Plural Phosphori Attached Indirectly To Each Other By Nonionic Bonding Patents (Class 562/12)
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Patent number: 10464958Abstract: The present invention is related to a new method for the synthesis of alpha-aminoalkylenephosphonic acid or its phosphonate esters comprising the steps of forming a reaction mixture by mixing a P—O—P anhydride moiety comprising compound, having one P-atom at the oxidation state (+III) and the other P-atom at the oxidation state (+III) or (+V), an aminoalkanecarboxylic acid and an acid catalyst, wherein said reaction mixture comprises an equivalent ratio of alpha-aminoalkylene carboxylic acid to P—O—P anhydride moieties of at least 0.2, and recovering the resulting alpha-aminoalkylene phosphonic acid compound or an ester thereof from the reaction mixture.Type: GrantFiled: December 20, 2017Date of Patent: November 5, 2019Assignee: Monsanto Technology LLCInventors: Patrick Notte, Samuel Cogels, Sebastian Burck
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Publication number: 20140336408Abstract: A process for the manufacture of alkylamino alkylene phosphonic acids is disclosed. In detail, a specific phosphonate is reacted with an agent selected to yield an alkylamino moiety substituted by a radical selected from OH, OR', NH2, NHR?, N(R?)2, NH, N, S, S—S and SH in aqueous alkaline medium having a pH of 8 or higher at a temperature of 0° C. or higher.Type: ApplicationFiled: July 28, 2014Publication date: November 13, 2014Inventors: Patrick P.B. Notte, Jan H.J. Van Bree, Albert Devaux
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Publication number: 20140296364Abstract: The invention relates to a dental material which comprises a polymerizable bisphosphonic acid of Formula I: The invention also relates to the use of a polymerizable bisphosphonic acid of Formula I for the preparation of a dental material and in particular for the preparation of an adhesive, cement or composite.Type: ApplicationFiled: December 6, 2012Publication date: October 2, 2014Inventors: Norbert Moszner, Yohann Catel, Jörg Angermann, Thorsten Bock, Volker Rheinberger
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Publication number: 20140107078Abstract: The invention relates to hypophosphorous acid derivatives of formula (I) wherein —X is H or OH, —R represents one or several radicals R1-R5, identical or different, two of R1-R5 optionally occupying the same position on the phenyl group, one to four of R1-R5 being H and the others being selected in the group comprising -0-(CH2)n—COOH; —S—(CH2)n—COOH; —NH—(CH2)n—COOH; -0-(CH,R?)—COOH; —O—(CH2)n—OH; OR?, —R? being a C1-C3 alkyl radical; —OH; —COOH; halogen, particularly —F, —CI, —Br, —I, —CF3; —OCF3; —N02; —CH?CH—COOH; —(CH2)n—COOH; O—(CH2)n—P03H2; O—(CF2)n—P03H2; O—(CH2)n—S03H; O—(CH2)n—CONHOH; O—(CH2)n-tetrazol; O—(CH2)n-hydroxyisoxazol—n=1 to 5, preferably 1-3; said hypophosrous acid derivatives being diastereoisomers or enantiomers.Type: ApplicationFiled: May 16, 2012Publication date: April 17, 2014Applicants: UNIVWESITE D"AUVERGNE, UNIVERSITE PARIS DESCARTESInventors: Francine Acher, Jean-Philippe Pin, Cyril Goudet, Alain Eschalier, Jérôme Busserolles, Delphine Rigault, Isabelle Lemasson, Sara Cesarini, Brono Commare
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Publication number: 20130299432Abstract: Scale control agents comprising organic phosphonates, either alone or in mixtures with inorganic phosphonates and also optionally polymers, such as low molecular weight polymeric dispersants. The scale control agents may be applied to inhibit scale formation or deposition in highly acidic aqueous systems by adding these agents to such systems in amounts effective to inhibit metal sulfate scale formation.Type: ApplicationFiled: May 8, 2013Publication date: November 14, 2013Inventors: Sachin Borkar, Michael James Bluemle, Lawrence J. Andermann, JR.
