Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 546/23)
  • Antiviral phosphinate compounds
    Patent number: 7893264
    Abstract: The invention is related to anti-viral phosphinate compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: July 6, 2007
    Date of Patent: February 22, 2011
    Assignee: 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
  • Indole compounds bearing aryl or heteroaryl groups having sphingosine 1-phosphate (S1P) receptor biological activity
    Patent number: 7888336
    Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as spingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: September 18, 2008
    Date of Patent: February 15, 2011
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
  • Derivatives of 1,2-dihydro-7-hydroxyquinolines Containing Fused Rings
    Publication number: 20110027800
    Abstract: The present invention describes novel dyes, including coumarins, rhodamines, and rhodols that incorporate additional fused aromatic rings. The dyes of the invention absorb at a longer wavelength than structurally similar dyes that do not possess the fused aromatic rings. Many of the dyes of the invention are useful fluorescent dyes. The invention includes chemically reactive dyes, dye-conjugates, and the use of such dyes in staining samples and detecting ligands or other analytes.
    Type: Application
    Filed: October 11, 2010
    Publication date: February 3, 2011
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Zhenjun DIWU, Jixiang Liu, Kyle Gee
  • Process for producing biphosphonic acids and forms thereof
    Patent number: 7872144
    Abstract: Disclosed herein is a process for producing bisphosphonic acids and salts thereof. The process comprising reacting a carboxylic acid of Formula [I] with phosphorous acid and halophosphorus compound in the presence of a solvent selected from aliphatic hydrocarbon or water miscible cyclic ether. Further, the present invention also provides novel forms of bisphosphonic acids and process for preparation thereof.
    Type: Grant
    Filed: June 13, 2005
    Date of Patent: January 18, 2011
    Assignee: Jubilant Organosys Limited
    Inventors: Satish Chandra Pandey, Hussain Haider, Sudhanshu Saxena, Manoj Kumar Singh, Rajesh Kumar Thaper, Sushil Kumar Dubey
  • HEPATITIS C VIRUS INHIBITORS
    Publication number: 20110008288
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: June 15, 2010
    Publication date: January 13, 2011
    Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Datong Tang, Ce Wang, Yao-Ling Qiu
  • Bisphosphonate Compounds and Methods for Bone Resorption Diseases, Cancer, Bone Pain, Immune Disorders, and Infectious Diseases
    Publication number: 20100316676
    Abstract: Bisphosphonate compounds and related methods of making and using are disclosed, including pyridinium-1-yl, quinolinium-1-yl, and related compounds. The activity of compounds is disclosed in the context of functional assays such as Leishmania major farnesyl diphosphate synthase (FPPS) inhibition, Dictyostelium discoideum growth inhibition, human gamma delta T cell activation, and bone resorption. The applicability of bisphosphonate compounds in the context of parasitic infections, for example against trypanosomes, is disclosed. Further potential applications of the invention are disclosed regarding the treatment of one or more conditions such as bone resorption disorders, cancer, bone pain, infectious diseases, and in immunotherapy.
    Type: Application
    Filed: June 28, 2010
    Publication date: December 16, 2010
    Inventors: John M. Sanders, Yongcheng Song, Julian M.W. Chan, Eric Oldfield, Yonghui Zhang
  • HETEROCYCLIC UREA DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20100317624
    Abstract: 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: Application
    Filed: June 7, 2010
    Publication date: December 16, 2010
    Inventors: Allison Laura CHOY, Ann EAKIN, Olga QUIROGA, Brian SHERER
  • Compounds Comprising A Cyclobutoxy Group
    Publication number: 20100292188
    Abstract: The present invention relates to compounds of formula (I) comprising a cyclobutoxy group, processes for preparing them, pharmaceutical compositions comprising said compounds and their use as pharmaceuticals.
    Type: Application
    Filed: January 22, 2009
    Publication date: November 18, 2010
    Applicant: UCB PHARMA S.A.
    Inventors: Frédéric Denonne, Sylvain Celanire, Anne Valade, Sabine Defays, Véronique Durieu
  • ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS
    Publication number: 20100261677
    Abstract: The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a medicament for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.
    Type: Application
    Filed: September 4, 2008
    Publication date: October 14, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Elke Langkopf, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
  • CHIRAL PHOSPHORUS COMPOUND
    Publication number: 20100240898
    Abstract: 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: Application
    Filed: October 1, 2007
    Publication date: September 23, 2010
    Applicant: JOHNSON MATTHEY PLC
    Inventors: Brian Adger, Alan Dyke, Giancarlo Francio, Frederick Emest Hancock, Walter Leitner, Thomas Pullmann, Andreas Seger, Antonio Zanotti-Gerosa
  • Indole Compounds Bearing Aryl or Heteroaryl Groups Having Sphingosine 1-Phosphate (S1P) Receptor Biological Activity
    Publication number: 20100240614
    Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as spingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: September 18, 2008
    Publication date: September 23, 2010
    Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
  • PHOSPHOTHIOPHENE AND PHOSPHOTHIAZOLE HCV POLYMERASE INHIBITORS
    Publication number: 20100233123
    Abstract: Provided herein are phosphothiophene and phosphothiazole compounds, for example, of any of Formulae I, IA, IIA, IIIA, IVA, VA, VIA, VIIA, IB, IIB, IIIB, IVB, VB, VIIB and VIIB disclosed herein, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host infected with HCV.
    Type: Application
    Filed: March 3, 2010
    Publication date: September 16, 2010
    Applicant: Idenix Pharmaceuticals, Inc.
    Inventors: Cyril Dousson, Claire Pierra, Jean-Francois Griffon, Frederic Leroy, Jean-Laurent Paparin, David Dukhan, Dominique Surleraux
  • COMPOSITIONS AND METHODS FOR CANCER TREATMENT
    Publication number: 20100227831
    Abstract: A novel composition of a phosphonoformic acid partial ester chemically linked to an anticancer compound of the general formula: wherein R1 is selected from the group consisting of methyl, alkyl, cholesteryl, aryl and aralkyl, R2 is selected from the group consisting of hydrogen, methyl, alkyl, and a water-soluble cation, Y is selected from the group consisting of oxygen, sulfur, carbon and nitrogen, and R3 is a cytotoxic agent. Methods for making and administering these compositions for treatment of cancer are also disclosed.
    Type: Application
    Filed: May 19, 2010
    Publication date: September 9, 2010
    Inventor: Jayanta Saha
  • Dyes linked to target molecules, oligonucleotides or polynucleotides comprising dye molecules, composite dyes and other compositions useful for detecting or quantifying desirable target molecules
    Publication number: 20100228008
    Abstract: 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: Application
    Filed: June 17, 2009
    Publication date: September 9, 2010
    Applicant: ENZO LIFE SCIENCES, INC. C/O ENZO BIOCHEM, INC.
    Inventors: Yuejun Xiang, Praveen Pande, Rajesh Khazanchi, Elazar Rabbani, Dakai Liu, Wei Cheng
  • Substituted Phosphonates and Their Use In Decreasing Amyloid Aggregates
    Publication number: 20100204183
    Abstract: The invention relates to novel and known substituted phosphonates for use in ameliorating amyloid aggregates, particularly for use in the treatment of Alzheimer's disease.
    Type: Application
    Filed: May 2, 2008
    Publication date: August 12, 2010
    Applicant: QUEEN MARY & WESTFIELD COLLEGE
    Inventors: Alice Sullivan, Adina Michael-Titus, Lesley Robson
  • LIGHT EMITTING DEVICE MATERIAL AND LIGHT EMITTING DEVICE
    Publication number: 20100187520
    Abstract: Disclosed is a light emitting device material characterized by containing a specific fluorine compound. This light emitting device material enables to obtain a light emitting device having high luminous efficiency, excellent color purity and excellent durability. Also disclosed is a light emitting device using such a light emitting device material.
    Type: Application
    Filed: July 16, 2008
    Publication date: July 29, 2010
    Applicant: Toray Industries, Inc.
    Inventors: Kazunori Sugimoto, Tsuyoshi Tominaga
  • QUINOLINONE DERIVATIVES AS PARP AND TANK INHIBITORS
    Publication number: 20100168065
    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: March 7, 2008
    Publication date: July 1, 2010
    Applicant: Janssen Pharmaceutica NV
    Inventors: Jorge Eduardo Vialard, Patrick René Angibaud, Laurence Anne Mevellec, Christophe Meyer, Eddy Jean Edgard Freyne, Isabelle Noëlle Pilatte, Bruno Roux, Elisabeth Thérèse Jeanne Pasquier, Xavier Marc Bourdrez, Christophe Denis Adelinet, Laurence Francoise Bernadette Marconnet-Decrane, Jacqueline Anne Macritchie, James Edward Stewart Duffy, Andrew Pate Owens, Pierre-Henri Storck, Virginie Sophie Poncelet
  • NOVEL HYDROPHILIC DERIVATIVES OF 2-ARYL-4-QUINOLONES AS ANTICANCER AGENTS
    Publication number: 20100168064
    Abstract: 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: Application
    Filed: December 7, 2007
    Publication date: July 1, 2010
    Applicant: China Medical University
    Inventors: 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
  • KINASE INHIBITORS
    Publication number: 20100160633
    Abstract: Compounds are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Application
    Filed: February 17, 2010
    Publication date: June 24, 2010
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Jason W. Brown, Qing Dong, Bheema R. Paraselli, Jeffrey A. Stafford, Xianchang Gong, Yan Liu, Nicholas Scorah, Michael B. Wallace
  • Heterobicyclic pyrazole compounds and methods of use
    Patent number: 7723330
    Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Grant
    Filed: March 6, 2007
    Date of Patent: May 25, 2010
    Assignees: Array BioPharma Inc., Genentech, Inc.
    Inventors: James F. Blake, Steven Armen Boyd, Jason De Meese, Kin Chiu Fong, John J. Gaudino, Tomas Kaplan, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian, Frederick Cohen, Wendy B. Young
  • Prodrugs of HIV protease inhibitors
    Patent number: 7718633
    Abstract: 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: Grant
    Filed: June 29, 2005
    Date of Patent: May 18, 2010
    Assignee: Abbott Laboratories
    Inventors: David A. DeGoey, William J. Flosi, David J. Grampovnik, Larry L. Klein, Dale J. Kempf, Xiu C. Wang
  • KINASE INHIBITORS
    Publication number: 20100120717
    Abstract: Compounds are provided for use with kinases that comprise a compound selected from the group consisting of formula (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture in comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Application
    Filed: October 8, 2007
    Publication date: May 13, 2010
    Inventors: Jason W. Brown, Qing Dong, Bheema R. Paraselli, Jeffrey A. Stafford, Michael B. Wallace, Hasanthi Wijesekera
  • Monophosphates as Mutual Prodrugs of Muscarinic Receptor Antagonists and Beta-Agonists for the Treatment of COPD And Chronic Bronchitis
    Publication number: 20100112061
    Abstract: A mutual prodrug of a MRA and a (?-agonist for formulation for delivery by aerosolization to inhibit pulmonary bronchoconstriction is described. The mutual prodrug is preferably formulated in a small volume solution (10-500 ?L) dissolved in a quarter normal saline having pH between 5.0 and 7.0 for the treatment of respiratory tract bronchoconstriction by an aerosol having mass median average diameter predominantly between 1 to 5?, produced by nebulization or by dry powder inhaler.
    Type: Application
    Filed: December 12, 2007
    Publication date: May 6, 2010
    Inventors: William Baker, Marcin Stasiak, Sundaramoorthi Swaminathan, Musong Kim
  • Synthesis of sodium narcistatin and related compounds
    Patent number: 7709643
    Abstract: The present invention involves use of the compounds narciclasine (2a) and 7-deoxy-narciclasine (2c), which are obtained via isolation from the medicinal plant species Narcissus (Amaryllidaceae), as precursors in a novel synthesis method in which each of these compounds are selectively hydrogenated to produce trans-dihydronarciclasine (1a) and 7-deoxy-trans-dihydronarciclasine (1c). Also described herein is a novel synthesis method for producing sodium narcistatin (11) from narciclasine (2a). Further described herein are certain novel 3,4-cyclic phosphate prodrugs, including sodium-7-deoxynarcistatin (8), sodium-7-deoxy-transdihydronarcistatin (9), and sodium transdihydronarcistatin (10).
    Type: Grant
    Filed: January 17, 2006
    Date of Patent: May 4, 2010
    Assignee: Arizona Board of Regents, a body corporate of the State of Arizona, Acting for and on Behalf of the Arizona State University
    Inventors: George R. Pettit, Noeleen Melody
  • Monophosphates as Mutual Prodrugs of Anti-Inflammatory Signal Transduction Modulators (AISTM's) and Beta-Agonists for the Treatment of Pulmonary Inflammation and Bronchoconstriction
    Publication number: 20100098641
    Abstract: A mutual prodrug of an AISTM and a ?-agonist in formulation for delivery by aerosolization to inhibit pulmonary inflammation and bronchoconstriction is described. The mutual prodrug is preferably formulated in a small volume solution (10-500 ?L) dissolved in a quarter normal saline having pH between about 5.0 and 7.0 for the treatment of respiratory tract inflammation and bronchoconstriction by an aerosol having mass median average diameter predominantly between about 1 to 5?, produced by nebulization or by dry powder inhaler.
    Type: Application
    Filed: December 12, 2007
    Publication date: April 22, 2010
    Inventors: William Baker, Marcin Stasiak, Sundaramoorthi Swaminathan, Musong Kim
  • METHOD OF PREPARING MONTELUKAST AND INTERMEDIATES USED THEREIN
    Publication number: 20100099876
    Abstract: The present invention relates to a method for preparing montelukast, an inhibitor against leukotrienes, and an intermediate used therein. According to the inventive method, high-purity montelukast or its sodium salt can be prepared in a high yield.
    Type: Application
    Filed: December 11, 2007
    Publication date: April 22, 2010
    Applicant: HANMI PHARM. CO., LTD.
    Inventors: Gwan Sun Lee, Young-Kil Chang, Jaeheon Lee, Chul Hyun Park, Eun-Ju Park, Jaeho Yoo
  • Novel fluorescent dyes and compounds, methods and kits useful for identifying specific organelles and regions in cells of interest
    Publication number: 20100068752
    Abstract: 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: Application
    Filed: September 21, 2009
    Publication date: March 18, 2010
    Inventors: Praveen Pande, Hilary J. Cox, Yuejun Xiang, Wayne Forrest Patton
  • FUSED AROMATIC PTP-1B INHIBITORS
    Publication number: 20100022477
    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: January 24, 2008
    Publication date: January 28, 2010
    Inventors: John Colucci, Marie-Claire Wilson, Yongxin Han, Claude Dufresne, Michel Belley, Cheuk K. Lau, Christopher Bayly
  • INTEGRASE INHIBITORS
    Publication number: 20090291921
    Abstract: Tricyclic compounds, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.
    Type: Application
    Filed: November 19, 2008
    Publication date: November 26, 2009
    Applicant: Gilead Sciences, Inc.
    Inventors: Salman Y. Jabri, Haolun Jin, Choung U. Kim, Jiayao Li, Samuel E. Metobo, Michael R. Mish
  • LIGAND-CONJUGATED MONOMERS
    Publication number: 20090286973
    Abstract: This invention relates composition and methods for making and using chemically modified oligonucleotides agents for inhibiting gene expression.
    Type: Application
    Filed: July 2, 2009
    Publication date: November 19, 2009
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah MANOHARAN, Venkitasamy KESAVAN, Kallanthottathil G. RAJEEV
  • Certain chemical entities, compositions, and methods
    Publication number: 20090275537
    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: August 11, 2008
    Publication date: November 5, 2009
    Inventors: Xiangping Qian, Chihyuan (Grace) Chuang, Pu-Ping Lu, Bing Yao, Qing (Kevin) Lu, Hong Jiang, Wenyue Wang, Bradley P. Morgan, David J. Morgans, JR.
  • QUINOLINONE FARNESYL TRANSFERASE INHIBITORS FOR THE TREATMENT OF SYNUCLEINOPATHIES AND OTHER INDICATIONS
    Publication number: 20090253655
    Abstract: Novel quinolinone farnesyl transferase inhibitors are provided. These new compounds are useful in the treatment or prevention of synucleinopathies, such as Parkinson's Disease, Diffuse Lewy Body Disease, multiple system atrophy, and disorders of brain iron concentration including pantothenate kinase-associated neurodegeneration (e.g., PANK1), or other neurodegenerative/neurological diseases. Provided compounds are also useful in the treatment of proliferative diseases such as cancer, and in the treatment of neurological diseases, such as cognitive impairment, depression, and anxiety. The treatment including administering to a subject a therapeutically effective amount of an inventive farnesyl transferase inhibitor compound.
    Type: Application
    Filed: March 12, 2009
    Publication date: October 8, 2009
    Inventors: Peter T. Lansbury, JR., Craig J. Justman, Ross A. Fredenburg, Robin Kate Meray, Mark E. Duggan, Peter Lin
  • Labeling of target molecules, identification of organelles and other applications, novel compositions, methods and kits
    Publication number: 20090226954
    Abstract: 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: Application
    Filed: December 4, 2008
    Publication date: September 10, 2009
    Inventors: Praveen Pande, Zaiguo Li, Maciej Szczepanik, Wayne F. Patton
  • Bone Targeted Therapeutics and Methods of Making and Using the Same
    Publication number: 20090227544
    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: March 30, 2009
    Publication date: September 10, 2009
    Applicant: MBC PHARMA, INC.
    Inventors: Alexander Karpeisky, Shawn Zinnen
  • KINASE INHIBITORS
    Publication number: 20090156557
    Abstract: Compounds are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Application
    Filed: April 15, 2008
    Publication date: June 18, 2009
    Applicant: TAKEDA SAN DIEGO, INC.
    Inventors: Jason W. Brown, Qing Dong, Bheema R. Paraselli, Jeffrey A. Stafford, Xianchang Gong, Yan Liu, Nicholas Scorah, Michael B. Wallace
  • Use of Dendrimers to Stimulate Cell Growth
    Publication number: 20090142316
    Abstract: The present invention relates to the use of dendrimers with monophosphonic or bisphosphonic terminations in order to stimulate the growth of cell cultures or to activate cells in culture.
    Type: Application
    Filed: July 29, 2005
    Publication date: June 4, 2009
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE M, RHODIA UK LIMITED
    Inventors: Jean-Pierre Majoral, Anne-Marie Jeannine Jacqueline Caminade, Jean-Jacques Fournie, Laurent Griffe, Mary Poupot-Marsan, Remy Poupot, Cedric-Olivier Turrin
  • PROCESS FOR MANUFACTURING BISPHOSPHONIC ACIDS
    Publication number: 20090137808
    Abstract: A manufacturing process for the preparation of bisphosphonic acids and in particular zoledronic acid is provided wherein diglyme, monoglyme, or a mixture thereof, is utilized to produce a homogenous, water soluble, solid reaction mass that upon cooling, dissolving in water and stripping results in a high purity product and comparatively good yield.
    Type: Application
    Filed: March 16, 2007
    Publication date: May 28, 2009
    Applicant: ALBEMARLE CORPORATION
    Inventors: Edward G. Samsel, Tse-Chong Wu
  • SYNTHESIS OF SODIUM NARCISTATIN AND RELATED COMPOUNDS
    Publication number: 20090131672
    Abstract: The present invention involves use of the compounds narciclasine (2a) and 7-deoxy-narciclasine (2c), which are obtained via isolation from the medicinal plant species Narcissus (Amaryllidaceae), as precursors in a novel synthesis method in which each of these compounds are selectively hydrogenated to produce trans-dihydronarciclasine (1a) and 7-deoxy-trans-dihydronarciclasine (1c). Also described herein is a novel synthesis method for producing sodium narcistatin (11) from narciclasine (2a). Further described herein are certain novel 3,4-cyclic phosphate prodrugs, including sodium-7-deoxynarcistatin (8), sodium-7-deoxy-transdihydronarcistatin (9), and sodium transdihydronarcistatin (10).
    Type: Application
    Filed: January 17, 2006
    Publication date: May 21, 2009
    Applicant: ARIZONA BOARD OF REGENTS acting on behalf of ARIZONA STATE UNIVERSITY
    Inventors: George R. Pettit, Noeleen Melody
  • AMIDE-SUBSTITUTED XANTHENE DYES
    Publication number: 20090093612
    Abstract: The present invention provides amide-substituted xanthene fluorescent dyes and reagent for the introduction of phosphonate or sulfo groups into the fluorescent dyes.
    Type: Application
    Filed: October 2, 2008
    Publication date: April 9, 2009
    Applicant: Epoch Biosciences, Inc.
    Inventor: Eugene Lukhtanov
  • Inhibitors of ?-lactamase
    Patent number: 7514556
    Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: July 30, 2007
    Date of Patent: April 7, 2009
    Assignee: Methylgene Inc.
    Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
  • NARCISTATIN PRODRUGS
    Publication number: 20090082569
    Abstract: The present invention provides prodrugs derived from the sparingly soluble anticancer isocarbostyril narciclasine, a component of various Narcissus species, said prodrugs having potential for use against animal and human cancers. Also disclosed is an efficient procedure for the synthetic conversion of narciclasine to several more soluble cyclic phosphate compounds, including “narcistatin”.
    Type: Application
    Filed: September 10, 2008
    Publication date: March 26, 2009
    Inventors: George R. Pettit, Noeleen Melody
  • Composition for treating bone disorders
    Publication number: 20090069272
    Abstract: Disclosed is a new composition of matter, substantially enantiomerically pure (1R,6S)-2-Azabicyclo-[4.3.0]nonane-8,8-diphosphonic acid, methods of preparing this new composition of matter, a pharmaceutical composition comprising the new composition, and administration of the composition in methods of treating bone disorders such as osteoporosis, osteolytic bone metastasis, rheumatoid arthritis and osteoarthritis.
    Type: Application
    Filed: December 11, 2007
    Publication date: March 12, 2009
    Applicant: The Procter & Gamble Company and University of Rochester
    Inventors: Frank Hallock Ebetino, Robert Kenneth Boeckman, JR., Xinyi Song
  • PHOSPHADIAZINE HCV POLYMERASE INHIBITORS I AND II
    Publication number: 20090060866
    Abstract: Provided herein are phosphadiazine polymerase inhibitor, for example, of any of Formula I, II, III, I?, II?, I?, II?, Ia, IIa, or IIIa, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
    Type: Application
    Filed: August 27, 2008
    Publication date: March 5, 2009
    Applicant: Idenix Pharmaceuticals, Inc.
    Inventors: Cyril Dousson, Dominique Surleraux, Arlene Roland, Claire Pierra, Daniel Da Costa
  • Novel inhibitors of chymase
    Publication number: 20090036409
    Abstract: The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.
    Type: Application
    Filed: August 20, 2008
    Publication date: February 5, 2009
    Inventors: Michael J. Hawkins, Michael N. Greco, Eugene Powell, Lawrence De Garavilla, Bruce E. Maryanoff
  • Pre-organized tricyclic integrase inhibitor compounds
    Publication number: 20090029939
    Abstract: Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. A1 and A2 are moieties forming a five, six, or seven membered ring. L is a bond or a linker connecting a ring atom of Ar to N. X is O, S, or substituted nitrogen. Ar is aryl or heteroaryl, Q is N, +NR, or CR4. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties covalently attached at any site.
    Type: Application
    Filed: May 25, 2007
    Publication date: January 29, 2009
    Inventors: James M. Chen, Xiaowu Chen, Maria Fardis, Haolun Jin, Choung U. Kim, Laura N. Schacherer
  • Prodrugs and methods of making and using the same
    Publication number: 20080318905
    Abstract: Prodrugs of parent drugs and methods of making and using the same are described. The prodrugs comprise an amine-containing parent drug moiety and a prodrug moiety, such as methoxyphosphonic acid or ethoxyphosphonic acid. The prodrugs may be employed in therapy for the treatment of various indications, such as pain, and in methods of decreasing the abuse potential of abuse-prone drugs and/or delaying the onset of parent drug activity and/or prolonging parent drug activity as compared to administration of a parent drug.
    Type: Application
    Filed: December 5, 2007
    Publication date: December 25, 2008
    Inventors: Naweed Muhammad, Keith R. Bley
  • Antiviral Compounds
    Publication number: 20080311077
    Abstract: The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: July 18, 2005
    Publication date: December 18, 2008
    Inventors: Kleem Chaudhary, Melissa Fleury, Choung U. Kim, Darren J. McMurtrie, Xiaoning C. Sheng
  • SYNTHESIS OF DRUG CONJUGATES VIA REACTION WITH EPOXIDE-CONTAINING LINKERS
    Publication number: 20080312440
    Abstract: The present invention relates to drug derivatives and linkers. The invention specifically relates to compounds and methods of phosphonates and linkers, that are useful as carriers for imaging agents and useful in the treatment of various bone diseases.
    Type: Application
    Filed: April 16, 2008
    Publication date: December 18, 2008
    Applicant: University of Southern California
    Inventors: Charles E. McKenna, Boris A. Kashemirov, Joy Lynn F. Bala
  • LINKERS FOR ANCHORING TARGETING LIGANDS
    Publication number: 20080305037
    Abstract: An improved linker which lacks chiral centers between a hydrophobic anchor for coupling to lipid-based particles and a targeting agent has suitable hydrophobic/hydrophilic properties for use in vivo.
    Type: Application
    Filed: October 16, 2007
    Publication date: December 11, 2008
    Inventor: William D. McGhee
  • Narcistatin prodrugs
    Patent number: 7462609
    Abstract: The present invention provides prodrugs derived from the sparingly soluble anticancer isocarbostyril narciclasine, a component of various Narcissus species, said prodrugs having potential for use against animal and human cancers. Also disclosed is an efficient procedure for the synthetic conversion of narciclasine to several more soluble cyclic phosphate compounds, including “narcistatin”.
    Type: Grant
    Filed: December 9, 2003
    Date of Patent: December 9, 2008
    Assignee: Arizona Board of Regents
    Inventors: George R. Pettit, Noeleen Melody