The Other Cyclo In The Bicyclo Ring System Is Also Six-membered (e.g., Naphthyridines, Etc.) Patents (Class 546/122)
  • Patent number: 11192889
    Abstract: Tetrahydronaphthyridines of formula are disclosed. These compounds selectively inhibit ?V?3 without activating the ?V?3 receptor. They are useful for treating osteoporosis, acute myelogenous leukemia, sickle cell disease, focal segmental glomerulosclerosis, fibrosis, supravalvular aortic stenosis associated with Williams syndrome, tumors expressing ?V?3, tumor metastasis, bone resorption, T-cell lymphoma, retinal disease, age-related macular degeneration, diabetic retinitis, and herpes simplex virus infection. They may also be used for inhibiting tumor angiogenesis.
    Type: Grant
    Filed: July 5, 2017
    Date of Patent: December 7, 2021
    Assignee: THE ROCKEFELLER UNIVERSITY
    Inventors: Barry S. Coller, Marta Filizola, Michael Andrew Foley
  • Patent number: 11046685
    Abstract: Disclosed are small molecule inhibitors of ?v?6 integrin, and methods of using them to treat a number of diseases and conditions.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: June 29, 2021
    Assignee: Morphic Therapeutic, Inc.
    Inventors: Bryce A. Harrison, Matthew G. Bursavich, Aleksey I. Gerasyuto, Kristopher N. Hahn, Kyle D. Konze, Fu-Yang Lin, Blaise S. Lippa, Alexey A. Lugovskoy, Bruce N. Rogers, Mats A. Svensson, Dawn M. Troast
  • Patent number: 11046684
    Abstract: Provided are a compound of formula (I), a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof, use thereof as a selective inhibitor for FGFR4 kinase and use thereof in manufacturing a medicament or pharmaceutical composition for treating diseases due to FGFR4 or FGF19. The compound disclosed by the invention has selective and significant inhibitory activities against FGFR4, and has wide application prospect in the field of tumor treatment.
    Type: Grant
    Filed: December 29, 2017
    Date of Patent: June 29, 2021
    Assignee: SHANGHAI ZHEYE BIOTECHNOLOGY LIMITED LIABILITY COMPANY
    Inventors: Jianyu Liu, Haidong Zhang
  • Patent number: 11040039
    Abstract: The present disclosure provides compounds and methods of use thereof for treating inflammatory diseases or disorders.
    Type: Grant
    Filed: October 10, 2018
    Date of Patent: June 22, 2021
    Assignee: Aldeyra Therapeutics, Inc.
    Inventors: Susan Macdonald, Adna Halilovic
  • Patent number: 11040955
    Abstract: Disclosed are small molecule inhibitors of ?v?6 integrin, and methods of using them to treat a number of diseases and conditions.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: June 22, 2021
    Assignee: Morphic Therapeutic, Inc.
    Inventors: Mark Brewer, Matthew G. Bursavich, Aleksey I. Gerasyuto, Kristopher N. Hahn, Bryce A. Harrison, Kyle D. Konze, Fu-Yang Lin, Blaise S. Lippa, Alexey A. Lugovskoy, Bruce N. Rogers, Mats A. Svensson, Dawn M. Troast
  • Patent number: 11021480
    Abstract: Disclosed are small molecule inhibitors of ?v?6 integrin, and methods of using them to treat a number of diseases and conditions.
    Type: Grant
    Filed: August 24, 2020
    Date of Patent: June 1, 2021
    Assignee: Morphic Therapeutic, Inc.
    Inventors: Bryce A. Harrison, James E. Dowling, Matthew G. Bursavich, Dawn M. Troast, Blaise S. Lippa, Bruce N. Rogers, Cheng Zhong, Qi Qiao, Fu-Yang Lin, Brian Sosa, Aleksey I. Gerasyuto, Andrea Bortolato
  • Patent number: 11014922
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to ?v-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of av-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: May 25, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Pratik Devasthale, Fang Moore, Guohua Zhao, Susan Nicole Pieniazek, Kumaravel Selvakumar, Suresh Dhanusu, Manoranjan Panda, Lawrence R. Marcin
  • Patent number: 10981905
    Abstract: This invention is directed to benzenesulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy and/or epileptic seizure disorders.
    Type: Grant
    Filed: August 29, 2019
    Date of Patent: April 20, 2021
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Jean-Christophe Andrez, Kristen Nicole Burford, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Qi Jia, Verner Alexander Lofstrand, Shaoyi Sun, Steven Sigmund Wesolowski, Michael Scott Wilson, Alla Yurevna Zenova
  • Patent number: 10959995
    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, as well as acutely restoring the vascular compliance at the treatment site of the blood vessel, while maintaining luminal gain during angioplasty. Methods of treatment comprising applying the disclosed composition are also disclosed. Plaque-softening compounds are also disclosed.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: March 30, 2021
    Assignee: Alumend, LLC
    Inventors: Barbara R. Haberer, Therese J. Downey, Ronald E. Utecht
  • Patent number: 10952996
    Abstract: The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.
    Type: Grant
    Filed: December 10, 2019
    Date of Patent: March 23, 2021
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Svitlana Kulyk, Christina Owens, Steven D. E. Sullivan, Jennifer Kozak, Adam D. Hughes
  • Patent number: 10906918
    Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: February 2, 2021
    Assignee: Genentech, Inc.
    Inventors: Andreas Stumpf, Remy Angelaud, Andrew McClory, Herbert Yajima, Chudi Ndubaku, Alan Olivero
  • Patent number: 10793564
    Abstract: The invention relates to compounds of formula (A) and formula (I): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are ?v?6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
    Type: Grant
    Filed: March 7, 2019
    Date of Patent: October 6, 2020
    Assignee: PLIANT THERAPEUTICS, INC.
    Inventors: Jacob Cha, Chengguo Dong, Timothy Hom, Lan Jiang, Katerina Leftheris, Hui Li, David J. Morgans, Jr., Manuel Munoz, Maureen Reilly, Yajun Zheng
  • Patent number: 10752625
    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: February 28, 2019
    Date of Patent: August 25, 2020
    Assignee: SciFluor Life Sciences, Inc.
    Inventor: Takeru Furuya
  • Patent number: 10519154
    Abstract: The present application relates to novel 7-substituted 1-pyridylnaphthyridine-3-carboxamides, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prevention of diseases, and to their use for the production of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders and/or renal disorders.
    Type: Grant
    Filed: July 4, 2017
    Date of Patent: December 31, 2019
    Assignees: Bayer Pharma Aktiengesellschaft, Bayer Aktiengesellschaft
    Inventors: Henrik Teller, Melissa Boultadakis Arapinis, Alexandros Vakalopoulos, Anne-Sophie Rebstock, Alexander Straub, Hanna Tinel, Markus Brechmann, Matthias Beat Wittwer, Maximillian Andreas Kullmann, Klaus Münter, Thomas Mondritzki, Tobias Marquardt
  • Patent number: 10494382
    Abstract: Disclosed herein is a crystalline solvate comprising the compound of formula: methanol, N,N-dimethylformamide, and water, that is useful to prepare a crystalline form of said compound, which is an inhibitor of JAK kinases.
    Type: Grant
    Filed: August 6, 2018
    Date of Patent: December 3, 2019
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Xiaojun Huang, Venkat R. Thalladi
  • 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: 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: 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: 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: 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: 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: 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: 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