The present invention relates to tetrahydrobenzo-isoquinoline sulfonamides derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use in treating disorders caused by IgE (such as allergic responses, non-allergic mast cell responses or certain autoimmune responses), and in particular disorders caused by the interaction of IgE with the FIERI receptor.

##STR00001##

The present invention relates to tetrahydrobenzo-isoquinoline sulfonamides derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use in treating disorders caused by IgE (such as allergic responses, non-allergic mast cell responses or certain autoimmune responses), and in particular disorders caused by the interaction of IgE with the FIERI receptor.

##STR00001##

The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer or solvate thereof for use in the prevention and/or treatment of a pathology associated with proinflammatory conditions, a disease associated with oxidative stress or production of reactive oxygen species or a skin pigmentation disorder. In addition, the invention also relates to a cosmetic method for preventing and/or treating skin aging, irradiated skin or for skin-whitening comprising administering a compound of formula (I) or a cosmetically acceptable salt, stereoisomer or solvate thereof. In addition, the invention relates to a method of inhibition of enzymatic browning in food or beverage comprising contacting said food or beverage with a compound of formula (I) or a salt, stereoisomer or solvate thereof under conditions sufficient to inhibit enzymatic browning of said food or beverage.

The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer or solvate thereof for use in the prevention and/or treatment of a pathology associated with proinflammatory conditions, a disease associated with oxidative stress or production of reactive oxygen species or a skin pigmentation disorder. In addition, the invention also relates to a cosmetic method for preventing and/or treating skin aging, irradiated skin or for skin-whitening comprising administering a compound of formula (I) or a cosmetically acceptable salt, stereoisomer or solvate thereof. In addition, the invention relates to a method of inhibition of enzymatic browning in food or beverage comprising contacting said food or beverage with a compound of formula (I) or a salt, stereoisomer or solvate thereof under conditions sufficient to inhibit enzymatic browning of said food or beverage.

A fluorine-containing compound represented by general formula (1) by which high water-repellency can be obtained despite the small number of fluorine atoms:

L-(R.sup.1—X—Rf—Y—R.sup.2).sub.n  (1)

wherein L represents an n-valent organic group; n represents an integer of 1 or more; Rf represents a linear or branched fluoroalkylene group containing 1 to 4 of at least any of a CF.sub.2 unit, a CFH unit and a CFRf′ unit, and optionally having an ether bond, wherein Rf′ represents a fluoroalkyl group having 1 carbon atom; R.sup.1 represents a direct bond, or a linear or branched hydrocarbon group having 1 to 4 carbon atoms; R.sup.2 represents a linear or branched hydrocarbon group having 7 to 29 carbon atoms, containing no fluorine atoms, and optionally having an ether bond; and X and Y each independently represent a direct bond or a divalent linking group.

A fluorine-containing compound represented by general formula (1) by which high water-repellency can be obtained despite the small number of fluorine atoms:

L-(R.sup.1—X—Rf—Y—R.sup.2).sub.n  (1)

wherein L represents an n-valent organic group; n represents an integer of 1 or more; Rf represents a linear or branched fluoroalkylene group containing 1 to 4 of at least any of a CF.sub.2 unit, a CFH unit and a CFRf′ unit, and optionally having an ether bond, wherein Rf′ represents a fluoroalkyl group having 1 carbon atom; R.sup.1 represents a direct bond, or a linear or branched hydrocarbon group having 1 to 4 carbon atoms; R.sup.2 represents a linear or branched hydrocarbon group having 7 to 29 carbon atoms, containing no fluorine atoms, and optionally having an ether bond; and X and Y each independently represent a direct bond or a divalent linking group.

A catalyst and a method for preparing S-indoxacarb using the catalyst. The catalyst is prepared using 3-tert-butyl-5-(chloromethyl)salicylaldehyde and cyclohexanediamine as raw materials, where an original quinine catalyst such as cinchonine is replaced with the catalyst for application in the asymmetric synthesis of tert-butyl hydroperoxide and 5-chloro-2-methoxycarbonyl-1-indanone ester, greatly improving selection in the asymmetric synthesis process, with the S-enantiomer content increasing from 75% to over 98%, achieving the recycling of a high-efficiency chiral catalyst, and greatly reducing production costs. The synthesis process of the catalyst is simple and is favorable for industrialization, and lays good foundations for the production of high-quality indoxacarb.

A catalyst and a method for preparing S-indoxacarb using the catalyst. The catalyst is prepared using 3-tert-butyl-5-(chloromethyl)salicylaldehyde and cyclohexanediamine as raw materials, where an original quinine catalyst such as cinchonine is replaced with the catalyst for application in the asymmetric synthesis of tert-butyl hydroperoxide and 5-chloro-2-methoxycarbonyl-1-indanone ester, greatly improving selection in the asymmetric synthesis process, with the S-enantiomer content increasing from 75% to over 98%, achieving the recycling of a high-efficiency chiral catalyst, and greatly reducing production costs. The synthesis process of the catalyst is simple and is favorable for industrialization, and lays good foundations for the production of high-quality indoxacarb.

A process for continuous preparation of oligomeric or polymeric isocyanates by catalytic modification of monomeric di- and/or triisocyanates, characterized in that at least one isocyanate component A and at least one catalyst component B are combined continuously in a reaction apparatus and conducted through the reaction apparatus as a reaction mixture, the residence time distribution being characterized according to the dispersion model by Bo (Bodenstein number) above 40, preferably above 60 and most preferably above 80.

A process for continuous preparation of oligomeric or polymeric isocyanates by catalytic modification of monomeric di- and/or triisocyanates, characterized in that at least one isocyanate component A and at least one catalyst component B are combined continuously in a reaction apparatus and conducted through the reaction apparatus as a reaction mixture, the residence time distribution being characterized according to the dispersion model by Bo (Bodenstein number) above 40, preferably above 60 and most preferably above 80.