Chalcogen Attached Indirectly To The Lactone Ring By Acyclic Nonionic Bonding Patents (Class 549/305)
  • Patent number: 10253011
    Abstract: This present invention relates to novel Lubiprostone crystals and methods for preparing the same. The preparation methods provided by the invention can effectively reduce or eliminate impurity in the obtained Lubiprostone crystals.
    Type: Grant
    Filed: July 13, 2018
    Date of Patent: April 9, 2019
    Assignee: CHIROGATE INTERNATIONAL INC.
    Inventors: Shih-Yi Wei, Jian-Bang Jheng
  • Patent number: 9505733
    Abstract: The present invention discloses single step, highly enantioselective catalytic oxidative cyclization process for the synthesis of 3-substituted chiral phthalides. In particular, the invention discloses asymmetric synthesis of chiral phthalides via synergetic nitrile accelerated oxidative cyclization of o-cyano substituted aryl alkenes in high yield and enantiomeric excess (ee) in short reaction time. Also, disclosed herein is “one-pot” asymmetric synthesis of biologically important natural compounds having 3-substituted chiral phthalide structural framework in the molecule.
    Type: Grant
    Filed: April 23, 2015
    Date of Patent: November 29, 2016
    Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Rekula Santosh Reddy, Chithanya Kiran Indukuru Naga, Sudalai Arumugam
  • Patent number: 9073887
    Abstract: The present invention discloses single step, highly enantioselective catalytic oxidative cyclization process for the synthesis of 3-substituted chiral phthalides. In particular, the invention discloses asymmetric synthesis of chiral phthalides via synergetic nitrile accelerated oxidative cyclization of o-cyano substituted aryl alkenes in high yield and enantiomeric excess (ee) in short reaction time. Also, disclosed herein is “one-pot” asymmetric synthesis of biologically important natural compounds having 3-substituted chiral phthalide structural framework in the molecule.
    Type: Grant
    Filed: November 12, 2012
    Date of Patent: July 7, 2015
    Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Rekula Santosh Reddy, Chithanya Kiran Indukuru Naga, Sudalai Arumugam
  • Publication number: 20150139978
    Abstract: The present invention relates to a novel monascuspurpurone compound of formula (I): or a pharmaceutically acceptable derivative thereof as described in the specification, the process for preparation of the same, and the composition comprising the same. The uses of a monascuspurpurone compound for promoting adipocyte differentiation, for increasing the activity of PPAR? and/or C/EBP?, for lowering blood glucose, for preventing and/or treating a disease or disorder related to insulin resistance, and for preventing and/or treating metabolic syndrome or its complications are also provided.
    Type: Application
    Filed: October 9, 2014
    Publication date: May 21, 2015
    Inventors: Ming-Jen Cheng, Ping-Hsun Yang, Ming-Der Wu, Shie-Jea Lin, Gwo-Fang Yuan, Yen-Lin Chen, Hsuen-Chun Liao, Kai-Ping Chen
  • Publication number: 20140356361
    Abstract: This invention relates to repeated administration of antigen-specific immunotherapeutics using protocols, or elements thereof, that do not induce immunosuppression. In some embodiments, the protocol has been previously shown not to induce immunosuppression in a subject.
    Type: Application
    Filed: June 4, 2014
    Publication date: December 4, 2014
    Applicant: Selecta Biosciences, Inc.
    Inventors: Roberto A. Maldonado, Takashi Kei Kishimoto
  • Patent number: 8901319
    Abstract: A process for the synthesis and purification of F-series prostaglandin compounds and synthetic intermediates used to prepare them. The synthetic intermediates are solid and may be purified by precipitation and therefore may form the representative F-series prostaglandin compounds such as latanoprost, bimatoprost, fluprostenol, cloprostenol, and substituted analogs therefrom in highly pure forms.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: December 2, 2014
    Assignee: Cayman Chemical Company, Incorporated
    Inventors: Gilles Chambournier, Andriy Kornilov, Hussein M. Mahmoud, Ivan Vesely, Stephen D. Barrett
  • Publication number: 20140330027
    Abstract: The present invention discloses single step, highly enantioselective catalytic oxidative cyclization process for the synthesis of 3-substituted chiral phthalides. In particular, the invention discloses asymmetric synthesis of chiral phthalides via synergetic nitrile accelerated oxidative cyclization of o-cyano substituted aryl alkenes in high yield and enantiomeric excess (ee) in short reaction time. Also, disclosed herein is “one-pot” asymmetric synthesis of biologically important natural compounds having 3-substituted chiral phthalide structural framework in the molecule.
    Type: Application
    Filed: November 12, 2012
    Publication date: November 6, 2014
    Inventors: Rekula Santosh Reddy, Chithanya Kiran Indukuru Naga, Sudalai Arumugam
  • Publication number: 20140288027
    Abstract: (?)-(S)-3-(3?-hydroxy)-butylphthalide (a compound shown by Formula I) and an ester formed of the same and an acid are proved by experiments to be applicable to treatment and prevention of cerebral ischemic diseases and have a sleep-improving function. The acid refers to a pharmaceutically acceptable inorganic or organic acid. The inorganic acid refers to nitric acid, sulfuric acid, or phosphoric acid. In addition to an acid radical, the organic acid at least comprises at least one of an amino group, a hydroxyl group, and a carboxyl group. None of the compound shown by Formula I and the ester thereof is water-soluble. An ester generated from the compound and the acid further react with an acid or a base to generate a salt which is water-soluble and is used to prepare injection preparation. The experiment proves that the salt does not stimulate vessels.
    Type: Application
    Filed: September 26, 2012
    Publication date: September 25, 2014
    Inventors: Wei Wang, Yayao Zhou, Ya'nan Liu
  • Publication number: 20140142170
    Abstract: A composition and method for influencing energy metabolism and treating metabolic and other disorders is provided. A terpenoid lactone that is a selective activator of SIRT1 is generally in the form of a terpenoid dilactone having a 5-alkeny-loxy-furan-2- one group, such as strigolactone, GR 24, or another strigolactone analog, and is used as a therapeutic agent in a method for influencing energy metabolism and treating metabolic and other disorders. The terpenoid lactone may be administered as an individual agent or combined with a second compound such as a flavonoid, chalconoid, tannin, or nicotinamide inhibition antagonist.
    Type: Application
    Filed: October 27, 2011
    Publication date: May 22, 2014
    Applicant: SIRTUIN VALLEY OY
    Inventors: Markku Laakso, Nagendra Yaluri
  • Patent number: 8569405
    Abstract: The invention describes a process for reducing the amount of saturated or unsaturated monomers and oligomers during production and processing of styrenic polymers comprising a mixture of at least two components selected from the group consisting of a) phenol thioethers, b) phenol acrylates, c) 3-arylbenzofuran-2-ones and d) 1,1-di-substituted ethylenes or tri-substituted ethylenes.
    Type: Grant
    Filed: January 19, 2009
    Date of Patent: October 29, 2013
    Assignee: BASF SE
    Inventors: Alex Wegmann, Sunghee Kim, Michèle Gerster
  • Publication number: 20130267717
    Abstract: Disclosed herein is novel process for preparation of atovaquone, which process includes reacting 1H-2-benzopyran-1,4(3H)-dione with 4-(4-chlorophenyl)cyclohexanecarbaldehyde. The invention further discloses novel intermediates useful in the preparation of atovaquone.
    Type: Application
    Filed: December 13, 2011
    Publication date: October 10, 2013
    Applicant: GLAXO GROUP LIMITED
    Inventors: Andrew Neil Dwyer, Andrew Gordon, Michael Urquhart
  • Publication number: 20130072519
    Abstract: Compounds of Formula I that inhibit microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion and their uses in the treatment of diseases linked thereto in animals are described herein.
    Type: Application
    Filed: May 9, 2011
    Publication date: March 21, 2013
    Inventors: Edward Lee Conn, David Hepworth, Yingmei Qi, Benjamin Neil Rocke, Roger Benjamin Ruggeri, Yan Zhang
  • Patent number: 8394844
    Abstract: Provided is a compound represented by the formula (1): wherein R1 and R2 are each independently a hydrogen atom or a straight chain alkyl group having a carbon number of 1-3, R3 is a hydrogen atom, an alkyl group having a carbon number of 1 -4, an alkoxyalkyl group, an aryl group, a halogen atom or a haloalkyl group, or a pharmaceutically acceptable salt thereof, which has, unlike known PGI2 analogs, a selective EP4 agonist action, and a medicament containing the compound, which is useful for the prophylaxis and/or treatment of immune diseases, diseases of the digestive tract, cardiovascular diseases, cardiac diseases, respiratory diseases, neurological diseases, ophthalmic diseases, renal diseases, hepatic diseases, bone diseases, skin diseases and the like.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: March 12, 2013
    Assignees: Asahi Glass Company, Limited, Kaken Pharmaceutical Co., Ltd.
    Inventors: Takahiko Murata, Masahiro Amakawa, Shin Teradaira, Yasushi Matsumura, Katsuhiko Konishi
  • Publication number: 20130005976
    Abstract: A process for preparing [(1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, by the resolution of racemic 4-oxo-1,2-cyclopentanedicarboxylic acid (V), said process comprising: (a) reacting 4-oxo-1,2-cyclopentanedicarboxylic acid (V) with brucine or (1R,2S)-(?)-ephedrine, thus preparing the bis-brucine or bis-(1R,2S)-(?)-ephedrine salt of (V), and (b) precipitating selectively the bis-brucine or bis-(1R,2S)-(?)-ephedrine salt of (1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, while the bis-brucine or bis-(1R,2S)-(?)-ephedrine salt of [(1S,2S)-4-oxo-1,2-cyclopentanedicarboxylic acid stays in solution; (c) liberating the acid II by removal of brucine or (1R,2S)-(?)-ephedrine from the precipitated salt obtained in step (b).
    Type: Application
    Filed: March 16, 2011
    Publication date: January 3, 2013
    Applicant: JANSSEN PHARMACEUTICALS, INC.
    Inventors: Dominic John Ormerod, Dominique Paul Michel Depre, Andras Horvath
  • Publication number: 20120283451
    Abstract: A process for the synthesis and purification of F-series prostaglandin compounds and synthetic intermediates used to prepare them. The synthetic intermediates are solid and may be purified by precipitation and therefore may form the representative F-series prostaglandin compounds such as latanoprost, bimatoprost, fluprostenol, cloprostenol, and substituted analogs therefrom in highly pure forms.
    Type: Application
    Filed: October 16, 2009
    Publication date: November 8, 2012
    Inventors: Gilles Chambournier, Andriy Kornilov, Hussein M. Mahmoud, Ivan Vesely, Stephen D. Barrett
  • Publication number: 20120164120
    Abstract: The present invention relates to a novel monascuspurpurone compound of formula (I): or a pharmaceutically acceptable derivative thereof as described in the specification, the process for preparation of the same, and the composition comprising the same. The uses of a monascuspurpurone compound for promoting adipocyte differentiation, for increasing the activity of PPAR? and/or C/EBP?, for lowering blood glucose, for preventing and/or treating a disease or disorder related to insulin resistance, and for preventing and/or treating metabolic syndrome or its complications are also provided.
    Type: Application
    Filed: December 23, 2011
    Publication date: June 28, 2012
    Applicant: FOOD INDUSTRY RESEARCH AND DEVELOPMENT INSTITUTE
    Inventors: Ming-Jen Cheng, Ping-Hsun Yang, Ming-Der Wu, Shie-Jea Lin, Gwo-Fang Yuan, Yen-Lin Chen, Hsuen-Chun Liao, Kai-Ping Chen
  • Publication number: 20120135347
    Abstract: There are provided a resist composition, a method of forming a resist pattern using the resist composition, a novel polymeric compound and a compound useful as a monomer for the polymeric compound, the resist composition including a base component (A) that exhibits changed solubility in a developing solution under action of acid and an acid generator component (B) that generates acid upon exposure, wherein the base component (A) contains a resin component (A0) including a structural unit (a0) represented by general formula (a0) shown below [wherein A represents a divalent linking group; and R1 represents a hydrogen atom or a hydrocarbon group of 1 to 6 carbon atoms which may have a substituent.
    Type: Application
    Filed: November 28, 2011
    Publication date: May 31, 2012
    Applicant: Tokyo Ohka Kogyo Co., Ltd.
    Inventors: Yoshiyuki UTSUMI, Takehiro SESHIMO, Tomoyuki HIRANO, Daichi TAKAKI, Junichi TSUCHIYA
  • Patent number: 8177896
    Abstract: A novel chemical genus of furan-2-one antifouling compound as non-toxic, environment friendly antifouling agent, a coating material for objects submerged under the water based on the furan-2-one compounds. The substituted furan-2-one antifouling compounds have a furan-2-one ring and an alkyl side chain thereto and are of the formula: where n=6-14, representing the number of carbon atoms in said side chain.
    Type: Grant
    Filed: April 16, 2009
    Date of Patent: May 15, 2012
    Assignee: The Hong Kong University of Science and Technology
    Inventors: Peiyuan Qian, Ying Xu, Xiaojian Zhou, Hongping He, Nobuhiro Fusetani, Wei-Min Dai
  • Publication number: 20120088869
    Abstract: Organic materials which possess outstanding stability to oxidative, thermal or light-induced degradation comprise as stabilizers at least one compound of the formula I wherein the general symbols are as defined in claim 1. The compounds of formula I are especially useful as stabilizers for protecting polymers and lubricants against oxidative, thermal or light-induced degradation and as scavengers for oxidized developer in color photographic material.
    Type: Application
    Filed: December 20, 2011
    Publication date: April 12, 2012
    Inventors: Michèle GERSTER, Peter NESVADBA
  • Publication number: 20120004232
    Abstract: A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.
    Type: Application
    Filed: September 8, 2011
    Publication date: January 5, 2012
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Akito YASUHARA, Kazunari SAKAGAMI, Hiroshi OHTA, Atsuro NAKAZATO
  • Patent number: 7994162
    Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide benzodiazepine compounds, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.
    Type: Grant
    Filed: November 10, 2008
    Date of Patent: August 9, 2011
    Assignee: Sanofi-Aventis
    Inventors: Jidong Zhang, Frederico Nardi, Alain Commerçon
  • Publication number: 20110166347
    Abstract: The present invention discloses an isolation and purification process for mycophenolic acid obtained from the fermentation process. Invention further discloses preparation of sodium salt of mycophenolic acid and mycophenolate mofetil from mycophenolic acid.
    Type: Application
    Filed: September 9, 2009
    Publication date: July 7, 2011
    Applicant: IPCA Laboratories Ltd.
    Inventors: Ashok Kumar, Dharmendra Singh, Umesh Luthara, Yogesh Mohandhai Patel
  • Publication number: 20110059907
    Abstract: This invention relates to certain complexes of ascorbic acid and its derivatives with certain natural antioxidant and anti-inflammatory ketones for topical or oral application; said complexes having general chemical formula (I), its isomers, and salts thereof, including their optically active or racemic forms.
    Type: Application
    Filed: November 16, 2010
    Publication date: March 10, 2011
    Applicant: Island Kinetics Inc.
    Inventors: SHYAM K. GUPTA, Linda Walker
  • Publication number: 20110028712
    Abstract: The present invention relates to a salt of a carboxylic acid with a diamine such as 2,2?-(ethylenedioxy)diethyl amine, 3,3?-(ethylenedioxy)dipropyl amine and 2,2?-oxybis(ethylamine) and a method of preparing such salts. Preferably the carboxylic acid is a fermentation product such as clavulanic acid, mycophenolic acid or pravastatin.
    Type: Application
    Filed: March 31, 2009
    Publication date: February 3, 2011
    Inventors: Robertus Mattheus De Pater, Adrianus Antonius Wijk Van, Piotr Wnukowski
  • Publication number: 20100323999
    Abstract: Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) as defined herein, is provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as part of a combination therapy. Novel heterocyclic compounds are also provided for.
    Type: Application
    Filed: March 22, 2010
    Publication date: December 23, 2010
    Inventors: Eric Francis Morand, Magdy Naguib Iskander, Basil Danylec
  • Publication number: 20100273824
    Abstract: The present invention relates to compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.
    Type: Application
    Filed: January 18, 2008
    Publication date: October 28, 2010
    Applicant: EVOLVA SA
    Inventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Mainkar S. Prathama
  • Publication number: 20100204489
    Abstract: Disclosed is a method for preparing a prostaglandin derivative of formula (A): which comprises reacting an aldehyde represented by formula (1): with a 2-oxoalkyl phosphonate in a reaction solvent under the presence of alkali hydroxide as sole base. By carrying out the reaction using an alkali hydroxide as sole base in the reaction system, the desired prostaglandin derivative can be obtained by simple procedures and with high yield.
    Type: Application
    Filed: April 19, 2010
    Publication date: August 12, 2010
    Applicants: SUCAMPO AG, R-TECH UENO, LTD.
    Inventors: Ryu HIRATA, Tatsuya Matsukawa, Kazuhiro Masuzaki, Ryuji Ueno
  • Publication number: 20100184852
    Abstract: The present invention refers to compounds of the general formula (I) wherein R1 is hydrogen or hydroxy; R2 is butyl or butyryl if R1 is hydroxy, but R2 is butyl if R1 is hydrogen; or R3 and R2 taken together are 1-propylidene or 1-butylidene optionally substituted by hydroxy, methyl, or 3-(?, ?-dimethylacryloyloxy); the dotted line is an optional bond; X is an optionally substituted aliphatic C4-residue selected from the group consisting of X1, X2, X3, X4, and X5; wherein X is X2, X3 or X5 if the dotted line in formula (I) is absent; and X is X1, X4 or X5 if the dotted line signifies a bond in formula (I) above; R3 and R4 are, independently from each other, hydrogen or hydroxy; and R5 is hydroxy or butyryl, for use in the treatment of disorders connected to impaired neurotransmission, as well as to dietary and pharmaceutical compositions containing such compounds, and their uses.
    Type: Application
    Filed: August 10, 2007
    Publication date: July 22, 2010
    Inventors: Antoine De Saizieu, Regina Goralczyk, Goede Schueler
  • Publication number: 20100104979
    Abstract: Compounds of the Formula (I) wherein x is an integer from 1-4; p is an integer from 1-3; q is an integer from 0-3; Ar is phenyl, naphthyl, anthryl or phenanthryl each of which optionally is substituted by one or more Cl, CN, OR5, C3-C5alkenyl or C1-C6alkyl which optionally is substituted by one or more OR6, COOR or halogen; R1 if x is 1, is ORS, O—X+, NR8R9, C1-C20alkyl optionally substituted by one or more COOR10, or is C2-C20alkyl interrupted by one ore more O, or is C2-C5alkenyl or phenyl-C1-C4alkyl; R1 if x is 2, is for example C1-C20alkylene; R1 if x is 3, is for example a tri-valent radical; R1if x is 4, is for example a tetravalent radical; R2and R3are hydrogen or C1-C8alkyl, or R2and R3 together are O, C1-C3alkylene or CH?CH; R4 is C1-C4alkyl; R5, R6, R7, R8, R9 and R10 are for example hydrogen or C1-C4alkyl; and X is a x-valent cationic counter ion; are in particular suitable as photoinitiators for the curing with UV-A light (320-450 nm).
    Type: Application
    Filed: March 25, 2008
    Publication date: April 29, 2010
    Inventors: Kurt Dietliker, Peter Murer, Rinaldo Hüsler, Tunja Jung
  • Patent number: 7626024
    Abstract: The present invention provides novel processes for the preparation of a cyclopentanone of Formula II and a lactone of Formula I, which are useful in the production of prostaglandins: wherein Z, R2, R3, X1, X2, and are as defined in the specification. The invention also provides novel enantiomerically enriched compounds.
    Type: Grant
    Filed: October 9, 2007
    Date of Patent: December 1, 2009
    Assignee: Irogate International Inc.
    Inventors: Shih-Yi Wei, Yu-Chih Yeh
  • Publication number: 20090233242
    Abstract: Lactone-containing compounds having formula (1) are novel wherein R1 is H, F, methyl or trifluoromethyl, R2 and R3 are H or monovalent hydrocarbon groups, or R2 and R3 may together form an aliphatic hydrocarbon ring, R4 is H or CO2R5, R5 is a monovalent hydrocarbon group, W is CH2, O or S, and k1 is 3, 4 or 5. They are useful as monomers to produce polymers which are transparent to radiation ?500 nm. Radiation-sensitive resist compositions comprising the polymers as base resin exhibit excellent properties including resolution, LER, pattern density dependency and exposure margin.
    Type: Application
    Filed: March 12, 2009
    Publication date: September 17, 2009
    Inventors: Koji HASEGAWA, Satoshi SHINACHI, Katsuhiro KOBAYASHI, Tsunehiro NISHI, Takeshi KINSHO
  • Patent number: 7582779
    Abstract: The present invention provides novel processes for the preparation of a cyclopentanone of Formula II and a lactone of Formula I, which are useful in the production of prostaglandins: wherein Z, R2, R3, X1, X2, and are as defined in the specification. The invention also provides novel enantiomerically enriched compounds.
    Type: Grant
    Filed: October 9, 2007
    Date of Patent: September 1, 2009
    Assignee: Chirogate International Inc.
    Inventors: Shih-Yi Wei, Yu-Chih Yeh
  • Patent number: 7576213
    Abstract: A hitherto unknown class of chemical compounds, 2H-furo[2,3-c]pyran-2-ones including derivatives and analogues thereof are disclosed herein. Methods for making compounds within said class are disclosed herein and includes, without limitation, at least the intermediates employed in the generation of said compounds. The invention also relates to the use of vinylogous 4H-pyrones, including but not limited to the hitherto unknown 2H-furo[2,3-c]pyran-2-ones. Disclosed herein are methods comprising the step of exposing biological plant material to at least a compound of the invention to promoting bioactivity within said material. In another aspect in methods for promoting growth of plant material in, for example, smoke-responsive plant species by exposing said material to a compound of the invention are disclosed herein. More specifically, methods comprising the use of these compounds for promoting seed germination of a plant, for example, a smoke-responsive plant, are disclosed herein.
    Type: Grant
    Filed: June 19, 2006
    Date of Patent: August 18, 2009
    Assignee: The University of Western Australia
    Inventors: Gavin Ray Flematti, Emilio Luciano Ghisalberti, Kingsly Wayne Dixon, Robert Donald Trengove
  • Patent number: 7569576
    Abstract: The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: August 4, 2009
    Assignee: XenoPort, Inc.
    Inventors: Mark A Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat
  • Publication number: 20090143340
    Abstract: Pyrocatechin derivatives of formula I wherein R illustrates a group of formulae Ia, Ib, Ic or Id R1 is 4-halogen-but-2-enyl, R2 is lower alkyl or cycloalkyl, R3 is lower alkoxy and R4 is lower alkoxy lower alkoxy, or, where R is a group of formula (Ia), it is hydroxy, hydroxy lower alkoxy or a group of formula Ie R5 is reactive esterified hydroxy, R6 is azido and R7 is lower alkyl, lower alkenyl, cycloalkyl or aryl lower alkyl, and their salts, are valuable intermediates in the production of active ingredients for medicaments.
    Type: Application
    Filed: July 10, 2006
    Publication date: June 4, 2009
    Inventors: Gottfried Sedelmeier, Kurt Nebel, Siem Jacob Veenstra, Janos Zergenyi
  • Publication number: 20090112002
    Abstract: A process for the preparation of L-gluconic acid or a salt thereof, comprises treating an aqueous solution of 6-bromo-6-deoxy-2,3-anhydro-D-manno-1,4-lactone with a base at a pH of at least 12 and at a temperature of 45 to 55° C. to obtain an aqueous solution of L-gluconic acid.
    Type: Application
    Filed: October 31, 2007
    Publication date: April 30, 2009
    Inventors: Alexander Charles Weymouth-Wilson, Robert Clarkson
  • Patent number: 7439373
    Abstract: Provided are crystalline mycophenolate sodium forms and processes for their preparation.
    Type: Grant
    Filed: July 20, 2005
    Date of Patent: October 21, 2008
    Assignee: TEVA Gyógyszergyár Zártkörúen Múködö Részvénytársaság
    Inventors: Sandor Molnar, Csaba Szabo, Tivadar Tamas, Janos Hajko, Adrienne Kovacsne-Mezei, Judith Aronhime
  • Publication number: 20080255228
    Abstract: This invention relates to certain complexes of ascorbic acid and its derivatives with certain aryl alkyl ketones; said complexes having being formed via a kinetically-controlled process, and having general chemical formula (I) in FIG. 1. Said complexes can be in their various optically active or racemic forms. This invention also relates to a method of treatment of skin condition, including dark skin, age spots, acne, inflammation, loss of cellular antioxidants, collagen loss with aging, loss of skin pliability, loss of skin suppleness, skin wrinkles, oxidation, damage from radiation, malfunction of matrix metalloproteases, malfunction of tyrosinases, damage from free radicals, photo-damage, and combinations thereof; [FIG. 1].
    Type: Application
    Filed: June 16, 2008
    Publication date: October 16, 2008
    Applicant: BIODERM RESEARCH
    Inventor: SHYAM K. GUPTA
  • Publication number: 20080254520
    Abstract: The present invention relates to methods for reducing impurities of mycophenolic acid during fermentation by controlling the level of carbon source during fermentation of mycophenolic acid and for the isolation and use as a standard marker of the impurity homo-mycophenolic acid.
    Type: Application
    Filed: April 11, 2008
    Publication date: October 16, 2008
    Inventors: Eva Gulyas, Gabor Balogh, Janos Erdei, Laszlo Toth, Boglarka Szikszai, Alexandr Jegorov, Jiri Faustmann
  • Publication number: 20080249319
    Abstract: There is described a process for the preparation of 5-carboxy phthalide, which comprises adding terephthalic acid to fuming sulfuric acid containing at least 20% of SO3, then adding formaldehyde to the mixture, heating the mixture at a temperature of 120-145° C. and isolating 5-carboxyphthalide from the reaction mixture.
    Type: Application
    Filed: October 22, 2007
    Publication date: October 9, 2008
    Inventors: Leone Dall'Asta, Umberto Casazza, Giovanni Cotticelli
  • Publication number: 20080242713
    Abstract: This invention is directed to compounds of formula (I): where A, B, D, E, m, and R1-R5 are as described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, clathrates, or prodrugs thereof, which compounds are useful in treating autoimmune diseases. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
    Type: Application
    Filed: March 27, 2008
    Publication date: October 2, 2008
    Inventors: William Guilford, Werner Skuballa, Daryl H. Faulds, Monica Kochanny, Wheeseong Lee, Bernd Raduchel
  • Publication number: 20080033176
    Abstract: A method for preparing a prostaglandin derivative represented by the following general formula (I): (wherein Ph represents phenyl group, R1 represents a C1-7 alkyl group, a C1-7 alkenyl group, phenyl group, or benzyl group), which comprises the successive steps (1) to (8) described in the specification, or any one step or two or more successive steps selected from the group consisting of the steps (1) to (8). A method for efficiently, inexpensively and safely preparing prostaglandin derivatives, of which typical example is latanoprost, is provided.
    Type: Application
    Filed: March 20, 2007
    Publication date: February 7, 2008
    Applicant: DAIICHI FINE CHEMICAL CO., LTD.
    Inventors: Noriaki MURATA, Atsunori ARAMATA
  • Patent number: 7282596
    Abstract: A method for preparing a prostaglandin F-type compound. Also disclosed is an intermediate of the following formula (II) compound wherein R?, X and A have the same meaning as given in the specification.
    Type: Grant
    Filed: April 11, 2005
    Date of Patent: October 16, 2007
    Assignee: Everlight USA, Inc.
    Inventors: Rung-Tian Suen, Yu-Liang Liu
  • Patent number: 7276533
    Abstract: This invention features the use of the spirolaxine of formula (I) for the treatment of those pathologies responding to the activation of the PPAR? receptor, such as the Type 2 insulin-resistant diabetes. This invention also features a pharmaceutical composition in which the spirolaxine of formula (I) acts as active principle in association with the all-trans retinoic acid of formula (II) for the treatment of those pathologies responding to the activation of the PPAR? receptor, such as the acute malignant haemopathies.
    Type: Grant
    Filed: July 13, 2004
    Date of Patent: October 2, 2007
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Claudio Pisano, Teresa Riccioni
  • Patent number: 7268239
    Abstract: Disclosed are processes for the synthesis and purification of prostaglandins and analogues thereof, especially analogues of PGF2?.
    Type: Grant
    Filed: July 27, 2005
    Date of Patent: September 11, 2007
    Assignee: Resolution Chemicals Limited
    Inventors: Alan Kenneth Greenwood, Derek McHattie, David George Thompson, Derek Clissold
  • Patent number: 7145020
    Abstract: This invention is drawn to compounds which are more easily metabolized by the metabolic drug detoxification systems. Particularly, warfarin analogs which have been designed to include esters within the structure of the compounds are taught. The invention teaches methods of reducing the toxicity of drugs comprising the introduction of ester groups into drugs during the synthesis of the drug. This invention is also drawn to methods of treating coagulation disorders comprising the administration of compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester containing warfarin, analogs are also taught.
    Type: Grant
    Filed: April 8, 2004
    Date of Patent: December 5, 2006
    Assignee: Aryx Therapeutics
    Inventors: Pascal Druzgala, Xiaoming Zhang, Jurg R. Pfiste
  • Patent number: 7122687
    Abstract: In one aspect, the present invention provides a process for producing a sodium salt of an immunosupressant of Formula I
    Type: Grant
    Filed: August 29, 2002
    Date of Patent: October 17, 2006
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Acharya Poornaprajna, Gopeekrishnan Sreenilayam, Sambasivam Ganesh
  • Patent number: 7026351
    Abstract: The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.
    Type: Grant
    Filed: March 20, 2003
    Date of Patent: April 11, 2006
    Assignee: Xenoport, Inc.
    Inventors: Mark A Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat
  • Patent number: 6992197
    Abstract: A novel monomer compound having a lactone moiety of the present invention can be converted into polymers usable as resist materials with excellent properties, etc., and an alcohol compound having a lactone moiety of the invention is useful as a material for the monomer compound. The compounds are represented by the following general formula [1]: wherein one of R1 and R2 represents a hydrogen atom, an acryloyl group, or a methacryloyl group, and the other represents an alkyl group; R3 and R4 independently represent a hydrogen atom or an alkyl group; R5 and R6 both represent a hydrogen atom or are combined to form a methylene chain that may have an alkyl group; and R7 and R8 independently represent a hydrogen atom or a methyl group.
    Type: Grant
    Filed: June 10, 2004
    Date of Patent: January 31, 2006
    Assignee: Takasago International Corporation
    Inventors: Junji Nakamura, Shigetaka Numasawa, Hiroyuki Kenmochi, Yoji Hori
  • Patent number: RE39755
    Abstract: A product corresponding to formula (I) or its ketonic tautomer form (II) which is 3-(1-hydroxy-pentylidene)-5-nitro-3H-benzofuran-2-one, a process for the preparation and use of the product corresponding to formula (I) or its tautomeric form (II), a process for the preparation and use, particularly for the production of synthesis intermediates.
    Type: Grant
    Filed: February 3, 2005
    Date of Patent: July 31, 2007
    Assignee: Clariant France
    Inventors: Alan Schouteeten, Francoise Mordacq