Plural Ring Nitrogens In The Additional Hetero Ring (e.g., Imidazole, Pyrazine, Etc.) Patents (Class 514/235.8)
  • Patent number: 10316002
    Abstract: The invention relates to compounds and their use in the treatment of disease. Novel irreversible inhibitors of wild-type and mutant forms of EGFR, FGFR, ALK, ROS, JAK, BTK, BLK, ITK, TEC, and/or TXK and their use for the treatment of cell proliferation disorders are described.
    Type: Grant
    Filed: September 6, 2017
    Date of Patent: June 11, 2019
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael Gray, Hwan Geun Choi, Li Tan
  • Patent number: 10196357
    Abstract: The invention relates to compounds of formula IB and methods for modulating one or more components of a kinase cascade using these compounds.
    Type: Grant
    Filed: April 14, 2008
    Date of Patent: February 5, 2019
    Assignee: Athenex, Inc.
    Inventor: David G. Hangauer, Jr.
  • Patent number: 10138223
    Abstract: An objective of the present invention is to obtain a stable crystal form of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4 (1H,3H)-pyrimidinedione hydrochloride. The present invention provides a crystal of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4 (1H,3H)-pyrimidinedione hydrochloride exhibiting characteristic peaks at angles of 11.6°, 17.2°, 17.8°, 23.3°, 27.1°, and 29.3° as a diffraction angle (2?±0.1°) in powder X-ray diffraction.
    Type: Grant
    Filed: November 16, 2016
    Date of Patent: November 27, 2018
    Assignee: TAIHO PHARMACEUTICALS CO., LTD.
    Inventors: Hideki Kazuno, Tomonobu Mutsumi
  • Patent number: 10130631
    Abstract: The present invention relates to a therapeutic agent for chronic myelogenous leukemia with reduced drug-resistance and side-effects containing a 1,6-disubstituted indole compound.
    Type: Grant
    Filed: August 15, 2017
    Date of Patent: November 20, 2018
    Assignee: Korea Institute of Science and Technology
    Inventors: Tae Bo Sim, Ho Jong Yoon, Woo Young Hur, Yun Ju Nam, Hwan Geun Choi
  • Patent number: 10117853
    Abstract: A compound exerts a strong analgesic effect against pain, in particular, neuropathic pain and/or fibromyalgia syndrome. A cyclic amine derivative represented by general formula or a pharmacologically acceptable salt thereof: A method of treating neuropathic pain includes administering a therapeutically effective amount of the cyclic amine derivative to a mammal. A method of treating fibromyalgia syndrome includes administering a therapeutically effective amount of the cyclic amine derivative to a mammal.
    Type: Grant
    Filed: March 24, 2016
    Date of Patent: November 6, 2018
    Assignee: Toray Industries, Inc.
    Inventors: Shuji Udagawa, Yasuhiro Morita, Naoki Izumimoto, Katsuhiko Iseki, Shunsuke Iwano, Tomoya Miyoshi, Yuji Osada, Tetsuro Koreeda, Masanori Murakami, Motohiro Shiraki, Kei Takahashi, Keiyu Oshida, Eriko Higashi
  • Patent number: 10059675
    Abstract: The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A1, X, A2, W1, W2, W3, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
    Type: Grant
    Filed: May 4, 2017
    Date of Patent: August 28, 2018
    Assignee: Purdue Pharma L.P.
    Inventors: Chiyou Ni, Laykea Tafesse, Jiangchao Yao, Mark A. Youngman, Minnie Park, Bin Shao
  • Patent number: 10053429
    Abstract: The present invention provides compounds of the Formula below: [Formula should be inserted here] Where A, X, R. and R2-R3 are as described herein; methods of treating patients for hypertriglyceridemia and cardiovascular disease including dyslipidemia and atherosclerosis, and processes for preparing the compounds.
    Type: Grant
    Filed: May 19, 2016
    Date of Patent: August 21, 2018
    Assignee: Eli Lilly and Company
    Inventors: Ana Maria Escribano, Maria Rosario Gonzalez, Celia Lafuente Blanco, Maria Dolores Martin-Ortega Finger, Michael R Wiley
  • Patent number: 10047056
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: July 20, 2017
    Date of Patent: August 14, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Makonen Belema, Van N. Nguyen
  • Patent number: 9890140
    Abstract: The present invention relates to AZD2171 maleate salt, to particular crystalline forms of AZD2171 maleate salt, to processes for their preparation, to pharmaceutical compositions containing them as active ingredient, to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to their use in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability.
