The Hetero Ring Is Six-membered Patents (Class 549/356)
Plural ring oxygens in the hetero ring (e.g., 1,2-dioxin, etc.) (Class 549/357)
Polycyclo ring system having the hetero ring as one of the cyclos (Class 549/381)
Plural hetero rings (Class 549/414)
Chalcogen bonded directly to the hetero ring (Class 549/416)
Nitrogen bonded directly to the hetero ring (Class 549/424)
Having -c(=x)-, wherein x is chalcogen, bonded directly to the hetero ring (Class 549/425)
Nitrogen attached indirectly to the hetero ring by nonionic bonding (Class 549/426)
Chalcogen attached indirectly to the hetero ring by nonionic bonding (Class 549/427)
Halogen attached directly or indirectly to the hetero ring by nonionic bonding (Class 549/428)
  • Pyrans as liquid crystals
    Patent number: 6974607
    Abstract: Tetrahydropyran derivatives having at least one ester group (—CO—O—) and at least one group —CN, —NCS, —F, —Cl, —OCHF2, —OCF3, —CF3, —OCHFCF3, —OCF2CHFCF3, SF5, or —OCF2CF3; a process for preparing said tetrahydropyran derivatives, and the use of said tetrahydropyran derivatives as a component in a liquid crystal composition.
    Type: Grant
    Filed: May 27, 2004
    Date of Patent: December 13, 2005
    Assignee: Merck Patent GmbH
    Inventors: Mark John Goulding, Warren Duffy, Kevin Adlem, Peer Kirsch, Alexander Hahn, Eike Poetsch, Werner Binder, Volker Meyer, Melanie Klasen-Memmer, Michael Heckmeier, Georg Lüssem
  • Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor Type-1 (PAI-1)
    Patent number: 6939886
    Abstract: This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.
    Type: Grant
    Filed: July 20, 2004
    Date of Patent: September 6, 2005
    Assignee: Wyeth
    Inventors: Scott Christian Mayer, Eric Gould Gundersen, Hassan Mahmoud Elokdah, David LeRoy Crandall
  • Flavanol and cysteamine conjugates
    Patent number: 6936726
    Abstract: The present invention refers to new products generated by the conjugation of flavanols with molecules that contain the thiol group. New molecules are obtained from polyphenolic plant extracts rich in oligomeric and polymeric procyanidines and prodelfinidins. In this way, new products are generated with antioxidant properties for application as protective agents for the organism against disorders such as cancer, cardiovascular diseases and premature aging. The invention also refers to obtaining these new agents from waste material generated by the agroalimentary industry. Since these waste materials are highly complex mixtures a simple and effective method is described to isolate and purify these, based on the physico-chemical characteristics of the new molecules.
    Type: Grant
    Filed: December 14, 2001
    Date of Patent: August 30, 2005
    Assignee: Consejo Superior de Investigaciones Cientificas
    Inventor: José Luis Torres Simón
  • Protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for the production and the use
    Patent number: 6933385
    Abstract: The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: August 23, 2005
    Assignee: Schering AG
    Inventors: Jurgen Westermann, Johannes Platzek, Orlin Petrov
  • Multicomponent synthesis of amino acids and derivatives thereof
    Patent number: 6930200
    Abstract: Mono-substituted and di-substituted alpha-amino acids and derivatives thereof, substituted at the alpha positon with one (mono-) or two (di-) substituents (R2 and/or R3) as shown in Formula 1: N(R4R5)C(R2R3)CO(OR1).
    Type: Grant
    Filed: June 26, 2003
    Date of Patent: August 16, 2005
    Assignee: Pharmacore, Inc.
    Inventor: Adnan M. M. Mjalli
  • Liquid-crystalline medium
    Patent number: 6902777
    Abstract: A liquid-crystalline mediums which contain one or more compounds of the formula A and at least one compound of the formula B wherein compounds of formula A contain at least one ring selected from and in which Ra, Rb, ring A and ring B, Y, Z1, Z2, a, L1, L2, L3, L4, L5, L6, L7, L8 and L9 are as defined herein, are suitable for use in twisted nematic (TN) and supertwisted nematic (STN) liquid-crystal displays. Such displays have very short response times and good steepnesses and angle dependencies.
    Type: Grant
    Filed: December 22, 2003
    Date of Patent: June 7, 2005
    Assignee: Merck Patent GmbH
    Inventors: Harald Hirschmann, Eike Poetsch, Peer Kirsch, Sabine Schoen
  • Triazolo-epothilones
    Patent number: 6900160
    Abstract: The invention relates to triazolo-thiazole analogues of epothilone A and epothilone B.
    Type: Grant
    Filed: September 21, 2001
    Date of Patent: May 31, 2005
    Assignee: Gesellschaft fuer Biotechnologische Forschung mbH
    Inventors: Gerhard Hoefle, Nicole Glaser
  • Epoxidized acetals and thioacetals, episulfidized acetals and thioacetals, and reworkable thermosetting resin compositions formulated therefrom
    Patent number: 6887737
    Abstract: This invention relates to epoxidized acetals and thioacetals, episulfidized acetals and thioacetals, thermosetting resin compositions based on such epoxidized acetals and thioacetals, episulfidized acetals and thioacetals, reaction products of which are controllably degradable when subjected to appropriate conditions.
    Type: Grant
    Filed: December 13, 2001
    Date of Patent: May 3, 2005
    Assignee: Henkel Corporation
    Inventors: John G. Woods, Afranio Torres-Filho, Rebecca L. Tishkoff, Erin K. Yaeger, Jianzhao Wang
  • Red-emitting organic electroluminescent compound
    Patent number: 6867309
    Abstract: A red-emitting organic electroluminescent compound, the structure of the compound as follows: wherein n is an integer of 1˜6; Ar represents aryl or heteroaryl; R1 and R2 individually represent alkyl of from 1 to 20 carbon atoms, aryl, carbocyclic and other heterocyclic systems; R3 and R4 individually represent hydrogen, alkyl of from 1 to 10 atoms, branched or unbranched 5 or 6 member substituent ring connecting respectively with R1 and R2, or alkyl methyl silane group; R5 represents alkyl of from 1 to 20 atoms, aryl, or heteroaryl; and R6 represents alkyl of from 1 to 10 atoms, and a 5 or 6-member carbocyclic ring connecting with R5.
    Type: Grant
    Filed: December 5, 2002
    Date of Patent: March 15, 2005
    Assignees: Chi Mei Optoelectronics Corporation, Kyocera Corporation
    Inventors: Ruey-Min Chen, Jun-Wen Chung, Chun-Che Hsu
  • Cyclic ketals, fragrance compositions containing the same and methods of using the same
    Patent number: 6864225
    Abstract: Compounds of the general formula (I) are described: wherein each of R1, R2, R3, R4, R5 and R6 independently represents a substituent selected from the group consisting of hydrogen, methyl, ethyl, n-propyl, and isopropyl; an wherein x represents either 0 or 1. The compounds are useful as fragrances and as added components in fragrance blends. Methods of improving the harmony, emanation, naturalness an staying power of other fragrance ingredients by the addition of such compounds are also described.
    Type: Grant
    Filed: April 28, 2001
    Date of Patent: March 8, 2005
    Assignee: Kao Corporation
    Inventors: Thomas Markert, Theo Ten Pierik, Werner Faber
  • Melvinolin derivatives
    Patent number: 6818638
    Abstract: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.
    Type: Grant
    Filed: July 11, 2002
    Date of Patent: November 16, 2004
    Assignee: Novartis AG
    Inventors: Rolf Baenteli, Wilfried Bauer, Sylvain Cottens, Claus Ehrhardt, Ulrich Hommel, Jörg Kallen, Josef Gottfried Meingassner, François Nuninger, Gabriele Weitz Schmidt
  • Derivatives of 2-(iminomethyl)amino-phenyl, their preparation, their use as medicaments and the pharmaceutical compositions containing them
    Patent number: 6809088
    Abstract: The invention relates to new derivatives of 2-(iminomethyl)amino-phenyl which are NO synthase inhibitors and can trap reactive oxygen species. These compounds can notably be used for the treatment of stroke, of neurodegenerative diseases and of ischemic or hemorragic cardiac or cerebral infarctions.
    Type: Grant
    Filed: July 9, 2002
    Date of Patent: October 26, 2004
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet, Jeremiah Harnett
  • Oxabicyclooctanes
    Patent number: 6808762
    Abstract: The present invention relates to oxabicyclooctanes of the general formula I. in which R1, R2, A1, A2, A3, A4, L1, L2, n1, n2 and n3 have the meanings specified in claim 1, and to their use in liquid-crystalline media.
    Type: Grant
    Filed: October 1, 2002
    Date of Patent: October 26, 2004
    Assignee: Merck Patent GmbH
    Inventors: Matthias Bremer, Michael Heckmeier, Melanie Klasen-Memmer, Harald Lannert
  • Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
    Patent number: 6800654
    Abstract: This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are eachH, alkyl,, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: October 5, 2004
    Assignee: Wyeth
    Inventors: Scott Christian Mayer, Eric Gould Gundersen, Hassan Mahmoud Elokdah, David LeRoy Crandall
  • Epoxy resin composition, cured article thereof, novel epoxy resin, novel phenol compound, and process for preparing the same
    Patent number: 6784228
    Abstract: The present invention relates to an epoxy resin composition a cure article thereof, a novel epoxy resin used therein, a polyhydric phenol compound suited for used as an intermediate thereof, and a process for preparing the same. One of the objects to be achieved by the present invention is to exert the heat resistance, the moisture resistance, the dielectric performances and the flame-resistant effect required of electric or electronic materials such as semiconductor encapsulating materials and varnishes for circuit boards in the epoxy resin composition.
    Type: Grant
    Filed: July 9, 2002
    Date of Patent: August 31, 2004
    Assignee: Dainippon Ink and Chemicals, Inc.
    Inventors: Ichiro Ogura, Yoshiyuki Takahashi, Tomoyuki Imada
  • Dihetero-substituted metalloprotease inhibitors
    Patent number: 6762198
    Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where J, M, Q, T, W, X, Z, R1, R2, R3, R4, R4′, R5, R6, R6′, R7, m, and n have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also disclosed are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
    Type: Grant
    Filed: March 25, 2003
    Date of Patent: July 13, 2004
    Assignee: The Procter & Gamble Company
    Inventors: Menyan Cheng, Neil Gregory Almstead, Michael George Natchus, Stanislaw Pikul, Biswanath De
  • Method for producing unsaturated cyclic ethers
    Publication number: 20040092753
    Abstract: A method for producing unsaturated cyclic ethers of general formula (I) wherein Z represents (CHR4)q— or (CHR4)q—O—, q 0, 1, 2 or 3 and R1, R2, R3, R4 represent hydrogen or C1-C4-alkyl, by reacting dioles of general formula (II), wherein Z, R1, R2 and R3 have the above-mentioned meanings, in a liquid phase at temperatures of 150-300° C. in the presence of a support catalyst which is not activated prior to use by reduction and which contains cobalt and is doped with sulphur, containing cobalt, and an earth metal which is deposited by sol impregnation and is selected from the group containing platinum, palladium, rhodium, iridium, ruthenium, osmium, rhenium or mixtures thereof, on an inert support, characterized in that water is added.
    Type: Application
    Filed: September 3, 2003
    Publication date: May 13, 2004
    Inventors: Hagen Weigl, Klaus Ebel, Sylvia Huber, Andreas Kusche, Karsten Eller, Michael Hesse, Arthur Hohn
  • 4,7-dichlororhodamine dye labeled polynucleotides
    Patent number: 6713622
    Abstract: A set of 4,7-dichlororhodamine compounds useful as fluorescent dyes are disclosed having the structures wherein R1-R6 are hydrogen, fluorine, chlorine, lower alkyl, lower alkene, lower alkyne, sulfonate, sulfone, amino, amido, nitrile, lower alkoxy, linking group, or, when taken together, R1 and R6 is benzo, or, when taken together, R4 and R5 is benzo; R7-R10, R12-R16 and R18 may be hydrogen, fluorine, chlorine, lower alkyl, lower alkene, lower alkyne, sulfonate, sulfone, amino, amido, nitrile, lower alkoxy, linking group; R11 and R17 may be hydrogen, lower alkyl, lower alkene, lower alkyne, phenyl, aryl, linking group; Y1-Y4 are hydrogen, lower alkyl, or cycloalkyl, or, when taken together, Y1 and R2, Y2 and R1 Y3 and R3, and/or Y4 and R4 is propano, ethano, or substituted forms thereof, and X1-X3 taken separately are hydrogen, chlorine, fluorine, lower alkyl, carboxylate, sulfonate, hydroxymethyl, and linking group, or any combinations thereof In another aspect, the invention includes reag
    Type: Grant
    Filed: May 25, 2000
    Date of Patent: March 30, 2004
    Assignee: Applera Corporation
    Inventor: Ronald J. Graham
  • Chemo-enzymatic synthesis of optically enriched rose-oxides
    Patent number: 6692944
    Abstract: The present invention relates to a process for the systhesis of optically enriched dextro- and laevo-rotatory isomers of rose oxide from racemic citronellol. The invention particularly relates to the preparation of optically enriched (−)-(2 S, 4 R)-rose oxide and its isomer (+)-(2 R, 4 S)-rose oxide torn racemic citronellol.
    Type: Grant
    Filed: March 29, 2002
    Date of Patent: February 17, 2004
    Inventors: Shubash Chandra Taneja, Vijay Kumar Sethi, Surrinder Koul, Samar Singh Andotra, Ghulam Nabi Qazi
  • Protecting groups useful in the synthesis of polysaccharides, natural products, and combinatorial libraries
    Patent number: 6693178
    Abstract: One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.
    Type: Grant
    Filed: May 15, 2002
    Date of Patent: February 17, 2004
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, Obadiah J. Plante, Peter H. Seeberger
  • Metalloprotease inhibitors
    Patent number: 6686348
    Abstract: A compound of formula (I): wherein: R1 represents hydrogen, halogen, alkyl or alkoxy, X represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl, A represents any one of the groups described in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitor.
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: February 3, 2004
    Assignee: Les Laboratoires Servier
    Inventors: Guillaume De Nanteuil, Alain Benoist, Philippe Pastoureau, Massimo Sabatini, John Hickman, Alain Pierre, Gordon Tucker
  • N-(4-carbamimidoyl-phenyl)-glycine derivatives
    Patent number: 6683215
    Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
    Type: Grant
    Filed: October 4, 2002
    Date of Patent: January 27, 2004
    Assignee: Hoffman-La Roche Inc.
    Inventors: Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
  • Il-8 receptor antagonists
    Patent number: 6664259
    Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Grant
    Filed: September 6, 2002
    Date of Patent: December 16, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Katherine Louisa Widdowson, Qi Jin
  • Difluorovinyl compound, liquid crystal composition and liquid crystal display
    Patent number: 6649227
    Abstract: Provided are liquid crystalline compounds having a wide liquid crystal phase temperature range, low viscosity, a large elastic constant ratio K33/K11 and excellent solubility at low temperature, a liquid crystal composition using the same and a liquid crystal display.
    Type: Grant
    Filed: July 6, 2001
    Date of Patent: November 18, 2003
    Assignees: Chisso Corporation, Chisso Petrochemical Corporation
    Inventors: Takashi Kato, Shuichi Matsui, Hiroyuki Takeuchi, Yasuhiro Kubo, Etsuo Nakagawa
  • Alkyl-dihalogenophenyl-substituted ketoenols
    Publication number: 20030199572
    Abstract: The present invention relates to new compounds of the formula (I) 1
    Type: Application
    Filed: December 14, 2001
    Publication date: October 23, 2003
    Inventors: Folker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Peter Dahmen, Markus Dollinger, Hans-Joachim Santel, Alan Graff, Wolfram Andersch, Norbert Mencke, Andreas Turberg
  • Polyalkylbicylic derivatives
    Patent number: 6632788
    Abstract: The compound according to the formula set forth below where A is B is or A and B together form the ring structure and X, R′ and R are independently H and CH3 and m=0 or 1. and the use of the compound in creating fragrances, and scents in items such as perfumes, colognes and personal care products is disclosed.
    Type: Grant
    Filed: May 17, 2001
    Date of Patent: October 14, 2003
    Assignee: International Flavors & Fragrances Inc.
    Inventors: Anthony T. Levorse, Jr., Anubhav P.S. Narula, Edward Mark Arruda, Charles E.J. Beck
  • Method for producing 3,4-dihydro-2h-pyran
    Publication number: 20030162980
    Abstract: A process for preparing 3,4-dihydro-2H-pyran by reacting tetrahydrofurfuryl alcohol over solid oxidic catalysts at temperatures of from 150 to 400° C. and pressures of from 0.001 to 50 bar, which comprises carrying out the reaction in the gas phase in a tube bundle reactor.
    Type: Application
    Filed: January 27, 2003
    Publication date: August 28, 2003
    Inventors: Hagen Weigl, Klaus Ebel, Joachim Simon
  • PROCESS FOR PRODUCING A SATURATED CYCLIC ETHER
    Publication number: 20030149282
    Abstract: A method for producing a saturated cyclic ether from a fatty acid ester of an &agr;,&dgr;-diol stably in high yield over a long period of time, is presented. It is a process for producing a saturated cyclic ether, which comprises reacting a mono- and/or di-fatty acid ester of an &agr;,&dgr;-diol in the presence of a solid acid catalyst, wherein the reaction is carried out in such a state that at least 50 mol % of the fatty acid ester supplied to the reaction system is vaporized.
    Type: Application
    Filed: December 12, 2002
    Publication date: August 7, 2003
    Applicant: MITSUBISHI CHEMICAL CORPORATION
    Inventors: Kazuhiko Kiyooka, Toshiharu Yokoyama
  • Novel methine compound, material for organic luminescence element, and organic luminescence element using the same
    Publication number: 20030134148
    Abstract: Disclosed is a novel methine compound, for examples, which is represented by the following formula (I): 1
    Type: Application
    Filed: November 8, 2002
    Publication date: July 17, 2003
    Applicant: FUJI PHOTO FILM CO., LTD.
    Inventors: Hisashi Okada, Terukazu Yanagi
  • Aryl or heteroaryl substituted 3,4-dihydroanthracene and aryl or heteroaryl substituted benzo[1,2-g]-chrom-3-ene, benzo[1,2-g]-thiochrom-3-ene and benzo [1,2-g]-1,2-dihydroquinoline derivatives having retinoid antagonist or retinoid inverse agonist type biological activity
    Publication number: 20030130515
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: January 2, 2003
    Publication date: July 10, 2003
    Inventors: Vidyasagar Vuligonda, Alan T. Johnson, Roshantha A. Chandraratna
  • Process for the production of oxandrolone
    Publication number: 20030109721
    Abstract: The present invention relates to a process for the synthesis of oxandrolone from mestanolone. The process comprises the steps of: (a) oxidizing mestanolone to form 17&bgr;-hydroxy-17&agr;-methyl-5&agr;-androst-1-en-3-one; (b) hydroxylating the 17&bgr;-hydroxy-17&agr;-methyl-5&agr;-androst-1-en-3-one to form 1&agr;,2&agr;,17&bgr;-trihydroxy-17&agr;-methylandrostan-3-one; (c) cleaving the 1&agr;,2&agr;,17&bgr;-trihydroxy-17&agr;-methylandrostan-3-one to form 17&bgr;-hydroxy-17&agr;-methyl-1-oxo-1,2,-seco-A-nor-5&agr;-androstan-2-oic acid; and (d) reducing the 17&bgr;-hydroxy-17&agr;-methyl-1-oxo-1,2,-seco-A-nor-5&agr;-androstan-2-oic acid to form oxandrolone.
    Type: Application
    Filed: December 11, 2001
    Publication date: June 12, 2003
    Inventors: Shaileshkumar Ramanlal Desai, David Wayne Ray, Yousry A. Sayed
  • Hetero-substituted metalloprotease inhibitors
    Patent number: 6566381
    Abstract: Heterocyclic substituted compounds having the general structure: which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: May 20, 2003
    Assignee: The Procter & Gamble Company
    Inventors: Menyan Cheng, Neil Gregory Almstead, Michael George Natchus, Stanislaw Pikul, Biswanath De
  • Cyclic pro-perfumes having modifiable fragrance raw material alcohol release rates
    Patent number: 6544945
    Abstract: The present invention relates to cyclic pro-perfumes comprising a moiety derived from a fragrance raw material alcohol. Such cyclic perfumes may contain dioxolane and glucosyl orthesters that are suitable for use in delivering enhanced fragrance longevity to human skin.
    Type: Grant
    Filed: August 23, 2000
    Date of Patent: April 8, 2003
    Assignee: The Procter & Gamble Company
    Inventors: Gregory Scot Miracle, Kenneth Nathan Price, Lon Montgomery Gray
  • Substituted diarylalkyl amides as calcium channel antagonists
    Patent number: 6458781
    Abstract: The present invention provides compounds that block calcium channels and have the Formula I: The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.
    Type: Grant
    Filed: October 25, 1999
    Date of Patent: October 1, 2002
    Inventors: David Thomas Connor, Lain-Yen Hu, Thomas Charles Malone, Michael Francis Rafferty, Bruce David Roth, Todd Robert Ryder, Anthony Denver Sercel, Yuntao Song
  • Methine compound, material for organic luminescence element, organic luminescence element using the same
    Patent number: 6458474
    Abstract: Disclosed is a novel methine compound, for example, which is represented by the following formula (I): wherein R1, R2, R3, R4 and R5 each represents a hydrogen atom or a substituent; X represents an oxygen atom, a sulfur atom, or N—R6; Z represents —NR7R8, or —OG; R6, R7 and R8 each represents a hydrogen atom or a substituent; G represents a hydrogen atom, a cation or a substituent; L1, L2 and L3 each represents a substituted or unsubstituted methine group; n represents 1 or 2; and W represents an electron attractive group.
    Type: Grant
    Filed: March 18, 1999
    Date of Patent: October 1, 2002
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Okada, Terukazu Yanagi
  • Process for the preparation of substitued pyranes
    Patent number: 6455707
    Abstract: Substituted pyranes such as 2-ethinyl-tetrahydro-2,6,6-trimethylpyran are prepared from dehydrolinalool or higher homologues thereof by heating or treatment with microwaves in the presence of a solid acid.
    Type: Grant
    Filed: August 31, 2001
    Date of Patent: September 24, 2002
    Assignee: Roche Vitamins, Inc.
    Inventors: Werner Bonrath, Fabio Cirillo
  • Acylaminoalkyl-substituted benzenesulfonamide derivatives, their preparation, their use and pharmaceutical preparations comprising them
    Publication number: 20020123494
    Abstract: One embodiment of the present invention relates to acylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), 1
    Type: Application
    Filed: November 2, 2001
    Publication date: September 5, 2002
    Inventors: Holger Heitsch, Heinrich Christian Englert
  • Process for the preparation of substitued pyranes
    Publication number: 20020103388
    Abstract: Substituted pyranes such as 2-ethinyl-tetrahydro-2,6,6-trimethylpyran are prepared from dehydrolinalool or higher homologues thereof by heating or treatment with microwaves in the presence of a solid acid.
    Type: Application
    Filed: August 31, 2001
    Publication date: August 1, 2002
    Inventors: Werner Bonrath, Fabio Cirillo
  • Tetracyclic acetals
    Patent number: 6420334
    Abstract: 2-Alkoxydecahydro-2,3a,4,4,7-pentamethyl-3,7a-methano-7aH-indeno[5,6-b]furans are valuable novel woody fragrances for the preparation of perfume oils.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: July 16, 2002
    Assignee: Haarmann & Reimer GmbH
    Inventors: Horst Surburg, Peter Wörner
  • Glycomimetics as selectin antagonists and pharmaceuticals having antiinflammatory activity
    Patent number: 6413936
    Abstract: The invention relates to novel mimetics of the tetrasaccharides sialyl-Lewis-X and sialyl-Lewis-A having an improved action as inhibitors of cell adhesion, to a process for the preparation of these compounds and to their use as pharmacological active compounds and diagnostic agents.
    Type: Grant
    Filed: October 30, 1996
    Date of Patent: July 2, 2002
    Assignee: Glycorex AB
    Inventors: Wolfgang Schmidt, Ulrich Sprengard, Gerhard Kretzschmar, Robert Klein, Horst Kunz
  • Optically active phosphate derivative
    Patent number: 6391926
    Abstract: An optically active binaphthol derivative of the following formula (1) or (2), an optically active phosphate derivative of the following formula (3) or, (4), processes for their production, and an asymmetry identifying agent comprising the derivative of the formula (3) or (4):
    Type: Grant
    Filed: March 8, 2001
    Date of Patent: May 21, 2002
    Assignee: Tosoh Corporation
    Inventor: Junji Inanaga
  • Method for synthesizing C-glycosides of ulosonic acids
    Patent number: 6376662
    Abstract: A method for synthesizing C-glycosides of ulosonic acids such as Neu5Ac, by which diastereocontrolled synthesis of &agr;-C-glycosides of ulosonic acids is attained is disclosed. In the method of the present invention, an ulosonic acid sulfone or phosphite is reacted with an aldehyde or ketone compound in the presence of a lanthanide metal halide.
    Type: Grant
    Filed: November 17, 1998
    Date of Patent: April 23, 2002
    Assignee: University of Iowa Research Foundation
    Inventors: Robert J. Linhardt, Iontcho R. Vlahov
  • Phenoketals and the use thereof as odoriferous substances
    Patent number: 6376457
    Abstract: Phenone ketals corresponding to formula (I): where X and Y independently of one another represent methoxy, ethoxy, propoxy or butoxy groups and R1 is a methyl, ethyl or propyl group, R2 is hydrogen or a methyl, ethyl, isopropyl, tert.butyl or methoxy group, R3 is hydrogen or a methoxy group and R4 is hydrogen or a methyl group; their use as a component of perfumes; and perfume compositions containing them.
    Type: Grant
    Filed: October 1, 1999
    Date of Patent: April 23, 2002
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventors: Thomas Markert, Ralph Nemitz
  • Method of locking 1 &agr;-OH of vitamin D compounds in axial orientation
    Patent number: 6369099
    Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.
    Type: Grant
    Filed: April 20, 2000
    Date of Patent: April 9, 2002
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Rafal R. Sicinski
  • (3R,4R)-&Dgr;8-tetrahydrocannabinol-11-oic acids useful as antiinflammatory agents and analgesics
    Patent number: 6355650
    Abstract: The present invention relates to non-psychoactive derivatives of tetrahydro-cannabinol, which exhibit anti-inflammatory, analgesic and leukocyte antiadhesion activities. The invention includes novel derivatives of (3R,4R)-&Dgr;8-tetrahydrocannabinol-11-oic acids [hereinafter referred to as (3R,4R)-&Dgr;8-THC-11-oic acid], as well as pharmaceutical compositions containing the (3R,4R)-&Dgr;8-THC-11-oic acid derivatives. The invention further covers methods of administering the novel derivatives and pharmaceutical compositions as therapeutic agents in the treatment of pain and tissue inflammation. Non-psychoactive derivatives of &Dgr;8-THC-11-oic acid are described which have analgesic and anti-inflammatory properties.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: March 12, 2002
    Assignee: Atlantic Technology Ventures, Inc.
    Inventor: Sumner H. Burstein
  • Liquid-crystal compounds having large negative value of permittivity anisotropy, liquid-crystal composition, and liquid-crystal display element
    Patent number: 6348244
    Abstract: An object of the present invention is to provide novel liquid crystalline compounds having a negative and extremely large dielectric anisotropy value and a small optical anisotropy value together, to provide liquid crystal compositions comprising the liquid crystalline compound, and to provide liquid crystal display devices fabricated by using the liquid crystal composition; the liquid crystalline compounds have 2,3-difluorophenyl moiety and are expressed by the general formula (1) wherein Ra and Rb each independently represent a straight chain or branched alkyl group having 1 to 10 carbon atoms in which group any methylene group may be replaced by —O—, —CH═CH—, or —C≡C—, but there is not a case wherein —O— continues; ring A1 represents cyclohexane-1,4-diyl not adjacent any methylene group may be replaced by —O—; ring A2 represents 2,3-difluoro-1,4-phenylene in which phenylene hydrogen atoms at 5-position and 6-position m
    Type: Grant
    Filed: April 24, 2000
    Date of Patent: February 19, 2002
    Assignee: Chisso Corporation
    Inventors: Kazutoshi Miyazawa, Hiroyuki Takeuchi, Yasuhiro Kubo, Fusayuki Takeshita, Etsuo Nakagawa
  • Disubstituted acetylenes bearing heterobicyclic groups and heteroaromatic or phenyl groups having retinoid like activity
    Patent number: 6344463
    Abstract: Compounds of the formula where R1 and R2, independently are alkyl groups having 2 to 8 carbons; R3 is hydrogen or lower alkyl; X is S, O or N—R4 where R4 is hydrogen or lower alkyl; Y is phenyl or pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl; A is (CH2)n where n is 0-5, or lower branched chain alkyl, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a salt thereof, COOR5, CONR6R7, —CH2OH, CH2OR8, CH2OCOR8, CHO, CH(OR9)2, CHOR10O, —COR11, CR11(OR9)2, or CR11OR10O, where R5 is alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or R5 is phenyl or lower alkylphenyl, R6 and R7 independently are hydrogen, alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or phenyl or lower alkylphenyl, R8 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R9 is lower alkyl, R10 is divalent alkyl radical of 2-5 carbons and R11 is alkyl, cycloalkyl or alkenyl containing 1
    Type: Grant
    Filed: July 7, 2000
    Date of Patent: February 5, 2002
    Assignee: Allergan Sales, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade
    Publication number: 20020010344
    Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 1,4-quinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
    Type: Application
    Filed: April 10, 2001
    Publication date: January 24, 2002
    Inventors: Michael S. South, John J. Parlow
  • 2-(iminomethyl) amino-phenyl derivatives, preparation, application as medicines and pharmaceutical compositions containing same
    Patent number: 6340700
    Abstract: A compound of the formula wherein the substituents are defined as in the specification and their pharmaceutically acceptable salts having NOS and ROS activity.
    Type: Grant
    Filed: September 22, 1999
    Date of Patent: January 22, 2002
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet
  • Haloalkyl derivatives of reporter molecules used to analyze metabolic activity in cells
    Patent number: RE38723
    Abstract: The subject invention provides substrates useful for analyzing the metabolic activity in cells by improving the retention of a detectable reporter molecule only in intact cells where a particular enzyme is present. In particular, improved retention results from a two part process involving conjugation of haloalkyl-substituted derivatives of a reporter molecule with intracellular cysteine-containing peptides while unblocking the reporter molecule. The substrates have the form XR-SPACER-REPORTER-BLOCK wherein -BLOCK is a group selected to be removable by action of a specific analyte, to give REPORTER spectral properties different from those of the substrate, -REPORTER- is a molecule that, when no longer bound to BLOCK by a BLOCK-REPORTER bond, has spectral properties different from those of the substrate, -SPACER- is a covalent linkage, and XR- is a haloalkyl moiety that can covalently react with an intracellular thiol (Z-S-H) to form a thioether conjugate (Z-S-R).
    Type: Grant
    Filed: August 12, 1997
    Date of Patent: April 12, 2005
    Assignee: Molecular Probes, Inc.
    Inventors: Fei Mao, Ram Sabnis, John Naleway, Nels Olson, Richard P. Haugland