Disclosed is a method of synthesizing an -amino acid derivative, where an azirine compound, used as raw material, is reacted with a sulfhydryl compound in a mixed system of an organic solvent and a buffer solution under the protection of nitrogen to produce the -amino acid derivative. In the reaction, the carbon-nitrogen double bond of the azirine compound is attacked by the sulfhydryl compound, so that the azirine compound is directly opened to form the -amino acid derivative of which the same carbon atom is added with two molecules of the sulfhydryl compound. This method can be performed directly in an aqueous phase without using a metal catalyst.

Disclosed is a method of synthesizing an -amino acid derivative, where an azirine compound, used as raw material, is reacted with a sulfhydryl compound in a mixed system of an organic solvent and a buffer solution under the protection of nitrogen to produce the -amino acid derivative. In the reaction, the carbon-nitrogen double bond of the azirine compound is attacked by the sulfhydryl compound, so that the azirine compound is directly opened to form the -amino acid derivative of which the same carbon atom is added with two molecules of the sulfhydryl compound. This method can be performed directly in an aqueous phase without using a metal catalyst.

Aromatic amides are described, having general formula (I):

##STR00001##

suitably substituted and having a high fungicidal activity, together with their use for controlling phytopathogenic fungi of important agricultural crops.

Aromatic amides are described, having general formula (I):

##STR00001##

suitably substituted and having a high fungicidal activity, together with their use for controlling phytopathogenic fungi of important agricultural crops.

The present invention discloses novel compounds which are useful as potassium channel openers, in particular as openers of the Kv7.4 potassium channel. The novel compounds are compounds according to formula I,

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wherein n=0 or 1, RL is a substituent selected from the group consisting of unsubstituted or substituted cycloalkyl groups, in particular bicycloalkyl groups, unsubstituted or substituted phenyl groups, unsubstituted or substituted thienyl groups or cyclopentathienyl groups, and unsubstituted or substituted indanyl groups, which optionally contain heteroatoms, and RR is a substituent selected from the group consisting of unsubstituted or substituted phenyl groups or unsubstituted or substituted benzyl groups, which optionally contain heteroatoms, or a stereoisomer, a tautomer, a prodrug or a salt, preferably pharmaceutically acceptable salt thereof.

The present invention discloses novel compounds which are useful as potassium channel openers, in particular as openers of the Kv7.4 potassium channel. The novel compounds are compounds according to formula I,

##STR00001##

wherein n=0 or 1, RL is a substituent selected from the group consisting of unsubstituted or substituted cycloalkyl groups, in particular bicycloalkyl groups, unsubstituted or substituted phenyl groups, unsubstituted or substituted thienyl groups or cyclopentathienyl groups, and unsubstituted or substituted indanyl groups, which optionally contain heteroatoms, and RR is a substituent selected from the group consisting of unsubstituted or substituted phenyl groups or unsubstituted or substituted benzyl groups, which optionally contain heteroatoms, or a stereoisomer, a tautomer, a prodrug or a salt, preferably pharmaceutically acceptable salt thereof.

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 2-amino-N-(arylsulfinyl)-acetamide compounds that, inter alia, inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase (aaRS) (e.g., bacterial leucyl-t RNA synthetase, LeuRS). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase; to treat disorders that are ameliorated by the inhibition (e.g., selective inhibition) of bacterial aminoacyl-tRNA synthetase; to treat bacterial infections; etc.

##STR00001##

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 2-amino-N-(arylsulfinyl)-acetamide compounds that, inter alia, inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase (aaRS) (e.g., bacterial leucyl-t RNA synthetase, LeuRS). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase; to treat disorders that are ameliorated by the inhibition (e.g., selective inhibition) of bacterial aminoacyl-tRNA synthetase; to treat bacterial infections; etc.

##STR00001##

Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases. ##STR00001##

Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases. ##STR00001##