    Type: Grant
    Filed: September 13, 2016
    Date of Patent: February 13, 2018
    Assignee: ASTRAZENECA AB
    Inventor: James McCabe
  • Patent number: 9856232
    Abstract: A dihydropyrimidinone derivative includes a compound having a chemical structure according to Formula 1: wherein Z is selected from CH2O, O, and N; X is selected from O and S; and R represents aryl, substituted aryl, heteroaryl, or substituted heteroaryl, wherein the substituted aryl or substituted heteroaryl have one or more substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, nitro, hydroxyl, alkylthio, alkylamino, heteroaryl, aryloxy, haloaryloxy, arylthio, arylamino, and pharmaceutically acceptable salts thereof. The present subject matter also relates to a method of making a dihydropyrimidinone derivative, a method of treating a gastrointestinal disease, a method of treating an ulcer, a pharmaceutical composition, and a method of making a pharmaceutical composition.
    Type: Grant
    Filed: June 20, 2017
    Date of Patent: January 2, 2018
    Assignee: KING SAUD UNIVERSITY
    Inventors: Mashooq Ahmad Bhat, Mohamed Abdulrahman Al-Omar
  • Patent number: 9809568
    Abstract: The present invention is directed to substituted indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
    Type: Grant
    Filed: November 10, 2014
    Date of Patent: November 7, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Duane DeMong, Michael Miller, Hong Liu, Xing Dai, Thomas Greshock, Andrew Stamford, Ravi Nargund
  • Patent number: 9809559
    Abstract: The present invention relates to stable novel salt forms of N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide that are suitable for the preparation of pharmaceutical formulations thereof, and their therapeutic use.
    Type: Grant
    Filed: August 8, 2016
    Date of Patent: November 7, 2017
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Brandon H. Brown, Ernest A. Carra, Jeffrey N. Hemenway, Henry Morrison, Troy Reynolds, Bing Shi, Dimitrios Stefanidis, Fang Wang, Matthew Robert Warr, James Andrew Whitney, Yan Xin
  • Patent number: 9802903
    Abstract: This invention is directed to: (a) processes for preparing a compound and salts thereof that, inter alia, are useful for inhibiting hepatitis C virus (HCV); (b) intermediates useful for the preparation of the compound and salts; (c) pharmaceutical compositions comprising the compound or salts; and (d) methods of use of such compositions.
    Type: Grant
    Filed: November 10, 2015
    Date of Patent: October 31, 2017
    Assignee: AbbVie Inc.
    Inventors: Jean-Christophe Califano, James J. Napier, Calvin L. Becker, Su Yu
  • Patent number: 9795596
    Abstract: The present invention relates to selective cancer treatment regimes based on assaying for the presence or absence of a glutamine or a nucleic acid that encodes glutamine at position 859 of the catalytic p110? subunit of PI3K; methods for producing a transmittable form of information for predicting the responsiveness of patient to (S)-Pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide), or a pharmaceutically acceptable salt thereof; and a kit thereof.
    Type: Grant
    Filed: March 27, 2013
    Date of Patent: October 24, 2017
    Assignee: Novartis AG
    Inventors: Pascal Furet, Christine Fritsch, Sauveur-Michel Maira
  • Patent number: 9789111
    Abstract: The invention relates to pharmaceutical compositions having casein kinase 1 delta (CK1?) inhibitors and to the use of the inhibitors in the treatment of neurodegenerative disorders such as Alzheimer's disease.
    Type: Grant
    Filed: April 2, 2015
    Date of Patent: October 17, 2017
    Assignee: ELECTROPHORETICS LIMITED
    Inventors: Joseph M. Sheridan, Jonathan R. Heal, William D. O. Hamilton, Ian H. Pike
  • Patent number: 9790229
    Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: January 25, 2016
    Date of Patent: October 17, 2017
    Assignees: Sunesis Pharmaceuticals, Inc., Biogen MA Inc.
    Inventors: Minna Bui, Patrick Conlon, Julio H. Cuervo, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Tracy J. Jenkins, Gnanasambandam Kumaravel, Alexey A. Lugovskoy, Doug Marcotte, Noel Powell, Daniel Scott, Laura Silvian, Art Taveras, Deping Wang, Min Zhong
  • Patent number: 9776992
    Abstract: 1-Oxo-1,2-dihydroisoquinolin-7-yl-(5-substituted-thiophen-2-yl)-sulfonamide compounds, formulations containing those compounds, and their use as AICARFT inhibitors.
    Type: Grant
    Filed: November 24, 2015
    Date of Patent: October 3, 2017
    Assignee: Eli Lilly and Company
    Inventors: Harold Burns Brooks, Robert Dean Dally, Timothy Barrett Durham, Kevin Robert Fales, Kwame Frimpong, Jefferson Ray McCowan, Frank George Njoroge, Timothy Alan Shepherd, Chong Si, Kenneth Jeff Thrasher, James Lee Toth, Zhipei Wu
  • Patent number: 9771347
    Abstract: Disclosed herein is a process of making a compound of formula I The compound of formula I is an inhibitor of MEK and thus can be used to treat cancer.
    Type: Grant
    Filed: April 13, 2015
    Date of Patent: September 26, 2017
    Assignee: Exelixis, Inc.
    Inventors: Sriram Naganathan, Nathan Guz, Matthew Pfeiffer, C. Gregory Sowell, Tracy Bostick, Jason Yang, Amit Srivastava
  • Patent number: 9758487
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: June 28, 2016
    Date of Patent: September 12, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
  • Patent number: 9750749
    Abstract: The present invention relates to a methods and compositions for the treatment of and management of symptoms for thyroid eye disease. The methods include administering to a patient having thyroid eye disease an agent that interferes with hyaluronan synthesis in an amount that is effective to inhibit hyaluronan synthesis in a retro-ocular space. The pharmaceutical compositions that includes a carrier suitable for ophthalmic delivery and an agent that interferes with hyaluronan synthesis. Combination therapies are also disclosed.
    Type: Grant
    Filed: March 4, 2016
    Date of Patent: September 5, 2017
    Assignee: University of Rochester
    Inventors: Richard P. Phipps, Naxin Guo, Steven Feldon
  • Patent number: 9725432
    Abstract: The present invention relates to novel compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein the integers are as defined in the description. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
    Type: Grant
    Filed: April 30, 2013
    Date of Patent: August 8, 2017
    Assignee: Janssen Sciences Ireland US
    Inventors: Jean-Francois Bonfanti, Philippe Muller, Frederic Marc Maurice Doublet, Jerome Michel Claude Fortin, Nacer Lounis
  • Patent number: 9718762
    Abstract: The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests; wherein R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts thereof.
    Type: Grant
    Filed: October 24, 2013
    Date of Patent: August 1, 2017
    Assignee: Syngenta Participations AG
    Inventors: Ottmar Franz Hueter, Pierre Joseph Marcel Jung, Thomas Pitterna, Helmars Smits, Andre Stoller
  • Patent number: 9649310
    Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
    Type: Grant
    Filed: February 12, 2016
    Date of Patent: May 16, 2017
    Assignee: CHDI Foundation, Inc.
    Inventors: Celia Dominguez, Leticia M. Toledo-Sherman, Stephen Martin Courtney, Michael Prime, William Mitchell, Christopher John Brown, Paula C. De Aguiar Pena, Peter Johnson
  • Patent number: 9630931
    Abstract: The invention provides compounds which inhibit or modulate the activity of Chk-1 kinase and which are useful in the treatment of cancer. The compounds have the general formula (1): and salts, N-oxides and tautomers thereof, wherein m is 2, 3 or 4; n is 0 or 1; Q1 is selected from a bond; C(?O); S(O); SO2; and an alkylene chain of 1 to 4 carbon atoms in length between the moiety R4 and the nitrogen atom.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: April 25, 2017
    Assignee: SENTINEL ONCOLOGY LIMITED
    Inventors: Robert George Boyle, Richard Justin Boyce
  • Patent number: 9604935
    Abstract: The present invention relates to a deuterated phenyl amino pyrimidine compound and pharmaceutical composition containing the same. Specifically provided are a deuterated phenyl amino pyrimidine compound as represented by formula (I), and pharmaceutical composition containing the compound, or polymorph, pharmaceutically acceptable salt, hydrate or solvate thereof. The compound of the present invention can treat and/or prevent JAK kinase-related diseases, such as bone marrow proliferative disease, cancer, immunologic diseases and the like.
