Carbocyclic Ring Bonded Directly To A Ring Carbon Of The Quinazoline Ring System Patents (Class 514/266.31)
  • Patent number: 10618886
    Abstract: The present invention relates compounds of Formula (A) as H3R antagonists, as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of Histamine 3 Receptor (H3R) functions. The present invention also relates to the uses of the compounds or pharmaceutical compositions in treating or preventing certain disorders and diseases which relate to H3R functions in humans.
    Type: Grant
    Filed: September 30, 2019
    Date of Patent: April 14, 2020
    Assignee: XW LABORATORIES INC.
    Inventors: Jia-Ning Xiang, Xuesong Xu, Yi Feng, Wai-Si Eng
  • Patent number: 10478437
    Abstract: The present invention relates to compositions and methods for reducing cell proliferation and/or promoting cell death. It is based, at least in part, on the discovery that in platinum drug-resistant cell lines, certain compounds, together with a second antiproliferative agent (e.g., cisplatin), act synergistically to promote apoptosis. Accordingly, the present invention provides for novel anticancer strategies.
    Type: Grant
    Filed: December 15, 2016
    Date of Patent: November 19, 2019
    Assignee: University of Pittsburgh—Of the Commonwealth System of Higher Education
    Inventors: Wei Qian, Peter Wipf, Bennett Van Houten
  • Patent number: 9708367
    Abstract: This invention provides novel guanylate cyclase C (GC-C) agonists and their therapeutic use. The agonists may be used either alone or in combination with one or more additional agents.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: July 18, 2017
    Assignee: SYNERGY PHARMACEUTICALS, INC.
    Inventor: Kunwar Shailubhai
  • Patent number: 9382261
    Abstract: Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, salts, and solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
    Type: Grant
    Filed: December 27, 2012
    Date of Patent: July 5, 2016
    Assignee: Janssen Sciences Ireland UC
    Inventors: Koen Vandyck, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 9206177
    Abstract: The invention relates to novel heterocyclic compounds which are pyrazolopyridine derivatives that induce FGFR dimerization, having the general formula: M-L-M2 in which M and M2, which may be identical or different, each represent, independently of one another, a monomer unit M and L represents a linker group which links M1 and M2 covalently with the monomer unit which follows (Formula M). Process for the preparation thereof and therapeutic use thereof.
    Type: Grant
    Filed: December 26, 2012
    Date of Patent: December 8, 2015
    Assignee: SANOFI
    Inventors: Alexandre Benazet, Nathalie Guillo
  • Patent number: 9133136
    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: January 28, 2014
    Date of Patent: September 15, 2015
    Assignee: University of Virginia Patent Foundation
    Inventor: Milton L. Brown
  • Patent number: 9119857
    Abstract: HslVU is the proteasome-related system composed of HslV peptidase and HslU chaperone. It is involved in intracellular proteolysis. The presence of HslVU homologs in pathogenic microbes and its absence in human makes it an antimicrobial drug target. The functional HslVU complex forms when HslV dodecamer is flanked at both ends by HslU hexamers. In the HslVU complex, intercalation of C-termini residues of HslU subunits into the clefts between adjacent HslV subunits results in allosteric activation of HslV. We identified small molecules capable of activating HslV peptidase in the absence of its natural activator HslU. Quinazoline and chromone derivatives were suggested by ligand docking to bind at the HslU C-termini intercalation pockets in the HslV. This was confirmed by HslV activation assays with these compounds that gave ED50 in sub-micromolar range. The results showed that small, extracellular non-peptidic molecules can activate the HslV peptidase which in turn would initiate intracellular proteolysis.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: September 1, 2015
    Inventors: M. Kamran Azim, Yasmeen Rashid, Khalid M. Khan
  • Publication number: 20150087636
    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: Application
    Filed: September 19, 2014
    Publication date: March 26, 2015
    Inventor: Francis M. Sverdrup
  • Publication number: 20150072955
    Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
    Type: Application
    Filed: October 14, 2014
    Publication date: March 12, 2015
    Applicant: Resverlogix Corp.
    Inventor: Henrik C. Hansen
  • Publication number: 20140371248
    Abstract: HslVU is the proteasome-related system composed of HslV peptidase and HslU chaperone. It is involved in intracellular proteolysis. The presence of HslVU homologs in pathogenic microbes and its absence in human makes it an antimicrobial drug target. The functional HslVU complex forms when HslV dodecamer is flanked at both ends by HslU hexamers. In the HslVU complex, intercalation of C-termini residues of HslU subunits into the clefts between adjacent HslV subunits results in allosteric activation of HslV. We identified small molecules capable of activating HslV peptidase in the absence of its natural activator HslU. Quinazoline and chromone derivatives were suggested by ligand docking to bind at the HslU C-termini intercalation pockets in the HslV. This was confirmed by HslV activation assays with these compounds that gave ED50 in sub-micromolar range. The results showed that small, extracellular non-peptidic molecules can activate the HslV peptidase which in turn would initiate intracellular proteolysis.
    Type: Application
    Filed: June 17, 2013
    Publication date: December 18, 2014
    Inventors: M. KAMRAN AZIM, YASMEEN RASHID, KHALID M. KHAN
  • Publication number: 20140329805
    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: Application
    Filed: January 28, 2014
    Publication date: November 6, 2014
    Applicant: University of Virginia Patent Foundation
    Inventor: Milton L. Brown
  • 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: 20140256754
    Abstract: Quinazoline derivatives 1-25, (2-[3,4-bis(methyloxy)phenyl]quinazolin-4-(3H)-one) and 2-[2-(ethyloxy)phenyl]quinazoline-4-(3H)-one) are reported as ?-glucuronidase inhibitors useful in the treatment of ?-glucuronidase hyperactivity disorders.
    Type: Application
    Filed: March 7, 2013
    Publication date: September 11, 2014
    Inventors: Muhammad Iqbal Choudhary, Kahalid Mohammed KHAN, Nimra Naveed SHAIKH, Syed Muhammad SAAD, Sammer YOUSUF, Atta-ur Rahman
  • Publication number: 20140249129
    Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: February 20, 2014
    Publication date: September 4, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Christian GNAMM, Thorsten OOST, Stefan PETERS, Klaus RUDOLF
  • Patent number: 8785459
    Abstract: A compound for treating protein kinase-related disease or disorder having a structure of formula (A): wherein X is N or CH; Y is NH, O, or CH2; Z is an aryl or a heteroaryl; and R1, R2, R3, and R4 are independently H, halo, nitro, cyano, aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, —ORa, —C(O)Ra, —C(O)NRaRb, —NRaC(O)Rb, —NRaRb, —S(O)2Ra, —S(O)2NRaRb, —NRaS(O)2Rb, —N?CRaRb, or —NRaC(O)NHRb, wherein each of Ra and Rb, independently, is H, alkyl, alkenyl, alkynyl, aryl, aryloxy, alkoxy, hydroxy, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, or Ra and Rb, together with the nitrogen atom to which they are bonded, form heteroaryl, heterocycloalkyl, or heterocycloalkenyl; or R3 and R4 are as defined above, and R1 and R2 together with the carbons, to which they are attached, form a heterocycloalkenyl or heteroaryl.
    Type: Grant
    Filed: December 27, 2011
    Date of Patent: July 22, 2014
    Assignee: Development Center for Biotechnology
    Inventors: Jiann-Jyh Huang, Chu-Bin Liao, Pao-Nien Chen
  • Patent number: 8741259
    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: Grant
    Filed: October 20, 2008
    Date of Patent: June 3, 2014
    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: 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
  • Publication number: 20140073574
    Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.
    Type: Application
    Filed: November 13, 2013
    Publication date: March 13, 2014
    Inventors: Robert L. Roden, Richard J. Gorczynski, Michael J. Gerber
  • 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
  • Patent number: 8618120
    Abstract: A synergistic combination of a vanilloid receptor VR-1 antagonist and an NSAID or a pharmaceutically acceptable salt or solvate of either or both compounds thereof.
    Type: Grant
    Filed: July 16, 2008
    Date of Patent: December 31, 2013
    Assignee: Novartis AG
    Inventors: Alyson Fox, Mark Nash, Bindi Sohal, Elliot Lilley
  • Patent number: 8569317
    Abstract: A compound of formula (1): wherein R1, R2, R3 and Y are as defined herein, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, useful for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: October 29, 2013
    Assignee: Novartis AG
    Inventors: Eva Altmann, Rene Beerli, Marc Gerspacher, Johanne Renaud, Sven Weiler, Leo Widler
  • Publication number: 20130281398
    Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 24, 2013
    Applicant: RVX Therapeutics Inc.
    Inventors: Kevin G. McLure, Peter R. Young
  • Publication number: 20130281473
    Abstract: The invention relates to substituted nitrogen containing bicyclic heterocycles of the formula (I) wherein Z is CH2 or N—R4 and X, R1, R2, R4, R6, R7 and n are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
    Type: Application
    Filed: February 27, 2013
    Publication date: October 24, 2013
    Inventors: Joerg BERGHAUSEN, Nicole BUSCHMANN, Pascal FURET, Francois GESSIER, Joanna HERGOVICH LISZTWAN, Philipp HOLZER, Edgar JACOBY, Joerg KALLEN, Keiichi MASUYA, Carole PISSOT SOLDERMANN, Haixia REN, Stefan STUTZ
  • Publication number: 20130281397
    Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer, including NUT midline carcinoma, Burkitt's Lymphoma, Acute Myelogenous Leukemia, and Multiple Myeloma; autoimmune or inflammatory diseases or conditions, and sepsis.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 24, 2013
    Applicant: RVX Therapeutics Inc.
    Inventors: Kevin G. McLure, Peter Ronald Young
  • Publication number: 20130267502
    Abstract: This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 10, 2013
    Inventors: Gregory A. Demopulos, George A. Gaitanaris, Roberto Ciccocioppo
  • Publication number: 20130225610
    Abstract: Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.
    Type: Application
    Filed: March 18, 2013
    Publication date: August 29, 2013
    Inventor: Marc Hansen
  • Publication number: 20130171101
    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: Application
    Filed: December 31, 2011
    Publication date: July 4, 2013
    Inventors: Sheikh Riazuddin, Osman Ali, Usman Ashfaq, Shaheen N. Khan, Javed Akram, Atta-ur Rahman, M. Iqbal Choudhary, Khalid M. Khan, Zulfiqa Ali Khan
  • Patent number: 8476286
    Abstract: Use of compound of formula (I), wherein, is, or, and wherein the symbols are as defined, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, for the preparation of a medicament for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: July 2, 2013
    Assignee: Novartis AG
    Inventors: René Beerli, Ruben A Tommasi, Sven Weiler, Leo Widler
  • Patent number: 8476298
    Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: July 2, 2013
    Assignee: Exelixis, Inc.
    Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrisson B. Mac, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wie Xu
  • Publication number: 20130150387
    Abstract: The present invention relates to substituted amino-quinazolinones of general formula (I) wherein the groups R1 to R14 and A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.
    Type: Application
    Filed: June 14, 2012
    Publication date: June 13, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Klaus FUCHS, Niklas HEINE, Christian EICKMEIER, Sandra HANDSCHUH, Cornelia DORNER-CIOSSEK, Stefan HOERER
  • Patent number: 8450333
    Abstract: The present invention provides compounds capable of regulating apoptosis, e.g., via regulating mitochondrial fission or fusion. The present invention also provides methods of screening for compounds capable of regulating apoptosis and methods of treating conditions association with apoptosis.
    Type: Grant
    Filed: February 8, 2008
    Date of Patent: May 28, 2013
    Assignee: The Regents of The University of California
    Inventors: Jodi Nunnari, Ann Cassidy-Stone, Mark Kurth
  • Publication number: 20130108672
    Abstract: The present disclosure relates to novel solid pharmaceutical formulations and process for their preparation. The present disclosure also provides, in part, methods of using the pharmaceutical formulations 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.
    Type: Application
    Filed: October 31, 2012
    Publication date: May 2, 2013
    Applicant: Resverlogix Corp.
    Inventor: Resverlogix Corp.
  • 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: 8389531
    Abstract: The present invention provides an improved and commercially viable process for preparation of erlotinib substantially free of N-methoxyethyl impurity, namely N-[(3-ethynylphenyl)-(2-methoxyethyl)]-6,7-bis(2-methoxyethoxy)-4-quinazolinamine, and its pharmaceutically acceptable acid addition salts thereof in high purity and in high yield. According to the present invention, erlotinib or a pharmaceutically acceptable acid addition salt of erlotinib substantially free of N-methoxyethyl impurity is prepared by isolating erlotinib or a pharmaceutically acceptable salt of erlotinib from a solvent medium comprising dimethyl sulfoxide and an alcoholic solvent.
    Type: Grant
    Filed: July 11, 2007
    Date of Patent: March 5, 2013
    Assignee: Hetero Drugs Limited
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivasa Rao
  • Publication number: 20130035348
    Abstract: Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.
    Type: Application
    Filed: April 6, 2011
    Publication date: February 7, 2013
    Applicant: BRIGHAM YOUNG UNIVERSITY
    Inventor: Marc Hansen
  • Patent number: 8349853
    Abstract: This invention generally relates to compositions and methods for cancer treatment and, in particular, to compositions able to interact (e.g., bind to) with MUC1 growth factor receptor or its ligands, and methods for treating the same. The invention also relates to assays or use of such compositions for the treatment of patients susceptible to or exhibiting symptoms characteristic of cancer or tumorigenesis. Other compositions of the present invention useful for the treatment or prevention of cancer or tumorigenesis include homologs, analogs, derivatives, enantiomers or functional equivalents. The present compositions can also be packaged in kits in some cases.
    Type: Grant
    Filed: September 5, 2002
    Date of Patent: January 8, 2013
    Assignee: Minerva Biotechnologies Corporation
    Inventor: Cynthia C. Bamdad
  • 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: 20120245147
    Abstract: Methods for screening for inhibitors of endoplasmic reticulum (ER) stress are provided. These methods involve the addition of thapsigargin, which induces ER stress, and a test agent to mammalian cells in multi-well plates. Cell survival can be readily monitored by measuring intracellular ATP content using a bioluminescent reagent. Screening a commercially available library of 50,000 compounds led to the identification of 93 hit compounds that were subjected to secondary assays to confirm their ability to rescue cells from thapsigargin-induced cell death.
    Type: Application
    Filed: April 19, 2012
    Publication date: September 27, 2012
    Inventors: John C. REED, In-Ki Kim
  • 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: 20120202800
    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: Application
    Filed: February 6, 2012
    Publication date: August 9, 2012
    Applicant: University of Virginia Patent Foundation
    Inventor: Milton L. Brown
  • Publication number: 20120129877
    Abstract: The present invention relates to the use of a series of quinazoline-derived compounds to produce a medicament for the treatment and/or prevention of neurological and/or neurodegenerative diseases, such as Parkinson's disease or Alzheimer's disease. The present invention also relates to a method for the treatment and/prevention of neurological and/neurodegenerative diseases comprising the administration of a therapeutically effective amount of said compounds.
    Type: Application
    Filed: May 20, 2010
    Publication date: May 24, 2012
    Applicant: Consejo Superior De Investigaciones Cientificas
    Inventors: Ana Martínez Gil, Carmen Gil Ayuso-Gontan, Concepción Pérez Martín, Ana Pérez Castillo, José Morales García, Miriam Redondo, Marina Sanz San Cristóbal
  • 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: 20120088782
    Abstract: A compound of the general formula (I): (wherein the symbols are as defined in the description), or a non-toxic salt thereof.
    Type: Application
    Filed: December 19, 2011
    Publication date: April 12, 2012
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Masahiko Terakado, Shinji Nakade, Takuya Seko, Yoshikazu Takaoka
  • 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: 20120053052
    Abstract: The present invention relates to the 3-arylquinazolin-4-one compounds of the formula I and the salts thereof, wherein n is 0, 1 or 2; X is O, S or N—R4; Y1 is N or CH; Y2 is N or C—R5; R1 is C1-C10-alkyl, C1-C10-haloalkyl, C2-C10-alkenyl, C2-C10-haloalkenyl, C2-C10-alkynyl, C2-C10-haloalkynyl, C3-C12-cycloalkyl, C5-C12-cycloalkenyl, C3-C12-cycloalkyl-C1-C4-alkyl, C5-C12-cycloalkenyl-C1-C4-alkyl, where the cycloalkyl radical and the cycloalkenyl radical in the last four mentioned radicals are unsubstituted, partially or fully halogenated and/or carry 1, 2, 3, 4, or 5 C1-C4-alkyl radicals; R2 is hydrogen, halogen, CN, C(Z)NH2, C1-C4-alkyl or C1-C4-haloalkyl, wherein Z is O, S or NR6; and the variables k, R, R3, R4, R5 and R6 are as defined in the claims. The invention also relates to the use of novel compounds of formula I for combating invertebrate pests and to a method for controlling invertebrate pests.
    Type: Application
    Filed: March 3, 2010
    Publication date: March 1, 2012
    Applicant: BASF SE
    Inventors: Steffen Gross, Karsten Körber, Wolfgang von Deyn, Florian Kaiser, Prashant Deshmukh, Joachim Dickhaut, Nina Gertrud Bandur, Arun Narine, Matthias Pohlman, Michael Puhl, Sarah Thompson, Cecille Ebuenga, Douglas D. Anspaugh, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, Faraneh Oloumi
  • Publication number: 20120015905
    Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
    Type: Application
    Filed: September 23, 2011
    Publication date: January 19, 2012
    Inventor: Henrik C. Hansen
  • 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