Polycyclo Ring System Having The Lactone Ring As One Of The Cyclos Patents (Class 549/297)
  • Patent number: 9084755
    Abstract: A method for extracting and separating ginkgolides. The ginkgolides obtained through steps of extraction on a ginkgo leaf, further extraction, column chromatography, crystallization, and crystal mixing comprise 25.0% to 50.0% of bilobalide (C15H18O8), 20.0% to 45.0% of ginkgolide A (C20H24O9), 10.0% to 30.0% of ginkgolide B (C20H24O10), and 5.0% to 15.0% of ginkgolide C (C20H24O11). The total quantity of the bilobalide, the ginkgolide A, the ginkgolide B, and the ginkgolide C is over 95%.
    Type: Grant
    Filed: October 23, 2014
    Date of Patent: July 21, 2015
    Assignee: CHENGDU BAIYU TECHNOLOGY PHARMACY CO., LTD.
    Inventors: Yi Sun, Yonghong Zhu, Zhengbing Tong, Jie Wang
  • Publication number: 20150148384
    Abstract: Disclosed herein are novel A-ring epoxidized triterpenoid compounds and derivatives thereof, including those of the formula (I), wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example as antioxidant inflammation modulators, and compositions thereof are also provided.
    Type: Application
    Filed: June 14, 2013
    Publication date: May 28, 2015
    Applicant: REATA PHARMACEUTICALS, INC.
    Inventors: Eric Anderson, Christopher F. Bender, Xin Jiang, Xiaofeng Liu, Haizhou Sun, Melean Visnick
  • Publication number: 20150141633
    Abstract: The disclosure relates to a method for enhancing the biosynthesis and/or secretion of sapogenins in the culture medium of plant and microbial cell cultures. Further, the disclosure also relates to the identification of novel genes involved in the biosynthesis of sapogenin intermediates, as well as to novel sapogenin compounds.
    Type: Application
    Filed: May 13, 2013
    Publication date: May 21, 2015
    Inventors: Alain Goossens, Tessa Moses, Jacob Pollier, Lorena Almagro Romero
  • Publication number: 20150044233
    Abstract: Methods for determining the presence of cancer stem cells by detecting GD2 expression. Also provided are methods for reducing proliferation of cancer stem cells by contacting the cells with a GD2 targeting agent, such as an anti-GD2 antibody or a GD3 synthase inhibitor. GD3 synthase inhibitor compounds are also provided.
    Type: Application
    Filed: February 27, 2013
    Publication date: February 12, 2015
    Inventors: Venkata Battula, Michael Andreeff, Sendurai A. Mani, Tapasree Roy Sarkar
  • Patent number: 8637623
    Abstract: Disclosed is a monomer having an electron-withdrawing substituent and a lactone skeleton, represented by Formula (1), wherein Ra represents, e.g., hydrogen or an alkyl group having 1 to 6 carbons; R1 represents, e.g., a halogen or an alkyl or haloalkyl group having 1 to 6 carbons; “A” represents an alkylene group having 1 to 6 carbons, oxygen, sulfur, or is nonbonding; “m” denotes an integer of 0 to 8; Xs each represent an electron-withdrawing substituent; “n” denotes an integer of 1 to 9; and Y represents a bivalent organic group having 1 to 6 carbons. The monomer is useful as a monomer component typically for a highly functional polymer, because, when the monomer is applied to a resist resin, the resin is stable and resistant to chemicals, is highly soluble in organic solvents, and has improved hydrolyzability and/or solubility in water after hydrolysis.
    Type: Grant
    Filed: February 3, 2009
    Date of Patent: January 28, 2014
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Hiroshi Koyama, Kyuhei Kitao, Akira Eguchi
  • Patent number: 8617906
    Abstract: The identification of triptolide target molecules is described. Also described are methods of screening triptolide-related compounds for binding to these molecules, including screening for enhanced and/or selective binding, and expression analysis of the target molecules in normal and in diseased tissue.
    Type: Grant
    Filed: October 12, 2005
    Date of Patent: December 31, 2013
    Assignee: Pharmagenesis, Inc.
    Inventors: John M. Fidler, John H. Musser
  • Patent number: 8461357
    Abstract: An expeditious synthesis of gibberellin A5 (GA5) esters is presented, from which GA5 may be prepared. The synthesis offers an inexpensive route of few steps to these compounds, starting from gibberellin A3 (GA3) esters in the presence of a metal hydride.
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: June 11, 2013
    Assignee: UTI Limited Partnership
    Inventors: Kelly A. Fairweather, Lewis N. Mander, Richard P. Pharis
  • Patent number: 8426616
    Abstract: Disclosed are compounds based on lactone ring modifications of triptolide and hydroxylated triptolide, for use in therapy, such as antiproliferative, anticancer, and immunosuppressive therapy.
    Type: Grant
    Filed: September 2, 2010
    Date of Patent: April 23, 2013
    Assignee: Pharmagenesis, Inc.
    Inventors: Hongwei Yuan, John H. Musser, Dongcheng Dai
  • Patent number: 8268882
    Abstract: Disclosed are compounds based on C- and D-ring modifications of triptolide and hydroxylated triptolide, for use in therapy, such as antiproliferative, anticancer, and immunosuppressive therapy.
    Type: Grant
    Filed: February 4, 2010
    Date of Patent: September 18, 2012
    Assignee: Pharmagenesis, Inc.
    Inventor: John H. Musser
  • Publication number: 20120225936
    Abstract: The invention relates to a method for producing triptolide from a suspension cell culture of Tripterygium sp., to a triptolide-enriched extract obtainable by means of extraction from the culture medium of an in vitro culture of dedifferentiated cells of the species Tripterygium, and to the therapeutic applications of said extract.
    Type: Application
    Filed: November 5, 2010
    Publication date: September 6, 2012
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Nicolas Steward, Nadine Chomarat, Ngoc Thien N'Guyen
  • Publication number: 20110288166
    Abstract: Disclosed are compounds based on C- and D-ring modifications of triptolide and hydroxylated triptolide, for use in therapy, such as antiproliferative, anticancer, and immunosuppressive therapy.
    Type: Application
    Filed: February 4, 2010
    Publication date: November 24, 2011
    Inventor: John H. Musser
  • Publication number: 20110263876
    Abstract: An expeditious synthesis of gibberellin A5 (GA5) esters is presented, from which GA5 may be prepared. The synthesis offers an inexpensive route of few steps to these compounds, starting from gibberellin A3 (GA3) esters in the presence of a metal hydride.
    Type: Application
    Filed: September 18, 2009
    Publication date: October 27, 2011
    Applicant: UNIVERSITY TECHNOLOGIES INTERNATIONAL
    Inventors: Kelly A. Fairweather, Lewis N. Mander, Richard P. Pharis
  • Patent number: 8017793
    Abstract: Disclosed is a method for oxidizing an alcohol in an amide solvent using a mixed reagent containing hydrogen peroxide and a tungsten catalyst.
    Type: Grant
    Filed: May 12, 2005
    Date of Patent: September 13, 2011
    Assignee: Shionogi & Co., Ltd.
    Inventors: Takemasa Hida, Kyozo Kawata, Mikio Kabaki
  • Publication number: 20110064662
    Abstract: Disclosed is a kit for use in the production of a molecular probe for PET drug screening for the purpose of producing a compound containing a short-lived radionuclide for PET applications. Specifically disclosed is a kit comprising a compound represented by the formula (I), (II) or (III) or a salt thereof. In the formulae, X1, X2, X3, X4, X5 and X6 are as defined in the description.
    Type: Application
    Filed: October 24, 2008
    Publication date: March 17, 2011
    Applicants: RIKEN, HAMAMATSU PHOTONICS K.K.
    Inventors: Hisashi Doi, Masaaki Suzuki, Hideo Tsukada
  • Patent number: 7863464
    Abstract: Disclosed are compounds based on lactone ring modifications of triptolide and hydroxylated triptolide, for use in therapy, such as antiproliferative, anticancer, and immunosuppressive therapy.
    Type: Grant
    Filed: March 2, 2005
    Date of Patent: January 4, 2011
    Assignee: Pharmagenesis, Inc.
    Inventors: Hongwei Yuan, John H. Musser, Dongcheng Dai
  • Publication number: 20100331554
    Abstract: Disclosed are compounds based on lactone ring modifications of triptolide and hydroxylated triptolide, for use in therapy, such as antiproliferative, anticancer, and immunosuppressive therapy.
    Type: Application
    Filed: September 2, 2010
    Publication date: December 30, 2010
    Inventors: Hongwei Yuan, John H. Musser, Dongcheng Dai
  • Patent number: 7847109
    Abstract: Variously substituted carbonate and carbamate derivatives of triptolide compounds have good aqueous solubility and convert to biologically active compounds in vivo, at a rate which can be modulated by varying the substitution on the prodrug. The prodrugs are useful as immunosuppressive, anti-inflammatory and anticancer agents.
    Type: Grant
    Filed: May 29, 2003
    Date of Patent: December 7, 2010
    Assignee: Pharmagenesis, Inc.
    Inventors: Dongcheng Dai, John H. Musser, Edwin S. Lennox
  • Patent number: 7820834
    Abstract: Compounds useful as immunosuppressive, anti-inflammatory and anticancer agents and methods of their preparation and use are described. The compounds are analogs or derivatives of triptolide and related compounds, modified at the 5- and/or 6-position relative to the naturally occurring compounds.
    Type: Grant
    Filed: December 20, 2004
    Date of Patent: October 26, 2010
    Assignee: Pharmagenesis, Inc.
    Inventors: Dongcheng Dai, John H. Musser, Hongwei Yuan
  • Patent number: 7759044
    Abstract: A dissolution modification agent suitable for use in a photoresist composition including a polymer, a photoacid generator and casting solvent. The dissolution modification agent is insoluble in aqueous alkaline developer and inhibits dissolution of the polymer in the developer until acid is generated by the photoacid generator being exposed to actinic radiation, whereupon the dissolution modifying agent, at a suitable temperature, becomes soluble in the developer and allows the polymer to dissolve in the developer. The DMAs are glucosides, cholates, citrates and adamantanedicarboxylates protected with acid-labile ethoxyethyl, tetrahydrofuranyl, and angelicalactonyl groups.
    Type: Grant
    Filed: January 25, 2008
    Date of Patent: July 20, 2010
    Assignee: International Business Machines Corporation
    Inventors: Robert David Allen, Phillip Joe Brock, Richard Anthony DiPietro, Ratnam Sooriyakumaran, Hoa D. Truong
  • Patent number: 7749679
    Abstract: A photosensitive composition containing a compound having a specific structure, a pattern-forming method using the photosensitive composition, and a compound having a specific structure used in the photosensitive composition.
    Type: Grant
    Filed: December 21, 2006
    Date of Patent: July 6, 2010
    Assignee: FUJIFILM Corporation
    Inventors: Kenji Wada, Kunihiko Kodama
  • Publication number: 20100056621
    Abstract: The present invention relates to agonists of the hTAS2R14 bitter taste receptor and its role in bitter taste transduction. The invention also relates to assays for screening molecules that modulate, e.g. suppress or block hTAS2R14 bitter taste transduction or bitter taste response.
    Type: Application
    Filed: April 20, 2005
    Publication date: March 4, 2010
    Applicant: Deutsches Institut fur Ernahrungsforschung
    Inventors: Maik Behrens, Anne Brockhoff, Bernd Bufe, Christina Kuhn, Wolfgang Meyerhof, Marcel Winnig
  • Patent number: 7662976
    Abstract: Variously substituted carbonate and carbamate derivatives of triptolide compounds have good aqueous solubility and convert to biologically active compounds in vivo, at a rate which can be modulated by varying the substitution on the prodrug. The prodrugs are useful as immunosuppressive, anti-inflammatory and anticancer agents.
    Type: Grant
    Filed: February 5, 2009
    Date of Patent: February 16, 2010
    Assignee: Pharmagenesis, Inc.
    Inventors: Dongcheng Dai, John H. Musser, Edwin S. Lennox
  • Patent number: 7626044
    Abstract: Triptolide derivatives of Formula (I), their pharmaceutically acceptable salts and optical isomers, Formula (I): wherein, C5 and C6 are connect with each other by a C-C single bond or double bond; when C5 and C6 are connected with C-C single bond, X and Y represent independently hydrogen, oxygen, hydroxyl, halogen, lower alkyl-oxy, lower alkyl-amino, mercapto, lower alkyl-thio, the group of formula —OCOR, —OSO2OR or —OPO(OH)2, each of which is attached to C5 and C6, R represents —(CH2)nCO2Na, —(CO2)nCO2K, or —(CH2)nCH3, wherein n=1-6; Z represents hydrogen, oxygen, hydroxyl, halogen, lower alkyl-oxy, lower alkyl-amino, mercapto, lower alkyl-thio, the group of formula -OCOR, -OSO2OR or —OPO(OH)2, each of which is linked at C14-position, R represents —(CH2)nCO2Na, —(CO2)nCO2K, or —(CH2)nCH2, wherein n=1-6; wherein, the“______” linked with X, Y, and Z represents the stereochemistry orientations “” or “” , but X and Y cannot both be hydrogen atom at the same time, methods for preparing the triptolides and the
    Type: Grant
    Filed: January 28, 2003
    Date of Patent: December 1, 2009
    Assignees: Shanghai Institute of Materia Medica Chinese Academy of Sciences, Shanghai Pharmaceutical (Group) Co., Ltd.
    Inventors: Yuanchao Li, Jianping Zuo, Fan Zhang, Ru Zhou, Jian Ding
  • Publication number: 20090171103
    Abstract: Variously substituted carbonate and carbamate derivatives of triptolide compounds have good aqueous solubility and convert to biologically active compounds in vivo, at a rate which can be modulated by varying the substitution on the prodrug. The prodrugs are useful as immunosuppressive, anti-inflammatory and anticancer agents.
    Type: Application
    Filed: February 5, 2009
    Publication date: July 2, 2009
    Inventors: Dongcheng Dai, John H. Musser, Edwin S. Lennox
  • Publication number: 20090131498
    Abstract: This invention provides a method of synthesizing enantioenriched merrilactone A and enantiopure merrilactone A, as well as an improved method of synthesizing racemic merrilactone.
    Type: Application
    Filed: January 18, 2006
    Publication date: May 21, 2009
    Inventors: Samuel J. Danishefsky, Zhaoyang Meng, Vladimir Birman
  • Publication number: 20080306145
    Abstract: The present invention relates to synthesis of C11 natural ginkgolide derivatives and C11 f-seco-gingkolide derivatives from the corresponding lactols which are selectively obtained using NaBH4.
    Type: Application
    Filed: November 23, 2005
    Publication date: December 11, 2008
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Koji Nakanishi, Nina Berova, Katsunori Tanaka
  • Publication number: 20080287530
    Abstract: Disclosed are compounds based on lactone ring modifications of triptolide and hydroxylated triptolide, for use in therapy, such as antiproliferative, anticancer, and immunosuppressive therapy.
    Type: Application
    Filed: March 2, 2005
    Publication date: November 20, 2008
    Inventors: Hongwei Yuan, John H. Musser, Dongcheng Dai
  • Publication number: 20080269509
    Abstract: Disclosed is a method for oxidizing an alcohol in an amide solvent using a mixed reagent containing hydrogen peroxide and a tungsten catalyst.
    Type: Application
    Filed: May 12, 2005
    Publication date: October 30, 2008
    Inventors: Takemasa Hida, Kyozo Kawata, Mikio Kabaki
  • Patent number: 7417069
    Abstract: Compounds having the structure I: are useful for inducing cell death (apoptosis) and in immunosuppression. In structure I, CR1R2 is selected from CHOH, C?O, CHF, CF2 and C(CF3)OH; CR6 and CR13 are selected from CH, COH and CF; CR7R8, CR9R10 and CR11R12 are selected from CH2, CHOH, C?O, CHF and CF2; and CR3R4R5 is selected from CH3, CH2OH, C?O, COOH, CH2F, CHF2 and CF3; such that: at least one of R1-R13 comprises fluorine; no more than two of CR3R4R5, CR6, CR7R8, CR9R10, CR11R12, and CR13 comprises fluorine or oxygen; and, when CR1R2 is CHOH, CR3R4R5 is not CH2F.
    Type: Grant
    Filed: August 23, 2005
    Date of Patent: August 26, 2008
    Assignee: Pharmagenesis, Inc.
    Inventors: Dongcheng Dai, John H. Musser
  • Publication number: 20080108837
    Abstract: The subject invention provides a method for separating a terpene trilactone from Ginkgo biloba plant material or from an extract of Ginkgo biloba comprising a mixture of terpene trilactones, the process comprising the steps of: a) subjecting the Ginkgo biloba plant material or the extract to column chromatography with an appropriate solvent system to produce at least a first fraction containing the terpene trilactone bilobalide, a second fraction eluted after the first fraction containing the terpene trilactones GA and GB, and a third fraction eluted after the second fraction containing at least a preponderance of the terpene trilactones GC and GJ; and b) alkylating the terpene trilactone GB of the second fraction so as to produce a first mixture including terpene trilactone GA and alkylated terpene trilactone GB; or alkylating the terpene trilactone GC of the third fraction so as produce a second mixture including terpene trilactone GJ and alkylated terpene trilactone GC, so as to thereby isolate a terpene t
    Type: Application
    Filed: November 9, 2004
    Publication date: May 8, 2008
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Koji Nakanishi, Stanislav Jaracz, Shahid Malik, Hideki Ishii, Sergei V. Dzyuba
  • Patent number: 7317113
    Abstract: A process for the preparation of 14?-hydroxy-baccatin III-1,14-carbonate useful for the preparation of novel taxane derivatives with antitumor activity.
    Type: Grant
    Filed: July 15, 2002
    Date of Patent: January 8, 2008
    Assignee: Indena S.p.A.
    Inventors: Ezio Bombardelli, Gabriele Fontana, Arturo Battaglia, Andrea Guerrini, Eleonora Baldelli
  • Patent number: 7314942
    Abstract: Alpha-methylenelactone is produced from butyrolactone and valerolactone by the addition of formaldehyde in a supercritical fluid.
    Type: Grant
    Filed: January 7, 2003
    Date of Patent: January 1, 2008
    Assignee: E. I. duPont de Nemours & Co.
    Inventors: Keith W. Hutchenson, Leo E. Manzer
  • Patent number: 7232916
    Abstract: The invention relates to an improved process for the synthesis of 13-(N-Boc-?-isobutylserinyl)-14-?-hydroxybaccatin III-1,14-carbonate (I), wherein carbonation of the 1,14-hydroxy groups of the baccatin skeleton is carried out with bis(trichloromethylcarbonate and the 7-hydroxy group is protected with a trichloroacetyl group.
    Type: Grant
    Filed: May 11, 2006
    Date of Patent: June 19, 2007
    Assignee: Indena S.p.A.
    Inventors: Bruno Gabetta, Daniele Ciceri
  • Patent number: 7145021
    Abstract: The subject invention provides compounds having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R2 is H, OH, a photoactivatable moiety, a fluorescent-moiety, or a radioactive moiety; R3 is H or OH; R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C1–C5) alkyl group, (C2–C5) alkenyl, or a (C2–C5) alkynyl, (C1–C5) alkoxy, (C2–C5) alkenyloxy, or (C2–C5) alkynyloxy, —N3, —COR5, —CONR5R6, —CO2R5, —OCOR5, —NH(OH), —NR5R6, —NHCOR5, —N(OH)COR5, —CH2OR5, —OCH2CO2R5, —CH2SR5, —CH2NR5R6, —SR5, —OSR5, or —NR5SO2R6, where R5 and R6 are each independently hydrogen, substituted or unsubstituted (C1–C5) alkyl, (C2–C5) alkenyl, or (C2–C5) alkynyl, or a cyclo
    Type: Grant
    Filed: March 28, 2003
    Date of Patent: December 5, 2006
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Kristian Stromgaard, Makiko Suehiro, Koji Nakanishi, Stine B. Vogensen
  • Patent number: 7098348
    Abstract: Compounds having the structure I: are useful for inducing cell death (apoptosis) and in immunosuppression. In structure I, R1 is H or R, R being selected from lower alkyl, alkenyl, alkynyl, and allenyl, or, R1 together with R2?O (oxo); R2?OH, or, R1 and R2 together=O (oxo); CR3R5 and CR4R6 are selected from CH2, CHOH and CROH; at least one of R1, R5 and R6 is R; and at least one of CR3R5 and CR4R6 is CH2.
    Type: Grant
    Filed: January 27, 2006
    Date of Patent: August 29, 2006
    Assignee: Pharmagenesis, Inc.
    Inventors: Dongcheng Dai, John H. Musser
  • Patent number: 7078432
    Abstract: A process for the preparation of 14?-hydroxy-baccatin III-1,14-carbonate useful for the preparation of novel taxane derivatives with antitumor activity.
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: July 18, 2006
    Assignee: Indena S.p.A.
    Inventors: Ezio Bombardelli, Gabriele Fontana, Maria Luisa Gelmi, Donato Pocar
  • Patent number: 7041838
    Abstract: A (meth)acrylate represented by the following formula (1): wherein each of R1, R2, R3 and R4 represents a hydrogen atom, a methyl group or an ethyl group; either one of X1 or X2 represents a (meth)acryloyloxy group and the other represents a hydrogen atom; both A1 and A2 represent hydrogen atoms, or A1 and A2 form —O—, —CH2— or —CH2CH2—, which can be produced by first producing a lactone by reducing an addition product obtained by the Diels-Alder reaction between 1,3-diene and maleic anhydride, and then hydrating the lactone to produce an alcohol followed by (meth)acrylation of the alcohol; a polymer produced by (co)polymerizing a monomer composition comprising the (meth)acrylate of the present invention is excellent in transparency, dry etching resistance, and solubility in organic solvents, and so it is preferably used as a resin for a chemically amplified resist composition.
    Type: Grant
    Filed: December 5, 2001
    Date of Patent: May 9, 2006
    Assignee: Mitsubishi Rayon Co., Ltd.
    Inventors: Yoshihiro Kamon, Tadayuki Fujiwara, Hideaki Kuwano, Hikaru Momose, Atsushi Koizumi
  • Patent number: 7037995
    Abstract: Novel tertiary (meth)acrylate compounds having a lactone structure are polymerizable into polymers having improved transparency, especially at the exposure wavelength of an excimer laser and dry etching resistance. Resist compositions comprising the polymers are sensitive to high-energy radiation, have a high resolution, and lend themselves to micropatterning with electron beams or deep-UV rays.
    Type: Grant
    Filed: September 29, 2003
    Date of Patent: May 2, 2006
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Takeru Watanabe, Takeshi Kinsho, Koji Hasegawa
  • Patent number: 6943259
    Abstract: Compounds having the structure I: are useful for inducing cell death (apoptosis) and in immunosuppression. In structure I, CR1R2 is selected from CHOH, C?O, CHF, CF2 and C(CF3)OH; CR6 and CR13 are selected from CH, COH and CF; CR7R8, CR9R10 and CR11R12 are selected from CH2, CHOH, C?O, CHF and CF2; and CR3R4R5 is selected from CH3, CH2OH, C?O, COOH, CH2F, CHF2 and CF3; such that: at least one of R1-R13 comprises fluorine; no more than two of CR3R4R5, CR6, CR7R8, CR9R10, CR11R12, and CR13 comprises fluorine or oxygen; and, when CR1R2 is CHOH, CR3R4R5 is not CH2F.
    Type: Grant
    Filed: February 24, 2004
    Date of Patent: September 13, 2005
    Assignee: Pharmagenesis, Inc.
    Inventors: Dongcheng Dai, John H. Musser
  • Patent number: 6933395
    Abstract: Process for the production of drospirenone (6?,7?; 15?,16?-dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, DRSP) (1) and 7?-(3-hydroxy-1-propyl)-6?,7?; 15?,16?-dimethylene-5?-androstane-3?,5,17?-triol (ZK 92836) and 6?,7?; 15?,16?-dimethylene-5?-hydroxy-3-oxo-17?-androstane-21,17-carbolactone (ZK 90965) as intermediate products of the process.
    Type: Grant
    Filed: August 18, 2000
    Date of Patent: August 23, 2005
    Assignee: Schering AG
    Inventors: Jörg-Thorsten Mohr, Klaus Nickisch
  • Patent number: 6887869
    Abstract: The invention concerns novel mikanolide derivatives, their preparation method and their therapeutic uses, in particular as anti-cancer and anti-viral agents.
    Type: Grant
    Filed: January 11, 2002
    Date of Patent: May 3, 2005
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Olivier Lavergne, Christophe Lanco, Grégoire Prevost, Beng Poon Teng
  • Patent number: 6844451
    Abstract: A method of isolating terpene trilactones from Ginkgo biloba plant material or extract comprising the steps of suspending the plant material or extract in either water or an aqueous solution of an oxidation reagent; extracting the terpene trilactones using an acceptable extraction agent; separating the organic layer from the aqueous layer; washing the organic layer with an acceptable aqueous salt or hydroxide solution, which may be an alkaline solution; and drying the organic layer to form a dried extract containing terpene trilactones. Further purification by treatment with or filtration over activated charcoal, by treatment with or filtration over alumina and by recrystallization with an acceptable solvent or solvent mixture leads to extracts with a content of terpene trilactones higher than 50%. Unwanted levels of ginkgolic acids are reduced to acceptable levels by reversed phase chromatography.
    Type: Grant
    Filed: July 7, 2003
    Date of Patent: January 18, 2005
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Dirk Lichtblau, Nina Berova, John Berger, Koji Nakanishi
  • Patent number: 6828347
    Abstract: This invention provides various biquinone and trimeric quinone derivatives. The invention also provides a method for synthesis of a multi-quinone compound including reacting a hydroxyquinone anion with a first quinone possessing a first directing group at a C-2 of the first quinone and a second directing group at a C-3 of the first quinone and obtaining a biquinone having one of the first and second directing groups at a C-3 of a first quinone monomer and a hydroxyl group at a C-3′ of a second quinone monomer. The biquinone can be further reacted to obtain various biquinone derivatives or with a second hydroxyquinone anion to obtain trimeric quinone derivatives, including trimeric naphthoquinone derivatives. The biquinones and trimeric quinones of this invention demonstrate antiviral activity and can be used to treat viral infections, particularly HIV infections.
    Type: Grant
    Filed: November 6, 2002
    Date of Patent: December 7, 2004
    Assignee: Illinois Institute of Technology
    Inventors: Kenneth William Stagliano, Ashkan Emadi
  • Patent number: 6808724
    Abstract: The present invention relates to a novel compound isolated from Artemisia Sylvatica, expressed by the formula 1, a method of isolation, and its use thereof, and more particularly to a novel compound isolated from Artemisia Sylvatica, a method of isolation, and its use in inhibiting farnesyl transferase activity, which is essential for activating Ras oncogene, and repressing cancer cell growth.
    Type: Grant
    Filed: January 28, 2003
    Date of Patent: October 26, 2004
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Byoung-Mog Kwon, Kwang-Hee Son, Dong-Choi Han, Jong-Han Kim, Hyun-Mi Kang, Sun Bok Jeon
  • Publication number: 20040198808
    Abstract: Compounds having the structure I: 1
    Type: Application
    Filed: February 23, 2004
    Publication date: October 7, 2004
    Inventors: Dongcheng Dai, John H. Musser
  • Publication number: 20040152767
    Abstract: Compounds having the structure I: 1
    Type: Application
    Filed: December 16, 2003
    Publication date: August 5, 2004
    Inventors: Dongcheng Dai, John H. Musser
  • Patent number: 6759065
    Abstract: A compound is extracted from vegetable material, wherein the vegetable material is reduced and treated with a solvent. According to the invention, the vegetable material is frozen using a liquid nitrogen and in frozen condition reduced in size. According to two important embodiments, the vegetable material comes from the ginkgo tree, in particular fresh leaves, and water is used as a solvent. The invention also relates to a pharmaceutical preparation and a cosmetic preparation comprising as active component a compound obtained by the method according to the invention.
    Type: Grant
    Filed: February 15, 2001
    Date of Patent: July 6, 2004
    Assignee: XenoBiosis
    Inventor: Henri M. Ruijten
  • Patent number: 6737534
    Abstract: A process for the preparation of the compound 13-(N-Boc-&bgr;-isobutylisoserinyl)-14&bgr;-hydroxybaccatine III 1,14-carbonate.
    Type: Grant
    Filed: May 27, 2003
    Date of Patent: May 18, 2004
    Assignee: Indena S.p.A.
    Inventors: Alessandro Pontiroli, Ezio Bombardelli
  • Publication number: 20040044068
    Abstract: The present invention relates to a novel compound isolated from Artemisia Sylvatica, expressed by the formula 1, a method of isolation, and its use thereof, and more particularly to a novel compound isolated from Artemisia Sylvatica, a method of isolation, and its use in inhibiting farnesyl transferase activity, which is essential for activating Ras oncogene, and repressing cancer cell growth.
    Type: Application
    Filed: January 28, 2003
    Publication date: March 4, 2004
    Inventors: Byoung-Mog Kwon, Kwang-Hee Son, Dong-Choi Han, Jong-Han Kim, Hyun-Mi Kang, Sun Bok Jeon
  • Patent number: 6693091
    Abstract: A compound having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; wherein R2 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; wherein R3 is H or OH; wherein R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety. Optically pure enantiomers and salts of the compound are also described. Also, the synthesis of the compound, and uses of the compound, such as in a method for detecting the localization of, or identifying, receptors, enzymes or other targets, whether in a cell or in a subject.
    Type: Grant
    Filed: March 29, 2002
    Date of Patent: February 17, 2004
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Kristian Stromgaard, Makiko Suehiro, Koji Nakanishi