Abstract: The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren, the invention relates to a process for the manufacture of a compound of the formula I, or a salt thereof, wherein R1 as well as Act are as defined in the specification, and processes of manufacturing this compound as well as intermediates in this process.
Abstract: Compounds, compositions and methods are provided for stabilizing transthyretin and for treating, preventing, or ameliorating one or more symptoms of transthyretin mediated diseases. In one embodiment, the compounds are benzoxazoles and related compounds.
Abstract: Methods for the preparation of indene-based thiazolidinethiones are provided comprising contacting 1-amino-2,3-dihydro-1H-inden-2-ol, or a substituted derivative thereof, with an acid under suitable reaction conditions to provide a first intermediate; and contacting the first intermediate with an alkali xanthate in the presence of an alkali hydroxide under suitable reaction conditions to provide a compound of formula (III), wherein R1-R8 are defined herein.
Type:
Grant
Filed:
January 11, 2010
Date of Patent:
November 13, 2012
Assignee:
University of Iowa Research Foundation
Inventors:
Horacio F. Olivo, Antonio Victor Osorio Lozada
Abstract: This invention relates to novel macrocyclic lactams intermediates useful for the preparation of diazonamide analogs. This invention also relates to a novel electrochemical oxidative cyclization for the preparation of such macrocyclic lactams, and their further elucidation to provide diazonamide analogs.
Type:
Grant
Filed:
July 19, 2011
Date of Patent:
October 30, 2012
Assignees:
Board of Regents, The University of Texas System, Joyant Pharmaceuticals, Inc.
Inventors:
Gunnar Hanson, Charles Caldwell, Patrick G. Harran, Susan Harran, Qi Wei, Ming Zhou
Abstract: A gel-like or solid electrolyte containing (i) an electrolyte solution containing an electrolyte dissolved in an organic solvent, (ii) a lamellar clay mineral and/or an organically modified lamellar clay mineral and (iii) a polyvalent onium salt compound and a photoelectric transducer element and a dye-sensitized solar cell using the same.
Abstract: The present invention provides a method of producing a compound (IIa) or a compound (IIb), provides a method of producing a compound (IIIa) or a compound (IIIb), provides a method of producing a compound (Va) or its salt or a compound (Vb) or its salt, provides a method of producing a compound (IIIa) or a compound (IIIb), further, provides a method of producing a compound (Va) or its salt or a compound (Vb) or its salt including these production methods.
Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.
Type:
Grant
Filed:
March 9, 2011
Date of Patent:
October 23, 2012
Assignee:
President and Fellows of Harvard College
Abstract: The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameliorated by inhibition of phosphatidylinositol 3-kinase.
Type:
Grant
Filed:
June 28, 2010
Date of Patent:
October 23, 2012
Assignee:
Novartis AG
Inventors:
Robin Alec Fairhurst, Pascal Furet, Marc Gerspacher, Robert Mah
Abstract: Provided are processes of preparing glycolurils and cucurbiturils using the glycolurils by microwave irradiation. Therefore, condensation and cyclization reactions for preparation of industrially widely applied cucurbituril derivatives, oxidation reaction for preparation of hydroxycucurbiturils, and condensation and cyclization reactions between glycolurils and paraformaldehyde or a formaldehyde solution can be efficiently performed in a short time.
Type:
Grant
Filed:
April 26, 2005
Date of Patent:
October 23, 2012
Assignee:
Postech Academy-Industry Foundation
Inventors:
Kimoon Kim, Samal Shashadhar, Nandha Kumar Raju, Selvapalam Narayanan, Dong Hyun Oh
Abstract: The present invention relates to processes for preparing (3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetylguanidine derivatives of the formula I via 3-hydroxy-2,3-dihydro-1H-isoindol-1-one derivatives or 3-(2-carbamoylphenyl)-acrylic ester derivatives as intermediates, to a process for optical resolution, and to intermediates of the process according to the invention.
Type:
Grant
Filed:
April 2, 2009
Date of Patent:
October 9, 2012
Assignee:
Sanofi-Aventis Deutschland GmbH
Inventors:
Gerrit Schubert, Joerg Rieke-Zapp, Johannes Keil, Heinz-Werner Kleemann, Reda Hanna, Bao-Guo Huang, Xiao-Dong Wu, Yves Gouraud
Abstract: This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A2 enzymes (cPLA2), more particularly including inhibitors of cytosolic phospholipase A2 alpha enzymes (cPLA2?). In some embodiments, the inhibitors have the Formula I: wherein the constituent variables are as defined herein.
Type:
Grant
Filed:
June 19, 2009
Date of Patent:
October 9, 2012
Assignee:
Pfizer Inc.
Inventors:
John C. McKew, Katherine L. Lee, Lihren Chen, Richard Vargas, James D. Clark, Cara Williams, Valerie Clerin, Suzana Marusic, Kevin Pong
Abstract: The present invention provides a method for the preparation of mycophenolate mofetil wherein mycophenolic acid or an amine salt of mycophenolic acid is esterified with 2-morpholinoethanol, the resulting mixture is extracted into water at a pH-value between 1.0 and 3.0, and mycophenolate mofetil is back-extracted in a water-immiscible solvent at a pH-value between 3.0 and 5.0.
Abstract: Provided is a fluoroboron compound which is highly safe and stable and is capable of forming a cyclic ether-fused ring by the intramolecular alkoxymethylation reaction, or a salt thereof. The compound can be synthesized by the intramolecular alkoxymethylation reaction of a fluoroboron compound represented by the formula (I) or a salt thereof in the presence of a metal catalyst. (wherein the moiety represented by the formula represents an aromatic ring; L represents a substituent such as a halogen atom; R represents a substituted or unsubstituted alkylene group having 1 or 2 carbon atoms; and M represents an alkali metal cation or the like, with the proviso that L and —R—OCH2BF3M are respectively located on contiguous carbon atoms on the aromatic ring, or in the case of a fused aromatic ring, on two carbon atoms adjacent to one carbon at the fused position).
Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Type:
Grant
Filed:
September 4, 2007
Date of Patent:
September 18, 2012
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Tiansheng Wang, Jeremy Green, Brian Ledford, François Maltais, Andreas P. Termin, Mark Cornebise, Jonathan Parsons, Adam Tanner, James Westcott
Abstract: The present invention relates to a composition comprising pesticide and polyalkylene oxide. The invention furthermore relates to pyrrolidone alkylene oxides and the use thereof in agrochemical formulations. It furthermore relates to the use of the composition according to the invention for controlling phytopathogenic fungi and/or undesired vegetation and/or undesired attack by insects or mites and/or for regulating the growth of plants. Furthermore, it relates to the use of a composition according to the invention for controlling undesired attack by insects or mites on plants and/or for controlling phytopathogenic fungi and/or for controlling undesired vegetation, where seeds of useful plants are treated with the composition. Finally, the present invention also relates to seed treated with the composition according to the invention. The present invention comprises combinations of preferred features together with other preferred features.
Abstract: The present invention relates to a new process for the preparation of 2-imino-thiazolidin-4-one compounds of the Formula (I) and (II) and to compounds of Formula (II) as such. The present compounds of Formula (II) can be used as intermediates in the preparation of thiazolidin-4-one derivatives of the General Formula (II), which thiazolidin-4-one derivatives being described in WO 2005/054215 to act as immunosuppressive agents.
Type:
Grant
Filed:
November 22, 2007
Date of Patent:
September 11, 2012
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Stefan Abele, Martin Bolli, Gunther Schmidt
Abstract: The invention discloses a dithiolopyrrolone compound represented by formula I or its pharmaceutically acceptable salts, wherein X1, R1, R2, R3, R4 are defined as in the description. The invention also discloses the preparation of such compounds, and the use of such compounds in preparation of medicaments for increasing peripheral white blood cells and in preparation of ancillary medicaments for inhibiting the decrease of peripheral white blood cells in radiotherapy or chemotherapy.
Type:
Grant
Filed:
August 29, 2008
Date of Patent:
September 4, 2012
Assignees:
Shanghai Institute of Pharmaceutical Industry, Shanghai Modern Pharmaceutical Co., Ltd.
Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.
Abstract: The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.
Type:
Grant
Filed:
March 12, 2009
Date of Patent:
August 28, 2012
Assignee:
The Regents of the University of Michigan
Inventors:
James R. Baker, Jr., Xue-min Cheng, Thommey P. Thomas, Baohua Mark Huang