Thioether, Thiol, Or Mercaptide Containing Patents (Class 554/101)
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Patent number: 10113136Abstract: A method for extracting successively essential oil, incensole derivatives and boswellic acids from frankincense resin.Type: GrantFiled: September 28, 2015Date of Patent: October 30, 2018Assignee: PHYTOVATION LTDInventor: Raymond Marriott
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Publication number: 20150141678Abstract: What is described is a compound of formula (1) wherein R1 and R2 are the same or different, each a linear or branched alkyl with 1-9 carbons, or an alkenyl or alkynyl with 2 to 11 carbon atoms; L1 and L2 are the same or different, each a linear alkyl having 5 to 18 carbon atoms, or form a heterocycle with N; X1 is a bond, or is —CO—O— whereby L2-CO—O—R2 is formed; X2 is S or O; L3 is a bond or a lower alkyl, or form a heterocycle with N; R3 is a lower alkyl; and R4 and R5 are the same or different, each a lower alkyl; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: November 18, 2014Publication date: May 21, 2015Inventors: Joseph E. Payne, Padmanabh Chivukula
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Publication number: 20150057347Abstract: The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing inflammation and lipid disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of hypertriglyceridemia, steatohepatitis, cystinosis and inflammatory diseases.Type: ApplicationFiled: November 5, 2014Publication date: February 26, 2015Inventor: Mahesh Kandula
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Publication number: 20150024037Abstract: Compositions, methods of making, and methods of using, xenoantigen-displaying anticancer vaccines are described. In another broad aspect, there is provided herein a method of synthesizing an alkynefunctionalized composition of claim 1, comprising: deprotecting an ester comprising a Fmoc moiety to form a free acid; coupling the free acid of step (a) with an amine; and, removing the Fmoc moiety, and coupling the remaining moiety with palmitic acid to yield an alkyne-functionalized composition.Type: ApplicationFiled: February 15, 2013Publication date: January 22, 2015Applicant: THE UNIVERSITY OF TOLEDOInventors: Steven J. Sucheck, Katherine A. Wall, Sourav Sarkar
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Publication number: 20140323390Abstract: The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.Type: ApplicationFiled: July 9, 2014Publication date: October 30, 2014Applicant: IRM LLCInventors: Tom Yao-Hsiang WU, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan
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Publication number: 20140235807Abstract: Disclosed herein is a chain transfer agent in a free-radical emulsion polymerization process, of at least one mercapto-methyl ester, and also relates to the free-radical emulsion (co)polymerization process comprising at least one such mercapto-methyl ester and uses thereof. Also disclosed herein are mercapto-methyl diesters.Type: ApplicationFiled: February 13, 2014Publication date: August 21, 2014Applicant: ARKEMA FRANCEInventors: Jean-Benoit Cazaux, Pascal Saint-Louis-Augustin, Georges Fremy
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Patent number: 8759558Abstract: The present invention relates to lipid compounds of the general formula (I): wherein R1 is selected from a C10-C22 alkyl, a C10-C22 alkenyl having 1-6 double bonds, and a C10-C22alkynyl having 1-6 triple bonds; R2 and R3 are the same or different and may be selected from a group of different substituents; Y is selected from sulphur, sulfoxide, and sulfone; and X represents a carboxylic acid or a derivative thereof, a carboxylic ester, a carboxylic anhydride or a carboxamide; or a pharmaceutically acceptable salt, complex or solvate thereof. The invention also relates to pharmaceutical compositions and lipid compositions comprising such compounds, and to such compounds for use as medicaments or for use in therapy, in particular for the treatment of diseases related to the cardiovascular, metabolic and inflammatory disease area.Type: GrantFiled: July 13, 2009Date of Patent: June 24, 2014Assignee: Pronova Biopharma Norge ASInventors: Anne Kristin Holmeide, Ragnar Hovland, Morten Brændvang
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Patent number: 8686167Abstract: Activated fatty acids, pharmaceutical compositions including activated fatty acids, methods for using activated fatty acids to treat a variety of diseases, and methods for preparing activated fatty acids are provided herein.Type: GrantFiled: October 1, 2010Date of Patent: April 1, 2014Assignee: Complexa, Inc.Inventor: Raymond A. Miller
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Publication number: 20140079728Abstract: The present invention provides an adjuvanting material, the adjuvanting material comprising a lipid dendritic cell targeting moiety to which is covalently linked a metal chelating group. Further, the present invention provides an immunogenic composition comprising (a) a lipid dendritic cell targeting moiety to which is covalently linked a metal chelating group; (b) an antigen comprising a metal affinity tag; and optionally (c) metal ions, whereby the antigen is linked to the lipid dendritic cell targeting moiety via the interaction between the metal affinity tag and the metal chelating group.Type: ApplicationFiled: September 11, 2013Publication date: March 20, 2014Applicant: Lipotek Pty Ltd.Inventors: David C. Jackson, Christopher R. Parish
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Publication number: 20130330401Abstract: The description is directed to ionizable lipids useful for enhancing the delivery of therapeutic agents in liposomes.Type: ApplicationFiled: June 10, 2013Publication date: December 12, 2013Applicant: Nitto Denko CorporationInventors: Joseph E. Payne, John A. Gaudette, Zheng Hou, Mohammad Ahmadian, Lei Yu, Victor Knopov, Violetta Akopian, Priya Karmali, Richard P. Witte, Neda Safarzadeh, Wenbin Ying, Jun Zhang
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Publication number: 20130303466Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.Type: ApplicationFiled: October 18, 2011Publication date: November 14, 2013Applicant: ELCELYX THERAPEUTICS, INC.Inventors: Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley, Alain D. Baron
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Publication number: 20130225681Abstract: Phenylketone carboxylate compounds of Formula I, wherein n=2-6; R?C(0); —OC(O)— or —CH(OH)—; A is (CH2)mCOOH, W(CH2)mCOOH or YCH(COOH)((CH2)pCH3) when B is Ft B is (CH2)mCOOH, W(CH2)mCOOH or YCH(COOH)((CH2)pCH3) when A is Ft or A and B form a 5-7 membered cycloalkyl substituted with COOFt W=0, S or NFt Y=0,S,NH or CH2; m=0-2; p=1-7; have been prepared. These compounds and their pharmaceutically acceptable salts have beneficial therapeutic effects to prevent or treat a condition related to (l) blood disorders, (ii) inflammation related diseases, (iii) renal disorders and/or renal disorders complications, or (iv) fibrosis-related organ dysfunction.Type: ApplicationFiled: October 26, 2011Publication date: August 29, 2013Applicant: PROMETIC BIOSCIENCES INC.Inventors: Boulos Zacharie, Christopher Penney, Shaun Abbott, Lyne Gagnon, Brigette Grouix, Pierre Laurin
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Publication number: 20130225837Abstract: An object of the present invention is to provide a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof and to provide a pharmaceutical agent which contains said compound as an active ingredient and has a highly safe neurotrophic factor-like activity or an alleviating action for side effect induced by administration of anti-cancer agents. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof which is the compound of the present invention is specifically represented by the formula (1): (In the formula, Y is —O—, —NR— or —S—, R is hydrogen atom, alkyl group, dialkylaminoalkyl group or the like and W is a substituent such as dialkylaminoalkyl group) and has a quite high usefulness as a pharmaceutical agent such as a preventive or therapeutic agent for dementia, Alzheimer's disease, Parkinson's disease, depression, etc., a treating or repairing agent for spinal cord injury.Type: ApplicationFiled: November 1, 2011Publication date: August 29, 2013Applicants: Nippon Zoki Pharmaceutical Co., Ltd., Nagoya Industrial Science Research InstituteInventors: Munekazu Iinuma, Shoei Furukawa, Mitsuru Naiki, Tomonori Matsumoto, Hachiro Sugimoto
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Patent number: 8445707Abstract: The disclosure herein provides the compounds of Formulas 1, 2 and 3 and their pharmaceutical acceptable salts, as well as polymorphs, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, transdermal administration, and/or injection. Such compositions may be used for the treatment of metabolic conditions, cystinosis, non-alcoholic Steatohepatitis, hypertriglyceridemia, and/or neurodegenerative disorders, and/or their associated complications.Type: GrantFiled: October 10, 2012Date of Patent: May 21, 2013Assignee: Krisani Biosciences (P) Ltd.Inventor: Mahesh Kandula
