公开(公告)号：US20240293392A1

公开(公告)日：2024-09-05

申请号：US18570244

申请日：2022-07-18

申请人： NeoPhore Limited

发明人： Julian Blagg ,  Martin Drysdale ,  David Clark ,  Paul Winship

IPC分类号： A61K31/4725 ,  A61K31/4035 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/501 ,  C07D209/44 ,  C07D217/06 ,  C07D401/12 ,  C07D405/14 ,  C07D471/04

CPC分类号： A61K31/4725 ,  A61K31/4035 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/501 ,  C07D209/44 ,  C07D217/06 ,  C07D401/12 ,  C07D405/14 ,  C07D471/04

摘要： The present invention relates to compounds of Formula (I) that target the MLH1 or MLH1 and PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process: Formula (I) wherein R6, Y1, Y2, A1, A2, A3, A4, R11, R12, R13 and R14 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which MLH1 or MLH1 and PMS2 activity is implicated.

公开(公告)号：US20240023549A1

公开(公告)日：2024-01-25

申请号：US18253822

申请日：2021-11-22

申请人： CORTEVA AGRISCIENCE LLC

发明人： ANN BUYSSE ,  ERIN HANCOCK ,  SUSANA LOPEZ ,  BRIAN LOY ,  STACY T. MEYER ,  JEFF PETKUS ,  ADRIAN TLAHUEXT-ACA ,  WEIWEI WANG ,  PULAN YU

IPC分类号： A01N37/52 ,  C07C257/12 ,  C07D213/75 ,  C07D213/40 ,  C07D295/195 ,  C07D217/06 ,  C07D215/08 ,  C07C323/41 ,  C07D333/20 ,  C07D209/12 ,  C07D317/28 ,  C07D317/58 ,  C07D233/64 ,  C07D491/107 ,  C07D209/44 ,  A01N43/40 ,  A01N43/84 ,  A01N43/42 ,  A01N43/36 ,  A01N43/60 ,  A01N43/10 ,  A01N43/38 ,  A01N43/28 ,  A01N43/30 ,  A01N43/50 ,  A01N43/90 ,  A01N43/44 ,  C07D205/04 ,  C07D211/32 ,  A01P3/00

CPC分类号： A01N37/52 ,  C07C257/12 ,  C07D213/75 ,  C07D213/40 ,  C07D295/195 ,  C07D217/06 ,  C07D215/08 ,  C07C323/41 ,  C07D333/20 ,  C07D209/12 ,  C07D317/28 ,  C07D317/58 ,  C07D233/64 ,  C07D491/107 ,  C07D209/44 ,  A01N43/40 ,  A01N43/84 ,  A01N43/42 ,  A01N43/36 ,  A01N43/60 ,  A01N43/10 ,  A01N43/38 ,  A01N43/28 ,  A01N43/30 ,  A01N43/50 ,  A01N43/90 ,  A01N43/44 ,  C07D205/04 ,  C07D211/32 ,  A01P3/00

摘要： This disclosure relates to aryl amidines of Formula I and their use as fungicides.

公开(公告)号：US20230219894A1

公开(公告)日：2023-07-13

申请号：US17794810

申请日：2020-11-16

申请人： ONECUREGEN CO., LTD.

发明人： Kyeong LEE ,  Mi Sun WON ,  Hyun-Seung BAN ,  Min Kyoung KIM ,  Bo-Kyung KIM

IPC分类号： C07D217/06 ,  A61P35/00

CPC分类号： C07D217/06 ,  A61P35/00

摘要： The present invention relates to: a disubstituted adamantyl derivative or a pharmaceutically acceptable salt thereof, and an anticancer pharmaceutical composition and a kit containing same as an active ingredient. The disubstituted adamantyl derivative according to the present invention suppresses the growth of cancer cells by targeting mitochondria ETC complex I and damaging the metabolism of cancer cells, and thus can be useful as an anticancer pharmaceutical composition that is a powerful therapeutic agent for cancer dependent on oxidative phosphorylation for producing ATP.

公开(公告)号：US20230174530A1

公开(公告)日：2023-06-08

申请号：US17999001

申请日：2021-06-04

申请人： PATHIOS THERAPEUTICS LIMITED

发明人： Tom MCCARTHY ,  Gavin MILNE ,  Tobias MOECHEL ,  Alan NAYLOR

IPC分类号： C07D471/04 ,  C07D217/06 ,  C07D498/04 ,  C07D217/26 ,  C07D471/14 ,  C07D413/04 ,  C07D401/04 ,  C07D409/04

CPC分类号： C07D471/04 ,  C07D217/06 ,  C07D498/04 ,  C07D217/26 ,  C07D471/14 ,  C07D413/04 ,  C07D401/04 ,  C07D409/04

摘要： The present invention relates to a compound of formula (Ia), or a pharmaceutically acceptable salt or solvate thereof, (I) wherein: ring A is a 5- or 6-membered monocyclic aromatic or heteroaromatic ring, or a 9- or 10-membered bicyclic aromatic or heteroaromatic ring, each of which is optionally substituted with one or more substituents selected from F, Cl, Br, I, CN, alkoxy, NR11R11′, OH, SO2-alkyl, CO2-alkyl, alkyl, haloalkyl, aralkyl, aryl, and heteroaryl, and wherein said aryl and heteroaryl substituents are in turn optionally substituted with one or more substituents each independently selected from F, Cl, Br, I, CN, alkoxy, NR11R11′, OH, alkyl, haloalkyl, and aralkyl; Y and Z are each independently CR10R10′, wherein R10 and R10′ are each independently selected from H, F, alkyl, and haloalkyl; R1, R4, and R5 are each independently selected from H, F, Cl, Br, I and haloalkyl; R2 and R3 are each independently selected from H, F, Cl, Br, I, CN, and haloalkyl; wherein at least two of R2, R3 and R4 are other than H; and R11 and R11′ are each independently selected from H, alkyl, haloalkyl, COR12, and SO2R13, wherein R12 and R13 are both alkyl; wherein the compound is other than: N-(3,4-Dichlorophenyl)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxamide; N-(3,4-Dichlorophenyl)-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-carboxamide; N-(4-Chloro-3-(trifluoromethyl)phenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide; N-(3,4-dichlorophenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide; N-(3,4-Dichlorophenyl)-6,7-dihydroisoxazolo[4,5-c]pyridine-5(4H)-carboxamide; and N-(3,4-Dichlorophenyl)-4-methyl-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-carboxamide. Further aspects of the invention relate to such compounds for use in the field of immunooncology, immunology, and related applications.

公开(公告)号：US20220162201A1

公开(公告)日：2022-05-26

申请号：US17431006

申请日：2020-02-14

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Dean A. Wacker ,  Susheel Jethanand Nara ,  Srinivas Cheruku ,  Kandhasamy Sarkunam ,  Firoz Ali Jaipuri ,  Rishikesh Narayan ,  Subba Reddy Bandreddy ,  Srinivas Jogi

IPC分类号： C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D403/12 ,  C07D217/06 ,  C07D271/06 ,  C07D417/14

摘要： Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a salt or solvate thereof, wherein Q is C2-6 alkenyl or C2-6 alkynyl, each substituted with zero to 2 R1; and the other variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

公开(公告)号：US20220153713A1

公开(公告)日：2022-05-19

申请号：US17562976

申请日：2021-12-27

申请人： SHENZHEN CELL INSPIRE PHARMACEUTICAL DEVELOPMENT CO., LTD.

发明人： Dane HUANG ,  Chao ZHAO ,  Qiong GU ,  Jun XU

IPC分类号： C07D277/56 ,  A61P17/14 ,  C07D277/82 ,  C07C251/76 ,  C07D213/75 ,  C07D213/85 ,  C07D211/58 ,  C07D217/06 ,  C07D295/185

摘要： The present disclosure provides a brand-new hydrazone amide derivative and an application thereof in preparation of medicaments for preventing and treating alopecia. The structural formula of the hydrazone amide derivative is shown in formula (I), and the hydrazone amide derivative is a brand-new compound for stimulating hair follicle growth and preventing and treating alopecia.

公开(公告)号：US20210309622A1

公开(公告)日：2021-10-07

申请号：US17352382

申请日：2021-06-21

申请人： Versitech Limited

发明人： Yi Tsun Richard KAO ,  Peng GAO ,  Xuechen LI ,  Ming LIU

IPC分类号： C07D295/08 ,  A61K9/00 ,  C07D215/58 ,  C07D217/06 ,  A61P31/04

摘要： Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (II): The present methods include administering to a subject an effective amount of one or more compounds of Formula (II). In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.

公开(公告)号：US20210300903A1

公开(公告)日：2021-09-30

申请号：US17184776

申请日：2021-02-25

申请人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM

发明人： Stephen F. MARTIN ,  James J. SAHN ,  Kathryn Taylor LINKENS

IPC分类号： C07D403/04 ,  C07D217/06 ,  C07D223/16 ,  C07D401/04 ,  C07D209/44 ,  A61P35/00

摘要： Provided herein, inter alia, are compounds and methods of treating diseases including cancer, neurological disease, alcohol withdrawal, depression and anxiety, and neuropathic pain.

公开(公告)号：US20210122750A1

公开(公告)日：2021-04-29

申请号：US17080247

申请日：2020-10-26

申请人： Saint Louis University

发明人： Daniela Salvemini ,  Christopher K. Arnatt

IPC分类号： C07D471/04 ,  C07D217/06 ,  C07D295/135 ,  A61P23/00 ,  A61P25/02

摘要： Disclosed herein are compositions and methods for treating neuropathic pain in a subject in need thereof. Compositions disclosed herein are GPR183 antagonists. The methods include administering to a subject in need thereof a therapeutically effective amount of a GPR183 antagonist.

公开(公告)号：US10781193B2

公开(公告)日：2020-09-22

申请号：US16244824

申请日：2019-01-10

申请人： KANEKA CORPORATION

发明人： Hiroaki Yasukouchi ,  Masaru Mitsuda ,  Akira Nishiyama ,  Makoto Funabashi

IPC分类号： C07D513/02 ,  C07D301/00 ,  C07C67/14 ,  C07C231/02 ,  C07D263/44 ,  C07C233/64 ,  C07D303/16 ,  C07D235/02 ,  C07C69/78 ,  C07D217/06 ,  C07D471/08

摘要： The present disclosure provides a reaction of a chlorine-containing compound using a flow reactor which is less restricted by a solvent to be used. In the present disclosure, an organic compound is produced by supplying a reaction substrate having at least one functional group which can react with chlorine and is selected from the group consisting of hydroxy group, a thiol group, an amino group, a carboxyl group, a thiocarboxyl group, and an acid amide group, and a chlorine-containing compound to a flow reactor together with a trialkyl amine having 9 to 40 carbon atoms and an organic solvent, and allowing the reaction substrate and the chlorine-containing compound to react with each other.