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51. 发明申请

WO2007002877A1 PREPARATION OF (+)-CATECHIN, (-)-EPICATECHIN, (-)-CATECHIN, (+)-EPICATECHIN, AND THEIR 5,7,3',4'-TETRA-O-BENZYL ANALOGUES 审中-公开
标题翻译：（+） - 卡培他滨（ - ） - EPICATECHIN，（ - ） - CATECHIN，（+） - EPICATECHIN及其5,7,3'，4'-四氮杂 - 邻苯甲酸类似物的制备
公开(公告)号：WO2007002877A1
公开(公告)日：2007-01-04
申请号：PCT/US2006/025482
申请日：2006-06-28
申请人： MARS, INCORPORATED , ROMANCZYK, Leo, J., Jr. , SHARMA, Pradeep, K. , GOU, Daming , GOU, Yanni
发明人： ROMANCZYK, Leo, J., Jr. , SHARMA, Pradeep, K. , GOU, Daming , GOU, Yanni
IPC分类号： C07D311/22 , C07C45/00 , C07C49/00
CPC分类号： C07C41/18 , C07C45/71 , C07C45/74 , C07D311/62 , C07C49/84 , C07C47/575 , C07C43/23
摘要： Processes for preparing racemic mixtures of 5,7,3',4'-tetra-O-benzyl-(±)-catechin and (±)-epicatechin involves (i) condensing 2-hydroxy-4,6-bis(benzyloxy)-acetophenone and 3,4-bis(benzyloxy)benzaldehyde, cyclizing the resulting compound, oxidizing the resulting compound; (ii) dihydroxylating (E)-3-(3',4'-bis(benzyloxy)phenyl)prop-2-ene-1 -ol and reducing the 1 ,2-diol; or (iii) coupling 3,5-bis(benzyloxy)phenol with (£)-3,5-bis(benzyloxy)-2-(3',4'-bis(benzyloxy)phenyl)allyl)phenol and cyclizing the resulting chalcone. A process for preparing the benzylated epimers of catechin and epicatechin involves seven steps. 3,4-Bis(benzyloxy)benzaldehyde is coupled with 2-hydroxy-4,6-benzyloxy-acetophenone to form a chalcone. The chalcone is selectively reduced to an alkene. The phenolic group of the alkene is protected. The protected alkene is asymetrically dihydroxylated. The resulting compound is deprotected, cyclized, and finally hydrolyzed. Epimers resulting from these processes are chemically resolved or separated by chiral high pressure liquid chromatography. Also disclosed is a method for preparing enantiomerically pure 5,7,3',4'-tetra-O-benzyl-(+)-catechin from a racemic mixture using dibenzoyl-L-tartaric acid monomethyl ester. Further, disclosed is an improved process for preparing dibenzoyl-L-tartaric acid monomethyl ester.
摘要翻译：制备5,7,3'，4'-四-O-苄基 - （±） - 儿茶素和（±） - 表儿茶素的外消旋混合物的方法包括（i）2-羟基-4,6-双（苄氧基） - 苯乙酮和3,4-双（苄氧基）苯甲醛，使所得化合物环化，氧化所得化合物; （ii）将（E）-3-（3'，4'-双（苄氧基）苯基）丙-2-烯-1-醇二羟基化并还原1,2-二醇; 或（iii）将3,5-二（苄氧基）苯酚与（£）-3,5-双（苄氧基）-2-（3'，4'-双（苄氧基）苯基）烯丙基）苯酚偶合并使所得查尔酮。制备儿茶素和表儿茶素的苄基化差向异构体的方法涉及七个步骤。 3,4-二（苄氧基）苯甲醛与2-羟基-4,6-苄氧基 - 苯乙酮偶联，形成查耳酮。查耳酮选择性还原成烯烃。烯烃的酚基被保护。受保护的烯是非对称二羟基化的。将所得化合物脱保护，环化，最后水解。通过手性高压液相色谱法化学拆分或分离由这些方法得到的异构体。还公开了使用二苯甲酰基-L-酒石酸单甲酯从外消旋混合物制备对映体纯的5,7,3'，4'-四-O-苄基 - （+） - 儿茶素的方法。此外，公开了一种制备二苯甲酰基-L-酒石酸单甲酯的改进方法。

