Tropanes (including Nor Or Dehydro Form) Patents (Class 514/304)
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Patent number: 10364242Abstract: Pharmaceutical compositions make up a compound acting as inhibitor of N-acylethanolamine-hydrolyzing acid amidase (NAAA), may be used for the therapeutical treatment and prevention of pain and inflammatory disorders and other disorders which benefit from the modulation of fatty acid ethanolamines, particularly palmitoylethanolamide (PEA). The compound is used in methods of inhibiting NAAA and methods of therapeutical treatment and prevention of pain and inflammation.Type: GrantFiled: November 3, 2017Date of Patent: July 30, 2019Assignee: FONDAZIONE ISTITUTO ITALIANO DI TECNOLOGIAInventors: Fabio Bertozzi, Tiziano Bandiera
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Patent number: 10251875Abstract: The inventive subject matter is directed to compositions and methods for sterile and storage stable low-dose atropine formulations with improved stability. Most preferably, the compositions presented herein are substantially preservative free and exhibit less than 0.35% tropic acid from degradation of atropine. Advantageously, contemplated formulations are also substantially free of preservatives.Type: GrantFiled: May 10, 2018Date of Patent: April 9, 2019Assignee: Nevakar Inc.Inventors: Navneet Puri, Prem Sagar Akasapu, Irfan A. Mohammed, Kumaresh Soppimath, Iouri V. Ilitchev, Tao Zhang
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Patent number: 10005711Abstract: The present invention relates to a process suitable for adoption to large scale manufacture of 1-isopropyl-3-{5-[1-(3-methoxypropyl)piperidin-4-yl]-[1,3,4]oxadiazol-2-yl}-1H-indazole oxalate of formula (I), which is a selective 5-HT4 receptor ligand intended for the symptomatic treatment of Alzheimer's disease and other disorders of memory and cognition like Attention deficient hyperactivity, Parkinson's and Schizophrenia.Type: GrantFiled: October 23, 2014Date of Patent: June 26, 2018Assignee: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Venkateswarlu Jasti
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Patent number: 9944601Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.Type: GrantFiled: September 21, 2016Date of Patent: April 17, 2018Assignee: ORYZON GENOMICS, S.A.Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Àngeles Estiarte Martinez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
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Patent number: 9827250Abstract: Ophthalmic devices, such as contact lenses, may incorporate myopia control optics in combination with therapeutic agents also known to control myopia to create a drug delivery mechanism to inhibit or arrest the progression of myopia in individuals. Any number of contact lenses incorporating myopia control optics may be combined with a therapeutic agent such as atropine, atropine sulphate monohydrate, and/or pirenzepine.Type: GrantFiled: July 31, 2012Date of Patent: November 28, 2017Assignee: Johnson & Johnson Vision Care, Inc.Inventors: Khaled Chehab, Arthur H. Shedden, Jr., Xu Cheng
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Patent number: 9603817Abstract: The invention features a method for inhibiting one or more voltage-gated ion channels in a cell by contacting the cell with (i) a first compound that activates a channel-forming receptor that is present on nociceptors and/or pruriceptors; and (ii) a second compound that inhibits one or more voltage-gated ion channels when applied to the internal face of the channels but does not substantially inhibit said channels when applied to the external face of the channels, wherein the second compound is capable of entering nociceptors or pruriceptors through the channel-forming receptor when the receptor is activated. The invention also features a quarternary amine derivative or other permanently or transiently charged derivative of a compound that inhibits one or more voltage-gated ion channels when applied to the internal face of the channels but does not substantially inhibit said channels when applied to the external face of the channels.Type: GrantFiled: September 25, 2014Date of Patent: March 28, 2017Assignees: President and Fellows of Harvard College, The General Hospital CorporationInventors: Bruce P. Bean, Clifford J. Woolf
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Patent number: 9605315Abstract: The present invention provides minimally invasive methods of detecting, diagnosing, and assessing neuronal damage associated with traumatic brain injury (TBI) or chronic traumatic encephalopathy (CTE). Specific species of microRNAs (miRNA), small, noncoding RNA molecules that play gene regulatory functions, are correlated with cellular damage and oxidative stress following TBI or CTE, allowing for rapid, minimally-invasive diagnosis and assessment of brain injury. The early identification and longitudinal assessment of neuronal damage in subjects suffering from or at risk of suffering from a TBI (e.g., football players, boxers, military personnel, fall victims) will improve clinical outcomes by guiding critical medical and behavioral decision making.Type: GrantFiled: March 26, 2015Date of Patent: March 28, 2017Assignee: The University of MontanaInventors: Sarjubhai Patel, Thomas Rau
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Patent number: 9402840Abstract: The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing such crystalline salt forms.Type: GrantFiled: August 3, 2015Date of Patent: August 2, 2016Assignee: Theravance Biopharma R&D IP, LLCInventors: Paul R. Fatheree, S. Derek Turner, Adam A. Goldblum, Robert S. Chao, Daniel Genov
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Patent number: 9387184Abstract: This invention relates to the use of pharmaceutical compositions comprising a therapeutically effective combination of Tesofensine and Metoprolol for preventing the cardiovascular side effects of Tesofensine, while leaving the robust inhibitory efficacy on food intake and body weight loss unaffected.Type: GrantFiled: November 10, 2015Date of Patent: July 12, 2016Assignee: Saniona A/SInventors: Henrik Bjork Hansen, Morten Grunnet, Bo Hjorth Bentzen, Lars Hyveled-Nielsen, Jorgen Buus Lassen, Claus Sundgreen
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Patent number: 9353106Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: January 13, 2015Date of Patent: May 31, 2016Assignee: Theravance Biopharma R&D IP, LLCInventors: Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long, Seok-Ki Choi, Adam A. Goldblum
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Patent number: 9345699Abstract: The invention provides isoquinoline, quinoline, and quinazoline derivatives to treat a variety of disorders, diseases and pathologic conditions, and more specifically to the use of isoquinoline, quinoline, and quinazoline derivatives to inhibit the hedgehog signaling pathway and to the use of those compounds to the treatment of hyperproliferative diseases and pathologic angiogenesis.Type: GrantFiled: June 9, 2010Date of Patent: May 24, 2016Assignee: NantBioScience, Inc.Inventors: Chunlin Tao, Xiaowen Sun, Hongna Han, Lukasz Koroniak, Neil Desai
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Patent number: 9265780Abstract: A method of enhancing the activity of lysosomal ?-Galactosidase A (?-Gal A) in mammalian cells and for treatment of Fabry disease by administration of 1-deoxy-galactonojirimycin and related compounds.Type: GrantFiled: December 20, 2013Date of Patent: February 23, 2016Assignee: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAIInventors: Jian-Qiang Fan, Satoshi Ishii
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Patent number: 9241938Abstract: This invention relates to the use of trigonelline compounds to increase muscle weight during periods of activity or to inhibit muscle loss during periods of inactivity.Type: GrantFiled: November 20, 2014Date of Patent: January 26, 2016Assignee: DSM IP ASSETS B.V.Inventors: Angelika Friedel, Karin Kuratli, Christof Wehrli, Karin Wertz, Swen Wolfram, Ying Wang-Schmidt
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Patent number: 9233106Abstract: The present invention relates to methods of using cocaine-binding-site ligands and cocaine-binding-site RNA aptamers to treat or prevent Alzheimer's Disease and to reduce or prevent aggregation of beta-amyloid peptides in a subject.Type: GrantFiled: July 12, 2007Date of Patent: January 12, 2016Assignee: CORNELL RESEARCH FOUNDATION, INC.Inventors: George P. Hess, Moataz M. Gadalla
