Abstract: An azolylmethylidenehydrazine derivative represented by the formula (I) wherein Ar is an aryl group optionally having substituent(s) or a heteroaryl group optionally having substituent(s), R1 and R2 are the same or different and each is an alkyl group, a cycloalkyl group, an aralkyl group optionally having substituent(s), an aryl group optionally having substituent(s), a heteroarylalkyl group optionally having substituent(s), or R1 and R2 are bonded to each other to form a nitrogen-containing heterocyclic group optionally having substituent(s), and X is CH or a nitrogen atom, or a pharmacologically acceptable salt thereof is useful as a medicament, particularly as an antifungal agent, or an anti-inflammatory agent or an antiallergic agent.
Abstract: The invention relates to compounds having an anti-parasitic, in particular antimalarial activity, characterized in that they correspond to general formula (I) Applications in particular as compounds with anti-parasitic activity.
Type:
Grant
Filed:
July 18, 2003
Date of Patent:
September 6, 2011
Assignee:
Centre National de la Recherche Scientifique (C.N.R.S.)
Inventors:
Henri Vial, Michele Calas, Roger Escale, Valerie Vidal, Francoise Bressolle, Marie-Laure Ancelin
Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
Type:
Grant
Filed:
October 5, 2006
Date of Patent:
August 30, 2011
Assignee:
AstraZeneca AB
Inventors:
Timothy Jon Luker, Rukhsana Tasneem Mohammed, Mark Dickinson, Stephen Thom
Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 such as obesity and diabetes.
Type:
Grant
Filed:
January 11, 2007
Date of Patent:
August 16, 2011
Assignee:
Incyte Corporation
Inventors:
Wenqing Yao, David M. Burns, Lihua Chen, Jincong Zhuo, Chunhong He
Abstract: This invention relates to novel carboxylic acid 4-phenylazo-phenyl ester derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
Type:
Grant
Filed:
November 27, 2008
Date of Patent:
August 9, 2011
Assignee:
Neurosearch A/S
Inventors:
Dan Peters, John Paul Redrobe, βlsebet Østergaard Nielsen
Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.
Type:
Grant
Filed:
October 23, 2009
Date of Patent:
August 2, 2011
Assignee:
Symphony Evolution, Inc.
Inventors:
Lynne Canne Bannen, Erick W. Co, Vasu Jammalamadaka, John M. Nuss, Moon Hwan Kim, Donna Tra Le, Amy Lew, Morrison B. Mac, Shumeye Mamo, Zhaoyang Wen, Wei Xu, Richard George Khoury
Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, or chronic pain.
Type:
Grant
Filed:
April 13, 2007
Date of Patent:
August 2, 2011
Assignee:
NeurAxon, Inc.
Inventors:
Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
Abstract: The present invention relates to screens for compounds that can induce stem cell differentiation. In addition, isoxazoles and sulfonyl hydrazones are identified as general classes of compounds that can induce differentiation of stem cells into cells of neuronal and cardiac fate, respectively.
Type:
Grant
Filed:
July 31, 2008
Date of Patent:
July 19, 2011
Assignee:
The Board of Regents of the University of Texas System
Inventors:
Eric Olson, Douglas Frantz, Jenny Hsieh, Steven L. McKnight, Jay Schneider
Abstract: The present invention provides a method for producing dry organic pigment, comprising the successive steps of, in this order: a first step wherein a wet organic pigment is obtained by drying an organic pigment presscake at 70 to 150° C. to a moisture content of 5 to 30%, and a second step wherein a dry organic pigment is obtained by pulverizing and drying the wet organic pigment at a temperature that is higher than the temperature employed in the first step but lower than the decomposition temperature of the organic pigment. The method for producing dry organic pigment enables the dry organic pigment to be obtained with superior productivity while consuming less energy than conventional methods.
Abstract: A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.
Abstract: The invention provides a method for obtaining the intermediate (II), useful for manufacturing Valsartan and a drug directed to a treatment of arterial hypertension or heart failure. The process comprises a) Imination of the aldehyde group of a compound (VII) by L-Valine (IV) salts with organic or inorganic bases and a polar solvent or water, where X means halogen or an —OSO2R group, where R is CF3, tolyl, methyl or F; to give an imine-type compound (VIII), where B+ is the protonated form of an organic base or an alkaline cation; b) Reduction of the imine group of the compound (VIII) followed by acidification, to give the compound (VI); and c) N-Acylation of the compound (VI) with valeryl chloride to give the compound (II). Steps a) and b) can be performed in a “one pot” reaction.
Type:
Grant
Filed:
October 19, 2006
Date of Patent:
June 21, 2011
Assignee:
Inke, S.A.
Inventors:
Pere Dalmases Barjoan, Joan Huguet Clotet
Abstract: To provide a dye capable of forming an anisotropic dye film showing high dichroism and having a high degree of molecular orientation, a composition containing the dye, an anisotropic dye film using the dye and a polarizing element. A trisazo dye, of which the free acid form is represented by the following formula (1), wherein at least one of B1 and D1 has at least one substituent as defined by the following Q1, a dye composition for an anisotropic dye film containing the dye, an anisotropic dye film and a polarizing element using the anisotropic dye film: Q1: an alkyl group or alkoxy group substituted by a hydrogen bond-forming group: wherein A1 is a phenyl group or a naphthyl group, each of B1 and D1 is a phenylene group or a naphthylene group, X1 is an amino group which may be substituted or a hydroxyl group, and m is 0 or 1.
Abstract: The invention provides a novel group of azo quencher compositions that are useful as quenchers of fluorescence and to methods for making and using them. The quenchers contain an azo bond and 1,3,3-trimethyl-2-methyleneindoline ring system. The quenchers can be derivatized to facilitate their conjugation to a variety of biologically relevant compounds, including lipids, nucleic acids, peptides, proteins, and the like.
Type:
Grant
Filed:
June 16, 2010
Date of Patent:
June 7, 2011
Assignee:
ChemGenes Corporation
Inventors:
Andrei Laikhter, Suresh C. Srivastava, Naveen P. Srivastava
Abstract: New polymorphs of Eltrombopag and Eltrombopag ethanolamine salt have been obtained and characterized. These polymorphs and pharmaceutical compositions comprising them are useful, for example, in treating conditions leading to thrombocytopenia.
Type:
Grant
Filed:
April 1, 2010
Date of Patent:
June 7, 2011
Assignee:
Pliva Hrvatska D.O.O.
Inventors:
Edislav Leksic, Helena Ceric, Tina Mundorfer, Irena Zrinski Antonac, Zrinka Mastelic Samardzic
Abstract: Products having the general formula A, particularly useful as non-coloring markers in a process for tagging mineral oils, petroleum derivatives in general and solvents. A method is also described for synthesizing the products by resorting to a classical diazocoupling reaction between a derivative of an aromatic amine and a coupling agent, preferably a functionalized ester. The invention also relates to the use of these tagging and dyeing molecules and mixtures which comprise them. In particular, the mixtures comprise the markers according to the invention and the markers and/or dyes classically used in the petroleum sector.
Abstract: There are provided a novel optical information recording material or medium excellent in various holographic optical information recording properties such as sensitivity, response speed, long-term storage stability, and repeatability, and a substance therefor.
Type:
Grant
Filed:
August 12, 2005
Date of Patent:
May 31, 2011
Assignee:
National Institute of Advanced Industrial Science and Technology
Inventors:
Takashi Fukuda, Jun Young Kim, Daisuke Barada, Nobuko Fukuda, Kyoko Tsuji, Hirobumi Ushijima, Kaoru Tamada
Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.
Type:
Grant
Filed:
March 13, 2008
Date of Patent:
May 31, 2011
Assignee:
NeurAxon, Inc.
Inventors:
Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
Abstract: Provided is an industrially safe and useful azodicarboxylic acid bis(2-alkoxyethyl) ester compound that is useful for the Mitsunobu reaction in which it is used in combination with a phosphorus compound to carry out a dehydration condensation reaction, and also useful as an oxidizing agent, and a starting material for various synthetic processes. Also provided are a production intermediate of the above-described compound, and methods for producing these compounds. An azodicarboxylic acid bis(2-alkoxyethyl) ester compound represented by formula (1); wherein A represents an alkyl group having 1 to 10 carbon atoms.
Abstract: Functionalized organosilicon compounds comprising at least one activated azo group of formula (I): [(G0)3SiO1/2]m [(G0)2SiO2/2]n [G0SiO3/2]o [SiO4/2]p [(G2)a(G1)a?(Z-CO—HN?NH—CO-A)SiO(3-a-a?)/2], for example a mixture of silane species of formula (ia): (C2H5O)3Si—(CH2)3—NH—CO—N?N—COOC2H3; with siloxane species of formulae: (2i.1a): [(CH3)3SiO1/2] [(C2H5O)2 {(CH2)3—NH—CO—N?N—COOC2H5} SiO2/2] and (2i.2a): [(CH3)3SiO1/2]2 [(C2H5O) {(CH2)3—NH—CO—N?N—COOC2H5} SiO2/2], are prepared from at least one hydrazino precursor (II) (—HN—NH—) of compound (I), by oxidizing the precursor (II) into an azo group for the compound (I) utilizing at least one oxidizing agent (Ox) and at least one vase (B) and also a supplementary reagent selected from among silanes of formula (III): (G DEG)4-p1Si (G2?)p1 [for example, (CH3)3(C2HSO)Si].