Abstract: The present disclosure discloses a sterol derivative, a preparation method therefor and a use thereof. The sterol derivative includes a sterol compound with Structural Formula (I) or a pharmaceutically acceptable salt thereof, or an extract containing the sterol compound, or a composition containing the sterol compound, wherein Structural Formula (I) is as follows: where R1 is —OH, ?O, H or C1-C3 alkyl; R2 is —OH, H or C1-C3 alkyl; R3 is —OH, ?O, H or C1-C3 alkyl; R4 is —OH, H or C1-C3 alkyl, and at least one of R1, R2, R3 and R4 is —OH. The compound with Structural Formula (I) can be used for preparing a drug having inhibitory effect on 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity and the prepared drug can effectively inhibit the HMG-CoA reductase activity or be used for preparing an anti-cancer drug.
Type:
Grant
Filed:
February 4, 2013
Date of Patent:
October 9, 2018
Assignee:
BEIJING PEKING UNIVERSITY WBL BIOTECH CO., LTD.
Abstract: The present invention relates to long acting pharmaceutical compositions or pharmaceutically acceptable salts thereof, useful in the treatment or prevention of Human Immunodeficiency Virus (HIV) infections.
Abstract: This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.
Type:
Grant
Filed:
November 2, 2016
Date of Patent:
October 2, 2018
Assignees:
RESEARCH TRIANGLE INSTITUTE, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
Inventors:
Scott P. Runyon, Michael Rogawski, Edgar Cook, John Kepler, Hernan Navarro, Rafal Kaminski, Matthew Orr
Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.
Type:
Grant
Filed:
March 24, 2016
Date of Patent:
September 11, 2018
Assignee:
Tetraphase Pharmaceuticals, Inc.
Inventors:
Chi-Li Chen, Roger B. Clark, Yonghong Deng, Minsheng He, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Magnus P. Ronn
Abstract: The present invention relates to compounds characterized by having a structure according to the following Formula I: or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.
Abstract: In one aspect, the present invention provides novel derivatives of viridicatumtoxin of the formula wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof.
Type:
Grant
Filed:
July 22, 2015
Date of Patent:
September 4, 2018
Assignee:
WILLIAM MARSH RICE UNIVERSITY
Inventors:
Kyriacos C Nicolaou, Christopher R. H. Hale, Christian Nilewski, Heraklidia Ioannidou, Abdellatif El Marrouni
Abstract: Provided herein are multiple solid forms of a defined steroid-like compound, and methods for the preparation and use thereof. In one aspect, there is provided a crystalline form of said steroid-like compound, and methods for the preparation and use thereof. In another aspect, there is provided a substantially amorphous form of said steroid-like compound, and methods for the preparation and use thereof. In yet another aspect, there are provided compositions containing compounds according to the present invention. In certain aspects, such compositions are suitable for delivery of active agents according to the present invention to a subject in need thereof. In another aspect of the invention, there are provided methods for the treatment of a variety of indications, including glaucoma, ocular hypertension, and the like. In still another aspect of the present invention, there are provided kits containing compounds according to the present invention and/or compositions containing same.
Type:
Grant
Filed:
December 12, 2014
Date of Patent:
September 4, 2018
Assignee:
ALLERGAN, INC.
Inventors:
Shaoxin Feng, Scott W. Smith, Olivier M. G. Lambert, Suzanne M. Buttar
Abstract: Synthetic methods for preparing deoxycholic acid and intermediates thereof, high purity synthetic deoxycholic acid, compositions and methods of use are provided. Also, provided are processes for the synthesis of 12-keto or 12-?-hydroxysteroids from ?-9,11-ene, 11-keto or 11-hydroxy-?-steroids. This invention is also directed to novel compounds prepared during the synthesis. This invention is also directed to the synthesis of deoxycholic acid starting from hydrocortisone.
Type:
Grant
Filed:
May 23, 2017
Date of Patent:
June 26, 2018
Assignee:
Kythera Biopharmaceuticals, Inc.
Inventors:
Robert M. Moriarty, Achampeta Rathan Prasad, John Gregory Reid, Roy A. Swaringen, Jr.
Abstract: The present invention discloses a novel bile acid derivatives having substituted nitrogen functionality at C-11 and process for synthesis thereof. These C-11 substituted bile acid derivatives shows anticancer and antimycobacterial activity.
Type:
Grant
Filed:
November 24, 2014
Date of Patent:
June 19, 2018
Assignee:
Council of Scientific and Industrial Research
Abstract: The present invention relates to a pure polymorph of Nor-UDCA or Bis-nor-UDCA, or of a pharmaceutically acceptable salt thereof. The invention further provides a pharmaceutical composition comprising the polymorph of the invention, and a method for preparing the polymorph. The invention includes the pharmaceutical use of the polymorph or of the pharmaceutical composition of the invention.
