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1. 发明申请

WO1998017631A2 PESTICIDES 审中-公开
标题翻译：农药
公开(公告)号：WO1998017631A2
公开(公告)日：1998-04-30
申请号：PCT/EP1997005857
申请日：1997-10-23
申请人： NOVARTIS AG , MÜLLER, Urs
发明人： NOVARTIS AG
IPC分类号： C07C251/00
CPC分类号： C07D213/643 , C07C251/60 , C07D231/12 , C07D233/56 , C07D239/34 , C07D249/08 , C07D277/28 , C07D277/32 , C07D307/81 , C07D417/04
摘要： The invention relates to novel pesticidally active compounds of formula (1) and to their possible isomers and mixtures of isomers, wherein: R1 is hydrogen, C1-C5alkyl, C3-C6alkenyl, C3-C6alkynyl, or Ar-C1-C5alkyl unsubstituted or substituted in the aryl moiety by halogen, C1-C5alkyl, C1-C5haloalkyl, C1-C5haloalkoxy or by cyano; R2 is C1-C5alkyl, C1-C3alkoxy-C1-C5alkyl, C3-C6alkenyl, C3-C6alkynyl, or Ar-C1-C5alkyl unsubstituted or substituted in the aryl moiety by halogen, C1-C5alkyl, C1-C5haloalkyl or by cyano; R3/R4 are each independently hydrogen, C1-C5alkyl or C1-C3alkoxy-C1-C5alkyl; A is a ketimino or aldimino group; and X is oxygen, NH or NR9 wherein R9 is hydrogen or C1-C5alkyl. The novel active ingredients have plant-protecting properties and are suitable for the protection of plants against infestation by phytopathogenic microorganisms.
摘要翻译：本发明涉及式（1）的新型杀虫活性化合物及其可能的异构体和异构体混合物，其中：R 1是氢，C 1 -C 5烷基，C 3 -C 6烯基，C 3 -C 6炔基或未取代或取代的Ar-C 1 -C 5烷基在芳基部分由卤素，C 1 -C 5烷基，C 1 -C 5卤代烷基，C 1 -C 5卤代烷氧基或氰基取代; R 2是在芳基部分被卤素，C 1 -C 5烷基，C 1 -C 5卤代烷基或氰基取代的C 1 -C 5烷基，C 1 -C 3烷氧基-C 1 -C 5烷基，C 3 -C 6烯基，C 3 -C 6炔基或C 1 -C 5烷基。 R 3 / R 4各自独立地为氢，C 1 -C 5烷基或C 1 -C 3烷氧基-C 1 -C 5烷基; A是酮缩酮或阿霉素基; 并且X是氧，NH或NR 9，其中R 9是氢或C 1 -C 5烷基。新型活性成分具有植物保护性质，适用于防止植物对植物病原微生物侵袭的侵害。

2. 发明申请

WO1998031704A2 TACHYKININ ANTAGONISTS 审中-公开
公开(公告)号：WO1998031704A2
公开(公告)日：1998-07-23
申请号：PCT/EP1997007307
申请日：1997-12-29
申请人： NOVARTIS AG , NOVARTIS PHARMACEUTICALS UK LIMITED , WALPOLE, Christopher, Simon, John , PRASHAD, Mahavir , HAR, Denis
发明人： NOVARTIS AG , NOVARTIS PHARMACEUTICALS UK LIMITED
IPC分类号： C07K05/00
CPC分类号： C07K5/06165 , A61K38/00 , C07K7/22
摘要： Compounds of formula (I) wherein X is -CH2-, -CO- or direct linkage, Y is -O-, -S- or -NH-, R1 is phenyl, R2=H or phenyl and R3 is H or -CH - and their pharmaceutically acceptable salts have tachykinin antagonist activity and are useful as pharmaceuticals e.g. for the treatment of pain and migraine.
摘要翻译：其中X为-CH 2 - ， - CO-或直接键合的式（I）化合物，Y为-O - ， - S-或-NH-，R1为苯基，R2 = H或苯基，R3为H或-CH 其药学上可接受的盐具有速激肽拮抗剂活性，并且可用作药物例如用于治疗痛苦和偏头痛。

