Phosphorus Attached Indirectly To Amino Nitrogen By Nonionic Bonding Patents (Class 564/15)
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Publication number: 20040147785Abstract: 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: ApplicationFiled: January 15, 2004Publication date: July 29, 2004Inventors: Roelof Van Ginkel, Alexander Van Der Made, Jan De With, Wolf Eilenberg, Ursula Eilenberg-Robben
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Publication number: 20040110979Abstract: The invention relates to a process for preparing diphosphines of the formulaType: ApplicationFiled: September 25, 2003Publication date: June 10, 2004Inventors: Ralf Jackstell, Holger Klein, Matthias Beller, Klaus-Diether Wiese, Cornelia Borgmann
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Publication number: 20040102649Abstract: 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: ApplicationFiled: April 23, 2003Publication date: May 27, 2004Inventors: Christine Saluzzo, Thierry Lamouille, Marc Lemaire, Robert Ter Halle
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Publication number: 20040068131Abstract: 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: ApplicationFiled: July 25, 2003Publication date: April 8, 2004Inventors: Matthias Beller, Andreas Ehrentraut, Wilhelm Hubert Ehrentraut, Theresia Elisabeth Ehrentraut, Christa Fuhrmann, Alexander Zapf
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Publication number: 20040048834Abstract: 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: ApplicationFiled: August 18, 2003Publication date: March 11, 2004Inventors: Jose Luis Acena, Javier Adrjo, Carmen Cuevas, Pilar Gallego, Ignacio Manzanares, Simon Munt, Ignacio Rodriguez
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Patent number: 6699851Abstract: 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: GrantFiled: May 6, 2003Date of Patent: March 2, 2004Assignee: Ardenia Investments, Ltd.Inventor: Oleg Strelchenok
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Patent number: 6693210Abstract: 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: GrantFiled: September 13, 2002Date of Patent: February 17, 2004Assignee: Mitsubishi Rayon Co., Ltd.Inventor: Norio Miyaura
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Publication number: 20040029913Abstract: 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: ApplicationFiled: February 24, 2003Publication date: February 12, 2004Inventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka
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Publication number: 20040014975Abstract: 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: ApplicationFiled: October 22, 2002Publication date: January 22, 2004Inventors: James T. Dalton, Duane D. Miller, Yali He, Donghua Yin
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Publication number: 20030225040Abstract: 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: ApplicationFiled: October 16, 2002Publication date: December 4, 2003Inventors: James T. Dalton, Duane D. Miller, Yali He, Donghua Yin
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Patent number: 6657081Abstract: 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: GrantFiled: May 29, 2001Date of Patent: December 2, 2003Assignee: Commissariat a l'Energie AtomiqueInventors: Jean-François Dozol, Alejandro Garcia Carrera, Volker Bohmer, Susan E. Matthews
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Patent number: 6646079Abstract: 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: GrantFiled: April 9, 2001Date of Patent: November 11, 2003Assignee: AtofinaInventors: Olivier Guerret, Sophie Robin, Yves Gnanou
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Patent number: 6630501Abstract: 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: GrantFiled: March 25, 2002Date of Patent: October 7, 2003Assignees: Commissariat a l'energie Atomique, Institut National de la Recherche Medical, Centre National de la Recherche ScientifiqueInventors: Vincent Dive, Philippe Cuniasse, Marie-Christine Rio, Paul Basset, Athanasios Yotakis, Fabrice Beau, Stamania Vassiliou
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Patent number: 6613848Abstract: 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: GrantFiled: May 16, 2000Date of Patent: September 2, 2003Assignee: National Science CouncilInventors: Chun-Shan Wang, Jeng-Yueh Shieh
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Publication number: 20030120122Abstract: Compounds of formula III, 1Type: ApplicationFiled: December 9, 2002Publication date: June 26, 2003Inventors: Benoit Pugin, Ivo Steiner, Rhony Niklaus Aufdenblatten, Antonio Togni
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Patent number: 6569967Abstract: 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: GrantFiled: March 19, 2002Date of Patent: May 27, 2003Assignee: AtofinaInventors: Jean-Luc Couturier, Christiane Henriet-Bernard, Christophe Le Mercier, Paul Tordo, Jean-Francois Lutz
