A Ring Nitrogen Is Shared By The Two Cyclos Of The Bicyclo Ring System (e.g., Pyrrolo [1,2-a]pyrimidine, Imidazo[1,2-a]pyrimidine, Etc.) Patents (Class 514/259.1)
  • Patent number: 10370373
    Abstract: Imidazopyridine derivatives according to formula I are described wherein X is selected from CH, N, S, and O, Y is selected from S, CO, and O, R1 and optional R2 are independently selected from H, OH, substituted or unsubstituted C1-C6 alkyl, and substituted or unsubstituted C4-C6 cycloalkyl or cycloheteroalkyl, R3 is selected from H, OH, substituted or unsubstituted C1-C6 alkyl, and optional Z is selected from OH, NH2, NH(CO)R4, NH(SO2)R4, guanidine, alkylguanidine, and fluoroguanidine, R4 is polyethylene glycol or substituted or unsubstituted C1-C6 alkyl, and pharmaceutically acceptable salt thereof. The imidazopyridine derivatives can be used for treatment of cancer in a subject.
    Type: Grant
    Filed: March 8, 2018
    Date of Patent: August 6, 2019
    Assignee: THE CLEVELAND CLINIC FOUNDATION
    Inventors: Yogenthiran Saunthararajah, Kwok Peng Ng, James G. Phillips, Babal Kant Jha, Anand Dev Tiwari
  • Patent number: 10246415
    Abstract: A process for preparing one or more carbazoles comprising (a) contacting one or more compounds represented by formula (1) below with diboron reagents in the presence of PdCl2(dppf) to form one or more 2,2?-dichlorobiaryl represented by formula (2) below; and (b) contacting the one or more 2,2?-dichlorobiaryls with one or more H2N—Y compounds, in the presence of one or more palladium containing catalytic components; thereby forming one or more carbazoles represented by formula (3) below is provided.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: April 2, 2019
    Assignee: Dow Global Technologies LLC
    Inventors: Chunming Zhang, Arvind Jaganathan, Heqi Pan, Philip Fontaine, Jerzy Klosin
  • Patent number: 10189846
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: June 8, 2017
    Date of Patent: January 29, 2019
    Assignee: ENANTA PHARMACEUTICALS, INC.
    Inventors: Yao-Ling Qiu, Hui Cao, Xiaowen Peng, Wei Li, Jorden Kass, Xuri Gao, Meizhong Jin, Yat Sun Or
  • Patent number: 10189789
    Abstract: The present invention relates to an improved process for the preparation of carboxamide structured androgen receptor (AR) antagonists such as N—((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide (1A) and key intermediates thereof such as 2-chloro-4-(1H-pyrazol-3-yl)benzonitrile (V). AR antagonists are useful in the treatment of cancer, particularly prostate cancer and other diseases where AR antagonism is desired.
    Type: Grant
    Filed: April 8, 2016
    Date of Patent: January 29, 2019
    Assignee: Orion Corporation
    Inventors: Ilpo Laitinen, Oskari Karjalainen
  • Patent number: 10092761
    Abstract: Systems and methods for evaluating multiple candidate electrostimulation vectors for use in therapeutic cardiac stimulation are disclosed. The system can include a programmable electrostimulator circuit for delivering electrostimulation to one or more sites of a heart according to multiple candidate electrostimulation vectors. One or more physiologic sensors can detect resulting physiologic responses to the electrostimulation. A processor circuit can generate categories of indicators including therapy efficacy indicators, battery longevity indicators, or complication indicators using the sensed physiologic responses. The candidate electrostimulation vectors can be ranked according to the categories of indicators in specified orders.
    Type: Grant
    Filed: June 20, 2016
    Date of Patent: October 9, 2018
    Assignee: Cardiac Pacemakers, Inc.
