Abstract: The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of HER2 or EGFR for the treatment or prevention of disease, including cancer.
Type:
Grant
Filed:
April 24, 2020
Date of Patent:
June 21, 2022
Assignee:
Board of Regents, The University of Texas System
Inventors:
John Heymach, Jacqulyne Robichaux, Monique Nilsson, Philip Jones, Jason Cross, Jay Theroff
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.
Type:
Grant
Filed:
September 21, 2018
Date of Patent:
June 14, 2022
Assignee:
KYMERA THERAPEUTICS, INC.
Inventors:
Nello Mainolfi, Nan Ji, Yi Zhang, Matthew M. Weiss
Abstract: A method of treating disorders associated with NO/SNO deficiency or benefiting from increased SNO in a subject in need thereof includes administering to the subject an ADH inhibitor, AKR inhibitor, SNO-CoAR inhibitor, and/or SNO-CoA at an amount(s) effective to promote S-nitrosylation of proteins in the subject.
Abstract: Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R? are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-?, and can be used to treat disease by blocking TGF-? signaling.
Type:
Grant
Filed:
March 21, 2019
Date of Patent:
June 7, 2022
Assignees:
Rigel Pharmaceuticals, hic., Bristol-Myers Squibb Company
Inventors:
Todd Kinsella, Marina Gelman, Hui Hong, Ihab S. Darwish, Rajinder Singh, Jiaxin Yu, Robert M. Borzilleri, Upender Velaparthi, Peiying Liu, Chetan Padmakar Dame, Hasibur Rahaman, Jayakumar Sankara Warrier
Abstract: Provided are a series of novel pyridine or pyrimidine derivatives which inhibit CDK9 and may be useful for the treatment of hyperproliferative diseases. In particular the compounds are of use in the treatment of proliferative disease such as cancer including hematological malignancies such as acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia, diffuse large B cell lymphoma, Burkitt's lymphoma, follicular lymphoma and solid tumors such as breast cancer, lung cancer, neuroblastoma and colon cancer.
Type:
Grant
Filed:
July 17, 2020
Date of Patent:
June 7, 2022
Assignee:
ASTRAZENECA AB
Inventors:
Bernard Barlaam, Christopher De Savi, Janet Hawkins, Alexander Hird, Michelle Lamb, Kurt Pike, Melissa Vasbinder
Abstract: The present invention relates to prodrug compounds and their use in the treatment of Cystic Fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.
Type:
Grant
Filed:
June 2, 2020
Date of Patent:
May 31, 2022
Assignees:
AbbVie Global Enterprises Ltd., Galapagos NV
Inventors:
Didier Philippe Robert Schils, Sam Bob Corveleyn, Herman Augustinus De Kock, Matthew Beau Dufek
Abstract: The present invention discloses compositions, methods, and systems of treating female sexual dysfunction by stimulating the contraction of the smooth muscle of the nipple. The smooth muscle in the nipple expresses trace amine associated receptors and thus can be contracted through a class of trace amine associated receptor agonists such as octopamine or tyramine, but any agent that promotes contraction of smooth muscle can be considered for the methods and compositions described herein. The contraction of the smooth muscle erects the nipple and increases female sexual arousal. The smooth muscle stimulatory compound can be formulated in a solution, foam, ointment, gel, spray, lotion, powder, topical cream, emulsion, slow release capsule or any similar method, compound, or delivery vehicle including a pre-wetted gauze or cotton pad. Additionally, the disclosed composition can be used to improve the quality of a sexual experience, e.g.
Abstract: The present invention relates to a method for preparing 3-[(4S)-8-bromo-1-methyl-6-(pyridin-2-yl)-4H-imidazo[1,2-a] [1,4]benzodiazepin-4-yl]-propionic acid methyl ester starting from 3-[(3S)-7-bromo-2-oxo-5-(pyridin-2-yl)-2,3-dihydro-1H-[1,4]-benzodiazepin-3-yl] propionic acid methyl ester, and novel compounds useful as intermediates in said method, i.e., (3S)-3-[7-bromo-2-(2,2-dimethoxypropylamino)-5-pyridin-2-yl-3H-benzo[e] [1,4]diazepin-3-yl]propionic acid methyl ester.
Abstract: The present invention provides compounds of Formula (Ia) or (Ib): (Ia) or (Ib), or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
Type:
Grant
Filed:
December 18, 2018
Date of Patent:
May 3, 2022
Assignee:
Bristol-Myers Squibb Company
Inventors:
Yan Shi, Ying Wang, Peter Tai Wah Cheng
Abstract: The present invention provides compounds of Formula (I): Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
Type:
Grant
Filed:
December 18, 2018
Date of Patent:
May 3, 2022
Assignee:
Bristol-Myers Squibb Company
Inventors:
Yan Shi, Peter Tai Wah Cheng, Ying Wang, Jun Li, Tianan Fang, James R. Corte, Jun Shi, Hao Zhang, Lawrence J. Kennedy, Shiwei Tao
Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
Type:
Grant
Filed:
December 18, 2018
Date of Patent:
April 26, 2022
Assignee:
Bristol-Myers Squibb Company
Inventors:
Yan Shi, Ying Wang, Peter Tai Wah Cheng, Jun Li, Steven J. Walker
Abstract: The present disclosure relates to the use of cannabidiol (CBD) in the treatment of absence seizures. In particular, the disclosure relates to the use of CBD for reducing absence seizures in patients suffering with etiologies that include: Lennox-Gastaut Syndrome; Tuberous Sclerosis Complex; Dravet Syndrome; Doose Syndrome; CDKL5; Dup15q; Jeavons syndrome; Myoclonic Absence Epilepsy; Neuronal ceroid lipofuscinoses (NCL) and brain abnormalities. The disclosure further relates to the use of CBD in combination with one or more anti-epileptic drugs (AEDs).
Type:
Grant
Filed:
June 17, 2015
Date of Patent:
April 26, 2022
Assignee:
GW Research Limited
Inventors:
Geoffrey Guy, Stephen Wright, Orrin Devinsky
Abstract: Provided are a pyrimidine compound represented by Formula 1, a method of preparing the compound, and a pharmaceutical use of the compound for the prevention or treatment of cancer.
Type:
Grant
Filed:
April 27, 2020
Date of Patent:
April 5, 2022
Assignee:
Hanmi Pharm. Co., Ltd.
Inventors:
In Hwan Bae, Ji Sook Kim, Jae Yul Choi, Seok Jong Kang, Young Gil Ahn, Kwee Hyun Suh
Abstract: The invention relates to a series of novel compounds containing acryloyl group. In particular, the invention relates to acryloyl group-containing compounds shown in formula (1) and the preparation method thereof, and application of the compounds shown in formula (1) and pharmaceutically acceptable salts thereof in preparation of medicaments for treating, regulating and/or preventing diseases related to physiological conditions related to CRM1 protein.
Abstract: The invention generally relates to methods to prevent and/or inhibit viral infection as well as to inhibit inflammation and/or pathogen infection by administering at least one xylitol lipid analog or compositions comprising at least one xylitol lipid analog to an individual. The invention also relates to methods to prevent or inhibit respiratory syncytial virus (RSV) infection by administering at least one xylitol lipid analog or compositions comprising at least one xylitol lipid analog to an individual.
Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An embodiment of the invention is the provision of a compound of Formula IIIA.
Type:
Grant
Filed:
March 20, 2020
Date of Patent:
March 22, 2022
Assignees:
Valo Health, Inc., Genentech, Inc.
Inventors:
Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng, Po-Wai Yuen
Abstract: The combination of (S)-2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5-carboxamide or pharmaceutically acceptable salt thereof, and 4-(4-(1-Isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4?-piperidine]-1?-carbonyl)-6-methoxypyridin-2-yl)benzoic acid or pharmaceutically acceptable salt thereof, for treatment of diseases, including non-alcoholic steatohepatitis (NASH), in mammals are described herein.
Type:
Grant
Filed:
August 28, 2019
Date of Patent:
February 22, 2022
Assignee:
Pfizer Inc.
Inventors:
William Paul Esler, Trenton Thomas Ross
Abstract: Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-?.
Type:
Grant
Filed:
November 3, 2020
Date of Patent:
February 1, 2022
Assignee:
Edgewise Therapecutics, Inc.
Inventors:
Kevin Hunt, Kevin Koch, Alan Russell, Stephen Schlachter, Paul Winship, Chris Steele, Grace Uzoho