Patent classifications
C07D487/00
Quinone-masked probes as labeling reagents for cell uptake measurements
Provided are labeling reagents and methods of using the reagents for cell uptake measurements. The labeling reagents can be quinone-masked probes including fluorophores and/or luminophores.
Polymers based on naphthodiones
The present invention relates to polymers comprising one or more (repeating) unit(s) of the formula (I), and compounds of formula (III), wherein Y, Y.sup.15, Y.sup.16 and Y.sup.17 are independently of each other a group of formula and their use as IR absorber, organic semiconductor in organic devices, especially in organic photovoltaics and photodiodes, or in a device containing a diode and/or an organic field effect transistor. The polymers and compounds according to the invention can have excellent solubility in organic solvents and excellent film-forming properties. In addition, high efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when the polymers and compounds according to the invention are used in organic field effect transistors, organic photovoltaics and photodiodes. ##STR00001##
USE OF ERK5 INHIBITORS FOR TREATING GLIOMAS IN PEDIATRIC SUBJECTS
The present disclosure relates to uses of an ERK5 inhibitor, e.g., ERK5-in-1, for treating a glioma in a pediatric human subject. In certain embodiments, the glioma can be a pediatric high-grade glioma (PHGG), e.g., a diffuse intrinsic pontine glioma (DIPG), and/or a H3.3-mutated glioma (e.g., a H3K27M-mutated glioma). The present disclosure further provides pharmaceutical compositions and kits that include an ERK5 inhibitor.
PYRROLOPYRAZOLE DERIVATIVES, PREPARATION METHOD THEREOF AND APPLICATION THEREOF IN MEDICINE
Disclosed are a pyrrolopyrazole derivative, a preparation method therefor, and the medical use thereof. In particular, disclosed are a novel class of pyrrolopyrazole derivatives represented by general formula (I), a preparation method therefor, and the use of the pyrrolopyrazole derivatives or pharmaceutical compositions containing the pyrrolopyrazole derivatives in biomedicine as therapeutic agents, particularly as gastric acid secretion inhibitors and potassium ion competitive acid blochers (P-CABs). The definitions of various substituent (R.sup.1, R.sup.2, R.sup.3, R.sup.4) and the group (X) in general formula (I) are the same as the definitions in the description.
Piperazine heteroaryl derivative, preparation method therefor and use of same in medicine
The present invention relates to a piperazine heteroaryl derivative, a preparation method therefor and the use of same in medicine. In particular, the present invention relates to the piperazine heteroaryl derivative as shown in the general formula (I), a preparation method therefor, a pharmaceutical composition comprising the derivative, and the use of same as a capsid protein inhibitor, in particular in the prevention and/or treatment of diseases such as hepatitis B, influenza, herpes, AIDS, etc. The definitions of each group in the general formula (I) are the same as those defined in the description. ##STR00001##
EGFR modulators and uses thereof
The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.
NEW AGENTS FOR TREATING NEUROGENIC INFLAMMATION AND NEUROPATHIC HYPERALGESIA RELATED DISORDERS
The present invention relates to 4-phenetylamino-7H-pyrrolo[2,3-d]pyrimidine derivatives of the and solvates, hydrates and pharmaceutically acceptable salts thereof, processes for manufacturing of them, the use of them, as well as pharmaceutical N compositions containing at least one of them as pharmaceutically active agent(s) together with pharmaceutically acceptable carrier, excipient and/or diluents, especially for the prevention and/or treatment of acute neurogenic inflammation and/or neuropathic hyperalgesia. Said 4-phenetylamino-7H-pyrrolo[2,3-d]pyrimidine compounds have been identified as new drug candidates for the prevention and/or treatment of acute neurogenic inflammation and/or neuropathic hyperalgesia.
NEW AGENTS FOR TREATING NEUROGENIC INFLAMMATION AND NEUROPATHIC HYPERALGESIA RELATED DISORDERS
The present invention relates to 4-phenetylamino-7H-pyrrolo[2,3-d]pyrimidine derivatives of the and solvates, hydrates and pharmaceutically acceptable salts thereof, processes for manufacturing of them, the use of them, as well as pharmaceutical N compositions containing at least one of them as pharmaceutically active agent(s) together with pharmaceutically acceptable carrier, excipient and/or diluents, especially for the prevention and/or treatment of acute neurogenic inflammation and/or neuropathic hyperalgesia. Said 4-phenetylamino-7H-pyrrolo[2,3-d]pyrimidine compounds have been identified as new drug candidates for the prevention and/or treatment of acute neurogenic inflammation and/or neuropathic hyperalgesia.
THE PROCESS FOR OBTAINING OF FLUORALKYLATED CARBON QUANTUM DOTS
The invention discloses a simple, scalable and convenient solvothermal method of obtaining fluoralkylated carbon quantum dots—Fluocar® Nano materials, by solvothermal pyrolysis of an organic substance in the presence of fluoroorganic substance that contain fluoroalkyl groups. The obtained material is water- and organic solvents soluble, grafted fluorine is hydrolytically stable, and obtained dots having intense luminescence in a wide range of wavelengths, from blue to NIR. Photoluminescent (PL) spectral map of obtained carbon dots solution is highly sensitive to pH changes and rare earth metal ions concentration in this solution. Also PL-map of such material is sensitive to organic complex moiety (e.g. Acidum salicylicum, and penicillinum).
Synthesized materials can find use as the classic and fluorescent dye replacement, as the carrier of biologically active substances, for bio-imaging, theranostic, for cytological studies, (photo)catalysis, as electrode component, as well as a sensor or biosensor, or for other uses.
THE PROCESS FOR OBTAINING OF FLUORALKYLATED CARBON QUANTUM DOTS
The invention discloses a simple, scalable and convenient solvothermal method of obtaining fluoralkylated carbon quantum dots—Fluocar® Nano materials, by solvothermal pyrolysis of an organic substance in the presence of fluoroorganic substance that contain fluoroalkyl groups. The obtained material is water- and organic solvents soluble, grafted fluorine is hydrolytically stable, and obtained dots having intense luminescence in a wide range of wavelengths, from blue to NIR. Photoluminescent (PL) spectral map of obtained carbon dots solution is highly sensitive to pH changes and rare earth metal ions concentration in this solution. Also PL-map of such material is sensitive to organic complex moiety (e.g. Acidum salicylicum, and penicillinum).
Synthesized materials can find use as the classic and fluorescent dye replacement, as the carrier of biologically active substances, for bio-imaging, theranostic, for cytological studies, (photo)catalysis, as electrode component, as well as a sensor or biosensor, or for other uses.