Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Six Membered Hetero Ring By Nonionic Bonding Patents (Class 514/313)
  • Patent number: 9056105
    Abstract: Described herein are compounds, compositions, and methods useful for treating bone diseases or defects. Also described herein are compounds, compositions and methods for treating bone diseases or defects by inhibiting phosphatase complexes.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: June 16, 2015
    Assignee: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventors: Hiroki Yokota, Ping Zhang
  • Patent number: 9045423
    Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.
    Type: Grant
    Filed: May 12, 2014
    Date of Patent: June 2, 2015
    Assignee: KOWA COMPANY, LTD.
    Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
  • Publication number: 20150148344
    Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Kerim Babaoglu, Britton K. Corkey, Robert H. Jiang, David Sperandio, Hai Yang
  • Patent number: 9040560
    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: December 13, 2013
    Date of Patent: May 26, 2015
    Assignee: Merck Patent GmbH
    Inventors: Amanda E. Sutton, Thomas E. Richardson, Bayard R. Huck, Srinivasa R. Karra, Xiaoling Chen, Yufang Xiao, Andreas Goutopoulos, Ruoxi Lan, David Perrey, Harold George Vandeveer, Lesley Liu-Bujalski, Frank Stieber, Brian L. Hodous, Hui Qiu, Reinaldo C. Jones, Brian H. Heasley
  • Patent number: 9040558
    Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 26, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
  • Publication number: 20150133436
    Abstract: The use of compounds in the treatment of autoimmune and inflammatory diseases or conditions, pharmaceutical compositions containing such compounds and to methods for identifying compounds for use in the treatment of such diseases or conditions.
    Type: Application
    Filed: January 23, 2015
    Publication date: May 14, 2015
    Inventors: Chun-Wa CHUNG, Edwige NICODEME
  • Publication number: 20150133441
    Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
    Type: Application
    Filed: June 6, 2014
    Publication date: May 14, 2015
    Inventor: Gerard M. Housey
  • Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Patent number: 9029395
    Abstract: Tetrahydroquinoline derivatives, pharmaceutical compositions containing such compounds and to their use in therapy.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: May 12, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Dominique Amans, Emmanuel Hubert Demont, Darren Jason Mitchell, Robert J. Watson
  • Patent number: 9029396
    Abstract: The present invention relates to substituted indole derivatives, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: March 3, 2014
    Date of Patent: May 12, 2015
    Assignee: Novartis AG
    Inventors: Nigel Graham Cooke, Rita Ramos, Karen Kammertoens, Maurice Van Eis
  • Publication number: 20150126550
    Abstract: Pharmaceutical uses of 6-amino quinazoline or 3-cyano quinoline derivatives are disclosed. Specifically, the 6-amino quinazoline or 3-cyano quinoline derivatives presented by general formula (I), or tautomers, enantiomers, diastereomers, racemates or pharmaceutically acceptable salts thereof, or metabolites, metabolic precursors or prodrugs thereof, are protein kinase inhibitors, in which each substitutent group of general formula (I) is as defined in the specification.
    Type: Application
    Filed: December 1, 2014
    Publication date: May 7, 2015
    Inventors: Xin LI, Bin WANG
  • Publication number: 20150119421
    Abstract: The present invention includes a method of inhibiting or reducing deregulated FLT3 tyrosine kinase activity or FLT3 tyrosine kinase expression in a subject with a proliferative disease by administering to the subject having or suspected to have the proliferative disease, a therapeutically or prophylactically effective amount of the compound (CP-673,451) of Formula I: or pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: July 30, 2014
    Publication date: April 30, 2015
    Inventor: Vinay K. Jain
  • Publication number: 20150105404
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 16, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings
  • Publication number: 20150105366
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 16, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings, William Moore Jones, Steven Goldberg
  • Publication number: 20150094310
    Abstract: The present invention relates to a corticotropin releasing hormone receptor type 1 (CRHR1) antagonist for use in the treatment of depressive symptoms and/or anxiety symptoms in a novel group of patients, i.e. patients having corticotropin releasing hormone (CRH) overactivity.
    Type: Application
    Filed: April 23, 2013
    Publication date: April 2, 2015
    Inventor: Florian Holsboer
  • Publication number: 20150094333
    Abstract: Disclosed are compounds having the formula: wherein R1, R2R3, R4 and R5 are as defined herein, and methods of making and using the same.
    Type: Application
    Filed: September 13, 2013
    Publication date: April 2, 2015
    Inventors: Linda N. Casillas, Michael P. Demartino, Pamela A. Haile, John F. Mehlmann, Joshi M. Ramanjulu, Robert Singhaus, JR.
  • Publication number: 20150094334
    Abstract: The present invention describes a method for the treatment of a neurological condition in a subject which comprises administering to a subject in need thereof a therapeutically effect amount of a compound of the formula or pharmaceutically acceptable salts, hydrates, or solvates thereof.
    Type: Application
    Filed: October 9, 2014
    Publication date: April 2, 2015
    Applicant: PRANA BIOTECHNOLOGY LIMITED
    Inventors: Kevin Jeffrey BARNHAM, Elisabeth Colette Louise GAUTIER, Gaik Beng KOK, Guy KRIPPNER
  • Patent number: 8993554
    Abstract: Tetrahydroquinoline compounds, pharmaceutical compositions containing such compounds and their use in therapy.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: March 31, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Dominique Amans, Emmanuel Hubert Demont, Darren Jason Mitchell, Jonathan Thomas Seal
  • Publication number: 20150086543
    Abstract: The present invention provides methods of predicting response to a cancer therapy based on the methylation status of the ERBB2 gene. One aspect of the invention provides a method of predicting response to an EGFR inhibitor therapy based on the methylation status of the ERBB2 gene.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 26, 2015
    Applicant: GENENTECH, INC.
    Inventors: Thomas E. Januario, David Shames
  • Patent number: 8987250
    Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: March 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
  • Patent number: 8987302
    Abstract: Methods of treating a hepatitis C virus (HCV) related disease, such as HCV infections in subjects non-responsive to anti-HCV therapy, are described herein, comprising administering to the subject a therapeutically effective amount of hydroxychloroquine. An antiviral agent may be co-administered with the hydroxychloroquine. Methods utilizing synergistic combinations of hydroxychloroquine and an antiviral agent are disclosed. Further disclosed are compositions comprising hydroxychloroquine and an antiviral agent, as well as hydroxychloroquine and uses thereof for the treatment of a hepatitis C virus (HCV) related disease.
    Type: Grant
    Filed: December 26, 2012
    Date of Patent: March 24, 2015
    Assignees: Panmed Ltd., Genoscience Pharma SAS
    Inventor: Philippe Halfon
  • Publication number: 20150080394
    Abstract: The invention provides for compounds that are phosphodiesterase inhibitors. The invention further provides for a method for screening compounds that bind to and modulate a phosphosdiesterase protein. The invention also provides methods for treating conditions associated with accumulated amyloid-beta peptide deposit accumulations by administering a phosphodiesterase-binding compound to a subject.
    Type: Application
    Filed: March 25, 2014
    Publication date: March 19, 2015
    Applicant: COLUMBIA UNIVERSITY
    Inventors: Yan FENG, Ottavio ARANCIO, Shixian DENG, Donald W. LANDRY
  • Publication number: 20150080324
    Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
    Type: Application
    Filed: November 25, 2014
    Publication date: March 19, 2015
    Inventors: Gavin David Heffernan, David Penman Jacobus, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
  • Patent number: 8980918
    Abstract: The invention relates to a stable amorphous form of (5-Fluoro-2-methyl-3-quinolin-2-ylmethyl-indol-1-yl)-acetic acid and its use in the treatment of conditions mediated by the action of PGD2 at the CRTH2 receptor.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 17, 2015
    Assignee: Atopix Therapeutics Limited
    Inventors: Aimesther Betancourt, Marc Lemieux, Roch Thibert
  • Patent number: 8980892
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: March 17, 2015
    Assignees: Syngenta Crop Protection LLC, Syngenta Limited
    Inventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
  • Publication number: 20150073017
    Abstract: Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.
    Type: Application
    Filed: November 14, 2014
    Publication date: March 12, 2015
    Inventors: Xi CHEN, Junfa FAN, Pingchen FAN, Antoni KRASINSKI, Lianfa LI, Rebecca M. LUI, Jeffrey P. McMAHON, Jay P. POWERS, Yibin ZENG, Penglie ZHANG
  • Patent number: 8974827
    Abstract: A pharmaceutical composition comprises nanoparticles comprising a poorly water-soluble drug, a poorly aqueous soluble non-ionizable cellulosic polymer, and a poorly aqueous soluble polymeric amphiphilic non-ionizable block copolymer.
    Type: Grant
    Filed: May 26, 2008
    Date of Patent: March 10, 2015
    Assignee: Bend Research, Inc.
    Inventors: Corey Jay Bloom, Marshall David Crew, Warren Kenyon Miller, Michael Mark Morgen, Daniel Tod Smithey
  • Patent number: 8975278
    Abstract: The present invention describes a method for the treatment of a neurological condition in a subject which comprises administering to a subject in need thereof a therapeutically effect amount of a compound of the formula or pharmaceutically acceptable salts, hydrates, or solvates thereof.
