Tricyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/458)
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Publication number: 20120022153Abstract: A novel compound derived from the culture product of an actinomycete and having an antitumor activity is provided. Provided is a compound represented by any one of formulas (I), (II) and (III) or an optical isomer thereof or a pharmaceutically acceptable salt thereof which can be isolated from the culture fluid of an actinomycete which belongs to the genus Streptomyces, wherein R1, R2, R5 and R6 each independently represent a hydrogen atom, a methyl group, a hydroxymethyl group, a hydroxyl group, or a double bond by which R1 and R2 or R5 and R6 are bonded; R3, R4, R7 and R8 each independently represent a methyl group or a hydroxymethyl group; and R9 represents a hydrogen atom or a hydroxyl group.Type: ApplicationFiled: March 24, 2010Publication date: January 26, 2012Applicant: NIPPON SUISAN KAISHA, LTD.Inventors: Seizo Sato, Fumie Iwata, Shoichi Yamada, Jiro Takeo, Akihisa Abe, Hiroyuki Kawahara
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Patent number: 8097737Abstract: An industrial process for production of high-purity optically active amine derivatives in high yield while inhibiting the formation of by-products, which comprises subjecting (E)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-ylidene)ethylamine to asymmetric reduction, catalytically reducing the obtained product at a reaction temperature of 40 to 100° C. and a pH of 3 to 9, subjecting the obtained (S)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethylamine to propionylation, and then crystallizing the reaction mixture.Type: GrantFiled: September 12, 2005Date of Patent: January 17, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Shinichi Urayama, Eigo Mutou, Atsushi Inagaki, Takashi Okada, Shigeharu Sugisaki
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Publication number: 20110319642Abstract: The present invention relates to a process for producing (±)-3a,6,6,9a-tetramethyl dodecahydronaphtho[2,1-b]furans from crude (±)-3a,6,6,9a-tetramethyl dodecahydronaphtho[2,1-b]furans obtained by subjecting (±)-3a,6,6,9a-tetramethyl dodecahydronaphtho[2,1-b]furan-2(1H)-ones which are produced by cyclizing a homofarnesylic acid amide or a monocyclohomofarnesylic acid amide in the presence of an acid agent and then hydrolyzing the cyclized product, to reduction reaction and then to cyclization reaction, said process including (i) an alkali treatment step in which the crude (±)-3a,6,6,9a-tetramethyl dodecahydronaphtho[2,1-b]furans are heated in the presence of an alcohol and a metal hydroxide; and (ii) a washing treatment step in which the crude (±)-3a,6,6,9a-tetramethyl dodecahydronaphtho[2,1-b]furans are washed with an aqueous acid solution. The thus obtained (±)-3a,6,6,9a-tetramethyl dodecahydronaphtho[2,1-b]furans have a less off-odor and hardly suffer from deterioration of their smell during storage.Type: ApplicationFiled: January 21, 2010Publication date: December 29, 2011Applicant: Kao CorporationInventors: Kenji Tanino, Takashi Aoki
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Patent number: 8084630Abstract: The present invention provides processes and intermediates for the synthesis of ramelteon.Type: GrantFiled: June 2, 2008Date of Patent: December 27, 2011Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Vinod Kumar Kansal, Dhirenkumar N. Mistry, Sanjay L. Vasoya, Michal Rafilovich, Elena Ben Moha-Lerman, Revital Lifshitz-Liron
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Patent number: 8030347Abstract: The present application relates to a novel cyclopenta[b]benzofuran derivatives, processes for their preparation and their use for the manufacture of medicaments, in particular for the prophylaxis and/or therapy of acute or chronic disorders characterized by elevated cellular stress, by local or systemic inflammatory processes or by hyperproliferation.Type: GrantFiled: May 14, 2005Date of Patent: October 4, 2011Assignee: Bayer HealthCare AGInventors: Nicole Diedrichs, Thomas Fahrig, Irene Gerlach, Jaques Ragot, Joachim Schuhmacher, Kai Thede, Ervin Horváth
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Publication number: 20110229464Abstract: Pharmaceutical compositions and methods for treating and/or preventing age-related macular degeneration with melatonin analogues are provided.Type: ApplicationFiled: June 17, 2009Publication date: September 22, 2011Inventors: David Baron, Keisuke Hirai, Yasushi Shintani, Osamu Uchikawa
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Publication number: 20110218347Abstract: The present invention concerns a process for the preparation of a compound of formula (I) wherein the dotted line is a single bond and n is 1 or the dotted line is a double bond and n is 0, and wherein the relative configuration is as shown, in the form of any one of its diastereoisomers or enantiomers or mixtures thereof.Type: ApplicationFiled: October 20, 2008Publication date: September 8, 2011Inventor: Charles Fehr
