公开(公告)号：US20240360096A1

公开(公告)日：2024-10-31

申请号：US18553525

申请日：2022-04-01

申请人： LYGOS, INC.

发明人： Nick Ohler ,  Owen Budavich ,  Jason Poulos ,  Camille Indey

IPC分类号： C07D311/80 ,  C07C39/23 ,  C07D311/58

CPC分类号： C07D311/80 ,  C07C39/23 ,  C07D311/58

摘要： Provided herein are processes and compositions comprising substituted resorcylic acid or substituted resorcinols.

公开(公告)号：US20240308954A1

公开(公告)日：2024-09-19

申请号：US18549986

申请日：2022-03-11

申请人： BIOMEDCODE HELLAS SA

发明人： George Kollias ,  Niki Karagianni ,  Maria C. Denis ,  Alexios N. Matralis ,  Dimitra Papadopoulou ,  Eleni Karkoulia

IPC分类号： C07C237/44 ,  A61K31/166 ,  A61K31/353 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/451 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/54 ,  A61P29/00 ,  C07C231/02 ,  C07D211/38 ,  C07D213/40 ,  C07D213/82 ,  C07D241/44 ,  C07D295/135 ,  C07D311/58 ,  C07D471/04

CPC分类号： C07C237/44 ,  A61K31/166 ,  A61K31/353 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/451 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/54 ,  A61P29/00 ,  C07C231/02 ,  C07D211/38 ,  C07D213/40 ,  C07D213/82 ,  C07D241/44 ,  C07D295/135 ,  C07D311/58 ,  C07D471/04 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18

摘要： A compound of formula (I) or a pharmaceutically acceptable salt, hydrate, or isomer thereof. Pharmaceutical compositions comprising the compounds of formula (I) as well as their use in therapy, particularly in the treatment of inflammatory conditions. Advantageously, the compounds show a broad and robust anti-inflammatory effect, and are therapeutically safe.

公开(公告)号：US20240279173A1

公开(公告)日：2024-08-22

申请号：US18367760

申请日：2023-09-13

申请人： Queen's University at Kingston

发明人： Donald Andrew Cameron ,  Martin Petkovich ,  Uttam Saha

IPC分类号： C07D209/08 ,  A61K9/00 ,  A61K45/06 ,  A61P17/10 ,  C07C59/84 ,  C07D307/79 ,  C07D311/58 ,  C07D407/04 ,  C07F5/02

CPC分类号： C07D209/08 ,  A61P17/10 ,  C07C59/84 ,  C07D307/79 ,  C07D311/58 ,  C07D407/04 ,  C07F5/025 ,  A61K9/0014 ,  A61K45/06

摘要： Compounds that are inhibitors of retinoic acid inducible P450 (CYP26) enzymes. The compounds have retinoid activity, are resistant to CYP26-mediated catabolismact as inhibitors of CYP26B1, and are used for treating diseases that are responsive to retinoids.

公开(公告)号：US20240109832A1

公开(公告)日：2024-04-04

申请号：US18252655

申请日：2021-11-09

申请人： The Scripps Research Institute

发明人： Jin-Quan YU ,  Zhe ZHUANG

IPC分类号： C07C51/353 ,  C07C29/149 ,  C07C67/08 ,  C07D311/58

CPC分类号： C07C51/353 ,  C07C29/149 ,  C07C67/08 ,  C07D311/58 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2603/26

摘要： Disclosed herein is a process for achieving a palladium-catalyzed cyclative C(sp3)-H/C(sp2)-H coupling reaction using a native free carboxylic acid as a directing group, an amino acid ligand, and oxidant. The process is useful for synthesizing a range of biologically important scaffolds, including tetralins, chromanes, and indanes.

公开(公告)号：US20230339879A1

公开(公告)日：2023-10-26

申请号：US18187380

申请日：2023-03-21

申请人： Northwestern University

发明人： Karl A. Scheidt ,  Rick C. Betori ,  Benjamin R. McDonald

IPC分类号： C07D311/58 ,  C07D311/64 ,  C07D311/92 ,  C07D215/14 ,  C07D307/80 ,  C07C67/303

CPC分类号： C07D311/58 ,  C07C67/303 ,  C07D215/14 ,  C07D307/80 ,  C07D311/64 ,  C07D311/92

摘要： Disclosed are chromane compounds, analogs thereof, and methods of their synthesis and use. The compounds may be synthesized by methods involving reductive annulations of arylidene malonates with unsaturated electrophiles using photoredox/Lewis acid cooperative catalysis. The compounds may be formulated in a pharmaceutical composition for treating one of the aforementioned diseases or disorders.

公开(公告)号：US20230202997A1

公开(公告)日：2023-06-29

申请号：US17928645

申请日：2021-06-02

申请人： Sulfateq B.V.

发明人： Hjalmar Roland BOUMA ,  Guido Krenning ,  Robert Henk HENNING ,  Adrianus Cornelis VAN DER GRAAF

IPC分类号： C07D311/66 ,  A61P31/00 ,  C07D311/58 ,  C07D405/12

CPC分类号： C07D311/66 ,  A61P31/00 ,  C07D311/58 ,  C07D405/12

摘要： The invention relates to certain chromanol, quinone or hydroquinone compounds and derivatives thereof for treatment of sepsis and sepsis-induced organ dysfunction. Specifically, the present invention relates to chromanol compounds chosen from S-(6-hydroxy-2,5,7,8-tetramethylchroman-2yl)(piperazin-1-yl)methanone and S-(6-hydroxy-2,5,7,8-tetramethylchroman-2-yl)(4-(2-hydroxyethyl)piperazin-1-yl)methanone, and pharmaceutically acceptable salts thereof.

