Tricyclo Ring System Having The Lactone Ring As One Of The Cyclos Patents (Class 549/299)
  • Patent number: 10918106
    Abstract: Disclosed herein are compounds, salts, solvates of Formula (1), and any formulation thereof. Also disclosed are methods of eliciting hydraulic enhancement and/or increasing yield of a plant by contacting a plant with compounds, salts, solvates of Formula (1), or any formulation thereof.
    Type: Grant
    Filed: April 23, 2016
    Date of Patent: February 16, 2021
    Assignee: Sound Agriculture Company
    Inventors: Travis Scott Bayer, Eric Alan Davidson, Yonek Hleba
  • Patent number: 9518037
    Abstract: Provided are: a method for producing N,N-dialkylhomofarnesic acid amide, which is a precursor of (±)-3a,6,6,9a-tetramethyldodecahydronaphtho[2.1-b]furan that is useful as a fragrance, at a high recovery rate of a raw material, at a high purity and at a high yield; and a method for producing (±)-3a,6,6,9a-tetramethyldodecahydronaphtho[2.1-b]furan. It is a method for producing N,N-dialkylhomofarnesic acid amide, said method including reacting nerolidol with N,N-dialkylformamide dimethyl acetal under the conditions that the N,N-dialkylformamide dimethyl acetal can be refluxed, wherein the molar ratio of the N,N-dialkylformamide dimethyl acetal to the nerolidol is in a range of 1.5 to 3.
    Type: Grant
    Filed: October 4, 2013
    Date of Patent: December 13, 2016
    Assignee: KAO CORPORATION
    Inventors: Kenji Tanino, Takashi Aoki
  • Patent number: 9379335
    Abstract: Disclosed is the synthesis of benzodipyrrolidone and their polymers and small molecules for electronic and optoelectronic applications. Also disclosed are devices that incorporate such polymers and small molecules.
    Type: Grant
    Filed: April 8, 2013
    Date of Patent: June 28, 2016
    Assignee: The Regents of the University of California
    Inventors: Weibin Cui, Fred Wudl
  • Patent number: 9364457
    Abstract: The present invention discloses a composition for lowering blood lipid and elevating high-density lipoprotein and a method for manufacturing the same; the composition comprises monascin or ankaflavin, or a combination thereof; the manufacturing method comprises the steps of: treating a Monascus fermented product with acetone for three times; elevating the concentration of the Monascus fermented product by a process of decompress concentration; and extracting the monascin and the ankaflavin from the Monascus fermented product with a silica gel column chromatography, a Sephadex LH-20 column chromatography, the silica gel column chromatography, and a preparative high performance liquid chromatography sequentially.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: June 14, 2016
    Assignee: SUNWAY BIOTECH CO., LTD.
    Inventors: Tzu-Ming Pan, Chun-Lin Lee, Cheng-Lun Wu
  • Patent number: 9303006
    Abstract: Preparation and application of line leaf inula flower lactone A for treating myocarditis having a structure of The compound shows positive therapeutic activity against Coxsackie virus and significant dose dependent correlation. The line leaf inula flower lactone A prevents disease in mouse models of experimental autoimmune myocarditis and onset of the process by intraperitoneal injection of a dose of 20 mg/kg/d. When increased to 100 mg/kg/d, the line leaf inula flower lactone A shows positive therapeutic effect on EAM. Line leaf inula flower lactone A is used as the sole active ingredient and combined with a conventional pharmaceutical carrier in a drug for treating myocarditis, and the pharmaceutical composition may be in the form of tablets, dispersible tablets, mouth collapse tablets, retard tablets, capsule, soft capsule, dropping pill, granules, injection, powder injection, or aerosol.
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: April 5, 2016
    Assignee: SHANXI ZHENDONG PILOT BIOLOGICAL SCIENCE AND TECHNOLOGY CO., LTD.