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Publication number: 20110207949Abstract: Disclosed herein is a process for resolving N-[2-(1,6,7,8-tetrahydro-2H-indeno [5,4-b] furan-8-yl)] ethylamine into its isomers using an optically active acid and a process for preparing ramelteon from the resolved isomer.Type: ApplicationFiled: November 12, 2009Publication date: August 25, 2011Applicant: WATSON PHARMA PRIVATE LIMITEDInventors: Manjunath Narayan Bhanu, Chandrasekhar Sinha, Bhupesh Aher, Amol Bandal, Atul Parab
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Publication number: 20110184058Abstract: The present invention describes the preparation of 6,7-dihydro-1H-indeno[5,4-b]furan-8(2H)-one, a key intermediate in preparation of ramelteon. The present invention also describes further preceding intermediate compounds useful for the synthesis of 6,7-dihydro-1H-indeno[5,4-b]furan-8(2H)-one.Type: ApplicationFiled: July 13, 2009Publication date: July 28, 2011Applicant: Lek Pharmaceuticals D.D.Inventor: Jerome Cluzeau
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Publication number: 20110168992Abstract: The present invention relates to a novel compound, a method for manufacturing the same, and an organic electronic device using the same, and the novel compound according to the present invention may act as a hole injection, hole transport, electron injection and transport, or light emitting material in an organic light emitting device and an organic electronic device, and the device according to the present invention shows excellent properties in terms of efficiency, a driving voltage, and stability.Type: ApplicationFiled: September 23, 2009Publication date: July 14, 2011Inventors: Jae-Soon Bae, Ji-Eun Kim, Jeung-Gon Kim, Jun-Gi Jang
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Publication number: 20110136752Abstract: The invention relates generally to novel antibiotics and their analogs, to processes for the preparation of these novel antibiotics, to pharmaceutical compositions comprising the novel antibiotics; and to methods of using the novel antibiotics to treat or inhibit various disorders.Type: ApplicationFiled: December 6, 2010Publication date: June 9, 2011Applicant: NOVOBIOTIC PHARMACEUTICALS LLCInventors: Aaron PEOPLES, Lucy Losee LING, Kim LEWIS, Zhizhen ZHANG
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Publication number: 20110123929Abstract: Provided are an oxime compound represented by General Formula (1), a photosensitive composition containing the oxime compound as a photopolymerization initiator, a production method for a color filter using the photosensitive composition, and a color filter obtained by the production method: in General Formula (1), R1 represents a hydrogen atom, an acyl group, an alkoxycarbonyl group or an aryloxylcarbonyl group, each of which may have a substituent; R2 represents or R2s each represent a halogen atom, an alkyl group, an aryl group, an alkyloxy group, an aryloxy group, an alkylthio group, an arylthio group or an amino group; m is an integer of 0 to 4; when m is an integer of 2 or more, R2s may be linked together to form a ring; and A represents a 4-, 5-, 6- or 7-membered ring.Type: ApplicationFiled: August 1, 2007Publication date: May 26, 2011Applicant: FUJIFILM CorporationInventors: Akinori Fujita, Takashi Tamura, Kimi Ikeda, Daisuke Kashiwagi
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Publication number: 20110112180Abstract: The present invention relates to a novel naphtho class of compounds as Stat3 pathway inhibitors and as cancer stem cell inhibitors; to methods of using such compounds to treat cancer; to methods of using such compounds to treat disorders in a mammal related to aberrent Stat3 pathway activity; to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: September 10, 2008Publication date: May 12, 2011Applicant: Boston Biomedical, Inc.Inventors: Zhiwei Jiang, Chiang Jia Li, Wei Li, David Leggett
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Publication number: 20110098351Abstract: The subject of the present invention is specific lactone compounds which can be used as antioxidant agents in pharmaceutical or cosmetic compositions or in food products, the said compounds containing a naphthalene ring onto which two lactone units are grafte.Type: ApplicationFiled: June 28, 2003Publication date: April 28, 2011Inventors: Charles Mioskoski, Thierry Le Gall, Marine Desage, Stephane Meunier, Frederic Taran, Stephanie Nowaczyk
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Patent number: 7910752Abstract: The present invention provides a method for easily and inexpensively preparing a racemate or an optically-active 2-(1 -hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione in high yields, 2-acetyl-2,3-dihydro-5-hydroxynaphtho[2,3-b]furan-4,9-dione which is useful as an intermediate for preparing NFD, and an anticancer agent comprising 2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione as an active ingredient. Said 2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione is obtained in 4 or 5 steps by using comparatively inexpensive 5 -hydroxynaphthalene-1,4-dione (also referred to as juglone) as a starting material.Type: GrantFiled: March 15, 2006Date of Patent: March 22, 2011Assignee: Taheebo Japan Co., Ltd.Inventors: Harukuni Tokuda, Katsumi Nishimura
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Publication number: 20110065786Abstract: The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-?B-dependent conditions.Type: ApplicationFiled: October 8, 2010Publication date: March 17, 2011Inventors: John A. Porco, JR., Baudouin Gerard, Guilford Jones, II
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Publication number: 20110049478Abstract: There is provided an electroactive material having Formula I wherein: Q is the same or different at each occurrence and can be O, S, Se, Te, NR, SO, SO2, or SiR3; R is the same or different at each occurrence and can be hydrogen, alkyl, aryl, alkenyl, or alkynyl; and R1 through R6 are the same or different and can be hydrogen, alkyl, aryl, halogen, hydroxyl, aryloxy, alkoxy, alkenyl, alkynyl, amino, alkylthio, phosphino, silyl, —COR, —COOR, —PO3R2, —OPO3R2, or CN.Type: ApplicationFiled: December 17, 2008Publication date: March 3, 2011Inventors: Hong Meng, Dengfu Wang
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Publication number: 20110049477Abstract: There is provided an electroactive material having Formula I wherein: Q is the same or different at each occurrence and can be O, S, Se, Te, NR, SO, SO2, or SiR3; R is the same or different at each occurrence and can be hydrogen, alkyl, aryl, alkenyl, or alkynyl; and R1 through R6 are the same or different and can be hydrogen, alkyl, aryl, halogen, hydroxyl, aryloxy, alkoxy, alkenyl, alkynyl, amino, alkylthio, phosphino, silyl, —COR, —COOK, —PO3R2, —OPO3R2, or CN.Type: ApplicationFiled: December 9, 2008Publication date: March 3, 2011Applicant: E I. DU PONT DE NEMOURS AND COMPANYInventors: Hong Meng, Fangping Sun
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Publication number: 20110009396Abstract: The present invention provides compounds represented by formula 1: wherein, R1 R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined in the specification, in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. These compounds are useful for treatment of inflammatory disorders including those caused by elevated levels of proinflammatory cytokines such as Tumor Necrosis Factor (TNF-? and/or interleukins (IL-1?, IL-6, IL-8). The invention also relates to processes for the manufacture of compounds of formula 1 and pharmaceutical compositions containing them.Type: ApplicationFiled: July 25, 2008Publication date: January 13, 2011Inventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Rada Dalal, Sapna Parikh, Aditi Amol Tannu
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Publication number: 20110002995Abstract: Provided is a pharmaceutical composition for the treatment and prevention of cardiac diseases, containing (a) a therapeutically effective amount of a compound represented by Formula 1 or 2 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof.Type: ApplicationFiled: December 18, 2008Publication date: January 6, 2011Applicants: MAZENCE INC., KT & G CORPORATIONInventors: Taehwan Kwak, Myung-Gyu Park
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Publication number: 20100331402Abstract: The present invention provides a novel prophylactic or therapeutic agent for attention deficit/hyperactivity disorder. A prophylactic or therapeutic agent for attention deficit/hyperactivity disorder, containing (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide as an active ingredient.Type: ApplicationFiled: January 30, 2009Publication date: December 30, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventor: Keisuke Hirai
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Publication number: 20100324313Abstract: The present invention provides a method for the purification of a prostaglandin by supercritical fluid chromatography, said method comprising the use of a stationary phase and a mobile phase comprising carbon dioxide, provided that when the stationary phase is unmodified silica gel, the prostaglandin is not luprostiol. The invention also provides prostaglandins obtainable by the method.Type: ApplicationFiled: June 22, 2010Publication date: December 23, 2010Applicant: Johnson Matthey Public Limited CompanyInventors: Robert R. Hogan, Ronald Rossi
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Publication number: 20100311990Abstract: The present invention concerns a process for the preparation of a compound of formula (I), wherein the dotted line is a single bond and n is 1 or the dotted line is a double bond and n is 0, and wherein the relative configuration is as shown, in the form of any one of its diastereoisomers or enantiomers or mixtures thereof.Type: ApplicationFiled: October 20, 2008Publication date: December 9, 2010Applicant: FIRMENICH SAInventor: Charles Fehr
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Publication number: 20100274030Abstract: A process of preparing cyclic ethers is described. The process involves the reaction of at least one organic compound such as a dioi or a polyol which it has at least one pair of hydroxyl groups separated by 4 or 5 carbon atoms, and which is capable of being converted into an ether linkage, with an organic carbonate in the presence of a base. The base is an alkoxy, a carbonate or a hydroxide base or is a mixture of such bases. At least one of the hydroxyl groups of the organic compound is not a tertiary hydroxyl group.Type: ApplicationFiled: July 14, 2008Publication date: October 28, 2010Inventors: Hanamanthsa Shankarsa Bevinakatti, Christopher Paul Newman, Simon Ellwood, Pietro Tundo, Fabio Arico, Martin Schroeder
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Publication number: 20100267821Abstract: The present invention provides a prophylactic or therapeutic agent for irritable bowel syndrome, which comprises a compound represented by formula (I): wherein, R1 represents an optionally substituted hydrocarbon group, etc., R2 represents a hydrogen atom or an optionally substituted hydrocarbon group, R3 represents a hydrogen atom, an optionally substituted hydrocarbon group, etc., X represents CHR4, NR4, CO, O or S (wherein, R4 represents a hydrogen atom, an optionally substituted hydrocarbon group, etc.), Y represents C, CH or N, represents a single bond or double bond, ring A represents an optionally substituted 5- to 7-membered oxygen-containing heterocyclic ring, ring B represents an optionally substituted benzene ring, and m represents an integer of 1 to 4, or a salt thereof.Type: ApplicationFiled: June 29, 2010Publication date: October 21, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Jun Terauchi, Fumihiko Sato, Nobuhiro Inatomi
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Patent number: 7816544Abstract: The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-?B-dependent conditions.Type: GrantFiled: March 23, 2005Date of Patent: October 19, 2010Assignee: Trustees of Boston UniversityInventors: Guilford Jones, II, Baudouin Gerard, John A. Porco, Jr.
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Publication number: 20100255054Abstract: Provided is a pharmaceutical composition for the treatment and/or prevention of restenosis including (a) a therapeutically effective amount of a particular compound represented by Formula 1 and 2, or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, a diluent or an excipient, or any combination thereof.Type: ApplicationFiled: November 26, 2007Publication date: October 7, 2010Inventors: Taehwan Kwak, Sang-ku Yoo, Myung-gyu Park
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Publication number: 20100249075Abstract: The present invention relates to novel tetralin ER-? agonist compounds, pharmaceutical compositions thereof, and use of these compounds to treat a ER-? mediated disease such as nocturia, obstructive uropathy, benign prostatic hypertrophy, obesity, dementia, hypertension, incontinence, colon cancer, prostate cancer, infertility, depression, leukemia, inflammatory bowel disease, and arthritis.Type: ApplicationFiled: February 10, 2006Publication date: September 30, 2010Applicant: ELI LILLY AND COMPANYInventors: Venkatesh Krishnan, Julian Stanley Kroin, Bryan Hurst Norman, Elizabeth Marie Thomas
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Publication number: 20100248316Abstract: A method for the cyclodehydration of a 1,4- or 1,5-diol includes the step of exposing a 1,4- or a 1,5-diol to an activated zeolite at a temperature of between about 0° C. and about 110° C. for a period of between about 1 and 24 hours. The activated zeolite is prepared from an inactive NaY or CaY type zeolite by ion exchange with an ammonium salt, to produce an ammonium zeolite and exchange of at least part of the ammonia of the ammonium zeolate with a group II A metal.Type: ApplicationFiled: March 18, 2010Publication date: September 30, 2010Applicant: CSIRInventors: Lucia H. Steenkamp, Mihloti Taka
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Publication number: 20100234622Abstract: A process is described for the preparation on an industrial scale of N-[2-(8S)-1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl]ethyl]propionamide, ramelteon, having the structure illustrated below:Type: ApplicationFiled: October 16, 2009Publication date: September 16, 2010Inventors: Roberto Lenna, Cristina Ghidoli, Luigi Panza
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Publication number: 20100215625Abstract: One of the problems to be resolved by the present invention is to stably and sustainably produce active ingredients contained in Bignoniaceous plants of which a mass production is difficult in a conventional manner. The present invention relates to a method for efficiently preparing an anticancer active ingredient NQ801 by a cell cultivation of Bignoniaceous plants under specific culture conditions. An ingredient-production system in the present invention has an anticancer activity.Type: ApplicationFiled: October 26, 2009Publication date: August 26, 2010Applicant: TAHEEBO JAPAN CO., LTD.Inventors: Akira Iida, Ryuji Takeda, Masafumi Kaneko, Harukuni Tokuda
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Publication number: 20100204315Abstract: An object of the present invention is to provide organic solvent extracts of red algae laurencia sp., compounds isolated and identified therefrom, and an agent for preventing attachment of barnacles comprising them. The present invention relates to a barnacle attachment preventive agent consisting of at least one selected from the group consisting of Laurencin, Thyrsiferol, Magireol A, Omaezallene, Hachijojimallene A and organic solvent extracts of red algae laurencia sp.Type: ApplicationFiled: September 5, 2008Publication date: August 12, 2010Inventors: Tatsufumi Okino, Yasuyuki Nogata
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Publication number: 20100187505Abstract: The present invention relates to the compounds of the formula (1) and to organic electroluminescent devices, in particular blue-emitting devices, in which these compounds are used as host material or dopant in the emitting layer and/or as hole-transport material and/or as electron-transport material.Type: ApplicationFiled: April 29, 2008Publication date: July 29, 2010Inventors: Philipp Stoessel, Arne Buesing, Holger Heil
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Publication number: 20100168441Abstract: Disclosed is a process for production of a substituted benzene, which comprises intramolecularly and/or intermolecularly trimerizing a triple bond in an alkyne in the presence of a transition metal catalyst to yield a substituted benzene compound. In the process, the transition metal catalyst is prepared from an iminomethylpyridine represented by the formula (1) or (2), a transition metal salt or a hydrate thereof, and a reducing agent in a reaction system and is used to perform the trimerization. The process can be used in any one of the intramolecular cyclization of a triyne compound, the cyclization of a diyne compound or an alkyne compound and the intermolecular cyclization of three molecules of an alkyne compound, is excellent in economic effectiveness and operability, and is practically advantageous.Type: ApplicationFiled: January 9, 2007Publication date: July 1, 2010Inventor: Sentaro Okamoto
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Publication number: 20100152467Abstract: The present invention provides a process for producing cercosporamide comprising culturing a fungus belonging to the genus Lachnum and/or fungus belonging to the genus Pseudaegerita and recovering cercosporamide from the culture thereof. In addition, the present invention provides cercosporamide acquired according to this production process. Further, the present invention provides novel microorganisms consisting of Lachnum fuscescens SANK 19096, Lachnum calycioides SANK 12497, Lachnum caesaliatum SANK 10906, and Pseudaegerita websteri SANK 11006.Type: ApplicationFiled: August 8, 2006Publication date: June 17, 2010Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Tsuyoshi Hosoya, Jun Ohsumi, Kiyoshi Hamano, Yasunori Ono, Masami Miura
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Publication number: 20100152468Abstract: The present invention provides processes and intermediates for the synthesis of ramelteon.Type: ApplicationFiled: October 16, 2009Publication date: June 17, 2010Inventors: Vinod Kumar Kansal, Dhirenkumar N. Mistry, Sanjay L. Vasoya, Arpan M. Jadav, Pratish Dadhaniya, Jitendra Nalawade
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Patent number: 7728155Abstract: Compounds of formula 1 or pharmaceutically acceptable salts thereof are provided: which are agonists and partial agonists of the 2c subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.Type: GrantFiled: October 21, 2004Date of Patent: June 1, 2010Assignee: Wyeth LLCInventors: Jonathan Laird Gross, Gary Paul Stack, Hong Gao
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Publication number: 20100120760Abstract: A compound of the formula (I): as defined herein, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing a compound of the formula (I) for use in inhibiting hepatitis C virus polymerase and/or of treating or preventing an illness due to hepatitis C virus,Type: ApplicationFiled: March 25, 2008Publication date: May 13, 2010Applicant: ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGInventors: Uwe Koch, Angela Claire Mackay, Frank Narjes, Ian Stansfield
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Publication number: 20100105931Abstract: The present invention provides a new bis(tetrahydrofuran) compound having an excellent neurotrophic factor activity-enhancing effect, and a process for producing the same. The bis(tetrahydrofuran) compound of the present invention is represented by formula (1): wherein R1 and R2 are the same or different, and represent a C1-4 alkyl group, a C1-5 alkoxy group, an aryl C1-5 alkoxy group, a C2-5 alkenyloxy group, or an aryl C2-5 alkenyloxy group, or R1 and R2 together represent ?O or ?CH2; R3 represents a hydrogen atom or a group —CH2—O—R4; R4 represents a C1-4 alkyl group, a C1-5 alkylcarbonyl group, or an aryl C1-4 alkyl group that may have a substituent on an aryl ring; and a carbon-carbon bond between “a” and “b” represents a single bond or a double bond. The bis(tetrahydrofuran) compound has an excellent neurotrophic factor activity-enhancing effect.Type: ApplicationFiled: February 28, 2008Publication date: April 29, 2010Applicant: Otsuka Chemical Co., Ltd.Inventors: Mugio Nishizawa, Yoshiyasu Fukuyama, Hiroshi Imagawa
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Patent number: 7695980Abstract: The present invention relates to novel chemiluminescent compounds, to a method for synthesizing these compounds, to derivatives and conjugates comprising these compounds, to the use of these compounds or conjugates thereof in chemiluminescence based assays, especially in immunoassays.Type: GrantFiled: January 25, 2006Date of Patent: April 13, 2010Assignee: Roche Diagnostics Operations, Inc.Inventors: Dieter Heindl, Rupert Herrmann, Wolfgang Jenni, Heribert Maerz
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Publication number: 20100069446Abstract: The present invention is directed to a derivative comprised of an L-Threonine bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. The derivative has the same utility as the drug from which it is made, but it has enhanced therapeutic properties. In fact, the derivatives of the present invention enhance at least one or more therapeutic qualities, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.Type: ApplicationFiled: September 10, 2009Publication date: March 18, 2010Applicant: SIGNATURE R&D HOLDINGSInventor: V. Ravi Chandran
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Publication number: 20100062065Abstract: Provided is an oral pharmaceutical composition with improved bioavailability and pharmacokinetic properties of a drug, by increasing a bioabsorption rate and an in vivo retention time of an active ingredient via intestine-targeted formulation of a particular naphthoquinone-based compound, or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as an active ingredient.Type: ApplicationFiled: November 26, 2007Publication date: March 11, 2010Applicants: MAZENCE INC., KT & G CP., LTDInventors: In Geun Jo, Sang-Ku Yoo, Myung-gyu Park, Taehwan Kwak
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Patent number: 7635781Abstract: A compound of formula (X): wherein R1, R2, equal to or different from each other are hydrogen or a linear or branched saturated or unsaturated C1-C20-alkyl, C3-C20-cycloalkyl, C6-C20-aryl, C7-C20-alkylaryl or C7-C20-arylalkyl radical, optionally containing heteroatoms belonging to groups 13-17 of the Periodic Table of the Elements; or they can form a C4-C7 ring optionally containing O, S, N, P or Si atoms that can bear substituents; R3 is hydrogen or a linear or branched saturated or unsaturated C1-C20-alkyl, C3-C20-cycloalkyl, C6-C20-aryl, C7-C20-alkylaryl or C7-C20-arylalkyl radical, optionally containing heteroatoms belonging to groups 13-17 of the Periodic Table of the Elements; or two adjacent R3 groups can form a C4-C7 ring optionally containing O, S, N, P or Si atoms, wherein said ring can bear substituents; and at least one of R1, R2 or R3 is different from hydrogen.Type: GrantFiled: June 27, 2007Date of Patent: December 22, 2009Assignee: Basell Polyolefine GmbHInventors: Ilya Nifant'ev, Igor Kashulin, Pavel Ivchenko, Peter Klusener, Frans Korndorffer, Kees de Kloe, Jos Rijsemus
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Publication number: 20090306200Abstract: The present invention provides a prophylactic or therapeutic agent for nocturnal conduct disorders associated with dementia, comprising (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide.Type: ApplicationFiled: April 3, 2006Publication date: December 10, 2009Applicant: Takeda Pharmaceutical Company LimitedInventors: Keisuke Hirai, Masaomi Miyamoto
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Publication number: 20090299081Abstract: The present invention provides a new strategies for the synthesis of compounds of the rocaglamide family and related natural products. The synthetic approach generally involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by an enantioselective 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile in the presence of a TADDOL derivative. This approach can be used for the formation of adducts containing an aglain core structure. Methods of the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-?B-dependent conditions.Type: ApplicationFiled: May 21, 2007Publication date: December 3, 2009Applicant: TRUSTEES OF BOSTON UNIVERSITYInventors: John A. Porco, JR., Baudouin Gerard
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Publication number: 20090281176Abstract: A process for the preparation of ramelteon and intermediates useful in the process. The process suitable for industrial scale provides increased yield and/or greater purity with fewer process steps.Type: ApplicationFiled: November 3, 2008Publication date: November 12, 2009Inventors: Vinod Kumar Kansal, Dhirenkumar N. Mistry, Sanjay L. Vasoya, Rakesh Patel, Arpan M. Jadav
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Publication number: 20090270639Abstract: 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: ApplicationFiled: July 27, 2007Publication date: October 29, 2009Applicant: KAO CORPORATIONInventors: Takashi Aoki, Yoshiharu Ataka
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Publication number: 20090143463Abstract: A therapeutic agent and a treatment method for uremia of human and animals, which therapeutic agent can be easily taken, has lower side effects, and which is not expensive in view of medical economics, are disclosed. The therapeutic agent for uremia in patients suffering from chronic renal failure comprises as an effective ingredient a prostaglandin I2 derivative having a specific structure, such as beraprost sodium. The therapeutic agent for uremia ameliorates the uremia concurred in patients with chronic renal failure without accompanying side effects, and restoration of decreased appetite, improvements in activities, increase in body weight and the like are achieved. The therapeutic effect of uremia is clear alleviation or disappearance of symptoms of uremia grasped as clinical symptoms, observed in the state of renal failure, especially even in spite of the state wherein the decrease in renal function is progressed.Type: ApplicationFiled: July 7, 2006Publication date: June 4, 2009Applicant: Toray Industries, Inc., a corporation of JapanInventors: Masahiko Takenaka, Yoshihisa Yamane, Nobutaka Ida, Hajimu Kurumatani
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Patent number: 7538234Abstract: An object of the present invention is to provide a method for efficiently preparing (S)-2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]-furan-4,9-dione useful as a medicine at a low cost and in large amounts. According to the present invention, the desired (S)-2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione can be prepared with high efficiency at a low cost and in large amounts by asymmetrically reducing 2-acetyl-5-hydroxynaphtho[2,3-b]furan-4,9-dione in the presence of an asymmetric ruthenium complex and a hydrogen donor.Type: GrantFiled: January 29, 2008Date of Patent: May 26, 2009Assignee: Taheebo Japan Co., Ltd.Inventors: Akira Iida, Harukuni Tokuda, Mitsuaki Yamashita
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Patent number: RE41366Abstract: The invention relates to a method for the synthesis of galanthamine, the derivatives and analogues thereof of formula (1) where R1=a hydrogen atom, R2=a hydroxy group, R1 and R2 together form ?O, R3, R4, and R5 independently=a hydrogen atom, a hydroxy group or a (C1-C2)alkoxy group, R6?H, (C1-C12)alkyl, (CH2)nNR7R8, or —(CH2)nN+R7R8R9 where n=1 to 12, Z=two hydrogen atoms, or an oxygen atom and X=an oxygen, sulphur or nitrogen atom, or a —SO, —SO2, or —NR6 group where R6 is as defined above or is an amine protecting group.Type: GrantFiled: June 14, 2002Date of Patent: June 1, 2010Assignee: Centre National del la Recherche Scientifique (CNRS)Inventors: Claude Thal, Catherine Guillou, Jean-Luc Beunard, Emmanuel Gras, Pierre Potier