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81. 发明公开

EP0861838A3 Process and intermediates for preparing cryptophycin compounds 失效
标题翻译： Verfahren und Intermediate zur Herstellung von Cryptophycinverbindungen
公开(公告)号：EP0861838A3
公开(公告)日：1998-12-09
申请号：EP98301367.3
申请日：1998-02-25
申请人： ELI LILLY AND COMPANY , UNIVERSITY OF HAWAII , Wayne State University
发明人： Patel, Vinod Francis , Hoard, David Warren , Moher, Eric David
IPC分类号： C07D413/06 , C07D419/06 , C07D303/46 , C07D303/38 , C07D303/40 , C07D405/12 , C07F7/18 , C07C271/22
CPC分类号： C07D303/38 , C07D303/40 , C07D303/46 , C07D405/06 , C07D405/12 , C07D413/06 , Y02P20/55
摘要： Cryptophycin compounds may be prepared utilizing an epoxidation step early in the synthetic process under the conditions set forth herein. This invention also relates to novel intermediates generated by this early epoxidation process.
摘要翻译：在本文所述的条件下，可以在合成过程的早期使用环氧化步骤制备Cryptocycin化合物。本发明还涉及通过该早期环氧化方法产生的新型中间体。

82. 发明公开

EP0871708A1 RECOMBINANT SWEET PROTEIN MABINLIN 失效
标题翻译：重组SÜSSPROTEIN马槟榔甜蛋白
公开(公告)号：EP0871708A1
公开(公告)日：1998-10-21
申请号：EP96926694.0
申请日：1996-06-21
申请人： UNIVERSITY OF HAWAII
发明人： SUN, Samuel S.M., Chinese University of Hong Kong , XIONG, Liwen, University of Hawaii , HU, Zhong, Kunming Institute of Botany , CHEN, Hang, Beijing Vegetable Research Center
IPC分类号： A23L1 , C07K14 , C12N15
CPC分类号： C12N15/8242 , A23L27/31 , C07K14/43
摘要： Recombinant materials for the production of practical amounts of the sweet protein, mabinlin are provided. In addition, transgenic plants which have inherently sweetened edible parts result from modifying native plants containing edible parts to express the mabinlin gene. Single-chain forms of this protein which retain their sweetening property are also provided.

83. 发明公开

EP0866848A1 IMPROVED NEUROSPORA HOSTS FOR THE PRODUCTION OF RECOMBINANT PROTEINS, AND METHODS FOR PRODUCING THE SAME 失效
标题翻译：改进脉宿主细胞生产重组蛋白质和它们的生产方法
公开(公告)号：EP0866848A1
公开(公告)日：1998-09-30
申请号：EP96939719.0
申请日：1996-11-12
申请人： UNIVERSITY OF HAWAII
发明人： STUART, W., Dorsey
IPC分类号： C12N15 , C12N1
CPC分类号： C12R1/645 , C12N15/80
摘要： The present invention provides improved host cells for use in producing secreted recombinant proteins, methods of making the improved hosts and uses thereof. The invention specifically provides strains of Neurospora crassa which produce reduced levels of extracellular proteases when compared with wild-type Neurospora crassa.

84. 发明公开

EP0861839A1 Selective epoxidation process for preparing cryptophycin compounds and intermediates 失效
标题翻译： Selektives Epoxidierungsverfahren zur Herstellung von Cryptophycinverbindungen und Intermediaten
公开(公告)号：EP0861839A1
公开(公告)日：1998-09-02
申请号：EP98301368.1
申请日：1998-02-25
申请人： ELI LILLY AND COMPANY , UNIVERSITY OF HAWAII , Wayne State University
发明人： Patel, Vinod Francis , Hoard, David Warren , Moher, Eric David , Norman, Bryan Hurst
IPC分类号： C07D413/06 , C07D419/06 , C07D303/46 , C07F7/18
CPC分类号： C07D303/38 , C07D303/40 , C07D303/46 , C07D405/06 , C07D405/12 , C07D413/06 , Y02P20/55
摘要： Cryptophycin compounds possessing a β-epoxy moiety may be made with high stereoselectivity at various steps in the overall synthetic process. This invention also provides novel intermediates useful in preparing Cryptophycin compounds.
摘要翻译：在本文所述的条件下，可以在合成过程的早期使用环氧化步骤制备Cryptocycin化合物。本发明还涉及通过该早期环氧化方法产生的新型中间体。

