公开(公告)号：US11851428B2

公开(公告)日：2023-12-26

申请号：US17328814

申请日：2021-05-24

申请人： ONO PHARMACEUTICAL CO., LTD. ,  VANDERBILT UNIVERSITY

发明人： Craig W. Lindsley ,  Joshua M. Wieting ,  Kevin M. Mcgowan ,  Jerod S. Denton ,  Kentaro Yashiro ,  Haruto Kurata ,  Yoko Sekioka ,  Takahiro Mori ,  Yuzo Iwaki

IPC分类号： C07D213/36 ,  C07D231/12 ,  C07D249/08 ,  C07D401/04 ,  A61K31/454 ,  C07D471/04 ,  C07C255/57 ,  C07C317/28 ,  C07D209/30 ,  C07D213/89 ,  C07D231/56 ,  C07D235/16 ,  C07D237/24 ,  C07D239/47 ,  C07D249/18 ,  C07D257/04 ,  C07D265/36 ,  C07D271/10 ,  C07D285/14 ,  C07D295/04 ,  C07D513/04

CPC分类号： C07D471/04 ,  C07C255/57 ,  C07C317/28 ,  C07D209/30 ,  C07D213/89 ,  C07D231/56 ,  C07D235/16 ,  C07D237/24 ,  C07D239/47 ,  C07D249/08 ,  C07D249/18 ,  C07D257/04 ,  C07D265/36 ,  C07D271/10 ,  C07D285/14 ,  C07D295/04 ,  C07D401/04 ,  C07D513/04

摘要： Disclosed is a compound of formula (I):






wherein all symbols are defined in the description. Also disclosed are pharmaceutical compositions comprising the compounds, methods of making the compounds, kits comprising the compounds, and methods of using the compounds, compositions and kits for treatment of disorders associated with TREK-1, TREK-2 or both TREK-1 and TREK-2 dysfunction in a mammal.

公开(公告)号：US20230354812A1

公开(公告)日：2023-11-09

申请号：US18010736

申请日：2021-06-16

申请人： Bayer Aktiengesellschaft

发明人： Julie GEIST ,  Cyril MONTAGNE ,  Lionel NICOLAS ,  Tomoki TSUCHIYA ,  Vincent THOMAS ,  Dominique LOQUE

IPC分类号： A01N43/58 ,  A01N43/38 ,  A01N43/88 ,  C07D237/24 ,  C07D209/48 ,  C07D237/14 ,  C07D413/04 ,  C07D403/12 ,  A01P3/00

CPC分类号： A01N43/88 ,  A01N43/38 ,  A01N43/58 ,  A01P3/00 ,  C07D209/48 ,  C07D237/14 ,  C07D237/24 ,  C07D403/12 ,  C07D413/04

摘要： The present invention relates to oxadiazinylpyridazine compounds and the uses thereof for controlling phytopathogenic microorganisms such as phytopathogenic fungi. It also relates to processes and intermediates for preparing these compounds.

公开(公告)号：US20230271946A1

公开(公告)日：2023-08-31

申请号：US18134564

申请日：2023-04-13

申请人： Bristol-Myers Squibb Company

发明人： Ke Chen ,  Joerg Deerberg ,  Dong Lin ,  Michael Dummeldinger ,  Bahar Inankur ,  Sergei Kolotuchin ,  Jun Li ,  Amanda J. Rogers ,  Victor W. Rosso ,  Eric M. Simmons ,  Maxime C.D. Soumeillant ,  Daniel S. Treitler ,  Jianji Wang ,  Bin Zheng ,  Michael J. Smith ,  Neil A. Strotman ,  Steven Tymonko ,  Tamas Benkovics

IPC分类号： C07D403/12 ,  C07C211/09 ,  C07D237/24 ,  C07D249/08

CPC分类号： C07D403/12 ,  C07C211/09 ,  C07D237/24 ,  C07D249/08 ,  C07B2200/13

摘要： The invention relates to an improved process for synthesizing 6-(cyclopropaneamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-5N-(methyl-d3)pyridazine-3-carboxamide of the formula:




Compound I is currently in clinical trials for the treatment of auto-immune and auto-inflammatory diseases such as psoriasis.

公开(公告)号：US20230054449A1

公开(公告)日：2023-02-23

申请号：US17297984

申请日：2019-11-27

申请人： Bayer Aktiengesellschaft ,  Bayer CropScience AG

发明人： Victor CHEN ,  Pierre CRISTAU ,  Jérémy DUFOUR ,  Mazen ES-SAYED ,  Julie GEIST ,  Mathieu GOURGUES ,  Dominique LOQUE ,  Anthony MILLET ,  Daniel RACKL ,  Anne-Sophie REBSTOCK ,  Philippe RINOLFI ,  Yoshitaka SATO ,  Alexander SUDAU ,  Vincent THOMAS ,  Valérie TOQUIN

IPC分类号： A01N43/58 ,  C07D237/24 ,  C07D471/04 ,  A01N43/90 ,  C07D401/04 ,  C07D405/12 ,  C07D401/12 ,  A01P3/00

摘要： The present disclosure relates to pyridazine (thio)amide compounds, processes and intermediates for their preparation as well as the uses thereof for controlling phytopathogenic microorganisms, such as phytopathogenic fungi.

公开(公告)号：US20220356180A1

公开(公告)日：2022-11-10

申请号：US17244938

申请日：2021-04-29

申请人： Bristol-Myers Squibb Company

发明人： Ryan M. Moslin ,  David S. Weinstein ,  Stephen T. Wrobleski ,  John S. Tokarski ,  Amit Kumar ,  Douglas G. Batt ,  Shuqun Lin ,  Chunjian Liu ,  Steven H. Spergel ,  Yanlei Zhang ,  Qingjie Liu

IPC分类号： C07D417/14 ,  C07D403/12 ,  C07D401/14 ,  C07D413/14 ,  C07D401/12 ,  C07D237/24 ,  C07D403/14 ,  C07D413/12 ,  C07D417/12 ,  C07B59/00

摘要： Compounds having the following formula I. or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.

公开(公告)号：US20220298168A1

公开(公告)日：2022-09-22

申请号：US17028778

申请日：2020-09-22

申请人： Yumanity Therapeutics, Inc.

发明人： Bertrand LE BOURDONNEC ,  Matthew LUCAS ,  Kerem OZBOYA ,  Bhaumik PANDYA ,  Daniel TARDIFF ,  Parcharee TIVITMAHAISOON ,  Iwona WRONA

IPC分类号： C07D491/107 ,  C07D237/04 ,  C07D401/12 ,  C07D237/24 ,  C07D213/82 ,  C07D403/12 ,  C07D409/14 ,  C07D487/04 ,  C07D401/14 ,  C07D471/04 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D513/04 ,  C07D417/14 ,  C07D495/04

摘要： The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.

公开(公告)号：US20220288065A1

公开(公告)日：2022-09-15

申请号：US17753138

申请日：2020-08-21

申请人： The Scripps Research Institute

发明人： H. Michael PETRASSI ,  Chenguang YU ,  Jie WANG ,  Arnab K. CHATTERJEE ,  Ana Maria Gamo ALBERO ,  Anil GUPTA ,  Junko TAMIYA ,  Peter G. SCHULTZ ,  Kristen JOHNSON ,  Alan CHU ,  Emily N. CHIN ,  Luke L. LAIRSON

IPC分类号： A61K31/501 ,  A61K39/395 ,  A61K45/06 ,  C07D401/04 ,  C07D403/04 ,  C07D413/14 ,  C07D237/24 ,  C07D213/82 ,  C07D401/14 ,  C07D403/14 ,  C07D417/04 ,  C07D413/04 ,  C07D409/14 ,  C07D498/04 ,  C07D239/28 ,  A61K31/497 ,  A61K31/506 ,  A61K31/50 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/536 ,  A61K31/5365

摘要： The invention provides compounds having STimulator of INterferon Genes (STING) agonistic bioactivity that can be used in the treatment of tumors inpatients afflicted therewith. The compounds are of formula (IA), formula (I), and formula (II): wherein the various substituents are as defined herein. Ring A is a 5- or 6-membered heteroaryl comprising 1, 2, or 3 N atoms, unsubstituted or substituted with 1, 2, or 3 groups as defined herein. Compounds for practice of a method of the invention can be delivered via oral delivery for systemic exposure, as well as delivered intratumorally. Antitumor therapy using a compound of formula (I) can further comprise administration of an effective dose of an immunecheckpoint targeting drug.

公开(公告)号：US11214542B2

公开(公告)日：2022-01-04

申请号：US17024842

申请日：2020-09-18

申请人： CELGENE QUANTICEL RESEARCH, INC.

发明人： Young K. Chen ,  Toufike Kanouni ,  Zhe Nie ,  Jeffrey Alan Stafford ,  James Marvin Veal ,  Michael Brennan Wallace

IPC分类号： C07D213/79 ,  C07D213/74 ,  C07D213/81 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D237/24

摘要： The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

公开(公告)号：US20210198252A1

公开(公告)日：2021-07-01

申请号：US16864891

申请日：2020-05-01

申请人： EPIZYME, INC.

发明人： Megan Alene Cloonan Foley ,  Kevin Wayne KUNTZ ,  James Edward John MILLS ,  Lorna Helen MITCHELL ,  Michael John MUNCHHOF ,  Darren Martin HARVEY

IPC分类号： C07D451/04 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D233/90 ,  C07D401/12 ,  C07D241/26 ,  C07D249/04 ,  C07D261/10 ,  C07D263/34 ,  C07D275/03 ,  C07D209/08 ,  C07D277/56 ,  C07C271/18 ,  C07D205/04 ,  C07D211/34 ,  C07D237/24 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/14

摘要： The present disclosure provides carboxamides and sulfonamides having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, Y, B, X, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of SMYD proteins such a SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.

公开(公告)号：US10899734B2

公开(公告)日：2021-01-26

申请号：US16307473

申请日：2017-06-23

申请人： St. Jude Children's Research Hospital

发明人： Lalit Kumar Sharma ,  Richard E. Lee ,  Charles O. Rock ,  Suzanne Jackowski ,  Mi Kyung Yun ,  Chitra Subramanian ,  Jiuyu Liu

IPC分类号： C07D241/04 ,  C07D237/24 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D401/04 ,  C07D401/14 ,  A61K31/501 ,  A61P3/10 ,  A61P25/00 ,  C07D409/14 ,  C07D413/14 ,  C07D409/12 ,  C07D401/12 ,  C07D213/85

摘要： The present disclosure relates to chemical compounds that modulate pantothenate kinase (PanK) activity for the treatment of metabolic disorders (such as diabetes mellitus type II), neurologic disorders (such as pantothenate kinase-associated neurodegeneration), pharmaceutical compositions containing such compounds, and their use in treatment. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.