Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
Type:
Grant
Filed:
February 7, 2011
Date of Patent:
March 27, 2012
Assignee:
Board of Regents, The University of Texas System
Inventors:
Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
Abstract: Disclosed are N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives having the following formula: wherein m, n, Het, R1, R2 and R3 are as defined herein, and their use as orexin antagonists.
Type:
Grant
Filed:
November 30, 2009
Date of Patent:
March 13, 2012
Assignee:
Glaxo Group Limited
Inventors:
Giuseppe Alvaro, David Amantini, Emiliano Castiglioni, Romano Di Fabio, Francesca Pavone
Abstract: The invention relates to novel dendritic molecules and methods of making them. The dendritic molecules comprise arms, each of which arms is a polymer. The dendritic molecules can be synthesised by way of a reasonably small number of versatile and reliable step-wise reactions, especially click chemistry reactions. Chemical and structural heterogeneity is possible in the dendritic molecule. The invention also provides for surface and interior functionalisation of the molecule.
Type:
Application
Filed:
April 24, 2009
Publication date:
March 8, 2012
Applicant:
THE UNIVERSITY OF QUEENSLAND
Inventors:
Michael John Monteiro, Michael Raymond Whittaker, Craig Andrew Bell, Carl N. Urbani, Daria Eden Lonsdale
Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, and Z are as defined herein, are useful for treating flaviviridae viral infections.
Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting an organic azide and a terminal alkyne with a source of reactive Cu(I) ion for a time sufficient to form by cycloaddition a 1,4-disubstituted 1,2,3-triazole. The source of reactive Cu(I) ion can be, for example, a Cu(I) salt or copper metal. The process is preferably carried out in a solvent, such as an aqueous alcohol. Optionally, the process can be performed in a solvent that comprises a ligand for Cu(I) and an amine.
Type:
Grant
Filed:
July 26, 2010
Date of Patent:
March 6, 2012
Assignee:
The Scripps Research Institute
Inventors:
K. Barry Sharpless, Valery Fokin, Vsevold V. Rostovtsev, Luke Green, Fahmi Himo
Abstract: The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.
Type:
Application
Filed:
April 22, 2010
Publication date:
March 1, 2012
Inventors:
David George Allen, Diane Mary Coe, Anthony William James Cooper, Paul Martin Gore, David House, Stefan Senger, Steven Leslie Sollis, Sadie Vile, Caroline Wilson
Abstract: The present technology discloses biotinidase assay, biotinidase substrates (I) and a kit wherein the biotinidase substrate includes a label molecule separated from the biotin carbamoyl group by a linker X longer than about 4 ? but shorter than about 27 ?.
Type:
Application
Filed:
March 10, 2010
Publication date:
February 23, 2012
Applicant:
Joachim Ngiamas trustee for Joachim Ngiam Trust Fund ABN
Inventors:
Jarkko Karvinen, Pertti Hurskainen, Pekka Mattsson, Outi Mulari, Jari Peuralahti, Lassi Jaakkola
Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).
Type:
Grant
Filed:
October 27, 2010
Date of Patent:
February 21, 2012
Assignee:
Pfizer Inc.
Inventors:
Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukui, Ru Zhou
Abstract: The present invention provides novel functionalized mixtures 4- and 5-vinyl substituted regioisomers of 1,2,3-triazoles via 1,3-dipolar cycloaddition. Functionalized alkyne moieties with a terminal alcoholic functionality are reacted with functionalized organic moieties with a terminal leaving group and an azide to provide an alcoholic functionalized mixture of 4- and 5-substituted regioisomers of 1,2,3-triazole moieties. The mixture may be converted to a wide variety of useful functionalized mixtures of 4- and 5-vinyl substituted regioisomers of 1,2,3-triazole moieties, which in turn can be converted to a wide variety of useful polymers The novel alcoholic functionalized mixtures of 4- and 5-substituted regioisomers can be separated by chromatography to provide the purified 4- and 5-alcoholic functionalized substituted 1,2,3-triazole moieties. The novel compounds of the invention can be employed in a wide variety of compositions (Formulae (I), (II)); wherein R1, R2, R3, and R4, are defined herein.
Abstract: 1,4-disubstituted-1,2,3-triazole UV absorbing monomers are disclosed. The UV absorbers are particularly suitable for use in intraocular lens materials.
Abstract: The present invention relates to amide compounds, processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing these compounds and to their use in therapy.
Type:
Application
Filed:
April 22, 2010
Publication date:
February 9, 2012
Inventors:
Diane Mary Coe, Anthony William James Cooper, Paul Martin Gore, David House, Stefan Senger, Sadie Vile
Abstract: There is provided compounds of formula I, wherein Y, ring A, D1, D2a, D2b, D3, L1, Y1, L2 and Y2 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
Type:
Application
Filed:
March 12, 2010
Publication date:
February 9, 2012
Applicant:
BIOLIPOX AB
Inventors:
Peter Nilsson, Benjamin Pelcman, Martins Katkevics, Edgars Suna, Ilya Popovs
Abstract: This invention relates to novel 1,2,3-triazole derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
Type:
Grant
Filed:
August 6, 2008
Date of Patent:
February 7, 2012
Assignee:
Neurosearch A/S
Inventors:
Antonio Nardi, Jeppe Kejser Christensen, Dan Peters, Gunnar M. Olsen, Tino Dyhring
Abstract: A process for the manufacture of a functional (per)fluoropolyether derivative comprising at least one triazole group, such process comprising: (1) reacting a (per)fluoropolyether hydroxyl derivative having at least one hydroxyl group [derivative (PFPE-OH)] with an activating agent, to yield an activated (per)fluoropolyether hydroxyl derivative comprising at least one activated hydroxyl group [derivative (a-PFPE-OH)]; (2) reacting said activated (per)fluoropolyether hydroxyl derivative [derivative (a-PFPE-OH)] with at least one azide salt to yield a functional (per)fluoropolyether derivative comprising at least one azido group [derivative (PFPE-N3)]; and (3) reacting said functional (per)fluoropolyether derivative comprising at least one azido group [derivative (PFPE-N3)] with a hydrocarbon compound having a terminal alkyne group to yield a functional (per)fluoropolyether derivative comprising at least one triazole group [derivative (PFPE-azole)].
Type:
Application
Filed:
April 2, 2010
Publication date:
February 2, 2012
Applicant:
SOLVAY SOLEXIS S.P.A.
Inventors:
Prakash Wadgaonkar, Shamal Menon, Claudio Adolfo Pietro Tonelli
Abstract: Disclosed are near IR emitting fluorescent compounds; methods of making and kits containing the described compounds; and their use in fluorescence-based detection of biological materials.
Type:
Application
Filed:
October 20, 2009
Publication date:
February 2, 2012
Applicant:
LIFE TECHNOLOGIES CORPORATION
Inventors:
Stephen Yue, Shih-Jung Huang, Jolene Bradford
Abstract: A clickable cross-linker compound provides an easily scanned reporter ion for effective and efficient cross-linking and identification of intermolecular and intramolecular interactions of proteins and peptides.
Abstract: Compounds of formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.
Type:
Grant
Filed:
May 22, 2007
Date of Patent:
January 31, 2012
Assignee:
Eli Lilly and Company
Inventors:
Michael Gregory Bell, Robert Anthony Doti, Matthew Scott Dowling, Michael James Genin, Peter Ambrose Lander, Tianwei Ma, Nathan Bryan Mantlo, Jason Matthew Ochoada, Lindsay Scott Stelzer, Ryan Edward Stites, Alan M Warshawsky
Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
Type:
Application
Filed:
October 4, 2011
Publication date:
January 26, 2012
Inventors:
Zachary Demko, Christopher Borella, Shoujun Chen, Lijun Sun
Abstract: Prostate-specific membrane antigen (PSMA) targeting compounds are described. Uses of the compounds for imaging, therapy, cell sorting, and tumor mapping are also described.
Type:
Application
Filed:
March 19, 2010
Publication date:
January 12, 2012
Applicant:
The Johns Hopkins University
Inventors:
Martin Pomper, Ronnie Charles Mease, Ray Sangeeta, Ying Chen
Abstract: The present invention provides in part a compound of Formula (I) or a pharmaceutically-acceptable salt or stereoisomer thereof: where R1 is selected from the group consisting of a substituted triazole group, a guanidine group, a urea group, a thiourea group, an amidine group, and N3; and R2 is selected from the group consisting of H, Me, Et and an amino acid, and methods and uses thereof.
Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I, processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including these compounds and related methods of treating or inhibiting certain diseases or conditions.
Abstract: The present invention provides compounds of formula (I), or pharmaceutically acceptable derivatives thereof wherein the variables Z, Q, Ring A, V, X, Y and Y? are as defined herein, and pharmaceutical compositions comprising these compounds. The compounds of formula (I) and pharmaceutical compositions comprising them are useful for treating a disorder for which a V1a antagonist is indicated, in particular, dysmenorrhoea.
Type:
Grant
Filed:
May 11, 2010
Date of Patent:
January 10, 2012
Assignee:
Pfizer Inc.
Inventors:
Justin Stephen Bryans, Patrick Stephen Johnson, Lee Richard Roberts, Thomas Ryckmans
Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.
Type:
Application
Filed:
May 4, 2011
Publication date:
January 5, 2012
Applicant:
YALE UNIVERSITY
Inventors:
William L. Jorgensen, Richard J. Bucala
Abstract: A method for fluorescently labeling a protein is provided that can also be used for labeling a biomolecule (a protein) in vivo with fluorescence.
Type:
Application
Filed:
March 10, 2010
Publication date:
December 29, 2011
Applicant:
OSAKA UNIVERSITY
Inventors:
Kazuya Kikuchi, Yuichirou Hori, Hideki Ueno
Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R4, R6, X, Y and Z are as defined herein. The compounds of Formula (I) have been found to act as glucokinase activators. Consequently, the compounds of Formula (I) and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucokinase.
Type:
Application
Filed:
March 4, 2010
Publication date:
December 29, 2011
Inventors:
Jeffrey W. Corbett, Angel Guzman-Perez, Jeffrey A. Pfefferkorn, Meihua Tu
Abstract: The refrigerating machine oil of the present invention contains a mineral oil whose nitrogen content is not more than 50 ppm by mass and whose percent in aromatic ring structures (% CA) is from 5 to 25. With the refrigerating machine oil of the present invention, high levels of lubricity, stability, and miscibility with refrigerants are attained, with a good balance between these, so refrigerating and air conditioning machines can be operated stably over a longer period.
Abstract: The present application relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.
Type:
Grant
Filed:
March 19, 2007
Date of Patent:
December 27, 2011
Assignee:
Bayer Cropscience AG
Inventors:
Peter Jeschke, Robert Velten, Thomas Schenke, Otto Schallner, Michael Edmund Beck, Olga Malsam, Ralf Nauen, Thomas Müller, Christian Arnold, Erich Sanwald, Ulrich Görgens
Abstract: The invention relates to a pentacyclic anion salt and to the use thereof in electrolyte compositions. The compound comprises an inorganic, organic or organometallic cation M of valency m (1?m?3) and m anions corresponding to the formula (I) in which Rf is a —CFZ?Z? group in which Z? is F or a perfluoroalkyl group having from 1 to 3 carbon atoms, and Z? is an H, F or Cl group, an optionally fluorinated or perfluorinated alkoxy group having from 1 to 5 carbon atoms, an optionally fluorinated or perfluorinated oxaalkoxy group having from 1 to 5 carbon atoms or an optionally fluorinated or perfluorinated alkyl group having from 1 to 5 carbon atoms; Z? being other than F when Z? is F. An electrolyte composition comprises said salt in solution in a liquid solvent or a polymer solvent.
Type:
Application
Filed:
August 28, 2009
Publication date:
December 22, 2011
Inventors:
Michel Armand, Sylvie Grugeon, Stephane Laruelle, Maria Bukowska, Przemyslaw Szczecinski, Wladyslaw Wieczorek, Leszek Niedzicki, Bruno Scrosati, Stefania Panero, Priscilla Realle
Abstract: According to the invention there is provided a compound of formula (I): (I) or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of A?42 and hence are useful in treatment of Alzheimer's disease and related conditions.
Type:
Application
Filed:
December 7, 2009
Publication date:
December 22, 2011
Inventors:
Christian Fischer, Adam J. Schell, Benito Munoz
Abstract: The present invention provides compounds of Formula (I), compositions comprising an effective amount of a compound of Formula (I), optionally with chemotherapeutic drugs such as a tubulin-binding drug, and methods of their use for reducing the toxicity of cytotoxic agents, treating or preventing cancer or a neuropathic disorder, inducing a chemoprotective phase II enzyme, DNA, or protein synthesis, enhancing the immune system, treating inflammation, improving and enhancing general health or well-being, and methods for making compounds of Formula (I).
Type:
Application
Filed:
August 27, 2009
Publication date:
December 22, 2011
Applicants:
SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH, TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
Inventors:
Samuel J. Danishefsky, Ting-Chao Chou, Xiaoguang Lei, Heedong Yun, Fay Ng, John Hartung, Dalibor Sames
Abstract: Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.
Abstract: There is provided a process for stereoselectively producing E-form of 3-acyloxyacrylonitrile compound (3) or Z-form which comprises reacting 3-oxopropionitrile compound (1) with an acid chloride (2), characterized in that the reaction is conducted with removal of hydrogen chloride, or by using an organic base or an inorganic base, to thereby regulate the stereostructure of the product; a process for producing the compound (1) characterized by reacting acetonitrile compound (5) with an aromatic ester compound (6) by use of an alkali metal alkoxide in a hydrocarbon solvent while removing alcohol formed as a by-product by azeotropic distillation in a separating tank; and a process for isomerizing E-form of 3-acyloxyacrylonitrile compound to Z-form thereof by use of an organic base.
Abstract: There is provided compounds of formula I, wherein A, X1, X2, X3, X4, Y1, Y2, Y3, Y4, Z1, Z2, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.
Type:
Grant
Filed:
April 12, 2006
Date of Patent:
December 20, 2011
Assignee:
Vicore Pharma AB
Inventors:
Mathias Alterman, Anders Hallberg, Xiongyu Wu
Abstract: The invention relates to dosage forms and formulations comprising the novel crystal modification A of the compound I-(2,6-difluorobenzyl)-I H-I,2,3-triazole-4-carboxamide, wherein crystal modification A is characterized by characteristic lines with interplanar spacings (d values) of 10.5 ?, 5.14 ?, 4.84 ?, 4.55 ?, 4.34 ?, 4.07 ?, 3.51 ?, 3.48 ?, 3.25 ?, 3.19 ?, 3.15 ?, 3.07 ?, and 2.81 ?, determined by means of an X-ray powder pattern. Dosage forms of crystal modification A of the compound I-(2,6-difluorobenzyl)-I H-I,2,3-triazole-4-carboxamide may be for oral or parenteral administration, in the form of a solid or liquid, and in a dosage range of 20 mg to less than 500 mg. Solid dosage forms comprise a tablet or capsule, and further comprise a pharmaceutically-acceptable carrier and film-coat.
Type:
Grant
Filed:
April 26, 2010
Date of Patent:
December 13, 2011
Assignee:
Novartis AG
Inventors:
Robert Portmann, Urs Christoph Hofmeier, Andreas Burkhard, Walter Scherrer, Martin Szelagiewicz
Abstract: It has been discovered that inhibiting mitochondrial respiration in platelets reduces platelet activation or platelet aggregation. Certain heterocyclic compounds significantly reduced one or more platelet functions including clumping, sticking or platelet-stimulated clotting. Thus diseases or disorders mediated by inappropriately high levels of platelet activation or platelet aggregation can be treated by administering a therapeutically effective amount of a heterocyclic compound or nonheterocyclic mitochondrial inhibitor that significantly reduces one or more platelet functions including clumping, sticking or platelet-stimulated clotting, preferably in a reversible manner.
Type:
Application
Filed:
April 25, 2011
Publication date:
December 8, 2011
Applicant:
Stanford University
Inventors:
James P. Collman, Paul Clifford Herrmann, David Alvin Tyvoll, Richard Decreau, Brian Stanley Bull, Christopher Jeffrey Barile
Abstract: Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is —CH2—; R is a mono- to tetra-substituted, mono- or bicyclic, unsaturated heterocyclic radical having 1 to 4 nitrogen atoms, R2 is C1-6alkyl or C3-6cycloalkyl; R3 is independently of one another H, C1-6alkyl, C1-6alkoxycarbonyl or C1-6alkanoyl; R4 is C2-6alkenyl, C1-6alkyl, unsubstituted or substituted aryl-C1-6alkyl or C3-8cycloalkyl; R5 is -Lm-R6; L is C1-6alkylene which is optionally substituted by 1-4 halogen, or a linker: formula (II) n=0, 1 or 2; m=0 or 1; R6 is a radical composed of 2 cyclic systems selected from bicyclo[x.y.z]alkyl, spiro[o.p]alkyl, mono- or bioxabicyclo[x.y.z]alkyl or mono- or bioxaspiro[o.
Type:
Grant
Filed:
September 14, 2006
Date of Patent:
December 6, 2011
Assignee:
Novartis AG
Inventors:
Peter Herold, Robert Mah, Vincenzo Tschinke, Stefan Stutz, Aleksandar Stojanovic, Christiane Marti, Dirk Behnke, Stjepan Jelakovic
Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.