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Patent number: 9211271Abstract: This invention relates to the use of pharmaceutical compositions comprising a therapeutically effective combination of Tesofensine and Metoprolol for preventing the cardiovascular side effects of Tesofensine, while leaving the robust inhibitory efficacy on food intake and body weight loss unaffected.Type: GrantFiled: February 14, 2013Date of Patent: December 15, 2015Assignee: SANIONA A/SInventors: Henrik Björk Hansen, Morten Grunnet, Bo Hjorth Bentzen, Lars Hyveled-Nielsen, Jørgen Buus Lassen, Claus Sundgreen
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Patent number: 9199993Abstract: The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: June 26, 2014Date of Patent: December 1, 2015Assignee: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Daisuke Roland Saito, Daniel D. Long, Lan Jiang, Bryan Frieman
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Patent number: 9163012Abstract: This invention relates to novel compounds of the invention pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.Type: GrantFiled: June 1, 2010Date of Patent: October 20, 2015Assignee: Vitae Pharmaceuticals, Inc.Inventors: David A. Claremon, Colin M. Tice, Linghang Zhuang, Katerina Leftheris, Yuanjie Ye, Suresh B. Singh
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Patent number: 9133184Abstract: The present application discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the application discloses the use of these compounds, a method for therapy and to pharmaceutical compositions comprising these compounds.Type: GrantFiled: April 28, 2014Date of Patent: September 15, 2015Assignee: ANIONA APSInventors: Dan Peters, Gordon Munro, Elsebet Ostergaard Nielsen, Karin Sandager Nielsen
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Patent number: 9126994Abstract: The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing such crystalline salt forms.Type: GrantFiled: January 8, 2014Date of Patent: September 8, 2015Assignee: Theravance Biopharma R&D IP, LLCInventors: Paul R. Fatheree, S. Derek Turner, Adam A. Goldblum, Robert S. Chao, Daniel Genov
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Patent number: 9108921Abstract: Compounds of general formula I: and compositions comprising compounds of general formula I that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.Type: GrantFiled: March 14, 2014Date of Patent: August 18, 2015Assignee: AGIOS PHARMACEUTICALS, INCInventors: Giovanni Cianchetta, Janeta Popovici-Muller, Robert Zahler, Sheldon Cao, Xiaolei Wang, Zhixiong Ye
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Publication number: 20150148344Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.Type: ApplicationFiled: November 21, 2014Publication date: May 28, 2015Inventors: Kerim Babaoglu, Britton K. Corkey, Robert H. Jiang, David Sperandio, Hai Yang
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Publication number: 20150099765Abstract: Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.Type: ApplicationFiled: October 6, 2014Publication date: April 9, 2015Inventors: Michael L. Hendrickson, Jeffrey C. Ockuly, Trevor M. Twose, Melinda L. Verdone, Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson
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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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Patent number: 8999972Abstract: The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, and depression. This invention could also be used for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells.Type: GrantFiled: September 13, 2011Date of Patent: April 7, 2015Assignee: Neuronascent, Inc.Inventor: Judith Kelleher-Andersson
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Patent number: 8999975Abstract: The present invention is directed to compounds of Formula I: wherein R1, R2 and n are described herein. These compounds and their pharmaceutically acceptable salts thereof are inhibitors of Cathepsin C.Type: GrantFiled: September 14, 2012Date of Patent: April 7, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Marc Grundl, Thorsten Oost, Alexander Pautsch, Stefan Peters, Doris Riether, Wolfgang Wienen
