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1. 发明授权

US10662192B2 Modulators of ATP-binding cassette transporters 有权
公开(公告)号：US10662192B2
公开(公告)日：2020-05-26
申请号：US16006105
申请日：2018-06-12
申请人： Vertex Pharmaceuticals Incorporated
发明人： Sara Hadida-Ruah , Anna Hazlewood , Peter Grootenhuis , Fredrick Van Goor , Ashvani Singh , Jinglan Zhou , Jason McCartney
IPC分类号： C07C205/11 , C07C205/58 , C07D471/10 , C07C211/17 , C07C209/00 , C07C215/28 , C07D209/08 , C07D209/14 , C07D209/18 , C07D209/42 , C07D209/94 , C07D213/20 , C07D213/73 , C07D215/227 , C07D215/38 , C07D217/06 , C07D223/16 , C07D265/36 , C07D279/16 , C07D311/58 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07C215/76 , C07D215/56 , C07D401/12 , C07D215/233 , A61K8/49 , A61K31/47 , A61K31/4709 , A61K45/06 , C07C215/78 , C07C217/84 , C07D209/12 , C07D209/20 , A61K31/136 , A61K31/265 , A61K31/352 , A61K31/404 , A61K31/4045 , A61K31/4747 , A61K31/55 , C07C219/34 , G01N33/566 , G01N33/487 , G01N33/50 , G01N33/68 , C07C217/80 , C07C229/52 , A61K31/04 , A61K31/27 , A61K31/277 , A61K31/403 , A61K31/44 , A61K31/472 , A61K31/538 , A61K31/5415 , C07C211/50 , C07C211/52 , C07C215/70 , C07C217/76 , C07C255/58 , C07C271/20 , C07C311/08 , C07C311/39 , C07D209/04 , C07D209/96 , C07D217/04
摘要： The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

2. 发明申请

US20200155511A1 ISOXAZOLINE-SUBSTITUTED BENZAMIDE COMPOUND AND PESTICIDE 审中-公开
公开(公告)号：US20200155511A1
公开(公告)日：2020-05-21
申请号：US16709370
申请日：2019-12-10
申请人： NISSAN CHEMICAL CORPORATION
发明人： Takeshi MITA , Takamasa Kikuchi , Takashi Mizukoshi , Manabu Yaosaka , Mitsuaki Komoda , Shinji Takii
IPC分类号： A61K31/421 , A61K9/00 , C07D413/14 , C07D261/04 , C07D413/04 , C07F7/08 , C07D417/12 , C07D417/06 , C07D413/12 , C07D413/06 , C07D261/16 , C07C323/09 , C07C281/02 , C07C255/60 , C07C255/50 , C07C255/29 , C07C251/48 , C07C211/52 , C07C205/12 , C07C205/11 , C07C43/174 , A01N43/80 , C07C25/08 , C07C25/06 , C07C25/02 , C07C25/24 , C07C25/13
摘要： A substituted alkenylbenzene compound of formula (4): wherein X1 is selected from the group consisting of a halogen atom, —SF5, C1-C6haloalkyl, hydroxy C1-C6haloalkyl, C1-C6alkoxy C1-C6haloalkyl, C3-C8halocycloalkyl, C1-C6haloalkoxy, C1-C3haloalkoxy C1-C3haloalkoxy, C1-C6haloalkylthio, C1-C6haloalkylsulfinyl and C1-C6haloalkylsulfonyl; X3 is selected from the group consisting of a hydrogen atom, halogen atom, cyano, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy and C1-C6alkylthio; X4 is selected from the group consisting of a hydrogen atom, halogen atom, cyano, C1-C4alkyl, C1-C4alkoxy and C1-C4haloalkoxy; R3 is —C(R3a)(R3b)R3c, where R3a and R3b independently of each other are a halogen atom, or R3a and R3b together form 3- to 6-membered ring together with the carbon atom bonding them by forming a C2-C5haloalkylene chain, and R3c is selected from the group consisting of a hydrogen atom, halogen atom, C1-C5alkyl, C1-C5haloalkyl, C1-C4haloalkoxy and C1-C4haloalkylthio, with a proviso that in case where X1 is a fluorine atom, chlorine atom or trifluoromethyl, and both X2 and X3 are a hydrogen atom, in case where both X1 and X2 are fluorine atom and X3 is a hydrogen atom, and in case where both X1 and X2 are trifluoromethyl and X3 is a hydrogen atom, R3c is a hydrogen atom, chlorine atom, bromine atom, iodine atom, C1-C5alkyl, C1-C5haloalkyl, C1-C4haloalkoxy or C1-C4haloalkylthio.

3. 发明授权

US09815768B2 Method for producing 2-(halogenomethyl)-3-methylnitrobenzene 有权
公开(公告)号：US09815768B2
公开(公告)日：2017-11-14
申请号：US15112617
申请日：2015-02-16
申请人： SUMITOMO CHEMICAL COMPANY, LIMITED
发明人： Satoru Ujita , Takashi Miyamoto
IPC分类号： C07C205/11 , C07C201/12 , B01J23/44
CPC分类号： C07C205/11 , B01J21/18 , B01J23/44 , C07C201/12
摘要： Position-1 halogen can be selectively reduced by reacting a compound represented by formula (3): [wherein X represents a chlorine atom, a bromine atom, or an iodine atom] with halogen in the presence of a heterogeneous transition metal catalyst to produce 2-(halogenomethyl)-1-methyl-3-nitrobenzene represented by formula (1): [wherein the symbol is as defined above].

4. 发明申请

US20120232278A1 Insecticidal Aryl Pyrrolidines 有权
标题翻译：杀虫芳基吡咯烷酮
公开(公告)号：US20120232278A1
公开(公告)日：2012-09-13
申请号：US13472020
申请日：2012-05-15
申请人： Jun MIHARA , Tetsuya MURATA , Daiei YAMAZAKI , Yasushi YONETA , Katsuhiko SHIBUYA , Eiichi SHIMOJO , Ulrich GÖRGENS
发明人： Jun MIHARA , Tetsuya MURATA , Daiei YAMAZAKI , Yasushi YONETA , Katsuhiko SHIBUYA , Eiichi SHIMOJO , Ulrich GÖRGENS
IPC分类号： C07D207/08 , C07D401/12 , C07C233/02 , C07C233/66 , C07C205/11
CPC分类号： C07D401/14 , A01N43/36 , A01N43/40 , C07C205/11 , C07D207/04 , C07D207/06 , C07D211/18 , C07D401/04 , C07D401/12 , C07D403/10
摘要： The present invention provides novel aryl pyrrolidines having an excellent insecticidal action as insecticides. Aryl pyrrolidines represented by the formula (I) and use thereof as insecticide.
摘要翻译：本发明提供作为杀虫剂具有优异杀虫作用的新型芳基吡咯烷。由式（I）表示的芳基吡咯烷酮及其作为杀虫剂的用途。

5. 发明申请

US20090312584A1 Process For Preparing High Purity TNT 有权
标题翻译：制备高纯度TNT的方法
公开(公告)号：US20090312584A1
公开(公告)日：2009-12-17
申请号：US10553825
申请日：2004-04-21
申请人： Keith S. Kyler , Andrew R. Wilson , Curtis Teague
发明人： Keith S. Kyler , Andrew R. Wilson , Curtis Teague
IPC分类号： C07C205/11
CPC分类号： C07C201/08 , C07C205/06
摘要： A process for preparing trinitrololuene (TNT) in which toluene is treated with nitric acid having a concentration of about 90% to about 99%, and preferably about 98% to about 99%, by weight at a temperature of less than about 60° C., and preferably less than 30° C., to produce high purity dinitrotoluene. The resulting dinitrotoluene is then treated with nitric acid having a concentration of about 98% to about 99% by weight and trifluoromethane sulfuric acid to produce high purity TNT.
摘要翻译：一种制备三硝基甲苯（TNT）的方法，其中甲苯在低于约60℃的温度下用浓度为约90％至约99％，优选约98％至约99％的硝酸处理优选小于30℃，以产生高纯度二硝基甲苯。然后用浓度为约98％至约99％重量的硝酸和三氟甲烷硫酸处理所得的二硝基甲苯以产生高纯度TNT。

6. 发明授权

US6166272A Molybdenum trioxide catalyzed fluorination reactions 失效
标题翻译：三氧化钼催化氟化反应
公开(公告)号：US6166272A
公开(公告)日：2000-12-26
申请号：US373133
申请日：1999-08-12
申请人： Sanjay Mandal
发明人： Sanjay Mandal
IPC分类号： C07B39/00 , C07C17/20 , C07C205/11 , C07C22/00 , C07C41/00 , C07C209/00
CPC分类号： C07C205/11 , C07B39/00 , C07C17/206 , C07C22/08
摘要： Disclosed is a method of fluorinating a substrate having the general formula ##STR1## where each R is independently selected from halogen, alkyl from C.sub.1 to C.sub.12, aryl from C.sub.6 to C.sub.12, alkoxide from C.sub.1 to C.sub.12, aryloxide from C.sub.6 to C.sub.12, nitro, amino, alkylamino from C.sub.1 to C.sub.12, and arylamino from C.sub.6 to C.sub.12, each X is independently selected from halogen and at least one X is chlorine or bromine, each m is independently selected from 0 to 5, n is 0 or 1, p is 0 or 1, q is 0 or 1, and n+p+q is 1. The substrate is heated to a temperature of about 40 to about 100.degree. C. and is reacted with a fluorinating agent in the presence of about 0.05 to about 2 wt % molybdenum trioxide. The composition of the substrate, the catalyst, and the fluorinating agent is also disclosed.
摘要翻译：公开了一种氟化具有以下通式的底物的方法，其中每个R独立地选自卤素，C1至C12的烷基，C6至C12的芳基，C1至C12的烷氧基，C6至C12的芳氧基，硝基，氨基，烷基氨基 C 1〜C 12的芳基氨基，C 6〜C 12的芳基氨基，X各自独立地选自卤素，至少一个X为氯或溴，m各自独立地选自0〜5，n为0或1，p为0或1 ，q为0或1，n + p + q为1.将基材加热至约40至约100℃的温度，并在约0.05至约2重量％的存在下与氟化剂反应，三氧化钼。还公开了底物，催化剂和氟化剂的组成。

7. 发明授权

US6100431A Process for the preparation of thioether-substituted aromatic ketones 失效
公开(公告)号：US6100431A
公开(公告)日：2000-08-08
申请号：US88778
申请日：1998-06-02
申请人： Neil W. Boaz
发明人： Neil W. Boaz
IPC分类号： C07C45/27 , C07C45/32 , C07C201/12 , C07C205/06 , C07C205/11 , C07C205/37 , C07C205/45 , C07C319/14 , C07C323/22 , C07C319/00
CPC分类号： C07C201/12 , C07C201/14 , C07C319/14 , C07C45/27 , C07C45/32
摘要： The preparation of aromatic ketones substituted with a thioether group at the ortho position is accomplished by the initial reaction of an aromatic nucleus substituted with a halide and an ortho nitro group with a nitroalkane in the presence of a hydroxide base. The resulting ortho-nitroalkyl nitroarene compound is converted to the corresponding ortho-nitroaryl ketone by an oxidative Nef reaction. The aromatic nitro group of the ortho-nitroaryl ketone is replaced with a thioether group by reaction with a thiolate anion, most preferably under phase-transfer conditions. Aromatic ketones may be used to prepare various pharmaceutical and herbicidal compounds.

8. 发明授权

US6096929A Process for the preparation of thioether-substituted aromatic ketones 失效
标题翻译：制备硫醚取代的芳族酮的方法
公开(公告)号：US6096929A
公开(公告)日：2000-08-01
申请号：US369300
申请日：1999-08-06
申请人： Neil W. Boaz
发明人： Neil W. Boaz
IPC分类号： C07C201/12 , C07C205/11 , C07C205/45 , C07C319/14 , C07C323/22 , C07C205/00
CPC分类号： C07C319/14 , C07C201/12
摘要： The preparation of aromatic ketones substituted with a thioether group at the ortho position is accomplished by the initial reaction of an aromatic nucleus substituted with a halide and an ortho nitro group with a nitroalkane in the presence of a hydroxide base. The resulting ortho-nitroalkyl nitroarene compound is converted to the corresponding ortho-nitroaryl ketone by an oxidative Nef reaction. The aromatic nitro group of the ortho-nitroaryl ketone is replaced with a thioether group by reaction with a thiolate anion, most preferably under phase-transfer conditions. Aromatic ketones may be used to prepare various pharmaceutical and herbicidal compounds.
摘要翻译：在邻位置由硫醚基取代的芳族酮的制备通过在氢氧化物碱存在下，用卤化物和邻硝基取代的芳香核与硝基烷烃的初始反应来实现。所得邻硝基烷基硝基芳烃化合物通过氧化Nef反应转化成相应的邻硝基芳基酮。通过与硫醇盐阴离子反应，最优选在相转移条件下，邻硝基芳基酮的芳基硝基被硫醚基取代。芳族酮可用于制备各种药物和除草化合物。

9. 发明授权

US5856576A Aryne intermediates and a process for the preparation thereof 失效
标题翻译： Aryne中间体及其制备方法
公开(公告)号：US5856576A
公开(公告)日：1999-01-05
申请号：US15817
申请日：1998-01-29
申请人： Philip M. Harrington , Kenneth A. M. Kremer
发明人： Philip M. Harrington , Kenneth A. M. Kremer
IPC分类号： C07C205/11 , C07C205/19 , C07C205/45 , C07C215/68 , C07C225/22 , C07C209/74
CPC分类号： C07C205/19 , C07C205/11 , C07C205/45 , C07C215/68 , C07C225/22
摘要： There are provided aryne intermediates of formula I, useful in the manufacture of herbicidal compounds. ##STR1## Also provided is a method to prepare the formula I intermediates via the palladium catalyzed coupling of an o-halonitrobenzene or o-haloaniline with 3-butyne-1-ol.
摘要翻译：提供了可用于制备除草化合物的式I的中间体。（I）还提供了通过钯 - 催化偶合O-卤代硝基苯或邻 - 卤代苯胺与3-丁炔-1-醇制备式I中间体的方法。

10. 发明授权

US5792892A Processes for preparing aromatic, bromine-containing compounds, novel bromine-containing compounds, and their use as intermediate products in the synthesis of active agents 失效
标题翻译：用于制备芳族，含溴化合物，新型含溴化合物的方法及其作为活性剂合成中的中间产物的用途
公开(公告)号：US5792892A
公开(公告)日：1998-08-11
申请号：US732306
申请日：1996-10-22
申请人： Hermann Hagemann
发明人： Hermann Hagemann
IPC分类号： C07D215/56 , B01J27/125 , B01J27/128 , C07B39/00 , C07B61/00 , C07C17/12 , C07C25/13 , C07C51/093 , C07C51/62 , C07C63/70 , C07C205/11 , C07C205/12 , C07C19/08 , C07C22/00 , C07C63/04
CPC分类号： C07C201/12 , C07B39/00 , C07C17/12 , C07C25/13 , C07C51/093 , C07C51/62
摘要： The present invention relates to processes for the preparation of bromine-containing aromatic compounds, to novel bromine-containing compounds and to their use as intermediates in the synthesis of active substances. Processes according to the invention for the preparation of known and novel bromine-containing compounds are characterized by specific conditions.
摘要翻译： PCT No.PCT / EP95 / 01439 Sec。 371日期1996年10月22日第 102（e）日期1996年10月22日PCT 1995年4月18日PCT PCT。公开号WO95 / 29886 日期：1995年11月9日本发明涉及制备含溴芳族化合物，新型含溴化合物的方法及其在合成活性物质中的用途。根据本发明制备已知和新型含溴化合物的方法的特征在于具体条件。

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