Bicyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos (e.g., 1,4-benzoxazines, Etc.) Patents (Class 514/230.5)
  • Patent number: 10301294
    Abstract: Disclosed are compounds that can be used for treating tuberculosis.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: May 28, 2019
    Assignees: THE BROAD INSTITUTE INC., MASSACHUSETTS GENERAL HOSPITAL, BRIGHAM AND WOMEN'S HOSPITAL
    Inventors: Timothy A. Lewis, Sivaraman Dandapani, Deborah Hung, Benito Munoz, Partha Nag, Sarah Grant, Tomohiko Kawate
  • Patent number: 10287299
    Abstract: A series of substituted 3,4-dihydro-2H-.1,4-benzoxazin-3-one derivatives, and analogs thereof, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neuradegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: June 7, 2016
    Date of Patent: May 14, 2019
    Assignee: UCB Biopharma SPRL
    Inventors: Gareth Neil Brace, Prafulkumar Tulshibhai Chovatia, Gregory Foulkes, James Andrew Johnson, Severine Danielle Jones, Boris Kroeplien, Fabien Claude Lecomte, Pui Leng Loke, Martin Alexander Lowe, Ajay Mandal, Timothy John Norman, Christopher Francis Palmer, Yolanda Pérez-Fuertes, John Robert Porter, Donald Smyth, Giancarlo Trani, Muhammed Uddin, Zhaoning Zhu
  • Patent number: 10287300
    Abstract: The invention provides novel imidazol-piperidinyl derivatives of the formula (I) in which R1, R2, W, X1, X2, X3, X4 and n have the meanings indicated in formula I, and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: November 20, 2017
    Date of Patent: May 14, 2019
    Assignee: Merck Patent GmbH
    Inventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Yufang Xiao
  • Patent number: 10273235
    Abstract: Substituted dihydroisoxazole derivatives useful as inhibitors of ?-lactamases are provided. The invention further provides medical uses of substituted dihydroisoxazole derivatives, for example, as antibacterial agents.
    Type: Grant
    Filed: March 9, 2018
    Date of Patent: April 30, 2019
    Assignee: LegoChem Biosciences, Inc.
    Inventors: Hye Kyung Chang, Sung Yoon Baek, Min Jung Kim, Kyu Man Oh, Jeung Soon Choi, Soo Bong Ha, Sung Min Kim, Chul-woong Chung, Dae Hyuck Kang, Hyun Jin Kwon, Young Lag Cho, Yong Zu Kim
  • Patent number: 10253041
    Abstract: Phenylethylamino-4H-pyrimido[4,5-d][1,3]oxazin-2-one compounds of Formula I, formulations containing those compounds, and their use as mutant isocitrate dehydrogenase 1 enzyme inhibitors.
    Type: Grant
    Filed: July 21, 2016
    Date of Patent: April 9, 2019
    Assignee: Eli Lilly and Company
    Inventors: Renato A. Bauer, Serge Louis Boulet, Timothy Paul Burkholder, Santiago Carballares Martin, James Ronald Gillig, Raymond Gilmour, Wenceslao Lumeras, Zhipei Wu
  • Patent number: 10246417
    Abstract: This disclosure relates to picolinamides of Formula I and their use as fungicides.
    Type: Grant
    Filed: January 5, 2018
    Date of Patent: April 2, 2019
    Assignee: Dow AgroSciences LLC
    Inventors: Brian A. Loy, Jared W. Rigoli, Brannon Sam, Kevin G. Meyer, Chenglin Yao
  • Patent number: 10233180
    Abstract: Disclosed are new substituted nitrogen-containing heterocyclic derivatives represented by formula (I) as AKT inhibitors, optical isomers, pharmaceutically acceptable salts or solvates thereof, wherein the definition of R1, R2, R3, R4, R5, R6, ring A, ring C, B, Q, Y, Z and m is shown in the description for details. In addition, medicaments comprising the derivatives as active components are also disclosed, which can be useful for treating proliferative diseases, such as cancer and inflammation, especially diseases relating to AKT kinase.
    Type: Grant
    Filed: March 21, 2015
    Date of Patent: March 19, 2019
    Assignees: ZHEJIANG UNIVERSITY, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Xiaowu Dong, Jia Li, Bo Yang, Yongzhou Hu, Yubo Zhou, Qinjie Weng, Wenhu Zhan, Lei Xu, Tao Liu, Qiaojun He
  • Patent number: 10227305
    Abstract: The present invention relates to a process for preparing indacaterol or salts thereof. The process comprises of forming compound of Formula 1 by reacting compound of Formula 2 and compound of Formula 3 in the presence of a solvent to Form compound of Formula 4, which on removal of the protecting groups forms compound of Formula 1.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: March 12, 2019
    Inventors: G. Pratap Reddy, Venkataiah Sunku, Sunkaraneni Suresh Babu
  • Patent number: 10221161
    Abstract: The present invention provides compounds of formula (I), compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R5, R6, R7, R12, R13, A, L, B, n, W, X, Y and Z are as defined herein.
    Type: Grant
    Filed: August 14, 2014
    Date of Patent: March 5, 2019
    Assignee: Kalvista Pharmaceuticals Limited
    Inventors: Hannah Joy Edwards, David Michael Evans, Premji Meghani, Andrew Richard Novak
  • Patent number: 10213477
    Abstract: Provided herein are peptidomimetic macrocycles containing amino acid sequences with at least two modified amino acids that form an intramolecular cross-link that can help to stabilize a secondary structure of the amino acid sequence. Suitable sequences for stabilization include those with homology to the p53 protein. These sequences can bind to the MDM2 and/or MDMX proteins. Also provided herein are methods of using such macrocycles for the treatment of diseases and disorders, such as cancers or other disorders characterized by a low level or low activity of a p53 protein or high level of activity of a MDM2 and/or MDMX protein.
    Type: Grant
    Filed: August 5, 2016
    Date of Patent: February 26, 2019
    Assignee: Aileron Therapeutics, Inc.
    Inventors: Vincent Guerlavais, Carl Elkin, Huw M. Nash, Tomi K. Sawyer, Bradford J. Graves, Eric Feyfant
  • Patent number: 10208061
    Abstract: The invention provides tetrahydro[1,8]naphthyridine and related compounds, pharmaceutical compositions, methods of promoting ROR activity, increasing the amount of IL-17 in a subject, and treating cancer using such tetrahydro[1,8]naphthyridine and related compounds.
    Type: Grant
    Filed: October 11, 2017
    Date of Patent: February 19, 2019
    Assignee: Lycera Corporation
    Inventors: Thomas D. Aicher, Peter L. Toogood, Xiao Hu
  • Patent number: 10208034
    Abstract: A compound represented by general formula (I) and having a quinoline skeleton has a strong Axl inhibitory activity, and therefore the compound can be an agent for treating Axl-related diseases, for example, cancer such as acute myeloid leukemia, chronic myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glioma, kidney diseases, immune system diseases, and circulatory system diseases.
    Type: Grant
    Filed: December 24, 2015
    Date of Patent: February 19, 2019
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Takayuki Inukai, Jun Takeuchi, Tomoko Yasuhiro
  • Patent number: 10195205
    Abstract: This invention relates to new use of dual NK-1/NK-3 receptor antagonists or a pharmaceutically acceptable salt thereof in the treatment of sex-hormone dependent diseases.
    Type: Grant
    Filed: May 18, 2016
    Date of Patent: February 5, 2019
    Assignee: NeRRe Therapeutics Limited
    Inventor: Mike Trower
  • Patent number: 10155731
    Abstract: The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.
    Type: Grant
    Filed: January 12, 2016
    Date of Patent: December 18, 2018
    Assignees: MITSUBISHI TANABE PHARMA CORPORATION, SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Toru Iijima, Hiroshi Sugama, Takayuki Kawaguchi, Jingkang Shen, Guangxin Xia, Jianshu Xie, Miki Hirai
  • Patent number: 10155758
    Abstract: The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.
    Type: Grant
    Filed: September 26, 2017
    Date of Patent: December 18, 2018
    Assignee: SciFluor Life Sciences, Inc.
    Inventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan
  • Patent number: 10149841
    Abstract: A compound of the following formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently H; R3 is selected from H, a C1-C7 straight-chain, and a branched or cyclic alkyl; and R4, R5, R6, R7, and R8 are each independently selected from C1-C7 alkyl, halo C1-C7 alkyl and the like. Also provided is a method for preparing the compound, pharmaceutical compositions including the compound or pharmaceutically acceptable salts thereof, and uses of the compound or pharmaceutically acceptable salt thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: December 11, 2018
    Assignee: SHENYANG SUNSHINE PHARMACEUTICAL CO. LTD.
    Inventors: Yunlong Zhou, Suixiong Cai, Guangfeng Wang, Lingling Jiao, Ping Min, Yu Jing, Ming Guo
  • Patent number: 10124004
    Abstract: The purpose of the present invention is to provide a compound having an excellent CDK4/6 inhibiting activity. The present invention is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: November 13, 2018
    Assignee: Teijin Pharma Limited
    Inventors: Tsuyoshi Mizuno, Tomohiro Shimada, Gen Unoki, Masaru Ebisawa, Susumu Takeuchi, Kunio Minamizono, Kosuke Sasaki, Takuya Yokosaka, Junji Igarashi, Akinobu Maruyama, Hiroshi Takahashi, Kyohei Horie, Yuri Sakai
  • Patent number: 10125145
    Abstract: The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: May 18, 2017
    Date of Patent: November 13, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Stephen Hitchcock, Holger Monenschein, Holly Reichard, Huikai Sun, Shota Kikuchi, Todd Macklin, Maria Hopkins
  • Patent number: 10077259
    Abstract: The present disclosure provides bicyclic heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as bromodomain inhibitors; (I), in which R1, R2, R3, R4, L1, L2, Cy1, Cy2, X, n, and dotted line have the same meaning given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in diseases or disorders associated as bromodomain inhibitors. The present disclosure also provides preparation of compounds and pharmaceutical formulations comprising at least one of bicyclic heterocyclic derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent, or excipient.
    Type: Grant
    Filed: January 6, 2015
    Date of Patent: September 18, 2018
    Assignee: Orion Corporation
    Inventors: Susanta Samajdar, Chandrasekhar Abbineni, Sanjita Sasmal, Subramanya Hosahalli
  • Patent number: 10064935
    Abstract: The disclosure describes HCMV ribonucleic acid (RNA) vaccines, as well as methods of using the vaccines and compositions comprising the vaccines.
    Type: Grant
    Filed: August 11, 2017
    Date of Patent: September 4, 2018
    Assignee: ModernaTX, Inc.
    Inventors: Giuseppe Ciaramella, Shinu John, Kambiz Mousavi
  • Patent number: 10034477
    Abstract: This disclosure relates to pyrido-1,3-oxazine-2,4-diones of Formula I and their use as fungicides.
    Type: Grant
    Filed: August 30, 2017
    Date of Patent: July 31, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Brannon Sam, Kevin G. Meyer, Chenglin Yao, Brian A. Loy, Jared W. Rigoli, Nicholas R. Babij
  • Patent number: 10010530
    Abstract: The present disclosure relates to solid crystalline forms of N—((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide (I) and the diastereomers thereof, and to methods for preparing such crystalline forms. Compound (I) and the diastereomers thereof are potent androgen receptor (AR) modulators useful as a medicament.
    Type: Grant
    Filed: January 28, 2016
    Date of Patent: July 3, 2018
    Assignee: Orlon Corporation
    Inventors: Olli Törmäkangas, Terhi Heikkinen
  • Patent number: 10000481
    Abstract: The inventions relates to compounds of (I) and therapeutic uses thereof: (I) The terms Z, Y, and R1 are as defined in the claims.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: June 19, 2018
    Assignee: Vernalis (R&D) Limited
    Inventors: Stephen Stokes, Christopher John Graham, Stuart Christopher Ray, Emma Jayne Stefaniak
  • Patent number: 10000450
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Grant
    Filed: February 16, 2017
    Date of Patent: June 19, 2018
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Muneaki Kurimura, Shinichi Taira, Takahiro Tomoyasu, Nobuaki Ito, Kuninori Tai, Noriaki Takemura, Takayuki Matsuzaki, Yasuhiro Menjo, Shin Miyamura, Yohji Sakurai, Akihito Watanabe, Yasuyo Sakata, Takumi Masumoto, Kohei Akazawa, Haruhiko Sugino, Naoki Amada, Satoshi Ohashi, Tomoichi Shinohara, Hirofumi Sasaki, Chisako Morita, Junko Yamashita, Satoko Nakajima
  • Patent number: 9993483
    Abstract: The present invention relates to methods for treating an ophthalmic, otic, or nasal infection comprising treating the infected tissue with a composition comprising finafloxacin or a finafloxacin derivative. The present invention also relates to antimicrobial compositions comprising finafloxacin or a finafloxacin derivative. The compositions are suitable for the treatment of ophthalmic, otic, or nasal infections.
    Type: Grant
    Filed: July 27, 2015
    Date of Patent: June 12, 2018
    Assignee: Alcon Research, Ltd.
    Inventors: David W. Stroman, Masood A. Chowhan, Kenneth C. Appell
  • Patent number: 9975862
    Abstract: The present invention provides arylpiperazine derivatives having Formula I as shown below, which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression,
    Type: Grant
    Filed: March 27, 2017
    Date of Patent: May 22, 2018
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Kouacou Adiey
  • Patent number: 9962362
    Abstract: Inhibitors of EYA tyrosine phosphatase are provided herein, as well as pharmaceutical compositions and methods relating thereto.
    Type: Grant
    Filed: March 6, 2013
    Date of Patent: May 8, 2018
    Assignee: Children's Hospital Medical Center
    Inventor: Rashmi Hegde
  • Patent number: 9956220
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically-acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Grant
    Filed: June 18, 2015
    Date of Patent: May 1, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Upender Velaparthi, Selvakumar Kumaravel, Arul Mozhi Selvan Subbiah Karupplah, Shilpa Holehatti Maheshwarappa, Chandrasekhar Reddy Rachamreddy, Mark D. Wittman
  • Patent number: 9951072
    Abstract: Substituted dihydroisoxazole derivatives useful as inhibitors of ?-lactamases are provided. The invention further provides medical uses of substituted dihydroisoxazole derivatives, for example, as antibacterial agents.
    Type: Grant
    Filed: September 30, 2016
    Date of Patent: April 24, 2018
    Assignee: LegoChem Biosciences, Inc.
    Inventors: Hye Kyung Chang, Sung Yoon Baek, Min Jung Kim, Kyu Man Oh, Jeung Soon Choi, Soo Bong Ha, Sung Min Kim, Chul-woong Chung, Dae Hyuck Kang, Hyun Jin Kwon, Young Lag Cho, Yong Zu Kim
  • Patent number: 9925193
    Abstract: The present invention relates to thioether derivatives (1) as protein kinase inhibitors, which are useful for the treatment, relieve and/or prevention of diseases associated with abnormal and hyperproliferation of cells in a mammal, especially humans, and which are particularly useful for the treatment of all forms of cancer.
    Type: Grant
    Filed: November 11, 2013
    Date of Patent: March 27, 2018
    Assignee: ProQinase GmbH
    Inventors: Michael Kubbutat, Christoph Schachtele, Jan Ehlert, Frank Totzke, Conrad Kunick, Sebastian Wolfel, Holger Weber
  • Patent number: 9920019
    Abstract: Base compounds including 1,3-oxazinan-6-one derivatives of N-alkyl or N-alkenyl or N-cycloalkyl or N-aryl propionic acids and paraformaldehyde, and their application as corrosion inhibitors with multifunctional properties serving as inhibitory/dispersant of asphaltene in production processes, transportation, refining and storage of crude oil and derivatives. The corrosion inhibitor with inhibitory/dispersant of asphaltenes properties comprises an active substance base of 1,3-oxaninan-6-ones and hydrocarbon solvents such as benzene, toluene, mixed xylenes, o-xylene, m-xylene and p-xylene, diesel, kerosene, jet fuel, alcohols, aliphatic branched and unbranched alcohols containing from 3 to 10 carbon atoms, such as isopropanol, butanol and pentanol, and mixtures of hydrocarbon solvents with aliphatic branched or unbranched liquid fuels. In addition, a process for obtaining 1,3-oxazinan-6-ones derivatives of N-alkyl or N-alkenyl or N-cycloalkyl or N-aryl propionic acids and paraformaldehyde is described.
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: March 20, 2018
    Assignee: Instituto Mexicano del Petroleo
    Inventors: Raul Hernandez Altamirano, Violeta Yasmin Mena Cervantes, Luis Silvestre Zamudio Rivera, Hiram Isaac Beltran Conde, Eduardo Buenrostro Gonzalez
  • Patent number: 9913842
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: July 8, 2016
    Date of Patent: March 13, 2018
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
  • Patent number: 9855273
    Abstract: Disclosed are compositions and methods for the treatment of disorders such as myelodysplastic syndrome (MDS) and acute myeloid leukemia (AML). The disclosed methods include administering to an individual in need of such treatment a composition that may include an IRAK1/4 inhibitor. In other aspects, the method may include administration of a BLC2 inhibitor.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: January 2, 2018
    Assignee: Children's Hospital Medical Center
    Inventors: Daniel Starczynowski, Garrett W. Rhyasen
  • Patent number: 9828370
    Abstract: The present invention provides compounds for the prevention or treatment of cancer or a bacterial or viral infection. Additionally, the present invention provides compositions and methods for using these compounds and compositions in the prevention or treatment of cancer or a bacterial or viral infection in a subject.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: November 28, 2017
    Assignee: INHIBIKASE THERAPEUTICS, INC.
    Inventors: Milton H. Werner, Terence A. Kelly
  • Patent number: 9828605
    Abstract: The present disclosure relates to a composition for enhancing radiation sensitivity including a PI4K isozyme inhibitor as an active ingredient. As the PI4K isozyme inhibitor, a PI4K isozyme-specific siRNA or antiviral agent according to the present disclosure has an excellent effect of enhancing radiation sensitivity such as reducing viability of the cancer cells and radiation resistance during in radiation irradiation and suppressing and delaying DNA damage repair induced by the radiation by inhibiting the PI4K isozyme to be used as a radiation sensitivity adjuvant and an anticancer treatment assisting agent.
    Type: Grant
    Filed: February 19, 2016
    Date of Patent: November 28, 2017
    Assignee: SEOUL NATIONAL UNIVERSITY R&DB FOUNDATION
    Inventors: In ah Kim, Dan Hyo Kim, Jean ny Kwon, Ji Min Park, Young hee Park
  • Patent number: 9808457
    Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
    Type: Grant
    Filed: October 28, 2016
    Date of Patent: November 7, 2017
    Assignee: Heptares Therapeutics Limited
    Inventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Bucknell, Francesca Deflorian, Mark Pickworth, Jonathan Stephen Mason
  • Patent number: 9790214
    Abstract: Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions in a method of treating cancer. The dUTPase inhibitors disclosed contain a uracil isostere in the molecule represented by a 2,6-diketopiperazine moiety. Thioanalogs of the uracil isostere where a thione replaces each of the ketone are also disclosed.
    Type: Grant
    Filed: January 2, 2015
    Date of Patent: October 17, 2017
    Assignee: University of Southern California
    Inventors: Robert D. Ladner, Bruno Giethlen
  • Patent number: 9777006
    Abstract: The present invention is directed to compounds encompassed by the Formula (I): pharmaceutical compositions thereof, methods for inhibiting LTA-4 hydrolase, and methods for the treatment of a disease and disorder which is ameliorated by the inhibition of LTA4h activity. Non-limiting examples of such diseases and conditions include inflammatory and autoimmune diseases and disorders.
    Type: Grant
    Filed: September 10, 2015
    Date of Patent: October 3, 2017
    Assignee: Celtaxsys, Inc.
    Inventor: William Guilford
  • Patent number: 9737546
    Abstract: A method of enhancing p53 activity of a p53 mutant polypeptide is provided. The method includes interacting a compound to an open L1/S3 binding site of the p53 mutant polypeptide, where the p53 activity of the p53 mutant polypeptide is enhanced in the presence of the compound. Compounds were identified from databases of compounds for virtual drug screening. Methods of screening for compounds that enhance p53 activity by binding to the open L1/S3 binding site, and methods of treatment using the identified compounds, are also provided.
    Type: Grant
    Filed: August 9, 2014
    Date of Patent: August 22, 2017
    Assignee: The Regents of the University of California
    Inventors: Rommie E. Amaro, Roberta Baronio, Ozlem Demir, Peter Kaiser, Richard H. Lathrop, Seyedey-Faezeh Salehi-Amin, Christopher D. Wassman
  • Patent number: 9725419
    Abstract: The present disclosure provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: August 8, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Ankush Argade, Rajinder Singh, Sambaiah Thota, David Carroll, Kin Tso, Vanessa Taylor, John McLaughlin, Vadim Markovtsov
  • Patent number: 9725461
    Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
    Type: Grant
    Filed: November 12, 2014
    Date of Patent: August 8, 2017
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Haixaio Zhai, Chengjung Lai, Changgeng Qian
  • Patent number: 9708338
    Abstract: The present invention is related to a compound represented by formula (I) wherein —X— is —NH— or —S—; —Z— is —O— or —S—; R3, R5 and R6 are each independently a hydrogen atom, substituted or unsubstituted alkyl, or the like; R7 is a cyano, substituted or unsubstituted amino, or the like; R7? is each independently a halogen; b is 0 or 1; or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising thereof.
    Type: Grant
    Filed: March 22, 2016
    Date of Patent: July 18, 2017
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Akira Yukimasa, Naoki Tsuno, Motohiro Fujiu, Hiroki Yamaguchi, Hiromi Kudo, Tatsuhiko Ueno, Yusuke Ichihashi, Takatsugu Inoue, Shinji Suzuki
  • Patent number: 9694008
    Abstract: The present invention relates to an orally fast dissolving film formulation including aripiprazole. The orally fast dissolving film formulation includes aripiprazole or a pharmaceutically acceptable salt thereof and an organic acid. The orally fast dissolving film formulation has a pH in the range of 4.7 to 6.0. The orally fast dissolving film formulation may further include a film base polymer. The orally fast dissolving film formulation has a high dissolution rate, causes no risk of damage to oral tissues, masks a bitter taste of aripiprazole, and gives a good feeling upon taking.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: July 4, 2017
    Assignee: CMG Pharmaceutical Co., LTD.
    Inventors: Yong Soo Kim, Jun Ho Shin
  • Patent number: 9676736
    Abstract: A molecule with neural activities, especially 4-substituent-2-hydroxymorpholin-3-one, as a new intermediate of neurokinin-1 receptor antagonist aprepitant, and preparation method thereof.
    Type: Grant
    Filed: April 15, 2013
    Date of Patent: June 13, 2017
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Fuli Zhang, Chonghao Liu, Pengcheng Qiu, Jian Chai, Qingfeng Cai
  • Patent number: 9670229
    Abstract: The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: May 9, 2016
    Date of Patent: June 6, 2017
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Stephen Hitchcock, Holger Monenschein, Holly Reichard, Huikai Sun, Shota Kikuchi, Todd Macklin, Maria Hopkins
  • Patent number: 9670209
    Abstract: Compounds of formula (I) and methods are provided for the treatment of disease or conditions in which modification of cholinergic, especially muscarinic receptor activity, has a beneficial effect.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: June 6, 2017
    Assignees: ACADIA PHARMACEUTICALS INC., ALLERGAN, INC.
    Inventors: Ethan S. Burstein, Jorgen Eskildsen, Roger Olsson
  • Patent number: 9636340
    Abstract: The disclosed molecules are inhibitors of Bcr-Abl and Src kinases. The molecules are cytotoxic to Gleevec resistant cells. Inhibitors of Bcr-Abl and Src kinases are used in the treatment of Chronic Myelogenous Leukemia among other diseases.
    Type: Grant
    Filed: November 11, 2014
    Date of Patent: May 2, 2017
    Inventor: Ayyappan K. Rajasekaran
  • Patent number: 9580423
    Abstract: The present disclosure relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR4 enzyme and are useful in the treatment of FGFR4-associated diseases such as cancer.
    Type: Grant
    Filed: February 19, 2016
    Date of Patent: February 28, 2017
    Assignee: Incyte Corporation
    Inventors: Liang Lu, Liangxing Wu, Bo Shen, Wenqing Yao
  • Patent number: 9545385
    Abstract: Compounds, compositions and methods related to the prevention or treatment of isoprostane-mediated tissue damage in a mammalian subject in need thereof.
    Type: Grant
    Filed: February 5, 2014
    Date of Patent: January 17, 2017
    Assignee: Vanderbilt University
    Inventors: John A. Oates, L. Jackson Roberts, Ned A. Porter, Olivier Boutaud
  • Patent number: 9539259
    Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
    Type: Grant
    Filed: May 23, 2013
    Date of Patent: January 10, 2017
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Donald J. Zack, Derek Stuart Welsbie, Zhiyong Yang