Plural Hetero Atoms In The Bicyclo Ring System Patents (Class 514/300)
  • 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: 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: 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: 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
  • Patent number: 10538486
    Abstract: The present invention relates to a hydroxamic acid-based contrast agent containing an isotope of fluorine, which comprises a compound having a structure of Formula (III): wherein R1 represents radioactive fluorine-18 (18F) or isotope fluorine-19 (19F), and R2 represents hydroxyamine —(NH)OH. The hydroxamic acid-based contrast agent containing an isotope of fluorine provided in the present invention has the capability of selectively inhibiting histone deacetylase (HDAC) subtypes 8/6/3, and specifically targets to the focus of spinocerebellar ataxia with over-activation of HDAC. By labeling with the radioisotope fluorine-18, a positron emission tomography (PET) image is obtained with the hydroxamic acid-based contrast agent containing radioisotope fluorine-18, whereby spinocerebellar ataxia is effectively detected.
    Type: Grant
    Filed: October 27, 2017
    Date of Patent: January 21, 2020
    Assignee: INSTITUTE OF NUCLEAR ENERGY RESEARCH, ATOMIC ENERGY COUNCIL, EXECUTIVE YUAN. R.O.C
    Inventors: Mei-Hui Wang, Chia-Yu Hu, Mao-Chi Weng, Jyun-Hong Chen, Chun-Hung Yang, Hung-Man Yu
  • Patent number: 10532981
    Abstract: The compounds are crystalline modifications of methyl (3Z)-3-{[4-{methyl[(4-methylpiperazin-1-yl)acetyl]amino}phenyl)amino](phenyl)methylidene}-2-oxo-2,3-dihydro-1H-indole-6-carboxylate salts of Formula I, wherein H—X represents at least one acid component, processes for the preparation thereof, and pharmaceutical compositions.
    Type: Grant
    Filed: February 20, 2017
    Date of Patent: January 14, 2020
    Assignee: Zentiva k.s.
    Inventors: Eszter Tieger, Marcela Tkadlecova, Ondrej Dammer, Tomas Gurgut
  • Patent number: 10526347
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: October 16, 2018
    Date of Patent: January 7, 2020
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10513517
    Abstract: A compound of formula (I) or a salt thereof: wherein R1 represents a five-membered aromatic heterocycle selected from a N- or a C-linked mono- or di-substituted pyrazole, an N- or a C-linked optionally mono- or di-substituted triazole or an N- or a C-linked optionally mono- or di-substituted imidazole, which five-membered aromatic heterocycle may be substituted by one or two of the groups selected from a hydrogen atom, a methyl group, an ethyl group, a fluorine atom, a hydroxymethyl group, a 2-hydroxypropan-2-yl group, a trifluoromethyl group, a difluoromethyl group or a fluoromethyl group, except that when R1 represents an N-linked mono- or di-substituted pyrazole, R1 does not represent 3,5-Dimethyl-1H-pyrazol-1-yl, 5-Methyl-1H-pyrazol-1-yl, 5-Ethyl-3-methyl-1H-pyrazol-1-yl, 3,5-Diethyl-1H-pyrazol-1-yl, 4-Fluoro-3,5-dimethyl-1H-pyrazol-1-yl, 3-Methyl-1H-pyrazol-1-yl or 1H-pyrazol-1-yl.
    Type: Grant
    Filed: October 19, 2018
    Date of Patent: December 24, 2019
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Niall Andrew Anderson, Ian Baxter Campbell, Matthew Howard James Campbell-Crawford, Ashley Paul Hancock, Seble Lemma, Simon John Fawcett MacDonald, John Martin Pritchard, Panayiotis Alexandrou Procopiou
  • Patent number: 10512645
    Abstract: Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
    Type: Grant
    Filed: April 4, 2018
    Date of Patent: December 24, 2019
    Assignee: Hutchinson Medipharma Limited
    Inventors: Wei-Guo Su, Hong Jia, Guangxiu Dai
  • Patent number: 10494368
    Abstract: Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: October 9, 2018
    Date of Patent: December 3, 2019
    Assignee: Syngenta Participations AG
    Inventors: Pierre Joseph Marcel Jung, Andrew Edmunds, Michel Muehlebach, Roger Graham Hall, Jerome Yves Cassayre
  • Patent number: 10487080
    Abstract: The invention relates to compounds of Formula (I): wherein R1, R2 and R3 are as defined in the description and claims, or pharmaceutically acceptable salts thereof, having ?v?6 integrin antagonist activity. The invention also relates to pharmaceutical compositions including a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and to the use of a compound of Formula (I), or a pharmaceutically acceptable salt thereof in therapy, including in the treatment of a disease or condition for which an ?v?6 integrin antagonist is indicated, in particular the treatment of idiopathic pulmonary fibrosis.
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: November 26, 2019
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Niall Andrew Anderson, Matthew Howard James Campbell-Crawford, Ashley Paul Hancock, Seble Lemma, John Martin Pritchard, Panayiotis Alexandrou Procopiou, Steven Leslie Sollis
  • Patent number: 10457678
    Abstract: The present invention relates to new N1- and N7-substituted sibiriline derivatives of the following general formula (I): (I) or a pharmaceutically acceptable salt and/or solvate thereof, notably for use as drug, in particular for use as inhibitor of cellular necroptosis. The present invention also relates to a pharmaceutical composition comprising such a compound and processes to prepare such a compound. The present invention also encompasses the use of a compound of the general formula (I) for organs preservation.
    Type: Grant
    Filed: October 13, 2016
    Date of Patent: October 29, 2019
    Assignees: Institut National de la Sante et de la Recherche Medicale (INSERM), Centre National de la Recherche Scientifique (CNRS), Sorbonne Universite, Universite Claude Bernard Lyon 1
    Inventors: Marie-Thérèse Dimanche-Boitrel, Stéphane Bach, Claire Delehouze, Peter Goekjian, Arnaud Comte
  • Patent number: 10450301
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts and esters thereof: which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcohol steatohepatitis disease (NASH).
    Type: Grant
    Filed: May 24, 2018
    Date of Patent: October 22, 2019
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Brett Granger, Guoqiang Wang, Ruichao Shen, Jing He, Yong He, Xuechao Xing, Jun Ma, Jiang Long, Bin Wang, Yat Sun Or
  • Patent number: 10435404
    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 24, 2018
    Date of Patent: October 8, 2019
    Assignees: Plexxikon Inc., Daiichi Sankyo Company, Limited
    Inventors: Prabha N. Ibrahim, Hamid Rezaei, Gary Conard Visor, Tomoari Kamo, Hiroshi Yamakose
  • Patent number: 10428068
    Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.
    Type: Grant
    Filed: July 11, 2018
    Date of Patent: October 1, 2019
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
  • Patent number: 10407422
    Abstract: The present invention provides compounds of Formula (I): wherein A is as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.
    Type: Grant
    Filed: August 30, 2016
    Date of Patent: September 10, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joanne M. Smallheer, Scott A. Shaw, Oz Scott Halpern, Carol Hui Hu, Ellen K. Kick
  • Patent number: 10399976
    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 2, 2018
    Date of Patent: September 3, 2019
    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: 10370374
    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: May 11, 2018
    Date of Patent: August 6, 2019
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Wayne Spevak, Jiazhong Zhang, Songyuan Shi, Ben Powell, Yan Ma
  • Patent number: 10364232
    Abstract: The present invention relates to the following compounds wherein the integers are as defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of tuberculosis.
    Type: Grant
    Filed: July 1, 2016
    Date of Patent: July 30, 2019
    Assignee: Janssen Sciences Ireland UC
    Inventors: Jérõme Émile Georges Guillemont, Magali Madeleine Simone Motte, Pierre Jean-Marie Bernard Rabiosson, Abdellah Tahri
  • Patent number: 10358445
    Abstract: The present invention relates to respiratory formulations comprising a compound of formula (I): and use of said compounds and compositions in treatment, for example in the treatment of an inflammatory disease or a respiratory disorder, in particular an inflammatory mediated and/or virally mediated respiratory disorder such as asthma and COPD or the treatment or prevention of viral infection, for example infection by influenza virus, rhinovirus or RSV. The invention also extends to certain novel compounds of formula (I).
    Type: Grant
    Filed: December 5, 2014
    Date of Patent: July 23, 2019
    Assignee: RESPIVERT, LTD.
    Inventors: Peter John Murray, Stuart Thomas Onions, Jonathan Gareth Williams, Kevin Joly
  • Patent number: RE47785
    Abstract: Disclosed is a technique for improving the water solubility and storage stability of 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound (1)) that is safe and not only has a strong antibacterial action but also is effective for resistant bacteria for which conventional antibacterial agent are less effective. Crystals of the hydrochloride salt of the compound (1), crystals of the hydrochloride salt hydrate of the compound (1), and crystals of the methanesulfonate salt of the compound (1) are provided. In these crystals, decomposition due to influences of light is suppressed as compared to that in crystals of the compound (1) in free, and their storage stability is high. These crystals have higher solubility in water than the crystals of the compound (1) in free.
    Type: Grant
    Filed: May 2, 2018
    Date of Patent: December 31, 2019
    Assignee: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Ichiro Araya, Akinori Goto, Wataru Minagawa, Keiko Funada, Muneki Nagao