Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai Patents (Class 514/183)
  • Patent number: 11026909
    Abstract: A method for amelioriation of, or prophylaxis against, a viral infection comprising administering to a patient in need of treatment a therapeutically effective amount of 5 aminolevulinic acid, optionally with at least one of cucumarin nano, zinc, vitamin C and methylene blue, and compositions thereof. Such compositions may be used for the treatment of coronavirus infections, including the SARS-CoV-2 virus, and/or rhinoviruses.
    Type: Grant
    Filed: December 23, 2020
    Date of Patent: June 8, 2021
    Inventors: Nadimpally Satyavarahala Raju, Venkata Satya Suresh Attili, Nadimpally Neha Varma, Steven Jerome Moore, Cullen Thomas Moore
  • Patent number: 11020496
    Abstract: The present disclosure relates to compositions and methods for enhancing mosquito feeding.
    Type: Grant
    Filed: September 11, 2018
    Date of Patent: June 1, 2021
    Assignee: University of Central Florida Research Foundation, Inc.
    Inventors: Bradley Jay Willenberg, Sudipta Seal, Alexander John Bosak, Alicia Renae Willenberg
  • Patent number: 11013712
    Abstract: A composition comprising doxepin, or a pharmaceutically acceptable salt, or prodrug thereof, and a compound that enhances sleep onset, sleep maintenance or reduces early morning awakenings. These compositions are useful for treating multiple manifestations of insomnia.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: May 25, 2021
    Assignee: Currax Pharmaceuticals LLC
    Inventors: Philip Jochelson, Robert Mansbach, Michael Skinner, Neil B. Kavey
  • Patent number: 11007168
    Abstract: The invention relates to use of the trans-(E) isomer or isomeric mixtures containing specified ratios of the trans-(E) and cis-(Z) isomers of doxepin, metabolites of doxepin, pharmaceutically-acceptable salts of doxepin and prodrugs of the same; compositions containing the same, for the treatment of sleep disorders.
    Type: Grant
    Filed: December 2, 2019
    Date of Patent: May 18, 2021
    Assignees: Currax Pharmaceuticals LLC, ProCom One, Inc.
    Inventors: Susan E. Dubé, Neil B. Kavey
  • Patent number: 11000514
    Abstract: The technical field of the invention is in pharmaceutical compounds and methods. In an aspect, the disclosure provides macrolide compounds suitable for use as antifungal agents, as well as methods for their use and compositions containing the same.
    Type: Grant
    Filed: February 20, 2020
    Date of Patent: May 11, 2021
    Assignee: Duke University
    Inventors: Jonathan A. Covel, Mitchell Mutz, Peter J. Webb, Robert Remme Webb, II
  • Patent number: 10987329
    Abstract: The present invention provides therapeutic combinations of 5-aminolevulinic acid, with at least one of: Vitamin C, curcumin, zinc, and methylene blue for the treatment of coronavirus infections, including the SARS-CoV-2 virus, and/or rhinoviruses. Optionally such compositions may comprise other dietary supplements and one or more pharmaceutically acceptable excipients and also process for preparing it. The composition can also include other antiviral agents.
    Type: Grant
    Filed: July 2, 2020
    Date of Patent: April 27, 2021
    Inventors: Nadimpally Satyavarahala Raju, Venkata Satya Suresh Attili, Nadimpally Neha Varma, Steven Jerome Moore, Cullen Thomas Moore
  • Patent number: 10973934
    Abstract: The present invention relates to the RRR/SSS pair of enantiomers of the of Gd(PCTA-tris-glutaric acid), the single enantiomers of the pair, the pharmaceutically acceptable salts thereof, their amide derivatives, and compositions comprising at least 50% of these compounds.
    Type: Grant
    Filed: August 6, 2019
    Date of Patent: April 13, 2021
    Assignee: BRACCO IMAGING S.P.A.
    Inventors: Roberta Napolitano, Luciano Lattuada, Zsolt Baranyai, Nicole Guidolin, Giuseppe Marazzi
  • Patent number: 10973874
    Abstract: The present disclosure relates to the control of fungal infection of horn-like envelopes covering dorsal and terminal phalanges in humans and animals and related cerebral protrusions in animals as well as keratin comprising material on surfaces of humans and animals. Agents and natural and synthetic formulations and extracts useful for the control of fungal infection of these envelopes and related protrusions and keratin comprising material are also encompassed by the subject disclosure. In an embodiment, the present disclosure teaches the treatment of fungal infection of nails and in particular onychomycosis in humans.
    Type: Grant
    Filed: April 21, 2017
    Date of Patent: April 13, 2021
    Assignee: Hexima Limited
    Inventors: Nicole Louise van der Weerden, Marilyn Anne Anderson
  • Patent number: 10973796
    Abstract: The present disclosure provides methods for treating and/or preventing cardiovascular-related disease and, in particular, a method of blood lipid therapy comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof. In some embodiments, the method comprises lowering high sensitivity CRP (hs-CRP) levels in a subject including, for example, a subject with a HbA1c value of about 5.00%-8.50% or at least about 6.8%.
    Type: Grant
    Filed: October 24, 2017
    Date of Patent: April 13, 2021
    Assignee: Amarin Pharmaceuticals Ireland Limited
    Inventors: Mehar Manku, Ian Osterloh, Pierre Wicker, Rene Braeckman, Paresh Soni
  • Patent number: 10968213
    Abstract: The present invention provides a compound having a lysine-specific demethylase-1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, developmental disorders, particularly diseases having intellectual disability (e.g., autistic spectrum disorders, Rett syndrome, Down's syndrome, Kabuki syndrome, fragile X syndrome, Kleefstra syndrome, neurofibromatosis type 1, Noonan syndrome, tuberous sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, spinocerebellar degeneration (e.g., dentatorubural pallidoluysian atrophy) and Huntington's disease), epilepsy (e.g., Dravet syndrome) or drug dependence, and the like. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Grant
    Filed: June 27, 2019
    Date of Patent: April 6, 2021
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shigemitsu Matsumoto, Yasushi Hattori, Masashi Toyofuku, Shinji Morimoto, Masaki Daini, Takuto Kojima, Tomohiro Kaku, Mitsuhiro Ito
  • Patent number: 10959982
    Abstract: The present invention relates in part a to multiparticulate sprinkle dosage form comprising duloxetine or a pharmaceutically acceptable salt thereof, having higher acid resistance as compared to commercially available delayed release formulations. It further relates to various methods of administering the said multiparticulate sprinkle dosage forms.
    Type: Grant
    Filed: September 13, 2019
    Date of Patent: March 30, 2021
    Assignee: Sun Pharmaceutical Industries Limited
    Inventors: Ravindra Agarwal, Tarun Singhal, Ravi Kochhar
  • Patent number: 10954246
    Abstract: A crystalline form of Mod. I of Formula I: And, a process for the preparation of the crystalline form and a pharmaceutical use of the crystalline form.
    Type: Grant
    Filed: October 11, 2019
    Date of Patent: March 23, 2021
    Assignee: Taizhou EOC Pharma Co., Ltd.
    Inventors: Heting Li, Deqiang Wang, Wei Chang, Hongrui Yu, Xiaoming Zou
  • Patent number: 10954273
    Abstract: Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.
    Type: Grant
    Filed: September 6, 2019
    Date of Patent: March 23, 2021
    Assignee: The Johns Hopkins University
    Inventors: Jun O. Liu, Jingxin Wang, Zufeng Guo, Wei Li, Shridhar Bhat, Manisha Das
  • Patent number: 10953019
    Abstract: A series of substituted fused pentacyclic imidazopyridine and imidazopyridazine derivatives, and analogues thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: March 14, 2018
    Date of Patent: March 23, 2021
    Assignees: UCB Biopharma SRL, Sanofi
    Inventors: Julien Alistair Brown, Daniel Christopher Brookings, Jag Paul Heer, James Andrew Johnson, Zhaoning Zhu
  • Patent number: 10947207
    Abstract: There are provided, inter alia, compounds and methods useful for the treatment of neurological conditions, such as neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.
    Type: Grant
    Filed: August 4, 2017
    Date of Patent: March 16, 2021
    Assignee: The Regents of the University of California
    Inventors: Mohammad Parvez Alam, Varghese John, Patricia Spilman, Kanagasabai Vadivel
  • Patent number: 10919894
    Abstract: Compounds of formula (I): wherein: R1 is butoxy or methylbutoxy; R2 is a group having the structure: where n is an integer having a value of five; Het is a six-membered saturated heterocycle containing five carbon atoms and one nitrogen atom, wherein Het is attached to the —(CH2)n— moiety at the carbon 4 position of the heterocycle; and R3 is hydrogen; or pharmaceutically acceptable salts thereof; and their use as vaccine adjuvants and in the treatment of various disorders.
    Type: Grant
    Filed: January 17, 2020
    Date of Patent: February 16, 2021
    Assignee: GLAXOSMITHKLINE BIOLOGICALS SA
    Inventors: Helene G. Bazin-Lee, Yufeng Li
  • Patent number: 10888549
    Abstract: Methods for preventing or treating subjects having cancer based on the identification of pharmaceutical agents that target cancer stem cells (CSCs) have been identified. These methods include administering to the subject an effective amount of a COX2 inhibitor and an effective amount of a YAP1 inhibitor. In addition, methods of enhancing chemotherapeutic responses in cancer patients have been discovered and are described herein.
    Type: Grant
    Filed: March 7, 2017
    Date of Patent: January 12, 2021
    Assignee: The Johns Hopkins University
    Inventors: Mohammad O. Hoque, David Sidransky, Akira Oki
  • Patent number: 10875840
    Abstract: A method for catalytically converting a dihydrotetrazine 1 into a tetrazine 2, wherein one R group on the dihydrotetrazine 1 is a substituted or unsubstituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, carbonyl, or heteroatom-containing group, and the other R group is selected from the group consisting of H and substituted or unsubstituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, carbonyl,- or heteroatom-containing groups; 1, 2 wherein the method comprises oxidizing dihydrotetrazine 1 in a reaction medium in the presence of a catalyst and a stoichiometric oxidant.
    Type: Grant
    Filed: December 15, 2016
    Date of Patent: December 29, 2020
    Assignee: UNIVERSITY OF DELAWARE
    Inventors: Joseph Fox, Xinqiao Jia, Will Trout, Joel Rosenthal, Han Zhang, Yinzhi Fang, Colin Thorpe, Shuang Liu, Yixin Xie
  • Patent number: 10857120
    Abstract: The present disclosure provides a method for the treatment of Parkinson's disease comprising simultaneously or sequentially administering to a patient in need of treatment of Parkinson's disease a dosage form comprising (i) levodopa in an amount ranging from 50 mg to 300 mg, (ii) carbidopa in an amount ranging from 25 mg to 150 mg or a therapeutically equivalent amount of another aromatic amino acid decarboxylase inhibitor, and (iii) entacapone in an amount ranging from 50 mg to 300 mg, wherein the proportion of entacapone to carbidopa in said dosage form ranges from 0.3:1.0 to 3.2:1.0 by weight, a moderately potent COMT inhibitor in an amount ranging from 25 mg to 200 mg, wherein the proportion of said COMT inhibitor to carbidopa in said dosage form ranges from 0.16:1.0 to 3.08:1.0 by weight, or a highly potent COMT Inhibitor in an amount ranging from 1 mg to 100 mg, wherein the proportion of said COMT inhibitor to carbidopa in said dosage form ranges from 0.006:1.0 to 1.54:1.0 by weight.
    Type: Grant
    Filed: October 2, 2014
    Date of Patent: December 8, 2020
    Assignee: ORION CORPORATION
    Inventors: Juha Rouru, Mikko Kuoppamäki, Juha Ellmen, Pekka Männistö
  • Patent number: 10858306
    Abstract: The present invention concerns a method of synthesizing a iodo- or astatoarene comprising the reaction of a diaryliodonium compound with a iodide or astatide salt, respectively. The invention also relates to said iodo- or astatoarene and diaryliodonium compound as such. The invention also concerns a method of synthesizing a iodo- or astatolabelled biomolecule and/or vector using said iodo- or astatoarene.
    Type: Grant
    Filed: April 9, 2020
    Date of Patent: December 8, 2020
    Assignees: INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE (INSERM), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE NANTES, UNIVERSITE D'ANGERS, THE GOVERNMENT OF THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
    Inventors: François Guerard, Jean-François Gestin, Martin W. Brechbiel, Yong-Sok Lee
  • Patent number: 10844076
    Abstract: The instant disclosure relates to (among other things) compounds that are derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine. The compounds provided possess unique effects and differences over other phenyltriazines known in the art.
    Type: Grant
    Filed: November 6, 2018
    Date of Patent: November 24, 2020
    Assignee: Nektar therapeutics
    Inventors: Pankaj Sharma, Vijay Kumar Khatri, Xuyuan Gu, Yuan Song, Michael Lixin Shen, Jennifer Riggs-Sauthier, Neel K. Anand, Antoni Kozlowski, Aleksandrs Odinecs, Timothy A. Riley, Zhongxu Ren, YongQi Mu, Xiaoming Shen, Xuejun Yuan, Natalia Aurrecoechea, Donogh John Roger O'Mahony, Bo-Liang Deng
  • Patent number: 10842791
    Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a quinazoline structure or a quinoline structure which function as dual inhibitors of EGFR proteins and PI3K proteins, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Grant
    Filed: December 3, 2018
    Date of Patent: November 24, 2020
    Assignee: The Regents of the University of Michigan
    Inventors: Christopher Emil Whitehead, Judith S. Leopold
  • Patent number: 10842784
    Abstract: Described are compositions comprising imino sugar acids for the treatment of energy utilization disease (e.g. metabolic syndrome, including any disease or disorder associated therewith, for example central obesity, elevated levels of triglycerides and diabetes, including type 1 diabetes, type 2 diabetes and insulin resistance), processes for producing said compositions from various plant sources, together with various products, compounds, compositions, medical uses and methods based thereon.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: November 24, 2020
    Assignee: Vida Pharma Limited
    Inventors: Robert James Nash, Francis Xavier Wilson, Graeme Horne
  • Patent number: 10823738
    Abstract: Disclosed herein are methods for treating subjects with breast cancer, comprising determining a therapeutic regimen for cancer by measuring the level (amount) of proteins of one or more biomarkers. Also disclosed are methods of treating a subject with breast cancer by predicting or assessing a therapeutic outcome for subject.
    Type: Grant
    Filed: December 7, 2016
    Date of Patent: November 3, 2020
    Assignee: George Mason Research Foundation, Inc.
    Inventors: Emanuel Petricoin, Julia Wulfkuhle
  • Patent number: 10815244
    Abstract: The present disclosure relates to compounds having an improved solubility thereby increasing their bioavailability, lower dosages, etc. The target compounds, may include but are not limited to, macrophage migration inhibitory factor (MIF) inhibitors, epidermal growth factor receptor (EGRF) inhibitors, kinase inhibitors and prodrugs of alpha4 beta1 and alpha4 beta7 integrin antagonists.
    Type: Grant
    Filed: August 26, 2019
    Date of Patent: October 27, 2020
    Assignee: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
    Inventor: Achyutharao Sidduri
  • Patent number: 10765653
    Abstract: The present invention provides dietary formulations comprising polyunsaturated fatty acids and vitamin E. The present invention further provides methods of treating various conditions, generally involving administering to an individual in need thereof an effective amount of a subject dietary formulation.
    Type: Grant
    Filed: July 9, 2019
    Date of Patent: September 8, 2020
    Assignee: Children's Hospital & Research Center Oakland
    Inventor: Claudia R. Morris
  • Patent number: 10758510
    Abstract: The invention relates to use of the cis-(Z) isomer or isomeric mixtures containing specified ratios of the cis-(Z) and trans-(E) isomers of doxepin, metabolites of doxepin, pharmaceutically-acceptable salts of doxepin and prodrugs of the same; compositions containing the same, for the treatment of sleep disorders
    Type: Grant
    Filed: April 8, 2019
    Date of Patent: September 1, 2020
    Assignees: Currax Pharmaceuticals LLC, ProCom One, Inc.
    Inventors: Susan E. Dubé, Neil B. Kavey
  • Patent number: 10758468
    Abstract: The present invention relates to a mixture comprising (i) one or a plurality of 1,2-alkane diols with 5 through 8 carbon atoms and (ii) one or a plurality of ammonium-, sodium- or potassium-Ralk-sarcosinates, wherein the structural element Ralk represents alkanoyl, alkenoyl or alkadienoyl with 12 through 22 carbon atoms, and optionally (iii) one or a plurality of sodium- or potassium-C10-C16-alkyl-sulfoacetates. The invention further relates to particular compositions and cosmetic preparations, in particular body care products, containing said mixture or composition and methods of production thereof. The present invention further relates to the use of said mixture as solubilizer and for increasing the transparency or decreasing the turbidity of a preparation containing one or a plurality of further organic substances.
    Type: Grant
    Filed: December 29, 2015
    Date of Patent: September 1, 2020
    Assignee: Symrise AG
    Inventors: Martina Issleib, Jürgen Claus, William Johncock, Rolf Ohrmann, Martina König
  • Patent number: 10729669
    Abstract: The invention provides compositions and methods to treat a hyperproliferative disorder with phenyl butyric acid (PBA) or a pharmaceutically acceptable salt thereof and an anti-cancer composition.
    Type: Grant
    Filed: July 26, 2016
    Date of Patent: August 4, 2020
    Assignee: University of Iowa Research Foundation
    Inventors: Michael K. Schultz, Somya Kapoor, Andrean L. Simons-Burnett
  • Patent number: 10722485
    Abstract: In various embodiments, the present invention provides compositions and methods for treating and/or preventing cardiovascular-related diseases in subject in need thereof.
    Type: Grant
    Filed: April 15, 2019
    Date of Patent: July 28, 2020
    Assignee: Amarin Pharmaceuticals Ireland Limited
    Inventors: Ian Osterloh, Pierre Wicker, Rene Braeckman, Paresh Soni, Mehar Manku
  • Patent number: 10716849
    Abstract: Methods for priming of vaccines including administering to a patient a composition including one or more integrin activating compounds capable of adjuvanting an antigen and capable of adjuvanting one or more antigens contained in a vaccine preparation.
    Type: Grant
    Filed: April 25, 2019
    Date of Patent: July 21, 2020
    Assignee: 7 Hills Pharma LLC
    Inventors: Darren G. Woodside, Peter Vanderslice, Upendra K. Marathi
  • Patent number: 10709715
    Abstract: Disclosed herein are methods of treating pulmonary hypertension, including pulmonary arterial hypertension, by administering to a patient in need thereof an effective amount of temozolomide, optionally in conjunction with one or more additional therapeutic agents. Compositions and kits including temozolomide for use in treating pulmonary hypertension, including pulmonary arterial hypertension, are also disclosed.
    Type: Grant
    Filed: December 3, 2018
    Date of Patent: July 14, 2020
    Assignee: Cipla Limited
    Inventors: Geena Malhotra, Kalpana Joshi, Jeevan Ghosalkar
  • Patent number: 10709780
    Abstract: Compositions including one or more antigens and one or more integrin activating compounds capable of adjuvanting the one or more antigens contained and increasing an immune response to the one or more antigen in a vaccine preparation.
    Type: Grant
    Filed: April 25, 2019
    Date of Patent: July 14, 2020
    Assignee: 7 Hills Pharma LLC
    Inventors: Darren G. Woodside, Peter Vanderslice, Upendra K. Marathi
  • Patent number: 10689708
    Abstract: In one aspect, provided herein are methods for predicting the responsiveness of DLBCL patients to treatment with lenolidomide or Compound A; or a stereoisomer thereof; or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate thereof; or a polymorph thereof utilizing biomarkers or classifiers that correlate with responsiveness to one of these drugs. In another aspect, provided herein are methods for treating a DLBCL patient determined to be responsive to treatment with lenolidomide or Compound A; or a stereoisomer thereof; or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate thereof; or a polymorph thereof utilizing biomarkers or classifiers (or output thereof) that correlate with responsiveness to one of these drugs.
    Type: Grant
    Filed: September 22, 2016
    Date of Patent: June 23, 2020
    Assignee: CELGENE CORPORATION
    Inventors: Matthew William Burnell Trotter, Alberto Risueno Perez, Michael Pourdehnad, Anita Gandhi, Patrick Hagner
  • Patent number: 10689374
    Abstract: Pyrimidine-thiazolidinone derivatives may be used for preventing or treating diseases in humans or animals, and have demonstrated efficacy specifically in treating type-2 diabetes. Methods of synthesizing the pyrimidine-thiazolidinone derivatives, described herein, can provide high yields in a short time and with high purity. The pyrimidine-thiazolidinone derivatives demonstrate improved hypoglycemic activity compared to most anti-diabetic drugs currently available.
    Type: Grant
    Filed: July 12, 2019
    Date of Patent: June 23, 2020
    Assignee: United Arab Emirates University
    Inventors: Abdu Adem, Shaikha S. Al Neyadi, Ibrahim M. Abdou, Alaa A. Salem, Naheed Amir
  • Patent number: 10675271
    Abstract: The present invention pertains to specific clonidine and/or clonidine derivatives for use in the prevention and/or treatment of adverse side effects of alkylating agent chemotherapy, other than those resulting from mucosal inflammation. It also pertains to the use of this clonidine and/or clonidine derivative for the manufacture of a pharmaceutical composition intended to prevent and/or alleviate the adverse side effects of alkylating agent chemotherapy, other than those resulting from mucosal inflammation. This invention is further directed to a kit comprising: (a) a clonidine and/or clonidine derivative, and (b) at least one alkylating chemotherapeutic agent, as a combined preparation for simultaneous, separate or sequential use in the treatment of cancer.
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: June 9, 2020
    Assignee: MONOPAR THERAPEUTICS, INC.
    Inventors: Bérangère Vasseur-Demarcy, Pierre Attali
  • Patent number: 10669289
    Abstract: Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmune disorder or hematological malignancies.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: June 2, 2020
    Assignee: MERCK PATENT GMBH
    Inventors: Markus Klein, Oliver Schadt, Philipp Haselmayer, Mireille Krier
  • Patent number: 10662191
    Abstract: Derivatives of N,N-diethyl-N?-phenyl-piperazine, a silent agonist of the mammalian ?7 nicotinic acetylcholine receptor, are provided. These silent agonists control the desensitization state of the receptor. Further provided are pharmaceutical compositions that allow the administration of the silent agonists of the disclosure to a subject animal or human in need of treatment for a pathological condition arising from such as inflammation. The novel silent agonists also may be co-administered to a patient simultaneously or consecutively with a type II positive allosteric modulator to modulate the activity of the receptor.
    Type: Grant
    Filed: October 14, 2016
    Date of Patent: May 26, 2020
    Assignee: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION INC.
    Inventors: Nicole Alana Horenstein, Roger Lee Papke, Marta Quadri
  • Patent number: 10654843
    Abstract: The present disclosure provides compounds that are Large Multifunctional Protease 7 (LMP7) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of LMP7. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: June 18, 2015
    Date of Patent: May 19, 2020
    Assignee: Principia Biopharma Inc.
    Inventors: Timothy Owens, Kenneth Albert Brameld
  • Patent number: 10647679
    Abstract: This disclosure relates to tetrahydroisoquinolines, salts, and derivatives useful for managing mental or cognitive diseases or conditions of the brain or central nervous system. In certain embodiments, the disclosure relates to compounds and compositions having formula I: prodrugs, esters, or salts thereof, wherein the substituents are described herein.
    Type: Grant
    Filed: March 15, 2016
    Date of Patent: May 12, 2020
    Assignee: Emory University
    Inventors: Katie L. Strong, David Menaldino, Dennis C. Liotta, Stephen F. Traynelis, Rose M. Freel, Matthew Epplin
  • Patent number: 10647699
    Abstract: The present invention relates to compounds of the general formula (I) in which Q, V, T, W, X, Y and A have the meanings given in the description—and to their use for controlling animal pests.
    Type: Grant
    Filed: February 6, 2017
    Date of Patent: May 12, 2020
    Assignee: Bayer CropScience Aktiengesellschaft
    Inventors: Johannes-Rudolf Jansen, Markus Heil, Reiner Fischer, David Wilcke, Matthieu Willot, Kerstin Ilg, Sascha Eilmus, Peter Lösel, Wolfram Andersch
  • Patent number: 10603308
    Abstract: Use of allosteric modulators and/or gaboxadol for the treatment of epileptic disorders in a subject in need thereof.
    Type: Grant
    Filed: June 20, 2019
    Date of Patent: March 31, 2020
    Assignee: OVID THERAPEUTICS INC.
    Inventor: Matthew During
  • Patent number: 10597368
    Abstract: The present invention provides, in certain aspects, novel syringolin analogues, In certain embodiments, the compounds of the invention are proteasome inhibitors, In other embodiments, the compounds treat or prevent a cancer such as, but not limited to, leukemia in a subject.
    Type: Grant
    Filed: May 7, 2016
    Date of Patent: March 24, 2020
    Assignee: BROWN UNIVERSITY
    Inventors: Jason K. Sello, Kyle A. Totaro
  • Patent number: 10588907
    Abstract: The present disclosure provides compositions and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The compositions and methods of use are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: March 17, 2020
    Assignees: KURA ONCOLOGY, INC., THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Jolanta Grembecka, Tomasz Cierpicki, Dmitry Borkin, Jonathan Pollock, Liansheng Li, Tao Wu, Jun Feng, Pingda Ren, Yi Liu
  • Patent number: 10583107
    Abstract: A method for treating benign prostatic hyperplasia (BPH), prostatitis, and/or prostate cancer, including the step of administering an isothiocyanate functional surfactant to a patient affected by benign prostatic hyperplasia, prostatitis, and/or prostate cancer.
    Type: Grant
    Filed: August 13, 2019
    Date of Patent: March 10, 2020
    Assignee: The William M. Yarbrough Foundation
    Inventor: Michael E. Silver
  • Patent number: 10568320
    Abstract: The present invention provides novel compositions and methods for using the insect neuromodulator tyramine and/or one or more derivatives thereof delivered to insect populations to control certain aspects of such populations. The amount of tyramine and/or one or more derivatives thereof delivered on a per insect basis is significantly greater than a naturally-occurring amount of tyramine normally found in insects and causes deleterious effects including mortality of certain insect life forms and disruption of the reproductive capacity of others in the population.
    Type: Grant
    Filed: February 28, 2018
    Date of Patent: February 25, 2020
    Assignees: The United States of America, as represented by the Secretary of Agriculture, Foresight Science & Technology Inc.
    Inventors: Robert K. Vander Meer, Satya P. Chinta
  • Patent number: 10561674
    Abstract: The present invention discloses processes for the preparation of phospholipid-enriched dairy products as nutraceuticals for the formulation of functional foods, the processes include the steps of: combining a non-dairy-based PL-containing material, having phosphatidylserine (PS) and/or phosphatidic acid (PA) in the PL-containing material, wherein the PS and/or PA is derived in part from an enzymatically-processed lecithin as a PS-calcium and/or -magnesium salt and/or a PA-calcium and/or-magnesium salt via transphosphatidylation with phospholipase D in the presence of L-serine and a calcium and/or magnesium salt, with water and an oil component to form a paste; removing an excess amount of the water from the paste to form a PL-oil solution; and mixing the PL-oil solution with a dairy component, thereby obtaining a PL-enriched dairy product. Alternatively, the PL-oil solution has a weight-to-weight (w-w) concentration of at least about 0.01% of a residual amount of the water to the PL-containing material.
    Type: Grant
    Filed: August 8, 2016
    Date of Patent: February 18, 2020
    Assignee: Lipogen Ltd.
    Inventors: David Rutenberg, Ilan Perry
  • Patent number: 10561460
    Abstract: Apparatus, systems, and methods for achieving thermally-induced renal neuromodulation by intravascular access are disclosed herein. One aspect of the present application, for example, is directed to apparatuses, systems, and methods that incorporate a treatment device comprising an elongated shaft. The elongated shaft is sized and configured to deliver a thermal element to a renal artery via an intravascular path. Thermally-induced renal neuromodulation may be achieved via direct and/or via indirect application of thermal energy to heat or cool neural fibers that contribute to renal function, or of vascular structures that feed or perfuse the neural fibers.
    Type: Grant
    Filed: July 19, 2017
    Date of Patent: February 18, 2020
    Assignee: MEDTRONIC ARDIAN LUXEMBOURG S.A.R.L.
    Inventors: Andrew Wu, Benjamin J. Clark, Denise Zarins, Erik Thai
  • Patent number: 10525009
    Abstract: The present invention provides improved formulations of 6-mercaptopurine that exhibit better bioavailability and faster dissolution than previous formulations.
    Type: Grant
    Filed: June 17, 2016
    Date of Patent: January 7, 2020
    Assignee: Hadasit Medical Research Services and Development Ltd.
    Inventors: Itzhak E. Lerner, Moshe Flashner-Barak, Erwin v Achthoven, Hans Keegstra, Ruud Smit
  • Patent number: 10526341
    Abstract: Described herein are thienopyrimidine compounds of Formula (I), and pharmaceutically acceptable salts, and pharmaceutical compositions thereof. Also provided are methods and kits involving the thienopyrimidine compounds or compositions for treating or preventing proliferative diseases such as cancers (e.g., brain tumors such as DIPGs) in a subject. The invention further provides an embryonic stem cell-based tumor cell model, which can be used for drug screening and disease target identification.
    Type: Grant
    Filed: November 19, 2015
    Date of Patent: January 7, 2020
    Assignee: Memorial Sloan-Kettering Cancer Center
    Inventors: Viviane Tabar, Kosuke Funato