C07D239/52

Heterocyclic compound and composition containing same

A heterocyclic compound is represented by formula (I): ##STR00001##
in which R.sup.2 represents a C1-C6 alkyl group optionally having one or more halogen atoms, n is 0, R.sup.3 represents a C1-C6 chain hydrocarbon group optionally having one or more substituents selected from Group B, q is 0, Het represents a group represented by the formulae Het 1 or Het 2, A.sup.1 represents a nitrogen atom, and Q.sup.2 represents an oxygen atom. The compound has excellent efficacy for controlling harmful arthropods. A composition is provided which contains the compound of formula (I) and one or more additional ingredients.

Heterocyclic compound and composition containing same

A heterocyclic compound is represented by formula (I): ##STR00001##
in which R.sup.2 represents a C1-C6 alkyl group optionally having one or more halogen atoms, n is 0, R.sup.3 represents a C1-C6 chain hydrocarbon group optionally having one or more substituents selected from Group B, q is 0, Het represents a group represented by the formulae Het 1 or Het 2, A.sup.1 represents a nitrogen atom, and Q.sup.2 represents an oxygen atom. The compound has excellent efficacy for controlling harmful arthropods. A composition is provided which contains the compound of formula (I) and one or more additional ingredients.

LpxC inhibitor and methods of making

Provided herein is an LpxC inhibitor compound, as well as methods of making and pharmaceutical compositions comprising said compound, and methods of use thereof in the treatment of disease that would benefit from treatment with an LpxC inhibitor, including gram-negative bacterial infections such as urinary tract infections and the like.

NOVEL THYROID HORMONE BETA RECEPTOR AGONIST

The present application provides a novel thyroid hormone ß receptor agonist having better activity, selectivity or safety and represented by formula (I), and use thereof in preventing or treating a disease related to the ß receptor agonist. The disease comprises, for example, obesity, hyperlipidemia, hypercholesterolemia, diabetes, the liver disease (fatty liver, NASH, NAFLD, etc.), the cardiovascular disease (atherosclerosis, etc.), the thyroid disease (hypothyroidism, thyroid cancer, etc.), etc.

NOVEL THYROID HORMONE BETA RECEPTOR AGONIST

The present application provides a novel thyroid hormone ß receptor agonist having better activity, selectivity or safety and represented by formula (I), and use thereof in preventing or treating a disease related to the ß receptor agonist. The disease comprises, for example, obesity, hyperlipidemia, hypercholesterolemia, diabetes, the liver disease (fatty liver, NASH, NAFLD, etc.), the cardiovascular disease (atherosclerosis, etc.), the thyroid disease (hypothyroidism, thyroid cancer, etc.), etc.

Methods And Formulations For Modulating Lyn Kinase Activity And Treating Related Disorders
20210361652 · 2021-11-25 ·

The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising the compounds or a pharmaceutically acceptable salts thereof that are useful in modulating lyn kinase activity, in particular, the compounds or a pharmaceutically acceptable salts thereof are useful for treating or preventing a disease or disorder including cardiovascular disease, dyslipidemia, dyslipoproteinemia, a disorder of glucose metabolism, metabolic syndrome (i.e., Syndrome X), a peroxisome proliferator activated receptor-associated disorder, septicemia, a thrombotic disorder, type II diabetes, obesity, pancreatitis, hypertension, renal disease, inflammation, or impotence.

Methods And Formulations For Modulating Lyn Kinase Activity And Treating Related Disorders
20210361652 · 2021-11-25 ·

The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising the compounds or a pharmaceutically acceptable salts thereof that are useful in modulating lyn kinase activity, in particular, the compounds or a pharmaceutically acceptable salts thereof are useful for treating or preventing a disease or disorder including cardiovascular disease, dyslipidemia, dyslipoproteinemia, a disorder of glucose metabolism, metabolic syndrome (i.e., Syndrome X), a peroxisome proliferator activated receptor-associated disorder, septicemia, a thrombotic disorder, type II diabetes, obesity, pancreatitis, hypertension, renal disease, inflammation, or impotence.

PROCESS FOR PREPARING 1,1,3-TRIOXO-1,2-BENZOTHIAZOLE-6-CARBOXAMIDE

A process for preparing, 1,1,3-trioxo-1,2-benzothiazole-6-carboxamide of formula (I) comprising: (a) oxidizing 2,5-dimethyl-benzenesulfonamide of formula (II) in the presence of an oxidizing agent to receive 2-sulfamoyl-terephthalic acid of formula (III); (b) converting the formed 2-sulfamoyl-terephthalic acid of formula (III) to receive 2-sulfamoyl-terephthalic acid derivative of formula (IV); and (c) reacting the resulting 2-sulfamoyl-terephthalic acid derivative of formula (IV) with ammonia (NH.sub.3) or ammonium containing-salt; wherein R represents OR′ or Cl and R′ represents a branched or non-branched C.sub.1-C.sub.12 alkyl.

PROCESS FOR PREPARING 1,1,3-TRIOXO-1,2-BENZOTHIAZOLE-6-CARBOXAMIDE

A process for preparing, 1,1,3-trioxo-1,2-benzothiazole-6-carboxamide of formula (I) comprising: (a) oxidizing 2,5-dimethyl-benzenesulfonamide of formula (II) in the presence of an oxidizing agent to receive 2-sulfamoyl-terephthalic acid of formula (III); (b) converting the formed 2-sulfamoyl-terephthalic acid of formula (III) to receive 2-sulfamoyl-terephthalic acid derivative of formula (IV); and (c) reacting the resulting 2-sulfamoyl-terephthalic acid derivative of formula (IV) with ammonia (NH.sub.3) or ammonium containing-salt; wherein R represents OR′ or Cl and R′ represents a branched or non-branched C.sub.1-C.sub.12 alkyl.

Preparation method for azoxystrobin and intermediate thereof

The present invention relates to the preparation field of azoxystrobin, and discloses a preparation method for a compound represented by formula (I). The method comprises the following steps: (1) a compound represented by formula (II) is hydrolyzed in a solvent under acidic conditions to obtain a compound represented by formula (III); and (2) the compound represented by formula (III) is reacted with a base and a methylating agent to obtain the compound represented by formula (I); in the formula, R.sub.3 is hydrogen or C.sub.1-C.sub.4 alkyl, and R.sub.4 is C.sub.1-C.sub.4 alkyl. The process for preparing azoxystrobin of the present invention not only successfully replaces trimethyl orthoformate and reduces the raw material cost, but also has high total reaction yield, and is suitable for industrial large-scale production. Experiments have proven that the yield of the prepared azoxystrobin can reach 95%. ##STR00001##