Hetero Ring Is Four-membered And Includes At Least One Ring Nitrogen Patents (Class 514/210.01)
  • Patent number: 10287247
    Abstract: The present disclosure relates to certain novel compounds and to their utility in modulation of levels of monoamines, dopamine, norepinephrine and serotonin, in cerebral cortical areas of the mammalian brain, and more specifically for the treatment of central nervous system disorders.
    Type: Grant
    Filed: September 27, 2018
    Date of Patent: May 14, 2019
    Assignee: Integrative Research Laboratories Sweden AB
    Inventors: Fredrik Pettersson, Clas Sonesson
  • Patent number: 10221190
    Abstract: The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and a method of prevention or treatment of cancer comprising the step of administering an effective amount of the composition to a subject in need thereof.
    Type: Grant
    Filed: October 30, 2014
    Date of Patent: March 5, 2019
    Assignee: ImmunoMet Therapeutics Inc.
    Inventors: Hong Woo Kim, Ji Sun Lee, Hye Jin Heo, Hong Bum Lee, Jae Kap Jeong, Ji Hyun Park, Seo-il Kim, Young Woo Lee
  • Patent number: 10202340
    Abstract: Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.
    Type: Grant
    Filed: February 1, 2016
    Date of Patent: February 12, 2019
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Scott D. Larsen, Akira Abe, Liming Shu, Michael William Wilson, Richard F. Keep, Duxin Sun, James A. Shayman
  • Patent number: 10087142
    Abstract: The present disclosure relates to certain novel compounds of Formula (I) and to their utility in modulation of levels of monoamines, dopamine, norepinephrine and serotonin, in cerebral cortical areas of the mammalian brain, and more specifically for the treatment of central nervous system disorders.
    Type: Grant
    Filed: May 20, 2016
    Date of Patent: October 2, 2018
    Assignee: INTEGRATIVE RESEARCH LABORATORIES
    Inventors: Fredrik Pettersson, Clas Sonesson
  • Patent number: 10047095
    Abstract: The present patent application discloses at least the compounds according to Formula I? shown below, or pharmaceutically acceptable salts thereof, wherein ring D, ring A, ring E, ring F, JB, n, JD, J, o, RC1, RC2, W, JE, r, JF, s, Z1, Z2 and Z3 are as defined herein.
    Type: Grant
    Filed: September 16, 2015
    Date of Patent: August 14, 2018
    Assignee: Ironwood Pharmaceuticals, Inc.
    Inventors: Nicholas Perl, Takashi Nakai, Thomas Wai-Ho Lee, Glen Robert Rennie, Paul Allan Renhowe, Rajesh R. Iyengar
  • Patent number: 10039744
    Abstract: Provided is a medicinal composition characterized by comprising an alkyl ether derivative represented by general formula [1] [wherein: R1 and R2 are the same or different and represent a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted aryl group, etc.; R3 represents an optionally protected hydroxyl group, etc.; and m and n are the same or different and represent an integer of 1 to 6] or a salt thereof. The medicinal composition according to the present invention is useful as a post nerve injury rehabilitation effect-enhancing agent.
    Type: Grant
    Filed: January 30, 2015
    Date of Patent: August 7, 2018
    Assignee: TOYAMA CHEMICAL CO., LTD.
    Inventors: Takuya Takahashi, Tomohiro Okuda
  • Patent number: 10023559
    Abstract: The present invention relates to compounds of formula of formula I wherein R, R1. R2, R2?, R3, R4, R5, L1, L2 and N are as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric, metabolic, cardiovascular or sleep disorders with compounds of formula I.
    Type: Grant
    Filed: February 8, 2017
    Date of Patent: July 17, 2018
    Assignee: Hoffman-La Roche Inc.
    Inventors: Giuseppe Cecere, Guido Galley, Roger Norcross, Philippe Pflieger, Etienne Rauber
  • Patent number: 9981909
    Abstract: Certain biphenyic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.
    Type: Grant
    Filed: October 28, 2015
    Date of Patent: May 29, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Nicholas I. Carruthers, Wenying Chai, Jill A. Jablonowski, Chandravadan R. Shah, Brock T. Shireman, Devin M. Swanson, Vi Tran, Victoria Wong
  • Patent number: 9872852
    Abstract: Disclosed are compounds of Formula (I): (I). Also disclosed are methods of using such compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of virological diseases or disorders and cancer.
    Type: Grant
    Filed: September 2, 2014
    Date of Patent: January 23, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Louis S. Chupak, Xiaofan Zheng
  • Patent number: 9814728
    Abstract: The use of BETi as a potential treatment for FSHD is provided. Specifically, the use of BETi, and particularly selective BETi for BRD4, are shown to inhibit DUX4 expression which is expected to result in a decrease in the severity of symptoms of FSHD. Further, the treatments are shown to work when pulsed as opposed to continuous. This allows for a BETi to be supplied to a human in a pulse, and then allows the human to not need any additional treatment for a window at least as long as the one of the treatment pulse.
    Type: Grant
    Filed: September 19, 2014
    Date of Patent: November 14, 2017
    Assignee: Saint Louis University
    Inventors: Francis M. Sverdrup, Stephen J. Tapscott
  • Patent number: 9694002
    Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables RA, RAA, subscript n, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, R5, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: September 23, 2016
    Date of Patent: July 4, 2017
    Assignees: GENENTECH, INC., XENON PHARMACEUTICALS INC.
    Inventors: Jean-Christophe Andrez, Paul Robert Bichler, Chien-An Chen, Sultan Chowdhury, Shannon Marie Decker, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Jun Li, Zhiguo Liu, Daniel F. Ortwine, Brian Safina, Daniel Sutherlin, Tao Sheng, Shaoyi Sun, Andrew D. White, Michael Scott Wilson, Alla Yurevna Zenova, Jiuxiang Zhu
  • Patent number: 9617251
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R, R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
    Type: Grant
    Filed: August 1, 2016
    Date of Patent: April 11, 2017
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Stefan Peters, Holger Wagner
  • Patent number: 9539238
    Abstract: The present invention provides novel uses of a biguanide derivative for preventing or treating glioblastoma. The compound of Formula 1 and its pharmaceutically acceptable salts can be used for preventing and treating glioblastoma. Further, the combined treatment of the compound of Formula 1 and temozolomide can provide superior effects compared to the administration of the compound of Formula 1 alone or temozolomide alone.
    Type: Grant
    Filed: May 13, 2016
    Date of Patent: January 10, 2017
    Assignee: IMMUNOMET THERAPEUTICS, INC
    Inventors: Seok Gu Kang, Ji Hyun Lee, Jong Hee Chang, Jae Ho Cheong, Jun Jeong Choi, Sung Wuk Kim, Sang Hee Yoo, Hong Woo Kim, Soon Im Lee
  • Patent number: 9238027
    Abstract: Use of a CB1 receptor antagonist and/or inverse agonist, preferably rimonabant, for the preparation of drugs useful for increasing motor neuron excitability in the cerebral cortex and/or in the brain stem and/or at the spinal level, as well as a method for increasing motor neuron excitability through the administration of a CB1 antagonist/inverse agonist receptors, and to the use of a pharmaceutical composition which comprises a CB1 receptor antagonist and/or inverse agonist, preferably rimonabant, for increasing motor neuron excitability in the cerebral cortex and/or in the brain stem and/or at the spinal level.
    Type: Grant
    Filed: January 11, 2010
    Date of Patent: January 19, 2016
    Assignee: Fundacion del Hospital Nacional de Paraplejicos para la investigacion y la integracion (Fuhnpaiin)
    Inventors: Antonio Oliviero, Juan de los Reyes Aguilar Lepe, Mario Rotondi, Eduardo Molina Holgado, Luca Chiovato, Guglielmo Foffani, Laura Mordillo Mateos, Ángel Lozano Sicilia, Daniel García Ovejero, Ángel Arévalo Martín, Yolanda Pérez Borrego
  • Patent number: 9238649
    Abstract: Salts and crystalline forms of 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}-sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: January 19, 2016
    Assignee: AbbVie Inc.
