Two Of The Cyclos Share At Least Three Ring Members (i.e., Bridged) Patents (Class 514/281)
  • Patent number: 11969421
    Abstract: Disclosed herein are methods of treating neurological or psychiatric diseases or disorders using a combination of bupropion and dextromethorphan. Related compositions and dosage forms are also described.
    Type: Grant
    Filed: June 15, 2022
    Date of Patent: April 30, 2024
    Assignee: Antecip Bioventures II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 11779579
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: September 1, 2022
    Date of Patent: October 10, 2023
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 11433067
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: December 9, 2021
    Date of Patent: September 6, 2022
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 11364233
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: September 7, 2021
    Date of Patent: June 21, 2022
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 11147808
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: March 8, 2021
    Date of Patent: October 19, 2021
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 10980800
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: October 12, 2020
    Date of Patent: April 20, 2021
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 10813924
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: March 12, 2020
    Date of Patent: October 27, 2020
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 10598594
    Abstract: The present invention relates to a method and system for identifying mechanical properties of a cell nucleus through a label-free cell analysis based on Brillouin light scattering techniques. The present application additionally provides a method and system for identifying cancerous cells based on mechanical properties of the cell nucleus.
    Type: Grant
    Filed: March 1, 2018
    Date of Patent: March 24, 2020
    Assignees: University of Maryland, Canon U.S.A., Inc.
    Inventors: Giuliano Scarcelli, Jitao Zhang, Hanyoup Kim
  • Patent number: 10456376
    Abstract: The present invention relates to a pharmaceutical composition for preventatively treating headaches, containing: a carbamate compound of chemical formula 1 or a pharmaceutically acceptable salt, solvent or hydrate thereof; and a pharmaceutically acceptable carrier. According to the present invention, the pharmaceutical composition can effectively prevent a headache, more specifically, headaches caused by cortical spreading depression, and particularly, chronic headaches including migraines.
    Type: Grant
    Filed: May 18, 2017
    Date of Patent: October 29, 2019
    Assignee: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Hye Won Shin, Yoon Kyung Park
  • Patent number: 10017507
    Abstract: Disclosed are a series of diaza-benzofluoranthrene compounds. The present invention particularly relates to a compound represented by formula (I), pharmaceutically acceptable salts or tautomers thereof.
    Type: Grant
    Filed: February 2, 2016
    Date of Patent: July 10, 2018
    Assignee: HARBIN PHARMACEUTICAL GROUP CO., LTD. GENERAL PHARMACEUTICAL FACTORY
    Inventors: Shujie Yuan, Xinchun Yang, Jinlong Zhao, Daoxu Zhang, Mingda Sun, Jiaji Liu, Tao Wei, Huanan Zhao, Yunfu Luo, Chundao Yang
  • Patent number: 9902726
    Abstract: The application is directed to Pyridone-sulfone morphinan analogs compounds of Formula I: or pharmaceutically acceptable salts and solvates thereof, wherein ==, R1, R2, R3, R4 and Z are as defined as set forth in the specification. The invention is also directed to use of the compounds of Formula I or the pharmaceutically acceptable salts and solvates thereof to treat disorders responsive to the odulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: September 12, 2014
    Date of Patent: February 27, 2018
    Assignee: Purdue Pharma L.P.
    Inventor: Mark Youngman
  • Patent number: 9862726
    Abstract: The application is directed to compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, Y, Z, and G are defined as set forth in the specification. The invention is also directed to use of compounds of Formula (I), and pharmaceutically acceptable salts and solvates thereof, to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: January 9, 2018
    Assignee: Purdue Pharma L.P.
    Inventor: Mark Youngman
  • Patent number: 9598414
    Abstract: The present invention discloses pyridoinolobenz[b,e]azepine derivatives of Formula 1, wherein X is —O—, —S—, —SO—, or —SO2—. Y is a single bond or a double bond. A and B are independently —(CH2)n—; and ‘n’ varies from 0 to 3. R1 to R9 are various electron donating, electron withdrawing, hydrophilic, or lipophilic groups selected to optimize the physicochemical and biological properties of compounds of Formula I.
    Type: Grant
    Filed: March 2, 2014
    Date of Patent: March 21, 2017
    Assignee: DAYA DRUG DISCOVERIES, INC.
    Inventor: Parthasarathi Rajagopalan
  • Patent number: 9434975
    Abstract: Compounds are provided that are either fluorogenic or fluorophoric. Compositions and articles that include the compounds are also provided. Additionally, methods of detecting a microorganism using the compounds are provided. The compounds are fluorinated and can be used advantageously under acidic conditions.
    Type: Grant
    Filed: March 5, 2012
    Date of Patent: September 6, 2016
    Assignee: 3M INNOVATIVE PROPERTIES COMPANY
    Inventors: Stephen B. Roscoe, Shih-Hung Chou, Stephanie J. Moeller, Jesse D. Miller, Kurt J. Halverson, Jason W. Bjork
  • Patent number: 9403824
    Abstract: The application is directed to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein , R1a-R3a, R4, Y and Za are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I-A to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: January 28, 2015
    Date of Patent: August 2, 2016
    Assignee: Purdue Pharma L.P.
    Inventors: Jeffrey Lockman, Laykea Tafesse, Mark A. Youngman
  • Patent number: 9340512
    Abstract: This invention relates to novel morphinan compounds and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a ?1 receptor agonist that also has NMDA antagonist activity.
    Type: Grant
    Filed: June 1, 2015
    Date of Patent: May 17, 2016
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Philip B. Graham, I. Robert Silverman
  • Patent number: 9040519
    Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: May 26, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20150110805
    Abstract: Numerous diseases have been linked to the production of effector cells. The present invention relates to the realization that effector cells are cycling in these diseases. In addition, the present invention relates to the determination that regulator cells are cycling in degenerative diseases. Based on these realizations, the present invention provides methods for treating conditions such as autoimmune diseases, degenerative diseases, and graft-versus-host disease. The present invention also relates to methods of determining when therapy should be administered to a patient.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Inventors: Martin Leonard Ashdown, Luisa Maria Ashdown
  • Patent number: 9012468
    Abstract: The present invention provides processes for preparing nal-opiates without the isolation of intermediates. In general, the process provides for alkylation and reduction in the same pot to give the nal-opiate.
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: April 21, 2015
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Tao Jiang
  • Patent number: 8993559
    Abstract: The present invention relates to a method of treating obesity in a subject by administering to the subject a compound having the formula: wherein n is from 0 to 8; R1 is CH2OH, CH(OH)R5, CH2OR5, CO2R5, C(O)NH2, C(O)NHR5, C(O)NR5R6, C(O)NHNH2, C(O)NHNHR5, C(O)NHNR5R6, C(O)NR5NH2, C(O)NR5NHR6, C(O)NR5NR6R7, C(O)NHNH(C(O)R5), C(O)NHNR5(C(O)R6), C(O)NR5NH(C(O)R6), C(O)NR5NR6(C(O)R7), CN, or C(O)R5; R2 is H, unsubstituted or substituted alkyl, YH, YR8, YR8R9, YR8YR9YR10, YC(O)R8, C(O)YR8, C(O)NH2, C(O)NHR8, C(O)NR8R9, NH2, NHR8, NR8R9, NHC(O)R8, or NR8C(O)R9; R3 and R4 are the same or different and are selected from the group consisting of H, halogens, unsubstituted or substituted alkyl, OH, OR10, NH2, NHR10, NR10R11, NHC(O)R10, or NR10C(O)R11; R5, R6, R7, R8, R9, R10, and R11 are the same or different and are selected from the group consisting of H, unsubstituted alkyl, substituted alkyl, unsubstituted aryl and substituted aryl; R12 is selected from the group consisting of H, unsubstituted alkyl, and substitu
    Type: Grant
    Filed: January 27, 2009
    Date of Patent: March 31, 2015
    Assignee: Albany Medical College
    Inventors: Stanley D. Glick, Isabelle M. Maisonneuve, Olga D. Taraschenko
  • Patent number: 8980906
    Abstract: The application is directed to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein , R1a—R3a, R4, Y and Za are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I-A to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: March 17, 2015
    Assignee: Purdue Pharma L.P.
