Patent classifications
A61K47/558
PHOSPHINATE ESTER-CONTAINING DYES HAVING TUNABLE PROPERTIES AND METHODS OF MAKING THE SAME
In one aspect, the disclosure relates to xanthene-, thiazine-, and oxazine-based dyes containing a phosphinate ester group and having near-infrared (NIR) absorption and methods of making the same. The fluorescence lifetimes and stabilities of the dyes can be tuned by modifying the molecule cores, making them suitable for a variety of chemical labeling, imaging, and other theranostic applications. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
ULTRASOUND METHOD
A method of regulating at least one cellular process in one or more cells by exposing the one or more cells to ultrasound, characterised in that the method comprises either (a) introducing into the one or more cells a construct comprising a regulatory transgene capable of regulating the at least one cellular process operably linked to a light-inducible control sequence and (b) inducing the expression of the regulatory transgene using sonoluminescence (SL) or sonochemiluminescence (SCL); or (i) contacting the one or more cells with one or more light-sensitive proteins capable of regulating the at least one cellular process and (ii) regulating the function of the one or more proteins using sonoluminescence or sonochemiluminescence.
NANOPARTICLE CONJUGATES
Conjugates comprising a drug, cell or biological molecule bound to a photoluminescent polymer nanoparticle, in particular a cross-linked polyfluorene nanoparticle, are described herein, as well as their methods of manufacture and their uses in biological imaging and sensing applications.
Coumarin dyes and conjugates thereof
The present invention describes novel 7-alkylamino-3-(thienyl) coumarin fluorescent dyes of formula (I) ##STR00001## These dyes are water soluble, can be excited by the 405 nm excitation source and exhibit a large Stokes shift (80 nm). Furthermore, the dyes possess a reactive group for the labeling of biomolecules or other analytes.
Treatment of proliferative disorders with a chemiluminescent agent
Methods employing chemiluminescent agents as therapeutically active agents in the treatment of proliferative disorders are disclosed. The chemiluminescent agents are used in the disclosed method without a therapeutically effective amount of a photosensitizer. Novel chemiluminescent agents having the general formula: ##STR00001##
are also disclosed, wherein X, Y, Z, R.sub.3 and R.sub.5-R.sub.9 are as defined herein.
Small Molecule Drug Conjugates
A binding moiety (B) for Carbonic Anhydrase IX (CAIX), the binding moiety comprising:
##STR00001##
The binding moiety is univalent, bivalent, or multivalent. A targeted therapeutic agent may comprise the binding moiety. The invention also includes a method for treating a disease expressing elevated levels of CAIX by administering the targeted therapeutic agent.
Activatable fluorogenic compounds and uses thereof as near infrared probes
Novel fluorogenic compounds designed such that upon a chemical event, compounds capable of emitting NIR light are generated, are disclosed. The compounds comprise two or more acceptor-containing moieties and a cleavable donor-containing moiety, being in complete pi-electrons conjugation and being such that no delocalization of pi-electrons is enabled. Also disclosed are fluorescent compounds generated upon subjecting the fluorogenic compounds to a chemical event (e.g., deprotonation). Also disclosed are uses of the fluorogenic compounds as NIR probed with a Turn-ON mechanism in monitoring presence and/or level of various analytes.
BIOORTHOGONAL REACTION OF AN AMINE N-OXIDE AND A BORON AGENT
Methods for chemoselective modification of a target molecule comprising an amine N-oxide in a biological sample are provided. Aspects of the methods include selectively reacting the amine N-oxide group of the target molecule with a boron agent, where the reacting reduces the amine N-oxide to an amine to produce a modified target molecule. Modification of the target molecule using the subject methods may produce an activated target molecule, e.g., a detectable or bioactive. In some cases, chemoselective modification leads to cleavage of the modified target molecule to produce a first target fragment and a second target fragment. Also provided are compositions useful in practicing various embodiments of the subject methods.
##STR00001##
Metal-salen complex compound, local anesthetic and antineoplastic drug
A metal-salen complex compound, which exhibits excellent noninvasiveness and can be efficiently transferred to an affected site, a local anesthetic containing this metal-salen complex compound, and an antineoplastic drug containing this metal-salen complex compound are provided. Regarding the metal-salen complex compound, a metal atom part in each of two molecules of a metal-salen complex or a derivative of the metal-salen complex is dimerized via water, and the metal-salen complex compound is mixed with a base to produce an ointment.
Small molecule drug conjugates
A binding moiety (B) for Carbonic Anhydrase IX (CAIX), the binding moiety comprising: ##STR00001##
The binding moiety is univalent, bivalent, or multivalent. A targeted therapeutic agent may comprise the binding moiety. The invention also includes a method for treating a disease expressing elevated levels of CAIX by administering the targeted therapeutic agent.