Chalcogen Bonded Directly To Pyrimidine At 2-position Patents (Class 514/274)
  • Combination Therapy With Organic Arsenicals
    Publication number: 20130261082
    Abstract: The invention provides a combination therapy wherein one or more other therapeutic agents are administered with an organic arsenical, preferably SGLU-I or a pharmaceutically acceptable salt thereof. The invention also relates to methods for the treatment of cancer, comprising administering SGLU-I in combination with another therapeutic agent. Another aspect of the invention relates to a kit comprising SGLU-I and another therapeutic agent.
    Type: Application
    Filed: March 6, 2013
    Publication date: October 3, 2013
    Applicant: ZIOPHARM ONCOLOGY, INC.
    Inventors: Barbara WALLNER, Philip B. KOMARNITSKY
  • Pyrrolopyridines as kinase inhibitors
    Patent number: 8545897
    Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Grant
    Filed: March 20, 2012
    Date of Patent: October 1, 2013
    Assignee: Array BioPharma Inc.
    Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunwardana, Pete Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
  • Amino-tetrazoles analogues and methods of use
    Patent number: 8546374
    Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: October 1, 2013
    Assignee: Abbvie Inc.
    Inventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biquin C. Li
  • PYRAZOLOPYRIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
    Publication number: 20130252941
    Abstract: The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy.
    Type: Application
    Filed: May 16, 2013
    Publication date: September 26, 2013
    Applicant: F. Hoffmann-La Roche AG
    Inventors: Toby Blench, Simon Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven Magnuson, Vickie Tsui, Karen Williams, Birong Zhang
  • BICYCLIC OXAZOLE LACTAMS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
    Publication number: 20130252943
    Abstract: In one aspect, the invention relates to substituted bicyclic oxazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. 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: February 27, 2013
    Publication date: September 26, 2013
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Gregor James Macdonald, Susana Conde-Ceide, María Luz Martín-Martín
  • PYRIMIDINONE COMPOUNDS FOR USE IN THE TREATMENT OF DISEASE OR CONDITIONS MEDIATED BY LP-PLA2
    Publication number: 20130252963
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, or example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Application
    Filed: December 5, 2011
    Publication date: September 26, 2013
    Inventors: Yun Jin, Zehong Wan, Qing Zhang
  • SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS
    Publication number: 20130252984
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: March 12, 2013
    Publication date: September 26, 2013
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing YUAN, Richard L. BEARD, Xiaoxia LIU, John E. DONELLO, Veena VISWANATH, Michael E. GARST
  • PAIN RELIEF COMPOSITIONS, MANUFACTURE AND USES
    Publication number: 20130252925
    Abstract: The present invention relates to TRPV1 selective agonist topical compositions including capsaicinoid and analgesic agent compositions and methods of manufacture and methods of providing pain relief as well as treating a variety of disorders with such compositions.
    Type: Application
    Filed: March 12, 2013
    Publication date: September 26, 2013
    Applicant: API Genesis, LLC
    Inventors: Daniel Bucks, Philip J. Birbara
  • NEW INDANYLOXYDIHYDROBENZOFURANYLACETIC ACIDS
    Publication number: 20130252937
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 26, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
  • CANCER CELL TARGETING USING NANOPARTICLES
    Publication number: 20130251766
    Abstract: The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.
    Type: Application
    Filed: May 10, 2013
    Publication date: September 26, 2013
    Applicant: Bind Therapeutics, Inc.
    Inventors: Stephen E. Zale, Mir Mukkaram Ali
  • Compounds And Methods For Treating Candidiasis And Aspergillus Infections
    Publication number: 20130252964
    Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for killing or inhibiting the growth of a Candida or Aspergillus species or preventing or treating a mammal having candidiasis (oral and/or disseminated) or an Aspergillus infection.
    Type: Application
    Filed: January 18, 2013
    Publication date: September 26, 2013
    Applicant: PolyMedix, Inc.
