Ring Nitrogen In The Additional Hetero Ring Patents (Class 514/235.5)
  • Patent number: 12097200
    Abstract: The present invention relates to a use of BI853520 or a pharmaceutically acceptable salt thereof in preparing drugs for treating tumors in combination with chemotherapeutic drugs.
    Type: Grant
    Filed: July 5, 2023
    Date of Patent: September 24, 2024
    Assignee: INXMED (NANJING) CO., LTD.
    Inventors: Zaiqi Wang, Jiangwei Zhang
  • Patent number: 11572368
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
    Type: Grant
    Filed: August 11, 2016
    Date of Patent: February 7, 2023
    Assignees: The General Hospital Corporation, The Broad Institute, Inc., Massachusetts Institute of Technology
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen J. Haggarty, Yan-Ling Zhang
  • Patent number: 11541050
    Abstract: This invention relates to pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections such as HCV or HBV.
    Type: Grant
    Filed: September 4, 2020
    Date of Patent: January 3, 2023
    Assignee: JANSSEN SCIENCES IRELAND UC
    Inventors: David Mc Gowan, Pierre Jean-Marie Bernard Raboisson, Werner Embrechts, Tim Hugo Maria Jonckers, Stefaan Julien Last, Serge Maria Aloysius Pieters, Jaromir Vlach
  • Patent number: 11542242
    Abstract: Provided herein are compounds of Formula IV, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.
    Type: Grant
    Filed: August 19, 2020
    Date of Patent: January 3, 2023
    Assignee: REGENACY PHARMACEUTICALS, LLC
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 11459308
    Abstract: The present invention is related to the development of therapeutics and prophylactics for the treatment and/or prevention of filovirus infection in humans and other mammals. A new class of small molecules is disclosed that inhibits the interaction of naturally processed (i.e., proteolytically cleaved) filovirus glycoprotein (GPCL) with its host receptor Niemann-Pick C1 (NPC1) protein and thus block infection of host cells by filoviruses. Also disclosed are methods of using the small molecule inhibitors in the treatment/prevention of filovirus infection.
    Type: Grant
    Filed: December 5, 2017
    Date of Patent: October 4, 2022
    Assignees: Microbiotix, Inc., Albert Einstein College of Medicine, The Government of the United States as Represented by the Secretary of the Army
    Inventors: Terry L. Bowlin, Donald T. Moir, Kartik Chandran, John M. Dye, Jr., John D. Williams, Zachary D. Aron, Jay P. Barbor, Kelly N. Lively, Peter J. Nash, Debra M. Mills, Arnab Basu
  • Patent number: 11433068
    Abstract: This disclosure provides compositions and methods of treating cancer by inhibiting histone methyltransferases alone or in combination by synergistically inhibiting a histone demethylase, or a histone deacetylase (HDAC), or a bromodomain (BRD)-containing protein, or a B-Raf kinase. In particular, the cancers have deficient of SWI/SNF chromatin remodeling complexes because of mutations in one or more of the complex's subunit members.
    Type: Grant
    Filed: September 7, 2017
    Date of Patent: September 6, 2022
    Assignee: THE GENERAL HOSPITAL CORPORATION
    Inventors: David E. Fisher, Qing Yu Weng, Shinichiro Kato
  • Patent number: 11434240
    Abstract: The present invention provides compounds of formula I, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
    Type: Grant
    Filed: July 24, 2020
    Date of Patent: September 6, 2022
    Assignee: Nimbus Lakshmi, Inc.
    Inventors: Craig E. Masse, Jeremy Robert Greenwood, Donna L. Romero, Geraldine C. Harriman, Ronald T. Wester, Mee Shelley, Joshua Jahmil Kennedy-Smith, Markus Dahlgren, Sayan Mondal, Shaughnessy Robinson
  • Patent number: 11420969
    Abstract: Anti-angiogenic treatments, for example treatment of ocular neovascularization or cancer, treatments of hyperpermeability disorders, treatments of neuropathic and neurodegenerative disorders, pain treatments, methods of treating or preventing fibrosis and compounds for use in such methods are described.
    Type: Grant
    Filed: September 26, 2018
    Date of Patent: August 23, 2022
    Assignee: Exonate Limited
    Inventors: Andrew Douglas Baxter, Jonathan Morris, Andrew David Morley
  • Patent number: 11407744
    Abstract: The present disclosure relates to a novel compound and a pharmaceutical composition comprising the same. The compound according to the present disclosure has effects for activating autophagy, and thus can be valuably used for preventing or treating diseases associated with autophagy regulation.
    Type: Grant
    Filed: May 31, 2019
    Date of Patent: August 9, 2022
    Assignee: AUTOPHAGYSCIENCES INC.
    Inventors: Jung Ju Kim, Seong-Won Song, Hye Jeong Shin, Hyeongwan Choi
  • Patent number: 11149035
    Abstract: A compound of formula (I) wherein R1, R2, R3, R4, X, Y, and A are as defined herein. The compounds of the present invention are inhibitors of hematopoletic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne muscular dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Grant
    Filed: June 11, 2018
    Date of Patent: October 19, 2021
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DFVELOPMENT LIMITED
    Inventors: David Norman Deaton, Barry George Shearer, Mark Andrew Youngman
  • Patent number: 11130779
    Abstract: Provided herein are deuterated compounds and compositions useful in increasing PPAR? activity. The compounds have a formula where L5 comprises at least one deuterium. Exemplary species include 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: December 17, 2019
    Date of Patent: September 28, 2021
    Assignee: The Salk Institute for Biological Studies
    Inventors: Ronald M. Evans, Michael Downes
  • Patent number: 10959984
    Abstract: The present invention provides compositions, methods, and kits comprising one or more ROR? inhibitors, alone or in combination with one or more anticancer drugs, such as an anti-androgen drug, that are useful for treating cancer, e.g., prostate cancer, such as castration-resistant prostate cancer (CRPC), and numerous other types of cancer including lung cancer, breast cancer, liver cancer, ovarian cancer, endometrial cancer, bladder cancer, colon cancer, lymphoma, and glioma.
    Type: Grant
    Filed: September 11, 2017
    Date of Patent: March 30, 2021
    Assignee: The Regents of the University of California
    Inventors: Hongwu Chen, June X. Zou, Junjian Wang
  • Patent number: 10946024
    Abstract: The present invention provides a method for treating or alleviating a symptom of a disorder, e.g., immune evasion, cancer-cell induced immune dysfunction, reduced immune response, lowered inflammation, decreased expression of a major histocompatibility complex (MHC), or cancer, characterized by aberrant, misregulated, or increased Enhancer of Zeste Homolog 2 (EZH2) activity in a cell or subject in need thereof by contacting the cell or administering to the subject a therapeutically effective amount of an EZH2 inhibitor.
    Type: Grant
    Filed: June 18, 2019
    Date of Patent: March 16, 2021
    Assignee: Epizyme, Inc.
    Inventor: Heike Keilhack
  • Patent number: 10864159
    Abstract: The present invention relates to an ophthalmic aqueous composition containing PGF2? analogues for treating ocular hypertension and glaucoma, to a method for treating ocular hypertension and glaucoma by administering said composition to a subject in need of such treatment, and to a method for increasing aqueous solubility and stability of PGF2? analogues in an aqueous composition.
    Type: Grant
    Filed: June 18, 2018
    Date of Patent: December 15, 2020
    Assignees: SANTEN PHARMACEUTICAL CO., LTD., AGC INC.
    Inventors: Timo Reunamaki, Pertti Pellinen, Olli Oksala, Kari Lehmussaari
  • Patent number: 10813920
    Abstract: Provided is an agent for treating or preventing a corneal endothelial disorder wherein cell proliferation is required. More specifically, provided is an agent for treating or preventing a corneal endothelial disorder, wherein cell proliferation is required, said agent comprising a p38MAP kinase inhibitor. In a preferred embodiment, the corneal endothelial disorder is a wound. In a preferred embodiment, the p38MAP kinase inhibitor is soluble in water. The p38MAP kinase inhibitor may comprise 4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)-1H-imidazole (SB203580) or a salt thereof.
    Type: Grant
    Filed: November 13, 2014
    Date of Patent: October 27, 2020
    Assignee: THE DOSHISHA
    Inventors: Noriko Koizumi, Naoki Okumura, Shigeru Kinoshita
  • Patent number: 10807952
    Abstract: Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I? and I?? or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.
    Type: Grant
    Filed: February 26, 2018
    Date of Patent: October 20, 2020
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, William Greenlee
  • Patent number: 10772858
    Abstract: This disclosure relates to benzhydrol derivatives for managing conditions related to the Hypoxia Inducible Factor (HIF) pathway such as uses in treating cancer. In certain embodiment, the disclosure contemplates compounds and pharmaceutical compositions. In certain embodiment, the disclosure contemplates compounds disclosed herein as prodrugs, optionally substituted with one or more substituents, derivatives, or salts thereof.
    Type: Grant
    Filed: May 2, 2016
    Date of Patent: September 15, 2020
    Assignees: GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC., EMORY UNIVERSITY
    Inventors: Binghe Wang, Erwin Van Meir, Jalisa Holmes Ferguson, Stefan Kaluz, Xingyue Ji
  • Patent number: 10745350
    Abstract: The invention relates to new compounds with low cytotoxicity for blocking ubiquitination-proteasome system in diseases. Accordingly, these compounds can be used in treatment of treating disorders including, but not limited to, cancers, neurodegenerative diseases, inflammatory disorders and autoimmune disorders and metabolic disorders.
    Type: Grant
    Filed: July 30, 2016
    Date of Patent: August 18, 2020
    Assignee: Calgent Biotechnology Co., Ltd.
    Inventors: Yun Yen, Jing-ping Liou, Shiow-lin Pan
  • Patent number: 10738010
    Abstract: Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.
    Type: Grant
    Filed: March 13, 2019
    Date of Patent: August 11, 2020
    Assignee: Akebia Therapeutics, Inc.
    Inventors: Christopher M. Lanthier, Boris Gorin, Jan Oudenes, Craig Edward Dixon, Alan Quigbo Lu, James Densmore Copp, John Michael Janusz
  • Patent number: 10577356
    Abstract: The present invention provides compounds having a CB1 receptor-binding moiety and a directing moiety. In related aspects, the invention provides pharmaceutical compositions containing compounds of the invention, methods for inhibiting a pathway modulated in part by the CB1 receptor activity, and methods for treating a condition or disorder mediated in part by CB1 receptor activity. In certain embodiments, the compounds are compounds of Formula I. Methods of preparing compounds of Formula I are also described. In another aspect, the invention provides methods of identifying a selective agonist of the beta-arrestin pathway over the G-protein pathway.
    Type: Grant
    Filed: October 5, 2018
    Date of Patent: March 3, 2020
    Assignee: The University of North Carolina at Greensboro
    Inventors: Patricia H. Reggio, Derek M. Shore, Dow P. Hurst
  • Patent number: 10550149
    Abstract: Provided herein are deuterated compounds and compositions useful in increasing PPAR? activity. The compounds have a formula where L5 comprises at least one deuterium. Exemplary species include 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: June 28, 2018
    Date of Patent: February 4, 2020
    Assignee: Salk Institute for Biological Studies
    Inventors: Ronald M. Evans, Michael Downes
  • Patent number: 10481169
    Abstract: Provided is a novel method and the like for diagnosing a lifestyle disease. The method for diagnosing a lifestyle disease provided by the present invention includes: collecting a biological sample from a subject; measuring the concentration of a fatty acid amide contained in the biological sample; determining whether the subject suffers from a lifestyle disease or a lifestyle disease has progressed when the measured value of the concentration of the fatty acid amide in the sample obtained from the subject is lower than a measurement result obtained from a healthy subject.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: November 19, 2019
    Assignees: TOYOTA JIDOSHA KABUSHIKI KAISHA, NATIONAL UNIVERSITY CORPORATION NAGOYA UNIVERSITY
    Inventors: Koji Uchida, Takahiro Shibata, Kenji Ishikawa, Oi Lun Helena Li, Tadashi Matsushita, Ryosuke Kikuchi, Junzo Ukai
  • Patent number: 10472314
    Abstract: Using a combination of Kumada, Suzuki and Biellmann chemistry, various menaquinones can synthesized rapidly and with stereochemical integrity offering a new way of preparing these vitamin K2 components for the pharmaceutical market. In one embodiment a process for the preparation of a compound of formula (I) is defined including a step in which (i) a compound of formula (II) is reacted with a compound of formula (III) wherein R is an alkyl group; LG is a leaving group; m is an integer from 0 to 8; n is an integer of from 0 to 9; and X is hydrogen, halide, hydroxyl or protected hydroxyl; in the presence of a copper, nickel or palladium catalyst.
    Type: Grant
    Filed: June 20, 2017
    Date of Patent: November 12, 2019
    Assignee: KAPPA BIOSCIENCE AS
    Inventors: Lars Skattebol, Inger Reidun Aukrust, Marcel Sandberg
  • Patent number: 10399950
    Abstract: The present invention relates to novel non-steroidal brassinosteroid mimetic derivatives of formula (I) as defined herein, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: September 3, 2019
    Assignee: Syngenta Partcipations AG
    Inventors: Mathilde Denise Lachia, Pierre Joseph Marcel Jung, Joerg Leipner, David Brocklehurst, Alain De Mesmaeker, Sebastian Volker Wendeborn
  • Patent number: 10357477
    Abstract: The invention provides compounds having the general formula I: and salts thereof, wherein the variables RA, RB, RC, L1, L2, L3, A, B, C, X, Y, Z, E, m, n, and p have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: September 13, 2017
    Date of Patent: July 23, 2019
    Assignee: Regents of the University of Minnesota
    Inventors: Liqiang Chen, Teng Ai
  • Patent number: 10329314
    Abstract: Compounds are provided to modulate the C5a receptor. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: February 28, 2018
    Date of Patent: June 25, 2019
    Assignee: ChemoCentryx, Inc.
    Inventors: Pingchen Fan, Antoni Krasinski, Venkat Reddy Mali, Shichang Miao, Sreenivas Punna, Yang Song, Valentino J. Stella, Yibin Zeng, Penglie Zhang
  • Patent number: 10266492
    Abstract: Intermediates and methods are provided for the preparation of selected C5aR antagonist compounds.
    Type: Grant
    Filed: July 25, 2017
    Date of Patent: April 23, 2019
    Assignee: ChemoCentryx, Inc.
    Inventors: Pingchen Fan, Jaroslaw Kalisiak, Antoni Krasinski, Rebecca M. Lui, Jay Powers, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
  • Patent number: 10266505
    Abstract: The invention describes compounds that inhibit both HDAC and GSK3? (i.e., HDAC/GSK3? dual inhibitors). The invention further describes compositions containing these HDAC/GSK3? dual inhibitors, as well as methods and kits using these HDAC/GSK3? dual inhibitors to treat various medical conditions. The invention also provides methods and kits using a HDAC inhibitor and a GSK3? to treat various medical conditions, and compositions containing a HDAC inhibitor and a GSK3?. Medical conditions treatable with various embodiments of the invention include but are not limited to cancers and tumors.
    Type: Grant
    Filed: June 19, 2018
    Date of Patent: April 23, 2019
    Assignee: CEDARS-SINAI MEDICAL CENTER
    Inventors: Mouad Edderkaoui, Ramachandran Murali, Stephen Pandol
  • Patent number: 10238661
    Abstract: Disclosed are methods for treating various bacterial infections with (2R,4S,4aS)-11-fluoro-2,4-dimethyl-8-[(4S)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]-1,2,4,4a-tetrahydro-2?H,6H-spiro[1,4-oxazino[4,3-a][1,2]oxazolo[4,5-g]quinoline-5,5?-pyrimidine]-2?,4?,6?(1?H,3?H)-trione, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 27, 2015
    Date of Patent: March 26, 2019
    Assignee: Entasis Therapeutics Limited
    Inventor: Michael Huband
  • Patent number: 10189830
    Abstract: Disclosed herein are alkyl-heteroaryl substituted quinone derivative compounds and methods of using such compounds for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: January 29, 2019
    Assignee: BIOELECTRON TECHNOLOGY CORPORATION
    Inventors: Andrew W. Hinman, Kieron E. Wesson, Christopher R. Cornell
  • Patent number: 10155725
    Abstract: The present invention relates to novel anthelmintic compounds of formula (I) below: wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X1, X2, X3, X4, X5, X6, X7 and X8 are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.
    Type: Grant
    Filed: December 28, 2015
    Date of Patent: December 18, 2018
    Assignee: MERIAL, INC.
    Inventors: Charles Q. Meng, Alan Long, Scot Huber, Srinivas Reddy Gurrala, Douglas Edward Wilkinson, Gregory Pacofsky
  • Patent number: 10118914
    Abstract: The present invention provides compounds having a CB1 receptor-binding moiety and a directing moiety. In related aspects, the invention provides pharmaceutical compositions containing compounds of the invention, methods for inhibiting a pathway modulated in part by the CB1 receptor activity, and methods for treating a condition or disorder mediated in part by CB1 receptor activity. In certain embodiments, the compounds are compounds of Formula I. Methods of preparing compounds of Formula I are also described. In another aspect, the invention provides methods of identifying a selective agonist of the beta-arrestin pathway over the G-protein pathway.
    Type: Grant
    Filed: December 19, 2016
    Date of Patent: November 6, 2018
    Assignee: The University of North Carolina at Greensboro
    Inventors: Patricia H. Reggio, Derek M. Shore, Dow P. Hurst
  • Patent number: 10112926
    Abstract: The present invention provides compounds of formula (I) which inhibit the activity of PI 3-kinase gamma isoform, which are useful for the treatment of diseases mediated by the activation of PI 3-kinase gamma isoform.
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: October 30, 2018
    Assignee: Novartis AG
    Inventors: Benjamin Richard Bellenie, Graham Charles Bloomfield, Ian Bruce, Andrew James Culshaw, Edward Charles Hall, Gregory John Hollingworth, James Neef, Matthew Spendiff, Simon James Watson
  • Patent number: 10100019
    Abstract: The present invention relates to a N2-(2-methoxyphenyl)pyrimidine derivative, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of cancer comprising the same as an active ingredient. The N2-(2-methoxyphenyl)pyrimidine derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention is very effective in suppressing anaplastic lymphoma kinase (ALK) activity and as a result it can improve the effectiveness of treatment on cancer cells having anaplastic lymphoma kinase (ALK) fusion proteins such as EML4-ALK and NPM-ALK, so that it can be effectively used as a pharmaceutical composition for preventing or treating cancer.
    Type: Grant
    Filed: April 6, 2016
    Date of Patent: October 16, 2018
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Pilho Kim, Hyoung Rae Kim, Sung Yun Cho, Jae Du Ha, Hee Jung Jung, Chang Soo Yun, Jong Yeon Hwang, Chi Hoon Park, Chong Ock Lee, Sunjoo Ahn, Chong Hak Chae
  • Patent number: 10080750
    Abstract: The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: September 25, 2018
    Assignee: Merck Patent GmbH
    Inventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Lizbeth C. Deselm, Hui Qiu, Yufang Xiao, Constantin Neagu, Igor Mochalkin, Theresa L. Johnson
  • Patent number: 10076529
    Abstract: Compositions, compounds, and methods with significant antiviral effect against RNA viruses and especially orthomyxoviruses are contemplated, and target the viral promoter that is formed by the 5? and 3?-UTR sequences of the viral genome.
    Type: Grant
    Filed: March 11, 2016
    Date of Patent: September 18, 2018
    Assignee: NANT HOLDINGS IP, LLC
    Inventors: Kayvan Niazi, Shahrooz Rabizadeh, Anne-Laure Le Ny, Oleksandr Buzko, Justin Golovato, Patrick Soon-Shiong
  • Patent number: 10065971
    Abstract: The present invention relates to compounds having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opiod receptor and more particularly to diazaspiro undecane compounds having this pharmacological activity, 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. wherein Y is n is 1 or 2; q is 1, 2, 3, 4, 5 or 6; X is a bond, —C(O)O—, —C(O)NR8—, —C(O)—, —O— or —C(R4R4?)—; R1 is C(O)R5 or S(O)2R5.
    Type: Grant
    Filed: June 2, 2015
    Date of Patent: September 4, 2018
    Assignee: ESTEVE PHARMACEUTICALS S.A.
    Inventors: Marina Virgili-Bernado, Monica Alonso-Xalma, Carlos Alegret-Molina, Carmen Almansa-Rosales, Ramón Merce-Vidal
  • Patent number: 10035819
    Abstract: Provided herein are deuterated compounds and compositions useful in increasing PPAR? activity. The compounds have a formula where L5 comprises at least one deuterium. Exemplary species include 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: April 7, 2017
    Date of Patent: July 31, 2018
    Assignee: The Salk Institute for Biological Studies
    Inventors: Ronald M. Evans, Michael Downes
  • Patent number: 10010547
    Abstract: This invention relates to compounds that inhibit or modulate the activity of Chk-1 kinase. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds.
    Type: Grant
    Filed: February 9, 2015
    Date of Patent: July 3, 2018
    Assignee: Cascadian Therapeutics, Inc.
    Inventors: Robert George Boyle, David Winter Walker, Richard Justin Boyce, Scott Peterson, Francine Farouz, Cong Hung Vo
  • Patent number: 9944597
    Abstract: The present invention provides polysubstituted pyrrole compounds, pharmaceutically effective salts, prodrugs, solvates and hydrates thereof, having antimitotic, antiproliferative and cytotoxic activity, activity against cells expressing the drug efflux protein, P-glycoprotein, or cells expressing the ?-III isotype of tubulin and antitumor activity. Also provided are methods of utilizing these compounds for inhibiting the proliferation of cancer cells as well as their medical use, in particular for treating cancer, including drug resistant cancer.
    Type: Grant
    Filed: September 16, 2014
    Date of Patent: April 17, 2018
    Assignees: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, VIRGINIA COMMONWEALTH UNIVERSITY, UNIVERSITY OF RICHMOND
    Inventors: Glen E. Kellogg, Chenxiao Da, Ashutosh Tripathi, John T. Gupton, Nakul Telang, James A. Sikorski, Susan L. Mooberry, Cristina Rohena
  • Patent number: 9938273
    Abstract: Disclosed are compounds of Formula I: or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Z2, Z3, and Z5 are as described herein, compositions thereof, and uses thereof.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: April 10, 2018
    Assignee: Plexxikon Inc.
    Inventors: Guoxian Wu, Jeffrey Wu, Katrina Chan, Ken Dong, Todd Ewing, Prabha N. Ibrahim, Jack Lin, Wayne Spevak, Ying Zhang
  • Patent number: 9932330
    Abstract: Anti-angiogenic treatments, treatments of hyperpermeability disorders, treatments of neuropathic and neurodegenerative disorders, pain treatments, methods of reducing the risk of pre-eclampsia and compounds for use in such methods are described.
    Type: Grant
    Filed: September 19, 2017
    Date of Patent: April 3, 2018
    Assignees: The University of Nottingham, NewSouth Innovations PTY Limited
    Inventors: David Bates, Jonathan Morris
  • Patent number: 9926319
    Abstract: The invention provides novel substituted pyridyl piperidine compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.
    Type: Grant
    Filed: March 10, 2015
    Date of Patent: March 27, 2018
    Assignees: MERCK PATENT GMBH, Cancer Research Technology Limited
    Inventors: Kai Schiemann, Frank Stieber, Michel Calderini, Julian Blagg, Aurelie Mallinger, Dennis Waalboer, Christian Rink, Simon Ross Crumpler
  • Patent number: 9889138
    Abstract: The present invention provides a method for treating or alleviating a symptom of a disorder, e.g., immune evasion, cancer-cell induced immune dysfunction, reduced immune response, lowered inflammation, decreased expression of a major histocompatibility complex (MHC), or cancer, characterized by aberrant, misregulated, or increased Enhancer of Zeste Homolog 2 (EZH2) activity in a cell or subject in need thereof by contacting the cell or administering to the subject a therapeutically effective amount of an EZH2 inhibitor.
    Type: Grant
    Filed: July 15, 2016
    Date of Patent: February 13, 2018
    Assignee: Epizyme, Inc.
    Inventor: Heike Keilhack
  • Patent number: 9850207
    Abstract: Provided are methods for treating, reducing, alleviating, and/or inhibiting neuropathic pain by orally, intravenously or intrathecally administering an effective amount of an inhibitor of soluble epoxide hydrolase (“sEH”), to a patient in need thereof. The neuropathic pain treated is selected from the group consisting of post-herpetic neuralgia, trigeminal neuralgia, focal peripheral nerve injury, and anesthesia dolorosa, central pain due to stroke or mass lesion, spinal cord injury, or multiple sclerosis, and peripheral neuropathy due to diabetes, HIV, or chemotherapy.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: December 26, 2017
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Kin Sing Lee, Bora Inceoglu, Karen Wagner
  • Patent number: 9796707
    Abstract: Anti-angiogenic treatments, treatments of hyperpermeability disorders, treatments of neuropathic and neurodegenerative disorders, pain treatments, methods of reducing the risk of pre-eclampsia and compounds for use in such methods are described.
    Type: Grant
    Filed: May 31, 2017
    Date of Patent: October 24, 2017
    Assignees: The University of Nottingham, NewSouth Innovations PTY Limited
    Inventors: David Bates, Jonathan Morris
  • Patent number: 9745268
    Abstract: Intermediates and methods are provided for the preparation of selected C5aR antagonist compounds.
    Type: Grant
    Filed: September 28, 2015
    Date of Patent: August 29, 2017
    Assignee: CHEMOCENTRYX, INC.
    Inventors: Pingchen Fan, Jaroslaw Kalisiak, Antoni Krasinski, Rebecca Lui, Jay Powers, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
  • Patent number: 9717737
    Abstract: Methods of treating autophagy related diseases, e.g. cancer and malaria, using novel autophagy inhibiting agents are described.
    Type: Grant
    Filed: February 25, 2015
    Date of Patent: August 1, 2017
    Assignee: THE UNIVERSITY OF HONG KONG
    Inventors: Jianbo Yue, Yingying Lu
  • Patent number: 9675584
    Abstract: Disclosed herein are substituted pyrazinyl acrylic acids of Formula (II): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.
    Type: Grant
    Filed: March 19, 2015
    Date of Patent: June 13, 2017
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • Patent number: 9610249
    Abstract: Methods for determining dosage of HER2-targeted anthracycline-containing immunoliposomes are disclosed, as are methods of treating cancer patients with HER2-positive tumors using dosages so determined. Upon administration, the dosages share the low cardiotoxicity profile of standard dosages of non-immunoliposomal (untargeted), anthracycline-containing liposomes.
    Type: Grant
    Filed: August 21, 2015
    Date of Patent: April 4, 2017
    Assignee: Merrimack Pharmaceuticals. Inc.
    Inventors: Joseph G. Reynolds, Kenneth J. Olivier, Jr., Bart S. Hendriks, Thomas Wickham, Stephan Klinz, Elena Geretti