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1. 发明申请

WO1997021451A1 ANTI-COCAINE VACCINE 审中-公开
标题翻译：抗COCAINE VACCINE
公开(公告)号：WO1997021451A1
公开(公告)日：1997-06-19
申请号：PCT/US1996019982
申请日：1996-12-16
申请人： THE SCRIPPS RESEARCH INSTITUTE , WIRSCHING, Peter , JANDA, Kim, D.
发明人： THE SCRIPPS RESEARCH INSTITUTE
IPC分类号： A61K39/395
CPC分类号： C07D451/04 , A61K31/46 , A61K39/0013 , A61K47/6803 , A61K2039/6081 , C07D451/12 , C07F9/6561 , C07K16/44 , Y10S530/807
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：抗可卡因疫苗采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作用。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。

2. 发明申请

WO1993014114A1 PEPTIDE LINKAGE UNIT COMPRISING METHYLENE PHOSPHINIC ACID 审中-公开
标题翻译：含有亚甲基磷酸的肽链接单元
公开(公告)号：WO1993014114A1
公开(公告)日：1993-07-22
申请号：PCT/US1993000228
申请日：1993-01-11
申请人： THE SCRIPPS RESEARCH INSTITUTE , JANDA, Kim, D. , WIRSCHING, Peter , IKEDA, Shoji
发明人： THE SCRIPPS RESEARCH INSTITUTE
IPC分类号： C07K05/02
CPC分类号： C07K7/02 , A61K38/00 , B60W40/09 , C07F9/301 , C07F9/3241 , C07K5/021 , F16H2059/003 , F16H2312/02
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 P1 and P1' residues and have a length of 3 to about 15 amino acid residues.
摘要翻译：肽连接单元用于连接肽和假肽序列，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。

3. 发明申请

WO1997035199A1 AZATIDE PEPTIDOMIMETICS 审中-公开
公开(公告)号：WO1997035199A1
公开(公告)日：1997-09-25
申请号：PCT/US1997004963
申请日：1997-03-20
申请人： THE SCRIPPS RESEARCH INSTITUTE , JANDA, Kim, D. , HAN, Hyunsoo
发明人： THE SCRIPPS RESEARCH INSTITUTE
IPC分类号： G01N33/53
CPC分类号： C40B40/04 , C07C281/06 , C40B50/08
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。

4. 发明申请

WO1998035927A1 PEG-BOUND ALKALOID LIGANDS AND USE THEREOF 审中-公开
标题翻译： PEG环糊精配体及其用途
公开(公告)号：WO1998035927A1
公开(公告)日：1998-08-20
申请号：PCT/US1997002442
申请日：1997-02-14
申请人： THE SCRIPPS RESEARCH INSTITUTE , JANDA, Kim, D. , HAN, Hyunsoo
发明人： THE SCRIPPS RESEARCH INSTITUTE
IPC分类号： C07C29/03
CPC分类号： C07C29/48 , C07C33/26 , C07C31/20
摘要： Polyethylene glycol monomethyl ether-bound alkaloid ligands (PEG-bound alkaloid ligands) are constructed and employed in the ligand-accelerated catalytic (LAC) Sharpless asymmetric dihydroxylation reaction (AD) with a range of olefins. The PEG serves as a scaffold which allows simple product separation, polymer-bound ligand recovery, and recycling of the chiral liquid phase support without a loss of catalytic activity or ligand acceleration.
摘要翻译：聚乙二醇单甲醚结合的生物碱配体（PEG结合的生物碱配体）被构建并用于具有一系列烯烃的配体加速催化（LAC）Sharpless不对称二羟基化反应（AD）中。 PEG用作支架，其允许简单的产物分离，聚合物结合的配体回收和手性液相支持物的循环，而不会失去催化活性或配体加速。

5. 发明申请

WO1996022391A1 ENCODED REACTION CASSETTE 审中-公开
标题翻译：编码反应CASSETTE
公开(公告)号：WO1996022391A1
公开(公告)日：1996-07-25
申请号：PCT/US1996000888
申请日：1996-01-18
申请人： THE SCRIPPS RESEARCH INSTITUTE , JANDA, Kim, D. , FENNIRI, Hicam , LERNER, Richard, A.
发明人： THE SCRIPPS RESEARCH INSTITUTE
IPC分类号： C12Q01/68
CPC分类号： C12Q1/68 , C12N9/0002 , C12Q1/6823 , C12Q1/686
摘要： A reaction cassette has been designed for the highly sensitive detection of the making and breaking of chemical bonds. The system may be employed as a companion device to be used in the search for antibody and other novel catalysts. The cassette also has important clinical applications in the design of diagnostic reagents. In its fully encoded format this methodology is capable of both detecting and decoding chemical events.
摘要翻译：反应盒已被设计用于高灵敏度地检测化学键的制造和断裂。该系统可以用作用于搜索抗体和其他新型催化剂的配套设备。该盒式磁带在诊断试剂的设计中也具有重要的临床应用。在其完全编码格式中，该方法能够检测和解码化学事件。

6. 发明申请

WO1998025929A1 EPOTHILONE ANALOGS 审中-公开
标题翻译： EPOTHILONE模拟
公开(公告)号：WO1998025929A1
公开(公告)日：1998-06-18
申请号：PCT/EP1997007011
申请日：1997-12-12
申请人： NOVARTIS AG , THE SCRIPPS RESEARCH INSTITUTE , NICOLAOU, Costa, Kyriacos , HE, Yun , NINKOVIC, Sacha , PASTOR, Joaquin , ROSCHANGAR, Frank , SARABIA, Francisco , VALLBERG, Hans , VOURLOUMIS, Dionisios , WINSSINGER, Nicolas , YANG, Zhen , KING, Nigel, Paul , FINLAY, Maurice, Raymond, Verschoyle
发明人： NOVARTIS AG , THE SCRIPPS RESEARCH INSTITUTE
IPC分类号： C07D493/04
CPC分类号： C07D417/06 , C07D313/00 , C07D493/04
摘要： Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancers agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of microtubulin assembly. The analogs of epothilone are novel. Several of the analogs are demonstrated to have a superior cytotoxic activity as compared to epothilone A or epothilone B as demonstrated by their enhanced ability to induce the polymerization and stabilization of microtubules.
摘要翻译：埃博霉素A，埃坡霉素B，埃坡霉素类似物和埃坡霉素类似物文库合成。埃博霉素A和B是已知的抗癌剂，其通过微管蛋白装配的诱导和稳定来预防有丝分裂来获得它们的抗癌活性。埃坡霉素的类似物是新颖的。与埃坡霉素A或埃坡霉素B相比，几种类似物被证明具有优异的细胞毒性活性，如通过增强诱导微管聚合和稳定化的能力所证实的。

7. 发明申请

WO1998008854A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO1998008854A2
公开(公告)日：1998-03-05
申请号：PCT/EP1997004649
申请日：1997-08-26
申请人： NOVARTIS AG , THE SCRIPPS RESEARCH INSTITUTE , WONG, Chi-Huey , LIN, Chun-Cheng , WOLTERING, Thomas, J. , MARRON, Thomas, G. , MORIS-VARAS, Francisco , JABLONOWSKI, Jill , WEITZ-SCHMIDT, Gabriele
发明人： NOVARTIS AG , THE SCRIPPS RESEARCH INSTITUTE
IPC分类号： C07H15/00
CPC分类号： C07H7/02 , C07H15/00
摘要： Sialyl Lewis X mimetics which mimic the inhibition of selectin-mediated cellular adhesion by sialyl Lewis X having a core of formula (I).
摘要翻译：本发明涉及模拟选择素诱导的细胞粘附的路易斯X唾液酸化抑制的路易斯X唾液酸模拟物，其具有式（I）的核心。

8. 发明申请

WO1997048819A1 CASSAVA VEIN MOSAIC VIRUS PROMOTERS AND USES THEREOF 审中-公开
标题翻译： CASSAVA VEIN MOSAIC VIRUS促销者及其用途
公开(公告)号：WO1997048819A1
公开(公告)日：1997-12-24
申请号：PCT/US1997010376
申请日：1997-06-20
申请人： THE SCRIPPS RESEARCH INSTITUTE , VERDAGUER, Bertrand , DE KOCHKO, Alexandre , BEACHY, Roger, N. , FAUQUET, Claude
发明人： THE SCRIPPS RESEARCH INSTITUTE
IPC分类号： C12P21/06
CPC分类号： C07K14/005 , C12N15/8216 , C12N2730/00022
摘要： The invention relates to compositions and methods useful for the production of transgenic plants. In particular, the invention relates to cassava vein mosaic virus (CsVMV) promoter sequences and expression cassettes containing CsVMV promoter sequences. The invention describes nucleic acid molecules, vectors and transgenic plants containing promoters derived from CsVMV promoter that are operatively linked to heterologous DNA sequences, and methods for producing transgenic plants containing these promoters.
摘要翻译：本发明涉及可用于生产转基因植物的组合物和方法。特别地，本发明涉及木薯静脉花叶病毒（CsVMV）启动子序列和含有CsVMV启动子序列的表达盒。本发明描述了含有源自与异源DNA序列有效连接的CsVMV启动子的启动子的核酸分子，载体和转基因植物以及用于产生含有这些启动子的转基因植物的方法。

9. 发明申请

WO1997041526A1 SMALL MOLECULE MIMETICS OF ERYTHROPOIETIN 审中-公开
标题翻译： ERYTHROPOIETIN的小分子物质
公开(公告)号：WO1997041526A1
公开(公告)日：1997-11-06
申请号：PCT/US1997007218
申请日：1997-04-28
申请人： THE SCRIPPS RESEARCH INSTITUTE
发明人： THE SCRIPPS RESEARCH INSTITUTE , WILSON, Ian, A. , LIVNAH, Oded , STURA, Enrico, A. , JOHNSON, Dana, L. , JOLLIFFE, Linda, K.
IPC分类号： C07B61/00 , A61B5/00 , C07K7/08 , C07K14/00 , C07K14/505 , G01N33/74 , G06Q50/22
CPC分类号： G01N33/746 , C07K7/08 , C07K14/001 , C07K14/505 , Y10S707/99943
摘要： The invention features computer-assisted methods (100, 102, 104, 106, 200, 202, 204) for identifying molecules which will bind to the EPO receptor and act as an erythropoietin (EPO) mimetic. Preferred EPO mimetics identified using the method of the invention act as agonists of the EPO receptor in one or more in vitro or in vivo biological assays of EPO activity.
摘要翻译：本发明的特征在于用于鉴定将结合EPO受体并用作促红细胞生成素（EPO）模拟物的分子的计算机辅助方法（100,102,104,106,200,2002,204）。使用本发明的方法鉴定的优选EPO模拟物在EPO活性的一个或多个体外或体内生物测定中作为EPO受体的激动剂。

10. 发明申请

WO1997021100A1 HIV PROTEASE INHIBITORS 审中-公开
标题翻译：艾滋病病毒蛋白酶抑制剂
公开(公告)号：WO1997021100A1
公开(公告)日：1997-06-12
申请号：PCT/US1996019571
申请日：1996-12-09
申请人： THE SCRIPPS RESEARCH INSTITUTE , WONG, Chi-Huey , SLEE, Deborah, H. , LASLO, Karen
发明人： THE SCRIPPS RESEARCH INSTITUTE
IPC分类号： G01N33/53
CPC分类号： C12Q1/37 , C07D207/08 , C07D207/12 , C07D207/16 , C07D211/60 , C12Q1/18 , C40B40/04 , G01N2333/16
摘要： Combinatorial libraries of HIV and FIV protease inhibitors are characterized by alpha -keto amide or hydroxyethylamine core structures flanked by on one side by substituted pyrrolidines, piperidines, or azasugars and on the other side by phenylalanine, tyrosine, or substituted tyrosines. The libraries are synthesized via a one step coupling reaction. Highly efficacious drug candidates are identified by screening the libraries for binding and inhibitory activity against both HIV and FIV protease. Drug candidates displaying clinically useful activity against both HIV and FIV protease are identified as being potentially resistive against a loss of inhibitory activity due to development of resistant strains of HIV.
摘要翻译：艾滋病毒和FIV蛋白酶抑制剂的组合文库的特征在于α-酮酰胺或羟乙基胺核心结构，其侧面为取代的吡咯烷酮，哌啶或氮杂异构体，另一侧为苯丙氨酸，酪氨酸或取代的酪氨酸。文库通过一步偶联反应合成。通过筛选文库对HIV和FIV蛋白酶的结合和抑制活性来鉴定高效药物候选物。鉴于HIV和FIV蛋白酶对临床有用的活性的候选药物被鉴定为可能阻止由于HIV的抗性株的发展而导致的抑制活性丧失。

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