C07K5/0827

Agents targeting inhibitor of apoptosis proteins

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.

PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII

The present invention provides compounds of formula (I)

##STR00001## wherein X.sup.1 to X.sup.8 and R.sup.1 to R.sup.8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.

18F labeled amino acids, derivatives thereof and method of making same

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##

Peptide macrocycles against <i>Acinetobacter baumannii</i>

The present invention provides compounds of formula (I) ##STR00001## wherein X, L.sup.1 and R.sup.1 to R.sup.10 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.

OLIGOPEPTIDE LINKER INTERMEDIATE AND PREPARATION METHOD THEREOF
20230128167 · 2023-04-27 · ·

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.

Cyclic Peptide Compound Simulating Natural Product Structure, And Method For Preparation Thereof
20220315623 · 2022-10-06 · ·

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##

PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII

The present invention provides compounds of formula (I)

##STR00001## wherein X.sup.1 to X.sup.8 and R.sup.1 to R.sup.8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.

COMPOUNDS FOR PROTEASOME ENZYME INHIBITION
20220267372 · 2022-08-25 ·

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Nn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Peptoids useful for the mineralization of apatite

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

Peptidomimetics for the treatment of coronavirus and picornavirus infections

Compounds, compositions and methods for preventing, treating or curing a coronavirus, picornavirus, and/or hepeviridae virus infection in human subjects or other animal hosts. Specific viruses that can be treated include enteroviruses. In one embodiment, the compounds can be used to treat an infection with a severe acute respiratory syndrome virus, such as human coronavirus 229E, SARS, MERS, SARS-CoV-1 (OC43), and SARS-CoV-2. In another embodiment, the methods are used to treat a patient co-infected with two or more of these viruses, or a combination of one or more of these viruses and norovirus.