Patents Issued in April 3, 2014
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Publication number: 20140094439Abstract: Novel drug carriers capable of targeted and/or pH dependent release of biologically active agents into selected pH environments including the gastrointestinal (GI), ophthalmic, urinary, or reproductive tracts. Unexpectedly, carriers including free fatty acids (FFA) are able to deliver biologically active agents to various pH environments. Such targeted delivery is tailorable and useful for active agents that are: (a) injurious to the upper GI tract (esophagus, stomach, and duodenum), (b) acid labile, (c) impermeable/insoluble compounds in GI fluids, (d) susceptible to first pass metabolism, and/or (e) cause stomach irritation, upset, or dyspepsia.Type: ApplicationFiled: June 3, 2013Publication date: April 3, 2014Inventors: Upendra K. Marathi, Susann Edler Childress, Shaun L. Gammill, Robert W. Strozier
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Publication number: 20140094440Abstract: Estrogen and progesterone replacement therapies are provided herein. Among others, the following formulations are provided herein: solubilized estradiol without progesterone; micronized progesterone without estradiol; micronized progesterone with partially solubilized progesterone; solubilized estradiol with micronized progesterone; solubilized estradiol with micronized progesterone in combination with partially solubilized progesterone; and solubilized estradiol with solubilized progesterone.Type: ApplicationFiled: December 6, 2013Publication date: April 3, 2014Applicant: TherapeuticsMD, Inc.Inventors: Brian A. Bernick, Janice Louise Cacace, Peter H.R. Persicaner, Neda Irani, Julia M. Amadio
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Publication number: 20140094441Abstract: Estrogen and progesterone replacement therapies are provided herein. Among others, the following formulations are provided herein: solubilized estradiol without progesterone; micronized progesterone without estradiol; micronized progesterone with partially solubilized progesterone; solubilized estradiol with micronized progesterone; solubilized estradiol with micronized progesterone in combination with partially solubilized progesterone; and solubilized estradiol with solubilized progesterone.Type: ApplicationFiled: December 6, 2013Publication date: April 3, 2014Applicant: TherapeuticsMD, Inc.Inventors: Brian A. Bernick, Janice Louise Cacace, Peter H.R. Persicaner, Neda Irani, Julia M. Amadio
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Publication number: 20140094442Abstract: Combinations comprising (a) a corticosteroid and (b) an antagonist of M3 muscarinic receptors which is 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid are useful, e.g., for treatment of respiratory disease, e.g., asthma or chronic obstructive pulmonary disease.Type: ApplicationFiled: April 2, 2013Publication date: April 3, 2014Inventors: Jordi GRAS ESCARDO, Jesus LLENAS CALVO, Hamish RYDER, Pio ORVIZ DIAZ
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Publication number: 20140094443Abstract: The invention relates to compounds of Formula A: or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including obesity, insulin sensitivity, inflammation, cholestasis, and bile desaturation.Type: ApplicationFiled: April 1, 2013Publication date: April 3, 2014Applicant: INTERCEPT PHARMACEUTICALS, INC.Inventor: Intercept Pharmaceuticals, Inc.
