Tetrazoles (including Hydrogenated) Patents (Class 514/381)
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Publication number: 20140323535Abstract: The present invention relates to novel pharmaceutically-useful compounds which are antagonists of the 5-oxo-ETE receptors, such as the OXE receptor. These compounds have use as therapeutic and/or prophylactic agents for diseases characterized by tissue eosinophilia, such as inflammatory conditions including respiratory diseases. The invention also relates to pharmaceutical compositions, to the use of such compounds and compositions as medicaments, and to therapeutic methods.Type: ApplicationFiled: July 7, 2014Publication date: October 30, 2014Applicants: THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/MCGILL UNIVERSITY, FLORIDA INSTITUTE OF TECHNOLOGYInventors: William S. POWELL, Joshua ROKACH
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Publication number: 20140323536Abstract: The present invention relates to a pharmaceutical combination composition comprising at least one renin-angiotensin-aldosterone system inhibitor in a subtherapeutic daily dose and at least one HMG-CoA reductase inhibitor in a subtherapeutic daily dose for use in maintaining or improving the functional and morphological properties of the arterial wall in a subject having at least one cardiovascular disorder or having at least one risk factor for cardiovascular disorder.Type: ApplicationFiled: December 7, 2012Publication date: October 30, 2014Applicant: ARTSKIN d.o.o.Inventor: Miso Sabovic
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Patent number: 8871792Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.Type: GrantFiled: June 6, 2013Date of Patent: October 28, 2014Assignee: Theravance Biopharma R&D IP, LLCInventors: Adam D. Hughes, Melissa Fleury
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Publication number: 20140314848Abstract: The present invention describes antihypertensive pharmaceutical formulations particularly formulations of losartan and indapamide.Type: ApplicationFiled: October 2, 2012Publication date: October 23, 2014Inventors: Giuseppe Soldati, Giancarlo Santus, Ricardo Vian Marques, Leticia Khater Covesi, Pedro Bordeaux Rego
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Publication number: 20140315808Abstract: A method of treating a disease or condition in which up-regulating GAGs is therapeutically beneficial is disclosed. The method comprises locally administering to a subject a therapeutically effective amount of an agent capable of down-regulating activity or expression of a component of the renin-angiotensin system.Type: ApplicationFiled: June 30, 2014Publication date: October 23, 2014Inventors: Talia WEINSTEIN, Uzi GAFTER, Zvi NEVO, Dror ROBINSON, Zoharia EVRON
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Publication number: 20140309190Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: ApplicationFiled: June 17, 2014Publication date: October 16, 2014Applicant: BIOGEN IDEC MA INC.Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Ma Bin, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
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Publication number: 20140301999Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: June 23, 2014Publication date: October 9, 2014Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
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Publication number: 20140302125Abstract: There is provided a once-a-day therapeutically synergistic pharmaceutical dosage form for treatment of cardiovascular disorders, wherein the dosage form comprises a fixed dose combination of metoprolol in extended release form and one or more calcium channel blocker, angiotensin II receptor blocker or angiotensin converting enzyme inhibitor along with one or more rate controlling excipient.Type: ApplicationFiled: August 23, 2012Publication date: October 9, 2014Applicant: Wockhardt Ltd.Inventors: Mandar Madhukar Kodgule, Premchand Dalichandji Nakhat, Amit Gupta, Girish Kumar Jain
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Publication number: 20140296292Abstract: Some embodiments include compositions and methods of using or identifying compounds that modulate the activity of the granulocyte colony-stimulating factor receptor (GCFR). Some embodiments include use of compounds to treat certain disorders, such as hematopoietic or neurological disorders.Type: ApplicationFiled: November 12, 2012Publication date: October 2, 2014Inventors: Lin Zhi, Keith Marschke, Virginia H. Grant, Steven L. Roach, Yixing Shen, Jason C. Pickens, Bijan Pedram, C. Arjan van Oeveren, Lino J. Valdez, Andrew R. Hudson
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Publication number: 20140296245Abstract: This invention is directed to benzensulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: October 30, 2012Publication date: October 2, 2014Inventors: Shaoyi Sun, Alla Yurevna Zenova, Mikhail Chafeev, Qi Jia, Zaihui Zhang, Renata Marcella Oballa
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Patent number: 8846735Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.Type: GrantFiled: October 11, 2013Date of Patent: September 30, 2014Assignee: Microdose Therapeutx, Inc.Inventors: Theodore J. Nitz, Janet A. Gaboury, Christopher J. Burns, Sylvie Laguerre, Daniel C. Pevear, Thomas A. Lessen, David J. Rys
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Publication number: 20140288090Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit cdk5-mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: November 20, 2012Publication date: September 25, 2014Inventors: Theodore Mark Kamenecka, Patrick R. Griffin, Amy S. Ripka, Jeffrey O. Saunders
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Patent number: 8841336Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: GrantFiled: September 22, 2011Date of Patent: September 23, 2014Assignee: Roche Palo Alto LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Publication number: 20140275107Abstract: Invented is a method of treating cancer or a pre-cancerous syndrome in a mammal, including a human, in need thereof which comprises the administration of an effective amount of a non-peptide thrombopoietin (TPO) receptor agonist to such mammal, suitably a human.Type: ApplicationFiled: May 30, 2014Publication date: September 18, 2014Applicant: GlaxoSmithKline LLCInventor: Connie L. ERICKSON-MILLER
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Publication number: 20140275074Abstract: The present invention is related to a compound represented by formula (I), wherein X1, X2, X3, X4, X5, R5, R6, R7, R8, n, p, q, ring A and ring B are as described in the specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 24, 2012Publication date: September 18, 2014Inventors: Kayoko Hata, Manami Masuda, Hiromi Nakai, Daisuke Taniyama, Hiroyuki Tobinaga, Yoshio Hato, Motohiro Fujiu
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Publication number: 20140275192Abstract: A compound or its pharmaceutically acceptable salt, as well as a pharmaceutical, composition containing that compound or salt dissolved or dispersed in a pharmaceutically acceptable carrier, and a method of using that compound or salt in an antibacterial treatment. A contemplated compound corresponds in structure to structural Formula I or a pharmaceutically acceptable salt of that compound, wherein V is O or NR9, Y is halogen, OR10, C1-C4 hydrocarbyl or NHR10, Z is NR2—X—R1 or CH2—R8, n is 1-6, X is H, S(O)2, C(O), C(O)NR7, C(NH)NR7 or C(O)O, and R1, R2, R7, R8, R9 and R10 are defined within.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Kenneth Charles Keiler, John Nandwa Alumasa
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Publication number: 20140275152Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Brian W. Metcalf, Zhe Li
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Publication number: 20140275193Abstract: Invented is a method of treating degenerative diseases/injuries, in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a non-peptide TPO receptor agonist to such mammal.Type: ApplicationFiled: June 2, 2014Publication date: September 18, 2014Inventors: Connie L. ERICKSON-MILLER, Julian JENKINS
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Patent number: 8835476Abstract: The synthesis and activity of novel LpxA inhibitors is described, these inhibitors present antibacterial activity. The compounds were designed based on a receptor model developed using the crystal structure of LpxA and are arranged to have a favorable binding interaction at the active site of the enzyme. In particular, the compounds present the following formula (I) where V, W, X, Y and Z can be independently C, S, N or O and P1, P2 and P3 are ligands to bind to the three points of the proposed pharmacophore model. They can be chosen from a variety of groups.Type: GrantFiled: March 6, 2006Date of Patent: September 16, 2014Inventors: Fan Wu, Donald Weaver, Chris Barden, Christopher McMaster, David Byers, Annette Henneberry, Fuqiang Ban
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Publication number: 20140256730Abstract: Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.Type: ApplicationFiled: January 13, 2014Publication date: September 11, 2014Applicant: Corsair Pharma, Inc.Inventors: Cyrus K. BECKER, Jürg R. PFISTER, Gwenaella RESCOURIO, Meenakshi S. VENKATRAMAN, Xiaoming ZHANG
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Publication number: 20140256684Abstract: The present invention relates to a method for treating ocular inflammatory diseases in a subject in need of such treatment, which comprises administering a pharmaceutical composition comprising a therapeutically effective amount of at least one agonist of Formyl peptide receptor 2.Type: ApplicationFiled: March 4, 2014Publication date: September 11, 2014Applicant: Allergan, Inc.Inventors: Richard L. Beard, John E. Donello, Veena Viswanath
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Publication number: 20140255517Abstract: In certain embodiments, the disclosure relates to methods of treating or preventing posttraumatic stress disorder comprising administering a pharmaceutical composition comprising effective amount of an angiotensin-converting enzyme inhibitor to a subject in need thereof. In certain embodiments, the angiotensin-converting enzyme inhibitor is administered in combination with an angiotensin receptor blocker.Type: ApplicationFiled: March 5, 2014Publication date: September 11, 2014Applicant: EMORY UNIVERSITYInventors: Kerry J. Ressler, Paul J. Marvar
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Publication number: 20140256685Abstract: The present invention relates to a method for treating dermal inflammation and dermal diseases by local or systemic delivery, in a subject in need of such treatment, which comprises administering a pharmaceutical composition comprising a therapeutically effective amount of at least one agonist of Formyl peptide receptor 2 (FPR2).Type: ApplicationFiled: March 4, 2014Publication date: September 11, 2014Applicant: Allergan, Inc.Inventors: Richard L. Beard, John E. Donello, Veena Viswanath, Edward Hsia
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Publication number: 20140256644Abstract: The present invention provides methods for improving muscular function or treating a muscular disorder in an individual by administering to the individual a pharmacologically effective amount of a compound that inhibits microtubule-dependent NADPH Oxidase 2 reactive oxygen species signaling production. In addition compounds that block sarcolemmal Ca2+ channel activation and/or renin-angiotensin signaling may be administered with the inhibitor of microtubule-dependent NADPH Oxidase 2 reactive oxygen species signaling production.Type: ApplicationFiled: May 22, 2014Publication date: September 11, 2014Inventors: Christopher W. Ward, Ramzi Khairallah
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Publication number: 20140256778Abstract: Inhibitors of beta lactamases and their use in treating bacterial infections are disclosed.Type: ApplicationFiled: October 12, 2012Publication date: September 11, 2014Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Ernesto Freire, Rogelio Siles, Patrick C. Ross
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Publication number: 20140255421Abstract: The invention relates generally to methods and compositions for treating sinusitis, asthma, or polyps. The invention also relates to methods and compositions for treating nasal polyps.Type: ApplicationFiled: February 12, 2014Publication date: September 11, 2014Applicant: Massachusetts Eye and Ear InfirmaryInventors: Konstantina M. Stankovic, Ralph Metson
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Patent number: 8828908Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.Type: GrantFiled: May 27, 2008Date of Patent: September 9, 2014Assignee: Syngenta LimitedInventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
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Patent number: 8828438Abstract: A solid amorphous dispersion comprises a cholesteryl ester transfer protein (CETP) inhibitor, an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase inhibitor), and a concentration enhancing polymer. At least a major portion of the CETP inhibitor in the dispersion is amorphous. The solid amorphous dispersion provides concentration-enhancement of the CETP inhibitor when administered to an aqueous use environment.Type: GrantFiled: May 22, 2006Date of Patent: September 9, 2014Assignee: Bend Research, Inc.Inventors: Dwayne Thomas Friesen, Bruno Caspar Hancock, Rodney James Ketner, David Keith Lyon, James Alan Shriver Nightingale, Ravi Mysore Shanker
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Publication number: 20140249163Abstract: The present disclosure describes new inhibitors or antagonists of Ras useful for the treatment of conditions resulting from Ras-induced or mediated cellular processes, including cellular proliferation, differentiation, apoptosis, senescence, and survival. These cellular processes may be associated with a non-malignant or malignant disease, disorder, or pathological condition. The present disclosure also describes a method for inhibiting such Ras-induced or mediated cellular processes. The method entails administering a Ras antagonist in an amount effective to inhibit such cellular processes.Type: ApplicationFiled: October 5, 2012Publication date: September 4, 2014Applicant: PICES THERAPEUTICS LLCInventors: James H. Wikel, Michael J. Brownstein
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Publication number: 20140248315Abstract: Provided are methods of enhancing an immune response and methods for reducing the recruitment of monocytes to a lymph node by administering to an individual an angiotensin II receptor blocker or a compound of Formula (I) in conjunction with an antigen. The invention also provides relate methods for amplifying vaccine immunity by administering to an individual an angiotensin II receptor blocker or a compound of Formula (I) in conjunction with an vaccine. The invention also provides related methods of inhibiting tumor growth and metastasis by administering to an individual with cancer an angiotensin II receptor blocker or a compound of Formula (I) in conjunction with an anti-tumor preparation. In addition, related compositions comprising an ARB or a compound of Formula (I) and an antigen, vaccine, or anti-tumor preparation are provided.Type: ApplicationFiled: March 3, 2014Publication date: September 4, 2014Applicant: Colorado State University Research FoundationInventors: Steven W. Dow, Daniel P. Regan, Amanda M. Guth, Leah Mitchell
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Publication number: 20140243380Abstract: The present technology provides compositions and methods for treating chronic kidney disease, end-stage renal disease, or diabetic nephropathy. The compositions comprise a nitrated lipid and an inhibitor of the renin-angiotensin-aldosterone system. The methods comprise administering a nitrated lipid in combination with an inhibitor of the renin-angiotensin-aldosterone system to a subject in need thereof, in an amount effective to treat diabetic nephropathy, chronic kidney disease, and/or end-stage renal disease. The use of a nitrated lipid with an inhibitor of the renin-angiotensin-aldosterone system exhibits a synergistic effect in treating chronic kidney disease and diabetic nephropathy.Type: ApplicationFiled: February 18, 2014Publication date: August 28, 2014Applicant: The University of Utah Research FoundationInventor: Tianxin Yang
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Publication number: 20140235556Abstract: The present invention provides, inter alia, methods for treating or ameliorating the effects of a glioma. Methods of this invention include administering to a subject in need thereof an effective amount of a first active agent, such as e.g., an angiotensin receptor blocker, an antifungal agent, a bisphosphonate, an oxytocin inhibitor, an interleukin-1 (IL-1) inhibitor, a cyclooxygenase inhibitor, an ?2? voltage-dependent calcium channel (VDCC) inhibitor, a dihydroorotate dehydrogenase inhibitor, a calcium channel blocker, a renal sodium-chloride symporter inhibitor, an a2 adrenergic agonist, a phenothiazine antipsychotic, a calcineurin inhibitor, a 5-HT agonist, an angiotensin-converting enzyme (ACE) inhibitor, a direct rennin inhibitor, or combinations thereof, and a second active agent, which is a chemotherapeutic agent. Compositions for treating or ameliorating the effects of a glioma are also provided.Type: ApplicationFiled: September 25, 2012Publication date: August 21, 2014Inventors: Reza Halse, Saurabh Saha, Jeffrey James Roix
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Publication number: 20140235622Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: January 28, 2014Publication date: August 21, 2014Applicant: Arena Pharmaceuticals, Inc.Inventors: Bradley Teegarden, Dennis Chapman, Juyi Choi, Konrad Feichtinger, Sangdon Han, Honnappa Jayakumar, Thuy-Anh Tran, Jay Xu, Ning Zou
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Patent number: 8809382Abstract: The present invention relates to novel pharmaceutically-useful compounds which are antagonists of the 5-oxo-ETE receptors, such as the OXE receptor. These compounds have use as therapeutic and/or prophylactic agents for diseases characterized by tissue eosinophilia, such as inflammatory conditions including respiratory diseases. The invention also relates to pharmaceutical compositions, to the use of such compounds and compositions as medicaments, and to therapeutic methods.Type: GrantFiled: May 4, 2010Date of Patent: August 19, 2014Assignees: The Royal Institution for the Advancement of Learning/McGill University, Florida Institute of TechnologyInventors: William S. Powell, Joshua Rokach
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Patent number: 8809306Abstract: The invention relates to the combination of Andolast, a calcium-activated potassium channel opener and glucocorticoids for the treatment of patients suffering for airway diseases. Pharmaceutical compositions comprising Andoalst and glucocorticoids are also disclosed.Type: GrantFiled: July 31, 2006Date of Patent: August 19, 2014Assignee: Rottapharm S.p.A.Inventors: Francesco Makovec, Massimo Maria D'Amato, Antonio Giordani, Lucio Claudio Rovati
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Patent number: 8809329Abstract: The present invention provides a method for diagnosing schizophrenia, and a schizophrenia diagnostic reagent or device for use in the method. The present invention further provides a therapeutic or ameliorating agent for schizophrenia, which is effective for the treatment or amelioration of schizophrenia. The therapeutic or ameliorating agent for schizophrenia contains a carbonyl scavenger or a carbonyl-modified protein formation inhibitor as an active ingredient. The method for diagnosing schizophrenia according to the present invention includes measuring at least one parameter in a subject, the parameter being selected from the group consisting of: (1) a genetic abnormality of glyoxalase I gene; (2) the expression level or activity of glyoxalase I in a biological sample; (3) the amount of a carbonyl compound or a carbonyl-modified protein that is a protein modified with the carbonyl compound; and (4) the amount of pyridoxal in a biological sample.Type: GrantFiled: July 31, 2008Date of Patent: August 19, 2014Assignees: Tokyo Metropolitan Institute of Medical Science, Renascience Co., Ltd.Inventors: Masanari Itokawa, Toshio Miyata, Makoto Arai
