Single Bond Between 3,4-positions Patents (Class 546/158)
  • Patent number: 10993938
    Abstract: Provided is a lactam compound, a tautomer, a stereoisomer, a racemate, a nonequal mixture of enantiomers, a geometric isomer, a solvate, a pharmaceutically acceptable salt thereof, or a solvate of the salt of the compound, and a pharmaceutical composition containing the compound. Also provided are the use of such compounds and their pharmaceutical compositions as drugs, especially as antiviral drugs.
    Type: Grant
    Filed: September 27, 2019
    Date of Patent: May 4, 2021
    Assignee: OCEAN UNIVERSITY OF CHINA
    Inventors: Changlun Shao, Changyun Wang, Xiaofeng Mou, Rufang Xu
  • Patent number: 9012445
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: January 12, 2013
    Date of Patent: April 21, 2015
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Publication number: 20150099779
    Abstract: The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 9, 2015
    Inventors: Anderson Gaweco, Jefferson W. Tilley, John Walker, Samantha Palmer, James Blinn
  • 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
  • Publication number: 20150079622
    Abstract: Disclosed herein are compounds, compositions, methods, and kits for detecting reactive oxygen species (ROS) by conventional fluorescence microscopy, fluorescence spectroscopy, flow cytometry, and/or high content imaging. The compounds disclosed herein are novel reduced nucleic acid binding cyanine dyes, which dyes are probes for detecting ROS and measuring oxidative stress in cells either in vitro and/or in vivo. Also described herein are processes for preparing novel reduced dyes, i.e., ROS probes, for use in the disclosed compositions, methods and kits.
    Type: Application
    Filed: February 26, 2013
    Publication date: March 19, 2015
    Inventors: Yi-Zhen Hu, Aimei Chen, Hee Chol Kang, Kyle Gee, Bhaskar Mandavilli
  • Patent number: 8957075
    Abstract: The present invention provides inhibitors of O-GIcNAc transferase. Typically, the inhibitors are quinolinone-6-sulfonamides. The invention also provides pharmaceutical compositions thereof and methods for using the same in diabetes and complications thereof, neurodegenerative diseases, cancers, autoimmune diseases, and inflammatory diseases.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: February 17, 2015
    Assignee: President and Fellows of Harvard College
    Inventors: Suzanne Walker Kahne, Michael Block Lazarus, Benjamin J. Gross
  • Publication number: 20150047073
    Abstract: The present invention provides agonist compounds that active ABA receptors, and agricultural formulations comprising the agonist compounds. The agricultural formulations are useful for inducing ABA responses in plant vegetative tissues, reducing abiotic stress in plants, and inhibiting germination of plant seeds. The compounds are also useful for inducing expression of ABA-responsive genes in cells that express endogenous or heterologous ABA receptors.
    Type: Application
    Filed: March 15, 2013
    Publication date: February 12, 2015
    Applicant: The Regents of the University of California
    Inventors: Sean R. Cutler, Masanori Okamoto
  • Patent number: 8952007
    Abstract: The present invention relates to sodium channel inhibitors of Formula I: in which R1, R2, R3, R4, R5, R6, and R7 are as defined above, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.
    Type: Grant
    Filed: December 10, 2013
    Date of Patent: February 10, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Matthew Abelman, Nancy Chu, Robert H. Jiang, Kwan Leung, Jeff Zablocki
  • Patent number: 8946446
    Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: February 3, 2015
    Assignee: Phenex Pharmaceuticals AG
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Publication number: 20150004597
    Abstract: Chemical compounds having a high selectivity for double stranded DNA over RNA and single stranded DNA are disclosed. The chemical compounds are stains that become fluorescent upon illumination and interaction with double stranded DNA, but exhibit reduced or no fluorescence in the absence of double stranded DNA. The compounds can be used in a variety of biological applications to qualitatively or quantitatively assay DNA, even in the presence of RNA.
    Type: Application
    Filed: September 17, 2014
    Publication date: January 1, 2015
    Inventors: Jolene BRADFORD, Ching-Ying CHEUNG, Shih-Jung HUANG, Patrick PINSON, Stephen YUE
  • Publication number: 20140349987
    Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: December 3, 2012
    Publication date: November 27, 2014
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Patent number: 8895535
    Abstract: Compounds of the formula I in which R1, R2, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumors.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: November 25, 2014
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Frank Zenke, Michel Calderini, Djordje Musil
  • Publication number: 20140329830
    Abstract: The present invention relates to a compound of formula (I), and to pharmaceutical compositions containing said compound and to the use of said compound in therapy, for instance in treating cognitive disorders, as well as to intermediates useful in the preparation thereof.
    Type: Application
    Filed: December 19, 2011
    Publication date: November 6, 2014
    Applicant: AstraZeneca AB
    Inventors: Helena Gybäck, Jonas Malmström, Elgaard Gitte Terp
  • Publication number: 20140315944
    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: Application
    Filed: March 11, 2014
    Publication date: October 23, 2014
    Inventors: Jillian Basinger, James Breitenbucher, Graeme Freestone, Varsha Gupta, Alan Kaplan, Chi-Ching Mak, Benjamin Pratt, Vincent Santora, Dipanjan Sengupta, Lino Valdez
  • Publication number: 20140221364
    Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.
    Type: Application
    Filed: February 5, 2014
    Publication date: August 7, 2014
    Applicant: ACADIA PHARMACEUTICALS, INC.
    Inventors: NIELS SKJAERBAEK, KRISTIAN NORUP KOCH, BO LENNART MIKAEL FRIBERG, BO-RAGNAR TOLF
  • Publication number: 20140206676
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: January 12, 2013
    Publication date: July 24, 2014
    Applicant: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Patent number: 8772493
    Abstract: The present invention relates to a compound represented by formula 1 in the present specification or a pharmaceutically acceptable thereof, which inhibits an apoptosis mechanism of auditory hair cells for various ototoxicities leading to deafness, and protects the auditory organ and hearing, a method for preparation thereof, and a composition containing the same.
    Type: Grant
    Filed: December 11, 2012
    Date of Patent: July 8, 2014
    Assignees: Ajou University Industry-Academic Cooperation Foundation, Korea Research Institute of Chemical Technology
    Inventors: Chul Ho Kim, Young Sik Jung
  • Patent number: 8765723
    Abstract: This invention relates to novel compounds which are derivatives of the phosphodiesterase inhibitor, cilostazol and pharmaceutically acceptable salts thereof. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administration of a phosphodiesterase inhibitor, such as cilostazol. The invention also relates to the use of the disclosed compounds and compositions as reagents in analytical studies involving cilostazol.
    Type: Grant
    Filed: January 7, 2013
    Date of Patent: July 1, 2014
    Assignee: CoNCERT Pharmaceuticals, Inc.
    Inventors: Rose A. Persichetti, Julie F. Liu, Craig E. Masse, Scott L. Harbeson
  • Patent number: 8722670
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: May 13, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Dalton King, Richard E. Olson, John E. Macor, Imadul Islam, Srinivasan Thangathirupathy, Jayakumar Sankara Warrier
  • Publication number: 20140128429
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3 and R4 n are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: February 13, 2013
    Publication date: May 8, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Bernd Kuhn, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Xuefei Tan
  • Publication number: 20140094460
    Abstract: The present invention relates to sodium channel inhibitors of Formula I: in which R1, R2, R3, R4, R5, R6, and R7 are as defined above, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.
    Type: Application
    Filed: December 10, 2013
    Publication date: April 3, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Matthew Abelman, Nancy Chu, Robert H. Jiang, Kwan Leung, Jeff Zablocki
  • Patent number: 8685960
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: April 1, 2014
    Assignee: Elexopharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Patent number: 8680279
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of certain neurologic disorders, including disorders related to NMDA receptor activation, neuropsychiatric disorders, neurodegenerative disorders and other neurologic diseases, disorders and related conditions. The compounds are of the Formulas I and Ia-Ij as described herein.
    Type: Grant
    Filed: June 13, 2012
    Date of Patent: March 25, 2014
    Assignee: Neurop, Inc.
    Inventors: Ruppa Poornachary Kamalesh Babu, Scott James Myers
  • Patent number: 8680115
    Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.
    Type: Grant
    Filed: May 27, 2009
    Date of Patent: March 25, 2014
    Assignee: Acadia Pharmaceuticals, Inc.
    Inventors: Niels Skjaerback, Kristian Norup Koch, Bo Lennart Mikael Friberg, Bo-Ragnar Tolf
  • Patent number: 8664379
    Abstract: The present invention relates to sodium channel inhibitors of Formula I: in which R1, R2, R3, R4, R5, R6, and R7 are as defined above, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: March 4, 2014
    Assignee: Gilead Sciences, INc.
    Inventors: Matthew Abelman, Nancy Chu, Robert H. Jiang, Kwan Leung, Jeff Zablocki
  • Patent number: 8653069
    Abstract: The present invention discloses an aralkyl substituted piperidine or piperazine derivative and the use of the derivative in preparation of medicaments for treating schizophrenia and correlative psychoneuroses. It is shown by pharmacological tests that the derivative of the present invention has better antischizophrenic effect and less toxicity. Said derivative is a free base or salt of the compound having the following general formula.
    Type: Grant
    Filed: July 28, 2008
    Date of Patent: February 18, 2014
    Assignee: Jiangsu Hengyi Pharmaceutical Co., Ltd.
    Inventors: Jianqi Li, Shaoping Peng, Wangping Cai, Kai Gao
  • Patent number: 8642618
    Abstract: The invention relates to a medicament for preventing and/or treating fatty liver which comprises as an active ingredient cilostazol or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 9, 2008
    Date of Patent: February 4, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Atsushi Nakajima, Koji Fujita, Masato Yoneda, Osamu Mukeda, Takako Ichimura
  • Patent number: 8642767
    Abstract: A process for the preparation in high yields and purity of the compound 6-(7-4(1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I) and of the pharmaceutically acceptable salts thereof is described. The process has various advantages over those previously described, in particular it avoids the use of acyl azide intermediates and their Curtius rearrangement. Novel intermediates useful for the preparation of compound (I) are also described.
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: February 4, 2014
    Assignee: EOS Ethical Oncology S.p.A. Abbreviated Form EOS S.p.A.
    Inventors: Silvano Spinelli, Valeria Livi
  • Publication number: 20130324570
    Abstract: The present invention is directed to methods, compositions and kits for treatment of cancer, e.g. heptacellular carcinoma. In some embodiments, the present invention discloses the use of a small-molecule compound of formulas (I)-(XXVI) as disclosed herein to inhibit transcription factor Late SV40 Factor (LSF) for treatment of cancer, e.g., HCC.
    Type: Application
    Filed: September 30, 2011
    Publication date: December 5, 2013
    Applicant: TRUSTEES OF BOSTON UNIVERSITY
    Inventors: Ulla Hansen, Scott Schaus, Trevor Grant, Joshua Bishop, John Kavouris, Lisa M. Christadore
  • Publication number: 20130310419
    Abstract: The present invention is related to pyrrole derivatives of formula I as the modulators of nicotinic acetylcholine receptors particularly the ?7 subtype. The invention includes pyrrole derivatives, analogues, their prodrugs, their isotopes, their metabolites, pharmaceutically acceptable salts, polymorphs, solvates, optical isomers, clathrates, co-crystals, combinations with suitable medicament and pharmaceutical compositions thereof. The present invention also includes process of preparation of the said compounds and intended use in therapy of them. Owing to the modulatory activity of the pyrrole derivatives on the nicotinic acetylcholine receptors, the invention finds application in the prophylaxis and therapy of disorders encompassing the involvement of cholinergic transmission in the central and peripheral nervous system.
    Type: Application
    Filed: January 31, 2012
    Publication date: November 21, 2013
    Applicant: LUPIN LIMITED
    Inventors: Neelima Sinha, Gourhari Jana, Navnath Popat Karche, Shridhar Keshav Adurkar, Girish Dhanraj Hatnapure, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20130296300
    Abstract: The invention provides certain quinolines and aza-quinolines of the Formula (I), and their pharmaceutically acceptable salts, wherein E, J1, Ja, Jb, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
    Type: Application
    Filed: December 19, 2011
    Publication date: November 7, 2013
    Inventors: Christopher W. Boyce, Salem Fevrier, Kevin D. McCormick, Anandan Palani, Robert G. Aslanian, Phieng Siliphaivanh, Joey L. Methot, William Colby Brown, Henry Vaccaro
  • Publication number: 20130296274
    Abstract: Compounds of the formula I in which R1, R2, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
    Type: Application
    Filed: September 14, 2011
    Publication date: November 7, 2013
    Applicant: Merck Patent GmbH
    Inventors: Timo Heinrich, Frank Zenke, Michel Calderini, Djordje Musil
  • Publication number: 20130281443
    Abstract: The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.
    Type: Application
    Filed: June 19, 2013
    Publication date: October 24, 2013
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Congxin Liang, Marcel Koenig, Yuanjun He, Par Holmberg
  • Publication number: 20130267558
    Abstract: Provided is a pharmaceutical composition for the treatment and prevention of alcoholic liver diseases, including cilostazol as an active ingredient. Cilostazol inhibits expression levels of TNF-? and FAS (fatty acid synthase) gene in a concentration-dependent manner, and also significantly inhibits the activity of caspase-3. Accordingly, cilostazol shows superior effects for the treatment or prevention of alcoholic liver diseases, in particular, alcoholic hepatitis compared to pentoxifylline which is conventionally used as a therapeutic agent for the treatment for alcoholic hepatitis. Thus, cilostazol is suitable for use as a drug for the treatment or prevention of alcoholic hepatitis.
    Type: Application
    Filed: October 7, 2011
    Publication date: October 10, 2013
    Applicant: INDUSTRY-ACADEMIC COOPERATION FOUNDATION YEUNGNAM UNIVERSITY
    Inventors: Jong-Yeon Kim, Jong-Ryul Eun, Youn-Ju Lee
  • Patent number: 8541404
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.
    Type: Grant
    Filed: November 3, 2010
    Date of Patent: September 24, 2013
    Assignee: ElexoPharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Publication number: 20130224136
    Abstract: Compounds that function, alone or in combination, as inhibitors of pigmentation for the improvement of mammalian skin are described herein. Specifically, the compounds of the present disclosure, namely chiral, non-racemic compounds, function as pigment formation inhibitors thereof to beautify skin and discourage the production of melanins. One or more products, consumer and otherwise, comprising the chiral, non-racemic compounds are disclosed herein. Methods of employing both the compounds of the present disclosure and the products incorporating the present compounds are also disclosed herein.
    Type: Application
    Filed: January 4, 2013
    Publication date: August 29, 2013
    Applicant: LASYA, INC.
    Inventor: Lasya, Inc.
  • Publication number: 20130203806
    Abstract: The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of cilostazol. Disclosed herein are several new compositions and cocrystals of cilostazol, including: a 1:1 cilostazol gentisic acid cocrystal, a 1:1:1 cilostazol gentisic acid H2O cocrystal, a 1:1 cilostazol 4-hydroxybenzoic acid cocrystal, and a 1:1 cilostazol 2,4-dihydroxybenzoic acid cocrystal. The therapeutic methods and uses of these cilostazol cocrystals are described as well as therapeutic compositions containing them.
    Type: Application
    Filed: April 28, 2011
    Publication date: August 8, 2013
    Applicant: NUFORMIX LIMITED
    Inventors: Alan Chorlton, Christopher Frampton, Daniel Gooding, Joanne Holland
  • Publication number: 20130172384
    Abstract: This invention relates to the use of triazolone and triazolethione derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones and triazolethiones in the treatment of cancer.
    Type: Application
    Filed: September 15, 2011
    Publication date: July 4, 2013
    Inventors: Nicholas D. Adams, Christopher Joseph Aquino, Jonathan M. Ghergurovich, David Lee Musso, Cynthia A. Parrish
  • Publication number: 20130143863
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, A1, A2, A3, A4, A5 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful, for example, as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.
    Type: Application
    Filed: November 29, 2012
    Publication date: June 6, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130131021
    Abstract: This invention relates to novel compounds which are derivatives of the phosphodiesterase inhibitor, cilostazol and pharmaceutically acceptable salts thereof. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administration of a phosphodiesterase inhibitor, such as cilostazol. The invention also relates to the use of the disclosed compounds and compositions as reagents in analytical studies involving cilostazol.
    Type: Application
    Filed: January 7, 2013
    Publication date: May 23, 2013
    Applicant: CONCERT PHARMACEUTICALS INC.
    Inventor: CONCERT PHARMACEUTICALS INC.
  • Publication number: 20130109672
    Abstract: Disclosed are pyruvate kinase M2 activators which are compounds of Formula (I), including those of Formula (II), wherein A1, A2, L, R, R1 to R3, X1 to X3, k, n, and m are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer. A1-NR-L-A2 (I).
    Type: Application
    Filed: April 26, 2011
    Publication date: May 2, 2013
    Applicant: The United States of America,as represented by the Secretary, Department of Health and Human Service
    Inventors: Matthew B. Boxer, Min Shen, Douglas S. Auld, Craig J. Thomas, Martin J. Walsh
  • Patent number: 8426597
    Abstract: Nitrate derivatives of cilostazol are described. They have superior properties and clinical advantages compared to cilostazol in the treatment of vascular and metabolic diseases.
    Type: Grant
    Filed: December 1, 2009
    Date of Patent: April 23, 2013
    Assignee: Cardiolynx AG
    Inventors: Dirk Sartor, Armin Scherhag
  • Publication number: 20130096122
    Abstract: The present invention relates to sodium channel inhibitors of Formula I: in which R1, R2, R3, R4, R5, R6, and R7 are as defined above, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.
    Type: Application
    Filed: December 6, 2012
    Publication date: April 18, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • Publication number: 20130085138
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Application
    Filed: September 26, 2012
    Publication date: April 4, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130079365
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1, A2 A3 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds of the present invention are useful as inhibitors of aldosterone synthase. The compounds may be used, for example, in the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.
    Type: Application
    Filed: September 14, 2012
    Publication date: March 28, 2013
    Inventors: Johannes Aebi, Kurt Amrein, Serena Maria Fantasia, Benoit Hornsperger, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Michelangelo Scalone, Xuefei Tan, Mingwei Zhou
  • Publication number: 20130072494
    Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
    Type: Application
    Filed: September 14, 2012
    Publication date: March 21, 2013
    Inventors: Hing L. SHAM, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gergely Toth
  • Publication number: 20130072679
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful for therapy or prophylaxis in a mammal, and in particular as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.
    Type: Application
    Filed: September 13, 2012
    Publication date: March 21, 2013
    Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Henner Knust, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Xuefei Tan, Mingwei Zhou
  • Patent number: 8357674
    Abstract: This invention relates to novel compounds which are derivatives of the phosphodiesterase inhibitor, cilostazol and pharmaceutically acceptable salts thereof. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administration of an phosphodiesterase inhibitor, such as cilostazol. The invention also relates to the use of the disclosed compounds and compositions as reagents in analytical studies involving cilostazol.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: January 22, 2013
    Assignee: CoNCERT Pharmaceuticals, Inc.
    Inventors: Julie F. Liu, Rose A. Persichetti
  • Patent number: 8349817
    Abstract: This invention relates to novel compounds which are derivatives of the phosphodiesterase inhibitor, cilostazol and pharmaceutically acceptable salts thereof. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administration of a phosphodiesterase inhibitor, such as cilostazol. The invention also relates to the use of the disclosed compounds and compositions as reagents in analytical studies involving cilostazol.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: January 8, 2013
    Assignee: CoNCERT Pharmaceuticals, Inc.
    Inventors: Rose A. Persichetti, Julie F. Liu, Craig E. Masse, Scott L. Harbeson
  • Publication number: 20120302543
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of certain neurologic disorders, including disorders related to NMDA receptor activation, neuropsychiatric disorders, neurodegenerative disorders and other neurologic diseases, disorders and related conditions. The compounds are of the Formulas I and Ia-Ij as described herein.
    Type: Application
    Filed: June 13, 2012
    Publication date: November 29, 2012
    Inventors: Ruppa Poornachary Kamalesh Babu, Scott James Myers