    Inventor: Laykea Tafesse
  • Publication number: 20150072396
    Abstract: Low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations for modifying biomolecules is provided. Compositions, methods, and kits relating to low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations are also provided.
    Type: Application
    Filed: March 1, 2012
    Publication date: March 12, 2015
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Kyle Gee, Upinder Singh, Scott Grecian, Scott Clarke
  • Publication number: 20150051240
    Abstract: The invention relates to a composition comprising buprenorphine and a ? opioid receptor antagonist, wherein the composition is characterized by an Agonist Antagonist Activity Index (AAnAI) of between about 0.7 and about 2.2; wherein; AAnAI = [ C max ? ( BUP ) / EC 50 ] [ C max ? ( ANTAGONIST ) / IC 50 ] .
    Type: Application
    Filed: July 29, 2014
    Publication date: February 19, 2015
    Inventors: Daniel Deaver, Elliot Ehrich
  • Publication number: 20150031628
    Abstract: Oral dosage compositions for drugs normally given intravenously such as Paclitaxel, containing a plant sterol to enhance solubility and a small intestine efflux inhibitor to prevent P-glycoprotein from being a barrier to absorption.
    Type: Application
    Filed: August 6, 2014
    Publication date: January 29, 2015
    Inventor: Curtis A. Spilburg
  • Publication number: 20150030672
    Abstract: A liposome comprising bilayer and inner water phase is disclosed. Said inner water phase may contain sulfobutyl ether cyclodextrin and an active compound.
    Type: Application
    Filed: September 25, 2014
    Publication date: January 29, 2015
    Inventors: Chunlei LI, Lan ZHANG, Caixia WANG, Li ZHANG, Dongmin SHEN, Yanhui LI, Xian XIU, Min LIANG, Yongfeng LI
  • Patent number: 8933092
    Abstract: Methods and compositions for the alleviation of pain in a patient. The methods and compositions sequentially administer a therapeutically effective amount of first compound having opioid receptor agonist activity, followed by a therapeutic effective amount of a second or subsequent compound(s) having opioid receptor agonist activity, one or more non-opioid analgesic compounds or one or more hybrid opioid compounds, or mixtures thereof. The methods and compositions effectively alleviate pain with a lower incidence of opioid-induced side effects.
    Type: Grant
    Filed: May 31, 2012
    Date of Patent: January 13, 2015
    Assignee: Qrxpharma Limited
    Inventor: John W. Holaday
  • Patent number: 8927569
    Abstract: A class of macrocyclic compounds of formula (I), wherein R1, R3, R4, Ra, Rb, A, Z, Y, X, M, W, n and m are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes 5 for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: January 6, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Steven Harper, Vincenzo Summa, Nigel J. Liverton, John A. McCauley, John W. Butcher, Marcello Di Filippo, Maria Emilia Di Francesco, Marco Ferrara, Joseph J. Romano, Michael T. Rudd
  • Publication number: 20140363491
    Abstract: The present disclosure provides lipid-containing compositions, including targeted liposomes encapsulating drug, and pharmaceutical formulations thereof, as well as methods for the making and using the lipid-containing compositions, including the use of the targeted liposomes in the treatment of cancer and other diseases.
    Type: Application
    Filed: May 9, 2014
    Publication date: December 11, 2014
    Applicant: Mebiopharm Co., Ltd.
