Carbocyclic Ring Bonded Directly At 2-position Patents (Class 544/289)
  • Patent number: 9006251
    Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
    Type: Grant
    Filed: June 24, 2014
    Date of Patent: April 14, 2015
    Assignee: Janssen Pharamceutica NV
    Inventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
  • Publication number: 20140301944
    Abstract: Disclosed are oxo-hydroquinazolines that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.
    Type: Application
    Filed: April 2, 2014
    Publication date: October 9, 2014
    Applicants: Forschungsverbund Berlin E.V., The United States of America, as represented by the Secretary, Department of Health and Human Serv
    Inventors: Marvin C. Gershengorn, Susanne Neumann, Bruce M. Raaka, Craig J. Thomas, James Inglese, Noel T. Southall, Steven Titus, Wenwei Huang, Gerd Krause, Gunnar Kleinau, Wei Zheng
  • Publication number: 20140234887
    Abstract: The invention relates to novel peptidase substrates of formula (I): wherein R0, R1, R2, R3, R4, R5 and n are as defined in claim 1, and a method for detecting the presence of a catalytically active peptidase, by means of one of these substrates.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 21, 2014
    Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTFIQUE
    Inventors: Jens Hasserodt, Oliver Thorn-Seshold
  • Patent number: 8809354
    Abstract: Surprising antiviral activity of 3-amino-2-(4-nitrophenyl)-4-(3H)-quinazolinone (Compound 1) was reported in the treatment or prevention of viral infections, particularly in combination with other antiviral agents such as interferon and/or ribavarin.
    Type: Grant
    Filed: December 31, 2011
    Date of Patent: August 19, 2014
    Inventors: Sheikh Riazuddin, Osman Ali, Usman Ashfaq, Shaheen N. Khan, Javed Akram, Atta-ur Rahman, M. Iqbal Choudhary, Khalid M. Khan, Zulfiqar Ali Khan
  • Publication number: 20140142102
    Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Application
    Filed: November 20, 2013
    Publication date: May 22, 2014
    Applicant: RVX Therapeutics Inc.
    Inventors: David John Fairfax, Bryan Cordell Duffy, Gregory Scott Martin, John Frederick Quinn, Shuang Liu, Gregory Steven Wagner, Peter Ronald Young
  • Publication number: 20140140956
    Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Application
    Filed: November 20, 2013
    Publication date: May 22, 2014
    Applicant: RVX Therapeutics Inc.
    Inventors: David John Fairfax, Gregory Scott Martin, John Frederick Quinn, Bryan Cordell Duffy, Gregory Steven Wagner, Peter Ronald Young
  • Patent number: 8642610
    Abstract: The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53.
    Type: Grant
    Filed: February 6, 2012
    Date of Patent: February 4, 2014
    Assignee: University of Virginia Patent Foundation
    Inventor: Milton L. Brown
  • Publication number: 20140018363
    Abstract: Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: wherein Ar represents R5, R7, R8, R2?, R4?, R5?, R6?, R7?, R8? independently represent H, OH, F, Cl, Br, methoxyl group, NH2 group or NMe2 group; X represents NH, O or S; and R6 is selected from the group consisting of: pyrrolidinyl group, piperidinyl group, morpholino group, methoxyl group, and dimethylamine group. The present invention also provides a composition comprising the compound of formula I. The compound and the composition in accordance with the present invention are effective on treating or alleviating a disease or disorder, such as malignant glioma.
    Type: Application
    Filed: July 30, 2013
    Publication date: January 16, 2014
    Applicant: China Medical University
    Inventors: Mann-Jen Hour, Po-Wu Gean, Sheng-Chu Kuo, Hong-Zin Lee, Jai-Sing Yang, Li-Chen Chou, Tai-Lin Chen
  • Publication number: 20130336887
    Abstract: The invention provides methods and compositions, e.g., for tumor imaging and therapy.
    Type: Application
    Filed: March 11, 2013
    Publication date: December 19, 2013
    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventor: President and Fellows of Harvard College
  • Publication number: 20130310376
    Abstract: Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: wherein Ar represents R5, R7, R8, R2?, R3?, R4?, R5?, R6?, R7?, R8? independently represent H, OH, F, Cl, Br methoxyl group, NH2 group or NMe2 group; X represents NH, O or S; R6 is selected from the group consisting of: piperidinyl group, morpholino group, methoxyl group, and dimethylamine group. The present invention also provides a composition comprising the compound of formula I. The compound and the composition in accordance with the present invention are effective on treating or alleviating a disease or disorder, such as malignant glioma.
    Type: Application
    Filed: July 30, 2013
    Publication date: November 21, 2013
    Applicant: China Medical University
    Inventors: Mann-Jen Hour, Po-Wu Gean, Sheng-Chu Kuo, Hong-Zin Lee, Jai-Sing Yang, Li-Chen Chou, Tai-Lin Chen
  • Publication number: 20130303551
    Abstract: This invention relates to the use of pyrimidinone 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 pyrimidinones in the treatment of cancer.
    Type: Application
    Filed: January 10, 2012
    Publication date: November 14, 2013
    Inventors: Nicholas D. Adams, Alexander Joseph Reif, Kenneth Wiggall
  • Publication number: 20130251631
    Abstract: Disclosed are oxo-hydroquinazolines that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.
    Type: Application
    Filed: May 17, 2013
    Publication date: September 26, 2013
    Applicants: Forschungsverbund Berlin E.V., The Government of the United States of America as represented by the Secretary of the Department of
    Inventors: Marvin C. Gershengorn, Susanne Neumann, Bruce M. Raaka, Craig J. Thomas, James Inglese, Noel T. Southall, Steven Titus, Wei Zheng, Wenwei Huang, Gerd Krause, Gunnar Kleinau
  • Publication number: 20130102602
    Abstract: Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: wherein Ar represents R5, R6, R7, R8, R1?, R2?, R3?, R4?, R5?, R6?, R7?, R8? independently represent H, OH, F, Cl, Br, C1 to C6 alkyl group, C1 to C6 alkoxy group, C2 to C6 alkenyl group, C2 to C6 alkenoxy group, C2 to C6 alkynyl group, C2 to C6 alkynoxy group, amine group, mono- or di-substituted amino group, cyclic C1 to C5 alkylamino group, imidazolyl group, morpholino group, piperazinyl group, optionally substituted with one or more hydroxy or halo; and X represents NH, O or S. The present invention also provides a composition comprising the compound of formula I. The compound and the composition in accordance with the present invention are effective on treating or alleviating a disease or disorder, such as malignant glioma.
    Type: Application
    Filed: October 20, 2011
    Publication date: April 25, 2013
    Applicant: China Medical University
    Inventors: Mann-Jen Hour, Po-Wu Gean, Sheng-Chu Kuo, Hong-Zin Lee, Jai-Sing Yang, Li-Chen Chou, Tai-Lin Chen
  • Patent number: 8394953
    Abstract: The invention provides methods and compositions, e.g., for tumor imaging and therapy.
    Type: Grant
    Filed: June 1, 2009
    Date of Patent: March 12, 2013
    Assignee: President and Fellows of Harvard College
    Inventor: Amin I. Kassis
  • Publication number: 20120315217
    Abstract: TSHR inverse agonists and neutral antagonists that are useful for treating Graves' orbitopathy, Graves' hyperthyroidism and/or thyroid cancer.
    Type: Application
    Filed: April 8, 2011
    Publication date: December 13, 2012
    Inventors: Marvin Gershengorn, Susanne Neumann, Wenwei Huang, Craig J. Thomas
  • Patent number: 8329713
    Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.
    Type: Grant
    Filed: April 9, 2010
    Date of Patent: December 11, 2012
    Assignee: Icagen Inc.
    Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato, James Barnwell Thomas, Jr.
  • Publication number: 20120288884
    Abstract: The present invention relates to a compound of the general formula (I) useful in the determining the presence, amount or activity of an enzyme in living cells, a method of preparing said compounds and a kit thereof.
    Type: Application
    Filed: July 28, 2011
    Publication date: November 15, 2012
    Applicant: NANYANG TECHNOLOGICAL UNIVERSITY
    Inventors: Bengang Xing, Junxin Aw, Qing Shao, Yanmei Yang, Tingting Jiang, Chungyen Ang
  • Publication number: 20120283439
    Abstract: The present invention provides a compound of general formulae 3a-i to 6a-i, 7a-i to 10a-i, 12a-i to 15a-i, 16a-i to 19a-i, 21a-i to 24a-i, 25a-i to 28a-i, 30a-i to 33a-i, 34a-i to 37a-i and 39a-i to 42a-i, 43a-i to 46a-i useful as potential antitumour agents against human cancer cell lines and a process for the preparation thereof.
    Type: Application
    Filed: September 8, 2009
    Publication date: November 8, 2012
    Applicant: Council of Scientific & Industrial Redearch
    Inventors: Ahmed Kamal, Earla V. Bharathi, Jonnala S. Reddy, Dudekula Dastagiri, Arutla Viswanath
  • Patent number: 8268845
    Abstract: The present invention relates to the use of tetrahydro- and dihydroquinazolinones of formula I as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases, their use for the manufacture of a pharmaceutical composition and new tetrahydro- and dihydroquinazolinones.
    Type: Grant
    Filed: February 14, 2006
    Date of Patent: September 18, 2012
    Assignee: Merck Patent GmbH
    Inventors: Dirk Finsinger, Armin De Meijere
  • Publication number: 20120213701
    Abstract: The present invention discloses a method for the enzyme-mediated, site-specific, in-vivo precipitation of a water soluble molecule in an animal. The enzyme is either unique to tumor cells, or is produced within a specific site (e.g., tumor) at concentrations that are higher than that in normal tissues. Alternatively, the enzyme is conjugated to a targeting moiety such as an antibody or a receptor-binding molecule.
    Type: Application
    Filed: April 30, 2012
    Publication date: August 23, 2012
    Applicant: President and Fellows of Harvard College
    Inventors: Amin I. Kassis, Ravi S. Harapanhalli
  • Publication number: 20120178915
    Abstract: This invention relates with the arylheterocycle-fused pyrimidines, derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: A-cycle is of 3-8 saturated or unsaturated arylheterocycles or aliheterocyclic, containing 1-4 heteroatoms, B-cycle 5-8 member saturated or unsaturated heterocycle containing 1-4 heteroatoms; X1, X2, X3, X4 are, independently at each occurrence, C, O, S, Se, N and P elements; R1, R2, R3 is a substituent containing alicyclic group, arylcycle group, heterocyclic group, adamantane alkyl, adamantane heterocycle, adamantane analogs, sugar group, hydroxyl group, amino acid group or a combination of the above substituents. This invention also relates with their preparative methods and applications.
    Type: Application
    Filed: December 24, 2009
    Publication date: July 12, 2012
    Inventor: Lifeng Xu
  • Patent number: 8178545
    Abstract: The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53.
    Type: Grant
    Filed: June 1, 2005
    Date of Patent: May 15, 2012
    Assignee: University of Virginia Patent Foundation
    Inventor: Milton L. Brown
  • Publication number: 20120094038
    Abstract: Yellow and yellow-green fluorescent compounds are provided herein that can be incorporated into carriers (e.g., inks) and applied (e.g., printed) as security features on substrates (e.g., documents). The compounds can be selected based upon their resistance to humidity, and preferably exhibit a high initial fluorescence intensity, and a relatively high fluorescence intensity as well as a low relative intensity loss after prolonged humidity exposure.
    Type: Application
    Filed: September 27, 2011
    Publication date: April 19, 2012
    Applicant: HONEYWELL INTERNATIONAL INC.
    Inventors: Thomas R. Potrawa, Michael Kessler
  • Publication number: 20120064025
    Abstract: Compounds, pharmaceutical compositions and methods for modulating the activity of nuclear receptors are provided. In particular, quinazolinones are provided for modulating the activity of farnesoid X receptor (FXR) and/or orphan nuclear receptors.
    Type: Application
    Filed: September 28, 2011
    Publication date: March 15, 2012
    Applicant: EXELIXIS, INC.
    Inventors: Richard Martin, Jeffrey D. Kahl, Brenton T. Flatt, Ronald Griffith
  • Publication number: 20120059002
    Abstract: Disclosed are methods of regulating interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1) and methods of treating and/or preventing cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s) by administering a naturally occurring or synthetic quinazolone derivative. The invention provides novel synthetic quinazolone compounds, as well as pharmaceutical compositions comprising those compounds.
    Type: Application
    Filed: April 21, 2010
    Publication date: March 8, 2012
    Inventors: Henrik C. Hansen, Gregory S. Wagner, Sarah C. Attwell, Kevin G. McLure, Ewelina B. Kulikowski
  • Publication number: 20120040954
    Abstract: Disclosed are novel compounds that are useful in regulating the expression of interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1), and their use in the treatment and/or prevention of cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s). Also, disclosed are compositions comprising the novel compounds, as well as methods for their preparation.
    Type: Application
    Filed: March 16, 2010
    Publication date: February 16, 2012
    Inventor: Henrik C. Hansen
  • Patent number: 8114995
    Abstract: The present disclosure relates to methods for preparing compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and in the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: February 14, 2012
    Assignee: Resverlogix Corp.
    Inventors: Henrik C. Hansen, Shubham P. Chopade, Janakiram R. Citineni, Robert P. Short, George P. Yiannikouros
  • Publication number: 20110306612
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: September 29, 2009
    Publication date: December 15, 2011
    Applicant: Sirtris Pharmaceuticals, Inc.
    Inventors: Chi B. Vu, Christopher Oalmann, Robert B. Perni, Brian White
  • Publication number: 20110294807
    Abstract: Disclosed are novel compounds that are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis. Also disclosed are pharmaceutical compositions comprising the novel compounds.
    Type: Application
    Filed: January 8, 2010
    Publication date: December 1, 2011
    Inventor: Henrik C. Hansen
  • Publication number: 20110071148
    Abstract: The compounds according to formula VIII, their pharmaceutically acceptable acid or base addition salts, and the uses thereof is disclosed. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for the preparing a medicament for modulating estrogen related receptor (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity, etc. The definition of the groups of the formula is defined as the description.
    Type: Application
    Filed: September 10, 2010
    Publication date: March 24, 2011
    Applicant: Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences
    Inventors: Ke Ding, Chiwai Wong, Zhanfang Kang, Xi Zhou
  • Publication number: 20100305109
    Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring G1, X, R1, and R2 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Application
    Filed: May 28, 2010
    Publication date: December 2, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Marc J. Scanio, William H. Bunnelle, William A. Carroll, Sridhar Peddi, Arturo Perez-Medrano, Lei Shi
  • Publication number: 20100273784
    Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.
    Type: Application
    Filed: April 9, 2010
    Publication date: October 28, 2010
    Applicant: Icagen, Inc.
    Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato, James Barnwell Thomas, JR.
  • Patent number: 7820649
    Abstract: Disclosed herein are quinazolinone or isoquinolinone derivatives of formula I, or pharmaceutically acceptable salts or solvates thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions comprising quinazolinone or isoquinolinone according to the present invention and its use in therapy.
    Type: Grant
    Filed: September 10, 2007
    Date of Patent: October 26, 2010
    Assignee: N.V. Organon
    Inventors: Jeffrey Letourneau, Patrick Jokiel, Susan Elizabeth Napier, Koc-Kan Ho, Michael Ohlmeyer, Duncan Robert McArthur, Fiona Jeremiah, Paul David Ratcliffe, Jurgen Schulz
  • Publication number: 20100267688
    Abstract: The present invention comprises compounds of Formula (I). wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Application
    Filed: April 15, 2010
    Publication date: October 21, 2010
    Inventors: Xuqing Zhang, Heather Rae Hufnagel, Chaozhong Cai, James C. Lanter, Thomas P. Markotan, Zhihua Sui
  • Publication number: 20100249161
    Abstract: The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.
    Type: Application
    Filed: November 15, 2007
    Publication date: September 30, 2010
    Inventors: Anders Klarskov Petersen, Preben Houlberg Olesen, Lise Brown Christiansen, Holger Claus Hansen, Flemming Elmelund Nielsen
  • Publication number: 20100189648
    Abstract: A hydrophobic binding pocket on ubiquitin-protein ligase E3 is described, and used in designing the inhibitors disrupting ubiquitin conjugating enzyme E2 and E3 interaction. Four types of inhibitors designed by using the binding pocket are provided, which can be used for cancer treatment.
    Type: Application
    Filed: November 1, 2007
    Publication date: July 29, 2010
    Inventors: Lan Huang, Li Xing
  • Publication number: 20100179176
    Abstract: The present invention relates to a V3 antagonist for use in the treatment of chronic pain, in particular neuropathic pain.
    Type: Application
    Filed: December 13, 2007
    Publication date: July 15, 2010
    Inventor: Inga Neumann
  • Publication number: 20100160316
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: March 1, 2010
    Publication date: June 24, 2010
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jesus E. Gonzalez, III, Dean M. Wilson, Andreas P. Termin, Peter D. J. Grootenhuis, Yulian Zhang, Benjamin J. Petzoldt, Lev Tyler Dewey Fanning, Timothy D. Neubert, Roger D. Tung, Esther Martinborough, Nicole Zimmerman
  • Patent number: 7741332
    Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.
    Type: Grant
    Filed: April 26, 2007
    Date of Patent: June 22, 2010
    Assignee: Icagen, Inc.
    Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato, James Barnwell Thomas, Jr.
  • Publication number: 20100152209
    Abstract: The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.
    Type: Application
    Filed: November 3, 2006
    Publication date: June 17, 2010
    Applicant: Hydra Biosciences Inc.
    Inventors: Jayhong A. Chong, Christopher Fanger, Glenn R. Larsen, William C. Lumma, JR., Anu Mahadevan, Peter Meltzer, Magdalene M. Moran, Amy Ripka, Dennis John Underwood, Manfred Weigele, Xiaoguang Zhen
  • Publication number: 20100125139
    Abstract: A process for the preparation of various quinazoline compounds which are useful as Rho-Kinase inhibitors, and thus having utility in the treatment of hypertension and other indications.
    Type: Application
    Filed: November 17, 2009
    Publication date: May 20, 2010
    Inventors: Donald BANKSTON, Dhanaphalan Nagarathnam, Davoud Asgari, Jianxing Shao, Xiao-Gao Liu, Uday Khire, Chunguang Wang, Barry Hart, Stephen Boyer, Olaf Weber, Mark Lynch
  • Publication number: 20100004448
    Abstract: The present disclosure relates to methods for preparing compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and in the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
    Type: Application
    Filed: June 24, 2009
    Publication date: January 7, 2010
    Applicant: Resverlogix Corp.
    Inventors: Henrik C. Hansen, Shubham P. Chopade, Janakiram R. Citineni, Robert P. Short, George P. Yiannikouros
  • Publication number: 20090324495
    Abstract: The invention provides methods and compositions, e.g., for tumor imaging and therapy.
    Type: Application
    Filed: June 1, 2009
    Publication date: December 31, 2009
    Applicant: President and Fellows of Harvard College
    Inventor: Amin I. Kassis
  • Publication number: 20090318444
    Abstract: The present invention relates to the use of tetrahydro- and dihydroquinazolinones of formula I as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases, their use for the manufacture of a pharmaceutical composition and new tetrahydro- and dihydroquinazolinones.
    Type: Application
    Filed: February 14, 2006
    Publication date: December 24, 2009
    Inventors: Dirk Finsinger, Armin De Meijere
  • Patent number: 7491728
    Abstract: The pyrimidinone compounds are disclosed. Methods of preparing the pyrimidinone compounds are also disclosed.
    Type: Grant
    Filed: April 7, 2004
    Date of Patent: February 17, 2009
    Assignee: SmithKline Beecham Corp.
    Inventors: Irina V. Shcherbakova, Manuel F. Balanddrin, Guangfei Huang, Otto Geoffroy, John Fox, Robert Marquis, Dennis Shinji Yamashita, Juan Luengo, Wenyong Wang
  • Publication number: 20090035306
    Abstract: The present invention relates to quinazolinone compounds useful as modulators of TGR5 and methods for the treatment or prevention of metabolic, cardiovascular, and inflammatory diseases.
    Type: Application
    Filed: November 20, 2007
    Publication date: February 5, 2009
    Applicant: KALYPSYS, INC.
    Inventors: Anthony B. Pinkerton, Ayman Kabakibi, Timothy Z. Hoffman, Dana L. Siegel, Stewart A. Noble
  • Publication number: 20080255111
    Abstract: A medicament which has an activity of inhibiting production of tissue factor and comprises an LXR ligand as an active ingredient; and a medicament for treatment and/or prophylaxis of vascular restenosis following angioplasty, endarterectomy, percutaneous transluminal coronary angioplasty (PTCA) or stent implantation, or treatment and/or prophylaxis of blood coagulation diseases, diseases induced by platelet aggregation including stable or unstable angina pectoris, cardiovascular and cerebrovascular diseases including thromboembolism formation diseases accompanying diabetes, rethrombosis following thrombolysis, cerebral ischemic attack, infarction, stroke, ischemia-derived dementia, peripheral artery disease, thromboembolism formation diseases during use of an aorta-coronary artery bypass, glomerulosclerosis, renal embolism, tumor or cancer metastasis, which comprises an LXR ligand as an active ingredient.
    Type: Application
    Filed: July 1, 2005
    Publication date: October 16, 2008
    Applicant: SANKYO COMPANY LIMITED
    Inventors: Naoki Terasaka, Ayano Hiroshima
  • Patent number: 7223768
    Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.
    Type: Grant
    Filed: September 10, 2004
    Date of Patent: May 29, 2007
    Assignee: Icagen, Inc.
    Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato, James Barnwell Thomas, Jr.
  • Patent number: 7119199
    Abstract: The present invention is directed to a method for producing a pyridopyrimidone of the formula wherein X is N or CH and R is an aryl, heteroaryl or alkyl group, said method comprising the step of reacting an acid derivative of the formula: wherein X is N or CH; Y is an appropriate leaving group; Z is a halogen, OR1, NHR1, or SR1; and R1 is a lower alkyl; and the amidine derivative is wherein R is an aryl, heteroaryl or alkyl group.
    Type: Grant
    Filed: December 31, 2004
    Date of Patent: October 10, 2006
    Assignee: Scios INC
    Inventors: Sarvajit Chakravarty, Sundeep Dugar, Richland Tester, Aurelia Conte
  • Patent number: 6967251
    Abstract: Novel fluorescent derivitization reagents are described that are suitable for coupling to biomolecules that contain aldehyde or ketone functional groups. In one embodiment is provided reagents that have the following formula: wherein Q is carbonyl, thiocarbonyl, or sulfonyl, and R5 is -L-Z; L is arylene, or a C1-6 perfluoroalkylene, or a single covalent bond; Z is a carbonyl hydrazide, hydrazide, sulfonyl hydrazide, or a thiocarbonyl hydrazide; R11-R14 are independently H, C1-6 alkyl, C1-6 alkoxy, C1-6 perfluoroalkyl, C1-6 alklyamino, di(C2-12alkyl)amino, amino, carboxy, cyano, halogen, hydroxy, nitro, phenyl, or sulfo; and R21-R24 are independently H, C1-6 alkyl, C1-6 alkoxy, C1-6 perfluoroalkyl, C1-6 alklyamino, di(C2-12-alkyl)amino, amino, carboxy, cyano, halogen, hydroxy, nitro, phenyl, sulfo, or -L-Z. The method of treating a sample with the derivativization reagents is described.
    Type: Grant
    Filed: October 2, 2001
    Date of Patent: November 22, 2005
    Assignee: Molecular Probes, Inc.
    Inventors: Richard P. Haugland, Thomas H. Steinberg, Wayne F. Patton, Zhenjun Diwu