Additional Chalcogen Bonded Directly To The Bicyclo Ring System Patents (Class 549/310)
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Publication number: 20150045564Abstract: The present invention disclosed herein is a novel commercially feasible, one pot synthesis of library of 3-substituted phthalides of formula I via CuCN mediated oxidative cyclization in high yield.Type: ApplicationFiled: January 3, 2013Publication date: February 12, 2015Inventors: Santhosh Rekula Reddy, Kishore Prasad Pragati, Kiran Naga, Arumugam Sudalai
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Publication number: 20140274936Abstract: A coordination complex having a physiologically acceptable pKa includes a metal and a biologically active agent. The pKa of the coordination complex is less than the pKa of the biologically active agent. A pharmaceutical solution for treating a patient includes a coordination complex and water, wherein the coordination complex is at least partially soluble in the water at physiological pH and in a therapeutically efficacious concentration. A method for treating a patient includes administering a pharmaceutical solution including a coordination complex and water to a patient in need of a biologically active agent.Type: ApplicationFiled: May 29, 2014Publication date: September 18, 2014Applicant: SYNTHONICS, INC.Inventors: Thomas Piccariello, John D. Price, Robert A. Oberlender, Michaela E. Mulhare, Mary C. Spencer, Scott B. Palmer
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Patent number: 8703814Abstract: The present invention relates to pharmaceutical and food compositions for preventing or treating diabetes or obesity, and more particularly to pharmaceutical compositions and functional foods for preventing or treating diabetes or obesity, which contain, as an active ingredient, a novel compound synthesized from a compound separated from an extract of the Stereocaulon alpinum. The novel compounds of the invention have very excellent PTP-1b (protein tyrosine phosphatase-1b) inhibitory activities, act selectively only on PTP-1b among protein tyrosine phosphatases, and are substantial PTP-1b inhibitors which are effective in preventing or treating diabetes or obesity.Type: GrantFiled: May 22, 2013Date of Patent: April 22, 2014Assignee: Korea Ocean Research and Development InstituteInventors: Joung Han Yim, Il Chan Kim, Doc Kyu Kim, Se Jong Han, Hyoung Seok Lee, Bhattarai Hari Datta, Jung Eun Kim, Tai Kyoung Kim, Hyun Cheol Oh, Dong-Gyu Jo, Cheolsoon Lee, Keun-Sik Kim, Pyung Cheon Lee, Mi Ra Park, Yu-Kyung Park, Sung Jin Kim, Pil-Sung Kang, Heeyong Park, Ha Ju Park
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Patent number: 8697745Abstract: The present invention relates to pharmaceutical and food compositions for preventing or treating diabetes or obesity, and more particularly to pharmaceutical compositions and functional foods for preventing or treating diabetes or obesity, which contain, as an active ingredient, a novel compound synthesized from a compound separated from an extract of the Stereocaulon alpinum. The novel compounds of the invention have very excellent PTP-1b (protein tyrosine phosphatase-1b) inhibitory activities, act selectively only on PTP-1b among protein tyrosine phosphatases, and are substantial PTP-1b inhibitors which are effective in preventing or treating diabetes or obesity.Type: GrantFiled: May 22, 2013Date of Patent: April 15, 2014Assignee: Korea Ocean Research InstituteInventors: Joung Han Yim, Il Chan Kim, Doc Kyu Kim, Se Jong Han, Hyoung Seok Lee, Bhattarai Hari Datta, Jung Eun Kim, Tai Kyoung Kim, Hyun Cheol Oh, Dong-Gyu Jo, Cheolsoon Lee, Keun-Sik Kim, Pyung Cheon Lee, Mi Ra Park, Yu-Kyung Park, Sung Jin Kim, Pil-Sung Kang, Heeyong Park, Ha Ju Park
