Oxy, Aldehyde Or Ketone Group In Acid Moiety Patents (Class 560/170)
  • Publication number: 20120201962
    Abstract: A composition comprising at least one compound represented by the following formula (Z) is disclose. A-L-{D1-(E)q-D2-(B)m—Z1—R}p??(Z) In the formula, A represents a p-valent, linear or cyclic residue; L represents a single bond or a divalent linking group; p indicates an integer of at least 2; D1 represents a carbonyl group (—C(?O)—) or a sulfonyl group (—S(?O)2—); D2 represents a carbonyl group (—C(?O)—), a sulfonyl group (—S(?O)2—), a carboxyl group (—C(?O)O—), a sulfoxyl group (—S(?O)2O—), a carbamoyl group (—C(?O)N(Alk)-), or a sulfamoyl group (—S(?O)2N(Alk)-); E represents a divalent group; R represents a hydrogen atom, or a substituted or unsubstituted alkyl group having at most 7 carbon atoms; B represents oxyethylene group or the like; Z1 represents a single bond, or a divalent group.
    Type: Application
    Filed: June 23, 2010
    Publication date: August 9, 2012
    Applicant: FUJIFILM Corporation
    Inventors: Ken Kawata, Saisuke Watanabe, Hiroshi Kawamoto
  • Publication number: 20120165385
    Abstract: The invention relates to novel compounds containing a carboxylic acid head group. The invention further provides compositions containing the novel compounds, a particulate solid and an organic medium or water.
    Type: Application
    Filed: March 5, 2012
    Publication date: June 28, 2012
    Applicant: LUBRIZOL LIMITED
    Inventor: Dean Thetford
  • Patent number: 8207370
    Abstract: It is an objective of the present invention to produce an anti-form of an optically active ?-hydroxy-?-aminocarboxylic acid ester efficiently, simply and industrially advantageously. The objective can be accomplished by directly and selectively producing the anti-form of the optically active ?-hydroxy-?-aminocarboxylic acid ester by asymmetric reduction of a ?-keto-?-aminocarboxylic acid ester using an optically active amine complex as a catalyst. Further, the ?-keto-?-aminocarboxylic acid ester as a raw material can be produced at a high yield by reacting a glycine derivative with a carboxylic acid derivative.
    Type: Grant
    Filed: September 26, 2007
    Date of Patent: June 26, 2012
    Assignee: Kaneka Corporation
    Inventors: Tatsuya Honda, Tatsuyoshi Tanaka, Masaru Mitsuda
  • Patent number: 8198325
    Abstract: Disclosed are unsaturated alkyl esters of 5-aminovulinic acid of the following chemical formula 1, or pharmaceutically acceptable salts thereof, a method for preparing the same, and uses thereof. [Chemical Formula I] NH2—CH2—CO—CH2—CH2—CO—O—R wherein, R is a group selected from a group consisting of 2-propenyl, 3-butenyl, 4-pentenyl, 5-hexenyl, cis-2-pentenyl, cis-3-hexenyl, cis-4-hexenyl, and trans-2-hexenyl. Also, a pharmaceutical composition comprising the unsaturated alkyl ester of 5-aminovulinic acid or a salt thereof as an active ingredient is provided. This pharmaceutical composition is easily absorbed transdermally and is of low cytotoxicity. Featuring no amino-protecting processes, the method guarantees high production yields.
    Type: Grant
    Filed: June 28, 2007
    Date of Patent: June 12, 2012
    Assignee: Industry Foundation of Chonnam National University
    Inventors: Jonghoon Oh, Jee-Bum Lee, Hyoung-Ryun Park
  • Patent number: 8188295
    Abstract: The present invention relates to a process for preparing 3-difluoromethyl-Substituted pyrazole compounds of the formula (I) in which R1 is H, halogen, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C3-C8-cycloalkyl, phenyl, naphthyl, hetaryl, cyano, —C(?O)—OR1a, —C(?O)—NR1bR1c, —C(?O)—SR1d or —C(?S)—SR1e; R2 is H, C1-C4-alkyl, benzyl or phenyl; R3 is H, halogen, C1-C8-alkoxy, C1-C8-haloalkoxy, C3-C8-cycloalkoxy, C2-C8-alkenyloxy, C1-C8-alkylthio, C1-C8-haloalkylthio, C3-C8-cyclo-alkylthio or C2-C8-alkenylthio; compounds of the formula (II.a) or (II.b), in which R1 and R3 each have one of the definitions given above; R4 is halogen, —OR4a, —SR4a, —O—SO2—R4a or an —NR4bR4c group; R5 and R6 are each C1-C8-alkyl, C1-C8-haloalkyl, C3-C8-cycloalkyl, benzyl or phenyl, or, together with the nitrogen atom to which they are bonded, are a 3- to 8-membered heterocycle; Lewis acid adducts of compounds of the formula (II.b); the use of compounds of the formula (II.a) or (II.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: May 29, 2012
    Assignee: BASF SE
    Inventors: Markus Nett, Thomas Grote, Jan Klaas Lohmann, Jochen Dietz, Sebastian Peer Smidt, Michael Rack, Thomas Zierke
  • Publication number: 20120108680
    Abstract: A gelator made of an aliphatic oxyglycyl polyol that is capable of forming a gel by a small amount of addition in a pH range from acidic to alkaline regions, and a gel having high environmental compatibility, biocompatibility and biodegradability. A gelator including an aliphatic oxyglycyl polyol of Formula (1) wherein R is a C18-20 saturated aliphatic group or a C18-20 unsaturated aliphatic group having one double bond) or a pharmaceutically usable salt thereof; a self-assembly formed by self-assembling of the gelator; and a gel comprising the gelator or the self-assembly, and water, an alcohol, an aqueous solution, an alcohol solution, a hydrophilic organic solution, or a hydrophobic organic solution.
    Type: Application
    Filed: May 14, 2010
    Publication date: May 3, 2012
    Applicants: KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION, NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Masahiro Goto, Tatsuo Maruyama, Nobuhide Miyachi
  • Publication number: 20120095096
    Abstract: The disclosure provides a series of 2-oxoamides based on dipeptides and pseudodipeptides, which were synthesized and their activities toward two human intracellular phospholipases A2 (GIVA CPLA2 and GVIA 1PLA2) and one human secretory phospholipase A2 (GVsPLA2) were evaluated. Derivatives containing a free carboxyl group are selective GIVA cPLA2 inhibitors. A derivative based on the ethyl ester of an ether pseudodipeptide is the first 2-oxoamide, which preferentially inhibits GVIA iPLA2. The effect of 2-oxoamides on the generation of arachidonic acid from RAW 264.7 macrophages was also studied. It was found that selective GIVA cPLA2 inhibitors preferentially inhibited cellular arachidonic acid release; in which one pseudodipeptide gave an IC50 value of 2 ?M.
    Type: Application
    Filed: April 19, 2010
    Publication date: April 19, 2012
    Applicant: The Regents of the University of California
    Inventors: Edward A. Dennis, George Kokotos, Violetta Constantinou-Kokotou
  • Publication number: 20120029198
    Abstract: Esters of O-substituted hydroxy carboxylic acids are provided having Formula 1, or 2, or both Formulas 1 and 2: wherein R and R1 are independently selected from the group consisting of substituted and unsubstituted, branched- and straight-chain, saturated, unsaturated, and polyunsaturated C1-C22 alkyl, substituted and unsubstituted C3-C8 cycloalkyl, substituted and unsubstituted C6-C20 carbocyclic aryl, and substituted and unsubstituted C4-C20 heterocyclic; wherein the heteroatoms are selected from sulfur, nitrogen, and oxygen; and wherein n is 1-6. Process of producing esters of O-substituted hydroxy carboxylic acids are also provided.
    Type: Application
    Filed: December 22, 2010
    Publication date: February 2, 2012
    Applicant: EASTMAN CHEMICAL COMPANY
    Inventors: Liu Deng, Neil Warren Boaz
  • Publication number: 20110306600
    Abstract: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.
    Type: Application
    Filed: June 10, 2011
    Publication date: December 15, 2011
    Applicant: Grunenthal GmbH
    Inventor: Ramesh SESHA
  • Patent number: 8034748
    Abstract: The present invention relates to an additive, and its use for inhibiting nucleation, growth and agglomeration of gas hydrates by adding an effective amount of an inhibitor to a multiphasic mixture which tends to hydrate formation and consists of water, gas and optionally condensate, or to a drilling fluid which tends to form gas hydrates. Said inhibitor comprising dialkoxylated quaternary ammonium compounds of the formula 1 where R1, R2 are each independently radicals of the formulae -(A-O)n—(C)—CO—O—R5, R3 is C1- to C30-alkyl or C2- to C30-alkenyl, R4 is an organic radical which optionally contains heteroatoms and has from 1 to 100 carbon atoms, R5 is an alkyl or an alkenyl, n is a number from 1 to 20, A is an alkylene group, B is an alkylene group, C is a C1- to C6-alkylene group and X is an anion, are used as gas hydrate inhibitors.
    Type: Grant
    Filed: January 26, 2007
    Date of Patent: October 11, 2011
    Assignee: Clariant Produkte (Deutschland) GmbH
    Inventors: Uwe Dahlmann, Michael Feustel
  • Patent number: 8013104
    Abstract: Hyperbranched polymers and methods for preparing the same are disclosed. The polymers are obtained based on monomers synthesized via reacting a substituted or unsubstituted cyclic anhydride with a bifunctional amine.
    Type: Grant
    Filed: August 13, 2009
    Date of Patent: September 6, 2011
    Assignee: Designer Molecules, Inc.
    Inventor: Stephen M. Dershem
  • Publication number: 20110166025
    Abstract: Esteramide compounds are useful solvents/coalescing agents for a variety of phytosanitary, cleaning, degreasing, stripping, lubricating, coating and pigment/ink compositions.
    Type: Application
    Filed: January 23, 2009
    Publication date: July 7, 2011
    Applicant: RHODIA OPERATIONS
    Inventors: Olivier Jentzer, Massimo Guglieri
  • Publication number: 20110105610
    Abstract: Phospholipase A2 (PLA2) forms are expressed in spinal cord whose inhibition induces a potent antihyperalgesia. PLA2 inhibitor compounds are provided that include a common motif consisting of a 2-oxoamide with a hydrocarbon tail and a four carbon tether. The compounds block Group IVA calcium dependent PLA2 (cPLA2) and/or Group VIA calcium independent PLA2 (iPLA2) and/or Group V secreted PLA2 (sPLA2). Pharmaceutical compositions of compounds having cPLA2 inhibitory activity (but not iPLA2 or sPLA2 inhibitory activity) are useful in treating multiple sclerosis, while compositions of compounds having sPLA2 inhibitory activity (as well as iPLA2 and CPLA2 activity) are useful in treating spinal cord injuries (with related functional recovery).
    Type: Application
    Filed: July 3, 2008
    Publication date: May 5, 2011
    Inventors: Edward A. Dennis, Daren Stephen, Samuel David, Ruben Lopez-Vales, Athena Kalyvas, George Kokotos, Violetta Constantinou-Kokoton, Efrosini Barbayianni, Victoria Magrioti
  • Patent number: 7932326
    Abstract: Novel di- and tripodal compounds useful as chelators, intermediates for their production and a method for treating an aqueous solution to remove trivalent metal ions are presented.
    Type: Grant
    Filed: April 16, 2008
    Date of Patent: April 26, 2011
    Assignee: The University of Kentucky Research Foundation
    Inventors: Robert A. Yokel, Wesley R. Harris, Christopher D. Spilling, Chang-Guo Zhan
  • Publication number: 20110086915
    Abstract: The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N—CH2COCH2—CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.
    Type: Application
    Filed: December 6, 2010
    Publication date: April 14, 2011
    Inventors: Karl E. GIERSKCKY, Johan Moan, Qian Peng, Harald Steen, Trond Warloe, Alf Bjørseth
  • Publication number: 20110065920
    Abstract: The present invention relates to a process for preparing pentanoic diacid derivatives useful for preparing pyrimidine derivatives, in particular as intermediates useful for preparing pyrimidine derivatives of a class that is effective at inhibiting the biosynthesis of cholesterol in humans, such as HMG-CoA reductase inhibitors, e.g. rosuvastatin.
    Type: Application
    Filed: August 27, 2008
    Publication date: March 17, 2011
    Applicant: ratiopharm GmbH
    Inventors: Armin Boerner, Gerd Koenig, Natalia Andrushko, Vasyl Andrushko
  • Patent number: 7906676
    Abstract: The present invention relates to a novel process for the production of 3-amino-5-fluoro-4-dialkoxypentanoic acid ester used in the precursor of 3-amino-5-fluoro-4-oxopentanoic acid, represented by the following formula (I): wherein R1 and R2 are as defined in the Description.
    Type: Grant
    Filed: August 9, 2007
    Date of Patent: March 15, 2011
    Assignee: LG Life Sciences Ltd.
    Inventors: Hyun Ik Shin, Hyeong Wook Choi, Jae Hoon Lee, Kyu Woong Lee
  • Patent number: 7888526
    Abstract: The present invention provides an acid addition salt of 5-aminolevulinic acid (5-ALA) or of a 5-ALA derivative (e.g. a 5-ALA ester) with an acid which has a pKa of about 5 or less, preferably about 3 or less, with the proviso that the acid is other than hydrochloric acid. Particularly preferred salts are those derived from acids selected from the group comprising sulphonic acid and its derivatives, hydrobromic acid, sulfuric acid, nitric acid and phosphoric acid. The salts in accordance with the invention are particularly suitable for use as photosensitizing agents in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body.
    Type: Grant
    Filed: March 29, 2005
    Date of Patent: February 15, 2011
    Assignee: Photocure ASA
    Inventors: Jon Erik Braenden, Aslak Godal, Nils Olav Nilsen, Jo Klaveness
  • Publication number: 20110021482
    Abstract: A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula I or Ia: or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.
    Type: Application
    Filed: September 17, 2010
    Publication date: January 27, 2011
    Inventors: Harold L. Kohn, Christophe Salomé, Elise Salomé-Grosjean
  • Publication number: 20110021761
    Abstract: Segmented water soluble polymers, containing a higher molecular weight segment linked to a lower molecular weight segment, are described. In one embodiment, the polymer segments are poly(ethylene glycol) segments. The segmented polymers are functionalized and are useful for conjugation to various moieties such as pharmacologically active substances. Also described are conjugates of such polymers and methods of their preparation.
    Type: Application
    Filed: October 5, 2010
    Publication date: January 27, 2011
    Applicant: Nektar Therapeutics
    Inventors: Antoni Kozlowski, Xiaoming Shen, Michael D. Bentley, Zhihao Fang, Tony L. Sander
  • Publication number: 20110015406
    Abstract: A halogenating agent is added to a mixture including a base, a fluoroalkylcarboxylic acid derivative and an acrylate derivative to produce a fluoroaclyacetic acid derivative represented by the following Formula (3): wherein Rf represents a fluorine containing alkyl group, R1 and R2 represent a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, an arylalkyl group or an acyl group, or together represent an atomic group that forms a 5- or 6-membered ring containing a nitrogen atom to which R1 and R2 are bonded; R3 represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, or an arylalkyl group; and R4 represents an alkyl group, a cycloalkyl group, an aryl group, or an aryl alkyl group.
    Type: Application
    Filed: March 11, 2009
    Publication date: January 20, 2011
    Applicant: Mitsui Chemicals Agro, Inc.
    Inventors: Hideki Umetani, Takeshi Kakimoto, Yoji Aoki
  • Publication number: 20100273725
    Abstract: The present invention relates to photosensitizer compounds for use in cosmetic and therapeutic applications of photodynamic therapy. The compounds of the present invention are designed for topical application and are characterized by a low permeability to the stratum corneum (the outer skin layer of an individual) and/or a low allergenic potential. Surprisingly, such compounds have beneficial properties in the treatment of certain diseases and lack the undesired damages to healthy skin entailed by prior art compounds. ALA (5-aminolevulinic acid)-esters of body-owned, natural compound such as aminoacids, steroids, carbohydrades, alcohols are preferred, examples of photosensitizers of the present invention. The compounds of the present invention are used in the treatment of skin diseases such as psoriasis, sebaceous glands related conditions including acne, seborrhoic dermatitis, rosacea, skin cancer and precancer, as well as in cosmetic hair removal.
    Type: Application
    Filed: December 12, 2008
    Publication date: October 28, 2010
    Inventors: Thomas Glanzmann, Jérôme Barge, Georges Wagnieres
  • Patent number: 7807716
    Abstract: There is provided novel amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one amino acid ester compound comprising at least one nitric oxide releasing group, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. Also provided are compositions for increasing nitric oxide physiological levels in a subject, methods for increasing nitric oxide physiological levels in a subject, methods for improving a subject's muscle strength, athletic performances and/or lean body mass gain and or performance in a subject.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: October 5, 2010
    Assignee: Oral Delivery Technology Ltd.
    Inventor: Michael Farber
  • Publication number: 20100240905
    Abstract: The invention relates to novel curcumin and tetrahydrocurcumin derivatives, which have been modified at one phenolic group to incorporate more-reactive groups. The curcumin and tetrahydrocurcumin derivatives are in the form of monomers, dimmers, and polymers.
    Type: Application
    Filed: October 12, 2007
    Publication date: September 23, 2010
    Applicant: RESEARCH FOUNDATION OF CITY UNIVERSITY OF NEW YORK
    Inventors: Krishnaswami Raja, Probal Banerjee, Andrew Auerbach, Wei Shi, William L'Amoreaux
  • Patent number: 7799941
    Abstract: There is provided a process for efficiently producing an anti form of an optically active ?-hydroxy-?-aminocarboxylic acid derivative that is useful as an intermediate for pharmaceuticals and agrochemicals. The process for producing optically active ?-hydroxy-?-aminocarboxylic acid derivative of formula (2) or (3) wherein R1 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, R2 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, characterized by comprising subjecting an ?-aminoacyl acetic acid ester compound of formula (1) wherein R1 and R2 have the same meaning as the above, to hydrogenation by catalytic asymmetric hydrogenation in the presence of an acid.
    Type: Grant
    Filed: July 9, 2004
    Date of Patent: September 21, 2010
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yasumasa Hamada, Kazuishi Makino
  • Publication number: 20100224063
    Abstract: The present invention relates to a carbon dioxide absorbent, an ionic liquid obtained by reacting amide and an organic acid and a method of using the same. The amidium-based ionic liquid of the present invention has excellent CO2 absorption capability, which is hardly reduced even with repeated use, is easy to synthesize and has low manufacturing cost thus being useful as a CO2 absorbent.
    Type: Application
    Filed: September 30, 2009
    Publication date: September 9, 2010
    Applicants: Hyundai Motor Company, Kia Motors Corporation
    Inventors: Seok Jin Choi, Jelliarko Palgunadi, Je Eun Kang, Hoon Sik Kim, Sung Yeup Chung
  • Patent number: 7781609
    Abstract: There is provided a process for efficiently producing an anti form of an optically active ?-hydroxy-?-aminocarboxylic acid derivative that is useful as an intermediate for pharmaceuticals and agrochemicals. The process for producing optically active ?-hydroxy-?-aminocarboxylic acid derivative of formula (2) or (3) therein R1 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, R2 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, comprising subjecting an ?-aminoacyl acetic acid ester compound of formula (1) wherein R1 and R2 have the same meaning as the above, to hydrogenation by catalytic asymmetric hydrogenation in the presence of an acid by using as a catalyst a rhodium complex containing as a ligand an optically active compound of formula (4), (4?) or (5) characterized in that the hydrogenation is conducted in the presence of an acetic acid salt.
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: August 24, 2010
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yasumasa Hamada, Kazuishi Makino
  • Publication number: 20100210569
    Abstract: The instant invention constitutes an unique subject matter as a whole which has four individual aspects: (1) a class of chiral, non-racemic, synthetic carnitinoid analog carrier molecules which constitute biocompatible transport compounds not found in nature; (2) a subsequently formed, mitochondria-targeting, coupled antioxidant-carrier complex comprising an antioxidant reversibly attached to and releasable from the synthetic carrier molecule; (3) a method for introducing a biologically active antioxidant into the interior of mitochondria of a living cell for subsequent reaction with such reactive oxygen species may then be present; and (4) a system for delivering a biologically active antioxidant to the interior of mitochondria within a living cell.
    Type: Application
    Filed: February 12, 2010
    Publication date: August 19, 2010
    Inventor: Kosta Steliou
  • Publication number: 20100209458
    Abstract: The present invention provides an amphiphilic molecule having a plurality of zwitterionic functional groups in its hydrophilic moiety and a molecular assembly comprising the amphiphilic molecule as a constituent lipid. According to a preferred embodiment of the present invention, the molecular assembly of the present invention forms a stable vesicular structure under a physiological pH environment to carry a substance of interest in the vesicular structure, and can release the substance of interest to the outside of the vesicular structure when it is deformed under an acidic pH environment. The molecular assembly of the present invention can be used as a carrier for a drug, a probe, a nucleic acid, a protein or the like.
    Type: Application
    Filed: May 16, 2008
    Publication date: August 19, 2010
    Applicants: Waseda University, JCR Pharmaceuticals Co., Ltd.
    Inventors: Shinji Takeoka, Yosuke Obata, Shoji Tajima, Manabu Ito, Atsushi Mizuno, Natsuko Nishiyama, Yoshito Takeuchi
  • Publication number: 20100204483
    Abstract: The present invention relates to a process for preparing hydrochloride-free 2-dihaloacyl-3-aminoacrylic esters by reacting acid fluorides with dialkylaminoacrylic acid derivatives.
    Type: Application
    Filed: September 13, 2008
    Publication date: August 12, 2010
    Inventors: Sergii Pazenok, Norbert Lui
  • Patent number: 7772340
    Abstract: A subject-matter of the invention is alkoxyamines resulting from ?-phosphorated nitroxides corresponding to the formula: in which R represents an alkyl radical having a number of carbon atoms ranging from 1 to 3, R1 represents a hydrogen atom or a residue: in which R3 represents an alkyl radical having a number of carbon atoms ranging from 1 to 20, and R2 represents a hydrogen atom, an alkyl radical having a number of carbon atoms ranging from 1 to 8, a phenyl radical, an alkali metal, such as Li, Na or K, H4N+, Bu4N+ or Bu3HN+, exhibiting a kinetic dissociation constant kd, measured at 120° C. by EPR, of greater than 0.05 s?1. These compounds can be used as initiators for the (co)polymerizations of at least one monomer which can be polymerized by the radical route.
    Type: Grant
    Filed: July 23, 2003
    Date of Patent: August 10, 2010
    Assignee: Arkema France
    Inventors: Jean-Luc Couturier, Olivier Guerret, Denis Bertin, Didier Gigmes, Sylvain Marque, Paul Tordo, Florence Chauvin, Pierre-Emmanuel Dufils
  • Patent number: 7767811
    Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.
    Type: Grant
    Filed: June 5, 2006
    Date of Patent: August 3, 2010
    Assignee: Brandeis University
    Inventors: Li Deng, Jianfeng Hang, Liang Tang
  • Patent number: 7767844
    Abstract: The present invention at first prepares a penta-alkyl DTPA and then processes a regioselective hydrolysis over the penta-alkyl DTPA while using a metal ion as a catalyst to obtain a tetra-alkyl DTPA, where, by the above two steps, a monoreactive DTPA derivative is manufactured.
    Type: Grant
    Filed: May 23, 2005
    Date of Patent: August 3, 2010
    Assignee: Atomic Energy Council
    Inventors: Te-Wei Lee, Chia-Hsi Yang, Yen-Sheng Ho, Li-Hui Lu, Shu-Ling Chen
  • Publication number: 20100184994
    Abstract: The present invention relates to a process for preparing 3-difluoromethyl-substituted pyrazole compounds of the formula (I) in which R1 is H, halogen, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C3-C8-cycloalkyl, phenyl, naphthyl, hetaryl, cyano, —C(?O)—OR1a, —C(?O)—NR1bR1c, —C(?O)—SR1d or —C(?S)—SR1e; R2 is H, C1-C4-alkyl, benzyl or phenyl; R3 is H, halogen, C1-C8-alkoxy, C1-C8-haloalkoxy, C3-C8-cycloalkoxy, C2-C8-alkenyloxy, C1-C8-alkylthio, C1-C8-haloalkylthio, C3-C8-cyclo-alkylthio or C2-C8-alkenylthio; compounds of the formula (II.a) or (II.b), in which R1 and R3 each have one of the definitions given above; R4 is halogen, —OR4a, —SR4a, —O—SO2—R4a or an —NR4bR4c group; R5 and R6 are each C1-C8-alkyl, C1-C8-haloalkyl, C3-C8-cycloalkyl, benzyl or phenyl, or, together with the nitrogen atom to which they are bonded, are a 3- to 8-membered heterocycle; Lewis acid adducts of compounds of the formula (II.b); the use of compounds of the formula (II.a) or (II.
    Type: Application
    Filed: June 13, 2008
    Publication date: July 22, 2010
    Applicant: BASF SE
    Inventors: Markus Nett, Thomas Grote, Jan Klaas Lohmann, Jochen Dietz, Sebastian Peer Smidt, Michael Rack, Thomas Zierke
  • Publication number: 20100184831
    Abstract: The invention provides a peptide derivative of formula A-B-C wherein A is a polycationic nucleic acid-binding component; B is a spacer element peptide that is susceptible to cleavage within a cell; and C is a cell surface receptor binding component. The invention also provides a lipid derivative of general formula (I): (PEG)q-Linker-Spacer-Cationic headgroup-carbon skeleton-(hydrophobic chain)o wherein: the Linker is a group susceptible to cleavage within a cell; the Spacer is a group linking the Linker to the Cationic headgroup; q denotes the number of PEG chains and q=1, 2 or 3; o denotes the number of hydrophobic chains and o=1, 2 or 3; the carbon skeleton is a group linking the hydrophobic chains to the cationic headgroup. The peptide and lipid derivatives find use in non-viral gene delivery systems.
    Type: Application
    Filed: May 30, 2007
    Publication date: July 22, 2010
    Inventors: Stephen Lewis Hart, Stephanie Grosse, Alethea Bernice Tabor, John Bosco Wong, Martin Elbs, Helen Claire Hailes, Mohd Firouz Mohd Mustapa
  • Publication number: 20100095749
    Abstract: The present invention provides a technique for crystallizing a desired protein at a high probability; namely, a protein crystallizing agent and a method of crystallizing protein. The present invention also provides a technique for determining the conditions for protein crystallization easily with high efficiency; namely, a method of screening the conditions for protein crystallization and a protein crystallization screening reagent. As the protein crystallizing agent, at least one compound selected from the group consisting of a basic amino acid, acidic amino acid, ester derivative of amino acid and amide derivative of amino acid is used, or at least one of these compounds is used in combination with another protein crystallizing agent.
    Type: Application
    Filed: September 19, 2007
    Publication date: April 22, 2010
    Inventors: Hiroshi Yamaguchi, Len Ito
  • Patent number: 7692034
    Abstract: The invention relates to novel synthesis methods for the preparation of the intermediates, which are suitable for the preparation of statin derivatives, especially to novel synthesis methods of the intermediate of formula VI wherein Ra and Rc are each independently of the other hydrogen or a hydroxy-protecting group or together are a bridging hydroxy-protecting group, and Rb is a carboxy-protecting group, which methods are carried out by conversion of the intermediate of formula XIX wherein Ra and Rc are each independently of the other hydrogen or a hydroxy-protecting group, and Rb is a carboxy-protective group.
    Type: Grant
    Filed: January 24, 2007
    Date of Patent: April 6, 2010
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Reinhold Öhrlein, Gabriele Baisch, Hans Jürg Kirner, Frank Bienewald, Stephan Burkhardt, Martin Studer
  • Patent number: 7687660
    Abstract: The present invention relates to intermediates of rosuvastatin and processes for the production thereof.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: March 30, 2010
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Vinod Kumar Kansal, Brijnath P. Chaurasia, Hitesh K. Patel, Vrajlal Gothalia, Hiren Gandhi
  • Publication number: 20100069446
    Abstract: The present invention is directed to a derivative comprised of an L-Threonine bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. The derivative has the same utility as the drug from which it is made, but it has enhanced therapeutic properties. In fact, the derivatives of the present invention enhance at least one or more therapeutic qualities, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.
    Type: Application
    Filed: September 10, 2009
    Publication date: March 18, 2010
    Applicant: SIGNATURE R&D HOLDINGS
    Inventor: V. Ravi Chandran
  • Publication number: 20100056588
    Abstract: In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.
    Type: Application
    Filed: February 14, 2007
    Publication date: March 4, 2010
    Inventors: James Elliot Bradner, Ralph Mazitschek
  • Patent number: 7671231
    Abstract: A process for making an amino acid by the steps of: (a) contacting a compound of formula I with a hydroformylation catalyst and synthesis gas to produce a mixture of aldehyde compounds comprising the formulas IIa, IIb and IIc; (b) reacting the mixture of aldehyde compounds from step (a) to produce a mixture of derivative compounds; (c) contacting the mixture of derivative compounds from step (b) with an enantioselective hydrolase enzyme in the presence of water to produce an L-amino acid having the formula IV; (d) isolating the amino acid having the formula IV in substantially pure form, wherein in formulas I, IIa, IIb, IIc, IIIa, IIIb, IIIc and IV, R is H, alkyl or aryl and R1 and R2 are the same or different alkyl groups and wherein R1 and R2 may be fused.
    Type: Grant
    Filed: January 18, 2006
    Date of Patent: March 2, 2010
    Inventors: Michael C. Lloyd, Edward D. Daugs, Cynthia L. Rand, Wei-Jun Peng
  • Publication number: 20100041803
    Abstract: Hyperbranched polymers and methods for preparing the same are disclosed. The polymers are obtained based on monomers synthesized via reacting a substituted or unsubstituted cyclic anhydride with a bifunctional amine.
    Type: Application
    Filed: August 13, 2009
    Publication date: February 18, 2010
    Applicant: DESIGNER MOLECULES, INC.
    Inventor: Stephen M. Dershem
  • Publication number: 20100022795
    Abstract: It is an objective of the present invention to produce an anti-form of an optically active ?-hydroxy-?-aminocarboxylic acid ester efficiently, simply and industrially advantageously. The objective can be accomplished by directly and selectively producing the anti-form of the optically active ?-hydroxy-?-aminocarboxylic acid ester by asymmetric reduction of a ?-keto-?-aminocarboxylic acid ester using an optically active amine complex as a catalyst. Further, the ?-keto-?-aminocarboxylic acid ester as a raw material can be produced at a high yield by reacting a glycine derivative with a carboxylic acid derivative.
    Type: Application
    Filed: September 26, 2007
    Publication date: January 28, 2010
    Inventors: Tatsuya Honda, Tatsuyoshi Tanaka, Masaru Mitsuda
  • Publication number: 20100009933
    Abstract: The invention relates to the cosmetic use, as a skin moisturizer, of a compound of formula (I): with (i) R1 and R2 represent a hydrogen atom or a C1-C6-alkyl group, or (ii) R1 and R2 can form, together with the nitrogen atom which bears them, a saturated heterocycle with 5 to 7 ring members; R5 representing a hydrogen atom or a (C1-C3) alkyl group; R6 representing a hydrogen atom or a (C1-C4) alkyl group; R3 represents a hydrogen atom or a (C1-C6) alkyl-group, or —OR3 represents a phosphate group; it being possible for the two groups R3 to form, together, an isopropylidene group; R4 represents a hydrogen atom or —OR4 represents a-phosphate group; and the salts, solvates and isomers thereof. The invention also relates to a cosmetic composition comprising a compound (I) and the corresponding new compounds.
    Type: Application
    Filed: May 3, 2007
    Publication date: January 14, 2010
    Applicant: L'OREAL
    Inventor: Xavier Marat
  • Publication number: 20090312450
    Abstract: Polyurethanes, and rigid polyurethane foams in particular, are made using certain amides of modified fatty acids. The fatty acid groups are substituted hydroxymethyl, N-hydroxyalkyl aminoalkyl or hydroxy-substituted ester groups. The amide portion of the molecule contains hydroxyalkyl or other hydroxyl-substituted organic groups bonded to the amide nitrogen.
    Type: Application
    Filed: July 26, 2006
    Publication date: December 17, 2009
    Inventors: Charles A. Martin, Aaron W. Sanders, Jimmy D. Earls, Kurt D. Olson, John R. Briggs, Alan K. Schrock, Zenon Lysenko, David A. Babb
  • Publication number: 20090292099
    Abstract: Methods of producing plant polyols from plant oils include reacting a plant oil with a designed reactant having one or more nucleophilic functional groups and one or more active hydrogen functional groups in the presence of an addition reaction catalyst in a single reaction step. The resultant polyols may be directly reacted with polyisocyanates to produce polyurethanes.
    Type: Application
    Filed: July 28, 2009
    Publication date: November 26, 2009
    Applicant: Athletic Polymer Systems, Inc.
    Inventors: Thomas M. Garrett, Xian Xian Du
  • Publication number: 20090281347
    Abstract: To provide a production method of phosphates of amino acids, typified by ?-aminolevulinic acid phosphate, or esters thereof. A method for producing phosphates of an amino acid or an ester thereof, which comprises allowing an amino acid, an ester thereof or a salt thereof to coexist with phosphoric acids and a basic nitrogen-containing compound.
    Type: Application
    Filed: March 1, 2007
    Publication date: November 12, 2009
    Applicant: COSMO OIL CO., LTD.
    Inventor: Naohisa Tachiya
  • Publication number: 20090261043
    Abstract: Novel di- and tripodal compounds useful as chelators, intermediates for their production and a method for treating an aqueous solution to remove trivalent metal ions are presented.
    Type: Application
    Filed: April 16, 2008
    Publication date: October 22, 2009
    Inventors: Robert A. Yokel, Wesley R. Harris, Christopher D. Spilling, Chang-Guo Zhan
  • Patent number: 7601864
    Abstract: A method for synthesizing 4,4-dihalogen-2-(dialkylamino)methylene-3-oxy-alkylbutyrate and its derivatives has acts of: (a) providing N,N-dialkylamino-alkyl-acrylate in a reaction vessel; (b) adding organic alkali, organic solvent and multiple molecular sieves into the reaction vessel; (c) mixing N,N-dialkylamino-alkyl-acrylate, the organic alkali, the organic solvent and the molecular sieves; and (d) adding 2,2-dihalogen-acetyl-chloride into the reaction vessel and allowing a synthetic reaction of 2,2-dihalogen-acetyl-chloride and N,N-dialkylamino-alkyl-acrylate to obtain 4,4-dihalogen-2-(dialkylamino)methylene-3-oxy-alkylbutyrate. The molecular sieves are able to remove water efficiently to prevent materials in the reaction vessel from undergoing side reactions or changing chemical properties. Furthermore, the molecular sieves are able to adsorb chloride to avoid polymerization reactions for improved yield.
    Type: Grant
    Filed: May 8, 2008
    Date of Patent: October 13, 2009
    Assignee: UFC Corporation
    Inventors: Ling Lu, Shu-Cheng Liao, Ching-Hung Chen, Yu-Sen Hou, Kai-Chiang Huang, Yu-Chin Lee
  • Publication number: 20090246671
    Abstract: The invention provides a developer and a processing method for a light sensitive planographic printing plate material (also referred to simply as a planographic printing plate material) providing excellent contamination resistance during printing and high reproduction of dot and line images.
    Type: Application
    Filed: August 11, 2006
    Publication date: October 1, 2009
    Applicant: KONICA MINOLTA MEDICAL & GRAPHIC, INC.
    Inventor: Toshitsugu Suzuki