The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 549/375)
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Patent number: 10519168Abstract: Methods of making compounds of Formula I are disclosed:Type: GrantFiled: June 30, 2017Date of Patent: December 31, 2019Assignee: Gilead Sciences, Inc.Inventors: John Enquist, Jr., Nolan Griggs, Christopher Hale, Norihiro Ikemoto, Andrew W. Waltman
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Patent number: 9644056Abstract: A compound represented by formula (I): wherein R1 represents a hydrogen atom or a methyl group; R2 represents a C1-C12 hydrocarbon group; Xa and Xb each independently represent an oxygen atom or a sulfur atom; X11 represents a C1-C12 divalent saturated hydrocarbon group where a hydrogen atom can be replaced by a fluorine atom; and A1 represents a C1-C12 divalent saturated hydrocarbon group or *-A2-X1-(A3-X2)a-A4-, where * represents a binding site to an oxygen atom, A2, A3 and A4 each independently represent a C1-C12 divalent hydrocarbon group, X1 and X2 each independently represent —O—, —CO—O—, —O—CO— or —O—CO—O—, and “a” represents 0 or 1.Type: GrantFiled: February 12, 2016Date of Patent: May 9, 2017Assignee: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Tatsuro Masuyama, Yuki Suzuki, Koji Ichikawa
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Publication number: 20150119586Abstract: To provide an industrial method for producing a substituted benzoic acid compound useful as an intermediate of pharmaceutical and agricultural chemicals with high purity and high yield.Type: ApplicationFiled: April 30, 2013Publication date: April 30, 2015Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Hisayoshi Jonishi, Tomohiro Okamoto, Norio Adachi, Akihiko Isogai, Tatsuya Jukurogi, Hideaki Konishi, Fumihiro Fukui
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Patent number: 8987478Abstract: The present invention relates to a process for the preparation of a precursor for the synthesis of hexanoic acid derived statins and to the use of said precursor in the manufacture of a medicament.Type: GrantFiled: December 6, 2012Date of Patent: March 24, 2015Assignee: DSM Sinochem Pharmaceuticals Netherlands B.V.Inventors: Ben De Lange, Dennis Heemskerk, Karin Henderika Maria Bessembinder
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Patent number: 8952053Abstract: The present invention relates to prodrugs of 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 prodrugs of the compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.Type: GrantFiled: March 6, 2013Date of Patent: February 10, 2015Assignee: Evolva SAInventors: Peteris Alberts, Alexandra Santana Sorensen
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Publication number: 20140371451Abstract: The invention discloses a method for the preparation of tert-butyl 6-chloro-3,5-dioxohexanoate from Meldrum's acid derivative and its use for the preparation of tert-butyl (4R,6S)-(6-hydroxymethyl-2,2-dimethyl-1,3-dioxan-4-yl)acetate (BHA), Rosuvastatin and Atorvastatin.Type: ApplicationFiled: August 28, 2014Publication date: December 18, 2014Inventors: Christian Noti, Guixian Hu, Barry Jackson
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Publication number: 20140357864Abstract: The present invention relates to a process for the preparation of a precursor for the synthesis of hexanoic acid derived statins and to the use of said precursor in the manufacture of a medicament.Type: ApplicationFiled: December 6, 2012Publication date: December 4, 2014Inventors: Ben De Lange, Dennis Heemskerk, Karin Henderika Maria Bessembinder
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Patent number: 8889890Abstract: A ketal ester of an oxocarboxylic acid and a process to make the same, where the ketal ester is of Structure (I): wherein a is 0 or an integer from 1 to 12; n is 0 or 1; R1 is a linear alkyl, aryl, arylalkylene, or branched alkyl group with 1-18 carbon atoms; R2 and R5 can be hydrogen, C1-6 straight chain or branched alkyl, phenyl, substituted phenyl, C1-6 alkyl substituted with up to four OH groups, C1-6 alkyl, or acetyl optionally substituted hydrocarbon radicals, or R2 and R4 together with the ?-carbon form a cycloaliphatic or heterocyclic ring with 3-6 carbon atoms and 0-3 heteroatoms, provided that only one of R2 and R5 is hydrogen; R3 is a linear alkyl or branched alkyl group with 1-18 carbon atoms; and R4 is hydrogen, or an alkyl, aryl, aralkyl or branched alkyl group with 1-10 carbon atoms.Type: GrantFiled: September 13, 2010Date of Patent: November 18, 2014Assignee: Segetis, Inc.Inventors: Douglas A. Wicks, Sergey Selifonov, Marc Davis Scholten
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Publication number: 20140212441Abstract: The present invention relates to methods and pharmaceutical compositions for immunosuppression by using the fatty acid derivative represented by formula (I). The present invention further relates to methods and pharmaceutical compositions for treating inflammatory diseases, allergic diseases and autoimmune diseases by using said fatty acid derivative.Type: ApplicationFiled: June 20, 2012Publication date: July 31, 2014Applicant: R-TECH UENO, LTD.Inventors: Yukihiko Mashima, Masahiro Tajima, Reiko Tabuchi
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Publication number: 20140163127Abstract: The present disclosure relates to the preparation of acrylate, alkacrylate, allyl, and polycarbonate derivatives of hydroxy ketal esters, and uses thereof.Type: ApplicationFiled: November 1, 2013Publication date: June 12, 2014Applicant: SEGETIS, INC.Inventors: Sergey SELIFONOV, Brian Daniel MULLEN, Douglas Alan WICKS, Vivek BADARINARAYANA
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Patent number: 8735322Abstract: Cyclohexanedione compounds, which are suitable for use as herbicides.Type: GrantFiled: September 23, 2009Date of Patent: May 27, 2014Assignee: Syngenta LimitedInventors: Christopher John Mathews, John Martin Clough, Kevin Beautement, Melloney Tyte, Louisa Robinson, Stephane AndréMarie Jeanmart
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Publication number: 20140093823Abstract: There are disclosed sulfonic acid precursor compositions, as are methods of using these compositions in, for example, photolithography.Type: ApplicationFiled: September 27, 2013Publication date: April 3, 2014Inventors: Robert L. BRAINARD, Shinya AKIBA, Ryo NADANO, Kenji HOSOI, Brian CARDINEAU
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Publication number: 20140051869Abstract: A continuous process for producing compounds having the general formula (6) is provided: wherein R is a straight or branched chain alkyl group, R1 is a straight or branched chain alkyl group substituted with a nitrile group, a hydroxy group or a halogen atom, R2 is a hydroxy group or a keto group, and each R3 is, independently, hydrogen or a straight or branched chain alkyl group, comprising providing a continuous stream of an alkyl acetate and a continuous stream of an alkali metal or alkaline earth metal amide base and contacting the continuous streams to yield an enolate compound, providing a continuous stream of a compound of formula (5): wherein R1 is as previously defined, and contacting the continuous stream of compound (5) with a continuous stream of the enolate above 20° C. to yield an intermediate compound and treating the intermediate compound with an acid.Type: ApplicationFiled: October 25, 2013Publication date: February 20, 2014Applicant: Phoenix Chemicals LimitedInventors: Peter McCormack, Antony John Warr, Elliot Latham
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Publication number: 20130316906Abstract: The invention relates to novel compounds of the formula (I) in which R1, R2, R3, R4, R5, Y, Q and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as herbicides and/or pesticides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the phenyl-substituted bicyclooctane-1,3-dione derivates and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as pesticides and/or for preventing unwanted plant growth.Type: ApplicationFiled: October 28, 2011Publication date: November 28, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Alfred Angermann, Stefan Lehr, Guido Bojack, Reiner Fischer, Isolde Häuser-hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Arnd Voerste, Dieter Feucht
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Publication number: 20130267561Abstract: Specifically useful stereoisomers of 1,3-dioxane derivatives are described and their use in the treatment of a disease or condition dependent on PPAR modulation, such as diabetes, cancer, inflammation, neurodegenerative disorders and infections as well as their use in the treatment of a disease related to TP, such as cardiovascular diseases.Type: ApplicationFiled: March 7, 2013Publication date: October 10, 2013Applicant: Evolva SaInventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Mainkar S. Prathama, Melya Hughes Crameri, Thierry Bonnaud, Joanne Kelleher, David Pearson
