Abstract: The invention discloses an ifosfamide intermediate, a preparation method and application thereof. The ifosfamide intermediate has formula I. The ifosfamide intermediate reacts with a chlorinating agent, and then cyclization is performed under the action of an organic base to obtain ifosfamide. Compared with the existing synthetic routes, the method of the invention has the advantages that the use of highly toxic and explosive ethyleneimine can be avoided, and the use of explosive chemicals can be avoided.
Abstract: There are provided for herein novel amine-containing transfection compounds and methods for making and using same. The compounds are generally obtained by reacting a primary amine with an unsaturated compound. Transfection complexes made using the amine-containing transfection compounds in combination with additional compounds to encapsulate biologically active agents such as nucleic acids are also provided for herein. Methods of using the transfection complexes for the in vivo or in vitro delivery of biologically active agents are also described. The transfection complexes of the present invention are highly potent, thereby allowing effective modulation of a biological activity at relatively low doses compared to analogous transfection compounds known in the art.
Type:
Grant
Filed:
August 30, 2019
Date of Patent:
October 11, 2022
Assignee:
LIFE TECHNOLOGIES CORPORATION
Inventors:
Zhiwei Yang, Parul Angrish, Xavier de Mollerat du Jeu, Kristin Wiederholt
Abstract: The present invention relates to a method for preparing 4,4?-dihydroxy-[1,1?-biphenyl-3,3?-dicarboxylic acid], the method comprising a step for preparing a compound represented by chemical formula 1 by reacting a compound represented by chemical formula 2 with a base according to reaction formula 1. [reaction formula 1] [chemical formula 1] [chemical formula 2] According to the present invention, because use of additional carbon dioxide is unnecessary during the reaction, internal pressure is lowered during same, the reaction can be carried out at a lower temperature, the yield from the synthesis is notably improved as hardening of the resulting substance is absent, and H4dobpdc can be synthesized in large amounts as an additional process for obtaining pure ligands is unnecessary.
Type:
Grant
Filed:
April 30, 2019
Date of Patent:
October 11, 2022
Assignee:
Korea University Research and Business Foundation
Inventors:
Chang Seop Hong, Jong Hyeak Choe, Jeong Eun Kim
Abstract: A process for preparing azelaic acid is disclosed. In particular, the process for preparing azelaic acid is an ozone free process. The process for preparing azelaic acid comprises a step of decarboxylation of tetra-carboxylic acid in the presence of a organic sulfonic acid.
Abstract: Organophosphorus or organosulfur compounds and methods of using the compounds as cleaning agents, particle dispersants, or surfactants, or to remove, disperse or inhibit the growth of a biofilm, or inhibit the growth of, or kill a fungus or bacteria are provided.
Abstract: This invention belongs to the modern pharmaceutical field of Traditional Chinese Medicine, and relates to an herbal extract of Chinese Motherwort and its application in pharmacy, which specifically relates to the crystal structure of a Chinese Motherwort extract: Leonurine, and its application in the preparation of medicine. The chemical name of the above-mentioned Leonurine is 4-guanidino-1-)butyl 4-hydroxy-3,5-dimethoxybenzoate. The invention by specific methods prepares leonurine as 6 kinds of crystals with different crystal forms. Specifically, there are six different structures of leonurine sulfate crystals, two of them are hydrate, two are anhydrous crystal form, one is methanol solvate, one is ethanol solvate. The leonurine crystal forms of this invention can applicate in preparing medicine such as insulin sensitizer, hypoglycemic and lipid-lowering drugs.
Type:
Grant
Filed:
September 18, 2018
Date of Patent:
September 20, 2022
Assignee:
ZHUHAI HENGQIN NEW DISTRICT ZHONGZHU ZHENGTAI MEDICAL MANAGEMENT CO., LTD.
Abstract: The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route.
Type:
Grant
Filed:
June 25, 2019
Date of Patent:
September 6, 2022
Assignee:
Novartis AG
Inventors:
Florian Karl Kleinbeck-Riniker, Benjamin Martin, Gerhard Penn, Francesco Venturoni, Thierry Schlama, Thomas Ruch, Thomas Allmendinger, Bernhard Wietfeld, Paolo Filipponi
Abstract: The present invention relates to Form IV of fenofibrate and its preparation methods thereof. Its X-ray powder diffraction pattern expressed as 2? angle has characteristic peaks at 14.15±0.2°, 15.94±0.2°, 16.49±0.2°, 17.45±0.2°, 20.21±0.2°, and 22.87±0.2°. The present invention also provides preparation methods of Form IV. The preparation methods are simple, easy to operate, short, and have good repeatability. The methods are also non-toxic and non-polluting by using water as a medium and using a pharmaceutically accepted excipient, such as polyvinylpyrrolidone or polyvinyl alcohol as an inducer. The results of stability experiments (light exposure, high humidity and grinding) and solubility tests show that Form IV is stable and has a higher solubility than the prior art crystal form.
Abstract: The present disclosure is directed certain Hypoxia Inducible Factor 2? (HIF-2?) inhibitors and their use in the treatment of diseases mediated by HIF-2? such as cancer. Also provided is the use of HIF-2? inhibitors in combination with a poly (ADP-ribose) polymerase (PARP) inhibitor. In particular, the present disclosure is directed to methods for the treatment of cancers using a HIF-2? inhibitor in combination with a PARP inhibitor and pharmaceutical compositions comprising the same.
Abstract: Method of making a second olefin using a first olefin, comprising steps (A) and (B): (A) performing a metathesis reaction with the first olefin in the presence of a metal complex configured to catalyse said metathesis reaction; (B) epoxidizing an olefin contained in the reaction mixture obtained in step (A) to form an epoxide; and deoxygenizing said epoxide to form said second olefin.
Type:
Grant
Filed:
May 30, 2018
Date of Patent:
August 23, 2022
Assignee:
Verbio Vereinigte BioEnergie AG
Inventors:
Georg Frater, Agota Bucsai, Krisztian Lorincz
Abstract: This invention includes fusogenic compounds, and compositions and methods of use thereof. The fusogenic compounds can be used for making nanoparticle compositions for use in biopharmaceuticals and therapeutics. More particularly, this invention relates to compounds, compositions and methods for providing nanoparticles to incorporate or encapsulate active agents, to deliver and distribute the active agents to cells, tissues, organs, and subjects.
Type:
Grant
Filed:
November 6, 2018
Date of Patent:
August 16, 2022
Assignee:
Nitto Denko Corporation
Inventors:
Kwok Yin Tsang, Bharat Majeti, John Gaudette, Roger Adami, Hao Bai, Wenbin Ying
Abstract: The invention provides methods of preparing 8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid and methods of making a pharmaceutical material comprising a purified amount of 8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid. Also provided are compositions and pharmaceutical materials including a purified amount of 8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid as well as methods of treating various diseases and conditions using the compositions and pharmaceutical materials.
Type:
Grant
Filed:
January 15, 2021
Date of Patent:
August 9, 2022
Assignee:
Esperion Therapeutics, Inc.
Inventors:
Richard Copp, Mohamed Abdelnasser, Christopher M. Cimarusti, Jonathan Lane, Michael Barkman, Rasidul Amin, Arthur John Cooper, Damodaragounder Gopal, Philipp Selig
Abstract: Disclosed herein are pharmaceutical salts of a cationic protonated polyamine pharmaceutical agent and an anionic organic carboxylate which is hydrophobic when in protonated form, particularly suited for oral administration, where these salts have good bioavailability in solid dosage forms and may be used in the treatment of cancer and other medical conditions for which the pharmaceutical agent is intended.
Abstract: A compound having Formula I or its derivative may inhibit metallo-beta-lactamases. An investigation studying the effects of the compounds was provided by the invention of the activities of all subclasses (B1, B2, and B3) metallo-beta-lactamases. The compounds can be used for a pharmaceutical product with the ability to restore an anti-bacterial activity of a beta-lactam antibiotic, thereby treating and preventing a bacterial infection in an animal or human subject.
Type:
Grant
Filed:
November 21, 2019
Date of Patent:
July 26, 2022
Assignee:
MYONGJI UNIVERSITY INDUSTRY AND ACADEMIA COOPERATION FOUNDATION
Inventors:
Sang Hee Lee, Jung Hun Lee, Jeong Ho Jeon
Abstract: An acrylated and/or methacrylated urethane oligomer obtained by reaction of a specific polyamine with a cyclic carbonate compound carrying m cyclic carbonate groups, giving an intermediate product carrying m formed urethane groups which carry residual reactive amine —NH— groups, and subsequently an addition reaction of each of the residual reactive amine groups of the intermediate product with an acrylate group of a compound carrying, in addition to the acrylate group, p additional acrylate and/or methacrylate groups, with each residual reactive amine —NH— group of the intermediate product being thus converted into a carbon-nitrogen bond carrying the acrylate and/or methacrylate groups, and thus production of the urethane oligomer, with the urethane oligomer carrying m urethane groups and m hydroxyl groups and having a functionality in acrylates and/or methacrylates ranging from m*p(n?1) to m*p(2n?2).
Type:
Grant
Filed:
October 13, 2015
Date of Patent:
July 26, 2022
Assignee:
Arkema France
Inventors:
Guillaume P. Monnier, Catherine M. Leroy
Abstract: A method of forming a probe, wherein the method includes converting cholenic acid into a compound with a terminal alkyne group, wherein the converting the cholenic acid comprises using a sequence, wherein the sequence comprises synthesizing a THP-protection group, LiAlH4 reduction, Dess-Martin oxidation, and Seyferth-Gilbert-Bestmann homologation. The method additionally includes forming A-Chol by removing the THP-protection. Further, the method includes forming PhA-Chol from the compound with the terminal alkyne group via a palladiumcatalyzed Sonogashira reaction. Additionally, the method includes forming PhDY Chol from the compound with the terminal alkyne group via a coppercatalyzed Cadiot-Chodkiewicz reaction.