Type:
Application
Filed:
December 21, 2010
Publication date:
December 1, 2011
Inventors:
Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
Abstract: Various methods and structures of complexes and molecules are described herein related to a zinc-centered catalyst for removing carbon dioxide from atmospheric or aqueous environments. According to one embodiment, a method for creating a tris(triazolyl)pentaerythritol molecule includes contacting a pentaerythritol molecule with a propargyl halide molecule to create a trialkyne molecule, and contacting the trialkyne molecule with an azide molecule to create the tris(triazolyl)pentaerythritol molecule. In another embodiment, a method for creating a tris(imidazolyl)pentaerythritol molecule includes alkylating an imidazole 2-carbaldehyde molecule to create a monoalkylated aldehyde molecule, reducing the monoalkylated aldehyde molecule to create an alcohol molecule, converting the alcohol molecule to create an alkyl halide molecule using thionyl halide, and reacting the alkyl halide molecule with a pentaerythritol molecule to create a tris(imidazolyl)pentaerythritol molecule.
Type:
Application
Filed:
May 25, 2010
Publication date:
December 1, 2011
Inventors:
Carlos A. Valdez, Joe H. Satcher, JR., Roger D. Aines, Sarah E. Baker
Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.
Type:
Application
Filed:
July 28, 2011
Publication date:
December 1, 2011
Inventors:
Hans Allgeier, Yves Auberson, David Carcache, Philipp Floersheim, Christel Guibourdenche, Wolfgang Froestl, Jörg Kallen, Manuel Koller, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud
Abstract: There is provided compounds of formula I, wherein the dotted line, X1, X2, X3, A, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.
Type:
Grant
Filed:
April 12, 2006
Date of Patent:
November 29, 2011
Assignee:
Vicore Pharma AB
Inventors:
Mathias Alterman, Anders Hallberg, Xiongyu Wu
Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particularly, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.
Type:
Application
Filed:
October 16, 2009
Publication date:
November 24, 2011
Applicant:
EXELIXIS, INC.
Inventors:
Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
Abstract: An organic light emitting diode with Ir complex is disclosed in this specification, wherein the Ir complex is used as the phosphorous emitter. The chemical containing pyridyl triazole or pyridyl imidazole functional group is used as the auxiliary monoanionic bidentate ligand in the mentioned Ir complex, so that the CIE coordinate of the mentioned Ir complex is adjustable and the light emitting performance of the Ir complex is improved.
Abstract: Methods of preparing heterocyclic triazolium-based nitrate salts by a streamlined process are provided. Such salts offer energetic performance as well as pharmaceutical potential.
Type:
Grant
Filed:
October 12, 2010
Date of Patent:
November 22, 2011
Assignee:
The United States of America as represented by the Secretary of the Air Force
Abstract: The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer.
Type:
Grant
Filed:
May 7, 2008
Date of Patent:
November 22, 2011
Assignee:
Eli Lilly and Company
Inventors:
Joyce Z. Crich, James Robert Henry, Hong Hu, Delu Jiang, Hong-Yu Li, William Thomas McMillen, Jason Scott Sawyer, Melissa Kate Slater, Yan Wang
Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A1, A2, A3 and L are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora and KDR.
Type:
Application
Filed:
May 12, 2011
Publication date:
November 17, 2011
Applicant:
ABBOTT LABORATORIES
Inventors:
Michael R. Michaelides, James H. Holms, Douglas H. Steinman
Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
Type:
Application
Filed:
February 2, 2010
Publication date:
November 17, 2011
Inventors:
Henricus, Jacobus, Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, Francois Paul Bischoff, Tongfei Wu, Sven, Franciscus, Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge, Maria, Aloysius Pieters, Didier Jean-Claude Berthelot, Michel, Anna, Josef De Cleyn, Daniel Oehlrich
Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).
Type:
Application
Filed:
July 8, 2011
Publication date:
November 17, 2011
Inventors:
Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
Abstract: A TAF compound that can have substitutions on either of the two benzene rings and/or the C-5 position of the triazole to alter the properties of the TAF compound can be wherein X can be H, an aromatic group, a hetero aromatic group, an alkyl or any substituted alkyl group, ketone, aldyhyde, carboxylic acid derivatives; Y1, Y2, Y3, Y4, and Y5 can be one or more of H, aromatic groups, hetero aromatic groups, alkyl or any substituted alkyl groups, ketone, aldyhyde, or carboxylic acid derivatives; and Z1, Z2, Z3, Z4, and Z5 can be one or more of H aromatic groups, hetero aromatic groups, alkyl or any substituted alkyl groups, ketone, aldyhyde, or carboxylic acid derivatives. Included is a preparation of the TAF compound and use as a photoactive and/or catalyst.