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1. 发明申请

US20180244662A1 PROCESSES FOR PREPARING ATR INHIBITORS 审中-公开
公开(公告)号：US20180244662A1
公开(公告)日：2018-08-30
申请号：US15849241
申请日：2017-12-20
申请人： Vertex Pharmaceuticals Incorporated
发明人： Jean-Damien Charrier , John Studley , Francoise Yvonne Theodora Marie Pierard , Steven John Durrant , Benjamin Joseph Littler , Robert Michael Hughes , David Andrew Siesel , Paul Angell , Armando Urbina , Yi Shi
IPC分类号： C07D413/04 , C07D241/20 , C07C251/48 , C07D413/14
CPC分类号： C07D413/04 , C07C251/48 , C07D241/20 , C07D413/14
摘要： The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention.The compounds of this invention have formula I or II: wherein the variables are as defined herein.

2. 发明申请

US20170362168A1 METHOD FOR PREPARATION OF 5-ALKYLSALICYLALDOXIMES AND APPLICATION THEREOF 审中-公开
公开(公告)号：US20170362168A1
公开(公告)日：2017-12-21
申请号：US15694032
申请日：2017-09-01
申请人： Politechnika Warszawska
发明人： Krzysztof BUJNOWSKI , Ludwik SYNORADZKI , Jerzy WISIALSKI , Agnieszka KROLIKOWSKA , Jacek BORDZILOWSKI , Marcin KOZIOROWSKI , Roman ZADROZNY , Anna JERZAK , Krzysztof DZIENIS
IPC分类号： C07C249/04 , C23F11/14 , C09D5/08
CPC分类号： C07C249/04 , C07C249/08 , C08K5/33 , C09D5/086 , C23F11/147 , C07C251/48
摘要： Method for preparation of 5-alkylsalicylaldoximes with formula 1, where R is a C6-C16 alkyl group, consisting in that into a water-alcohol solvent system, p-alkylphenol, sodium hydroxide, chloroform and hydroxylamine are introduced, while in relation to the alkylphenol used, sodium hydroxide and chloroform are used in amounts from the stoichiometric amount to a 100% excess, and hydroxylamine is used in amounts from the stoichiometric amount to a 60% excess, and the reaction is carried out at a temperature of 60-75° C. for 1.5-4 h, and then, at a temperature of 20-30° C., the post-reaction mixture is acidified till the pH of the aqueous phase

3. 发明授权

US09523683B2 Functionalized polydiacetylene sensors 有权
标题翻译：功能化聚二乙炔传感器
公开(公告)号：US09523683B2
公开(公告)日：2016-12-20
申请号：US14157670
申请日：2014-01-17
申请人： The Regents of the University of Michigan
发明人： Jinsang Kim , Jiseok Lee
IPC分类号： G01N33/542 , G01N33/543 , C07C233/20 , C07C233/49 , C07C233/55 , C07C251/48 , C07D251/30 , C07H21/00 , C40B40/04 , C40B80/00 , G01N33/52 , G01N33/58
CPC分类号： G01N33/5432 , C07B2200/11 , C07C233/20 , C07C233/49 , C07C233/55 , C07C251/48 , C07D251/30 , C07H21/00 , C40B40/04 , C40B80/00 , G01N33/52 , G01N33/542 , G01N33/582
摘要： A microarray includes a solid substrate having a surface, the surface having a plurality of binding spots and a plurality of reaction moieties bound to the binding spots. A reaction moiety includes a plurality of polyacetylene monomers, the polyacetylene monomers having a first coupling region and a second coupling region, the first coupling region having a first functional group operable to bind to the binding spot and the second coupling region comprising a second functional group operable to bind to an accessory molecule; and an accessory molecule having a binding region and an analyte reaction region, the analyte reaction region operable to selectively bind to the target analyte, and the binding region operable to bind to the second coupling region of the polyacetylene monomer. Upon binding a target analyte with the reaction moiety, a color change from the polyacetylene monomer occurs and the reaction moiety produces fluorescence.
摘要翻译：微阵列包括具有表面的固体基质，该表面具有多个结合点和与结合点结合的多个反应部分。反应部分包括多个聚乙炔单体，所述聚乙炔单体具有第一耦合区域和第二耦合区域，所述第一耦合区域具有可操作以结合至所述结合点的第一官能团，所述第二耦合区域包含第二官能团可操作地结合辅助分子; 以及具有结合区域和分析物反应区域的辅助分子，所述分析物反应区域可操作以选择性地结合靶分析物，以及结合区域可操作以结合聚乙炔单体的第二耦合区域。在将目标分析物与反应部分结合时，发生来自聚乙炔单体的颜色变化，并且反应部分产生荧光。

4. 发明申请

US20160324880A1 4-DEDIMETHYLAMINO TETRACYCLINE COMPOUNDS 审中-公开
公开(公告)号：US20160324880A1
公开(公告)日：2016-11-10
申请号：US14962347
申请日：2015-12-08
申请人： Paratek Pharmaceuticals, Inc.
发明人： Mark L. Nelson , Kwasi Ohemeng
IPC分类号： A61K31/65
CPC分类号： A61K31/65 , C07C235/70 , C07C237/26 , C07C251/48 , C07C255/41 , C07C271/22 , C07C271/54 , C07C271/58 , C07C275/42 , C07C275/54 , C07C279/18 , C07C311/06 , C07C311/08 , C07C333/08 , C07C335/22 , C07C381/10 , C07C2601/08 , C07C2601/10 , C07C2601/16 , C07C2603/46 , C07D295/155 , C07D295/185 , C07D317/60 , C07F9/2475 , C07F9/4006
摘要： The present invention pertains, at least in part, to novel substituted 4-dedimethylamino tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

5. 发明申请

US20160318919A1 OXIME-SUBSTITUTED AMIDE COMPOUND AND PEST CONTROL AGENT 审中-公开
标题翻译： OXIME取代的AMIDE化合物和PEST控制剂
公开(公告)号：US20160318919A1
公开(公告)日：2016-11-03
申请号：US15207764
申请日：2016-07-12
申请人： NISSAN CHEMICAL INDUSTRIES, LTD.
发明人： Motoyoshi IWASA , Keisuke TSUJI , Mitsutaka TOMIZAWA , Takeshi MITA , Hidehito KUWAHARA , Miho ASAHI , Hotaka IMANAKA
IPC分类号： C07D417/12 , A01N37/18 , C07C321/28 , A01N41/12 , C07C317/32 , A01N41/10 , C07C255/64 , A01N37/34 , C07D213/53 , A01N43/40 , C07D213/65 , C07F7/08 , A01N55/00 , C07D213/82 , C07D401/12 , C07D241/24 , A01N43/60 , C07D405/12 , C07D333/38 , A01N43/10 , C07D409/12 , C07D413/12 , A01N43/80 , A01N43/76 , A01N43/78 , C07C251/48
CPC分类号： C07D417/12 , A01N37/18 , A01N37/20 , A01N37/34 , A01N41/10 , A01N41/12 , A01N43/10 , A01N43/40 , A01N43/56 , A01N43/60 , A01N43/713 , A01N43/76 , A01N43/78 , A01N43/80 , A01N43/84 , A01N47/12 , A01N55/00 , C07C251/48 , C07C251/52 , C07C255/64 , C07C317/32 , C07C321/28 , C07D213/42 , C07D213/53 , C07D213/61 , C07D213/65 , C07D213/82 , C07D241/24 , C07D333/38 , C07D401/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07F7/0814
摘要： To provide a novel pesticide, especially a fungicide and a nematocide.An oxime-substituted amide compound represented by the formula (I) or its salt, and a pesticide containing it: wherein G1 is a structure represented by G1-1 or the like, G2 is a structure represented by G2-2 or the like: W is an oxygen atom or the like, X1 is a halogen atom, methyl, trifluoromethyl or the like, each of X2, X3, X4 and X5 is independently a hydrogen atom, a halogen atom or the like, each of Y1 and Y3 is independently a halogen atom, cyano, methyl, trifluoromethyl, C2-C6 alkynyl or the like, each of Y2 and Y4 is independently a hydrogen atom, a halogen atom or the like, R1 is C1-C6 alkyl, C1-C4 haloalkyl, (C1-C4)alkyl substituted with R18, C3-C6 cycloalkyl, C3-C6 alkenyl or the like, each of R2 and R3 is independently a hydrogen atom, methyl or the like, R4 is a hydrogen atom or the like, R18 is C3-C6 cycloalkyl, phenyl, phenyl substituted with (Z)m or the like, Z is a halogen atom or the like, and m is an integer of 1, 2 or 3.
摘要翻译： W是氧原子等，X 1是卤素原子，甲基，三氟甲基等，X 2，X 3，X 4和X 5各自独立地为氢原子，卤素原子等，Y 1和Y 3各自为卤素原子，氰基，甲基，三氟甲基，C2-C6炔基等，Y2和Y4各自独立地为氢原子，卤素原子等，R1为C1-C6烷基，C1-C4卤代烷基，（被R 18，C 3 -C 6环烷基，C 3 -C 6烯基等取代的C 1 -C 4烷基，R 2和R 3各自独立地为氢原子，甲基等，R 4为氢原子等，R 18为C 3 -C 6环烷基，苯基，被（Z）m取代的苯基等，Z是卤素原子等，m是1,2或3的整数。

6. 发明申请

US20160207874A1 IMPROVED PROCESS FOR THE REDUCTIVE AMINATION AND SELECTIVE HYDROGENATION OF SUBSTRATES CONTAINING A SELECTED HALOGEN 审中-公开
标题翻译：用于选择性氢化物的底物的还原胺化和选择性加氢的改进方法
公开(公告)号：US20160207874A1
公开(公告)日：2016-07-21
申请号：US14914744
申请日：2014-08-26
申请人： TAMINCO BVBA
发明人： Kristof Moonen , Bart Vandeputte , Daan Scheldeman , Kim Dumoleijn
IPC分类号： C07C209/26 , C07C249/04
CPC分类号： C07C209/26 , C07C209/365 , C07C249/04 , C07C211/52 , C07C251/48 , C07C211/29
摘要： Disclosed is a process for performing a chemical reaction selected from reductive amination and hydrogenation of a first functional group in an organic feed substrate, which feed substrate comprises at least one further functional group containing a halogen atom, wherein the halogen atom is selected from the list consisting of chlorine, bromine, iodine, and combinations thereof, in the presence of hydrogen and a heterogeneous catalyst comprising at least one metal from the list of Pd, Rh, and Ru, together with at least a second metal from the list consisting of Ag, Ni, Co, Sn, Cu and Au. The process is preferably applied for the reductive amination of 2-chloro-benzaldehyde to form 2-chloro-benzyldimethylamine, as an intermediate in the production of agrochemically active compounds and microbiocides of the methoximinophenylglyoxylic ester series. Further disclosed is a composition rich in 2-chloro-benzyldimethylamine, further comprising an amount of 2-chloro-benzyl alcohol and being low in chlorotoluene isomers.
摘要翻译：公开了一种用于进行选自有机原料底物中的第一官能团的还原胺化和氢化的化学反应的方法，该进料底物包含至少一个含有卤素原子的另外的官能团，其中所述卤素原子选自列表由氯，溴，碘及其组合组成，在氢存在下和包含来自Pd，Rh和Ru列表中的至少一种金属的非均相催化剂以及来自列表中的至少一种第二金属由Ag ，Ni，Co，Sn，Cu和Au。该方法优选用于2-氯 - 苯甲醛的还原胺化以形成2-氯 - 苄基二甲胺，作为生产邻氨基苯基乙醛酸酯系列的农业化学活性化合物和杀微生物剂的中间体。进一步公开的是富含2-氯 - 苄基二甲基胺的组合物，其还包含一定量的2-氯 - 苄基醇，并且氯代甲苯异构体低。

7. 发明申请

US20160130219A1 METABOLITES AND OXIMES WITH VASODILATOR AND HYPOTENSIVE ACTIVITY 有权
标题翻译：代谢物和具有血管扩张剂和低血压活性的毒素
公开(公告)号：US20160130219A1
公开(公告)日：2016-05-12
申请号：US14876084
申请日：2015-10-06
申请人： Universidad de Antofagasta
发明人： Adrian Guillermo Paredes Poblete , Glauco Segundo Morales Borcosque , Fredi Eduardo Cifuentes Jorquera
IPC分类号： C07C249/08 , C07C251/48 , C07D307/79 , C07C45/79 , C07C249/14
CPC分类号： C07C249/08 , C07C45/79 , C07C249/14 , C07C251/48 , C07D307/79 , C07C49/835
摘要： Semi-synthetic oximes derived from metabolites extracted from medicinal plants, Senecio nutans and Xenophyllum poposum, the method of preparation thereof and their use as agents with vasodilator and hypotensive effects are provided.
摘要翻译：提供了从药用植物，塞西西诺和爪蟾属植物提取的代谢物，其制备方法及其作为血管扩张剂和降血压作用的药剂的半合成肟。

8. 发明授权

US09278915B2 Agonists of GPR40 有权
标题翻译： GPR40的激进分子
公开(公告)号：US09278915B2
公开(公告)日：2016-03-08
申请号：US13811825
申请日：2011-07-20
申请人： Jagannath Madanahalli Ranganath Rao , Nagarajan Arumugam , Mohd Mudabbir Ansari , Chandrasekhar Gudla , Shanmugam Pachiyappan , Manivannan Ramalingam , Jenson George , George Fernanda Arul , Kenchegowda Bommegowda, Y , Sathesh Kumar Angupillai , Ramamoorthy Kottamalai , Pradeep Jidugu , Shivanageshwara Rao, D
发明人： Jagannath Madanahalli Ranganath Rao , Nagarajan Arumugam , Mohd Mudabbir Ansari , Chandrasekhar Gudla , Shanmugam Pachiyappan , Manivannan Ramalingam , Jenson George , George Fernanda Arul , Kenchegowda Bommegowda, Y , Sathesh Kumar Angupillai , Ramamoorthy Kottamalai , Pradeep Jidugu , Shivanageshwara Rao, D
IPC分类号： C07C251/36 , C07C251/52 , C07C255/52 , C07C255/61 , C07C257/06 , C07C317/32 , C07C251/48 , C07C255/41 , C07D209/14 , C07D213/53 , C07D213/64 , C07D213/74 , C07D249/04 , C07D249/08 , C07D257/04 , C07D261/08 , C07D263/32 , C07D271/10 , C07D277/64 , C07D307/79 , C07D333/22 , C07D333/58 , C07D401/04 , C07D487/04 , C07F9/40 , C07D307/80
CPC分类号： C07C257/06 , C07C251/48 , C07C251/52 , C07C255/41 , C07C255/61 , C07C317/32 , C07C2601/02 , C07C2601/14 , C07D209/14 , C07D213/53 , C07D213/64 , C07D213/74 , C07D249/04 , C07D249/08 , C07D257/04 , C07D261/08 , C07D263/32 , C07D271/10 , C07D277/64 , C07D307/79 , C07D307/80 , C07D333/22 , C07D333/58 , C07D401/04 , C07D487/04 , C07F9/4015 , C07F9/4056
摘要： The present invention relates to compounds that have the ability to modulate the activity of GPR40 and are therefore useful in the treatment of GPR40 related disorders. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders related to GPR40 activity.
摘要翻译：本发明涉及具有调节GPR40活性的能力的化合物，因此可用于治疗GPR40相关疾病。此外，本发明涉及化合物，其制备方法，含有这些化合物的药物组合物以及这些化合物在治疗与GPR40活性相关的某些疾病中的用途。

9. 发明申请

US20160031797A1 ESTROGEN RECEPTOR LIGANDS AND METHODS OF USE THEREOF 有权
标题翻译：雌激素受体配体及其使用方法
公开(公告)号：US20160031797A1
公开(公告)日：2016-02-04
申请号：US14733852
申请日：2015-06-08
申请人： GTx, Inc.
发明人： James T. DALTON , Christina Herring , Duane D. MILLER , Seoung-Soo HONG , Yali HE , Michael L. MOHLER , Ramesh NARAYANAN , Zhongzhi WU
IPC分类号： C07C215/82 , C07C235/56 , C07D295/135 , C07C233/75
CPC分类号： C07C215/82 , A61K31/137 , A61K31/167 , A61K31/4453 , C07C233/75 , C07C235/16 , C07C235/24 , C07C235/38 , C07C235/56 , C07C251/48 , C07C255/58 , C07C311/21 , C07C311/29 , C07C2601/14 , C07D211/06 , C07D221/12 , C07D295/135 , C07D295/155
摘要： The present invention relates to a novel class of nuclear receptor binding agents (NRBAs). The NRBA compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including, inter alia, prevention and treatment of hormone-related diseases, cancers, inflammation, osteoporosis, peripheral vascular disease, reducing circulating lipid levels, and cardiovascular disease.
摘要翻译：本发明涉及一类新的核受体结合剂（NRBAs）。 NRBA化合物适用于预防和/或治疗各种疾病和病症，包括特别是预防和治疗激素相关疾病，癌症，炎症，骨质疏松症，外周血管疾病，降低循环脂质水平，和心血管疾病。

10. 发明授权

US09227923B2 Pesticidal carboxamides 有权
标题翻译：杀虫甲酰胺
公开(公告)号：US09227923B2
公开(公告)日：2016-01-05
申请号：US13390302
申请日：2010-08-03
申请人： Jun Mihara , Koichi Araki , Takuma Mori , Tetsuya Murata , Yasushi Yoneta , Yukiyoshi Watanabe , Eiichi Shimojo , Teruyuki Ichihara , Masashi Ataka , Katsuhiko Shibuya , Ulrich Gorgens
发明人： Jun Mihara , Koichi Araki , Takuma Mori , Tetsuya Murata , Yasushi Yoneta , Yukiyoshi Watanabe , Eiichi Shimojo , Teruyuki Ichihara , Masashi Ataka , Katsuhiko Shibuya , Ulrich Gorgens
IPC分类号： C07C233/65 , A01N37/18 , C07C233/66 , A01N37/42 , A01N37/44 , A01N37/48 , A01N37/50 , A01N43/40 , A01N43/56 , C07C235/84 , C07C237/40 , C07C237/42 , C07C237/48 , C07C251/44 , C07C251/48 , C07C255/19 , C07C255/57 , C07C271/22 , C07C275/24 , C07C309/66 , C07C311/06 , C07C323/60 , C07D209/48 , C07D213/61 , C07D213/81 , C07D213/82 , C07D213/84 , C07D213/85 , C07D231/12 , C07D231/16 , C07D249/08 , C07D249/18 , C07D249/20 , C07D257/04 , C07D295/155 , C07D401/12
CPC分类号： C07C233/66 , A01N37/42 , A01N37/44 , A01N37/48 , A01N37/50 , A01N43/40 , A01N43/56 , C07C235/84 , C07C237/40 , C07C237/42 , C07C237/48 , C07C251/44 , C07C251/48 , C07C255/19 , C07C255/57 , C07C271/22 , C07C275/24 , C07C309/66 , C07C311/06 , C07C323/60 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D209/48 , C07D213/61 , C07D213/81 , C07D213/82 , C07D213/84 , C07D213/85 , C07D231/12 , C07D231/16 , C07D249/08 , C07D249/18 , C07D249/20 , C07D257/04 , C07D295/155 , C07D401/12
摘要： The object of the present invention is to provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Disclosed are the carboxamides represented by the following Formula (I): wherein each substituent is as defined in the specification, and use thereof as pesticides and animal parasite controlling agents.
摘要翻译：本发明的目的是提供一种作为农药具有优良杀虫活性的新型甲酰胺。公开了由下式（I）表示的羧酰胺：其中每个取代基如说明书中所定义，以及其作为农药和动物寄生虫控制剂的用途。

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