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111. 发明授权

US08309714B2 Process for producing laurolactam 有权
标题翻译：生产月桂内酰胺的方法
公开(公告)号：US08309714B2
公开(公告)日：2012-11-13
申请号：US12744675
申请日：2008-11-19
申请人： Junichi Kugimoto , Joji Kawai , Hideo Shimomura , Ryouta Yasumatsu , Nobuhiro Ii
发明人： Junichi Kugimoto , Joji Kawai , Hideo Shimomura , Ryouta Yasumatsu , Nobuhiro Ii
IPC分类号： C07D201/04 , C07D225/02
CPC分类号： C07D201/04 , C07D225/02 , Y02P20/582
摘要： Provided is a process for efficiently producing laurolactam by simple steps from cyclododecanone and hydroxylamine. This production process comprises the steps of: (a) reacting cyclododecanone with hydroxylamine in an aqueous solution in the presence of an oxime-formation solvent to produce cyclododecanone oxime; (b) separating the reaction mixture obtained after the oxime-forming step into an oil and an aqueous phases and collecting a solution of cyclododecanone oxime of the oil phase; (c) removing a part or all of the oxime-formation solvent and dissolved water from the solution of cyclododecanone oxime which is collected as an oil phase in the oil/aqueous phase separation step, whereby preparing a solution containing a rearrangement solvent to be used in a rearrangement reaction in a later step and the cyclododecanone oxime; (d) producing laurolactam from cyclododecanone oxime by rearrangement reaction using an aromatic-ring containing compound as a rearrangement catalyst; and (e) separating and removing the rearrangement solvent and the rearrangement catalyst from the reaction mixture after the rearrangement step, and purifying the laurolactam.
摘要翻译：提供一种通过简单的步骤从环十二酮和羟胺有效地生产十二内酰胺的方法。该制备方法包括以下步骤：（a）在肟形成溶剂存在下，使环十二酮与羟胺在水溶液中反应，生成环十二烷酮肟; （b）将在肟形成步骤后获得的反应混合物分离成油相和水相，并收集油相的环十二烷酮肟溶液; （c）从油/水相分离步骤中以油相收集的环十二烷酮肟溶液中除去部分或全部肟形成溶剂和溶解的水，由此制备含有使用的重排溶剂的溶液在后续步骤中的重排反应和环十二酮肟; （d）使用含芳环的化合物作为重排催化剂，通过重排反应从环十二酮肟生产月桂内酰胺; 和（e）在重排步骤之后从反应混合物中分离和除去重排溶剂和重排催化剂，并纯化月桂内酰胺。

112. 发明申请

US20120238538A1 MACROCYCLIC AMIDES, PHARMACEUTICAL COMPOSITIONS, PREPARATION METHODS AND USES THEREOF 有权
标题翻译：高分子化合物，药物组合物，制备方法及其用途
公开(公告)号：US20120238538A1
公开(公告)日：2012-09-20
申请号：US13512672
申请日：2010-11-30
申请人： Chongren Yang , Haizhou Li , Ping Zhao , Yingjun Zhang
发明人： Chongren Yang , Haizhou Li , Ping Zhao , Yingjun Zhang
IPC分类号： C07D225/02 , C12P17/10 , A61P31/04 , A61P35/02 , A61K31/395 , A61P35/00
CPC分类号： C07D225/02 , A01N43/46 , A01N63/02
摘要： Macrocyclic amide WH-21091 with antibacterial and antitumor activities, its analogs, preparation methods and uses thereof. The said macrocyclic amides are prepared by microbes of Xenorhabdus and Photorhabdus, or they can be prepared by other living beings through transgenic techniques. The compositions of the said macrocyclic amide and its analogs can be used as drugs and/or agricultural chemicals for treatment of microbial infections, especially for treatment of infectious diseases of Staphylococcus aureus with drug resistance. The said compositions can also be used as drugs for treatment of cancers of human beings or animals.
摘要翻译：具有抗菌和抗肿瘤活性的大环酰胺WH-21091，其类似物，其制备方法和用途。所述大环酰胺由Xenorhabdus和Photorhabdus的微生物制备，或者它们可以通过转基因技术由其他生物制备。所述大环酰胺及其类似物的组合物可用作药物和/或农药用于治疗微生物感染，特别是用于治疗具有耐药性的金黄色葡萄球菌感染性疾病。所述组合物还可以用作治疗人类或动物癌症的药物。

113. 发明申请

US20110281916A1 MIGRASTATIN ANALOGS AND USES THEREOF 有权
标题翻译：麦格拉他汀类似物及其用途
公开(公告)号：US20110281916A1
公开(公告)日：2011-11-17
申请号：US13106625
申请日：2011-05-12
申请人： Samuel J. Danishefsky , Christoph Gaul , Jon T. Njardarson
发明人： Samuel J. Danishefsky , Christoph Gaul , Jon T. Njardarson
IPC分类号： A61K31/4427 , A61K31/365 , A61P35/04 , A61K31/4412
CPC分类号： C07D313/00 , A61K31/365 , A61K31/395 , A61K31/435 , C07D225/02 , C07D405/06 , C07D495/04 , A61K2300/00
摘要： The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof, compositions thereof, and methods for the use thereof in the treatment of various disorders including cancer, metastasis and disorders involving increased angiogenesis, wherein R1-R6, Ra-Rc, Q, Y1, Y2 and n are as defined herein.
摘要翻译：本发明提供了具有式（I）的化合物：另外提供了其合成方法，组合物及其在治疗包括癌症，转移和涉及血管生成增加的疾病的各种疾病中的应用的方法，其中R1-R6， Ra-Rc，Q，Y1，Y2和n如本文所定义。

114. 发明申请

US20110117606A1 NRPS-PKS Gene Cluster and its Manipulation and Utility 有权
标题翻译： NRPS-PKS基因簇及其操作和实用性
公开(公告)号：US20110117606A1
公开(公告)日：2011-05-19
申请号：US12922718
申请日：2009-03-20
申请人： Hanne Jørgensen , Trond Erling Ellingsen , Kristin Fløgstad Degnes , Per Bruheim , Håvard Sletta , Espen Fjaervik , Geir Klinkenberg , Sergey Zotchev
发明人： Hanne Jørgensen , Trond Erling Ellingsen , Kristin Fløgstad Degnes , Per Bruheim , Håvard Sletta , Espen Fjaervik , Geir Klinkenberg , Sergey Zotchev
IPC分类号： C12P19/34 , C07H21/04 , C12N9/00 , C12P7/26 , C12P17/10 , C12N1/00 , C12N1/21 , C12N1/20
CPC分类号： C12N15/52 , C07D225/02 , C07K14/36 , C12P17/10 , C12P19/62 , C12R1/465
摘要： The present invention provides a nucleic acid molecule comprising: (a) a nucleotide sequence as shown in SEQ ID No. 1; or (b) a nucleotide sequence which is the complement of SEQ ID No. 1; or (c) a nucleotide sequence which is degenerate with SEQ ID No. 1; or (d) a nucleotide sequence having at least 85% sequence identity (preferably at least 87%, 90%, 91%, 92%, 93%, 94%, 95%, 96%, 97%, 98% or 99% sequence identity) with SEQ ID No. 1; or (e) a part of any one of (a) to (d), wherein said nucleic acid molecule encodes or is a complementary to a nucleic acid molecule encoding one or more polypeptides, or comprises or is complementary to a nucleic acid molecule comprising one or more genetic elements, having functional activity in the synthesis of a polyketide-based or macrolactam molecule. Particularly the invention contemplates the modification of the nucleic acid of the invention, encoding the biosynthetic machinery for the synthesis of the polyketide macrolactam BE-14106, including expressing in a microorganism the modified nucleic acid molecule. In certain aspects the modification includes introducing, mutating, deleting, replacing or inactivating a sequence encoding one or more activities or proteins encoded by said nucleic acid molecule. Other aspects of the invention include a microorganism containing the modified and unmodified nucleic acid and recovering the polyketide-based or macrolactam molecule from said mircoorganism.
摘要翻译：本发明提供了一种核酸分子，其包含：（a）SEQ ID No.1所示的核苷酸序列; 或（b）作为SEQ ID No.1的互补序列的核苷酸序列; 或（c）与SEQ ID No.1退行的核苷酸序列; 或（d）具有至少85％序列同一性（优选至少87％，90％，91％，92％，93％，94％，95％，96％，97％，98％或99％序列同一性）; 或（e）（a）至（d）中任一项的一部分，其中所述核酸分子编码或与编码一种或多种多肽的核酸分子互补，或包含或互补于包含一种或多种在合成聚酮化合物或大内酰胺分子中具有功能活性的遗传元件。特别地，本发明考虑了本发明的核酸的修饰，其编码用于合成聚酮化物大内酰胺BE-14106的生物合成机理，包括在微生物中表达经修饰的核酸分子。在某些方面，修饰包括引入，突变，缺失，替换或失活编码由所述核酸分子编码的一种或多种活性或蛋白质的序列。本发明的其它方面包括含有经修饰和未修饰的核酸的微生物，并从所述微生物中回收聚酮化合物或大环内酰胺分子。

