Spiro Ring System Patents (Class 514/278)
  • Patent number: 11202776
    Abstract: Provided herein is a method of treating or alleviating one or more symptoms of a disorder, disease, or condition mediated by a dopamine D2 or D3 receptor with 3-((1-cyclohexyl-4-oxo-8-(4-oxo-4-phenylbutyl)-1,3,8-triazaspiro[4.5]decan-3-yl)methyl)benzoic acid or a pharmaceutically acceptable salt thereof. Also provided herein is a method of increasing the serum prolactin level with 3-((1-cyclohexyl-4-oxo-8-(4-oxo-4-phenylbutyl)-1,3,8-triazaspiro[4.5]decan-3-yl)methyl)benzoic acid or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 11, 2018
    Date of Patent: December 21, 2021
    Inventor: Emil Chuang
  • Patent number: 11124505
    Abstract: The disclosure provides a process of making the compound of Formula I, and pharmaceutically acceptable salts thereof: and the process of making the intermediate of Formula III: wherein PG is as defined as set forth in the specification.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: September 21, 2021
    Assignee: Minoryx Therapeutics S.L.
    Inventors: Ana Maria García Collazo, Wolter Ten Hoeve, Johannes Nicolaas Koek, Johannes B. M. Rewinkel, Sander De Wilde
  • Patent number: 11103506
    Abstract: The present invention relates to combinations comprising a positive allosteric modulator (“PAM”) of metabotropic glutamatergic receptor subtype 2 (“mGluR2”) or a pharmaceutically acceptable salt or a solvate thereof, or an orthosteric agonist of metabotropic glutamatergic receptor subtype 2 compound or a pharmaceutically acceptable salt or a solvate thereof, and a synaptic vesicle protein 2A (“SV2A”) ligand.
    Type: Grant
    Filed: December 19, 2019
    Date of Patent: August 31, 2021
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Brian D. Klein, Hilde Lavreysen, Stefan Maria Christiaan Pype, Roy E. Twyman, Nancy Eulalie Sylvain Van Osselaer, H. Steven White, Marc André Ceusters, José Maria Cid-Núñez, Andrés Avelino Trabanco-Suárez
  • Patent number: 11059766
    Abstract: The present invention relates to ethynyl derivatives of formula I with variables as defined herein, or to a pharmaceutically acceptable acid addition salt thereof. Compounds of formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
    Type: Grant
    Filed: December 1, 2017
    Date of Patent: July 13, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Eric Vieira
  • Patent number: 11052080
    Abstract: The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3? or GSK3?) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychiatric disorders, metabolic disorders, and cancer.
    Type: Grant
    Filed: November 21, 2018
    Date of Patent: July 6, 2021
    Assignees: The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., The General Hospital Corporation
    Inventors: Florence Fevrier Wagner, Jennifer Q. Pan, Sivaraman Dandapani, Andrew Germain, Edward Holson, Benito Munoz, Partha P. Nag, Michael C. Lewis, Stephen J. Haggarty, Joshua A. Bishop, Kimberly Stegmaier, Michel Weiwer, Versha Banerji
  • Patent number: 10981910
    Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
    Type: Grant
    Filed: June 26, 2020
    Date of Patent: April 20, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guanglin Luo, Carolyn Diane Dzierba, John E. Macor
  • Patent number: 10968178
    Abstract: The present invention aims to provide a heterocyclic compound having an IP6K inhibitory action and expected to be useful as a prophylactic or therapeutic agent for—diseases such as cardiac failure, diabetes and the like. A compound represented by the formula (I): wherein each symbol is as defined in the SPECIFICATION, or a salt thereof has an IP6K inhibitory action and is expected to be useful as a prophylactic or therapeutic agent for diseases such as cardiac failure, diabetes and the like.
    Type: Grant
    Filed: March 29, 2018
    Date of Patent: April 6, 2021
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Yoshito Terao, Masashi Takahashi, Ryoma Hara, Kousuke Hidaka, Hideki Furukawa, Takeshi Yamasaki, Shizuo Kasai
  • Patent number: 10961244
    Abstract: The present invention provides a compound having the structure: or a pharmaceutically acceptable salt or ester thereof, and a method of treating a subject afflicted with pain, a depressive disorder, a mood disorder or an anxiety disorder by administering the compound to the subject.
    Type: Grant
    Filed: March 24, 2017
    Date of Patent: March 30, 2021
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Andrew Kruegel, Dalibor Sames, Madalee G. Wulf, Jonathan A. Javitch
  • Patent number: 10960005
    Abstract: Methods are provided for the treatment of relapsed and/or refractory solid tumors (including neuroendocrine carcinomas (NEC)) and non-Hodgkin's lymphomas (NHLs) and the like, using substituted heterocyclic derivative compounds and pharmaceutical compositions comprising compounds useful for the inhibition of lysine specific demethylase-1 (LSD-1).
    Type: Grant
    Filed: June 10, 2020
    Date of Patent: March 30, 2021
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Jiangchun Xu, Robert Cho, Aaron Nguyen
  • Patent number: 10934269
    Abstract: The present invention relates to a process for the preparation of apalutamide. In particular, the present invention relates to a process for the preparation of apalutamide and its intermediates. The present invention also relates to pharmaceutical compositions comprising apalutamide.
    Type: Grant
    Filed: September 27, 2019
    Date of Patent: March 2, 2021
    Assignee: CADILA HEALTHCARE LIMITED
    Inventors: Kumar Kamlesh Singh, Nikhil Amar Singh, Ganpatdan Shimbhu Charan, Nimeshkumar Mukeshkumar Shah
  • Patent number: 10906874
    Abstract: Binding of the transcriptional co-activator, YAP1, to the transcription factor Oct4, induces Sox2, which is a transcription actor necessary for the self-renewal of stem-like cells from non-small cell lung cancer. The WW domain of YAP1 binds to the PPxY motif of Oct4 to induce Sox2. Delivering a peptide corresponding to the WAV domain could prevent the induction of Sox2 and stemness. Similarly, peptides and mimetics of the PPxY motif would be able to inhibit stemness. Disclosed are compounds that affect the Yap1:Oct4 interaction.
    Type: Grant
    Filed: September 18, 2017
    Date of Patent: February 2, 2021
    Assignee: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.
    Inventors: Srikumar Chellappan, Nicholas J. Lawrence, Sujeewa Ranatunga Mahanthe Mudiyanselage
  • Patent number: 10874649
    Abstract: The present invention is directed to inhibitors of histone deacetylases (HDACs) such as HDAC6, and their use in the treatment of diseases such as cell proliferative diseases (e.g., cancer), neurological (e.g., neurodegenerative disease or neurodevelopmental disease), inflammatory or autoimmune disease, infection, metabolic disease, hematologic disease, or cardiovascular disease.
    Type: Grant
    Filed: December 18, 2019
    Date of Patent: December 29, 2020
    Assignee: Valo Early Discovery, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Mary-Margaret Zablocki
  • Patent number: 10875848
    Abstract: The present disclosure is directed to inhibitors of FASN. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of FASN. For instance, the disclosure is concerned with compounds and compositions for inhibition of FASN, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of FASN, and methods of synthesis of these compounds.
    Type: Grant
    Filed: October 10, 2019
    Date of Patent: December 29, 2020
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Matthew W. Martin, Mary-Margaret Zablocki, Scot Mente, Christopher Dinsmore, Zhongguo Wang, Xiaozhang Zheng
  • Patent number: 10858373
    Abstract: The present invention provides, in part, heterocyclic spiro compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.
    Type: Grant
    Filed: June 3, 2019
    Date of Patent: December 8, 2020
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Laura Ann McAllister, Christopher John Helal, Steven Victor O'Neil, Patrick Robert Verhoest
  • Patent number: 10822335
    Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Grant
    Filed: April 1, 2019
    Date of Patent: November 3, 2020
    Assignee: Pfizer Inc.
    Inventors: Mary Theresa Didiuk, Robert Lee Dow, David Andrew Griffith
  • Patent number: 10779537
    Abstract: In crop production in the fields of agriculture, horticulture and the like, the damage caused by insect pests etc. is still immense, and insect pests resistant to existing insecticides have emerged. Under such circumstances, the development of novel agricultural and horticultural insecticides is desired. The present invention provides an agricultural and horticultural insecticide comprising a 1H-pyrrolo-condensed heterocyclic compound represented by the general formula (1): {wherein A and A1 each represent a nitrogen atom, R3 and R4 each represent a haloalkyl group, R2 represents a hydrogen atom or an acetyl group, R1 represents a halogen atom, and m represents 0 or 2}, an N-oxide thereof or a salt thereof as an active ingredient, and a method for using the insecticide.
    Type: Grant
    Filed: October 12, 2017
    Date of Patent: September 22, 2020
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Yusuke Sano, Ikki Yonemura, Akiyuki Suwa, Shunpei Fujie
  • Patent number: 10759788
    Abstract: Pharmaceutical uses of pyridinecarboxamide derivatives are provided. In particular, pharmaceutical uses of pyridinecarboxamide derivatives represented by general formula (I), wherein the substituents of the formula (I) are defined in the specification, are provided. The pyridinecarboxamide derivatives can be used as therapeutic agents, especially as inhibitors of the Renal Outer Medullary Potassium channel (ROMK) and in the preparation of medicaments for treating and/or preventing ROMK mediated disorders, such as hypertension and heart failure.
    Type: Grant
    Filed: January 25, 2019
    Date of Patent: September 1, 2020
    Assignees: JIANGSU HENGRUI MEDICINE CO., LTD., SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD.
    Inventors: Xin Li, Qing Dong, Piaoyang Sun
  • Patent number: 10702508
    Abstract: Described herein are methods of treating non-metastatic castrate-resistant prostate cancer using an approved drug product comprising apalutamide, enzalutamide or darolutamide. Also described here are drug products containing apalutamide enzalutamide or darolutamide, and methods of selling or offering for sale an anti-androgen drug product.
    Type: Grant
    Filed: April 30, 2018
    Date of Patent: July 7, 2020
    Assignee: Aragon Pharmaceuticals, Inc.
    Inventor: Arturo Molina
  • Patent number: 10689368
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof, wherein Q, R1, R2, R3 and R4 are as defined herein.
    Type: Grant
    Filed: July 1, 2019
    Date of Patent: June 23, 2020
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Michael Alistair O'Brien, Mark Pickworth, Mark David Rackham, Benjamin Gerald Tehan, Barry John Teobald
  • Patent number: 10633384
    Abstract: Compounds having the general formula (I) wherein R1, R2, Y and W are as described herein, compositions including the compounds and methods of using the compounds as autotaxin inhibitors.
    Type: Grant
    Filed: October 13, 2016
    Date of Patent: April 28, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniel Hunziker, Patrizio Mattei, Harald Mauser, Marco Prunotto, Christoph Ullmer
  • Patent number: 10626125
    Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.
    Type: Grant
    Filed: May 23, 2019
    Date of Patent: April 21, 2020
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Laura Ann McAllister, Christopher John Helal, Steven Victor O'Neil, Patrick Robert Verhoest
  • Patent number: 10538530
    Abstract: Compounds are provided that antagonize vasopressin receptors, particularly the V1a receptor products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof: wherein Q1, Q2, Q3, R2a, R2b, R3 and X are as defined herein.
    Type: Grant
    Filed: September 5, 2018
    Date of Patent: January 21, 2020
    Assignee: BlackThorn Therapeutics, Inc.
    Inventors: Robert M. Jones, Mariangela Urbano, Gary Brandt, Mark Chambers, David Hardick, Chris Knight, Jason Tierney, Chris Lock
  • Patent number: 10479796
    Abstract: The present invention provides spiro-oxazolones, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The present compounds are useful as therapeutics acting peripherally and centrally in the conditions of inappropriate secretion of vasopressin, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, aggressive behavior and phase shift sleep disorders, in particular jetlag.
    Type: Grant
    Filed: June 6, 2016
    Date of Patent: November 19, 2019
    Assignee: Hoffman-La Roche Inc.
    Inventors: Valerie Runtz-Schmitt, Patrick Schnider, Cosimo Dolente, Bernhard Fasching
  • Patent number: 10428088
    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 where m, p, q, W, Z, Y, X1, X2, R1, R2, R3 and R4 are as defined herein.
    Type: Grant
    Filed: May 23, 2018
    Date of Patent: October 1, 2019
    Assignee: Heptares Therapeutics Limited
    Inventors: Miles Stuart Congreve, Giles Albert Brown, Benjamin Gerald Tehan, Mark Pickworth, Julie Elaine Cansfield
  • Patent number: 10407428
    Abstract: The present invention relates to spiro-isoquinoline-1,4?-piperidine compounds having dual pharmacological activity towards both the sigma (?) receptor and the ?-opiod receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Grant
    Filed: November 20, 2015
    Date of Patent: September 10, 2019
    Assignee: ESTEVE PHARMACEUTICALS, S.A.
    Inventors: Carmen Almansa-Rosales, Monica Garcia Lopez, Ana-Maria Caamano-Moure
  • Patent number: 10329308
    Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: June 25, 2019
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Laura Ann McAllister, Christopher John Helal, Steven Victor O'Neil, Patrick Robert Verhoest
  • Patent number: 10294225
    Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Grant
    Filed: January 30, 2018
    Date of Patent: May 21, 2019
    Assignee: Pfizer Inc.
    Inventors: Mary Didiuk, Robert Lee Dow, David Andrew Griffith
  • Patent number: 10246459
    Abstract: Use of a tetramic acid compound according to formula (I) or (I?) with a second nematicide as a treatment for crop plants to combat and control nematodes in the soil of said crop plants.
    Type: Grant
    Filed: October 11, 2017
    Date of Patent: April 2, 2019
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: Fabienne Hatt, Anke Buchholz
  • Patent number: 10233158
    Abstract: The present invention relates to the compound of the formula: or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.
    Type: Grant
    Filed: April 4, 2018
    Date of Patent: March 19, 2019
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Patent number: 10226459
    Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: March 12, 2019
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian W. Metcalf
  • Patent number: 10220091
    Abstract: Methods for treating cancer using a combination of an inhibitor of the sonic hedgehog signaling pathway (e.g., LDE225) with radiation and a tumor antigen-specific monoclonal antibody (e.g., heat shock protein (HSP) glucose regulated protein of 94000 daltons (Grp94)-specific mAb W9, or chondroitin sulfate proteoglycan 4 (CSPG4)-targeted mAbs), or with a BRAF inhibitor, e.g., in BRAF inhibitor resistant cancers.
    Type: Grant
    Filed: April 3, 2014
    Date of Patent: March 5, 2019
    Assignee: The General Hospital Corporation
    Inventors: Francesco Sabbatino, Yangyang Wang, Xinhui Wang, Steven Isakoff, Cristina Ferrone, Joe Schwab, Soldano Ferrone
  • Patent number: 10220025
    Abstract: A solid self-micro/nano emulsifying formulation comprising CARP-1 functional mimetics (CFM; e.g., CFM-4.16 or CFM-4.17) for oral administration, and methods of fabrication and use thereof to treat cancer (e.g., breast cancer, triple negative breast cancer, resistant lung cancer, and non-resistant lung cancer) and reduce tumor volume. Solid self-micro/nano emulsifying formulation of CFM compounds was found to have significantly enhanced drug loading, aqueous solubility, and oral bioavailability of the formulation.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: March 5, 2019
    Assignee: Florida A&M University
    Inventors: Mandip Sachdeva, Ketankumar Patel, Arun Rishi
  • Patent number: 10196369
    Abstract: Provided herein are small molecule Epstein-Barr virus-induced G-protein coupled receptor 2 (EBI2) modulator compounds, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds. In some embodiments, EBI2 is a therapeutic target for the treatment of diseases or conditions such as, but not limited to, autoimmune diseases or conditions, cancer, and cardiovascular disease.
    Type: Grant
    Filed: September 26, 2014
    Date of Patent: February 5, 2019
    Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
    Inventors: Anthony B. Pinkerton, Robert Ardecky, Eduard A. Sergienko, Marcos Gonzalez-Lopez, Santhi Reddy Ganji, Jiwen Zou
  • Patent number: 10183963
    Abstract: The present invention relates to methods of treating immune disorders and/or inflammation using certain modulator compounds. In one embodiment, the present invention provides a method of treating an immune and inflammatory disorders disorder by administering a composition comprising a therapeutically effective dosage of an ascaroside compound, or a mixture of ascaroside compounds, or a mixture containing at least one ascaroside.
    Type: Grant
    Filed: December 6, 2017
    Date of Patent: January 22, 2019
    Assignees: California Institute of Technology, Boyce Thompson Institute for Plant Research
    Inventors: Andrea Choe, Paul W. Sternberg, Frank C. Schroeder, Stephan H. Von Reuss
  • Patent number: 10174050
    Abstract: The present invention concerns a spiroisoxazoline compound of general formula (I): in which m and n are 0 or 1, R1 represents, inter alia, an optionally substituted alkyl chain, in particular substituted with fluorine or with a cyclic group, and R2 is chosen from phenyl and optionally substituted benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and the heterocycles having 5 or 6 vertices comprising at least one atom chosen from S, N and O. The present invention also concerns the use of this compound as a drug, in particular in the treatment of bacterial and mycobacterial infections such as tuberculosis in combination with an antibiotic that is active against bacteria and/or mycobacteria, said compound potentiating the activity of said antibiotic.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: January 8, 2019
    Assignee: Universite de Droit et de la Sante de Lille 2
    Inventors: Nicolas Willand, Benoit Deprez, Alain Baulard, Priscille Brodin, Matthieu Frederik Desroses, Laurence Agouridas-Dutot
  • Patent number: 10172838
    Abstract: A solid self-micro/nano emulsifying formulation comprising CARP-1 functional mimetics (CFM; e.g., CFM-4.16 or CFM-4.17) for oral administration, and methods of fabrication and use thereof to treat cancer (e.g., breast cancer, triple negative breast cancer, resistant lung cancer, and non-resistant lung cancer) and reduce tumor volume. Solid self-micro/nano emulsifying formulation of CFM compounds was found to have significantly enhanced drug loading, aqueous solubility, and oral bioavailability of the formulation.
