Phosphorus Attached Directly Or Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/5)
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Patent number: 9249356Abstract: A guest-host liquid crystal dye mixture comprising a calamatic, thermotropic liquid crystal as host and a dichroic fluorescent dye as guest, characterized in that the dichroic fluorescent dye is a multichromophoric dye containing at least a group with the general formula Ry-X1—C1, wherein Ry is a chromophore from the rylene family, C1 is a second chromophore and X1 is a spacer that interrupts the conjugation between Ry and C1, the spacer X1 is selected such that it introduces rigidity against bending or folding over an axis perpendicular to the length of the molecule.Type: GrantFiled: July 3, 2012Date of Patent: February 2, 2016Assignee: PEER+ B.V.Inventors: Casper Laurens Van Oosten, Albertus Petrus Hendrikus Johannes Schenning
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Publication number: 20150087620Abstract: The present invention provides a compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION, which has a superior peripheral blood lymphocyte decreasing action, and is useful for the treatment or prophylaxis of autoimmune diseases; prophylaxis or suppression of resistance or acute rejection or chronic rejection of transplantation of organ or tissue; treatment or prophylaxis of graft-versus-host (GvH) disease due to bone marrow transplantation; or treatment or prophylaxis of allergic diseases.Type: ApplicationFiled: April 23, 2013Publication date: March 26, 2015Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Maiko Hamada, Kaoru Tashiro, Hiroshi Sakashita, Masatoshi Kiuchi, Shuzo Takeda, Kunitomo Adachi
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Publication number: 20140329929Abstract: The invention relates to a dental restorative material which comprises a thermolabile or photolabile polymerizable compound of Formula I: [(Z1)m-Q1-X)]k-T-[Y-Q2-(Z2)n]1??Formula I, in which T represents a thermolabile or photolabile group, Z1 and Z2 in each case independently represent a polymerizable group selected from vinyl groups, CH2?CR1—CO—O— and CH2?CR1—CO—NR2— or an adhesive group selected from —Si(OR)3, —COOH, —O—PO(OH)2, —PO(OH)2, —SO2OH and —SH, wherein at least one Z1 or Z2 is a polymerizable group, Q1 in each case independently is missing or represents an (m+1)-valent linear or branched aliphatic C1-C20 radical which can be interrupted by —O—, —S—, —CO—O—, —O—CO—, —CO—NR3—, —NR3—CO—, —O—CO—NR3—, —NR3—CO—O— or —NR3—CO—NR3—, Q2 in each case independently is missing or represents an (n+1)-valent linear or branched aliphatic C1-C20 radical which can be interrupted by —O—, —S—, —CO—O—, —O—CO—, —CO—NR3—, —NR3—CO—, —O—CO—NR3—, —NR3—CO—O— or —NR3—CO—NR3—, X and Y in each case independently are missingType: ApplicationFiled: September 10, 2012Publication date: November 6, 2014Applicant: IVOCLAR VIVADENT AGInventors: Norbert Moszner, Iris Lamparth, Thorsten Bock, Urs Karl Fischer, Ulrich Salz, Volker Rheinberger, Robert Liska
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Publication number: 20140213725Abstract: The present invention provides a polymerizable inorganic particle dispersant that can achieve an inorganic-organic composite particle and inorganic-organic resin composite material, which have a high refractive index and a high Abbe's number, i.e., which can achieve both of a high refractive index and a high Abbe's number that is non-conventional in a composite with an inorganic particle. The present invention relates to a polymerizable inorganic particle dispersant comprising a compound which includes the following functional groups A, B and Q: A: Polymerizable functional group; B: Carboxyl group, Oxo acid group containing a phosphorous or Oxo acid group containing sulfur; and C: Sulfur-containing divalent or more aliphatic hydrocarbon group, which may contain a hetero atom other than sulfur.Type: ApplicationFiled: March 31, 2014Publication date: July 31, 2014Applicant: NIPPON KASEI CHEMICAL COMPANY LIMITEDInventors: Masanori YAMAZAKI, Naoko Sumitani, Ritsuko Yamauchi, Tomoko Maeda, Takako Takahashi
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Publication number: 20130052184Abstract: The invention provides compounds, compositions, and methods for the treatment of diseases, disorders, or conditions that are modulated by matrix metalloproteinases (MMPs). The disease, disorder, or condition can include, for example, stroke, neurological disorders, or ophthalmological disorders. The treatment can include administering a compound or composition described herein, thereby providing a prodrug compound that metabolizes to an active MMP inhibitor in vivo. The MMP inhibition can be selective inhibition, for example, selective inhibition of MMP-2, MMP-9, and/or MMP-14. Thus, the invention provides non-mutagenic prodrug compounds of the formulas described herein that result in the inhibition of MMPs upon in vivo administration.Type: ApplicationFiled: March 4, 2011Publication date: February 28, 2013Applicant: UNIVERSITY OF NOTRE DAME DU LACInventors: Mayland Chang, Shahriar Mobashery, Mijoon Lee
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Publication number: 20130040209Abstract: A non-aqueous electrolyte solution containing a cyclic sulfone compound having a 1,3-dithietane-1,1,3,3-tetraoxide structure is provided. The cyclic sultone compound is preferably a compound represented by formula (I) [wherein in formula (I), R1 to R4 each represent a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl group, or the like].Type: ApplicationFiled: April 25, 2011Publication date: February 14, 2013Applicant: MITSUI CHEMICALS, INC.Inventors: Shigeru Mio, Mitsuo Nakamura, Hidenobu Nogi, Takashi Hayashi, Takeshi Kobayashi
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Patent number: 8263785Abstract: The present invention is a process for the preparation of chymase modulators, useful in the treatment of inflammatory and serine protease mediated disorders.Type: GrantFiled: October 29, 2009Date of Patent: September 11, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Luigi Anzalone, Penina Feibush, Ilias Konstantinos Dorziotis, Xun Li, Frank J. Villani
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Publication number: 20120016128Abstract: The present invention provides rhodamine lactone phosphoramidites and polymer compositions, methods for making these phosphoramidites and polymer compositions, and methods for using these phosphoramidites and polymer compositions for labeling oligonucleotides. In particular, the present invention provides compositions and methods for labeling the 3?- and 5?-end of oligonucleotides during synthesis of the oligonucleotides.Type: ApplicationFiled: June 27, 2011Publication date: January 19, 2012Inventors: Zhenjun Diwu, Haitao Guo
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Patent number: 7998944Abstract: The present invention is to provide a polymerizable compound which can be a raw material for a resin having high transparency, good heat resistance and mechanical strength required for optical components such as plastic lenses and the like, while attaining a high refractive index (nd) exceeding 1.7, and an optical component composed of such a resin. Disclosed is a compound represented by the general formula (3), wherein, in the formula, M represents a metal atom; X1 and X2 each independently represent a sulfur atom or an oxygen atom; R1 represents a divalent organic group; m represents an integer of 0 or 1 or more; p represents an integer of from 1 to n; q represents an integer of from 1 to (n?p); n represents a valence of a metal atom M; Yq each independently represent an inorganic or organic residue; and when q is 2 or more, Yq may be bonded to one another for forming a ring structure with the intermediary of a metal atom M.Type: GrantFiled: March 26, 2010Date of Patent: August 16, 2011Assignee: Mitsui Chemicals, Inc.Inventors: Atsuo Otsuji, Hiroshi Naruse, Mitsuo Nakamura
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Patent number: 7928247Abstract: Disclosed is a polymerizable composition containing a compound represented by the following general formula (1), wherein, in the formula, M represents P, P?O or P?S; X1 and X2 each independently represent a sulfur atom or an oxygen atom; R1 represents a divalent organic group; m represents 0 or an integer of not less than 1; n represents an integer of not less than 1 but not more than 3; p and q represent (1, 0) or (0, 1); and Y represents an inorganic or organic residue.Type: GrantFiled: June 14, 2007Date of Patent: April 19, 2011Assignee: Mitsui Chemicals, Inc.Inventors: Mitsuo Nakamura, Shinichi Usugi, Hiroshi Naruse, Atsuo Otsuji
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Patent number: 7763739Abstract: The present invention concerns novel bidentante optionally N-containing P-ligands of general formula (I) embracing a two-ring-system and processes for synthesizing them, transition metal complexes of these compounds and their use as catalysts.Type: GrantFiled: April 14, 2005Date of Patent: July 27, 2010Assignee: Evonik Degussa, GmbHInventors: Renat Kadyrov, Juan José Almena Perea, Axel Monsees, Thomas Riermeier, Ilias Ilaldinov
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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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Patent number: 7709598Abstract: To obtain a polymerization initiator (acid generating agent) having excellent power for initiation of cationic polymerization without containing arsenic or antimony. Provided is a specific onium salt or transition metal complex salt of a fluorinated alkyl fluorophosphoric acid.Type: GrantFiled: May 27, 2005Date of Patent: May 4, 2010Assignee: San-Apro LimitedInventors: Hideki Kimura, Jiro Yamamoto, Shinji Yamashita, Mitsuo Kurumaya, Takaaki Sonoda
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Patent number: 7635792Abstract: Polyfluorene polymers and copolymers having substantial amounts (10-100%) of fluorenes coupled at the 2 and 5 positions of fluorene are useful as active layers in OLED devices where triplet energies >2.10 eV are required.Type: GrantFiled: October 14, 2008Date of Patent: December 22, 2009Assignee: General Electric CompanyInventors: James Anthony Cella, Joseph John Shiang, Elliott West Shanklin, Paul Michael Smigelski
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Publication number: 20090192288Abstract: Disclosed is a polymerizable composition containing a compound represented by the following general formula (1), wherein, in the formula, M represents P, P?O or P?S; X1 and X2 each independently represent a sulfur atom or an oxygen atom; R1 represents a divalent organic group; m represents 0 or an integer of not less than 1; n represents an integer of not less than 1 but not more than 3; p and q represent (1, 0) or (0, 1); and Y represents an inorganic or organic residue.Type: ApplicationFiled: June 14, 2007Publication date: July 30, 2009Applicant: MITSUI CHEMICALS, INC.Inventors: Mitsuo Nakamura, Shinichi Usugi, Hiroshi Naruse, Atsuo Otsuji
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Patent number: 7560231Abstract: The present invention is related to compounds comprising mannitol or glucitol derivatives which may be used to build up oligomeric compounds. The invention is further related to uses of these oligomeric compounds for hybridization and as probes. In addition, methods for the detection of nucleic acids are disclosed wherein the oligomeric compounds are used.Type: GrantFiled: December 5, 2003Date of Patent: July 14, 2009Assignee: Roche Molecular Systems, Inc.Inventors: Frank Bergmann, Herbert Von Der Eltz, Christoph Seidel, Kurt Weindel
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Patent number: 7514563Abstract: A process for producing cyano substituted arene boranes is described. The compounds are useful intermediates to pharmaceutical compounds using the cyano group as a reactant.Type: GrantFiled: June 8, 2006Date of Patent: April 7, 2009Assignee: Board of Trustees of Michigan State UniversityInventors: Milton R. Smith, III, Robert E. Maleczka, Ghayoor A. Chotana
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Patent number: 7468360Abstract: Disclosed herein is a compound having a structure: Therapeutic methods, compositions, and medicaments relating thereto are also disclosed.Type: GrantFiled: August 8, 2007Date of Patent: December 23, 2008Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Patent number: 7339066Abstract: The invention relates to intermediate compounds of the formula wherein R1 is H or a protecting group, R2 and R3 each independently represent H, methyl, or a leaving group, provided that at least one, but not both, of R2 and R3 is a leaving group. The intermediate compounds are useful for the synthesis of discodermolide, its derivatives, and related compounds.Type: GrantFiled: April 6, 2007Date of Patent: March 4, 2008Assignee: The Research Foundation of State University of New YorkInventors: Kathlyn Parker, Huanyan Cao
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Patent number: 7297807Abstract: The invention relates to intermediate compounds of the formula wherein R1 is H or a protecting group, R2 and R3 each independently represent H, methyl, or a leaving group, provided that at least one, but not both, of R2 and R3 is a leaving group. The intermediate compounds are useful for the synthesis of discodermolide, its derivatives, and related compounds.Type: GrantFiled: May 31, 2006Date of Patent: November 20, 2007Assignee: The Research Foundation of State University of New YorkInventors: Kathlyn Parker, Huanyan Cao
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Patent number: 7169766Abstract: A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.Type: GrantFiled: June 20, 2003Date of Patent: January 30, 2007Assignees: Idenix Pharmaceuticals, Inc., Universita Degli Studi di CagliariInventors: Jean-Pierre Sommadossi, Paulo LaColla
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Patent number: 7038039Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.Type: GrantFiled: February 13, 2001Date of Patent: May 2, 2006Assignee: Mitsui Chemicals, Inc.Inventors: Hironori Komatsu, Hirokazu Awano, Nobuyuki Fukazawa, Kiyoshi Ito, Ichirou Ikeda, Tadashi Araki, Takeshi Nakamura, Tamotsu Asano, Junya Fujiwara, Tomoyuki Ando, Katsutoshi Tsuchiya, Kyoko Maruyama, Hideki Umetani, Takahiro Yamauchi, Hitoki Miyake
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Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 6916831Abstract: Compounds are described having a structure according to Formula I or Formula II: wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O and S; m is from 1 to 3; n is from 1 to 5; R1 and R3 are each independently selected from the group consisting of H, hydroxy, lower alky, lower alkoxy, halo, amino, aminoalkyl, nitro, heteroaryl, —OC(?O)R6, —O(C?O)OR6; and —O(C?O)N(R6)2; and R2 is side chain such as an acetic acid side chain, where p is O to 4, R5 is hydroxy, alkoxy or amino, and R6 is H or lower alkyl, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer.Type: GrantFiled: February 24, 2003Date of Patent: July 12, 2005Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Yi Xia, Zheng-Yu Yang, Kenneth F. Bastow, Sheng-Chu Kuo
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Patent number: 6908722Abstract: A novel photoacid generator containing a structure of the following formula (I), wherein R is a monovalent organic group with a fluorine content of 50 wt % or less, a nitro group, a cyano group, or a hydrogen atom, and Z1 and Z2 are individually a fluorine atom or a linear or branched perfluoroalkyl group having 1-10 carbon atoms, is provided. When used in a chemically amplified radiation-sensitive resin composition, the photoacid generator exhibits high transparency, comparatively high combustibility, and no bioaccumulation, and produces an acid exhibiting high acidity, high boiling point, moderately short diffusion length in the resist coating, and low dependency to mask pattern density.Type: GrantFiled: June 28, 2002Date of Patent: June 21, 2005Assignee: JSR CorporationInventors: Satoshi Ebata, Eiji Yoneda, Tomoki Nagai, Tatsuya Toneri, Yong Wang, Haruo Iwasawa, Yukio Nishimura
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Publication number: 20040157247Abstract: The present invention is related to compounds comprising mannitol or glucitol derivatives which may be used to build up oligomeric compounds. The invention is further related to uses of these oligomeric compounds for hybridization and as probes. In addition, methods for the detection of nucleic acids are disclosed wherein the oligomeric compounds are used.Type: ApplicationFiled: December 5, 2003Publication date: August 12, 2004Applicant: ROCHE MOLECULAR SYSTEMS, INCInventors: Frank Bergmann, Herbert Von Der Eltz, Christoph Seidel, Kurt Weindel
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Publication number: 20040067872Abstract: Mono-fluorinated and di-fluorinated benzothiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as well as pharmaceutical compositions containing the same compounds.Type: ApplicationFiled: November 4, 2002Publication date: April 8, 2004Applicant: G.D. SEARLE, LLCInventors: Samuel J. Tremont, Kevin J. Koeller
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Publication number: 20040044059Abstract: A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.Type: ApplicationFiled: April 29, 2003Publication date: March 4, 2004Inventors: Kevin G. Pinney, Vani P. Mocharla, Zhi Chen, Charles M. Garner, Mallinath Hadimani, Raymond Kessler, James M. Dorsey, Klaus Edvardsen, David J. Chaplin, Joseph Prezioso, Anjan Ghatak, Usha Ghatak
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Publication number: 20030236406Abstract: Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.Type: ApplicationFiled: December 23, 2002Publication date: December 25, 2003Inventors: Kevin A. Babiak, Andrew Carpenter, Shine Chou, Pierre-Jean Colson, Payman Farid, Robert Hett, Christian H. Huber, Kevin J. Koeller, Jon P. Lawson, James Li, Eduardo K. Mar, Lawrence M. Miller, Vladislav Orlovski, James C. Peterson, Mark J. Pozzo, Claire A. Przybyla, Samuel J. Tremont, Jay S. Trivedi, Grace M. Wagner, Gerald A. Weisenburger, Benxin Zhi
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Publication number: 20030236410Abstract: A compound of formula (I) or pharmaceutically acceptable salt thereof wherein: 1Type: ApplicationFiled: June 2, 2003Publication date: December 25, 2003Applicant: SmithKline Beecham p.l.c.Inventors: Wai Ngor Chan, John Morris Evans, Geoffrey Stemp, Neil Upton, Robert Nicholas Willette
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Patent number: 6632807Abstract: This invention relates to an optically active benzothiepin derivative represented by the formula: wherein R represents a lower alkyl group; R1 and R2 independently represent a lower alkyl group, or may bind together to form a ring, which exhibits excellent osteogenesis-promoting action and is useful as a prophylactic or therapeutic drug for bone diseases.Type: GrantFiled: August 9, 2000Date of Patent: October 14, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
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Patent number: 6613945Abstract: The invention concerns a resolution method for a racemic mixture of aldehyde of formula (I). The aldehydes of formula I are useful in their enantiomeric form or their racemic form for preparing transition metal complexes useful as catalysts in hydroformylation reactions of olefins.Type: GrantFiled: August 7, 2001Date of Patent: September 2, 2003Assignee: Rhodia ChimieInventors: François Mercier, Stéphane Lelievre, François Mathey, Michel Spagnol
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Publication number: 20030109500Abstract: Treatment of warm-blooded animals having a tumor or non-malignant hypervascularation, by administering a sufficient amount of a cytotoxic agent formulated into a phosphate prodrug form having substrate specificity for microvessel phosphatases, so that microvessels are destroyed preferentially over other normal tissues, because the less cytotoxic prodrug form is converted to the highly cytotoxic dephosphorylated form.Type: ApplicationFiled: August 14, 2002Publication date: June 12, 2003Inventors: Ronald W. Pero, David Sherris, Kevin G. Pinney, Vani P. Mocharla, Zhi Chen
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Patent number: 6576772Abstract: Chiral ligands and transition metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The chiral ligands include (R,S,S,R)-DIOP*. The ruthenium complex reduces enamide to the corresponding amine with up to 99% enantioselectivity. The transition metal complexes of the chiral ligands are useful in asymmetric reactions such as asymmetric hydrogenation, hydride transfer, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, hydrocarboxylation, isomerization, allylic alkylation, cyclopropanation, Diels-Alder reaction, Heck reaction, isomerization, Aldol reaction, Michael addition and epoxidation reactions.Type: GrantFiled: November 10, 2000Date of Patent: June 10, 2003Assignee: The Penn State Research FoundationInventor: Xumu Zhang
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Patent number: 6541645Abstract: Complexes of organic ligands with a metal ion exhibit unique conformation and spectroscopic properties upon changes in oxidation state of the metal ion. The metal is a redox-active metal ion and may possess additional ligands bonded to it. The organic ligand has three “arms” that are linked together at a central atom; each arm contains atoms that may also coordinate to the metal ion. At least two of the arms possess chromophoric properties. At least one arm contains two different groups that may coordinate to the metal ion. In one oxidation state, a first atom binds to the metal. In a second oxidation state, a second atom binds to the metal. This change in coordination of the metal ion results in a rotation of one of the arms, which changes the orientation of another group, which inverses the orientation of the two chromophoric species with respect to one another.Type: GrantFiled: July 26, 2000Date of Patent: April 1, 2003Assignee: New York UniversityInventors: James W. Canary, Steffen Zahn
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Patent number: 6528627Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.Type: GrantFiled: November 28, 2000Date of Patent: March 4, 2003Assignee: NeoRx CorporationInventor: Sudhakar Kasina
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Publication number: 20030008849Abstract: Compounds of the formula: 1Type: ApplicationFiled: December 27, 2000Publication date: January 9, 2003Inventors: Jeremy I. Levin, James M. Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
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Publication number: 20030004322Abstract: One aspect of the present invention relates to differentially protected glycosyl phosphates. Another aspect of the present invention relates to the preparation of glycosyl phosphates from glycal precursors. In another aspect of the present invention, glycosyl phosphates are used as glycosyl donors in glycosylation reactions.Type: ApplicationFiled: November 1, 2001Publication date: January 2, 2003Inventors: Peter H. Seeberger, Obadiah J. Plante
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Publication number: 20020193314Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.Type: ApplicationFiled: May 7, 2002Publication date: December 19, 2002Inventors: Hironori Komatsu, Hirokazu Awano, Nobuyuki Fukazawa, Kiyoshi Ito, Ichirou Ikeda, Tadashi Araki, Takeshi Nakamura, Tamotsu Asano, Junya Fujiwara, Tomoyuki Ando, Katsutoshi Tsuchiya, Kyoko Maruyama, Hideki Umetani, Takahiro Yamauchi, Hitoki Miyake
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Patent number: 6479471Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.Type: GrantFiled: December 17, 1999Date of Patent: November 12, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Barbara S. Slusher, Kevin L. Tays, Keith M. Maclin
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Patent number: 6440899Abstract: Cyclohexenonedioxothiochromanoyl derivatives of the formula I where X is oxygen, sulfur, S═O, S(═O)2, CR4R5, C═O or C═NR6, the other substituents are as defined in the specification, and and agriculturally useful salts thereof; processes for preparing the cyclohexenonedioxotheiochromanoyl derivatives; compositions comprising them, and the use of these derivatives or of compositions comprising them for controling undesirable piants.Type: GrantFiled: October 30, 2000Date of Patent: August 27, 2002Assignee: BASF AktiengesellschaftInventors: Matthias Witschel, Klaus Langemann, Wolfgang von Deyn, Ulf Misslitz, Ernst Baumann, Stefan Engel, Guido Mayer, Ulf Neidlein, Oliver Wagner, Roland Götz, Martina Otten, Karl-Otto Westphalen, Helmut Walter
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Publication number: 20020086853Abstract: The present application describes novel cyclic sulfonyl derivatives of formula I: 1Type: ApplicationFiled: September 17, 2001Publication date: July 4, 2002Inventors: Robert J. Cherney, Bryan W. King
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Publication number: 20020077316Abstract: The present invention relates to novel sulfide and disulfide compounds, compositions comprising sulfide and disulfide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.Type: ApplicationFiled: October 11, 2001Publication date: June 20, 2002Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
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Publication number: 20020055653Abstract: The invention relates to the preparation and use as catalysts of diphosphines of the formula (I) 1Type: ApplicationFiled: September 7, 2001Publication date: May 9, 2002Inventors: Birgit Driessen-Holscher, Joachim Kralik, Inga Ritzkopf, Christian Steffens, Guido Giffels, Claus Dreisbach, Thomas Prinz, Walter Lange
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Patent number: 6376532Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and and methods for their use.Type: GrantFiled: January 25, 2001Date of Patent: April 23, 2002Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Darryl Hugh Steensma, Werner Tueckmantel, Gian Luca Araldi
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Patent number: 6346521Abstract: This invention relates to an optically active benzothiepin derivative represented by the formula: wherein R represents a lower alkyl group; R1 and R2 independently represent a lower alkyl group, or may bind together to form a ring, which exhibits excellent osteogenesis-promoting action and is useful as a prophylactic or therapeutic drug for bone diseases.Type: GrantFiled: December 28, 1995Date of Patent: February 12, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
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Publication number: 20020013476Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.Type: ApplicationFiled: April 9, 2001Publication date: January 31, 2002Applicant: G.D. Searle & Co.Inventors: Len F. Lee, Shyamal C. Banerjee, Horng-Chih Huang, Jinglin J. Li, Raymond E. Miller, David B. Reitz, Samuel J. Tremont
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Publication number: 20010020037Abstract: This invention provides compounds of Formula I having the structure 1Type: ApplicationFiled: April 20, 2001Publication date: September 6, 2001Applicant: American Home Products CorporationInventors: Jay E. Wrobel, Zenan Li
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Patent number: 6270695Abstract: Novel heterocyclic compounds which generate chemiluminescence on reaction with a phosphatase enzyme are provided as well as a process for their preparation and intermediates useful therein. The compounds comprise a nitrogen, oxygen or sulfur-containing heterocyclic ring system bearing an exocyclic carbon-carbon double bond. The double bond is further substituted at the distal carbon with a phosphate group and an oxygen or sulfur atom-containing group. Novel compositions further comprising a cationic aromatic compound (CAC) in addition to the heterocyclic phosphate compound are provided. The addition of the CAC in the composition greatly increases the production of chemiluminescence and provides improved detection sensitivity. Compositions further comprising an anionic surfactant and a non-ionic surfactant provide additional improvements in detection sensitivity.Type: GrantFiled: July 21, 1999Date of Patent: August 7, 2001Assignee: Lumigen, Inc.Inventors: Hashem Akhavan-Tafti, Zahra Arghavani, Renuka DeSilva
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Patent number: 6057316Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein B and D are each, independently, hydrogen, halogen, --CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms;R.sup.1 is hydrogen, alkyl of 1-6 carbon atoms, --CH(R.sup.2)W, --C(CH.sub.3).sub.2 CO.sub.2 R.sup.3, 5-thiazolidine-2,4-dione, --CH(R.sup.4)CH.sub.2 CO.sub.2 R.sup.3, --COR.sup.3, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, --CH.sub.2 (1H-imidazol-4-yl), --CH.sub.2 (3-1H-indolyl), --CH.sub.2 CH.sub.2 (1,3-dioxo-1,3-dihydro-isoindol-2-yl), --CH.sub.2 CH.sub.2 (1-oxo-1,3-dihydro-isoindol-2-yl), or --CH.sub.2 (3-pyridyl);W is --CO.sub.2 R.sup.3, --CONH.sub.2, --CONHOH, --CN, CONH(CH.sub.2).sub.2 CN, 5-tetrazole, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl;R.sup.Type: GrantFiled: May 10, 1999Date of Patent: May 2, 2000Assignee: American Home Products CorporationInventors: Jay E. Wrobel, Zenan Li