The Phosphorus Is Part Of A Substituent Which Is Attached Directly To Ring Carbon Of The Five-membered Hetero Ring Patents (Class 548/119)
  • Patent number: 9981040
    Abstract: An object of the present invention is to provide a capsule formulation comprising a phosphonooxymethyl derivative of ravuconazole which suppresses delay in dissolution due to storage regardless of an encapsulated amount of the phosphonooxymethyl derivative of ravuconazole. The present invention provides a capsule formulation comprising an encapsulated material comprising {[(1R,2R)-2-[4-(4-cyanophenyl)-1,3-thiazol-2-yl]-1-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-ylmethyl)propyl]oxy}methyl dihydrogen phosphate or a pharmacologically acceptable salt thereof, or a solvate of any of the foregoing, and a capsule shell not comprising gelatin.
    Type: Grant
    Filed: April 17, 2013
    Date of Patent: May 29, 2018
    Assignee: Eisai R&D Management Co., Ltd.
    Inventor: Yosuke Ueki
  • Publication number: 20150119571
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: September 4, 2014
    Publication date: April 30, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury
  • 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: 20150065466
    Abstract: The present invention generally concerns particular methods and compositions for antimicrobial therapy. In particular embodiments, the compositions target DXR. In some cases, the antimicrobial agent comprises an electron-deficient hydrophobic group that has interacts with Trp211 of DXR. In specific embodiments, the compound contains electron-deficient heterocyclic rings that specifically interact with the electron-rich indole ring of Trp211. In certain aspects, the compositions comprise a phosphate group, a pyridine group, and a hydroxymate group.
    Type: Application
    Filed: April 18, 2013
    Publication date: March 5, 2015
    Inventor: Yongcheng Song
  • Publication number: 20150057451
    Abstract: The present invention provides organic molecules and methods thereof for reactions between organoboron reagents and double bonds, such as imines or carbonyls, to stereoselectively provide chiral products including amines and alcohols, entities useful for the preparation of biologically active molecules.
    Type: Application
    Filed: March 1, 2013
    Publication date: February 26, 2015
    Inventors: Amir H. Hoveyda, Daniel L. Silverio, Tatiana Pilyugina, Sebastian Torker, Daniel Robbins
  • Publication number: 20150050659
    Abstract: Protected fluorescent reagent compounds and their methods of synthesis are provided. The compounds are useful in various fluorescence-based analytical methods, including the analysis of highly multiplexed optical reactions in large numbers at high densities, such as single molecule real time nucleic acid sequencing reactions. The compounds contain fluorescent dye elements, that allow the compounds to be detected with high sensitivity at desirable wavelengths, binding elements, that allow the compounds to be recognized specifically by target biomolecules, and protective shield elements, that decrease undesirable contacts between the fluorescent dye elements and the bound target biomolecules and that therefore decrease photodamage of the bound target biomolecules by the fluorescent dye elements.
    Type: Application
    Filed: August 5, 2014
    Publication date: February 19, 2015
    Inventors: Lubomir SEBO, Jeremiah HANES, Gene SHEN, Louis BROGLEY, Stephen YUE, Frank ZHENG, Yuri LAPIN, John LYLE, Honey OSUNA, Andrei FEDOROV
  • Patent number: 8901106
    Abstract: Imidazole prodrugs, pharmaceutically acceptable salts, or isomers thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Grant
    Filed: March 26, 2012
    Date of Patent: December 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ellen K. Kick, Michael J. Hageman, Victor R. Guarino, Ching-Chiang Su, Chenkou Wei, Jayakumar S. Warrier, Satheesh Nair
  • Publication number: 20140339098
    Abstract: A process for the catalyzed electrochemical reduction of carbon dioxide wherein a metal organic framework comprising metal ions and an organic ligand is used as a catalyst and novel metal organic frameworks based on bisphosphonic acids.
    Type: Application
    Filed: December 13, 2012
    Publication date: November 20, 2014
    Inventors: Adam Wieslaw Mazur, Jean-Yves Nedelec, Christine Cachet-Vivier, Maniyan Padmanilayam, Armin T. Liebens
  • Patent number: 8859509
    Abstract: The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) through a linker and optionally, a connector molecule.