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Publication number: 20140094514Abstract: The present invention relates to pharmaceutical and food compositions for preventing or treating diabetes or obesity, and more particularly to pharmaceutical compositions and functional foods for preventing or treating diabetes or obesity, which contain, as an active ingredient, a novel compound synthesized from a compound separated from an extract of the Stereocaulon alpinum. The novel compounds of the invention have very excellent PTP-1b (protein tyrosine phosphatase-1b) inhibitory activities, act selectively only on PTP-1b among protein tyrosine phosphatases, and are substantial PTP-1b inhibitors which are effective in preventing or treating diabetes or obesity.Type: ApplicationFiled: May 22, 2013Publication date: April 3, 2014Applicant: Korea Ocean Research and Development InstituteInventors: Joung Han YIM, Il Chan KIM, Doc Kyu KIM, Se Jong HAN, Hyoung Seok LEE, Bhattarai HARI DATTA, Jung Eun KIM, Tai Kyoung KIM, Hyun Cheol OH, Dong-Gyu JO, Cheolsoon LEE, Keun-Sik KIM, Pyung Cheon LEE, Mi Ra PARK, Yu-Kyung PARK, Sung Jin KIM, Pil-Sung KANG, Heeyong PARK, Ha Ju PARK
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Publication number: 20140073614Abstract: The present invention relates to pharmaceutical and food compositions for preventing or treating diabetes or obesity, and more particularly to pharmaceutical compositions and functional foods for preventing or treating diabetes or obesity, which contain, as an active ingredient, a novel compound synthesized from a compound separated from an extract of the Stereocaulon alpinum. The novel compounds of the invention have very excellent PTP-1b (protein tyrosine phosphatase-1b) inhibitory activities, act selectively only on PTP-1b among protein tyrosine phosphatases, and are substantial PTP-1b inhibitors which are effective in preventing or treating diabetes or obesity.Type: ApplicationFiled: May 22, 2013Publication date: March 13, 2014Applicant: Korea Ocean Research and Development InstituteInventors: Joung Han YIM, Il Chan KIM, Doc Kyu KIM, Se Jong HAN, Hyoung Seok LEE, Bhattarai HARI DATTA, Jung Eun KIM, Tai Kyoung KIM, Hyun Cheol OH, Dong-Gyu JO, Cheolsoon LEE, Keun-Sik KIM, Pyung Cheon LEE, Mi Ra PARK, Yu-Kyung PARK, Sung Jin KIM, Pil-Sung KANG, Heeyong PARK, Ha Ju PARK
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Publication number: 20130273114Abstract: The present invention describes immunosuppressant pharmaceutical formulations particularly formulations of mycophenolate salts with pulsatile release behaviour.Type: ApplicationFiled: January 18, 2012Publication date: October 17, 2013Applicant: EMS S.A.Inventors: Giancarlo Santus, Giuseppe Soldati
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Patent number: 8518302Abstract: 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: GrantFiled: December 20, 2011Date of Patent: August 27, 2013Assignee: BASF SEInventors: Michèle Gerster, Peter Nesvadba
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Patent number: 8350060Abstract: 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: GrantFiled: September 8, 2011Date of Patent: January 8, 2013Assignee: Taisho Pharamceutical Co., Ltd.Inventors: Akito Yasuhara, Kazunari Sakagami, Hiroshi Ohta, Atsuro Nakazato
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Patent number: 8124795Abstract: A process for modifying the crystal habit of acicular drug substances, crystals obtained by such a process, and particular crystal forms or modifications of mycophenolic acid or mycophenolate sodium are provided, as well as pharmaceutical compositions comprising the crystals, methods of treatment and uses thereof.Type: GrantFiled: August 4, 2011Date of Patent: February 28, 2012Assignee: Novartis AGInventors: Sabine Pfeffer, Dierk Wieckhusen
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Patent number: 8105504Abstract: 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: GrantFiled: August 22, 2005Date of Patent: January 31, 2012Assignee: BASF SEInventors: Michèle Gerster, Peter Nesvadba
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Publication number: 20110288313Abstract: A process for modifying the crystal habit of acicular drug substances, crystals obtained by such a process, and particular crystal forms or modifications of mycophenolic acid or mycophenolate sodium are provided, as well as pharmaceutical compositions comprising the crystals, methods of treatment and uses thereof.Type: ApplicationFiled: August 4, 2011Publication date: November 24, 2011Inventors: Sabine Pfeffer, Dierk Wieckhusen
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Publication number: 20110288053Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: July 20, 2011Publication date: November 24, 2011Applicant: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, Carina Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Heolun Jin, Ralph F. Hirschmann, Alan X. Huang, Choung U. Kim, Thorsten Kirschberg, Christopher P. Lee, William A. Lee, Richard L. Mackman, David Y. Markevitch, David A. Oare, Vidya K. Prasad, Hyung-Jung Pyun, Adrian S. Ray, Rosemarie Sherlock, Sundaramoothi Swaninathan, William J. Watkins, Jenneifer Zhang
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Publication number: 20110213028Abstract: The invention relates to fatty acid mycophenolate derivatives; compositions comprising an effective amount of a fatty acid mycophenolate derivative; and methods for treating and preventing organ rejection and autoimmune diseases such as systemic lupus erythematosus, psoriasis and multiple sclerosis comprising the administration of an effective amount of a fatty acid mycophenolate derivative.Type: ApplicationFiled: February 25, 2011Publication date: September 1, 2011Applicant: CATABASIS PHARMACEUTICALS, INC.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Patent number: 8008511Abstract: A process for modifying the crystal habit of acicular drug substances, crystals obtained by such a process, and particular crystal forms or modifications of mycophenolic acid or mycophenolate sodium are provided, as well as pharmaceutical compositions comprising the crystals, methods of treatment and uses thereof.Type: GrantFiled: December 18, 2008Date of Patent: August 30, 2011Assignee: Novartis AGInventors: Sabine Pfeffer, Dierk Wieckhusen
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Publication number: 20100298427Abstract: The present invention relates to the use of compounds of the formula (I) wherein the clotted line is an optional bond; R1 is butyl or butyryl if R2 is hydroxyl but is butyl if R2 is hydrogen; or R1 and R2 taken together are 1-butylidene optionally substituted by hydroxyl, methyl, or 3-(?,?-dimethylacrylyloxy)-pentylidenyl; X is a 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 is hydroxyl or butyryl; and n is 1 or 2, as agents for the prevention, control and treatment of conditions requiring modulation of inflammation in mammals. In another aspect, the present invention relates to the use of compounds of the formula (I) as active ingredients in the manufacture of medicaments/compositions for the prevention, control and treatment of conditions requiring modulation of inflammation.Type: ApplicationFiled: June 18, 2010Publication date: November 25, 2010Applicant: DSM IP ASSETS B.V.Inventors: Ann Fowler, Daniel Raederstorff, Goede Schuler, Joseph Schwager
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Publication number: 20100184852Abstract: 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: ApplicationFiled: August 10, 2007Publication date: July 22, 2010Inventors: Antoine De Saizieu, Regina Goralczyk, Goede Schueler
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Patent number: 7704995Abstract: This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such compounds. Even more specifically, the invention relates to compounds that inhibit, regulate and/or modulate kinases, particularly Checkpoint Kinases, even more particularly Checkpoint Kinase 1, or Chk1. Methods of therapeutically or prophylactically using the compounds and compositions to treat kinase-dependent diseases and conditions are also an aspect of the invention, and include methods of treating cancer, as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, by administering effective amounts of such compounds.Type: GrantFiled: May 2, 2003Date of Patent: April 27, 2010Assignee: Exelixis, Inc.Inventors: Chris A. Buhr, Tae-Gon Baik, Sunghoon Ma, Zerom Tesfai, Longcheng Wang, Erick Wang Co, Sergey Epshteyn, Abigail R Kennedy, Baili Chen, Larisa Dubenko, Neel Kumar Anand, Tsze H. Tsang, John M. Nuss, Csaba J Peto, Kenneth D. Rice, Mohamed Abdulkader Ibrahim, Kevin Luke Schnepp, Xian Shi, James William Leahy, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Grace Mann, Larry Wayne Mann, Craig Stacy Takeuchi, Peter Lamb, David J. Matthews, Nicole Miller