85. 发明公开

EP0820497A1 CATALYTIC SUPERCRITICAL GASIFICATION OF WET BIOMASS 失效
标题翻译：湿生物质的催化超临界气化
公开(公告)号：EP0820497A1
公开(公告)日：1998-01-28
申请号：EP96910689.0
申请日：1996-03-28
申请人： UNIVERSITY OF HAWAII
发明人： ANTAL, Michael, J., Jr.
IPC分类号： C10J3 , B01J3
CPC分类号： B01J3/008 , C10J3/00 , C10J2200/06 , C10J2300/0916 , C10J2300/0946 , C10J2300/0979 , C10J2300/0986 , C10J2300/1276 , Y02P20/145 , Y02P20/544
摘要： A method for catalytically decomposing organic matter in a reaction medium is presented. Virtually complete gasification is achieved in relatively short periods of time. A hydrogen-rich gas may be formed from feedstocks (12) that include wet biomass, such as water hyacinth or algae, or organic waste or mixtures of biomass and organic waste. The reaction is catalyzed by a carbon-containing catalyst (22). The reaction medium may include supercritical water and is substantially oxygen-free. The carbon-containing catalyst (22) is stable in the environment of a supercritical water medium and maintains activity over long periods of time. Suitable carbon-containing catalysts are activated carbons or charcoals. Reaction products (26) are substantialy free of tars or chars.
摘要翻译：介绍了催化分解反应介质中有机物质的方法。在相对较短的时间内实现几乎完全的气化。富含氢气的气体可以由包括湿生物质的原料（12）形成，如水葫芦或藻类，或有机废物或生物质和有机废物的混合物。该反应由含碳催化剂催化（22）。反应介质可以包括超临界水并且基本上不含氧。含碳催化剂（22）在超临界水介质的环境中是稳定的并且长时间保持活性。合适的含碳催化剂是活性炭或木炭。反应产物（26）基本上不含焦油或焦油。

86. 发明公开

EP0792875A1 Cryptophycin derivatives and their use as anti-microtubule agents 失效
标题翻译： Cryptophycinderivate und ihre Verwendung als antimikrotubuli Mittel
公开(公告)号：EP0792875A1
公开(公告)日：1997-09-03
申请号：EP97301272.7
申请日：1997-02-26
申请人： ELI LILLY AND COMPANY , UNIVERSITY OF HAWAII , Wayne State University
发明人： Norman, Bryan Hurst , Shih, Chuan , Kroin, Julian Stanley
IPC分类号： C07D255/02 , C07D257/02 , C07D273/02 , C07D273/08 , C07D273/00 , C07D285/00 , C07D291/02 , C07D413/06 , C07D417/06 , C07D419/06 , A61K31/395
CPC分类号： C07D273/00 , C07D273/02 , C07D413/06
摘要： The invention provides novel cryptophycin compounds which can be useful for disrupting the microtubulin system, as antineoplastic agents, and for the treatment of cancer. The invention further provides a formulation for administering the novel cryptophycin compounds. The compounds are of the formula
wherein

