Plural Chalcogens Bonded Directly To The Hetero Ring Patents (Class 549/476)
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Patent number: 10836776Abstract: The present application relate to process for preparation of tetrahydrofuran compound of formula II, 4-Methylene tetrahydrofuran compound of formula V and tetrahydropyran compound of formula IX which are useful as intermediates for the preparation of halichondrin B analogues such as Eribulin or its pharmaceutically acceptable salts.Type: GrantFiled: November 23, 2017Date of Patent: November 17, 2020Assignee: DR. REDDY'S LABORATORIES LIMITEDInventors: Kumar Sarvesh, Debjit Basu, Raja gopal Penumandla, Prapulla Kumar Palvai
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Patent number: 10533017Abstract: A method for producing 1,4:3,6-dianhydrohexitols, including the steps of: a) supplying at least one hexitol, b) dehydrating the hexitol, and c) distillating the dehydration product produced in step b), wherein: the hexitol is supplied in the form of an aqueous solution in step a); and the distillation is carried out by means of a thin-film evaporator in step c).Type: GrantFiled: March 16, 2017Date of Patent: January 14, 2020Assignee: ROQUETTE FRERESInventors: Hervé Wyart, Mathias Ibert
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Patent number: 10487066Abstract: In the present invention, a sugar alcohol can be efficiently produced from a cellulose-containing biomass by carrying out a step (1) of filtering an aqueous sugar solution, which is obtained by hydrolysis of a cellulose-containing biomass, by passing the solution through a separation membrane having a molecular cut-off of 300-800 so as to remove catalyst poisons to the non-permeate side and collecting a sugar solution from the permeate side, and a step (2) of subjecting the sugar solution obtained in step (1) to a hydrogenation reaction in the presence of a metal catalyst.Type: GrantFiled: February 16, 2017Date of Patent: November 26, 2019Assignee: Toray Industries, Inc.Inventors: Takahiro Arai, Masateru Ito, Hiroyuki Kurihara, Katsushige Yamada
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Patent number: 9499559Abstract: Long-chain alkyl cyclic acetals made from sugars are obtainable by a method that comprises the steps consisting of: dehydrating a hexitol in a monoanhydrohexitol substrate; reacting the monoanhydrohexitol substrate obtained with an alkyl aldehyde reagent containing 5 to 18 carbon atoms, by means of an acetalization reaction with a substrate/reagent ratio of between 5:1 and 1:1, or with a derivative of an alkyl aldehyde reagent containing 5 to 18 carbon atoms, by means of a transacetalization reaction with a substrate/reagent ratio of between 1:1 and 1:3, in the presence of acid catalyst and in an environment that is free of solvent or that consists of non-aqueous polar solvent; collecting the long-chain alkyl acetal of hexitan from the mixture obtained.Type: GrantFiled: June 13, 2014Date of Patent: November 22, 2016Assignees: SYRAL BELGIUM NV, UNIVERSITÉ CLAUDE BERNARD LYON 1, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (C.N.R.S.)Inventors: Charlotte Gozlan, Nicolas Duguet, Marc Lemaire, Yves Queneau, Andreas Redl
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Publication number: 20150133777Abstract: The invention disclosed herein discloses selected ribose isomers that are useful as PET probes (e.g. [18F]-2-fluoro-2-deoxy-arabinose). These PET probes are useful, for example, in methods designed to monitor physiological processes including ribose metabolism and/or to selectively observe certain tissue/organs in vivo. The invention disclosed herein further provides methods for making and using such probes.Type: ApplicationFiled: May 9, 2013Publication date: May 14, 2015Inventors: Owen Witte, Peter M. Clark, Blanca Graciela Flores Castillo, Michael E. Jung, Nikolai M. Evdokimov
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Patent number: 8933251Abstract: A fluorinated monomer of cyclic acetal structure has formula (1) wherein R is a C1-C20 alkyl group which may be substituted with halogen or separated by oxygen or carbonyl, and Z is a divalent organic group which forms a ring with alkylenoxy and contains a polymerizable unsaturated group. A polymer derived from the fluorinated monomer may be endowed with appropriate water repellency, water sliding property, lipophilicity, acid lability and hydrolyzability and is useful in formulating a protective coating composition and a resist composition.Type: GrantFiled: March 20, 2013Date of Patent: January 13, 2015Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Takeru Watanabe, Satoshi Shinachi, Takeshi Kinsho, Koji Hasegawa, Yuji Harada, Jun Hatakeyama, Kazunori Maeda, Tomohiro Kobayashi
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Publication number: 20140316148Abstract: Polyol ether compounds and processes for their preparation. A representative process comprises melting a polyol, and reacting the molten polyol, a carbonyl compound, and hydrogen in the presence of a hydrogenation catalyst to provide the poly of ether. The polyol ether has surfactant properties.Type: ApplicationFiled: February 22, 2012Publication date: October 23, 2014Applicant: DOW GLOBAL TECHNOLOGIES LLCInventors: Michael L. Tulchinsky, Sze-Sze Ng, Cynthia L. Rand
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Publication number: 20140314852Abstract: The invention relates to systems comprising homogenous nanoparticles having an average size of less than 1 micrometer and containing at least a sorbitan ester, a macrogol ester, a macrogol ether or a derivative of same and, optionally, at least one component derived from oxyethylene and/or at least one component having an electric charge (positive or negative). According to the invention, the components are incorporated in a single step consisting in mixing two solutions. The invention also relates to the use of said systems as medicines or medical devices, in tissue engineering or regenerative medicine, for cosmetic, hygienic or nutritional uses, and in surface coatings. The invention further relates to methods for preparing same.Type: ApplicationFiled: November 8, 2012Publication date: October 23, 2014Inventors: Alejandro Sanchez Barreiro, Begoña Seijo Rey, Giovanni Konat Zorzi, Edison Luis Santana Carvalho, Andrea Pensado Lopez
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Publication number: 20140275580Abstract: A method is disclosed for making an unsaturated glycitan ester by reacting intramolecular condensates of glycitols having four or more carbons with a metathesis-derived unsaturated fatty acid in the presence of an alkaline catalyst and under conditions sufficient to form the aforesaid unsaturated glycitan fatty ester. A composition is also disclosed comprising a compound of the following structure: wherein R1 is hydrogen, alkyl, aryl or (CH2)1-9—COOR5; wherein R5 is wherein R2, R3 and R4 are hydrogen, or —(O)C—(CH2)m—CH?CH—R1 or —(CH2CH2O)nH or mixtures thereof; wherein m is 1 to 9; and wherein n is 1 to 100.Type: ApplicationFiled: March 10, 2014Publication date: September 18, 2014Applicant: ELEVANCE RENEWABLE SCIENCES, INC.Inventors: Ryan A. Littich, Timothy Montavon
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Publication number: 20140200257Abstract: The invention provides poly(ethylene glycol)-lipid conjugates for use in drug delivery.Type: ApplicationFiled: January 11, 2012Publication date: July 17, 2014Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Kallanthottathil G Rajeev, Muthiah Manoharan, Muthusamy Jayaraman, Martin Maier, Jayaprakash K. Nair, David Butler
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Patent number: 8648113Abstract: The present invention relates to a compound derived from mycelium of Antrodia camphorata. The present invention also relates to the composition or mycelium comprising the compounds of the invention. The composition of the invention decreases systolic blood pressure and increases high density lipoprotein.Type: GrantFiled: October 12, 2012Date of Patent: February 11, 2014Assignee: Simpson Biotech Co., Ltd.Inventors: Masao Hattori, Chia-Chin Sheu
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Publication number: 20140039208Abstract: A process is disclosed for converting polysaccharides to platform chemicals. The process comprises dissolving the polysaccharides in a inorganic molten salt hydrate, converting the polysaccharides to monosaccharides, and converting the monosaccharides to platform chemicals that are easily separable from the inorganic molten salt hydrate. Preferably the polysaccharides are provided in the form of a biomass, more preferably a ligno-cellulosic biomass.Type: ApplicationFiled: April 22, 2013Publication date: February 6, 2014Applicant: BIOeCON International Holding N.V.Inventor: BIOeCON International Holding N.V.
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Publication number: 20130309324Abstract: The present invention provides O-nitro compounds, pharmaceutical compositions of O-nitro compounds and methods of using O-nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.Type: ApplicationFiled: July 26, 2013Publication date: November 21, 2013Applicants: RadioRx, Inc., c/o Interwest Venture Partners, Alliant Techsystems Inc.Inventors: Mark D. Bednarski, Susan Knox, Louis F. Cannizzo, Kristin F. Warner, Robert B. Wardle, Stephen P. Velarde, Shoucheng Ning
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Patent number: 8445704Abstract: A process is disclosed for converting polysaccharides to platform chemicals. The process comprises dissolving the polysaccharides in a inorganic molten salt hydrate, converting the polysaccharides to monosaccharides, and converting the monosaccharides to platform chemicals that are easily separable from the inorganic molten salt hydrate. Preferably the polysaccharides are provided in the form of a biomass, more preferably a ligno-cellulosic biomass.Type: GrantFiled: September 13, 2010Date of Patent: May 21, 2013Assignee: BIOeCON International Holding N.V.Inventors: Paul O'Connor, Rafael Menegassi De Almeida, Jacob A. Moulijn, Michiel Makkee, Sjoerd Daamen
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Patent number: 8440845Abstract: A process is disclosed for converting a polysaccharide-containing biomass material to platform chemicals. The process comprises dissolving the polysaccharides in an inorganic molten salt hydrate, converting the polysaccharides to monosaccharides, and converting the monosaccharides to derivatized (di)anhydro sugars that are easily separable from the inorganic molten salt hydrate. The derivatized (di)anhydro sugars are useful as fuel additives and fuel substitutes.Type: GrantFiled: September 19, 2011Date of Patent: May 14, 2013Assignee: BIOeCON International Holding N.V.Inventors: Michiel Makkee, Jacob Adriaan Moulijn, Rafael Menegassi De Almeida, Paul O'Connor
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Publication number: 20110178102Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: June 30, 2004Publication date: July 21, 2011Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Vern L Schramm, Anthony A. Suave
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Publication number: 20110172447Abstract: The present disclosure relates to p-toluene sulfonic acid salt of 5-amino-3-(2?-O-acetyl-3?-deoxy-beta-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and to its use in treating conditions such as viral infections, tumors, and cancer. Also disclosed is a method of preparing the p-toluene sulfonic acid salt of 5-amino-3-(2?-O-acetyl-3?-deoxy-?-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and methods for producing furanose compounds which are useful intermediates in the preparation of pharmaceutical compounds such as p-toluene sulfonic acid salt of 5-amino-3-(2?-O-acetyl-3?-deoxy-?-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and the like.Type: ApplicationFiled: March 23, 2011Publication date: July 14, 2011Applicant: Anadys Pharmaceuticals, Inc.Inventors: David Kucera, Gregory J. Haley, Erik J. Rueden, Tingmin Wang
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Publication number: 20110123468Abstract: Described is the use of benzotropolone and their derivatives, especially the compounds of formula (1); wherein R2, R3, R4, R5 and R6 independently of one another are hydrogen; OH; C1-C30alkyl, C2-C30al-kenyl, C1-C30alkoxy, C3-C12cycloalkyl or C1C30hydroxyalkyl, which may be substituted by one or more E and/or interrupted by one or more D; C6-C20aryl, which may be substituted by one or more G; C4-C20heteroaryl, which may be substituted by one or more G, C2-C18alkenyl, C2-C18alkynyl, C7-C25aralkyl, CN, or —CO—R17; C1-C30mono- or dialkylamino; COR9; COOR9; CONR9R10; CN; SO2R9; OCOOR9; OCOR9; NHCOOR9; NR9COR10; NH2; *—(CO)—NH—(CH2)n1—(PO)—(OR11)2; —(CO)—O—(CH2)n1—(PO)—(OR11)2; sulphate; sulphonate; phosphate; phosphonate; —(CH2)n2—[O—(SO2)]n3—OR11; —O—(CH2)n4(CO)n5—R11; —(O)n6—(CH2)n7—(PO)—(OR9)2; —(O)n6—(CH2)n7—SO2—OR9; halogen; organosilanyl; organo-siloxanyl; or a sugar residue linked directly in an ?- or ?-mode via the anomeric oxygen to the benzotropolone system or via a linear or branched alkylene, alkenyleType: ApplicationFiled: June 18, 2009Publication date: May 26, 2011Applicant: BASF SEInventors: Barbara Wagner, Reinhold Ohrlein, Bernd Herzog, Kai Eichin, Gabriele Baisch, Stephanie Portmann
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Publication number: 20110060148Abstract: A process is disclosed for converting polysaccharides to platform chemicals. The process comprises dissolving the polysaccharides in a inorganic molten salt hydrate, converting the polysaccharides to monosaccharides, and converting the monosaccharides to platform chemicals that are easily separable from the inorganic molten salt hydrate. Preferably the polysaccharides are provided in the form of a biomass, more preferably a ligno-cellulosic biomass.Type: ApplicationFiled: September 13, 2010Publication date: March 10, 2011Applicant: BIOeCON International Holding N.V.Inventors: Paul O'CONNOR, Rafael Menegassi De Almeida, Sjoerd Daamen, Jacob A. Moulijn, Michiel Makkee
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Publication number: 20100311582Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6, independently of each other, are for example, selected from the group consisting of H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C3-C8-cycloalkyl, R7C(?O), and a ring system; provided that at least one of R1 and R6 is a —C2-C6-alkenylthio-C1-C6-alkyl, —C1-C6-alkoxy-C(?O)NRx-C1-C6-alkyl, —partially or fully unsaturated ring system containing in at least one ring in the ring system at least one hetero atom selected from N, O and S, which ring system is bound (i.e. through the N bonded to R1 and R6 in formula I) either directly or via a a C1-C6-alkylene group to the remainder of the compound, —partially or fully unsaturated ring system containing a ring that is bound to the remainder of the compound (i.e.Type: ApplicationFiled: January 23, 2009Publication date: December 9, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Thomas Pitterna, Peter Renold, Ottmar Franz Hueter, Peter Maienfisch, Werner Zambach
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Patent number: 7652172Abstract: This invention provides a practical synthesis route for 4,5-dihydroxypentane-2,3-dione (DPD), an unstable small molecule which is proposed to be the source of universal signaling agents for quorum sensing in bacteria. The synthesis route includes new intermediates and allows preparation of isotopically-labeled DPD and ent-DPD. The method provides sufficient quantities of DPD for study of spontaneous binding of borate to DPD, the signal for the marine bacteria V. harveyi.Type: GrantFiled: September 20, 2005Date of Patent: January 26, 2010Assignee: The Trustees of Princeton UniversityInventors: Martin F. Semmelhack, Shawn R. Campagna, Bonnie L. Bassler, Michael J. Federle
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Patent number: 7638256Abstract: Silicon compounds having fluorinated hemiacetal structure are provided. Silicone resins having the same structure have an appropriate acidity to enable formation of a finer pattern by minimizing the pattern collapse by swelling, exhibit improved resistance to the etching used in the pattern transfer to an organic film, and are thus suited for use in resist compositions for the bilayer process.Type: GrantFiled: July 6, 2006Date of Patent: December 29, 2009Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Takeshi Kinsho, Takeru Watanabe, Mutsuo Nakashima, Yoshitaka Hamada
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Patent number: 7622598Abstract: A compound represented by formula (I): [wherein, for example, X is a hydrogen atom or a halogen atom; R1 is a hydrogen atom; R2 is a hydrogen atom or a C1-4 alkyl group; R3 is —CHO or —COOH; and R4 is —CH?CH—(CH2)p—CH3 (wherein p is an integer of 1 to 12), —CH(OH)—(CH2)q—CH3 (wherein q is an integer of 1 to 13), —CH(OH)—CH2—CH(CH3)—(CH2)2—CH?C(CH3)2, —CH?CH—CH(CH3)—(CH2)3—CH(CH3)2, —(CH2)2—CH(CH3)—(CH2)3—CH(CH3)2 or —(CH2)8—CH3], an optical isomer thereof and a pharmaceutically acceptable salt thereof. These compounds have antitrypanosoma activity, and accordingly are useful as drugs for preventing or treating the diseases caused by trypanosoma.Type: GrantFiled: October 18, 2004Date of Patent: November 24, 2009Assignee: aRigen Pharmaceuticals, Inc.Inventors: Hiroyuki Saimoto, Yoshihiro Shigemasa, Kiyoshi Kita, Yoshisada Yabu, Tomoyoshi Hosokawa, Masaichi Yamamoto
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Publication number: 20090286873Abstract: This invention relates to crystals comprising apo-LsrB and holo-LsrB. The structure of holo-LsrB identifies a tetrahydroxytetrahydrofuran derived from 4,5-dihydroxy-2,3-pentanedione (DPD) as the active autoinducer-2 (AI-2) molecule in Salmonella typhimurium. The X-ray crystallographic data can be used in a drug discovery method. Additionally the invention provides AI-2 analogs based on this discovery as well as pharmaceutical compositions containing those analogs.Type: ApplicationFiled: March 13, 2009Publication date: November 19, 2009Inventors: Stephen T. Miller, Karina B. Xavier, Michiko E. Taga, Shawn R. Campagna, Martin F. Semmelhack, Bonnie L. Bassler, Frederick M. Hughson
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Publication number: 20090069557Abstract: A process for preparation of gemcitabine hydrochloride and purification thereof.Type: ApplicationFiled: February 6, 2007Publication date: March 12, 2009Applicants: Dr. Reddy's Laboratories Ltd., Dr. Reddy's Laboratories, Inc.Inventors: Venkata Raghavendra Acharyulu Palle, Sekhar Munaswamy Nariyam, Veerender Murki, Anirudha Arvind Waghmare, Vishnu Nandkishore Mundhada
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Patent number: 7435838Abstract: The present invention relates to the diol intermediate of citalopram useful for treatment of depression, which is the crystal of free base of 3-hydroxylmethyl-4-[1-(4-fluorophenyl)-1-hydroxyl-4-(dimethylamino)]butylbenzonitrile and the method of crystallization thereof. The present invention has disclosed the method to prepare pure citalopram and its purified salts through crystallization of the described base; the optical resolution method of citalopram diol intermediate, the method to prepare S-citalopram and its purified salts by crystals mentioned above. The present invention has also disclosed the method to prepare citalopram and its purified salts, S-citalopram and its purified salts, as well as pharmaceutical formulation thereof obtained. Using methods of the present invention, the quality and yield of the product can be significantly improved, and the production cost of the medicinal material can be reduced.Type: GrantFiled: December 6, 2004Date of Patent: October 14, 2008Assignee: Hangzhou Minsheng Pharmaceutical Co. Ltd.Inventors: Runan Mei, Dianwu Guo, Shulong Wang
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Patent number: 7423057Abstract: The present invention relates to a novel compounds that can be used as anti-inflammatory, immunomodulatory and antiproliferatory agents. In particular, the invention refers to new compounds which inhibit dihydroorotate dehydrogenase (DHODH), a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of diseases, in particular their use in diseases where there is an advantage in inhibiting dihydroorotate dehyrogenase (DHODH).Type: GrantFiled: February 17, 2006Date of Patent: September 9, 2008Assignee: 4SC AGInventors: Johan Leban, Bernd Kramer, Wael Saeb, Gabriel Garcia
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Patent number: 7390913Abstract: In the following, citalopram diol means 4-(4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl)-3-(hydroxymethyl)-benzonitrile, as free base and/or acid addition salt. The invention relates to a process for the preparation of racemic citalopram diol and/or R- or S-citalopram diol, comprising the separation of a non-racemic mixture of R- and S-citalopram diol with more than 50% of one of the enantiomers into a fraction being enriched with S- or R-citalopram diol and a fraction comprising RS-citalopram diol wherein the ratio of R-citalopram diol:S-citalopram diol is equal to 1:1 or closer to 1:1 than in the initial mixture.Type: GrantFiled: December 18, 2003Date of Patent: June 24, 2008Assignee: H. Lundbeck A/SInventors: Hans Petersen, Brian Christiansen, Robert Dancer, Rikke E. Humble
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Publication number: 20080146579Abstract: The invention pertains to a method and compositions for treatment or prevention of chronic pulmonary dysfunction in a patient.Type: ApplicationFiled: December 15, 2006Publication date: June 19, 2008Inventors: Erwin Peke MEIJER, George Verlaan, Maarteen Anne Hoijer
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Publication number: 20080110763Abstract: A process for the preparation of 2,5-dihydrofuran derivatives substituted in the 3- or 4-position, which in the 2- or in the 5-position or at both positions each carry a C1- to C6-alkoxy radical (DHF-alkoxy derivatives 1), or 1,1,4,4-tetraalkoxy-but-2-ene derivatives substituted in the 3- or 4-position, from 2-butene-1 ,4-diol derivatives of the general formula (I) in which the radicals R1 and R2 independently of one another are hydrogen, C1- to C6-alkyl, C6- to C12-aryl or C5- to C12-cycloalkylene or R1 and R2, together with the double bond to which they are bonded, form a C6- to C12-aryl radical or a mono- or polyunsaturated C5- to C12-cycloalkyl radical, or from their mixture with 2,5-dihydrofuran derivatives substituted in the 3- position or 4-position, which in the 2- or in the 5-position carry a C1- to C6-alkoxy radical, by electro-chemical oxidation in the presence of a C1- to C6-monoalkyl alcohol.Type: ApplicationFiled: March 23, 2006Publication date: May 15, 2008Applicant: BASF AktiengesellschaftInventors: Ingo Richter, Hermann Putter, Ulrich Griesbach, Nils Bottke
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Publication number: 20070213544Abstract: A process is provided for the preparation of anhydrosugar alcohols. The process involves heating a sugar alcohol or a monoanhydrosugar alcohol starting material in the presence of an acid catalyst and under pressure. Optionally the resulting product is purified. Very high purities are achieved, without necessitating the use of organic solvents in the process.Type: ApplicationFiled: March 9, 2007Publication date: September 13, 2007Inventor: Alexandra J. Sanborn
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Patent number: 7132001Abstract: The object of the present patent application are 3-aminophenol derivatives of formula (I) or the physiologically compatible, water-soluble salts thereof and colorants based on a developer-coupler combination containing these compounds.Type: GrantFiled: January 8, 2003Date of Patent: November 7, 2006Assignee: Wella AGInventors: Gisela Umbricht, Franco Jose Rosato, Hans-Juergen Braun
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Patent number: 7128764Abstract: The object of the present patent application are 3-aminophenol derivatives of formula (I) or the physiologically tolerated, water-soluble salts thereof wherein R denotes a heterocyclic aromatic 5-membered ring of formula (Ia) and colorants based on a developer-coupler combination and containing these compounds.Type: GrantFiled: April 24, 2002Date of Patent: October 31, 2006Assignee: Wella AGInventors: Cècile Pasquier, Patrick Wyss, Hans-Juergen Braun
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Patent number: 7122061Abstract: The present invention has for an object compounds of formula (I) and colorants containing these 4-aminobiphenyl-3-ol derivatives of general formula (I) for dyeing keratin fibers, particularly hair, wherein R1 and R2 independently of each other denote hydrogen, a halogen atom, a cyano group, a hydroxyl group, a C1–C4-alkoxy group, a C2–C4-hydroxyalkoxy group, a C1–C6-alkyl group, a nitro group, a trifluoromethyl group, a —C(O)H group, a —C(O)CH3 group, a —C(O)CF3 group, an —Si(CH3)3 group or a C1–6-hydroxyalkyl group or R1 and R2 together form an —O—CH2—O— bridge.Type: GrantFiled: May 13, 2003Date of Patent: October 17, 2006Assignee: Wella AGInventors: Laurent Chassot, Hans-Juergen Braun
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Patent number: 7112686Abstract: The invention relates to a process for the preparation of racemic citalopram free base or an acid addition salt thereof and/or R- or S-citalopram as the free base or an acid addition salt thereof by separation of a mixture of R- and S-citalopram with more than 50% of one of the enantiomers into a fraction consisting of racemic citalopram and/or a fraction of S-citalopram or R-citalopram characterized in that i) citalopram is precipitated from a solvent as the free base or as an acid addition salt thereof; ii) the precipitate formed is separated from the mother liquor; iia) if the precipitate is crystalline it is optionally recrystallised one or more times to form racemic citalopram, and then optionally converted into an acid addition salt thereof; iib) if the precipitate is not crystalline, steps i) and ii) are optionally repeated until a crystalline precipitate is obtained and the crystalline precipitate is recrystallised one or more times to form racemic citalopram, and then optionally converted into an aciType: GrantFiled: June 25, 2002Date of Patent: September 26, 2006Assignee: H. Lundbeck A/SInventors: Rikke E. Humble, Troels V. Christensen, Michael H. Rock, Ole Nielsen, Hans Petersen, Robert Dancer
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 7029606Abstract: A dihydrofuran-containing nonlinear optical chromophore having a ?-electron donor group conjugated to the dihydrofuran group through a ?-electron conjugated bridge group. The nonlinear optical chromophore is a hyperpolarizable chromophore that can be used as an electro-optic modulator in electro-optic devices.Type: GrantFiled: July 24, 2001Date of Patent: April 18, 2006Assignee: University of WashingtonInventors: Larry R. Dalton, Kwan-Yue Jen, Timothy Londergan, William Brenden Carlson, Gregory Phelan, Diyun Huang, Daniel Casmier, Todd Ewy, Nicholas Buker
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Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 6916948Abstract: Derivatives of bis-(1,3-dihydroxy-prop-2-yl)amine are disclosed, together with the use of such derivatives and of bis(1,3-dihydroxy-prop-2-yl)amine itself in the preparation of polymers, in particular dendrimers. Some of the derivatives may be useful as non-ionic surfactants.Type: GrantFiled: September 12, 2001Date of Patent: July 12, 2005Assignee: Isis Innovation LimitedInventors: George W. J. Fleet, David Scott, Malcolm Finn, Thomas Krūlle
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Patent number: 6897302Abstract: The invention provides a method of synthesizing ?-L-5-fluoro-2?,3?-dideoxy-2?,3?-didehydrocytidine (?-L-FD4C). The method allows for large-scale production of ?-L-FD4C in an efficient, cost-effective, and environmentally sound manner.Type: GrantFiled: April 11, 2003Date of Patent: May 24, 2005Assignee: Achillion Pharmaceuticals, Inc.Inventors: Bo Kowalczyk, Zhao Lei, Ralph M. Schure, Lisa Dunkle
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Patent number: 6864283Abstract: Compounds of formula (I) wherein R1is selected from H, C(?O)R?, P(?O)R?R?, S(?O)R?R?, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, or substituted or unsubstituted aryl; or R1 together with R2 forms a saturated or unsaturated heterocyclic ring; R2 and R3 are each, independently, selected from H, C(?O)R?, P(?O)R?R?, S(?O)R?R?, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, or substituted or unsubstituted aryl; or one of R2 or R3 together with R1 forms a saturated or unsaturated heterocyclic ring; or R2 and R3 together form a saturated or unsaturated heterocyclic ring; R4 is selected from H, C(?O)R?, P(?O)R?R?, S(?O)R?R?, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18, alkynyl, or substituted or unsubstituted aryl, wherein R? is selected from the group consisting ofType: GrantFiled: February 16, 2001Date of Patent: March 8, 2005Assignee: Pharma Mar, S.A.Inventors: Tatsuo Higa, Junichi Tanaka, Dolores Garcia Gravalos
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Patent number: 6849733Abstract: There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of formula I are agonists and antagonists of neuropeptide Y, and are therefore useful as regulators.Type: GrantFiled: August 22, 1997Date of Patent: February 1, 2005Assignee: Agouron Pharmaceuticals, Inc.Inventors: Yufeng Hong, Vlad Edward Gregor, Anthony Lai Ling, Eileen Valenzuela Tompkins
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Patent number: 6840965Abstract: The object of the invention are p-aminophenol derivatives of general formula (I) or physiologically tolerated, water-soluble salts thereof and oxidative coloring preparations based on a developer-coupler combination containing at least one p-aminophenol derivative of formula (I).Type: GrantFiled: March 9, 2001Date of Patent: January 11, 2005Assignee: Wella AktiengesellschaftInventors: Laurent Chassot, Hans-Juergen Braun
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Patent number: 6831181Abstract: A process for recycling reaction byproducts in the manufacture of dianhydro sugar alcohols, such as isosorbide, from corresponding sugar alcohols.Type: GrantFiled: April 16, 2003Date of Patent: December 14, 2004Assignee: E. I. Dupont de Nemours and Co.Inventor: Kamlesh Kumar Bhatia
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Patent number: 6824805Abstract: This invention pertains to a method for flavoring an ingestible composition with a flavoring agent, furfuryl propyl disulfide, in organoleptically purified form, unaccompanied by substances of natural origin present in cooked beef and onions. The flavoring agent may be used in a wide variety of ingestible vehicles to augment or enhance the aroma or taste of foodstuffs, particularly roasted nut, roasted meat, beef broth, black pepper, onion, fine herbs, omelet, and cooked onion omelet flavored foodstuffs. The present invention also pertains to an ingestible composition comprising an ingestible vehicle and an organoleptically effective amount of the purified flavoring agent. The present invention also pertains to furfuryl propyl disulfide represented by the formula, (2-Furan-CH2SSCH2CH2CH3), in purified form, unaccompanied by substances of natural origin present in cooked beef and onions, and to methods for preparing furfuryl propyl disulfide.Type: GrantFiled: January 4, 2002Date of Patent: November 30, 2004Assignee: Bush Boake Allen Ltd.Inventors: Ronald Louis Belanger, Benjamin Owen Isaac, Anne-Dominique Fortineau
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Publication number: 20040152907Abstract: A process is provided for the preparation of anhydrosugar alcohols. The process involves heating a sugar alcohol or a monoanhydrosugar alcohol starting material in the presence of an acid catalyst, and subsequent purification of the anhydrosugar alcohol. In some embodiments of the present invention, film evaporators are used in distillation and purification of the anhydrosugar alcohols. Anhydrosugar alcohols of very high purity are achieved in the practice of the present invention. In some embodiments of the present invention, very high purities of the anhydrosugar alcohols are achieved without the use of organic solvents.Type: ApplicationFiled: November 14, 2003Publication date: August 5, 2004Applicant: Archer-Daniels-Midland CompanyInventors: Kevin M. Moore, Alexandra J. Sanborn
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Publication number: 20030229235Abstract: A process for recycling reaction byproducts in the manufacture of dianhydro sugar alcohols, such as isosorbide, from corresponding sugar alcohols.Type: ApplicationFiled: April 16, 2003Publication date: December 11, 2003Inventor: Kamlesh Kumar Bhatia
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Publication number: 20030092738Abstract: Compounds of formula (I) wherein the substituent groups defined by R1, R2, R3 and R4 are each independently selected of H, C(═O)R, P(═O)R′R″, S(═O)R′R″, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl; wherein each of the R′, R″ groups is independently selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstitued aryl; wherein R1, R2, R3 could form part of a heterocyclic ring; R2 can be independently an internal salt; wherein X1, X2 and X3 on formula (I) are independently placed in any particular position of the chain and independently selected of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′Type: ApplicationFiled: October 10, 2002Publication date: May 15, 2003Inventors: Tatsuo Higa, Junichi Tanaka, Dolores Garcia Gravalos
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Publication number: 20030032818Abstract: 1 A new, more efficient and highly stereospecific process is described for the preparation of compounds with general formula (R)-(I) and of absolute configuration (R), where the groups M, W, Q and Q1 are as defined in the description, starting from compounds of absolute configuration (S) by hydrolysis, in the presence of acids, of the corresponding esterified derivatives. The (R)-(I) products obtained with the process described herein are chiral synthons useful for the production of enanthiomerically pure drugs. The preparation of (R)-carnitine is also provided.Type: ApplicationFiled: June 24, 2002Publication date: February 13, 2003Inventors: Oreste Piccolo, Roberto Castagnani, Paolo De Witt
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Patent number: 6426421Abstract: One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.Type: GrantFiled: November 21, 2000Date of Patent: July 30, 2002Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Obadiah J. Plante, Peter H. Seeberger