Phosphorus Attached Indirectly To Amino Nitrogen By Nonionic Bonding Patents (Class 564/15)
  • Publication number: 20040147785
    Abstract: This invention relates to processes for making phosphorus compounds R2P—X—PR2, R2P-M, R2P-L and R3P, and the novel cation R2P+(L)-X—P+(L)R2, where R represents an optionally substituted hydrocarbyl group, X represents a bridging group, L represents a leaving group and M represents an alkali metal atom. The invention relates further to a process for making a compound R2P-L from a compound R—H via a new process for making the compound R—Li followed by its reaction with a compound Hal2P-L. The compound R2P—X—PR2 is a ligand suitable for making catalysts for copolymerizing carbon monoxide and a olefinically unsaturated compound.
    Type: Application
    Filed: January 15, 2004
    Publication date: July 29, 2004
    Inventors: Roelof Van Ginkel, Alexander Van Der Made, Jan De With, Wolf Eilenberg, Ursula Eilenberg-Robben
  • Publication number: 20040110979
    Abstract: The invention relates to a process for preparing diphosphines of the formula
    Type: Application
    Filed: September 25, 2003
    Publication date: June 10, 2004
    Inventors: Ralf Jackstell, Holger Klein, Matthias Beller, Klaus-Diether Wiese, Cornelia Borgmann
  • Publication number: 20040102649
    Abstract: The invention concerns a water soluble compound of formula (a) wherein: A represents naphthyl or phenyl; and Ar1 and Ar2 independently represent a saturated or aromatic carbocyclic group; Xa, Xb are independently selected among an amino group, an ammonium group and an amino group modified by a linear polyoxyalkylene chain, provided that at least one of Xa and Xb represents ammonium or modified amino.
    Type: Application
    Filed: April 23, 2003
    Publication date: May 27, 2004
    Inventors: Christine Saluzzo, Thierry Lamouille, Marc Lemaire, Robert Ter Halle
  • Publication number: 20040068131
    Abstract: The invention relates to novel phosphane ligands of formula (Ia) and (Ib): (adamantyl)nP(alkyl)m(1a); (adamantyl)o(Alkyl)qP (alkylen′)P(adamantyl)r(alkyl)s (1b), wherein adamantyl represents an adamantyl radical (IIa, IIb) bonded to the phosphorous atom in position 1 or 2. The invention also relates to the production and use of the above-mentioned ligands in the presence of transitional metal compounds of the 8th. Subgroup of PSE for catalytic reactions, particularly for the refining of halogen aromatics for producing aryl olefins, dienes, diarylene, benzoic acid and acrylic acid derivatives, aryl alkanes and also amines.
    Type: Application
    Filed: July 25, 2003
    Publication date: April 8, 2004
    Inventors: Matthias Beller, Andreas Ehrentraut, Wilhelm Hubert Ehrentraut, Theresia Elisabeth Ehrentraut, Christa Fuhrmann, Alexander Zapf
  • Publication number: 20040048834
    Abstract: New spisulosine derivatives of use in treating tumors are of the formula (I) wherein: each X is the same or different, and represents H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, CN, halogen, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, or two groups X may together form ═O; Y is NR1, OR1, PR1, SR1, or halogen, wherein the number of substituents R1 is selected to suit the valency and each R1 is independently selected of H, OH, C(═O)R′, P(═O)R′R″, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, and wherein the dotted line indicates an optional double bond; each Z is the same different, and represents H, OH,
    Type: Application
    Filed: August 18, 2003
    Publication date: March 11, 2004
    Inventors: Jose Luis Acena, Javier Adrjo, Carmen Cuevas, Pilar Gallego, Ignacio Manzanares, Simon Munt, Ignacio Rodriguez
  • Patent number: 6699851
    Abstract: Novel amides of polyunsaturated fatty acids with cysteamine-S-phosphate have been synthesized. Combinations of the all-trans-retinoic acid and/or amides of the 13-cis-retinoic acid with O-phospho-L-tyrosine, and N-docosahexaenoyl-cysteamine-S-phosphate, N-eicosapentaenoyl-cysteamine-S-phosphatee, N-arachidonoyl-cysteamine-S-phosphate, N-&agr;-linolenoyl-cysteamine-S-phosphate, and N-&ggr;-linolenoyl-cysteamine-S-phosphate and their analogues N-docosahexaenoyl-O-phospho-2-aminoethanol, N-eicosapentaenoyl-O-phospho-2-aminoethanol, N-arachidonoyl-O-phospho-2-aminoethanol, N-&agr;-linolenoyl-O-phospho-2-aminoethanol, N-&ggr;-linolenoyl-O-phospho-2-aminoethanol in different compositions exhibit a marked cell-growth inhibiting effect and display anti-tumor activity.
