Additional Hetero Ring Patents (Class 514/397)
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Publication number: 20120295897Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: July 25, 2012Publication date: November 22, 2012Applicant: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Sultan Chowdhury, Lauren Fraser, Jianmin Fu, Jonathan Langille, Shifeng Liu, Jianyu Sun, Shaoyi Sun, Serguei Sviridov, Mark Wood, Alla Yurevna Zenova, Qi Jia, Jean-Jacques Cadieux, Simon J. Gauthier, Amy Frances Douglas, Tom Hsieh, Nagasree Chakka, Zoran Cikojevic
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Publication number: 20120289562Abstract: Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release darifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release darifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 9, 2012Publication date: November 15, 2012Applicant: THERAVIDA, INC.Inventors: Mehdi PABORJI, Kenneth L. DUCHIN, Wendy Jade Limayo HERNANDEZ, Roger S. FLUGEL
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Publication number: 20120289567Abstract: Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release darifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release darifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 21, 2012Publication date: November 15, 2012Applicant: THERAVIDA, INC.Inventors: Mehdi PABORJI, Kenneth L. DUCHIN, Wendy Jade Limayo HERNANDEZ, Roger S. FLUGEL
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Publication number: 20120289565Abstract: Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release tolterodine, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release tolterodine, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 21, 2012Publication date: November 15, 2012Applicant: TheraVida, Inc.Inventors: Mehdi PABORJI, Kenneth L. DUCHIN, Wendy Jade Limayo HERNANDEZ, Roger S. FLUGEL
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Publication number: 20120289564Abstract: Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release oxybutynin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release oxybutynin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 9, 2012Publication date: November 15, 2012Applicant: THERAVIDA, INC.Inventors: Mehdi PABORJI, Kenneth L. DUCHIN, Wendy Jade Limayo HERNANDEZ, Roger S. FLUGEL
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Publication number: 20120289560Abstract: Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release tolterodine, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release tolterodine, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 9, 2012Publication date: November 15, 2012Applicant: THERAVIDA, INC.Inventors: Mehdi PABORJI, Kenneth L. DUCHIN, Wendy Jade Limayo HERNANDEZ, Roger S. FLUGEL
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Publication number: 20120289568Abstract: Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release oxybutynin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release oxybutynin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 21, 2012Publication date: November 15, 2012Applicant: THERAVIDA, INC.Inventors: Mehdi PABORJI, Kenneth L. DUCHIN, Wendy Jade Limayo HERNANDEZ, Roger S. FLUGEL
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Publication number: 20120289566Abstract: Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release fesoterodine, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release fesoterodine, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 21, 2012Publication date: November 15, 2012Applicant: THERAVIDA, INC.Inventors: Mehdi PABORJI, Kenneth L. DUCHIN, Roger S. FLUGEL
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Publication number: 20120289561Abstract: Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release fesoterodine, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release fesoterodine, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 9, 2012Publication date: November 15, 2012Applicant: THERAVIDA, INC.Inventors: Mehdi PABORJI, Kenneth L. DUCHIN, Roger S. FLUGEL
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Publication number: 20120289563Abstract: Disclosed are pharmaceutical compositions comprising a therapeutically effective amount of immediate release or orally disintegrating imidafenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of immediate release or orally disintegrating imidafenacin, or pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 9, 2012Publication date: November 15, 2012Applicant: THERAVIDA, INC.Inventors: Mehdi PABORJI, Wendy Jade Limayo HERNANDEZ, Kenneth L. DUCHIN, Roger S. FLUGEL
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Patent number: 8309103Abstract: The present invention refers to a treatment for mixed infectious diseases in the human reproductive system, wherein an association of compounds containing fluconazole and either tinidazole or secnidazole is used, the same being associated in doses lower to those commonly used therapeutically. The combination has proven to be highly efficacious and shown a good degree of tolerance.Type: GrantFiled: January 22, 2004Date of Patent: November 13, 2012Assignee: Alparis, S.A. DE C.V.Inventors: Luisa Hernandez-Ramirez, Angelica Arzola-Paniagua, Raul E. Garcia-Salgado-Lopez, Fernando Poot-Lopez
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Patent number: 8309554Abstract: Hypoxia activated drug compounds having a structure of formula (I) are useful in the treatment of cancer and other hyperproliferative diseases.Type: GrantFiled: May 14, 2009Date of Patent: November 13, 2012Assignee: Threshold PharmaceuticalsInventors: Jason Lewis, Mark Matteucci, Tao Chen, Hailong Jiao
