1,3-oxazoles (including Hydrogenated) Patents (Class 514/374)
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Publication number: 20110183947Abstract: The invention provides a series of -?ketoheterocyclic compounds, for example, compounds of formula (I). The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula (I), useful intermediates for the preparation of compounds of formula (I), and methods of using compounds of formula (I) and compositions thereof.Type: ApplicationFiled: July 8, 2009Publication date: July 28, 2011Applicant: THE SCRIPPS RESEARCH INSTITUTEInventor: Dale L. Boger
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Publication number: 20110183964Abstract: The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, Y, Z, and are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of using compounds of Formula I in treating, inhibiting, or preventing pathologic conditions or disorders mediated wholly or in part by deacetylases.Type: ApplicationFiled: April 8, 2011Publication date: July 28, 2011Applicant: NOVARTIS AGInventors: Michael SHULTZ, Christine Hiu-Tung CHEN, Young Shin CHO, Lei JIANG, Jianmei FAN, Gang LIU, Dyuti MAJUMDAR, Jianke LI
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Publication number: 20110178123Abstract: Novel compounds and compositions for treating patients in need of relief from HIV, AIDS, and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described.Type: ApplicationFiled: July 1, 2009Publication date: July 21, 2011Applicant: PURDUE RESEARCH FOUNDATIONInventor: Arun K. Ghosh
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Publication number: 20110178075Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the ?7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: March 7, 2011Publication date: July 21, 2011Inventors: Wenge XIE, Brian Herbert, Jianguo Ma, Truc Minh Nguyen, Richard Schumacher, Carla Maria Gauss, Ashok Tehim
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Patent number: 7981913Abstract: There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.Type: GrantFiled: May 14, 2010Date of Patent: July 19, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Lorin A. Thompson, III, Kenneth M. Boy, Jianliang Shi, John E. Macor
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Patent number: 7981911Abstract: Improved pharmaceutical compositions are provided comprising one or more solubilized HIV protease inhibiting compounds having improved solubility properties in a medium and/or long chain fatty acid, or mixtures thereof, a pharmaceutically acceptable alcohol, and water.Type: GrantFiled: July 31, 2008Date of Patent: July 19, 2011Assignee: Abbott LaboratoriesInventors: Laman Alani, Soumojeet Ghosh
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Patent number: 7977362Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, methods for using the compounds and processes for making the compounds. More specifically, the disclosure relates to alpha-(N-benzenesulfonamido)cycloalkyl compounds that may inhibit one or both of: (i) the functioning of a ?-secretase enzyme; or (ii) the production of ?-amyloid. Such compounds may be beneficial in the treatment of Alzheimer's disease and other conditions. Representative compounds have the following formula I: wherein: A, R1, and R2 are described herein.Type: GrantFiled: March 17, 2010Date of Patent: July 12, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Dalton King, Zhaoxing Meng, Ivar M. McDonald, Richard E. Olson, John E. Macor
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Patent number: 7977332Abstract: Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re, Rf, Rg, Rh, R5, d, e, U, V, X, WR6 and R7 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: December 2, 2004Date of Patent: July 12, 2011Assignee: FMC CorporationInventors: David M. Roush, John F. Chiarello, Jianming Yu, Benjamin J. Dugan, George Theodoridis, Manorama M. Patel, Walter H. Yeager, Steven W. Szczepanski
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Publication number: 20110166060Abstract: The present invention provides compositions and methods for noninvasive delivery of therapeutic agents across an intact tympanic membrane. For example, the compositions include a penetration enhancer which increases the flux of a therapeutic agent (e.g., antibiotic) across the tympanic membrane. Such compositions are particularly useful in the treatment of otitis media. Additionally, the composition may include a sustained release agents that, in some embodiments form sustained release reservoirs, in situ, once administered to a patient.Type: ApplicationFiled: May 19, 2009Publication date: July 7, 2011Applicants: Massachusettes Institute of Technology, Children's Medical Center CorporationInventors: Emmanuel John Simons, Todd R. Hoare, Daniel S. Kohane, Robert S. Langer
