Abstract: Herein, methods of modulating inclusion formation and stress granules in cells are described. The methods comprise contacting a cell with an inclusion inhibitor. Methods for screening for modulators of TDP-43 aggregation are also described.
Type:
Grant
Filed:
May 21, 2012
Date of Patent:
June 7, 2016
Assignees:
AQUINNAH PHARMACEUTICALS, INC., THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
Inventors:
Benjamin Wolozin, Marcie Glicksman, Gregory D. Cuny, Justin Boyd
Abstract: A cream base for the topical application of skin care therapeutics and a process for making the cream base. In one embodiment, the therapeutic is tretinoin, hydroquinone and fluocinolone acetonide for the treatment of hyperpigmented skin conditions, such as melasma.
Type:
Grant
Filed:
January 9, 2014
Date of Patent:
May 10, 2016
Assignee:
GALDERMA S.A.
Inventors:
Nancy Puglia, Jerry Roth, Rosario Ramirez
Abstract: The invention provides for the use of antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit anti-mycobacteria activity, including the mycobacterium causing tuberculosis. Multiple compounds were synthesized and screened for anti-tuberculosis activity. Disclosed herein are a series of compounds with anti-tuberculosis activity, including six leads that completely inhibited bacterial growth at 5 micrograms per ml or less. Three of these compounds were tested to determine MIC and these ranged between 1 and 4 micrograms per ml against both drug susceptible Mycobacterium tuberculosis strains and strains that are multi-drug resistant (MDR) including XDR strains. The compounds developed are derived from parent compound nitazoxanide, which had no inhibitory activity in the stringent testing format used herein.
Type:
Grant
Filed:
September 20, 2011
Date of Patent:
May 10, 2016
Assignee:
UNIVERSITY OF VIRGINIA PATENT FOUNDATION
Inventors:
Paul S. Hoffman, Timothy L. MacDonald, Eric R. Houpt, Thomas E. Ballard, Jr.
Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
Type:
Grant
Filed:
March 12, 2013
Date of Patent:
May 3, 2016
Assignee:
ALLERGAN, INC.
Inventors:
Haiqing Yuan, Richard L. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
Type:
Grant
Filed:
June 25, 2014
Date of Patent:
May 3, 2016
Assignee:
SANOFI
Inventors:
Matthias Schaefer, Josef Pernerstorfer, Dieter Kadereit, Hartmut Strobel, Werngard Czechtizky, L. Charlie Chen, Alena Safarova, Aleksandra Weichsel, Marcel Patek
Abstract: A method of improving cognition in a patient with Down syndrome, which entails administering one or more ?2 adrenergic receptor agonists to the patient in an amount and with a frequency effective to improve cognition of the patient as measured by contextual learning tests.
Type:
Grant
Filed:
February 12, 2014
Date of Patent:
April 26, 2016
Assignee:
The Board of Trustees of the Leland Stanford Junior University
Inventors:
Ahmad Salehi, Brian Mediana, Sarah Moghadam, Van Dang, Devsmita Das, Kara Martin
Abstract: Highly acidic, stabilized peroxycarboxylic acid compositions are disclosed as having both improved antimicrobial efficacy in comparison to conventional peroxyoctanoic acid and peroxyacetic acid compositions for sanitizing applications, and improved transport and shipping stability. In particular, low odor and low/no VOC compositions having dual functionality as both acid wash and sanitizing compositions are disclosed.
Type:
Grant
Filed:
December 29, 2014
Date of Patent:
March 22, 2016
Assignee:
Ecolab USA, Inc.
Inventors:
Junzhong Li, David D. McSherry, Richard Staub
Abstract: Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.
Type:
Grant
Filed:
July 9, 2014
Date of Patent:
March 22, 2016
Assignee:
Infinity Pharmaceuticals, Inc.
Inventors:
Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp
Abstract: Compounds selected from the group of N-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C0-4)alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C0-4)alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, or 14-O-[(amino(C0-4)alkyl-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins, optionally in the form of a salt and/or a solvate, a pharmaceutical compositions comprising such compounds and their use as pharmaceuticals, e.g. for the treatment of microbial infections and for the treatment of acne, optionally in combination with other pharmaceutically active agents.
Type:
Grant
Filed:
August 11, 2011
Date of Patent:
March 8, 2016
Assignee:
Nabriva Therapeutics AG
Inventors:
Rosemarie Riedl, Klaus Thirring, Werner Heilmayer
Abstract: The invention includes compositions comprising selective AKR1C3 inhibitors. The invention also includes compositions comprising bifunctional AKR1C3 inhibitors and selective androgen receptor modulators. The invention further includes methods of treatment using the compositions of the invention.
