1,2,3-triazoles (including Hydrogenated) Patents (Class 548/255)
Polycyclo heterocyclic ring system containing ring oxygen (Class 548/256)
Polycyclo ring system having the triazole ring as one of the cyclos (Class 548/257)
  • NOVEL FXR (NR1H4) BINDING AND ACTIVITY MODULATING COMPOUNDS
    Publication number: 20120232116
    Abstract: The present invention relates to compounds which bind to the NR1 H4 receptor (FXR) and act as agonists of the NR1 H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
    Type: Application
    Filed: August 19, 2010
    Publication date: September 13, 2012
    Applicant: PHENEX PHARMACEUTICALS AG
    Inventors: Claus Kremoser, Ulrich Abel, Christoph Steeneck, Olaf Kinzel
  • Intraocular lenses with combinations of UV absorbers and blue light chromophores
    Patent number: 8262948
    Abstract: Disclosed are ophthalmic device materials having improved light transmission characteristics. The materials contain a combination of certain UV absorbers and blue-light absorbing chromophores.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: September 11, 2012
    Assignee: Novartis AG
    Inventors: Walter R. Laredo, Ali E. Akinay
  • 1,2,3-triazoles as 11-beta hydroxysteroid dehydrogenase type I inhibitors
    Patent number: 8263630
    Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein R1, R2, and R3 are defined herein.
    Type: Grant
    Filed: February 11, 2009
    Date of Patent: September 11, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventor: James J. Li
  • UV/visible light absorbers for ophthalmic lens materials
    Patent number: 8262947
    Abstract: Benzotriazole UV/Visible light-absorbing monomers are disclosed. The UV/Vis absorbers are particularly suitable for use in intraocular lens materials.
    Type: Grant
    Filed: July 2, 2010
    Date of Patent: September 11, 2012
    Assignee: Novartis AG
    Inventor: Walter R. Laredo
  • SCD1 inhibitors triazole and tetrazole compounds
    Patent number: 8258160
    Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: September 4, 2012
    Assignee: Novartis AG
    Inventors: Natalie Dales, Zaihui Zhang, Julia Fonarev, Jianmin Fu, Rajender Kamboj, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Shaoyi Sun
  • NEPRILYSIN INHIBITORS
    Publication number: 20120213806
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: February 16, 2012
    Publication date: August 23, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
  • NEPRILYSIN INHIBITORS
    Publication number: 20120213807
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: February 16, 2012
    Publication date: August 23, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
  • P2Xreceptor antagonists for treatment of pain
    Patent number: 8247401
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Grant
    Filed: October 29, 2008
    Date of Patent: August 21, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Diem Nguyen, Zhengwu Deng, Daniel V. Paone, Craig M. Potteiger, Joseph P. Vacca
  • Triazole derivatives for treating alzheimer'S disease and related conditions
    Patent number: 8242150
    Abstract: Compounds of formula I: Selectively attenuate production of A?(1-42) and hence find use in treatment or prevention of diseases associated with deposition of A? in the brain, in particular Alzheimer's disease.
    Type: Grant
    Filed: June 9, 2008
    Date of Patent: August 14, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christian Fischer, Ben Munoz, Susan Zultanski, Joey Methot, Hua Zhou, W. Colby Brown
  • INHIBITORS OF IAP
    Publication number: 20120202750
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.
    Type: Application
    Filed: January 23, 2012
    Publication date: August 9, 2012
    Applicant: Genentech, Inc.
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • HETEROCYCLE AMIDE T-TYPE CALCIUM CHANNEL ANTAGONISTS
    Publication number: 20120202852
    Abstract: The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
    Type: Application
    Filed: October 25, 2010
    Publication date: August 9, 2012
    Inventors: James Barrow, Kelly-Ann Schlegel, Yoheng Shu, Zhi-Qiang Yang
  • UV/visible light absorbers for ophthalmic lens materials
    Patent number: 8232326
    Abstract: Benzotriazole UV/Visible light-absorbing monomers are disclosed. The UV/Vis absorbers are particularly suitable for use in intraocular lens materials.
    Type: Grant
    Filed: February 8, 2012
    Date of Patent: July 31, 2012
    Assignee: Novartis AG
    Inventor: Walter R. Laredo
  • PREPARATION OF METAL-TRIAZOLATE FRAMEWORKS
    Publication number: 20120186449
    Abstract: The disclosure provides for novel metal-triazolate frameworks, methods of use thereof, and devices comprising the frameworks thereof.
    Type: Application
    Filed: January 20, 2012
    Publication date: July 26, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Omar M. Yaghi, Fernando J. Uribe-Romo, Felipe Gandara-Barragan, David K. Britt
  • 2,4-disubsituted thiazoles and pharmaceutical compositions thereof
    Patent number: 8227495
    Abstract: The present disclosure provides 2,4-disubstituted thiazoles of the general structure shown below that are agonists of G-protein coupled receptor (IC-GPCR2). Also, provided are compositions comprising these compounds as well as methods for using these compounds in a variety of applications including diabetes and metabolic disorders.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: July 24, 2012
    Assignee: Metabolex Inc.
    Inventors: Xin Chen, Peng Cheng, L. Edward Clemens, Jeffrey D. Johnson, Jingyuan Ma, Alison Murphy, Imad Nashashibi, Christopher J. Rabbat, Jiangao Song, Maria E. Wilson, Yan Zhu, Zuchun Zhao
  • Bifunctional histone deacetylase inhibitors
    Patent number: 8222423
    Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
    Type: Grant
    Filed: February 14, 2007
    Date of Patent: July 17, 2012
    Assignees: Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard College, Howard Hughes Medical Institute
    Inventors: James Elliot Bradner, Ralph Mazitschek, Tang Weiping, Stuart S. Schreiber
  • Hepatitis C virus inhibitors
    Patent number: 8221737
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: June 15, 2010
    Date of Patent: July 17, 2012
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
  • FACTOR XA INHIBITORS
    Publication number: 20120178733
    Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
    Type: Application
    Filed: August 19, 2011
    Publication date: July 12, 2012
    Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
  • COPPER-CATALYSED LIGATION OF AZIDES AND ACETYLENES
    Publication number: 20120165542
    Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting an organic azide and a terminal alkyne with a source of reactive Cu(I) ion for a time sufficient to form by cycloaddition a 1,4-disubstituted 1,2,3-triazole. The source of reactive Cu(I) ion can be, for example, a Cu(I) salt or copper metal. The process is preferably carried out in a solvent, such as an aqueous alcohol. Optionally, the process can be performed in a solvent that comprises a ligand for Cu(I) and an amine.
    Type: Application
    Filed: March 5, 2012
    Publication date: June 28, 2012
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: K. Barry SHARPLESS, Valery FOKIN, Vsevold A. ROSTOVTSEV, Luke GREEN, Fahmi HIMO
  • Triazole derivatives as SCD inhibitors
    Patent number: 8207204
    Abstract: The present invention relates to substituted triazole compounds of the formula (I): and salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for inhibiting SCD activity, such as diseases related to elevated lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome, skin disorders such as acne, diseases or conditions related to cancer and the treatment of symptoms linked to the production of the amyloid plaque-forming A?42 peptide such as Alzheimer's disease and the like.
    Type: Grant
    Filed: November 7, 2008
    Date of Patent: June 26, 2012
    Assignee: GlaxoSmithKline LLC
    Inventors: Anne Marie Jeanne Bouillot, Alain Laroze
  • METALLOENZYME INHIBITOR COMPOUNDS
    Publication number: 20120149729
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: December 13, 2011
    Publication date: June 14, 2012
    Applicant: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
  • 1,2,3-TRIAZOLE-IMIDAZOLECOMPOUNDS
    Publication number: 20120149675
    Abstract: The present invention is concerned with novel 1,2,3-triazole-imidazole compounds of formula (I) wherein X, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention provides a method for the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutic agents.
    Type: Application
    Filed: December 2, 2011
    Publication date: June 14, 2012
    Inventor: Andrew Thomas
  • N-(2-(hetaryl)aryl) arylsulfonamides and N-(2-(hetaryl)hetaryl arylsulfonamides
    Patent number: 8198309
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Grant
    Filed: July 8, 2010
    Date of Patent: June 12, 2012
    Assignee: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M. K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Chemical compounds
    Patent number: 8198308
    Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R2 to R4, L, Q and n are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: November 15, 2010
    Date of Patent: June 12, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis, Ioannis Sapountzis, Martin Steegmaier
  • Method for the preparation of rufinamide
    Patent number: 8198459
    Abstract: The invention provides a novel process for the regioselective preparation of a compound of formula (I)
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: June 12, 2012
    Assignee: Dipharma Francis S.r.l.
    Inventors: Emanuele Attolino, Lino Colombo, Ilaria Mormino, Pietro Allegrini
  • BENZAMIDES AND NICOTINAMIDES AS SYK MODULATORS
    Publication number: 20120142671
    Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.
    Type: Application
    Filed: November 1, 2011
    Publication date: June 7, 2012
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
  • 4- AND 5 SUBSTITUTED 1,2,3-TRIAZOLE MOIETIES WITH AT LEAST ONE REMOTE POLYMERIZABLE MOIETY AND POLYMERS THEREOF
    Publication number: 20120142846
    Abstract: The present invention provides novel 4- and 5-substituted 1,2,3-triazole moieties, with at least one remote polymerizable moiety. The novel mixtures of 4- and 5-substituted regioisomers of 1,2,3-triazole moieties can be separated by chromatography to provide the purified 4- and 5-substituted 1,2,3-triazole moieties. The novel mixtures of 4- and 5-substituted regioisomers of 1,2,3-triazole moieties, and the purified 4- and 5-substituted 1,2,3-triazole moieties, with at least one remote polymerizable moiety, can be converted to a wide variety of useful polymers. The novel compounds of the invention can be employed in a wide variety of compositions. E, Q, Z, X, a, and R1-R4, in the structures below, are defined herein.
    Type: Application
    Filed: July 7, 2010
    Publication date: June 7, 2012
    Inventor: Osama M. Musa
  • ACID-LABILE TRIGGER UNITS
    Publication number: 20120142711
    Abstract: The present invention relates to a compound comprising an imine bond as an acid-labile trigger group, the use of such an imine bond as an acid-labile trigger group, a process of cleaving the imine bond in said compound, and a pharmaceutical composition comprising said compound.
    Type: Application
    Filed: June 21, 2010
    Publication date: June 7, 2012
    Applicant: KTB TUMORFORSCHUNGSGESELLSCHAFT MBH
    Inventors: André Warnecke, Ivonne Müller
  • COPPER CATALYZED CYCLOADDITION OF ORGANIC AZIDES AND 1-HALOALKYNES
    Publication number: 20120142935
    Abstract: This invention provides a method for preparing a 1,2,3-triazole compound comprising contacting an organic azide with a 2-substituted-1-haloalkyne, in the presence of a copper catalyst and a copper-coordinating ligand (preferably a tertiary amine) in a liquid reaction medium, thereby forming a 1,4,5-substituted-1,2,3-triazole compound including a halo substituent at the 5-position of the triazole, the organic portion of the organic azide at the 1-position of the triazole, and the substituent of the 1-iodoalkyne at the 4-position of the triazole. A method for preparing 1-iodoalkynes is also provided.
    Type: Application
    Filed: August 11, 2010
    Publication date: June 7, 2012
    Inventors: Jason E. Hein, Jonathan C. Tripp, Larissa Krasnova, K.Barry Sharpless, Valery V. Fokin
  • 1,2,3-triazole derivatives as sigma receptor inhibitors
    Patent number: 8193223
    Abstract: The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to 1,2,3-triazole derivatives of formula (I) and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis or pain.