3. 发明申请

WO1998028313A1 (THIO)MORPHOLINE-SUBSTITUTED CARBOXYLIC AND PHOSPHINIC ACIDS 审中-公开
标题翻译：（THIO）吗啉取代的羧基和磷酸
公开(公告)号：WO1998028313A1
公开(公告)日：1998-07-02
申请号：PCT/EP1997007235
申请日：1997-12-22
申请人： NOVARTIS AG , COOKE, Nigel, Graham , IRVING, Edward , FRÖSTL, Wolfgang
发明人： NOVARTIS AG
IPC分类号： C07F09/6533
CPC分类号： C07D265/30 , C07D279/12 , C07F9/6533 , C07F9/6544
摘要： A compound of formula (I), wherein X is carboxy or a group of formula -PO(OH)-R where R is an unsubstituted or substituted hydrocarbyl group, R is a monovalent aromatic or araliphatic group connected through a carbon atom thereof to the indicated carbon atom, R is hydrogen or an unsubstituted or substituted hydrocarbyl group, and Y is oxygen or sulphur when X is carboxy, or sulphur when X is -PO(OH)-R, or a salt or ester thereof. Compound I is useful in the treatment or prevention of a condition characterized by stimulation of a GABAB receptor.
摘要翻译：式（I）化合物，其中X是羧基或式-PO（OH）-R基团，其中R是未取代或取代的烃基，R 1是通过碳原子连接的一价芳族或芳脂族基团其中R 2为氢或未取代或取代的烃基，当X为羧基时，Y为氧或硫，或X为-PO（OH）-R时为硫或盐或酯它们。化合物I可用于治疗或预防以刺激GABA B受体为特征的病症。

4. 发明申请

WO1998027218A2 METHODS FOR CONFERRING INSECT RESISTANCE TO A MONOCOT USING A PEROXIDASE CODING SEQUENCE 审中-公开
标题翻译：使用过氧化物酶编码序列确定单体抗性的方法
公开(公告)号：WO1998027218A2
公开(公告)日：1998-06-25
申请号：PCT/EP1997007089
申请日：1997-12-17
申请人： NOVARTIS AG , OHIO STATE UNIVERSITY , U.S. DEPARTMENT OF AGRICULTURE , PRIVALLE, Laura, Stein , LAGRIMINI, Lawrence, Mark , DOWD, Patrick, Francis , ESTRUCH, Juan, Jose
发明人： NOVARTIS AG , OHIO STATE UNIVERSITY , U.S. DEPARTMENT OF AGRICULTURE
IPC分类号： C12N153/82
CPC分类号： C12N9/0065 , A01N65/38 , C12N15/8286 , Y02A40/162
摘要： The present invention relates, in general, to methods and compositions for controlling insects in monocotyledonous plants (monocots), particularly maize. More precisely, the present invention relates to (1) a method for controlling insects comprising feeding or contacting an insect with an insecticidal amount of transgenic monocotyledonous plant cells comprising a recombiant DNA sequence comprising a coding sequence encoding peroxidase and (2) a fertile transgenic monocot plant comprising a recombinant DNA sequence comprising a coding sequence encoding peroxidase.
摘要翻译：本发明一般涉及用于在单子叶植物（单子叶植物），特别是玉米中控制昆虫的方法和组合物。更准确地说，本发明涉及（1）一种防治昆虫的方法，包括向昆虫喂食或接触杀虫剂量的转基因单子叶植物细胞，其包含重组DNA序列，其包含编码过氧化物酶的编码序列和（2）可育转基因单子叶植物植物包含含有编码过氧化物酶的编码序列的重组DNA序列。

5. 发明申请

WO1998027074A1 PROCESS FOR THE PREPARATION OF THIAZOLE DERIVATIVES 审中-公开
标题翻译：制备噻唑衍生物的方法
公开(公告)号：WO1998027074A1
公开(公告)日：1998-06-25
申请号：PCT/EP1997007087
申请日：1997-12-17
申请人： NOVARTIS AG , PITTERNA, Thomas , SZCZEPANSKI, Henry , MAIENFISCH, Peter , HÜTER, Ottmar, Franz , RAPOLD, Thomas , SENN, Marcel , GÖBEL, Thomas , O'SULLIVAN, Anthony, Cornelius , SEIFERT, Gottfried
发明人： NOVARTIS AG
IPC分类号： C07D277/32
CPC分类号： C07D277/32 , C07D277/16 , C07D277/36 , C07D417/06
摘要： The invention relates to a process for the preparation of a compound of formula (I), wherein Q, Y, Z, R1, R2, R3, R4 and R5 are as defined in the specification, which comprises a) reacting a compound of formula (II), with a halogenating agent to form a compound of formula (III), or b) converting a compound of formula (II) by means of a halogenating agent into a compound of formula (IV); optionally c) converting the compound of formula (IV) into a compound of formula (III); d) converting a compound of formula (III) by means of a compound of formula (V) into a compound of formula (VI); or e) converting a compound (IV) by means of a compound (V) into a compound (VI); and f) converting a compound (VI) by means of a chlorinating agent into a compound (I); a compound (IV); to a process for the preparation of a compound (III) and to a process for the preparation of a compound (IV).
摘要翻译：本发明涉及制备式（I）化合物的方法，其中Q，Y，Z，R 1，R 2，R 3，R 4和R 5如本说明书中所定义，其包括：a）使式（II）化合物与卤化剂反应形成式（III）化合物，或b）将式（Ⅱ）化合物用卤化剂转化为式（Ⅳ）化合物; 任选地c）将式（IV）的化合物转化成式（III）的化合物; d）通过式（V）化合物将式（III）化合物转化为式（VI）化合物; 或e）通过化合物（V）将化合物（IV）转化为化合物（VI）; 和f）通过氯化剂将化合物（VI）转化为化合物（I）; 化合物（IV）; 涉及制备化合物（III）的方法和制备化合物（IV）的方法。

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

WO1998015532A1 SOLID PHASE SYNTHESIS OF HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：固相化合物的固相合成
公开(公告)号：WO1998015532A1
公开(公告)日：1998-04-16
申请号：PCT/EP1997005547
申请日：1997-10-08
申请人： NOVARTIS AG , MARZINZIK, Andreas , FELDER, Eduard
发明人： NOVARTIS AG
IPC分类号： C07D239/42
CPC分类号： C07D231/12 , C07D211/86 , C07D211/90 , C07D213/56 , C07D213/85 , C07D215/14 , C07D239/22 , C07D239/26 , C07D239/42 , C07D243/12 , C07D401/04 , C07D403/04 , C07D409/04 , C07D417/04 , C40B40/00
摘要： Here we report a study on a reaction sequence on solid phase, suitable for the generation of molecular diversity on small heterocycles. For each reaction, suitable conditions on solid phase were worked out and a variety of reactive agents (building blocks) was utilized in an effort to grasp the system's breadth of applicability. The inventive reaction sequence can be applied, for example, to exploit by the combinatorial approaches of the split and mix concept. The reaction sequence comprises the following steps: a) a solid carrier having reactive surface groups is loaded directly or via a spacer group with a compound bearing an aldehyde or a methylketon function, b) said function is modified using the Witting reaction or the aldol condensation, c) the heterocyclic ring is closed using a compound comprising two nucleophiles, wherein at least one of the said nucleophiles is NH2.
摘要翻译：在这里，我们报告了关于固相反应序列的研究，适用于在小杂环上产生分子多样性。对于每个反应，制备了固相上的合适条件，并利用各种反应剂（构件）来努力掌握系统的适用范围。本发明的反应序列可以应用于例如通过分组和混合概念的组合方法的利用。反应顺序包括以下步骤：a）具有反应性表面基团的固体载体直接或通过间隔基团与具有醛或甲基酮官能团的化合物一起加载，b）使用Witting反应或醛醇缩合 c）使用包含两个亲核试剂的化合物封闭杂环，其中所述亲核试剂中的至少一个是NH 2。

8. 发明申请

WO1998011242A2 NEUROLOGICAL DISEASE MODEL 审中-公开
标题翻译：神经病变模型
公开(公告)号：WO1998011242A2
公开(公告)日：1998-03-19
申请号：PCT/EP1997004985
申请日：1997-09-11
申请人： NOVARTIS AG , VAN DER PUTTEN, Petrus, Herman, Maria
发明人： NOVARTIS AG
IPC分类号： C12N15/85
CPC分类号： C12N15/8509 , A01K67/0276 , A01K2217/075 , A01K2227/105 , A01K2267/03 , A01K2267/0356 , C07K14/70571 , C12N2800/30
摘要： There is provided the use of a metabotropic glutamate receptor mGluR7 agonist for the facilitation of neurotransmitter release from a nerve ending and the treatment of neurological conditions, including epilepsy. Moreover, the invention provides transgenic knockout non-human mammals lacking the mGluR7 gene, suitable for studying mGluR7 and modulators thereof as well as epilepsy.
摘要翻译：提供了代谢型谷氨酸受体mGluR7激动剂用于促进从神经末梢释放神经递质和治疗神经病症（包括癫痫）的方法。此外，本发明提供了缺乏适合于研究mGluR7及其调节剂以及癫痫的mGluR7基因的转基因敲除非人哺乳动物。

9. 发明申请

WO1998011235A2 TRANSGENIC PLANTS EXPRESSING CELLULOLYTIC ENZYMES 审中-公开
标题翻译：表达微生物酶的转基因植物
公开(公告)号：WO1998011235A2
公开(公告)日：1998-03-19
申请号：PCT/US1997016187
申请日：1997-09-12
申请人： NOVARTIS AG , LEBEL, Edouard , HEIFETZ, Peter , WARD, Eric , UKNES, Scott
发明人： NOVARTIS AG
IPC分类号： C12N15/56
CPC分类号： C12N15/8216 , C12N9/2437 , C12N15/8214 , C12N15/8217 , C12N15/8237 , C12N15/8238 , C12N15/8242 , C12N15/8246 , C12Y302/01004 , Y02E50/16 , Y02E50/17
摘要： The invention provides novel methods of controlling gene expression in plastids, using an inducible, transactivator-mediated system, and plants comprising the novel expression systems. The present invention further describes the production of cellulose-degrading enzymes in plants via the application of genetic engineering techniques. Cellulase coding sequences are fused to promoters active in plants and transformed into the nuclear genome and the chloroplast genome. As cellulases may be toxic to plants, preferred promoters are those that are chemically-inducible. In this manner, expression of the cellulase genes transformed into plants may be chemically induced at an appropriate time. In addition, the expressed cellulases may be targeted to vacuoles or other organelles to alleviate toxicity problems. The present invention finds utility in any industrial process requiring a plentiful supply of cellulases, but particularly finds utility in the conversion of cellulosic biomass to ethanol.
摘要翻译：本发明提供了使用诱导型反式激活因子介导的系统以及包含新型表达系统的植物来控制质体中基因表达的新方法。本发明进一步描述了通过应用基因工程技术在植物中生产纤维素降解酶。纤维素酶编码序列与在植物中有活性的启动子融合，并转化到核基因组和叶绿体基因组中。由于纤维素酶对植物有毒性，优选的启动子是化学诱导型的启动子。以这种方式，可以在适当的时间化学诱导转化到植物中的纤维素酶基因的表达。此外，表达的纤维素酶可以靶向液泡或其他细胞器以减轻毒性问题。本发明可用于需要大量供应纤维素酶的任何工业过程中，特别是在纤维素生物质转化为乙醇方面具有实用价值。

10. 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。

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