Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbon Atoms Patents (Class 514/277)
Spiro ring system (Class 514/278)
Polycyclo ring system having the six-membered hetero ring as one of the cyclos (Class 514/279)
Piperidines (Class 514/315)
Plural six-membered hetero rings consisting of one nitrogen and five carbon atoms (Class 514/332)
Additional hetero ring containing (Class 514/336)
Cyano bonded directly to the six-membered hetero ring (Class 514/344)
Chalcogen bonded directly to ring carbon of the six-membered hetero ring (Class 514/345)
Nitrogen attached directly to the six-membered hetero ring by nonionic bonding (Class 514/352)
C=o bonded directly to the six-membered hetero ring (Class 514/354)
Nitrogen attached indirectly to the six-membered hetero ring by nonionic bonding (Class 514/357)
The ring nitrogen of the six-membered hetero ring is pentavalent (e.g., quaternary pyridinium salt, etc.) (Class 514/358)
  • Drug Delivery Coating For Use With A Stent
    Publication number: 20120315219
    Abstract: A coated medical device and a method of providing a coating on an implantable medical device result in a medical device having a bio-absorbable coating. The coating includes a bio-absorbable carrier component. In addition to the bio-absorbable carrier component, a therapeutic agent component can also be provided. The coated medical device is implantable in a patient to effect controlled delivery of the coating, including the therapeutic agent, to the patient.
    Type: Application
    Filed: August 24, 2012
    Publication date: December 13, 2012
    Inventors: Roger Labrecque, Geoffrey Moodie, Joseph Ferraro, Lisa Rogers, Paul Martakos, Theodore Karwoski, Steve A. Herweck
  • ARYL-PYRIDINE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS
    Publication number: 20120316195
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: November 16, 2010
    Publication date: December 13, 2012
    Applicant: NOVARTIS AG
    Inventors: Martin Allan, Sylvie Chamoin, Qi-Ying Hu, Hidetomo Imase, Julien Papillon
  • Synergistic active ingredient combinations
    Patent number: 8324130
    Abstract: The novel active compound combinations comprising compounds of the formula (I) where R represents methyl or cyclopropyl, and at least one compound selected from the active compound groups (1) to (24) listed in the description have very good insecticidal and fungicidal properties.
    Type: Grant
    Filed: May 16, 2007
    Date of Patent: December 4, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Peter Jeschke, Robert Velten, Thomas Schenke, Wolfram Andersch, Heike Hungenberg, Wolfgang Thielert
  • PHENYL-PIPERAZINE DERIVATIVES AS SEROTONIN REUPTAKE INHIBITORS
    Publication number: 20120302553
    Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
    Type: Application
    Filed: February 6, 2012
    Publication date: November 29, 2012
    Applicant: H. LUNDBECK A/S
    Inventors: Thomas Ruhland, Garrick P. Smith, Benny Bang-Anderson, Ask Puschl, Ejner Knud Moltzen, Kim Andersen
  • Pyridine compound, pesticidal composition and method of controlling pests
    Patent number: 8318776
    Abstract: A pyridine compound represented by the following general formula (1); the pyridine compound in which R1 is a C1-C3 fluoroalkyl group or a C1-C3 fluoroalkoxy group; the pyridine compound in which R2 is a hydrogen atom; the pyridine compound in which R2 is a group represented by Q1; a pesticidal composition containing the pyridine compound as an active ingredient; and a method of controlling a pest including applying an effective amount of the pyridine compound to the pest or a place where the pest inhabits, are provided.
    Type: Grant
    Filed: November 18, 2008
    Date of Patent: November 27, 2012
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Hajime Mizuno
  • Substituted arylsulfonamides as antiviral agents
    Patent number: 8318761
    Abstract: The invention relates to substituted arylsulfonamides of formula (I) and methods for their preparation as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, particularly against cytomegaloviruses.
