Abstract: The present invention provides a compound represented by General Formula (I). The compound according to the present invention prevents the liquid crystal composition from being deteriorated due to light, has high compatibility with the liquid crystal composition, and does not impair the storage stability of the liquid crystal composition, thus the compound is useful as a constituent member of a liquid crystal composition. Since the liquid crystal composition and the liquid crystal display element containing the compound of the present invention exhibit UV resistance and have a high VHR, it is possible to obtain a liquid crystal display element with excellent display quality in which display defects such as burn-in and display unevenness do not occur or are suppressed.
Abstract: The present invention relates to substituted xanthine derivatives, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment of conditions having an association with TRPC5 containing ion channels.
Type:
Grant
Filed:
July 10, 2018
Date of Patent:
June 25, 2019
Assignees:
Boehringer Ingelheim International GmbH, Hydra Biosciences, Inc.
Inventors:
Kai Gerlach, Christian Eickmeier, Achim Sauer, Stefan Just, Bertrand L. Chenard
Abstract: The invention relates to a novel process for the preparation of rac-6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide (I) in pharmaceutically acceptable polymorphic form, through the conversion of a 3-bromo-2-oxo-cyclohexanecarboxylic acid alkyl ester into 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxylic acid alkyl ester, which in turn is processed to yield the final product.
Type:
Grant
Filed:
April 20, 2016
Date of Patent:
June 25, 2019
Assignee:
AOP ORPHAN PHARMACEUTICALS AG
Inventors:
Enrica Diodato, Katia Marcucci, Russell Thomas, Paul Wiedenau, Martin Rettig, Huw Roberts
Abstract: The present invention is concerned with derivatives of 3,5-diphenyl-diazole compounds, which are effective therapeutic agents for use in treating diseases linked to protein aggregation and/or neurodegenerative diseases such as Alzheimer's disease (AD), Parkinson's disease (PD), and Transmissible spongiform encephalopathies (TSEs) such as Creutzfeldt-Jakob disease (CJD). The therapeutic effect is caused by the inhibition of the protein aggregation in the affected tissue, such as the brain. 3,5-Diphenyl-diazole derivatives have been shown to be effective in inhibiting aggregation of proteins but are also characterized by their poor solubility in aqueous solutions. The prodrugs of the invention are modified 3,5-diphenyl-diazole derivatives, which are characterized by their improved solubility in aqueous solutions, and by their increased bioavailability.
Type:
Grant
Filed:
December 14, 2016
Date of Patent:
June 4, 2019
Assignee:
Max-Planck-Gesellschaft zur Forderung
Inventors:
Armin Giese, Felix Schmidt, Christian Griesinger, Andrei Leonov, Sergey Ryazanov
Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.
Type:
Grant
Filed:
May 6, 2015
Date of Patent:
May 28, 2019
Assignee:
Bristol-Myers Squibb Company
Inventors:
Xiang-Yang Ye, Bruce A. Ellsworth, Elizabeth A. Jurica
Abstract: A breast cancer therapeutic agent containing 5?-hydroxy-5-nitro-indirubin-3?-oxime as active ingredient has been disclosed. Further, a breast cancer therapeutic agent containing 5?-hydroxy-5-nitro-indirubin-3?-oxime as cyclin-dependent kinase (CDK) inhibitor, wherein said breast cancer is triple negative breast cancer (TNBC) and/or an estrogen receptor (ER) positive breast cancer including the tamoxifen-resistant estrogen receptor (ER) positive breast cancer has been disclosed.
Type:
Grant
Filed:
May 15, 2017
Date of Patent:
May 14, 2019
Assignee:
ANYGEN CO., LTD.
Inventors:
Jae il Kim, Seon-Myung Kim, San Ho Kim, Moon Young Park
Abstract: The present invention relates to novel processes for the preparation of apremilast of formula I, or a pharmaceutically acceptable salt thereof.
Abstract: The invention relates to a combination of two or more pharmaceutically active substances, of which at least one is a metabolic product (“metabolite”) of the other (“parent substance”), wherein in particular the dosages thereof are selected such that genotypically or phenotypically related variability in the conversion of the parent substance to the metabolite in particular individuals is compensated for.
Type:
Grant
Filed:
May 27, 2013
Date of Patent:
May 14, 2019
Assignee:
BAYER AKTIENGESELLSCHAFT
Inventors:
Stefan Willmann, Thomas Eiβing, Kristin Dickschen
Abstract: An organic light-emitting device having a light-emitting layer containing a compound represented by the general formula below has a high light emission efficiency. In the general formula, at least one of R1 to R5 represents a cyano group, at least one of R1 to R5 represents a 9-carbazolyl group, a 1,2,3,4-tetrahydro-9-carbazolyl group, a 1-indolyl group or a diarylamino group, and the balance of R1 to R5 represents a hydrogen atom or a substituent.
Abstract: A derivative of inula lineariifolia lactone A, and in particular, a dimethylamine 4-O-acetyl inula lineariifolia lactone A or a salt thereof, preparation of same, and an application of same in preparation of medicine for treating multiple sclerosis.
Type:
Grant
Filed:
August 31, 2016
Date of Patent:
April 30, 2019
Assignee:
Shanxi Zhendong Leading Biotechnology Co., Ltd.
Inventors:
Weidong Zhang, Qingyan Sun, Minghua Li, Baohua Yang
Abstract: A novel substance with which an increase in life and emission efficiency of a light-emitting element can be achieved is provided. A carbazole compound having a structure represented by General Formula (G1) is provided. Note that a substituent which makes the HOMO level and the LUMO level of a compound in which a bond of the substituent is substituted with hydrogen deep and shallow, respectively is used as each of substituents in General Formula (G1) (R1, R2, Ar3, and ?3). Further, a substituent which makes the band gap (Bg) and the T1 level of a compound in which a bond of the substituent is substituted with hydrogen wide and high is used as each of the substituents in General Formula (G1) (R1, R2, Ar3, and ?3).
Type:
Grant
Filed:
February 17, 2017
Date of Patent:
April 16, 2019
Assignee:
Semiconductor Energy Laboratory Co., Ltd.
Abstract: A method of treating a bacterial infection in a subject in need thereof includes administering to the subject therapeutically effective amounts of at least one ?-lactam antibiotic and at least one bisthiazolidine metallo-?-lactamase inhibitor.
Type:
Grant
Filed:
March 20, 2017
Date of Patent:
April 9, 2019
Assignee:
CASE WESTERN RESERVE UNIVERSITY
Inventors:
Robert Bonomo, Alejandro Jose Vila, S. Graciela Mahler
Abstract: A process for preparing one or more carbazoles comprising (a) contacting one or more compounds represented by formula (1) below with diboron reagents in the presence of PdCl2(dppf) to form one or more 2,2?-dichlorobiaryl represented by formula (2) below; and (b) contacting the one or more 2,2?-dichlorobiaryls with one or more H2N—Y compounds, in the presence of one or more palladium containing catalytic components; thereby forming one or more carbazoles represented by formula (3) below is provided.
Type:
Grant
Filed:
May 27, 2016
Date of Patent:
April 2, 2019
Assignee:
Dow Global Technologies LLC
Inventors:
Chunming Zhang, Arvind Jaganathan, Heqi Pan, Philip Fontaine, Jerzy Klosin
Abstract: Modulators of adenosin A3 receptors of formula (I): And procedure for preparing these compounds. Other objectives of the present invention are to provide pharmaceutical compositions comprising an effective amount of these compounds and the use of the compounds for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by modulation of the adenosine A3 receptor.
Type:
Grant
Filed:
January 22, 2016
Date of Patent:
March 26, 2019
Assignee:
PALOBIOFARMA, S.L.
Inventors:
Julio Castro-Palomino Lária, Juan Camacho Gómez
Abstract: The present application provides bifunctional compounds of Formula I or II: or an enantiomer, diastereomer, or stereoisomer, or a pharmaceutically acceptable salt thereof, which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds of Formula (I) or (II) that link a mutant cereblon-binding moiety to a ligand that is capable of binding to a targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof. The present application also relates to polynucleotides or polypeptides of a mutant cereblon and methods of use thereof.
Type:
Grant
Filed:
July 25, 2018
Date of Patent:
March 26, 2019
Assignee:
Dana-Farber Cancer Institute, Inc.
Inventors:
James Bradner, Mette Ishoey, Dennis Buckley, Joshiawa Paulk, Marc Andrew Cohen, Rhamy Zeid
Abstract: Provided herein are processes for the preparation of 2-thiophenecarbonyl chloride, which is useful, for example, in the preparation of 3,5-disubstituted-1,2,4-oxadiazoles, such as tioxazafen (3-phenyl-5-(2-thienyl)-1,2,4-oxadiazole).
Abstract: The present application provides novel quinazolines and azaquinazolines and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in for co-regulating RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways by administering a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, T and R4, and R6 to R8? are defined herein, to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.
Type:
Grant
Filed:
April 28, 2017
Date of Patent:
March 12, 2019
Assignee:
Asana BioSciences, LLC
Inventors:
Scott K. Thompson, Roger A. Smith, Sanjeeva Reddy, Tyler M. John, Vijay Kumar Nyavanandi, Subramanya Hoshalli, Vijay Potluri, Sunil Kumar Panigrahi, Prabhakara Rao Nadipalli, Saumitra Sengupta
Abstract: The present invention provides compounds that can enhance functional O-mannosylation of proteins including alpha-dystroglycan. Also provided are methods of preparation of the compounds defined by the formula I. Also provided are the methods of using the compounds or the pharmaceutical acceptable salts or prodrugs thereof in treating and preventing subjects suffering from the diseases including muscular dystrophies and cancers.
Abstract: This application relates to solabegron zwitterion useful for the treatment of lower urinary tract symptoms such as, for example, overactive bladder and prostate disorders. Additionally, this application relates to pharmaceutical compositions and methods of treatment utilizing the solabegron zwitterion for treating lower urinary tract symptoms. This application also relates to methods of preparing solabegron hydrochloride from the solabegron zwitterion.
Type:
Grant
Filed:
June 26, 2018
Date of Patent:
March 5, 2019
Assignee:
VELICEPT THERAPEUTICS, INC.
Inventors:
Raymond E. Stevens, Dalian Zhao, Bingidimi Itute Mobele