The Other Cyclo In The Bicyclo Ring System Is Also Six-membered (e.g., Naphthyridines, Etc.) Patents (Class 546/122)
  • Patent number: 10358447
    Abstract: The present invention includes novel substituted 2-N-hydroxy-1,3-dioxo-1,2,3,4-tetrahydronaphthyridines, which can be used to treat or prevent hepatitis B virus (HBV) infections in a patient. In certain embodiments, the compounds and compositions of the invention inhibit HBV RNAse H activity.
    Type: Grant
    Filed: November 29, 2018
    Date of Patent: July 23, 2019
    Assignee: Arbutus Biopharma Corporation
    Inventors: Ramesh Kakarla, Bruce D. Dorsey
  • Patent number: 10342783
    Abstract: A compound of formula (I): being 4-(3-Fluoro-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl) ethyl) pyrrolidin-1-yl)-3-(3-(2-methoxyethoxy) phenyl) butanoic acid, or a salt thereof.
    Type: Grant
    Filed: March 15, 2018
    Date of Patent: July 9, 2019
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Niall Andrew Anderson, Matthew Howard James Campbell-Crawford, Ashley Paul Hancock, John Martin Pritchard, Joanna Mary Redmond
  • Patent number: 10253025
    Abstract: The present application relates to methods of preparing a compound of formula I: or a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: March 30, 2018
    Date of Patent: April 9, 2019
    Assignee: SciFluor Life Sciences, Inc.
    Inventor: Takeru Furuya
  • Patent number: 10131635
    Abstract: Disclosed herein is a compound for use in a composition applied to a blood vessel, wherein the compound softens and/or disrupts the crystalline matrix of calcified plaque. Methods of treatment comprising applying the disclosed composition are also disclosed. Plaque-softening compounds are also disclosed.
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: November 20, 2018
    Assignee: Alumend, LLC
    Inventors: Barbara R. Haberer, Therese J. Downey, Ronald E. Utecht, Jeffrey E. Elbert
  • Patent number: 10106537
    Abstract: The present invention relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing the fluorinated compounds of the invention, and methods of treating macular degeneration, diabetic retinopathy (DR), macular edema, diabetic macular edema (DME), and macular edema following retinal vein occlusion (RVO), by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: June 27, 2017
    Date of Patent: October 23, 2018
    Assignee: SciFluor Life Sciences, Inc.
    Inventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan, D. Scott Edwards
  • Patent number: 9975892
    Abstract: The present invention relates to chemical compounds of general formula (I) which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.
    Type: Grant
    Filed: January 4, 2017
    Date of Patent: May 22, 2018
    Assignee: Bionomics Limited
    Inventors: Jonathan Bayldon Baell, Brad Sleebs, Bernard Luke Flynn, Ian Phillip Street, Nurul Quazi, Chinh Thien Bui
  • Patent number: 9956209
    Abstract: A compound of formula (I): which is 4-(3-fluoro-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)-3-(3-(2-methoxyethoxy)phenyl)butanoic acid, or a salt thereof.
    Type: Grant
    Filed: September 22, 2015
    Date of Patent: May 1, 2018
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Niall Andrew Anderson, Matthew Howard James Campbell-Crawford, Ashley Paul Hancock, John Martin Pritchard, Joanna Mary Redmond
  • Patent number: 9745282
    Abstract: This invention relates to indoline compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.
    Type: Grant
    Filed: June 30, 2016
    Date of Patent: August 29, 2017
    Assignees: Merck Sharp & Dohme Corp, ElexoPharm GmbH
    Inventors: Amjad Ali, Michael Man-Chu Lo, Edward Metzger, Lina Yin, Rolf Hartmann, Qingzhong Hu, Ralf Heim, Christina Zimmer
  • Patent number: 9717729
    Abstract: The present invention relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing the fluorinated compounds of the invention, and methods of treating macular degeneration, diabetic retinopathy (DR), macular edema, diabetic macular edema (DME), and macular edema following retinal vein occlusion (RVO), by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: November 4, 2016
    Date of Patent: August 1, 2017
    Assignee: SciFluor Life Sciences, Inc.
    Inventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan, D. Scott Edwards
  • Patent number: 9714247
    Abstract: Kinase with inhibitory activity against kinases disposed in multiple signaling pathways and their therapeutic uses.
    Type: Grant
    Filed: September 26, 2016
    Date of Patent: July 25, 2017
    Assignees: Tolero Pharmaceuticals, Inc., Mannkind Corporation
    Inventors: Qingping Zeng, Mary Faris, Alexis Mollard, Steven L. Warner, Gary A. Flynn
  • Patent number: 9701622
    Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.
    Type: Grant
    Filed: June 10, 2016
    Date of Patent: July 11, 2017
    Assignee: Achaogen, Inc.
    Inventors: Brian D. Patterson, Qing Lu, James Bradley Aggen, Paola Dozzo, Ramesh Annasaheb Kasar, Martin Sheringham Linsell, Timothy Robert Kane, Micah James Gliedt, Darin James Hildebrandt, Glenn A. McEnroe, Frederick Cohen
  • Patent number: 9675605
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, Y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting MAO, and MAO-B selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.
    Type: Grant
    Filed: September 23, 2015
    Date of Patent: June 13, 2017
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Jillian Basinger, Graeme Freestone, Varsha Gupta, Alan Kaplan, Chi Ching Mak, Benjamin Pratt, Vincent Santora, Dipanjan Sengupta, Lino Valdez
  • Patent number: 9650343
    Abstract: The present invention provides a heterocyclic compound having a ROR?t inhibitory action. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification. or a salt thereof.
    Type: Grant
    Filed: February 26, 2016
    Date of Patent: May 16, 2017
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Satoshi Yamamoto, Junya Shirai, Tsuneo Oda, Mitsunori Kono, Atsuko Ochida, Takashi Imada, Hidekazu Tokuhara, Yoshihide Tomata, Naoki Ishii, Michiko Tawada, Yoshiyuki Fukase, Tomoya Yukawa, Shoji Fukumoto
  • Patent number: 9579309
    Abstract: The present invention relates to a prophylactic or therapeutic agent for a posterior ocular disease containing the compound represented by a formula (1), its enantiomer or diastereomer, or their pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: February 28, 2017
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Atsushi Yoshida, Sae Akao, Shinji Yoneda, Komei Okabe, Tomomi Kohara
  • Patent number: 9573903
    Abstract: The present invention provides a heterocyclic compound having a ROR?t inhibitory action. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification. or a salt thereof.
    Type: Grant
    Filed: February 26, 2016
    Date of Patent: February 21, 2017
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Satoshi Yamamoto, Junya Shirai, Tsuneo Oda, Mitsunori Kono, Atsuko Ochida, Takashi Imada, Hidekazu Tokuhara, Yoshihide Tomata, Naoki Ishii, Michiko Tawada, Yoshiyuki Fukase, Tomoya Yukawa, Shoji Fukumoto
  • Patent number: 9452159
    Abstract: A method or composition including 6-aminopyridin-3-ol derivatives or pharmaceutically acceptable salts thereof for treating a disease caused by angiogenesis, the 6-aminopyridin-3-ol derivatives represented by Formula 1 or the pharmaceutically acceptable salts thereof have excellent neoangiogenesis inhibition effects in the chorioallantoic membrane model, and are suitable for use as a drug for the treatment of disease caused by angiogenesis.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: September 27, 2016
    Assignee: RESEARCH COOPERATION OF YEUNGNAM UNIVERSITY
    Inventors: Byeong Seon Jeong, Jung Ae Kim, Dong Guk Kim, You Ra Kang, Tae Gyu Nam
  • Patent number: 9365520
    Abstract: The present invention provides a heterocyclic compound having a ROR?t inhibitory action. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification. or a salt thereof.
    Type: Grant
    Filed: June 30, 2015
    Date of Patent: June 14, 2016
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Satoshi Yamamoto, Junya Shirai, Tsuneo Oda, Mitsunori Kono, Atsuko Ochida, Takashi Imada, Hidekazu Tokuhara, Yoshihide Tomata, Naoki Ishii, Michiko Tawada, Yoshiyuki Fukase, Tomoya Yukawa, Shoji Fukumoto
  • Patent number: 9315499
    Abstract: Compounds of Formula (I) wherein n, m, R1, R2, R3, R4, R5 and R6 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
    Type: Grant
    Filed: April 3, 2013
    Date of Patent: April 19, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Lee Fader, Olivier Lepage, Murray Bailey, Pierre Louis Beaulieu, Francois Bilodeau, Rebekah J. Carson, André Giroux, Cédrickx Godbout, Benoît Moreau, Julie Naud, Mathieu Parisien, Martin Poirier, Maude Poirier, Simon Surprenant, Carl Thibeault
  • Patent number: 9309241
    Abstract: The invention relates to new naphthyridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: April 12, 2016
    Assignee: ASTEX THERAPEUTICS LTD
    Inventors: Patrick Rene Angibaud, Michel Obringer, Julien Jeremie Joseph Marin, Matthieu Jeanty
  • Patent number: 9271970
    Abstract: The present disclosure relates to novel compounds, methods, and compositions capable of inhibiting HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: March 1, 2016
    Assignee: FIBROGEN, INC.
    Inventors: Danny Ng, Michael P. Arend, Lee A. Flippin
  • Patent number: 9249142
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R1d, R2a, R2b, X1, X2, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: February 2, 2016
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Patent number: 9187478
    Abstract: The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 is selected from among —O—R3 or —NR3R4, R3 is C1-6-alkyl which is substituted by R5 and R6, R5 is selected from hydrogen, branched or linear C1-6-alkyl, C2-6-alkenyl, —C1-6-alkylen-O—C1-3-alkyl, C1-3-haloalkyl, R6 is ring X wherein n is either 0 or 1, and is a either a single or a double bond and wherein A, B, D and E are each independently from one another selected from CH2, CH, C, N, NH, O or S and wherein ring X is attached to the molecule either via position A, B, D or E, wherein said ring X may optionally be further substituted by one, two or three residues each selected individually from the group consisting of -oxo, hydroxy, —C1-3-alkyl, —C1-3-haloalkyl, —O—C1-3-alkyl, —C1-3-alkanol and halogen, and wherein R4, R2, R7, R8, R9, R10, R11 and Q may have the meanings as given in claim 1, as well a
    Type: Grant
    Filed: January 8, 2015
    Date of Patent: November 17, 2015
    Assignee: Boehringer Ingellheim International GmbH
    Inventors: Matthias Hoffmann, Georg Dahmann, Dennis Fiegen, Sandra Handschuh, Jasna Klicic, Guenter Linz, Gerhard Schaenzle, Andreas Schnapp, Stephen Peter East, Michael Philip Mazanetz, Robert John Scott, Edward Walker
  • Patent number: 9067940
    Abstract: The invention relates to novel alicyclic N,N?-substituted diazabicyclo[3.3.1]nonane derivatives of general formula (I) which act as allosteric AMPA receptor modulators, and to drugs based thereon which can be used for treating Alzheimer's, Parkinson's and other neurodegenerative diseases.
    Type: Grant
    Filed: April 10, 2012
    Date of Patent: June 30, 2015
    Inventors: Maxim Eduardovich Zapolsky, Nikolay Serafimovich Zefirov, Vladimir Alexandrovich Palyulin, Mstislav Igorevich Lavrov
  • Publication number: 20150144846
    Abstract: The invention relates to novel compounds containing one or more units derived from 1,5-disubstituted-1,5-dihydro-[1,5]naphthyridine-2,6-dione, to methods for their preparation and educts or intermediates used therein, to mixtures and formulations containing them, to the use of the compounds, mixtures and formulations as organic semiconductors in organic electronic (OE) devices, especially in organic photovoltaic (OPV) devices and organic photodetectors (OPD), and to OE, OPV and OPD devices comprising these compounds, mixtures or formulations.
    Type: Application
    Filed: May 6, 2013
    Publication date: May 28, 2015
    Applicant: MERCK PATENT GmbH
    Inventors: Lana Nanson, Nicolas Blouin, William Mitchell, Steven Tierney, Toby Cull
  • Patent number: 9040515
    Abstract: This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: May 26, 2015
    Assignee: Pfizer Inc.
    Inventors: Martin Paul Edwards, Robert Arnold Kumpf, Pei-Pei Kung, Indrawan James McAlpine, Sacha Ninkovic, Eugene Yuanjin Rui, Scott Channing Sutton, John Howard Tatlock, Martin James Wythes, Luke Raymond Zehnder
  • Publication number: 20150141423
    Abstract: Disclosed are pesticidally active pyridyl- and pyrimidyl-substituted thiazole derivatives, processes for their preparation, compositions comprising those compounds, and their use for controlling insects.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 21, 2015
    Applicant: Syngenta Participations AG
    Inventors: Ruifang Chen, Laura Quaranta, Andrew Edmunds, Andre Jeanguenat, Aurelien Bigot, Sebastian Rendler, Roger Graham Hall, Long Lu, Peter Renold
  • Publication number: 20150133437
    Abstract: The invention provides tetrahydro[1,8]naphthyridine and related compounds, methods of promoting RORy activity and/or increasing the amount of iL-17 in a subject, and therapeutic uses of the tetrahydro[1,8]naphthyridine and related compounds. In particular, the invention provides sulfonamide-tetrahydro[1,8]naphthyridine and related compounds, methods of using such compounds to promote RORy activity and/or increase the amount of iL-17 in a subject, and treat medical conditions in which activation of immune response would be beneficial such as in cancer and infections.
    Type: Application
    Filed: May 8, 2013
    Publication date: May 14, 2015
    Inventors: Thomas D. Aicher, Peter L. Toogood, Xiao Hu
  • Publication number: 20150126503
    Abstract: The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 is selected from among —O—R3 or —NR3R4, R3 is C1-6-alkyl which is substituted by R5 and R6, R5 is selected from hydrogen, branched or linear C1-6-alkyl, C2-6-alkenyl, —C1-6-alkylen-O—C1-3-alkyl, C1-3-haloalkyl, R6 is ring X wherein n is either 0 or 1, and is a either a single or a double bond and wherein A, B, D and E are each independently from one another selected from CH2, CH, C, N, NH, O or S and wherein ring X is attached to the molecule either via position A, B, D or E, wherein said ring X may optionally be further substituted by one, two or three residues each selected individually from the group consisting of -oxo, hydroxy, —C1-3-alkyl, —C1-3-haloalkyl, —O—C1-3-alkyl, —C1-3-alkanol and halogen, and wherein R4, R2, R7, R8, R9, R10, R11 and Q may have the meanings as given in claim 1, as well as pha
    Type: Application
    Filed: January 8, 2015
    Publication date: May 7, 2015
    Inventors: Matthias HOFFMANN, Georg DAHMANN, Dennis FIEGEN, Sandra HANDSCHUH, Jasna KLICIC, Guenter LINZ, Gerhard SCHAENZLE, Andreas SCHNAPP, Stephen Peter EAST, Michael Philip MAZANETZ, Robert John SCOTT, Edward Walker
  • Publication number: 20150126506
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: January 8, 2015
    Publication date: May 7, 2015
    Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
  • Publication number: 20150119405
    Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
    Type: Application
    Filed: October 23, 2014
    Publication date: April 30, 2015
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Neil Bifulco, Jr., Lucian V. DiPietro, Brian L. Hodous, Chandrasekhar V. Miduturu
  • Publication number: 20150119387
    Abstract: The present invention relates to a compound having the structure of Formula I as inhibitor of WNT signal transduction pathways, as well as a composition comprising the compound. Further, the present invention relates to the use of the compound and the method of inhibiting the WNT signal transduction pathways.
    Type: Application
    Filed: June 15, 2012
    Publication date: April 30, 2015
    Applicant: Curegenix Inc.
    Inventor: Songzhou An
  • Publication number: 20150119385
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.
    Type: Application
    Filed: October 24, 2014
    Publication date: April 30, 2015
    Applicant: Novartis AG
    Inventors: Nicole Buschmann, Robin Alec Fairhurst, Pascal Furet, Thomas Knöpfel, Catherine Leblanc, Lv Liao, Robert Mah, Pierre Nimsgern, Sebastien Ripoche, Jing Xiong, Bo Han, Can Wang, Xianglin Zhao
  • Publication number: 20150111877
    Abstract: The invention provides tetrahydronaphthyridine and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydronaphthyridine and related compounds.
    Type: Application
    Filed: May 7, 2013
    Publication date: April 23, 2015
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Blair T. Lapointe, Valdimir Simov, Karin A. Stein, William D. Thomas, Peter L. Toogood, Chad A. Van Huis, Catherine M. White
  • Publication number: 20150111874
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 23, 2015
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Martin R. TREMBLAY
  • Publication number: 20150112071
    Abstract: The present invention relates to synthetic processes for preparation of aminotetralin compounds with kinase inhibitory activity. The invention also provides synthetic intermediates useful in the processes of the invention.
    Type: Application
    Filed: May 29, 2014
    Publication date: April 23, 2015
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Alexandra E. Gould, Sean J. Harrison, Hirotake Mizutani, Ming Shen, Thomas E. Smyser, Stephen G. Stroud
  • Publication number: 20150111750
    Abstract: N-(tetrazol-5-yl)- and N-(triazol-5-yl)hetarylcarboxamides of formula I and their use as herbicides. The invention relates to N-(tetrazol-5-yl)- and N-(triazol-5-yl)hetarylcarboxamides of formula I and their use as herbicides. In said formula I, B represents N or CH, whereas X1 is N or CR1, X2 is N or CR2, X3 is N or CR3 and X4 is N or CR4; provided that a least one of X1, X3 and X4 is N; R, R1, R2, R3, R4 and R5 represent groups such as hydrogen, halogen or organic groups such as alkyl or phenyl.
    Type: Application
    Filed: April 16, 2013
    Publication date: April 23, 2015
    Inventors: Helmut Kraus, Matthias Witschel, Thomas Seitz, Trevor William Newton, Liliana Parra Rapado, Klaus Kreuz, Johannes Hutzler, Maciej Pasternak, Jens Lerchl, Richard Roger Evans
  • Patent number: 9012443
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: April 21, 2015
    Assignee: Amgen Inc.
    Inventors: Christiane Boezio, Howard Bregman, James R. Coats, Erin F. Dimauro, Thomas Dineen, Bingfan Du, Russell Graceffa, Charles Kreiman, Daniel La, Isaac E. Marx, Nagasree Chakka, Hanh Nho Nguyen, Emily Anne Peterson, Matthew Weiss, Katrina W. Copeland, Holly L. Deak, Alessandro Boezio
  • Patent number: 9012634
    Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the Fab1 enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: April 21, 2015
    Assignee: Janssen R&D Ireland
    Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans
  • Publication number: 20150105367
    Abstract: This invention provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I); and use of a compound of Formula (I) for treating specified cancers.
    Type: Application
    Filed: March 5, 2013
    Publication date: April 16, 2015
    Inventors: Daniel L. Flynn, Michael D, Kaufman, Lakshminarayana Vogeti, Scott Wise, Wei-Ping Lu, Bryan Smith, Timothy Malcolm Caldwell, William C. Patt, James R. Henry, Philip A. Hipskind, Sheng-Bin Peng
  • Publication number: 20150105418
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R1d, R2a, R2b, X1, X2, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Patent number: 9006265
    Abstract: The use of substituted fused pyrimidinones and dihydropyrimidinones of the formula (I) or salts thereof where the radicals of the formula (I) are each as defined in the description, for enhancing stress tolerance in plants to abiotic stress, and for invigorating plant growth and/or for increasing plant yield.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: April 14, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Jens Frackenpohl, Hans-Joachim Zeiβ, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döring, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills, Monika H. Schmitt
  • Publication number: 20150087840
    Abstract: The invention relates to a new process suitable for manufacturing the compounds of formula I (I) wherein W is H, Br, Cl or methyl, which are synthetic intermediates useful in the preparation of antibiotic compounds.
    Type: Application
    Filed: April 26, 2013
    Publication date: March 26, 2015
    Inventors: Stefan Abele, Hans Meier, Gunther Schmidt, Heinz Steiner
  • Patent number: 8987250
    Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: March 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
  • Patent number: 8987455
    Abstract: The present invention relates to a method of controlling plants or inhibiting plant growth which comprises applying to the plants or to the locus thereof a herbicidally effective amount of a compound of formula (I) wherein A1, A2, A3, A4, R3, R4 and R5 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to intermediates used in the preparation of compounds of formula (I), to herbicidal compositions comprising compounds of formula (I) and to certain novel pyridopyridines, pyridodiazines and pyridotriazines.
    Type: Grant
    Filed: September 6, 2013
    Date of Patent: March 24, 2015
    Assignee: Syngenta Limited
    Inventors: Matthew Robert Cordingley, Michael Drysdale Turnbull, Nigel James Willetts, Patrick Jelf Crowley
  • Publication number: 20150080413
    Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Inventors: Jerome Emile Georges Guillemont, David Francis Alain Lancois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
  • Publication number: 20150072974
    Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.
    Type: Application
    Filed: May 9, 2013
    Publication date: March 12, 2015
    Inventors: Phillip G. Jones, Robert Lew, Kerry L. Spear, Linghong Xie
  • Patent number: 8975261
    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: Grant
    Filed: May 21, 2012
    Date of Patent: March 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Christopher D. Cox, Timothy J. Hartingh, Joseph Pero, Izzat T. Raheem, Michael Rossi, Laura Vassallo
  • Publication number: 20150065468
    Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.
    Type: Application
    Filed: August 29, 2014
    Publication date: March 5, 2015
    Inventors: Mark W. HOLLADAY, Gang LIU, Martin W. ROWBOTTON
  • Patent number: 8969568
    Abstract: The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 is selected from among —O—R3 or —NR3R4, R3 is C1-6-alkyl which is substituted by R5 and R6, R5 is selected from hydrogen, branched or linear C1-6-alkyl, C2-6-alkenyl, —C1-6-alkylen-O—C1-3-alkyl, C1-3-haloalkyl, R6 is ring X wherein n is either 0 or 1, and is a either a single or a double bond and wherein A, B, D and E are each independently from one another selected from CH2, CH, C, N, NH, O or S and wherein ring X is attached to the molecule either via position A, B, D or E, wherein said ring X may optionally be further substituted by one, two or three residues each selected individually from the group consisting of -oxo, hydroxy, —C1-3-alkyl, —C1-3-haloalkyl, —O—C1-3-alkyl, —C1-3-alkanol and halogen, and wherein R4, R2, R7, R8, R9, R10, R11 and Q may have the meanings as given in claim 1, as wel
    Type: Grant
    Filed: January 26, 2011
    Date of Patent: March 3, 2015
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Matthias Hoffmann, Georg Dahmann, Dennis Fiegen, Sandra Handschuh, Jasna Klicic, Guenter Linz, Gerhard Schaenzle, Andreas Schnapp, Stephen Peter East, Michael Philip Mazanetz, Robert John Scott, Edward Walker
  • Publication number: 20150057293
    Abstract: The invention relates to new naphthyridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: October 26, 2012
    Publication date: February 26, 2015
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Patrick Rene Angibaud, Michel Obringer, Julien Jeremie Joseph Marin, Matthieu Jeanty