Patents Issued in January 28, 2014
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Patent number: 8637493Abstract: Described are methods for treating cancers, e.g., glioblastoma, including administering an inhibitor of Notch signalling, e.g., a gamma secretase inhibitor, in combination with a chemotherapeutic agent.Type: GrantFiled: November 10, 2010Date of Patent: January 28, 2014Assignee: University of MassachusettsInventors: Alonzo H. Ross, Candace Gilbert, Richard Moser
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Patent number: 8637494Abstract: Method and compositions for reducing the inflammation after cytokine exposure of an islet cell transplant without affecting the viability and potency are disclosed herein. The present invention describes a composition comprising Withaferin A (WA), a steroidal lactone derived from Withania somnifera to effectively block NF-kB activation in beta cells, minimize cytokine-induced cell death and improve survival of transplanted islets. The method of the present invention involves identifying a subject having islet cells in need of treatment; and providing a effective amount of a Withaferin A composition disposed in a pharmaceutically acceptable carrier in an amount sufficient to reduce the inflammation after cytokine exposure without affecting the viability and potency of the islet cell population.Type: GrantFiled: June 14, 2011Date of Patent: January 28, 2014Assignee: Baylor Research InstituteInventors: Bashoo Naziruddin, Han Peng, Shinichi Matsumoto, Marlon F. Levy
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Patent number: 8637495Abstract: Dietary formulations and methods for treating, preventing or delay onset of osteoarthritis in canines and other animals are disclosed. The formulations are enriched in n-3 fatty acids and limited in n-6 fatty acids.Type: GrantFiled: July 1, 2005Date of Patent: January 28, 2014Assignee: Nestec S.A.Inventors: Mark K. Waldron, Steven S. Hannah
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Patent number: 8637496Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.Type: GrantFiled: June 2, 2008Date of Patent: January 28, 2014Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche ScientifiqueInventors: Anne-Laure Bonneau, Cyrille Botte, Michael Deligny, Nadia Saidani, Hélène Hardre, Bernard Rousseau, Roman Lopez, Eric Marechal
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Patent number: 8637497Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.Type: GrantFiled: July 18, 2011Date of Patent: January 28, 2014Assignee: Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian Metcalf
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Patent number: 8637498Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (Ia) and Formula (Ib) as follows: wherein Y, Z, and n are defined herein; and wherein Yb and Zb are as defined herein.Type: GrantFiled: September 27, 2011Date of Patent: January 28, 2014Assignee: Janssen Pharmaceutica, NVInventors: Peter J. Connolly, Mark J. Macielag, Mark E. McDonnell, Bin Zhu
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Patent number: 8637499Abstract: The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals. This invention also provides methods of making the compound methods of using such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: May 25, 2010Date of Patent: January 28, 2014Assignee: Exelixis, Inc.Inventors: Naing Aay, Arlyn Arcalas, Joerg Bussenius, Steven Charles DeFina, Larisa Dubenko, Jason R. Harris, Eileen E. Jackson-Ugueto, Angie Inyoung Kim, Jean-Claire Limun Manalo, Michael Pack, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang, Owen Joseph Bowles, Jeffry Kimo Curtis
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Patent number: 8637500Abstract: Pyridine and pyrimidine compounds: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, R6, R7, X1, X2, X3, X4, X5, X6, X7, X8, and Y are as defined in the specification; or a pharmaceutically acceptable salt thereof, wherein ring A, m, n, y, R2, R3, R4, R5, R6, R7, R8, R9, X1, X2, and ring A are as defined in the specification; and or a pharmaceutically acceptable salt thereof, wherein m, n, y, R2, R3, R4, R5, R6, R7, R9, X1, X2, and ring A are as defined in the specification; compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: December 16, 2009Date of Patent: January 28, 2014Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Ning Chen, James R. Falsey, Michael J. Frohn, Paul E. Harrington, Essa Hu Harrington, Matthew R. Kaller, Roxanne K. Kunz, Thomas T. Nguyen, Alexander J. Pickrell, Andreas Reichelt, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Aaron C. Siegmund, Guomin Yao
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Patent number: 8637501Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.Type: GrantFiled: July 1, 2010Date of Patent: January 28, 2014Assignee: Albany Molecular Research, Inc.Inventors: Peter R. Guzzo, Matthew David Surman, James Francis Grabowski, Jr., Emily Elizabeth Freeman
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Patent number: 8637502Abstract: The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound.Type: GrantFiled: January 12, 2012Date of Patent: January 28, 2014Assignees: Purde Pharma L.P., Shionogi & Co., Ltd.Inventors: Kevin C. Brown, R. Richard Goehring
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Patent number: 8637503Abstract: Disclosed is the unexpected finding that enantiomers of phenothiazines, preferably the (+) enantiomer of promethazine, are particularly effective in inhibiting the bone resorbing cells, osteoclasts, thus providing new uses and methods for reducing bone loss and, e.g., treating periodontitis and osteoporosis. The invention provides a range of such uses, methods, medicaments and associated compositions and kits.Type: GrantFiled: May 17, 2004Date of Patent: January 28, 2014Assignees: Board of Regents, The University of Texas System, Southwest Research InstituteInventors: Edward J. Boland, Joe McDonough
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Patent number: 8637504Abstract: The following compound is provided as an agent for treating a disease induced by production, secretion and/or deposition of amyloid ? protein, for example, a compound represented by the formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group, R1 is optionally substituted lower alkyl or the like, R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or the like, R3a and R3c are each independently hydrogen, halogen, hydroxy, optionally substituted lower alkyl or the like, or a pharmaceutically acceptable salt thereof, or a solvate thereof.Type: GrantFiled: June 11, 2009Date of Patent: January 28, 2014Assignee: Shionogi & Co., Ltd.Inventors: Akihiro Hori, Terukazu Kato
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Patent number: 8637505Abstract: This invention relates to novel compounds of the Formula Formulas (I), (Ia1-20), (Ib1-20), (Ic1-20), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.Type: GrantFiled: February 3, 2010Date of Patent: January 28, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Frank Himmelsbach
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Patent number: 8637506Abstract: The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm.Type: GrantFiled: May 19, 2004Date of Patent: January 28, 2014Assignees: Enzo Biochem, Inc., University of Connecticut, St. Jude's Childrens HospitalInventors: Dianqing Wu, Yazhou Zhang, Peng Liu, Xiaofeng Li, Jie Zhang, Jufang Shan, Dean Engelhardt
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Patent number: 8637507Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below: formula (I).Type: GrantFiled: March 16, 2010Date of Patent: January 28, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Gang Zhou, Grant Wishart, Pauline C. Ting, Robert G. Aslanian, Nicolas Zorn, David Won-shik Kim
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Patent number: 8637508Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.Type: GrantFiled: January 11, 2012Date of Patent: January 28, 2014Assignee: Novartis AGInventors: Sangamesh Badiger, Murali Chebrolu, Konstanze Hurth, Sébastien Jacquier, Rainer Martin Lueoend, Rainer Machauer, Heinrich Rueeger, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
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Patent number: 8637509Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: GrantFiled: May 5, 2011Date of Patent: January 28, 2014Assignee: GlaxoSmithKline LLCInventors: Joelle Lorraine Burgess, Neil Johnson, Steven D. Knight, Louis LaFrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma, Dominic Suarez
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Patent number: 8637510Abstract: The present invention relates to morpholinothiazole derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulators having the capability to increase the efficacy of nicotinic receptor agonists.Type: GrantFiled: November 25, 2010Date of Patent: January 28, 2014Assignee: Janssen Pharmaceutica NVInventors: Gregor James Macdonald, Benoit Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
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Patent number: 8637511Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: GrantFiled: June 8, 2010Date of Patent: January 28, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Michael Mortimore, Chris Davis, Dean Boyall, Simon Everitt, Daniel Robinson, Sham Ramaya, Damien Fraysse, John Studley, Andrew Miller, Michael O'Donnell, Alistair Rutherford, Joanne Pinder
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Patent number: 8637512Abstract: A sustained release formulation of lamotrigine or a pharmaceutically acceptable derivative thereof and methods of treatment and uses thereof.Type: GrantFiled: December 2, 2003Date of Patent: January 28, 2014Assignee: Glaxo Group LimitedInventors: Ian Richard Buxton, Wlodzimierz Karolak, Mehran Maleki, Vijay Mohan Iyer
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Patent number: 8637513Abstract: The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.Type: GrantFiled: October 23, 2008Date of Patent: January 28, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: James C. Barrow, Paul J. Coleman, Thomas S. Reger, Kelly-Ann S. Schlegel, Youheng Shu, Zhi-Qiang Yang
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Patent number: 8637514Abstract: A polymorph of brimonidine pamoate having the formula exhibits characteristics disclosed herein. The polymorph is included in a composition, device, or implant for use in the treatment or control of elevated intraocular pressure or in the neuroprotection of components of a neurological tissue to prevent progressive degeneration of such components. In particular, such a composition, device, or implant can be used to provide neuroprotection to cells and components of the optic nerve system.Type: GrantFiled: March 14, 2013Date of Patent: January 28, 2014Assignee: Bausch & Lomb IncorporatedInventors: Hongna Wang, Stephen R. Davio, Gregory L. McIntire, Michael Hall, Shazad Suchit, Jon Summersett, Brent Whitehead
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Patent number: 8637515Abstract: A polymorph of brimonidine pamoate having the formula exhibits characteristics disclosed herein. The polymorph is included in a composition, device, or implant for use in the treatment or control of elevated intraocular pressure or in the neuroprotection of components of a neurological tissue to prevent progressive degeneration of such components. In particular, such a composition, device, or implant can be used to provide neuroprotection to cells and components of the optic nerve system.Type: GrantFiled: March 14, 2013Date of Patent: January 28, 2014Assignee: Bausch & Lomb IncorporatedInventors: Hongna Wang, Stephen R. Davio, Gregory L. McIntire, Michael Hall, Shazad Suchit, Jon Summersett, Brent Whitehead
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Patent number: 8637516Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TRK kinase activity.Type: GrantFiled: September 8, 2011Date of Patent: January 28, 2014Assignee: IRM LLCInventors: Yi Fan, Jon Loren, Valentina Molteni, Pamela A. Albaugh, Gregory Chopiuk, Jeffrey M. Smith, Brenton T. Flatt
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Patent number: 8637517Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.Type: GrantFiled: October 4, 2011Date of Patent: January 28, 2014Assignee: Novartis AGInventors: Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Beatrix Wagner
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Patent number: 8637518Abstract: Compounds of the formula (I), in which Y, R1, R2, R3 and R3? have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: November 24, 2009Date of Patent: January 28, 2014Assignee: MERCK PATENT GmbHInventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Patent number: 8637519Abstract: Dihydrothienopyrimidinesulphoxides of formula 1 wherein X is SO or SO2, R1 is H or C1-6-alkyl, R2 is H or an organic group as disclosed herein, and R3 is an optionally substituted, mono- or bicyclic, unsaturated, partially saturated or saturated heterocycle or an optionally substituted, mono- or bicyclic heteroaryl, and the pharmacologically acceptable salts thereof, as well as pharmaceutical compositions which contain these compounds. These dihydrothienopyrimidinesulphoxides are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system, or cancers.Type: GrantFiled: October 16, 2008Date of Patent: January 28, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Pascale Pouzet, Ralf Anderskewitz, Horst Dollinger, Dennis Fiegen, Thomas Fox, Rolf Goeggel, Christoph Hoenke, Domnic Martyres, Peter Nickolaus, Klaus Klinder
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Patent number: 8637520Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.Type: GrantFiled: July 1, 2010Date of Patent: January 28, 2014Assignee: Janssen Pharmaceutica NVInventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
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Patent number: 8637521Abstract: The present invention discloses multifunctional bioactive compounds of formula (I) constituted of an immunoregulatory portion linked to a stabilizer moiety and pharmaceutical compositions thereof useful in the treatment of immune disorders and hemopoietic disorders such as immune cytopema, multiple myeloma, chronic lymphoid leucosis, lymphocytic lymphomas, lymphosarcomas.Type: GrantFiled: August 1, 2007Date of Patent: January 28, 2014Assignee: Manus Pharmaceuticals (Canada) Ltd.Inventor: Vladislav I. Deigin
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Patent number: 8637522Abstract: The present invention relates to pyrazinone derivatives of formula (I), wherein n, R1, R2, R3 and R4 are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.Type: GrantFiled: January 15, 2009Date of Patent: January 28, 2014Assignee: Merck Patent GmbHInventors: Gérard Botton, Micheline Kergoat, Christine Charon, Samer Elbawab
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Patent number: 8637523Abstract: Compounds of the formula (I) are provided, including pharmaceutically acceptable salts thereof: which modulate ?-amyloid peptide (?-AP) production, and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: GrantFiled: July 12, 2011Date of Patent: January 28, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Lorin A. Thompson, III, Yong-Jin Wu, Yunhui Zhang
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Patent number: 8637524Abstract: The present invention relates to new pyrimidinone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereofType: GrantFiled: July 21, 2010Date of Patent: January 28, 2014Assignee: Auspex Pharmaceuticals, IncInventors: Tadimeti Rao, Chengzhi Zhang
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Patent number: 8637525Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: GrantFiled: January 25, 2011Date of Patent: January 28, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Richard E. Olson, Jianliang Shi, Lorin A. Thompson, III, Yong-Jin Wu, Li Xu, Yunhui Zhang, Dmitry S. Zuev
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Patent number: 8637526Abstract: The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.Type: GrantFiled: May 2, 2011Date of Patent: January 28, 2014Assignee: Genentech, Inc.Inventors: Jeffrey Blaney, Paul A. Gibbons, Emily Hanan, Joseph P. Lyssikatos, Steven R. Magnuson, Richard Pastor, Thomas E. Rawson, Aihe Zhou, Bing-Yan Zhu
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Patent number: 8637527Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: GrantFiled: September 12, 2012Date of Patent: January 28, 2014Assignee: Janssen Pharmaceutica NVInventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C Rech, Wei Xiao
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Patent number: 8637528Abstract: A method of treating a movement abnormality associated with the pathology of a neurological movement disorder, such as Parkinson's disease or Restless Leg(s) Syndrome by administering a therapeutically effective amount of a PDE7 inhibitory agent. An aspect of the invention provides for the administration of a PDE& inhibitory agent in conjunction with a dopamine agonist or precursor, such as levodopa. In another aspect of the invention, the PDE7 inhibitory agent may be selective for PDE7 relative to other molecular targets (i) known to be involved with the pathology of Parkinson's disease or (ii) at which other drug(s) that are therapeutically effective to treat Parkinson's disease act.Type: GrantFiled: May 4, 2009Date of Patent: January 28, 2014Assignee: Omeros CorporationInventors: John E Bergmann, Neil S Cutshall, Gregory A Demopulos, Vincent A Florio, George Gaitanaris, Patrick Gray, John Hohmann, Rene Onrust, Hongkui Zeng
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Patent number: 8637529Abstract: The present disclosure is directed to novel compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variables are as defined herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, Crohn's disease, psoriasis and asthma.Type: GrantFiled: June 10, 2011Date of Patent: January 28, 2014Assignee: AbbYie Inc.Inventors: Kevin R. Woller, Michael L. Curtin, Kristine E. Frank, Nathan S. Josephsohn, Biqin C. Li, Neil Wishart
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Patent number: 8637530Abstract: The invention relates to 8-[3-amino-piperidin-1-yl]-xanthines and the physiologically acceptable salts thereof, particularly the hydrochlorides thereof.Type: GrantFiled: January 9, 2012Date of Patent: January 28, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Waldemar Pfrengle, Peter Sieger
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Patent number: 8637531Abstract: This invention provides pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (I), wherein: R1 is amino, R4 is hydrogen, and R2 and R3 together provide a specific substitution pattern, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro-drugs thereof, are useful in the treatment of hepatitis C.Type: GrantFiled: December 24, 2007Date of Patent: January 28, 2014Assignee: Gilead Sciences, Inc.Inventors: Steven S. Bondy, William J. Watkins, Lee S. Chong, Piet Andre Maurits Maria Herdewijn, Steven Cesar Alfons De Jonghe
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Patent number: 8637532Abstract: The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: GrantFiled: February 4, 2010Date of Patent: January 28, 2014Assignee: Merck Patent GmbHInventors: Amanda E. Sutton, Ruoxi Lan, Thomas E. Richardson, David Perrey, Harold George Vandeveer, Bayard R. Huck, Srinivasa R. Karra, Xiaoling Chen, Yufang Xiao, Lesley Liu-Bujalski, Andreas Goutopoulos, Frank Stieber, Brian L. Hodous, Hui Qiu, Reinaldo Jones, Brian H. Heasley
