Quinolinyl Or Isoquinolinyl (including Hydrogenated) Patents (Class 514/82)
  • Patent number: 9809574
    Abstract: Compounds of formula (I): wherein Het, R3, R4, R5, R7, R8, R9, T, p, p?, q, and q? are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Grant
    Filed: July 22, 2014
    Date of Patent: November 7, 2017
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: James Edward Paul Davidson, James Brooke Murray, I-Jen Chen, Claire Walmsley, Mark Dodsworth, Johannes W. G. Meissner, Paul Brough, Imre Fejes, János Tatai, Miklós Nyerges, András Kotschy, Zoltán Szlávik, Olivier Geneste, Arnaud Le Tiran, Thierry Le Diguarher, Jean-Michel Henlin, Jérôme-Benoît Starck, Anne-Françoise Guillouzic, Guillaume De Nanteuil
  • Publication number: 20150148313
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are Factor VIIa inhibitors which may be used as medicaments.
    Type: Application
    Filed: June 5, 2013
    Publication date: May 28, 2015
    Inventors: Xiaojun Zhang, Peter Glunz, Eldon Scott Priestley, James A. Johnson, Nicholas Ronald Wurtz, Vladimir Ladziata
  • Publication number: 20150141353
    Abstract: This invention relates to combinations of therapeutic molecules useful for treating hepatitis C virus infection. The present invention relates to methods, uses, dosing regimens, and compositions.
    Type: Application
    Filed: October 14, 2014
    Publication date: May 21, 2015
    Inventors: William E. Delaney, IV, John O. Link, Hongmei Mo, David W. Oldach, Adrian S. Ray, William J. Watkins, Cheng Yong Yang, Weidong Zhong
  • Patent number: 9029322
    Abstract: The present invention relates to a method for identifying a drug candidate for enhancing expression of p21cip1/waf1 in a human patient suffering from a medical condition that can be treated by enhancing expression of p21C?1/waf1. The method includes (a) providing a cell line comprising a nucleic acid sequence that comprises a p21cip1/waf1 promoter operationally ligated to a reporter domain; (b) exposing the cell line to a compound; and (c) identifying a compound that induces expression of the reporter domain. The compound that induces expression of the reporter domain is a drug candidate for treating a medical condition that can be treated by enhancing expression of p21cip1/waf1.
    Type: Grant
    Filed: June 5, 2008
    Date of Patent: May 12, 2015
    Assignee: Cornell University
    Inventors: Rajiv R. Ratan, Brett C. Langley, Brian S. Ko
  • Publication number: 20150119365
    Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Application
    Filed: December 29, 2014
    Publication date: April 30, 2015
    Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
  • Publication number: 20150057220
    Abstract: Fused aromatic phosphonates of structural formula I are precursors to inhibitors of protein tyrosine phosphatase-1B (PTP-1B). The compounds of the present invention are therefore useful for the treatment in a mammal of a disorder, condition, or disease responsive to inhibition of protein tyrosine phosphatase-1B, including Type 2 diabetes, insulin resistance, a lipid disorder, obesity, Metabolic Syndrome, and cancer.
    Type: Application
    Filed: April 16, 2013
    Publication date: February 26, 2015
    Inventors: Michel Therien, Yves Leblanc, Yongxin Han
  • Patent number: 8962598
    Abstract: The present invention relates to compounds which are 1,2-dihydro-4-hydroxy-2-oxo-quinoline-3-carboxanilides, their thieno-pyridone analogs, and prodrugs thereof. This invention specifically relates to such derivatives containing an N-hydrogen in the carboxanilide moiety and which exhibit modulating activity towards the aromatic hydrocarbon receptor (AhR), and, specifically, also to prodrugs thereof. The present invention also relates to use of said compounds as a medicament, and for the treatment of cancer, autoimmune disorders and other disorders with an immunological component, and a pharmaceutical composition comprising one or more of said compounds and a method of treatment.
    Type: Grant
    Filed: October 11, 2011
    Date of Patent: February 24, 2015
    Assignee: Immunahr AB
    Inventor: Lars Pettersson
  • Publication number: 20150045325
    Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
    Type: Application
    Filed: October 28, 2014
    Publication date: February 12, 2015
    Applicant: Kaneq Pharma Inc.
