Abstract: Use of 2,3-dihydroquinazolin-4(1H)-one cyclic derivatives of formula (I) for the treatment of infection with viruses entering cells by endocytosis, especially filovirus such as Ebolavirus.
Type:
Grant
Filed:
October 18, 2013
Date of Patent:
June 13, 2017
Assignees:
Commissariat a l'Energie Atomique et aux Energies Alternatives, The Board of Regents of the University of Texas System
Inventors:
Daniel Gillet, Julien Barbier, Robert Davey, Jean-Christophe Cintrat, Romain Noel
Abstract: Described herein are assays directed to determining the level of bioavailable or free vitamin D in a blood sample in a subject. The values determined for bioavailable or free vitamin D indicate whether the subject suffers from insufficient levels of vitamin D. Also described herein are methods of treatment for vitamin D insufficiency.
Type:
Grant
Filed:
May 2, 2014
Date of Patent:
June 6, 2017
Assignees:
Beth Israel Deaconess Medical Center, Inc., The General Hospital Corporation
Inventors:
Ravi Thadhani, S. Ananth Karumanchi, Anders Hayden Berg, Ishir Bhan
Abstract: The present invention relates to combinations of phosphodiesterase 2 (PDE2) inhibitors with inhibitors of phosphodiesterase 10 (PDE10). In particular, the invention relates to combinations of 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives which have been found to inhibit phosphodiesterase 2 (PDE2), with inhibitors of phosphodiesterase 10 (PDE10). Particular PDE10 inhibitors are selected from the group of MP-10, PQ-10, TP-10, papaverine, and the compounds disclosed in WO 2011/051324 and in WO 2011/110545.
Type:
Grant
Filed:
June 25, 2013
Date of Patent:
June 6, 2017
Assignee:
JANSSEN PHARMACEUTICA NV
Inventors:
Antonius Adrianus Hendrikus Petrus Megens, Xavier Jean Michel Langlois, José Ignacio Andrés-Gil
Abstract: Certain embodiments of the present invention provide selected compounds having a molecular structure according to Formula 1: In Formula 1, Z is —CO—, —SO—, or —SO2—; Ar is phenyl, heteroaryl, or heterocycloalkyl; Het is heteroaryl; R is R?, X, or NR1R2; R? is R3, or OR3; R? is R4, or OR4; R1 and R2 are each independently H, alkyl, or acyl; R3 is H, heteroaryl, or alkyl; R4 is H, heteroaryl, or CnH2n+1 (n>2); and X is F, Br, I, CN, or NO2. In some embodiments, compounds having a molecular structure according to Formula 1 have the property of inhibiting a growth of a cell line selected from HeLa and MB468 with a sub-micromolar IC50.
Type:
Grant
Filed:
July 8, 2016
Date of Patent:
June 6, 2017
Assignee:
The Regents of the University of California
Abstract: The present invention relates to a process for preparing substituted anthranilic acid derivatives of the formula (I) in which R1, R2, R3 and R4 are each as defined in the description, by conversion of compounds of the general formula (IV) in the presence of a palladium catalyst and carbon monoxide. The present invention likewise relates to compounds of the general formula (IV).
Type:
Grant
Filed:
October 28, 2015
Date of Patent:
June 6, 2017
Assignee:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Thomas Himmler, Sergii Pazenok, Frank Volz, Norbert Lui
Abstract: The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can be alkaloids and, more particularly, the tertiary amines can be opioids. In specific embodiments, the present disclosure provides methods for use in processes for the synthesis of naloxone and naltrexone from oripavine.
Type:
Grant
Filed:
August 14, 2015
Date of Patent:
May 23, 2017
Assignee:
Rhodes Technologies
Inventors:
Joshua Robert Giguere, Keith Edward McCarthy, Helge Alfred Reisch, Sergio Sandoval, Jake Larry Stymiest
Abstract: The present invention relates to transition-metal-free process for the synthesis of tertiary arylamines comprises coupling reaction between arynes and N,N-dimethyl aniline compounds in presence of 18-crown-6, KF and THF.
Type:
Grant
Filed:
June 24, 2014
Date of Patent:
May 16, 2017
Assignee:
COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
Abstract: Disclosed is use of andrographolide derivative as shown by general formula 1 in manufacture of medicaments for anti-hepatitis C virus, and preventing and treating immunological liver damage caused by virus infection and different chemical liver damage.
