公开(公告)号：US20210402380A1

公开(公告)日：2021-12-30

申请号：US17350431

申请日：2021-06-17

申请人： San Diego State University Foundation

发明人： Yong YAN

IPC分类号： B01J27/135 ,  B01J31/12 ,  B01J31/30 ,  B01J27/128 ,  B01J35/00 ,  B01J35/02 ,  B01J19/12 ,  C07C45/72 ,  C07D217/16 ,  C07D498/04 ,  C07D231/12 ,  C07D207/34 ,  C07C67/10 ,  C07D217/12 ,  C07D413/12 ,  C07D211/94 ,  C07D405/04 ,  C07D211/90

摘要： Nature is capable of storing solar energy in chemical bonds via photosynthesis through a series of C—C, C—O and C—N bond-forming reactions starting from CO2 and light. Direct capture of solar energy for organic synthesis is a promising approach. Lead (Pb)-halide perovskite solar cells reach 24.2% power conversion efficiency, rendering perovskite a unique type material for solar energy capture. We show that photophysical properties of perovskites is useful in photoredox organic synthesis. Because the key aspects of these two applications are both relying on charge separation and transfer. Here we demonstrated that perovskites nanocrystals are exceptional candidates as photocatalysts for fundamental organic reactions, i.e. C—C, C—N and C—O bond-formations. Stability of CsPbBr3 in organic solvents and ease-of-tuning their bandedges garner perovskite a wider scope of organic substrate activations.

公开(公告)号：US20210308121A1

公开(公告)日：2021-10-07

申请号：US17189989

申请日：2021-03-02

申请人： Epizyme, Inc.

发明人： Kenneth W. Duncan ,  Richard Chesworth ,  Paula Ann Boriack-Sjodin ,  Michael John Munchhof ,  Lei Jin

IPC分类号： A61K31/4725 ,  C07D401/14 ,  C07D217/12 ,  C07D401/12 ,  C07D405/12 ,  C07D217/04 ,  C07D405/14 ,  C07D413/12 ,  A61K31/506 ,  C12N9/10 ,  A61P7/06 ,  A61P3/04 ,  A61P3/10 ,  A61P35/00 ,  A61K31/496 ,  A61K31/498 ,  A61K31/5377 ,  A61K31/538

摘要： Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.

公开(公告)号：US10702517B2

公开(公告)日：2020-07-07

申请号：US15788741

申请日：2017-10-19

申请人： Celgene Quanticel Research, Inc.

发明人： Juan Manuel Betancort ,  Jeffrey Alan Stafford ,  Ryan Stansfield ,  James Marvin Veal

IPC分类号： A61K31/472 ,  A61K47/32 ,  A61K47/38 ,  A61K9/10 ,  A61K9/16 ,  A61K9/20 ,  C07D217/12 ,  C07D217/24

摘要： Described herein is the bromodomain inhibitor 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one, including crystalline forms, amorphous forms, solvates, and hydrates thereof, as well as pharmaceutical compositions that include this bromodomain inhibitor. In some embodiments, the pharmaceutical composition comprises 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one that has been processed by micronization or spray dried dispersion. In some embodiments, the pharmaceutical composition further comprises at least one polymer. In some embodiments, the pharmaceutical composition comprises a solid polymer matrix comprising 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one and at least one polymer. Pharmaceutical compositions comprising 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one are useful for the treatment of cancer or neoplastic disease.

公开(公告)号：US10696635B2

公开(公告)日：2020-06-30

申请号：US16094707

申请日：2017-04-18

申请人： The Scripps Research Institute

发明人： Jin-Quan Yu

IPC分类号： C07C6/02 ,  C07D213/68 ,  C07D401/14 ,  C07D405/14 ,  C07D231/12 ,  C07D231/56 ,  C07D401/12 ,  C07D405/12 ,  C07D239/42 ,  C07D409/12 ,  C07D409/14 ,  C07D241/12 ,  C07D413/12 ,  C07D217/12 ,  C07D213/36 ,  C07D213/26 ,  B01J23/44 ,  C07D213/30 ,  C07D213/40 ,  C07D213/55 ,  C07D213/72 ,  C07D215/38 ,  C07D217/18 ,  C07D217/24 ,  C07D239/26

摘要： A class of mono-protected 3-amino-2-hydroxypyridine (MPAHP) ligands that enable the meta-C—H arylation of anilines, phenols, phenylacetic acids, and biologically relevant heterocyclic compounds using norbornene as a transient mediator is disclosed, such as in the formation of a reaction product of Formula IA: The applicability of this meta-arylation methodology in the pharmaceutical industry is illustrated for heteroaryl substrates and heteroaryl iodide coupling partners, a feat made possible by using the MPAHP ligand. The enabling nature of MPAHP ligands to achieve other meta-C—H functionalization processes is also illustrated by the development of a meta-C—H amination reaction and a meta-C—H alkynylation reaction.

公开(公告)号：US20180282281A1

公开(公告)日：2018-10-04

申请号：US15524396

申请日：2015-11-05

申请人： FLEXUS BIOSCIENCES, INC.

发明人： Hilary Plake BECK ,  Juan Carios JAEN ,  Maksim OSIPOV ,  Jay Patrick POWERS ,  Maureen Kay REILLY ,  Hunter Paul SHUNATONA ,  James Ross WALKER ,  Mikhail ZIBINSKY ,  James Aaron BALOG ,  David K. WILLIAMS ,  Jay A. MARKWALDER ,  Emily Charlotte CHERNEY ,  Welfang SHAN ,  Audris HUANG

IPC分类号： C07D215/12 ,  C07D215/233 ,  C07D217/12 ,  C07D217/24 ,  C07D231/56 ,  C07D239/74 ,  C07D401/12 ,  C07D471/04 ,  C07D487/04 ,  A61P35/02

摘要： Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

公开(公告)号：US20180098987A1

公开(公告)日：2018-04-12

申请号：US15586775

申请日：2017-05-04

申请人： Epizyme, Inc.

发明人： Kenneth W. Duncan ,  Richard Chesworth ,  Paula Ann Boriack-Sjodin ,  Michael John Munchhof ,  Lei Jin

IPC分类号： A61K31/506 ,  C12N9/10 ,  C07D217/04 ,  C07D217/12 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12

摘要： Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.

公开(公告)号：US09604930B2

公开(公告)日：2017-03-28

申请号：US14654253

申请日：2013-12-20

申请人： Epizyme, Inc.

发明人： Kenneth W. Duncan ,  Richard Chesworth ,  Paula Ann Boriack-Sjodin ,  Michael John Munchhof ,  Lei Jin

IPC分类号： A61K31/00 ,  C07D217/04 ,  C07D401/14 ,  C07D217/12 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12

CPC分类号： A61K31/506 ,  C07D217/04 ,  C07D217/12 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C12N9/1007

摘要： Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5 mediated disorders are also described.

公开(公告)号：US08367832B2

公开(公告)日：2013-02-05

申请号：US11791557

申请日：2004-08-23

申请人： Chava Satyanarayana ,  Vasireddy Umamaheswara-Rao ,  Vellanki Siva Ram Prasad ,  Balusu Rajababu

发明人： Chava Satyanarayana ,  Vasireddy Umamaheswara-Rao ,  Vellanki Siva Ram Prasad ,  Balusu Rajababu

IPC分类号： C07D217/12

CPC分类号： C07D217/26

摘要： The present invention provides novel crystalline forms of Nelfinavir mesylate, Form-A, Form-B, Form-C, Form-D and the process for their preparation without the use of any special equipment such as a spray drier, avoiding the use of highly flammable solvents such as ethers. The crystalline form can be tailored with the selection of the ante solvent and appropriate conditions for the process.

摘要翻译： 本发明提供奈非那韦甲状结晶形式A，形式B，形式C，形式D的新型结晶形式及其制备方法，而不使用任何特殊设备如喷雾干燥器，避免使用高度 易燃溶剂如醚。 可以通过选择前体溶剂和适合该方法的条件来调整结晶形式。

公开(公告)号：US07868003B2

公开(公告)日：2011-01-11

申请号：US11776041

申请日：2007-07-11

申请人： Uwe Heinelt ,  Hans-Jochen Lang ,  Klaus Wirth ,  Thomas Licher ,  Armin Hofmeister

发明人： Uwe Heinelt ,  Hans-Jochen Lang ,  Klaus Wirth ,  Thomas Licher ,  Armin Hofmeister

IPC分类号： C07D217/12 ,  A61K31/47

CPC分类号： C07D401/10 ,  C07D217/18

摘要： The invention relates to substituted 4-phenyltetrahydroisoquinolines of formula I wherein R1-R8, N, W, X and Z are defined herein. These compounds and pharmaceutical compositions comprising them are useful in the treatment of respiratory disorders, sleep apnea, kidney disorders, high blood pressure, hypertension, disorders of the central nervous system and the like.

摘要翻译： 本发明涉及式I的取代的4-苯基四氢异喹啉，其中R1-R8，N，W，X和Z如本文所定义。 这些化合物和包含它们的药物组合物可用于治疗呼吸障碍，睡眠呼吸暂停，肾脏疾病，高血压，高血压，中枢神经系统疾病等。

公开(公告)号：US20100298374A1

公开(公告)日：2010-11-25

申请号：US12780132

申请日：2010-05-14

申请人： Krishna MENON

发明人： Krishna MENON

IPC分类号： A61K31/275 ,  C07C257/10 ,  A61K31/277 ,  C07D213/59 ,  A61K31/44 ,  C07D215/16 ,  C07D217/12 ,  A61K31/472 ,  A61K31/47 ,  A61K31/4375 ,  C07D471/04 ,  A61P35/00 ,  A61P31/12 ,  A61P31/04 ,  A61P29/00

CPC分类号： C07C255/03 ,  A61K31/275 ,  A61K31/277 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/47 ,  A61K31/472 ,  C07C335/32 ,  C07C335/34 ,  C07C335/36 ,  C07C2601/02 ,  C07C2601/04 ,  C07D213/57 ,  C07D215/12 ,  C07D217/02 ,  C07D471/04

摘要： Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I and the pharmaceutically acceptable salts of such compounds. Also disclosed are processes for the preparation of such compounds, intermediates used in the preparation of such compounds, and the uses of such compounds in treating hyperproliferative diseases, inflammatory diseases and viral and bacterial infections and inducing apoptosis in cancer cells.

摘要翻译： 公开了腈衍生物和包含腈衍生物的药物组合物。 药物组合物包含式I化合物和这些化合物的药学上可接受的盐。 还公开了制备这些化合物的方法，用于制备这些化合物的中间体，以及这些化合物在治疗过度增殖性疾病，炎性疾病和病毒和细菌感染中的用途以及诱导癌细胞凋亡。