Chalcogen Attached Directly To The 1,3-diazole Ring By Nonionic Bonding Patents (Class 546/274.4)
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Publication number: 20120289526Abstract: The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizophrenia, substance abuse disorders, sleep disorders or epilepsy.Type: ApplicationFiled: December 6, 2010Publication date: November 15, 2012Inventors: Giuseppe Alvaro, Anne Décor, Stefano Fontana, Dieter Hamprecht, Charles Large, Agostino Marasco
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Publication number: 20120251551Abstract: The invention relates to substituted (heteroarylmethyl) thiohydantoin compounds of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, and their use for the preparation of medicaments for the treatment and/or prophylaxis of disorders, in particular of prostate cancer.Type: ApplicationFiled: August 28, 2010Publication date: October 4, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ulrich Lücking, Arwed Cleve, Bernard Haendler, Hortensia Faus Gimenez, Silke Köhr, Horst Irlbacher
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Publication number: 20120245153Abstract: Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and use thereof.Type: ApplicationFiled: September 7, 2010Publication date: September 27, 2012Applicant: VANDERBILT UNIVERSITYInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Darren W. Engers, Patrick R. Gentry, Yiu-Yin Cheung, James M. Salovich, Rocco D. Gogliotti
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Patent number: 8268847Abstract: The invention relates to a product containing the compound of formula (I) below or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having PDE5-inhibitory properties, or a pharmaceutically acceptable salt thereof, for therapeutic use, simultaneously, separately or over a period of time, in the treatment of a disease wherein vasoconstriction is involved.Type: GrantFiled: August 28, 2007Date of Patent: September 18, 2012Assignee: Actelion Pharmaceuticals, Ltd.Inventor: Martine Clozel
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Publication number: 20120225910Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 areas described herein.Type: ApplicationFiled: April 23, 2012Publication date: September 6, 2012Applicant: PFIZER INC.Inventors: Jeffrey Allen Pfefferkorn, Meihua Mike Tu
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Publication number: 20120220622Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.Type: ApplicationFiled: November 2, 2010Publication date: August 30, 2012Inventors: Julia Adam, Jonathan Gillespie, Steven Laats, John Kinnaird Ferguson MacLean, Duncan Robert McArthur
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Patent number: 8207155Abstract: In one aspect, the invention relates to compounds which are useful as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: March 31, 2010Date of Patent: June 26, 2012Assignee: Vanderbilt UniversityInventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
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Patent number: 8178513Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W, U, X, R1, R2, R3, and R4 are as defined herein, and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of using such compounds to inhibit aspartyl protease and to treat a variety of disease or disorders, including cardiovascular diseases, cognitive and neurodegenerative diseases.Type: GrantFiled: June 8, 2009Date of Patent: May 15, 2012Assignees: Schering Corporation, Pharmacopeia Drug Discovery Inc.Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey O. Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, Jr., John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X. H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
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Patent number: 8178553Abstract: 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: GrantFiled: January 20, 2010Date of Patent: May 15, 2012Assignee: Schering CorporationInventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Shankar B. Bandarpalle, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta Maria Kosinski, Seong-Heon Kim, De-Yi Yang, Razia K. Rizvi
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Publication number: 20120115894Abstract: The present invention is directed to certain Inidazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.Type: ApplicationFiled: February 22, 2010Publication date: May 10, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Ping Liu, Robert J. DeVita, Linus S. Lin, Marc D. Chioda, Terence G Hamill, Wenping Li
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Publication number: 20120101078Abstract: Disclosed are a series of neuropeptide Y Y5 receptor ligands, and as such are useful to treat disorders related to mood, stress, ADHD, cognition, stress and dementia.Type: ApplicationFiled: March 19, 2010Publication date: April 26, 2012Applicant: H. Lundbrck A/SInventors: Bin Chen, James Ford Burns, Dario Doller
