公开(公告)号：US10590156B2

公开(公告)日：2020-03-17

申请号：US15978815

申请日：2018-05-14

申请人： Hoffmann-La Roche Inc.

发明人： Rene Trussardi

IPC分类号： C07H15/08 ,  C07H21/04 ,  C07H1/00

摘要： The invention comprises GalNAc phosphoramidite derivatives of the formula I wherein R1 is a hydroxy protecting group, n is an integer from 0 to 10 and m is an integer from 0 to 20 and its corresponding enantiomers and/or optical isomers thereof. The invention further comprises a process for the preparation of the GalNAc phosphoramidite derivatives of the formula I and its use in the preparation of therapeutically valuable GalNAc-cluster oligonucleotide conjugates.

公开(公告)号：US20180162894A1

公开(公告)日：2018-06-14

申请号：US15890181

申请日：2018-02-06

申请人： Hoffmann-La Roche Inc.

发明人： Joerg Lill ,  Rene Trussardi

IPC分类号： C07H15/08 ,  C07H1/00 ,  C07C229/26 ,  A61K47/54

摘要： The invention comprises a new process for the preparation of GalNAc derivatives of the formula I wherein n is an integer between 0 and 10 and its salts, corresponding enantiomers and/or optical isomers thereof. The GalNAc acid derivative of formula I can be used for the preparation of therapeutically valuable GalNAc oligonucleotide conjugates.

公开(公告)号：US20130060038A1

公开(公告)日：2013-03-07

申请号：US13665980

申请日：2012-11-01

申请人： Hoffmann-La Roche Inc.

发明人： Christophe Pfleger ,  Paul Spurr ,  Rene Trussardi ,  Pius Waldmeier ,  Shaoning Wang

IPC分类号： C07D471/04

CPC分类号： C07D209/44 ,  C07D471/04

摘要： The invention is concerned with a new scalable process for the preparation of compounds of formula I comprising a new process for the preparation of the key intermediate, a dihydropyrrole derivative formula II or a salt thereof.

摘要翻译： 本发明涉及用于制备式I化合物的新的可伸缩方法，其包括制备关键中间体的新方法，式II的二氢吡咯衍生物或其盐。