    Type: Grant
    Filed: March 15, 2017
    Date of Patent: January 8, 2019
    Assignee: Florida A&M University
    Inventors: Mandip Sachdeva, Ketankumar Patel, Arun Rishi
  • Patent number: 10174052
    Abstract: There are disclosed a series of quinuclidines having the Formula (I), which bind to the nicotinic ?7 receptor and may be useful for the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: November 3, 2015
    Date of Patent: January 8, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: James H. Cook, II, F. Christopher Zusi, Matthew D. Hill
  • Patent number: 10150769
    Abstract: Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: June 12, 2018
    Date of Patent: December 11, 2018
    Assignee: Aptinyx Inc.
    Inventor: M. Amin Khan
  • Patent number: 10072017
    Abstract: The invention relates to a compound of Formula I or IA compositions comprising compounds of Formula I or IA, and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:
    Type: Grant
    Filed: December 28, 2016
    Date of Patent: September 11, 2018
    Assignee: Flatley Discovery Lab, LLC
    Inventors: Michael P. Zawistoski, Asmita Deshpande, Bridget M. Cole
  • Patent number: 10035816
    Abstract: The present invention declares a kind of compound to treat respiratory syncytial virus infection and its preparation method and application. The compound stated is cyclopamine's chemical analogs, has the property of inhibiting respiratory syncytial virus replication, and does not have the property of inhibiting Hedgehog signaling pathways. The preparation method stated is to get the cyclopamine's chemical analogs through drug chemical synthesis, then to screen the analogs with two parallel in vitro experiment. The compound described can be used to treat respiratory virus infection, paramyxovirus, respiratory syncytial virus infection, capillary bronchitis/pneumonia/tympanitis caused by respiratory syncytial virus. Furthermore, the compound described never cause the side effects of fetal malformation, and it overcame the teratogenicity of cyclopamine, and filled the gap of anti-human respiratory syncytial virus drug, especially of the field of pediatric drug.
    Type: Grant
    Filed: December 7, 2017
    Date of Patent: July 31, 2018
    Assignee: SHANDONG UNIVERSITY
    Inventors: Ralf Altmeyer, Jingjing Cao
  • Patent number: 10030021
    Abstract: In one aspect, the invention provides compounds of Formula I: (I) and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, Y, Za are defined as set forth in the disclosure. The invention also provides compounds of any one of Formulae II to VII, IA to IC, and IIA to IIC, and pharmaceutically acceptable salts and solvates thereof. Other aspects of the invention include the use of compounds of Formulae I to VII, IA to IC, and IIA to IIC, and pharmaceutically acceptable salts and solvates thereof for the treatment of disorders responsive to modulation of one or more opioid receptors. In certain embodiments, the Compounds of the Invention are useful for treating pain.
    Type: Grant
    Filed: May 26, 2015
    Date of Patent: July 24, 2018
    Assignee: Purdue Pharma L.P.
    Inventors: Mark A. Youngman, Laykea Tafesse, R. Richard Goehring, Jianming Yu
  • Patent number: 10011601
    Abstract: The present invention relates to compounds according to Formula 1 and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancer, lymphocyte homing, chronic inflammation, neuropathic pain, fibrotic diseases, thrombosis, and cholestatic pruritus, mediated at least in part by ATX.
    Type: Grant
    Filed: April 3, 2015
    Date of Patent: July 3, 2018
    Assignee: X-Rx, Inc.
    Inventors: Lee Babiss, Matthew Clark, Anthony D. Keefe, Mark J. Mulvihill, Haihong Ni, Louis Renzetti, Frank Ruebsam, Ce Wang, Zhifeng Xie, Ying Zhang
  • Patent number: 10000502
    Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the antagonism of one or more androgen receptor types. Such compounds are represented by Formula (I) as follows: wherein R1 and G are defined herein.
