公开(公告)号：US20240182511A1

公开(公告)日：2024-06-06

申请号：US18552676

申请日：2022-04-04

申请人： Stephanus AXNANDA ,  Zachary E. DANCE ,  David J. LAMBERTO ,  Zhijian LIU ,  Feng Peng ,  Marc POIRIER ,  Matthew A. WINSTON ,  Merck Sharp & Dohme LLC

发明人： Stephanus Axnanda ,  Zachary E. Dance ,  David J. Lamberto ,  Zhijian Liu ,  Feng Peng ,  Marc Poirier ,  Matthew S. Winston

IPC分类号： C07H21/00 ,  A61K31/7084

CPC分类号： C07H21/00 ,  A61K31/7084

摘要： Novel forms of 2-amino-9-[(2R,5R,7R,8S,10R,12aR,14R,15S,15aR,16R)-14-(6-amino-9H-purin-9)-yl)-15,16-difluoro-2,10-dihydroxy-2,10-disulfidooctahydro-12H-5.8-methanofuro[3,2-1][1,3,6,9,11,2,10]pentaoxa-diphosphacyclotetradecin-7-yl]-1,9-dihydro-6H-purin-6-one, which include crystalline salts and hydrates of 2-amino-9)-[(2R,5R,7R,8,S,10R,12aR,14R,15S,15aR,16R)-14-(6-amino-9H-purin-9-yl)-15,16-difluoro-2,10-dihydroxy-2,10-disulfido-octahydro-12H-5,8-methanofuro[3,2-1][1,3,6,9,11,2,10]pentaoxa-diphosphacyclotetradecin-7-yl]-1,9-dihydro-6H-purin-6-one, may be useful as inductors of type I interferon production, specifically as STING active agents.

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.