At Least Three Rings In The Polycyclo Ring System Patents (Class 514/250)
  • Patent number: 10661099
    Abstract: A method for the treatment of a person suffering from neurodegenerative disease such as Alzheimer's, Parkinson's, or Huntington's disease by treating the patient's brain, over the span of one year or less with a plurality of doses of ionizing radiation, each dose being more than 2.5 mJ/kg but less than 150 mJ/kg with the total dose being more than 10 mJ/kg but less than 400 mJ/kg.
    Type: Grant
    Filed: June 14, 2016
    Date of Patent: May 26, 2020
    Inventor: Eugene R. Moore
  • Patent number: 10597400
    Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.
    Type: Grant
    Filed: July 1, 2019
    Date of Patent: March 24, 2020
    Assignee: AbbVie Inc.
    Inventors: Ahmed A. Othman, Mohamed-Eslam F. Mohamed, Ben Klünder, Aileen L. Pangan
  • Patent number: 10576078
    Abstract: The present invention relates to method of treating chronic myeloid leukemia (CML) or drug resistant CML comprising, administering to human being or any other mammal or animal in need thereof, a therapeutically effective amount of Clofazimine (CFZ) or its pharmaceutically acceptable derivative, analogue, salt or composition; or a combination of a therapeutically effective amount of Clofazimine (CFZ) or its pharmaceutically acceptable derivative, analogue, salt or composition with a tyrosine kinase inhibitor (TKI). The invention also provides the kit for treatment of CML or drug resistant CML.
    Type: Grant
    Filed: August 30, 2018
    Date of Patent: March 3, 2020
    Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Sabyasachi Sanyal, Harish Kumar, Naibedya Chattopadhyay, Ravishankar Ramachandran, Arun Kumarv Trivedi, Sonal Shree, Anagha Ashok Gurjar, Sourav Chattopadhyay, Sapana Kushwaha, Abhishek Kumar Singh, Shikha Dubey, Kiran Lata, Riyazuddin Mohammed, Jiaur Rahaman Gayen, Anil Kumar Tripathi
  • Patent number: 10544124
    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: January 28, 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: 10526331
    Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
    Type: Grant
    Filed: February 26, 2019
    Date of Patent: January 7, 2020
    Assignee: Janssen Sciences Ireland Unlimited Company
    Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
  • Patent number: 10517876
    Abstract: The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.
    Type: Grant
    Filed: January 5, 2017
    Date of Patent: December 31, 2019
    Assignee: CTI BIOPHARMA CORP.
    Inventors: Stephanie Blanchard, Cheng Hsia Angeline Lee, Harish Kumar Mysore Nagaraj, Anders Poulsen, Eric T. Sun, Yee Ling Evelyn Tan, Anthony Deodaunia William
  • Patent number: 10513524
    Abstract: The present invention relates to PDE9 inhibitors and their use for treatment of benign prostate hyperplasia and sickle cell disease.
    Type: Grant
    Filed: July 6, 2016
    Date of Patent: December 24, 2019
    Assignee: H. LUNDBECK A/S
    Inventors: Niels Svenstrup, Kate Wen, Yazhou Wang
  • Patent number: 10500202
    Abstract: Disclosed herein are pharmaceutical compositions comprising Tadalafil, or a salt, or derivatives thereof and pharmaceutical excipients, processes for the preparation thereof, and pharmaceutical compositions containing them. The pharmaceutical compositions have improved physicochemical properties that provide faster onset of action for the treatment of erectile dysfunction.
    Type: Grant
    Filed: November 30, 2017
    Date of Patent: December 10, 2019
    Assignee: Druggability Technologies IP Holdco Limited
    Inventors: Betti Szabóné Ordasi, Tamás Jordán, Richárd Balázs Kárpáti, Andrea Ujhelyi, Tamás Solymosi, Hristos Glavinas, Genovéva Filipcsei
  • Patent number: 10501463
    Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
    Type: Grant
    Filed: November 16, 2018
    Date of Patent: December 10, 2019
    Assignee: Janssen Sciences Ireland Unlimited Company
    Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
  • Patent number: 10493075
    Abstract: The present invention relates to a method of preparing 4-Amino-(6R,S)-5,6,7,8-tetrahydro-L-biopterin dihydrochloride dihydrate.
    Type: Grant
    Filed: June 8, 2018
    Date of Patent: December 3, 2019
    Assignee: VASOPHARM GMBH
    Inventors: Peter Scheurer, Frank Tegtmeier, Reinhard Schinzel
  • Patent number: 10479801
    Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, R1, R2, R3 and R7 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: November 30, 2017
    Date of Patent: November 19, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas H. Graham, Tao Yu, Yonglian Zhang, John A. McCauley
  • Patent number: 10456395
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein L, R1, R5, W, X, Y1, Y2, and Z are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: May 17, 2018
    Date of Patent: October 29, 2019
    Assignee: Gilead Sciences, Inc.
