Nitrogen Attached Indirectly To The Morpholine Ring By Acyclic Nonionic Bonding Patents (Class 514/237.8)
  • Patent number: 9884833
    Abstract: The present invention includes crystalline forms of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide disulfate and crystalline forms of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide monosulfate. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic use of the crystalline forms. In one embodiment, the crystalline compound is (2S,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide.
    Type: Grant
    Filed: September 13, 2016
    Date of Patent: February 6, 2018
    Assignee: PharmatrophiX, Inc.
    Inventors: Rajgopal Munigeti, Frank M. Longo
  • Patent number: 9884806
    Abstract: Cyclic vinylogous amides of Formula I are disclosed The compounds are useful for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are inhibitors of bromodomain.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: February 6, 2018
    Assignee: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI
    Inventors: Ming-Ming Zhou, Michael Ohlmeyer, Adam Vincek, Nilesh Zaware
  • Patent number: 9630914
    Abstract: Multitarget inhibitors of the enzymes Fatty Acid Amide Hydrolase (FAAH), Cyclooxygenase-1 (COX-1) and/or Cyclooxygenase-2 (COX-2) having a specific carbamate moiety on the meta or ortho position of the A ring of a substituted biphenyl core and having an halogen in the ortho position of the B ring of the biphenyl core. Also concerns the therapeutical application of the multitarget inhibitors, in particular, in the prevention and treatment of cancer.
    Type: Grant
    Filed: August 1, 2013
    Date of Patent: April 25, 2017
    Assignees: Fondazione Istituto Italiano Di Tecnologia, The Regents of the University of California, Alma Mater Studiorum—Universita' Di Bologna
    Inventors: Marco De Vivo, Rita Scarpelli, Andrea Cavalli, Marco Migliore, Daniele Piomelli, Damien Habrant, Angelo Favia
  • Patent number: 9314466
    Abstract: Disclosed herein are methods of treating a patient suffering from a cognitive disorder using the following compounds:
    Type: Grant
    Filed: February 19, 2014
    Date of Patent: April 19, 2016
    Assignee: Allergan, Inc.
    Inventors: John E. Donello, Fabien J. Schwieghoffer, Lauren M. Luhrs
  • Patent number: 9271986
    Abstract: The present invention includes crystalline forms of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide and crystalline forms of salts and/or solvates of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic use of the crystalline forms.
    Type: Grant
    Filed: November 12, 2010
    Date of Patent: March 1, 2016
    Assignee: PharmatrophiX, Inc.
    Inventors: Rajgopal Munigeti, Frank M. Longo
  • Patent number: 9238625
    Abstract: The present invention provides novel phenylcycloalkylmethylamine derivatives, and methods of preparing phenylcycloalkylmethylamine derivatives. The present invention also provides methods of using phenylcycloalkylmethylamine derivatives and compositions of phenylcycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.
    Type: Grant
    Filed: December 31, 2012
    Date of Patent: January 19, 2016
    Assignee: REVIVA PHARMACEUTICALS, INC.
    Inventors: Laxminarayan Bhat, Kouacou Adiey, Seema Rani Bhat
  • Patent number: 9199936
    Abstract: Disclosed are compounds of formula: that inhibiting GPBP activity, making them useful as therapeutics in antibody-mediated disorders, drug-resistant cancer, inflammation, protein misfolding and ER stress-mediated disorders, and aberrant apoptosis.
    Type: Grant
    Filed: October 25, 2013
    Date of Patent: December 1, 2015
    Assignee: Fibrostatin Sociedad Limitada
    Inventors: Juan Saus, Santos Fustero, Juan F Sanz-Cervera, Enrique Pérez-Payá, Raül Blasco, Francisco Revert-Ros, Fernando Revert
  • Patent number: 9156801
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-substituted oleanolic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: October 13, 2015
    Assignee: Hangzhou Bensheng Pharmaceutical Co., Ltd.
    Inventors: Rongzhen Xu, Frank Rong, Hongxi Lai, Fuwen Xie
  • Patent number: 9150865
    Abstract: Certain embodiments are directed to compositions and methods of inhibiting pathogenic bacterial infection involving ADAMIO comprising administering an effective amount of a metalloprotease inhibitor to a patient. Certain embodiments are directed to method of inhibiting Staphylococcal infection comprising administering an effective amount of a metalloprotease inhibitor to a patient. Other embodiments concern methods of inhibiting infection by a bacteria from the genus Clostridium, Streptococcus, Listeria, Bacillus, or Arcanobacterium.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: October 6, 2015
    Assignee: The University of Chicago
    Inventor: Juliane Bubeck Wardenburg
  • Patent number: 9120765
    Abstract: The present invention relates to compounds which activate the p53 response, and find use in, for example, hyperproliferative diseases such as cancer treatment and potentially other diseases/conditions involving sirtuin function.
