Abstract: The present invention refers to a pharmaceutical composition that includes an active ingredient, such as a peptide, which acts as an antagonist and/or inverse agonist of a G protein-coupled receptor and pharmaceutically acceptable vehicle. The pharmaceutical composition may be used for the treatment of obesity and the prevention of and the treatment of diabetes.
Type:
Grant
Filed:
May 4, 2015
Date of Patent:
September 27, 2016
Assignee:
Sociedade Beneficente de Senhoras Hospital Sirio Libanes
Inventors:
Andrea Sterman Heimann, Camila Squarzoni Dale, Lakshmi A. Devi
Abstract: The present application is directed to rapid and efficient synthesis of radiometal-labeled probes, pharmaceutical compositions comprising radiometal-labeled probes, and methods of using the radiometal-labeled probes. Such radiometal-labeled probes can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT), and therapy studies.
Abstract: The present invention provides a novel macrocyclic compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
Type:
Grant
Filed:
May 29, 2014
Date of Patent:
August 23, 2016
Assignee:
The Regents of the University of Colorado, A Body Corporate
Inventors:
Xuedong Liu, Andrew J. Phillips, Dana Ungermannova, Christopher G. Nasveschuk, Gan Zhang
Abstract: A composition which is reversible inhibitor of at least one neuron-specific PDZ domain comprising wherein R is a molecular transporter with or without a linker amino acid; R1 is at least about one amino acid covalently bound; and, R2 is isoleucine, leucine, alanine, phenylalanine, or valine, and methods of use.
Type:
Grant
Filed:
May 18, 2010
Date of Patent:
August 2, 2016
Assignee:
Brown University
Inventors:
Mark Spaller, John Marshall, Dennis J. Goebel
Abstract: Compounds of formula (I), salts thereof, and compositions and uses thereof are described. The compounds are useful as V1a vasopressin agonists, for the treatment of, e.g., complications of cirrhosis, including bacterial peritonitis, HRS2 and refractory ascites.
Type:
Grant
Filed:
November 5, 2014
Date of Patent:
July 12, 2016
Assignee:
Ferring B.V.
Inventors:
Kazimierz Wisniewski, Geoffrey S. Harris, Robert Galyean
Abstract: There are provided compounds of formula I: wherein k, m, n, p, R, R?, R?, R??, R3, R4, R7 and R8 are as defined in the application. Other embodiments are also disclosed.
Type:
Grant
Filed:
August 24, 2012
Date of Patent:
July 5, 2016
Inventors:
Janusz Zabrocki, Michal Zimecki, Andrzej Kaszuba, Krzysztof Kaczmarek
Abstract: The present invention relates to novel cycloundecadepsipeptide compounds and their analoges which bind and inhibit cyclophilins, have reduced immunosuppressive activity and improved physicochemical properties including water solubility. The present invention further relates to pharmaceutical compositions containing said depsipeptide compounds and their analoges for use in the treatment or prevention of diseases and pathologies which may be ameliorated by the inhibition of cyclophilin activity.
Type:
Grant
Filed:
October 2, 2013
Date of Patent:
July 5, 2016
Assignee:
Cypralis Limited
Inventors:
Hans Georg Fliri, Rhonan Lee Ford, Antonio Kuok Keong Vong
Abstract: The invention relates to synthetic routes for preparing telaprevir and boceprevir, and its intermediates as well as peptides other than telaprevir. The synthetic routes are based on a Mukaiyama aldol addition reaction of a silyl enol ether or an enolate with an imine. The invention also refers to novel intermediates for preparing telaprevir/boceprevir or other peptides.
Type:
Grant
Filed:
June 19, 2013
Date of Patent:
May 24, 2016
Assignee:
Sandoz AG
Inventors:
Kathrin Hoeferl-Prantz, Wolfgang Felzmann, Thorsten Wilhelm, David Benito-Garagorri
Abstract: There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
Abstract: Novel protein tyrosine phosphatase (PTP) inhibitor compounds synthesized from phosphonodifluoromethyl phenylalanine (F2Pmp) are provided. Use of these compounds for inhibiting a PTP enzyme (such as PTP-MEG2), as well as treating a disease, disorder, or condition associated with inappropriate activity of a PTP (such as type 2 diabetes), is also provided.
