Oxy Patents (Class 562/444)
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Publication number: 20090036673Abstract: An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxicarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.Type: ApplicationFiled: July 24, 2008Publication date: February 5, 2009Applicant: JAPAN SCIENCE AND TECHNOLOGY AGENCYInventors: Tohru FUKUYAMA, Toshiyuki KAN
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Publication number: 20090010882Abstract: The present invention relates to amorphous and polymorphic forms of sodium 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoate and their use for facilitating the delivery of active agents, such as insulin, to a target.Type: ApplicationFiled: July 2, 2008Publication date: January 8, 2009Applicant: Emisphere Technologies, Inc.Inventors: Satej Bhandarkar, Shingai Majuru, Halina Leuchyk
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Patent number: 7459582Abstract: There is provided methods for producing nateglinide crystals, which comprises the steps of adding an acid(s) to a reaction mixture containing nateglinide to make it acidic, the reaction mixture being obtained by reacting trans-4-isopropylcyclohexylcarbonyl chloride with D-phenylalanine in a mixed solvent of ketone solvent and water in the presence of an alkali; and then adjusting the temperature of the mixture to 58° C. to 72° C. and the concentration of ketone solvent to more than 8 wt % and less than 22 wt % to conduct precipitation of nateglinide crystals. This producing method is the industrially beneficial methods for crystallization of nateglinide.Type: GrantFiled: March 14, 2007Date of Patent: December 2, 2008Assignee: Ajinomoto Co., Inc.Inventors: Daisuke Takahashi, Seiichi Nishi, Satoji Takahashi
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Publication number: 20080292552Abstract: The invention relates to novel 18F-labelled compounds which may be suitable for use as Positron Emission Tomography (PET) radiotracers, and to processes for preparation of such. The 18F-labelled compounds of the invention comprise a [18F]fluoroalkenyl group.Type: ApplicationFiled: December 15, 2006Publication date: November 27, 2008Inventors: Erik Arstad, Edward George Robins
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Publication number: 20080248012Abstract: A promoter of ATP release from red blood cells, comprising a substance capable of stabilizing the structure of hemoglobin in red blood cells in its T-state; and a method of releasing ATP from red blood cells with the use of the promoter. There are further provided an inhibitor of ATP release from red blood cells, comprising a substance capable of stabilizing the structure of hemoglobin in red blood cells in its R-state; and a method of inhibiting ATP release from red blood cells with the use of the inhibitor.Type: ApplicationFiled: July 1, 2004Publication date: October 9, 2008Applicant: KEIO UNIVERSITYInventor: Makoto Suematsu
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Patent number: 7427600Abstract: The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.Type: GrantFiled: August 23, 2004Date of Patent: September 23, 2008Assignee: Shire LLCInventors: Travis Mickle, Suma Krishnan, James Scott Moncrief, Christopher Lauderback, Thomas Piccariello, Randal Kirk
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Patent number: 7425648Abstract: The present invention relates to a process for the preparation of nateglinide, preferably in B-form, substantially free from the H-form, comprising three steps starting from D-phenylalanine methyl ester or a salt thereof.Type: GrantFiled: January 3, 2005Date of Patent: September 16, 2008Assignee: A.M.S.A. Anonima Materie Sintetiche E. Affini S.p.A.Inventors: Enrico Vigano', Enrica Pizzatti, Simona Lanfranconi, Renato Molteni, Ernesto Landonio
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Patent number: 7423172Abstract: Compounds of general formula I, and the salts and solvates thereof, wherein R1 represents the radical 2-benzoylphenylamino; R2 represents —(CH2)s—N(COR3)-A-J-T or —(CH2)s—N(R4)—B-J-T; and s. R3, R4, A, B, J and T have the meanings disclosed in the description. These compounds are PPAR? modulators and, therefore, are useful for the treatment or prevention of a condition or a disease mediated by these receptors.Type: GrantFiled: July 29, 2005Date of Patent: September 9, 2008Assignee: Laboratorios Salvat, S.A.Inventors: Carmen Serra Comas, Anna Fernández Serrat, Dolors Balsa López, Isabel Masip Masip, Juan Lorenzo Catena Ruiz, José Hidalgo Rodriguez, Carmen Lagunas Arnal, Carolina Salcedo Roca, Andrés Fernández García
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Publication number: 20080152603Abstract: The present invention relates to the use of compounds of the formula (I), with radicals defined in the description, as antioxidants, to corresponding novel compounds and compositions, and to corresponding processes for the preparation of compounds and compositions.Type: ApplicationFiled: March 21, 2006Publication date: June 26, 2008Inventors: Thomas Rudolph, Herwig Buchholz
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Publication number: 20080146509Abstract: The present invention relates to a composition comprising a delivery agent, parathyroid hormone, and calcitonin. This composition exhibits increased delivery of parathyroid hormone and/or calcitonin and is useful for the treatment of osteoporosis. The composition also permits simultaneous oral delivery of parathyroid hormone and calcitonin. The composition of the present invention may be formulated into a dosage unit form, such as an oral dosage unit form. The invention also provides a method for administering parathyroid hormone and calcitonin to an animal in need thereof by administering the composition of the present invention.Type: ApplicationFiled: February 25, 2008Publication date: June 19, 2008Applicant: EMISPHERE TECHNOLOGIES, INC.Inventor: Michael M. Goldberg
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Patent number: 7384982Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are indepedently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substitued or unsubstituted C2-C16 alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above.Type: GrantFiled: July 7, 2003Date of Patent: June 10, 2008Assignees: Emisphere Technologies, Inc., Novartis AGInventors: William E. Bay, Rajesh K. Agarwal, Kiran Chaudhary, Shingai Majuru, Michael M. Goldberg, JoAnne P. Russo, Mosise Azria, Joseph M. Ault, Simon D. Bateman, Subash Patel, Joseph Sikora, Rebecca F. Yang, Joseph L Zielinski
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Publication number: 20080114064Abstract: The invention relates to a compound selected from one or more of the following: a tris (hydroxymethyl) methylamine salt of (2S)-2-ethoxy-3-(4-{2-[hexyl (2-phenylethyl) amino]-2-oxoethoxy}phenyl) propanoic acid; an ethanol amine salt of (2S)-2-ethoxy-3-(4-{2-[hexyl (2-phenylethyl) amino]-2-oxoethoxy}phenyl) propanoic acid; or a pharmaeutical composition comprising the compound.Type: ApplicationFiled: December 14, 2005Publication date: May 15, 2008Applicant: ASTRAZENECA ABInventors: Rebecca J. Booth, Mikael Dahlstrom
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Patent number: 7314955Abstract: The present invention relates to a novel crystalline form of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine and methods for preparing the same.Type: GrantFiled: April 29, 2002Date of Patent: January 1, 2008Assignee: Biocon LimitedInventors: Shanmughasamy Rajamahendra, Chandrashekhar Aswathanarayanappa, Tom Thomas Puthiaparampil, Madhavan Sridharan, Sambasivam Ganesh
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Patent number: 7314890Abstract: The present invention provides wherein R1 is selected from the group consisting of C1-C10 alkoxy, OH and NR4R5; R2 is selected from the group consisting of C1-C10 alkyl and (CH2)nOH; R3 is selected from the group consisting of C1-C10 alkyl, heteroaryl, e.g. thienyl, furanyl and pyridyl, phenyl, mono, -di-, tri-substituted phenyl and heteroaryl; R4 and R5 are independently selected from the group consisting of H, C1-C10 alkyl, C1-C10 alkyl hydroxyl; m is 0 or an integer from 1 to 3 and n is an integer of from 1 to 4. These compounds are useful in lowering intraocular pressure and/or treating glaucoma or providing neuroprotection to the eye of a human patient.Type: GrantFiled: June 26, 2006Date of Patent: January 1, 2008Assignee: Allergan, Inc.Inventor: Robert M. Burk
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Patent number: 7265245Abstract: The present invention provides new amyloidogenesis inhibiting compounds of formula (I): in which R1 is a —NRaRb group, where Ra and Rb, independently, are a hydrogen atom or a C1-C6 alkyl group; —ORC group, where RC is a hydrogen atom or a C1-C6 alkyl group; a glycosyl; a C1-C6 polyhydroxyalkyl; or a —NH—CH(Rd)—COORe group, where Rd is a side chain of one of the 20 natural alpha-amino acids in either of their two enantiomerically pure forms L or D, and Re is a hydrogen atom or a C1-C6 alkyl group; and R2 is a hydrogen atom, a C1-C6 alkyl group, a glycosyl; a C1-C6 polyhydroxyalkyl; —C(?O)—Rf group, where Rf is a C1-C6 alkyl group; or a —CH2—COO—Rg group, where Rg is a hydrogen atom or a C1-C6 alkyl group; and pharmaceutically acceptable salts thereof, which are useful in the treatment of neurodegenerative diseases, among others.Type: GrantFiled: October 8, 2003Date of Patent: September 4, 2007Assignee: Innovaprotean, S.LInventors: Maria Joao Mascarenhas Saraiva, Maria do Rosario Rodrigues Almeida, José Barluenga Mur, Alfredo Ballesteros Gimeno, Antoni Planas Sauter, Gemma Arsequell Ruiz, Gregorio Valencia Parera
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Patent number: 7247746Abstract: New crystal forms of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine, also known asnateglinide, may be produced by dissolving nateglinide in any of its forms, including solvates, in an organic solvent to form a solution followed by precipitation of nateglinide from the solution, and isolating and drying the precipitated crystal form of nateglinide. The precipitation of nateglinide may be induced either by cooling the solution, or by addition of another solvent which is miscible with the first solvent but in which nateglinide is only poorly soluble, or by combination of the two. Depending on the solvent a specific crystal form of nateglinide may be obtained, e.g., the R?-type crystal form of nateglinide produced by the described method has a different melting point, infra red spectra and X-ray diffraction patterns from the previously known crystal forms of nateglinide.Type: GrantFiled: April 14, 2003Date of Patent: July 24, 2007Assignee: Novartis, AGInventor: Paul Allen Sutton
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Patent number: 7247652Abstract: L-threo-?-benzyloxyaspartate derivatives having a substituent on the benzene ring, represented by the following formula (1): wherein R is hydrogen, a linear or branched lower aliphatic acyl group with the acyl portion optionally substituted, an alicyclic acyl group, an aromatic acyl group with a substituent on the aromatic ring, an amino acid-derived group or a biotin derivative-derived group, having an amino substituent on the benzene ring, and salts thereof, which can easily bind to affinity column chromatography carriers as ligands of glutamate transporter proteins.Type: GrantFiled: June 24, 2002Date of Patent: July 24, 2007Assignee: Suntory LimitedInventor: Keiko Shimamoto
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Patent number: 7217835Abstract: The present invention relates to a method of producing a compound represented by the formula [I] or a salt thereof, which comprises reacting a compound represented by the formula [II] or a salt thereof with a compound represented by the formula [III] or a salt thereof, in the presence of a base, in alcohol, and provides a production method of an O-substituted tyrosine compound, which is superior in productivity, versatility and safety, and economically and industrially useful: wherein each symbol is as defined in the specification.Type: GrantFiled: September 10, 2004Date of Patent: May 15, 2007Assignee: Ajinomoto Co., Inc.Inventors: Takayuki Hamada, Masanobu Yatagai
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Patent number: 7208622Abstract: There is provided methods for producing nateglinide crystals, which comprises the steps of adding an acid(s) to a reaction mixture containing nateglinide to make it acidic, the reaction mixture being obtained by reacting trans-4-isopropylcyclohexylcarbonyl chloride with D-phenylalanine in a mixed solvent of ketone solvent and water in the presence of an alkali; and then adjusting the temperature of the mixture to 58° C. to 72° C. and the concentration of ketone solvent to more than 8 wt % and less than 22 wt % to conduct precipitation of nateglinide crystals. This producing method is the industrially beneficial methods for crystallization of nateglinide.Type: GrantFiled: April 18, 2003Date of Patent: April 24, 2007Assignee: Ajinomoto Co., Inc.Inventors: Daisuke Takahashi, Seiichi Nishi, Satoji Takahashi
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Patent number: 7183430Abstract: The invention relates to compounds having formula (I), which can block the response to chemical substances or thermal stimuli or mediators of inflammation of nociceptors, a production method thereof and compositions containing same.Type: GrantFiled: May 16, 2003Date of Patent: February 27, 2007Assignee: Diverdrugs, S.L.Inventors: Antonio Ferrer Montiel, Asia Fernández Carvajal, Carolina Garcia Martínez, Carlos Belmonte Martínez, Wim Van Den Nest, Cristina Carreño Serraïma
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Patent number: 7166606Abstract: The compounds of formula (I) in which R represents a hydrogen atom or a fluorine atom, or a pharmaceutically acceptable salt thereof are Factor Xa inhibitors useful in the treatment of thrombotic disorders.Type: GrantFiled: March 24, 2003Date of Patent: January 23, 2007Assignee: Eli Lilly and CompanyInventors: Michael Robert Wiley, Gary Lowell Engel
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Patent number: 7153997Abstract: This invention relates to novel compounds, which are thyroid receptor ligands, and to methods of preparing such compounds. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described herein is administered in a therapeutically effective amount.Type: GrantFiled: July 8, 2003Date of Patent: December 26, 2006Assignees: Karo Bio AB, Bristol-Myers Squibb CompanyInventors: Neeraj Garg, Mahmoud Rahimi Ghadim, Thomas Anders Wilson Ericsson, Lars Johan Malm, Denis Evan Ryono
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Patent number: 7153869Abstract: This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.Type: GrantFiled: March 12, 2004Date of Patent: December 26, 2006Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
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Patent number: 7145040Abstract: The present invention provides process useful for the preparation of intermediates which are useful in the preparation of amino acids useful in preparing peptide receptor modulators, for example agonists or partial agonists of such peptide receptors. Such peptide receptor modulators include, for example glucagon like peptide-1 receptor modulators which are useful for the amelioration of the diabetic condition.Type: GrantFiled: June 30, 2005Date of Patent: December 5, 2006Assignee: Bristol-Myers Squibb Co.Inventors: Arvind Mathur, K. Selva Kumar
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Patent number: 7081535Abstract: Hydroxy-amino acids are provided and are prepared by contacting a substituted ?-ketodiester having a ketone group and two ester functional groups with a ketoreductase under conditions permitting the reduction of the keytone group to an alcohol. Only one of the ester functional groups is regioselectively hydrolyzed to the corresponding carboxylic acid, whereby a non-hydrolyzed ester functional group remains. The carboxylic acid is converted to an amine to produce a hydroxy-amino acid.Type: GrantFiled: December 16, 2004Date of Patent: July 25, 2006Assignee: BioCatalytics, Inc.Inventors: J. David Rozzell, Jr., Spiros Kambourakis
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Patent number: 7071350Abstract: The present invention relates to a method for introducing an amino group into an organic acid or an organic ester by reacting an organic salt or an organic ester and ammonia under high-temperature and high-pressure water conditions, a method for synthesizing an amino acid or an amino ester by the above method, and a method for manufacturing an amino acid compound by synthesizing an amino acid or an amino ester by the above method and separating and refining it with an ion exchange resin.Type: GrantFiled: October 30, 2001Date of Patent: July 4, 2006Assignee: National Institute of Advanced Industrial Science and TechnologyInventors: Kiyotaka Hatakeda, Osamu Sato, Mitsuhiro Kanakubo, Yutaka Ikushima, Kazuo Torii
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Patent number: 7057066Abstract: The present invention provides a process for preparing 3-amino-2-hydroxypropionic acid derivatives (1) which does not use dangerous reagents, is economically advantageous, and is suitable for an industrial production, which process comprises: treating N-protected-3-amino-2-hydroxypropionic acid derivatives (2) having a steric configuration at 2-position carbon reverse to that of derivatives (1) with a leaving group-introducing agent to convert into N-protected-3-aminopropionic acid derivatives (3), then treating the derivatives with a basic substance to convert into substituted-3-amino-2-hydroxypropionic acid derivatives (4) having an inverted steric configuration at 2-position carbon, and then converting the derivatives into 3-amino-2-hydroxypropionic acid derivatives (1).Type: GrantFiled: June 26, 2001Date of Patent: June 6, 2006Assignee: Kaneka CorporationInventors: Hiroshi Murao, Koki Yamashita, Toshihiro Takeda, Yasuyoshi Ueda
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Patent number: 7056707Abstract: The present invention relates to a novel compound having a molecular formula C13H15NO5 having molecular structure of Formula I and a process for the isolation of said compound. The present invention also relates to a method of inhibiting 13-lipoxygenase and having free radical scavenging activity.Type: GrantFiled: December 2, 2003Date of Patent: June 6, 2006Assignee: Council of Scientific and Industrial ResearchInventors: Avinash Prahlad Sattur, Chandrasekhar Rao Kadiyala, Divakar Soundar, Karanth Naikanakatte Ganesh, Tumkur Ramachandraiah Shamala, Appu Rao Appu Rao Gopal Rao
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Patent number: 7034178Abstract: This invention is drawn to a process for the production of (R,R)-phenylisoserine or a 1–4C-alkyl ester thereof.Type: GrantFiled: June 27, 2002Date of Patent: April 25, 2006Assignee: Altana Pharma AGInventors: Wijnand Faber, Jan Koek, Jörg Senn-Bilfinger, Ton Vries
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Patent number: 7030268Abstract: There is provided a method for producing easily highly-purified acylphenylalanine that is useful as a raw material of pharmaceutical products and the like, which comprises the step of reacting an acid chloride with phenylalanine in a mixed solvent of an organic solvent and water, while keeping the solvent under the alkali condition by using potassium hydroxide.Type: GrantFiled: April 18, 2003Date of Patent: April 18, 2006Assignee: Ajinomoto Co., Inc.Inventors: Michito Sumikawa, Takao Ohgane
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Patent number: 7005538Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac arrhythmias, thyrotoxicosis and subclinical hyperthyrodism.Type: GrantFiled: November 16, 2000Date of Patent: February 28, 2006Assignee: Karo Bio ABInventors: Johan Malm, Chris Litten, Theresa Apelqvist, Asa Hedfors, Peter Brandt, Karin Edvinsson, Sandra Gordon
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Patent number: 6992067Abstract: Compounds of the formula I, in which R1, R2, R3, R4, R5, and R6 have the meanings given in the description, and their physiologically acceptable salts. The compounds are suitable for use, for example, as hypolipidemics.Type: GrantFiled: December 19, 2001Date of Patent: January 31, 2006Assignee: Aventis Pharma Deutschland GmbHInventors: Heiner Glombik, Werner Krame, Stefanie Flohr, Wendelin Frick, Hubert Heuer, Gerhard Jaehne, Andreas Lindenschmidt, Hans-Ludwig Schäfer
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Patent number: 6989380Abstract: A method of treating pain by the co-administration of an antidepressant together with one or more precursors or inducers of neurotransmitters, particularly amino acids selected from L-phenylalanine, L-tyrosine, L-tryptophan and L-DOPA.Type: GrantFiled: August 7, 2002Date of Patent: January 24, 2006Assignee: The WKK TrustInventors: David Frederick Horrobin, Cari Loder, Graham Cooper
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Patent number: 6989402Abstract: New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR?R?) or an acylsulphonamide (CONHSO2R?) derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, R4 may be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR?R?). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5=H).Type: GrantFiled: December 23, 1999Date of Patent: January 24, 2006Assignee: Karo Bio ABInventors: Jon Hangeland, Minsheng Zhang, Yolanda Caringal, Denis Ryono, Yi-Lin Li, Johan Malm, Ye Liu, Neeraj Garg, Chris Litten, Ana Maria Garcia Collazo, Konrad Koehler
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Patent number: 6982098Abstract: The present invention relates to an agent that suppresses appetite and provides quick energy. According to at least one aspect of the present invention, a lollipop is provided that suppresses appetite and provides quick energy. The lollipop is made from a premixed herbal formula that is combined with a hard candy confection base. The herbal premixed formula includes the following active ingredients: Guarana PE 22%; CitriMax®; and L-Tyrosine. The herbal premix formula can also include Vitamin B6; and Vitamin B12 Cyanacobalamin. The premixed formula is added to a candy base that may include corn syrup, Maltodextrin, sugar, natural color and natural flavorings.Type: GrantFiled: May 26, 2004Date of Patent: January 3, 2006Assignee: Fun Unlimited Inc.Inventor: Michael P. Wenniger
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Patent number: 6921774Abstract: The invention provides novel compounds of the formula I below: wherein the meaning of each substituent is defined in the application. The compounds are useful as inhibitors of the glycine transporter and useful in the treatment of diseases responsive to the inhibition of the glycine transporter. The invention provides a pharmaceutical composition comprising a compound of Formula I as defined above and the use of compounds as above for the manufacture of medicaments for treatment of diseases responsive to ligands of the glycine transporter.Type: GrantFiled: January 17, 2003Date of Patent: July 26, 2005Assignee: H. Lundbeck A/SInventors: Ejner Knud Moltzen, Paul Garrick Smith, Christian Krog-Jensen, Klaus Peter Bøgesø
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Patent number: 6900344Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide via a dicarboxylated salicylamide intermediate. The present invention also relates to dicarboxylic salicylamide delivery agent compounds for the delivery of active agents. Methods of administration are provided as well.Type: GrantFiled: March 21, 2001Date of Patent: May 31, 2005Assignee: Emisphere Technologies, Inc.Inventors: Joseph N. Bernadino, Doris C. O'Toole, William E. Bay
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Patent number: 6878723Abstract: The invention concerns compounds inhibiting LTA4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.Type: GrantFiled: April 6, 2000Date of Patent: April 12, 2005Assignees: Institut National de la Sante et de la rescherche Medicale (INSERM), BioprojetInventors: Denis Danvy, Thierry Monteil, Jean-Christophe Plaquevent, Pierre Duhamel, Lucette Duhamel, Nadine Noel, Claude Gros, Olivier Chamard, Jean-Charles Schwartz, Jeanne-Marie Lecomte, Serge Piettre
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Patent number: 6849649Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.Type: GrantFiled: October 28, 2003Date of Patent: February 1, 2005Assignee: Pfizer Inc.Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
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Patent number: 6846936Abstract: The invention relates to 2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl-5-nitrobenzofuran hydrochloride, to its preparation and to its use as synthetic intermediate, in particular in preparing 2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl)-5-nitrobenzofuran, itself an intermediate for dronedarone.Type: GrantFiled: December 10, 2001Date of Patent: January 25, 2005Assignee: Sanofi-SynthelaboInventor: Michel Biard
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Patent number: 6833471Abstract: A methods for producing a hydroxy-amino acid or derivative thereof, such as statine, phenylstatine or isostatine, is provided. A substituted &bgr;-ketodiester having a ketone group and two ester functional groups is contacted with a ketoreductase under conditions permitting the reduction of the ketone group to an alcohol. Only one of the ester functional groups is regioselectively hydrolyzed to the corresponding carboxylic acid, whereby a non-hydrolyzed ester functional group remains. Either the carboxylic acid or the non-hydrolyzed ester functional group is converted to an amine or a derivative thereof to produce a hydroxy-amino acid or derivative thereof.Type: GrantFiled: September 9, 2002Date of Patent: December 21, 2004Assignee: BioCatalytics, Inc.Inventors: J. David Rozzell, Jr., Spiros Kambourakis
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Publication number: 20040209957Abstract: The present invention relates to a tetrafluorobenzyl derivative and a pharmaceutical composition for prevention and treatment of acute and chronic neurodegenerative disease in central nervous system and ophthalmic diseases containing the same. The tetrafluorobenzyl derivative of the present invention can effectively be used to prevent and treat chronic neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease and Huntington's disease, degenerative brain disease such as epilepsy and ischemic brain disease such as stroke.Type: ApplicationFiled: December 22, 2003Publication date: October 21, 2004Inventors: Byoung-Joo Gwag, Sung-Hwa Yoon, Ho-Sang Moon, Eun-Chan Park, Seok-Joon Won, Young-Ae Lee, Hae-Un Lee
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Patent number: 6806384Abstract: The present invention provides a production method of an optically active &bgr;-amino-&agr;-hydroxycarboxylic acid, which includes the following steps (a)-(c): (a) treating an optically active N-carbamate protected &bgr;-amino epoxide with an acid to give an optically active 5-hydroxymethyl-2-oxazolidinone; (b) oxidizing the resulting compound in the presence of 2,2,6,6-tetramethyl-1-piperidinyloxy and hypochlorite to give an optically active 4-benzyl-2-oxo-5-oxazolidinecarboxylic acid; and (c) treating the 4-benzyl-2-oxo-5-oxazolidinecarboxylic acid with a base, and a production method of an optically active N-carbamate protected &bgr;-amino-&agr;-hydroxycarboxylic acid which includes protection of the amino group with a carbamate type protecting group. The industrial production method of the present invention can produce these compounds efficiently.Type: GrantFiled: April 10, 2002Date of Patent: October 19, 2004Assignee: Ajinomoto Co., Inc.Inventors: Yasuyuki Otake, Tomoyuki Onishi, Sachiko Oka, Daisuke Takahashi
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Patent number: 6797284Abstract: Phytopharmaceutical food products which contain plant extracts and aminoacids and which can be used in order to reduce tobacco smoke addiction.Type: GrantFiled: December 11, 2001Date of Patent: September 28, 2004Inventor: Ursula Mariah Rothlin
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Publication number: 20040180401Abstract: The present invention discloses methods of determining highly precise interactions between the HERG ion channel and various compounds. The methods of the present invention utilize the nonsense codon suppression methods combined with heterologous in vivo expression in Xenopus oocytes.Type: ApplicationFiled: May 23, 2003Publication date: September 16, 2004Applicant: Neurion Pharmaceuticals, Inc.Inventors: Dennis A. Dougherty, Henry A. Lester, Jonathan G. Lasch
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Patent number: 6790865Abstract: The present invention provides novel 2-methylpropionic acid derivatives represented by the general formula: (wherein R1 represents a hydrogen atom, a lower alkyl group or an aralkyl group; R2 represents a hydrogen atom, a lower alkyl group or a halogen atom; A represents an oxygen atom or an imino group; the carbon atom marked with (R) represents a carbon atom in R configuration; and the carbon atom marked with (S) represents a carbon atom in S configuration) and pharmaceutically acceptable salts thereof, which have excellent &bgr;3-adrenoceptor stimulating effects and are useful as agents for the prevention or treatment of obesity, hyperglycemia, the diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression, or the diseases caused by biliary calculi or hypermotility of the biliary tract.Type: GrantFiled: February 5, 2003Date of Patent: September 14, 2004Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Tetsuro Tamai, Nobuyuki Tanaka, Harunobu Mukaiyama, Akihito Hirabayashi, Hideyuki Muranaka, Masaaki Sato, Masuo Akahane
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Patent number: 6777391Abstract: A composition for an infant formula which comprises a low threonine content; a method of producing the composition; use of the composition in the manufacture of a medicament or nutritional product for addressing the nutritional needs and providing healthy growth of an infant; and a method of addressing the nutritional needs and providing healthy growth of an infant which comprises administering an effective amount of the composition. A preferred embodiment of the composition comprises all of: i) acid whey protein or sweet whey protein from which caseino-glyco-macropeptide has been removed; and ii) free arginine; and iii) free histidine; and iv) free tyrosine or free tryptophan or tryptophan rich milk protein or a mixture thereof.Type: GrantFiled: April 22, 2002Date of Patent: August 17, 2004Assignee: Nestec S.A.Inventors: Zdenek Kratky, Jean-Claude Maire, Olivier Ballevre, Ferdinand Haschke, Rolf Jost, Martinas Kuslys, Niklaus Meister, Marie-Christine Secretin
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Patent number: 6777440Abstract: The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the following formula, or a tautomer of said compound, or a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R1, R2 and B1 are as defined herein.Type: GrantFiled: December 6, 2002Date of Patent: August 17, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Walker, Jacques Banville, Roger Remillard, Serge Plamondon
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Publication number: 20040142983Abstract: Disclosed are nitrone compounds and pharmaceutical compositions containing such compounds. The nitrone compounds have one to six additional carbons bridging between the nitrone functionality and the nitrone aryl ring. The disclosed compositions are useful as therapeutics for inflammation-related conditions and analgesia in mammals, such as arthritis, and for neuropathic pain and traumatic injuries such as traumatic brain injury and acute spinal cord injury.Type: ApplicationFiled: October 14, 2003Publication date: July 22, 2004Inventors: M. Amin Khan, Ravindra B. Upasani, Paul L. Wood
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Patent number: RE39088Abstract: An amide compound of the formula (I): ? wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R1, R2, R3 and R4 are H, hydroxy and the like, R5 is H, alkyl and the like, m is an integer of 0-6, R6 is an optionally substituted aryl and the like, and R7 is H, an optionally substituted alkyl and the like, a pharmaceutically acceptable acid addition salt thereof and a pharmaceutical containing same as an active ingredient. The amide compounds exhibit superior suppressive effects on cytokines directly or indirectly involved in inflammations, such as IL-8, IL-1, IL-6, TNF-?, GM-CSF and the like, and are useful for the prophylaxis and treatment of rheumatic diseases, arthritis due to gout and the like.Type: GrantFiled: August 15, 1996Date of Patent: May 2, 2006Assignee: Japan Tobacco, Inc.Inventors: Junichi Haruta, Kazuhiko Sakuma, Yoshihiro Watanabe