    Inventors: Weidong Zhang, Lei Shan, Huizi Jin, Juan Su, Huiliang Li, Yunheng Shen, Xike Xu, Runhui Liu
  • Patent number: 9278948
    Abstract: Preparation and application of line leaf inula flower lactone A in the multiple sclerosis, having a structure of Line leaf inula flower lactone A has therapeutic effects on experimental autoimmune encephalomyelitis (EAE) model, and is used to develop drug for treating multiple sclerosis (MS). Line leaf inula flower lactone A drug is a combination containing the active ingredient of line leaf inula flower lactone A and conventional pharmaceutically carrier, and may be in forms of tablets, dispersible tablets, mouth collapse tablets, retard tablets, capsule, soft capsule, dropping pill, granules, injection, powder injection, or aerosol. The pharmaceutical composition is used for treating multiple sclerosis, has tremendous developing potentiality because of its high value of clinical application.
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: March 8, 2016
    Assignee: Shanxi Zhendong Pilot Biological Science And Technology Co., Ltd.
    Inventors: Weidong Zhang, Lei Shan, Juan Su, Huizi Jin, Huiliang Li, Yunheng Shen, Xike Xu, Runhui Liu
  • Publication number: 20150133444
    Abstract: The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, and thiocarbamates. The derivatives may be synthesized via an MMB triazole intermediate. These derivatives are useful for treating cancer in humans.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 14, 2015
    Inventors: Venumadhav Janganati, Narsimha Reddy Penthala, Peter A. Crooks, Craig T. Jordan
  • Publication number: 20150105457
    Abstract: Preparation and application of line leaf inula flower lactone A for treating myocarditis having a structure of The compound shows positive therapeutic activity against Coxsackie virus and significant dose dependent correlation. The line leaf inula flower lactone A prevents disease in mouse models of experimental autoimmune myocarditis and onset of the process by intraperitoneal injection of a dose of 20 mg/kg/d. When increased to 100 mg/kg/d, the line leaf inula flower lactone A shows positive therapeutic effect on EAM. Line leaf inula flower lactone A is used as the sole active ingredient and combined with a conventional pharmaceutical carrier in a drug for treating myocarditis, and the pharmaceutical composition may be in the form of tablets, dispersible tablets, mouth collapse tablets, retard tablets, capsule, soft capsule, dropping pill, granules, injection, powder injection, or aerosol.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Weidong ZHANG, Lei SHAN, Huizi JIN, Juan SU, Huiliang LI, Yunheng SHEN, Xike XU, Runhui LIU
  • Publication number: 20150105458
    Abstract: Preparation and application of line leaf inula flower lactone A in the multiple sclerosis, having a structure of Line leaf inula flower lactone A has therapeutic effects on experimental autoimmune encephalomyelitis (EAE) model, and is used to develop drug for treating multiple sclerosis (MS). Line leaf inula flower lactone A drug is a combination containing the active ingredient of line leaf inula flower lactone A and conventional pharmaceutically carrier, and may be in forms of tablets, dispersible tablets, mouth collapse tablets, retard tablets, capsule, soft capsule, dropping pill, granules, injection, powder injection, or aerosol. The pharmaceutical composition is used for treating multiple sclerosis, has tremendous developing potentiality because of its high value of clinical application.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Weidong ZHANG, Lei SHAN, Juan SU, Huizi JIN, Huiliang LI, Yunheng SHEN, Xike XU, Runhui LIU
  • Publication number: 20150098914
    Abstract: The invention relates to the use of specific glucuronolactone derivatives as self-tanning substances, as tanning enhancers for dihydroxyacetone or for a mixture of self-tanning substances comprising dihydroxyacetone, for modulation of the colour shade achieved in the case of tanning with dihydroxyacetone or by the mixture or preparation comprising dihydroxyacetone, as contrast-reduction agents or for colouring keratin-containing fibres, and to preparations or compositions for colouring keratin-containing fibres comprising these specific glucuronolactone derivatives.
    Type: Application
    Filed: November 10, 2012
    Publication date: April 9, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Christophe Carola, Tatjana Best
  • Patent number: 8969410
    Abstract: A pharmaceutical composition for alleviating or treating gout and the applications thereof are provided. The pharmaceutical composition includes p-coumaryl diacetate as an active ingredient.
    Type: Grant
    Filed: September 26, 2014
    Date of Patent: March 3, 2015
    Assignee: Industrial Technology Research Institute
    Inventors: Ying-Chu Shih, Jenn-Line Sheu, Cheng-Yu Lee, Jir-Mehng Lo, Yi-Ching Lee, Ying-Fei Tsai, Yi-Cheng Cheng
  • Patent number: 8957230
    Abstract: The present invention provides a method for preparing Cleistanthin A, a diphyllin glycoside, derivatives thereof and intermediates thereto. In particular the present invention provides in one of the aspect a method for synthesis of compound of formula D a key intermediate of diphyllin, which can be carried out in a shorter duration and at an ordinary temperature.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: February 17, 2015
    Inventors: Nilesh Shridhar Mulik, Kailash Dattatraya Panghavane
  • Publication number: 20150031725
    Abstract: Provided herein, inter alia, are compositions and methods useful for treating hyperproliferative diseases, including cancer and non-malignant hyperproliferative diseases.
    Type: Application
    Filed: October 2, 2014
    Publication date: January 29, 2015
    Inventors: Richard J. Pietras, Michael E. Jung, Diana C. Marquez-Garban, Gang Deng
  • Publication number: 20140350096
    Abstract: The present invention provides a method for preparing antrocin of pharmaceutically acceptable salts thereof via a series of gold-catalyzed cyclization to construct the (6-6-5) tricyclic core frame. The present invention also provides a use of a composition in preparing drugs for suppressing growth of non-small cell lung cancer cells, wherein the composition comprises an effective amount of antrocin or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: August 10, 2011
    Publication date: November 27, 2014
    Inventors: YEW-MIN TZENG, ZHEN YANG
  • Patent number: 8884027
    Abstract: Melampomagnolide B is disclosed as a new antileukemic sesquiterpene. A biotin-conjugated derivative of melampomagnolide B was prepared to elucidate its mechanism of action. Prodrugs of Melampomagnolide B are disclosed.
    Type: Grant
    Filed: October 21, 2011
    Date of Patent: November 11, 2014
    Assignees: University of Rochester, University of Kentucky Research Foundation
    Inventors: Peter A. Crooks, Craig T. Jordan, Shanshan Pei, Shama Nasim
  • Publication number: 20140330027
    Abstract: The present invention discloses single step, highly enantioselective catalytic oxidative cyclization process for the synthesis of 3-substituted chiral phthalides. In particular, the invention discloses asymmetric synthesis of chiral phthalides via synergetic nitrile accelerated oxidative cyclization of o-cyano substituted aryl alkenes in high yield and enantiomeric excess (ee) in short reaction time. Also, disclosed herein is “one-pot” asymmetric synthesis of biologically important natural compounds having 3-substituted chiral phthalide structural framework in the molecule.
    Type: Application
    Filed: November 12, 2012
    Publication date: November 6, 2014
    Inventors: Rekula Santosh Reddy, Chithanya Kiran Indukuru Naga, Sudalai Arumugam
  • Publication number: 20140142170
    Abstract: A composition and method for influencing energy metabolism and treating metabolic and other disorders is provided. A terpenoid lactone that is a selective activator of SIRT1 is generally in the form of a terpenoid dilactone having a 5-alkeny-loxy-furan-2- one group, such as strigolactone, GR 24, or another strigolactone analog, and is used as a therapeutic agent in a method for influencing energy metabolism and treating metabolic and other disorders. The terpenoid lactone may be administered as an individual agent or combined with a second compound such as a flavonoid, chalconoid, tannin, or nicotinamide inhibition antagonist.
    Type: Application
    Filed: October 27, 2011
    Publication date: May 22, 2014
    Applicant: SIRTUIN VALLEY OY
    Inventors: Markku Laakso, Nagendra Yaluri
  • 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: 8669378
    Abstract: The present invention relates to a process for the total synthesis of epicocconone analogs of formula (I): The invention also relates to novel epicocconone analogs.
    Type: Grant
    Filed: October 25, 2010
    Date of Patent: March 11, 2014
    Assignees: Universite de Rouen, Centre National de la Recherche Scientifique-CNRS, Institut National des Sciences Appliquees de Rouen, Macquarie University
    Inventors: Xavier Franck, Philippe Peixoto, Peter Helmuth Karuso
  • Patent number: 8618314
    Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: December 31, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: George G. Wu, Anantha Sudhakar, Tao Wang, Ji Xie, Frank X. Chen, Marc Poirier, Mingsheng Huang, Vijay Sabesan, Daw-long Kwok, Jian Cui, Xiaojing Yang, Tiruvettipuram K. Thiruvengadam, Jing Liao, Illia Zavialov, Hoa N. Nguyen, Ngiap Kie Lim
  • Publication number: 20130338379
    Abstract: Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required ?-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.
    Type: Application
    Filed: August 19, 2013
    Publication date: December 19, 2013
    Applicant: Alphora Research Inc.
    Inventors: Dino ALBERICO, Joshua CLAYTON, Boris Ivanovich GORIN, Jan OUDENES
  • Patent number: 8586112
    Abstract: The invention provides a process for the production of a substance or composition for the treatment, by therapy or prophylaxis, of parasitic infections, in particular malarial infections such as Plasmodium falciparum infections, of the human or animal body. The process comprises extracting the substance or composition from roots of the plant species Dicoma anomala, by an extraction using an organic solvent to obtain a liquid extract containing the substance or composition and removing the solvent from the liquid extract to leave a dried extract containing the substance or composition. The invention extends also to the use of the substance or composition in the manufacture of a medicament or preparation for such treatment of infections; to a substance or composition for use in such treatment of said infections; to compounds for use in such treatment of said infections; and to a method of treating said infections using such compounds.
    Type: Grant
    Filed: November 2, 2005
    Date of Patent: November 19, 2013
    Assignees: South African Medical Research Council, University of Cape Town
    Inventors: Motlalepula Gilbert Matsabisa, William Ernest Campbell, Peter Ian Folb, Peter John Smith
  • Patent number: 8513441
    Abstract: Fused cyclopentane-4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required ?-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: August 20, 2013
    Assignee: Alphora Research Inc.
    Inventors: Dino Alberico, Joshua Clayton, Boris Ivanovich Gorin, Jan Oudenes
  • Publication number: 20130184473
    Abstract: The present invention discloses a composition for lowering blood lipid and elevating high-density lipoprotein and a method for manufacturing the same; the composition comprises monascin or ankaflavin, or a combination thereof; the manufacturing method comprises the steps of: treating a Monascus fermented product with acetone for three times; elevating the concentration of the Monascus fermented product by a process of decompress concentration; and extracting the monascin and the ankaflavin from the Monascus fermented product with a silica gel column chromatography, a Sephadex LH-20 column chromatography, the silica gel column chromatography, and a preparative high performance liquid chromatography sequentially.
    Type: Application
    Filed: March 7, 2013
    Publication date: July 18, 2013
    Applicant: SUNWAY BIOTECH CO., LTD.
    Inventor: SUNWAY BIOTECH CO., LTD.
  • Publication number: 20130136809
    Abstract: The invention discloses biologically active ingredient(s) selected from 7-hydroxyfrullanolide, its analogs, the ex-tract(s) and fraction(s) standardized to 7-hydroxyfrullanolide or its analogs or both or mixtures thereof or their composition(s) for the prevention, control and treatment of one or more obesity, overweight, metabolic syndrome, diabetes and other metabolic disorders or for producing lean body mass in a warm blooded animal in need thereof.
    Type: Application
    Filed: January 28, 2013
    Publication date: May 30, 2013
    Applicant: LAILA NUTRACEUTICALS
    Inventor: LAILA NUTRACEUTICALS
  • 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
  • Publication number: 20130072695
    Abstract: Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required ?-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.
    Type: Application
    Filed: November 12, 2012
    Publication date: March 21, 2013
    Applicant: Alphora Research Inc.
    Inventor: Alphora Research Inc.
  • Publication number: 20130066071
    Abstract: Anti-virally active carbanucleosides such as entecavir are prepared by a process which utilizes, throughout the synthesis, an aromatic protectant group for the hydroxyl and the alkyl hydroxy groups of the starting material, removed as the final step of a multi-step synthesis. Such protectant groups yield intermediates which are solid and therefore easily purified at various stages of the process, for an economical and relatively fast process for synthesizing the final product.
    Type: Application
    Filed: May 30, 2011
    Publication date: March 14, 2013
    Applicant: ALPHORA RESEARCH INC.
    Inventors: Dino Alberico, Boris Gorin, Ryan Beharrilall, Craig Dixon, Joshua Clayton, Varghese Rexon
  • Publication number: 20130052160
    Abstract: The present invention relates to the fields of genetics, immunology and medicine. The present invention more specifically relates to in vitro or ex vivo methods for determining the susceptibility to a cancer treatment of a subject having a tumour. These methods comprise a step of determining the ability of the treatment, of the subject and/or of the tumour to induce an anticancer immune response, the inability of at least one of the treatment, the subject and the tumor to induce an anticancer immune response being indicative of a resistance of the subject to the therapeutic treatment of cancer. Inventors in particular identify genes specific of a human subject or of cancerous cells which can be used to predict or assess the sensitivity of a subject to a treatment of cancer. The invention also relates to particular compounds capable of activating or enhancing the immune system of a particular subject, when the subject is exposed to a therapeutic treatment of cancer or before such an exposition.
    Type: Application
    Filed: April 1, 2011
    Publication date: February 28, 2013
    Applicant: INSTITUT GUSTAVE ROUSSY
    Inventors: Laurence Zitvogel, Guido Kroemer, Nicolas Delahaye, Yuting Ma, Oliver Kepp
  • Patent number: 8383837
    Abstract: The invention relates to a process for the catalytic conversion of a carbohydrate, an alcohol, an aldehyde or a polyhydroxy compound in the presence of a catalyst containing gold in a solvent.
    Type: Grant
    Filed: June 5, 2008
    Date of Patent: February 26, 2013
    Assignee: DSM IP Assets B.V.
    Inventors: Werner Bonrath, Jocelyn Fischesser
  • Publication number: 20130023586
    Abstract: A compound of the formula I, wherein the symbols are as defined in the remaining specification, or a mixture of two or more compounds of the formula I, for use as active ingredient in the therapeutic—including prophylactic—treatment of a warm-blooded animal for the regulation of body weight (preferred) and/or fat loss (preferred) and/or for the management of obesity and/or for improving the total cholesterol HDL/LDL ratio; where the compound(s) of the formula I may be present in free form, in the form of a pharmaceutically and/or nutraceutically acceptable salt, in the form of tautomers, in the form of esters and/or in the form of solvates, as well as related invention embodiments.
    Type: Application
    Filed: January 13, 2011
    Publication date: January 24, 2013
    Applicant: INTERMED DISCOVERY GMBH
    Inventors: Torsten Grothe, Ernst Roemer, Philipp Wabnitz
  • Publication number: 20130012727
    Abstract: The present invention provides a method for preparing Cleistanthin A, a diphyllin glycoside, derivatives thereof and intermediates thereto. In particular the present invention provides in one of the aspect a method for synthesis of compound of formula D a key intermediate of diphyllin, which can be carried out in a shorter duration and at an ordinary temperature.
    Type: Application
    Filed: June 29, 2012
    Publication date: January 10, 2013
    Inventors: Nilesh Shridhar Mulik, Kailash Dattatraya Panghavane
  • Publication number: 20120302745
    Abstract: This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists.
    Type: Application
    Filed: August 2, 2012
    Publication date: November 29, 2012
    Inventors: Tiruvettipuram K. Thiruvengadam, Anantha R. Sudhakar, Ngiap Kie Lim, Daw-Iong Kwok, George G. Wu, Tao Wang, Mingsheng Huang, Michael D. Green
  • Publication number: 20120296093
    Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.
    Type: Application
    Filed: July 31, 2012
    Publication date: November 22, 2012
    Inventors: George Wu, Anantha R. SUDHAKAR, Tao WANG, Ji XIE, Frank Xing CHEN, Marc POIRIER, Mingsheng HUANG, Vijay SABESAN, Daw-long KWOK, Jian CUI, Xiaojing YANG, Tiruvettipuram K. THIRUVENGADAM, Jing LIAO, Ilia A. Zavialov, Hoa N. NGUYEN, Ngiap Kie LIM
  • Patent number: 8309744
    Abstract: Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required ?-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.
    Type: Grant
    Filed: April 7, 2011
    Date of Patent: November 13, 2012
    Assignee: Alphora Research Inc.
    Inventors: Dino Alberico, Joshua Clayton, Boris Ivanovich Gorin, Jan Oudenes
  • Publication number: 20120271021
    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: Application
    Filed: June 18, 2012
    Publication date: October 25, 2012
    Applicant: FUJIFILM CORPORATION
    Inventors: Shuji HIRANO, Kaoru IWATO, Hiroshi SAEGUSA, Yusuke IIZUKA
  • Patent number: 8258319
    Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: September 4, 2012
    Assignee: Schering Corporation
    Inventors: George G. Wu, Anantha Sudhakar, Tao Wang, Ji Xie, Frank X. Chen, Marc Poirier, Mingsheng Huang, Vijay Sabesan, Daw-long Kwok, Jian Cui, Xiaojing Yang, Tiruvettipuram K. Thiruvengadam, Jing Liao, Ilia Zavialov, Hoa N. Nguyen, Ngiap Kie. Lim
  • Publication number: 20120214194
    Abstract: The present invention relates to a process for the total synthesis of epicocconone analogs of formula (I): The invention also relates to novel epicocconone analogs.
    Type: Application
    Filed: October 25, 2010
    Publication date: August 23, 2012
    Applicants: UNIVERSITE DE ROUEN, MACQUARIE UNIVERSITY, INSTITUT NATIONAL DES SCIENCES APPLIQUEES DE ROUEN, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE-CNRS
    Inventors: Xavier Franck, Philippe Peixoto, Peter Helmuth Karuso
  • Publication number: 20120142914
    Abstract: This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists.
    Type: Application
    Filed: February 10, 2012
    Publication date: June 7, 2012
    Inventors: Tiruvettipuram K. Thiruvengadam, Anantha R. Sudhakar, Ngiap Kie Lim, Daw-Iong Kwok, George G. Wu, Tao Wang, Mingsheng Huang, Michael D. Green
  • Publication number: 20120122943
    Abstract: Melampomagnolide B is disclosed as a new antileukemic sesquiterpene. A biotin-conjugated derivative of melampomagnolide B was prepared to elucidate its mechanism of action. Prodrugs of Melampomagnolide B are disclosed.
    Type: Application
    Filed: October 21, 2011
    Publication date: May 17, 2012
    Applicant: UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION
    Inventors: Peter A. Crooks, Craig T. Jordan, Shanshan Pei, Shama Nasim
  • Publication number: 20120093724
    Abstract: Various embodiments of this invention relate generally to targeted activation and delivery of therapeutic drugs to cells that produce prostate specific antigen (PSA), prostate specific membrane antigen (PSMA) or human glandular kallikrein (hK2). Various further embodiments relate more specifically to PSMA-specific peptide prodrugs that become activated to yield therapeutic drugs. Further aspects of various embodiments of the present invention also relate to methods and compositions for treating or preventing cancers and methods and compositions for detecting and/or imaging cancers.
    Type: Application
    Filed: March 17, 2010
    Publication date: April 19, 2012
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Samuel Ray Denmeade, John Thomas Isaacs, Soeren Brogger Christensen
  • Patent number: 8153826
    Abstract: The present invention relates to industrially useful production processes in which (±)-3a,6,6,9a-tetramethyldecahydronaphtho[2,1-b]furan-2(1H)-ones and further (±)-3a,6,6,9a-tetramethyldo decahydronaphtho[2,1-b]furans are produced from raw materials which are readily available at low costs, through short steps and in a simple manner.
    Type: Grant
    Filed: July 27, 2007
    Date of Patent: April 10, 2012
    Assignee: Kao Corporation
    Inventors: Takashi Aoki, Yoshiharu Ataka
  • Patent number: 8114963
    Abstract: Fluorescent dye compounds of formula (I) are disclosed. These compounds are useful as they interact with organic compounds in a manner such that excitation with certain wavelengths of light results in fluorescent emission. Detection and/or monitoring of the fluorescence provides a means for the detection or quantification of organic compounds when bound to these fluorescent dye compounds. Formula (I), wherein: each of R, R? and R? is a hydrogen atom, halogen atom or a straight or branched C1-20 alkyl, alkenyl or alkynl group optionally substituted with one or more halogen, hydroxyl, and/or oxy group; rings A, B and C optionally include one or more double bonds; rings B and C are optionally substituted with one or more halogen atoms.
    Type: Grant
    Filed: December 3, 2007
    Date of Patent: February 14, 2012
    Assignee: Flurotechnics Pty Limited
    Inventors: Philip John Livingston Bell, Peter Karuso
  • Publication number: 20110251392
    Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.
    Type: Application
    Filed: June 24, 2011
    Publication date: October 13, 2011
    Inventors: George Wu, Anantha R. Sudhakar, Mingsheng Huang, Tao Wang, Vijay Sabesan, Ji Xie, Frank Xing Chen, Marc Poirier, Daw-long Kwok, Jian Cui, Xiaojing Yang, Tiruvettipuram K. Thiruvengadam, Jing Liao, Ilia A. Zavialov, Hoa N. Nguyen, Ngiap Kie. Lim
  • Publication number: 20110250656
    Abstract: The present invention relates to the field of biotechnological production of polyketide based colorants from filamentous fungi, in particular a method for preparing a biomass comprising a Monascus-like pigment composition from a nontoxigenic and non-pathogenic fungal source. The present invention further relates to use of the Monascus-like pigment composition as a colouring agent for food items and/or non-food items, and a cosmetic composition comprising the Monascus-like pigment composition.
    Type: Application
    Filed: August 28, 2008
    Publication date: October 13, 2011
    Applicant: DTU, TECHNICAL UNIVERSITY OF DENMARK
    Inventors: Sameer A.S. Mapari, Anne S. Meyer, Jens C. Frisvad, Ulf Thrane
  • Publication number: 20110230352
    Abstract: A treatment process for a superior plant in order to control the growth of the plant, is characterized in that an adapted quantity of strigolactones is brought in contact with the plant so as to inhibit the formation of at least one ramification. A method of using strigolactones to identify genes and/or molecules involved in the growth of buds and/or ramifications in superior plants is also disclosed.
    Type: Application
    Filed: April 21, 2009
    Publication date: September 22, 2011
    Applicants: INSTITUT NATIONAL DE LA RECHERCHE AGRONOMIQUE, UNIVERSITE PAUL SABATIER, UNIVERSITY OF QUEENSLAND
    Inventors: Catherine Rameau, Jean-Paul Pillot, Guillaume Becard, Victoria Gomez-Roldan, Virginie Puech-Pages, Francoise Rochange, Christine Beveridge, Elizabeth Dun, Phil Brewer
  • Publication number: 20110184192
    Abstract: Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required ?-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.
    Type: Application
    Filed: April 7, 2011
    Publication date: July 28, 2011
    Applicant: ALPHORA RESEARCH INC.
    Inventors: Dino ALBERICO, Joshua CLAYTON, Boris Ivanovich GORIN, Jan OUDENES
  • Publication number: 20110112312
    Abstract: Fused cyclopentane-4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required ?-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.
    Type: Application
    Filed: January 13, 2011
    Publication date: May 12, 2011
    Applicant: ALPHORA RESEARCH INC.
    Inventors: Dino ALBERICO, Joshua CLAYTON, Boris Ivanovich GORIN, Jan OUDENES
  • Patent number: 7928252
    Abstract: Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required ?-side chain and then the required ?-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: April 19, 2011
    Assignee: Alphora Research Inc.
    Inventors: Dino Alberico, Joshua Clayton, Boris Ivanovich Gorin, Jan Oudenes
  • Publication number: 20100267947
    Abstract: This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists.
    Type: Application
    Filed: June 30, 2010
    Publication date: October 21, 2010
    Applicant: SCHERING CORPORATION
    Inventors: Tiruvettipuram K. Thiruvengadam, Anantha R. Sudhakar, Ngiap Kie Lim, Daw-long Kwok, George G. Wu, Tao Wang, Mingsheng Huang, Michael D. Green