The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 544/399)
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Patent number: 8987263Abstract: Basic esters of fatty alcohols of the general formula: R1-O—CO-A or pharmaceutically acceptable salts thereof, wherein R1 is C12-C24 alkyl or C10-C24 alkenyl, and A is a residue containing at least one acyclic or cyclic amino group and/or at least one heteroaromatic ring containing a tertiary or quaternary nitrogen atom, are anti-inflammatory and immunomodulatory agents, useful in the treatment of immunologically-mediated inflammation, as adjuvants for antigens involved in both cellular and humoral responses.Type: GrantFiled: October 9, 2003Date of Patent: March 24, 2015Inventors: Meir Shinitzky, Irun R. Cohen, Raanan Margalit, Yaacov Herzig, Jeffrey Sterling, Gyorgy Toth, Istvan Miskolczi, Ferenc Rantal, Tivadar Tamas
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Publication number: 20150045372Abstract: The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to salts of compounds of Formula (I) and pharmaceutical compositions thereof.Type: ApplicationFiled: October 24, 2014Publication date: February 12, 2015Inventors: Ashwin M. Krishnan, Tawfik Gharbaoui
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Publication number: 20140371232Abstract: Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.Type: ApplicationFiled: December 18, 2012Publication date: December 18, 2014Inventors: Zhuorong Li, Xingyue Ji, Situ Xue, Guanghui Zheng, Yuhuan Li, Peizhen Tao, Jiandong Jiang
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Patent number: 8912329Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C?CH, C?N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.Type: GrantFiled: June 25, 2010Date of Patent: December 16, 2014Assignee: Bioversys AGInventors: Ronald Schoenmakers, Wilfried Weber, Marc Gitzinger, Martin Fussenegger, Marcel Tigges, Peter Schneider
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Publication number: 20140315786Abstract: The present invention relates to targeting an intracellular enzyme for release of covalently linked bioactives which results in a synergistic effect between the bioactives. The present invention relates to the use of bioactives that are directly connected covalently or through a covalent molecular linker which have increased therapeutic activity when released as the free bioactives by intracellular enzymes as compared to when the bioactives are administered individually (i.e. not covalently linked). Further, methods are described of administering to patients in need thereof, bioactives as linked bioactives having increased therapeutic activity. Accordingly, this invention also relates to methods of treating patients for certain diseases.Type: ApplicationFiled: March 16, 2012Publication date: October 23, 2014Applicant: Catabasis Pharmaceuticals, Inc.Inventors: Michael R. Jirousek, Jill C. Milne, David Carney, Jean E. Bemis, Chi B. Vu
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Publication number: 20140228357Abstract: The present invention relates to novel compounds as HIF-1? inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1?, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1?-mediated VEGFA expression.Type: ApplicationFiled: September 27, 2012Publication date: August 14, 2014Inventors: Kyeong Lee, Mi-Sun Won, Hwan-Mook Kim, Song-Kyu Park, Ki-Ho Lee, Chang-Woo Lee, Bo-Kyung Kim, Hyun-Seung Ban, Kyung-Sook Chung, Naik Ravi
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Publication number: 20140161830Abstract: Provided herein are lipidoids that may be prepared from the conjugate addition of alkylamines to acrylates. In some embodiments, provided lipidoids are biodegradable and may be used in a variety of drug delivery systems. Given the amino moiety of the lipidoids, they are well-suited for the delivery of polynucleotides, in addition to other agents. Nanoparticles containing the inventive lipidoids and polynucleotides have been prepared and have been shown to be effective in delivering siRNA.Type: ApplicationFiled: November 25, 2013Publication date: June 12, 2014Applicant: Massachusetts Institute of TechnologyInventors: Daniel Griffith Anderson, Kathryn Ann Whitehead, Joseph R. Dorkin, Arturo Jose Vegas, Yunlong Zhang
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Patent number: 8685979Abstract: The invention relates to (among other things) oligomer-diarylpiperazine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated diarylpiperazine compounds.Type: GrantFiled: January 22, 2009Date of Patent: April 1, 2014Assignee: Nektar TherapeuticsInventors: Zhongxu Ren, Jennifer Riggs-Sauthier
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Patent number: 8569071Abstract: The present teachings provide methods for analyzing one or more amine-containing compounds in one or more samples using isobaric labels and parent-daughter ion transition monitoring (PDITM). In various embodiments, the methods comprise the steps of: (a) labeling one or more amine-containing compounds with different isobaric tags from a set of isobaric tags, each isobaric tag comprising a reporter ion portion; (b) combining at least a portion of each of the isobarically labeled amine-containing compounds to produce a combined sample; (c) subjecting at least a portion of the combined sample to PDITM; (d) measuring the ion signal of one or more of the transmitted reporter ions; and (e) determining the concentration of one or more of the isobarically labeled amine-containing compounds based at least on a comparison of the measured ion signal of the corresponding reporter ion to one or more measured ion signals of a standard compound.Type: GrantFiled: September 8, 2009Date of Patent: October 29, 2013Assignee: DH Technologies Development Pte. Ltd.Inventors: Subodh B. Nimkar, Subhasish Purkayastha, Darryl Pappin, Scott Daniels
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Publication number: 20130225561Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 21, 2011Publication date: August 29, 2013Inventors: Haifeng Tang, Alexander Pasternak, Lihu Yang, Shawn P. Walsh, Barbara Pio, Aurash Shahripour, Nardos Teumelsan
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Patent number: 8492163Abstract: This invention pertains to methods, mixtures, kits and compositions pertaining to analyte determination by mass spectrometry using labeling reagents that comprise a nucleophilic reactive group that reacts with a functional group of an analyte to produce a labeled analyte. The labeling reagents can be used as isobaric sets, mass differential labeling sets or in a combination of isobaric and mass differential labeling sets.Type: GrantFiled: January 31, 2011Date of Patent: July 23, 2013Assignee: DH Technologies Development Pte. Ltd.Inventors: Subhasish Purkayastha, Subhakar Dey, Scott B. Daniels
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Publication number: 20130177507Abstract: An improved special molecule provides a useful composition with following formula: R1 R2 . . . C . . . wherein: R1 is a phenyl hydrazine PM 108.14 C is a Leucine 131.17 R2 is a methyl piperazina 111 100.16 339.69. The user friendly molecule inhibits Streptococcus mutans bacteria responsible for tooth decay and is especially useful in products used in oral hygiene.Type: ApplicationFiled: January 5, 2013Publication date: July 11, 2013Inventor: José Luis Córdova Rojas
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Publication number: 20130064871Abstract: The present invention relates to a cosmetic composition comprising the combination i) of at least one screening agent of the dibenzoylmethane derivative type and ii) of at least one specific merocyanine dicyano or cyanoacetate derivative. It also relates to a method for the photostabilization, with regard to radiation, of at least one screening agent of the dibenzoylmethane derivative type by an effective amount of at least one specific merocyanine dicyano or cyanoacetate derivative.Type: ApplicationFiled: March 7, 2011Publication date: March 14, 2013Applicant: L'OREALInventors: Herve Richard, Benoit Muller
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Patent number: 8389772Abstract: The present invention relates to aldehydes of the formula (I) which contain tertiary amino groups and at least one hydroxyl group. Aldehydes of this kind can be utilized broadly. Aldehydes of particular advantage can be incorporated into a polymer, and find use as curing agents and/or catalysts. Preferably they find use in adhesives and sealants.Type: GrantFiled: August 29, 2008Date of Patent: March 5, 2013Assignee: Sika Technology AGInventor: Urs Burckhardt
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Publication number: 20130052585Abstract: Provided are novel symmetrical and asymmetrical bifunctional photodecomposable bases (PDBs) with dicarboxylate anion groups that show increased imaging performance. Also provided are photoresist compositions prepared with the bifunctional dicarboxylated PDBs and lithography methods that use the photoresist compositions of the present invention.Type: ApplicationFiled: August 26, 2011Publication date: February 28, 2013Applicants: JSR CORPORATION, INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Ramakrishnan Ayothi, William D. Hinsberg, Sally A. Swanson, Gregory M. Wallraff
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Patent number: 8357679Abstract: The present invention relates to hexafluoroisopropanol derivatives having the general formula I to pharmaceutical compositions comprising the same and to the use of these hexafluoroisopropanol derivatives in the treatment of atherosclerosis.Type: GrantFiled: May 13, 2009Date of Patent: January 22, 2013Assignee: MSD Oss B.V.Inventors: Andrew John Cooke, Andrew Stanley Edwards, Fiona Elizabeth Andrews, David Jonathan Bennett, Olaf Nimz, Emma Louise Carswell
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Patent number: 8334240Abstract: One or more compositions and methods for inhibiting the formation of hydrate agglomerates in a fluid that contain a specified generic formula are disclosed. The fluid can be contained in an oil or gas pipeline or refinery.Type: GrantFiled: March 9, 2009Date of Patent: December 18, 2012Assignee: Nalco CompanyInventor: Erick J. Acosta
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Patent number: 8329620Abstract: One or more compositions and methods for inhibiting the formation of hydrate agglomerates in an aqueous medium that contain a specified generic formula are disclosed. The aqueous medium can be contained in an oil or gas pipeline or refinery.Type: GrantFiled: October 6, 2008Date of Patent: December 11, 2012Assignee: Nalco CompanyInventor: Erick J. Acosta
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Patent number: 8329751Abstract: The invention relates to aryl-sulphonamido compounds endowed with inhibitory activity against metallo proteases MMP, having formula (I) below wherein R, R1, R2, R3, R4, R5, n and m have the meanings reported in the specification; the invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders.Type: GrantFiled: March 14, 2008Date of Patent: December 11, 2012Assignee: Bracco Imaging S.p.A.Inventors: Aldo Balsamo, Armando Rossello, Elisa Nuti, Elisabetta Orlandini, Tiziano Tuccinardi
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Patent number: 8236565Abstract: In various aspects, the present teachings provide labeling reagents and sets of labeling reagents for the relative quantitation, absolute quantitation, or both, of hydroxylated compounds including, but not limited to, hydroxylated ring containing compounds, steroids and sterols. In various aspects, the present teachings also provide methods for the analysis hydroxylated compounds including, but not limited to, hydroxylated ring containing compounds, steroids and sterols my MS/MS methods.Type: GrantFiled: May 29, 2007Date of Patent: August 7, 2012Assignee: DH Technologies Development Pte. Ltd.Inventors: Subhasish Purkayastha, Subhakar Dey, Sasi Pillai
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Patent number: 8188107Abstract: Disclosed is a pharmaceutical composition, comprising two analgesic compounds and/or pharmaceutically acceptable salts thereof consisting of N-[3 -(formylamino)-4-oxo-6-phenoxy-4H-1-benzopyran-7-yl] methanesulfonamide and/or at least one a pharmaceutically acceptable salt thereof and a-dose oxycodone and/or at least one a pharmaceutically acceptable salt thereof, the two analgesic compounds in an amount sufficient to provide an analgesic effect in a human patient. Also disclosed is a method of effectively treating pain in humans or other mammals, comprising orally administering to the patient a an oral dosage form comprising two analgesic compounds consisting of N-[3-(formylamino)-4-oxo-6 -phenoxy-4H-1-benzopyran-7-yl] methanesulfonamide and/or at least one a pharmaceutically acceptable salt thereof and oxycodone and/or at least one a pharmaceutically acceptable salt thereof such that the two analgesic compounds in an amount sufficient to provide an analgesic effect in a human patient.Type: GrantFiled: January 25, 2002Date of Patent: May 29, 2012Assignee: Purdue Pharma L.P.Inventors: Ronald M. Burch, Paul D. Goldenheim, Richard S. Sackler
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Publication number: 20120052574Abstract: Compositions and methods for improved delivery of macromolecules into eukaryotic cells are provided. Fusogenic peptides from fusion proteins of non-enveloped viruses enhance the efficiency of transfection of eukaryotic cells mediated by transfection agents such as cationic lipids, polycationic polymers such as PEI and dendrimers. These fusogenic peptides are used as part of a transfection complex that efficiently delivers a macromolecule, for example, a nucleic acid, into a eukaryotic cell. Novel cationic lipids and compositions of cationic lipids also are provided that may be used for the introduction of macromolecules such as nucleic acids, proteins and peptides into a variety of cells and tissues. The lipids can be used alone, in combination with other lipids and/or in combination with fusogenic peptides to prepare transfection complexes.Type: ApplicationFiled: March 28, 2011Publication date: March 1, 2012Applicant: Molecular Transfer, Inc.Inventors: Joel Jessee, Gulilat Gebeyehu
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Publication number: 20110301350Abstract: The present invention relates to a process for preparing compounds of general formula I wherein m, n, o, R1, R2 and R3 are defined as mentioned hereinafter, the enantiomers thereof and the diastereomers thereof, which are particularly suitable for preparing compounds of general formula II wherein m, o, R1, R2, R3 and R4 are defined as mentioned hereinafter. The compounds of general formula II have B1-antagonistic properties.Type: ApplicationFiled: February 13, 2009Publication date: December 8, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Waldemar Pfrengle, Markus Frank, Thorsten Pachur, Guenther Huchler
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Patent number: 8044048Abstract: Derivatives of sulindac are provided along with pharmaceutical compositions containing them and use for precancerous conditions and treating cancer. Derivatives of sulindac are also suitable for treating chronic inflammatory conditions. A method for preparing the derivatives is also provided.Type: GrantFiled: January 4, 2007Date of Patent: October 25, 2011Assignee: Southern Research InstituteInventors: Gary Piazza, Robert Reynolds
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Publication number: 20110232870Abstract: Nitrogen-containing fluorochemical ketones are provided that can be useful in apparatuses that includes a device and a mechanism for transferring heat. The provided fluorochemical ketones are stable at temperatures above 170° C., are environmentally friendly, and are economical to produce. The provided apparatuses can be useful for vapor phase soldering of electronic devices.Type: ApplicationFiled: March 26, 2010Publication date: September 29, 2011Inventors: Richard M. FLYNN, Michael G. COSTELLO, Michael J. BULINSKI, Daniel R. VITCAK, Phillip E. TUMA
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Aminothiolester compounds, pharmaceutical and cosmetic compositions containing same and uses thereof
Patent number: 8026231Abstract: The invention relates to novel aminothiol ester compounds having the general formula (I): and to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (cancers and precancers, dermatological, rheumatic and ophthalmological complaints in particular) or in cosmetic compositions. The invention also relates to a pharmaceutical or cosmetic composition, characterized in that it comprises, as active agent, a compound of general formula (I) in combination with a pharmaceutically or cosmetically acceptable support.Type: GrantFiled: March 28, 2006Date of Patent: September 27, 2011Assignee: CNRSInventors: Guy Fournet, Gerard Anthony Quash, Jacques Gore -
Patent number: 8022111Abstract: Compounds of formula (I) [in which: A and B are terminal groups; R1 represents a group of formula (II) or (III); R2 is alkyl or aryl; Z is a group —(CHR3)n, where R3 is hydrogen, hydroxy or alkyl, and n is a number from 0 to 6; Y is carbonyl or a group —CH2—; Q represents a residue of a dihydroxy compound; and x is a number from 1 to 100] are useful sensitisers for use with Type II photoinitiators in the formulation of printing inks and other energy curable coatings.Type: GrantFiled: January 28, 2005Date of Patent: September 20, 2011Assignee: Sun Chemical CorporationInventors: Shaun Lawrence Herlihy, Brian Rowatt
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Publication number: 20110195242Abstract: The present invention relates to aldehydes of the formula (I) which contain tertiary amino groups and at least one hydroxyl group. Aldehydes of this kind can be utilized broadly. Aldehydes of particular advantage can be incorporated into a polymer, and find use as curing agents and/or catalysts.Type: ApplicationFiled: August 29, 2008Publication date: August 11, 2011Applicant: SIKA TECHNOLOGY AGInventor: Urs Burckhardt
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Patent number: 7968548Abstract: Melanocortin receptor-specific compounds with diamine groups of the general formula and pharmaceutically acceptable salts thereof, where W is a diamine heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, J, Q, L1, L2, L3, R1a, R1b, R2a, R2b and X are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.Type: GrantFiled: August 11, 2006Date of Patent: June 28, 2011Assignee: Palatin Technologies, Inc.Inventors: Shubh D. Sharma, Yi-Qun Shi, Kevin D. Burris, Zhijun Wu, Papireddy Purma, Yadi Reddy Bonuga
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Publication number: 20110117591Abstract: Chemical stain compounds containing a fluorophore and a reducible quenching unit are disclosed. The reducible quenching unit quenches the fluorophore while in its oxidized state. Upon reduction, the quenching properties of the quenching unit are diminished or eliminated. The chemical compounds can be used in a variety of applications, including the detection of bacterial cells, monitoring the electron transport chain function of bacterial cells, monitoring the oxidation state of non-biological systems, and assaying the effectiveness of antibacterial or antimicrobial agents.Type: ApplicationFiled: October 20, 2010Publication date: May 19, 2011Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Ching-Ying CHEUNG, Diane R. Gray, Stephen T. Yue
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Patent number: 7932388Abstract: In some embodiments, this invention pertains to isotopically enriched N-substituted piperazines. In some embodiments, this invention pertains to methods for the preparation of isotopically enriched N-substituted piperazines.Type: GrantFiled: December 11, 2007Date of Patent: April 26, 2011Assignee: DH Technologies Development Pte. Ltd.Inventors: Darryl J. C. Pappin, Sasi Pillai, James M. Coull
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Patent number: 7906341Abstract: This invention pertains to methods, mixtures, kits and compositions pertaining to analyte determination by mass spectrometry using labeling reagents that comprise a nucleophilic reactive group that reacts with a functional group of an analyte to produce a labeled analyte. The labeling reagents can be used as isobaric sets, mass differential labeling sets or in a combination of isobaric and mass differential labeling sets.Type: GrantFiled: June 28, 2007Date of Patent: March 15, 2011Assignee: DH Technologies Development Pte, Ltd.Inventors: Subhasish Purkayastha, Subhakar Dey, Scott B. Daniels
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Publication number: 20110021534Abstract: The present invention relates to 2-(substituted sulphur, sulphone or sulphoxide)-3-(substituted phenyl) propionic acid derivatives, 2-(substituted oxygen)-3-(substituted phenyl) propionic acid derivatives, benzoic acid derivatives, and derivatives of 2-methyl-2-(phenoxy or phenylthio)propanoic acid and 2-(methylor ethyl)-2-(phenoxy or phenylthio)butanoic acid, to processes for preparing such compounds, to their use in the treatment of inflammatory conditions, and to pharmaceutical compositions containing them.Type: ApplicationFiled: March 7, 2008Publication date: January 27, 2011Applicant: ALBIREO ABInventors: Anders Broo, Johan Gottfries, Michael Kossenjans, Li Lanna, Eva-Lotte Lindstedt-Alstermark, Kristina A. Nilsson, Bengt Ohlsson, Maria Thorstensson, Maria Boije, Olof Sjogren
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Publication number: 20100298328Abstract: 1-Heterocyclylamino-2-hydroxy-3-amino-?-arylalkanes of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, medicinally active ingredients.Type: ApplicationFiled: March 30, 2007Publication date: November 25, 2010Inventors: John J. Baldwin, David A. Claremon, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wenguang Zeng
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Publication number: 20100298341Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: ApplicationFiled: December 11, 2008Publication date: November 25, 2010Inventors: Stephen A. Hitchcock, Wenyuan Qian, Albert Amegadzie
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Publication number: 20100280024Abstract: The present invention relates to renin inhibitors of formula (I), their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (I), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.Type: ApplicationFiled: October 13, 2008Publication date: November 4, 2010Inventors: Jigar Desai, Pravin S. Thombare, Mukul R. Jain, Pankaj Ramanbhai Patel
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Patent number: 7812025Abstract: A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R1 represents an aryl or heterocyclic group which may be substituted, provided that R1 is not a 3-ethyl-6-methoxy-2-methyl-5-naphthalen-1-yl group; R1a represents a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxyl group or the like; R2 represents a piperidin-1,4-diyl or piperazin-1,4-diyl which may be substituted; R3 represents a bivalent group which is formed by removing two hydrogen atoms from a benzene ring or 6-membered aromatic heterocyclic ring which may have a substituent, provided that R3 is not a pyridazin-3,6-diyl; and R4 represents a group which is formed by removing one hydrogen atom from a benzene ring or 5- to 6-membered heterocyclic ring which may be substituted, provided that the substituent on the heterocyclic ring is not a phenylethyl group whicType: GrantFiled: August 11, 2006Date of Patent: October 12, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiro Matsumoto, Masakuni Kori, Mitsunori Kouno
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Publication number: 20100228015Abstract: This invention relates to novel homotopic prodrugs and medicaments and methods for their preparation, testing and use. In one embodiment, the homotopic prodrug has the general formula wherein is a biologically-active moiety comprising a carboxylic acid functional group, and Rb is a homotopically-symmetrical alcohol bonded to the biologically-active moiety through the carboxylic acid functional group to form an ester linkage, as well as optical isomers, enantiomers, pharmaceutically acceptable salts, biohydrolyzable amides, esters, and imides thereof and combinations thereof.Type: ApplicationFiled: April 23, 2010Publication date: September 9, 2010Inventors: Mitchell A. deLong, Jill M. McFadden, Susan M. Royalty, Eric J. Toone, Jeffrey D. Yingling
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Publication number: 20100222239Abstract: One or more compositions and methods for inhibiting the formation of hydrate agglomerates in a fluid comprising water, gas, and optionally liquid hydrocarbon are disclosed. The fluid can be contained in an oil or gas pipeline or refinery.Type: ApplicationFiled: March 2, 2009Publication date: September 2, 2010Inventors: Erick J. Acosta, Peter A. Webber
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Publication number: 20100190753Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-+related disease.Type: ApplicationFiled: August 27, 2009Publication date: July 29, 2010Applicant: BELLUS Health (International) LimitedInventors: Xianqi KONG, Walter A. Szarek, Francine Gervais
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Patent number: 7741323Abstract: An indene derivative for selectively modulating the activities of peroxisome proliferator activated receptors (PPARs) having the following formula (I): wherein, R1 is C1-6 alkyl, C1-6 alkenyl, or C3-6 cycloalkyl, each of which is unsubstituted or substituted with one or more phenyl groups; R2 is H, CN, CO2Ra, CH2CO2Ra, CONRbRc, or phenyl; R3 is C1-6 alkyl, C3-6 cycloalkyl, naphthyl, phenyl, being each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, CN, NH2, NO2, ORa, phenyloxy, C1-6 alkyl, and C3-6 cycloalkyl; and R4, R5, R6, and R7 are each independently H, OH, OSO2CH3, O(CH2)mRe, CH2Rf, OCOCH2ORg, OCH2CH2ORg, OCH2CH?CHRg, or pyridine-2-yloxy, or R5 and R6 together form OCH2O.Type: GrantFiled: April 13, 2005Date of Patent: June 22, 2010Assignees: Korea Research Institute of Chemical Technology, Jeil Pharm. Co., Ltd., Korea Research Institute of Bioscience and Biotechnology, CJ Corp.Inventors: Hyae Gyeong Cheon, Sung-Eun Yoo, Sung Soo Kim, Sung-Don Yang, Kwang-Rok Kim, Sang Dal Rhee, Jin Hee Ahn, Seung Kyu Kang, Won Hoon Jung, Sung Dae Park, Nam Gee Kim, Jang Hyuk Lee, Sun Chul Huh, Jae Mok Lee, Seog Beom Song, Soon Ji Kwon, Jong Hoon Kim, Jeong-Hyung Lee, Seung Jun Kim
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Patent number: 7727990Abstract: Melanocortin receptor-specific compounds of the general formula and pharmaceutically acceptable salts thereof, where X, W, J, Q, L1, L2, L3, R1a, R1b, R2a, and R2b are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.Type: GrantFiled: August 11, 2006Date of Patent: June 1, 2010Assignee: Palatin Technologies, Inc.Inventors: Shubh D. Sharma, Yi-Qun Shi, Kevin D. Burris, Zhijun Wu, Papireddy Purma, Yadi Reddy Bonuga
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Publication number: 20100130507Abstract: Prostaglandin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.Type: ApplicationFiled: November 6, 2009Publication date: May 27, 2010Applicant: NICOX S.A.Inventors: Ennio ONGINI, Valerio Chiroli, Francesca Benedini, Piero Del Soldato
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Patent number: 7718704Abstract: The invention provides a novel class of cyclic oximes of Formula I: wherein A, X, Y, Z, W, R1, R2, R3 and n are as described in the summary of the invention; useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.Type: GrantFiled: February 24, 2005Date of Patent: May 18, 2010Assignee: IRM LLCInventors: Shifeng Pan, Wenqi Gao, Nathanael Schiander Gray, Yuan Mi
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Publication number: 20100087338Abstract: One or more compositions and methods for inhibiting the formation of hydrate agglomerates in an aqueous medium that contain a specified generic formula are disclosed. The aqueous medium can be contained in an oil or gas pipeline or refinery.Type: ApplicationFiled: October 6, 2008Publication date: April 8, 2010Inventor: Erick J. Acosta
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Publication number: 20100084611Abstract: One or more methods for inhibiting corrosion in an aqueous medium that contain a composition with a specified generic formula are disclosed. The aqueous medium can be contained in an oil or gas pipeline or refinery.Type: ApplicationFiled: October 6, 2008Publication date: April 8, 2010Inventors: Erick J. Acosta, Jeffery Caleb Clark
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Publication number: 20100087339Abstract: One or more compositions and methods for inhibiting the formation of hydrate agglomerates in a fluid that contain a specified generic formula are disclosed. The fluid can be contained in an oil or gas pipeline or refinery.Type: ApplicationFiled: March 9, 2009Publication date: April 8, 2010Inventor: Erick J. Acosta
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Publication number: 20100056545Abstract: Disclosed herein are a new phenylacetate derivative represented by Chemical Formula 1 or pharmaceutically acceptable salt thereof, a preparation method thereof, and a composition for prevention or treatment of diseases induced by the activation of T-type calcium ion channels containing the same. The composition containing the phenylacetate derivative according to the present invention effectively inhibits the activation of T-type calcium ion channels and may be useful in the prevention or treatment of diseases such as hypertension, cancer, epilepsy, and neurogenic pains induced by the activation of T-type calcium ion channels. wherein, X, R1, and R3 are as defined herein.Type: ApplicationFiled: April 23, 2009Publication date: March 4, 2010Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Kye Jung SHIN, Hyung Kook LEE, Eun Joo ROH, Dong Jin KIM, Kyung Il CHOI, Hyewhon RHIM, Hye Jin CHUNG, Seon Hee SEO
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Publication number: 20100041573Abstract: The present invention relates to a product of reaction between a primary and/or secondary amine and one or more active ingredients. By the present invention, there is provided a release of the active component over a longer period of time than by the use of the active itself.Type: ApplicationFiled: October 22, 2009Publication date: February 18, 2010Applicant: The Procter & Gamble CompanyInventors: Jean-Luc Philippe Bettiol, Alfred Busch, Hugo Denutte, Christophe Laudamiel, Peter Marie Kamiel Perneel, Marie Montserrat Sanchez-Pena, Johan Smets
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Publication number: 20100029621Abstract: The present invention relates to hexafluoroisopropanol derivatives having the general formula I to pharmaceutical compositions comprising the same and to the use of these hexafluoroisopropanol derivatives in the treatment of atherosclerosis.Type: ApplicationFiled: May 13, 2009Publication date: February 4, 2010Inventors: Andrew John Cooke, Andrew Stanley Edwards, Fiona Elizabeth Andrews, David Jonathan Bennett, Olaf Nimz, Emma Louise Carswell