The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 544/399)
  • Patent number: 8987263
    Abstract: 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: Grant
    Filed: October 9, 2003
    Date of Patent: March 24, 2015
    Inventors: Meir Shinitzky, Irun R. Cohen, Raanan Margalit, Yaacov Herzig, Jeffrey Sterling, Gyorgy Toth, Istvan Miskolczi, Ferenc Rantal, Tivadar Tamas
  • Publication number: 20150045372
    Abstract: 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: Application
    Filed: October 24, 2014
    Publication date: February 12, 2015
    Inventors: Ashwin M. Krishnan, Tawfik Gharbaoui
  • Publication number: 20140371232
    Abstract: 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: Application
    Filed: December 18, 2012
    Publication date: December 18, 2014
    Inventors: Zhuorong Li, Xingyue Ji, Situ Xue, Guanghui Zheng, Yuhuan Li, Peizhen Tao, Jiandong Jiang
  • Patent number: 8912329
    Abstract: 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: Grant
    Filed: June 25, 2010
    Date of Patent: December 16, 2014
    Assignee: Bioversys AG
    Inventors: Ronald Schoenmakers, Wilfried Weber, Marc Gitzinger, Martin Fussenegger, Marcel Tigges, Peter Schneider
  • Publication number: 20140315786
    Abstract: 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: Application
    Filed: March 16, 2012
    Publication date: October 23, 2014
    Applicant: Catabasis Pharmaceuticals, Inc.
    Inventors: Michael R. Jirousek, Jill C. Milne, David Carney, Jean E. Bemis, Chi B. Vu
  • Publication number: 20140228357
    Abstract: 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: Application
    Filed: September 27, 2012
    Publication date: August 14, 2014
    Inventors: 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
  • Publication number: 20140161830
    Abstract: 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: Application
    Filed: November 25, 2013
    Publication date: June 12, 2014
    Applicant: Massachusetts Institute of Technology
    Inventors: Daniel Griffith Anderson, Kathryn Ann Whitehead, Joseph R. Dorkin, Arturo Jose Vegas, Yunlong Zhang
  • Patent number: 8685979
    Abstract: 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: Grant
    Filed: January 22, 2009
    Date of Patent: April 1, 2014
    Assignee: Nektar Therapeutics
    Inventors: Zhongxu Ren, Jennifer Riggs-Sauthier
  • Patent number: 8569071
    Abstract: 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: Grant
    Filed: September 8, 2009
    Date of Patent: October 29, 2013
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Subodh B. Nimkar, Subhasish Purkayastha, Darryl Pappin, Scott Daniels
  • Publication number: 20130225561
    Abstract: 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: Application
    Filed: October 21, 2011
    Publication date: August 29, 2013
    Inventors: Haifeng Tang, Alexander Pasternak, Lihu Yang, Shawn P. Walsh, Barbara Pio, Aurash Shahripour, Nardos Teumelsan
  • Patent number: 8492163
    Abstract: 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: Grant
    Filed: January 31, 2011
    Date of Patent: July 23, 2013
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Subhasish Purkayastha, Subhakar Dey, Scott B. Daniels
  • Publication number: 20130177507
    Abstract: 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: Application
    Filed: January 5, 2013
    Publication date: July 11, 2013
    Inventor: José Luis Córdova Rojas
  • Publication number: 20130064871
    Abstract: 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: Application
    Filed: March 7, 2011
    Publication date: March 14, 2013
    Applicant: L'OREAL
    Inventors: Herve Richard, Benoit Muller
  • Patent number: 8389772
    Abstract: 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: Grant
    Filed: August 29, 2008
    Date of Patent: March 5, 2013
    Assignee: Sika Technology AG
    Inventor: Urs Burckhardt
  • Publication number: 20130052585
    Abstract: 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: Application
    Filed: August 26, 2011
    Publication date: February 28, 2013
    Applicants: JSR CORPORATION, INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Ramakrishnan Ayothi, William D. Hinsberg, Sally A. Swanson, Gregory M. Wallraff
  • Patent number: 8357679
    Abstract: 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: Grant
    Filed: May 13, 2009
    Date of Patent: January 22, 2013
    Assignee: MSD Oss B.V.
    Inventors: Andrew John Cooke, Andrew Stanley Edwards, Fiona Elizabeth Andrews, David Jonathan Bennett, Olaf Nimz, Emma Louise Carswell
  • Patent number: 8334240
    Abstract: 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: Grant
    Filed: March 9, 2009
    Date of Patent: December 18, 2012
    Assignee: Nalco Company
    Inventor: Erick J. Acosta
  • Patent number: 8329751
    Abstract: 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: Grant
    Filed: March 14, 2008
    Date of Patent: December 11, 2012
    Assignee: Bracco Imaging S.p.A.
    Inventors: Aldo Balsamo, Armando Rossello, Elisa Nuti, Elisabetta Orlandini, Tiziano Tuccinardi
  • Patent number: 8329620
    Abstract: 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: Grant
    Filed: October 6, 2008
    Date of Patent: December 11, 2012
    Assignee: Nalco Company
    Inventor: Erick J. Acosta
  • Patent number: 8236565
    Abstract: 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: Grant
    Filed: May 29, 2007
    Date of Patent: August 7, 2012
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Subhasish Purkayastha, Subhakar Dey, Sasi Pillai
  • Patent number: 8188107
    Abstract: 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: Grant
    Filed: January 25, 2002
    Date of Patent: May 29, 2012
    Assignee: Purdue Pharma L.P.
    Inventors: Ronald M. Burch, Paul D. Goldenheim, Richard S. Sackler
  • Publication number: 20120052574
    Abstract: 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: Application
    Filed: March 28, 2011
    Publication date: March 1, 2012
    Applicant: Molecular Transfer, Inc.
    Inventors: Joel Jessee, Gulilat Gebeyehu
  • Publication number: 20110301350
    Abstract: 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: Application
    Filed: February 13, 2009
    Publication date: December 8, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Waldemar Pfrengle, Markus Frank, Thorsten Pachur, Guenther Huchler
  • Patent number: 8044048
    Abstract: 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: Grant
    Filed: January 4, 2007
    Date of Patent: October 25, 2011
    Assignee: Southern Research Institute
    Inventors: Gary Piazza, Robert Reynolds
  • Publication number: 20110232870
    Abstract: 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: Application
    Filed: March 26, 2010
    Publication date: September 29, 2011
    Inventors: Richard M. FLYNN, Michael G. COSTELLO, Michael J. BULINSKI, Daniel R. VITCAK, Phillip E. TUMA
  • Patent number: 8026231
    Abstract: 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: Grant
    Filed: March 28, 2006
    Date of Patent: September 27, 2011
    Assignee: CNRS
    Inventors: Guy Fournet, Gerard Anthony Quash, Jacques Gore
  • Patent number: 8022111
    Abstract: 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: Grant
    Filed: January 28, 2005
    Date of Patent: September 20, 2011
    Assignee: Sun Chemical Corporation
    Inventors: Shaun Lawrence Herlihy, Brian Rowatt
  • Publication number: 20110195242
    Abstract: 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: Application
    Filed: August 29, 2008
    Publication date: August 11, 2011
    Applicant: SIKA TECHNOLOGY AG
    Inventor: Urs Burckhardt
  • Patent number: 7968548
    Abstract: 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: Grant
    Filed: August 11, 2006
    Date of Patent: June 28, 2011
    Assignee: Palatin Technologies, Inc.
    Inventors: Shubh D. Sharma, Yi-Qun Shi, Kevin D. Burris, Zhijun Wu, Papireddy Purma, Yadi Reddy Bonuga
  • Publication number: 20110117591
    Abstract: 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: Application
    Filed: October 20, 2010
    Publication date: May 19, 2011
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Ching-Ying CHEUNG, Diane R. Gray, Stephen T. Yue
  • Patent number: 7932388
    Abstract: 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: Grant
    Filed: December 11, 2007
    Date of Patent: April 26, 2011
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Darryl J. C. Pappin, Sasi Pillai, James M. Coull
  • Patent number: 7906341
    Abstract: 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: Grant
    Filed: June 28, 2007
    Date of Patent: March 15, 2011
    Assignee: DH Technologies Development Pte, Ltd.
    Inventors: Subhasish Purkayastha, Subhakar Dey, Scott B. Daniels
  • Publication number: 20110021534
    Abstract: 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: Application
    Filed: March 7, 2008
    Publication date: January 27, 2011
    Applicant: ALBIREO AB
    Inventors: Anders Broo, Johan Gottfries, Michael Kossenjans, Li Lanna, Eva-Lotte Lindstedt-Alstermark, Kristina A. Nilsson, Bengt Ohlsson, Maria Thorstensson, Maria Boije, Olof Sjogren
  • Publication number: 20100298341
    Abstract: 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: Application
    Filed: December 11, 2008
    Publication date: November 25, 2010
    Inventors: Stephen A. Hitchcock, Wenyuan Qian, Albert Amegadzie
  • Publication number: 20100298328
    Abstract: 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: Application
    Filed: March 30, 2007
    Publication date: November 25, 2010
    Inventors: John J. Baldwin, David A. Claremon, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wenguang Zeng
  • Publication number: 20100280024
    Abstract: 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: Application
    Filed: October 13, 2008
    Publication date: November 4, 2010
    Inventors: Jigar Desai, Pravin S. Thombare, Mukul R. Jain, Pankaj Ramanbhai Patel
  • Patent number: 7812025
    Abstract: 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 whic
    Type: Grant
    Filed: August 11, 2006
    Date of Patent: October 12, 2010
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiro Matsumoto, Masakuni Kori, Mitsunori Kouno
  • Publication number: 20100228015
    Abstract: 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: Application
    Filed: April 23, 2010
    Publication date: September 9, 2010
    Inventors: Mitchell A. deLong, Jill M. McFadden, Susan M. Royalty, Eric J. Toone, Jeffrey D. Yingling
  • Publication number: 20100222239
    Abstract: 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: Application
    Filed: March 2, 2009
    Publication date: September 2, 2010
    Inventors: Erick J. Acosta, Peter A. Webber
  • Publication number: 20100190753
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-+related disease.
    Type: Application
    Filed: August 27, 2009
    Publication date: July 29, 2010
    Applicant: BELLUS Health (International) Limited
    Inventors: Xianqi KONG, Walter A. Szarek, Francine Gervais
  • Patent number: 7741323
    Abstract: 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: Grant
    Filed: April 13, 2005
    Date of Patent: June 22, 2010
    Assignees: 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
  • Patent number: 7727990
    Abstract: 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: Grant
    Filed: August 11, 2006
    Date of Patent: June 1, 2010
    Assignee: Palatin Technologies, Inc.
    Inventors: Shubh D. Sharma, Yi-Qun Shi, Kevin D. Burris, Zhijun Wu, Papireddy Purma, Yadi Reddy Bonuga
  • Publication number: 20100130507
    Abstract: Prostaglandin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.
    Type: Application
    Filed: November 6, 2009
    Publication date: May 27, 2010
    Applicant: NICOX S.A.
    Inventors: Ennio ONGINI, Valerio Chiroli, Francesca Benedini, Piero Del Soldato
  • Patent number: 7718704
    Abstract: 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: Grant
    Filed: February 24, 2005
    Date of Patent: May 18, 2010
    Assignee: IRM LLC
    Inventors: Shifeng Pan, Wenqi Gao, Nathanael Schiander Gray, Yuan Mi
  • Publication number: 20100087338
    Abstract: 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: Application
    Filed: October 6, 2008
    Publication date: April 8, 2010
    Inventor: Erick J. Acosta
  • Publication number: 20100087339
    Abstract: 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: Application
    Filed: March 9, 2009
    Publication date: April 8, 2010
    Inventor: Erick J. Acosta
  • Publication number: 20100084611
    Abstract: 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: Application
    Filed: October 6, 2008
    Publication date: April 8, 2010
    Inventors: Erick J. Acosta, Jeffery Caleb Clark
  • Publication number: 20100056545
    Abstract: 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: Application
    Filed: April 23, 2009
    Publication date: March 4, 2010
    Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Kye Jung SHIN, Hyung Kook LEE, Eun Joo ROH, Dong Jin KIM, Kyung Il CHOI, Hyewhon RHIM, Hye Jin CHUNG, Seon Hee SEO
  • Publication number: 20100041573
    Abstract: 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: Application
    Filed: October 22, 2009
    Publication date: February 18, 2010
    Applicant: The Procter & Gamble Company
    Inventors: Jean-Luc Philippe Bettiol, Alfred Busch, Hugo Denutte, Christophe Laudamiel, Peter Marie Kamiel Perneel, Marie Montserrat Sanchez-Pena, Johan Smets
  • Publication number: 20100029621
    Abstract: 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: Application
    Filed: May 13, 2009
    Publication date: February 4, 2010
    Inventors: Andrew John Cooke, Andrew Stanley Edwards, Fiona Elizabeth Andrews, David Jonathan Bennett, Olaf Nimz, Emma Louise Carswell