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Publication number: 20110166157Abstract: The present invention relates to 2-(substituted sulphur, sulphone or sulphoxide)-3-(substituted phenyl)propionic acid derivatives, 2-(substituted oxygen)-3-(substituted phenyl)propionic acid derivatives, benzoic acid derivatives, and derivatives of 2-methyl-2-(phenoxy or phenylthio)propanoic acid and 2-(methyl or ethyl)-2-(phenoxy or phenylthio)butanoic acid, to processes for preparing such compounds, to their use in the treatment of inflammatory conditions, and to pharmaceutical compositions containing them.Type: ApplicationFiled: March 11, 2011Publication date: July 7, 2011Applicant: ALBIREO ABInventors: Anders Broo, Johan Gottfries, Michael Kossenjans, Li Lanna, Eva-Lotte Lindstedt-Alstermark, Kristina A. Nilsson, Bengt Ohlsson, Maria Thorstensson, Maria Boije, Per Olof Sjögren
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Publication number: 20110160176Abstract: The invention relates to compounds of the formula (I) wherein n is 0, 1 or 2; G is CH2 or CHR3; R1 is H, C,-C6-alkyl, C,-C6-alkyl substituted by C3-C6-cycloalkyl, C1-C6-hydroxyalkyl, fluorinated C,-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6 alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; R2, R3 and R4 are, independently of each other, H, methyl, fluoromethyl, difluoromethyl, or trifluoromethyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1-C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2Type: ApplicationFiled: August 25, 2010Publication date: June 30, 2011Applicant: Abbott GmbH & Co. KGInventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel, Christophe Henry, Gisela Backfisch, Armin Beyerbach, Wilfried Lubisch
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Publication number: 20110160255Abstract: Invented are novel hetero-pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: June 24, 2009Publication date: June 30, 2011Inventors: Meagan B. Rouse, Mark A. Seefeld
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Publication number: 20110158983Abstract: In alternative embodiments, this invention provides compositions and methods for treating cancer or any condition caused by dysfunctional cells, side effects from treatments for cancer or any condition caused by dysfunctional cells, e.g., mucositis therapies (e.g., for oral mucositis; digestive mucositis; esophageal mucositis; intestinal mucositis). In alternative embodiments, the invention provides cytoprotection products that may be used either alone or in combination with other medical therapies such as cancer chemotherapies and radiation therapies.Type: ApplicationFiled: March 5, 2009Publication date: June 30, 2011Inventors: Newell Bascomb, John Maki, Fredric S. Young
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Patent number: 7968572Abstract: It is intended to provide a compound represented by the formula (I): wherein all the symbols are as defined in the description; which has a p38 MAP kinase inhibitory activity, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. The compound of the invention is useful for preventing or treating a disease in which the abnormal production of a cytokine such as an inflammatory cytokine or a chemokine or overreaction to them is considered to be involved in the cause and aggravation of pathological conditions, in other words, an inflammatory disease, a respiratory disease, a cardiovascular disease, a central nervous system disease or the like, which is a cytokine-mediated disease.Type: GrantFiled: October 2, 2006Date of Patent: June 28, 2011Assignee: Ono Pharmaceuticals Co., Ltd.Inventors: Hisao Nakai, Shingo Yamamoto, Shingo Nakatani, Tomomi Hirosaki
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Publication number: 20110152331Abstract: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.Type: ApplicationFiled: February 25, 2011Publication date: June 23, 2011Inventors: Derek B. Lowe, Philip L. Wickens, Xin Ma, Mingbao Zhang, William H. Bullock, Philip D. G. Coish, Ingo A. Mugge, Andreas Stolle, Ming Wang, Yamin Wang, Chengzhi Zhang, Hai-Jun Zhang, Lei Zhu, Manami Tsutsumi, James N. Livingston
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ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Publication number: 20110152290Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: November 4, 2010Publication date: June 23, 2011Applicant: SANOFI-AVENTISInventors: Matthias SCHAEFER, Josef PERNERSTORFER, Dieter KADEREIT, Hartmut STROBEL, Werngard CZECHTIZKY, L. Charlie CHEN, Alena SAFAROVA, Aleksandra WEICHSEL, Marcel PATEK -