    Type: Grant
    Filed: January 28, 2014
    Date of Patent: March 28, 2017
    Assignee: Suzhou Zelgen Biopharmaceuticals Co., Ltd.
    Inventors: Binhua LV, Zelin Sheng, Benwen Cao
  • Patent number: 9598432
    Abstract: The present invention 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 proliferative diseases such as tumorigenic cancers.
    Type: Grant
    Filed: July 7, 2014
    Date of Patent: March 21, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Ankush Argade, Rajinder Singh, Hui Li, David Carroll, Susan Catalano
  • Patent number: 9592232
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: October 16, 2014
    Date of Patent: March 14, 2017
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • Patent number: 9592224
    Abstract: The invention relates to a family of differently substituted benzothiazoles having inhibitory activity against casein kinase 1 (CK-1) enzyme, as a result of which they are suitable for use in the treatment or prevention of diseases caused by this enzyme, particularly diseases associated with circadian rhythm and inflammatory, autoimmune, psychiatric, neurodegenerative, neurological or ophthalmic diseases, as well as for inducing cell regeneration
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: March 14, 2017
    Assignee: DONSEJO SUPERIOR DE INVESTIGACIONES CIENTÍFICAS (CSIC)
    Inventors: Ana Martínez Gil, Daniel Ignacio Pérez Fernández, Carmen Gil Ayuso-Gontán, Irene García Salado, Miriam Redondo Sancho, Concepción Pérez Martínez
  • Patent number: 9573907
    Abstract: The present invention relates to novel 2,4-pyrimidine derivatives and a use thereof, and more particularly, to pyrimidine derivatives which are effective for systemic lupus erythematosus, a composition for preventing and treating systemic lupus erythematosus comprising the same as an active ingredient and a method for screening the same. The present inventors found novel materials inhibiting surface translocation of gp96 by mimicking a function of AIMP1 which is a molecular anchor for an intracellular residence of gp96, and identified in vitro and in vivo activity of the materials for preventing and treating SLE by alleviating SLE plasma in autoimmune diseases. Therefore, the present invention provides a novel method for screening a therapeutic agent for SLE, and preventing or treating SLE using the mechanism.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: February 21, 2017
    Assignees: SNU R&DB FOUNDATION, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Sunghoon Kim, Jung Min Han, Hyeong Rae Kim, Dong Ju Jeon, Jong Hwan Song, Kyung Eun Park
  • Patent number: 9555115
    Abstract: This invention relates to a pharmaceutical composition for oral administration comprising 4-((1-methylpyrrol-2-yl)-carbonyl)-N-(4-(4-morpholin-1-yl-carbonylpiperidin-1-yl)-phenyl)-1-piperazinecarboxamide, a salt thereof, or a solvate thereof, as an active pharmaceutical ingredient; and at least one acid additive selected from the group consisting of adipic acid, succinic acid, fumaric acid, L-aspartic acid, and L-glutamic acid.
    Type: Grant
    Filed: September 18, 2013
    Date of Patent: January 31, 2017
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventor: Takashi Suefuji
  • Patent number: 9533972
    Abstract: The present application relates to sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-olate, to processes for its preparation, to its use for the treatment and/or prophylaxis of diseases and to its use for the preparation of medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.
    Type: Grant
    Filed: November 15, 2011
    Date of Patent: January 3, 2017
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Hans-Christian Militzer, Jörg Gries, Stefan Koep
  • Patent number: 9527833
    Abstract: An objective of the present invention is to obtain a stable crystal form of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride. The present invention provides a crystal of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride exhibiting characteristic peaks at angles of 11.6°, 17.2°, 17.8°, 23.3°, 27.1°, and 29.3° as a diffraction angle (2?±0.1°) in powder X-ray diffraction.
    Type: Grant
    Filed: June 17, 2014
    Date of Patent: December 27, 2016
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Hideki Kazuno, Tomonobu Mutsumi
  • Patent number: 9475799
    Abstract: The present invention relates to a novel synthetic route for the preparation of raltegravir and pharmaceutically acceptable salts, starting from 2-amino-2-methylpropanenitrile and oxadiazole carbonyl chloride, through the formation of a pyrimidinone intermediate of formula (V).
    Type: Grant
    Filed: June 28, 2016
    Date of Patent: October 25, 2016
    Assignee: Emcure Pharmaceuticals Limited
    Inventors: Mukund Keshav Gurjar, Swapnil Panditrao Sonawane, Golakchandra Sudarshan Maikap, Gulabrao Dagadu Patil, Shivnath Bhaupatil Shinde, Pankaj Shalikrao, Samit Satish Mehta
  • Patent number: 9469613
    Abstract: The present invention relates to stable novel salt forms of N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide that are suitable for the preparation of pharmaceutical formulations thereof, and their therapeutic use.
    Type: Grant
    Filed: June 11, 2015
    Date of Patent: October 18, 2016
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Brandon H. Brown, Ernest A. Carra, Jeffrey N. Hemenway, Henry Morrison, Troy Reynolds, Bing Shi, Dimitrios Stefanidis, Fang Wang, Matthew Robert Warr, James Andrew Whitney, Yan Xin
  • Patent number: 9458146
    Abstract: A crystalline sodium salt of a compound of formula I (INN: Raltegravir) or a hydrate/solvate thereof is disclosed as well as a process for obtaining the same.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: October 4, 2016
    Assignee: SANDOZ AG
    Inventors: Frtiz Blatter, Katharina Reichenbächer, Robert Ziegert, Josef Wieser, Johannes Ludescher
  • Patent number: 9439884
    Abstract: The invention features methods of treating an immune disorder characterized by elevated Pin1 marker levels in a subject by administering a retinoic acid compound. Additionally, the invention features methods of treating immune disorders (e.g., immune disorders characterized by elevated Pin1 marker levels) by administering a retinoic acid compound in combination with an anti-inflammatory, anti-viral, or anti-microbial compound.
    Type: Grant
    Filed: May 29, 2012
    Date of Patent: September 13, 2016
    Assignee: Beth Israel Deaconess Medical Center, Inc.
    Inventors: Kun Ping Lu, Adrian Tun-Kyi, Greg Finn
  • Patent number: 9428522
    Abstract: Disclosed are novel piperazine derivatives that act as agonists of the ?7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: August 30, 2016
    Assignee: The Feinstein Institute for Medical Research
    Inventors: Roger B. Clark, Daniel Elbaum
  • Patent number: 9409921
    Abstract: The present invention provides 2,4-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: April 16, 2014
    Date of Patent: August 9, 2016
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
  • Patent number: 9382213
    Abstract: Compounds of Formula I and Formula IA are inhibitors of dihydrofolate reductase and are suitable for use in compositions and methods for dihydrofolate reductase inhibition or, more specifically, treatment of a fungal infection, a bacterial infection or a protozoal infection, and, in specific embodiments, treatment of a fungal infection caused by C. albicans or C. glabrata: wherein R, R1, R2, R3, R4, A, B, E, V, W, X, Y and Z are as defined herein.
    Type: Grant
    Filed: February 12, 2015
    Date of Patent: July 5, 2016
    Assignees: PROMILIAD BIOPHARMA INC., UNIVERSITY OF CONNECTICUT
    Inventors: Dennis L Wright, Amy C Anderson, Grant Sormunen
  • Patent number: 9376398
    Abstract: The present disclosure concerns at least one entity chosen from compounds of Formula (I) and pharmaceutically acceptable salts thereof: (I) wherein the variable groups X, R1, R2, R3 m, n and p are as defined herein. The present disclosure also relates to methods for the preparation of at least one such entity, and intermediates useful in the preparation thereof, to pharmaceutical compositions containing at least one such entity, to the use of at least one such entity in the preparation of medicaments, and to the use of at least one such entity in the treatment of conditions such as, for example, allergic diseases, autoimmune diseases, viral diseases, and cancer.
    Type: Grant
    Filed: May 17, 2013
    Date of Patent: June 28, 2016
    Assignees: Sumitomo Dainippon Pharma Co., LTD, Astrazeneca Aktiebolag
    Inventors: Seiji Hori, Futoshi Hasegawa, Daisuke Urabe, Hirotaka Kurebayashi
  • Patent number: 9371380
    Abstract: This invention provides a method for predicting a therapeutic effect of chemotherapy that uses an antitumor agent comprising ?,?,?-trifluorothymidine and 5-chloro-6-(1-(2-iminopyrrolidinyl)methyl)uracil hydrochloride at a molar ratio of 1:0.5 on a colorectal cancer patient, the method comprising: (1) detecting the presence or absence of KRAS gene mutation in a biological sample obtained from the patient; and (2) predicting that the patient is likely to sufficiently respond to the chemotherapy, when KRAS gene mutation is detected in Step (1).
    Type: Grant
    Filed: August 15, 2012
    Date of Patent: June 21, 2016
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Masanobu Ito, Hiroyuki Okabe
  • Patent number: 9339486
    Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: February 2, 2015
    Date of Patent: May 17, 2016
    Assignee: The Cleveland Clinic Foundation
    Inventors: Mohamed Naquib Attala, Philippe Diaz
  • Patent number: 9321736
    Abstract: The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.
    Type: Grant
    Filed: November 7, 2014
    Date of Patent: April 26, 2016
    Assignee: Corcept Therapeutics, Inc.
    Inventors: Robin Clark, George Hynd, Nicholas Ray, Mohammad Sajad
  • Patent number: 9315507
    Abstract: The present invention relates to novel compounds as HIF-1? inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1?, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1?-mediated VEGFA expression.
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: April 19, 2016
    Assignees: Dongguk University Industry-Academic Cooperation Foundation, Korea Research Institute of Bioscience and Biotechnology
    Inventors: Kyeong Lee, Mi-Sun Won, Hwan-Mook Kim, Song-Kyu Park, Ki-Ho Lee, Chang-Woo Lee, Bo-Kyung Kim, Hyun-Seung Ban, Kyung-Sook Chung, Naik Ravi
  • Patent number: 9303028
    Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: April 5, 2016
    Assignee: AMGEN INC.
    Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Matthew R. Kaller, Qingyian Liu, Thomas T. Nguyen, Alexander J. Pickrell, Wenyuan Qian, Robert M. Rzasa, Wenge Zhong
  • Patent number: 9271962
    Abstract: Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.
    Type: Grant
    Filed: March 17, 2009
    Date of Patent: March 1, 2016
    Assignee: NORTHEASTERN UNIVERSITY
    Inventors: Alexandros Makriyannis, Lakshmipathi Pandarinathan, Nikolai Zvonok, Teija Parkkari, Lauren Chapman
  • Patent number: 9255074
    Abstract: This disclosure is directed to: (a) processes for preparing compounds and salts thereof that, inter alia, are useful for inhibiting hepatitis C virus (HCV); (b) intermediates useful for the preparation of the compounds and salts; (c) pharmaceutical compositions comprising the compounds or salts; and (d) methods of use of such compositions.
    Type: Grant
    Filed: August 21, 2012
    Date of Patent: February 9, 2016
    Assignee: AbbVie Inc.
    Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
  • Patent number: 9249124
    Abstract: Described herein are inhibitors of Aurora kinase and their use in the treatment of cancer. Methods of screening for selective inhibitors of Aurora kinases are also disclosed.
    Type: Grant
    Filed: March 30, 2012
    Date of Patent: February 2, 2016
    Assignee: H. Lee Moffitt Cancer Center and Research Institute, Inc.
    Inventors: Said M. Sebti, Ernst Schönbrunn, Nicholas J. Lawrence, Harshani R. Lawrence, Matthew P. Martin
  • Patent number: RE46284
    Abstract: The present invention relates to a method for treating a cancer comprising orally administering a composition containing ?,?,?-trifluorothymidine (FTD) and 5-chloro-6-(1-(2-iminopyrrolidinyl)methyl)uracil hydrochloride in a molar ratio of 1:0.5 at a dose of 20 to 80 mg/m2/day in terms of FTD in 2 to 4 divided portions per to patients in need of the treatment.
    Type: Grant
    Filed: December 30, 2015
    Date of Patent: January 24, 2017
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Tomohiro Emura, Akira Mita
  • Patent number: RE46757
    Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Grant
    Filed: June 30, 2015
    Date of Patent: March 20, 2018
    Assignee: Novartis AG
    Inventors: Urs Baettig, Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Glyn Alan Hughes, Darren Mark Legrand, Katrin Spiegel