C07D311/04

PROCESS FOR THE PRODUCTION OF CANNABIDIOL AND DELTA-9-TETRAHYDROCANNABINOL
20180319763 · 2018-11-08 · ·

The present disclosure relates to the preparation of a cannabidiol compound or a derivative thereof. The cannabidiol compound or derivatives thereof can be prepared by an acid-catalyzed reaction of a suitably selected and substituted di-halo-olivetol or derivative thereof with a suitably selected and substituted cyclic alkene to produce a dihalo-cannabidiol compound or derivative thereof. The dihalo-cannabidiol compound or derivative thereof can be produced in high yield, high stereospecificity, or both. It can then be converted under reducing conditions to a cannabidiol compound or derivatives thereof.

PROCESS FOR THE PRODUCTION OF CANNABIDIOL AND DELTA-9-TETRAHYDROCANNABINOL
20180319763 · 2018-11-08 · ·

The present disclosure relates to the preparation of a cannabidiol compound or a derivative thereof. The cannabidiol compound or derivatives thereof can be prepared by an acid-catalyzed reaction of a suitably selected and substituted di-halo-olivetol or derivative thereof with a suitably selected and substituted cyclic alkene to produce a dihalo-cannabidiol compound or derivative thereof. The dihalo-cannabidiol compound or derivative thereof can be produced in high yield, high stereospecificity, or both. It can then be converted under reducing conditions to a cannabidiol compound or derivatives thereof.

Therapeutic compounds

The invention provides compounds formula (I) and salts thereof: wherein the bond represented by ---- is a single bond or a double bond, and R1 has any of the values defined in the specification. The compounds are useful for treating conditions including Alzheimer's disease, Parkinson's disease, diabetes, cancer, and psychotic disorders such as schizophrenia. ##STR00001##

Therapeutic compounds

The invention provides compounds formula (I) and salts thereof: wherein the bond represented by ---- is a single bond or a double bond, and R1 has any of the values defined in the specification. The compounds are useful for treating conditions including Alzheimer's disease, Parkinson's disease, diabetes, cancer, and psychotic disorders such as schizophrenia. ##STR00001##

A PROCESS FOR THE PURIFICATION OF ANTHOCYANINS AND ANTHOCYANIDINS FROM NATURAL EXTRACTS USING ADSORPTION RESINS AND ACIDIFIED WATER AS DESORBENT

A purification process of anthocyanins and anthocyanidins which allows purity increases of at least 3.5 times the initial purity of the extract with yields greater than 50% of recovery, having the following steps: a) contacting the anthocyanin- and anthocyanidin-containing extract with a non-ionic adsorption resin to retain the anthocyanins and anthocyanidins; and b) eluting the resin using water acidified with a monocarboxylic acid at a concentration in the range of 0.01 to 1 M at a temperature between 35 to 100? C., which avoids the use of organic solvents and only uses compounds suitable for human consumption.

A PROCESS FOR THE PURIFICATION OF ANTHOCYANINS AND ANTHOCYANIDINS FROM NATURAL EXTRACTS USING ADSORPTION RESINS AND ACIDIFIED WATER AS DESORBENT

A purification process of anthocyanins and anthocyanidins which allows purity increases of at least 3.5 times the initial purity of the extract with yields greater than 50% of recovery, having the following steps: a) contacting the anthocyanin- and anthocyanidin-containing extract with a non-ionic adsorption resin to retain the anthocyanins and anthocyanidins; and b) eluting the resin using water acidified with a monocarboxylic acid at a concentration in the range of 0.01 to 1 M at a temperature between 35 to 100? C., which avoids the use of organic solvents and only uses compounds suitable for human consumption.

ISOFORM SPECIFIC AGONISTS TARGETING AKT KINASE

The invention relates in one aspect to compounds, pharmaceutical compositions thereof, and methods using the same for selectively activating either all or a single isoform of Akt. Isoform selective-targeting is necessary for avoiding pathologies driven by concomitantly activated Akt1, Akt2 and/or Akt3.

ISOFORM SPECIFIC AGONISTS TARGETING AKT KINASE

The invention relates in one aspect to compounds, pharmaceutical compositions thereof, and methods using the same for selectively activating either all or a single isoform of Akt. Isoform selective-targeting is necessary for avoiding pathologies driven by concomitantly activated Akt1, Akt2 and/or Akt3.

Chromene derivatives and their analogs as Wnt pathway antagonists

Compounds of formula (IIc); wherein X.sup.3 and X.sup.4 independently from each other are N or CR.sup.8 wherein R.sup.8 may be same or different; Y.sup.1, Y.sup.2, Y.sup.3 and Y.sup.4 independently from each other are N or CR.sup.9 wherein R.sup.9 may be same or different and wherein up to 3 of the group Y.sup.1, Y.sup.2, Y.sup.3 and Y.sup.4 may be N; their solvates, hydrates, and pharmaceutically acceptable salts, their use for modulating the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer. ##STR00001##

Chromene derivatives and their analogs as Wnt pathway antagonists

Compounds of formula (IIc); wherein X.sup.3 and X.sup.4 independently from each other are N or CR.sup.8 wherein R.sup.8 may be same or different; Y.sup.1, Y.sup.2, Y.sup.3 and Y.sup.4 independently from each other are N or CR.sup.9 wherein R.sup.9 may be same or different and wherein up to 3 of the group Y.sup.1, Y.sup.2, Y.sup.3 and Y.sup.4 may be N; their solvates, hydrates, and pharmaceutically acceptable salts, their use for modulating the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer. ##STR00001##