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。

公开(公告)号：WO1998031699A1

公开(公告)日：1998-07-23

申请号：PCT/US1997023607

申请日：1997-12-19

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  SPANTON, Stephen, G. ,  HENRY, Rodger, F. ,  RILEY, David, A. ,  LIU, Jih-Hua

IPC: C07H17/08

CPC classification number: C07H17/08

Abstract: The present invention concerns the novel antibiotic 6-O-methylerythromycin A form 0 solvate of formula (I), a process for its preparation, pharmaceutical compositions comprising this compound and a method of use as a therapeutic agent.

Abstract translation: 本发明涉及式（I）的新型抗生素6-O-甲基红霉素A型0溶剂合物，其制备方法，包含该化合物的药物组合物和用作治疗剂的方法。

公开(公告)号：WO1998031698A1

公开(公告)日：1998-07-23

申请号：PCT/US1997023356

申请日：1997-12-18

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  PAREKH, Shyamal, I. ,  GRAHAM, Alexandra, E. ,  DiPIERRO, Michael, J. ,  THOMAS, Albert, V. ,  RILEY, David, A.

IPC: C07H17/08

CPC classification number: C07H17/08

Abstract: A process for the preparation of 4''-deoxyerythromycins, having formula (I), wherein R is H or OH, Rp is H or acetyl, and R is H or loweralkyl; by treatment of the 2'-O-acetyl-4''-imidazolylthionocarbonyl-erythromycin starting material with the radical initiator 4,4'-azobis-(4-cyanovaleric acid), H3PO2 and an organic base in a water-miscible solvent other than an alcohol, and optionally eliminating the 2'-O-acetyl group. In a preferred embodiment, the water-miscible solvent is an alcohol and the deoxygenation and deacetylation is carried out in one step.

Abstract translation: 制备具有式（I）的4“ - 脱氧红霉素的方法，其中R为H或OH，Rp为H或乙酰基，R 1为H或低级烷基; 通过用自由基引发剂4,4'-偶氮双（4-氰基戊酸），H 3 PO 2和有机碱在水混溶性溶剂中处理2'-O-乙酰基-4“ - 咪唑基硫羰基 - 红霉素原料 并且任选地除去2'-O-乙酰基。 在优选的实施方案中，水混溶性溶剂是醇，脱氧和脱乙酰化在一个步骤中进行。

公开(公告)号：WO1998028979A1

公开(公告)日：1998-07-09

申请号：PCT/US1997022919

申请日：1997-12-12

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  VENBURG, Gregory, D. ,  HANSEN, James, R. ,  WOOLARD, Derek, D. ,  SHAFER, Warren, E. ,  BLACK-SCHAEFER, Candace

IPC: A01N37/44

CPC classification number: A01N37/36 ,  A01N37/44

Abstract: A process of inhibiting stem elongation in ornamental bulbous plants or to cut flowers from such plants, involving treating such plants or flowers with an effective amount of ACC synthase inhibitor, such as aminoethoxyvinylglycine and aminooxyacetic acid to inhibit stem elongation, by administration of a solid, semi-solid or a solution of such ACC synthase inhibitor.

Abstract translation: 一种抑制装饰性球茎植物茎茎伸长或从这些植物切花的方法，涉及用有效量的ACC合成酶抑制剂如氨基乙氧基乙烯基甘氨酸和氨基氧乙酸处理这样的植物或花，以抑制茎伸长，通过施用固体， 半固体或这种ACC合酶抑制剂的溶液。

公开(公告)号：WO1998025665A1

公开(公告)日：1998-06-18

申请号：PCT/US1997022462

申请日：1997-12-09

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  GRABENKORT, Richard, W.

IPC: A61M16/18

CPC classification number: A61M16/183 ,  A61M2205/6045

Abstract: A system is provided for draining an anesthetic agent from a reservoir of an anesthetic vaporizer. The system includes an anesthetic agent container having an inlet into which the agent can drain. The vaporizer has a draining station that defines an outlet and that defines a drain passage between the vaporizer reservoir and the outlet. A valve is operable to open and close the drain passage. A connector is provided with a receiving end for connecting to the draining station at the outlet. The connector has a discharge end for connecting to the container inlet. The connector holds the container below the draining station outlet and defines a transfer passage between the receiving end and the discharge end for draining the agent from the draining station into the container. Structural key configurations, uniquely associated with a specific anesthetic, are preferably provided at the connection of the container and connector and at the connection of the draining station and connector.

Abstract translation: 提供一种用于从麻醉蒸发器的储存器排出麻醉剂的系统。 该系统包括具有入口的麻醉剂容器，药剂可以排出入口。 蒸发器具有限定出口并且在蒸发器储存器和出口之间限定排放通道的排水站。 阀可操作以打开和关闭排水通道。 连接器设置有用于连接到出口处的排水站的接收端。 连接器具有用于连接到容器入口的排放端。 连接器将容器保持在排水站出口下方，并且在接收端和排放端之间限定了一个传送通道，用于将试剂从排水站排出到容器中。 优选地，在容器和连接器的连接处以及在排水站和连接器的连接处提供与特定麻醉剂唯一相关联的结构关键构造。

公开(公告)号：WO1998022488A1

公开(公告)日：1998-05-28

申请号：PCT/US1997020836

申请日：1997-11-17

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  PREMCHANDRAN, Ramiya, H. ,  THOMAS, Albert, V. ,  BUSSE, Juliette, K. ,  DETE, John, E.

IPC: C07H17/08

CPC classification number: C07H17/08

Abstract: A process for the preparation of N-demethyl-4"-deoxy-erythromycins A and B, having formula (I), wherein R is H or OH, by stepwise addition of iodine and base to the N-dimethyl-4"-deoxy-erythromycin, preferably, accompanied by sparging with an inert gas.

Abstract translation: 制备具有式（I）的N-脱甲基-4“ - 脱氧 - 红霉素A和B的方法，其中R a是H或OH，通过逐步加入碘和碱向N-二甲基-4 “脱氧红霉素，优选伴随着用惰性气体喷雾。

公开(公告)号：WO1998022437A1

公开(公告)日：1998-05-28

申请号：PCT/US1997021081

申请日：1997-11-18

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  WANG, Wei-bo ,  LI, Qun ,  CHU, Daniel, T. ,  HASVOLD, Lisa, Anne

IPC: C07D207/14

CPC classification number: C07D207/14 ,  C07D455/02 ,  C07D471/04 ,  Y02P20/55

Abstract: A process for the preparation of chiral 3-aminopyrrolidine of formula (I) and analogous bicyclic derivatives of formula (II) from dihydroxy olefins such as for the formula: HO-CH2-CH=CH-CH2-OAr by treatment with titanium isopropoxide, an optically active tartrate ester and tert-butyl hydroperoxide, followed by subsequent alkylation of the intermediate with an alkyl or alkenyl magnesium halide, then pyrrolidine ring formation by condensation with an arylmethylamine, subsequent chiral replacement of a ring hydroxyl group with an amino group with further protection thereof, optional additional substitution closing of the second ring, and hydrogenolysis to remove a ring-nitrogen protecting group.

Abstract translation: 通过用异丙醇钛处理从二羟基烯烃如式HO-CH2-CH = CH-CH2-OAr制备式（I）的手性3-氨基吡咯烷和式（Ⅱ）的类似双环衍生物的方法， 光学活性酒石酸酯和叔丁基过氧化氢，然后用烷基或烯基卤化镁随后烷基化中间体，然后通过与芳基甲胺缩合形成吡咯烷环，随后进一步用氨基取代环羟基 其保护，第二环的任选的另外的取代封闭，以及氢解以除去环 - 氮保护基。

公开(公告)号：WO1998022106A1

公开(公告)日：1998-05-28

申请号：PCT/US1997020794

申请日：1997-11-12

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  LIPARI, John ,  AL-RAZZAK, Laman, A. ,  GHOSH, Soumojeet ,  GAO, Rong ,  KAUL, Dilip

IPC: A61K31/425

CPC classification number: A61K38/55 ,  A61K9/4858 ,  A61K31/341 ,  A61K31/426 ,  A61K31/4433 ,  A61K31/47 ,  A61K31/4704 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/513 ,  A61K31/5375 ,  A61K31/551 ,  A61K38/05 ,  A61K47/10 ,  A61K47/12 ,  A61K47/26 ,  A61K47/44 ,  Y02A50/465

Abstract: A liquid pharmaceutical composition providing improved oral bioavailability is disclosed for compounds which are inhibitors of HIV protease. In particular, the composition comprises a solution in a pharmaceutically acceptable organic solvent of (a) the HIV protease inhibitor and optionally, (b) a surfactant. The composition can optionally be encapsulated in either hard gelating capsules or soft elastic capsules (SEC).

Abstract translation: 对于作为HIV蛋白酶抑制剂的化合物，公开了提供改善的口服生物利用度的液体药物组合物。 特别地，组合物包含（a）HIV蛋白酶抑制剂和任选的（b）表面活性剂的药学上可接受的有机溶剂中的溶液。 组合物可任选地包封在硬胶囊或软弹性胶囊（SEC）中。

公开(公告)号：WO1998017829A2

公开(公告)日：1998-04-30

申请号：PCT/US1997019467

申请日：1997-10-17

Applicant: ABBOTT LABORATORIES

Inventor： ABBOTT LABORATORIES ,  KROEGER, Paul, E. ,  ABRAVAYA, Klara ,  GORZOWSKI, Jacek, J. ,  HOENLE, Robert, J. ,  MOORE, Jennifer, J.

IPC: C12Q01/68

CPC classification number: C12Q1/708

Abstract: Probe sequences that are useful for detecting oncogenic HPV types 16, 18, 31, 33, 35, 39, 45, 51, 52, 56, 58, 59 and 68 are herein provided. These sequences can be used in hybridization assays or amplification based assays designed to detect the presence of these oncogenic HPV types in a test sample. Additionally, the sequences can be provided as part of a kit.

Abstract translation: 本文提供了可用于检测致癌HPV类型16,18,31,33,35,39,45,51,52,56,58,59和68的探针序列。 这些序列可用于杂交测定或基于扩增的测定，其设计用于检测测试样品中这些致癌HPV类型的存在。 另外，序列可以作为试剂盒的一部分提供。

公开(公告)号：WO1998014785A1

公开(公告)日：1998-04-09

申请号：PCT/JP1997003065

申请日：1997-09-02

Applicant: ABBOTT LABORATORIES ,  OHTA, Yumi ,  MORIKAWA, Tetsuya ,  SHIGA, Tetsuya ,  ISHII, Yuko ,  SAITO, Mitsuhiro

Inventor： ABBOTT LABORATORIES

IPC: G01N35/06

CPC classification number: G01N35/10 ,  G01N1/38 ,  G01N2035/1032 ,  Y10T436/114998 ,  Y10T436/115831 ,  Y10T436/119163 ,  Y10T436/25625 ,  Y10T436/2575

Abstract: In an automatic sample examination and measurement instrument for use in conducting random measurement concerning a plurality of items, the measurement accuracy and measurement reproducibility are improved, and failure, which is ascribed to inclusion of bubbles, of an aliquoting apparatus is prevented. Diluent is fed into sample-containing dilution vessels (11) by an aliquoting means so as to prepare diluted samples to be used for measurement. In order to remove small bubbles (13) produced during the preparation of such diluted samples, a predetermined quantity of diluted samples (12) are sucked from upper surfaces thereof by the aliquoting means, discharged into waste liquid cups, and discarded. The diluted samples (12) remaining in the dilution vessels (11) are used for measurement. Thus, the measurement accuracy and measurement reproducibility are improved, and failure, which is ascribed to inclusion of bubbles, of the aliquoting apparatus is prevented.

Abstract translation: 在用于对多个项目进行随机测量的自动样品检查和测量仪器中，提高了测量精度和测量再现性，并且防止了等分装置的气泡引起的故障。 将稀释液通过等分装置送入含样品的稀释容器（11）中，以制备用于测量的稀释样品。 为了除去在制备这些稀释样品期间产生的小气泡（13），通过等分装置从上表面吸入预定量的稀释样品（12），排出到废液杯中并丢弃。 残留在稀释容器（11）中的稀释样品（12）用于测量。 因此，提高了测量精度和测量再现性，并且防止了等分装置的气泡引起的故障。