公开(公告)号：US20170233383A1

公开(公告)日：2017-08-17

申请号：US15514584

申请日：2015-09-25

申请人： Zachary E. DANCE ,  Scott TRZASKA ,  Yong LIU ,  Richard John VARSOLONA ,  Gregory YORK ,  Merck Sharp & Dohme Corp.

发明人： Scott Trzaska ,  Zachary E. Dance ,  Yong Liu ,  Richard John Varsolona ,  Gregory York

IPC分类号： C07D417/12 ,  C07C309/30

CPC分类号： C07D417/12 ,  C07B2200/13 ,  C07C309/30

摘要： The present invention provides four crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an Aβ pathology and/or a symptom or symptoms thereof. Non-limiting examples of such Aβ pathologies, including Alzheimer's disease, are disclosed herein.

公开(公告)号：US09873707B2

公开(公告)日：2018-01-23

申请号：US15029876

申请日：2014-10-14

申请人： Merck Sharp & Dohme Corp.

发明人： Feng Xu ,  Richard Desmond ,  Guy R. Humphrey ,  Hongming Li ,  Ji Qi ,  Rebecca T. Ruck ,  Zhiguo Jake Song ,  Tao Wang ,  Yong-Li Zhong ,  Jeonghan Park ,  Laura Marie Artino ,  Richard John Varsolona

IPC分类号： C07C69/14 ,  C07K5/083 ,  C07D498/16 ,  C07C69/63 ,  C07D403/12 ,  C07C269/04 ,  C07C271/34 ,  C07C231/12 ,  C07K5/062 ,  C07C27/20 ,  C07C29/36 ,  C07C29/58 ,  C07C45/00 ,  C07C45/63 ,  C07K5/12

CPC分类号： C07D498/16 ,  C07C27/20 ,  C07C29/36 ,  C07C29/58 ,  C07C45/00 ,  C07C45/63 ,  C07C69/14 ,  C07C69/63 ,  C07C231/12 ,  C07C269/04 ,  C07C271/34 ,  C07C2601/02 ,  C07D403/12 ,  C07K5/06034 ,  C07K5/0808 ,  C07K5/126 ,  C07C233/58

摘要： The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.

公开(公告)号：US10017505B2

公开(公告)日：2018-07-10

申请号：US15514584

申请日：2015-09-25

申请人： Merck Sharp & Dohme Corp.

发明人： Scott Trzaska ,  Zachary E. Dance ,  Yong Liu ,  Richard John Varsolona ,  Gregory York

IPC分类号： C07D417/12 ,  C07C309/30

CPC分类号： C07D417/12 ,  C07B2200/13 ,  C07C309/30

摘要： The present invention provides four crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an Aβ pathology and/or a symptom or symptoms thereof. Non-limiting examples of such Aβ pathologies, including Alzheimer's disease, are disclosed herein.