Disclosed herein are ETBR antagonist compounds, pharmaceutical compositions thereof, methods for treating cancers, and methods of forming tertiary lymphoid organs.

A new composition capable of preventing adhesion of pollutants by forming a film on the skin or the hair surface and promoting skin permeation as well as preventing the skin and the hair surface from being polluted by the substance. The composition characterized by containing a sucrose ester and a lipidic peptide in which a peptide moiety formed of at least two identical or different amino acid repeats is bounded to a lipidic moiety having a C.sub.10-C.sub.24 aliphatic group.

The invention relates to novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.

A peptide of 3 to 8 amino acid residues may include the sequence:

X.sub.mZ.sub.nPU.sub.q(I),

wherein P is proline, Z is independently a lysine (K) and/or asparagine (N) residue, X is an amino acid residue independently selected from isoleucine (I), phenylalanine (F), methionine (M), alanine (A), valine (V), tryptophan (W), tyrosine (Y), histidine (H), cysteine (C), arginine (R), glutamine (Q) and serine (S), U is an amino acid residue independently selected from arginine (R), glycine (G), serine (S), lysine (K), threonine (T), leucine (L), asparagine (N), histidine (H) and isoleucine (I), m is 0, 1, 2 or 3, n is 1 or 2, and q is 0, 1, 2 or 3.

The present invention relates to novel compounds which effectively inhibit the melanin synthesis in human melanocytes and are thus suitable for the treatment of senile lentigines, for smoothening skin color irregularities and/or for lightening natural skin color.

The invention relates to novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.

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.

The present disclosure relates to bifunctional compounds, which find utility as modulators of focal adhesion kinase (FAK) or protein tyrosine kinase 2 (PTK2). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

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.

The invention relates to novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.