Exactly Five Ring Nitrogens In The Bicyclo Ring System (e.g., Triazolo[4,5-d]pyrimidine, Etc.) Patents (Class 514/261.1)
  • Patent number: 10183946
    Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 and n are defined as in the description and in the claims. The compound of formula (I) can be for treating.
    Type: Grant
    Filed: April 4, 2017
    Date of Patent: January 22, 2019
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Uwe Grether, Matthias Nettekoven, Mark Rogers-Evans, Sebastien Schmitt, Benjamin James Stenton
  • Patent number: 10106547
    Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.
    Type: Grant
    Filed: August 21, 2017
    Date of Patent: October 23, 2018
    Assignee: Vernalis (R&D) Limited
    Inventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
  • Patent number: 10017515
    Abstract: The present invention relates to a stable amorphous ticagrelor and a process for its preparation.
    Type: Grant
    Filed: August 11, 2015
    Date of Patent: July 10, 2018
    Assignee: Sun Pharmaceutical Industries Limited
    Inventors: Nagaraju Gottumukkala, Anil Saini, Ram Thaimattam, Mahavir Singh Khanna, Mohan Prasad
  • Patent number: 9982061
    Abstract: The disclosure generally provides antibodies and antigen binding fragments of antibodies that bind ticagrelor and metabolites of ticagrelor. The disclosure also provides compositions comprising the antibodies, nucleic acid molecules encoding the antibodies, methods of treating a patient comprising administering the antibodies, and methods of making and using the antibodies.
    Type: Grant
    Filed: September 30, 2015
    Date of Patent: May 29, 2018
    Assignee: MEDIMMUNE LIMITED
    Inventors: Andrew Buchanan, Sven Nylander, Mark Penney, Philip Newton, Feenagh Keyes, Tord Inghardt
  • Patent number: 9795669
    Abstract: The compound N-(4-{[4-amino-2-butyl-1H-imidazo[4,5-c]quinolin-1-yl]oxyl}butyl)octadecanamide is a useful drug compound for enhancing immune response and can be used, for example, as a vaccine adjuvant and a cancer treatment.
    Type: Grant
    Filed: December 15, 2015
    Date of Patent: October 24, 2017
    Assignee: 3M INNOVATIVE PROPERTIES COMPANY
    Inventor: Paul D. Wightman
  • Patent number: 9376443
    Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.
    Type: Grant
    Filed: February 10, 2015
    Date of Patent: June 28, 2016
    Assignee: VERNALIS (R&D) LIMITED
    Inventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
  • Publication number: 20150099751
    Abstract: The in situ gel loaded with phosphodiesterase Type V (PDE5) inhibitors nanoemulsion was prepared using an innovative approach to reformulate the PDE5 inhibitors in a nanoemulsion, and then loading the nanoemulsion into an in situ gel base. These preparations are administered by intramuscular injection in order to give a depot effect for a period of time that exceeds 15 days. The in situ gel composition gives slow, controlled release of the PDE5 inhibitor. The in situ gel composition is useful for prophylaxis and treatment of some important chronic diseases, such as diabetic complications, benign prostatic hyperplasia, erectile dysfunction, and diseases associated with endothelial dysfunction.
    Type: Application
    Filed: October 7, 2013
    Publication date: April 9, 2015
    Applicant: KING ABDULAZIZ UNIVERSITY
    Inventors: HISHAM AHMED MOHAMMED MOSLI, SALAH ABDELMONEIM GHAREIB ATTEIAH, KHALED MOHAMED HOSNY OMAR, HANY MOHAMED ABD EL-MALIK EL-BASSOSSY, MOHAMED HANY ABDULWAHAB MOSILHY HELAL
  • 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
  • Patent number: 8987279
    Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.
    Type: Grant
    Filed: May 8, 2013
    Date of Patent: March 24, 2015
    Assignee: Vernalis (R&D) Limited
    Inventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
  • Publication number: 20150072970
    Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.
    Type: Application
    Filed: May 19, 2014
    Publication date: March 12, 2015
    Applicant: MELINTA THERAPEUTICS, INC.
    Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
  • Publication number: 20140378431
    Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.
    Type: Application
    Filed: December 21, 2012
    Publication date: December 25, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Dieter Dorsch, Guenter Hoelzemann, Kai Schiemann, Ansgar Wegener
  • Patent number: 8883802
    Abstract: The present invention relates to novel co-crystal forms of the compound of formula (I); wherein the co-former molecule is selected from glycolic acid, salicylic acid, decanoic (capric) acid, gentisic acid (2,5-dihydroxybenzoic acid), glutaric acid, vanillic acid (4-hydroxy-3-methoxybenzoic acid), succinic acid, malonic acid or maltol (3-hydroxy-2-methyl-4-pyrone); and to processes for their preparation, to pharmaceutical compositions containing such co-crystals, to the use of such co-crystals in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a co-crystal of the compound of formula (I).
    Type: Grant
    Filed: December 3, 2010
    Date of Patent: November 11, 2014
    Assignee: Astrazeneca AB
    Inventors: Stephen David Cosgrove, Matthew Jonathan Jones, Anna Polyakova-Akkus, Valeriya Nikolayevna Smolenskaya, Brenton Skylar Wolfe
  • Publication number: 20140329781
    Abstract: The present invention relates to a once-a-day therapeutically synergistic pharmaceutical dosage form for treatment of cardiovascular disorders, wherein the dosage form comprises a fixed dose combination of metoprolol in extended release form and one or more antiplatelet agent along with one or more rate controlling excipients.
    Type: Application
    Filed: November 1, 2012
    Publication date: November 6, 2014
    Applicant: WOCKHARDT LIMITED
    Inventors: Mandar Kodgule, Amit Gupta, Premchand Nakhat, Girish Kumar Jain
  • Publication number: 20140296258
    Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.
    Type: Application
    Filed: October 31, 2013
    Publication date: October 2, 2014
    Applicant: AstraZeneca UK Limited
    Inventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
  • Publication number: 20140286943
    Abstract: The present invention relates to new cyclopropyl modulators of P2Y12 receptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: June 9, 2014
    Publication date: September 25, 2014
    Inventors: Tadimeti Rao, Chengzhi Zhang
  • Publication number: 20140288032
    Abstract: Agents that inhibit or prevent restenosis are identified by assaying test agents in a battery of assays to measure the effect of the test agent on cell proliferation, thrombosis, tissue modeling, and inflammation. Treatment for restenosis is provided using compositions of the invention.
    Type: Application
    Filed: March 18, 2014
    Publication date: September 25, 2014
    Applicant: DiscoveRx Corporation
    Inventors: Eric J. Kunkel, Evangelos Hytopoulos, Ivan Plavec
  • Publication number: 20140288046
    Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: April 11, 2014
    Publication date: September 25, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Jean-Michel Adam, Caterina Bissantz, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans
  • Publication number: 20140256747
    Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives.
