The Nitrogen Is Bonded Directly To A Ring And Is In Same Side Chain As Ester Function Patents (Class 560/43)
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Publication number: 20120122708Abstract: New compounds are continually sought after for the treatment and prevention of disorders. The invention relates to N-(2-oxo-1-phenylpiperidin-3-yl)sulfonamides which can be biologically and pharmacologically traced, in order to be used in the search for, and identification of, new lead compounds that can modulate the functional activity of a biological target.Type: ApplicationFiled: December 29, 2011Publication date: May 17, 2012Inventors: JOSEP CASTELLS BOLIART, David Enrique MIGUEL CENTENO, Marta PASCUAL GILABERT
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Publication number: 20120122950Abstract: New compounds are continually being sought for the treatment and prevention of disorders. The invention relates to 1-(sulfonyl)-N-phenyl-pyrrolidine 2-carboxamides which can be used in the search for, and identification of, new lead compounds that could modulate the functional activity of a biological target.Type: ApplicationFiled: December 22, 2011Publication date: May 17, 2012Inventors: JOSEP CASTELLS BOLIART, David Enrique Miguel Centeno, Marta Pascual Gilabert
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Publication number: 20120122709Abstract: New compounds are continually sought after for the treatment and prevention of disorders. The invention relates to 1-(sulfonyl)-N-phenylpyrrolidine-2-carboxamides which can be biologically and pharmacologically traced, in order to be used in the search for, and identification of, new lead compounds that can modulate the functional activity of a biological target.Type: ApplicationFiled: December 29, 2011Publication date: May 17, 2012Inventors: JOSEP CASTELLS BOLIART, DAVID ENRIQUE MIGUEL CENTENO, MARTA PASCUAL GILABERT
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Publication number: 20120114633Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.Type: ApplicationFiled: April 6, 2010Publication date: May 10, 2012Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams
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Patent number: 8143448Abstract: The present invention relates to a process for the preparation of (2S,3S)-3-amino-N-cyclopropyl-2-hydroxyalkanamides as well as novel compounds prepared or used in the process.Type: GrantFiled: June 12, 2009Date of Patent: March 27, 2012Assignee: ViroBay, Inc.Inventor: Jeffrey Dener
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Publication number: 20120064034Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.Type: ApplicationFiled: November 10, 2011Publication date: March 15, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: ROBERT EDWARD BABINE, SHU HUI CHEN, IVAN COLLADO, CRISTINA GARCIA-PAREDES, JOHN IRVIN GLASS, DEQI GUO, LING JIN, JASON ERIC LAMAR, RAYMOND SAMUEL PARKER, III, NANCY JUNE SNYDER, XICHENG DAVID SUN, YVONNE YEE MAI YIP, Q. MAY WANG, FRANTZ VICTOR, MARK JOSEPH TEBBE, ROBERT B. PERNI, LUC FARMER
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Patent number: 8124802Abstract: The invention provides novel N-benzyl-N-propargyl-amines that are monoamine oxidase inhibitors, but generally exhibit little or no CNS effects.Type: GrantFiled: January 25, 2008Date of Patent: February 28, 2012Assignee: Jenrin Discovery, Inc.Inventors: John F. McElroy, Robert J. Chorvat
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Patent number: 8110703Abstract: The invention relates to a retinoid derivative and pharmaceutical composition and use thereof. The compound of the invention is capable of preventing or treating hematological tumors, such as acute leukemia, chronic leukemia, multiple myeloma and lymphoma, solid tumors, such as liver cancer, rectal cancer, mammary cancer and esophagus cancer, and skin disorders, such as psoriasis and acne.Type: GrantFiled: May 31, 2009Date of Patent: February 7, 2012Assignees: Anhui Medical University, Anhui New Star Pharmaceutical Development Co., Ltd.Inventors: Feihu Chen, Jingbo Shi, Yuan Wang, Jun Li, Juan Shen, Jingjing Ruan, Fanrong Wu
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Publication number: 20120028316Abstract: The present invention provides an enzymatic process for the preparation of (S)-5-(4-Fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one by the reduction of 1-(4-Fluoro-phenyl)-5-morpholin-4-yl-pentane-1,5-dione by using a suitable enzyme or by the resolution of (R,S)-5-(4-Fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one by using an enzyme. The present invention also provides process for the preparation of Ezetimibe comprising the steps of a) protecting the compound (S)-5-(4-Fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one with hydroxy protecting group b) hydrolyzing the obtained compound c) condensing with a chiral auxiliary d) reacting with an protected imine compound e) converting to alkyl ester f) cyclizing and g) deprotecting to obtain Ezetimibe.Type: ApplicationFiled: March 30, 2010Publication date: February 2, 2012Inventors: Mofazzal Husain, G.S.C Srikanth, Swapna Thorpunuri, Datta Debashish
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Publication number: 20110312007Abstract: Provided are compositions and methods for intracellular detection of enzyme activity. One example of a composition is a histone deacetylase substrate comprising a compound of the following formula (I): One example of a method is a method for detecting histone deacetylase activity comprising introducing a compound according to formula (I) to a plurality of cells and monitoring the cells with magnetic resonance spectroscopy.Type: ApplicationFiled: August 1, 2011Publication date: December 22, 2011Inventors: Sabrina M. Ronen, Juri G. Gelovani, William G. Bornmann, Jihai Pang, Ashutosh Pal, William P. Tong, David S. Maxwell, Madhuri Sankaranarayanapillai
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Patent number: 8080551Abstract: HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.Type: GrantFiled: June 26, 2006Date of Patent: December 20, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Jérôme Emile Georges Guillemont, Patrice Palandijian, Marc René De Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative
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Publication number: 20110263604Abstract: The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases.Type: ApplicationFiled: April 18, 2011Publication date: October 27, 2011Applicant: Oryzon Genomics, S.A.Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
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Publication number: 20110263873Abstract: 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: November 16, 2009Publication date: October 27, 2011Inventors: Murat Acemoglu, Andreas Pfaltz, Claude Schaerer
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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: 20110251393Abstract: The invention provides a helicene derivative, axially chiral amino acid, amine or amino alcohol derivative, and azaperylene, such as compounds represented by Formulae (I), (I?), (II), (II?), and (III): and a method for producing the same.Type: ApplicationFiled: October 20, 2009Publication date: October 13, 2011Applicant: KYOTO UNIVERSITYInventors: Takumi Furuta, Takeo Kawabata
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Publication number: 20110178084Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof are disclosed, wherein a dashed line represents the presence or absence of a bond; and, wherein Y, A, R, D, and n are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: May 13, 2009Publication date: July 21, 2011Applicant: ALLERGAN, INC.Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20110178088Abstract: This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.Type: ApplicationFiled: March 21, 2011Publication date: July 21, 2011Applicant: XENTION LIMITEDInventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
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Publication number: 20110137068Abstract: An amide derivative represented by Formula (3), which exhibits excellent efficacy in pest control effect, is produced by allowing a compound represented by the following Formula (1) and a compound represented by Formula (2) to react with each other. In Formula (1) to Formula (3), Y1 and Y2 each represent a halogen atom or a haloalkyl group; Rf represents a C3-C4 perfluoroalkyl group; and R1 and R2 each represent a hydrogen atom or an alkyl group; LG represents a leaving group; T represents a hydrogen atom or a fluorine atom; X1, X3, X4, and X5 each represent a hydrogen atom, a halogen atom, or the like; and A represents a nitrogen atom, a methine group, or the like.Type: ApplicationFiled: August 13, 2009Publication date: June 9, 2011Applicant: MITSUI CHEMICALS AGRO, INC.Inventors: Youji Aoki, Yumi Kobayashi, Hidenori Daido, Hiroyuki Katsuta, Hidetaka Tsukada, Atsushi Hirabayashi, Yusuke Takahashi, Michikazu Nomura, Atsuko Kawahara
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Publication number: 20110132439Abstract: Amorphous fullerene derivatives and their use in organic electronic devices that include the fullerene derivative as the electron acceptor component in the device's active layer.Type: ApplicationFiled: November 2, 2010Publication date: June 9, 2011Applicant: University of Washington Center for CommercializationInventors: Alex Kwan-yue Jen, Yong Zhang, Hin-Lap Yip
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Patent number: 7956195Abstract: The present invention discloses processes for the preparation and isolation of the individual stereoisomers of 1-amino, 3-substituted phenylcyclopentane-carboxylates.Type: GrantFiled: December 21, 2007Date of Patent: June 7, 2011Assignee: Abbott LaboratoriesInventors: Thomas D. Gordon, Grier A. Wallace, Martin E. Hayes, Kirill A. Lukin, Lei Wang, Dilinie P. Fernando
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Publication number: 20110130448Abstract: The present invention relates to a compound of the formula: R-AR—O—Y—R? Wherein R represents one or more members selected from H, alkoxy, benzyloxy, aldehyde, halogen, carboxylic acid, —NO2, —NH2, —NHCOCH3, and —NH—Y—R?, which is attached directly to AR or attached through an aliphatic chain. The carboxylic acid moiety in R includes but is not limited to the following carboxylic acids: benzoic acids, cinnamic acids, ferulic acid, caffeic acid, syringic acid, salicyclic acid, vanillic acid, phenylacetic acids, phenylpropionic acids, and sinapinic acid. -AR—O— is a biologically active phenolic moiety comprising 1 to 6 substituted or unsubstituted aryl rings that are directly bonded to each other, fused together, or joined through a linking group.Type: ApplicationFiled: December 7, 2010Publication date: June 2, 2011Applicant: Bezwada Biomedical LLCInventor: Rao S. Bezwada
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Publication number: 20110086818Abstract: The invention features methods, compositions, and kits for selective inhibition of pain-and itch sensing neurons (nociceptors and pruriceptors) by drug molecules of small molecule weight, while minimizing effects on non-pain-sensing neurons or other types of cells.Type: ApplicationFiled: March 11, 2009Publication date: April 14, 2011Applicants: Presidents and Fellows of Harvard College, The General Hospital CorporationInventors: Bruce P. Bean, Clifford J. Woolf
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Publication number: 20110027179Abstract: This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.Type: ApplicationFiled: October 14, 2010Publication date: February 3, 2011Inventors: Matthias FRIEBE, Peter Muschick, Andreas Huth
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Patent number: 7872151Abstract: The present invention relates to a phenylalanine derivative of Formula (I) wherein X1 is a halogen atom, X2 is a halogen atom, Q is a CH2R— is a carboxyl group which may be esterified; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 7, 2010Date of Patent: January 18, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Takayuki Kawaguchi, Sumihiro Nomura, Mikiko Tsukimoto, Toshiyuki Kume, Ila Sircar
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Patent number: 7868031Abstract: The present invention relates to propionamide compounds of formula I for use as antiinflammatory agents: wherein R1, R2 and R3 are as defined herein and pharmaceutically acceptable salts thereof. The invention also relates to methods of using the compounds of formula I and pharmaceutical compositions comprising the compounds of formula I.Type: GrantFiled: December 8, 2006Date of Patent: January 11, 2011Assignee: Roche Palo Alto LLCInventors: Leyi Gong, Counde O'Yang, Yun-chou Tan
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Publication number: 20100317865Abstract: Covalent conjugates of an ?,?-disubstituted glycine ester and a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid and the ?,?-disubstituted glycine ester is conjugated to the modulator at a position remote from the binding interface between the inhibitor and the target enzyme or receptor pass into cells and the active acid hydrolysis product accumulates within the cells.Type: ApplicationFiled: February 27, 2009Publication date: December 16, 2010Applicant: c/o Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Alan Hastings Drummond, David Festus Charles Moffat, Alistair David Graham Donald, Stephen John Davies
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Publication number: 20100279873Abstract: The invention relates to novel haloalkoxyspirocyclic tetramic and tetronic acid derivatives of the formula (I) in which W, X, Y, Z, A, D, Q1, Q2, m 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. Moreover, the invention provides selective herbicidal compositions comprising, firstly, haloalkoxyspirocyclic tetramic and tetronic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to increasing the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.Type: ApplicationFiled: September 12, 2008Publication date: November 4, 2010Applicant: BAYER CROPSCIENCE AGInventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Christian Arnold, Jan Dittgen, Dieter Feucht, Heinz Kehne, Olga Malsam, Christopher Hugh Rosinger, Eva-Maria Franken, Ulrich Görgens
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Patent number: 7807708Abstract: Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.Type: GrantFiled: June 25, 2007Date of Patent: October 5, 2010Assignee: Galderma Research & DevelopmentInventors: Thibaud Biadatti, Laurence Dumais, Catherine Soulet, Sandrine Talano, Sebastien Daver
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Patent number: 7799739Abstract: Novel biphenylcarboxamides of the formula (I) There is further provided a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: GrantFiled: December 5, 2006Date of Patent: September 21, 2010Assignee: Bayer CropScience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Herbert Gayer, Arnd Voerste, Ulrike Wachendorff-Neumann, Peter Dahmen
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Publication number: 20100196922Abstract: The present invention provides fluorogenic compounds for the detection of target metal ions wherein the compounds exhibit a Stokes shift greater than 50 nm and the detectable signal is modulated by photoinduced electron transfer (PET). The present compounds consist of three functional elements, the ion sensing moiety (chelating moiety), the reporter moiety (fluorophore or fluorescent protein) and spacer or linker between the sensing and reporter moieties of the present compound that allows for PET upon binding of a metal ion and excitation by an appropriate wavelength.Type: ApplicationFiled: December 31, 2009Publication date: August 5, 2010Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Kyle Richard GEE, Vladimir Martin
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Publication number: 20100168068Abstract: The invention provides novel compounds of formulae I and II: that are monoamine oxidase-B inhibitors, which can be useful in treating obesity, diabetes, and/or cardiometabolic disorders (e.g., hypertension, dyslipidemias, high blood pressure, and insulin resistance).Type: ApplicationFiled: December 31, 2009Publication date: July 1, 2010Applicant: JENRIN DISCOVERYInventors: John Francis McElroy, Robert J. Chorvat, Parthasarathi Rajagopalan
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Publication number: 20100158996Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R9 and R9 are each independently hydrogen atom, C1-C6 alkyl, —CON(R18) (R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.Type: ApplicationFiled: February 12, 2010Publication date: June 24, 2010Inventors: Atsushi Hagiwara, Yasuhiro Ohe, Naoya Odani, Shizue Watanabe, Taku Ikenogami, Takashi Kawai, Kenya Madono, Toshio Taniguchi
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Publication number: 20100139773Abstract: N-bridged PCBMs are prepared by the cycloaddition of an organic azide to C60. The N-bridged PCBMs are imino PCBMs, exemplified by an isomeric mixture of [5,6]-open APCBM and [6,6]-closed APCBM. An organic electronic material containing a fullerene adduct, such as an organic field effect transistor or an organic photovoltaic device, is provided containing the N-bridged PCBM as the fullerene adduct.Type: ApplicationFiled: October 21, 2009Publication date: June 10, 2010Inventors: Changduk Yang, Fred Wudl
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Publication number: 20100144977Abstract: A variety of curing agents for epoxy resins and methods for preparation thereof are disclosed, including compounds having the structures of formulas III and IV: wherein each of R1, R2, R3, R4, and R5 is independently selected from the group consisting of H, methyl, ethyl, n-propyl, iso-propyl, a butyl, and phenyl. Epoxy-based compositions including various curing agents are also disclosed. Other epoxy curatives containing amino, phenol, and/or imine groups are disclosed.Type: ApplicationFiled: November 20, 2009Publication date: June 10, 2010Applicant: DESIGNER MOLECULES, INC.Inventor: Stephen M. Dershem
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Publication number: 20100137296Abstract: Compounds that can be used as openers or blockers of voltage-dependent potassium channels, and which are useful in the treatment of conditions such as central or peripheral nervous system disorders through the modulation of potassium ion flux through voltage-dependent potassium channels and/or depressing or enhancing cortical and/or peripheral neuron activity, compositions containing same and methods utilizing same are disclosed. Also disclosed are modulators of voltage-dependent potassium channels, which exhibit blocking of a TRPV1 channel, and hence are useful in the treatment of TRPV1-related conditions.Type: ApplicationFiled: September 18, 2008Publication date: June 3, 2010Applicant: Ramot At Tel Aviv University Ltd.Inventors: Bernard Attali, Asher Peretz
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Publication number: 20100137599Abstract: The present invention relates to a process for the preparation of 1,4-butanediol mononitrate as intermediate for large scale preparation of high purity nitrooxybutyl ester of pharmaceutically active compounds.Type: ApplicationFiled: June 18, 2008Publication date: June 3, 2010Applicant: NICOX S.A.Inventors: Achim Hack, Gunter Weingarner, Matthias Kramer
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Publication number: 20100130754Abstract: The present invention relates to the field of catalytic hydrogenation and, more particularly, to the use of Ru complexes with bidentate ligands, having one amino or imino coordinating group and one phosphino coordinating group, in hydrogenation processes for the reduction of esters or lactones into the corresponding alcohol or diol respectively.Type: ApplicationFiled: January 27, 2010Publication date: May 27, 2010Inventors: Lionel Saudan, Philippe Dupau, Jean-Jacques Riedhauser, Patrick Wyss
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Publication number: 20100105921Abstract: A process for preparing hydroxamic acids is provided. The process comprises reacting an aldehyde with a nitroso compound in the presence of a N-heterocyclic carbene (NHC) catalyst.Type: ApplicationFiled: March 20, 2008Publication date: April 29, 2010Inventor: Yugen Zhang
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Publication number: 20100093733Abstract: Compounds of formula (I): or pharmaceutically acceptable salts and esters thereof, are useful for the treatment of obesity, type II diabetes and the metabolic syndrome.Type: ApplicationFiled: February 15, 2008Publication date: April 15, 2010Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Graham Dawson, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Philippe Wong-Kai-In
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Publication number: 20100087668Abstract: The present disclosure provides for the synthesis of branched polyamines. In embodiments, branched polyamines may be formed by reacting a branched polyol with a nitroaryl carboxylic acid to form a nitrobenzoyl ester which, in turn, may then be subjected to a hydrogenating step to form the branched polyamine. The resulting branched polyamine may then be reacted with another hydrogel precursor to form a hydrogel.Type: ApplicationFiled: July 14, 2009Publication date: April 8, 2010Inventor: Mbiya Kapiamba
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Publication number: 20100063312Abstract: The present invention describes a process for the synthesis of an amino acid methyl ester comprising the following steps: (a) refluxing a reaction mixture comprising a free amino acid, methanol and a strong acid; (b) concentrating the mixture; (c) adding methanol; (d) repeating steps a-c one or more times.Type: ApplicationFiled: March 10, 2008Publication date: March 11, 2010Inventor: Harold Monro Moody
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Publication number: 20100048550Abstract: The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta(TR-Beta). Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them.Type: ApplicationFiled: October 15, 2007Publication date: February 25, 2010Inventors: Saurin Raval, Preeti Raval, Braj Lohray, Vidya Bhushan Lohray, Pankaj R. Patel
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Publication number: 20100041665Abstract: The present invention is related to a family of N-phenyl-prenylamine derivatives of formula (I), and to their use in the treatment of cognitive, neurodegenerative or neuronal diseases or disorders, such as Alzheimer's disease or Parkinson's Disease. The present invention also relates to pharmaceutical compositions comprising the same. Further, the present invention is directed to the use of the compounds in the manufacture of a medicament for the treatment and/or prevention of a cognitive, neurodegenerative or neuronal disease or disorder.Type: ApplicationFiled: August 1, 2007Publication date: February 18, 2010Applicant: NOSCIRA, S.A.Inventors: Ana Martinez Gil, Ana Castro Morera, Miguel Medina Padilla, Pilar Munoz Ruiz, Javier Lopez Ogalla, Esther Garcia Palomero, Celia De Austria De Luque, Paola Usan Egea, Rita Valenzuela Liminana, Pablo Garcia Fernandez, Elena Delgado Hernandez, Daniel Ignacio Perez Fernandez
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Publication number: 20100036149Abstract: The present invention provides an industrially advantageous production method of optically active tetrahydroquinolines of formula (1), which comprises: 1) a step of reacting a ?-ketoester of formula (2) with an amine of formula (3) to produce an enaminoester of formula (4); 2) a step of subjecting the enaminoester of formula (4) above obtained in 1) to asymmetric hydrogenation to produce an optically active ?-amino acid derivative of formula (5); 3) a step of amidating the optically active ?-amino acid derivative (5) above obtained in 2) to produce an amide of formula (6); 4) a step of alkoxycarbonylating the amide of formula (6) above obtained in 3) to produce a compound of formula (7); and 5) a step of subjecting the compound of formula (7) above to cyclization to produce the optically active tetrahydroquinoline of formula (1).Type: ApplicationFiled: August 31, 2009Publication date: February 11, 2010Applicant: TAKASAGO INTERNATIONAL COPORATIONInventors: Takashi Moroi, Tsukasa Sotoguchi, Kazuhiko Matsumura, Motonobu Takenaka, Wataru Kuriyama, Toshiyuki Murayama, Hideki Nara, Tohru Yokozawa, Kenji Yagi
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Patent number: 7645793Abstract: The present invention relates to a process for suppressing the foaming which may occur at the time of the preparation of a solution or a suspension. Particularly, the present invention relates to pharmaceuticals, foods, and the like wherein the foaming at the time of the preparation of a solution or a suspension, which may cause any disadvantage, is suppressed.Type: GrantFiled: July 16, 2002Date of Patent: January 12, 2010Assignee: Shionogi & Co., Ltd.Inventors: Yasuhiro Miyako, Hideaki Tai, Kazuichi Fujikane
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Publication number: 20090312571Abstract: The present invention relates to a process for the preparation of (2S,3S)-3-amino-N-cyclopropyl-2-hydroxyalkanamides as well as novel compounds prepared or used in the process.Type: ApplicationFiled: June 12, 2009Publication date: December 17, 2009Applicant: ViroBay, Inc.Inventor: Jeffrey Dener
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Patent number: 7625988Abstract: The present invention is directed to novel flame retardant monomers and polymers, wherein the flame retardant properties of the polymers are provided by functionality in pendant groups attached to a polymer backbone (as opposed to the polymer backbone itself possessing flame retardant properties. The present invention is also directed to methods of making such polymers and monomers, and articles of manufacture incorporating such monomers and polymers.Type: GrantFiled: June 18, 2004Date of Patent: December 1, 2009Assignee: William Marsh Rice UniversityInventors: James M. Tour, Joshua L. Jurs, Jason J. Stephenson
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Patent number: 7612225Abstract: Disclosed herein are a novel crystal of a novel triterpene derivative, a method for producing the crystals, and a pharmaceutical preparation obtained by using the crystals.Type: GrantFiled: March 24, 2005Date of Patent: November 3, 2009Assignee: Shionogi & Co., Ltd.Inventor: Masataka Fumoto
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Publication number: 20090264469Abstract: The present patent application concerns new compounds of formula (I): displaying agonistic activity at sphingosine-1-phosphate (S1P) receptors, their process of preparation and their use as immunosuppressive agents.Type: ApplicationFiled: October 18, 2005Publication date: October 22, 2009Applicants: BIO-PROJET, SUN PHARMACEUTICAL INDUSTRIES LTD.Inventors: Marc Capet, Nicolas Levoin, Isabelle Berrebi-Bertrand, Olivia Poupardin, Philippe Robert, Jean-Charles Schwartz, Jeanne-Marie Lecomte, Thennati Rajamannar, Ranjan Kumar Pal, Biswajit Samanta, Jignesh K. Jivani, Bhavesh M. Panchal, Isha H. Bhatt, Jayraj D. Aradhye
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Publication number: 20090240052Abstract: An anthranilic acid derivative represented by the general formula (X) [wherein R1 represents hydrogen or a carboxy-protecting group; R2 represents optionally substituted phenyl, a heterocyclic group, etc.; R3 represents optionally substituted phenyl, a monocyclic heterocyclic group, etc.; X1 represents carbonyl, etc.; X2 represents optionally substituted alkylene group, a bond, etc.; X3 represents oxygen, a bond, etc.; and X4 represents a group represented by the general formula -X5-X6- or -X6-X5- (wherein X5 means oxygen, a bond, etc.; and X6 means optionally substituted alkylene, a bond, etc.)] or a salt of the derivative. The derivative or salt has the inhibitory activity of MMP-13 production and is hence useful as a therapeutic agent for articular rheumatism, osteoarthritis, cancer, etc.Type: ApplicationFiled: December 6, 2005Publication date: September 24, 2009Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Yukie Tada