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Publication number: 20130253045Abstract: The present invention relates to prodrugs of 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 prodrugs of the compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.Type: ApplicationFiled: March 6, 2013Publication date: September 26, 2013Applicant: Evolva SaInventors: Peteris Alberts, Alexandra Santana Sorensen
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Patent number: 8536196Abstract: Specifically useful stereoisomers of 1,3-dioxane derivatives are described and their use in the treatment of a disease or condition dependent on PPAR modulation, such as diabetes, cancer, inflammation, neurodegenerative disorders and infections as well as their use in the treatment of a disease related to TP, such as cardiovascular diseases.Type: GrantFiled: January 18, 2008Date of Patent: September 17, 2013Assignee: Evolva SAInventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Prathama S. Mainkar, Melya Hughes Crameri, Thierry Bonnaud, Joanne Kelleher, David Pearson
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Publication number: 20130197030Abstract: 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: ApplicationFiled: March 8, 2013Publication date: August 1, 2013Applicant: Evolva SaInventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Mainkar S. Prathama
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Patent number: 8486994Abstract: The present invention relates to prodrugs of 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 prodrugs of the compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.Type: GrantFiled: January 18, 2008Date of Patent: July 16, 2013Assignee: Evolva SAInventors: Peteris Alberts, Alexandra Santana Sorensen
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Publication number: 20130085201Abstract: Ketal lactones of and methods for making such ketal lactones are disclosed. Also described are methods for making isolated cis- and trans-stereoisomers of hydroxyester ketals of oxocarboxylic acids and polymers having ketal units of such stereoisomers within the polymer backbone.Type: ApplicationFiled: September 27, 2010Publication date: April 4, 2013Applicant: SEGETIS, INC.Inventors: Sergey Selifonov, Ning Zhou, Brian D. Mullen
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Publication number: 20120323024Abstract: A ketal ester of an oxocarboxylic acid and a process to make the same, where the ketal ester is of Structure (I): wherein a is 0 or an integer from 1 to 12; n is 0 or 1; R1 is a linear alkyl, aryl, arylalkylene, or branched alkyl group with 1-18 carbon atoms; R2 and R5 can be hydrogen, C1-6 straight chain or branched alkyl, phenyl, substituted phenyl, C1-6 alkyl substituted with up to four OH groups, C1-6 alkyl, or acetyl optionally substituted hydrocarbon radicals, or R2 and R4 together with the ?-carbon form a cycloaliphatic or heterocyclic ring with 3-6 carbon atoms and 0-3 heteroatoms, provided that only one of R2 and R5 is hydrogen; R3 is a linear alkyl or branched alkyl group with 1-18 carbon atoms; and R4 is hydrogen, or an alkyl, aryl, aralkyl or branched alkyl group with 1-10 carbon atoms.Type: ApplicationFiled: September 13, 2010Publication date: December 20, 2012Applicant: SEGETIS, INC.Inventors: Douglas A. Wicks, Sergey Selifonov, Marc Davis Scholten
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Publication number: 20120323005Abstract: The present invention relates to an improved process for the preparation of amide intermediates useful in the preparation of cholesterol reducing agents.Type: ApplicationFiled: January 17, 2011Publication date: December 20, 2012Inventors: Manne Satyanarayana Reddy, Srinivasan Thirumalai Rajan, Maramreddy Sahadeva Reddy
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Publication number: 20120252836Abstract: 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: ApplicationFiled: June 18, 2012Publication date: October 4, 2012Applicant: EVOLVA SAInventors: Alexandra Santana Sorensen, Jean-Phillippe Meyer, Peteris Alberts, Mainkar Prathama
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Publication number: 20120142766Abstract: 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: ApplicationFiled: January 18, 2008Publication date: June 7, 2012Applicant: EVOLVA SAInventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Mainkar S. Prathama
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Publication number: 20120136151Abstract: The present invention relates to novel intermediate compounds used in preparing Rosuvastatin or the pharmaceutically acceptable salts thereof, to a method for preparing same, and to a method for preparing Rosuvastatin or the pharmaceutically acceptable salts thereof from the intermediates. The preparation method of the present invention has the effect of providing Rosuvastatin hemi-calcium salts with an excellent yield rate.Type: ApplicationFiled: April 8, 2010Publication date: May 31, 2012Inventors: Hongwoo Lee, Daejong Park, Choongleol Yoo, Donghyuk Nam, Hohyung Ryu, Dongjin Kim
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Publication number: 20120122745Abstract: Various esterified alkyl ketal ester or hydroxyalkyl ketal ester products are useful as components of organic polymer compositions. The ketal esters are produced in certain transesterifications between alkyl ketal esters and/or hydroxyalkyl ketal esters and polyols, aminoalcohols, polyamines and/or polycarboxylic acids. The products are excellent plasticizers for a variety of organic polymers, notable poly(vinyl chloride) plastisols. The products are also very good lubricants for many lubrication applications.Type: ApplicationFiled: December 21, 2011Publication date: May 17, 2012Applicant: SEGETIS, INC.Inventors: Brian D. MULLEN, Chunyong WU, Tara J. MULLEN, Marc D. SCHOLTEN, Vivek BADARINARAYANA
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Publication number: 20120035053Abstract: Cyclohexanedione compounds, which are suitable for use as herbicides.Type: ApplicationFiled: September 23, 2009Publication date: February 9, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Christopher John Mathews, John Martin Clough, Kevin Beautement, Melloney Tyte, Louisa Robinson, Stephane André Marie Jeanmart
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Publication number: 20110319586Abstract: Novel ketal compounds can be made from an oxocarboxylate and a triol. Novel polymeric structures are, in turn, synthesized from the ketal compounds. Such ketal compounds and associated polymers are useful in a broad range of applications as a substitute for materials derived from petroleum or other such nonrenewable resources.Type: ApplicationFiled: September 4, 2008Publication date: December 29, 2011Applicant: SEGETIS, INC.Inventors: Douglas Alan Wicks, Charles Todd Williams, Sergey A. Selifonov
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Patent number: 8076494Abstract: Disclosed is a process for the manufacture of a compound of formula (I) wherein Hal represents fluoro or chloro, and R1 and R2 represent, independently from one another, hydrogen or Hal; in which process a compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ether in a polar non-nucleophilic solvent at a temperature of ?10 to 50° C. to give the compound of formula (I).Type: GrantFiled: August 31, 2010Date of Patent: December 13, 2011Assignee: Basilea Pharmaceutica AGInventors: Marc Muller, Lin Xu
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Publication number: 20110223365Abstract: The present disclosure relates to the preparation of acrylate, alkacrylate, allyl, and polycarbonate derivatives of hydroxy ketal esters, and uses thereof.Type: ApplicationFiled: September 25, 2009Publication date: September 15, 2011Applicant: SEGETIS, INC.Inventors: Sergey Selionov, Brian Daniel Mullen, Douglas Alan Wicks, Vivek Badarinarayana
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Patent number: 8008513Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: GrantFiled: August 28, 2009Date of Patent: August 30, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Gee-Hong Kuo, Rui Zhang, Aihua Wang, Alan R. DeAngelis
