Plural Rings Patents (Class 562/435)
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Patent number: 9018414Abstract: The present application relates to novel 3-phenylpropionic acid 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: October 3, 2013Date of Patent: April 28, 2015Assignee: Bayer Intellectual Property GmbHInventors: Thomas Lampe, Michael Hahn, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Sherif El Sheikh, Volkhart Min-Jian Li, Eva-Maria Becker-Pelster, Friederike Stoll, Andreas Knorr
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Publication number: 20150064455Abstract: This invention relates to the direct grafting of a calixarene mostly onto the surface of a material, as well as to a grafting process, and certain calixarene intermediates useful for carrying the grafting process.Type: ApplicationFiled: March 28, 2013Publication date: March 5, 2015Inventors: Ivan Jabin, Alice Mattiuzzi, Corlnne Lagrost, Philippe Hapiot, Olivia Reinaud
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Publication number: 20140249306Abstract: The present invention provides a novel compound having an antiviral action, in particular, an HIV replication inhibiting action, as well as a pharmaceutical composition, in particular, an anti-HIV agent. wherein, a broken line means the presence or absence of a bond; R1 is substituted or unsubstituted alkyl etc., R2 is substituted or unsubstituted alkyloxy etc.; n is 1 or 2; R3 is a substituted or unsubstituted aromatic carbocyclic group; R4 is a hydrogen atom etc.; R5 is a substituted or unsubstituted aromatic carbocyclic group etc.; Y is a single bond etc.; R6 is substituted or unsubstituted alkyl; R7 is —Z—R71 etc.; Z is —NR72—CO— etc.; R71 is substituted or unsubstituted alkyl etc.; R72 is a hydrogen atom etc.Type: ApplicationFiled: October 25, 2012Publication date: September 4, 2014Applicant: Shionogi & Co., Ltd.Inventors: Tsutomu Iwaki, Kenji Tomita
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Publication number: 20140107085Abstract: The invention includes compositions comprising selective AKR1C3 inhibitors. The invention also includes compositions comprising bifunctional AKR1C3 inhibitors and selective androgen receptor modulators. The invention further includes methods of treatment using the compositions of the invention.Type: ApplicationFiled: October 10, 2013Publication date: April 17, 2014Applicant: The Trustees of The University of PennsylvaniaInventors: Trevor M. Penning, Adegoke O. Adeniji, Michael C. Burns, Jeffrey Winkler, Barry Twenter
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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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Publication number: 20130331452Abstract: Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula (I). The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, cognitive impairment, early-onset essential hypertension, and Plasmodium falciparum-induced inflammation. In Formula I, t, q, r, R6, R7, X and A are as defined herein.Type: ApplicationFiled: September 6, 2011Publication date: December 12, 2013Applicant: WELLSTAT THERAPEUTICS CORPORATIONInventors: Shalini Sharma, Reid W von Borstel
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Patent number: 8586782Abstract: Compounds of formula (I) pharmaceutically acceptable salts thereof; and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.Type: GrantFiled: September 12, 2012Date of Patent: November 19, 2013Assignee: Novartis AGInventors: Lauren G. Monovich, Benjamin Biro Mugrage
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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: 8362294Abstract: Compounds of formula (I) pharmaceutically acceptable salts thereof, and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.Type: GrantFiled: June 25, 2007Date of Patent: January 29, 2013Assignee: Novartis AGInventors: Lauren G. Monovich, Benjamin Biro Mugrage
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Publication number: 20130018202Abstract: The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) in which A, D, G, W, X, Y and Z are as defined above, to a plurality of processes for the preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to selective herbicidal compositions comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) and a crop plant compatibility-improving compound.Type: ApplicationFiled: January 11, 2012Publication date: January 17, 2013Applicant: Bayer CropScience AGInventors: Reiner Fischer, Thomas Bretschneider, Ernst Rudolf F. Gesing, Dieter Feucht, Karl-Heinz Kuck, Peter Lösel, Olga Malsam, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne
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Publication number: 20120289602Abstract: The present invention relates to a pharmaceutical composition and the method of use for treating or preventing burn injury in patients or subjects in need, including the compound represented by the specific chemical formula as an active ingredient or its pharmaceutically acceptable salts or solvates.Type: ApplicationFiled: April 5, 2010Publication date: November 15, 2012Inventors: Byoung-Joo Gwag, Ui-Jin Park
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Patent number: 8309767Abstract: The invention relates to 2-aminobenzoyl-alkylamines, -alkylamides and -alkylthioamides, and their application for treatment or prevention of various physiological conditions.Type: GrantFiled: June 24, 2004Date of Patent: November 13, 2012Assignee: Neurim Pharmaceuticals (1991) Ltd.Inventors: Nava Zisapel, Moshe Laudon, Dvorah Daily
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Patent number: 8299123Abstract: The invention relates to a compound of formula (I): or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.Type: GrantFiled: October 14, 2008Date of Patent: October 30, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Kaka Dey, Donghong Amy Gao, Daniel R. Goldberg, Alexander Heim-Riether, John Edward Mangette, Ingo Andreas Mugge, Roger John Snow, Alan David Swinamer, Jiang-Ping Wu, Zhaoming Xiong, Yu Yang
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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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Publication number: 20120201803Abstract: A process for forming a solid electrolytic capacitor and an electrolytic capacitor formed by the process. The process includes: providing an anode wherein the anode comprises a porous body and an anode wire extending from the porous body; applying a thin polymer layer onto the dielectric, and forming a dielectric on the porous body to form an anodized anode; applying a first slurry to the anodized anode to form a blocking layer wherein the first slurry comprises a first conducting polymer with an median particle size of at least 0.05 ?m forming a layer of crosslinker on the blocking layer; and applying a layer of a second conducting polymer on the layer of crosslinker.Type: ApplicationFiled: September 15, 2011Publication date: August 9, 2012Applicant: WELLSTAT THERAPEUTICS CORPORATIONInventors: Shalini Sharma, James Dennen O'Neil, Reid W. von Borstel, Ramchandran Arudchandran
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Patent number: 8211878Abstract: The present invention provides methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death in a patient. The invention includes use of 5-benzylamino salicylic acid (BAS) and its derivatives. Thus, the present invention provides methods for reducing neuronal death in nervous system injuries resulting from amyotrophic lateral sclerosis.Type: GrantFiled: May 24, 2010Date of Patent: July 3, 2012Assignee: Neurotech Pharmaceuticals Co., Ltd.Inventors: Byoung Joo Gwag, Young Ae Lee, Bo Rum Ryu, Sung Hwa Yoon, Ho Sang Moon
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Patent number: 8211877Abstract: The present invention provides compositions and methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death. The invention includes synthesis of 5-benzylamino salicylic acid (BAS) and its derivatives. BAS and its derivatives protect cortical neurons from toxic insults by N-methyl-D-aspartate, Zn2+, and reactive oxygen species. Thus, the present invention provides compositions and methods for treating stroke, traumatic brain and spinal cord injury, epilepsy, and neurodegenerative diseases that are accompanied by severe neuronal loss via excitotoxicity, Zn2+ neurotoxicity, and free radical neurotoxicity.Type: GrantFiled: May 24, 2010Date of Patent: July 3, 2012Assignee: Neurotech Pharmaceuticals Co., Ltd.Inventors: Byoung Joo Gwag, Young Ae Lee, Bo Rum Ryu, Sung Hwa Yoon, Ho Sang Moon
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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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Patent number: 8138369Abstract: A process for producing an adsorbent where a metal oxide is reacted with an alkoxy silane to produce an epoxy-functionalized metal oxide. This product is reacted with an amino-substituted propionic acid and a nitro-substituted fluorenone, and this product is grafted to the epoxy-functionalized metal oxide. This grafted product is the adsorbent, which may be contacted with a hydrocarbon mixture having at least one sulfur containing compound in order to remove this sulfur containing compound. Also disclosed is a process for adding polymerization groups to an adsorbent.Type: GrantFiled: June 6, 2008Date of Patent: March 20, 2012Assignee: Chevron U.S.A. Inc.Inventors: Xiaolin Wei, Scott Michael Husson, Marcus V. Dutra e Mello, Daniel Chinn
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Patent number: 8129087Abstract: A block copolymer that can form selectively a microphase-separated structure under exposure with an ultraviolet exposure device, and a substrate processing method by which a micropattern can be formed at a low cost on the substrate by using the block copolymer. The block copolymer has as a basic skeleton a hydrophobic block that has a repeating structure of a hydrophobic monomer and a hydrophilic block that has a repeating structure of a hydrophilic monomer having a hydrophilic functional group. At least some of the hydrophilic functional groups are covered with a hydrophobic protective group and the hydrophobic protective group, which covers the hydrophilic functional group, is dissociated from the hydrophilic functional group by light irradiation. The substrate processing method uses the block copolymer to form a micropattern on the substrate.Type: GrantFiled: June 10, 2009Date of Patent: March 6, 2012Assignee: Canon Kabushiki KaishaInventor: Toshiki Ito
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Publication number: 20120016158Abstract: There is provided a novel loxoprofen derivative that has no side effect such as a gastrointestinal disorder and also has excellent anti-inflammatory and analgesic effects and is represented by the following formula (I) or (II): (wherein R1 and R2 each represent a halogen atom or a substituted or unsubstituted phenyl group) or a pharmacologically acceptable salt thereof. In the derivative, the halogen atom is selected from a chlorine atom, a bromine atom, a fluorine atom, and an iodine atom, and a substituent of the substituted phenyl group is a halogen atom, a hydroxyl group, a substituted or unsubstituted lower alkyl group, a lower alkylthio group, a lower alkoxy group, a nitro group, an amino group, or a carboxyl group.Type: ApplicationFiled: February 18, 2010Publication date: January 19, 2012Applicants: LTT BIO-PHARMA CO., LTD., National University Corporation, Kumamoto UniversityInventors: Toru Mizushima, Masami Ohtsuka, Yoshinari Okamoto, Naoki Yamakawa
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Publication number: 20110281898Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: July 26, 2011Publication date: November 17, 2011Inventors: Roger Victor Bonnert, Anil Patel, Stephen Thom
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Publication number: 20110166117Abstract: The invention relates to substituted phenoxyacetic acids (I) as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: December 30, 2010Publication date: July 7, 2011Inventors: Roger Bonnert, Stephen Brough, Andrew Davies, Timothy Luker, Thomas McInally, Ian Millichip, Garry Pairaudeau, Anil Patel, Rukhsana Rasul, Stephen Thom
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Publication number: 20110152543Abstract: The present invention describes a novel process for the preparation of optically active (S)-(?)-2-(N-propylamino)-5-methoxytetraline and (S)-(?)-2-(N-propylamino)-5-hydroxytetraline compounds based on the optical resolution of mixtures of the enantiomers of 2-(N-propylamino)-5-methoxytetraline and 2-(N-propylamino)-5-hydroxytetraline respectively. This process comprises (a) reacting a mixture of the enantiomers of said compounds with an optically active organic acid to form diastereoisomeric salts and separating the salts by crystallization. Said compounds are useful in the preparation of (6S)-(?)-5,6,7,8-tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-1-naphthol (Rotigotine). Rotigotine is a dopamine agonist and is indicated for the treatment of Parkinson's disease.Type: ApplicationFiled: October 9, 2009Publication date: June 23, 2011Inventors: Francisco Marquillas Olondriz, Marta Pomares Marco
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Publication number: 20110071197Abstract: 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: April 16, 2009Publication date: March 24, 2011Inventors: Peter Nilsson, Martins Katkevics, Benjamin Pelcman
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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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Publication number: 20110039851Abstract: The invention relates to a compound of formula (I): or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.Type: ApplicationFiled: October 14, 2008Publication date: February 17, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Kaka Dey, Donghong Amy Gao, Daniel R. Goldberg, Alexander Heim-Riether, John Edward Mangette, Ingo Andreas Mugge, Roger John Snow, Alan David Swinamer, Jiang-Ping Wu, Zhaoming Xiong, Yu Yang
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Patent number: 7888528Abstract: A photosensitive monolayer is self-assembled on an oxide surface. The chemical compound of the photosensitive monolayer has three components. A first end group provides covalent bonds with the oxide surface for self assembly on the oxide surface. A photosensitive group that dissociates upon exposure to ultraviolet radiation is linked to the first end group. A second end group linked to the photosensitive group provides hydrophobicity. Upon exposure to the ultraviolet radiation, the dissociated photosensitive group is cleaved and forms a hydrophilic derivative in the exposed region, rendering the exposed region hydrophilic. Carbon nanotubes or nanocrystals applied in an aqueous dispersion are selectively attracted to the hydrophilic exposed region to from electrostatic bonding with the hydrophilic surface of the cleaved photosensitive group.Type: GrantFiled: August 8, 2009Date of Patent: February 15, 2011Assignee: International Business Machines CorporationInventors: Ali Afzali-Ardakani, Teresita O. Graham, James B. Hannon, George S. Tulevski
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Publication number: 20100331570Abstract: The aim of the invention is to provide a widely applicable method for the nitration of substituted benzenes.Type: ApplicationFiled: February 21, 2008Publication date: December 30, 2010Applicant: SALTIGO GMBHInventors: Reinhard Langer, Matthias Gotta, Wolfram Kissener, Bettina Holzer
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Publication number: 20100330032Abstract: Compounds having the formula I wherein R1, R2, R3, R4, and R5 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: June 24, 2010Publication date: December 30, 2010Inventors: Elbert Chin, Javier de Vicente Fidalgo, Jim Li, Alfred Sui-Ting Lui, Kristen Lynn McCaleb, Ryan Craig Schoenfeld, Francisco Xavier Talamas
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Publication number: 20100286276Abstract: The present invention concerns substituted 1,3-diphenylpropane derivatives, pharmaceutical compositions comprising them and the therapeutic uses thereof, particularly in the field of human and animal health.Type: ApplicationFiled: June 21, 2007Publication date: November 11, 2010Applicant: GENFITInventors: Jean-Fancois Delhomel, Rémy Hanf, Karine Caumont-Bertrand
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Patent number: 7659396Abstract: The invention relates to an improved method for the production of 3-amidino- or 3-guanidinophenylalanine derivatives, especially triisopropylphenyl-sulfonyl-substituted 3-amidino- or 3-guanidinophenylalanine derivatives.Type: GrantFiled: May 16, 2007Date of Patent: February 9, 2010Assignee: Wilex AGInventors: Katja Wosikowski-Buters, Stefan Sperl, Joachim Sommer
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Publication number: 20100003616Abstract: A photosensitive monolayer is self-assembled on an oxide surface. The chemical compound of the photosensitive monolayer has three components. A first end group provides covalent bonds with the oxide surface for self assembly on the oxide surface. A photosensitive group that dissociates upon exposure to ultraviolet radiation is linked to the first end group. A second end group linked to the photosensitive group provides hydrophobicity. Upon exposure to the ultraviolet radiation, the dissociated photosensitive group is cleaved and forms a hydrophilic derivative in the exposed region, rendering the exposed region hydrophilic. Carbon nanotubes or nanocrystals applied in an aqueous dispersion are selectively attracted to the hydrophilic exposed region to from electrostatic bonding with the hydrophilic surface of the cleaved photosensitive group.Type: ApplicationFiled: August 8, 2009Publication date: January 7, 2010Inventors: Ali Afzali-Ardakani, Teresita O. Graham, James B. Hannon, George S. Tulevski
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Publication number: 20090322212Abstract: New, highly photoluminescent compounds are described having structural formula (I) wherein: R1, R2, R3, R4, independently from each other, represent H; alkyl, alkenyl; aryl; —(CH2CH2—O)n—CH3. These compounds are highly photoluminescent and have high quantum yield; they have optimal plasticity characteristics and optimal miscibility with other amorphous polymers; they lead to the formation of thin, stable and uniform layers of photoluminescent material, obtainable by simple techniques of deposition from solution. A simple and high yield process is described for obtaining the aforesaid compounds. In addition, the use of the compounds of formula (I) and their polymer derivatives is described in the preparation of electroluminescent devices, for example LEDs.Type: ApplicationFiled: June 26, 2008Publication date: December 31, 2009Applicant: STMICROELECTRONICS S.R.L.Inventors: Giovanna Salzillo, Antonio Roviello, Giuseppina Roviello, Giuseppe Russo
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Patent number: 7553873Abstract: The present invention relates to modulators of metalloproteinase activity.Type: GrantFiled: July 11, 2006Date of Patent: June 30, 2009Assignee: WyethInventors: Phaik-Eng Sum, Jerauld Stanley Skotnicki, Steve Yik-Kai Tam, Tarek Suhayl Mansour, David Brian How, Joshua James Sabatini, Jason Shaoyun Xiang, Eric Feyfant
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Publication number: 20090163547Abstract: The present invention makes reference to new indene derivatives with general formula (I), as well as to their preparation procedures, their application as medicament and the pharmaceutical compositions containing them. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.Type: ApplicationFiled: November 7, 2006Publication date: June 25, 2009Inventors: Maria De Las Ermitas Alcalde-Pais, Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria De Les Neus Mesquida-Estevez, Sara Lopez-Perez
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Publication number: 20090131527Abstract: The present invention relates to novel anthranilic acid derivatives represented by Chemical Formula I, and a chloride channel blocking agent containing the anthranilic acid derivative or its pharmacologically acceptable salts as an active ingredient. In another aspect, the present invention relates to a method of accurately and efficiently detecting the intracellular chloride channel inhibition and method of screening a chloride channel blocking agent.Type: ApplicationFiled: January 30, 2008Publication date: May 21, 2009Applicant: Korea Institute of Science and TechnologyInventors: Changjoon Justin Lee, Eun-Joo Roh, Soo-Jin Oh, Jung-Hwan Park, Jae-Kyun Lee
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Publication number: 20090076221Abstract: A process for producing an adsorbent where a metal oxide is reacted with an alkoxy silane to produce an epoxy-functionalized metal oxide. This product is reacted with an amino-substituted propionic acid and a nitro-substituted fluorenone, and this product is grafted to the epoxy-functionalized metal oxide. This grafted product is the adsorbent, which may be contacted with a hydrocarbon mixture having at least one sulfur containing compound in order to remove this sulfur containing compound. Also disclosed is a process for adding polymerization groups to an adsorbent.Type: ApplicationFiled: June 6, 2008Publication date: March 19, 2009Inventors: Xiaolin Wei, Scott Michael Husson, Marcus V. Dutra e Mello, Daniel Chinn
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Publication number: 20090036423Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.Type: ApplicationFiled: February 1, 2008Publication date: February 5, 2009Inventors: Shifeng Pan, Wenqi Gao, Nathanael S. Gray, Yuan Mi, Yi Fan
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Publication number: 20080255198Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, m, n, p and s are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases that are associated with the activation of the glycogen synthase enzyme, such as diabetes.Type: ApplicationFiled: June 13, 2008Publication date: October 16, 2008Inventors: Chang An Chu, Paul Gillespie, Jefferson Wright Tilley
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Patent number: 7314888Abstract: A compound or a salt thereof having the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, said atoms constitute the pharmacophore represented by the following formula: and inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases into which over expression of AP-1 participates and as an AP-1 inhibitor.Type: GrantFiled: November 5, 1999Date of Patent: January 1, 2008Assignee: Toyama Chemical Co., Ltd.Inventors: Hisaaki Chaki, Tadakazu Takakura, Keiichi Tsuchida, Hironori Kotsubo, Yukihiko Aikawa, Shuichi Hirono, Shunichi Shiozawa
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Patent number: 7247724Abstract: The invention relates to an improved method for the production of 3-amidinophenylalanine derivatives, especially triisopropylphenyl-sulfonyl-substituted 3-amidinophenylalanine derivatives.Type: GrantFiled: July 25, 2003Date of Patent: July 24, 2007Assignee: Wilex AGInventors: Katja Wosikowski-Buters, Stefan Sperl, Joachim Sommer
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Patent number: 7153869Abstract: This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.Type: GrantFiled: March 12, 2004Date of Patent: December 26, 2006Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
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Patent number: 7138538Abstract: Process for the separation of enantiomers comprising at least one free functional group, in which process a reagent based on an enantiopure amino acid is reacted in basic medium with a mixture comprising enantiomers.Type: GrantFiled: May 7, 2004Date of Patent: November 21, 2006Assignee: Solvay (Societe Anonyme)Inventors: Thierry Delplanche, Roland Callens
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Patent number: 7105698Abstract: The process for separating the R(?)- and S(+)-5-[2-[[2-(2-ethoxyphenoxy)ethyl]amino]propyl]-2-methoxybenzene-sulfonamide enantiomers comprises (a) reacting a mixture of said enantiomers with an optically active organic acid to form diastereoisomeric salts with said enantiomers, where in said diastereoisomeric salts have different solubility and can be separated by crystallization; (b) separating the diastereoisomeric salt mixture enriched in the salt of one of the enantiomers; and (c) releasing said salts to obtain the R(?)or S(+) enantiomer. The R(?)-5-[2-[[2-(2-ethoxyphenoxy) ethyl]amino]propyl]-2-methoxybenzenesulfonamide enantiomer has ?-adrenergic blocking activity and is useful as an antihypertensive agent suitable for the treatment of congestive heart failure and benign prostatic hypertrophy.Type: GrantFiled: March 12, 2004Date of Patent: September 12, 2006Assignee: Ragactives, S.L.Inventors: Cristina Blanco Fernandez, Antonio Lorente Bonde-Larsen, Jorge Martin Juarez, Luis Octavio Silva Guisasola
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Patent number: 7056903Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 are each independently in each occurrence aryl or heteroaryl; R4 is —COOH or tetrazolyl; A, B, m, n, and r are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and processes for their preparation.Type: GrantFiled: May 9, 2003Date of Patent: June 6, 2006Assignee: Syntex (U.S.A.) LLCInventors: Richard Leo Cournoyer, Paul Francis Keitz, Lee Edwin Lowrie, Jr., Alexander Victor Muehldorf, Counde O'Yang, Dennis Mitsugu Yasuda
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Patent number: 6946523Abstract: In accordance with the present invention, there are provided novel heterobifunctional monomers and users for the same. Invention compounds have many of the properties required by the microelectronics industry, such as, for example, hydrophobicity, high Tg values, low dielectric constant, ionic purity, low coefficient of thermal expansion (CTE), and the like. These properties result in a thermoset that is particularly well suited to high performance applications where typical operating temperatures are often significantly higher than those at which prior art materials were suitable. Invention compounds are particularly ideal for use in the manufacture of electronic components, such as, for example, printed circuit boards, and the like.Type: GrantFiled: July 1, 2003Date of Patent: September 20, 2005Assignee: Henkel CorporationInventors: Stephen M. Dershem, Kevin J. Forrestal, Puwei Liu
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Patent number: 6936636Abstract: Compounds of the formula: where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of reducing serum thyroxine levels and transiently increasing triglyceride levels.Type: GrantFiled: June 26, 2003Date of Patent: August 30, 2005Assignee: Allergan, Inc.Inventors: Santosh Sinha, Kwok Yin Tsang, Smita Bhat, Roshantha A. Chandraratna
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Patent number: 6884907Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-? activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.Type: GrantFiled: May 10, 2002Date of Patent: April 26, 2005Assignee: Guilford Pharmaceuticals Inc.Inventors: Takashi Tsukamoto, Pavel Majer, Bunda Hin, Weizheng Xu, Qun Liu, Doris Stoermer
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Patent number: 6875884Abstract: Urea and thiourea derivatives inhibit cell function of the chemokine receptor CCR-3. These compounds offer an effective means for treating a range of diseases thought to be mediated by the CCR-3 receptor. A variety of useful urea and thiourea derivatives can be synthesized using liquid and solid phase synthesis protocols.Type: GrantFiled: July 28, 2000Date of Patent: April 5, 2005Assignee: Kirin Beer Kabushiki KaishaInventors: Janak Padia, Michael Hocker, Tsuyoshi Nishitoba, Hirohi Ohashi, Eiji Sawa