    Type: Grant
    Filed: September 3, 2008
    Date of Patent: November 27, 2012
    Assignee: Aicuris GmbH & Co. KG
    Inventors: Niels Svenstrup, Holger Zimmermann, Dagmar Karthaus, Andreas Goeller, Dirk Heimbach, Kerstin Henninger, Dieter Lang, Daniela Paulsen, Bernd Riedl, Rudolf Schohe-Loop, Joachim Schuhmacher, Tobias Wunberg
  • Substituted aryl and heteroaryl derivatives, compositions containing such compounds and methods of use
    Patent number: 8318760
    Abstract: Substituted aryl and heteroaryl derivatives are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: November 27, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John E. Stelmach, Keith G. Rosauer, Emma R. Parmee, James R. Tata
  • Fluorinated Oxa or Thia Heteroarylalkylsulfide Derivatives for Combating Invertebrate Pests
    Publication number: 20120289403
    Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.
    Type: Application
    Filed: November 11, 2010
    Publication date: November 15, 2012
    Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
  • Bone Growth Compositions and Methods
    Publication number: 20120276204
    Abstract: The present invention provides an improved technique for spinal fusion involving the administration of an HMG-CoA reductase inhibitor to a fusion. The HMG-CoA reductase inhibitor is preferably delivered to the site by a carrier. More preferably, the HMG-CoA reductase inhibitor is delivered to the site by a non-compressible delivery vehicle. The invention is suitable for promoting non-anatomic or heterotopic bone growth between any bony surfaces where bone growth is desired but does not naturally occur.
    Type: Application
    Filed: November 29, 2011
    Publication date: November 1, 2012
    Applicant: Neuropro Technologies, Inc.
    Inventors: Benjamin J. Remington, David J. Bearss, Kavian Shahi
  • Aminoisoquinoline thrombin inhibitor with improved bioavailability
    Patent number: 8299091
    Abstract: The invention relates to the compound N-(2-oxo-2-propoxyethyl)-?-phenyl-D-phenyl-alanyl-N-[(1-amino-6-iso-quinolinyl)methyl]-L-prolinamide or a pharmaceutically acceptable salt thereof, to a pharmaceutical composition comprising said compound, as well as to the use of the compound for the manufacture of a medicament for treating or for preventing thrombin mediated diseases.
    Type: Grant
    Filed: August 6, 2007
    Date of Patent: October 30, 2012
    Assignee: MSD Oss B.V.
    Inventors: Robert Gilfillan, David Jonathan Bennett
  • INDENE DERIVATIVES AS PHARMACEUTICAL AGENTS
    Publication number: 20120270901
    Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5, and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Application
    Filed: December 8, 2011
    Publication date: October 25, 2012
    Applicant: Aquinox Pharmaceuticals Inc.
    Inventors: Jeffery R. Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
  • Oil dispersions of nAChR binding neonicotinoids
    Patent number: 8293733
    Abstract: Selective insect neonicotinoids is a class of pesticide active ingredients that share some characteristics in their chemical structures and bind to the nAChR acetylcholine receptors. Formulation of such compounds in oil suspension or oil dispersion is challenging due to their electrostatic interactions of the heteroatoms in oily media, that lead to irreversible flocculation or diminished homogeneicity and bleeding of such oil dispersions. Imidacloprid, Thiamethoxam, Thiachloprid, Nitenpyram, Acetamiprid, Clothianidin and Dinetofuran and derivatives thereof with nAChR binding ability are successfully formulated in oil suspension with the use of certain copolymeric anionic fatty-acid based dispersants, sorbitan derivatives, ionic surfactants, other non-ionic surfactants and inorganic polyvalent cationic salt dispersed in the oil.
    Type: Grant
    Filed: March 4, 2010
    Date of Patent: October 23, 2012
    Assignee: GAT Microencapsulation AG
    Inventors: Victor Casaña Giner, Miguel Gimeno Sierra, Bárbara Gimeno Sierra
  • Compounds
    Patent number: 8293798
    Abstract: A compound of formula (I) or salts thereof, wherein R1, R2, R3, R4, n and X are as defined in the specification; a process for preparing such compounds, a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
    Type: Grant
    Filed: October 30, 2008
    Date of Patent: October 23, 2012
    Assignee: Glaxo Group Limited
    Inventors: Alessandra Gaiba, Susan Roomans, Martin Edward Swarbrick
  • BIOMARKERS FOR SENSITIVE DETECTION OF STATIN-INDUCED MUSCLE TOXICITY
    Publication number: 20120258123
    Abstract: The present invention inter alia provides a method, and uses thereof, of predicting statin-induced muscle toxicity or its complications, such as myalgia, myopathy and rhabdomyolysis, by detecting the lipid concentrations or lipid-lipid concentration ratios of a biological sample and comparing them to a control. This method has identified lipid markers that are more specific and sensitive in detecting these statin-induced muscle toxicity than the currently utilized clinical markers. Also provided is an antibody towards said lipids, and the use thereof for predicting, diagnosing, statin-induced muscle toxicity. The invention additionally relates to kits comprising lipids and/or an antibody thereto, for use in the prediction and/or diagnosis of statin-induced muscle toxicity.
    Type: Application
    Filed: December 21, 2011
    Publication date: October 11, 2012
    Applicant: Zora Biosciences Oy
    Inventors: Reijo Laaksonen, Kim Ekroos, Reini Hurme, Minna Jänis, Riikka Katainen, Kirill Tarasov
  • Boron dipyrromethene difluoro (BODIPY) conjugates
    Patent number: 8277775
    Abstract: The present invention relates to FTY720 analogs bearing a boron dipyrromethene difluoro (BODIPY) fluorophore in the alkyl side chain and methods of preparation. The compounds of the present invention can be used in fluorescence spectroscopy and fluorescence microscopy and in chromatography using fluorescence detection.
    Type: Grant
    Filed: August 15, 2008
    Date of Patent: October 2, 2012
    Assignee: The Research Foundation of the City University of New York
    Inventors: Robert Bittman, Zaiguo Li
  • Potassium channel inhibitors
    Patent number: 8278317
    Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: July 18, 2006
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: B. Wesley Trotter, Kausik K. Nanda, Scott E. Wolkenberg, M. Brad Nolt, David Wisnoski
  • CYCLOOXYGENASE INHIBITOR AND CALCIUM CHANNEL ANTAGONIST COMPOSITIONS AND METHODS FOR USE IN UROLOGICAL PROCEDURES
    Publication number: 20120238940
    Abstract: Compositions of a cyclooxygenase inhibitor and a calcium channel antagonist in a liquid carrier. The composition may be administered the urinary tract during urological diagnostic, interventional, surgical and other medical procedures. One disclosed composition comprises ketoprofen and nifedipine in a liquid irrigation carrier, and includes a solubilizing agent, stabilizing agents and a buffering agent.
    Type: Application
    Filed: April 24, 2012
    Publication date: September 20, 2012
    Applicant: OMEROS CORPORATION
    Inventors: Gregory A. Demopulos, Jeffrey M. Herz
  • Oxazolopyridine and isoxazolopyridine derivatives for use in the treatment of HIF-mediated conditions
    Patent number: 8269008
    Abstract: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF) by inhibiting the activity of at least one HIF hydroxylase enzyme.
    Type: Grant
    Filed: December 2, 2008
    Date of Patent: September 18, 2012
    Assignee: FibroGen, Inc.
    Inventors: Michael P. Arend, Heng Cheng, Lee A. Flippin, Danny Ng, Eric D. Turtle, Min Wu
  • Heterocyclic inhibitors of MEK and methods of use thereof
    Patent number: 8268852
    Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: January 20, 2009
    Date of Patent: September 18, 2012
    Assignee: Array BioPharma Inc.
    Inventors: James F. Blake, Joseph P. Lyssikatos, Hong-Woon Yang, Eli M. Wallace, Jeongbeob Seo
  • COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN FOR THE TREATMENT OF DIABETES
    Publication number: 20120225854
    Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: August 23, 2011
    Publication date: September 6, 2012
    Applicant: AMGEN INC.
    Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, JR., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
  • COMPOUNDS, COMPOSITIONS AND METHODS FOR THE TREATMENT OF AMYLOID DISEASES AND SYNUCLEINOPATHIES SUCH AS ALZHEIMER'S DISEASE, TYPE 2 DIABETES AND PARKINSON'S DISEASE
    Publication number: 20120225890
    Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
    Type: Application
    Filed: March 6, 2012
    Publication date: September 6, 2012
    Inventors: Alan D. Snow, Beth Nguyen, Gerardo Castillo, Virginia Sanders, Thomas Lake, Lesley Larsen, Rex T. Weavers, Stephen Lorimer, David Larsen, David L. Coffen, Charlotte Coffen
  • Isoquinoline derivatives
    Patent number: 8258149
    Abstract: The invention provides novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R7 are as described herein, compositions including the compounds and methods of preparing and using the compounds.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: September 4, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Lichun Feng, Yongguo Li, Guolong Wu
  • Composition for regenerative treatment of cartilage disease
    Patent number: 8252794
    Abstract: A composition for regenerative treatment of cartilage disease, which comprises a PDE4 inhibitor as an active ingredient, specifically a composition comprising a PDE4 inhibitor and a biocompatible and biodegradable polymer is provided, which composition, when formulated into a form suited to administer locally to affected cartilage region, such as microsphere preparation, can provide a pharmaceutical composition showing an excellent effect in regenerative treatment of cartilage.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: August 28, 2012
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Masaharu Takigawa, Naoki Sakurai, Toshiki Takagi, Noriyuki Yanaka, Yuji Horikiri, Takashi Tamura
  • Transdermal delivery system
    Patent number: 8246980
    Abstract: An improved transdermal delivery system (TDS) comprises a self-adhesive matrix comprising a solid or semi-solid semi-permeable polymer which contains an amine-functional drug in its free base form as a multitude of microreservoirs within the matrix. The self-adhesive matrix is highly permeable to the free base of the amine-functional drug and is impermeable to the protonated form of the amine-functional drug.
    Type: Grant
    Filed: July 28, 2003
    Date of Patent: August 21, 2012
    Assignee: UCB Pharma GmbH
    Inventors: Dietrich Wilhelm Schacht, Mike Hannay, Hans-Michael Wolff
  • Flavanoids and isoflavanoids for the prevention and treatment of cardiovascular diseases
    Patent number: 8242130
    Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for treatment and prevention of cardiovascular disease and related disease states, including cholesterol or lipid related disorders, such as, e.g., atherosclerosis.
    Type: Grant
    Filed: February 11, 2009
    Date of Patent: August 14, 2012
    Assignee: Resverlogix Corp.
    Inventors: Norman C. W. Wong, Joseph E. L. Tucker, Henrik C. Hansen, Fabrizio S. Chiacchia, David McCaffrey
  • Assays for S100 inhibitors
    Patent number: 8236791
    Abstract: Provided are methods of determining whether a compound is an inhibitor of an S100 protein. The methods utilize a biosensor that comprises the S100 protein that has a covalently bound fluorescent dye at an amino acid residue of the S100 protein that becomes less exposed to the aqueous solution upon activation of the S100 protein, where the fluorescent dye has decreased fluorescence when exposed to the aqueous solution than when protected from exposure to the aqueous solution. Also provided are methods of treating a subject having metastatic cancer.
    Type: Grant
    Filed: August 10, 2006
    Date of Patent: August 7, 2012
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Anne Reba Bresnick, Sarah Claire Garrett
  • Use of 1-hydroxy-2-pyridones for the treatment of seborrheic dermatitis
    Patent number: 8227490
    Abstract: Compounds of the formula (I) are disclosed and are suitable for the treatment of seborrheic dermatitis.
    Type: Grant
    Filed: July 7, 2011
    Date of Patent: July 24, 2012
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Manfred Bohn, Karl Theodor Kraemer, Astrid Markus
  • DHA esters and use thereof in treatment and prevention of cardiovascular disease
    Patent number: 8227479
    Abstract: The present invention relates to a docosahexaenoic acid ester with an alcohol chosen among the group-B vitamins or provitamins, advantageously comprised by: nicotinyl alcohol of the following formula (I), panthenol of the following formula (II), and inositol of the following formula (III) or with isosorbide of the following formula (IV) or isosorbide mononitrate of the following formula (V). It also relates to a method of preparation of same, a pharmaceutical composition comprising same and the use of same in the treatment or prevention of cardiovascular disease, in particular auricular fibrillation.