公开(公告)号：US11673885B2

公开(公告)日：2023-06-13

申请号：US17241662

申请日：2021-04-27

申请人： BioSplice Therapeutics, Inc.

发明人： Sunil Kumar KC ,  David Mark Wallace ,  John Hood ,  Charlene F. Barroga

IPC分类号： C07D411/06 ,  C07D213/50 ,  C07D317/46 ,  C07D319/16 ,  C07D327/06 ,  C07D339/08 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D263/56 ,  C07D311/58 ,  C07D317/54 ,  C07D319/18 ,  C07D231/56 ,  C07D333/54 ,  C07D235/06 ,  C07D407/06 ,  C07D413/06 ,  C07D307/80 ,  A61P25/00

CPC分类号： C07D411/06 ,  A61P25/00 ,  C07D213/50 ,  C07D231/56 ,  C07D235/06 ,  C07D263/56 ,  C07D307/80 ,  C07D311/58 ,  C07D317/46 ,  C07D317/54 ,  C07D319/16 ,  C07D319/18 ,  C07D327/06 ,  C07D333/54 ,  C07D339/08 ,  C07D401/06 ,  C07D405/06 ,  C07D407/06 ,  C07D409/06 ,  C07D413/06

摘要： The present disclosure provides γ-diketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.

公开(公告)号：US20180318252A1

公开(公告)日：2018-11-08

申请号：US15773306

申请日：2016-11-04

申请人： UNIVERSITÉ LAVAL

发明人： Sylvain GUERIN ,  Lucie GERMAIN ,  Karine ZANIOLO ,  Camille COUTURE ,  Pascale DESJARDINS

IPC分类号： A61K31/353 ,  A61P27/02 ,  A61P17/02 ,  A61K31/4155 ,  G01N33/50

CPC分类号： A61K31/353 ,  A61K31/4152 ,  A61K31/4155 ,  A61P17/02 ,  A61P27/02 ,  C07D311/58 ,  C07D405/06 ,  G01N33/5044 ,  A61K2300/00

摘要： Disclosed are methods of favouring epithelial wound healing in a subject. Wounds suitable for this method include wounds located on the skin or in a cornea The methods comprise contacting a wound with an activator of an AKT pathway and/or an inhibitor of the MAPK pathway such as CREB inhibitors. Preferred compounds include SC-79, C646, curcumin, platelet-derived growth factor, 4′chloro-3-hydroxy-2-naphthanilide and fumonisin B. A model for wound healing is also disclosed. The model can be used to identify test compounds that are AKT activators or inhibitors of MAPK pathway, which are suitable to favoring epithelial wound healing.

公开(公告)号：US20180312499A1

公开(公告)日：2018-11-01

申请号：US15769079

申请日：2016-11-28

申请人： Merck Sharp & Dohme Corp.

发明人： Yongxin Han ,  Satyanarayana Tummanapalli ,  Phieng Siliphaivanh ,  Kerrie Spencer

IPC分类号： C07D417/14 ,  C07D405/14 ,  A61P3/10

CPC分类号： C07D417/14 ,  A61K31/35 ,  A61P3/10 ,  C07D311/22 ,  C07D311/58 ,  C07D405/14

摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.

公开(公告)号：US20180208552A1

公开(公告)日：2018-07-26

申请号：US15576345

申请日：2016-05-26

申请人： KYORIN PHARMACEUTICAL CO., LTD.

发明人： Hiroyasu TAKAHASHI ,  Hiroyuki WATANABE ,  Kiyoshi FUJII ,  Mitsuhito SHIBASAKI ,  Mikako KAWASHIMA ,  Megumi KAMIYA ,  Kohei OHATA

IPC分类号： C07C275/30 ,  C07C275/42 ,  C07C275/50 ,  C07D231/12 ,  C07D285/08 ,  C07D285/135 ,  C07D271/113 ,  C07D271/07 ,  C07D239/36 ,  A61P29/00 ,  A61P35/00 ,  A61P31/18

CPC分类号： C07C275/30 ,  A61P29/00 ,  A61P31/18 ,  A61P35/00 ,  C07B2200/07 ,  C07C275/42 ,  C07C275/50 ,  C07C311/51 ,  C07C317/32 ,  C07C317/40 ,  C07C2601/02 ,  C07D213/61 ,  C07D231/12 ,  C07D239/36 ,  C07D249/04 ,  C07D249/08 ,  C07D249/12 ,  C07D257/04 ,  C07D261/08 ,  C07D263/32 ,  C07D263/34 ,  C07D271/06 ,  C07D271/07 ,  C07D271/10 ,  C07D271/113 ,  C07D273/04 ,  C07D277/28 ,  C07D285/08 ,  C07D285/12 ,  C07D285/135 ,  C07D307/79 ,  C07D311/58 ,  C07D333/16 ,  C07D333/28 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12

摘要： The present invention provides a urea compound or a pharmacologically acceptable salt thereof that has a formyl peptide receptor like 1 (hereinafter may be abbreviated as FPRL1) agonist effect, a pharmaceutical composition containing the urea compound or the pharmacologically acceptable salt thereof, and a pharmaceutical use thereof. It has been found that a urea derivative represented by the general formula (I) below or a pharmacologically acceptable salt thereof has a superior FPRL1 agonist effect. Compound (I) or a pharmacologically acceptable salt thereof is highly useful for treatment, prevention, or suppression of inflammatory diseases, chronic airway diseases, cancers, septicemia, allergic symptoms, HIV retrovirus infection, circulatory disorders, neuroinflammation, nervous disorders, pains, prion diseases, amyloidosis, immune disorders and the like.