Abstract: Provided herein are methods and compositions for improving muscle performance and increasing endurance. Agonists of AMP-activated protein kinase (AMPK) and agonists of peroxisome proliferator-activated receptor delta (PPAR?) can be used in such treatments.
Type:
Grant
Filed:
December 29, 2008
Date of Patent:
November 24, 2015
Assignee:
Salk Institute for Biological Studies
Inventors:
Ronald M. Evans, Vihang A. Narkar, Reuben J. Shaw, Michael Downes, Ruth T. Yu
Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.
Type:
Grant
Filed:
October 15, 2010
Date of Patent:
November 24, 2015
Assignee:
Melinta Therapeutics, Inc.
Inventors:
Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Marco DeVivo, Zoltan F. Kanyo, Jacek G. Martinow, Ik-Hyeon Paik, Matthew H. Scheideman, Sandra Sinishtaj, Brian T. Wimberly, Yusheng Wu
Abstract: Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.
Type:
Grant
Filed:
August 15, 2008
Date of Patent:
November 24, 2015
Assignee:
Purdue Research Foundation
Inventors:
Philip Stewart Low, Sumith A. Kularatne
Abstract: The present invention concerns methods for treating a proliferation disorder, such as prostate cancer, basal cell carcinoma, lung cancer, and other cancers, using an inhibitor of the Hedgehog pathway (HhP); and methods for monitoring subjects undergoing such treatments based on biomarkers and other criteria predictive of efficacy.
Type:
Grant
Filed:
February 5, 2014
Date of Patent:
November 24, 2015
Assignee:
HEDGEPATH PHARMACEUTICALS, INC.
Inventors:
Nicholas J. Virca, Francis E. O'Donnell, Jr.
Abstract: The invention relates to an oral pharmaceutical composition comprising the combination of an ibuprofen salt or S(+)-ibuprofen with L-arginine and/or the pharmaceutically acceptable salts thereof, and additionally pharmaceutically acceptable vehicles and/or excipients. The invention also relates to the method of producing the composition and to the use of said composition having synergic therapeutic activity, for treating moderate to severe inflammatory pain, fever and inflammation.
Type:
Grant
Filed:
April 28, 2011
Date of Patent:
November 17, 2015
Assignee:
LABORATORIOS SENOSIAIN S.A. DE C.V.
Inventors:
Juan Pablo Senosiain Peláez, Angélica Arzola Paniagua, Enrique Raúl García-Salgado López
Abstract: The present invention relates to bisaryl-linked 5-aryl-1,2,4-triazolone derivatives according to the following formula: wherein Ar1, Ar2, R1, R2, L1, L2, Q and n are defined herein. The invention further related to the process of making the bisaryl-linked 5-aryl-1,2,4-triazolone derivatives.
Type:
Grant
Filed:
February 25, 2011
Date of Patent:
November 17, 2015
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Chantal Furstner, Joerg Keldenich, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Ingo Pluschkell, Elisabeth Pook, Carsten Schmeck, Hubert Trubel
Abstract: Methods for preparing sterilized baclofen solutions include adjusting the pH to below a desired pH, and steam sterilizing the solution with adjusted pH, which results in the solution having the desired pH. Such solutions may also have low concentrations of 4-CPP. Injectable baclofen solutions having greater than 2 mg/mL baclofen include between 5 mM and 25 mM of a phosphate or sulfate species. The solution has an ionic strength equivalent of about 1.5 M NaCl. The present application also provides baclofen formulations for use in treating spasticity, brain injury, cerebral palsy, spinal cord injury, cervical injury, multiple sclerosis, thoracic injury, or withdrawal symptoms.
Type:
Grant
Filed:
October 26, 2012
Date of Patent:
November 10, 2015
Assignee:
Medtronic, Inc.
Inventors:
Michael C. Schmitz, Corinne Dominguez, Thomas E. Keene, Deanna S. Lane, Lanchi T. Le, Jianwei Li, Ngoc T. Lu, Carmen E. Snaza
Abstract: The invention relates to the compounds of formula I and pharmaceutically acceptable salts and esters thereof, wherein R1-R11 are as defined in the description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are useful in differentiating stem cells into more mature or adult-like hepatocytes for use as drug screening platforms and in disease modeling applications.
Type:
Grant
Filed:
February 3, 2015
Date of Patent:
November 10, 2015
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Eric Chiao, Matthew Michael Hamilton, Sei Kameoka, Brian Leonard, Miriam Triyatni
Abstract: Insecticidal, acaricidal, nematicidal or molluscicidal compounds of formula (I) wherein Y is a single bond, C?O, C?S or S(O)q where q is 0, 1 or 2; and R1, R2, R3, R4, R8, R9 are R10 are as defined in the claims or salts or N-oxides thereof, processes for preparing them and compositions containing them.
Type:
Grant
Filed:
September 16, 2011
Date of Patent:
November 3, 2015
Assignees:
Syngenta Limited, Syngenta Participations AG
Inventors:
David John Hughes, Paul Anthony Worthington, Charles Adam Russell, Eric Daniel Clarke, James Edward Peace, Mark Richard Ashton, Thomas Stephen Coulter, Richard Spurring Roberts, Louis-Pierre Molleyres, Fredrik Cederbaum, Jerome Cassayre, Peter Maienfisch
Abstract: The present invention is drawn to a pharmaceutical composition comprising the following compound: The compound and other azacycle derivatives can be used in method of treatments for retroviral infections, such as HIV.
Abstract: This invention relates to the use of a ligand of the 5-HT4 receptor or of a pharmaceutically acceptable salt of this ligand and to a nucleic acid coding for a 5-HT4 receptor or of a functionally equivalent receptor for a drug for treating and/or preventing a pathology associated with an obsessional behavior such as anorexia, bulimia and the addiction to drugs of abuse or obesity. The invention also relates to a method for identifying a compound that is biologically active in the treatment and/or the prevention of a pathology associated with an obsessional conduct or obesity including: a) placing the 5-HT4 receptor or a functionally equivalent receptor in contact with this biologically active compound, and b) the determination of whether this biologically active compound is capable of modulating the basal activity of the 5-HT4 receptor or of a functionally equivalent receptor.
Type:
Grant
Filed:
April 3, 2013
Date of Patent:
October 27, 2015
Assignee:
Centre National de la Recherche Scientifique-CNRS
Abstract: Provided is a compound which has strong intraocular pressure lowering action and has no side effect on eyes such as ocular stimulating property, humor protein rise etc. Since a compound represented by the formula (I): (wherein definition of each group is as described in the specification), or a salt thereof, a solvate thereof, or a prodrug thereof has strong intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
Abstract: Disclosed are novel compounds which inhibit RSK, methods of making such compounds and pharmaceutical compositions comprising such compounds. Also disclosed are methods of treating RSK2 regulated disorders using compounds of the invention.
Type:
Grant
Filed:
November 30, 2010
Date of Patent:
October 6, 2015
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Stephen J. Boyer, Donghong Amy Gao, Xin Guo, Thomas Martin Kirrane, Jr., Christopher Ronald Sarko, Roger John Snow, Fariba Soleymanzadeh, Yunlong Zhang
Abstract: The present invention is directed to a pharmaceutical composition comprising the following compound or a pharmaceutically acceptable salt thereof. The compound is a modulator of Nrf2 protein and binds at least one of the BTB domain, IVR domain and Kelch domain of Keap1 protein, activating or inhibiting Nrf2.
Abstract: Disclosed are methods and compositions for treating subjects with Cornelia de Lange Syndrome (CdLS). Specifically disclosed are methods for using Indomethacin or Acemetacin to treat subjects with CdLS. Also disclosed are methods for identifying compounds beneficial for the treatment of CdLS using an assay based on the expression of NIPBL or NIPBL homologous or orthologous genes. Also disclosed is a method of identifying compounds beneficial for the treatment of CdLS based on administering a test compound to Drosophila lava with reduced expression of Nipbl, and determining the normalization of CdLS phenotypes.
Type:
Grant
Filed:
May 7, 2013
Date of Patent:
September 22, 2015
Assignees:
Saint Louis University, Washington University
Abstract: Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of cytopathic diseases. Cytopathic diseases may be caused by a variety means such as viral infections like HIV and AIDS in a mammalian subject. The methods and compositions of the invention are effective for inhibiting de novo HIV infection, upregulating viral expression from latent provirus, inhibiting HIV-induced cytopathic effects, down regulating the HIV receptor, increasing ThI cytokine expression, and decreasing Th2 cytokine expression. Additional compositions and methods are provided which employ a phorbol ester or derivative compound in combination with at least one additional agent such as those used in HAART protocols or therapeutic agents used to treat opportunistic infections due to HIV in mammalian subjects.
Abstract: This disclosure relates to 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine or a pharmaceutically acceptable salt thereof in a crystalline form.
Type:
Grant
Filed:
July 9, 2014
Date of Patent:
September 8, 2015
Assignee:
H. Lundbeck A/S
Inventors:
Benny Bang-Andersen, Andre Faldt, Arne Mork, Heidi Lopez de Diego, Rene Holm, Tine Bryan Stensbol
Abstract: The invention relates to compounds of the formulae (I), (II) and (III) in which R1, R2, R3, R4, Y, W1, W2, L, A, Alk, Cyc, Ar, Het1, Het2, Hal and n have the meaning indicated in Claim 1, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of their salts.
Type:
Grant
Filed:
February 17, 2011
Date of Patent:
September 8, 2015
Assignee:
Merck Patent GmbH
Inventors:
Werner Mederski, Thomas Fuchss, Frank Zenke
Abstract: 1-[2-(2,4-dimethylphenylsulphanyl)phenyl]piperazine exhibits potent activity on SERT, 5-HT3 and 5-HT1A and may as such be useful for the treatment of cognitive impairment, especially in depressed patients.
Type:
Grant
Filed:
April 1, 2014
Date of Patent:
September 8, 2015
Assignee:
H. Lundbeck A/S
Inventors:
Benny Bang-Andersen, Arne Mork, Tine Bryan Stensbol, Andre Faldt, Rene Holm, Heidi Lopez de Diego
Abstract: This invention provides novel pharmaceutical compositions of the compound of formula (I): or a pharmaceutically acceptable salt thereof, that are suitable for the bulk production of an oral pharmaceutical dosage form; processes for the production of said oral pharmaceutical dosage form; and the use of the pharmaceutical composition for the treatment of patients suffering from or subject to diseases, disorders, or conditions involving cell survival, proliferation and migration, including chronic inflammatory proliferative disorders, proliferative ocular disorders, benign proliferative disorders, and cancer.
Type:
Grant
Filed:
June 11, 2013
Date of Patent:
September 8, 2015
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Vijayalakshmi Ramanan, Irene S. Tobias, Raymond D. Skwierczynski, Dauntel S. Verwijs