Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
Type:
Grant
Filed:
March 17, 2014
Date of Patent:
September 20, 2016
Assignee:
ArQule, Inc.
Inventors:
Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi Moussa, Neru Munshi
Abstract: A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory diseases and/or allergic conditions, in cancer therapy, specifically heme malignancies, and autoimmune conditions.
Type:
Grant
Filed:
February 19, 2015
Date of Patent:
September 20, 2016
Assignee:
Glaxo Group Limited
Inventors:
Francis Louis Atkinson, Michael David Barker, John Liddle, David Matthew Wilson
Abstract: Embodiments of the present disclosure provide for compounds such as those shown in FIG. 1.1 (compounds A, B, C, and D), 2?substituted nicotine compounds, azetidine compounds, ether linked nicotine compounds (FIG. 1.2, compounds E, F, G, and H), methods of synthesis of the compounds, methods of treatment of a condition using compounds A, B, C, D, 2?substituted nicotine compounds, azetidine compounds, or ether linked nicotine compounds, methods of selectively stimulating alpha7 nAChR and/or alpha4beta2 receptors, and the like.
Type:
Grant
Filed:
September 2, 2011
Date of Patent:
September 13, 2016
Assignees:
UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC., THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
Inventors:
William Reade Kem, Ferenc Soti, Anne Rouchaud, Hong Xing, Jon Lindstrom, Kristin Marie Andrud
Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating EGFR activity, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated EGFR activity.
Type:
Grant
Filed:
June 5, 2013
Date of Patent:
September 13, 2016
Assignee:
Novartis AG
Inventors:
Gerald Lelais, Robert Epple, Thomas H. Marsilje, III, Pierre-Yves Michellys, Matthew McNeill, Yun Long, Wenshuo Lu, Bei Chen, Badry Bursulaya, Songchun Jiang
Abstract: The present invention relates to the field of medicine, and disclosed are an L-setastine hydrochloride and a preparation method therefor. The compound of the present invention has the advantages of stronger histamine Hi receptor antagonism and small side effect; the yield of the preparation method is more than 80%, and the product purity is high. The present invention also provides an application of the compound as an H1 histamine receptor antagonist.
Type:
Grant
Filed:
July 10, 2012
Date of Patent:
September 6, 2016
Assignee:
ANHUI QINGYUN PHARMACEUTICAL & CHEMICAL CO., LTD.
Abstract: Provided is an industrially scalable process for the preparation of a benzazepine derivative, namely, 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methyl benzoyl amino) benzoyl]-2,3,4,5-tetrahydro-1H-1-benzazepine (generically referred as Tolvaptan).
Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and relates to novel homoharringtonine acylated derivatives of formula (I) and formula (II) and a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.
Abstract: A dye, having a structure represented by formula (1A): wherein A represents a group of atoms necessary for forming a ring together with the carbon-nitrogen bond; at least one of Y1A and Y2A represents an acidic group, in which when they each represent an acidic group, they may be the same as or different from each other, or when only one of them represents an acidic group, the other represents an electron-withdrawing group; D represents a group to give a dye; n represents an integer of 1 or greater; L represents a single bond or a divalent linking group; and Y3A represents an acidic group.
Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
Type:
Grant
Filed:
May 4, 2012
Date of Patent:
August 23, 2016
Assignee:
Constellation Pharmaceuticals, Inc.
Inventors:
Brian K. Albrecht, Victor S. Gehling, Michael Charles Hewitt, Alexander M. Taylor, Jean-Christophe Harmange
Abstract: Certain tetrahydro-pyrimidoazepine compounds are described, which are useful as TRPV1 modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by TRPV1. Thus, the compounds may be administered to treat, e.g., pain, itch, cough, asthma, or inflammatory bowel disease.
Type:
Grant
Filed:
January 17, 2014
Date of Patent:
August 23, 2016
Assignee:
Janssen Pharmaceutica NV
Inventors:
Brett D. Allison, Bryan James Branstetter, J. Guy Breitenbucher, Michael D. Hack, Natalie A. Hawryluk, Alec D. Lebsack, Kelly J. McClure, Jeffrey E. Merit
Abstract: The present invention relates to novel polymorphic forms of alcaftadine, processes of preparing novel polymorphic forms of alcaftadine and pharmaceutical compositions thereof.
Abstract: The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.
Type:
Grant
Filed:
June 13, 2014
Date of Patent:
August 2, 2016
Assignee:
Albany Molecular Research, Inc.
Inventors:
Bruce F. Molino, Shuang Liu, Aruna Sambandam, Peter R. Guzzo, Min Hu, Congxiang Zha, Kassoum Nacro, David D. Manning, Matthew L. Isherwood, Kristen N. Ryan, Wenge Cui, Richard E. Olson
Abstract: The present invention is related to pyrazoline dione derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
Type:
Grant
Filed:
September 27, 2010
Date of Patent:
July 19, 2016
Assignee:
GENKYOTEX SA
Inventors:
Patrick Page, Francesca Gaggini, Benoît Laleu
Abstract: It is described of a process for the preparation of drospirenone, the compound of formula 1 shown below, a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions having contraceptive action, starting from 17?-(3-hydroxypropyl)-6?,7?;15?,16?-dimethylene-5?-androstane-3?,5,17?-triol.
Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
Type:
Grant
Filed:
August 10, 2012
Date of Patent:
July 19, 2016
Assignee:
Janssen Sciences Ireland UC
Inventors:
Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans
Abstract: The present invention relates to the field of pharmaceutical chemistry, and particularly to an aza-benzo[f]azulen derivative (I) and an antitumor effect thereof. Pharmacological tests show that the compound of the present invention has in vitro and in vivo antitumor activities, and can be developed into clinical drugs for treating or controlling diseases such as stomach cancer, lung cancer, liver cancer, breast cancer, colon cancer, prostate cancer, and oral cancer.
Type:
Grant
Filed:
January 24, 2013
Date of Patent:
July 5, 2016
Assignee:
TIANYI BIOSCIENCE CO., LTD.
Inventors:
Xihan Wu, Liwu Fu, Dongmei Zhang, Yurong Wang
Abstract: The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor.
Type:
Grant
Filed:
October 11, 2013
Date of Patent:
June 28, 2016
Assignees:
ABBVIE DEUTSCHLAND GMBH & CO. KG, ABBVIE INC.
Inventors:
Andreas Haupt, Jürgen Dinges, Liliane Unger, Karsten Wicke, Robert van Waterschoot, Scott Mittelstadt, Karla Drescher, Ana Relo
Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Type:
Grant
Filed:
December 17, 2013
Date of Patent:
June 7, 2016
Assignee:
Novartis AG
Inventors:
Mahbub Ahmed, Alexander Ashall-Kelly, Louisa Gueritz, Jeffrey McKenna, Joseph McKenna, Simon Mutton, Rakesh Parmar, Jon Shepherd, Paul Wright