    Inventors: John Colucci, Marie-Claire Wilson, Yongxin Han, Claude Dufresne, Michel Belley, Cheuk K. Lau, Christopher Bayly
  • Publication number: 20150031648
    Abstract: Compounds of formula (I): wherein X, Y, A1, A2, Ra, Rb, Rc, Rd, R3, R4, T and R5 are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Application
    Filed: July 22, 2014
    Publication date: January 29, 2015
    Inventors: Arnaud LE TIRAN, Thierry LE DIGUARHER, Jérôme-Benoît STARCK, Jean-Michel HENLIN, Anne-Françoise GUILLOUZIC, Guillaume DE NANTEUIL, Olivier GENESTE, James Edward Paul DAVIDSON, James Brooke MURRAY, I-Jen CHEN
  • Publication number: 20140274960
    Abstract: The present invention provides compounds of Formula (I) or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 18, 2014
    Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
  • Publication number: 20140243289
    Abstract: The present invention relates to prodrugs of modulators of ABC transporters, particularly, CFTR modulators, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: May 2, 2014
    Publication date: August 28, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Peter D.J. Grootenhuis, Sara Hadida Ruah, Jinglan Zhou, Anna Hazlewood, Hayley Binch
  • Publication number: 20140200199
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Application
    Filed: March 17, 2014
    Publication date: July 17, 2014
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi Moussa, Neru Munshi
  • Publication number: 20140179634
    Abstract: The present invention relates to substituted indole derivatives, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 3, 2014
    Publication date: June 26, 2014
    Applicant: NOVARTIS AG
    Inventors: Nigel Graham COOKE, Rita RAMOS, Karen KAMMERTOENS, Maurice VAN EIS
  • Publication number: 20140162964
    Abstract: Disclosed is a new use for sphingosine-1-phosphate (S1P) receptor agonists in the treatment of progressive dementia or brain degenerative diseases.
    Type: Application
    Filed: December 2, 2013
    Publication date: June 12, 2014
    Applicant: NOVARTIS AG
    Inventors: Volker Brinkmann, Nicole Kaneider, Christian J. Wiedermann
  • Patent number: 8716265
    Abstract: The present invention relates to substituted 4-qinolinemethanols and pharmaceutical compositions thereof and methods of using the same for treating of malaria, tuberculosis, and other infectious diseases.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: May 6, 2014
    Assignee: Jenrin Discovery, Inc.
    Inventors: John F. McElroy, Robert J. Chorvat, David Nugiel
  • Publication number: 20140107074
    Abstract: The present disclosure is directed to compounds of the structure (X): wherein: n is 2 or 3; NHE has the structure wherein: R1 is H or —SO2—NR7R8—; R2 is selected from H, —NR7(CO)R8, —SO2—NR7R8— and —NR7R8; R3 is hydrogen; R7 is hydrogen; R8 is a bond linking to L; L is a polyalkylene glycol linker; and Core has the following structure: wherein: X is selected from the group consisting of a bond, —O—, —NH—, NHC(?O)—, —NHC(?O)NH— and —NHSO2—; and Y is selected from the group consisting of a bond, optionally substituted C1-6 alkylene, optionally substituted benzene, pyridinyl, a polyethylene glycol linker and —(CH2)1-6O(CH2)1-6—, and methods of using such compounds for the treatment of irritable bowel syndrome, chronic kidney disease and end-stage renal disease.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 17, 2014
    Applicant: Ardelyx, Inc.
    Inventors: Noah BELL, Christopher CARRERAS, Dominique CHARMOT, Jeffrey W. JACOBS, Michael Robert LEADBETTER, Marc NAVRE
  • Publication number: 20140100195
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Application
    Filed: October 5, 2012
    Publication date: April 10, 2014
    Inventors: Richard D. Caldwell, Kevin M. GUCKIAN, Gnanasambandam KUMARA VEL, Wen-Cherng LEE, Edward Yin-Shiang LIN, Xiaogao LlU, Bin MA, Daniel M. SCOTT, Zhan SHl, Jermaine THOMAS, Arthur G. TAVERAS, Guo Zhu ZHENG
  • Publication number: 20140080788
    Abstract: Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R3, R4, R4a, R5a, R5b, R5c, R5d, R5e, R6a, R6b, and R6c are defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
    Type: Application
    Filed: April 27, 2012
    Publication date: March 20, 2014
    Inventors: Jeffrey A. Robl, Jun Li, Lawrence J. Kennedy, Steven J. Walker, Haixia Wang, William N. Washburn, Saleem Ahmad, Khehyong Ngu
  • Patent number: 8658623
    Abstract: The present invention relates to novel substituted bicyclic methyl amine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: February 25, 2014
    Assignee: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im
  • Publication number: 20140051625
    Abstract: The present invention provides novel bisphosphonate conjugates, pharmaceutical compositions comprising bisphosphonate conjugates and methods of using such analogs in the treatment of bone cancer, bone-related diseases, bone infection, bone inflammation, and diseases of the soft tissues surrounding bones.
    Type: Application
    Filed: October 25, 2013
    Publication date: February 20, 2014
    Applicant: MBC Pharma, Inc.
    Inventors: Alexander Karpeisky, Shawn Patrick Zinnen
  • Patent number: 8653050
    Abstract: The present invention relates to novel phenyl bicyclic methyl amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: February 18, 2014
    Assignee: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im
  • Publication number: 20140045793
    Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 13, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Kenji OTSUBO, Takahito YAMAUCHI, Yuji OCHI
  • Patent number: 8637492
    Abstract: Novel molecular transporter compositions and their use for transporting bioactive substances into cells in living animals are disclosed. To afford in vivo delivery, the composition is covalently linked to the bioactive substance and the resultant composite structure is introduced into the subject. The transporter composition includes multiple guanidine moieties on a dendrimeric scaffold having a tri-functional core. The tri-functional core is a phosphorodiamidate or phosphoramide moiety.
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: January 28, 2014
    Assignee: Gene Tools, LLC
    Inventor: Yong-Fu Li
  • Publication number: 20140018320
    Abstract: There are disclosed compound of Formula (1): A1, A2, A3 and A4 which may be the same or different, represent N or CR1, X is a divalent group selected from O, S(O)n, C?W, NR4, NC(?O)R5 and CR6R7, W is O, S, NR20, Y is N or CR8, one of R4, R5, R6, R8, R9 and NR20 represents -L-R3, in which L is a single bond or a linker group, additionally, R1, R3-R9, which may be the same or different, independently represent hydrogen or a substituent and R20 represents hydrogen, hydroxyl, alkyl optionally substituted by aryl, alkoxy optionally substituted by aryl, aryl, CN, optionally substituted alkoxy, optionally substituted aryloxy, optionally substitute alkanoyl, optionally substituted aroyl, NO2, NR30R31, in which R30 and R31, which may be the same or different, represent hydrogen, optionally substituted alkyl or optionally substituted aryl; additionally, one of R30 and R31 may represent optionally substituted alkanoyl or optionally substituted aroyl, n represents an integer from 0 to 2, in addition, when an adjacent pai
    Type: Application
    Filed: July 11, 2013
    Publication date: January 16, 2014
    Applicant: Summit Corporation PLC
    Inventors: GRAHAM MICHAEL WYNNE, STEPHEN PAUL WREN, PETER DAVID JOHNSON, PAUL DAMIEN PRICE, OLIVIER DE MOOR, GARY NUGENT, RICHARD STORER, RICHARD JOSEPH PYE, COLIN RICHARD DORGAN
  • Patent number: 8629126
    Abstract: Disclosed are quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; —N(R0)C(O)-lower alkylene-CO2R0, lower alkylene-CO2R0, lower alkenylene-CO2R0, —O-lower alkylene-CO2R0, —O-(lower alkylene which may be substituted with —CO2R0)-aryl or —O-lower alkenylene-CO2R0 (wherein R0 is H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof, has excellent P2Y12 inhibitory activity. The quinolone derivatives have excellent platelet aggregation inhibitory activity. A method of using the compounds is also disclosed.
    Type: Grant
    Filed: February 2, 2012
    Date of Patent: January 14, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Yuji Koga, Takao Okuda, Susumu Watanuki, Takashi Kamikubo, Fukushi Hirayama, Hiroyuki Moritomo, Jiro Fujiyasu, Michihito Kageyama, Toshio Uemura, Jun Takasaki
  • Publication number: 20130338108
    Abstract: The present invention relates to novel phenyl bicyclic methyl amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: July 8, 2013
    Publication date: December 19, 2013
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im
  • Publication number: 20130338109
    Abstract: The present invention relates to novel substituted bicyclic methyl amine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: July 16, 2013
    Publication date: December 19, 2013
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im
  • Patent number: 8609638
    Abstract: The invention provides compounds, compositions, and methods for studying the Rohmer pathway and for treating bacterial infections or parasitic infections. The parasitic infection can be a protozoan infection, such as malaria. The compounds and compositions can also be used as antibiotics, for example, to kill bacteria or parasites, or to inhibit bacterial or parasite growth. The invention further provides inhibitors of isoprenoid biosynthesis enzymes, and methods of inhibiting the activity of isoprenoid biosynthesis enzymes. The compounds can be, for example, alkynes or allenes that bind to a unique Fe of an Fe4S4 cluster of an isoprenoid biosynthesis enzyme.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: December 17, 2013
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Eric Oldfield, Ke Wang, Weixue Wang, Yonghui Zhang
  • Publication number: 20130331359
    Abstract: Phosphorus-containing group-substituted quinolines of formula (I) are provided in the present invention. The preparation process and application of the compound, and formulation comprising phosphorus-containing group-substituted quinolines are also disclosed. The compounds are protein kinase inhibitor and can be used for treating protein kinase abnormal activity-associated diseases, such as tumor, etc.