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Publication number: 20100010082Abstract: The present disclosure relates to ophthalmic solutions and methods of using the solutions to treat ocular disordersType: ApplicationFiled: July 9, 2009Publication date: January 14, 2010Applicant: Aspreva International Ltd.Inventors: Eddie CHONG, Clive BURGE, Lee MIZZEN
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Publication number: 20090240069Abstract: Provided are processes for preparation of mycophenolic acid.Type: ApplicationFiled: April 1, 2009Publication date: September 24, 2009Inventors: Vilmos Keri, Zoltan Czovek
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Publication number: 20090209639Abstract: A process for modifying the crystal habit of acicular drug substances, crystals obtained by such a process, and particular crystal forms or modifications of mycophenolic acid or mycophenolate sodium are provided, as well as pharmaceutical compositions comprising the crystals, methods of treatment and uses thereof.Type: ApplicationFiled: December 18, 2008Publication date: August 20, 2009Inventors: Sabine Pfeffer, Dierk Wieckhusen
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Publication number: 20090192218Abstract: The present invention relates to the use of a compound as effective agent for the prevention or treatment of diabetes mellitus in a mammal. Said compounds being selected from the group of phthalide derivatives and exhibit excellent blood glucose lowering effects and thus are effective agents in the prevention or treatment of diabetes mellitus in mammals.Type: ApplicationFiled: March 27, 2009Publication date: July 30, 2009Inventors: Daniel D'Orazio, Antoine De Saizieu, Goede Schueler, Daniel Raederstorff, Sandra Renata Teixeira, Ying Wang Schmidt, Peter Weber, Swen Wolfram
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Publication number: 20090176873Abstract: The present invention relates to the use of compounds of the formula (I) wherein the clotted line is an optional bond; R1 is butyl or butyryl if R2 is hydroxyl but is butyl if R2 is hydrogen; or R1 and R2 taken together are 1-butylidene optionally substituted by hydroxyl, methyl, or 3-(?,?-dimethylacrylyloxy)-pentylidenyl; X is a 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 is hydroxyl or butyryl; and n is 1 or 2, as agents for the prevention, control and treatment of conditions requiring modulation of inflammation in mammals. In another aspect, the present invention relates to the use of compounds of the formula (I) as active ingredients in the manufacture of medicaments/compositions for the prevention, control and treatment of conditions requiring modulation of inflammation.Type: ApplicationFiled: May 24, 2006Publication date: July 9, 2009Applicant: DSM IP ASSETS B.V.Inventors: Ann Fowler, Daniel Raederstorff, Goede Schuler, Joseph Schwager
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Patent number: 7528266Abstract: The present invention relates to a first compound having the formula wherein R is halogen, R1S(O)n or (R1)2NC(X)O; R1 is C1-C8alkyl, C1-C8haloalkyl, aryl-C1-C8-alkyl or aryl; n is 0, 1, 2 or 3; X is O or S; and R3 is C2-C5alkyl or C1-C5haloalkyl, or a salt thereof. The present invention is also directed to a second compound having the formula wherein R is fluorine, bromine, iodine, R1S(O)n or (R1)2NC(X)O; R1 is C1-C8alkyl, C1-C8- haloalkyl, aryl-C1-C8alkyl or aryl; n is 0, 1, 2 or 3; X is O or S; and R2 is hydrogen, C1-C4alkyl or C1-C4haloalkyl, with the proviso that R1 is different from C1-C8 alkyl or aryl if X is S, R is different from iodine if R2 is methyl, and R is different from fluorine, bromine or iodine if R2 is hydrogen.Type: GrantFiled: October 19, 2007Date of Patent: May 5, 2009Assignee: Syngenta Crop Protection, Inc.Inventors: Anita Schnyder, Marco Passafaro, Thomas Rapold
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Patent number: 7468436Abstract: A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (?)-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner.Type: GrantFiled: March 5, 2004Date of Patent: December 23, 2008Assignee: Emory UniversityInventors: Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
