Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 546/23)
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Patent number: 10851292Abstract: The present invention provides a thermally activated delayed fluorescence (TADF) material, which is composed of a molecular compound having an ultra-fast reverse intersystem crossing rate, and when the TADF material serves as a host material in light-emitting layers of electroluminescent devices, both the resulting blue light fluorescence device and phosphorescent electroluminescent device can achieve very high efficiency.Type: GrantFiled: January 10, 2019Date of Patent: December 1, 2020Assignee: Wuhan China Star Optoelectronics Semiconductor Display Technology Co., Ltd.Inventor: Jiajia Luo
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Patent number: 10774099Abstract: The present invention relates to a process for phospholipidation of imidazoquinolines and oxoadenines. More particularly, the present invention relates to a high-yielding and scalable procedure for the phospholipidation of imidazoquinolines and oxoadenines which obviates the need to isolate unstable phosphoramidite intermediates. This process may be used for the phospholipidation of toll-like receptor 7 (TLR7)—active and toll-like receptor (TLR8)—active imidazoquinolines and oxoadenines.Type: GrantFiled: December 12, 2016Date of Patent: September 15, 2020Assignee: GLAXOSMITHKLINE BIOLOGICALS SAInventors: Helene G. Bazin-Lee, Laura S. Bess, David A. Johnson
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Patent number: 10774035Abstract: The invention relates to a method for synthesizing amino acids or amino acid derivatives involving cross metathesis of functionalized olefins and a tandem amination-reduction process. Amino acids and amino acid derivatives present many interesting physical and chemical properties finding many uses in the automotive, fuel, electronic, and textile industries.Type: GrantFiled: September 6, 2017Date of Patent: September 15, 2020Assignee: Umicore AG & Co. KGInventors: Adam M. Johns, Jessica R. Herron, Richard L. Pederson, Thay A. Ung, Ba L. Tran, Daryl P. Allen
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Patent number: 10702809Abstract: A cylindrical filtration filter includes a cylindrical filter main body. The filter main body is constituted by at least two split filters. Each of the split filters has an arc shape in cross section. Each of the split filters includes a filter element for filtration and side frame bodies provided along side portions of the filter element. The side frame body of one of the two split filters adjacent to each other includes a first facing surface having an uneven shape. The side frame body of the other split filter includes a second facing surface having an uneven shape complementary to the first facing surface. The first facing surface and the second facing surface are fitted to each other when the filter main body is assembled.Type: GrantFiled: August 22, 2018Date of Patent: July 7, 2020Assignee: KABUSHIKI KAISHA TOYOTA JIDOSHOKKIInventors: Hidekatsu Sakaguchi, Yasuhito Matoba
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Patent number: 10604540Abstract: 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: GrantFiled: July 9, 2018Date of Patent: March 31, 2020Assignee: The Regents of the University of CaliforniaInventors: Amir Mazaheripour, Anthony Burke, Alon Gorodetsky
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Patent number: 10351582Abstract: 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: GrantFiled: December 12, 2016Date of Patent: July 16, 2019Assignee: GLAXOSMITHKLINE BIOLOGICALS, S.A.Inventors: Helene G. Bazin-Lee, David A. Johnson
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Patent number: 10017528Abstract: 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: GrantFiled: September 18, 2017Date of Patent: July 10, 2018Assignee: The Regents of the University of CaliforniaInventors: Amir Mazaheripour, Anthony Burke, Alon Gorodetsky
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Patent number: 9951094Abstract: 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: GrantFiled: January 22, 2015Date of Patent: April 24, 2018Assignee: NATIONAL UNIVERSITY CORPORATION NAGOYA UNIVERSITYInventors: Shigehiro Yamaguchi, Aiko Fukazawa, Eriko Yamaguchi, Chenguang Wang
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Publication number: 20150148313Abstract: 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: ApplicationFiled: June 5, 2013Publication date: May 28, 2015Inventors: Xiaojun Zhang, Peter Glunz, Eldon Scott Priestley, James A. Johnson, Nicholas Ronald Wurtz, Vladimir Ladziata
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Publication number: 20150133400Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.Type: ApplicationFiled: September 15, 2014Publication date: May 14, 2015Inventors: Jiazhong Zhang, John Buell, Katrina Chan, Prabha N. Ibrahim, Jack Lin, Phuongly Pham, Songyuan Shi, Wayne Spevak, Guoxian Wu, Jeffrey Wu
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Publication number: 20150125475Abstract: 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: ApplicationFiled: March 7, 2013Publication date: May 7, 2015Inventors: Stephanie Kay Dodd, Siddhartha Jain
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Publication number: 20150119553Abstract: Compounds are disclosed that are useful for noninvasive imaging in the near-infrared spectral range.Type: ApplicationFiled: November 24, 2014Publication date: April 30, 2015Inventors: Xinshe Xu, Daniel R. Draney, Lael Cheung
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Publication number: 20150065415Abstract: In part, the present disclosure is directed to prodrug derivatives of (E)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide compounds with significant solubility and bioavailability profiles.Type: ApplicationFiled: November 6, 2014Publication date: March 5, 2015Inventors: John J. Partridge, John Colucci, Yves Gareau, Michel Therien, Robert Zamboni, Barry Hafkin, Anthony Marfat, Helmi Zaghdane
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Publication number: 20150065464Abstract: 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: ApplicationFiled: September 21, 2012Publication date: March 5, 2015Inventors: Rajendra Kharul, Debnath Bhuniya, Kasim A. Mookhtiar, Umesh Singh, Atul Hazare, Satish Patil, Laxmikant Datrange, Mahesh Thakkar
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Publication number: 20150057220Abstract: 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: ApplicationFiled: April 16, 2013Publication date: February 26, 2015Inventors: Michel Therien, Yves Leblanc, Yongxin Han
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Patent number: 8957051Abstract: 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: GrantFiled: September 30, 2013Date of Patent: February 17, 2015Assignee: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
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Publication number: 20150034927Abstract: A compound represented by the following formula (1-1):Type: ApplicationFiled: February 7, 2013Publication date: February 5, 2015Applicant: Idemitsu Kosan Co., Ltd.Inventors: Yuki Nakano, Hiroshi Yamamoto, Ryohei Hashimoto, Hideaki Nagashima
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PHOSPHATE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
Publication number: 20150031648Abstract: 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: ApplicationFiled: July 22, 2014Publication date: January 29, 2015Inventors: 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: 20150011508Abstract: 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: ApplicationFiled: August 28, 2012Publication date: January 8, 2015Inventors: Xiaodong Liu, Xiaolin Li, Jon Loren, Valentina Molteni, Juliet Nabakka, Bao Nguyen, Hank Michael James Petrassi, Vince Yeh
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Publication number: 20150011509Abstract: 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: ApplicationFiled: October 12, 2012Publication date: January 8, 2015Applicants: The Board of Trustees of the University of Illnois, The Board of Regents of the University of Texas SystemInventors: Paul J. Hergenrother, David A. Boothman, Joseph S. Bair, Rahul Palchaudhuri, Elizabeth I. Parkinson
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Patent number: 8906852Abstract: 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: GrantFiled: April 8, 2011Date of Patent: December 9, 2014Assignee: MethylGene Inc.Inventors: Stéphane Raeppel, Franck Raeppel, Stephen William Claridge, Lijie Zhan, Frédéric Gaudette, Michael Mannion, Norifumi Sato, Yohei Yuki, Masashi Kishida, Arkadii Vaisburg
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Patent number: 8901105Abstract: 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: GrantFiled: August 26, 2013Date of Patent: December 2, 2014Assignee: Debiopharm International SAInventors: John J. Partridge, John Colucci, Yves Gareau, Michel Therien, Robert Zamboni, Barry Hafkin, Anthony Marfat, Helmi Zaghdane
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Publication number: 20140349970Abstract: 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: ApplicationFiled: June 9, 2014Publication date: November 27, 2014Applicant: 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
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Publication number: 20140339098Abstract: 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: ApplicationFiled: December 13, 2012Publication date: November 20, 2014Inventors: Adam Wieslaw Mazur, Jean-Yves Nedelec, Christine Cachet-Vivier, Maniyan Padmanilayam, Armin T. Liebens
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Publication number: 20140332790Abstract: 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: ApplicationFiled: November 30, 2012Publication date: November 13, 2014Inventors: Omrane Fadhel, Ramona Pretsch, Carsten Rothe, Rudolf Lessmann, Francois Cardinali
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Publication number: 20140323416Abstract: 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: ApplicationFiled: April 16, 2014Publication date: October 30, 2014Inventors: Anthony MARFAT, Peter CORNELIUS, Robert VOLKMANN, Panayiotis ZAGOURAS, Frederick Raymond NELSON, Anton Franz Joseph FLIRI
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Publication number: 20140323731Abstract: 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: ApplicationFiled: December 20, 2013Publication date: October 30, 2014Applicant: GLAXOSMITHKLINE BIOLOGICALS S.A.Inventor: David A. JOHNSON
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Publication number: 20140309191Abstract: In part, the present invention is directed to antibacterial compounds and salts thereof.Type: ApplicationFiled: November 8, 2013Publication date: October 16, 2014Applicant: Affinium Pharmaceuticals, Inc.Inventors: Henry Pauls, Jailall Ramnauth
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Publication number: 20140309423Abstract: 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: ApplicationFiled: October 24, 2012Publication date: October 16, 2014Applicant: EVONIK DEGUSSA GmbHInventors: Andrea Christiansen, Robert Franke, Dirk Fridag, Dieter Hess, Burkard Kreidler, Detlef Selent, Armin Boerner
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Patent number: 8859529Abstract: 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: GrantFiled: September 22, 2009Date of Patent: October 14, 2014Assignee: 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
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Patent number: 8859110Abstract: 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: GrantFiled: June 17, 2009Date of Patent: October 14, 2014Assignees: BASF SE, Koninklijke Philips Electronics N.V., Osram Opto Semiconductors GmbH, Siemens AktiengesellschaftInventors: Evelyn Fuchs, Oliver Molt, Nicolle Langer, Christian Lennartz, Peter Strohriegl, Pamela Schroegel, Herbert Friedrich Boerner, Volker Van Elsbergen, Arvid Hunze, Ralf Krause, Guenter Schmid
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Publication number: 20140303121Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.Type: ApplicationFiled: March 14, 2014Publication date: October 9, 2014Inventors: Jiazhong Zhang, Wayne Spevak
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Publication number: 20140274960Abstract: 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: ApplicationFiled: October 12, 2012Publication date: September 18, 2014Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
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Publication number: 20140243289Abstract: The present invention relates to prodrugs of modulators of ABC transporters, particularly, CFTR modulators, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: May 2, 2014Publication date: August 28, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Peter D.J. Grootenhuis, Sara Hadida Ruah, Jinglan Zhou, Anna Hazlewood, Hayley Binch
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Publication number: 20140220588Abstract: 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: ApplicationFiled: October 18, 2011Publication date: August 7, 2014Applicant: 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
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Publication number: 20140213554Abstract: 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: ApplicationFiled: December 20, 2013Publication date: July 31, 2014Inventors: Guoxian Wu, Katrina Chan, Todd Ewing, Prabha N. Ibrahim, Jack Lin, Marika Nespi, Wayne Spevak, Ying Zhang
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Publication number: 20140200199Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.Type: ApplicationFiled: March 17, 2014Publication date: July 17, 2014Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi Moussa, Neru Munshi
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Patent number: 8779136Abstract: 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: GrantFiled: October 18, 2013Date of Patent: July 15, 2014Assignee: Yeda Research and Development Co. Ltd.Inventors: David Milstein, Chidambaram Gunanathan
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Patent number: 8779135Abstract: 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: GrantFiled: October 4, 2010Date of Patent: July 15, 2014Assignee: Straitmark Holding AGInventors: Samuel Corentin Cogels, David Lemin, Patrick Notté
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Publication number: 20140194389Abstract: Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.Type: ApplicationFiled: March 12, 2014Publication date: July 10, 2014Applicant: WARNER CHILCOTT COMPANY, LLCInventors: Frank Hallock Ebetino, Adam Wieslaw Mazur, Roy Lee Martin Dobson
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Patent number: 8754078Abstract: 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: GrantFiled: February 7, 2013Date of Patent: June 17, 2014Assignee: ArQule, Inc.Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi M. Moussa, Neru Munshi
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Patent number: 8735583Abstract: 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: GrantFiled: February 6, 2013Date of Patent: May 27, 2014Assignee: Johnson Matthey Public Limited Co.Inventors: Brian Adger, Alan Dyke, Giancarlo Francio, Frederick Ernest Hancock, Walter Leitner, Thomas Pullmann, Andreas Seger, Antonio Zanotti-Gerosa
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Patent number: 8710215Abstract: 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: GrantFiled: October 12, 2012Date of Patent: April 29, 2014Assignee: Warner Chilcott Company, LLCInventors: Frank Hallock Ebetino, Adam Wieslaw Mazur, Roy Lee Martin Dobson
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Publication number: 20140110694Abstract: 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: ApplicationFiled: June 12, 2012Publication date: April 24, 2014Applicant: LG CHEM, LTD.Inventors: Changhwan Shin, Kongkyeom Kim, Hyok Joon Kwon, Dong Hoon Lee, Jinyoung Lee, Boonjae Jang, Jungi Jang, Hyungjin Lee
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Patent number: 8703437Abstract: The present invention provides fluorogenic substrates and methods of use in detecting and analyzing phospholipase C isozyme (PLC) activity.Type: GrantFiled: June 7, 2011Date of Patent: April 22, 2014Assignee: The University of North Carolina at Chapel HillInventors: Qisheng Zhang, Wei Gang Huang, John Sondek, Stephanie Hicks
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Publication number: 20140107342Abstract: 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: ApplicationFiled: December 19, 2013Publication date: April 17, 2014Inventors: Wenqiang Zhou, Jing Deng
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Publication number: 20140107074Abstract: 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: ApplicationFiled: March 14, 2013Publication date: April 17, 2014Applicant: Ardelyx, Inc.Inventors: Noah BELL, Christopher CARRERAS, Dominique CHARMOT, Jeffrey W. JACOBS, Michael Robert LEADBETTER, Marc NAVRE
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Publication number: 20140100197Abstract: 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: ApplicationFiled: September 30, 2013Publication date: April 10, 2014Applicant: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
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Publication number: 20140100195Abstract: 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: ApplicationFiled: October 5, 2012Publication date: April 10, 2014Inventors: 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
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Publication number: 20140100194Abstract: 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: ApplicationFiled: December 5, 2013Publication date: April 10, 2014Applicant: Janssen Pharmaceutica, NVInventors: Raymond W Colburn, Scott L. Dax, Christopher M. Flores, Jay M. Matthews