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Publication number: 20140094444Abstract: The present application discloses strategies to recruit and mobilize stem cells using S1P receptor selective agonists and antagonists as wells as regulators of chemokine receptors. In an in vivo ischemic model, S1P1/S1P3 activation with FTY720 impeded inflammatory cell infiltration and recruited endothelial progenitor cells (EPCs) with the potential to increase microvascular remodeling. S1P3 expression on marrow-derived cells was essential for this remodeling. Concurrent systemic S1P3 and CXCR4 antagonism mobilized hematopoietic stem cells (HSCs) with the ability to engraft and repopulate blood cells. Pre-treatment of donor HSCs with FTY720 increased homing toward SDF-1 and improved engraftment in marrow. FTY720-coated bone allografts coupled with systemic administration of VPC01091 enhanced bone allograft integration and new bone formation in bone defects. MSCs pre-treated with FTY720 exhibited increased migration toward SDF-1, a CXCR4+ ligand.Type: ApplicationFiled: March 16, 2012Publication date: April 3, 2014Applicant: University of Virginia Patent FoundationInventors: Edward A. Botchwey, III, Mary J. Laughlin, Kevin R. Lynch, Anusuya Das, Anthony Awojoodu
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Publication number: 20140094445Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: August 15, 2012Publication date: April 3, 2014Applicant: University of Utah Research FoundationInventors: Hariprasad Vakayalapati, Venkataswamy Soma, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
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Publication number: 20140094446Abstract: Compositions comprising cyclic amino acids or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier. Said compositions are for use in the treatment of pain. Pain includes both acute and chronic forms of pain. The preferred cyclic amino acid is 1-aminocyclobutane-1-carboxylic acid (ACBC).Type: ApplicationFiled: July 29, 2013Publication date: April 3, 2014Applicant: Therexcell Pharma Inc.Inventors: Ernest Puil, Bernard A. MacLeod, Richard Wall
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Publication number: 20140094447Abstract: Pharmaceutical compositions and methods for treating or preventing bacterial infections are disclosed. The pharmaceutical compositions typically comprise pharmaceutically effective amount of: (a) sulbactam or a pharmaceutically acceptable salt thereof, and (b) at least one beta-lactamase inhibitor or a pharmaceutically acceptable salt thereof, with the provision that the beta-lactamase inhibitor is not sulbactam.Type: ApplicationFiled: October 4, 2011Publication date: April 3, 2014Inventors: Sachin Subhash Bhagwat, Mahesh Vithalbhai Patel
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Publication number: 20140094448Abstract: The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds.Type: ApplicationFiled: September 13, 2013Publication date: April 3, 2014Applicant: SENHWA BIOSCIENCES, INC.Inventors: Mustapha Haddach, Joe A. Tran, Fabrice Pierre, Collin F. Regan, Nicholas Raffaele, Suchitra Ravula, David M. Ryckman
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Publication number: 20140094449Abstract: The invention relates to sulphur- and/or selenium-containing compounds that can inhibit the enzyme inositol mono-phosphatase (IMPase), and which can be used in treating conditions that are treatable through inhibition of this enzyme, such as bi-polar disorder, the compounds having a structure of Formula (I), or is a pharmaceutically acceptable salt thereof; Formula (I); in which: E is S or Se and each of phenyl rings A and B is optionally substituted with one or more substituents, in which each substituent is selected independently from: (1) a halogen, which is preferably selected from F, Cl and Br; (2) C1-C4 alkyl, such as C1-C2 alkyl or C1 alkyl, optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br; and (3) C1-C4 alkoxy, such as C1-C2 alkoxy or C1 alkoxy; optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br.Type: ApplicationFiled: January 18, 2012Publication date: April 3, 2014Applicant: ISIS INNOVATION LTD.Inventors: Grant C. Churchill, Sridhar R. Vasudevan, Nisha Singh
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Publication number: 20140094450Abstract: The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R?, R?, R??, R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: September 19, 2013Publication date: April 3, 2014Applicant: SANOFIInventors: Stephanie HACHTEL, Paulus WOHLFART, John WESTON, Marco MUELLER, Elisabeth DEFOSSA, Katharina MERTSCH, Jian-Hui WENG, Robert Alan BINNIE, Farid ABDUL-LATIF, William Jerome BOCK, Armin WALSER
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Publication number: 20140094451Abstract: There is provided a preventive for glaucoma or a preventive or a remedy for ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. A preventive or a remedy for glaucoma comprising a Rho kinase inhibitor and an ?1 blocker in combination.Type: ApplicationFiled: December 6, 2013Publication date: April 3, 2014Applicant: Kowa Co., Ltd.Inventors: Ken MIZUNO, Jiro MATSUMOTO
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Publication number: 20140094452Abstract: This application discloses liquid compositions for administration to a patient comprising midazolam and a pharmaceutically acceptable carrier, wherein the pH of the composition is about 6 or higher, the composition comprises less than about 200 mg/ml cyclodextrin, and at least about 50% of the midazolam is present in solution. Uses of these compositions are also disclosed.Type: ApplicationFiled: May 2, 2013Publication date: April 3, 2014Applicant: Special Products, Ltd.Inventor: Special Products, Ltd.
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Publication number: 20140094453Abstract: The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of modulating the sweet taste of compositions.Type: ApplicationFiled: December 4, 2013Publication date: April 3, 2014Inventors: Catherine TACHDJIAN, Donald KARANEWSKY, Sara WERNER, Vincent DARMOHUSODO, Jeff YAMAMOTO
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Publication number: 20140094454Abstract: The present invention provides compounds of Formula I: wherein A is selected from the group consisting of; R1 is H or F; R2 is H, —CH2OH, C1-C3 alkyl, R3 is H, F, or CN; R4 is H, F; or CN; and R5 is H, —CH3, or —OCH3; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 4, 2013Publication date: April 3, 2014Applicant: Eli Lilly and CompanyInventors: James Peter BECK, Steven James GREEN, Jose Eduardo LOPEZ, Brian Michael MATHES, Dustin James MERGOTT, Warren Jaye PORTER, Zoran RANKOVIC, Yuan SHI, Brian Morgan WATSON, Leonard Larry WINNEROSKI, JR.
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Publication number: 20140094455Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.Type: ApplicationFiled: August 19, 2013Publication date: April 3, 2014Applicant: ARIZONA BOARD OF REAGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONAInventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
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Publication number: 20140094456Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.Type: ApplicationFiled: March 13, 2013Publication date: April 3, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
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Publication number: 20140094457Abstract: The present invention relates to pharmaceutical compositions comprising a compound and a pharmaceutically acceptable carrier. The present invention is also directed to a method of treating a genetic disease caused by premature termination codons, or other conditions that render messenger ribonucleic acid (mRNA) susceptible to nonsense mediated RNA decay, in a subject. Also disclosed is a method of inhibiting nonsense mediated RNA decay and/or induction of autophagy. The present invention also relates to a method of identifying inhibitors of nonsense mediated RNA decay and/or inducing autophagy. The present invention further relates to a method of inhibiting nonsense mediated RNA decay and/or induction of autophagy in a subject.Type: ApplicationFiled: October 2, 2013Publication date: April 3, 2014Applicant: NEW YORK UNIVERSITYInventors: Lawrence B. Gardner, Timothy J. Cardozo, Leenus Martin
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Publication number: 20140094458Abstract: A method of contraception is provided which involves delivery of 21 to 27 consecutive days of a progestin in the absence of an estrogen or other steroidal compound, followed by 1 to 7 days without an effective amount of an active agent. Also described is a pharmaceutically useful kit to facilitate delivery of this regimen.Type: ApplicationFiled: November 8, 2013Publication date: April 3, 2014Applicant: Wyeth LLCInventors: Gary Sondermann Grubb, Ginger Dale Constantine
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Publication number: 20140094459Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: May 16, 2012Publication date: April 3, 2014Applicant: Princpia Biopharma Inc.Inventors: David Michael Goldstein, Kenneth Albert Brameld
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Publication number: 20140094460Abstract: The present invention relates to sodium channel inhibitors of Formula I: in which R1, R2, R3, R4, R5, R6, and R7 are as defined above, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.Type: ApplicationFiled: December 10, 2013Publication date: April 3, 2014Applicant: Gilead Sciences, Inc.Inventors: Matthew Abelman, Nancy Chu, Robert H. Jiang, Kwan Leung, Jeff Zablocki
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Publication number: 20140094461Abstract: A method of selecting a subject having cancer for treatment with a Hedgehog signaling inhibitor by determining the level of expression of at least one biomarker in a biological sample derived from the subject.Type: ApplicationFiled: April 3, 2012Publication date: April 3, 2014Inventors: Raj Bandaru, Asifa Haider, Douglas Michael Robinson, Kristine Lynn Rose, Thad Tyson Sharp, Yaping Shou
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Publication number: 20140094462Abstract: Sonic Hedgehog modulators and methods of use thereof are provided for.Type: ApplicationFiled: February 28, 2013Publication date: April 3, 2014Inventors: Sara Buhrlage, Chris Dockendorff, Mike Foley, Han-Je Kim, Andrew Germain, Lawrence MacPherson, Partha Nag, Stuart Schreiber, Amal Ting, Michel Weiwer, Willmen Youngsaye
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Publication number: 20140094463Abstract: The present invention relates to carrier systems useful for pharmaceutical compositions. These carriers comprise an emulsifier, and also in further embodiments a polymeric dissolution aid. These carriers are useful for delivering pharmaceutical actives such as antimicrobial agents.Type: ApplicationFiled: November 1, 2011Publication date: April 3, 2014Applicant: RIB-X PHARMACEUTICALS, INC.Inventors: Eric S. Burak, Danping Li, David S. Dresback
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Publication number: 20140094464Abstract: The invention described herein pertains to compounds and compositions for treating Ape1 mediated diseases. In particular, the invention described herein pertains to quinone compounds and pharmaceutical compositions containing them for treating Ape1 mediated diseases.Type: ApplicationFiled: May 25, 2012Publication date: April 3, 2014Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventors: Mark R. Kelley, James H. Wikel
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Publication number: 20140094465Abstract: The present invention is directed to compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: June 5, 2012Publication date: April 3, 2014Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Publication number: 20140094466Abstract: In alternative embodiments, the invention provides compositions that inhibit the polypeptide SSH-2, or SlingSHot-2, a phosphatase enzyme that regulates actin filaments, and methods for making and using them, including methods comprising administering compositions of the invention to regulate or modify actin filament polymerization by inhibiting SSH-2, where in one embodiment compositions of the invention slow or inhibit F-actin depolymerization and severing. In alternative embodiments, compositions and methods of the invention are used to slow or inhibit cell motility and/or internal remodeling. In alternative embodiments, compositions and methods of the invention are used to slow or inhibit, or reverse, or ameliorate the progression of a cancer or a metastasis or other uncontrolled or unregulated cell growth, and/or Alzheimer's disease.Type: ApplicationFiled: March 15, 2012Publication date: April 3, 2014Inventors: Jason H. Haga, Shu Chien, Matt Mui, Marshall J. Levesque, Phillip D. Pham
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Publication number: 20140094467Abstract: The canonical Wnt signaling pathway is implicated in many disorders including neural tube defects, limb malformations, and heart defects, developmental disorders associated with alcohol exposure (fetal alcohol syndrome) or exposure to bipolar medications (i.e. lithium), wound healing, and Alzheimer's disease. Elevated plasma homocysteine (HCy), which results from folate (folic acid, FA) deficiency, the mood-stabilizing drug lithium (Li), and alcohol (ethanol) are linked to the induction of human congenital heart and neural tube defects. FA supplementation ameliorates the observed developmental errors in the Li-HCy, or alcohol-exposed mouse embryos and normalized heart function. Li, HCy or Wnt3A suppress Wnt-modulated Hex and Islet-1 expression. FA protects from the gene misexpression that is induced by all three factors. Administration of myo-inositol with FA synergistically enhances the protective effect.Type: ApplicationFiled: October 8, 2013Publication date: April 3, 2014Applicant: UNIVERSITY OF SOUTH FLORIDAInventor: Kersti K. Linask
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Publication number: 20140094468Abstract: The present invention relates to the use of pteridines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to compounds per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents.Type: ApplicationFiled: December 3, 2013Publication date: April 3, 2014Applicant: Tibotec Pharmaceuticals Ltd.Inventors: Pierre Jean-Marie Bernard Raboisson, Dominique LouisNestorGhislain Surleraux, Tse-I Lin, Oliver Lenz, Kenneth Alan Simmen
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Publication number: 20140094469Abstract: Improved methods and compositions for safe and effective treatment of erythema or a symptom associated with erythema in a subject are described. The methods involve topically applying to an affected skin area a topical composition comprising about 0.3% to about 10% by weight of brimonidine and a pharmaceutically acceptable carrier.Type: ApplicationFiled: December 5, 2013Publication date: April 3, 2014Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Michael GRAEBER, Christian LOESCHE, Philip FREIDENREICH, Yin-sang LIU, Matthew James LEONI
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Publication number: 20140094470Abstract: The invention relates to a method of treating dermatological conditions or symptoms associated therewith in a patient in need thereof by topically administering an effective amount of a combination of brimonidine or a pharmaceutically acceptable salt thereof and oxymetazoline or a pharmaceutically acceptable salt thereof to the affected area of skin on the patient. The invention further relates to topical compositions including the combination of compounds and a pharmaceutically acceptable carrier.Type: ApplicationFiled: December 10, 2013Publication date: April 3, 2014Applicant: Galderma Laboratories Inc.Inventors: Michael Graeber, Matthew James Leoni, Nathalie Wagner
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Publication number: 20140094471Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: September 26, 2013Publication date: April 3, 2014Applicants: AbbVie Inc., The Walter and Eliza Hall Institute of Medical Research, Genentech, Inc.Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa A. Hasvold, Laura Hexamer, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Robert A. Mantei, Todd M. Hansen
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Publication number: 20140094472Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.Type: ApplicationFiled: September 24, 2013Publication date: April 3, 2014Applicant: Alkermes Pharma Ireland LimitedInventors: Laura Cook Blumberg, Julius F. Remenar, Orn Almarsson, Tarek A. Zeidan
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Publication number: 20140094473Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.Type: ApplicationFiled: December 6, 2013Publication date: April 3, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, Michael J. Boyd, Ioana Davies, Hongbo Deng, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Joseph M. Kennedy, Brian Ledford, Mark W. Ledeboer, Francois Maltais, Emanuele Perola, Tiansheng Wang
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Publication number: 20140094474Abstract: Compounds of formula (I) or (II) wherein Rx, Rz, R9, R10, R14, R14?, R15, R15?, A and B are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds possess utility as tissue-selective androgen receptor modulators (SARM) and are useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.Type: ApplicationFiled: April 20, 2012Publication date: April 3, 2014Applicant: ORION CORPORATIONInventors: Olli Törmakängas, Gerd Wohlfahrt, Harri Salo, Rathna Durga Ramasurbamanian, Pranab Kumar Patra, Arputharaj Ebenezer Martin, Terhi Heikkinen, Anniina Vesalainen, Anu Moilanen, Arja Karjalainen
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Publication number: 20140094475Abstract: Disclosed are solid forms of antiretroviral compounds and anti-oxidative acids, and processes for their preparation. Pharmaceutical compositions using the solid forms are also disclosed.Type: ApplicationFiled: April 9, 2012Publication date: April 3, 2014Applicant: LAURUS LABS PRIVATE LIMITEDInventors: Venkata S. Indukuri, Vamsee K. Muppidi, Sree R. Joga, Seeta R. Gorantla, Satyanarayana Chava
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Publication number: 20140094476Abstract: The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: ApplicationFiled: December 5, 2013Publication date: April 3, 2014Inventors: James D. Rodgers, Hui-Yin Li
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Publication number: 20140094477Abstract: The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: ApplicationFiled: December 5, 2013Publication date: April 3, 2014Inventors: James D. Rodgers, Hui-Yin Li
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Publication number: 20140094478Abstract: The present invention relates to a composition and tablet comprising raltegravir and to a process for the preparation of such tablet.Type: ApplicationFiled: May 29, 2012Publication date: April 3, 2014Applicant: ratiopharm GmbHInventors: Daniela Stumm, Dominique Meergans
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Publication number: 20140094479Abstract: A process for producing a solid dispersion of an active ingredient which comprises feeding the active ingredient and a matrix-forming agent to an extruder and forming a uniform extrudate, wherein the extruder comprises at least two rotating shafts (2), each of the shafts (2) carrying a plurality of processing elements disposed axially one behind the other, the processing elements defining (i) a feeding and conveying section (A), (ii) at least one mixing section (B), and (iii) a discharging section (E), wherein the processing element(s) defining the mixing section (B) comprise(s) a mixing element (11, 12, 13) that is derived from a screw type element (FIG. 2).Type: ApplicationFiled: December 2, 2013Publication date: April 3, 2014Applicant: AbbVie Deutschland GmbH & Co. KGInventors: Thomas Kessler, Jörg Breitenbach, Christoph Schmidt, Matthias Degenhardt, Jörg Rosenberg, Harald Krull
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Publication number: 20140094480Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protection from neuron cell death.Type: ApplicationFiled: December 9, 2013Publication date: April 3, 2014Applicant: Board of Regents of The University of Texas SystemInventors: Steven L. McKnight, Joseph M. Ready, Andrew A. Pieper, Jef K. De Brabander
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Publication number: 20140094481Abstract: Tamper resistant controlled release formulations.Type: ApplicationFiled: April 19, 2013Publication date: April 3, 2014Applicant: Euro-Celtique S.A.Inventor: Euro-Celtique S.A.
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Publication number: 20140094482Abstract: A method of inhibiting hyperphosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system a FLNA-binding effective amount of a FLNA-binding benzazocine-ring compound or a pharmaceutically acceptable salt thereof such as a) an opioid receptor antagonist compound or b) a mixed opioid receptor agonist and antagonist (agonist/antagonist) compound, c) an opioid receptor agonist compound or d) an enantiomer of an opioid receptor interacting compound, that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1. The administered compound preferably contains at least four of the six pharmacophores of FIGS. 5-10.Type: ApplicationFiled: August 15, 2013Publication date: April 3, 2014Inventors: George B. Thornton, Hoau-Yan Wang, Lindsay Burns Barbier, Michael S. Zamloot
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Publication number: 20140094483Abstract: Provided herein are novel iso-ergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and/or the 5-HT1B receptor, without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2B receptors using the compounds and compositions disclosed herein.Type: ApplicationFiled: October 3, 2013Publication date: April 3, 2014Applicant: MAP PHARMACEUTICALS, INC.Inventors: Jian Zhang, Robert O. Cook
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Publication number: 20140094484Abstract: The present invention relates to a rapamycin sustained release delivery system for treatment of diseases responsive to rapamycin. The sustained release delivery system of the invention includes a flowable composition containing rapamycin or a rapamycin derivative, which is capable of providing an implant containing the rapamycin or derivative thereof. The flowable composition may be injected into tissue whereupon it coagulates to become the solid or gel, monolithic implant. The flowable composition includes a biodegradable, thermoplastic polymer, an organic liquid and rapamycin or a rapamycin derivative.Type: ApplicationFiled: October 2, 2012Publication date: April 3, 2014Applicants: QLT Inc., Tolmar Therapeutics, Inc.Inventors: Philippe Maria Clotaire Margaron, Eric Dadey, Christopher M. Lindemann, Ruihong Li
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Publication number: 20140094485Abstract: The invention relates to a novel hemi-succinate salt form of (2S)-2-tert-butoxy-2-(4-(2,3-dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid and a novel crystalline form thereof, methods for the preparation thereof, pharmaceutical compositions thereof and their use in the treatment of Human Immunodeficiency Virus (HIV) infection.Type: ApplicationFiled: October 2, 2013Publication date: April 3, 2014Inventors: Brandon H. Brown, Ernest Anthony Carra, Xiang Wang
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Publication number: 20140094486Abstract: The invention relates to novel crystalline forms of (2S)-2-tert-butoxy-2-(4-(2,3-dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid, the hydrochloride salt thereof, novel crystalline forms of the hydrochloride salt, methods for the preparation thereof, pharmaceutical compositions thereof and their use in the treatment of Human Immunodeficiency Virus (HIV) infection.Type: ApplicationFiled: October 3, 2013Publication date: April 3, 2014Inventors: Zheng Jane LI, Zhibin LI, Laibin LUO, Thomas OFFERDAHL, Soojin KIM, Bing-Shiou YANG
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Publication number: 20140094487Abstract: In one embodiment, the present application discloses 2-aza-, 2-oxa- and 2-thia-2,3-dihydro-6-azaphenalene compounds and compositions, and methods for treating a neurological disease in a patient in need thereof using the compounds and compositions as disclosed herein.Type: ApplicationFiled: November 8, 2013Publication date: April 3, 2014Applicant: Warner Babcock Institute for Green Chemistry, LLCInventors: John C. Warner, Jeffrey Allen Gladding, Srinivasa R. Cheruku, Dieu Nguyen, Jean R. Loebelenz, James J. Norman, Sambaiah Thota, John W. Lee, JR., Craig Rosenfeld
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2-AMINO-3-(IMIDAZOL-2-YL)-PYRIDIN-4-ONE DERIVATIVES AND THEIR USE AS VEGF RECEPTOR KINASE INHIBITORS
Publication number: 20140094488Abstract: The invention relates to the compounds of general formula (I): Preparation process and therapeutic use.Type: ApplicationFiled: May 16, 2012Publication date: April 3, 2014Applicant: SANOFIInventors: Alain BRAUN, Olivier DUCLOS, Gilbert LASSALLE, Franz LORGE, Valerie MARTIN, Olaf RITZELER, Aurelie STRUB