Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 546/23)
  • Patent number: 10351582
    Abstract: The present invention provides novel phospholipidated imidazoquinolines of formula (I) as TLR7 and TLR8 agonists, pharmaceutical compositions, therapeutic uses and processes for preparing the same.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: July 16, 2019
    Assignee: GLAXOSMITHKLINE BIOLOGICALS, S.A.
    Inventors: Helene G. Bazin-Lee, David A. Johnson
  • Patent number: 10017528
    Abstract: Perylene diimide phosphoramidite derivatives and methods for polymerization of perylene diimide phosphoramidite derivatives and applications thereof are provided. Compounds comprise at least an electronically active base surrogate and may also include a solubilizing functionality. The base surrogate may be comprised of an electrochemically active perylene diimide (PDI) molecule, the solubility chain may comprise a PEG functionality, and the PDI may further comprise a phosphoramidite functionality as an imide substituent. The phosphoramidite functionality may be used as a chemical coupling handle for use with established nucleic acid synthesis protocols and/or automated synthesis. One or more aromatic core functionalizations may be incorporated into the PDI molecules to allow for tuning the molecule's electronic and optical properties.
    Type: Grant
    Filed: September 18, 2017
    Date of Patent: July 10, 2018
    Assignee: The Regents of the University of California
    Inventors: Amir Mazaheripour, Anthony Burke, Alon Gorodetsky
  • Patent number: 9951094
    Abstract: The following formula is an example of a phosphole compound of the present invention. The phosphole compound of the present invention has the characteristic of maintaining a high fluorescence quantum yield in a wide range of solvents from low-polarity solvents to high-polarity solvents, as well as the characteristic in which the fluorescence wavelength shifts to the longer wavelength side as the polarity of the solvent increases. Because of these characteristics, the phosphole compound of the present invention is expected to be used, for example, for quantitatively determining the polarity in the environment therearound by using the absorption wavelength and fluorescence wavelength thereof, or used as a new fluorescent probe dye or a highly efficient luminescent material in organic electronic devices.
    Type: Grant
    Filed: January 22, 2015
    Date of Patent: April 24, 2018
    Assignee: NATIONAL UNIVERSITY CORPORATION NAGOYA UNIVERSITY
    Inventors: Shigehiro Yamaguchi, Aiko Fukazawa, Eriko Yamaguchi, Chenguang Wang
  • Publication number: 20150148313
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are Factor VIIa inhibitors which may be used as medicaments.
    Type: Application
    Filed: June 5, 2013
    Publication date: May 28, 2015
    Inventors: Xiaojun Zhang, Peter Glunz, Eldon Scott Priestley, James A. Johnson, Nicholas Ronald Wurtz, Vladimir Ladziata
  • Publication number: 20150133400
    Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.
    Type: Application
    Filed: September 15, 2014
    Publication date: May 14, 2015
    Inventors: Jiazhong Zhang, John Buell, Katrina Chan, Prabha N. Ibrahim, Jack Lin, Phuongly Pham, Songyuan Shi, Wayne Spevak, Guoxian Wu, Jeffrey Wu
  • Publication number: 20150125475
    Abstract: The invention is in the field of salt forms of an immunopotentiator compound and their formulation for in vivo use. In particular the invention relates to arginine salts.
    Type: Application
    Filed: March 7, 2013
    Publication date: May 7, 2015
    Inventors: Stephanie Kay Dodd, Siddhartha Jain
  • Publication number: 20150119553
    Abstract: Compounds are disclosed that are useful for noninvasive imaging in the near-infrared spectral range.
    Type: Application
    Filed: November 24, 2014
    Publication date: April 30, 2015
    Inventors: Xinshe Xu, Daniel R. Draney, Lael Cheung
  • Publication number: 20150065415
    Abstract: 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: Application
    Filed: November 6, 2014
    Publication date: March 5, 2015
    Inventors: John J. Partridge, John Colucci, Yves Gareau, Michel Therien, Robert Zamboni, Barry Hafkin, Anthony Marfat, Helmi Zaghdane
  • Publication number: 20150065464
    Abstract: The present disclosure relates to substituted amide compounds that are inhibitors of Fatty Acid Amide Hydrolase (FAAH), their stereoisomers, tautomers, prodrugs, polymorphs, solvates, pharmaceutically acceptable salts, and pharmaceutical compositions containing them.
    Type: Application
    Filed: September 21, 2012
    Publication date: March 5, 2015
    Inventors: Rajendra Kharul, Debnath Bhuniya, Kasim A. Mookhtiar, Umesh Singh, Atul Hazare, Satish Patil, Laxmikant Datrange, Mahesh Thakkar
  • Publication number: 20150057220
    Abstract: Fused aromatic phosphonates of structural formula I are precursors to inhibitors of protein tyrosine phosphatase-1B (PTP-1B). The compounds of the present invention are therefore useful for the treatment in a mammal of a disorder, condition, or disease responsive to inhibition of protein tyrosine phosphatase-1B, including Type 2 diabetes, insulin resistance, a lipid disorder, obesity, Metabolic Syndrome, and cancer.
    Type: Application
    Filed: April 16, 2013
    Publication date: February 26, 2015
    Inventors: Michel Therien, Yves Leblanc, Yongxin Han
  • Patent number: 8957051
    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: Grant
    Filed: September 30, 2013
    Date of Patent: February 17, 2015
    Assignee: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Publication number: 20150034927
    Abstract: A compound represented by the following formula (1-1):
    Type: Application
    Filed: February 7, 2013
    Publication date: February 5, 2015
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Yuki Nakano, Hiroshi Yamamoto, Ryohei Hashimoto, Hideaki Nagashima
  • Publication number: 20150031648
    Abstract: Compounds of formula (I): wherein X, Y, A1, A2, Ra, Rb, Rc, Rd, R3, R4, T and R5 are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Application
    Filed: July 22, 2014
    Publication date: January 29, 2015
    Inventors: Arnaud LE TIRAN, Thierry LE DIGUARHER, Jérôme-Benoît STARCK, Jean-Michel HENLIN, Anne-Françoise GUILLOUZIC, Guillaume DE NANTEUIL, Olivier GENESTE, James Edward Paul DAVIDSON, James Brooke MURRAY, I-Jen CHEN
  • Publication number: 20150011509
    Abstract: Compounds of Formula (I) can be selectively lethal toward a variety of different cancer cell types. The compounds are useful for the management, treatment, control, or adjunct treatment of diseases, where the selective lethality is beneficial in chemotherapeutic therapy.
    Type: Application
    Filed: October 12, 2012
    Publication date: January 8, 2015
    Applicants: The Board of Trustees of the University of Illnois, The Board of Regents of the University of Texas System
    Inventors: Paul J. Hergenrother, David A. Boothman, Joseph S. Bair, Rahul Palchaudhuri, Elizabeth I. Parkinson
  • Publication number: 20150011508
    Abstract: The invention provides compounds of formulae (I) and (II) and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.
    Type: Application
    Filed: August 28, 2012
    Publication date: January 8, 2015
    Inventors: Xiaodong Liu, Xiaolin Li, Jon Loren, Valentina Molteni, Juliet Nabakka, Bao Nguyen, Hank Michael James Petrassi, Vince Yeh
  • Patent number: 8906852
    Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions.
    Type: Grant
    Filed: April 8, 2011
    Date of Patent: December 9, 2014
    Assignee: MethylGene Inc.
    Inventors: Stéphane Raeppel, Franck Raeppel, Stephen William Claridge, Lijie Zhan, Frédéric Gaudette, Michael Mannion, Norifumi Sato, Yohei Yuki, Masashi Kishida, Arkadii Vaisburg
  • Patent number: 8901105
    Abstract: 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: Grant
    Filed: August 26, 2013
    Date of Patent: December 2, 2014
    Assignee: Debiopharm International SA
    Inventors: John J. Partridge, John Colucci, Yves Gareau, Michel Therien, Robert Zamboni, Barry Hafkin, Anthony Marfat, Helmi Zaghdane
  • Publication number: 20140349970
    Abstract: The invention provides a compound of Formula (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ii), (Ij), (Ik), or (Il) as defined herein, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: June 9, 2014
    Publication date: November 27, 2014
    Applicant: ABBVIE INC.
    Inventors: Neil Wishart, Maria A. Argiriadi, Eric C. Breinlinger, David J. Calderwood, Anna M. Ericsson, Bryan A. Fiamengo, Kristine E. Frank, Michael Friedman, Dawn M. George, Eric R. Goedken, Michael Z. Hoemann, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Kelly D. Mullen, Gagandeep Somal, Kent D. Stewart, Jeffrey W. Voss, Grier A. Wallace, Lu Wang, Kevin R. Woller
  • 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
  • Publication number: 20140332790
    Abstract: Display comprising at least one organic light emitting diode, wherein the at least one organic light emitting diode comprises an anode, a cathode, a light emitting layer between the anode and the cathode, and at least one layer comprising a compound according to formula (I) between the cathode and the light emitting layer: wherein A1 and A2 are independently selected from halogen, CN, substituted or unsubstituted C1-C20-alkyl or heteroalkyl, C6-C20-aryl or C5-C20-heteroaryl, C1-C20-alkoxy or C6-C20-aryloxy, A3 is selected from substituted or unsubstituted C6-C40-aryl or C5-C40-heteroaryl, m=0, 1 or 2, n=0, 1 or 2.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 13, 2014
    Inventors: Omrane Fadhel, Ramona Pretsch, Carsten Rothe, Rudolf Lessmann, Francois Cardinali
  • Publication number: 20140323416
    Abstract: The aspects of the present disclosure are directed to novel compounds, formulations containing said compounds or pharmaceutically acceptable salts thereof which are suitable for administration to a patient. In particular, to 5-methyldihydromorphone prodrug compounds described in general Formula I and II and the use of the compounds for treating pain associated with a variety of chronic human disorders including for example neuropathic pain and pain associated with cancer, surgeries or injuries.
    Type: Application
    Filed: April 16, 2014
    Publication date: October 30, 2014
    Inventors: Anthony MARFAT, Peter CORNELIUS, Robert VOLKMANN, Panayiotis ZAGOURAS, Frederick Raymond NELSON, Anton Franz Joseph FLIRI
  • Publication number: 20140323731
    Abstract: The compounds of the subject invention are adjuvant molecules that comprise an 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: Application
    Filed: December 20, 2013
    Publication date: October 30, 2014
    Applicant: GLAXOSMITHKLINE BIOLOGICALS S.A.
    Inventor: David A. JOHNSON
  • Publication number: 20140309423
    Abstract: The subject matter of the present invention is a plurality of products and the use thereof as a catalytically active composition in a method for producing aldehydes.
    Type: Application
    Filed: October 24, 2012
    Publication date: October 16, 2014
    Applicant: EVONIK DEGUSSA GmbH
    Inventors: Andrea Christiansen, Robert Franke, Dirk Fridag, Dieter Hess, Burkard Kreidler, Detlef Selent, Armin Boerner
  • Publication number: 20140309191
    Abstract: In part, the present invention is directed to antibacterial compounds and salts thereof.
    Type: Application
    Filed: November 8, 2013
    Publication date: October 16, 2014
    Applicant: Affinium Pharmaceuticals, Inc.
    Inventors: Henry Pauls, Jailall Ramnauth
  • Patent number: 8859110
    Abstract: An organic light-emitting diode comprising at least one cyclic phosphazene compound, a light-emitting layer formed from at least one matrix material and at least one emitter material, wherein the at least one matrix material comprises at least one cyclic phosphazene compound, the use of cyclic phosphazene compounds in organic light-emitting diodes and a device selected from the group consisting of stationary visual display units, mobile visual display units and illumination units comprising at least one inventive organic light-emitting diode, and selected cyclic phosphazene compounds and processes for preparing them.
    Type: Grant
    Filed: June 17, 2009
    Date of Patent: October 14, 2014
    Assignees: BASF SE, Koninklijke Philips Electronics N.V., Osram Opto Semiconductors GmbH, Siemens Aktiengesellschaft
    Inventors: Evelyn Fuchs, Oliver Molt, Nicolle Langer, Christian Lennartz, Peter Strohriegl, Pamela Schroegel, Herbert Friedrich Boerner, Volker Van Elsbergen, Arvid Hunze, Ralf Krause, Guenter Schmid
  • Patent number: 8859529
    Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: October 14, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K. C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
  • Publication number: 20140303121
    Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 9, 2014
    Inventors: Jiazhong Zhang, Wayne Spevak
  • Publication number: 20140274960
    Abstract: The present invention provides compounds of Formula (I) or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 18, 2014
    Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
  • Publication number: 20140243289
    Abstract: The present invention relates to prodrugs of modulators of ABC transporters, particularly, CFTR modulators, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: May 2, 2014
    Publication date: August 28, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Peter D.J. Grootenhuis, Sara Hadida Ruah, Jinglan Zhou, Anna Hazlewood, Hayley Binch
  • Publication number: 20140220588
    Abstract: The invention relates to novel fluorescent dyes with phosphorylated hydroxymethyl groups, a method for preparing the same as well as to their use in imaging techniques. The fluorescent dyes are coumarin, rhodamine or BODIPY dyes having of one of the following general formulae I-III: wherein W=OP(O) Y1Y2 or P(O) Y1Y2, where Y1 and Y2 independently denote any of the following residues: OH, O(?), ORa and ORb, NHRa and NHRb, NRaRb and NRcRd, ORa and NHRb, ORa and NRbRc, NHRa and NRbRc; and any salt thereof.
    Type: Application
    Filed: October 18, 2011
    Publication date: August 7, 2014
    Applicant: Max-Planck-Gesellschaft zur Foerderung der Wissenschaften e.V.
    Inventors: Stefan W. Hell, Shamil Nizamov, Gerald Donnert, Kirill Kolmakov, Heiko Schill, Lars Kastrup, Christian A. Wurm, Vladimir N. Belov, Johanna Bueckers, Katrin Willig
  • Publication number: 20140213554
    Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and/or mutant c-kit protein kinases.
    Type: Application
    Filed: December 20, 2013
    Publication date: July 31, 2014
    Inventors: Guoxian Wu, Katrina Chan, Todd Ewing, Prabha N. Ibrahim, Jack Lin, Marika Nespi, Wayne Spevak, Ying Zhang
  • Publication number: 20140200199
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Application
    Filed: March 17, 2014
    Publication date: July 17, 2014
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi Moussa, Neru Munshi
  • Patent number: 8779135
    Abstract: The technology of this invention concerns a method for the manufacture of hydroxy diphosphonic acids containing an amino moiety. The method specifically involves reacting a liquid P4O6 with an aminocarboxylic acid in the presence of a sulfonic acid. The aminocarboxylic acid is selected from 3 structurally different compounds. The amino hydroxy diphosphonic acids can be synthesized with high selectivity and purity and the unreacted starting raw materials can easily and conveniently be recirculated.
    Type: Grant
    Filed: October 4, 2010
    Date of Patent: July 15, 2014
    Assignee: Straitmark Holding AG
    Inventors: Samuel Corentin Cogels, David Lemin, Patrick Notté
  • Patent number: 8779136
    Abstract: 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: Grant
    Filed: October 18, 2013
    Date of Patent: July 15, 2014
    Assignee: Yeda Research and Development Co. Ltd.
    Inventors: David Milstein, Chidambaram Gunanathan
  • Publication number: 20140194389
    Abstract: 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: Application
    Filed: March 12, 2014
    Publication date: July 10, 2014
    Applicant: WARNER CHILCOTT COMPANY, LLC
    Inventors: Frank Hallock Ebetino, Adam Wieslaw Mazur, Roy Lee Martin Dobson
  • Patent number: 8754078
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: June 17, 2014
    Assignee: ArQule, Inc.
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi M. Moussa, Neru Munshi
  • Patent number: 8735583
    Abstract: 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: Grant
    Filed: February 6, 2013
    Date of Patent: May 27, 2014
    Assignee: Johnson Matthey Public Limited Co.
    Inventors: Brian Adger, Alan Dyke, Giancarlo Francio, Frederick Ernest Hancock, Walter Leitner, Thomas Pullmann, Andreas Seger, Antonio Zanotti-Gerosa
  • Patent number: 8710215
    Abstract: 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: Grant
    Filed: October 12, 2012
    Date of Patent: April 29, 2014
    Assignee: Warner Chilcott Company, LLC
    Inventors: Frank Hallock Ebetino, Adam Wieslaw Mazur, Roy Lee Martin Dobson
  • Publication number: 20140110694
    Abstract: The present invention provides a new compound and an organic electronic diode using the same. The compound according to the present invention may be used as hole injection, hole transport, electron injection and transport, and light emitting materials in an organic light emitting diode and an organic electronic diode, and the organic electronic diode according to the present invention exhibits excellent efficiency, driving voltage, and life-span properties.
    Type: Application
    Filed: June 12, 2012
    Publication date: April 24, 2014
    Applicant: LG CHEM, LTD.
    Inventors: Changhwan Shin, Kongkyeom Kim, Hyok Joon Kwon, Dong Hoon Lee, Jinyoung Lee, Boonjae Jang, Jungi Jang, Hyungjin Lee
  • Patent number: 8703437
    Abstract: The present invention provides fluorogenic substrates and methods of use in detecting and analyzing phospholipase C isozyme (PLC) activity.
    Type: Grant
    Filed: June 7, 2011
    Date of Patent: April 22, 2014
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Qisheng Zhang, Wei Gang Huang, John Sondek, Stephanie Hicks
  • Publication number: 20140107074
    Abstract: The present disclosure is directed to compounds of the structure (X): wherein: n is 2 or 3; NHE has the structure wherein: R1 is H or —SO2—NR7R8—; R2 is selected from H, —NR7(CO)R8, —SO2—NR7R8— and —NR7R8; R3 is hydrogen; R7 is hydrogen; R8 is a bond linking to L; L is a polyalkylene glycol linker; and Core has the following structure: wherein: X is selected from the group consisting of a bond, —O—, —NH—, NHC(?O)—, —NHC(?O)NH— and —NHSO2—; and Y is selected from the group consisting of a bond, optionally substituted C1-6 alkylene, optionally substituted benzene, pyridinyl, a polyethylene glycol linker and —(CH2)1-6O(CH2)1-6—, and methods of using such compounds for the treatment of irritable bowel syndrome, chronic kidney disease and end-stage renal disease.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 17, 2014
    Applicant: Ardelyx, Inc.
    Inventors: Noah BELL, Christopher CARRERAS, Dominique CHARMOT, Jeffrey W. JACOBS, Michael Robert LEADBETTER, Marc NAVRE
  • Publication number: 20140107342
    Abstract: The present invention relates to a camptothecin derivative having a structure as represented by Formula (II), in which Xn+ is selected from H+, K+, Na+, Li+, Mg2+, Ca2+, Zn2+, Fe3+, and ammonium ion, while R1, R2, R3, and R4 independently represent a hydrogen, a hydroxyl group, a nitro group, a cyano group, a halogen, a carboxyl group, an optionally substituted amino group, a silicon-containing group, a monocyclic aryloxy group, an optionally substituted C1-C6 alkoxy group, an optionally substituted C1-C6 alkylcarbonyl group, an optionally substituted C1-C6 alkyl group, or an optionally substituted C3-C6 cycloalkyl group; alternatively, R1 and R2 are connected via one to three other atoms to form a heterocyclic ring; and in another embodiment, R3 and R4 are oxygen atoms and connected via —O—(CH2)n—O—, forming a ring, in which n=I or 2. The compound has great water-solubility, chemical stability, and great efficacy in treatment on cancer.
    Type: Application
    Filed: December 19, 2013
    Publication date: April 17, 2014
    Inventors: Wenqiang Zhou, Jing Deng
  • 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
  • Publication number: 20140100194
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Application
    Filed: December 5, 2013
    Publication date: April 10, 2014
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Raymond W Colburn, Scott L. Dax, Christopher M. Flores, Jay M. Matthews
  • Publication number: 20140100195
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Application
    Filed: October 5, 2012
    Publication date: April 10, 2014
    Inventors: Richard D. Caldwell, Kevin M. GUCKIAN, Gnanasambandam KUMARA VEL, Wen-Cherng LEE, Edward Yin-Shiang LIN, Xiaogao LlU, Bin MA, Daniel M. SCOTT, Zhan SHl, Jermaine THOMAS, Arthur G. TAVERAS, Guo Zhu ZHENG
  • Publication number: 20140088305
    Abstract: The present invention relates to organic electroluminescent devices which comprise heteroaromatic compounds.
    Type: Application
    Filed: May 7, 2012
    Publication date: March 27, 2014
    Applicant: Merck Patent GmbH
    Inventors: Amir Hossain Parham, Arne Buesing, Christof Pflumm, Teresa Mujica-Fernaud, Philipp Toessel, Thomas Eberle
  • Publication number: 20140080788
    Abstract: Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R3, R4, R4a, R5a, R5b, R5c, R5d, R5e, R6a, R6b, and R6c are defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
    Type: Application
    Filed: April 27, 2012
    Publication date: March 20, 2014
    Inventors: Jeffrey A. Robl, Jun Li, Lawrence J. Kennedy, Steven J. Walker, Haixia Wang, William N. Washburn, Saleem Ahmad, Khehyong Ngu
  • Patent number: 8674102
    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: Grant
    Filed: January 3, 2013
    Date of Patent: March 18, 2014
    Assignee: Enzo Life Sciences, Inc.
    Inventors: Praveen Pande, Zaiguo Li, Maciej Szczepanik, Wayne Forrest Patton
  • Publication number: 20140051666
    Abstract: 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: Application
    Filed: August 26, 2013
    Publication date: February 20, 2014
    Applicant: AFFINIUM PHARMACEUTICALS, INC.
    Inventors: John J. Partridge, John Colucci, Yves Gareau, Michel Therien, Robert Zamboni, Barry Hafkin, Anthony Marfat, Helmi Zaghdane
  • Publication number: 20140046065
    Abstract: 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: Application
    Filed: October 18, 2013
    Publication date: February 13, 2014
    Applicant: YEDA RESEARCH AND DEVELOPMENT CO. LTD.
    Inventors: David Milstein, Chidambaram Gunanathan