    Inventors: Nathaniel Catron, Shuang Chen, Yuchuan Gong, Geoff G. Zhang
  • Patent number: 9199992
    Abstract: Provided herein is a process for the preparation of an apoptosis-inducing agent, and chemical intermediates thereof. Also provided herein are novel chemical intermediates related to the process provided herein.
    Type: Grant
    Filed: March 11, 2015
    Date of Patent: December 1, 2015
    Assignee: AbbVie Inc.
    Inventors: Vincent S. Chan, Alan C. Christesen, Timothy A. Grieme, Yi-Yin Ku, Mathew M. Mulhern, Yu-Ming M. Pu
  • Patent number: 9133105
    Abstract: The present disclosure provides novel compounds capable of functioning as transcription factor modulators, as well as compositions, pharmaceutical formulations, and kits. Also provided are methods of treating a condition regulatable by a transcription factor and/or cofactor using the compounds, compositions, pharmaceutical formulations, and kits provided herein.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: September 15, 2015
    Assignee: C&C BIOPHARMA, LLC
    Inventors: Lin Chen, Xiaojiang Chen, Yongqing Wu, Dahai Gai
  • Patent number: 9133122
    Abstract: Compounds are provided according to formula 1: where A, B, W, X?, L, R1, R3, R4b, and m? are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
    Type: Grant
    Filed: July 9, 2014
    Date of Patent: September 15, 2015
    Assignee: EVOTEC AG
    Inventors: Zhi-Liang Wei, Sumithra Gowlugari, Carl Kaub, Zhan Wang, Yeyu Cao, John Kincaid
  • Patent number: 9126948
    Abstract: The present invention provides pyrimidine-4,6-diamine derivatives of Formula (I): wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Grant
    Filed: March 23, 2012
    Date of Patent: September 8, 2015
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Andrew P. Combs, Yun-Long Li, Eddy W. Yue, Song Mei
  • Patent number: 9108984
    Abstract: The present invention provides substituted diamino-pyrimidine and substituted diamino-pyridine derivatives of Formula I; wherein X, Y, R1, R2, and Ar are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Grant
    Filed: March 13, 2012
    Date of Patent: August 18, 2015
    Assignees: Incyte Corporation, Incyte Holdings Corporation
    Inventors: Andrew P. Combs, Yun-Long Li, Song Mei, Eddy W. Yue
  • Patent number: 9079878
    Abstract: The present invention is directed to imidazole derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new imidazole NaV1.8 modulators of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description. NaV1.8 modulators are useful in the treatment of a wide range of disorders, particularly pain.
    Type: Grant
    Filed: October 15, 2012
    Date of Patent: July 14, 2015
    Assignee: Pfizer Limited
    Inventors: Sharanjeet Kaur Bagal, Mark Ian Kemp, Duncan Charles Miller, Yoshihisa Murata
  • Publication number: 20150148301
    Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.
    Type: Application
    Filed: May 23, 2013
    Publication date: May 28, 2015
    Inventors: Virginie Clement-Schatlo, Thomas Fessard, Damien Barbaras, Joana Matos, Erick Carreira
  • Publication number: 20150148318
    Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 28, 2015
    Inventors: Hoau-Yan Wang, Lindsay Burns Barbier
  • Publication number: 20150126491
    Abstract: Compounds of the formula I: or a pharmaceutical salt thereof, wherein X, Ar1, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 7, 2015
    Applicant: Genentech, Inc.
    Inventors: Monique Bodil van Niel, Andrew Cridland, Benjamin Fauber, Alberto Gobbi, Christopher Hurley, David Hurst, Jonathan Killen, Robert Maxey, Stuart Ward
  • Patent number: 9006227
    Abstract: The present invention relates to novel substituted phenoxyethylamine derivatives, useful as modulators of cortical and basal ganglia dopaminergic and N-methyl-D-aspartate (NMDA) receptor-mediated glutamatergic neurotransmission. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: April 17, 2012
    Date of Patent: April 14, 2015
    Assignee: Integrative Research Laboratories Sweden AB
    Inventors: Clas Sonesson, Jonas Karlsson, Peder Svensson
  • Patent number: 8987247
    Abstract: Disclosed are compounds, compositions and methods for treating metabolic diseases, including obesity and diabetes, and for reducing weight gain. Such compounds are represented by formula (I) as follows: wherein Y and Z are defined herein.
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: March 24, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Margery Connelly, Christopher M. Flores, Mark J. Macielag
  • Publication number: 20150080369
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 19, 2015
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • Publication number: 20150072969
    Abstract: The present invention relates to phenyl alkanoic acid derivatives (the compounds of Formula (I)); and their isotopic forms, stereoisomeric and tautomeric forms and mixtures thereof in all ratios, or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, prodrugs, polymorphs, N-oxides, S-oxides or carboxylic acid isosteres thereof. The invention also relates to processes for the preparation of compounds of Formula (I) and pharmaceutical compositions comprising one or more of the compounds of Formula (I). The said compounds and the pharmaceutical composition function as GPR (G-protein coupled receptor) agonists, particularly as GPR40 agonists, and are useful in the treatment of diseases or conditions mediated by GPR40. The present invention further relates to a method of treatment of diseases or conditions mediated by GPR40 comprising administering to a subject in need thereof a therapeutically effective amount of the compounds of Formula (I).
    Type: Application
    Filed: February 27, 2013
    Publication date: March 12, 2015
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Sanjay Kumar, Rajiv Sharma, Vishal Ashok Mahajan, Sangameshwar Prabhakar Sawargave
  • Patent number: 8975250
    Abstract: The present invention relates to 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives having Formula (I) as defined herein, their preparation and their therapeutic use.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: March 10, 2015
    Assignee: SANOFI
    Inventors: Philippe Beauverger, Guillaume Begis, Sandrine Biscarrat, Olivier Duclos, Gary McCort
  • Patent number: 8957059
    Abstract: Certain biphenyl compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.
    Type: Grant
    Filed: October 10, 2013
    Date of Patent: February 17, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Nicholas I. Carruthers, Jill A. Jablonowski, Brock T. Shireman, Vi T. Tran
  • Patent number: 8951999
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Orexo AB
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
  • Publication number: 20150038480
    Abstract: The invention provides methods of preventing, treating or ameliorating autoimmune diseases, such as diabetes and celiac disease, by decreasing the binding of MHC class II molecules to antigenic peptides or fragments of antigenic peptides of the autoimmune disease by the administration of small organic compounds. The invention also provides pharmaceutical compositions comprising the therapeutically effective small organic compounds and methods of using the same.
    Type: Application
    Filed: May 29, 2012
    Publication date: February 5, 2015
    Applicants: UNIVERSITY OF FLORIDA RESERCH FOUNDATION INCORPORTED, THE REGENTS OF THE UNIVERSITY OF COLORADO, a body corporate
    Inventors: Aaron Michels, Maki Nakayama, David Ostrov
  • Publication number: 20150025054
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: January 22, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estirate Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Lar
  • Publication number: 20140349989
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and complications associated with these diseases and disorders.
    Type: Application
    Filed: December 20, 2013
    Publication date: November 27, 2014
    Applicant: ALZHEIMER'S INSTITUTE OF AMERICA
    Inventors: Dange Vijay Kumar, Paul M. Slattum, Kraig M. Yager, Mark D. Shenderovich, Rajendra Tangallapally, Se-Ho Kim
  • Publication number: 20140349986
    Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 27, 2014
    Applicant: SANOFI
    Inventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
  • Patent number: 8889716
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: November 18, 2014
    Assignee: CHDI Foundation, Inc.
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas MacDonald, John Wityak
  • Patent number: 8877741
    Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Publication number: 20140323462
    Abstract: Provided are compounds of Formula I, R1-L1-A-L2-R2??(I), and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein A, L1, L2, R1 and R2 are defined herein. The present invention also provides a pharmaceutical composition and methods of using such compounds. The compounds are useful for therapy and/or prophylaxis in a patient, and in particular to inhibitors of Soluble Epoxide Hydrolase (sEH).
