Pentacyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/342)
  • Publication number: 20110059977
    Abstract: The present invention relates to the use, for the preparation of a medicament intended for the treatment or the prevention of pathologies linked to, or caused by mycobacteria, of at least one of the compounds of the following formula (I): in which B represents in particular a nitrogen atom, and R1, R2, R3, R4, R5, R6, R7 and R8 represent in particular a hydrogen atom.
    Type: Application
    Filed: March 22, 2007
    Publication date: March 10, 2011
    Applicant: INSTITUT DE RECHERCHE POUR LE DEVELOPPEMENT (I.R.D.)
    Inventors: Alain Robert Francois Maxime Fournet, Delphine Lagoutte, Erwan Poupon, Flor Soriano-Agaton
  • Publication number: 20110020931
    Abstract: A proliferation promoting agent for neural stem cells, which comprises a compound produced by Penicillium sp. CND1007 (FERM BP-10917) or a pharmaceutically acceptable salt thereof, as an active ingredient; a novel compound produced by Penicillium sp. CND 1007 or a pharmaceutically acceptable salt thereof; a method for producing neural stem cells, which comprises culturing a neural stem cells to proliferate the neural stem cells in a presence of the compound produced by Penicillium sp. CND 1007 or a pharmaceutically acceptable salt thereof, and harvesting the neural stem cells from the culture; and the like are provided.
    Type: Application
    Filed: January 29, 2009
    Publication date: January 27, 2011
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Hideyuki Onodera, Michio Ichimura, Kouji Baba, Tsutomu Agatsuma, Setsuya Sasho, Makoto Suzuki, Susumu Iwamoto, Shingo Kakita
  • Publication number: 20110006287
    Abstract: A copolymer comprising at least one donor monomer and at least one acceptor monomer is described. The polymer may optionally further comprise, consist or consist essentially of at least one additional comonomer. Various donor monomers, acceptor monomers and additional comonomers are also described. The polymer is useful in the manufacture of microelectronic devices such as optoelectronic devices.
    Type: Application
    Filed: March 18, 2010
    Publication date: January 13, 2011
    Inventors: Wei You, Shengqiang Xiao
  • Publication number: 20100331325
    Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Application
    Filed: August 5, 2010
    Publication date: December 30, 2010
    Inventors: José Maria CID-NÚÑEZ, Antonius Adrianus Hendrikus Petrus MEGENS, Andrés Avelino TRABANCO-SUÁREZ, Mohamed KOUKNI, Georges Joseph Cornelius HOORNAERT, Frans Josef Cornelius COMPERNOLLE, Tomasz KOZLECKI, Hua MAO, Sushil Chandra JHA, Francisco Javier FERNÁNDEZ-GADEA
  • Patent number: 7820838
    Abstract: An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxycarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.
    Type: Grant
    Filed: July 24, 2008
    Date of Patent: October 26, 2010
    Assignee: Japan Science and Technology Agency
    Inventors: Tohru Fukuyama, Toshiyuki Kan
  • Patent number: 7807833
    Abstract: An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxicarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: October 5, 2010
    Assignee: Japan Science and Technology Agency
    Inventors: Tohru Fukuyama, Toshiyuki Kan
  • Patent number: 7799785
    Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: September 21, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: José Maria Cid-Núñez, Antonius Andrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez, Mohamed Koukni, Georges Joseph Cornelius Hoornaert, Frans Josef Cornelius Compernolle, Tomasz Kozlecki, Hua Mao, Sushil Chandra Jha, Francisco Javier Fernández-Gadea
  • Publication number: 20100202984
    Abstract: Disclosed are naphthalinamidinimide of formula (I), wherein R1, R2, R3, R4, R5 and R6 independently from each other are hydrogen; or C1-C37alkyl; wherein—one to 10 of the CH2 units of C1-C37alkyl independently from each may be substituted by carbonyl groups; oxygen atoms; sulphur atoms; selenium atoms; tellurium atoms; cis- or trans-CH?CH— groups; acetylenic C?C— groups; 1,2-, 1,3- or 1,4-substituted phenyl radicals; 2,3-, 2,4-, 2,5-, 2,6-, 3,4- or 3,5-disubstituted pyridine radicals; 2,3-, 2,4-, 2,5- or 3,4-disubstituted thiophene radicals; 1,2-, 1,3-, 1,4-, 1,5-, 1,6-, 1,7-, 1,8-, 2,3-, 2,6- or 2,7-disubstituted 1,2-, 1,3-, 1,4-, 1,5-, 1,6-, 1,7-, 1,8-, 1,9-, 1,10-, 2,3-, 2,6-, 2,7-, 2,9-, 2,10- or 9,10-disubstituted anthracene radicals; wherein one or 2 CH— groups of the CH?CH— groups, the naphthalene radicals and the anthracene radicals may be substituted by nitrogen atoms; —up to 12 single hydrogen atoms of the CH2— groups independently from each other may be substituted at the same carbon atoms by fluor
    Type: Application
    Filed: July 21, 2006
    Publication date: August 12, 2010
    Inventors: Heinz Langhals, Harald Jaschke, Thomas Ehlis, Olof Wallquist
  • Patent number: 7741325
    Abstract: A compound selected from those of formula (I): wherein: B1, B2 represent carbon or nitrogen, X, Y, X1 and Y1 represent a group selected from hydrogen, halogen, hydroxy, alkoxy, nitro, cyano, trihaloalkyl and NRaRb wherein Ra and Rb are as defined in the description, R1 represents hydrogen or alkyl, R2 represents a group selected from hydrogen, alkyl, —OR?a, —NR?aR?b, —O-Ta-OR?a, —NR?a-Ta-NR?aR?b, NR?a—C(O)-TaH, —O—C(O)-TaH, —O-Ta-NRa?Rb?, —NR?a-Ta-OR?a, —NR?a-Ta-CO2R?a and —NR?a—C(O)-Ta-NR?aR?b wherein R?a, R?b, R?a and Ta are as defined in the description, R3, R4 represent hydrogen or alkyl, A represents a group of formula —CH(R5)—CH(R6)—, —CH?C(R7)—, —C(R7)?CH—, —C(O)—CH(R8)— or —CH(R8)—C(O)— wherein R5, R6, R7 and R8 are as defined in the description, its isomers, N-oxides, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful in the treatment of cancer.
    Type: Grant
    Filed: January 31, 2005
    Date of Patent: June 22, 2010
    Inventors: Michel Koch, François Tillequin, Sylvie Michel, John Hickman, Alain Pierre, Stéphane Leonce, Bruno Pfeiffer, Pierre Renard
  • Patent number: 7736707
    Abstract: The present invention provides a birefringent film that hardly generates cracks even when the film is exposed under a high-temperature and high-humidity environment for a long period of time. The birefringent film of the present invention is a film containing, as a major component, a lyotropic liquid crystalline polycyclic compound containing an acenaphtho[1,2-b]quinoxaline derivative unit in a molecular structure and having a molecular weight of 500 or higher. The birefringent film of the present invention preferably has a refractive index ellipsoid showing a relationship of nx?nz>ny, and more preferably has an in-plane birefringence of 0.01 or higher at the wavelength of 590 nm.
    Type: Grant
    Filed: March 17, 2008
    Date of Patent: June 15, 2010
    Assignee: Nitto Denko Corporation
    Inventors: Shoichi Matsuda, Junzo Miyazaki
  • Publication number: 20100098630
    Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a phenazine or quinoxaline substituent. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides.
    Type: Application
    Filed: December 28, 2007
    Publication date: April 22, 2010
    Applicant: AMBRX, INC.
    Inventor: Zhenwei Miao
  • Publication number: 20100075911
    Abstract: Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes.
    Type: Application
    Filed: March 13, 2009
    Publication date: March 25, 2010
    Applicant: TETRALOGIC PHARMACEUTICALS CORPORATION
    Inventors: Stephen M. CONDON, Matthew G. LaPORTE, Yijun DENG, Susan R. RIPPIN
  • Publication number: 20100047483
    Abstract: The present invention provides a birefringent film having an index ellipsoid satisfying a relationship of nz>nx>ny, and having thinness and light weight, which can be relatively easily produced. The birefringent film of the present invention contains an acenaphtho[1,2-b]quinoxaline derivative represented by the following general formula (I), and an index ellipsoid of the film satisfies a relationship of nz>nx>ny. Here, in the formula (I), X, Y, and Z each independently represent a halogen atom, an alkoxy group, an —R group, an —OM group, a —COOM group, an —OCOR group, an —NHCOR group, a —CONHR group, an —NH2 group, an —NO2 group, a —CF3 group, a —CN group, an —OCN group, an —SCN group, an —SM group, and a —PO3M group; M represents a counterion; R represents hydrocarbon; k, l, m, and n represent the number of substitutions, k is an integer of 1 to 4, and l, m and n are each independently an integer of 0 to 3.
    Type: Application
    Filed: March 3, 2008
    Publication date: February 25, 2010
    Applicant: NITTO DENKO CORPORATION
    Inventor: Shoichi Matsuda
  • Patent number: 7662487
    Abstract: The invention aims at providing a novel azaaromatic compound having an azafluoranthene skeleton which is useful as the constituent of organic EL devices and at realizing a long lifetime, high-efficiency and practical organic EL device by using the compound in at least one of the organic compound layers.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: February 16, 2010
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventor: Toshihiro Iwakuma
  • Publication number: 20090325971
    Abstract: The present invention relates to Pentacyclic Alkaloid Compounds, compositions comprising an effective amount of a Pentacyclic Alkaloid Compound and methods for treating or preventing cancer, a bacterial infection, a fungal infection, or a yeast infection, comprising administering to a subject in need thereof an effective amount of a Pentacyclic Alkaloid Compound. The present invention also relates to compounds and methods that are useful for making Cribrostatin IV.
    Type: Application
    Filed: February 28, 2006
    Publication date: December 31, 2009
    Applicant: The Trustees Of Columbia University In The City Of New York
    Inventors: Samuel J. Danishefsky, Collin Chan
  • Publication number: 20090318421
    Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
    Type: Application
    Filed: April 28, 2006
    Publication date: December 24, 2009
    Inventors: Brian Alvin Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
  • Publication number: 20090315022
    Abstract: An azaindenofluorenedione derivative shown by the following formula (I), (IIa) or (IIb):
    Type: Application
    Filed: November 28, 2008
    Publication date: December 24, 2009
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Hironobu MORISHITA, Yuichiro KAWAMURA
  • Publication number: 20090269846
    Abstract: The teachings relate to methods of identifying inhibitors of dimerization of tyrosine receptor kinases such as EGFR. The methods comprise providing, on a digital computer, a molecular model comprising a complex of extracellular dimerization domains of an RTK, docking a chemical databases to the molecular model, scoring the compounds comprised by the database, and identifying one or more high-scoring compounds. The methods further comprise testing a compound for RTK inhibitory activity in vitro, and testing a compound for specificity as an RTK inhibitor. Also disclosed are compounds selected by the described methods, and methods of treatment using the compounds. Two compounds (NSC11241 and NSC56452) are disclosed that inhibit EGF receptor kinase activation in a dose-dependent manner.
    Type: Application
    Filed: April 6, 2009
    Publication date: October 29, 2009
    Applicant: Washington University
    Inventors: Garland R. Marshall, Linda J. Pike, Robert Yang
  • Publication number: 20090243476
    Abstract: An acenaphthoquinoxaline derivative represented by a general formula (G1) is provided. The acenaphthoquinoxaline derivative represented by the general formula (G1) easily receives electrons and has an electron-transporting property. Therefore, the acenaphthoquinoxaline derivative can be suitably used for a light-emitting element.
    Type: Application
    Filed: March 20, 2009
    Publication date: October 1, 2009
    Inventors: Ryoji Nomura, Takako Takasu, Satoko Shitagaki, Tsunenori Suzuki, Satoshi Seo
  • Publication number: 20090197065
    Abstract: A birefringent film of the present invention comprises at least one kind of polycyclic compound including a —COOM group (the M denotes a counter ion), wherein an index ellipsoid satisfies a relation of nz>nx=ny. The polycyclic compound includes, for example, acenaphtho[1,2-b]quinoxaline derivative represented by the following general formula (I). The birefringent film of the present invention can be formed thin-type and have a high birefringent index in the thickness direction, since the birefringent film comprises the polycyclic compound.
    Type: Application
    Filed: May 17, 2007
    Publication date: August 6, 2009
    Applicant: NITTO DENKO CORPORATION
    Inventors: Junzo Miyazaki, Shoichi Matsuda, Tatsuki Nagatsuka
  • Publication number: 20090191394
    Abstract: The present invention is related to the synthesis of acenaphthoquinoxaline sulfonamide derivatives and the manufacture of optical crystal films based on these compounds. Said acenaphthoquinoxaline sulfonamide heterocyclic derivatives have the general structural formula: where n is 1, 2 or 3; X is an acid group; m is 1, 2 or 3; Y is a counterion selected from the list consisting of H+, NH4+, Na+, K+, and Li+; p is the number of counterions providing neutral state of the molecule; R is a substituent selected from the list consisting of —CH3, —C2H5, —NO2, —Cl, —Br, —F, —CF3, —CN, —OH —OCH3, —OC2H5, —OCOCH3, —OCN, —SCN, —NH2, —NHCOCH3, —CONH2; and z is 1, 2, 3 or 4.
    Type: Application
    Filed: October 9, 2006
    Publication date: July 30, 2009
    Inventors: Pavel I. Lazarev, Elena N. Sidorenko
  • Publication number: 20090167167
    Abstract: Disclosed is a novel compound useful as a constituent of an organic EL device. Also disclosed is a practical organic EL device using this compound. This organic EL device has low driving voltage, long life, and reduced leakage current. Specifically disclosed is a compound characterized by having at least one structure (1) shown below in a molecule.
    Type: Application
    Filed: December 5, 2008
    Publication date: July 2, 2009
    Applicants: Idemitsu Kosan Co., Ltd., Sony Corporation
    Inventors: Yoshiaki Aoyama, Hironobu Morishita, Chishio Hosokawa, Shigeyuki Matsunami, Yasunori Kijima
  • Patent number: 7524956
    Abstract: Methods are provided for preparing a compound with a fused ring structure of formula (XIV) which comprises one or more reactions starting from a 21-cyano compound of formula (XVI) where typically; R1 is an amidomethylene group or an acyloxymethylene group; R5 and R8 are independently chosen from —H, —OH or —OCOCH2OH, or R5 and R8 are both keto and the ring A is a p-benzoquinone ring; R14a and R14b are both —H ozone is —H and the other is —OH, —OCH3 or —OCH2CH3, or R14a and R14b together form a keto group; and R15 and R18 are independently chosen from —H or —OH, or R5 and R8 are both keto and the ring A is a p-benzoquinone ring. In modified starting materials, the 21-cyano group can be replaced by other groups introduced using nucleophilic reagents.
    Type: Grant
    Filed: July 9, 2007
    Date of Patent: April 28, 2009
    Assignee: Pharma Mar, S.A.
    Inventors: Carmen Cuevas, Marta Perez, Andres Francesch, Carolina Fernandez, Jose Luis Chicharro, Pilar Gallego, Maria Zarzuelo, Fernando de Calle, Ignacio Manzanares
  • Publication number: 20090105447
    Abstract: The present invention relates to polymers comprising a repeating unit of the formula (I), and their use in electronic devices. The polymers according to the invention have excellent 5 solubility in organic solvents and excellent film-forming properties. In addition, high charge carrier mobilities and high temperature stability of the emission color are observed, if the polymers according to the invention are used in polymer light emitting diodes (PLEDs).
    Type: Application
    Filed: March 8, 2006
    Publication date: April 23, 2009
    Inventors: Thomas Schafer, Beat Schmidhalter, Peter Murer, Kristina Bardon, Tobias Hintermann
  • Patent number: 7517476
    Abstract: A polymer represented by Formula or structure (I) wherein at least one of each R, R1, R2, R3, R4, R5, and R6 is independently hydrogen, alkyl, aryl, arylalkyl, alkoxy, halogen, cyano, or nitro; x, y, a and b represent the number of groups and rings, respectively; and n represents the number of repeating groups or moieties.
    Type: Grant
    Filed: April 6, 2006
    Date of Patent: April 14, 2009
    Assignee: Xerox Corporation
    Inventors: Yiliang Wu, Ping Liu, Beng S. Ong
  • Patent number: 7517477
    Abstract: An electronic device, such as a thin film transistor, containing a polymer of the formula or structure wherein at least one of each R, R1, R2, R3, R4, R5 and R6 is independently hydrogen, alkyl, aryl, alkoxy, halogen, arylalkyl, cyano, or nitro; x and y represent the number of R substituents; a and b represent the number of rings; and n represents the number of repeating groups or moieties.
    Type: Grant
    Filed: April 6, 2006
    Date of Patent: April 14, 2009
    Assignee: Xerox Corporation
    Inventors: Yiliang Wu, Ping Liu, Beng S. Ong
  • Patent number: 7517883
    Abstract: The invention provides compounds of formula I: wherein A, B, W, Y, Z, and R1 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.
    Type: Grant
    Filed: August 24, 2005
    Date of Patent: April 14, 2009
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Alexander L. Ruchelman, Leroy F. Liu
  • Publication number: 20090023721
    Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Application
    Filed: May 24, 2006
    Publication date: January 22, 2009
    Inventors: Antonius Adrianus Hendrikus Petrus Megens, Andres Avelino Trabanco-Suarez, Jose Maria Cid-Nunez, Hua Mao, Sushil Chandra Jha, Francisco Javier Fernandez-Gadea, Mohamed Koukni, Georges Joseph Cornelius Hoornaert, Frans Josef Cornelius Compernolle, Tomasz Kozlecki
  • Patent number: 7468366
    Abstract: The invention provides compounds of the invention pharmaceutical compositions comprising a compound of the invention, processes for preparing compounds of the invention, intermediates useful for preparing compounds of the invention, and therapeutic methods for treating cancer and other topoisomerase mediated conditions.
    Type: Grant
    Filed: December 12, 2007
    Date of Patent: December 23, 2008
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Alexander L. Ruchelman, Sudhir K. Singh, Abhijit Ray, Leroy F. Liu
  • Publication number: 20080305082
    Abstract: Disclosed are compounds having Formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, A, and B are as defined herein, for use in methods for treating, preventing or ameliorating hyperproliferative disorders, such as cancer and other diseases and conditions. The invention also relates to pharmaceutical compositions and formulations comprising a compound having Formula I, and in combination with one or more other active agents and/or treatments.
    Type: Application
    Filed: September 14, 2005
    Publication date: December 11, 2008
    Inventors: John G. Curd, Robert L. Capizzi, John F.W. Keana
  • Publication number: 20080287450
    Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Application
    Filed: December 6, 2005
    Publication date: November 20, 2008
    Inventors: Jose Maria Cid-Nunez, Antonius Adrianus Hendrikus Petrus Megens, Andres Avelino Trabanco-Suarez, Mohamed Koukni, Georges Joseph Cornelius Hoornaert, Frans Josef Cornelius Compernolle, Tomasz Kozlecki, Hua Mao, Sushil Chandra Jha, Francisco Javier Fernandez-Gadea
  • Publication number: 20080224095
    Abstract: The present invention provides a birefringent film that hardly generates cracks even when the film is exposed under a high-temperature and high-humidity environment for a long period of time. The birefringent film of the present invention is a film containing, as a major component, a lyotropic liquid crystalline polycyclic compound containing an acenaphtho[1,2-b]quinoxaline derivative unit in a molecular structure and having a molecular weight of 500 or higher. The birefringent film of the present invention preferably has a refractive index ellipsoid showing a relationship of nx?nz>ny, and more preferably has an in-plane birefringence of 0.01 or higher at the wavelength of 590 nm.
    Type: Application
    Filed: March 17, 2008
    Publication date: September 18, 2008
    Applicant: NITTO DENKO CORPORATION
    Inventors: Shoichi MATSUDA, Junzo MIYAZAKI
  • Publication number: 20080206597
    Abstract: The invention aims at providing a novel azaaromatic compound having an azafluoranthene skeleton which is useful as the constituent of organic EL devices and at realizing a long lifetime, high-efficiency and practical organic EL device by using the compound in at least one of the organic compound layers.
    Type: Application
    Filed: October 31, 2007
    Publication date: August 28, 2008
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventor: Toshihiro IWAKUMA
  • Patent number: 7417145
    Abstract: An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxicarbonyl (Troc) to which various substituents can be introduced by mild condition, further having a 10-membered ring structure which can be converted to a ring of other numbered members.
    Type: Grant
    Filed: September 20, 2002
    Date of Patent: August 26, 2008
    Assignee: Japan Science and Technology Agency
    Inventors: Tohru Fukuyama, Toshiyuki Kan
  • Publication number: 20080121873
    Abstract: An objective is to provide an organic thin film transistor material exhibiting an excellent property as a transistor together with reduced aging degradation, and also to provide an organic thin film transistor, a field-effect transistor, a switching element, an organic semiconductor material and an organic semiconductor film employing the organic thin film transistor material. Disclosed is an organic thin film transistor material possessing a compound represented by the following Formula (1). where A composed of a condensed ring formed with a 6 membered aromatic cycle or a 6 membered aromatic heterocycle represents C—R, N or P; at least one of As is N or P; R represents a hydrogen atom, a halogen atom or a substituent; and R may be bonded with other Rs with each other to form a ring.
    Type: Application
    Filed: November 17, 2005
    Publication date: May 29, 2008
    Applicant: KONICA MINOLTA HOLDINGS, INC.
    Inventors: Rie Katakura, Hiroshi Kita, Katsura Hirai, Tatsuo Tanaka
  • Patent number: 7345172
    Abstract: In accordance with the present invention there is provided a new class of sterically demanding metallo-intercalators. These compounds intercalate between bases in a duplex polynucleotide, but only where the bases are not fully complementary, for example, where there is a base-pair mismatch. The compounds are sufficiently sterically demanding that intercalation between bases in fully complementary duplexes does not occur to a significant degree. These mismatch intercalators are useful for detecting DNA and RNA defects, for diagnosing disorders characterized by the presence or increase in DNA and/or RNA defects, and for treating such disorders. Further, the compounds are capable of catalyzing photolytic cleavage of nucleic acids at relatively long wavelengths, and under normal sunlight.
    Type: Grant
    Filed: October 26, 2004
    Date of Patent: March 18, 2008
    Assignee: Calfornia Institute of Technology
    Inventors: Jacqueline K. Barton, Henrik Junicke
  • Patent number: 7338553
    Abstract: A process for printing an image on a substrate comprising applying to the substrate an ink comprising a compound of Formula (1) or a salt thereof: wherein: R1 and R2 are each independently H or a substituent; each X and Y independently is a substituent; and a and b are each independently 0, 1, 2, 3 or 4. The compounds used in the process have particularly good ozone fastness and are suitable for preparing inks which can be ink jet printed.
    Type: Grant
    Filed: September 21, 2006
    Date of Patent: March 4, 2008
    Assignee: Fujifilm Imaging Colorants Limited
    Inventor: Clive Edwin Foster
  • Patent number: 7319105
    Abstract: The invention provides compounds of the invention pharmaceutical compositions comprising a compound of the invention, processes for preparing compounds of the invention, intermediates useful for preparing compounds of the invention, and therapeutic methods for treating cancer and other topoisomerase mediated conditions.
    Type: Grant
    Filed: May 14, 2004
    Date of Patent: January 15, 2008
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Alexander L. Ruchelman, Sudhir K. Singh, Abhijit Ray, Leroy F. Liu
  • Patent number: 7241892
    Abstract: Methods are provided for preparing a compound with a fused ring structure of formula (XIV) which comprises one or more reactions starting from a 21-cyano compound of formula (XVI) where typically: R1 is an amidomethylene group or an acyloxymethylene group; R5 and R8 are independently chosen from —H, —OH or —OCOCH2OH, or R5 and R8 are both keto and the ring A is a p-benzoquinone ring; R14a and R14b are both —H ozone is —H and the other is —OH, —OCH3 or —OCH2CH3, or R14a and R14b together form a keto group; and R15 and R18 are independently chosen from —H or —OH, or R5 and R8 are both keto and the ring A is a p-benzoquinone ring. In modified starting materials, the 21-cyano group can be replaced by other groups introduced using nucleophilic reagents.
    Type: Grant
    Filed: May 15, 2000
    Date of Patent: July 10, 2007
    Assignee: Pharma Mar, S.A.
    Inventors: Carmen Cuevas, Marta Perez, Andres Francesch, Carolina Fernandez, Jose Luis Chicharro, Pilar Gallego, Maria Zarzuelo, Fernando de la Calle, Ignacio Manzanares
  • Patent number: 7144608
    Abstract: A color-correcting polarizer is provided comprising a polarizer layer and at least one discotic film layer. The discotic film layer is optically transparent within the range of visible wavelength. The discotic film layer works as a polarizer in the wavelength ranges at least from 380 to 500 nm and/or from 600 to 780 nm. A liquid crystal cell comprising the color correcting polarizer is also disclosed.
    Type: Grant
    Filed: June 18, 2003
    Date of Patent: December 5, 2006
    Assignee: Nitto Denko Corporation
    Inventors: Michael V. Paukshto, Louis D. Silverstein
  • Patent number: 7122549
    Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I), and methods for the synthesis thereof. In another aspect, the present invention provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. In yet another aspect, the present invention provides methods for treating cancer comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof.
    Type: Grant
    Filed: April 16, 2004
    Date of Patent: October 17, 2006
    Assignee: President and Fellows of Harvard College
    Inventors: Andrew G. Myers, Alleyn T. Plowright
  • Patent number: 7098209
    Abstract: Compounds of the general structural formula (I), and use of the compounds and salts and solvates thereof, as thereapeutic agents.
    Type: Grant
    Filed: April 15, 2002
    Date of Patent: August 29, 2006
    Assignee: Lilly Icos LLC
    Inventors: Mark W. Orme, Jason S. Sawyer, Lisa M. Schultze
  • Patent number: 7049315
    Abstract: The invention provides compounds of formula I: wherein A, B, W, Y, Z, and R1 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.
    Type: Grant
    Filed: May 14, 2004
    Date of Patent: May 23, 2006
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Alexander L. Ruchelman, Leroy F. Liu
  • Patent number: 7045177
    Abstract: The present invention provides a series of new chemical compounds, lyotropic liquid crystal systems, materials, blends, mixtures, namely acenaphtho[1,2-b]quinoxaline sulfoderivatives of the general structural formula: wherein n is an integer in the range of 1 to 4; m is an integer in the range of 0 to 4; z is an integer in the range of 0 to 6, and m+z+n?10; X and Y are individually selected from the group consisting of CH3, C2H5, OCH3, OC2H5, Cl, Br, OH, OCOCH3NH2, NHCOCH3, NO2, F, CF3, CN, OCN, SCN, COOH, and CONH2; M is a counterion; and j is the number of counterions in the molecule.
    Type: Grant
    Filed: November 17, 2004
    Date of Patent: May 16, 2006
    Assignee: Nitto Denko Corporation
    Inventors: Tatyana Y. Dutova, Alexey Y. Nokel, Elena N. Sidorenko, Sergey V. Timofeev
  • Patent number: 6987109
    Abstract: The invention provides compounds of formula I: wherein A, B, W, Y, Z, and R1 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.
    Type: Grant
    Filed: May 14, 2004
    Date of Patent: January 17, 2006
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Alexander L. Ruchelman
  • Patent number: 6982333
    Abstract: The present invention provides a short, convergent total synthesis of camptothecin and related compounds which consists of a novel 4+1 radical annulation. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.
    Type: Grant
    Filed: September 16, 2003
    Date of Patent: January 3, 2006
    Assignee: University of Pittsburgh
    Inventors: Dennis P. Curran, Hubert Josien, Sung Bo Ko
  • Patent number: 6964964
    Abstract: The invention provides compounds of formula I: wherein A, B, W, Y, Z, R1, R3 and R4 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.
    Type: Grant
    Filed: May 14, 2004
    Date of Patent: November 15, 2005
    Assignee: Rutgers The State University of New Jersey
    Inventors: Edmond J. LaVoie, Alexander L. Ruchelman
  • Patent number: 6936714
    Abstract: Compounds of the saframycin-ecteinascidin series with cytotoxic properties having the following general formula, their uses and synthesis, are disclosed: wherein R1 and R4 is H, a C1 to C4 alkyl group, or an acyl group; wherein R2 is an ether, ester, amide, or a phthalimide group; wherein R3 is ?O, OH, an ether group, an acyl group such as OC(O)Me, OC(O)Bn and OC(O)Et, or a sulfide group; wherein R5 is H, halogen, OH, an ether group, an acyl group, or an amide group; wherein R6 is ?O, OH, OCH3, CN, or an acyloxy group; wherein R7, is ?O, OH, halogen, an ether group, or an acyl group; wherein R8 and R9 are independently H, CH3, OCH3, OC2H5, CF3, halogen such as Br and F, or R8 and R9 are joined together as a methylenedioxy group, or other five or six membered ring; wherein R10 and R11 are independently CH3, OCH3, OC2H5, SCH3, or SC2H5; wherein R12 is H, a C1 to C4 alkyl group, or an acyl group; and wherein the chiral center marked * has the R or the S configuration.
    Type: Grant
    Filed: December 5, 2003
    Date of Patent: August 30, 2005
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Samuel J. Danishefsky, Bishan Zhou
  • Patent number: 6878711
    Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Grant
    Filed: October 9, 2001
    Date of Patent: April 12, 2005
    Assignee: Lilly Icos LLC
    Inventors: Mark W. Orme, Jason Scott Sawyer, Lisa M. Schultze
  • Patent number: RE41614
    Abstract: The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from the group consisting of H, OH, OR?, SH, SR?, SOR?, SO2R?, NO2, NH2, NHR?, N(R?)2, NHC(?O)R? NHC(?O)R?, CN, halogen, ?O, C(?O)H, C(?O)R?, CO2H, CO2R?, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and substituted or unsubstituted heteroaromatic; wherein each of the R? groups is independently selected from the group consisting of H, OH, NH2, NO2, SH, CN, halogen, ?O, C(?O)H, C(?O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl, and heteroaromatic; wherein each dotted circle represents one, two or three optional double bonds; wherein R7 and R8 may be are joined into a carbocyclic or heterocyclic ring system; and wherein X1 and X2 are each independently defined as above for R1-R8 R1-R6 and R9, and each further includes s
    Type: Grant
    Filed: December 17, 2003
    Date of Patent: August 31, 2010
    Assignee: President and Fellows of Harvard College
    Inventor: Elias J. Corey