Chalcogen Attached Indirectly To The Phosphorus By Nonionic Bonding Patents (Class 562/23)
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Publication number: 20100145034Abstract: The present invention provides a method for selectively placing carbon nanotubes on a substrate surface by using functionalized carbon nanotubes having an organic compound that is covalently bonded to such carbon nanotubes. The organic compound comprises at least two functional groups, the first of which is capable of forming covalent bonds with carbon nanotubes, and the second of which is capable of selectively bonding metal oxides. Such functionalized carbon nanotubes are contacted with a substrate surface that has at least one portion containing a metal oxide. The second functional group of the organic compound selectively bonds to the metal oxide, so as to selectively place the functionalized carbon nanotubes on the at least one portion of the substrate surface that comprises the metal oxide.Type: ApplicationFiled: August 14, 2009Publication date: June 10, 2010Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Alina Afzali-Ardakani, Phaedon Avouris, James B. Hannon, Christian Klinke
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Patent number: 7691898Abstract: This invention related to a series of new phosphonic acid derivatives having anti-hyperphosphatemia activity. wherein: A is selected from —(CH2)n—, —CO—, —(CH2)n—CO—(CH2)m—, —(CH2)n—CS—(CH2)m— or a branched alkylene group, B ring and C ring are selected from a benzene ring, naphthalene ring, azulene ring or, heterocycle or fused heterocycle compound, D is —(CH2)(n+1)—, —(CH2)—O—(CH2)m—, —(CH2)—S(O)o—(CH2)m—, —CF3 or —(CH2)n—NR10—(CH2)m— wherein a D ring is connected with the carbon atom composing the C ring, E is selected from an oxygen atom or a sulfur atom, P is a phosphine atom, R1˜R7, wherein R1 and R2, R4 and R5 are joined together with neighbored carbon atom to form 5˜7 membered saturated or unsaturated hydrocarbon ring, or 5˜6 membered fused heterocycle, R1, R2 and R3 are not a hydrogen atom if the B ring is a benzene ring and may be the same or different and are substituents, R8 and R9 are may be the same or different and are substituents, R10 is an alkyl group, n and m are 0-10 and o is 0-2.Type: GrantFiled: October 5, 2005Date of Patent: April 6, 2010Assignee: Kotobuki Pharmaceutical Co., Ltd.Inventors: Hiroshi Tomiyama, Masayuki Yokota, Kazuo Tokuzaki, Ryoko Tomita
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Patent number: 7662313Abstract: This invention provides compositions and devices having structurally ordered nanostructures, as well as methods for producing structurally ordered nanostructures.Type: GrantFiled: September 4, 2003Date of Patent: February 16, 2010Assignee: NANOSYS, Inc.Inventors: Jeffery A. Whiteford, Mihai Buretea, Erik Scher, Steve Empedocles, Andreas Meisel
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Publication number: 20090240078Abstract: Multifunctional alcohols, polyols derived from cardanol containing at least 3 hydroxyl groups are disclosed. Such alcohols allow for synthesis of multifunctional crosslinkers such as acrylates, epoxies, and vinyl ethers and flame retardants such as >phosphates. The multifunctional alcohols or polyols can be used in polyurethanes and polycarbonates. The multifunctional crosslinkers can be used in optical coating and waveguide compositions to increase curing speed and crosslink density. The multifunctional phosphates can be used in flame resistant plastics as the highly pendant phosphorus containing phosphate non-halogen flame retardant additives.Type: ApplicationFiled: December 30, 2005Publication date: September 24, 2009Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Vadakkethonippurathu Sivankutty Nair Prasad, Chennakkattu Krishna Sadasivan Pillai
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Publication number: 20090239829Abstract: There are described compounds having the general formula (I) below and their pharmaceutically acceptable salts thereof, wherein E, X, m, q, R1, R2, n and ZBG have the meanings reported in the description useful, in therapy, as inhibitors of zinc metalloproteinases.Type: ApplicationFiled: July 25, 2007Publication date: September 24, 2009Applicant: BRACCO IMAGING SPAInventors: Armando Rossello, Elisabetta Orlandini, Aldo Balsamo, Laura Panelli, Elisa Nuti
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Patent number: 7572395Abstract: The present invention provides compositions (small molecules, oligomers and polymers) that can be used to modify charge transport across a nanocrystal surface or within a nanocrystal-containing matrix, as well as methods for making and using the novel compositions.Type: GrantFiled: May 16, 2005Date of Patent: August 11, 2009Assignee: Nanosys, IncInventors: Jeffery A. Whiteford, Mihai A. Buretea, Erik C. Scher
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Patent number: 7572393Abstract: The present invention provides polymeric compositions that can be used to modify charge transport across a nanocrystal surface or within a nanocrystal-containing matrix, as well as methods for making and using the novel compositions.Type: GrantFiled: August 26, 2004Date of Patent: August 11, 2009Assignee: Nanosys Inc.Inventors: Jeffery A. Whiteford, Mihai A. Buretea, Linh Nguyen, Erik Scher
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Publication number: 20090187019Abstract: The present invention relates to a new process for preparing diisopropyl {[1-(hydroxymethyl)-cyclopropyl]oxy}methylphosphonate (2), which is a key intermediate for synthesizing an antiviral (particularly, against hepatitis B virus) nucleoside analogue. The present invention also relates to new intermediates, and a process for preparing the antiviral nucleoside analogue from the compound (2) prepared according to the present invention.Type: ApplicationFiled: June 27, 2005Publication date: July 23, 2009Applicant: LG LIFE SCIENCE LTD.Inventors: Suk-Kyoon Yoon, Kun-Hye Nam, Sang-Who Lee, Won-Kyo Joung, Sang-Chul Choi, Ki-Kon Lee
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Publication number: 20090099355Abstract: The present invention relates to processes for the production of 4-(biphenylyl)azetidin-2-one phosphonic acid derivatives of formulaType: ApplicationFiled: May 25, 2006Publication date: April 16, 2009Applicant: MICROBIA, INC.Inventors: Stephen Antonelli, Timothy C. Barden, Peter Lee, Eduardo J. Martinez, Wayne C. Schairer, John J. Talley
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Publication number: 20090076299Abstract: The present invention relates to the use of phosphated 2-propylheptanol or a phosphated 2-propylheptanol alkoxylate as a hydrotrope in aqueous alkaline solutions for a C8-C18-alcohol alkoxylate containing 1-20 ethyleneoxy units. It also relates to a phosphated 2-propylheptanol alkoxylate per se, and an alkaline cleaning composition comprising a C8-C18-alcohol alkoxylate containing 1-20 ethyleneoxy units and phosphated 2-propylheptanol and/or a phosphated 2-propylheptanol alkoxylate as a hydrotrope. The cleaning compositions may be used for industrial cleaning of hard surfaces, for example for vehicle cleaning or machine dishwashing.Type: ApplicationFiled: November 10, 2008Publication date: March 19, 2009Applicant: Akzo Nobel N.V.Inventors: Mahnaz Company, Magnus Franck, Anette Thyberg
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Publication number: 20090012325Abstract: Methods of synthesizing phosphoric acid of combretastatin A-4, phosphoric acid of combretastatin A-4 derivatives, and trans-isomers thereof are disclosed.Type: ApplicationFiled: February 21, 2008Publication date: January 8, 2009Inventors: Ajith Manage, Richard Hallewell, Amanda Stewart
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Publication number: 20080306027Abstract: Combretastatin derivatives of formula (I), preparation and use thereof are disclosed, wherein: Rf is alkyl with 1-8 carbon atoms and 1-17 fluorine atoms, R is amino, substituted amino, hydroxyl, nitro, halo, alkyloxy, phosphate or amino acid side chain. Said derivatives have a capability to inhibit the polymerization of microtubules and are useful in treatment against tumor and neovascularization.Type: ApplicationFiled: November 22, 2006Publication date: December 11, 2008Applicant: Zhejiang Dade Pharmaceutical Group Co., Ltd.Inventors: Weiping Shen, Jianping Wang, Jianguo Wang, Feng Qian, Fei Wang, Hongmei Jin
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Patent number: 7438833Abstract: The present invention provides compositions (small molecules, oligomers and polymers) that can be used to modify charge transport across a nanocrystal surface or within a nanocrystal-containing matrix, as well as methods for making and using the novel compositions.Type: GrantFiled: May 16, 2005Date of Patent: October 21, 2008Assignee: Nanosys, Inc.Inventors: Jeffery A. Whiteford, Mihai A. Buretea, Erik C. Scher
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Publication number: 20080146708Abstract: The invention relates to salts of asymmetrically substituted bis(1-hydroxymethyl)phosphinic acids, of the formula (I) A-P(?O)(OX)—B ??(I) in which A is R1R2C(OH)— and B is R3R4C(OH)—, with the proviso that the respective groups R1R2C(OH)— and —C(OH)R3R4 are always different, and where R1, R2, R3, and R4 are hydrogen, alkyl, alkenyl, alkynyl, aralkyl, aryl and/or substituted aryl, and X is an element of the first main group, an element of the second main or transition group, an element of the third main or transition group, an element of the fourth main or transition group, an element of the eighth transition group and/or a nitrogen base.Type: ApplicationFiled: December 14, 2007Publication date: June 19, 2008Inventors: Harald Bauer, Werner Krause, Wiebke Maas
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Publication number: 20080119441Abstract: This invention related to a series of new phosphonic acid derivatives having anti-hyperphosphatemia activity. (I) [wherein: A is selected from —(CH2)n—, —CO—, —(CH2)n—CO—(CH2)m—, —(CH2)n—CS—(CH2)m— or branched alkylene group. B ring and C ring are selected from benzene ring, naphthalene ring, azulene ring or, heterocycle or fused heterocycle. D is —(CH2)(n+1)—, —(CH2)-O—(CH2)m—, —(CH2)—S(O)o—(CH2)m—, —CF3 or —(CH2)n—NR10—(CH2)m— (wherein: D ring is connected with the carbon atom composing C ring.) E is selected from oxygen atom or sulfur atom. P is phosphine atom. R1˜R7 (wherein R1 and R2, R4 and R5 are joined together with neighbored carbon atom to form 5˜7 membered saturated or unsaturated hydrocarbon ring, or 5˜6 membered fused heterocycle. R1, R2 and R3 are not hydrogen atom if B ring is benzene ring.) may be the same or different and are substituents. R8 and R9 are may be the same or different and are substituents. R10 is alkyl group. n and m are 0-10. o is 0-2.Type: ApplicationFiled: October 5, 2005Publication date: May 22, 2008Inventors: Hiroshi Tomiyama, Masayuki Yokota, Kazuo Tokuzaki, Ryoko Tomita
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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: 7053240Abstract: This invention relates to a process for producing a substantially pure disulfide compound of Formula II as disclosed herein, such as disodium 2,2?-dithiobis ethane sulfonate, by an efficient procedure from available, relatively inexpensive raw materials.Type: GrantFiled: December 17, 2004Date of Patent: May 30, 2006Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Koh Kawami, Osamu Tokuda, Yoshihide Niimoto
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Patent number: 6949206Abstract: The present invention provides compositions (small molecules, oligomers and polymers) that can be used to modify charge transport across a nanocrystal surface or within a nanocrystal-containing matrix, as well as methods for making and using the novel compositions.Type: GrantFiled: September 4, 2003Date of Patent: September 27, 2005Assignee: Nanosys, Inc.Inventors: Jeffery A. Whiteford, Mihai A. Buretea, Erik Scher
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Patent number: 6924390Abstract: Compounds useful as surface coating agents, including compounds of the formula: wherein X1 comprises a first photoreactive species; X2 comprises a second photoreactive species; Y comprises a nonpolymeric core molecule comprising an aromatic group; and Z comprises at least one charged group. The Y core can include an aromatic group such as a benzene radical, the charged groups Z can be independently selected from the organic acids that include sulfonic acid, carboxylic acid, and phosphoric acid, and the photoreactive species of X1 and X2 can independently be aryl ketones, such as those selected from the group acetophenone, benzophenone, anthraquinone, anthrone, and anthrone-like heterocycles, and their substituted derivatives.Type: GrantFiled: July 14, 2003Date of Patent: August 2, 2005Assignee: SurModics, Inc.Inventor: Dale G. Swan
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Patent number: 6919322Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.Type: GrantFiled: March 7, 2001Date of Patent: July 19, 2005Assignee: Metabasis Therapeutics, Inc.Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy
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Patent number: 6891057Abstract: Novel compounds comprising a C—C double bond substituted at one carbon with two oxygen or sulfur atom-containing groups are disclosed. The compounds are useful in methods and compositions for generating chemiluminescence by reaction with a peroxidase enzyme and a peroxide. The chemiluminescence thus produced can be used as a detectable signal in assays for peroxidase enzymes and in assays employing enzyme-labeled specific binding pairs.Type: GrantFiled: January 9, 2004Date of Patent: May 10, 2005Assignee: Lumigen, Inc.Inventors: Hashem Akhavan-Tafti, Zahra Arghavani, Renuka DeSilva
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Patent number: 6852878Abstract: Thioketals and thioethers are provided that inhibit the expression of VCAM-1, and which can be used in the treatment of VCAM-1 mediated diseases including inflammatory disorders, cardiovascular diseases, occular diseases, autoimmune diseases, neurological disorders, and cancer. The compounds also can be used to treat hyperlipidemia and/or hypercholesterolemia.Type: GrantFiled: March 21, 2001Date of Patent: February 8, 2005Assignee: Atherogenics, Inc.Inventors: Charles Q. Meng, Lee K. Hoong, Patricia K. Somers
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Publication number: 20040249195Abstract: Lithium p-diarylphosphinobenzenesulfonates represented by the general formula (I) 1Type: ApplicationFiled: December 8, 2003Publication date: December 9, 2004Inventors: Tomoaki Tsuji, Masayuki Matsumoto, Shigeaki Suzuki
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Publication number: 20040043969Abstract: A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.Type: ApplicationFiled: April 1, 2003Publication date: March 4, 2004Inventors: Kevin G. Pinney, Vani P. Mocharla, Zhi Chen, Charles M. Garner, Anjan Ghatak, Mallinath Hadimani, Jimmy Kessler, James M. Dorsey, Klaus Edvardsen, David J. Chaplin, Joseph Prezioso, Usha R. Ghatak
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Patent number: 6603040Abstract: Compounds useful as surface coating agents, including compounds of the formula: wherein X1 comprises a first photoreactive species; X2 comprises a second photoreactive species; Y comprises a nonpolymeric core molecule comprising an aromatic group; and Z comprises at least one charged group. The Y core can include an aromatic group such as a benzene radical, the charged groups Z can be independently selected from the organic acids that include sulfonic acid, carboxylic acid, and phosphoric acid, and the photoreactive species of X1 and X2 can independently be aryl ketones, such as those selected from the group acetophenone, benzophenone, anthraquinone, anthrone, and anthrone-like heterocycles, and their substituted derivatives.Type: GrantFiled: June 25, 2001Date of Patent: August 5, 2003Assignee: SurModics, Inc.Inventor: Dale G. Swan
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Patent number: 6504049Abstract: A process for synthesizing pharmaceutically active disulfides, particularly Dimesna and certain derivatives thereof. The process includes reacting an alkylene salt with a sulfurating reagent, then alkalizing the intermediate and flowing oxygen through the mixture to produce the final compound in high yield.Type: GrantFiled: April 30, 2002Date of Patent: January 7, 2003Assignee: BioNumerik Pharmaceuticals, Inc.Inventor: Harry Kochat
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Patent number: 6486142Abstract: The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and conditions related to diabetes.Type: GrantFiled: December 21, 2000Date of Patent: November 26, 2002Assignee: Merck Frosst Canada & Co.Inventors: Yves Leblanc, Claude Dufresne, Jacques Yves Gauthier, Cheuk Kun Lau, Chun Sing Li, Patrick Roy, Michel Therien, John Scheigetz, Zhaoyin Wang
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Patent number: 6486141Abstract: The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related conditions.Type: GrantFiled: December 21, 2000Date of Patent: November 26, 2002Assignee: Merck Frosst Canada & Co.Inventors: Cheuk Kun Lau, Christopher Bayly, Jacques Yves Gauthier, Yves Leblanc, Chun Sing Li, Patrick Roy, Michel Therien, Zhaoyin Wang
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Patent number: 6465687Abstract: Novel thyroid receptor ligands are provided which have the general formula (I) where R1 is alkyl of 1 to 4 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 3 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; n is an integer from 0 to 4; R4 is an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid ester thereof, alkenyl carboxylic acid or ester thereof, hydroxy, halogen, cyano, or a phosphonic acid or an ester thereof, or a pharmaceutically acceptible salt thereof. A method for treating diseases associated with metabolism dysfunction or which are dependent on the expression of a T3 regulated gene, such as obesity, hypercholesterolemia, osteoporosis, hypothyroidism, and goiter, is also provided.Type: GrantFiled: March 20, 2000Date of Patent: October 15, 2002Assignee: Karo Bio ABInventors: Yi-Lin Li, Ye Liu, Asa Hedfors, Johan Malm, Charlotta Mellin, Minsheng Zhang
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Patent number: 6410782Abstract: Diphosphonates or their salts between acids and linear, branch substituted and non-substituted, cyclic, heterocyclic and aromatic amino alcohols are used to treat osteoporosis. Pharmaceutical compositions and therapeutic methods of treating osteoporosis are described.Type: GrantFiled: April 3, 2000Date of Patent: June 25, 2002Assignees: Geange Ltd., Eurodrug Ltd., Lipotec SAInventors: Fred VanGulik, Antonio Parente
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Patent number: 6399814Abstract: An improved hydrolysis process comprising a process for the preparation of 2-carboxyalkyl(aryl)phosphinic acid using a controlled addition of water to an acrylation reaction mixture, and control of the temperature. Preparation of 2-carboxyalkyl(aryl)phosphinic acid cyclic anhydride is disclosed using a controlled addition of water, wherein up to about one mole of water per mole of dichloro(aryl)-phosphine charged to the acrylation reaction is added, and temperature is controlled.Type: GrantFiled: March 20, 2000Date of Patent: June 4, 2002Assignee: Solutia Inc.Inventors: David J. Weinkauff, Frank E. Paulik
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Patent number: 6355833Abstract: A catalyst comprising at least one nickel(O) complex which comprises at least one mono-, bi- or multidentate phosphonite ligand of the formula I or salts and mixtures thereof, is prepared as described, and the catalysts are used to prepare mixtures of monoolefinic C5 mononitriles with nonconjugated C═C and C≡N bonds by catalytic hydrocyanation of butadiene or of a 1,3-butadiene-containing hydrocarbon mixture in the presence of a catalyst of this type.Type: GrantFiled: February 14, 2001Date of Patent: March 12, 2002Assignee: BASF AktiengesellschaftInventors: Jakob Fischer, Wolfgang Siegel
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Publication number: 20020016497Abstract: Water-soluble sulfonated organophosphorus compounds are purified by at least partially removing contaminating sulfite values therefrom, by decreasing the pH of a solution of such sulfonated organophosphorus compounds to a value of less than or equal to 4, and maintaining the pH of the solution at this value of 4 or less for such period of time as to reduce the weight concentration of sulfite in the solution to less than 100 ppm; the organophosphorus compounds thus purified are well suited for the two-phase cocatalysis of a wide variety of organic reactions.Type: ApplicationFiled: June 25, 2001Publication date: February 7, 2002Inventors: Larbi Aouni, Paolo Burattin, Pierre Coqueret, Marc Huser
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Patent number: 6303674Abstract: Aluminum salts of alkylhydroxymethylphosphinic acids are prepared by reacting phosphonous acids with aluminum hydroxide or paraformaldehyde or trioxane or mixtures thereof in water at 110 to 250° C. under pressure. The resulting aluminumphosphinates are incorporated into polymers, in particular into polyesters, and have a flame retardant action therein.Type: GrantFiled: December 6, 1999Date of Patent: October 16, 2001Assignee: Ticona GmbHInventor: Hans-Jerg Kleiner
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Publication number: 20010025084Abstract: A substrate for solid phase synthesis comprising a solid phase-linker combination of the formula I is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediates useful therein. Among the novel intermediates are compounds of the formula II wherein R1 is —NO2 or —CHO; R2 is —OCH3, —CHO or —H; R3 is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n=1 or 3-12.Type: ApplicationFiled: January 22, 2001Publication date: September 27, 2001Inventors: Vinh D. Tran, Vu Van Ma, Ruiyan Liu
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Patent number: 6245754Abstract: The present invention relates to the preparation and biological activity of 3-deoxy-D-myo-inositol ether lipid analogs as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth. The compounds of the present invention are useful as anti-tumor agents which effectively inhibit the growth of mammalian cells.Type: GrantFiled: June 25, 1999Date of Patent: June 12, 2001Inventors: Alan P. Kozikowski, Lixin Qioa, Garth Powis
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Patent number: 6242433Abstract: The present invention relates to novel geranylgeranyl derivatives and the pharmaceutically acceptable salts thereof having antiproliferative activity in eukaryotic cells with respect to the inhibition of protein geranygeranylation. The invention also relates to the pharmaceutical compositions containing the novel derivatives and to the process of preparation thereof.Type: GrantFiled: September 15, 1998Date of Patent: June 5, 2001Assignee: Laboratori Baldacci SpAInventors: Aldo Balsamo, Bruno Macchia, Marco Macchia, Massimo Baldacci, Romano Danesi, Mario Del Tacca
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Patent number: 6229044Abstract: Aluminum salts of alky-(1-alkoxyethyl)phosphinic acids are prepared by reacting alky-(1-alkoxyethyl)phospihnic acids with aluminum hydroxide in a molar ratio of 3:1. The resulting aluminum phosphinates are used as flame retardants in thermoplastics, particularly in polyesters.Type: GrantFiled: November 17, 1999Date of Patent: May 8, 2001Assignee: Ticona GmbH Deutschland KGInventors: Hans-Jerg Kleiner, Elke Jenewein, Wolfgang Wanzke
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Patent number: 6174874Abstract: The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases.Type: GrantFiled: September 17, 1999Date of Patent: January 16, 2001Assignee: Merck Frosst Canada & Co.Inventors: Zhaoyin Wang, Claude Dufresne, Yves Leblanc, Chun Sing Li, Jacques Y. Gauthier, Cheuk K. Lau, Michel Therien, Patrick Roy
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Patent number: 6160166Abstract: 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 21, 1999Date of Patent: December 12, 2000Assignee: The University of Kentucky Research FoundationInventors: Delwood C. Collins, Antonio R. Gagliardi, Peter Nickel
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Patent number: 6107506Abstract: In the coexistence of an a 5.about.20 molar excess of water based upon 2-phenylphenol compound which is reacted with phosphorus trihalide to form a 6-halo-(6H)-dibenzo[c.e][1,2]-oxaphosphorin compound and an organic solvent which is unsoluble in water and is inert in the reaction system, an organic phosphorus compound expressed by the structural formula (1) is hydrolyzed under heating to obtain a biphenyl phosphorus compound expressed by the general formula (2) and then, a cyclising dehydration reaction under heating of the resulting compound is carried out to obtain an organic phosphorus compound expressed by the structural formula (3). This constitution can produce a product of high purity and high quality without using specific chemicals or an equipment made of specific materials.Type: GrantFiled: April 23, 1998Date of Patent: August 22, 2000Inventors: Toranosuke Saito, Takumi Hirayama, Yukinori Kohguchi
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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: 6090345Abstract: The present invention relates to phosphorus-containing compounds based on 1-hydroxypropane-1,3-diphosphonic acid and to the acid itself of general formula (I) ##STR1## in which M.sup.1, M.sup.2, M.sup.3, M.sup.4 and M.sup.5, independently of one another, each denote a radical from the series hydrogen, alkali metal, an equivalent of ammonium, alkyl- or hydroxyalkyl-substituted ammonium,a process for the preparation thereof, novel intermediates and the use thereof as a corrosion inhibitor, scale inhibitor and as a flame retardant.Type: GrantFiled: January 29, 1999Date of Patent: July 18, 2000Assignee: Bayer AGInventors: Christoph Holzner, Armin Spaniol, Hans Dahmen
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Patent number: 6031091Abstract: A versatile reagent with a non-nucleotide monomeric unit having a ligand, and first and second coupling groups which are linked to the non-nucleotide monomeric unit. The ligand can be either a chemical moiety, such as a label or intercalator, or a linking arm which can be linked to such a moiety. Such reagent permits preparation of versatile nucleotide/non-nucleotide polymers, having any desired sequence of nucleotide and non-nucleotide monomeric units, each of the latter of which bear a desired ligand. These polymers can for example, be used as probes which can exhibit enhanced sensitivity and/or which are capable of detecting a genus of nucleotides each species of which has a common target nucleotide sequence of interest bridged by different sequences not of interest.Type: GrantFiled: August 7, 1997Date of Patent: February 29, 2000Assignee: Gen-Probe IncorporatedInventors: Lyle J. Arnold, Jr., Mark A. Reynolds, Ram S. Bhatt
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Patent number: 5861385Abstract: Substituted triols are prepared by reducing appropriately substituted carboxylic esters. The substituted triols can be used as active substances in medicaments.Type: GrantFiled: August 8, 1995Date of Patent: January 19, 1999Assignee: Bayer AktiengesellschaftInventors: Rolf Angerbauer, Peter Fey, Walter Hubsch, Thomas Philipps, deceased, Hilmar Bischoff, Hans-Peter Krause, Jorg Petersen von Gehr, Delf Schmidt
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Patent number: 5840963Abstract: Novel methods and compositions which generate chemiluminescence are provided. The compositions comprise a heterocyclic enol phosphate compound and a dihydroxyaromatic compound in which the two hydroxy groups are separated by an even number of ring carbon atoms. Novel methods and compositions for generating chemiluminescence by reaction with a hydrolytic enzyme are provided as well. The compositions comprise a heterocyclic enol phosphate compound and a protected dihydroxyaromatic compound in which one of the hydroxy groups of the dihydroxyaromatic compound is protected with an enzyme-cleavable group. The novel chemiluminescent compositions are useful in methods for producing chemiluminescence for use in assays of hydrolytic enzymes and enzyme inhibitors and in assays employing labeled specific binding pairs.Type: GrantFiled: February 10, 1998Date of Patent: November 24, 1998Assignee: Lumigen, Inc.Inventor: Hashem Akhavan-Tafti
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Patent number: 5821376Abstract: The invention relates to a process for the preparation of 2'-hydroxydiphenyl-2-phosphinic acid in the form of a commercial mixture with 6-hydroxy-(6H)-dibenzo-(c,e)(1,2)-oxaphosphorine, the process being carried out on a commercial scale, more simply and more cheaply than previously, as a one-pot reaction without isolating intermediate products and avoiding a distillation step, with said process comprising the steps:(a) o-phenylphenol is added to a mixture of PCl.sub.3 and a Lewis acid as a catalyst while simultaneously heating the reaction mixture, and the reaction mixture is then fluxed;(b) the resulting reaction mixture is allowed to cool and, stirring continuously, is hydrolysed, being mixed first with water and then with a low alkanol;(c) next, the product is crystallised during further stirring, and(d) the crystalline product obtained is sucked off, washed and dried.Type: GrantFiled: October 24, 1997Date of Patent: October 13, 1998Assignee: Schill & Seilacher GmbH & Co.Inventors: Paul Rathfelder, Horst Rieckert, Jorg Dietrich
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Patent number: 5739374Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: February 14, 1997Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5731299Abstract: The present invention relates to phosphonsulfonates and the pharmaceutically-acceptable salts and esters thereof, having the following structure according to formula (I): ##STR1## The present invention further relates to pharmaceutical compositions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients. Finally, the present invention relates to methods for treating or preventing pathological conditions characterized by abnormal calcium and phosphate metabolism in humans or other mammals, including treating or preventing osteoporosis and arthritis, especially rheumatoid arthritis and osteoarthritis. This method comprises administering to a human or other mammal in need of such treatment of a safe and effective amount of a compound or composition of the present invention.Type: GrantFiled: May 7, 1993Date of Patent: March 24, 1998Assignee: The Procter & Gamble CompanyInventors: Frank Hallock Ebetino, Allan Vincent Bayless, Susan Mary Dansereau
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Patent number: 5712396Abstract: .alpha.-Phosphonosulfonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is H, alkyl, arylalkyl or aryl; R4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.Type: GrantFiled: July 5, 1994Date of Patent: January 27, 1998Inventors: David R. Magnin, Scott A. Biller, John K. Dickson, Jr., R. Michael Lawrence, Richard B. Sulsky