Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/220)
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Publication number: 20110040108Abstract: Embodiments of the invention relate to natural and synthetic inositolphospholipid (IPL) materials, their preparation and applications. They provide compositions of the parent IPL comprising phosphatidylinositol (PI), PI-phosphates (phosphoinositides) and derivatives and analogues, and a process for their production starting from natural IPL. The embodiments further provide functional derivatives of PI for biomedical applications including a platform for drug design and delivery to therapeutic targets in the phosphoinositide mediated cellular signaling and allied cascades. The embodiments pertain to IPL having absolute stereo-structure. The embodiments further pertain to unique IPL and PI product compositions for defined applications, particularly pharmaceutical compositions for prophylaxis and treatment of diseases related to aberrant cellular and nuclear signaling mediated by PI and PI derived phosphates, and associated phosphoinositide specific enzymes including PI-PLC and PI 3-kinase.Type: ApplicationFiled: October 26, 2010Publication date: February 17, 2011Applicant: Nutrimed BioetechInventor: Rajindra Aneja
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Publication number: 20110038952Abstract: This invention relates with the gambogic acid glycoside derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: X1, X2, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 or/and R12 is, independently at each occurrence, optionally substituted glycosyl, optionally substituted multi-hydroxyl, optional substituent oxy, optional substituent containing carbon, oxygen, sulfur, nitrogen or phosphorus element. Compounds of the present invention are useful as therapeutically effective agents of anti-cancer, anti-virus and anti-bacterial. This invention also relates with their preparative methods and applications.Type: ApplicationFiled: September 26, 2008Publication date: February 17, 2011Inventor: Lifeng Xu
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Patent number: 7872044Abstract: The present invention is directed to a compound of Formula (I): or an enantiomer, diastereomer, polymorph or pharmaceutically acceptable salt thereof and methods for preparing said compounds and compositions, intermediates and derivatives thereof, and methods for treating inflammatory or serine protease mediated disorders.Type: GrantFiled: October 18, 2007Date of Patent: January 18, 2011Assignee: Janssen Pharmaceutica NVInventors: Michael Greco, Michael Hawkins, Eugene Powell, Bruce E. Maryanoff
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Patent number: 7868147Abstract: A fluorescent probe which is represented by the following formula (I): (wherein, R1 represents a monovalent substituent other than hydrogen atom, carboxy group, or sulfo group; R2 represents hydrogen atom, or a monovalent substituent; R3 and R4 each independently represents hydrogen atom or a halogen atom; and R5 represents a monovalent group which is cleaved by contact with a measuring object, provided that a combination of R1 and R2 is selected so that the oxidation potential of the benzene ring to which they bind makes (1) the compound represented by the formula (I) substantially no fluorescent before the cleavage, and (2) a compound after the cleavage, which is derived from the compound represented by the formula (I), substantially highly fluorescent after the cleavage).Type: GrantFiled: September 3, 2004Date of Patent: January 11, 2011Assignees: Sekisui Medical Co., Ltd.Inventors: Tetsuo Nagano, Mako Kamiya, Yasuteru Urano
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Patent number: 7858784Abstract: Ligands for transition metals are disclosed herein, which may be used in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The disclosed methods provide improvements in many features of the transition-metal-catalyzed reactions, including the range of suitable substrates, number of catalyst turnovers, reaction conditions, and efficiency. For example, improvements have been realized in transition-metal-catalyzed cross-coupling reactions.Type: GrantFiled: December 12, 2008Date of Patent: December 28, 2010Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Brett P. Fors, David S. Surry
