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121. 发明授权

US5393877A Linkers for the synthesis of multiple oligonucleotides in seriatim from a single support attachment 失效
标题翻译：用于从单个支持附件合成多个寡核苷酸的连接体
公开(公告)号：US5393877A
公开(公告)日：1995-02-28
申请号：US41599
申请日：1993-04-05
申请人： Michael J. McLean , David Holland , Andrew J. Garman , Robert C. Sheppard
发明人： Michael J. McLean , David Holland , Andrew J. Garman , Robert C. Sheppard
IPC分类号： C12N15/09 , C07F9/655 , C07H21/00 , C07H21/04
CPC分类号： C07F9/65515 , C07H21/00
摘要： A method for the synthesis of a plurality of oligonucleotides comprising the steps of(i) forming a first oligonucleotide on a first cleavable link attached to a solid support;(ii) attaching to the first oligonucleotide a cleavable linker moiety;(iii) forming a second oligonucleotide on the cleavable linker moiety; and(iv) cleaving the first cleavable link and the cleavable linker moiety to give a plurality of oligonucleotides; wherein the cleavable linker moiety is of the Formula (1): ##STR1## in which A.sup.1, A.sup.2 and E are as defined herein, and novel compounds which may be used in the operation of the method.
摘要翻译：一种用于合成多种寡核苷酸的方法，包括以下步骤：（i）在连接到固体支持物上的第一可切割链节上形成第一寡核苷酸; （ii）将第一寡核苷酸连接到可切割的接头部分上; （iii）在可切割接头部分上形成第二寡核苷酸; 和（iv）切割第一可切割连接和可切割连接部分以产生多个寡核苷酸; 其中所述可切割接头部分具有式（1）：其中A1，A2和E如本文所定义的式（1）和可用于该方法操作的新化合物。

122. 发明授权

US5393779A Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US5393779A
公开(公告)日：1995-02-28
申请号：US889196
申请日：1992-05-28
申请人： Brian R. Holloway , Ralph Howe , Balbir S. Rao
发明人： Brian R. Holloway , Ralph Howe , Balbir S. Rao
IPC分类号： A61K31/19 , A61K31/195 , A61K31/196 , A61K31/216 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P9/12 , A61P25/02 , C07C213/00 , C07C215/00 , C07C217/18 , C07C217/22 , C07C225/16 , C07C229/00 , C07C231/12 , C07C235/34 , C07C251/08 , C07C251/16 , C07D263/22 , A61K31/24
CPC分类号： C07C251/08 , C07C217/22 , C07C225/16 , C07C235/34 , C07C251/16 , C07D263/22
摘要： Compounds of the formula (I): ##STR1## and bioprecursors and pharmaceutically acceptable salts thereof are described as .beta..sub.3 -adrenoceptor agonists having anti-obesity, hypoglycaemic and related therapeutic utilities. Processes for their preparation are described as are compositions containing them.
摘要翻译：式（I）化合物：其中和其生物前体及其药学上可接受的盐被描述为具有抗肥胖，低血糖和相关治疗效用的β3肾上腺素受体激动剂。其制备方法描述为含有它们的组合物。

123. 发明授权

US5387445A Liquid crystal display device 失效
标题翻译：液晶显示装置
公开(公告)号：US5387445A
公开(公告)日：1995-02-07
申请号：US847170
申请日：1992-03-09
申请人： Shin Horiuchi , Sumio Wakabayashi , Takahisa Doba
发明人： Shin Horiuchi , Sumio Wakabayashi , Takahisa Doba
IPC分类号： C08G59/00 , C08G59/16 , C08G59/17 , C08L63/00 , G02F1/1339 , G03F7/027
CPC分类号： G02F1/1339 , G03F7/0275 , G02F2202/023 , Y10T428/1077
摘要： A liquid crystal display device including two electrically insulating substrates, electrodes on the inner surfaces of the substrates, a film of liquid crystal material contained between the electrodes and a resinous material as sealant and/or encapsulant and/or inner structural component characterised in that the resinous material is the product of light-curing a light-curable resin composition comprising at least one compound having two or more non-aromatic carbon-carbon unsaturated bonds per molecule, at least one compound having two or more mercapto groups per molecule and a photoinitiator.
摘要翻译：一种液晶显示装置，包括两个电绝缘基板，基板的内表面上的电极，包含在电极之间的液晶材料的膜和作为密封剂的树脂材料和/或密封剂和/或内部结构部件，其特征在于，树脂材料是光固化树脂组合物的产物，其包含至少一种每分子具有两个或多个非芳族碳 - 碳不饱和键的化合物，至少一种每分子具有两个或更多个巯基的化合物和光引发剂。

