N-hexanoyl to n-heptadecanoyl 5-hydroxy
tryptophan-5-hydroxytryptophanamides and use as analgesics
    13.
    发明授权
    N-hexanoyl to n-heptadecanoyl 5-hydroxy tryptophan-5-hydroxytryptophanamides and use as analgesics 失效
    N-己酰基至正十七烷酰基-5-羟基色氨酸-5-羟基色氨酰胺,用作止痛剂

    公开(公告)号:US4482567A

    公开(公告)日:1984-11-13

    申请号:US433283

    申请日:1982-10-07

    CPC分类号: C07K5/06156 C07D209/20

    摘要: Analgesia-effecting 5-hydroxytryptophan derivatives are disclosed of the formulae: ##STR1## wherein R is selected from the group consisting of C.sub.2 -C.sub.16 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.16 alkenyl, C.sub.2 -C.sub.16 alkynyl, aryl containing up to 14 carbon atoms, and arylalkyl containing up to 20 carbon atoms;R.sup.1 and R.sup.1a are each H or methyl;R.sup.2 and R.sup.2a are each H or R, as defined above;R.sup.3 and R.sup.3a are each H or alkyl containing from 1 to 4 carbons;R.sup.4 and R.sup.4a are each H or alkyl containing from 1 to 4 carbons;and their non-toxic, pharmacologically acceptable acid addition salts.

    摘要翻译: 镇痛作用的5-羟色氨酸衍生物公开于下列通式:其中R选自C 2 -C 16烷基,C 3 -C 8环烷基,C 2 -C 16烯基,C 2 -C 16炔基 ,含有至多14个碳原子的芳基和含有至多20个碳原子的芳基烷基; R1和R1a各自为H或甲基; R2和R2a各自为H或R,如上所定义; R3和R3a各自为H或含有1至4个碳的烷基; R4和R4a各自为H或含有1至4个碳的烷基; 及其无毒,药理学上可接受的酸加成盐。

    Pharmaceutical agents for the treatment of sickle cell disease
    14.
    发明授权
    Pharmaceutical agents for the treatment of sickle cell disease 失效
    用于治疗镰状细胞病的药剂

    公开(公告)号:US4390526A

    公开(公告)日:1983-06-28

    申请号:US157107

    申请日:1980-06-06

    摘要: The present invention relates to novel compounds selected from R.sub.1 --COO(CH.sub.2).sub.n --R.sub.2 and ##STR1## wherein R.sub.1 is selected from heterocyclic aromatic and hydrophobic naturally occuring and modified amino acids in the D- and in the L-form, and from peptides, wherein n is an integer of from 1 to 5 and R.sub.2 is selected from unsubstituted and substituted phenyl rings, and from heterocyclic rings, as well as to pharmaceutical compositions for preventing sickling of erythrocytes during sickle cell crisis and for desickling of sickle cells of patients afflicted by sickle cell disease, the active ingredient of which is a compound as defined above.

    摘要翻译: 本发明涉及选自R 1 -COO(CH 2)n -R 2和R 1的新化合物,其中R 1选自D-和L-型的杂环芳族和疏水天然存在和修饰的氨基酸, 肽,其中n为1至5的整数,并且R 2选自未取代和取代的苯环,以及杂环,以及用于防止镰状细胞危象期间红细胞镰刀形成的药物组合物和用于镰状细胞 患有镰状细胞病的患者,其活性成分是如上所定义的化合物。

    Avidin derivatives and uses thereof
    15.
    发明授权
    Avidin derivatives and uses thereof 失效
    抗生物素蛋白衍生物及其用途

    公开(公告)号:US07217575B2

    公开(公告)日:2007-05-15

    申请号:US10624503

    申请日:2003-07-23

    摘要: A covalent conjugate of a 4′-hydroxyazobenzene-2-carboxylic acid derivative (HABA) and an avidin-type molecule, of the formula: wherein A is (CH2)n or —CH═CH—, wherein n is an integer from 0–10; B is (CH2)n wherein n is an integer from 2 to 10; m is zero or 1; and Av is the residue of an avidin-type molecule selected from the group comprising native egg-white avidin, recombinant avidin, deglycosylated avidins, bacterial streptavidin, recombinant streptavidin, truncated streptavidin and other derivatives of said avidin-type molecules. These HABAylated avidins are red colored in the quinone configuration and can be used in many applications in the avidin-biotin technology.