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Publication number: 20100317625Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases.Type: ApplicationFiled: May 21, 2007Publication date: December 16, 2010Inventors: Frank Dininno, Milton L. Hammond, Kevin Dykstra, Seongkon Kim, Qiang Tan, Katherine Young, Jeffrey Donald Hermes, Stephane Raeppel, Michael Mannion, Nancy Z. Zhou, Frederic Gaudette, Arkadii Vaisburg, Jubrail Rahil, Nafsika Georgopapadakou
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Publication number: 20100305070Abstract: The disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.Type: ApplicationFiled: April 30, 2010Publication date: December 2, 2010Applicant: The University Court of the University of DundeeInventors: Steven Albert Everett, Saraj Ulhaq
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Publication number: 20100298272Abstract: A new anticancer compounds of formula (1) Drugs and pharmaceutical compositions to be used in human or veterinary medicine, which include at least one compound of formula (1).Type: ApplicationFiled: July 7, 2008Publication date: November 25, 2010Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Jean-Luc Pirat, David Virieux, Ludovic Clarion, Jean-Noel Volle, Norbert Bakalara, Marcel Mersel, Jerome Montbrun, Henri-Jean Cristau
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Publication number: 20100292190Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.Type: ApplicationFiled: February 14, 2006Publication date: November 18, 2010Applicant: Bionomics LimitedInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
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Publication number: 20100291547Abstract: The present disclosure is directed to fluorogenic schiff base-forming dyes capable of detecting analytes containing aldehyde and ketone groups. The dyes contain nucleophilic hydrazinyl appendages and are capable of binding and detecting analytes in situ.Type: ApplicationFiled: January 23, 2009Publication date: November 18, 2010Applicant: Life Technologies CorporationInventors: Aimei Chen, Kyle Gee, Hee Chol Kang
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Publication number: 20100279983Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroarylsulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammonium groups. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazidime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 21, 2007Publication date: November 4, 2010Inventors: Frank Dininno, Milton L. Hammond, Kevin Dykstra, Seongkon Kim, Qiang Tan, Katherine Young, Jeffrey Donald Hermes, Helen Chen, Stephane Raeppel, Michael Mannion, Frederic Gaudette, Arkadii Vaisburg, Jubrail Rahil, Nafsika Georgopapadakou, Nancy Z. Zhou
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Publication number: 20100267673Abstract: Tocopheryl succinate derivatives according to formula I: are described. These compounds increase the activity of protein phosphatase 2A, can be included in pharmaceutical compositions, and can be used for the treatment of androgen receptor-dependent cancers such as prostate cancer.Type: ApplicationFiled: April 13, 2010Publication date: October 21, 2010Applicant: THE OHIO SATE UNIVERSITY RESEARCH FOUNDATIONInventors: Ching-Shih Chen, Dasheng Wang, Samuel K. Kulp
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Publication number: 20100261903Abstract: Reagents are provided for the introduction of phosphonate groups into fluorescent dyes. Methods are also provided for preparing dye conjugates.Type: ApplicationFiled: January 6, 2010Publication date: October 14, 2010Inventors: Eugeny Lukhtanov, Alexei Vorobiev
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Publication number: 20100255521Abstract: Disclosed are compounds of the formula (I): wherein R3, R4, R5, R9, and R10 are selected from the group consisting of H and groups or atoms other than H, and R6 and R8 are halo or hydrogen; X1, X2, and X3 are independently O or S; provided that R9 and R10 are not simultaneously H, when all of X1, X2, and X3 are O; and of the formula (II) wherein R11-R14 are selected from the group consisting of H and groups or atoms other than H; X4-X9 are independently O or S; n and m are 0 or 1 but m and n cannot be 0 simultaneously; R15-R24 can be H or any substituent so long as the compound of formula II upon hydrolysis provides a fluorescent compound. These compounds are useful as substrates with high specificity for organophosphatase particularly human paraoxonase and bacterial organophosphorus hydrolase.Type: ApplicationFiled: January 3, 2007Publication date: October 7, 2010Inventors: Serguei Soukharev, David Hammond
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Publication number: 20100204183Abstract: The invention relates to novel and known substituted phosphonates for use in ameliorating amyloid aggregates, particularly for use in the treatment of Alzheimer's disease.Type: ApplicationFiled: May 2, 2008Publication date: August 12, 2010Applicant: QUEEN MARY & WESTFIELD COLLEGEInventors: Alice Sullivan, Adina Michael-Titus, Lesley Robson
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Publication number: 20100183517Abstract: Compounds of the formula, A-L-B, wherein A is glutamate or a glutamate analog; L is a phosphoramidate or a phosphoramidate analog; and B is serine or a serine analog are described which are potent inhibitors of prostate-specific membrane antigen (PMSA). Such compounds are useful in treatment of prostate cancer; and when chemically attached to a fluorescent dye, can efficiently and selectively label prostate cancer cells for fluorescent imaging.Type: ApplicationFiled: January 22, 2010Publication date: July 22, 2010Applicant: CANCER TARGETED TECHNOLOGY LLCInventor: Cliff Berkman
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Publication number: 20100168422Abstract: Provided herein are compounds and methods useful for preparing hexahydrofuro[2,3-b]furan-3-ol. Hexahydrofuro[2,3-b]furan-3-ol can be efficiently synthesized in four steps from readily available starting materials.Type: ApplicationFiled: December 30, 2008Publication date: July 1, 2010Inventor: Weiping Chen
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Patent number: 7741506Abstract: A myo-inositol derivative: R1, R2, R3 and R4 are identical, being selected from PO3H2, PO3Na2, PO3K2, PO3Li2, PO3Ca, PO3Mg, PO3(NH4)2, PO3(RNH3)2, PO3(R2NH2)2, PO3(R4N)2, PO(OR)2, H, COZ and BHPP, where R is benzyl or alkyl of 1 to 6 carbon atoms and Z is an alkyl or arylalky group providing a cleavable protecting group; R5 is one of H, benzyl, 4-methoxybenzyl, COZ, PO3H2, PO3Na2, PO3K2, PO3Li2, PO3Ca, PO3Mg, PO3(NH4)2, PO3(RNH3)2, PO3(R2NH2)2, PO3(R4N)2, PO(OR)2, and BHPP, where R is benzyl or alkyl of 1 to 6 carbon atoms and Z is an alkyl or arylalky group providing a cleavable protecting group; X is one of CH2, CH2CH2O, and CH2CH2CH2O; n is an integer from 1 to 8; L1 is a single bond or CH2; L2 is one of a single bond, CONH, CH2CONH, CH2CH2CONH, CH2CH2NHCO, CH2CH2NHCONH, CH2CH2NHCSNH, CH2CH2NHSO2, CH2CH2CH2NHCO, CH2CH2CH2NHCONH, CH2CH2CH2NHCSNH, CH2CH2CH2NHSO2, NHCO, NHCONH, NHCSNH, OCONH, CH2, CH2CH2, CH2CH2O, CH2CH2S, CH2CH2NH, CH2CH2CH2, CH2CH2CH2O, CH2CH2CH2S, CH2CH2CH2NH, and NH—SO2; and R6 is a UType: GrantFiled: November 5, 2007Date of Patent: June 22, 2010Assignee: Berry & Associates, Inc.Inventor: David A. Berry
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Publication number: 20100143296Abstract: The present invention relates to new podophyllotoxin inhibitors of topoisomerase II, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 10, 2009Publication date: June 10, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Publication number: 20100130448Abstract: The present invention provides a 3?,4?,5-trimethoxy flavone derivative and a pharmaceutically acceptable salt thereof, preparation thereof, and a pharmaceutical composition for the treatment and prevention of dry eye syndrome comprising the same as an active ingredient. The 3?,4?,5-trimethoxy flavone derivative and its pharmaceutically acceptable salt inhibit corneal damage through excellent stimulatory action on mucus secretion in the conjunctiva and therefore may be effective as a prophylactic or therapeutic agent for dry eye syndrome.Type: ApplicationFiled: June 2, 2008Publication date: May 27, 2010Applicant: DONG-A PHARM. CO., LTDInventors: Seul-Min Choi, Kyung-Koo Kang, Dong-Sung Kim, Jeong-Hoon Kim, Byoung-Ok Ahn, Moo-Hi Yoo, Mi-Jeong Seo, Ju-Mi Kim, Yong-Duck Kim, Sun-Woo Jang, Yong-Sung Shon
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Patent number: 7714149Abstract: The present invention provides a chiral ligand, represented by a formula or its enantiomer: X and X? can be independently O, NH, NR, NCOR or S; each of Z1-Z7 and Z1?-Z7? can be independently H, alkyl, aryl, substituted alkyl, substituted aryl, alkoxyl, aryloxyl, nitro, amide, aryoxide, halide, hydroxyl, carboxylate, hetereoaryl, or a cyclic alkene, fused aryl, or cyclic ether group formed from any two adjacent Z groups or any two adjacent Z? groups; Y and Y? can be independently OH, OR, NH2, NHR, NR2, SH, PR2, OPR2, NHPR2, OP(OR)2, COOH, COOR, CONHR, or a linking group formed from Y and Y? groups together. Processes of preparing these ligands, catalysts that employ them and methods of using the catalysts are also provided.Type: GrantFiled: September 1, 2005Date of Patent: May 11, 2010Assignee: The Penn State Research FoundationInventor: Xumu Zhang
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Publication number: 20100113255Abstract: Novel bidentate ligands of general formula (I) are described Formula (I): R represents a hydrocarbyl aromatic structure. The substituent(s) Yx on the aromatic structure has a total X=1-n ?tYX of atoms other than hydrogen such that X-1-n?tYX is 4 where n is the total number of substituent(s) YX and tYX represents the total number of atoms other than hydrogen on a particular substituent YX. The groups X1, X2, X3 and X4 are joined to Q1 or Q2 via tertiary carbon atoms to the respective atom Q1 or Q2; and Q1 and Q2 each independently represent phosphorus, arsenic or antimony. A catalyst system and a process for the carbonylation of ethylenically unsaturated compounds utilising the catalyst system is also described.Type: ApplicationFiled: November 27, 2007Publication date: May 6, 2010Applicant: LUCITE INTERNATIONAL UK LIMITEDInventors: Graham Ronald Eastham, Ian Butler
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Publication number: 20100099875Abstract: The invention relates to novel organo phosphorus P-chiral optically active compounds of formula (I) having a hydroxyl, mercapto, amino, carboxyl, sulfonyl group on aryl near a phosphorus atom, to the preparation and the use thereof in then asymmetrical catalysis of unsaturated compounds. Novel acylphosphine optically pure ligands embodied in the form of transition metal complexes exhibit an increased activity and enantloselectivity, in particular in asymmetrical hydrogenation, in comparison with the same type Uganda such as DiPAMP.Type: ApplicationFiled: June 20, 2006Publication date: April 22, 2010Applicants: PHOSPHOENIX SARL, NATIONAL INSTITUTE OF CHEMISTRYInventors: Michel Stephan, Barbara Mohar
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Publication number: 20100087634Abstract: Fluorous-tagged oligonucleotide reagents and an oligonucleotide purification methodology making use thereof, the method comprising: Synthesizing oligonucleotides using oligonucleotide reagents each bearing at least one fluorous group to yield a mixture of synthesis products and reagents, the mixture including at least one target synthesized oligonucleotide bearing at least one fluorous group; passing the mixture through a separation medium having an affinity for the at least one fluorous group so that the target synthesized oligonucleotide bearing at least one fluorous group is adsorbed by the separation medium; washing the separation medium with at least a first solvent to selectively dissociate therefrom substantially all synthesis products and reagents of the heterogenous mixture other than the at least one target synthesized oligonucleotide bearing at least one fluorous group; and subsequently dissociating the at least one synthesized oligonucleotide from the separation medium, with or without the fluorouType: ApplicationFiled: October 20, 2009Publication date: April 8, 2010Applicant: BERRY & ASSOCIATES, INC.Inventors: David A. Berry, William H. Pearson
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Patent number: 7687540Abstract: The present invention relates to certain esters of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1 and R2 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.Type: GrantFiled: July 10, 2007Date of Patent: March 30, 2010Assignee: Aventis Pharmaceuticals Inc.Inventors: Alan John Collis, Gregory Bernard Poli, Yong Mi Choi-Sledeski
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Patent number: 7683186Abstract: A phosphorus compound of formula (1): wherein R1 denotes a hydrogen atom or a hydroxy protective group; R2 denotes a group defined by the following formula (R2-1) or (R2-2); R3, R4, R5, and R6 may be the same or different and independently denote a hydrogen atom, an alkyl group, an alkoxy group, an acyloxy group, a halogen atom, a haloalkyl group, or a dialkylamino group; two among R3, R4, R5, and R6 may form an aromatic ring optionally having a substituent group, and two among R3, R4, R5, and R6 may form a methylene chain optionally having a substituent group or a (poly)methylenedioxy group optionally having a substituent group: wherein (R2-1) and (R2-2), R7 denotes an alkyl group, a cycloalkyl group, an aryl group, an alkoxy group, or an aryloxy group; R8 and R9 independently denote a hydrogen atom, an alkyl group, or an aryl group; z denotes a divalent group; and a denotes an integer of 0 or 1.Type: GrantFiled: December 7, 2007Date of Patent: March 23, 2010Assignees: National University Corporation Tokyo University of Agriculture and technology, Takasago International CorporationInventors: Ken Tanaka, Wataru Kuriyama
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Publication number: 20100048512Abstract: Administration of either a tocopherol represented by the general formula (1) or a tocotrienol compound ester derivative before or after exposure to radiation is effective in preventing or treating health disorders caused by the radiation exposure.Type: ApplicationFiled: November 14, 2007Publication date: February 25, 2010Applicants: National Institute of Radiological Sciences, Fukuoka UniversityInventors: Kazunori Anzai, Megumi Ueno, Haruko Yakumaru, Junichi Ueda, Makoto Akashi, Shizuko Kobayashi, Jiro Takata, Nobuo Ikota
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Publication number: 20100016261Abstract: A compound of formula (I) is described; wherein the substituents are as defined in the text and wherein the compound is intended for use in the production of a vascular damaging effect in a warm-blooded animal.Type: ApplicationFiled: December 19, 2007Publication date: January 21, 2010Inventors: Timothy William Wallace, David John Edwards, John Anthony Hadfield
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Patent number: 7648710Abstract: There is provided an emulsion composition for therapeutic administration comprising: (a) at least one mono-electron transfer agent phosphate derivative; (b) at leas tone di-electron transfer agent phosphate derivative; wherein the amount of mono-electron transfer agent phosphate derivatives is no less than equimolar to the amount of di-electron transfer agent phosphate; and (c) a suitable carrier.Type: GrantFiled: November 14, 2001Date of Patent: January 19, 2010Assignee: Vital Health Sciences Pty Ltd.Inventor: Simon Michael West
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Patent number: 7649015Abstract: Phosphonate substituted compounds with HIV protease inhibitory properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit HIV protease activity and/or are useful therapeutically for the treatment of AIDS and other antiviral infections, as well as in assays for the detection of HIV protease.Type: GrantFiled: April 25, 2003Date of Patent: January 19, 2010Assignee: Gilead Sciences, Inc.Inventors: Murty N. Arimili, Xiaowu Chen, Maria Fardis, Gong-Xin He, Haolun Jin, Choung U. Kim, William A. Lee, Kuei-Ying Lin, Hongtao Liu, Richard L. Mackman, Michael L. Mitchell, Hyung-Jung Pyun, Mark Sparacino, Sundaramoorthi Swaminathan, Jianying Wang, Matthew A. Williams, Lianhong Xu, Zheng-Yu Yang, Richard H. Yu, Jiancun Zhang, Lijun Zhang
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Publication number: 20100004209Abstract: The present invention relates to compounds of the formula (I), where R1 to each, independently of one another, denote H, hydroxyl or alkoxy having 1 to 8 C atoms, R4 denotes alkyl having 1 to 4 C atoms, H, hydroxyl or alkoxy having 1 to 8 C atoms, R5 denotes H or hydroxyl, and R6 denotes H or alkyl having 1 to 18 C atoms, or salts thereof, but where all R1 to R4 together cannot be equal to H, to compositions, and to the preparation and use thereof.Type: ApplicationFiled: October 4, 2007Publication date: January 7, 2010Applicant: MERCK PATENT GESELLSCHAFTInventors: Christophe Carola, Herwig Buchholz
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Publication number: 20090298870Abstract: 4-O esters of podophyllotoxin and 4?-demethylepipodophyllotoxin are provided. The compounds are 4-O esters of an alkanoic acid or substituted alkanoic acid and podophyllotoxin and 4?-demethylepipodophyllotoxin. The compounds are useful for treating cancer.Type: ApplicationFiled: August 3, 2009Publication date: December 3, 2009Inventor: Li-Xi Yang
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Publication number: 20090291923Abstract: The invention provides novel trioxane dimers having formulae III, IV or V: methods for their preparation, pharmaceutical compositions containing these compounds, and methods for treating cancer and/or malaria using these compounds and compositions.Type: ApplicationFiled: November 17, 2006Publication date: November 26, 2009Applicants: Johns Hopkins Universoty, The Government of the United States of America as Represented by the Secretary of the DHHS NIH, OffiInventors: Gary H. Posner, Ikhyeon Paik, Kristina Borstnik, Wonsuk Chang, Sandra Sinishtaj, William Malo, John Gaetano D'Angelo, Lauren Elaine Woodard, Alvin Solomon Kalinda, Aimee R. Usera, Lindsey Catherine Hess, Andrew Scott Rosenthal, Seongho Oh, Astrid C. Baege
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Patent number: 7589218Abstract: The present invention provides a chiral ligand, represented by a formula or its enantiomer: X and X? can be independently O, NH, NR, NCOR or S; each of Z1-Z7 and Z1?-Z7? can be independently H, alkyl, aryl, substituted alkyl, substituted aryl, alkoxyl, aryloxyl, nitro, amide, aryloxide, halide, hydroxyl, carboxylate, heteroaryl, or a cyclic alkene, fused aryl, or cyclic ether group formed from any two adjacent Z groups or any two adjacent Z? groups; Y and Y? can be independently OH, OR, NH2, NHR, NR2, SH, PR2, OPR2, NHPR2, OP(OR)2, COOH, COOR, CONHR, or a linking group formed from Y and Y? groups together. Processes of preparing these ligands, catalysts that employ them and methods of using the catalysts are also provided.Type: GrantFiled: July 15, 2008Date of Patent: September 15, 2009Assignee: The Penn State Research FoundationInventor: Xumu Zhang
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Publication number: 20090227543Abstract: The invention is related to phosphonate substituted compounds having immuno-modulatory activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: July 1, 2008Publication date: September 10, 2009Inventors: Carina Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Manoj Desai, Maria Fardis, Alan X. Huang, Thorsten Kirschberg, Christopher P. Lee, Richard L. Mackman, Peter H. Nelson, Hyung-Jung Pyun, Adrian S. Ray, William J. Watkins, Jennifer R. Zhang, Sundaramoorthi Swaminathan
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Publication number: 20090227805Abstract: Problem to be Solved: To provide an axially asymmetric optically active biarylphosphorus compound that can easily produced without the step of optical resolution which was almost indispensable in conventional methods. Solution: A method for producing an axially asymmetric phosphorus compound represented by the general formula (1), comprising a cycloaddition reaction of a compound having a triple bond with the use of a catalyst containing rhodium metal and an optically active bisphosphine. (In the formula, J is an oxygen atom, a sulfur atom or BH3; R1 and R2 independently are an alkyl, cycloalkyl, aryl, alkoxy and aryloxy group; a1 and a2 independently are 0 or 1; R3 to R10 independently are an alkyl, cycloalkyl, aryl, alkoxy and aryloxy group; two among R3 to R10 may form a ring; and * is axial asymmetry.Type: ApplicationFiled: March 3, 2009Publication date: September 10, 2009Inventors: Ken Tanaka, Goushi Nishida, Tohru Yokozawa, Yukinori Yusa
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Publication number: 20090221820Abstract: Ligands for transition metals are disclosed herein, which may be used in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The disclosed methods provide improvements in many features of the transition-metal-catalyzed reactions, including the range of suitable substrates, number of catalyst turnovers, reaction conditions, and efficiency. For example, improvements have been realized in transition-metal-catalyzed cross-coupling reactions.Type: ApplicationFiled: December 12, 2008Publication date: September 3, 2009Applicant: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Brett P. Fors, David S. Surry
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Publication number: 20090203649Abstract: A dermatological anti-wrinkle agent and an anti-wrinkle cosmetic are stable and satisfactorily effective against wrinkles. The dermatological anti-wrinkle agent comprises a tocopherol phosphate represented by the following formula (1): and/or a salt thereof, wherein R1, R2, and R3 represent a hydrogen atom or a methyl group. The anti-wrinkle cosmetic includes the anti-wrinkle agent.Type: ApplicationFiled: June 25, 2007Publication date: August 13, 2009Applicant: SHOWA DENKO K.K.Inventors: Eiko Kato, Toshi Tsuzuki
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Publication number: 20090163725Abstract: A phosphonic acid diester derivative represented by the following general formula (1): wherein at least one of R1 and R2 denotes a leaving group.Type: ApplicationFiled: November 30, 2006Publication date: June 25, 2009Inventors: Jun Hiratake, Kanzo Sakata, Liyou Han
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Patent number: 7541454Abstract: Compounds useful in the fluorescent labeling of biological materials are provided along with methods for their use and preparation.Type: GrantFiled: October 25, 2004Date of Patent: June 2, 2009Assignee: Epoch Biosciences, Inc.Inventor: Eugeny A. Lukhtanov
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Publication number: 20090131686Abstract: The present invention relates to a sesamol derivative or its salt, and a skin external composition containing the same. More particularly, the invention relates to a sesamol derivative or its salt, which consists of sesamol and 3-aminopropane phosphoric acid, linked with each other by a phosphoric acid diester bond, and can be degraded into sesamol and 3-aminopropane phosphoric acid by enzymes present on the skin so as to simultaneously show the physiological activities of sesamol and 3-aminopropane phosphoric acid, as well as a preparation method thereof and a skin external composition containing the same.Type: ApplicationFiled: May 29, 2006Publication date: May 21, 2009Applicant: AMOREPACIFIC CORPORATIONInventors: Jae Won You, Ho Sik Rho, Duc Hee Kim, Ih Seop Chang, Ok Sub Lee
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Patent number: 7531682Abstract: The present invention concerns a process for hydrocyanating ethylenically unsaturated organic compounds to compounds containing at least one nitrile function. It relates more particularly to the hydrocyanation of diolefins such as butadiene or of substituted olefins such as alkenenitriles, for instance pentenenitriles. According to the process of the invention the reaction is implemented in the presence of a metal complex catalyst comprising a transition metal such as nickel and an organic ligand.Type: GrantFiled: July 11, 2003Date of Patent: May 12, 2009Assignee: Rhodia Polyamide IntermediatesInventors: Jean-Christophe Galland, Blaise Didillon, Philippe Marion, Damien Bourgeois
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Publication number: 20090069273Abstract: The invention relates to phosphorylated polyphenols, phosphorylated flavonoids, and phosphorylated pyrone analogs. Methods and compositions for the modulation of side effects of substances using such phosphorylated compounds are described. Methods and compositions are described for the modulation of blood-tissue barrier (BTB) transporter activity to increase the efflux of drugs and other compounds out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide lowered side effects when phosphorylated pyrone analogs are coadministered with therapeutic agents.Type: ApplicationFiled: July 30, 2008Publication date: March 12, 2009Inventors: Wendye ROBBINS, Ving Lee
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Publication number: 20090054376Abstract: The present invention relates to novel benzofuran compounds, to pharmaceutical compositions that include such compounds, and to methods of use thereof. Certain compounds of the invention share some pharmacological properties with cannabinoids and have a common wide range of beneficial therapeutic indications. In particular, compounds of the invention are useful as analgesic, neuroprotective, immunomodulatory and anti-inflammatory agents.Type: ApplicationFiled: May 31, 2006Publication date: February 26, 2009Inventors: Avihai Yacovan, Flavio Grynszpan, Alexander Aizikovich, Marcus Stephen Brody, Avi Bar-Joseph, Sigal Meilin
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Publication number: 20090036409Abstract: The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.Type: ApplicationFiled: August 20, 2008Publication date: February 5, 2009Inventors: Michael J. Hawkins, Michael N. Greco, Eugene Powell, Lawrence De Garavilla, Bruce E. Maryanoff
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Publication number: 20080319209Abstract: An improved process is described for preparing (disubstitutedpropenyl) phenylalkyl substituted dihydrobenzofurans. This improved process is focused on steps to produce key intermediates, namely disubstitutedphenolylalkyl substituted dihydrobenzofurans of formula I: where R3, R4, R5, R6 and x are defined herein.Type: ApplicationFiled: February 16, 2006Publication date: December 25, 2008Inventors: Guozhi Wang, Charles E. Hatch III, Jaidev S. Goudar, Russell Patera
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Patent number: 7456214Abstract: Chrome compounds have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds as well as related derivatives are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.Type: GrantFiled: May 21, 2004Date of Patent: November 25, 2008Assignees: Baylor University, OXiGENE, Inc.Inventors: Kevin G. Pinney, Phyllis Arthasary, Anupama Shirali, Klaus Edvardsen, David J. Chaplin
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Publication number: 20080261237Abstract: The present invention relates to inositol phosphate derivatives, in which the inositol phosphate is substituted with one or two reactive groups G or one or two conjugated substances or molecules M, said reactive group(s) G or said substance(s) or molecule(s) M being linked to IP1 via a linkage group L, M being chosen from the following group: a tracer, an immunogen, a member of a binding partner pair, a solid support. Application: tools allowing the study of the inositol phosphate cycle and therefore, indirectly, the study of seven transmembrane domain receptors coupled to phospholipase C, receptors having a tyrosine kinase activity, and in general enzymes involved in the variations of the intracellular concentration of IP1.Type: ApplicationFiled: December 2, 2005Publication date: October 23, 2008Inventors: Herve Bazin, Herve Ansanay, Eric Trinquet, Gerard Mathis
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Publication number: 20080221070Abstract: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion. The Bone Active Portion is derived from an estrogenic agent. Compounds can also include a Blocking Group (RP) that reduces or eliminates the estrogenic activity of the Bone Active Portion.Type: ApplicationFiled: March 6, 2008Publication date: September 11, 2008Inventors: William M. Pierce, K. Grant Taylor, Leonard C. Waite
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Publication number: 20080214811Abstract: The invention provides a novel class of xanthene dyes, some of which are functionalized to allow their coupling to conjugation partners of interest, e.g. biomolecules, drugs, toxins and the like. Also provided are conjugates of the dyes, methods of preparing and using the dyes and their conjugates and kits including the dyes and their conjugates.Type: ApplicationFiled: February 25, 2008Publication date: September 4, 2008Applicant: Biosearch Technologies, Inc.Inventors: Mark Reddington, Matt Lyttle