Disclosed herein, inter alia, are methods of use and composition of novel inhibitors that target the Smac binding site of a variety of inhibitor of apoptosis proteins that contain a Bir domain, including XIAP, cIAP1, cIAP2, or other IAP proteins.

The present invention provides .sup.18F-labeled amino acids or derivatives thereof having formula (I) and methods of making same, which can be suitable for PET imaging: ##STR00001##

The invention provides a new oligopeptide linker intermediate and a preparation method thereof. The preparation method of the oligopeptide intermediate is easily carried out under mild reaction conditions, and since almost no side reactions occur in the reaction, the method produces a high-purity product with fewer impurities and easy to be purified, achieving unexpected technical effects.

Provided are a cyclic peptide compound simulating a natural product structure- and a method for preparation thereof. The method is: the compound of formula I, a divalent palladium catalyst, and a silver salt undergoing an intramolecular arylation in a solvent under heating and stirring to construct a cyclic peptide, to generate the compound of formula II, in which the arylation sites are diverse, and can be extended to the side chain γ-position methyl or methylene of the majority hydrophobic amino acids to perform intramolecular arylation, thus overcoming the previous defect of the restriction of the types of selectable amino acids, and effectively constructing a novel aromatic ring-supported cyclic peptide compound. The aromatic ring support structure can form a novel 3D structure similar to a natural product, and provide a very favorable support for the subsequent construction of a cyclic peptide molecular library and high-throughput drug screening.

##STR00001##

Certain embodiments of the invention provide a compound of formula (I):

R.sup.1—C(═O)—W—X—Y—Z—N(R.sup.2).sub.2   (I)

or a salt thereof, wherein R.sup.1, R.sup.2, W, X, Y and Z are as defined herein, as well as methods of use thereof.

The present invention provides for a bio-mimetic polymer capable of catalyzing or mineralizing calcium ion and phosphate ions into an apatite.

The present disclosure relates to methods of preparing and crystallizing β-turn cyclic peptidomimetic salts of formula I: ##STR00001##
where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.10, X, Y and n are as defined in the specification. The present disclosure provides a more efficient route for preparing a crystalline form of a β-turn cyclic peptidomimetic compounds and salts thereof.

Methods for the synthesis of arginine-containing peptides are provided. The methods include a deprotection step that minimizes the transfer of by-products deriving from cleaved sulfonyl-5 based side chain protecting groups from arginine to amino acids carrying electron rich side chains.

The present disclosure relates to methods of preparing and crystallizing β-turn cyclic peptidomimetic salts of formula I:

##STR00001## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.10, X, Y and n are as defined in the specification.

The present disclosure provides a more efficient route for preparing a crystalline form of a β-turn cyclic peptidomimetic compounds and salts thereof.

The present disclosure relates to an in vitro method for enhancing engraftment of neurosensory precursor cell comprising the step of contacting an isolated neurosensory precursor cell prior to a transplantation in a subject in need thereof, with a gem-difluorinated C-glycopeptide compound of general formula I, or a pharmaceutically acceptable base, addition salt with an acid, hydrate or solvate thereof: ##STR00001##