124. 发明授权

US5373007A Pyridooxazinyl or pyridothiazinyl as inhibitors of leukotrienes 失效
标题翻译：吡啶并恶嗪基或吡啶并噻嗪类作为白细胞三烯的抑制剂
公开(公告)号：US5373007A
公开(公告)日：1994-12-13
申请号：US217844
申请日：1994-03-25
申请人： Pierre A. R. Bruneau , Graham C. Crawley
发明人： Pierre A. R. Bruneau , Graham C. Crawley
IPC分类号： A61K31/35 , A61K31/535 , A61K31/536 , A61K31/54 , A61K31/5415 , A61P29/00 , A61P37/08 , A61P43/00 , C07D265/36 , C07D279/16 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04 , C07D265/14 , C07D513/04
CPC分类号： C07D413/10 , C07D413/12 , C07D417/12
摘要： The invention concerns a bicyclic heterocyclic compound of the formula I ##STR1## wherein Q is an optionally substituted 10-membered bicyclic heterocyclic moiety containing 1 or 2 N's and a further O or S heteroatom;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is optionally substituted phenylene or pyridylene;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which,together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl; or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
摘要翻译：本发明涉及式I的双环杂环化合物其中Q是任选取代的含有1或2个N和另外的O或S杂原子的10元双环杂环部分; A1是与X1或（1-3C）亚烷基的直接键; X1是氧基，硫基，亚磺酰基，磺酰基或亚氨基; Ar是任选取代的亚苯基或亚吡啶基; R1是（1-4C）烷基，（3-4C）烯基或（3-4C）炔基; 并且R2和R3一起形成式-A2-X2-A3-的基团，其与A2和A3所连接的碳原子一起定义为具有5至7个环原子的环，其中A2和A3各自为（1-3C）亚烷基，X 2为氧基，硫基，亚磺酰基或磺酰基; 或其药学上可接受的盐。本发明的化合物是5-脂氧合酶的抑制剂。

125. 发明授权

US5364778A Copolymer production 失效
标题翻译：共聚物生产
公开(公告)号：US5364778A
公开(公告)日：1994-11-15
申请号：US103155
申请日：1993-08-09
申请人： David Byrom
发明人： David Byrom
IPC分类号： C08G63/06 , C12N1/20 , C12P7/62 , C12R1/05
CPC分类号： C12P7/625 , C08G63/06 , Y10S435/829
摘要： A microbiological process, and novel bacteria e.g. Alcaligenes eutrophus NCIMB 40124, for use in such a process. The process enables the more efficient production of copolymers comprising hydroxyvalerate and hydroxybutyrate monomer units.
摘要翻译：微生物过程，以及新的细菌产碱金属蛋白酶NCIMB 40124，用于这种过程。该方法能够更有效地制备包含羟基戊酸酯和羟基丁酸酯单体单元的共聚物。

126. 发明授权

US5334718A Chemical process and intermediates used therein 失效
标题翻译：其中使用的化学工艺和中间体
公开(公告)号：US5334718A
公开(公告)日：1994-08-02
申请号：US7930
申请日：1993-01-25
申请人： Andrew P. Thomas , David M. G. Martin , Stanley A. Lee , Lyn Powell
发明人： Andrew P. Thomas , David M. G. Martin , Stanley A. Lee , Lyn Powell
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The invention provides a novel chemical process for the manufacture of certain imidazo[4,5-b]pyridine derivatives of the formula I wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the various meanings defined herein, and their non-toxic salts, which are angiotensin II inhibitors. The process involves the removal of an electron-deficient phenyl group or a pyridyl or pyrimidyl group from a compound of the formula II as defined herein. Certain of the intermediates are novel and are provided as a further feature of the invention.
摘要翻译：本发明提供了制备式I的某些咪唑并[4,5-b]吡啶衍生物的新颖化学方法，其中R1，R2，R3和R4具有本文定义的各种含义及其无毒盐，血管紧张素II抑制剂。该方法包括从如本文定义的式II化合物中除去电子缺乏的苯基或吡啶基或嘧啶基。某些中间体是新颖的，并且作为本发明的进一步特征提供。

