Tricyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/458)
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Patent number: 8703979Abstract: The present invention is directed to provide a novel preparation of anticancer-active tricyclic compounds via alkyne coupling reaction. The present invention provides a process for preparing a compound of formula (Ia) or (Ib): wherein R1 is optionally substituted C1-6 alkyl, etc.; W is O, S or NR2; R2 is hydrogen atom, etc., which comprises Step (a) in which a compound of formula (II): wherein R1 is the same as defined above, and a compound of formula (III) or (IV): wherein R2 is the same as defined above; R3 is hydrogen atom, etc.; X is halogen atom, etc., are reacted in the presence of a base, a copper catalyst and a palladium catalyst in an aprotic polar solvent.Type: GrantFiled: July 26, 2011Date of Patent: April 22, 2014Assignee: Taheebo Japan Co., Ltd.Inventors: Akira Iida, Kazunori Ueda, Mitsuaki Yamashita
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Publication number: 20140066499Abstract: 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: ApplicationFiled: November 13, 2013Publication date: March 6, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Shinichi Urayama, Eigo Mutou, Atsushi Inagaki, Takashi Okada, Shigeharu Sugisaki
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Patent number: 8653286Abstract: Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.Type: GrantFiled: August 7, 2012Date of Patent: February 18, 2014Assignee: Nektar TherapeuticsInventors: Samuel P. McManus, Antoni Kozlowski, Tracy L. Hutchison, Brian Bray, Xiaoming Shen
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Patent number: 8642649Abstract: The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture.Type: GrantFiled: October 9, 2012Date of Patent: February 4, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Yutaka Tanoue, Tetsuya Matsuura, Yutaka Yamagata, Naoki Nagahara
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Patent number: 8642648Abstract: The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture.Type: GrantFiled: October 9, 2012Date of Patent: February 4, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Yutaka Tanoue, Tetsuya Matsuura, Yutaka Yamagata, Naoki Nagahara
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Publication number: 20130344183Abstract: The present invention relates to a novel compound isolated from Kaempferia pandurata Roxb and the use thereof as an antiviral agent. The compound isolated from Kaempferia pandurata Roxb shows the ability to inhibit highly pathogenic virus, and thus is a promising candidate for an antiviral agent.Type: ApplicationFiled: February 16, 2012Publication date: December 26, 2013Applicant: KONKUK UNIVERSITY INDUSTRIAL COOPERATION CORP.Inventors: Soo Ki Kim, Jun Hyeong Lee, Hyung In moon, Sang Heui Seo, Hyun Dong Paik, Sang Buem Cho
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Publication number: 20130345176Abstract: The present invention discloses esters of 4,9-dihydroxy-naphtho[2,3-b]furans and methods of making and using the same. The present invention also discloses conversion of the esters into therapeutically active 4,9-dihydroxy-naphtho[2,3-b]furans in vivo. The present invention furthermore discloses pharmaceutical compositions comprising the esters of 4,9-dihydroxy-naphtho[2,3-b]furans for the treatment of various indications including proliferative diseases.Type: ApplicationFiled: March 4, 2011Publication date: December 26, 2013Applicant: Zhoushan Haizhongzhou Xinsheng Pharmaceuticals Co., Ltd.Inventors: Zhiwei Jiang, Aijin Wang, Hongwei Hu, Jiali Xu, Yuesong Hu, Xian Li, Yan Ye, Jie Wang, Qinglong Li
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Patent number: 8609871Abstract: 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: August 29, 2012Date of Patent: December 17, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Shinichi Urayama, Eigo Mutou, Atsushi Inagaki, Takashi Okada, Shigeharu Sugisaki
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Publication number: 20130315841Abstract: Methods for the synthesis and use of functionalized, substituted naphthalenes are described. The functionalized, substituted naphthalenes display useful properties including liquid crystals and fluorescence properties, such as solvatochromatic fluorescence, with high quantum yields, Stoke's shift, and show emission maxima that are significantly red-shifted.Type: ApplicationFiled: March 15, 2013Publication date: November 28, 2013Inventor: Kay M. Brummond
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Patent number: 8586764Abstract: An organic dye and preparation method thereof and dye-sensitized solar cells using this organic dye are provided. The structure of the organic dye molecule is donor-conjugated unit(s)-acceptor. The organic dye with broad spectrum response and high molar-absorption coefficient is obtained by modifying the structure by using various conjugated unit(s) in combination with donor and acceptor. The conditions of preparation of the organic dye are mild and the yield is high, and the organic dye can be used for highly effective dye-sensitized solar cells.Type: GrantFiled: July 9, 2010Date of Patent: November 19, 2013Assignee: China National Academy of Nanotechnology and EngineeringInventors: Peng Wang, Yupeng Wang, Ning Cai, Wangdong Zeng, Mingfei Xu, Jingyuan Liu
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Publication number: 20130302422Abstract: Provided is a pharmaceutical composition for the treatment and prevention of kidney diseases, containing (a) a therapeutically effective amount of a compound represented by Formulae 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: May 22, 2013Publication date: November 14, 2013Applicants: KT & G CORPORATION, MAZENCE INC.Inventors: Taehwan Kwak, Myung-Gyu Park, Kyoung Hoon Jung
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Publication number: 20130273619Abstract: The present invention relates to new types of processes for the improved preparation of homofarnesol, in particular of (3E,7E)-homofarnesol and homofarnesol preparations with an increased content of (3E,7E)-homofarnesol (also referred to as all E-homofarnesol).Type: ApplicationFiled: April 16, 2013Publication date: October 17, 2013Applicant: BASF SEInventors: Melanie Bonnekessel, Hansgeorg Ernst, Wolfgang Siegel, Ekkehard Winterfeldt, Reinhard W. Hoffmann
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Publication number: 20130248839Abstract: 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: May 20, 2013Publication date: September 26, 2013Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: HONG MENG, FANGPING SUN
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Publication number: 20130225674Abstract: The invention relates to a pharmaceutical product comprising a dibenzofuranone derivative as the active ingredient. The invention further relates to the use of dibenzofuranone derivatives to inhibit kinases, in particular serine/threonine kinases, to the use of dibenzofuranone derivatives for producing drugs and/or medicinal products for treatment, and to the use of dibenzofuranone derivatives as a diagnostic product for analyzing the role of protein kinases, in particular serine/threonine kinases, in particular protein kinase CK2 in cellular processes, the pathogenesis of diseases, ontogenesis and/or other developmental biological phenomena or relationships.Type: ApplicationFiled: June 22, 2011Publication date: August 29, 2013Inventors: Joachim Jose, Claudia Götz, Andreas Gratz, Uwe Kuckländer
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Publication number: 20130175481Abstract: The invention relates to novel polymers containg repeating units based on benzodifuran, benzodipyrrole or benzodithiophene, monomers and methods for their preparation, their use as semiconductors in organic electronic (OE) devices, especially in organic photovoltaic (OPV) devices, and to OE and OPV devices comprising these polymers.Type: ApplicationFiled: June 14, 2011Publication date: July 11, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Nicolas Blouin, Steven Tierney, William Mitchell, Miguel Carrasco-Orozco, Frank Egon Meyer
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Publication number: 20130171415Abstract: Disclosed is a photosensitive resin composition comprising: (Component A) an oxime sulfonate compound represented by Formula (1); (Component B) a resin comprising a constituent unit having an acid-decomposable group that is decomposed by an acid to form a carboxyl group or a phenolic hydroxy group; and (Component C) a solvent wherein in Formula (1) R1 denotes an alkyl group, an aryl group, or a heteroaryl group, each R2 independently denotes a hydrogen atom, an alkyl group, an aryl group, or a halogen atom, Ar1 denotes an o-arylene group or an o-heteroarylene group, X denotes O or S, and n denotes 1 or 2, provided that of two or more R2s present in the compound, at least one denotes an alkyl group, an aryl group, or a halogen atom.Type: ApplicationFiled: February 27, 2013Publication date: July 4, 2013Applicant: FUJIFILM CorporationInventor: FUJIFILM Corporation
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Publication number: 20130158094Abstract: Tricylic ether carbamates that inhibit HIV proteolytic enzymes and processes for preparing the compounds are describes. Methods of using the disclosed compounds for treating patients infected with HIV are also described.Type: ApplicationFiled: September 2, 2011Publication date: June 20, 2013Applicant: PURDUE RESEARCH FOUNDATIONInventors: Arun K. Ghosh, Chun-Xiao Xu, Hiroaki Mitsuya, Garth Parham
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Publication number: 20130158082Abstract: The disclosure relates to methods of managing blood sugar levels and compositions related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing diabetes, insulin resistance, or hyperglycemia comprising administering to a subject diagnosed with, at risk of or exhibiting symptoms of diabetes, insulin resistance, or hyperglycemia a pharmaceutical composition comprising a compound comprising formula I.Type: ApplicationFiled: September 27, 2011Publication date: June 20, 2013Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
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Publication number: 20130150437Abstract: The present invention discloses novel naphtho[2,3-b]furan-4,9-diones and naphtho[2,3-b]thiophene-4,9-diones and methods of making and using the same. The present invention also discloses pharmaceutical compositions comprising novel naphtho[2,3-b]furan-4,9-dione or naphtho[2,3-b]thiophene-4,9-diones for the treatment of various indications including proliferative diseases.Type: ApplicationFiled: August 24, 2010Publication date: June 13, 2013Applicant: Zhoushan HaiZhongZhou Xinsheng Pharmaceuticals Co., Ltd.Inventors: Zhiwei Jiang, Aijin Wang, Xian Li, Qingrong Li, Hongwei Hu, Jiali Xu, Yuesong Hu, Yan Ye
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Publication number: 20130119359Abstract: The disclosure relates to organic electroluminescent elements, materials for use in the elements, and devices using the elements, which include a compound represented by the following General Formula (1): where R1 to R12 each independently represents a hydrogen atom or a substituent and which may be bound to each other to form a non-aromatic ring, where Z1 to Z4 each independently represents a hydrogen atom or a substituent, and where Z1 and Z2, and Z3 and Z4 may be bound to each other to form a ring.Type: ApplicationFiled: November 15, 2012Publication date: May 16, 2013Applicant: UDC Ireland LimitedInventor: UDC Ireland Limited
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Publication number: 20130123266Abstract: A benzene sulphonamide compound of formula I or one of its addition salts with pharmaceutically acceptable acids, for its use in a method for treating a pathology linked to an excessive effect of TNF-alpha and for its use in a method for treating the human or animal body as a direct inhibitor of TNF-alpha.Type: ApplicationFiled: July 19, 2011Publication date: May 16, 2013Applicant: VAX-CONSULTINGInventors: Jean-François Zagury, Matthieu Montes, Hadley Mouhsine, Hélène Guillemain
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Publication number: 20130105769Abstract: A condensed-cyclic compound represented by Formula 1, and an organic light-emitting device including the condensed-cyclic compound. wherein R1 and R2, Ar1 through Ar4, L1 and L2, X1 and X2, and a and b are defined as in the specification.Type: ApplicationFiled: May 22, 2012Publication date: May 2, 2013Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.Inventors: Jin-O Lim, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Sang-Hyun Han, Soo-Yon Kim, Hee-Joo Ko
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Patent number: 8426461Abstract: The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture.Type: GrantFiled: June 8, 2012Date of Patent: April 23, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Yutaka Tanoue, Tetsuya Matsuura, Yutaka Yamagata, Naoki Nagahara
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Publication number: 20130079397Abstract: 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: ApplicationFiled: August 29, 2012Publication date: March 28, 2013Applicant: Takeda Pharmaceutical Company LimitedInventors: Shinichi Urayama, Eigo Mutou, Atsushi Inagaki, Takashi Okada, Shigeharu Sugisaki
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Patent number: 8404088Abstract: 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: GrantFiled: March 19, 2012Date of Patent: March 26, 2013Assignee: Trustees of Boston UniversityInventors: John A. Porco, Jr., Baudouin Gerard
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Publication number: 20130060052Abstract: The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture.Type: ApplicationFiled: July 25, 2012Publication date: March 7, 2013Inventors: Yutaka Tanoue, Tetsuya Matsuura, Yutaka Yamagata, Naoki Nagahara
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Patent number: 8383844Abstract: 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: GrantFiled: January 21, 2010Date of Patent: February 26, 2013Assignee: Kao CorporationInventors: Kenji Tanino, Takashi Aoki
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Publication number: 20130034591Abstract: The invention provides naphthofuran compounds, polymorphs of naphthofuran compounds, naphthofuran compounds in particle form, purified compositions that contain one or more naphthofuran compounds, purified compositions that contain one or more naphthofuran compounds in particle form, methods of producing these naphthofuran compounds, polymorphs, purified compositions and/or particle forms, and methods of using these naphthofuran compounds, polymorphs, purified compositions and/or particle forms to treat subjects in need thereof.Type: ApplicationFiled: March 21, 2011Publication date: February 7, 2013Applicant: Boston Biomedical, Inc.Inventors: Chiang Jia Li, David Leggett, Youzhi Li, Wei Li
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Patent number: 8362072Abstract: A pharmaceutical composition for use in treating, inhibiting, and/or preventing breast and/or ovarian cancer can include: a molecule having a structure of one of Compounds 1-38, pharmaceutically acceptable salt thereof, or analog thereof; and a pharmaceutically acceptable carrier containing the compound. The pharmaceutically acceptable carrier can be configured for oral, systemic, transdermal, intranasal, suppository, parenteral, intramuscular, intravenous, or subcutaneous administration. The compound can be present in the composition in a therapeutically effective amount for treating, inhibiting, and/or preventing breast and/or ovarian cancer. Also, the compound can be present in a therapeutically effective amount for enhancing production of BRCA1.Type: GrantFiled: June 18, 2012Date of Patent: January 29, 2013Assignee: University of KansasInventors: Roy A. Jensen, Lisa M. Harlan-Williams, Frank J. Schoenen, Jeffrey Aube, Gerald H. Lushington
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Patent number: 8362170Abstract: Provided is a polymerizable compound represented by the following general formula (ca-1) or (cb-1): wherein the variables in the formulae are defined in the specification.Type: GrantFiled: June 18, 2012Date of Patent: January 29, 2013Assignee: FUJIFILM CorporationInventors: Shuji Hirano, Kaoru Iwato, Hiroshi Saegusa, Yusuke Iizuka
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Patent number: 8349839Abstract: Compounds of formula (I): wherein R1, R2, A1, A2, A3, A4, X and Y are as defined herein, are useful as inhibitors of HIV replication.Type: GrantFiled: April 8, 2010Date of Patent: January 8, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Claudio Sturino, Patrick Deroy, Martin Duplessis, Paul J. Edwards, Anne-Marie Faucher, Teddy Halmos, Clint James, Jean-Eric Lacoste, Eric Malenfant, Joannie Minville, Louis Morency, Sebastien Morin, Martin Tremblay, Christiane Yoakim
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Publication number: 20120323025Abstract: An improved method is described for making single isomers of synthetic benzoprostacyclin analogue compounds, in particular the pharmacologically active 314-d isomer of beraprost. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.Type: ApplicationFiled: June 15, 2012Publication date: December 20, 2012Inventors: Vijay Sharma, Hitesh Batra, Sudersan Tuladhar
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Publication number: 20120289577Abstract: The present invention relates to a composition for treating or preventing hearing loss comprising naphthoquinone-based compounds.Type: ApplicationFiled: December 27, 2010Publication date: November 15, 2012Applicant: KT&G LIFE SCIENCES CORPORATIONInventors: Tae Hwan Kwak, Myung-Gyu Park, Hong-Seob So, Raekil Park, Hyung-Jin Kim
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Publication number: 20120282191Abstract: The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture.Type: ApplicationFiled: January 16, 2012Publication date: November 8, 2012Inventors: Yutaka Tanoue, Tetsuya Matsuura, Yutaka Yamagata, Naoki Nagahara
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Publication number: 20120271059Abstract: A process for the preparation of ?,?-unsaturated-?,?-disubstituted esters 1 with high E/Z- and ?,?/?,?-ratios, Formula (1) by reacting at a temperature of between about 130 and 170 degrees centigrade the conjugated malonate Formula (3) with, a group I, II or III metal halide or an organic cation/halide anion pair, an inorganic proton source and a polar solvent.Type: ApplicationFiled: December 17, 2010Publication date: October 25, 2012Inventors: Fridtjof Schröder, Urs Mueller, Peter Gygax
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Publication number: 20120238766Abstract: 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: March 19, 2012Publication date: September 20, 2012Applicant: TRUSTEES OF BOSTON UNIVERSITYInventors: John A. Porco, JR., Baudouin Gerard
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Patent number: 8258178Abstract: 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: GrantFiled: September 5, 2008Date of Patent: September 4, 2012Assignee: Central Research Institute of Electric Power IndustryInventors: Tatsufumi Okino, Yasuyuki Nogata
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Patent number: 8252877Abstract: Provided is a polymerizable compound represented by the following general formula (ca-1) or (cb-1): wherein the variables in the formulae are defined in the specification.Type: GrantFiled: December 11, 2009Date of Patent: August 28, 2012Assignee: FUJIFILM CorporationInventors: Shuji Hirano, Kaoru Iwato, Hiroshi Saegusa, Yusuke Iizuka
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Patent number: 8242291Abstract: 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: GrantFiled: October 16, 2009Date of Patent: August 14, 2012Assignee: Industriale Chimica S.r.L.Inventors: Roberto Lenna, Cristina Ghidoli, Luigi Panza
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Patent number: 8227629Abstract: 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: GrantFiled: October 20, 2008Date of Patent: July 24, 2012Assignee: Firmenich SAInventor: Charles Fehr
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Patent number: 8227630Abstract: 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: GrantFiled: October 20, 2008Date of Patent: July 24, 2012Assignee: Firmenich SAInventor: Charles Fehr
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Publication number: 20120101153Abstract: The present invention discloses new rocaglaol derivatives and the use of rocaglaol derivatives to prevent or to limit the cardiotoxicity of an antineoplastic agent, in particular to prevent or to limit the apoptosis of cardiomyocytes induced by such agent.Type: ApplicationFiled: November 24, 2009Publication date: April 26, 2012Applicant: Universite De StrasbourgInventors: Laurent Desaubry, Gunsel Canan Desaubry, Thierry Cresteil, Gülen Türkeri
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Publication number: 20120088826Abstract: 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: ApplicationFiled: December 14, 2011Publication date: April 12, 2012Applicant: Takeda Pharmaceutical Company LimitedInventors: Shinichi Urayama, Eigo Mutou, Atsushi Inagaki, Takashi Okada, Shigeharu Sugisaki
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Publication number: 20120083526Abstract: The present invention relates in general to the field of organic chemistry and in particular to the preparation of 1-(2,3-dihydrobenzofuran-4-yl)ethanone, an intermediate in preparation of (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4-b]furan-8-yl)ethyl]propionamide, i.e. ramelteon.Type: ApplicationFiled: April 6, 2010Publication date: April 5, 2012Applicant: LEK PHARMACEUTICALS D.D.Inventor: Jerome CLuzeau
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Publication number: 20120077986Abstract: The present invention is directed to provide a novel preparation of anticancer-active tricyclic compounds via alkyne coupling reaction. The present invention provides a process for preparing a compound of formula (Ia) or (Ib): wherein R1 is optionally substituted C1-6 alkyl, etc.; W is O, S or NR2; R2 is hydrogen atom, etc., which comprises Step (a) in which a compound of formula (II): wherein R1 is the same as defined above, and a compound of formula (III) or (IV): wherein R2 is the same as defined above; R3 is hydrogen atom, etc.; X is halogen atom, etc., are reacted in the presence of a base, a copper catalyst and a palladium catalyst in an aprotic polar solvent.Type: ApplicationFiled: July 26, 2011Publication date: March 29, 2012Applicant: TAHEEBO JAPAN CO., LTD.Inventors: Akira IIDA, Kazunori UEDA, Mitsuaki YAMASHITA
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Publication number: 20120074396Abstract: 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 2, 2011Publication date: March 29, 2012Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: HONG MENG, FANPING SUN
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Publication number: 20120071673Abstract: The present invention relates in general to the field of organic chemistry and in particular to the preparation of (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4-b]furan-8-yl)ethyl]propionamide, i.e. ramelteon, and analogues thereof.Type: ApplicationFiled: February 11, 2010Publication date: March 22, 2012Applicant: LEK Pharmaceuticals D.D.Inventor: Jerome Cluzeau
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Publication number: 20120071523Abstract: The instant invention provides novel benzofuran-4,5-diones and pharmaceutical compositions thereof useful for inhibiting PDF and for treating proliferative and infectious diseases. Compounds may be selective for eukaryotic (e.g., human) PDF or prokaryotic PDF.Type: ApplicationFiled: May 5, 2010Publication date: March 22, 2012Applicant: Sloan-Kettering Institute for Cancer ResearchInventors: Hakim Djaballah, Christophe Antczak
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Patent number: 8137509Abstract: 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: GrantFiled: May 21, 2007Date of Patent: March 20, 2012Assignee: Trustees of Boston UniversityInventors: John A. Porco, Jr., Baudouin Gerard
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Patent number: 8115200Abstract: 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: GrantFiled: December 9, 2008Date of Patent: February 14, 2012Assignee: E.I. du Pont de Nemours and CompanyInventors: Hong Meng, Fanping Sun