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Patent number: 7989643Abstract: The invention relates to the preparation of 2-(6-substituted-1,3-dioxane-4-yl)acetic acid derivatives of formula 1, where X stands for a leaving group, and R1, R2, and R3 each independently stand for an alkyl group with 1-3 carbon atoms from 4-hydroxy-6-X-substituted-methyl-tetrahydropyran-2-one compounds, where X is as defined above, with the aid of an acetalization agent, in the presence of an acid catalyst. The invention also relates to the novel compounds of formula 1 as well as salts and acids to be prepared from these, with the OR3 group in formula 1 being replaced by an OY group, where X, R1 and R2 have the meanings defined above and where Y stands for an alkaline (earth) metal or a substituted or unsubstituted ammonium group or stands for hydrogen, and to the novel compounds of formula 2. The products concerned are, after conversion into the t-butyl ester of 2-(6-hydroxymethyl-1,3-dioxane-4-yl)acetic acid, important as intermediary products in the preparation of statins.Type: GrantFiled: November 24, 2009Date of Patent: August 2, 2011Assignee: AstraZeneca UK Ltd.Inventors: Jacob Hermanus Mattheus Hero Kooistra, Hubertus Josephus Marie Zeegers, Daniel Mink, Joannes Maria Cornelis Antonius Mulders
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Publication number: 20110178112Abstract: 1,3-dioxane derivatives are described and their use in the treatment of a disease or condition dependent on PPAR modulation, such as diabetes, cancer, inflammation, neurodegenerative disorders and infections.Type: ApplicationFiled: January 18, 2007Publication date: July 21, 2011Applicant: EVOLVA SAInventors: Karsten Kristiansen, Prathama S. Mainkar, Jean-Philippe Meyer, Alexandra Santana Sorensen
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Patent number: 7906502Abstract: Compounds of formula (I) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.Type: GrantFiled: June 21, 2006Date of Patent: March 15, 2011Assignee: AstraZeneca ABInventors: Susanne Alenfalk, Mikael Dahlstrom, Fana Hunegnaw, Staffan Karlsson, Ingemar Starke
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Patent number: 7893048Abstract: Compounds of formula (I): (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.Type: GrantFiled: June 21, 2006Date of Patent: February 22, 2011Assignee: AstraZeneca ABInventors: Susanne Alenfalk, Mikael Dahlstrom, Fana Hunegnaw, Staffan Karlsson, Malin Lemurell, Ingemar Starke
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Patent number: 7863265Abstract: Compounds of formula (I) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.Type: GrantFiled: June 19, 2006Date of Patent: January 4, 2011Assignee: AstraZeneca ABInventors: Susanne Alenfalk, Mikael Dahlstrom, Fana Hunegnaw, Staffan Karlsson, Malin Lemurell, Ann-Margret Lindqvist, Tore Skjaret, Ingemar Starke
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Publication number: 20100273824Abstract: 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: ApplicationFiled: January 18, 2008Publication date: October 28, 2010Applicant: EVOLVA SAInventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Mainkar S. Prathama
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Patent number: 7815950Abstract: Ketomethionine ketals and hemiketals and derivatives thereof are useful as feed additives, in particular for the nutrition of ruminants.Type: GrantFiled: November 20, 2007Date of Patent: October 19, 2010Assignee: Evonik Degussa GmbHInventors: Christoph Kobler, Martin Hateley, Philipp Roth, Barbara Jaeger, Rainer Peter, Christoph Weckbecker, Klaus Huthmacher
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Publication number: 20100168169Abstract: Specifically useful stereoisomers of 1,3-dioxane derivatives are described and their use in the treatment of a disease or condition dependent on PPAR modulation, such as diabetes, cancer, inflammation, neurodegenerative disorders and infections as well as their use in the treatment of a disease related to TP, such as cardiovascular diseases.Type: ApplicationFiled: January 18, 2008Publication date: July 1, 2010Applicant: EVOLVA SAInventor: Alexandra Santana Sorensen
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Publication number: 20100136339Abstract: The invention relates to the preparation of 2-(6-substituted-1,3-dioxane-4-yl)acetic acid derivatives of formula 1, where X stands for a leaving group, and R1, R2, and R3 each independently stand for an alkyl group with 1-3 carbon atoms from 4-hydroxy-6-X-substituted-methyl-tetrahydropyran-2-one compounds, where X is as defined above, with the aid of an acetalization agent, in the presence of an acid catalyst. The invention also relates to the novel compounds of formula 1 as well as salts and acids to be prepared from these, with the OR3 group in formula 1 being replaced by an OY group, where X, R1 and R2 have the meanings defined above and where Y stands for an alkaline (earth) metal or a substituted or unsubstituted ammonium group or stands for hydrogen, and to the novel compounds of formula 2. The products concerned are, after conversion into the t-butyl ester of 2-(6-hydroxymethyl-1,3-dioxane-4-yl)acetic acid, important as intermediary products in the preparation of statins.Type: ApplicationFiled: November 24, 2009Publication date: June 3, 2010Applicant: AstraZeneca UK Ltd.Inventors: Jacob Hermanus Mattheus Hero Kooistra, Hubertus Josephus Marie ZEEGERS, Daniel MINK, Joannes Maria Cornelis Antonius MULDERS
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Patent number: 7718812Abstract: The invention relates to a process for the conversion of group X in a 2-(6-substituted)-1,3-dioxane-4yl) acetic acid derivative according to formula 2 into a group OY in the presence of a phase transfer catalyst and an oxylating agent, by using as a phase transfer catalyst a quarternary phosphonium ion and by using as an oxylating agent an OY-ion. X stands for a halogen and R1, R2 and R3 are each independently a C1–4 alkylgroup or R1 and R2 together with the C-atom to which they are bound form a 5- or 6-membered cycloalkyl; Y stands for RA-CO— or for RB—SO2- with RA, RB are chosen from the group of alkyl or aryl with 1–12 C-atoms.Type: GrantFiled: December 9, 2002Date of Patent: May 18, 2010Assignee: AstraZeneca UK LimitedInventor: Robert Patrick Hof
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Publication number: 20100087517Abstract: The present invention relates to prodrugs of 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 prodrugs of the compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.Type: ApplicationFiled: January 18, 2008Publication date: April 8, 2010Applicant: EVOLVA SAInventors: Peteris Alberts, Alexandra Santana Sorensen
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Publication number: 20100004470Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: ApplicationFiled: August 28, 2009Publication date: January 7, 2010Inventors: Gee-Hong Kuo, Rui Zhang, Aihua Wang, Alan R. DeAngelis
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Patent number: 7642363Abstract: The invention relates to the preparation of 2-(6-substituted-1,3-dioxane-4-yl)acetic acid derivatives of formula 1, where X stands for a leaving group, and R1, R2, and R3 each independently stand for an alkyl group with 1-3 carbon atoms from 4-hydroxy-6-X-substituted-methyl-tetrahydropyran-2-one compounds, where X is as defined above, with the aid of an acetalization agent, in the presence of an acid catalyst. The invention also relates to the novel compounds of formula 1 as well as salts and acids to be prepared from these, with the OR3 group in formula 1 being replaced by an OY group, where X, R1 and R2 have the meanings defined above and where Y stands for an alkaline (earth) metal or a substituted or unsubstituted ammonium group or stands for hydrogen, and to the novel compounds of formula 2. The products concerned are, after conversion into the t-butyl ester of 2-(6-hydroxymethyl-1,3-dioxane-4-yl)acetic acid, important as intermediary products in the preparation of statins.Type: GrantFiled: February 7, 2005Date of Patent: January 5, 2010Assignee: AstraZeneca UK Ltd.Inventors: Jacob Hermanus Mattheus Hero Kooistra, Hubertus Josephus Marie Zeegers, Daniel Mink, Joannes Maria Cornelis Antonius Mulders
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Publication number: 20090192321Abstract: A process produces a 2-benzoyloxyacetaldehyde derivative represented by following Formula (3): wherein R1 and R2 may be the same as or different from each other and are each a hydrocarbon group, wherein R1 and R2 may be combined to form a ring with the adjacent oxygen-carbon-oxygen bond, and wherein the benzene ring in the formula may be substituted, by allowing a halogenated acetaldehyde acetal derivative represented by following Formula (1): wherein R1 and R2 are as defined above; and X represents a halogen atom, to react with a benzoate represented by following Formula (2): wherein M represents an alkali metal atom and wherein the benzene ring in the formula may be substituted, in the presence of an alkali-metal halide.Type: ApplicationFiled: March 4, 2009Publication date: July 30, 2009Inventor: Kazuyoshi NISHIKAWA
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Publication number: 20090163576Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed, compound of the formula (I): wherein n is 1 or 2; m is 0, 1, 2, 3, 4, 5, 6, 7 or 8; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; R3 and R4 together are alkyl having two or three carbon atoms; or R3 and R4 are the same as each other and each is methyl or ethyl; R5 is hydrogen or alkyl having from one to six carbon atoms.Type: ApplicationFiled: May 11, 2007Publication date: June 25, 2009Applicant: WELLSTAT THERAPEUTICS CORPORATIONInventors: Shalini Sharma, Reid W. von Borstel
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Patent number: 7498451Abstract: The invention relates to a process for obtaining a pure aliphatic dialdehyde monoacetal by reaction of the corresponding aliphatic dialdehyde or a precursor of the corresponding aliphatic dialdehyde with one or more aliphatic mono- or polyhydric alcohols while distillatively removing water to obtain a reaction mixture which is separated distillatively, which comprises carrying out the distillative separation continuously in a dividing wall column to obtain pure aliphatic dialdehyde monoacetal as a sidestream from the dividing wall column, or in two distillation columns to obtain crude aliphatic dialdehyde monoacetal as a sidestream in the first distillation column, feed the crude aliphatic dialdehyde monoacetal to the second distillation column and obtain pure aliphatic dialdehyde monoacetal as the sidestream from the second distillation column.Type: GrantFiled: November 27, 2003Date of Patent: March 3, 2009Assignee: BASF AktiengesellschaftInventors: Gerd Haderlein, Hans-Georg Göbbel, Wolfgang Siegel
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Patent number: 7442811Abstract: Process for the preparation of an ester of formula (1), wherein R1 represents a leaving group, CN, OH or a COOR5 group, R3 and R4 each independently represent a 1-3 C alkyl group, and R2 and R5 each independently represent an ester residue, wherein the corresponding salt with formula (2), wherein M represents H or an alkali (earth) metal in an inert solvent is contacted with an acid chloride forming agent to form the corresponding acid chloride, and the acid chloride is contacted with an alcohol with formula R2OH in the presence of N-methyl-morpholine. Preferably M represents an alkali metal, and R2 represents an alkyl group, particularly a t.-butyl group.Type: GrantFiled: June 12, 2003Date of Patent: October 28, 2008Assignee: AstraZeneca UK LimitedInventors: Hermanus Carolus Catherina Karel Bakel Van, Dominique Monique Charles Callant, Jacob Hermanus Mattheus Hero Kooistra, Peter Johannes Dominicus Maas
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Patent number: 7439046Abstract: The invention relates to a process for the preparation of a 2,4-dideoxyhexose or a 2,4,6-trideoxyhexose from a substituted or unsubstituted carbonyl compound with at least 2 carbon atoms and at least one ?-hydrogen atom and a substituted or unsubstituted aldehyde in the presence of an aldolase and water, the reaction between the substituted or unsubstituted carbonyl compound with at least 2 carbon atoms and at least one ?-hydrogen atom and the substituted or unsubstituted aldehyde being carried out at a carbonyl concentration of at most 6 moles/l of reaction mixture and the final concentration of the 2,4-dideoxyhexose or the 2,4,6-trideoxyhexose being at least 2 mass % of the reaction mixture. The invention also relates to the use of a 2,4-dideoxyhexose or a 2,4,6-trideoxyhexose obtained by means of a process according to the invention in the preparation of a medicine, particularly in the preparation of a statine.Type: GrantFiled: August 17, 2005Date of Patent: October 21, 2008Assignee: DSM IP Assets B.V.Inventors: Joannes Gerardus Kierkels, Daniel Mink, Sven Panke, Franciscus Alphons Lommen, Dennis Heemskerk
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Publication number: 20080246002Abstract: Compounds that are useful in compositions for flat panel displays, for example, are provided. The compounds provided are polar, and are useful in low threshold voltage mixtures. The compounds provided have the general structure: CpCOCH2[A]nZ1[B]mZ2PhX1X2Y, where CpCOCH2 is the structure: A and B are independently in each instance selected from the group consisting of 1,4-cyclohexane, 1,4-phenyl, 1,3-dioxan-5,2-diyl; pyridine-5,2-diyl; and pyrimidin-5,2-diyl; n and m are independently in each instance 0, 1 or 2; Z1 and Z2 are independently a single bond, —(CH2)2—, CF2O, OCF2, CH2O, OCH2, —C?C—, COO, OOC; and Y is selected from the group consisting of: F, Cl, CN, OCH2F, CHF2, OCF3, and CF3.Type: ApplicationFiled: April 3, 2007Publication date: October 9, 2008Inventor: Xinhua Chen