Abstract: Medicaments for use in treating T-cell acute lymphoblastic leukemia, acute lymphoblastic leukemia, acute myelogenous leukemia, chronic myelogenous leukemia, breast cancer, ovarian cancer, melanoma, lung cancer, pancreatic cancer, glioblastoma, sarcoma, desmoid tumors, adenoid cystic carcinoma, colorectal cancer, head and neck cancer, cervical cancer, prostate cancer, liver cancer, or skin cancer in a patient comprising combination therapy with 4,4,4-trifluoro-N-[(1S)-2-[[(7S)-5-(2-hydroxyethyl)-6-oxo-7H-pyrido[2,3-d][3]benzazepin-7-yl]amino]-1-methyl-2-oxoethyl]butanamide, or a pharmaceutically acceptable salt or hydrate thereof, and 8-[5-(1-hydroxy-1-methylethyl)pyridin-3-yl]-1-[(2S)-2-methoxypropyl]-3-methyl-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one, or a pharmaceutically acceptable salt thereof.
Abstract: A compound with anti-drug resistant bacteria activity having the following formula (I): is disclosed. The methods of preparing the compound of formula (I) are also disclosed.
Type:
Grant
Filed:
January 25, 2021
Date of Patent:
January 17, 2023
Assignee:
SHAANXI UNIVERSITY OF SCIENCE AND TECHNOLOGY
Inventors:
Yongbo Wang, Han Li, Gennian Mao, Bin Tian, Dan Yang, Chengyuan Liang, Xiuding Yang, Wenbo Yao, Guaiping Qiao, Nan Hui, Juan Li, Liang Xin, Jingyi Li, Ruina Bian
Abstract: The compounds of the invention as shown by general structure I, as shown below, are effective in treating filovirus infections. X is selected from the group consisting of O and H; R1 is selected from (C6 to C10) aryl and (C2 to C9) heteroaryl, and R2 is selected from (C1 to C10) alkyl, (C1 to C10) alkenyl, (C1 to C10) alkynyl, (C3 to C10) cycloalkyl, and (C5 to C10) cycloalkenyl, and NR3aR3b is defined in the specification. These compounds are effective in treating filovirii infections including Ebolavirus and Marburg virus.
Type:
Grant
Filed:
July 11, 2018
Date of Patent:
January 10, 2023
Assignee:
Arisan Therapeutics Inc.
Inventors:
Michael Bruno Plewe, Kenneth McCormack, Gregory Henkel, Nadezda V. Sokolova, Eric Brown, Vidyasagar Reddy Gantla
Abstract: Provided is a process for the formation of nitrated compounds by the nitration of hydrocarbon compounds with dilute nitric acid. Also provided are processes for preparing industrially useful downstream derivatives of the nitrated compounds, as well as novel nitrated compounds and derivatives, and methods of using the derivatives in various applications.
Type:
Grant
Filed:
June 25, 2019
Date of Patent:
January 3, 2023
Assignee:
ANGUS CHEMICAL COMPANY
Inventors:
Daniel M. Trauth, George D. Green, Raymond J. Swedo, Richard L. James, Ian A. Tomlinson
Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, wherein R1, Z1, W, Z2 and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
Abstract: A process for the continuous distillative separation of mixtures comprising morpholine (MO), monoaminodiglycol (ADG), ammonia, water and methoxyethanol (MOE), obtained by reacting diethylene glycol (DEG) with ammonia, wherein ammonia, water, ADG and DEG are removed by distillation and the resulting stream comprising MO and MOE is supplied to a distillation column K40 in which at a top pressure of from 20 to 2000 mbar MO, MOE and organic products having a boiling point 128° C. (1.013 bar) are removed via the bottom and organic products having a boiling point 128° C. are removed overhead, and also MO is removed via a side draw, where K40 is equipped with an evaporator for heating the bottoms, into which is fed heating vapor having a pressure of from 1 to 10 bar.
Type:
Grant
Filed:
February 11, 2019
Date of Patent:
December 6, 2022
Assignee:
BASF SE
Inventors:
Oliver Bussmann, Eva Koch, Manfred Heilig, Joachim Pfeffinger, Joerg Pastre, Johann-Peter Melder
Abstract: The purpose of the invention is to develop, as drug-candidate compounds, a group of novel compounds having the activity of inhibiting functions of Pin1. The invention provides: a compound represented by formula (I) or a salt thereof; and a Pin1 inhibitor, a pharmaceutical composition, a therapeutic or prophylactic agent for inflammatory diseases, a therapeutic or prophylactic agent for cancer, and a therapeutic or prophylactic agent for adiposity that use said compound/salt.
Type:
Grant
Filed:
August 6, 2018
Date of Patent:
November 22, 2022
Assignees:
Hiroshima University, Tokyo University of Pharmacy & Life Sciences, The University of Tokyo
Abstract: Cavitand compositions that comprise void spaces are disclosed. The void spaces may be empty, which means that voids are free of guest molecules or atoms, or the void spaces may comprise guest molecules or atoms that are normally in their gas phase at standard temperature and pressure. These cavitands may be useful for industrial applications, such as the separation or storage of gasses. Novel cavitand compounds are also disclosed.
Abstract: The invention relates to pharmaceutical compositions comprising PPAR agonists and Nrf2 activators and methods of using combinations of PPAR agonists and Nrf2 activators for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis.
