公开(公告)号：US20240174605A1

公开(公告)日：2024-05-30

申请号：US18279985

申请日：2022-03-01

申请人： RESEARCH TRIANGLE INSTITUTE

发明人： Yanan ZHANG ,  Dehui ZHANG

IPC分类号： C07C311/37 ,  A61K31/167 ,  A61K31/18 ,  A61K31/381 ,  A61K31/40 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4453 ,  A61K31/4545 ,  A61K31/496 ,  A61P25/28 ,  C07C237/42 ,  C07D213/40 ,  C07D213/75 ,  C07D213/76 ,  C07D213/81 ,  C07D213/82 ,  C07D277/56 ,  C07D295/16 ,  C07D333/38 ,  C07D401/12 ,  C07D417/12

CPC分类号： C07C311/37 ,  A61K31/167 ,  A61K31/18 ,  A61K31/381 ,  A61K31/40 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4453 ,  A61K31/4545 ,  A61K31/496 ,  A61P25/28 ,  C07C237/42 ,  C07D213/40 ,  C07D213/75 ,  C07D213/76 ,  C07D213/81 ,  C07D213/82 ,  C07D277/56 ,  C07D295/16 ,  C07D333/38 ,  C07D401/12 ,  C07D417/12 ,  C07C2601/02

摘要： The present disclosure provides novel arylsulfonamide compounds as embodiments of the present disclosure. The compounds are believed to be orexin receptor agonists, useful for the treatment of diseases and conditions caused by reduced activity of orexin.

公开(公告)号：US20240043443A1

公开(公告)日：2024-02-08

申请号：US18228452

申请日：2023-07-31

申请人： CASE WESTERN RESERVE UNIVERSITY ,  BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM ,  UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION

发明人： Sanford Markowitz ,  James K.V. Willson ,  Bruce Posner ,  Joseph Ready ,  Yongyou Zhang ,  Hsin-Hsiung Tai ,  Monica Antczak ,  Stanton Gerson ,  KiBeom Bae ,  Sung Yeun Yang ,  Amar Desai

IPC分类号： C07D495/04 ,  C07C311/21 ,  C07D213/71 ,  C07D213/73 ,  C07D213/75 ,  C07D213/76 ,  C07D215/08 ,  C07D237/20 ,  C07D405/12 ,  C07D239/42 ,  C07D241/20 ,  C07D261/14 ,  C07D207/263 ,  C07D275/03 ,  C07D209/08 ,  C07D277/46 ,  C07D295/185 ,  A61K31/4365 ,  A61K31/519

CPC分类号： C07D495/04 ,  C07C311/21 ,  C07D213/71 ,  C07D213/73 ,  C07D213/75 ,  C07D213/76 ,  C07D215/08 ,  C07D237/20 ,  C07D405/12 ,  C07D239/42 ,  C07D241/20 ,  C07D261/14 ,  C07D207/263 ,  C07D275/03 ,  C07D209/08 ,  C07D277/46 ,  C07D295/185 ,  A61K31/4365 ,  A61K31/519 ,  C07C2601/14

摘要： Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.

公开(公告)号：US20230373939A1

公开(公告)日：2023-11-23

申请号：US18030519

申请日：2021-10-06

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Jason MCCARTNEY ,  Sunny ABRAHAM ,  Corey Don ANDERSON ,  Vijayalaksmi ARUMUGAM ,  Jaclyn CHAU ,  Thomas CLEVELAND ,  Timothy A. DWIGHT ,  Bryan A. FRIEMAN ,  Peter GROOTENHUIS ,  Sara Sabina HADIDA RUAH ,  Yoshihiro ISHIHARA ,  Mark Thomas MILLER ,  Alina SILINA ,  Jinglan ZHOU

IPC分类号： C07D279/06 ,  C07D241/22 ,  C07D251/24 ,  C07D239/69 ,  C07D403/04 ,  C07D213/76 ,  C07D401/14 ,  C07D401/12 ,  A61K45/06

CPC分类号： C07D279/06 ,  C07D241/22 ,  C07D251/24 ,  C07D239/69 ,  C07D403/04 ,  C07D213/76 ,  C07D401/14 ,  C07D401/12 ,  A61K45/06 ,  C07B2200/05

摘要： This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) having the structure: (I), pharmaceutical compositions containing at least one such modulator, methods of treatment of cystic fibrosis using such modulators and pharmaceutical compositions, combination therapies, and processes and intermediates for making such modulators.

公开(公告)号：US20190016670A1

公开(公告)日：2019-01-17

申请号：US16133297

申请日：2018-09-17

申请人： Ming-Yu Ngai ,  Katarzyna N. Hojczyk

发明人： Ming-Yu Ngai ,  Katarzyna N. Hojczyk

IPC分类号： C07C233/25 ,  C07D209/08 ,  C07J43/00 ,  C07D473/40 ,  C07D239/91 ,  C07D239/47 ,  C07D405/04 ,  C07D347/00 ,  C07D213/76 ,  C07D213/75 ,  C07C255/60 ,  C07C233/54 ,  C07C233/80 ,  C07C231/12 ,  C07C233/33 ,  C07C233/81 ,  C07D263/57 ,  C07D215/40 ,  C07D401/04 ,  C07D417/04 ,  C07D471/04 ,  C07C259/06 ,  C07C259/10 ,  C07C269/06 ,  C07C273/18 ,  C07C231/14 ,  C07C253/30 ,  C07C275/64 ,  C07C271/38 ,  C07C255/58 ,  C07C275/34

CPC分类号： C07C233/25 ,  C07C231/12 ,  C07C231/14 ,  C07C233/33 ,  C07C233/54 ,  C07C233/80 ,  C07C233/81 ,  C07C253/30 ,  C07C255/58 ,  C07C255/60 ,  C07C259/06 ,  C07C259/10 ,  C07C269/06 ,  C07C271/38 ,  C07C273/1809 ,  C07C273/1854 ,  C07C275/34 ,  C07D209/08 ,  C07D213/75 ,  C07D213/76 ,  C07D215/40 ,  C07D239/47 ,  C07D239/91 ,  C07D263/57 ,  C07D347/00 ,  C07D401/04 ,  C07D405/04 ,  C07D417/04 ,  C07D471/04 ,  C07D473/40 ,  C07J43/003 ,  C07C275/64

摘要： The present invention provides a process of producing a trifluoromethoxylated aryl or trifluoromethoxylated heteroaryl having the structure: wherein A is an aryl or heteroaryl, each with or without subsutitution; and R1 is —H, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(alkylaryl), -(alkylheteroaryl), —NH-(alkyl), —N(alkyl)2, —NH-(alkenyl), —NH-(alkynyl) —NH-(aryl), —NH-(heteroaryl), —O-(alkyl), —O-(alkenyl), —O-(alkynyl), —O-(aryl), —O-(heteroaryl); —S-(alkyl), —S-(alkenyl), —S-(alkynyl), —S-(aryl), or —S-(heteroaryl), comprising: (a) reacting a compound having the structure: with a trifluoromethylating agent in the presence of a base in a first suitable solvent under conditions to produce a compound having the structure: and (b) maintaining the compound produced in step (a) in a second suitable solvent under conditions sufficient to produce the trifluoromethoxylated aryl or trifluormethoxylated heteroaryl having the structure:

公开(公告)号：US09938236B2

公开(公告)日：2018-04-10

申请号：US14759385

申请日：2013-12-27

申请人： DREXEL UNIVERSITY ,  BARUCH S. BLUMBERG INSTITUTE ,  ARBUTUS BIOPHARMA, INC.

发明人： Xiaodong Xu ,  Ju-Tao Guo ,  Tong Xiao ,  Yanming Du ,  Timothy Block ,  Simon David Peter Baugh ,  Hong Ye

IPC分类号： C07C311/16 ,  C07D213/75 ,  C07D213/76 ,  C07D309/04 ,  C07D215/38 ,  C07D215/42 ,  C07D217/24 ,  C07D319/18 ,  C07D231/40 ,  C07D231/42 ,  C07D239/26 ,  C07D261/14 ,  C07D263/48 ,  C07D263/50 ,  C07D203/26 ,  C07D263/58 ,  C07D205/04 ,  C07D277/46 ,  C07D277/52 ,  C07D211/96 ,  C07D295/26 ,  C07D295/30 ,  C07D213/40 ,  C07D305/08 ,  C07C309/89 ,  C07C311/17 ,  C07C311/18 ,  C07C311/19 ,  C07C311/20 ,  C07C311/48 ,  C07C233/66 ,  C07C317/14 ,  C07D295/32 ,  C07D319/16

CPC分类号： C07C311/16 ,  C07B2200/07 ,  C07C233/66 ,  C07C309/89 ,  C07C311/17 ,  C07C311/18 ,  C07C311/19 ,  C07C311/20 ,  C07C311/48 ,  C07C317/14 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D203/26 ,  C07D205/04 ,  C07D211/96 ,  C07D213/40 ,  C07D213/75 ,  C07D213/76 ,  C07D215/38 ,  C07D215/42 ,  C07D217/24 ,  C07D231/40 ,  C07D231/42 ,  C07D239/26 ,  C07D261/14 ,  C07D263/48 ,  C07D263/50 ,  C07D263/58 ,  C07D277/46 ,  C07D277/52 ,  C07D295/26 ,  C07D295/30 ,  C07D295/32 ,  C07D305/08 ,  C07D309/04 ,  C07D319/16 ,  C07D319/18

摘要： The present invention provides novel compounds of formula (I) and methods of use thereof. In certain embodiments, the compounds of the invention are useful as nucleocapsid assembly inhibitors. In other embodiments, the compounds of the invention are useful as pregenomic RNA encapsidation inhibitors of Hepatitis B virus (HBV). In yet other embodiments, the compounds of the invention are useful for the treatment of viral infection, including HBV and related viral infections.

公开(公告)号：US20180071289A1

公开(公告)日：2018-03-15

申请号：US15658211

申请日：2017-07-24

申请人： Motonari UESUGI ,  Salih J. WAKIL ,  Lutfi ABU-ELHEIGA ,  Mizuki WATANABE

发明人： Motonari UESUGI ,  Salih J. WAKIL ,  Lutfi ABU-ELHEIGA ,  Mizuki WATANABE

IPC分类号： A61K31/5025 ,  C07D213/06 ,  A61K31/426 ,  C07D417/14 ,  C07D417/04 ,  C07D487/04 ,  C07D277/24 ,  A61K31/4709 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  C07D213/76 ,  C07D235/14 ,  C07D417/12 ,  C07D277/22 ,  C07D213/16 ,  A61K31/437 ,  A61K31/427 ,  A61K31/428 ,  C07D471/04 ,  C07D277/66

CPC分类号： A61K31/5025 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  C07D213/06 ,  C07D213/16 ,  C07D213/76 ,  C07D235/14 ,  C07D277/22 ,  C07D277/24 ,  C07D277/66 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： The present invention relates to methods of treating a disease related to cell hyper-proliferation via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently.

公开(公告)号：US09890117B2

公开(公告)日：2018-02-13

申请号：US15187163

申请日：2016-06-20

申请人： Northwestern University ,  The General Hospital Corporation

发明人： Richard B. Silverman ,  Hua Wang ,  Mohammad Khanfar ,  Aleksey G. Kazantsev

IPC分类号： C07C311/21 ,  C07C311/16 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D213/85 ,  C07D217/04 ,  C07D207/16 ,  C07C317/44 ,  C07C323/49 ,  C07C323/42 ,  C07C257/18 ,  C07C255/60 ,  C07D295/26 ,  C07D305/06 ,  C07C311/29 ,  C07D213/76 ,  C07D213/80 ,  C07D223/04 ,  C07D237/20 ,  C07D239/42 ,  C07D261/14 ,  C07D271/113 ,  C07D277/46 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C323/62 ,  C07C311/47 ,  C07C317/22 ,  C07C317/34 ,  C07C323/20 ,  C07C235/60

