Indena S.p.a.

Inverni Della Beffa Spa

Societe De Recherches Industrielles Sori

I D B Holding S.p.a.

Sigma-tau Industrie Farmaceutiche Riunite S.p.a.

Inverni Della Beffa Industria Chimico Farmeceutica Derivati Naturali

Enrico Mercalli

Bruno Gabetta

Ezio Bombardelli

Maria J Magistretti

Andrea Gambini

Daniele Ciceri

Gianfranco Zini

Paolo De Bellis

Paolo Morazzoni

Gabriele Fontana

Philippe L Dostert

Alessandro Pontiroli

Giorgio Pifferi

Beat Theodor Weber

Piero Foresta

Aldo Cristoni

Orlando Ghirardi

Attilio Bonati

Marisa Conti

Nicola Sardone

Maurizio Ricotti

Raffaello Giorgi

Frieder Mitzel

Robert Seghizzi

Nicola Vignola

Stephen Beszant

Beat T Weber

A process for the preparation of 10-deacetyl-7,10-bis-trichloroacetylbaccatine III with HPLC purity higher than 99% and free from 2-debenzoyl-2-pentenoylbaccatine III by purification of 10-deacetyl-7,10-bis-trichloroacetylbaccatineIII followed by alkaline hydrolysis of the protecting groups in position 7 and 10.

Process for the purification 10-deacetylbaccatine III from 10-deacetyl-2-debenzoyl-2-pentenoylbaccatine III

The present invention relates to solid forms of 13-(N-Boc-&#x3b2;-isobutylserinyl)-14-&#x3b2; hydroxybaccatin III 1, 14-carbonate (Ortataxel). Amorphous Form A, crystalline Form B, mixtures thereof and processes for preparing them are disclosed. Amorphous Form A is prepared by fast precipitation of Ortataxel from a mixture of acetone and water. Form A transforms in Form B when suspended and stirred in a mixture of ethanol and water for 4-8 hours. If the suspension is stirred for less than 4 hours, mixtures of Form B and Form A are obtained. Form B or mixtures of Forms A and B can also be obtained dissolving Ortataxel in a protic organic solvent, followed by addition of water.

Solid forms of ortataxel

A process for the preparation of compounds having formula (I) is disclosed, wherein: &#x2014;Ris a methoxy or methylthio group; &#x2014;Ris a O-glycosyloxy residue. Compounds having formula (I) are prepared by reacting the corresponding precursor having R&#x2550;OH and the suitably protected 1-acetyl-glycose. 

Process for the glycosidation of colchicine and thiocolchicine

A process for the preparation of 10-deacetyl-bis-7,10-trichloroacetylbaccatin III (VI) 

Semisynthesis process for the preparation of 10 deacetyl-N-debenzoyl-paclitaxel

A process for the enantioselective preparation of (2R,3S)-3-phenylisoserine methyl ester acetate salt of formula (I) which is an useful building block for the synthesis of taxane derivatives. The process involves the resolution of racemic threo-phenylisoserine amide and its conversion into (I). 

Process for the preparation of (2R,3S)-3-phenylisoserine methyl ester acetate salt

A process for the purification of galanthamine (I) comprising precipitation of galanthamine hydrobromide from a mixture of alkaloids obtained from a plant of the Amaryllidaceae family containing galanthamine, treatment of the hydrobromide with alkali, extraction and crystallization of galanthamine with a solvent of general formula (II), in which Ris hydrogen or methyl and Ris selected from n-butyl, isobutyl, sec-butyl and t-butyl. The resulting pure galanthamine can be conveniently used for the preparation of galanthamine hydrobromide. 

Process for the preparation of galanthamine hydrobromide

A novel taxane derivative with anticancer activity, a process for its preparation and a process for the preparation of 14-&#x3b2;-hydroxy-1,14-carbonate-baccatine III and V derivatives 13-substituted by an isoserine residue.

Taxane derivatives and processes for the preparation thereof

A process is provided for the preparation of 10-deacetyl-N-debenzoyl-paclitaxel (I) a synthon useful for the preparation of taxanes with antitumour activity, and intermediates for the preparation thereof. Also described is a process for the preparation of Docetaxel starting from the compound of formula (I).

Semisynthesis process for the preparation of 10-deacetyl-N-debenzoyl-paclitaxel

The invention relates to an improved process for the synthesis of 13-(N-Boc-&#x3b2;-isobutylserinyl)-14-&#x3b2;-hydroxybaccatin III-1,14-carbonate (I), wherein carbonation of the 1,14-hydroxy groups of the baccatin skeleton is carried out with bis(trichloromethylcarbonate and the 7-hydroxy group is protected with a trichloroacetyl group.

Process for the preparation of a taxane derivative

Methods for obtaining paclitaxel from plants containing paclitaxel are disclosed. Plant material is first obtained from plants containing paclitaxel. Paclitaxel is then extracted from the plant material. Subsequently, paclitaxel is separated from the paclitaxel extract using a series of column chromatography separation steps to obtain at least one fraction containing paclitaxel. The paclitaxel in a fraction that is obtained from the final chromatography step is crystallized. Using these methods, high purity paclitaxel may be efficiently obtained from plants containing paclitaxel.

Methods for obtaining paclitaxel from taxus plants

A soya extract having a content of glucoside isoflavones of at least 13% by weight and a content of 0.6 to 1.5 parts by weight of group 3 soya saponins per 1 part by weight of glucoside isoflavones. Also, pharmaceutical compositions containing this extract and methods of administering the extract to treat conditions such as pre- or post-menopausal symptoms, cancer, such as breast or prostate cancer, or alcoholism. The extracts are made by a process which includes the steps of treating ripe whole soya beans or oil-free soya flour with an aliphatic alcohol to obtain a first extract; concentrating the first extract to form a concentrated first extract; purifying the concentrated first extract by treatment with at least one aliphatic hydrocarbon; and extracting active components from the purified concentrated first extract with a water-immiscible aliphatic alcohol to obtain a second extract. Preferably, the final extract is concentrated dried to form the desired soya extract.

Methods of treatment using a soya extract

A soya extract having a content of glucoside isoflavones of at least 13% by weight and a content of 0.6 to 1.5 parts by weight of group B soya saponins per 1 part by weight of glucoside isoflavones. Also, pharmaceutical compositions containing this extract and methods of administering the extract to treat conditions such as pre- or post-menopausal symptoms, cancer, such as breast or prostrate cancer, or alcoholism. The extracts are made by a process which includes the steps of treating ripe whole soya beans or oil-free soya flour with an aliphatic alcohol to obtain a first extract; concentrating the first extract to form a concentrated first extract; purifying the concentrated first extract by treatment with at least one aliphatic hydrocarbon; and extracting active components from the purified concentrated first extract with a water-immiscible aliphatic alcohol to obtain a second extract. Preferably, the final extract is concentrated and dried to form the desired soya extract.

Soya extract, process for its preparation and pharmaceutical composition

The invention relates to a method for extracting (St.-Johns-wort) by fractioning water-alcohol, alcohol extracts of the plant with esters of water-immiscible C -C alcohols. The extracts have high activity and are stable over time. The invention also relates to formulations containing the extract.

Extracts of Hypericum perforatum and formulations containing them

The extract of the pericarp of prepared by extraction with carbon dioxide in supercritical conditions, has remarkable analgesic activity without exerting the local anesthetic activity characteristic of the extracts obtained by solvent means. The product of the present invention is prepared by extracting the pericarp of finely ground or transformed into pellets, with carbon dioxide under pressure conditions ranging from 150 to 300 bars at temperatures ranging from 35 to 55&deg; C.

Growing community of inventors

Milan, Italy

Bruno Gabetta