Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbon Of The 1,4-diazine Ring Patents (Class 514/255.06)
  • Patent number: 11318135
    Abstract: The present application relates to a Favipiravir compound represented by Formula I, a geometric isomer, a pharmaceutically acceptable salt, a solvate and/or a hydrate thereof, and a pharmaceutical composition comprising the compound for treating a coronavirus infection.
    Type: Grant
    Filed: July 16, 2021
    Date of Patent: May 3, 2022
    Assignee: Academy of Military Medical Sciences
    Inventors: Wu Zhong, Ruiyuan Cao, Cheng Cao, Ting Gao, Gengfu Xiao, Zhihong Hu, Manli Wang, Leike Zhang, Song Li
  • Patent number: 11293067
    Abstract: The present application provides a method for genotyping M. tuberculosis, comprising obtaining amplifying and obtaining a first DNA fragment from a DNA sample by using one or more primer sets selected from the group consisting of primer sets 1 to 25 (SEQ ID Nos. 1 to 50); amplifying and obtaining a second DNA fragment from the obtained first DNA fragment by using one or more extension primers selected from the group consisting of SEQ ID Nos. 51 to 75; and detecting the second DNA fragment by using mass spectrometry, particularly by matrix-assisted laser desorption ionization time-of-flight mass spectrometry (MALDI-TOF MS).
    Type: Grant
    Filed: March 14, 2018
    Date of Patent: April 5, 2022
    Assignee: National Health Research Institutes
    Inventors: Shih-Feng Tsai, Chien-Hsing Lin, Horng-Yunn Dou
  • Patent number: 11285156
    Abstract: Provided herein are KRAS G12C inhibitors, such as composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
    Type: Grant
    Filed: June 11, 2019
    Date of Patent: March 29, 2022
    Assignee: AMGEN INC.
    Inventors: John Gordon Allen, Brian Alan Lanman, Jian Chen, Anthony B. Reed, Victor J. Cee, Longbin Liu, Patricia Lopez, Ryan Paul Wurz, Thomas T. Nguyen, Shon Booker, Jennifer Rebecca Allen, Margaret Chu-Moyer, Albert Amegadzie, Ning Chen, Clifford Goodman, Jonathan D. Low, Vu Van Ma, Ana Elena Minatti, Nobuko Nishimura, Alexander J. Pickrell, Hui-Ling Wang, Youngsook Shin, Aaron C. Siegmund, Kevin C. Yang, Nuria A. Tamayo, Mary Walton, Qiufen Xue
  • Patent number: 11260054
    Abstract: Provided herein are methods of treating cancer, including colorectal cancer, pancreatic cancer, and cancer associated with a hypoxic tumor. Also provided are methods of treating cancer, including colorectal cancer, pancreatic cancer, and cancer associated with a hypoxic tumor with a combination of treatments.
    Type: Grant
    Filed: November 25, 2020
    Date of Patent: March 1, 2022
    Assignee: Pano Therapeutics, Inc.
    Inventor: Francesca Fieni
  • Patent number: 11123326
    Abstract: The present invention provides 5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine˜2˜carbonitrile and pharmaceutically acceptable salts and solvates thereof that is capable of inhibiting CHK1 and is useful in the treatment of neuroblastomas and/or soft tissue sarcomas.
    Type: Grant
    Filed: July 15, 2016
    Date of Patent: September 21, 2021
    Assignee: Eli Lilly and Company
    Inventor: Louis Frank Stancato
  • Patent number: 11034660
    Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Grant
    Filed: November 26, 2019
    Date of Patent: June 15, 2021
    Assignee: Karyopharm Therapeutics Inc.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
  • Patent number: 10993943
    Abstract: The present disclosure relates to solid state forms of Selinexor, processes for preparation thereof and pharmaceutical compositions thereof.
    Type: Grant
    Filed: January 5, 2018
    Date of Patent: May 4, 2021
    Assignee: WATSON LABORATORIES INC.
    Inventors: Anantha Rajmohan Muthusamy, Sundara Lakshmi Kanniah, Akash Ravi, Tonmoy Chitta Das, Rajendra Popat Chemate, Anil Kumar Singh, Yogesh Dhananjay Wagh
  • Patent number: 10980239
    Abstract: The invention concerns a three component system comprising surface-active substances, vitamins and metal ions for efficient destruction and removal of contaminating proteins, nucleic acids and microorganisms from surfaces like for example laboratory benches, floors, equipment and instruments. These non-corrosive and non-toxic solutions for removal of proteins, nucleic acids and microorganisms are applied by spraying, rubbing or immersion of contaminated surfaces thereby destroying, solubilizing inactivating and removing proteins and nucleic acids. In that way also microorganisms are killed with high efficiency and at the same time all genetic information is inactivated.
    Type: Grant
    Filed: October 2, 2017
    Date of Patent: April 20, 2021
    Inventors: Thomas Lisowsky, Karlheinz Esser, Richard Lisowsky
  • Patent number: 10961232
    Abstract: The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: May 30, 2017
    Date of Patent: March 30, 2021
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
  • Patent number: 10779536
    Abstract: The present invention relates to pesticidal mixtures comprising one fungicidal compound I selected from the group consisting of 1-[3-chloro-2-[[1-(4-chlorophenyl)pyrazol-3-yl]oxymethyl]phenyl]-4-methyl-tetrazol-5-one (I-1), 1-[3-bromo-2-[[1-(4-chlorophenyl)pyrazol-3-yl]oxymethyl]phenyl]-4-methyl-tetrazol-5-one (I-2), 1-[2-[[1-(4-chlorophenyl)pyrazol-3-yl]oxymethyl]-3-methyl-phenyl]-4-methyl-tetrazol-5-one (I-3), 1-[2-[[1-(4-chlorophenyl)pyrazol-3-yl]oxymethyl]-3-fluoro-phenyl]-4-methyl-tetrazol-5-one (I-4), 1-[2-[[1-(2,4-dichlorophenyl)pyrazol-3-yl]oxymethyl]-3-fluoro-phenyl]-4-methyl-tetrazol-5-one (I-5), 1-[2-[[4-(4-chlorophenyl)thiazol-2-yl]oxymethyl]-3-methyl-phenyl]-4-methyl-tetrazol-5-one (I-6), 1-[3-chloro-2-[[4-(p-tolyl)thiazol-2-yl]oxymethyl]phenyl]-4-methyl-tetrazol-5-one (I-7), 1-[3-cyclopropyl-2-[[2-methyl-4-(1-methylpyrazol-3-yl)phenoxy]methyl]phenyl]-4-methyl-tetrazol-5-one (I-8), 1-[3-(difluoromethoxy)-2-[[2-methyl-4-(1-methylpyrazol-3-yl)phenoxy]methyl]phenyl]-4-methyl-tetrazol-5-one (I-9), 1-
    Type: Grant
    Filed: October 28, 2015
    Date of Patent: September 22, 2020
    Assignee: BASF SE
    Inventors: Jurith Montag, Markus Gewehr
  • Patent number: 10676474
    Abstract: Disclosed is a series of compounds acting as CDK4/6 inhibitors. Specifically disclosed are compounds as represented by formula (I), pharmaceutically acceptable salts or isomers thereof, pharmaceutical compositions containing same, and the use thereof in the preparation of drugs for treating cancers.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: June 9, 2020
    Assignees: CSTONE PHARMACEUTICALS, MEDSHINE DISCOVERY INC.
    Inventors: Zhaobing Xu, Lihong Hu, Charles Z. Ding, Shuhui Chen
  • Patent number: 10633389
    Abstract: Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein X, R1, R1a, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of Formula: wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.
    Type: Grant
    Filed: October 2, 2018
    Date of Patent: April 28, 2020
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
  • Patent number: 10576069
    Abstract: The present invention provides methods and compositions for treating chemotherapy-induced cognitive impairment. One embodiment of the present invention is directed to a method of treating chemotherapy-induced cognitive impairment by administering to a patient in need at least one thiosemicarbazone compound.
    Type: Grant
    Filed: February 1, 2016
    Date of Patent: March 3, 2020
    Inventors: Hossein A. Ghanbari, Zhi-Gang Jiang
  • Patent number: 10537102
    Abstract: A composition for controlling a plant disease is provided, containing a tetrazolinone compound represented by formula (1), wherein X1 represents a halogen atom, a C1-C6 alkyl group, or a C1-C6 alkoxy group, and X2 represents a C1-C3 alkyl group, a C3-C4 cycloalkyl group, a halogen atom, or a C1-C3 alkoxy group, and a carboxamide compound represented by formula (2). A method for controlling a plant disease is also provided, containing a step of applying an effective amount of the tetrazolinone compound represented by formula (1) and an effective amount of the carboxamide compound represented by formula (2) to a plant or soil for cultivating the plant. Both the composition and the method have excellent control efficacies against plant diseases.
    Type: Grant
    Filed: March 10, 2017
    Date of Patent: January 21, 2020
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: So Kiguchi
  • Patent number: 10526292
    Abstract: Sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: January 7, 2020
    Assignee: Parion Sciences, Inc.
    Inventors: Michael Ross Johnson, William Robert Thelin, Richard C. Boucher
  • Patent number: 10525044
    Abstract: The present invention provides methods and compositions for treating chemotherapy induced peripheral neuropathy. One embodiment of the present invention is directed to a method of treating chemotherapy induced peripheral neuropathy by administering to a patient in need at least one thiosemicarbazone compound.
    Type: Grant
    Filed: December 1, 2017
    Date of Patent: January 7, 2020
    Inventors: Hossein Ghanbari, Zhi-Gang Jiang
  • Patent number: 10479784
    Abstract: The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: April 30, 2018
    Date of Patent: November 19, 2019
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jean-Damien Charrier, Steven John Durrant, David Kay, Ronald Marcellus Alphonsus Knegtel, Somhairle MacCormick, Michael Paul Mortimore, Michael Edward O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Clinton Young, Philip Michael Reaper
  • Patent number: 10188648
    Abstract: The present disclosure relates to solid state forms of Selexipag, in particular selexipag forms IV and V, and processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: September 2, 2016
    Date of Patent: January 29, 2019
    Assignee: TEVA PHARMACEUTICALS INTERNATIONAL GMBH
    Inventors: Nidia Villalva, Ivon Cante, Martin Aybar, Angel Rodriguez, Alejandro Guillen Torres, Hana Kantor, Ales Gavenda, Hugo Herrera, Alexander Jegorov, Nydia Lopez
  • Patent number: 10167266
    Abstract: The present invention relates to compounds of Formula (I) and pharmaceutical compositions thereof. Compounds of Formula (I) are epithelial sodium channel (ENaC) blockers useful in the hydration of mucosal surfaces, enhancement of mucociliary clearance, or restoration of mucosal defense in a subject. The compounds and compositions can therefore be used to treat diseases which rely on the hydration of mucosal surfaces.
    Type: Grant
    Filed: October 27, 2016
    Date of Patent: January 1, 2019
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Patent number: 9890110
    Abstract: An amide derivative represented by Formula (3), which exhibits excellent efficacy in pest control effect, is produced by allowing a compound represented by the following Formula (1) and a compound represented by Formula (2) to react with each other. In Formula (1) to Formula (3), Y1 and Y2 each represent a halogen atom or a haloalkyl group; Rf represents a C3-C4 perfluoroalkyl group; and R1 and R2 each represent a hydrogen atom or an alkyl group; LG represents a leaving group; T represents a hydrogen atom or a fluorine atom; X1, X3, X4, and X5 each represent a hydrogen atom, a halogen atom, or the like; and A represents a nitrogen atom, a methine group, or the like.
    Type: Grant
    Filed: June 17, 2016
    Date of Patent: February 13, 2018
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Youji Aoki, Yumi Kobayashi, Hidenori Daido, Hiroyuki Katsuta, Hidetaka Tsukada, Atsushi Hirabayashi, Yusuke Takahashi, Michikazu Nomura, Atsuko Kawahara
  • Patent number: 9878988
    Abstract: Sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.
    Type: Grant
    Filed: January 5, 2016
    Date of Patent: January 30, 2018
    Assignee: PARION SCIENCES, INC.
    Inventors: Michael Ross Johnson, William Robert Thelin, Richard C. Boucher
  • Patent number: 9861593
    Abstract: Method for the treatment or prophylaxis of dry eye disorders by the administration of alkylamino-polyhydroxyalkanes and compositions thereof.
    Type: Grant
    Filed: November 7, 2016
    Date of Patent: January 9, 2018
    Assignee: Dynamis Pharmaceuticals, Inc.
    Inventors: Alice Marcy, Annette Tobia
  • Patent number: 9849129
    Abstract: Provided are methods of treating a variety of disorders of the skin with inhibitors of the epithelial sodium channel (ENaC). The inhibitors are represented by formula (I)-(IV): where R is defined herein.
    Type: Grant
    Filed: February 18, 2016
    Date of Patent: December 26, 2017
    Assignee: PARION SCIENCES, INC.
    Inventors: Michael Ross Johnson, William Robert Thelin, Richard C. Boucher
  • Patent number: 9738651
    Abstract: Provided herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R1a, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of Formula (II) wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: August 22, 2017
    Assignee: EPIZYME, INC.
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
  • Patent number: 9714226
    Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: July 25, 2017
    Assignee: Karyopharm Therapeutics Inc.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
  • Patent number: 9688639
    Abstract: Disclosed are solid forms of 4-(2-bromo-4-fluorophenyl)-N-(2-chloro-6-fluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed. Disclosed are compositions for protecting a plant or plant seed from diseases caused by fungal pathogens comprising a biologically effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other nematocide, insecticide and/or fungicide are also disclosed. Also disclosed are methods for protecting a plant or plant seed from diseases caused by fungal pathogens comprising applying to a plant or seed, or to the environment of the plant or seed, a biologically effective amount of a solid form of Compound 1.
    Type: Grant
    Filed: May 15, 2014
    Date of Patent: June 27, 2017
    Assignee: E I DU PONT DE NEMOURS AND COMPANY
    Inventor: Matthew Richard Oberholzer
  • Patent number: 9586911
    Abstract: The present invention relates to the compound of the formula: or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: March 7, 2017
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Patent number: 9550777
    Abstract: The present invention provides for compounds of Formula (I) and various embodiments thereof, and compositions comprising compounds of Formula (I) and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6 and R7 have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula (I) as DLK inhibitors and for treating neurodegeneration diseases and disorders.
    Type: Grant
    Filed: July 16, 2015
    Date of Patent: January 24, 2017
    Assignee: Genentech, Inc.
    Inventors: Anthony Estrada, Wen Liu, Snahel Patel, Michael Siu
  • Patent number: 9491941
    Abstract: The present invention relates to new compounds of formula (I) wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: November 15, 2016
    Assignee: NOVARTIS TIERGESUNDHEIT AG
    Inventors: Emilie Dupont, Noelle Gauvry, Steve Nanchen, Chikako Ogawa, Chouaib Tahtaoui
  • Patent number: 9493427
    Abstract: The invention relates to compounds of structural formula (I) and structural formula (VI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R, R1, R2, Z, L, and n are defined herein. Those compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: November 15, 2016
    Assignee: SYNTA PHARMACEUTICALS CORP.
    Inventors: Lijun Sun, Shoujun Chen, Jun Jiang, Yu Xie, Chih-Yi Yu
  • Patent number: 9458106
    Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, A and W are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: February 20, 2015
    Date of Patent: October 4, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hui Hu, Min Jiang, Taiguang Jin, Rui Niu, Jianhua Wang, Min Wang, Song Yang, Taichang Yuan, Chengang Zhou, Zheng Zhou
  • Patent number: 9394240
    Abstract: An amide derivative represented by Formula (3), which exhibits excellent efficacy in pest control effect, is produced by allowing a compound represented by the following Formula (1) and a compound represented by Formula (2) to react with each other. In Formula (1) to Formula (3), Y1 and Y2 each represent a halogen atom or a haloalkyl group; Rf represents a C3-C4 perfluoroalkyl group; and R1 and R2 each represent a hydrogen atom or an alkyl group; LG represents a leaving group; T represents a hydrogen atom or a fluorine atom; X1, X3, X4, and X5 each represent a hydrogen atom, a halogen atom, or the like; and A represents a nitrogen atom, a methine group, or the like.
    Type: Grant
    Filed: June 17, 2014
    Date of Patent: July 19, 2016
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Youji Aoki, Yumi Kobayashi, Hidenori Daido, Hiroyuki Katsuta, Hidetaka Tsukada, Atsushi Hirabayashi, Yusuke Takahashi, Michikazu Nomura, Atsuko Kawahara
  • Patent number: 9365557
    Abstract: The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. Certain compounds of this invention have formula IA: wherein the variables are as defined herein.
    Type: Grant
    Filed: March 24, 2014
    Date of Patent: June 14, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
  • Patent number: 9260398
    Abstract: Sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.
    Type: Grant
    Filed: December 9, 2014
    Date of Patent: February 16, 2016
    Assignee: PARION SCIENCES, INC.
    Inventors: Michael Ross Johnson, William Robert Thelin, Richard C. Boucher
  • Patent number: 9139560
    Abstract: Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerization and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).
    Type: Grant
    Filed: February 28, 2014
    Date of Patent: September 22, 2015
    Assignee: YM Biosciences Australia Pty Ltd.
    Inventors: Christopher John Burns, Andrew Frederick Wilks, Michael Francis Harte, Harrison Sikanyika, Emmanuelle Fantino
  • Patent number: 9116161
    Abstract: Provided is a preparation method of a free fatty acid particle dispersion solution, the preparation method including: a) dissolving fatty acid in a solvent to prepare a fatty acid solution; and b) injecting the fatty acid solution in a non-solvent having miscibility with the solvent to prepare a free fatty acid particle dispersion solution.
    Type: Grant
    Filed: November 7, 2013
    Date of Patent: August 25, 2015
    Assignee: KOREA RESEARCH INSTITUTE OF STANDARDS AND SCIENCE
    Inventors: Se Hwa Kim, Eun-Soo Lee
  • Patent number: 9102633
    Abstract: The present invention relates to the compound of the formula: or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: August 11, 2015
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Patent number: 9096548
    Abstract: The present invention relates to compounds of formula 1 or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, R4, R5, R6 and X? have the meanings as indicated in the specification, to their use as a medicament, to their use in the treatment of a disease selected from among respiratory diseases or complaints and allergic diseases of the airways, to pharmaceutical composition comprising at least one of said compound or a pharmaceutically acceptable salt thereof, as well as to medicament combinations containing one or more of said compounds or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 7, 2014
    Date of Patent: August 4, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dieter Wiedenmayer, Armin Heckel, Dieter Hamprecht
  • Patent number: 9090570
    Abstract: The invention relates to compounds of structural formula (I) and structural formula (VI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R, R1, R2, Z, L, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: July 23, 2013
    Date of Patent: July 28, 2015
    Inventors: Lijun Sun, Shoujun Chen, Jun Jiang, Yu Xie, Chih-Yi Yu
  • Publication number: 20150141427
    Abstract: The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Saliha Moussaoui, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Publication number: 20150141387
    Abstract: The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is N-Cyclopropyl-3-fluoro-4-methyl-5-[3-[[1-[2-[2-(methylamino)ethoxy]phenyl]cyclopropyl]amino]-2-oxo-1(2H)-pyrazinyl]-benzamide or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a ?2 adrenoceptor agonist; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DPI antagonist; an Histone Deacetylase activator; an IKK2 kinase inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; a MABA compound; an MPO inhibitor; a muscarinic antagonist; a PDE4 inhibitor; a PPAR? agonist; a protease inhibitor; a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 21, 2015
    Inventors: Anne Elizabeth COOPER, Timothy Jon LUKER, Jerzy Andrzej SCHMIDT
  • Publication number: 20150133414
    Abstract: It was determined whether SNPs in SLC4A5 are associated with salt sensitivity of blood pressure (BP). Subjects consumed an isocaloric constant diet with a randomized order of 7 days low Na+ (10 mmol/d) and 7 days high Na+ (300 mmol/d) intake. Salt sensitivity was defined as a ?7 mm Hg increase in mean arterial pressure (MAP). 35 polymorphisms in 17 candidate genes were assayed. Association analyses with salt sensitivity revealed three variants that associated with salt sensitivity, two in SLC4A5 (rs7571842, rs10177833; P<0.001), and one in GRK4 (rs1801058; P=0.020). Paradoxical changes in blood pressure in response to changes in salt intake were also found associated with a SNP for DRD2 (rs6276). In conclusion, SLC4A5 variants are strongly associated with salt sensitivity of BP in Caucasian and a DRD2 SNP is a marker for paradoxical response to salt intake.
    Type: Application
    Filed: April 22, 2013
    Publication date: May 14, 2015
    Applicant: University of Virginia Patent Foundation
    Inventors: Robin A. Felder, Robert M. Carey, John E. Jones, Pedro A. Jose, Scott M. Williams
  • Patent number: 9029382
    Abstract: The present invention relates compounds of the formula: or pharmaceutically acceptable salts thereof, useful as sodium channel blockers, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including cystic fibrosis, chronic obstructive pulmonary disease, asthma, bronchiectasis, acute and chronic bronchitis, emphysema, and pneumonia.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: May 12, 2015
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Publication number: 20150126527
    Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Application
    Filed: October 9, 2014
    Publication date: May 7, 2015
    Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J.M. Sadeque, Anna Shifrina, Young-Jun Shin, Pureza Vallar, Ning Zou
  • Publication number: 20150126490
    Abstract: The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.
    Type: Application
    Filed: October 29, 2014
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Jeffrey T. BAGDANOFF, Yu DING, Wooseok HAN, Zilin HUANG, Qun JIANG, Jeff Xianming JIN, Xiang KOU, Patrick LEE, Mika LINDVALL, Zhongcheng MIN, Yue PAN, Sabina PECCHI, Keith Bruce PFISTER, Daniel POON, Vivek RAUNIYAR, Xiaojing Michael WANG, Qiong ZHANG, Jianguang ZHOU, Shejin ZHU
  • Publication number: 20150110871
    Abstract: The present invention relates to a gastric retentive tablet composition comprising: (1) coated particles essentially consisting of a drug and an amino methacrylate copolymer, (2) a methacrylic acid copolymer and (3) an excipient, wherein items 1, 2, and 3 are blended together, and then compressed into a gastric retentive tablet. Thus, the coated particles (item 1), a methacrylic acid copolymer and the excipient are evenly distributed in the tablet. The excipient is selected from a group consisting of a retarding agent, a binder, a filler, a chelating agent, a diluent, a disintegrant, a lubricant, a colorant, a solubilizing agent, or a mixture thereof. The coated particles (item 1) do not contain methacrylic acid polymer.
    Type: Application
    Filed: January 3, 2015
    Publication date: April 23, 2015
    Inventor: David Wong
  • Patent number: 9005581
    Abstract: Provided herein are compounds, preparations and formulations comprising pyrazine derivatives having multiple poly(ethylene glycol) containing substituents. Many of the compounds disclosed herein are excretable by the renal system of a subject or patient and are useful for visualizing the renal system of a subject or patient. Upon excitation by electromagnetic radiation, a number of the compounds disclosed herein exhibit luminescence and are externally detectable when present in the body fluid of a patient or subject. Also provided herein are methods for visualizing the renal system of a subject or patient.
    Type: Grant
    Filed: March 4, 2014
    Date of Patent: April 14, 2015
    Assignee: MediBeacon, LLC
    Inventors: Amruta Poreddy, William L. Neumann
  • Publication number: 20150099764
    Abstract: Sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.
    Type: Application
    Filed: December 9, 2014
    Publication date: April 9, 2015
    Applicant: PARION SCIENCES, INC.
    Inventors: Michael Ross JOHNSON, William Robert Thelin, Richard C. Boucher
  • Patent number: 8999996
    Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Grant
    Filed: March 19, 2014
    Date of Patent: April 7, 2015
    Assignee: Karyopharm Therapeutics Inc.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
  • Publication number: 20150087656
    Abstract: Prolongation compositions for prolonging the presence of drugs in blood.
    Type: Application
    Filed: November 26, 2014
    Publication date: March 26, 2015
    Inventors: Aida Salatinjants, Robert Salatinjants