The Bicyclo Ring System Consists Of The Five-membered Hetero Ring And A Benzene Ring (e.g., Indole, Etc.) Patents (Class 514/415)
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Publication number: 20140155443Abstract: The present invention provides for a composition comprising a tryptamine based drug that acts as a 5-hydroxytryptamine-1 inhibitor in an amount sufficient to reduce the effects of psoriasis and wherein the composition is formulated for topical or oral administration.Type: ApplicationFiled: February 3, 2014Publication date: June 5, 2014Inventor: AVI DASCALU
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Publication number: 20140148439Abstract: The invention relates to the use of antioxidants such as, ascorbic acid (Vitamin C), Tocopherol (Vitamin E), vitamin A and polyphenols, for the treatment of cognitive and behavioural disorders in patients with Fragile X syndrome. Specifically, the invention relates to the use of said antioxidants in a pre-determined concentration in a therapeutic doses, in order to obtain the greatest amount of antioxidants possible in all the tissues of the organism, so as to eliminate the excess free radicals produced in the cells and to treat the aforementioned cognitive and behavioural disorders in patients with Fragile X syndrome.Type: ApplicationFiled: December 16, 2011Publication date: May 29, 2014Applicants: SERVICIO ANDALUZ DE SALUD, INSTITUTO MEDITERRANEO PARA EL AVANCE DE LA BIOTECNOLOGIA Y LA INVESTIGACIONInventors: María Yolanda De Diego Otero, Lucia María Pérez Costillas, Ignacio Del Arco Herrera
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Publication number: 20140148495Abstract: An improved monolithic drug delivery dosage form releases a pharmaceutically active agent at a predetermined rate. The dosage form comprises a salted-out or crosslinked polymer and a pharmaceutically active agent. The salted-out or crosslinked polymer functions to polymerically entangle the pharmaceutically active agent but, progressively relaxes on contact with an aqueous medium in use to release the pharmaceutically active agent at a predetermined rate.Type: ApplicationFiled: October 18, 2013Publication date: May 29, 2014Applicant: University of the Witwatersrand, JohannesburgInventors: Sibongile Ruth Sibambo, Viness Pillay, Yahya Essop Choonara
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Patent number: 8735432Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Y and W are as defined herein. The invention also concerns a method for preparing said compounds and their therapeutic use.Type: GrantFiled: October 23, 2012Date of Patent: May 27, 2014Assignee: SanofiInventors: Laurent Dubois, Yannick Evanno, Andre Malanda
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Publication number: 20140128391Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.Type: ApplicationFiled: November 1, 2013Publication date: May 8, 2014Inventors: John H. van Duzer, Ralph Mazitschek
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Publication number: 20140128408Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.Type: ApplicationFiled: January 31, 2012Publication date: May 8, 2014Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventors: Alan Kozikowski, Jay H. Kalin, Kyle V. Butier, Joel Bergman, Wayne W. Hancock
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Patent number: 8716527Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2- substituted-p-quinone derivatives as disclosed herein.Type: GrantFiled: March 4, 2009Date of Patent: May 6, 2014Assignee: Edison Pharmaceuticals, Inc.Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christopher R. Cornell
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Patent number: 8716325Abstract: The present invention provides a means for prevention and treatment of cachexia and other chronic illnesses including but not limited to the promotion of weight gain, reduction or prevention of weight loss by administration of a substance that both reduces the sensitivity of beta-adrenergic receptors and of 5-HT1a receptors. (S)-pindolol, (S)-propranolol, tertatolol or bopindolol are preferred for this purpose.Type: GrantFiled: December 5, 2007Date of Patent: May 6, 2014Assignee: PsiOxus Therapeutics LimitedInventor: David Cavalla
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Publication number: 20140121155Abstract: Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.Type: ApplicationFiled: December 27, 2013Publication date: May 1, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Jack Z. Gougoutas, Mary F. Malley, John D. DiMarco, Xiaotian S. Yin, Chenkou Wei, Jurong Yu, Truc Chi Vu, Gregory Scott Jones, Scott A. Savage
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Patent number: 8710242Abstract: The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R1 to R6, Q1 to Q8, A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.Type: GrantFiled: September 14, 2012Date of Patent: April 29, 2014Assignee: Bayer CropScience AGInventors: Markus Heil, Eike Kevin Heilmann, Alexander Sudau, Tobias Kapferer, Friedrich August Mühlthau, Peter Jeschke, Arnd Voerste, Ulrich Görgens, Klaus Raming, Ulrich Ebbinghaus-Kintscher, Mark Drewes, Martin Adamczewski, Angela Becker
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Publication number: 20140113948Abstract: The present specification discloses compositions comprising a pharmaceutical composition to reduce or maintain LDL and/or cholesterol levels in an individual and a plurality of therapeutic compounds to increase or maintain HDL levels in an individual. The present specification also discloses a treatment protocol wherein a pharmaceutical composition is administered to an individual on a schedule wherein the pharmaceutical composition is provided for a period of time and then not provided to the individual and this treatment protocol is repeated for the term of the individual's treatment.Type: ApplicationFiled: October 24, 2013Publication date: April 24, 2014Applicant: BIOCOPEA LIMITEDInventors: John Brew, Robin Mark Bannister
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Patent number: 8703808Abstract: The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: for the manufacture of a pharmaceutical composition intended for the treatment of cancer.Type: GrantFiled: August 17, 2012Date of Patent: April 22, 2014Assignees: Centre National de la Recherche Scientifique, Commissariat a l'Energie Atomique et aux Energies AlternativesInventors: Catherine Guillou, Frank Kozielski, Christophe Labriere, Francoise Gueritte, Sergey Tcherniuk, Dimitrios Skoufias, Claude Thal, Henri-Philippe Husson
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Publication number: 20140106003Abstract: The present specification provides compositions comprising a thioxanthone-based autophagy inhibitor and/or a cancer therapeutic autophagy inducing compound, pharmaceutical kits comprising these compositions, and methods of treating cancer using such compounds, compositions and kits. Additionally, the present specification provides methods of treating cancer using a thioxanthone-based autophagy inhibitor and a radiotherapy.Type: ApplicationFiled: August 6, 2013Publication date: April 17, 2014Applicant: SPECTRUM PHARMACEUTICALS, INC.Inventors: Steffan Nawrocki, Jennifer Carew, Guru Reddy
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Patent number: 8697730Abstract: Described herein are methods for the synthesis of 3-[5-(pyridin-2-ylmethoxy)-3-(2-methyl-2-propylthio)-1-[4-(2-methoxypyridin-5-yl)benzyl]-indol-2-yl]-2,2-dimethyl-propionic acid, pharmaceutically acceptable salts, pharmaceutically acceptable solvates thereof. Also described are pharmaceutical compositions suitable for oral administration to a mammal that include, as well as methods of using such oral pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.Type: GrantFiled: October 24, 2008Date of Patent: April 15, 2014Assignee: Panmira Pharmaceuticals, LLCInventors: Melissa Virginia Rewolinski, Kevin Murray Schaab, Christopher David King, Nicholas Simon Stock
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Patent number: 8697740Abstract: The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.Type: GrantFiled: January 8, 2010Date of Patent: April 15, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: John Y. L. Chung, Yanfeng Zhang, Laura Artino, Jennifer Baxter, Aaron S. Cote, Yekaterina Vaynshteyn, Donal Desmond, Jeremy Scott
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Patent number: 8691275Abstract: This disclosure relates to controlled-release melatonin compositions and related methods. In one embodiment, a controlled-release medicament composition comprises melatonin dispersed in a controlled melatonin release portion comprising a polymer matrix, the polymer matrix adapted to encapsulate the melatonin in a melatonin solubility enhancing pH environment and to maintain the melatonin solubility enhancing pH environment when the composition is located in a melatonin solubility diminishing pH environment for allowing an effective amount of melatonin to be released into the melatonin solubility diminishing pH environment.Type: GrantFiled: January 27, 2012Date of Patent: April 8, 2014Assignee: ZX Pharma, LLCInventors: Syed M. Shah, Daniel Hassan
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Patent number: 8691859Abstract: Disclosed herein are methods of inhibiting, reducing or preventing growth of or destroying bacteria of at least one bacterial strain which comprises contacting the bacteria with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing an infection or intoxication caused by bacteria of at least one bacterial strain in a subject and pharmaceutical and cosmetic compositions comprising the compounds disclosed herein.Type: GrantFiled: August 11, 2006Date of Patent: April 8, 2014Assignee: The United States of America as Represented by the Secretary of the ArmyInventors: Sina Bavari, Rekha G. Panchal, Rick Gussio
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Patent number: 8692001Abstract: The invention relates to sulfonamide compounds and methods for activating PKM2. The compounds and methods are useful in treating or preventing a disease or disorder selected from cancer, cell proliferative disorder, inflammatory disorder, metabolic disorder, and immune system disorder.Type: GrantFiled: October 26, 2011Date of Patent: April 8, 2014Assignee: Dynamix Pharmaceuticals Ltd.Inventors: Oren M. Becker, Alina Shitrit, Nili Schutz, Efrat Ben-Zeev, Avihai Yacovan, Rachel Ozeri, Tzofit Kehat, Sima Mirilashvili, Alex Aizikovich, Daniel Sherman, Vered Behar, Osnat Kashtan
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Patent number: 8686048Abstract: The present invention provides dihydroorotate dehydrogenase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.Type: GrantFiled: May 5, 2011Date of Patent: April 1, 2014Assignee: Rhizen Pharmaceuticals SAInventors: Meyyappan Muthuppalaniappan, Prashant K. Bhavar, Srikant Viswanadha, Swaroop Kumar V. S. Vakkalanka, Gayatri S. Merikapudi
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Patent number: 8686022Abstract: The present invention provides compounds according to general formula (I) which are proposed for the treatment of respiratory complaints, particularly asthma and COPD.Type: GrantFiled: August 26, 2009Date of Patent: April 1, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Holger Wagner, Birgit Jung, Frank Himmelsbach, Rolf Goeggel, Georg Dahmann
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Patent number: 8686021Abstract: Use of a benzoyl derivative of 3-aminocarbazole to produce a drug for the preventive or therapeutic treatment of a disorder selected form the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis. Method for the preventive or therapeutic treatment of a disorder selected from the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis in which a therapeutically effective quantity of a benzoyl derivative of 3-aminocarbazole according to the invention is administered to an individual.Type: GrantFiled: May 3, 2006Date of Patent: April 1, 2014Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Lorenzo Polenzani, Giorgina Mangano, Isabella Coletta, Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Caterina Maugeri
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Patent number: 8680134Abstract: The present invention provides for a composition comprising a tryptamine based drug that acts as a 5-hydroxytryptamine-1 inhibitor in an amount sufficient to reduce the effects of psoriasis and wherein the composition is formulated for topical or oral administration.Type: GrantFiled: October 22, 2010Date of Patent: March 25, 2014Inventor: Avi Dascalu
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Patent number: 8680120Abstract: A compound (I) of the present invention, which has an EP1 receptor antagonism: [wherein A represents a benzene ring or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic ring which may have a substituent, a 6-membered aromatic heterocyclic ring which may have a substituent or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.Type: GrantFiled: July 26, 2010Date of Patent: March 25, 2014Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kazuya Tatani, Naohiro Kawamura, Tatsuhiro Kondo, Atsushi Kondo
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Patent number: 8680133Abstract: Compounds and methods for treating cancer or inducing apoptosis in proliferating cells. The compounds are shown in formula I: wherein X is selected from hydroxyl, thiol, and amino; Y is selected from carboxyl and sulfonyl; R1, R2, R3, and R4 are selected from hydrogen, lower alkyl, and combinations thereof; R5, R6, and R7 are selected from hydrogen, halo, ni tro, amino, methoxy, and combinations thereof; and pharmaceutically acceptable salts thereof.Type: GrantFiled: March 26, 2012Date of Patent: March 25, 2014Assignee: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Jing-Ru Weng
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Publication number: 20140080826Abstract: 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: September 25, 2013Publication date: March 20, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: SARA SABINA HADIDA RUAH, Peter Diederik Jan Grootenhuis, Frederick F. Van Goor, Jinglan Zhou, Brian Richard Bear, Mark Thomas Miller, Jason Mc Cartney, Mehdi Numa, Xiaoqing Yang
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Patent number: 8673947Abstract: The present invention relates to method of enhancing the absorption of migraine medications and thereby treating migraines by co-administering to a subject in need thereof an effective amount of a ghrelin mimetic or pharmaceutically acceptable salt, hydrate or solvate thereof and at least one migraine medication selected from a serotonin 5-HT1B/1D receptor agonist, a tryptamine derivative, an ergoline derivative, a non-steroidal anti-inflammatory drug, or an analgesic, or any combination thereof.Type: GrantFiled: June 18, 2013Date of Patent: March 18, 2014Assignee: Helsinn Therapeutics (U.S.), Inc.Inventor: William J. Polvino
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Patent number: 8673958Abstract: A fullerene derivative having a partial structure represented by formula (1): wherein R represents a monovalent group, and r represents an integer of 0 to 4, in particular, a fullerene derivative, which has one to four structures represented by formula (1), can be applied to an organic photoelectric conversion element having a high open-circuit voltage and is therefore suitable for an organic thin-film solar cell or an organic photosensor, and thus it is extremely useful.Type: GrantFiled: July 20, 2010Date of Patent: March 18, 2014Assignee: Sumitomo Chemical Company, LimitedInventors: Yasunori Uetani, Jun Fujiwara
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Publication number: 20140073681Abstract: The present invention describes methods of treating dementia comprising administering an effective daily dose of N-(2-(6-fluoro-1H-indol-3-yl)ethyl-(2,2,3,3-tetrafluoropropoxy)benzylamine to improve or augment the effect of an acetylcholinesterase inhibitor.Type: ApplicationFiled: September 9, 2013Publication date: March 13, 2014Applicant: H. LUNDBECK A/SInventors: Ellen Schmidt, Johan Areberg
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Publication number: 20140073587Abstract: Provided herein are methods for identifying a cancer patient at risk for resistance to an HDAC inhibitor therapy, comprising obtaining a tumor sample from the cancer patient; detecting the presence of Testis-specific Y-encoded-like protein 5 (TSPYL5) expression in the sample; quantifying a level of the TSPYL5 expression in the sample, wherein a high level of the TSPYL5 expression, relative to a defined expression threshold of the TSPYL5, correlates with resistance to the HDAC inhibitor therapy; and applying the correlation to identify the cancer patient at risk for resistance to the HDAC inhibitor therapy.Type: ApplicationFiled: September 5, 2013Publication date: March 13, 2014Applicant: Celgene CorporationInventor: Torsten Bernhard Trowe
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Publication number: 20140073574Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.Type: ApplicationFiled: November 13, 2013Publication date: March 13, 2014Inventors: Robert L. Roden, Richard J. Gorczynski, Michael J. Gerber
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Patent number: 8664261Abstract: Provided are compounds of formula (I) wherein m is 0, 1 or 2; R1 is a mono- or bicyclic heterocyclic ring system including one, two or three heteroatoms selected from nitrogen, sulphur and oxygen; R2 is selected from hydrogen, methyl and ethyl; I) R3 is hydrogen, methyl, or ethyl; and R4 and R5 are independently selected from ethyl and isopropyl; and R3, R4 and R5 together have at least 6 carbon atoms; or II) any two or all of R3, R4 and R5 form together with the carbon atom to which they are attached 3-para-menthyl, bornyl, or adamantyl; having cooling properties, their use as cooling agent and compositions including them.Type: GrantFiled: May 4, 2010Date of Patent: March 4, 2014Assignee: Givaudan S.A.Inventor: Stefan Michael Furrer
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Publication number: 20140051687Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.Type: ApplicationFiled: October 21, 2013Publication date: February 20, 2014Applicant: NeurAxon, Inc.Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
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Publication number: 20140051717Abstract: The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising ergopeptines, triptans, and other compounds, including salts and derivatives of these, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.Type: ApplicationFiled: October 30, 2013Publication date: February 20, 2014Applicant: Strategic Science & Technologies, LLCInventor: Eric T. Fossel
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Patent number: 8653072Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R5 and R6 are as defined in the specification.Type: GrantFiled: January 11, 2013Date of Patent: February 18, 2014Assignee: Karo Bio ABInventors: Patrik Rhonnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstal, Aiping Cheng
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Patent number: 8653071Abstract: The present invention relates to novel ?4?2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them. The present invention relates to novel ?4?2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them.Type: GrantFiled: May 3, 2010Date of Patent: February 18, 2014Assignee: Suven Life Sciences LimitedInventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Kana Ram Kumawat, Ishtiyaque Ahmad, Pradeep Jayarajan, Anil Karbhari Shinde, Nagaraj Vishwottam Kandikere, Koteshwara Mudigonda, Venkateswarlu Jasti
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Publication number: 20140045884Abstract: Methods for the treatment of cognitive, emotional and mental ailments using therapeutically effective amounts of compositions including leukotriene receptor antagonists, leukotriene synthesis inhibitors or leukotriene modifiers, zafirlukasts, montelukasts, other members of the family—lukasts, zileutons.Type: ApplicationFiled: October 18, 2013Publication date: February 13, 2014Inventor: Jack William Schultz
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Patent number: 8648208Abstract: A compound represented by the formula (I) or a pharmacologically acceptable salt thereof is used as an activator of PPAR wherein each of R1 and R2 is hydrogen, C1-8 alkyl, C1-8 alkyl substituted with halogen, or the like; each of R3, R4, R5, and R6 is hydrogen, C1-8 alkyl, or the like; X is sulfur or the like; Y is oxygen, a bond, or the like; p is 0 or 1; A is oxygen, CH2, N—NH2, or the like; when p is 1, B is phenyl, which can have a substituent; when p is 0, B is a condensed ring such as benzisoxazole, which can have a substituent; m is an integer of 1 to 4; and n is an integer of 0 to 5.Type: GrantFiled: April 15, 2009Date of Patent: February 11, 2014Assignee: Nippon Chemiphar Co. Ltd.Inventors: Shogo Sakuma, Rie Takahashi, Hideki Nakamura
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Patent number: 8648110Abstract: Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from their activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: April 22, 2011Date of Patent: February 11, 2014Assignee: Dompe Pha.R.Ma S.p.A.Inventors: Alessio Moriconi, Marcello Allegretti, Maria Candida Cesta, Riccardo Bertini, Cinzia Bizzarri, Francesco Colotta
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Publication number: 20140037577Abstract: The present invention includes methods and compositions for the treatment and prevention of protozoal parasitic infections utilizing Diindolylmethane-related indoles. Additive and synergistic interaction of Diindolylmethane-related indoles with other known anti-parasitic and pro-apoptotic agents is believed to permit more effective therapy and prevention of protozoal parasitic infections. The methods and compositions described provide new treatment of protozoal parasitic diseases of mammals and birds including malaria, leishmaniasis, trypanosomiasis, trichomoniasis, neosporosis and coccidiosis.Type: ApplicationFiled: October 10, 2013Publication date: February 6, 2014Inventor: Michael A. Zeligs
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Publication number: 20140037622Abstract: Methods of treating a head and neck cancer are disclosed.Type: ApplicationFiled: August 2, 2013Publication date: February 6, 2014Applicants: UCL BUSINESS PLC, FOUNDATION MEDICINE, INC.Inventors: Chris Hendrik Boshoff, Timothy Robert Fenton, Matthias Alexander Lechner, Philip James Stephens, Matthew J. Hawryluk, Roman Yelensky, Garrett Michael Frampton
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Patent number: 8642624Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like.Type: GrantFiled: November 15, 2011Date of Patent: February 4, 2014Assignee: Amgen Inc.Inventors: Guoqing Chen, Jeffrey A. Adams, Jean E. Bemis, Shon Booker, Guolin Cai, Lucian V. DiPietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Stephanie Geuns-Meyer, Michael K. Handley, Qi Huang, Joseph L. Kim, Tae-Seong Kim, Alexander S. Kiselyov, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Markian M. Stec, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael D. Croghan
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Patent number: 8642770Abstract: The present invention provides an indole derivative having a melanin-concentrating hormone receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.Type: GrantFiled: January 5, 2011Date of Patent: February 4, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Shinichi Masada, Yoshito Terao, Toshiki Murata
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Publication number: 20140024694Abstract: This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds.Type: ApplicationFiled: July 15, 2013Publication date: January 23, 2014Applicant: GlaxoSmithKline Intellectual Property (No.2) Limit edInventors: Philip Stewart Turnbull, Rodolfo Cadilla
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Publication number: 20140024641Abstract: A method of treating exposure to organophosphate agents and preventing morbidity due to such exposure through the administration of a triptan compound to a subject.Type: ApplicationFiled: January 7, 2013Publication date: January 23, 2014Inventors: David Reed HELTON, David Brian FICK, Ernest H. PFADENHAUER, James LUCOT
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Publication number: 20140024657Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: September 20, 2013Publication date: January 23, 2014Applicant: President and Fellows of Harvard CollegeInventors: Junying YUAN, Emily S. Hsu
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Patent number: 8633182Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.Type: GrantFiled: May 22, 2013Date of Patent: January 21, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Dieter Hamprecht, Sara Frattini, Iain Lingard, Stefan Peters
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Publication number: 20140018355Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.Type: ApplicationFiled: June 27, 2013Publication date: January 16, 2014Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Timothy L. MACDONALD, Jerry L. NADLER, Peng CUI
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Publication number: 20140018335Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a pyridine ring, a furan ring, or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents —C(?O)—NH—SO2R6, an acidic 5-membered hetero ring group, or the like; R2 represents an optionally substituted phenyl group, an optionally substituted 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], and a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.Type: ApplicationFiled: January 24, 2012Publication date: January 16, 2014Applicant: Kissei Pharmaceutical Co., Ltd.Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
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Publication number: 20140010866Abstract: The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising ergopeptines, triptans, and other compounds, including salts and derivatives of these, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.Type: ApplicationFiled: December 29, 2011Publication date: January 9, 2014Applicant: Strategic Science & Technologies, LLCInventor: Eric T. Fossel
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Patent number: 8623853Abstract: The present invention is directed, inter alia, to methods of treating NUT midline carcinoma (NMC) by administering compounds that promote increased histone acetylation. The invention also includes assay methods for determining the responsiveness of NMC to specific histone deacetylases and other compounds.Type: GrantFiled: July 21, 2009Date of Patent: January 7, 2014Assignees: The Brigham and Women's Hospital, Inc., Dana-Farber Cancer Institute, Inc.Inventors: Christopher French, Jon Aster, Matthias Hofer, James Bradner