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1. 发明申请

US20170273933A1 ANTI-TUMOR COMPOUND AND THE MEDICAL USE THEREOF 审中-公开
公开(公告)号：US20170273933A1
公开(公告)日：2017-09-28
申请号：US15508516
申请日：2015-09-02
申请人： Tianjin Medical University Cancer Institute and Hospital
发明人： Ning ZHANG , Yinsong WANG , Ping ZHOU , Hua GUO , Yi LUO , Xishan HAO , Hua GENG
IPC分类号： A61K31/337 , C07C233/87 , C07C205/59 , C07C229/60 , A61K45/06 , A61K31/192
CPC分类号： A61K31/337 , A61K31/192 , A61K45/06 , A61K2300/00 , C07C205/59 , C07C229/60 , C07C231/00 , C07C233/87
摘要： The invention disclose a compound of formula (I), wherein, R1 is selected from —H or C1-C6 hydrocarbon group, —NH2, —OH, —O(CH2)nCH3 (n=0, 1 or 2), —N(CH3)2, or —CH2N(CH3)2, R2 is selected from an amino acid or an hydroxy acid or —OH (R1, R2 are not —CH3 and —OH at the same time), wherein X, Y are —H, —CH3, —CH2OH, —CH(OH)CH3, —CH2SH, —CH(CH3)2, —CH2CH(CH3)2, —CH(CH3)CH2CH3, —CH2CH2SCH3, —CH2COOH, —CH2CONH2, —CH2CH2COOH, —CH2CH2CH2CH2NH2, or —CH2CH2CONH2, R3-R5 are H or C1-C6 hydrocarbon group. The compound has a low toxicity, can significantly inhibit the migration and invasion of tumor cells in vitro, and can inhibit tumor metastasis in vivo in mice at low concentration, while showing notable sensitizing effect on cytotoxic anti-tumor drugs such as Paclitaxel etc.

2. 发明授权

US08022157B2 Light sensitive initiator integrated polydimethylsiloxane 有权
标题翻译：光敏引发剂一体化聚二甲基硅氧烷
公开(公告)号：US08022157B2
公开(公告)日：2011-09-20
申请号：US12529229
申请日：2008-08-29
申请人： Hongwei Ma
发明人： Hongwei Ma
IPC分类号： C08F230/08 , C07C205/59
CPC分类号： C07C205/57 , C07B2200/11 , C08G77/388
摘要： Disclosed herein is a surface functionalized poly(dimethylsiloxane) (PDMS) and methods for making the same. The surface functionalized poly(dimethylsiloxane) (PDMS) disclosed herein is applicable in the general field of microfluidics, bioMEMS (bio-microelectromechanical systems), soft lithography and other related biotechnology fields.
摘要翻译：本文公开了表面官能化聚（二甲基硅氧烷）（PDMS）及其制备方法。本文公开的表面官能化聚（二甲基硅氧烷）（PDMS）可应用于微流体，bioMEMS（生物微电子机械系统），软光刻和其他相关生物技术领域的一般领域。

3. 发明授权

US5952531A Nitration process 失效
标题翻译：硝化过程
公开(公告)号：US5952531A
公开(公告)日：1999-09-14
申请号：US960924
申请日：1997-10-30
申请人： Ian Jeffrey Grassham Priestley , James Peter Muxworthy , John Heathcote Atherton , Martin Lennon , Stephen Martin Brown
发明人： Ian Jeffrey Grassham Priestley , James Peter Muxworthy , John Heathcote Atherton , Martin Lennon , Stephen Martin Brown
IPC分类号： C07B43/02 , C07C201/08 , C07C205/38 , C07C205/59 , C07C231/12 , C07C235/44 , C07C303/40 , C07C311/51 , C07C43/00 , C07C29/00 , C07C205/00
CPC分类号： C07C303/40 , C07B43/02 , C07C201/08
摘要： A process for the nitration of an aromatic or heteroaromatic compound with a nitrating agent comprising nitric acid or a mixture of nitric and sulphuric acids, characterised in that nitration is performed in a solvent comprising at least 50% v/v of a C.sub.1 -C.sub.6 alkyl ester of a C.sub.1 -C.sub.4 carboxylic acid. The process is of particular use for the nitration of diphenyl ethers to give compounds which are useful as herbicides or as intermediates in the synthesis of herbicides.
摘要翻译：一种用包含硝酸或硝酸和硫酸的混合物的硝化剂硝化芳族或杂芳族化合物的方法，其特征在于，在包含至少50％v / v的C 1 -C 6烷基的溶剂中进行硝化酯的C 1 -C 4羧酸。该方法特别用于二苯醚的硝化，得到可用作除草剂的化合物或作为除草剂合成中的中间体。

4. 发明授权

US5910604A Purification process 失效
标题翻译：净化过程
公开(公告)号：US5910604A
公开(公告)日：1999-06-08
申请号：US816930
申请日：1997-03-13
申请人： Stephen Martin Brown , Brian David Gott , Thomas Gray , Seyed Mehdi Tavana
发明人： Stephen Martin Brown , Brian David Gott , Thomas Gray , Seyed Mehdi Tavana
IPC分类号： C07C201/16 , C07C205/59 , C07C303/36 , C07C303/44 , C07C311/51
CPC分类号： C07C303/44 , C07C201/16
摘要： A process for the purification of a compound of general formula I: ##STR1## wherein R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl, any of which may optionally be substituted with one or more substituents selected from halogen and hydroxy; or COOR.sup.4, COR.sup.6, CONR.sup.4 R.sup.5 or CONHSO.sub.2 R.sup.4 ;R.sup.4 and R.sup.5 independently represent hydrogen or C.sub.1 -C.sub.4 alkyl optionally substituted with one or more halogen atoms;R.sup.6 is a halogen atom or a group R.sup.4 ;R.sup.2 is hydrogen or halo; andR.sup.3 is C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.4 alkynyl, any of which may optionally be substituted with one or more halogen atoms; or halo; or, where appropriate, a salt thereof;from a mixture containing the compound of general formula I together with one or more isomers or di-nitrated analogs thereof; the process comprising dissolving the mixture in a suitable crystallization solvent and recrystallizing the product from the resulting crystallization solution wherein the crystallization solution contains not more than 25% loading of the compound of general formula I, loading being defined as: ##EQU1## and wherein the temperature to which the solution is cooled for crystallization is not greater than about 30.degree. C.; wherein, after the addition of the crystallizing solvent but before recrystallization, the crystallization solution is subjected to at least one wash with an aqueous solution having an acid pH. The process is particularly useful for purifying acifluorfen produced via a route starting with m-cresol.
摘要翻译：一种用于纯化通式I化合物的方法：其中R 1是氢或C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基，其中任何一个可任选被一个或多个选自卤素和羟基的取代基取代 ; 或COOR4，COR6，CONR4R5或CONHSO2R4; R4和R5独立地表示氢或任选被一个或多个卤素原子取代的C 1 -C 4烷基; R6是卤素原子或基团R4; R2是氢或卤素; 并且R 3是C 1 -C 4烷基，C 2 -C 4烯基或C 2 -C 4炔基，其中任何一个可任选地被一个或多个卤素原子取代; 或卤素; 或者在适当情况下为其盐; 由含有通式I化合物的混合物与一种或多种异构体或其二硝化类似物一起混合; 该方法包括将混合物溶解在合适的结晶溶剂中并从所得结晶溶液中重结晶产物，其中结晶溶液含有不超过25％的通式I化合物的负载，负载定义为：并且其中温度为该溶液冷却结晶不超过约30℃。其中，在加入结晶溶剂之后但重结晶之前，用酸性pH值的水溶液对结晶溶液进行至少一次洗涤。该方法特别可用于纯化通过以间甲酚开始的途径产生的三氟果霜。

5. 发明授权

US5856083A Lawn assay for compounds that affect enzyme activity or bind to target molecules 失效
标题翻译：影响酶活性或结合靶分子的化合物的草坪测定
公开(公告)号：US5856083A
公开(公告)日：1999-01-05
申请号：US553056
申请日：1995-11-03
申请人： Daniel Chelsky , Jonathan J. Burbaum
发明人： Daniel Chelsky , Jonathan J. Burbaum
IPC分类号： C07B61/00 , C07C205/59 , C07D311/08 , C07D311/22 , C07D311/96 , C07D491/10 , C07D493/10 , C07D495/10 , C12Q1/00 , G01N33/573
CPC分类号： C07C205/59 , C07D311/08 , C07D311/22 , C07D311/96 , C07D491/10 , C07D493/10 , C07D495/10 , C12Q1/00 , G01N33/573 , C07B2200/11 , C40B40/00
摘要： A lawn assay is described for determining compounds that affect enzyme activity or that bind to target molecules. Compounds to be screened are cleaved, and diffused from solid supports into a colloidal matrix. Enzymatic catalysis or binding to target molecules by the compounds is carried out in the matrix. Active compounds are found by monitoring a photometrically detectable change in a substrate, coenzyme, or cofactor involved in the enzymatic reaction, or in a labeled ligand bound to the target molecule, that produces a zone of activity associated with the compounds.
摘要翻译：描述了用于确定影响酶活性或结合靶分子的化合物的草坪测定。待筛选的化合物被切割，并从固体载体扩散到胶体基质中。通过化合物的酶催化或与靶分子的结合在基质中进行。通过监测参与酶反应的底物，辅酶或辅因子或与靶分子结合的标记配体中的光学上可检测的变化，发现活性化合物，其产生与化合物相关的活性区。

