公开(公告)号：US20240059696A1

公开(公告)日：2024-02-22

申请号：US18270781

申请日：2022-02-18

Applicant: OLON S.P.A.

Inventor： Simona TRABACE ,  Stella DE FIORE ,  Matteo FUSARI ,  Jacopo BONANOMI ,  Barbara NOVO ,  Mara SADA ,  Giorgio BERTOLINI

IPC: C07D487/04

CPC classification number: C07D487/04

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.

公开(公告)号：US20210070781A1

公开(公告)日：2021-03-11

申请号：US16771567

申请日：2018-06-25

Applicant: OLON S.P.A.

Inventor： Federico GASSA ,  Lazzaro FELICIANI ,  Alberto MAZZA ,  Marco QUARONI ,  Mara SADA ,  Giorgio BERTOLINI

IPC: C07F5/02

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

公开(公告)号：US20210061757A1

公开(公告)日：2021-03-04

申请号：US17046096

申请日：2019-04-11

Applicant: OLON S.p.A.

Inventor： Filippo NISIC ,  Faris GARIS ,  Corrado COLLI ,  Giorgio BERTOLINI ,  Mara SADA ,  Stefania BERTUOLO ,  Silvano RONZONI ,  Romano DI FABIO ,  Stefano MAIORANA

IPC: C07C269/06 ,  C07C213/02

Abstract: Subject-matter of the present invention is a process for the preparation of optically active phenyl-beta-amino alcohols by means of a specific reduction of the corresponding phenyl-beta-amino ketones. Further subject-matter of the invention are said novel synthesis intermediates and their use for the preparation of active pharmaceutical ingredients.

公开(公告)号：US20220153718A1

公开(公告)日：2022-05-19

申请号：US17438948

申请日：2020-03-09

Applicant: OLON S.P.A.

Inventor： Valentina Grande ,  Barbara Novo ,  Mara SADA ,  Gabriele Ferretti ,  Alessia Manfredi

IPC: C07D401/04

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.

公开(公告)号：US20190194230A1

公开(公告)日：2019-06-27

申请号：US15927264

申请日：2018-03-21

Applicant: OLON S.p.A.

Inventor： Federico GASSA ,  Lazzaro FELICIANI ,  Alberto MAZZA ,  Marco QUARONI ,  Mara SADA ,  Giorgio BERTOLINI

IPC: C07F5/02 ,  C07C37/02 ,  C07C39/15 ,  C07C39/205 ,  B01J23/42 ,  B01J23/44 ,  B01J27/053 ,  B01J27/232

CPC classification number: C07F5/027 ,  B01J23/42 ,  B01J23/44 ,  B01J27/053 ,  B01J27/232 ,  C07B47/00 ,  C07C37/02 ,  C07C39/15 ,  C07C39/205 ,  C07C255/50 ,  C07F5/025

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

公开(公告)号：US20240150282A1

公开(公告)日：2024-05-09

申请号：US18273813

申请日：2021-07-07

Applicant: OLON S.P.A.

Inventor： Matteo VALLI ,  Alberto MAZZA ,  Lazzaro FELICIANI ,  Mara SADA ,  Giorgio BERTOLINI

IPC: C07D205/04

CPC classification number: C07D205/04

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.

公开(公告)号：US20230098051A1

公开(公告)日：2023-03-30

申请号：US17783449

申请日：2020-12-10

Applicant: OLON S.P.A.

Inventor： Giuseppe CREMONESI ,  Christian INVERNIZZI ,  Mara SADA ,  Lazzaro FELICIANI ,  Giorgio BERTOLINI

IPC: C07D401/06

Abstract: A process for the preparation of Lasmiditan and of a synthesis intermediate of formula (II): including reacting a compound of Formula (III) wherein X and Y, each independently, represent a halogen atom, with an aqueous solution of ammonia, in presence of at least one bidentate ligand and of at least one copper-based catalyst, and optionally converting the so-obtained compound of Formula (II) into a salt and/or solvate thereof.

公开(公告)号：US20230322658A1

公开(公告)日：2023-10-12

申请号：US18017713

申请日：2021-07-30

Applicant: OLON S.P.A.

Inventor： Matteo VALLI ,  Mara SADA ,  Lazzaro FELICIANI ,  Giorgio BERTOLINI

IPC: C07C249/12 ,  C07C251/52 ,  C07C249/08

CPC classification number: C07C249/12 ,  C07C249/08 ,  C07C251/52

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.

公开(公告)号：US20190119244A1

公开(公告)日：2019-04-25

申请号：US16093176

申请日：2017-03-23

Applicant: OLON S.P.A.

Inventor： Giorgio BERTOLINI ,  Corrado COLLI ,  Mara SADA ,  Federica COLOMBO

IPC: C07D401/06 ,  C07D491/10

Abstract: Subject-matter of the invention is a process for preparing intermediates useful in the synthesis of drugs, for example antifungal drugs, such as efinaconazole. Subject-matter of the invention are also such novel synthesis intermediates and the use thereof.

公开(公告)号：US20180282339A1

公开(公告)日：2018-10-04

申请号：US15772140

申请日：2016-11-16

Applicant: OLON S.P.A.

Inventor： Giorgio BERTOLINI ,  Lazzaro FELICIANI ,  Ilaria FERRANDO ,  Mara SADA

IPC: C07D487/04

Abstract: Subject-matter of the invention is a process for the preparation of the amorphous form of ibrutinib and a novel crystalline form.