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    LIGAND SCREENING AND DESIGN BY X-RAY CRYSTALLOGRAPHY
    2.
    发明申请
    LIGAND SCREENING AND DESIGN BY X-RAY CRYSTALLOGRAPHY 审中-公开
    通过X射线晶体学的配镜筛选和设计

    公开(公告)号：WO1999045389A2

    公开(公告)日：1999-09-10

    申请号：PCT/US1999004518

    申请日：1999-03-01

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  NIENABER, Vicki, L. ,  GREER, Jonathan ,  ABAD-ZAPATERO, Celerino ,  NORBECK, Daniel, W.

    IPC: G01N33/50

    CPC classification number: G01N33/6845 ,  C07K2299/00 ,  C30B7/00 ,  G01N23/20 ,  G01N33/68 ,  G01N33/6803 ,  G01N33/6842 ,  G01N2333/9723 ,  G01N2500/00

    Abstract: X-ray crystallography can be used to screen compounds that are not known ligands of a target biomolecule for their ability to bind the target biomolecule. The method includes obtaining a crystal of a target biomolecule; exposing the target biomolecule crystal to one or more test samples; and obtaining an X-ray crystal diffraction pattern to determine whether a ligand/receptor complex is formed. The target is exposed to the test samples by either co-crystallizing a biomolecule in the presence of one or more test samples or soaking the biomolecule crystal in a solution of one or more test samples. In another embodiment, structural information from ligand/receptor complexes are used to design ligands that bind tighter, that bind more specifically, that have better biological activity or that have better safety profile. A further embodiment of the invention comprises identifying or designing biologically-active moieties by the instant process. In a further embodiment, a biomolecule crystal having an easily accessible active site is formed by co-crystallizing the biomolecule with a degradable ligand and degrading the ligand.

    Abstract translation: 可以使用X射线晶体学来筛选目标生物分子的未知配体的化合物，以获得其结合目标生物分子的能力。 该方法包括获得目标生物分子的晶体; 将目标生物分子晶体暴露于一个或多个测试样品; 并获得X射线晶体衍射图，以确定是否形成配体/受体复合物。 通过在一个或多个测试样品的存在下共生结晶生物分子或将生物分子晶体浸泡在一个或多个测试样品的溶液中，将靶标暴露于测试样品。 在另一个实施方案中，来自配体/受体复合物的结构信息用于设计更紧密结合的配体，其更具体地结合，具有更好的生物活性或具有更好的安全性。 本发明的另一个实施方案包括通过本方法识别或设计生物活性部分。 在另一个实施方案中，通过使生物分子与可降解配体共结晶并使配体降解而形成具有易于接近的活性位点的生物分子晶体。

    PROCESS FOR THE PREPARATION OF A SUBSTITUTED 2,5-DIAMINO-3-HYDROXYHEXANE
    4.
    发明申请
    PROCESS FOR THE PREPARATION OF A SUBSTITUTED 2,5-DIAMINO-3-HYDROXYHEXANE 审中-公开
    制备取代的2,5-二氨基-3-羟基己酸的方法

    公开(公告)号：WO1995011224A1

    公开(公告)日：1995-04-27

    申请号：PCT/US1994010852

    申请日：1994-09-26

    Applicant: ABBOTT LABORATORIES

    Inventor： ABBOTT LABORATORIES ,  STUK, Timothy, L. ,  KERDESKY, Francis, A., J. ,  LIJEWSKI, Linda, M. ,  NORBECK, Daniel, W. ,  SCARPETTI, David ,  TIEN, Jien-Heh, J. ,  ALLEN, Michael, S. ,  LANGRIDGE, Denton, C. ,  MELCHER, Laura ,  RENO, Daniel, S. ,  SHAM, Hing, Leung ,  ZHAO, Chen ,  HAIGHT, Anthony, R. ,  LEANNA, M., Robert ,  MORTON, Howard, E. ,  ROBBINS, Timothy, A. ,  SOWIN, Thomas, J.

    IPC: C07C225/16

    CPC classification number: C07D221/14 ,  C07B2200/07 ,  C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C251/40 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07C215/08

    Abstract: Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of formula (3), wherein R6 and R7 are each hydrogen or R6 and R7 are independently selected from (i), wherein Ra and Rb are independently selected from hydrogen, loweralkyl and phenyl and Rc, Rd and Re are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and (ii) wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R6 is as defined above and R7 is R7aOC (O)-wherein R7a is loweralkyl or benzyl; or R6 and R7 taken together with the nitrogen atom to which they are bonded are (a) or (b), wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R8 is hydrogen or -C(O)R" wherein R" is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.

    Abstract translation: 公开了可用于制备基本上纯的式（3）化合物的中间体和方法，其中R 6和R 7各自为氢或R 6和R 7独立地选自（ⅰ），其中R a和R b独立地选自氢 ，低级烷基和苯基，Rc，Rd和Re独立地选自氢，低级烷基，三氟甲基，烷氧基，卤素和苯基; 和（ii）其中萘基环是未取代的或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或R 6如上所定义，且R 7为R 7 a OC（O） - 其中R 7a为低级烷基或苄基; 或R 6和R 7与它们所键合的氮原子一起是（a）或（b），其中R f，R g，Rh和R 1独立地选自氢，低级烷基，烷氧基，卤素和三氟甲基，并且R 8是氢或 -C（O）R“其中R”是低级烷基，烷氧基，苄氧基或苯基，其中苯环是未取代的或被一个，两个或三个独立地选自低级烷基，三氟甲基，烷氧基和卤素的取代基取代; 或其酸加成盐。

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