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)
  • Crystal modification A of 1-(2,6-difluorobenzyl)-1 H-1,2,3-triazole-4-carboxamide and dosage forms and formulations thereof
    Publication number: 20100310655
    Abstract: The invention relates to dosage forms and formulations comprising the novel crystal modification A of the compound I-(2, 6-difluorobenzyl)-I H-I,2,3-triazole-4-carboxamide, wherein crystal modification A is characterized by characteristic lines with interplanar spacings (d values) of 10.5 ?, 5.14 ?, 4.84 ?, 4.55 ?, 4.34 ?, 4.07 ?, 3.51 ?, 3.48 ?, 3.25 ?, 3.19 ?, 3.15 ?, 3.07 ?, and 2.81 ?, determined by means of an X-ray powder pattern. Dosage forms of crystal modification A of the compound I-(2, 6-difluorobenzyl)-I H-I,2,3-triazole-4-carboxamide may be for oral or parenteral administration, in the form of a solid or liquid, and in a dosage range of 20 mg to less than 500 mg. Solid dosage forms comprise a tablet or capsule, and further comprise a pharmaceutically-acceptable carrier and film-coat.
    Type: Application
    Filed: April 26, 2010
    Publication date: December 9, 2010
    Inventors: Robert Portmann, Urs Christoph Hofmeier, Andreas Burkhard, Walter Scherrer, Martin Szelagiewicz
  • NOVEL COLORANT COMPOUND AND BLUE RESIST COMPOSITION FOR USE IN COLOR FILTER CONTAINING THE SAME
    Publication number: 20100308285
    Abstract: The present invention provides (I) a method of manufacturing a triphenylmethane colorant that can suppress the sub-reactions in conversion to a sulfonamide and is industrially advantageous, (II) a colorant compound that has both excellent spectral characteristics and a high solubility relative to organic solvents or polymers as a coloring agent to be used in color filters and (III) a blue resist composition for use in a color filter that shows a high lightness and an excellent hue particularly for blue color and can be used to display an image that is excellent in terms of spectral characteristics and contrast.
    Type: Application
    Filed: August 19, 2010
    Publication date: December 9, 2010
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Yasuaki Murai, Takayuki Toyoda, Yuko Yamagishi, Takeshi Miyazaki
  • Ultraviolet light absorbing ketones of 2-(2-hydroxyphenyl) benzotriazole
    Patent number: 7847103
    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 unsubstituted 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 4, 2008
    Date of Patent: December 7, 2010
    Inventor: Chia-Hu Chang
  • 1,2,3-TRIAZOLE DERIVATIVES FOR USE AS STEAROYL-COA DESATURASE INHIBITORS
    Publication number: 20100297054
    Abstract: The present invention relates to substituted triazole compounds of the formula (I): and pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for modulating SCD activity.
    Type: Application
    Filed: November 7, 2008
    Publication date: November 25, 2010
    Inventors: Anne Marie Jeanne Bouillot, Alain Laroze, Lionel Trottet
  • Photoresponsive Base Having Triazole Skeleton
    Publication number: 20100298530
    Abstract: To provide a photocrosslinkable compound and a photocrosslinking agent which are capable of ligation of nucleic acids within a short period of time compared to the conventional cases, and to which modifications depending on the intended use can easily be made, and a method of producing the photocrosslinking agent. Nucleic acids including a group represented by the formulae I, III, IV, or V as a nucleobase; a photocrosslinking agent including the nucleic acids, a method of producing nucleic acids by reacting nucleic acids including a group represented by the formulae VI, VII, VIII, or IX as a nucleobase with an aromatic azidated product represented by the formula X.
    Type: Application
    Filed: May 14, 2010
    Publication date: November 25, 2010
    Applicant: TOPPAN PRINTING CO., LTD.
    Inventors: KENZOU FUJIMOTO, TAKEHIRO AMI, CHIFUMI NAGATA, AKIO YAMANE
  • NOVEL DIARYLPHOSPHINE- AND DIALKYLPHOSPHINE-CONTAINING COMPOUNDS, PROCESSES OF PREPARING SAME AND USES THEREOF AS TRIDENTATE LIGANDS
    Publication number: 20100292084
    Abstract: A novel process of preparing tridentate ligands containing one or more of a diarylphosphine and/or dialkylphosphine electron donating groups are disclosed. Use of this process for preparing a combinatorial library of such tridentate ligands and of organometallic complexes containing same is also disclosed. Further disclosed are novel diarylphosphine-containing and dialkylphosphine-containing compounds that can serve as tridentate ligands (e.g., pincer ligands), combinatorial libraries of such tridentate ligands, organometallic complexes containing these ligands (e.g., pincer complexes), and combinatorial libraries of such complexes. Methods utilizing these libraries for screening for candidate organometallic catalysts are also disclosed. Novel precursor molecules useful for preparing the tridentate ligands and processes of preparing same are also disclosed.
    Type: Application
    Filed: May 13, 2010
    Publication date: November 18, 2010
    Applicant: Technion Research & Development Foundation Ltd.
    Inventors: Mark GANDELMAN, Elaine Melissa Schuster, Gennady Nisnevich
  • NOVEL TUBULIN POLYMERISATION INHIBITORS
    Publication number: 20100292190
    Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.
    Type: Application
    Filed: February 14, 2006
    Publication date: November 18, 2010
    Applicant: Bionomics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
  • Methods for preparing nonpeptidic oligomers from amino acids
    Patent number: 7834038
    Abstract: The present invention relates to nonpeptidic oligomers. Methods for preparing nonpeptidic oligomers from amino acids by replacing the amide bond with heterocyclic rings are also disclosed.
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: November 16, 2010
    Assignee: New York University
    Inventors: Paramjit S. Arora, Nicholas G. Angelo
  • Ruthenium-Catalyzed Cycloaddition of Alkynes and Organic Azides
    Publication number: 20100286405
    Abstract: A convenient process for the regioselective synthesis of 1,5-disubstituted 1,2,3-triazoles and 1,4,5-trisubstituted 1,2,3-triazoles from organic azides and alkynes employs catalytic ruthenium.
    Type: Application
    Filed: September 29, 2006
    Publication date: November 11, 2010
    Inventors: Valery Fokin, Guocheng Jia, K. Barry Sharpless
  • 1H-[1, 2, 3] TRIAZOLE SUBSTITUTED AMINO ACIDS AND USES THEREOF
    Publication number: 20100278732
    Abstract: Tracers for cationic amino acid transport systems and methods of synthesis are disclosed, including compounds comprising a 1H-[1,2,3]triazole moiety. Further disclosed are uses of the analogues, including in vivo imaging of tumors by Positron emission tomography (PET) or Single Photon Emission Computed Tomography (SPECT).
    Type: Application
    Filed: May 3, 2010
    Publication date: November 4, 2010
    Applicant: WASHINGTON UNIVERSITY
    Inventors: Robert H. Mach, Jonathan McConathy
  • BETULIN DERIVED COMPOUNDS USEFUL AS ANTIBACTERIAL AGENTS
    Publication number: 20100273801
    Abstract: The invention relates to compouns derived from betulin, and to the use thereof as antibacterial agents in pharmaceutical and cosmetic applications.
    Type: Application
    Filed: June 6, 2007
    Publication date: October 28, 2010
    Applicant: Valition teknillinen tutikimuskeskus
    Inventors: Jari Yli-Kauhaluoma, Salme Koskimies, Sami Alakurtti, Taru Mäkelä, Päivi Tammela
  • N-substituted-azacyclylamines as histamine-3 antagonists
    Patent number: 7820825
    Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
    Type: Grant
    Filed: March 14, 2007
    Date of Patent: October 26, 2010
    Assignee: Wyeth LLC
    Inventors: Derek Cecil Cole, Magda Asselin, Joseph Raymond Stock, Albert Jean Robichaud, Ji-In Kim, William Ronald Solvibile, Jonathan Laird Gross
  • MIF MODULATORS
    Publication number: 20100267714
    Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.
    Type: Application
    Filed: May 4, 2010
    Publication date: October 21, 2010
    Inventors: William L. Jorgensen, Richard J. Bucala
  • INHIBITORS OF Akt ACTIVITY
    Publication number: 20100267759
    Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
    Type: Application
    Filed: February 7, 2008
    Publication date: October 21, 2010
    Applicant: SMITHKLINE BEECHAM CORPORATION
    Inventors: Mark A. Seefeld, Meagan B. Rouse, Dirk A. Heerding, Simon Peace, Dennis S. Yamashita, Kenneth C. McNulty
  • Triazolone derivatives
    Patent number: 7816522
    Abstract: A Compound represented by the following general formula (1), salts thereof or hydrates of the foregoing is a novel compound useful for treatment and/or prevention of diseases associated with thrombus formation, and which is safer with suitable physicochemical stability. [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.
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: October 19, 2010
    Assignee: Eisai 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
  • Amido-organoborate initiator systems
    Patent number: 7816562
    Abstract: The invention is amido-borate compounds containing one or more anionic amido-borate moieties comprising an organoborate anion wherein the boron atom is bonded to a nitrogen atom of ammonia or an organic compound containing one or more nitrogen atoms, such as a hydrocarbyl amine, a hydrocarbyl polyamine, or an aromatic heterocycle containing one or more nitrogen atoms, and a cationic counter ion.
    Type: Grant
    Filed: October 6, 2006
    Date of Patent: October 19, 2010
    Assignee: Dow Global Technologies Inc.
    Inventors: Shaoguang Feng, Gary L. Jialanella, Peter Nickias, Toni Ristoski
  • Dimeric small molecule potentiators of apoptosis
    Patent number: 7816538
    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: July 24, 2009
    Date of Patent: October 19, 2010
    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
  • Imidazole derivatives having a positive allosteric GABAreceptor modulator effect and methods of use
    Patent number: 7812026
    Abstract: The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and R4 are as defined in the description. For example, R1 may be phenyl, R2 may be dimethylamino pyrrolidin-1-yl, R3 may be alkoxy and R4 may be alkyl, ai arylalkyl, aryloxyalkyl, aryloxy or heterocyclylalkyl.
    Type: Grant
    Filed: December 21, 2006
    Date of Patent: October 12, 2010
    Assignee: AstraZeneca AB
    Inventors: Udo Bauer, Wayne Brailsford, Linda Gustafsson, Tor Svensson
  • INHIBITORS OF IAP
    Publication number: 20100256115
    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: March 18, 2010
    Publication date: October 7, 2010
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • Nitro-imidazole hypoxia imaging agents
    Patent number: 7807394
    Abstract: The present invention relates to novel radioactively labeled bioreducible tracers of Formula I useful for detecting hypoxic tumors or ischemic tissue in vivo. In one embodiment, the tracers consist of a 2-nitroimidazole moiety, a triazole, metabolically stable linker with pharmacokinetics enhancing substituents, and a radioisotope. The preferred in vivo imaging modality is positron emission tomography.
    Type: Grant
    Filed: April 4, 2008
    Date of Patent: October 5, 2010
    Assignee: Siemens Medical Solutions USA, Inc.
    Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Umesh B. Gangadharmath, Farhad Karimi, Henry Clifton Padgett, Dhanalakshmi Kasi, Zhiyong Gao, Qianwa Liang, Thomas Lee Collier, Brian A. Duclos, Tieming Zhao
  • Dimeric pyrrolidine amide-containing small molecule apoptosis promoters
    Patent number: 7807699
    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: Grant
    Filed: March 21, 2007
    Date of Patent: October 5, 2010
    Assignee: Joyant Pharmaceuticals, Inc.
    Inventors: Gunnar J. Hanson, David Thomas, Nizal Chandrakumar, Susan Harran
  • Triazole derivative and use thereof
    Patent number: 7803822
    Abstract: The present invention relates to a thrombin receptor antagonist containing a compound represented by the formula (I) wherein R1a, R1b and R2 are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted alkoxy, R3 is a group represented by the formula —NHCOR4, —NHSO2R5, —NHCON(R6a)(R6b), —NHCOOR7 or —CONHR8 wherein R4, R5, R6a, R6b, R7 and R8 are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group and the like), ring A is monocyclic aromatic ring optionally further having substituent(s), R1a and R1b are optionally bonded to each other to form an optionally substituted nitrogen-containing non-aromatic heterocycle, or a salt thereof or a prodrug thereof.
    Type: Grant
    Filed: April 6, 2006
    Date of Patent: September 28, 2010
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Keiji Kubo, Mamoru Tobisu, Eiji Honda, Takahiko Taniguchi, Yoshiyuki Fukase, Masaki Kawamura, Masaharu Nakayama
  • CHEMICAL COMPOUNDS
    Publication number: 20100240657
    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 characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition with the above-mentioned properties.
    Type: Application
    Filed: July 1, 2008
    Publication date: September 23, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Ioannis Sapountzis, Peter Ettmayer, Christian Klein, Andreas Mantoulidis, Martin Steegmaier, Steffen Steurer, Irene Waizenegger
  • Novel Curcumin and Tetrahydrocurcumin Derivatives
    Publication number: 20100240905
    Abstract: The invention relates to novel curcumin and tetrahydrocurcumin derivatives, which have been modified at one phenolic group to incorporate more-reactive groups. The curcumin and tetrahydrocurcumin derivatives are in the form of monomers, dimmers, and polymers.
    Type: Application
    Filed: October 12, 2007
    Publication date: September 23, 2010
    Applicant: RESEARCH FOUNDATION OF CITY UNIVERSITY OF NEW YORK
    Inventors: Krishnaswami Raja, Probal Banerjee, Andrew Auerbach, Wei Shi, William L'Amoreaux
  • ALKYLSULFONAMIDE-SUBSTITUTED TRIAZOLES AS MATRIX METALLOPROTEASE INHIBITORS
    Publication number: 20100234378
    Abstract: Provided are MMP-2, MMP-3, MMP-9, MMP-12 and/or MMP-13 inhibitors having the Formula (I): wherein R2, R3, R4, R5, and Y are as defined herein, which are useful in the treatment and/or prevention of MMP mediated diseases and disorders.
    Type: Application
    Filed: August 21, 2007
    Publication date: September 16, 2010
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Andrew M. Fryer, James Rizzi
  • METHOD FOR THE PREPARATION OF RUFINAMIDE
    Publication number: 20100234616
    Abstract: The invention provides a novel process for the regioselective preparation of a compound of formula (I)
    Type: Application
    Filed: March 12, 2010
    Publication date: September 16, 2010
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Emanuele ATTOLINO, Lino COLOMBO, Ilaria MORMINO, Pietro ALLEGRINI
  • Process for the synthesis of triazoles
    Publication number: 20100234615
    Abstract: The present invention relates to processes for the preparation of triazoles. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.
    Type: Application
    Filed: June 8, 2006
    Publication date: September 16, 2010
    Inventors: Shili Chen, Rongliang Lou, Yusheng Wu, Jiacheng Zhou, Roger Hanselmann
  • NOVEL MICROBIOCIDES
    Publication number: 20100222389
    Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Application
    Filed: June 13, 2008
    Publication date: September 2, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Harald Walter, Daniel Stierli, Hans Tobler
  • Process For The Preparation Of Onium Alkylsulfates Having A Low Halide Content
    Publication number: 20100222580
    Abstract: The invention relates to a process for the preparation of onium alkylsulfates by reaction of an onium halide with a symmetrically substituted dialkyl sulfate, in which the alkyl group can have 1 to 14 C atoms, with an asymmetrically substituted dialkyl sulfate, in which one alkyl group can have 4 to 20 C atoms and the second alkyl group denotes methyl or ethyl, with an alkyl trialkylsilyl sulfate, with an alkyl acyl sulfate or with an alkyl sulfonyl sulfate, where the reaction with a dialkyl sulfate is carried out at room temperature.
    Type: Application
    Filed: November 18, 2005
    Publication date: September 2, 2010
    Applicant: MERCK PATENT GMBH
    Inventors: Nikolai Ignatyev, Urs Welz-Biermann, Andriy Kucheryna, Helge Willner
  • METHODS AND COMPOSITIONS FOR PROTEIN LABELLING
    Publication number: 20100221176
    Abstract: A modular platform is provided for rapid preparation of various water-soluble prosthetic groups capable to efficiently introduce 18F into proteins with 18F labelling reagents.
    Type: Application
    Filed: February 25, 2010
    Publication date: September 2, 2010
    Inventors: Herman Gill, Jan Marik, Jeff Tinianow, Simon Williams
  • NOVEL 1,2,3-TRIAZOLE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
    Publication number: 20100222398
    Abstract: This invention relates to novel 1,2,3-triazole derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Application
    Filed: August 6, 2008
    Publication date: September 2, 2010
    Applicant: NeuroSearch A/S
    Inventors: Antonio Nardi, Jeppe Kejser Christensen, Dan Peters, Gunnar M. Olsen, Tino Dyhring
  • 2-Oxo-1-pyrrolidine derivatives, processes for preparing them and their uses
    Publication number: 20100222576
    Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.
    Type: Application
    Filed: February 17, 2010
    Publication date: September 2, 2010
    Inventors: Edmond Differding, Benoît Kenda, Bénédicte Lallemand, Alain Matagne, Philippe Michel, Patrick Pasau, Patrice Talaga
  • TRIAZOLE DERIVATIVES FOR TREATING ALZHEIMER'S DISEASE AND RELATED CONDITIONS
    Publication number: 20100222320
    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: Application
    Filed: June 9, 2008
    Publication date: September 2, 2010
    Inventors: Christian Fischer, Ben Munoz, Susan Zultanski, Joey Methot, Hua Zhou, W. Colby Brown
  • LINKED DIBENZIMIDAZOLE DERIVATIVES
    Publication number: 20100221215
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: February 9, 2010
    Publication date: September 2, 2010
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Pesticidal arylpyrrolidines
    Publication number: 20100216792
    Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
    Type: Application
    Filed: October 14, 2009
    Publication date: August 26, 2010
    Applicant: Bayer CropScience AG
    Inventors: Ulrich Görgens, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
  • NOVEL CHROMOPHORIC SILYL PROTECTING GROUPS AND THEIR USE IN THE CHEMICAL SYNTHESIS OF OLIGONUCLEOTIDES
    Publication number: 20100216984
    Abstract: The present invention provides compounds of the formula (I): C-Q-O—Si(R1)(R2)—N wherein C is a chromophore; Q is selected from the group consisting of optionally substituted aliphatic, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R1 and R2 are independently selected from the group consisting of optionally substituted C1-8 alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C1-8 alkyloxy, cycloalkyloxy, heterocycloalkyloxy, alkylsilyloxy and arylsilyloxy; and N is a glycosylamine or abasic moiety.
    Type: Application
    Filed: May 16, 2008
    Publication date: August 26, 2010
    Applicant: Dharmacon, Inc.
    Inventor: Michael Oren Delaney
  • Compounds and uses thereof in modulating amyloid beta
    Patent number: 7781442
    Abstract: Novel compounds, compositions, and kits are provided. Methods of modulating A? levels, and methods of treating a disease associated with aberrant A? levels are also provided.
    Type: Grant
    Filed: July 17, 2007
    Date of Patent: August 24, 2010
    Assignee: Neurogenetic Pharmaceuticals, Inc.
    Inventors: Soan Cheng, Daniel D. Comer, Long Mao, Guity P. Balow, David Pleynet
  • Compounds for the treatment of proliferative disorders
    Patent number: 7781462
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
    Type: Grant
    Filed: July 24, 2006
    Date of Patent: August 24, 2010
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Zachary Demko, Christopher Borella, Shoujun Chen, Lijun Sun
  • Substituted heterocyclic compounds with CXCR3 antagonist activity
    Patent number: 7781437
    Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.
    Type: Grant
    Filed: October 10, 2006
    Date of Patent: August 24, 2010
    Assignee: Schering Corporation
    Inventors: Seong Heon Kim, Bandarpalle B. Shankar, Joseph A. Kozlowski, Stuart B. Rosenblum, Neng-Yang Shih
  • CINNAMOYL INHIBITORS OF TRANSGLUTAMINASE
    Publication number: 20100204280
    Abstract: A compound of Formula, (I) or Formula: (II)
    Type: Application
    Filed: May 29, 2008
    Publication date: August 12, 2010
    Applicant: UNIVERSITE DE MONTREAL
    Inventors: Christophe Pardin, Jeffrey W. Keillor, William D. Lubell
  • Surface modifying agent, laminated structure and transistor including the same, and method of manufacturing the laminated structure
    Publication number: 20100200842
    Abstract: Disclosed is a surface modifying agent including a compound having an ethynyl group at one terminal end, a laminated structure manufactured using the surface modifying agent, a method of manufacturing the laminated structure, and a transistor including the same.
    Type: Application
    Filed: February 12, 2010
    Publication date: August 12, 2010
    Inventors: Jeong-il Park, Byung-Wook Yoo, Do-hwan Kim, Sang-Yoon Lee, Bang-lin Lee, Eun-jeong Jeong
  • LIGANDS FOR COPPER-CATALYZED AZIDE-ALKYNE CYCLOADDITION REACTIONS
    Publication number: 20100197871
    Abstract: Ligands useful for promoting copper-catalyzed azide-alkyne cycloaddition reactions comprise a compound represented by structural Formula (I) as described in the specification, wherein in Formula (I) Z1 is a nitrogen-containing heterocyclic group or a group represented by the formula: Y1—(CH2)c—Y2—(CH2)d—Y3—CH2—N(CH2Z4)(CH2Z5), where Y1 is -E1-C(O)O—, -E1-C(O)NH—, -E1-, or a covalent bond; Y2 is a covalent bond, —CH?CH—, or a 1,4-(1,2,3-triazolyl) group; Y3 is —OC(O)-E2-, —NHC(O)-E2-, -E2-, or a covalent bond; each of E1 and E2 is a benzimidazolyl group attached at the 1 and 2 positions; each of c and d is independently 1, 2, 3, 4, or 5; each of Z2, Z3, Z4 and Z5 is a nitrogen-containing heterocyclic group including a substituent X1 and optionally including a substituent (CH2)n—R1, and Y1, Y2, Y3, X1, R1, c, d and n are each as defined in the specification.
    Type: Application
    Filed: September 15, 2008
    Publication date: August 5, 2010
    Inventors: M.G. Finn, Valentin O. Rodionov
  • Copper-catalysed ligation of azides and acetylenes
    Patent number: 7763736
    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: Grant
    Filed: May 9, 2008
    Date of Patent: July 27, 2010
    Assignee: The Scripps Research Institute
    Inventors: K. Barry Sharpless, Valery Fokin, Vsevold V. Rostovtsev, Luke Green, Fahmi Himo
  • AGONISTS OF PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR-ALPHA
    Publication number: 20100184815
    Abstract: Disclosed are compounds of the formula: And pharmaceutically acceptable salts thereof, wherein the variables are as defined herein, which are useful in activating PPAR? and in treating atherosclerosis hypercholesterolemia, primary hypercholesterolemia or mixed dyslipidemia, hypertriglyceridemia, Frederickson Types IV and V hyperlipidemia. Pharmaceutical compositions, intermediates useful in the preparation of the compounds of formula I and methods of making the compounds of formula I are also disclosed.
    Type: Application
    Filed: December 18, 2009
    Publication date: July 22, 2010
    Inventors: Gary W. Luehr, Arathi Sundaram, Priya Jaishankar, Chhaya Bhakta, Pascal Druzgala
  • HIGH CHARGE DENSITY STRUCTURES, INCLUDING CARBON-BASED NANOSTRUCTURES AND APPLICATIONS THEREOF
    Publication number: 20100179054
    Abstract: The present invention generally provides compositions including carbon-based nanostructures, catalyst materials and systems, and related methods. In some cases, the present invention relates to carbon-based nanostructures comprising a high density of charged moieties. Methods of the invention may provide the ability to introduce a wide range of charged moieties to carbon-based nanostructures. The present invention may provide a facile and modular approach to synthesizing molecules that may be useful in various applications including sensors, catalysts, and electrodes.
    Type: Application
    Filed: December 11, 2009
    Publication date: July 15, 2010
    Applicant: Massachusetts Institute of Technology
    Inventors: Timothy M. Swager, Jan Schnorr
  • SUBSTITUTED N-PHENYL-BIPYRROLIDINE CARBOXAMIDES AND THERAPEUTIC USE THEREOF
    Publication number: 20100173897
    Abstract: The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.
    Type: Application
    Filed: March 15, 2010
    Publication date: July 8, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Werngard CZECHTIZKY, Zhongli GAO, William J. HURST, Lothar SCHWINK, Siegfried STENGELIN
  • Crystal modifications of 1-(2,6-difluorobenzyl)-1H-1, 2,3-triazole-4-carboxamide
    Patent number: 7750028
    Abstract: The invention relates to the novel modifications B and C of the compound 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide of the formula its use and pharmaceutical preparations comprising this crystal modifications.
    Type: Grant
    Filed: January 11, 2006
    Date of Patent: July 6, 2010
    Assignee: Novartis AG
    Inventors: Robert Portmann, Urs C Hofmeier, Andreas Burkhard, Walter Scherrer, Martin Szelagiewicz
  • Cholesteryl Ester Transfer Protein Inhibitors
    Publication number: 20100167986
    Abstract: Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring, and Z is an aromatic or heterocyclic ring.
    Type: Application
    Filed: September 28, 2006
    Publication date: July 1, 2010
    Inventors: Amjad Ali, Peter J. Sinclair
  • THERAPEUTIC SUBSTITUTED LACTAMS
    Publication number: 20100168189
    Abstract: Therapeutic compounds, compositions, methods, and medicaments related thereto are disclosed herein.
    Type: Application
    Filed: February 8, 2008
    Publication date: July 1, 2010
    Inventors: David W. Old, Wha Bin Im, Vinh X. Ngo
  • ANTIMICROBIAL N-CHLORINATED COMPOSITIONS
    Publication number: 20100158818
    Abstract: The present application relates to N-chlorinated cationic compounds of Formula I or a salt thereof, and associated compositions and methods of use as antimicrobial agents.
    Type: Application
    Filed: November 6, 2009
    Publication date: June 24, 2010
    Inventors: Rakesh K. Jain, Eddy Low, Charles Francavilla, Timothy P. Shiau, Satheesh K. Nair