Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 546/23)
-
Publication number: 20140088305Abstract: The present invention relates to organic electroluminescent devices which comprise heteroaromatic compounds.Type: ApplicationFiled: May 7, 2012Publication date: March 27, 2014Applicant: Merck Patent GmbHInventors: Amir Hossain Parham, Arne Buesing, Christof Pflumm, Teresa Mujica-Fernaud, Philipp Toessel, Thomas Eberle
-
Publication number: 20140080788Abstract: 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: ApplicationFiled: April 27, 2012Publication date: March 20, 2014Inventors: Jeffrey A. Robl, Jun Li, Lawrence J. Kennedy, Steven J. Walker, Haixia Wang, William N. Washburn, Saleem Ahmad, Khehyong Ngu
-
Patent number: 8674102Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins, nucleic acids and cellular organelles. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified to provide beneficial properties.Type: GrantFiled: January 3, 2013Date of Patent: March 18, 2014Assignee: Enzo Life Sciences, Inc.Inventors: Praveen Pande, Zaiguo Li, Maciej Szczepanik, Wayne Forrest Patton
-
Publication number: 20140051666Abstract: In part, the present disclosure is directed to prodrug derivatives of (E)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1, 8-naphthyridin-3-yl)acrylamide compounds with significant solubility and bioavailability profiles.Type: ApplicationFiled: August 26, 2013Publication date: February 20, 2014Applicant: AFFINIUM PHARMACEUTICALS, INC.Inventors: John J. Partridge, John Colucci, Yves Gareau, Michel Therien, Robert Zamboni, Barry Hafkin, Anthony Marfat, Helmi Zaghdane
-
Publication number: 20140046065Abstract: The present invention provides novel ruthenium based catalysts, and a process for preparing amines, by reacting a primary alcohol and ammonia in the presence of such catalysts, to generate the amine and water. According to the process of the invention, primary alcohols react directly with ammonia to produce primary amines and water in high yields and high turnover numbers. This reaction is catalyzed by novel ruthenium complexes, which are preferably composed of quinolinyl or acridinyl based pincer ligands.Type: ApplicationFiled: October 18, 2013Publication date: February 13, 2014Applicant: YEDA RESEARCH AND DEVELOPMENT CO. LTD.Inventors: David Milstein, Chidambaram Gunanathan
-
Publication number: 20140045793Abstract: 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: ApplicationFiled: October 18, 2013Publication date: February 13, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kenji OTSUBO, Takahito YAMAUCHI, Yuji OCHI
-
Publication number: 20140018320Abstract: 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 paiType: ApplicationFiled: July 11, 2013Publication date: January 16, 2014Applicant: Summit Corporation PLCInventors: 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: 8624029Abstract: The compounds of the subject invention are adjuvant molecules that comprise a imidazoquinoline molecule covalently linked to a phospho- or phosphonolipid group. The compounds of the invention have been shown to be inducers of interferon-a, IL-12 and other immunostimulatory cytokines and possess an improved activity profile in comparison to known cytokine inducers when used as adjuvants for vaccine antigens.Type: GrantFiled: October 23, 2009Date of Patent: January 7, 2014Assignee: GlaxoSmithKline Biologicals S.A.Inventor: David A. Johnson
-
Publication number: 20130336996Abstract: A conjugated compound of formula Q-Z—R4 wherein Q is a TLR7 and/or TLR8 agonist and Z—R4 is a lipid covalently linked to an amino acid or peptide coupled to a polyamine group, and a process for the manufacture of the conjugated compound, as well as a complex formed between the conjugated compound and a polyanionic molecule and a pharmaceutical composition containing the conjugated compound or complex. Also described is the use of the conjugated compound or complex in the treatment of infection, cancer or immune disorders or for use in vaccines.Type: ApplicationFiled: March 15, 2013Publication date: December 19, 2013Applicant: CAYLAInventors: Fabienne VERNEJOUL, Arnaud DEBIN, Daniel DROCOURT, Eric PEROUZEL, Gerard TIRABY, Thierry LIOUX