    Type: Grant
    Filed: January 11, 2017
    Date of Patent: June 19, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gilles Bignan, Peter J Connolly, Ian Hickson, Lieven Meerpoel, Vineet Pande, Zhuming Zhang, Jonathan Branch, Christian Rocaboy, Luis B Trabalón Escolar
  • Patent number: 9956193
    Abstract: Sustained release compositions of sotalol, or a pharmaceutically acceptable salt thereof, are provided. In certain examples, sotalol, or a pharmaceutically acceptable salt thereof, may be administered in an effective amount to provide a therapeutic effect to a patient, such as, for example, a patient suffering from a cardiac disorder. In some examples, sotalol combined with a sustained release system may be administered to provide a sustained release of sotalol for a desired period, e.g., at least about 24 hours.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: May 1, 2018
    Assignee: The Roshni Singh 2015 Trust
    Inventor: Bramah N. Singh
  • Patent number: 9957238
    Abstract: The present invention relates to the compound of the formula: or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.
    Type: Grant
    Filed: March 1, 2017
    Date of Patent: May 1, 2018
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Patent number: 9943508
    Abstract: There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of Alzheimer type dementia in combination with an acetyl choline esterase inhibitor (AChEI) and pharmaceutical compositions comprising (a) a 5HT3 receptor antagonist, a dopamine antagonist, a H1-receptor antagonist, a cannabinoid agonist, aprepitant or casopitant as an antiemetic agent and (b) an acetylcholine esterase inhibitor are also described.
    Type: Grant
    Filed: July 17, 2017
    Date of Patent: April 17, 2018
    Assignee: Chase Pharmaceuticals Corporation
    Inventors: Thomas N. Chase, Kathleen E. Clarence-Smith
  • Patent number: 9908883
    Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Grant
    Filed: August 15, 2016
    Date of Patent: March 6, 2018
    Assignee: Pfizer Inc.
    Inventors: Mary Didiuk, Robert Lee Dow, David Andrew Griffith
  • Patent number: 9873699
    Abstract: An anti-cancer agent having the formula: wherein Ph is a phenyl group and Ar is an aromatic group independently selected from the group consisting of phenyl, 2-bromophenyl, 4-bromophenyl, 2-chlorophenyl, 2,4, dichlorophenyl, 4-chlorophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2 methoxyphenyl, 3-methoxyphenyl, 4-methoxyphenyl, and 3-nitrophenyl; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 17, 2017
    Date of Patent: January 23, 2018
    Assignee: KING SAUD UNIVERSITY
    Inventors: Abdulrahman I. Almansour, Natarajan Arumugam, Raju Suresh Kumar, Periasamy Vaiyapuri Subbarayan, Ali Abdullah Alshatwi, Jegan Athinarayanan
  • Patent number: 9868754
    Abstract: The present invention relates to methods of treating immune disorders and/or inflammation using certain modulator compounds. In one embodiment, the present invention provides a method of treating an immune and inflammatory disorders disorder by administering a composition comprising a therapeutically effective dosage of an ascaroside compound, or a mixture of ascaroside compounds, or a mixture containing at least one ascaroside.
    Type: Grant
    Filed: August 8, 2012
    Date of Patent: January 16, 2018
    Assignees: California Institute of Technology, Boyce Thompson Institute for Plant Research
    Inventors: Andrea Choe, Paul W. Sternberg, Frank C. Schroeder, Stephan H. Von Reuss
  • Patent number: 9845330
    Abstract: The present invention relates to newer generation of triazoles, tetrazoles, isoxazoles, urea and sulphonamide functionalities containing 6-nitro-2,3-dihydronitroimidazooxazoles agents of formula 1, their method of preparation, and their use as drugs for treating Mycobacterium tuberculosis, MDR-TB and XDR-TB either alone or in combination with other anti-tubercular agents. In the present invention, new generation 6-nitro-2,3-dihydronitroimidazooxazoles agents also show acceptable pharmacokinetic properties and synergistic or additive effects with known anti-tubercular drugs.
    Type: Grant
    Filed: March 31, 2014
    Date of Patent: December 19, 2017
    Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Parvinder Pal Singh, Gurunadham Munagala, Reddy Yempalla Kushalava, Inshad Ali Khan, Nitin Pal Kalia, Vikrant Singh Rajput, Amit Nargotra, Sanghapal Damodhar Sawant, Ram Asray Vishwakarma