公开(公告)号：US10738013B2

公开(公告)日：2020-08-11

申请号：US16481297

申请日：2018-01-26

申请人： Quimica Sintetica, S.A.

发明人： Giuseppe Barreca ,  Giampiero Ventimiglia ,  Norberto Masciocchi

IPC分类号： C07D233/56

摘要： Novel crystalline forms of Eluxadoline, having the formula (I), are described. Also described are the processes for the preparation of said crystalline forms.

公开(公告)号：US20200179290A1

公开(公告)日：2020-06-11

申请号：US16784716

申请日：2020-02-07

申请人： Quimica Sintetica, S.A.

发明人： Giuseppe Barreca ,  Giampiero Ventimiglia ,  Sonja Bellomi

IPC分类号： A61K9/19 ,  C07C233/47 ,  C07D257/04 ,  A61K31/41 ,  A61K31/216 ,  A61K9/16 ,  A61P9/04 ,  A61P9/12

摘要： Several methods for the preparation of an amorphous powder that includes a 1:1 stoichiometric mixture of the trisodium salts of Valsartan and Sacubitril are described, as well as the resulting amorphous powder, pharmaceutical compositions containing it, and their use in the treatment of essential hypertension and/or cardiac failure.

公开(公告)号：US10689332B2

公开(公告)日：2020-06-23

申请号：US16500673

申请日：2018-03-28

申请人： Quimica Sintetica, S.A.

发明人： Giuseppe Barreca ,  Giovanni Marras ,  Fabio Morana

IPC分类号： C07C315/00 ,  C07C317/00 ,  C07C261/00 ,  C07C315/04 ,  C07C251/16 ,  C07C317/28

摘要： It is described an industrially viable and advantageous process for the preparation of racemic beta-aminosulfone (1), an useful intermediate for the preparation of N-(2-((1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl)acetamide, also known as Apremilast, the latter being suitable for use in methods of treating, preventing and/or managing psoriasis or psoriatic arthritis.

公开(公告)号：US20200087254A1

公开(公告)日：2020-03-19

申请号：US16500673

申请日：2018-03-28

申请人： Quimica Sintetica, S.A.

发明人： Giuseppe Barreca ,  Giovanni Marras ,  Fabio Morana

IPC分类号： C07C315/04

摘要： It is described an industrially viable and advantageous process for the preparation of racemic beta-aminosulfone (1), an useful intermediate for the preparation of N-(2-((1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl)acetamide, also known as Apremilast, the latter being suitable for use in methods of treating, preventing and/or managing psoriasis or psoriatic arthritis.

公开(公告)号：US11149003B2

公开(公告)日：2021-10-19

申请号：US16500671

申请日：2018-03-28

申请人： Quimica Sintetica, S.A.

发明人： Giuseppe Barreca ,  Giovanni Marras ,  Bruno Romanò

IPC分类号： C07D209/48 ,  C07C317/28

摘要： It is described an industrially viable and advantageous process for the preparation of (S)-beta-aminosulfone (1) starting from the corresponding racemic compound, said (S)-beta-aminosulfone being a useful intermediate for the preparation of N-(2-((1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl)acetamide, also known as Apremilast, the latter being suitable for use in methods of treating, preventing and/or managing psoriasis or psoriatic arthritis.

公开(公告)号：US10407456B2

公开(公告)日：2019-09-10

申请号：US15560862

申请日：2016-03-25

申请人： QUIMICA SINTETICA, S.A.

发明人： Giuseppe Barreca ,  Marcello Rasparini ,  Andrea Poggiali ,  Luca Carcone ,  Roberto Rocco Tufaro ,  Giovanni Marras ,  Maurizio Taddei ,  Elena Cini

IPC分类号： C07H19/10 ,  C07H1/00 ,  C07H19/06 ,  C07H1/02

摘要： 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.

公开(公告)号：US20180353430A1

公开(公告)日：2018-12-13

申请号：US15745297

申请日：2016-07-12

申请人： Quimica Sintetica, S.A.

发明人： Giuseppe Barreca ,  Giampiero Ventimiglia ,  Sonja Bellomi

IPC分类号： A61K9/19 ,  A61K9/16 ,  A61K31/41 ,  A61K31/216 ,  A61P9/12 ,  A61P9/04

CPC分类号： A61K9/19 ,  A61K9/1682 ,  A61K31/216 ,  A61K31/41 ,  A61P9/04 ,  A61P9/12 ,  C07C233/47 ,  C07D257/04

摘要： Several methods for the preparation of an amorphous powder comprising a 1:1 stoichiometric mixture of the trisodium salts of Valsartan and Sacubitril are described, as well as the resulting amorphous powder, pharmaceutical compositions containing it, and their use in the treatment of essential hypertension and/or cardiac failure.

公开(公告)号：US10131624B2

公开(公告)日：2018-11-20

申请号：US15523560

申请日：2015-11-03

申请人： QUIMICA SINTETICA, S.A.

发明人： Giuseppe Barreca ,  Bruno Gaetano Romano

IPC分类号： C07C233/57 ,  C07C231/06 ,  C07C231/12 ,  C07C231/02

摘要： The invention relates to a process for the preparation of Levomilnacipran or salts thereof, compounds useful in the treatment of depression, with high yield.