Polycyclo Ring System Which Includes Ring Chalcogen Patents (Class 548/525)
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Publication number: 20110021556Abstract: The invention relates to 3,3 disubstituted pyrrole derivatives useful for treatment of diseases associated with monoamine reuptake inhibitors. Also provided pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: ApplicationFiled: March 10, 2009Publication date: January 27, 2011Applicant: Hoffman-La Roche, Inc.Inventors: Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
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Publication number: 20110021528Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: PHARMACYCLICS, INC.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Publication number: 20110015185Abstract: The present invention relates to compounds of formula (I): wherein P, R3, W1, and W2 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.Type: ApplicationFiled: September 28, 2010Publication date: January 20, 2011Applicant: BIOVITRUM ABInventors: Gary Johansson, Peter Brandt, Björn M. Nilsson
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Benzothiophene hydroxamic acid derivatives with carbamate, urea, amide and sulfonamide substitutions
Patent number: 7872024Abstract: The present invention relates to a novel class of hydroxamic acid derivatives carbamate, urea, amide and sulfonamide substitutions. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: April 14, 2006Date of Patent: January 18, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Joey Methot, Thomas A. Miller, David J. Witter -
Publication number: 20110009396Abstract: The present invention provides compounds represented by formula 1: wherein, R1 R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined in the specification, in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. These compounds are useful for treatment of inflammatory disorders including those caused by elevated levels of proinflammatory cytokines such as Tumor Necrosis Factor (TNF-? and/or interleukins (IL-1?, IL-6, IL-8). The invention also relates to processes for the manufacture of compounds of formula 1 and pharmaceutical compositions containing them.Type: ApplicationFiled: July 25, 2008Publication date: January 13, 2011Inventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Rada Dalal, Sapna Parikh, Aditi Amol Tannu
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Patent number: 7858657Abstract: Novel wortmannin analogs and their use in inhibiting PI-3-kinase activity in mammals and the treatment or prevention of cancer and tumor formation in a subject are described herein. Preferably, the wortmannin analogs may be administered with other chemotherapeutic agents in the treatment of cancer.Type: GrantFiled: September 23, 2008Date of Patent: December 28, 2010Assignees: Proix Pharmaceutical Corp., Arizona Board of Regents, Acting on Behalf of The University of Arizona, University of Pittsburgh - Of the Commonwealth System of Higher EducationInventors: Lynn D. Kirkpatrick, Garth Powis, Peter Wipf
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Publication number: 20100324009Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.Type: ApplicationFiled: August 24, 2010Publication date: December 23, 2010Applicant: Gruenenthal GmbHInventors: Stefan OBERBOERSCH, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Franz-Martin Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
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Publication number: 20100324296Abstract: A naphthopyran compound represented by the formula B1 and B2 may include a phenyl, naphthyl, or heterocyclic aromatic group, or may combine to form one or more aromatic rings. B1 and B2 may further include one or more substituents. Ra may include an alkyl, polycycloalkyl, alkenyl, polyalkenyl, haloalkyl, perhaloalkyl, alkynyl, polyalkynyl, hydroxyalkynyl, polyhydroxyalkynyl; or (C3-20)cycloalkyl group. Rb and Rc may include hydrogen or alkyl groups, or may combine to form a saturated heterocyclic group, or together with an adjacent phenyl group may form a julolidinyl group. R3, R4, R5, R6, and R10 may include hydrogen, halogen, —Ra, —OH, —ORa, —O—CO—Ra, —CN, —NO2, —SO2Ra, —SORa, —SH, —SRa, —NH2, —NHRa, —NRaRa, or —NRbRc; or any two or more may combine to form a cyclic group. R7 is a mesogenic group. And the naphthopyran, which may be referred to as a dichroic-photochromic compound, may be incorporated into an optical article.Type: ApplicationFiled: October 17, 2007Publication date: December 23, 2010Inventors: Ludmila Sukhomlinova, Linli Su, Tamas Kosa, Bahman Taheri
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Publication number: 20100317871Abstract: A method of preparing (3S)-1-[2-(2,3-dihydro-5-benzofuranyl)ethyl}-?,?-diphenyl-3-pyrrolidine acetamide hydrogen bromide, wherein 3-(S)-(I-carbamoyl-1,1-diphenylmethyl)pyrrolidine or its salt with an organic acid is alkylated in the presence of an inorganic base with 5-(2-bromoethyl)-2,3-dihydrobenzofurane in a heterogeneous system of the solvents water and an organic solvent selected from C6 to C9 aliphatic, alicyclic or aromatic hydrocarbons, after separation of the two phases the crude darifenacin base is isolated, which is converted to the hydrobromide by addition of a C3 to C9 ketone or C3 to C9 alcohol and concentrated hydrobromic acid.Type: ApplicationFiled: January 14, 2009Publication date: December 16, 2010Inventors: Ludmila Hejtmankova, Josef Jirman
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Publication number: 20100317644Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.Type: ApplicationFiled: August 24, 2010Publication date: December 16, 2010Applicant: Gruenenthal GmbHInventors: Stefan OBERBOERSCH, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Franz-Martin Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
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Publication number: 20100292190Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.Type: ApplicationFiled: February 14, 2006Publication date: November 18, 2010Applicant: Bionomics LimitedInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
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Patent number: 7834034Abstract: The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: April 14, 2006Date of Patent: November 16, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Dawn M. Mampreian, Thomas A. Miller, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
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Patent number: 7834194Abstract: The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, R0 is (II), or (III) G1 is methylene or ethylene; L is a divalent linking group selected from —(C1-C4) alkylene-, —S—, —CH(OH)—, or —O—; A is methylene, —S—, —O—, or —NH—; and the other substituents are as defined in the claims.Type: GrantFiled: December 16, 2005Date of Patent: November 16, 2010Assignee: Eli Lilly and CompanyInventors: Thomas Daniel Aicher, Mark Joseph Chicarelli, Ronald Jay Hinklin, Hongqi Tian, Owen Brendan Wallace
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Publication number: 20100280246Abstract: Novel linkers for linking a donor dye to an acceptor dye in an energy transfer fluorescent dye are provided. These linkers facilitate the efficient transfer of energy between a donor and acceptor dye in an energy transfer dye. One of these linkers for linking a donor dye to an acceptor dye in an energy transfer fluorescent dye has the general structure R21Z1C(O)R22R28 where R21 is a C1-5 alkyl attached to the donor dye, C(O) is a carbonyl group, Z1 is either NH, sulfur or oxygen, R22 is a substituent which includes an alkene, diene, alkyne, a five and six membered ring having at least one unsaturated bond or a fused ring structure which is attached to the carbonyl carbon, and R28 includes a functional group which attaches the linker to the acceptor dye.Type: ApplicationFiled: December 28, 2006Publication date: November 4, 2010Applicant: Applera CorporationInventors: Linda G. Lee, Sandra L. Spurgeon, Barnett Rosenblum
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Patent number: 7812178Abstract: The present invention relates to an isoquinoline compound represented by the following formula (I), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction. Furthermore, this compound is useful as a prophylactic and/or therapeutic agent that improves neurological symptoms associated with cerebral infarction, particularly acute cerebral infarction. wherein the symbols are the same as defined in the description.Type: GrantFiled: November 3, 2008Date of Patent: October 12, 2010Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Masakazu Fujio, Hiroyuki Satoh, Shinya Inoue, Toshifumi Matsumoto, Yasuhiro Egi
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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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Publication number: 20100249205Abstract: Novel metabolites of wortmannin and wortmannin analogs and their use in inhibiting PI-3 kinase activity in mammals and the treatment and prevention of cancer or tumor formation in a subject are described herein.Type: ApplicationFiled: April 1, 2010Publication date: September 30, 2010Applicant: ARIZONA BOARD OF REGENTSInventor: Garth Powis
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Publication number: 20100240653Abstract: The present invention relates to certain biphenyl sulfonamide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3-receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease and the like.Type: ApplicationFiled: October 16, 2007Publication date: September 23, 2010Inventors: Vincent J. Santora, Ryan M. Hart, Jason B. Ibarra, Douglas M. Park, Albert S. Ren, Graeme Semple, Jeffrey A. Schultz, Brian M. Smith, Jeffrey Smith
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Publication number: 20100222381Abstract: Compounds represented by Formula (I): are useful in treating diseases, such as cancer, that are mediated and/or associated (at least in part) with DNMT3b activity. The compounds can be formulated as pharmaceutically acceptable compositions for administration to a subject in need thereof.Type: ApplicationFiled: February 26, 2010Publication date: September 2, 2010Inventors: Hariprasad Vankayalapati, Krzysztof Swierczek, Scott Albert Pearce
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Publication number: 20100222338Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.Type: ApplicationFiled: May 13, 2010Publication date: September 2, 2010Inventors: Wenge Zhong, Stephen Hitchcock, Brian K. Albrecht, Michael D. Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Dean Hickman, Daniel Horne, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig E. Masse, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang, Holger Monenschein, Thomas Nguyen
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Publication number: 20100204198Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.Type: ApplicationFiled: March 29, 2010Publication date: August 12, 2010Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Jörg Velker, Thomas Weller
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Publication number: 20100204296Abstract: The present invention provides a novel and stable amorphous form of darifenacin free base, process for preparation, pharmaceutical compositions, and method of treating thereof. The present invention further provides a novel and stable polymorphic form of darifenacin hydrobromide, process for preparation, pharmaceutical compositions, and method of treating thereof.Type: ApplicationFiled: June 9, 2008Publication date: August 12, 2010Applicant: ACTAVIS GROUP PTC EHFInventors: Eswara Rao Kodali, Sreekanth Medikonduri, Praveen Kumar Neela, Nitin Sharadchandra Pradhan, Jon Valgeirsson
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Publication number: 20100204470Abstract: The present invention provides a new method for preparation and crystallization of hydrochlorides, hydrobromides or hydroiodides of pharmaceutical compounds or their intermediates in which the base or its acid addition salt is reacted in a solvent with a Trialkylsilylhalogenide.Type: ApplicationFiled: June 25, 2007Publication date: August 12, 2010Inventors: Josef Wieser, Hannes Lengauer, Elfriede Klingler, Arthur Pichler, Hubert Sturm
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Publication number: 20100197030Abstract: The present invention relates to fluorescent dyes in general. The present invention provides a wide range of fluorescent dyes and kits containing the same, which are applicable for labeling a variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes for research and development, forensic identification, environmental studies, diagnosis, prognosis, and/or treatment of disease conditions.Type: ApplicationFiled: February 3, 2010Publication date: August 5, 2010Applicant: Biotium, Inc.Inventors: Fei Mao, Wai-Yee Leung, Ching-Ying Cheung
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Patent number: 7759389Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1, R2, R3 and R4 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.Type: GrantFiled: December 21, 2005Date of Patent: July 20, 2010Assignee: Roche Palo Alto LLCInventors: Nancy Elisabeth Krauss, Shu-Hai Zhao
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Publication number: 20100179210Abstract: The present invention relates to an enantiomerically pure (+)-trans-enantiomer of a compound represented by the following formula (I): wherein R1, R2, R3, R4 and R9 are as defined in the specification; enantiomerically pure intermediates thereof, to processes for the preparation of the enantiomerically pure compound and its intermediates, and to a pharmaceutical composition comprising the enantiomerically pure compound. The compound of formula (I) is useful for the treatment of diseases or disorders mediated by the inhibition of cyclin dependant kinase, such as cancer.Type: ApplicationFiled: June 21, 2006Publication date: July 15, 2010Inventors: Meenakshi Sivakumar, Malcolm Mascarenhas, Ankush Sarde, Pramod Kumar Jadhav, Manoj Shukla, Kalpana Joshi, Maggie Rathos
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Patent number: 7745645Abstract: Compounds having the general of formula I and/or formula II wherein R1 and R2 are the same or different and are independently selected from the group consisting of —H, —C1-C18-alkyl or -?-sulfoalkyl; X and Y are the same or different and are independently selected from the group consisting of —O?, —OH, —SH, —NH—NH2, —F, —Cl, —Br, —I, —O-Su (succinimidyl/sulfosuccinimidyl), —O-STP (4-sulfo-2,3,5,6-tetrafluorophenyl), —O-TFP (2,3,5,6-tetrafluorophenyl), —O-benzotriazole, -benzotriazole, —NR—CO—CH2—I, —NR2, —NR-biomolecule, —NR-L-COO?, —NR-L-COOH, —NR-L-COO-Su, —NR-L-COO-STP, —NR-L-COO-TFP, —NR-L-CONR2, —NR-L-CO-biomolecule, —NR-L-CO—NH—NH2, —NR-L-OH, —NR-L-O-phosphoramidite, —NR-L-CHO, —NR-L-maleimid, or —NR-L-NH—CO—CH2—I; where R is equal to R1 and R2 and L is selected from the group consisting of a divalent linear (—(CH2)o—, o=1 to 15), crossed, or cyclic alkane group that can be substituted by at least one atom selected from the group consisting of oxygen, substituted niType: GrantFiled: January 22, 2007Date of Patent: June 29, 2010Assignee: Pierce Biotechnology, Inc.Inventors: Wilhelm G. Frank, Matthias S. Wenzel, Peter T. Czerney, Surbhi Desai, Greg Hermanson
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Publication number: 20100160289Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: ApplicationFiled: December 15, 2009Publication date: June 24, 2010Inventors: Mark J. Macielag, James J. McNally
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Patent number: 7737166Abstract: A 1,6-?-glucan synthetase inhibitor is provided, having potent growth inhibition and having excellent safety. A compound is provided, capable of expressing in a wide spectral range and specifically or selectively, an antifungal effect based on its functional mechanism of 1,6-?-glucan synthesis inhibition. Also provided is a drug, a salt or hydrate thereof, especially an antifungal that contains the compound.Type: GrantFiled: August 16, 2006Date of Patent: June 15, 2010Assignee: Daiichi Sankyo Company, LimitedInventors: Katsuhiro Kawakami, Kazuo Kanai, Takao Horiuchi, Hiroshi Takeshita, Syozo Kobayashi, Yuichi Sugimoto, Issei Achiwa, Junichi Kuroyanagi
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Publication number: 20100145056Abstract: Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.Type: ApplicationFiled: November 23, 2009Publication date: June 10, 2010Inventors: Varghese John, Michel Maillard, James P. Beck, Eric T. Baldwin, Robert Hughes, Shon R. Pulley, Ruth T. TenBrink
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Publication number: 20100144729Abstract: A compound of formula (I) wherein R1, R2, R3 and R4 are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.Type: ApplicationFiled: January 31, 2008Publication date: June 10, 2010Inventors: Rolf Baenteli, Nigel Graham Cooke, Frederic Zecri, Alexander Baxter Smith
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Patent number: 7723375Abstract: Novel metabolites of wortmannin and wortmannin analogs and their use in inhibiting PI-3 kinase activity in mammals and the treatment and prevention of cancer or tumor formation in a subject are described herein.Type: GrantFiled: December 29, 2006Date of Patent: May 25, 2010Assignee: Arizona Board of Regents, acting on behalf of The University of ArizonaInventor: Garth Powis
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Patent number: 7714150Abstract: Compounds corresponding to formula I, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n have the meanings given in the description, and also a process for the preparation of these compounds and intermediate products of this process. Furthermore, pharmaceutical compositions comprising the compounds of Formula I and related methods of treatment.Type: GrantFiled: April 10, 2006Date of Patent: May 11, 2010Assignee: Solvay Pharmaceuticals GmbHInventors: Brian Moloney, Lester Marrison, Dieter Ziegler, Michael Mlinaric, Christiane Boecker, Reinhard Brueckner, Michael Weske, Klaus Witte, Yvan Fischer
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Publication number: 20100113549Abstract: The present invention relates to a process for the preparation of a pyrrolidone compound of the formula (I): where R1 is substituted or unsubstituted alkyl, alkenyl, or alkynyl, or an aromatic or non-aromatic cyclic or heterocyclic structure, R2 is substituted or unsubstituted alkyl or cycloalkyl, and each P is independently a protecting group.Type: ApplicationFiled: December 6, 2005Publication date: May 6, 2010Applicant: ISIS INNOVATION LTD.Inventors: Timothy Block, Ben Davis, Timothy Chapman, Christopher Schofield
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Patent number: 7700584Abstract: The present invention provides curcumol derivatives of the following formula (I) or pharmaceutical acceptable salts thereof: wherein, Y is selected from the group consisting of ?CHR2, —CH2R2, ?O, ?—OH or —OR1;R1 is selected from H, R, RCO or HO3S; and R is selected from the group consisting of H; saturated or unsaturated linear C1-10 hydrocarbon group and the like; R2 is selected from the group consisting of F; Cl; Br; I; H; —OH; —OR; —HSO3 and the like; with the proviso that both R1 and R2 are not H. The present invention also provides anti-tumor or antiviral pharmaceutical compositions comprising said derivatives or pharmaceutical acceptable salts thereof. The present invention further provides the use of said derivatives or pharmaceutical acceptable salts thereof in the preparation of a medicament for prophylaxis and/or treatment tumor or an antiviral medicament.Type: GrantFiled: May 26, 2005Date of Patent: April 20, 2010Assignee: Hangzhou Minsheng Pharmaceuticals Co., Ltd.Inventors: Shulong Wang, Dianwu Guo, Zhaoke Meng
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Patent number: 7696350Abstract: This invention relates to chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: GrantFiled: September 28, 2005Date of Patent: April 13, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Jørgen Scheel-Krüger, Elsebet Østergaard Nielsen
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Publication number: 20100048512Abstract: Administration of either a tocopherol represented by the general formula (1) or a tocotrienol compound ester derivative before or after exposure to radiation is effective in preventing or treating health disorders caused by the radiation exposure.Type: ApplicationFiled: November 14, 2007Publication date: February 25, 2010Applicants: National Institute of Radiological Sciences, Fukuoka UniversityInventors: Kazunori Anzai, Megumi Ueno, Haruko Yakumaru, Junichi Ueda, Makoto Akashi, Shizuko Kobayashi, Jiro Takata, Nobuo Ikota
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Publication number: 20100039688Abstract: A naphthopyran compound represented by the formula (I) wherein: n1, n2, p, m and q represent an integer; R1, R2 and R4, represent a group selected from halogen, —Ra, —OH, —ORa, —SH, —SRa, —NH2, —NRaRa1, —NRbRc, —CO—Ra, —CO2Ra1, —OC(O)—Rd, —X—(Re)—Y, linear or branched (C1-C18) perfluoroalkyl group, wherein Ra, Ra1, Rb, Rc, X, Y, Re, and Rd are as defined in the description; Z represents a group selected from CO, CS, SO, SO2, CO2, C(O)S, CS2, C(O)NH, C(O)NRa, C(S)NH, C(S)NRa and C?NRa; R3 represents a group selected from halogen, —Ra, linear or branched (C1-18) perfluoroalkyl group —OH, —ORa, —SH, —SRa, —NH2, and —NRaRa1; R6 represents a group selected from —Ra which may be optionally substituted, linear or branched (C1-18) perfluoroalkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl, which may be optionally substituted; R5 represents a group selected from: halogen, —Ra, linear or branched (C1-18) perfluoroalkyl group, —OH, —ORa, —SH, —SRa, —NH2, —NRaRa1, —CO—Ra, —O—C(O)—Ra and —CO2Ra1; or when q is equaType: ApplicationFiled: September 5, 2007Publication date: February 18, 2010Inventors: Stuart Aiken, Jean-Paul Cano, Christopher David Gabbutt, Bernard Mark Heron
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Patent number: 7662977Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.Type: GrantFiled: December 21, 2007Date of Patent: February 16, 2010Assignee: Semafore Pharmaceuticals, Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
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Patent number: 7662824Abstract: The invention is directed to acylhydrazones compounds of Formula I: where R1, R2 and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.Type: GrantFiled: March 16, 2006Date of Patent: February 16, 2010Assignee: Janssen Pharmaceutica NVInventors: Kristi Leonard, Tianbao Lu, Robert W. Tuman, Dana L. Johnson, Anna C. Maroney, Jan L. Sechler, Richard W. Connors, Richard S. Alexander, Maxwell D. Cummings, Robert A. Galemmo, Thomas P. Markotan
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Patent number: 7649001Abstract: The present invention provides a compound represented by the general formula: [wherein Ring A represents an optionally substituted 5- to 8-membered ring, Ring B represents a further optionally substituted 4- to 10-membered ring, Ring C represents a further optionally substituted benzene ring, X1 represents carbon atom, X2 represents a carbon atom, an oxygen atom, etc., W represents a nitrogen atom, etc., Y11 represents a group represented by the formula CR2R3? (wherein R2 represents a hydrogen atom, a cyano group, a nitro group, etc., and R3? represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), Y21 represents a group represented by the formula CR4R5? (wherein R4 represents a hydrogen atom, a cyano group, a nitro group, etc., and R5? represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), etc., and R1 represents an electron-withdrawing group, respectively.Type: GrantFiled: August 11, 2003Date of Patent: January 19, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Mitsuru Shiraishi, Takahito Hara, Masami Kusaka, Naoyuki Kanzaki, Satoshi Yamamoto, Toshio Miyawaki
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Patent number: 7649011Abstract: Pharmaceutical compositions containing organic compounds or salts thereof that serve as modulators for the SDF-1 or I-TAC chemokines are disclosed. The compounds and compositions are useful in the treatment of cancer, especially in the inhibition of cancer proliferation, growth, and metastasis. Methods of interfering with SDF-1 and/or I-TAC binding to the CCXCKR2 receptor and treating cancer using the compounds and pharmaceutical compositions of the present invention are also disclosed.Type: GrantFiled: December 22, 2003Date of Patent: January 19, 2010Assignee: Chemocentryx, Inc.Inventors: Anita Melikian, Jennifer Burns, Brian E. McMaster, Thomas Schall, J. J. Wright
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Publication number: 20090306406Abstract: A process for preparing substituted pyrrolidine compounds, including (5)-2-{1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]-3-pyrrolidinyl}-2,2-diphenylacetamide hydrobromide, commonly known in the art as darifenacin, comprising reacting a pyrrolidine compound with a benzofuran derivative in the presence of a phase-transfer catalyst.Type: ApplicationFiled: September 7, 2007Publication date: December 10, 2009Applicant: Medichem ,S.A.Inventors: Núria Soldevilla Madrid, Ernesto Durán López, Jordi Puig Serrano
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Publication number: 20090305410Abstract: The present invention relates to fluorescent dyes in general. The present invention provides a wide range of fluorescent dyes and kits containing the same, which are applicable for labeling a variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes for research and development, forensic identification, environmental studies, diagnosis, prognosis, and/or treatment of disease conditions.Type: ApplicationFiled: December 12, 2008Publication date: December 10, 2009Applicant: Biotium, Inc.Inventors: Fei Mao, Wai-Yee Leung, Ching-Ying Cheung, Hye Eun Hoover
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Patent number: 7629340Abstract: Disclosed are compounds having Formula (I) and the compositions and methods relating to these compounds, for treating or preventing a viral infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, R2, m, R, V, W, T, Z, R1, Y, and p are disclosed herein.Type: GrantFiled: December 12, 2006Date of Patent: December 8, 2009Assignee: SmithKline Beecham CorporationInventors: Franz Ulrich Schmitz, Christopher Don Roberts, Ali Dehghani Mohammad Abadi, Ronald Conrad Griffith, Martin Robert Leivers
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Patent number: 7608592Abstract: The present invention is directed to compounds that are antiviral agents. Specifically the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: GrantFiled: June 28, 2006Date of Patent: October 27, 2009Assignee: ViroBay, Inc.Inventors: Michael Graupe, John O. Link, Chandrasekar Venkataramani
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Publication number: 20090219526Abstract: The present disclosure provides isotopically substituted compounds of the formula (I): wherein T, U, V, W, X, Y, Z, R0, R3, R4, R5 and R6 are as defined in the detailed description. The method for detection and quantification using the same is also disclosed.Type: ApplicationFiled: December 29, 2008Publication date: September 3, 2009Inventors: Vincent Jo Davisson, Shirshendu K. Deb, Giselle Marcelline Knudsen-Mooney, Meiguo Xin
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Publication number: 20090221666Abstract: The present invention provides stilbene derived compounds having antineoplastic and/or antimicrobial activity. Preferred compounds of the invention include compounds of the formula (I) wherein R is Dap, Dap-Dil, Dap-Dil-Val, or Dap-Dil-Val-Dov; R1 is H, OH, or PO3Na2; and R2 and R3 are jointly —CH2— or each independently H, OH, CH3, or PO3Na2; and compounds of the formulas (II), (III) and salts thereof, wherein R and R1 are independently H or P(O)(OH). The present invention is further directed to methods of inhibiting cancer cell growth and/or microbial growth and compositions for use therewith.Type: ApplicationFiled: May 12, 2006Publication date: September 3, 2009Inventors: George R. Pettit, Collin R. Anderson
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Publication number: 20090215993Abstract: Described are immunogenic compounds useful for generation of antibodies which are highly specific for mycophenolic acid which do not react or have substantially no cross-reactivity with the glucuronide metabolites of mycophenolic acid, especially the acyl-glucuronide metabolite.Type: ApplicationFiled: October 24, 2008Publication date: August 27, 2009Inventors: Mitali Ghoshal, Raymond Hui, Shaker Rashid
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Publication number: 20090208449Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5 and X are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: February 12, 2009Publication date: August 20, 2009Inventors: Sharada Shenvi Labadie, Clara Jeou Jen Lin, Francisco Xavier Talamas, Robert James Weikert