    Type: Grant
    Filed: June 13, 2011
    Date of Patent: July 24, 2012
    Assignee: Pierre Fabre Medicament
    Inventors: Frédérique Brune, André Delhon, Jean Gardette, Jean François Patoiseau, Alain Marty, Etienne Severac
  • Compositions for Reducing the Incidence of Drug Induced Arrhythmia
    Publication number: 20120178724
    Abstract: In accordance with the present invention, novel methods and formulations are provided for treating and preventing the incidence of drug-induced pro-arrhythmia, including torsades de pointes. The methods and formulations comprise a combination of a drug that induces torsade de pointes, such as Class III antiarrhythmics, certain antimicrobials, antihistamines, antidepressants, antipsychotics, diuretics, with an aspirin and/or a statin. In certain embodiments, the compositions and methods for treatment comprise azimilide and aspirin and/or a statin. These compositions may be administered by different routes, including orally. In certain embodiments where the antiarrhythmic is azimilide it may be administered orally in a dose of about 25 mg to about 300 mg.
    Type: Application
    Filed: March 22, 2012
    Publication date: July 12, 2012
    Applicant: WARNER CHILCOTT COMPANY, LLC
    Inventors: Joseph Michael Sprafka, II, Jose Mauro Goulart-Brum
  • Indene derivatives, their preparation and use as medicaments
    Patent number: 8217041
    Abstract: The present invention makes reference to new indene derivatives with general formula (I), as well as to their preparation procedures, their application as medicament and the pharmaceutical compositions containing them. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.
    Type: Grant
    Filed: November 7, 2006
    Date of Patent: July 10, 2012
    Assignee: Laboratories del Sr. Esteve, S.A.
    Inventors: Maria de las Ermitas Alcalde-Pais, Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria de les Neus Mesquida-Estevez, Sara Lopez-Perez
  • AMINE-BASED AND AMIDE-BASED INHIBITORS OF SEMICARBAZIDE-SENSITIVE AMINE OXIDASE (SSAO) ENZYME ACTIVITY AND VAP-1 MEDIATED ADHESION USEFUL FOR TREATMENT OF DISEASES
    Publication number: 20120172392
    Abstract: Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders.
    Type: Application
    Filed: March 7, 2012
    Publication date: July 5, 2012
    Inventors: LUISA M. SALTER-CID, ERIC Y. WANG, MARY T. MACDONALD, JINGJING ZHAO
  • Compositions and Methods for Selectively Activating Human Sirtuins
    Publication number: 20120172340
    Abstract: Methods for identifying selective activators of SIRT5 and/or SIRT1 and methods for using these selective activators in the modulation of SIRT5 and/or SIRT1 are provided.
    Type: Application
    Filed: October 7, 2010
    Publication date: July 5, 2012
    Applicant: BIOMOL International L.P.
    Inventors: Konrad T. Howitz, Robert E. Zipkin
  • Phosphonic acid compounds as inhibitors of serine proteases
    Patent number: 8212039
    Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: July 3, 2012
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Michael N. Greco, Harold R. Almond, Jr., Michael J. Hawkins, Eugene Powell
  • Inhibitors of IAP
    Patent number: 8207183
    Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: June 26, 2012
    Assignee: Novartis AG
    Inventors: Mark G. Palermo, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming Wang, Leigh Zawel, Yanling Zhang, Zhuoliang Chen, Yaping Wang, Fan Yang, Wojciech Wrona, Gang Liu, Mark G. Charest, Feng He
  • TREATMENT AND PREVENTION OF SECONDARY INJURY AFTER TRAUMA OR DAMAGE TO THE CENTRAL NERVOUS SYSTEM
    Publication number: 20120157420
    Abstract: A method of administering one or multiple medications to human patients with CNS injury through oral or parenteral (including transdermal, intravenous, subcutaneous, intramuscular) routes. Inflammatory and immunological processes have been shown to cause secondary damage to CNS tissues in individuals with acute CNS injury. The present invention administers one or more of the following medications, which have properties that mitigate the inflammatory and immunological processes that lead to secondary CNS damage, via trans-dermal absorption: a statin compound (e.g., a HMG-CoA reductase inhibitor), a progesterone compound, or a cholinesterase inhibiting compound, among others, either alone or in combination with other compounds.
    Type: Application
    Filed: August 31, 2010
    Publication date: June 21, 2012
    Inventor: Eric B Schneider
  • DRUG ELUTING PATCH FOR THE TREATMENT OF LOCALIZED TISSUE DISEASE OR DEFECT
    Publication number: 20120156255
    Abstract: A polymeric matrix for delivery of an HMG CoA reductase inhibitor such as a statin to tissue such as cardiac tissue in need thereof for the treatment or prevention of a disease or defect such as atrial fibrillation has been developed. In the preferred embodiment, a statin is delivered by means of a patch sutured to cardiac tissue at the time of cardiothoracic surgery. In the most preferred embodiment, the patch is a biodegradable material providing controlled or sustained release over a prolonged period of time, such as a week. Suitable materials include extracellular matrix, or other biodegradable hydrogels or polymeric materials providing sustained or controlled release of statin at the site of application.
    Type: Application
    Filed: December 16, 2011
    Publication date: June 21, 2012
    Inventors: Jaipal Singh, Nicolas Chronos
  • Aryl potassium channel blockers and uses thereof
    Patent number: 8202513
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Grant
    Filed: October 3, 2008
    Date of Patent: June 19, 2012
    Assignee: Bionomics Limited
    Inventors: Bernard Luke Flynn, Jonathan Bayldon Baell, Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Andrew John Harvey, Jorgen Alvar Mould, Dharam Paul
  • Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as phosphodiesterase inhibitors
    Patent number: 8203000
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Grant
    Filed: February 22, 2011
    Date of Patent: June 19, 2012
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Maurizio Delcanale, Elisabetta Armani, Gabriele Amari
  • TRP INHIBITORS AND USES THEREOF
    Publication number: 20120148604
    Abstract: The present invention, relates to methods including compounds, derivatives, antibodies, interfering RNA, biologies, polypeptides, dominant negative effectors, and their use in the treatment of neuropathic pain by inhibition of transient receptor potential (TRP) channels. In another embodiment, this invention relates to inhibitors, antagonists, and agonists of TRPC4. TRPC4 therapeutic agents and modulators include but are not limited to small molecule inhibitors, compounds, amino acid derivatives, polypeptides, RNA interference agents, natural chemicals, ligand derivatives, and ions. TRPC4 therapeutic agents and modulators are developed for the treatment of neuropathic pain, including but not limited to pain sensations such as nociception, hyperalgesia, allodynia, and loss of sensory function.
    Type: Application
    Filed: August 20, 2010
    Publication date: June 14, 2012
    Applicant: TRANSPOSAGEN BIOPHARMACEUTICALS, INC.
    Inventors: Eric M. Ostertag, John Stuart Crawford
  • Oxymatrine compositions and related methods for treating and preventing chronic infectious diseases
    Patent number: 8198293
    Abstract: Compositions and methods for treating chronic infectious diseases using substantially pure oxymatrine or pharmaceutically acceptable salts or esters thereof are disclosed. In one embodiment described herein, the chronic infectious disease is chronic fatigue syndrome. Further described are compositions having an anti-infective amount of substantially pure oxymatrine or pharmaceutically acceptable salts or esters thereof.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: June 12, 2012
    Inventor: John K. S. Chia
  • METHODS AND COMPOSITIONS FOR ENHANCING LIFESPAN INVOLVING SIRTUIN-MODULATING COMPOUNDS AND CHALCOGENIDES
    Publication number: 20120135091
    Abstract: The present invention concerns the use of active compounds, including chalcogenides and sirtuin-modulating compounds, either alone or in combination for increasing or enhancing survivability and/or longevity in biological matter. In general aspects, the chalcogenides and other active compounds may modulate one or more sirtuin proteins. It includes compositions, methods, articles of manufacture and apparatuses for enhancing survivability in any of these biological materials, so as to preserve and/or protect them. In specific embodiments, there are also therapeutic methods and apparatuses for aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, organ transplantation, hyperthermia, wound healing, hemorrhagic shock, cardioplegia for bypass surgery, neurodegeneration, hypothermia, and cancer using the active compounds described.
    Type: Application
    Filed: January 18, 2008
    Publication date: May 31, 2012
    Inventors: Mark B. Roth, Dana L. Miller
  • Ligand activators of the RAR receptors and pharmaceutical/cosmetic applications thereof
    Patent number: 8188106
    Abstract: Novel ligand compounds having the structural formula (I): in which: Ar is a radical selected from among the radicals of formulae (a)-(c) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine, or, alternatively into cosmetic compositions.