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Patent number: 7101912Abstract: Prodrugs of carbidopa, derivatives of carbidopa prodrugs, methods of making prodrugs of carbidopa and derivatives thereof, methods of using prodrugs of carbidopa and derivatives thereof, and compositions of prodrugs of carbidopa and derivatives thereof are disclosed.Type: GrantFiled: December 8, 2003Date of Patent: September 5, 2006Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Mark A. Gallop, Kenneth C. Cundy, Jianhua Li, Feng Xu, Cindy X. Zhou, Laxminarayan Bhat
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Patent number: 6872839Abstract: Benzofuran-2-ones, compositions comprising benzofuranones, processes for preparing them, and their use as colorants for high or low molecular mass organic material.Type: GrantFiled: March 3, 2000Date of Patent: March 29, 2005Assignee: Cibaspecialty Chemicals Corp.Inventors: Leonhard Feiler, Thomas Ruch, Olof Wallquist, Peter Nesvadba
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Patent number: 6858743Abstract: The invention relates to a method for the production of 2-coumarone or substituted 2-coumarones, whereby cyclohexanone or substituted cyclohexanone is reacted with a carboxyl-containing acylating agent a) to give methyl 2-(2-oxo-cyclohexyl)-2-hydroxyacetate or substituted methyl 2-(2-oxo-cyclohexyl)-2-hydroxyacetates, which are either a1) directly converted to 2-coumarone or substituted 2-coumarones by means of catalytic gas-phase dehydrogenation, or a2) dehydrated by means of azeotropic distillation under basic conditions, or by use of a strong acid, or a strongly acidic ion exchanger to a mixture of methyl 2-oxocyclohexylidenacetate and the enol-lactone of the 2-oxocyclohexylidenacetic acid, or a mixture of substituted methyl 2-oxocyclohexylidenacetate and the enol-lactone of the substituted 2-oxocyclohexylidenacetic acid, which is finally converted in turn by catalytic gas-phase dehydrogenation to 2-coumarone, or substituted 2-coumarones, or b) are directly converted under acidic or basic conditions into aType: GrantFiled: May 9, 2001Date of Patent: February 22, 2005Assignee: DSM Fine Chemicals Austria NFG GmbH & Co, KGInventors: Michael Stanek, Peter Hildebrand, Curt Zimmermann, Marianne Castelijns
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Patent number: 6710187Abstract: A process to isolate dianhydride from an exchange reaction comprises extracting a bisimide/anhydride exchange reaction aqueous phase with an organic solution comprising an exchange catalyst at a first temperature and pressure to form an extracted aqueous phase comprising water, exchange catalyst and a dianhydride precursor; removing water from the extracted aqueous phase at a second temperature and pressure to form a molten phase, wherein the second pressure is less than the first pressure; removing water and exchange catalyst from the molten phase at a third temperature and pressure to form an isolation mixture; and converting the dianhydride precursor in the isolation mixture to dianhydride at a fourth temperature and pressure, wherein the fourth temperature is greater than the second and third temperatures and the fourth pressure is less than the second and third pressures.Type: GrantFiled: May 14, 2002Date of Patent: March 23, 2004Assignee: General Electric CompanyInventors: Thomas Link Guggenheim, David Anthony Mongilio
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Patent number: 6503942Abstract: This invention provides O-&agr;-acyloxyalkyl ethers of the venlafaxine metabolite 4-[2-(Dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenol, represented by Formula (I): wherein: the configuration at the steriogenic center (*) may be R, S, or RS (the racemate); R1 is selected from C1-C6 alkyl, C1-C6 alkoxy, C3-C6 cycloalkyl, or the moiety: R2 is selected from H, or C1-C6 alkyl; or, R1 and R2 may be concatenated such that form a moiety having formula (b): R3 is selected from H or C1-C6 alkyl; and R4 and R5 are independently selected from H, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 thioalkoxy, —CN, —OH, —CF3, —OCF3, halogen, —NH2, —NO2, or mono or dialkylamino wherein each alkyl group has 1 to 6 carbon atoms, or pharmaceutically acceptable salts or hydrates thereof, R, S, or RS forms thereof; as well as pharmaceutical compositions and methods treating central nervous system disoType: GrantFiled: November 21, 2001Date of Patent: January 7, 2003Assignee: WyethInventors: John P. Yardley, Magid A. Abou-Gharbia, John W. Ullrich
