Additional Polycyclo Heterocyclic Ring System Containing Patents (Class 548/159)
  • Publication number: 20100292208
    Abstract: Compounds with two fused bicyclic heteroaryl moieties and their pharmaceutical compositions, and methods of using them as leukotriene A4 hydrolase (LTA4H) modulators and for the treatment of diseases, disorders and conditions mediated by LTA4H.
    Type: Application
    Filed: May 12, 2010
    Publication date: November 18, 2010
    Inventors: Genesis Bacani, Christa C. Chrovian, Wendy Eccles, Anne M. Fourie, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Alejandro Santillán, JR., Virginia M. Tanis, John J. M. Wiener
  • Publication number: 20100285470
    Abstract: Monomethine dyes that have no or minimal fluorescence in buffer or in the presence of single stranded DNA or RNA, but strongly fluoresce in the presence of double-stranded DNA. In one embodiment, the dye is useful in quantitative RT-PCR.
    Type: Application
    Filed: September 30, 2008
    Publication date: November 11, 2010
    Applicant: Thermo Fisher Scientific (Milwaukee) LLC
    Inventors: Charles K. Brush, Jianqin Liu, Peter Czerney, Matthias Wenzel
  • Patent number: 7825155
    Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.
    Type: Grant
    Filed: September 13, 2006
    Date of Patent: November 2, 2010
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
  • Publication number: 20100273840
    Abstract: A cantharimide compound may include the backbone of formula (1). R1, R2, R3, and R4 may be independently selected from the group consisting of H, C(O)OR5, C(O)R6, C(O)NR7R8, NR9C(O)R10, N—R11R12, O—R13, S—R14, P(O)(OR15)(OR16), As(O)(OR17)(OR18), SO2R19, SO3R20, and B(OR21). X1 to X4 may be independently selected from the group consisting of nitrogen and carbon, such that X1 to X4 are not all hydrogen. Y1, Y2 and R5 to R21 may be independently selected from the group consisting of hydrogen, C1-12-alkyl, -aryl, heteroaryl, and a bioactive polymer.
    Type: Application
    Filed: April 23, 2009
    Publication date: October 28, 2010
    Inventors: Johnny Cheuk-on Tang, Albert Sun-chi Chan, Kim-hung Lam, Chung-hin Chui, Stanton Hon Lung Kok, Marcus Chun Wah Yuen, Sau Hing Chan, Chor Hing Cheng, Filly Cheung
  • Publication number: 20100267671
    Abstract: The present invention includes and relates generally to compounds which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.
    Type: Application
    Filed: February 9, 2010
    Publication date: October 21, 2010
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Publication number: 20100267712
    Abstract: Disclosed is a compound of Formula (I) in which W and R1-R6 are defined herein. Also disclosed is a method of treating spinal muscular atrophy, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced directly or indirectly by mutation or frameshift.
    Type: Application
    Filed: September 26, 2008
    Publication date: October 21, 2010
    Applicants: Human Services, Science Applications International Coporation Saic, Albany Molecular Research, Inc.,
    Inventors: Jill E. Heemskerk, John M. McCall, Keith D. Barnes
  • Publication number: 20100255504
    Abstract: Chemically-reactive, water-soluble, heterocycle-substituted 7-hydroxycoumarin dyes, their bioconjugates and uses are described. The conjugates derived from reactive heterocycle-substituted 7-hydroxycoumarin dyes are used for analyzing biological compounds. These heterocycle-substituted 7-hydroxycoumarin dyes are particularly useful as fluorescent labels for biopolymer detection reagents, such as antibodies or nucleic acid probes. The dye-antibody conjugates of the invention are particularly useful for analyzing analytes using a flow cytometer equipped with a violet laser as an excitation source due to their strong absorption at 405 nm and high fluorescence quantum yield.
    Type: Application
    Filed: March 17, 2010
    Publication date: October 7, 2010
    Applicant: BECTON, DICKINSON AND COMPANY
    Inventors: Zhenjun Diwu, Timothy Dubrovsky, Barnaby Abrams, Jinfang Liao, Qinglin Meng
  • Patent number: 7795297
    Abstract: Indole compounds corresponding to the formula (I): as defined in the claims, pharmaceutically acceptable addition salts of such compounds, pharmaceutical compositions containing such compounds, the process for their preparation, and their use as pharmacologically active substances, especially in the treatment of hypertriglyceridemia, hyperlipidemia, hypercholesterolemia, diabetes, endothelial dysfunction, cardiovascular disease, inflammatory disease and neurodegeneration.