Type:
Grant
Filed:
October 3, 2013
Date of Patent:
May 17, 2016
Assignee:
Indiana University Research and Technology Corporation
Abstract: The present invention relates to a method of removing an Fmoc group, including a step of mixing a compound represented by the formula (I): HS-L-COOH??(I) wherein L is a C1-8 alkylene group optionally having substituent(s), an amino group-containing compound protected by an Fmoc group, and a base to give a reaction mixture containing a compound represented by the formula (II): Fm—S-L-COOH??(II) wherein Fm is a 9-fluorenylmethyl group, and L is as mentioned above, and an amino group-containing compound, and a step of removing the compound represented by the formula (II) by washing the obtained reaction mixture with a basic aqueous solution. According to the present invention, a removal method of Fmoc group, which can remove a dibenzofulvene derivative as a byproduct with ease, can be provided.
Abstract: Heteroaryl pyridone and aza-pyridone amide compounds of Formula I are provided, and various substituents including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Type:
Grant
Filed:
July 2, 2014
Date of Patent:
May 3, 2016
Assignee:
Genentech, Inc.
Inventors:
James John Crawford, Wendy Lee, Wendy B. Young
Abstract: The invention provides compounds, compositions, and methods for the treatment of diseases, disorders, or conditions that are modulated by matrix metalloproteinases (MMPs). The disease, disorder, or condition can include, for example, stroke, neurological disorders, or ophthalmological disorders. The treatment can include administering a compound or composition described herein, thereby providing a prodrug compound that metabolizes to an active MMP inhibitor in vivo. The MMP inhibition can be selective inhibition, for example, selective inhibition of MMP-2, MMP-9, and/or MMP-14. Thus, the invention provides non-mutagenic prodrug compounds of the formulas described herein that result in the inhibition of MMPs upon in vivo administration.
Type:
Grant
Filed:
December 11, 2014
Date of Patent:
April 26, 2016
Assignee:
University of Notre Dame du Lac
Inventors:
Mayland Chang, Shahriar Mobashery, Mijoon Lee
Abstract: Disclosed herein are polypeptides, polynucleotides encoding, cells and organisms comprising novel DNA-binding domains, including TALE DNA-binding domains. Also disclosed are methods of using these novel DNA-binding domains for modulation of gene expression and/or genomic editing of endogenous cellular sequences.
Type:
Grant
Filed:
October 28, 2013
Date of Patent:
April 26, 2016
Assignee:
Sangamo BioSciences, Inc.
Inventors:
Philip D. Gregory, Jeffrey C. Miller, David Paschon, Edward J. Rebar, Siyuan Tan, Fyodor Urnov, Lei Zhang
Abstract: The present invention relates to the use of a Somatostatin (SRIF) analog which has a high binding affinity to human SSTR1,2,3,5, or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical composition for the control of hypoglycemia.
Abstract: The present invention is directed to an inventive polymeric carrier molecule according to generic formula (I) and variations thereof, which allows for efficient transfection of nucleic acids into cells in vivo and in vitro, a polymeric carrier cargo complex formed by a nucleic acid and the inventive polymeric carrier molecule, but also to methods of preparation of this inventive polymeric carrier molecule and of the inventive polymeric carrier cargo complex. The present invention also provides methods of application and use of this inventive polymeric carrier molecule and the inventive polymeric carrier cargo complex as a medicament, for the treatment of various diseases, and in the preparation of a pharmaceutical composition for the treatment of such diseases.
Abstract: The present invention provides a biocompatible polymer conjugated to FVIIa via one or more cysteine residues, suitably via a linker across a reduced disulphide bond in FVIIa, and pharmaceutical compositions comprising such conjugated forms of FVIIa.
Abstract: The present invention provides novel amino-lipids, compositions comprising such amino-lipids and methods of producing them. In addition, lipid nanoparticles comprising the novel amino-lipids and a biologically active compound are provided, as well as methods of production and their use for intracellular drug delivery.
Type:
Grant
Filed:
February 12, 2014
Date of Patent:
March 8, 2016
Assignee:
AXOLABS GMBH
Inventors:
Rainer Constien, Anke Geick, Philipp Hadwiger, Torsten Haneke, Ludger Markus Ickenstein, Carla Alexandra Hernandez Prata, Andrea Schuster, Timo Weide
Abstract: The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound.