Patent classifications
C07D231/22
Edaravone prodrug compound and pharmaceutical use thereof in treatment or alleviation of neurodegenerative or motor neuron disease
The present invention provides a novel prodrug of an edaravone compound or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising same as an active ingredient, and a use thereof in treatment or alleviation of neurodegenerative and/or motor neuron disease.
Edaravone-gossypol derivatives with antitumor activities and a method of preparing the same
A compound with antitumor activities represented by formula I: ##STR00001##
In formula I, R.sub.1 is alkyl, alkoxy, or ethenyl; and R.sub.2 is alkyl, alkoxy, or halogen.
Edaravone-gossypol derivatives with antitumor activities and a method of preparing the same
A compound with antitumor activities represented by formula I: ##STR00001##
In formula I, R.sub.1 is alkyl, alkoxy, or ethenyl; and R.sub.2 is alkyl, alkoxy, or halogen.
Heterocyclic compounds as pesticides
The present application relates to the use of heterocyclic compounds for controlling animal pests including arthropods, insects and nematodes, to novel heterocyclic compounds, to processes for their preparation and to intermediates for preparing the heterocyclic compounds.
Heterocyclic compounds as pesticides
The present application relates to the use of heterocyclic compounds for controlling animal pests including arthropods, insects and nematodes, to novel heterocyclic compounds, to processes for their preparation and to intermediates for preparing the heterocyclic compounds.
A PROCESS FOR PREPARING ANTHRANILIC DIAMIDES AND INTERMEDIATES THEREOF
The present invention relates a novel process for preparing a compound of Formula I,
##STR00001##
wherein, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.3c, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and Z are as defined in the description.
The process comprises a novel and inventive step of converting a dione of Formula II into an isatoic anhydride of Formula V in a single step.
##STR00002##
wherein, R.sup.2 is F, Cl, Br or I; R.sup.1, R.sup.3a, R.sup.3b, R.sup.3c, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and Z are as defined in the description.
Pyrazole compound
The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT.sub.2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT.sub.2C inverse agonistic action comprising Compound (1): ##STR00001## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen or C.sub.1-6 alkyl etc.; R.sup.5 is C.sub.4-7 alkyl or —(CR.sup.8R.sup.9).sub.r-E; R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are independently hydrogen, fluorine or C.sub.1-6 alkyl; A is C.sub.6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C.sub.3-8 cycloalkyl or C.sub.6-10 aryl etc.; L is oxygen, sulfur or —NR.sup.10—; n is 1, 2 or 3; R.sup.10 is hydrogen or C.sub.1-6 alkyl etc.; and X is hydrogen or halogen etc.
Pyrazole compound
The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT.sub.2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT.sub.2C inverse agonistic action comprising Compound (1): ##STR00001## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen or C.sub.1-6 alkyl etc.; R.sup.5 is C.sub.4-7 alkyl or —(CR.sup.8R.sup.9).sub.r-E; R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are independently hydrogen, fluorine or C.sub.1-6 alkyl; A is C.sub.6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C.sub.3-8 cycloalkyl or C.sub.6-10 aryl etc.; L is oxygen, sulfur or —NR.sup.10—; n is 1, 2 or 3; R.sup.10 is hydrogen or C.sub.1-6 alkyl etc.; and X is hydrogen or halogen etc.
COMPOUNDS WITH COPPER- OR ZINC-ACTIVATED TOXICITY AGAINST MICROBIAL INFECTION
Heterocyclic compounds with a novel pyrazole thioamide-based NNSN structural motif, having highly effective zinc- or copper-activated toxicity against microbial infections at micromolar or nanomolar minimum inhibitory concentrations (MIC), and methods of making and using same.
COMPOUNDS WITH COPPER- OR ZINC-ACTIVATED TOXICITY AGAINST MICROBIAL INFECTION
Heterocyclic compounds with a novel pyrazole thioamide-based NNSN structural motif, having highly effective zinc- or copper-activated toxicity against microbial infections at micromolar or nanomolar minimum inhibitory concentrations (MIC), and methods of making and using same.