CPC分类号： C07C311/21 ,  C07B2200/07 ,  C07C235/60 ,  C07C255/60 ,  C07C257/18 ,  C07C311/16 ,  C07C311/29 ,  C07C311/46 ,  C07C311/47 ,  C07C317/22 ,  C07C317/34 ,  C07C317/40 ,  C07C317/44 ,  C07C317/48 ,  C07C323/20 ,  C07C323/42 ,  C07C323/49 ,  C07C323/62 ,  C07C2601/02 ,  C07D207/16 ,  C07D213/75 ,  C07D213/76 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D213/85 ,  C07D217/04 ,  C07D223/04 ,  C07D237/20 ,  C07D239/42 ,  C07D261/14 ,  C07D271/113 ,  C07D277/46 ,  C07D295/26 ,  C07D305/06 ,  C07D311/16 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

摘要： Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.

公开(公告)号：US09867813B2

公开(公告)日：2018-01-16

申请号：US15352848

申请日：2016-11-16

申请人： Thomas Daly

发明人： Thomas Daly

IPC分类号： A61K31/437 ,  A61K31/444 ,  C07D401/12

CPC分类号： A61K31/444 ,  A61K31/437 ,  C07D213/76 ,  C07D401/12 ,  C07D513/04

摘要： Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. Aminopyridines channel blocking, combined with buffering and zwitterionic charge states make promising therapies for myelin diseases and as antibiotics.

公开(公告)号：US20170290337A1

公开(公告)日：2017-10-12

申请号：US15514048

申请日：2014-09-18

申请人： SYNGENTA PARTICIPATIONS AG

发明人： Neil Brian CARTER ,  Derek MCCORMACK ,  Anne Mary SEVILLE ,  Matthew John WEBBER ,  Matthew Murdoch MCLACHLAN ,  Alison Clare ELLIOTT

IPC分类号： A01N43/78 ,  C07D213/76 ,  C07D277/44 ,  A01N47/18 ,  A01N47/36

CPC分类号： A01N43/78 ,  A01N47/18 ,  A01N47/36 ,  C07D213/76 ,  C07D277/44

摘要： The present invention relates to herbicidally active pyridino-/pyrimidino-thiazole derivatives, as well as to processes and intermediates used for the preparation of such derivatives. The invention further extends to herbicidal compositions comprising such derivatives, as well as to the use of such compounds and compositions in controlling undesirable plant growth: in particular the use in controlling weeds, in crops of useful plants.

公开(公告)号：US20170165241A1

公开(公告)日：2017-06-15

申请号：US15359330

申请日：2016-11-22

申请人： CASE WESTERN RESERVE UNIVERSITY ,  Board of Regents of the University of Texas System ,  University of Kentucky Research Foundation

发明人： Sanford Markowitz ,  James K.V. Willson ,  Bruce Posner ,  Joseph Ready ,  Youngyou Zhang ,  Hsin-Hsiung Tai ,  Melissa Moss ,  Monika Antczak ,  Stanton Gerson ,  KiBeom Bae ,  Sung Yeun Yang ,  Amar Desai

IPC分类号： A61K31/4365 ,  A61K31/519

CPC分类号： C07D495/04 ,  A61K31/4365 ,  A61K31/519 ,  C07C311/21 ,  C07C2601/14 ,  C07D207/263 ,  C07D209/08 ,  C07D213/71 ,  C07D213/73 ,  C07D213/75 ,  C07D213/76 ,  C07D215/08 ,  C07D237/20 ,  C07D239/42 ,  C07D241/20 ,  C07D261/14 ,  C07D275/03 ,  C07D277/46 ,  C07D295/185 ,  C07D405/12

摘要： Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.