    Type: Grant
    Filed: May 13, 2009
    Date of Patent: October 14, 2014
    Assignee: Yale University
    Inventors: David Spiegel, Ryan Murelli, Andrew Zhang
  • Patent number: 8828974
    Abstract: The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1, P1, P2 and P3 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.
    Type: Grant
    Filed: April 24, 2012
    Date of Patent: September 9, 2014
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Yong Mi Choi-Sledeski, Julian Levell, Gregory Bernard Poli, Mark Czekaj, Alan John Collis, Roy Vaz
  • Publication number: 20140243288
    Abstract: The present invention relates to a fused ring-containing oxazolidinone compound shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof, wherein R1, R2, R3, R4, R5, R6, A, B and C are as defined in the description. The present invention further relates to a method for preparing the compound, a pharmaceutical composition and a pharmaceutical formulation comprising the compound, and a use of the compound for the manufacture of a medicament for the treatment and/or prevention of infectious diseases and a use for the treatment and/or prevention of infectious diseases.
    Type: Application
    Filed: September 29, 2012
    Publication date: August 28, 2014
    Inventors: Hui Zhang, Aichen Wang
  • Publication number: 20140243292
    Abstract: The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 11, 2014
    Publication date: August 28, 2014
    Applicant: Sanofi
    Inventors: Werngard CZECHTIZKY, John WESTON, Nils RACKELMANN, Michael PODESCHWA, Petra ARNDT, Klaus WIRTH, Heinz GOEGELEIN, Olaf RITZELER, Volker KRAFT, Patrice BELLEVERGUE, Gary McCORT
  • Patent number: 8816070
    Abstract: 5-[4-(2-Methylphenyl)-3-hydroxy-4H-1,2,4-triazol-5-yl]-2,4-dihydroxy-N-methyl-N-butylbenzamide is an HSP90 inhibitor and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: December 11, 2007
    Date of Patent: August 26, 2014
    Assignee: Merck Patent GmbH
    Inventors: Hans Michael Eggenweiler, Michael Wolf, Hans Peter Buchstaller, Christian Sirrenberg
  • Publication number: 20140235585
    Abstract: The present invention relates to substituted diaryl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 19, 2014
    Publication date: August 21, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, KEN CHOW
  • Publication number: 20140235586
    Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: PTC Therapeutics, Inc.
    Inventors: Jeffrey A. Campbell, Atiyya Kahn, James Takasugi, Ellen Welch
  • Publication number: 20140235588
    Abstract: The present invention relates to substituted 1H-pyrazol-1,2,4-oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 13, 2014
    Publication date: August 21, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, KEN CHOW
  • Publication number: 20140235587
    Abstract: The present invention relates to substituted pyrazoles, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 13, 2014
    Publication date: August 21, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, KEN CHOW
  • Publication number: 20140228324
    Abstract: The present invention relates to substituted dihydropyrazoles, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 13, 2014
    Publication date: August 14, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, Ken Chow
  • Publication number: 20140227345
    Abstract: The invention suggests amphoteric lipids wherein one or more amphoteric groups having an isoelectric point between 4 and 9 are substituted on a membranous or membrane-forming amphiphilic substance, as well as liposomes containing such compounds.
    Type: Application
    Filed: October 11, 2013
    Publication date: August 14, 2014
    Applicant: Marina Biotech, Inc.
    Inventors: Frank Essler, Steffen Panzner, Gerold Endert
  • Publication number: 20140221645
    Abstract: N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, N2-phosphinyl amidinate metal salt complexes are described. Methods for making N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, and N2-phosphinyl amidinate metal salt complexes are also disclosed. Catalyst systems utilizing the N2-phosphinyl amidine metal salt complexes and N2-phosphinyl amidinate metal salt complexes are also disclosed along with the use of the N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, and N2-phosphinyl amidinate metal salt complexes for the oligomerization and/or polymerization of olefins.
    Type: Application
    Filed: January 31, 2014
    Publication date: August 7, 2014
    Applicant: CHEVRON PHILLIPS CHEMICAL COMPANY LP
    Inventors: Orson L. Sydora, Michael Carney, Brooke L. Small, Jeffery C. Gee, Steven Hutchison
  • Publication number: 20140206651
    Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II): and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L1-L4, A, B, R1-R4, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.
    Type: Application
    Filed: March 24, 2014
    Publication date: July 24, 2014
    Applicant: Pfizer Inc.
    Inventors: Matthew Frank Brown, Charles Francis Donovan, Edmund Lee Ellsworth, Denton Wade Hoyer, Timothy Allan Johnson, Manjinder Singh Lall, Chris Limberakis, Sean Timothy Murphy, Debra Ann Sherry, Clarke Bentley Taylor, Joseph Scott Warmus
  • Patent number: 8765722
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: June 26, 2013
    Date of Patent: July 1, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
  • Publication number: 20140178462
    Abstract: An amphoteric liposome comprising neutral lipids wherein said neutral lipids are selected from the group comprising cholesterol or mixtures of cholesterol and at least one neutral or zwitterionic lipid and wherein K (neutral) of said mixtures is 0.3 or less. Said amphoteric liposome may encapsulate an active agent, such as nucleic acid therapeutics. Also disclosed are pharmaceutical compositions comprising said amphoteric liposomes as a carrier for the delivery or targeted delivery of active agents or ingredients.
    Type: Application
    Filed: October 9, 2013
    Publication date: June 26, 2014
    Applicant: Marina Biotech, Inc.
    Inventors: Steffen Panzner, Silke Lutz, Evgenios Siepi, Claudia Muller, Ute Vinzens
  • Publication number: 20140135291
    Abstract: The present invention relates to novel 2-thio-1,3,4-oxadiazoles derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 7, 2013
    Publication date: May 15, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Publication number: 20140135292
    Abstract: To provide a novel compound that has S1P lyase inhibitory ability and induces a reduction in the number of lymphocytes, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the compound or pharmaceutically acceptable salt thereof as an active ingredient. A compound represented by the general formula (I): or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 27, 2012
    Publication date: May 15, 2014
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Nobuo Machinaga, Jun Chiba, Ryuji Hashimoto, Mamoru Otoyo, Ryotaku Inoue
  • Publication number: 20140128499
    Abstract: A rubber composition for the manufacture of tyres is based on one or more diene elastomers, one or more reinforcing fillers, and a vulcanization system. The vulcanization system includes one or more thiazole compounds chosen from compounds having the following formula (I): Certain specific thiazole derivatives are described.
    Type: Application
    Filed: April 16, 2012
    Publication date: May 8, 2014
    Applicants: MICHELIN RECHERCHE ET TECHNIQUE S.A., COMPAGNIE GENERALE DES ETABLISSEMENTS MICHELIN
    Inventors: Anne Veyland, Nicolas Seeboth
  • Publication number: 20140128348
    Abstract: The present invention relates to substituted 1,3,4-oxadiazoles-2-thio derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 4, 2013
    Publication date: May 8, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Publication number: 20140107075
    Abstract: The present invention relates to novel 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: February 21, 2013
    Publication date: April 17, 2014
    Applicant: ALLERGAN, INC.
    Inventors: TODD M. HEIDELBAUGH, PHONG X. NGUYEN
  • Publication number: 20140100199
    Abstract: The present invention relates to substituted aryl 1,2,4-oxadiazoles derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: September 30, 2013
    Publication date: April 10, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Publication number: 20140100197
    Abstract: The present invention relates to bicyclic aryl 1,2,4-oxadiazoles derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: September 30, 2013
    Publication date: April 10, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Patent number: 8680003
    Abstract: N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, N2-phosphinyl amidinate metal salt complexes are described. Methods for making N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, and N2-phosphinyl amidinate metal salt complexes are also disclosed. Catalyst systems utilizing the N2-phosphinyl amidine metal salt complexes and N2-phosphinyl amidinate metal salt complexes are also disclosed along with the use of the N2-phosphinyl amidine compounds, N2-phosphinyl amidinates, N2-phosphinyl amidine metal salt complexes, and N2-phosphinyl amidinate metal salt complexes for the oligomerization and/or polymerization of olefins.