Publication number: 20110151024Abstract: The present invention relates to compositions and methods for preventing migraines. The migraine prophylaxis composition is a single dosage form comprising at least one form of elemental magnesium and at least one NSAID. The prophylaxis composition, comprising at least one form of elemental magnesium and a therapeutically effective concentration of acetylsalicylic acid may also provide cardiac protection and prevent cardiovascular diseases.Type: ApplicationFiled: March 1, 2011Publication date: June 23, 2011Inventor: Alexander Mauskop
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Publication number: 20110152330Abstract: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.Type: ApplicationFiled: February 25, 2011Publication date: June 23, 2011Inventors: Derek B. Lowe, Philip L. Wickens, Xin Ma, Mingbao Zhang, William H. Bullock, Philip D. G. Coish, Ingo A. Mugge, Andreas Stolle, Ming Wang, Yamin Wang, Chengzhi Zhang, Hai-Jun Zhang, Lei Zhu, Manami Tsutsumi, James N. Livingston
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Patent number: 7964622Abstract: This invention is directed to indole acetic acid derivatives and their use in pharmaceutical compositions for the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic disease. The invention is also directed to intermediates useful in preparation of indole acetic derivatives and to methods of preparation.Type: GrantFiled: July 23, 2009Date of Patent: June 21, 2011Assignee: Bayer Healthcare LLCInventors: Xin Ma, Louis-David Cantin, Soongyu Choi, Roger Clark, Martin Hentemann, Joachim Rudolph, Rico Lavoie, Zhonghua Zhang
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Publication number: 20110144153Abstract: [Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided. [Solving Means] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic activity, and confirmed that the amide compound of the present invention has an EP4 receptor antagonistic activity, thereby completing the present invention. The amide compound of the present invention has an EP4 receptor antagonistic activity, and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating various EP4-related diseases, for example, chronic renal failure and/or diabetic nephropathy, and the like.Type: ApplicationFiled: May 12, 2009Publication date: June 16, 2011Applicant: Astellas Pharma Inc.Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo, Susumu Watanuki, Michihito Kageyama
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Publication number: 20110144096Abstract: Novel compounds and methods for activating the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing four six-membered rings and a substituted or unsubstituted C5 or C6 heteroaryl or hetero-cycloalkyl ring and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods and compounds for the treatment of disorders including neurologic, neuropsychiatric, and metabolic disorders are provided. For example, a method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of the described compounds.Type: ApplicationFiled: July 28, 2009Publication date: June 16, 2011Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
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Publication number: 20110144168Abstract: The present invention provides therapeutically active oxazolidine derivatives and compositions as NMDA antagonists, which are useful in preventing and treating central nervous system disorders by inhibiting over-activation of NMDA receptors. In one aspect, the present invention provides methods of treating and/or preventing neurodegenerative diseases and neuropathological disorders, methods of providing neuroprotection under stress conditions such as a stroke, and methods of enhancing the brain's cognitive functions in mammals and humans. For example, the compounds can prevent glutamate-induced neuro-toxicity by inhibiting the activities of the NMDA receptor in the presence of toxic doses of NMDA. In addition, the compounds can potentiate the calcium current in the presence of low dose of NMDA.Type: ApplicationFiled: January 16, 2009Publication date: June 16, 2011Applicant: Biotechnology Research Corporation LimitedInventors: Nancy Yuk-Yu Ip, Hua-Jie Zhu, Fanny Chui-Fun Ip
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Publication number: 20110144057Abstract: The present invention is directed to compounds of formula (I) wherein variables W, X, Y, D, A, n, R1, R2 and R9 are as defined in the description.Type: ApplicationFiled: February 8, 2011Publication date: June 16, 2011Applicant: ABBOTT LABORATORIESInventors: Arthur Gomtsyan, Richard J. Perner, John R. Koenig, Margaret Chi-Ping Hsu, Dilinie P. Fernando, Chih-Hung Lee
