公开(公告)号：US20190269637A1

公开(公告)日：2019-09-05

申请号：US16149524

申请日：2018-10-02

申请人： Nogra Pharma Limited

发明人： Sergio Baroni ,  Salvatore Bellinvia ,  Francesca Viti

IPC分类号： A61K31/196 ,  A61Q7/00 ,  A61Q5/00 ,  C07C233/54 ,  C07C235/38 ,  C07D319/08 ,  A61K8/42 ,  A61Q19/08 ,  A61Q19/06 ,  A61Q19/02 ,  C07D307/79

摘要： Disclosed herein are compounds that may be specific to PPAR and/or EGF receptors, and methods of making and using same.

公开(公告)号：US10352929B2

公开(公告)日：2019-07-16

申请号：US15244135

申请日：2016-08-23

申请人： SENOMYX, INC.

发明人： Xiaodong Li ,  Lena Luukkonen ,  Hong Xu

IPC分类号： G01N33/543 ,  C07C233/65 ,  C07C235/54 ,  C07C275/30 ,  C07C275/34 ,  C07D307/84 ,  C07D317/68 ,  G01N33/566 ,  G01N33/74 ,  G01N33/50 ,  A23L2/56 ,  A61K8/49 ,  A61K8/55 ,  A61K47/22 ,  A61K47/24 ,  C07D405/12 ,  C07F9/655 ,  A23L27/00 ,  A23L27/20 ,  C07D263/56 ,  C07D213/81 ,  C07D213/85 ,  C07D215/48 ,  C07D217/06 ,  C07D231/14 ,  C07D333/24 ,  C07D333/38 ,  C07D401/04 ,  C07D409/12 ,  C07D417/12 ,  C07D261/18 ,  C07D271/12 ,  C07D275/03 ,  C07D209/08 ,  C07D277/64 ,  C07D209/42 ,  C07D285/135 ,  C07D213/40 ,  C07D307/52 ,  C07D307/68 ,  C07D307/79 ,  C07D307/82 ,  C07K14/705

摘要： The invention relates to compounds that specifically bind a T1R1/T1R3 or T1R2/T1R3 receptor or fragments or sub-units thereof. The present invention also relates to the use of hetero-oligomeric and chimeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging.

公开(公告)号：US10351783B2

公开(公告)日：2019-07-16

申请号：US15712082

申请日：2017-09-21

申请人： Anellotech, Inc.

发明人： Michael Tanzio ,  Charles M. Sorensen, Jr. ,  Marc E. Schneidkraut ,  Jeffrey P. Whiting

IPC分类号： C07C37/70 ,  C10G7/00 ,  C07D209/08 ,  C07D307/79 ,  C07C209/86 ,  C10K1/08 ,  C10L1/02 ,  C10L1/04 ,  C10B57/06 ,  C10G1/08 ,  C10G1/10 ,  C10G3/00

摘要： Methods of separating products from the catalytic fast pyrolysis of biomass are described. In a preferred method, a portion of the products from a pyrolysis reactor are recovered and separated using a quench system and solvent contacting system that employs materials produced in the pyrolysis process.

公开(公告)号：US20190192516A1

公开(公告)日：2019-06-27

申请号：US16285996

申请日：2019-02-26

申请人： AUTIFONY THERAPEUTICS LIMITED

发明人： Giuseppe ALVARO ,  Paolo DAMBRUOSO ,  Simona TOMMASI ,  Anne DECOR ,  Charles LARGE ,  Agostino MARASCO

IPC分类号： A61K31/506 ,  C07D317/46 ,  C07D405/14 ,  C07D307/94 ,  A61K31/4439 ,  C07D413/14 ,  C07D413/12 ,  C07D405/12 ,  C07D307/79

CPC分类号： A61K31/506 ,  A61K31/4439 ,  C07D307/79 ,  C07D307/94 ,  C07D317/46 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14

摘要： The disclosure provides compounds of formula (I): said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.

公开(公告)号：US20190119239A1

公开(公告)日：2019-04-25

申请号：US16300303

申请日：2017-02-19

申请人： ZHEJIANG JINGXIN PHARMACEUTICAL CO., LTD.

发明人： Jianrong ZHU ,  Chunyong PENG ,  Hongban ZHONG ,  Xiurong HU

IPC分类号： C07D307/79 ,  B01D9/00

摘要： Crystal forms I and II of tasimelteon. Crystal form I: an X-ray powder diffraction spectrum using CuKα radiation and represented by a 2θ angle has diffraction peaks at least at 7.2°±0.2°, 7.9°±0.2°, 10.6°±0.2°, 14.4°±0.2°, 15.9°±0.2°, 17.3°±0.2°, 21.0°±0.2°, 23.2°±0.2°, and 24.4°±0.2°. Crystal form II: an X-ray powder diffraction spectrum using CuKα radiation and represented by a 2θ angle has diffraction peaks at least at 6.8°±0.2°, 12.1°±0.2°, 12.5°±0.2°, 13.1°±0.2°, 13.6°±0.2°, 13.8°±0.2°, 15.8°±0.2°, 17.0°±0.2°, 18.4°±0.2°, 20.8°±0.2°, 24.2°±0.2°, and 24.4°±0.2°. Crystal forms I and II of tasimelteon have advantages of excellent physicochemical property, good stability and solubility, and simple operation for preparation.

公开(公告)号：US10265316B2

公开(公告)日：2019-04-23

申请号：US15621400

申请日：2017-06-13

申请人： AUTIFONY THERAPEUTICS LIMITED

发明人： Giuseppe Alvaro ,  Paolo Dambruoso ,  Simona Tommasi ,  Anne Decor ,  Charles Large ,  Agostino Marasco

IPC分类号： C07D405/12 ,  A61K31/506 ,  C07D413/12 ,  C07D413/14 ,  C07D307/79 ,  C07D307/94 ,  C07D405/14 ,  C07D317/46 ,  A61K31/4439

摘要： The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.

公开(公告)号：US20190092749A1

公开(公告)日：2019-03-28

申请号：US16034558

申请日：2018-07-13

申请人： Haitao Hu ,  Jia Zhou ,  Zhiqing Liu ,  Xiuzhen Fan

发明人： Haitao Hu ,  Jia Zhou ,  Zhiqing Liu ,  Xiuzhen Fan

IPC分类号： C07D401/12 ,  A61P31/18 ,  C07D417/12 ,  C07D209/12 ,  C07D209/24 ,  C07D307/79

摘要： The invention relates generally to novel EPAC1 activators, such as Formula I and the preparation thereof as well as the use of EPAC1 activators as human immunodeficiency virus (HIV) latency reversal agents (LRAs).

公开(公告)号：US20190031624A1

公开(公告)日：2019-01-31

申请号：US16046696

申请日：2018-07-26

申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY ,  TAXIS PHARMACEUTICALS, INC.

发明人： Edmond J. LaVoie ,  Ajit K. Parhi ,  Yangsheng Sun

IPC分类号： C07D251/08 ,  C07C335/32 ,  C07D213/70 ,  C07D209/08 ,  C07D215/12 ,  C07D307/79 ,  C07D333/54 ,  A61P31/04

摘要： Disclosed herein are compounds of formula I: or a salt thereof and compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods for treating or preventing a bacterial infection in an animal comprising administering to the animal a compound of formula I or a pharmaceutically acceptable salt thereof, alone or in combination with a bacterial efflux pump inhibitor.

公开(公告)号：US20190016671A1

公开(公告)日：2019-01-17

申请号：US16032799

申请日：2018-07-11

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Nadia AHMAD ,  Corey ANDERSON ,  Vijayalaksmi ARUMUGAM ,  Iuliana Luci ASGIAN ,  Joanne Louise CAMP ,  Lev Tyler Dewey FANNING ,  Sara Sabina HADIDA RUAH ,  Dennis HURLEY ,  Yvonne SCHMIDT ,  David SHAW ,  Urvi Jagdishbhai SHETH ,  Stephen Andrew THOMSON

IPC分类号： C07C235/64 ,  C07D213/81 ,  C07D213/89 ,  C07D239/34 ,  C07D317/46 ,  C07D405/12 ,  C07D213/69 ,  C07D213/82 ,  C07D307/79

摘要： Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.

公开(公告)号：US20180361370A1

公开(公告)日：2018-12-20

申请号：US15767862

申请日：2016-10-12

申请人： The University of Chicago

发明人： Wenbin Lin ,  Kuntal Manna ,  Pengfei Ji

IPC分类号： B01J31/16 ,  C07F5/02 ,  C07C5/03 ,  C07C41/20 ,  C07C67/303 ,  C07F7/18 ,  C07F7/08 ,  C07C209/24 ,  C07D207/06 ,  C07D213/127 ,  C07C209/62 ,  C07D307/79 ,  C07D209/08 ,  C07D215/04 ,  C07D333/54 ,  C07F9/50

摘要： Metal-organic framework (MOFs) compositions based on post¬synthetic metalation of secondary building unit (SBU) terminal or bridging OH or OH2 groups with metal precursors or other post-synthetic manipulations are described. The MOFs provide a versatile family of recyclable and reusable single-site solid catalysts for catalyzing a variety of asymmetric organic transformations, including the regioselective boryiation and siiylation of benzyiic C—H bonds, the hydrogenation of aikenes, imines, carbonyls, nitroarenes, and heterocycles, hydroboration, hydrophosphination, and cyclization reactions. The solid catalysts can also be integrated into a flow reactor or a supercritical fluid reactor.