    Inventors: Hyung-Jung Pyun, Manoj C. Desai, Haolun Jin, Mingzhe Ji, Teresa Alejandra Trejo Martin
  • Patent number: 10414777
    Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
    Type: Grant
    Filed: October 27, 2017
    Date of Patent: September 17, 2019
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 10413553
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.
    Type: Grant
    Filed: February 1, 2018
    Date of Patent: September 17, 2019
    Assignee: Heptares Therapeutics Limited
    Inventors: Miles Stuart Congreve, Giles Albert Brown, Julie Elaine Cansfield, Benjamin Gerald Tehan
  • Patent number: 10376509
    Abstract: Methods for inhibiting the activity of Clostridium difficile in a subject comprise administering to the subject in need thereof a pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and a clofazimine analog selected from B746 clofazimine analog or B826 clofazimine analog.
    Type: Grant
    Filed: August 22, 2018
    Date of Patent: August 13, 2019
    Assignee: KamTek, Inc.
    Inventors: Venkata M. Reddy, Wolf Prensky, Sharanjit VedBrat
  • Patent number: 10254297
    Abstract: Components for enabling immunodetection of methoxetamine are described including immunogens, haptens, antibodies and kits.
    Type: Grant
    Filed: July 1, 2016
    Date of Patent: April 9, 2019
    Assignee: Randox Laboratories Ltd.
    Inventors: Ivan McConnell, Philip Lowry, Elouard Benchikh, Peter Fitzgerald
  • Patent number: 10220099
    Abstract: The synthesis of various pyrazino[1?,2?:1,5]pyrrolo[2,3-b]-indole-1,4-dione analogs has been successfully implemented in the present application. From these efforts, compounds having the structure of Formula I-c: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein R1, R2, R4-R8, R3?, R6?, and n are as defined herein, are provided. These biologically active derivatives have been further used to prepare cell-specific drug conjugates effective in treating various diseases including cancer.
    Type: Grant
    Filed: May 10, 2016
    Date of Patent: March 5, 2019
    Assignees: Massachusetts Institute of Technology, The Board of Trustees of the University of Illinois
    Inventors: Mohammad Movassaghi, Justin Kim, Paul J. Hergenrother, Karen Morrison, Nicolas Boyer
  • Patent number: 10184932
    Abstract: The present invention inter alia provides a method, and use thereof, of predicting CV events such as AMI, ACS, stroke, and CV death by determining the concentration of at least one ceramide of Formula I or one lysophospholipid of Formula II and/or III and at least one lysophospholipid of Formula IV, V, VI, VII and/or VIII in a biological sample and comparing those concentrations to a control. Finding an increased concentration of the at least one Formula I ceramide or Formula II and/or III lysophospholipid and a decreased concentration of the at least one Formula IV, V, VI, VII and/or VIII lysophospholipid indicates that the subject has an increased risk of developing one or more CV events. The present disclosure also provides a method, and use thereof, of diagnosing subjects suffering acute ischemia. Also provided are kits and compositions comprising the same for use in predicting and/or diagnosing CV events.
    Type: Grant
    Filed: December 7, 2016
    Date of Patent: January 22, 2019
    Assignee: Zora Biosciences OY
    Inventors: Mika Hilvo, Reini Hurme, Reijo Laaksonen, Virve Vaeisaenen
  • Patent number: 10172854
    Abstract: The invention described herein relates to methods for treating mitochondrial diseases. In particular, the invention relates to methods for treating mitochondrial diseases by administering therapeutically effective amounts of one or more tetracyclic pyrazinoindoles, and/or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 22, 2017
    Date of Patent: January 8, 2019
    Assignee: BIOVISTA, INC.
    Inventors: Spyros Deftereos, Andreas Persidis
  • Patent number: 10155759
    Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
    Type: Grant
    Filed: December 18, 2017
    Date of Patent: December 18, 2018
    Assignee: Janssen Sciences Ireland UC
    Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
  • Patent number: 10150780
    Abstract: The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, B, X, R1, R2, R3 and R4 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: December 4, 2015
    Date of Patent: December 11, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas H. Graham, Mark W. Embrey, Abbas Walji, Sherman T. Waddell
  • Patent number: 10138244
    Abstract: The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof, for use as a human PDE1 inhibitor.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: November 27, 2018
    Assignee: Eli Lilly and Company
    Inventors: Mark David Rekhter, Qing Shi
  • Patent number: 10081818
    Abstract: The present invention provides methods for producing cannabinoids and cannabinoid analogs as well as a system for producing these compounds. The inventive method is directed to contacting a compound according to Formula I or Formula II with a cannabinoid synthase. Also described is a system for producing cannabinoids and cannabinoid analogs by contacting a THCA synthase with a cannabinoid precursor and modifying at least one property of the reaction mixture to influence the quantity formed of a first cannabinoid relative to the quantity formed of a second cannabinoid.
    Type: Grant
    Filed: February 10, 2017
    Date of Patent: September 25, 2018
    Assignee: TEEWINOT TECHNOLOGIES LIMITED
    Inventors: Richard Peet, Malcolm J. Kavarana, Robert Winnicki, Marc Donsky, Mingyang Sun
  • Patent number: 10072010
    Abstract: The invention relates to substituted pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]-quinoxaline compounds, represented by Formula 1, defined herein, free base or pharmaceutically acceptable salt forms of the compounds, pharmaceutical compositions thereof, and methods of treating conditions of the central nervous system therewith:
    Type: Grant
    Filed: June 21, 2017
    Date of Patent: September 11, 2018
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Qiang Zhang, Robert Davis, Lawrence P. Wennogle
  • Patent number: 10064860
    Abstract: Methods for inhibiting the activity of Clostridium difficile in a subject comprises administering to the subject a pharmaceutical composition consisting of clofazimine and at least one pharmaceutically acceptable excipient. Pharmaceutical compositions consisting of clofazimine at least one pharmaceutically acceptable excipient are provided for treating Clostridium difficile infection and diseases or symptoms associated therewith.
    Type: Grant
    Filed: December 4, 2017
    Date of Patent: September 4, 2018
    Assignee: KamTek, Inc.
    Inventors: Venkata M. Reddy, Wolf Prensky, Sharanjit VedBrat
  • Patent number: 10035809
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: May 18, 2017
    Date of Patent: July 31, 2018
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Elizabeth M. Bacon, Zhenhong R. Cai, Xiaowu Chen, Jeromy J. Cottell, Manoj C. Desai, Mingzhe Ji, Haolun Jin, Scott E. Lazerwith, Michael R. Mish, Philip Anthony Morganelli, Hyung-Jung Pyun, James G. Taylor, Teresa Alejandra Trejo Martin
  • Patent number: 10017517
    Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.
    Type: Grant
    Filed: February 7, 2018
    Date of Patent: July 10, 2018
    Assignee: AbbVie Inc.
    Inventors: Thomas B. Borchardt, Ahmad Y. Sheikh
  • Patent number: 10011604
    Abstract: Methods for treating a disease or disorder selected from pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection and osteolytic disease in a mammal, which comprise administering to said mammal a therapeutically effective amount of a compound of Formula I in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification.
    Type: Grant
    Filed: December 30, 2015
    Date of Patent: July 3, 2018
    Assignee: Array BioPharma, Inc.
    Inventors: Steven W. Andrews, Julia Haas, Yutong Jiang, Gan Zhang
  • Patent number: 10000482
    Abstract: The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.
    Type: Grant
    Filed: October 18, 2013
    Date of Patent: June 19, 2018
    Assignee: ORIGENIS GMBH
    Inventors: Michael Almstetter, Michael Thormann, Andreas Treml, Roland Koestler, Nasser Yehia
  • Patent number: 9962383
    Abstract: The present invention, among other things, provides compounds, compositions and methods for treatment of cancer. In some embodiments, the present invention provides methods for treating blood cancer using agelastatin alkaloids.
    Type: Grant
    Filed: September 2, 2016
    Date of Patent: May 8, 2018
    Assignees: Massachusetts Institute of Technology, The Board of Trustees of the University of Illionois
    Inventors: Mohammad Movassaghi, Paul J. Hergenrother
  • Patent number: 9963459
    Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.
    Type: Grant
    Filed: December 29, 2017
    Date of Patent: May 8, 2018
    Assignee: AbbVie Inc.
    Inventors: Jayanthy Jayanth, Patrick J. Marroum, Peter T. Mayer, Mohamed-Eslam F. Mohamed, Ahmed A. Othman
  • Patent number: 9963430
    Abstract: The present invention provides a novel processes for preparation of methyl 3-(benzyloxy)-5-(2,4-difluorobenzylcarbamoyl)-4-oxo-1-(2-oxoethyl)-1,4-dihydropyiridine-2-carboxylate using novel intermediates.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: May 8, 2018
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Mogili Narsingam, Bandi Vamsi Krishna
  • Patent number: 9951080
    Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.
    Type: Grant
    Filed: November 3, 2017
    Date of Patent: April 24, 2018
    Assignee: AbbVie Inc.
    Inventor: Ayman Allian
  • Patent number: 9944635
    Abstract: This invention in one embodiment is directed to a compound of Formula Ia; where the designation (R) indicates that the designated carbon has the (R) stereochemistry; and wherein Z1 is hydrogen or fluorine; Z2 is hydrogen, deuterium, or fluorine; Z3 is deuterium; Z4 is fluorine; m is an integer from 0 to 10; n is an integer from 0 to 2; provided that: the sum of m+n does not exceed 10; and when both Z1 and Z2 are hydrogen, the sum of m+n is greater than 0, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.
    Type: Grant
    Filed: December 3, 2015
    Date of Patent: April 17, 2018
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Julie F. Liu, Scott L. Harbeson, Roger D. Tung
  • Patent number: 9938244
    Abstract: The invention relates to a process for manufacturing the compound of formula I wherein R is H, (C1-C6)alkyl or benzyl, or a salt thereof, said process comprising the reaction of the compound of formula I-1 wherein X is Br, Cl or F, or a salt thereof, with the compound of formula I-2 wherein R is H, (C1-C6)alkyl or benzyl, or a salt thereof, in the presence of a base, and, when X is Br or Cl, in the presence of tetra-n-butyl ammonium fluoride hydrate or cesium fluoride. The invention further relates to the compound of formula I-1 and uses thereof.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: April 10, 2018
    Assignee: IDORSIA PHARMACEUTICALS LTD
    Inventors: Stefan Abele, Jacques-Alexis Funel, Ivan Schindelholz
  • Patent number: 9926318
    Abstract: Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity.
    Type: Grant
    Filed: November 20, 2014
    Date of Patent: March 27, 2018
    Assignee: PHARMAKEA, INC.
    Inventors: John Howard Hutchinson, David Lonergan, Martin Rowbottom, Andiliy Gokching Lai
  • Patent number: 9895328
    Abstract: Compositions and method for treating a folate-resistant disease in a subject are disclosed. The methods involve administering to the subject an effective amount of a composition containing a formate. For example, the method can be used to reducing the risk of neural tube defects during pregnancy. The method can also be used to treat other conditions normally treatable by folate supplementation.
    Type: Grant
    Filed: August 13, 2014
    Date of Patent: February 20, 2018
    Assignee: Board of Regents, The University of Texas System
    Inventors: Dean R. Appling, Jessica E. Momb
  • Patent number: 9884864
    Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
    Type: Grant
    Filed: March 9, 2017
    Date of Patent: February 6, 2018
    Assignee: Janssen Sciences Ireland UC
    Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
  • Patent number: 9879019
    Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.
    Type: Grant
    Filed: August 21, 2017
    Date of Patent: January 30, 2018
    Assignee: ABBVIE INC.
    Inventors: Lars Frederick Nordstroem, Ahmad Y. Sheikh
  • Patent number: 9879018
    Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.
    Type: Grant
    Filed: August 21, 2017
    Date of Patent: January 30, 2018
    Assignee: ABBVIE INC.
    Inventors: Mathew M. Mulhern, Lars Fredrick Nordstroem, Ahmad Y. Sheikh
  • Patent number: 9861576
    Abstract: Biocompatible intraocular implants include an alpha-2 adrenergic receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 adrenergic receptor agonist into an eye for an extended period of time. The alpha-2 adrenergic receptor agonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants can be placed in an eye to treat one or more ocular conditions, such as an ocular vasculopathy or glaucoma, including reduction of an elevated intraocular pressure.
    Type: Grant
    Filed: December 19, 2016
    Date of Patent: January 9, 2018
    Assignee: Allergan, Inc.
    Inventors: Lon T. Spada, Alazar N. Ghebremeskel, Michael R. Robinson
  • Patent number: 9855263
    Abstract: A tamper-resistant pharmaceutical dosage form comprising a multitude of particles which comprise a pharmacologically active compound, a polyalkylene oxide, and a disintegrant; wherein the pharmacologically active compound is dispersed in a matrix comprising the polyalkylene oxide and the disintegrant; wherein the content of the disintegrant is more than 5.0 wt.-%, based on the total weight of the pharmaceutical dosage form and/or based on the total weight of the particles; wherein the content of the polyalkylene oxide is at least 25 wt.-%, based on the total weight of the pharmaceutical dosage form and/or based on the total weight of the particles; and wherein the dosage form provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur.
    Type: Grant
    Filed: June 1, 2016
    Date of Patent: January 2, 2018
    Assignee: GRÜNENTHAL GMBH
    Inventors: Klaus Wening, Anja Geiβler, Jana Denker, Lutz Barnscheid
  • Patent number: 9856260
    Abstract: The present invention includes compositions that are useful in preventing or treating metastasis in a subject diagnosed with cancer. The present invention also includes methods of preventing or treating metastasis in a subject diagnosed with cancer, wherein the method comprises administering to the subject in need thereof an effective amount of a pharmaceutical formulation comprising at least one pharmaceutically acceptable carrier and at least one CX3CR1 or fractalkine antagonist.
    Type: Grant
    Filed: June 6, 2016
    Date of Patent: January 2, 2018
    Assignees: Drexel University, Alliance Discovery, Inc.
    Inventors: Alessandro Fatatis, Joseph M. Salvino, Olimpia Meucci, Whitney L. Gladney
  • Patent number: 9856225
    Abstract: The present invention provides novel phenazine derivatives, such as compounds of Formula (I) and (II), and pharmaceutically acceptable salts thereof. The compounds of the invention are expected to be antimicrobial agents and may act by a microbial warfare strategy (e.g., a reactive oxygen species (ROS)-based competition strategy). The present invention also provides pharmaceutical compositions, kits, uses, and methods that involve the compounds of the invention and may be useful in preventing or treating a microbial infection (e.g., a bacterial infection) in a subject, inhibiting the growth and/or reproduction of a microorganism (e.g., a bacterium), killing a microorganism (e.g., a bacterium), inhibiting the formation and/or growth of a biofilm, or reducing or clearing a biofilm.
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: January 2, 2018
    Assignee: University of Florida Research Foundation, Incorporated
    Inventors: Robert William Huigens, III, Shouguang Jin
  • Patent number: 9849130
    Abstract: Methods for treating a subject infected with Clostridium difficile comprises administering to the subject a synergistic combination of clofazimine and metronidazole. Pharmaceutical compositions comprising clofazimine and metronidazole are provided for treating Clostridium difficile infection and diseases or symptoms associated therewith.
    Type: Grant
    Filed: February 1, 2017
    Date of Patent: December 26, 2017
    Assignee: KamTek, Inc.
    Inventors: Venkata M. Reddy, Wolf Prensky, Sharanjit VedBrat
  • Patent number: 9828344
    Abstract: The invention relates to dihydropyridine compounds as inhibitors of the notch signalling pathway and/or inhibitors of secretion for the treatment of secretion-dependent disease, such as cancer or senescence-related ageing, in addition to pharmaceutical compositions thereof and methods of treatment.
    Type: Grant
    Filed: June 3, 2013
    Date of Patent: November 28, 2017
    Assignee: LEIBNIZ-INSTITUT FÜR ALTERSFORSCHUNG FRITZ-LIPMANN-INSTITUT E.V. (FLI)
    Inventors: Christoph Kaether, Andreas Krämer
  • Patent number: 9820985
    Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
    Type: Grant
    Filed: February 26, 2015
    Date of Patent: November 21, 2017
    Assignee: Medivation Technologies LLC
    Inventors: Bing Wang, Daniel Chu
  • Patent number: 9814715
    Abstract: Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.
    Type: Grant
    Filed: June 15, 2016
    Date of Patent: November 14, 2017
    Assignee: Vitae Pharamceuticals, Inc.
    Inventors: Chengguo Dong, Yi Fan, Katerina Leftheris, Stephen D. Lotesta, Suresh B. Singh, Colin M. Tice, Wei Zhao, Yajun Zheng, Linghang Zhuang
  • Patent number: 9796723
    Abstract: Methods for treating a disease or disorder selected from pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection and osteolytic disease in a mammal, which comprise administering to said mammal a therapeutically effective amount of a compound of Formula I in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification.
    Type: Grant
    Filed: January 9, 2017
    Date of Patent: October 24, 2017
    Assignee: Array BioPharma, Inc.
    Inventors: Steven W. Andrews, Julia Haas, Yutong Jiang, Gan Zhang
  • Patent number: RE47221
    Abstract: The invention provides compounds of Formula (I) and Formula (II) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Grant
    Filed: March 1, 2017
    Date of Patent: February 5, 2019
    Assignee: AbbVie Inc.
    Inventors: Neil Wishart, Kristine E. Frank, Michael Friedman, Dawn M. George, Kent D. Stewart, Grier A. Wallace