At Least Three Rings In The Polycyclo Ring System Patents (Class 514/250)
  • Patent number: 10995095
    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 and atopic dermatitis), kits, methods of synthesis, and products-by-process.
    Type: Grant
    Filed: December 19, 2019
    Date of Patent: May 4, 2021
    Assignee: AbbVie Inc.
    Inventors: Aileen L. Pangan, Henrique D. Teixeira, Mohamed-Eslam F. Mohamed, Ahmed A. Othman, Ben Klünder
  • Patent number: 10981924
    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 3, 2020
    Date of Patent: April 20, 2021
    Assignee: AbbVie Inc.
    Inventors: Jayanthy Jayanth, Ben Klünder, Mohamed-Eslam Mohamed, Ahmed A. Othman, Patrick J. Marroum, Peter T. Mayer
  • Patent number: 10981888
    Abstract: Methods for preparing compounds of formula (I) Wherein R1 to R5 and A1 to A4 are as defined in the application.
    Type: Grant
    Filed: December 4, 2017
    Date of Patent: April 20, 2021
    Assignee: Bayer CropScience Aktiengesellschaft
    Inventors: Florian Erver, Frank Memmel, Alexander Arlt, Werner Hallenbach, Tobias Harschneck, Christoph Schotes, Robert Velten
  • Patent number: 10981923
    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: June 18, 2020
    Date of Patent: April 20, 2021
    Assignee: AbbVie Inc.
    Inventors: Ayman Allian, Thomas B. Borchardt, Jayanthy Jayanth, Patrick J. Marroum, Peter T. Mayer, Mathew M. Mulhern, Fredrik Lars Nordstrom, Ahmad Y. Sheikh
  • Patent number: 10927129
    Abstract: The present invention is directed to N-[(2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide of the formula: or a pharmaceutically acceptable salt or stereoisomer thereof, and pharmaceutical compositions comprising the same. The present invention has HIV integrase inhibitory activity.
    Type: Grant
    Filed: May 1, 2019
    Date of Patent: February 23, 2021
    Assignees: SHINOGI & CO., LTD., VIIV HEALTHCARE COMPANY
    Inventors: Brian A. Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
  • Patent number: 10918735
    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-a or Formula I-b: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, are provided herein. These biologically active derivatives have been used to effectively treat various diseases including cancer.
    Type: Grant
    Filed: March 5, 2019
    Date of Patent: February 16, 2021
    Assignees: Massachusetts Institute of Technology, The Board of Trustees of the University of Illinois
    Inventors: Mohammad Movassaghi, Justin Kim, Paul Hergenrother, Karen Morrison, Nicolas Boyer
  • Patent number: 10913747
    Abstract: Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine.
    Type: Grant
    Filed: May 15, 2018
    Date of Patent: February 9, 2021
    Assignee: F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Ottorino De Lucchi, Pierluigi Padovan, Elena Brasola
  • Patent number: 10898449
    Abstract: The present invention relates to transdermal therapeutic systems (TTS) for the transdermal administration of asenapine comprising a self-adhesive layer structure containing a therapeutically effective amount of asenapine, such asenapine TTS for use in a method of treatment, processes of manufacture of such TTS as well as asenapine and transdermal therapeutic systems containing asenapine for use in a method of treatment and to a method of treating a human patient by transdermal administration of asenapine.
    Type: Grant
    Filed: February 11, 2020
    Date of Patent: January 26, 2021
    Assignee: LTS LOHMANN THERAPIE-SYSTEME AG
    Inventors: Patrick Mohr, René Rietscher, René Eifler, Olga Bourquain
  • Patent number: 10829499
    Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula 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: June 20, 2019
    Date of Patent: November 10, 2020
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Thomas H. Graham, Tao Yu, Yonglian Zhang, John A. McCauley
  • Patent number: 10813919
    Abstract: Compositions including combinations of class I histone deacetylase (HDAC) inhibitors and programmed cell death protein 1 (PD-1) inhibitors for enhancing antitumor activity are disclosed. Further disclosed are methods of administering these compositions as immunotherapies for suppressing regulatory T cells in renal cell carcinoma.
    Type: Grant
    Filed: January 27, 2017
    Date of Patent: October 27, 2020
    Assignee: Indiana University Research and Technology Corporation
    Inventor: Roberto Pili
  • Patent number: 10787456
    Abstract: Disclosed is a composition and method for a therapeutic treatment that is able to combat certain conditions such as alcohol dependence, opioid abuse treatment, neurological disorders, neuropathic pain, and fibromyalgia. The novel gliotoxin analog compound acts by acting as an antagonist to one or more opioid receptors, which, when present leads to the inhibition of conditions, providing increased performance over known treatments. The disclosed compounds also shows the ability to cross the blood-brain-barrier in a highly efficient manner.
    Type: Grant
    Filed: October 30, 2018
    Date of Patent: September 29, 2020
    Assignee: TEXAS TECH UNIVERSITY SYSTEM
    Inventors: Nadezhda German, Mohammad Anwar Hossain
  • Patent number: 10758530
    Abstract: Described herein are carboxamide derivatives that are useful as inhibitors of p90 ribosomal S6 kinase (RSK), pharmaceutical compositions comprising the derivatives, and methods of using the derivatives in treating diseases or conditions associated with RSK activity. Such carboxamide derivatives form bicyclic and tricyclic ring systems and the disease or condition associated with RSK activity in a mammal is cancer.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: September 1, 2020
    Assignee: PHOENIX MOLECULAR DESIGNS
    Inventors: Sandra E. Dunn, Aarthi Jayanthan, Jaipal Reddy Nagireddy, Subhash Annedi, John H. Van Drie, Timothy S. Daynard, My-my Huynh
  • Patent number: 10758532
    Abstract: Disclosed herein are pharmaceutical compositions, devices, their combinations, and their uses thereof for example in treating or preventing headaches.
    Type: Grant
    Filed: December 11, 2019
    Date of Patent: September 1, 2020
    Assignee: Satsuma Pharmaceuticals, Inc.
    Inventors: John Kollins, Fumiyoshi Iwashima, Detlef Albrecht, Robert David Schultz
  • Patent number: 10752624
    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: May 18, 2018
    Date of Patent: August 25, 2020
    Assignee: ORIGENIS GMBH
    Inventors: Michael Almstetter, Michael Thormann, Andreas Treml, Roland Koestler, Nasser Yehia
  • Patent number: 10736893
    Abstract: In some embodiments, the invention relates to a BTK inhibitor or a pharmaceutically acceptable salt, cocrystal, ester, prodrug, solvate, hydrate or derivative thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, in some embodiments, the present invention relates to imidazopyrazine compounds, pharmaceutical compositions thereof, and the use of the compounds and pharmaceutical compositions in the treatment of a hyperproliferative disorder, an inflammatory disorder, an immune disorder, or an autoimmune disorder.
    Type: Grant
    Filed: November 4, 2016
    Date of Patent: August 11, 2020
    Assignee: Acerta Pharma B.V.
    Inventors: Tjeerd Barf, Edwin de Zwart, Saskia Verkaik, Niels Hoogenboom, Dennis Demont
  • Patent number: 10736972
    Abstract: Described herein is a method of induced cell death via ferroptosis by nanoparticle ingestion. Moreover, the present disclosure describes the administration of high concentrations of ultrasmall nanoparticles at multiple times over the course of treatment in combination with a nutrient-depleted environment, thereby modulating cellular metabolic pathways to induce cell death by the mechanism ferroptosis. Ferroptosis involves iron, reactive oxygen species, and a synchronous mode of cell death execution.
    Type: Grant
    Filed: May 26, 2016
    Date of Patent: August 11, 2020
    Assignees: Memorial Sloan Kettering Cancer Center, Cornell University
    Inventors: Michelle S. Bradbury, Ulrich Wiesner, Michael Overholtzer, Howard Scher, Kai Ma
  • Patent number: 10730883
    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 11, 2020
    Date of Patent: August 4, 2020
    Assignee: AbbVie Inc.
    Inventors: Ayman Allian, Jayanthy Jayanth, Ben Klünder, Mohamed-Eslam F. Mohamed, Ahmed A. Othman, Patrick J. Marroum, Peter T. Mayer
  • Patent number: 10716786
    Abstract: The disclosure provides new transmucosal and subcutaneous pharmaceutical compositions comprising 1-(4-fluoro-phenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or 1-(4-fluoro-phenyl)-4-((6bR,10aS)-2,2-d2-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or comprising -(4-fluoro-phenyl)-4-((6bR,10aS)-1,1,2,2-d4-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one, in free base, co-crystal or salt form, together with methods of making and using them.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: July 21, 2020
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Wei Yao, Robert Davis
  • Patent number: 10702521
    Abstract: The present invention relates to methods for treating Neisseria Gonorrhoeae infection which comprises administering to a subject in need thereof novel 1,2-dihydro-2a,5,8a-triazaacenaphthylene-3,8-dione compounds: or pharmaceutically acceptable salts thereof and/or corresponding pharmaceutical compositions.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: July 7, 2020
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventor: Katherine Louisa Widdowson
  • Patent number: 10695345
    Abstract: The present disclosure relates to pharmaceutical capsules comprising lumateperone, in free, or pharmaceutically acceptable salt form, optionally in combination with one or more additional therapeutic agents, processes for manufacture thereof and methods of use in the treatment or prophylaxis of disease.
    Type: Grant
    Filed: August 30, 2019
    Date of Patent: June 30, 2020
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Robert Davis
  • Patent number: 10696682
    Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
    Type: Grant
    Filed: December 19, 2018
    Date of Patent: June 30, 2020
    Assignee: G1 Therapeutics, Inc.
    Inventors: Francis X. Tavares, Jay Copeland Strum
  • Patent number: 10689399
    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: June 25, 2018
    Date of Patent: June 23, 2020
    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: 10689387
    Abstract: A crystalline form of (1R,2R)-2-[4-(3-Methyl-1H-pyrazol-5-yl)benzoyl]-N-(4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-3-yl)cyclohexanecarboxamide, pharmaceutical compositions containing it and its use in the prevention or treatment of cardiovascular diseases.
    Type: Grant
    Filed: October 27, 2017
    Date of Patent: June 23, 2020
    Assignee: AstraZeneca AB
    Inventor: Anna Matilda Angelica Pettersen
  • Patent number: 10682354
    Abstract: The invention provides methods for the prophylaxis or treatment of one or more disorders associated with dementia comprising administering to a patient in need thereof, a therapeutically effective amount of (i) a 5-HT2A or 5-HT2A/D2 receptor ligand and (ii) a PDE1 inhibitor, and pharmaceutical compositions comprising (i) a 5-HT2A or 5-HT2A/D2 receptor ligand and (ii) a PDE1 inhibitor.
    Type: Grant
    Filed: March 28, 2017
    Date of Patent: June 16, 2020
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventor: Lawrence P. Wennogle
  • 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: 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: 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: 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: 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