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Patent number: 8637533Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.Type: GrantFiled: February 17, 2012Date of Patent: January 28, 2014Assignee: ICOS CorporationInventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
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Patent number: 8637534Abstract: The novel active compound combinations comprising 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro-[1,2,4]-triazole-3-thione of the formula and the active compound of groups (1) to (24) listed in the description have very good fungicidal properties.Type: GrantFiled: June 10, 2009Date of Patent: January 28, 2014Assignee: Bayer Intellectual Property GmbHInventors: Stefan Dutzmann, Klaus Stenzel, Manfred Jautelat
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Patent number: 8637535Abstract: Solid phases of (?)-cis-FTC, which are designated herein as amorphous (?)-FTC and Forms II and III (?)-cis-FTC) are provided that can be distinguished from Form I (?)-cis-FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. A hydrated crystalline form of (±)-cis-FTC (i.e. racemic cis-FTC), and a dehydrated form of the hydrate, are also provided, and can similarly be distinguished from other forms of FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These FTC forms can be used in the manufacture of other forms of FTC, or in pharmaceutical compositions. Particularly preferred uses of these forms are in the treatment of HIV or hepatitis B.Type: GrantFiled: June 9, 2009Date of Patent: January 28, 2014Assignees: Gilead Sciences, Inc., Abbvie, Inc.Inventors: Yuerong Hu, Kenneth R. Phares, Devalina Law
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Patent number: 8637536Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.Type: GrantFiled: December 5, 2011Date of Patent: January 28, 2014Assignee: Glaxo Group LimitedInventors: Yun Jin, Zehong Wan, Qing Zhang
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Patent number: 8637537Abstract: Compounds having the formula I wherein A, Z, R1a, R1b, R2, R3, R4, R5, R6, R7, R9, R10, Ra, Rb and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.Type: GrantFiled: August 24, 2012Date of Patent: January 28, 2014Assignee: Genentech, Inc.Inventors: Ignacio Aliagas-Martin, James Crawford, Wendy Lee, Simon Mathieu, Joachim Rudolph
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Patent number: 8637538Abstract: The present invention relates to methods for treating uremic pruritus with anti-pruritic compositions.Type: GrantFiled: December 14, 2012Date of Patent: January 28, 2014Assignee: Trevi Therapeutics, Inc.Inventor: Thomas Sciascia
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Patent number: 8637539Abstract: The present invention relates to a therapeutic agent for neuropathic pain containing, as an active ingredient, a compound represented by general formula (I) or a pharmacologically acceptable acid addition salt thereof: (wherein R1, R2, R3, R4, R5, R6, R7, R8, A, and B have the same definitions as those described in the specification), and an animal model produced by administering (+)-4a-(3-hydroxyphenyl)-2-methyl-1,2,3,4,4a,5,12,12a-octohydro-trans-quinolino[2,3-g]isoquinoline. The present invention makes it possible to perform drug treatment for neuropathic pain. The therapeutic effect of a compound against neuropathic pain can also be evaluated.Type: GrantFiled: August 18, 2005Date of Patent: January 28, 2014Assignee: Toray Industries, Inc.Inventors: Hiroshi Nagase, Takashi Endo, Kuniaki Kawamura, Toshiaki Tanaka, Tomohiko Suzuki, Tsutomu Suzuki, Yasushi Kuraishi, Kimiyasu Shiraki
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Patent number: 8637540Abstract: This invention relates to an abuse deterrent dosage form of opioid analgesics, wherein an analgesically effective amount of opioid analgesic is combined with a polymer to form a matrix.Type: GrantFiled: June 25, 2013Date of Patent: January 28, 2014Assignee: Acura PharmaceuticalsInventors: Vijai Kumar, David Dixon, Divya Tewari, Dilip B. Wadgaonkar
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Patent number: 8637541Abstract: The compound (+) {7R-[[(4-fluorophenyl)sulfonyl] (methyl)ammo]-6,7,8,9-tetrahydropyrido[1,2-a]mdol-10-yl}acetic acid and pharmaceutically acceptable salts thereof are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-meidated diseases such as asthma.Type: GrantFiled: September 17, 2009Date of Patent: January 28, 2014Assignee: Merck Canada Inc.Inventor: Zhaoyin Wang
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Patent number: 8637542Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating lipid kinases such PB kinases, tryosine kinases and protein kinases such as mTOR. Also provided in the present invention are methods of using these compositions to modulate these kinases especially for therapeutic applications.Type: GrantFiled: March 16, 2009Date of Patent: January 28, 2014Assignee: Intellikine, Inc.Inventors: Yi Liu, Pingda Ren, Liansheng Li, Katrina Chan, Troy Edward Wilson