6. 发明授权

US5789172A Methods of determining the structure of a compound encoded by identifiers having tags 失效
标题翻译：确定具有标签的标识符编码的化合物的结构的方法
公开(公告)号：US5789172A
公开(公告)日：1998-08-04
申请号：US680716
申请日：1996-07-11
申请人： W. Clark Still , Michael H. Wigler , Michael H. J. Ohlmeyer , Lawrence W. Dillard , John C. Reader
发明人： W. Clark Still , Michael H. Wigler , Michael H. J. Ohlmeyer , Lawrence W. Dillard , John C. Reader
IPC分类号： G01N33/566 , C07B61/00 , C07C43/225 , C07C205/59 , C07C245/14 , C07C317/28 , C07D243/24 , C07D521/00 , C07H21/00 , C07K1/00 , C07K1/04 , C40B70/00 , G01N33/532 , G01N33/543 , G01N33/68 , C12Q1/68 , G01N33/53
CPC分类号： G01N33/68 , C07D243/24 , C07H21/00 , C07K1/047 , C40B50/16 , G01N33/532 , G01N33/54353 , B01J2219/00572 , C07B2200/11 , C40B40/00 , C40B70/00
摘要： Encoded combinatorial chemistry is provided, where sequential synthetic schemes are recorded using organic molecules, which define choice of reactant, and stage, as the same or different bit of information. Various products can be produced in the multi-stage synthesis, such as oligomers and synthetic non-repetitive organic molecules. Conveniently, nested families of compounds can be employed as identifiers, where number and/or position of a substituent define the choice. Alternatively, detectable functionalities may be employed, such as radioisotopes, fluorescers, halogens, and the like, where presence and ratios of two different groups can be used to define stage or choice. Particularly, pluralities of identifiers may be used to provide a binary or higher code, so as to define a plurality of choices with only a few detachable tags. The particles may be screened for a characteristic of interest, particularly binding affinity, where the products may be detached from the particle or retained on the particle. The reaction history of the particles which are positive for the characteristic can be determined by the release of the tags and analysis to define the reaction history of the particle.
摘要翻译：提供了编码的组合化学，其中使用有机分子记录顺序合成方案，其定义了反应物的选择和阶段，作为相同或不同的信息位。可以在多级合成中产生各种产物，例如低聚物和合成的非重复有机分子。方便地，化合物的嵌套族可以用作标识符，其中取代基的数目和/或位置定义了选择。或者，可以使用可检测的官能团，例如放射性同位素，荧光剂，卤素等，其中两个不同基团的存在和比例可用于限定阶段或选择。特别地，可以使用多个标识符来提供二进制或更高代码，以便仅限定几个可拆卸标签来定义多个选择。可以筛选颗粒以获得感兴趣的特征，特别是结合亲和力，其中产物可以与颗粒分离或保留在颗粒上。对特征呈阳性的颗粒的反应历程可以通过标签的释放和分析来确定以确定颗粒的反应历程。

7. 发明授权

US5728831A Process for preparing oxazines 失效
标题翻译：制备辛嗪的方法
公开(公告)号：US5728831A
公开(公告)日：1998-03-17
申请号：US660969
申请日：1996-06-12
申请人： Shy-Fuy Lee
发明人： Shy-Fuy Lee
IPC分类号： A01N43/72 , C07C205/59 , C07D265/02
CPC分类号： C07C205/59 , A01N43/72 , C07D265/02
摘要： A process for preparing a compound of formula III ##STR1## which comprises decarboxylating a compound of formula V ##STR2## wherein R.sup.20 is alkoxy and R.sub.1, R.sub.2, and R.sub.3 are independently hydrogen or C.sub.1-8 alkyl.
摘要翻译：制备式III化合物的方法，其包括使式V化合物脱羧，其中R 20是烷氧基，且R 1，R 2和R 3独立地是氢或C 1-8烷基。

