Abstract: A method of cancer intervention or eradication by administering an effective amount of an endogenous ligand for the aryl hydrocarbon (Ah) receptor (AhR) named ITE or one of its analogs (the active ingredient) to a subject with cancer is disclosed. An effective dose and dosing frequency of the active ingredient are determined by measuring its blood levels of the subject after dosing. The active ingredient formulated with a carrier system is applied topically, enterally, or parenterally to the subject. The formulated drug can also be administered together with one or more of other cancer therapeutic agents. A maintenance dosing is provided after the subject is free of cancer to insure the cancer eradication. Subjects with cancers of prostate, liver, lung, ovarian, and breast are preferably accepted for treatment.
Abstract: Provided herein are compounds of formula (I), pharmaceutical compositions comprising the compounds, and methods of use thereof The compounds provided herein modulate kinase activity, including PI3 kinase activity, and are useful for treating diseases and conditions associated with kinase activity, including diseases and conditions associated with PI3 kinase activity.
Type:
Grant
Filed:
May 20, 2011
Date of Patent:
December 10, 2013
Assignee:
Infinity Pharmaceuticals, Inc.
Inventors:
Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Alfredo C. Castro, Catherine A. Evans
Abstract: The present invention provides compositions comprising at least one oligomeric compound comprising an alternating motif and further include a region that is complementary to a nucleic acid target. The compositions are useful for targeting selected nucleic acid molecules and modulating the expression of one or more genes. In preferred embodiments the compositions of the present invention hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA. The present invention also provides methods for modulating gene expression.
Type:
Grant
Filed:
November 4, 2003
Date of Patent:
December 10, 2013
Assignee:
Isis Pharmaceuticals, Inc.
Inventors:
Charles Allerson, Balkrishen Bhat, Anne B. Eldrup, Muthiah Manoharan, Richard H. Griffey, Brenda F. Baker, Eric E. Swayze
Abstract: The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.
Abstract: Pharmaceutical compositions for the prophylaxis and treatment of HIV infection and its use are provided. Particularly, the present invention provides a pharmaceutical composition comprising anti-virus peptides, use of said composition for manufacturing a medicament for the prophylaxis and treatment of HIV infection, and method for preventing and treating HIV infection by using said composition.
Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.
Type:
Grant
Filed:
October 13, 2011
Date of Patent:
December 10, 2013
Assignee:
Inspire Pharmaceuticals, Inc.
Inventors:
John W. Lampe, Paul S. Watson, David J. Slade, Ward M. Peterson, Christopher S. Crean, Jason L. Vittitow, Jonathan Bryan DeCamp, Nicholas F. Pelz
Abstract: The present disclosure describes cyclohexenyl nucleic acid analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, cyclo-hexenyl nucleic acid analogs are provided, having one or more chiral substituents, that are expected to be useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.
Type:
Grant
Filed:
September 13, 2012
Date of Patent:
December 10, 2013
Assignee:
Inspire Pharmaceuticals, Inc.
Inventors:
John W. Lampe, Paul S. Watson, David J. Slade, Ward M. Peterson, Christopher S. Crean, Jason L. Vittitow, Jonathan Bryan DeCamp, Nicholas F. Pelz
Abstract: Monoclonal antibodies that bind and inhibit activation of human RON (Recepteur d' Origine Nantais) are disclosed. The antibodies can be used to treat certain forms of cancer that are associated with activation of RON.
Type:
Grant
Filed:
July 6, 2011
Date of Patent:
December 10, 2013
Assignee:
AVEO Pharmaceuticals, Inc.
Inventors:
Kerry Whalen, Steve Bottega, Andrea Boudrow, Lyne Breault, Ting Chen, James Gifford, May Han, Jinwei Jiang, Lorena Lerner, Qing Liu, Kristan Meetze, Sylvie Vincent, Solly Weiler, William M. Winston, Jr., Jeno Gyuris
Abstract: Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and/or the 5-HT1B receptor, without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2B receptors using the compounds and compositions disclosed herein.
Type:
Grant
Filed:
June 22, 2012
Date of Patent:
December 10, 2013
Assignee:
Map Pharmaceuticals, Inc.
