Patents Issued in July 10, 2014
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Publication number: 20140194427Abstract: Provided is a compound of formula (I): or a pharmaceutically acceptable salt thereof. Also provided is a method of treating, prophylaxis, or amelioration of a disease, comprising administering to a subject in need of treatment for the disease an effective amount of a compound of formula (I) described herein. In one embodiment, the method is a neurodegenerative disease, such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, Huntington's disease, or Alzheimer's disease.Type: ApplicationFiled: March 7, 2014Publication date: July 10, 2014Applicant: Biogen IDEC MA Inc.Inventor: Jianhua CHAO
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Publication number: 20140194428Abstract: The invention relates generally to novel compositions and methods comprising a scyllo-inositol compound and one or both of valproic acid compound and lamotrigine. The compositions and methods provide beneficial effects in the treatment of bipolar disorders.Type: ApplicationFiled: September 28, 2012Publication date: July 10, 2014Applicant: Elan Pharmaceuticals. Inc.Inventor: Elan Pharmaceuticals. Inc.
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Publication number: 20140194429Abstract: Compounds that are specifically toxic to cancer stem cells are disclosed.Type: ApplicationFiled: March 13, 2013Publication date: July 10, 2014Inventors: Feridoun KARIMI-BUSHERI, Habib FAKHRAI
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Publication number: 20140194430Abstract: The present invention relates to substituted aminoimidazopyridazine compounds of general formula (I): in which A, R1, R2, R3 and R4 are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: May 30, 2012Publication date: July 10, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Knut Eis, Florian Pühler, Ludwig Zorn, Arne Scholz, Philip Lienau, Mark Jean Gnoth, Ulf Bömer, Judith Günther, Jörg Fanghänel, Daniel Korr
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PYRIMIDONE DERIVATIVES AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE
Publication number: 20140194431Abstract: The present invention relates to a compound having the general formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: January 7, 2014Publication date: July 10, 2014Inventors: Andrea Wolkerstorfer, Oliver Szolar, Norbert Handler, Helmut Buschmann, Stephen Cusack, Mark Smith, Sung-Sau So, Ronald Charles Hawley, Achyutharao Sidduri, Zhuming Zhang -
Publication number: 20140194432Abstract: The present invention relates to a compound having the general formula (V), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: January 7, 2014Publication date: July 10, 2014Inventors: Andrea Wolkerstorfer, Oliver Szolar, Norbert Handler, Helmut Buschmann, Stephen Cusack, Mark Smith, Sung-Sau So, Ronald Charles Hawley, Achyutharao Sidduri
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Publication number: 20140194433Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.Type: ApplicationFiled: March 12, 2014Publication date: July 10, 2014Applicant: BASF SEInventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
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Publication number: 20140194434Abstract: Provided herein are novel ergoline derivatives and pharmaceutical 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 5-HT1B 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 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of regulating serotonin transport using the compounds and compositions disclosed herein.Type: ApplicationFiled: March 10, 2014Publication date: July 10, 2014Applicant: MAP Pharmaceuticals, Inc.Inventors: Robert O. Cook, THOMAS A. ARMER, Sergey Alexandrovich KOSAREV, Dejian Xie, Jian Zhang
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Publication number: 20140194435Abstract: Provided herein are novel ergoline derivatives and pharmaceutical 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 5-HT1B 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 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of regulating serotonin transport using the compounds and compositions disclosed herein.Type: ApplicationFiled: March 10, 2014Publication date: July 10, 2014Applicant: MAP Pharmaceuticals, Inc.Inventors: Robert O. COOK, Thomas A. ARMER, Sergey Alexandrovich KOSAREV, Dejian XIE, Jian ZHANG
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Publication number: 20140194436Abstract: The present invention relates to compounds of the formula wherein A1, A2, A3 and R1 to R8 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: February 24, 2014Publication date: July 10, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Paul Hebeisen, Hugues Matile, Stephan Roever, Matthew Wright, Sannah Zoffmann Jensen
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Publication number: 20140194437Abstract: 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: ApplicationFiled: October 11, 2013Publication date: July 10, 2014Inventor: Andreas Haupt
