公开(公告)号：US11278530B2

公开(公告)日：2022-03-22

申请号：US16755864

申请日：2018-10-26

申请人： SUVEN LIFE SCIENCES LIMITED

发明人： Ramakrishna Nirogi ,  Abdul Rasheed Mohammed ,  Anil Karbhari Shinde ,  Shankar Reddy Gagginapally ,  Durga Malleshwari Kancharla ,  Santosh Kumar Pandey ,  Renny Abraham ,  Venkateswarlu Jasti

IPC分类号： A61K31/437 ,  A61P25/28 ,  A61K31/13 ,  A61K31/27 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/427 ,  A61K31/445 ,  A61K31/4709 ,  A61K31/473 ,  A61K31/538 ,  A61K31/55 ,  C07D215/48 ,  C07D235/04 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D405/14 ,  C07D413/10 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04

摘要： The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers or pharmaceutically acceptable salt (s) thereof as muscarinic M1 receptor positive allosteric modulators (M1 PAMs). The present invention describes the preparation, pharmaceutical composition and the use of compound formula (I).

公开(公告)号：US20210140972A1

公开(公告)日：2021-05-13

申请号：US17072665

申请日：2020-10-16

申请人： UCB BIOPHARMA SRL

发明人： James Philip O'CONNELL ,  John Robert PORTER ,  Alastair LAWSON ,  Boris KROEPLIEN ,  Stephen Edward RAPECKI ,  Timothy John NORMAN ,  David James MCMILLAN ,  Graham John WARRELLOW ,  Daniel Christopher BROOKINGS ,  Rikki Peter ALEXANDER

IPC分类号： G01N33/68 ,  C07D401/14 ,  C07K14/525 ,  C07D471/00 ,  C07K14/705 ,  C07K16/24 ,  C07D213/72 ,  C07D235/04 ,  C07D239/26 ,  C07D471/04 ,  A61K47/64 ,  A61P37/00 ,  A61P35/00

摘要： The invention is in the field of TNF signalling. Compounds have been identified which are capable of modulating signalling of TNF trimers through receptors. Methods of identifying such compounds are therefore provided. The compounds themselves have utility in therapy.

公开(公告)号：US10969393B2

公开(公告)日：2021-04-06

申请号：US15736535

申请日：2015-10-22

申请人： UCB Biopharma SRL

发明人： James Philip O'Connell ,  John Robert Porter ,  Alastair Lawson ,  Daniel John Lightwood ,  Rebecca Jayne Munro

IPC分类号： C07D401/14 ,  C07K14/525 ,  C07D471/00 ,  C07K14/705 ,  C07K16/24 ,  C07D213/72 ,  C07D235/04 ,  C07D239/26 ,  C07D471/04 ,  A61K47/64 ,  A61P37/00 ,  A61P35/00 ,  G01N33/68

摘要： It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Antibodies which selectively bind to complexes of such compounds with TNF superfamily members are disclosed. These antibodies may be used to detect further compounds with the same activity, and as target engagement biomarker.

公开(公告)号：US20210088530A1

公开(公告)日：2021-03-25

申请号：US17013326

申请日：2020-09-04

申请人： UCB BIOPHARMA SRL

发明人： James Philip O'CONNELL ,  John Robert PORTER ,  Alastair LAWSON ,  Boris KROEPLIEN ,  Stephen Edward RAPECKI ,  Timothy John NORMAN ,  Graham John WARRELLOW ,  Tracy Lynn ARAKAKI ,  Alex Buntin BURGIN ,  William Ross PITT ,  Mark Daniel CALMIANO ,  David Andreas SCHUBERT ,  Daniel John LIGHTWOOD ,  Rebecca Jayne MUNRO

IPC分类号： G01N33/68 ,  C07D401/14 ,  C07K14/525 ,  C07D471/00 ,  C07K14/705 ,  C07K16/24 ,  C07D213/72 ,  C07D235/04 ,  C07D239/26 ,  C07D471/04 ,  A61K47/64 ,  A61P37/00 ,  A61P35/00

摘要： A new, stable trimeric TNFα structure is disclosed with distorted symmetry which can bind to the TNFR1 receptor to attenuate signalling therefrom, which can be used in the treatment and/or prevention of diseases associated with the soluble TNFα/TNFR1 interaction. Membrane-bound TNFα is not affected in its ability to signal through TNFR2, and thus the new structure of TNFα may be used in therapies which do not significantly raise the risk of infection or malignancy.

公开(公告)号：US10669268B2

公开(公告)日：2020-06-02

申请号：US15583679

申请日：2017-05-01

申请人： Hoffmann-La Roche Inc.

发明人： Jerome Hert ,  Daniel Hunziker ,  Patrizio Mattei ,  Harald Mauser ,  Guozhi Tang ,  Lisha Wang

IPC分类号： C07D231/56 ,  C07D235/04 ,  C07D471/04 ,  C07D519/00 ,  C07D413/12 ,  C07D403/12 ,  C07D487/04

摘要： The invention provides novel compounds having the general formula (I) wherein R1, Y, A, W, R2, m, n, p and q are as described herein, compositions including the compounds and methods of using the compounds.

公开(公告)号：US10662174B2

公开(公告)日：2020-05-26

申请号：US15650295

申请日：2017-07-14

申请人： Hubei Bio-Pharmaceutical Industrial Technological Institute Inc. ,  Humanwell Healthcare (Group) Co., Ltd.

发明人： Xuehai Wang ,  Chengde Wu ,  Yong Xu ,  Chunli Shen ,  Li'e Li ,  Guoping Hu ,  Yang Yue ,  Jian Li ,  Diliang Guo ,  Nengyang Shi ,  Lu Huang ,  Shuhui Chen ,  Ronghua Tu ,  Zhongwen Yang ,  Xuwen Zhang ,  Qiang Xiao ,  Hua Tian ,  Yanping Yu ,  Hailiang Chen ,  Wenjie Sun ,  Zhenyu He ,  Jie Shen ,  Jing Yang ,  Jing Tang ,  Wen Zhou ,  Jing Yu ,  Yi Zhang ,  Quan Liu

IPC分类号： C07D487/04 ,  A61K31/5025 ,  C07D401/14 ,  C07D471/04 ,  A61K31/505 ,  C07D401/04 ,  A61K31/506 ,  C07D239/48 ,  C07D239/04 ,  C07D213/74 ,  C07D213/73 ,  C07D401/12 ,  C07D235/04 ,  A61K31/5383 ,  A61K31/496 ,  C07D231/54 ,  C07D251/12 ,  C07D403/02 ,  C07D473/32 ,  C07D498/02 ,  A61K31/366 ,  A61K31/52 ,  C07C13/04

摘要： Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug thereof represented by formula (I), (II), (III) or (IV).

公开(公告)号：US10538507B2

公开(公告)日：2020-01-21

申请号：US16301769

申请日：2017-05-24

申请人： ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD ,  ZHEJIANG HUAHAI ZHICHENG PHARMACEUTICAL CO., LTD.

发明人： Lingjie Chen ,  Wenling Zhang ,  Peng Wang

IPC分类号： C07D235/04 ,  C07D401/12 ,  B01D9/00

摘要： Provided is a purifying method for dabigatran etexilate free base, comprising subjecting a dabigatran etexilate free base crude product to water slurrying to obtain a crude product B; then conducting recrystallization on the crude product B with acetone and water to obtain a crude product C; and subsequently, purifying the crude product C with a mixed solvent of tetrahydrofuran and ethyl acetate, filtering and drying to obtain a dabigatran etexilate free base finished product. The purifying method of the present invention can effectively remove various impurities and is suitable for workshop production. Salts and water-soluble organic impurities are removed by purified water slurrying, impurities with a high polarity are removed by purifying with an acetone-water solution, and impurities with a low polarity are removed by purifying with a mixed solvent of tetrahydrofuran and ethyl acetate.

公开(公告)号：US10513523B2

公开(公告)日：2019-12-24

申请号：US15569273

申请日：2016-04-28

申请人： Janssen Pharmaceutica NV

发明人： Michael K. Ameriks ,  Bradley M. Savall ,  Devin M. Swanson ,  Dongpei Wu

IPC分类号： C07D487/04 ,  A61P25/00 ,  C07D231/54 ,  C07D235/04 ,  C07D239/80 ,  C07D249/18 ,  C07D275/06 ,  C07D277/62

摘要： Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, Also provided herein are pharmaceutical compositions, comprising compounds of Formula (I), and methods of using compounds of Formula (I).

公开(公告)号：US10256427B2

公开(公告)日：2019-04-09

申请号：US14253811

申请日：2014-04-15

申请人： Universal Display Corporation

发明人： Vadim Adamovich ,  James Esler ,  Jason Brooks ,  Michael S. Weaver ,  Julia J. Brown

IPC分类号： C09K11/06 ,  H05B33/14 ,  H01L51/50 ,  C07D213/02 ,  C07D401/04 ,  C07D233/54 ,  C07D235/04 ,  H01L51/00

摘要： An OLED device includes, in order, an electron blocking layer, an organic emissive layer, and a hole blocking layer. Its organic emissive layer contains at least four components: an electron transporting compound, a host, a hole transporting compound, and an emitting compound capable of phosphorescence emission at room temperature. The emitting compound has HOMO energy level of 5.2 eV or lower and a LUMO energy level of 2.5 eV or higher.

公开(公告)号：US10172840B2

公开(公告)日：2019-01-08

申请号：US15584459

申请日：2017-05-02

申请人： vTv Therapeutics LLC

发明人： Otis Clinton Attucks

IPC分类号： C07D235/04 ,  A61K31/437 ,  A61K31/428 ,  A61K31/56

摘要： The disclosure provides pharmaceutical compositions comprising Bach1 Inhibitors and Nrf2 Activators. The disclosure also provides methods of treating diseases such as psoriasis, multiple sclerosis, and COPD comprising administering a Bach1 Inhibitor and a Nrf2 Activator to a subject in need thereof.