Oxy Patents (Class 562/452)
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Patent number: 11892435Abstract: Methods for measuring pH of gel, paste, colloid, and aqueous solutions, such as a consumer product, a food product, a pet food product, a beverage product, a pharmaceutical product, and/or a medical product, are provided. The method may include preparing a calibration curve of a chemical species including or having an acid dissociation constant. Preparing the calibration curve may include plotting a chemical shift of the chemical species relative to pH. The method may also include determining a chemical shift of a gel, paste, and colloid, aqueous solutions, such as a consumer product, a food product, a pet food product, a beverage product, a pharmaceutical product, and/or a medical product, including the chemical species.Type: GrantFiled: December 5, 2019Date of Patent: February 6, 2024Assignee: Colgate-Palmolive CompanyInventors: Chi-Yuan Cheng, Zhigang Hao, Long Pan, Zolijargal Balsandorj
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Patent number: 11738009Abstract: The present disclosure is directed to novel compounds of Formula I and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of cancer, including glioblastoma, bone cancer, head and neck cancer, melanoma, basal cell carcinoma, squamous cell carcinoma, adenocarcinoma, oral cancer, esophageal cancer, gastric cancer, intestinal cancer, colon cancer, bladder cancer, hepatocellular carcinoma, renal cell carcinoma, pancreatic cancer, ovarian cancer, cervical cancer, lung cancer, breast cancer, and prostate cancer. The compounds of the disclosure are selective antagonists of the EP4 receptor and useful treatment of various diseases that may be ameliorated with blockade of PGE2-mediated signaling.Type: GrantFiled: April 17, 2018Date of Patent: August 29, 2023Assignee: TEMPEST THERAPEUTICS, INC.Inventors: Yalda Bravo, Jason David Burch, Austin Chih-Yu Chen, Joe Fred Nagamizo
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Patent number: 9333222Abstract: Embodiments herein relate to the field of lysosomal storage disorders, and, more specifically, to methods of treating lysosomal storage disorders such as Niemann-Pick type C disease, for instance with inhibitors of histone deacetylases, particularly inhibitors of class 1 histone deacetylases. In various embodiments, methods of treating Niemann-Pick type C disease with inhibitors of class 1 histone deacetylases are described.Type: GrantFiled: September 22, 2010Date of Patent: May 10, 2016Assignees: University of Notre Dame du Lac, Cornell UniversityInventors: Olaf Wiest, Frederick R. Maxfield, Paul Helquist
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Patent number: 9040553Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).Type: GrantFiled: July 11, 2013Date of Patent: May 26, 2015Assignee: CELL VIABLE CORPORATIONInventors: Iraj Lalezari, Jill Fabricant
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Publication number: 20140364339Abstract: The ?,?-unsaturated ?-amino acids of general formula (I). Also, a versatile process for the stereospecific synthesis of said compounds of formula (I), involving a Wittig reaction. Further, intermediate products of general formulae (II) and (III), as shown below, which are involved in the synthesis of compounds (I). Compounds of general formula (I) may be useful as therapeutic substances, or as reagents or intermediates for fine chemistry.Type: ApplicationFiled: August 28, 2012Publication date: December 11, 2014Inventors: Sylvain Jugé, Jérôme Bayardon, Emmanuelle Remond, Marie-Joëlle Ondel-Eymin
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Publication number: 20140350019Abstract: The present invention relates to aniline derivatives of formula (I), to their preparation and to their therapeutic application, for example in treating glaucoma: Formula (I), R1a represents H, an halogen, a (C1-C6)alkyl or a CN; R1b represents H, an halogen or a (C1-C6)alkyl; R1c represents H or a (C1-C6)alkyl; R2 represents H, an halogen, an OH, an O—(C1-C6)alkyl or (C1-C6)alkyl; R3 represents H, an halogen, a (C1-C6)alkyl, an OH, an O—(C1-C6)alkyl, a CONH2 or CN; R4 represents H, an halogen or a (C1-C6)alkyl; R5 represents H or F: R7 represents H or F; R8 represents H or F; R9 represents H or (C1-C6)alkyl, or one of its enantiomers.Type: ApplicationFiled: September 7, 2012Publication date: November 27, 2014Applicant: FOVEA PHARMACEUTICALSInventors: John Feutrill, Caroline Leriche, David Middlemiss
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Publication number: 20140350045Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).Type: ApplicationFiled: July 11, 2013Publication date: November 27, 2014Inventors: IRAJ LALEZARI, JILL FABRICANT
