Abstract: The present invention relates to pyridazinones and related compounds having Formula I: and pharmaceutically acceptable salts thereof, which are inhibitors of PARP7 and are useful in the treatment of cancer.
Type:
Grant
Filed:
October 29, 2020
Date of Patent:
July 4, 2023
Assignee:
Ribon Therapeutics, Inc.
Inventors:
Nicholas Robert Perl, Melissa Marie Vasbinder, Kevin Wayne Kuntz
Abstract: Disclosed are compounds active towards nuclear receptors, pharmaceutical compositions containing the compounds and use of the compounds in therapy.
Type:
Grant
Filed:
December 18, 2020
Date of Patent:
June 27, 2023
Assignee:
NUEVOLUTION A/S
Inventors:
Sanne Schrøder Glad, Ian Sarvary, Alex Haahr Gouliaev, Thomas Franch, Søren Jensby Nielsen, Luigi Piero Stasi, Montserrat Erra Solà, Lorena Taboada Martínez, Joan Taltavull Moll, Juan Francisco Caturla Javaloyes, Lluís Miquel Pagès Santacana
Abstract: Described herein are MK2 inhibitors of Formula (II) and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of autoimmune disorders, chronic inflammatory disorders, acute inflammatory disorders, auto-inflammatory disorders, fibrotic disorders, metabolic disorders, neoplastic disorders, and cardiovascular or cerebrovascular disorders.
Type:
Grant
Filed:
July 19, 2022
Date of Patent:
June 20, 2023
Assignee:
XINTHERA, INC.
Inventors:
Lynnie Trzoss, Qing Dong, Stephen W. Kaldor, Robert L. Hoffman
Abstract: Hydantoin based compounds of formula (I) useful as inhibitors of matrix metalloproteinases (MMPs), particularly macrophage elastase (MMP-12) are described. Also described are related compositions and methods of using the compounds to inhibit MMP-12 and treat diseases mediated by MMP-12, such as asthma, chronic obstructive pulmonary disease (COPD), emphysema, acute lung injury, idiopathic pulmonary fibrosis (IPF), sarcoidosis, systemic sclerosis, liver fibrosis, nonalcoholic steatohepatitis (NASH), arthritis, cancer, heart disease, inflammatory bowel disease (IBD), acute kidney injury (AKI), chronic kidney disease (CKD), Alport syndrome, and nephritis.
Abstract: The application relates to a compound having Formula (I): which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.
Type:
Grant
Filed:
November 17, 2020
Date of Patent:
June 13, 2023
Assignee:
Dana-Farber Cancer Institute, Inc.
Inventors:
Nathanael S. Gray, Pasi Janne, Hwan Geun Choi, Jaebong Jang
Abstract: Provided is a novel and industrially useful method for producing a 3,6-disubstituted imidazo[1,2-b]pyridazine derivative. The present invention provides a method for producing a 3,6-disubstituted imidazo[1,2-b]pyridazine derivative, which uses 6-fluoroimidazo[1,2-b]pyridazine as a starting material, while using an aromatic substitution reaction that utilizes C—H activation by means of palladium.
Abstract: A main object of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}acetic acid (hereinafter referred to as “Compound B”). A form-I crystal of Compound B, which shows peaks at diffraction angles (2?) of 6.4°, 8.1°, 9.5°, 10.9°, 13.2°, 15.7°, 17.0°, 19.5°, 20.3°, 21.0°, and 22.8° in a powder X-ray diffraction spectrum obtained using a Cu-K? radiation (?=1.54 ?). A form-II crystal of Compound B, which shows peaks at diffraction angles (2?) of 9.6°, 11.4°, 11.7°, 16.3°, 17.5°, 18.5°, 18.7°, 19.9°, 20.1°, 21.0°, and 24.6° in a powder X-ray diffraction spectrum obtained using a Cu-K? radiation (?=1.54 ?).
Abstract: The present disclosure relates to a fused ring pyrimidine amino compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically disclosed in the present disclosure are the compound shown in formula I, a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a metabolite thereof, a metabolic precursor thereof, or a prodrug thereof. The fused ring pyrimidine amino compound of the present application has good inhibitory activity against DDRs, particularly DDR2, and has a good therapeutic effect on tumors and fibrotic diseases, especially pulmonary inflammation and pulmonary fibrosis. Also disclosed in the present disclosure are a preparation method for the compound shown in formula I, and a use thereof.
Type:
Grant
Filed:
July 17, 2020
Date of Patent:
May 23, 2023
Assignee:
Shanghai Institute Of Material Medica, Chinese Academy of Sciences
Inventors:
Bing Xiong, Jia Li, Meiyu Geng, Jingkang Shen, Yi Zang, Jing Ai, Danqi Chen, Qi Wang, Ying Dong, Xia Peng, Yinchun Ji, Qian Tan
Abstract: A compound having the formula (LA)mIr(LB)3-m, where LA is and LB is selected from is disclosed. In the formula (LA)mIr(LB)3-m, LA and LB are different; each of X1 to X5 is C—RF or nitrogen; X is selected from O, S, and Se; each R1, R2, RB, RD, RE, and RF is hydrogen or a substituent; R3 is alkyl, cycloalkyl, or a combination thereof; and m is 1 or 2. OLEDs, consumer products, and formulations including the compound are also disclosed.
Type:
Grant
Filed:
May 22, 2019
Date of Patent:
May 16, 2023
Assignee:
Universal Display Corporation
Inventors:
Bin Ma, Edward Barron, Alan DeAngelis, Walter Yeager, Zeinab Elshenawy, Harvey Wendt, Ting-Chih Wang, Kwang-Ohk Cheon, Chuanjun Xia
Abstract: Compositions, methods, and kits for the labeling, detecting, isolating and/or analysis of biomolecules modified by attachment of chemical handles are disclosed.
Type:
Grant
Filed:
January 10, 2020
Date of Patent:
May 2, 2023
Assignee:
BIOCONJUGATE TECHNOLOGIES, LLC
Inventors:
Andrei Polukhtin, Peter J. An, Alexandra Kulyashova, Jakub M. Labedz, Valentin A. Rassadin, Nikita V. Savelyev, Kostiantyn Ziabrev
Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject, and the compound has the structure of Formula I including any possible deuterated isomers, stereoisomers or tautomeric forms thereof.
Type:
Grant
Filed:
June 26, 2018
Date of Patent:
May 2, 2023
Assignee:
Janssen Pharmaceutica NV
Inventors:
Zhao-Kui Wan, Yimin Jiang, Xuedong Dai, Qian Liu, Wing Shun Cheung, Gang Deng, Liqiang Fu
Abstract: A compound has the following formula: The compound is a p38 MAP kinase inhibitor. The compound and its pharmaceutically acceptable salts can be used for treatment of conditions, such as inflammatory diseases.
Type:
Grant
Filed:
September 24, 2020
Date of Patent:
April 25, 2023
Assignee:
RESPIVERT LTD.
Inventors:
Alistair Ian Longshaw, Euan Alexander Fraser Fordyce, Stuart Thomas Onions, John King-Underwood, Jennifer Venable
Abstract: The present invention relates to the Compound of following formula (I): or a pharmaceutically acceptable salt thereof. The present invention also relates to a pharmaceutical composition containing such a compound and a method for preparing such a compound.
Type:
Grant
Filed:
April 26, 2019
Date of Patent:
April 25, 2023
Assignees:
UNIVERSITE PARIS-SACLAY PARC TECHNOLOGIQUE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), INSTITUT GUSTAVE-ROUSSY, INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM)
Abstract: An iridium complex which has a phenylpyridine bidentate ligand containing a group represented by the following general formula (A): wherein X represents a cyano group or a halogenated alkyl group; L represents a single bond or a divalent linking group; R represents a substituent; n represents an integer of 0 to 4; * represents a binding site to a phenylpyridine bidentate ligand.
Abstract: Provided are a uracil compound represented by Formula (IV) or a pharmaceutically acceptable salt thereof and a pharmaceutical composition of the same. Also provided is a use thereof as a c-MET/AXL inhibitor in preparing a c-MET/AXL-inhibiting drug or a drug for treating a tumor.
Type:
Grant
Filed:
November 23, 2018
Date of Patent:
April 11, 2023
Assignee:
MEDSHINE DISCOVERY, INC.
Inventors:
Jinping Li, Xiongbin Xu, Gang Li, Lihong Hu, Charles Z. Ding, Yaling Zhou, Guoping Hu, Jian Li, Shuhui Chen
Abstract: The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R5, R6, R7, A, B, W, X, Y and Z are as defined herein.
Type:
Grant
Filed:
October 8, 2021
Date of Patent:
March 28, 2023
Assignee:
KalVista Pharmaceuticals Limited
Inventors:
Rebecca Louise Davie, Hannah Joy Edwards, David Michael Evans, Simon Teanby Hodgson, Alessandro Mazzacani, Michael John Stocks, Thomas Matthew Baker, Matthew Robert Conroy, Alun John Smith, David Edward Clark
Abstract: Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
Abstract: The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof. It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses, in particular to modulate CFTR protein or ABC protein activities.
Type:
Grant
Filed:
March 14, 2018
Date of Patent:
March 7, 2023
Assignees:
Fondazione Istituto Italiano Di Technologia, Istituto Giannina Gasiini, FondaZione Per La Ricerca Sulla Fibrosi Cristica—Onlus
Inventors:
Tiziano Bandiera, Fabio Bertozzi, Paolo Di Fruscia, Federico Sorana, Emanuela Caci, Loretta Ferrera, Nicoletta Pedemonte, Luis Juan Vicente Galietta
Abstract: Disclosed in the present invention are a heterocyclic compound, an application thereof and a pharmaceutical composition comprising the same. Provided by the present invention are a heterocyclic compound represented by formula I or a pharmaceutically acceptable salt thereof. The compound has a novel structure and a good inhibitory activity against autotaxin (ATX).
Abstract: A porphyrin compound of Formula III and composition made therefrom comprising a therapeutically effective dose of a porphyrin bound via a linker to an anti-cancer agent useful in treating cancer in a patient in need thereof or to treat cancer cells in-vitro. The compounds and compositions may be delivered by a drug delivery device as disclosed here and be part of a kit.
Type:
Grant
Filed:
December 17, 2018
Date of Patent:
February 28, 2023
Assignee:
ONCOSELECT THERAPEUTICS, LLC
Inventors:
Maria Zannes, Vivienne I. Rebel, William E. Bauta