    Inventors: Richard W. Scott, Katie Freeman, Haizhong Tang, Gill Diamond
  • Flavoring Systems for Pharmaceutical Compositions and Methods of Making Such Compositions
    Publication number: 20130252985
    Abstract: A flavoring system for a liquid pharmaceutical composition and pharmaceutical compositions containing such flavoring systems are disclosed. Flavoring systems of the invention include at least one sweetening agent, at least two flavored ingredients, and at least one flavor modifier selected from the group consisting of citric acid, sodium citrate, sodium chloride, and mixtures thereof. At least two of the flavored ingredients are selected from the group consisting of a vanilla flavored ingredient, a peppermint flavored ingredient, a menthol flavored ingredient, a cotton candy flavored ingredient, and mixtures thereof. The one or more sweetening agents comprise glycerin, monoammonium glycyrrhizinate, saccharin sodium, acesulfame potassium, high fructose corn syrup, and/or mixtures thereof.
    Type: Application
    Filed: May 10, 2013
    Publication date: September 26, 2013
    Inventors: Laman Alani, Donald P. Gauwitz, Dilip Kaul, John M. Lipari, Soumojeet Ghosh, Kennan C. Marsh
  • COMPOUNDS
    Publication number: 20130252986
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease and/or diabetic macular edema.
    Type: Application
    Filed: December 5, 2011
    Publication date: September 26, 2013
    Inventors: Zehong Wan, Xiaomin Zhang, Jian Wang, Cheng Peng, Yun Jin, Yimin Hu
  • SERINE/THREONINE KINASE INHIBITORS
    Publication number: 20130252934
    Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Application
    Filed: March 1, 2013
    Publication date: September 26, 2013
    Applicants: Genentech, Inc., Array BioPharma Inc.
    Inventors: James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
  • METHOD AND COMPOSITIONS FOR THE TREATMENT AND DETECTION OF ENDOTHELIN-1 RELATED KIDNEY DISEASES
    Publication number: 20130252898
    Abstract: The present application relates to methods of treating HIV-associated nephropathy (HIVAN) and/or focal segmental glomerulosclerosis (FSGS) using endothelin-1 (ET-1) antagonists. The application further relates to a composition for the treatment of HIVAN and/or FSGS. A kit for detecting the presence of ET-1 or ET-1-associated biomarker in a biological sample is also disclosed.
    Type: Application
    Filed: May 30, 2013
    Publication date: September 26, 2013
    Applicant: Morehouse School Of Medicine
    Inventors: Gale W. Newman, Barbara A. Jacob-Mungin, Chamberlain Obialo
  • Combination comprising macitentan and paclitaxel for treating multi-drug resistant ovarian cancer
    Patent number: 8541433
    Abstract: The invention relates to the combination of an endothelin receptor antagonist of formula (I) with paclitaxel, and in particular to this combination for therapeutic use, simultaneously, separately or over a period of time, in the treatment of ovarian cancer.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: September 24, 2013
    Assignee: Actelion Pharmaceuticals, Ltd.
    Inventors: Martine Clozel, Urs Regenass
  • MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
    Publication number: 20130245010
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: April 26, 2013
    Publication date: September 19, 2013
    Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
  • CYCLIC UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1
    Publication number: 20130245051
    Abstract: This invention relates to novel compounds of the Formula (I), (Ia) and (Ib), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, j which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell Or the inhibition of the conversion of cortisone to Cortisol in a cell.
    Type: Application
    Filed: April 30, 2013
    Publication date: September 19, 2013
    Applicant: VITAE PHARMACEUTICALS, INC.
    Inventors: David A. Claremon, Linghang Zhuang, Colin M. Tice, Yuanjie Ye, Wei He, Suresh B. Singh, Zhenrong Xu, Salvacion Cacatian, Wei Zhao
  • NOVEL HIV-1 REVERSE TRANSCRIPTASE CODON DELETION AND ITS USE IN THE MANAGEMENT AND TREATMENT OF HIV INFECTIONS
    Publication number: 20130244964
    Abstract: The present invention provides an isolated HIV-1 mutant and isolated nucleic acid molecules comprising HIV-RT coding sequences harboring a novel mutation in the S68 codon, and in particular, deletions of the S68 codon. This novel deletion reduces the sensitivity of HIV to various nucleoside reverse transcriptase inhibitors. Methods of using this mutation for selecting effective antiretroviral agents in vitro and in vivo, methods for monitoring infection progression in HIV-infected individuals and methods for avoiding the emergence of and/or to treat individuals infected with HIV comprising mutations, including deletions, at the S68 codon of HIV-RT are provided.
    Type: Application
    Filed: November 9, 2012
    Publication date: September 19, 2013
    Applicant: EMORY UNIVERSITY
    Inventor: Raymond F. Schinazi
  • BIORESORABLE DRUG DELIVERY MATRICES BASED ON CROSS-LINKED POLYSACCHARIDES, DOSAGE FORMS DESIGNED FOR DELAYED/CONTROLLED RELEASE
    Publication number: 20130245549
    Abstract: Bioactive agents are embedded in a cross-linked dextran and coated with a bioresorbable polymer. When implanted in a mammal, the coated cross-linked dextran composition produces controlled release of the embedded bioactive agent.
    Type: Application
    Filed: September 12, 2012
    Publication date: September 19, 2013
    Applicant: ROYER BIOMEDICAL, INC.
    Inventors: Garfield P. ROYER, Tatiana Bizikova
  • HETEROCYCLIC COMPOUNDS AND METHODS OF USE
    Publication number: 20130243754
    Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.
    Type: Application
    Filed: December 20, 2012
    Publication date: September 19, 2013
    Applicant: TARGEGEN, INC.
    Inventors: Wolfgang WRASIDLO, Elena DNEPROVSKAIA
  • Dosing regimens for treatment of proliferative disorders comprising administration of sapacitabine
    Patent number: 8536188
    Abstract: One aspect of the present invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating a proliferative disorder, wherein the sapacitabine or metabolite thereof is administered in a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine or metabolite thereof for about 2 to about 6 days per week, for 2 weeks out of 3 weeks. Another aspect of the invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating cutaneous T-cell lymphoma (CTCL).
    Type: Grant
    Filed: April 24, 2008
    Date of Patent: September 17, 2013
    Assignee: Cyclacel Limited
    Inventor: Judy H. Chiao
  • Piperidine derivatives as modulators of chemokine receptor activity
    Patent number: 8536198
    Abstract: The present application describes modulators of MIP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.
    Type: Grant
    Filed: July 23, 2008
    Date of Patent: September 17, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joseph B. Santella, John Hynes, Daniel S. Gardner
  • NOVEL COMPOUNDS THAT ARE ERK INHIBITORS
    Publication number: 20130237518
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).
    Type: Application
    Filed: October 24, 2011
    Publication date: September 12, 2013
    Inventors: Sobhana Babu Boga, Joseph M. Kelly, Hugh Y. Zhu, Abdul-Basit Alhassan, Xin Yao, Xiaolei Gao, James J-S Wang, Jagdish A. Desai, Subrahmanyam Gudipati, Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, JR.
  • SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS
    Publication number: 20130237552
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: April 29, 2013
    Publication date: September 12, 2013
    Applicant: ALLERGAN, INC.
    Inventors: HAIQING YUAN, RICHARD L. BEARD, MICHAEL E. GARST, JOHN E. DONELLO, XIAOXIA LIU, VEENA VISWANATH
  • Pharmaceutical compounds
    Patent number: 8530444
    Abstract: Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice, for example, in treatment of cancer and immune disorders.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: September 10, 2013
    Assignee: Aposense Ltd.
    Inventors: Ilan Ziv, Hagit Grimberg
  • Uracil compound or salt thereof having human deoxyuridine triphosphatase inhibitory activity
    Patent number: 8530490
    Abstract: Provided is a uracil compound or a salt thereof, which has potent human dUTPase inhibitory activity and is useful as, for example, an antitumor drug. A uracil compound represented by the general formula (I) or a salt thereof: wherein n represents an integer of 1 to 3; X represents a bond, an oxygen atom, a sulfur atom, or the like; Y represents a linear or branched alkylene group having 1 to 8 carbon atoms, or the like; and Z represents —SO2NR1R2 or —NR3SO2—R4, wherein R1 and R2 each represent an alkyl group having 1 to 6 carbon atoms, an aralkyl group which is optionally substituted, or the like; R3 represents an alkyl group having 1 to 6 carbon atoms, or the like; and R4 represents an aromatic hydrocarbon group, an unsaturated heterocyclic group, or the like.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: September 10, 2013
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Masayoshi Fukuoka, Tatsushi Yokogawa, Seiji Miyahara, Hitoshi Miyakoshi, Wakako Yano, Junko Taguchi, Yayoi Takao
  • Purified Crocetin Compound And Method For Treating, Inhibiting, And/Or Prophylaxis of Cancer, Such As Pancreatic Cancer
    Publication number: 20130231300
    Abstract: A fraction separated from crude crocetin by preparative HPLC, and identified using LC/MS and NMR as crocetinic acid, markedly regressed the proliferation and increased apoptosis in pancreatic cancer cells. Purified crocetinic acid showed more potency than 15 commercial or crude crocetin using proliferation and apoptosis as markers. Purified crocetinic acid also showed significant anti-tumorigenic activity against pancreatic cancer cells in a mouse model of pancreatic cancer. Given crocetinic acid's low toxicity, crocetinic acid could be used as a chemotherapeutic or chemopreventative agent for pancreatic cancer.