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Publication number: 20140194438Abstract: Provided are compositions and methods for treating or preventing nausea and vomiting in patients undergoing chemotherapy, radiotherapy, or surgery.Type: ApplicationFiled: November 1, 2013Publication date: July 10, 2014Applicant: Helsinn Healthcare S.A.Inventors: Fabio TRENTO, Sergio CANTOREGGI, Giorgia ROSSI, Roberta CANNELLA, Daniele BONADEO
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Publication number: 20140194439Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.Type: ApplicationFiled: December 4, 2013Publication date: July 10, 2014Inventor: Joseph P. Errico
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Publication number: 20140194440Abstract: The present invention relates to novel 5,6-disubstituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the manufacture of a medicament.Type: ApplicationFiled: September 27, 2013Publication date: July 10, 2014Inventors: Wilfried Braje, Thorsten Oost, Astrid Netz, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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3-(BENZOIMIDAZOL-2-YL)-INDAZOLE INHIBITORS OF THE WNT SIGNALING PATHWAY AND THERAPEUTIC USES THEREOF
Publication number: 20140194441Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: ApplicationFiled: January 8, 2014Publication date: July 10, 2014Applicant: Samumed, LLCInventors: Sunil Kumar KC, John Hood -
Publication number: 20140194442Abstract: The invention describes anti-cancer therapies comprising using dual Aurora kinase/MEK inhibitors as described herein.Type: ApplicationFiled: January 12, 2012Publication date: July 10, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Flavio Solca, Ulrich Guertler, Michael Sanderson, Ulrike Tontsch-Grunt, Irene Waizenegger
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Publication number: 20140194443Abstract: The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.Type: ApplicationFiled: January 10, 2014Publication date: July 10, 2014Applicant: Grünenthal GmbHInventors: Sonja Nordhoff, Sebastian Wachten, Achim Kless, Felix Voss, Stefanie Ritter
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Publication number: 20140194444Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: January 15, 2014Publication date: July 10, 2014Inventors: Juan-Miguel Jimenez, Andrew Miller, Jeremy Green, Huai Gao, Gregory Henkel, Michael Liu, Timothy Neuberger
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Publication number: 20140194445Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, 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: ApplicationFiled: March 10, 2014Publication date: July 10, 2014Applicant: SANOFIInventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
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Publication number: 20140194446Abstract: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.Type: ApplicationFiled: November 26, 2013Publication date: July 10, 2014Applicant: Pharmacyclics, Inc.Inventors: Jospeh J. BUGGY, Laurence Elias, Gwen Fyfe, Eric Hedrick, David J. Loury, Tarak D. Mody
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Publication number: 20140194447Abstract: Compounds and their pharmaceutically acceptable salts for treatment of ?-amyloid diseases, such as observed in Alzheimer's disease and synucleinopathies, such as Parkinson's disease.Type: ApplicationFiled: October 10, 2012Publication date: July 10, 2014Inventors: Luke Esposito, Kelsey Hanson, Marisa C. Yadon, Thomas Lake, Alan D. Snow, Joel Cummings, Anil Kumar
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Publication number: 20140194448Abstract: The present invention relates to a new application of phosphodiesterase inhibitors for couple infertility treatment which forms an effective alternative to the invasive assisted reproductive techniques such as conjugal artificial insemination and which consists of the transvaginal administration of a phosphodiesterase inhibitor immediately before and/or after coitus. It also relates to dosage forms suitable for the intravaginal administration of phosphodiesterase inhibitors.Type: ApplicationFiled: June 20, 2012Publication date: July 10, 2014Inventors: Maria Carmen Pardina Palleja, Miguel Angel Vaz-Romero Uña
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Publication number: 20140194449Abstract: Provided herein is an optically active pyrozolylaminoquinazaline, and pharmaceutical compositions thereof. Also provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a JAK-mediated condition, disorder, or disease. Further provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a proliferative disease, inflammatory disease, or renal disease.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: Ambit Biosciences Corp.Inventors: Mark W. HOLLADAY, Eduardo SETTI
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Publication number: 20140194450Abstract: The present invention is directed to compositions and methods for the treatment of post-chemotherapeutic hypotrichosis. More specifically, the present invention is directed to the use of compositions comprising bimatoprost for the treatment of post-chemotherapeutic hypotrichosis which may be applied before, during and after receiving chemotherapeutic treatment.Type: ApplicationFiled: January 10, 2013Publication date: July 10, 2014Applicant: ALLERGAN, INC.Inventors: Gurpreet Ahluwalia, Frederick C. Beddingfield, Sydney G. Edwards, Scott M. Whitcup
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Publication number: 20140194451Abstract: Compounds which inhibit the small G protein Rho GTPase cell division cycle protein Cdc42 are provided. Morphological analyses of filopodia, western blots of Ccd42 phosphorylation, and effects on cellular wound healing and on growth cone formation all demonstrate that the described compounds are able to inhibit all tested Cdc42-mediated processes. The compounds effectively inhibit, the effects of Cdc42 and effectively inhibit Cdc42-related cellular functions involving actin, such as Golgi organization and cell movement. Furthermore, the described Cdc42 inhibitor compounds may be provided as a medicament for the treatment of various conditions.Type: ApplicationFiled: November 22, 2013Publication date: July 10, 2014Inventors: Qun Lu, Huchen Zhou, Yanhua Chen, Amy Friesland
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Publication number: 20140194452Abstract: The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.Type: ApplicationFiled: January 10, 2014Publication date: July 10, 2014Applicant: Grünenthal GmbHInventors: Sonja Nordhoff, Sebastian Wachten, Achim Kless, Felix Voss, Stefanie Ritter
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Publication number: 20140194453Abstract: A novel solid form of Rosuvastatin comprises as the active ingredient a salt of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)-amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] and vanillin or vanillin derivatives. The crystal comprising the two components, and minor amounts of water, shows improved properties such as crystallization behavior stability and decreased hydroscopic behavior.Type: ApplicationFiled: January 31, 2014Publication date: July 10, 2014Applicant: BASF SEInventors: Andreas HAFNER, Fritz BLATTER, Martin SZELAGIEWICZ, Bernd SIEBENHAAR
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Publication number: 20140194454Abstract: Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of immediate release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of immediate release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: TheraVida, Inc.Inventors: Mehdi PABORJI, Kenneth L. DUCHIN, Wendy Jade Limayo HERNANDEZ, Roger S. FLUGEL
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Publication number: 20140194455Abstract: A thermoformed pharmaceutical dosage form having a breaking strength of at least 300 N, said dosage form comprising a pharmacologically active ingredient (A), a free physiologically acceptable acid (B) in an amount of from 0.001 wt.-% to 5.0 wt.-%, based on the total weight of the pharmaceutical dosage form, and a polyalkylene oxide (C) having a weight average molecular weight Mw of at least 200,000 g/mol.Type: ApplicationFiled: February 28, 2014Publication date: July 10, 2014Applicant: GRUNENTHAL GMBHInventors: Lutz BARNSCHEID, Eric GALIA, Sebastian SCHWIER, Ulrike BERTRAM, Anja GEISSLER, Kornelia GRIESSMANN, Johannes BARTHOLOMÄUS
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Publication number: 20140194456Abstract: Abuse-resistant, controlled release opioid tablets are a combination containing an opioid antagonist such as naloxone at a level above that needed to suppress the euphoric effect of the opioid, if the combination were crushed to break the controlled release properties causing the opioid and opioid antagonist to be released as a immediate release product as a single dose. The controlled release nature of the table prevents the accumulation of orally effective amounts of opioid antagonist when taken normally. The opioid antagonist is contained in a controlled-release matrix and released, over time, with the opioid.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: Purdue PharmaInventors: Frank S. CARUSO, Huai-Hung KAO
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Publication number: 20140194457Abstract: A compound of formula I is disclosed. Compounds of formula I are useful as analgesics, anti-inflammatory agents, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: ApplicationFiled: March 12, 2014Publication date: July 10, 2014Applicant: Rensselaer Polytechnic InstituteInventor: Mark P. WENTLAND
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Publication number: 20140194458Abstract: Provided is a 10-methoxycamptothecine derivate of formula (1), wherein R is selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, aryl substituted C1-6 alkyl, phosphate substituted C1-6 alkyl, amino-substituted C1-6 alkyl, carboxyl substituted C1-6 alkyl, hydroxyl substituted C1-6 alkyl, and amide- substituted C1-6 alkyl; R1 is selected from hydrogen and t-butoxycarbonyl substituted amino. Also provided in the present invention are the preparation method of the derivate and the use thereof in anti-tumor drug preparation.Type: ApplicationFiled: June 15, 2012Publication date: July 10, 2014Applicant: Northeast Forestry UniversityInventors: Yang Wang, Xiufeng Yan, Lijia Jing, Weimin Ding, Jian Zheng, Qiuying Pang, Tao Yu
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Publication number: 20140194459Abstract: Methods and compositions for the treatment of alpha-adrenoceptor mediated conditions.Type: ApplicationFiled: March 5, 2014Publication date: July 10, 2014Applicant: Vanda Pharmaceuticals, Inc.Inventors: Mihael H. Polymeropoulos, Paolo Baroldi, Curt D. Wolfgang
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Publication number: 20140194460Abstract: A pharmaceutical composition comprising quinagolide for the treatment and/or prevention of endometriosis.Type: ApplicationFiled: August 7, 2013Publication date: July 10, 2014Applicant: Ferring B.V.Inventors: Antonio Pellicer-Martinez, Carlos Simon-Valles, Edurne Novella-Maestre, Joan Carles Arce Saez
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Publication number: 20140194461Abstract: Described herein are liquid rapamycin formulations. Described herein are methods of treating or preventing diseases or conditions, such as choroidal neovascularization, wet AMD and dry AMD, and preventing transition of dry AMD to wet AMD, using the liquid rapamycin formulations described herein.Type: ApplicationFiled: January 9, 2014Publication date: July 10, 2014Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Sreenivasu MUDUMBA, Philippe JM DOR, Thierry NIVAGGIOLI, David A. WEBER, Sidiq FAROOQ
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Publication number: 20140194462Abstract: The present application is related to compounds represented by Formula I, which are novel allosteric modulators of ?7nAChR. The application also discloses the treatment of disorders that are responsive to modulation of acetylcholine action on ?7nAChR in a mammal by administering an effective amount of a compound of Formula I.Type: ApplicationFiled: October 8, 2013Publication date: July 10, 2014Applicant: Anvyl LLCInventor: Richard Kanner
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Publication number: 20140194463Abstract: Compounds that are specifically toxic to cancer stem cells are disclosed.Type: ApplicationFiled: March 13, 2013Publication date: July 10, 2014Inventors: Feridoun KARIMI-BUSHERI, Habib FAKHRAI
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Publication number: 20140194464Abstract: The present invention relates to the use of crenolanib, in a pharmaceutically acceptable salt form for the treatment of FLT3 mutated proliferative disorders driven by constitutively activated mutant FLT3, and to a method of treatment of warm-blooded animals, preferably humans, in which a therapeutically effective dose of crenolanib is administered to an animal suffering from said disease or condition:Type: ApplicationFiled: October 14, 2013Publication date: July 10, 2014Inventor: Vinay K. Jain
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Publication number: 20140194465Abstract: Compounds that are specifically toxic to cancer stem cells are disclosed.Type: ApplicationFiled: March 13, 2013Publication date: July 10, 2014Inventors: Feridoun KARIMI-BUSHERI, Habib FAKHRAI
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Publication number: 20140194466Abstract: The invention relates to perhexiline, or a pharmaceutically acceptable salt or enantiomer thereof, for use in the treatment of hypertrophic cardiomyopathy, as well as to a method of treating HCM, which comprises administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt or enantiomer thereof, to treat said HCM. The invention further relates to a treatment programme for treating HCM, which involves the co-use or co-administration of perhexiline with one or more other compounds that are advantageous in treating HCM or the symptoms thereof.Type: ApplicationFiled: February 21, 2014Publication date: July 10, 2014Applicant: The University of BirminghamInventors: Houman ASHRAFIAN, Michael Paul FRENNEAUX
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Publication number: 20140194467Abstract: The invention relates to novel biological markers for plasma cell disorders, such as multiple myeloma, and in particular to the use of microRNAs as diagnostic and prognostic markers in assays for detecting such disorders. The invention also relates to methods of determining the efficacy of treating a plasma cell disorder with a therapeutic agent, and kits for carrying 5 out the assays and methods. The assays are qualitative and/or quantitative, and are adaptable to large-scale screening and clinical trials.Type: ApplicationFiled: December 13, 2011Publication date: July 10, 2014Applicant: THE UNIVERSITY OF SUSSEXInventors: Sarah Faith Newbury, Timothy James Telfer Chevassut, Christopher Iain Jones, Maria Vasilyevna Zabolotskaya, Helen Jayne Susan Stewart
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Publication number: 20140194468Abstract: The present invention provides compounds S3I-201.1066 (Formula 1) and S3I-201.2096 (Formula 2) as selective Stat3 binding agents that block Stat3 association with cognate receptor pTyr motifs, Stat3 phosphorylation and nuclear translocation, Stat3 transcriptional function, and consequently induced Stat3-specific antitumor cell effects in vitro and antitumor response in vivo.Type: ApplicationFiled: November 10, 2013Publication date: July 10, 2014Applicants: The Governing Council of the University of Toronto, University of Central Florida Research Foundation, Inc.Inventors: James Turkson, Patrick Gunning
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Publication number: 20140194469Abstract: Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: ApplicationFiled: December 5, 2013Publication date: July 10, 2014Applicant: Quanticel Pharmaceuticals, Inc.Inventors: Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennen Wallace
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Publication number: 20140194470Abstract: The invention relates to compounds corresponding to formula (I), in the form of the base or of an acid-addition salt: in which n is equal to 0, 1, 2, 3 or 4; m is equal to 0, 1 or 2; o is equal to 0 or 1; X represents a group —CH2, —CH(R?)—, —NH(R?)— or a heteroatom chosen from O and S, it being understood that R? represents a group —(C1-C5)alkyl, —(C1-C5)alkoxy, —CH2-aryl, —C(O)R5 or —COOR5; R1 represents an oxo group, —COOR5, —W—OH or —W—NR5R6; R2 represents an H atom or a group chosen from the groups (i) —(C1-C5)alkyl, (ii) —(C1-C5)alkoxy, (iii) —COOR5, (iv) —NR5R6, (v) —C(O)—NR5R6, (vi) —SO2—NR3R4, (vii) heteroaryl optionally substituted with a group —(C1-C5)alkyl, (viii) —W-aryl, (ix) —W-heteroaryl, (x) —O—W-aryl, (xi) —O—W-heteroaryl and (xii) —O—W—NR5R6; it being understood that R3 and R4, (i) which may be identical or different, represent, independently of each other, an H atom, a group —(C1-C5)alkyl, —(C3-C6)cycloalkyl, aryl, heteroaryl, —CH2-heteroaryl, —(C1-C5)alkyl-NR5R6, —W—OH or —W—NR5R6; orType: ApplicationFiled: March 7, 2014Publication date: July 10, 2014Applicant: SANOFIInventors: Jean-Michel Altenburger, Valerie Fossey, Stephane Illiano, Geraldine Manette
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Publication number: 20140194471Abstract: In one aspect, the invention relates to substituted 1-benzylindolin-2-one analog compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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: January 6, 2013Publication date: July 10, 2014Applicant: Vanderbilt UniversityInventors: Craig W. Lindlsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney
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Publication number: 20140194472Abstract: Described herein are compounds, pharmaceutical compositions and methods for inhibiting the expression of a vitamin D receptor target gene, inhibiting interactions between the vitamin D receptor and at least one vitamin D receptor coactivator, for treating cancer in a subject, and for inhibiting angiogenesis in a subject.Type: ApplicationFiled: August 26, 2012Publication date: July 10, 2014Applicants: WOMEN AND INFANTS' HOSPITAL OF RHODE ISLAND, UWM RESEARCH FOUNDATION, INC.Inventors: Alexander E. Arnold, Preetpal Singh Sidhu, Premchendar Nandhikonda, Rakesh K. Singh
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Publication number: 20140194473Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2 and R3 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: December 10, 2013Publication date: July 10, 2014Applicant: E I Du Pont De Nemours And CompanyInventor: THOMAS FRANCIS PAHUTSKI, JR.
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Publication number: 20140194474Abstract: Disclosed are a composition for preventing and treating atherosclerosis which includes chalcone compound. In particular, the chalcone compound bound with 2-hydroxyl in ring A and 4?-methyoxy in ring B has versatile therapeutic potentials on anti-atherosclerosis by acting as PPAR? inducer, p44/42 MAPK inhibitor and cell cycle blocker and does not show toxicity to human aortic smooth muscle cells (HASMCs). In addition, the chalcone compound exhibits synergistic effect with the PPAR? ligand (rosiglitazone) to inhibit cell proliferation and the upregulation of cyclin D1, cyclin D3, interleukin-1? (IL-1?) and interleukin-6 (IL-6) induced by oxidized low density lipoprotein (Ox-LDL).Type: ApplicationFiled: March 10, 2014Publication date: July 10, 2014Applicant: Kaohsiung Medical UniversityInventors: Yang-Chang WU, Fang-Rong Chang, Tusty-Jiuan Hsieh, Suh-Hang Juo, An-Shen Lin, Ying-Chi Du
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Publication number: 20140194475Abstract: Methods and formulations for treating animal ectoparasites, effective against parasites such as fleas and ticks are provided. The methods comprise topically co-administering a non-mobile insect growth regulator and a mobile insect growth regulator to the animal. Parasiticidal formulations for treating animal ectoparasites are also provided, which can be safe to use and avoid the many common deleterious side effects of conventional topical formulations. The topical formulations comprise a combination of two insect growth regulators, a non-mobile insect growth regulator and a mobile insect growth regulator. The topical formulation can be packaged with the two insect growth regulators together or packaged to prevent mixing of the two insect growth regulators prior to administering the topical insecticide formulation to the animal.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: The Hartz Mountain CorporationInventors: William Ecker, Lance Hemsarth
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Publication number: 20140194476Abstract: The present invention relates to a compound having the general formula (II), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: January 7, 2014Publication date: July 10, 2014Inventors: Andrea Wolkerstorfer, Oliver Szolar, Norbert Handler, Helmut Buschmann, Stephen Cusack, Mark Smith, Sung-Sau So, Ronald Charles Hawley