    Type: Grant
    Filed: September 19, 2007
    Date of Patent: March 10, 2015
    Assignee: Prana Biotechnology Limited
    Inventors: Kevin Jeffrey Barnham, Elisabeth Colette Louise Gautier, Gaik Beng Kok, Guy Krippner
  • Patent number: 8975274
    Abstract: The present invention is bis-acridine or bis-quinoline intercalators having a modified bis(4-aminophenyl)ether tether to improve activity, selectivity, solubility and bioavailability of the antitumor compound.
    Type: Grant
    Filed: September 18, 2012
    Date of Patent: March 10, 2015
    Assignee: Trustees of Dartmouth College
    Inventors: Gordon W. Gribble, Justin M. Lopchuk
  • Publication number: 20150057288
    Abstract: A pest control method for honeybee parasitic pests has been found, which is highly safe to honeybees and demonstrates excellent pest control effects against honeybee parasitic pests by using a honeybee parasitic pest control agent containing at least one of a compound represented by Formula (I) and acid addition salts thereof.
    Type: Application
    Filed: November 10, 2014
    Publication date: February 26, 2015
    Applicant: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Ryo HORIKOSHI, Masaaki MITOMI
  • Publication number: 20150057312
    Abstract: The present invention is directed to novel quinolines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are useful for the treatment of protein kinases mediated diseases and conditions. The disclosed substituted quinolines include Bruton's tyrosine kinase (Btk) inhibitors.
    Type: Application
    Filed: April 3, 2013
    Publication date: February 26, 2015
    Inventor: Dawei Zhang
  • Publication number: 20150057279
    Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Publication number: 20150050239
    Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: July 19, 2013
    Publication date: February 19, 2015
    Applicants: Calitor Sciences, LLC, Sunshine Lake Pharma Co., Ltd.
    Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
  • Publication number: 20150051245
    Abstract: The invention relates to protein binding inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating cell proliferative disorders, especially cancer.
    Type: Application
    Filed: November 13, 2012
    Publication date: February 19, 2015
    Inventors: William G. Cance, Ravindra K. Pandey, Elena V. Kurenova, Manivannan Ethirajan
  • Patent number: 8957092
    Abstract: A compound of formula 6-(methylcarbamoyl)-4-[(4-methylphenyl)amino]quinoline-3-carboxylic acid, and pharmaceutically acceptable salts thereof, is provided. The compound can be used to treat cancer, diabetic retinopathy, age-related macular degeneration, inflammation, stroke, ischemic myocardium, atherosclerosis, macular edema and psoriasis.
    Type: Grant
    Filed: August 30, 2013
    Date of Patent: February 17, 2015
    Assignee: ClanoTech AB
    Inventors: Jacob Westman, Natalia Nekhotiaeva, Johan Wannberg, Ulrika Backman, Johan Malm
  • Patent number: 8951999
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Orexo AB
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
  • Publication number: 20150037397
    Abstract: The present invention relates to pharmaceutical compositions comprising a compound of formula (I) and a cyclodextrin or a liposome, to the process of preparing said compositions and their use for antitumor, antiviral, antiparasitic and antifungal treatment.
    Type: Application
    Filed: December 22, 2011
    Publication date: February 5, 2015
    Applicant: TRASLATIONAL CANCER DRUGS PHARMA, S.L.
    Inventors: Beatriz Palacios Izquierdo, Peter Van HoogeVest, Mathew L.S. Leigh
  • Publication number: 20150038509
    Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
    Type: Application
    Filed: June 12, 2014
    Publication date: February 5, 2015
    Inventors: Gary J. Bridger, Renato T. Skerlj, Al Kaller, Curtis Harwig, David Earl Bogucki, Trevor R. Wilson, Jason B. Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosario DiFluri
  • Publication number: 20150038531
    Abstract: An aminopyridine derivative of Formula 1 and a method of preventing or treating cancer using the same. Formula 1: In Formula 1: X1 and X2 are each independently selected from the group consisting of carbon and nitrogen; R1 to R5 are each independently selected from the group consisting of a hydrogen, a straight, a branched, or cyclo alkyl of C1-C4, a halogen, and a hydroxyl; and R6 is a hydrogen or an alkyl of C1-C6.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Inventors: Sunghoon Kim, Hee Sook Lee, Young Sun Oh, Dae Gyu Kim
  • Patent number: 8946261
    Abstract: The present invention relates to novel substituted 1,2,3,4-tetrahydroquinolin-7-yl carbamates, their preparation, and use as therapeutic agents, particularly in the prevention or treatment of neurodegenerative or Alzheimer's disease, or senile dementia, or memory disturbances, and more particularly to the prevention, treatment and amelioration of Alzheimer's disease with the novel substituted 1,2,3,4-tetrahydroquinolin-7-yl carbamates, which act as inhibitors of central cholinesterase enzymes, particularly acetylcholinesterase (AChE) following the indirect cholinomimetic pathway. The present invention particularly relates to compounds of formula A: Formula A wherein R1=alkyl, aryl, substituted aryl; R2=H, methyl; R3=H, alkyl, alkenyl, alkynyl, aralkyl, substituted aralkyl, aryl, heteroaryl.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: February 3, 2015
    Assignee: Council of Scientific & Industrial Research
    Inventors: Kuldeep Kumar Roy, Santoshkumar Tota, Chandishwar Nath, Rakesh Shukla, Anil Kumar Saxena
  • Patent number: 8946443
    Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents a C1 to C6 alkyl group which may be substituted by one to three groups selected from substituent group A, or the like (substituent group A: a hydroxy group, a halogeno group, a cyano group, a nitro group, an amino group, a carboxy group, a C1 to C3 alkyl group, etc.); R2, R3, and R8 each independently represent a hydrogen atom or a C1 to C3 alkyl group; R4, R5, R6, R7, R9, and R10 each independently represent a hydrogen atom or the like; and R11 represents a hydrogen atom or the like, has TAFIa enzyme inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, or the like.
