C07C323/22

1,3-Di-oxo-indene derivative, pharmaceutically acceptable salt or optical isomer thereof, preparation method thereof, and pharmaceutical composition containing same as an antiviral, active ingredient

Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, cold, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.

1,3-Di-oxo-indene derivative, pharmaceutically acceptable salt or optical isomer thereof, preparation method thereof, and pharmaceutical composition containing same as an antiviral, active ingredient

Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, cold, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.

VISIBLE LIGHT ACTIVE BIOMASS DERIVED PHOTOINITIATORS

Biomass derived benzoin derivatives, and methods of making and using the same, are described. Benzoin derivatives may be used as visible light photoinitiators.

VISIBLE LIGHT ACTIVE BIOMASS DERIVED PHOTOINITIATORS

Biomass derived benzoin derivatives, and methods of making and using the same, are described. Benzoin derivatives may be used as visible light photoinitiators.

CATALYTIC OXIDATION OF BUT-3-ENE-1,2-DIOL

The invention concerns a synthesis process of a compound of the following formula (I) or one of the salts thereof,

##STR00001## wherein R represents a COOH, CH.sub.2OH or CHO group, comprising the step according to which the but-3-ene-1,2-diol (BDO) is subjected to an oxidation in the presence of a catalyst, said catalyst comprising an active phase based on at least one noble metal selected from palladium, gold, silver, platinum, rhodium, osmium, ruthenium and iridium, and a support containing alkaline sites.

The invention also concerns the application of this reaction to the preparation of bioavailable compounds of methionine used, in particular, in animal nutrition.

CATALYTIC OXIDATION OF BUT-3-ENE-1,2-DIOL

The invention concerns a synthesis process of a compound of the following formula (I) or one of the salts thereof,

##STR00001## wherein R represents a COOH, CH.sub.2OH or CHO group, comprising the step according to which the but-3-ene-1,2-diol (BDO) is subjected to an oxidation in the presence of a catalyst, said catalyst comprising an active phase based on at least one noble metal selected from palladium, gold, silver, platinum, rhodium, osmium, ruthenium and iridium, and a support containing alkaline sites.

The invention also concerns the application of this reaction to the preparation of bioavailable compounds of methionine used, in particular, in animal nutrition.

Inhibitors of the N-terminal domain of the androgen receptor

The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.

PHARMACEUTICAL PROCESS AND INTERMEDIATES

The present disclosure concerns the large-scale manufacture of pharmaceutical compounds, and novel intermediates for use in the manufacture. International Patent Application WO2011154737 discloses morpholine pyrimidines useful for treating cancer, processes for their preparation and pharmaceutical compositions thereof. In particular, WO2011154737 discloses, as experimental Example 2.02 on page 60, the compound 4-{4-[(3R)-3-methylmorpholin-4-yl]-6-[1-((R)—S-methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl}-1H-pyrrolo[2,3-b]pyridine (hereafter referred to as the compound of Formula (I)). The structure of the compound of Formula (I) is shown below. A synthetic route to the compound of Formula (I) is described at pages 51 to 57, 66 and 67 of WO2011154737, and is summarised below in Scheme 1.

##STR00001##

PHARMACEUTICAL PROCESS AND INTERMEDIATES

The present disclosure concerns the large-scale manufacture of pharmaceutical compounds, and novel intermediates for use in the manufacture. International Patent Application WO2011154737 discloses morpholine pyrimidines useful for treating cancer, processes for their preparation and pharmaceutical compositions thereof. In particular, WO2011154737 discloses, as experimental Example 2.02 on page 60, the compound 4-{4-[(3R)-3-methylmorpholin-4-yl]-6-[1-((R)—S-methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl}-1H-pyrrolo[2,3-b]pyridine (hereafter referred to as the compound of Formula (I)). The structure of the compound of Formula (I) is shown below. A synthetic route to the compound of Formula (I) is described at pages 51 to 57, 66 and 67 of WO2011154737, and is summarised below in Scheme 1.

##STR00001##

Field effect transistor

A heterocyclic compound represented by formula (1) and a field effect transistor having a semiconductor layer comprising the compound. (In the formula, X.sup.1 and X.sup.2 each independently represents a sulfur atom or a selenium atom, and R.sup.1 and R.sup.2 each independently represents a C.sub.5-16 alkyl.) ##STR00001##