Type:
Grant
Filed:
November 11, 2016
Date of Patent:
June 19, 2018
Assignee:
Dr. Falk Pharma GmbH
Inventors:
Rudolf Wilhelm, Markus Pröls, Erik Fischer, Heidi Waenerlund Poulsen
Abstract: The invention relates to processes for preparing 17-alkynyl-7-hydroxy-steroids, such as 17-Ethynyl-10R,13S-dimethyl 2,3,4,7,8R,9S,10,11,12,13,14S,15,16,17-hexadecahydro-1H-cyclopenta[a]phenanthrene-3R,7R,17S-triol (also referred to as 17?-ethynyl-androst-5-ene-3?,7?,17?-triol), that are essentially free of process impurities having binding activity at nuclear estrogen receptors.
Abstract: Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.
Type:
Grant
Filed:
March 28, 2017
Date of Patent:
June 5, 2018
Assignee:
Kythera Biopharmaceuticals, Inc.
Inventors:
Robert M. Moriarty, Nathaniel E. David, Nadir Ahmeduddin Mahmood
Abstract: The present invention relates to a cocrystal of progesterone and a coformer selected from the group consisting of vanillic acid, benzoic acid, salicylic acid, cinnamic acid, and vanillin. The present invention also relates to a pharmaceutical composition comprising a cocrystal of the present invention and at least one pharmaceutically acceptable carrier. The present invention further relates to a method of supplementing progesterone in women. This method involves administering to a female subject in need thereof a pharmaceutical composition of the present invention.
Type:
Grant
Filed:
October 25, 2016
Date of Patent:
May 29, 2018
Assignee:
AMRI SSCI, LLC
Inventors:
Ekaterina Albert, Patricia Andres, Melanie Janelle Bevill, Jared Smit, Jennifer Nelson
Abstract: The present invention relates to novel glucocorticoid compounds. The invention also relates to methods of using these compounds, the synthesis of these compounds, and to compositions and formulations comprising the glucocorticoid compounds, and uses thereof.
Type:
Grant
Filed:
September 25, 2014
Date of Patent:
May 22, 2018
Assignees:
VAN ANDEL RESEARCH INSTITUTE, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Inventors:
Huaqiang Eric Xu, Yuanzheng He, Karsten Melcher, Wei Yi, Jingjing Shi
Abstract: Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.
Type:
Grant
Filed:
November 11, 2016
Date of Patent:
April 24, 2018
Assignee:
Kythera Biopharmaceuticals, Inc.
Inventors:
Robert M. Moriarty, Nathaniel E. David, Nadir Ahmeduddin Mahmood
Abstract: Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, stroke (MELAS), or Kearns-Sayre Syndrome (KSS) are disclosed, as well as compounds useful in the methods of the invention. Methods and compounds useful in treating other disorders are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.
Type:
Grant
Filed:
December 29, 2015
Date of Patent:
April 3, 2018
Assignee:
BioElectron Technology Corporation
Inventors:
Guy M. Miller, Sidney M. Hecht, Orion D. Jankowski, Kieron E. Wesson, Paul Mollard
Abstract: The present invention relates to compounds of the formula (I) wherein Ar1 and Ar2 are as described in the description and to their use as pharmaceuticals for the treatment of sundown syndrome. The invention also relates to the preparation of such compounds and of pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
December 3, 2014
Date of Patent:
March 13, 2018
Assignee:
IDORSIA PHARMACEUTICALS LTD
Inventors:
Christoph Boss, Catherine Roch, Christine Brotschi, Markus Gude, Bibia Heidmann, Francois Jenck, Thierry Sifferlen, Michel Steiner, Jodi T. Williams
Abstract: The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, Alzheimer's disease), as well as methods of treating these diseases.
Type:
Grant
Filed:
April 1, 2013
Date of Patent:
March 6, 2018
Assignee:
Agency for Science, Technology and Research
Abstract: The invention relates to a method for obtaining and purifying phytosterols and/or tocopherols from distillation residue from a transesterification of vegetable oils, in particular from the vegetable oil-based fatty acid methyl ester production for the field of use of biodiesel (FAME), comprising a first transesterification stage for converting partial glycerides contained in the distillation residue; separating the glycerin phase from a reaction mixture resulting from the first transesterification stage; a second transesterification stage for converting sterol esters contained in the reaction mixture; adding water to the reaction mixture after the second transesterification stage in order to generate a multiphase system; simultaneously or sequentially separating the phases of the multiphase system into a substantially sterol-containing phase; a substantially glycerin- and methanol-containing aqueous phase; and a tocopherol-containing methyl ester phase; and obtaining phytosterols from the sterol-containing ph
Type:
Grant
Filed:
November 2, 2011
Date of Patent:
February 6, 2018
Assignee:
VERBIO VEREINIGTE BIOENERGIE AG
Inventors:
Joachim Lemp, Nico Baade, Emanuel Pöhls