Bicyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 514/367)
  • Patent number: 10414760
    Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.
    Type: Grant
    Filed: November 29, 2016
    Date of Patent: September 17, 2019
    Assignee: ANGION BIOMEDICA CORP.
    Inventors: Bijoy Panicker, Dong Sung Lim, Rama K. Mishra, Lambertus J. W. M. Oehlen, James G. Tarrant, Xiaokang Zhu, Dawoon Jung
  • Patent number: 10407600
    Abstract: The invention relates to a yeast protein extract with adhesive properties, comprising extracts of Rhodotorula rubra, Pichia pastoris and Sacharomyces cerevisiae, which have been deposited. The invention also relates to an adhesive composition for wood panels, comprising the yeast protein extract in equal quantities. The invention further relates to a method for preparing the yeast protein extract. The composition can be used in wood panels.
    Type: Grant
    Filed: October 25, 2016
    Date of Patent: September 10, 2019
    Assignee: UNIVERSIDAD DEL BIO BIO
    Inventors: Mario A. Núñez, Julio E. Alarcón, Aldo A. Ballerini
  • Patent number: 10383858
    Abstract: The invention relates to the use of a pan-PPAR agonist, or of a pharmaceutical composition containing said agonist, for the treatment of a fibrotic condition.
    Type: Grant
    Filed: July 24, 2018
    Date of Patent: August 20, 2019
    Assignee: INVENTIVA
    Inventors: Irena Konstantinova, Jean-Michel Luccarini, Jean-Louis Junien, Pierre Broqua
  • Patent number: 10357497
    Abstract: Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1A2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of riluzole from a pro-drug agent.
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: July 23, 2019
    Assignee: Biohaven Pharmaceutical Holding Company Limited
    Inventors: Allen B. Reitz, Garry R. Smith
  • Patent number: 10285981
    Abstract: A method for treating amyotrophic lateral sclerosis (ALS) in a subject in need thereof comprising administering to said subject an effective amount of (6R)-2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole or pharmaceutically acceptable salt thereof, wherein said subject is a treatment responder. In certain embodiments, said subject is a subject with definite amyotrophic lateral sclerosis, a subject with amyotrophic lateral sclerosis symptom onset duration of less than about 18 months, a subject with a high level of serum creatinine, a subject with concomitant riluzole administration and combinations thereof.
    Type: Grant
    Filed: March 20, 2018
    Date of Patent: May 14, 2019
    Assignee: Knopp Biosciences LLC
    Inventors: Michael E. Bozik, Thomas Petzinger, Jr., James L. Mather, Donald Archibald
  • Patent number: 10231954
    Abstract: The present invention provides a compound of formula (I) wherein: Y represents a C or N atom which may be substituted or form a cyclic group with R?? but may not be a quaternary C atom; R? is —OR1, —CONH2, —CF3, F, —OH, —NO2, —CN or —OCOR1 in which R1, is C1-3 alkyl and each may be in the beta or gamma position; R? is C1-3 alkyl or H; and R?? is H or a group consisting of 1-12 non-hydrogen atoms and may be linear, branched and/or incorporate one or more cyclic groups, cyclic groups may be aromatic and/or heterocyclic and 2 or more cyclic groups may be linked or fused and each may be substituted; or a salt, hydrate or solvate of a compound of formula (I) for use in the treatment or prevention of a neurodegenerative disorder by inhibiting formation of neurofibrillary (tau) tangles and/or by inhibiting Dyrk 1A. The invention further relates to non-therapeutic uses of these compounds.
    Type: Grant
    Filed: February 4, 2015
    Date of Patent: March 19, 2019
    Assignee: LYTIX BIOPHARMA AS
    Inventors: John S. Svendsen, Wenche Stensen, Frederick A. Leeson
  • Patent number: 10195183
    Abstract: Disclosed herein are methods of treating conditions, which may be associated with elevated levels of mast cells, basophils, eosinophils, or a combination thereof, with a therapeutically effective amount of dexpramipexole or pharmaceutical acceptable salt thereof.
    Type: Grant
    Filed: August 14, 2017
    Date of Patent: February 5, 2019
    Assignee: Knopp Biosciences LLC
    Inventors: Michael E Bozik, Steven Dworetzky
  • Patent number: 10195213
    Abstract: Disclosed herein are compounds that are effective for treatment of various disease states associated with senescence. The disclosed compounds can be used to eliminate senescent cells for disease treatment. The dosing of the compounds includes both single administration and regimens of cycling dosages.
    Type: Grant
    Filed: March 14, 2016
    Date of Patent: February 5, 2019
    Assignee: UNITY BIOTECHNOLOGY, INC.
    Inventor: Nathaniel David
  • Patent number: 10076528
    Abstract: This invention relates the use of cortisol blockers (glucocorticoid receptor [GR] antagonists) for the treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease.
    Type: Grant
    Filed: December 26, 2017
    Date of Patent: September 18, 2018
    Assignee: Pop Test Oncology Limited Liability Company
    Inventors: Randice Lisa Altschul, Neil David Theise, Myron Rapkin, Rebecca O'Brien
  • Patent number: 10052311
    Abstract: The invention relates to the use of a pan-PPAR agonist, or of a pharmaceutical composition containing said agonist, for the treatment of a fibrotic condition.
    Type: Grant
    Filed: June 12, 2015
    Date of Patent: August 21, 2018
    Assignee: INVENTIVA
    Inventors: Irena Konstantinova, Jean-Michel Luccarini, Jean-Louis Junien, Pierre Broqua
  • Patent number: 9968579
    Abstract: The present disclosure describes how all-retinoic acid (ATRA) binds and inhibits Pin1 activity and induces degradation of the activated Pin1 monomer selectively in cancer cells. Identification of the binding mechanism of ATRA with Pin1 confirm ATRA binding specificity to Pin1 residues in the PPIase active site, thus demonstrating that drug-induced Pin1 ablation has potent anticancer activity, such as in acute promyelocytic leukemia (APL), by inducing PML-RARa degradation, as well as against other types of cancer and diseases that are associated with Pin1 overexpression, such as aggressive triple negative breast cancer, lupus, asthma, cocaine addiction, among others, due to their unique ability to simultaneously block numerous cancer-driving pathways, with relatively lower toxicity. The present disclosure also provides a rationale for developing sustained released ATRA-containing formulations.
    Type: Grant
    Filed: July 16, 2015
    Date of Patent: May 15, 2018
    Assignee: Beth Isreal Deaconess Medical Center, Inc.
    Inventors: Kun Ping Lu, Xiao Zhen Zhou, Shuo Wei
  • Patent number: 9956206
    Abstract: A method for treating amyotrophic lateral sclerosis (ALS) in a subject in need thereof comprising administering to said subject an effective amount of (6R)-2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole or pharmaceutically acceptable salt thereof, wherein said subject is a treatment responder. In certain embodiments, said subject is a subject with definite amyotrophic lateral sclerosis, a subject with amyotrophic lateral sclerosis symptom onset duration of less than about 18 months, a subject with a high level of serum creatinine, a subject with concomitant riluzole administration and combinations thereof.
    Type: Grant
    Filed: April 20, 2017
    Date of Patent: May 1, 2018
    Assignee: Knopp Biosciences LLC
    Inventors: Michael E. Bozik, Thomas Petzinger, Jr., James L. Mather, Donald Archibald
  • Patent number: 9856252
    Abstract: Substituted benzimidazole and 3H-imidazo[4,5-b]pyridines or formula I: where X and Y respectively are selected from: (i) N and N; and (ii) N and CR4; A2 is selected from: a C5 heteroarylene group, containing 2 or 3 ring heteroatoms, where the bonds to L1 and the core are ? to one another; L1 is selected from: (i) A1—O—CH2—A2; (ii) A1—CH2—O—A2; (iii) A1—C(?O)—NH—A2; (iv) A1—CH(OH)—A2; (v) A1—CH2—NH—C(?O)—A2; (vi) A1—S—CH2—A2; (vii) A1—CH2—S—A2; (viii) A1—CH2—A2; and (ix) A1—CH(CH3)—O—A2; A1 is phenyl, optionally substituted by F or CF3; their use as pharmaceuticals, and in particular, in treating cancer and hemoglobinopathies.
