Indena S.p.a.

Daniele Ciceri

Andrea Gambini

Federico Peterlongo

Bruno Gabetta

Nicola Sardone

Maurizio Ricotti

Walter Cabri

Pietro Allegrini

Luca Domenighini

Beat Theodor Weber

Massimo Ronchi

Anna Bernardi

Katia Miele

Nicola Vignola

Luca Senaldi

Frieder Mitzel

Beat T Weber

Disclosed is a process for the purification of staurosporine (1), which comprises salification of staurosporine (1) (Formula (1)) by treatment with a mineral acid to give a precipitated salt, isolation of the staurosporine (1) precipitated salt, treatment of the staurosporine (1) isolated salt with an organic base, and isolation of staurosporine (1). Also disclosed are novel polymorphic forms of the mono- and bis-hydrochloride salts of staurosporine (1).

Process for the purification of indole carbazole alkaloids

The present invention relates to a process for the preparation of Lenvatinib of formula (I) from 4-amino-3-chloro-phenol and 4-chloro-7-methoxyquinoline-6-carboxamide.

Process for the preparation of Lenvatinib

The invention relates to a solid dispersion comprising Coenzyme Qand a phospholipid, in the presence of a cellulosic derivative and/or a polymeric material selected from the group consisting of polyvinylpyrrolidone, polyvinyl acetate, poly (methacrylic acid, methyl methacrylate), poloxamers, chitosan, alginates, hyaluronic acid, pectin, pullulan, cyclodextrins, starch polymers, D-alpha-tocopheryl polyethylene glycol 1000 succinate.

Solid dispersions of Coenzyme Q

Disclosed are solid forms of ingenol 3-(3,5-diethylisoxazole-4-carboxylate) selected from an amorphous form or a crystalline anhydrous form. Also disclosed are solid solvates of ingenol 3-(3,5-diethylisoxazole-4-carboxylate) selected from an acetone solvate, a dimethylcarbonate solvate, an isopropyl ether solvate, an acetonitrile solvate, a toluene solvate, a mesitylene solvate, a nitromethane solvate, a dichloromethane/heptane solvate and an ethyl acetate solvate, for use as intermediates.

Solid forms of ingenol 3-(3,5-diethylisoxazole-4-carboxylate) and method for preparing the same

The present invention refers to an amorphous form of a thiocolchicine derivative, IDN 5404, to a process for producing it and to pharmaceutical compositions thereof. The amorphous form is characterized by the XRPD pattern, DSC profile and/or TG/DTA profile.

Amorphous form of a thiocolchicine derivative

The present invention relates to a new anhydrous crystalline form of Cabazitaxel of formula (I), designated as form H. A further object of the present invention is a processes for the preparation of the above mentioned form H by recrystallization of Cabazitaxel from a mixture of decanoyl- and octanoyl triglycerides or from glycerol trioctanoate. Form H of Cabazitaxel is useful for the preparation of Cabazitaxel, Cabazitaxel salts, and polymorphic forms thereof. It is also particularly useful as a medicament, especially for the treatment of cancers. 

Crystalline anhydrous form of Cabazitaxel, process for the preparation and pharmaceutical compositions thereof

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 crystalline from of 13-[(N-tert-butoxycarbonyl)-2'-O-hexanoyl-3-phenylisoserinyl]-10-deacetylbaccatin III.

Crytalline form of 13-[(N-tert-butoxycarbonyl)-2'-O-hexanoyl-3-phenylisoserinyl]-10-deacetylbaccatin III

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

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.

Growing community of inventors

Milan, Italy

Daniele Ciceri