C07D295/185

Use of stereoselective transaminase in asymmetric synthesis of chiral amine

Use of a stereoselective transaminase in the asymmetric synthesis of a chiral amine. In particular, provided is use of a polypeptide in the production of a chiral amine or a downstream product using a chiral amine as a precursor. Further provided is a method for producing a chiral amine, comprising culturing a strain expressing the polypeptide so as to obtain a chiral amine. Further provided are a chiral amine production strain and a method for constructing the chiral amine production strain. The stereoselective transaminase has a broad substrate spectrum and thus has a broad application potential in the preparation of a chiral amine.

Inhibitors of histone deacetylase

The present invention relates to compounds of formula (I): ##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.

Inhibitors of histone deacetylase

The present invention relates to compounds of formula (I): ##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.

FLUORENE DERIVATIVE, AND PRODUCTION METHOD AND USE FOR SAME
20230098716 · 2023-03-30 · ·

The fluorene derivative of the present disclosure is represented by the following formula (1):

##STR00001##

Wherein R.sup.1 represents a substituent, k denotes an integer of 0 to 8, R.sup.2a, R.sup.2b, R.sup.2c, and R.sup.2d each represent a hydrogen atom or a substituent, R.sup.3a and R.sup.3b each represent a hydrogen atom or a substituent, and X.sup.1a and X.sup.1b each represent a group defined in the following formula (X1):

##STR00002##

wherein R.sup.4 and R.sup.5 each represent a hydrogen atom or an aliphatic hydrocarbon group, provided that the case where both R.sup.4 and R.sup.5 are a hydrogen atom is excluded; or R.sup.4 and R.sup.5 bond together to form a heterocyclic ring containing the nitrogen atom adjacent to R.sup.4 and R.sup.5. The present disclosure provides a novel fluorene derivative useful as an additive for improving the properties of a resin, a method for producing the same and a use thereof.

FLUORESCENT SYSTEMS FOR BIOLOGICAL IMAGING AND USES THEREOF
20220347299 · 2022-11-03 ·

The invention discloses a dye sensitizer molecule taking triazole as a core and a preparation method of the dye sensitizer molecule. According to the dye molecule, a triazole ring is introduced to the design of a molecular structure, and the electronic absorption and transmission capability among D-pi-A dye molecules are greatly improved by substituting donors with different carbon chain lengths and receptors with triple bonds at the periphery, so that a novel triazole dye with high efficiency is obtained. The preparation method of the compound comprises: click chemical reaction, detrimethylsilyl reaction, Sonogashira coupling reaction and the like; and the prepared dye molecule can be applied to a dye-sensitive solar cell and can show favorable photoelectric conversion property so as to have wide application prospects on the aspects of energy development and utilization. In addition, the material also has liquid crystal property under a certain condition so as to also have a huge potential on the aspect of application to photoelectric devices.

FLUORESCENT SYSTEMS FOR BIOLOGICAL IMAGING AND USES THEREOF
20220347299 · 2022-11-03 ·

The invention discloses a dye sensitizer molecule taking triazole as a core and a preparation method of the dye sensitizer molecule. According to the dye molecule, a triazole ring is introduced to the design of a molecular structure, and the electronic absorption and transmission capability among D-pi-A dye molecules are greatly improved by substituting donors with different carbon chain lengths and receptors with triple bonds at the periphery, so that a novel triazole dye with high efficiency is obtained. The preparation method of the compound comprises: click chemical reaction, detrimethylsilyl reaction, Sonogashira coupling reaction and the like; and the prepared dye molecule can be applied to a dye-sensitive solar cell and can show favorable photoelectric conversion property so as to have wide application prospects on the aspects of energy development and utilization. In addition, the material also has liquid crystal property under a certain condition so as to also have a huge potential on the aspect of application to photoelectric devices.

SULFUR AND AMIDE TROPOLONE INHIBITORS OF NUCLEOTIDYL TRANSFERASES AND USES THEREFOR

The present disclosure provides inhibitors of microorganisms including viruses and fungi of the formula (I) or (II) wherein the variables are defined herein. Also provided are methods of treatment using these agents in the treatment of infections of microorganisms such as viruses and fungi.

##STR00001##

SULFUR AND AMIDE TROPOLONE INHIBITORS OF NUCLEOTIDYL TRANSFERASES AND USES THEREFOR

The present disclosure provides inhibitors of microorganisms including viruses and fungi of the formula (I) or (II) wherein the variables are defined herein. Also provided are methods of treatment using these agents in the treatment of infections of microorganisms such as viruses and fungi.

##STR00001##

CHEMICAL COMPOUNDS TARGETING THE EYE AND USE THEREOF IN THE TREATMENT OF EYE DISEASES

Disclosed is chemical compounds C that are derivatives of norbixin and have tropism for the eye, and are intended to be used in the treatment of eye diseases in mammals, in particular in the context of altering the retinal pigment epithelium and more particularly in the context of age-related macular degeneration (AMD) and Stargardt's disease.

P38ALPHA MITOGEN-ACTIVATED PROTEIN KINASE INHIBITORS
20230090562 · 2023-03-23 ·

Disclosed herein are p38α mitogen-activated protein kinase inhibitors, pharmaceutical compositions thereof, and therapeutic methods of using the p38α mitogen-activated protein kinase inhibitors.