Sinclair Pharmaceuticals Limited

Enantia, S.l.

Union Quimico-farmaceutica S.a.

Finorga Sas

Alexander Christian Comely

Nicolas Tesson

Llorenç Rafecas Jané

Xavier Verdaguer Espaulella

Antonio Domingo Coto

Llorenç Rafecas Jane

Antoni Riera Escale

Montserrat Trilla Castaño

Marta Marfil Sánchez

Carmen Jiménez González

Francesc Xavier Verdaguer Espaulella

Antoni Riera Escalé

Atoni Escale Riera

The present invention relates to solid compositions comprising cocrystals of cannabinoids, processes for their preparation, and their use as in therapy or in cosmetics or for the purification of cannabinoids. It also relates to cocrystals of cannabinoids.

Solid compositions of cocrystals of cannabinoids

The present invention relates to cocrystals of 2-[(1R,6R)-6-isopropenyl-3-methylcyclohex-2-en-1-yl]-5-pentylbenzene-1,3-diol and a zwitterion coformer, processes for their preparation, and their use as a medicament and for the purification of 2-[(1R,6R)-6-isopropenyl-3-methylcyclohex-2-en-1-yl]-5-pentylbenzene-1,3-diol. The invention also relates to compositions comprising the cocrystal.

Cocrystal of 2-[(1R,6R)-6-isopropenyl-3-methylcyclohex-2-en-1-yl]-5-pentylbenzene-l,3-diol

It comprises a process for the production of delmopinol or a pharmaceutically acceptable salt and/or a solvate thereof, by subjecting the compound of formula (II) where R1 and R2 are the same or different, independently selected from the group consisting of H, (C1-C6) alkyl or, alternatively, R1 and R2 form, together with the carbon atom to which they are attached, a (C5-C6) cycloalkyl radical; and R3 is a radical selected from the group consisting of CF3, (C1-C4) alkyl, phenyl, and phenyl mono- or disubstituted by a radical selected from the group consisting of (C1-C4)-alkyl, halogen and nitro to a deprotection and cyclisation reaction. The process is useful to prepare delmopinol or its salts on an industrial scale. The compound of formula (II) is new and also forms part of the present invention, as well as its preparation process and other new intermediates of said preparation process. 

Preparation of delmopinol

A process for the preparation of an 11-(4-substituted-1-piperazinyl)dibenzo[b,f][1,4]thiazepine derivative, of general Formula (I), where A is hydrogen or a &#x2014;(CH)&#x2014;OH group or a &#x2014;(CH)-0-(CH)&#x2014;OH group, or of a salt thereof, comprises a step in which 10H-dibenzo[b,f][1,4]thiazepin-11-one is reacted with a piperazine derivative in the presence of a titanium alkoxide of general formula Ti(OR), where R is a straight or branched alkyl group, having from one to eight carbon atoms to obtain said Formula I derivative or a salt thereof. Where A is &#x2014;CH)-0-(CH)&#x2014;OH, then the piperazine derivative is 1-(2-(2-hydroxyethoxy)ethyl)piperazine and the 11-(4-substituted-1-piperazinyl)dibenzo[b,f][1,4]thiazepine is quetiapine, (11-(4-(2-(2-hydroxyethoxy)ethyl)-1-piperazinyl)dibenzo[b,f][1,4]thiazepine). The process may comprise an additional step of reacting the quetiapine with fumaric acid to obtain quetiapine hemifumarate. 

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It comprises a preparation process of delmopinol or a pharmaceutically acceptable salt and/or a solvate thereof, by submitting the compound of formula (II) where Rand Rare the same or different, independently selected from the group consisting of H, (C-C)-alkyl or, alternatively, Rand Rform, together with the carbon atom to which they are attached, a (C-C)-cycloalkyl radical; and Ris a radical selected from the group consisting of CF, (C-C)-alkyl, phenyl, and phenyl mono- or disubstituted by a radical selected from the group consisting of (C-C)-alkyl, halogen and nitro to a deprotection and cyclisation reaction. The process is useful to prepare delmopinol or its salts on an industrial scale. The compound of formula (II) is new and also forms part of the present invention, as well as its preparation process and other new intermediates of said preparation process. 

A process for the preparation of (S)-omeprazole from racemic omeprazole via the formation of an inclusion complex with (S)-1,1,2-triphenyl-1,2-ethanediol. (S)-Omeprazole is recovered in a substantially optically pure form either in neutral form or as a pharmaceutically acceptable salt or as its solvates including hydrates. The (S)-omeprazole 2[(S)-1,1,2-triphenyl-1,2-ethanediol] inclusion complex is new. This resolution process proceeds with high yields and high optical purity.

Process for the preparation of the (S)-enantiomer of omeprazole

Process for the obtaining of 1-adamantane (tricycle[3.3.1.1 (3,7)]decane) derivatives, or of a pharmaceutically acceptable salt thereof, based on a carboxylation reaction, via metallation, of a precursor compound with an adequate leaving group. It also comprises the preparation of the precursor compound by means of a selective coupling of the corresponding boron, magnesium or zinc derivative with the corresponding disubstitute aromatic derivative. It is especially useful for the obtaining of Adapalene at industrial scale with good yield and high purity.

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Barcelona, Spain

Alexander Christian Comely