Benzene Ring Bonded Directly Or Attached Indirectly By An Acyclic Carbon Or An Acyclic Carbon Chain To Ring Carbon Of The Five-membered Hetero Ring Patents (Class 548/511)
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Patent number: 10473666Abstract: The present invention relates to dye compounds represented by Formulae I and II, which are described in the specification. The dye compounds of the present invention have markedly improved quantum yields and emit strong fluorescence compared to existing cyanine dyes. Due to these advantages, the dye compounds of the present invention can find applications in various fields, for example, as probes for various biological systems where optical imaging is required. Particularly, the dye compounds of the present invention can be used as mitotrackers capable of labeling and tracking mitochondria. Therefore, the dye compounds of the present invention can be used to quantitatively image mitochondria in live tissues and cells. Furthermore, the dye compounds of the present invention can be applied as pH probes for measuring the pH of live cells.Type: GrantFiled: July 18, 2016Date of Patent: November 12, 2019Assignee: SFC CO., LTD.Inventors: Ju-man Song, Seon-Gi Min, Seung-Soo Lee, Do-min Lee, Kyung-Hwa Park, Moon-Chan Hwang, Bong-Ki Shin, Jong-Tae Je
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Patent number: 9017828Abstract: Disclosed are a compound represented by Formula below, including an indole derivative in which two tertiary amines are substituted, an organic electronic element using the same, and a terminal thereof.Type: GrantFiled: March 9, 2011Date of Patent: April 28, 2015Assignee: Duk San Neolux Co., Ltd.Inventors: Dongha Kim, Jungcheol Park, Jinuk Ju, Jangyeol Baek, Wonsam Kim, Eunkyung Kim, Daehyuk Choi, Junghwan Park
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Patent number: 9012488Abstract: The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.Type: GrantFiled: February 21, 2014Date of Patent: April 21, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: John Y. L. Chung, Yanfeng Zhang, Laura Artino, Aaron S. Cote, Donal Desmond, Jeremy Scott, Yekaterina Vaynshteyn
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Publication number: 20150099720Abstract: Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions.Type: ApplicationFiled: October 20, 2014Publication date: April 9, 2015Inventors: Lin Zhi, Robert I. Higuchi, E. Adam Kallel, Cornelis Arjan Van Oeveren, Jyun-Hung Chen, Daniel A. Ruppar, Bijan Pedram, Thomas Lot Stevens Lau, Todd A. Miller
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Publication number: 20150065487Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: November 11, 2014Publication date: March 5, 2015Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fred Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Publication number: 20150057248Abstract: Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors.Type: ApplicationFiled: September 1, 2014Publication date: February 26, 2015Applicant: The Board of Regents of The University of Texas SystemInventors: Jia Zhou, Haijun Chen, Kenneth M. Johnson, Cheng Z. Wang
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Publication number: 20150031738Abstract: The present invention provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.Type: ApplicationFiled: December 10, 2012Publication date: January 29, 2015Applicant: University of MassachusettsInventors: Yan Li, Hitest Thaker, Gregory N. Tew, Dahui Liu, Wenxi Pan
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Publication number: 20150023916Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.Type: ApplicationFiled: February 14, 2013Publication date: January 22, 2015Applicant: SIGA TECHNOLOGIES INC.Inventors: Dongcheng Dai, James R. Burgeson, Sean M. Amberg, Dennis E. Hruby
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Publication number: 20150004698Abstract: Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.Type: ApplicationFiled: August 29, 2014Publication date: January 1, 2015Applicants: YALE UNIVERSITY, UNIVERSITY OF SOUTH FLORIDAInventors: Said M. Sebti, Jin Q. Cheng, Andrew D. Hamilton, Katherine Kayser-Bricker
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Publication number: 20140374722Abstract: A compound represented by Formula 1. An organic electric element includes a first electrode, a second electrode, and an organic material layer including the compound of Formula 1. The organic material layer include a light emitting layer, a hole transport layer including a compound represented by Formula 2, and an emission-auxiliary layer including the compound represented by Formula 1. When the organic electric element includes the compound in the organic material layer, luminous efficiency, color purity, and life span can be improved.Type: ApplicationFiled: January 14, 2013Publication date: December 25, 2014Inventors: Dongha Kim, Sunhee Lee, Yeonhee Choi, Soungyun Mun, Jungcheol Park, Yongwook Park, Heesun Ji, Junghwan Park, Bumsung Lee, Sunpil Hwang
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Publication number: 20140361259Abstract: An arylamine-based compound is represented by Formula 1 below. The arylamine-based compound is included in an organic light emitting diode.Type: ApplicationFiled: October 23, 2013Publication date: December 11, 2014Applicant: SAMSUNG DISPLAY CO., LTD.Inventors: Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jun-Ha Park, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jong-Hyuk Lee
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Patent number: 8889678Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.Type: GrantFiled: July 19, 2010Date of Patent: November 18, 2014Assignees: Centre National de la Recherche Scientifique, Universite de StrasbourgInventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
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Patent number: 8883437Abstract: The invention relates to the use of a compound having formula (I) as an enzymatic substrate for the detection of a nitroreductase activity, wherein: W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination of same; n=0, 1 or 2; X is NR, CZ5Z6, S or O, R being H, alkyl, aralkyl, aryl, alkanoic or alkylsulphonic, Z5 and Z6 being an alkyl; Y is N or N+R, R being alkyl, aralkyl, aryl, alkanoic or alkylsulphonic; Z1, Z2, Z3 and Z4 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulphonyl, including the sulphonyl or carboxyl amides or esters thereof, and the salts of same.Type: GrantFiled: July 29, 2010Date of Patent: November 11, 2014Assignee: bioMérieux S.A.Inventors: Olivier Fabrega, Arthur James, Sylvain Orenga, John Perry, Vindhya Salwatura, Stephen Stanforth
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Patent number: 8871948Abstract: An (aza)indole derivative substituted in position 5, of formula (I) in which X, Y, Z, G1, G2, G3, R1, W, and R2 have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor.Type: GrantFiled: February 15, 2013Date of Patent: October 28, 2014Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Maria Alessandra Alisi, Guido Furlotti, Nicola Cazzolla, Caterina Maugeri, Patrizia Dragone, Barbara Garofalo, Isabella Coletta, Giorgina Mangano, Beatrice Garrone
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Publication number: 20140296524Abstract: Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.Type: ApplicationFiled: May 5, 2014Publication date: October 2, 2014Applicant: Nanoquantum Sciences, Inc.Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
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Publication number: 20140295437Abstract: The present invention provides methods and non-fluorescent carbocyanine quencher compounds having the general formula: Wherein the A moiety is a substituted pyridinium, unsubstituted pyridinium, substituted quinolinium, unsubstituted quinolinium, substituted benzazolium, unsubstituted benzazolium, substituted indolinium, or substituted indolinium. The invention further provides luminescent donor molecule-quencher pairs and luminescent donor molecule-quencher-luminescent acceptor molecule conjugates wherein the quencher is a cyanine compound of the present invention. The energy transfer pairs are used to detect an analyte of interest in a sample.Type: ApplicationFiled: December 17, 2013Publication date: October 2, 2014Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Rosaria HAUGLAND, Ching-Ying CHEUNG, Stephen YUE
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Publication number: 20140246094Abstract: Asymmetric dyes of the D-?-A type have the Formula (1), including the valence tautomers thereof. The dyes of Formula (1) are suitable for use in dye-sensitized solar cells (DSSC), in photoelectrochemical devices or in photonic devices. A solar cell and a device for photoelectric conversion contain an asymmetric dye of Formula (1). The dyes of Formula (1) are also suitable for conjugating with optically active nanoparticles (NP).Type: ApplicationFiled: August 24, 2012Publication date: September 4, 2014Applicant: PIANETA S.R.L.Inventor: Giuseppe Caputo
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Patent number: 8815903Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a benzene ring, a pyridine ring, or the like; Y1 represents a C1-6 alkylene group or the like; Y2 represents a single bond or the like; Z represents —C(?O)—NHSO2R6, an acidic 5-membered hetero ring group, or the like; R1 represents a hydrogen atom or the like; R2 represents a phenyl group, a 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.Type: GrantFiled: January 24, 2012Date of Patent: August 26, 2014Assignees: Kissei Pharmaceutical Co., Ltd., Kyorin Pharmaceutical Co., Ltd.Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
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Publication number: 20140220050Abstract: The present invention provides dihydroorotate dehydrogenase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.Type: ApplicationFiled: February 4, 2014Publication date: August 7, 2014Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SAInventors: Meyyappan MUTHUPPALANIAPPAN, Prashant Kashinath Bhavar, Srikant Viswanadha, Swaroop Kumar V.S. Vakkalanka, Gayatri Swaroop Merikapudi
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Publication number: 20140212359Abstract: AIE (aggregation-induced emission)-active TPE derivatives, TPE-TPP, TPE-MitoR and TPE-IQ are contemplated. These specific TPE derivatives are useful as fluorescent agents for mitochondrial imaging and as apoptosis inducers. Possessing high specificity to mitochondria, superior photostability and appreciable tolerance to microenvironment change, TPE derivatives are well-suited imaging agents for mitochondrial targeting and morphological change tracking. Because of their synthetic flexibility, TPE derivatives can be further modified as dual-functional probes for an array of applications such as sensing of ROS, metal ions, or pH change in mitochondria.Type: ApplicationFiled: January 27, 2014Publication date: July 31, 2014Applicant: The Hong Kong University of Science and TechnologyInventors: Benzhong TANG, Yuning HONG, Sijie CHEN, Wai Tung LEUNG, Engui ZHAO, Haiqin DENG
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Publication number: 20140179681Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.Type: ApplicationFiled: January 8, 2014Publication date: June 26, 2014Inventor: Joseph P. Errico
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Publication number: 20140171480Abstract: The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.Type: ApplicationFiled: February 21, 2014Publication date: June 19, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: John Y. L. Chung, Yanfeng Zhang, Laura Artino, Aaron S. Cote, Donal Desmond, Jeremy Scott, Yekaterina Vaynshteyn
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Publication number: 20140155431Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: December 19, 2013Publication date: June 5, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Patent number: 8710243Abstract: The invention provides a compound of formula(I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. Formula(I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined in the specification.Type: GrantFiled: October 6, 2010Date of Patent: April 29, 2014Assignee: Karo Bio ABInventors: Lars Hagberg, Sandra Gordon, Aiping Cheng, Theresa Apelqvist, Patrik Rhönnstad, Mattias Wennerstål
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Patent number: 8697740Abstract: The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.Type: GrantFiled: January 8, 2010Date of Patent: April 15, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: John Y. L. Chung, Yanfeng Zhang, Laura Artino, Jennifer Baxter, Aaron S. Cote, Yekaterina Vaynshteyn, Donal Desmond, Jeremy Scott
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Patent number: 8686021Abstract: Use of a benzoyl derivative of 3-aminocarbazole to produce a drug for the preventive or therapeutic treatment of a disorder selected form the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis. Method for the preventive or therapeutic treatment of a disorder selected from the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis in which a therapeutically effective quantity of a benzoyl derivative of 3-aminocarbazole according to the invention is administered to an individual.Type: GrantFiled: May 3, 2006Date of Patent: April 1, 2014Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Lorenzo Polenzani, Giorgina Mangano, Isabella Coletta, Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Caterina Maugeri
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Patent number: 8680120Abstract: A compound (I) of the present invention, which has an EP1 receptor antagonism: [wherein A represents a benzene ring or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic ring which may have a substituent, a 6-membered aromatic heterocyclic ring which may have a substituent or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.Type: GrantFiled: July 26, 2010Date of Patent: March 25, 2014Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kazuya Tatani, Naohiro Kawamura, Tatsuhiro Kondo, Atsushi Kondo
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Publication number: 20130317065Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a benzene ring, a pyridine ring, or the like; Y1 represents a C1-6 alkylene group or the like; Y2 represents a single bond or the like; Z represents —C(?O)—NHSO2R6, an acidic 5-membered hetero ring group, or the like; R1 represents a hydrogen atom or the like; R2 represents a phenyl group, a 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.Type: ApplicationFiled: January 24, 2012Publication date: November 28, 2013Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
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Patent number: 8580843Abstract: Presented herein are diindolylmethane derivative compounds useful for the prevention and or treatment of neurological conditions, including neurological conditions related to neuroinflammation. One such neurological condition is Parkinson's disease.Type: GrantFiled: October 7, 2009Date of Patent: November 12, 2013Assignees: Colorado State University Research Foundation, The Texas A&M University SystemInventors: Ronald B. Tjalkens, Stephen Safe
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Publication number: 20130259830Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed.Type: ApplicationFiled: June 24, 2011Publication date: October 3, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Timothy Barden, Colleen Hudson, James Jia, Charles Kim, Regina Graul, Ara Mermerian, Joel Moore, Kevin Sprott, Yueh-tyng Chien
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Publication number: 20130231604Abstract: Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.Type: ApplicationFiled: March 3, 2012Publication date: September 5, 2013Applicant: NANOQUANTUM SCIENCES, INC.Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
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Patent number: 8501713Abstract: Combinations comprising (or consisting essentially of) one or more compounds of formula (1) with one or more ancillary agents, to processes for preparing the combinations, and to various therapeutic uses of the combinations. Also provided are pharmaceutical compositions containing the combinations as well as a method of treatment of Duchenne muscular dystrophy, Becker muscular dystrophy or cachexia using the combinations.Type: GrantFiled: August 1, 2008Date of Patent: August 6, 2013Assignee: Summit Corporation PLCInventors: Graham Michael Wynne, Stephen Paul Wren, Peter David Johnson, Paul Damien Price, Olivier De Moor, Gary Nugent, Richard Storer, Richard Joseph Pye, Colin Richard Dorgan
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Publication number: 20130192978Abstract: A photoacid includes a nucleophilic (NuH) moiety having a photodissociable proton, an electron accepting (EA) moiety, and a bridge structure (X) bonded to both the NuH moiety and EA moiety positioned between the NuH and EA moieties. The NuH and EA moieties each include respective structure so that the EA moiety bonds to a proton photodissociated form of the NuH moiety during a reversible photoinduced intramolecular reaction to form a ring, which has been found to significantly increase the lifetime of the proton dissociation state.Type: ApplicationFiled: January 23, 2013Publication date: August 1, 2013Applicant: University of Central Florida Research Foundation, Inc.Inventor: University of Central Florida Research Foundation, Inc.
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Patent number: 8476432Abstract: The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2—N—O—R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.Type: GrantFiled: June 30, 2011Date of Patent: July 2, 2013Assignee: Yuhan CorporationInventors: Hyun Ju, Sang-Sun Joung, Hyun-Jik Yi, Ja-Heouk Khoo, Jong-Chul Lim, Jae-Gyu Kim
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Publication number: 20130158269Abstract: An (aza)indole derivative substituted in position 5, of formula (I) in which X, Y, Z, G1, G2, G3, R1, W, and R2 have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor.Type: ApplicationFiled: February 15, 2013Publication date: June 20, 2013Applicant: AZIENDE CHIMICHE RIUNITE ANGELIN FRANCESCO A.C.R.A.F. S.P.A.Inventor: Aziende Chimiche Riunite Angelin Francesco A.C.R.A.F S.P.A.
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Publication number: 20130001540Abstract: Disclosed are a compound including an indole derivative in which two tertiary amines are substituted, an organic electronic element using the same, and a terminal thereof.Type: ApplicationFiled: March 9, 2011Publication date: January 3, 2013Applicant: DUKSAN HIGH METAL CO., LTD.Inventors: Dongha Kim, Jungcheol Park, Jinuk Ju, Jangyeol Baek, Wonsam Kim, Eunkyung Kim, Daehyuk Choi, Junghwan Park
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Publication number: 20120309769Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), and inhibit kinase-mediated (e.g., cdk5-mediated) phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. Side effects such as significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, can be avoided in the mammal receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: June 6, 2012Publication date: December 6, 2012Applicant: SCRIPPS RESEARCH INSTITUTE, THEInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
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Publication number: 20120305906Abstract: Disclosed are a compound including an indole derivative, an organic electronic element using the same, and a terminal thereof.Type: ApplicationFiled: July 12, 2010Publication date: December 6, 2012Applicant: DUKSAN HIGH METAL CO., LTD.Inventors: Dongha Kim, Jungcheol Park, Jinuk Ju, Jangyeol Baek, Wonsam Kim, Eunkyung Kim, Daehyuk Choi, Junghwan Park
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Publication number: 20120196865Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.Type: ApplicationFiled: July 19, 2010Publication date: August 2, 2012Applicants: UNIVERSITE DE STRASBOURG, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
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Publication number: 20120122137Abstract: The invention relates to the use of a compound having formula (I) as an enzymatic substrate for the detection of a nitroreductase activity, wherein: W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination of same; n=0, 1 or 2; X is NR, CZ5Z6, S or O, R being H, alkyl, aralkyl, aryl, alkanoic or alkylsulphonie, Z5 and Z6 being an alkyl; Y is N or N+R, R being alkyl, aralkyl, aryl, alkanoic or alkylsulphonic; Z1, Z2, Z3 and Z4 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulphonyl, including the sulphonyl or carboxyl amides or esters thereof, and the salts of same.Type: ApplicationFiled: July 29, 2010Publication date: May 17, 2012Applicant: bioMérieux S.A.Inventors: Olivier Fabrega, Arthur James, Sylvain Orenga, John Perry, Vindhya Salwatura, Stephen Stanforth
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Publication number: 20120122931Abstract: A compound represented by the general formula (I) of the present invention, which has an EP1 receptor antagonism: [wherein A represents a benzene ring or the like; Y represents a C1-6 alkylene group or the like; RN represents a hydrogen atom or a C1-6 alkyl group; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic group which may have a substituent, a 6-membered aromatic heterocyclic group which may have a substituent or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.Type: ApplicationFiled: July 26, 2010Publication date: May 17, 2012Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Tatsuhiro Kondo, Atsushi Kondo, Kazuya Tatani, Naohiro Kawamura
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Publication number: 20120037892Abstract: The present invention relates to a novel cycloalkene derivative, and an organic electronic device using the same. The cycloalkene derivative according to the exemplary embodiment of the present invention may act as a hole injection, a hole transport, an electron injection, an electron transport, or a light emitting material in an organic light emitting diode and an organic electronic device, and in particular, may be used alone as a light emitting host or a dopant.Type: ApplicationFiled: January 20, 2010Publication date: February 16, 2012Applicant: LG CHEM, LTD.Inventors: Hye-Young Jang, Jae-Chol Lee, Jae-Soon Bae, Jeung-Gon Kim, Seong-So Kim, Chang-Hwan Kim
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Publication number: 20120010262Abstract: The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.Type: ApplicationFiled: January 8, 2010Publication date: January 12, 2012Inventors: John Y.L. Chung, Yanfeng Zhang, Laura Artino, Jennifer Baxter, Aaron S. Cote, Donal Desmond, Jeremy Scott, Yekaterina Vaynshteyn
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Publication number: 20110275663Abstract: The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them.Type: ApplicationFiled: April 16, 2009Publication date: November 10, 2011Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Angèle Schoenfelder, André Mann, Maurizio Taddei, Antonio Solinas, Fabrizio Manetti
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Patent number: 8013006Abstract: In accordance with the present invention, compounds that inhibit viral replication, preferably Hepatitis C Virus (HCV) replication, have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the treatment or prevention of a viral infection are provided. In another aspect of the invention, compounds useful in the treatment or prevention of HCV infection are provided.Type: GrantFiled: July 14, 2005Date of Patent: September 6, 2011Assignee: PTC Therapeutics, Inc.Inventors: Gary Mitchell Karp, Peter Seongwoo Hwang, James Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey Allen Campbell, Christine Espiritu, Concetta Freund, Zhengxian Gu, Takashi Komatsu
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Patent number: 8003670Abstract: The present invention relates to novel aminoalkoxy arylsulfonamide compounds of the formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. These compounds are useful in the treatment of various disorders that are related to 5-HT6 receptor functions. Specifically, the compounds of this invention are also useful in the treatment of various CNS disorders, hematological disorders, eating disorders, diseases associated with pain, respiratory diseases, genito-urological disorders, cardiovascular diseases and cancer.Type: GrantFiled: April 15, 2008Date of Patent: August 23, 2011Assignee: Suven Life Sciences LimitedInventors: Ramakrishna Nirogi, Rama Sastri Kambhampati, Anil Karbhari Shinde, Anand Vijaykumar Daulatabad, Adi Reddy Dwarampudi, Nagaraj Vishwottam Kandikere, Santosh Vishwakarma, Venkateswarlu Jasti
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Publication number: 20110195932Abstract: Combinations comprising (or consisting essentially of) one or more compounds of formula (1) with one or more ancillary agents, to processes for preparing the combinations, and to various therapeutic uses of the combinations. Also provided are pharmaceutical compositions containing the combinations as well as a method of treatment of Duchenne muscular dystrophy, Becker muscular dystrophy or cachexia using the combinations.Type: ApplicationFiled: August 1, 2008Publication date: August 11, 2011Inventors: Graham Michael Wynne, Stephen Paul Wren, Peter David Johnson, Paul Damien Price, Olivier De Moor, Gary Nugent, Richard Storer, Richard Joseph Pye, Colin Richard Dorgan
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Patent number: 7968589Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: February 9, 2010Date of Patent: June 28, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: John E. Stelmach, Emma R. Parmee, James R. Tata, Keith G. Rosauer, Ronald M. Kim, Amy R. Bittner, Jiang Chang, Christopher Joseph Sinz
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Patent number: 7956083Abstract: The present invention relates to novel indole derivatives having pharmacological activity, processes for their preparation, compositions containing them and the use of these compounds in the treatment of estrogen receptor beta mediated diseases.Type: GrantFiled: February 17, 2009Date of Patent: June 7, 2011Assignee: Glaxo Group LimitedInventors: Christopher Norbert Johnson, David G. Jones, Xi Liang, David Timothy MacPherson, Aaron B Miller, Steven James Stanway, Andrew Kenneth Takle, Giancarlo Trani, Antoinette Wilson
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Publication number: 20110098483Abstract: The invention relates to a nitrogen heterocycle compound of formula 1: Also disclosed are a method of synthesizing the compound and use of the compound for treating various diseases and conditions.Type: ApplicationFiled: March 27, 2009Publication date: April 28, 2011Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Nicos A. Petasis, Malgorzata Myslinska