127. 发明授权

US5306626A Process for production of restrictocin 失效
标题翻译：生产限释片的方法
公开(公告)号：US5306626A
公开(公告)日：1994-04-26
申请号：US32842
申请日：1993-03-16
申请人： John E. Fitton
发明人： John E. Fitton
IPC分类号： C07K14/37 , C07K14/415 , C12N9/22 , C12N9/88 , C12N15/31 , C12N15/70 , C12P21/02
CPC分类号： C12N9/22 , C07K14/37 , C07K14/415 , C12N15/70 , C12N9/88 , C07K2319/034 , C07K2319/55 , Y10S435/849
摘要： Methods for recombinant production in procayotic microorganisms such as E. coli of ribotoxins such as restrictocin, alpha-sarcin and mitogillin are described. Known methods were relatively low yielding and not cost effective for commercial use such as in the pharmaceutical industry where relatively large quantities of toxin with consistent batch to batch quality may be required for immunotoxin production. Use of recombinant methods of production open up the possibility of making ribotoxin analogues. Toxicity of ribotoxins was recognised as a concern in development of a high yielding cost effective production method. Methods for high yielding intracellular accumulation or secretion of ribotoxins are described. Use of protease deficient strains and other methods of minimising breakdown of ribotoxin by protease are preferred. Vectors and host strains for use in the methods are described.
摘要翻译：描述了在诸如限制性细胞毒素，α-丝氨酸蛋白酶和丝裂霉素的核毒素如大肠杆菌等原生微生物中重组生产的方法。已知的方法相对低的产率并且在商业上不是成本有效的，例如在制药工业中，对于免疫毒素生产可能需要相对大量的具有一致批次质量的毒素。使用重组生产方法开辟制作核毒素类似物的可能性。在开发高产成本有效的生产方法中，核糖核酸的毒性被认为是关注的问题。描述了高产细胞内积累或分泌核毒素的方法。优选使用蛋白酶缺陷菌株和通过蛋白酶使核酸毒素最小化的其它方法。描述了用于该方法的载体和宿主菌株。

128. 发明授权

US5296023A Phthalocyanine colorants and their use in ink jet printing 失效
标题翻译：酞菁染料及其在喷墨印刷中的应用
公开(公告)号：US5296023A
公开(公告)日：1994-03-22
申请号：US000006
申请日：1993-01-04
申请人： Peter Gregory , Ronald W. Kenyon
发明人： Peter Gregory , Ronald W. Kenyon
IPC分类号： C09B47/24 , B41J2/01 , B41M5/00 , C09B47/26 , C09B67/46 , C09D11/00 , C09D11/02
CPC分类号： C09D11/328 , C09B47/26
摘要： A colorant of Formula (1): ##STR1## wherein: L is a metal cation or hydrogen;Pc is a phthalocyanine radical having a valency from 3 to 4;R.sup.1 is H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, aralkyl or substituted aralkyl;R.sup.2 is H, alkyl, alkoxy, halo or an optionally substituted amino group;M.sup.+ is NH.sub.4.sup.+ or a substituted annonium cation; and(t+q) is from 3 to 4 inclusive;with the proviso that the group CO.sub.2 -M.sup.+ is at the 2-, 3-, 5- or 6-position in Formula (1).
摘要翻译：式（1）的着色剂：（*化学结构*）式（1）其中：L是金属阳离子或氢; Pc是具有3至4价的酞菁基; R1是H，烷基，取代的烷基，烯基，取代的烯基，芳烷基或取代的芳烷基; R2是H，烷基，烷氧基，卤素或任选取代的氨基; M +是NH 4 +或取代的onium阳离子; 和（t + q）为3〜4; 条件是CO 2 -CO 2基团在式（1）中为2-，3-，5-或6-位。

129. 发明授权

US07173025B1 Aminoheterocyclic derivatives as antithrombotic or anticoagulant agents 失效
标题翻译：氨基杂环衍生物作为抗血栓形成或抗凝血剂
公开(公告)号：US07173025B1
公开(公告)日：2007-02-06
申请号：US09117436
申请日：1997-01-31
申请人： Andrew Stocker , John Preston , Michael James Smithers
发明人： Andrew Stocker , John Preston , Michael James Smithers
IPC分类号： A61K31/55 , A61K31/495 , C07D401/00 , C07D223/00
CPC分类号： C07D401/14 , C07D213/74 , C07D237/20 , C07D239/42 , C07D401/04 , C07D401/12
摘要： Compounds of formula (I), wherein G1 is CH or N; G2 is CH or N; R1 is a variety of optional substituents; L1 is (1-4C)alkylene; T1 is CH or N; R2 and R3 are independently hydrogen or (1-4C)alkyl or are joined to form a ring; X1 and X2 represent various linking groups; Ar is phenylene or certain heteroaryl rings and Q represents a variety of aromatic or heterocyclic rings systems, and pharmaceutically acceptable salts thereof are described as useful antithrombotic and anticoagulant agents, and are selective Factor Xa inhibitors. Processes for their preparation and pharmaceutical compositions containing them are also described.
摘要翻译：式（I）的化合物，其中G 1是CH或N; G 是CH或N; R 1是各种任选的取代基; L 1是（1-4C）亚烷基; T 1是CH或N; R 2和R 3独立地是氢或（1-4C）烷基或连接形成环; X 1和X 2代表各种连接基团; Ar是亚苯基或某些杂芳基环，Q表示各种芳族或杂环体系，其药学上可接受的盐被描述为有用的抗血栓形成和抗凝血剂，并且是选择性因子Xa抑制剂。还描述了其制备方法和含有它们的药物组合物。

130. 发明授权

US06946468B1 3-mercaptopyrrolidines as farnesyl protein transferase inhibitors 失效
标题翻译： 3-巯基吡咯烷作为法呢基蛋白转移酶抑制剂
公开(公告)号：US06946468B1
公开(公告)日：2005-09-20
申请号：US09242461
申请日：1997-08-13
申请人： Francis Thomas Boyle , James Michael Wardleworth
发明人： Francis Thomas Boyle , James Michael Wardleworth
IPC分类号： A61K31/40 , A61K31/427 , A61K31/4439 , A61K31/496 , A61P25/00 , A61P35/00 , A61P43/00 , C07D207/12 , C07D401/12 , C07D403/06 , C07D403/12 , C07D417/12 , A16K31/495 , C07D403/00 , A16K31/50
CPC分类号： C07D401/12 , C07D207/12 , C07D403/06 , C07D417/12
摘要： The present invention relates to inhibitors of ras farnesylation of the Formula I wherein: R1 is for example H and further values as defined in the specification; R2 is for example H and further values as defined in the specification; R3 is for example H or a substituent having values as defined in the specification; p is 0-3 in which R3 values can be the same or different; L is a linking moiety for example —CH2—NH— and further values as defined in the specification; A is selected from phenyl; naphthyl; a 5-10 membered monocyclic or bicyclic heteroaryl ring containing upto 5 heteroatoms where the heteroatoms are independently selected from O, N & S; or a —S—S— dimer thereof when R2═H; or a N-oxide or a pharmaceutically-acceptable salt, prodrug or solvate thereof. Processes for their preparation their use as therapeutic agents and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式I的Ras法呢基化抑制剂，其中：R 1是例如H和如说明书中定义的其它值; R 2是例如H和说明书中定义的其它值; R 3是例如H或具有本说明书中定义的值的取代基; p为0-3，其中R 3 3可以相同或不同; L是例如-CH 2 - NH-的连接部分和如说明书中定义的进一步的值; A选自苯基; 萘基; 含有至多5个杂原子的5-10元单环或双环杂芳基环，其中杂原子独立地选自O，N和S; 或其-S-S-二聚体;当R 2〜或N-氧化物或其药学上可接受的盐，前药或溶剂化物。其制备方法用作治疗剂和含有它们的药物组合物。

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