Abstract: Industrially viable and advantageous processes for the preparation of Ozanimod are described. The invention also discloses the intermediates obtained in the process.

Abstract: The invention discloses a process for the preparation of maytansinoid esters of formula (I) comprising a thiol or disulphide group wherein R1, R4 and R5 and the asterisk are as defined in the description, by reacting maytansinol with an enantiopure alpha-azido acid, followed by reduction of the azido group and reacting the obtained amino-ester with a compound of formula (IX) (IX) R3—S—S—X—COOH wherein X and R3 are as defined in the description, or with a reactive derivative thereof and optionally reducing the obtained disulfide-containing maytansinoid ester to give a maytansinoid ester wherein R1 is a —X—SH group.

Abstract: The invention discloses a process for the preparation of maytansinoid esters of formula (I) comprising a thiol or disulphide group wherein R1, R4 and R5 and the asterisk are as defined in the description, by reacting maytansinol with an enantiopure alpha-azido acid, followed by reduction of the azido group and reacting the obtained amino-ester with a compound of formula (IX) (IX) R3—S—S—X—COOH wherein X and R3 are as defined in the description, or with a reactive derivative thereof and optionally reducing the obtained disulfide-containing maytansinoid ester to give a maytansinoid ester wherein R1 is a —X—SH group.

Abstract: Industrially viable and advantageous processes for the preparation of Ozanimod are described. The invention also discloses the intermediates obtained in the process.

Abstract: The present invention relates to novel Histone Deacetylase Inhibitors (HDACi)-based antibody drug conjugates particularly with antibodies directed to ErbB, ErbB2 and ErbB3 receptors, pharmaceutical compositions comprising said antibodies as well as to their use in the treatment of cancer or tumor and other diseases where a modulation of one or more histone deacetylase isoforms can be effective for therapeutic interventions.

Abstract: Two processes are described for preparing, in different diastereomeric purity degrees, the compound (S)-isopropyl-2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)-phosphoryl)amino) propanoate, having the formula given below, known as Sofosbuvir and used for the treatment of hepatitis C.

Abstract: Two processes are described for preparing, in different diastereomeric purity degrees, the compound (S)-isopropyl-2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)-phosphoryl)amino) propanoate, having the formula given below, known as Sofosbuvir and used for the treatment of hepatitis C.

Abstract: The invention relates to a process for the synthesis of Cariprazine, an antipsychotic compound useful in the treatment of positive and negative symptoms associated to schizophrenia, with the following structural formula: (A) The invention further relates to the synthesis of intermediates useful in the preparation of Cariprazine.

Abstract: The invention relates to a process for the synthesis of Cariprazine, an antipsychotic compound useful in the treatment of positive and negative symptoms associated to schizophrenia, with the following structural formula: (A) The invention further relates to the synthesis of intermediates useful in the preparation of Cariprazine.

Abstract: A new route of synthesis of the compound Aliskiren of formula (I), used in the treatment of hypertension, is described.

Abstract: The present invention relates to aryl triazole derivatives of Formula I having antitumoural activity through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical composition containing such compounds.

Abstract: The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them.

Abstract: The present invention relates to compounds which are quinolinone derivatives of general formula (I) capable of modulating the activity, in particular of inducing the differentiation, of stem and progenitor cells; these compounds are of use in the treatment of disorders related to a stem differentiation defect; the invention also relates to novel compounds among these quinolinone derivatives and to pharmaceutical compositions containing the same.

Abstract: The invention relates to compounds of formula (I), and the use thereof as a drug, particularly for the treatment of tumors associated with hyperactivation of the hedgehog protein signaling pathway, treatment of neurodegenerative diseases, treatment of diseases related to cerebral development (holoprosencephaly), for stem cell monitoring treatment of cerebrovascular accidents and cardiovascular accidents, treatment of diseases involving oligodendrocytes and diseases involving neurolemmocytes, for application thereof in vitro for modulating human or animal stem cell renewal, and for the treatment of diabetes. The invention also relates to pharmaceutical compositions having a compound of formula (I).

Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.

Abstract: The present invention relates to aryl triazole derivatives of Formula I having antitumoural activity through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical composition containing such compounds.

Abstract: Process for the preparation of a viral protease inhibitor and intermediates useful in its preparation.

Abstract: Process for the preparation of a piperazinyl derivative, and its intermediates, which has known activity as a serotonin reuptake inhibitor and is used in therapy for treating serious symptoms of depression in adults.

Abstract: The invention relates to compounds of formula (I), and the use thereof as a drug, particularly for the treatment of tumors associated with hyperactivation of the hedgehog protein signaling pathway, treatment of neurodegenerative diseases, treatment of diseases related to cerebral development (holoprosencephaly), for stem cell monitoring treatment of cerebrovascular accidents and cardiovascular accidents, treatment of diseases involving oligodendrocytes and diseases involving neurolemmocytes, for application thereof in vitro for modulating human or animal stem cell renewal, and for the treatment of diabetes. The invention also relates to pharmaceutical compositions having a compound of formula (I).

Abstract: The present invention relates to compounds which are quinolinone derivatives of general formula (I) capable of modulating the activity, in particular of inducing the differentiation, of stem and progenitor cells; these compounds are of use in the treatment of disorders related to a stem differentiation defect; the invention also relates to novel compounds among these quinolinone derivatives and to pharmaceutical compositions containing the same.