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)
  • Patent number: 9017828
    Abstract: 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: Grant
    Filed: March 9, 2011
    Date of Patent: April 28, 2015
    Assignee: Duk San Neolux Co., Ltd.
    Inventors: Dongha Kim, Jungcheol Park, Jinuk Ju, Jangyeol Baek, Wonsam Kim, Eunkyung Kim, Daehyuk Choi, Junghwan Park
  • Patent number: 9012488
    Abstract: 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: Grant
    Filed: February 21, 2014
    Date of Patent: April 21, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John Y. L. Chung, Yanfeng Zhang, Laura Artino, Aaron S. Cote, Donal Desmond, Jeremy Scott, Yekaterina Vaynshteyn
  • Publication number: 20150099720
    Abstract: 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: Application
    Filed: October 20, 2014
    Publication date: April 9, 2015
    Inventors: 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
  • Publication number: 20150065487
    Abstract: 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: Application
    Filed: November 11, 2014
    Publication date: March 5, 2015
    Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fred Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
  • Publication number: 20150057248
    Abstract: Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors.
    Type: Application
    Filed: September 1, 2014
    Publication date: February 26, 2015
    Applicant: The Board of Regents of The University of Texas System
    Inventors: Jia Zhou, Haijun Chen, Kenneth M. Johnson, Cheng Z. Wang
  • Publication number: 20150031738
    Abstract: 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: Application
    Filed: December 10, 2012
    Publication date: January 29, 2015
    Applicant: University of Massachusetts
    Inventors: Yan Li, Hitest Thaker, Gregory N. Tew, Dahui Liu, Wenxi Pan
  • Publication number: 20150023916
    Abstract: 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: Application
    Filed: February 14, 2013
    Publication date: January 22, 2015
    Applicant: SIGA TECHNOLOGIES INC.
    Inventors: Dongcheng Dai, James R. Burgeson, Sean M. Amberg, Dennis E. Hruby
  • Publication number: 20150004698
    Abstract: 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: Application
    Filed: August 29, 2014
    Publication date: January 1, 2015
    Applicants: YALE UNIVERSITY, UNIVERSITY OF SOUTH FLORIDA
    Inventors: Said M. Sebti, Jin Q. Cheng, Andrew D. Hamilton, Katherine Kayser-Bricker
  • Publication number: 20140374722
    Abstract: 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: Application
    Filed: January 14, 2013
    Publication date: December 25, 2014
    Inventors: Dongha Kim, Sunhee Lee, Yeonhee Choi, Soungyun Mun, Jungcheol Park, Yongwook Park, Heesun Ji, Junghwan Park, Bumsung Lee, Sunpil Hwang
  • Publication number: 20140361259
    Abstract: An arylamine-based compound is represented by Formula 1 below. The arylamine-based compound is included in an organic light emitting diode.
    Type: Application
    Filed: October 23, 2013
    Publication date: December 11, 2014
    Applicant: 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
  • Patent number: 8889678
    Abstract: 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: Grant
    Filed: July 19, 2010
    Date of Patent: November 18, 2014
    Assignees: Centre National de la Recherche Scientifique, Universite de Strasbourg
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
  • Patent number: 8883437
    Abstract: 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: Grant
    Filed: July 29, 2010
    Date of Patent: November 11, 2014
    Assignee: bioMérieux S.A.
    Inventors: Olivier Fabrega, Arthur James, Sylvain Orenga, John Perry, Vindhya Salwatura, Stephen Stanforth
  • Patent number: 8871948
    Abstract: 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: Grant
    Filed: February 15, 2013
    Date of Patent: October 28, 2014
    Assignee: 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
  • Publication number: 20140296524
    Abstract: 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: Application
    Filed: May 5, 2014
    Publication date: October 2, 2014
    Applicant: Nanoquantum Sciences, Inc.
    Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
  • Publication number: 20140295437
    Abstract: 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: Application
    Filed: December 17, 2013
    Publication date: October 2, 2014
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Rosaria HAUGLAND, Ching-Ying CHEUNG, Stephen YUE
  • Publication number: 20140246094
    Abstract: 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: Application
    Filed: August 24, 2012
    Publication date: September 4, 2014
    Applicant: PIANETA S.R.L.
    Inventor: Giuseppe Caputo
  • Patent number: 8815903
    Abstract: 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: Grant
    Filed: January 24, 2012
    Date of Patent: August 26, 2014
    Assignees: Kissei Pharmaceutical Co., Ltd., Kyorin Pharmaceutical Co., Ltd.
    Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
  • Publication number: 20140220050
    Abstract: 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: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SA
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Prashant Kashinath Bhavar, Srikant Viswanadha, Swaroop Kumar V.S. Vakkalanka, Gayatri Swaroop Merikapudi
  • Publication number: 20140212359
    Abstract: 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: Application
    Filed: January 27, 2014
    Publication date: July 31, 2014
    Applicant: The Hong Kong University of Science and Technology
    Inventors: Benzhong TANG, Yuning HONG, Sijie CHEN, Wai Tung LEUNG, Engui ZHAO, Haiqin DENG
  • Publication number: 20140179681
    Abstract: 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: Application
    Filed: January 8, 2014
    Publication date: June 26, 2014
    Inventor: Joseph P. Errico
  • Publication number: 20140171480
    Abstract: 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: Application
    Filed: February 21, 2014
    Publication date: June 19, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: John Y. L. Chung, Yanfeng Zhang, Laura Artino, Aaron S. Cote, Donal Desmond, Jeremy Scott, Yekaterina Vaynshteyn
  • Publication number: 20140155431
    Abstract: 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: Application
    Filed: December 19, 2013
    Publication date: June 5, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
  • Patent number: 8710243
    Abstract: 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: Grant
    Filed: October 6, 2010
    Date of Patent: April 29, 2014
    Assignee: Karo Bio AB
    Inventors: Lars Hagberg, Sandra Gordon, Aiping Cheng, Theresa Apelqvist, Patrik Rhönnstad, Mattias Wennerstål
  • Patent number: 8697740
    Abstract: 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: Grant
    Filed: January 8, 2010
    Date of Patent: April 15, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John Y. L. Chung, Yanfeng Zhang, Laura Artino, Jennifer Baxter, Aaron S. Cote, Yekaterina Vaynshteyn, Donal Desmond, Jeremy Scott
  • Patent number: 8686021
    Abstract: 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: Grant
    Filed: May 3, 2006
    Date of Patent: April 1, 2014
    Assignee: 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
  • Patent number: 8680120
    Abstract: 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: Grant
    Filed: July 26, 2010
    Date of Patent: March 25, 2014
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuya Tatani, Naohiro Kawamura, Tatsuhiro Kondo, Atsushi Kondo
  • Publication number: 20130317065
    Abstract: 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: Application
    Filed: January 24, 2012
    Publication date: November 28, 2013
    Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
  • Patent number: 8580843
    Abstract: 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: Grant
    Filed: October 7, 2009
    Date of Patent: November 12, 2013
    Assignees: Colorado State University Research Foundation, The Texas A&M University System
    Inventors: Ronald B. Tjalkens, Stephen Safe
  • Publication number: 20130259830
    Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed.
    Type: Application
    Filed: June 24, 2011
    Publication date: October 3, 2013
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Timothy Barden, Colleen Hudson, James Jia, Charles Kim, Regina Graul, Ara Mermerian, Joel Moore, Kevin Sprott, Yueh-tyng Chien
  • Publication number: 20130231604
    Abstract: 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: Application
    Filed: March 3, 2012
    Publication date: September 5, 2013
    Applicant: NANOQUANTUM SCIENCES, INC.
    Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
  • Patent number: 8501713
    Abstract: 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: Grant
    Filed: August 1, 2008
    Date of Patent: August 6, 2013
    Assignee: Summit Corporation PLC
    Inventors: 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
  • Publication number: 20130192978
    Abstract: 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: Application
    Filed: January 23, 2013
    Publication date: August 1, 2013
    Applicant: University of Central Florida Research Foundation, Inc.
    Inventor: University of Central Florida Research Foundation, Inc.
  • Patent number: 8476432
    Abstract: 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: Grant
    Filed: June 30, 2011
    Date of Patent: July 2, 2013
    Assignee: Yuhan Corporation
    Inventors: Hyun Ju, Sang-Sun Joung, Hyun-Jik Yi, Ja-Heouk Khoo, Jong-Chul Lim, Jae-Gyu Kim
  • Publication number: 20130158269
    Abstract: 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: Application
    Filed: February 15, 2013
    Publication date: June 20, 2013
    Applicant: 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.
  • Publication number: 20130001540
    Abstract: 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: Application
    Filed: March 9, 2011
    Publication date: January 3, 2013
    Applicant: DUKSAN HIGH METAL CO., LTD.
    Inventors: Dongha Kim, Jungcheol Park, Jinuk Ju, Jangyeol Baek, Wonsam Kim, Eunkyung Kim, Daehyuk Choi, Junghwan Park
  • Publication number: 20120309769
    Abstract: 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: Application
    Filed: June 6, 2012
    Publication date: December 6, 2012
    Applicant: SCRIPPS RESEARCH INSTITUTE, THE
    Inventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
  • Publication number: 20120305906
    Abstract: Disclosed are a compound including an indole derivative, an organic electronic element using the same, and a terminal thereof.
    Type: Application
    Filed: July 12, 2010
    Publication date: December 6, 2012
    Applicant: DUKSAN HIGH METAL CO., LTD.
    Inventors: Dongha Kim, Jungcheol Park, Jinuk Ju, Jangyeol Baek, Wonsam Kim, Eunkyung Kim, Daehyuk Choi, Junghwan Park
  • Publication number: 20120196865
    Abstract: 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: Application
    Filed: July 19, 2010
    Publication date: August 2, 2012
    Applicants: UNIVERSITE DE STRASBOURG, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
  • Publication number: 20120122137
    Abstract: 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: Application
    Filed: July 29, 2010
    Publication date: May 17, 2012
    Applicant: bioMérieux S.A.
    Inventors: Olivier Fabrega, Arthur James, Sylvain Orenga, John Perry, Vindhya Salwatura, Stephen Stanforth
  • Publication number: 20120122931
    Abstract: 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: Application
    Filed: July 26, 2010
    Publication date: May 17, 2012
    Applicant: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Tatsuhiro Kondo, Atsushi Kondo, Kazuya Tatani, Naohiro Kawamura
  • Publication number: 20120037892
    Abstract: 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: Application
    Filed: January 20, 2010
    Publication date: February 16, 2012
    Applicant: LG CHEM, LTD.
    Inventors: Hye-Young Jang, Jae-Chol Lee, Jae-Soon Bae, Jeung-Gon Kim, Seong-So Kim, Chang-Hwan Kim
  • Publication number: 20120010262
    Abstract: 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: Application
    Filed: January 8, 2010
    Publication date: January 12, 2012
    Inventors: John Y.L. Chung, Yanfeng Zhang, Laura Artino, Jennifer Baxter, Aaron S. Cote, Donal Desmond, Jeremy Scott, Yekaterina Vaynshteyn
  • Publication number: 20110275663
    Abstract: 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: Application
    Filed: April 16, 2009
    Publication date: November 10, 2011
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Angèle Schoenfelder, André Mann, Maurizio Taddei, Antonio Solinas, Fabrizio Manetti
  • Patent number: 8013006
    Abstract: 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: Grant
    Filed: July 14, 2005
    Date of Patent: September 6, 2011
    Assignee: 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
  • Patent number: 8003670
    Abstract: 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: Grant
    Filed: April 15, 2008
    Date of Patent: August 23, 2011
    Assignee: Suven Life Sciences Limited
    Inventors: Ramakrishna Nirogi, Rama Sastri Kambhampati, Anil Karbhari Shinde, Anand Vijaykumar Daulatabad, Adi Reddy Dwarampudi, Nagaraj Vishwottam Kandikere, Santosh Vishwakarma, Venkateswarlu Jasti
  • Publication number: 20110195932
    Abstract: 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: Application
    Filed: August 1, 2008
    Publication date: August 11, 2011
    Inventors: 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
  • Patent number: 7968589
    Abstract: 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: Grant
    Filed: February 9, 2010
    Date of Patent: June 28, 2011
    Assignee: 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
  • Patent number: 7956083
    Abstract: 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: Grant
    Filed: February 17, 2009
    Date of Patent: June 7, 2011
    Assignee: Glaxo Group Limited
    Inventors: Christopher Norbert Johnson, David G. Jones, Xi Liang, David Timothy MacPherson, Aaron B Miller, Steven James Stanway, Andrew Kenneth Takle, Giancarlo Trani, Antoinette Wilson
  • Publication number: 20110098483
    Abstract: 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: Application
    Filed: March 27, 2009
    Publication date: April 28, 2011
    Applicant: UNIVERSITY OF SOUTHERN CALIFORNIA
    Inventors: Nicos A. Petasis, Malgorzata Myslinska
  • Publication number: 20110077406
    Abstract: Embodiments of the invention provide methods and materials for chemical cross-coupling reactions that utilize unconventional phenol derivatives as cross-coupling partners. Embodiments of the invention can be used to synthesize a variety of useful organic compounds, for example the anti-inflammatory drug flurbiprofen.
    Type: Application
    Filed: September 24, 2010
    Publication date: March 31, 2011
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Neil K. Garg, Kyle W. Quasdorf, Xia Tian