    Type: Grant
    Filed: March 14, 2011
    Date of Patent: February 3, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Tsutomu Nagata, Jun Kobayashi, Yoshiyuki Onishi, Masamichi Kishida, Kengo Noguchi
  • Publication number: 20150031677
    Abstract: Monomeric and dimeric trioxane thioacetals and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
    Type: Application
    Filed: February 28, 2013
    Publication date: January 29, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Gary H. Posner, Alexander M. Jacobine, Rachel D. Slack, Jennifer R. Mazzone
  • Publication number: 20150031723
    Abstract: A new medical therapy, and more particularly certain quinoline compounds which are anti-angiogenic integrin aplha5beta1 inhibitors, for use in the treatment of fibrosis, or a fibrosis-related disease, such as a fibrotic disease affecting the lung, liver, kidney, skin, epidermis, endodermis, muscle, tendon, cartilage, heart, stomach, large intestine, small intestine, colon, uterus, nervous system, testis, adrenal gland, artery, vein, biliary tract, or eye.
    Type: Application
    Filed: January 4, 2013
    Publication date: January 29, 2015
    Inventor: Yihai Cao
  • Patent number: 8940724
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjogren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: January 27, 2015
    Assignee: Amgen Inc.
    Inventors: Timothy D. Cushing, Paul John Dransfield, Felix Gonzalez Lopez de Turiso, Michael G. Johnson, Todd Kohn, Vatee Pattaropong, Jillian L. Simard
  • Patent number: 8940764
    Abstract: Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed.
    Type: Grant
    Filed: May 26, 2006
    Date of Patent: January 27, 2015
    Assignee: Aldexa Therapeutics, Inc.
    Inventors: Thomas A. Jordan, John E. Dowling, John Clifford Chabala
  • Publication number: 20150025054
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: January 22, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estirate Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Lar
  • Patent number: 8937085
    Abstract: The present invention relates to a pharmaceutical carrier composition and a pharmaceutical composition comprising said pharmaceutical carrier composition. The pharmaceutical composition comprises: (a) at least 20% (w/w) of the composition of a sugar or a sugar alcohol; (b) one or more pharmaceutically acceptable excipients; (c) one or more pharmaceutically active ingredients in their base form; and (d) water up to 100% (w/w). The present pharmaceutical composition is especially resistant against flocculation, clumping and/or precipitation at room temperature during prolonged time-periods such as one or more years.
    Type: Grant
    Filed: February 13, 2008
    Date of Patent: January 20, 2015
    Assignee: Dafra Pharma N.V.
    Inventor: Frans Herwig Jansen
  • Publication number: 20150018371
    Abstract: Positive allosteric modulators of melanocortin receptors, especially allosteric potentiators of the receptors MC3R and MC4R are described herein. Also provided are pharmaceutical compositions containing the positive allosteric modulators and methods of treating obesity or an obesity-related disorder such as type 2 diabetes, comprising administering an effective amount of the positive allosteric modulator.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 15, 2015
    Inventors: Roger D. Cone, Julien A. Sebag, Jacques Pantel, Savannah Y. Williams, David C. Weaver, Gary A. Sulikowski, Craig W. Lindsley, Padma S. Portonova, Chao Zhang
  • Publication number: 20150011551
    Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 8, 2015
    Applicant: Sanford- Burnham Medical Reseach Institute
    Inventors: Anthony B. Pinkerton, Russell Dahl, Nicholas D.P. Cosford, Jose Luis Millan
  • Patent number: 8927577
    Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: January 6, 2015
    Assignee: Pfizer Inc.
    Inventors: Mary Didiuk, Kevin J. Filipski, Angel Guzman-Perez, Esther C. Lee, Jeffrey A. Pfefferkorn, Benjamin Stevens, Meihua Tu