Type:
Grant
Filed:
October 10, 2013
Date of Patent:
March 1, 2016
Assignee:
The Trustees of the University of Pennsylvania
Inventors:
Trevor M. Penning, Adegoke O. Adeniji, Michael C. Burns, Jeffrey Winkler, Barry Twenter
Abstract: The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, F, G, H, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.
Abstract: An occlusive dressing made with an elastomeric gel and one or more active agents is described. The elastomeric gel contains a plasticizing oil phase and a block copolymer agent. Methods of preventing, treating, curing or mitigating an infectious disease and methods of making the dressings are also disclosed.
Abstract: The present invention relates to 1,4 Oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
Type:
Grant
Filed:
January 12, 2012
Date of Patent:
January 26, 2016
Assignees:
SIENA BIOTECH S.P.A., HOFFMANN-LA ROCHE INC.
Inventors:
Matteo Andreini, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Massimiliano Travagli, Thomas Woltering, Wolfgang Wostl, Harald Mauser
Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.
Abstract: The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
Type:
Grant
Filed:
October 10, 2014
Date of Patent:
December 29, 2015
Assignee:
SynAffix B.V.
Inventors:
Floris Louis Van Delft, Floris Petrus Johannes Theodorus Rutjes, Frederik Jan Dommerholt
Abstract: The invention relates to hypophosphorous acid derivatives of formula (I) wherein —X is H or OH, —R represents one or several radicals R1-R5, identical or different, two of R1-R5 optionally occupying the same position on the phenyl group, one to four of R1-R5 being H and the others being selected in the group comprising -0-(CH2)n—COOH; —S—(CH2)n—COOH; —NH—(CH2)n—COOH; -0-(CH,R?)—COOH; —O—(CH2)n—OH; OR?, —R? being a C1-C3 alkyl radical; —OH; —COOH; halogen, particularly —F, —CI, —Br, —I, —CF3; —OCF3; —N02; —CH?CH—COOH; —(CH2)n—COOH; O—(CH2)n—P03H2; O—(CF2)n—P03H2; O—(CH2)n—S03H; O—(CH2)n—CONHOH; O—(CH2)n-tetrazol; O—(CH2)n-hydroxyisoxazol—n=1 to 5, preferably 1-3; said hypophosrous acid derivatives being diastereoisomers or enantiomers.
Type:
Grant
Filed:
May 16, 2012
Date of Patent:
December 15, 2015
Assignees:
UNIVERSITE PARIS DESCARTES, UNIVERSITE D'AUVERGNE
Inventors:
Francine Acher, Jean-Philippe Pin, Cyril Goudet, Alain Eschalier, Jérôme Busserolles, Delphine Rigault, Isabelle Lemasson, Sara Cesarini, Bruno Commare
Abstract: The present invention is related to the development of compounds and methods for inhibiting viral infection in a mammal. A pseudotype virus was developed for use in a high throughput assay for identifying nonpeptidic small molecule inhibitors that prevent viral entry into a host cell.
Type:
Grant
Filed:
September 13, 2011
Date of Patent:
December 15, 2015
Assignee:
Microbiotix, Inc.
Inventors:
Arnab Basu, Debra M. Mills, John D. Williams, Bing Li, Norton P. Peet, Terry L. Bowlin
Abstract: The present invention provides for a method of treating a disease such as cancer, comprising the step of administering to a patient a therapeutically effective amount of an isomer or analog of monoterpene or sesquiterpene (or its derivative), such as an isoperillyl alcohol. The present invention also provides for a method of treating a disease comprising the step of administering to a patient a therapeutically effective amount of a derivative of an isomer or analog of monoterpene or sesquiterpene, such as an isoperillyl alcohol carbamate. The derivative may be an isoperillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The route of administration may vary, including inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.
Type:
Grant
Filed:
December 16, 2011
Date of Patent:
December 15, 2015
Assignee:
NEONC TECHNOLOGIES INC.
Inventors:
Thomas Chen, Daniel Levin, Satish Pupalli, Daniel A Dickman
Abstract: This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salts thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.
Type:
Grant
Filed:
November 9, 2011
Date of Patent:
November 24, 2015
Assignees:
Novartis AG, Astex Therapeutics, LTD
Inventors:
John Vincent Calienni, Guang-Pei Chen, Baoqing Gong, Prasad Koteswara Kapa, Vishal Saxena