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Patent number: 8505626Abstract: Novel aminoacid alkylphosphonic acid compounds are disclosed. These compounds can be used in multiple applications, in particular in a scale inhibitor functionality in aqueous systems, including in marine oil recovery.Type: GrantFiled: May 25, 2007Date of Patent: August 13, 2013Assignee: Dequest AGInventors: Patrick Notte, Albert Devaux
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Publication number: 20120316359Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.Type: ApplicationFiled: August 17, 2012Publication date: December 13, 2012Inventor: Thomas Daly
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Patent number: 8221712Abstract: An absorption medium for the removal of acid gases from a fluid stream comprises an aqueous solution a) of at least one amine and b) at least one phosphonic acid, wherein the molar ratio of b) to a) is in the range from 0.0005 to 1.0. The phosphonic acid is, e.g., 1-hydroxyethane-1,1-diphosphonic acid. The absorption medium exhibits a reduced regeneration energy requirement compared with absorption media based on amines or amine/promoter combinations, without significantly decreasing the absorption capacity of the solution for acid gases.Type: GrantFiled: October 9, 2009Date of Patent: July 17, 2012Assignee: BASF SEInventors: Gerald Vorberg, Torsten Katz, Georg Sieder, Christian Riemann, Erika Dengler
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Publication number: 20120142641Abstract: The present invention relates to a complex of a bisphosphonate compound, methods of preparing such complex and uses thereof.Type: ApplicationFiled: June 7, 2010Publication date: June 7, 2012Applicant: NANYANG TECHNOLOGICAL UNIVERSITYInventors: Subramanian Venkatraman, Say Chye Joachim Loo
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Publication number: 20120136171Abstract: A method for the manufacture of aminoalkylene phosphonic acids broadly is disclosed. In the essence, an amine corresponding to a specific formula is reacted in aqueous medium with phosphorous acid and formaldehyde to thereby yield a medium insoluble reaction product. The insoluble product formed i.e. the aminoalkylene phosphonic acid can be separated, optionally washed, and recovered. This process yields high purity and selectivity reaction products. The excess phosphonic acid can be recycled into the processing sequence.Type: ApplicationFiled: May 28, 2010Publication date: May 31, 2012Applicant: STRAITMARK HOLDING AGInventors: Patrick Notté, Cedric Nicolas Pirard, David Lemin
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Publication number: 20120107323Abstract: The invention provides compounds capable of treating a subject suffering from or being susceptible to a cell proliferative disorder (especially, cancer), methods of identifying and using the compounds, pharmaceutical compositions and kits thereof.Type: ApplicationFiled: March 12, 2010Publication date: May 3, 2012Applicant: University of FloridaInventors: Steven N. Hochwald, David A. Ostrov, William G. Cance, Elena Kurenova
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Publication number: 20120073475Abstract: The invention relates to a compound of following formula (I): the preparation method thereof and the use of same.Type: ApplicationFiled: March 31, 2010Publication date: March 29, 2012Applicant: CHRYSOInventors: Philippe Maitrasse, Bruno Pellerin, Frederic Leising
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Patent number: 8003820Abstract: A process for preparing a bisphosphonate compound comprises reacting a carboxylic acid with a phosphonating agent, in a cresol solvent.Type: GrantFiled: October 18, 2006Date of Patent: August 23, 2011Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.Inventors: Venkata Naga Brahmeswara Rao Mandava, Radha Krishna Singam Setty, Nagaraju Manne
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Patent number: 7833993Abstract: The present invention is directed to methods of treating diseases and disorders related to immune responses by administering one or more immunomodulatory compounds. In particular, the invention is directed to methods of stimulating and reducing immune responses, treating autoimmune conditions, treating allergic reactions and asthma, and preventing ischemic damage and asthma by administering one or more immunomodulatory compounds.Type: GrantFiled: March 9, 2005Date of Patent: November 16, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Lynn D. Hawkins, Sally T. Ishizaka
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Publication number: 20100174110Abstract: A process for the manufacture of alkylamino alkylene phosphonic acids is disclosed. In detail, a specific phosphonate is reacted with an agent selected to yield an alkylamino moiety substituted by a radical selected from OH, OR?, NH2, NHR?, N(R?)2, NH, N, S, S—S and SH in aqueous alkaline medium having a pH of 8 or higher at a temperature of 0° C. or higher.Type: ApplicationFiled: December 11, 2007Publication date: July 8, 2010Applicant: THERMPHOS TRADING GMBHInventors: Patrick P.B. Notte, Jan H.J. Van Bree, Albert Devaux
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Publication number: 20080227961Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.Type: ApplicationFiled: September 4, 2007Publication date: September 18, 2008Inventor: Sudhakar Kasina
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Patent number: 7081212Abstract: Solid free-flowing compositions of a magnesium salt of bis(hexamethylene)triamino penta(methylenephosphonic) acid are disclosed. The compositions exhibit desirable scale inhibitor properties and can be used in water treatment. In addition, a method of scale control is disclosed using the magnesium phosphonic acids under ambient conditions of relative humidity of at least 30% as can apply under subtropical or tropical conditions of high relative humidity. The preferred molar ratios of magnesium to phosphonic acid are in the range of from 1:1 to 3:1.Type: GrantFiled: August 1, 2002Date of Patent: July 25, 2006Assignee: N.V. Solutia Europe S.A.Inventor: Bernard Marin
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Patent number: 7053138Abstract: Compounds of formula (I) or (II), wherein R1 is C1–C18alkyl; C5–C12cycloalkyl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups; C5–C22aryl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups; or C7–C30aralkyl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups, and the radicals R2 to R13 are each independently of the others hydrogen; —NO2; dialkylamino; alkylthio; alkylsulfonyl; halogen; C1–C18alkyl; C1–C18alkoxy; C1–C18alkoxyalkyl; C5–C12cycloalkyl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups; C5–C22aryl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups; or C7–C30aralkyl that is unsubstituted or substituted by one or more C1–C6alkyl groups or C1–C6alkoxy groups, are suitable as flame-proofing agents for thermoplastic or thermosetting polymersType: GrantFiled: November 20, 2001Date of Patent: May 30, 2006Assignee: Huntsman Advanced Materials Americas Inc.Inventors: Franck Magendie, Ulrich Weidmann
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Patent number: 6699910Abstract: The present invention relates to novel ketone compounds, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.Type: GrantFiled: October 11, 2001Date of Patent: March 2, 2004Assignee: Esperion Therapeutics, Inc.Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
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Patent number: 6683209Abstract: A method is provided for making aromatic-imide and aromatic-methylidynetrissulfonyl species by reaction of aromatic species with a reactant according to formula (I): (X—SO2—)m—QH—(—SO2—R1)n (I) wherein Q is C or N; wherein each X is independently selected from the group consisting of halogens, typically F or Cl; wherein each R1 is independently selected from the group consisting of aliphatic and aromatic groups, which may or may not be saturated, unsaturated, straight-chain, branched, cyclic, heteroatomic, polymeric, halogenated, fluorinated or substituted; wherein m is greater than 0; wherein m+n=2 when Q is N; and wherein m+n=3 when Q is C. Ar may be derived from an aromatic polymeric compound.Type: GrantFiled: May 12, 2003Date of Patent: January 27, 2004Assignee: 3M Innovative Properties CompanyInventor: Steven Joseph Hamrock
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Patent number: 6590118Abstract: Disclosed are compounds of formula I wherein A, R1, R2, R3, R4 and R5 are described in the specification, pharmaceutical formulations comprising these compounds, the use of these compounds are medicaments, the use of these medicaments in the treatment of and/or prevention of diabetes, especially non-insulin dependent diabetes (NIDDM or Type 2 diabetes), as well as methods for treating diabetes comprising administration of these compounds.Type: GrantFiled: September 28, 2000Date of Patent: July 8, 2003Assignee: Novo Nordisk A/SInventors: Marit Kristiansen, Palle Jakobsen, Jane Marie Lundbeck
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Patent number: 6509324Abstract: Compounds able to chelate bi- and trivalent paramagnetic metal ions, their chelated complexes with these metal ions and physiologically compatible salts thereof and therein magnetic resonance imaging.Type: GrantFiled: September 24, 2001Date of Patent: January 21, 2003Assignee: Bracco S.p.A.Inventors: Maurizio Franzini, Andrea Beltrami, Luisella Calabi, Alessandro Maiocchi, Mario Virtuani, Pier Lucio Anelli, Kondareddiar Ramalingam, Ramachandran S. Ranganathan
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Publication number: 20020187928Abstract: The invention provides a compound of formula (I): 1Type: ApplicationFiled: May 30, 2001Publication date: December 12, 2002Inventors: Lixin Qiao, Rene Etcheberrigaray
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Publication number: 20020156308Abstract: Chelating agents (chelants) of the general structure: 1Type: ApplicationFiled: April 25, 2002Publication date: October 24, 2002Inventors: Christer L. Hakanson, Martin Heus
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Publication number: 20020090342Abstract: Tripodal polyaminophosphonate chelants are disclosed, as well as chelates of the chelants with metal ions to form radiopharmaceutical and radioactive, MRI and X-ray or CT imaging compounds and compositions. Therapeutic and imaging methods of use are also disclosed.Type: ApplicationFiled: December 27, 2001Publication date: July 11, 2002Inventor: Shuang Liu
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Patent number: 6403826Abstract: A description is given of compounds of the formula in which the general symbols are as defined in claim 1, and of their zirconium, bismuth and calcium salts, and of the salts with the compounds of the formula II in which the general symbols are as defined in claim 1, as corrosion inhibitors in coating compositions for protecting metallic surfaces.Type: GrantFiled: September 11, 2000Date of Patent: June 11, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Adalbert Braig, Andreas Kramer, Jean-Pierre Wolf, Markus Frey
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Patent number: 6395930Abstract: A method for enhancing the purity of a desired compound comprising: Step (a) treating a crude reaction product which contains at least one desired compound, unreacted starting materials and/or byproducts with at least one bifunctional quenching agent that is capable of selective covalent reaction with unwanted byproducts, or excess reagents; Step (b) allowing the quenching agent to covalently react with unreacted starting materials and/or byproducts to afford a derivatized compound of the quenching agent: and Step (c) isolating the desired compound is described as well as novel quenching agents and methods for their use in the rapid purification of synthetic intermediates and products in synthesis, combinatorial chemistry, and automated organic synthesis.Type: GrantFiled: May 25, 2000Date of Patent: May 28, 2002Assignee: Warner LambertInventor: Sham Nikam
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Patent number: 6388131Abstract: The invention provides compounds, compositions and methods relating to novel electrophilic aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: May 31, 2001Date of Patent: May 14, 2002Assignee: Tularik, Inc.Inventors: Julio Cesar Medina, David Louis Clark, John A. Flygare, Terry J. Rosen, Bei Shan
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Publication number: 20020049185Abstract: There is described the use of a compound represented by general formulae (I), (II) or (III), for the inhibition of matrix metalloproteinases (MMP), wherein X1 is oxygen or sulfur, R1 is OH, SH, CH2OH, CH2SH or NHOH, R2 is a residue of 2 to 10 hydrocarbon backbone atoms, which binds to the amino acid 161 of HNC, said residue being saturated or unsaturated, linear or branched, and contains preferably homocyclic or heterocyclic structures, X2 is oxygen or sulfur and binds as hydrogen acceptor on amino acid 160 of HNC, Y is a residue which binds to the S1′ pocket of HNC and consists of at least 4 backbone atoms Z1-Z2-Z3-Z4-R3, and R3 is n-propyl, isopropyl, isobutyl or a residue with at least 4 backbone atoms, which is not larger than a tricyclic ring system. These compounds bind to MMPs in a manner different from the mode of binding of the inhibitors of the state of the art.Type: ApplicationFiled: February 2, 2001Publication date: April 25, 2002Applicant: ROCHE DIAGNOSTICS GMBHInventors: Luis Moroder, Wolfram Bode, Frank Grams, Robert Huber
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Patent number: 6372726Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel methods of using phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives to inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.Type: GrantFiled: September 27, 1999Date of Patent: April 16, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Barbara S. Slusher, Paul F. Jackson, Kevin L. Tays, Keith M. Maclin
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Patent number: 6350903Abstract: Novel reactions used to prepare phosphole and bisphosphole compounds are detailed. Novel phosphole compounds and metal coordination compounds of phosphole and bisphosphole compounds are also provided. These metal coordination compounds are useful as catalysts for the polymerization or olefins with carbon monoxide and for the polymerization of acrylic monomers.Type: GrantFiled: August 30, 2000Date of Patent: February 26, 2002Assignee: E. I. du Pont de Nemours and CompanyInventors: Paul J. Fagan, George Yanwu Li, Zhibin Guan, Lin Wang
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Publication number: 20020002281Abstract: Novel compounds, N,N′-bis(phosphonomethyl)-N,N′-bis(hydroxycarbonylmethyl)urea and N,N,N′,N′-tetrakis(hydroxycarbonylmethyl)urea, suitable for use in preparing N-acyl aminocarboxylic acids that can be readily converted to N-(phosphonomethyl)glycine are provided. The compounds may be formed by the reaction of bis-(phosophonomethyl)urea or urea respectively with carbon monoxide and formaldehyde in the presence of a carboxymethylation catalyst precursor and solvent.Type: ApplicationFiled: June 1, 2001Publication date: January 3, 2002Inventors: Todd J. Johnson, Michael K. Stern, David A. Morgenstern, Michael D. Rogers, Yvette M. Fobian, Jeffrey A. Levine
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Publication number: 20010021705Abstract: Disclosed is a method for treating and preventing bone loss in patients by administering a formulation of 4-amino-1-hydroxy-butylidene-1,1-bisphosphonic acid, disodium salt, or its hydrates. Also described is a pharmaceutical composition containing said disodium salt in a pharmaceutically acceptable excipient.Type: ApplicationFiled: April 24, 2001Publication date: September 13, 2001Applicant: MERCK & CO., Inc.Inventors: Gerald S. Brenner, Earl R. Oberholtzer, J. Eric Thies
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Patent number: 6284923Abstract: The invention provides compounds, compositions and methods relating to novel electrophilic aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: August 22, 1997Date of Patent: September 4, 2001Assignee: Tularik INCInventors: Julio Cesar Medina, David Louis Clark, John A. Flygare, Terry J. Rosen, Bei Shan
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Patent number: 6232494Abstract: This invention is directed to an improved process for the preparation of N-(phosphonomethyl)glycine (i.e., “glyphosate”), a salt of N-(phosphonomethyl)glycine, or an ester of N-(phosphonomethyl)glycine. The process comprises combining an N-substituted N-(phosphonomethyl)glycine reactant with oxygen in the presence of a noble metal catalyst. The N-substituted N-(phosphonomethyl)glycine reactant has formula (V): wherein R1 and R2 are independently selected from the group consisting of hydrogen, halogen, —PO3R12R131, —SO3R14, —NO2, hydrocarbyl, and substituted hydrocarbyl other than —CO2R15; and R7, R8, R9, R12, R13, R14, and R15 are independently selected from the group consisting of hydrogen, hydrocarbyl, substituted hydrocarbyl, and an agronomically acceptable cation.Type: GrantFiled: March 5, 1999Date of Patent: May 15, 2001Assignee: Monsanto CompanyInventors: David A. Morgenstern, David E. McKenzie, Robert Orth, David Oburn, Cindy Ludwig, Kam-to Wan, John M. Dzenitis
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Patent number: 6160164Abstract: A description is given of compounds of the formula ##STR1## in which the general symbols are as defined in claim 1, and of their zirconium, bismuth and calcium salts, and of the salts with the compounds of the formula II ##STR2## in which the general symbols are as defined in claim 1, as corrosion inhibitors in coating compositions for protecting metallic surfaces.Type: GrantFiled: July 29, 1999Date of Patent: December 12, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Adalbert Braig, Andreas Kramer, Jean-Pierre Wolf, Markus Frey
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Patent number: 6096730Abstract: Phosphonic acid agents are synthesized and characterized which are potent inhibitors of angiogenesis, tumorigenesis and metalloproteinase activity. Their method of use for the inhibition of angiogenesis and metalloproteinase and the treatment of tumors is also shown.Type: GrantFiled: July 23, 1998Date of Patent: August 1, 2000Assignee: University of Kentucky Research FoundationInventors: Delwood C. Collins, Antonio R. Gagliardi, Peter Nickel
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Patent number: 6005083Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.Type: GrantFiled: March 28, 1997Date of Patent: December 21, 1999Assignee: NeoRx CorporationInventor: Sudhakar Kasina
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Patent number: 6005140Abstract: This invention is directed to process for making a composition having the formula (I): ##STR1## wherein R.sup.3, R.sup.4, and R.sup.5 are independently hydrogen, substituted or unsubstituted hydrocarbyl, or an agronomically acceptable cation. The process comprises contacting a solution with a noble metal catalyst and introducing oxygen into the solution. The solution contains an N-substituted glyphosate having the formula (II): ##STR2## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen, --PO.sub.3 H.sub.2, --SO.sub.3 H, --NO.sub.2, or substituted or unsubstituted hydrocarbyl other than --CO.sub.2 H. R.sup.3, R.sup.4, and R.sup.5 are as defined for formula (I).This invention also relates to an oxidation catalyst comprising a noble metal having a hydrophobic electroactive molecular species adsorbed thereon.Type: GrantFiled: February 12, 1998Date of Patent: December 21, 1999Assignee: Monsanto CompanyInventors: David A. Morgenstern, Yvette M. Fobian
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Patent number: 5985855Abstract: The present invention includes compositions and methods of treatment for glutamate abnormalities and associated nervous tissue insult in a animal by inhibition of NAALADase enzyme. Compositions include glutamate-derived hydroxyphosphinyl derivative compounds, acidic peptide analogs, phosphinic acid derivatives and mixtures thereof that inhibit NAALADase enzyme activity and their use for treating glutamate abnormalities such as created by global and focal ischemia.Type: GrantFiled: November 20, 1997Date of Patent: November 16, 1999Assignee: Guilford Pharmaceuticals Inc.Inventors: Barbara S. Slusher, Paul F. Jackson
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Patent number: 5968915Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme inhibitors which are proposed as novel agents for the treatment of prostate cancer. NAALADase is enzyme which is a membrane-bound metalloprotease which hydrolyzes the dipeptide, N-acetyl-L-aspartate-L-glutamate (NAAG) to yield glutamate and N-acetylaspartate. The compounds of the present invention include phosphinic acid derivatives that inhibit NAALADase enzyme activity and which have been found useful for inhibiting the growth of prostate cancer cells.Type: GrantFiled: April 8, 1997Date of Patent: October 19, 1999Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Barbara S. Slusher
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Patent number: 5962438Abstract: A novel estrogen derivative represented by the formula: ##STR1## is useful for treating or preventing diseases caused by estrogen deficiency.Type: GrantFiled: October 17, 1997Date of Patent: October 5, 1999Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Michihiro Yamamoto, Akira Sasaki, Takashi Katsumata, Naomi Tsushima, Hideyuki Harada
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Patent number: 5824662Abstract: The present invention includes compositions and methods of treatment for glutamate abnormalities and associated nervous tissue insult in a animal by inhibition of NAALADase enzyme. Compositions include glutamate-derived hydroxyphosphinyl derivative compounds, acidic peptide analogs, phosphinic acid derivatives and mixtures thereof that inhibit NAALADase enzyme activity and their use for treating glutamate abnormalities such as created by global and focal ischemia.Type: GrantFiled: September 27, 1996Date of Patent: October 20, 1998Assignee: Guilford Pharmaceuticals Inc.Inventors: Barbara S. Slusher, Paul F. Jackson
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Patent number: 5672592Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme inhibitors which are proposed as novel agents for the treatment of prostate cancer. NAALADase is enzyme which is a membrane-bound metalloprotease which hydrolyzes the dipeptide, N-acetyl-L-aspartate-L-glutamate (NAAG) to yield glutamate and N-acetylaspartate. The compounds of the present invention include phosphinic acid derivatives that inhibit NAALADase enzyme activity and which have been found useful for inhibiting the growth of prostate cancer cells.Type: GrantFiled: June 17, 1996Date of Patent: September 30, 1997Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Barbara S. Slusher
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Patent number: 5495042Abstract: A process for the purification of aminophosphonic acids under non-alkaline conditions is described. In particular, aminophosphonic acids are slurred in neutral or acidic water, heated to reflux, cooled and then filtered. Product purities approaching 100% are thus obtained.Type: GrantFiled: November 4, 1993Date of Patent: February 27, 1996Assignee: Cytogen CorporationInventors: Benjamin A. Belinka, Jr., Daniel J. Coughlin
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Patent number: 5466682Abstract: Compounds of formula (I) ##STR1## in which A is (CH.sub.2).sub.n in which n is 1-10, preferably 3 or 5, and R is the acyl group from a known anti-inflammatory agent, exhibit high anti-inflammatory activity. The mechanism of action is novel because they do not release the anti-inflammatory agent in the body but exhibit an activity superior to the activity of the known anti-inflammatory agent. The compounds are also active in combating bone calcium loss.Type: GrantFiled: July 26, 1993Date of Patent: November 14, 1995Assignee: Istituto Gentili S.p.A.Inventors: Sergio Rosini, Maurizio Mian
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Patent number: 5414112Abstract: Certain N-bis(phosphonomethyl) amino acids are novel compounds and are useful in preventing calcium carbonate scale.Type: GrantFiled: November 9, 1993Date of Patent: May 9, 1995Assignee: Nalco Chemical CompanyInventor: Vera Dragisich
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Patent number: 5405601Abstract: The present invention provides new and structurally diverse compositions for diagnostic imaging comprising compounds of the general formula: ##STR1## wherein A is N or CR.sub.1, R.sub.1 is hydrogen, C.sub.1 -C.sub.8 alkyl, or C.sub.6 -C.sub.10 aryl, where the alkyl or aryl group may be optionally substituted with one or more hydroxy, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 hydroxyalkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.6 -C.sub.10 aryl, C.sub.6 -C.sub.10 hydroxyaryl, C.sub.6 -C.sub.10 aryloxy, --CO.sub.2 R.sub.2, --CONR.sub.3 R.sub.4, or NR.sub.3 R.sub.4 ; D is O, --O(CH.sub.2).sub.2 O--, --O(CH.sub.2).sub.3 O--, or NR.sub.5 ; E is O, --O(CH.sub.2).sub.2 O--, --O(CH.sub.2).sub.3 O-- or NR.sub.6 ; F is O, --O(CH.sub.2).sub.2 O--, --O(CH.sub.2).sub.3 O-- or NR.sub.7 ; R.sub.2 -R.sub.7 are as defined within; g, h, i, j, k and m may be the same or different and are an integer from one to about six; X is --CO.sub.2 H, --PO.sub.3 H.sub.2, --SO.sub.3 H or --CONHOH.Type: GrantFiled: July 2, 1993Date of Patent: April 11, 1995Assignee: Mallinckrodt Medical Inc.Inventors: T. Jeffrey Dunn, Dennis A. Moore, Muthanadar Periasamy, Milorad M. Rogic, Rebecca A. Wallace, David H. White, Steven R. Woulfe
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Patent number: 5326906Abstract: The ampholytes are extracted from the reaction solution with a liquid cation exchanger which is immiscible with the acidic aqueous reaction solution, where the cation exchanger is dissolved in at least one organic solvent which is immiscible with water and forms an organic phase with the organic solvent. Subsequently the organic phase which is loaded with the ampholyte is separated from the reaction solution, and then the ampholytes are back-extracted from the organic phase with aqueous solvents. The product losses in the process are low, and the residual salt content is very low.Type: GrantFiled: January 10, 1992Date of Patent: July 5, 1994Assignee: Hoechst AktiengesellschaftInventors: Heribert Tetzlaff, Matthias Krull, Gernot Kremer, Christoph Porz
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Patent number: 5315035Abstract: The present invention is concerned with aniline derivatives of the general formula: ##STR1## wherein R.sub.1 is hydrogen or a lower alkyl or aryl, R.sub.2 is hydrogen or a lower alkyl which can be substituted by hydroxyl, amino carboxyl, lower alkoxycarbonyl, lower alkanoylamide lower alkyl or aryl or by a group of the structure ##STR2## is which R.sub.5 and R.sub.6 have the meanings given hereinafter, R.sub.3 is a hydrogen or halogen atom or a carboxyl group, R.sub.4 and R'.sub.4, which can be the same or different, are hydrogen or halogen, carboxyl or lower alkoxy or lower alkyl radicals which are preferably in the m-position, R.sub.5 is hydrogen or a lower alkyl and R.sub.Type: GrantFiled: December 23, 1991Date of Patent: May 24, 1994Assignee: Boehringer Mannheim GmbHInventors: Gunter Frey, Gerd Zimmermann