C07D241/44

Methods and Compositions for Targeting Tregs using CCR8 Inhibitors
20230159446 · 2023-05-25 ·

The present invention provides compounds of Formula (I) which can be used as CCR8 inhibitors, which can be used as treatment or prevention of cancer using CCR8 inhibitors targeted tumor specific T regulatory cells.

##STR00001##

Labile esters of agrochemicals for controlled release and reduction of off-site movement
11465960 · 2022-10-11 · ·

The present invention relates to esters of carboxylic acid agrochemicals comprising a labile protecting group and having formula (I). Certain of the esters of carboxylic acid agrochemicals do not undergo hydrolysis to a significant degree in the dark, but are cleaved to regenerate the parent carboxylic acid agrochemical when exposed to light. Others of the esters of carboxylic acid agrochemicals undergo hydrolysis under both light and dark conditions. The present invention further relates to methods for the controlled release of a carboxylic acid agrochemicals, and to methods of controlling unwanted plants comprising applying to the unwanted plants an ester of a carboxylic acid agrochemical.

Labile esters of agrochemicals for controlled release and reduction of off-site movement
11465960 · 2022-10-11 · ·

The present invention relates to esters of carboxylic acid agrochemicals comprising a labile protecting group and having formula (I). Certain of the esters of carboxylic acid agrochemicals do not undergo hydrolysis to a significant degree in the dark, but are cleaved to regenerate the parent carboxylic acid agrochemical when exposed to light. Others of the esters of carboxylic acid agrochemicals undergo hydrolysis under both light and dark conditions. The present invention further relates to methods for the controlled release of a carboxylic acid agrochemicals, and to methods of controlling unwanted plants comprising applying to the unwanted plants an ester of a carboxylic acid agrochemical.

Synthesis of N-vinyl compounds by reacting cylic NH-compounds with acetylene in presence of homogenous catalyst

A process can be used to produce N-vinyl compounds by homogeneous catalysis. In the process, acetylene is reacted with a cyclic compound having at least one nitrogen as a ring member, hearing a substitutable hydrogen residue (cyclic compound C), in a liquid phase in the presence of a ruthenium complex containing at least one phosphine as a ligand (RuCat).

Synthesis of N-vinyl compounds by reacting cylic NH-compounds with acetylene in presence of homogenous catalyst

A process can be used to produce N-vinyl compounds by homogeneous catalysis. In the process, acetylene is reacted with a cyclic compound having at least one nitrogen as a ring member, hearing a substitutable hydrogen residue (cyclic compound C), in a liquid phase in the presence of a ruthenium complex containing at least one phosphine as a ligand (RuCat).

Methods for Producing Nitroso Compound and Quinoxaline Compound

A method for producing a compound of a formula (3), including reacting a compound of a formula (1) with a compound of a formula (2) by using a tertiary alcohol and a base:

##STR00001##

where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are each independently a hydrogen atom, a halogen atom, a (C1-C4)alkyl, or a (C1-C4)alkoxy, the amount of the base used is 2.0-4.0 equivalents per 1 equivalent of the compound of formula (2), the amount of the tertiary alcohol used is 0.3-2.5 equivalents per 1 equivalent of the compound of formula (2), the base is a plurality of compounds comprising a lithium-containing base as a first compound, and a second compound selected from the group consisting of alkali metal hydrides, alkali metal amides, alkoxides, alkyl metals, alkali metals, and organic bases, and the reaction is performed in the presence of an aromatic hydrocarbon solvent.

Methods for Producing Nitroso Compound and Quinoxaline Compound

A method for producing a compound of a formula (3), including reacting a compound of a formula (1) with a compound of a formula (2) by using a tertiary alcohol and a base:

##STR00001##

where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are each independently a hydrogen atom, a halogen atom, a (C1-C4)alkyl, or a (C1-C4)alkoxy, the amount of the base used is 2.0-4.0 equivalents per 1 equivalent of the compound of formula (2), the amount of the tertiary alcohol used is 0.3-2.5 equivalents per 1 equivalent of the compound of formula (2), the base is a plurality of compounds comprising a lithium-containing base as a first compound, and a second compound selected from the group consisting of alkali metal hydrides, alkali metal amides, alkoxides, alkyl metals, alkali metals, and organic bases, and the reaction is performed in the presence of an aromatic hydrocarbon solvent.

Novel 3,5-Diaminobenzoic Acid Compound, and PIN1 Inhibitor and Therapeutic Agent for Inflammatory Diseases Using Same

[Problem] To develop a group of novel compounds with an inhibitory activity against the function of Pin1 so as to use them as candidate compounds for medicaments.

[Solution] The present invention provides: a compound represented by the following Formula (I) or a salt thereof, as well as a Pin1 inhibitor, a pharmaceutical composition, a therapeutic or prophylactic agent for inflammatory diseases, a therapeutic or prophylactic agent for fatty liver diseases, a therapeutic or prophylactic agent for obesity, and a therapeutic or prophylactic agent for COVID-19 that utilize the aforementioned compounds or the salts thereof:

Substituted quinazolines as inhibitors of KRAS G12C

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): ##STR00001##
or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R.sup.1, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, G.sup.1, G.sup.2, L.sup.1, L.sup.2, m.sup.1, m.sup.2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Substituted quinazolines as inhibitors of KRAS G12C

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): ##STR00001##
or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R.sup.1, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, G.sup.1, G.sup.2, L.sup.1, L.sup.2, m.sup.1, m.sup.2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.