115. 发明申请

US20100324283A1 PROCESS FOR PRODUCING LAUROLACTAM 有权
标题翻译：生产乳酸菌的方法
公开(公告)号：US20100324283A1
公开(公告)日：2010-12-23
申请号：US12526494
申请日：2008-02-08
申请人： Kazuaki Ishihara , Junichi Kugimoto , Joji Kawai
发明人： Kazuaki Ishihara , Junichi Kugimoto , Joji Kawai
IPC分类号： C07D225/02
CPC分类号： C07D201/04 , C07D225/02 , Y02P20/582
摘要： Disclosed is a method for producing laurolactam from cyclododecanone and hydroxylamine in a simple process and with high efficiency. The method comprises the following steps (a) to (e): (a) reacting cyclododecanone with hydroxylamine in an aqueous solution in the presence of an excess amount of cyclododecanone or a solvent to produce cyclododecanone oxime; (b) separating the reaction mixture obtained after the oxime-forming step into an oil and an aqueous phases and collecting a solution of cyclododecanone oxime of the oil phase as; (c) removing dissolved water from the solution of cyclododecanone oxime which is collected as an oily phase in the oil/aqueous phase separation step; (d) producing laurolactam from cyclododecanone oxime by rearrangement reaction using an aromatic-ring containing compound as a rearrangement catalyst; and (e) separating the produced laurolactam from the reaction mixture after the rearrangement step and purifying the laurolactam.
摘要翻译：公开了一种以简单的工艺和高效率从环十二酮和羟胺制备月桂内酰胺的方法。该方法包括以下步骤（a）至（e）：（a）在过量的环十二烷酮或溶剂存在下，使环十二酮与羟胺在水溶液中反应，生成环十二酮肟; （b）将在肟形成步骤后获得的反应混合物分离成油和水相，并收集油相的环十二酮肟溶液; （c）从在油/水相分离步骤中以油相收集的环十二酮肟溶液中除去溶解的水; （d）使用含芳环的化合物作为重排催化剂，通过重排反应从环十二酮肟生产月桂内酰胺; 和（e）在重排步骤之后将所生产的月桂内酰胺与反应混合物分离并纯化十二内酰胺。

116. 发明授权

US07608611B2 Hsp90 inhibitors, methods of making and uses therefor 有权
标题翻译： Hsp90抑制剂，其制备方法和用途
公开(公告)号：US07608611B2
公开(公告)日：2009-10-27
申请号：US11218320
申请日：2005-08-31
申请人： David Ross , David Siegel , Philip Reigan , Wenchang Guo , Daniel L. Gustafson
发明人： David Ross , David Siegel , Philip Reigan , Wenchang Guo , Daniel L. Gustafson
IPC分类号： A01N43/00 , A61K31/33 , C07D225/00 , C07D295/00
CPC分类号： C07D225/02 , C07D225/06 , C07H17/02 , C07H19/00
摘要： The invention provides purified 18,21-didehydro-18,21-dideoxo-18,21-dihydroxy-geldanamycin derivatives, pharmaceutically acceptable salts thereof and prodrugs thereof that are potent Hsp90 binding agents that are useful for the treatment and/or the amelioration of symptoms of cancer and other proliferative tissue disorders.
摘要翻译：本发明提供了纯化的18,21-二脱氢-18,21-二脱氧-18,21-二羟基 - 格尔德霉素衍生物，其药学上可接受的盐和其前体药物，其是有效的Hsp90结合剂，其可用于治疗和/或改善癌症和其他增生性组织疾病的症状。

117. 发明申请

US20090093628A1 Process for Production of Amides or Lactams 审中-公开
标题翻译：酰胺或内酰胺的生产工艺
公开(公告)号：US20090093628A1
公开(公告)日：2009-04-09
申请号：US12224660
申请日：2007-02-27
申请人： Yasutaka Ishii , Tatsuya Nakano , Takahiro Iwahama
发明人： Yasutaka Ishii , Tatsuya Nakano , Takahiro Iwahama
IPC分类号： C07D403/04
CPC分类号： C07D201/04 , C07C231/10 , C07D223/10 , C07D225/02
摘要： An amide or lactam is produced by conducting a rearrangement of a corresponding oxime compound in the presence of a cyclic compound containing a structure represented by following Formula (1) as a ring constituent and a fluorinated alcohol: wherein Z represents a halogen atom or an —OR group, where R represents an organic group.Z is preferably chlorine atom. Exemplary fluorinated alcohols include fluorine-containing branched-chain aliphatic alcohols represented by following Formula (3): wherein Rf1 and Rf2 may be the same as or different from each other and each represent a perfluoroalkyl group having one to eight carbon atoms; and “n” denotes an integer of 0 to 8.According to this process, amides or lactams can be simply produced in high yields without causing large amounts of by-products.
摘要翻译：酰胺或内酰胺通过在含有下式（1）表示的结构的环状化合物作为环成分和氟化醇的存在下进行相应的肟化合物的重排而制备：其中Z表示卤素原子或 - OR基，其中R表示有机基团。 Z优选为氯原子。示例性的氟化醇包括由下式（3）表示的含氟支链脂族醇：其中Rf1和Rf2可以相同或不同，并且各自表示具有1-8个碳原子的全氟烷基; “n”表示0〜8的整数。根据该方法，可以高产率地简单地制造酰胺或内酰胺而不会产生大量的副产物。

118. 发明授权

US07494986B2 Cycloalkylamine derivatives as NK-1/SSRI antagonists 有权
标题翻译：环烷基胺衍生物作为NK-1 / SSRI拮抗剂
公开(公告)号：US07494986B2
公开(公告)日：2009-02-24
申请号：US11183699
申请日：2005-07-18
申请人： Yong-Jin Wu , Huan He
发明人： Yong-Jin Wu , Huan He
IPC分类号： A01N43/00 , A61K31/33 , C07D225/00 , C07D295/00
CPC分类号： C07D225/02
摘要： The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment relates to compounds of Formula (I) or an isomer, a pharmaceutically acceptable salt or solvate thereof and pharmaceutically acceptable formulations comprising said compounds useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.
摘要翻译：本公开涉及化学化合物及其在人类治疗中的用途。具体实施方案涉及式（I）化合物或其异构体，药学上可接受的盐或溶剂合物和药学上可接受的制剂，其包含用于治疗或预防由速激肽介导的病症和/或选择性抑制5-羟色胺再摄取转运蛋白。该化合物作为双重NK-1拮抗剂和选择性5-羟色胺再摄取抑制剂。

119. 发明申请

US20070105861A1 NOVEL VANILLOID RECEPTOR LIGANDS AND USE THEREOF FOR THE PRODUCTION OF PHARMACEUTICAL PREPARATIONS 失效
标题翻译：新型VANILLOID受体配体及其用于生产药物制剂的用途
公开(公告)号：US20070105861A1
公开(公告)日：2007-05-10
申请号：US11551060
申请日：2006-10-19
申请人： Jeewoo Lee , Hyung Ryu , Robert Frank , Gregor Bahrenberg , Jean De Vry , Thomas Christoph , Derek Saunders , Klaus Schiene , Bernd Sundermann
发明人： Jeewoo Lee , Hyung Ryu , Robert Frank , Gregor Bahrenberg , Jean De Vry , Thomas Christoph , Derek Saunders , Klaus Schiene , Bernd Sundermann
IPC分类号： A61K31/53 , A61K31/506 , A61K31/501 , A61K31/497 , C07D403/04
CPC分类号： C07D409/04 , C07C311/08 , C07C2601/08 , C07C2601/14 , C07D211/14 , C07D211/18 , C07D213/40 , C07D213/64 , C07D213/70 , C07D213/74 , C07D213/81 , C07D213/83 , C07D223/04 , C07D225/02 , C07D295/135 , C07D401/04 , C07D401/12 , C07D401/14 , C07D413/04
摘要： The present invention relates to novel vanilloid receptor ligands, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use of these compounds for the production of pharmaceutical preparations.
摘要翻译：本发明涉及新型香草酸受体配体，其制备方法，含有这些化合物的药物制剂以及这些化合物用于制备药物制剂的用途。

120. 发明申请

US20070037852A1 Migrastatin analogs and uses thereof 有权
标题翻译： Migrastatin类似物及其用途
公开(公告)号：US20070037852A1
公开(公告)日：2007-02-15
申请号：US10551158
申请日：2004-03-26
申请人： Samuel Danishefsky , Christoph Gaul , Jon Njardarson
发明人： Samuel Danishefsky , Christoph Gaul , Jon Njardarson
IPC分类号： A61K31/452 , A61K31/45 , C07D405/02 , C07D403/02
CPC分类号： C07D313/00 , A61K31/365 , A61K31/395 , A61K31/435 , C07D225/02 , C07D405/06 , C07D495/04 , A61K2300/00
摘要： The present invention provides compounds having formula (I), and additionally provides methods for the synthesis thereof, compositions thereof, and methods for the use thereof in the treatment of various disorders including cancer, metastasis and disorders involving increased angiogenesis, wherein R1—R6, Ra—Rc, Q, Y1, Y2 and n are as defined herein.
摘要翻译：本发明提供了具有式（I）的化合物，另外提供了其合成方法，组合物及其在治疗包括癌症，转移和涉及血管生成增加的疾病的各种疾病中的应用的方法，其中R 1个R 6，R 1，R 2，C 1，Y 1， SUB＆gt; 2＆gt;和n如本文所定义。

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