C07D515/04

Hybrid cyclic libraries and screens thereof

Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.

Hybrid cyclic libraries and screens thereof

Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.

FLUORESCENT PREMIX PARTICLES, FLUORESCENT STAIN CONTAINING SAME, AND FLUORESCENT STAINING METHOD IN WHICH THESE ARE USED
20210011007 · 2021-01-14 ·

The present invention relates to fluorescent premix particles, a fluorescent stain containing the same, and a fluorescent staining method in which these are used, and the fluorescent premix particles are particles including: phosphor integrated particles that are modified with a first reactive substance; and at least one target protein-binding substance that is modified with a second reactive substance and is selected from the group consisting of an antibody and an aptamer, wherein the phosphor integrated particles and the at least one target protein-binding substance are linked by interaction between the first reactive substance and the second reactive substance.

FLUORESCENT PREMIX PARTICLES, FLUORESCENT STAIN CONTAINING SAME, AND FLUORESCENT STAINING METHOD IN WHICH THESE ARE USED
20210011007 · 2021-01-14 ·

The present invention relates to fluorescent premix particles, a fluorescent stain containing the same, and a fluorescent staining method in which these are used, and the fluorescent premix particles are particles including: phosphor integrated particles that are modified with a first reactive substance; and at least one target protein-binding substance that is modified with a second reactive substance and is selected from the group consisting of an antibody and an aptamer, wherein the phosphor integrated particles and the at least one target protein-binding substance are linked by interaction between the first reactive substance and the second reactive substance.

FLUOROSULFONYL-CONTAINING COMPOUND, INTERMEDIATE THEREOF, PREPARATION METHOD THEREFOR AND USE THEREOF

Disclosed in the present invention were a fluorosulfonyl-containing compound, an intermediate thereof, a preparation method therefor and use thereof. The fluorosulfonyl-containing compound disclosed in the present invention comprises a cation and an anion, the cation being as shown in Formula (1). The fluorosulfonyl-containing compound of the present invention can react with a substrate to efficiently synthesize a fluorosulfonylation product, has low toxicity, was simple to prepare, was convenient to use, and was in a solid stable state at normal temperature. Furthermore, the compound has a wide range of adaptable substrates, including phenolic compounds and amine compounds, and was the only solid form agent that can achieve such a chemical conversion, and therefore has important academic and application value.

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BICYCLIC SULFONAMIDES
20200345749 · 2020-11-05 ·

Provided herein are compounds of Formulae (I) and (II), or pharmaceutically acceptable salts of the foregoing, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formulae (I) and/or (II), or a pharmaceutically acceptable salt of any of the foregoing.

BICYCLIC SULFONAMIDES
20200345749 · 2020-11-05 ·

Provided herein are compounds of Formulae (I) and (II), or pharmaceutically acceptable salts of the foregoing, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formulae (I) and/or (II), or a pharmaceutically acceptable salt of any of the foregoing.

BICYLIC COMPOUND ACTING AS AN INHIBITOR

A bicyclic compound acting as a ROR inhibitor. Provided are a compound of formula (I) or a pharmaceutically acceptable salt thereof, the compound having a structure as represented by formula (I-A) or formula (I-B). The provided compound of formula (I-A) or formula (I-B) or pharmaceutically acceptable salt thereof has good ROR inhibitory activities, being expected to be used for treating diseases mediated by ROR receptors in a mammal.

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Sulfonyl pyridyl TRP inhibitors
10695348 · 2020-06-30 · ·

The invention provides compounds of formula I: ##STR00001##
and pharmaceutically acceptable salts thereof where R.sup.1 is a substituted or unsubstituted phenyl or a fused bicyclic comprising a substituted or unsubstituted phenyl. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

Heterocyclic compounds as immunomodulators

Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. ##STR00001##