    Type: Grant
    Filed: July 6, 2010
    Date of Patent: May 29, 2012
    Assignee: Galderma Research & Development
    Inventors: Thibaud Biadatti, Jean-Marie Arlabosse
  • Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
    Patent number: 8188077
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: March 16, 2011
    Date of Patent: May 29, 2012
    Assignee: Abbott Laboratories
    Inventors: Hong Ding, Steven W. Elmore, Laura A. Hexamer, Aaron R. Kunzer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Michael D. Wendt
  • CADHERIN-11 INHIBITORS AND METHODS OF USE THEREOF
    Publication number: 20120128693
    Abstract: Cadherin-11 inhibitors and methods for the prevention and treatment of cadherin-11 related diseases are described herein. Cadherin-11 related diseases include cancer and rheumatoid arthritis.
    Type: Application
    Filed: February 9, 2010
    Publication date: May 24, 2012
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Stephen W. Byers, Sivanesan Dakshanamurthy, Jaime M. Guidry Auvil, Milton L. Brown
  • Novel C-4 Substituted Retinoids
    Publication number: 20120122908
    Abstract: C-4 substituted retinoic acid analogs, synthesis methods of C-4 substituted retinoic acid analogs and methods of using C-4 substituted retinoic acid analogs to treat various cancers and dermatological diseases and conditions. The C-4 substituted retinoic acid analogs include C-4 all-trans retinoic acid (ATRA) and 13-cis retinoic acid (13-CRA) analogs. The C-4 substituted retinoic acid analogs inhibit all-trans retinoic acid (ATRA) 4-hydroxylase activity, thereby inhibiting the catabolism of ATRA. The C-4 substituted retinoic acid analogs also have ATRA-mimetic activity. The preferred substitutions at C-4 are an azole group, a sulfur, oxygen, or nitrogen containing group, a pyridyl group, an ethinyl group, a cyclopropyl-amine group, an ester group, or a cyano group, or forms, together with the C-4 carbon atom, an oxime, an oxirane or aziridine group.
    Type: Application
    Filed: July 25, 2007
    Publication date: May 17, 2012
    Applicant: University of Maryland
    Inventors: Vincent C.O. Njar, Angela M.H. Brodie, Ivo P. Nnane
  • Pharmaceutical composition comprising phenylamidine derivative and method of using the pharmaceutical composition in combination with antifungal agent
    Patent number: 8173157
    Abstract: A pharmaceutical composition comprising a phenylamidine derivative or a salt thereof, represented by a general formula, wherein R1 and R2 may be same or different, and represent an optionally substituted C3-4alkyl group; and one or more agents selected from azole antifungal agents, polyene antifungal agents, candin antifungal agents and fluoropyrimidine antifungal agents, and a method for combination use of the phenylamidine derivative or a salt thereof and the agents are useful for treating fungal infections caused by a fungal pathogen.
    Type: Grant
    Filed: October 3, 2007
    Date of Patent: May 8, 2012
    Assignee: Toyama Chemical Co., Ltd.
    Inventor: Hiroshi Nishikawa
  • Kappa opioid receptor ligands
    Patent number: 8173678
    Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.
    Type: Grant
    Filed: October 25, 2010
    Date of Patent: May 8, 2012
    Assignee: Research Triangle Institute
    Inventors: Frank Ivy Carroll, Hernan A. Navarro, Lawrence E. Brieaddy, Scott P. Runyon, James B. Thomas
  • 6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling
    Patent number: 8173689
    Abstract: Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.
    Type: Grant
    Filed: May 8, 2009
    Date of Patent: May 8, 2012
    Assignee: Novartis AG
    Inventors: James C. Sutton, Marion Wiesmann
  • OSTEOCONDUCTIVE MATRICES COMPRISING CALCIUM PHOSPHATE PARTICLES AND STATINS AND METHODS OF USING THE SAME
    Publication number: 20120107383
    Abstract: Osteoconductive matrices and methods are provided that have one or more statins disposed in calcium phosphate particles. The matrices may be injected into a fracture site. The osteoconductive matrices provided allow for sustained release of the statin and facilitate bone formation and repair of the fracture site.
    Type: Application
    Filed: October 27, 2010
    Publication date: May 3, 2012
    Applicant: WARSAW ORTHOPEDIC, INC.
    Inventor: William F. McKay
  • ?- and ?-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
    Patent number: RE43596
    Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: April 23, 2007
    Date of Patent: August 21, 2012
    Assignee: G.D. Searle LLC
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw