Tricyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 514/411)
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Patent number: 9744154Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.Type: GrantFiled: December 4, 2015Date of Patent: August 29, 2017Assignee: SIGA TECHNOLOGIES, INC.Inventors: Shanthakumar R. Tyavanagimatt, Melialani A.C.L.S. Anderson, William C. Weimers, Dylan Nelson, Tove′ C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
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Patent number: 9701676Abstract: Compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.Type: GrantFiled: August 23, 2013Date of Patent: July 11, 2017Assignee: Board of Regents of the University of Texas SystemInventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Enrique Fernandez
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Patent number: 9642841Abstract: The present invention features compositions and methods for treatment of snoring. We describe compositions comprising an antihistamine or a pharmaceutically acceptable salt thereof and one or more dietary supplements or pharmaceutically acceptable salts thereof. The compositions can be administered to a subject suffering from snoring.Type: GrantFiled: March 14, 2014Date of Patent: May 9, 2017Inventors: James M. Hand, Linda M. Hand
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Patent number: 9629825Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient selected from gabapentinoids and the physiologically acceptable salts thereof.Type: GrantFiled: March 15, 2016Date of Patent: April 25, 2017Assignee: Gruenenthal GmbHInventors: Stefanie Frosch, Klaus Linz, Thomas Christoph
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Patent number: 9462455Abstract: Disclosed is a method, performed in a Body Area Network (BAN) enabled media experience device for enabling transmission of a media experience according to a stored, predefined user configuration associated with an identification data, userID, of a BAN enabled communication device, the method comprising: establishing a connection between the BAN enabled media experience device and the BAN enabled communication device by using BAN; retrieving the identification data, userID, of the BAN enabled communication device; retrieving the stored, predefined user configuration associated with the userID of the BAN enabled communication device; and initiating transmission of the media experience by the BAN enabled media experience device according to the stored, predefined user configuration.Type: GrantFiled: November 11, 2014Date of Patent: October 4, 2016Assignees: SONY CORPORATION, SONY MOBILE COMMUNICATIONS INC.Inventors: Aleksandar Rodzevski, Thomas Bolin, Henrik Bengtsson, Erik Bengtsson, Kristian Tärnhed, Malin Larsson, Ola Thörn
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Patent number: 9447041Abstract: The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (I) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).Type: GrantFiled: September 30, 2015Date of Patent: September 20, 2016Assignee: Arena Pharmaceuticals, Inc.Inventors: Antonio Garrido Montalban, Daniel J. Buzard, John A. DeMattei, Tawfik Gharbaoui, Stephen R. Johannsen, Ashwin M. Krishnan, Young Mi Kuhlman, You-An Ma, Michael John Martinelli, Suzanne Michiko Sato, Dipanjan Sengupta
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Patent number: 9393232Abstract: Disclosed are substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compounds, pharmaceutical compositions comprising at least one such 4 substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compound processes for the preparation thereof, and the use thereof for inhibiting BET family of bromodomains and for treating disorders mediated thereby, such as certain cancers.Type: GrantFiled: April 14, 2014Date of Patent: July 19, 2016Assignee: BeiGene, Ltd.Inventors: Bo Ren, Changyou Zhou, Hexiang Wang
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Patent number: 9364472Abstract: Amino, amido, and heterocyclic compounds are disclosed. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diabetes complications, inflammation, and neurodegeneration, obesity, cancer, ischemia/reperfusion injury, cardiovascular disease and other diseases related to RAGE activity.Type: GrantFiled: August 6, 2015Date of Patent: June 14, 2016Assignees: New York University, The Research Foundation for The State University of New YorkInventors: Ann Marie Schmidt, Ravichandran Ramasamy, Alexander Shekhtman, Vivek Rai, Michaele B. Manigrasso
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Patent number: 9365586Abstract: The present invention relates to a process for preparing dithiinetetracarboximides by reaction of succinic monoamides with thionyl chloride, with continuous performance of at least one of the process steps.Type: GrantFiled: March 18, 2013Date of Patent: June 14, 2016Assignees: Bayer Cropscience AG, Bayer Intellectual Property GmbHInventors: Thomas Himmler, Thomas Geller, Lars Rodefeld, Mark James Ford, Guenter Hoemberger, Dieter Heinz
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Patent number: 9345737Abstract: Topical compositions are provided useful for treating keratosis. The compositions comprise an extract of the plant Hamelia patens and are applied topically to skin having radiation dermatitis to relieve symptoms thereof.Type: GrantFiled: February 12, 2014Date of Patent: May 24, 2016Assignee: BERRY PHARMACEUTICALS, L.L.C.Inventor: Don Wayne Berry
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Patent number: 9345736Abstract: Topical compositions are provided useful for treating radiation dermatitis. The compositions comprise an extract of the plant Hamelia patens and are applied topically to skin having radiation dermatitis to relieve symptoms thereof.Type: GrantFiled: March 16, 2013Date of Patent: May 24, 2016Assignee: BERRY PHARMACEUTICALS, L.L.C.Inventor: Don Wayne Berry
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Patent number: 9346818Abstract: Provided in the present invention are novel benzodioxole derivatives and preparation methods thereof. These compounds represented by formula (I) or pharmaceutically acceptable salts thereof have acetylcholinesterase inhibitory activity, so can be used in the treatment or prevention of Alzheimer's disease. The definitions of R1, R2 and A of formula (I) can be seen in the description.Type: GrantFiled: July 3, 2013Date of Patent: May 24, 2016Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.Inventors: Hua Bai, Xuyang Zhao, Jinqing Zhong, Yongxiang Gong, Qifeng Zhu, Xiaoyu Liu, Xiaohe Zheng, Lifei Liu
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Patent number: 9339466Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.Type: GrantFiled: March 23, 2011Date of Patent: May 17, 2016Assignee: SIGA TECHNOLOGIES, INC.Inventors: Shanthakumar R. Tyavanagimatt, Melialani A. C. L. Stone, William C. Weimers, Dylan Nelson, Tove′ C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
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Patent number: 9295665Abstract: There are provided inter alia methods and compounds useful for decreasing neovascularization (e.g., choroidal neovascularization) in a subject in need thereof.Type: GrantFiled: March 5, 2014Date of Patent: March 29, 2016Assignee: ALLERGAN, INC.Inventors: Jenny W. Wang, David F. Woodward
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Patent number: 9253980Abstract: The present invention relates to the use of dithiine-tetracarboximide compounds of formula I as defined in the description, and the N-oxides, and salts thereof for combating harmful fungi and seed coated with at least one such compound. The invention also relates to novel dithiine-tetracarboximides, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound.Type: GrantFiled: April 10, 2012Date of Patent: February 9, 2016Assignee: BASF SEInventors: Bernd Mueller, Nadege Boudet, Jochen Dietz, Wassilios Grammenos, Jan Klaas Lohmann, Richard Riggs, Ian Robert Craig, Jurith Montag, Egon Haden
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Patent number: 9221837Abstract: The present invention relates to a new process for preparing dithiine-tetracarboximides.Type: GrantFiled: September 3, 2011Date of Patent: December 29, 2015Assignee: Bayer Intellectual Property GmbHInventors: Thomas Himmler, Frank Volz, Thomas Geller
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Patent number: 9220672Abstract: The present invention relates to a peptide of the following formula (I) X1(X2)-X3-X4 or a salt or solvate thereof, wherein is an amino acid comprising two or more NH-functionalities, and X2, X3, and X4 are, independently from one another, an amino acid residue, and wherein the salt or solvate is preferably a physiologically acceptable salt or solvate.Type: GrantFiled: February 3, 2012Date of Patent: December 29, 2015Assignee: ORGANOBALANCE GMBHInventor: Christine Lang
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Patent number: 9210929Abstract: The present invention relates to novel strigolactam derivatives of formula (I), to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.Type: GrantFiled: December 14, 2012Date of Patent: December 15, 2015Assignee: Syngenta Participations AGInventors: Mathilde Denise Lachia, Alain De Mesmaeker, Emmanuelle Villedieu-Percheron, Hanno Christian Wolf, Pierre Joseph Marcel Jung, Franciscus Cornelis Lanfermeijer, Paul Willem Jan Van Den Wijngaard, Claudio Screpanti
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Patent number: 9175320Abstract: The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).Type: GrantFiled: August 20, 2014Date of Patent: November 3, 2015Assignee: Arena Pharmaceuticals, Inc.Inventors: Antonio Garrido Montalban, Daniel J. Buzard, John A. DeMattei, Tawfik Gharbaoui, Stephen R. Johannsen, Ashwin M. Krishnan, Young Mi Kuhlman, You-An Ma, Michael John Martinelli, Suzanne Michiko Sato, Dipanjan Sengupta
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Patent number: 9169207Abstract: The present invention relates to the treatment of breast cancer which is estrogen receptor positive (ER+) and/or human epidermal growth factor receptor 2 positive (HER2) and/or progesterone receptor positive (PR) and/or facilitates chromatin transcription positive (FACT+) with a curaxin, including curaxin 137. The present invention also pertains to a method of identifying a subject who has a breast cancer tumor and is likely to respond to treatment with a curaxin.Type: GrantFiled: March 27, 2013Date of Patent: October 27, 2015Assignee: Incuron, LLCInventors: Andrei Gudkov, Katerina Gurova
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Patent number: 9169220Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.Type: GrantFiled: July 2, 2014Date of Patent: October 27, 2015Assignee: SOUTHWEST RESEARCH INSTITUTEInventors: Stanton F. McHardy, Richard M. Corbett, Donald M. Maxwell, Michael W. Tidwell, Bismarck Campos, Christopher J. Bemben
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Patent number: 9102712Abstract: Novel peptide compounds and pharmaceutical compositions thereof are disclosed that have a formula represented by the following formula (I) wherein L1, L2, L3, Z, R1, R2, R4 and R5 are as described herein. The compounds demonstrate antimicrobial activity and may be prepared as pharmaceutical compositions and used for the prevention and treatment of a variety of conditions in mammals including humans where microbial invasion is involved. The present peptides are particularly valuable as their effect is rapid, broad in spectrum and mostly indifferent to resistance provided by standard antibiotics.Type: GrantFiled: August 26, 2011Date of Patent: August 11, 2015Assignee: New York UniversityInventors: Filbert Totsingan, Neville Robert Kallenbach
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Patent number: 9095140Abstract: The present invention relates to the use of novel and of known dithiine-tetracarboximides for controlling phytopathogenic fungi, and to methods of controlling phytopathogenic fungi in plant protection, and to plant protection compositions comprising these dithiine-tetracarboximides.Type: GrantFiled: September 15, 2014Date of Patent: August 4, 2015Assignee: Bayer Intellectual Property GmbHInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Jürgen Benting, Peter Dahmen, Arnd Voerste, Ralf Dunkel, Stefan Hillebrand, Klaus-Günther Tietjen, Stephane Brunet
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Patent number: 9044385Abstract: Methods for treating a vascular disease by delivering therapeutic compositions with enhanced endothelium targeting are disclosed.Type: GrantFiled: May 16, 2007Date of Patent: June 2, 2015Assignee: Abbott Cardiovascular Systems Inc.Inventors: Stephen Pacetti, Syed Faiyaz Ahmed Hossainy, Florian Niklas Ludwig
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Publication number: 20150148359Abstract: Uses of a compound of any of Formulas I-VI as a cytotoxic inhibitor of undifferentiated cells are disclosed herein, as well as pharmaceutical compositions comprising a compound of any of Formulas I-VI, and methods for identifying a lead candidate for inhibiting undifferentiated cells. Further disclosed are uses of an SCD-1 inhibitor as a cytotoxic inhibitor of undifferentiated cells.Type: ApplicationFiled: May 22, 2013Publication date: May 28, 2015Inventors: Uri Ben-David, Nissim Benvenisty, Payal Arora, Qing-Fen Gan, Ralph J. Garippa
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Publication number: 20150141418Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.Type: ApplicationFiled: January 26, 2015Publication date: May 21, 2015Applicant: PTC Therapeutics, Inc.Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
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Publication number: 20150133527Abstract: Methods are provided herein for treating cardiac arrhythmias, such as for treating an arrhythmia syndrome, for example Brugada syndrome, in a subject. In some embodiments, the methods include selecting a subject with Brugada syndrome and administering to the subject an effective amount of an agent that increases the expression or activity of SIRT1 in the subject. In some embodiments, the agent increases Nav1.5 activation. In some embodiments, the agent increases the expression or activity of SRIT1 and increases Nav1.5 activation.Type: ApplicationFiled: May 6, 2013Publication date: May 14, 2015Inventors: Barry London, Kaikobad J. Irani
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Publication number: 20150126573Abstract: The present invention relates to methods and compositions for the prevention or treatment of chronic obstructive pulmonary disease.Type: ApplicationFiled: May 7, 2013Publication date: May 7, 2015Inventors: Jorge Bernardo Boczkowski, Serge Adnot, Maylis Dagouassat, Jean-Marie Gagliolo
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Publication number: 20150126473Abstract: The present disclosure provides an isolated particle comprising very high density, ultra small, lipid depleted apo B containing particles, and may also contain cytokeratin 8. The isolated particle is useful in diagnostic assays, which are also provided.Type: ApplicationFiled: June 14, 2012Publication date: May 7, 2015Applicant: Children's Hospital & Research Center at OaklandInventors: Ronald M. Krauss, Mohmed Elfatih Ashmaig
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Patent number: 9023394Abstract: Controlled release formulations and methods for preparing controlled release formulations for delivery of active drug substances are described herein. The formulations described herein may be employed to produce pharmaceutical compositions, such as controlled release dosage forms, adjusted to a specific administration scheme.Type: GrantFiled: June 26, 2013Date of Patent: May 5, 2015Assignee: Egalet Ltd.Inventors: Christine Andersen, Karsten Lindhardt, Jan Martin Oevergaard, Louise Inoka Lyhne-Iversen, Martin Rex Olsen, Anne-Mette Haahr, Pernille Kristine Hoeyrup Hemmingsen
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Patent number: 9023864Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.Type: GrantFiled: February 7, 2013Date of Patent: May 5, 2015Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.Inventors: Carl Berthelette, Michael Boyd, John Colucci, Karine Villeneuve, Joey L. Methot
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Patent number: 9018133Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: GrantFiled: August 19, 2014Date of Patent: April 28, 2015Assignee: Bayer Intellectual Property GmbHInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
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Patent number: 9018132Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: GrantFiled: August 18, 2014Date of Patent: April 28, 2015Assignee: Bayer Intellectual Property GmbHInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
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Patent number: 9012362Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: GrantFiled: August 19, 2014Date of Patent: April 21, 2015Assignee: Bayer Intellectual Property GmbHInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
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Publication number: 20150106976Abstract: This invention relates to a pesticidal compositions containing at least one pyrrolizidine alkaloid compound derived from a plant and endophyte combination, and applying the pesticidal compositions to another plan without pesticidal protection, where upon application of the composition, the plant confers pest protection. The pyrrolizidine alkaloid compound is of Formula (I) wherein: R?H or CH3 and R??H, CH3, CHO, COCH3.Type: ApplicationFiled: December 19, 2014Publication date: April 16, 2015Inventor: Christopher Gerald Lee Pennell
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Patent number: 9006139Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: GrantFiled: August 19, 2014Date of Patent: April 14, 2015Assignee: Bayer Intellectual Property GmbHInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
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Publication number: 20150099015Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.Type: ApplicationFiled: November 24, 2014Publication date: April 9, 2015Inventor: Guochuan Emil TSAI
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Publication number: 20150094304Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: December 11, 2014Publication date: April 2, 2015Inventors: SARA SABINA HADIDA RUAH, PETER DIEDERIK JAN GROOTENHUIS, FREDRICK F. VAN GOOR, JINGLAN ZHOU, BRIAN RICHARD BEAR, MARK THOMAS MILLER, JASON MC CARTNEY, MEHDI MICHEL DJAMEL NUMA
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Patent number: 8993614Abstract: There are provided compounds of the formula wherein X, Y, Z, R1, R2, R3 and R4 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.Type: GrantFiled: March 5, 2013Date of Patent: March 31, 2015Assignee: F. Hoffmann-La Roche AGInventors: David Joseph Bartkovitz, Xin-Jie Chu, Binh Thanh Vu, Chunlin Zhao, Daniel Fishlock
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Publication number: 20150087605Abstract: Disclosed are compositions and methods for treating anthrax, inhibiting anthrax toxins and inhibiting anthrax toxin-induced cytotoxicity. Carboxylic acid-containing small molecules can be used in the methods and compositions disclosed herein, for example, sulindac and derivatives thereof may be used. Methods of screening for carboxylic acid-containing small molecules that can be used to treat anthrax are disclosed. Targeting the anthrax toxin reduces the risks of anthrax spores.Type: ApplicationFiled: September 19, 2014Publication date: March 26, 2015Inventors: J. Manuel Perez Figueroa, Oscar Santiesteban, Charalambos Kaittanis
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Patent number: 8987262Abstract: The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.Type: GrantFiled: November 16, 2012Date of Patent: March 24, 2015Assignees: Universite de Bordeaux, Centre Hospitalier Universitaire de BordeauxInventors: Christine Leaute-Labreze, Eric Dumas De La Roque, Alain Taieb, Jean-Benoit Thambo
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Patent number: 8987319Abstract: This invention provides compounds of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and or salts thereof, pharmaceutical compositions comprising a compound of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type II diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and intermediates useful in the preparation of same.Type: GrantFiled: February 4, 2011Date of Patent: March 24, 2015Assignee: Radius Health, Inc.Inventor: Chris P. Miller
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Publication number: 20150073030Abstract: The T cells specific to human collagen type II, one of the possible autoantigens, have a crucial role in the development of rheumatoid arthritis in the context of HLA-DR4. The protein-protein interactions between the T cell receptor (TCR) and the type II collagen linked to the allele MHC of class II HLA-DR4 may thus represent the target for the development of new drugs against rheumatoid arthritis. Using computational virtual screening techniques, families of pharmacologically active molecules have been identified that interfere with the TCR/collagen ll-MHCII interaction. The compounds identified here open up new possibilities in the treatment of rheumatoid arthritis.Type: ApplicationFiled: April 2, 2013Publication date: March 12, 2015Inventors: Maria Cristina De Rosa, Francesco Ria, Bruno Giardina, Gianfranco Ferraccioli, Davide Pirolli, Chiara Nicolo'
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Publication number: 20150071919Abstract: The present application relates to compositions and methods for treating a proliferative disorder by administering to a subject a pharmaceutical composition of a dual kinase inhibitor. Catecholic butanes cane serve as dual kinase inhibitors for purposes of methods described herein. Patients to be treated include those that have been treated with Tarceva or other therapeutic compounds and relapsed or are resistant to treatment. The compounds described herein may exhibit a synergistic effect when administered with another agent.Type: ApplicationFiled: September 9, 2014Publication date: March 12, 2015Inventors: Thomas F. WHITE, Dan HOTH
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Publication number: 20150072963Abstract: The invention relates to compositions and methods for regulating hair growth. Specifically, the invention relates to regulating hair growth by regulating the activity one of the prostaglandin D2 (PGD2) receptors, DP-2 (GPR44). Compositions and methods for regulating hair growth include inhibiting hair growth by administering a DP-2 agonist, or stimulating hair growth by administering a DP-2 antagonist.Type: ApplicationFiled: March 15, 2013Publication date: March 12, 2015Inventors: George Cotsarelis, Garret Fitzgerald, Luis Garza
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Publication number: 20150065551Abstract: The present invention relates to the use of novel and of known dithiine-tetracarboximides for controlling phytopathogenic fungi, and to methods of controlling phytopathogenic fungi in plant protection, and to plant protection compositions comprising these dithiine-tetracarboximides.Type: ApplicationFiled: September 15, 2014Publication date: March 5, 2015Inventors: Thomas SEITZ, Ulrike WACHENDORFF-NEUMANN, Jürgen BENTING, Peter DAHMEN, Arnd VOERSTE, Ralf DUNKEL, Stefan HILLEBRAND, Klaus-Günther TIETJEN, Stephane BRUNET
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Publication number: 20150065498Abstract: The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: May 11, 2012Publication date: March 5, 2015Inventors: Scott D. Kuduk, Douglas C. Beshore, Zhi-Qiang Yang, Youheng Shu, Daniel Pitts
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Publication number: 20150065431Abstract: The present invention provides methods of reducing cutaneous scar formation by treating a cutaneous wound with a composition comprising a therapeutic agent that is a sodium channel blocker and/or an inhibitor of the Nax/SCN7A pathway. The present invention also provides wound cover components impregnated with such compositions, kits composed of such compositions with a wound dressing or sterile wipe, and mixtures of such compositions with a topical component (e.g., cream, ointment, or gel) suitable for application to a cutaneous wound. The present invention also provides compositions, kits, devices, and methods for treating skin conditions (e.g., dermatitis, psoriasis, or other skin conditions) with such compositions and devices. Examples of such therapeutic agents include, but are not limited to, an inhibitor of a gene or protein selected from: ENac, COX-2, PGE2, PI3K, PKB, Nax Prss8, IL-1?, IL-8, SAPK, Erk gene, p38 gene, PAR2, S100A8, S100A9, S100A12.Type: ApplicationFiled: August 27, 2014Publication date: March 5, 2015Inventors: Wei Xu, Seok Jong Hong, Robert D. Galiano, Thomas A. Mustoe
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Publication number: 20150057326Abstract: A method of synthesizing cycloalkanyl[b]indoles, as well as related cycloalkanyl[b]benzofurans and cycloalkanyl[b]benzothiophenes is provided. The method is a single, multicomponent reaction that combines (1) an indole, benzofuran, or benzothiopene, (2) an aldehyde, ketone, or ketal, and (3) a diene in the presence of an acid, in particular a Ga(III) or In(III) salt. Compositions and methods of using these compounds to stimulate secretion and/or production of glucagon-like peptide-1 or inhibit the activity of Calcitonin Gene-Related Peptide receptor are also provided.Type: ApplicationFiled: November 10, 2014Publication date: February 26, 2015Applicant: Trustees of Dartmouth CollegeInventor: Jimmy Wu
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Publication number: 20150057301Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protectiong from neuron cell death.Type: ApplicationFiled: July 24, 2014Publication date: February 26, 2015Inventors: Steven L. McKnight, Joseph M. Ready, Andew A. Pieper, Jef K. De Brabander