52. 发明申请

WO2006125276A1 PHENYLALKANOL COMPOUNDS 审中-公开
标题翻译：苯丙醇化合物
公开(公告)号：WO2006125276A1
公开(公告)日：2006-11-30
申请号：PCT/AU2006/000710
申请日：2006-05-26
申请人： ZINGOTX PTY LTD , EDE, Nicholas , ROUFOGALIS, Basil , OWEN, David , BOURKE, David, Gerard , TRAN, Van, Hoan , DUKE, Colin, Charles
发明人： EDE, Nicholas , ROUFOGALIS, Basil , OWEN, David , BOURKE, David, Gerard , TRAN, Van, Hoan , DUKE, Colin, Charles
IPC分类号： C07C49/255 , A61K31/121 , A61P29/00
CPC分类号： C07C45/673 , C07C45/00 , C07C45/513 , C07C45/567 , C07C45/62 , C07C45/71 , C07C49/255 , C07C47/21 , C07C47/277 , C07C47/575
摘要： The present invention relates to phenylalkanol compounds of formula (I) and derivatives, prodrugs, isomers and/or tautomers thereof. The present invention also relates to processes for the preparation of a compound of formula (I) and their use as pharmaceutical or veterinary agents, in particular as modulators of the vanilloid receptor for the treatment and/or prophylaxis of pain.
摘要翻译：本发明涉及式（I）的苯基链烷醇化合物及其衍生物，前体药物，异构体和/或互变异构体。本发明还涉及制备式（I）化合物及其作为药物或兽药的用途的方法，特别是作为用于治疗和/或预防疼痛的香草素受体的调节剂。

53. 发明申请

WO2006069533A1 毛叶假鹰爪素, 其制法和抗肿瘤和抗艾滋病的应用审中-公开
公开(公告)号：WO2006069533A1
公开(公告)日：2006-07-06
申请号：PCT/CN2005/002334
申请日：2005-12-28
申请人：吴久鸿 , 後藤中川享子 , 王夕红 , 史宁
发明人：吴久鸿 , 後藤中川享子 , 王夕红 , 史宁
IPC分类号： C07C49/753 , C07C49/84 , C07C41/09 , C07D311/74 , A61K31/122 , A61K31/352 , A61P35/00 , A61P31/12 , A61P31/18 , C07C49/683 , C07C49/794 , C07C33/30
CPC分类号： C07D307/46 , C07C45/46 , C07C45/512 , C07C45/673 , C07C45/71 , C07C45/74 , C07C49/713 , C07C49/753 , C07C2601/14 , C07D277/24 , C07D311/74 , C07D333/22 , C07C49/825
摘要： The invention discloses a method for preparing desmosdumotin C, the series of desmosdumotin C derivatives and their manufactures, and the total synthesis of desmosdumotin B. The invention also discloses applications of the derivatives and medicinal compositions containing them in manufacturing medicines for treating tumor or AIDS.

54. 发明申请

WO2006014918A3 HETEROCYCLIC ACETOPHENONE POTENTIATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：代谢型谷氨酸受体的异源性乙酰胆碱酯电位
公开(公告)号：WO2006014918A3
公开(公告)日：2006-06-01
申请号：PCT/US2005026425
申请日：2005-07-26
申请人： MERCK & CO INC , PINKERTON ANTHONY B , VERNIER JEAN-MICHEL , CUBE ROWENA V , HUTCHINSON JOHN H , HUANG DEHUA , BONNEFOUS CELINE , GOVAK STEVEN P , KAMENECKA THEODORE
发明人： PINKERTON ANTHONY B , VERNIER JEAN-MICHEL , CUBE ROWENA V , HUTCHINSON JOHN H , HUANG DEHUA , BONNEFOUS CELINE , GOVAK STEVEN P , KAMENECKA THEODORE
IPC分类号： C07D213/02 , A61K31/44 , A61K31/47 , C07D215/00 , C07D217/00
CPC分类号： C07D311/16 , C07C45/71 , C07C49/84 , C07C69/734 , C07C69/92 , C07C217/76 , C07C217/92 , C07C235/42 , C07C255/54 , C07C323/12 , C07D205/04 , C07D209/08 , C07D213/30 , C07D213/53 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/84 , C07D213/89 , C07D215/20 , C07D217/02 , C07D231/56 , C07D233/20 , C07D233/60 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/16 , C07D235/18 , C07D239/34 , C07D257/04 , C07D263/58 , C07D271/10 , C07D277/74 , C07D307/80 , C07D311/22 , C07D311/24 , C07D311/58 , C07D401/04 , C07D417/04 , C07D471/04 , C07D473/38
摘要： The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译：本发明涉及作为代谢型谷氨酸受体的增强剂（包括mGluR2受体）的化合物，它们可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及涉及代谢型谷氨酸受体的疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

55. 发明申请

WO2006018104A1 UV-FILTER 审中-公开
标题翻译：紫外线过滤器
公开(公告)号：WO2006018104A1
公开(公告)日：2006-02-23
申请号：PCT/EP2005/008141
申请日：2005-07-27
申请人： MERCK PATENT GmbH , CAROLA, Christophe , PFLUECKER, Frank , BUCHHOLZ, Herwig , DRILLER, Hansjürgen , NEUNHOEFFER, Hans , BLYUMIN, Evgeniy, V.
发明人： CAROLA, Christophe , PFLUECKER, Frank , BUCHHOLZ, Herwig , DRILLER, Hansjürgen , NEUNHOEFFER, Hans , BLYUMIN, Evgeniy, V.
IPC分类号： C07D251/54
CPC分类号： C07F7/1856 , A61K8/42 , A61K8/44 , A61K8/494 , A61K8/4946 , A61K8/4966 , A61K8/585 , A61Q5/00 , A61Q17/04 , A61Q19/00 , A61Q19/007 , A61Q19/08 , C07C45/515 , C07C45/71 , C07C49/753 , C07C49/84 , C07C69/734 , C07C225/18 , C07C229/60 , C07C235/34 , C07C237/32 , C07C255/41 , C07C309/73 , C07C2602/42 , C07D235/18 , C07D235/20 , C07D251/70 , C07D317/16 , C07F7/1852
摘要： Die Erfindung betrifft Verbindungen nach Formel (I) oder (II) Zubereitungen, die solche Verbindungen enthalten, entsprechende verfahen zur Herstellung der Verbindungen bzw. der diese enthaltenden Zubereitungen und deren Verwendung als Lichtschutzfilter.
摘要翻译：本发明涉及式（I）或式（II）化合物含有这类化合物的，相应的程序制备的化合物或包含它们和它们作为遮光剂使用的组合物中的制剂。

56. 发明申请

WO2006014918A2 HETEROCYCLIC ACETOPHENONE POTENTIATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：代谢型谷氨酸受体的杂环乙烯酮增效剂
公开(公告)号：WO2006014918A2
公开(公告)日：2006-02-09
申请号：PCT/US2005/026425
申请日：2005-07-26
申请人： MERCK & CO., INC. , PINKERTON, Anthony, B. , VERNIER, Jean-Michel , CUBE, Rowena, V. , HUTCHINSON, John, H. , HUANG, Dehua , BONNEFOUS, Celine , GOVAK, Steven, P. , KAMENECKA, Theodore
发明人： PINKERTON, Anthony, B. , VERNIER, Jean-Michel , CUBE, Rowena, V. , HUTCHINSON, John, H. , HUANG, Dehua , BONNEFOUS, Celine , GOVAK, Steven, P. , KAMENECKA, Theodore
IPC分类号： A61K31/47
CPC分类号： C07D311/16 , C07C45/71 , C07C49/84 , C07C69/734 , C07C69/92 , C07C217/76 , C07C217/92 , C07C235/42 , C07C255/54 , C07C323/12 , C07D205/04 , C07D209/08 , C07D213/30 , C07D213/53 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/84 , C07D213/89 , C07D215/20 , C07D217/02 , C07D231/56 , C07D233/20 , C07D233/60 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/16 , C07D235/18 , C07D239/34 , C07D257/04 , C07D263/58 , C07D271/10 , C07D277/74 , C07D307/80 , C07D311/22 , C07D311/24 , C07D311/58 , C07D401/04 , C07D417/04 , C07D471/04 , C07D473/38
摘要： The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译：本发明涉及作为代谢型谷氨酸受体增效剂的化合物，包括mGluR2受体，并且其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍和疾病，其中涉及代谢型谷氨酸受体。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗其中代谢型谷氨酸受体参与的疾病中的用途。

57. 发明申请

WO2005056499A2 OLIGO(P-PHENYLENE VINYLENE) AMPHIPHILES AND METHODS FOR SELF-ASSEMBLY 审中-公开
标题翻译： OLIGO（对苯乙烯乙烯基）AMPHIPHILES和自组装方法
公开(公告)号：WO2005056499A2
公开(公告)日：2005-06-23
申请号：PCT/US2004/040548
申请日：2004-12-06
申请人： NORTHWESTERN UNIVERSITY , STUPP, Samuel, I. , HULVAT, James, F. , SOFOS, Marina , TAJIMA, Keisuke
发明人： STUPP, Samuel, I. , HULVAT, James, F. , SOFOS, Marina , TAJIMA, Keisuke
IPC分类号： C07C
CPC分类号： C07C217/20 , C07C45/44 , C07C45/71 , C07C47/575 , C07F9/4056 , C09K19/16 , C09K19/582 , C09K2019/168 , H01L51/0038 , H01L51/0071 , H01L51/0073 , H01L51/0076 , H01L51/5012
摘要： Amphiphilic oligo(p-phenylene vinylene) compounds and methods of use en route to self-assembled composites and device fabrication.
摘要翻译：两亲寡聚（对亚苯基亚乙烯基）化合物和使用途径，途经自组装复合材料和器件制造。

58. 发明申请

WO2005037756A2 NOVEL METHODS FOR THE PREPARATION OF 4-[4-(4-METHOXYMETHOXY-4'-METHYL-BIPHENYL-2-YL)-BUT-3-ENE-(E)-1-YNYL]-BENZOIC ACID 审中-公开
标题翻译：制备4- [4-（4-甲氧基甲基-4'-甲基 - 联苯-2-基） - 丁-3-烯 - （E）-1-亚硝基] - 苯甲酸的新方法
公开(公告)号：WO2005037756A2
公开(公告)日：2005-04-28
申请号：PCT/EP2004013741
申请日：2004-09-09
申请人： GALDERMA RES & DEV , MOUREOU CHRISTINE , MULLER FRANCK , BIADATTI THIBAUD , PASCAL JEAN-CLAUDE
发明人： MOUREOU CHRISTINE , MULLER FRANCK , BIADATTI THIBAUD , PASCAL JEAN-CLAUDE
IPC分类号： C07C41/48 , C07C41/50 , C07C43/313 , C07C45/68 , C07C45/71 , C07C47/57 , C07C47/575 , C07C51/09 , C07C51/347 , C07C51/353
CPC分类号： C07C47/575 , C07C41/48 , C07C41/50 , C07C43/313 , C07C45/68 , C07C45/71 , C07C47/57 , C07C51/09 , C07C65/28
摘要： The invention relates to novel methods for the preparation of 4-[4-(4-methoxymethoxy-4'-methyl-biphenyl-2-yl)-but-3-ene (E)-1-ynyl]-benzoic acid.
摘要翻译：本发明涉及制备4- [4-（4-甲氧基甲氧基-4'-甲基 - 联苯-2-基） - 丁-3-烯（E）-1-基] - 苯甲酸的新方法。

59. 发明申请

WO2004007407A3 FLUOROUS TAGGING AND SCAVENGING REACTANTS AND METHODS OF SYNTHESIS AND USE THEREOF 审中-公开
标题翻译：荧光标记和扫描反应物及其合成和使用方法
公开(公告)号：WO2004007407A3
公开(公告)日：2004-11-25
申请号：PCT/US0321686
申请日：2003-07-11
申请人： FLUOROUS TECHNOLOGIES INC
发明人： ZHANG WEI , LUO ZHIYONG , NAGASHIMA TADAMICHI , CHEN CHRISTINE HIU-TUNG , YU MARVIN S
IPC分类号： C07B51/00 , C07B63/02 , C07C17/16 , C07C22/08 , C07C43/23 , C07C45/71 , C07C47/575 , C07C53/50 , C07C211/14 , C07C211/15 , C07C213/00 , C07C217/34 , C07C265/04 , C07C273/18 , C07C275/28 , C07C311/16 , C07C323/20 , C07C335/16 , C07D207/46 , C07D209/14 , C07D209/16 , C07D211/62 , C07D213/74 , C07D217/04 , C07D217/06 , C07D231/38 , C07D265/26 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/10
CPC分类号： C07D491/10 , C07B51/00 , C07B63/02 , C07C17/16 , C07C22/08 , C07C43/23 , C07C45/71 , C07C47/575 , C07C53/50 , C07C211/14 , C07C211/15 , C07C213/00 , C07C265/04 , C07C273/1827 , C07C311/16 , C07C323/20 , C07C335/16 , C07D207/46 , C07D209/14 , C07D209/16 , C07D211/62 , C07D213/74 , C07D217/04 , C07D217/06 , C07D231/38 , C07D265/26 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07C217/34 , C07C275/28
摘要： The present invention includes methods and compositions for increasing the fluorous nature of an organic compound by reacting it with at least one fluorous compound to produce a fluorous tagged organic compound. The increased fluorous nature of the fluorous tagged organic compound can then be utilized to separate the fluorous organic compound from untagged reagents, reactants, catalysts and/or products derived therefrom. The resultant fluorous tagged organic compound can be subjected to subsequent chemical transformations, wherein the fluorous nature of the tagged compound is utilized to increase the ease of separation of the fluorous tagged organic compound from untagged reagents, reactants, catalysts and/or products derived therefrom, after each chemical transformation. The chemical transformations result in a second fluorous tagged organic compound wherein the fluorous nature of the second fluorous tagged organic compound can then be reduced by removing the fluorous group therefrom, thereby producing a second organic compound that may be employed as a pharmaceutical compound or intermediate, or a combinatorial library component.
摘要翻译：本发明包括通过使其与至少一种氟化合物反应以产生氟标记的有机化合物来增加有机化合物的氟性质的方法和组合物。然后可以利用氟标记的有机化合物的增加的氟性质将含氟有机化合物与未标记的试剂，反应物，催化剂和/或由其衍生的产物分离。所得氟标记的有机化合物可以进行随后的化学转化，其中使用标记化合物的氟性质来增加氟标记的有机化合物与未标记的试剂，反应物，由其衍生的催化剂和/或产物的分离容易性，每次化学转化后。化学转化产生第二氟标记的有机化合物，其中可以通过从其中除去含氟基团来减少第二氟标记的有机化合物的氟性质，从而产生可用作药物化合物或中间体的第二有机化合物，或组合库组件。

60. 发明申请

WO2004087630A1 PROCESS FOR PRODUCING CYCLOHEXENONE LONG-CHAIN ALCOHOLS 审中-公开
标题翻译：生产环己酮长链醇的方法
公开(公告)号：WO2004087630A1
公开(公告)日：2004-10-14
申请号：PCT/JP2003/003994
申请日：2003-03-28
申请人： MEIJI DAIRIES CORPORATION , LUU, Bang , NEUBERG, Patrick , TRANCARD, Delphine , YAMADA, Masashi , OSHIBA, Yukio , SUZUKI, Hiroto
发明人： LUU, Bang , NEUBERG, Patrick , TRANCARD, Delphine , YAMADA, Masashi , OSHIBA, Yukio , SUZUKI, Hiroto
IPC分类号： C07C45/51
CPC分类号： C07C49/753 , C07C45/511 , C07C45/513 , C07C45/68 , C07C45/71 , C07C49/713
摘要： A process for producing cyclohexenone long-chain alcohol represented by the following formula (1): (wherein A represents a C10-C18 alkylene or alkenylene group, and each of R 1 , R 2 , and R 3 individually represents hydrogen or methyl), comprising reacting a 3-alkoxy-2-cyclohexen-1-one derivative represented by the following formula (2): (wherein R 1 , R 2 , and R 3 have the same meanings as above, and R 4 represents a C1-C5 alkyl group) with a Grignard's reagent prepared by protecting the hydroxyl groups of C10-C18 ω-halogenoalcohol through silylation, and hydrolyzing the resultant reaction product. The process of the present invention for producing cyclohexenone long-chain alcohol requires a reduced number of reaction steps, can be performed with ease and with reduced production cost, and thus finds utility in the industry.
摘要翻译：由下式（1）表示的生产环己烯酮长链醇的方法：（其中A表示C 10 -C 18亚烷基或亚烯基，R 1，R 2和R 3各自独立地代表氢或甲基），包括使由下式（2）表示的3-烷氧基-2-环己烯-1-酮衍生物：其中R 1，R 2和R 3具有相同的 R 4表示C 1 -C 5烷基）与通过甲硅烷基保护C10-C18ω-卤代醇的羟基制备的Grignard试剂反应，并水解所得的反应产物。本发明用于制备环己烯酮长链醇的方法需要减少数量的反应步骤，可以容易地进行并且降低生产成本，从而在工业上发挥效用。

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