Oxadiazoles (including Hydrogenated) Patents (Class 514/364)
  • Patent number: 11021452
    Abstract: The present invention relates to a process for the preparation of substituted 3-aryl-5-trifluoromethyl-1,2,4-oxadiazoles (compounds I), which can be obtained through reaction of hydroxyamidine compounds of formula II with trifluoroacetyl halides IIa.
    Type: Grant
    Filed: July 21, 2018
    Date of Patent: June 1, 2021
    Assignee: BASF SE
    Inventors: Christopher Koradin, Wassilios Grammenos, Michael Rack, Kailaskumar Borate, Roland Goetz
  • Patent number: 10934255
    Abstract: Compounds that inhibit histone (HDACI) and/or activate Nrf2 and HIF, and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC and/or activation of Nrf2 and HIF provide a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
    Type: Grant
    Filed: April 25, 2018
    Date of Patent: March 2, 2021
    Assignee: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Irina Gaisina, Alan Kozikowski
  • Patent number: 10898483
    Abstract: Provided herein, inter alia, are compositions and methods for generating a immune response in an individual and/or inducing the expression of neoantigens on the surface of abnormal (such as proliferative) cells via promotion of premature termination codon (PTC) read-through of messenger RNAs (mRNAs) bearing PTCs.
    Type: Grant
    Filed: December 23, 2016
    Date of Patent: January 26, 2021
    Assignee: MOONSHOT PHARMA LLC
    Inventor: Angela Christiano
  • Patent number: 10870644
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to crystalline forms of 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid (referred to herein as “BHBA-001”), which, inter alia, is a (selective) retinoic acid receptor beta (RAR?) (e.g., RAR?2) agonist. The present invention also pertains to pharmaceutical compositions comprising such crystalline forms, and the use of such crystalline forms and compositions, both in vitro and in vivo, to (selectively) activate RAR? (e.g., RAR?2), to cause or promote neurite development, neurite outgrowth, and/or neurite regeneration, and in the treatment of diseases and conditions that are mediated by RAR?(e.g., RAR?2), that are ameliorated by the activation of RAR? (e.g., RAR?2), etc., including, e.g., neurological injuries such as spinal cord injuries.
    Type: Grant
    Filed: June 16, 2017
    Date of Patent: December 22, 2020
    Assignee: King's College London
    Inventors: Ronnie Maxwell Lawrence, Edwin Aret, Alan David Borthwick, Jane Theresa Brown, Jonathan Patrick Thomas Corcoran, Maria Beatriz de Castro Vasconcelos Goncalves, Sarkis Barrett Kalindjian
  • Patent number: 10851072
    Abstract: Disclosed herein are inhibitors of Rho/MRTF/SRF-mediated gene transcription, and methods for their use in treating or preventing diseases such as cancer and fibrosis. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the substituents are as described.
    Type: Grant
    Filed: April 5, 2019
    Date of Patent: December 1, 2020
    Assignees: THE REGENTS OF THE UNIVERSITY OF MICHIGAN, BOARD OF TRUSTEES OF MICHIGAN STATE UNIVERSITY
    Inventors: Scott D. Larsen, Richard Neubig, Kim Hutchings, Dylan Kahl, Erika Mathes Lisabeth
  • Patent number: 10829485
    Abstract: Compounds as inhibitors of Activating Transcription Factor 6 (ATF6) are provided. The compounds may find use as therapeutic agents for the treatment of diseases or disorders mediated by ATF6 and may find particular use in the treatment of viral infections, neurodegenerative diseases, vascular diseases, or cancer.
    Type: Grant
    Filed: April 6, 2019
    Date of Patent: November 10, 2020
    Assignee: BLACK BELT TX LTD
    Inventors: Jennifer Alfaro, Sebastian Belmar, Gonzalo Esteban Núñez Vasquez, Brahmam Pujala, Balaji Dashrath Sathe, Pooja Thakral, Rajesh Kumar Patidar, Sebastian Bernales, Sarvajit Chakravarty
  • Patent number: 10780081
    Abstract: Provided herein are methods for treating multiple sclerosis using (?) 5-((((trans)-2-(4-(benzyloxy)phenyl)cyclopropyl)amino)methyl)-1,3,4-oxadiazol-2-amine, or a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: June 9, 2017
    Date of Patent: September 22, 2020
    Assignee: Oryzon Genomics, S.A.
    Inventors: Tamara Maes, Cristina Mascarò Crusat, David Rotllant Pozo
  • Patent number: 10781189
    Abstract: The present invention relates to 1,2,4-oxadiazole compounds of formula (I) and their use to inhibit the programmed cell death 1 (PD-1) signaling pathway and/or for treatment of disorders by inhibiting an immunosuppressive signal induced by PD-1, PD-L1 or PD-L2.
    Type: Grant
    Filed: March 7, 2016
    Date of Patent: September 22, 2020
    Assignee: Aurigene Discovery Technologies Limited
    Inventors: Pottayil Govindan Nair Sasikumar, Muralidhara Ramachandra, Seetharamaiah Setty Sudarshan Naremaddepalli
  • Patent number: 10744104
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Grant
    Filed: October 5, 2018
    Date of Patent: August 18, 2020
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Adam D. Hughes, Erik Fenster, Melissa Fleury, Roland Gendron, Edmund J. Moran
  • Patent number: 10738007
    Abstract: The present disclosure relates to certain amides and heterocyclic compounds. The present disclosure also relates to uses of these compounds to inhibit Rho-associated protein kinases and treat diseases including autoimmune disorders, graft versus host disease (GVHD), inflammation, cardiovascular disorders, central nervous system disorders, and neoplastic disorders.
    Type: Grant
    Filed: April 24, 2019
    Date of Patent: August 11, 2020
    Assignee: Translation Drug Development, LLC
    Inventors: Tong Wang, Stephen Gately
  • Patent number: 10724072
    Abstract: Use of phospho-Akt as a biomarker for predicting the response, such as resistance, to a compound, wherein phospho-Akt is Akt that has been phosphorylated on one or more residues, with the proviso that fir Akt1, Akt2, and Akt3 the designation phospho-Akt is used to indicate phosphorylation at a site other than T308, T309 or T305 respectively, wherein the compound is a compound of general formula (I) wherein R represents phenyl, thienyl or pyridinyl wherein phenyl is optionally substituted by one or two substituents independently selected from alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, cyano, halo
    Type: Grant
    Filed: May 30, 2018
    Date of Patent: July 28, 2020
    Assignee: Basilea Pharmaceutica AG
    Inventors: Heidi Alexandra Lane, Felix Bachmann
  • Patent number: 10675272
    Abstract: The present invention relates to specific doses of and dosing regimens for using a 1,2,4-oxadiazole benzoic acid compound in treating or preventing diseases associated with nonsense mutations. In particular, the invention relates to specific doses and dosing regimens for the use of 3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid in mammals having diseases associated with nonsense mutations.
    Type: Grant
    Filed: March 29, 2019
    Date of Patent: June 9, 2020
    Assignee: PTC Therapeutics, Inc.
    Inventors: Samit Hirawat, Langdon Miller
  • Patent number: 10668102
    Abstract: This application discloses alginate microencapsulation-mediated differentiation of embryonic stem cells and use of the stem cell differentiation method for the development of effective treatment of various diseases and disorders. The microencapsulation of embryonic stem (ES) cells results in decreased cell aggregation and enhanced neural lineage differentiation through incorporating the soluble inducer retinoic acid (RA) into the permeable microcapsule system. This differentiation process can be augmented by differentiation pathway regulators such as PPAR agonists.
    Type: Grant
    Filed: October 20, 2016
    Date of Patent: June 2, 2020
    Assignee: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
    Inventors: Jean-Pierre Dolle, Rene S. Schloss, Martin L. Yarmush
  • Patent number: 10653677
    Abstract: The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.
    Type: Grant
    Filed: June 19, 2019
    Date of Patent: May 19, 2020
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Wenyu Zhu
  • Patent number: 10646459
    Abstract: The invention provides methods and compositions for treating cancers and myeloproliferative disorders using sphingosine kinase-1 inhibitors, such as SK1-I, and selective sphingosine-1-phosphate receptor agonists, such as ozanimod.
    Type: Grant
    Filed: February 27, 2019
    Date of Patent: May 12, 2020
    Assignee: Enzo Biochem, Inc.
    Inventors: Elazar Rabbani, James J. Donegan
  • Patent number: 10618877
    Abstract: Provided herein are pharmaceutical compositions, which comprise a 1,2,4-oxadiazole benzoic acid or a pharmaceutically acceptable salt thereof. Further provided herein are certain pharmaceutically acceptable salts of a 1,2,4-oxadiazole benzoic acid and methods for making the same. Further provided herein are methods of treating or preventing a disease associated with a nonsense mutation or a premature stop codon, comprising administering such pharmaceutical compositions or pharmaceutically acceptable salts to a patient having a disease associated with a nonsense mutation or a premature stop codon.
    Type: Grant
    Filed: January 18, 2019
    Date of Patent: April 14, 2020
    Assignee: PTC Therapeutics, Inc.
    Inventors: Marla L. Weetall, Ellen Welch, Mandar V. Dali, James Takasugi
  • Patent number: 10611757
    Abstract: Provided are a preparation method for a crystalline form of the compound represented by formula (A), as well as a method for preparation thereof, a composition thereof, and an application thereof in preparing an angiotensin II receptor antagonist or an application in preparing a drug for preventing and/or treating hypertension, chronic heart failure and diabetic nephropathy.
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: April 7, 2020
    Assignees: Wuhan LL Science and Technology Development Co., Ltd., Wuhan QR Pharmaceuticals Co., Ltd.
    Inventors: Sijun Lei, Xiang Fang, Yongkai Chen, Wei Feng, Chaodong Wang
  • Patent number: 10550071
    Abstract: Provided herein are compounds and compositions useful in increasing PPAR? activity. The compounds and compositions provided herein are useful for the treatment of PPAR? related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
    Type: Grant
    Filed: February 15, 2018
    Date of Patent: February 4, 2020
    Assignees: Salk Institute for Biological Studies, Mitobridge, Inc.
    Inventors: Ronald M. Evans, Michael Downes, Thomas J. Baiga, Joseph P. Noel, Emi Kanakubo Embler, Weiwei Fan, John F. W. Keana, Mark G. Bock, Arthur F. Kluge, Mike A. Patane
  • Patent number: 10538516
    Abstract: An amyloid fibril formation inhibitor comprising a compound represented by the following general formulae (I) to (III): wherein Q is —C(?O)—; X is —C(?O)—, —NH—C(?O)—; Y is —(CH2)m—; Z is —(CH2)n—; R1, R2, and R3 are each independently a hydrogen atom, an alkyl group, a hydroxyalkyl group, an alkylaminoalkyl group; and R4 is an amino group, an alkylamino group or the like; or a pharmaceutically acceptable salt thereof or a solvate thereof.
    Type: Grant
    Filed: March 25, 2016
    Date of Patent: January 21, 2020
    Assignee: National Center for Geriatrics and Gerontology
    Inventors: Katsuhiko Yanagisawa, Akiyoshi Kawai
  • Patent number: 10538497
    Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: January 21, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yongxin Han, Abdelghani Achab, Purakkattle Biju, Yongqi Deng, Xavier Fradera, Liangqin Guo, Shuwen He, Joseph Kozlowski, Ravi Kurukulasuriya, Kun Liu, Meredeth Ann McGowan, Qinglin Pu, Nunzio Sciammetta, Hongjun Zhang, Hua Zhou
  • Patent number: 10442777
    Abstract: The present invention relates to the use of novel oxadiazoles of the formula I or an N-oxide and/or their agriculturally useful salts for controlling phytopathogenic fungi, or to a method for combating phytopathogenic harmful fungi, which process comprises treating the fungi or the materials, plants, the soil or seeds to be protected against fungal attack, with an effective amount of at least one compound of formula I or an N-oxide or an agriculturally acceptable salt thereof; and to agrochemical compositions comprising at least one such compound and to agrochemical compositions further comprising seeds.
