Polyoxy Patents (Class 568/660)
  • Patent number: 7550619
    Abstract: Intermediates useful in the preparation of the antiviral agent entecavir are disclosed. A resin adsorption process for the isolation and purification of entecavir is also disclosed. Various processes useful in the preparation of entecavir are also disclosed.
    Type: Grant
    Filed: December 19, 2005
    Date of Patent: June 23, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yadagiri R. Pendri, Chung-Pin H. Chen, Jing Liang, Shaopeng Wang, Milan Stojanovic, Richard P. Polniaszek, John Thottathil, Dhileepkumar Krishnamurty
  • Publication number: 20090048280
    Abstract: Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds (e.g.
    Type: Application
    Filed: December 28, 2006
    Publication date: February 19, 2009
  • Patent number: 7462683
    Abstract: It is an object of the invention to provide a novel ?-conjugated polymer compound capable of expecting an application as a functional material having a solubility, a heat resistance, an electrochemical activity and a fluorescence, and a method for producing the same. A dihalide is represented by the following formula: (wherein R1 represents a halogen, R2 represents an alkyl group or a silyl group having a substituent, and R3 represents a hydrogen or an alkyl group).
    Type: Grant
    Filed: February 15, 2005
    Date of Patent: December 9, 2008
    Assignee: Tokyo Institute of Technology
    Inventors: Takakazu Yamamoto, Hiroki Fukumoto, Takahiro Asao
  • Publication number: 20080293824
    Abstract: The invention relates to the use of phenylether derivatives of formula (I), to compositions thereof for the control of pests, including arthropods and helminths.
    Type: Application
    Filed: April 3, 2008
    Publication date: November 27, 2008
    Inventors: Stefan Schnatterer, Michael Maier, Friederike Lochhaas, Werner Knauf, Karl Seeger
  • Patent number: 7422702
    Abstract: The present invention provides, in a method for transporting charge using the molecular orientation in a liquid-crystalline state, a novel benzene derivative having a long, linear conjugated structure expected to have satisfactory charge-transport properties without photoexcitation, a process for producing the benzene derivative, and a liquid-crystal material including the benzene derivative.
    Type: Grant
    Filed: March 22, 2004
    Date of Patent: September 9, 2008
    Assignee: Nippon Chemical Industrial Co., Ltd.
    Inventor: Yuichiro Haramoto
  • Patent number: 7420074
    Abstract: A process to prepare substituted aryl pnictogen derivatives comprising contacting a fluoropolyether or fluoroalkyl primary bromide or iodide, with a pnictogen derivative such as triaryl phosphine, triaryl arsine, or triaryl stibine or triaryl phosphine oxide, triaryl arsine oxide or triaryl stibine oxide, to produce the corresponding fluoropolyether- or fluoroalkyl- substituted aryl phosphine oxide, aryl arsine oxide or aryl stibine oxide; and optionally, contacting the oxide product with a reducing agent to form the corresponding substituted aryl phosphine, arsine or stibine.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: September 2, 2008
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: Jon L. Howell, Kevin Anthony Hay
  • Patent number: 7396948
    Abstract: A process to prepare substituted aryl pnictogen derivatives comprising contacting a fluoropolyether or fluoroalkyl primary bromide or iodide, with a pnictogen derivative such as triaryl phosphine, triaryl arsine, or triaryl stibine or triaryl phosphine oxide, triaryl arsine oxide or triaryl stibine oxide, to produce the corresponding fluoropolyether- or fluoroalkyl-substituted aryl phosphine oxide, aryl arsine oxide or aryl stibine oxide; and optionally, contacting the oxide product with a reducing agent to form the corresponding substituted aryl phosphine, arsine or stibine.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: July 8, 2008
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: Jon L. Howell, Kevin Anthony Hay
  • Publication number: 20070299243
    Abstract: A method of purifying a polymerization reaction mixture containing a poly(arylene ether) is described. The method uses multiple separations of organic and aqueous phases to achieve rapid and efficient removal of polymerization catalyst metal from the poly(arylene ether). When combined with particular precipitation conditions, the method produces a poly(arylene ether) having an improved combination of particle size distribution and low catalyst metal concentration.
    Type: Application
    Filed: June 22, 2006
    Publication date: December 27, 2007
    Inventors: Erik R. Delsman, Gert-Jan Schoenmakers, Paul Tock
  • Patent number: 7034152
    Abstract: Processes are disclosed for preparing the antiviral agent entecavir. A resin adsorption process for the isolation and purification of entecavir is also disclosed. Various intermediates useful in the preparation of entecavir are also disclosed.
    Type: Grant
    Filed: December 11, 2003
    Date of Patent: April 25, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yadagiri R. Pendri, Chung-Pin H. Chen, Sunil S. Patel, Jeffrey M. Evans, Jing Liang, David R. Kronenthal, Gerald L. Powers, Siva Josyula Prasad, Jeffrey T. Bien, Zhongping Shi, Ramesh N. Patel, Amit Banerjee, Yeung Yu Chan, Sushil K. Rijhwani, Ambarish K. Singh, Shaopeng Wang, Milan Stojanovic, David J. Kucera, Richard P. Polniaszek, Charles Lewis, John Thottathil, Dhileepkumar Krishnamurty, Maotang X. Zhou, Purushotham Vemishetti
  • Patent number: 6943271
    Abstract: A fluorine-containing styrene monomer of the formula (2) is produced by a first, second or third process. The first process includes (a) reacting a compound of the formula (1) with a compound of the formula (3), in the presence of a metal catalyst; (b) reacting the product of the step (a) with a base; and (c) reacting the product of the step (b) with hydrogen, in the presence of a metal catalyst and a phosphine or amine, thereby producing the target styrene monomer. The second process includes reacting a compound of the formula (1) with a compound of the formula (12), in the presence of a metal catalyst, thereby producing the target styrene monomer. The third process includes reacting a compound of the formula (13) with a compound of the formula (14) or (15), in the presence of a base, thereby producing the target styrene monomer.
    Type: Grant
    Filed: June 23, 2003
    Date of Patent: September 13, 2005
    Assignee: Central Glass Company, Limited
    Inventors: Shinichi Sumida, Takashi Kume, Sunao Koga, Haruhiko Komoriya
  • Patent number: 6939845
    Abstract: The present invention provides a fragrance precursor of formula I: that is capable of forming a fragrant ketone of formula II: and a fragrant lactone of formula III:
    Type: Grant
    Filed: June 18, 2001
    Date of Patent: September 6, 2005
    Assignee: Givaudan SA
    Inventors: Markus Gautschi, Caroline Plessis, Samuel Derrer
  • Patent number: 6844461
    Abstract: The present invention provides a method for the synthesis of an A-ring synthon phosphine oxide used in the preparation of 19-nor vitamin D compounds, and to novel synthetic intermediates formed during the synthesis. The new method prepares the phosphine oxide from (D)-glucose.
    Type: Grant
    Filed: November 26, 2003
    Date of Patent: January 18, 2005
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Masato Shimizu, Sachiko Yamada
  • Publication number: 20040259958
    Abstract: Antimicrobial compounds, compositions containing the same, and methods of using of the same for reducing the presence of microorganisms on a substrate or in a fluid environment comprising an antimicrobial effective carrier and at least one antimicrobial compounds including non-halogenated phenoxy and/or benzyloxy substituted phenol compounds.
    Type: Application
    Filed: June 14, 2004
    Publication date: December 23, 2004
    Inventors: David Scott Harper, robert A. Coburn, Constantine Georgiades, Andre Soshinsky, Marianne D. Huntley
  • Publication number: 20040235963
    Abstract: The present invention is directed to 4-cyclopentyl resorcinol monohydrate, its Form I polymorph, formulations containing at least one of these compounds, and their use to lighten skin.
    Type: Application
    Filed: May 19, 2004
    Publication date: November 25, 2004
    Inventor: William Thomas Gattrell
  • Publication number: 20040210076
    Abstract: The present invention relates to process wherein (+)-2-carene epoxide is coupled with a compound X-Y that contains nucleophilic and electrophilic moieties, to produce a compound of formula (5). The reaction mixture consists essentially of a source of (+)-2-carene epoxide, compound X-Y, optionally an inert solvent and optionally a pH buffer. No acid catalyst is used in the process.
    Type: Application
    Filed: June 7, 2004
    Publication date: October 21, 2004
    Inventors: Michael Casner, Theodore Maurice Resnick, Lee Jonathan Silverberg
  • Publication number: 20040158074
    Abstract: A class of substituted biphenyl compounds is described for use in treating inflammation and inflammation-related disorders.
    Type: Application
    Filed: January 13, 2004
    Publication date: August 12, 2004
    Applicant: G.D. Searle & Co.
    Inventors: David B. Reitz, James J. Li, Monica B. Norton
  • Publication number: 20040147788
    Abstract: The invention relate to stilbene derivatives having formula I 1
    Type: Application
    Filed: November 4, 2003
    Publication date: July 29, 2004
    Inventors: Jean-Francois Savouret, Marc Poirot, Philippe De Medina, Robert F. Casper
  • Publication number: 20040143023
    Abstract: The present invention relates materials and methods for synthesizing stilbenes, and in particular to processes for the synthesis of substituted stilbenes such as combretastatin A4. The present invention relates in particular to methods which are stereoselective for either the cis or the trans isomer of the substituted stilbene, using a Perkin-type condensation of an arylacetic acid and a substituted benzaldehyde, followed by a decarboxylation reaction to produce the substituted cis-stilbenes or a Suzuki-type reaction involving a Z or E-ethenyl halide and a substituted boronic acid in the presence of a palladium catalyst to produce specifically either the Z or E-isomer of substituted stilbenes.
    Type: Application
    Filed: March 3, 2004
    Publication date: July 22, 2004
    Inventors: John Anthony Hadfield, Alan Thomson McGown, Keira Gaukroger, Lucy Annette Hepworth, Nicolas James Lawrence
  • Publication number: 20040127749
    Abstract: A compound having the general formula I wherein R comprises a hydrocarbon group including H, branched or linear alkyl chains, substituted alkyl, alkenyl, aryl, alkaryl or cylcic groups; R1 is any of C, N, P, B, S, or SiO4 or any subgroups thereof; R2 is any of a covalent bond, O, CH2, (CH2)n where n may be 1-10 carbons long; R3 is any of a covalent bond, O, CH2, (CH2)n where n may be 1-10 carbons long; R2 and R3 may be the same or different; R4 is any of O, H, OH, CH3, (CH2)nCH3, (CH2)nOH, (CH2)nOX or any combinations thereof where n is from 1 to 10. OX is a water soluble group; chains a and b are in the range 1-10 carbons each; and the alkoxy chains c and d are in the range 1-20 units each.
    Type: Application
    Filed: December 10, 2003
    Publication date: July 1, 2004
    Inventors: John Harrison, Mark Zwinderman
  • Patent number: 6753444
    Abstract: The invention relates to a process for preparing 2,3,5,6-tetrahaloxylylidene compounds of formula (I) where each Hal is independently fluorine or chlorine, and X is fluorine, chlorine, bromine, —O—R, or —O—C(═O)R, where R is hydrogen, a straight-chain or branched C1-C12-alkyl- or a C6-C14-aryl radical, by reacting 2,3,5,6-tetrahaloxylylidenediamines of formula (II) with an alkyl nitrite and/or nitrous acid in HX as a solvent.
    Type: Grant
    Filed: July 24, 2002
    Date of Patent: June 22, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhard Langer, Lars Rodefeld
  • Publication number: 20040116538
    Abstract: This invention relates to a new method for the preparation of a selective estrogen receptor modulator and its isomers. The invention concerns also new intermediates prepared and further used in said method.
    Type: Application
    Filed: October 10, 2003
    Publication date: June 17, 2004
    Inventors: Arja Kalapudas, Marja Sodervall
  • Publication number: 20040049085
    Abstract: The present invention relates to a novel neolignan (NEOLASA-I) 3-ethyl-2-methyl-3-(2″, 4″, 5″-trimethoxy-phenyl-1-(2′,4′,5′-trimethoxy) phenyl-1-(2′,4′,5′-trimethoxy)phenyl-1-propene and a process for the preparation of high purity, higher yield neolignan, &agr;-asarone, 2,4,5-trimethoxy-phenyl propionone from &bgr;-asarone or &bgr;-asarone rich Acorus calamus oil containing &agr; and &ggr;-asarone by hydrogenating and dimerizing by treatment with DDQ in presence of an organic acid.
    Type: Application
    Filed: September 12, 2003
    Publication date: March 11, 2004
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Arun Kumar Sinha, Bhupendra Prasad Joshi, Ruchi Acharya
  • Publication number: 20040043916
    Abstract: The use of various novel oxime ethers are described as fragrance chemicals. These chemicals are suitable for use in creating fragrance, and scents in items such as perfumes, colognes and personal care products is disclosed.
    Type: Application
    Filed: August 29, 2002
    Publication date: March 4, 2004
    Inventors: Anubhav P.S. Narula, Rajamony Mahesh, Manfred Pawlak, Patrick M. Merritt, Clint Dee Winton Brooks
  • Publication number: 20040043917
    Abstract: The use of various oxime ethers are described as fragrance chemicals, suitable for use in creating fragrance, and scents in items such as perfumes, colognes and personal care products is disclosed. Novel compounds are also disclosed.
    Type: Application
    Filed: August 29, 2002
    Publication date: March 4, 2004
    Inventors: Anubhav P.S. Narula, Rajamony Mahesh, Manfred Pawlak, Clint Dee Winton Brooks
  • Patent number: 6683219
    Abstract: The present invention provides a method for the synthesis of an A-ring synthon phosphine oxide used in the preparation of 19-nor vitamin D compounds, and to novel synthetic intermediates formed during the synthesis. The new method prepares the phosphine oxide from (D)-glucose.
    Type: Grant
    Filed: July 25, 2002
    Date of Patent: January 27, 2004
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Masato Shimizu, Sachiko Yamada
  • Publication number: 20030229256
    Abstract: A process for producing 2,2′,3,3′,5,5′-hexamethyl-[1,1′-biphenyl]-4,4′-diol, which process comprises,
    Type: Application
    Filed: October 16, 2002
    Publication date: December 11, 2003
    Inventors: Kenji Ishii, Kiyonari Hiramatsu, Makoto Miyamoto, Yasumasa Norisue, Katsuhiko Yanagida
  • Publication number: 20030229149
    Abstract: Disclosed is the use of hydroxydiphenylether compounds of formula 1
    Type: Application
    Filed: May 23, 2003
    Publication date: December 11, 2003
    Inventors: Werner Baschong, Helmut Luther, Dietmar Ochs, Sebastien Mongiat
  • Publication number: 20030207938
    Abstract: Benzhydryl derivatives of the formula I, 1
    Type: Application
    Filed: October 29, 2002
    Publication date: November 6, 2003
    Inventors: Ingo Rose, Jordi Tormo i Blasco, Markus Gewehr, Wassilios Grammenos, Bernd Muller, Joachim Rheinheimer, Peter Schafer, Frank Schieweck, Thomas Grote, Andreas Gypser, Eberhard Ammermann, Gisela Lorenz, Reinhard Stierl, Siegfried Strathmann, Paul Carter, Jurgen Curtze
  • Publication number: 20030207945
    Abstract: A antimicrobial compound, compositions containing the same, and method of using the same for reducing the presence of microorganism on a substrate or in a fluid environment comprising an antimicrobial effective carrier and at least one antimicrobial compounds including non-halogenated phenyl substituted phenol compounds.
    Type: Application
    Filed: April 28, 2003
    Publication date: November 6, 2003
    Inventors: David Scott Harper, Robert A. Coburn, Constantine Georgiades, Andre Soshinsky, Marianne D. Huntley
  • Publication number: 20030186939
    Abstract: A &ohgr;-cycloalkyl-prostaglandin E2 derivatives of the formula (I) 1
    Type: Application
    Filed: September 11, 2002
    Publication date: October 2, 2003
    Inventors: Kousuke Tani, Shuichi Ohuchida
  • Publication number: 20030187306
    Abstract: The present invention relates to a novel neolignan (NEOLASA-I) 3-ethyl-2-methyl-3-(2″,4″,5″-trimethoxy-phenyl-1-(2′,4′,5′-trimethoxy)phenyl-1-(2′,4′,5′-trimethoxy)phenyl-1-propene and a process for the preparation of high purity, higher yield neolignan, &agr;-asarone, 2,4,5-trimethoxy-phenyl propionone from &bgr;-asarone or &bgr;-asarone rich Acorus calamus oil containing &agr; and &ggr;-asarone by hydrogenating and dimerizing by treatment with DDQ in presence of an organic acid.
    Type: Application
    Filed: March 28, 2002
    Publication date: October 2, 2003
    Applicant: Council of Scientific & Industrial Research
    Inventors: Arun Kumar Sinha, Bhupendra Prasad Joshi, Ruchi Acharya
  • Patent number: 6620977
    Abstract: A process for preparing a butanetriol derivative of the formula (1) useful as intermediates of medicines wherein R1 is the same defined below, which comprises reacting a compound of the formula (3) wherein R1 and R2 are the different protecting groups, and an ethylene glycol derivative in a basic condition to prepare a compound of the formula (4) or (4a) wherein R1 and R2 are the same defined above, and then subjecting the compound (4) or (4a) to selective deprotection reaction.
    Type: Grant
    Filed: June 9, 2000
    Date of Patent: September 16, 2003
    Assignee: Daiso Co., Ltd.
    Inventors: Makoto Hirata, Masafumi Mikami, Yoshiro Furukawa
  • Patent number: 6617475
    Abstract: Optically active &agr;-hydroxyethers are prepared from prochiral &agr;-ketoethers by heterogeneous hydrogenation using platinum catalysts in the presence of a chiral nitrogen base in high chemical and optical yields, since this type of hydrogenation selectively hydrogenates only one diastereomer virtually to completion. The yields may be substantially increased by adding a solid, strong base which has a racemizing effect on the non-hydrogenatable diasteromer.
    Type: Grant
    Filed: September 4, 2002
    Date of Patent: September 9, 2003
    Assignee: Solvias AG
    Inventors: Martin Studer, Stephan Burkhardt
  • Publication number: 20030163005
    Abstract: There is described a process for the preparation of halogenated hydroxydiphenyl compounds of formula (1) by acylation of a halogenated benzene compound (first stage), etherification of the acylated compound with a halogenated phenol compound, which is not further substituted in the ortho-position (second stage), oxidation of the etherified compound (third stage) and hydrolysis of the oxidized compound in a fourth stage, wherein the reaction of the second stage is carried out in the presence of K2CO3 and any desired copper catalyst, where K2CO3 is used in a concentration of from 0.5 to 30 mol, based on the phenol compound employed of formula (6), according to the reaction scheme (I) in which R1 and R2 independently of one another are F, Cl or Br; R3 and R4 independently of one another are hydrogen; or C1-C4alkyl; m is 1 to 3; and n is 1 or 2. The compounds of formula (1) are used for protecting organic materials and articles from microorganisms.
    Type: Application
    Filed: October 31, 2002
    Publication date: August 28, 2003
    Inventors: Armando Di Teodoro, Werner Holzl, Dieter Reinehr, Rudolf Zink
  • Publication number: 20030105078
    Abstract: The invention relates to novel diphenyl derivatives, to processes for their preparation and to their use in medicaments.
    Type: Application
    Filed: February 26, 2002
    Publication date: June 5, 2003
    Inventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Christiane Faeste, Hilmar Bischoff, Axel Kretschmer, Verena Vohringer, Peter Ellinghaus
  • Publication number: 20030078447
    Abstract: Disclosed is a tetracyclic compound of the formula I 1
    Type: Application
    Filed: August 13, 2001
    Publication date: April 24, 2003
    Applicant: MERCK PATENTGESELLSCHAFT
    Inventors: Peer Kirsch, Joachim Krause, Georg Lussem, Dagmar Klement
  • Patent number: 6552088
    Abstract: Biphenyl substituted amides with activity as antagonists of the neurokinin 1 (NK-1, substance P) receptor.
    Type: Grant
    Filed: June 21, 2001
    Date of Patent: April 22, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Bös, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
  • Patent number: 6552213
    Abstract: The present invention relates to a new stereoselective method for the preparation of tris-O-substituted-(E)-1-(3,5-dihydroxyphenyl)-2-(4-hydroxyphenyl)ethene derivative of the formula (I) which is a key intermediate in the synthesis of trans-resveratrol (I, R2=R2=R3=H). The invention also provides a method for the exclusive synthesis of trans-isomer of compounds of formula (I) without any contamination of cis-isomer.
    Type: Grant
    Filed: May 24, 2002
    Date of Patent: April 22, 2003
    Assignee: Orchid Chemicals & Pharmaceuticals Limited, India
    Inventors: Pandurang Balwant Deshpande, Udayampalayam Palanisamy Senthilkumar, Gnanaprakasam Andrew
  • Publication number: 20030073872
    Abstract: A composition comprising a guest/host assembly having a spheroidal host assembly comprised of a hexamer of a methylene-bridged trihydroxybenzene tetramer and a guest component encapsulated within the spheroidal host assembly to provide a highly stable guest/host assembly. A guest component, specifically a pharmaceutically active agent, is encapsulated within the spheroidal host assembly to provide a guest/host assembly exhibiting a high stability, being stable upon a solubilization in a mixture of acetone and water in a one-to-one ratio for a period of one day at a temperature of 37° C. The pharmaceutically active agent encapsulated within the spheroidal hexamer is selected from the group consisting of Depakote, Wellbutrin, Allegra, Neurontin, Zovirax, and Claritin. A process for the preparation of a hexameric complex, as described above, from a methylene-bridged tetramer solubilized in an amphiphilic organic solvent. An activator is incorporated into the amphiphilic solvent containing the tetramer.
    Type: Application
    Filed: October 16, 2001
    Publication date: April 17, 2003
    Inventor: Jerry L. Atwood
  • Publication number: 20030045757
    Abstract: Disclosed is a modified polyphenylene ether having a number average molecular weight of not smaller than 4,000, which is obtained by reacting a precursory modified polyphenylene ether with a phenolic compound in the presence of a radical generator, wherein the precursory modified polyphenylene ether comprises a plurality of polyphenylene ether chains each having a terminal phenolic hydroxyl group, wherein the plurality of polyphenylene ether chains collectively have at least one terminal phenolic hydroxyl group modified and wherein not all of the terminal phenolic hydroxyl groups of the plurality of polyphenylene ether chains are modified. Also disclosed is a method for producing the modified polyphenylene ether.
    Type: Application
    Filed: July 31, 2002
    Publication date: March 6, 2003
    Inventors: Yoshiyuki Ishii, Kumi Sorita
  • Patent number: 6518314
    Abstract: Compositions comprising a pharmaceutically effective amount of a compound that impedes disruption of intact dense microspheres (DMS) by acting on DMS either to prevent disruption, or if disrupted, act on pre-disrupted DMS in such a way that, when the composition is administered to a test animal that has received an injection of DMS, it reduces the mean volume of tissue occupied by disrupted DMS, reduces the ratio of the number of inflammatory cells per DMS, or increases the ratio of the number of macrophages containing disrupted DMS per DMS, are useful for treating cerebral amyloidosis.
    Type: Grant
    Filed: October 6, 2000
    Date of Patent: February 11, 2003
    Assignee: Nymox Corporation
    Inventors: Paul Averback, Hossein Ghanbari, Iraj Beheshti, David Morse
  • Patent number: 6515163
    Abstract: The invention concerns hydrogenated phenanthrenes of formula I wherein the parameters have the meanings given in the text and their use in liquid crystal compositions.
    Type: Grant
    Filed: June 8, 2001
    Date of Patent: February 4, 2003
    Assignee: Merck Patent Gesellschaft
    Inventors: Rainer Wingen, Barbara Hornung, Wolfgang Schmidt
  • Publication number: 20030009060
    Abstract: This invention relates to 1,2-di(4-hydroxyaryl)tetrafluoroethanes of the general formula (I) 1
    Type: Application
    Filed: May 29, 2002
    Publication date: January 9, 2003
    Inventors: Albrecht Marhold, Kathe Baumann
  • Patent number: 6461876
    Abstract: The present invention provides novel 1,2-dioxetanes derived from spiro-fused ketones with or without &pgr;-electrons in the ring or with carbon-carbon double bond(s) in the spiro-fused ring. Additionally, these new dioxetanes have electron donating or withdrawing groups at the four-membered peroxide ring to render these dioxetanes active at all sites.
    Type: Grant
    Filed: August 21, 2000
    Date of Patent: October 8, 2002
    Inventor: Brij P. Giri
  • Patent number: 6423753
    Abstract: Colchinol derivatives of formula wherein R1, R2, R3 and R6 are each independently H, optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, alkanoyl, PO3H2; X is carbonyl (CO), thiocarbonyl (CS), methylene (CH2) or a group CHR4; R4 is OH, O-alkyl or NR8R9; R5 and R7 are each independently H, alkyl, halogen, hydroxy, alkoxy, nitro or amino; R8 is H, optionally substituted alkyl, cycloalkyl, alkanoyl, thioalkanoyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, arylaminocarbonyl, alkylsulphonyl, arylsulphonyl, aminosulphonyl, alkylaminosulphonyl, dialkylaminosulphonyl or arylaminosulphonyl; and R9 is H, alkyl or cycloalkyl; and the pharmaceutically acceptable salts, solvates, and hydrates thereof have been found to be useful for treatment of diseases involving angiogenesis. Some of these compounds are novel. Particularly preferred are those compounds in which R6 is PO3H2.
    Type: Grant
    Filed: January 5, 2000
    Date of Patent: July 23, 2002
    Assignee: Angiogene Pharmaceuticals Ltd.
    Inventor: Graeme Dougherty
  • Patent number: 6410802
    Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: June 25, 2002
    Assignee: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • Publication number: 20020062049
    Abstract: A two-step process for the preparation of fluoroolefin compounds of formula I 1
    Type: Application
    Filed: September 12, 2001
    Publication date: May 23, 2002
    Applicant: BASF Aktiengesellschaft
    Inventor: William Wakefield Wood
  • Patent number: 6391916
    Abstract: Novel C3-substituted cyclodeca-1,5-diynes can be prepared through novel synthetic procedures using starting (E)-C3-substituted-4-(aryl- or heteroarylmethylidene)cyclodeca-1,5-diynes reagents. Both the C3-substituted cyclodeca-1,5-diyn-3-enes and the starting reagents have improved thermal stability compared to unsubstituted counterparts.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: May 21, 2002
    Assignee: The Hong Kong University of Science and Technology
    Inventors: Wei-Min Dai, Anxin Wu, Yuk Ha Lee, Wataru Hamaguchi, Sei-ichi Nishimoto, Ling Zhou, Atsushi Ishii
  • Publication number: 20020037918
    Abstract: The present invention provides an efficient synthetic strategy for the preparation of analogs that incorporate important structural elements of the marine natural product curacin A, the compositions and various uses of the compositions. The most active of these compounds at nanomolar concentrations inhibit tubulin polymerization, show growth inhibition activity, inhibited colchicines binding to tubulin and block mitotic progression. The compounds of the present invention represent some of the most potent synthetic curacin A analogs synthesized, with an activity profile rivaling that of the natural product despite the simplified structure, greater water solubility, and increased chemical stability.
    Type: Application
    Filed: July 19, 2001
    Publication date: March 28, 2002
    Inventors: Peter Wipf, Jonathan T. Reeves, Billy W. Day, Raghavan Balachandran
  • Patent number: 6320085
    Abstract: The subject matter of the invention is the process for the preparation of mixed ethers of formula I, wherein Ar represents an aromatic or one or more heteroatom-containing moiety, optionally substituted by one or more C1-4 alkoxy, methylenedioxy, C1-4 alkyl, halogen, C1-4 haloalkyl or nitro-group, and/or condensed with a benzene ring; R1 and R2 independently mean hydrogen, C1-4 alkyl, C1-4 haloalkyl, C2-4 alkenyl, phenyl, substituted phenyl, C3-6 cycloalkyl group, R3 means C3-6 alkynyl, optionally substituted by one or more C1-6 alkyl, C3-6 alkenyl, C3-6 alkynyl, C1-6 haloalkyl group, or halogen atom, R3 also means a C1-4 alkyloxy-C1-4 alkyloxy-C1-4 alkyl group.
    Type: Grant
    Filed: July 13, 1999
    Date of Patent: November 20, 2001
    Assignee: Agro-Chemie Novenyvedoszer Gyarto Ertekesito est Forgalmazo Kft.
    Inventors: Geza Arvai, Bela Bertok, Zsuzsanna Kuruczne Ribai, Laszlo Pap, Istvan Szekely