Tetracyclo Ring System Having The Lactone Ring As One Of The Cyclos Patents (Class 549/298)
  • Publication number: 20150119388
    Abstract: An ester of ArOH according to the formula R—X—CO—OAr, wherein ArOH is a pharmaceutically active compound selected from the group consisting of SN-38, PI-103, etoposide and fenretinide, wherein a) R is a residue of cholesterol, sitosterol, SN-38, PI-103, etoposide or fenretinide and X is O—CO-L, wherein L is either a direct bond or a linking group including a branched or unbranched hydrocarbyl moiety that may optionally include in-chain or pendant heteroatom substituents and/or cyclic moieties; b) R—X—CO-0 is an all-trans retinoate radical or the 9-cis or 13-cis isomer thereof; or c) R—X— is a branched or unbranched, saturated or unsaturated hydrocarbyl moiety comprising at least 5 carbon atoms and optionally including at least one in-chain or pendant heteroatom substituent and/or cyclic moiety.
    Type: Application
    Filed: June 14, 2013
    Publication date: April 30, 2015
    Applicant: THE CHILDREN'S HOSPITAL PHILADELPHIA
    Inventors: Ivan Alferiev, Michael Chorny, Garrett M. Brodeur, Robert J. Levy
  • Patent number: 8987475
    Abstract: The invention relates to a one-pot reaction for the preparation of a compound of Formula (I). The compound of Formula (I) may be further transformed into picropodophyllin and derivatives thereof.
    Type: Grant
    Filed: August 30, 2011
    Date of Patent: March 24, 2015
    Assignee: Alexar AB
    Inventors: Magnus Axelsson, Ulf Bremberg, Auri Linden, Fredrik Von Kieseritzky
  • Publication number: 20150031759
    Abstract: Compounds, compositions, methods of making, and methods of using analogues of (?)-picropodophyllin, as well as a transgenic animal model and its use for identifying anticancer agents.
    Type: Application
    Filed: July 10, 2014
    Publication date: January 29, 2015
    Inventors: David B. Berkowitz, Sylvain Broussy
  • Publication number: 20140088186
    Abstract: A composition for preventing and/or treating dementia and ameliorating memory impairment and/or improving memory, comprising one or more arylnaphthalene lignan derivatives, such as Justicidin A, 5-methoxyjusticidin A, Chinensinaphthol, and a pharmaceutically-acceptable salt thereof, as active ingredient.
    Type: Application
    Filed: September 25, 2013
    Publication date: March 27, 2014
    Applicants: The Council for Scientific and Industrial Research, KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Hyun Ok Yang, Sung-Kwon Chung, Hak Cheol Kwon, Jin Wook Cha, Young-Joo Kim, Gerda Fouche, Rudzani Nthambeleni, Dashnie Naidoo, Jeremiah Senabe, Vinesh Jaichand Maharaj, Eric Khorombi, Jungyeob Ham, Joon Ki Kim
  • Patent number: 8673969
    Abstract: The present invention provides compounds of general formula (3) as useful potential antitumour agents against human cancer cell lines. The present invention further provides a process for the synthesis of 4?-acrylamidopodophyllotoxin congeners of general formula (3), wherein R and R1 are an aryl group and R is selected from 3,4,5-trimethoxyphenyl or 2-methoxy phenyl and R1 is selected from the group consisting of 4-hydroxy-3-methoxyphenyl, 3-hydroxy-4-methoxyphenyl, 4-fluoro-3-methoxyphenyl, 3-fluoro-4-methoxyphenyl, 2-fluoro-5-methoxyphenyl, 2-fluoro-4-methoxyphenyl, 4-hydroxy-3-nitrophenyl, 4-methoxy-3-nitrophenyl, 4-nitrophenyl, 3-nitrophenyl, 2-nitro phenyl, 4-methoxyphenyl, 3-methoxyphenyl and 4-hydroxyphenyl.
    Type: Grant
    Filed: March 9, 2011
    Date of Patent: March 18, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Kamal Ahmed, Suresh Paidakula, Ashwini Kumar Banala, Adla Malla Reddy, Papagiri Venkat Reddy
  • Patent number: 8664409
    Abstract: The present invention relates to a new process for the preparation of (poly)aminoalkylaminoacetamide derivatives of epipodophyllotoxin and salts thereof, characterized in that it comprises a step of peptide coupling of 4-amino-4?-demethylepipodophyllotoxin with an amine-containing reactant having protecting groups.
    Type: Grant
    Filed: September 23, 2008
    Date of Patent: March 4, 2014
    Assignee: Pierre Fabre Medicament
    Inventors: Yves Guminski, Martial Grousseaud, Thierry Imbert
  • Patent number: 8653283
    Abstract: The present disclosure relates generally to compositions and methods for treating cancer. In some aspects, novel spirohexenolides and methods of using and producing them are described.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: February 18, 2014
    Assignee: The Regents of The University of California
    Inventors: Michael D. Burkart, James J. La Clair, MinJin Kang, Brian D. Jones, Alexander L. Mandel, Wei-Luen Yu, Justin C. Hammons
  • 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
  • Publication number: 20130317099
    Abstract: The invention relates to novel polymorphs of picropodophyllin, methods for preparing said polymorphs and pharmaceutical compositions comprising said polymorphs, as well as the use of said polymorphs in therapy such as cancer therapy.
    Type: Application
    Filed: October 7, 2011
    Publication date: November 28, 2013
    Applicant: Axelar AB
    Inventors: Mikael Bisrat, Magnus Brisander
  • Publication number: 20130245285
    Abstract: The invention relates to a one-pot reaction for the preparation of a compound of Formula (I). The compound of Formula (I) may be further transformed into picropodophyllin and derivatives thereof.
    Type: Application
    Filed: August 30, 2011
    Publication date: September 19, 2013
    Applicant: AXELAR AB
    Inventors: Magnus Axelsson, Ulf Bremberg, Auri Linden, Fredrik Von Kieseritzky
  • Publication number: 20130225672
    Abstract: The present invention provides compounds of general formula (3) as useful potential antitumour agents against human cancer cell lines. The present invention further provides a process for the synthesis of 4?-acrylamidopodophyllotoxin congeners of general formula (3), wherein R and R1 are an aryl group and R is selected from 3,4,5-trimethoxyphenyl or 2-methoxy phenyl and R1 is selected from the group consisting of 4-hydroxy-3-methoxyphenyl, 3-hydroxy-4-methoxyphenyl, 4-fluoro-3-methoxyphenyl, 3-fluoro-4-methoxyphenyl, 2-fluoro-5-methoxyphenyl, 2-fluoro-4-methoxyphenyl, 4-hydroxy-3-nitrophenyl, 4-methoxy-3-nitrophenyl, 4-nitrophenyl, 3-nitrophenyl, 2-nitro phenyl, 4-methoxyphenyl, 3-methoxyphenyl and 4-hydroxyphenyl.
    Type: Application
    Filed: March 9, 2011
    Publication date: August 29, 2013
    Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH
    Inventors: Kamal Ahmed, Suresh Paidakula, Ashwini Kumar Banala, Adla Malla Reddy, Papagiri Venkat Reddy
  • Patent number: 8492567
    Abstract: The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamide, or alkyl-urea or alkyl-sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent.
    Type: Grant
    Filed: July 17, 2012
    Date of Patent: July 23, 2013
    Assignee: Pierre Fabre Medicament
    Inventors: Thierry Imbert, Yves Guminski, Jean-Marc Barret, Anna Kruczynski
  • Publication number: 20130109749
    Abstract: The present invention provides a compound of formula (I)
    Type: Application
    Filed: April 14, 2011
    Publication date: May 2, 2013
    Applicants: NANKAI UNIVERSITY, ACCENDATECH
    Inventors: Yue Chen, Quan Zhang, Yaxin Lu, Jiadai Zhai, Yahui Ding, Jing Long, Hongxia Fan, Haoliang Zhang, Miao Wang, Weiwei Ma
  • Patent number: 8389747
    Abstract: The invention refers to the use of specific cyclolignans, wherein the carbon atoms in positions 9 and 9? have cis configuration, for inhibition of the insulin-like growth factor-1 receptor. Said compounds can be used for treatment of IGF-1R dependent diseases, such as cancer, psoriasis, artherosclerosis and acromegaly. A preferred compound is picropodophyllin.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: March 5, 2013
    Assignee: Axelar AB
    Inventors: Olle Larsson, Magnus Axelson
  • Patent number: 8362170
    Abstract: Provided is a polymerizable compound represented by the following general formula (ca-1) or (cb-1): wherein the variables in the formulae are defined in the specification.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: January 29, 2013
    Assignee: FUJIFILM Corporation
    Inventors: Shuji Hirano, Kaoru Iwato, Hiroshi Saegusa, Yusuke Iizuka
  • Patent number: 8354547
    Abstract: The present invention provides novel ?-amino podophyllotoxin congeners of general formula (A); R=CH3, or H; R1=(a) or (b) or (c) or (d) or (e) or (f). The present invention also provides a process for the preparation of 4?-amino podophyllotoxin congeners useful as antitumour agents.
    Type: Grant
    Filed: March 24, 2009
    Date of Patent: January 15, 2013
    Assignee: Council of Scientific & Industrial Research
    Inventors: Kamal Ahmed, Ashwini Kumar Banala, Suresh Paidakula
  • Patent number: 8288567
    Abstract: The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamidc, or alkyl-urea or alkyl-sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent. Formula (1) wherein: —R represents hydrogen or C1-4alkyl, —A represents CO(CH2)n or CONH(CH2)n where n=2, 3, 4, or 5, —R1 and R2 are as described herein.
    Type: Grant
    Filed: August 19, 2009
    Date of Patent: October 16, 2012
    Assignee: Pierre Fabre Medicament
    Inventors: Thierry Imbert, Yves Guminski, Jean-Marc Barret, Anna Kruczynski
  • Patent number: 8252877
    Abstract: Provided is a polymerizable compound represented by the following general formula (ca-1) or (cb-1): wherein the variables in the formulae are defined in the specification.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: August 28, 2012
    Assignee: FUJIFILM Corporation
    Inventors: Shuji Hirano, Kaoru Iwato, Hiroshi Saegusa, Yusuke Iizuka
  • Patent number: 8158809
    Abstract: 4-O esters of podophyllotoxin and 4?-demethylepipodophyllotoxin are provided. The compounds are 4-O esters of an alkanoic acid or substituted alkanoic acid and podophyllotoxin and 4?-demethylepipodophyllotoxin. The compounds are useful for treating cancer.
    Type: Grant
    Filed: August 3, 2009
    Date of Patent: April 17, 2012
    Assignees: Sutter West Bay Hospitals, Catholic Healthcare West
    Inventor: Li-Xi Yang
  • Publication number: 20120083527
    Abstract: The present disclosure relates generally to compositions and methods for treating cancer. In some aspects, novel spirohexenolides and methods of using and producing them are described.
    Type: Application
    Filed: April 16, 2010
    Publication date: April 5, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Michael D. Burkart, James J. La Clair, Minjin Kang, Brian D. Jones, Alexander L. Mandel, Wei-Luen Yu, Justin C. Hammons
  • Patent number: 8148552
    Abstract: The present invention describes a new process for the preparation of (poly)aminoalkylaminoacetamide compounds of epipodophyllotoxin useful for their applications in therapeutics as anticancer agents. This process comprises a step of condensation of a primary-amine-containing reactant, whose amine functions are not protected, with ?-chloroacetamido-4?-epipodophyllotoxin in a polar aprotic organic solvent.
    Type: Grant
    Filed: September 23, 2008
    Date of Patent: April 3, 2012
    Assignee: Pierre Fabre Medicament
    Inventors: Yves Guminski, Martial Grousseaud, Thierry Imbert
  • Publication number: 20120022273
    Abstract: The present invention relates to a new process for the preparation of (poly)aminoalkylaminoacetamide derivatives of epipodophyllotoxin and salts thereof, characterised in that it comprises a step of peptide coupling of 4-amino-4?-demethylepipodophyllotoxin with an amine-containing reactant having protecting groups.
    Type: Application
    Filed: September 23, 2008
    Publication date: January 26, 2012
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Yves Guminski, Martial Grousseaud, Thierry Imbert
  • Publication number: 20120009521
    Abstract: A resist composition including: a base component (A) which exhibits changed solubility in an alkali developing solution under action of acid; and an acid-generator component (B) which generates acid upon exposure, wherein said acid-generator component (B) comprises an acid generator (B1) including a compound represented by general formula (b1-11) shown below: wherein R7? to R9? each independently represent an aryl group or an alkyl group, wherein two of R7? to R9? may be bonded to each other to form a ring with the sulfur atom, and at least one of R7? to R9? represents a substituted aryl group having a group represented by general formula (I) shown below as a substituent; X? represents an anion; and Rf represents a fluorinated alkyl group.
    Type: Application
    Filed: September 15, 2011
    Publication date: January 12, 2012
    Applicant: Tokyo Ohka Kogyo Co., Ltd.
    Inventors: Akiya Kawaue, Yoshiyuki Utsumi, Takehiro Seshimo, Tsuyoshi Nakamura, Naoto Motoike, Hiroaki Shimizu, Kensuke Matsuzawa, Hideo Hada
  • Publication number: 20110213165
    Abstract: The present invention provides novel ?-amino podophyllotoxin congeners of general formula (A); R?CH3, or H; R1=(a) or (b) or (c) or (d) or (e) or (f). The present invention also provides a process for the preparation of 4?-amino podophyllotoxin congeners useful as antitumour agents.
    Type: Application
    Filed: March 24, 2009
    Publication date: September 1, 2011
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Kamal Ahmed, Ashwini Kumar Banala, Suresh Paidakula
  • Publication number: 20110172257
    Abstract: The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamide, or alkyl-urea or alkyl-sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent. Formula (1) wherein: —R represents hydrogen or C1-4alkyl, —A represents CO(CH2)n or CONH(CH2)n where n=2, 3, 4, or 5, —R1 and R2 are as described herein.
    Type: Application
    Filed: August 19, 2009
    Publication date: July 14, 2011
    Inventors: Thierry Imbert, Yves Guminski, Jean-Marc Barret, Anna Kruczynski
  • Publication number: 20110021791
    Abstract: The invention relates to a method for synthesizing 4?-amino-4?-demethyl-4-desoxypodophyllotoxin of formula (1), characterized by comprising the following successive steps: a) reacting, in a pure weak acid or in a mixture consisting of acid, water and of organic solvent, without another solvent, at a temperature higher than the ambient temperature, thiourea with 4?-halogenoacetamido-4?-demethyl-4-desoxypodophyllotoxin, and; b) recovering the 4?-amino-4?-demethyl-4-desoxypodophyllotoxin.
    Type: Application
    Filed: September 30, 2010
    Publication date: January 27, 2011
    Inventors: Yves Guminski, Martial Grousseaud, Thierry Imbert
  • Patent number: 7846926
    Abstract: The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.
    Type: Grant
    Filed: April 14, 2005
    Date of Patent: December 7, 2010
    Assignee: Pierre Fabre Medicament
    Inventors: Thierry Imbert, Yves Guminski, Jean-Marc Barret, Anna Kruczynski
  • 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
  • Publication number: 20100285141
    Abstract: A method of increasing an activity of a podophyllotoxin or a derivative thereof is disclosed. The method comprises contacting the podophyllotoxin or the derivative with a liquid composition having a liquid and nanostructures, each of the nanostructures comprising a core material of the nanometric size surrounded by an envelope of ordered fluid molecules, the core material and the envelope of ordered fluid molecules being in a steady physical state, thereby increasing the activity of the podophyllotoxin or the derivative. Pharmaceutical compositions comprising same and uses thereof are also disclosed.
    Type: Application
    Filed: December 28, 2008
    Publication date: November 11, 2010
    Inventor: Eran Gabbai
  • Publication number: 20100280263
    Abstract: The present invention describes a new process for the preparation of (poly)aminoalkylaminoacetamide compounds of epipodophyllotoxin useful for their applications in therapeutics as anticancer agents. This process comprises a step of condensation of a primary-amine-containing reactant, whose amine functions are not protected, with ?-chloroacetamido-4?-epipodophyllotoxin in a polar aprotic organic solvent.
    Type: Application
    Filed: September 23, 2008
    Publication date: November 4, 2010
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Yves Guminski, Martial Grousseaud, Thierry Imbert
  • Publication number: 20100168160
    Abstract: Genipin derivatives and pharmaceutical compositions thereof that inhibit the activity of uncoupling protein-2 (UCP2) and are useful in treating deficient first-phase insulin secretion, non-insulin dependent diabetes mellitus, and ischemia in a mammal are disclosed.
    Type: Application
    Filed: November 19, 2009
    Publication date: July 1, 2010
    Applicant: Beth Israel Deaconess Medical Center , Inc. And Trustees of Boston University
    Inventors: Chen-Yu Zhang, Bradford B. Lowell, John A. Porco, JR., Ruichao Shen, Cheng T. Lin, Stefan Krauss
  • Publication number: 20100143296
    Abstract: The present invention relates to new podophyllotoxin inhibitors of topoisomerase II, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: December 10, 2009
    Publication date: June 10, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventor: Thomas G. Gant
  • Patent number: 7671088
    Abstract: Etoposide analogs with improved water-solubility such as 4?-O-Demethyl-4?-(N?,N?-dimethyl-glycyl)-4?-(4?-nitroanilino)-4-desoxy-podophyllotoxin (8) and 4?-O-Demethyl-4?-(N?,N?-dimethyl-glycyl)-4?-(4?-fluoroanilino)-4-desoxy-podophyllotoxin (9) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.
    Type: Grant
    Filed: January 3, 2007
    Date of Patent: March 2, 2010
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Kuo-Hsiung Lee, Zhiyan Xiao, Kenneth F. Bastow
  • Patent number: 7662851
    Abstract: The invention refers to the use of specific cyclolignans, wherein the carbon atoms in positions 9 and 9? have cis configuration, for inhibition of the insulin-like growth factor-1 receptor. Said compounds can be used for treatment of IGF-1R dependent diseases, such as cancer, psoriasis, atherosclerosis and acromegaly. A preferred compound is picropodophyllin.
    Type: Grant
    Filed: January 29, 2008
    Date of Patent: February 16, 2010
    Assignee: Axelar AB
    Inventors: Olle Larsson, Magnus Axelson
  • Patent number: 7629381
    Abstract: The invention refers to the use of specific cyclolignans, wherein the carbon atoms in positions 9 and 9? have cis configuration, for inhibition of the insulin-like growth factor-1 receptor. Said compounds can be used for treatment of IGF-1R dependent diseases, such as cancer, psoriasis, artherosclerosis and acromegaly. A preferred compound is picropodophyllin.
    Type: Grant
    Filed: January 29, 2008
    Date of Patent: December 8, 2009
    Assignee: Axelar AB
    Inventors: Olle Larsson, Magnus Axelson
  • Publication number: 20090298870
    Abstract: 4-O esters of podophyllotoxin and 4?-demethylepipodophyllotoxin are provided. The compounds are 4-O esters of an alkanoic acid or substituted alkanoic acid and podophyllotoxin and 4?-demethylepipodophyllotoxin. The compounds are useful for treating cancer.
    Type: Application
    Filed: August 3, 2009
    Publication date: December 3, 2009
    Inventor: Li-Xi Yang
  • Patent number: 7582778
    Abstract: The invention relates to podophyllotoxins, uses thereof and methods of their production.
    Type: Grant
    Filed: December 3, 2002
    Date of Patent: September 1, 2009
    Assignee: Universitatsklinikum Charite der Humboldt-Universitat zu
    Inventors: Gerhard Gaedicke, Holger N. Lode, Wolfgang Wrasidlo
  • Publication number: 20090170843
    Abstract: The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.
    Type: Application
    Filed: April 14, 2005
    Publication date: July 2, 2009
    Inventors: Thierry Imbert, Yves Guminski, Jean-Marc Barret, Anna Kruczynski
  • 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
  • Patent number: 7459555
    Abstract: The present invention relates to photochromic 2H-naphtho[1,2-b]pyrans as well as their use in synthetic resins of all types, especially for ophthalmic purposes. In particular, the present invention relates to photochromic naphthopyran compounds, for which a further ring system is bonded to the f side of the naphthopyran. The inventive photochromic dyes generally have the general formula (I) wherein n, R1, R2, R3, X, B and B? are defined as in claim 1. The inventive compounds are distinguished by good darkening and decolorizing properties and a very good service life.
    Type: Grant
    Filed: December 13, 2001
    Date of Patent: December 2, 2008
    Assignee: Rodenstock GmbH
    Inventors: Manfred Melzig, Claudia Mann, Udo Weigand
  • Publication number: 20080207747
    Abstract: The present invention provides lipase inhibitors containing flavan-3-ol monomers or acylates thereof derived from teas as well as foods and beverages and medicines containing said inhibitors. More specifically, the present invention provides lipase inhibitors containing at least one of flavan-3-ol monomers represented by the formula: wherein R1 and R3 independently represent H or OH, R2 represents H, R4 represents H, G, 3MeG or p-cou, R5 represents H or G, R4? and R5? independently represent H or G, R4? represents H or G, and G, 3MeG and p-cou respectively represent the groups of the formulae: or acylates thereof; as well as foods and beverages and medicines containing said lipase inhibitors.
    Type: Application
    Filed: July 5, 2005
    Publication date: August 28, 2008
    Applicant: SUNTORY LIMITED
    Inventors: Masaaki Nakai, Yuko Fukui, Sumio Asami, Fumio Hashimoto
  • Patent number: 7348358
    Abstract: The invention refers to the use of specific cyclolignans, wherein the carbon atoms in positions 9 and 9? have cis configuration, for inhibition of the insulin-like growth factor-1 receptor. Said compounds can be used for treatment of IGF-1R dependent diseases, such as cancer, psoriasis, artherosclerosis and acromegaly. A preferred compound is picropodophyllin.
    Type: Grant
    Filed: June 19, 2002
    Date of Patent: March 25, 2008
    Assignee: Axelar AB
    Inventors: Olle Larsson, Magnus Axelson
  • Patent number: 7342114
    Abstract: 4-O esters of podophyllotoxin and 4?-demethylepipodophyllotoxin are provided. The compounds are 4-O esters of an alkanoic acid or substituted alkanoic acid and podophyllotoxin and 4?-demethylepipodophyllotoxin. The compounds are useful for treating cancer.
    Type: Grant
    Filed: July 1, 2003
    Date of Patent: March 11, 2008
    Assignees: California Pacific Medical Center, Catholic Healthcare West, DBA St. Mary's Medical Center
    Inventor: Li-Xi Yang
  • Patent number: 7192682
    Abstract: There is provided a chemically-amplified resist composition having high transparency to light having a wavelength of 220 nanometers or smaller, excellent resistance to etching, and excellent adhesion to a substrate. The chemically-amplified resist composition is prepared through the use of at least one of a repeated structural unit having a bridged alicyclic ?-lactone structure defined in the general formula (III), a repeated structural unit having a bridged alicyclic ?-lactone structure defined in the general formula (IV), and a repeated structural unit having a bridged alicyclic ?-lactone structure defined in the general formula (V).
    Type: Grant
    Filed: June 27, 2003
    Date of Patent: March 20, 2007
    Assignee: NEC Corporation
    Inventors: Katsumi Maeda, Kaichiro Nakano
  • Patent number: 7186495
    Abstract: There are here disclosed a photoresist material for lithography using a light of 220 nm or less which comprises at least a polymer represented by the following formula (2) and a photo-acid generator for generating an acid by exposure: wherein R1, R2, R3 and R5 are each a hydrogen atom or a methyl group; R4 is an acid-labile group, an alicyclic hydrocarbon group having 7 to 13 carbon atoms, which has an acid labile group, an alicyclic hydrocarbon group having 7 to 13 carbon atoms, which has a carboxyl group, or a hydrocarbon group having 3 to 13 carbon atoms, which has an epoxy group; R6 is a hydrogen atom, a hydrocarbon group having 1 to 12 carbon atoms, or an alicyclic hydrocarbon group having 7 to 13 carbon atoms, which has a carboxyl group; x, y and z are optional values which meet x+y+z=1, 0<x?1, 0?y<1 and 0?z<1; and a weight-average molecular weight of the polymer is in the range of 2000 to 200000, and a resin having a (meth)acrylate unit of an alicyclic lactone structure represented by the
    Type: Grant
    Filed: December 29, 2000
    Date of Patent: March 6, 2007
    Assignee: NEC Corporation
    Inventors: Katsumi Maeda, Shigeyuki Iwasa, Kaichiro Nakano, Etsuo Hasegawa
  • Patent number: 7176236
    Abstract: Etoposide analogs with improved water-solubility such as 4?-O-Demethyl-4?-(N?,N?-dimethyl-glycyl)-4?-(4?-nitroanilino)-4-desoxy-podophyllotoxin (8) and 4?-O-Demethyl-4?-(N?,N?-dimethyl-glycyl)-4?-(4?-fluoroanilino)-4-desoxy-podophyllotoxin (9) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.
    Type: Grant
    Filed: November 13, 2003
    Date of Patent: February 13, 2007
    Assignee: University of North Carolina at Chapel Hill
    Inventors: Kuo-Hsiung Lee, Zhiyan Xiao, Kenneth F. Bastow
  • 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: 7094805
    Abstract: This invention provides a total synthesis of Merrillactone and Merrilactone analogues for use as neurotrophic agents in the treatment of neurodegenerative diseases. The invention also provides intermediates for use in the synthesis of Merrilactone and its analogues.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: August 22, 2006
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Samuel J. Danishefsky, Vladimir B. Birman
  • Patent number: 7087641
    Abstract: The present invention provides a new class of compounds 4?-1?-[{2?-benzoyl substituted}anilino] podophyllotoxin exhibiting anti cancer activity and a process for preparing the same.
    Type: Grant
    Filed: March 28, 2002
    Date of Patent: August 8, 2006
    Assignee: Council of Scientific & Industrial Research
    Inventors: Ahmed Kamal, Peram Surakattula Murali Mohan Reddy