Tricyclo Ring System Having The Lactone Ring As One Of The Cyclos Patents (Class 549/299)
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Patent number: 11884653Abstract: Ebola virus and Marburg virus are filoviruses and are responsible for outbreaks that cause up to 90% fatality, including the recent outbreak in West Africa that has resulted in over 11,000 deaths. The present disclosure generally relates to series novel arylnaphthalene compounds, having a formula (I) or a pharmaceutically acceptable salt thereof, as a vacuolar-ATPase inhibitor that are useful for the treatment for a broad spectrum of viral infections, including those infections caused by filoviruses. Pharmaceutical composition matters and methods of use are within the scope of this invention.Type: GrantFiled: April 6, 2021Date of Patent: January 30, 2024Assignees: Purdue Research Foundation, Trustees of Boston UniversityInventors: Vincent Jo Davisson, Aaron Raymond Lindstrom, Naoaki Fujii, Robert A. Davey
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Patent number: 11691928Abstract: The invention provides compositions and systems comprising a carrier and an element. The carrier is a network of polymers insoluble in water comprising phenolic hydroxyl moieties, aliphatic hydroxyl moieties or a combination thereof. An association between the carrier and the element is labile in response to biological demand and the lability of the association in the presence of water is less than the lability of the association in response to biological demand. Also provided are methods of making such compositions and methods for delivering the element to an organism.Type: GrantFiled: May 17, 2019Date of Patent: July 4, 2023Assignee: Lucent Biosciences, Inc.Inventors: Neil Robin Branda, Farahnaz Nourmohammadian, Peter Gross
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Patent number: 10918106Abstract: 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: GrantFiled: April 23, 2016Date of Patent: February 16, 2021Assignee: Sound Agriculture CompanyInventors: Travis Scott Bayer, Eric Alan Davidson, Yonek Hleba
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Patent number: 9518037Abstract: 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: GrantFiled: October 4, 2013Date of Patent: December 13, 2016Assignee: KAO CORPORATIONInventors: Kenji Tanino, Takashi Aoki
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Patent number: 9379335Abstract: 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: GrantFiled: April 8, 2013Date of Patent: June 28, 2016Assignee: The Regents of the University of CaliforniaInventors: Weibin Cui, Fred Wudl
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Method for manufacturing composition for lowering blood lipid and elevating high-density lipoprotein
Patent number: 9364457Abstract: 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: GrantFiled: March 7, 2013Date of Patent: June 14, 2016Assignee: SUNWAY BIOTECH CO., LTD.Inventors: Tzu-Ming Pan, Chun-Lin Lee, Cheng-Lun Wu -
Patent number: 9303006Abstract: 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: GrantFiled: December 18, 2014Date of Patent: April 5, 2016Assignee: 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
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Patent number: 9278948Abstract: 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: GrantFiled: December 18, 2014Date of Patent: March 8, 2016Assignee: 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
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Publication number: 20150133444Abstract: 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: ApplicationFiled: November 10, 2014Publication date: May 14, 2015Inventors: Venumadhav Janganati, Narsimha Reddy Penthala, Peter A. Crooks, Craig T. Jordan
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Publication number: 20150105457Abstract: 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: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Inventors: Weidong ZHANG, Lei SHAN, Huizi JIN, Juan SU, Huiliang LI, Yunheng SHEN, Xike XU, Runhui LIU
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Publication number: 20150105458Abstract: 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: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Inventors: Weidong ZHANG, Lei SHAN, Juan SU, Huizi JIN, Huiliang LI, Yunheng SHEN, Xike XU, Runhui LIU
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Publication number: 20150098914Abstract: 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: ApplicationFiled: November 10, 2012Publication date: April 9, 2015Applicant: MERCK PATENT GMBHInventors: Christophe Carola, Tatjana Best
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Patent number: 8969410Abstract: 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: GrantFiled: September 26, 2014Date of Patent: March 3, 2015Assignee: Industrial Technology Research InstituteInventors: Ying-Chu Shih, Jenn-Line Sheu, Cheng-Yu Lee, Jir-Mehng Lo, Yi-Ching Lee, Ying-Fei Tsai, Yi-Cheng Cheng
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Patent number: 8957230Abstract: 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: GrantFiled: June 29, 2012Date of Patent: February 17, 2015Inventors: Nilesh Shridhar Mulik, Kailash Dattatraya Panghavane
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Publication number: 20150031725Abstract: Provided herein, inter alia, are compositions and methods useful for treating hyperproliferative diseases, including cancer and non-malignant hyperproliferative diseases.Type: ApplicationFiled: October 2, 2014Publication date: January 29, 2015Inventors: Richard J. Pietras, Michael E. Jung, Diana C. Marquez-Garban, Gang Deng
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METHOD FOR CHEMICAL SYNTHESIS OF ANTROCIN AND USE THEREOF FOR SUPPRESSING NON-SMALL CELL LUNG CANCER
Publication number: 20140350096Abstract: 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: ApplicationFiled: August 10, 2011Publication date: November 27, 2014Inventors: YEW-MIN TZENG, ZHEN YANG -
Patent number: 8884027Abstract: 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: GrantFiled: October 21, 2011Date of Patent: November 11, 2014Assignees: University of Rochester, University of Kentucky Research FoundationInventors: Peter A. Crooks, Craig T. Jordan, Shanshan Pei, Shama Nasim
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Publication number: 20140330027Abstract: 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: ApplicationFiled: November 12, 2012Publication date: November 6, 2014Inventors: Rekula Santosh Reddy, Chithanya Kiran Indukuru Naga, Sudalai Arumugam
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Publication number: 20140142170Abstract: 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: ApplicationFiled: October 27, 2011Publication date: May 22, 2014Applicant: SIRTUIN VALLEY OYInventors: Markku Laakso, Nagendra Yaluri
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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: 8669378Abstract: 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: GrantFiled: October 25, 2010Date of Patent: March 11, 2014Assignees: Universite de Rouen, Centre National de la Recherche Scientifique-CNRS, Institut National des Sciences Appliquees de Rouen, Macquarie UniversityInventors: Xavier Franck, Philippe Peixoto, Peter Helmuth Karuso
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Patent number: 8618314Abstract: 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: GrantFiled: July 31, 2012Date of Patent: December 31, 2013Assignee: 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
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Publication number: 20130338379Abstract: 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: ApplicationFiled: August 19, 2013Publication date: December 19, 2013Applicant: Alphora Research Inc.Inventors: Dino ALBERICO, Joshua CLAYTON, Boris Ivanovich GORIN, Jan OUDENES
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Patent number: 8586112Abstract: 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: GrantFiled: November 2, 2005Date of Patent: November 19, 2013Assignees: South African Medical Research Council, University of Cape TownInventors: Motlalepula Gilbert Matsabisa, William Ernest Campbell, Peter Ian Folb, Peter John Smith
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Patent number: 8513441Abstract: 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: GrantFiled: August 28, 2009Date of Patent: August 20, 2013Assignee: Alphora Research Inc.Inventors: Dino Alberico, Joshua Clayton, Boris Ivanovich Gorin, Jan Oudenes
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Publication number: 20130184473Abstract: 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: ApplicationFiled: March 7, 2013Publication date: July 18, 2013Applicant: SUNWAY BIOTECH CO., LTD.Inventor: SUNWAY BIOTECH CO., LTD.
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Publication number: 20130136809Abstract: 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: ApplicationFiled: January 28, 2013Publication date: May 30, 2013Applicant: LAILA NUTRACEUTICALSInventor: LAILA NUTRACEUTICALS
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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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Publication number: 20130072695Abstract: 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: ApplicationFiled: November 12, 2012Publication date: March 21, 2013Applicant: Alphora Research Inc.Inventor: Alphora Research Inc.
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Publication number: 20130066071Abstract: 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: ApplicationFiled: May 30, 2011Publication date: March 14, 2013Applicant: ALPHORA RESEARCH INC.Inventors: Dino Alberico, Boris Gorin, Ryan Beharrilall, Craig Dixon, Joshua Clayton, Varghese Rexon
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Publication number: 20130052160Abstract: 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: ApplicationFiled: April 1, 2011Publication date: February 28, 2013Applicant: INSTITUT GUSTAVE ROUSSYInventors: Laurence Zitvogel, Guido Kroemer, Nicolas Delahaye, Yuting Ma, Oliver Kepp
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Patent number: 8383837Abstract: 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: GrantFiled: June 5, 2008Date of Patent: February 26, 2013Assignee: DSM IP Assets B.V.Inventors: Werner Bonrath, Jocelyn Fischesser
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Publication number: 20130023586Abstract: 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: ApplicationFiled: January 13, 2011Publication date: January 24, 2013Applicant: INTERMED DISCOVERY GMBHInventors: Torsten Grothe, Ernst Roemer, Philipp Wabnitz
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Publication number: 20130012727Abstract: 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: ApplicationFiled: June 29, 2012Publication date: January 10, 2013Inventors: Nilesh Shridhar Mulik, Kailash Dattatraya Panghavane
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Publication number: 20120302745Abstract: 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: ApplicationFiled: August 2, 2012Publication date: November 29, 2012Inventors: Tiruvettipuram K. Thiruvengadam, Anantha R. Sudhakar, Ngiap Kie Lim, Daw-Iong Kwok, George G. Wu, Tao Wang, Mingsheng Huang, Michael D. Green
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Publication number: 20120296093Abstract: 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: ApplicationFiled: July 31, 2012Publication date: November 22, 2012Inventors: 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
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Patent number: 8309744Abstract: 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: GrantFiled: April 7, 2011Date of Patent: November 13, 2012Assignee: Alphora Research Inc.Inventors: Dino Alberico, Joshua Clayton, Boris Ivanovich Gorin, Jan Oudenes
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Publication number: 20120271021Abstract: 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: ApplicationFiled: June 18, 2012Publication date: October 25, 2012Applicant: FUJIFILM CORPORATIONInventors: Shuji HIRANO, Kaoru IWATO, Hiroshi SAEGUSA, Yusuke IIZUKA
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Patent number: 8258319Abstract: 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: GrantFiled: June 24, 2011Date of Patent: September 4, 2012Assignee: Schering CorporationInventors: 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
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Publication number: 20120214194Abstract: 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: ApplicationFiled: October 25, 2010Publication date: August 23, 2012Applicants: UNIVERSITE DE ROUEN, MACQUARIE UNIVERSITY, INSTITUT NATIONAL DES SCIENCES APPLIQUEES DE ROUEN, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE-CNRSInventors: Xavier Franck, Philippe Peixoto, Peter Helmuth Karuso
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Publication number: 20120142914Abstract: 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: ApplicationFiled: February 10, 2012Publication date: June 7, 2012Inventors: Tiruvettipuram K. Thiruvengadam, Anantha R. Sudhakar, Ngiap Kie Lim, Daw-Iong Kwok, George G. Wu, Tao Wang, Mingsheng Huang, Michael D. Green
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Publication number: 20120122943Abstract: 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: ApplicationFiled: October 21, 2011Publication date: May 17, 2012Applicant: UNIVERSITY OF KENTUCKY RESEARCH FOUNDATIONInventors: Peter A. Crooks, Craig T. Jordan, Shanshan Pei, Shama Nasim
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Publication number: 20120093724Abstract: 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: ApplicationFiled: March 17, 2010Publication date: April 19, 2012Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Samuel Ray Denmeade, John Thomas Isaacs, Soeren Brogger Christensen
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Patent number: 8153826Abstract: 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: GrantFiled: July 27, 2007Date of Patent: April 10, 2012Assignee: Kao CorporationInventors: Takashi Aoki, Yoshiharu Ataka
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Patent number: 8114963Abstract: 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: GrantFiled: December 3, 2007Date of Patent: February 14, 2012Assignee: Flurotechnics Pty LimitedInventors: Philip John Livingston Bell, Peter Karuso
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Publication number: 20110250656Abstract: 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: ApplicationFiled: August 28, 2008Publication date: October 13, 2011Applicant: DTU, TECHNICAL UNIVERSITY OF DENMARKInventors: Sameer A.S. Mapari, Anne S. Meyer, Jens C. Frisvad, Ulf Thrane
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Publication number: 20110251392Abstract: 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: ApplicationFiled: June 24, 2011Publication date: October 13, 2011Inventors: 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
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Publication number: 20110230352Abstract: 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: ApplicationFiled: April 21, 2009Publication date: September 22, 2011Applicants: INSTITUT NATIONAL DE LA RECHERCHE AGRONOMIQUE, UNIVERSITE PAUL SABATIER, UNIVERSITY OF QUEENSLANDInventors: Catherine Rameau, Jean-Paul Pillot, Guillaume Becard, Victoria Gomez-Roldan, Virginie Puech-Pages, Francoise Rochange, Christine Beveridge, Elizabeth Dun, Phil Brewer
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Publication number: 20110184192Abstract: 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: ApplicationFiled: April 7, 2011Publication date: July 28, 2011Applicant: ALPHORA RESEARCH INC.Inventors: Dino ALBERICO, Joshua CLAYTON, Boris Ivanovich GORIN, Jan OUDENES
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Publication number: 20110112312Abstract: 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: ApplicationFiled: January 13, 2011Publication date: May 12, 2011Applicant: ALPHORA RESEARCH INC.Inventors: Dino ALBERICO, Joshua CLAYTON, Boris Ivanovich GORIN, Jan OUDENES