Plural Six-membered Hetero Rings Consisting Of One Nitrogen And Five Carbon Atoms Patents (Class 514/332)
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Publication number: 20130065911Abstract: The present invention relates to compounds of the formula wherein R1 to R3 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 10, 2012Publication date: March 14, 2013Inventors: Uwe Grether, Stephan Roever
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Patent number: 8394834Abstract: The present invention relates to a compounds of formula I wherein R1, R2, Ar1, Ar2, R?, R?, m, n, and o are defined in the specification or to a pharmaceutically active salt, racemic mixture, enantiomer, optical isomer or to tautomeric form thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: GrantFiled: August 16, 2010Date of Patent: March 12, 2013Assignee: Hoffman-La Roche Inc.Inventors: Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angelique Patiny-Adam, Hasane Ratni, Claus Riemer
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Patent number: 8389519Abstract: The present invention provides adamantyl-diamide derivatives of formula (I): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: GrantFiled: May 15, 2012Date of Patent: March 5, 2013Assignee: H. Lundbeck A/SInventors: Hermogenes N. Jimenez, Guiying Li, Dario Doller, Michel Grenon, Andrew D. White, Gil Ma, Maojun Guo
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Publication number: 20130053418Abstract: The present invention provides acyclic, geminal-dinitro organic compounds, methods of synthesizing the compounds, pharmaceutical compositions, therapeutic methods, and medical kits for treating various conditions using such compounds and pharmaceutical compositions. The compounds and compositions are useful in the treatment of cancer.Type: ApplicationFiled: August 24, 2012Publication date: February 28, 2013Inventors: Jan Scicinski, Bryan T. Oronsky, Robert Wardle, Louis Cannizzo, Nicholas A. Straessler
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Publication number: 20130053417Abstract: The invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity, the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.Type: ApplicationFiled: March 21, 2012Publication date: February 28, 2013Applicant: JAPAN TOBACCO INC.Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
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Publication number: 20130040992Abstract: The present invention relates to substituted 2,6-diamino-3,5-dicyano-4-arylpyridines of the formula (I) wherein the definitions of substituent groups R1-R7 are as provided in the specification and claims, to a pharmaceutical composition containing such a compound, to a process for preparation of such materials, and to their use as medicaments for the treatment of cardiovascular disorders and diabetes.Type: ApplicationFiled: August 13, 2012Publication date: February 14, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ulrich Rosentreter, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stasch
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Publication number: 20130040975Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: ApplicationFiled: August 10, 2012Publication date: February 14, 2013Applicant: NEUROCRINE BIOSCIENCES, INC.Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Jinghua Yu, Willy Moree, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
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Publication number: 20130035339Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).Type: ApplicationFiled: September 13, 2012Publication date: February 7, 2013Applicant: Gilead Sciences, IncInventors: Britton Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, JR., Gregory Notte
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Patent number: 8367836Abstract: The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2, R3, R4, R5 and R6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.Type: GrantFiled: April 27, 2010Date of Patent: February 5, 2013Assignee: Elan Pharmaceuticals, Inc.Inventors: Ying-zi Xu, Shendong Yuan, David Wone, Andrei Konradi
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Tris-Quaternary Ammonium Salts and Methods for Modulating Neuronal Nicotinic Acetylcholine Receptors
Publication number: 20130030018Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: ApplicationFiled: September 21, 2012Publication date: January 31, 2013Inventor: University of Kentucky Research Foundation -
Publication number: 20130029961Abstract: Heterocyclic aza compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds and also methods of using these compounds for the treatment and/or inhibition of pain and further diseases and/or disorders.Type: ApplicationFiled: July 25, 2012Publication date: January 31, 2013Applicant: Gruenenthal GmbHInventors: Robert FRANK, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
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Patent number: 8362256Abstract: The present invention relates to the salts of N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl)amino-3-pyridine carboxamide, especially hydrochloride and mesylate thereof, and the use of said salts in the preparation of an antineoplastic medicament.Type: GrantFiled: June 11, 2009Date of Patent: January 29, 2013Assignee: Jiangsu Hengrui Medicine Co. Ltd.Inventors: Kaihong Yuan, Piaoyang Sun, Yunshu Zhou, Yongjiang Chen
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Publication number: 20130023495Abstract: The present invention relates to the use of a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia. The present invention further relates to the use of a pharmaceutical composition comprising a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia.Type: ApplicationFiled: March 29, 2011Publication date: January 24, 2013Applicant: Novartis AGInventors: Charles Meyers, Michael H. Serrano-Wu, Tom Thuren
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Patent number: 8354433Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, for the use as a medicament.Type: GrantFiled: May 3, 2010Date of Patent: January 15, 2013Assignee: 4SC AGInventors: Daniel Vitt, Manfred Groeppel, Roland Baumgartner, Johann Leban
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Publication number: 20130012385Abstract: The invention disclosed in this document is related to field of pesticides and their use in controlling pests. In particular compounds having the following formula are disclosed.Type: ApplicationFiled: September 10, 2012Publication date: January 10, 2013Applicant: DOW AGROSCIENCES LLCInventors: Benjamin M. Nugent, Ann M. Buysse, Jonathan M. Babcock, Matthias S. Ober, Timothy P. Martin
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Patent number: 8349830Abstract: The present invention is directed to aryl aminopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: October 26, 2010Date of Patent: January 8, 2013Assignee: Merck Sharp & DohmeInventors: Michael J. Breslin, Christopher D. Cox, Izzat T. Raheem
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Publication number: 20130004586Abstract: Compositions, solid polymeric compositions, and/or articles of manufacture are provided that can include a polymer matrix having a plurality of ion-exchange particles distributed therein. Products by process are provided that can include prior to solidifying the polymeric precursors, blending the precursors with ion-exchange particles to form a mixture, and solidifying the mixture to form a solid polymeric composition product. Solid polymeric composition production methods are also provided that can include providing a plurality of ion-exchange particles, prior to solidifying the polymeric precursors, blending the precursors with the ion-exchange particles to form a mixture, and solidifying the mixture to form a solid polymeric composition. Article of manufacture production methods are provided that can include incorporating a solid polymeric composition into an article of manufacture, the solid polymeric composition including a polymer matrix and a plurality of ion-exchange particles distributed therein.Type: ApplicationFiled: June 25, 2012Publication date: January 3, 2013Inventors: David J. Vachon, Nathan Knapp
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Patent number: 8344001Abstract: Compound of formula (I) wherein W, X, Y, Z is —C(R1)? or N; R1 is hydrogen or alkyl, V is N or C (i.e.Type: GrantFiled: May 19, 2008Date of Patent: January 1, 2013Assignee: High Point Pharmaceuticals, LLCInventors: Rolf Hohlweg, Jane Marie Lundbeck, Johannes Cornelis de Jong
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Publication number: 20120329821Abstract: The invention disclosed in this document is related to field of pesticides and their use in controlling pests.Type: ApplicationFiled: September 7, 2012Publication date: December 27, 2012Applicant: DOW AGROSCIENCES LLCInventors: Zoltan L. Benko, Gary D. Crouse, William R. Erickson, James M. Gifford, Gary D. Gustafson, Nailah Orr, Gerald B. Watson
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Publication number: 20120322801Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.Type: ApplicationFiled: March 4, 2011Publication date: December 20, 2012Applicant: Amakem NVInventors: Dirk Leysen, Olivier Defert, Nadzeya Kaval, Petra Blom, Sandro Boland
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Publication number: 20120316147Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: June 1, 2012Publication date: December 13, 2012Inventors: Caterina Bissantz, Uwe Grether, Paul Hebeisen, Atsushi Kimbara, Qingping Liu, Matthias Nettekoven, Marco Prunotto, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch, Christoph Ullmer, Zhiwei Wang, Wulun Yang
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Patent number: 8329732Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: GrantFiled: August 31, 2009Date of Patent: December 11, 2012Assignee: Novartis AGInventors: Matthew T. Burger, Wooseok Han, Jiong Lan, Gisele Nishiguchi
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Publication number: 20120309791Abstract: The present invention relates to novel compounds of formula (II) that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating, or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins.Type: ApplicationFiled: July 25, 2012Publication date: December 6, 2012Applicant: AC IMMUNE SAInventors: Wolfgang FROESTL, Nampally Sreenivasachary, Sophie Lohmann, Maria Pilar Lopez Deber, Andreas MUHS, Maria Pihlgren Bosch
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Publication number: 20120294826Abstract: The present invention provides, inter alia, methods for ameliorating an adverse effect in a patient caused by an acute transfusion into the patient of a composition containing aged red blood cells using an iron chelator. Apparatuses and kits for ameliorating such adverse effects are also provided.Type: ApplicationFiled: December 1, 2011Publication date: November 22, 2012Inventors: Steven L. Spitalnik, Eldad A. Hod, Gary M. Brittenham
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Publication number: 20120295922Abstract: The present invention provides methods for treating and/or preventing mucostitis with one or more compounds, or pharmaceutically acceptable salts thereof, disclosed herein, or compositions comprising the same.Type: ApplicationFiled: May 15, 2012Publication date: November 22, 2012Applicant: POLYMEDIX, INC.Inventors: Richard W. Scott, Bozena Korczak
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Publication number: 20120295889Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: May 16, 2012Publication date: November 22, 2012Applicant: Merck Serono S.A.Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
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Publication number: 20120294927Abstract: The invention relates to a sterile wound dressing having a backing and a nonabsorbent elastomer wound contact layer, wherein the elastomer matrix is formed by a synthetic three-block elastomer, preferably a copolymer of polystyrene block and polyolefin block (SEPS, SEBS, SEEPS, etc.) or mixtures thereof, wherein the total polymer content is less than 3.2 wt %, in particular 3.0 wt % or less, preferably 2.6 wt % or less, and is plasticized by an apolar oil and/or petroleum jelly.Type: ApplicationFiled: May 16, 2012Publication date: November 22, 2012Applicant: Lohmann & Rauscher GmbH & Co. KGInventor: MARIUS-THOMAS GORKA
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Patent number: 8304438Abstract: The present invention relates to heteroarylacrylamides of the formula I, in which Het, X, Ra, Rb, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.Type: GrantFiled: June 17, 2009Date of Patent: November 6, 2012Assignee: SanofiInventors: Hartmut Strobel, Paulus Wohlfart, Heinz-Werner Kleemann, Gerhard Zoller, David William Will
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Patent number: 8299253Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: GrantFiled: December 22, 2006Date of Patent: October 30, 2012Assignee: University of Kentucky Research FoundationInventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha P Sumithran
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Publication number: 20120270852Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or C—R3; R3 is hydrogen, methyl, halogen or nitrile; R1 is phenyl or pyridinyl, each of which is optionally substituted by halogen, lower alkyl or lower alkoxy; R2/R2? are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2? together with the N-atom to which they are attached form a morpholine ring, a piperidine ring or an azetidine ring, each of which is unsubstituted or substituted one or more substituents selected from lower alkoxy, halogen, hydroxy and methyl; R4/R4? are each independently hydrogen or lower alkyl, or R4 and R4? together form a C3-5 cycloalkyl-, tetrahydrofuran- or an oxetane-ring; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.Type: ApplicationFiled: April 11, 2012Publication date: October 25, 2012Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Publication number: 20120270873Abstract: The present invention provides adamantyl-diamide derivatives of formula (I): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: ApplicationFiled: May 15, 2012Publication date: October 25, 2012Applicant: H. Lundbeck A/SInventors: Hermogenes N. JIMENEZ, Guiying LI, Dario DOLLER, Michel GRENON, Andrew D. WHITE, Gil MA, Maojun GUO
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Publication number: 20120270885Abstract: The use of a compound of formula I Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; the ring is a 6 membered aromatic ring or is a 5 or 6 membered heteroaromatic ring; Z and Z? are provided that both are not N; R1, R2, R3, R3a, R4, R8 and Ra are specified organic groups and n and p are independently 0, 1, 2, 3 or 4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.Type: ApplicationFiled: February 10, 2012Publication date: October 25, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Peter Maienfisch, Louis-Pierre Molleyres, Jérôme Cassayre, Fredrik Cederbaum, Camilla Corsi, Thomas Pitterna
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Publication number: 20120230978Abstract: The present invention relates to a modulator of glucocorticoid biosynthesis, degradation and/or receptor activation for use in preventing or treating symptoms and/or diseases associated with jet lag. The compositions of the invention may be used as a lead compound for developing a drug for preventing or treating symptoms and/or diseases associated with jet lag. The invention relates to the discovery that administration of the modulator(s) to a subject results in a directional change of the time point of maximum amounts of glucocorticoids in the subject as compared to the time point of maximum amounts of glucocorticoids in a subject not treated with the modulator(s).Type: ApplicationFiled: March 7, 2012Publication date: September 13, 2012Applicant: Max-Planck-Gesellschaft-zur-Forderung der Wissenschaften e.V.Inventors: Gregor Eichele, Henrik Oster, Silke Kiessling
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Publication number: 20120225062Abstract: The present invention provides compounds of Formula I: and related compounds as further described herein, and pharmaceutical compositions comprising these compounds. The invention further provides methods to use these compounds and compositions for treating disorders associated with undesired levels of Pim kinase activity, including cancers and autoimmune disorders.Type: ApplicationFiled: March 2, 2012Publication date: September 6, 2012Inventors: Matthew Burger, Gisele Nishiguchi, Timothy D. Machajewski, Alice Rico, Robert Lowell Simmons, Aaron R. Smith, Victoriano Tamez, JR., Huw Tanner, Lifeng Wan
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Publication number: 20120225782Abstract: Compounds having the following generic formula are disclosed.Type: ApplicationFiled: April 11, 2012Publication date: September 6, 2012Applicant: DOW AGROSCIENCES LLCInventors: Nneka T. Breaux, Michael R. Loso, Timothy C. Johnson, Jonathan M. Babcock, Benjamin M. Nugent, Timothy P. Martin, Annette V. Brown, Ronald Ross, JR., William C. Lo, Matthias S. Ober
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Publication number: 20120225061Abstract: The present invention provides a compound of formula (I): as further described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: March 1, 2012Publication date: September 6, 2012Inventors: Matthew Burger, Yu Ding, Wooseok Han, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Aaron R. Smith, Victoriano Tamez, JR., Huw Tanner, Lifeng Wan
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Patent number: 8258125Abstract: A pharmaceutical composition including therapeutically effective amounts of at least one HMG-CoA reductase inhibitor present as a dyhydroxyacid salt and at least one additional therapeutic agent.Type: GrantFiled: June 20, 2008Date of Patent: September 4, 2012Inventor: Josefino B. Tunac
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Patent number: 8258308Abstract: The present disclosure relates to compounds of formula (I): or a pharmaceutically acceptable salt or N-oxide thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds of formula (I), and to their methods of use in therapy.Type: GrantFiled: December 21, 2007Date of Patent: September 4, 2012Assignee: Laboratorios Almirall, S.A.Inventors: Julio Cesar Castro Palomino Laria, Montserrat Erra Sola, Maria Estrella Lozoya Toribio, Eloisa Navarro Romero
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Publication number: 20120220590Abstract: Compounds of formula (I) and pharmaceutical compositions containing them are described. The use of the compounds and compositions are also described.Type: ApplicationFiled: July 30, 2010Publication date: August 30, 2012Inventors: Pravin S. Thombare, Amitgiri Goswami, Edouard Zamaratski, Tomas Hansson, Thomas Norin
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Publication number: 20120214799Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: April 9, 2012Publication date: August 23, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Juan-Miguel Jimenez, Guy Bemis, Francois Maltais, Tiansheng Wang, Ronald Knegtel, Chris Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Mortimore
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Patent number: 8247401Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: GrantFiled: October 29, 2008Date of Patent: August 21, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher S. Burgey, Diem Nguyen, Zhengwu Deng, Daniel V. Paone, Craig M. Potteiger, Joseph P. Vacca