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Patent number: 8993592Abstract: Provided is a cyclic amine compound, represented by the following formula (I) that has superior acaricidal activity, has superior properties and safety, and which can be synthesized industrially advantageously, a salt thereof and an acaricide: (wherein, Cy1 and Cy2 respectively and independently represent, for example, an aryl group, R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b and R5a respectively and independently represent, for example, a hydrogen atom, R1a and R2a or R3a and R4a may together form, for example, an ethylene group, R10, R11, R20 and R21 respectively and independently represent, for example, an alkyl group, R10 or R11 may respectively or mutually, or together with an atom that bonds on Cy1, form a ring, R20 or R21 on Cy2 may respectively or mutually, or with an atom that bonds on Cy2, form a ring, m represents an integer of 0 to 5, n represents an integer of 0 to 5, p represents an integer of 0 to 5, and r represents an integer of 0 to 5).Type: GrantFiled: December 17, 2010Date of Patent: March 31, 2015Assignee: Nippon Soda Co., Ltd.Inventors: Isami Hamamoto, Keiji Koizumi, Makio Yano, Masahiro Kawaguchi, Hazumi Nomura, Tetsuya Haruyama
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Patent number: 8987249Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.Type: GrantFiled: March 12, 2014Date of Patent: March 24, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Ralf Anderskewitz, Florian Binder, Matthias Grauert, Marc Grundl, Peter Wilhelm Haebel, Thorsten Oost, Alexander Pautsch, Stefan Peters, Viktor Vintonyak
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Bridged Ring compounds As Hepatitis C Virus (HCV) Inhibitors And Pharmaceutical Applications Thereof
Publication number: 20150079028Abstract: Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.Type: ApplicationFiled: August 5, 2013Publication date: March 19, 2015Applicant: SUNSHINE LAKE PHARMA CO., LTDInventors: Yingjun Zhang, Jaincun Zhang, Hongming Xie, Qingyun Ren, Yumei Tan, Huichao Luo -
Patent number: 8980912Abstract: The present invention provides a cyclic amine compound represented by formula (I) (in formula (I), Cy1 and Cy2 independently represent a C6-10 aryl group or a heterocyclyl group; R1a to R5a independently represent a hydrogen atom or an unsubstituted or substituted C1-6 alkyl group; R10, R11, R20 and R21 independently represent an unsubstituted or substituted C1-6 alkyl group, an unsubstituted or substituted C1-6 alkoxy group, a halogen atom or the like; m, n, p, and r each represent an integer of 0 to 5; and Y represents an oxygen atom or the like) or salt thereof, and an acaricide including the same.Type: GrantFiled: February 24, 2011Date of Patent: March 17, 2015Assignee: Nippon Soda Co., Ltd.Inventors: Isami Hamamoto, Keiji Koizumi, Masahiro Kawaguchi, Hisashi Tanigawa, Takehiko Nakamura, Tomomi Kobayashi
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Publication number: 20150072970Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: ApplicationFiled: May 19, 2014Publication date: March 12, 2015Applicant: MELINTA THERAPEUTICS, INC.Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Publication number: 20150073014Abstract: The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms.Type: ApplicationFiled: July 16, 2014Publication date: March 12, 2015Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Sean M. Dalziel, Leticia M. Preza, Miroslav Rapta, Pierre-Jean Colson
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Publication number: 20150065471Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.Type: ApplicationFiled: March 28, 2013Publication date: March 5, 2015Inventors: Carlos Puig Duran, Francesc Carrera Carrera, Juan Bautista Pérez Garcia, Enrique Moyes Valles, Iolanda Marchueta Hereu
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Publication number: 20150056163Abstract: The present invention relates to methods for preventing or treating Human Immunodeficiency Virus (HIV) infection, inflammatory conditions, and graft-versus-host-disease (GVHD) in a subject. Therapeutic compositions of the present invention comprise Leukocidin E (LukE) and/or D proteins or polypeptides. The invention further relates to methods of treating Staphylococcus aureus infection by administering a composition comprising a CCR5 antagonist or any molecule that blocks LukE/D interaction with CCR5+ cells in an amount effective to treat the S. aureus infection in the subject.Type: ApplicationFiled: August 25, 2014Publication date: February 26, 2015Inventors: Victor J. Torres, Derya Unutmaz, Francis Alonzo, III
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Patent number: 8962653Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: October 1, 2013Date of Patent: February 24, 2015Assignee: Theravance Biopharma R&D IP, LLCInventors: Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long, Seok-Ki Choi, Adam A. Goldblum, Daniel Genov
