Tricyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/220)
  • Patent number: 11391740
    Abstract: This document provides methods and materials involved in identifying and/or treating mammals having a treatment-resistant prostate cancer (e.g., an enzalutamide-resistant, castration-resistant prostate cancer). For example, methods and materials for identifying a mammal (e.g., a human) having treatment-resistant prostate cancer (e.g., an enzalutamide-resistant, castration-resistant prostate cancer) as having an elevated level of one or more polypeptides (e.g., one or more of a CXXC5, a CXXC4, a TET2, an ID1, an ID3, and/or a PFN2 polypeptide) in treatment-resistant prostate tissue are provided. Methods and materials for administering one or more targeted therapies with or without one or more chemotherapeutic agents to a mammal having treatment-resistant prostate cancer identified as having an elevated level of one or more polypeptides (e.g., one or more of a CXXC5, a CXXC4, a TET2, an ID1, an ID3, and/or a PFN2 polypeptide) in treatment-resistant prostate tissue also are provided.
    Type: Grant
    Filed: May 19, 2020
    Date of Patent: July 19, 2022
    Assignee: Mayo Foundation for Medical Education and Research
    Inventor: Haojie Huang
  • Patent number: 11369583
    Abstract: Provided are a long-acting prodrug of Rasagiline, which has application in the treatment of Central Nervous System diseases such as Parkinson's disease, preparation method and use thereof. The long-acting prodrug of Rasagiline has a structure of formula (I), wherein T is absent, or T is selected from each of R1 and R2 is independently selected from H, D, and alkyl; W is absent, or W is selected from (CH2)n, wherein n is an integer selected from 1 to 15; X is absent, or X is selected from (CH2)m, wherein m is an integer selected from 1 to 10; Y is absent, or Y is selected from —C(?O)NH—, —NHC(?O)—; R3 is selected from substituted or unsubstituted C1-C30 alkyl, substituted or unsubstituted C2-C30 alkenyl, substituted or unsubstituted C2-C30 alkynyl, substituted or unsubstituted C3-C30 cycloalkyl, cholane aliphatic group, —R3a—C(?O)O—R3b, —R3a—OC(?O)—R3b, —R3a—C(?O)NH—R3b, —R3a—NHC(?O)—R3b, —R3a—S(?O)1-2O—R3b and —R3a—OS(?O)1-2—R3b.
    Type: Grant
    Filed: August 27, 2018
    Date of Patent: June 28, 2022
    Assignee: GUANGZHOU HENOVCOM BIOSCIENCE CO. LTD
    Inventors: Jiancun Zhang, Deyao Li, Yiqian Zhou, Yiwu Wu
  • Patent number: 11324732
    Abstract: The disclosure is directed to methods of treating dyskinesia in cerebral palsy in human patients using deutetrabenazine and its active metabolites.
    Type: Grant
    Filed: December 13, 2019
    Date of Patent: May 10, 2022
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Juha-Matti Savola, Mark Forrest Gordon, Frank Schneider
  • Patent number: 11273158
    Abstract: The present invention relates to methods of treating schizophrenia using a combination of aripiprazole, aripiprazole lauroxil, and a nanoparticle dispersion of aripiprazole lauroxil.
    Type: Grant
    Filed: March 4, 2019
    Date of Patent: March 15, 2022
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Lisa L. von Moltke, Peter J. Weiden, Marjie L. Hard
  • Patent number: 11267822
    Abstract: The present disclosure provides compounds represented by Formula (I): Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, Y, ?, Ar, W, L, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I)I for use to treat a condition or disorder responsive to inhibition and/or degradation of BET bromodomains such as cancer.
    Type: Grant
    Filed: September 12, 2018
    Date of Patent: March 8, 2022
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Weiguo Xiang, Fuming Xu, Longchuan Bai, Ester Fernandez-Salas, Donna McEachern
  • Patent number: 11241441
    Abstract: Formulations of lixivaptan, and methods of using the same, are provided for the treatment of polycystic disease.
    Type: Grant
    Filed: June 8, 2018
    Date of Patent: February 8, 2022
    Assignee: PALLADIO BIOSCIENCES, INC.
    Inventor: Lorenzo Pellegrini
  • Patent number: 11173132
    Abstract: Methods, compositions, and devices for transdermally administering an active agent such as memantine are provided.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: November 16, 2021
    Assignee: Corium, Inc.
    Inventors: Eun Soo Lee, Parminder Singh, Appala Sagi, Amit K. Jain
  • Patent number: 11155555
    Abstract: The invention relates to new quinoxaline, quinoline and quinazolinone derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: September 22, 2016
    Date of Patent: October 26, 2021
    Assignee: Janssen Pharmaceutica NV
    Inventors: Patrick Rene Angibaud, Diego Fernando Domenico Broggini, Helene France Solange Colombel, Filip Albert C Cuyckens, Steven Anna Hostyn, Russell Mark Jones, Olivier Alexis Georges Querolle, Wim Vermeulen
  • Patent number: 11141388
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: November 24, 2020
    Date of Patent: October 12, 2021
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 11090300
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: March 18, 2020
    Date of Patent: August 17, 2021
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 11066419
    Abstract: The present invention relates to 1H-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into tissue cells.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: July 20, 2021
    Assignee: Frequency Therapeutics, Inc.
    Inventors: Christopher Loose, Bradley Tait, Rajesh Manchanda, Will Mclean
  • Patent number: 11046709
    Abstract: The present disclosure provides fused 1,4-diazepines represented by Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, E, R1, R2, R3, R4, R5, and Ar are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds having Formula (I) to treat diseases, conditions, or disorders responsive to inhibition of BET bromodomain proteins such as cancer.
    Type: Grant
    Filed: February 2, 2018
    Date of Patent: June 29, 2021
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Jiantao Hu, Fuming Xu
  • Patent number: 11034697
    Abstract: The present disclosure relates to novel processes for the preparation of short acting benzodiazepines as well as to novel intermediates in this process. More particularly the disclosure relates to processes and intermediates for preparation of Methyl 3-[(4S)-8-bromo-1-methyl-6-(pyridin-2-yl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propanoate, commonly known as Remimazolam. The present disclosure also relates to solid state forms of Remimazolam salts, processes for the preparation thereof, pharmaceutical formulations/compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: February 8, 2018
    Date of Patent: June 15, 2021
    Assignee: WATSON LABORATORIES INC.
    Inventors: Dolitzky Ben-Zion, Mendelovici Marioara, Bodkhe Arjun Rajaram, Mane Ganesh Shivaji, Samala Rajamouli Srihari, Joshi Ashutosh Vijay, Parven Kumar Luthra, Amit Singh, Anantha Rajmohan Muthusamy
  • Patent number: 11007189
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: March 23, 2020
    Date of Patent: May 18, 2021
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 10988459
    Abstract: The invention provides novel compounds having the general formula I: wherein R1, X, Z1, L, n, the A ring, the B ring, and the C ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: July 1, 2016
    Date of Patent: April 27, 2021
    Assignee: Genentech, Inc.
    Inventors: Snahel Patel, Gregory Hamilton, Craig Stivala, Huifen Chen, Guiling Zhao
  • Patent number: 10966974
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: March 18, 2020
    Date of Patent: April 6, 2021
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 10966999
    Abstract: Provided herein are the 3?3? cyclic phosphonate dinucleotides of general formula J, their pharmaceutically acceptable salts, a pharmaceutical composition containing them and combinations of said substances and other medicaments or pharmaceuticals. The disclosure also relates to the use of said compounds for the treatment or prevention of diseases or conditions modifiable by STING protein modulation, such as cancer or viral, allergic and inflammatory diseases. In addition, these substances can be used as adjuvants in vaccines.
    Type: Grant
    Filed: December 19, 2018
    Date of Patent: April 6, 2021
    Assignee: INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ASCR, V.V.I.
    Inventors: Gabriel Birkus, Ondrej Pav, Tomas Jandusik, Ivan Rosenberg, Radim Nencka
  • Patent number: 10945973
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: August 3, 2020
    Date of Patent: March 16, 2021
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 10925967
    Abstract: The present application provides bifunctional compounds of Formula (X): or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for Bruton's tyrosine kinase (BTK). The present application also relates to methods for the targeted degradation of BTK through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BTK which can be utilized in the treatment of disorders modulated by BTK.
    Type: Grant
    Filed: November 22, 2017
    Date of Patent: February 23, 2021
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Dennis Dobrovolsky, Hai-Tsang Huang
  • Patent number: 10913752
    Abstract: The present invention provides bivalent inhibitors of BET bromodomains, such as compounds of Formulae (I), (II), (III), (IV), (V), and (VI). Some bromdomain-containing proteins (e.g., BRD4) have a tandem bromodomain primary structure comprising more than one bromodomain binding site (e.g., BRD4 comprises BD1 and BD2). Bivalent inhibitors of BET bromodomains provided herein can target bromodomains through advantageous multivalent interactions, and can therefore can be to treat diseases or conditions associated with bromodomain-containing proteins. The present also provides pharmaceutical compositions and kits comprising the inventive compounds, as well as methods of using the inventive compounds.
    Type: Grant
    Filed: November 23, 2016
    Date of Patent: February 9, 2021
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: James E. Bradner, Jun Qi, Minoru Tanaka, Justin M. Roberts
  • Patent number: 10894047
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: March 20, 2020
    Date of Patent: January 19, 2021
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 10894046
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: March 17, 2020
    Date of Patent: January 19, 2021
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 10874664
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: March 19, 2020
    Date of Patent: December 29, 2020
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 10874665
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: March 19, 2020
    Date of Patent: December 29, 2020
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 10874663
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: March 17, 2020
    Date of Patent: December 29, 2020
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 10864209
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: March 20, 2020
    Date of Patent: December 15, 2020
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 10836764
    Abstract: The present invention relates to compounds of Formula A and pharmaceutical compositions thereof that modulate the activity of the 5-HT2C receptor.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: November 17, 2020
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Graeme Semple, Albert S. Ren, Thomas O. Schrader, Michelle Kasem, Xiuwen Zhu
  • Patent number: 10807973
    Abstract: New compounds and a method of treating a retinal disease that leads to photoreceptor loss or outer-retina degeneration, including administering compound of the formula (I) or a pharmaceutically acceptable salt, a racemic mixture, a corresponding enantiomer or, if applicable, a corresponding diastereomer thereof, wherein: A is a 5-oxazolyl residue or a pyridine-4-yl residue, R1 is selected from the group consisting of fluoro, chloro and methoxy; B is selected from the group consisting of a residue of formula (II), (III) and (IV) wherein, “*” denotes the point of attachment to the remainder of the molecule, and R2, R2?, R2?, R3, R3?, R3?, R4, R4?, R4?, R5, R5? and R5? are independently selected from the group consisting of hydrogen, a linear or branched alkyl having 1 to 4 carbon atoms, trifluoromethyl, 2,2,2-trifluoroethyl, methylsulfanyl, ethylsulfanyl, methylsulfonyl, ethylsulfonyl, difluoromethoxy, trifluoromethoxy, fluoro, bromo, chloro, methoxy, ethoxy, propoxy, butoxy, hydroxy and amino.
    Type: Grant
    Filed: December 28, 2018
    Date of Patent: October 20, 2020
    Assignee: ENDOGENA THERAPEUTICS, INC.
    Inventors: Matthias Steger, Alex Mueller, Bernhard Fasching, Daphna Mokady
  • Patent number: 10799511
    Abstract: The present invention includes compounds, compositions and methods for reducing or ameliorating mortality and/or morbidity due to chlorine inhalation.
    Type: Grant
    Filed: August 17, 2018
    Date of Patent: October 13, 2020
    Assignee: The Regents of the University of Colorado, a body corporate
    Inventor: Livia A. Veress
  • Patent number: 10786498
    Abstract: The present invention relates to a pharmaceutical composition comprising a combination of trazodone or a salt thereof, and gabapentin or a salt or prodrug thereof, said combination having a synergistic effect in the treatment of pain.
    Type: Grant
    Filed: October 17, 2016
    Date of Patent: September 29, 2020
    Assignee: AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.
    Inventors: Beatrice Garrone, Lucia Durando, Fabrizio Calisti
  • Patent number: 10772894
    Abstract: The invention comprises methods of modulating the complement cascade in a mammal and for treating and/or preventing diseases and disorders associated with the complement pathway by administering a compound of Formula I or Formula II, such as, for example, 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 26, 2018
    Date of Patent: September 15, 2020
    Assignee: Resverlogix Corp.
    Inventors: Ewelina B. Kulikowski, Dean E. Gilham, Sylwia Wasiak, Christopher R. A. Halliday, Henrik C. Hansen
  • Patent number: 10722479
    Abstract: Described are dimethoxyphenyl inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: February 17, 2016
    Date of Patent: July 28, 2020
    Assignee: AUSPEX PHARMACEUTICALS, INC.
    Inventor: Chengzhi Zhang
  • Patent number: 10716792
    Abstract: The present inventive concept describes a method for treating the neurovascular disruption underlying Epileptic Seizures and other traits of Epilepsy and Infantile Spasms by improving the neurophysiological environment and then enabling by sustained sedation a biomechanism of glial cells for neuronal repairs.
    Type: Grant
    Filed: November 27, 2019
    Date of Patent: July 21, 2020
    Inventors: Gary Aaron Howard, Debora Zucco Sassi Yonezawa Siviglia
  • Patent number: 10695355
    Abstract: Described herein are methods for the treatment of a human subject who has had a stroke by administering to the subject a pharmaceutical composition including an antagonist of the P2X4 receptor. The antagonist of the P2X4 receptor can be administered in the acute phase of stroke, optionally in combination with a thrombolytic therapeutic or a procedure on the subject involving a clot-removal device.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: June 30, 2020
    Assignees: UNIVERSITY OF CONNECTICUT, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
    Inventors: Bruce Liang, Rajkumar Verma, Kenneth A. Jacobson
  • Patent number: 10688047
    Abstract: Physically and chemically stable oral liquid formulations of Givinostat (Diethyl-[6-(4-hydroxycarbamoyl-phenylcarbamoyloxymethyl)-naphthalen-2-yl-methyl]-ammonium chloride) are disclosed, together with methods for the preparation thereof. Such oral formulations are in the form of aqueous suspensions and contain Givinostat and/or pharmaceutically acceptable salts and/or derivatives thereof, at least a wetting agent and/or at least a density-imparting agent. Such formulations are suitable for oral administration for systemic therapeutic action.
    Type: Grant
    Filed: October 28, 2016
    Date of Patent: June 23, 2020
    Assignee: ITALFARMACO SPA
    Inventors: Giuseppe Colombo, Roberta Artico, Paolo Mascagni, Maria Valmen Monzani, Silvia Puccianti
  • Patent number: 10675258
    Abstract: Provided herein are pharmaceutical compositions and formulations comprising mixed salts of gamma-hydroxybutyrate (GHB). Also provided herein are methods of making the pharmaceutical compositions and formulations, and methods of their use for the treatment of sleep disorders such as apnea, sleep time disturbances, narcolepsy, cataplexy, sleep paralysis, hypnagogic hallucination, sleep arousal, insomnia, and nocturnal myoclonus.
    Type: Grant
    Filed: December 21, 2018
    Date of Patent: June 9, 2020
    Assignee: Jazz Pharmaceuticals Ireland Limited
    Inventors: Clark P. Allphin, Michael DesJardin
  • Patent number: 10676484
    Abstract: The invention provides compositions, methods, and kits for the treatment of acute myeloid leukemia in a subject.
    Type: Grant
    Filed: October 17, 2017
    Date of Patent: June 9, 2020
    Assignees: Dana-Farber Cancer Institute, Inc., Cold Spring Harbor Institute
    Inventors: James Elliott Bradner, Johannes Zuber, Junwei Shi, Christopher R. Vakoc, Scott W. Lowe, Constantine S. Mitsiades
  • Patent number: 10668030
    Abstract: The present invention relates to methods of treatment of a disease or pathology of the central nervous system, an eating disorder, or substance use disorder, drug dependence/abuse and withdrawal therefrom comprising administering at least one N-phenylalkyl amphetamine derivative and pharmaceutical compositions comprising at least one N-phenylalkyl amphetamine derivative to an individual in need thereof.
    Type: Grant
    Filed: April 21, 2017
    Date of Patent: June 2, 2020
    Assignee: University of Kentucky Research Foundation
    Inventors: Linda P. Dwoskin, Peter Anthony Crooks, Guangrong Zheng, Justin R. Nickell, Zheng Cao, Na-Ra Lee
  • Patent number: 10646443
    Abstract: The disclosure is directed to methods of treating schizophrenia or bipolar disorder by subcutaneously administering a sustained-release dosage form of olanzapine, or a pharmaceutically acceptable salt thereof. Methods of subcutaneously administering olanzapine, or a pharmaceutically acceptable salt thereof, are also described.
    Type: Grant
    Filed: March 20, 2018
    Date of Patent: May 12, 2020
    Assignee: Teva Pharmaceuticals International GmbH
    Inventors: Carine Claassen-Punt, Mark Alan Smith, Ling Chen, Ari Andrew Gershon
  • Patent number: 10640507
    Abstract: The invention relates to pyrrolobenzodiazepines compounds (PBDs) and to pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular, to treat bacterial infections.
    Type: Grant
    Filed: December 9, 2016
    Date of Patent: May 5, 2020
    Assignees: King's College London, Secretary of State for Health and Social Care
    Inventors: Khondaker Mirazur Rahman, John Mark Sutton, Pietro Picconi
  • Patent number: 10526294
    Abstract: The present disclosure relates generally to derivatives of pyrrolobenzodiazepines and antibody-drug conjugates thereof and to methods of using these conjugates as therapeutics and/or diagnostics.
    Type: Grant
    Filed: June 22, 2017
    Date of Patent: January 7, 2020
    Assignee: Mersana Therapeutics, Inc.
    Inventors: Joshua D. Thomas, Mao Yin, Aleksandr V. Yurkovetskiy, Patrick R. Conlon, Ahmed Hilmy, Eugene W. Kelleher, Timothy B. Lowinger, Cheri A. Stevenson, Shuyi Tang
  • Patent number: 10512643
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: November 22, 2017
    Date of Patent: December 24, 2019
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 10493045
    Abstract: A method for treating alcohol dependence or alcohol abuse in a subject comprising administering to the subject a composition comprising an effective amount of memantine, wherein the effective amount of memantine is 2-4.7 mg/day. Low dose of memantine having anti-inflammatory and neurotrophic effect is able to reduce alcohol use.
    Type: Grant
    Filed: December 8, 2017
    Date of Patent: December 3, 2019
    Inventor: Ru-Band Lu
  • Patent number: 10463638
    Abstract: Technologies are described for a formulation and production of a formulation. The methods may comprise depositing a non-steroidal anti-inflammatory drug (NSAID) compound into a chamber. The methods may comprise depositing a N-methyl-D-aspartate (NMDA) receptor antagonist into the chamber. The methods may comprise respectively depositing a muscle relaxant, a local anesthetic into the chamber, depositing an anticonvulsant into the chamber, depositing an antidepressant into the chamber, and depositing a calcium channel blocking agent into the chamber. The methods may comprise milling the NSAID compound, the NMDA receptor antagonist, the muscle relaxant, the local anesthetic, the anticonvulsant, the antidepressant, and the calcium channel blocking agent into a powder. The methods may comprise adding a solvent with the powder and mixing the solvent with the powder to form a solution. The methods may comprise adding a base cream to the solution and mixing the base cream and the solution to form the formulation.
    Type: Grant
    Filed: April 12, 2018
    Date of Patent: November 5, 2019
    Assignee: SYNERGISTIC THERAPEUTICS, LLC
    Inventors: Anthony H. Salce, Jr., William F. Greenwood, Shivsankar Misir
  • Patent number: 10450319
    Abstract: The present invention relates to a salt form of a benzodiazepine derivative, in particular crystalline solid state forms, to pharmaceutical compositions comprising the same and to its use in therapy.
    Type: Grant
    Filed: April 18, 2018
    Date of Patent: October 22, 2019
    Assignee: GlaxoSmithKline Intellectual Property (No.2) Limited
    Inventors: Gossett Augustus Campbell, Asa Elisabeth Gladwin
  • Patent number: 10442819
    Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: October 15, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christian Fischer, Stephane L. Bogen, Matthew L. Childers, Francesc Xavier Fradera Llinas, J. Michael Ellis, Sara Esposite, Qingmei Hong, Chunhui Huang, Alexander J. Kim, John W. Lampe, Michelle R. Machacek, Daniel R. McMasters, Ryan D. Otte, Dann L. Parker, Jr., Michael Reutershan, Nunzio Sciammetta, Pengcheng P. Shao, David L. Sloman, Feroze Ujjainwalla, Catherine White, Zhicai Wu, Yang Yu, Kake Zhao, Craig Gibeau, Tesfaye Biftu, Purakkattle Biju, Lei Chen, Joshua Close, Peter H. Fuller, Xianhai Huang, Min K. Park, Valdimir Simov, David J. Witter, Hongjun Zhang
  • Patent number: 10421763
    Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.
    Type: Grant
    Filed: August 14, 2017
    Date of Patent: September 24, 2019
    Assignee: Purdue Pharma L.P.
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Patent number: 10399972
    Abstract: The present invention is directed to tricyclic compounds of formula (I), (Ia) or (Ib) which are inhibitors of one or more mutant IDH enzymes. The present invention is also directed to uses of these tricyclic compounds in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
    Type: Grant
    Filed: October 25, 2016
    Date of Patent: September 3, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: David J. Witter, Tesfaye Biftu, Purakkattle Biju, Stephane L. Bogen, Qingmei Hong, Chunhui Huang, Xianhai Huang, Bing Li, Min K. Park, David L. Sloman
  • Patent number: 10369143
    Abstract: Provided herein is a method of treating a central nervous system disorder in a patient in need thereof, wherein the central nervous system disorder is selected from schizophrenia, Alzheimer's disease, Huntington's disease, Parkinson's disease, and Lewy Body dementia. The method comprises orally administering an initial dose of between 75 mg and 300 mg xanomeline and an initial dose of between 20 mg and 200 mg trospium chloride to the patient during a 24-hour period. Provided that the patient tolerates said administration, an increased dose of trospium chloride and an increased dose of xanomeline are orally administering to the patient, wherein the increased dose of trospium chloride is greater than the initial dose of the trospium chloride, and wherein the increased dose of xanomeline is greater than the initial dose of the xanomeline.
    Type: Grant
    Filed: February 7, 2019
    Date of Patent: August 6, 2019
    Assignee: PureTech Health LLC
    Inventors: Eric Elenko, Philip E. Murray, III, Andrew C. Miller
  • Patent number: 10328076
    Abstract: The present invention relates to a stable pharmaceutical formulation of solid dosage forms for oral administration comprising a therapeutically effective amount of a triazole antifungal agent or pharmaceutical acceptable salt thereof, in particular Voriconazole and an effective amount of a solubility enhancing agent. It also relates to a process for the preparation thereof.
    Type: Grant
    Filed: June 9, 2015
    Date of Patent: June 25, 2019
    Assignee: PHARMATHEN S.A.
    Inventor: Evangelos Karavas