Benzene Ring Containing Patents (Class 568/308)
  • Publication number: 20120141394
    Abstract: Substituted benzylidene 2,4-pentanediones are found to provide stabilization to otherwise photosensitive compounds and compositions.
    Type: Application
    Filed: December 5, 2011
    Publication date: June 7, 2012
    Applicant: SYTHEON LIMITED
    Inventor: Ratan K. Chaudhuri
  • Patent number: 8119041
    Abstract: The present invention provides a two-photon light-emitting compound represented by formula (1), an optical data recording medium comprising a compound represented by formula (1), a two-photon polymerizable composition comprising a polymerizable monomer or polymerizable oligomer and at least compound represented by formula (1), and a photopolymerization process: X2—(—CR4?CR3—)m—C(?O)—(—CR1?CR2—)n—X1??(1) wherein X1 and X2 may be the same or different and each represent a substituted or unsubstituted aryl group or a substituted or unsubstituted heterocyclic group; R1, R2, R3 and R4 each independently represent a hydrogen atom or substituent; some of R1, R2, R3 and R4 may be connected to each other to form at least one ring; and n and m each independently represent an integer of from 1 to 4, with the proviso that when n and m are 2 or more, the plurality of R1's, R2's, R3's, and R4's each may be the same or different.
    Type: Grant
    Filed: September 4, 2002
    Date of Patent: February 21, 2012
    Assignee: Fujifilm Corporation
    Inventors: Masaharu Akiba, Jun Kawamata
  • Publication number: 20120029192
    Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such, the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
    Type: Application
    Filed: October 7, 2011
    Publication date: February 2, 2012
    Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
  • Publication number: 20110308555
    Abstract: The present application relates to perfume raw materials, perfume delivery systems and consumer products comprising such perfume raw materials and/or such perfume delivery systems, as well as processes for making and using such perfume raw materials, perfume delivery systems and consumer products. Such perfume raw materials and compositions, including the delivery systems, disclosed herein expand the perfume communities' options as such perfume raw materials can provide variations on character and such compositions can provide desired odor profiles.
    Type: Application
    Filed: June 22, 2011
    Publication date: December 22, 2011
    Inventors: Johan SMETS, Hugo Robert Germain Denutte, An Pintens, Koen Van Aken, Freek Annie Camiel Vrielynck
  • Patent number: 8076494
    Abstract: Disclosed is a process for the manufacture of a compound of formula (I) wherein Hal represents fluoro or chloro, and R1 and R2 represent, independently from one another, hydrogen or Hal; in which process a compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ether in a polar non-nucleophilic solvent at a temperature of ?10 to 50° C. to give the compound of formula (I).
    Type: Grant
    Filed: August 31, 2010
    Date of Patent: December 13, 2011
    Assignee: Basilea Pharmaceutica AG
    Inventors: Marc Muller, Lin Xu
  • Publication number: 20110263720
    Abstract: The present invention is directed to a method of synthesizing a compound of Formula I: the method comprising oxidizing alpha-tocopherol with a metal salt oxidizing agent to form the compound of Formula I, wherein the stoichiometric ratio (mol/mol) of metal salt oxidizing agent/alpha-tocopherol is 1.6 to 4. The invention is also directed to a method of synthesizing a compound of Formula I, the method comprising (a) hydrolyzing alpha-tocopheryl acetate in the presence of a base; (b) neutralizing the hydrolyzing of (a), thereby forming alpha-tocopherol; and (c) oxidizing the alpha-tocopherol of (b) with a metal salt oxidizing agent to form the compound of Formula I, wherein the stoichiometric ratio (mol/mol) of metal salt oxidizing agent/alpha-tocopherol is 1.6 to 4.
    Type: Application
    Filed: March 9, 2011
    Publication date: October 27, 2011
    Applicant: Penwest Pharmaceuticals Co.
    Inventors: Steven D. PAISLEY, Jason M. LePree, Amale Hawi, Michael Eckhoff
  • Publication number: 20110257047
    Abstract: Methods for labeling a substrate using a hetero-Diels-Alder reaction are disclosed. The hetero-Diels-Alder reaction includes the reaction of an o-quinone methide (e.g., an o-naphthoquinone methide) with a polarized olefin to form a hetero-Diels-Alder adduct. The o-quinone methide or the polarized olefin can be attached to a surface of a substrate, and the other of the o-quinone methide or the polarized olefin can include a detectable label. The o-quinone methide can conveniently be generated by irradiation of a precursor compound, preferably in an aqueous solution, suspension, or dispersion.
    Type: Application
    Filed: May 5, 2011
    Publication date: October 20, 2011
    Inventors: Vladimir V. Popik, Selvanathan Arumugam
  • Publication number: 20110178314
    Abstract: The present invention relates to a process for the preparation of a compound of formula wherein R1 is selected from C1-6-alkyl, C3-6-cycloalkyl and aralkyl, and wherein R2 at each occurrence independently is halogen or C1-6-alkyl, and m is an integer from 0 to 4, Q is selected from halogen, —NO2 and —NR3R4, wherein R3 and R4 are independently selected from hydrogen, C1-6-alkyl, C3-6-cycloalkyl, aryl, aralkyl, mesyl and tosyl, or wherein R3 and R4 together form a C4-6-alkylene group, Y at each occurrence is hydrogen or a hydroxy protection group W that can be hydrolytically cleaved under acidic conditions, and n is an integer from 1 to 3, and n is an integer from 1 to 3, with the proviso that n and m together are not greater than 5.
    Type: Application
    Filed: October 10, 2008
    Publication date: July 21, 2011
    Inventors: Alain Wellig, Jean-Paul Roduit, Danmei Dai, Rongmin Chen
  • Publication number: 20110136916
    Abstract: The present invention relates to the field of natural drugs, particularly to 6-shogaol for using in a method for the treatment of leukemia. The present invention provides a method for treating leukemia by applying a therapeutically effective dose of 6-shogaolt and this therapeutic method can be used for treating leukemia in mammals including human being.
    Type: Application
    Filed: November 3, 2010
    Publication date: June 9, 2011
    Applicant: China Pharmaceutical University
    Inventors: Ping Li, Yongbo Peng, Lianwen Qi, Xiaodong Wen, Jiang Ma, Ping Zhou, Lei Zhang, Qun Liu, Ehu Liu, Jun Chen
  • Patent number: 7935848
    Abstract: Cooling compounds of formula (I) wherein R1 is selected from the group consisting of hydrogen, methyl, C1-C3 alkoxy, phenyl, C1-C3 alkylphenyl, C1-C3 alkoxyphenyl, thienyl, pyridyl, furyl, and indoyl; R2 is selected from the group consisting of hydrogen and hydroxyl, or R2 forms together with the carbon atom to which it is attached a carbonyl group; and R3 is selected from the group consisting of 2,4-dimethylpent-3-yl, 2,3,4-trimethylpent-3-yl, adamantyl and 2-isopropyl-5-methyl-cyclohexyl-1-yl; and, product compositions comprising them.
    Type: Grant
    Filed: May 14, 2008
    Date of Patent: May 3, 2011
    Assignee: Givaudan S.A.
    Inventors: Stefan Michael Furrer, David Max Dastrup, Thomas Scott McCluskey
  • Publication number: 20110071178
    Abstract: Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.
    Type: Application
    Filed: April 16, 2010
    Publication date: March 24, 2011
    Applicant: Northeastern University
    Inventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
  • Publication number: 20110039874
    Abstract: Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.
    Type: Application
    Filed: April 16, 2010
    Publication date: February 17, 2011
    Applicant: Northeastern University
    Inventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
  • Patent number: 7884249
    Abstract: A method for producing highly purified fused aromatic ring compounds with high yield by a simpler method. A method for producing a fused aromatic ring compound comprising irradiating the bicyclo compound containing at least one bicyclo ring represented by formula (1) in a molecule with light to detach a leaving group X from a residual part to form an aromatic ring: wherein R1 and R3 each denotes a group to form an aromatic ring or a heteroaromatic ring which may be substituted, together with a group to which each thereof is bonded; R2 and R4 each denotes a hydrogen atom, an alkyl group, an alkoxy group, an ester group or a phenyl group; and X is a leaving group, which denotes a carbonyl group or —N?.
    Type: Grant
    Filed: September 1, 2009
    Date of Patent: February 8, 2011
    Assignee: Canon Kabushiki Kaisha
    Inventors: Hidemitsu Uno, Noboru Ono
  • Publication number: 20100331566
    Abstract: The invention provides synthetic methods that utilize bromo or chloro substituents as blocking groups during the functionalization of aromatic rings, as well as compounds that are prepared from such methods.
    Type: Application
    Filed: June 25, 2010
    Publication date: December 30, 2010
    Inventors: Leslie S. Jimenez, Ahalya Ramanathan
  • Publication number: 20100316631
    Abstract: The present disclosure describes the design and synthesis of a novel class of water soluble curcumin-based compounds. These water soluble curcumin-based compounds are shown to provide superior cell killing activity and exhibit increased and cell internalization solubility in aqueous solutions as compared to the free (unconjugated) curcumin. The present disclosure provides compositions for the treatment or prevention of a variety of disease states or conditions, such as but not limited to, cancer, other cell hyperproliferative disorders and chronic inflammatory conditions, said compositions comprising a water soluble curcumin-based compound.
    Type: Application
    Filed: October 19, 2007
    Publication date: December 16, 2010
    Applicant: THE UAB RESEARCH FOUNDATION
    Inventor: Ahmad Safavy
  • Patent number: 7838126
    Abstract: The present invention relates to the improvement of organic electronic devices, in particular fluorescent electroluminescent devices, by using electron-transport materials of the formula (I).
    Type: Grant
    Filed: February 18, 2005
    Date of Patent: November 23, 2010
    Assignee: Merck Patent GmbH
    Inventors: Anja Gerhard, Horst Vestweber, Philipp Stössel
  • Publication number: 20100286283
    Abstract: The present invention provides a novel microtubule-disrupting agent, and also provides a use of the microtubule-disrupting agent. A microtubule-disrupting agent containing an ?,?-unsaturated carbonyl compound as an active ingredient is provided. Further, a cancer cell proliferation inhibitor containing the microtubule-disrupting agent is also provided. As the ?,?-unsaturated carbonyl compound, 6-shogaol is preferably used.
    Type: Application
    Filed: May 1, 2009
    Publication date: November 11, 2010
    Inventors: Kazuhiro Ishiguro, Hidemi Goto, Takafumi Ando
  • Publication number: 20100273890
    Abstract: A bacterial autoinducer, CAI-1, was purified and its structure identified. Methods for synthesis of the autoinducer and its analogues were elucidated. Methods of using the autoinducer or its analogues for treating bacterial pathogenicity and bio film formation are described. Methods for prevention and treatment of cholera are described. Synthetic (S)-3-hydroxytridecan-4-one functions as well as natural CAI-1 in repressing production of the virulence factor toxin co-regulated pilus (TCP). Strategies are described to manipulate bacterial quorum sensing in the clinical arena.
    Type: Application
    Filed: October 1, 2008
    Publication date: October 28, 2010
    Inventors: Bonnie L. Bassler, Martin Semmelhack, Douglas A. Higgins, Megan A. Pomianek, Kristina M. Kraml, Wai-Leung Ng
  • Publication number: 20100261674
    Abstract: Fatty acid amide hydrolase (FAAH) is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors). Disclosed herein are potent inhibitors of FAAH and methods for their use for treating a variety of disorder, including hypertension and cardiac hypertrophy.
    Type: Application
    Filed: April 6, 2010
    Publication date: October 14, 2010
    Inventors: George Kunos, Alexandros Makriyannis
  • Patent number: 7795258
    Abstract: A pyridazine compound represented by formula (1): wherein R1 and R2 are same or different and represent a C1-C4 alkyl group; R3 represents a halogen atom, a nitro group, a cyano group, a C1-C4 alkyl group optionally substituted by at least one halogen atom, a C1-C4 alkoxy group optionally substituted by at least one halogen atom or a C1-C4 alkylthio group optionally substituted by at least one halogen atom; R4 and R5 each represents a halogen atom, a nitro group, a cyano group, a C1-C4 alkyl group optionally substituted by at least one halogen atom or a C1-C4 alkoxy group optionally substituted by at least one halogen atom; and m and n each represents an integer.
    Type: Grant
    Filed: June 2, 2005
    Date of Patent: September 14, 2010
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hiroshi Morishita, Akio Manabe
  • Publication number: 20100228033
    Abstract: A method of manufacturing 5-[2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl acetate, known under the INN name prasugrel of formula (I), in which the substance of formula (VI) is reacted with a cyclopropyl magnesium halide to produce the substance of formula (V), which reacted with methanesulfonyl chloride to give the methanesulfonate of formula (IV), which is further reacted with the compound of formula (III) to be converted the substance of formula (II) and the latter is converted to the substance of formula (I) with an acetylation agent.
    Type: Application
    Filed: July 8, 2008
    Publication date: September 9, 2010
    Inventors: Hana Stepankova, Josef Hajicek
  • Publication number: 20100222426
    Abstract: The invention relates to novel acylphloroglucinols which have strong growth inhibitory effects on multi-drug resistant strains of bacteria, particularly MRSA. Typically the compounds have a terpene substituent, or a terpene-derived substituent. Methods of isolating the compounds from natural sources, and synthetic methods for forming the compounds are also provided.
    Type: Application
    Filed: September 15, 2008
    Publication date: September 2, 2010
    Inventors: Simon Gibbons, John P. Malkinson, Winnie Shiu
  • Patent number: 7772285
    Abstract: A benzophenone derivative represented by the following formula: wherein R1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl; R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.
    Type: Grant
    Filed: November 13, 2002
    Date of Patent: August 10, 2010
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Hisaaki Chaki, Hironori Kotsubo, Tadashi Tanaka, Yukihiko Aikawa, Shuichi Hirono, Shunichi Shiozawa
  • Publication number: 20100197713
    Abstract: Cooling compounds of formula (I) wherein R1 is selected from the group consisting of hydrogen, methyl, C1-C3 alkoxy, phenyl, C1-C3 alkylphenyl, C1-C3 alkoxyphenyl, thienyl, pyridyl, furyl, and indoyl; R2 is selected from the group consisting of hydrogen and hydroxyl, or R2 forms together with the carbon atom to which it is attached a carbonyl group; and R3 is selected from the group consisting of 2,4-dimethylpent-3-yl, 2,3,4-trimethylpent-3-yl, adamantly and 2-isopropyl-5-methyl-cyclohe?yl-1-yI; and, product compositions comprising them.
    Type: Application
    Filed: May 14, 2008
    Publication date: August 5, 2010
    Applicant: GIVAUDAN SA
    Inventors: Stefan Michael Furrer, David Max Dastrup, Thomas Scott McCluskey
  • Publication number: 20100184986
    Abstract: Organocatalysts, particularly proline sulfonamide organocatalysts, having a first general formula as follows are disclosed. Embodiments of a method for using these organocatalysts also are disclosed. The method comprises providing a disclosed organocatalyst, and performing a reaction, often an enantioselective or diastereoselective reaction, using the organocatalyst. Solely by way of example, disclosed catalysts can be used to perform aldol reactions, conjugate additions, Michael additions, Robinson annulations, Mannich reactions, ?-aminooxylations, ?-hydroxyaminations, ?-aminations and alkylation reactions. Certain of such reactions are intramolecular cyclizations used to form cyclic compounds, such as 5- or 6-membered rings, having one or more chiral centers. Disclosed organocatalysts generally are much more soluble in typical solvents used for organic synthesis than are known compounds.
    Type: Application
    Filed: March 17, 2010
    Publication date: July 22, 2010
    Inventors: Rich Garrett Carter, Hua Yang
  • Patent number: 7749525
    Abstract: A composition-of-matter comprising a substance usable in producing packaging material and at least one compound selected from the group consisting of ar-turmerone, a sesquiterpene alcohol and a turmeric oleoresin solid residue.
    Type: Grant
    Filed: April 5, 2004
    Date of Patent: July 6, 2010
    Assignees: The State of Israel, Ministry of Agriculture & Rural Development, Agricultural Research Organization, (A.R.O.), Volcani Center, Biopack Ltd.
    Inventors: Shlomo Navarro, Simcha Finkelman, Dov Zehavi, Refael Dias, Sam Angel, Fadel Mansur, Miriam Rindner
  • Patent number: 7732643
    Abstract: The present invention relates to a transition metal complex represented by the formula (I): wherein M represents a Group 4 transition metal; —Y— represents (a): —C(R1)(R20)-A-, (b): —C(R1)(R20)-A1(R30)—, (c): —C(R1)=A1-, or (d): —C(R1)=A1-A2-R30; A represents a Group 16 element and A1 and A2 each represents a Group 15 element; R1 to R9, R20, and R30 are the same or different and each represents an optionally substituted hydrocarbon group, etc.; and X1 and X2 are the same or different and each represents a hydrogen atom, a halogen atom, an optionally substituted C1-10 alkyl group, etc., and an intermediate product thereof, and a catalyst for olefin polymerization which comprises said transition metal complex as a component.
    Type: Grant
    Filed: November 2, 2009
    Date of Patent: June 8, 2010
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hidenori Hanaoka, Eiji Yoshikawa, Yuka Imamoto
  • Publication number: 20100137178
    Abstract: The present application relates to perfume raw materials, perfume delivery systems and consumer products comprising such perfume raw materials and/or such perfume delivery systems, as well as processes for making and using such perfume raw materials, perfume delivery systems and consumer products. Such perfume raw materials and compositions, including the delivery systems, disclosed herein expand the perfume communities options as such perfume raw materials can provide variations on character and such compositions can provide desired odor profiles.
    Type: Application
    Filed: December 1, 2009
    Publication date: June 3, 2010
    Inventors: Johan Smets, Hugo Robert Germain Denutte, An Pintens, David Thomas Stanton, Koen Van Aken, Inge Helena Hubert Laureyn, Bram Denolf, Freek Annie Camiel Vrielynck
  • Publication number: 20100113807
    Abstract: A solid phase reaction system for oxidation of an organic compound, having high industrial value in which an organic solvent exerting a reverse influence on earth environments is not necessary, reuse of a catalyst is possible, and high yield can be attained, comprising a mixture of a powdery dispersion medium and a powder of a solid catalyst for the above-described oxidation reaction, and the above-described organic compound and aqueous hydrogen peroxide, wherein the above-described organic compound, the above-described solid catalyst and the above-described aqueous hydrogen peroxide are dispersed in the above-described mixture so that they get into contact mutually.
    Type: Application
    Filed: January 30, 2008
    Publication date: May 6, 2010
    Applicant: OSAKA UNIVERSITY
    Inventors: Jyunko Ichihara, Syunrou Yamaguchi
  • Publication number: 20100113460
    Abstract: Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 20, 2008
    Publication date: May 6, 2010
    Applicant: Givaudan SA
    Inventors: Boris Schilling, Wolf D. Woggon, Antoinette Chougnet, Thierry Granier, Georg Frater, Andreas Hanhart
  • Publication number: 20100111888
    Abstract: Disclosed are compounds having the ability to modulate, namely to improve, enhance and or modify fragrance compositions due to their ability to inhibit cytochrome P450 enzymes, e.g. CYP2A13 and CYP2B6.
    Type: Application
    Filed: March 20, 2008
    Publication date: May 6, 2010
    Applicant: GIVAUDAN SA
    Inventors: Boris Schilling, Thierry Granier, Georg Frater, Andreas Hanhart
  • Patent number: 7691647
    Abstract: Compositions suitable for use as signal generation components of an immunoassay, and methods for their use. According to one aspect of the invention, the composition includes a carrier having a coating of an aminodextran and a metal chelate incorporated therein. The metal chelate is present in the amount of at least 0.065 ?Mole per gram of carrier, and the aminodextran coating density averaging at least about 45 ?g per milligram of carrier. In another aspect of the invention, carrier is dyed with a complex having the formula: M(L1)x(L2)y, wherein M is a metal selected from the group consisting of europium, terbium, dysprosium, samarium, osmium and ruthenium; L1 is a ligand selected from the group consisting of DPP, TOPO, TPPO; L2 comprises a ligand having the formula wherein R is one or more substituents, each substituent comprising an electron donating group; n=2-10; x=1-2; and y=2-4.
    Type: Grant
    Filed: August 4, 2006
    Date of Patent: April 6, 2010
    Assignee: Siemens Healthcare Diagnostics Inc.
    Inventors: Alan R. Craig, Zhu Teng, Richard C. Wright, Chengrong Wang
  • Publication number: 20100068139
    Abstract: The invention relates to conjugates of formula (V) or (VI): wherein X is —CO—NH—, —NH—, —O—, —NHCONH—, or —NHCSNH—; their use as radiopharmaceuticals, processes for their preparation, and synthetic intermediates used in such processes.
    Type: Application
    Filed: March 12, 2004
    Publication date: March 18, 2010
    Inventors: Alan Cuthbertson, Magne Solbakken, Joseph Maduabuchi Arukwe, Hege Karlsen, Matthias Eberhard Glaser
  • Publication number: 20100048727
    Abstract: Novel perfluoroketone compounds of formula [I] and [Ia] are described. Also described are uses thereof, such as for inhibition of phospholipase A2 activity. Therapeutic uses thereof are also described, such as for the treatment of neural conditions and/or inflammatory conditions, such as demyelinating (e.g., multiple sclerosis) and neural injury (e.g., spinal cord injury).
    Type: Application
    Filed: April 4, 2008
    Publication date: February 25, 2010
    Inventors: Samuel David, Athena Kalyvas, Ruben Lopez-Vales, George Kokotos, Violetta Constantinou-Kokotou, Constantinos Baskakis, Christoforos G. Kokotos, Edward A. Dennis, Daren Stephens
  • Publication number: 20090318702
    Abstract: The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, the present invention provides, for example, compounds represented by the formulas (6), (7-1), (7-2) and (8): wherein R is a fluorine atom or a methoxy group, R1 is a C1-C4 alkyl group, R2 is a hydroxyl-protecting group, and X2 is a halogen atom, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.
    Type: Application
    Filed: March 6, 2007
    Publication date: December 24, 2009
    Inventors: Koji Matsuda, Koji Ando, Shigeji Ohki, Takahiro Yamasaki, Jun-ichi Hoshi
  • Publication number: 20090306016
    Abstract: Disclosed are compounds of formula R—X—Y that may be used to inhibit the action of fatty acid amide hydrolase (FAAH). Inhibition of fatty acid amide hydrolase (FAAH) will slow the normal degradation and inactivation of endogenous cannabinoid ligands by FAAH hydrolysis and allow higher levels of those endogenous cannabinergic ligands to remain present. These higher levels of endocannabinoid ligands provide increased stimulation of the cannabinoid CB1i and CB2 receptors and produce physiological effects related to the activation of the cannabinoid receptors. They will also enhance the effects of other exogenous cannabinergic ligands and allow them to produce their effects at lower concentrations as compared to systems in which fatty acid amide hydrolase (FAAH) action is hot inhibited. Thus, a compound that inhibits the inactivation of endogenous cannabinoid ligands by fatty acid amide hydrolase (FAAH) may increase the levels of endocannabinoids and, thus, enhance the activation of cannabinoid receptors.
    Type: Application
    Filed: July 27, 2007
    Publication date: December 10, 2009
    Inventors: Alexandros Makriyannis, Spyridon P. Nikas, Shakiru O. Alapafuja, Vidyanand G. Shukla
  • Publication number: 20090281094
    Abstract: The present invention concerns pyrrole compounds, derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine (BM212). The invention concerns the use of the described compounds as antitubercular agents having high activity and low toxicity and process to obtain intermediates and final compounds.
    Type: Application
    Filed: March 3, 2006
    Publication date: November 12, 2009
    Inventors: Mariangela Biava, Fabrizio Manetti, Delia Deidda, Raffaello Pompei, Maurizio Botta, Giulio Cesare Porretta
  • Publication number: 20090270513
    Abstract: The present invention refers especially to 3,5-dihydroxy-2,4-cyclohexadienones of the general formula (I) wherein R1 and R2 are independently from each other C1-6-alkyl, C2-6-alkenyl or x-oxo-Cx-alkyl with x being an integer from 1 to 6, preferably R1 and R2 are independently from each other C2-6-alkenyl or y-oxo-Cy-alkyl with y being an integer from 2 to 5, and wherein R3 and R4 are independently from each other hydroxy, C1-6-alkyl, C2-6-alkenyl or x-oxo-Cx- alkyl with x being an integer from 1 to 6, preferably R3 and R4 are independently from each other hydroxy or y-oxo-Cy-alkyl with y being an integer from 2 to 5, for use as mood balancing agents and stress relievers, as well as to dietary compositions and fortified food/feed/beverages containing such 3,5-dihydroxy-2,4-cyclohexadienones of the general formula (I), and their uses.
    Type: Application
    Filed: May 24, 2007
    Publication date: October 29, 2009
    Inventors: Regina Goralczyk, Ann Fowler, Goede Schueler, Antoine De Saizieu
  • Publication number: 20090263492
    Abstract: Disclosed are methods for identifying individuals suffering from a CNS disorder (including Alzheimer's Disease, behavioral disorders, and the like) that could be treated with a CNS drug with greater therapeutic efficacy and lower side effects and the compounds useful for such treatment. Also disclosed are methods for predicting the efficacy of a drug candidate for the treatment of a CNS disorder. The technology is also applicable to drug discovery for use in animal models of neurodegenerative diseases.
    Type: Application
    Filed: March 19, 2009
    Publication date: October 22, 2009
    Inventors: John R. Cashman, Milan Fiala
  • Patent number: 7589123
    Abstract: Compounds of general formula I: wherein: R1 and R2 are, independently of each other, selected from hydrogen, optionally substituted C1-10alkyl, optionally substituted —CO—(C1-10alkyl), optionally substituted C3-10cycloalkyl, optionally substituted —CO—(C3-10cycloalkyl), optionally substituted C2-10alkenyl, optionally substituted —CO—(C2-10alkenyl), optionally substituted aryl, and optionally substituted —CO-aryl, or R1 and R2 together represent an optionally substituted saturated or unsaturated C1-10alkylidene group, or an optionally substituted saturated or unsaturated C3-10cycloalkylidene group, or R1 and R2 together with the carbon atom to which they are attached represent an optionally substituted saturated or unsaturated organic ring containing 3, 4, 5, 6, 7 or 8 ring carbon atoms and optionally 1, 2 or 3 ring heteroatoms selected from O, N and S; R3, which may be the same as, or different from, either of R1 and R2, is selected from optionally substituted C1-10alkyl, optionally substituted C3-10cycl
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: September 15, 2009
    Assignee: Phytopharm PLC
    Inventors: Daryl David Rees, Phillip James Gunning, Antonia Orsi, Patrick A. Howson, Paul Barraclough, Noelle Callizot
  • Publication number: 20090221702
    Abstract: The present invention provides the use of a compound of the Formula: (I) wherein R1 is C1-5 alkoxy, OCOC1-3Alkyl, O(CH2)2O(CH2)2O(CH2)2OMe, O(CH2)2O(CH2)2O(CH2)2OH or OH; R2 is H, (CH2)nOH, OCH3, Hal or (II) or (III) R3 is H or (CH2)nOH; and R4 is C1-6 alkyl, optionally substituted by one or more of Hal, OH, COCH3, NH2, NHCH3, NHMe, NMe2, OCOCH3, CO2H or esters or amides thereof where n is 1-5; and pharmaceutically acceptable salts thereof, in the manufacture of a medicament for use in modulating PKB activity.
    Type: Application
    Filed: March 17, 2006
    Publication date: September 3, 2009
    Inventors: Rudiger Woscholski, Helen Hailes, Macba Numbere, Erika Rosivatz
  • Patent number: 7582801
    Abstract: The present invention is directed to labeled compounds, of the formulae wherein C* is each independently selected from the group consisting of 13C and 12C with the proviso that at least one C* is 13C, each hydrogen of the methylene group can independently be either hydrogen or deuterium, the methyl group includes either zero or three deuterium atoms, Q is from the group of sulfide, sulfinyl, and sulfone, Z is an aryl group from the group of 1-naphthyl, substituted 1-naphthyl, 2-naphthyl, substituted 2-naphthyl, and phenyl groups with the structure wherein R1, R2, R3, R4 and R5 are each independently from the group of hydrogen, a C1-C4 lower alkyl, a halogen, and an amino group from the group of NH2, NHR and NRR? where R and R? are each independently from the group of a C1-C4 lower alkyl, a phenyl, and an alkoxy group, and the methyl group can include either zero or three deuterium atoms.
    Type: Grant
    Filed: February 7, 2005
    Date of Patent: September 1, 2009
    Assignee: Los Alamos National Security, LLC
    Inventors: Rodolfo A. Martinez, Clifford J. Unkefer, Marc A. Alvarez
  • Publication number: 20090209651
    Abstract: A cosmetic or dermatological preparation which is suitable for application to skin and comprises 3-(4-hydroxy-3-methoxyphenyl)-1-(4-hydroxyphenyl)-propane-1-one in a concentration which is effective for at least one of increasing skin moisture content, moisturizing skin, improving the surface structure of the skin, reducing cellulite, increasing the resilience and elasticity of skin, strengthening the connective tissue of skin, and reducing stretch marks on skin. This Abstract is not intended to define the invention disclosed in the specification, nor intended to limit the scope of the invention in any way.
    Type: Application
    Filed: January 15, 2009
    Publication date: August 20, 2009
    Applicant: Beiersdorf AG,
    Inventors: Ralf SIEGNER, Ursula Holtzmann, Julia Eckert, Stefan Heuser, Marc Winnefeld
  • Publication number: 20090186790
    Abstract: The present invention relates to photo-labile pro-fragrance conjugates comprising: a) a photo-labile unit which upon exposure to electromagnetic radiation is capable of releasing a pro-fragrance unit; and b) a pro-fragrance unit, which when so released is either i) a pro-fragrance compound capable of releasing a fragrance raw material; or ii) a fragrance raw material. The present invention relates to systems for delivering fragrances to a situs, and to laundry detergent compositions, fine fragrances, personal care and hair care compositions comprising said systems.
    Type: Application
    Filed: March 26, 2009
    Publication date: July 23, 2009
    Inventors: Robert Richard Dykstra, Gregory Scot Miracle, Lon Montgomery Gray
  • Patent number: 7547697
    Abstract: Compounds of formula (I): as well as pharmaceutically acceptable salts and esters thereof for use as pharmaceutical compositions.
    Type: Grant
    Filed: July 2, 2007
    Date of Patent: June 16, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Werner Neidhart, Alexander V. Mayweg
  • Patent number: 7534880
    Abstract: The present invention relates to clear photopolymerisable systems for the preparation of high thickness coatings, to a procedure for their application and to the solid surfaces coated with them.
    Type: Grant
    Filed: August 3, 2004
    Date of Patent: May 19, 2009
    Assignee: Lamberti SpA
    Inventors: Gabriele Norcini, Stefano Romagnano, Marco Visconti, Giuseppe Li Bassi
  • Publication number: 20090111975
    Abstract: The present invention relates to methods of preparing anthocyanins, and methods of preparing precursors of anthocyanins. The methods utilise a coupling reaction between a sugar and a suitable electrophilic precursor to form Eastern half intermediates that are then reacted with Western half intermediates to form the target anthocyanins. Some Eastern half intermediates and electrophilic precursors also form part of the invention.
    Type: Application
    Filed: June 15, 2006
    Publication date: April 30, 2009
    Applicant: BIOSYNTH AS
    Inventor: Einar Bakstad
  • Patent number: 7501544
    Abstract: The present invention relates to a process for the preparation of compounds of formula (I), wherein the substituents are as defined in claim 1, by reacting a compound of formula (II), either with a chlorination or bromination agent or with a compound of formula (III) CI—SO2R9, R9 being C1-C4alkyl, C1-C4haloalkyl, phenyl or C1-C4alkyl-substituted phenyl, to form the compound of formula (IV), reacting the compound of formula (IV) with a compound of formula (V) M+-O?—C(O)—Y wherein Y is as defined above and M+ is the hydrogen cation or an alkali metal ion, alkaline earth metal ion or ammonium ion, to form the compound of formula (VI) and treating that compound with a cyanide source in the presence of a base.
    Type: Grant
    Filed: April 29, 2005
    Date of Patent: March 10, 2009
    Assignees: Syngenta Crop Protection, Inc., Syngenta Limited
    Inventors: David Anthony Jackson, Andrew Edmunds, Martin Charles Bowden, Ben Brockbank
  • Publication number: 20080300304
    Abstract: The present invention relates to a process for preparing a ginger fraction, the fraction prepared by this process and the use thereof on its own or combined with drugs for inhibiting human cytochrome P450 (CYP) enzymes (particularly cytochrome P450 3A4, CYP3A4) for positively influencing the oral bioavailability and pharmacokinetics of active substances.
    Type: Application
    Filed: December 20, 2006
    Publication date: December 4, 2008
    Inventors: Thomas Ebner, Eva Christine Ludwig-Schwellinger, Stefan Blech, Rolf-Stefan Brickl
  • Publication number: 20080246002
    Abstract: Compounds that are useful in compositions for flat panel displays, for example, are provided. The compounds provided are polar, and are useful in low threshold voltage mixtures. The compounds provided have the general structure: CpCOCH2[A]nZ1[B]mZ2PhX1X2Y, where CpCOCH2 is the structure: A and B are independently in each instance selected from the group consisting of 1,4-cyclohexane, 1,4-phenyl, 1,3-dioxan-5,2-diyl; pyridine-5,2-diyl; and pyrimidin-5,2-diyl; n and m are independently in each instance 0, 1 or 2; Z1 and Z2 are independently a single bond, —(CH2)2—, CF2O, OCF2, CH2O, OCH2, —C?C—, COO, OOC; and Y is selected from the group consisting of: F, Cl, CN, OCH2F, CHF2, OCF3, and CF3.
    Type: Application
    Filed: April 3, 2007
    Publication date: October 9, 2008
    Inventor: Xinhua Chen