    Type: Grant
    Filed: May 6, 2003
    Date of Patent: March 2, 2004
    Assignee: Ardenia Investments, Ltd.
    Inventor: Oleg Strelchenok
  • Patent number: 6693210
    Abstract: Provided are a novel triphenyl phosphine derivative synthesized from a triphenylphosphine and a hydroxy-containing lactone; a palladium and a nickel complexes comprising the derivative as a ligand; and a process for preparing a biaryl derivative using the complex as a catalyst. A product can be easily separated from a catalyst or a phosphorus compound, and biaryl derivative can be synthesized in a higher yield, by using the complex of the present invention as a catalyst.
    Type: Grant
    Filed: September 13, 2002
    Date of Patent: February 17, 2004
    Assignee: Mitsubishi Rayon Co., Ltd.
    Inventor: Norio Miyaura
  • Publication number: 20040029913
    Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.
    Type: Application
    Filed: February 24, 2003
    Publication date: February 12, 2004
    Inventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka
  • Publication number: 20040014975
    Abstract: The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor.
    Type: Application
    Filed: October 22, 2002
    Publication date: January 22, 2004
    Inventors: James T. Dalton, Duane D. Miller, Yali He, Donghua Yin
  • Publication number: 20030225040
    Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.
    Type: Application
    Filed: October 16, 2002
    Publication date: December 4, 2003
    Inventors: James T. Dalton, Duane D. Miller, Yali He, Donghua Yin
  • Patent number: 6657081
    Abstract: The invention relates to new calixarenes according to the formula: wherein: R1 is an alkyl or aryl group, or a hydrogen atom, R2 and R3, which may be identical or different, are alkyl or aryl groups, n is an integer ranging from 2 to 8, and p is an integer ranging from 4 to 8. Said calixarenes may be used to extract actinides and lanthanides from aqueous solutions.
    Type: Grant
    Filed: May 29, 2001
    Date of Patent: December 2, 2003
    Assignee: Commissariat a l'Energie Atomique
    Inventors: Jean-François Dozol, Alejandro Garcia Carrera, Volker Bohmer, Susan E. Matthews
  • Patent number: 6646079
    Abstract: For the preparation of a multimodal polymer at least one monomer is subjected to free radical polymerization in the presence of several alkoxyamines comprising the sequence of formula: in which RL is a monovalent radical exhibiting a molar mass of greater than 15, A represents the core of the alkoxyamine and n is a non-zero integer, the alkoxyamines exhibiting different values of n.
    Type: Grant
    Filed: April 9, 2001
    Date of Patent: November 11, 2003
    Assignee: Atofina
    Inventors: Olivier Guerret, Sophie Robin, Yves Gnanou
  • Patent number: 6630501
    Abstract: The invention relates to pseudo-peptides according to the formula: wherein R1 is a group inhibiting an amine function, or an amino acid residue or peptide with an inhibited terminal amino function, R2 represents the lateral chain of a natural or non-natural amino acid, R3 represents: 1) the lateral chain of a natural amino acid except for Gly and Ala, not substituted or substituted by an aryl group, 2) an aralkyl group, or 3) an alkyl group comprising at least 3 carbon atoms, and R4 represents a lateral chain of natural or non-natural amino acid. They are useful as matrix zinc metalloprotease inhibitors, particularly in the treatment of cancer.
    Type: Grant
    Filed: March 25, 2002
    Date of Patent: October 7, 2003
    Assignees: Commissariat a l'energie Atomique, Institut National de la Recherche Medical, Centre National de la Recherche Scientifique
    Inventors: Vincent Dive, Philippe Cuniasse, Marie-Christine Rio, Paul Basset, Athanasios Yotakis, Fabrice Beau, Stamania Vassiliou
  • Patent number: 6613848
    Abstract: A hardener for an epoxy resin comprises a phenolic, thiophenolic, aminophenyl, tris-phenolic, tris-thiophenolic, tris-aminophenyl, tetrakis-phenolic, tetrakis-thiophenolic, or tetrakis-aminophenyl compounds; or phenol-formaldehyde or phenol-formaldehyde/melamine-formaldehyde resins wherein the phenyl rings are substituted with at least one of the structures wherein R1 and R2 independently are H, C1-C18 alkyl, C6-C18 aryl, C6-C18 substituted aryl, C6-C18 aryl methylene, or C6-C18 substituted aryl methylene; X is O, S or NH and Ar is wherein R is C1-C4 alkyl and n=0-5.
    Type: Grant
    Filed: May 16, 2000
    Date of Patent: September 2, 2003
    Assignee: National Science Council
    Inventors: Chun-Shan Wang, Jeng-Yueh Shieh
  • Publication number: 20030120122
    Abstract: Compounds of formula III, 1
    Type: Application
    Filed: December 9, 2002
    Publication date: June 26, 2003
    Inventors: Benoit Pugin, Ivo Steiner, Rhony Niklaus Aufdenblatten, Antonio Togni
  • Patent number: 6569967
    Abstract: The invention concerns alkoxyamines derived from &bgr;-phosphorous nitroxides corresponding to formula (I). Said compounds can be used as (co)polymerization initiators of at least a monomer polymerizable by radical polymerization.
    Type: Grant
    Filed: March 19, 2002
    Date of Patent: May 27, 2003
    Assignee: Atofina
    Inventors: Jean-Luc Couturier, Christiane Henriet-Bernard, Christophe Le Mercier, Paul Tordo, Jean-Francois Lutz
  • Publication number: 20030087307
    Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
    Type: Application
    Filed: March 28, 2002
    Publication date: May 8, 2003
    Applicant: Advanced Medicine, Inc.
    Inventors: Edmund J. Moran, Seok-Ki Choi
  • Patent number: 6555227
    Abstract: Combination compounds from curing agents/accelerators and flame-protection agents for the latent curing/acceleration of epoxide resin systems and their endowment with flame-retarding properties, the epoxide resin systems being able to be thermally cured, as well as the products prepared from the epoxide resin systems.
    Type: Grant
    Filed: February 2, 2001
    Date of Patent: April 29, 2003
    Assignee: Schill & Seilacher (GmbH & Co.)
    Inventors: Stephan Sprenger, Rainer Utz, Michael Ciesielski, Manfred Doering
  • Patent number: 6548567
    Abstract: The invention relates to an ionic compound corresponding to the formula [R1X1(Z1)—Q−—X2(Z2)—R2]m Mm+ in which Mm+ is a cation of valency m, each of the groups Xi is S═Z3, S═Z4, P—R3 or P—R4; Q is N, CR5, CCN or CSO2R5, each of the groups Zi is ═O, ═NC≡N, ═C(C≡N)2, ═NS(═Z)2R6 or ═C[S(═Z)2R6]2, each of the groups Ri, is Y, YO—, YS—, Y2N— or F, Y represents a monovalent organic radical or alternatively Y is a repeating unit of a polymeric frame. The compounds are useful for producing ion conducting materials or electrolytes, as catalysts and for doping polymers.
    Type: Grant
    Filed: August 17, 2001
    Date of Patent: April 15, 2003
    Inventors: Michel Armand, Christophe Michot, Yurii Yagupolskii, Lev Yagupolskii, Andrej Bezdudny, Natalya Kondratenko
  • Patent number: 6538141
    Abstract: The invention concerns a method for preparing nitroxides, which consists in oxidising, in a two-phase medium, using an aliphatic peroxide, secondary amines with steric hindrance or having a —CH in the nitrogen atom &agr;.
    Type: Grant
    Filed: September 24, 2001
    Date of Patent: March 25, 2003
    Assignee: Atofina
    Inventors: Jean-Philippe Gillet, Olivier Guerret, Jean-Pierre Lascombe
  • Publication number: 20030045670
    Abstract: Polyimides displaying low color in thin films, atomic oxygen resistance, vacuum ultraviolet radiation resistance, solubility in organic solvents in the imide form, high glass transistion (Tg) temperatures, and high thermal stability are provided. The poly(amide acid)s, copoly(amide acid)s, polyimides and copolyimides are prepared by the reaction of stoichiometric ratios of an aromatic dianhydride with diamines which contain phenylphosphine oxide groups in polar aprotic solvents.
    Type: Application
    Filed: March 8, 2002
    Publication date: March 6, 2003
    Inventors: John W. Connell, Joseph G. Smith, Paul M. Hergenrother, Kent A. Watson, Craig M. Thompson
  • Patent number: 6509100
    Abstract: The present invention discloses hydrogen bond stabilized surface modifying agents having a fluorinated or semi-fluorinated carbon-containing tail group, an internal moiety capable of intermolecular hydrogen bonding or related acid-base interactions and a head group capable of reacting or interacting with surfaces such as metal, non-metallic, ceramic, other inorganic oxide or organic surfaces. The present invention also discloses cost effective method for making the agents, methods for treating surfaces therewith, the treated surfaces and devices made therefrom.
    Type: Grant
    Filed: August 18, 1999
    Date of Patent: January 21, 2003
    Assignee: The University of Houston System
    Inventors: T. Randall Lee, Michael Graupe
  • Patent number: 6506934
    Abstract: This invention relates to a compound that is represented by the following Structure I: R1—SO2—C(R2)R3—(CO)m—(L)n—SG  I wherein R1 is an aliphatic or cyclic group, R2 and R3 are independently hydrogen or bromine as long as at least one of them is bromine, L is an divalent linking group, m and n are independently 0 or 1, SG is a solubilizing group with a pKa of 8 or less, with the proviso that when m and n are both 0, SG is not a sulfo (or salt thereof) or a sulfonamido (or salt thereof) and when m is 0 and n is 1, either L is not an alkylene group or SG is not a carboxy (or salt thereof).
    Type: Grant
    Filed: December 11, 2001
    Date of Patent: January 14, 2003
    Assignee: Eastman Kodak Company
    Inventors: George J. Burgmaier, Roger L. Klaus
  • Publication number: 20020193592
    Abstract: The present invention relates to compounds of the formula 1
    Type: Application
    Filed: April 30, 2002
    Publication date: December 19, 2002
    Applicant: Clariant GmbH
    Inventors: Berthold Schiemenz, Thomas Wessel, Ralf Pfirmann
  • Patent number: 6486347
    Abstract: A process for the preparation of a compound having the formula R3R4P—Ar—CO—X wherein Ar is an aryl group bearing the PR3R4 and COX groups in a 1,2-relationship, and optionally bearing also one or more non-interfering groups, R3 and R4 are each a hydrocarbon group optionally substituted by any non-interfering group, and X is OH or a non-interfering group, comprises (i) the reaction of NaPR3R4 with F—Ar—COX, or (ii) when X is an amine group, the reaction of R3R4P—Ar—COOY, OY being OH or a leaving group, with a solution of the amine obtained in situ by adding a base to a salt thereof. Certain ligands prepared by such a process are in a novel, crystalline form.
    Type: Grant
    Filed: March 29, 2001
    Date of Patent: November 26, 2002
    Assignee: Chirotech Technology, Ltd.
    Inventors: Ian Campbell Lennon, Ulrich Berens
  • Publication number: 20020165411
    Abstract: The present invention is directed to a catalyst composition, comprising a Group 8 metal; and a ligand having a structure selected from the group consisting of: 1
    Type: Application
    Filed: December 10, 2001
    Publication date: November 7, 2002
    Inventors: John F. Hartwig, James Stambuli, Shaun Stauffer
  • Publication number: 20020099036
    Abstract: The present invention relates to a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for male hormone therapy such as oral testosterone replacement therapy, treating prostate cancer, imaging prostate cancer.
    Type: Application
    Filed: August 23, 2001
    Publication date: July 25, 2002
    Inventors: James T. Dalton, Duane D. Miller, Donghua Yin, Yali He
  • Patent number: 6413947
    Abstract: This invention is to provide a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring; W is a divalent group of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an, optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.
    Type: Grant
    Filed: September 13, 2000
    Date of Patent: July 2, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Shiraishi, Takahito Kitayoshi, Yoshio Aramaki, Susumu Honda, Tsuneo Oda
  • Publication number: 20020072632
    Abstract: New ligands having a backbone comprised of NCCX can be combined with a metal or metal precursor compound or formed into a metal-ligand complex to catalyze a number of different chemical transformations, including polymerization.
    Type: Application
    Filed: February 1, 2002
    Publication date: June 13, 2002
    Applicant: Symyx Technologies
    Inventors: Anil S. Guram, Anne Marie LaPointe, Howard W. Turner, Tetsuo Uno
  • Patent number: 6395916
    Abstract: One aspect of the present invention relates to novel, electron-rich bidentate ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.
    Type: Grant
    Filed: July 10, 1998
    Date of Patent: May 28, 2002
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, John P. Wolfe, David W. Old, Ken Kamikawa, Michael Palucki
  • Publication number: 20020058814
    Abstract: The invention relates to the preparation of enantiomerically pure bis-diphenylphosphine oxides in a particularly advantageous manner by (1) reacting an aromatic bromine compound with a diphenylphosphinic chloride in a mixture of tetrahydrofuran and an aromatic hydrocarbon to give a diphenylphosphine oxide, which is isolated from a solution in an aromatic hydrocarbon by adding a saturated aliphatic hydrocarbon; (2) metalating the resulting diphenylphosphine oxide in the 6-position and reacting the metalated diphenylphosphine oxide with iodine at temperatures not less than −25° C.
    Type: Application
    Filed: November 13, 2001
    Publication date: May 16, 2002
    Inventors: Torsten Pohl, Thomas Prinz, Guido Giffels, Wolfram Sirges
  • Publication number: 20020058837
    Abstract: A novel 2,2-(diaryl)vinylphosphine compound represented by the following general formula (1): 1
    Type: Application
    Filed: June 27, 2001
    Publication date: May 16, 2002
    Inventors: Ken Suzuki, Tohru Kobayashi, Takenobu Nishikawa, Yoji Hori, Toshimitsu Hagiwara
  • Patent number: 6388130
    Abstract: The invention provides a metal complex comprising a ligand and a metal. The ligand is an aminophosphine compound represented by the following formula (1) The metal is rhodium, ruthenium, iridium or nickel.
    Type: Grant
    Filed: June 7, 2001
    Date of Patent: May 14, 2002
    Assignee: Takasago International Corporation
    Inventors: Sumi Kenzo, Noyori Ryoji, Ikariya Takao
  • Publication number: 20020012631
    Abstract: This invention relates to novel highly functionalized phosphine ligands as ancillary ligands in radiopharmaceuticals. Also, this invention provides radiopharmaceuticals comprised of highly functionalized phosphine ligated 99mTc labeled HYNIC-conjugated biomolecules that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy. The invention also provides methods of use of the radiopharmaceuticals as imaging agents for the diagnosis of cardiovascular disorders such as thromboembolic disease or atherosclerosis, infectious disease and cancer.
    Type: Application
    Filed: April 5, 2001
    Publication date: January 31, 2002
    Inventor: Shuang Liu
  • Patent number: 6307098
    Abstract: This invention relates to water soluble phosphines of the following structural formula and method of preparing these phosphines: Wherein A is a moiety which is stable to the reaction conditions and does not interfere with solubility of the compound in the preparation reaction. R1 and R2 are selected from hydroxyl groups, dialkylamino group, and alkoxide groups.
    Type: Grant
    Filed: June 9, 2000
    Date of Patent: October 23, 2001
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: Terrence L. Schull, Walter J. Dressick
  • Patent number: 6307087
    Abstract: One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.