    Type: Grant
    Filed: February 20, 2014
    Date of Patent: January 2, 2018
    Assignee: Cancer Therapeutics CRC Pty Ltd
    Inventors: Paul Anthony Stupple, Scott Raymond Walker, Jo-Anne Pinson, Helen Rachel Lagiakos, Gillian Elizabeth Lunniss, Ian Peter Holmes, Alexandra Elizabeth Stupple, Ylva Elisabet Bergman, Richard Charles Foitzik, Wilhelmus Johannes Antonius Kersten, Michelle Ang Camerino
  • Patent number: 9801893
    Abstract: Methods are directed to the treatment of subjects with prostate cancer, in particular those with castration resistant prostate cancer, with glucocorticoid receptor antagonists. The prostate cancer may be one that has become resistant to androgen deprivation therapy, for example, by increase in glucocorticoid receptor expression and/or activity.
    Type: Grant
    Filed: February 2, 2016
    Date of Patent: October 31, 2017
    Assignee: The University of Chicago
    Inventors: Russell Z. Szmulewitz, Suzanne D. Conzen
  • Patent number: 9763918
    Abstract: Disclosed herein are methods of treating conditions, which may be associated with elevated levels of mast cells, basophils, eosinophils, or a combination thereof, with a therapeutically effective amount of dexpramipexole or pharmaceutical acceptable salt thereof.
    Type: Grant
    Filed: August 13, 2014
    Date of Patent: September 19, 2017
    Assignee: Knopp Biosciences LLC
    Inventors: Michael E. Bozik, Steven Dworetzky
  • Patent number: 9725427
    Abstract: Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: August 8, 2017
    Assignees: Biohaven Pharmaceutical Holding Company Limited, Rutgers, The State University of New Jersey
    Inventors: Garry R. Smith, Allen B. Reitz, Mark McDonnell, Suzie Chen, Matthew D. Vera, Benjamin E. Blass, Jeffery C. Pelletier, Venkata N. Velvadapu, Jay E. Wrobel
  • Patent number: 9675591
    Abstract: The present invention provides methods for treating seizure disorders. The method includes administering to a subject in need thereof 2-amino-6-trifluoromethylthio-benzothiazole, or a pharmaceutically acceptable salt thereof. Methods for the treatment of pain are also described.
    Type: Grant
    Filed: April 15, 2016
    Date of Patent: June 13, 2017
    Assignee: The Regents of the University of California
    Inventors: Heike Wulff, Nichole Coleman, David Paul Jenkins
  • Patent number: 9662313
    Abstract: A method for treating amyotrophic lateral sclerosis (ALS) in a subject in need thereof comprising administering to said subject an effective amount of (6R)-2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole or pharmaceutically acceptable salt thereof, wherein said subject is a treatment responder. In certain embodiments, said subject is a subject with definite amyotrophic lateral sclerosis, a subject with amyotrophic lateral sclerosis symptom onset duration of less than about 18 months, a subject with a high level of serum creatinine, a subject with concomitant riluzole administration and combinations thereof.
    Type: Grant
    Filed: February 28, 2014
    Date of Patent: May 30, 2017
    Assignee: Knopp Biosciences LLC
    Inventors: Michael E. Bozik, Thomas Petzinger, Jr., James L. Mather, Donald Archibald
  • Patent number: 9648877
    Abstract: The present invention provides a method for increasing tolerance to abiotic stress and/or reducing the consequence of abiotic stress in a plant or part thereof comprising contacting a plant or part thereof with a composition comprising an effective amount of dicarboxylic acid or derivative thereof.
    Type: Grant
    Filed: August 25, 2014
    Date of Patent: May 16, 2017
    Assignee: Crop Microclimate Management Inc.
    Inventor: Charles Christian Kupatt
  • Patent number: 9642840
    Abstract: Disclosed herein are methods of treating conditions, which may be associated with elevated levels of plasma cells and/or B-cells, with a therapeutically effective amount of dexpramipexole or pharmaceutical acceptable salt thereof.
    Type: Grant
    Filed: August 13, 2014
    Date of Patent: May 9, 2017
    Assignee: Knopp Biosciences, LLC
    Inventors: Michael E. Bozik, Steven Dworetzky
  • Patent number: 9623012
    Abstract: The present invention relates to a pharmaceutical composition in solid oral dosage form comprising (R)-7-(2-(1-(4-butoxyphenyl)-2-methylpropan-2-ylamino)-1-hydroxyethyl)-5-hydroxybenzo[d]thiazol-2(3H)-one acetate salt.
    Type: Grant
    Filed: February 26, 2014
    Date of Patent: April 18, 2017
    Assignee: NOVARTIS AG
    Inventors: Miloud Achour, Robin Alec Fairhurst, Arnaud Grandeury, Shinji Hatakeyama, Magdalena Koziczak-Holbro, Nicola Tufilli, Thomas Ullrich
  • Patent number: 9512096
    Abstract: The present invention is related to an improved process for the preparation of amino-substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: December 6, 2016
    Assignee: Knopp Biosciences, LLP
    Inventors: Weirong Chen, Michael Humora, Daw-long Albert Kwok, William F. Kiesman, Erwin Ayandra Irdam
  • Patent number: 9428474
    Abstract: The present invention relates to the following compounds for use in the treatment of a bacterial infection wherein the integers are as defined in the description. The invention also relates to compounds for use as medicaments, pharmaceutical compositions and some novel compounds.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: August 30, 2016
    Assignee: Janssen Sciences Ireland UC
    Inventors: Jérôme Émile Georges Guillemont, Magali Madeleine Simone Motte, Anil Koul, Nacer Lounis
  • Patent number: 9334251
    Abstract: Compounds and their pharmaceutically acceptable salts for treatment of tauopathies, such as Alzheimer's disease, Pick's disease, progressive supranuclear palsy, corticobasal degeneration, familial frontotemporal dementia/Parkinsonism linked to chromosome 17, amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia.
    Type: Grant
    Filed: June 16, 2015
    Date of Patent: May 10, 2016
    Assignee: PROTAMED, INC.
    Inventors: Luke A Esposito, Marisa C Yadon, Joel Cummings, F Michael Hudson, Thomas Lake, Qubai Hu, Judy Cam, Alan D Snow
  • Patent number: 9259495
    Abstract: Methods for detecting or ruling out a meningioma in a patient using a phenylbenzothiazole derivative or a stilbene derivative or a biphenylalkyne derivative, and a medical imaging technique such as positron emission tomography/computed tomography are disclosed.
    Type: Grant
    Filed: October 11, 2011
    Date of Patent: February 16, 2016
    Assignee: MAYO FOUNDATION FOR MEDICAL EDUCATION AND RESEARCH
    Inventors: Geoffrey B. Johnson, Val J. Lowe, Mark A. Nathan, Joseph E. Parisi
  • Patent number: 9243020
    Abstract: The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: January 26, 2016
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Ramesh Kaul, Ernest J. McEachern, Harold G. Selnick, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu
  • Patent number: 9241929
    Abstract: An object of the present invention is to provide a prophylactic or ameliorating agent for a genetic disease that is caused by a mutation in an exon of a gene and is capable of forming a functional truncated protein by skipping of the exon comprising the mutation. The prophylactic or ameliorating agent used in the present invention is a prophylactic or ameliorating agent for a genetic disease that is caused by a mutation in an exon of a gene and is capable of forming a functional truncated protein by skipping of the exon comprising the mutation, wherein the prophylactic or ameliorating agent contains a compound having a molecular weight of 1500 or lower.
    Type: Grant
    Filed: June 27, 2011
    Date of Patent: January 26, 2016
    Inventors: Masatoshi Hagiwara, Masafumi Matsuo, Naoyuki Kataoka, Atsushi Nishida
  • Patent number: 9206130
    Abstract: Novel compounds which are inhibitors of receptor tyrosine kinases of the AXL receptor family are described herein. These compounds are suitable for the treatment or prevention of disorders associated with, accompanied by or caused by hyperfunction of a receptor of the AXL family. The compounds are suitable for the treatment of hyperproliferative disorders, such as cancer, particularly cancer metastases.
    Type: Grant
    Filed: April 16, 2009
    Date of Patent: December 8, 2015
    Assignee: Max-Planck-Gesellschaft zur Förderung der Wissenschaften E.V.
    Inventors: Axel Ullrich, Pjotr Knyazev, Yixiang Zhang, Kéri György, László Örfi, István Szabadkai
  • Patent number: 9096499
    Abstract: The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. Compounds of the present invention display significant potency as kinase inhibitors, cause the downregulation of c-myc, and inhibit the growth and survival of cancerous cell lines.
    Type: Grant
    Filed: January 3, 2014
    Date of Patent: August 4, 2015
    Assignee: Board of Regents, The University of Texas System
    Inventors: Waldemar Priebe, Nicholas Donato, Moshe Talpaz, Slawomir Szymanski, Izabela Fokt, Alexander Levitzki
  • Publication number: 20150148308
    Abstract: A harmful arthropod control composition comprising a compound represented by the following Formula (1) wherein each symbol represents definitions described in the specification, and one or more fungicidal compounds, which are selected from among azoles, strobilurins, phenylamides, rice blast controlling compounds, rice sheath blight disease controlling compounds, and other fungicidal compounds. The composition has an excellent controlling effect against harmful arthropods.
    Type: Application
    Filed: June 5, 2013
    Publication date: May 28, 2015
    Applicant: Sumitomo Chemical Company, Limited
    Inventors: Tatsuya Suzuki, Atsushi Iwata, Yoshihiko Nokura
  • Publication number: 20150148329
    Abstract: Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1A2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of riluzole from a pro-drug agent.
    Type: Application
    Filed: June 24, 2013
    Publication date: May 28, 2015
    Inventors: Allen B. Reitz, Garry Robert Smith
  • Patent number: 9034319
    Abstract: A method of treating a cancer of the central nervous system in a subject in need thereof is provided. The method comprising administering to the subject a therapeutically effective amount of an agent which reduces blood glutamate levels and enhances brain to blood glutamate efflux to thereby treat the cancer of the central nervous system in the subject.
    Type: Grant
    Filed: May 26, 2008
    Date of Patent: May 19, 2015
    Assignee: Yeda Research and Development Co. Ltd.
    Inventors: Vivian I. Teichberg, Angela Ruban-Matuzani
  • Publication number: 20150133495
    Abstract: Disclosed herein is a compound of Formula I or a pharmaceutically acceptable salt thereof, in which A, G, R1 and R2 are as defined herein. The compounds and pharmaceutical compositions of the compounds are suitable for the treatment of HCV infection in mammals and are also useful to modulate or inhibit NS3/4 dimerization.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 14, 2015
    Inventor: Daniel Lamarre
  • Publication number: 20150133513
    Abstract: Pharmaceutical compositions are provided for treatment of Parkinson's disease comprising a pharmaceutically acceptable carrier and a fixed dose combination of two active agents selected from compounds having either neuroprotective or symptomatic effects, or both, in Parkinson's disease patients, wherein the molar ratio of the two compounds is in the range of 1:1 to 1:100. The compositions are formulated for immediate release, controlled release, or both immediate and controlled release.
    Type: Application
    Filed: January 22, 2015
    Publication date: May 14, 2015
    Inventors: Itschak LAMENSDORF, Yoram Sela
  • Publication number: 20150133465
    Abstract: The invention provides compounds of formula (I): wherein R1-R3, n, and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Inventors: Edmond J. LaVoie, Ajit Parhi, Daniel S. Pilch, Yongzheng Zhang, Malvika Kaul
  • Patent number: 9029357
    Abstract: The present patent application concerns new ligands of the H4-receptor, their process of preparation and their therapeutic use.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: May 12, 2015
    Assignee: Bioprojet
    Inventors: Isabelle Berrebi-Bertrand, Xavier Billot, Thierry Calmels, Marc Capet, Denis Danvy, Stéphane Krief, Olivier Labeeuw, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Philippe Robert, Jean-Charles Schwartz
  • Publication number: 20150126507
    Abstract: The invention is directed, in part, to compounds of structure (I) to treat or prevent hearing loss. Compounds of the present invention also promote sensory hair cell regeneration. Particular compositions comprise compounds of structure (I), and optionally one or more small molecules that increase the proliferation of supporting cells.
    Type: Application
    Filed: September 5, 2014
    Publication date: May 7, 2015
    Inventors: Robert Scott Thies, Zhiyong Wang, Bonnie Jacques, Chin-Chun Jean Lu
  • Publication number: 20150126371
    Abstract: The present invention relates to a pyrazolopyran of the general formula I wherein the variables are defined according to the description, including a tautomer, salt, cleavable prodrug, or mixtures thereof, in particular to said pyrazolopyran for use as a medicament and/or an inhibitor of the enzyme serinehydroxymethyltransferase (SHMT). The invention also relates to a process the preparation of a pyrazolopyran of the formula I, to compositions comprising said compound and processes for the preparation of these compositions. Further it relates to use of the pyrazolopyran of formula I as an herbicide as well as to a method of controlling undesired vegetation.
    Type: Application
    Filed: May 29, 2013
    Publication date: May 7, 2015
    Inventors: Matthias Witschel, Frank Stelzer, Johannes Hutzler, Tao Qu, Thomas Mietzner, Klaus Kreuz, Klaus Grossmann, Raphael Aponte, Hans Wolfgang Hoeffken, Frederick Calo, Thomas Ehrhardt, Anja Simon, Liliana Parra Rapado
  • Patent number: 9024038
    Abstract: Inhibitors of HIV-1 protease and compositions containing them are described. Use of the inhibitors and compositions containing them to treat HIV, AIDS, and AIDS-related diseases is described.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: May 5, 2015
    Assignee: Purdue Research Foundation
    Inventors: Arun K. Ghosh, Bruno D. Chapsal, Hiroaki Mitsuya, Cuthbert D. Martyr
  • Publication number: 20150119380
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.
    Type: Application
    Filed: December 28, 2012
    Publication date: April 30, 2015
    Inventors: Matthew G. Woll, Guangming Chen, Soongyu Choi, Amal Dakka, Song Huang, Gary Mitchell Karp, Chang-Sun Lee, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Sergey Paushkin, Hongyan Qi, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Emmanuel Pinard, Hasane Ratni
  • Publication number: 20150118311
    Abstract: Brain-penetrating polymeric nanoparticles that can be loaded with drugs and are optimized for intracranial convection-enhanced delivery (CED) have been developed. In the preferred embodiment, these are loaded with FDA-approved compounds, identified through library screening to target brain cancer stem cells (BSCSs). The particles are formed by emulsifying a polymer-drug solution, then removing solvent and centrifuging at a first force to remove the larger particles, then collecting the smaller particles using a second higher force to sediment the smaller particles having a diameter of less than 100 nm, more preferably less than 90 nanometers average diameter, able to penetrate brain interstitial spaces.
    Type: Application
    Filed: May 6, 2013
    Publication date: April 30, 2015
    Applicant: Yale Universit
    Inventors: Jiangbing Zhou, Toral R. Patel, Joseph M. Piepmeier, William Mark Saltzman
  • Patent number: 9018206
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: April 28, 2015
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Publication number: 20150111932
    Abstract: The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing neurological degenerative disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of Parkinson's disease (PD), restless legs syndrome (RLS), cluster headache, depression, fibromyalgia, sexual dysfunction, amyotrophic lateral sclerosis (ALS), also known as Lou Gehrig's disease and depression.
    Type: Application
    Filed: February 2, 2013
    Publication date: April 23, 2015
    Inventor: Mahesh KANDULA
  • Patent number: 9012481
    Abstract: Novel benzoarylureido compounds and a use thereof for prevention and/or treatment of the neurodegenerative brain disease are provided. The neurodegenerative brain diseases may include Alzheimer's disease, dementia, Parkinson's disease, stroke, amyloidosis, Pick's disease, Lou Gehrig's disease, Huntington's disease, Creutzfeld-Jakob disease, and the like.
    Type: Grant
    Filed: December 29, 2009
    Date of Patent: April 21, 2015
    Assignee: Korea Institute of Science and Technology
    Inventors: Hoh-Gyu Hahn, Kee-Dal Nam, Dong-Yun Shin, Chan-Ho Park, Sung-Woo Cho, Eun-A Kim, Ghil-Soo Nam, Kyung-Il Chol, Seon-Hee Seo, Hee-Sup Shin, Dong-Jin Kim, Ae-Nim Pae, Hye-Jin Chung, Hyun-Ah Choo, Hye-Whon Rhim, Yong-Seo Cho, Eun-Joo Roh, Gyo-Chang Keum, Kee-Hyun Choi, Kye-Jung Shin, Chan-Seong Cheong, Jae-Kyun Lee, Yong-Koo Kang, Young-Soo Kim, Woong-Seo Park, Key-Sun Kim, He-Sson Chung, Chi-Man Song, Sun-Joon Min, Eunice Eun-Kyeong Kim, Cheol-Ju Lee, Soon-Bang Kang
  • Patent number: 9012445
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor 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: Grant
    Filed: January 12, 2013
    Date of Patent: April 21, 2015
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Publication number: 20150105378
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20150105403
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 16, 2015
    Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Jackaline D. Julien, Johnny Y. Nagasawa, Karensa L. Douglas, Celine Bonnefous, Andiliy G. Lai
  • Patent number: 9006275
    Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L2, are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: April 14, 2015
    Assignee: AbbVie Inc.
    Inventors: Alan S. Florjancic, Michael J. Dart, Keith B. Ryther, Arturo Perez-Medrano, William A. Carroll, Meena V. Patel, Karin Rosemarie Tietje, Tongmei Li, Teodozyj Kolasa, Megan E. Gallagher, Sridhar Peddi, Jennifer M. Frost, Derek W. Nelson
  • Patent number: 9006139
    Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.
    Type: Grant
    Filed: August 19, 2014
    Date of Patent: April 14, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
  • Patent number: RE47404
    Abstract: The present disclosure relates to methods for treating viral hepatitis, compounds useful in the treatment of viral hepatitis, and pharmaceutical compositions comprising such compounds. In one embodiment, pharmaceutical compositions comprising nitazoxanide, tizoxanide, or derivatives and/or mixtures thereof are provided, as well as methods of treating hepatitis C using such compositions.
    Type: Grant
    Filed: July 7, 2017
    Date of Patent: May 28, 2019
    Assignee: ROMARK LABORATORIES, L.C.
    Inventor: Jean-Francois Rossignol