At Least Three Rings In The Polycyclo Ring System Patents (Class 514/250)
  • Patent number: 11311544
    Abstract: CRF1 receptor antagonists have the potential to directly inhibit ACTH release in patients with CAH and thereby allow normalization of androgen production while using lower, more physiologic doses of hydrocortisone, and thus reducing treatment-associated side effects.
    Type: Grant
    Filed: August 4, 2021
    Date of Patent: April 26, 2022
    Assignee: Neurocrine Biosciences, Inc.
    Inventor: Dimitri E. Grigoriadis
  • Patent number: 11311547
    Abstract: The present invention provides prodrugs and methods of use thereof.
    Type: Grant
    Filed: May 24, 2021
    Date of Patent: April 26, 2022
    Assignee: Board of Regents of the University of Nebraska
    Inventors: Howard Gendelman, Benson Edagwa
  • Patent number: 11306094
    Abstract: The invention is directed towards stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid and its hemisulfate salt as well as pharmaceutical compositions and uses thereof in therapy, preferably chemotherapy.
    Type: Grant
    Filed: February 20, 2020
    Date of Patent: April 19, 2022
    Assignee: MERCK & CIE
    Inventors: Rudolf Moser, Viola Groehn, Thomas Egger, Thomas Ammann
  • Patent number: 11292793
    Abstract: The present application relates to solid state forms of Lumateperone p-Tosylate and processes for preparation thereof. The present application provides amorphous Lumateperone p-tosylate and a solid dispersion comprising amorphous Lumateperone p-tosylate and one or more pharmaceutically acceptable polymers and processes for preparation thereof. The compounds are useful as 5-HT2 receptor agonists and antagonists used in treating disorders of the central nervous system including a disorder associated with 5HT2C or 5HT2A receptor modulation.
    Type: Grant
    Filed: April 9, 2018
    Date of Patent: April 5, 2022
    Assignee: DR. REDDY'S LABORATORIES LIMITED
    Inventors: Vishweshwar Peddy, Raja Sekhar Voguri
  • Patent number: 11279707
    Abstract: Compounds of the present application or pharmaceutically acceptable salts thereof are provided and methods involving compounds of the present application as effective inhibitors of NEK are also provided.
    Type: Grant
    Filed: December 21, 2018
    Date of Patent: March 22, 2022
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Quan Cai, Tinghu Zhang
  • Patent number: 11267823
    Abstract: Substituted 1,2,3,3a,4,5,7,9,13,13a-decahydropyrido[1?,2?:4,5]pyrazino[1,2-a]pyrrolo[1,2-c]pyrimidines having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a pharmaceutical composition containing the same, particularly an anti-HIV pharmaceutical composition.
    Type: Grant
    Filed: July 9, 2020
    Date of Patent: March 8, 2022
    Assignees: SHIONOGI & CO., LTD., VIIV HEALTHCARE COMPANY
    Inventors: Brian A. Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
  • Patent number: 11267817
    Abstract: The disclosure provides compounds of formula (I) having the structure: Compounds of formula (I) are fractalkine receptor agonists and useful in treating, preventing or minimizing metastasis in a subject diagnosed with cancer. The compounds of the invention are further useful in treating central nervous system diseases (such as, but not limited to, HIV Associated Neurocognitive Disorders (HAND), and/or Alzheimer's disease), pain, inflammation (such as, but not limited to, arthritis), cardiovascular disease (such as, but not limited to, undesired vascular smooth muscle proliferation, atherosclerosis, coronary vascular endothelial dysfunction, and/or coronary artery disease), and/or multiple sclerosis.
    Type: Grant
    Filed: May 1, 2018
    Date of Patent: March 8, 2022
    Assignee: Drexel University
    Inventors: Joseph M. Salvino, Xin Feng, Alessandro Fatatis, Fei Shen, Olimpia Meucci
  • Patent number: 11213523
    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: September 16, 2019
    Date of Patent: January 4, 2022
    Assignee: Gilead Sciences, Inc.
    Inventors: Manoj C. Desai, Mingzhe Ji, Haolun Jin, Hyung-Jung Pyun, Teresa Alejandra Trejo Martin
  • Patent number: 11198697
    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: April 14, 2021
    Date of Patent: December 14, 2021
    Assignee: AbbVie Inc.
    Inventors: Ayman Allian, Jayanthy Jayanth, Mohamed-Eslam F. Mohamed, Mathew Mulhern, Fredrik Lars Nordstrom, Ahmed A. Othman, Michael J. Rozema, Lakshmi Bhagavatula, Patrick J. Marroum, Peter T. Mayer, Ahmad Y. Sheikh, Thomas B. Borchardt, Ben Klünder
  • Patent number: 11186584
    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: April 14, 2021
    Date of Patent: November 30, 2021
    Assignee: AbbVie Inc.