    Type: Application
    Filed: July 10, 2014
    Publication date: October 30, 2014
    Inventors: Simona M. Ceccarelli, Carine Guerot, Henner Knust
  • Publication number: 20140315877
    Abstract: The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions.
    Type: Application
    Filed: July 1, 2014
    Publication date: October 23, 2014
    Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Ronald Joseph Heemstra, Matt S. Melvin, Jason Speake, Yunde Xiao, Daniel Yohannes
  • Patent number: 8865698
    Abstract: Provided herein are methods for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal, which comprises administering to said mammal in need thereof a therapeutically effective amount of a compound of Formula I: in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification.
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: October 21, 2014
    Assignee: Array BioPharma Inc.
    Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
  • Publication number: 20140309206
    Abstract: The present invention relates to aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminoindane derivatives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 16, 2014
    Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins
  • Publication number: 20140301999
    Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.
    Type: Application
    Filed: June 23, 2014
    Publication date: October 9, 2014
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
  • Publication number: 20140288040
    Abstract: The invention provides compounds of the formula (6): or a salt, N-oxide or tautomer thereof, wherein A is CH, CF or nitrogen; E is CH, CF or nitrogen; and R0 is hydrogen or C1-2 alkyl; R1a is selected from CONH2; CO2H; an optionally substituted acyclic C1-8 hydrocarbon group; and an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1, 2, 3 or 4 are heteroatom ring members selected from O, N and S; R2 is selected from hydrogen and a group R2a; R2a is selected from an optionally substituted acyclic C1-8 hydrocarbon group; an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1 or 2 ring members are heteroatom ring members selected from O, N and S; and an optionally substituted bicyclic heterocyclic group of 9 or 10 ring members, of which 1 or 2 ring members are nitrogen atoms; wherein at least one of R1 and R2 is other than hydrogen; R3 is an optionally substituted 3- to 10-membered monocyclic or bicyc
    Type: Application
    Filed: October 31, 2012
    Publication date: September 25, 2014
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Andrew James Woodhead, Gianni Chessari, Gilbert Ebai Besong, Maria Grazia Carr, Steven Douglas Hiscock, Michael Alistair O'Brien, David Charles Rees, Susanne Maria Saalau-Bethell, Hendrika Maria Gerarda Willems, Neil Thomas Thompson
  • Publication number: 20140256702
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: March 4, 2014
    Publication date: September 11, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Erik Fenster, Melissa Fleury, Adam D. Hughes
  • Publication number: 20140256698
    Abstract: The present invention is directed to inhibitors of cathepsins and the methods for using and making such inhibitors.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 11, 2014
    Inventors: Robert Booth, Jeff Dener, Michael Green
  • Patent number: 8809315
    Abstract: Use of a monobactam antibiotic of formula (I) wherein the oxyimino group i.e. >C?N—O— has Z-orientation, or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of a bacterial infection in combination with a carbapenem antibiotic or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: August 19, 2014
    Assignee: Basilea Pharmaceutica AG
    Inventors: Eric Desarbre, Malcolm G. P. Page
  • Patent number: 8778628
    Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: July 15, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Okabe, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Publication number: 20140187533
    Abstract: The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns compounds (e.g., compounds according to any of Formulas (I)-(XIII) or Compounds (1)-(236) of Table 1) that are useful in treatment of a variety of diseases and conditions.
    Type: Application
    Filed: March 2, 2012
    Publication date: July 3, 2014
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan Pajouhesh, Richard Holland, Lingyun Zhang, Hossein Pajouhesh, Jason Lamontagne, Brendan Whelan
  • Publication number: 20140179665
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
    Type: Application
    Filed: December 9, 2013
    Publication date: June 26, 2014
    Inventors: George D. Hartman, Osvaldo A. Flores
  • Publication number: 20140179661
    Abstract: A N1-cyclic amine-N5-substituted biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.
    Type: Application
    Filed: April 8, 2012
    Publication date: June 26, 2014
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Sung Wuk Kim, Chang Hee Min, Se Hwan Park, Duck Kim, Ji Sun Lee, Yong Eun Kim, Ju Hoon Oh