Patents Issued in January 28, 2014
  • Patent number: 8637493
    Abstract: 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: Grant
    Filed: November 10, 2010
    Date of Patent: January 28, 2014
    Assignee: University of Massachusetts
    Inventors: Alonzo H. Ross, Candace Gilbert, Richard Moser
  • Patent number: 8637494
    Abstract: 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: Grant
    Filed: June 14, 2011
    Date of Patent: January 28, 2014
    Assignee: Baylor Research Institute
    Inventors: Bashoo Naziruddin, Han Peng, Shinichi Matsumoto, Marlon F. Levy
  • Patent number: 8637495
    Abstract: 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: Grant
    Filed: July 1, 2005
    Date of Patent: January 28, 2014
    Assignee: Nestec S.A.
    Inventors: Mark K. Waldron, Steven S. Hannah
  • Patent number: 8637496
    Abstract: 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: Grant
    Filed: June 2, 2008
    Date of Patent: January 28, 2014
    Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche Scientifique
    Inventors: Anne-Laure Bonneau, Cyrille Botte, Michael Deligny, Nadia Saidani, Hélène Hardre, Bernard Rousseau, Roman Lopez, Eric Marechal
  • Patent number: 8637497
    Abstract: 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: Grant
    Filed: July 18, 2011
    Date of Patent: January 28, 2014
    Assignee: Incyte Corporation
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian Metcalf
  • Patent number: 8637498
    Abstract: 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: Grant
    Filed: September 27, 2011
    Date of Patent: January 28, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Peter J. Connolly, Mark J. Macielag, Mark E. McDonnell, Bin Zhu
  • Patent number: 8637499
    Abstract: 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: Grant
    Filed: May 25, 2010
    Date of Patent: January 28, 2014
    Assignee: 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
  • Patent number: 8637500
    Abstract: 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: Grant
    Filed: December 16, 2009
    Date of Patent: January 28, 2014
    Assignee: 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
  • Patent number: 8637501
    Abstract: 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: Grant
    Filed: July 1, 2010
    Date of Patent: January 28, 2014
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter R. Guzzo, Matthew David Surman, James Francis Grabowski, Jr., Emily Elizabeth Freeman
  • Patent number: 8637502
    Abstract: 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: Grant
    Filed: January 12, 2012
    Date of Patent: January 28, 2014
    Assignees: Purde Pharma L.P., Shionogi & Co., Ltd.
    Inventors: Kevin C. Brown, R. Richard Goehring
  • Patent number: 8637503
    Abstract: 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: Grant
    Filed: May 17, 2004
    Date of Patent: January 28, 2014
    Assignees: Board of Regents, The University of Texas System, Southwest Research Institute
    Inventors: Edward J. Boland, Joe McDonough
  • Patent number: 8637504
    Abstract: 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: Grant
    Filed: June 11, 2009
    Date of Patent: January 28, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Akihiro Hori, Terukazu Kato
  • Patent number: 8637505
    Abstract: 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: Grant
    Filed: February 3, 2010
    Date of Patent: January 28, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Frank Himmelsbach
  • Patent number: 8637506
    Abstract: 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: Grant
    Filed: May 19, 2004
    Date of Patent: January 28, 2014
    Assignees: Enzo Biochem, Inc., University of Connecticut, St. Jude's Childrens Hospital
    Inventors: Dianqing Wu, Yazhou Zhang, Peng Liu, Xiaofeng Li, Jie Zhang, Jufang Shan, Dean Engelhardt
  • Patent number: 8637507
    Abstract: 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: Grant
    Filed: March 16, 2010
    Date of Patent: January 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gang Zhou, Grant Wishart, Pauline C. Ting, Robert G. Aslanian, Nicolas Zorn, David Won-shik Kim
  • Patent number: 8637508
    Abstract: 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: Grant
    Filed: January 11, 2012
    Date of Patent: January 28, 2014
    Assignee: Novartis AG
    Inventors: Sangamesh Badiger, Murali Chebrolu, Konstanze Hurth, Sébastien Jacquier, Rainer Martin Lueoend, Rainer Machauer, Heinrich Rueeger, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
  • Patent number: 8637509
    Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Grant
    Filed: May 5, 2011
    Date of Patent: January 28, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: 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
  • Patent number: 8637510
    Abstract: 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: Grant
    Filed: November 25, 2010
    Date of Patent: January 28, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gregor James Macdonald, Benoit Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
  • Patent number: 8637511
    Abstract: 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: Grant
    Filed: June 8, 2010
    Date of Patent: January 28, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: 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
  • Patent number: 8637512
    Abstract: A sustained release formulation of lamotrigine or a pharmaceutically acceptable derivative thereof and methods of treatment and uses thereof.
    Type: Grant
    Filed: December 2, 2003
    Date of Patent: January 28, 2014
    Assignee: Glaxo Group Limited
    Inventors: Ian Richard Buxton, Wlodzimierz Karolak, Mehran Maleki, Vijay Mohan Iyer
  • Patent number: 8637513
    Abstract: 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: Grant
    Filed: October 23, 2008
    Date of Patent: January 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Paul J. Coleman, Thomas S. Reger, Kelly-Ann S. Schlegel, Youheng Shu, Zhi-Qiang Yang
  • Patent number: 8637514
    Abstract: 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: Grant
    Filed: March 14, 2013
    Date of Patent: January 28, 2014
    Assignee: Bausch & Lomb Incorporated
    Inventors: Hongna Wang, Stephen R. Davio, Gregory L. McIntire, Michael Hall, Shazad Suchit, Jon Summersett, Brent Whitehead
  • Patent number: 8637515
    Abstract: 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: Grant
    Filed: March 14, 2013
    Date of Patent: January 28, 2014
    Assignee: Bausch & Lomb Incorporated
    Inventors: Hongna Wang, Stephen R. Davio, Gregory L. McIntire, Michael Hall, Shazad Suchit, Jon Summersett, Brent Whitehead
  • Patent number: 8637516
    Abstract: 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: Grant
    Filed: September 8, 2011
    Date of Patent: January 28, 2014
    Assignee: IRM LLC
    Inventors: Yi Fan, Jon Loren, Valentina Molteni, Pamela A. Albaugh, Gregory Chopiuk, Jeffrey M. Smith, Brenton T. Flatt
  • Patent number: 8637517
    Abstract: 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: Grant
    Filed: October 4, 2011
    Date of Patent: January 28, 2014
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Beatrix Wagner
  • Patent number: 8637518
    Abstract: 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: Grant
    Filed: November 24, 2009
    Date of Patent: January 28, 2014
    Assignee: MERCK PATENT GmbH
    Inventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
  • Patent number: 8637519
    Abstract: 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: Grant
    Filed: October 16, 2008
    Date of Patent: January 28, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pascale Pouzet, Ralf Anderskewitz, Horst Dollinger, Dennis Fiegen, Thomas Fox, Rolf Goeggel, Christoph Hoenke, Domnic Martyres, Peter Nickolaus, Klaus Klinder
  • Patent number: 8637520
    Abstract: Certain substituted pyridyl amide compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: January 28, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: John M. Keith, Michael A. Letavic, Kiev S. Ly, Neelakandha S. Mani, John E. Mills, Chennagiri R. Pandit, Frank J. Villani, Hua Zhong
  • Patent number: 8637521
    Abstract: 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: Grant
    Filed: August 1, 2007
    Date of Patent: January 28, 2014
    Assignee: Manus Pharmaceuticals (Canada) Ltd.
    Inventor: Vladislav I. Deigin
  • Patent number: 8637522
    Abstract: 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: Grant
    Filed: January 15, 2009
    Date of Patent: January 28, 2014
    Assignee: Merck Patent GmbH
    Inventors: Gérard Botton, Micheline Kergoat, Christine Charon, Samer Elbawab
  • Patent number: 8637523
    Abstract: 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: Grant
    Filed: July 12, 2011
    Date of Patent: January 28, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Lorin A. Thompson, III, Yong-Jin Wu, Yunhui Zhang
  • Patent number: 8637524
    Abstract: The present invention relates to new pyrimidinone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereof
    Type: Grant
    Filed: July 21, 2010
    Date of Patent: January 28, 2014
    Assignee: Auspex Pharmaceuticals, Inc
    Inventors: Tadimeti Rao, Chengzhi Zhang
  • Patent number: 8637525
    Abstract: 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: Grant
    Filed: January 25, 2011
    Date of Patent: January 28, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: 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
  • Patent number: 8637526
    Abstract: 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: Grant
    Filed: May 2, 2011
    Date of Patent: January 28, 2014
    Assignee: 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
  • Patent number: 8637527
    Abstract: 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: Grant
    Filed: September 12, 2012
    Date of Patent: January 28, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C Rech, Wei Xiao
  • Patent number: 8637528
    Abstract: 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: Grant
    Filed: May 4, 2009
    Date of Patent: January 28, 2014
    Assignee: Omeros Corporation
    Inventors: John E Bergmann, Neil S Cutshall, Gregory A Demopulos, Vincent A Florio, George Gaitanaris, Patrick Gray, John Hohmann, Rene Onrust, Hongkui Zeng
  • Patent number: 8637529
    Abstract: 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: Grant
    Filed: June 10, 2011
    Date of Patent: January 28, 2014
    Assignee: AbbYie Inc.
    Inventors: Kevin R. Woller, Michael L. Curtin, Kristine E. Frank, Nathan S. Josephsohn, Biqin C. Li, Neil Wishart
  • Patent number: 8637530
    Abstract: The invention relates to 8-[3-amino-piperidin-1-yl]-xanthines and the physiologically acceptable salts thereof, particularly the hydrochlorides thereof.
    Type: Grant
    Filed: January 9, 2012
    Date of Patent: January 28, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Peter Sieger
  • Patent number: 8637531
    Abstract: 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: Grant
    Filed: December 24, 2007
    Date of Patent: January 28, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Steven S. Bondy, William J. Watkins, Lee S. Chong, Piet Andre Maurits Maria Herdewijn, Steven Cesar Alfons De Jonghe
  • Patent number: 8637532
    Abstract: 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: Grant
    Filed: February 4, 2010
    Date of Patent: January 28, 2014
    Assignee: Merck Patent GmbH
    Inventors: 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
  • Patent number: 8637533
    Abstract: 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: Grant
    Filed: February 17, 2012
    Date of Patent: January 28, 2014
    Assignee: ICOS Corporation
    Inventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • Patent number: 8637534
    Abstract: 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: Grant
    Filed: June 10, 2009
    Date of Patent: January 28, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Stefan Dutzmann, Klaus Stenzel, Manfred Jautelat
  • Patent number: 8637535
    Abstract: 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: Grant
    Filed: June 9, 2009
    Date of Patent: January 28, 2014
    Assignees: Gilead Sciences, Inc., Abbvie, Inc.
    Inventors: Yuerong Hu, Kenneth R. Phares, Devalina Law
  • Patent number: 8637536
    Abstract: 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: Grant
    Filed: December 5, 2011
    Date of Patent: January 28, 2014
    Assignee: Glaxo Group Limited
    Inventors: Yun Jin, Zehong Wan, Qing Zhang
  • Patent number: 8637537
    Abstract: 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: Grant
    Filed: August 24, 2012
    Date of Patent: January 28, 2014
    Assignee: Genentech, Inc.
    Inventors: Ignacio Aliagas-Martin, James Crawford, Wendy Lee, Simon Mathieu, Joachim Rudolph
  • Patent number: 8637538
    Abstract: The present invention relates to methods for treating uremic pruritus with anti-pruritic compositions.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: January 28, 2014
    Assignee: Trevi Therapeutics, Inc.
    Inventor: Thomas Sciascia
  • Patent number: 8637539
    Abstract: 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: Grant
    Filed: August 18, 2005
    Date of Patent: January 28, 2014
    Assignee: Toray Industries, Inc.
    Inventors: Hiroshi Nagase, Takashi Endo, Kuniaki Kawamura, Toshiaki Tanaka, Tomohiko Suzuki, Tsutomu Suzuki, Yasushi Kuraishi, Kimiyasu Shiraki
  • Patent number: 8637540
    Abstract: 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: Grant
    Filed: June 25, 2013
    Date of Patent: January 28, 2014
    Assignee: Acura Pharmaceuticals
    Inventors: Vijai Kumar, David Dixon, Divya Tewari, Dilip B. Wadgaonkar
  • Patent number: 8637541
    Abstract: 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: Grant
    Filed: September 17, 2009
    Date of Patent: January 28, 2014
    Assignee: Merck Canada Inc.
    Inventor: Zhaoyin Wang
  • Patent number: 8637542
    Abstract: 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: Grant
    Filed: March 16, 2009
    Date of Patent: January 28, 2014
    Assignee: Intellikine, Inc.
    Inventors: Yi Liu, Pingda Ren, Liansheng Li, Katrina Chan, Troy Edward Wilson