Oxadiazoles (including Hydrogenated) Patents (Class 514/364)
  • Patent number: 11958845
    Abstract: The present invention provides a heterocyclic compound having a HDAC6 inhibitory action, which is useful for the treatment of central nervous system diseases including neurodegenerative diseases, and the like, and a medicament comprising the compound. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof.
    Type: Grant
    Filed: September 26, 2022
    Date of Patent: April 16, 2024
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masahiro Ito, Hideyuki Sugiyama, Takeshi Yamamoto, Keiko Kakegawa, Jinxing Li, Junsi Wang, Takahito Kasahara, Masato Yoshikawa
  • Patent number: 11958816
    Abstract: A N?-({[(5-phenyl-1,3,4-oxadiazol-2-yl)sulfanyl]acetyl}oxy)benzenecarboximidamide compound, its synthesis, and its use as an antimicrobial agent.
    Type: Grant
    Filed: October 13, 2023
    Date of Patent: April 16, 2024
    Assignee: KING FAISAL UNIVERSITY
    Inventors: Mai Mostafa Khalaf Ali, Hany Mohamed Abd El-Lateef Ahmed, Antar Ahmed Abdelhamid Ahmed, Amer A. Amer
  • Patent number: 11932632
    Abstract: A N?-(2-(5-phenyl-1,3,4-oxadiazol-2-ylthio)acetoxy)benzo[d][1,3]dioxole-5-carboximidamide compound, its synthesis, and its use as an antimicrobial agent.
    Type: Grant
    Filed: October 13, 2023
    Date of Patent: March 19, 2024
    Assignee: KING FAISAL UNIVERSITY
    Inventors: Mai Mostafa Khalaf Ali, Hany Mohamed Abd El-Lateef Ahmed, Antar Ahmed Abdelhamid Ahmed, Amer A. Amer
  • Patent number: 11926621
    Abstract: A N?-(2-(5-(4-chlorophenyl)-1,3,4-oxadiazol-2-ylthio) acetoxy)benzo[d][1,3]dioxole-5-carboximidamide compound, its synthesis, and its use as an antimicrobial agent.
    Type: Grant
    Filed: October 12, 2023
    Date of Patent: March 12, 2024
    Assignee: KING FAISAL UNIVERSITY
    Inventors: Mai Mostafa Khalaf Ali, Hany Mohamed Abd El-Lateef Ahmed, Antar Ahmed Abdelhamid Ahmed, Amer A. Amer
  • Patent number: 11919872
    Abstract: A N?-(2-(5-(4-chlorophenyl)-1,3,4-oxadiazol-2-ylthio)acetoxy)benzimidamide compound, its synthesis, and its use as an antimicrobial agent.
    Type: Grant
    Filed: October 11, 2023
    Date of Patent: March 5, 2024
    Assignee: KING FAISAL UNIVERSITY
    Inventors: Mai Mostafa Khalaf Ali, Hany Mohamed Abd El-Lateef Ahmed, Antar Ahmed Abdelhamid Ahmed, Amer A. Amer
  • Patent number: 11905264
    Abstract: A N?-(2-(5-(4-chlorophenyl)-1,3,4-oxadiazol-2-ylthio)acetoxy)-4-nitrobenzimidamide compound, its synthesis, and its use as an antimicrobial agent.
    Type: Grant
    Filed: October 13, 2023
    Date of Patent: February 20, 2024
    Assignee: KING FAISAL UNIVERSITY
    Inventors: Mai Mostafa Khalaf Ali, Hany Mohamed Abd El-Lateef Ahmed, Antar Ahmed Abdelhamid Ahmed, Amer A. Amer
  • Patent number: 11884655
    Abstract: The present embodiments are directed, in part, to processes and compositions that can, for example, be used in the preparation compounds of Formula (I), or a pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 17, 2020
    Date of Patent: January 30, 2024
    Assignee: Trevena, Inc.
    Inventors: Brian H. Heasley, Jennifer Wilent, Patrick J. Koestler
  • Patent number: 11878981
    Abstract: The present disclosure provides certain substituted 1,2,4-oxadiazole derivatives of the below formula (I) that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.
    Type: Grant
    Filed: April 13, 2022
    Date of Patent: January 23, 2024
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Florian Paul Christian Binder, Georg Dahmann, Martin Thomas Fleck, Annekatrin Charlotte Heimann, Thorsten Oost
  • Patent number: 11771682
    Abstract: A method for treating AR+ breast cancer in a subject comprising administering to the subject an AR agonist (e.g., SARMs such as RAD140), or in combination with one or more therapeutic agents selected from the group consisting of cdk4/6 inhibitors, m-TOR inhibitors, PI3k inhibitors, PARP inhibitors, BCL-2 inhibitors, and MCL-1 inhibitors.
    Type: Grant
    Filed: November 26, 2019
    Date of Patent: October 3, 2023
    Assignee: Ellipses Pharma Ltd.
    Inventors: Gary Hattersley, Jamal Saeh, Ziyang Yu, Chris Miller, Teeru Bihani
  • Patent number: 11453661
    Abstract: The present invention provides a heterocyclic compound having a HDAC6 inhibitory action, which is useful for the treatment of central nervous system diseases including neurodegenerative diseases, and the like, and a medicament comprising the compound. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof.
    Type: Grant
    Filed: September 24, 2020
    Date of Patent: September 27, 2022
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masahiro Ito, Hideyuki Sugiyama, Takeshi Yamamoto, Keiko Kakegawa, Jinxing Li, Junsi Wang, Takahito Kasahara, Masato Yoshikawa
  • Patent number: 11439623
    Abstract: A method of modulating ribonucleotide reductase activity in a neoplastic cell includes administering to the cell an amount of a triazole or an oxadiazole ribonucleotide reductase modulator (RRmod), the amount being effective to inhibit neoplastic cell growth.
    Type: Grant
    Filed: April 4, 2018
    Date of Patent: September 13, 2022
    Assignee: CASE WESTERN RESERVE UNIVERSITY
    Inventors: Chris G. Dealwis, Rajesh Viswanathan, Sarah E. Huff, William Harte
  • Patent number: 11370766
    Abstract: Provided in the present application are a sulfonyl amidine as represented by formula (I) as an indoleamine-2,3-dioxygenase inhibitor, and a preparation method therefor and the use thereof. The compound of formula (I) in the present application can be used as an indoleamine-2,3-dioxygenase inhibitor in the preparation of a drug for preventing and/or treating indoleamine-2,3-dioxygenase-mediated diseases.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: June 28, 2022
    Assignee: SHANGHAI LONGWOOD BIOPHARMACEUTICALS CO., LTD.
    Inventors: Zhe Wang, Zhihong Zeng
  • Patent number: 11342573
    Abstract: The present invention relates to a class of polymer ion imbibed membranes for electrolyte flow batteries. The membranes are a conducting aromatic polyether type copolymer bearing nitrogen heterocycles groups, especially pyridine type. While the membranes can be used in acid, basic, and neutral electrolytes, the nitrogen heterocycles in the membrane interact with acid in the electrolyte to form a proton transport network, so as to keep the proton transport performance of the membrane. The membrane has excellent mechanical stability and thermostability as well as tunable porosity.
    Type: Grant
    Filed: March 2, 2020
    Date of Patent: May 24, 2022
    Assignee: ADVENT TECHNOLOGIES INC.
    Inventors: George Paloumbis, Christos L. Chochos, Emory Sayre De Castro, Nora Gourdoupi, Ryan Pavlicek, Manav Sharma, Vasilis G. Gregoriou
  • Patent number: 11337972
    Abstract: A pharmaceutical preparation includes a first active component, a second active component and pharmaceutically acceptable excipients. The first active component is at least one selected from the group consisting of a neutral endopeptidase inhibitor and a precursor, an active metabolite, a stereoisomer, a pharmaceutically acceptable salt, a prodrug and a solvate thereof. The second active component is at least one selected from the group consisting of a compound represented by the following formula (I) or a precursor, an active metabolite, a stereoisomer, a pharmaceutically acceptable salt, a prodrug and a solvate thereof. The pharmaceutically acceptable excipients include one or more disintegrants and/or one or more fillers.
    Type: Grant
    Filed: March 8, 2019
    Date of Patent: May 24, 2022
    Assignees: WUHAN LL SCIENCE AND TECHNOLOGY DEVELOPMENT CO., LTD., WUHAN QR PHARMACEUTICALS CO., LTD., WUHAN ZY PHARMACEUTICALS CO., LTD.
    Inventors: Xiaojing Hu, Lina Qian, Zhichao Zhang, Yuanping Wang, Yongkai Chen, Wei Feng, Wenwen Qi, Chaodong Wang
  • Patent number: 11311517
    Abstract: The present invention relates to a composition of a CD47-SIRP? blocking agent and one or more anti-cancer agent(s), where the CD47-SIRP? blocking agents are represented by a compound of formula (I). The present invention also relates to a method of treating a cancer in a subject by administering a therapeutically effective amount of a CD47-SIRP? blocking agent represented by formula (I) in combination with one or more anti-cancer agent(s).
    Type: Grant
    Filed: November 8, 2019
    Date of Patent: April 26, 2022
    Assignee: AURIGENE DISCOVERY TECHNOLOGIES LIMITED
    Inventors: Muralidhara Ramachandra, Pottayil Govindan Nair Sasikumar, Girish Chandrappa Daginakatte, Kiran Aithal Balkudru
  • Patent number: 11299457
    Abstract: This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds.
    Type: Grant
    Filed: May 12, 2020
    Date of Patent: April 12, 2022
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Philip Stewart Turnbull, Rodolfo Cadilla
  • Patent number: 11292788
    Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein Ar, Z and Y are as described herein and R1 is a group of the structure wherein n is 0 or 1; R2 is H, deuterium or methyl; R3 is methyl, trifluoromethyl, ethyl, or taken with R2 together forms a cyclopropyl group, or R3 forms a methylene bridge to the carbon atom marked *, which are suitable for the treatment of autoimmune diseases and chronic inflammation.
    Type: Grant
    Filed: September 6, 2018
    Date of Patent: April 5, 2022
    Assignee: Immunic AG
    Inventors: Jakob Felding, Hella Kohlhof, Manfred Groppel, Rolf Andreas Muhler, Daniel Vitt, Carine Chevrier, Mirko Zaja, Stefan Tasler
  • Patent number: 11207302
    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 15, 2020
    Date of Patent: December 28, 2021
    Assignees: Incyte Corporation, Incyte Holdings Corporation
    Inventors: Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Wenyu Zhu, Jiacheng Zhou, Qiyan Lin, Lingkai Weng, Tai-Yuen Yue, Pingli Liu
  • Patent number: 11207300
    Abstract: The invention relates to compounds for the treatment of ribosomopathies. In particular, it refers to compounds for the treatment of Shwachman-Diamond Syndrome (SDS) and other ribosomopathies, such as Diamond-Blackfan Anemia (DBA), X-linked dyskeratosiscongenita (DKC) and Treacher Collins syndrome (TCS).
    Type: Grant
    Filed: September 13, 2017
    Date of Patent: December 28, 2021
    Inventor: Marco Cipolli
  • Patent number: 11180518
    Abstract: The present invention relates to a compound represented by the formula (E) which is useful for treating or preventing melanoma.
    Type: Grant
    Filed: May 11, 2018
    Date of Patent: November 23, 2021
    Assignees: MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V., LUDWIG-MAXIMILIANS-UNIVERSITÄT MÜNCHEN
    Inventors: Dorothea Becker, Thomas M. Jovin, Christian Griesinger, Andrei Leonov, Sergey Ryazanov, Armin Giese, Tiago F. Outeiro, Diana F. Lazaro, Michael P. Schön, Margarete Schön
  • Patent number: 11147275
    Abstract: The present invention relates to trifluoromethyloxadiazoles of the formula (I), or the N-oxides, or the agriculturally useful salts thereof; to a process for preparing compounds of the formula (I); to intermediates which are useful in the preparation of compounds of the formula (I); to the use of compounds of the formula (I) for controlling phytopathogenic fungi; to a method for combating phytopathogenic harmful fungi, which process comprises treating the fungi, the plants, the soil or seeds to be protected against fungal attack, with an effective amount of at least one compound of the formula (I), or an N-oxide, or an agriculturally acceptable salt thereof; and to agrochemical compositions comprising at least one compound of the formula (I), or an N-oxide, or an agriculturally acceptable salt thereof; and to agrochemical compositions further comprising seeds.
    Type: Grant
    Filed: November 7, 2018
    Date of Patent: October 19, 2021
    Assignee: BASF SE
    Inventors: Christine Wiebe, Wassilios Grammenos, Violeta Terteryan-Seiser, Maria Angelica Quintero-Palomar, Marcus Fehr, Tobias Mentzel, Ian Robert Craig, Georg Christoph Rudolf, Thomas Grote, Christian Winter, Ana Escribano Cuesta, Jan Klaas Lohmann, Michael Seet, Bernd Mueller
  • Patent number: 11096928
    Abstract: The present invention relates to a pharmaceutical composition comprising: (a) at least one neutral endopeptidase inhibitor or a pharmaceutically acceptable salt or ester thereof, (b) at least one compound represented by formula (I) or a pharmaceutically acceptable salt or ester thereof, and a pharmaceutically acceptable carrier. Combined administration showed better medicinal effects than separate administration.
    Type: Grant
    Filed: September 27, 2017
    Date of Patent: August 24, 2021
    Assignee: WUHAN LL SCIENCE AND TECHNOLOGY DEVELOPMENT CO., LTD.
    Inventors: Chaodong Wang, Yongkai Chen, Liu Hu, Xian Zeng, Daiwu Kang
  • Patent number: 11040948
    Abstract: The invention relates to crystalline forms of a 3-substituted 1,2,4-oxadiazole compound, including an anhydrous crystalline form, methods of their preparation, and related pharmaceutical preparations thereof. The invention also relates to preparations suitable for pharmaceutical, veterinary, and agriculturally-relevant uses.
    Type: Grant
    Filed: September 27, 2018
    Date of Patent: June 22, 2021
    Assignee: Curis, Inc.
    Inventor: Shu Yu
  • 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: 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: 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: 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