C07K5/0606

PSMA-targeted NIR dyes and their uses
11484607 · 2022-11-01 · ·

The present disclosure relates to prostate specific membrane antigen (PSMA) targeted compounds conjugated to near-infra red (NIR) dyes and methods for their therapeutic and diagnostic use. More specifically, this disclosure provides compounds and methods for diagnosing and treating diseases associated with cells and/or vasculature expressing prostate specific membrane antigen (PSMA), such as prostate cancer and related diseases. The disclosure further describes methods and compositions for making and using the compounds, methods incorporating the compounds, and kits incorporating the compounds.

Nitrogen-containing compound or salt thereof, or metal complex thereof

The present invention provides a compound represented by the formula (1) or a salt thereof, or a complex of the compound or the salt with a metal, in the formula (1), A.sup.1 represents a chelate group; R.sup.1 represents a hydrogen atom or the like; R.sup.2 represents a hydrogen atom or the like; and Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4, and Z.sup.5 are the same or different and each represent a nitrogen atom or CR.sup.3 or the like wherein R.sup.3 represents a hydrogen atom or an optionally substituted C.sub.1-6 alkyl group or the like; L.sup.1 represents a group represented by the formula (3) wherein R.sup.13, R.sup.14, R.sup.15, and R.sup.16 are the same or different and each represent a hydrogen atom or the like; L.sup.2 represents an optionally substituted C.sub.1-6 alkylene group; and L.sup.3 represents an optionally substituted C.sub.1-6 alkylene group. ##STR00001##

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.

Skin treatment devices and methods with pre-stressed configurations

Devices, bandages, kits and methods are described that can control or regulate the mechanical environment of a wound to ameliorate scar and/or keloid formation. The mechanical environment of a wound includes stress, strain, and any combination of stress and strain. The control of a wound's mechanical environment can be active, passive, dynamic, or static. The devices are configured to be removably secured to a skin surface in proximity to the wound site and shield the wound from endogenous and/or exogenous stress.

Process for preparing tubulysins

The invention described herein pertains to processes for preparing tubulysins and derivatives thereof. The invention described herein also pertains to processes for preparing tubulysin conjugates. The invention described herein also pertains to processes for preparing intermediates for preparing tubulysin conjugates. In one step, the alpha-thiazolyl alcohol is protected with triethylsilyl chloride in the presence of imidazole in an aprotic solvent.

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.

COMPUNDS FOR ENZYME INHIBITION
20170260230 · 2017-09-14 ·

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.

Metal compound having phase transformation and method of preparing the same
11396453 · 2022-07-26 · ·

The present invention relates to a metal phase transformation compound and a method for preparing the same.

COMPOSITIONS AND METHODS FOR THE DELIVERY OF NUCLEIC ACIDS
20220226362 · 2022-07-21 ·

A compound comprising formula (I):

##STR00001## wherein R.sup.1 is an akylamino group or a group containing at least one aromatic group; R.sup.2 and R.sup.3 are independently an aliphatic group or hydrophobic group; R.sup.4 and R.sup.5 are independently H, a substituted or unsubstituted akyl group, an akenyl group, an acyl group, an aromatic group, polymer, a targeting group, or a detectable moiety; a, b, c, and d are independently an integer from 1 to 10; and pharmaceutically acceptable salts thereof.

METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease