Additional Hetero Ring Which Is Not Part Of The Bicyclo Ring System Patents (Class 514/414)
  • Patent number: 8759303
    Abstract: This invention generally relates to compositions and methods for treating myelodysplastic syndrome. In one embodiment, this invention relates to methods for treating myelodysplastic syndrome with ezatiostat or a salt thereof and lenalidomide.
    Type: Grant
    Filed: May 16, 2011
    Date of Patent: June 24, 2014
    Assignee: Telik, Inc.
    Inventors: Gail L. Brown, Lixin Meng
  • Patent number: 8759539
    Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
  • Publication number: 20140165223
    Abstract: Described are methods and compositions for inhibiting the trimerization of ligands belonging to the TNF superfamily, in particular, inhibiting RANKL trimerization. Accordingly, the methods and compositions provided herein can be used to treat disorders associated with increased RANK signaling, in particular those related to bone loss. Compounds that inhibit trimerization of ligands belonging to the TNF superfamily are also described.
    Type: Application
    Filed: February 12, 2014
    Publication date: June 12, 2014
    Applicant: B.S.R.C. "Alexander Fleming"
    Inventors: Eleni Ntouni, Georgios Kollias
  • Patent number: 8748475
    Abstract: The invention relates to compositions and methods for treating lupus. The methods typically comprise the step of administrating one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, such as, Meisoindigo and NATURA in an amount sufficient to treat the lupus; preferably by modulating cytokine expression. Preferably the compound is in an amount less than sufficient to substantially inhibit cyclin dependent kinases.
    Type: Grant
    Filed: August 3, 2011
    Date of Patent: June 10, 2014
    Assignee: Natrogen Therapeutics International, Inc.
    Inventors: Longgui Wang, Simon K. Mencher
  • Patent number: 8747837
    Abstract: Embodiments of the invention are directed methods that include a thymidine kinase deficient vaccinia virus. The methods include evaluating a tumor for reperfusion after treatment with vaccinia virus and administering an anti-angiogenic agent if reperfusion is detected.
    Type: Grant
    Filed: September 14, 2010
    Date of Patent: June 10, 2014
    Assignee: Jennerex, Inc.
    Inventors: David Kirn, Caroline Breitbach
  • Patent number: 8748428
    Abstract: The present invention demonstrates that chronic active BCR signaling through CD79A/B confers a strong dependence on downstream PKCb kinase signaling. Hence, provided herein is a method for inhibiting the growth of B-cell lymphoma having chronic active B-cell-receptor signaling, or inhibiting the growth of cancers with molecular lesions that lead to chronic active BCR signaling, by administering to a patient in need of such treatment a therapeutically effective amount of a PKC inhibitor or a use of a PKC inhibitor to inhibit the growth of B-cell lymphoma having chronic active B-cell-receptor signaling or to inhibit the growth of cancers with molecular lesions that lead to chronic active BCR signaling.
    Type: Grant
    Filed: March 28, 2011
    Date of Patent: June 10, 2014
    Assignee: Novartis AG
    Inventors: Walter Schuler, Frank P. Stegmeier, Markus Warmuth
  • Publication number: 20140155413
    Abstract: The present invention is directed to compounds of formula I and 1a: which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Application
    Filed: July 6, 2012
    Publication date: June 5, 2014
    Inventors: Barbara Hanney, Peter Manley, Michael T. Rudd, John M. Sanders, Shawn J. Stachel, Darrell Henze
  • Publication number: 20140155369
    Abstract: An agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that activates a serotonin 5-HT2C receptor, an agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that stimulates an androgen binding site, and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence, which includes electrostimulating the abdominal muscles or a nerve controlling them of an animal to increase the abdominal pressure, and measuring the leak point pressure at that time.
    Type: Application
    Filed: January 16, 2014
    Publication date: June 5, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Izumi KAMO, Tadatoshi HASHIMOTO
  • Patent number: 8741928
    Abstract: Provided are protected antimicrobial compounds which are useful for controlling microorganisms in aqueous or water-containing systems, such as oil or gas field fluids, at elevated temperature. The antimicrobial compounds are of the formula I: wherein R, R1, R2, X and Y are as defined herein.
    Type: Grant
    Filed: December 2, 2011
    Date of Patent: June 3, 2014
    Assignees: Dow Global Technologies LLC, ANGUS Chemical Company
    Inventors: Charles E. Coburn, Michael V. Enzien, Heather R. Mcginley, David W. Moore
  • Patent number: 8741905
    Abstract: The invention relates to a compound of Formula I:
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: June 3, 2014
    Assignees: The Broad Institute, Inc., President and Fellows of Harvard College
    Inventors: Bridget Wagner, Jeremy Duvall, Danny Hung-Chieh Chou
  • Patent number: 8741945
    Abstract: The present invention pertains generally to certain compounds of the deoxyactagardine A and B type. Such compounds are suitable for use in the treatment of microbial infections, for example Clostridium infection, such as C. perfringens, C. difficile, C. tetani, and/or C. botulinum, in particular C. difficile, especially infection of the colon and/or lower intestines and diarrhea associated with the microbial infection.
    Type: Grant
    Filed: May 21, 2012
    Date of Patent: June 3, 2014
    Assignee: Novacta Biosystems Limited
    Inventor: Sjoerd Nicolaas Wadman
  • Patent number: 8735441
    Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
    Type: Grant
    Filed: October 5, 2012
    Date of Patent: May 27, 2014
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Kevin D. Shenk, Francesco Parlati, Han-jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
  • Publication number: 20140140931
    Abstract: This invention relates to antioxidant, neuroprotective and antineoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer. Methods of synthesizing the antioxidant derivatives of camptothecin and anti-oxidant derivatives of camptothecin analogs, NSAIDs and statins, spontaneous emulsification or nanoprecipitation thereof to produce antioxidant, neuroprotective and anti-neoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer and their use in treating cancerous diseases are also provided. A further aspect of this invention is the use of these neuroprotective and anti-neoplastic nanoparticles for the preparation of delivery devices of other pharmaceuticals and/or drugs.
    Type: Application
    Filed: July 27, 2012
    Publication date: May 22, 2014
    Applicant: CEDARS-SINAI MEDICAL CENTER
    Inventors: John S. Yu, Bong Seop Lee
  • Publication number: 20140142072
    Abstract: Provided is a composition for use in treating a skin condition, the composition comprising: (a) a first component comprising a substituted or unsubstituted diindolylmethane compound; and (b) a second component comprising a substituted or unsubstituted retinoid compound.
    Type: Application
    Filed: March 21, 2012
    Publication date: May 22, 2014
    Applicant: IIAA LIMITED
    Inventor: David Alpert
  • Publication number: 20140142147
    Abstract: Cyanines which selectively bind to G-quadruplex DNA complexes, particularly quadruplexes expressed in cancer cells, and methods of making and using thereof are described herein. The cyanine can be a symmetrical or unsymmetrical streptocyanine, hemicyanine, closed chain cyanine, or combinations thereof. The cyanine is preferably substituted with one or more groups that minimize or prevent aggregation of the cyanine and/or inhibit binding of the cyanine to duplex DNA. One or more of the cyanines can be formulated with one or more pharmaceutical excipients and/or carrier to prepare pharmaceutical compositions suitable for administration to a patient, particular a human patient. The compounds and compositions described herein can be used to treat diseases or disorders characterized by the expression of G-quadruplex DNA, such as cancer.
    Type: Application
    Filed: July 18, 2012
    Publication date: May 22, 2014
    Applicant: GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION
    Inventors: Maged Henary, W. David Wilson
  • Publication number: 20140142082
    Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 13, 2012
    Publication date: May 22, 2014
    Applicant: PHENEX PHARMACEUTICALS AG
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Publication number: 20140135322
    Abstract: The present invention relates to novel chemical compounds formula (I) (C)n—B-(A)m-B—(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five- and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group (—CO—), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1. The compounds are useful in therapy, especially therapy of a mammal suffering from a disease involving misfolded or aggregated forms of proteins.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 15, 2014
    Inventors: Peter Asberg, Kristin Hammer, Johan Olsson, Martin Henriksson
  • Publication number: 20140135310
    Abstract: Sulphonamide derivatives of alicyclic amines of formula (I), wherein A represents naphthyl or 9- or 10-membered bicyclic group, consisting of benzene ring fused with 5- or 6-membered heterocyclic ring; D represents phenyl, naphthyl, 5-membered aromatic heterocyclic group, bicyclic group consisting of a ring selected from benzene and pyridine, fused with aromatic or non-aromatic 5-membered heterocyclic ring; p, r independently represent 0 or 1; x, z independently represent 1 or 2; n is 2 or 3; and enancjomers, pharmaceutically acceptable salts and solvates thereof. The compounds may be useful for the treatment and/or prevention of the central nervous system disorders.
    Type: Application
    Filed: June 29, 2012
    Publication date: May 15, 2014
    Applicant: Adamed Sp. z o.o.
    Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Maciej Pawlowski, Andrzej Krukowski, Rafal Rusiecki, Agata Magdalena Siwek, Malgorzata Anna Wolak
  • Publication number: 20140127272
    Abstract: The present invention describes nanoprodrugs of non-steroidal anti-inflammatory drug (NSAIDs) and nanoprodrugs of ?-lipoic acid-containing and NSAIDs. These nanoprodrugs have antioxidant properties and stimuli-responsiveness, which can be used to treat various disease conditions.
    Type: Application
    Filed: October 31, 2013
    Publication date: May 8, 2014
    Applicant: Cedars-Sinai Medical Center
    Inventors: John S. Yu, Bong Seop Lee
  • Publication number: 20140127157
    Abstract: Antiviral activity of Nilotinib against Hepatitis C virus.
    Type: Application
    Filed: November 4, 2013
    Publication date: May 8, 2014
    Inventors: Erica Canino, Adam Feire, Christopher Jones, Paul W. Manley
  • Publication number: 20140128409
    Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R6 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.
    Type: Application
    Filed: January 13, 2014
    Publication date: May 8, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: John Edward PARK, Nveed CHAUDHARY, Gerald Juergen ROTH, Armin HECKEL, Thorsten LEHMANN-LINTZ, Joerg KLEY
  • Patent number: 8710068
    Abstract: Disclosed herein are methods of treating cancer by administering to a patient a small molecule inhibitor of Survivin. Also disclosed herein are methods of inhibiting Survivin dimerization in a patient by administering a compound of formula (I), (II), (III), or (IV). Methods of inducing cell cycle arrest in cancer cells, comprising G2/M stage arrest, in a patient by administering a compound of formula (I), (II), (III), or (IV) are also disclosed. Further disclosed herein are methods of inducing apoptosis in cancer cells in a patient by administering a compound of formula (I), (II), (III), or (IV).
    Type: Grant
    Filed: January 19, 2010
    Date of Patent: April 29, 2014
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Alan Berezov, Qiang Wang, Ramachandran Murali, Mark I. Greene
  • Publication number: 20140113927
    Abstract: Hydrophobic weak base compounds such as hydrophobic weak base chemotherapeutic agents (which are not an anthracycline) for use in the treatment of medical conditions such as proliferative disease or disorder in a subject, in combination with illumination of a region in a body of the subject which is characterized by the presence of proliferating cells, are disclosed. The hydrophobic weak base compound and a wavelength of illumination are selected such that the hydrophobic weak base compound acts as a therapeutically effective photosensitizer when exposed to the illumination.
    Type: Application
    Filed: January 2, 2014
    Publication date: April 24, 2014
    Applicant: Technion Research & Development Foundation Limited
    Inventors: Yehuda G. ASSARAF, Yamit Adar Turgeman, Andrzej M. Skladanowski, Arjan W. Griffioen, Henk Verheul, Kristy Gotink, Hubert Van Den Bergh, Patrycja Nowak-Sliwinska
  • Publication number: 20140107124
    Abstract: Disclosed herein are compositions comprising an amide related to a prostaglandin and a biogenic amine. Other aspects relate to certain chemical compounds, pharmaceutical compositions, and methods of treating glaucoma.
    Type: Application
    Filed: December 20, 2013
    Publication date: April 17, 2014
    Applicant: Allergan, Inc.
    Inventors: David F. Woodward, Robert M. Burk
  • Patent number: 8697739
    Abstract: The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.
    Type: Grant
    Filed: July 25, 2011
    Date of Patent: April 15, 2014
    Assignee: Novartis AG
    Inventors: David Weninger Barnes, Gregory Raymond Bebernitz, Kevin Clairmont, Scott Louis Cohen, Robert Edson Damon, Robert Francis Day, Stephanie Kay Dodd, Christoph Gaul, Hatice Belgin Gulgeze Efthymiou, Monish Jain, Rajeshri Ganesh Karki, Louise Clare Kirman, Kai Lin, Justin Yik Ching Mao, Tajesh Jayprakash Patel, Brian Kenneth Raymer, Liansheng Su
  • Patent number: 8691815
    Abstract: The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress-and/or oxytocin-dependent-diseases are also disclosed.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: April 8, 2014
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Thorsten Oost, Wilfried Lubisch, Wilfried Hornberger, Liliane Unger, Andrea Hager-Wernet
  • Publication number: 20140094493
    Abstract: A compound of Formula (I), and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein R1 is independently selected from F, Cl, Br, CN, NH2, OH, CHO, COOH, oxo, C1-4alkyl, C1-4alkoxy, CONH2 (optionally mono- or di-substituted by C1-4alkyl) and SO2NH2, R2 is independently selected from C1-6allkyl substituted by R3 wherein the C1-6alkyl chain optionally comprises one or two heteroatoms select from O; R3 is selected from aryl, C3-6cycloalkyl, C3-6heterocyclyl and C3-6heteroaryl, wherein the heterocyclyl and heteroaryl rings are nitrogen containing; and wherein R3 is optonally substituted by one or more groups selected from R1; n1 is zero or an integer from 1 to 2; n2 is an integer from 1 to 2; and the sum of n1 and 2 is less than or equal to 2; R5 is selected from any group defined for R1 and R2; R6a and R6b are independently selected from H or C1-4alkyl; R7 is independently selected from F, Cl, Br, CN, NH2, OH, CHO, COOH, oxo, C1-4al
    Type: Application
    Filed: February 6, 2012
    Publication date: April 3, 2014
    Inventors: Jillian G. Baker, Peter M. Fischer, Christophe Fromont, Sheila M. Gardiner, Stephen J. Hill, Gopal Jadhav, Barrie Kellam, Shailesh Mistry, Jeanette Woolard
  • Publication number: 20140094499
    Abstract: The present invention relates to formulations of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), pharmaceutical packs or kits thereof, and methods of treatment therewith.
    Type: Application
    Filed: September 16, 2013
    Publication date: April 3, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: ROSSITZA GUEORGUIEVA ALARGOVA, Irina Nikolaevna Kadiyala, Noreen Tasneem Zaman
  • Publication number: 20140093490
    Abstract: The present invention investigate the two modes of glutamate release and the releasing rate of glutamate, and thus can provide a useful technique for neuron protection and acceleration of neurotransmission by controlling the glutamate release in astroctye. Thus, the present invention provides an inhibitor of the fast-mode release and/or the slow-mode release of astrocytic glutamate, a screening method of the inhibitor and a pharmaceutical composition or method of ameliorating, preventing and/or treating the disease associated with the over-release of glutamate via the Ca2+-activated anion channel, with the inhibition of fast-mode glutamate release.
    Type: Application
    Filed: July 23, 2013
    Publication date: April 3, 2014
    Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Changjoon Justin LEE, Soo Jin OH, Eun Mi HWANG, Dong Ho WOO
  • Patent number: 8686023
    Abstract: Pharmaceutically acceptable salts of sunitinib, processes of making sunitinib salts, as well as related pharmaceuticals and methods of treating are described.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: April 1, 2014
    Assignee: Lek Pharmaceuticals D.D.
    Inventor: Lovro Selic
  • Patent number: 8686022
    Abstract: The present invention provides compounds according to general formula (I) which are proposed for the treatment of respiratory complaints, particularly asthma and COPD.
    Type: Grant
    Filed: August 26, 2009
    Date of Patent: April 1, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Holger Wagner, Birgit Jung, Frank Himmelsbach, Rolf Goeggel, Georg Dahmann
  • Publication number: 20140088079
    Abstract: The present invention relates to a compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. The present invention also provides a method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound.
    Type: Application
    Filed: June 1, 2012
    Publication date: March 27, 2014
    Applicant: GREEN CROSS CORPORATION
    Inventors: Soongyu Choi, Kwang Seop Song, Suk Ho Lee, Min Ju Kim, Hee Jeong Seo, Eun-Jung Park, Younggyu Kong, So Ok Park, Hyunku Kang, Myung Eun Jung, Kinam Lee, Hyun Jung Kim, Jun Sung Lee, Min Woo Lee, Mi-Soon KIM, Dong Ho Hong, Misuk Kang
  • Patent number: 8680120
    Abstract: A compound (I) of the present invention, which has an EP1 receptor antagonism: [wherein A represents a benzene ring or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic ring which may have a substituent, a 6-membered aromatic heterocyclic ring which may have a substituent or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.
    Type: Grant
    Filed: July 26, 2010
    Date of Patent: March 25, 2014
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuya Tatani, Naohiro Kawamura, Tatsuhiro Kondo, Atsushi Kondo
  • Publication number: 20140080772
    Abstract: The present invention relates to mono- and combination therapies for melanoma, and in particular, metastatic melanoma. Drugs for use in such therapies in include RO 31-8220, bafetinib, and cardiac glycosides.
    Type: Application
    Filed: September 5, 2013
    Publication date: March 20, 2014
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Sean MORRISON, Elena PISKOUNOVA, Ugur ESKIOCAK
  • Publication number: 20140080826
    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 (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: September 25, 2013
    Publication date: March 20, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: SARA SABINA HADIDA RUAH, Peter Diederik Jan Grootenhuis, Frederick F. Van Goor, Jinglan Zhou, Brian Richard Bear, Mark Thomas Miller, Jason Mc Cartney, Mehdi Numa, Xiaoqing Yang
  • Patent number: 8673904
    Abstract: Provided herein are novel epoxide inhibitors of cysteine proteases, compositions comprising the epoxide inhibitors, and packaged pharmaceuticals. Also provided are methods of inhibiting a papain-family cysteine protease and methods of treating or preventing a disease by administering a composition containing an epoxide inhibitor of the invention. The compositions may be administered in combination with another therapeutic agent.
    Type: Grant
    Filed: June 13, 2007
    Date of Patent: March 18, 2014
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Matthew S. Bogyo, Amir M. Sadaghiani, Steven Verhelst
  • Patent number: 8673909
    Abstract: The invention features methods of treating visceral pain or a condition in a mammal caused by the action of nitric oxide synthase (NOS) or by the action of serotonin 5HT1D/1B receptors, by administering to a patient in need thereof a therapeutically effective amount of an indole compound of Formula (I), or a pharmaceutically acceptable salt or prodrug thereof. The methods of the invention may further comprise the administration of additional therapeutic agent. The invention also features new compounds of Formula (I), pharmaceutical compositions thereof, and methods of resolving enantiomeric mixtures.
    Type: Grant
    Filed: November 17, 2008
    Date of Patent: March 18, 2014
    Assignee: NeurAxon, Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi, John S. Andrews, Gabriela Mladenova
  • Publication number: 20140073680
    Abstract: Therapeutic compositions comprising an indoloquinone compound and various bladder cancer treatments and methods are disclosed. More specifically, the compositions comprise an indoloquinone compound and a formulation vehicle. The formulation vehicle improves the solubility and stability of the indoloquinone compound. Additionally, the coating compositions can include coating agents that provide better adhesion of the coating composition to the bladder wall during intravesical delivery of the coating composition.
    Type: Application
    Filed: August 30, 2013
    Publication date: March 13, 2014
    Applicant: Spectrum Pharmaceuticals, Inc.
    Inventors: Bastiaan Nuijen, Ernie Pfadenhauer, Jos H. Beijnen, Dorla Mirejovsky, Guru Reddy, Luigi Lenaz
  • Publication number: 20140073656
    Abstract: Novel compounds for the treatment of estrogen receptor-mediated disorders, including breast cancer, and methods of treatment using the novel compounds. The novel compounds, when administered in a safe and effective amount, present extended binding to estrogen receptors in breast tissue without activating the estrogen receptors. Estrogen is blocked from binding to the estrogen receptors for an extended period of time, effectively hindering growth of breast cancer cells.
    Type: Application
    Filed: October 10, 2013
    Publication date: March 13, 2014
    Applicant: Florida A&M University
    Inventor: John S. Cooperwood
  • Publication number: 20140066388
    Abstract: Disclosed are compositions and methods for treating or preventing diseases or disorders associated with mitochondrial CaMKII activity.
    Type: Application
    Filed: September 4, 2013
    Publication date: March 6, 2014
    Applicant: UNIVERSITY OF IOWA RESEARCH FOUNDATION
    Inventors: Mark E. Anderson, Mei-ling A. Joiner, Aliasger K. Salem, Amaraporn Wongrakpanich, Frederick E. Domann, Duane D. Hall, Olha M. Koval, Douglas R. Spitz
  • Publication number: 20140050694
    Abstract: A method of treating autoimmune diseases and transplant rejection, comprising the step of treating the autoimmune or transplant patient with an effective amount of SU-5416 is disclosed.
    Type: Application
    Filed: August 19, 2013
    Publication date: February 20, 2014
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Joshua David Mezrich, Christopher A. Bradfield
  • Publication number: 20140051687
    Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.
    Type: Application
    Filed: October 21, 2013
    Publication date: February 20, 2014
    Applicant: NeurAxon, Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
  • Publication number: 20140051682
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: September 24, 2013
    Publication date: February 20, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, Xiaoxia Liu, John E. Donello, Veena Viswanath
  • Patent number: 8653071
    Abstract: The present invention relates to novel ?4?2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them. The present invention relates to novel ?4?2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them.
    Type: Grant
    Filed: May 3, 2010
    Date of Patent: February 18, 2014
    Assignee: Suven Life Sciences Limited
    Inventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Kana Ram Kumawat, Ishtiyaque Ahmad, Pradeep Jayarajan, Anil Karbhari Shinde, Nagaraj Vishwottam Kandikere, Koteshwara Mudigonda, Venkateswarlu Jasti
  • Patent number: 8653072
    Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R5 and R6 are as defined in the specification.
    Type: Grant
    Filed: January 11, 2013
    Date of Patent: February 18, 2014
    Assignee: Karo Bio AB
    Inventors: Patrik Rhonnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstal, Aiping Cheng
  • Publication number: 20140045910
    Abstract: Novel amino-pyrrolinic derivatives, their pharmacologically acceptable salts and use thereof in the prevention and/or treatment of metabolic syndrome.
    Type: Application
    Filed: April 17, 2012
    Publication date: February 13, 2014
    Applicant: UNIVERSITE DE STRASBOURG
    Inventors: Pascal Bousquet, Jean Daniel Ehrhardt, Lyne Fellmann, Vincent Gasparik, Hugues Greney, Mohamed Hadjeri, Andre Mann, Nathalie Niederhoffer, Stephan Schann
  • Publication number: 20140044789
    Abstract: This invention provides melanin nanoshells and their use for protection against radiation, particularly ionizing radiation, and electronic pulses, and methods of making materials comprising melanin nanoshells.
    Type: Application
    Filed: October 22, 2013
    Publication date: February 13, 2014
    Applicant: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Ekaterina Dadachova, Arturo Casadevall
  • Patent number: 8648108
    Abstract: Anti-cancer coating compositions comprising 3-hydroxymethyl-5-aziridinyl-1-1-methyl-2-[1H-indole-4,7-dione]propenol (E09) are disclosed. More specifically, the coating compositions comprise EO9 and a formulation vehicle. The formulation vehicle improves the solubility and stability of EO9. Additionally, the coating compositions can include coating agents that provide better adhesion of the coating composition to the bladder wall during intravesical delivery of the coating composition.
    Type: Grant
    Filed: June 11, 2012
    Date of Patent: February 11, 2014
    Assignee: Spectrum Pharmaceuticals, Inc.
    Inventors: Bastiaan Nuijen, Ernie Pfadenhauer, Jos H. Beijen
  • Publication number: 20140038944
    Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R3 and R4 is H, and the other is selected from C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, and C6-12-aralkyl; or R3 and R4 are each independently selected from C1-6-alkyl and halo; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high efficacies for human cathepsin S, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, Sjogrens syndrome, Grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.
    Type: Application
    Filed: October 4, 2013
    Publication date: February 6, 2014
    Applicant: Amura Therapeutics Limited
    Inventors: Martin Quibell, John Paul Watts, Nicholas Sean Flinn
  • Publication number: 20140039031
    Abstract: The present disclosure is directed to compositions and methods for formulating a pharmaceutical dosage form by forming a composition comprising acetyl-11-keto-?-boswellic acid, diindolylmethane, or curcumin with one or more pharmaceutically acceptable excipients for enhanced solubility to increase bioavailability and improve therapeutic efficacy. The composition can be processed by thermo-kinetic compounding along with conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding.
    Type: Application
    Filed: February 23, 2012
    Publication date: February 6, 2014
    Applicants: Dispersol Technologies. LLC, Board of Regents, The University of Texas System
    Inventors: Chris Brough, Robert O. Williams, III, James W. McGinity, Dave A. Miller, Justin Hughey, Ryan Bennett