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Patent number: 8153634Abstract: [Object] To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate.Type: GrantFiled: May 29, 2009Date of Patent: April 10, 2012Assignee: Kowa Company, Ltd.Inventors: Yuki Yamaguchi, Minoru Koura, Sayaka Kurobuchi, Takayuki Matsuda, Ayumu Okuda, Hisashi Sumida, Yuichiro Watanabe, Takashi Enomoto, Kimiyuki Shibuya
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Patent number: 8143294Abstract: The invention relates to 2-thio-substituted imidazole derivatives of the Formula I, and to methods of use thereof.Type: GrantFiled: December 31, 2008Date of Patent: March 27, 2012Inventors: Michael Burnet, Stefan Laufer, Pierre Koch
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Publication number: 20120052096Abstract: SOAT-1 inhibitors of general formula (I) and cosmetic and pharmaceutical compositions containing such a compound are described.Type: ApplicationFiled: February 26, 2010Publication date: March 1, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Laurence Dumais, Cédric Poinsard, Thibaud Portal
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Publication number: 20120015980Abstract: The present invention relates to novel anthranilic acid derivatives of the general formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and a plurality of processes for their preparation.Type: ApplicationFiled: June 14, 2011Publication date: January 19, 2012Applicant: BAYER CROPSCIENCE AGInventors: Rüdiger FISCHER, Christoph Grondal, Markus Heil, Heinz-Juergen Wroblowsky, Ernst Rudolf Gesing, Christian Funke, Eva-Maria Franken, Olga Malsam, Arnd Voerste, Ulrich Görgens, Tetsuya Murata
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Publication number: 20120010181Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (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: November 9, 2009Publication date: January 12, 2012Inventors: Joseph A. Kozlowski, Wensheng Yu, Michael K.C. Wong, Seong Heon Kim, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, De-Yi Yang, Robert Feltz, Aneta Maria Kosinski, Guowei Zhou, Razia K. Rizvi, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristen E. Rosner, M. Arshad Siddiqui, Liping Yang
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Publication number: 20110294812Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof, which are inhibitors of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.Type: ApplicationFiled: December 11, 2009Publication date: December 1, 2011Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Simon Christopher Hirst, David Michel Adrien Taddei, Catherine Elisabeth Charron
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Publication number: 20110288054Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: ApplicationFiled: September 22, 2009Publication date: November 24, 2011Applicant: Schering CorporationInventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K.C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
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Publication number: 20110288077Abstract: This invention relates to compounds of the Formula (I)-(IX):, as defined herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? combinations thereof.Type: ApplicationFiled: September 22, 2009Publication date: November 24, 2011Applicant: SCHERING CORPORATIONInventors: Michael K.C. Wong, Wensheng Yu, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Joseph A. Kozlowski, Seong Heon Kim, Guowei Zhou, De-Yi Yang, Razia K. Rizvi, Lei Chen, Aneta Maria Kosinski, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
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Publication number: 20110251208Abstract: The present invention relates to a phosphodiesterase type III (PDE III) inhibitor and/or Ca2+- sensitizing agent or a pharmaceutically acceptable derivative thereof for the treatment of a patient suffering from hypertrophic cardiomyopathy (HCM). According to another aspect the present invention relates to the use of a PDE III inhibitor and/or Ca2+-sensitizing agent for the preparation of a medicament for the treatment of a patient suffering from HCM.Type: ApplicationFiled: November 23, 2009Publication date: October 13, 2011Applicant: BOEHRINGER INGELHEIM VETMEDICA GMBHInventors: Juergen Daemmgen, Olaf Joens
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Patent number: 8034832Abstract: The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: GrantFiled: June 4, 2009Date of Patent: October 11, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Paul Charifson, David Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud LeTiran, Joseph Drumm
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Publication number: 20110219686Abstract: Described are compositions and methods for regulating plant growth that use a complex of an imidazolinone ion and a metal counterion; the compositions and methods include methods of regulation plant growth, optionally in combination with herbicidal, fungicidal, and fertilizer compositions and effects.Type: ApplicationFiled: March 11, 2011Publication date: September 15, 2011Inventor: Volker Heide
