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414 条记录 (耗时 0.024 秒)

    25-methylene and 24-25 -epoxy marcfortines and paraherquamides
    65.
    发明授权
    25-methylene and 24-25 -epoxy marcfortines and paraherquamides 失效
    25-亚甲基和24-25-环氧马可氟汀和对甲酰喹啉

    公开(公告)号：US5886180A

    公开(公告)日：1999-03-23

    申请号：US924347

    申请日：1997-09-05

    申请人： Byung H. Lee ,  Michael F. Clothier

    发明人： Byung H. Lee ,  Michael F. Clothier

    IPC分类号： A01N43/90 ,  A61K31/55 ,  A61P33/00 ,  C07D491/22 ,  C07D241/36

    CPC分类号： C07D491/22

    摘要： The present invention are marefortines and paraherquamides where the 7-member oxygenated ring has been modified to produce 25-methylene compounds (VII) and 24,25-epoxy compounds (VIII) all of which are useful as antiparasitic agents against endo and ecto parasites, particularly helminths and arthropods.

    摘要翻译： 本发明是马来酸和对甲酰喹啉，其中7元氧化环已被改性以产生25-亚甲基化合物（VII）和24,25-环氧化合物（VIII），所有这些都可用作抗内寄生虫和寄生虫的抗寄生虫剂， 特别是蠕虫和节肢动物。

    Antiarrhythmic (S)-enantiomers of methanesulfonamides
    67.
    发明授权
    Antiarrhythmic (S)-enantiomers of methanesulfonamides 失效
    甲磺酰胺的抗心律不齐（S） - 对映异构体

    公开(公告)号：US5874475A

    公开(公告)日：1999-02-23

    申请号：US860531

    申请日：1997-06-20

    申请人： Jackson B. Hester, Jr. ,  J. Kenneth Gibson

    发明人： Jackson B. Hester, Jr. ,  J. Kenneth Gibson

    IPC分类号： C07C311/08 ,  A61K31/18

    CPC分类号： C07C311/08 ,  C07B2200/07 ,  Y10S514/821

    摘要： Compounds of formula (I) and pharmacologically acceptable salts thereof wherein: n is 1 to 3, R is an alkyl, R.sub.1 is hydrogen or alkyl, R.sub.2 is alkyl, R.sub.3 is an alkyl; b) alkyl substituted with an aryl, heteroaryl or cycloalkyl; c) alkyl substituted with one to eight fluorine atoms; d) cycloalkyl; e) alkenyl; f) alkyl substituted with one to three hydroxy, acyloxy or alkoxy substituents, and where the sum of carbons in R.sub.2 and R.sub.3 is greater than five br where R.sub.2 and R.sub.3 with the nitrogen atom form a saturated heterocyclic group having one nitrogen and form 4-8 carbon atoms or a 4-substituted piperazine group in which the 4-substituent can be alkyl, aryl, benzyl, or heteroaryl, and X is hydrogen, hydroxy, alkoxy, alkyl, carbon trifluoride or a halogen, or compounds of formula (I') and pharmacologically acceptable salts thereof wherein: n is 1 to 3, R is an alkyl, R.sub.1 is hydrogen or alkyl, R.sub.2 is an alkyl, R.sub.3 is an alkyl substituted with an aryl, heteroaryl or cycloalkyl, or an alkyl substituted with one to eight fluorine atoms, one to three hydroxy, acyloxy or alkoxy substituents, and where the sum of carbons in R.sub.2 and R.sub.3 is greater than five; X is hydrogen, hydroxy, alkoxy, alkyl, carbon trifluoride or a halogen, useful as class III antiarrhythmic agents.

    摘要翻译： PCT No.PCT / US95 / 16017 Sec。 371日期：1997年6月20日 102（e）日期1997年6月20日PCT 1995年12月21日PCT PCT。 公开号WO96 / 21643 日本时间1996年7月18日式（I）化合物及其药学上可接受的盐，其中n为1至3，R为烷基，R 1为氢或烷基，R 2为烷基，R 3为烷基; b）被芳基，杂芳基或环烷基取代的烷基; c）被1至8个氟原子取代的烷基; d）环烷基; e）烯基; f）被1至3个羟基，酰氧基或烷氧基取代基取代的烷基，其中R 2和R 3中的碳的和大于5个Br，其中R 2和R 3与氮原子形成具有一个氮的饱和杂环基并形成4- 8个碳原子或4-取代的哌嗪基，其中4-取代基可以是烷基，芳基，苄基或杂芳基，X是氢，羟基，烷氧基，烷基，三氟化碳或卤素，或式（I '）及其药理学上可接受的盐，其中n为1至3，R为烷基，R 1为氢或烷基，R 2为烷基，R 3为被芳基，杂芳基或环烷基取代的烷基或被一个 至8个氟原子，一至三个羟基，酰氧基或烷氧基取代基，并且其中R2和R3中的碳之和大于5; X是氢，羟基，烷氧基，烷基，三氟化碳或卤素，可用作III类抗心律失常药。

    Scintillation proximity assay for N-acetylgalactosaminyltransferase activity
    68.
    发明授权
    Scintillation proximity assay for N-acetylgalactosaminyltransferase activity 失效
    N-乙酰半乳糖胺转移酶活性的闪烁邻近测定

    公开(公告)号：US5861318A

    公开(公告)日：1999-01-19

    申请号：US340283

    申请日：1994-11-16

    申请人： Ake P. Elhammer

    发明人： Ake P. Elhammer

    IPC分类号： C07K7/06 ,  C12Q1/48 ,  G01N33/543

    CPC分类号： C07K7/06 ,  C12Q1/48

    摘要： This invention comprises a scintillation proximity assay designed to assay for the presence of N-acetylgalactosaminyltransferase, also known as GalNAc-transferase. The assay is most conveniently carried out on 96-well microtiterplates. The assay is especially suitable for large volume screens for compounds affecting GalNAc-transferase activity.

    摘要翻译： 本发明包括设计用于测定N-乙酰半乳糖胺基转移酶（也称为GalNAc-转移酶）的存在的闪烁亲近测定。 该测定最方便地在96孔微量滴定板上进行。 该测定特别适用于影响GalNAc转移酶活性的化合物的大体积筛选。

    DNA encoding a novel kidney ATP-dependent potassium channels
    69.
    发明授权
    DNA encoding a novel kidney ATP-dependent potassium channels 失效
    DNA编码新型肾ATP依赖性钾通道

    公开(公告)号：US5831055A

    公开(公告)日：1998-11-03

    申请号：US709923

    申请日：1996-09-09

    申请人： Michael J. Bienkowski

    发明人： Michael J. Bienkowski

    IPC分类号： C12N15/00 ,  C07K14/47 ,  C07K14/705 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N15/12 ,  C12Q1/02 ,  C12N15/09 ,  C12N15/10 ,  C12N15/11

    CPC分类号： C07K14/705

    摘要： The present invention comprises human DNA compositions, including cDNA clones, with full sequences, called, KIRK-2 and KIRK-3, encoding proteins that confer potassium channel activity to membranes or recipient cell lines. The DNA compositions include structural genes coding for the potassium channel proteins, expression and replication plasmids or vectors containing the structural genes and host cells expressing those genes. Methods of screening compounds for potassium channel modulating activity are also described.

    摘要翻译： 本发明包括人类DNA组合物，包括具有完整序列的cDNA克隆，称为KIRK-2和KIRK-3，其编码赋予膜或受体细胞系钾通道活性的蛋白质。 DNA组合物包括编码钾通道蛋白，表达和复制质粒的结构基因或含有结构基因的载体和表达这些基因的宿主细胞。 还描述了筛选化合物钾通道调节活性的方法。

    Fine-beaded colestipol hydrochloride and pharmaceutically elegant dosage forms made therefrom
    70.
    发明授权
    Fine-beaded colestipol hydrochloride and pharmaceutically elegant dosage forms made therefrom 失效
    精细串珠盐酸舍曲坦泊醇和由其制成的药学上优雅的剂型

    公开(公告)号：US5807582A

    公开(公告)日：1998-09-15

    申请号：US289141

    申请日：1994-08-11

    申请人： Dae Yang Cha

    发明人： Dae Yang Cha

    IPC分类号： A61K31/785 ,  A61K9/14 ,  A61K9/20

    CPC分类号： A61K31/785 ,  Y10S514/951

    摘要： The present invention provides for an improvement in the emulsion copolymerization process for the preparation of fine-beaded colestipol hydrochloride (FBCH) wherein the improvement comprises: 1) utilizing a weight ratio of water to polyethylenepolyamine in the process of 1.8 to 3.6 grams per gram, and 2) utilizing a weight ratio of surface active agent or surfactant to polyethylenepolyamine in the process of 1.0 to 3.0 grams per kilogram. The colestipol hydrochloride product thus produced is a novel fine-beaded form of a known pharmaceutical composition, yielding pharmaceutically elegant dosage forms exhibiting increased potency, including non-gritty oral powders and oral tablets. Conventional colestipol hydrochloride was heretofore available in large spherical granules which produced less elegant (gritty) oral suspensions.

    摘要翻译： 本发明提供了用于制备细珠状的考来替泊盐酸盐（FBCH）的乳液共聚方法的改进，其中改进包括：1）在1.8-3.6克/克的过程中使用水与聚亚乙基多胺的重量比， 和2）在1.0-3.0克/千克的过程中使用表面活性剂或表面活性剂与聚亚乙基多胺的重量比。 如此生产的盐酸考来替泊是一种新颖的已知药物组合物的细珠状形式，产生显示出增强效力的药学上优雅的剂型，包括非粗粒口服粉剂和口服片剂。 迄今为止，常规的盐酸考来替泊可用于产生较不优雅（粗壮）口服悬浮液的大球形颗粒。