公开(公告)号：US20240376068A1

公开(公告)日：2024-11-14

申请号：US18647374

申请日：2024-04-26

Applicant: Minerva Neurosciences, Inc.

Inventor： Remy LUTHRINGER ,  Nadine NOEL ,  Florent SCHMITT ,  Sandra WERNER ,  Hans MAAG ,  Jay SAOUD

IPC: C07D401/04 ,  C07D217/06 ,  C07D217/08 ,  C07D223/16 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D417/06

Abstract: The present disclosure relates to compounds of Formula (I): and their prodrugs, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods of their preparation. The compounds disclosed herein are useful for modulating Sigma receptors and have antiviral activity, and may also be useful in the treatment and/or prevention of pain disorders, neurological disorders (e.g., Parkinson's disease and Alzheimer's disease), and cancer.

公开(公告)号：US20240293392A1

公开(公告)日：2024-09-05

申请号：US18570244

申请日：2022-07-18

Applicant: NeoPhore Limited

Inventor： Julian Blagg ,  Martin Drysdale ,  David Clark ,  Paul Winship

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

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

Abstract: 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

Applicant: CORTEVA AGRISCIENCE LLC

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

IPC: 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 classification number: 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

Abstract: 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

Applicant: ONECUREGEN CO., LTD.

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

IPC: C07D217/06 ,  A61P35/00

CPC classification number: C07D217/06 ,  A61P35/00

Abstract: 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

Applicant: PATHIOS THERAPEUTICS LIMITED

Inventor： Tom MCCARTHY ,  Gavin MILNE ,  Tobias MOECHEL ,  Alan NAYLOR

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

CPC classification number: C07D471/04 ,  C07D217/06 ,  C07D498/04 ,  C07D217/26 ,  C07D471/14 ,  C07D413/04 ,  C07D401/04 ,  C07D409/04

Abstract: 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

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

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

Abstract: 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

Applicant: SHENZHEN CELL INSPIRE PHARMACEUTICAL DEVELOPMENT CO., LTD.

Inventor： Dane HUANG ,  Chao ZHAO ,  Qiong GU ,  Jun XU

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

Abstract: 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

Applicant: Versitech Limited

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

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

Abstract: 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

Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM

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

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

Abstract: 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

Applicant: Saint Louis University

Inventor： Daniela Salvemini ,  Christopher K. Arnatt

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

Abstract: 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.