Plural Diazine Rings Patents (Class 544/295)
  • Patent number: 10844005
    Abstract: Provided is a method for preparing an N-cyclopropylmethyl aniline compound, which comprises reacting a compound represented by Formula IV with cyclopropyl formaldehyde in the presence of metal zinc and an acid to generate an N-cyclopropylmethyl aniline compound represented by Formula I. The method of the present disclosure has mild reaction conditions, short reaction time, a high yield, simple processes, simple operations and low costs, and is more applicable to industrial production.
    Type: Grant
    Filed: April 1, 2020
    Date of Patent: November 24, 2020
    Assignee: CHANG SHA JIA QIAO BIOTECH CO., LTD.
    Inventors: Liangming Luo, Chaoqun Huang, Jintao Zhu, Zheng Luo, Rong Zhang
  • Patent number: 10807985
    Abstract: Compounds and compositions useful for treating disorders related to mutant KIT are described herein.
    Type: Grant
    Filed: May 7, 2018
    Date of Patent: October 20, 2020
    Assignee: Blueprint Medicines Corporation
    Inventor: Kevin J. Wilson
  • Patent number: 10774074
    Abstract: Compounds of formula I, wherein A is an optionally substituted five-membered unsaturated heterocyclic ring containing 1, 2, or 3 N, O, or S ring heteroatom(s) exhibit alpha2C antagonistic activity and are thus useful for the treatment of diseases or conditions of the peripheric or central nervous system.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: September 15, 2020
    Assignee: ORION CORPORATION
    Inventors: Shouming Wang, Esa Kumpulainen, Jarmo Pystynen, Antti Pohjakallio, Anssi Haikarainen
  • Patent number: 10493131
    Abstract: The subject invention provides methods for recruitment of bone marrow-derived cells, including bone marrow-derived endothelial cells (BMDEC), and increasing their function by administration of relaxin. The methods of the invention can be used in, for example, treating conditions amenable to treatment by recruitment of bone marrow-derived cells, such as BMDEC and bone marrow-derived angio-osteogcnic progenitor cell.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: December 3, 2019
    Assignee: University of Florida Research Foundation, Incorporated
    Inventors: Kirk P. Conrad, Mark S. Segal
  • Patent number: 10464933
    Abstract: The present invention provides crystalline form of (R)-propylene glycol solvate of dasatinib and crystalline form of (S)-propylene glycol solvate of dasatinib.
    Type: Grant
    Filed: February 3, 2017
    Date of Patent: November 5, 2019
    Assignee: DR. REDDY'S LABORATORIES LIMITED
    Inventors: Satyanarayana Thirunahari, Anish Anil Gupta, Srividya Ramakrishnan, Sonawane Swapnil, Rakeshwar Bandichhor, Srinivasula Reddy Lakkireddy
  • Patent number: 10344027
    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: October 24, 2018
    Date of Patent: July 9, 2019
    Assignee: Inhibikase Therapeutics, Inc.
    Inventors: Milton H. Werner, Terence A. Kelly
  • Patent number: 10316031
    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: October 24, 2018
    Date of Patent: June 11, 2019
    Assignee: Inhibikase Therapeutics, Inc.
    Inventors: Milton H. Werner, Terence A. Kelly
  • Patent number: 10307420
    Abstract: The invention relates to the use of flibanserin, or a pharmaceutically acceptable acid addition salt thereof, for the treatment of disorders of sexual desire.
    Type: Grant
    Filed: September 10, 2018
    Date of Patent: June 4, 2019
    Assignee: Sprout Pharmaceuticals, Inc.
    Inventors: Franco Borsini, Kenneth Robert Evans
  • Patent number: 10239887
    Abstract: Disclosed herein are tricyclic compounds, including pyrimido[4?,5?:4,5]thieno[2,3-c]pyridazine-8-amine, pyrido[3?,2?:4,5]thieno[3,2-d]pyrimidine-4-amine, pyrazino[2?,3?:4,5]thieno[3,2-d]pyrimidin-4-amine, pyrido[3?,2?:4,5]furo[3,2-d]pyrimidin-4-amine, and pyrimido[4?,5?:4,5]furo[2,3-c]pyridazin-8-amine compounds, which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.
    Type: Grant
    Filed: June 22, 2017
    Date of Patent: March 26, 2019
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Darren W. Engers, Sean Bollinger, James C. Tarr, Paul Spearing, Julie L. Engers, Madeline Long, Thomas M. Bridges
  • Patent number: 10118923
    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: November 7, 2017
    Date of Patent: November 6, 2018
    Assignee: Inhibikase Therapeutics, Inc.
    Inventors: Milton H. Werner, Terence A. Kelly
  • Patent number: 10112945
    Abstract: The present invention relates to the compounds of formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with cancers associated with protein kinases, to their use as medicaments for use in the production of inhibition of mTor, pi3k reducing effects in warm-blooded animals such as humans.
    Type: Grant
    Filed: July 11, 2015
    Date of Patent: October 30, 2018
    Inventors: Guoqing Paul Chen, Changren Yan, Michael Reale, Monica Chen
  • Patent number: 10100027
    Abstract: Provided is a benzofuran analog having a structure represented by formula (I) and used as an NS4B inhibitor, or a pharmaceutically acceptable salt of the benzofuran analog. The benzofuran analog has anti-hepatitis C virus activity.
    Type: Grant
    Filed: September 23, 2015
    Date of Patent: October 16, 2018
    Assignees: CHANGZHOU YINSHENG PHARMACEUTICAL CO., LTD., SICHUAN UNIVERSITY
    Inventors: Yang Zhang, Zhifei Fu, Jianfei Wang, Jian Li, Shuhui Chen, Yuquan Wei, Luoting Yu, Xin Tao
  • Patent number: 9969753
    Abstract: Disclosed are compounds or pharmaceutically acceptable salts thereof having the following general formula: R-Linker-R. The compounds or pharmaceutically acceptable salts thereof provided by the present invention are used as Bcr-Abl diploid inhibitors, which can effectively inhibit the activity of tyrosine kinase, are applicable in treating diseases concerning abnormal activation of such kinases, and have good effects in treating malignant tumors. The method for preparing such inhibitors is simple and convenient, has low cost, and has good application prospects.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: May 15, 2018
    Assignee: SHENZHEN YONGZE PHARMACEUTICAL CO., LTD.
    Inventor: Zhebin Zheng
  • Patent number: 9963453
    Abstract: The invention refers to compounds of general formula (I) wherein the variables take the various meanings, pharmaceutical compositions containing them and their use in medicine, particularly in pain therapy.
    Type: Grant
    Filed: April 22, 2014
    Date of Patent: May 8, 2018
    Assignee: LABORATORIOS DEL DR. ESTEVE S.A.
    Inventors: Ramón Merce-Vidal, José-Luis Díaz-Fernández, Carmen Almansa-Rosales
  • Patent number: 9844549
    Abstract: A compound which is useful as an active ingredient for a pharmaceutical composition for treating urine storage dysfunction, voiding dysfunction, lower urinary tract dysfunction, and the like. The present inventors have found that a 2-aminothiazole derivative has an excellent muscarinic M3 receptor-positive allosteric modulator activity and is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic M3 receptor, thereby completing the present invention. 2-aminothiazole derivative or a salt thereof of the present invention is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic M3 receptor, for example voiding dysfunction such as underactive bladder.
    Type: Grant
    Filed: August 25, 2015
    Date of Patent: December 19, 2017
    Assignee: Astellas Pharma Inc.
    Inventors: Taisuke Takahashi, Hiroaki Tanaka, Michinori Akaiwa, Kenji Negoro, Hisashi Mihara, Hideyoshi Fuji, Hajime Takamatsu
  • Patent number: 9822111
    Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Q, R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent ATM kinase mediated disease, including cancer. The specification further relates to crystalline forms of compounds of imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating ATM kinase mediated disease, including cancer, using such compounds and salts.
    Type: Grant
    Filed: July 22, 2016
    Date of Patent: November 21, 2017
    Assignee: AstraZeneca AB
    Inventors: Bernard Christophe Barlaam, Kurt Gordon Pike
  • Patent number: 9802929
    Abstract: Compounds of formula (I) and its pharmaceutically acceptable salts are described wherein R1, R2, X, Y, A, B are as defined in the specification. Also disclosed are methods for preparing the compounds of formula (I) or pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the compounds of formula (I) or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: October 31, 2017
    Assignee: SHENYANG HAIWANG BIOTECHNOLOGY CO., LTD.
    Inventors: Yan Zhou, Lirong Zhang, Jie Zhou, Xin Zhou
  • Patent number: 9708285
    Abstract: A dioxolane derivative represented by formula (G1) is provided. The explanation of the substituents is given in the specification. The use of the dioxolane derivative enables the production of a liquid crystal composition and a liquid crystal display device including the liquid crystal composition.
    Type: Grant
    Filed: March 8, 2016
    Date of Patent: July 18, 2017
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Momoko Kato, Yasuhiro Niikura, Tetsuji Ishitani, Yuko Kawata
  • Patent number: 9630944
    Abstract: The invention relates to an improved process for the preparation of Imatinib and salts thereof, in particular Imatinib Mesylate, having a content of a particular genotoxic impurity, named impurity F, within the pharmacopeia limits.
    Type: Grant
    Filed: February 11, 2015
    Date of Patent: April 25, 2017
    Assignee: F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Ennio Grendele, Alberto Soldà
  • Patent number: 9603950
    Abstract: A method of synthesizing a compound of imaging agent with HDAC (histone deacetylase) inhibitor consists of two parts, the first part of the method is to provide the inhibitor of HDAC with a compound of imaging agent that includes HDAC inhibitor BNL-26 (C22H23N3O) and its analogs to be labeled with radionuclide F-18, producing a series of new nuclear medicine tracers: BNL-26-CH2CH218F, BNL-26a-CH2CH218FF, BNL-26b-CH2CH218F, BNL-26c-CH2CH218F and BNL-26d-CH2CH218F. These nuclear medicine with imaging agents can be used as a tracer in vivo binding to over-expression HDAC and produce a HDAC nuclear medicine imaging effect to serve for clinical diagnosis. The second part of the method is to provide a slightly adjusted a structural framework of BNL-26 and use pyridine to substitute the benzene ring of the BNL-26 structure, and then synthesize with other substituent to produce a series of additional 30 more HDAC inhibitors, named from Iner-1 to Iner-30 compounds.
    Type: Grant
    Filed: October 25, 2015
    Date of Patent: March 28, 2017
    Assignee: INSTITUTE OF NUCLEAR ENERGY RESEARCH
    Inventors: Ming-Hsin Li, Chyng-Yann Shiue, Han-Chih Chang, Han-Hsiang Chu
  • Patent number: 9604980
    Abstract: The present invention relates to substituted pyrimidinyl- and pyridinylpyrrolopyridinone compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular RET family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions containing these compounds.
    Type: Grant
    Filed: October 31, 2013
    Date of Patent: March 28, 2017
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Maria Menichincheri, Mauro Angiolini, Jay Aaron Bertrand, Michele Caruso, Paolo Polucci, Francesca Quartieri, Barbara Salom, Matteo Salsa, Fabio Zuccotto
  • Patent number: 9566344
    Abstract: A dasatinib and nonlinear configuration polyethylene glycol conjugate represented by formula I, wherein core is the core structure of a nonlinear configuration of polyethylene glycol, selected from a residue of pentaerythritol, methylglucoside, sucrose, diethylene glycol, propanediol, glycerol or polyglycerol removaed the hydrogen atom from the hydroxyl group; P is a polyethylene glycol residue with a number-average molecular weight of 300-60000 Da; X is selected from single bond, —CH2CO—, —CH2CH2OCO— or CH2CH2NHCO—; and i is selected from 3, 4, 6 or 8.
    Type: Grant
    Filed: December 16, 2015
    Date of Patent: February 14, 2017
    Assignee: Jenkem Technology Co., Ltd. (Tianjin)
    Inventors: Jinliang Wang, Xuan Zhao, Zhenguo Wang
  • Patent number: 9550760
    Abstract: The present invention relates generally to the use of compounds to treat a variety of disorders, diseases and pathologic conditions and more specifically to the use of substituted indol-5-ol derivatives to modulate protein kinases and for treating protein kinase-mediated diseases.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: January 24, 2017
    Assignee: NantBioScience, Inc.
    Inventor: Chunlin Tao
  • Patent number: 9540335
    Abstract: The present invention provides a salt form and compositions thereof, which are useful as an inhibitor of EGFR kinases and which exhibits desirable characteristics for the same.
    Type: Grant
    Filed: August 10, 2015
    Date of Patent: January 10, 2017
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Mei Lai, Steven Richard Witowski, Richland Wayne Tester, Kwangho Lee
  • Patent number: 9382229
    Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
    Type: Grant
    Filed: February 15, 2012
    Date of Patent: July 5, 2016
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Donald J. Zack, Cynthia Berlinicke, Laszlo Hackler, Zhiyong Yang, Joseph P. Steiner, Tomas Vojkovsky, Dana Ferraris, Barbara S. Slusher, James Inglese
  • Patent number: 9266864
    Abstract: This invention relates to compounds of the formula (I): The invention also relates to processes for the preparation of the compound of the formula (I), pharmaceutical agents or compositions containing the compound or a method of using the compound for the treatment of proliferative diseases, such as cancer, as well as the treatment of diseases ameliorated by the control and/or inhibition of lymphangiogenesis.
    Type: Grant
    Filed: August 16, 2013
    Date of Patent: February 23, 2016
    Assignee: CANCER THERAPEUTICS CRC PTY LIMITED
    Inventors: Richard Charles Foitzik, Neil Choi, Benjamin Joseph Morrow, Catherine Fae Hemley, Gillian Elizabeth Lunniss, Michelle Ang Camerino, Danny Ganame, Paul Anthony Stupple, Romina Lessene, Wilhelmus Johannes Antonius Kersten, Andrew John Harvey, Ian Peter Holmes
  • Patent number: 9238644
    Abstract: This invention relates to a compound of the formula (I): The invention also relates to processes for the preparation of the compound of the formula (I), pharmaceutical agents or compositions containing the compound or a method of using the compound for the treatment of proliferative diseases, such as cancer, as well as the treatment of diseases ameliorated by the control and/or inhibition of lymphangiogenesis.
    Type: Grant
    Filed: August 16, 2013
    Date of Patent: January 19, 2016
    Assignee: CANCER THERAPEUTICS CRC PTY LIMITED
    Inventors: Richard Charles Foitzik, Benjamin Joseph Morrow, Catherine Fae Hemley, Gillian Elizabeth Lunniss, Michelle Ang Camerino, Danny Ganame, Paul Anthony Stupple, Romina Lessene, Wilhelmus Johannes Antonius Kersten, Andrew John Harvey, Ian Peter Holmes
  • Patent number: 9233969
    Abstract: The present invention provides a novel therapeutic drug for cerebral infarction, which contains a piperazine compound as an active ingredient. The compound of the present invention can be provided as a novel therapeutic drug for cerebral infarction having an effect of suppressing brain injury volume or improving neurological deficit, since it suppresses production of plural inflammatory cytokines and chemokines present in the brain such as TNF-?, IL-1?, IL-6 and MCP-1 and the like.
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: January 12, 2016
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Haruto Nakagawa, Naoko Ando
  • Patent number: 9199944
    Abstract: Disclosed herein are a new N2,N4-bis(4-(piperazin-1-yl)phenyl)pyrimidin-2,4-diamine derivative or a pharmaceutically acceptable salt thereof and a pharmaceutical composition for the prevention or treatment of cancers containing the same as an active ingredient. The compound of the present invention has excellent inhibitory effects against the activities of anaplastic lymphoma kinase (ALK) and activated cdc42-associated kinase (ACK1) and thus can improve the therapeutic effects on the treatment of cancer cells having anaplastic lymphoma kinase fusion proteins such as EML4-ALK and NPM-ALK, and also effectively prevent the recurrence of cancers thus being useful as a pharmaceutical composition for the prevention and treatment of cancers.
    Type: Grant
    Filed: February 9, 2015
    Date of Patent: December 1, 2015
    Assignee: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Kwangho Lee, Hyoung Rae Kim, Chi Hoon Park, Chong Ock Lee, Jong Kook Lee, Hee Jung Jung, Sung Yun Cho, Chong Hak Chae, Sang Un Choi, Jae Du Ha
  • Patent number: 9120761
    Abstract: A compound of the formula (I): where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: September 1, 2015
    Assignee: Cancer Therapeutics CRC PTY LTD
    Inventors: Ian Peter Holmes, Ylva Bergman, Gillian Elizabeth Lunniss, Marica Nikac, Neil Chol, Catherine Fae Hemley, Scott Raymond Walker, Richard Charles Foitzik, Danny Ganame, Romina Lessene
  • Patent number: 9120787
    Abstract: Compounds of Formula (I) wherein B is selected from the group consisting of substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl; Y is a linker moiety selected from the group consisting of a direct bond. R, R1, R2, and R3 are each individually selected from the group consisting substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or heterocycle.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: September 1, 2015
    Assignees: Southern Research Institute, Sanford-Burnham Medical Research Institute
    Inventors: Marintha L. Heil, Nicholas D. P. Cosford, Nicholas Pagano, Peter Teriete
  • Patent number: 9115124
    Abstract: The present invention relates to a process for the synthesis of dasatinib and to intermediates useful for its preparation.
    Type: Grant
    Filed: February 26, 2015
    Date of Patent: August 25, 2015
    Assignee: CERBIOS-PHARMA SA
    Inventors: Alessandro Baruto, Mauro Gaboardi, Marta Castaldi, Graziano Castaldi
  • Patent number: 9108954
    Abstract: Synthesis process of dasatinib is disclosed, which includes the step of reacting the compound of formula I with that of formula II to obtain the compound of formula III. Also disclosed is the compound of formula III which is used as an intermediate for synthesizing dasatinib. The substituents of R1, R2, R3 or R4 in formulae I, II or III are defined as in the description.
    Type: Grant
    Filed: January 30, 2011
    Date of Patent: August 18, 2015
    Assignees: Nan Jing Cavendish Bio-Engineering Technology Co., Ltd.
    Inventors: Rong Yan, Hao Yang, Wen Hou, Yongxiang Xu
  • Patent number: 9078896
    Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: January 10, 2014
    Date of Patent: July 14, 2015
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Laurence Francoise Bernadette Marconnet-Decrane, Sandrine Francoise Dominique Gaurrand, Patrick René Angibaud
  • Patent number: 9067951
    Abstract: The present invention relates to a process for the production of novel antagonists for CCR2 (CC chemokine receptor 2) and intermediates thereof.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: June 30, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Thomas Trieselmann, Patrick Tielmann
  • Patent number: 9061028
    Abstract: The present invention relates a process for the preparation of a compound of formula (I): or a pharmaceutically acceptable salt thereof, which process comprises converting a compound of formula (IV): or a pharmaceutically acceptable salt thereof, into the compound of formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 15, 2012
    Date of Patent: June 23, 2015
    Assignee: Natco Pharma Limited
    Inventors: Amala Kompella, Adibhatla Kali Satya Bhujanga Rao, Sreenivas Rachakonda, Venugopala Krishna Gampa, Venkaiah Chowdary Nannapaneni
  • Publication number: 20150148327
    Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: June 17, 2013
    Publication date: May 28, 2015
    Applicant: Merck Canada Inc.
    Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
  • Patent number: 9040538
    Abstract: The present invention features compounds having the Formula (Ia) and (Ib) (e.g., a compound of any of Formulas ((Ia-2)-(Ia-21)), including other tautomers, stereoisomers, E/Z stereoisomers, prodrugs, pharmaceutically acceptable salts, and compositions thereof. The invention also features methods for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient by administering an effective amount of a compound of Formula (Ia) or (Ib). The invention also features a method for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient that includes administering to a patient in need thereof an effective amount of a compound of Formula (IIa) or (IIb) (e.g., a compound of any of Formulas ((IIa-2)-(IIa-6)). The compounds described herein (e.g., a compound of Formulas (Ia), (Ib), (IIa), or (IIb)) can also be used as anticonvulsants.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: May 26, 2015
    Assignee: Universite Laval
    Inventors: Giorgio Attardo, Sasmita Tripathy, Martin Gagnon
  • Patent number: 9040516
    Abstract: The present invention provides: an uracil derivative represented by general formula (I) or a physiologically acceptable salt thereof (in the formula, R1 represents a hydrogen atom, a C1-10 alkyl group, a C2-6 alkene group or a 3- to 6-membered saturated or 4- to 6-membered unsaturated aliphatic ring group which may contain 1 to 2 hetero atoms independently selected from the group consisting of N, O and S; R2 represents a hydrogen atom, a halogen atom, a cyano group, —NRcRd, —N?CHN(CH3)2, or an C1-3 alkyl group; Ar1 and Ar2 independently represent a 5- to 6-membered aromatic ring group which may contain 1 to 3 hetero atoms independently selected from the group consisting of N, O and S; and L represents a 6-membered aromatic ring group which may contain 1 to 4 nitrogen atoms, a pyrazole group, a triazole group, or an imidazole group); and a therapeutic agent or prophylactic agent for various inflammatory diseases associated with elastase, comprises the compound or the like as an active ingredient.
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: May 26, 2015
    Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.
    Inventors: Tomoya Shiro, Masanori Tobe, Katsumi Kubota, Yosuke Takanashi, Tomoaki Nakamura, Toshihiko Sone
  • Patent number: 9040542
    Abstract: The present application is directed to solid forms of compounds of formula I: and pharmaceutically acceptable salts thereof, that inhibit bacterial gyrase and/or Topo IV and pharmaceutical compositions comprising said compounds and salts. These compounds and salts are useful in treating bacterial infections.
    Type: Grant
    Filed: June 3, 2013
    Date of Patent: May 26, 2015
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Dean Shannon, Brian Luisi, Mariusz Krawiec, Anuj K. Kuldipkumar
  • Publication number: 20150141403
    Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
    Type: Application
    Filed: December 1, 2014
    Publication date: May 21, 2015
    Inventors: Jose Maria CID-NUNEZ, Daniel OEHLRICH, Andres Avelino TRABANCO-SUAREZ, Gary John TRESADERN, Juan Antonio VEGA RAMIRO, Gregor James MACDONALD
  • 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: 20150141434
    Abstract: The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: or pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein R1, R4, X, G, n, p, W1, W2, W3, W4, and the E ring are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II-XIII as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.
    Type: Application
    Filed: September 5, 2014
    Publication date: May 21, 2015
    Inventor: Jae Hyun Park
  • Publication number: 20150141396
    Abstract: The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases.
    Type: Application
    Filed: July 3, 2013
    Publication date: May 21, 2015
    Applicant: Ares Trading S.A.
    Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Patrick Gerber, Mathilde Muzerelle
  • Publication number: 20150139905
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Application
    Filed: October 9, 2014
    Publication date: May 21, 2015
    Inventors: Dinesh Chimmanamada, Weiwen Ying
  • Patent number: 9034850
    Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: May 19, 2015
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
  • Publication number: 20150133428
    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: Application
    Filed: November 14, 2014
    Publication date: May 14, 2015
    Inventors: Upender Velaparthi, Chetan Padmakar Darne, Peiying Liu, Mark D. Wittman, Bradley C. Pearce, Erika M. V. Araujo, Bireshwar Dasgupta, Jalathi Surendran Nair, Sakthi Kumaran Janakiraman, Chandrasekhar Reddy Rachamreddy, Mettu Mallikarjuna Rao, Arul Mozhi Selvan Subbiah Karuppiah, Bandreddy Subba Reddy, Pulicharla Nagalakshmi, Rajesh Onkardas Bora, Shilpa Holehatti Maheshwarappa, Selvakumar Kumaravel, Dibakar Mullick, Ramesh Sistla
  • Publication number: 20150133463
    Abstract: Provided are a multicomponent crystalline system (co-crystal), use thereof, as well as a process for obtaining the same. The said multicomponent crystalline system (co-crystal) comprises Dasatinib and a second compound selected from methyM-hydrobenzoate, nicotinamide, ethyl gallate, methyl gallate, propyl gallate, ethyl maltol, vanillin, menthol, or (1R,2S,5R)-(?)-menthol.
    Type: Application
    Filed: June 13, 2013
    Publication date: May 14, 2015
    Applicant: BASF SE
    Inventors: Tiziana Chiodo, Andreas Hafner, Tobias Hintermann, Beate Salvador, Martin Szelagiewicz, Fritz Blatter, Bernd Siebenhaar, Marcus Vossen
  • Publication number: 20150133457
    Abstract: The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the respective pathways.
    Type: Application
    Filed: July 11, 2014
    Publication date: May 14, 2015
    Inventors: Xiao XU, Xiaobo WANG, Long MAO, Li ZHAO, Biao XI
  • Publication number: 20150126504
    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: Application
    Filed: January 12, 2015
    Publication date: May 7, 2015
    Applicant: 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