公开(公告)号：US20200255385A1

公开(公告)日：2020-08-13

申请号：US16789687

申请日：2020-05-04

申请人： CV6 Therapeutics (NI) Limited

发明人： Mark Spyvee ,  Pravin S. Shirude

IPC分类号： C07D233/74 ,  C07D277/34 ,  C07D263/44 ,  C07D251/10 ,  C07D249/12 ,  C07D241/08 ,  C07D239/22 ,  C07D233/46 ,  C07D207/404 ,  C07D207/36 ,  C07D487/04 ,  C07D405/12 ,  C07D403/12 ,  C07D401/12 ,  A61P35/00 ,  C07D207/40 ,  C07D211/88 ,  A61K31/4015 ,  C07F9/6506

摘要： Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.

公开(公告)号：US20200223827A1

公开(公告)日：2020-07-16

申请号：US16712660

申请日：2019-12-12

申请人： YUHAN CORPORATION

发明人： Tae Dong HAN ,  Hee Jae TAK ,  Eun Kyung KIM ,  Eui Chul LEE ,  Sol PARK ,  Hyok Jun CHO ,  Cheol Hee LIM ,  So Young KIM ,  Hyun Ho CHOI ,  Da Na JEONG ,  Na Yeon YANG ,  Na Ry HA

IPC分类号： C07D403/10 ,  C07D249/12 ,  C07D403/04 ,  C07D401/04 ,  C07D405/10 ,  C07D401/10 ,  C07D401/14 ,  C07D405/14 ,  C07D403/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14

摘要： The present technology provides 3,3-difluoroallylamines or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The 3,3-difluoroallylamines or their pharmaceutically acceptable salts exhibit potent inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).

公开(公告)号：US20200178530A1

公开(公告)日：2020-06-11

申请号：US16629879

申请日：2017-07-15

申请人： QINGDAO KINGAGROOT CHEMICAL COMPOUND CO., LTD.

发明人： De ZHAO ,  Tao JIN ,  Beibei LIN ,  Qiang RU

IPC分类号： A01N43/653 ,  C07D249/12

摘要： The present invention relates to the technical field of herbicide crystallization process, particularly to Crystalline form C of shuangzuocaotong, and a preparation method therefor and use thereof. The Crystalline form C of shuangzuocaotong has an X-ray powder diffraction pattern having characteristic absorption peaks at the following 2θ positions: 10.159, 10.658, 13.318, 14.579, 16.096, 18.061, 19.322, 19.68, 20.04, 20.659, 21.281, 23, 24.16, 24.619, 26.101, 26.74, 30.359, 31.018, 32.378, 35.398 and 38.26 degrees, wherein 2θ has an error range within ±0.2°. The Crystalline form C of shuangzuocaotong has good stability, and its compounded composition with additional active ingredient(s) has a good control effect to broadleaf weeds and some gramineous weeds in wheat, significantly better than that of Crystalline form A of shuangzuocaotong.

公开(公告)号：US20200148628A1

公开(公告)日：2020-05-14

申请号：US16740466

申请日：2020-01-12

申请人： National Institute of Biological Sciences, Beijing

发明人： Niu Huang ,  Shiming Peng

IPC分类号： C07C255/34 ,  C07C255/43 ,  C07D277/64 ,  C07D213/75 ,  C07D257/04 ,  C07D307/46 ,  C07D261/08 ,  C07D277/24 ,  C07D233/56 ,  C07D239/26 ,  C07D209/08 ,  C07D231/14 ,  C07D235/08 ,  C07D487/04 ,  C07D211/82 ,  C07D249/12 ,  C07D277/56 ,  C07D215/233 ,  C07D239/42 ,  C07D261/12 ,  C07D249/08 ,  C07D241/12 ,  C07D295/185 ,  C07D285/08 ,  C07D241/20 ,  C07D213/80 ,  C07D471/04 ,  C07D241/52 ,  C07D251/16 ,  C07D241/24 ,  C07D239/36 ,  C07D237/14 ,  C07D213/57 ,  C07D277/46 ,  C07D277/30 ,  A61P3/04 ,  A61P25/28

摘要： The invention provides compounds that inhibit FTO (fat mass and obesity), including pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof, particularly obesity, with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

公开(公告)号：US10645930B2

公开(公告)日：2020-05-12

申请号：US14799692

申请日：2015-07-15

申请人： BASF SE

发明人： Eberhard Ammermann ,  Reinhard Stierl ,  Gisela Lorenz ,  Siegfried Strathmann ,  Klaus Schelberger ,  V. James Spadafora ,  Thomas Christen

IPC分类号： A01N43/653 ,  A01N43/40 ,  A01N43/56 ,  C07D249/12 ,  A01N47/24 ,  A01N37/50 ,  A01N37/18

摘要： Disclosed is a fungicidal mixture containing (1) 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro[1,2,4]-triazole-3-thion of formula (I) or the salts or adducts thereof, and at least one additional fungicidal compound or the salts or adducts thereof, selected among (2) trifloxystrobin of formula (II), (3) picoxystrobin of formula (III), (4) pyraclostrobin of formula (IV), (5) dimoxystrobin of formula (V), and (6) a strobilurin derivative of formula (VI), in a synergistically active quantity.

公开(公告)号：US10570098B2

公开(公告)日：2020-02-25

申请号：US15741202

申请日：2016-07-07

申请人： CV6 Therapeutics (NI) Limited

发明人： Mark Spyvee ,  Pravin S. Shirude

IPC分类号： A61K31/4015 ,  C07D233/74 ,  C07F9/6506 ,  C07D211/88 ,  C07D207/40 ,  A61P35/00 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D487/04 ,  C07D207/36 ,  C07D207/404 ,  C07D233/46 ,  C07D239/22 ,  C07D241/08 ,  C07D249/12 ,  C07D251/10 ,  C07D263/44 ,  C07D277/34

摘要： Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.

公开(公告)号：US20190135766A1

公开(公告)日：2019-05-09

申请号：US16236039

申请日：2018-12-28

申请人： ORIENTAL (LUZHOU) AGROCHEMICALS. CO., LTD.

发明人： Qiuju SHENG ,  Zhiming ZHANG ,  Junliang WANG ,  Bangchi CHEN

IPC分类号： C07D249/12 ,  C07C251/78

摘要： Disclosed are a method of synthesizing prothioconazole and optically active isomers thereof and intermediates. The method includes reacting hydrazine with glyoxylic acid to produce a hydrazono acetic acid as an intermediate, and then reacting the intermediate with thiocyanate to produce the target product prothioconazole. The present method is very specific in terms of regioselectivity, resulting in minimum byproducts and a high product yield. The present method does not require special equipment, nor anhydrous or oxygen-free manipulations. The process is simple and generates minimum wastes, suitable for industrial production.

公开(公告)号：US20190111028A1

公开(公告)日：2019-04-18

申请号：US16218856

申请日：2018-12-13

申请人： Ardea Biosciences, Inc.

发明人： Laszlo R. Treiber ,  Irina Zamansky ,  Jean-Luc Girardet

IPC分类号： A61K31/4196 ,  C07D249/06 ,  A61K31/519 ,  C07D249/12 ,  A61K31/426 ,  A61K31/522

摘要： Crystalline polymorph forms of 2-(5-bromo-4-(4-cyclopropyl naphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid are described. Pharmaceutical compositions and the uses of such compounds, compound forms, and compositions for the treatment of a variety of diseases and conditions are also presented.

公开(公告)号：US10252984B2

公开(公告)日：2019-04-09

申请号：US14354326

申请日：2012-10-26

申请人： Mayo Foundation for Medical Education and Research

发明人： Alexander Keith Stewart ,  Artem Plekhov ,  Robert Greenhouse

IPC分类号： C07D403/10 ,  C07D221/18 ,  C07D237/34 ,  C07D239/70 ,  C07D249/12 ,  C07D285/135 ,  C07D295/13 ,  C07D311/30 ,  C07D311/58 ,  C07D401/08 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/056 ,  C07C233/65 ,  C07H15/22 ,  A61K31/4196 ,  A61K31/433 ,  A61K31/454 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/352 ,  A61K31/4245 ,  A61K31/47 ,  A61K31/4985 ,  A61K31/549 ,  A61K31/55

摘要： This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.

公开(公告)号：US20190071405A1

公开(公告)日：2019-03-07

申请号：US16181864

申请日：2018-11-06

申请人： AUTIFONY THERAPEUTICS LIMITED

发明人： Agostino Marasco ,  Giuseppe Alvaro ,  Anne Dècor ,  Dieter Hamprecht ,  Paolo Dambruoso ,  Simona Tommasi

IPC分类号： C07D249/12 ,  C07C255/37 ,  C07C43/225 ,  C07C255/46 ,  C07C43/313 ,  C07D307/87 ,  C07D401/04 ,  C07D311/96 ,  C07D311/76 ,  C07D311/04 ,  C07D307/94 ,  C07D405/14 ,  C07C255/48 ,  C07C43/29

摘要： Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders.