The Scripps Research Institute

Theracos, Inc.

Chinese Academy of Sciences

Zhonghongxin Investment Holdings (shenzhen) Co., Ltd

Jiajia Dong

K Barry Sharpless

Jeffery W Kelly

Wentao Chen

Brian Seed

Yan Feng

Binhua Lv

Valery Fokin

Yuanwei Chen

Baihua Xu

Aleksandra Baranczak

Larisa Krasnova

Luke R Kwisnek

James S Oakdale

Lili Zhang

Ge Xu

Kun Peng

Jiyan Du

Min Xu

Jacques Y Roberge

Michael J Hadd

Peng Wu

Qian Yang

Xinxing Tang

Hua Wang

Bing Gao

Taijie Guo

Xiongjie Zhan

Genyi Meng

Vasanthakumar Rajappan

This application describes modified amino acids and polypeptides comprising a SOF or CHCHSOF group bound to the side chain of an amino acid or amino acid residue of a polypeptide in place of a hydrogen of a hydroxyl or amino substituent thereof. Methods of covalently binding the polypeptides to receptor sites of receptor proteins are also described herein.

Sulfur (VI) fluoride compounds and methods for the preparation thereof

This application describes a compound represented by Formula (I): wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; Xis a covalent bond or &#x2014;CHCH&#x2014;, Xis O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.

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. 

Fluorosulfonyl-containing compound, intermediate thereof, preparation method therefor and use thereof

This application describes a compound represented by Formula (I):YZX&#x2014;S(O)(X)F)]&#x2003;&#x2003;(I)wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; Xis a covalent bond or &#x2014;CHCH&#x2014;, Xis O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.

Sulfur(VI) fluoride compounds and methods for the preparation thereof

Condensation of fluoro-substituted and silyl-substituted monomers provides polymers suitable for use, e.g., as engineering polymers. A monomer composition is condensed in the presence of a bifluoride or poly(hydrogen fluoride) fluoride salt. The monomer composition contains a compound of formula F-X-F and a compound of formula (R)Si&#x2014;Z&#x2014;Si(R), and forms an alternating X-Z polymer chain and a silyl fluoride byproduct. X has the formula -A(-R-A)n-; each A is SO, C(&#x2550;O), or Het; Ris an organic moiety; n is 0 or 1; Het is an aromatic nitrogen heterocycle; Z has the formula -L-R-L-; each L is O, S, or N(R); and each Ris an organic moiety, and Rcomprises H or an organic moiety.

Polymerization of silyl- and fluoro-containing monomers

This application describes a compound represented by Formula (I): (I) wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; Xis a covalent bond or &#x2014;CHCH&#x2014;, Xis O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.

Condensation of fluoro-substituted and silyl-substituted monomers provides polymers suitable for use, e.g., as engineering polymers. A monomer composition is condensed in the presence of a basic catalyst. The monomer composition contains a compound of formula F&#x2014;X&#x2014;F and a compound of formula (R)Si&#x2014;Z&#x2014;Si(R), and forms an alternating X&#x2014;Z polymer chain and a silyl fluoride byproduct. X has the formula -A(&#x2014;R-A)n-; each A is SO, C(&#x2550;O), or Het; Ris an organic moiety; n is 0 or 1; Het is an aromatic nitrogen heterocycle; Z has the formula -L-R-L; each L is O, S, or N(R); and each Ris an organic moiety, and Rcomprises H or an organic moiety.

Polymerization method and polymers formed therewith

Condensation of fluoro-substituted and silyl-substituted monomers provides polymers suitable for use, e.g., as engineering polymers. A monomer composition is condensed in the presence of a basic catalyst. The monomer composition contains a compound of formula F&#x2014;X&#x2014;F and a compound of formula (R)Si&#x2014;Z&#x2014;Si(R), and forms an alternating X&#x2014;Z polymer chain and a silyl fluoride byproduct. X has the formula -A(-R-A)n-; each A is SO, C(&#x2550;O) or Het; Ris an organic moiety; n is 0 or 1; Het is an aromatic nitrogen heterocycle; Z has the formula -L-R-L-; each L is O, S, or N(R); and each Ris an organic moiety, and Rcomprises H or an organic moiety.

Condensation of fluoro-substituted and silyl-substituted monomers provides polymers suitable for use, e.g., as engineering polymers. A monomer composition is condensed in the presence of a basic catalyst. The monomer composition contains a compound of formula F&#x2014;X&#x2014;F and a compound of formula (R)3Si&#x2014;Z&#x2014;Si(R)3, and forms an alternating X&#x2014;Z polymer chain and a silyl fluoride byproduct. X has the formula -A(-R-A)n-; each A is SO, C(&#x2550;O), or Het; Ris an organic moiety; n is 0 or 1; Het is an aromatic nitrogen heterocycle; Z has the formula -L-R-L-; each L is O, S, or N(R); and each Ris an organic moiety, and Rcomprises H or an organic moiety.

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by SGLT inhibition.

Deuterated benzylbenzene derivatives and methods of use

Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

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Shanghai, China

Jiajia Dong