Carbocyclic Ring Bonded Directly At 2-position Patents (Class 544/289)
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Patent number: 9006251Abstract: 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: GrantFiled: June 24, 2014Date of Patent: April 14, 2015Assignee: Janssen Pharamceutica NVInventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
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Publication number: 20140301944Abstract: 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: ApplicationFiled: April 2, 2014Publication date: October 9, 2014Applicants: Forschungsverbund Berlin E.V., The United States of America, as represented by the Secretary, Department of Health and Human ServInventors: 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
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Publication number: 20140234887Abstract: 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: ApplicationFiled: September 27, 2012Publication date: August 21, 2014Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTFIQUEInventors: Jens Hasserodt, Oliver Thorn-Seshold
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Patent number: 8809354Abstract: 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: GrantFiled: December 31, 2011Date of Patent: August 19, 2014Inventors: Sheikh Riazuddin, Osman Ali, Usman Ashfaq, Shaheen N. Khan, Javed Akram, Atta-ur Rahman, M. Iqbal Choudhary, Khalid M. Khan, Zulfiqar Ali Khan
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Publication number: 20140142102Abstract: 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: ApplicationFiled: November 20, 2013Publication date: May 22, 2014Applicant: RVX Therapeutics Inc.Inventors: David John Fairfax, Bryan Cordell Duffy, Gregory Scott Martin, John Frederick Quinn, Shuang Liu, Gregory Steven Wagner, Peter Ronald Young
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Publication number: 20140140956Abstract: 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: ApplicationFiled: November 20, 2013Publication date: May 22, 2014Applicant: RVX Therapeutics Inc.Inventors: David John Fairfax, Gregory Scott Martin, John Frederick Quinn, Bryan Cordell Duffy, Gregory Steven Wagner, Peter Ronald Young
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Patent number: 8642610Abstract: 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: GrantFiled: February 6, 2012Date of Patent: February 4, 2014Assignee: University of Virginia Patent FoundationInventor: Milton L. Brown
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Publication number: 20140018363Abstract: 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: ApplicationFiled: July 30, 2013Publication date: January 16, 2014Applicant: China Medical UniversityInventors: Mann-Jen Hour, Po-Wu Gean, Sheng-Chu Kuo, Hong-Zin Lee, Jai-Sing Yang, Li-Chen Chou, Tai-Lin Chen
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Publication number: 20130336887Abstract: The invention provides methods and compositions, e.g., for tumor imaging and therapy.Type: ApplicationFiled: March 11, 2013Publication date: December 19, 2013Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventor: President and Fellows of Harvard College
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Publication number: 20130310376Abstract: 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: ApplicationFiled: July 30, 2013Publication date: November 21, 2013Applicant: China Medical UniversityInventors: Mann-Jen Hour, Po-Wu Gean, Sheng-Chu Kuo, Hong-Zin Lee, Jai-Sing Yang, Li-Chen Chou, Tai-Lin Chen
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Publication number: 20130303551Abstract: 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: ApplicationFiled: January 10, 2012Publication date: November 14, 2013Inventors: Nicholas D. Adams, Alexander Joseph Reif, Kenneth Wiggall
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Publication number: 20130251631Abstract: 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: ApplicationFiled: May 17, 2013Publication date: September 26, 2013Applicants: Forschungsverbund Berlin E.V., The Government of the United States of America as represented by the Secretary of the Department ofInventors: 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
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Publication number: 20130102602Abstract: 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: ApplicationFiled: October 20, 2011Publication date: April 25, 2013Applicant: China Medical UniversityInventors: Mann-Jen Hour, Po-Wu Gean, Sheng-Chu Kuo, Hong-Zin Lee, Jai-Sing Yang, Li-Chen Chou, Tai-Lin Chen
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Patent number: 8394953Abstract: The invention provides methods and compositions, e.g., for tumor imaging and therapy.Type: GrantFiled: June 1, 2009Date of Patent: March 12, 2013Assignee: President and Fellows of Harvard CollegeInventor: Amin I. Kassis
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Publication number: 20120315217Abstract: TSHR inverse agonists and neutral antagonists that are useful for treating Graves' orbitopathy, Graves' hyperthyroidism and/or thyroid cancer.Type: ApplicationFiled: April 8, 2011Publication date: December 13, 2012Inventors: Marvin Gershengorn, Susanne Neumann, Wenwei Huang, Craig J. Thomas
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Patent number: 8329713Abstract: 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: GrantFiled: April 9, 2010Date of Patent: December 11, 2012Assignee: Icagen Inc.Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato, James Barnwell Thomas, Jr.
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Publication number: 20120288884Abstract: 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: ApplicationFiled: July 28, 2011Publication date: November 15, 2012Applicant: NANYANG TECHNOLOGICAL UNIVERSITYInventors: Bengang Xing, Junxin Aw, Qing Shao, Yanmei Yang, Tingting Jiang, Chungyen Ang
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Publication number: 20120283439Abstract: 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: ApplicationFiled: September 8, 2009Publication date: November 8, 2012Applicant: Council of Scientific & Industrial RedearchInventors: Ahmed Kamal, Earla V. Bharathi, Jonnala S. Reddy, Dudekula Dastagiri, Arutla Viswanath
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Patent number: 8268845Abstract: 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: GrantFiled: February 14, 2006Date of Patent: September 18, 2012Assignee: Merck Patent GmbHInventors: Dirk Finsinger, Armin De Meijere
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Publication number: 20120213701Abstract: 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: ApplicationFiled: April 30, 2012Publication date: August 23, 2012Applicant: President and Fellows of Harvard CollegeInventors: Amin I. Kassis, Ravi S. Harapanhalli
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Publication number: 20120178915Abstract: 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: ApplicationFiled: December 24, 2009Publication date: July 12, 2012Inventor: Lifeng Xu
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Patent number: 8178545Abstract: 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: GrantFiled: June 1, 2005Date of Patent: May 15, 2012Assignee: University of Virginia Patent FoundationInventor: Milton L. Brown
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Publication number: 20120094038Abstract: 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: ApplicationFiled: September 27, 2011Publication date: April 19, 2012Applicant: HONEYWELL INTERNATIONAL INC.Inventors: Thomas R. Potrawa, Michael Kessler
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Publication number: 20120064025Abstract: 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: ApplicationFiled: September 28, 2011Publication date: March 15, 2012Applicant: EXELIXIS, INC.Inventors: Richard Martin, Jeffrey D. Kahl, Brenton T. Flatt, Ronald Griffith
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Publication number: 20120059002Abstract: 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: ApplicationFiled: April 21, 2010Publication date: March 8, 2012Inventors: Henrik C. Hansen, Gregory S. Wagner, Sarah C. Attwell, Kevin G. McLure, Ewelina B. Kulikowski
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Publication number: 20120040954Abstract: 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: ApplicationFiled: March 16, 2010Publication date: February 16, 2012Inventor: Henrik C. Hansen
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Patent number: 8114995Abstract: 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: GrantFiled: June 24, 2009Date of Patent: February 14, 2012Assignee: Resverlogix Corp.Inventors: Henrik C. Hansen, Shubham P. Chopade, Janakiram R. Citineni, Robert P. Short, George P. Yiannikouros
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Publication number: 20110306612Abstract: 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: ApplicationFiled: September 29, 2009Publication date: December 15, 2011Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Chi B. Vu, Christopher Oalmann, Robert B. Perni, Brian White
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Publication number: 20110294807Abstract: 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: ApplicationFiled: January 8, 2010Publication date: December 1, 2011Inventor: Henrik C. Hansen
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Publication number: 20110071148Abstract: 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: ApplicationFiled: September 10, 2010Publication date: March 24, 2011Applicant: Guangzhou Institute of Biomedicine and Health, Chinese Academy of SciencesInventors: Ke Ding, Chiwai Wong, Zhanfang Kang, Xi Zhou
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Publication number: 20100305109Abstract: 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: ApplicationFiled: May 28, 2010Publication date: December 2, 2010Applicant: ABBOTT LABORATORIESInventors: Marc J. Scanio, William H. Bunnelle, William A. Carroll, Sridhar Peddi, Arturo Perez-Medrano, Lei Shi
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Publication number: 20100273784Abstract: 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: ApplicationFiled: April 9, 2010Publication date: October 28, 2010Applicant: Icagen, Inc.Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato, James Barnwell Thomas, JR.
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Patent number: 7820649Abstract: 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: GrantFiled: September 10, 2007Date of Patent: October 26, 2010Assignee: N.V. OrganonInventors: Jeffrey Letourneau, Patrick Jokiel, Susan Elizabeth Napier, Koc-Kan Ho, Michael Ohlmeyer, Duncan Robert McArthur, Fiona Jeremiah, Paul David Ratcliffe, Jurgen Schulz
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Publication number: 20100267688Abstract: 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: ApplicationFiled: April 15, 2010Publication date: October 21, 2010Inventors: Xuqing Zhang, Heather Rae Hufnagel, Chaozhong Cai, James C. Lanter, Thomas P. Markotan, Zhihua Sui
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Publication number: 20100249161Abstract: 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: ApplicationFiled: November 15, 2007Publication date: September 30, 2010Inventors: Anders Klarskov Petersen, Preben Houlberg Olesen, Lise Brown Christiansen, Holger Claus Hansen, Flemming Elmelund Nielsen
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Publication number: 20100189648Abstract: 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: ApplicationFiled: November 1, 2007Publication date: July 29, 2010Inventors: Lan Huang, Li Xing
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Publication number: 20100179176Abstract: The present invention relates to a V3 antagonist for use in the treatment of chronic pain, in particular neuropathic pain.Type: ApplicationFiled: December 13, 2007Publication date: July 15, 2010Inventor: Inga Neumann
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Publication number: 20100160316Abstract: 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: ApplicationFiled: March 1, 2010Publication date: June 24, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: 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
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Patent number: 7741332Abstract: 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: GrantFiled: April 26, 2007Date of Patent: June 22, 2010Assignee: Icagen, Inc.Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato, James Barnwell Thomas, Jr.
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Publication number: 20100152209Abstract: The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.Type: ApplicationFiled: November 3, 2006Publication date: June 17, 2010Applicant: 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
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Publication number: 20100125139Abstract: 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: ApplicationFiled: November 17, 2009Publication date: May 20, 2010Inventors: Donald BANKSTON, Dhanaphalan Nagarathnam, Davoud Asgari, Jianxing Shao, Xiao-Gao Liu, Uday Khire, Chunguang Wang, Barry Hart, Stephen Boyer, Olaf Weber, Mark Lynch
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Publication number: 20100004448Abstract: 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: ApplicationFiled: June 24, 2009Publication date: January 7, 2010Applicant: Resverlogix Corp.Inventors: Henrik C. Hansen, Shubham P. Chopade, Janakiram R. Citineni, Robert P. Short, George P. Yiannikouros
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Publication number: 20090324495Abstract: The invention provides methods and compositions, e.g., for tumor imaging and therapy.Type: ApplicationFiled: June 1, 2009Publication date: December 31, 2009Applicant: President and Fellows of Harvard CollegeInventor: Amin I. Kassis
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Publication number: 20090318444Abstract: 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: ApplicationFiled: February 14, 2006Publication date: December 24, 2009Inventors: Dirk Finsinger, Armin De Meijere
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Patent number: 7491728Abstract: The pyrimidinone compounds are disclosed. Methods of preparing the pyrimidinone compounds are also disclosed.Type: GrantFiled: April 7, 2004Date of Patent: February 17, 2009Assignee: 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
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Publication number: 20090035306Abstract: 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: ApplicationFiled: November 20, 2007Publication date: February 5, 2009Applicant: KALYPSYS, INC.Inventors: Anthony B. Pinkerton, Ayman Kabakibi, Timothy Z. Hoffman, Dana L. Siegel, Stewart A. Noble
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Publication number: 20080255111Abstract: 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: ApplicationFiled: July 1, 2005Publication date: October 16, 2008Applicant: SANKYO COMPANY LIMITEDInventors: Naoki Terasaka, Ayano Hiroshima
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Patent number: 7223768Abstract: 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: GrantFiled: September 10, 2004Date of Patent: May 29, 2007Assignee: Icagen, Inc.Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato, James Barnwell Thomas, Jr.
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Patent number: 7119199Abstract: 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: GrantFiled: December 31, 2004Date of Patent: October 10, 2006Assignee: Scios INCInventors: Sarvajit Chakravarty, Sundeep Dugar, Richland Tester, Aurelia Conte
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Patent number: 6967251Abstract: 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: GrantFiled: October 2, 2001Date of Patent: November 22, 2005Assignee: Molecular Probes, Inc.Inventors: Richard P. Haugland, Thomas H. Steinberg, Wayne F. Patton, Zhenjun Diwu