Alicyclic Acid Moiety Containing N, S, P, B Or Halogen Patents (Class 560/125)
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Patent number: 8343465Abstract: A topical cosmetic and dermatological preparation for reducing skin reddening which comprises (1R,2S,5R)-2-isopropyl-5-methyl-N-(2-(pyridin-2-yl)ethyl)-cyclohexane carboxamide and/or (1R,2S,5R)—N-(4-cyanomethyl-phenyl)-2-isopropyl-5-methylcyclohexane carboxamide.Type: GrantFiled: March 12, 2009Date of Patent: January 1, 2013Assignee: Beiersdorf AGInventors: Ludger Kolbe, Julia Eckert, Gitta Neufang, Stefanie Knaupmeier
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Patent number: 8343972Abstract: The present invention relates to compounds selected from the group consisting of 14-0-[((Mono- or dialkylamino)-cycloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[((Cycloalkyl- or heterocyclylamino)-cycloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioaceyl or -imino-oxy]-mutilins, 14-O-[((Heterocyc-N-yl-cycloalkyl)-sulfanyl- or -oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Mono- or dialkylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Cycloalkyl- or heterocyclylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and 14-O-[((Heterocyc-N-yl-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and their use as pharmaceuticals.Type: GrantFiled: July 26, 2006Date of Patent: January 1, 2013Assignee: Nabriva Therapeutics AGInventors: Rosemarie Mang, Heinz Berner
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Publication number: 20120330030Abstract: Provided is an enantioselective, palladium-catalyzed method for the preparation of ?-amino-?,?-unsaturated carboxylic acid derivatives having the formulas II, III, VII and VIII:Type: ApplicationFiled: September 6, 2012Publication date: December 27, 2012Inventors: Murat Acemoglu, Andreas Pfaltz, Claude Shaerer
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Patent number: 8334319Abstract: The present invention relates to polymorphic forms of (3R,4R,5S)-5-amino-4-acetylamino-3-(1-ethyl-propoxy)-cyclohex-1-ene-carboxylic acid ethyl ester phosphate, which is a potent inhibitor of viral neuraminidase.Type: GrantFiled: December 19, 2008Date of Patent: December 18, 2012Assignee: Roche Palo Alto LLCInventors: Pierre Goldbach, Olaf Grassmann, Ines Sauer
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Patent number: 8329745Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules of the general formula: Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.Type: GrantFiled: September 6, 2011Date of Patent: December 11, 2012Assignee: Board of Regents, The University of Texas SystemInventors: Patrcik G. Harran, Michael S. Brown, Joseph L. Goldstein, Jing Yang, Tong-Jin Zhao
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Patent number: 8324422Abstract: The enhydrazone esters for treating asthma, allergy, and inflammation relate to the use of two cyclohexenone derivatives and pharmaceutically acceptable salts thereof in the treatment of asthma, allergies, and inflammation. The esters have the formula: wherein R is ethyl or methyl. Administration of the esters inhibits the degranulation of eosinophils, the degranulation of mast cells, and the release or expression of tumor necrosis factor-?, thereby alleviating the debilitating symptoms of asthma, allergic reactions, and inflammatory responses.Type: GrantFiled: May 3, 2010Date of Patent: December 4, 2012Assignee: Kuwait UniversityInventors: Charles I. Ezeamuzie, Ivan O. Edafiogho
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Publication number: 20120296093Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.Type: ApplicationFiled: July 31, 2012Publication date: November 22, 2012Inventors: George Wu, Anantha R. SUDHAKAR, Tao WANG, Ji XIE, Frank Xing CHEN, Marc POIRIER, Mingsheng HUANG, Vijay SABESAN, Daw-long KWOK, Jian CUI, Xiaojing YANG, Tiruvettipuram K. THIRUVENGADAM, Jing LIAO, Ilia A. Zavialov, Hoa N. NGUYEN, Ngiap Kie LIM
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Patent number: 8304553Abstract: A process is provided for the synthesis of 4,5-diamino cyclohexene carboxylate ester (1): or a pharmaceutically acceptable salt thereof. R1-R3 are a silyl-, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. R4, R11 and R12 are H, a silyl-group, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. 3,4-Dihydropyran compound (9): with R5 and R6 being suitable protecting groups, is reacted to form aldehyde (4): which is oxidized and converted to N-substituted carbamate (3): with R7 being a suitable protecting group. (3) is, via oxazolinidone (13): converted to azido carboxylate ester (2): and then to 4,5-diamino cyclohexene carboxylate ester (1).Type: GrantFiled: December 10, 2008Date of Patent: November 6, 2012Assignee: Nanyang Technological UniversityInventors: Xuewei Liu, Jimei Ma
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Publication number: 20120252890Abstract: The present application relates to processes for the preparation of intermediates useful in the manufacture of oseltamivir and the H3PO4 salt of oseltamivir, Tamiflu®. The application further relates to novel intermediate and compounds and oseltamivir analogs and to pharmaceutical compositions comprising said analog compounds. The application further relates to a method of using the novel analogs of oseltamivir to treat or prevent influenza.Type: ApplicationFiled: October 15, 2010Publication date: October 4, 2012Applicant: BROCK UNIVERSITYInventors: Tomas Hudlicky, Lukas Werner, Ales Machara
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Patent number: 8278477Abstract: The method for making a phosphorus ylide produces the ylide 2,3-bismethoxycarbonyl-4-phenyl-5-arylhydrazono-cyclopenta-1,3-dienyl-triphenylphosphonium in pure form by simple recrystallization of the reaction product. 3-Oxo-3-phenyl-2-(arylhydrozono)propanal and dimethylacetylenedicarboxylate are mixed in dichloromethane at room temperature. After cyclization of the intermediate (preferably at least two hours), triphenylphosphine is added to the mixture, ultimately resulting in formation of 2,3-bismethoxycarbonyl-4-phenyl-5-arylhydrazono-cyclopenta-1,3-dienyl-triphenylphosphonium. The product is recrystallized to produce 2,3-bismethoxycarbonyl-4-phenyl-5-arylhydrazono-cyclopenta-1,3-dienyl-triphenylphosphonium in pure form and in high yield. The aryl group may be any aromatic or aliphatic group.Type: GrantFiled: December 22, 2009Date of Patent: October 2, 2012Assignee: King Abdulaziz UniversityInventor: Khadijah M. Al-Zaydi
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Publication number: 20120231376Abstract: The invention relates to a photopolymer formulation comprising matrix polymers, writing monomers, and photoinitiators, to the use of the photopolymer formulation for producing optical elements, in particular for producing holographic elements and images, to a method for illuminating holographic media made of the photopolymer formulation, and to special fluorourethanes.Type: ApplicationFiled: November 2, 2010Publication date: September 13, 2012Applicant: Bayer Intellectual Property GmbHInventors: Thomas Rölle, Friedrich-Karl Bruder, Thomas Fäcke, Marc-Stephan Weiser, Dennis Hönel
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Publication number: 20120197015Abstract: The present invention is directed to providing epoxycarboxamide compounds, azide compounds and amino alcohol compounds which serve as manufacturing intermediates that can lead to useful ?-ketoamide compounds, and the present invention is also is directed to processes for preparing ?-ketoamide compounds using the intermediates. The epoxycarboxamide compounds, azide compounds and amino alcohol compounds are represented by the following formulae: wherein R1, R2, R3, R4 and R5, as well as subvariables for one or more of R1, R2, R3, R4 and R5 are as defined herein.Type: ApplicationFiled: December 14, 2011Publication date: August 2, 2012Applicant: Seikagaku Kogyo Kabushiki Kaisha d/b/a Seikagaku CorporationInventors: Nobuo KOBAYASHI, Tsuneo Koji, Takashi Fujita, Tomofumi Nishimura, Akihiko Hosoda
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Publication number: 20120190865Abstract: The present invention relates to a novel process for the preparation of 1-H-pyrrolidine-2,4-dione derivatives and to novel intermediates and to a process for their preparation.Type: ApplicationFiled: January 25, 2012Publication date: July 26, 2012Applicant: Bayer CropScience AGInventors: Reiner FISCHER, Thomas HIMMLER
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Patent number: 8222447Abstract: Compounds of formula (I), which are 14-O-{[(optionally substituted hydroxy)cyclohexyl)sulfanyl]acetyl}mutilins further substituted at the cyclohexyl group by an acylated amino group, salts and solvates thereof, pharmaceutical compositions comprising such compounds and their use as a pharmaceutical, e.g. for the treatment of diseases mediated by microbes and for the treatment of inflammation where microbes are mediating said inflammation.Type: GrantFiled: August 17, 2009Date of Patent: July 17, 2012Assignee: Nabriva Therapeutics AGInventors: Rosemarie Mang, Werner Heilmayer
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Publication number: 20120165559Abstract: The present invention relates to compounds of general formula (I): having a physiological effect, and to the preparation thereof and to the use of same.Type: ApplicationFiled: April 15, 2010Publication date: June 28, 2012Inventors: Jean Mane, Jean-Claude Clinet
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Publication number: 20120130092Abstract: It is possible to produce oseltamivir safely and stably in large quantities by using as a starting material tartaric acid, mannitol or arabinose, via dihydroxyhexenoic acid ester of the formula (4c).Type: ApplicationFiled: December 6, 2011Publication date: May 24, 2012Inventors: Teruhiko Ishikawa, Seiki Saito, Takayuki Kudoh, Kotaro Suto, Hironori Nishiuchi, Makoto Okada, Masatoshi Taniguchi
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Publication number: 20120108801Abstract: The invention relates to disubstituted-aminodifluorosulfinium salts represented by the formula (I). Processes for preparing same and methods of use as deoxofluorinating reagent is also provided.Type: ApplicationFiled: June 18, 2010Publication date: May 3, 2012Applicant: OMEGACHEM INCInventors: Michel A. Couturier, Alexandre L'Heureux
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Publication number: 20120058937Abstract: A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.Type: ApplicationFiled: April 15, 2009Publication date: March 8, 2012Applicant: TSRL, Inc.Inventors: John Hilfinger, Gordon Amidon
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Publication number: 20120046272Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.Type: ApplicationFiled: August 19, 2011Publication date: February 23, 2012Applicant: GRUNENTHAL GMBHInventor: Ramesh SESHA
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Publication number: 20120046276Abstract: A method of preventing or treating diseases caused by Mycobacterium, comprising administering to a subject in need of such treatment an effective amount of a pleuromutilin.Type: ApplicationFiled: October 25, 2011Publication date: February 23, 2012Applicant: Nabriva Therapeutics AGInventors: Gerd Ascher, Heinz Berner, Rosemarie Mang
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Patent number: 8115030Abstract: Disclosed is a process for the preparation of Compound (III), salt or solvate thereof by reacting Compound (I), salt or solvate thereof with Compound (II) in a toluene solvent in the presence of an additive such as water or an alcohol. Also disclosed is a process for the preparation of Compound (IV) comprising hydrolyzing the obtained Compound (III) if necessary, and then oxidizing. In the formula, R1 is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or optionally substituted aryl lower alkyl, and R2 is optionally substituted lower alkyl, optionally substituted cycloalkyl or optionally substituted aryl lower alkyl.Type: GrantFiled: March 30, 2006Date of Patent: February 14, 2012Assignee: Shionogi & Co., Ltd.Inventors: Toshiaki Masui, Kazuhiro Yoshida
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Patent number: 8115027Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound or the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: July 2, 2010Date of Patent: February 14, 2012Assignee: Shionogi & Co., Ltd.Inventors: Yasuyuki Kawanishi, Hideyuki Takenaka, Kohji Hanasaki, Tetsuo Okada
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Publication number: 20120029072Abstract: Disclosed are pleuromutilin derivatives of formula (I) an their use in the treatment of diseases mediated by microbes.Type: ApplicationFiled: October 4, 2011Publication date: February 2, 2012Inventors: Rosemarie Mang, Werner Heilmayer, Rudolf Badegruber, Dirk B. Strickmann, Rodger Novak, Mathias Ferencic, Atchyuta Rama Chandra Murty Bulusu
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Publication number: 20110313190Abstract: When sulfinating a carboxylic acid bromofluoroalkyl ester by using a sulfinating agent, an organic base is used, thereby obtaining a fluoroalkanesulfinic acid ammonium salt. This is oxidized to obtain a fluoroalkanesulfonic acid ammonium salt. This is used as the raw material and is converted to an onium salt or is converted to an onium salt by going through saponification and esterification, thereby obtaining a fluoroalkanesulfonic acid onium salt. This fluoroalkanesulfonic acid onium salt is useful as a photoacid generator used for chemically amplified resist materials, etc.Type: ApplicationFiled: March 12, 2010Publication date: December 22, 2011Applicant: Central Glass Company, LimitedInventors: Masashi Nagamori, Yuji Hagiwara, Takashi Masubuchi, Satoru Narizuka
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Publication number: 20110306600Abstract: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.Type: ApplicationFiled: June 10, 2011Publication date: December 15, 2011Applicant: Grunenthal GmbHInventor: Ramesh SESHA
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Publication number: 20110288329Abstract: The invention relates to a process for the preparation of trans 4-amino-cyclohexil ethyl acetate HCl wherein d) hydrogenating 4-nitrophenyl acetic acid in a protic solvent at a temperature between 40-50° C. in the presence of Pd/C under 0.1-0.6 bar overpressure, and e) further hydrogenating the 4-aminophenyl acetic acid obtained in situ in step a) at a temperature between 50-60° C. under 1-4 bar overpressures, then f) heating to reflux the 4-aminocyclohexil acetic acid obtained in step b) for 1-3 hours in hydrochloric ethanol, and if desired after removing the solvent acetonitrile was added to the residue obtained and distilled off.Type: ApplicationFiled: December 17, 2009Publication date: November 24, 2011Inventors: Tibor Bence Mathe, Olga Marianna Mathe, Julia Mathe Heiress, Laszlo Hegedus, Laszlo Czibula, Balint Juhasz, Judit Nagyne Bagdy, Denes Markos
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Publication number: 20110288328Abstract: A method for preparing a trans-{4-[(alkylamino)methyl]cyclohexyl}acetic acid, which is useful as a raw material compound for manufacture of medicaments and the like, comprising the step of reducing amide group of a compound represented by the following general formula (6) (R1 represents hydrogen atom or a C1-6 alkyl group, and R2 represents a C1-6 alkyl group, a C3-6 cycloalkyl group, a (C3-6 cycloalkyl)(C1-6 alkyl) group, a C6-10 aryl group, or a C7-12 aralkyl group).Type: ApplicationFiled: November 27, 2009Publication date: November 24, 2011Applicant: KOWA COMPANY, LTD.Inventors: Taichi Kusakabe, Koichi Yamazaki, Tadaaki Ohgiya, Kimiyuki Shibuya
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Publication number: 20110280931Abstract: Compounds of FIG. 3: ###FIG. 3### Whereby R and R1 preferentially correspond to ring structure consisting of FIG. : ###FIG. 4### Whereby R or R1, S or S1 is a Carbon, Nitrogen or Sulfur atom Z or Z1 and B or B1 is independently H or an alkyl, amino acid residue or amide thereof. Alternatively, Z or Z1 and B or B1 may constitute an fused, unsubstituted, cyclic ring structure, a cyclic amine or heterocyclic amine, or heavy metal, halogen or oxygen species. Compounds and derivatives are useful in treating conditions whereby matrix metalloproteinase activity is not desired, and inhibition is therapeutically beneficial.Type: ApplicationFiled: May 12, 2010Publication date: November 17, 2011Inventor: Curt Harold Grob
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Patent number: 8039661Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders. The invention also relates to processes for preparing compounds of the inventions.Type: GrantFiled: November 9, 2010Date of Patent: October 18, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy Brenchley, Jean-Damien Charrier, Steven Durrant, Ronald Knegtel, Sharn Ramaya, Shazia Sadiq
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Patent number: 8039663Abstract: The invention is based on the discovery that certain well-defined compounds derived from pentacyclopentadecane dimethanol are useful components in adhesive formulations. In particular, the invention compounds described herein provide high Tg values and low shrinkage. Compounds of the invention are useful as adhesives for use in the semiconductor packaging industry.Type: GrantFiled: April 9, 2008Date of Patent: October 18, 2011Assignee: Designer Molecules, Inc.Inventor: Stephen M. Dershem
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Publication number: 20110251392Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.Type: ApplicationFiled: June 24, 2011Publication date: October 13, 2011Inventors: George Wu, Anantha R. Sudhakar, Mingsheng Huang, Tao Wang, Vijay Sabesan, Ji Xie, Frank Xing Chen, Marc Poirier, Daw-long Kwok, Jian Cui, Xiaojing Yang, Tiruvettipuram K. Thiruvengadam, Jing Liao, Ilia A. Zavialov, Hoa N. Nguyen, Ngiap Kie. Lim
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Patent number: 8026279Abstract: A crystalline form of a ?-aminobutyric acid analog, and methods of preparing same, are provided.Type: GrantFiled: October 14, 2004Date of Patent: September 27, 2011Assignee: XenoPort, Inc.Inventors: Tono Estrada, Stephen P. Raillard
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Patent number: 8013015Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.Type: GrantFiled: October 1, 2009Date of Patent: September 6, 2011Assignee: Board of Regents, The University of Texas SystemInventors: Patrcik G. Harran, Michael S. Brown, Joseph L. Goldstein, Jing Yang, Tong-Jin Zhao
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Publication number: 20110212166Abstract: This invention concerns compounds of adamantanamines and neramexane, including their pharmaceutically-acceptable salts, diesterioisomers, and formulations for treating Alzheimer's related dementias, depression, AIDS related dementias, as antivirals, inflammatory diseases such as rheumatoid arthritis, and cerebral ischemia, hyperlipidemia, and diabetes.Type: ApplicationFiled: May 7, 2011Publication date: September 1, 2011Applicant: SSV Therapeutics, Inc.Inventor: Om P. Goel
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Publication number: 20110201577Abstract: The present application relates to processes for the preparation of oseltamivir and the H3PO4 salt of oseltamivir, Tamiflu®. The application further relates to novel intermediate compounds and to pharmaceutical compositions containing said compounds. The application further relates to a method of using the novel intermediates to treat or prevent influenza.Type: ApplicationFiled: May 12, 2009Publication date: August 18, 2011Applicant: BROCK UNIVERSITYInventors: Tomas Hudlicky, Bradford Sullivan
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Publication number: 20110184022Abstract: Compounds of formula (I), which are 14-O-{[(optionally substituted hydroxy)cyclohexyl)sulfanyl]acetyl}mutilins further substituted at the cyclohexyl group by an acylated amino group, salts and solvates thereof, pharmaceutical compositions comprising such compounds and their use as a pharmaceutical, e.g. for the treatment of diseases mediated by microbes and for the treatment of inflammation where microbese are mediating said inflammation.Type: ApplicationFiled: August 17, 2009Publication date: July 28, 2011Applicant: NABRIVA THERAPEUTICS AGInventors: Rosemarie Mang, Werner Heilmayer
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Publication number: 20110160303Abstract: The present invention generally relates to refreshing, soothing, and cooling compounds that affect sensory processes. More particularly, the present invention pertains to certain N-alkylcarbonyl-amino acid ester and N-alkylcarbonyl-amino lactone compounds as described herein; compositions and articles comprising such compounds; and methods of treatment, for example, methods of alleviating the discomforts of irritation, itch, and pain in the skin and in the linings of the oral cavity and upper respiratory tract, for example, in methods of treatment of cough and/or asthma.Type: ApplicationFiled: February 18, 2011Publication date: June 30, 2011Inventor: Edward Tak WEI
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Publication number: 20110160127Abstract: A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.Type: ApplicationFiled: April 15, 2009Publication date: June 30, 2011Applicant: TSRL, Inc.Inventors: John Hilfinger, Gordon Amidon
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Publication number: 20110130284Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the cis-alkoxyspirocyclic biphenyl-substituted tetramic acid derivatives of the formula (I) and, secondly, at least one crop plant compatibility-improving compound. The invention relates furthermore to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.Type: ApplicationFiled: November 22, 2007Publication date: June 2, 2011Applicant: Bayer CropScience AGInventors: Reiner Fischer, Christian Arnold, Olga Malsam, Jan Dittgen, Dieter Feucht, Ulrich Görgens, Martin Jeffrey Hills, Christopher Hugh Rosinger
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Publication number: 20110126734Abstract: The present disclosure relates to surface-modified zirconia nanoparticles, methods for making and using the same, and high index of refraction films made therefrom. The provided zirconia nanoparticles are surface modified with ligands that include N-hydroxyurea functionalities. The provided ligands also can contain compatibilizing groups that allow the provided surface-modified zirconia nanoparticles to be incorporated into an organic matrix. High index of refraction films can be made using these organic matrices.Type: ApplicationFiled: November 16, 2010Publication date: June 2, 2011Inventors: Guy D. JOLY, Nathan E. Schultz, Encai Hao
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Publication number: 20110118440Abstract: The invention provides compounds and methods, for example, to carry out organocatalytic Michael additions of aldehydes to cyclically constrained nitroethylene compounds catalyzed by a proline derivative to provide cyclically constrained ?-substituted-?-nitro-aldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96 to >99% e.e.). The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to cyclically constrained protected ?-amino acid residues, which are essential for systematic conformational studies of ?-peptide foldamers. New methods are also provided to prepare other ?-amino acids and peptides. These new building blocks can be used to prepare foldamers, such as ?/?-peptide foldamers, that adopt specific helical conformations in solution and in the solid state.Type: ApplicationFiled: October 14, 2010Publication date: May 19, 2011Inventors: Samuel Helmer Gellman, Li Guo, Michael Giuliano
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Publication number: 20110082111Abstract: Compounds of the following formula are provided for use with kinases: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: December 7, 2010Publication date: April 7, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Sheldon X. Cao, Victoria Feher, Takashi Ichikawa, Benjamin Jones, Stephen W. KALDOR, Andre A. KIRYANOV, Betty Lam, Yan Liu, Christopher McBride, Srinivasa Reddy Natala, Zhe Nie, Jeffrey A. Stafford
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Publication number: 20110082204Abstract: The present invention generally relates to refreshing, soothing, and cooling compounds that affect sensory processes. More particularly, the present invention pertains to certain N-alkylcarbonyl-amino acid ester as described herein; compositions and articles comprising such compounds; and methods of treatment, for example, methods of increasing alertness, and decreasing fatigue or sleepiness, and alleviating ocular discomforts of irritation, itch, and pain.Type: ApplicationFiled: December 6, 2010Publication date: April 7, 2011Inventor: Edward T. Wei
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Publication number: 20110082302Abstract: Disclosed are a process suited to large scale synthesis with high yield for producing oseltamivir phosphate, in which a preparation of oseltamivir phosphate which is highly safe as a pharmaceutical product can be produced, and an intermediate compound for producing oseltamivir phosphate. In this production process, an intermediate compound represented by general formula (V) is synthesized by employing Michael reaction/Michael reaction/Horner-Wadsworth-Emmons reaction, and oseltamivir phosphate is produced by converting the substituent groups in this intermediate compound.Type: ApplicationFiled: May 28, 2009Publication date: April 7, 2011Inventors: Yujiro Hayashi, Hayato Ishikawa
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Patent number: 7915309Abstract: The present application describes deuterium-enriched oseltamivir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: GrantFiled: June 20, 2007Date of Patent: March 29, 2011Assignee: Protia, LLCInventor: Anthony W. Czarnik
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Patent number: 7897803Abstract: The invention relates to a plurality of processes for the preparation of novel cis-alkoxy-substituted spirocyclic 1 H-pyrrolidine-2,4-dione derivatives of the formula (I) in which A, G, X and Y are as defined in the disclosure.Type: GrantFiled: November 10, 2009Date of Patent: March 1, 2011Assignee: Bayer CropScience AGInventors: Thomas Himmler, Reiner Fischer, Bernd Gallenkamp, Hans-Joachim Knops, Lubbertus Mulder, Reinhard Lantzsch, Christoph Erdelen, Angelika Lubos-Erdelen, legal representative, Jorg Konze, Ralf Nauen, Olga Malsam, Christian Arnold
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Publication number: 20110040120Abstract: Novel processes for the preparation of the anti-viral agent, Oseltamivir Phosphate and novel intermediates prepared in such processes. The novel processes use as starting materials D-glucose or D-xylose in the preparation of Oseltamivir Phosphate.Type: ApplicationFiled: October 21, 2010Publication date: February 17, 2011Applicant: APOTEX PHARMACHEM INC.Inventors: Bruno Konrad RADATUS, K.S. Keshava MURTHY, Gamini WEERATUNGA, Stephen E. HORNE, Kiran Kumar KOTHAKONDA, Eckardt C.G. WOLF, Zhongyi WANG
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Publication number: 20110039812Abstract: The present invention pertains to certain N-alkylcarbonyl-D-amino acid hydroxylalkyl esters (NACHE), including, for example, (R)-2-[((1R,2S,5R)-2-isopropyl-5-methyl-cyclohexanecarbonyl)-amino]-propionic acid 3-hydroxy-propyl ester, and compositions comprising such compounds, that target sensory elements on nerve fibers and which are usefully administered to refresh and cool the skin and mucous membranes. This disclosure generally relates to menthol-like cooling compounds, which do not have the smell, taste, or short duration of action of menthol. These compounds are designed for delivery onto the surfaces of the oral cavity, upper respiratory tract and skin. These compositions produce refreshing and cooling sensations and are expected to inhibit the perception of cough stimuli, itch, pain, and discomfort from the body's surfaces. In the oral cavity these compositions produce refreshing cooling without adverse effects on taste.Type: ApplicationFiled: November 5, 2007Publication date: February 17, 2011Inventor: Edward Tak Wei
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Publication number: 20110021762Abstract: A process is provided for the synthesis of 4,5-diamino cyclohexene carboxylate ester (1): or a pharmaceutically acceptable salt thereof. R1-R3 are a silyl-, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. R4, R11 and R12 are H, a silyl-group, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. 3,4-Dihydropyran compound (9): with R5 and R6 being suitable protecting groups, is reacted to form aldehyde (4): which is oxidized and converted to N-substituted carbamate (3): with R7 being a suitable protecting group. (3) is, via oxazolinidone (13): converted to azido carboxylate ester (2): and then to 4,5-diamino cyclohexene carboxylate ester (1).Type: ApplicationFiled: December 10, 2008Publication date: January 27, 2011Applicant: NANYANG TECHNOLOGICAL UNIVERSITYInventors: Xuewei Liu, Jimei Ma
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Patent number: 7858820Abstract: Described herein are both non-hygroscopic salts of L-carnitine and alkanoyl L-carnitine with taurine chloride (2-aminoethane-sulphonic chloride) and non-hygroscopic salts of L-carnitine and alkanoyl L-carnitine with glycine chloride which lend themselves favorably to the preparation of solid compositions suitable for oral administration. Also described are solid compositions containing said salts.Type: GrantFiled: September 28, 2001Date of Patent: December 28, 2010Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventor: Maria Ornella Tinti