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Publication number: 20110224433Abstract: A process for manufacturing 5,6-disubstituted-3-pyridylmethyl ammonium bromides (I), wherein Q is a tertiary aliphatic or cyclic, saturated, partially unsaturated or aromatic amine; Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; Y and Y1 are each independently OR1, NR1R2, or when taken together YY1 is —O—, —S— or NR3—; R1 and R2 are each independently hydrogen, C1-C4 alkyl optionally substituted with C1-C4 alkoxy or phenyl optionally substituted with one to three C1-C4 alkyl groups, C1-C4 alkoxy groups or halogen atoms, or phenyl optionally substituted with one to three C1-C4 alkyl groups, C1-C4 alkoxy groups or halogen atoms; R3 is hydrogen or C1-C4 alkyl; comprises the steps of (i) reacting a compound of formula (II), wherein the symbols have the meaning given in formula (I), with bromine in the presence of a radical initiator in a solvent mixture comprising an aqueous phase and an organic phase, where the organic phase comprises a solvent selected from 1,2-dichloroethane,Type: ApplicationFiled: November 13, 2009Publication date: September 15, 2011Applicant: BASF SEInventors: Joachim Gebhardt, Frederik Menges, Michael Rack, Michael Keil, Jochen Schroeder, Stefan Orsten, Helmut Zech, David Cortes, Robert Leicht, Tony Yegerlehner, Rodney F. Klima
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Publication number: 20110223093Abstract: This invention relates to sulfur functionalized ionic liquid compounds that are useful in methods of carbon dioxide or sulfur dioxide removal to which they may be applied.Type: ApplicationFiled: March 11, 2011Publication date: September 15, 2011Applicant: E.I. DU PONT DE NEMOURS AND COMAPNYInventor: MARK A. SCIALDONE
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Publication number: 20110224439Abstract: A process for manufacturing 5-chloromethyl-2,3-pyridine dicarboxylic acid anhydrides (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; comprising the steps of (i) reacting a compound of formula (II), wherein the symbols have the meaning given in formula (I), with a chlorinating agent, optionally in the presence of a radical initiator in a solvent selected from halogenated hydrocarbons, and (ii) crystallizing the compound (I) formed in step (i) from a solvent selected from chlorobenzene, 1,2-dichlorobenzene, 1,3-dichlorobenzene, 1,4-dichlorobenzene, dichloroethane, trichloromethane, dichloromethane, toluene, xylenes, ethyl acetate, methyl tert.-butyl ether, and mixtures thereof. Compounds (I) are useful intermediates in the synthesis of herbicidal imidazolinones.Type: ApplicationFiled: November 13, 2008Publication date: September 15, 2011Inventors: Frederik Menges, Joachim Gebhardt, Michael Rach, Michael Keil, Rodney F. Klima, David Cortes, Robert Leicht, Helmut Zech, Jochen Schroeder
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Patent number: 8003653Abstract: The present invention is directed to imidazolidinone compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: November 10, 2006Date of Patent: August 23, 2011Assignee: Merck. Sharp & Dohme Corp.Inventors: James C. Barrow, Kenneth E. Rittle, Phung Le Bondiskey
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Publication number: 20110195998Abstract: Disclosed is a compound usable as a pest control agent and has excellent pest control activity. A compound represented by formula (I) has excellent pest control activity. The compound or an agriculturally or horticulturally acceptable salt thereof is thus useful as a pest control agent.Type: ApplicationFiled: November 30, 2007Publication date: August 11, 2011Inventors: Kimihiko Goto, Ryo Horikoshi, Kazuhiko Oyama, Satoshi Omura, Toshiaki Sunazuka
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Patent number: 7994204Abstract: The present invention aims to provide compounds which have an inhibitory effect on the binding between S1P and its receptor Edg-1(S1P1) and which are useful for pharmaceutical purposes. A compound represented by formula (I) or a pharmaceutically acceptable salt thereof: [wherein Ar represents a monocyclic heterocyclic ring containing one or two nitrogen atoms, A represents an oxygen atom or the like, Y1, Y2 and Y3 each represent a carbon atom or a nitrogen atom, R1 represents a hydrogen atom, a C1-C6 alkyl group or the like, R2 represents a C1-C6 alkyl group, a C3-C8 cycloalkyl group or the like, R3 represents a C1-C18 alkyl group or the like, R4 represents a hydrogen atom or a C1-C6 alkyl group, and R5 represents a C1-C10 alkyl group or the like].Type: GrantFiled: February 6, 2007Date of Patent: August 9, 2011Assignee: Taisho Pharmaceutical Co., LtdInventors: Naoya Ono, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Takeshi Koami, Rie Nishikawa
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Publication number: 20110178134Abstract: The invention relates to compounds of formula (I) wherein the groups have stated meanings, and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs and for treating cardiometabolic syndrome.Type: ApplicationFiled: August 6, 2010Publication date: July 21, 2011Applicant: SANOFI-AVENTISInventors: Gerhard JAEHNE, Siegfried STENGELIN, Matthias GOSSEL, Thomas KLABUNDE, Irvin WINKLER, Antony BIGOT, Anita DIU-HERCEND, Gilles TIRABOSCHI
