Abstract: The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV and formula V and the methods for the treatment of xerostomia may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of oral mucosal inflammatory, dry mouth or oral dry mouth mediated infectious diseases.
Abstract: Aspects of the present disclosure generally relate to compounds for targeting and healing bone fractures. Some of these compounds include a negatively charged oligopeptide comprising an acidic oligopeptide, a linker, which may be hydrolyzable or may be a substrate for the protease cathepsin K, and at least one molecule that promotes bone healing. In some compounds the molecule that promotes bone healing is an anabolic compound that inhibits GSK3?, in some compounds the molecule that promotes the healing of bone fracture is a pro-inflammatory agent such as PGE1. Other embodiments include methods of treating a bone fracture comprising administering a therapeutic amount of any one of the compounds disclosed herein.
Type:
Grant
Filed:
July 13, 2020
Date of Patent:
April 11, 2023
Assignees:
Purdue Research Foundation, University of Utah
Inventors:
Stewart Andrew Low, Philip S. Low, Christopher Galliford, Jindrich Kopecek, Jiyan Yang
Abstract: Provided are topical analgesic gel compositions having relatively high payloads of menthol and camphor by micro-emulsion technology and methods of preparing topical analgesic gel compositions having relatively high payloads of menthol and camphor. Topical analgesic gel compositions may include from 12 to 16 wt. % menthol; from 4 to 8 wt. % camphor; from 0.1 to 2 wt. % carbomer; and 60 to 70 wt. % solvent. Topical analgesic gel compositions can have a viscosity from 60,000 to 110,000 centipoise.
Type:
Grant
Filed:
April 23, 2020
Date of Patent:
April 4, 2023
Assignee:
Bayer Healthcare LLC
Inventors:
Debanjan Das, Emanuel Vizzotti, Thomas Dann, Renee Nelson, Courtney C. Haynes, Soundarya Vaithianathan, Reginald Bradley, Reinhard Walter, Gerard Meisel
Abstract: The present disclosure relates to small molecule or polymer conjugated MetAP2 inhibitors. The present disclosure also relates to methods of treating, or ameliorating at least one symptom of metabolic dysfunction associated with a treatment in a subject having a disease, such as cancer. The present disclosure also relates to methods of treating, or ameliorating at least one symptom of cancer comprising administering a combination of a polymer conjugated MetAP2 inhibitors and at least one second agent wherein the second agent may induce metabolic dysfunction.
Abstract: The present disclosure relates to the technical field of organic photoelectric materials, in particular to an organic compound, an electronic component containing the organic compound, and an electronic device. The compound has a structure as shown by chemical formula 1?, wherein one of R1 to R4 is aa, and the other three are selected from substituents such as an alkyl, halogen and cyano; one of R5 to R8 is bb, and the other three are selected from substituents such as an alkyl, halogen and cyano; Y and Y1 are each independently cc; and L and L1 are a single bond, aryl, heteroaryl, etc. By using the organic compound of the present disclosure in an organic component, the driving voltage, luminous efficiency and lifespan of the organic component can be improved.
Type:
Grant
Filed:
October 16, 2020
Date of Patent:
March 21, 2023
Assignee:
SHAANXI LIGHTE OPTOELECTRONICS MATERIAL CO., LTD.
Abstract: An organic molecule is disclosed comprising: a first chemical moiety with a structure of formula I, and two second chemical moieties, each independently from another with a structure of formula II, wherein the first chemical moiety is linked to each of the two second chemical moieties via a single bond.
Abstract: This disclosure relates to methods of reducing itch in patients with atopic dermatitis and treating patients with atopic dermatitis by administering a topical 0.75% or 1.5% ruxolitinib cream two times per day.
Type:
Grant
Filed:
March 28, 2022
Date of Patent:
February 28, 2023
Assignee:
Incyte Corporation
Inventors:
Michael Kuligowski, Kang Sun, Michael Howell, May Grace E. Venturanza, Jim Lee
Abstract: The present invention provides a pharmaceutical combination comprising the EP4 antagonist of Formula (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)-benzoic acid or a pharmaceutically acceptable salt thereof and at least one immune checkpoint inhibitor, preferably the sodium salt of (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl) benzoic acid. A polymorphic form A of sodium salt of (R)-4-(1-(6-(4-(trifluoromethyl) benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)benzoate characterized by a powder XRD spectrum with peaks at values of the angle 2?+0.2° of 4.3, 5.0, 5.8, 6.4, 7.1, 8.3, 8.7, 12.8, 15.3, 15.9 is also described. The combination and the polymorphic form A are described for use in the treatment of tumours.
Type:
Grant
Filed:
April 8, 2020
Date of Patent:
February 28, 2023
Assignee:
ROTTAPHARM BIOTECH S.R.L.
Inventors:
Lucio Claudio Rovati, Antonio Giordani, Filippo Magaraci, Gianfranco Caselli, Tiziana Piepoli, Daniele Maggioni, Albino Bonazzi
Abstract: A compound represented by formula I or II. X represents a mono substituent on a benzene ring, and is selected from —H, —I, —Br, —Cl, —F, —CN, an amino, and a derivative thereof; R1 is a C2-10 alkyl, C2-10 alkyl substituted by cyclopropane or fluorine, except n-butyl; and M is an amine ion or metal ion.
Type:
Grant
Filed:
September 21, 2020
Date of Patent:
February 14, 2023
Assignee:
HENAN GENUINE BIOTECH CO., LTD.
Inventors:
Junbiao Chang, Jinfa Du, Kaikai Zhu, Kai Wang
Abstract: A method of preparing a 2,6 disubstituted anilines includes, reacting a 2-amino isophthalic acid diester with sufficient Grignard reagent R2CH2MgX to form the corresponding diol product, dehydrating the diol product to the corresponding dialkene; and hydrogenating the diol product to form the corresponding aniline. The 2,6 disubstituted anilines can be used to produce N-Heterocyclic Carbenes (NHCs). The NHCs can find application in various fields such as organic synthesis, catalysis and macromolecular chemistry. Palladium catalysts containing the NHCs are also described.
Abstract: A thermally activated delayed fluorescent molecular material, a synthesizing method therefor, and an electroluminescent device are provided. The thermally activated delayed fluorescent molecular containing an indenobenzoselenoheteroaromatic ring donor is synthesized, so that an electron donating ability of the donor is increased, and an non-radiative transition rate is effectively inhibited, thereby increasing photo-luminescence quantum yield (PLQY) of the molecule; and increasing the twist angle between the electron donor and the electron acceptor. Meanwhile, electron cloud overlapping between highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO) is reduced, thereby obtaining a smaller ?EST value. The organic electroluminescent device adopts the thermally activated delayed fluorescent molecular material prepared according to the synthesizing method, and thus has high luminous efficiency and long service life.
Type:
Grant
Filed:
October 24, 2019
Date of Patent:
January 10, 2023
Assignee:
WUHAN CHINA STAR OPTOELECTRONICS SEMICONDUCTOR DISPLAY TECHNOLOGY CO., LTD.
Abstract: The present invention relates to substituted 2-(morpholin-4-yl)-1,7-naphthyridine compounds of general formula (I) or (Ib), to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative disease as a sole agent or in combination with other active ingredients.
Type:
Grant
Filed:
August 21, 2020
Date of Patent:
December 20, 2022
Assignee:
Bayer Pharma Aktiengesellschaft
Inventors:
Lars Wortmann, Ulrich Lücking, Julien Lefranc, Hans Briem, Marcus Koppitz, Knut Eis, Franz Von Nussbaum, Benjamin Bader, Antje Margret Wengner, Gerhard Siemeister, Wilhelm Bone, Philip Lienau, Joanna Grudzinska-Goebel, Dieter Moosmayer, Uwe Eberspächer, Hans Schick
Abstract: Being used for drug modification, the multi-arm single molecular weight polyethylene glycol and an active derivative thereof provided herein can effectively improve the solubility, stability, and immunogenicity of the drugs, improve the absorption of the drugs in vivo, prolong the half-life of the drugs, and increase bioavailability, enhance efficacy, and reduce toxic and side effects of the drugs. A gel formed from the active derivative of the multi-arm single molecular weight polyethylene glycol provided herein can be used for the preparation of controlled release drugs so as to prolong the action time of the drugs, thereby reducing the number of administrations and improving patient compliance.
Abstract: Compositions and methods for the treatment of viral infections include conjugates containing inhibitors of viral neuraminidase (e.g., zanamivir, peramivir, or analogs thereof) linked to an Fc monomer, an Fc domain, and Fc-binding peptide, an albumin protein, or albumin-binding peptide. In particular, conjugates can be used in the treatment of viral infections (e.g., influenza viral infections).
Type:
Grant
Filed:
April 21, 2021
Date of Patent:
November 29, 2022
Assignee:
Cidara Therapeutics, Inc.
Inventors:
Allen Borchardt, Thomas P. Brady, Zhi-Yong Chen, Thanh Lam, Leslie W. Tari
Abstract: The present invention describes compounds and uses thereof in applications relating to absorption of electromagnetic energy. Preferred compounds are double bond-containing compounds capable of absorbing electromagnetic radiation energy and having improved properties.
Type:
Grant
Filed:
December 23, 2016
Date of Patent:
November 29, 2022
Assignee:
Commonwealth Scientific and Industrial Research Organisation
Abstract: This disclosure relates to methods of reducing itch in patients with atopic dermatitis and treating patients with atopic dermatitis by administering a topical 0.75% or 1.5% ruxolitinib cream two times per day.
Type:
Grant
Filed:
September 4, 2020
Date of Patent:
November 29, 2022
Assignee:
Incyte Corporation
Inventors:
Michael Kuligowski, Kang Sun, Michael Howell, May Grace E. Venturanza, Jim Lee
Abstract: The present disclosure belongs to the technical field of organic materials, and provides an organic compound. An adamantane spirofluorenyl and an anthryl are connected to obtain a novel compound for an organic electroluminescence device. In this compound, adamantane in the adamantane spirofluorene greatly increases the density of electron clouds on the fluorenyl through the hyperconjugation effect, which reduces the HOMO energy level of the compound and improves the hole migration ability. Both the adamantane spirofluorene and the anthryl have high hole mobility, so when the two are connected, the overall hole mobility of molecules is further improved, which is beneficial to reducing the working voltage of the device and improving the luminous efficiency. The present disclosure further provides an electronic component and an electronic apparatus including the compound. The organic compound can improve the performance of the electronic component.
Type:
Grant
Filed:
July 24, 2020
Date of Patent:
November 8, 2022
Assignee:
SHAANXI LIGHTE OPTOELECTRONICS MATERIAL CO., LTD.
Abstract: The invention relates to a crosslinking compound of formula (I) In particular, the present invention relates to a liquid composition comprising a monomer, a (meth)acrylic polymer and at least one crosslinking compound of formula (I). This liquid composition may be used in the form of a syrup and in particular in the form of a syrup for impregnating fibers or fibrous material. The invention also relates to a pseudo-thermoplastic material obtained after polymerization of the liquid composition being at least partially crosslinked. The invention also relates to a process for manufacturing such a liquid composition. The invention also relates to a process for impregnating a long-fiber fibrous substrate with said liquid composition. The invention also relates to a fibrous substrate impregnated with said liquid composition which is useful for manufacturing composite parts.
Abstract: Provided is a composition comprising a polyglycolized glyceride and a compound having the following structure (I): or a pharmaceutically acceptable salt thereof. Also provided are crystalline forms of the compound of structure (I), or a pharmaceutically acceptable salt thereof. Methods of making the same, and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated diseases, disorders or conditions are also disclosed.
Type:
Grant
Filed:
February 12, 2020
Date of Patent:
October 18, 2022
Assignee:
Sumitomo Pharma Oncology, Inc.
Inventors:
Steven L. Warner, Adam Siddiqui-Jain, Paul Flynn