Plural Hetero Atoms In The Bicyclo Ring System Patents (Class 514/300)
  • Patent number: 11439628
    Abstract: The present invention relates to non-steriodal mineralocorticoid receptor (MR) and the pharmacology of mineralocorticoid receptor antagonists (MR Antagonists, MRAs). In particular, the invention relates to the use of MRAs alone and in combination preferably in combination with sGC stimulators and/or sGC activators for preparation of medicaments for the prevention and/or treatment of muscular or neuromuscular diseases, especially for the treatment of Duchenne Muscular Dystrophy (DMD).
    Type: Grant
    Filed: May 10, 2019
    Date of Patent: September 13, 2022
    Assignee: BAYER AKTIENGESELLSCHAFT
    Inventors: Peter Sandner, Peter Kolkhof, Ilka Mathar, Stefanie Breitenstein
  • Patent number: 11426412
    Abstract: Heterocyclic compounds of Formula (I), (II), and (III) are described herein along with their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof. The compounds described herein, their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosis, cutaneous lupus erythematosis, ulcerative colitis, cancer, cystic fibrosis, asthma, multiple sclerosis and psoriasis.
    Type: Grant
    Filed: October 16, 2018
    Date of Patent: August 30, 2022
    Assignee: JUBILANT EPIPAD LLC
    Inventors: Gurulingappa Hallur, Athisayamani Jeyaraj Duraiswamy, Buchi Reddy Purra, N.V.S.K. Rao, Sridharan Rajagopal, Rajendra Kristam
  • Patent number: 11384085
    Abstract: Compounds useful in the modulation of ion channel activity in cells are disclosed herein. This disclosure also relates to use of these compounds in the treatment of pain, and pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Grant
    Filed: May 17, 2019
    Date of Patent: July 12, 2022
    Assignee: BIONOMICS LIMITED
    Inventors: Belinda Huff, Courtney Hollis, Hamish Toop, Nathan Kuchel, Lorna Helen Mitchell, Rajinder Singh
  • Patent number: 11377698
    Abstract: Provided herein, among other things, is a method of treating a cancer patient without the need for a tissue biopsy. In some embodiments, the method may comprise (a) performing or having performed a sequencing assay on cell-free DNA (cfDNA) from a sample of blood from the patient to determine if the cell-free DNA comprises actionable and/or non-actionable sequence variations in one or more target genes, and (b) treating the patient using the following method: i. administering a therapy that is targeted to an actionable sequence variation if the patient is identified as having the actionable sequence variation, and ii. administering a non-targeted therapy in the absence of any follow-up genetic testing on DNA extracted from a tissue biopsy if one or more non-actionable sequence variations and no actionable sequence variations are identified.
    Type: Grant
    Filed: September 4, 2019
    Date of Patent: July 5, 2022
    Assignee: INIVATA LTD.
    Inventors: Clive Morris, Vincent Plagnol, Tim Forshew
  • Patent number: 11376241
    Abstract: The present invention relates to compounds which can act as aryl hydrocarbon receptor (AhR) modulators and, in particular, as AhR antagonists. The invention further relates to the use of the compounds for the treatment and/or prophylaxis of diseases and/or conditions through binding of said aryl hydrocarbon receptor by said compounds.
    Type: Grant
    Filed: February 1, 2018
    Date of Patent: July 5, 2022
    Assignee: PHENEX PHARMACEUTICALS AG
    Inventors: Christoph Steeneck, Ulrich Deuschle, Michael Albers, Thomas Hoffmann
  • Patent number: 11370803
    Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
    Type: Grant
    Filed: September 17, 2020
    Date of Patent: June 28, 2022
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Nikolaos Papaioannou, Jeremy Mark Travins, Sarah Jocelyn Fink, John Mark Ellard, Alastair Rae
  • Patent number: 11352355
    Abstract: Disclosed are chemical entities which are inhibitors of spleen tyrosine kinase (SYK), namely, chemical entities comprising 6-((1R,2S)-2-aminocyclohexylamino)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,4-c]pyridine-3(2H)-one and certain solid state forms thereof. Also disclosed are methods of using the chemical entities to treat disorders such as a cancer.