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Patent number: 6310220Abstract: This invention relates to compositions comprising a polycarbonate, polyester or polyketone which is subject to oxidative, thermal and/or light-induced degradation, or their mixtures and blends, and at least one benzofuran-2-one type compound, to the use thereof for stabilising polycarbonate, polyester or polyketone or their mixtures or blends against oxidative, thermal and/or light-induced degradation, as well as to a process for stabilising these plastic materials.Type: GrantFiled: March 2, 2000Date of Patent: October 30, 2001Assignee: Ciba Specialty Chemicals CorporationInventors: André Schmitter, Alfred Georges Oertli
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Patent number: 6204394Abstract: Disclosed is a method for preparing oxy-diphthalic anhydrides, which comprises reacting a halo-phthalic anhydride represented by the formula (1): where Hal represents F, Cl, Br or I, with a carbonate salt selected from the group consisting of lithium carbonate, sodium carbonate, magnesium carbonate and calcium carbonate in a solvent to prepare oxy-diphthalic anhydrides represented by the formula (2):Type: GrantFiled: July 14, 1999Date of Patent: March 20, 2001Assignee: Manac Inc.Inventors: Junichi Sakata, Shinsuke Inoue, Shinichi Kadono
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Patent number: 6143779Abstract: The present invention provides new benzofuranone derivatives and a method for producing the derivatives useful for a therapeutic agent for preventing and/or treating hormone dependent diseases.The present invention is a new benzofuranone derivative represented by a particular general formula (I). ##STR1## In the production, a particular benzofuranone compound and a particular benzaldehyde are reacted.Type: GrantFiled: December 7, 1998Date of Patent: November 7, 2000Assignee: Snow Brand Milk Products Co., Ltd.Inventors: Makoto Yoshihama, Masamichi Nakakoshi, Junji Nakamura, Shoji Nakayama
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Patent number: 6020501Abstract: The disclosure is a process for preparing a phthalide of the general formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently of the others hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy, by hydrogenation of a phthalic anhydride of the general formula II ##STR2## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each as defined above, with the aid of a hydrogenation catalyst, which comprises performing the hydrogenation with the aid of a nickel catalyst doped with metals of subgroup 1, subgroup 6 and/or subgroup 7 of the Periodic Table.Type: GrantFiled: January 7, 1999Date of Patent: February 1, 2000Assignee: BASF AktiengesellschaftInventors: Klemens Massonne, Rainer Becker, Wolfgang Reif, Joachim Wulff-Doring
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Patent number: 5892025Abstract: A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that referentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (-)-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner.Type: GrantFiled: July 14, 1998Date of Patent: April 6, 1999Assignee: Emory UniversityInventors: Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
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Patent number: 5693829Abstract: The invention relates to compounds of formula I ##STR1## wherein the general symbols are as defined in claim 1, as stabilizers for protecting organic materials against thermal, oxidative or light-induced degradation.Type: GrantFiled: September 17, 1996Date of Patent: December 2, 1997Assignee: Ciba Specialty Chemicals CorporationInventors: Peter Nesvadba, Samuel Evans
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Patent number: 5538969Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.Type: GrantFiled: May 26, 1995Date of Patent: July 23, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: David Morgans, Jr., Eric B. Sjogren, David B. Smith, Francisco X. Talam as, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fern andez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, John W. Patterson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
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Patent number: 5516920Abstract: The invention described novel compounds of formula ##STR1## wherein the general symbols are as defined in claim 1, as stabilisers for protecting organic materials, in particular polymers and lubricants, against thermal, oxidative or light-induced degradation.Type: GrantFiled: September 12, 1994Date of Patent: May 14, 1996Assignee: Ciba-Geigy CorporationInventors: Peter Nesvadba, Samuel Evans, Christoph Krohnke, Jurg Zingg
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Patent number: 5512568Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.Type: GrantFiled: February 18, 1994Date of Patent: April 30, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: David Morgans, Jr., Eric B. Sjogren, David B. Smith, Francisco X. Talamas, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fernandez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, John W. Patterson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
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Patent number: 5506262Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthetase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.Type: GrantFiled: November 10, 1993Date of Patent: April 9, 1996Assignee: Merck & Co., Inc.Inventors: Robert M. Burk, William H. Parsons, John J. Acton, III, Gregory D. Berger, Tesfaye Biftu, Robert L. Bugianesi, Yuan-Ching P. Chiang, Claude Dufresne, Narindar N. Girotra, Robert W. Marquis, Jr., Chan-Hwa Kuo, Sandra P. Plevyak, Mitree M. Ponpipom, Lori L. Whiting, James D. Bergstrom, Conrad Santini
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Patent number: 5502216Abstract: An anti-hyperlipemic agent which has a potent activity of reducing LDL and VLDL cholesterols, which are thought to be a risk factor for arteriosclerosis among total blood cholesterols, and which is excellent in the antioxidant activity on LDL, is provided. Additionally, a compound and a pharmaceutically acceptable salt thereof are disclosed, which is represented by Formula (I): ##STR1## wherein R.sup.1 is a lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl or aralkyl group which is optionally substituted; R.sup.2 is a group represented by the formula: -COOR' (wherein R' is a lower alkyl or aralkyl which is optionally substituted), lower alkyl or halogenated lower alkyl; or R.sup.1 and R.sup.2, together with adjacent carbonyl group, form a cyclohexanone ring represented by the formula: ##STR2## R.sup.3 is a phenyl group optionally being substituted, and, ring A is a benzene nucleus which is optionally substituted, or a heterocyclic ring containing S or 0 optionally being substituted!.Type: GrantFiled: May 22, 1995Date of Patent: March 26, 1996Assignee: Shionogi & Co., Ltd.Inventors: Sachio Mori, Shozo Takechi, Shiro Kida, Takuji Mizui, Teruhisa Ichihashi
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Patent number: 5493030Abstract: The disclosed hexenoic acid side-chain derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil, including immune, inflammatory, tumor, proliferative, viral or psoriatic disorders.Type: GrantFiled: February 18, 1994Date of Patent: February 20, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: David Morgans, Jr., David B. Smith, Francisco X. Talamas, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fernandez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, John W. Patterson, John C. Rohloff, Eric B. Sjogren, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
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Patent number: 5488117Abstract: Compounds of the formula (1) ##STR1## in which R.sub.2, R.sub.3, R.sub.4 and R.sub.5 independently of one another, are hydrogen, C.sub.1 -C.sub.25 alkyl, C.sub.7 -C.sub.9 phenylalkyl, unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted phenyl, unsubstituted or C.sub.1 -C.sub.4 alkyl-substituted C.sub.5 -C.sub.8 cycloalkyl; C.sub.1 -C.sub.18 alkoxy, hydroxyl, C.sub.1 -C.sub.25 alkanoyloxy, C.sub.3 -C.sub.25 alkenoyloxy, C.sub.3 -C.sub.25 alkanoyloxy which is interrupted by oxygen, sulfur or >N--R.sub.16 ; C.sub.6 -C.sub.9 cycloalkylcarbonyloxy, benzoyloxy or C.sub.1 -C.sub.12 alkyl-substituted benzoyloxy, where R.sub.16 is hydrogen or C.sub.1 -C.sub.8 alkyl, or, furthermore, the radicals R.sub.2 and R.sub.3 or the radicals R.sub.4 and R.sub.5 together with the carbon atoms to which they are bound form a phenyl ring, R.sub.4 is additionally --(CH.sub.2).sub.n --COR.sub.11, in which n is 0, 1 or 2, R.sub.11 is hydroxyl, ##STR2## R.sub.14 and R.sub.15, independently of one another, are hydrogen or C.sub.1 -C.Type: GrantFiled: July 26, 1994Date of Patent: January 30, 1996Assignee: Ciba-Geigy CorporationInventor: Peter Nesvadba
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Patent number: 5441953Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.Type: GrantFiled: September 23, 1994Date of Patent: August 15, 1995Assignee: Syntex (U.S.A.) Inc.Inventor: Eric B. Sjogren
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Patent number: 5380879Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.Type: GrantFiled: February 18, 1994Date of Patent: January 10, 1995Assignee: Syntex (U.S.A.) Inc.Inventor: Eric B. Sjogren
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Patent number: 5326783Abstract: This invention is directed to compounds of formula (I) which are novel C3- or C5-acyl sulfonamide, carboxamic acid or tetrazolyl analogs of the Zaragozic acids. These compounds inhibit the enzyme squalene synthase and are useful as cholesterol lowering agents.Type: GrantFiled: January 19, 1993Date of Patent: July 5, 1994Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, Chan-Hwa Kuo, Conrad Santini
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Patent number: 5308829Abstract: There are disclosed novel benzofuran derivatives of the formula: ##STR1## Also disclosed are a herbicidal composition containing the above benzofuran derivative as an active ingredient and a method for exterminating undesired weeds by the application of a herbicidally effective amount of the above benzofuran derivative to an area where the undesired weeds grow or will grow.Type: GrantFiled: March 18, 1993Date of Patent: May 3, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Susumu Takemura, Masayuki Enomoto, Toru Uekawa, Masaharu Sakaki, Ryo Sato, Eiki Nagano
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Patent number: 5296614Abstract: A process for the preparation of phthalides of the formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently of one another, are hydrogen, C.sub.1 - to C.sub.4 -alkyl or C.sub.1 - to C.sub.4 -alkoxy, by reacting phthalic anhydrides of the formula II ##STR2## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined as above, on hydrogenation catalysts at from 50.degree. to 400.degree. C. and at from 1 to 400 bar, wherein the hydrogenation catalysts employed are essentially free from Lewis acids.Type: GrantFiled: October 30, 1992Date of Patent: March 22, 1994Assignee: BASF AktiengesellschaftInventors: Jochem Henkelmann, Thomas Ruehl, Horst Zimmermann
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Patent number: 5274097Abstract: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A--denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X--denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --O--,n--denotes a number from 1 to 19, andB--denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.Type: GrantFiled: April 9, 1991Date of Patent: December 28, 1993Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Peter-Rudolf Seidel, Jorg Traber, Thomas Glaser
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Patent number: 5258401Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.Type: GrantFiled: September 10, 1992Date of Patent: November 2, 1993Assignee: Merck & Co., Inc.Inventors: Gregory D. Berger, Robert W. Marquis, Jr., Albert J. Robichaud, Edward M. Scolnick