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Patent number: 8796331Abstract: The invention relates a pharmaceutical composition comprising a combination of: (i) the AT 1-antagonist valsartan or a pharmaceutically acceptable salt thereof; and (ii) a NEP inhibitor or a pharmaceutically acceptable salt thereof and optionally a pharmaceutically acceptable carrier and to a method for the treatment or prevention of a condition or disease selected from the group consisting of hypertension, heart failure, such as (acute and chronic) congestive heart failure, left ventricular dysfunction and hypertrophic cardiomyopathy, diabetic cardiac myopathy, supraventricular and ventricular arrhythmias, atrial fibrillation, atrial flutter, detrimental vascular remodeling, myocardial infarction and its sequelae, atherosclerosis, angina (whether unstable or stable), renal insufficiency (diabetic and non-diabetic), heart failure, angina pectoris, diabetes, secondary aldosteronism, primary and secondary pulmonary hypertension, renal failure conditions, diabetic retinopathy, the management of other vascular dType: GrantFiled: November 28, 2012Date of Patent: August 5, 2014Assignee: Novartis AGInventors: Gary Michael Ksander, Randy Lee Webb
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Patent number: 8778366Abstract: Provided herein are stable enalapril powder compositions for oral liquid formulation. Also provided herein are methods of using enalapril oral liquid formulations for the treatment of certain diseases including hypertension, heart failure and asymptomatic left ventricular dysfunction.Type: GrantFiled: June 10, 2013Date of Patent: July 15, 2014Assignees: University of Kanasas, Silvergate Pharmaceuticals, Inc.Inventors: Lian G. Rajewski, Roger A. Rajewski, John L. Haslam, Kathleen Heppert, Michael C. Beckloff, Frank Segrave, Robert Mauro, Peter Colabuono
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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: 20140193363Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: January 15, 2014Publication date: July 10, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20140194425Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: N30 Pharmaceuticals, Inc.Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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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: 20140194481Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: N30 Pharmaceuticals, Inc.Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Patent number: 8772278Abstract: The present invention relates to a method of prophylaxis or treatment of systemic diseases in cats, wherein the method comprising administration of a therapeutically effective amount of angiotensin II receptor 1 (AT-1) antagonist (sartan) to a cat in need of such a treatment.Type: GrantFiled: October 5, 2007Date of Patent: July 8, 2014Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Marcus Stark, Ulrike Sent, Ingo Lang
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Patent number: 8772276Abstract: The present invention is directed to alkyne benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: GrantFiled: April 30, 2012Date of Patent: July 8, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Jason W. Skudlarek
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Patent number: 8765797Abstract: Methods and compounds for treating cancer, dmg resistance and/or metastasis are described herein. These methods and compounds can inhibit the expression of aberrant TG2 expression and/or inhibit the binding of GTP to TG2, and thereby prevent the induction of epithelial to mesenchymal transition of cancer cells, and a stem cell-like phenotype.Type: GrantFiled: June 21, 2011Date of Patent: July 1, 2014Assignee: Board of Regents, The University of Texas SystemInventors: Kapil Mehta, Anupam Kumar, Jansina Fok, Shuxing Zhang
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Patent number: 8759365Abstract: The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.Type: GrantFiled: December 1, 2008Date of Patent: June 24, 2014Assignee: Novartis AGInventors: Muneto Mogi, Toshio Kawanami, Ken Yamada, Kayo Yasoshima, Hidetomo Imase, Takahiro Miyake, Osamu Ohmori
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Publication number: 20140170158Abstract: As described below, the present invention features compositions and methods for treating or preventing lung disease (e.g., chronic obstructive pulmonary disease (COPD), emphysema, and other conditions associated with cigarette smoke exposure) are urgently required.Type: ApplicationFiled: December 17, 2012Publication date: June 19, 2014Applicant: The Johns Hopkins UniversityInventors: Enid R. Neptune, Robert A. Wise
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Publication number: 20140163032Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: February 18, 2014Publication date: June 12, 2014Applicant: ARENA PHARMACEUTICALS, INC.Inventors: BRADLEY TEEGARDEN, Dennis Chapman, Marc Decaire, Peter I. Dosa, Konrad Feichtinger, HONNAPPA JAYAKUMAR, THUY-ANH Tran, Sonja Strah-Pleynet, Jay Xu
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Publication number: 20140163088Abstract: This invention describes methods and pharmaceutical compositions for combinational cancer treatments that are capable of inducing JNK phosphorylation and induce programmed cell death. It also identified genes as target for anti-cancer drug development and enhancement of the chemotherapeutic drug effect for the treatment of cancer. This invention points to a novel method and principle for a new avenue of developing more efficient and low or non cytotoxic cancer treatment.Type: ApplicationFiled: January 9, 2014Publication date: June 12, 2014Inventor: Ming YU