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Publication number: 20140221662Abstract: Chiral amino compounds, methods of preparation and uses thereof. Tamiflu can be obtained from the said compounds. Multi-substituted chiral tetrahydropyrrolyl amine which can be used as intermediate compounds of medicament can also be produced by the said compounds.Type: ApplicationFiled: December 17, 2010Publication date: August 7, 2014Applicants: SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES, LIANHE CHEMICAL TECHNOLOGY CO., LTD.Inventors: Dawei Ma, Shaolin Zhu, Shouyun Yu, You Wang, Qianghui Zhou
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Patent number: 8785494Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating trifluoromethylphenylene cyclopentylene compounds represented in formula (I) and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.Type: GrantFiled: May 26, 2010Date of Patent: July 22, 2014Assignee: LEO-Pharma A/SInventor: Bjarne Nørremark
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Publication number: 20140179014Abstract: Nitric oxide probes including a compound represented by Formula, I, II, III, IV, V, VI or a combination thereof are provided. Methods of using these nitric oxide probes to detect nitric oxide are also provided.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Inventors: Eric V. Anslyn, Youjun Yang, Michelle M. Adams
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Publication number: 20140135397Abstract: The present invention provides compositions and methods for the targeted delivery, release and/or formation of a drug compound at a target site(s) within the body of an individual, such as a diseased and/or inflamed tissue in the body of the individual. These compositions may comprise a halogenated phenol ring cleavably linked to a core structure of a drug compound. Due to the variety of substituents that may be utilized in forming the different types of linkages, numerous examples of drug compounds linked to a halogenated phenol ring are proposed. The present invention further provides compositions comprising halogenated phenol starting compounds that do not undergo cleavage during a dehalogenation reaction to form a drug compound in a targeted tissue when administered to an individual. Methods of administering these non-cleaving compounds are further provided.Type: ApplicationFiled: January 21, 2014Publication date: May 15, 2014Inventor: Keith R. Latham
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Publication number: 20140100353Abstract: The invention relates to a method or process for the chemical manufacture of depsipeptides of the formula I employing an aldehyde acetal intermediate, wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.Type: ApplicationFiled: October 1, 2013Publication date: April 10, 2014Applicant: NOVARTIS AGInventors: Murat ACEMOGLU, Heribert HELLSTERN, Bernard RISS, Christian SPRECHER
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Publication number: 20140094615Abstract: Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.Type: ApplicationFiled: April 26, 2012Publication date: April 3, 2014Applicant: The Board of Trustees of the University of IllinoisInventors: Martin D. Burke, Junqi Li, Eric P. Gillis
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Patent number: 8680320Abstract: The present invention provides a metal chelator and methods that facilitate binding, detecting, monitoring and quantitating of heavy metal ions in a sample.Type: GrantFiled: December 11, 2009Date of Patent: March 25, 2014Assignee: Life Technologies CorporationInventors: Kyle Gee, Jolene Bradford, Vladimir Martin
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Patent number: 8673903Abstract: The present application relates to novel substituted 8-alkoxy-2-aminotetraline derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: May 9, 2011Date of Patent: March 18, 2014Assignee: Bayer Intellectual Property GmbHInventors: Walter Hübsch, Michael Hahn, Alexandros Vakalopoulos, Volkhart Min-Jian Li, Frank Wunder, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Friederike Stoll, Niels Lindner
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Patent number: 8664249Abstract: Tetrasubstituted benzenes that act as modulators of gamma secretase and their use in the treatment of one or more symptoms of treating neurodegenerative disorders, e.g., Alzheimer's disease, are described.Type: GrantFiled: February 1, 2013Date of Patent: March 4, 2014Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Gideon Shapiro, Richard Chesworth
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Patent number: 8653298Abstract: The biphenyl acetate is biphenyl acetic ammonia butantriol salt, which is obtained by reacting biphenyl acetic acid with ammonia butantriol in organic solvent. The salt is adapted to be used for producing analgesic, anti-inflammatory and antithermic medicines.Type: GrantFiled: September 27, 2007Date of Patent: February 18, 2014Assignee: Shijiazhuang Yiling Pharmaceutical Co., Ltd.Inventors: Wei Wang, Wenzhan Chen
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Publication number: 20130302903Abstract: Nitric oxide probes comprising a compound represented by Formula, I, II, III, IV, V, VI or a combination thereof are provided. Methods of using these nitric oxide probes to detect nitric oxide are also provided.Type: ApplicationFiled: October 4, 2012Publication date: November 14, 2013Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventors: Eric V. Anslyn, Youjun Yang, Michelle M. Adams
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Publication number: 20130244995Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.Type: ApplicationFiled: November 21, 2011Publication date: September 19, 2013Applicant: LEO PHARMA A/SInventors: Per Vedsø, Lars Kristian Albert Blæhr
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Publication number: 20130245084Abstract: Compounds of general formula (I) their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.Type: ApplicationFiled: November 21, 2011Publication date: September 19, 2013Applicant: LEO PHARMA A/SInventor: Kristoffer Mansson
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Publication number: 20130230542Abstract: Provided are compounds according to the following Formula I: The Formula I compounds are activated in the presence of reactive oxygen species (ROS) and are therefore selective anti-cancer therapeutics for cancers associated with elevated ROS. Also provided are methods and pharmaceutical compositions for treating cancers associated with increased ROS.Type: ApplicationFiled: March 1, 2013Publication date: September 5, 2013Applicants: CINCINNATI CHILDREN'S HOSPITAL MEDICAL CENTER, UNIVERSITY OF CINCINNATIInventors: Edward J. Merino, James C. Mulloy, Guorui Li, Tiffany Bell-Horwath
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Publication number: 20130203751Abstract: The present application relates to novel substituted 8-alkoxy-2-aminotetraline derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: May 9, 2011Publication date: August 8, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Walter Hübsch, Michael Hahn, Alexandros Vakalopoulos, Volkhart Min-Jian Li, Frank Wunder, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Friederike Stoll, Niels Lindner
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Publication number: 20130165486Abstract: Tetrasubstituted benzenes that act as modulators of gamma secretase and their use in the treatment of one or more symptoms of treating neurodegenerative disorders, e.g., Alzheimer's disease, are described.Type: ApplicationFiled: February 1, 2013Publication date: June 27, 2013Applicant: ENVIVO PHARMACEUTICALS, INC.Inventor: ENVIVO PHARMACEUTICALS, INC.
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Patent number: 8470871Abstract: Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.Type: GrantFiled: June 19, 2012Date of Patent: June 25, 2013Assignee: Galderma Research & DevelopmentInventors: Thibaud Biadatti, Laurence Dumais, Catherine Soulet, Sandrine Talano, Sebastien Daver
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Publication number: 20130143846Abstract: The present invention relates to the crystalline, polymorphic Form X of the calcimimetic compound {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, to methods of preparation thereof, to methods of characterization thereof by single crystal X-Ray crystallography (XRC), X-Ray Powder diffractometry, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, Solid State NMR spectroscopy and Differential Scanning Calorimetry (DSC), and to its use. The invention also relates to the preparation of Form X by crystallization from a saturated solution of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid in a C1-C6 alkyl alcohol, or alternatively by precipitation from a neutralized saponification reaction mixture following the alkaline hydrolysis of a C1-C6 alkyl ester of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid.Type: ApplicationFiled: June 24, 2011Publication date: June 6, 2013Applicant: LEO PHARMA A/SInventors: Søren Ebdrup, Kim Troensegaard Nielsen, Tanja Maria Greve
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Publication number: 20130131023Abstract: The present invention relates to the crystalline, polymorphic Form C of the calcimimetic compound {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, to methods of preparation thereof, to methods of characterization thereof by single crystal X-Ray crystallography (XRC), X-Ray Powder diffractometry, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, Solid State NMR spectroscopy and Differential Scanning Calorimetry (DSC), and to its use.Type: ApplicationFiled: June 24, 2011Publication date: May 23, 2013Applicant: LEO PHARMA A/SInventors: Soren Ebdrup, Kim Troensegaard Nielsen, Tanja Maria Greve
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Patent number: 8399507Abstract: Tricyclic compounds containing a cyclopropanecarboxylic acid fused to a bicyclic ring, including pharmaceutically acceptable salts, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.Type: GrantFiled: October 27, 2008Date of Patent: March 19, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Gui-Bai Liang, Xibin Liao, Weiguo Liu, Paul E. Finke, Dooseop Kim, Lihu Yang, Songnian Lin
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Publication number: 20130060063Abstract: Disclosed is a method for producing precursors for L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 2-[18F]fluoro-L-tyrosine and the ?-methylated derivatives thereof, the precursor, and to a method for producing L-3,4-dihydroxy-6[18F]fluorophenylalanine and 2-[18F]fluoro-L-tyrosine and the ?-methylated derivatives thereof from the precursor. A compound of formula (3) is provided which enables automated synthesis of L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 2-[18F]fluoro-L-tyrosine. The enantiomeric purity of the product is ?98%.Type: ApplicationFiled: November 6, 2012Publication date: March 7, 2013Inventors: Franziska WAGNER, Johannes Ermert, Heinrich Hubert Coenen
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Publication number: 20120295943Abstract: Provided is a therapeutic agent for hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like, which has a CaSR activating (agonist) action. A compound represented by the following general formula (1): [wherein, Ar which is a partial structure in the general formula (1) represents a phenyl group or a naphthyl group; R1a and R1b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; R2a and R2b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; A represents a single bond, an oxygen atom, or the like; B represents a single bond, a C1-C4 alkanediyl group, or the like; Z represents a carboxyl group or a tetrazolyl group; and m represents an integer of 1 to 3] or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: August 20, 2009Publication date: November 22, 2012Inventors: Shinji Marumoto, Toyoki Nishimata, Masayuki Ebisawa, Yusuke Asoh, Yasuo Fukushima, Mikio Kato
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Patent number: 8283453Abstract: 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: GrantFiled: August 14, 2009Date of Patent: October 9, 2012Assignee: International Business Machines CorporationInventors: Ali Afzali-Ardakani, Phaedon Avouris, James B. Hannon, Christian Klinke
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Publication number: 20120232150Abstract: The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo.Type: ApplicationFiled: August 31, 2010Publication date: September 13, 2012Inventors: Shahriar Mobashery, Dusan Hesek, Mayland Chang
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Patent number: 8263659Abstract: A method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described in the general formula I below is administered in a therapeutically effective amount:Type: GrantFiled: May 21, 2009Date of Patent: September 11, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Denis E. Ryono, Jon J. Hangeland, Todd J. Friends, Tamara Dejneka, Pratik Devasthale, Yolanda V. Caringal, Minsheng Zhang, Arthur M. P. Doweyko, Johan Malm, Andrei Sanin
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Patent number: 8227507Abstract: Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.Type: GrantFiled: July 23, 2010Date of Patent: July 24, 2012Assignee: Galderma Research & DevelopmentInventors: Thibaud Biadatti, Laurence Dumais, Catherine Soulet, Sandrine Talano, Sebastien Daver
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Patent number: 8227254Abstract: The present invention pertains to compounds and polymers which incorporate a boronic acid sensor group (SG) of the formula (I): wherein: J is independently —CH2— or —CH2CH2—; n is independently 0, 1, 2, or 3; and each RR, if present, is independently a ring substituent; and wherein the ring attachment (i.e., where sensor group is attached) is via the 3-, 4-, 5-, or 6-ring position. Such compounds and polymers are useful in the selective chemical detection and/or quantitation of alpha-hydroxy carboxylic acids, such as lactic acid/lactate and malic acid/malate. The present invention also pertains to methods of preparing such compounds and polymers; methods and assays which employ these compounds and polymers; devices (e.g., holographic sensors) and kits for use in such methods and assays, etc.Type: GrantFiled: January 31, 2006Date of Patent: July 24, 2012Assignee: Cambridge Enterprise LimitedInventors: Christopher Robin Lowe, Felicity Kate Sartain, Xiaoping Yang
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Patent number: 8217027Abstract: The present invention is directed to novel, potent, and selective agents, which are agonists or antagonists of the one or more of the individual receptors of the S1P receptor family. The compounds of the invention are useful as therapeutics for treating medical conditions associated with agonism or antagonism of the individual receptors of the S1P receptor family.Type: GrantFiled: March 11, 2008Date of Patent: July 10, 2012Assignee: Abbott LaboratoriesInventors: Grier A. Wallace, Eric C. Breinlinger, Kevin P. Cusack, Shannon R. Fix-Stenzel, Thomas D. Gordon, Adrian D. Hobson, Martin E. Hayes, Graham K. Ansell, Pintipa Grongsaard
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Publication number: 20120158127Abstract: Absorbable polyurethanes, polyamides and polyester urethanes prepared from at least one compound selected from: or the corresponding diamines or diisocyanates thereof, wherein each X independently represents —CH2COO—, —CH(CH3)COO—, —CH2CH2OCH2COO—, —CH2CH2CH2CH2CH2COO—, —(CH2)yCOO— where y is 2 to 4 or 6 to 24, or —(CH2CH2O)z?CH2COO— where z? is 2 to 24; each Y represents —COCH2O—, —COCH(CH3)O—, —COCH2OCH2CH2O—, —COCH2CH2CH2CH2CH2O—, —CO(CH2)mO— where m is 2 to 4 or 6 to 24, or —COCH2O(CH2CH2O)n— where n is 2 to 24; R? is hydrogen, benzyl or straight-chained or branched alkyl; p is 1 to 4; and Rn represents one or more members selected from H, alkoxy, benzyloxy, aldehyde, halogen, carboxylic acid and —NO2, which is attached directly to an aromatic ring or attached through an aliphatic chain. Absorbable polymers prepared from these compounds are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention and other implantable medical devices.Type: ApplicationFiled: February 22, 2012Publication date: June 21, 2012Applicant: BEZWADA BIOMEDICAL, LLCInventor: Rao S. Bezwada
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Patent number: 8203016Abstract: The use of specific compounds of the Formula 1 (and also corresponding mixtures) in particular as cosmetic agents for the inhibition of the substance P-induced release of histamine from mast cells is described.Type: GrantFiled: November 20, 2003Date of Patent: June 19, 2012Assignee: Symrise AGInventors: Gerhard Schmaus, Holger Joppe, Martinia Herrmann, Christopher Sabater-Lüntzel, Tobias Vössing
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Publication number: 20120129926Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating trifluoromethylphenylene cyclopentylene compounds represented in formula (I) and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.Type: ApplicationFiled: May 26, 2010Publication date: May 24, 2012Applicant: LEO PHARMA A/SInventor: Bjarne Nørremark
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Publication number: 20120122941Abstract: Provided is a therapeutic agent for hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like, which has a CaSR activating (agonist) action. A compound represented by the following general formula (1): [wherein, Ar which is a partial structure in the general formula (1) represents a phenyl group or a naphthyl group; R1a and R1b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; R2a and R2b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; A represents a single bond, an oxygen atom, or the like; B represents a single bond, a C1-C4 alkanediyl group, or the like; Z represents a carboxyl group or a tetrazolyl group; and m represents an integer of 1 to 3] or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: August 20, 2009Publication date: May 17, 2012Inventors: Shinji Marumoto, Toyoki Nishimata, Masayuki Ebisawa, Yusuke Asoh, Yasuo Fukushima, Mikio Kato
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Publication number: 20120071502Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).Type: ApplicationFiled: September 13, 2011Publication date: March 22, 2012Applicant: CELL VIABLE CORPORATIONInventors: Iraj Lalezari, Jill Fabricant
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Publication number: 20120004453Abstract: An organic solvent includes a photo decomposition type polyimide acid which forms an alignment film of a liquid crystal display device by radiation of a polarized light. A viscosity of the photo decomposition type polyimide acid is not more than 35 mPa·s.Type: ApplicationFiled: September 12, 2011Publication date: January 5, 2012Inventors: Hidehiro Sonoda, Chikae Matsui, Noboru Kunimatsu
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Publication number: 20110178088Abstract: This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.Type: ApplicationFiled: March 21, 2011Publication date: July 21, 2011Applicant: XENTION LIMITEDInventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
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Publication number: 20110130448Abstract: The present invention relates to a compound of the formula: R-AR—O—Y—R? Wherein R represents one or more members selected from H, alkoxy, benzyloxy, aldehyde, halogen, carboxylic acid, —NO2, —NH2, —NHCOCH3, and —NH—Y—R?, which is attached directly to AR or attached through an aliphatic chain. The carboxylic acid moiety in R includes but is not limited to the following carboxylic acids: benzoic acids, cinnamic acids, ferulic acid, caffeic acid, syringic acid, salicyclic acid, vanillic acid, phenylacetic acids, phenylpropionic acids, and sinapinic acid. -AR—O— is a biologically active phenolic moiety comprising 1 to 6 substituted or unsubstituted aryl rings that are directly bonded to each other, fused together, or joined through a linking group.Type: ApplicationFiled: December 7, 2010Publication date: June 2, 2011Applicant: Bezwada Biomedical LLCInventor: Rao S. Bezwada
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Publication number: 20110112193Abstract: There is provided compounds of formula (I), wherein ring A, D1, D2a, D2b, D3, L1, Y1, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.Type: ApplicationFiled: May 5, 2009Publication date: May 12, 2011Inventors: Peter Nilsson, Benjamin Pelcman, Martins Katkevics
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Publication number: 20110071286Abstract: A process for preparing compounds of the formula (I) in which R1.1, R1.2, R1.3 and R2 are as defined in the description.Type: ApplicationFiled: August 12, 2008Publication date: March 24, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Kathrin Pachur, Stefan Goepper, Guenther Huchler, Michael Konrad, Kathrin Maier, Werner Rall, Uwe Joerg Ries, Andreas Zopf
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Publication number: 20110053974Abstract: To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ?C(R5)- or ?N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R1 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C6 haloalkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 aliphatic acyl group, a C1-C6 alkoxy C1-C6 alkyl group, or a C6-C10 aryl group; and R2, R3, R4, and R5 may be the same or different and each represent a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, or a nitro group.Type: ApplicationFiled: September 29, 2010Publication date: March 3, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Narihiro TODA, Masao YOSHIDA, Rieko TAKANO, Masahiro INOUE, Takeshi HONDA, Koji MATSUMOTO, Ryutaro NAKASHIMA
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Patent number: 7893297Abstract: The present invention relates to amorphous and polymorphic forms of sodium 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoate and their use for facilitating the delivery of active agents, such as insulin, to a target.Type: GrantFiled: July 2, 2008Date of Patent: February 22, 2011Assignee: Emisphere Technologies, Inc.Inventors: Satej Bhandarkar, Shingai Majuru, Halina Leuchyk
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Publication number: 20110040094Abstract: Compounds that are 1,3,4-trisubstituted benzenes which modulate (e.g., inhibit) the activity of ?-secretase. The compounds are expected to reduce the level of A?42 in patients and be useful in the treatment of diseases (e.g., Alzheimer's disease) characterized by elevated levels of A?42 and/or the formation of A? plaques.Type: ApplicationFiled: September 15, 2008Publication date: February 17, 2011Applicant: ENVIVO PHARMACEUTICALS, INC.Inventors: Gideon Shapiro, Richard Chesworth
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Publication number: 20110028463Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.Type: ApplicationFiled: July 2, 2008Publication date: February 3, 2011Applicant: Astellas Pharma Inc.Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo
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Patent number: 7879907Abstract: Novel 3-phenylpropanoic acid compounds have the general formula (I) below: and are formulated into pharmaceutical compositions for administration in human or veterinary medicine (in dermatology, and also in the field of cardiovascular diseases, immune diseases and/or lipid metabolism-related diseases), or, alternatively, into cosmetic compositions.Type: GrantFiled: December 7, 2009Date of Patent: February 1, 2011Assignee: Galderma Research & DevelopmentInventors: Jean-Guy Boiteau, Laurence Clary, Jean-Claude Pascal, Veronique Parnet