    Type: Grant
    Filed: February 28, 2008
    Date of Patent: September 14, 2010
    Assignee: Laboratories Fournier S.A.
    Inventors: Jean Binet, Benaiessa Boubia, Pierre Dodey, Christiane Legendre, Martine Barth, Olivia Poupardin-Olivier
  • Publication number: 20100222358
    Abstract: Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.
    Type: Application
    Filed: March 2, 2010
    Publication date: September 2, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Marlon D. Cowart, Chen Zhao, Minghua Sun, Lawrence A. Black, Guo Zhu Zheng, Robert J. Gregg, Geoff G.Z. Zhang, Ahmad Y. Sheikh, Xiaochun Lou, Rodger F. Henry, David M. Barnes, Lawrence Kolaczkowski, Anthony R. Haight, Sou-Jen Chang, Steven J. Wittenberger, Michael G. Fickes
  • Publication number: 20100216787
    Abstract: A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula.
    Type: Application
    Filed: December 22, 2009
    Publication date: August 26, 2010
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Masakazu Sato, Yuko Matsunaga, Hajime Asanuma, Hideaki Amada, Takeshi Koami, Tetsuo Takayama, Tetsuya Yabuuchi, Fumiyasu Shiozawa, Hironori Katakai, Hiroki Umemiya, Akiko Ikeda
  • Publication number: 20100216833
    Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXR? and/or LXR? agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.
    Type: Application
    Filed: May 6, 2010
    Publication date: August 26, 2010
    Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
  • Publication number: 20100210685
    Abstract: The present invention relates to substituted indoles of formula (I), useful as pharmaceutical compounds for treating respiratory disorders.
    Type: Application
    Filed: April 28, 2010
    Publication date: August 19, 2010
    Inventors: Timothy Birkinshaw, Roger Bonnert, Tony Cook, Rukhsana Rasul, Hitesh Sanganee, Simon Teague
  • Publication number: 20100197716
    Abstract: The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.
    Type: Application
    Filed: April 16, 2010
    Publication date: August 5, 2010
    Inventors: Jennifer Qiao, Tammy C. Wang, James C. Sutton, Timur Gungor
  • Publication number: 20100197871
    Abstract: Ligands useful for promoting copper-catalyzed azide-alkyne cycloaddition reactions comprise a compound represented by structural Formula (I) as described in the specification, wherein in Formula (I) Z1 is a nitrogen-containing heterocyclic group or a group represented by the formula: Y1—(CH2)c—Y2—(CH2)d—Y3—CH2—N(CH2Z4)(CH2Z5), where Y1 is -E1-C(O)O—, -E1-C(O)NH—, -E1-, or a covalent bond; Y2 is a covalent bond, —CH?CH—, or a 1,4-(1,2,3-triazolyl) group; Y3 is —OC(O)-E2-, —NHC(O)-E2-, -E2-, or a covalent bond; each of E1 and E2 is a benzimidazolyl group attached at the 1 and 2 positions; each of c and d is independently 1, 2, 3, 4, or 5; each of Z2, Z3, Z4 and Z5 is a nitrogen-containing heterocyclic group including a substituent X1 and optionally including a substituent (CH2)n—R1, and Y1, Y2, Y3, X1, R1, c, d and n are each as defined in the specification.
    Type: Application
    Filed: September 15, 2008
    Publication date: August 5, 2010
    Inventors: M.G. Finn, Valentin O. Rodionov
  • Publication number: 20100197644
    Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments
    Type: Application
    Filed: December 21, 2009
    Publication date: August 5, 2010
    Inventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrecher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
  • Publication number: 20100190782
    Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.
    Type: Application
    Filed: December 17, 2009
    Publication date: July 29, 2010
    Inventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Danette A. Dudley, Wayne J. Fairbrother, John A. Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Carl Steven Rye, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Andrew M. Petros, Andrew J. Souers
  • Patent number: 7745443
    Abstract: The present invention relates to compounds of the formula I, in which R1, R2, A, B, D, E, n, m or o have the meanings indicated below. The compounds of the formula I are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb). They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of atherothrombotic diseases.
