公开(公告)号：US12012421B2

公开(公告)日：2024-06-18

申请号：US17645876

申请日：2021-12-23

申请人： Hoffmann-La Roche Inc.

发明人： Katja Grosse-Sender ,  Urs Schwitter ,  Frank Stowasser ,  Xuemei Wang ,  Jing Xiong

IPC分类号： C07D513/04 ,  A61P31/20

CPC分类号： C07D513/04 ,  A61P31/20 ,  C07B2200/13

摘要： The present invention relates to novel solid forms of compound (I),




[(1S)-1-[(2S,4R,5R)-5-(5-amino-2-oxo-thiazolo[4,5-d]pyrimidin-3-yl)-4-hydroxy-tetrahydrofuran-2-yl]propyl] acetate and pharmaceutical compositions comprising the solid forms thereof disclosed herein, which may be used as a TLR7 agonist, or for the treatment or prophylaxis of a viral disease in a patient relating to HBV infection or a disease caused by HBV infection.

公开(公告)号：US11873302B2

公开(公告)日：2024-01-16

申请号：US16828408

申请日：2020-03-24

申请人： Hoffmann-La Roche Inc.

发明人： Jing Xiong ,  Xuemei Wang

IPC分类号： A61K31/505 ,  C07D239/28 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention relates to novel solid forms of compound (I),




3-[(8aS)-7-[[(4S)-5-ethoxycarbonyl-4-(3-fluoro-2-methyl-phenyl)-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1H-imidazo[1,5-a]pyrazin-2-yl]-2,2-dimethyl-propanoic acid and pharmaceutical compositions comprising solid forms thereof disclosed herein, which can be used as a HBV capsid inhibitor (or HBV Core Protein Allosteric Modifier), or for the treatment or prophylaxis of a viral disease in a patient relating to HBV infection or a disease caused by HBV infection.

公开(公告)号：US20240116941A1

公开(公告)日：2024-04-11

申请号：US18539773

申请日：2023-12-14

申请人： Hoffmann-La Roche Inc.

发明人： Jing Xiong ,  Xuemei Wang

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： Disclosed are novel solid forms of compound (I),




(3-[(8aS)-7-[[(4S)-5-ethoxycarbonyl-4-(3-fluoro-2-methyl-phenyl)-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1H-imidazo[1,5-a]pyrazin-2-yl]-2,2-dimethyl-propanoic acid), and pharmaceutical compositions comprising solid forms thereof having characteristics described herein, which can be used as a HBV capsid inhibitor (or HBV Core Protein Allosteric Modifier), or for the treatment or prophylaxis of a viral disease in a patient relating to HBV infection or a disease caused by HBV infection.

公开(公告)号：US11230559B2

公开(公告)日：2022-01-25

申请号：US16476172

申请日：2018-01-04

申请人： Hoffmann-La Roche Inc.

发明人： Katja Grosse-Sender ,  Urs Schwitter ,  Frank Stowasser ,  Xuemei Wang ,  Jing Xiong

IPC分类号： C07D513/04 ,  A61P31/20

摘要： The present invention relates to novel solid forms of compound (I) [(1S)-1-[(2S,4R,5R)-5-(5-amino-2-oxo-thiazolo[4,5-d]pyrimidin-3-yl)-4-hydroxy-tetrahydrofuran-2-yl]propyl] acetate and pharmaceutical compositions comprising the solid forms thereof disclosed herein, which may be used as a TLR7 agonist, or for the treatment or prophylaxis of a viral disease in a patient relating to HBV infection or a disease caused by HBV infection.

公开(公告)号：US12012420B2

公开(公告)日：2024-06-18

申请号：US17645875

申请日：2021-12-23

申请人： Hoffmann-La Roche Inc.

发明人： Katja Grosse-Sender ,  Urs Schwitter ,  Frank Stowasser ,  Xuemei Wang ,  Jing Xiong

IPC分类号： C07D513/04 ,  A61P31/20

CPC分类号： C07D513/04 ,  A61P31/20 ,  C07B2200/13

摘要： The present invention relates to novel solid forms of compound (I),




[(1S)-1-[(2S,4R,5R)-5-(5-amino-2-oxo-thiazolo[4,5-d]pyrimidin-3-yl)-4-hydroxy-tetrahydrofuran-2-yl]propyl] acetate and pharmaceutical compositions comprising the solid forms thereof disclosed herein, which may be used as a TLR7 agonist, or for the treatment or prophylaxis of a viral disease in a patient relating to HBV infection or a disease caused by HBV infection.

公开(公告)号：US11142534B2

公开(公告)日：2021-10-12

申请号：US16476165

申请日：2018-01-04

申请人： Hoffmann-La Roche Inc.

发明人： Junli Chen ,  Manuel Konrath ,  Roland Meier ,  Yan Ren ,  Xuemei Wang ,  Jing Xiong ,  Jianhua Yu

IPC分类号： C07D513/04

摘要： The present invention relates to a process for synthesizing a compound of formula (I), R1 is H or C1-6alkyl; R2 is H or hydroxy; or pharmaceutically acceptable salt or diastereomer thereof, which is useful for prophylaxis and treatment of a viral disease in a patient relating to hepatitis B infection or a disease caused by hepatitis B infection.

公开(公告)号：US20200308178A1

公开(公告)日：2020-10-01

申请号：US16828408

申请日：2020-03-24

申请人： Hoffmann-La Roche Inc.

发明人： Jing Xiong ,  Xuemei Wang

IPC分类号： C07D487/04

摘要： The present invention relates to novel solid forms of compound (I), 3-[(8aS)-7-[[(4S)-5-ethoxycarbonyl-4-(3-fluoro-2-methyl-phenyl)-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1H-imidazo[1,5-a]pyrazin-2-yl]-2,2-dimethyl-propanoic acid and pharmaceutical compositions comprising solid forms thereof disclosed herein, which can be used as a HBV capsid inhibitor (or HBV Core Protein Allosteric Modifier), or for the treatment or prophylaxis of a viral disease in a patient relating to HBV infection or a disease caused by HBV infection.