Abstract: Disclosed herein are compositions and methods for the treatment of pulmonary hypertension, including pulmonary arterial hypertension. The methods include administering to a patient in need thereof an effective amount of anagrelide or derivative thereof. The compositions include an effective amount of anagrelide or derivative thereof, in some instances combined with one or more additional agents for the treatment of pulmonary hypertension.
Abstract: Disclosed herein is a method for producing silica gel-immobilized phosphonium salt catalysts including the steps of (a) reacting a silane compound with a silica gel in the presence of xylene, to obtain a catalyst precursor having a haloalkyl group or a haloaryl group, wherein the silane compound has a haloalkyl group or a haloaryl group, and a proportion of the silane compound is from 0.001 to 0.
Type:
Grant
Filed:
April 22, 2014
Date of Patent:
July 3, 2018
Assignees:
MARUZEN PETROCHEMICAL CO., LTD., National Institute of Advanced Industrial Science and Technology
Abstract: The present invention provides a method for producing an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, and an intermediate thereof. A method for producing an atropisomer of a pyrrole derivative using a compound represented by (B) [wherein R1 represents a C1-C4 alkyl group, and R2 represents a 2-hydroxyethyl group or a carboxymethyl group] as a production intermediate.
Type:
Grant
Filed:
September 8, 2017
Date of Patent:
June 26, 2018
Assignee:
Daiichi Sankyo Company, Limited
Inventors:
Masashi Watanabe, Hiroshi Nagasawa, Noritada Sato
Abstract: The present invention relates to a method for preparing a curable bicyclic compound derived from biomass. The method includes preparing starting materials furan and methyl acrylate by preparing furan from hemicellulose extracted from biomass, and methyl acrylate from glycerol generated from biomass, preparing an intermediate compound comprising a bicycle and an alcohol functional group by reacting the furan and the methyl acrylate through a Diels-Alder reaction and consecutive reduction, and preparing a curable bicyclic compound that includes the bicycle and an epoxide functional group by reacting the intermediate compound and epichlorohydrin.
Type:
Grant
Filed:
July 28, 2016
Date of Patent:
June 12, 2018
Assignee:
Korea Institute of Industrial Technology
Inventors:
Jin-Ku Cho, Sang-Yong Kim, Do-Hoon Lee, Bo-Ra Kim, Baek-Jin Kim, Jae-Won Jung, Sang-Hyeup Lee, Jae-Soung Lee
Abstract: The technology described herein relates to dimethyl boronate esters of the following formula for the treatment of cancers expressing abnormally high levels of SREBP1:
Abstract: The present invention is directed to process for preparation of ?-form crystal of Mirabegron, (R)-2-(2-aminothiazol-4-yl)-N-(4-(2-((2-hydroxy-2-phenylethyl) amino) ethyl) phenyl) acetamide of formula (1).
Abstract: Chiral oligomeric pentenoate amides are bio-oligomer mimetics possessing a high degree of conformation rigidity. Conformational rigidity is desirable in the design of molecules with high affinities for biological receptors and enzymes. Libraries of such oligomeric mimetics, such as of chiral oligomeric pentenoate amides can be used to probe biological systems. The present invention provides a method for preparation of chiral oligomeric pentanoate amides comprising conversion of a chiral oxazolidinone (4) to a chiral monomer of formula (1) which can be oligomerized to a chiral compound of formula (12) and so forth.
Type:
Grant
Filed:
September 7, 2012
Date of Patent:
May 8, 2018
Assignee:
The Scripps Research Institute
Inventors:
Glenn C. Micalizio, Thomas Kodadek, Mohosin Sarkar
Abstract: A method for the preparation of compounds of formula (I), for example, N-methyl-3-difluoromethyl-5-fluorpyrazole aldehyde, starting from compounds of formula (II), for example, N-methyl-3-haloalkyl-5 chloropyrazole aldehyde, comprising simultaneous fluorination (one step process) of haloalkyl group in position 3 and replacing haloatom in position 5 by fluorine.
Abstract: The present invention discloses a process for the preparation of Iopamidol of formula (II) and comprising the following steps: a) reacting the Compound (I) wherein X is OR2 or R3, and wherein R2 and R3 are a Ci-C6 linear or branched alkyl, C3-C6 cycloalkyl, C6 aryl, optionally substituted with a group selected from the group consisting of methyl, ethyl, n-propyl, i-propyl, n-butyl, sec-butyl, t-butyl and phenyl, with the acylating agent (S)-2-(acetyloxy)propanoyl chloride in a reaction medium to provide the acetyloxy derivative of Compound (I); b) hydrolyzing the intermediate from step a) with an aqueous solution at a pH comprised from 0 to 7, by adding water or a diluted alkaline solution such as sodium hydroxide or potassium hydroxide, freeing the hydroxyls from the boron-containing protective groups, obtaining the N—(S)-2-(acetyloxy)propanoyl derivative of Compound (II); c) alkaline hydrolysis to restore the (S)-2-(hydroxy)propanoyl group and to obtain Iopamidol (II) and optional recovery of the boron deri
Abstract: A cannabidiol extraction and conversion process includes an extraction process including a sizing unit wherein raw Cannabis plant material is reduced to a uniform size, a blending unit wherein an extraction solvent is blended together with the Cannabis plant material to form an initial extract, and a primary solvent exchange rotary evaporator unit wherein an exchange solvent is added to the initial extract, and a processed extract rich in cannabidiol is obtained. A conversion process includes a conversion rotary reflux unit wherein the processed extract is combined and processed with an acidic component, a separator unit wherein a solvent is added and a separator organic effluent is obtained, a secondary solvent exchange rotary evaporator unit wherein a further solvent is added, and a fractionation unit wherein the tetrahydrocannabinol obtained is separated into a plurality of functional fractions for selective blending.
Abstract: The present invention relates to Saroglitazar free acid of Formula (IA) or its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable esters, stereoisomers, tautomers, analogs and derivatives thereof. The present invention also provides an amorphous form of saroglitazar free acid and processes of preparation thereof. The present invention also provides pharmaceutical composition comprising an amorphous form saroglitazar magnesium.
Abstract: The invention relates to novel chemical entities that act as thromboxane (TX) A2 receptor, or T prostanoid receptor (TP), antagonists and to their use in the treatment of human diseases in which thromboxane (TX) A and of all other agents that act as incidental ligands of TP, including the endoperoxide prostaglandin (PG)G2/PGH2, 20-hydroxyeicosatetraenoic acid (20-HETE) and the free-radical derived isoprostanes (e.g., 8-iso-prostaglandin (PG)F2?), play a role. Compounds of the invention preferably include a benzenesulfonyl urea in which the benzene is substituted by a substituted biphenylyloxy group (e.g., at the 2 position) and by a nitrile group (e.g., at the 5 position), which compounds show promising results as TP-isoform selective TP antagonists.
Type:
Grant
Filed:
June 13, 2016
Date of Patent:
April 3, 2018
Assignee:
UNIVERSITY COLLEGE DUBLIN, NATIONAL UNIVERSITY OF IRELAND, DUBLIN
Abstract: A novel vinyl-group-containing fluorene compound and a method for producing the same, a polymerizable monomer and cross-linking agent including this compound, a leaving-group-containing fluorene compound, a monovinyl-group-containing fluorene compound, and methods for producing the same. This vinyl-group-containing fluorene compound is represented by formula (1). In the formula, W1 and W2 represent a group represented by formula (2), a group represented by formula (4), a hydroxyl group, or a (meth)acryloyloxy group, R3a and R3b represent a cyano group, a halogen atom, or a monovalent hydrocarbon, and n1 and n2 are integers of 0-4. In formulas (2) and (4), a ring (Z) is an aromatic hydrocarbon ring, X is a single bond or a group represented by —S—, R1 is a single bond or a C1-4 alkylene group, R2 is a specific substituent group such as a monovalent hydrocarbon, and m is an integer of 0 or greater.
Type:
Grant
Filed:
March 28, 2014
Date of Patent:
February 27, 2018
Assignees:
TOKYO OHKA KOGYO CO., LTD., DAICEL CORPORATION
Abstract: The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided.
Abstract: Disclosed herein are compositions and methods of making phenolic compounds, and resins comprising these phenolic compounds. The compounds include multifunctional epoxies, amino glycidyl derivatives, and multi-functional amines prepared from hydroxymethyl derivatives of phenols and bisphenols.
Abstract: The invention relates to thiophosphates and derivatives thereof useful as antiwear additive components, lubricant additive compositions and lubricant compositions each comprising such compounds, methods for making and using the same, including methods of lubricating machines and machine parts and methods of extending the useful life of elastomeric seal components of such machines.
Type:
Grant
Filed:
October 10, 2016
Date of Patent:
February 6, 2018
Assignee:
Afton Chemical Corporation
Inventors:
David Edwards, Kristine Durbin, Robert E. McCovick
Abstract: A composition and a process for straightening hair are disclosed. The process includes coating keratin fibers with a composition comprising a thermally-activated agent and contacting the coated keratin fibers with a heating device at a temperature of at least 185° C. for sufficient time to modify the keratin fibers. The thermally-activated agent comprises a heterocyclic compound containing two heteroatoms selected from nitrogen and oxygen in a 5 or 6-membered ring, such as a cyclic alkylene carbonate.