Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 514/222.8)
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Publication number: 20130345128Abstract: The invention relates to the compounds of formula (I) and physiologically acceptable salts thereof. The compounds are suitable, e.g., for treating hyperglycemia.Type: ApplicationFiled: March 7, 2012Publication date: December 26, 2013Applicant: SANOFIInventors: Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Gerhard Kretzschmar, Kurt Ritter, Georg Tschank
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Publication number: 20130338095Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.Type: ApplicationFiled: October 18, 2011Publication date: December 19, 2013Applicant: ELCELYX THERAPEUTICS, INC.Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
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Patent number: 8591885Abstract: Biocompatible intraocular drug delivery systems include a carbonic anhydrase inhibitor therapeutic agent and a polymeric component in the form of an implant, a microparticle, a plurality of implants or microparticles, and combinations thereof. The therapeutic agent is released in a biologically active form, for example, the therapeutic agent may retain its three dimensional structure when released into an eye of a patient, or the therapeutic agent may have an altered three. The implants may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions, such as retinal damage, including glaucoma and proliferative vitreoretinopathy among others.Type: GrantFiled: October 31, 2007Date of Patent: November 26, 2013Assignee: Allergan, Inc.Inventors: James N. Chang, Patrick M. Hughes, Gerald W. Devries
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Publication number: 20130310340Abstract: A method for treating muscular deterioration is disclosed. Also disclosed are embodiments of a compound, and compositions comprising the compound, for inhibiting muscular deterioriation, including atrophy, dystrophy, and cachexia, such as may result from ventilation.Type: ApplicationFiled: May 15, 2013Publication date: November 21, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Donald G. Payan, Esteban Masuda, Todd Kinsella
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Publication number: 20130310364Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: ApplicationFiled: July 16, 2013Publication date: November 21, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Thilo Heckrodt, Yan Chen, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
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Patent number: 8575154Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.Type: GrantFiled: August 9, 2011Date of Patent: November 5, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Masakuni Kori, Toshihiro Imaeda, Shinji Nakamura, Masashi Toyofuku, Eiji Honda, Yasutomi Asano, Osamu Ujikawa, Michiyo Mochizuki
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Publication number: 20130190291Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.Type: ApplicationFiled: August 9, 2011Publication date: July 25, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masakuni Kori, Toshihiro Imaeda, Shinji Nakamura, Masashi Toyofuku, Eiji Honda, Yasutomi Asano, Osamu Ujikawa, Michiyo Mochizuki
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Publication number: 20130184266Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.Type: ApplicationFiled: February 22, 2013Publication date: July 18, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventor: TAKEDA PHARMACEUTICAL COMPANY LIMITED
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Publication number: 20130164386Abstract: Therapeutic agents that target the alpha3 expressing isozymes of the sodium pump at the peripheral terminals of cough receptors and methods of use thereof to prevent or treat cough are disclosed.Type: ApplicationFiled: June 17, 2011Publication date: June 27, 2013Applicant: THE JOHNS HOPKINS UNIVERSITYInventor: Brendan J. Canning
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Publication number: 20130116243Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: December 23, 2010Publication date: May 9, 2013Applicant: ALMAC DISCOVERY LIMITEDInventors: Lixin Zhang, Graham Peter Trevitt, Hugues Miel, Frank Burkamp, Timothy Harrison, Andrew John Wilkinson, Charles-Henry Fabritius
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Publication number: 20130109656Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: August 15, 2012Publication date: May 2, 2013Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robinson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtli
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Publication number: 20130089606Abstract: It now has been found that oral administration of pharmaceutical agents, including N-methylol transfer agents such as Taurolidine may be used to provide efficacious blood plasma concentration of the agents for treatment of diseases by providing release of the active agent into the duodenum or jejunum of a patient and/or at a pH of about 5.4 to about 6.5. Embodiments of the invention therefore provide oral dosage forms, compositions and methods for administration of pharmaceutical agents to the duodenum or jejunum of a patient, and/or which release at a pH of about 5.4 to about 6.5.Type: ApplicationFiled: June 1, 2011Publication date: April 11, 2013Applicant: GEISTLICH PHARMA AGInventors: Rolf W. Pfirrmann, Peter Geistlich
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Publication number: 20130029927Abstract: The invention relates to a combination comprising the N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)-ethyl]-amino]methyl]phenyl]-2E-2-propenamide; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination.Type: ApplicationFiled: July 25, 2012Publication date: January 31, 2013Inventors: Peter Wisdom Atadja, Wenlin Shao, Kapil N. Bhalla
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Publication number: 20120321590Abstract: The invention is directed to amides of bicyclic amine compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.Type: ApplicationFiled: April 5, 2012Publication date: December 20, 2012Applicant: Anadys Pharmaceuticals, Inc.Inventors: Stephen E. Webber, Chinh V. Tran, Alan X. Xiang, Douglas E. Murphy
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Publication number: 20120316156Abstract: The present invention describes [1,2,4]thiadiazine 1,1-dioxide compounds and pharmaceutically acceptable salts thereof, which are useful in lowering serum uric acid in a patient in need thereof comprising administering to the patient a therapeutically or prophylactically effective amount of a [1,2,4]thiadiazine 1,1-dioxide compound.Type: ApplicationFiled: June 6, 2012Publication date: December 13, 2012Applicant: Anadys Pharmaceuticals, Inc.Inventor: James L. Freddo
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Publication number: 20120238447Abstract: The present invention relates to synergistic mixtures comprising, as active components, 1) triazamate as insecticidal compound I; and 2) one fungicidal compound II selected from the group of strobilurines in synergistic effective amounts.Type: ApplicationFiled: November 29, 2010Publication date: September 20, 2012Applicant: BASF SEInventors: Markus Gewehr, Egon Haden, Lutz Brahm
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Publication number: 20120232068Abstract: A compound of formula (I) wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur associated disorders, and other disorders mediated by ion channel function.Type: ApplicationFiled: September 1, 2010Publication date: September 13, 2012Applicant: Briston-Myers Squibb CompanyInventors: James A. Johnson, John Lloyd, Heather Finlay, Ji Jiang, James Neels, Naveen Kumar Dhondi, Prashantha Gunaga, Abhisek Banerjee
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Publication number: 20120219568Abstract: Compositions containing epidithiodioxopiprazines and methods of their use are provided. Epidithiodioxopiprazines can be isolated from natural resources or synthesized de novo. Moreover, epidithiodioxopiprazines, including Verticillin A, are shown to effectively sensitize multiple types of tumor cells to TRAIL-induced apoptosis. In addition, epidithiodioxopiprazines, including Verticillin A, are shown to effectively overcome cancer cell resistance to existing drugs (i.e. Etoposide, Cisplatin, 5-FU and Doxorubicin). Therefore, compositions and methods are provided for use in sensitizing target cancer cells to death receptor- and other anticancer drugs-induced apoptosis. Methods of treating cancer in a subject in need thereof are also provided.Type: ApplicationFiled: February 24, 2012Publication date: August 30, 2012Inventors: Feiyan Liu, Kebin Liu, Ping Wu
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Publication number: 20120214803Abstract: The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.Type: ApplicationFiled: February 2, 2012Publication date: August 23, 2012Applicant: VIFOR (INTERNATIONAL) AGInventors: Wilm Buhr, Susanna Burckhardt, Franz Dürrenberger, Felix Funk, Peter O. Geisser, Vincent A. Corden, Stephen M. Courtney, Graham Dawson, Tara Davenport, Mark Slack, Mark P. Ridgill, Chrostopher J. Yarnold, Susan Boyce, Albertus A. Ellenbroek
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Patent number: 8178677Abstract: Certain imidazoquinolines with a hydroxymethyl or hydroxyethyl substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for preferentially inducing IFN-? biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: GrantFiled: February 22, 2006Date of Patent: May 15, 2012Assignee: 3M Innovative Properties CompanyInventors: Tushar A. Kshirsagar, Bryon A. Merrill, Scott E. Langer, Kyle J. Lindstrom, Sarah J. Slania, Gregory J. Marszalek, Karl J. Manske, Philip D. Heppner, Gregory D. Lundquist, Jr.
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Patent number: 8173641Abstract: The present invention relates to novel benzoxathiazine derivatives of the formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to several processes for preparation thereof and to the use thereof as insecticides and/or acaricides in combination with further compositions such as penetrants and/or ammonium or phosphonium salts.Type: GrantFiled: December 11, 2009Date of Patent: May 8, 2012Assignee: Bayer CropScience AGInventors: Bernd Alig, Klaus-Helmut Müller, Eva-Maria Franken, Ulrich Görgens, Arnd Voerste
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Publication number: 20120107273Abstract: The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof and an anti-HCV agent and an HCV polymerase inhibitor containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: ApplicationFiled: April 25, 2011Publication date: May 3, 2012Applicant: Japan Tobacco Inc.Inventors: Hiroyuki Abe, Masahiro Tanaka, Kazuyuki Sugimoto, Akira Suma, Masahiro Yokota, Makoto Shiozaki, Kiyosei Ilo, Kazuhito Ueyama, Dai Motoda, Toru Noguchi, Tsuyoshi Adachi, Junichiro Tsuruha, Satoki Doi
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Publication number: 20120094983Abstract: A compound of formula I wherein R1, R2, R3, R4 and R5 are described herein.Type: ApplicationFiled: March 15, 2011Publication date: April 19, 2012Inventors: James A. Johnson, Yoon Jeon, John Lloyd, Heather Finlay
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Patent number: 8158794Abstract: Certain imidazoquinolines with a hydroxymethyl or hydroxyethyl substituent at the 2-position, and an aryl or heteroaryl substituent at the 7-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for preferentially inducing IFN-? biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: GrantFiled: February 22, 2006Date of Patent: April 17, 2012Assignee: 3M Innovative Properties CompanyInventors: Tushar A. Kshirsagar, Bryon A. Merrill, Shri Niwas, Gregory D. Lundquist, Jr., Philip D. Heppner, Michael E. Danielson
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Publication number: 20120077799Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.Type: ApplicationFiled: August 9, 2011Publication date: March 29, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masakuni KORI, Toshihiro IMAEDA, Shinji NAKAMURA, Masashi TOYOFUKU, Eiji HONDA, Yasutomi ASANO, Osamu UJIKAWA, Michiyo MOCHIZUKI
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Patent number: 8138176Abstract: Heterocyclic compounds of the formula (I) and salts, preferably pharmaceutically acceptable salts thereof, are provided in which R, R1, R2, Q, m and n have the meanings explained in detail in the description. Also provided are a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.Type: GrantFiled: December 22, 2010Date of Patent: March 20, 2012Assignee: Novartis AGInventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Christiane Marti, Stjepan Jelakovic, Stefan Stutz
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Publication number: 20120035160Abstract: Compounds derived from imidazo[4,5-c][1,2,6]thiadiazine 2,2-dioxides, for use as a drug or pharmaceutical composition for treatment of parasitic diseases, preferably of diseases caused by parasites of the Trypanosoma genus, and more preferably for treatment of the Chagas disease. Furthermore, the invention also relates to the pharmaceutical compositions comprising said compounds.Type: ApplicationFiled: January 26, 2010Publication date: February 9, 2012Applicants: UNIVERSIDAD DE LA REPUB'LICA URUGUAY, CONSEJP SUPERIOR DE INVESTIGACIONES CIENTIFICAS (CISIC)Inventors: Juan Antonio Paez Prosper, Nuria Eugenia Campillo Martín, Ángela Guerra Álvarez, Maria Mercedes González Hormaizteguy, Hugo Cerecetto Meyer
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Patent number: 8101599Abstract: The present invention relates to a combination of organic compounds, a pharmaceutical composition and a kit of parts comprising said combination of organic compounds and to a method of treatment or prevention of certain conditions or diseases.Type: GrantFiled: December 18, 2008Date of Patent: January 24, 2012Assignee: Novartis AGInventors: Suraj S Shetty, Randy L Webb
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Patent number: 8097613Abstract: The invention is directed to [1,2,4]thiadiazine 1,1-dioxide compounds of formula I wherein A is B is and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.Type: GrantFiled: June 9, 2009Date of Patent: January 17, 2012Assignee: Anadys Pharmaceuticals, Inc.Inventors: Frank Ruebsam, Peter Dragovich, Stephen E. Webber, Douglas Eric Murphy, Chinh Viet Tran
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Publication number: 20110319378Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.Type: ApplicationFiled: June 3, 2011Publication date: December 29, 2011Applicant: AMGEN INC.Inventors: Michael David BARTBERGER, Ana GONZALEZ BUENROSTRO, Hilary Plake BECK, Xiaoqi CHEN, Richard Victor CONNORS, Jeffrey DEIGNAN, Jason DUQUETTE, John EKSTEROWICZ, Benjamin FISHER, Brian Matthew FOX, Jiasheng FU, Zice FU, Felix GONZALEZ LOPEZ DE TURISO, Michael GRIBBLE, JR., Darin James GUSTIN, Julie Anne HEATH, Xin HUANG, Xianyun JIAO, Michael G. JOHNSON, Frank KAYSER, David John KOPECKY, Sujen LAI, Yihong LI, Zhihong LI, Jiwen LIU, Jonathan Dante LOW, Brian Stuart LUCAS, Zhihua MA, Lawrence McGEE, Joel McINTOSH, Dustin McMINN, Julio Cesar MEDINA, Jeffrey Thomas MIHALIC, Steven Howard Olson, Yosup REW, Philip Marley ROVETO, Daqing SUN, Xiaodong WANG, Yingcai WANG, Xuelei YAN, Ming YU, Jiang ZHU
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Publication number: 20110306601Abstract: Antagonists of group 1 metabotropic glutamate receptors (mGluR) potentiate the effect of positive AMPA receptor modulators on neurotrophin expression, such as brain-derived neurotrophic factor (BDNF). The findings described herein suggest a combinatorial approach for drug therapies, using both positive AMPA receptor modulators and mGluR antagonists, to enhance brain neurotrophism.Type: ApplicationFiled: August 19, 2011Publication date: December 15, 2011Applicant: The Regents of the University of CaliforniaInventors: Julie C. Lauterborn, Christine M. Gall, Gary Lynch
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Patent number: 8058264Abstract: Described is a novel combination therapy for diabetes mellitus type I and/or for obesity and its concomitant and/or secondary diseases or conditions, in particular the metabolic syndrome and/or syndrome X, and/or diabetes mellitus type II, by administering a combination of at least one KATP channel opener as a first active agent and at least one CB1 cannabinoid receptor antagonist as a second active agent. The invention is further directed to such novel combination therapy wherein a dually acting compound with combined KATP channel opening and CB1 antagonistic properties is used.Type: GrantFiled: October 25, 2005Date of Patent: November 15, 2011Assignee: Abbott Products GmbHInventors: Michael Firnges, Peter-Colin Gregory, Jochen Antel, Josephus Hubertus Maria Lange, Harald Waldeck
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Publication number: 20110257162Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein m, n, X, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: June 29, 2011Publication date: October 20, 2011Inventors: Vincenzo Summa, Paola Pace, Philip Jones, Alessia Petrocchi, Maria del Rosario Rico Ferreira, Giuseppe Cecere
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Publication number: 20110224155Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.Type: ApplicationFiled: June 3, 2008Publication date: September 15, 2011Applicant: SENOMYX INC.Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Xiaodong Li, Feng Zhang, Guy Servant, Qing Chen, Vincent Darmohusodo, Richard Fine, Joseph R. Fotsing, Jeffrey Robert Hammaker, Xinshan Kang, Rachel D.A. Kimmich, Boris Klebansky, Haitian Liu, Goran Petrovic, Marketa Rinnova, Sara Adamski-Werner, Jeffrey Yamamoto, Hong Zhang, Albert Zlotnik, Mark Zoller, Karen Zoller
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Patent number: 8008287Abstract: Tricyclic compounds, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.Type: GrantFiled: May 16, 2007Date of Patent: August 30, 2011Assignee: Gilead Sciences, Inc.Inventors: Zhenhong R. Cai, Salman Y. Jabri, Haolun Jin, Rachael A. Lansdown, Samuel E. Metobo, Michael R. Mish, Richard M. Pastor
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Publication number: 20110207723Abstract: A compound represented by the general formula (I): a pharmaceutically acceptable salt thereof, or a solvate of the compound or salt has an A? production inhibitory activity or BACE 1 inhibitory activity, and is thus useful as an agent for treating neurodegenerative diseases caused by A? as typified by Alzheimer's disease. In the formula, ring A represents a C6-14 aryl group or the like; L represents —NR1CO— (wherein RL represents a hydrogen atom or the like) or the like; ring B represents a C6-14 aryl group or the like; X represents a C1-3 alkylene group or the like; Y represents a C1-3 alkylene group or the like; Z represents an oxygen atom or the like; R1 and R2 each independently represents a hydrogen atom or the like; and R3, R4, R5 and R6 each independently represents a hydrogen atom, a halogen atom or the like.Type: ApplicationFiled: September 28, 2009Publication date: August 25, 2011Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Takafumi Motoki, Kunitoshi Takeda, Yoichi Kita, Mamoru Takaishi, Yuichi Suzuki, Tasuku Ishida
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Patent number: 7981878Abstract: The present invention describes the use of Notch2 inhibitors for producing a medicament for the treatment of tumours, which tumours are characterized by ligand-independent Notch2 fragments.Type: GrantFiled: June 21, 2006Date of Patent: July 19, 2011Assignee: Medizinische Universitat WienInventors: Rainer Hubmann, Wolfgang Sieghart
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Patent number: 7951800Abstract: The present invention provides HCV polymerase inhibiting compounds having the formula (I): where R1 is cyclobutyl-N(Ra)—, n is 1, 2, 3 or 4, and at least one R5 is RaSO2N(Rj)alkyl-. In a non-limiting example, a compound of the present invention is N-[(3-{1-[(cyclobutyl)amino]-4-hydroxy-2-oxo-1,2-dihydro-quinolin-3-yl}-1,1-dioxo-1,4-dihydro-1?6-thieno[2,3-e][1,2,4]thiadiazin-7-yl)methyl]methanesulfonamide. The present invention also features compositions comprising the compounds of the present invention or pharmaceutically acceptable salts, stereoisomers or tautomers thereof, and methods of using the same to treat or prevent HCV infection.Type: GrantFiled: November 6, 2009Date of Patent: May 31, 2011Assignee: Abbott Laboratories, Inc.Inventors: Rolf Wagner, Pamela L. Donner, Dale J. Kempf, Clarence J. Maring, Vincent S. Stoll
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Publication number: 20110112079Abstract: The invention related to compounds for formula I useful for inhibiting phosphodiesterase-4.Type: ApplicationFiled: January 8, 2009Publication date: May 12, 2011Inventors: Craig J. Thomas, Menghang Xia, Amanda P. Skoumbourdis, Christopher A. LeClair, Ruili Huang, Martin J. Walsh
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BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS
Publication number: 20110110948Abstract: Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.Type: ApplicationFiled: July 15, 2008Publication date: May 12, 2011Applicant: SCHERING CORPORATIONInventors: Thavalakulamgara K. Sasikumar, Duane A. Burnett, Theodros Asberom, Wen-Lian Wu, Hongmei Li, Ruo Xu, Hubert B. Josien -
Publication number: 20110071141Abstract: Condensed-ring aryl compounds of formula (I) and use of the same as a agrochemical for controlling noxious organisms wherein (X)mQ, A, R1, (Y)n and the grouping —W1—W2—W3—W4— are as defined herein.Type: ApplicationFiled: March 13, 2009Publication date: March 24, 2011Inventors: Tetsuya Murata, Yasushi Yoneta, Jun Mihara, Kei Domon, Mamoru Hatazawa, Koichi Araki, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara, Ulrich Görgens, Arnd Voerste, Angela Becker, Eva-Maria Franken, Klaus-Helmut Müller
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Patent number: 7872052Abstract: The present invention relates to heterocyclic inhibitors of stratum corneum chymotryptic enzyme (SCCE). More particularly, the invention relates to the use of compounds with the formula (I) or (II) for treatment of certain diseases, in particular skin diseases such as pruritus, as well as cancer such as ovarian cancer.Type: GrantFiled: June 7, 2004Date of Patent: January 18, 2011Assignee: Arexis ABInventor: Marcel Linschoten
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Publication number: 20100305109Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring G1, X, R1, and R2 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: ApplicationFiled: May 28, 2010Publication date: December 2, 2010Applicant: ABBOTT LABORATORIESInventors: Marc J. Scanio, William H. Bunnelle, William A. Carroll, Sridhar Peddi, Arturo Perez-Medrano, Lei Shi
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Preparation of antimicrobial formulations using 7-oxa-2-thia-1,5-diazabicyclo[3.3.1]nonane-2,2-dione
Patent number: 7820651Abstract: Use of 7-oxa-2-thia-1,5-diazabicyclo[3.3.1]nonane-2,2-dione (“cyclotaurolidin”) for the preparation of antimicrobial formulations, in particular antimicrobial solutions for technical or medical purposes and of aqueous lock solutions for catheters and port systems for preventing infections and sepsis of patients.Type: GrantFiled: February 8, 2007Date of Patent: October 26, 2010Inventors: Claus Herdeis, Christian Edwin Weis -
Publication number: 20100267703Abstract: The present invention relates to novel benzoxathiazine derivatives of the formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to several processes for preparation thereof and to the use thereof as insecticides and/or acaricides in combination with further compositions such as penetrants and/or ammonium or phosphonium salts.Type: ApplicationFiled: December 11, 2009Publication date: October 21, 2010Applicant: BAYER CROPSCIENCE AGInventors: Bernd Alig, Klaus-Helmut Müller, Eva-Maria Franken, Ulrich Görgens, Arnd Voerste
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Publication number: 20100261641Abstract: The present invention relates to a spiro-piperidine compound represented by formula (I): wherein R1 represents hydrogen, an aliphatic hydrocarbon group which may have a substituent(s) or a cyclic group which may have a substituent(s); and ring A represents a 5- to 8-membered cyclic group which may have a substituent(s), a salt thereof, an N-oxide thereof, a quaternary ammonium salt thereof or a solvate thereof, or a prodrug thereof. The compounds represented by formula (I) have chemokine antagonistic action, so that they are useful for prevention and/or treatment of various inflammatory diseases, immune diseases such as autoimmune diseases or allergic diseases, or HIV infection.Type: ApplicationFiled: December 11, 2008Publication date: October 14, 2010Applicant: Ono Pharmaceutical Co., Ltd.Inventors: Rena Nishizawa, Yoshikazu Takaoka, Hiromu Habashita, Shiro Shibayama, Masaya Kokubo
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Publication number: 20100261714Abstract: Compounds of formula (I): wherein R1, R2, A1, A2, A3, A4, X and Y are as defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: April 8, 2010Publication date: October 14, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Claudio STURINO, Patrick DEROY, Martin DUPLESSIS, Paul J. EDWARDS, Anne-Marie FAUCHER, Teddy HALMOS, Clint JAMES, Jean-Eric LACOSTE, Eric MALENFANT, Joannie MINVILLE, Louis MORENCY, Sebastien MORIN, Martin TREMBLAY, Christiane YOAKIM
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Patent number: 7799776Abstract: Inhibitors of indoleamine 2,3-dioxygenase (IDO) are provided as are pharmaceutical compositions containing such inhibitors as well as the use of such inhibitors and compositions for the treatment of a condition in a mammalian subject characterized by pathology of the IDO-mediated tryptophan metabolic pathway. Such conditions may involve suppression of T-cell mediated immune response or may directly result from depletion of tryptophan or accumulation of a product of tryptophan degradation. Specific disease conditions include cataracts, age-related yellowing in the eye, neurodegenerative disorders, mood disorders, cancer and various bacterial/viral infections. IDO inhibitors of this invention are substituted naphthalene and anthracene diones. Novel compounds of this invention include the following taurine-substituted naphthaquinone structure.Type: GrantFiled: July 13, 2005Date of Patent: September 21, 2010Assignee: The University of British ColumbiaInventors: Raymond J. Andersen, Alban Pereira, Xin-Hui Huang, Grant Mauk, Eduardo Vottero, Michel Roberge, Aruna Balgi
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Publication number: 20100234350Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 14, 2009Publication date: September 16, 2010Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-McGuire, Hans-Michael Jantzen, David M. Sedlock
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Publication number: 20100215620Abstract: The present invention relates to a co-culture method of Sphingomonas sp. bacterial strain and Aspergillus sp. fungus strain, in which the novel Sphingomonas sp. bacterial strain KMK-001 is cultured in a liquid medium and the novel Aspergillus sp. strain KMC-901 separately cultured in another liquid medium is added to the above culture solution, a novel glionitrin biosynthesized therefrom and a pharmaceutical composition comprising the said glionitrin or its pharmaceutically acceptable salt as an active ingredient. The glionitrin herein has strong cytotoxic effect on cancer cells and has antibiotic effect on 10 pathogenic bacteria including the novel Sphingomonas sp. bacterial strain KMK-001, so that it can be effectively applied in antibiotics or anti-cancer agents.Type: ApplicationFiled: October 23, 2008Publication date: August 26, 2010Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Hyun Ok Yang, Hak Cheol Kwon, Hyun-Bong Park, Ji-Hye Yoo