Abstract: A novel production method enables selective production of an isocyanuric acid N-substituted product of interest in one pot, requiring neither multiple steps nor cumbersome treatment, the method producing an N-(hydrocarbon)isocyanuric acid which includes a step N for reacting, in a solvent, a dihalogenated isocyanuric acid derivative with at least one hydrocarbonization agent selected from the group consisting of a halogenated hydrocarbon compound, a pseudo-halogenated hydrocarbon compound, and a dialkyl sulfate compound.
Abstract: A compound represented by general formula (I): (wherein in the formula, all the symbols have the same meanings as those described in the specification), or a pharmaceutically acceptable salt thereof is useful as a medicament's active ingredient having an EP4 receptor antagonistic activity, in preventing and/or treating disease caused by activation of an EP4 receptor.
Abstract: The application relates to a series of 2-imino-6-methylhexahydropyrimidin-4-one derivatives and 3-imino-5-methyl-1,2,4-thiadiazinane 1,1-dioxide derivatives of formula (I), substituted by an arylaminophenyl or heteroarylaminophenyl moiety. The compounds are potent inhibitors of the growth and propagation of the Plasmodium falciparum parasite in human blood and thus useful as pharmaceutical agents for the treatment of malaria.
Type:
Grant
Filed:
April 2, 2019
Date of Patent:
October 25, 2022
Inventors:
Teresa De Haro Garcia, Lloyd Malcolm King, Martin Alexander Lowe, Malcolm Maccoss, Richard David Taylor, Zhaoning Zhu
Abstract: Provided herein is a peptide epoxyketone immunoproteasome inhibitor, crystal forms, salts, and processes for making the same, and formulations thereof.
Type:
Grant
Filed:
October 9, 2020
Date of Patent:
October 25, 2022
Assignee:
KEZAR LIFE SCIENCES
Inventors:
Henry Johnson, Evan Lewis, Sean Dalziel, Dustin McMinn
Abstract: Provided are omecamtiv mecarbil dihydrochloride salt forms, compositions and pharmaceutical formulations thereof, and methods for their preparation and use.
Type:
Grant
Filed:
July 2, 2020
Date of Patent:
October 18, 2022
Assignee:
CYTOKINETICS, INC.
Inventors:
Sheng Cui, Henry Morrison, Karthik Nagapudi, Shawn D. Walker, Charles Bernard, Karl Bennett Hansen, Neil Fred Langille, Alan Martin Allgeier, Steven Mennen, Jacqueline C. S. Woo, Bradley Paul Morgan, Alex Muci
Abstract: The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer, by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism.
Type:
Grant
Filed:
April 17, 2015
Date of Patent:
October 11, 2022
Assignee:
ImmunoMet Therapeutics, Inc.
Inventors:
Sung Wuk Kim, Hong Woo Kim, Sang Hee Yoo, Ji Sun Lee, Hye Jin Heo, Hong Bum Lee, Ji Ae Kook, Young Woo Lee, Mi Jeong Kim, Woong Cho
Abstract: Provided herein are methods of treating cancer in an individual in need thereof, the methods comprising administering to the individual a CXCR7 inhibitor. In some embodiments, additional therapeutic agents are used. Also provided herein are methods of preventing precancerous cells expressing FRS2? from developing into cancer, the method comprising administering to an individual having precancerous cells expressing FRS2? a CXCR7 inhibitor. In some embodiments, additional therapeutic agents are used.
Abstract: The present invention relates to novel mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yppyrimidine-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, a novel crystalline form thereof, and a process for preparing the same. More specifically, the present invention relates to mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidine-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, which is excellent in stability, solubility, and bioavailability when it is administered not only alone but also in combination with other drugs and which has a high purity, a crystalline form thereof, and a process for preparing the same.
Type:
Grant
Filed:
April 18, 2018
Date of Patent:
September 27, 2022
Assignee:
Yuhan Corporation
Inventors:
Sang Ho Oh, Jong Gyun Kim, Se-Woong Oh, Tae Dong Han, Soo Yong Chung, Seong Ran Lee, Kyeong Bae Kim, Young Sung Lee, Woo Seob Shin, Hyun Ju, Jeong Ki Kang, Su Min Park, Dong Kyun Kim
Abstract: The present invention relates to compounds of formula I wherein A1, A2, A3, R1, R2, R3, R4, R5, R6, L, Ar and Q are each as defined herein. The compounds of the present invention are inhibitors of autotaxin (ATX) enzyme activity. 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 (e.g. fibrosis) in which ATX activity is implicated.
Type:
Grant
Filed:
March 20, 2020
Date of Patent:
September 27, 2022
Assignee:
Cancer Research Technology Limited
Inventors:
Martin Lee Stockley, Ellen Catherine Macdonald, Pritom Shah, Allan Jordan, James Hitchin, Niall Hamilton
Abstract: Provided is a drug or method for treating or preventing a condition, disorder, or disease of the corneal endothelium caused by transforming growth factor-? (TGF-?) signals and/or mitochondrial abnormalities in corneal endothelial cells. The present invention provides a drug which includes caspase inhibitors, and which is for treating or preventing a condition, disorder, or disease of the corneal endothelium caused by TGF-? signals and/or mitochondrial abnormalities in corneal endothelial cells. In the preferred embodiment, the condition, disorder, or disease of the corneal endothelium is Fuchs' corneal endothelial dystrophy.