Bicyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 514/367)
  • Patent number: 11911369
    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: May 4, 2020
    Date of Patent: February 27, 2024
    Assignee: Biohaven Therapeutics Ltd.
    Inventors: Jay Edward Wrobel, Allen B. Reitz, Jeffery Claude Pelletier, Garry Robert Smith, Haiyan Bian
  • Patent number: 11884673
    Abstract: Compounds useful in the modulation of ion channel activity in cells are disclosed herein. This disclosure also relates to use of these compounds in the treatment of pain, and pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Grant
    Filed: April 20, 2022
    Date of Patent: January 30, 2024
    Assignee: BIONOMICS LIMITED
    Inventors: Belinda Huff, Courtney Hollis, Hamish Toop, Nathan Kuchel, Lorna Helen Mitchell, Rajinder Singh
  • Patent number: 11845740
    Abstract: The invention relates to chemistry of organic substances, pharmacology and medicine, and concerns treating diseases associated and with aberrant activity of cells of the immune system, more particularly for treating lung, respiratory tract and abdominal diseases, radiation sickness and pain syndrome, and also other diseases by using compounds of formula (A) wherein R1 is —C(O)—R2—(O)— or —R2—C(O)— group, where R2 is —(CH2)n-group optionally substituted with one or two C1-C6 alkyls, or phenyl, n is an integer from 0 to 4; wherein compounds are selected from the group consisting of the group of compounds as set out in the description. These compounds, as well as pharmaceutically acceptable salts thereof, are highly effective in inhibiting glutaminyl cyclase, which is involved, in particular, in processes of post-translational modification of chemokines and chemotaxis of monocytes, macrophages and other cells of the immune system.
    Type: Grant
    Filed: May 24, 2018
    Date of Patent: December 19, 2023
    Assignees: LTD “VALENTA-INTELLEKT”
    Inventors: Vladimir Evgenievich Nebolsin, Anastasia Vladimirovna Rydlovskaya, Tatyana Alexandrovna Kromova
  • Patent number: 11827630
    Abstract: Provided are novel crystalline forms of Lanifibranor (Referred to as “Compound I”) and preparation methods thereof, pharmaceutical compositions containing the crystalline forms, and uses of the crystalline forms for preparing pan-PPAR agonists drugs and drugs for treating NASH. Compared with prior arts, the provided crystalline forms of Compound I have one or more improved properties, which solve the problems of the prior art and is of great value to the optimization and development of the drugs.
    Type: Grant
    Filed: August 15, 2022
    Date of Patent: November 28, 2023
    Assignee: CRYSTAL PHARMACEUTICAL (SUZHOU) CO., LTD.
    Inventors: Minhua Chen, Hongyan Zhu
  • Patent number: 11739104
    Abstract: The present invention provides compositions and methods for inhibiting group II intron splicing for treating or preventing a disease or disorder associated with an organism harboring an active group II intron. The present invention also provides compositions and methods for inhibiting group II intron splicing for inhibiting, preventing or reducing growth of an organism harboring an active group II intron.
    Type: Grant
    Filed: January 25, 2019
    Date of Patent: August 29, 2023
    Assignee: YALE UNIVERSITY
    Inventors: Anna Pyle, Olga Fedorova, Erik Gunnar Jagdmann, Michael Van Zandt, Lin Yuan, Albert DeBerardinis
  • Patent number: 11717804
    Abstract: An 8-hydroxyquinoline modified halloysite nanoclay (8-HQHNC) is provided. The 8-HQHNC is used in a method of removing heavy metals and/or salt from a solution which includes steps of contacting the solution with 8-HQHNC under conditions suitable for the adsorption of the heavy metals and/or salt to the 8-HQHNC and recovering the 8-HQHNC from the solution.
    Type: Grant
    Filed: November 16, 2022
    Date of Patent: August 8, 2023
    Assignee: KING ABDULAZIZ UNIVERSITY
    Inventors: Mohamed Abdel Salam, Radwan K. Al-Farawati, Naif Salama Aljohani, Ibrahim I. Shabbaj
  • Patent number: 11639337
    Abstract: The present invention relates compounds of Formula (A), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological and psychiatric disorders and diseases as well as cancer in humans.
    Type: Grant
    Filed: June 8, 2022
    Date of Patent: May 2, 2023
    Assignee: XWPHARMA LTD.
    Inventors: Jia-Ning Xiang, Xuesong Xu, Wei Zhou
  • Patent number: 11554117
    Abstract: Methods of treating mental disorders, including anxiety disorders such as obsessive-compulsive disorder, are provided. The methods comprise administering an effective amount of a glutamate modulator to an individual in need thereof. Also provided are methods of enhancing the activity of a serotonin reuptake inhibitor (SRI) comprising co-administering a glutamate modulator and a serotonin reuptake inhibitor. Pharmaceutical composition comprising a serotonin reuptake inhibitor and a glutamate modulator are also provided.
    Type: Grant
    Filed: July 10, 2018
    Date of Patent: January 17, 2023
    Assignee: YALE UNIVERSITY
    Inventors: Vladimir Coric, John H. Krystal, Gerard Sanacora
  • Patent number: 11547700
    Abstract: The present invention describes the use of a 5HT3-antagonist, in combination with a 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine, to reduce adverse effects and to facilitate the neuroprotective treatment of a patient suffering from a synucleinopathic disorder to enable a therapeutically effective 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine daily dose without the dose-limiting adverse effects caused by pramipexole when administered alone.
    Type: Grant
    Filed: August 31, 2020
    Date of Patent: January 10, 2023
    Assignee: CHASE THERAPEUTICS CORPORATION
    Inventors: Thomas N. Chase, Kathleen E. Clarence-Smith
  • Patent number: 11504380
    Abstract: The invention relates to a method of treating cirrhosis which comprises administering to a subject in need thereof lanifibranor or a deuterated derivative thereof.
    Type: Grant
    Filed: November 8, 2019
    Date of Patent: November 22, 2022
    Assignee: INVENTIVA
    Inventors: Guillaume Wettstein, Pierre Broqua, Jean-Louis Junien
  • Patent number: 11400155
    Abstract: Disclosed are methods of treating cancer using a combination of an immunotherapeutic agent, such as, for example, a PD-1, PD-L1 or CTLA-4 checkpoint inhibitor, and a glutamate modulating agent such as riluzole or trigriluzole. Pharmaceutical compositions including the immunotherapeutic agents and glutamate modulating agents are also disclosed.
    Type: Grant
    Filed: May 19, 2017
    Date of Patent: August 2, 2022
    Assignee: Biohaven Therapeutics Ltd.
    Inventor: Vladimir Coric
  • Patent number: 11366121
    Abstract: Research tool assay for identifying a specific modulator of GNAI, compositions and methods of use. The assay includes combining a drug candidate with GNAI and a C-terminal GIV peptide and determining if the drug candidate inhibits GNAI interaction with the C-terminal GIV peptide; and combining the drug candidate with GNAI and a DAPLE peptide and determining if the drug candidate inhibits GNAI interaction with DAPLE peptide. Also provided are compositions and methods of treatment relating to the same.
    Type: Grant
    Filed: February 22, 2018
    Date of Patent: June 21, 2022
    Assignee: The Regents of the University of California
    Inventor: Pradipta Ghosh
  • Patent number: 11324740
    Abstract: A method is provided for using of type-2 dopaminergic receptor agonists, for example, cabergoline, in treatment of eye diseases caused by an elevated level of vascular endothelial growth factor (VEGF), particularly in treatment or prevention of diseases of an eye retina resulting from an increase in permeability of blood vessels and their angiogenesis using cabergoline, a dopaminergic D2 receptor agonist.
    Type: Grant
    Filed: March 31, 2020
    Date of Patent: May 10, 2022
    Inventor: Maciej Oseka
  • Patent number: 11318122
    Abstract: The present invention describes the combination of a 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine or of a pharmaceutically acceptable salt or solvate thereof with fluoxetine or a pharmaceutically acceptable salt or solvate thereof, for use for treating a synucleinopathy such as Parkinson's disease, Lewy body disease, mutations in the glucocerebrosidase gene, or multiple system atrophy.
    Type: Grant
    Filed: April 11, 2018
    Date of Patent: May 3, 2022
    Assignee: CHASE THERAPEUTICS CORPORATION
    Inventors: Thomas N. Chase, Kathleen E. Clarence-Smith
  • Patent number: 11234961
    Abstract: In various embodiments, provided herein are pamoate salts of monoamine Anti-Parkinsons disease agents including rotigotine, ropinirole, pramipexole, selegiline, rasagiline, and safinamide, pharmaceutical composition comprising the same, methods of preparing the same, and methods of using the same. For example, the pamoate salt herein can be characterized by a molar ratio of rotigotine, ropinirole, pramipexole, selegiline, rasagiline, or safinamide to pamoic acid of about 1:1 or about 2:1. The pamoate salt herein can also be crystalline including anhydrous, hydrate or solvate forms, or their polymorphs, or amorphous. The pamoate salts described herein can provide a long acting and/or extended release profile of the monoamine agents for the treatment of Parkinsons disease (PD). Thus, also provided herein are methods of preparing a long acting and/or extended release injectable formulation of the monoamine agents using their respective pamoate salts.
    Type: Grant
    Filed: August 17, 2018
    Date of Patent: February 1, 2022
    Inventor: Zi-Qiang Gu
  • Patent number: 10851114
    Abstract: A compound of formula (I?) wherein R6 is H, C1-6alkyl, —(CH2)pCOOH, —(CH2)pCOOC1-6alkyl, —(CH2)pCONH2, —(CH2)pCONHC1-6alkyl, —(CH2)pCON(C1-6alkyl)2, R7 is as defined for R6; or and R7 taken together with the atoms joining them can form a 6-membered aromatic or non aromatic, saturated or unsaturated, carbocyclic or heteroatom containing (e.g.
    Type: Grant
    Filed: December 10, 2018
    Date of Patent: December 1, 2020
    Assignee: Avexxin AS
    Inventors: Berit Johansen, Marcel Sandberg, Inger-Reidun Aukrust, George Kokotos, Johan Evenäs, Thomas Brimert, Kildahl-Andersen Geir
  • Patent number: 10844026
    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: January 21, 2020
    Date of Patent: November 24, 2020
    Assignees: Biohaven Pharmaceutical Holding Company Ltd., Rutgers, The State University of New Jersey
    Inventors: Garry Robert Smith, Allen B. Reitz, Mark McDonnell, Suzie Chen, Matthew D. Vera, Benjamin E. Blass, Jeffrey Claude Pelletier, Venkata N. Velvadapu, Jay Edward Wrobel
  • Patent number: 10799484
    Abstract: The present invention describes the use of a 5HT3-antagonist, in combination with a 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine, to reduce adverse effects and to facilitate the neuroprotective treatment of a patient suffering from a synucleinopathic disorder to enable a therapeutically effective 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine daily dose without the dose-limiting adverse effects caused by pramipexole when administered alone.
    Type: Grant
    Filed: March 26, 2018
    Date of Patent: October 13, 2020
    Assignee: CHASE THERAPEUTICS CORPORATION
    Inventors: Thomas N. Chase, Kathleen E. Clarence-Smith
  • Patent number: 10774046
    Abstract: Some embodiments of the invention include inventive compounds. Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions (e.g., pharmaceutical compositions) for treating, for example, certain diseases using the compounds. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating (e.g., diseases such as cancer). Further embodiments include methods for making the inventive compounds. Other embodiments include PFKFB4 inhibitors and methods of using the same that can target neoplastic cells, including, such as, mechanisms within those cells that relate to the use of the glycolytic pathway. In other embodiments, small molecule PFKFB4 inhibitors are used to disrupt the kinase domain of PFKFB4 and, in some instances, decrease the glucose metabolism and growth of human cancers.
    Type: Grant
    Filed: October 25, 2018
    Date of Patent: September 15, 2020
    Assignee: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: Sucheta Telang, Jason Chesney, John O. Trent, Joseph A. Burlison, Nagaraju Miriyala
  • Patent number: 10724070
    Abstract: Stable, constitutively expressed, chromosomal fluorescent transcriptional fusions in bacterial pathogens and methods of using the same to screen candidate compounds for anti-bacterial efficacy.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: July 28, 2020
    Assignees: University of Cincinnati, Government of the United States as Represented by the Secretary of the Air Force
    Inventors: Daniel J. Hassett, Shengchang Su, Thomas J. Lamkin, Roland Saldanha
  • Patent number: 10640476
    Abstract: The present invention relates compounds of Formula (A), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological and psychiatric disorders and diseases as well as cancer in humans.
    Type: Grant
    Filed: September 30, 2019
    Date of Patent: May 5, 2020
    Assignee: XW LABORATORIES INC.
    Inventors: Jia-Ning Xiang, Xuesong Xu, Wei Zhou
  • Patent number: 10611730
    Abstract: Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, Also provided herein are pharmaceutical compositions comprising compounds of Formula (I) and methods of using compounds of Formula (I).
    Type: Grant
    Filed: April 28, 2016
    Date of Patent: April 7, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael K. Ameriks, Suchitra Ravula, Devin M. Swanson, Bradley M. Savall
  • Patent number: 10562870
    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: August 4, 2017
    Date of Patent: February 18, 2020
    Assignee: Biohaven Pharmaceutical Holding Company Ltd.
    Inventors: Garry Robert Smith, Allen B. Reitz, Mark Mcdonnell, Suzie Chen, Matthew D. Vera, Benjamin E. Blass, Jeffery Claude Pelletier, Venkata N. Velvadapu, Jay Edward Wrobel
  • 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: 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: 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