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Publication number: 20030087307Abstract: 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: ApplicationFiled: March 28, 2002Publication date: May 8, 2003Applicant: Advanced Medicine, Inc.Inventors: Edmund J. Moran, Seok-Ki Choi
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Patent number: 6555227Abstract: 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: GrantFiled: February 2, 2001Date of Patent: April 29, 2003Assignee: Schill & Seilacher (GmbH & Co.)Inventors: Stephan Sprenger, Rainer Utz, Michael Ciesielski, Manfred Doering
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Patent number: 6548567Abstract: 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: GrantFiled: August 17, 2001Date of Patent: April 15, 2003Inventors: Michel Armand, Christophe Michot, Yurii Yagupolskii, Lev Yagupolskii, Andrej Bezdudny, Natalya Kondratenko
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Patent number: 6538141Abstract: 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: GrantFiled: September 24, 2001Date of Patent: March 25, 2003Assignee: AtofinaInventors: Jean-Philippe Gillet, Olivier Guerret, Jean-Pierre Lascombe
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Publication number: 20030045670Abstract: 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: ApplicationFiled: March 8, 2002Publication date: March 6, 2003Inventors: John W. Connell, Joseph G. Smith, Paul M. Hergenrother, Kent A. Watson, Craig M. Thompson
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Patent number: 6509100Abstract: 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: GrantFiled: August 18, 1999Date of Patent: January 21, 2003Assignee: The University of Houston SystemInventors: T. Randall Lee, Michael Graupe
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Patent number: 6506934Abstract: 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: GrantFiled: December 11, 2001Date of Patent: January 14, 2003Assignee: Eastman Kodak CompanyInventors: George J. Burgmaier, Roger L. Klaus
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Publication number: 20020193592Abstract: The present invention relates to compounds of the formula 1Type: ApplicationFiled: April 30, 2002Publication date: December 19, 2002Applicant: Clariant GmbHInventors: Berthold Schiemenz, Thomas Wessel, Ralf Pfirmann
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Patent number: 6486347Abstract: 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: GrantFiled: March 29, 2001Date of Patent: November 26, 2002Assignee: Chirotech Technology, Ltd.Inventors: Ian Campbell Lennon, Ulrich Berens
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Publication number: 20020165411Abstract: 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: 1Type: ApplicationFiled: December 10, 2001Publication date: November 7, 2002Inventors: John F. Hartwig, James Stambuli, Shaun Stauffer
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Publication number: 20020099036Abstract: 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: ApplicationFiled: August 23, 2001Publication date: July 25, 2002Inventors: James T. Dalton, Duane D. Miller, Donghua Yin, Yali He
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Patent number: 6413947Abstract: 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: GrantFiled: September 13, 2000Date of Patent: July 2, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Takahito Kitayoshi, Yoshio Aramaki, Susumu Honda, Tsuneo Oda
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Publication number: 20020072632Abstract: 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: ApplicationFiled: February 1, 2002Publication date: June 13, 2002Applicant: Symyx TechnologiesInventors: Anil S. Guram, Anne Marie LaPointe, Howard W. Turner, Tetsuo Uno
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Patent number: 6395916Abstract: 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: GrantFiled: July 10, 1998Date of Patent: May 28, 2002Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, John P. Wolfe, David W. Old, Ken Kamikawa, Michael Palucki
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Publication number: 20020058814Abstract: 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: ApplicationFiled: November 13, 2001Publication date: May 16, 2002Inventors: Torsten Pohl, Thomas Prinz, Guido Giffels, Wolfram Sirges
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Publication number: 20020058837Abstract: A novel 2,2-(diaryl)vinylphosphine compound represented by the following general formula (1): 1Type: ApplicationFiled: June 27, 2001Publication date: May 16, 2002Inventors: Ken Suzuki, Tohru Kobayashi, Takenobu Nishikawa, Yoji Hori, Toshimitsu Hagiwara
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Patent number: 6388130Abstract: 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: GrantFiled: June 7, 2001Date of Patent: May 14, 2002Assignee: Takasago International CorporationInventors: Sumi Kenzo, Noyori Ryoji, Ikariya Takao
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Publication number: 20020012631Abstract: 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: ApplicationFiled: April 5, 2001Publication date: January 31, 2002Inventor: Shuang Liu
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Patent number: 6307098Abstract: 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: GrantFiled: June 9, 2000Date of Patent: October 23, 2001Assignee: The United States of America as represented by the Secretary of the NavyInventors: Terrence L. Schull, Walter J. Dressick
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Patent number: 6307087Abstract: 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: GrantFiled: January 13, 1999Date of Patent: October 23, 2001Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, David W. Old, John P. Wolfe, Michael Palucki, Ken Kamikawa
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Patent number: 6291702Abstract: 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: GrantFiled: February 8, 2000Date of Patent: September 18, 2001Assignee: Florida International UniversityInventor: David Alan Becker
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Publication number: 20010011145Abstract: A process for the preparation of a compound having the formulaType: ApplicationFiled: March 29, 2001Publication date: August 2, 2001Inventors: Ian Campbell Lennon, Ulrich Berens
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Patent number: 6262278Abstract: 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: GrantFiled: August 14, 1998Date of Patent: July 17, 2001Assignee: President and Fellows of Harvard CollegeInventors: Eric N. Jacobsen, Makoto Tokunaga, Jay F. Larrow
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Patent number: 6225499Abstract: 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: GrantFiled: July 14, 1997Date of Patent: May 1, 2001Assignee: Catalytica Pharmaceuticals, Inc.Inventor: John M. Gruber
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Patent number: 6221898Abstract: 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: GrantFiled: August 29, 1997Date of Patent: April 24, 2001Assignee: Astra AktiebolagInventor: Thomas Antonsson
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Patent number: 6211304Abstract: 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: GrantFiled: August 30, 1995Date of Patent: April 3, 2001Assignee: 3M Innovative Properties CompanyInventor: Omar Farooq
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Patent number: 6197825Abstract: 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: GrantFiled: May 28, 1998Date of Patent: March 6, 2001Assignee: Florida International UniversityInventor: David Alan Becker
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Patent number: 6187953Abstract: 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: GrantFiled: November 17, 1999Date of Patent: February 13, 2001Assignee: Celanese GmbHInventors: Othmar Stelzer, Franz Peter Schmidtchen, Antonella Hessler, Michael Tepper, Harald Dibowski, Michael Riedel, Helmut Bahrmann
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Patent number: 6153794Abstract: 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: GrantFiled: July 7, 1999Date of Patent: November 28, 2000Assignee: Mitsui Chemicals, Inc.Inventors: Katsuhiko Funaki, Isao Hara, Takaomi Hayashi, Shinji Kiyono, Atsushi Shibahara, Kazumi Mizutani, Tadahito Nobori, Usaji Takaki
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Patent number: 6147061Abstract: 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: GrantFiled: July 14, 1997Date of Patent: November 14, 2000Assignee: Pfizer Inc.Inventor: Lawrence A. Reiter
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Patent number: 6121252Abstract: 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: GrantFiled: March 30, 1998Date of Patent: September 19, 2000Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Takashi Tsukamoto, Yao-Sen Ko, Barbara S. Slusher
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Patent number: 6100429Abstract: 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: GrantFiled: June 16, 1999Date of Patent: August 8, 2000Assignee: Catalytica Pharmaceuticals, Inc.Inventor: John M. Gruber
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Patent number: 6060614Abstract: 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: GrantFiled: July 10, 1998Date of Patent: May 9, 2000Assignee: The University of British ColumbiaInventors: Chris Orvig, Mark P. Lowe
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Patent number: 6060522Abstract: 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: GrantFiled: August 14, 1997Date of Patent: May 9, 2000Assignee: Rhodia Inc.Inventors: Norman Robert Pallas, James Lyle Hazen