oxirane derivatives, which are useful for inhibiting HIV are disclosed. Particularly of value are peptidomimetic compounds, containing a terminal epoxide group on a peptide or psuedopeptide backbone, which are believed to inhibit HIV protease by extruding enzyme-bound water molecules from the active site of the enzyme.

    摘要翻译: 公开了一系列用于抑制HIV的新型环氧乙烷衍生物。 值得特别的是肽模拟化合物,其在肽或肽肽主链上含有末端环氧基团,据信通过从酶的活性位点挤出酶结合水分子来抑制HIV蛋白酶。

    Peptide linkage unit
    5.
    发明授权
    Peptide linkage unit 失效
    肽连接单元

    公开(公告)号:US5563121A

    公开(公告)日:1996-10-08

    申请号:US256236

    申请日:1994-06-30

    摘要: A peptide linkage unit is employed for joining peptide and pseudopeptide sequences, including peptides and pseudopeptides that inhibit aspartic proteinase enzymes. The peptide linkage unit includes a phosphinate methylene ammonium linkage in place of a peptidyl carboxamide bond. If the peptide linkage unit is incorporated into a peptide sequence that would otherwise serve as an aspartic proteinase substrate and if it is positioned at a cleavage site within such peptide sequence, the phosphinate methylene ammonium linkage is resistant to cleavage and serves as an exploding transition state analog of such cleavage site. When so incorporated, the phosphinate methylene ammonium linkage can bind or interfere with the active site of aspartic proteinase enzymes and inhibit its activity. Preferred inhibitors contain a phosphinic acid methylene amine group joining the P.sub.1 and P.sub.1 ' residues and have a length of 3 to about 15 amino acid residues.

    摘要翻译: PCT No.PCT / US93 / 00228 Sec。 371日期:1994年6月30日 102(e)1994年6月30日PCT 1993年1月11日PCT PCT。 公开号WO93 / 00228 日期1993年1月11日使用肽连接单元连接肽和假肽序列,包括抑制天冬氨酸蛋白酶的肽和假肽。 肽连接单元包括次膦酸亚甲基铵键代替肽基羧酰胺键。 如果将肽连接单元并入到否则将用作天冬氨酸蛋白酶底物的肽序列中,并且如果其位于该肽序列内的切割位点,则次膦酸亚甲基铵键对切割具有抗性并且用作爆炸过渡态 类似物的这种切割位点。 当这样结合时,次膦酸亚甲基铵键可以结合或干扰天冬氨酸蛋白酶的活性位点并抑制其活性。 优选的抑制剂含有连接P1和P1'残基的次膦酸亚甲基基团,并且具有3至约15个氨基酸残基的长度。

    Anti-cocaine vaccine
    7.
    发明授权
    Anti-cocaine vaccine 失效
    抗可卡因疫苗

    公开(公告)号:US06383490B1

    公开(公告)日:2002-05-07

    申请号:US09077434

    申请日:1998-06-12

    IPC分类号: A61K39395

    摘要: An anti-cocaine vaccine employs a cocaine hapten conjugated to a carrier protein. The anti-cocaine vaccine elicits an immune response which reduces the psychoactive effects of cocaine consumption by the production of anti-cocaine polyclonal antibodies. The antibodies may be employed in an ELISA test for assaying cocaine. The immune response elicited by the anti-cocaine vaccine produces antibody producing cells which may be isolated and cloned for producing anti-cocaine monoclonal antibodies.

    摘要翻译: 抗可卡因疫苗使用与载体蛋白缀合的可卡因半抗原。 抗可卡因疫苗引发免疫反应,通过生产抗可卡因多克隆抗体降低可卡因消费的精神影响。 抗体可用于测定可卡因的ELISA试验。 由抗可卡因疫苗引起的免疫应答产生抗体产生细胞,其可以被分离并克隆以产生抗可卡因单克隆抗体。

    Heroin Haptens, Immunoconjugates and Related Uses
    8.
    发明申请
    Heroin Haptens, Immunoconjugates and Related Uses 审中-公开
    海洛因半抗原,免疫接种物及相关用途

    公开(公告)号:US20150343054A1

    公开(公告)日:2015-12-03

    申请号:US14367511

    申请日:2011-12-21

    申请人: Kim D. Janda

    发明人: Kim D. Janda

    摘要: The present invention provides novel heroin hapten compounds and heroin immunoconjugates which can be used for in vivo production of antibodies that specifically bind to heroin and its psychoactive metabolites. The invention also provides methods of using vaccines comprising the heroin immunoconjugates in active or passive immunization protocols. The compositions and methods of the invention are useful for prevention and treatment of heroin addiction.

    摘要翻译: 本发明提供了可用于体内产生特异性结合海洛因及其精神活性代谢物的抗体的海洛因半抗原化合物和海洛因免疫缀合物。 本发明还提供了在主动或被动免疫方案中使用包含海洛因免疫缀合物的疫苗的方法。 本发明的组合物和方法可用于预防和治疗海洛因成瘾。

    Azatide peptidomimetics
    10.
    发明授权
    Azatide peptidomimetics 有权
    阿魏酸肽模拟物

    公开(公告)号:US06664372B1

    公开(公告)日:2003-12-16

    申请号:US09142148

    申请日:1998-09-01

    IPC分类号: C07K700

    摘要: Peptidomimetic azatides and combinatorial oligoazitide libraries are produced by means of a stepwise synthesis. Combinatorial library construction of this new biomimetic polymer provides a means to fabricate global peptidomimetic libraries.

    摘要翻译: 通过逐步合成产生拟肽阿扎肽和组合寡聚氮杂文库。 这种新的仿生聚合物的组合图书馆建设提供了制造全球拟肽库的手段。