Tricyclo Ring System Having The Diazole Ring As One The Cyclos Patents (Class 548/302.1)
  • Patent number: 10596145
    Abstract: In certain embodiments, the disclosure relates to heterocyclic flavone derivatives, such as those described by formula provided herein, pharmaceutical compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing diseases or conditions related to BDNF and TrkB activity, such as depression, stroke, Rett syndrome, Parkinson's disease, and Alzheimer's disease by administering effective amounts of pharmaceutical compositions comprising compounds disclosed herein.
    Type: Grant
    Filed: January 28, 2019
    Date of Patent: March 24, 2020
    Assignee: Emory University
    Inventor: Keqiang Ye
  • Patent number: 10010526
    Abstract: In certain embodiments, the disclosure relates to heterocyclic flavone derivatives, such as those described by formula provided herein, pharmaceutical compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing diseases or conditions related to BDNF and TrkB activity, such as depression, stroke, Rett syndrome, Parkinson's disease, and Alzheimer's disease by administering effective amounts of pharmaceutical compositions comprising compounds disclosed herein.
    Type: Grant
    Filed: January 26, 2017
    Date of Patent: July 3, 2018
    Assignee: Emory University
    Inventor: Keqiang Ye
  • Patent number: 9913921
    Abstract: Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has a flattened structure as a result of the position of at least two exocyclic bonds.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: March 13, 2018
    Assignee: TAGWORKS PHARMACEUTICALS B.V.
    Inventors: Marc Stefan Robillard, Johan Lub, Raffaella Rossin, Sandra Martina Van Ben Bosch, Ronny Mathieu Versteegen
  • Patent number: 9593125
    Abstract: In certain embodiments, the disclosure relates to heterocyclic flavone derivatives, such as those described by formula provided herein, pharmaceutical compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of 5 treating or preventing diseases or conditions related to BDNF and TrkB activity, such as depression, stroke, Rett syndrome, Parkinson's disease, and Alzheimer's disease by administering effective amounts of pharmaceutical compositions comprising compounds disclosed herein to a subject in need thereof.
    Type: Grant
    Filed: July 25, 2013
    Date of Patent: March 14, 2017
    Assignee: Emory University
    Inventor: Keqiang Ye
  • Patent number: 9029561
    Abstract: Compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering a 7,8-dihydroxyflavone derivative with modified flavone or heterocyclic ring to a subject in need thereof. Methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided.
    Type: Grant
    Filed: June 8, 2011
    Date of Patent: May 12, 2015
    Assignee: Emory University
    Inventor: Keqiang Ye
  • Publication number: 20150123089
    Abstract: The present application provides a new nitrogen-containing heterocyclic compound and an organic electronic device using the same.
    Type: Application
    Filed: April 12, 2013
    Publication date: May 7, 2015
    Inventors: Dong Hoon Lee, Tae Yoon Park, Sung Kil Hong, Boonjae Jang, Minseung Chun, Dong Sik Kim, Minyoung Kang
  • Publication number: 20150038501
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Inventors: Leping LI, Min ZHONG
  • Publication number: 20140343045
    Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.
    Type: Application
    Filed: May 23, 2014
    Publication date: November 20, 2014
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
  • Patent number: 8865713
    Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: October 21, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
  • Patent number: 8865756
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Grant
    Filed: December 2, 2009
    Date of Patent: October 21, 2014
    Assignee: Presidio Pharmaceuticals, Inc.
    Inventors: Leping Li, Min Zhong
  • Patent number: 8809548
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: February 8, 2010
    Date of Patent: August 19, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jeffrey Lee Romine, Denis R. St. Laurent, Makonen Belema, Lawrence B. Snyder, Lawrence G. Hamann, John F. Kadow, Jayne Kapur, Andrew C. Good, Omar D. Lopez, Rico Lavoie, John A. Bender
  • Patent number: 8796466
    Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: August 5, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: John A. Bender, Piyasena Hewawasam, John F. Kadow, Omar D. Lopez, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Lawrence B. Snyder, Denis R. St. Laurent, Gan Wang, Ningning Xu, Makonen Belema
  • Patent number: 8796304
    Abstract: The invention is directed to compounds with the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: August 5, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Jan Kehler, Jacob Nielsen, Mauro Marigo, John Paul Kilburn, Morten Langgård
  • Patent number: 8791269
    Abstract: A stable complex of tomoxiprole with 2-hydroxypropyl-beta-cyclodextrin with fast dissolution rate and rapid absorption wherein amorphous tomoxiprole forms a complex with 2-hydroxypropyl-beta-cyclodextrin in about equimolecular ratio. The complex shows a remarkably faster dissolution rate and absorption with respect to crystalline tomoxiprole and is particularly suitable for the production of pharmaceutical oral dosage forms, such as tablets and capsules, where rapid onset of therapeutical action is required. A method of manufacture of the complex is also described and claimed.
    Type: Grant
    Filed: June 14, 2012
    Date of Patent: July 29, 2014
    Assignees: Fondazione Istituto Insubrico di Ricerca per la Vita, Fondazione Cariplo
    Inventors: Alberto Milanese, Marino Nebuloni, Lucia Carrano
  • Publication number: 20140205564
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: March 21, 2014
    Publication date: July 24, 2014
    Inventors: Jeffrey Lee Romine, Denis R. St. Laurent, Makonen Belema, Lawrence B. Snyder, Lawrence G. Hamann, John F. Kadow, Jayne Kapur, Andrew C. Good, Omar D. Lopez, Rico Lavoie, John A. Bender
  • Patent number: 8765760
    Abstract: Provided herein are compounds of formula (I): A-L-B??(I) and pharmaceutically acceptable salts and stereoisomers thereof, wherein A is wherein X is (i) CR1 or N, or (ii) O or NR2, each Y is independently N or CR3, and each Z is independently N or C, wherein R1, R2 and R3 are defined in the specification; L is a linker, and B is a multicyclic ring; methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are inhibitors of phosphodiesterases and useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, e.g., neurological disorders, psychosis, schizophrenia, obesity and diabetes.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: July 1, 2014
    Assignee: Sunovion Pharmaceuticals, Inc.
    Inventors: John Emmerson Campbell, Philip Jones, Michael Charles Hewitt
  • Patent number: 8759345
    Abstract: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: June 24, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
  • Publication number: 20140142307
    Abstract: Singly and multiply charged imidazolium cations (ICs) have been identified as a class of chemical compositions that possess potent antineoplastic, antibacterial and antimicrobial properties. The imidazolium cations disclosed demonstrate greater or equivalent potency towards cancerous cells as the current clinical standard, cisplatin. These imidazolium cations, however, achieve this efficacy without any of the known toxic side effects caused by heavy metal-based antineoplastic drugs such as cisplati.
    Type: Application
    Filed: April 30, 2012
    Publication date: May 22, 2014
    Inventors: Wiley Youngs, Matthew Panzner, Claire Tessier, Michael Deblock, Brian Wright, Patrick Wagers, Nikki Robishaw
  • Publication number: 20140066629
    Abstract: Aromatic azole compounds such as 2-(4-aminophenyl)-5-amino-benzimidazole are prepared in an organic sulfonic acid solvent instead of polyphosphoric acid. This allows recovery and recycle of the solvent and avoids the handling and environmental concerns resulting from the use of polyphosphoric acid. The resulting compounds find use in the pharmaceutical industry, as anticorrosion agents, and as precursors for high-performance fibers having high strength, stiffness, and flame resistance.
    Type: Application
    Filed: August 29, 2012
    Publication date: March 6, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: MARC B. GOLDFINGER, TIMOTHY PELLENBARG
  • Publication number: 20140018313
    Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: November 16, 2011
    Publication date: January 16, 2014
    Inventors: Elizabeth M. Bacon, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, Evan S. Krygowski, John O. Link, James Taylor, Chinh Tran, Teresa Alejandra Trejo Martin, Zheng-Yu Yang, Sheila Zipfel
  • Publication number: 20140005193
    Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
    Type: Application
    Filed: September 3, 2013
    Publication date: January 2, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Frances Meredith Hocutt, BARRY EASTMAN LEONARD, JR., HILLARY M. PELTIER, VICTOR K. PHUONG, MICHAEL H. RABINOWITZ, MARK D. ROSEN, KYLE T. TARANTINO, HARIHARAN VENKATESAN, LUCY XIUMIN ZHAO
  • Publication number: 20130345261
    Abstract: The various embodiments relate to a compound comprising: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are each independently hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocyclyl, alkoxy, aryloxy, heteroaryloxy, alkoxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, alkylsulfonyl, arylsulfonyl, aminosulfonyl, alkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, acyl, acylamino, amino, alkylamino, dialkylamino, arylamino, carboxylate (—CO2H), cyano, nitro, —CONH2, heteroarylamino, oxime, alkyloxime, aryloxime, amino-oxime or halogen when A, B, C, D, E, F, G, H, I, J, K, L, M, N, O, P, and Q are carbon, and X is O, NR (where R is hydrogen, alkyl, aryl or acyl), S, SO (sulfoxide), SO2 (sulfone), or C(R)2 (where R?H, alkyl, aryl, alkenyl, alkynyl, or acyl); or wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are each independently hydrogen or hydroxyl when A, B, C, D, E, F, G, H, I, J, K, L, M, N, O, P, and Q are each independently nitrogen, and compositions, combination
    Type: Application
    Filed: February 4, 2012
    Publication date: December 26, 2013
    Inventors: Christopher Waters, Karthik Sambanthamoorthy, Matthew Neiditch, Martin Semmelhack
  • Patent number: 8609861
    Abstract: Provided are hexaaza[3.3.3]propellane compounds represented by the following formula (I), which can be used as a main skeleton structure for novel molecular explosives and method for preparing the same: wherein, R is H, C1-C20 alkyl, cycloalkyl, arylalkyl or aryl, which may contain heteroatoms such as oxygen, nitrogen, sulfur, halogen, etc. or unsaturations; and X is H2, O or S.
    Type: Grant
    Filed: October 15, 2012
    Date of Patent: December 17, 2013
    Assignee: Agency for Defense Development
    Inventors: Young Gyu Kim, Jin Seuk Kim, Kyoo Hyun Chung, Moon Yong Shin, Seung Hee Kim, Tae Hwan Ha, Hye Ryoung Lee, Myeong Hak Kim
  • Patent number: 8598196
    Abstract: Pharmaceutical formulations and methods for the topical and/or transdermal delivery of imiquimod, including creams, ointments and pressure-sensitive adhesive compositions to treat dermatological disorders, namely, viral infections, such as Type I or Type II Herpes simplex infections and genital and perianal warts, actinic keratosis and superficial basal cell carcinoma, and to induce interferon biosynthesis to achieve an antiviral effect, with shorter durations of therapy, than currently approved for imiquimod by the Food & Drug Administration (“FDA”).
    Type: Grant
    Filed: July 18, 2012
    Date of Patent: December 3, 2013
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Jefferson J. Gregory, Michael T. Nordsiek
  • Publication number: 20130317213
    Abstract: The present disclosure relates to methods for making compounds useful in the treatment of Hepatitis C virus (HCV) infection.
    Type: Application
    Filed: August 1, 2013
    Publication date: November 28, 2013
    Inventors: Shawn K. Pack, Steven Tymonko, Bharat P. Patel, Kenneth J. Natalie, JR., Makonen Belema
  • Publication number: 20130302248
    Abstract: Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formula (I) capable of binding to tau proteins and ?-amyloid peptides are presented herein. The invention also relates to methods of imaging A? and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.
    Type: Application
    Filed: June 25, 2013
    Publication date: November 14, 2013
    Inventors: Umesh B. Gangadharmath, Hartmuth C. Kolb, Peter J.H. Scott, Joseph C. Walsh, Wei Zhang, Anna Katrin Szardenings, Anjana Sinha, Gang Chen, Eric Wang, Vani P. Mocharla, Chul Yu, Changhui Liu, Daniel Kurt Cashion, Dhanalakshmi Kasi
  • Publication number: 20130296311
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: May 26, 2011
    Publication date: November 7, 2013
    Applicant: PRESIDIO PHARMACEUTICALS, INC.
    Inventors: Leping Li, Min Zhong
  • Publication number: 20130267501
    Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.
    Type: Application
    Filed: January 22, 2013
    Publication date: October 10, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventor: The Board of Trustees of the Leland Stanford Junior University
  • Publication number: 20130261148
    Abstract: Provided are protected antimicrobial compounds which are useful for controlling microorganisms in aqueous or water-containing systems, such as oil or gas field fluids, at elevated temperature. The antimicrobial compounds are of the formula I: wherein R, R1, R2, X and Y are as defined herein.
    Type: Application
    Filed: December 2, 2011
    Publication date: October 3, 2013
    Applicants: DOW GLOBAL TECHNOLOGIES LLC, ANGUS CHEMICAL COMPANY
    Inventors: Charles E. Coburn, Michael V. Enzien, Heather R. McGinley, David W. Moore
  • Patent number: 8546376
    Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: October 1, 2013
    Assignee: Almac Discovery Limited
    Inventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
  • Patent number: 8519149
    Abstract: The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
    Type: Grant
    Filed: October 28, 2011
    Date of Patent: August 27, 2013
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Laxmikant A. Gharat, Nagarajan Muthukaman, Lakshminarayana Narayana, Neelima Khairatkar-Joshi, Vidya G. Kattige
  • Publication number: 20130196987
    Abstract: The present invention provides compounds, methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis.
    Type: Application
    Filed: October 30, 2012
    Publication date: August 1, 2013
    Applicant: EISAI CO., LTD.
    Inventors: Roch Boivin, Kenichi Chiba, Jesse Chow, Hong Du, Yoshihito Eguchi, Masanori Fujita, Masaki Goto, Fabian Gusovsky, Jean-Christophe Harmange, Atsushi Inoue, Yimin Jiang, Megumi Kawada, Takatoshi Kawai, Yoshiyuki Kawakami, Akifumi Kimura, Makoto Kotake, Yoshikazu Kuboi, Charles-Andre Lemelin, Xiang-Yi Li, Tomohiro Matsushima, Yoshiharu Mizui, Kenzo Muramoto, Hideki Sakurai, Yong-Chun Shen, Hiroshi Shirota, Mark Spyvee, Isao Tanaka, John (Yuan) Wang, Satoshi Yamamoto, Naoki Yoneda
  • Patent number: 8492374
    Abstract: An azaazulene compound is provided. The azaazulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. The compound can be used to treat cancer. The invention also provides a method for treating cancer. The method includes administering to a subject in need thereof an effective amount of one or more azaazulene compounds of formula (I).
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: July 23, 2013
    Assignee: Industrial Technology Research Institute
    Inventors: On Lee, Chih-Hung Chen, Chi-Y Hung, Yow-Lone Chang, Ting-Shou Chen
  • Publication number: 20130156731
    Abstract: The present invention relates to novel Fused Tricyclic Compounds, compositions comprising at least one Fused Tricyclic Compound, and methods of using Fused Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: December 20, 2010
    Publication date: June 20, 2013
    Inventors: Kevin X. Chen, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Publication number: 20130136782
    Abstract: Compounds described herein inhibit biofilm formation or disperse pre-formed biofilms of Gram-negative bacteria. Biofilm-inhibitory compounds can be encapsulated or contained in a polymer matrix for controlled release. Coatings, films, multilayer films, hydrogels, microspheres and nanospheres as well as pharmaceutical compositions and disinfecting compositions containing biofilm-inhibitory compounds are also provided. Methods for inhibiting formation of biofilms or dispersing already formed biofilms are provided. Methods for treating infections of gram-negative bacteria which form biofilms, particularly those of Pseudomonas and more particularly P. aeruginosa.
    Type: Application
    Filed: November 5, 2012
    Publication date: May 30, 2013
    Inventors: Helen BLACKWELL, Reto Frei, Anthony Breitbach, David M. Lynn, Adam H. Broderick
  • Patent number: 8394968
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: March 12, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventor: Jeffrey Lee Romine
  • Publication number: 20130040947
    Abstract: Compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering a 7,8-di-hydroxyflavone derivative with modified flavone or heterocyclic ring to a subject in need thereof. Methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided.
    Type: Application
    Filed: June 8, 2011
    Publication date: February 14, 2013
    Applicant: EMORY UNIVERSITY
    Inventor: Keqiang Ye
  • Publication number: 20130029964
    Abstract: An object of the present invention is to provide a novel low molecular weight compound exhibiting an osteogenesis-promoting action. This object is achieved by a compound having the general formula (I) or a pharmacologically acceptable salt thereof. In the general formula (I), R1 and R2 represent hydrogen atoms, and the like; R3 represents a hydrogen atom, and the like; X, Y, and Z represent nitrogen atoms, and the like; A represents a phenylene group, and the like; n represents 1 or 2, and the like; and V and W represent oxygen atoms, and the like.
    Type: Application
    Filed: August 27, 2012
    Publication date: January 31, 2013
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Kazumasa Aoki, Satoshi Matsui, Kenji Yoshikawa, Hiroki Shimizu, Junko Sasaki, Katsuyoshi Nakajima, Osamu Kanno, Kiyoshi Oizumi
  • Patent number: 8349473
    Abstract: An organic electroluminescent device is provided and includes: a cathode; an anode; and at least one organic layer between the cathode and the anode. The at least one organic layer includes a light emitting layer containing at least one light emitting material. A compound represented by the following formula (I) is contained in the at least one organic layer. where n stands for an integer of 2 or greater, L represents an n-valent linking group, and R1, R2, R3, and R4 each independently represents a hydrogen atom or a substituent.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: January 8, 2013
    Assignee: UDC Ireland Limited
    Inventors: Toshihiro Ise, Wataru Sotoyama
  • Publication number: 20120276047
    Abstract: The present invention relates to novel fused tricyclic compounds, compositions comprising at least one fused tricyclic compound, and methods of using fused tricyclic compounds for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: November 23, 2010
    Publication date: November 1, 2012
    Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge
  • Patent number: 8299061
    Abstract: This invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof; as well as a method for treating obesity, a method for treating diabetes, and a pharmaceutical composition.
    Type: Grant
    Filed: December 7, 2010
    Date of Patent: October 30, 2012
    Assignee: Eli Lilly and Company
    Inventors: Macklin Brian Arnold, Thomas James Beauchamp, Emily Jane Canada, Erik James Hembre, Jianliang Lu, John Robert Rizzo, John Mehnert Schaus, Qing Shi
  • Publication number: 20120270071
    Abstract: A chromene compound having a skeleton represented by the following formula (1) and exhibiting double peak characteristic: wherein Z is a group represented by any one of the following formulas: n is an integer of 1 to 3, when n is 2 or 3, Z? s may be the same or different, with the proviso that when n is 1, Z cannot be —CH2—, and when n is 2 or 3, Z's cannot be —CH2— at the same time; R1 is an electron absorbing group having a Hammett constant ?p of more than 0, with the proviso that when there are a plurality of R1's, R1's may be the same or different; and X and Y are each independently an oxygen atom or ?NR2, with the proviso that X and Y cannot be oxygen atoms at the same time.
    Type: Application
    Filed: July 21, 2010
    Publication date: October 25, 2012
    Inventors: Toshiaki Takahashi, Junji Takenaka
  • Publication number: 20120264760
    Abstract: One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5?-monophosphate-dehydrogenase over human inosine-5?-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.
    Type: Application
    Filed: June 6, 2012
    Publication date: October 18, 2012
    Applicants: University of Georgia Research Foundation, Inc., Brandeis University
    Inventors: Lizbeth K. Hedstrom, Boris Striepen
  • Publication number: 20120251491
    Abstract: The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: May 12, 2010
    Publication date: October 4, 2012
    Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge, Craig A. Coburn
  • Publication number: 20120238541
    Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
    Type: Application
    Filed: September 17, 2010
    Publication date: September 20, 2012
    Applicant: Almac Discovery Limited
    Inventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
  • Patent number: 8247429
    Abstract: The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group optionally having substituent(s), R2 is a hydrogen atom or a hydrocarbon group optionally having substituent(s), R3 is a hydrogen atom, a halogen atom, a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or mercapto optionally having a substituent, Xa, Xb, Xc and Xd are each a carbon atom or a nitrogen atom, provided that any one or two of Xa, Xb, Xc and Xd is/are nitrogen atom(s), m is 0 to 2, and rings A to C are each a ring optionally having substituent(s), or a salt thereof, which is useful as an agent for the prophylaxis or treatment of a disease relating to an action of melatonin, and the like.
    Type: Grant
    Filed: December 27, 2007
    Date of Patent: August 21, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Osamu Uchikawa, Tatsuki Koike, Takafumi Takai, Yasutaka Hoashi
  • Patent number: 8232393
    Abstract: An electron transport material based on fused aromatic electron-deficient compounds. The accumulation of aromatic rings with an electron deficiency allows free-radical anions to be stabilized very efficiently in these systems.
    Type: Grant
    Filed: July 3, 2007
    Date of Patent: July 31, 2012
    Assignee: OSRAM Opto Semiconductors GmbH
    Inventors: Jürgen Adler, Andreas Kanitz
  • Patent number: 8207173
    Abstract: Provided are compounds of the formula: wherein RN1 is a substituent of formula G1-NX1X2, wherein G1 is an optionally further substituted alkylene, which optionally forms, together with RN2, a cyclic group, and each of X1 and X2 is independently H or an N-substituent, or X1 and X2 together form a heterocyclic ring, or X1 together with G1 forms a cyclic group and X2 is H or an N-substituent; and each of Z1, Z2, Z3 and Z4 is H or a substituent, or two of Z1, Z2, Z3 and Z4 together form an optionally substituted ring, and further wherein at least one of Z1, Z2, Z3 and Z4 is other than H, and salts thereof, pharmaceutical compositions and methods of using the compounds. The compounds have antiviral activity.
    Type: Grant
    Filed: November 17, 2009
    Date of Patent: June 26, 2012
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Punit P. Seth, Elizabeth Anne Jefferson, Richard H. Griffey, Eric E. Swayze
  • Patent number: 8187727
    Abstract: The present invention relates to a new imidazole derivative, a method for preparing the derivative, and an organic electronic device using the derivative. The imidazole derivative according to the invention can perform functions of hole injection, hole transportation, electron injection, electron transportation, and/or light emission in an organic electronic device including an organic light-emitting device. The organic electronic device according to the invention exhibits excellent characteristics in terms of efficiency, drive voltage and stability.
    Type: Grant
    Filed: July 18, 2006
    Date of Patent: May 29, 2012
    Assignee: LG Chem, Ltd.
    Inventors: Jae Soon Bae, Dong Hoon Lee, Dae Woong Lee, Jun Gi Jang
  • Publication number: 20120115820
    Abstract: The present invention relates to a use of a compound having an acid pump antagonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for prevention or treatment of diseases in which abnormal gastrointestinal motility is involved. In addition, the present invention relates to the method of prevention or treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agent. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound having an acid pump antagonistic activity or a pharmaceutically acceptable salt thereof for the prevention or treatment of said diseases.
    Type: Application
    Filed: July 9, 2010
    Publication date: May 10, 2012
    Inventors: Nobuyuki Takahashi, Shinichi Koizumi