    Type: Application
    Filed: April 6, 2011
    Publication date: December 12, 2013
    Applicant: BEIJING KONRUNS PHARMACEUTICAL CO., LTD.
    Inventors: Ziwei Yun, Hongtao Wang
  • Publication number: 20130303484
    Abstract: The present invention relates to prodrugs of modulators of ABC transporters, particularly, CFTR modulators, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: July 10, 2013
    Publication date: November 14, 2013
    Inventors: Peter D.J. Grootenhuis, Sara Hadida Ruah, Jinglan Zhou, Ann Hazlewood, Hayley Binch
  • Publication number: 20130296275
    Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:
    Type: Application
    Filed: July 2, 2013
    Publication date: November 7, 2013
    Inventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi
  • Publication number: 20130231306
    Abstract: Compounds of Formula 1, as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.
    Type: Application
    Filed: January 25, 2013
    Publication date: September 5, 2013
    Applicant: OSI Pharmaceuticals, LLC
    Inventors: Andrew P. CREW, Dan Sherman, Rama Devi Appari, Xin Chen, Ramesh Chilukuri, Hanqing Dong, Caterina Ferraro, Kenneth Foreman, Ramesh C. Gupta, An-Hu Li, Kathryn M. Stolz, Brian Volk, Robert Zahler
  • Publication number: 20130203703
    Abstract: The present invention relates to compounds which are 1,2-dihydro-4-hydroxy-2-oxo-quinoline-3-carboxanilides, their thieno-pyridone analogs, and prodrugs thereof. This invention specifically relates to such derivatives containing an N-hydrogen in the carboxanilide moiety and which exhibit modulating activity towards the aromatic hydrocarbon receptor (AhR), and, specifically, also to prodrugs thereof. The present invention also relates to use of said compounds as a medicament, and for the treatment of cancer, autoimmune disorders and other disorders with an immunological component, and a pharmaceutical composition comprising one or more of said compounds and a method of treatment.
    Type: Application
    Filed: October 11, 2011
    Publication date: August 8, 2013
    Applicant: Immunahr AB
    Inventor: Lars Pettersson
  • Publication number: 20130157980
    Abstract: The present invention relates to substituted indole derivatives, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Application
    Filed: May 15, 2012
    Publication date: June 20, 2013
    Applicant: NOVARTIS AG
    Inventors: Nigel Graham COOKE, Rita RAMOS, Karen KAMMERTOENS, Maurice VAN EIS
  • Publication number: 20130150330
    Abstract: A compound can include a structure having decoquinate coupled to a prodrug moiety, or derivative or isomer or pharmaceutically acceptable salt thereof. The compound can be a decoquinate prodrug. The decoquinate prodrug can have a structure of any of the formulae described herein. The decoquinate prodrug can be synthesized in any manner, such as a synthetic method that includes Scheme 1A or Scheme 1B and Schemes 2, 3, and/or 4. The decoquinate prodrug can be prepared into a pharmaceutical composition with a pharmaceutically acceptable carrier, such as an aqueous composition. The decoquinate prodrug can be used for inhibiting or treating a parasitic infection, such as a malarial infection or a coccidian infection.
    Type: Application
    Filed: June 13, 2012
    Publication date: June 13, 2013
    Applicant: UNIVERSITY OF KANSAS
    Inventors: Stefano A. Pogany, Mehmet Tanol, Michael J. Baltezor
  • Publication number: 20130150310
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Application
    Filed: February 7, 2013
    Publication date: June 13, 2013
    Applicant: ARQULE, INC.
    Inventor: ARQULE, INC.
  • Publication number: 20130131018
    Abstract: The present invention relates generally to substituted isoquinolines and their use as tubulin polymerization inhibitors. In particular, the invention relates to substituted isoquinolines which possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.
    Type: Application
    Filed: June 1, 2011
    Publication date: May 23, 2013
    Applicant: Exonhit S.A.
    Inventors: Bertrand Leblond, Thierry Taverne, Eric Beausoleil, Cédric Chauvignac, Anne-Sophie Casagrande, Laurent Desire
  • Publication number: 20130108605
    Abstract: A method of supplementing a diet and ameliorating oxidative stress in a mammal includes administering a pharmaceutically effective amount of lipid soluble, hydrophobic active compounds having a chemical structure: wherein R1 is an aromatic backbone and R2 is a sulfur containing ligand. Through formation of disulfide linkages other moieties can be attached to R2 converting the hydrophobic base into a water soluble entity, for ease of delivery, which can be reconverted back to the original compound by biochemical reduction in the blood stream.
    Type: Application
    Filed: December 17, 2012
    Publication date: May 2, 2013
    Applicant: THE UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION
    Inventor: THE UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION
  • Publication number: 20130096089
    Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.
    Type: Application
    Filed: September 7, 2012
    Publication date: April 18, 2013
    Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
  • Publication number: 20130065857
    Abstract: The present invention generally concerns particular methods and compositions for antimicrobial therapy. In particular embodiments, the compositions target DXR. In specific embodiments, the compositions are electron-deficient heterocyclic rings.
    Type: Application
    Filed: October 12, 2010
    Publication date: March 14, 2013
    Applicant: Baylor College of Medicine
    Inventor: Yongcheng Song
  • Publication number: 20130053348
    Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.
    Type: Application
    Filed: September 12, 2012
    Publication date: February 28, 2013
    Inventors: Xiangping Qian, Chihyuan (Grace) Chuang, Pu-Ping Lu, Sing Yao, Qing (Kevin) Lu, Hong Jiang, Wenyue Wang, Bradley P. Morgan, David J. Morgans, JR.
  • Publication number: 20130018017
    Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, n, m and X have defined meanings.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 17, 2013
    Inventors: Jorge Eduardo VIALARD, Patrick René ANGIBAUD, Laurence Anne MEVELLEC, Christophe MEYER, Eddy Jean Edgard FREYNE, Isabelle Noëlle Constance PILATTE, Bruno ROUX, Elizabeth Thérèse Jeanne PASQUIER, Xavier Marc BOURDREZ, Christophe Denis ADELINET, Laurence Françoise Bernadette MARCONNET-DECRANE, Jacqueline Anne MACRITCHIE, James Edward Stewart DUFFY, Andrew Pate OWENS, Pierre-Henri STORCK, Virginie Sophie PONCELET
  • Publication number: 20130004518
    Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicant: Merck, Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
  • Publication number: 20120322766
    Abstract: The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of anthrax and other infections.
    Type: Application
    Filed: August 28, 2012
    Publication date: December 20, 2012
    Applicant: Morphochem Aktiengesellschaft fuer Kombinatorische Chemie
    Inventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Hans Locher, Christine Schmitt
  • Publication number: 20120264715
    Abstract: The present invention relates to novel substituted bicyclic methyl amine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: April 13, 2012
    Publication date: October 18, 2012
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im
  • Publication number: 20120264716
    Abstract: The present invention relates to novel phenyl bicyclic methyl amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: April 13, 2012
    Publication date: October 18, 2012
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im
  • Publication number: 20120178717
    Abstract: The present invention relates to substituted 4-qinolinemethanols and pharmaceutical compositions thereof and methods of using the same for treating of malaria, tuberculosis, and other infectious diseases.
    Type: Application
    Filed: November 18, 2011
    Publication date: July 12, 2012
    Applicant: JENRIN DISCOVERY
    Inventors: John F. McElroy, Robert J. Chorvat
  • Publication number: 20120178679
    Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
    Type: Application
    Filed: March 13, 2012
    Publication date: July 12, 2012
    Applicant: KANEQ PHARMA INC.
    Inventors: John COLUCCI, Marie-Claire WILSON, Yongxin HAN, Claude DUFRESNE, Michel BELLEY, Cheuk K. LAU, Christopher BAYLY
  • Publication number: 20120157371
    Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    Type: Application
    Filed: December 12, 2011
    Publication date: June 21, 2012
    Inventors: Chongxi YU, Lina Xu, Yuhua Chen, Binbing Yan, Shiqian Tu
  • Publication number: 20120142635
    Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:
    Type: Application
    Filed: February 8, 2012
    Publication date: June 7, 2012
    Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische Chemie
    Inventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi