C07D273/04

Dihydrooxadiazine compounds for treating infections and cancer

The invention relates to the use of 1-(4,6-dipentyl-5,6-dihydro-2H-1,2,3-oxadiazin-2-yl)-3-hydroxypropan-1-one in treating and/or preventing infections caused by a bacterium, fungus or virus or in treating and/or preventing cancer. Additionally, the invention relates to a process for obtaining the compound of formula (I) of the invention, said process comprising the steps of cultivating a strain of Dolichospermum sp in an aqueous nutrient medium with assimilable carbon and nitrogen sources and salts, under controlled aerobic conditions, and then recovering the compound of general formula (I) from the culture broth.

Dihydrooxadiazinones

The present invention provides dihydrooxydiazinone compounds of general formula (I): in which R.sup.1, R.sup.2, R.sup.3, and R.sup.4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients. ##STR00001##

Dihydrooxadiazinones

The present invention provides dihydrooxydiazinone compounds of general formula (I): in which R.sup.1, R.sup.2, R.sup.3, and R.sup.4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients. ##STR00001##

POLYISOCYANURATE MATERIALS AS ELECTRICAL POTTING COMPOUNDS

The invention relates to potting compounds which cure to polyisocyanurate plastics, to the production of said potting compounds and to the use of the potting compounds for manufacturing electrical components.

PREPARATION METHOD FOR HIGH OPTICAL INDOXACARB INTERMEDIATE

A field of asymmetric catalytic synthesis, and in particular a preparation method for a high optical indoxacarb intermediate includes reacting 5-chloro-2-methoxycarbonyl-1-indanone ester (or indanone ester for short) with an oxidizing agent in the presence of a chiral Zr-salen polymer to obtain an indoxacarb intermediate (2S)-5-chloro-2,3-dihydro-2-hydroxy-1-oxo-1H-indole-2-carboxylic acid methyl ester. The yield is stabilized between 86% and 90%, and the S-enantiomer content is up to 99%. Such catalyst can replace catalysts such as cinchonine, and greatly increase the content of the effective S-enantiomer of the indoxacarb, so that the content of the hydroxyl intermediate S-enantiomer of the indoxacarb is raised from 75% to 99% or more. In addition, the chiral Zr-salen polymer catalyst is recycled without retreatment, and can be recycled at least 5 times or more, greatly reducing the production cost and laying a foundation for the industrial production of high quality indoxacarb.

PREPARATION METHOD FOR HIGH OPTICAL INDOXACARB INTERMEDIATE

A field of asymmetric catalytic synthesis, and in particular a preparation method for a high optical indoxacarb intermediate includes reacting 5-chloro-2-methoxycarbonyl-1-indanone ester (or indanone ester for short) with an oxidizing agent in the presence of a chiral Zr-salen polymer to obtain an indoxacarb intermediate (2S)-5-chloro-2,3-dihydro-2-hydroxy-1-oxo-1H-indole-2-carboxylic acid methyl ester. The yield is stabilized between 86% and 90%, and the S-enantiomer content is up to 99%. Such catalyst can replace catalysts such as cinchonine, and greatly increase the content of the effective S-enantiomer of the indoxacarb, so that the content of the hydroxyl intermediate S-enantiomer of the indoxacarb is raised from 75% to 99% or more. In addition, the chiral Zr-salen polymer catalyst is recycled without retreatment, and can be recycled at least 5 times or more, greatly reducing the production cost and laying a foundation for the industrial production of high quality indoxacarb.

Dihydrooxadiazinones

The present invention provides dihydrooxydiazinone compounds of general formula (I) ##STR00001##
in which R.sup.1, R.sup.2, R.sup.3, and R.sup.4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.

Dihydrooxadiazinones

The present invention provides dihydrooxydiazinone compounds of general formula (I) ##STR00001##
in which R.sup.1, R.sup.2, R.sup.3, and R.sup.4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.

SYNTHESIS OF HETEROCYCLIC COMPOUNDS FROM CARBOXAMIDE AND CARBOXAMIDE DERIVATIVES WITH HALOALKANOLS

The invention provides for methods for the synthesis of various compounds through reaction of carboxamide, or carboxamide derivatives, with various substituted or unsubstituted haloalkanols in a one-step, single vessel, reaction mechanism. Preferably, but not exclusively, the reaction proceeds in the absence of any solvents, catalyst, base, or any further reagents.

SYNTHESIS OF HETEROCYCLIC COMPOUNDS FROM CARBOXAMIDE AND CARBOXAMIDE DERIVATIVES WITH HALOALKANOLS

The invention provides for methods for the synthesis of various compounds through reaction of carboxamide, or carboxamide derivatives, with various substituted or unsubstituted haloalkanols in a one-step, single vessel, reaction mechanism. Preferably, but not exclusively, the reaction proceeds in the absence of any solvents, catalyst, base, or any further reagents.