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公开(公告)号：US09944659B2
公开(公告)日：2018-04-17
申请号：US14855646
申请日：2015-09-16
申请人： Intrexon Corporation
CPC分类号： C07F5/025 , A01N37/28 , A01N55/08 , A61K31/69 , A61K45/06 , C07D263/06 , A61K2300/00
摘要： The present disclosure provides boron-containing diacylhydrazines having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein A, R4, and R5 are defined as set forth in the specification. The present disclosure also provides the use of boron-containing diacylhydrazines is ecdysone receptor-based inducible gene expression systems. Thus, the present disclosure is useful for applications such as gene therapy, treatment of disease, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable.
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公开(公告)号：US09828333B2
公开(公告)日：2017-11-28
申请号：US14354654
申请日：2012-10-29
发明人： Bernd Clement , Joscha Kotthaus , Jurke Kotthaus , Dennis Schade
IPC分类号： C07C235/68 , C07C231/12 , A61K31/165 , A61K31/192 , A61K31/609 , C07C275/14 , C07C279/16 , C07D263/06
CPC分类号： C07C235/68 , C07C231/12 , C07C275/14 , C07C279/16 , C07C2601/16 , C07D263/06
摘要： The invention relates to oseltamivir derivatives as influenza neuraminidase inhibitors for treating influenza infections and to a method for producing said compounds.
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公开(公告)号：US09732049B2
公开(公告)日：2017-08-15
申请号：US15121836
申请日：2015-03-02
申请人： Nosopharm
发明人： Emilie Racine
IPC分类号： C07C269/04 , C07C227/04 , C07C227/16 , C07C227/18 , C07D263/06
CPC分类号： C07D263/06 , C07C227/04 , C07C227/16 , C07C227/18 , C07C269/04 , C07C229/26 , C07C271/22
摘要： The present invention relates to a process for the synthesis of 2,4-diamino-3(S)-hydroxycarboxylic acid derivatives from 5-hydroxyectoine.
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公开(公告)号：US09724682B2
公开(公告)日：2017-08-08
申请号：US15345266
申请日：2016-11-07
IPC分类号： C07D263/04 , C07D211/16 , C07D209/54 , C07D207/06 , C07D207/16 , C07D205/04 , B01J31/22 , C07C209/02 , C07F15/02 , C07D263/06
CPC分类号： B01J31/2273 , C07C209/02 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2603/74 , C07D205/04 , C07D207/06 , C07D207/16 , C07D209/54 , C07D211/16 , C07D263/04 , C07D263/06 , C07F15/025 , C07C211/40 , C07C211/38 , C07C211/41
摘要： The present invention provides novel synthetic methods for making acyclic secondary amines by reacting an azide with a compound bearing one or more C—H groups, catalyzed by a FeII-dipyrromethene complex. The acyclic secondary amines are thought to be formed through an intermolecular nitrene transfer. Also provided herein are methods of synthesizing protected (e.g., Boc- or Fmoc-protected) cyclic secondary amines (e.g., 5-, 6-, and 7-membered cyclic secondary amines) by reacting an azide that bears one or more C—H groups, catalyzed by a FeII-dipyrromethene complex. The protected cyclic secondary amines are thought to be formed through an intramolecular nitrene transfer and may be subsequently deprotected to yield cyclic secondary amines.
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5.发明授权Synthesis of acyclic and cyclic amines using iron-catalyzed nitrene group transfer 有权使用铁催化的硝基转移合成无环和环胺公开(公告)号：US09487472B2
公开(公告)日：2016-11-08
申请号：US14770217
申请日：2014-02-26
IPC分类号： C07C209/02 , C07C211/40 , C07C211/41 , C07F15/02 , C07D205/04 , C07D207/06 , C07D207/16 , C07D209/54 , C07D211/16 , C07D263/04
CPC分类号： B01J31/2273 , C07C209/02 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2603/74 , C07D205/04 , C07D207/06 , C07D207/16 , C07D209/54 , C07D211/16 , C07D263/04 , C07D263/06 , C07F15/025 , C07C211/40 , C07C211/38 , C07C211/41
摘要： The present invention provides novel synthetic methods for making acyclic secondary amines by reacting an azide with a compound bearing one or more C—H groups, catalyzed by a FeII-dipyrromethene complex. The acyclic secondary amines are thought to be formed through an intermolecular nitrene transfer. Also provided herein are methods of synthesizing protected (e.g., Boc- or Fmoc-protected) cyclic secondary amines (e.g., 5-, 6-, and 7-membered cyclic secondary amines) by reacting an azide that bears one or more C—H groups, catalyzed by a FeII-dipyrromethene complex. The protected cyclic secondary amines are thought to be formed through an intramolecular nitrene transfer and may be subsequently deprotected to yield cyclic secondary amines.
摘要翻译： 本发明提供了通过使叠氮化物与含有一个或多个C-H基团的化合物反应，由FeII-二吡咯亚甲基络合物催化制备无环仲胺的新型合成方法。 认为无环仲胺是通过分子间硝基转移而形成的。 本文还提供了通过使含有一个或多个C-H的叠氮化物反应合成受保护（例如，Boc-或Fmoc保护的）环状仲胺（例如，5-，6-和7-元环状仲胺）的方法 基团，由FeII-二吡咯亚甲基络合物催化。 保护的环状仲胺被认为是通过分子内的nitrene转移形成的，随后可以去保护以产生环状仲胺。
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公开(公告)号：US20160176828A1
公开(公告)日：2016-06-23
申请号：US14565890
申请日：2013-06-12
IPC分类号： C07D265/06 , C07D263/06 , A01N43/76 , A01N43/86
CPC分类号： C07D265/06 , A01N43/76 , A01N43/86 , C07D263/06
摘要： Provided are compounds which are useful for controlling microorganisms in aqueous or water-containing systems or in systems which are exposed to moisture, including at elevated temperature. The antimicrobial compounds are of the formula I: wherein n, R1, R2, R3, R4, R5, and X are as defined herein.
摘要翻译： 提供了可用于控制含水或含水体系中的微生物或暴露于水分的系统中的化合物，包括在升高的温度下。 抗微生物化合物具有式I：其中n，R1，R2，R3，R4，R5和X如本文所定义。
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公开(公告)号：US09278922B2
公开(公告)日：2016-03-08
申请号：US12759986
申请日：2010-04-14
申请人： Pamela L. Donner , Lissa T. Nelson , Tammie K. Jinkerson , Ryan G. Keddy , Christopher E. Motter , Mark A. Matulenko , Allan C. Krueger , David A. DeGoey , Sachin V. Patel , John T. Randolph , Warren M. Kati , Charles W. Hutchins , Todd N. Soltwedel
发明人： Pamela L. Donner , Lissa T. Nelson , Tammie K. Jinkerson , Ryan G. Keddy , Christopher E. Motter , Mark A. Matulenko , Allan C. Krueger , David A. DeGoey , Sachin V. Patel , John T. Randolph , Warren M. Kati , Charles W. Hutchins , Todd N. Soltwedel
IPC分类号： A61K38/05 , A61K31/4025 , A61K31/4184 , A61K31/5377 , C07K5/02 , C07K5/062 , A61P31/14 , C07D403/12 , C07D403/14 , C07D413/14 , C07D207/16 , A61K31/454 , C07D205/04 , C07D207/22 , C07D209/52 , C07D211/60 , C07D263/06 , C07D277/06 , C07D401/14 , C07D405/14 , C07D417/14 , C07D487/04 , C07K5/065 , C07K5/078 , A61K38/00
CPC分类号： C07D207/16 , A61K31/4025 , A61K31/4184 , A61K31/454 , A61K31/5377 , A61K38/00 , C07D205/04 , C07D207/22 , C07D209/52 , C07D211/60 , C07D263/06 , C07D277/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07K5/06034 , C07K5/06043 , C07K5/0606 , C07K5/06069 , C07K5/06078 , C07K5/06139
摘要： Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
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公开(公告)号：US20150087832A1
公开(公告)日：2015-03-26
申请号：US14354158
申请日：2012-10-22
发明人： John Y.L. Chung , Kevin Campos , Edward Cleator , Robert F. Dunn , Andrew Gibson , R. Scott Hoerrner , Stephen Keen , Dave Liebermann , Zhuqing Liu , Joseph Lynch , Kevine M. Maloney , Feng Xu , Nobuyoshi Yasuda , Naoki Yoshikawa , Yong-Li Zhong
IPC分类号： C07D487/04 , C07D263/06 , C07D403/12 , C07D207/09
CPC分类号： C07D487/04 , A61K31/4196 , A61K31/519 , C07B2200/13 , C07D207/09 , C07D263/06 , C07D403/12
摘要： The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.
摘要翻译： 本发明涉及制备式（I）和式（II）及其中间体的β3激动剂的方法。 β3激动剂可用于治疗某些疾病，包括膀胱过度活动症，尿失禁和尿急。
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公开(公告)号：US20120237448A9
公开(公告)日：2012-09-20
申请号：US12584131
申请日：2009-08-31
IPC分类号： A61K49/00 , C07C215/28 , A61P35/00 , A61K31/137 , A61P25/00
CPC分类号： A61K31/135 , A61K31/40 , C07C215/28 , C07C217/64 , C07C233/18 , C07C323/32 , C07D263/06 , C07D295/092
摘要： Provided are novel compositions and analogs which are useful in a number of applications, indications and diseases, as well as for monitoring pharmakinetics and patient management. These compounds and analogs are applicable to treating tumors of the central nervous system, e.g., glioblastoma (GBM).
摘要翻译： 提供了可用于许多应用，适应症和疾病以及用于监测药物药物和患者管理的新型组合物和类似物。 这些化合物和类似物可用于治疗中枢神经系统的肿瘤，例如胶质母细胞瘤（GBM）。
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公开(公告)号：US20120172604A1
公开(公告)日：2012-07-05
申请号：US13410405
申请日：2012-03-02
申请人： Gordon T. Rivers , Jun Tian , James A. Hackerott
发明人： Gordon T. Rivers , Jun Tian , James A. Hackerott
IPC分类号： C07D263/06
CPC分类号： C07C7/20 , C07D263/06 , C09K8/52 , C09K2208/22 , C10L1/233 , C10L3/06 , C10L3/107 , C07C9/04
摘要： Oxazolidinium compounds are formed by the reaction of a halohydrin or an epoxide with a secondary amine and an aldehyde or a ketone. The oxazolidinium compounds are formed directly and do not require the reaction of a pre-formed oxazolidine with an alkylating agent. The compounds are useful as gas hydrate inhibitors in oil and gas production and transportation. The oxazolidinium compounds have the structure: where R is a saturated or unsaturated alkyl group containing from 3 to 20 carbon atoms, where R has an absence of aryl groups; R1 and R2 each independently have 1 to 20 carbon atoms, may be linear, branched or cyclic; linear, branched or cyclic groups having 1 to 20 carbon atoms substituted with alkyl groups, aryl groups, alkylaryl groups, and aryl groups substituted with alkoxy groups, and X is selected from the group consisting of chlorine, fluorine, bromine or iodine.
摘要翻译： 恶唑烷鎓化合物通过卤代醇或环氧化物与仲胺和醛或酮的反应形成。 恶唑烷鎓化合物直接形成，不需要预形成的恶唑烷与烷基化剂的反应。 该化合物可用作油气生产和运输中的天然气水合物抑制剂。 恶唑烷鎓化合物具有以下结构：其中R是含有3至20个碳原子的饱和或不饱和烷基，其中R不存在芳基; R 1和R 2各自独立地具有1至20个碳原子，可以是直链，支链或环状的; 被烷基取代的具有1至20个碳原子的直链，支链或环状基团，芳基，烷基芳基和被烷氧基取代的芳基，X选自氯，氟，溴或碘。
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