    Type: Grant
    Filed: November 7, 2007
    Date of Patent: June 5, 2012
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Nadine Jagerovic, Cristina Ana Gomez-De La Oliva, Maria Pilar Goya-Laza, Alberto Dordal Zueras, Maria Rosa Cuberes-Altisent
  • SYNTHESIS OF NOVEL MULTIFUNCTIONAL CARDANOL'S DERIVATIVES AND THEIR USE AS HALOGEN FREE POLYURETHANIC FOAMS PRECURSORS
    Publication number: 20120129963
    Abstract: Cardanol derivative comprising one or more units of the formula and a method for obtaining such cardanol derivative.
    Type: Application
    Filed: July 8, 2009
    Publication date: May 24, 2012
    Inventors: Elena Benedetti, Pietro Campaner, Daniele D'Amico, Andrea Minigher, Cristina Stifani, Antonella Tarzia
  • METALLOENZYME INHIBITOR COMPOUNDS
    Publication number: 20120129886
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: November 10, 2011
    Publication date: May 24, 2012
    Applicant: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
  • Process for the preparation of rufinamide
    Patent number: 8183269
    Abstract: The present invention relates to a process for the preparation of rufinamide of formula I, which process comprises: (i) reacting a 2,6-difluorobenzylhalide of formula II, wherein X is chloride, bromide or iodide, with an azide to obtain 2-(azidomethyl)-1,3-difluorobenzene of formula III; (ii) reacting 2-(azidomethyl)-1,3-difluorobenzene of formula III with methyl propiolate to obtain methyl 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylate of formula IV; and (iii) reacting methyl 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylate of formula IV with ammonia to obtain rufinamide of formula I.
    Type: Grant
    Filed: October 9, 2009
    Date of Patent: May 22, 2012
    Assignee: CIPLA Limited
    Inventors: Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao, Dilip Ramdas Birari
  • Compounds, Compositions and Methods for Modulating Uric Acid Levels
    Publication number: 20120122780
    Abstract: Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: May 20, 2010
    Publication date: May 17, 2012
    Applicant: Ardea Biosciences Inc.
    Inventors: Martha De La Rosa, Jean-Luc Girardet
  • NOVEL TRIAZOLE COMPOUNDS II
    Publication number: 20120115868
    Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u, v, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. The compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
    Type: Application
    Filed: November 2, 2011
    Publication date: May 10, 2012
    Inventors: Stephen Deems Gabriel, Andrew Thomas
  • Insecticidal Arylpyrrolines
    Publication number: 20120108635
    Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.
    Type: Application
    Filed: May 18, 2010
    Publication date: May 3, 2012
    Applicant: Bayer CropScience AG
    Inventors: Tetsuya Murata, Yasushi Yoneta, Hidetoshi Kishikawa, Jun Mihara, Daiei Yamazaki, Mamoru Hatazawa, Norio Sasaki, Kei Domon, Eiichi Shimojo, Teruyuki Ichihara, Katsuhiko Shibuya, Masashi Ataka, Ulrich Görgens
  • 18F-LABELED AZIDE COMPOUND, REAGENT FOR 18F-LABELING AND METHOD FOR 18F-LABELING OF ALKYNE COMPOUND USING SAME
    Publication number: 20120101266
    Abstract: [OBJECT] The present invention provides an 18F-labeled azide compound usable in the Huisgen reaction which enables 18F-labeling although only a small quantity of alkyne compound is available as a counterpart substrate, more specifically the 18F-labeled azide compound enabling the PET to be applied to peptides or oligonucleotides and enabling the 18F-labeling of any sites of oligonucleotide other than the 5? end or 3? end thereof, a reagent for 18F-labeling, and a method for 18F-labeling of an alkyne compound using the same. [SOLVING MEANS] An 18F-labeled azide compound according to the present invention is expressed by the following structural formula 1.
    Type: Application
    Filed: May 14, 2010
    Publication date: April 26, 2012
    Applicant: RIKEN
    Inventors: Yasuyoshi Watanabe, Masaaki Suzuki, Hisashi Doi, Takeshi Kuboyama, Satoshi Obika, Takeshi Imanichi
  • HISTONE DEACETYLASE INHIBITORS
    Publication number: 20120101099
    Abstract: The disclosure provides compounds of formula I and methods for preparation thereof. The compounds act as inhibitor of histone deacetylase.
    Type: Application
    Filed: July 7, 2010
    Publication date: April 26, 2012
    Applicant: ANTHEM BIOSCIENCES PRIVATE LIMITED
    Inventors: Natesan Selvakumar, Gavara Govinda Rajulu, Annamalai Pazhanimuthu, Sambasivam Ganesh
  • METHOD FOR PREPARING MOLECULARLY IMPRINTED POLYMERS (MIP) THROUGH RADICAL POLYMERISATION
    Publication number: 20120100358
    Abstract: The invention relates to a method for preparing molecular imprint polymers (MIP) by radical polymerisation that uses at least one primer including at least two chemical functions capable of forming reactive radicals, thereby providing a locally high radical concentration for priming the polymerisation on or about the imprint entity or molecule. The invention also relates to molecular imprint polymers (MIP) that can be obtained by the method of the invention, and to the use thereof in the production of biomimetic biosensors, biomimetic biochips, chemical sensors, specific adsorption separation devices, as a coating, particularly for releasing active ingredients.
    Type: Application
    Filed: September 1, 2009
    Publication date: April 26, 2012
    Applicant: Universite De Technologie De Compiegne - UTC
    Inventors: Karsten Haupt, Arnaud Cutivet, Jeanne Bernadette Tse Sum Bui, Pinar Cakir
  • PET RADIOTRACERS FOR IMAGING FATTY ACID METABOLISM AND STORAGE
    Publication number: 20120100073
    Abstract: Fatty acid analogue (FAA) molecules comprising positron-emitting radionuclides, salts thereof, and FAA-triglycerides are disclosed. Also disclosed are methods of synthesis, and methods of imaging distribution and metabolism of fatty acids and fatty acid triglycerides.
    Type: Application
    Filed: May 4, 2010
    Publication date: April 26, 2012
    Applicant: WASHINGTON UNIVERSITY
    Inventors: Robert H. Mach, Robert John Gropler, Zhude Tu, Pilar Herrero
  • Ultraviolet light absorbing ketones of 2-(2-hydroxyphenyl) benzotriazole
    Patent number: 8163934
    Abstract: The invention relates to ultraviolet light absorbing compounds, their preparation and uses as protective agents and stabilizers in coatings, plastics and topically applied products. The compounds are ketone derivatives of 2-(2-hydroxyphenol)benzotriazole of formula I, where R1 is hydrogen atom, or a halogen atom, or a straight-chain or branched lower alkyl or lower alkoxy of 1 to 4 carbon atoms; R2 is an unsubtituted or substituted aryl group or an unsubstituted or substituted straight-chain or branched alkyl having 1 to 18 carbon atoms or a cycloaliphatic group having 5 to 6 carbon atoms; and R3 is a straight-chain or branched alkyl or alkylaryl group or alkoxyl or phenyl or phenyl substituted with alkyl, cycloalkyl, carboalkoxy, chlorine or arylalkyl groups.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: April 24, 2012
    Inventor: Chia-Hu Chang
  • Triazolone derivatives
    Patent number: 8163787
    Abstract: A compound represented by the following general formula (1) or salts thereof or hydrates of the foregoing: wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: April 24, 2012
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Richard Clark, Fumiyoshi Matsuura, Kazunobu Kira, Shinsuke Hirota, Hiroshi Azuma, Tadashi Nagakura, Tatsuo Horizoe, Kimiyo Tabata, Kazutomi Kusano, Takao Omae, Atsushi Inoue
  • NOVEL HERBICIDES
    Publication number: 20120094832
    Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Application
    Filed: August 6, 2008
    Publication date: April 19, 2012
    Applicant: SYNGENTA LIMITED
    Inventors: Melloney Tyte, Christopher John Mathews, Gavin John Hall, William Guy Whittingham, Jeffrey Steven Wailes, James Nicholas Scutt, Stephane André Marie Jeanmart, Russell Viner
  • Fluorogenic compounds converted to fluorophores by photochemical or chemical means and their use in biological systems
    Patent number: 8153446
    Abstract: Fluorophores derived from photoactivatable azide-pi-acceptor fluorogens or from a thermal reaction of an azide-pi-acceptor fluorogen with an alkene or alkyne are disclosed. Fluorophores derived from a thermal reaction of an alkyne-pi-acceptor fluorogen with an azide are also disclosed. The fluorophores can readily be activated by light and can be used to label a biomolecule and imaged on a single-molecule level in living cells.
    Type: Grant
    Filed: May 13, 2009
    Date of Patent: April 10, 2012
    Assignees: Kent State University, Leland Stanford Junior University
    Inventors: Robert J. Twieg, William E. Moerner, Samuel J. Lord, Na Liu, Reichel Samuel
  • UV/visible light absorbers for ophthalmic lens materials
    Patent number: 8153703
    Abstract: Benzotriazole UV/Visible light-absorbing monomers are disclosed. The UV/Vis absorbers are particularly suitable for use in intraocular lens materials.
    Type: Grant
    Filed: November 3, 2009
    Date of Patent: April 10, 2012
    Assignee: Novartis AG
    Inventor: Walter R. Laredo
  • Synthesis of methyl nonactate derivatives
    Patent number: 8153817
    Abstract: Methyl nonactate is converted into a variety of different triazoloamide antibacterial agents by a reaction scheme involving (1) inversion of the secondary alcohol of the methyl nonactate to produce the corresponding azidoester, (2) converting the azido ester to the corresponding azidoamide, and (3) converting the azido group of the azidoamide to a triazole to produce the corresponding triazoloamide.
    Type: Grant
    Filed: September 11, 2007
    Date of Patent: April 10, 2012
    Assignee: Ohio University
    Inventors: Stephen C. Bergmeier, Nigel D. Priestley
  • Small molecule apoptosis promoters
    Publication number: 20120082640
    Abstract: The invention provides small molecule mimics of the Smac peptide that are dimer- or dimer-like compounds having two amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.
    Type: Application
    Filed: October 4, 2010
    Publication date: April 5, 2012
    Inventors: Gunnar J. Hanson, David Thomas, Nizal Chandrakumar, Susan Harran
  • INDOLE AMIDE DERIVATIVES AND RELATED COMPOUNDS FOR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES
    Publication number: 20120083475
    Abstract: This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic ?-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.
    Type: Application
    Filed: June 11, 2010
    Publication date: April 5, 2012
    Inventors: Gerard Griffioen, Tom Van Dooren, Veronica Rojas De La Parra, Arnaud Marchand, Sara Allasia, Amuri Kilonda, Patrick Chaltin
  • Heterocyclic compounds as factor IXA inhibitors
    Patent number: 8148363
    Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: April 3, 2012
    Assignee: Schering Corporation
    Inventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick, Liyuan Wang, Xiaobang Gao
  • Anti-mitotic anti-proliferative compounds
    Patent number: 8143299
    Abstract: Substituted triazole compounds and pharmaceutical compositions thereof are presented. Also presented are methods for treating a pathology linked to a hyperproliferative disorder by administering the substituted triazole compounds to a patient in need thereof.
    Type: Grant
    Filed: October 25, 2005
    Date of Patent: March 27, 2012
    Assignee: University of Medicine and Dentistry of New Jersey
    Inventors: William J. Welsh, Youyi Peng, Xin Wang, Susan M. Keenan, Qiang Zhang, Sonia Arora
  • Dimeric small molecule potentiators of apoptosis
    Patent number: 8143418
    Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
    Type: Grant
    Filed: February 7, 2011
    Date of Patent: March 27, 2012
    Assignee: Board of Regents, The University of Texas System
    Inventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki