Additional Polycyclo Heterocyclic Ring System Containing Patents (Class 548/159)
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Publication number: 20100292208Abstract: 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: ApplicationFiled: May 12, 2010Publication date: November 18, 2010Inventors: 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
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Publication number: 20100285470Abstract: 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: ApplicationFiled: September 30, 2008Publication date: November 11, 2010Applicant: Thermo Fisher Scientific (Milwaukee) LLCInventors: Charles K. Brush, Jianqin Liu, Peter Czerney, Matthias Wenzel
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Patent number: 7825155Abstract: 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: GrantFiled: September 13, 2006Date of Patent: November 2, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
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Publication number: 20100273840Abstract: 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: ApplicationFiled: April 23, 2009Publication date: October 28, 2010Inventors: 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
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Publication number: 20100267671Abstract: 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: ApplicationFiled: February 9, 2010Publication date: October 21, 2010Inventors: Jay Jie-Qiang Wu, Ling Wang
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Publication number: 20100267712Abstract: 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: ApplicationFiled: September 26, 2008Publication date: October 21, 2010Applicants: Human Services, Science Applications International Coporation Saic, Albany Molecular Research, Inc.,Inventors: Jill E. Heemskerk, John M. McCall, Keith D. Barnes
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Publication number: 20100255504Abstract: 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: ApplicationFiled: March 17, 2010Publication date: October 7, 2010Applicant: BECTON, DICKINSON AND COMPANYInventors: Zhenjun Diwu, Timothy Dubrovsky, Barnaby Abrams, Jinfang Liao, Qinglin Meng
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Patent number: 7795297Abstract: 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: GrantFiled: February 28, 2008Date of Patent: September 14, 2010Assignee: Laboratories Fournier S.A.Inventors: Jean Binet, Benaiessa Boubia, Pierre Dodey, Christiane Legendre, Martine Barth, Olivia Poupardin-Olivier
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Publication number: 20100222358Abstract: 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: ApplicationFiled: March 2, 2010Publication date: September 2, 2010Applicant: ABBOTT LABORATORIESInventors: 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
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Publication number: 20100216787Abstract: 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: ApplicationFiled: December 22, 2009Publication date: August 26, 2010Applicant: 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
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Publication number: 20100216833Abstract: 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: ApplicationFiled: May 6, 2010Publication date: August 26, 2010Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
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Publication number: 20100210685Abstract: The present invention relates to substituted indoles of formula (I), useful as pharmaceutical compounds for treating respiratory disorders.Type: ApplicationFiled: April 28, 2010Publication date: August 19, 2010Inventors: Timothy Birkinshaw, Roger Bonnert, Tony Cook, Rukhsana Rasul, Hitesh Sanganee, Simon Teague
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Publication number: 20100197716Abstract: 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: ApplicationFiled: April 16, 2010Publication date: August 5, 2010Inventors: Jennifer Qiao, Tammy C. Wang, James C. Sutton, Timur Gungor
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Publication number: 20100197871Abstract: 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: ApplicationFiled: September 15, 2008Publication date: August 5, 2010Inventors: M.G. Finn, Valentin O. Rodionov
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Publication number: 20100197644Abstract: 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 medicamentsType: ApplicationFiled: December 21, 2009Publication date: August 5, 2010Inventors: 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
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Publication number: 20100190782Abstract: 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: ApplicationFiled: December 17, 2009Publication date: July 29, 2010Inventors: 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
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Patent number: 7745443Abstract: 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: GrantFiled: April 2, 2007Date of Patent: June 29, 2010Assignees: Sanofi-Aventis Deutschland GmbH, Ajinomoto Co., Inc.Inventors: Otmar Klingler, Melitta Just, Kuniya Sakurai, Naoyuki Fukuchi
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Patent number: 7745632Abstract: 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 substType: GrantFiled: April 4, 2006Date of Patent: June 29, 2010Assignee: Adeka CorporationInventors: Yohei Aoyama, Koichi Shigeno
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Publication number: 20100152195Abstract: 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 substituentType: ApplicationFiled: December 16, 2009Publication date: June 17, 2010Inventors: Luca Arista, Giorgio Bonanomi, Anna Maria Capelli, Federica Damiani, Romano Di Fabio, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco, Silvia Terreni
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Publication number: 20100137301Abstract: 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: ApplicationFiled: February 8, 2010Publication date: June 3, 2010Inventors: Michael Lee Jones, David Gunn, John Howard Jones, Michael C. Van Zandt
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Publication number: 20100136491Abstract: 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: ApplicationFiled: April 24, 2008Publication date: June 3, 2010Inventors: Akira Matsumoto, Junichi Tanabe, Hisatoshi Kura, Masaki Ohwa
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Publication number: 20100136467Abstract: 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: ApplicationFiled: April 28, 2008Publication date: June 3, 2010Inventors: Akira Matsumoto, Junichi Tanabe, Hisatoshi Kura, Masaki Ohwa
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Publication number: 20100121059Abstract: 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: ApplicationFiled: July 6, 2009Publication date: May 13, 2010Applicant: The Regents of the University of CaliforniaInventors: Heike Wulff, Ananthakrishnan Sankaranarayanan, Wolfram Haensel, Alexander Schmitz, Kristina Schmidt-Lassen
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Publication number: 20100113789Abstract: 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: ApplicationFiled: September 30, 2005Publication date: May 6, 2010Applicants: FUJIFILM CORPORATIONInventors: Masataka Ihara, Kiyosei Takasu, Khanitha Pudhom, Hiroshi Kitaguchi, Masayuki Kawakami, Kozo Sato
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Publication number: 20100093651Abstract: 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: ApplicationFiled: October 19, 2007Publication date: April 15, 2010Inventors: Lorraine V. Brando, Gary H. Posner, John G. D'Angelo, Robert H. Yolken, Christopher P. Hencken, Lauren Woodard
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Patent number: 7674809Abstract: 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: GrantFiled: March 1, 2005Date of Patent: March 9, 2010Assignee: Rottapharm S.p.A.Inventors: Francesco Makovec, Antonio Giordani, Roberto Artusi, Stefano Mandelli, Ilario Verpilio, Simona Zanzola, Lucio Claudio Rovati
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Patent number: 7659404Abstract: 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, C1-6Type: GrantFiled: February 14, 2002Date of Patent: February 9, 2010Assignee: 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
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Patent number: 7659269Abstract: 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: GrantFiled: December 4, 2007Date of Patent: February 9, 2010Assignee: The Institute for Pharmaceutical Discovery, LLCInventors: Michael Jones, David Gunn, John Jones, Michael Van Zandt
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Patent number: 7625758Abstract: 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: GrantFiled: January 26, 2005Date of Patent: December 1, 2009Inventor: Thomas R. Berkelman
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Publication number: 20090281321Abstract: 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: ApplicationFiled: July 17, 2009Publication date: November 12, 2009Inventors: 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
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Publication number: 20090263843Abstract: 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: ApplicationFiled: March 26, 2009Publication date: October 22, 2009Applicant: Promega CorporationInventors: Jessica Anderson, Poncho Meisenheimer, John Shultz
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Publication number: 20090253656Abstract: 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: ApplicationFiled: March 29, 2006Publication date: October 8, 2009Applicant: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
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Patent number: 7598390Abstract: 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: GrantFiled: May 11, 2006Date of Patent: October 6, 2009Assignee: Life Technologies CorporationInventors: Jolene A. Bradford, Ching-Ying Cheung, Shih-Jung Huang, Patrick R. Pinson, Stephen T. Yue
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Patent number: 7592361Abstract: 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: GrantFiled: April 28, 2004Date of Patent: September 22, 2009Assignee: Bayer Pharmaceuticals CorporationInventors: Xin Ma, Louis-David Cantin, Soongyu Choi, Roger Clark, Martin Hentemann, Joachim Rudolph, Rico Lavoie, Zhonghua Zhang
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Publication number: 20090221564Abstract: 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: ApplicationFiled: February 20, 2007Publication date: September 3, 2009Applicant: TRIGEN LIMITEDInventors: Shouming Wang, Toby Jonathan Blench, Frederic Marlin, Richard Beck, Roger Peter Dickinson
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Publication number: 20090218039Abstract: 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: ApplicationFiled: February 27, 2009Publication date: September 3, 2009Applicant: FUJIFILM CorporationInventors: Yoshihiko FUJIE, Tetsuya WATANABE, Hisashi MIKOSHIBA
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Patent number: 7582672Abstract: The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.Type: GrantFiled: October 22, 2004Date of Patent: September 1, 2009Assignee: Oxagen LimitedInventors: David Middlemiss, Mark Richard Ashton, Edward Andrew Boyd, Frederick Arthur Brookfield, Eric R. Pettipher, Michael George Hunter, Mark Whittaker, Chris Palmer
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Publication number: 20090209583Abstract: 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: ApplicationFiled: June 22, 2007Publication date: August 20, 2009Inventors: 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
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Patent number: 7563902Abstract: 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: GrantFiled: January 25, 2006Date of Patent: July 21, 2009Assignee: Roche Diagnostics Operations, Inc.Inventors: Dieter Heindl, Rupert Herrmann, Wolfgang Jenni
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Publication number: 20090176840Abstract: 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: ApplicationFiled: June 17, 2008Publication date: July 9, 2009Inventors: Michael Konkel, John M. Werzel, Jamie Talisman
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Patent number: 7557138Abstract: 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: GrantFiled: October 4, 2004Date of Patent: July 7, 2009Assignee: The Regents of the University of CaliforniaInventors: Heike Wulff, Ananthakrishnan Sankaranarayanan, Wolfram Haensel, Alexander Schmitz, Kristina Schmidt-Lassen
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Patent number: 7553848Abstract: 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: GrantFiled: January 21, 2005Date of Patent: June 30, 2009Assignee: Amgen Inc.Inventors: Christopher Hulme, Mqhele Vellah Ncube, Mark H. Norman, Vassil I. Ognyanov, Liping H. Pettus, Jiawang Zhu
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Publication number: 20090156586Abstract: 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: ApplicationFiled: February 3, 2009Publication date: June 18, 2009Inventors: 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
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Patent number: 7514460Abstract: 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: GrantFiled: December 15, 2005Date of Patent: April 7, 2009Assignee: 4SC AGInventors: Thomas Herz, Rolf Krauss, Michael Kubbutat, Martin Lang, Christoph Schaechtele, Stefan Tasler, Frank Totzke
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Patent number: 7507831Abstract: 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: GrantFiled: January 11, 2006Date of Patent: March 24, 2009Inventors: Alan P. Kozikowski, Werner Tückmantel, Leo J. Romanczyk, Jr.
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Publication number: 20090066245Abstract: 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: ApplicationFiled: February 23, 2006Publication date: March 12, 2009Applicant: TORAY INDUSTRIES, INC.Inventors: Kazunori Sugimoto, Seiichiro Murase, Daisuke Kitazawa, Kazumasa Nagao, Takafumi Ogawa, Tsuyoshi Tominaga
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Publication number: 20090054652Abstract: 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: ApplicationFiled: March 23, 2007Publication date: February 26, 2009Applicant: ADEKA CORPORATIONInventors: Toru Yano, Satoshi Yanagisawa, Yohei Aoyama, Koichi Shigeno
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Publication number: 20090035810Abstract: 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: ApplicationFiled: May 29, 2008Publication date: February 5, 2009Applicant: INVITROGEN CORPORATIONInventors: Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue
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Publication number: 20090035809Abstract: 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: ApplicationFiled: May 29, 2008Publication date: February 5, 2009Applicant: INVITROGEN CORPORATIONInventors: Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue
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Patent number: 7482344Abstract: 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: GrantFiled: December 15, 2004Date of Patent: January 27, 2009Assignee: Eli Lilly and CompanyInventors: Michael Joseph Coghlan, Prabhakar Kondaji Jadhav, James Joseph Droste, Jonathan Edward Green, Donald Paul Matthews