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101. 发明申请

WO1997012046A1 IMPROVED INTEGRATION OF EXOGENOUS DNA DELIVERED TO EUKARYOTIC CELLS 审中-公开
标题翻译：改进了提供给原核细胞的异源DNA的整合
公开(公告)号：WO1997012046A1
公开(公告)日：1997-04-03
申请号：PCT/EP1996004006
申请日：1996-09-12
申请人： NOVARTIS AG , HANSEN, Geneviève , CHILTON, Mary-Dell
发明人： NOVARTIS AG
IPC分类号： C12N15/82
CPC分类号： C12N15/8207 , C12N15/8201
摘要： The present invention provides an improved method for achieving stable integration of an exogenous DNA fragment in intact form into the genome of a eukaryotic cell, particularly a plant cell. The method comprises providing the exogenous DNA together with one or more proteins which promote integration of the exogenous DNA to the eukaryotic cell targeted for transformation, wherein the proteins are provided in the form of a chimeric gene or translatable RNA capable of expression in the eukaryotic cell. The method is particularly applied to plant cells to achieve stable integration of an exogenous DNA fragment bounded by T-DNA borders in intact form using integration-promoting proteins derived from Agrobacterium. Transgenic cultures, tissues and whole organisms, particularly transgenic plants, can be generated from cells transformed according to the method of the invention.
摘要翻译：本发明提供了一种改进的方法，用于将完整形式的外源DNA片段稳定整合到真核细胞，特别是植物细胞的基因组中。该方法包括提供外源DNA与一种或多种促进外源DNA整合到靶向转化的真核细胞的蛋白质，其中蛋白质以能够在真核细胞中表达的嵌合基因或可翻译RNA的形式提供。该方法特别适用于植物细胞，以使用来自农杆菌的整合促进蛋白质以完整形式实现由T-DNA边界限制的外源DNA片段的稳定整合。可以从根据本发明的方法转化的细胞产生转基因培养物，组织和整个生物，特别是转基因植物。

102. 发明申请

WO1997008155A1 NOVEL 2,3-DIOXO-1,2,3,4-TETRAHYDRO-QUINOYXALINYL DERIVATIVES 审中-公开
标题翻译：新的2,3-二氧代-1,2,3,4-四氢喹啉衍生物
公开(公告)号：WO1997008155A1
公开(公告)日：1997-03-06
申请号：PCT/EP1996003644
申请日：1996-08-19
申请人： NOVARTIS AG , ACKLIN, Pierre , ALLGEIER, Hans , AUBERSON, Yves , BIOLLAZ, Michel , MORETTI, Robert , OFNER, Silvio , VEENSTRA, Siem, Jacob
发明人： NOVARTIS AG
IPC分类号： C07D241/44
CPC分类号： C07D401/06 , C07D241/44 , C07D401/12 , C07D417/12 , C07F9/650994
摘要： 2,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), wherein one of the radicals R1, and R2 is a group R5 and the other is a group of formula -CH(R6)-alk-R7 (Ia), -alk-CH(R6-R7 (Ib), -alk-N(R8)-X-R7 (Ic), -alk-N (R8)(R9)-X-R7A (Id), -alk-O-X-R7 (Ie) or -alk-S-X-R7 (If), R3, R4 and R5 are each independently of the others hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, R6 is unsubstituted or lower alkylated and/or lower alkanoylated amino, R7 is hydrogen; an aliphatic, cycloaliphatic or heterocycloaliphatic radical; cyano; acyl derived from carbonic acid or from a semiester or semiamide of carbonic acid, from sulfuric acid or from an aliphatic or aromatic sulfonic acid or from phosphoric acid or from a phosphonic acid ester; amino that is unsubtituted or aliphatically or araliphatically substituted and/or substituted by aliphatic, araliphatic or aromatic acyl; or an aromatic or heteroaromatic radical, R8 is hydrogen; an aliphatic or araliphatic radical; or acyl derived from an aliphatic or araliphatic carboxylic acid or from an aliphatic or araliphatic semiester of carbonic acid, or R7 and R8, together with X and the nitrogen atom bonding R8 and X, form an unsubstitued or substituted mono- or di-azaxycloalkyl, azoxacycloalkyl, azathiacycloalkyl or optionally oxidised thiacycloalkyl radical bonded via a nitrogen atom, or an unsubstituted or substituted, optionally partially hxdrogenated aryl or heteroaryl radical, R9 is an aliphatic or araliphatic radical, or R7, R8 and R9 together with X and the nitrogen atom bonding R8, R9 and X, form an unsubstituted or substituted quaternary heteroaryl radical bonded via the quaternary nitrogen atom, with A being the anion of a protonic acid, alk is lower alkylene, and X (unless, together with R7 and R8 and the nitrogen atom bonding R8 and X or together with the nitrogen atom bonding R8, R9 and X, it forms part of one of the mentioned ring systems) is a divalent aliphatic, cycloaliphatic or araliphatic radical or a direct bond, and the pharmaceutically acceptable salts thereof can be used in the preparation of a medicament for the treatment of pathological conditions that are responsive to blocking of AMPA, kainate and/or glycine binding sites of the NMDA receptor.
摘要翻译：式（I）的2,3-二氧代-1,2,3,4-四氢 - 喹喔啉基衍生物，其中基团R 1和R 2之一是基团R 5，另一个是式-CH（R 6） -alk-R7（Ia），-alk-CH（R6-R7（Ib））-alk-N（R8）-X-R7（Ic），-alk-N +（R8）（R9）-X -R7A - （Id），-alk-OX-R7（Ie）或-alk-SX-R7（If），R3，R4和R5各自独立地为氢，低级烷基，卤素，三氟甲基，氰基或硝基，R 6是未取代的或低级烷基化的和/或低级烷酰基化的氨基，R 7是氢;脂族，脂环族或杂环脂族基团;氰基;衍生自碳酸的酰基或来自碳酸的半酯或半酰胺，脂族或芳族磺酸或磷酸或膦酸酯;未取代或脂族或芳烃取代和/或被脂族或芳族酰基取代的氨基;或芳族或杂芳族基团，R 8为氢; 脂肪族或芳脂族辐射 CAL; 或衍生自脂族或芳脂族羧酸的酰基或来自碳酸或R 7和R 8的脂族或芳脂肪族半酯与X以及键合R 8和X的氮原子形成未取代或取代的单 - 或二 - 氮杂环烷基的酰基，氮杂环烷基，氮杂环烷基或任意氧化的经氮原子键合的硫代环烷基，或未取代或取代的，任选部分羟基化的芳基或杂芳基，R 9为脂族或芳脂族基，或者R 7，R 8和R 9与X和氮原子键合 R8，R9和X形成通过季氮原子键合的未取代或取代的季杂芳基，A 1是质子酸的阴离子，alk是低级亚烷基和X（除非与R 7和R 8一起键合R8和X的氮原子或与R8，R9和X键合的氮原子一起形成所述环系中一个的一部分）是二价脂族，脂环族或芳族脂肪族基团或直接键合，并且其药学上可接受的盐可用于制备用于治疗对阻断NMDA受体的AMPA，红藻氨酸和/或甘氨酸结合位点有反应的病理状况的药物。

103. 发明申请

WO1998045185A1 WATER SOLUBLE PACKAGING SYSTEM, FILM AND METHOD 审中-公开
标题翻译：水溶性包装系统，薄膜和方法
公开(公告)号：WO1998045185A1
公开(公告)日：1998-10-15
申请号：PCT/US1997006413
申请日：1997-04-17
申请人： NOVARTIS AG , CHRIS-CRAFT INDUSTRIALS PRODUCTS, INC. , DESMARAIS, Armand, Joseph , KNOOP, Henry, Earl , DULL, Lawrence, Clifford , RAYMOND, Jean, Alain
发明人： NOVARTIS AG , CHRIS-CRAFT INDUSTRIALS PRODUCTS, INC.
IPC分类号： B65D65/46
CPC分类号： B65D65/46
摘要： The present invention relates to a bag packaging system composed of a bag sealable to contain a liquid, in which the bag is composed of a continuous outer water soluble film and an inner continuous protective film layer that allows storage therein of a liquid that would chemically or physically react with the water soluble film but is prevented from doing so by the presence of the continuous protective film layer on the inner portion of the bag.
摘要翻译：本发明涉及一种袋包装系统，其由可密封以容纳液体的袋子组成，袋子由连续的外部水溶性膜和内部连续的保护膜层组成，其允许在其中储存液体，该液体将化学或与水溶性膜物理反应，但是通过在袋的内部存在连续的保护膜层而防止这样做。

104. 发明申请

WO1998029537A2 METHOD FOR PROTECTING PLANTS 审中-公开
标题翻译：保护植物的方法
公开(公告)号：WO1998029537A2
公开(公告)日：1998-07-09
申请号：PCT/EP1997007253
申请日：1997-12-23
申请人： NOVARTIS AG
发明人： NOVARTIS AG , RYALS, John, Andrew , UKNES, Scott, Joseph , MOLINA FERNANDEZ, Antonio , FRIEDRICH, Leslie, Bethards
IPC分类号： C12N15/00
CPC分类号： C12N15/8282 , A01N43/82 , A01N61/00 , A01N65/08 , C07K14/415 , A01N59/20 , A01N57/12 , A01N53/00 , A01N47/14 , A01N43/90 , A01N43/84 , A01N43/653 , A01N43/54 , A01N43/40 , A01N37/50 , A01N37/38 , A01N37/22 , A01N2300/00 , A01N65/00
摘要： The present invention concerns a method of protecting plants from pathogen attack through synergistic disease resistance attained by applying a conventional microbicide to immunomodulated plants. Immunomodulated plants are those in which SAR is activated and are therefore referred to as "SAR-on" plants. Immunomodulated plants may be provided in at least three different ways: by applying to plants a chemical inducer of SAR such as BTH, INA, or SA; through a selective breeding program based on constitutive expression of SAR genes and/or a disease-resistant phenotype; or by transforming plants with one or more SAR genes such as a functional form of the N/M1 gene. By concurrently applying a microbicide to an immunomodulated plant, disease resistance is unexpectedly synergistically enhanced; i.e., the level of disease resistance is greater than the expected additive levels of disease resistance.
摘要翻译：本发明涉及一种通过将常规杀微生物剂施用于免疫调节植物而获得的协同疾病抗性来保护植物免受病原体攻击的方法。免疫调节植物是SAR被激活的植物，因此被称为“SAR-on”植物。免疫调节的植物可以以至少三种不同的方式提供：通过向植物施用诸如BTH，INA或SA的SAR化学诱导剂; 通过基于SAR基因的组成型表达和/或抗病性表型的选择性育种程序; 或通过用一种或多种SAR基因如N / M1基因的功能形式转化植物。通过同时向免疫调节的植物施用杀微生物剂，抗病性意外地协同增强; 即抗病性水平大于预期的抗病性的添加剂水平。