8. 发明授权

US5698711A Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic- or heteroatom-containing linking group 失效
标题翻译：含有通过含脂肪族或含杂原子的连接基与芳基或杂芳基连接的苯基的化合物
公开(公告)号：US5698711A
公开(公告)日：1997-12-16
申请号：US487377
申请日：1995-06-07
申请人： Malcolm Norman Palfreyman
发明人： Malcolm Norman Palfreyman
IPC分类号： C07C43/225 , C07C45/00 , C07C45/29 , C07C45/71 , C07C47/575 , C07C49/84 , C07C59/58 , C07C59/60 , C07C59/62 , C07C65/21 , C07C65/24 , C07C65/26 , C07C65/42 , C07C69/76 , C07C69/92 , C07C205/59 , C07C217/88 , C07C235/56 , C07C255/57 , C07C255/60 , C07C275/34 , C07C311/29 , C07C311/46 , C07C317/40 , C07C323/42 , C07C327/48 , C07D213/50 , C07D213/75 , C07D213/89 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/02 , C07D275/03 , C07D409/12 , C07D333/02 , C07C13/10 , C07C3/20
CPC分类号： C07C43/225 , C07C205/59 , C07C217/88 , C07C235/56 , C07C255/57 , C07C255/60 , C07C275/34 , C07C311/29 , C07C311/46 , C07C317/40 , C07C323/42 , C07C327/48 , C07C45/004 , C07C45/292 , C07C45/71 , C07C47/575 , C07C49/84 , C07C59/58 , C07C59/60 , C07C59/62 , C07C65/21 , C07C65/24 , C07C65/26 , C07C65/42 , C07C69/76 , C07C69/92 , C07D213/50 , C07D213/75 , C07D213/89 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/03 , C07D409/12 , C07C2101/08 , C07C2101/14 , C07C2102/42
摘要： This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
摘要翻译：本发明涉及通过各种连接与芳基部分连接的用于抑制肿瘤坏死因子的苯基化合物的药物用途。本发明还涉及含有这些化合物的化合物及其制备方法和药物组合物。此外，本发明涉及化合物抑制环AMP磷酸二酯酶的药物用途。

9. 发明授权

US5449834A Method of synthesizing 2,6-dinitro benzyl compounds 失效
标题翻译： 2,6-二硝基苄基化合物的合成方法
公开(公告)号：US5449834A
公开(公告)日：1995-09-12
申请号：US274613
申请日：1994-07-13
申请人： Charles F. Kahle, II , Raphael O. Kollah , Gregory J. McCollum
发明人： Charles F. Kahle, II , Raphael O. Kollah , Gregory J. McCollum
IPC分类号： C07C205/19 , C07C205/35 , C07C205/57 , C07C205/59 , C07C205/61 , C08G18/38 , C07C205/06
CPC分类号： C08G18/384 , C07C201/12
摘要： Described is a method of preparing dinitrobis(hydroxymethyl)benzene, useful as a photoreactive monomer, from a derivative of stilbene. Also disclosed is a novel dinitrocarbomethoxybenzaldehyde compound useful as an intermediate.
摘要翻译：描述了从二苯乙烯的衍生物制备可用作光反应性单体的二硝基苯酚（羟甲基）苯的方法。还公开了可用作中间体的新型二硝基甲氧基苯甲醛化合物。

10. 发明授权

US5446197A Method of purifying acifluorfen 失效
标题翻译：三氟化合物的净化方法
公开(公告)号：US5446197A
公开(公告)日：1995-08-29
申请号：US78993
申请日：1993-06-17
申请人： Mark Sandison , Ron Eva , Lawrence E. James
发明人： Mark Sandison , Ron Eva , Lawrence E. James
IPC分类号： C07C41/40 , C07C43/257 , C07C43/275 , C07C43/285 , C07C43/29 , C07C201/16 , C07C205/59 , C07C205/00
CPC分类号： C07C201/16
摘要： A method of purifying acifluorfen to achieve a purity of greater than about 85% by weight involves heating to dissolution a solution of an acifluorfen crude wet cake and at least one solvent from the group of 1,2-dichlorobenzene, monochlorobenzene, o-xylene and p-xylene, with the solution having from about 10 to about 30 weight percent of acifluorfen crude wet cake. The-solution is then cooled until crystals of purified acifluorfen form. The crystals are then filtered at a temperature within the range of from about 0.degree. to about 30.degree. C. The filtered crystals are then recovered.
摘要翻译：净化三氟果霜以达到大于约85重量％的纯度的方法涉及加热溶解氟锁草醚粗湿滤饼和至少一种来自1,2-二氯苯，一氯苯，邻二甲苯和对二甲苯，溶液具有约10至约30重量％的三氟果霜粗湿饼。然后将溶液冷却至纯化的三氟果霜形成晶体。然后将晶体在约0℃至约30℃的温度范围内过滤。然后回收过滤的晶体。

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