    Type: Grant
    Filed: May 8, 2020
    Date of Patent: June 7, 2022
    Assignee: Calithera Biosciences, Inc.
    Inventors: Rongliang Chen, Tomonori Ichibakase, Chunrong Ma, Christopher F. Matthews, Hajime Motoyoshi, Colin O'Bryan, Kentaro Yaji, Naoki Yoshikawa
  • Patent number: 11351227
    Abstract: The present disclosure generally provides compositions and methods related to the field of immunology. Specifically, disclosed herein are chemokine binding proteins and methods of use thereof.
    Type: Grant
    Filed: April 27, 2018
    Date of Patent: June 7, 2022
    Assignee: Washington University
    Inventors: Daved Fremont, Olga Lubman, Andrew E. Gelman, Yun Hsuan Lu
  • Patent number: 11319318
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R9, X1 and X2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, e.g. cancer, pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Grant
    Filed: March 4, 2016
    Date of Patent: May 3, 2022
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Laetitia Martin, Steffen Steurer, Xiao-Ling Cockcroft
  • Patent number: 11306084
    Abstract: The present disclosure provides pharmaceutical agents, including those of the formula: (I) wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods of using the pharmaceutical agents are also provided. The compounds may be used for the inhibition or antagonism of integrins ???? and/or ?5??. In some embodiments, the compounds provided herein exhibit reduced inhibitory or antagonistic activity of integrins ???3, ???5, ???6, ???8, and/or ?IIb?3.
    Type: Grant
    Filed: December 28, 2017
    Date of Patent: April 19, 2022
    Assignees: Saint Louis University, Indalo Therapeutics, Inc.
    Inventors: Peter G. Ruminski, David W. Griggs, Scott Seiwert
  • Patent number: 11273147
    Abstract: This invention provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
    Type: Grant
    Filed: August 30, 2019
    Date of Patent: March 15, 2022
    Assignee: University of Tennessee Research Foundation
    Inventors: Ramesh Narayanan, Duane D. Miller, Thamarai Ponnusamy, Dong-Jin Hwang, Yali He, Jayaprakash Pagadala, Christopher C. Coss, James T. Dalton, Charles B. Duke
  • Patent number: 11273150
    Abstract: The invention provides compositions and methods for the treatment of presbyopia. The methods preferably comprise storing an aceclidine composition in a container having a headspace at a temperature from about 2 to about 8 degrees Celsius. The methods further comprise filling the container under an inert gas overlay and/or enclosing the container an anti-leaching material or disposing the container in a second container containing an anti-leaching material.
    Type: Grant
    Filed: October 13, 2020
    Date of Patent: March 15, 2022
    Assignee: LENZ THERAPEUTICS, INC.
    Inventor: Gerald Horn
  • Patent number: 11254667
    Abstract: Some embodiments of the invention include inventive compounds (e.g., compounds of Formula (I)). Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions (e.g., pharmaceutical compositions) for treating, for example, certain diseases using the inventive compounds. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating (e.g., diseases such as cancer or blood disorders). Further embodiments include methods for making the inventive compounds. Additional embodiments of the invention are also discussed herein.
    Type: Grant
    Filed: August 16, 2017
    Date of Patent: February 22, 2022
    Assignees: CHILDREN'S HOSPITAL MEDICAL CENTER, THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY, DEPT. OF HEALTH AND HUMAN SERVICES
    Inventors: Daniel T. Starczynowski, Craig J. Thomas, Garrett Rhyasen, Katelyn Melgar, Morgan MacKenzie Walker, Jian-kang Jiang
  • Patent number: 11242342
    Abstract: Isoquinoline amine compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
    Type: Grant
    Filed: November 8, 2017
    Date of Patent: February 8, 2022
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Andrew Felts
  • Patent number: 11180494
    Abstract: The invention relates to compounds of formula (I): or a salt thereof, wherein R1, G, L1, L2, L3, and Y are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are inhibitors of one, or both of, ?v?1 integrin and ?v?6 integrin that are useful for treating fibrosis such as in nonalcoholic steatohepatitis (NASH), idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
    Type: Grant
    Filed: October 8, 2019
    Date of Patent: November 23, 2021
    Assignee: Pliant Therapeutics, Inc.
    Inventors: Jacob Cha, Manuel Munoz, Maureen Reilly, Nicole Cooper, Katerina Leftheris, David J. Morgans, Jr., Timothy Hom, Yajun Zheng
  • Patent number: 11155546
    Abstract: The present disclosure relates to 4,6,7-trisubstituted 1,2-dihydropyrrolo[3,4-c]pyridin/pyrimidin-3-one derivatives, and their preparations and medicinal use. Specifically, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof, wherein the definition of each group is as described in the specification and claims.
    Type: Grant
    Filed: March 27, 2020
    Date of Patent: October 26, 2021
    Assignees: SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD., YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Shuchun Guo, Fusheng Zhou, Xiang Chen, Jinzhu Zhao, Dong Huang, Jing Xie, Changjiang Qiao, Wan He, Kai Zhang, Xi Chen, Jiong Lan
  • Patent number: 11130755
    Abstract: The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula (I), in which A, E, G, R1 to R6 and R10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: November 2, 2017
    Date of Patent: September 28, 2021
    Assignee: SANOFI
    Inventors: Dirk Gretzke, Olaf Ritzeler, Uwe Heinelt, Volkmar Wehner, Friedemann Schmidt
  • Patent number: 11110092
    Abstract: The present application relates to treatment of hematologic cancers, which treatments can include, e.g., administration of a purine nucleoside phosphorylase (PNP) inhibitor, an alkylating agent and/or an anti-CD20 agent, and related compositions and kits.
    Type: Grant
    Filed: May 1, 2019
    Date of Patent: September 7, 2021
    Assignee: BIOCRYST PHARMACEUTICALS, INC.
    Inventors: Shanta Bantia, Philip Breitfeld, Yarlagadda S Babu
  • Patent number: 11098043
    Abstract: This disclosure relates to compounds that are CBP inhibitor and methods of using such compounds in the treatment and diagnosis of diseases and disorders.
    Type: Grant
    Filed: July 13, 2018
    Date of Patent: August 24, 2021
    Assignee: University of Massachusetts
    Inventors: Wei Zhang, Alex Mugwiria Muthengi, Hailemichael O. Yosief
  • Patent number: 11083198
    Abstract: In crop production in the fields of agriculture, horticulture and the like, the damage caused by insect pests etc. is still immense, and insect pests resistant to existing insecticides have emerged. Under such circumstances, the development of novel agricultural and horticultural insecticides is desired. The present invention provides an agricultural and horticultural insecticide comprising a 4H-pyrrolopyridine compound represented by the general formula (1): {wherein R1 represents a halogen atom, R2 and R3 each represent a haloalkyl group, Q represents Q-A, Q-B or Q-C, X represents a nitrogen atom, R4 and R7 each represent a hydrogen atom, R2 and R3 each represent a halogen atom, a haloalkyl group or a substituted phenyl group, and m represents 2} or a salt thereof as an active ingredient; and a method for using the insecticide.
    Type: Grant
    Filed: December 26, 2017
    Date of Patent: August 10, 2021
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Ikki Yonemura, Yusuke Sano, Naoto Shimizu, Akihiro Miyasaka, Akiyuki Suwa, Shunpei Fujie, Ryosuke Tanaka
  • Patent number: 11072611
    Abstract: The present invention discloses compounds according to Formula I: Wherein R1a, R1b, R2, R4, R5, R6a, R6b, R8, W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.
    Type: Grant
    Filed: November 13, 2019
    Date of Patent: July 27, 2021
    Assignee: GALAPAGOS NV
    Inventors: Nicolas Desroy, Bertrand Heckmann, Reginald Christophe Xavier Brys, Agnès Marie Joncour, Christophe Peixoto, Xavier Marie Bock
  • Patent number: 11046669
    Abstract: Disclosed are small molecule inhibitors of ?v?6 integrin, and methods of using them to treat a number of diseases and conditions.
    Type: Grant
    Filed: June 26, 2019
    Date of Patent: June 29, 2021
    Assignee: Morphic Therapeutic, Inc.
    Inventors: Bryce A. Harrison, Matthew G. Bursavich, Mark Brewer, Aleksey I. Gerasyuto, Kristopher N. Hahn, Kyle D. Konze, Fu-Yang Lin, Blaise S. Lippa, Alexey A. Lugovskoy, Bruce N. Rogers, Mats A. Svensson, Dawn M. Troast
  • Patent number: 11040027
    Abstract: The invention relates to MKK4 (mitogen-activated protein kinase 4) and their use in promoting liver regeneration or reducing or preventing hepatocyte death. The MKK4 inhibitors selectively inhibit protein kinase MKK4 over protein kinases JNK and MKK7.
    Type: Grant
    Filed: January 17, 2018
    Date of Patent: June 22, 2021
    Assignee: Heparegenix GMBH
    Inventors: Wolfgang Albrecht, Stefan Laufer, Roland Selig, Phillip Klövekorn, Bent Präfke
  • Patent number: 11026954
    Abstract: The present invention provides the steroid compound 3beta-hydroxy-5alpha-pregnan-20-one for use in treatment of Tourette's syndrome, obsessive compulsive disorder and/or gambling disorder, as well as methods for treating said disorders and pharmaceutical compositions for use in treatment of said disorders.
    Type: Grant
    Filed: September 2, 2018
    Date of Patent: June 8, 2021
    Assignee: ASARINA PHARMA AB
    Inventor: Torbjörn Bäckström
  • Patent number: 10993935
    Abstract: Methods of treating a bacterial lung infection are provided and comprise administering an effective amount of rifaximin to a subject in need thereof. The rifaximin can be delivered by inhalation therapy, such as by delivering the rifaximin in aerosol form. The rifaximin is administered alone or in combination with tobramycin, including in multiple doses. Methods of reducing biofilm formation are also provided and comprise contacting a bacteria with an effective amount of rifaximin. Pharmaceutical composition are also included and comprise rifaximin and a pharmaceutically-acceptable vehicle suitable for administering the rifaximin in aerosol form.
    Type: Grant
    Filed: June 3, 2019
    Date of Patent: May 4, 2021
    Assignee: MARSHALL UNIVERSITY RESEARCH CORPORATION
    Inventors: Hongwei Yu, Thomas Ryan Withers, Brandon Kirby
  • Patent number: 10953005
    Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
    Type: Grant
    Filed: January 10, 2020
    Date of Patent: March 23, 2021
    Assignee: Array Biopharma Inc.
    Inventors: Steven W. Andrews, Sean Aronow, James F. Blake, Barbara J. Brandhuber, Adam Cook, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Elizabeth A. McFaddin, Megan L. McKenney, Oren T. McNulty, Andrew T. Metcalf, David A. Moreno, Tony P. Tang, Li Ren
  • Patent number: 10947254
    Abstract: Disclosed are methods for treating ulcerative colitis using a compound of the formula: or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: October 11, 2019
    Date of Patent: March 16, 2021
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Ryan Hudson, Jennifer Kozak, Dante D. Podesto, Xiaojun Huang, Venkat R. Thalladi
  • Patent number: 10947234
    Abstract: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.
    Type: Grant
    Filed: November 5, 2018
    Date of Patent: March 16, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michelle R. Machacek, David J. Witter, Michael Hale Reutershan, Michael D. Altman, Paul Anthony Stupple
  • Patent number: 10941142
    Abstract: Provided are compositions comprising Compound I having the following structure: or a pharmaceutically acceptable salt thereof, and a solubilizing agent; methods of making the same; and methods of using the same.
    Type: Grant
    Filed: July 12, 2019
    Date of Patent: March 9, 2021
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Hamid Rezaei, Gary Conard Visor, Tomoari Kamo, Hiroshi Yamakose
  • Patent number: 10933056
    Abstract: The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
    Type: Grant
    Filed: November 5, 2019
    Date of Patent: March 2, 2021
    Assignees: Merck Sharp & Dohme Corp., MSD R&D (China) Co. Ltd.
    Inventors: John J. Acton, III, Jianming Bao, Melissa Egbertson, Xiaolei Gao, Scott T. Harrison, Sandra L. Knowles, Chunsing Li, Michael Man-Chu Lo, Robert D. Mazzola, Jr., Zhaoyang Meng, Michael T. Rudd, Oleg B. Selyutin, David M. Tellers, Ling Tong, Jenny Miu-Chun Wai
  • Patent number: 10899761
    Abstract: Provided herein are heterocyclic compounds of Formula (I), pharmaceutical compositions containing such a compound and their therapeutic uses, methods for their preparation, intermediate compounds, pharmaceutical compositions containing such a compound, and their therapeutic uses.
    Type: Grant
    Filed: April 2, 2020
    Date of Patent: January 26, 2021
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Wayne Spevak, Jiazhong Zhang, Songyuan Shi, Ben Powell, Yan Ma
  • Patent number: 10888550
    Abstract: Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the modulation of MALT1. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, R5, R6, R7, G1 and G2, are defined herein.
    Type: Grant
    Filed: June 13, 2019
    Date of Patent: January 12, 2021
    Assignee: Janssen Pharmaceutica NV
    Inventors: Tianbao Lu, Peter J. Connolly, Maxwell David Cummings, Gaston Stanislas Marcella Diels, Jan Willem Thuring, Ulrike Philippar, James Patrick Edwards, Didier Jean-Claude Berthelot, Tongfei Wu
  • Patent number: 10864203
    Abstract: Disclosed herein is a pharmaceutical combination for use in the prevention, delay of progression or treatment of cancer, wherein the pharmaceutical combination exhibits a synergistic efficacy. The pharmaceutical combination comprises a humanized antagonist monoclonal antibody against PD- and a RAF inhibitor. Also disclosed herein is a combination for use in the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject a therapeutically effective amount of a humanized antagonist monoclonal antibody against PD-1 and a therapeutically effective amount of a RAF inhibitor.
    Type: Grant
    Filed: June 14, 2017
    Date of Patent: December 15, 2020
    Assignee: BEIGENE, LTD.
    Inventors: Jing Song, Lai Wang, Kang Li, Tong Zhang, Lusong Luo, Min Wei, Zhiyu Tang, Guoliang Zhang, Changyou Zhou
  • Patent number: 10829518
    Abstract: Provided herein are compositions including peptides, pharmaceutical preparations thereof, and methods of preventing photoreceptor death therewith and protecting of retinal cells, including, but not limited to, photoreceptors and retinal pigment epithelium, from Fas- or TRAIL-mediated apoptosis.
    Type: Grant
    Filed: November 4, 2019
    Date of Patent: November 10, 2020
    Assignees: ONL THERAPEUTICS. INC., THE REGENT OF THE UNIVERSITY OF MICHIGAN
    Inventors: Cagri G. Besirli, Alexander J. Bridges, John K. Freshley, William A. Hunke, Linda L. Johnson, Francis X. Smith, Ethan Sylvain, David N. Zacks
  • Patent number: 10807980
    Abstract: Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by ROR?. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.
    Type: Grant
    Filed: July 9, 2019
    Date of Patent: October 20, 2020
    Assignee: Vitae Pharmaceuticals, LLC
    Inventors: David A. Claremon, Lawrence Wayne Dillard, Chengguo Dong, Yi Fan, Lanqi Jia, Zhijie Liu, Stephen D. Lotesta, Andrew Marcus, Suresh B. Singh, Colin M. Tice, Jing Yuan, Wei Zhao, Yajun Zheng, Linghang Zhuang
  • Patent number: 10759800
    Abstract: The present invention relates to crystalline forms of a diazabicyclooctane derivative represented by Compound I, the process for producing the same and methods for using the same:
    Type: Grant
    Filed: September 25, 2018
    Date of Patent: September 1, 2020
    Assignees: FEDORA PHARMACEUTICALS INC., MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Michael Kammerer, Frederic Ran
  • Patent number: 10752626
    Abstract: Disclosed are compounds inhibiting the conversion of ?-KG to D-2-HG pharmaceutically acceptable salts, hydrates, solvates or stereoisomers thereof and pharmaceutical compositions comprising the compounds. The compound and the pharmaceutical composition can effectively treat IDH associated diseases, including cancer.
    Type: Grant
    Filed: July 11, 2017
    Date of Patent: August 25, 2020
    Assignee: SHANGHAI METON PHARMACEUTICAL CO., LTD
    Inventor: Jibin Yang
  • Patent number: 10744123
    Abstract: Methods and dosing regimens for treating glioblastoma or recurrent glioblastoma and its associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine) or a pharmaceutically acceptable salt thereof and at least one or more other therapeutic agent.
    Type: Grant
    Filed: February 11, 2019
    Date of Patent: August 18, 2020
    Assignee: MediciNova, Inc.
    Inventors: Kazuko Matsuda, Kerrie McDonald
  • Patent number: 10731199
    Abstract: Aspects of embodiments may include methods for automated enzymatic detection of glucose-6-phosphate dehydrogenase (G6PD) activity. Aspects of embodiments may include methods for enzymatic detection of G6PD activity in droplets in oil. Aspects of embodiments may include a system including a droplet actuator. Aspects of embodiments may include a treatment method.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: August 4, 2020
    Assignee: ADVANCED LIQUID LOGIC, INC.
    Inventors: Carrie A. Graham, Allen E. Eckhardt
  • Patent number: 10723719
    Abstract: The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    Type: Grant
    Filed: May 1, 2019
    Date of Patent: July 28, 2020
    Assignee: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim
  • Patent number: 10703741
    Abstract: The present invention provides compounds of formula I useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
    Type: Grant
    Filed: July 27, 2017
    Date of Patent: July 7, 2020
    Assignee: Padlock Therapeutics, Inc.
    Inventors: Edward Jean Beaumont, Rajesh Devraj, Philip Stephen Kerry, Gnanasambandam Kumaravel, Pui Leng Loke, Mirco Meniconi, Jordan John Palfrey, Carl North, Cristina Lecci, Heather Tye
  • Patent number: 10696671
    Abstract: The present disclosure relates to novel imidazo[1,2-a]pyridine derivatives, and more particularly to imidazo[1,2-a]pyridine derivatives of Formula 1 wherein Y1, Y2 and Y3 are each independently H, halogen, a C1-C6 straight chain alkyl unsubstituted or substituted with R1, or hydroxy; R1 is hydroxy; Y4 is H, C1-C6 straight chain alkyl, or C1-C6 alkoxy; and X is H or halogen, and having an excellent activity of inhibiting gastric acid secretion, methods for preparing the same, and the use thereof. The imidazo[1,2-a]pyridine derivatives according to the present disclosure have gastric acid secretion inhibitory activity, and thus may be effectively used for the prevention or treatment of gastrointestinal inflammatory diseases or gastric acid-related diseases.
    Type: Grant
    Filed: July 4, 2017
    Date of Patent: June 30, 2020
    Assignee: Jeil Pharmaceutical Co., Ltd.
    Inventors: Jeongmin Kim, Hyunho Lee, Kwangwoo Chun, Chun-Ho Park, Eunsung Jang, Yoonsun Park, Joseph Kim
  • Patent number: 10669238
    Abstract: The present invention provides an inhibitor of Bruton's tyrosine kinase, which is a compound of formula (I), or its pharmaceutically acceptable salt, solvate, ester, acid, metabolite or prodrug. The present invention also provides a pharmaceutical composition comprising the compound. The present invention also provides a method for inhibiting the activity of tyrosine kinase activity or for treating a disease, disorder, or condition, which would benefit from the inhibition of Bruton's tyrosine kinase(s), by using the Bruton's tyrosine kinase inhibitor, as well application of the Bruton's tyrosine kinase inhibitor for the same.
    Type: Grant
    Filed: December 22, 2016
    Date of Patent: June 2, 2020
    Assignee: HEFEI INSTITUTES OF PHYSICAL SCIENCE, CHINESE ACADEMY OF SCIENCES
    Inventors: Jing Liu, Qingsong Liu, Qianmao Liang, Yongfei Chen, Cheng Chen, Aoli Wang, Hong Wu, Kailin Yu, Wei Wang, Chen Hu, Wenchao Wang, Shuang Qi, Beilei Wang, Li Wang
  • Patent number: 10646478
    Abstract: Embodiments of the present invention are directed to methods for treatment of melanoma using an inhibitor of dihydroorotate dehydrogenase (DHODH) and to combination therapies that involve administering to a subject an inhibitor of oncogenic BRAF (e.g. BRAF(V600E)), as well as an inhibitor of dihydroorotate dehydrogenase (DHODH). Assays for identifying compounds useful for the treatment of melanoma are also provided. The methods comprise screening for compounds or agents that inhibit neural crest progenitor formation in a zebra fish model of melanoma.
    Type: Grant
    Filed: July 6, 2018
    Date of Patent: May 12, 2020
    Assignees: CHILDREN'S MEDICAL CENTER CORPORATION, DANA-FARBER CANCER INSTITUTE
    Inventors: Leonard Zon, Richard M. White
  • Patent number: 10633379
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R6, X1, and X2 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising compounds of formula (I).
    Type: Grant
    Filed: April 14, 2017
    Date of Patent: April 28, 2020
    Assignee: AbbVie Inc.
    Inventors: Lisa A. Hasvold, Dachun Liu, Keith F. McDaniel, John Pratt, George Sheppard, Le Wang
  • Patent number: 10611762
    Abstract: The present disclosure relates to solid forms of N-{[2?-(2,6-difluoro-3,5-dimethoxyphenyl)-3?-oxo-2?,3?-dihydro-1?H-spiro[cyclopropane-1,4?-[2,7]naphthyridin]-6?-yl]methyl}acrylamide, methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of the FGFR-associated or mediated diseases such as cancer.
    Type: Grant
    Filed: May 25, 2018
    Date of Patent: April 7, 2020
    Assignee: Incyte Corporation
    Inventors: Zhongjiang Jia, Qun Li
  • Patent number: 10577366
    Abstract: Forms of 4-(1-(1,1-di(pyridin-2-yl)ethyl)-6-(3,5-dimethylisoxazol-4-yl)-1H-pyrrolo[3,2-b]pyridin-3-yl)benzoic acid were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the forms of Compound I.
    Type: Grant
    Filed: March 19, 2018
    Date of Patent: March 3, 2020
    Assignee: Plexxikon Inc.
    Inventors: Jack Lin, Marika Nespi, Jason Walters
  • Patent number: 10570133
    Abstract: A compound of Formula III as the raw material is hydrolyzed in an alkaline condition, then acidized to prepare a compound of Formula IV, and the resulting compound of formula IV and a solid phosgene or diphosgene are concurrently subjected to the urea cyclization and the chloroformylation reaction in the presence of an organic base and a catalyst to obtain a compound of formula V, and then the compound of formula V is amidated to obtain the final product (II). In the present invention, a “one-pot” method is adopted for urea cyclization, chloroformylation, and amidation reaction, and the intermediate products do not need post-treatments such as separation and purification.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: February 25, 2020
    Assignee: XINFA PHARMACEUTICAL CO., LTD
    Inventors: Yuxin Qi, Xinfa Li, Baolin Wang, Xin Xu, Yinlong Zhao, Yuqi Teng
  • Patent number: 10555944
    Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
    Type: Grant
    Filed: October 29, 2018
    Date of Patent: February 11, 2020
    Assignee: Eli Lilly and Company
    Inventors: Steven W. Andrews, Sean Aronow, James F. Blake, Barbara J. Brandhuber, Adam Cook, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Elizabeth A. McFaddin, Megan L. McKenney, Oren T. McNulty, Andrew T. Metcalf, David A. Moreno, Tony P. Tang, Li Ren
  • Patent number: 10544161
    Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
    Type: Grant
    Filed: January 16, 2019
    Date of Patent: January 28, 2020
    Assignee: INTERMUNE, INC.
    Inventors: Johnnie Y. Ramphal, Brad Owen Buckman, Kumaraswamy Emayan, John Beamond Nicholas, Scott D. Seiwert