    Type: Grant
    Filed: January 13, 1999
    Date of Patent: October 23, 2001
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, David W. Old, John P. Wolfe, Michael Palucki, Ken Kamikawa
  • Patent number: 6291702
    Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be colorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.
    Type: Grant
    Filed: February 8, 2000
    Date of Patent: September 18, 2001
    Assignee: Florida International University
    Inventor: David Alan Becker
  • Publication number: 20010011145
    Abstract: A process for the preparation of a compound having the formula
    Type: Application
    Filed: March 29, 2001
    Publication date: August 2, 2001
    Inventors: Ian Campbell Lennon, Ulrich Berens
  • Patent number: 6262278
    Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.
    Type: Grant
    Filed: August 14, 1998
    Date of Patent: July 17, 2001
    Assignee: President and Fellows of Harvard College
    Inventors: Eric N. Jacobsen, Makoto Tokunaga, Jay F. Larrow
  • Patent number: 6225499
    Abstract: This invention provides a process for preparing aminoarylacetylenes comprising reacting a N-arylmethylidene aminoarylhalide with a terminal acetylene in the presence of a base and a catalyst system comprising a palladium catalyst and a cuprous salt to produce a novel N-arylmethylidene aminoarylacetylene, and hydrolyzing the N-arylmethylidene aminoarylacetylene to the aminoarylacetylene. In one embodiment, the invention provides a process for preparing aminophenylacetylenes comprising reacting a N-benzylidene aminophenylhalide with a terminal acetylene in the presence of a base and the catalyst system to produce a novel N-benzylidene aminophenylacetylene, and hydrolyzing the N-benzylidene aminophenylacetylene to the aminophenylacetylene.
    Type: Grant
    Filed: July 14, 1997
    Date of Patent: May 1, 2001
    Assignee: Catalytica Pharmaceuticals, Inc.
    Inventor: John M. Gruber
  • Patent number: 6221898
    Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
    Type: Grant
    Filed: August 29, 1997
    Date of Patent: April 24, 2001
    Assignee: Astra Aktiebolag
    Inventor: Thomas Antonsson
  • Patent number: 6211304
    Abstract: Novel mordants based upon a poly(alkylene oxide) backbone and either pendant phosphonium or quaternized-nitrogen compounds are disclosed. The mordants find use in stopping or controlling ink-bleeding in ink-jet receptors and photographic films.
    Type: Grant
    Filed: August 30, 1995
    Date of Patent: April 3, 2001
    Assignee: 3M Innovative Properties Company
    Inventor: Omar Farooq
  • Patent number: 6197825
    Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be calorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.
    Type: Grant
    Filed: May 28, 1998
    Date of Patent: March 6, 2001
    Assignee: Florida International University
    Inventor: David Alan Becker
  • Patent number: 6187953
    Abstract: Guanidinium phosphanes of Formula I wherein the substituents are defined as in the specification which are useful catalyst ligands for the carbon-carbon linkage reactions of the hect reaction.
    Type: Grant
    Filed: November 17, 1999
    Date of Patent: February 13, 2001
    Assignee: Celanese GmbH
    Inventors: Othmar Stelzer, Franz Peter Schmidtchen, Antonella Hessler, Michael Tepper, Harald Dibowski, Michael Riedel, Helmut Bahrmann
  • Patent number: 6153794
    Abstract: An organic compound which is basic and soluble in an organic solvent, does not have a problem in preparation or handling and exhibits catalytic activity as a basic compound, i.e., a phosphine sulfide represented by formula (1), and a manufacturing process therefor, i.e., manufacturing a phosphine sulfide represented by formula (1), by reacting one molecule of thiophosphoryl chloride with three molecules of a phosphorane represented by formula (2). The phosphine sulfide can be used in a process for effectively manufacturing a poly(alkylene oxide) by polymerizing an alkylene oxide in the presence of the phosphine sulfide or of the phosphine sulfide and an active hydrogen compound selected from water and organic compounds having a partial structure of --OH or --NH--; and 2) a process for manufacturing a 1,2-dioxyethane derivative from an epoxy compound, i.
    Type: Grant
    Filed: July 7, 1999
    Date of Patent: November 28, 2000
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Katsuhiko Funaki, Isao Hara, Takaomi Hayashi, Shinji Kiyono, Atsushi Shibahara, Kazumi Mizutani, Tadahito Nobori, Usaji Takaki
  • Patent number: 6147061
    Abstract: A compound of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, synergy with cytotoxic anticancer agents, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, in combination with standard NSAID'S and analgesics and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinim, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.
    Type: Grant
    Filed: July 14, 1997
    Date of Patent: November 14, 2000
    Assignee: Pfizer Inc.
    Inventor: Lawrence A. Reiter
  • Patent number: 6121252
    Abstract: The present invention relate to phosphinic acid derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising the same, and methods of using the same to inhibit NAALADase activity and to treat glutamate abnormalities and prostate diseases.
    Type: Grant
    Filed: March 30, 1998
    Date of Patent: September 19, 2000
    Assignee: Guilford Pharmaceuticals Inc.
    Inventors: Paul F. Jackson, Takashi Tsukamoto, Yao-Sen Ko, Barbara S. Slusher
  • Patent number: 6100429
    Abstract: This invention provides a process for preparing aminoarylacetylenes comprising reacting a N-arylmethylidene aminoarylhalide with a terminal acetylene in the presence of a base and a catalyst system comprising a palladium catalyst and a cuprous salt to produce a novel N-arylmethylidene aminoarylacetylene, and hydrolyzing the N-arylmethylidene aminoarylacetylene to the aminoarylacetylene.
    Type: Grant
    Filed: June 16, 1999
    Date of Patent: August 8, 2000
    Assignee: Catalytica Pharmaceuticals, Inc.
    Inventor: John M. Gruber
  • Patent number: 6060614
    Abstract: The invention relates to novel chelating ligands which incorporate a tripodal backbone. More particularly, the invention pertains to novel tripodal ligands which form coordination compounds with a variety of metal ions, particularly, but not exclusively, trivalent metal ions and lanthanide metal ions, which are useful in nuclear medicine. A novel amine phosphinate tripodal ligand, a chelating ligand and a process therefor involving a metal ion and particularly a trivalent metal ion of the group 13 metals and the rare earths. The process comprises complexing Tc or Re or any one of the group 13 metals, Al, Ga and In, and any one of the rare earths, Sc, Y, La, Ce, Pr, Nd, Pm, Sm, Eu, Gd, Th, Dy, Ho, En, Tm, Yb and Lu, with an amine phosphinate tripodal ligand.
    Type: Grant
    Filed: July 10, 1998
    Date of Patent: May 9, 2000
    Assignee: The University of British Columbia
    Inventors: Chris Orvig, Mark P. Lowe
  • Patent number: 6060522
    Abstract: A solid, water-soluble complex comprising:a) a polysiloxane of the formula: ##STR1## wherein n is from 2 to 6; a is from 8 to 25; and b is from 0 to 25; and the oxyalkylene groups may be random or block mixtures; y is from 0 to 5; x is from 1 to 5; and R is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 alkyl, and a C.sub.1 -C.sub.4 alkyl ester; or ##STR2## wherein A is a linear or branched alkyl having 6 to 30 carbon atoms; G is a glycol moiety of the formula --R'(OCH.sub.2 CH.sub.2).sub.m OR" wherein R' is a divalent alkylene group having 2 to 6 carbon atoms; R" is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 alkyl, and a C.sub.1 -C.sub.4 alkyl ester; m is 8 to 100; y is 0 to 5; X is 0.1 to 2.5; and z is 0.1 to 5.0;b) a complex-forming agent of the formula: ##STR3## wherein X is O, S, Se, or Te, and c) a readily clathratable polyoxyethylene, e.g. a tridecyl alcohol ethoxylate having eight or more oxyethylene units.
    Type: Grant
    Filed: August 14, 1997
    Date of Patent: May 9, 2000
    Assignee: Rhodia Inc.
    Inventors: Norman Robert Pallas, James Lyle Hazen