-
Publication number: 20130331359Abstract: 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: ApplicationFiled: April 6, 2011Publication date: December 12, 2013Applicant: BEIJING KONRUNS PHARMACEUTICAL CO., LTD.Inventors: Ziwei Yun, Hongtao Wang
-
Patent number: 8604201Abstract: The invention relates to the use of cyclovinyl phosphine compounds in the form of complexes with copper, as catalysts for reactions leading to the formation of carbon-carbon and carbon-heteroatom bonds. The invention also relates to complexes of copper with at least one cyclovinyl phosphine, as well as to the method for creating a carbon-carbon or a carbon-heteroatom bond catalysed by a cyclovinyl phosphine/copper complex.Type: GrantFiled: September 26, 2008Date of Patent: December 10, 2013Assignee: Centre National de Recherche Scientifique (C.N.R.S.)Inventors: Marc Taillefer, Hamid Kaddouri, Fouad Ouazzani
-
Patent number: 8592395Abstract: The present invention relates to compounds of Formula (I) and (Ia) useful in the treatment of CCR5-related diseases and disorders, for example, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).Type: GrantFiled: July 23, 2010Date of Patent: November 26, 2013Assignee: GlaxoSmithKline LLCInventors: Maosheng Duan, Wieslaw Mieczyslaw Kazmierski, Matthew Tallant
-
Patent number: 8586744Abstract: The invention is related to a method of treating disorders associated with hepatitis C by administering to an individual a pharmaceutical composition which comprises a therapeutically effective amount of an anti-viral phosphinate compound.Type: GrantFiled: October 27, 2010Date of Patent: November 19, 2013Assignee: Gilead Sciences, Inc.Inventors: Anthony Casarez, Kleem Chaudhary, Aesop Cho, Michael Clarke, Edward Doerffler, Maria Fardis, Choung U. Kim, Hyungjung Pyun, Xiaoning C. Sheng, Jianying Wang
-
Publication number: 20130303484Abstract: 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: ApplicationFiled: July 10, 2013Publication date: November 14, 2013Inventors: Peter D.J. Grootenhuis, Sara Hadida Ruah, Jinglan Zhou, Ann Hazlewood, Hayley Binch
-
Publication number: 20130296275Abstract: 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: ApplicationFiled: July 2, 2013Publication date: November 7, 2013Inventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi
-
Patent number: 8574881Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins and nucleic acids. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified by the addition of charged and polar groups to provide beneficial properties.Type: GrantFiled: June 17, 2009Date of Patent: November 5, 2013Assignee: Enzo Life Sciences, Inc.Inventors: Praveen Pande, Yuejun Xiang, Elazar Rabbani
-
Patent number: 8569484Abstract: Compounds of formula (IA) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: GrantFiled: May 28, 2010Date of Patent: October 29, 2013Assignee: Astrazeneca ABInventors: Neil Bifulco, Allison Laura Choy, Olga Quiroga, Brian Alan Sherer
-
Publication number: 20130274465Abstract: Immunopotentiators can be adsorbed to insoluble metal salts, such as aluminium salts, to modify their pharmacokinetics, pharmacodynamics, intramuscular retention time, and/or immunostimulatory effect. Immunopotentiators are modified to introduce a moiety, such as a phosphonate group, which can mediate adsorption. These modified compounds can retain or improve their in vivo immunological activity even when delivered in an adsorbed form.Type: ApplicationFiled: September 1, 2011Publication date: October 17, 2013Applicants: IRM LLC, NOVARTIS AGInventors: Manmohan Singh, David A.G. Skibinski, Tom Yao-Hsiang Wu, Yongkai Li, Alex Cortez, Xiaoyue Zhang, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan, Kathy Yue
-
Publication number: 20130253185Abstract: The present invention provides novel compounds and ligands that are useful in transition metal catalyzed cross-coupling reactions. For example, the compounds and ligands of the present invention are useful in palladium or gold catalyzed cross-coupling reactions.Type: ApplicationFiled: November 17, 2011Publication date: September 26, 2013Applicant: Dalhousie UniversityInventors: Rylan J. Lundgren, Mark Stradiotto
-
Patent number: 8541582Abstract: 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: GrantFiled: April 13, 2012Date of Patent: September 24, 2013Assignee: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im
-
Publication number: 20130244983Abstract: 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120 (Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and N,N-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.Type: ApplicationFiled: May 13, 2013Publication date: September 19, 2013Applicant: China Medical UniversityInventors: Sheng-Chu KUO, Che-Ming TENG, Kuo-Hsiung LEE, Li-Jiau HUANG, Li-Chen CHOU, Chih-Shiang CHANG, Chung-Ming SUN, Tian-Shung WU, Shiow-Lin PAN, Tzong-Der WAY, Jang-Chang LEE, Jing-Gung CHUNG, Jai-Sing YANG, Chien-Ting CHEN, Ching-Che HUANG, Shih-Ming HUANG
-
Publication number: 20130245006Abstract: The invention relates to indolizine derivatives of general formula (I), where A, B, m, W, n and R2 are as defined in claim 1, as well as to the method for preparing same and to the therapeutic use thereof.Type: ApplicationFiled: November 16, 2011Publication date: September 19, 2013Applicant: SANOFIInventors: Jean-Michel Altenburger, Franck Caussanel, Sergio Mallart, Marie-Claire Philippo-Orts
-
Patent number: 8513418Abstract: 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: GrantFiled: April 13, 2012Date of Patent: August 20, 2013Assignee: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im
-
Publication number: 20130209994Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins, nucleic acids and cellular organelles. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified to provide beneficial properties.Type: ApplicationFiled: January 3, 2013Publication date: August 15, 2013Applicant: ENZO LIFE SCIENCES, INC.Inventor: ENZO LIFE SCIENCES, INC.
-
Publication number: 20130203978Abstract: The invention provides a compound of formula (I), wherein R1-R6 and X have any of the values described, as well as pharmaceutical compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.Type: ApplicationFiled: January 29, 2013Publication date: August 8, 2013Applicant: Regents of the University of MinnesotaInventor: Regents of the University of Minnesota
-
Publication number: 20130203703Abstract: 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: ApplicationFiled: October 11, 2011Publication date: August 8, 2013Applicant: Immunahr ABInventor: Lars Pettersson
-
Publication number: 20130183701Abstract: The present invention provides fluorogenic substrates and methods of use in detecting and analyzing phospholipase C isozyme (PLC) activity.Type: ApplicationFiled: June 7, 2011Publication date: July 18, 2013Inventors: Qisheng Zhang, Wei Gang Huang, John Sondek, Stephanie Hicks
-
Patent number: 8481742Abstract: 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: GrantFiled: March 13, 2012Date of Patent: July 9, 2013Assignee: Kaneq Pharma Inc.Inventors: John Colucci, Marie-Claire Wilson, Yongxin Han, Claude Dufresne, Michel Belley, Cheuk K. Lau, Christopher Bayly
-
Publication number: 20130150330Abstract: 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: ApplicationFiled: June 13, 2012Publication date: June 13, 2013Applicant: UNIVERSITY OF KANSASInventors: Stefano A. Pogany, Mehmet Tanol, Michael J. Baltezor
-
Publication number: 20130150310Abstract: 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: ApplicationFiled: February 7, 2013Publication date: June 13, 2013Applicant: ARQULE, INC.Inventor: ARQULE, INC.
-
Publication number: 20130150583Abstract: Methods of making a chiral phosphorus compound of formula (X) are disclosed: wherein R1, R2, R3 are chiral or achiral groups selected from the list consisting of substituted or unsubstituted straight-chain, branched-chain or cyclic aliphatic or aromatic groups and in which the pair R1/R2 may be interconnected to form a ring.Type: ApplicationFiled: February 6, 2013Publication date: June 13, 2013Applicant: JOHNSON MATTHEY PUBLIC LIMITED COMPANYInventor: Johnson Matthey Public Limited Company
-
Publication number: 20130131018Abstract: 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: ApplicationFiled: June 1, 2011Publication date: May 23, 2013Applicant: Exonhit S.A.Inventors: Bertrand Leblond, Thierry Taverne, Eric Beausoleil, Cédric Chauvignac, Anne-Sophie Casagrande, Laurent Desire
-
Patent number: 8440692Abstract: 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120 (Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and ?/, ?/-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.Type: GrantFiled: December 7, 2007Date of Patent: May 14, 2013Assignee: China Medical UniversityInventors: Sheng-Chu Kuo, Che-Ming Teng, Kuo-Hsiung Lee, Li-Jiau Huang, Li-Chen Chou, Chih-Shiang Chang, Chung-Ming Sun, Tian-Shung Wu, Shiow-Lin Pan, Tzong-Der Way, Jang-Chang Lee, Jing-Gung Chung, Jai-Sing Yang, Chien-Ting Chen, Ching-Che Huang, Shih-Ming Huang
-
Patent number: 8426388Abstract: A compound of the formula is disclosed as a prodrug of an HIV protease inhibitor. Methods and compositions for inhibiting HIV protease activity and treating HIV infection are also disclosed.Type: GrantFiled: April 7, 2010Date of Patent: April 23, 2013Assignee: AbbVie Inc.Inventors: David A. DeGoey, William J. Flosi, David J. Grampovnik, Larry L. Klein, Dale J. Kempf, Xiu C. Wang
-
Patent number: 8415348Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.Type: GrantFiled: July 28, 2009Date of Patent: April 9, 2013Assignee: Pierre Fabre MedicamentInventors: Frédéric Marion, Jean-Philippe Annereau, Jacques Fahy
-
Patent number: 8404843Abstract: The present invention relates to novel chiral phosphorus compounds which can be readily prepared from quinoline derivatives as inexpensive starting compounds and have the general formula (I) wherein R1, R2, R3, R4, R5 are chiral or achiral organic residues which are derived from substituted or unsubstituted straight or branched chain or cyclic aliphatic or aromatic groups and which, in the case of the pairs R1/R2 and R4/R5, may be interconnected. Further, the invention relates to methods for the synthesis of chiral phosphorus compounds of general formula (I) and their use as catalyst components in processes for the preparation of optically active products.Type: GrantFiled: June 25, 2012Date of Patent: March 26, 2013Assignee: Johnson Matthey Public Limited CompanyInventors: Brian Adger, Alan Dyke, Giancarlo Francio, Frederick Ernest Hancock, Walter Leitner, Thomas Pullmann, Andreas Seger, Antonio Zanotti-Gerosa
-
Publication number: 20130071936Abstract: The present invention is directed to an indicator for targeting zinc(II) ions in a composition, e.g., a biological sample such as for targeting mitochondrial zinc (II) ions. The present invention is directed to a method for preparing an indicator that targets mitochondrial zinc(II), and a method of measuring the concentration of mitochondrial zinc(II) ions.Type: ApplicationFiled: September 17, 2012Publication date: March 21, 2013Applicant: The Florida State University Research Foundation, Inc.Inventor: The Florida State University Research Foundation,
-
Publication number: 20130053347Abstract: The present invention relates to the biology and mechanism of action of the naturally occurring compound Narciclasine, especially as an anti-cancer agent for brain tumors. The invention provides new insights on the target molecule of Amaryllidaceae isocarbostyril derivatives as for example Narciclasine and provides new prodrugs of these Amaryllidceae isocabostyril constituents for treating cancer, specifically cancers or tumors located in the brain.Type: ApplicationFiled: May 3, 2010Publication date: February 28, 2013Applicant: Universite Libre de BruxellesInventors: Veronique Mathieu, Gwendoline Van Goietsenoven, Jacques Dubois, Florence Lefranc-Kiss, Laurent Ingrassia, Robert Kiss
-
Publication number: 20130053348Abstract: 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: ApplicationFiled: September 12, 2012Publication date: February 28, 2013Inventors: 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: 20130040914Abstract: Compounds of Formula I are described: (I), wherein RP and RQ are defined herein. The compounds transcriptase, the prophylaxis and treatment of infection by HIV, and the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: April 4, 2011Publication date: February 14, 2013Inventors: Samson M. Jolly, Neville Anthony, Robert Gomez, David C. Dubost, Rick G. Woodward
-
Publication number: 20130035482Abstract: Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.Type: ApplicationFiled: October 12, 2012Publication date: February 7, 2013Applicant: WARNER CHILCOTT COMPANY, LLCInventor: WARNER CHILCOTT COMPANY, LLC
-
Patent number: 8362250Abstract: The present invention provides dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins, nucleic acids and cellular organelles. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes provided in this invention can comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been substituted with specific groups to provide beneficial properties.Type: GrantFiled: September 21, 2009Date of Patent: January 29, 2013Assignee: Enzo Biochem, Inc.Inventors: Praveen Pande, Hilary J. Cox, Yuejun Xiang, Wayne Forrest Patton
-
Patent number: 8357801Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins, nucleic acids and cellular organelles. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified to provide beneficial properties.Type: GrantFiled: December 4, 2008Date of Patent: January 22, 2013Assignee: Enzo Life Sciences, Inc.Inventors: Praveen Pande, Zaiguo Li, Maciej Szczepanik, Wayne F. Patton
-
Publication number: 20130004518Abstract: 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: ApplicationFiled: September 11, 2012Publication date: January 3, 2013Applicant: 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: 20130005675Abstract: 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: ApplicationFiled: September 14, 2012Publication date: January 3, 2013Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kenji OTSUBO, Takahito YAMAUCHI, Yuji OCHI
-
Publication number: 20120295877Abstract: The present invention relates to compounds of Formula (I) and (Ia) useful in the treatment of CCR5-related diseases and disorders, for example, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).Type: ApplicationFiled: July 23, 2010Publication date: November 22, 2012Inventors: Maosheng Duan, Wieslaw Mieczyslaw Kazmierski, Matthew Tallant
-
Publication number: 20120264940Abstract: The present invention relates to novel chiral phosphorus compounds which can be readily prepared from quinoline derivatives as inexpensive starting compounds and have the general formula (I) wherein R1, R2, R3, R4, R5 are chiral or achiral organic residues which are derived from substituted or unsubstituted straight or branched chain or cyclic aliphatic or aromatic groups and which, in the case of the pairs R1/R2 and R4/R5, may be interconnected. Further, the invention relates to methods for the synthesis of chiral phosphorus compounds of general formula (I) and their use as catalyst components in processes for the preparation of optically active products.Type: ApplicationFiled: June 25, 2012Publication date: October 18, 2012Applicant: JOHNSON MATTHEY PUBLIC LIMITED COMPANYInventors: Brian Adger, Alan Dyke, Giancarlo Francio, Frederick Ernest Hancock, Walter Leitner, Thomas Pullmann, Andreas Seger, Antonio Zanotti-Gerosa
-
Publication number: 20120263670Abstract: The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.Type: ApplicationFiled: June 29, 2011Publication date: October 18, 2012Applicant: Ardelyx, Inc.Inventors: Dominique Charmot, Jeffrey W. Jacobs, Michael Robert Leadbetter, Marc Navre, Christopher Carreras, Noah Bell
-
Publication number: 20120264716Abstract: 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: ApplicationFiled: April 13, 2012Publication date: October 18, 2012Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im
-
Publication number: 20120264715Abstract: 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: ApplicationFiled: April 13, 2012Publication date: October 18, 2012Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im