    Inventors: Qi An, Yinghong Yu, Pramodsingh Hirasingh Thakur, David L. Perschbacher, Jason Humphrey, Yi Zhang
  • Patent number: 9949483
    Abstract: Compounds of formula I, wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: July 31, 2015
    Date of Patent: April 24, 2018
    Assignee: Syngenta Participations AG
    Inventors: Roger Graham Hall, Tibor Goegh, Pierre Joseph Marcel Jung, Andrew Edmunds, Andre Jeanguenat, Michel Muehlebach, Andre Stoller
  • Patent number: 9932342
    Abstract: A series of substituted imidazo[1,2-a]pyrimidine derivatives of formula (I), 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 neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: April 3, 2018
    Assignee: UCB BIOPHARMA SPRL
    Inventors: Mezher Hussein Ali, Daniel Christopher Brookings, Julien Alistair Brown, Victoria Elizabeth Jackson, Boris Kroeplien, John Robert Porter
  • Patent number: 9926316
    Abstract: Imidazopyridine derivatives according to formula I are described wherein X is selected from CH, N, S, and O, Y is selected from S, CO, and O, R1 and optional R2 are independently selected from H, OH, substituted or unsubstituted C1-C6 alkyl, and substituted or unsubstituted C4-C6 cycloalkyl or cycloheteroalkyl, R3 is selected from H, OH, substituted or unsubstituted C1-C6 alkyl, and optional Z is selected from OH, NH2, NH(CO)R4, NH(SO2)R4, guanidine, alkylguanidine, and fluoroguanidine, R4 is polyethylene glycol or substituted or unsubstituted C1-C6 alkyl, and pharmaceutically acceptable salt thereof. The imidazopyridine derivatives can be used for treatment of cancer in a subject.
    Type: Grant
    Filed: March 3, 2017
    Date of Patent: March 27, 2018
    Assignee: The Cleveland Clinic Foundation
    Inventors: Yogenthiran Saunthararajah, Kwok Peng Ng, James G. Phillips, Babal Kant Jha, Anand Dev Tiwari
  • Patent number: 9920061
    Abstract: The invention provides substituted imidazo[1,5-a]pyrimidinyl carboxamide and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted imidazo[1,5-a]pyrimidinyl carboxamide compounds described herein include substituted 2-heterocyclyl-4-alkyl-imidazo[1,5-a]pyrimidine-8-carboxamide compounds and variants thereof.
    Type: Grant
    Filed: August 16, 2017
    Date of Patent: March 20, 2018
    Assignee: Lysosomal Therapeutics Inc.
    Inventors: Renato T. Skerlj, Elyse Marie Josee Bourque, Peter T. Lansbury
  • Patent number: 9828382
    Abstract: Pyrimidone compounds defined herein exhibit human neutrophil elastase inhibitory properties and are useful for treating diseases and condition in which HNE is implicated.
    Type: Grant
    Filed: May 10, 2016
    Date of Patent: November 28, 2017
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Lilian Alcaraz, Robert Andrew Heald, Jonathan Mark Sutton, Elisabetta Armani, Carmelida Capaldi
  • Patent number: 9777000
    Abstract: It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.
    Type: Grant
    Filed: August 11, 2016
    Date of Patent: October 3, 2017
    Assignee: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro Okano, Kouki Ogawa
  • Patent number: 9422291
    Abstract: Antiviral compositions and methods are contemplated that are especially effective in the treatment and prevention of influenza A viruses. Also presented are cellular assays to identify small molecule compounds having antiviral properties, particularly as it relates to detection of influenza A RNA-dependent RNA polymerase activity in a mammalian cell independent of other influenza A components. Preferred assays allow for identification of viral replication inhibitors that do not disrupt normal cellular activity.
    Type: Grant
    Filed: December 11, 2013
    Date of Patent: August 23, 2016
    Assignee: Nant Holdings IP, LLC
    Inventors: Kayvan Niazi, Shahrooz Rabizadeh, Anne-Laure LeNy, Oleksandr Buzko, Justin Golovato, Patrick Soon-Shiong
  • Patent number: 9296706
    Abstract: The present invention relates to methods for synthesizing energetic compounds and intermediates thereof. Specifically, the present invention relates to methods for synthesizing adamantanes and intermediates that are useful in such synthesis. Synthesized intermediates are useful in the synthesis of bicyclic and tricyclic substituted adamantanes. Examples of various intermediates are: acyclic 2-nitromalonaldehyde intermediates, 2,6,9-tri-substituted-4,8-dinitro-2,6,9-triazabicyclo[3.3.1]nona-3,7-dienes and 2,6-dinitro-4,8,9,10-tetra-aza-4,8,9,10-tetra-substituted adamantanes. Intermediates synthesized according to the methods of the present invention are useful toward the synthesis of tetraaza-adamantanes, which can serve as precursors to potentially superior new high-energy-density compounds (HEDCs).
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: March 29, 2016
    Assignee: The United States of America as Represented by the Secretary of the Navy
    Inventors: Alfred G. Stern, Craig J. Diamond
  • Patent number: 9089561
    Abstract: Disclosed is an antidepressant, neuroprotectant, amyloid ? deposition inhibitor, or age retardant composition containing a heterocyclic compound having the general formula (I):
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: July 28, 2015
    Assignee: ZENYAKU KOGYO KABUSHIKI KAISHA
    Inventors: Yoshimasa Yamaguchi, Toshiyuki Matsuno, Kenichi Saitoh
  • Publication number: 20150126530
    Abstract: The present invention relates to novel substituted imidazo[1,2-a]pyrimidine compounds of formula (I), their pharmaceutically acceptable salts, and their isomers, stereoisomers, conformers, tautomers, polymorphs, hydrates and solvates. The present invention also encompasses pharmaceutically acceptable compositions of said compounds and process for preparing novel compounds. The invention further” relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals. (Formula I).
    Type: Application
    Filed: October 15, 2012
    Publication date: May 7, 2015
    Applicant: Torrent Pharmaceuticals Limited
    Inventors: Chaitanya Dutt, Vijay Chauthaiwale, Ramesh Chandra Gupta, Sameer Ghalsasi, Davinder Tuli, Shailesh Deshpande, Anita Chaudhari, Shitalkumar Zambad
  • Patent number: 9023855
    Abstract: Compounds of formula (I): are useful as inhibitors of human neutrophil elastase.
    Type: Grant
    Filed: February 11, 2014
    Date of Patent: May 5, 2015
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Toby Jonathan Blench, Christine Edwards, Robert Andrew Heald, Janusz Jozef Kulagowski, Jonathan Mark Sutton, Carmelida Capaldi
  • Patent number: 9023850
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: May 5, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Francis Pahutski, Jr.
  • Patent number: 9018219
    Abstract: The present invention provides, for example, the following compound: wherein ring A is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, X1—X2?X3 is CR5—CR6?CR7, N—CR6?CR7, CR5—N?CR7 or CR5—CR6?N, R1 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2a and R2b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R4a, R4b, R5, R6 and R7 are each independently hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid ? production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid ? proteins.
    Type: Grant
    Filed: October 27, 2011
    Date of Patent: April 28, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Moriyasu Masui, Genta Tadano
  • Publication number: 20150104384
    Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 16, 2015
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
  • Publication number: 20150105374
    Abstract: The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating and/or preventing diseases, in particular for treating and/or preventing cardiovascular diseases.
    Type: Application
    Filed: September 19, 2014
    Publication date: April 16, 2015
    Inventors: Markus FOLLMANN, Johannes-Peter STASCH, Gorden REDLICH, Nils GRIEBENOW, Dieter LANG, Frank WUNDER, Walter HÜBSCH, Niels LINDNER, Alexandros VAKALOPOULOS, Adrian TERSTEEGEN
  • Publication number: 20150094275
    Abstract: The present invention provides novel heteroaryl compounds having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.
    Type: Application
    Filed: November 13, 2014
    Publication date: April 2, 2015
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. GRAY, Jianming ZHANG, Barun OKRAM, Xianming DENG, Jae Won CHANG, Amy WOJCIECHOWSKI
  • Patent number: 8975400
    Abstract: Disclosed are 2,3-dihydroimiazo[1,2-c]pyrimidin-5(IH)-one compounds that inhibit Lp-PLA2,processes for their preparation, compositions containing them and their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: March 10, 2015
    Assignee: Glaxo Group Limited
    Inventors: Zehong Wan, Kai Long, Yingxia Sang, Xiaobo Su
  • Publication number: 20150065497
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: August 5, 2014
    Publication date: March 5, 2015
    Inventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
  • Publication number: 20150065482
    Abstract: The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Application
    Filed: August 22, 2014
    Publication date: March 5, 2015
    Applicant: GENENTECH, INC.
    Inventors: Nicole Blaquiere, Georgette Castanedo, Jianwen A. Feng, Baihua Hu, Steven Staben, Po-wai Yuen, Guosheng Wu, Jason Burch
  • Patent number: 8962627
    Abstract: The present invention provides new oxime derivatives of the general formula (I), pharmaceutical compositions containing them and their use for the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. This invention further provides new oxime derivatives of the general formula (I) consisting of modulators of nervous system receptors sensitive to glutamate, which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders. In particular embodiments, the new oxime derivatives of the invention are modulators of metabotropic glutamate receptors (mGluRs). The invention further provides positive allosteric modulators of mGluRs and more specifically positive alSosteric modulators of mGluR4.
    Type: Grant
    Filed: October 29, 2010
    Date of Patent: February 24, 2015
    Assignee: Prestwick Chemical, Inc.
    Inventors: Stephan Schann, Stanislas Mayer, Christophe Morice, Bruno Giethlen
  • Patent number: 8962596
    Abstract: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
    Type: Grant
    Filed: April 11, 2011
    Date of Patent: February 24, 2015
    Assignee: Array BioPharma Inc.
    Inventors: Laurence E. Burgess, Mark Laurence Boys, Robert D. Groneberg, Darren M. Harvey, Timothy Kercher, Christopher F. Kraser, Ellen Laird, Eugene Tarlton, Qian Zhao, Lily Huang
  • Patent number: 8957064
    Abstract: Compounds of formula (I) or an N-oxide, a salt, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer or stereoisomer, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6, R7, m and n have the meanings as given in the description and the claims, which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
    Type: Grant
    Filed: February 2, 2010
    Date of Patent: February 17, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Matthias Vennemann, Thomas Bär, Thomas Maier, Swen Hölder, Gerrit Beneke, Florian Dehmel, Armin Zülch, Andreas Strub, Stuart Ince, Hartmut Rehwinkel, Ningshu Liu, Ulf Bömer, Barbara Beckers
  • Publication number: 20150031691
    Abstract: The present invention relates to compounds represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.
    Type: Application
    Filed: October 8, 2014
    Publication date: January 29, 2015
    Inventors: Lawrence Wayne Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh B. Singh, Yajun Zheng
  • Patent number: 8921378
    Abstract: Compounds of formula (I) or (II) wherein Rx, Rz, R9, R10, R14, R14?, R15, R15?, A and B are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds possess utility as tissue-selective androgen receptor modulators (SARM) and are useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: December 30, 2014
    Assignee: Orion Corporation
    Inventors: Olli Törmäkangas, Gerd Wohlfahrt, Harri Salo, Rathna Durga Ramasubramanian, Pranab Kumar Patra, Arputharaj Ebenezer Martin, Terhi Heikkinen, Anniina Vesalainen, Anu Moilanen, Arja Karjalainen
  • Patent number: 8921336
    Abstract: The present invention provides novel heteroaryl compounds of formula (I) having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.
    Type: Grant
    Filed: November 28, 2008
    Date of Patent: December 30, 2014
    Assignees: Dana-Farber Cancer Institute, Inc., The Scripps Research Institute
    Inventors: Nathanael Gray, Jianming Zhang, Barun Okram, Xianming Deng, Jae Won Chang
  • Publication number: 20140357633
    Abstract: The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. 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 cancerous diseases.
    Type: Application
    Filed: December 12, 2012
    Publication date: December 4, 2014
    Inventors: Daniel Ford, John Robert Porter, Michael Scott Visser, Naeem Yusuff
  • Publication number: 20140343066
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
    Type: Application
    Filed: December 20, 2013
    Publication date: November 20, 2014
    Inventors: Irini Akritopoulou-Zanze, Brian D. Wakefield, Helmut Mack, Sean C. Turner, Alan F. Gasiecki, Vijaya J. Gracias, Kathy A. Sarris, Douglas M. Kalvin, Melissa J. Michmerhuizen, Qi Shuai, Jyoti R. Patel, Margaretha H.M. Bakker, Nicole Teusch, Eric F. Johnson, Peter J. Kovar, Stevan W. Djuric, Andrew J. Long, Anil Vasudevan, Dawn M. George, Lu Wang, Biqin Li, Nigel S. Moore, Adrian D. Hobson, Keith W. Woods, Julie M. Miyashiro, Steven L. Swann, Jr., Thomas D. Penning
  • Publication number: 20140336195
    Abstract: The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: May 21, 2012
    Publication date: November 13, 2014
    Inventors: Michael J. Breslin, Christopher D. Cox, Timothy J. Hartingh, Joseph Pero, Izzat T. Raheem, Michael Rossi, Laura Vassallo
  • Patent number: 8877225
    Abstract: The present invention provides a constant release copolymer composition adapted for use in a controlled release formulation for a bioactive agent, such as a formulation adapted for implantation within a patient's body tissues as a depot to release the agent over a period of time, wherein the copolymer provides a substantially constant rate of release of the bioactive agent over the time period for which the depot persists in the body tissues. The copolymer includes a PLG copolymer and a PLG oligomer of about 5-10 kDa average molecular weight, which can lack free carboxylic acid groups. When the PLG copolymer is a low burst copolymer, the constant release copolymer composition is a low burst, constant release copolymer composition adapted for implantation in the body tissues of a mammal, wherein a substantially constant rate of release of the bioactive agent is achieved.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: November 4, 2014
    Assignee: Tolmar Therapeutics, Inc.
    Inventors: Richard L. Norton, Eric Dadey
  • Publication number: 20140323464
    Abstract: Provided herein are kinase inhibiting compounds and methods of using the same.
    Type: Application
    Filed: May 16, 2012
    Publication date: October 30, 2014
    Inventors: John William Taunton, JR., Kenneth Albert Brameld, David Michael Goldstein, Jesse Mcfarland, Shyam Krishnan, Jonathan Choy
  • Patent number: 8865725
    Abstract: In one aspect, the invention relates to imidazopyrimidin-5(6H)-one analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: March 14, 2012
    Date of Patent: October 21, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Jose Manuel Bartolome-Nebreda, Gregor James MacDonald, Susana Conde-Ceide, Carrie K. Jones, Maria Luz Martin-Martin, Han Min Tong
  • Publication number: 20140309233
    Abstract: The disclosure relates to methods, compositions, and kits for treatment of parasite-mediated disease. In one embodiment, the disclosure relates to compounds, compositions, methods and kits for the treatment of malaria. In still another embodiment, the disclosure relates to a method for treating malaria comprising the use of a Syk kinase inhibitor.
    Type: Application
    Filed: December 18, 2013
    Publication date: October 16, 2014
    Applicant: HULOW, LLC
    Inventors: Philip S. Low, Francesco Michelangelo Turrini, Kristina Rose Kesely
  • Publication number: 20140303158
    Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: May 9, 2014
    Publication date: October 9, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
  • Patent number: 8853125
    Abstract: The present invention relates to a method for controlling invertebrate pests which method comprises treating the pests, their food supply, their habitat or their breeding ground or a plant, seed, soil, area, material or environment in which the pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from pest attack or infestation with a pesticidally effective amount of a pyrazole compound of formulae I or II or a salt or an N-oxide thereof, wherein A is a pyrazole radical of the formulae A1 or A2, wherein # denotes the binding; D is a 5- or 6-membered heterocyclic radical fused to the pyrazole moiety; Rp1, Rp2 and Rpx are H, halogen, CN, NO2, C1-C10-alkyl, C2-C10-alkenyl, C2-C10-alkynyl, etc.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: October 7, 2014
    Assignee: BASF SE
    Inventors: Steffen Groβ, Karsten Körber, Wolfgang von Deyn, Florian Kaiser, Ronan Le Vezouet, Sebastian Sörgel, Matthias Pohlman, Prashant Deshmukh, Joachim Dickhaut, Douglas D. Anspaugh, Deborah L. Culbertson, Faraneh Oloumi
  • Publication number: 20140294805
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
    Type: Application
    Filed: September 2, 2011
    Publication date: October 2, 2014
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Bingsong Han, Jian Lin, Dominic J. Reynolds, Bruce Roth, Chase C. Smith, Zhongguo Wang, Po-Wai Yuen, Xiaozhang Zheng
  • Publication number: 20140275119
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as Leishmaniasis, Human African Trypanosomiasis and Chagas disease.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicants: NOVARTIS AG, IRM LLC
    Inventors: Fang LIANG, Pranab Kumar MISHRA, Valentina MOLTENI, Advait Suresh NAGLE, Frantisek SUPEK, Liying Jocelyn TAN, Agnes VIDAL
  • Publication number: 20140256736
    Abstract: This invention is directed to biaryl ether sulfonamides, or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
    Type: Application
    Filed: October 30, 2012
    Publication date: September 11, 2014
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Shifeng Liu, Thilo Focken, Navjot Chahal, Zaihui Zhang, Renata Marcella Oballa, Julia Fonarev
  • Publication number: 20140235647
    Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 21, 2014
    Inventors: James Aaron Balog, Audris Huang, Upender Velaparthi, Peiying Liu
  • Patent number: 8809344
    Abstract: Various tetrahydropyrazolo[1,5-a]pyrimidine compounds, compositions, methods of making, and methods for the prevention and treatment of HCV infections and associated diseases are disclosed. The invention further relates to biomarkers for identification of HCV strains which are resistant to the tetrahydropyrazolo[1,5-a]pyrimidine compounds.
    Type: Grant
    Filed: October 29, 2009
    Date of Patent: August 19, 2014
    Assignee: Apath, LLC
    Inventors: Urszula Slomczynska, Paul Olivo, Jodi Beattie, Gale Starkey, Amine Noueiry, Robert Roth
  • Publication number: 20140228349
    Abstract: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
    Type: Application
    Filed: October 9, 2012
    Publication date: August 14, 2014
    Inventors: Mark Laurence Boys, Laurence E. Burgess, C. Todd Eary, Robert Groneberg, Bruno P. Hache, Darren Harvey, Erik James Hicken, Christopher F. Kraser, Ellen Laird, David A. Moreno, Mark C. Munson, Li Ren, John E. Robinson, Stephen T. Schlachter
  • Patent number: 8785452
    Abstract: The present invention relates to 4H-pyrido[1,2-a]pyrimidin-4-one compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.
    Type: Grant
    Filed: June 17, 2009
    Date of Patent: July 22, 2014
    Assignees: Institut National de la Sante et de la Recherche Medicale, Institut Pasteur Korea
    Inventors: Priscille Brodin, Thierry Christophe, Zaesung No, Jaeseung Kim, Auguste Genovesio, Denis Philippe Cedric Fenistein, Heekyoung Jeon, Fanny Anne Ewann, Sunhee Kang, Saeyeon Lee, Min Jung Seo, Eunjung Park, Monica Contreras Dominguez, Ji Youn Nam, Eun Hye Kim
  • Publication number: 20140194418
    Abstract: Compounds of formula (I) or pharmaceutical acceptable salts are provided, wherein X1˜X5, R1˜R3, A, B, Z and n are defined in the description. And compositions containing said compounds, and the uses for inhibitors of kinases such as ALK, and the uses for treating cancer thereof are provided.
    Type: Application
    Filed: January 20, 2012
    Publication date: July 10, 2014
    Applicant: ABBVIE INC.
    Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Fengchun Wu, Yan Shen, Cuihua Liu, Zhenguang Zou, Marina Pliushchev
  • Publication number: 20140179714
    Abstract: Compounds of formula (I): are useful as inhibitors of human neutrophil elastase.
    Type: Application
    Filed: February 11, 2014
    Publication date: June 26, 2014
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Toby Jonathan Blench, Christine Edwards, Robert Andrew Heald, Janusz Jozef Kulagowski, Jonathan Mark Sutton, Carmelida Capaldi
  • Publication number: 20140179695
    Abstract: The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases or conditions associated with and/or mediated by ?-secretase activity, hydrolysis of a ?-secretase site of a ?-amyloid precursor protein, and/or ?-amyloid protein accumulation, including a pharmaceutical composition for preventing or treating diseases including, but not limited to, Glaucoma, MCI (Mild cognitive impairment) or Alzheimer's disease, especially, Alzheimer's disease.
    Type: Application
    Filed: February 27, 2014
    Publication date: June 26, 2014
    Applicants: CoMentis, Inc., ASTELLAS PHARMA INC.
    Inventors: Ryosuke MUNAKATA, Makoto INOUE, Hiroaki TOMINAGA, Shingo YAMASAKI, Yasuhiro SHIINA, Kiyohiro SAMIZU, Hisao HAMAGUCHI, Lin HONG
  • Publication number: 20140171414
    Abstract: Compounds of formula (I) defined herein exhibit human neutrophil elastase inhibitory properties and are useful for treating diseases and conditions in which HNE is implicated.
    Type: Application
    Filed: December 17, 2013
    Publication date: June 19, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Lilian ALCARAZ, Robert Andrew Heald, Jonathan Mark Sutton, Elisabetta Armani, Carmelida Capaldi