Oxy, Aldehyde Or Ketone Group In Acid Moiety Patents (Class 560/170)
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Publication number: 20120201962Abstract: 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: ApplicationFiled: June 23, 2010Publication date: August 9, 2012Applicant: FUJIFILM CorporationInventors: Ken Kawata, Saisuke Watanabe, Hiroshi Kawamoto
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Publication number: 20120165385Abstract: 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: ApplicationFiled: March 5, 2012Publication date: June 28, 2012Applicant: LUBRIZOL LIMITEDInventor: Dean Thetford
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Patent number: 8207370Abstract: 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: GrantFiled: September 26, 2007Date of Patent: June 26, 2012Assignee: Kaneka CorporationInventors: Tatsuya Honda, Tatsuyoshi Tanaka, Masaru Mitsuda
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Patent number: 8198325Abstract: 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: GrantFiled: June 28, 2007Date of Patent: June 12, 2012Assignee: Industry Foundation of Chonnam National UniversityInventors: Jonghoon Oh, Jee-Bum Lee, Hyoung-Ryun Park
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Patent number: 8188295Abstract: 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: GrantFiled: June 13, 2008Date of Patent: May 29, 2012Assignee: BASF SEInventors: Markus Nett, Thomas Grote, Jan Klaas Lohmann, Jochen Dietz, Sebastian Peer Smidt, Michael Rack, Thomas Zierke
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Publication number: 20120108680Abstract: 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: ApplicationFiled: May 14, 2010Publication date: May 3, 2012Applicants: KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION, NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Masahiro Goto, Tatsuo Maruyama, Nobuhide Miyachi
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Publication number: 20120095096Abstract: 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: ApplicationFiled: April 19, 2010Publication date: April 19, 2012Applicant: The Regents of the University of CaliforniaInventors: Edward A. Dennis, George Kokotos, Violetta Constantinou-Kokotou
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Publication number: 20120029198Abstract: 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: ApplicationFiled: December 22, 2010Publication date: February 2, 2012Applicant: EASTMAN CHEMICAL COMPANYInventors: Liu Deng, Neil Warren Boaz
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Publication number: 20110306600Abstract: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.Type: ApplicationFiled: June 10, 2011Publication date: December 15, 2011Applicant: Grunenthal GmbHInventor: Ramesh SESHA
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Patent number: 8034748Abstract: 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: GrantFiled: January 26, 2007Date of Patent: October 11, 2011Assignee: Clariant Produkte (Deutschland) GmbHInventors: Uwe Dahlmann, Michael Feustel
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Patent number: 8013104Abstract: 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: GrantFiled: August 13, 2009Date of Patent: September 6, 2011Assignee: Designer Molecules, Inc.Inventor: Stephen M. Dershem
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Publication number: 20110166025Abstract: Esteramide compounds are useful solvents/coalescing agents for a variety of phytosanitary, cleaning, degreasing, stripping, lubricating, coating and pigment/ink compositions.Type: ApplicationFiled: January 23, 2009Publication date: July 7, 2011Applicant: RHODIA OPERATIONSInventors: Olivier Jentzer, Massimo Guglieri
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Publication number: 20110105610Abstract: 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: ApplicationFiled: July 3, 2008Publication date: May 5, 2011Inventors: Edward A. Dennis, Daren Stephen, Samuel David, Ruben Lopez-Vales, Athena Kalyvas, George Kokotos, Violetta Constantinou-Kokoton, Efrosini Barbayianni, Victoria Magrioti
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Patent number: 7932326Abstract: 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: GrantFiled: April 16, 2008Date of Patent: April 26, 2011Assignee: The University of Kentucky Research FoundationInventors: Robert A. Yokel, Wesley R. Harris, Christopher D. Spilling, Chang-Guo Zhan
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Publication number: 20110086915Abstract: 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: ApplicationFiled: December 6, 2010Publication date: April 14, 2011Inventors: Karl E. GIERSKCKY, Johan Moan, Qian Peng, Harald Steen, Trond Warloe, Alf Bjørseth
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Publication number: 20110065920Abstract: 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: ApplicationFiled: August 27, 2008Publication date: March 17, 2011Applicant: ratiopharm GmbHInventors: Armin Boerner, Gerd Koenig, Natalia Andrushko, Vasyl Andrushko
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Patent number: 7906676Abstract: 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: GrantFiled: August 9, 2007Date of Patent: March 15, 2011Assignee: LG Life Sciences Ltd.Inventors: Hyun Ik Shin, Hyeong Wook Choi, Jae Hoon Lee, Kyu Woong Lee
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Patent number: 7888526Abstract: 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: GrantFiled: March 29, 2005Date of Patent: February 15, 2011Assignee: Photocure ASAInventors: Jon Erik Braenden, Aslak Godal, Nils Olav Nilsen, Jo Klaveness
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Publication number: 20110021482Abstract: 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: ApplicationFiled: September 17, 2010Publication date: January 27, 2011Inventors: Harold L. Kohn, Christophe Salomé, Elise Salomé-Grosjean
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Publication number: 20110021761Abstract: 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: ApplicationFiled: October 5, 2010Publication date: January 27, 2011Applicant: Nektar TherapeuticsInventors: Antoni Kozlowski, Xiaoming Shen, Michael D. Bentley, Zhihao Fang, Tony L. Sander
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Publication number: 20110015406Abstract: 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: ApplicationFiled: March 11, 2009Publication date: January 20, 2011Applicant: Mitsui Chemicals Agro, Inc.Inventors: Hideki Umetani, Takeshi Kakimoto, Yoji Aoki
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Publication number: 20100273725Abstract: 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: ApplicationFiled: December 12, 2008Publication date: October 28, 2010Inventors: Thomas Glanzmann, Jérôme Barge, Georges Wagnieres
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Patent number: 7807716Abstract: 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: GrantFiled: September 23, 2009Date of Patent: October 5, 2010Assignee: Oral Delivery Technology Ltd.Inventor: Michael Farber
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Publication number: 20100240905Abstract: 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: ApplicationFiled: October 12, 2007Publication date: September 23, 2010Applicant: RESEARCH FOUNDATION OF CITY UNIVERSITY OF NEW YORKInventors: Krishnaswami Raja, Probal Banerjee, Andrew Auerbach, Wei Shi, William L'Amoreaux
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Patent number: 7799941Abstract: 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: GrantFiled: July 9, 2004Date of Patent: September 21, 2010Assignee: Nissan Chemical Industries, Ltd.Inventors: Yasumasa Hamada, Kazuishi Makino
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Publication number: 20100224063Abstract: 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: ApplicationFiled: September 30, 2009Publication date: September 9, 2010Applicants: Hyundai Motor Company, Kia Motors CorporationInventors: Seok Jin Choi, Jelliarko Palgunadi, Je Eun Kang, Hoon Sik Kim, Sung Yeup Chung
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Patent number: 7781609Abstract: 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: GrantFiled: January 12, 2006Date of Patent: August 24, 2010Assignee: Nissan Chemical Industries, Ltd.Inventors: Yasumasa Hamada, Kazuishi Makino
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Publication number: 20100210569Abstract: 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: ApplicationFiled: February 12, 2010Publication date: August 19, 2010Inventor: Kosta Steliou
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Publication number: 20100209458Abstract: 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: ApplicationFiled: May 16, 2008Publication date: August 19, 2010Applicants: Waseda University, JCR Pharmaceuticals Co., Ltd.Inventors: Shinji Takeoka, Yosuke Obata, Shoji Tajima, Manabu Ito, Atsushi Mizuno, Natsuko Nishiyama, Yoshito Takeuchi
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Publication number: 20100204483Abstract: 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: ApplicationFiled: September 13, 2008Publication date: August 12, 2010Inventors: Sergii Pazenok, Norbert Lui
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Patent number: 7772340Abstract: 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: GrantFiled: July 23, 2003Date of Patent: August 10, 2010Assignee: Arkema FranceInventors: Jean-Luc Couturier, Olivier Guerret, Denis Bertin, Didier Gigmes, Sylvain Marque, Paul Tordo, Florence Chauvin, Pierre-Emmanuel Dufils
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Patent number: 7767811Abstract: 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: GrantFiled: June 5, 2006Date of Patent: August 3, 2010Assignee: Brandeis UniversityInventors: Li Deng, Jianfeng Hang, Liang Tang
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Patent number: 7767844Abstract: 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: GrantFiled: May 23, 2005Date of Patent: August 3, 2010Assignee: Atomic Energy CouncilInventors: Te-Wei Lee, Chia-Hsi Yang, Yen-Sheng Ho, Li-Hui Lu, Shu-Ling Chen
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Publication number: 20100184994Abstract: 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: ApplicationFiled: June 13, 2008Publication date: July 22, 2010Applicant: BASF SEInventors: Markus Nett, Thomas Grote, Jan Klaas Lohmann, Jochen Dietz, Sebastian Peer Smidt, Michael Rack, Thomas Zierke
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Publication number: 20100184831Abstract: 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: ApplicationFiled: May 30, 2007Publication date: July 22, 2010Inventors: Stephen Lewis Hart, Stephanie Grosse, Alethea Bernice Tabor, John Bosco Wong, Martin Elbs, Helen Claire Hailes, Mohd Firouz Mohd Mustapa
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Publication number: 20100095749Abstract: 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: ApplicationFiled: September 19, 2007Publication date: April 22, 2010Inventors: Hiroshi Yamaguchi, Len Ito
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Patent number: 7692034Abstract: 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: GrantFiled: January 24, 2007Date of Patent: April 6, 2010Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Reinhold Öhrlein, Gabriele Baisch, Hans Jürg Kirner, Frank Bienewald, Stephan Burkhardt, Martin Studer
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Patent number: 7687660Abstract: The present invention relates to intermediates of rosuvastatin and processes for the production thereof.Type: GrantFiled: April 18, 2008Date of Patent: March 30, 2010Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Vinod Kumar Kansal, Brijnath P. Chaurasia, Hitesh K. Patel, Vrajlal Gothalia, Hiren Gandhi
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Publication number: 20100069446Abstract: 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: ApplicationFiled: September 10, 2009Publication date: March 18, 2010Applicant: SIGNATURE R&D HOLDINGSInventor: V. Ravi Chandran
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Publication number: 20100056588Abstract: 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: ApplicationFiled: February 14, 2007Publication date: March 4, 2010Inventors: James Elliot Bradner, Ralph Mazitschek
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Patent number: 7671231Abstract: 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: GrantFiled: January 18, 2006Date of Patent: March 2, 2010Inventors: Michael C. Lloyd, Edward D. Daugs, Cynthia L. Rand, Wei-Jun Peng
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Publication number: 20100041803Abstract: 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: ApplicationFiled: August 13, 2009Publication date: February 18, 2010Applicant: DESIGNER MOLECULES, INC.Inventor: Stephen M. Dershem
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Publication number: 20100022795Abstract: 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: ApplicationFiled: September 26, 2007Publication date: January 28, 2010Inventors: Tatsuya Honda, Tatsuyoshi Tanaka, Masaru Mitsuda
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Publication number: 20100009933Abstract: 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: ApplicationFiled: May 3, 2007Publication date: January 14, 2010Applicant: L'OREALInventor: Xavier Marat
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Publication number: 20090312450Abstract: 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: ApplicationFiled: July 26, 2006Publication date: December 17, 2009Inventors: Charles A. Martin, Aaron W. Sanders, Jimmy D. Earls, Kurt D. Olson, John R. Briggs, Alan K. Schrock, Zenon Lysenko, David A. Babb
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Publication number: 20090292099Abstract: 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: ApplicationFiled: July 28, 2009Publication date: November 26, 2009Applicant: Athletic Polymer Systems, Inc.Inventors: Thomas M. Garrett, Xian Xian Du
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Publication number: 20090281347Abstract: 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: ApplicationFiled: March 1, 2007Publication date: November 12, 2009Applicant: COSMO OIL CO., LTD.Inventor: Naohisa Tachiya
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Publication number: 20090261043Abstract: 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: ApplicationFiled: April 16, 2008Publication date: October 22, 2009Inventors: Robert A. Yokel, Wesley R. Harris, Christopher D. Spilling, Chang-Guo Zhan
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Patent number: 7601864Abstract: 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: GrantFiled: May 8, 2008Date of Patent: October 13, 2009Assignee: UFC CorporationInventors: Ling Lu, Shu-Cheng Liao, Ching-Hung Chen, Yu-Sen Hou, Kai-Chiang Huang, Yu-Chin Lee
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Publication number: 20090246671Abstract: 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: ApplicationFiled: August 11, 2006Publication date: October 1, 2009Applicant: KONICA MINOLTA MEDICAL & GRAPHIC, INC.Inventor: Toshitsugu Suzuki