    Inventors: Kazushi OKADA, Tadayuki IBUKI, Donghyun KIM, Tadashi FUJISAWA
  • Publication number: 20140301947
    Abstract: A method for aiding in selecting or adjusting a dose of TSPO imaging or therapeutic agent for use with a subject, the method comprising the step of determining the subject's genotype for TSPO rs6971. A TSPO imaging or therapeutic agent for use in TSPO imaging or therapy in a subject, wherein the subject is a subject whose genotype at TSPO polymorphism position rs6971 is determined. The subject's genotype for TSPO may be taken into account when assessing the results of the TSPO imaging, for example normalising the subject's determined measure of binding of the TSPO agent to take account of the subject's determined genotype. The subject's genotype for TSPO may be taken into account when choosing the TSPO agent and/or the dose of TSPO agent. The subject may be a subject who has been determined to have genotype CC or CT at TSPO polymorphism position rs6971, for example when using a TSPO agent that binds with higher affinity to Aia147TSPO than to Thr147TSPO.
    Type: Application
    Filed: May 31, 2012
    Publication date: October 9, 2014
    Applicant: IMPERIAL INNOVATIONS LIMITED
    Inventors: David Owen, Martin Wilkins
  • Publication number: 20140296273
    Abstract: Pharmaceutical compositions and methods for treating or preventing an inflammatory condition in a patient are disclosed. The pharmaceutical compositions and methods include the use of vincamine or a vincamine derivative, either alone or in combination with one or more additional therapeutic agents, including a steroid (preferably a corticosteroid), an angiotensin II receptor (type 1) antagonist, an angiotensin-converting enzyme (ACE) inhibitor, and a non-steroidal anti-inflammatory drug.
    Type: Application
    Filed: February 26, 2014
    Publication date: October 2, 2014
    Inventors: Chen Yan, Jian-Dong Li, Bradford Berk, Kye-Im Jeon, Xiangbin Xu
  • Patent number: 8835461
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: September 16, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
  • Publication number: 20140242190
    Abstract: Methods for preventing and/or reducing side effects of an anti-cancer agent in a subject in need thereof are disclosed. The method comprises administering to the subject, who is under an anti-cancer agent treatment, a composition comprising a therapeutically effective amount of isolated deoxyelephantopin and/or an analogue thereof; and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: May 2, 2014
    Publication date: August 28, 2014
    Applicant: Academia Sinica
    Inventors: Lie-Fen SHYUR, Wen-Wan CHAO, Ya-Wen CHENG
  • Publication number: 20140187549
    Abstract: The application is directed to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein , R1a, R3a, R4, Y and Za are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I-A to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: December 13, 2013
    Publication date: July 3, 2014
    Applicant: Purdue Pharma L.P.
    Inventor: Laykea TAFESSE
  • Publication number: 20140187571
    Abstract: The application is directed to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein Cy, R1a-R3a, R4a, and R4b are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I-A to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: December 23, 2013
    Publication date: July 3, 2014
    Applicant: Purdue Pharma L.P.
    Inventors: Donald J. KYLE, Laykea Tafesse, Xiaoming Zhou
  • Publication number: 20140148398
    Abstract: Compounds useful for the treatment of giardiasis are described.
    Type: Application
    Filed: October 12, 2011
    Publication date: May 29, 2014
    Applicants: The United States of America, as represented by the Secretary, Dept. of Health and Human Service, UNIVERSITY OF MARYLAND, COLLEGE PARK
    Inventors: Wei Zheng, Catherine Chen, Juan Jose Marugan, Noel Southall, Christopher P. Austin, Andrey Galkin, Liudmila Kulakova, Osnat Herzberg
  • Patent number: 8703790
    Abstract: Novel compounds which are alkaloids related to bis [O-(14-Benzoylaconine-8-YL)]esters.
