The present disclosure relates to the field of organic light emitting materials, and in particular, to a fluorescent probe compound for zinc ion, as well as a preparation method and use in zinc ion detection thereof. The fluorescent probe compound of the present disclosure has a name of 2-(7-(2,8-dimethyl quinoline-6-yl)-5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl) phenol, and is synthesized with 2,8-dimethyl tetrahydroquinoline and 2-(2-phenolyl)-1,8-naphthyridine as main raw materials. Fluorescence property tests show that the fluorescent probe compound of the present disclosure has a high selectivity and sensitivity for Zn.sup.2+, a high chemical stability and a good water solubility, which particularly suitable for detecting Zn.sup.2+ in a water environment system. The excitation and emission spectrums of the compound are in a visible region, which could serve as a fluorescent probe applied to the field of zinc ion detection.

The present invention is directed to derivatives of aceclidine. The present invention is further directed to ophthalmological compositions comprising a therapeutically effective amount of a compound of the present invention and one or more pharmaceutically acceptable excipients. The present invention is further directed to a methods of treating presbyopia or glaucoma or reducing hyperemia comprising administering to a patient in need thereof a therapeutically effective amount of a compound of the present invention.

The present invention is directed to derivatives of aceclidine. The present invention is further directed to ophthalmological compositions comprising a therapeutically effective amount of a compound of the present invention and one or more pharmaceutically acceptable excipients. The present invention is further directed to a methods of treating presbyopia or glaucoma or reducing hyperemia comprising administering to a patient in need thereof a therapeutically effective amount of a compound of the present invention.

A condensed cyclic compound represented by Formula 1: ##STR00001## wherein in Formula 1, A.sub.1, A.sub.11, X.sub.21, XY.sub.1, XY.sub.11, R.sub.4, R.sub.14, b4, b14, c1, and c11 are as described in the specification.

A new, stable trimeric TNFα structure is disclosed with distorted symmetry which can bind to the TNFR1 receptor to attenuate signalling therefrom, which can be used in the treatment and/or prevention of diseases associated with the soluble TNFα/TNFR1 interaction. Membrane-bound TNFα is not affected in its ability to signal through TNFR2, and thus the new structure of TNFα may be used in therapies which do not significantly raise the risk of infection or malignancy.

A new, stable trimeric TNFα structure is disclosed with distorted symmetry which can bind to the TNFR1 receptor to attenuate signalling therefrom, which can be used in the treatment and/or prevention of diseases associated with the soluble TNFα/TNFR1 interaction. Membrane-bound TNFα is not affected in its ability to signal through TNFR2, and thus the new structure of TNFα may be used in therapies which do not significantly raise the risk of infection or malignancy.

A dihydropyrimidine compound and use as a medicament, especially application as a medicament used for treating and preventing hepatitis B, specifically, is a compound having Formula (I) or (Ia), or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, wherein the variables of the formulas are as defined in the specification; and also includes the use of the compound having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof as a medicament, especially use as a medicament for treating and preventing hepatitis B. ##STR00001##

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.

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.

The present invention relates to a method for the synthesis of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. iriniotecan), comprising: (a) preparing 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptotecin; and (b) selectively ethylating the compound of step (a) at the 7-position, thus resulting in the preparation of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin. The present invention is further directed to the use of 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. 7-des-ethyl-irinotecan) as intermediate in a method for the synthesis of irinotecan as described.