    Type: Grant
    Filed: December 29, 2010
    Date of Patent: March 25, 2014
    Assignee: Chevron Phillips Chemical Company LP
    Inventors: Orson L. Sydora, Michael Carney, Brooke L. Small, Jeffery C. Gee, Steven Hutchison
  • Publication number: 20140079632
    Abstract: The present invention relates to selective trypsine-like serine protease activity-based probes, in particular urokinase plasminogen activator-activity based probes, the use thereof and methods for detecting selective urokinase activity by making use of said probes.
    Type: Application
    Filed: May 9, 2012
    Publication date: March 20, 2014
    Applicant: UNIVERSITEIT ANTWERPEN
    Inventors: Koen Augustyns, Pieter Van Der Veken, Jonas Messagie, Jurgen Joossens, Anne-Marie Lambeir
  • Publication number: 20140072624
    Abstract: Formulations and unit dose forms of TH-302 and other hypoxia activated prodrugs suitable for oral administration are useful for treating cancer.
    Type: Application
    Filed: April 13, 2012
    Publication date: March 13, 2014
    Applicant: THRESHOLD PHARMACEUTICALS, INC.
    Inventors: Donald Jung, Mark Matteucci, Stewart Kroll
  • Patent number: 8664204
    Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: March 4, 2014
    Assignee: Threshold Pharmaceuticals, Inc.
    Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao
  • Publication number: 20140057874
    Abstract: Dosage forms or pharmaceutical compositions comprise a compound having the structure of Formula IV: wherein n is a non-negative integer; wherein each Z is an oxazolidinone-containing moiety having antibiotic activity in vivo upon cleaving, wherein M is independently OR1 or NR1R2; wherein R1 and R2 are independently selected from the group consisting of H, an optionally-substituted hydrocarbyl residue or a pharmaceutically acceptable cation; wherein the compound in the dosage form or a pharmaceutical composition is present in an amount effective for treating or preventing an antibacterial infection in a mammalian subject. Methods of preparing and using these dosage forms or pharmaceutical compositions are also disclosed.
    Type: Application
    Filed: October 31, 2013
    Publication date: February 27, 2014
    Applicant: TRIUS THERAPEUTICS, INC.
    Inventors: David Keith Hester, II, Robert J. Duguid, John Finn
  • Patent number: 8653270
    Abstract: The present invention relates to novel derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: February 18, 2014
    Assignee: Allergan, Inc.
    Inventors: Todd M. Heidelbaugh, Phong X. Nguyen
  • Publication number: 20140045795
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
    Type: Application
    Filed: October 15, 2013
    Publication date: February 13, 2014
    Applicant: SYNTA PHARMACEUTICALS CORPORATION
    Inventors: Lijun Sun, Christopher Borella, Hao Li, Jun Jiang, Shoujun Chen, Keizo Koya, Takayo Inoue, Zhenjian Du, Kevin Foley, Yaming Wu, Mei Zhang, Weiwen Ying
  • Publication number: 20140024530
    Abstract: Use of N-(tetrazol-4-yl)- or N-(triazol-3-yl)arylcarboxamides of formula (I) or salts thereof for controlling unwanted plants in areas of transgenic crop plants being tolerant to HPPD inhibitor herbicides by containing one or more chimeric gene(s) comprising (I) a DNA sequence encoding hydroxyphenylpyruvate dioxygenase (HPPD) derived from a member of a group of organisms consisting of (a) Avena, (b) Pseudomonas, (c) Synechococcoideae, (d) Blepharismidae, (e) Rhodococcus, (f) Picrophilaceae, (g) Kordia, or (II) comprising one or more mutated DNA sequences of HPPD encoding genes of the before defined organisms.
    Type: Application
    Filed: March 21, 2012
    Publication date: January 23, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Fabien Poree, Andreas Almsick, Ralf Braun, Bernd Laber, Ruediger Hain
  • Publication number: 20140018321
    Abstract: Imidazole prodrugs, pharmaceutically acceptable salts, or isomers thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Application
    Filed: March 26, 2012
    Publication date: January 16, 2014
    Inventors: Ellen K. Kick, Michael J. Hageman, Victor R. Guarino, Ching-Chiang Su, Chenkou Wei, Jayakumar S. Warrier, Satheesh Nair
  • Publication number: 20140005036
    Abstract: An efficient method for the preparation of backbone-substituted imidazolinium salts for use as N-heterocyclic carbene ligands, e.g., for organometallic catalysts is provided. These functionalized N-heterocyclic carbene ligands are used to prepare solid-supported catalysts, e.g., for olefin metathesis.
    Type: Application
    Filed: June 26, 2013
    Publication date: January 2, 2014
    Inventors: Raymond Weitekamp, Robert H. Grubbs
  • Patent number: 8609639
    Abstract: A small-molecule Stat3 dimerization inhibitor, S3I-M2001, is described and the dynamics of intracellular processing of activated Stat3 within the context of the biochemical and biological effects of the Stat3 chemical probe inhibitor are elucidated. S3I-M2001 is a newly-identified oxazole-based peptidomimetic of the Stat3 Src Homology (SH) 2 domain-binding phosphotyrosine peptide that selectively disrupts active Stat3:Stat3 dimers. Stat3-dependent malignant transformation, survival, and migration and invasion of mouse and human cancer cells harboring persistently-activated Stat3 were inhibited by S3I-M2001. S3I-M2001 inhibited Stat3-dependent transcriptional regulation of tumor survival genes, such as Bcl-xL. The disclosed compound is useful as a new potential treatment for certain cancers.
    Type: Grant
    Filed: December 5, 2007
    Date of Patent: December 17, 2013
    Assignees: University of South Florida, Yale University, University of Central Florida Research Foundation, Inc.
    Inventors: James Turkson, Said Sebti, Richard Jove, Andrew D. Hamilton
  • Publication number: 20130330365
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Adam D. Hughes, Melissa Fleury
  • Publication number: 20130302280
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: June 26, 2013
    Publication date: November 14, 2013
    Inventors: Aesop Cho, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
  • Publication number: 20130303778
    Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
    Type: Application
    Filed: July 12, 2013
    Publication date: November 14, 2013
    Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao, Jacob Kaizerman
  • Patent number: 8580297
    Abstract: The invention suggests amphoteric lipids wherein one or more amphoteric groups having an isoelectric point between 4 and 9 are substituted on a membranous or membrane-forming amphiphilic substance, as well as liposomes containing such compounds.
    Type: Grant
    Filed: November 8, 2011
    Date of Patent: November 12, 2013
    Assignee: Marina Biotech, Inc.
    Inventors: Frank Essler, Steffen Panzner, Gerold Endert
  • Patent number: 8557982
    Abstract: The present invention relates to compounds of general formula (I) as tublin polymerization inhibitors and methods for preparing such compounds.
    Type: Grant
    Filed: August 13, 2012
    Date of Patent: October 15, 2013
    Assignee: Bionomics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
  • Patent number: 8507464
    Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: August 13, 2013
    Assignee: Threshold Pharmaceuticals, Inc.
    Inventors: Mark Matteucci, Jian-Xin Duan, Hailong Jiao, Jacob Kaizerman
  • Publication number: 20130203705
    Abstract: The present invention relates to a pyrazole amide derivative, pharmaceutical compositions containing this compound and to its use in therapy.
    Type: Application
    Filed: October 19, 2011
    Publication date: August 8, 2013
    Applicant: Glaxo Group Limited
    Inventors: Anthony William James Cooper, Paul Martin Gore, David House
  • Patent number: 8501714
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: September 7, 2010
    Date of Patent: August 6, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
  • Patent number: 8497255
    Abstract: The present invention relates to novel phosphonic acids derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 16, 2011
    Date of Patent: July 30, 2013
    Assignee: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Ken Chow, Wha-Bin Im