C07D333/06

ACTIVATION OF CARBONYL BETA-CARBONS FOR CHEMICAL TRANSFORMATIONS
20190337955 · 2019-11-07 ·

The present invention relates to a method for synthesizing a compound of Formula (I)

##STR00001## as defined herein, comprising: (i) activating a compound of Formula (II)

##STR00002## as defined herein, by reacting said compound of Formula (II) with a compound of Formula (III)

##STR00003## as defined herein, in the presence of a base, to obtain a compound of Formula (IV)

##STR00004## as defined herein; and (ii) reacting the compound of Formula (IV) with an electrophile to obtain the compound of Formula (I). The present invention further relates to the organocatalysts used in the described methods and their respective uses.

ACTIVATION OF CARBONYL BETA-CARBONS FOR CHEMICAL TRANSFORMATIONS
20190337955 · 2019-11-07 ·

The present invention relates to a method for synthesizing a compound of Formula (I)

##STR00001## as defined herein, comprising: (i) activating a compound of Formula (II)

##STR00002## as defined herein, by reacting said compound of Formula (II) with a compound of Formula (III)

##STR00003## as defined herein, in the presence of a base, to obtain a compound of Formula (IV)

##STR00004## as defined herein; and (ii) reacting the compound of Formula (IV) with an electrophile to obtain the compound of Formula (I). The present invention further relates to the organocatalysts used in the described methods and their respective uses.

Hexabenzocoronene-based compound for organic photovoltaic cells

Provided is a hexabenzocoronene-based compound and a donor: acceptor layer having this compound. Also provided are processes for manufacturing this compound and to a photovoltaic cell having at least one hexabenzocoronene-based compound. The hexabenzocoronene-based compound has following formula I: ##STR00001##
wherein R.sup.1, R.sup.3, R.sup.4 and R.sup.6 are independently from each other chosen among a carboxylic (COOH) group, a cyano (CN) group, an isocyano (N.sup.+C.sup.) group, a cyanate (OCN) group and a F group, and R.sup.2 and R.sup.5 are, independently from each other, chosen among a poly(3-oxypentylthiophene) (P3OPT) substituent and a poly(3-hexylthiophene) (P3HT) substituent.

Hexabenzocoronene-based compound for organic photovoltaic cells

Provided is a hexabenzocoronene-based compound and a donor: acceptor layer having this compound. Also provided are processes for manufacturing this compound and to a photovoltaic cell having at least one hexabenzocoronene-based compound. The hexabenzocoronene-based compound has following formula I: ##STR00001##
wherein R.sup.1, R.sup.3, R.sup.4 and R.sup.6 are independently from each other chosen among a carboxylic (COOH) group, a cyano (CN) group, an isocyano (N.sup.+C.sup.) group, a cyanate (OCN) group and a F group, and R.sup.2 and R.sup.5 are, independently from each other, chosen among a poly(3-oxypentylthiophene) (P3OPT) substituent and a poly(3-hexylthiophene) (P3HT) substituent.

Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof

Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof

Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

OPTO-ELECTRONIC DEVICE AND ELECTRONIC APPARATUS INCLUDING THE SAME

Provided is an opto-electronic device including a first electrode, a second electrode facing the first electrode, and a photoactive layer arranged between the first electrode and the second electrode, wherein the photoactive layer includes a first layer and a second layer, the first layer including a first compound, and the second layer including a second compound that does not include a 5-membered ring, the first compound is an electron-donating compound, the second compound is an electron-accepting compound, and the opto-electronic device satisfies Equation 1:


0.1?(E.sup.1.sub.LUMO?E.sup.2.sub.LUMO)/(E.sup.1.sub.LUMO?E.sup.1.sub.HOMO)?0.5Equation 1 wherein, in Equation 1, E.sup.1.sub.LUMO, E.sup.1.sub.HOMO, and E.sup.2.sub.LUMO are each as defined herein.

OPTO-ELECTRONIC DEVICE AND ELECTRONIC APPARATUS INCLUDING THE SAME

Provided is an opto-electronic device including a first electrode, a second electrode facing the first electrode, and a photoactive layer arranged between the first electrode and the second electrode, wherein the photoactive layer includes a first layer and a second layer, the first layer including a first compound, and the second layer including a second compound that does not include a 5-membered ring, the first compound is an electron-donating compound, the second compound is an electron-accepting compound, and the opto-electronic device satisfies Equation 1:


0.1?(E.sup.1.sub.LUMO?E.sup.2.sub.LUMO)/(E.sup.1.sub.LUMO?E.sup.1.sub.HOMO)?0.5Equation 1 wherein, in Equation 1, E.sup.1.sub.LUMO, E.sup.1.sub.HOMO, and E.sup.2.sub.LUMO are each as defined herein.

Thiocycloheptyne derivatives and their use

The present invention pertains to novel thiocycloheptyne derivatives of general formula (I): and in particular to thiacycloalkynesulfoimine derivatives and their synthesis. The invention also relates to the use of the novel thiocycloheptyne derivatives in coupling reactions with linkers and drugs. The invention further relates to the use of the novel thiocycloheptynes in bioorthogonal (copper-free) click reactions. The invention further pertains to the use of the novel thiocycloheptyne derivatives in the generation of advanced multifunctional drug delivery systems (drug-loaded) nanoparticles. ##STR00001##

METHOD FOR PREPARING THIENYL ALANINE HAVING OPTICAL ACTIVITY

This invention relates to a method of preparing optically active -2-thienyl-alanine, and more particularly to a method of preparing optically active -2-thienyl-L-alanine or optically active -2-thienyl-D-alanine through an optical resolution reaction using chiral dibenzoyl tartaric acid or a derivative thereof as an optical resolving agent.