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Publication number: 20120283298Abstract: Methods for administering a therapeutically effective amount of a somatostatin receptor-4 (SSTR4) agonist in order to treat learning and memory impairment for Alzheimer's disease is disclosed.Type: ApplicationFiled: October 14, 2010Publication date: November 8, 2012Inventors: Albert Michael Crider, Kenneth A. Witt, Karin E. Sandoval
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Patent number: 8303944Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: February 13, 2008Date of Patent: November 6, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Publication number: 20120277217Abstract: Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.Type: ApplicationFiled: October 27, 2010Publication date: November 1, 2012Applicant: NewLink Genetics CorporationInventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani, Xiaoxia Zhang
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Publication number: 20120277222Abstract: Novel compounds and methods for activating the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing four six-membered rings and a substituted or unsubstituted C5 or C6 heteroaryl or heterocycloalkyl ring and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods and compounds for the treatment of disorders including neurologic, neuropsychiatric, and metabolic disorders are provided. For example, a method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of the described compounds.Type: ApplicationFiled: May 24, 2012Publication date: November 1, 2012Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
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Publication number: 20120277266Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: July 13, 2012Publication date: November 1, 2012Inventors: Omar D. Lopez, Qi Chen, Makonen Belema, Lawrence G. Hamann
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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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Patent number: 8299079Abstract: This application relates to the use of one or more parasympathomimetic drugs in combination with one or more alpha agonists to create optically beneficial miosis to, for example, temporarily treat presbyopia. The invention provides a pharmaceutical preparation comprising a therapeutically effective amount of one or more parasympathomimetic drugs or cholinesterase inhibitors, or a pharmaceutically acceptable salt thereof, in combination with one or more alpha agonists or antagonists, or a pharmaceutically acceptable salt thereof. The invention further provides for a method for treating, ameliorating or reducing presbyopia of a patient having an eye, comprising administering to said eye a pharmaceutically effective amount of the ophthalmic preparation.Type: GrantFiled: December 20, 2010Date of Patent: October 30, 2012Inventor: Herbert E. Kaufman
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Patent number: 8299102Abstract: The present invention relates to heteroarylcyclopropanecarboxamides of the formula I, in which Het, X, Ra, Rb, Rc, Rd, 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: October 30, 2012Assignee: SanofiInventors: Hartmut Strobel, Paulus Wohlfart, Gerhard Zoller, David William Will
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Publication number: 20120270853Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: July 3, 2012Publication date: October 25, 2012Inventors: Donald J.P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith
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Patent number: 8293723Abstract: Inclusion compounds consisting of certain Angiotensin II AT1 receptors antagonist and cyclodextrins are described. These inclusion compounds are useful in the treatment of hypertension.Type: GrantFiled: December 23, 2010Date of Patent: October 23, 2012Assignee: Universidade Federal de Minas GeraisInventors: Ruben Dario Sinisterra Millan, Robson Augusto Souza Dos Santos, Frederic Jean Georges Frezard, Washington Xavier De Paula
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Publication number: 20120264711Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: June 7, 2012Publication date: October 18, 2012Applicant: GILEAD SCIENCES, INC.Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Michael Graupe, Evan S. Krygowski, Scott E. Lazerwith, Qi Liu, Richard L. Mackman, Hyung-Jung Pyun, Joseph H. Saugier, James D. Trenkle, Winston C. Tse, Randall W. Vivian, Scott D. Schroeder, William J. Watkins, Lianhong Xu
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Publication number: 20120264725Abstract: Substituted metalloporphyrin compounds are described, along with pharmaceutical compositions containing the same, and methods of use thereof in protecting cells from oxidant-induced toxicity and pathological conditions such as inflammatory lung disease, neurodegenerative conditions, radiation injury, cancer, diabetes, cardiac conditions and sickle cell disease. Mn(III) porphyrins bearing oxygen atoms within side chains are particularly described.Type: ApplicationFiled: April 23, 2012Publication date: October 18, 2012Inventors: Ines Batinic-Haberle, Irwin Fridovich, Ivan Spasojevic
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Patent number: 8288403Abstract: The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.Type: GrantFiled: November 4, 2009Date of Patent: October 16, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Karlheinz Baumann, Erwin Goetschi, Synese Jolidon, Anja Limberg, Thomas Luebbers
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Patent number: 8288425Abstract: The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.Type: GrantFiled: January 4, 2005Date of Patent: October 16, 2012Assignee: Aventis Pharmaceuticals Inc.Inventors: Michael L. Edwards, Paul J. Cox, Shelley Amendola, Stephanie D. Deprets, Timothy A. Gillespy, Christopher D. Edlin, Andrew D. Morley, Charles J. Gardner, Brian Pedgrift, Herve Bouchard, Didier Babin, Laurence Gauzy, Alain Le-Brun, Tahir N. Majid, John C. Reader, Lloyd J. Payne, Nawaz M. Khan, Michael Cherry
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Publication number: 20120258963Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: ApplicationFiled: June 20, 2012Publication date: October 11, 2012Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
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Publication number: 20120258992Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: June 19, 2012Publication date: October 11, 2012Applicant: THERAVANCE, INC.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
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Publication number: 20120258078Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.Type: ApplicationFiled: May 28, 2010Publication date: October 11, 2012Applicant: Schering CorporationInventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
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Publication number: 20120251491Abstract: The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.Type: ApplicationFiled: May 12, 2010Publication date: October 4, 2012Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge, Craig A. Coburn
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Publication number: 20120252721Abstract: Provided herein are methods for treating or preventing drug-resistant hepatitis C virus infection in a subject, which comprises administering to the subject a 5,5-fused heteroarylene hepatitis C virus inhibitor compound, for example, of Formula I, IA, or IB.Type: ApplicationFiled: March 29, 2012Publication date: October 4, 2012Applicant: IDENIX PHARMACEUTICALS, INC.Inventors: Cyril B. Dousson, David Dukhan, John P. Billelo, Christophe Claude Parsy, Claire Pierra, Francois-Rene Alexandre, Guillaume Brandt, Daniel Da Costa, Houcine Rahali, Jean-Laurent Paparin, Michel Derock, Thierry Convard, Dominique Surleraux
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Patent number: 8278345Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents hydrogen; halogen; alkenyl; alkynyl; -alkenylaryl; -alkenylheteroaryl; alkyl, which may optionally be substituted by one or more groups selected from halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; -alkylcarbocyclyl; -alkylheterocyclyl; aryl; heteroaryl; heterocyclyl; -alkylaryl; -alkyl(aryl)2, -alkylheteroaryl; -aryl-heteroaryl; -heterocyclyl-aryl; -aryl-aryl; -heteroaryl-aryl; -heteroaryl-heteroaryl, and —C(O)R4; R3 represents halogen; alkyl optionally substituted by one or more groups selected from halogen, hydroxyl, alkoxy, thioalkyl, —C(O)OH and —C(O)O-alkyl; aryl; heteroaryl; —C(O)R5; R4 and R5 independently repreType: GrantFiled: November 8, 2007Date of Patent: October 2, 2012Assignee: Probiodrug AGInventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
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Patent number: 8278307Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: GrantFiled: May 8, 2007Date of Patent: October 2, 2012Assignee: ARIAD Pharmaceuticals, Inc.Inventors: William C. Shakespeare, Wei-Sheng Huang, David C. Dalgarno, Xiaotian Zhu, R. Mathew Thomas, Yihan Wang, Jiwei Qi, Rajeswari Sundaramoorthi, Dong Zou, Chester A. Metcalf, III, Tomi K. Sawyer, Jan Antoinette C. Romero
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Publication number: 20120245210Abstract: The present invention is directed to novel thiophene inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: December 14, 2010Publication date: September 27, 2012Applicant: N30 PHARMACEUTICALS, LLCInventor: Xicheng Sun
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Patent number: 8273341Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: November 8, 2011Date of Patent: September 25, 2012Assignee: Gilead Sciences, Inc.Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Michael Graupe, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Evan S. Krygowski, Scott E. Lazerwith, Qi Liu, Richard Mackman, Hyung-Jun Pyun, Joseph H. Saugier, James D. Trenkle, Winston C. Tse, Randall W. Vivian, Scott D. Schroeder, William J. Watkins, Lianhong Xu
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Publication number: 20120238541Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: September 17, 2010Publication date: September 20, 2012Applicant: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
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Patent number: 8268876Abstract: Provided is a pharmaceutical composition for external use, including: (i) luliconazole represented by the following structural formula (1) and/or a salt thereof; and (ii) ?-hydroxycarboxylic acid and/or a salt thereof.Type: GrantFiled: October 2, 2006Date of Patent: September 18, 2012Assignees: Nihon Nohyaku Co., Ltd., Pola Pharma Inc.Inventors: Toyohiko Miki, Akira Nozawa, Nobuo Kubota, Susumu Tomiyama, Hirokazu Kobayashi
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Publication number: 20120232028Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.Type: ApplicationFiled: May 21, 2012Publication date: September 13, 2012Applicant: Tobira Therapeutics, Inc.Inventors: Mitsuru SHIRAISHI, Masanori BABA, Katsuji AIKAWA, Naoyuki KANZAKI, Masaki SETO, Yuji IIZAWA
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Publication number: 20120232031Abstract: Described herein are injectable formulations for intra-articular or peri-articular administration, wherein the formulation is administered to treat joint pain. An injectable formulation for intra-articular or peri-articular administration disclosed herein comprises a therapeutically-effective amount of a leukotriene synthesis inhibitor compound formulated for intra-articular or peri-articular administration.Type: ApplicationFiled: October 19, 2010Publication date: September 13, 2012Applicant: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Petpiboon Peppi Prasit, Isabelle Marguerite Dearmond
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Publication number: 20120220622Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.Type: ApplicationFiled: November 2, 2010Publication date: August 30, 2012Inventors: Julia Adam, Jonathan Gillespie, Steven Laats, John Kinnaird Ferguson MacLean, Duncan Robert McArthur
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Patent number: 8252829Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein each of Ring A, Ring B, T, R2, R2?, and RA is as defined and described herein and methods for treating subjects or patients with a disease, disorder, or condition.Type: GrantFiled: June 7, 2010Date of Patent: August 28, 2012Assignee: Link Medicine CorporationInventor: Mark E. Duggan
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Patent number: 8252830Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: October 8, 2010Date of Patent: August 28, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Donald J. P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith, II
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Publication number: 20120214770Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.Type: ApplicationFiled: May 1, 2012Publication date: August 23, 2012Applicant: BIONOMICS LIMITEDInventors: JASON HUGH CHAPLIN, GURMIT SINGH GILL, DAMIAN WOJCIECH GROBELNY, BERNARD LUKE FLYNN, GABRIEL KREMMIDIOTIS
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Publication number: 20120213791Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof, and combinations thereof with other anti-cancer agents, for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3.Type: ApplicationFiled: November 4, 2011Publication date: August 23, 2012Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Adrian Liam GILL, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
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Patent number: 8247432Abstract: The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs).Type: GrantFiled: May 19, 2011Date of Patent: August 21, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Henry Joseph Breslin, Hans Louis Jos De Winter, Michael Joseph Kukla
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Publication number: 20120207765Abstract: A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease (for example, arteriosclerosis, myocardial infarction, stenocardia, cerebral infarction, chronic arterial occlusive disease, etc.), metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.Type: ApplicationFiled: March 8, 2012Publication date: August 16, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Masaya Kokubo, Hiroshi Ochiai, Yoshikazu Takaoka, Shiro Shibayama
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Publication number: 20120207769Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: ApplicationFiled: April 26, 2012Publication date: August 16, 2012Applicant: NOVARTIS AGInventors: Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
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Patent number: 8242159Abstract: Disclosed herein are novel 1,3-dihydro-5-isobenzofurancarbonitrile derivatives represented by Formula 1, or pharmaceutically acceptable salts thereof. Also disclosed is a pharmaceutical composition for treating or preventing premature ejaculation including the compound. The 1,3-dihydro-5-isobenzofurancarbonitrile derivatives have a short half-life and inhibit the ejaculation process by selectively inhibiting serotonin reuptake via a serotonin reuptake transporter present in a presynaptic neuron. Thus, the compounds are useful in the treatment and prevention of premature ejaculation.Type: GrantFiled: October 31, 2008Date of Patent: August 14, 2012Assignee: Dong-A Pharmaceutical. Co., LtdInventors: Yeong Geon Lee, Soo-Jung Choi, Tae-Kyung Kang, Mi-Jeong Seo, Chang-Yong Shin, Kyung-Seok Lee, Gook-Jun Ahn, Seul-Min Choi, Yong-Duck Kim, Dong-Hwan Kim, Kyung-Koo Kang, Hyun-Joo Shim, Dong-Sung Kim, Byoung-Ok Ahn, Moo-Hi Yoo
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Publication number: 20120201894Abstract: Disclosed herein are pharmaceutical compositions comprising a plurality of first beads each comprising: a core; a first layer comprising pilocarpine or a pharmaceutically acceptable salt thereof; and a second layer comprising a first polymer. Also disclosed are pharmaceutical compositions comprising a plurality of second beads each comprising: a core; and a first layer comprising tolterodine or a pharmaceutically acceptable salt thereof. Further disclosed are pharmaceutical formulations comprising: a) a plurality of the first beads; b) a plurality of the second beads; or c) a plurality of the first beads and a plurality of the second beads.Type: ApplicationFiled: April 17, 2012Publication date: August 9, 2012Applicant: THERAVIDA, INC.Inventors: Mehdi PABORJI, Robert V. TUOHY, III, Peter R.P. FREED, Roger S. FLUGEL
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Publication number: 20120202866Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvents have now been developed which provide ondansetron for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, ondansetron, and optional flavoring agent; formulation II: aqueous polar solvent, ondansetron, optionally flavoring agent, and propellant; formulation III: non-polar solvent, ondansetron, and optional flavoring agent; formulation IV: non-polar solvent, ondansetron, optional flavoring agent, and propellant; formulation V: a mixture of a polar solvent and a non-polar solvent, ondansetron, and optional flavoring agent; formulation VI: a mixture of a polar solvent and a non-polar solvent, ondansetron, optional flavoring agent, and propellant.Type: ApplicationFiled: April 19, 2012Publication date: August 9, 2012Inventors: Harry A. Dugger, III, Mohammed Abd El-Shafy