Abstract: The present invention relates to a novel crystalline compound of Siponimod Hemifumarate, to processes and to intermediates for its preparation, to pharmaceutical compositions containing it and to the use in therapy.

Abstract: A process for preparing Larotrectinib sulfate includes: comprising (a) conducting unblocking reaction of Larotrectinib hydrochloride in a chlorinated hydrocarbon in a presence of a base to obtain Larotrectinib; (b) treating the Larotrectinib with sulfuric acid in methyl ethyl ketone and water to obtain Larotrectinib sulfate; (c) filtering the Larotrectinib sulfate. A content of S-Larotrectinib in the Larotrectinib sulfate is less than 0.10% by weight.

Abstract: The present invention relates to a process for the preparation of Apalutamide of formula (A) Apalutamide is a latest-generation androgen receptor inhibitor, used to treat non-metastatic castration-resistant prostate cancer.

Abstract: The present invention relates to a process for the preparation of a key intermediate and other intermediates useful for the synthesis of Siponimod, a drug used for the treatment of multiple sclerosis. Object of the invention are also said novel intermediates.

Abstract: The invention relates to a process for the preparation of Lifitegrast of formula (I), which comprises: a) condensation of the compound of formula (II) with the compound of formula (III) to give the compound of formula (IV) wherein R1, R2 and R3 are independently selected from straight or branched C1-C6 alkyl groups; b) chlorination of compound (IV) in the presence of a chlorinating agent (IV), (V), c) condensation of compound (V) with amino acid (VI) to give compound (I), c) condensation of compound (V) with amino acid (VI) to give compound (I), d) optional purification of the crude Lifitegrast in mixtures of polar aprotic solvents and water.

Abstract: The present invention relates to a novel non-solvated crystalline form of apalutamide in pure, stable form, and the process for the preparation thereof.

Abstract: The present invention relates to a process for the preparation of apalutamide in stable amorphous form. The invention also relates to a novel intermediate crystalline form, called form X, which gives rise to said amorphous form, and a process for obtaining said form X.

Abstract: The present invention relates to a process for the preparation of crisaborole of formula (I): by preparing intermediates of formulas (II) and (III):

Abstract: Disclosed is a process for the synthesis of pimavanserin base with a high yield and purity, which comprises: a) converting tert-butyl-N-[(4-propan-2-yloxyphenyl)methyl]carbamate (Formula (I)) to 1-(isocyanatomethyl)-4-propan-2-yloxybenzene of formula (II) b) adding N-[(4-fluorophenyl)methyl]-1-methylpiperidin-4-amine (Formula (IV)) to the solution obtained in a) to give pimavanserin base, and c) purifying the pimavanserin base obtained in step b).

Abstract: Disclosed is a process for the preparation of Cangrelor in salt form by preparation and subsequent hydrolysis of an intermediate of formula (IV): The process is characterized by the high yield and purity of the product, and can be used industrially.

Abstract: The invention relates to a process for the preparation of Lifitegrast of formula (I), which comprises: a) condensation of the compound of formula (II) with the compound of formula (III) to give the compound of formula (IV) wherein R1, R2 and R3 are independently selected from straight or branched C1-C6 alkyl groups; b) chlorination of compound (IV) in the presence of a chlorinating agent (IV), (V), c) condensation of compound (V) with amino acid (VI) to give compound (I), c) condensation of compound (V) with amino acid (VI) to give compound (I), d) optional purification of the crude Lifitegrast in mixtures of polar aprotic solvents and water.

Abstract: The present invention relates to a process for the preparation of Apalutamide of formula (A) Apalutamide is a latest-generation androgen receptor inhibitor, used to treat non-metastatic castration-resistant prostate cancer.

Abstract: Subject-matter of the present invention is a process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction of the corresponding beta-amino ketones. Subject-matter of the invention are also said novel synthesis intermediates and the use thereof in the preparation of active pharmaceutical ingredients, among which vilanterol and the salts thereof.

Abstract: The present invention relates to a process for the preparation of a novel and versatile synthesis intermediate and its use in the preparation of umeclidinium. The invention also relates to some reference standards allowing to detect impurity traces recurring in the preparation of umeclidinium and a process for their preparation.

Abstract: Disclosed is a process for the synthesis of pimavanserin base with a high yield and purity, which comprises: a) converting tert-butyl-N-[(4-propan-2-yloxyphenyl)methyl]carbamate (Formula (I)) to 1-(isocyanatomethyl)-4-propan-2-yloxybenzene of formula (II) b) adding N-[(4-fluorophenyl)methyl]-1-methylpiperidin-4-amine (Formula (IV)) to the solution obtained in a) to give pimavanserin base, and c) purifying the pimavanserin base obtained in step b).

Abstract: Disclosed are new crystalline forms of venetoclax, a selective Bcl2 inhibitor used as a chemotherapy agent, and the processes for preparation of said crystalline forms by treating venetoclax with suitable solvents.

Abstract: Subject-matter of the invention is a process for the preparation of key intermediates in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates.

Abstract: Disclosed is a partly crystalline form of nintedanib ethanesulphonate and its preparation process.

Abstract: The present invention relates to a process for the preparation of crisaborole of formula (I): by preparing intermediates of formulas (II) and (III):

Abstract: Subject-matter of the invention is a process for the preparation of a key intermediate in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates.