Tetracyclo Ring System Having The Lactone Ring As One Of The Cyclos Patents (Class 549/298)
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Patent number: 11384095Abstract: The present invention is directed to the preparation of phthalic anhydride compounds and the intermediate phthalide compounds. In particular, the invention is directed to an improved bio-based route from furanic compounds to phthalic anhydride compounds by reacting furfuryl alcohol (i.e. 2-hydroxymethylfuran) or an analogue thereof having a nucleophilic atom on the 2-methyl, with a dienophile comprising an ?,?-unsaturated carbonyl comprising an ??-leaving group. The inventions further involved preparation of phthalic anhydride compounds, phthalic acid compounds and reduction products of the intermediate phthalide compounds.Type: GrantFiled: August 29, 2019Date of Patent: July 12, 2022Assignee: Nederlandse Organisatie Voor Toegepast-Natuurwetenschappelijk Onderzoek TNOInventors: Marc Crockatt, Johan Urbanus, Pieter Cornelis Antonius Bruijnincx, Christopher Stuart Lancefield, Bart Fölker
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Publication number: 20150119388Abstract: 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: ApplicationFiled: June 14, 2013Publication date: April 30, 2015Applicant: THE CHILDREN'S HOSPITAL PHILADELPHIAInventors: Ivan Alferiev, Michael Chorny, Garrett M. Brodeur, Robert J. Levy
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Patent number: 8987475Abstract: 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: GrantFiled: August 30, 2011Date of Patent: March 24, 2015Assignee: Alexar ABInventors: Magnus Axelsson, Ulf Bremberg, Auri Linden, Fredrik Von Kieseritzky
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Publication number: 20150031759Abstract: 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: ApplicationFiled: July 10, 2014Publication date: January 29, 2015Inventors: David B. Berkowitz, Sylvain Broussy
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Publication number: 20140088186Abstract: 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: ApplicationFiled: September 25, 2013Publication date: March 27, 2014Applicants: The Council for Scientific and Industrial Research, KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: 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
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Patent number: 8673969Abstract: 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: GrantFiled: March 9, 2011Date of Patent: March 18, 2014Assignee: Council of Scientific & Industrial ResearchInventors: Kamal Ahmed, Suresh Paidakula, Ashwini Kumar Banala, Adla Malla Reddy, Papagiri Venkat Reddy
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Patent number: 8664409Abstract: 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: GrantFiled: September 23, 2008Date of Patent: March 4, 2014Assignee: Pierre Fabre MedicamentInventors: Yves Guminski, Martial Grousseaud, Thierry Imbert
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Patent number: 8653283Abstract: 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: GrantFiled: April 16, 2010Date of Patent: February 18, 2014Assignee: The Regents of The University of CaliforniaInventors: Michael D. Burkart, James J. La Clair, MinJin Kang, Brian D. Jones, Alexander L. Mandel, Wei-Luen Yu, Justin C. Hammons
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Patent number: 8637623Abstract: 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: GrantFiled: February 3, 2009Date of Patent: January 28, 2014Assignee: Daicel Chemical Industries, Ltd.Inventors: Hiroshi Koyama, Kyuhei Kitao, Akira Eguchi
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Patent number: 8617906Abstract: 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: GrantFiled: October 12, 2005Date of Patent: December 31, 2013Assignee: Pharmagenesis, Inc.Inventors: John M. Fidler, John H. Musser
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Publication number: 20130317099Abstract: 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: ApplicationFiled: October 7, 2011Publication date: November 28, 2013Applicant: Axelar ABInventors: Mikael Bisrat, Magnus Brisander
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Publication number: 20130245285Abstract: 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: ApplicationFiled: August 30, 2011Publication date: September 19, 2013Applicant: AXELAR ABInventors: Magnus Axelsson, Ulf Bremberg, Auri Linden, Fredrik Von Kieseritzky
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Publication number: 20130225672Abstract: 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: ApplicationFiled: March 9, 2011Publication date: August 29, 2013Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Kamal Ahmed, Suresh Paidakula, Ashwini Kumar Banala, Adla Malla Reddy, Papagiri Venkat Reddy
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Patent number: 8492567Abstract: 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: GrantFiled: July 17, 2012Date of Patent: July 23, 2013Assignee: Pierre Fabre MedicamentInventors: Thierry Imbert, Yves Guminski, Jean-Marc Barret, Anna Kruczynski
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Publication number: 20130109749Abstract: The present invention provides a compound of formula (I)Type: ApplicationFiled: April 14, 2011Publication date: May 2, 2013Applicants: NANKAI UNIVERSITY, ACCENDATECHInventors: Yue Chen, Quan Zhang, Yaxin Lu, Jiadai Zhai, Yahui Ding, Jing Long, Hongxia Fan, Haoliang Zhang, Miao Wang, Weiwei Ma
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Patent number: 8389747Abstract: 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: GrantFiled: July 23, 2009Date of Patent: March 5, 2013Assignee: Axelar ABInventors: Olle Larsson, Magnus Axelson
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Patent number: 8362170Abstract: 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: GrantFiled: June 18, 2012Date of Patent: January 29, 2013Assignee: FUJIFILM CorporationInventors: Shuji Hirano, Kaoru Iwato, Hiroshi Saegusa, Yusuke Iizuka
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Patent number: 8354547Abstract: 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: GrantFiled: March 24, 2009Date of Patent: January 15, 2013Assignee: Council of Scientific & Industrial ResearchInventors: Kamal Ahmed, Ashwini Kumar Banala, Suresh Paidakula
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Patent number: 8288567Abstract: 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: GrantFiled: August 19, 2009Date of Patent: October 16, 2012Assignee: Pierre Fabre MedicamentInventors: Thierry Imbert, Yves Guminski, Jean-Marc Barret, Anna Kruczynski
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Patent number: 8252877Abstract: 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: GrantFiled: December 11, 2009Date of Patent: August 28, 2012Assignee: FUJIFILM CorporationInventors: Shuji Hirano, Kaoru Iwato, Hiroshi Saegusa, Yusuke Iizuka
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Patent number: 8158809Abstract: 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: GrantFiled: August 3, 2009Date of Patent: April 17, 2012Assignees: Sutter West Bay Hospitals, Catholic Healthcare WestInventor: Li-Xi Yang
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Publication number: 20120083527Abstract: 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: ApplicationFiled: April 16, 2010Publication date: April 5, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Michael D. Burkart, James J. La Clair, Minjin Kang, Brian D. Jones, Alexander L. Mandel, Wei-Luen Yu, Justin C. Hammons
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Patent number: 8148552Abstract: 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: GrantFiled: September 23, 2008Date of Patent: April 3, 2012Assignee: Pierre Fabre MedicamentInventors: Yves Guminski, Martial Grousseaud, Thierry Imbert
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Publication number: 20120022273Abstract: 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: ApplicationFiled: September 23, 2008Publication date: January 26, 2012Applicant: PIERRE FABRE MEDICAMENTInventors: Yves Guminski, Martial Grousseaud, Thierry Imbert
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Publication number: 20120009521Abstract: 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: ApplicationFiled: September 15, 2011Publication date: January 12, 2012Applicant: Tokyo Ohka Kogyo Co., Ltd.Inventors: Akiya Kawaue, Yoshiyuki Utsumi, Takehiro Seshimo, Tsuyoshi Nakamura, Naoto Motoike, Hiroaki Shimizu, Kensuke Matsuzawa, Hideo Hada
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Publication number: 20110213165Abstract: 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: ApplicationFiled: March 24, 2009Publication date: September 1, 2011Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Kamal Ahmed, Ashwini Kumar Banala, Suresh Paidakula
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Publication number: 20110172257Abstract: 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: ApplicationFiled: August 19, 2009Publication date: July 14, 2011Inventors: Thierry Imbert, Yves Guminski, Jean-Marc Barret, Anna Kruczynski
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Publication number: 20110021791Abstract: 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: ApplicationFiled: September 30, 2010Publication date: January 27, 2011Inventors: Yves Guminski, Martial Grousseaud, Thierry Imbert
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Patent number: 7846926Abstract: 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: GrantFiled: April 14, 2005Date of Patent: December 7, 2010Assignee: Pierre Fabre MedicamentInventors: Thierry Imbert, Yves Guminski, Jean-Marc Barret, Anna Kruczynski
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Patent number: 7847109Abstract: 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: GrantFiled: May 29, 2003Date of Patent: December 7, 2010Assignee: Pharmagenesis, Inc.Inventors: Dongcheng Dai, John H. Musser, Edwin S. Lennox
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Publication number: 20100285141Abstract: 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: ApplicationFiled: December 28, 2008Publication date: November 11, 2010Inventor: Eran Gabbai
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Publication number: 20100280263Abstract: 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: ApplicationFiled: September 23, 2008Publication date: November 4, 2010Applicant: PIERRE FABRE MEDICAMENTInventors: Yves Guminski, Martial Grousseaud, Thierry Imbert
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Publication number: 20100168160Abstract: 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: ApplicationFiled: November 19, 2009Publication date: July 1, 2010Applicant: Beth Israel Deaconess Medical Center , Inc. And Trustees of Boston UniversityInventors: Chen-Yu Zhang, Bradford B. Lowell, John A. Porco, JR., Ruichao Shen, Cheng T. Lin, Stefan Krauss
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Publication number: 20100143296Abstract: The present invention relates to new podophyllotoxin inhibitors of topoisomerase II, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 10, 2009Publication date: June 10, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Patent number: 7671088Abstract: 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: GrantFiled: January 3, 2007Date of Patent: March 2, 2010Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Zhiyan Xiao, Kenneth F. Bastow
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Patent number: 7662851Abstract: 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: GrantFiled: January 29, 2008Date of Patent: February 16, 2010Assignee: Axelar ABInventors: Olle Larsson, Magnus Axelson
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Patent number: 7629381Abstract: 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: GrantFiled: January 29, 2008Date of Patent: December 8, 2009Assignee: Axelar ABInventors: Olle Larsson, Magnus Axelson
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Publication number: 20090298870Abstract: 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: ApplicationFiled: August 3, 2009Publication date: December 3, 2009Inventor: Li-Xi Yang
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Patent number: 7582778Abstract: The invention relates to podophyllotoxins, uses thereof and methods of their production.Type: GrantFiled: December 3, 2002Date of Patent: September 1, 2009Assignee: Universitatsklinikum Charite der Humboldt-Universitat zuInventors: Gerhard Gaedicke, Holger N. Lode, Wolfgang Wrasidlo
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Publication number: 20090170843Abstract: 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: ApplicationFiled: April 14, 2005Publication date: July 2, 2009Inventors: Thierry Imbert, Yves Guminski, Jean-Marc Barret, Anna Kruczynski
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Publication number: 20090131498Abstract: 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: ApplicationFiled: January 18, 2006Publication date: May 21, 2009Inventors: Samuel J. Danishefsky, Zhaoyang Meng, Vladimir Birman
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Patent number: 7459555Abstract: 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: GrantFiled: December 13, 2001Date of Patent: December 2, 2008Assignee: Rodenstock GmbHInventors: Manfred Melzig, Claudia Mann, Udo Weigand
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Publication number: 20080207747Abstract: 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: ApplicationFiled: July 5, 2005Publication date: August 28, 2008Applicant: SUNTORY LIMITEDInventors: Masaaki Nakai, Yuko Fukui, Sumio Asami, Fumio Hashimoto
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Patent number: 7348358Abstract: 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: GrantFiled: June 19, 2002Date of Patent: March 25, 2008Assignee: Axelar ABInventors: Olle Larsson, Magnus Axelson
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Patent number: 7342114Abstract: 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: GrantFiled: July 1, 2003Date of Patent: March 11, 2008Assignees: California Pacific Medical Center, Catholic Healthcare West, DBA St. Mary's Medical CenterInventor: Li-Xi Yang
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Patent number: 7192682Abstract: 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: GrantFiled: June 27, 2003Date of Patent: March 20, 2007Assignee: NEC CorporationInventors: Katsumi Maeda, Kaichiro Nakano
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Patent number: 7186495Abstract: 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 theType: GrantFiled: December 29, 2000Date of Patent: March 6, 2007Assignee: NEC CorporationInventors: Katsumi Maeda, Shigeyuki Iwasa, Kaichiro Nakano, Etsuo Hasegawa
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Patent number: 7176236Abstract: 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: GrantFiled: November 13, 2003Date of Patent: February 13, 2007Assignee: University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Zhiyan Xiao, Kenneth F. Bastow
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Patent number: 7098348Abstract: 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: GrantFiled: January 27, 2006Date of Patent: August 29, 2006Assignee: Pharmagenesis, Inc.Inventors: Dongcheng Dai, John H. Musser
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Patent number: 7094805Abstract: 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: GrantFiled: December 13, 2002Date of Patent: August 22, 2006Assignee: The Trustees of Columbia University in the City of New YorkInventors: Samuel J. Danishefsky, Vladimir B. Birman