Abstract: Disclosed is a method of synthesizing linaclotide through completely selective formation of three disulfide bonds, comprising the steps of: 1) synthesizing linaclotide precursor resin through solid-phase synthesis; 2) forming the first disulfide bond through solid phase oxidation; 3) forming the second disulfide bond through liquid phase oxidation; and 4) deprotecting methyl in the methyl-protected cysteine, and oxidatively coupling the third disulfide bond to obtain linaclotide. The method has mild reaction conditions with low cost, high yield and high purity product, is a simple and stable process and is suitable for large-scale production.
Abstract: The present invention relates to a new pharmaceutical composition containing nicotinic acid, nicotinamide, tryptophanor related compounds for positively influencing the intestinal microbiota. In certain embodiments, the pharmaceutical composition is partially or entirely released into the small intestine or large intestine.
Abstract: New gelatinase inhibitors, processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy and/or prophylaxis of conditions wherein inhibition of gelatinases is useful such as epilepsy, schizophrenia, Alzheimer disease, autism (in particular associated to fragile X syndrome), mental retardation, mood disorders such as bipolar disorders, depression, vascular diseases such as ischemic stroke and atherosclerosis, inflammatory diseases such as multiple sclerosis, rheumatoid arthritis and inflammatory bowel disease, drug addiction, neuropathic pain, lung diseases such as asthma and chronic obstructive pulmonary disease, cancer and sepsis.
Type:
Grant
Filed:
November 15, 2016
Date of Patent:
September 17, 2019
Assignee:
Iproteos S.L
Inventors:
Roger Prades Cosano, Jésus Seco Moral, María Teresa Tarragó Clua
Abstract: The present invention provides protease-resistant peptides, methods of making such peptides, as well as compositions comprising protease-resistant peptides and method of treatment utilizing such peptides. A combination of lipidation of certain amino acid residues and substitution of alpha-methyl functionalized amino acids for natural amino acids has been determined to produce protease-resistant peptides.
Abstract: Disclosed herein are heat-stable dry powders which include peptides or protein such as oxytocin for use as a pharmaceutical composition. The composition is highly stable at increased temperatures and relatively high humid environments, and are intended for storage at room temperature with an improved shelf-life. In particular, the dry powders are intended for inhalation, however, other routes of administration can be used when reconstituted in solution.
Type:
Grant
Filed:
January 31, 2018
Date of Patent:
September 17, 2019
Assignee:
Mannkind Corporation
Inventors:
Karine Fabio, Joseph J. Guarneri, Kieran Curley, Marshall L. Grant, Andrea Leone-Bay
Abstract: The present invention relates to methods for detecting protein S-sulfinylation and S-sulfinylation within thiol groups in proteins, metabolites, or materials.
Type:
Grant
Filed:
February 17, 2017
Date of Patent:
September 10, 2019
Assignee:
The Regents of the University of Michigan
Abstract: Disclosed herein are diketopiperazine microparticles having high capacity for adsorbing a drug or active agent. In particular, the diketopiperazine microparticle are formed using fumaryl diketopiperazine and can comprise a drug in large doses for the treatment of disease or disorders by pulmonary delivery via oral inhalation.
Type:
Grant
Filed:
October 4, 2018
Date of Patent:
August 13, 2019
Assignee:
MannKind Corporation
Inventors:
Marshall Grant, Paul Menkin, Grayson W. Stowell
Abstract: Methods are provided for drying a particle. Specifically, there is provided a spray-dried diketopiperazine-insulin particle formulation having improved aerodynamic performance and in which the active agent is more stabile and efficiently delivered as compared to that of the lyophilized diketopiperazine-insulin formulation. The dry powders have utility as pharmaceutical formulations for pulmonary delivery.
Abstract: Fusion proteins containing active agonist or antagonist fragments of parathyroid hormone (PTH) and parathyroid hormone related peptide (PTHrP) coupled to a collagen-binding domain are presented. The fusion proteins can be used to promote bone growth, to promote hair growth, to prevent cancer metastasis to bone, to promote immune reconstitution with a bone marrow stem cell transplant, to promote mobilization of bone marrow stem cells for collection for autologous stem cell transplant, and to treat renal osteodystrophy. Pharmaceutical agents comprising a collagen-binding polypeptide segment linked to a non-peptidyl PTH/PTHrP receptor agonist or antagonist are also presented.
Type:
Grant
Filed:
January 16, 2019
Date of Patent:
July 23, 2019
Assignees:
The Board of Trustees of the University of Arkansas, Ochsner Clinic Foundation, National University Corporation Kagawa university
Inventors:
Robert C. Gensure, Joshua Sakon, Osamu Matsushita, Tulasi Ponnapakkam
Abstract: The present invention relates to complexes of transcription factor decoys, their delivery to bacteria and their formulation. In particular, the present invention resides in an antibacterial complex comprising a nucleic acid sequence and one or more delivery moieties selected from quaternary amine compounds; bis-aminoalkanes and unsaturated derivatives thereof, wherein the amino component of the aminoalkane is an amino group forming part of a heterocyclic ring; and an antibacterial peptide.
Abstract: The present invention generally relates to systems and methods for the transdermal delivery of the heptapeptide ZW1. In some aspects, ZW1 may be contained with a composition comprising a lecithin, such as phosphatidylcholine. In certain embodiments, the lecithin is present in liposomes, micelles, liquid crystals, or other configurations. The composition can take the form of a gel, a cream, a lotion, an ointment, a solution, a solid “stick,” etc., that can be rubbed or sprayed onto the skin. Other aspects of the present invention are generally directed to methods of making or using such compositions, methods of promoting such compositions, kits including such compositions, or the like.
Abstract: A method for treating a patient suffering from one of septic shock, acute kidney injury, severe hypotension, cardiac arrest, and refractory hypotension, but not from myocardial infarction, is provided. The method includes administering a therapeutically effective dose of Angiotensin II, or Ang II, to the patient.
Type:
Grant
Filed:
August 7, 2018
Date of Patent:
July 2, 2019
Assignee:
The George Washington University a Congressionally Chartered Not-for-Profit Corporation
Abstract: The invention relates to granules and pharmaceutical compositions comprising a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and a lubricant obtained by mixing hereof for more than 5 minutes prior to granulation as well as processes for their preparation and use thereof in medicine.
Abstract: An object of the present invention is to provide methods for preventing or treating a steroid-resistant or steroid-dependent inflammatory bowel disease. The object can be achieved by a method for preventing or treating a steroid-resistant or steroid-dependent inflammatory bowel disease in a patient in need of the prevention or treatment of the inflammatory bowel disease, comprises administering an effective amount of adrenomedullin, a modified product thereof having an activity of suppressing steroid-resistant or steroid-dependent inflammation, or a salt thereof having an activity of suppressing steroid-resistant or steroid-dependent inflammation, to the patient.
Type:
Grant
Filed:
March 3, 2017
Date of Patent:
July 2, 2019
Assignee:
University of Miyazaki
Inventors:
Kazuo Kitamura, Shinya Ashizuka, Haruhiko Inatsu, Toshihiro Kita
Abstract: The embodiments include methods of improving sexual function in a male with benign prostatic hyperplasia (BPH), using compositions containing compounds based on small peptides and a pharmaceutically acceptable carrier. The method includes, but is not limited to, administering the compounds intramuscularly, orally, intravenously, intraprostatically, intrathecally, intratumorally, intranasally, topically, transdermally, etc., either alone or conjugated to a carrier to a male in need thereof.
Abstract: C1q is shown to be expressed in neurons, where it acts as a signal for synapse elimination. Methods are provided for protecting or treating an individual suffering from adverse effects of synapse loss. These findings have broad implications for a variety of clinical conditions, including Alzheimer's disease.
Type:
Grant
Filed:
November 11, 2016
Date of Patent:
June 25, 2019
Assignee:
The Board of Trustees of the Leland Stanford Junior University
Abstract: A method for treating a patient suffering from one of septic shock, acute kidney injury, severe hypotension, cardiac arrest, and refractory hypotension, but not from myocardial infarction, is provided. The method includes administering a therapeutically effective dose of Angiotensin II, or Ang II, to the patient.
Type:
Grant
Filed:
March 15, 2018
Date of Patent:
June 18, 2019
Assignee:
The George Washington University a Congressionally Chartered Not-for-Profit Corporation
Abstract: The present invention is directed to a novel class of antimicrobial agents called ?-AApeptides. The current invention provides various categories of ?-AApeptides, for example, linear ?-AApeptides, cyclic ?-AApeptides, and lipidated ?-AApeptides. ?-AApeptides of the current invention are designed to exert antimicrobial activity while being stable and non-toxic. ?-AApeptides also do not appear to lead to the development of microbial resistance in treated microorganisms. Thus, the disclosed ?-AApeptides can be used for the treatment of various medical conditions associated with pathogenic microorganisms.
Abstract: The invention relates to a new bicyclic lipolantipeptide, representing a new class of lantipeptide, and salts thereof, their preparation from a culture of a Microbacterium arborescens, and their use as antimicrobial agent in the prevention and treatment of infections in humans, animals or plants.
Type:
Grant
Filed:
July 1, 2016
Date of Patent:
June 4, 2019
Assignee:
DEINOVE
Inventors:
Josef Aszodi, Denis Carniato, Dominique Le Beller, Guillaume Lesquame, Marie-Helene Quernin