Abstract: Novel 1-oxa-4-azonium cyclohexane salts are described. These compounds can be used as structure directing agents, and they overcome many of the typical problems associated with OSDA synthesis and subsequent zeolite synthesis. Methods for synthesis of the 1-oxa-4-azonium cyclohexane salts from a variety of starting materials are also described. A substituted hydrocarbon is added to water to form a mixture, and a 1-oxa-4-azacyclohexane derivative is then added. The reaction mixture stirred until a solution containing the 1-oxa-4-azonium cyclohexane salt is obtained.
Type:
Grant
Filed:
May 16, 2018
Date of Patent:
April 28, 2020
Inventors:
Christopher P. Nicholas, Mark A. Miller, Melissa M. Galey, Benjamin D. Yuhas, Sesh Prabhakar
Abstract: The present invention is directed to certain amides and heterocyclic compounds. The present invention also relates to uses of these compounds to treat several diseases including autoimmune disorders, cardiovascular disorders, inflammation, central nervous system disorders, arterial thrombotic disorders, fibrotic disorders, glaucoma, and neoplastic disorders.
Abstract: A method for producing a compound (4), which comprises allowing a compound (1) to react with hydrogen gas in an inert solvent, in the presence of a specific chiral ligand and a ruthenium catalyst, or in the presence of an asymmetric transition metal complex catalyst previously generated from the chiral ligand and the ruthenium catalyst.
Abstract: The present invention relates to an improved process for the preparation of enzalutamide by conventional synthesis, which avoids utilization of microwave irradiation and noxious reagents. The present invention also relates to an improved process for preparation of 4-isothiocyanato-2-(trifluoromethyl) benzonitrile, which is an intermediate in the synthesis of Enzalutamide.
Abstract: Isoindoline sigma-2 receptor antagonist compounds, pharmaceutical compositions comprising such compounds, and methods for inhibiting Abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology are provided.
Type:
Grant
Filed:
December 21, 2018
Date of Patent:
April 7, 2020
Assignee:
COGNITION THERAPEUTICS, INC.
Inventors:
Gilbert M. Rishton, Susan M. Catalano, Gary C. Look
Abstract: This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Bruton's tyrosine kinase, for example cancer, lymphoma, leukemia and immunological diseases.
Abstract: Novel 1-oxa-4-azonium cyclohexane salts are described. These compounds can be used as structure directing agents, and they overcome many of the typical problems associated with OSDA synthesis and subsequent zeolite synthesis. Methods for synthesis of the 1-oxa-4-azonium cyclohexane salts from a variety of starting materials are also described. A substituted hydrocarbon is added to water to form a mixture, and a 1-oxa-4-azacyclohexane derivative is then added. The reaction mixture stirred until a solution containing the 1-oxa-4-azonium cyclohexane salt is obtained.
Type:
Grant
Filed:
May 16, 2018
Date of Patent:
March 24, 2020
Inventors:
Christopher P. Nicholas, Mark A. Miller, Melissa M. Galey, Benjamin D. Yuhas, Sesh Prabhakar
Abstract: The present invention relates to the compound (2R,2?R)-bis(((((tetrahydro-2H-pyran-4-yl)oxy)carbonyl)oxy)methyl) 1,1?-adipoylbis(pyrrolidine-2-carboxylate), pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.
Type:
Grant
Filed:
December 11, 2017
Date of Patent:
March 24, 2020
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Abstract: The specification relates to compounds of Formula (I): and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cell proliferative disorders.
Type:
Grant
Filed:
October 9, 2018
Date of Patent:
March 17, 2020
Assignee:
AstraZeneca AB
Inventors:
Bernard Christophe Barlaam, Daniel Hillebrand O'Donovan, Samantha Jayne Hughes, Thomas Andrew Moss, Johannes Wilhelmus Maria Nissink, James Stewart Scott, Bin Yang
Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of Cezanne 1 and ubiquitin C-terminal hydrolase 30 or Ubiquitin Specific Peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of cancer. Compounds of the invention include compounds having the formula (I): pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c, R1d, R1e, R1f and A are as defined herein.
Abstract: A process for preparing (3R)-3-[2-Hydroxy(di-2-thienyl)acetoxy]-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide) comprises reacting 2-hydroxy-2,2-dithien-2-ylacetic acid 1-azabicyclo[2.2.2]oct-3(R) yl methyl ester and 3-phenoxypropyl bromide, wherein the reaction takes place in a solvent or mixture of solvents selected from the group of amides and/or the group of solvents with a sulfoxide group. Also provided is a crystalline aclidinium bromide characterized by a powder XRPD pattern having peaks at 7.7±0.2° 2?, 10.4±0.2° 2?, 13.2±0.2° 2?, 13.8±0.2° 2?, 19.9±0.2° 2?, 20.3±0.2° 2?, 20.8±0.2° 2?, 24.2±0.2° 2?, 25.7±0.2° 2?, 26.1±0.2° 2?, 29.2±0.2° 2?, 30.8±0.2° 2?. A pharmaceutical composition comprises aclidinium bromide according to the invention and a pharmaceutically acceptable excipient.
Type:
Grant
Filed:
August 28, 2018
Date of Patent:
March 17, 2020
Assignee:
Hovione Scienta Limited
Inventors:
Zita Mendes, Constança Cacela, Ana Carina Constantino, Bruno Santos
Abstract: The invention relates to a process for the manufacture of diastereomerically and enantiomerically enriched triazole compounds isavuconazole and ravuconazole, comprising a Reformatsky reaction between a ketone and a 2-halozincpropionate ester, followed by a resolution step, preferably an enzymatic resolution with an esterase enzyme.
Type:
Grant
Filed:
September 11, 2017
Date of Patent:
March 17, 2020
Assignee:
Basilea Pharmaceutica AG
Inventors:
Ruben Van Summeren, Harrie Vaessen, Daniel Mink, Mario Waser
Abstract: The present invention relates to the tromethamine salt of (1R,3S)-3-(5-cyano-4-phenyl-1,3-thiazol-2-ylcarbamoyl)cyclopentane carboxylic acid, a process for obtaining said salt, combination products and pharmaceutical compositions comprising said salts and their medical uses, in particular for the treatment or prevention of diseases known to ameliorate by A1 adenosine receptor antagonism.
Type:
Grant
Filed:
March 6, 2018
Date of Patent:
March 10, 2020
Assignee:
PALOBIOFARMA, S.L.
Inventors:
Julio Castro Palomino Laria, Juan Camacho Gómez
Abstract: A method for treating a lysophosphatidic acid-dependent disease or condition in a subject in need thereof is provided. The method includes administering to the subject a therapeutically effective amount of a heterocyclic compound. The heterocyclic compound is a lysophosphatidic acid receptor ligand. Lysophosphatidic acid-dependent diseases and conditions include diseases involving fibrosis, such as fibrosis of the heart, kidney, liver and lung, and scleroderma; inflammatory diseases such as diabetic nephropathy and inflammatory bowel disease; ocular diseases such as diseases involving retinal degeneration; nerve diseases such as pruritus and pain.
Type:
Grant
Filed:
June 5, 2018
Date of Patent:
February 25, 2020
Assignee:
EPIGEN BIOSCIENCES, INC.
Inventors:
Graham Beaton, Fabio C. Tucci, Satheesh B. Ravula, Chandravadan R. Shah, Hiep Luu
Abstract: The invention disclosed herein is directed to compounds of Formula I and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, colon, pancreatic, chronic lymphocytic leukemia, melanoma and other cancers comprising administration of a therapeutically effective amount of a selective PPAR? antagonist.
Type:
Grant
Filed:
May 9, 2017
Date of Patent:
February 25, 2020
Assignee:
TEMPEST THERAPEUTICS, INC.
Inventors:
Nicholas Simon Stock, Austin Chih-Yu Chen, Yalda Mostofi Bravo, Jason Duarte Jacintho, Jill Melissa Baccei, Brian Andrew Stearns, Ryan Christopher Clark
Abstract: The invention relates to salts of Compound 1, crystalline forms thereof, methods of their preparation, pharmaceutical compositions thereof and methods of their use.
Type:
Grant
Filed:
July 19, 2019
Date of Patent:
February 18, 2020
Assignee:
PRAXIS PRECISION MEDICINES, INC.
Inventors:
Nelson B. Olivier, Kiran Reddy, Gabriel Martinez Botella, Magnus Ronn, Paul A. Laskar
Abstract: The present invention provides compounds having the general structural formula (I) (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.
Abstract: A crystalline form of (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide is disclosed. The crystalline form has a diffraction peak when a diffraction angle, 2?, is 16.66±0.2°, 17.54±0.20, 21±0.2°, 22.16±0.20, or 30.96±0.20. The crystalline form can be dissolved quickly in water with a solubility greater than or equal to 90 mg/mL, features high bioavailability, has high stability at high temperature, is suitable for preparing multiple pharmaceutical compositions, and can prepare multiple formulations, such as tablets, capsules, dripping pills, sustained-release and controlled-release formulations, and lyophilized powder for injection. The method for preparing the crystalline form is carried out under a mild condition, is easy to operate, introduces a few impurities, and features good reproducibility, an easy-to-control production process and high safety, and is suitable for industrial production.
Type:
Grant
Filed:
July 7, 2017
Date of Patent:
February 11, 2020
Assignee:
CHONGQING RUZER PHARMACEUTICAL COMPANY LIMITED
Abstract: A compound of Formula I is provided: or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula I.
Type:
Grant
Filed:
August 4, 2016
Date of Patent:
January 28, 2020
Assignees:
Pfizer Inc., iTeos Therapeutics
Inventors:
Sacha Ninkovic, Michael Raymond Collins, Stefano Crosignani, Andreas Maderna, Indrawan James McAlpine, Stephanie Anne Scales, Martin Wythes