Carboxamide, Cyano, Or Isocyanate Containing Patents (Class 554/112)
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Patent number: 8816095Abstract: Disclosed are molecules and their synthesis, for use in blocking gated ion channels such as voltage-gated sodium channels (VGSCs) and prostate voltage sodium channels (PVSCs). These inhibitors have superior blocking efficacy, for instance in displacing the radioligand [3H]-Batrachotoxin-B ([3H]-BTX-B) that binds to site 2 of a VGSC. The molecules of the invention comprise a moiety which increases the binding affinity of molecules for the protein binding site in prostate cancer cells (PCs), and which is also fluorescent. In one embodiment the invention molecules are an inhibition system that can be used to target over-abundant or hyperactive VGSCs selectively in pain, epilepsy or prostate cancer, inhibiting the proliferation of PCs. The fluorescent moiety also facilitates screening, tracking, and pharmacodynamic studies of the drug in a biological system both in vitro and in vivo.Type: GrantFiled: August 17, 2009Date of Patent: August 26, 2014Assignee: Georgetown UniversityInventors: Milton L. Brown, Scott Grindrod, Thomas H. Walls, Todd Hansen, Simeng Suy, Mikell A. Paige
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Publication number: 20130232860Abstract: The present invention relates to alkanolamide-containing compositions, and more particularly to alkanolamide-containing compositions formed by the reaction of a fatty acid and diethanolamine (DEA) which contain low levels of undesirable by-products. Such compositions are particularly suitable for use as fuel additives.Type: ApplicationFiled: April 22, 2013Publication date: September 12, 2013Applicant: AFTON CHEMICAL CORPORATIONInventors: William J. Colucci, Abbas Kadkhodayan
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Patent number: 8435410Abstract: A method for making a surfactant-based monolithic column is provided. The method comprises providing a mixture comprising at least one surfactant monomer, at least one crosslinker, at least one initiator, and at least one porogen and polymerizing the mixture to form the surfactant-based monolithic column. The present disclosure also provides a surfactant-based monolithic column, a method for separating molecules, and a process for preparing a surfactant monomer.Type: GrantFiled: March 30, 2009Date of Patent: May 7, 2013Assignee: Georgia State University Research Foundation, Inc.Inventors: Shahab Ahmed Shamsi, Congying Gu, Jun He
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Patent number: 8304565Abstract: New diacylglycerol-polyethylene glycol (DAG-PEG) conjugates are described. A variety of linkers between the PEG chain and glycerol backbone of the DAG-PEGs may be selected to optimize liposomal formulations of pharmaceuticals and cosmetics.Type: GrantFiled: June 10, 2009Date of Patent: November 6, 2012Inventors: Nian Wu, Brian Charles Keller
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Publication number: 20120137930Abstract: A composition and processes for the reduction of the tendency to baking, moisture absorption and/or dust formation of a granulate being susceptible therefore, such as fertilizers, minerals, ores, as well as to obtain stable coloring dispersions, density control of cokes and the reduction of foam in industrial processes, wherein synthetic polymers of fatty alkyl compounds, especially fatty acid esters and fatty-alcohols, fatty amines, fatty amides and fatty ethers, or distillation residues of the original monomers themselves, can be used, are disclosed. The distillation residues are preferably derived from the bottom fraction, obtained by distillation of the fraction being suitable as biodiesel during the biodiesel production process.Type: ApplicationFiled: June 15, 2009Publication date: June 7, 2012Applicant: Holland Novochem B.V.Inventors: Erik Alexander Bijpost, Alexander Maslow, Jacobus Gerardus Korver
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Publication number: 20110230442Abstract: Disclosed are molecules and their synthesis, for use in blocking gated ion channels such as voltage-gated sodium channels (VGSCs) and prostate voltage sodium channels (PVSCs). These inhibitors have superior blocking efficacy, for instance in displacing the radioligand [3H]-Batrachotoxin-B ([3H]-BTX-B) that binds to site 2 of a VGSC. The molecules of the invention comprise a moiety which increases the binding affinity of molecules for the protein binding site in prostate cancer cells (PCs), and which is also fluorescent. In one embodiment the invention molecules are an inhibition system that can be used to target over-abundant or hyperactive VGSCs selectively in pain, epilepsy or prostate cancer, inhibiting the proliferation of PCs. The fluorescent moiety also facilitates screening, tracking, and pharmacodynamic studies of the drug in a biological system both in vitro and in vivo.Type: ApplicationFiled: August 17, 2009Publication date: September 22, 2011Applicant: GEORGETOWN UNIVERSITYInventors: Milton L. Brown, Scott Grindrod, Thomas H. Walls, Todd Hansen, Simeng Suy, Mikell A. Paige
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Publication number: 20110086409Abstract: A method for making a surfactant-based monolithic column is provided. The method comprises providing a mixture comprising at least one surfactant monomer, at least one crosslinker, at least one initiator, and at least one porogen and polymerizing the mixture to form the surfactant-based monolithic column. The present disclosure also provides a surfactant-based monolithic column, a method for separating molecules, and a process for preparing a surfactant monomer.Type: ApplicationFiled: March 30, 2009Publication date: April 14, 2011Inventors: Shahab Ahmed Shamsi, Jun He, Congying Gu
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Publication number: 20100279959Abstract: A composition and method for promoting neutrophil survival and activation such as the treatment of neutropenia arising as an undesirable side effect of chemotherapy and radiation therapy. A composition containing medium-chain fatty acids, such as Capri acid or caprylic acid, or salts or triglycerides thereof, or mono- or diglycerides or other analogues thereof or medium-chain triglycerides (MCT) is administered to a human or animal needing treatment in an amount sufficient to reduce or eliminate neutropenia. The composition is administered in an amount effective to treat the disorder. The methods are also useful in the management of bone narrow transplantation and in the treatment of various neutropenic diseases.Type: ApplicationFiled: June 11, 2010Publication date: November 4, 2010Inventors: Lyne Gagnon, Jean Barabe, Pierre Laurin, Christopher Penney, Boulos Zacharie
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Publication number: 20100203637Abstract: The preparation and use of fluorescent cell markers of the structure F—S1-S2-L is described where F is a fluorophore, S1-S2 is a spacer linking F to L, and L is a diacyl lipid.Type: ApplicationFiled: September 6, 2007Publication date: August 12, 2010Inventors: Elena Korchagina, Nicolai Bovin, Stephen Henry
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Publication number: 20100076209Abstract: New diacylglycerol-polyethylene glycol (DAG-PEG) conjugates are described. A variety of linkers between the PEG chain and glycerol backbone of the DAG-PEGs may be selected to optimize liposomal formulations of pharmaceuticals and cosmetics.Type: ApplicationFiled: June 10, 2009Publication date: March 25, 2010Inventors: Nian Wu, Brian Charles Keller
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Patent number: 7115663Abstract: Cyanophenoxy carboxylic acid compounds and compositions for the delivery of active agents are provided. Methods of administration, treatment of disease and preparation are provided as well.Type: GrantFiled: September 5, 2001Date of Patent: October 3, 2006Assignee: Emisphere Technologies, Inc.Inventors: Destardi Moye-Sherman, David Gschneider
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Patent number: 6921747Abstract: The present invention provides a basic amino acid derivative represented by the formula (1): The present invention also provides a method of making a gelled product by employing the aforementioned compound, as well as a gel, perfumery, and/or cosmetic containing the same.Type: GrantFiled: February 13, 2004Date of Patent: July 26, 2005Assignee: Ajinomoto Co., Inc.Inventors: Kenji Hanabusa, Masahiro Suzuki
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Patent number: 6696606Abstract: A solid phase synthetic method for preparing arylretinamides is provided. The method comprises reacting hexachloroacetone with a solvent-suspended resin-bound triphenylphosphine to provide a suspension comprising an activated chlorinating reagent; reacting retinoic acid with the activated chlorinating reagent to provide retinoyl chloride; adding pyridine and a select arylamine to the resulting mixture; and stirring the resulting mixture for a time and at a temperature sufficient for the select arylamine to react with the retinoyl chloride and provide the arylretinamide. Also provided, are select arylretinamides that can be prepared by the present method, and methods of using such arylretinamides to induce apoptosis in cancer cells.Type: GrantFiled: July 8, 2002Date of Patent: February 24, 2004Assignee: The Ohio State University Research FoundationInventors: Robert W. Curley, Jr., Serena M. Mershon
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Patent number: 6455715Abstract: A method is described for producing saturated dicarboxylic acids with a chain length of C6 to C21 or the corresponding diamidic dicarboxylic acids from fatty acid cleavage of unsaturated fatty acids or the bis-fatty acid diamides of these unsaturated fatty acids by oxidative ozonolysis and subsequent separation and purification of the dicarboxylic acids, whereby after oxidative ozonolysis, the reaction products are dissolved at a high temperature in a carboxylic acid or a mixture of several carboxylic acids with a medium chain length of C6 to C12 or esters of short-chain alcohols of these carboxylic acids as the recrystallization solvent.Type: GrantFiled: October 24, 2001Date of Patent: September 24, 2002Assignee: Dr. Frische GmbHInventors: Rainer Frische, Katja Hegwein, Jürgen Volkheimer
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Patent number: 6090958Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: February 7, 1997Date of Patent: July 18, 2000Assignee: Emisphere Technologies, Inc.Inventors: Andrea Leone-Bay, Koc-Kan Ho, Donald J. Sarubbi, Harry R. Leipold
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Patent number: 6071510Abstract: The present invention provides modified amino acids for delivering active agents, and particularly biologically or chemically active agents. The preferred modified amino acids of the present invention include N-acylated or sulfonated amino acids. These modified amino acids are used as carriers to facilitate the delivery of a cargo to a target. Such modified amino acids are well suited to form non-covalent mixtures with biologically-active agents for oral administration to animals. Methods for the preparation and administration of the modified amino acids and compositions including the same are also provided.Type: GrantFiled: April 23, 1997Date of Patent: June 6, 2000Assignee: Emisphere Technologies, Inc.Inventors: Andrea Leone-Bay, Koc-Kan Ho, Jeffery Bruce Press, Nai-Fang Wang
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Patent number: 6060513Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: February 7, 1997Date of Patent: May 9, 2000Assignee: Emisphere Technologies, Inc.Inventors: Andrea Leone-Bay, Eric Wang, Donald J. Sarubbi, Harry R. Leipold
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Patent number: 5962710Abstract: A method for preparing salicyloylamino acids is provided. An oligosalicylate and an amino acid are reacted to yield the salicyloylamino acid.Type: GrantFiled: May 9, 1997Date of Patent: October 5, 1999Assignee: Emisphere Technologies, Inc.Inventors: David Gschneidner, Doris O'Toole, John Freeman
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Patent number: 5773465Abstract: Tartronic acid acetalic ethers and esters of the general formula: ##STR1## are provided and are useful in treatment of bone dysmetabolism. As examples, Ra and Rb may be hydrogen, B is a C.sub.2 -C.sub.12 acyl group, R is phenyl and n is 0-12.Type: GrantFiled: March 12, 1997Date of Patent: June 30, 1998Assignee: Dompe Farmaceutici S.p.A.Inventors: Carmelo A. Gandolfi, Lorella Cotini, Marco Mantovanini, Gianfranco Caselli, Gaetano Clavenna, Claudio Omini
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Patent number: 5576416Abstract: A new epoxy hardener composition is the product of the reaction of (A) a poly(alkylene oxide) monoamine or diamine with a molecular weight (Mn) of about 500 to 3000 and (B) a di- or polycarboxylic acid, in a ratio of moles of carboxylic acid to equivalents of amine of about 1:1 to 6:1 to yield an intermediate (C), which in a second step is reacted with (D) a di- or polyamine. The compositions of the invention are excellent emulsifiers of liquid epoxy resins in aqueous media without the addition of added surfactants or acidic compounds, and can be used to prepare water resistant water-borne coatings and related products from both liquid and solid epoxy resins, that possess long pot lives and contain relatively small amounts of volatile organic compounds.Type: GrantFiled: December 13, 1994Date of Patent: November 19, 1996Assignee: Air Products and Chemicals, Inc.Inventor: Frederick H. Walker
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Patent number: 5559268Abstract: A process for the preparation of N-substituted dehydroamino acid esters by contacting a .beta.-hydroxy-.alpha.-amino acid ester or N- or O-substituted .beta.-hydroxy-.alpha.-amino acid ester with an excess of acetic anhydride and a base is disclosed.Type: GrantFiled: November 17, 1994Date of Patent: September 24, 1996Assignee: E. I. Du Pont de Nemours and CompanyInventor: William A. Nugent
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Patent number: 5380894Abstract: A process for the production of hydroxy fatty acids and novel estolide compounds, each of which may be used as lubricants, greases, plasticizers and printing inks, as well as in cosmetics. The estolides are of the formula (I): ##STR1## wherein R.sub.1 is selected from C.sub.6 -C.sub.16 hydrocarbons which may be saturated or unsaturated, and branched or straight chain, and optionally substituted, such as with one or more hydroxy groups; R.sub.2 is independently selected from C.sub.2 -C.sub.17 hydrocarbons which may be saturated or unsaturated, and branched or straight chain, and optionally substituted, such as with one or more hydroxy groups; A is selected from C.sub.3 -C.sub.14 hydrocarbons which may be saturated or unsaturated, and branched or straight chain, and optionally substituted; n is greater than or equal to 1; y is an integer from 3-13; x is 1 or 2; and . . . designates a single or double carbon/carbon bond.Type: GrantFiled: March 1, 1991Date of Patent: January 10, 1995Assignee: The United States of America as represented by the Secretary of AgricultureInventors: Douglas A. Burg, Robert Kleiman, Selim M. Erhan
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Patent number: 5292915Abstract: The invention relates to compounds containing carbonate groups and carbonyl groups and having the general formula ##STR1## in which R stands for a C.sub.1 -C.sub.4 -alkyl radical, an aryl radical, or a radical R.sup.1, whereR.sup.1 has the following formula ##STR2## in which R.sup.2 to R.sup.6 stand for H, alkyl, OH, O-alkyl, SH, S-alkyl, halogen, N(alkyl).sub.2, or N(alkyl)(aryl) and at least one but not more than three of the radicals R.sup.2 to R.sup.6 stand for a radical of the formula ##STR3## in which A, B and C stand for alkylene, cycloalkylene, oxaalkylene, polyoxaalkylene or arylene, k and l both stand for an integer from 1 to 80, and the end group Z stands for alkyl, aryl, alkoxycarbonyl, alkoxycarbonyloxy, or aryl.These compounds are suitable for use as emulsifiers for dispersions.Type: GrantFiled: February 4, 1992Date of Patent: March 8, 1994Assignee: BASF AktiengesellschaftInventors: Andreas Boettcher, Manfred Schwartz
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Patent number: 5266576Abstract: The invention relates to a compound of formula (I): ##STR1## which can be used as N-myristoyltransferase inhibitors, in which R.sub.1 represents hydrogen, substituted or unsubstituted (C.sub.1 -C.sub.6) alkyl, substituted or unsubstituted phenyl, (C.sub.3 -C.sub.7) cycloalkyl methyl, substituted or unsubstituted (imidazolyl-2-yl)methyl, substituted or unsubstituted (indol-3-yl)methyl or (1-azaindolizin-2-yl)methyl,R.sub.2, R.sub.3, which are identical or different, represent hydrogen or (Cl-C6) alkyl,or when R.sub.1 represents hydrogen, R.sub.2 and R.sub.3 form with the carbon and nitrogen atoms to which they are attached, a mono-, bi- or tricyclic heterocycle,X represents --CO--, --SO.sub.2 --, --PO(OH)--,Y represents --COR.sub.5 or --POR.sub.6 R.sub.6 ',R.sub.4 represents substituted or unsubstituted, linear or branched (C.sub.6 -C.sub.Type: GrantFiled: February 10, 1992Date of Patent: November 30, 1993Assignee: Adir et CompagnieInventors: Michel Vincent, Georges Remond, Bernard Portevin, Jean-Albert Boutin, Ghanem Atassi
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Patent number: 5252706Abstract: A peptide derivative amphiphatic compound or N-terminal salt thereof represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2 each represents a straight-chain or branched alkyl or acyl group having 8 to 24 carbon atoms optionally having a substituent or an unsaturated group; X represents --O--or --NH--; R.sup.3n and R.sup.3(n+1) each represents an .alpha.--amino acid side chain; n is an integer of from 0 to 5; the compound may be a racemic compound or an optically active compound when the compound has an asymmetric carbon atom; and the N-terminal salt of the compound optionally forms with an acid component; an intermediate thereof, a liposome comprising said peptide derivative amphiphatic compound and a film consisting of a monolayer or multilayers comprising the peptide derivative amphiphatic compound are disclosed.Type: GrantFiled: April 8, 1991Date of Patent: October 12, 1993Assignee: Fuji Photo Film Co., Ltd.Inventors: Hiroshi Kitaguchi, Ryoichi Nemori
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Patent number: 5240630Abstract: A refrigeration lubricant suitable for use with R-134a-type refrigerants comprises at least one dialkanolamine diester-amide oil corresponding to one of the formulas: ##STR1## in which formulas R is a hydrocarbylene group containing 1-10 carbons; n represents zero or one; each R' is independently selected from alkylene groups containing 1-10 carbons; R" is hydrogen or a hydrocarbyl group containing 1-10 carbons; and each G, when not linked with another G, is independently selected from hydrocarbyl groups containing 1-10 carbons or, when linked with another G, is a hydrocarbylene group which, together with the colinked G, forms a hydrocarbylene group containing 1-10 carbons.Type: GrantFiled: October 9, 1992Date of Patent: August 31, 1993Assignee: Ethyl CorporationInventors: Mahmood Sabahi, Donald R. Bell