Patent classifications
A61K49/0021
SUBCUTANEOUS AND INTRAMUSCULAR ADMINISTRATION OF PYRAZINE COMPOUNDS
The present disclosure relates to methods for determining the renal glomerular filtration rate or assessing the renal function in a patient in need thereof. The method comprises administering, subcutaneously or intramuscularly, a pyrazine compound of Formula I to a patient, wherein the administration produces a plasma concentration of the compound that is substantially similar to a plasma concentration produced by intravenous administration of an identical amount of the compound; and monitoring the rate in which the kidneys of the patient eliminate the pyrazine from the systemic circulation of the patient. The pyrazine compound fluoresces when exposed to electromagnetic radiation which may be detected using one or more sensors. The rate in which the fluorescence decreases in the patient may be used to calculate the renal glomerular filtration rate in the patient.
Library of pH responsive polymers and nanoprobes thereof
The present disclosure relates to polymers which contain a hydrophobic and hydrophilic segment which is sensitive to pH. In some aspects, the polymers form a micelle which is sensitive to pH and results in a change in fluorescence based upon the particular pH. In some aspects, the disclosure also provides methods of using the polymers for the imaging of cellular or extracellular environment or delivering a drug.
a-SYNUCLEIN AGGREGATE BINDING AGENT AND IMAGING METHOD
The present invention provides an α-synuclein aggregate binding agent that has high binding selectivity for an α-synuclein aggregate.
The α-synuclein aggregate binding agent contains a compound represented by a formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof:
##STR00001##
in the formula (I), R.sub.1 and R.sub.2 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, acyl, and hydroxyalkyl; R.sub.3 is hydrogen or halogen; the ring A is a benzene or pyridine ring; the ring B is represented by the following formula (i) or (ii):
##STR00002##
R.sub.4 and R.sub.5 are each independently selected from the group consisting of hydrogen, hydroxy, alkoxy, haloalkoxy, halohydroxyalkoxy, and aminoalkyl.
FLUORESCENT PYRAZINE DERIVATIVES AND METHODS OF USING THE SAME IN ASSESSING RENAL FUNCTION
The present invention relates to pyrazine derivatives such as those represented by Formulas I and II. X.sup.1 to X.sup.4 formulas I and II may be characterized as electron withdrawing groups, white Y.sup.1 to Y.sup.4 of Formulas I and II may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing organ (e.g., kidney) function. In a particular example, an effective amount of a pyrazine derivative that is capable of being renally cleared may be administered into a patient's body. The pyrazine derivative may capable of one or both absorbing and emanating spectral energy of at least about 400 nm (e.g., visible and/or infrared light). At least some of the derivative that is in the body may be exposed to spectral energy and, in turn, spectral energy may emanate from the derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient.
##STR00001##
METHODS AND COMPOSITION FOR DYE-BASED ENCODING AND QUANTIFICATION
Fluorescently tagged nucleotides have a wide array of uses; however, methods of quantifying said nucleotides are lacking. The present invention features compositions and methods for quantifying cellular dyes within a sample. Compositions described herein comprise an oligonucleotide barcode conjugated to a cellular dye.
Near-infrared fluorescent molecule active targeting folate receptor and preparation method thereof
The present disclosure relates to the fields of near-infrared surgical navigation fluorescent molecules, cell marker imaging and so on, and in particular discloses an active targeting near-infrared fluorescent small molecule structure and a preparation method thereof. The present disclosure prepares the active targeting near-infrared fluorescent small molecule with pemetrexed disodium and derivatives thereof as active targeting groups by utilizing an organic total synthesis method. Such active targeting near-infrared fluorescent molecule has the advantages of high active targeting property, strong specificity, good water solubility, high fluorescence quantum yield and so on.
Programmable polymeric drugs
Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): ##STR00001##
or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, L, L.sup.1, L.sup.2, L.sup.3, M and n are as defined herein. Methods associated with preparation and use of such compounds is also provided.
APPLICATION OF DIPYRRINATO-IRIDIUM COMPLEXES IN ANTI-TUMOR AND ANTI-BACTERIAL THERAPY
Biologically active compounds and their methods of preparation are provided that may be used as photosensitizers for diagnostic and therapeutic applications, particularly for PDT of cancer, infectious and other hyperproliferative diseases, fluorescence diagnosis and PDT treatment of non-tumorous indications such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological otorhinolanyingology disorders, ophthalmological or urological disorders. As the compounds exhibit also toxicity against targets (tumor cells, bacteria, inflammation-related cells) without light these biologically active compounds may also be used for the light-independent treatment of such indications. Embodiments also include methods to synthesize iridium(III) complex structures incorporating a substituted 2,3,5,6-tetrafluorophenyl-dipyrromethene (2,3,5,6-tetrafluorophenyldipyrrin) unit or a substituted 3-mtrophenyl-dipyrromethene (3-nitroplienyl-dipyrritt) unit. Amphiphilic compounds with increased anti-tumour and anti-bacterial efficacy are also provided. Specifically, this is achieved by substitution with bromine atoms and sugar moieties.
CELL ACTIVATABLE IRON CHELATORS
Provided herein are compounds of the formula (I): wherein the variables are as defined herein. Pharmaceutical compositions of the compounds are also provided. In some aspects, these compounds may be used for the treatment of diseases or disorders, such as a bacterial infection.
##STR00001##
COMPOSITIONS AND METHODS FOR ASSESSING EYE VASCULATURE
Compositions and methods for assessing blood vessels and organs of the body are disclosed herein, specifically methods for assessing the vasculature of the eye.