Abstract: The present invention relates to a process for preparing azabicyclic compounds that are useful intermediates for synthesizing pharmaceutical compounds or salts thereof.
Type:
Grant
Filed:
March 9, 2012
Date of Patent:
June 11, 2013
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Narendra Bhalchandra Ambhaikar, Brian Richard Bear, Lev T. D. Fanning, Robert Hughes, Benjamin Littler
Abstract: The present invention relates to novel imidazoline derivatives and their use as insecticidal, acaricidal, molluscicidal and nematocidal agents. The invention also extends to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising such imidazoline derivatives, and to methods of using such derivatives and/or compositions to combat and control insect, acarine, mollusc and nematode pests.
Type:
Grant
Filed:
September 9, 2008
Date of Patent:
June 4, 2013
Assignee:
Syngenta Crop Protection LLC
Inventors:
Anthony Cornelius O'Sullivan, Thomas Pitterna, Jürgen Harry Schaetzer, Christoph Luethy
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:
July 12, 2012
Date of Patent:
May 21, 2013
Assignee:
The Regents of the University of Michigan
Inventors:
James R. Baker, Jr., Xue-min Cheng, Thommey P. Thomas, Baohua Mark Huang
Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease.
Type:
Grant
Filed:
February 28, 2011
Date of Patent:
May 14, 2013
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Kevin M. Cottrell, John Maxwell, Qing Tang, Anne-Laure Grillot, Arnaud Le Tiran, Emanuele Perola
Abstract: Disclosed are precursors having a pyrrolecarbaldiminates ligand and methods of synthesizing the same. The pyrrolecarbaldiminates ligand may be substituted.
Type:
Grant
Filed:
December 30, 2011
Date of Patent:
April 30, 2013
Assignee:
American Air Liquide, Inc.
Inventors:
Andrey V. Korolev, Clément Lansalot-Matras
Abstract: The invention provides an improved, highly efficient method for preparing 5-(2-ethyl-2,3-dihydro-1H-inden-2-yl)-1H-imidazole, and its salts, in particular its pharmaceutically acceptable salts.
Abstract: Disclosed is a process for producing a protected optically active fluoroamine, which comprises the step of reacting an imine-protected optically active hydroxyamine, an oxazolidine-protected optically active hydroxyamine, or a mixture of the imine-protected optically active hydroxyamine and the oxazolidine-protected optically active hydroxyamine, with sulfuryl fluoride (SO2F2) in the presence of a tertiary amine having a carbon number of 7 to 18 (produced by substituting all of three hydrogen atoms in ammonia by alkyl groups). The desired optically active fluoroamine can be produced by hydrolyzing the protected optically active fluoroamine under acidic conditions.
Abstract: The present invention is related to the preparation and pharmaceutical use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification: (I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases.
Type:
Grant
Filed:
November 19, 2008
Date of Patent:
April 23, 2013
Assignee:
Pharmaxis Ltd.
Inventors:
Ian A. McDonald, Craig Ivan Turner, Mandar Deodhar, Jonathan Stuart Foot
Abstract: Disclosed are JAK inhibitors of formula I where G1, R1, R2, R3, R4, R5, R6, and R7 are defined in the specification. Also disclosed are pharmaceutical compositions, kits and articles of manufacture which contain the compounds, methods and materials for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other diseases, disorders or conditions associated with JAK.
Type:
Grant
Filed:
June 8, 2010
Date of Patent:
April 16, 2013
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Qing Dong, Toufike Kanouni, John David Lawson, Michael B. Wallace
Abstract: An electrolyte additive is selected from N-alkyl benzimidazole derivatives and is applicable to dye-sensitized solar cells. Accordingly, the electrolyte additive can be added to electrolyte at low concentration, and loss of function due to crystallization after long-term use can be prevented; in addition, short circuit photocurrent density and solar energy-to-electricity conversion efficiency of solar cells incorporating the electrolyte additive can be increased.
Type:
Grant
Filed:
July 15, 2010
Date of Patent:
April 2, 2013
Assignee:
National Taipei University of Technology
Abstract: Hydrated celecoxib sodium salt forms and processes to prepare hydrated celecoxib sodium salt forms are disclosed. The celecoxib sodium salt forms are particularly useful and suitable for pharmaceutical applications.
Type:
Grant
Filed:
July 29, 2011
Date of Patent:
April 2, 2013
Assignee:
McNeil-PPC, Inc.
Inventors:
Julius F. Remenar, Mark D. Tawa, Matthew L. Peterson
Abstract: The present invention relates to novel aryl sulfonamide amine compounds of the formula (I), their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates described herein and pharmaceutically acceptable compositions containing them.
Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.
Type:
Grant
Filed:
September 16, 2011
Date of Patent:
February 26, 2013
Assignee:
Cephalon, Inc.
Inventors:
Nadine C. Becknell, Peter D. Brown, Reddeppareddy Dandu, James L. Diebold, Diane E. Gingrich, Robert L. Hudkins, Bruce A. Ruggeri, Ming Tao, Theodore L. Underiner, Allison L. Zulli
Abstract: The present application relates to a method for producing an optically active ?-amino acid derivative, comprising steps of reacting an ?-haloester derivative represented by the general formula (1): of which alcohol part of the ester group is an optically active alcohol derivative, with an amine compound; then deprotecting the obtained compound; further carrying out an ester exchange reaction. According to the present invention method, it is possible to easily produce an optically active ?-amino acid ester derivative which is useful as an intermediate for drugs with high selectivity.
Abstract: Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
Type:
Grant
Filed:
August 11, 2011
Date of Patent:
February 19, 2013
Assignee:
XenoPort, Inc.
Inventors:
Mark A. Gallop, Xuedong Dai, Randall A. Scheuerman, Stephen P. Raillard, Suresh K. Manthati, Fenmei Yao, Thu Phan, Maria Ludwikow, Ge Peng, Seema Bhat
Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof. These compounds inhibit serine protease, particularly the hepatitis C virus NS3-NS4A protease.
Type:
Grant
Filed:
March 29, 2011
Date of Patent:
February 12, 2013
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Kevin M. Cottrell, John Maxwell, Qing Tang, Anne-Laure Grillot, Arnaud Le Tiran, Emanuele Perola