Patent classifications
C07K5/097
COMPOUNDS HAVING TRIPLE ACTIVITIES OF THROMBOLYSIS, ANTITHROMBOTIC AND RADICAL SCAVENGING
The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the formula I shown below:
##STR00001##
wherein the definitions of T, Q, R.sub.1 and R.sub.2 are described herein. The compound of the present invention simultaneously has triple functions of thrombolysis, free radical scavenging and thrombus-targeting/antithrombosis. The present invention also relates to a pharmaceutical composition comprising the compound, and a preparation method and a nanostructure of the compound.
PEPTIDE INHIBITORS OF TIGHT JUNCTION PERMEABILITY
Novel compounds and methods for the inhibition of biological barrier permeability and for the inhibition of peptide translocation across biological barriers are identified. Assays for determining modulators of biological barrier permeability and for peptide translocation across biological barriers are provided. Methods for treating diseases relating to aberrant biological barrier permeability and peptide translocation across biological barriers are provided. Such diseases include celiac disease, necrotizing enterocolitis, diabetes, cancer, inflammatory bowel diseases, asthma, COPD, excessive or undesirable immune response, gluten sensitivity, gluten allergy, food allergy, rheumatoid arthritis, multiple sclerosis, immune-mediated or type 1 diabetes mellitus, systemic lupus erythematosus, psoriasis, scleroderma and autoimmune thyroid diseases.
Neuropeptide S receptor (NPSR) agonists
Neuropeptide S receptor agonists are provided. The NPS agonists include trimeric, tetrameric, pentameric or hexameric peptidomimetic analogs exhibiting affinity for and activity at the neuropeptide S receptor. The peptidomimetic molecules may be useful in the treatment of disorders, syndromes and conditions mediated by modulation of the neuropeptide S receptor such as substance abuse, narcolepsy, insomnia, obesity, cognitive decline, dementia, Alzheimer's disease, panic disorder, generalized anxiety, PTSD, phobias, schizophrenia and as supportive medication during any kind of cessation program in cognitive behavioral therapy, such as drug addiction, eating disorders and gambling.
PROCESS FOR THE PREPARATION OF CYCLIC DEPSIPEPTIDES
Processes for preparing compounds of Formula (1) and Formula (2) are described, wherein X, Y, Z, R.sub.1-R.sub.7, L and n are defined herein. Intermediates useful in the preparation of the compounds of Formula (1) and Formula (2) are also described.
##STR00001##
Compositions comprising cyclic peptides derived from an A-beta peptide
The disclosure pertains to methods of treating or preventing a disease or condition associated with and/or induced by soluble A-beta oligomer such as Alzheimer's disease by administering to a subject in need thereof conformation specific and/or selective antibodies or binding fragments thereof and related products.
COMPOUNDS HAVING TRIPLE ACTIVITIES OF THROMBOLYSIS, ANTITHROMBOTIC AND RADICAL SCAVENGING
The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the formula I shown below:
##STR00001##
wherein the definitions of T, Q, R.sub.1 and R.sub.2 are described herein. The compound of the present invention simultaneously has triple functions of thrombolysis, free radical scavenging and thrombus-targeting/antithrombosis. The present invention also relates to a pharmaceutical composition comprising the compound, and a preparation method and a nanostructure of the compound.
PYRROLIDINE CARBOXAMIDO DERIVATIVES AND METHODS FOR PREPARING AND USING THE SAME
Pyrrolidine carboxamido derivatives, optical isomers thereof, and salts thereof that are able to prevent, improve, and/or treat inflammatory conditions, including inflammatory bowel disease, and methods for preparing and using the same are provided.
MPRO CYSTEINE PROTEASE INHIBITORS
Described herein are Mpro cysteine protease inhibitors and methods of utilizing such inhibitors in the treatment of diseases, disorders, or conditions. Also described herein are pharmaceutical compositions containing such compounds.
Bioactive Collagen Peptides, Method Of Production Thereof, And Use Thereof
The invention provides a composition comprising one or more bioactive peptides from collagen hydrolysate and use thereof for reducing joint and/or bone pain such as in arthritis or osteoarthritis. The invention also provides a use of the composition for inhibiting the activity and/or expression of osteoclasts, increasing the activity and/or expression of osteoblasts, or for the treatment and/or prevention of osteoclast-related diseases. The invention also provides a method for generating bioactive peptides from collagen hydrolysate in vitro.
Collagen mimics
Novel collagen mimics are disclosed with a tripeptide unit having the formula (Xaa-Yaa-Gly).sub.n, where one of the positions Xaa or Yaa is a bulky, non-electron withdrawing proline derivative. By substituting a proline derivative at either the Xaa or Yaa position in the native collagen helix, the stability of the helix is increased due solely to steric effects relative to prior known collagen-related triple helices. Methods are also disclosed for making the novel collagen mimics.