    Type: Grant
    Filed: April 2, 2007
    Date of Patent: June 29, 2010
    Assignees: Sanofi-Aventis Deutschland GmbH, Ajinomoto Co., Inc.
    Inventors: Otmar Klingler, Melitta Just, Kuniya Sakurai, Naoyuki Fukuchi
  • Patent number: 7745632
    Abstract: A cyanine compound represented by the general formula (I), (VI) or (VII): wherein ring-A1 is an optionally substituted benzene or naphthalene ring; B is a group represented by the general formula (II) or (III); R1 is a hydrogen atom, a halogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, or an aryl group having 6 to 30 carbon atoms; R2 is a substituent represented by the general formula (IV); and Y1 is a hydrogen atom, an organic group having 1 to 30 carbon atoms, or a substituent represented by the general formula (IV): wherein ring-A2 is the same as the ring-A1 in the general formula (I); Y4 and Y5 each are independently the same as Y1 in the general formula (I); X2 is the same as X1 in the general formula (I); R10 is the same as R1 in the general formula (I); R11 is the same as R2 in the general formula (I); R23 and R24 are the same as R21 and R22 in the formulas (II) and (III); n is an integer of 0 to 6; the polymethine chain may have a subst
    Type: Grant
    Filed: April 4, 2006
    Date of Patent: June 29, 2010
    Assignee: Adeka Corporation
    Inventors: Yohei Aoyama, Koichi Shigeno
  • Publication number: 20100152195
    Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituent
    Type: Application
    Filed: December 16, 2009
    Publication date: June 17, 2010
    Inventors: Luca Arista, Giorgio Bonanomi, Anna Maria Capelli, Federica Damiani, Romano Di Fabio, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco, Silvia Terreni
  • Publication number: 20100137301
    Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.
    Type: Application
    Filed: February 8, 2010
    Publication date: June 3, 2010
    Inventors: Michael Lee Jones, David Gunn, John Howard Jones, Michael C. Van Zandt
  • Publication number: 20100136491
    Abstract: Compounds of formula (I), (II), and (III), wherein R1, R2, R?2 and R??2 for example are C1-C20alkyl, provided that at least one of R1, R2, R?2 and R??2 carries a specified substituent; R3, R4, and R5 for example independently of one another are hydrogen or a defined substituent provided that at least one of R3, R4 or R5 is other than hydrogen or C1-C20alkyl; R6, R7, R8, R?7, RV, R?8, R?6, R?7, R??6 and R??7 for example independently of one another have one of the meanings as given for R3, R4, and R5; and R9 for example is C1-C20alkyl; exhibit an unexpectedly good performance in photopolymerization reactions.
    Type: Application
    Filed: April 24, 2008
    Publication date: June 3, 2010
    Inventors: Akira Matsumoto, Junichi Tanabe, Hisatoshi Kura, Masaki Ohwa
  • Publication number: 20100136467
    Abstract: Compounds of the formula (I) and (II) M1, M2 and M3 independently of one another are no bond, a direct bond, CO, O, S, SO, SO2or NR14; provided that at least one of M1, M2 or M3 is a direct bond, CO, O, S, SO, SO2 or NR14; M4 is a direct bond, CR?3R?4, CS, O, S, SO, or SO2; Y is S or NR18; R1 for example is hydrogen, C3-C8cycloalkyl, phenyl or napthyl, both of which are optionally substituted; R2 for example is C1-C20alkyl; R?2 has one of the meanings given for R2; R3 and R4 are for example hydrogen, halogen, C1-C20alkyl; R?3, R?4, R?3 and R?4 indepedently of one another have one of the meanings given for R3 and R4; and R5 is for example hydrogen, halogen, C1-C20alkyl; provided that in the compounds of the formula (I) at least two oxime ester groups are present and provided that at least one specified substituent R2 or R?2 is present; exhibit an unexpectedly good performance in photopolymerization reactions.
    Type: Application
    Filed: April 28, 2008
    Publication date: June 3, 2010
    Inventors: Akira Matsumoto, Junichi Tanabe, Hisatoshi Kura, Masaki Ohwa
  • Publication number: 20100121059
    Abstract: Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects, including autoimmune diseases. The compounds inhibit potassium channels, including the Kv1.3 channel and at least some of the therapeutic effects of such compounds may be due at least in part to potassium channel inhibition. In some embodiments, the compounds are more selective for certain potassium channels (e.g., Kv1.3 channels) than other potassium channels (e.g., Kv1.5 channels).
    Type: Application
    Filed: July 6, 2009
    Publication date: May 13, 2010
    Applicant: The Regents of the University of California
    Inventors: Heike Wulff, Ananthakrishnan Sankaranarayanan, Wolfram Haensel, Alexander Schmitz, Kristina Schmidt-Lassen
  • Publication number: 20100113789
    Abstract: The present invention is to provide a medicinal composition for preventing or treating parasitic protozoan infections, having a high selective toxicity against parasitic protozoan infection, and a superior preventive or treating effect.
    Type: Application
    Filed: September 30, 2005
    Publication date: May 6, 2010
    Applicants: FUJIFILM CORPORATION
    Inventors: Masataka Ihara, Kiyosei Takasu, Khanitha Pudhom, Hiroshi Kitaguchi, Masayuki Kawakami, Kozo Sato
  • Publication number: 20100093651
    Abstract: This disclosure provides improved derivatives of artemisinin; pharamaceutical compositions containing these compounds; methods for preparing these compounds and compositions; methods of using these compounds and compositions for preventing, controlling or treating infectious diseases including but not limited to parasitic infectious diseases such as T. gondii infection, trypanosome parasite infection, plasmodia parasite infection, and cryptosporidium parasite infection; methods for preventing, controlling or treating toxoplasma infection; and methods for treating psychiatric disorders associated with toxoplasma infection including but not limited to schizophrenia using the disclosed compounds and compositions alone or in combination with one or more antipsychotic drugs.
    Type: Application
    Filed: October 19, 2007
    Publication date: April 15, 2010
    Inventors: Lorraine V. Brando, Gary H. Posner, John G. D'Angelo, Robert H. Yolken, Christopher P. Hencken, Lauren Woodard
  • Patent number: 7674809
    Abstract: Heterocyclic amidines with anti-inflammatory and analgesic activity that inhibit nitrogen oxide production, of formula (I): in which: G1 and G2 are hydrogen, halogen, hydroxyl, C1-C4 alkoxy, C1-C4 alkyl, and an amidino substituent of formula Q, provided that, for each compound of formula (I), only one of the two substituents G1 or G2 is an amidino substituent of formula Q: and in which the substituents W, Y and X are combined to form 9- or 10-membered bicyclic heteroaromatic derivatives containing up to 2 hetero atoms in the same ring; and Z is an aryl or heteroaryl group, a linear or branched C1-C6 alkyl or alkenyl chain, a C1-C4 alkyl-aryl group or a C1-C4 alkyl-heteroaryl group.
    Type: Grant
    Filed: March 1, 2005
    Date of Patent: March 9, 2010
    Assignee: Rottapharm S.p.A.
    Inventors: Francesco Makovec, Antonio Giordani, Roberto Artusi, Stefano Mandelli, Ilario Verpilio, Simona Zanzola, Lucio Claudio Rovati
  • Patent number: 7659404
    Abstract: The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(?O)—, —O—C(?O)—, —NR8—C(?O)—, —O—C1-6alkanediyl-C(?O)—, —NR8—C1-6alkanediyl-C(?O)—, —S(?O)2—, —O—S(?O)2—, —NR8—S(?O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(?O), carboxyl, aminoC(?O), mono- or di(C1-4alkyl)aminoC(?O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, —C(?O)—, —C(?S)—, —S(?O)2—, C1-6alkanediyl-C(?O)—, C1-6alkanediyl-C(?S)— or C1-6alkanediyl-S(?O)2—; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted aminoC1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6
    Type: Grant
    Filed: February 14, 2002
    Date of Patent: February 9, 2010
    Assignee: Tibotec Pharmaceuticals Ltd.
    Inventors: Dominique Louis Nestor Ghislain Surleraux, Piet Tom Bert Paul Wigerinck, Daniel Getman, Wim Gaston Verschueren, Sandrine Vendeville, Marie-Pierre De Bethune, Jan Octaaf Antoon De Kerpel, Samuel Leo Christiaan Moors, Herman Augustinus De Kock, Marieke Christiane Johanna Voets
  • Patent number: 7659269
    Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: February 9, 2010
    Assignee: The Institute for Pharmaceutical Discovery, LLC
    Inventors: Michael Jones, David Gunn, John Jones, Michael Van Zandt
  • Patent number: 7625758
    Abstract: Protein dyes whose molecular structure is that of a coumarin moiety coupled to a quaternary ammonium heterocycle through a vinyl or polyvinyl linkage demonstrate the ability to associate with proteins in a non-covalent, non-specific manner at low pH, where the associated form displays a significantly higher fluorescence emission than the unassociated form. This makes the dyes useful as selective labels for proteins at the low pH and eliminates the need for the removal of extraneous components from the medium in which the proteins reside prior to detection.
    Type: Grant
    Filed: January 26, 2005
    Date of Patent: December 1, 2009
    Inventor: Thomas R. Berkelman
  • Publication number: 20090281321
    Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.
    Type: Application
    Filed: July 17, 2009
    Publication date: November 12, 2009
    Inventors: George Wu, Anantha R. Sudhakar, Tao Wang, Ji Xie, Frank Xing Chen, Marc Poirier, Mingsheng Huang, Vijay Sabesan, Daw-long Kwok, Jian Cui, Xiaojing Yang, Tiruvettipuram K. Thiruvengadam, Jing Liao, Ilia A. Zavialov, Hoa N. Nguyen, Ngiap Kie Lim
  • Publication number: 20090263843
    Abstract: The invention provides compounds and methods for site-specifically labeling proteins with cyanobenzothiazole derivatives of formula I. For example, the invention provides methods for labeling the N-terminus of a protein that terminates with a cysteine residue. The invention also provides methods for isolating an N-terminally labeled protein and methods for detecting an N-terminally labeled protein.
    Type: Application
    Filed: March 26, 2009
    Publication date: October 22, 2009
    Applicant: Promega Corporation
    Inventors: Jessica Anderson, Poncho Meisenheimer, John Shultz
  • Publication number: 20090253656
    Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.
    Type: Application
    Filed: March 29, 2006
    Publication date: October 8, 2009
    Applicant: Kabushiki Kaisha Yakult Honsha
    Inventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
  • Patent number: 7598390
    Abstract: Chemical compounds having a high selectivity for double stranded DNA over RNA and single stranded DNA are disclosed. The chemical compounds are stains that become fluorescent upon illumination and interaction with double stranded DNA, but exhibit reduced or no fluorescence in the absence of double stranded DNA. The compounds can be used in a variety of biological applications to qualitatively or quantitatively assay DNA, even in the presence of RNA.
    Type: Grant
    Filed: May 11, 2006
    Date of Patent: October 6, 2009
    Assignee: Life Technologies Corporation
    Inventors: Jolene A. Bradford, Ching-Ying Cheung, Shih-Jung Huang, Patrick R. Pinson, Stephen T. Yue
  • Patent number: 7592361
    Abstract: This invention is directed to indole acetic acid derivatives and their use in pharmaceutical compositions for the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic disease. The invention is also directed to intermediates useful in preparation of indole acetic derivatives and to methods of preparation.
    Type: Grant
    Filed: April 28, 2004
    Date of Patent: September 22, 2009
    Assignee: Bayer Pharmaceuticals Corporation
    Inventors: Xin Ma, Louis-David Cantin, Soongyu Choi, Roger Clark, Martin Hentemann, Joachim Rudolph, Rico Lavoie, Zhonghua Zhang
  • Publication number: 20090221564
    Abstract: Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R1, R2, R3, R4, Y, m, n and q are as identified herein. R1 is in particular amidino. The invention further provides particular benzothiophene compounds. Compounds of the invention may be useful as inhibitors of Factor IXa and in the therapy of cardiovascular conditions and diseases, e.g. thrombosis.
    Type: Application
    Filed: February 20, 2007
    Publication date: September 3, 2009
    Applicant: TRIGEN LIMITED
    Inventors: Shouming Wang, Toby Jonathan Blench, Frederic Marlin, Richard Beck, Roger Peter Dickinson
  • Publication number: 20090218039
    Abstract: An dye compound of the following formula (1): wherein D represents a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group; L represents ?CR2—, ?N—, or ?N—NH—; R1 represents a monovalent substituent; R2 represents a hydrogen atom or a cyano group; n indicates an integer of from 0 to 4; when n is 2 or more, then plural R1's may be the same or different.
    Type: Application
    Filed: February 27, 2009
    Publication date: September 3, 2009
    Applicant: FUJIFILM Corporation
    Inventors: Yoshihiko FUJIE, Tetsuya WATANABE, Hisashi MIKOSHIBA
  • Patent number: 7582672
    Abstract: The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.
    Type: Grant
    Filed: October 22, 2004
    Date of Patent: September 1, 2009
    Assignee: Oxagen Limited
    Inventors: David Middlemiss, Mark Richard Ashton, Edward Andrew Boyd, Frederick Arthur Brookfield, Eric R. Pettipher, Michael George Hunter, Mark Whittaker, Chris Palmer
  • Publication number: 20090209583
    Abstract: The present invention relates to 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broad-spectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.
    Type: Application
    Filed: June 22, 2007
    Publication date: August 20, 2009
    Inventors: Herman De Kock, Tim Hugo Maria Jonckers, Paul Jozef Gabriel Maria Boonants, Stefaan Julien Last, Inge Dierynck, Judith Eva Baumeister, Gerben Albert Van ' T Klooster
  • Patent number: 7563902
    Abstract: The present invention relates to novel chemiluminescent compounds, to a method for synthesizing these compounds, to derivatives and conjugates comprising these compounds, to the use of these compounds or conjugates thereof in chemiluminescence based assays, especially in immunoassays.
    Type: Grant
    Filed: January 25, 2006
    Date of Patent: July 21, 2009
    Assignee: Roche Diagnostics Operations, Inc.
    Inventors: Dieter Heindl, Rupert Herrmann, Wolfgang Jenni
  • Publication number: 20090176840
    Abstract: This invention is directed to indolone derivatives which are antagonists or the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: June 17, 2008
    Publication date: July 9, 2009
    Inventors: Michael Konkel, John M. Werzel, Jamie Talisman
  • Patent number: 7557138
    Abstract: Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects, including autoimmune diseases. The compounds inhibit potassium channels, including the Kv1.3 channel and at least some of the therapeutic effects of such compounds may be due at least in part to potassium channel inhibition. In some embodiments, the compounds are more selective for certain potassium channels (e.g., Kv1.3 channels) than other potassium channels (e.g., Kv1.5 channels).
    Type: Grant
    Filed: October 4, 2004
    Date of Patent: July 7, 2009
    Assignee: The Regents of the University of California
    Inventors: Heike Wulff, Ananthakrishnan Sankaranarayanan, Wolfram Haensel, Alexander Schmitz, Kristina Schmidt-Lassen
  • Patent number: 7553848
    Abstract: bis-Bicyclic amides and derivatives thereof and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration,
    Type: Grant
    Filed: January 21, 2005
    Date of Patent: June 30, 2009
    Assignee: Amgen Inc.
    Inventors: Christopher Hulme, Mqhele Vellah Ncube, Mark H. Norman, Vassil I. Ognyanov, Liping H. Pettus, Jiawang Zhu
  • Publication number: 20090156586
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.
    Type: Application
    Filed: February 3, 2009
    Publication date: June 18, 2009
    Inventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Bandarpalle B. Shankar, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Razia Rizvi, Lei Chen, De-Yi Yang, Robert Feltz, Seong Heon Kim
  • Patent number: 7514460
    Abstract: The present invention relates to N2-heteroaryl-benzazole-2,(5 or 6)-diamine derivatives and compositions thereof as protein kinase inhibitors for the treatment of e.g. cancer.
    Type: Grant
    Filed: December 15, 2005
    Date of Patent: April 7, 2009
    Assignee: 4SC AG
    Inventors: Thomas Herz, Rolf Krauss, Michael Kubbutat, Martin Lang, Christoph Schaechtele, Stefan Tasler, Frank Totzke
  • Patent number: 7507831
    Abstract: Various processes are disclosed for preparing protected epicatechin oligomers having (4?,8)-interflavan linkages. In one process, a tetra-O-protected epicatechin monomer or oligomer is coupled with a protected, C-4 activated epicatechin monomer in the presence of an acidic clay such as a mortmorillonite clay. In another process, a 5,7,3?,4?-benzyl protected or a 3 -acetyl-, 5,7,3?,4?-benzyl protected epicatechin or catechin monomer or oligomer is reacted with 3 -O-acetyl-4-[(2-benzothiazolyl)thio]-5,7,3?,4?-tetra-O-benzylepicatechin in the presence of silver tetrafluoroborate. In another process, two 5,7,3?,4?-benzyl protected epicatechin monomers activated with 2-(benzothiazolyl)thio groups at the C-4 positions are cross-coupled in the presence of silver tetrofluoroborate. A process is also disclosed for reacting an unprotected epicatechin or catechin monomer with 4-(benzylthio) epicatechin or catechin.
    Type: Grant
    Filed: January 11, 2006
    Date of Patent: March 24, 2009
    Inventors: Alan P. Kozikowski, Werner Tückmantel, Leo J. Romanczyk, Jr.
  • Publication number: 20090066245
    Abstract: The present invention is a light-emitting device material characterized by containing a pyrene compound represented by the following general formula (1): wherein R1 to R10 are specific functional groups, provided that at least one of the R1 to R10 is a substituent represented by the following general formula (2): wherein R11 to R14 are specific functional groups, provided that any one of the R11 to R14 is used for a single bond with a pyrene skeleton; X1 is a group represented by the following general formula (3): wherein R15 is a specific functional group; and Y1 to Y4 is selected from among a nitrogen atom and a carbon atom, provided that at least one of the Y1 to Y4 is a nitrogen atom and at least one thereof is a carbon atom, and no substituents exist on the nitrogen atom in the case of the nitrogen atom. This material provides a light-emitting device having high luminous efficiency and excellent durability.
    Type: Application
    Filed: February 23, 2006
    Publication date: March 12, 2009
    Applicant: TORAY INDUSTRIES, INC.
    Inventors: Kazunori Sugimoto, Seiichiro Murase, Daisuke Kitazawa, Kazumasa Nagao, Takafumi Ogawa, Tsuyoshi Tominaga
  • Publication number: 20090054652
    Abstract: A cyanine compound is represented by formula (I): A1: benzene or naphthalene ring. A3: 5- or 6-membered ring. R1, R2: hydrogen atom and the like. R7: an alkyl group and the like. R12: a substituent by formula (II) or (II?). R20: a hydrogen atom and the like. Anq-: a q-valent anion. q: 1 or 2; p: a coefficient for neutral charge. In formula (II): bond between L and T is a double, conjugated double, or triple bond. L: carbon atom. T: carbon, oxygen, sulfur, or nitrogen atom. x, y, z: 0 or 1. s: 0-4. R13: hydrogen atom and the like. R14, R15, and R16: hydrogen atom and the like. In formula (II?), the bond between L? and T? is a double or conjugated double bond. L?: carbon atom. T?: carbon, oxygen, nitrogen atom. s?: 0-4. Ring containing L? and T?: 5-membered ring, may contain a heteroatom.
    Type: Application
    Filed: March 23, 2007
    Publication date: February 26, 2009
    Applicant: ADEKA CORPORATION
    Inventors: Toru Yano, Satoshi Yanagisawa, Yohei Aoyama, Koichi Shigeno
  • Publication number: 20090035810
    Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.
    Type: Application
    Filed: May 29, 2008
    Publication date: February 5, 2009
    Applicant: INVITROGEN CORPORATION
    Inventors: Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue
  • Publication number: 20090035809
    Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.
    Type: Application
    Filed: May 29, 2008
    Publication date: February 5, 2009
    Applicant: INVITROGEN CORPORATION
    Inventors: Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue
  • Patent number: 7482344
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly congestive heart disease, hypertension, rheumatoid arthritis or inflammation, comprising administering to a patient in thereof an effective amount of a compound of Formula (I).
    Type: Grant
    Filed: December 15, 2004
    Date of Patent: January 27, 2009
    Assignee: Eli Lilly and Company
    Inventors: Michael Joseph Coghlan, Prabhakar Kondaji Jadhav, James Joseph Droste, Jonathan Edward Green, Donald Paul Matthews