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1. 发明申请

US20170224679A1 Use of CXCR2 Antagonists For The Prevention and/or Treatment of Chemotherapy Induced Peripheral Neuropathy (CIPN) 审中-公开
公开(公告)号：US20170224679A1
公开(公告)日：2017-08-10
申请号：US15500758
申请日：2015-07-27
申请人： GlaxoSmithKline Intellectual Property Development Limited
发明人： Ebere F. IGBOKO , Paul Bryan WREN
IPC分类号： A61K31/495 , A61K45/06 , A61K31/282 , A61K31/341 , A61K31/277 , A61K31/40 , A61K31/17 , A61K31/445 , A61K31/351
CPC分类号： A61K31/495 , A61K31/17 , A61K31/277 , A61K31/282 , A61K31/341 , A61K31/351 , A61K31/40 , A61K31/445 , A61K31/4462 , A61K31/555 , A61K45/06 , C07D211/54 , C07D295/135 , C07D307/18 , C07D309/08 , A61K2300/00
摘要： The invention relates to the use of a CXCR2 antagonist for the prevention and/or treatment of chemotherapy induced peripheral neuropathy (CIPN).

2. 发明授权

US09718798B2 Solid forms of 5-(halomethyl)furfural and methods for preparing thereof 有权
公开(公告)号：US09718798B2
公开(公告)日：2017-08-01
申请号：US14852152
申请日：2015-09-11
申请人： MICROMIDAS, INC.
发明人： Shawn M. Browning , Makoto N. Masuno , John Bissell, II , Benjamin F. Nicholson
IPC分类号： C07D307/18 , C07D307/46 , C07D307/48
CPC分类号： C07D307/46 , C07D307/18 , C07D307/48
摘要： Provided are solid forms of 5-(halomethyl)furfural, including a crystalline form of 5-(chloromethyl)furfural. Provided are also methods for preparing solid forms of 5-(halomethyl)furfural by crystallization using certain solvents.

3. 发明申请

US20170190681A1 1-(CYCLOPENT-2-EN-1-YL)-3-(2-HYDROXY-3-(ARYLSULFONYL)PHENYL)UREA DERIVATIVES AS CXCR2 INHIBITORS 审中-公开
公开(公告)号：US20170190681A1
公开(公告)日：2017-07-06
申请号：US15314124
申请日：2015-05-27
申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
发明人： Weichun CHEN , Ebere F. IGBOKO , Xichen LIN , Hongfu LU , Feng REN , Paul Bryan WREN , Zhongmiao XU , Ting YANG , Lingdong ZHU
IPC分类号： C07D307/18 , C07D241/04
CPC分类号： C07D307/18 , C07C311/47 , C07C317/42 , C07C317/50 , C07C2101/10 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07D207/10 , C07D211/54 , C07D213/34 , C07D233/64 , C07D239/26 , C07D241/04 , C07D295/135 , C07D305/06 , C07D309/08 , C07D471/04 , C07D487/04
摘要： The invention relates to 1-(3-sulfonylphenyl)-3-(cyclopent-2-en-1-yl)urea derivatives, and their use in treating or preventing diseases and conditions mediated by the CXCR2 receptor In addition, the invention relates to compositions containing the derivatives and processes for their preparation

4. 发明申请

US20150225335A1 NOVEL HYDROXAMIC ACID DERIVATIVE 审中-公开
标题翻译：新型羟基酸衍生物
公开(公告)号：US20150225335A1
公开(公告)日：2015-08-13
申请号：US14692200
申请日：2015-04-21
申请人： TAISHO PHARMACEUTICAL CO., LTD. , TOYAMA CHEMICAL CO., LTD.
发明人： Hajime TAKASHIMA , Risa TSURUTA , Tetsuya YABUUCHI , Yusuke OKA , Hiroki URABE , Yoichiro SUGA , Masato TAKAHASHI , Fumito UNEUCHI , Hironori KOTSUBO , Muneo SHOJI , Yasuko KAWAGUCHI
IPC分类号： C07C233/83 , C07C235/84 , C07C309/30 , C07D317/60 , C07D498/04 , C07D263/32 , C07D261/08 , C07D307/81 , C07D265/36 , C07C237/36 , C07D209/08
CPC分类号： C07C233/83 , C07C235/84 , C07C237/36 , C07C259/06 , C07C271/22 , C07C271/28 , C07C309/30 , C07C311/08 , C07C317/28 , C07C317/44 , C07C323/41 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/08 , C07D205/04 , C07D205/12 , C07D207/10 , C07D207/12 , C07D207/27 , C07D207/327 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/44 , C07D209/52 , C07D211/14 , C07D211/18 , C07D211/38 , C07D211/46 , C07D211/56 , C07D211/70 , C07D213/38 , C07D213/40 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/70 , C07D213/74 , C07D213/81 , C07D215/14 , C07D217/04 , C07D217/12 , C07D231/12 , C07D231/56 , C07D233/61 , C07D235/04 , C07D257/04 , C07D261/08 , C07D263/14 , C07D263/32 , C07D263/56 , C07D265/30 , C07D265/36 , C07D265/38 , C07D267/10 , C07D271/12 , C07D277/20 , C07D277/30 , C07D277/62 , C07D277/66 , C07D285/12 , C07D295/08 , C07D295/12 , C07D295/14 , C07D295/16 , C07D305/06 , C07D305/08 , C07D307/14 , C07D307/18 , C07D307/52 , C07D307/54 , C07D307/78 , C07D307/81 , C07D307/82 , C07D307/87 , C07D309/04 , C07D309/14 , C07D317/30 , C07D317/60 , C07D319/18 , C07D319/20 , C07D333/24 , C07D405/06 , C07D413/06 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/20 , C07D498/04 , C07D498/08 , C07F9/091
摘要： Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including Pseudomonas aeruginosa and its drug resistant bacteria. Provided is a hydroxamic acid derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof:
摘要翻译：提供了通过抑制LpxC活性可用作药物组合物的新型化合物，从而对包括绿脓假单胞菌及其耐药细菌在内的革兰氏阴性细菌表现出有效的抗微生物活性。提供由以下通式[1]表示的异羟肟酸衍生物或其药学上可接受的盐：

5. 发明授权

US08933236B2 N-substituted benzamides and methods of use thereof 有权
标题翻译： N-取代苯甲酰胺及其使用方法
公开(公告)号：US08933236B2
公开(公告)日：2015-01-13
申请号：US13899469
申请日：2013-05-21
申请人： Genentech, Inc. , Xenon Pharmaceuticals Inc.
发明人： Sultan Chowdhury , Christoph Martin Dehnhardt , Thilo Focken , Michael Edward Grimwood , Ivan William Hemeon , Qi Jia , Daniel Ortwine , Brian Safina , Shaoyi Sun , Daniel P. Sutherlin , Alla Yurevna Zenova
IPC分类号： C07C311/51 , C07D403/12 , C07D213/82 , C07D213/64 , C07D205/04 , C07D311/58 , A61K31/445 , A61K31/44 , A61K31/18 , C07D265/30 , C07D233/84 , C07D257/04 , C07C307/06 , C07D295/26 , C07D207/48 , C07D311/70 , C07D413/12 , C07D451/02 , C07D307/12 , C07D309/08 , C07D311/72 , C07D405/12 , C07D491/107 , C07D211/22 , C07D295/192 , C07D211/96 , C07D307/18
CPC分类号： C07D491/107 , A61K31/18 , A61K31/397 , A61K31/40 , A61K31/41 , A61K31/4164 , A61K31/44 , A61K31/5375 , C07B2200/05 , C07C307/06 , C07C311/51 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/10 , C07C2602/18 , C07C2602/20 , C07C2602/42 , C07C2602/44 , C07C2602/50 , C07C2603/66 , C07C2603/68 , C07C2603/74 , C07D205/04 , C07D207/46 , C07D207/48 , C07D209/52 , C07D211/22 , C07D211/96 , C07D213/64 , C07D213/82 , C07D233/84 , C07D257/04 , C07D265/30 , C07D295/192 , C07D295/26 , C07D307/12 , C07D307/18 , C07D309/08 , C07D311/58 , C07D311/70 , C07D311/72 , C07D403/12 , C07D405/12 , C07D413/12 , C07D451/02 , C07D471/08
摘要： The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
摘要翻译：本发明提供具有以下通式的新化合物及其药学上可接受的盐，其中变量RA，下标n，环A，X2，L，下标m，X1，B，R1，R2，R3，R4，R5和RN具有本文所述的含义，以及含有这些化合物的组合物和使用这些化合物和组合物的方法。

6. 发明申请

US20130317001A1 N-SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF 有权
公开(公告)号：US20130317001A1
公开(公告)日：2013-11-28
申请号：US13899526
申请日：2013-05-21
申请人： XENON PHARMACEUTICALS INC. , GENENTECH, INC.
发明人： Jean-Christophe Andrez , Sultan Chowdhury , Shannon Marie Decker , Christoph Martin Dehnhardt , Thilo Focken , Michael Edward Grimwood , Ivan William Hemeon , Qi Jia , Jun Li , Daniel F. Ortwine , Brian Safina , Tao Sheng , Shaoyi Sun , Daniel P. Sutherlin , Michael Scott Wilson , Alla Yurevna Zenova
IPC分类号： C07D403/12 , C07D213/64 , C07D205/04 , C07D311/58 , C07D295/26 , C07D233/84 , C07D257/04 , C07C311/51 , C07C307/06 , C07D213/82 , C07D265/30
CPC分类号： C07D491/107 , A61K31/18 , A61K31/397 , A61K31/40 , A61K31/41 , A61K31/4164 , A61K31/44 , A61K31/5375 , C07B2200/05 , C07C307/06 , C07C311/51 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/10 , C07C2602/18 , C07C2602/20 , C07C2602/42 , C07C2602/44 , C07C2602/50 , C07C2603/66 , C07C2603/68 , C07C2603/74 , C07D205/04 , C07D207/46 , C07D207/48 , C07D209/52 , C07D211/22 , C07D211/96 , C07D213/64 , C07D213/82 , C07D233/84 , C07D257/04 , C07D265/30 , C07D295/192 , C07D295/26 , C07D307/12 , C07D307/18 , C07D309/08 , C07D311/58 , C07D311/70 , C07D311/72 , C07D403/12 , C07D405/12 , C07D413/12 , C07D451/02 , C07D471/08
摘要： The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

7. 发明授权

US07851411B2 α-Cyanoacrylates 失效
标题翻译： α-氰基丙烯酸酯
公开(公告)号：US07851411B2
公开(公告)日：2010-12-14
申请号：US10499522
申请日：2002-12-17
申请人： Peter Plath , Norbert Götz , Michael Rack , Andreas Landes , Cyrill Zagar , Matthias Witschel , Klaus Groβmann
发明人： Peter Plath , Norbert Götz , Michael Rack , Andreas Landes , Cyrill Zagar , Matthias Witschel , Klaus Groβmann
IPC分类号： A01N43/36 , A01N37/00 , A01N37/34 , C07D295/104 , C07D305/06 , C07C255/07
CPC分类号： C07D295/185 , A01N37/44 , A01N43/08 , A01N43/16 , C07C255/30 , C07C323/60 , C07C327/22 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D305/08 , C07D307/18 , C07D307/20 , C07D307/22 , C07D309/14 , C07D319/06 , C07D331/04
摘要： α-Cyanoacrylates of the formula I, where: R1 is ORa wherein Ra is hydrogen, substituted alkyl, branched alkyl, branched alkenyl, cycloloalkyl, heterocyclyl, aryl, phenylalkyl or alkylimino; is NRbRc wherein Rb is hydrogen, alkyl which may be substituted, alkenyl, alkynyl; Rc is hydrogen, alkyl which may be substituted alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, phenylalkyl or alkylimino; or Rb and Rc form an alkandiyl-chain which may be substituted; or is SRd wherein Rd is hydrogen, alkyl which may be substituted, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, phenylalkyl or alkylimino; R2 is alkyl which may be substituted; is alkenyl or alkynyl; R3 is alkyl may be substituted; is alkenyl or alkynyl; R4 is hydrogen, halogen, cyano or alkyl; and their agriculturally useful salts, processes and intermediates for their preparation; and the use of these compounds or of compositions comprising these compounds for controlling undesirable plants are described.
摘要翻译：式I的α-氰基丙烯酸酯，其中：R 1是OR a，其中R a是氢，取代的烷基，支链烷基，支链烯基，环烷基，杂环基，芳基，苯基烷基或烷基亚氨基; 是NRbRc，其中Rb是氢，可以被取代的烷基，烯基，炔基; Rc是氢，可以被取代的烯基，炔基，环烷基，杂环基，芳基，苯基烷基或烷基亚氨基的烷基; 或R b和R c形成可被取代的烷撑二链; 或者是其中Rd为氢的SRd，可以被取代的烷基，烯基，炔基，环烷基，杂环基，芳基，苯基烷基或烷基亚氨基; R2是可被取代的烷基; 是烯基或炔基; R3是烷基可以被取代; 是烯基或炔基; R4是氢，卤素，氰基或烷基; 及其农业上有用的盐，其制备方法和中间体; 并且描述了这些化合物或包含这些化合物的组合物用于防治不期望的植物的用途。

8. 发明申请

US20040167029A1 Substituted benzoyl derivatives as herbicides 审中-公开
标题翻译：取代的苯甲酰基衍生物作为除草剂
公开(公告)号：US20040167029A1
公开(公告)日：2004-08-26
申请号：US10754081
申请日：2004-01-08
申请人： Bayer CropScience GmbH
发明人： Andreas Van Almsick , Lothar Willms , Hermann Bieringer , Hubert Menne , Thomas Auler
IPC分类号： A01N043/76 , A01N043/84 , C07D265/30 , C07D263/02
CPC分类号： C07D307/18 , C07D307/20 , C07D307/33 , C07D309/12 , C07D309/18 , C07D319/06 , C07D405/12
摘要： What is described are derivatives of benzoyl derivatives of the formula (I) and their use as herbicides. 1 In this formula (I), R1, R2 and R3 are different radicals, X is a bridge atom selected from the group consisting of oxygen and sulfur and Het is a saturated heterocyclic group which comprises oxygen and carbon atoms.
摘要翻译：所描述的是式（I）的苯甲酰基衍生物的衍生物及其作为除草剂的用途。在该式（I）中，R 1，R 2和R 3是不同的基团，X是选自氧和硫的桥原子，Het是饱和杂环基，其包含氧和碳原子。

9. 发明授权

US5625075A Metal radionuclide chelating compounds for improved chelation kinetics 失效
标题翻译：用于改善螯合动力学的金属放射性核素螯合化合物
公开(公告)号：US5625075A
公开(公告)日：1997-04-29
申请号：US459414
申请日：1995-06-02
申请人： Ananthachari Srinivasan , Alan R. Fritzberg , David S. Jones
发明人： Ananthachari Srinivasan , Alan R. Fritzberg , David S. Jones
IPC分类号： A61K47/48 , A61K51/10 , C07C327/30 , C07C327/32 , C07D207/46 , C07D209/48 , C07D307/18 , C07D405/12 , C07C67/00 , C07C233/01 , C07D315/00
CPC分类号： C07D209/48 , A61K47/48707 , A61K51/1093 , C07C327/30 , C07C327/32 , C07D207/46 , C07D307/18 , C07D405/12 , A61K2121/00 , A61K2123/00
摘要： The present invention provides metal chelating compounds, to chelates and chelate-targeting agent conjugates formed from the chelating compounds, and to methods for making and using these compositions. The chelating compounds incorporate two nitrogen atoms and three sulfur atoms ("N.sub.2 S.sub.3 "), two nitrogen atoms and four sulfur atoms ("N.sub.2 S.sub.4 "), or three nitrogen atoms and three sulfur atoms ("N.sub.3 S.sub.3 "). Metals, and metal oxides, capable of being chelated by the compounds include those that are radionuclides, such as .sup.99m Tc and .sup.186/188 Re.The targeting agent portion of the chelate-targeting agent conjugates provided includes antibodies, peptides, hormones, enzymes and biological response modifiers. Methods for making the conjugates are provided and encompass the addition of a metal, or metal oxide, to a chelating compound prior to attachment to a targeting agent as well as subsequent to the attachment.Another aspect of the invention provides kits for producing chelate-targeting agent conjugates for radiopharmaceutical use.An additional aspect of the invention provides methods for using the chelate-targeting agent conjugates for diagnostic and therapeutic purposes, such as detection of a target site and delivery of a radionuclide to the site, respectively.
摘要翻译：本发明提供金属螯合化合物，由螯合化合物形成的螯合物和螯合靶向试剂缀合物，以及制备和使用这些组合物的方法。螯合化合物包含两个氮原子和三个硫原子（“N2S3”），两个氮原子和四个硫原子（“N2S4”）或三个氮原子和三个硫原子（“N3S3”）。能够被化合物螯合的金属和金属氧化物包括那些是放射性核素，例如99mTc和186 / 188Re。提供的螯合靶向药物缀合物的靶向剂部分包括抗体，肽，激素，酶和生物反应调节剂。提供了制备缀合物的方法，并且包括在附着到靶向剂之前以及在附着之后将金属或金属氧化物加入到螯合化合物中。本发明的另一方面提供了用于制备用于放射性药物用途的螯合靶向剂缀合物的试剂盒。本发明的另一方面提供了用于诊断和治疗目的的螯合靶向剂缀合物的使用方法，例如分别检测靶位点和将放射性核素递送至位点。

10. 发明授权

US5623081A Method for producing tetrahydrofuranyl compounds 失效
标题翻译：四氢呋喃基化合物的制备方法
公开(公告)号：US5623081A
公开(公告)日：1997-04-22
申请号：US448052
申请日：1995-05-23
申请人： Yang-I Lin , Panayota Bitha , Subas Sakya , Timothy W. Strohmeyer , Karen Bush , Carl B. Ziegler , Gregg B. Feigelson
发明人： Yang-I Lin , Panayota Bitha , Subas Sakya , Timothy W. Strohmeyer , Karen Bush , Carl B. Ziegler , Gregg B. Feigelson
IPC分类号： A61K31/40 , A61K31/397 , A61K31/4015 , A61K31/403 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/495 , A61K31/535 , A61P31/00 , A61P31/04 , C07D307/18 , C07D333/34 , C07D333/48 , C07D477/00 , C07D477/04 , C07D477/06 , C07D477/12 , C07D477/14 , C07D477/20 , C07F9/6561 , C07H11/00 , C07H19/01 , C07D307/02
CPC分类号： C07D307/18 , C07D333/34 , C07D477/14 , C07F9/65611 , C07H11/00 , C07H19/01 , Y02P20/582
摘要： Tetrahydrofuanyl compounds of the following formulae: ##STR1## are disclosed.
摘要翻译：公开了下式的四氢芳烃基化合物：。

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