Patent classifications
C07D239/52
Methods and formulations for modulating Lyn kinase activity and treating related disorders
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
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.
Method for preparing azoxystrobin and its intermediates
The present invention discloses a method for preparing azoxystrobin intermediates represented by formulae (1) and (2), comprising: controlling a compound represented by formula (3) to contact with sodium methoxide and 4,6-dichloropyrimidine, to obtain a mixture of intermediates represented by formulae (1) and (2), in the existence of a catalyst, the catalyst is an azabicyclic compound or its salt. The present invention further discloses a method for preparing azoxystrobin, comprising: controlling the intermediate represented by formula (2) provided in the present invention to react with 2-cyanophenol or its salt under the catalytic action of an azabicyclic compound or its salt, to obtain an azoxystrobin compound represented by formula (4). The method provided in the present invention has advantages including high transformation ratio, high product purity, easy and convenient operation, and environmental friendliness. ##STR00001##
Method for preparing azoxystrobin and its intermediates
The present invention discloses a method for preparing azoxystrobin intermediates represented by formulae (1) and (2), comprising: controlling a compound represented by formula (3) to contact with sodium methoxide and 4,6-dichloropyrimidine, to obtain a mixture of intermediates represented by formulae (1) and (2), in the existence of a catalyst, the catalyst is an azabicyclic compound or its salt. The present invention further discloses a method for preparing azoxystrobin, comprising: controlling the intermediate represented by formula (2) provided in the present invention to react with 2-cyanophenol or its salt under the catalytic action of an azabicyclic compound or its salt, to obtain an azoxystrobin compound represented by formula (4). The method provided in the present invention has advantages including high transformation ratio, high product purity, easy and convenient operation, and environmental friendliness. ##STR00001##
Method for preparing azoxystrobin
The present invention provides a process for preparing azoxystrobin, which is performed by reacting 2-cyanophenol or a salt thereof with a compound represented by formula I under the catalysis of a trimethylamine catalyst to obtain the azoxystrobin represented by formula II, which allows the yield of the product azoxystrobin to reach 98% or more, the yield of separated product to reach 95% or more and the post-processing to be simple. The trimethylamine catalyst can be recycled and reused in synthesizing the target product azoxystrobin, which not only reduces the cost but also reduces the total nitrogen and COD in wastewater. The advantages regarding of cost and environmental protection of the method according to the present invention are significant and thus the method is suitable for industrial production.
Method for preparing azoxystrobin
The present invention provides a process for preparing azoxystrobin, which is performed by reacting 2-cyanophenol or a salt thereof with a compound represented by formula I under the catalysis of a trimethylamine catalyst to obtain the azoxystrobin represented by formula II, which allows the yield of the product azoxystrobin to reach 98% or more, the yield of separated product to reach 95% or more and the post-processing to be simple. The trimethylamine catalyst can be recycled and reused in synthesizing the target product azoxystrobin, which not only reduces the cost but also reduces the total nitrogen and COD in wastewater. The advantages regarding of cost and environmental protection of the method according to the present invention are significant and thus the method is suitable for industrial production.
METHOD FOR SYNTHESIZING ENANIOMERICALLY PURE N-(PYRIDIN-4-YL)-2-HYDROXY-ALKYLAMIDE DERIVATIVES
The present invention relates to a novel process for preparing enantiomerically pure compounds of N-(pyrid-4-yl)-2-hydroxyalkylamide type corresponding to the general formula (C) below:
##STR00001## and also to processes for preparing the reaction intermediates used in this synthesis, said intermediates having the general formulae (A) and (B) below:
##STR00002##
Treatment of pulmonary and other conditions
Disclosed is a compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of:
X.sup.1-L-X.sup.2 wherein L is a linking moiety comprising an enone; and X.sup.1 and X.sup.2 are each independently an optionally-substituted N-heterocycle. Also disclosed are method for treating pulmonary conditions and other organ or system conditions with the compounds.
Treatment of pulmonary and other conditions
Disclosed is a compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of:
X.sup.1-L-X.sup.2 wherein L is a linking moiety comprising an enone; and X.sup.1 and X.sup.2 are each independently an optionally-substituted N-heterocycle. Also disclosed are method for treating pulmonary conditions and other organ or system conditions with the compounds.
Methods and formulations for modulating Lyn kinase activity and treating related disorders
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.