Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione monohydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione monohydrate are also disclosed.
Abstract: The present invention relates to compounds which are inhibitors of SSAO activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth.
Type:
Grant
Filed:
July 20, 2016
Date of Patent:
March 17, 2020
Assignee:
PROXIMAGEN, LLC
Inventors:
Max Espensen, Lee Patient, David Evans, Edward Savory, Iain Simpson
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 30, 2015
Date of Patent:
March 17, 2020
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
Abstract: A highly pure optically active proton pump inhibitor compound can be produced safely and inexpensively in a high yield and enantioselectivity by a method of producing an optically active sulfoxide of Formula 2 or a salt thereof, comprising oxidizing a sulfide of Formula 1 or a salt thereof with hydrogen peroxide using an iron salt in the presence of a chiral ligand of Formula 3; wherein A is CH or N; R1 is hydrogen atom, an alkyl optionally substituted by halogen(s), or an alkoxy optionally substituted by halogen(s); one to three R2 may exist, and each of R2 is independently an alkyl, a dialkylamino, or an alkoxy optionally substituted by halogen(s) or alkoxy(s); each of R3 is independently hydrogen atom, a halogen, cyano or the like; R4 is a tertiary alkyl; and * and ** represent respectively R configuration or S configuration.
Type:
Grant
Filed:
April 11, 2019
Date of Patent:
March 17, 2020
Assignees:
THE UNIVERSITY OF TOKYO, TOWA PHARMACEUTICAL CO. LTD.
Abstract: Disclosed are chemical entities of Formula (I), wherein R1 and Z are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).
Abstract: The present application describes deuterium-enriched pioglitazone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
Abstract: A composition comprising (S)—N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.
Type:
Grant
Filed:
December 14, 2015
Date of Patent:
March 3, 2020
Assignee:
MERCK SHARP & DOHME CORP.
Inventors:
Pranav Gupta, Jason Wan, Scott T. Trzaska
Abstract: The present disclosure relates to a novel crystalline form of Galunisertib, processes for preparation and use thereof. The present disclosure also relates to a pharmaceutical composition comprises the novel crystalline form of Galunisertib and use of the novel crystalline form of Galunisertib and pharmaceutical composition for preparing drugs treating disease. The crystalline form of the present disclosure has good stability, solubility and hygroscopicity, which has significant value for future drug optimization and development.
Abstract: The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof. The compounds of formula (I) are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
Type:
Grant
Filed:
August 31, 2015
Date of Patent:
February 25, 2020
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Jason Imbriglio, Rui Liang, Clare London, Kenneth Marby, James Tata, Ming You, Yusheng Xiong
Abstract: The present invention describes novel diamino pyridine derivatives exhibiting JAK modulating properties. The present invention also relates to pharmaceutical compositions comprising these novel compounds, methods of using said compounds in the treatment of various diseases and disorders being susceptible to JAK modulation, and processes for preparing the compounds described hereinafter.
Abstract: The present disclosure discusses salt forms of 4-cyano-N-[2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl]-1H-imidazole-2-carboxamide.
Abstract: The present disclosure relates to a novel crystalline form of lenvatinib mesylate and the preparation method thereof. The novel crystalline form of mesylate of the present disclosure can be used for treating invasive and differentiated thyroid cancer. The novel crystalline form of mesylate of the present disclosure has good solubility, stability, and remarkable purification effect in process. The preparation method of this novel crystalline form is simple, low cost, and has an important value for future optimization and development of the drug.
Abstract: Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.
Type:
Grant
Filed:
July 10, 2019
Date of Patent:
February 11, 2020
Assignees:
Aragon Pharmaceuticals, Inc., Sloan-Kettering Institute For Cancer Research
Inventors:
Anna Dilhas, Mark R. Herbert, Ouathek Ouerfelli, Nicholas D. Smith
Abstract: The invention provides certain nicotine salts, co-crystals, and salt co-crystals and provides novel polymorphic forms of certain nicotine salts. In particular, nicotine salts with mucic acid, 3,5-dihydroxybenzoic acid, and 2,3-dihydroxybenzoic acid, and crystalline polymorphic forms of nicotine 4-acetamidobenzoate, nicotine gentisate, and nicotine 1-hydroxy-2-naphthoate are described. The invention further provides methods of preparation and characterization of such nicotine salts, co-crystals, and salt co-crystals and polymorphic forms thereof. In addition, tobacco products, including smoking articles, smokeless tobacco products, and electronic smoking articles comprising nicotine salts, co-crystals, and/or salt co-crystals are also provided.
Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Type:
Grant
Filed:
December 11, 2018
Date of Patent:
February 4, 2020
Assignee:
NOVARTIS AG
Inventors:
Christopher M. Adams, Doug Bevan, Michael Paul Capparelli, Takeru Ehara, Luciana Ferrara, Nan Ji, Erik Meredith, Muneto Mogi, James J. Powers, Ganesh Prasanna, Nello Mainolfi, Mitsunori Kato
Abstract: 4-Alkoxy-3-hydroxypicolinic acids may be conveniently prepared from 4,6-dibromo-3-hydroxypicolinonitrile in a series of chemical steps selected from bromo substitution, nitrile hydrolysis and halogen reduction that are conducted as a single pot process. 4,6-Dibromo-3-hydroxypicolinonitrile may be prepared from furfural in a series of chemical steps selected from cyano-amination, amine salt formation and bromination-rearrangement.
Type:
Grant
Filed:
January 23, 2017
Date of Patent:
February 4, 2020
Assignee:
Dow AgroSciences LLC
Inventors:
Kenneth E. Stockman, Gregory T. Whiteker, Erich J. Molitor, Nakyen Choy
Abstract: The invention includes taxoid compounds represented by the formula: wherein: R1 represents a methyl group or a fluorine; R2 represents an alkyl or alkenyl group having one to six carbon atoms; or a cycloalkyl or cycloalkenyl group having three to seven ring carbon atoms; R3 represents an alkyl, alkenyl, dialkylamino, alkylamino, or alkoxy group having one to six carbon atoms; a cycloalkyl or cycloalkenyl group having three to seven ring carbon atoms; an aryl group having six to eighteen ring carbon atoms; or a heteroaryl group having three to seventeen ring carbon atoms; R4 represents hydrogen or a methyl group; and X represents hydrogen or fluorine.
Type:
Grant
Filed:
July 1, 2016
Date of Patent:
February 4, 2020
Assignee:
THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORK
Abstract: Compounds having the following formula: or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R2 is a monocyclic heteroaryl group, and R1, R3, R4, R5 and R6 are as defined herein, are useful as kinase modulators, including IRAK-4 inhibition.
Type:
Grant
Filed:
June 15, 2018
Date of Patent:
January 28, 2020
Assignee:
Bristol-Myers Squibb Company
Inventors:
Rajeev S. Bhide, John V. Duncia, John Hynes, Satheesh Kesavan Nair, William J. Pitts, Sreekantha Ratna Kumar, Daniel S. Gardner, Natesan Murugesan, Venkatram Reddy Paidi, Joseph B. Santella, Ramesh Kumar Sistla, Hong Wu