    Inventors: Ayman Allian, Jayanthy Jayanth, Mohamed-Eslam F. Mohamed, Mathew Mulhern, Fredrik Lars Nordstrom, Ahmed A. Othman, Michael J. Rozema, Lakshmi Bhagavatula, Patrick J. Marroum, Peter T. Mayer, Ahmad Y. Sheikh, Thomas B. Borchardt, Ben Klünder
  • Patent number: 11179397
    Abstract: The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, therapeutic methods for treating cancers.
    Type: Grant
    Filed: October 2, 2019
    Date of Patent: November 23, 2021
    Assignee: Gilead Sciences, Inc.
    Inventors: Gregory Chin, Michael O' Neil Hanrahan Clarke, Xiaochun Han, Tim Hansen, Yunfeng Eric Hu, Dmitry Koltun, Ryan McFadden, Michael R. Mish, Eric Q. Parkhill, David Sperandio, Lianhong Xu, Hai Yang
  • Patent number: 11160785
    Abstract: The invention relates to compositions comprising a synaptic vesicle glycoprotein 2A (SV2A) inhibitor in an extended release and an acetylcholinesterase inhibitor (AChEIs). The invention also relates to using such compositions in treating cognitive impairment associated with central nervous system disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease (PD), autism, compulsive behavior, and substance addiction.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: November 2, 2021
    Assignee: AgeneBio Inc.
    Inventor: Gardiner Smith
  • Patent number: 11154557
    Abstract: The present invention provides prodrugs and methods of use thereof.
    Type: Grant
    Filed: March 22, 2021
    Date of Patent: October 26, 2021
    Assignee: Board of Regents of the University of Nebraska
    Inventors: Howard Gendelman, Benson Edagwa
  • Patent number: 11066406
    Abstract: 2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK.
    Type: Grant
    Filed: January 29, 2020
    Date of Patent: July 20, 2021
    Assignee: Janssen Pharmaceutica NV
    Inventors: Philippe Fernandes, Paul J. Krawczuk, Mark S. Tichenor
  • Patent number: 11059826
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g., cancer).
    Type: Grant
    Filed: April 23, 2019
    Date of Patent: July 13, 2021
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: David J. Lauffer, Guy Bemis, Michael Boyd, David Deininger, Hongbo Deng, Warren Dorsch, Wenxin Gu, Russell R. Hoover, Mac Arthur Johnson, Jr., Mark Willem Ledeboer, Brian Ledford, Francois Maltais, Marina Penney, Darin Takemoto, Nathan D. Waal, Tiansheng Wang, Pan Li
  • Patent number: 11052083
    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: June 12, 2020
    Date of Patent: July 6, 2021
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Wei Yao, Robert Davis
  • Patent number: 11041856
    Abstract: The invention provides immunochromatographic test strips and methods and systems or kits for detecting and quantifying S-Adenosylmethionine (SAM), S-Adenosylhomocysteine (SAH) and Homocysteine (HCy) in a sample, comprising: (a) making fluorophore conjugated antibodies; (b) immobilizing SAM, SAH and HCy on a solid support; (c) providing a sample, combining said sample with a conjugate selected from the group consisting of lanthanide chelate conjugates and quantum dot conjugates (QD) with anti-SAM, anti-SAH or anti-HCy, wherein said combining is performed under conditions that allow formation of a competitive complex comprising said conjugate, said SAM, SAH or HCy on the solid support and SAM, SAH or HCy in a sample when present; and (d) detecting the presence of the complex, if present, by monitoring a spectral emission mediated by the fluorescent conjugates in the complex, wherein the emission indicates the presence and quantity of SAM, SAH or HCy in the sample.
    Type: Grant
    Filed: September 3, 2018
    Date of Patent: June 22, 2021
    Assignee: HUNAN SKYWORLD BIOTECHNOLOGIES CO
    Inventors: Xiujuan Hao, Chaoyi Deng
  • Patent number: 11020491
    Abstract: The present invention provides a biocompatible conjugate for treating a disease or an injury. The conjugate contains a polymer covalently linked to one or more moieties each containing a polymerizable functional group. The conjugate forms a cross-linked polymer network after being exposed to an elevated level of free radicals associated with the disease or injury.
    Type: Grant
    Filed: June 14, 2018
    Date of Patent: June 1, 2021
    Assignee: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
    Inventors: Christopher Lowe, David I. Shreiber, Emily DiMartini, Adam Gormley
  • 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: 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: 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: 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: 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: 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: 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: RE48842
    Abstract: Provided herein are benzopyrimido-pyrrolo-oxazine-dione (BPO) compounds and pyrimido-pyrrolo-quinoxalinedione (PPQ) compounds, and compositions comprising these compounds, that inhibit cystic fibrosis transmembrane conductance regulator (CFTR) mediated ion transport and that are useful for treating diseases and disorders associated with aberrantly increased CFTR chloride channel activity, such as polycystic kidney disease and secretory diarrheas. The compounds and compositions comprising the compounds described herein may be used for inhibiting expansion or preventing formation of cysts in persons who have polycystic kidney disease.
    Type: Grant
    Filed: January 14, 2020
    Date of Patent: December 7, 2021
    Assignee: The Regents of the University of California
    Inventors: Alan S. Verkman, David S. Snyder