Ar is phenyl or any simple unsubstituted or substituted aromatic or heteroaromatic group;
R 1 is halogen, SH, amino, monoalkylamino, dialkylamino, trialkylammonium, alkylthio, dialkylsulfonium, sulfate, or phosphate;
R 2 is OH or SH; or
R 1 and R 2 may be taken together to form an epoxide ring, and aziridine ring, an episulfide ring, a sulfate ring, or monoalkylphosphate ring; or
R 1 and R 2 may be taken together to form a second bond between C 18 and C 19 ;
R 3 is a lower alkyl group;
R 4 is H;
R 5 is H;
R 4 and R 5 may be taken together to form a second bond between C 13 and C 14 ;
R 6 is benzyl, hydroxybenzyl, alkoxybenzyl, halohydroxybenzyl, dihalohydroxybenzyl, haloalkoxybenzyl, or dihaloalkoxybenzyl group;
R 7 is H or a lower alkyl group;
R 8 is H or a lower alkyl group; or
R 7 and R 8 may optionally be taken together to form a cyclopropyl ring;
R 9 is selected from the group consisting of H, a lower alkyl group, (C 1 -C 3 ) alkylaryl, and aryl;
R 10 is selected from the group consisting of H, a lower alkyl group, (C 1 -C 3 ) alkylaryl, and aryl;
R 11 is H; simple alkyl; phenyl, substituted phenyl, benzyl, substituted benzyl;
X is O, NH or alkylamino;
Y is C, O, NH, S, SO, SO 2 or alkylamino; and
a pharmaceutically acceptable salt or solvate thereof.
摘要翻译：本发明提供了可用于破坏微管蛋白系统作为抗肿瘤药物和用于治疗癌症的新颖的cryptophycin化合物。本发明还提供了一种用于施用新型cryptophycin化合物的制剂。所述化合物具有式CHEM，其中Ar是苯基或任何简单的未取代或取代的芳族或杂芳基; R 1是卤素，SH，氨基，一烷基氨基，二烷基氨基，三烷基铵，烷硫基，二烷基锍，硫酸盐或磷酸盐; R 2是OH或SH; 或R 1和R 2可以一起形成环氧化物环，氮丙啶环，环硫醚环，硫酸酯环或磷酸单烷基酯环; 或R 1和R 2可以一起形成C 18和C 19之间的第二个键; R 3是低级烷基; R 4为H; R 5为H; R 4和R 5可以一起形成C13和C14之间的第二键; R 6是苄基，羟基苄基，烷氧基苄基，卤代羟基苄基，二卤代羟基苄基，卤代烷氧基苄基或二卤代烷氧基苄基; R 7是H或低级烷基; R 8是H或低级烷基; 或R 7和R 8可以任选地一起形成环丙基环; R 9选自H，低级烷基，（C 1 -C 3）烷基芳基和芳基; R 10选自H，低级烷基，（C 1 -C 3）烷基芳基和芳基; R 11是H; 简单烷基; 苯基，取代的苯基，苄基，取代的苄基; X是O，NH或烷基氨基; Y是C，O，NH，S，SO，SO 2或烷基氨基; 及其药学上可接受的盐或溶剂合物。

87. 发明公开

EP0735819A1 NEW CRYPTOPHYCINS 失效
标题翻译：新的CRYPTOPHYCINS
公开(公告)号：EP0735819A1
公开(公告)日：1996-10-09
申请号：EP95906059.0
申请日：1994-12-21
申请人： UNIVERSITY OF HAWAII , WAYNE STATE UNIVERSITY
发明人： MOORE, Richard, E. , SMITH, Charles, D. , PATTERSON, Gregory M. L. , MOOBERRY, Susan, L. , CORBETT, Thomas, H. , VALERIOTE, Frederick, A. , GOLAKOTI, Trimurtulu
IPC分类号： C12P13 , A61K31 , A61K38 , A61K45 , A61P35 , A61P43 , C07C237 , C07D273 , C07D303 , C07D307 , C07D413 , C07J21 , C12P21
CPC分类号： C07D273/00 , C07D307/20 , C07D413/06 , Y10S930/27
摘要： The present invention provides novel cryptophycin compounds having structure (I). The present invention also provides methods for producing cryptophycins from the Nostoc sp. of blue-green algae (cyanobacteria). Pharmaceutical compositions comprising novel cryptophycins are also provided by the present invention, as are methods for using cryptophycins to inhibit the proliferation of hyperproliferative cells. The present invention further provides methods for using cryptophycins to inhibit the proliferation of hyperproliferative cells with drug resistant phenotypes, and to treat pathological conditions, such as neoplasia.
摘要翻译：本发明提供了具有结构（I）的新隐藻菌素化合物。本发明还提供了从念珠藻生产隐藻菌素的方法。蓝绿藻（蓝细菌）。本发明还提供了包含新型隐藻菌素的药物组合物，以及使用隐藻菌素抑制过度增殖性细胞增殖的方法。本发明进一步提供了使用隐藻菌素抑制具有药物抗性表型的过度增殖细胞的增殖并治疗病理状况如瘤形成的方法。

88. 发明公开

EP0631474A4 CYCLIC ANTI-TUMOR PROMOTER COMPOUNDS, COMPOSITIONS AND METHODS FOR PRODUCTION AND USE. 失效
标题翻译：循环抗肿瘤促进剂化合物，组合物和生产和使用方法。
公开(公告)号：EP0631474A4
公开(公告)日：1995-01-25
申请号：EP93907442
申请日：1993-03-19
申请人： UNIVERSITY OF HAWAII
发明人： TIUS, MARCUS, A.
IPC分类号： A61K31/045 , A61K31/075 , A61K31/19 , A61K31/215 , A61P35/00 , C07C35/08 , C07C35/18 , C07C35/20 , C07C35/205 , C07C35/21 , C07C43/188 , C07C45/51 , C07C45/67 , C07C49/587 , C07C61/08 , C07C61/10 , C07C61/12 , C07C61/22 , C07C61/26 , C07C61/28 , C07C61/35 , C07C61/39 , C07C62/02 , C07C62/32 , C07C255/16 , C07C255/46 , C07F7/18 , A01N37/02
CPC分类号： C07C255/46 , A61K31/045 , C07C35/18 , C07C35/205 , C07C35/21 , C07C45/511 , C07C45/515 , C07C45/67 , C07C45/673 , C07C49/587 , C07C255/16 , C07C2601/18 , C07C49/753 , C07C49/647

89. 发明公开

EP0631474A1 CYCLIC ANTI-TUMOR PROMOTER COMPOUNDS, COMPOSITIONS AND METHODS FOR PRODUCTION AND USE 失效
标题翻译：循环抗肿瘤促进剂化合物组合物及其制备方法和用途。
公开(公告)号：EP0631474A1
公开(公告)日：1995-01-04
申请号：EP93907442.0
申请日：1993-03-19
申请人： UNIVERSITY OF HAWAII
发明人： TIUS, Marcus, A.
IPC分类号： A61K31 , A61P35 , C07C35 , C07C43 , C07C45 , C07C49 , C07C61 , C07C62 , C07C255 , C07F7
CPC分类号： C07C255/46 , A61K31/045 , C07C35/18 , C07C35/205 , C07C35/21 , C07C45/511 , C07C45/515 , C07C45/67 , C07C45/673 , C07C49/587 , C07C255/16 , C07C2601/18 , C07C49/753 , C07C49/647
摘要： Novel cyclic anti-tumor promoter compounds and therapeutic compositions are disclosed, along with method for their production and use as anti-cancer and cancer-prevention agents.
摘要翻译：新型环状抗肿瘤促进剂化合物和治疗组合物是游离缺失盘，非常久远方法对于它们的生产和作为抗癌症和癌症预防剂使用。

90. 发明公开

EP0426291A3 Colour liquid crystal display 失效
标题翻译：彩色液晶显示
公开(公告)号：EP0426291A3
公开(公告)日：1992-06-17
申请号：EP90310216.8
申请日：1990-09-18
申请人： UNIVERSITY OF HAWAII
发明人： Crooker, Peter P. , Yang, Dengke
IPC分类号： G02F1/1347
CPC分类号： C09K19/544 , G02F1/1334 , G02F1/13476 , G02F1/13718 , G02F2201/343 , G02F2203/02
摘要： A color liquid crystal display and display material formed by microdroplets of chiral or cholesteric liquid crystal phase dispersed in a polymeric matrix. The liquid crystal in the microdroplets exhibits strong negative dielectric anisotropy so that in the presence of an electric field the helical planes of the chiral material align perpendicular to the field. Incident light is reflected at a selected wavelength depending upon the helical pitch. In the field-OFF state, the liquid crystal directors are configured or randomly oriented so as to scatter incident light.

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