    Type: Application
    Filed: October 26, 2012
    Publication date: September 11, 2014
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Borut Zupancic, Nenad Maras, Damjan Sterk
  • Publication number: 20140235593
    Abstract: In one aspect, the invention relates to novel substituted 2-alkyl-1-oxo-N-phenyl-3-heteroaryl-1,2,3,4-tetrahydroisoquinoline-4-carboxamides; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating and/or preventing malaria. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: August 24, 2012
    Publication date: August 21, 2014
    Applicants: ST. JUDE CHILDREN'S RESEARCH HOSPITAL, RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY, MMV MEDICINES FOR MALARIA VENTURE
    Inventors: Rodney Kiplin Guy, Fangyi Zhu, Wendyam Armand Guiguemde, David Floyd, Spencer Knapp, Philip Stein, Steve Castro
  • Patent number: 8791124
    Abstract: The present invention pertains to the use of inhibitors of phosphodiesterase I, IV and V for the prophylaxis and treatment of prostatic diseases, in particular the use of a) 2-(2-propoxy-phenyl)-8-azapurin-6-one (zaprinast); b) dipyridamole; c) 1-(3-chlorophenylamino)-4-phenylphthalazine (M5445); d) 2-(N-(4-carboxypiperidine-6-chloro-4-(3,4-(methylendioxy)benzyl)amino)quinazoline (E 4021, ER 21355); e) 2,3-dihydro-8-hydroxy-7-nitro-1,4-benzodioxine-2-methanol, alpha-nitrate (E 4701); f) 4-((3,4-(methylendioxy)benzyl)amino)-6,7,8-trimethoxy-quinazoline; g) 1-methly-3-propyl-6-(5-(N-(4-methylmorpholino)sulfonyl)-2-ethoxyphenyl)pyrazole[4,5]pyrimidin-4(5H)one (sildenafil); i) 1-cyclopentyl-3-methyl-6-(4-pyridinyl)pyrazolo(3,4-d)pyrimidin-4(5H)-one (WIN 58237); j) 7-(3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxypropoxy)-2-carboxy-2,3-didehydro-chronan-4-one (PPL-557212); k) quinazolines and their trimethoxy derivatives; l) Pyrazolopyrimidones; as well as pharmacologically compatible salts thereof, quinazolin
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: July 29, 2014
    Assignee: Uropep Biotech GBR
    Inventors: Wolf-Georg Forssmann, Christian Georg Stief, Michael Carsten Truβ, Stefan Uckert, Udo Jonas
  • Publication number: 20140179518
    Abstract: The present invention relates to pesticidal mixtures comprising as active components 1) at least one cyanosulfoximine compound I of the formula I wherein R1, R2 and G are defined as in the description; and 2) at least one fungicidal compounds II selected from azoles, strobilurins, carboxamides, carbamates, heterocyclic and various other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes and harmful fungis in and on plants, and for protecting such plants being infested with pests, especially also for protecting seeds.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: BASF SE
    Inventors: Delphine BREUNINGER, Henricus Maria Martinus BASTIAANS, Wolfgang VON DEYN, Matthias POHLMAN, Juergen LANGEWALD, Egon HADEN
  • Publication number: 20140162970
    Abstract: The present invention relates to new methods for treating and/or preventing cardiac arrhythmias, heart failure, stroke and/or peripheral artery disease by administering a composition comprising triazolopyrimidine, or derivative or metabolite thereof. In particular, the present invention relates to methods for treating cardiac arrhythmias, heart failure, stroke and/or peripheral artery disease by administering CycloPentyl-TriazoloPyrimidine.
    Type: Application
    Filed: August 7, 2013
    Publication date: June 12, 2014
    Applicant: HearlDrug Research, L.L.C.
    Inventor: Victor L. Serebruany
  • Patent number: 8741906
    Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: June 3, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Michel Adam, Caterina Bissantz, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans
  • Publication number: 20140148433
    Abstract: The present application relates to novel bicyclic azaheterocycles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: August 31, 2011
    Publication date: May 29, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Lars Bärfacker, Stefan Weigand
  • Publication number: 20140147505
    Abstract: The present invention relates to a solid pharmaceutical dosage form comprising ticagrelor as pharmaceutically active ingredient, to certain particles of ticagrelor and to processes of preparing the same.
    Type: Application
    Filed: January 29, 2014
    Publication date: May 29, 2014
    Applicant: ratiopharm GmbH
    Inventors: Sandra BRUECK, Dominique MEERGANS
  • Publication number: 20140148472
    Abstract: Disclosed are compounds able to modulate the activity of the GPR17 receptor in a highly specific way, which are useful in the treatment and diagnosis of diseases or dysfunctions involving the activation of said receptor. In particular, the compounds according to the invention can be used for neuroprotective and/or reparatory purposes, in cerebral, cardiac and renal ischaemia, in cerebral trauma, in chronic neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS), and in demyelinating diseases such as multiple sclerosis.
    Type: Application
    Filed: November 2, 2011
    Publication date: May 29, 2014
    Applicant: CENTRO CARDIOLOGICO MONZINO SpA
    Inventors: Mariapia Abbracchio, Ivano Eberini, Chiara Parravicini, Claudia Martini, Maria Letizia Trincavelli, Simona Daniele
  • Publication number: 20140128399
    Abstract: Methods and compositions are provided for treating a urinary tract infection (UTI). The methods involve administering to a subject in need thereof a cAMP elevator or agent that mimics cAMP, particularly a labdane diterpene such as forskolin or a derivative or analog thereof in a therapeutically effective amount to treat a UTI. The methods may further include administration of at least one cAMP elevator in combination with one or more additional active compounds from other classes of therapeutic agents, such as antimicrobial agents or cholesterol lowering drugs. Compositions of the invention include pharmaceutical compositions and kits for treating a UTI in a subject in need thereof that include therapeutically effective amounts of at least two cAMP elevators, particularly where one of the cAMP elevators is a labdane diterpene such as forskolin or a derivative or analog thereof.
    Type: Application
    Filed: December 6, 2013
    Publication date: May 8, 2014
    Applicant: DUKE UNIVERSITY
    Inventors: Soman N. Abraham, Brian L. Bishop, Matthew J. Duncan, K. Ranga Rama Krishnan, Jeongmin Song, Guojie Li, David W. Zaas
  • Publication number: 20140073624
    Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.
    Type: Application
    Filed: February 19, 2013
    Publication date: March 13, 2014
    Applicant: RIB-X PHARMACEUTICALS, INC.
    Inventor: Rib-X Pharmaceuticals, Inc.
  • Patent number: 8623901
    Abstract: The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones of formula (I), in which Hc is a tetrahydropyranyl-group and R1 is the group V?W?*, whereby V and W independently of each other may be an aryl group or an heteroaryl group, which independently of each other may optionally be substituted. According to one aspect of the invention the new compounds are for use as medicaments or for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments and/or for use in the treatment of e.g. Alzheimer's disease, in particular for cognitive impairment associated with Alzheimer's disease.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: January 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Riccardo Giovannini, Cornelia Dorner-Ciossek, Christian Eickmeier, Dennis Fiegen, Thomas Fox, Klaus Fuchs, Niklas Heine, Holger Rosenbrock, Gerhard Schaenzle
  • Patent number: 8598184
    Abstract: The present invention is directed to low molecular weight and orally bioavailable 3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the tyrosine kinase MET. The invention is also directed to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: February 28, 2009
    Date of Patent: December 3, 2013
    Assignee: Tiger Pharmatech
    Inventor: Junhu Zhang
  • Publication number: 20130310401
    Abstract: The invention relates to methods and kits for determining platelet susceptibility to activation in a patient. More particularly, the present invention relates to a method for determining platelet susceptibility to activation in a patient, comprising a step consisting of measuring the level of GPVI dimers at the platelet surface in a blood sample obtained from said patient.
    Type: Application
    Filed: December 1, 2011
    Publication date: November 21, 2013
    Applicants: UNIVERSITE PARIS DIDEROT, Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Martine Jandrot-Perrus, Laurent Feldman, Stéphane Loyau
  • Patent number: 8569295
    Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: July 28, 2010
    Date of Patent: October 29, 2013
    Assignee: Merck Patent GmbH
    Inventors: Xiaoling Chen, Srinivasa R. Karra, Bayard R. Huck, Ruoxi Lan, Amanda E. Sutton, Andreas Goutopoulos, Brian L. Hodous, Reinaldo Jones
  • Publication number: 20130245044
    Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.
    Type: Application
    Filed: May 8, 2013
    Publication date: September 19, 2013
    Applicant: Vernalis Research Limited
    Inventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
  • Patent number: 8536138
    Abstract: This disclosure relates generally to methods and pharmaceutical compositions useful in treating pulmonary hypertension. In one embodiment, for example, the disclosure provides a method for treating pulmonary hypertension comprising administering a therapeutically effective dose of a carbonic anhydrase inhibitor to a patient in need of treatment. The disclosure finds utility in the fields of medicine and pharmacology.
    Type: Grant
    Filed: December 5, 2011
    Date of Patent: September 17, 2013
    Assignee: Vivus, Inc.
    Inventors: Thomas Najarian, Peter Y. Tam, Leland F. Wilson, Craig Peterson
  • Publication number: 20130224255
    Abstract: Embodiments of the present invention include methods for the treatment, prevention, or amelioration of vascular disease in diabetic patients. The methods include both implantation of a stent including a first drug. Some embodiments include additional therapy, such as the co-administration of another drug. Some embodiments involve different stent selection for a diabetic patient compared to a non-diabetic patient.
    Type: Application
    Filed: February 23, 2012
    Publication date: August 29, 2013
    Applicant: Abbott Cardiovascular Systems Inc.
    Inventors: Syed F.A. Hossainy, Paul M. Consigny
  • Publication number: 20130210826
    Abstract: The present invention features methods and compositions for preventing, reducing, or treating a traumatic, metabolic, or toxic peripheral nerve lesion or pain including neuropathic pain, inflammatory, and nociceptive pain by administering to a mammal a compound that reduces expression or activity of BH4. This reduction may be achieved by reducing activity of a BH4 synthetic enzyme, including GTP cyclohydrolase, sepiapterin reductase, or dihydropteridine reductase; antagonizing the cofactor function of BH4 or BH4-dependent enzymes; or blocking BH4 binding to membrane bound receptors. The invention provides methods for diagnosing pain or a peripheral nerve lesion in a mammal by measuring levels of BH4 or its metabolites in biological sample or the levels or activity of any one of the BH4 synthetic enzyme in tissue samples of a mammal.
    Type: Application
    Filed: October 11, 2012
    Publication date: August 15, 2013
    Applicant: The General Hospital Corporation
    Inventor: The General Hospital Corporation
  • Patent number: 8501811
    Abstract: Provided herein are small molecule inhibitors of Taspase1 and methods of using the small molecule inhibitors of Taspase1 to treat neoplasm in subjects in need thereof.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: August 6, 2013
    Assignee: Washington University
    Inventors: James Hsieh, Emily Cheng
  • Publication number: 20130184295
    Abstract: The present invention is directed to a method of screening for a therapeutic agent useful for treating pulmonary hypertension comprising: contacting an erythrocyte with a candidate therapeutic agent; and detecting a presence or absence of erythrocyte-derived adenosine triphosphate, wherein a greater erythrocyte-derived adenosine triphosphate level indicates the candidate therapeutic agent has greater activity in treating pulmonary hypertension. Additionally, the present invention is directed to methods of treating pulmonary arterial hypertension by stimulating ATP release from erythrocytes through co-administration to a subject in need thereof an amount of a PDE5 inhibitor compound, and an amount of a prostacyclin compound.
    Type: Application
    Filed: January 10, 2013
    Publication date: July 18, 2013
    Applicant: United Therapeutics Corporation
    Inventor: United Therapeutics Corporation
  • Publication number: 20130137676
    Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: November 19, 2012
    Publication date: May 30, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8450328
    Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.
    Type: Grant
    Filed: June 25, 2009
    Date of Patent: May 28, 2013
    Assignee: Vernalis (R&D) Limited
    Inventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
  • Publication number: 20130131087
    Abstract: The present invention relates to pharmaceutical compositions and, more particularly, to a pharmaceutical composition containing the compound {1S-[1?, 2?, 3?(1S*,2R*),5?]}-3-(7-{[2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol.
    Type: Application
    Filed: December 21, 2012
    Publication date: May 23, 2013
    Applicant: AstraZeneca AB
    Inventor: Simon Banks
  • Patent number: 8440671
    Abstract: The invention relates generally to novel pharmaceutical methods for the treatment of various conditions. Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; a serotonin-norepinephrine reuptake inhibitor; a cholinesterase inhibitor; a dopamine agonist; or a medication suitable to increase the chemical concentrations of the neurotransmitters, selected from amino acids, monoamines, neuropeptides and other agents capable of primary neurotransmission in the synaptic clefts, and their use for treating a neurodegenerative disease in a subject. The invention also relates to: Compositions comprising: at least one phosphodiestersa-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; or a cholinesterase inhibitor, and their use for treating damaged skin in a subject.
