Additional Hetero Atom In The Polycyclo Ring System Patents (Class 514/215)
  • Patent number: 10709686
    Abstract: The present invention is related to a method of treating idiopathic pulmonary fibrosis comprising administering to a subject in need thereof an effective amount of a composition containing a compound that binds FK506 binding protein 4.
    Type: Grant
    Filed: March 20, 2019
    Date of Patent: July 14, 2020
    Assignee: DAVID WEINSTEIN CONSULTING, INC.
    Inventor: David Weinstein
  • Patent number: 10526339
    Abstract: Glucosepane is a structurally complex protein post-translational modification (PTM) believed to exist in all living organisms. Glucosepane possesses a unique chemical structure that incorporates a surprising, never-before-prepared non-aromatic tautomer of imidazole, rendering it a challenging target for chemical synthesis. In this application, the inventors report the first total synthesis of glucosepane and related compounds according to the chemical structure: Methods of synthesis, compounds obtained therefrom, pharmaceutical compositions and methods of treatment provide embodiments of the present invention.
    Type: Grant
    Filed: September 23, 2016
    Date of Patent: January 7, 2020
    Assignee: YALE UNIVERSITY
    Inventors: David Spiegel, Cristian Draghici
  • Patent number: 10509044
    Abstract: The present invention provides a method for predicting whether a human patient 65 years of age or older is at increased risk for developing heart failure, comprising obtaining the results of an assay that measures levels of NT-proBNP and/or cardiac troponin T in a specimen from the patient wherein an increased NT-proBNP and/or cardiac troponin T level compared to levels in a control indicate an increased risk for developing heart failure.
    Type: Grant
    Filed: May 8, 2015
    Date of Patent: December 17, 2019
    Assignees: UNIVERSITY OF MARYLAND, BALTIMORE, BOARD OF REGENT, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Christopher Defilippi, Stephen Seliger, James De Lemos, Robert H. Christenson
  • Patent number: 10472375
    Abstract: There is provided a 5,6-dihydro-4H-benzo[b]thieno-[2,3-d]azepine derivative which is useful in the treatment of respiratory syncytial virus (RSV) infection and for the prevention of disease associated with RSV infection. (Formula (I)).
    Type: Grant
    Filed: March 11, 2019
    Date of Patent: November 12, 2019
    Assignee: PULMOCIDE LIMITED
    Inventors: Simon Fraser Hunt, Stuart Thomas Onions, Vladimir Sherbukhin, Euan Alexander Fraser Fordyce, Peter John Murray, Daniel William Brookes, Kazuhiro Ito, Peter Strong, Matthew Stephen Coates
  • Patent number: 10414770
    Abstract: This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.
    Type: Grant
    Filed: September 18, 2017
    Date of Patent: September 17, 2019
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher F. Claiborne, Lloyd J. Payne, Richard J. Boyce, Todd B. Sells, Stephen G. Stroud, Stuart Travers, Tricia J. Vos, Gabriel S. Weatherhead
  • Patent number: 10363240
    Abstract: The present invention is directed to a composition for treating alopecia containing minoxidil, cyclosporine A and a compound that binds FK506 binding protein 4 suitable for administration to humans. The present invention is further directed to treating alopecia in humans by administering a composition of the invention.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: July 30, 2019
    Assignee: DAVID WEINSTEIN CONSULTING, INC.
    Inventor: David Weinstein
  • Patent number: 10307409
    Abstract: A combination of a muscarinic cholinergic receptor agonist, a non-anticholinergic antiemetic agent and a non-selective, peripheral anticholinergic agent for the treatment of hypocholinergic disorders of the central nervous system.
    Type: Grant
    Filed: September 9, 2016
    Date of Patent: June 4, 2019
    Assignee: Chase Pharmaceuticals Corporation
    Inventors: Thomas N. Chase, Kathleen E. Clarence-Smith
  • Patent number: 10285977
    Abstract: The present invention is directed to a composition for treating alopecia containing minoxidil, cyclosporine A and a compound that binds FK506 binding protein 4 suitable for administration to humans. The present invention is further directed to treating alopecia in humans by administering a composition of the invention.
    Type: Grant
    Filed: April 4, 2017
    Date of Patent: May 14, 2019
    Assignee: DAVID WEINSTEIN CONSULTING, INC.
    Inventor: David Weinstein
  • Patent number: 10189835
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: January 29, 2019
    Assignee: NOVIRA THERAPEUTICS, INC.
    Inventors: George D. Hartman, Scott Kuduk
  • Patent number: 10100046
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: January 10, 2018
    Date of Patent: October 16, 2018
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 10077268
    Abstract: Novel FXR agonists are disclosed, embodiments of a method of making the same, and of a composition comprising them are disclosed herein. Also disclosed are embodiments of a method of treating or preventing a metabolic disorder in a subject, comprising administering to a subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and treating or preventing a metabolic disorder in the subject. Additionally disclosed are embodiments of a method of treating or preventing inflammation in an intestinal region of a subject, comprising administering to the subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and thereby treating or preventing inflammation in the intestinal region of the subject.
    Type: Grant
    Filed: September 12, 2016
    Date of Patent: September 18, 2018
    Assignee: Salk Institute for Biological Studies
    Inventors: Ronald M. Evans, Michael Downes, Thomas J. Baiga, John F.W. Keana, Christopher Liddle
  • Patent number: 10017513
    Abstract: The present invention is directed to a compound of formula (I): or a crystalline form thereof, or a solvate thereof; to a solid pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula (I), or a crystalline form thereof, or a solvate thereof, and at least one pharmaceutically acceptable carrier or diluent, and to the use of a compound of formula (I), or a crystalline form thereof, or a solvate thereof, for treating a patient suffering from, or subject to, a disease, disorder, or condition mediated by Aurora kinase, and methods related thereto.
    Type: Grant
    Filed: October 13, 2016
    Date of Patent: July 10, 2018
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Ian Armitage, Martin I. Cooper, Mark D. Eddleston, Neil C. Faiber, Quentin J. McCubbin, Stephen W. Watt
  • Patent number: 10011615
    Abstract: Disclosed are compounds of Formula G1: where “RG3”. “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein, which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2A receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.
    Type: Grant
    Filed: February 2, 2017
    Date of Patent: July 3, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Yeon-Hee Lim, Andrew Stamford, Rongze Kuang, Paul Tempest, Younong Yu, Xianhai Huang, Timothy J. Henderson, Jae-Hun Kim, Christopher Boyce, Pauline Ting, Junying Zheng, Edward Metzger, Nicolas Zorn, Dong Xiao, Gioconda V. Gallo, Walter Won, Heping Wu, Qiaolin Deng
  • Patent number: 10004703
    Abstract: NSC antagonists are disclosed as useful in the treatment of dementia, in delaying the onset of dementia, and in the prevention of dementia. Dementia so treated may be, for example, Alzheimer's Disease (AD). NSC antagonists for treating dementia such as AD may be administered alone, a) in combination with other drugs used for treating dementia, b) in combination with drugs that stabilize or increase blood plasma glucose levels, or with both a) and b). Pharmaceutical compositions, dosage forms, and methods for using the same are disclosed, which include NSC antagonists, NSC antagonists combined with dementia drugs, NSC antagonists combined with glucose-level stabilizing or enhancing drugs, or combinations of these. Dosage forms may be designed to provide stable plasma levels for extended periods of time.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: June 26, 2018
    Assignee: Biogen Chesapeake LLC
    Inventors: Sven Martin Jacobson, Robert Ang
  • Patent number: 10000484
    Abstract: The present invention provides compounds of Formula (I) (Formula (I)) including pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: December 16, 2014
    Date of Patent: June 19, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harry Chobanian, Barbara Pio, Yan Guo, Fa-Xiang Ding, Shuzhi Dong, Shawn P. Walsh, Jinlong Jiang, Dooseop Kim
  • Patent number: 9988384
    Abstract: The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: June 5, 2018
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher F. Claiborne, Todd B. Sells, Stephen G. Stroud
  • Patent number: 9969747
    Abstract: The present disclosure relates to a crystalline form of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, which is useful as an inhibitor of bromodomain-containing proteins. The present disclosure also provides pharmaceutically acceptable compositions comprising the crystalline form and methods of using said compositions in the treatment of various disorders.
    Type: Grant
    Filed: June 18, 2015
    Date of Patent: May 15, 2018
    Assignee: Constellation Pharmaceuticals, Inc.
    Inventor: Michael L. Hall
  • Patent number: 9937182
    Abstract: Compositions and methods for treating preeclampsia in a subject in need thereof are disclosed.
    Type: Grant
    Filed: February 10, 2014
    Date of Patent: April 10, 2018
    Inventors: Justin L. Grobe, Mark K. Santillan, Donna Ann Santillan
  • Patent number: 9932309
    Abstract: The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts or solvates thereof, and their use.
    Type: Grant
    Filed: July 28, 2015
    Date of Patent: April 3, 2018
    Assignees: Universite de Lille 2 Droit et Sante, Institut Pasteur de Lille, INSERM
    Inventors: Julie Charton, Benoit Deprez, Florence Leroux, Bart Staels, Anne Muhr-Tailleux, Nathalie Hennuyer, Sophie Lestavel, Sylvain Picon, Karen Aknin, Rajaa Boulahjar, Barbara Dubanchet
  • Patent number: 9925197
    Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
    Type: Grant
    Filed: September 27, 2016
    Date of Patent: March 27, 2018
    Assignee: Constellation Pharmaceuticals, Inc.
    Inventors: Brian K. Albrecht, Michael Charles Hewitt, Victor S. Gehling, Rishi G. Vaswani
  • Patent number: 9902719
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: June 29, 2015
    Date of Patent: February 27, 2018
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 9895363
    Abstract: Pharmaceutical compositions and methods for inhibiting cell growth, modulating function of PCNA, treating prostate cancer, and enhancing PCNA trimer formation are disclosed. The methods include administering an effective amount of a compound of Formula (I): (a representative image), or an effective amount of a specific compound of Formula (II): (a representative image).
    Type: Grant
    Filed: September 8, 2011
    Date of Patent: February 20, 2018
    Assignee: University of Cincinnati
    Inventors: Zhongyun Dong, Matthew Wortman, Zonqing Tan, Kelsey Dillehay
  • Patent number: 9879033
    Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
    Type: Grant
    Filed: October 19, 2015
    Date of Patent: January 30, 2018
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Irini Akritopoulou-Zanze, Wilfried Braje, Stevan W. Djuric, Noel S. Wilson, Sean C. Turner, Albert W. Kruger, Ana-Lucia Relo, Shashank Shekhar, Dennie S. Welch, Hongyu Zhao, Jorge Gandarilla, Alan F. Gasiecki, Huanqiu Li, Christina M. Thompson, Min Zhang
  • Patent number: 9862737
    Abstract: In part, the present invention is directed to antibacterial compounds and salts thereof.
    Type: Grant
    Filed: November 8, 2013
    Date of Patent: January 9, 2018
    Assignee: Debiopharm International SA
    Inventors: Henry Pauls, Jailall Ramnauth
  • Patent number: 9765078
    Abstract: This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.
    Type: Grant
    Filed: July 27, 2015
    Date of Patent: September 19, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher F. Claiborne, Lloyd J. Payne, Richard J. Boyce, Todd B. Sells, Stephen G. Stroud, Stuart Travers, Tricia J. Vos, Gabriel S. Weatherhead
  • Patent number: 9750729
    Abstract: The present invention is directed to immune adjuvants containing IAP inhibitors, including Smac mimetics. The invention further provides pharmaceutical compositions and vaccines containing an IAP inhibitor and an antigen. Methods of enhancing an immune response by administration of an IAP inhibitor, methods of treating or preventing cancer, methods of treating or preventing infections, methods of treating autoimmune disorders, and methods of potentiating cytokine or antibody production are also provided.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: September 5, 2017
    Assignees: Dana-Farber Cancer Institute, Inc., Novartis AG
    Inventors: Leigh Zawel, Christopher S. Straub, Brant G. Firestone, Glenn Dranoff, Michael Dougan
  • Patent number: 9738649
    Abstract: Certain tetrahydro-pyrimidoazepine compounds are described, which are useful as TRPV1 modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by TRPV1. Thus, the compounds may be administered to treat, e.g., pain, itch, cough, asthma, or inflammatory bowel disease.
    Type: Grant
    Filed: July 12, 2016
    Date of Patent: August 22, 2017
    Assignee: JANSSEN PHARMACEUTICA N.V.
    Inventors: Brett D. Allison, Bryan James Branstetter, J. Guy Breitenbucher, Michael D. Hack, Natalie A. Hawryluk, Alec D. Lebsack, Kelly J. McClure, Jeffrey E. Merit
  • Patent number: 9730903
    Abstract: A gel useful in reducing bacterial colonization in or around the area of a wound can be provided from at least one PEG and an aqueous composition having a pH of from 2 to 4, a total solute concentration of from 1.8 to 4.0 Osm/L, and from 0.9 to 1.7 g/L of at least one cationic surfactant. The aqueous composition can include a buffer system that includes an organic acid and a salt of an organic acid. The resulting gel is effective even when free of materials having antimicrobial properties other than those provided by the aqueous composition such as sporicides, antifungals and antibiotics.
    Type: Grant
    Filed: October 31, 2016
    Date of Patent: August 15, 2017
    Assignee: Next Science, LLC
    Inventor: Matthew Franco Myntti
  • Patent number: 9724354
    Abstract: Disclosed are methods for the treatment of proliferative disorders. Disclosed in particular, are methods for treatment of proliferative disorders such as cancer, by administering an mTORC1/2 inhibitor in combination with a selective inhibitor of Aurora A kinase. Preferred MTORC1/2 inhibitors include MLN0128 and the preferred Aurora A kinase inhibitor of the combination is MLN8237.
    Type: Grant
    Filed: March 21, 2014
    Date of Patent: August 8, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Rachael L. Brake, Huifeng Niu
  • Patent number: 9708334
    Abstract: The invention provides a chemical entity of Formula (I), wherein R1, R2, R3, R4, R5 and X have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by GlyT1 activity; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training; and treating other disorders, including pain and alcohol-dependence.
    Type: Grant
    Filed: April 22, 2015
    Date of Patent: July 18, 2017
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Jillian Basinger, Brett Bookser, Mi Chen, DeMichael Chung, Varsha Gupta, Andrew Hudson, Alan Kaplan, James Na, Joel Renick, Vincent Santora
  • Patent number: 9623009
    Abstract: This invention pertains to a method for the treatment of non-small cell lung cancer in a subject who is a smoker, comprising administering to the subject an effective amount of 2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (veliparib or ABT-888), or a pharmaceutically acceptable salt thereof, in combination with carboplatin and paclitaxel.
    Type: Grant
    Filed: September 16, 2015
    Date of Patent: April 18, 2017
    Assignee: AbbVie, Inc.
    Inventors: Vincent Giranda, Gary Gordon, Mark D. McKee, Jane Qian, Qin Qin
  • Patent number: 9624173
    Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.
    Type: Grant
    Filed: March 19, 2015
    Date of Patent: April 18, 2017
    Assignee: 3-V Biosciences, Inc.
    Inventors: Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu
  • Patent number: 9624244
    Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: April 18, 2017
    Assignee: Constellation Pharmaceuticals, Inc.
    Inventors: Brian K. Albrecht, Victor S. Gehling, Alexander M. Taylor, Rishi G. Vaswani
  • Patent number: 9598434
    Abstract: Provided is a compound which is useful as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like. The present inventors have investigated compounds having a 5-HT2C receptor agonist activity and have found that the benzazepine compounds of the present invention have an excellent 5-HT2C receptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HT2C receptor agonist activity and can be used as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.
    Type: Grant
    Filed: July 13, 2015
    Date of Patent: March 21, 2017
    Assignee: ASTELLAS PHARMA INC.
    Inventors: Hiroyuki Koshio, Norio Asai, Taisuke Takahashi, Takafumi Shimizu, Yasuhito Nagai, Keiko Kawabata, Karl Bruce Thor
  • Patent number: 9598365
    Abstract: A method of synthesizing cycloalkanyl[b]indoles, as well as related cycloalkanyl[b]benzofurans and cycloalkanyl[b]benzothiophenes is provided. The method is a single, multicomponent reaction that combines (1) an indole, benzofuran, or benzothiopene, (2) an aldehyde, ketone, or ketal, and (3) a diene in the presence of an acid, in particular a Ga(III) or In(III) salt. Compositions and methods of using these compounds to stimulate secretion and/or production of glucagon-like peptide-1 or inhibit the activity of Calcitonin Gene-Related Peptide receptor are also provided.
    Type: Grant
    Filed: November 10, 2014
    Date of Patent: March 21, 2017
    Assignee: TRUSTEES OF DARTMOUTH COLLEGE
    Inventor: Jimmy Wu
  • Patent number: 9556200
    Abstract: The present invention provides a compound having a superior serotonin 5-HT2C receptor activating action. The present invention relates to a compound represented by the formula (1) wherein ring A is an aromatic carbocycle optionally having substituent(s) or an aromatic heterocycle optionally having substituent(s), X is —N(R1)—, —O— or the like, when ring A is an aromatic carbocycle optionally having substituent(s), then R1 is a hydrogen atom, an alkyl group optionally having substituent(s), or the like, and when ring A is an aromatic heterocycle optionally having substituent(s), then R1 is a hydrogen atom, an alkyl group optionally having substituent(s), a cycloalkyl group optionally having substituent(s), or the like, is a single bond or a double bond, and n is an integer of 0, 1 or 2, or a salt thereof.
    Type: Grant
    Filed: March 6, 2013
    Date of Patent: January 31, 2017
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tomokazu Kusumoto, Shigekazu Sasaki, Hironobu Maezaki
  • Patent number: 9550782
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: January 24, 2017
    Assignee: MEDIVATION TECHNOLOGIES, INC.
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain, Michael John Green
  • Patent number: 9527845
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Grant
    Filed: December 30, 2015
    Date of Patent: December 27, 2016
    Assignee: NOVIRA THERAPEUTICS, INC.
    Inventors: George D. Hartman, Scott Kuduk
  • Patent number: 9522920
    Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
    Type: Grant
    Filed: June 24, 2014
    Date of Patent: December 20, 2016
    Assignee: CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: Brian K. Albrecht, James Edmund Audia, Alexandre Côté, Victor S. Gehling, Jean-Christophe Harmange, Michael Charles Hewitt, Yves Leblanc, Christopher G. Nasveschuk, Alexander M. Taylor, Rishi G. Vaswani
  • Patent number: 9518057
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Grant
    Filed: December 30, 2015
    Date of Patent: December 13, 2016
    Assignee: NOVIRA THERAPEUTICS, INC.
    Inventors: George D. Hartman, Scott Kuduk
  • Patent number: 9504693
    Abstract: This invention provides novel pharmaceutical compositions of the compound of formula (I): or a pharmaceutically acceptable salt thereof, that are suitable for the bulk production of an oral pharmaceutical dosage form; processes for the production of said oral pharmaceutical dosage form; and the use of the pharmaceutical composition for the treatment of patients suffering from or subject to diseases, disorders, or conditions involving cell survival, proliferation and migration, including chronic inflammatory proliferative disorders, proliferative ocular disorders, benign proliferative disorders, and cancer.
    Type: Grant
    Filed: August 28, 2015
    Date of Patent: November 29, 2016
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Vijayalakshmi Ramanan, Irene S. Tobias, Raymond D. Skwierczynski, Dauntel S. Verwijs
  • Patent number: 9493483
    Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: November 15, 2016
    Assignee: Constellation Pharmaceuticals, Inc.
    Inventors: Brian K. Albrecht, Michael Charles Hewitt, Victor S. Gehling, Rishi G. Vaswani
  • Patent number: 9486420
    Abstract: A gel useful in reducing bacterial colonization in or around the area of a wound includes at least one PEG and an aqueous composition having a pH of from 2 to 4, a total solute concentration of from 1.8 to 4.0 Osm/L, and from 0.9 to 1.7 g/L of at least one cationic surfactant. The aqueous composition can include a buffer system that includes an organic acid and a salt of an organic acid. The gel is effective even when free of materials having antimicrobial properties other than those provided by the aqueous composition such as sporicides, antifungals and antibiotics.
    Type: Grant
    Filed: July 25, 2016
    Date of Patent: November 8, 2016
    Assignee: Next Science, LLC
    Inventor: Matthew Franco Myntti
  • Patent number: 9433626
    Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: April 30, 2015
    Date of Patent: September 6, 2016
    Assignee: Medivation Technologies, Inc.
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Patent number: 9427417
    Abstract: A process for reducing bacterial colonization in or around the area of a wound includes applying to the area a gel that includes at least one PEG and an aqueous composition which has a pH of from 2 to 4, a total solute concentration of from 1.8 to 4.0 Osm/L, and from 0.9 to 1.7 g/L of at least one cationic surfactant. The aqueous composition can include a buffer system that includes an organic acid and a salt of an organic acid. The gel is effective even when free of materials having antimicrobial properties other than those provided by the aqueous composition, such as sporicides, antifungals and antibiotics.
    Type: Grant
    Filed: March 19, 2016
    Date of Patent: August 30, 2016
    Assignee: Next Science, LLC
    Inventor: Matthew Franco Myntti
  • Patent number: 9422293
    Abstract: Certain tetrahydro-pyrimidoazepine compounds are described, which are useful as TRPV1 modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by TRPV1. Thus, the compounds may be administered to treat, e.g., pain, itch, cough, asthma, or inflammatory bowel disease.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: August 23, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Brett D. Allison, Bryan James Branstetter, J. Guy Breitenbucher, Michael D. Hack, Natalie A. Hawryluk, Alec D. Lebsack, Kelly J. McClure, Jeffrey E. Merit
  • Patent number: 9409910
    Abstract: This disclosure relates to new azepino[4,5-b]indole compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new 1,2,3,4,5,6-tetrahydroazepino[4,5-b]indoles. Pharmaceutical compositions are also provided.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: August 9, 2016
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Rajendra Parasmal Jain, Sarvajit Chakravarty
  • Patent number: 9353059
    Abstract: The composition containing a pamoate salt of donepezil, the method of preparation and the use thereof are disclosed.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: May 31, 2016
    Inventor: Zi-Oiang Gu
  • Patent number: 9346816
    Abstract: The present invention relates to compounds defined by formula I wherein the groups X, Y, W and R1 to R4 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are agonists of the 5-HT2C receptor, and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this receptor, such as metabolic and CNS-related disorders.
    Type: Grant
    Filed: November 5, 2013
    Date of Patent: May 24, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Stephan-Georg Mueller, Christopher John Brown, Alexander Heifetz, Bernd Nosse, Juergen Prestle, Natacha Prevost, Klaus Rudolf, Stefan Scheuerer, Marcus Schindler, Dirk Stenkamp, Leo Thomas, Heather Tye
  • Patent number: 9284277
    Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are benzazepine compounds. These compounds are serotonin receptor (5-HT2c) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT2c) is desired (e.g. addiction, anxiety, depression, obesity, and others).
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: March 15, 2016
    Assignee: ABT Holding Company
    Inventors: Mike Robarge, John Harrington, David Gerrish, John Mecom