5 results about "Reversible inhibition" patented technology

Described herein are aptamers for temperature-dependent reversible inhibition of thermostable polymerase activity in order to improve sensitivity and specificity of various reactions and assays involving hot start polynucleotide synthesis. Methods for use of the aptamers and related compositions and kits are also provided.

Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts or deuterated forms thereof, wherein R0 , L and R1 are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt or deuterated form thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt or deuterated form thereof, e.g., in the treatment of a disease that is treatable by administration of a DPP1 inhibitor.

This invention discloses BacPROTACs targeting dihydropteranoic acid synthase, their preparation method, and their applications, belonging to the fields of medicinal chemistry and anti-infective drug technology. The BacPROTACs have the structure shown in Formula I, II, or III, and are composed of a DHPS inhibitor fragment, a linker group, and a phosphorylated arginine (pArg) fragment. The pArg fragment, as a functional group capable of interacting with the bacterial ClpCP protease system, is coupled to a DHPS inhibitor through linkers of different types and chain lengths, resulting in bifunctional molecules possessing both DHPS binding and ClpCP recruitment capabilities. These compounds can recruit the ClpCP protease system while binding to DHPS, thereby inducing or promoting DHPS degradation, reducing target protein levels, and expanding the pharmacodynamic mechanism of DHPS-targeted drugs. Compared with existing DHPS inhibitors that mainly rely on reversible inhibition, this invention provides a new technical solution for the development of antibacterial drugs through a design strategy combining inhibition and targeted degradation. These compounds can be used to prepare antibacterial drugs.

A fused bicyclic compound having an effect in inhibition of the activity of a tyrosine kinase, and preparation and use thereof are disclosed. In particular, a compound of formula (IV) or a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a polymorph, a prodrug or an isotopic variation thereof, as well as a pharmaceutical composition including the same are disclosed. As a selective irreversible inhibitor of Bruton's tyrosine kinase, the described compound can be used for preventing or treating diseases such as inflammation, autoimmune diseases (such as rheumatoid arthritis), xenogeneic immune diseases and cancers.

The invention belongs to the technical field of biological medicines, and relates to application of a histone deacetylase inhibitor HDACi in preparation of a medicine for preventing and / or treating hyperammonemia-induced encephalopathy. According to the invention, a histone deacetylase inhibitor HDACi is used as a new medicine, the HDACi can enter a central nervous system, and the GS is triggered to be degraded through a proteasome mediated by CRBN E3 ubiquitin ligase by improving the acetylation level of a key enzyme, namely glutamine synthetase (GS), of astrocytes, so that the GS protein abundance is reversibly reduced, and the GS protein abundance is reduced. The application has the advantages that pathological accumulation of toxic metabolite glutamine can be reduced from the source, cerebral edema, autophagy-lysosomal dysfunction, neuroinflammation and neuron injury caused by the pathological accumulation can be synchronously improved, severe neurotoxicity such as persistent enzyme inhibition and acute epilepsy caused by irreversible inhibitors such as MSO can be avoided, clinical transformation risks can be obviously reduced, and the safety is high.