    Type: Grant
    Filed: September 19, 2018
    Date of Patent: October 15, 2019
    Assignee: BASF SE
    Inventors: Andy Wieja, Christian Winter, Claudia Rosenbaum, Doris Kremzow-Graw, Franz Roehl, Joachim Rheinheimer, Manojkumar Poonoth, Violeta Terteryan, Egon Haden, Ana Escribano Cuesta, Janosch Harald Achenbach, Tobias Mentzel, Christine Wiebe
  • Patent number: 10369137
    Abstract: The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.
    Type: Grant
    Filed: February 23, 2018
    Date of Patent: August 6, 2019
    Assignees: Incyte Corporation, Incyte Holdings Corporation
    Inventors: Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Wenyu Zhu
  • Patent number: 10292981
    Abstract: The present invention relates to compounds of Formula (I), along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I).
    Type: Grant
    Filed: July 6, 2017
    Date of Patent: May 21, 2019
    Assignee: LUPIN LIMITED
    Inventors: Nageswara Rao Irlapati, Gokul Keruji Deshmukh, Vijay Pandurang Karche, Santosh Madhukar Jachak, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 10285980
    Abstract: The present invention relates to specific doses of and dosing regimens for using a 1,2,4-oxadiazole benzoic acid compound in treating or preventing diseases associated with nonsense mutations. In particular, the invention relates to specific doses and dosing regimens for the use of 3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid in mammals having diseases associated with nonsense mutations.
    Type: Grant
    Filed: June 28, 2018
    Date of Patent: May 14, 2019
    Assignee: PTC Therapeutics, Inc.
    Inventors: Samit Hirawat, Langdon Miller
  • Patent number: 10233161
    Abstract: Provided herein are pharmaceutical compositions, which comprise a 1,2,4-oxadiazole benzoic acid or a pharmaceutically acceptable salt thereof. Further provided herein are certain pharmaceutically acceptable salts of a 1,2,4-oxadiazole benzoic acid and methods for making the same. Further provided herein are methods of treating or preventing a disease associated with a nonsense mutation or a premature stop codon, comprising administering such pharmaceutical compositions or pharmaceutically acceptable salts to a patient having a disease associated with a nonsense mutation or a premature stop codon.
    Type: Grant
    Filed: December 12, 2017
    Date of Patent: March 19, 2019
    Assignee: PTC Therapeutics, Inc.
    Inventors: Marla L. Weetall, Ellen Welch, Mandar V. Dali, James Takasugi
  • Patent number: 10123983
    Abstract: The present disclosure is directed to compositions and methods for treating osteoarthritis comprising increasing the expression of Dnmt3b and/or inhibiting aminobutyrate aminotransferase.
    Type: Grant
    Filed: September 14, 2016
    Date of Patent: November 13, 2018
    Assignee: Washington University
    Inventors: Regis J. O'Keefe, Jie Shen, Audrey McAlinden
  • Patent number: 10118906
    Abstract: The present invention relates to the use of novel oxadiazoles of the formula I or an N-oxide and/or their agriculturally useful salts for controlling phytopathogenic fungi, or to a method for combating phytopathogenic harmful fungi, which process comprises treating the fungi or the materials, plants, the soil or seeds to be protected against fungal attack, with an effective amount of at least one compound of formula I or an N-oxide or an agriculturally acceptable salt thereof; and to agrochemical compositions comprising at least one such compound and to agrochemical compositions further comprising seeds.
    Type: Grant
    Filed: June 1, 2015
    Date of Patent: November 6, 2018
    Assignee: BASF SE
    Inventors: Andy Wieja, Christian Winter, Claudia Rosenbaum, Doris Kremzow-Graw, Franz Roehl, Joachim Rheinheimer, Manojkumar Poonoth, Violeta Terteryan, Egon Haden, Ana Escribano Cuesta, Janosch Harald Achenbach, Tobias Mentzel, Christine Wiebe
  • Patent number: 10117434
    Abstract: Provided herein are aqueous suspension concentrate compositions comprising biologically active 3,5-disubstituted-1,2,4-oxadiazoles or salts thereof that are useful, for example, in the control of nematodes.
    Type: Grant
    Filed: December 4, 2013
    Date of Patent: November 6, 2018
    Assignee: Monsanto Technology LLC
    Inventors: Yiwei Ding, Shaun Raj Selness, Urszula J. Slomczynska
  • Patent number: 10034863
    Abstract: The present invention relates to specific doses of and dosing regimens for using a 1,2,4-oxadiazole benzoic acid compound in treating or preventing diseases associated with nonsense mutations. In particular, the invention relates to specific doses and dosing regimens for the use of 3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid in mammals having diseases associated with nonsense mutations.
    Type: Grant
    Filed: October 12, 2016
    Date of Patent: July 31, 2018
    Assignee: PTC Therapeutics, Inc.
    Inventors: Samit Hirawat, Langdon Miller
  • Patent number: 10034864
    Abstract: The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.
    Type: Grant
    Filed: February 27, 2017
    Date of Patent: July 31, 2018
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Wenyu Zhu
  • Patent number: 10028939
    Abstract: The present invention relates to crystalline forms of 3-[5-(2-fluorophenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid, pharmaceutical compositions and dosage forms comprising the crystalline forms, methods of making the crystalline forms and methods for their use for the treatment, prevention or management of diseases ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay.
    Type: Grant
    Filed: March 14, 2016
    Date of Patent: July 24, 2018
    Assignee: PTC Therapeutics, Inc.
    Inventors: Neil G. Almstead, Peter Seongwoo Hwang, Young-Choon Moon
  • Patent number: 9994559
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicycloheteroaryl-heteroaryl-benzoic acid compounds of the following formula (for convenience, collectively referred to herein as “BHBA compounds”), which, inter alia, are (selective) retinoic acid receptor beta (RAR?) (e.g., RAR?2) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RAR? (e.g., RAR?2), to cause or promote neurite development, neurite outgrowth, and/or neurite regeneration, and in the treatment of diseases and conditions that are mediated by RAR? (e.g., RAR?2), that are ameliorated by the activation of RAR? (e.g., RAR?2), etc., including, e.g., neurological injuries such as spinal cord injuries.
    Type: Grant
    Filed: December 16, 2015
    Date of Patent: June 12, 2018
    Assignee: KING'S COLLEGE LONDON
    Inventors: Alan David Borthwick, Mark Trevor Mills, Jane Theresa Brown, Jonathan Patrick Thomas Corcoran, Maria Beatriz De Castro Vasconcelos Goncalves, Sarkis Barret Kalindjian
  • Patent number: 9926275
    Abstract: The present technology relates to compounds and compositions of Formulas I, II, VII, and VIII, and methods using such compounds. The compounds and compositions described herein may be used in the treatment or prophylaxis of addiction, metabolic syndrome, obesity, and/or a CB1 receptor-mediated disorder.
    Type: Grant
    Filed: August 22, 2014
    Date of Patent: March 27, 2018
    Assignee: Northeastern University
    Inventors: Ganeshsingh Arjunsingh Thakur, Ritesh B. Tichkule, Pushkar Mukund Kulkarni, Abhijit Raghunath Kulkarni
  • Patent number: 9913829
    Abstract: The present invention relates to the compound of formula (I) for use in the treatment of a nonsense-mutation-mediated genetic disease.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: March 13, 2018
    Assignees: UNIVERSITE DE DROIT ET DE SANTE DE LILLE, INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), INSTITUT PASTEUR DE LILLE
    Inventors: Fabrice Lejeune, Benoit Deprez, Terence Beghyn, Sara Sofia Gonzalez-Hilarion
  • Patent number: 9902717
    Abstract: The present invention relates to a process for the preparation of Azilsartan Medoxomil Potassium. The invention further relates to novel highly crystalline polymorph of Azilsartan Medoxomil Potassium and composition comprising it. The invention provides thermostable highly crystalline polymorph of Azilsartan Medoxomil Potassium and process to produce a composition comprising the novel highly crystalline polymorph of Azilsartan Medoxomil Potassium.
    Type: Grant
    Filed: March 21, 2016
    Date of Patent: February 27, 2018
    Assignee: UNICHEM LABORATORIES LIMITED
    Inventors: Dhananjay G. Sathe, Dnyaneshwar V. Gawas, Sashikant D. Metkar
  • Patent number: 9890126
    Abstract: Antibacterial and antimalarial IspF inhibitor compounds and compositions are described. Methods include administering described compounds and compositions to treat bacterial or parasitic infections and to inhibit parasite or bacterial growth.
    Type: Grant
    Filed: March 9, 2016
    Date of Patent: February 13, 2018
    Assignees: Board of Trustees of Northern Illinois University, Beryllium Discovery Corp.
    Inventors: Timothy J. Hagen, Zheng Zhang, Zachary Lazowski, Michael Clare, Darren W. Begley
  • Patent number: 9873677
    Abstract: Provided herein are pharmaceutical compositions, which comprise a 1,2,4-oxadiazole benzoic acid or a pharmaceutically acceptable salt thereof. Further provided herein are certain pharmaceutically acceptable salts of a 1,2,4-oxadiazole benzoic acid and methods for making the same. Further provided herein are methods of treating or preventing a disease associated with a nonsense mutation or a premature stop codon, comprising administering such pharmaceutical compositions or pharmaceutically acceptable salts to a patient having a disease associated with a nonsense mutation or a premature stop codon.
    Type: Grant
    Filed: March 5, 2015
    Date of Patent: January 23, 2018
    Assignee: PTC Therapeutics, Inc.
    Inventors: Marla L. Weetall, Ellen Welch, Mandar V. Dali, James Takasugi
  • Patent number: 9861617
    Abstract: Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: January 9, 2018
    Assignee: PTC Therapeutics, Inc.
    Inventors: Gary Mitchell Karp, Seongwoo Hwang, Guangming Chen, Neil Gregory Almstead, Young-Choon Moon
  • Patent number: 9862710
    Abstract: The present invention relates to novel oxazolidinone compounds of general formula (I) having antibiotic activity also against multiresistant bacterial strains.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: January 9, 2018
    Assignees: ISTITUTO EURO MEDITERRANEO DI SCIENZA E TECNOLOGIA, UNIVERSITA' DEGLI STUDI DI MILANO—BICOCCA
    Inventors: Rosario Musumeci, Clementina Elvezia Anna Cocuzza, Cosimo Gianluca Fortuna, Andrea Pace, Antonio Palumbo Piccionello
  • Patent number: 9855250
    Abstract: One example embodiment relates to a method of treating lung cancer by administering a compound of formula I to a subject in need thereof. Another embodiment relates to a method to treat Non-Small Cell Lung Cancer (NSCLC) by administering the compound of formula I to a patient.
    Type: Grant
    Filed: November 14, 2016
    Date of Patent: January 2, 2018
    Assignee: Macau University of Science and Technology
    Inventors: Liang Liu, Elaine Lai-Han Leung, Xiao-Jun Yao, Vincent Kam-Wai Wong, Xi Chen
  • Patent number: 9849146
    Abstract: Provided are methods for treating a NAD comprising administering to a patient suffering from a NAD an inhibitor of NMD and a nonsense suppressor, whereby degradation of NMD susceptible mRNA is decreased and translation termination at a misplaced nonsense codon is blocked.
    Type: Grant
    Filed: June 13, 2012
    Date of Patent: December 26, 2017
    Assignee: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
    Inventors: Tsafi Pe'ery, Michael B. Mathews, Mainul Hoque, Hartmut M. Hanauske-Abel
  • Patent number: 9789094
    Abstract: The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.
    Type: Grant
    Filed: April 7, 2016
    Date of Patent: October 17, 2017
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Wenyu Zhu
  • Patent number: 9771338
    Abstract: The present invention relates to 1,2,4-oxadiazole and 1,2,4-thiadiazole compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signaling pathway. The invention also refers to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.
    Type: Grant
    Filed: October 20, 2016
    Date of Patent: September 26, 2017
    Assignee: Auirgene Discovery Technologies Limited
    Inventors: Pottayil Govindan Nair Sasikumar, Muralidhara Ramachandra, Seetharamaiah Setty Sudarshan Naremaddepalli
  • Patent number: 9737513
    Abstract: The present invention relates to specific doses of and dosing regimens for using a 1,2,4-oxadiazole benzoic acid compound in treating or preventing diseases associated with nonsense mutations. In particular, the invention relates to specific doses and dosing regimens for the use of 3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid in mammals having diseases associated with nonsense mutations.
    Type: Grant
    Filed: November 8, 2016
    Date of Patent: August 22, 2017
    Assignee: PTC Therapeutics, Inc.
    Inventors: Samit Hirawat, Langdon Miller
  • Patent number: 9737534
    Abstract: The present invention relates to compounds of Formula (I), along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I).
    Type: Grant
    Filed: August 31, 2015
    Date of Patent: August 22, 2017
    Assignee: LUPIN LIMITED
    Inventors: Nageswara Rao Irlapati, Gokul Keruji Deshmukh, Vijay Pandurang Karche, Santosh Madhukar Jachak, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 9604945
    Abstract: Derivatives of Sydnonimine and its analogues, which bind selectively to dopamine transporter (DAT) proteins are useful for treating and delaying the progression of disorders and illnesses that are alleviated by inhibiting dopamine reuptake.
    Type: Grant
    Filed: March 27, 2013
    Date of Patent: March 28, 2017
    Assignee: Caliper Life Sciences, Inc.
    Inventors: Hao Chen, Ming Liu, Qi Su, Manish Raisinghani
  • Patent number: 9550793
    Abstract: The present disclosure relates to a series of spirocyclic compounds of formula (I), their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates, hydrates, N-Oxides, Co crystals and formulations thereof. The disclosure also relates to process of preparation of these spirocyclic compounds. These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of acyl CoA diacyl glycerol acyltransferase 1 (DGAT1).
    Type: Grant
    Filed: October 1, 2013
    Date of Patent: January 24, 2017
    Assignee: Advinus Therapeutics Limited
    Inventors: Summon Koul, Debnath Bhuniya, Kasim Mookhtiar, Sandeep Bhosale, Suresh Kurhade, Keshav Naik, Ravikumar Velayutham, Videsh Salunkhe
  • Patent number: 9481658
    Abstract: An optical film including at least one compound represented by formula (1) is disclosed. In the formula, Y11, Y12 and Y13 each independently represent methine or a nitrogen atom; R11, R12 and R13 each independently represent formula (A), (B) or (C) or a hydrogen atom, provided that at least two of R11, R12 and R13 each independently represent formula (A), (B) or (C). In the formulae, L12, L22, and L32 each represent a 5-membered heterocyclic group.
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: November 1, 2016
    Assignee: FUJIFILM Corporation
    Inventors: Ryo Hamasaki, Hideyuki Nishikawa, Makoto Takahashi, Takashi Miyahara, Masuji Motoki, Masaaki Tsukase
  • Patent number: 9474743
    Abstract: The present invention relates to specific doses of and dosing regimens for using a 1,2,4-oxadiazole benzoic acid compound in treating or preventing diseases associated with nonsense mutations. In particular, the invention relates to specific doses and dosing regimens for the use of 3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid in mammals having diseases associated with nonsense mutations.
    Type: Grant
    Filed: March 21, 2014
    Date of Patent: October 25, 2016
    Assignee: PTC Therapeutics, Inc.
    Inventors: Samit Hirawat, Langdon Miller
  • Patent number: 9458126
    Abstract: Disclosed herein is a monomer for binding nano-metal, which is useful for the preparation of a conductor having increased conductivity with ensuring flexibility and transparency. Polymerization of the monomer for binding nano-metal provides a conductive polymer composite including a nano-metal rod. A method of preparing the conductive polymer composite is also provided.
    Type: Grant
    Filed: June 26, 2015
    Date of Patent: October 4, 2016
    Assignee: SAMSUNG ELECTRONICS CO., LTD.
    Inventors: Byung Hee Sohn, Young Kwan Lee, Yi Yoiung Yun, Won Jae Joo