105. 发明申请

WO1998028262A1 O-BENZYL OXIME ETHER DERIVATIVES AS PECTICIDES 审中-公开
公开(公告)号：WO1998028262A1
公开(公告)日：1998-07-02
申请号：PCT/EP1997007122
申请日：1997-12-18
申请人： NOVARTIS AG , HÜTER, Ottmar, Franz , FAROOQ, Saleem , TRAH, Stephan , SZCZEPANSKI, Henry
发明人： NOVARTIS AG
IPC分类号： C07C251/60
CPC分类号： C07C251/40 , C07C251/34 , C07C251/38 , C07C251/60
摘要： Compounds of formula (I), wherein either X is CH or N, Y is OR1 and Z is O, or X is N, Y is NHR8 and Z is O, S or S(=O); U is (a) or (b); R1 is H or C1-C4alkyl; R2 is, for example, H, C1-C4alkyl or halo-C1-C4alkyl; R3 and R4 are, for example, H, C1-C4alkyl or C1-C4alkoxy; l is 0, 1 or 2; R5 and R6 are, for example, C1-C6alkyl, halo-C1-C6alkyl, C3-C6cycloalkyl, C3-C6cycloalkenyl, halo-C3-C6cycloalkyl, C1-C6alkoxy, halo-C1-C6alkoxy or C1-C6alkylthio; R55 is, for example, C1-C6alkyl, halo-C1-C6alkyl, C3-C6cycloalkyl or C3-C6cycloalkenyl; R66 is, for example, hydrogen, C1-C6alkyl, halo-C1-C6alkyl, C3-C6cycloalkyl, C3-C6cycloalkenyl, halo-C3-C6cycloalkyl, C1-C6alkylsulfinyl or halo-C1-C6alkylsulfinyl; m is 0, 1, 2, 3, 4, or 5; n is 0, 1, 2, 3 or 4; q is 0, 1, 2, 3 or 4; A is a direct bond, C1-C10alkylene, -C(=O)-, -C(=S)- or halo-C1-C10alkylene and R7 is a radical R10; or A is, for example, C1-C10alkylene and R7 is -CN, OR10, N(R10)2 or -S(=O)pR10; R8 is H or C1-C4alkyl; R9 is methyl, fluoromethyl or difluoromethyl; R10 is, for example, H, C1-C6alkyl, C2-C8alkenyl, C2-C8alkynyl or C3-C6cycloalkyl; and, where applicable, their possible E/Z isomers, mixtures of E/Z isomers and/or tautomers, in each case in free form or in salt form, can be used as agrochemical active ingredients.
摘要翻译：式（I）化合物，其中X为CH或N，Y为OR 1，Z为O，X为N，Y为NHR 8，Z为O，S或S（= O）; U是（a）或（b）; R1是H或C1-C4烷基; R2是例如H，C1-C4烷基或卤代-C1-C4烷基; R3和R4是例如H，C1-C4烷基或C1-C4烷氧基; l为0,1或2; R 5和R 6是例如C 1 -C 6烷基，卤代-C 1 -C 6烷基，C 3 -C 6环烷基，C 3 -C 6环烯基，卤代-C 3 -C 6环烷基，C 1 -C 6烷氧基，卤代-C 1 -C 6烷氧基或C 1 -C 6烷硫基; R 55是例如C 1 -C 6烷基，卤代-C 1 -C 6烷基，C 3 -C 6环烷基或C 3 -C 6环烯基; R 66是例如氢，C 1 -C 6烷基，卤代-C 1 -C 6烷基，C 3 -C 6环烷基，C 3 -C 6环烯基，卤代-C 3 -C 6环烷基，C 1 -C 6烷基亚磺酰基或卤代-C 1 -C 6烷基亚磺酰基; m为0,1,2,3,4或5; n为0,1,2,3或4; q是0，1，2，3或4; A是直接键，C 1 -C 10亚烷基，-C（= O） - ， - C（= S） - 或卤代-C 1 -C 10亚烷基，R 7是基团R 10; 或A为例如C 1 -C 10亚烷基，且R 7为-CN，OR 10，N（R 10）2或-S（= O）p R 10; R8是H或C1-C4烷基; R9是甲基，氟甲基或二氟甲基; R 10是例如H，C 1 -C 6烷基，C 2 -C 8烯基，C 2 -C 8炔基或C 3 -C 6环烷基; 并且如果适用，其可能的E / Z异构体，E / Z异构体和/或互变异构体的混合物，在每种情况下为游离形式或盐形式，可用作农业化学活性成分。

106. 发明申请

WO1998025982A1 POROUS POLYORGANOSILOXANE POLYMERS 审中-公开
标题翻译：多孔聚硅氧烷聚合物
公开(公告)号：WO1998025982A1
公开(公告)日：1998-06-18
申请号：PCT/EP1997006936
申请日：1997-12-11
申请人： NOVARTIS AG , COMMONWEALTH SCIENTIFIC AND INDUSTRIAL RESEARCH ORGANISATION , CHAOUK, Hassan , MEIJS, Gordon, Francis
发明人： NOVARTIS AG , COMMONWEALTH SCIENTIFIC AND INDUSTRIAL RESEARCH ORGANISATION
IPC分类号： C08F290/06
CPC分类号： C08J9/28 , B01D71/70 , C08F290/068 , C08F290/148 , C08J2383/04 , G02B1/043 , Y10S623/926
摘要： A hydratable porous polymer comprising a polymerized polyorganosiloxane macromonomer of formula (I): Q-[M-L]c-M-Q wherein c is in the range of from 0 to 5, preferably in the range of from 0 to 3; M may be the same or different and is a difunctional block of molecular weight in the range of from 100 to 8000 and wherein at least one M comprises a residue from a difunctional polymer or copolymer comprising siloxane repeat units of formula (II) where R and R may be the same or different and are selected from the group consisting of hydrogen, optionally substituted alkyl, alkenyl, alkynyl, aryl, haloalkyl, haloalkenyl, haloalkynyl, haloaryl, heterocyclyl, and haloheterocyclyl; L may be the same or different and is a difunctional group; and Q may be the same or different and is a polymerizable group.
摘要翻译：包含式（I）的聚合的聚有机硅氧烷大分子单体的可水合的多孔聚合物：Q- [M-L] c-M-Q其中c在0至5的范围内，优选在0至3的范围内; M可以相同或不同，并且是分子量在100至8000范围内的双官能嵌段，并且其中至少一个M包含来自包含式（II）的硅氧烷重复单元的双官能聚合物或共聚物的残基， R 1和R 2可以相同或不同，并且选自氢，任选取代的烷基，烯基，炔基，芳基，卤代烷基，卤代烯基，卤代炔基，卤代芳基，杂环基和卤代杂环基。 L可以相同或不同，是双官能团; Q可以相同或不同，为可聚合基团。

107. 发明申请

WO1998025887A2 FORMULATIONS AND POLYMORPHIC FORMS OF DESFERRIOXAMINE AND THE PREPARATION THEREOF 审中-公开
标题翻译： DESFERRIOXAMINE的制剂和多形态及其制备方法
公开(公告)号：WO1998025887A2
公开(公告)日：1998-06-18
申请号：PCT/EP1997006849
申请日：1997-12-08
申请人： NOVARTIS AG , MARTI, Erwin , GEOFFROY, Andre, Joseph , HIRT, Hans , BURKHARD, Andreas , HASSAN, Ian, Francis , LOWTHER, Nicholas , NICKLIN, Joanne , STEWARD, Alan , VAN HOOGEVEST, Peter
发明人： NOVARTIS AG
IPC分类号： C07C259/00
CPC分类号： A61K31/16 , C07C259/06 , Y02A50/411
摘要： A parenterally injectable composition comprising particles of a desferrioxamine-B salt of an aliphatic sulphonic acid having at least 8 carbon atoms suspended in a parenterally administrable oil. New crystalline modifications of desferrioxamine B decanesulphonic salt are provided, and one crystal form with outstanding stability is disclosed.
摘要翻译：一种肠胃外可注射组合物，其包含悬浮在肠胃外给药的油中的具有至少8个碳原子的脂肪族磺酸的去铁胺B盐的颗粒。提供了去铁胺B癸烷磺酸盐的新的结晶改性，并且公开了一种具有突出稳定性的一种晶体形式。

108. 发明申请

WO1998022100A2 NEW USE FOR 1,3-PROPANEDIOL DERIVATIVES 审中-公开
标题翻译：新用于1,3-丙二醇衍生物
公开(公告)号：WO1998022100A2
公开(公告)日：1998-05-28
申请号：PCT/EP1997006408
申请日：1997-11-17
申请人： NOVARTIS AG , COTTENS, Sylvain , HOF, Robert, Paul , WENGER, Roland
发明人： NOVARTIS AG
IPC分类号： A61K31/00
CPC分类号： A61K31/13 , A61K31/131 , A61K31/133 , A61K31/137 , A61K31/436 , A61K39/395 , A61K2300/00
摘要： Use of a compound of formula (I) wherein R1 is an optionally substituted straight- or branched carbon chain having 12 to 22 carbon atoms which may be optionally interrupted by an optionally substituted phenylene, and each of R2, R3, R4 and R5, independently, is H or lower alkyl, in free form or in pharmaceutically acceptable salt form, in the prevention or treatment of chronic rejection in a recipient of organ or tissue allo- or xenotransplant, or of acute rejection in a xenograft transplant recipient.
摘要翻译：式（I）化合物的用途，其中R 1是任选取代的具有12-22个碳原子的直链或支链碳链，其可任选地被任选取代的亚苯基中间，R2，R3，R4和R5各自独立地是游离形式或药学上可接受的盐形式的H或低级烷基，用于预防或治疗异种移植受体的器官或组织异种移植物的受体中的慢性排斥反应或急性排斥反应。

109. 发明申请

WO1998020018A1 PROCESS FOR THE PREPARATION OF AN OLIGOMERIC COMPOUND 审中-公开
标题翻译：制备低分子化合物的方法
公开(公告)号：WO1998020018A1
公开(公告)日：1998-05-14
申请号：PCT/EP1997006123
申请日：1997-11-05
申请人： NOVARTIS AG , NATT, François , HÄNER, Robert
发明人： NOVARTIS AG
IPC分类号： C07H21/00
CPC分类号： C07H21/00 , C07K1/04
摘要： The present invention relates to a process for the preparation of an oligomeric compound, comprising introduction of a lipophilic capping group to an unreacted reactive group, suitable for chain elongation, of a not elongated oligomeric compound intended to be elongated in a preceeding chain-elongation step, by reacting a lipophilic capping compound with said unreacted reactive group, which lipophilic capping group is not removable under the applied conditions of the synthesis and work-up of the oligomeric compound; and which not elongated oligomeric compound capped with said lipophilic capping group can be separated from said oligomeric compound on a hydrophobic stationary phase.
摘要翻译：本发明涉及一种制备低聚化合物的方法，包括将亲油性封端基团引入未延伸的未伸缩的低分子化合物的未反应的反应基团，该未反应的反应基团预期在前述的链延伸步骤中被拉长通过使亲油性封端化合物与所述未反应的反应性基团反应，该亲油性封端基团在合成和低聚化合物的后处理条件下不能除去; 并且在所述亲油性封端基上封闭的不伸长的低聚化合物可以在疏水性固定相上与所述低聚化合物分离。

110. 发明申请

WO1998018796A1 NAPHTHYRIDINE DERIVATIVES 审中-公开
标题翻译：萘啶衍生物
公开(公告)号：WO1998018796A1
公开(公告)日：1998-05-07
申请号：PCT/EP1997005898
申请日：1997-10-24
申请人： NOVARTIS AG , HERSPERGER, Rene
发明人： NOVARTIS AG
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Novel 8-aryl-1,7-naphthyridines, in free or salt form, are PDE IV inhibitors and are thus useful as pharmaceuticals, e.g. for asthma therapy. Preferred compounds include compounds of formulae (I and II) wherein the R groups are as defined. Pharmaceutical compositions comprising the compounds, processes for preparation of the compounds and novel intermediates for use in the processes are disclosed.
摘要翻译：游离或盐形式的新型8-芳基-1,7-萘啶是PDE IV抑制剂，因此可用作药物，例如，用于哮喘治疗。优选的化合物包括其中R基团如所定义的式（I和II）的化合物。公开了包含化合物的药物组合物，用于制备化合物的方法和用于该方法的新型中间体。

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