    Type: Grant
    Filed: May 3, 2013
    Date of Patent: September 1, 2015
    Assignees: University Court of the University of Dundee, University Court of the University of St. Andrews
    Inventors: Sonia Lain, David Phillip Lane, Michael John Raymond Stark, Anna Rose McCarthy, Jonathan James Hollick, Nicholas James Westwood
  • Publication number: 20150148318
    Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 28, 2015
    Inventors: Hoau-Yan Wang, Lindsay Burns Barbier
  • Publication number: 20150133297
    Abstract: The present invention relates to new antifungal compositions and their use in the treatment of agricultural products.
    Type: Application
    Filed: April 25, 2013
    Publication date: May 14, 2015
    Inventors: Jacobus Stark, Eva Louise Wilhelmine Sack
  • Publication number: 20150119396
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft 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: April 30, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Publication number: 20150118221
    Abstract: The present invention relates to the field of cardiology. More specifically, the present invention provides methods and compositions useful for treating cardiac hypertrophy. In a specific embodiment, a method for treating or preventing cardiac hypertrophy in a patient comprises the step of administering a therapeutically effective amount of a glycolipid synthesis inhibitor.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 30, 2015
    Applicant: The John Hopkins University
    Inventor: Subroto Chatterjee
  • Publication number: 20150087649
    Abstract: Methods and agents are provided for treatment of disorders associated with aberrant adrenocortical cell behavior, including (but not limited to) treatment of adrenocortical carcinoma (ACC) and/or Cushing's syndrome. Such methods involve administration of an agent which exhibits an IC50 value against huACAT1 of less than 10 ?M, and one or more further characteristics including effects on adrenocortical cells, disruption of cholesterol homeostasis, reduction in steroid biosynthesis, reduction of mitochondrial function, and/or preferential binding to by low-density lipoprotein (LDL).
    Type: Application
    Filed: September 26, 2014
    Publication date: March 26, 2015
    Inventors: Stephen Warren Hunt, III, Julia Christine Owens, William E. Rainey, JR., Christopher R. LaPensee, Gary D. Hammer
  • Publication number: 20150079035
    Abstract: The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.
    Type: Application
    Filed: April 2, 2013
    Publication date: March 19, 2015
    Inventors: Brent R. Stockwell, Scott J. Dixon, Rachid Skouta
  • Publication number: 20150080400
    Abstract: The compounds of formula (1) in which R1, R4, A and X have the meanings as given in the description, are novel effective EP2 agonists.
    Type: Application
    Filed: April 30, 2013
    Publication date: March 19, 2015
    Applicant: TAKEDA GMBH
    Inventors: Angelika Hoffmeyer, Rainer Boer, Manuela Hessmann, Andreas Pahl, Torsten Dunkern, Simone Hartung, Christof Zitt, Jurgen Volz, Christiane Praechter, Mahindra Makhija, Hiteshkumar Jain, Sandip Gavade, Arati Prabhu, Manojkumar Tiwari, Ashish Keche, Sarvesh Patel
  • Publication number: 20150051144
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as hyperlipidemia and also have a beneficial effect on cholesterol.
    Type: Application
    Filed: September 26, 2012
    Publication date: February 19, 2015
    Inventors: Harikishore Pingali, Vrajesh Pandya
  • Publication number: 20150031663
    Abstract: The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo.
    Type: Application
    Filed: October 13, 2014
    Publication date: January 29, 2015
    Applicant: UNIVERSITY OF NOTRE DAME DU LAC
    Inventors: Shahriar Mobashery, Dusan Hesek, Mayland Chang
  • Publication number: 20150025077
    Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives.
    Type: Application
    Filed: February 27, 2013
    Publication date: January 22, 2015
    Applicant: COYOTE PHARMACEUTICALS, INC.
    Inventors: Hiroaki Serizawa, Ankush B. Argade, Akash Datwani, Natalie Spencer, Yonghua Pan, Florian Ermini
  • Publication number: 20150018340
    Abstract: The present invention relates to compounds having a pipecolate diketoamide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said pipecolate diketoamide compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.
    Type: Application
    Filed: December 24, 2012
    Publication date: January 15, 2015
    Inventors: Ranganath Gopalakrishnan, Felix Hausch
  • Publication number: 20140378459
    Abstract: [Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.
    Type: Application
    Filed: September 14, 2012
    Publication date: December 25, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Jiro Fujiyasu, Kazuhiko Ohne, Susumu Yamaki, Tomoyoshi Imaizumi, Takeshi Hondo, Keisuke Matsuura, Tomohki Satou, Satoshi Sasamura
  • Patent number: 8916556
    Abstract: Methods and compounds for treating neurodegenerative and other disorders. Included is the administering to a subject in need thereof an effective amount of a compound having binding specificity for a p75NTR receptor molecule. Enhanced survival of neural and other cells has been observed.
    Type: Grant
    Filed: April 19, 2010
    Date of Patent: December 23, 2014
    Assignees: The University of North Carolina at Chapel Hill, The Regents of The University of California, The United States of America represented by the Department of Vetran Affairs
    Inventors: Frank M. Longo, Stephen M. Massa
  • Publication number: 20140371316
    Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropiomc acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
    Type: Application
    Filed: November 23, 2012
    Publication date: December 18, 2014
    Inventors: Jill S. FABRICANT, Iraj LALEZARI
  • Publication number: 20140371176
    Abstract: This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.
    Type: Application
    Filed: September 3, 2014
    Publication date: December 18, 2014
    Inventors: Neil W. Johnson, Jiri Kasparec, Meagan B. Rouse, Xinrong Tian
  • Patent number: 8912177
    Abstract: A method of treating polycystic kidney disease in a subject comprises administering to the subject an effective amount of a compound represented by Structural Formula (1): or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 3, 2008
    Date of Patent: December 16, 2014
    Assignee: Genzyme Corporation
    Inventors: Thomas A. Natoli, Oxana Ibraghimov-Beskrovnaya, John P. Leonard, Nelson S. Yew, Seng H. Cheng
  • Patent number: 8912185
    Abstract: The invention relates to the use of glutaric acid derivatives of general formula (I), which are disclosed in the invention description, as anti-arrhythmic agents.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: December 16, 2014
    Assignee: Obschestvo S Ogranichennoi Otvetstvennostyu “Pharmenterprises”
    Inventors: Vladimir Evgenievich Nebolsin, Dmitry Sergeevich Blinov, Vladimir Pavlovich Balashov, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina
  • Publication number: 20140350017
    Abstract: Compounds, compositions, and methods comprising a polyamine compound are described, which may be used to kill, disperse, treat, reduce biofilms, and/or inhibit or substantially prevent biofilm formation. In certain aspects, the present invention relates to compounds, compositions, and methods comprising polyamine compounds that have antimicrobial or dispersing activity against a variety of bacterial strains capable of forming biofilms.
    Type: Application
    Filed: November 8, 2013
    Publication date: November 27, 2014
    Applicants: The University of Utah, Curza Global, LLC
    Inventors: Dustin Williams, Ryan Looper, Sujeevini Jeyapalina, Travis Haussener, Paul R. Sebahar, Hari Kanna Reddy
  • Patent number: 8895551
    Abstract: The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: April 2, 2010
    Date of Patent: November 25, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hidenori Mikamiyama, Akira Matsumura, Moriyasu Masui, Kosuke Anan, Kayoko Hata
  • Publication number: 20140343064
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-substituted oleanolic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 20, 2014
    Applicant: Hanghzhou Bensheng Pharmaceutical Co., Ltd
    Inventors: Rongzhen Xu, Frank Rong, Hongxi Lai, Fuwen Xie
  • Publication number: 20140343000
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 20, 2014
    Inventors: Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Ny Sin, Brian Lee Venables, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell
  • Publication number: 20140336194
    Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.
    Type: Application
    Filed: July 28, 2014
    Publication date: November 13, 2014
    Applicant: NOVARTIS AG
    Inventor: Shi Yin FOO
  • Publication number: 20140335083
    Abstract: The present invention provides compositions and methods useful for treating and preventing neovascular AMD by inhibition of CCR3.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 13, 2014
    Applicant: Glaxo Group Limited
    Inventors: Peter Adamson, David Shima, Yin Shan Eric Ng
  • Publication number: 20140336185
    Abstract: Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP (1-42), PTH (1-34), Glucagon (1-29), GLP-2 (1-33), GLP-1 (7-36), GLP-1 (9-36), oxyntomodulin and exendin variants.
    Type: Application
    Filed: May 31, 2012
    Publication date: November 13, 2014
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Thomas Fowler, Andrew Novak, Premji Meghani, Enugurthi Brahmachary, Adam Richard Yeager
  • Patent number: 8884007
    Abstract: The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof; to a composition comprising a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluent; and also to use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, or preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, or preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.
    Type: Grant
    Filed: May 16, 2011
    Date of Patent: November 11, 2014
    Assignee: Institute of Pharmacology and Toxicology Medical Sciences P.L.A. China
    Inventors: Song Li, Wu Zhong, Juan Liu, Lili Wang, Kunlun He, Long Long, Junhai Xiao, Zhibing Zheng, Wei Li, Xin Li, Guoliang Hu
  • Patent number: 8877747
    Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.
    Type: Grant
    Filed: October 21, 2009
    Date of Patent: November 4, 2014
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
  • Publication number: 20140309181
    Abstract: Small compounds that modulate the expression of and/or function of sodium channel, voltage-gated, alpha subunit (SCNxA) are presented. Pharmaceutical compositions containing such small molecules and their use in treating diseases and disorders associated with the expression of SCNxA are also presented.
    Type: Application
    Filed: August 28, 2012
    Publication date: October 16, 2014
    Applicant: CuRNA, Inc.
    Inventors: Joseph Collard, Olga Khorkova Sherman, Jane H. Hsiao
  • Publication number: 20140301979
    Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.
    Type: Application
    Filed: June 25, 2014
    Publication date: October 9, 2014
    Applicant: SIGA TECHNOLOGIES, INC.,
    Inventors: Sean M. AMBERG, Dongcheng DAI, Tove C. BOLKEN, Dennis E. HRUBY
  • Publication number: 20140296240
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 2, 2014
    Inventors: Gary Mark COPPOLA, Yuki IWAKI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Gary Michael KSANDER, Muneto MOGI, Robert SUN
  • Publication number: 20140275091
    Abstract: Provided herein is a pharmaceutical formulation comprising a GGA derivative in the form of an eye drop. Also provided herein are methods of treating neural diseases or disorders by administering such pharmaceutical formulations.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Hiroaki Serizawa, Tilmann M. Brotz
  • Publication number: 20140256702
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: March 4, 2014
    Publication date: September 11, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Erik Fenster, Melissa Fleury, Adam D. Hughes
  • Publication number: 20140256729
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft 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: September 11, 2014
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Publication number: 20140256698
    Abstract: The present invention is directed to inhibitors of cathepsins and the methods for using and making such inhibitors.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 11, 2014
    Inventors: Robert Booth, Jeff Dener, Michael Green
  • Patent number: 8802673
    Abstract: The present invention relates to compounds of formula I wherein A, B, X, Y, Ar, R1, R2, R?, m and n are as defined herein and to pharmaceutical active acid addition salts thereof, which have a good affinity to the trace amine associated receptors TAAR1, so that they can be used for the treatment of depression, anxiety disorders and bipolar disorder.
    Type: Grant
    Filed: March 20, 2012
    Date of Patent: August 12, 2014
    Assignee: Hoffmann-La Roche Inc
    Inventors: Guido Galley, Roger David Norcross, Philippe Pflieger
  • Patent number: 8802666
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: August 12, 2014
    Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
  • Publication number: 20140221361
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-19 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I and II: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Inventors: Jacob Swidorski, Brian Lee Venables, Zheng Liu, Ny Sin, Nicholas A. Meanwell, Alicia Regueiro-Ren
  • Patent number: 8796298
    Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: August 5, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Melissa Dumble, Tona Gilmer, Rakesh Kumar, Peter F. Lebowitz, Shannon Renae Morris, Sylvie Laquerre
  • Publication number: 20140200197
    Abstract: The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: September 9, 2013
    Publication date: July 17, 2014
    Inventors: JOHN A. MCCAULEY, CHRISTIAN BEAULIEU, DAVID J. BENNETT, CHRISTOPHER J. BUNGARD, RONALD K. CHANG, SHELDON CRANE, THOMAS J. GRESHOCK, LI HAO, KATE HOLLOWAY, JESSE J. MANIKOWSKI, DANIEL MCKAY, CARMELA MOLINARO, OSCAR MIGUEL MORADEI, PHILIPPE G. NANTERMET, CHRISTIAN NADEAU, TUMMANAPALLI SATYANARAYANA, WILLIAM SHIPE, SANJAY KUMAR SINGH, VOUY LINH TRUONG, SIVALENKA VIJAYARADHI, PETER D. WILLIAMS, CATHERINE M. WISCOUNT
  • Publication number: 20140179687
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Application
    Filed: February 21, 2014
    Publication date: June 26, 2014
    Applicant: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michael Pawlotsky
  • Publication number: 20140178503
    Abstract: The present invention relates to new cyclohexyl urea modulators of D2 receptors and/or modulators of D3 receptors, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: February 26, 2014
    Publication date: June 26, 2014
    Applicant: Auspex Pharmaceuticals, Inc.
    Inventors: Ronald C. Newbold, Chengzhi Zhang