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Patent number: 8247435Abstract: The present disclosure provides for a scientific formulation useful in the treatment and prevention of human and animal diseases. A biologically effective amount of each of the components of the formulation is administered to patients in pill (or capsule) form via multiple different and identifiable pills. The compounds of the formulation are segregated into different pill types, and contain various amounts of the compounds Curcumin, Genistein, Squalamine, Vitamin E, N-Acetyl-Cysteine, Methylselenocysteine, Zinc Gluconate, B Complex, Lentinen, Coenzyme Q10 Acetyl-L-Carnitine, Lipoic Acid, Resveratrol, and Vitamin C. Furthermore, Arabinoxylan and/or Peperine may be added to the various pill formulations.Type: GrantFiled: February 19, 2009Date of Patent: August 21, 2012Inventor: Jerry T. Thornthwaite
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Publication number: 20120208795Abstract: The present invention is based, in part, on our discovery that certain types of therapeutic agents can be used in combination to treat a variety of neuropsychiatric and related disorders, including addiction (e.g., to a substance or to an activity) as well as to alleviate some of the symptoms experienced during menopause or associated with the menstrual cycle. Regardless of the precise formulation, the compositions of the invention can include at least one active ingredient that targets the hypothalamopituitary-adrenal (HPA) axis and at least one active ingredient that targets the prefrontal cortex. Either or both of these types of agents can be combined with an agent that inhibits activity in the sympathetic nervous system. Thus, the compositions or combination pharmacotherapies can also include an agent that inhibits a beta-adrenergic receptor or that otherwise acts as an anti-hypertensive or anxiolytic agent.Type: ApplicationFiled: January 13, 2012Publication date: August 16, 2012Applicant: Board of Supervisors of Louisiana State University & Agricultural & Mechanical CollegeInventor: Nicholas E. Goeders
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Publication number: 20120196856Abstract: The present invention is directed to aryl aminopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: October 26, 2010Publication date: August 2, 2012Inventors: Michael J. Breslin, Christopher D. Cox, Izzat T. Raheem
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Publication number: 20120190686Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: ApplicationFiled: December 22, 2011Publication date: July 26, 2012Applicant: H. LUNDBECK A/SInventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
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Publication number: 20120178749Abstract: The present invention generally relates to compounds to treat viral infections and methods of their use. In particular, compounds of the present invention inhibit the activity of NS1 protein, thereby mitigating viral infection and, in particular, influenza virus infection. Accordingly, NS1 protein inhibitors and methods of treatment that employ such inhibitors are contemplated by the present invention.Type: ApplicationFiled: February 21, 2012Publication date: July 12, 2012Inventors: Michael Roth, Beatriz Fontoura, Shuguang Wei, Neal Satterly
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Patent number: 8211402Abstract: A compound that recognizes and binds to the CA-IX protein has Formula I, II, III, or IV. The compounds may include a radioactive element for radioimaging or therapeutic applications. Thus, pharmaceutical compositions may be prepared with one or more of the compounds of Formula I, II, III, or IV.Type: GrantFiled: December 4, 2009Date of Patent: July 3, 2012Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, Genliang Lu, Shawn Hillier
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Publication number: 20120165343Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: ApplicationFiled: December 22, 2011Publication date: June 28, 2012Applicant: Pfizer Inc.Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Patent number: 8207346Abstract: Anatabine is obtained by reacting benzophenoneimine with 3-aminomethyl pyridine to form benzylhydrylidene-pyridin-3-yl-methyl-amine. The benzylhydrylidene-pyridin-3-yl-methyl-amine is treated with a non-nucleophilic base and a dielectrophile, such as cis-1,4-dichloro-2-butene, followed by acidification, then basification, to provide anatabine. The resulting anatabine is substantially free from contaminants and displays good stability. In an alternative embodiment, the benzylhydrylidene-pyridin-3-yl-methyl-amine may be used in the synthesis of other alkaloids such as anabasine, nornicotine, N-methylanabasine, and anabaseine.Type: GrantFiled: March 23, 2010Date of Patent: June 26, 2012Assignee: Rock Creek Pharmaceuticals, Inc.Inventors: Tom Thomas Puthiaparampil, Thomas Kanathkunn David, Muppala Sarveswara Raju
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Publication number: 20120157462Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of aniline and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.Type: ApplicationFiled: January 30, 2008Publication date: June 21, 2012Inventors: Alan T. Johnson, Guan-Sheng Jiao