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Publication number: 20110178092Abstract: Described are novel protease inhibitors and methods for using said protease inhibitors in the treatment of human immunodeficiency virus (HIV) infection.Type: ApplicationFiled: December 19, 2007Publication date: July 21, 2011Inventors: Akbar Ali, Michael D. Altman, Saima G. Anjum, Hong Cao, Sripriya Chellappan, Miguel X. Fernandes, Michael K. Gilson, Visvaldas Kairys, Nancy King, Ellen Nalivaika, Moses Prabu, Tariq M. Rana, Kiran Kumar Sai, Celia A. Schiffer, Bruce Tidor
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Publication number: 20110144068Abstract: 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: July 23, 2009Publication date: June 16, 2011Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maurizio Pulici, Fabio Zuccotto, Alessandra Badari, Stefano Nuvoloni, Giovanni Cervi, Gabriella Traquandi, Sonia Biondaro, Paolo Trifiro', Chiara Marchionni, Michele Modugno
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Publication number: 20110135604Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: December 1, 2010Publication date: June 9, 2011Applicant: Gilead Sciences, Inc.Inventors: Anthony Casarez, Mingzhe Ji, Choung U. Kim, Xiaoning C. Sheng, Qiaoyin Wu
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Patent number: 7939523Abstract: Imidazolidinone and imidazolinethione compounds of formula (I): wherein R1, R2, R3, A1, A2, X, Y, Z, m, n, p, x, and y are defined herein. Also disclosed is a method of treating hepatitis C virus infection with these compounds.Type: GrantFiled: January 5, 2009Date of Patent: May 10, 2011Assignee: National Health Research InstitutesInventors: Jyh-Haur Chern, Tsu-An Hsu, Iou-Jiun Kang, Li-Wen Wang, Chung-Chi Lee, Yen-Chun Lee, Yen-Shian Wu, Sheng-Ju Hsu, Yueh Andrew Yueh, Yu-Sheng Chao
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Publication number: 20110105530Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: June 25, 2009Publication date: May 5, 2011Inventors: Natalie Dales, Zaihui Zhang, Jianmin Fu, Duanjie Hou, Shaoyi Sun, Vishnumurthy Kodumuru, Natalia Pokrovskaia
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Publication number: 20110046185Abstract: The invention relates to compounds of formula (I) wherein the groups R and R? A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.Type: ApplicationFiled: August 6, 2010Publication date: February 24, 2011Applicant: SANOFI-AVENTISInventors: Gerhard JAEHNE, Peter BELOW, Siegfried STENGELIN, Matthias GOSSEL, Thomas KLABUNDE, Irvin WINKLER
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Publication number: 20110009637Abstract: The present invention relates to crystals of the Active Pharmaceutical Ingredient (API) Dexlansoprazole, including methods of making the crystals, pharmaceutical compositions comprising the crystals, and methods of treating a patient with the crystals.Type: ApplicationFiled: February 9, 2010Publication date: January 13, 2011Inventors: Dario Braga, Stefano Luca Giaffreda, Marco Curzi
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Publication number: 20110003825Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.Type: ApplicationFiled: August 23, 2010Publication date: January 6, 2011Applicant: Schering CorporationInventors: Ying Huang, Guoqing Li, Andrew W. Stamford
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Publication number: 20100305095Abstract: The present invention relates to, inter alia, the use of a compound capable of inhibiting 4-hydroxyphenylpyruvate dioxygenase (HPPD) in an animal in the manufacture of a medicament for use in the treatment and/or prevention of depression. The invention also provides for the use of a compound capable of inhibiting HPPD in an animal in the manufacture of a medicament for use in the treatment of the withdrawal symptoms associated with an addictive drug which causes dopamine dependant associative learning disorders in said animal. In a particular embodiment said HPPD inhibitor is selected from the group consisting of the compound depicted as compound 1; 2; and 3.22.Type: ApplicationFiled: August 18, 2006Publication date: December 2, 2010Inventors: Kim Zachary Travis, John Posner
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Publication number: 20100286212Abstract: Compounds that are useful in treating or preventing viral infections, such as influenza, are described herein. Further described are compositions made from these compounds and methods for using the compounds and their compositions in treating or preventing viral infections.Type: ApplicationFiled: October 31, 2008Publication date: November 11, 2010Applicant: THE UAB RESEARCH FOUNDATIONInventors: Ming Luo, Zhen Yang
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Patent number: 7825255Abstract: The invention relates to the compounds of formula (I), to a method for producing the same and to the use thereof as medicaments.Type: GrantFiled: February 28, 2002Date of Patent: November 2, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Ulrich Rosentreter, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stásch
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Publication number: 20100274006Abstract: A clathrate compound containing a polymolecular host compound as a host compound and an agricultural chemical active ingredient having a saturated solubility in water at 25° C. of not less than 500 ppm as a guest compound.Type: ApplicationFiled: May 4, 2010Publication date: October 28, 2010Applicant: NIPPON SODA CO., LTDInventors: Natsuki Amanokura, Tetsuya Sahara, Hiroshi Suzuki, Yuichi Maekawa, Kiyoshi Katsuura, Yoshihiro Enomoto
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Publication number: 20100261696Abstract: In one aspect, the invention relates to compounds which are useful as as inhibitors of glycine type 1 transporter (G1yT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (G1yT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: March 31, 2010Publication date: October 14, 2010Inventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
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Publication number: 20100240656Abstract: The invention provides novel compounds of formula (I) wherein: one of the a, b, c or d members is a nitrogen atom and the remaining members are carbon atoms; and R3 is a radical selected from the group consisting of: —S—R14 and —CH2—R15. The compounds of formula (I) are useful for treating diseases mediated by a heat shock protein 90 (Hsp 90).Type: ApplicationFiled: July 9, 2008Publication date: September 23, 2010Applicant: ORYZON GENOMICS, S.A.Inventors: Marc Martinell Pedemonte, Isabel Navarro Muñoz, Montserrat Soler López, David Mormeneo Julián, Malgorzata Rosol, Amadeo Llebaria Soldevila, Juan Aymami Bofarull
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Publication number: 20100233116Abstract: The present invention provides heterocyclic derivatives hat modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: August 13, 2007Publication date: September 16, 2010Inventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Rajender Kamboj, Vishnumurthy Kodumuru, Shifeng Liu, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
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Publication number: 20100216855Abstract: Imidazolone derivatives, as medicaments, of formula wherein: R1?H, C1 to C5 alkyl, aryl or a 5- or 6-membered heterocyclic group; Ar1=optionally substituted aryl or an aromatic heterocycle; R?R2—S—, R3—HN—, R4COHN or Ar2, with R2=a C1-C5 alkyl, vinyl or vinyl(C1-C5)alkyl, nitrile or nitrile(C1-C5)alkyl, aryl or benzyl radical, which are optionally substituted; R3=the meanings given above and H; Ar2=substituted or unsubstituted aryl.Type: ApplicationFiled: August 1, 2008Publication date: August 26, 2010Inventors: Francois Carreaux, Jean-Pierre Bazureau, Steven Renault, Laurent Meijer, Olivier Lozach
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Publication number: 20100168106Abstract: The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tanglesType: ApplicationFiled: March 8, 2010Publication date: July 1, 2010Applicant: Wyeth LLCInventors: Michael Sotirios Malamas, Ping Zhou, William Floyd Fobare, William Ronald Solvibile, Iwan Suwandi Gunawan, James Joseph Erdei, Yinfa Yan, Patrick Michael Andrae, Dominick Anthony Quagliato
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Publication number: 20100120838Abstract: 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: January 20, 2010Publication date: May 13, 2010Inventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Shankar B. Bandarpalle, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta M. Micula, Seong Heon Kim, De-Yi Yang, Razia Rizvi
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Patent number: 7705030Abstract: The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.Type: GrantFiled: July 28, 2008Date of Patent: April 27, 2010Assignee: Wyeth LLCInventors: Michael Sotirios Malamas, Ping Zhou, William Floyd Fobare, William Ronald Solvibile, Iwan Suwandi Gunawan, James Joseph Erdei, Yinfa Yan, Patrick Michael Andrae, Dominick Anthony Quagliato
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Patent number: 7700602Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated ?-amyloid deposits or ?-amyloid levels in a patient.Type: GrantFiled: December 10, 2008Date of Patent: April 20, 2010Assignee: Wyeth LLCInventors: Michael S. Malamas, James J. Erdei, Iwan S. Gunawan, Ping Zhou, Yinfa Yan, Dominic A. Quagliato
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Patent number: 7696226Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: December 10, 2004Date of Patent: April 13, 2010Assignee: Abbott LaboratoriesInventors: John T. Randolph, Hui-Ju Chen, David A. DeGoey, Charles A. Flentge, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Douglas K. Hutchinson, Dale J. Kempf, Larry L. Klein, Ming C. Yeung