    Type: Grant
    Filed: November 26, 2009
    Date of Patent: April 22, 2014
    Assignee: Universite Victor Segalen Bordeaux 2
    Inventors: Jean-Jacques Bosc, Christian Jarry, Ainura Chodoeva, Jean Guillon, Isabelle Forfar, Jacques Robert
  • Publication number: 20140105895
    Abstract: The present invention is directed to the use of rapamycin derivatives for use in treating solid tumors, optionally in combination with a chemotherapeutic agent.
    Type: Application
    Filed: December 19, 2013
    Publication date: April 17, 2014
    Inventors: Heidi Lane, Terence O'Reilly, Jeanette Marjorie Wood
  • Publication number: 20140038997
    Abstract: The invention relates to a pharmaceutical composition of vinflunine in the form of a stable sterile aqueous solution of a water-soluble salt of vinflunine with a pH of between 3 and 4. The invention also relates to the method of preparing said composition and to the use thereof as a parenterally-administered medicament for the treatment of cancer.
    Type: Application
    Filed: October 8, 2013
    Publication date: February 6, 2014
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Elie LEVERD, Joel BOUGARET, Marie-Dominique IBARRA
  • Publication number: 20140030351
    Abstract: The present disclosure relates in part to pharmaceutical compositions comprising polymeric nanoparticles having certain glass transition temperatures. Other aspects of the invention include methods of making such nanoparticles.
    Type: Application
    Filed: September 27, 2013
    Publication date: January 30, 2014
    Applicant: BIND Therapeutics, Inc.
    Inventors: Stephen E. Zale, Greg Troiano, Mir Mukkaram Ali, Jeff Hrkach, James Wright
  • Patent number: 8633221
    Abstract: A method of enhancing the activity of lysosomal ?-Galactosidase A (?-Gal A) in mammalian cells and for treatment of Fabry disease by administration of 1-deoxy-galactonojirimycin and related compounds.
    Type: Grant
    Filed: November 23, 2009
    Date of Patent: January 21, 2014
    Assignee: Mount Sinai School of Medicine of New York University
    Inventors: Jian-Qiang Fan, Satoshi Ishii
  • Patent number: 8569328
    Abstract: Pain and/or neurological disorders may be treated by administering a therapeutically effective amount of dextromethorphan and a therapeutically effective amount of a compound such as tilidine that inhibits the cytochrome P450 isozyme CYP2D6, to a person in need thereof. The two compounds may be administered separately, or in a single dosage form or composition as described herein.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: October 29, 2013
    Assignee: Antecip Bioventures II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 8551456
    Abstract: A combination therapy for treating a bacterial biofilm comprises a therapeutically effective amount of an antibiotic comprising an aminoglycoside or tetracycline, or a combination of two or more thereof, and a cationic porphyrin in an amount effective for enhancing the effectiveness of the antibiotic in treating the bacterial biofilm. A method of treating a bacterial biofilm comprising Pseudomonas aeruginosa comprises contacting the bacterial biofilm with a combination therapy comprising a therapeutically effective amount of an antibiotic, and a cationic porphyrin in an amount effective for enhancing the effectiveness of the antibiotic in treating the bacterial biofilm. A method of treating a bacterial biofilm comprising Pseudomonas aeruginosa in a patient comprises administering to the patient a combination therapy comprising a therapeutically effective amount of an antibiotic, and a cationic porphyrin in an amount effective for enhancing the effectiveness of the antibiotic in treating the bacterial biofilm.
    Type: Grant
    Filed: March 4, 2011
    Date of Patent: October 8, 2013
    Assignee: University of Dayton
    Inventors: Jayne Robinson, Tracy Collins
  • Publication number: 20130217672
    Abstract: A (+)-3-hydroxymorphinan-based polycycle derivative of formula (I) is effective as a neuroprotective agent for neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, and ischemic stroke.
