Tricyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/458)
  • Patent number: 10329332
    Abstract: A film of the present invention contains a polypeptide derived from spider silk proteins. The decomposition temperature of the film is 240 to 260° C. The film absorbs ultraviolet light having a wavelength of 200 to 300 nm and has a light transmittance of 85% or more at a wavelength of 400 to 780 nm. The film is transparent and colorless in a visible light region. A method for producing a film of the present invention includes: dissolving a polypeptide derived from spider silk proteins in a dimethyl sulfoxide solvent to prepare a dope; and cast-molding the dope on a surface of a base. Thus, the present invention provides a spider silk protein film that can be formed easily and has favorable stretchability, and a method for producing the same.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: June 25, 2019
    Assignee: SPIBER INC.
    Inventors: Kaori Sekiyama, Mizuki Ishikawa, Shinya Murata
  • Patent number: 10294211
    Abstract: A method of isolating and purifying (?)-Ambrox from a reaction mixture comprising (?)-Ambrox and one or more of the compounds (II), (III) and (IV)
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: May 21, 2019
    Assignee: Givaudan S.A.
    Inventor: Eric Eichhorn
  • Patent number: 10246430
    Abstract: The present invention is directed to methods for preparing Beraprost and novel synthetic intermediates for Beraprost.
    Type: Grant
    Filed: May 4, 2018
    Date of Patent: April 2, 2019
    Assignee: Lung Biotechnology PBC
    Inventors: Hitesh Batra, Sudersan M. Tuladhar, Sri Harsha Tummala, Raju Penmasta, David A. Walsh
  • Patent number: 10081613
    Abstract: Compounds of the formula 1 wherein, R is hydrogen, alkyl or substituted alkyl, aryl or substituted aryl, are useful intermediates in the synthesis of fragrance ingredients such as Ambrox 2
    Type: Grant
    Filed: July 6, 2017
    Date of Patent: September 25, 2018
    Assignee: Givaudan, S.A.
    Inventors: Fridtjof Schröder, Urs Mueller, Jürg Daniel Oetiker
  • Patent number: 10005753
    Abstract: The present invention is directed to methods for preparing Beraprost and novel synthetic intermediates for Beraprost. In one aspect, a process is provided to produce a pharmaceutical compound represented by the general Formula (I) via a radical cyclization route. The process is completed in fewer steps than the known synthetic methods and may be conducted to prepare commercially useful quantities. In another aspect, synthetic methods are provided for producing Beraprost and its derivatives, which are stereoselective, efficient, scalable and economical. In another aspect, substantially isomerically pure compounds and intermediates are produced by the above processes.
    Type: Grant
    Filed: May 19, 2015
    Date of Patent: June 26, 2018
    Assignee: Lung Biotechnology PBC
    Inventors: Hitesh Batra, Sudersan M. Tuladhar, Sri Harsha Tummala, Raju Penmasta, David A. Walsh
  • Patent number: 9969706
    Abstract: An improved method is described for making single isomers of synthetic benzoprostacyclin analog 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: Grant
    Filed: February 23, 2017
    Date of Patent: May 15, 2018
    Assignee: Lung Biotechnology PBC
    Inventors: Vijay Sharma, Hitesh Batra, Sudersan Tuladhar
  • Patent number: 9834532
    Abstract: 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: Grant
    Filed: September 29, 2014
    Date of Patent: December 5, 2017
    Assignee: BOSTON BIOMEDICAL, INC.
    Inventors: Zhiwei Jiang, Chiang Jia Li, Wei Li, David Leggett
  • Patent number: 9758500
    Abstract: 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: Grant
    Filed: October 12, 2016
    Date of Patent: September 12, 2017
    Assignee: BASF SE
    Inventors: Melanie Weingarten, Hansgeorg Ernst, Wolfgang Siegel, Ekkehard Winterfeldt, Reinhard W. Hoffmann
  • Patent number: 9732056
    Abstract: Compounds of the formula 1 wherein, R is hydrogen, alkyl or substituted alkyl, aryl or substituted aryl, are useful intermediates in the synthesis of fragrance ingredients such as Ambrox 2
    Type: Grant
    Filed: September 15, 2015
    Date of Patent: August 15, 2017
    Assignee: Givaudan, S.A.
    Inventors: Fridtjof Schröder, Urs Mueller, Jurg Daniel Oetiker
  • Patent number: 9493385
    Abstract: 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: Grant
    Filed: July 21, 2015
    Date of Patent: November 15, 2016
    Assignee: BASF SE
    Inventors: Melanie Weingarten, Hansgeorg Ernst, Wolfgang Siegel, Ekkehard Winterfeldt, Reinhard W. Hoffmann
  • Patent number: 9381184
    Abstract: 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: Grant
    Filed: March 10, 2015
    Date of Patent: July 5, 2016
    Assignee: Boston Biomedical, Inc.
    Inventors: Chiang Jia Li, David Leggett, Youzhi Li, Wei Li
  • Patent number: 9376415
    Abstract: A 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: Grant
    Filed: March 24, 2010
    Date of Patent: June 28, 2016
    Assignee: NIPPON SUISAN KAISHA, LTD.
    Inventors: Seizo Sato, Fumie Iwata, Shoichi Yamada, Jiro Takeo, Akihisa Abe, Hiroyuki Kawahara
  • Patent number: 9353385
    Abstract: Provided are labdenediol diphosphate synthase polypeptides, sclareol synthase polypeptides, nucleic acid molecules encoding the labdenediol diphosphate synthase polypeptides and sclareol synthase polypeptides, and methods of using the labdenediol diphosphate synthase polypeptides, sclareol synthase polypeptides. Also provided are methods for producing labdenediol diphosphate, sclareol and (?)-ambroxide.
    Type: Grant
    Filed: July 30, 2013
    Date of Patent: May 31, 2016
    Assignee: Evolva, Inc.
    Inventors: Grace Eunyoung Park, Bryan N. Julien, Richard Burlingame
  • Patent number: 9217121
    Abstract: 4,8-Dimethyl-3,7-nonadien-2-ol in which the weight ratio of (E)-4,8-dimethyl-3,7-nonadien-2-ol to the sum of (E)- and (Z)-4,8-dimethyl-3,7-nonadien-2-ol is at least 80% or in which the weight ratio of (Z)-4,8-dimethyl-3,7-nonadien-2-ol to the sum of (E)- and (Z)-4,8-dimethyl-3,7-nonadien-2-ol is at least 80%, is used as fragrance. The fragrances have a unique rose-like, floral character. Citrus-like, minty, green accompanying notes reminiscent of rhubarb arise.
    Type: Grant
    Filed: January 24, 2014
    Date of Patent: December 22, 2015
    Inventors: Stefan Rüdenauer, Ralf Pelzer, Wolfgang Krause
  • Patent number: 9084766
    Abstract: 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: Grant
    Filed: March 21, 2011
    Date of Patent: July 21, 2015
    Assignee: Boston Biomedical, Inc.
    Inventors: Chiang Jia Li, David Leggett, Youzhi Li, Wei Li
  • Publication number: 20150142085
    Abstract: Pharmaceutical compositions and methods for treating and/or preventing age-related macular degeneration with melatonin analogues are provided.
    Type: Application
    Filed: July 21, 2014
    Publication date: May 21, 2015
    Inventors: David Baron, Keisuke Hirai, Yasushi Shintani, Osamu Uchikawa
  • Patent number: 9028977
    Abstract: The present invention relates to a novel compound of Formula 1, 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: Grant
    Filed: September 23, 2009
    Date of Patent: May 12, 2015
    Assignee: LG Chem, Ltd.
    Inventors: Jae-Soon Bae, Ji-Eun Kim, Jeung-Gon Kim, Jun-Gi Jang
  • Publication number: 20150094476
    Abstract: Compounds of the formula 1 wherein, R is hydrogen, alkyl or substituted alkyl, aryl or substituted aryl, are useful intermediates in the synthesis of fragrance ingredients such as Ambrox 2
    Type: Application
    Filed: December 8, 2014
    Publication date: April 2, 2015
    Inventors: Fridtjof SCHRÖDER, Urs MUELLER, Jürg Daniel OETIKER
  • Patent number: 8981131
    Abstract: The present invention provides compounds represented by formula I: 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: Grant
    Filed: July 25, 2008
    Date of Patent: March 17, 2015
    Assignee: Piramal Enterprises Limited
    Inventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Roda Dalal, Sapna Parikh, Aditi Amol Tannu
  • Publication number: 20150025255
    Abstract: The presently disclosed subject matter provides methods of preparing synthetic prostacyclin analogues, including Beraprost, either as racemic mixtures or as single stereoisomers. Also provided are novel synthetic intermediates for use in these methods.
    Type: Application
    Filed: September 12, 2012
    Publication date: January 22, 2015
    Applicant: Lung Biotechnology Inc.
    Inventors: George Petros Yiannikouros, Panos Kalaritis, Chaminda Priyapushpa Gamage, Denis Viktorovich Arefyev
  • Publication number: 20150018410
    Abstract: 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: Application
    Filed: September 29, 2014
    Publication date: January 15, 2015
    Inventors: Zhiwei Jiang, Chiang Jia Li, Wei Li, David Leggett
  • Patent number: 8933253
    Abstract: Compounds of the formula 1 wherein, R is hydrogen, alkyl or substituted alkyl, aryl or substituted aryl are useful intermediates in the synthesis of fragrance ingredients such as Ambrox 2.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: January 13, 2015
    Assignee: Givaudan S.A.
    Inventors: Fridtjof Schröder, Urs Mueller, Jürg Daniel Oetiker
  • Publication number: 20140357682
    Abstract: Non ligand binding pocket antagonists for the human androgen receptor. The androgen receptor (AR) is a member of the Nuclear Receptor (NR) family and its role is to modulate the biological effects of the endogenous androgens, testosterone (tes) and dihydrotestosterone (DHT). Synthetic androgens and anti-androgens have therapeutic value in the treatment of various androgen dependent conditions, from regulation of male fertility to prostate cancer. Current treatment of prostate cancer (PCa) typically involves administration of ‘classical’ antiandrogens, competitive inhibitors of natural AR ligands, DHT and tes, for the ligand binding pocket (LBP) in the C-terminal ligand binding domain (LBD) of the AR. However, prolonged LBP-targeting can often lead to androgen resistance and alternative therapies and therapeutic strategies are urgently required. Disclosed herein are a class of non-steroidal, small molecule AR antagonists which inhibit the transcriptional activity of the AR by non LBP-mediated modulation.
    Type: Application
    Filed: November 23, 2012
    Publication date: December 4, 2014
    Applicant: THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, & THE OTHER MEMBERS OF BOARD, OF THE COLLEGE OF THE HOLY
    Inventors: David George Lloyd, Darren Fayne, Mary Jane Meegan, Miriam Carr, Gemma Karena Kinsella, Laura Caboni, Wiliam Nicholas Jagoe, Billy Egan, Fernando Blanco
  • Patent number: 8877803
    Abstract: 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 aberrant Stat3 pathway activity; to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: September 10, 2008
    Date of Patent: November 4, 2014
    Assignee: Boston Biomedical, Inc.
    Inventors: Zhiwei Jiang, Chiang Jia Li, Wei Li, David Leggett
  • Patent number: 8871802
    Abstract: 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: Grant
    Filed: August 24, 2010
    Date of Patent: October 28, 2014
    Assignee: Zhoushan HaiZhongZhou Xinsheng Pharmaceuticals Co., Ltd.
    Inventors: Zhiwei Jiang, Aijin Wang, Xian Li, Qingrong Li, Hongwei Hu, Jiali Xu, Yuesong Hu, Yan Ye
  • Publication number: 20140314746
    Abstract: The invention includes novel methods of treating or preventing fibrosis in a subject afflicted with scleroderma, comprising administering to the subject a therapeutically effective amount of an agent that inhibits formation of at least one inflammasome signaling product in the subject.
    Type: Application
    Filed: March 11, 2014
    Publication date: October 23, 2014
    Applicant: Philadelphia Health and Education Corporation, d/b/a Drexel University College of Medicine
    Inventors: CAROL M. ARTLETT, PETER D. KATSIKIS
  • Publication number: 20140288314
    Abstract: A process provides for producing chiral prostacyclin derivatives of Formula (I) in high yield from meso anhydrides.
    Type: Application
    Filed: March 24, 2014
    Publication date: September 25, 2014
    Applicant: United Therapeutics Corporation
    Inventors: Hitesh Batra, Liang Guo
  • Publication number: 20140275573
    Abstract: 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: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicant: LUNG BIOTECHNOLOGY INC.
    Inventors: Vijay Sharma, Hitesh Batra, Sudersan Tuladhar
  • Publication number: 20140275578
    Abstract: Compounds of the formula 1 wherein, R is hydrogen, alkyl or substituted alkyl, aryl or substituted aryl are useful intermediates in the synthesis of fragrance ingredients such as Ambrox 2.
    Type: Application
    Filed: December 21, 2011
    Publication date: September 18, 2014
    Applicant: GIVAUDAN S.A.
    Inventors: Fridtjof Schröder, Jürg Daniel Oetiker
  • Publication number: 20140275237
    Abstract: In various embodiments the use of single isomer of beraprost as a therapeutic for the treatment of viral disease and other pathologies associated with the induction of a cytokine storm, such as influenza A viruses and the SARS-causing coronvirus and mutations thereof is provided.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: Gemmus Pharma Inc.
    Inventors: DARYL H. FAULDS, WILLIAM J. GUILFORD
  • Publication number: 20140249193
    Abstract: The present invention provides compounds that modulate protein translocation in mitochondria, compositions thereof, and methods of identifying, making and using these.
    Type: Application
    Filed: April 12, 2012
    Publication date: September 4, 2014
    Applicant: The Regents of the University of California
    Inventors: Carla M. Koehler, Samuel A. Hasson, Kiyoko Miyata, Micheal A. Teitell, Deepa Dabir
  • Publication number: 20140235879
    Abstract: 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: Application
    Filed: January 30, 2014
    Publication date: August 21, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Yutaka Tanoue, Tetsuya Matsuura, Yutaka Yamagata, Naoki Nagahara
  • Publication number: 20140235709
    Abstract: 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: Application
    Filed: January 30, 2014
    Publication date: August 21, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Yutaka Tanoue, Tetsuya Matsuura, Yutaka Yamagata, Nacki Nagahara
  • Publication number: 20140227184
    Abstract: Methods of halogenating a carbon containing compound having an sp3 C—H bond are provided. Methods of fluorinating a carbon containing compound comprising halogenation with Cl or Br followed by nucleophilic substitution with F are provided. Methods of direct oxidative C—H fluorination of a carbon containing compound having an sp3 C—H bond are provided. The halogenated products of the methods are provided.
    Type: Application
    Filed: August 20, 2012
    Publication date: August 14, 2014
    Applicant: The Trustees of Princeton University
    Inventors: John T. Groves, Wei Liu, Xiongyi Huang
  • Publication number: 20140199741
    Abstract: A process for manufacturing tetrahydrofuran, tetrahydropyran and, more generally, cycloether derivatives through the cyclodehydration of 1,4- or 1,5-diols. More specifically, the process of the invention involves (i) the stereoselective cyclodehydration in water of 1,4- or 1,5-diols including at least one chiral tertiary alcohol functional group with retention of the initial chirality, and/or (ii) the cyclodehydration in water of 1,4- or 1,5-diols, said diols being non-miscible with and/or non-soluble in water, into corresponding cycloether derivatives, by bringing the reaction mixture to high temperature water (HTW) conditions and/or by mixing the aqueous reaction mixture with a solid catalyst, such as for example a smectite clay. Also, the use of the process for manufacturing ambrafuran, especially (?)-ambrafuran and other cycloether derivatives.
    Type: Application
    Filed: July 13, 2012
    Publication date: July 17, 2014
    Applicant: KOSTE BIOCHEMICALS
    Inventor: Charles Carey
  • Patent number: 8779170
    Abstract: 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: Grant
    Filed: June 15, 2012
    Date of Patent: July 15, 2014
    Assignee: Lung Biotechnology Inc.
    Inventors: Vijay Sharma, Hitesh Batra, Sudersan Tuladhar
  • Patent number: 8765980
    Abstract: 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: Grant
    Filed: December 17, 2010
    Date of Patent: July 1, 2014
    Assignee: Givaudan S.A.
    Inventors: Fridtjof Schröder, Urs Mueller, Peter Gygax
  • Publication number: 20140179754
    Abstract: 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: Application
    Filed: October 8, 2013
    Publication date: June 26, 2014
    Applicants: NATIONAL UNIVERSITY CORPORATION KUMAMOTO UNIVERSITY, PURDUE RESEARCH FOUNDATION
    Inventors: Arun K. GHOSH, Chun-Xiao Xu, Hiroaki Mitsuya, Garth Parham
  • Patent number: 8728708
    Abstract: 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: Grant
    Filed: February 27, 2013
    Date of Patent: May 20, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Kyouhei Sakita, Wataru Kikuchi, Masatoshi Yumoto, Masanori Hikita
  • Patent number: 8703979
    Abstract: 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: Grant
    Filed: July 26, 2011
    Date of Patent: April 22, 2014
    Assignee: Taheebo Japan Co., Ltd.
    Inventors: Akira Iida, Kazunori Ueda, Mitsuaki Yamashita
  • Publication number: 20140066499
    Abstract: 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: Application
    Filed: November 13, 2013
    Publication date: March 6, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Shinichi Urayama, Eigo Mutou, Atsushi Inagaki, Takashi Okada, Shigeharu Sugisaki
  • Patent number: 8653286
    Abstract: 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: Grant
    Filed: August 7, 2012
    Date of Patent: February 18, 2014
    Assignee: Nektar Therapeutics
    Inventors: Samuel P. McManus, Antoni Kozlowski, Tracy L. Hutchison, Brian Bray, Xiaoming Shen
  • Patent number: 8642649
    Abstract: 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: Grant
    Filed: October 9, 2012
    Date of Patent: February 4, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yutaka Tanoue, Tetsuya Matsuura, Yutaka Yamagata, Naoki Nagahara
  • Patent number: 8642648
    Abstract: 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: Grant
    Filed: October 9, 2012
    Date of Patent: February 4, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yutaka Tanoue, Tetsuya Matsuura, Yutaka Yamagata, Naoki Nagahara
  • Publication number: 20130345176
    Abstract: 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: Application
    Filed: March 4, 2011
    Publication date: December 26, 2013
    Applicant: 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
  • Publication number: 20130344183
    Abstract: 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: Application
    Filed: February 16, 2012
    Publication date: December 26, 2013
    Applicant: KONKUK UNIVERSITY INDUSTRIAL COOPERATION CORP.
    Inventors: Soo Ki Kim, Jun Hyeong Lee, Hyung In moon, Sang Heui Seo, Hyun Dong Paik, Sang Buem Cho
  • Patent number: 8609871
    Abstract: 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: Grant
    Filed: August 29, 2012
    Date of Patent: December 17, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shinichi Urayama, Eigo Mutou, Atsushi Inagaki, Takashi Okada, Shigeharu Sugisaki
  • Publication number: 20130315841
    Abstract: 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: Application
    Filed: March 15, 2013
    Publication date: November 28, 2013
    Inventor: Kay M. Brummond
  • Patent number: 8586764
    Abstract: 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: Grant
    Filed: July 9, 2010
    Date of Patent: November 19, 2013
    Assignee: China National Academy of Nanotechnology and Engineering
    Inventors: Peng Wang, Yupeng Wang, Ning Cai, Wangdong Zeng, Mingfei Xu, Jingyuan Liu
  • Publication number: 20130302422
    Abstract: 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: Application
    Filed: May 22, 2013
    Publication date: November 14, 2013
    Applicants: KT & G CORPORATION, MAZENCE INC.
    Inventors: Taehwan Kwak, Myung-Gyu Park, Kyoung Hoon Jung