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Publication number: 20130065861Abstract: The invention provides a novel class of compounds viz. generally lipopeptides like Pam3CSK4, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness a vaccine.Type: ApplicationFiled: March 23, 2011Publication date: March 14, 2013Inventors: Tom Yao-Hsiang Wu, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan
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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: 20120277133Abstract: This invention relates to functionalized polymers derived from functionalized monomers. The functionalized polymer may be reacted with an enophilic reagent (e.g., maleic anhydride) to form an enophilic reagent modified functionalized polymer. The functionalized polymer may be further reacted with one or more additional reagents, e.g., an oxygen-containing reagent (e.g., alcohol, polyol), a nitrogen-containing reagent (e.g., amine, polyamine, aminoalcohol), a metal, a metal compound, or a mixture of two or more thereof. The invention relates to lubricants, functional fluids, fuels, dispersants, detergents and polymer compositions.Type: ApplicationFiled: March 23, 2012Publication date: November 1, 2012Inventors: Stephen A. DiBiase, Syed Q.A. Rizvi, Georgeta Hategan
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Publication number: 20110190395Abstract: The present disclosure relates to lipid compounds of general formula (I) wherein R1 is chosen from a C10-C22 alkyl group, a C10-C22 alkenyl group having 1-6 double bonds, and a C10-C22 alkynyl group having 1-6 triple bonds; R2 and R3 are the same or different and may be selected from different substituents; Y is chosen from sulphur, sulfoxide, and sulfone; and X is a carboxylic acid or a derivative thereof, a carboxylic ester, a carboxylic anhydride, or a carboxamide; or a pharmaceutically acceptable salt, complex, or solvate thereof. The present disclosure also relates to pharmaceutical compositions and lipid compositions comprising such compounds, and methods of using such compounds such as for treating diseases related to cardiovascular, metabolic, and/or inflammatory diseases.Type: ApplicationFiled: July 13, 2009Publication date: August 4, 2011Inventors: Anne Kristin Holmeide, Ragnar Hovland, Morten Brændvang
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Publication number: 20110082206Abstract: Activated fatty acids, pharmaceutical compositions including activated fatty acids, methods for using activated fatty acids to treat a variety of diseases, and methods for preparing activated fatty acids are provided herein.Type: ApplicationFiled: October 1, 2010Publication date: April 7, 2011Inventor: Raymond A. Miller
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Publication number: 20100152293Abstract: Psoriasis is a common, chronic, inflammatory skin disorder. This invention provides the use of a compound of formula (I) R—CO—X) (Wherein R is a C16-24 unsaturated hydrocarbon group optionally interrupted by ?, ?, ?, or ? to the carbonyl group by a heteroatom or group of heteroatoms selected from S, O, N, SO, SO2 said hydrocarbon group comprising at least 5 non-conjugated double bonds; and X is an electron withdrawing group) in the manufacture of a medicament for the treatment of psoriasis.Type: ApplicationFiled: February 26, 2010Publication date: June 17, 2010Applicant: Avexxin ASInventors: Berit Johansen, Marit Anthonsen, Wenche Sjursen, Anne Kristen Holmeide, Lars Skattebol
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Patent number: 7713326Abstract: Thiol ester compositions, methods of making the thiol ester compositions, and methods of using the thiol ester compositions are provided. In some embodiments, the thiol ester compositions include thiol esters, hydroxy thiol esters and cross-linked thiol esters. The thiol ester composition can be used to produce cross-linked thiol esters, sulfonic acid-containing esters, sulfonate containing esters and thioacrylate containing esters. The thiol ester compositions can be used to produce polythiourethanes. The polythiourethanes can be used in fertilizers and fertilizer coatings.Type: GrantFiled: February 17, 2005Date of Patent: May 11, 2010Assignee: Agrium Inc.Inventors: Leslie E. Carstens, Baozhong Xing, Mitchell D. Refvik, Jim D. Byers
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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: 7538193Abstract: S-nitrosohemoglobin can liberate NO by transfer to a low molecular weight thiol in the circulatory system, allowing the delivery of NO to the tissues. The effect of administering isolated S-nitrosohemoglobin and low molecular weight thiol to a mammal is to increase delivery of oxygen and NO.Type: GrantFiled: April 9, 2007Date of Patent: May 26, 2009Assignee: Duke UniversityInventor: Jonathan S. Stamler
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Patent number: 7521401Abstract: Fuels, especially hydrocarbon fuels, and lubricants, especially lubricating oils, contain dithiocarbamyl ?-hydroxy fatty acid esters, a class of anti-corrosion, anti-wear, anti-fatigue, and extreme pressure additives that are derived from epoxidized fatty acid esters. The additives exhibit synergistic anti-wear activity in combination with phosphorus containing additives.Type: GrantFiled: November 14, 2005Date of Patent: April 21, 2009Assignee: ChemTura CorporationInventor: Robert G. Rowland
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Patent number: 7279563Abstract: A hydrocarbyldithiomethyl-modified compound of the Formula: R1—O—CH2—S—S—R2 or a salt thereof wherein R1 is an organic molecule and R2 is a hydrocarbyl is useful for protecting and/or blocking hydroxyl groups in organic molecules such as nucleotides. The hydrocarbyldithiomethyl-modified compounds can also be used for chemically synthesizing oligonucleotides and for sequencing nucleic acid compounds.Type: GrantFiled: October 27, 2003Date of Patent: October 9, 2007Assignee: Helicos BioSciences CorporationInventor: Marek Kwiatkowski
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Patent number: 7253296Abstract: The invention relates to novel acylated aminopropanediols and the nitrogen and sulfur analogues thereof, pharmaceutical compositions comprising same, therapeutic uses thereof, in particular for the treatment of cerebral ischemia. The invention also provides a method of preparing said derivatives.Type: GrantFiled: February 12, 2004Date of Patent: August 7, 2007Assignee: GenfitInventors: Raphaël Darteil, Karine Caumont-Bertrand, Jamila Najib
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Patent number: 6977292Abstract: The invention is directed to nucleophile-stable thioester generating compounds comprising a carboxyester thiol. The compounds have wide applicability in organic synthesis, including the generation of peptide-, polypeptide- and other polymer-thioesters. The invention is particularly useful for generating activated-thioesters from precursors that are made under conditions in which strong nucleophiles are employed, such as peptides or polypeptides made using Fmoc SPPS, as well as multi-step ligation or conjugation schemes that require (or benefit from the use of) compatible selective approaches for directing a specific ligation or conjugation reaction of interest.Type: GrantFiled: August 30, 2001Date of Patent: December 20, 2005Assignee: Gryphon TherapeuticsInventors: Paolo Botti, James A. Bradburne, Stephen B. H. Kent
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Patent number: 6780418Abstract: A method of detecting a member of the taxa actinomycetos is provided. A method also is provided for detecting mycothiol or precursor thereof. An antibody is provided which binds to mycothiol or a mycothiol precursor. A method is further provided for diagnosis of a subject having or at risk of having an actinomycetes-associated disorder. A method is also provided for identifying a sample with altered production of mycothiol or a precursor thereof. A method is provided for detecting mycothiol or precursor thereof in a bacterial colony. Kits are also disclosed which arc useful for detecting the presence of mycothiol or precursor thereof in a sample.Type: GrantFiled: July 6, 2000Date of Patent: August 24, 2004Assignee: The Regents of the University of CaliforniaInventors: Robert C. Fahey, Gerald L. Newton, Maria Margarita D. Unson, Charles E. Davis, Sara J. Anderberg
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Patent number: 6639088Abstract: A hydrocarbyldithiomethyl-modified compound of the Formula: R1—O—CH2—S—S—R2 or a salt thereof wherein R1 is an organic molecule and R2 is a hydrocarbyl is useful for protecting and/or blocking hydroxyl groups in organic molecules such as nucleotides. The hydrocarbyldithiomethyl-modified compounds can also be used for chemically synthesizing oligonucleotides and for sequencing nucleic acid compounds.Type: GrantFiled: September 12, 2001Date of Patent: October 28, 2003Assignee: Quiatech ABInventor: Marek Kwiatkowski
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Patent number: 6569411Abstract: Serine carbonates of formula I are precursors for organoleptic compounds, masking agents and antimicrobial agents. Further they are alternative substrates for malodor producing enzymes. The symbols in formula I are defined in claim 1.Type: GrantFiled: August 15, 2002Date of Patent: May 27, 2003Assignee: The Gillette CompanyInventors: Georg Frater, Denise Anderson, Frank Kumli, Jens Wittenberg, Virginia Streusand Goldman
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Patent number: 6511670Abstract: Novel pharmaceutically/cosmetically-active (poly)thiaalkynoic compounds have the structural formula (I): R1—Y—CH2—C≡C—CH2—S—CH2—R2 (I) and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example inflammation disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: April 13, 2000Date of Patent: January 28, 2003Assignee: Societe L'Oreal S.A.Inventors: Jean Maignan, Sylvie Genard, Serge Michel
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Patent number: 6407137Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.Type: GrantFiled: July 9, 2001Date of Patent: June 18, 2002Assignee: Protarga, Inc.Inventor: Victor E. Shashoua
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Patent number: 6376688Abstract: The present invention provides polyunsaturated fatty acid compounds having antimalarial and/or neutrophil stimulatory activity. The polyunsaturated fatty acids contain 18-25 carbons and 1-6 double bonds and are characterized in that they have one or two substitutions selected from the group consisting of &bgr; oxa, &ggr; oxa, &bgr; thia and &ggr; thia. It is also preferred that the polyunsaturated fatty acid compound includes a further substitution selected from the group consisting of hydroxy, hydroperoxy, peroxy, carboxymethyl substitutions or attached to an amino acid.Type: GrantFiled: May 29, 1997Date of Patent: April 23, 2002Assignee: Peptide Technology LimitedInventors: Antonio Ferrante, Alfred Poulos, Christopher John Easton, Michael Joseph Pitt, Thomas Alistair Robertson, Deborah Ann Rathjen
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Patent number: 6258836Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.Type: GrantFiled: November 29, 1999Date of Patent: July 10, 2001Assignee: Protarga, Inc.Inventor: Victor E. Shashoua
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Patent number: 6224903Abstract: A fusogenic liposome composition for delivering a liposome-entrapped compound into the cytoplasm of a target cell is described. The liposomes have an outer surface coating of chemically releasable hydrophilic polymer chains which shield hydrophobic polymers on the liposome outer surface. Release of the hydrophilic polymer chains exposes the hydrophobic polymers for interaction with outer cell membranes of the target cells to promote fusion of the liposome with the target cells. Also disclosed is a polymer-lipid conjugate for use in promoting fusion between target membranes. The conjugate is composed of a first segment composed of a hydrophilic polymer and a second hydrophobic polymer segment. The second segment is joined to the first segment by a bond effective to release the first segment in response to an existing or an induced physiologic condition. Attached to the second segment is a vesicle-forming lipid member.Type: GrantFiled: December 10, 1998Date of Patent: May 1, 2001Assignee: Sequus Pharmaceuticals, Inc.Inventors: Francis J. Martin, Samuel Zalipsky
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Patent number: 6180667Abstract: Esters of alkanoyl L-carnitines wherein the alkanoyl is a saturated or unsaturated, staight or branched alkanoyl having 2-26 carbon atoms, optionally &ohgr;-substituted with trialkylammonium, dialkylsulfonium, hydroxyl, carboxyl, halogen, methanesulfonyl and hydroxysulfonyl, are useful for preparing pharmaceutical compositions for the treatment of endotoxic shock.Type: GrantFiled: March 28, 1997Date of Patent: January 30, 2001Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Piero Foresta, Vito Ruggiero, Maria Ornella Tinti, Nazareno Scafetta
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Patent number: 6150542Abstract: The invention relates to agents preventing (the formation of) human malodor. In particular, the invention relates to the use of several classes of compounds which can act as such agents in cosmetic products, such as deodorants and antiperspirants. These compounds are normally odorless or nearly so, but upon contacting the skin as for example, in skin care compositions or in personal care compositions, they prevent malodor.The compounds under consideration are compounds of the formula:X--(Z).sub.n --CO--NH--CH--(COO--Y)--CH.sub.2 CH.sub.2 CONH.sub.2I.Type: GrantFiled: April 13, 1999Date of Patent: November 21, 2000Assignee: Givaudan Roure (International) SAInventors: Gonzalo Acuna, Georg Frater, Peter Gygax
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Patent number: 6013815Abstract: The invention relates to the production and purification of salts of 6,8-bis (amidiniumthio)octanoic acid, its enantiomers (+)-6,8-bis(amidiniumthio)octanoic acid and (-)-6,8-bis (amidiniumthio)octanoic acid and of the esters of these compounds as well as to their use to produce dihydrolipoic acid and .alpha.-lipoic acid.Type: GrantFiled: March 18, 1998Date of Patent: January 11, 2000Assignee: ASTA Medica AktiengesellschaftInventors: Thomas Beisswenger, Rainer Gewald, Alfred Olbrich, Horst Bethge, Frank Hubner, Klaus Huthmacher, Herbert Klenk, Roland Moller, Stephan Rautenberg, Gerhard Sator
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Patent number: 6001869Abstract: A method of inhibiting parasitic activity is disclosed in which the biosynthesis, structure and/or function of the glycosyl phosphatidylinositol (GPI) anchor of said parasite may be affected by incorporating into said GPI anchor selected analogs of myristic acid containing various heteroatoms, substituents and unsaturated bonds, including ester-containing analogs, ketocarbonyl-containing analogs, sulfur-containing analogs, double bond- and triple bond-containing analogs, aromatic moiety-containing analogs, nitrated analogs and halogenated analogs.Type: GrantFiled: December 15, 1997Date of Patent: December 14, 1999Assignees: Washington University, Johns Hopkins UniversityInventors: Jeffrey I. Gordon, George W. Gokel, Paul T. Englund
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Patent number: 6002029Abstract: Lipid prodrugs of phosphonoacids and their analogs that have increased antiviral activity over the parent drugs in inhibiting cytomegalovirus and other susceptible viruses.Type: GrantFiled: December 8, 1997Date of Patent: December 14, 1999Inventors: Karl Y. Hostetler, Ganesh D. Kini
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Patent number: 5994392Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.Type: GrantFiled: June 5, 1995Date of Patent: November 30, 1999Assignee: Neuromedica, Inc.Inventor: Victor E. Shashoua
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Patent number: 5925339Abstract: The invention relates to agents preventing (the formation of) human malodor. In particular, the invention relates to the use of several classes of compounds which can act as such agents in cosmetic products, such as deodorants and antiperspirants. These compounds are normally odorless or nearly so, but upon contacting the skin as for example, in skin care compositions or in personal care compositions, they prevent malodor. The compounds under consideration are compounds of the formulaX--(Z).sub.n --CO--NH--CH--(COO--Y)--CH.sub.2 CH.sub.2 CONH.sub.2IThe definition of the substituents is given in the specification.Type: GrantFiled: June 19, 1997Date of Patent: July 20, 1999Assignee: Givaudan Roure SAInventors: Gonzalo Acuna, Georg Frater, Peter Gygax
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Patent number: 5811384Abstract: Novel nonionic gemini surfactants are extremely effective emulsifiers for oil-in-water emulsions that provide improved detergency at even low concentration levels. The surfactants are characterized by the formula: ##STR1## wherein R.sub.1 is independently H or a C.sub.1 to C.sub.22 alkyl, R.sub.2 is H or C.sub.1 to C.sub.22 alkyl and R.sub.3 is D.sub.1 --R.sub.4 --D.sub.1 or R.sub.4 --D.sub.1 --R.sub.4 wherein R.sub.4 is independently a C.sub.1 -C.sub.10 alkyl group, --C(O)--, --R.sub.5 ?O(EO).sub.a (PO).sub.b !--, --O--R.sub.5 --O--, or aryl, e.g. phenyl, and D.sub.1 is independently --O--, --S--, --S--S--, --SO.sub.2 --, --C(O)--, a polyether group ?--O(EO).sub.a (PO).sub.b --!, an amide group ?--C(O)N(R.sub.6)--!, an amino group ?--N(R.sub.6)--!, --O--R.sub.5 --O--, or aryl. (EO).sub.a (PO).sub.b is a polyether group and Z is a C.sub.1 -C.sub.Type: GrantFiled: November 26, 1997Date of Patent: September 22, 1998Assignee: Rhodia Inc.Inventors: David James Tracy, Ruoxin Li, Manilal S. Dahanayake, Jiang Yang
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Patent number: 5696277Abstract: Lipid prodrugs of phosphonoacids and their analogs that have increased antiviral activity over the parent drugs in inhibiting cytomegalovirus and other susceptible viruses.Type: GrantFiled: November 15, 1994Date of Patent: December 9, 1997Assignee: Karl Y. HostetlerInventors: Karl Y. Hostetler, Ganesh D. Kini
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Patent number: 5643948Abstract: Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from diterpenes of the phorbol-, resiniferonol- and ingenol-classes.Type: GrantFiled: September 13, 1993Date of Patent: July 1, 1997Assignee: Procyon Pharmaceuticals, Inc.Inventors: Paul E. Driedger, James Quick
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Patent number: 5637616Abstract: A method for the topical or systemic treatment of disorders mediated by proteases which result in skin or mucosal lesions, and in particular, pemphigus, cicatricial pemphigoid, bullous pemphigoid, lichen planus, and canker sores, is disclosed wherein the host is treated with an effective amount of N-acetyl ysteine or a derivative thereof, or its pharmaceutically acceptable salt, optionally in a pharmaceutically acceptable diluent or carrier for systemic or topical delivery.Type: GrantFiled: October 5, 1993Date of Patent: June 10, 1997Assignee: Arcturus Pharmaceutical CorporationInventors: Richard J. Sharpe, Maureen H. McAloon, Stephen J. Galli, Kenneth A. Arndt
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Patent number: 5625085Abstract: Esters of alkanoyl L-carnitines wherein the alkanoyl is a saturated or unsaturated, straight or branched alkanoyl having 2-26 carbon atoms, optionally .omega.-substituted with trialkylammonium, dialkylsulfonium, hydroxyl, carboxyl, halogen, methanesulfonyl and hydroxysulfonyl, are useful for preparing pharmaceutical compositions for the treatment of endotoxic shock.Type: GrantFiled: July 14, 1994Date of Patent: April 29, 1997Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Piero Foresta, Vito Ruggiero, Maria O. Tinti, Nazareno Scafetta
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Patent number: 5587499Abstract: These compounds are denoted by the following formula (I): ##STR1## in which: Z denotes H or a linear or branched alkyl radical,X denotes O or S,each of A and B independently denotes an alkylene radical, it being possible for this radical to be substituted,R denotes H or an alkali metal, or else a linear or branched alkyl radical,x has the value of 0 or 1, andy has the value of 0, 1 or 2,the radical A not existing if x and y are both equal to 0, X being incapable of denoting O when R=alkyl and when R=H with x=y=0, and B being incapable of denoting optionally substituted methylene when X=S, x=y=0 and R=alkyl.According to the invention, different simple and efficient processes are proposed for preparing these new compounds, which can be applied to the preparation of new polymers and copolymers.Type: GrantFiled: May 11, 1995Date of Patent: December 24, 1996Assignee: ELF Atochem S.A.Inventors: Mich ele Curci, Jean-Luc Mieloszynski, Daniel Paquer
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Patent number: 5506267Abstract: A compound of the invention is represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different, an acyl group; R.sup.3, R.sup.4, R.sup.6 and R.sup.7 are the same or different, hydrogen or an alkyl group; R.sup.5 is hydrogen, an alkyl group or a hydroxyl group which may optionally be protected, or R.sup.4 and R.sup.5 are combined to form a chemical bond; X is a carbonyl group or a sulfonyl group; Y is an amino acid sequence consisting of 1 to 7 amino acid residues which may optionally be protected and having optionally an intervening --SO.sub.2 NH--; n is an integer of 0 to 2, or a salt thereof.Type: GrantFiled: September 8, 1994Date of Patent: April 9, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Tetsuya Aono, Koichi Yukishige, Seiichi Tanida
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Patent number: 5498786Abstract: This invention relates to novel processes for synthesizing intermediates in the preparation of N-aryl and N-heteroarylamide inhibitors of the enzyme acyl coenzyme A: cholesterol acyltransferase (ACAT), and to novel intermediates used in such processes.Type: GrantFiled: September 13, 1993Date of Patent: March 12, 1996Assignee: Pfizer Inc.Inventors: Sarah E. Kelly, George Chang