    Type: Application
    Filed: May 13, 2011
    Publication date: August 22, 2013
    Applicant: GREEN CROSS CORPORATION
    Inventors: Jinhwa Lee, Jong Yup Kim, Jeongmin Kim, Kwang Woo Ahn
  • Publication number: 20130210803
    Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b]indoles and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: February 18, 2011
    Publication date: August 15, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Patent number: 8399502
    Abstract: Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2?-diindolylmethane, 2?,3-diindolylmethane, and 3,3?-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: March 19, 2013
    Assignee: SRI International
    Inventors: Ling Jong, Faming Jiang, Gaoquan Li, Kristien Mortelmans
  • Publication number: 20130053363
    Abstract: [Problem] To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like. [Measures for Solution] The present inventors examined compounds having PDE4B inhibitory activity and found that a tricyclic or tetracyclic imidazo[1,2-a]pyridine derivative or salts thereof had a superior PDE4B inhibitory activity, thereby completing the present invention. The imidazo[1,2-a]pyridine derivative can be used as an agent for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.
    Type: Application
    Filed: October 26, 2012
    Publication date: February 28, 2013
    Applicant: Astellas Pharma Inc.
    Inventor: Astellas Pharma Inc.
  • Publication number: 20130005666
    Abstract: The NF-E2-related factor 2 (Nrf2) is a key transcriptional regulator of antioxidant defense and detoxification. To directly monitor stabilization of Nrf2 we fused its Neh2 domain, responsible for the interaction with its nucleocytoplasmic regulator, Keap1, to firefly luciferase (Neh2-luciferase). It is shown herein that Neh2 domain is sufficient for recognition, ubiquitination and proteasomal degradation of Neh2-luciferase fusion protein. The novel Neh2-luc reporter system allows direct monitoring of the adaptive response to redox stress and classification of drugs based on the time-course of reporter activation. The novel reporter was used to screen a library of compounds to identify activators of Nrf2. The most robust and yet non toxic Nrf2 activators found—nordihydroguaiaretic acid, fisetin, and gedunin-induced astrocyte-dependent neuroprotection from oxidative stress via an Nrf2-dependent mechanism.
    Type: Application
    Filed: June 29, 2012
    Publication date: January 3, 2013
    Applicant: CORNELL UNIVERSITY
    Inventors: Rajiv RATAN, Irina GAZARYAN, Natalya A. SMIRNOVA
  • Patent number: 8343991
    Abstract: The present invention relates to anhydrous crystalline vinflunine salts obtained with 1 or 2 equivalents of a pharmaceutically acceptable mineral or organic acid [Acid] 1 or 2 in which [Acid] represents hydrobromic, sulfuric, lactic and fumaric acids for the group of water-soluble crystalline salts, and para-toluene sulfonic, benzoic, mandelic and para-hydroxy benzoic acids for the group of relatively insoluble crystalline salts.
    Type: Grant
    Filed: February 13, 2008
    Date of Patent: January 1, 2013
    Assignee: Pierre Fabre Medicament
    Inventors: Jean-Louis Maurel, Richard Pena, Jean-Paul Ribet
  • Patent number: 8318764
    Abstract: The present invention relates to the use of novel macrocyclic compounds of Formula I, wherein the variables Q, Q1, Q2, Q3, and Q4 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: November 27, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Alam Jahangir, Stephen M Lynch, Michael Soth, Hanbiao Yang
  • Publication number: 20120289533
    Abstract: Manzamine compounds have been discovered to decrease cell dissociation and cell migration associated with the metastatic potential of cancer cells and a restoration of cancer cell susceptibility to agents, such as TRAIL, which can induce apoptosis. Specifically, Manzamine A has a formerly unrecognized utility in both blocking tumor cell invasion and tumor metastasis as well in restoring cancer cell susceptibility to standard chemotherapeutic agents which induce apoptosis and, therefore, has utility in treating cancer.
    Type: Application
    Filed: July 17, 2012
    Publication date: November 15, 2012
    Inventors: Esther A. Guzman, Jacob D. Johnson, Amy E. Wright