    Type: Application
    Filed: October 7, 2011
    Publication date: September 5, 2013
    Applicant: U.S. Department of Veterans Affairs
    Inventors: Animesh Dhar, William G. Gutheil
  • Amido derivatives and their use as positive allosteric modulators of metabotropic glutamate receptors
    Patent number: 8524726
    Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: September 3, 2013
    Assignee: Addex Pharma S.A.
    Inventor: Christelle Bolea
  • COMPOSITIONS AND METHODS FOR COATING MEDICAL IMPLANTS
    Publication number: 20130224276
    Abstract: Medical implants are provided which release an anthracycline, fluoropyrimidine, folic acid antagonist, podophylotoxin, camptothecin, hydroxyurea, and/or platinum complex, thereby inhibiting or reducing the incidence of infection associated with the implant.
    Type: Application
    Filed: March 18, 2013
    Publication date: August 29, 2013
    Applicant: ANGIOTECH INTERNATIONAL AG
    Inventor: ANGIOTECH INTERNATIONAL AG
  • PYRAZOLOQUINOLINE COMPOUND
    Publication number: 20130225553
    Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.
    Type: Application
    Filed: March 7, 2013
    Publication date: August 29, 2013
    Applicant: ASTELLAS PHARMA INC.
    Inventor: ASTELLAS PHARMA INC.
  • SUBSTITUTED BENZAZOLES AND METHODS OF THEIR USE AS INHIBITORS OF RAF KINASE
    Publication number: 20130224195
    Abstract: New substituted benzazole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Application
    Filed: April 3, 2013
    Publication date: August 29, 2013
    Inventors: Abran Costales, Teresa Hansen, Barry H. Levine, Christopher McBride, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Cynthia M. Shafer, Sharadha Subramanian, Joelle Verhagen
  • NOSCAPINE ANALOGS AND THEIR USE IN TREATING CANCERS
    Publication number: 20130224310
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are noscapine analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers. While the antitussive plant alkaloid, noscapine, binds tubulin, displays anticancer activity, and has a safe pharmacological profile in humans, structure-function analyses pointed to a proton at position 9 of the isoquinoline ring that can be modified without compromising tubulin binding activity. Noscapine analogs with various functional moieties at position 9 on the isoquinoline ring kill human cancer cells resistant to other anti-microtubule agents, such as vincas and taxanes.
    Type: Application
    Filed: June 5, 2012
    Publication date: August 29, 2013
    Applicant: Emory University
    Inventors: Harish C. Joshi, Ritu Aneja, Surya N. Vangapandu
  • Spiro[2.4]heptanes for Treatment of Flaviviridae Infections
    Publication number: 20130224152
    Abstract: Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an effective amount of a spiro[2.4]heptane as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier, are provided. The spiro[2.4]heptane compounds either possess antiviral activity, or are metabolized to a compound that exhibits such activity.
    Type: Application
    Filed: February 14, 2013
    Publication date: August 29, 2013
    Applicant: UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.
    Inventor: UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.
  • SILICON NANOCARRIER FOR DELIVERY OF DRUG, PESTICIDES AND HERBICIDES , AND FOR WASTE WATER TREATMENT
    Publication number: 20130225412
    Abstract: The various embodiments herein provide a nano silicon carrier as a drug delivery mechanism. The nano silicon carrier comprises a diatom frustules loaded with a drug molecule to be released at the target site. The diatom frustules are of Hannaea arcus and Navicula inflexa species of diatom. The pore size of the diatom frustules is 1 to 100 nm. The diatom frustules are comb-like in structure. The diatom frustules are in the form of powdered diatomaceous earth. The drug delivery mechanism described in the embodiments herein is a controlled release mechanism. The nano silicon carrier described in the embodiments herein is also used for delivery of pesticides and herbicides in plants. The nano silicon carrier described in the embodiments herein is also used in hormone waste water treatment.
    Type: Application
    Filed: February 28, 2012
    Publication date: August 29, 2013
    Inventors: Soroush Sardari Lodriche, Saeed Soltani, Roghieh Mirzazadeh
  • METHOD FOR TREATING A PULMONARY HYPERTENSION CONDITION WITHOUT COMPANION DIAGNOSIS
    Publication number: 20130225607
    Abstract: There is provided a method for treating pulmonary hypertension in a subject, comprising: administering to the subject in need thereof a daily dose of ambrisentan from 1 mg to about 15 mg, wherein the method is carried out without drug labeling instruction to monitor liver aminotransferase levels during ambrisentan treatment.
    Type: Application
    Filed: August 9, 2012
    Publication date: August 29, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Hunter Campbell Gillies, Tobias Peschel, David J. Pizzuti
  • METHOD AND COMPOSITION FOR TREATING ALZHEIMER'S DISEASE AND DEMENTIAS OF VASCULAR ORIGIN
    Publication number: 20130225531
    Abstract: A composition and method of treating Alzheimer's disease or a dementia of vascular origin are disclosed. The composition and method utilize an endothelin antagonist as the active agent to treat Alzheimer's disease or a dementia of vascular origin in mammals, including humans.
    Type: Application
    Filed: December 19, 2012
    Publication date: August 29, 2013
    Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventor: The Board Of Trustees Of The University of Illinois
  • METHOD FOR TREATING PULMONARY ARTERIAL HYPERTENSION IN A PATIENT NOT HAVING IDIOPATHIC PULMONARY FIBROSIS
    Publication number: 20130225595
    Abstract: There is provided a method of treating pulmonary hypertension in a patient in need thereof, said method comprising: administering a therapeutically effective amount of ambrisentan to the patient with pulmonary arterial hypertension, wherein the patient has been determined not to have idiopathic pulmonary fibrosis.
    Type: Application
    Filed: March 14, 2013
    Publication date: August 29, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • METHOD FOR TREATING A PULMONARY HYPERTENSION CONDITION WITHOUT COMPANION DIAGNOSIS
    Publication number: 20130224306
    Abstract: There is provided a method for treating pulmonary hypertension in a subject, comprising: administering to the subject in need thereof a daily dose of ambrisentan from 1 mg to about 15 mg, wherein the method is carried out without drug labeling instruction to monitor liver aminotransferase levels during ambrisentan treatment.
    Type: Application
    Filed: June 28, 2012
    Publication date: August 29, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Hunter Campbell Gillies, Tobias Peschel, David J. Pizzuti
  • Chemical Compounds
    Publication number: 20130225524
    Abstract: The invention is directed to substituted quinoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, R4, and R5 are defined herein. The compounds of the invention are inhibitors of lactate dehydrogenase A and can be useful in the treatment of cancer and diseases associated with tumor cell metabolism, such as cancer, and more specifically cancers of the breast, colon, prostate and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting lactate dehydrogenase A activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: November 3, 2011
    Publication date: August 29, 2013
    Inventors: Deping Chai, Mariela Colon, Christopher Dodson, Kevin J. Duffy, Antony Nicholas Shaw
  • OXAZOLE AND THIAZOLE COMPOUNDS AS KSP INHIBITORS
    Publication number: 20130224186
    Abstract: Disclosed are new substituted oxazole and thiazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:
    Type: Application
    Filed: April 13, 2011
    Publication date: August 29, 2013
    Inventors: Paul A. Barsanti, Yu Ding, Wooseok Han
  • SUBSTITUTED HETEROCYCLIC COMPOUNDS FOR DISEASE TREATMENT
    Publication number: 20130225619
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: January 18, 2013
    Publication date: August 29, 2013
    Applicant: Acucela Inc.
    Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
  • PROCESS FOR PREPARING ANTIVIRAL COMPOUNDS
    Publication number: 20130224149
    Abstract: This disclosure is directed to: (a) processes for preparing compounds and salts thereof that, inter alia, are useful for inhibiting hepatitis C virus (HCV); (b) intermediates useful for the preparation of the compounds and salts; (c) pharmaceutical compositions comprising the compounds or salts; and (d) methods of use of such compositions.
    Type: Application
    Filed: August 21, 2012
    Publication date: August 29, 2013
    Applicant: ABBVIE INC.
    Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
  • Heterocyclic derivatives as M-GLU5 antagonists
    Patent number: 8518916
    Abstract: This invention relates to novel heterocyclic compounds having selective affinity for the mGlu5 subtype of metabotropic receptors, pharmaceutical compositions thereof and uses for such compounds and compositions in the treatment of lower urinary tract disorders, such as neuromuscular dysfunction of the lower urinary tract, and in the treatment of migraine and gastroesophagael reflux disease (GERD).
    Type: Grant
    Filed: August 4, 2008
    Date of Patent: August 27, 2013
    Assignee: Recordati Ireland Limited
    Inventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Elena Poggesi, Davide Graziani, Matteo Longhi
  • IMIDAZOPYRIDINE DERIVATIVES AS JAK INHIBITORS
    Publication number: 20130216498
    Abstract: New imidazopyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
    Type: Application
    Filed: December 23, 2010
    Publication date: August 22, 2013
    Inventors: Paul Robert Eastwood, Jacob Gonzales Rodriguez, Jordi Bach Taña, Lluis Miquel Pages Santacana, Joan Taltavull Moll, Juan Francisco Caturla Javaloyes, Victor Giulio Matassa
  • NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
    Publication number: 20130217664
    Abstract: Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. Wherein R1, L1, R3, R4, Cy, L2 and R5 are as defined herein.
    Type: Application
    Filed: February 7, 2013
    Publication date: August 22, 2013
    Inventors: Christel Jeanne Marie MENET, Benoit Antoine SCHMITT, Raphael Jean Joel GENEY, Kevin James DOYLE, Joanne PEACH, Nicholas John PALMER, Graham Peter JONES, David HARDY, James Edward Stewart DUFFY
  • Compounds and Compositions for the Treatment of Cancer
    Publication number: 20130217645
    Abstract: New uses for phenylketone carboxylate compounds and substituted aromatic compounds of Formula I, Formula I.1, Formula I.2, Formula IA, Formula IB, Formula IC and Formula II and their pharmaceutical acceptable salts for the treatment of cancer. The use of a combination of two of these compounds is described and the use of the combination of one of these compounds with an anticancer agent such as decarbazine, doxorubicin, daunorubicin, cyclophosphamide, busulfex, busulfan, vinblastine, vincristine, bleomycin, etoposide, topotecan, irinotecan, taxotere, taxol, 5-fluorouracil, methotrexate, gemcitabine, cisplatin, carboplatin and chlorambucil.
    Type: Application
    Filed: October 26, 2011
    Publication date: August 22, 2013
    Applicant: PROMETIC BIOSCIENCES INC.
    Inventors: Lyne Gagnon, Brigitte Grouix, Lilianne Geerts, Pierre Laurin, Christopher Penney, Boulos Zacharie
  • Substituted spirocyclic piperidine derivatives as histamine-3 (H3) receptor ligands
    Patent number: 8513232
    Abstract: The present invention provides compounds of Formula (I): their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceuticals compositions thereof.
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: August 20, 2013
    Assignees: Cephalon, Inc., Pharmacopeia, LLC
    Inventors: Edward R. Bacon, Nadine C. Becknell, Reddeppa reddy Dandu, Lisa Guise-Zawacki, Tao Guo, Chia-yu Huang, Robert L. Hudkins, Babu G. Sundar, Ming Tao, Minglang Wu, Allison L. Zulli
  • Pyrazole derivatives and their use as positive allosteric modulators of metabotropic glutamate receptors
    Patent number: 8513252
    Abstract: The present invention relates to novel compounds of Formula (I), wherein M, P, X1, X2, (A)m and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
    Type: Grant
    Filed: July 14, 2010
    Date of Patent: August 20, 2013
    Assignee: Addex Pharma S.A.
    Inventor: Christelle Boléa
  • Pyridone GPR119 G protein-coupled receptor agonists
    Patent number: 8513424
    Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.
    Type: Grant
    Filed: June 12, 2012
    Date of Patent: August 20, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Dean A. Wacker, Karen A. Rossi, Ying Wang