Inventors:
Robert O. Cook, Jian Zhang, Thomas A. Armer
Abstract: The invention discloses highly purified daptomycin and to pharmaceutical compositions comprising this compound. The invention discloses a method of purifying daptomycin comprising the sequential steps of anion exchange chromatography, hydrophobic interaction chromatography and anion exchange chromatography. The invention also discloses a method of purifying daptomycin by modified buffer enhanced anion exchange chromatography. The invention also discloses an improved method for producing daptomycin by fermentation of Streptomyces roseosporus. The invention also discloses high pressure liquid chromatography methods for analysis of daptomycin purity. The invention also discloses lipopeptide micelles and methods of making the micelles. The invention also discloses methods of using lipopeptide micelles for purifying lipopeptide antibiotics, such as daptomycin. The invention also discloses using lipopeptide micelles therapeutically.
Type:
Grant
Filed:
February 16, 2012
Date of Patent:
December 10, 2013
Assignee:
Cubist Pharmaceuticals, Inc.
Inventors:
Thomas J. Kelleher, Jan-Ji Lai, Joseph P. DeCourcey, Paul D. Lynch, Maurizio Zenoni, Auro R. Tagliani
Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
Type:
Application
Filed:
August 7, 2013
Publication date:
December 5, 2013
Applicant:
Rigel Pharmaceuticals, Inc.
Inventors:
Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
Abstract: Silicone adhesive formulations are provided, in which fentanyl particles are suspended one or more a solvated silicone adhesives. The formulations can be used for manufacturing improved, matrix-type transdermal devices for administering fentanyl.
Type:
Application
Filed:
April 29, 2013
Publication date:
December 5, 2013
Applicant:
Mylan Pharmaceuticals, Inc.
Inventors:
Kenneth J. Miller, Sharad K. Govil, Kuljit Singh Bhatia
Abstract: Genetically modified mice are provided that express human ? variable (hV?) sequences, including mice that express hV? sequences from an endogenous mouse ? light chain locus, mice that express hV? sequences from an endogenous mouse ? light chain locus, and mice that express hV? sequences from a transgene or an episome wherein the hV? sequence is linked to a mouse constant sequence. Mice are provided that are a source of somatically mutated human ? variable sequences useful for making antigen-binding proteins. Compositions and methods for making antigen-binding proteins that comprise human ? variable sequences, including human antibodies, are provided.
Type:
Application
Filed:
July 18, 2013
Publication date:
December 5, 2013
Applicant:
Regeneron Pharmaceuticals, Inc.
Inventors:
Lynn Macdonald, Sean Stevens, Cagan Gurer, Andrew J. Murphy, Karolina A. Meagher
Abstract: The present invention provides methods for treating cancer. More particularly, the invention provides methods for treating cancer comprising administrating doses of a Notch2/3 antibody.
Type:
Application
Filed:
May 16, 2013
Publication date:
December 5, 2013
Applicant:
OncoMed Pharmaceuticals, Inc.
Inventors:
Timothy Charles HOEY, John A. Lewicki, Wan-Ching Yen, Jakob Dupont
Abstract: Provided herein are methods for cell therapy by modifying transfused cells to express an inducible caspase 9 protein, so that the cells may be selectively killed if the patient experiences dangerous side effects. Provided also within relates in part to methods for preventing or treating Graft versus Host Disease by modifying T cells before administration to a patient, so that they may be selectively killed if GvHD develops in the patient.
Inventors:
Iver Larson, Shilpa Sawhney, Shawn Lynn Goodman, Irache B. Visiers, Lilla O. Swan, Susan Proulx, Stephanie DeGraw, Michael Wiklund, Jonathan Kendler, Cynthia Inez Phillips, Christopher Hurff
Inventors:
Iver Larson, Shilpa Sawhney, Shawn Lynn Goodman, Irache B. Visiers, Lilla O. Swan, Susan Proulx, Stephanie DeGraw, Michael Wiklund, Jonathan Kendler, Cynthia Inez Phillips, Christopher Hurff
Inventors:
Iver Larson, Shilpa Sawhney, Shawn Lynn Goodman, Irache B. Visiers, Lilla O. Swan, Susan Proulx, Stephanie DeGraw, Michael Wiklund, Jonathan Kendler, Cynthia Inez Phillips, Christopher Hurff
Inventors:
Iver Larson, Shilpa Sawhney, Shawn Lynn Goodman, Irache B. Visiers, Lilla O. Swan, Susan Proulx, Stephanie DeGraw, Michael Wiklund, Jonathan Kendler, Cynthia Inez Phillips, Christopher Hurff