The Phosphorus Is Bonded Directly To The Chalcogen Patents (Class 546/25)
  • Patent number: 11926589
    Abstract: This invention relates to a process for the synthesis of a non-racemic cyclohexene compound of formula (I) by a Diels-Alder reaction of a compound of formula (II) with a compound of formula (III) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and Y have the meanings as defined in the description in the presence of a catalyst comprising at least one m-valent metal cation Mm+ wherein the metal M is selected from Scandium (Sc), Yttrium (Y), Lanthanum (La), Cerium (Ce), Praseodymium (Pr), Neodymium (Nd), Promethium (Pm), Samarium (Sm), Europium (Eu), Gadolinium 15 (Gd), Terbium (Tb), Dysprosium (Dy), Holmium (Ho), Erbium (Er), Thulium (Tm), Ytterbium (Yb), Lutetium (Lu), Gallium (Ga) and Indium (In), and m is an integer of 1, 2 or 3, and a chiral ligand of the formula (IV) wherein R10a, R10b, R10c, R10d, R10a?, R10b?, R10c?, R10d?, Z and Z? have the meanings as defined in the description.
    Type: Grant
    Filed: July 6, 2020
    Date of Patent: March 12, 2024
    Assignees: BASF CORPORATION, CALIFORNIA INSTITUTE OF TECHNOLOGY
    Inventors: Sarah Reisman, Michael Rombola, Carolyn L. Ladd, Martin John McLaughlin, Stephan Zuend, Roland Goetz
  • Publication number: 20150141557
    Abstract: A stabilizer including a first component and a second component. The first component is a compound represented by the formula (1). The second component is a compound represented by the formula (2).
    Type: Application
    Filed: January 28, 2014
    Publication date: May 21, 2015
    Applicant: DOUBLE BOND CHEMICAL IND., CO., LTD.
    Inventors: Chiung-Ta Chen, Chih-Wei Lin, Ming-Yang Chien, En-Ching Wang, Chien-Liang Liu
  • Patent number: 8999526
    Abstract: An organic photoelectric device may include an anode and a cathode configured to face each other, and an active layer between the anode and cathode, wherein the active layer includes a quinacridone derivative and a thiophene derivative having a cyanovinyl group.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: April 7, 2015
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Kwang Hee Lee, Kyu Sik Kim, Kyung Bae Park, Dong-Seok Leem, Seon Jeong Lim
  • Publication number: 20150057220
    Abstract: Fused aromatic phosphonates of structural formula I are precursors to inhibitors of protein tyrosine phosphatase-1B (PTP-1B). The compounds of the present invention are therefore useful for the treatment in a mammal of a disorder, condition, or disease responsive to inhibition of protein tyrosine phosphatase-1B, including Type 2 diabetes, insulin resistance, a lipid disorder, obesity, Metabolic Syndrome, and cancer.
    Type: Application
    Filed: April 16, 2013
    Publication date: February 26, 2015
    Inventors: Michel Therien, Yves Leblanc, Yongxin Han
  • Publication number: 20150050659
    Abstract: Protected fluorescent reagent compounds and their methods of synthesis are provided. The compounds are useful in various fluorescence-based analytical methods, including the analysis of highly multiplexed optical reactions in large numbers at high densities, such as single molecule real time nucleic acid sequencing reactions. The compounds contain fluorescent dye elements, that allow the compounds to be detected with high sensitivity at desirable wavelengths, binding elements, that allow the compounds to be recognized specifically by target biomolecules, and protective shield elements, that decrease undesirable contacts between the fluorescent dye elements and the bound target biomolecules and that therefore decrease photodamage of the bound target biomolecules by the fluorescent dye elements.
    Type: Application
    Filed: August 5, 2014
    Publication date: February 19, 2015
    Inventors: Lubomir SEBO, Jeremiah HANES, Gene SHEN, Louis BROGLEY, Stephen YUE, Frank ZHENG, Yuri LAPIN, John LYLE, Honey OSUNA, Andrei FEDOROV
  • Publication number: 20140336137
    Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
    Type: Application
    Filed: July 28, 2014
    Publication date: November 13, 2014
    Inventors: Lisa Marie Frost, Stephen Martin Courtney, Frederick Arthur Brookfield, Vincent Jacob Kalish
  • Publication number: 20140309413
    Abstract: The present invention relates to the novel diastereoselective syntheses for generating phosphorothioate compounds. Examples include nucleoside phosphorothioate analogs that are useful in treating diseases and/or conditions such as viral infections.
    Type: Application
    Filed: March 10, 2014
    Publication date: October 16, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Peter Jamison Rose, Young Chun Jung, Cavan McKeon Bligh, Shereen Ibrahim, Luigi Anzalone, David B. Miller, JR., John Gregg Van Alsten, Timothy Thomas Curran
  • Publication number: 20130296569
    Abstract: The invention relates to a process to prepare pharmacologically active phosphoric acid mono-(1-{4-[(S)-5-(acetylamino-methyl)-2-oxo-oxazolidin-3-yl]-2,6-difluoro phenyl}-4-methoxy methyl-piperidin-4-yl)ester.
    Type: Application
    Filed: February 3, 2011
    Publication date: November 7, 2013
    Inventors: Vijaykumar Jagdishwar Patil, Rajkumar Vishwanath Hangarge, Burhanuddin Munshi Zaki Ahmed, Loganathan Velupillai, Bharat Kalidas Trivedi
  • Patent number: 8436153
    Abstract: The invention provides a novel class of cyanine dyes that are functionalized with a linker moiety that facilitates their conjugation to other species. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.
    Type: Grant
    Filed: January 5, 2010
    Date of Patent: May 7, 2013
    Assignee: Biosearch Technologies, Inc.
    Inventors: Tim Carter, Mark Reddington
  • Publication number: 20130045951
    Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
    Type: Application
    Filed: October 18, 2012
    Publication date: February 21, 2013
    Applicant: CARDIOXYL PHARMACEUTICALS, INC.
    Inventor: CARDIOXYL PHARMACEUTICALS, INC.
  • Publication number: 20120015908
    Abstract: A compound of Formula I is disclosed as follows: or a pharmaceutically acceptable salt, prodrug, solvate, or metabolite thereof, wherein R is hydrogen, P(?O)(OH)2, P(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, P(?O)(OH)(OM), P(?O)(OM)2, P?O(O2M), S(?O)(OH)2, S(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, S(?O)(OH)(OM), S(?O)(OM)2; M is a monovalent or divalent metal ion, or alkylammonium ion; W is (C6-C20)aryl, (C6-C20)heteroaryl, (C1-C18)alkyl(C6-C20)aryl, (C1-C18)alkyl(C6-C20)heteroaryl, hydroxy(C6-C20)aryl, hydroxy(C6-C20)heteroaryl, (C1-C18)alkoxy(C6-C20)aryl, (C1-C18)alkoxy(C6-C20)heteroaryl, (C1-C18)alkylenedioxy(C6-C20)aryl, (C1-C18)alkylenedioxy(C6-C20)heteroaryl, halo(C6-C20)aryl, halo(C6-C20)heteroaryl, (C1-C18)alkylamino(C6-C20)aryl, (C1-C18)alkylamino(C6-C20)heteroaryl, (C1-C18)cycloalkylamino(C6-C20)aryl, or (C1-C18)cycloalkylamino(C6-C20)heteroaryl, and their OR8 substutes; R5 is (C1-C18alkoxy, hydrogen, hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or OR8, or R5 and R6 are (C1-C18)dioxy provided that R7 i
    Type: Application
    Filed: July 13, 2011
    Publication date: January 19, 2012
    Applicant: Efficient Pharma Management Corporate
    Inventors: Sheng-Chu Kuo, Kuo-Hsiung Lee, Li-Jiau Huang, Li-Chen Chou, Tian-Shung Wu, Tzong-Der Way, Jing-Gung Chung, Jai-Sing Yang, Chi-Hung Huang, Meng-Tung Tsai
  • Publication number: 20110054165
    Abstract: 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: Application
    Filed: November 8, 2010
    Publication date: March 3, 2011
    Applicant: BIOSEARCH TECHNOLOGIES, INC.
    Inventors: MARK REDDINGTON, MATT LYTTLE
  • Publication number: 20110046052
    Abstract: This invention is a method of using a class of excipients for protein formulation to reduce and/or eliminate protein aggregation in solutions or solids. This class of compounds contains carbonyl group(s) to form Schiff base(s) with amino groups of proteins and also contains moieties to keep protein molecules spatially separated. This method has never been disclosed anywhere in the literature.
    Type: Application
    Filed: November 17, 2008
    Publication date: February 24, 2011
    Inventor: Guohan Yang
  • Publication number: 20100317625
    Abstract: 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: Application
    Filed: May 21, 2007
    Publication date: December 16, 2010
    Inventors: 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
  • Publication number: 20100279983
    Abstract: 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: Application
    Filed: May 21, 2007
    Publication date: November 4, 2010
    Inventors: 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
  • Publication number: 20100120721
    Abstract: The present invention relates to oxazolidinones of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof. The invention also relates to processes for the preparation of the compound of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof, and to pharmaceutical compositions containing the compounds of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof and to methods for treating or preventing microbial infections using the compounds of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof.
    Type: Application
    Filed: September 22, 2007
    Publication date: May 13, 2010
    Applicant: WOCKHARDT RESEARCH CENTRE
    Inventors: Vijaykumar Jadgishwar Patil, Mahesh Vithalbhai Patel, Bharat Kalidas Trivedi, Deepak Vijaykumar Dekhane, Mohammad Usman Shaikh, Yati Chugh, Rajesh Prabhakar Chavan, Mohammad Alam Jafri
  • Patent number: 7705150
    Abstract: The invention provides a novel class of cyanine dyes that are functionalized with a linker moiety that facilitates their conjugation to other species. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.
    Type: Grant
    Filed: February 4, 2005
    Date of Patent: April 27, 2010
    Assignee: Biosearch Technologies, Inc.
    Inventors: Tim Carter, Mark Reddington
  • Patent number: 7514556
    Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: July 30, 2007
    Date of Patent: April 7, 2009
    Assignee: Methylgene Inc.
    Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
  • Publication number: 20090023926
    Abstract: The present invention provides a compound of the formula: (IIa); having a reactive functional group M, capable of reacting with a biopolymer, BP, having at least one group capable of reacting with M to form a covalent linkage, to provide a biopolymer derivative of the formula: (IIIa). The biopolymer derivatives of the invention have enhanced ionisability with respect to free 10 biopolymer (Bp) enabling improved analysis of the biopolymer using mass spectrometry. The invention further provides specific examples of compounds formula (IIa), e.g. compounds of formula: (IIa-2a) and (IIa-58a).
    Type: Application
    Filed: September 22, 2005
    Publication date: January 22, 2009
    Inventors: Edwin Mellor Southern, Vladimir Korshun, Mikhail Sergeevich Shchepinov
  • Patent number: 7442732
    Abstract: Disclosed herein are compounds of the structure: wherein R1, R2, R3, R4, R5, and R6 are independently selected alkyl groups, provided that R1 is different from R2. The compounds are useful as stabilizers for thermoplastic resins.
    Type: Grant
    Filed: March 29, 2005
    Date of Patent: October 28, 2008
    Assignee: Crompton Corporation
    Inventors: Michael E. Gelbin, Carloss L. Gray
  • Publication number: 20080214811
    Abstract: 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: Application
    Filed: February 25, 2008
    Publication date: September 4, 2008
    Applicant: Biosearch Technologies, Inc.
    Inventors: Mark Reddington, Matt Lyttle
  • Patent number: 7358361
    Abstract: Bisphosphonate compounds and related methods of making and using are disclosed, including pyridinium-1-yl, quinolinium-1-yl, and related compounds. The activity of compounds is disclosed in the context of functional assays such as Leishmania major farnesyl diphosphate synthase (FPPS) inhibition, Dictyostelium discoideum growth inhibition, human gamma delta T cell activation, and bone resorption. The applicability of bisphosphonate compounds in the context of parasitic infections, for example against trypanosomes, is disclosed. Further potential applications of the invention are disclosed regarding the treatment of one or more conditions such as bone resorption disorders, cancer, bone pain, infectious diseases, and in immunotherapy.
    Type: Grant
    Filed: October 7, 2005
    Date of Patent: April 15, 2008
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: John M. Sanders, Yongcheng Song, Julian M. W. Chan, Eric Oldfield, Yonghui Zhang
  • Patent number: 7354771
    Abstract: The absolute configuration of a chiral compound is determined by (i) coordinating the chiral compound to a metalloporphyrin having a carbon chain-crosslinked porphyrin dimer structure in which one of the two porphyrin rings has at least one ethyl or substituent bulkier than ethyl at at least one of the second peripheral carbon atoms from the carbon atom at the carbon chain crosslink site, and (ii) analyzing the resultant coordination compound by circular dichroism spectrophotometry to determine the absolute configuration of the asymmetric carbon based on the sign of the Cotton effect. The chiral compound has an asymmetric carbon bonded to a basic group capable of coordinating to the metal of the other porphyrin ring of the metalloporphyrin dimer or an asymmetric carbon atom adjacent to the carbon atom bonded to the basic group.
    Type: Grant
    Filed: December 4, 2000
    Date of Patent: April 8, 2008
    Assignee: Japan Science and Technology Corporation
    Inventors: Yoshihisa Inoue, Victor Borovkov, Juha Lintuluoto
  • Patent number: 7030103
    Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: October 8, 2002
    Date of Patent: April 18, 2006
    Assignee: Methylgene, Inc.
    Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
  • Patent number: 6921756
    Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: April 8, 2003
    Date of Patent: July 26, 2005
    Assignee: MethylGene, Inc.
    Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
  • Patent number: 6884791
    Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: April 26, 2005
    Assignee: MethylGene, Inc.
    Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
  • Patent number: 6818770
    Abstract: Phosphinines of formula (I) can be combined with metal salts to prepare hydroformylation catalysts. The phosphinine complexes have two phosphorus centers that may be substituted with a variety of hetero atoms or alkyl substituents to modify the ligand characteristics of the phosphinine. Phosphinine metal complexes are employed under normal hydroformylation reaction conditions. The preparatory routes to the phosphinine ligands of formula (I) allow for their convenient synthesis.
    Type: Grant
    Filed: November 21, 2001
    Date of Patent: November 16, 2004
    Assignee: OXENO Olefinchemie GmbH
    Inventors: Detlef Selent, Armin Börner, Renat Kadyrov, Cornelia Borgmann, Dieter Hess, Klaus-Diether Wiese, Dirk Röttger
  • Patent number: 6660860
    Abstract: The invention relates to a process for the selective oxidation of alcohols to ketones or to aldehydes by means of an alkali hypohalite under alkaline conditions, which comprises carrying out the oxidation in the presence of a heterogeneous oxidation catalyst that is insoluble in the reaction medium and is selected from the group comprising the compounds of formula (I) wherein n is a number from 3 to 3000; or a 4-oxy-2,2,6,6-tetramethylpiperidin-1-oxyl that is 4-oxy-bound to a Merrifield polymer. The invention relates also to the compounds of formulae (II) and (III) and to the use of the above-mentioned oxidation catalysts for the oxidation of alcohols.
    Type: Grant
    Filed: June 7, 2002
    Date of Patent: December 9, 2003
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Reinhard Sommerlade, Hansjörg Grützmacher, Souâd Boulmaâz
  • Publication number: 20030203877
    Abstract: The present invention provides novel compounds, pharmaceutical compositions, methods, and kits for inhibiting the conversion of Amadori compounds to post Amadori advanced glycation endproducts, and for treating and preventing chronic tissue damage and diabetic complication
    Type: Application
    Filed: March 13, 2003
    Publication date: October 30, 2003
    Applicant: Kansas University Medical Center
    Inventors: Raja Khalifah, Aaron Ashley Booth
  • Patent number: 6562974
    Abstract: The present invention relates to a novel process for making geminal bisphosphonates. The process provides for bisphosphorylation using phosphorus trihalide, phosphorous acid as a reactant/solvent, and a base as an acid acceptor/solvent.
    Type: Grant
    Filed: January 29, 2001
    Date of Patent: May 13, 2003
    Assignee: The Procter & Gamble Company
    Inventors: Frederick Dana Cazer, William Douglas Cramer, Dennis Michael Billings, Gregory Eugene Parry
  • Publication number: 20030004322
    Abstract: 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: Application
    Filed: November 1, 2001
    Publication date: January 2, 2003
    Inventors: Peter H. Seeberger, Obadiah J. Plante
  • Patent number: 6472406
    Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: July 5, 2000
    Date of Patent: October 29, 2002
    Assignee: MethylGene, Inc.
    Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
  • Patent number: 6211370
    Abstract: The present invention relates to a process for stereoselective cycloaddition reactions which generally comprises a cycloaddition reaction between a pair of substrates, each either chiral or prochiral, that contain reactive &pgr;-systems, in the presence of a non-racemic chiral catalyst, to produce a stereoisomerically enriched product. The present invention also relates to novel asymmetric catalyst complexes comprising a metal and an asymmetric tridentate ligand.
    Type: Grant
    Filed: February 23, 1999
    Date of Patent: April 3, 2001
    Assignee: Harvard University
    Inventors: Eric N. Jacobsen, Scott E. Schaus, Alexander G. Dossetter, Timothy F. Jamison
  • Patent number: 6187913
    Abstract: A double- or single-stranded oligonucleotide comprising one or more respectively inter- or intra-oligonucleotide covalent cross-linkages, wherein the or each covalent linkage consists of an amide bond between a primary amine group of one strand and a carboxyl group of the other strand or the same strand, respectively, said primary amine group being directly substituted in the 2′ position of the strand nucleotide monosaccharide ring, and said carboxyl group being carried by an aliphatic spacer group substituted on a nucleotide or nucleotide analog of the other strand or the same strand, respectively. A method for preparing such oligonucleotides, and nucleotide or non-nucleotide synthons useful for preparing an oligonucleotide of the above kind, are also disclosed.
    Type: Grant
    Filed: December 23, 1997
    Date of Patent: February 13, 2001
    Assignee: Genset
    Inventors: Marta Blumenfeld, Irena Merenkova
  • Patent number: 6172050
    Abstract: Phospholipid derivatives of Formula X: wherein A is the ring system in which R is a linear or branched alkyl radical having 10 to 24 carbon atoms which may contain one or more double or triple bonds; R1 and R2 are independently hydrogen or linear alkyl radicals having 1 to 3 carbon atoms; y is 0, 1, 2 or 3; m and n are independently 0 or in an integer, with the proviso that m+n is between 2 and 8; or A is a tropanio or quinuclidinio ring system, which is linked via a carbon-carbon bond and is optionally substituted by one or more methyl groups; processes for the preparation of the derivatives, and methods for treating tumors therewith.
    Type: Grant
    Filed: August 4, 1997
    Date of Patent: January 9, 2001
    Assignee: Asta Medica Aktiengesellschaft
    Inventors: Gerhard Nössner, Bernhard Kutscher, J{umlaut over (u)}rgen Engel, Wolfgang Schumacher, Jurij Stekar, Peter Hilgard
  • Patent number: 6130340
    Abstract: The present invention relates to a process for stereoselective cycloaddition reactions which generally comprises a cycloaddition reaction between a pair of chiral or prochiral substrates that contain reactive .pi.-systems, in the present of a non-racemic chiral catalyst, to produce a stereoisomerically enriched product.
    Type: Grant
    Filed: January 13, 1998
    Date of Patent: October 10, 2000
    Assignee: President and Fellows of Harvard College
    Inventors: Eric N. Jacobsen, Scott E. Schaus
  • Patent number: 6054444
    Abstract: The present invention relates to phosphonic acid derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.
    Type: Grant
    Filed: April 24, 1997
    Date of Patent: April 25, 2000
    Assignee: Guilford Pharmaceuticals Inc.
    Inventors: Paul F. Jackson, Keith M. Maclin, Kevin L. Tays, Barbara S. Slusher
  • Patent number: 6046334
    Abstract: The present application is directed to a heterocyclic compound having the structural formula: ##STR1## where R is hydrogen, C.sub.1 -C.sub.2 alkyl, cyclohexyl, phenyl, benzyl, phenylethyl, 2-hydroxyethyl, 3-hydroxypropyl, carboxymethyl, 4-(carboxylamine)butyl or diphenylmethyl; M is hydrogen, sodium, potassium, magnesium or ammonium; and x is 1 or 2. The heterocyclic compound having the aforementioned structural formula finds application in many pharmaceutical applications.
    Type: Grant
    Filed: May 13, 1998
    Date of Patent: April 4, 2000
    Assignee: Perstorp AB
    Inventors: Lars Persson, Nicola Rehnberg
  • Patent number: 5986098
    Abstract: A compound of formula (I) to (III) ##STR1## in which the symbols R to R.sub.6 are organic radicals. These compounds can be used as intermediates in the production of a phosphite-HALS product.
    Type: Grant
    Filed: July 28, 1997
    Date of Patent: November 16, 1999
    Assignee: Clariant Finance (BVI) Limited
    Inventor: Peter Staniek
  • Patent number: 5958969
    Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides benzothiophene compounds, intermediates, formulations, and methods.
    Type: Grant
    Filed: September 3, 1997
    Date of Patent: September 28, 1999
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, Michael John Martin, Ken Matsumoto
  • Patent number: 5925758
    Abstract: The invention relates to novel compounds of the formula I in which the general symbols are as defined in claim 1, as stabilizers for organic materials against oxidative, thermal or light-induced degradation.
    Type: Grant
    Filed: April 5, 1995
    Date of Patent: July 20, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Rita Pitteloud
  • Patent number: 5910600
    Abstract: A bisphosphite compound of the following formula (A): ##STR1## wherein --Ar--Ar-- is a bisarylene group represented by any one of the formulae (A-I) to (A-III) defined in the specification, and each of Z.sub.1 to Z.sub.4 is a C.sub.4-20 aromatic or heteroaromatic group which may have a substituent, wherein each of substituents on carbon atoms of an aromatic ring adjacent to the carbon atom bonded to the oxygen atom in each of Z.sub.1 to Z.sub.4, is a C.sub.0-2 group, and each pair of Z.sub.1 and Z.sub.2, and Z.sub.3 and Z.sub.4, are not bonded to each other.
    Type: Grant
    Filed: April 28, 1997
    Date of Patent: June 8, 1999
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Hisao Urata, Hiroaki Itagaki, Eitaro Takahashi, Yasuhiro Wada, Yoshiyuki Tanaka, Yasukazu Ogino
  • Patent number: 5795982
    Abstract: A compound having a formula selected from ##STR1## wherein A and B are selected from the group consisting of ##STR2## K and K' are selected from the group consisting of ##STR3## n is 2 or 3 and R.sub.1 is an ether or ester residue.
    Type: Grant
    Filed: September 13, 1996
    Date of Patent: August 18, 1998
    Assignee: Roussel Uclaf
    Inventors: Catherine Geurts, Michel Vivat
  • Patent number: 5726185
    Abstract: Acetic acid derivatives of the formula ##STR1## wherein L, M, T and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion, and are manufactured by cleaving protecting groups in the corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.
    Type: Grant
    Filed: December 1, 1994
    Date of Patent: March 10, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Paul Hadvary, Marianne Hurzeler Muller, Marcel Muller, Beat Steiner, Thomas Weller
  • Patent number: 5677432
    Abstract: A compound useful for forming immunoconjugates used in the detection of organophosphate pesticides is provided. The compound has the formula ##STR1## wherein X is selected from the group consisting of R--O--, R--S-- and R--NH--, where R is an optionally substituted aromatic or heterocyclic group, or an optionally substituted alkyl or alkenyl group;Y is O or S;R.sup.1 is H or alkyl; andR.sup.2 is a group of the formula --(CH.sub.2).sub.n -- wherein n is an integer of from 1 to 10, or branched chain alkylene, or a group of the formula R.sup.3 --O--R.sup.4 wherein R.sup.3 and R.sup.4 are both or straight or branched chain alkylene;or a salt or ester thereof.
    Type: Grant
    Filed: August 19, 1994
    Date of Patent: October 14, 1997
    Assignee: The Horticulture and Food Research Institute of New Zealand Limited
    Inventors: William Thomas Jones, Hans Wynberg, Wolter Ten Hoeve
  • Patent number: 5654430
    Abstract: The invention relates to novel oligomeric compounds of the formula I ##STR1## in which L is a group of the formula ##STR2## where the oxygen in the group L is in each case bonded to the phosphorus in the recurring structural units and the radical R.sub.2 or the carbon in the 4-position of the piperidinyl ring in the group L is in each case bonded to the oxygen in the recurring structural units; and the general symbols are as defined in claim 1, as stabilizers for organic materials against oxidative, thermal or light-induced degradation.
    Type: Grant
    Filed: April 5, 1995
    Date of Patent: August 5, 1997
    Assignee: Ciba-Geigy Corporation
    Inventor: Rita Pitteloud
  • Patent number: 5637747
    Abstract: A compound of the formula ##STR1##
    Type: Grant
    Filed: September 22, 1992
    Date of Patent: June 10, 1997
  • Patent number: 5623080
    Abstract: A compound of the formula (I) or (II): ##STR1## where R.sup.1, R.sup.2, R.sup.5 and R.sup.6 are the same or different and represent a hydrogen atom or a halogen atom and R.sup.1 and R.sup.2 may combine to form a ring; R.sup.3, and R.sup.4 are the same or different and represent a hydrogen atom, a halogen atom, a benzoyl group, a group of the formula --L(CH.sub.2).sub.n R.sup.8 where n is 1 to 8, R.sup.8 is a hydrogen, hydroxy, amino, dialkylamino, --COR.sup.16 or --COOR.sup.14 where R.sup.16 is a hydrogen, chlorine, COCl, C.sub.1 -C.sub.8 alkyl, --NR.sub.2 or aryl and R.sup.14 is a hydrogen, C.sub.1 -C.sub.8 alkyl, aryl, COR, 2,4-dinitrophenyl, N-imido or --NR.sub.2 and L is a direct bond or C.dbd.O; W is .dbd.O; W.sup.1 is hydrogen or --OR.sup.9, where R.sup.9 is hydrogen, C.sub.1 -C.sub.8 alkyl, acyl or a group of the formula --(CH.sub.2).sub.n R.sup.10 where n is 1 to 8 and R.sup.10 is amino, dialkylamino, hydroxy, acryloyl or methacryloyl; Y is oxygen, sulfur, selenium, tellurium, C.dbd.O, or >N--R.
    Type: Grant
    Filed: February 15, 1995
    Date of Patent: April 22, 1997
    Assignee: Spectra Group Limited, Inc.
    Inventors: Douglas C. Neckers, Jianmin Shi
  • Patent number: 5616636
    Abstract: A composition comprising:a) a compound containing a phosphite or phosphonite group and at least one 2,2,6,6-tetraalkylpiperidinyl group, andb) a polyolefin which has been produced in the presence of a catalyst which is eitheri) a supported Zeigler catalyst orii) a metallocene catalyst,from which polyolefin the catalyst has not been removed.
    Type: Grant
    Filed: February 27, 1995
    Date of Patent: April 1, 1997
    Assignee: Sandoz Ltd.
    Inventors: Lajos Avar, Peter Staniek, Klaus Stoll, Wolf D. Habicher, Uwe Hahner
  • Patent number: 5468742
    Abstract: The invention relates to new 8-vinyl- and 8-ethinylquinolonecarboxylic acids, process for their preparation, and antibacterial agents and feed additives containing them.
    Type: Grant
    Filed: November 1, 1993
    Date of Patent: November 21, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Uwe Petersen, Thomas Himmler, Thomas Schenke, Andreas Krebs, Klaus Grohe, Klaus-Dieter Bremm, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler