Patent classifications
C07K5/065
PROCESS FOR THE LIQUID PHASE SYNTHESIS OF H-INP-(D)BAL-(D)TRP-PHE-APC-NH2, AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
The present invention provides a process for the liquid phase synthesis of the Ghrelin analog H-Inp-(D)Bal-(D)Trp-Phe-Apc-NH2 (SEQ ID NO: 1, Formula (I)), pharmaceutically acceptable salts thereof.
Antimicrobial compounds and/or modulators of microbial infections and methods of using the same
Some embodiments include compounds that can inhibit the growth of bacterial and/or inhibit or reduce microbial infections caused by one or more microorganisms (e.g., Pseudomonas aeruginosa and Cryptococcus neoformans) and methods of using these compounds to treat microbial infection and outbreaks and/or to reduce the formation of biofilms. Other embodiments include synthesis of the compounds that can inhibit the growth of one or more microorganisms and/or inhibit or reduce microbial infections.
Derivatives of 1-amino-2-cyclobutylethylboronic acid
The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
COMPUNDS FOR ENZYME INHIBITION
Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. 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. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.
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.
PEPTIDOMIMETICS FOR THE TREATMENT OF NOROVIRUS INFECTION
The present invention is directed to compounds, compositions and methods for preventing, treating or curing Norovirus infection in human subjects or other animal hosts.
FAP-ACTIVATED PROTEASOME INHIBITORS FOR TREATING SOLID TUMORS
Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.
PIEZOELECTRIC PEPTIDE-BASED MATERIALS AND PIEZOELECTRIC DEVICES CONTAINING SAME
A piezoelectric transducer is provided herein, comprising a three-dimensional structure made of a plurality of peptides, the peptides being self-assembling and the structure being piezoelectric, wherein at least a portion, or each, of said plurality of peptides comprises peptides of 2 to 10 amino acid residues, provided that the plurality of peptides is not consisted of a plurality of Phe-Phe dipeptides. Further described herein are peptides having an amino acid sequence Hyp-Phe-Phe, Boc-Dip-Dip, (L)Trp-(D)Trp or (D)Trp-(L)Trp, as well as three-dimensional structures comprising such peptides.
Tripeptide compound, preparation method therefor, and application thereof
Provided are a tripeptide compound, a preparation method therefor, and an application thereof. The structure of the related compound is represented by formula (I). The provided compound has angiotensin converting enzyme inhibiting bioactivity, and the compound and a pharmaceutical composition thereof play a role in preventing and treating hypertension and other cardiocerebral vascular system diseases.
IBAT inhibitors for the treatment of liver diseases
The present invention regards specific IBAT inhibitors useful in the prophylaxis and/or treatment of a liver disease. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.