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Publication number: 20110144123Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: October 27, 2010Publication date: June 16, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Mark Thomas Miller, Sara S. Hadida Ruah, Peter Diederik Jan Grootenhuis, Matthew Hamilton
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Patent number: 7960381Abstract: A compound comprising or a pharmaceutically acceptable salt, prodrug, or a metabolite thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.Type: GrantFiled: January 29, 2008Date of Patent: June 14, 2011Assignee: Allergan, Inc.Inventors: David W. Old, Wha-Bin Im
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Publication number: 20110135691Abstract: The present invention is directed to immune adjuvants containing IAP inhibitors, including Smac mimetics. The invention further provides pharmaceutical compositions and vaccines containing an IAP inhibitor and an antigen. Methods of enhancing an immune response by administration of an IAP inhibitor, methods of treating or preventing cancer, methods of treating or preventing infections, methods of treating autoimmune disorders, and methods of potentiating cytokine or antibody production are also provided.Type: ApplicationFiled: May 14, 2009Publication date: June 9, 2011Inventors: Leigh Zawel, Christopher S. Straub, Brant G. Firestone, Glenn Dranoff, Michael Dougan
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Publication number: 20110136735Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 30, 2010Publication date: June 9, 2011Inventors: David BARNES, Gregory Raymond BEBERNITZ, Scott Louis COHEN, Robert Edson DAMON, Robert Francis DAY, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, Herbert Franz SCHUSTER, Wei ZHANG
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Patent number: 7956055Abstract: A compound having the formula or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. Y, A, U, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.Type: GrantFiled: March 20, 2009Date of Patent: June 7, 2011Assignee: Allergan, Inc.Inventor: David W. Old
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Patent number: 7956077Abstract: The present invention comprises compounds and compositions for the treatment of metabolic disorders and more particularly, those insulin-related metabolic disorders of the blood such as hyperlipidemia, diabetes, insulin-resistence and the like comprising acetic acid derivatives with cyclohexylmethoxy substituents and their salts. Known as peroxisome proliferator-activated receptors (PPAR) agonists/antagonists, the invention relates to compounds of formula I wherein the various substituent R-groups are more specifically defined herein.Type: GrantFiled: February 6, 2007Date of Patent: June 7, 2011Assignee: Sanofi-Aventis Deutschland GmbHInventors: Heiner Glombik, Christian Stapper, Eugen Falk, Stefanie Keil, Hans-Ludwig Schaefer, Wolfgang Wendler, Stephanie Knieps
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Publication number: 20110130390Abstract: The invention concerns the use of a COX-2 inhibitor for the treatment of psychiatric disorders such as schizophrenia, delusional disorders, affective disorders, autism or tic disorders, in particular chronic schizophrenic psychoses and schizoaffective psychoses, temporary acute psychotic disorders, depressive episodes, recurring depressive episodes, manic episodes and bipolar affective disorders. Moreover, the invention is concerned with the use of a COX-2 inhibitor, in particular celecoxib, in combination with a neuroleptic drug, in particular risperidone, or an antidepressant, for the treatment of psychiatric disorders such as schizophrenia, delusional disorders, affective disorders, autism or tic disorders.Type: ApplicationFiled: January 3, 2011Publication date: June 2, 2011Inventor: Norbert Müller
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Publication number: 20110130400Abstract: The present invention relates to diazabicyclo[2.2.1]hept-2-yl analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.Type: ApplicationFiled: July 24, 2009Publication date: June 2, 2011Inventors: Michael Jonathan Bury, Mui Cheung, Hilary Schenck Eidam, Ryan Michael Fox, Krista Goodman, Eric Steven Manas
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Publication number: 20110130426Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).Type: ApplicationFiled: October 26, 2005Publication date: June 2, 2011Applicant: ASTRAZENECA ABInventors: Håkan Bladh, Krister Henriksson, Vijaykumar Hulikal, Matti Lepistö
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Patent number: 7947719Abstract: The present invention relates to a novel group of compounds having antibiotic, antifungal and/or cytostatic properties, which are obtainable from myxobacteria, especially of the genus Sorangium, preferably Sorangium cellulosum.Type: GrantFiled: July 13, 2006Date of Patent: May 24, 2011Assignee: Hemholtz-Zentrum fur Infektionsforschung GmbHInventors: Herbert Irschik, Rolf Jansen, Florenz Sasse
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Patent number: 7947713Abstract: The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.Type: GrantFiled: October 30, 2007Date of Patent: May 24, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Henry Joseph Breslin, Hans Louis Jos De Winter, Michael Joseph Kukla
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Patent number: 7947675Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.Type: GrantFiled: February 16, 2006Date of Patent: May 24, 2011Assignee: Merck Patent GmbHInventors: Bruno Roux, Isabelle Berard
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Patent number: 7947683Abstract: The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.Type: GrantFiled: April 12, 2006Date of Patent: May 24, 2011Assignee: Glaxo Group LimtedInventors: Giorgio Bonanomi, Anna Checchia, Elettra Fazzolari, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Silvia Terreni
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Publication number: 20110118250Abstract: 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, 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: October 21, 2010Publication date: May 19, 2011Applicant: Amgen Inc.Inventors: Brian K. Albrecht, Denise Lyn Andersen, Michael Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Stephen Hitchcock, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig Masse, Holger Monenschein, Thomas Nguyen, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang, Wenge Zhong
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Publication number: 20110118303Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.Type: ApplicationFiled: April 9, 2009Publication date: May 19, 2011Applicants: EMS S.A., Universidade Estadual Paulista Julio De Mesquita Filho - UNESPInventors: Ednir de Oliveira Vizioli, Chung Man Chin, Renato Farina Menegon, Lorena Blau, Jean Leandro Dos Santos, Maria do Carmo Longo
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Publication number: 20110118274Abstract: The present invention relates to proteasome inhibitors and their use in methods of treating a subject for a pathogen infection or cancer. The methods involve administering to the subject a compound of Formula (I). (I) where: Q is Formula or Formula, where the crossing dashed line illustrates the bond formed joining Q to the rest of the compound of Formula (I). The remainder of substituents of the compound of Formula (I) are defined in the present application.Type: ApplicationFiled: August 25, 2008Publication date: May 19, 2011Applicant: CORNELL RESEARCH FOUNDATION, INC.Inventors: Carl Nathan, Gang Lin
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Patent number: 7943593Abstract: The present invention relates to compositions comprising an apoptosis inducing anti-cancer agent and an IMPDH inhibitor. This invention also relates to methods for inducing apoptosis and for treating tumors and cancers in mammals.Type: GrantFiled: December 4, 2003Date of Patent: May 17, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jugnu Jain-Pandey, Robert J. Fram
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Publication number: 20110105447Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.Type: ApplicationFiled: October 6, 2010Publication date: May 5, 2011Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Gayatri S. Merikapudi, Swaroop Kumar V.S. Vakkalanka
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Publication number: 20110104305Abstract: Methods for therapy of cystic fibrosis and other conditions such as cancer are provided. The methods comprise one or more agents capable of increasing thiol-containing compound transport via a transporter system (i.e. ABC transporters such as MDR-1 or MRP-2) in cells. Other embodiments include the use of agents to modulate transport of thiol-containing compounds within the cell. Therapeutic methods involve the administration of such agents to a patient afflicted with cystic fibrosis, cancer and/or another condition responsive to stimulation of thiol-containing compound transport.Type: ApplicationFiled: June 30, 2010Publication date: May 5, 2011Inventors: Brian J. DAY, Remy KACHADOURIAN
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Publication number: 20110105440Abstract: The present invention is directed to hexahydrocyclopentylf]indazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: February 24, 2009Publication date: May 5, 2011Inventors: William P. Dankulich, Mildred L. Kaufman, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
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Publication number: 20110105460Abstract: [Problem] A compound, which can be used for preventing or treating diseases, in which 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11?-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.Type: ApplicationFiled: July 2, 2009Publication date: May 5, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Seiji Yoshimura, Noriyuki Kawano, Tomoaki Kawano, Daisuke Sasuga, Takanori Koike, Hideyuki Watanabe, Hiroki Fukudome, Nobuyuki Shiraishi, Ryosuke Munakata, Hiroaki Hoshii, Kayoko Mihara
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Publication number: 20110105567Abstract: Disclosed herein are compounds represented by: therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: August 21, 2008Publication date: May 5, 2011Applicant: Allergan, Inc.Inventors: Richard L. Beard, Hiaqing Yuan, John E. Donello, Ken Chow, Liming Wang
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Patent number: 7935701Abstract: Microbicidal composition for product preservation, including a microbicidal composition which comprises a) at least one formaldehyde donor compound and b) at least one antioxidant chosen from gallic esters, phenol derivatives, L-ascorbic acid, and salts and derivatives thereof, and tocopherols and derivatives thereof, and to the use thereof for the preservation of technical products, for example fuels and lubricants.Type: GrantFiled: June 1, 2006Date of Patent: May 3, 2011Assignee: Air Liquide Sante (International)Inventors: Ralf Gradtke, Wolfgang Beilfuss, Klaus Weber, Wolfgang Siegert
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Publication number: 20110098221Abstract: Invented are novel hetero-pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: June 24, 2009Publication date: April 28, 2011Inventors: Hong Lin, Meagan B. Rouse, Mark A. Seefeld, Ren Xie
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Publication number: 20110092423Abstract: Invented are novel hetero-pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: June 24, 2009Publication date: April 21, 2011Inventors: Meagan B. Rouse, Mark A. Seefeld
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Publication number: 20110092524Abstract: The invention relates to a pharmacological action of a compound which functions as a PPAR? agonist on the barrier function of the corneal epithelium. A PPAR? agonist such as rivoglitazone, DRF-2593, GW-544 or BMS-298585 exhibits an excellent effect of enhancing the corneal epithelial barrier function in a test for enhancement of corneal epithelial barrier function, and therefore is useful as a preventive agent or a therapeutic agent for ocular infection or ocular unidentified complaint caused by a decrease in the corneal epithelial barrier function. Further, the PPAR? agonist can enhance the corneal epithelial barrier function of diabetic patients, patients with decreased corneal epithelial barrier function due to aging and patients who underwent refractive surgery such as PRK (photorefractive keratectomy) or LASIK (laser in situ keratomileusis) or cataract surgery.Type: ApplicationFiled: February 25, 2009Publication date: April 21, 2011Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Shin-ichiro Hirai, Atsushi Yoshida
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Publication number: 20110092517Abstract: Provided herein are methods for treatment, prevention, or amelioration of one or more symptoms of a disease or condition related to disorders of insulin and/or glucose metabolism, inflammatory conditions, mitochondrial disease, muscle disorders, or pulmonary disorders, involving administering a PPAR? agonist or a pharmaceutical composition comprising a PPAR? agonist. In one embodiment, the disease or condition is selected from myopathy, inflammatory vascular diseases, Parkinson's and Alzheimer's diseases, systemic inflammatory disorders, renal ischemia, inflammatory rheumatic disorders, and inflammatory diseases of the lung. In another embodiment, methods for increasing oxidative muscle fibers, reducing mitochondria disease, decreasing insulin resistance, decreasing plasma glucose, or decreasing weight, involving administering a PPAR? agonist or a pharmaceutical composition comprising a PPAR? agonist, are provided.Type: ApplicationFiled: August 13, 2010Publication date: April 21, 2011Inventors: Ronald Barbaras, Daniela Carmen Oniciu, Jean-Louis H. Dasseux, Robert A. Scott, John R. Wetterau