C07D213/89

Stereodynamic chemosensors
09815746 · 2017-11-14 · ·

The present invention relates to multifunctional chemosensors that can measure the concentration, enantiomeric excess (ee), and absolute configuration of chiral compounds. The chemosensors described herein may contain a backbone moiety that is bonded to a fluorescent moiety and a moiety for bonding a chiral compound. Backbone moieties may include aromatic groups, for example, naphthyl. The chemosensors described herein are useful for measuring concentration, enantiomeric excess, and absolute configuration of organic molecules in areas such as high throughput screening.

Stereodynamic chemosensors
09815746 · 2017-11-14 · ·

The present invention relates to multifunctional chemosensors that can measure the concentration, enantiomeric excess (ee), and absolute configuration of chiral compounds. The chemosensors described herein may contain a backbone moiety that is bonded to a fluorescent moiety and a moiety for bonding a chiral compound. Backbone moieties may include aromatic groups, for example, naphthyl. The chemosensors described herein are useful for measuring concentration, enantiomeric excess, and absolute configuration of organic molecules in areas such as high throughput screening.

METHOD FOR PRODUCING 2-PYRIDONE COMPOUND

To provide a method for producing a compound represented by the formula (1) which is a 2-pyridone compound useful as a pharmaceutical or an intermediate for a pharmaceutical, etc. at a high yield.

##STR00001##

A method for producing a 2-pyridone compound represented by the formula (1), which comprises reacting a 6-benzoyl-2-pyridone compound represented by the formula (3) with a sulfone compound represented by the formula (4):

##STR00002##

Precursors for Electron Beam-Induced Deposition of Gold and Silver

Precursors are prepared and employed in electron beam induced decomposition (EBID). The EBID precursors are complexes of the formula: X-M-Y, where M is Au or Ag; X is F, Cl, Br, I, CN, OR.sup.1, O.sub.2CR.sup.2, or R.sup.3; Y is P(OR).sub.3, NR.sub.3, unsubstituted or substituted pyrrole, unsubstituted or substituted pyridine, unsubstituted or substituted pyrrolidine, or unsubstituted or substituted piperidine; and where R, R.sup.1, R.sup.2, R.sup.3, and substituents of the substituted pyrrole, pyridine, pyrrolidine, or piperidine are independently H, C.sub.1-C.sub.8 alkyl, C.sub.6-C.sub.10 aryl, C.sub.1-C.sub.8 perfluoroalkyl, C.sub.1-C.sub.8 partially fluorinated alkyl, and SiR.sup.5R.sup.6R.sup.7 where R.sup.5, R.sup.6, and R.sup.7 are independently H, C.sub.1-C.sub.8 alkyl, or C.sub.1-C.sub.8 fluorinated alkyl. The decomposition of the EBID precursor results in the formation of one or more gold, silver, or any combination thereof features on a substrate.

GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:

##STR00001##

wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:

##STR00001##

wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Inhibitors of nucleotidyl transferases and uses in herpes and hepatitis viral infections therefor

The present disclosure relates to identification of inhibitors of hepatitis and herpesvirus replication including compounds of the formula: ##STR00001##
wherein the variables are as defined herein. Also provided are methods of treatment using agents so identified.

Inhibitors of nucleotidyl transferases and uses in herpes and hepatitis viral infections therefor

The present disclosure relates to identification of inhibitors of hepatitis and herpesvirus replication including compounds of the formula: ##STR00001##
wherein the variables are as defined herein. Also provided are methods of treatment using agents so identified.

Substituted 1,6-dihydropyridinones and 1,2-dihydroisoquinolinones as bet inhibitors

Novel bromodomain and extraterminal domain (BET) inhibitors contanining substituted 2-pyridones and therapeutic methods of treating conditions and diseases using these novel BET inhibitors are provided.

Substituted 1,6-dihydropyridinones and 1,2-dihydroisoquinolinones as bet inhibitors

Novel bromodomain and extraterminal domain (BET) inhibitors contanining substituted 2-pyridones and therapeutic methods of treating conditions and diseases using these novel BET inhibitors are provided.