Abstract: The present invention provides a process for preparing a compound represented by formula (VII), which comprises reacting a compound represented by formula (VI) with a malonic acid derivative in the presence of a base and an asymmetric catalyst in a two layer solvent system of hydrophobic solvent and water. (wherein R2 and R3 each independently represents a protecting group for carboxyl group).
Abstract: The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I): wherein X, Y, Z, R1, R2, R4 and R7 are defined herein.
Type:
Grant
Filed:
May 12, 2020
Date of Patent:
August 10, 2021
Assignee:
FORMA Therapeutics, Inc.
Inventors:
Kenneth W. Bair, Torsten Herbertz, Goss S. Kauffman, Katherine J. Kayser-Bricker, George P. Luke, Matthew W. Martin, David S. Millan, Shawn E. R. Schiller, Adam C. Talbot, Mark J. Tebbe
Abstract: The present invention relates to the use of one or more particular dihydroisoquinolinium salts of formula (I) for treating keratin materials, in particular keratin fibres, especially human keratin fibres such as the hair. The invention also relates to a process for treating keratin materials using said salts and optionally one or more chemical oxidizing agents. A subject of the invention is also a composition for lightening keratin materials, comprising one or more dihydroisoquinolinium salts and one or more chemical oxidizing agents. The present invention also relates to one or more particular dihydroisoquinolinium salts and also to compositions containing them, in particular compositions comprising a physiologically acceptable medium.
Type:
Grant
Filed:
December 23, 2016
Date of Patent:
August 10, 2021
Assignee:
L'OREAL
Inventors:
Stéphane Sabelle, Aziz Fadli, Alexandra Charrier
Abstract: A first aspect of the invention relates to betahistine, or a pharmaceutically acceptable salt thereof, and a monoamine oxidase inhibitor, for use in the treatment or prevention of one or more symptoms of vertigo in a subject. A second aspect of the invention relates to a method of treating or preventing one or more symptoms of vertigo in a subject, said method comprising administering to the subject (i) betahistine, or a pharmaceutically acceptable salt thereof, and (ii) a monoamine oxidase inhibitor.
Abstract: The invention provides novel compounds having the general formula I: wherein R1, R2, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.
Abstract: 2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK.
Type:
Grant
Filed:
January 29, 2020
Date of Patent:
July 20, 2021
Assignee:
Janssen Pharmaceutica NV
Inventors:
Philippe Fernandes, Paul J. Krawczuk, Mark S. Tichenor
Abstract: The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (II) or a pharmaceutically acceptable sat thereof, wherein R1, R2, R3, R4, R5, R8, R9, R10, R12, Z, Y and m are as defined herein.
Type:
Grant
Filed:
May 22, 2019
Date of Patent:
July 20, 2021
Assignee:
Mission Therapeutics Limited
Inventors:
Alison Jones, Mark Kemp, Martin Stockley, Karl Gibson, Gavin Whitlock
Abstract: A condensed cyclic compound represented by Formula 1: Ar1-L1-Ar2??Formula 1 wherein, in Formula 1, Ar1, Ar2, and L are the same as described in the specification.
Abstract: The present invention provides compositions and methods of use for treating, preventing, or ameliorating a disease, disorder, or condition associated with a chemokine receptor such as CXCR4.
Abstract: Disclosed in the present invention are a compound as shown in formula (II), a tautomer or a pharmaceutically acceptable salt thereof, and also disclosed is the use thereof in preparing a drug for treating an ASK1-associated disease.
Type:
Grant
Filed:
January 22, 2018
Date of Patent:
June 22, 2021
Inventors:
Chengde Wu, Tao Yu, Ning Li, Shuhui Chen
Abstract: The present invention relates to novel compounds, particularly to compounds comprising a photoactive unit, said novel compounds being particularly suitable for compositions and ophthalmic devices as well as to compositions and ophthalmic devices comprising such compounds.
Type:
Grant
Filed:
February 14, 2018
Date of Patent:
June 22, 2021
Assignee:
Merck Patent GmbH
Inventors:
Lars Dobelmann-Mara, Stefan Riedmueller, Martin Schraub
Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
Type:
Grant
Filed:
December 30, 2019
Date of Patent:
June 8, 2021
Assignee:
Aerie Pharmaceuticals, Inc.
Inventors:
Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
Abstract: The invention relates to a process for the synthesis of 6-chloromethyluracil (6-(chloromethyl)pyrimidin-2,4(1H,3H)-dione) from ethyl 4-chloroacetoacetate and S-methylisothiourea hemisulfate via isolation of the novel intermediate 6-(chloromethyl)-6-hydroxy-2-(methylthio)-5,6-dihydropyrimidin-4(1H)-one, and its subsequent treatment with aqueous sulfuric acid. Formula (I).
Type:
Grant
Filed:
February 13, 2019
Date of Patent:
June 8, 2021
Assignee:
Procos S.P.A.
Inventors:
Fabio Morana, Stefano Gobbato, Jacopo Roletto, Paolo Paissoni
Abstract: Provided herein are methods and compositions for treating cancers, inflammatory diseases, rasopathies, and fibrotic disease involving aberrant Ras superfamily signaling through the binding of compounds to the GTP binding domain of Ras superfamily proteins including, in certain cases, K-Ras and mutants thereof, and a novel method for assaying such compositions.
Type:
Grant
Filed:
April 13, 2020
Date of Patent:
June 8, 2021
Assignee:
Shy Therapeutics LLC
Inventors:
Yaron R. Hadari, Luca Carta, Michael Schmertzler, Theresa M. Williams, Charles H. Reynolds, Rebecca Hutcheson
Abstract: The present invention relates to a novel brominated furanone derivative, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient, wherein the novel brominated furanone derivative or a pharmaceutically acceptable 5 salt thereof according to the present invention exhibits a quorum sensing inhibitory activity of bacteria and also can effectively inhibit the formation of biofilm of bacteria, and thus can be used as a pharmaceutical composition containing the same as an active ingredient, thereby having an effect of being useful, 10 for example, for periodontal diseases such as gingivitis and periodontitis, oral diseases, and the like.
Type:
Grant
Filed:
June 13, 2017
Date of Patent:
June 1, 2021
Assignee:
Seoul National University R&DB Foundation
Inventors:
Byeong Moon Kim, Bong Kyu Choi, Jae Hyun Sim, Eun Ju Ryu, Ji Su Park, Il Hak Bae
Abstract: The present invention is directed to 5-fluoro-C-(aryl or heterocyclyl)-glycoside derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by SGLT activity, more particularly dual SGLT1/2 activity.
Abstract: Methods of synthesizing and isolating facial-tris-homoleptic phenylpyridinato iridium (III) photocatalysts are disclosed. Also disclosed are methods of recovering excess 2-phenylpyridine ligands from said syntheses.
Type:
Grant
Filed:
March 6, 2018
Date of Patent:
May 25, 2021
Assignee:
The Board of Regents for Oklahoma State University
Inventors:
Jimmie Dean Weaver, Kip Allen Teegardin
Abstract: Provided herein are methods and compositions for treating cancers, inflammatory diseases, rasopathies, and fibrotic disease involving aberrant Ras superfamily signaling through the binding of compounds to the GTP binding domain of Ras superfamily proteins including, in certain cases, K-Ras and mutants thereof, and a novel method for assaying such compositions.
Type:
Grant
Filed:
October 16, 2019
Date of Patent:
May 11, 2021
Assignee:
Shy Therapeutics LLC
Inventors:
Yaron R. Hadari, Luca Carta, Michael Schmertzler, Theresa M. Williams, Charles H. Reynolds, Rebecca Hutcheson