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Publication number: 20150050294Abstract: The present invention relates to a method for diagnosing neuroendocrine cancers via detecting the presence of N-methyl D-asparate-associated (NMDA) glutamate receptors type 1 and/or type 2. Methods for preventing and treating neuroendocrine cancers are also disclosed.Type: ApplicationFiled: October 27, 2014Publication date: February 19, 2015Inventor: William G. North
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Patent number: 8946258Abstract: Methods of performing non-gastrointestinal endoscopic procedures with concomitant dosing with rapidly disintegrating oral formulations of single active ingredient L-Hyoscyamine rapidly dissolving tablets.Type: GrantFiled: August 13, 2013Date of Patent: February 3, 2015Inventor: Jugal K. Taneja
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Publication number: 20150030683Abstract: In certain embodiments the methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease, and/or of promoting the processing of amyloid precursor protein (APP) by the non-amyloidogenic pathway are provided. In certain embodiments the methods involve administering, or causing to be administered, to a subject in need thereof certain formulations comprising or more active agent(s) selected from the group consisting of tropisetron disulfiram, honokiol, nimetazepam, and/or derivatives or analogs thereof.Type: ApplicationFiled: February 15, 2013Publication date: January 29, 2015Inventors: Varghese John, Dale E. Bredesen, Stelios Tzannis
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Publication number: 20150031655Abstract: The disclosure provides a method of treating a mammal afflicted with an age-related disorder, comprising administering to the mammal a combination of liver X receptor (LXR) modulator and estrogen receptor (ER) modulator, in an amount effective to treat the mammal. Further disclosed are the LXR modulators and ER modulators used in the combination therapy.Type: ApplicationFiled: April 10, 2012Publication date: January 29, 2015Applicant: UNIVERSITY OF NORTH DAKOTAInventor: Othman Ghribi
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Patent number: 8940762Abstract: The present invention is directed to methods of treating pain by administering a therapeutically effective amount of an ?7 nAChR ligand or a pharmaceutically acceptable salt thereof, to a mammal in need of treatment thereof and to pharmaceutical compositions comprising such a compound or salt.Type: GrantFiled: December 22, 2010Date of Patent: January 27, 2015Assignee: AbbVie Inc.Inventors: Chih-Hung Lee, Michael R. Schrimpf, Timothy A. Esbenshade, Chang Z. Zhu
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Publication number: 20150025054Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.Type: ApplicationFiled: October 22, 2012Publication date: January 22, 2015Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estirate Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Lar
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Publication number: 20150025107Abstract: This invention relates to the use of pharmaceutical compositions comprising a therapeutically effective combination of Tesofensine and Metoprolol for preventing the cardiovascular side effects of Tesofensine, while leaving the robust inhibitory efficacy on food intake and body weight loss unaffected.Type: ApplicationFiled: February 14, 2013Publication date: January 22, 2015Inventors: Henrik Björk Hansen, Morten Grunnet, Bo Hjorth Bentzen, Lars Hyveled-Nielsen, Jorgen Buus Lassen, Claus Sundgreen
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Publication number: 20150018342Abstract: The present invention relates to fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in the claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example.Type: ApplicationFiled: February 1, 2013Publication date: January 15, 2015Applicant: SANOFIInventors: Laurent Bialy, Katrin Lorenz, Klaus Wirth, Klaus Steinmeyer, Gerhard Hessler
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Patent number: 8933236Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.Type: GrantFiled: May 21, 2013Date of Patent: January 13, 2015Assignees: Xenon Pharmaceuticals Inc., Genentech, Inc.Inventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Daniel Ortwine, Brian Safina, Shaoyi Sun, Daniel P. Sutherlin, Alla Yurevna Zenova
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Publication number: 20150010632Abstract: Aerosol formulations of granisetron useful for pulmonary delivery are provided. The formulations are useful in the reduction, elimination or prevention of nausea and vomiting associated with chemotherapy, radiation therapy, and surgery. Also provided are novel methods to treat chemotherapy-induced nausea and vomiting (CINV), radiation-induced nausea and vomiting (RINV), and post-operative nausea and vomiting (PONV) using the inhalation formulations.Type: ApplicationFiled: July 3, 2014Publication date: January 8, 2015Applicant: Luxena Pharmaceuticals, Inc.Inventors: George Lu, Xiaodong Li
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Patent number: 8927573Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: January 15, 2014Date of Patent: January 6, 2015Assignee: Theravance Biopharma R&D IP, LLCInventors: Daniel D. Long, John R. Jacobsen, Lan Jiang
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Publication number: 20140364451Abstract: In various embodiments, compositions and methods are provided for treatment and/or prevention of amyloidogenic diseases. In certain embodiments, the methods entail administering an effective amount of a tropinol ester to a subject in need thereof for prophylactic or therapeutic effect. The methods are particularly useful for prophylactic and therapeutic treatment of Alzheimer's disease. In certain embodiments, methods of reducing the risk, lessening the severity, or delaying the progression or onset of a disease characterized by beta-amyloid deposits in the brain of a mammal are also provided. In certain embodiments, methods of directly or indirectly inhibiting the C-terminal cleavage of APP resulting in the formation of APP-C31 peptide and APPneo (AP-P664) in a mammal are provided.Type: ApplicationFiled: August 1, 2012Publication date: December 11, 2014Applicant: BUCK INSTITUTE FOR RESEARCH ON AGINGInventors: Varghese John, Dale E. Bredesen
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Patent number: 8906392Abstract: Compositions, methods of making, and methods of using nanoclusters in which the nanoclusters comprise a plurality of nanoparticles having a core of nanoparticles arranged such that the surfaces of the nanoparticles contact adjacent nanoparticles, the nanoparticles comprise an active ingredient, and the nanocluster has a mass median aerodynamic diameter of from about 0.25 ?m to about 20 ?m.Type: GrantFiled: November 24, 2010Date of Patent: December 9, 2014Assignee: University of KansasInventors: Cory J. Berkland, Lianjun Shi, Nashwa El Gendy, Carl Plumley, Mark Bailey
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Publication number: 20140343091Abstract: Compounds of formula in free or salt or solvate form, where Ar is a group of formula Y is carbon or nitrogen and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.Type: ApplicationFiled: August 4, 2014Publication date: November 20, 2014Applicant: NOVARTIS AGInventors: Bernard Cuenoud, Ian Bruce, Robin Alec Fairhurst, David Beattie
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Publication number: 20140336198Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.Type: ApplicationFiled: May 16, 2012Publication date: November 13, 2014Applicants: MERCK PATENT GMBH, BIONOMICS LIMITEDInventors: Andrew Harvey, Agnes Bombrun, Rachel Cooke, Isabelle Jeanclaude-Etter, Nathan Kuchel, Jerome Molette, Jorgen Mould, Dharam Paul, Rajinder Singh, Cristina Donini, Veronique Colovray, Thomas Avery, Julia Crossman, Justin Ripper
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Patent number: RE45364Abstract: A chemical compound represented by the formula [I]: (wherein R1 represents a hydroxyl group or the like, m represents 0 or an integer of 1 to 5, R2 represents a halogen atom or the like, k represents 0 or an integer of 1 to 4, R3, R31, R4, R41, R5, R51, R6, R61, and R7 each independently represents a hydrogen atom or the like, X represents an oxygen atom or the like, and n represents 1), a salt, an N-oxide of the chemical compound represented by formula [I], and a pest control agent containing the formula [I] as its active constituent.Type: GrantFiled: January 21, 2014Date of Patent: February 3, 2015Assignee: Nippon Soda Co., Ltd.Inventors: Isami Hamamoto, Jun Takahashi, Makio Yano, Daisuke Hanai, Takao Iwasa