    Type: Grant
    Filed: May 19, 2008
    Date of Patent: May 14, 2013
    Assignee: Vivus, Inc.
    Inventor: Jerry M. Held
  • Publication number: 20130116236
    Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: November 6, 2012
    Publication date: May 9, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130109702
    Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.
    Type: Application
    Filed: October 31, 2012
    Publication date: May 2, 2013
    Applicant: AstraZeneca AB
    Inventor: AstraZeneca AB
  • Publication number: 20130072503
    Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.
    Type: Application
    Filed: March 19, 2012
    Publication date: March 21, 2013
    Applicant: AstraZeneca
    Inventors: David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
  • Publication number: 20130045962
    Abstract: The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives. Specifically, the invention is directed to compounds of formula (I): wherein R1, R2 and R3 are defined below and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.
    Type: Application
    Filed: November 6, 2008
    Publication date: February 21, 2013
    Inventors: Donghui Qin, Beth Norton, Xiangmin Liao, Andrew Nicholson Knox, Jinhwa Lee, Yuhong Fang, Jason Christopher Dreabit, Siegfried Benjamin Christensen, IV, Andrew B. Benowitz, Kelly M. Aubart
  • Publication number: 20130040970
    Abstract: The present invention relates to novel co-crystal forms of the compound of formula (I); wherein the co-former molecule is selected from glycolic acid, salicylic acid, decanoic (capric) acid, gentisic acid (2,5-dihydroxybenzoic acid), glutaric acid, vanillic acid (4-hydroxy-3-methoxybenzoic acid), succinic acid, malonic acid or maltol (3-hydroxy-2-methyl-4-pyrone); and to processes for their preparation, to pharmaceutical compositions containing such co-crystals, to the use of such co-crystals in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a co-crystal of the compound of formula (I).
    Type: Application
    Filed: December 3, 2010
    Publication date: February 14, 2013
    Applicant: AstraZeneca AB
    Inventors: Stephen David Cosgrove, Matthew Jonathan Jones, Anna Polyakova-Akkus, Valeriya Nikolayevna Smolenskaya, Brenton Skylar Wolfe
  • Publication number: 20130028938
    Abstract: The present invention relates to a solid pharmaceutical dosage form comprising ticagrelor as pharmaceutically active ingredient, to certain particles of ticagrelor and to processes of preparing the same.
    Type: Application
    Filed: December 20, 2010
    Publication date: January 31, 2013
    Applicant: ratiopharm GmbH
    Inventors: Sandra Brueck, Dominique Meergans
  • Patent number: 8354414
    Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted heterobicyclic pyrimidines of Formula (I): wherein R1, R2, R3, R4, R5, X, W, and ring A are as defined herein; pharmaceutical compositions of substituted heterobicyclic pyrimidines of Formula (I); and their use in the treatment of chronic neurodegenerative diseases, neurotraumatic diseases, depression and/or diabetes. More particularly, the present invention relates to substituted pyrazolopyrimidines of Formula (I).
    Type: Grant
    Filed: November 4, 2010
    Date of Patent: January 15, 2013
    Assignee: Cephalon, Inc
    Inventors: Edward R. Bacon, Thomas Bailey, Nadine C. Becknell, Diane E. Gingrich, Greg A. Hostetler, Robert L. Hudkins, Keith S. Learn, Jason C. Wagner
  • Patent number: 8324188
    Abstract: A method to determine the utility of small molecules as functional replacements (mimetics) for protein receptor ligands is described. The method uses cellular biological assays on a systematic array of compounds, comprising known protein receptor ligands and other biologically active molecules to determine if a proposed small molecule is a functional equivalent of a receptor ligand, having therapeutic utility as a pharmaceutically relevant and useful agent either alone or in combination with other molecules. Furthermore, the invention provides for a method for the treatment of cancer comprising administering a combination of ET-18-O-CH3 and an anti-cancer agent.
    Type: Grant
    Filed: November 9, 2007
    Date of Patent: December 4, 2012
    Inventors: Vladimir Khazak, Lutz Weber