Patent classifications
C07K5/0804
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.
PEPTIDE DERIVATIVE WITH COLLAGENASE INHIBITORY ACTIVITY, AND USE THEREOF
The present invention relates to a peptide derivative, having collagenase inhibitory activity, or a use thereof and has the effects of increasing a percutaneous absorption rate, inhibiting collagenase activity, and reducing wrinkles.
Methods of preparing cytotoxic benzodiazepine derivatives
The invention relates to novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.
INHIBITORS OF IAP
Novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies and have the general formula I:
##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as described herein.
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.
Inhibitors of IAP
Novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies and have the general formula I: ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as described herein.
METHODS OF PREPARING CYTOTOXIC BENZODIAZEPINE DERIVATIVES
The invention relates to novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.
METHODS OF PREPARING CYTOTOXIC BENZODIAZEPINE DERIVATIVES
The invention relates to novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
Trifluoromethylpropanamide derivatives as HTRA1 inhibitors
The invention provides novel compounds having the general formula (I) ##STR00001##
wherein R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.3, R.sup.8, R.sup.10, R.sup.11 and R.sup.23 are as described herein, compositions including the compounds and methods of using the compounds.