Abstract: The invention relates to a process for the preparation of Melphalan (4-[bis(2-chloroethyl)amino]-L-phenylalanine of formula (I) said process comprising the reaction of a 4-amino-L-phenylalanine protected at the carboxy and amino aminoacidic groups with an agent able to convert the aromatic amino group into a group of formula: —N(CH2CH2OS(O)nO?)2, wherein n is 1 or 2 followed by conversion of the —N(CH2CH2OS(O)nO?)2 group into a —N(CH2CH2Cl)2 group. The invention also provides novel intermediates useful for the preparation of Melphalan.

Abstract: The invention relates to a process for the preparation of Melphalan (4-[bis(2-5 chloroethyl)amino]-L-phenylalanine of formula (I) said process comprising the reaction of a 4-amino-L-phenylalanine protected at the carboxy and amino aminoacidic groups with an agent able to convert the aromatic amino group into a group of formula: —N(CH2CH2OS(O)nO—)2, wherein n is 1 or 2 followed by conversion of the ?N(CH2CH2OS(O)nO—)2 group into a —N(CH2CH2Cl)2 group. The invention also provides novel intermediates useful for the preparation of Melphalan.

Abstract: The invention relates to a process for the preparation of Melphalan (4-[bis(2-chloroethyl)amino]-L-phenylalanine of formula (I) said process comprising the reaction of a 4-amino-L-phenylalanine protected at the carboxy and amino aminoacidic groups with an agent able to convert the aromatic amino group into a group of formula: —N(CH2CH2OS(O)nO?)2, wherein n is 1 or 2 followed by conversion of the —N(CH2CH2OS(O)nO?)2 group into a —N(CH2CH2Cl)2 group. The invention also provides novel intermediates useful for the preparation of Melphalan.

Abstract: The invention relates to a process for the preparation of colchicine 1 from colchicoside 2 which comprises enzymatic conversion of colchicoside 2 to 3-O-demethylcolchicine 3, wherein the enzyme used is a cellulase. According to another aspect of the invention, 3-O-demethylcolchicine 3 can be converted to colchicine 1 using an alkylating agent. The invention also relates to a process or enriching the colchicine 1 content of extracts from plants belonging to the Colchicaceae family containing colchicine 1, colchicoside 2 and 3-(9-demethyl colchicine 3, which comprises conversion by means of a colchicoside 2 cellulase to 3-O-demethylcolchicine 3, followed by conversion of 3-O-demethylcolchicine 3 to colchicine 1 using an alkylating agent.

Abstract: The invention relates to a process for the preparation of Melphalan (4-[bis(2-5 chloroethyl)amino]-L-phenylalanine of formula (I) said process comprising the reaction of a 4-amino-L-phenylalanine protected at the carboxy and amino aminoacidic groups with an agent able to convert the aromatic amino group into a group of formula: —N(CH2CH2OS(O)nO—)2, wherein n is 1 or 2 followed by conversion of the ?N(CH2CH2OS(O)nO—)2 group into a —N(CH2CH2Cl)2 group. The invention also provides novel intermediates useful for the preparation of Melphalan.

Abstract: The present invention provides novel crystalline forms of 4-[3-Chloro-4-(N?-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide methanesulfonate, as well as methods for their preparation.

Abstract: 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.

Abstract: The present invention provides novel crystalline forms of 4-[3-Chloro-4-(N?-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide methanesulfonate, as well as methods for their preparation.

Abstract: 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.

Abstract: Systems and methods for processing images to recognize characters. Such may include locating background in an image which separate lines of characters, and then locating background which separate characters. The inter-character spaces within a line may be used to determine a probable inter-character spacing for the characters. Within each detected line, the character having an inter-character spacing most similar to the probable inter-character spacing may be set as a starting character for classification. Using the probable inter-character spacing and the location of the starting character, the location of a character adjacent to the starting character in a first direction may be determined and the character classified. Such process may repeat in the first direction until a first end of the line is reached. The process may then move to a character adjacent the starting character in a second direction and repeat until a second end of the line is reached.

Abstract: 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.

Abstract: 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.

Abstract: Systems and methods for processing images to recognize characters. Such may include locating background in an image which separate lines of characters, and then locating background which separate characters. The inter-character spaces within a line may be used to determine a probable inter-character spacing for the characters. Within each detected line, the character having an inter-character spacing most similar to the probable inter-character spacing may be set as a starting character for classification. Using the probable inter-character spacing and the location of the starting character, the location of a character adjacent to the starting character in a first direction may be determined and the character classified. Such process may repeat in the first direction until a first end of the line is reached. The process may then move to a character adjacent the starting character in a second direction and repeat until a second end of the line is reached.

Abstract: 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 characterised by the XRPD pattern, DSC profile and/or TG/DTA profile.

Abstract: The present invention relates to new crystalline forms of Cabazitaxel of formula (I). Specifically, the present invention provides four new crystalline solvate forms of Cabazitaxel, designated as form S2 (solvate with 2-methyltetrahydrofuran), form S4 (solvate with tent-butyl acetate), form S5 (solvate with dimethylcarbonate) and form S6 (solvate with N-methyl-2-pyrrolidinone). A further object of the present invention are processes for the preparation of the above mentioned crystalline forms. The crystalline solvate forms of the invention are especially useful for the preparation of Cabazitaxel, Cabazitaxel salts, and polymorphic forms thereof.

Abstract: 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.

Abstract: 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.

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

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

Abstract: A process for the preparation of 10-deacetyl-bis-7,10-trichloroacetylbaccatin III (VI) said process comprising: reacting 10-deacetylbaccatin III with a trichloroacetic acid activated derivative to obtain a reaction mixture, and performing an isolation step on said reaction mixture obtain purified 10-deacetyl-bis-7,10-trichloroacetylbaccatin III (VI) having a content, of corresponding 7- or 10 mono-trichloroacetyl derivatives lower than 0.1% as determined by HPLC.