    摘要翻译: 4'-羟基偶氮苯-2-羧酸衍生物(HABA)和抗生物素蛋白型分子的共价缀合物,其分子式如下:其中A是(CH 2 N 2)n 或-CH-CH-,其中n是0-10的整数; B是(CH 2)n N n其中n是2至10的整数; m为零或1; Av是选自天然蛋白抗生物素蛋白,重组抗生物素蛋白,去糖基化抗体,细菌链霉抗生物素蛋白,重组链霉抗生物素蛋白,截短的链霉抗生物素蛋白和所述抗生物素蛋白型分子的其它衍生物的组的抗生物素蛋白型分子的残基。 这些HABA化的avidins在醌配体中是红色的,并且可以用于抗生物素蛋白 - 生物素技术的许多应用。

    Modified avidin-type molecules as targeting agents for the liver and cells of the reticuloendothelial system
    16.
    发明授权
    Modified avidin-type molecules as targeting agents for the liver and cells of the reticuloendothelial system 失效
    修饰的抗生物素蛋白型分子作为肝脏的靶向剂和网状内皮系统的细胞

    公开(公告)号:US06638508B2

    公开(公告)日:2003-10-28

    申请号:US09100015

    申请日:1998-06-19

    IPC分类号: A61K39395

    摘要: The present invention relates to avidin-type molecules having 2,4,6-trinitrophenyl or lactosyl groups or being complexed with an antibody specific to the avidin-type molecule, which shifts the biodistribution pattern in tissues and organs to the liver, where these molecules accumulate at high levels over several days. These modified avidin-type molecules provide a means for delivery of diagnostic and therapeutic agents, including radionuclides to the liver and cells of the reticuloendothelial system (RES) for diagnosing and treating hepatic disorders and disorders of the RES.

    摘要翻译: 本发明涉及具有2,4,6-三硝基苯基或乳糖基或与抗生物素蛋白型分子特异性抗体复合的抗生物素蛋白型分子,其将组织和器官中的生物分布模式转移到肝脏,其中这些分子 几天内积累在高水平。 这些修饰的抗生物素蛋白型分子提供了用于诊断和治疗RES的肝脏疾病和病症的诊断和治疗剂(包括放射性核素)到肝脏和网状内皮系统(RES)的细胞的递送手段。

    Chromatography adsorbents utilizing mercapto heterocyclic ligands
    17.
    发明授权
    Chromatography adsorbents utilizing mercapto heterocyclic ligands 失效
    使用巯基杂环配体的色谱吸附剂

    公开(公告)号:US06610630B2

    公开(公告)日:2003-08-26

    申请号:US09023266

    申请日:1998-02-13

    IPC分类号: B01J2022

    摘要: A pseudobioaffinity chromatography adsorbent adapted for use in selectively adsorbing immunoglobulins. In one embodiment, the adsorbent includes: (a) a solid support material; and (b) a ligand immobilized on the surface of the solid support material, said ligand being a compound of the formula wherein Y1 is selected from the group consisting of S, SCH3+, O, NH, NCH3, CH2 and CR1R2 wherein at least one of R1 and R2 is not hydrogen; wherein each of Y2, Y3 and Y4 is selected from the group consisting of N, NCH3+, CH, and CR wherein R is not hydrogen; and wherein at least two of Y1, Y2, Y3 and Y4 are neither CH2, CH, CR nor CR1R2.

    摘要翻译: 适用于选择性吸附免疫球蛋白的假离子亲和层析吸附剂。 在一个实施方案中,吸附剂包括:(a)固体支持材料; 和(b)固定在固体载体材料表面上的配体,所述配位体是酉环的化合物Y 1选自S,SCH 3 +,O,NH,NCH 3,CH 2和CR 1 R 2,其中至少一个 R1和R2不是氢; 其中Y2,Y3和Y4各自选自N,NCH 3 +,CH和CR,其中R不是氢; 并且其中Y 1,Y 2,Y 3和Y 4中的至少两个既不是CH 2,CH,CR和CR 1 R 2。

    Avidin derivatives and uses thereof
    18.
    发明授权
    Avidin derivatives and uses thereof 失效
    抗生物素蛋白衍生物及其用途

    公开(公告)号:US06632929B1

    公开(公告)日:2003-10-14

    申请号:US09831499

    申请日:2001-08-07

    IPC分类号: C07K100

    摘要: A covalent conjugate of a 4′-hydroxyazobenzene-2-carboxylic acid derivative (HABA) and an avidin-type molecule, of the formula: wherein A is (CH2)n or —CH═CH—, wherein n is an integer from 0-10; B is (CH2)n wherein n is an integer from 2 to 10; m is zero or 1; and Av is the residue of an avidin-type molecule selected from the group comprising native egg-white avidin, recombinant avidin, deglycosylated avidins, bacterial streptavidin, recombinant streptavidin, truncated streptavidin and other derivatives of said avidin-type molecules. These HABAylated avidins are red colored in the quinone configuration and can be used in many applications in the avidin-biotin technology.

    摘要翻译: 4'-羟基偶氮苯-2-羧酸衍生物(HABA)和抗生物素蛋白型分子的共价缀合物,其分子式如下:其中A是(CH 2 H 2 O) HIL> n 或-CH = CH-,其中n是0-10的整数; B是(CH 2 n 其中n是2至10的整数; m为零或1; Av是选自天然蛋白抗生物素蛋白,重组抗生物素蛋白,去糖基化抗体,细菌链霉抗生物素蛋白,重组链霉抗生物素蛋白,截短的链霉抗生物素蛋白和所述抗生物素蛋白型分子的其它衍生物的组的抗生物素蛋白型分子的残基。 这些HABA化的avidins在醌配体中是红色的,可用于许多应用中的抗生物素蛋白 - 生物素技术。