Type:
Grant
Filed:
June 8, 2016
Date of Patent:
May 2, 2017
Assignee:
Zhengzhou University
Inventors:
Guifu Dai, Jing Zhao, Haiwei Xu, Huanfei Liu, Zhenwei Wu, Di Wu, Jian Wu, Hongmin Liu
Abstract: A low calorie sweetener composition with sweetness synergy, providing a reduction in off-taste and a desirable temporal profile. The sweetener composition comprises allulose, fructose and sucralose. In a preferred embodiment, the sweetener composition comprises allulose in an amount of at least about 45%, fructose in an amount of at least about 20%, and sucralose in an amount of at least about 0.01% by weight relative to the total weight of allulose, fructose and sucralose in the composition. The sweetener composition is suitable for use as a substitute for high calorie sugars. The sweetener composition is for use in food and beverage products, pharmaceutical products, nutritional product and cosmetic products.
Type:
Grant
Filed:
March 14, 2014
Date of Patent:
May 2, 2017
Assignee:
TATE & LYLE INGREDIENTS AMERICAS LLC
Inventors:
Ryan D. Woodyer, Jason C. Cohen, John R. Bridges
Abstract: The invention relates to the identification of genetic signatures and expression profiles that are a part of the Base Excision Repair (BER) pathway, a major DNA repair pathway that modifies base lesions. In one embodiment, the present invention provides a method of determining responsiveness of treatment by BER inhibitors for malignant glioma by determining the presence of a low level of expression of Apex 1, a low level of expression of Apex 2, and a high level of expression of MPG.
Type:
Grant
Filed:
May 21, 2014
Date of Patent:
May 2, 2017
Assignees:
Dignity Health, The Translational Genomics Research Institute
Inventors:
Shwetal V. Mehta, Michael E. Berens, Harshil Dineshkumar Dhruv
Abstract: The disclosure relates to Compounds of Formula (I) and pharmaceutically acceptable derivatives thereof, where R1, R4, R8, R9, and m are as defined herein, compositions comprising an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, pain associated with osteoarthritis, osteoarthritis, UI, an ulcer, IBD, and IBS, comprising administering to an animal in need thereof an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof.
Abstract: The present invention provides a small compound targeting at TACC3. The present invention further provides a drug, particularly, an anticancer agent, comprising the small compound targeting at TACC3. A compound represented by the general formula (I) or a pharmaceutically acceptable salt, solvate, or ester derivative thereof binds to TACC3 and inhibits cell growth. Thus, these compounds can be used as drugs, particularly, anticancer agents.
Abstract: Cysteamine prodrugs, pharmaceutical compositions comprising the cysteamine prodrugs, and methods of using cysteamine prodrugs and pharmaceutical compositions thereof for treating eye, kidney, liver, metabolic, and neurological disorders such as cystinosis, cystinuria, non-alcoholic steatohepatitis, Batten disease, Leigh syndrome, and Huntington's disease.
Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
Type:
Grant
Filed:
October 14, 2014
Date of Patent:
April 18, 2017
Assignee:
Janssen Pharmaceutica NV
Inventors:
Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Xiaohua Xue, Maxwell D. Cummings, Kelly McClure, Virginia Tanis
Abstract: The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can be alkaloids and, more particularly, the tertiary amines can be opioids. In specific embodiments, the present disclosure provides methods for use in processes for the synthesis of naloxone and naltrexone from oripavine.
Type:
Grant
Filed:
August 14, 2015
Date of Patent:
April 18, 2017
Assignee:
Rhodes Technologies
Inventors:
Joshua Robert Giguere, Keith Edward McCarthy, Helge Alfred Reisch, Sergio Sandoval, Jake Larry Stymiest
Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.
Type:
Grant
Filed:
December 28, 2012
Date of Patent:
April 11, 2017
Assignees:
PTC Therapeutics, Inc., F. Hoffmann-La Roche AG
Inventors:
Matthew G. Woll, Guangming Chen, Soongyu Choi, Amal Dakka, Song Huang, Gary Mitchell Karp, Chang-Sun Lee, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Sergey Paushkin, Hongyan Qi, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Emmanuel Pinard, Hasane Ratni
Abstract: The invention relates to isoxazolo[5,4-b]pyridine compounds of formula I, to the agriculturally useful salts of isoxazolo[5,4-b]pyridine compounds of formula I, and to their use as herbicides.
Type:
Grant
Filed:
August 17, 2015
Date of Patent:
April 4, 2017
Assignee:
BASF SE
Inventors:
Anna Aleksandra Michrowska-Pianowska, Julia Major, Johannes Hutzler, Trevor William Newton, Richard Roger Evans, Klaus Kreuz, Klaus Grossmann, Dschun Song, Anja Simon, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Helmut Kraus, Thomas Seitz, Andree van der Kloet, Ruediger Reingruber
Abstract: [Problem] To provide a solid pharmaceutical composition which contains a compound represented by general formula (1) or a salt thereof and suppresses decomposition of said compound or salt thereof, and a production method of said solid pharmaceutical composition. [Solution] This solid pharmaceutical composition contains a compound represented by general formula (1) or a salt thereof, a cellulosic excipient, and an acidic substance of pH 4.0 or less.