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公开(公告)号：EP3259264A1
公开(公告)日：2017-12-27
申请号：EP16711043.6
申请日：2016-02-15
发明人： DING, Pingyu , GELMAN, Marina , KINSELLA, Todd , SINGH, Rajinder , BHAMIDIPATI, Somasekhar , VELAPARTHI, Upender , BORZILLERI, Robert, M. , RAHAMAN, Hasibur , WARRIER, Jayakumar, Sankara
IPC分类号： C07D401/14 , C07D471/04 , C07D487/04 , A61K31/44 , A61P21/00
CPC分类号： C07D401/14 , C07B59/002 , C07B2200/05 , C07C53/06 , C07C53/18 , C07D471/04 , C07D487/04
摘要： and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R1, Z and n are as described herein. In certain embodiments, a compound disclosed herein inhibits GDF8, and can be used to treat disease by blocking GDF8 signaling.
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公开(公告)号：EP4021901A1
公开(公告)日：2022-07-06
申请号：EP20768221.2
申请日：2020-08-27
发明人： VELAPARTHI, Upender , OLSON, Richard E. , DARNE, Chetan Padmakar , DASGUPTA, Bireshwar , WARRIER, Jayakumar Sankara , RAHAMAN, Hasibur , JALAGAM, Prasada Rao , ROY, Saumya , GRUNENFELDER, Denise C.
IPC分类号： C07D401/04 , A61P31/12 , A61P35/00 , A61K31/519
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公开(公告)号：EP3265454B1
公开(公告)日：2020-02-26
申请号：EP16710547.7
申请日：2016-02-26
发明人： KINSELLA, Todd , GELMAN, Marina , HONG, Hui , DARWISH, Ihab, S. , SINGH, Rajinder , YU, Jiaxin , BORZILLERI, Robert, M. , VELAPARTHI, Upender , LIU, Peiying , DARNE, Chetan , RAHAMAN, Hasibur , WARRIER, Jayakumar, Sankara
IPC分类号： C07D401/04 , C07D403/04 , C07D417/04 , C07D471/04 , C07D487/04 , A61K31/4164 , A61K31/426 , A61P35/00
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公开(公告)号：EP4305038A1
公开(公告)日：2024-01-17
申请号：EP22714667.7
申请日：2022-03-14
发明人： FINK, Brian Edward , CHERNEY, Robert Joseph , NGU, Khehyong , VELAPARTHI, Upender , VACCARO, Wayne David , RUAN, Zheming , QIN, Lan-Ying , SHIRUDE, Pravin S. , RAHAMAN, Hasibur
IPC分类号： C07D487/08 , A61K31/4995 , A61P35/00
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公开(公告)号：EP4081516A1
公开(公告)日：2022-11-02
申请号：EP20845304.3
申请日：2020-12-22
IPC分类号： C07D403/04 , A61K31/517 , A61P35/00
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公开(公告)号：EP4305037A1
公开(公告)日：2024-01-17
申请号：EP22714316.1
申请日：2022-03-14
发明人： FINK, Brian Edward , CHERNEY, Robert Joseph , NGU, Khehyong , VELAPARTHI, Upender , VACCARO, Wayne David , RUAN, Zheming , QIN, Lan-Ying , SHIRUDE, Pravin S. , RAHAMAN, Hasibur
IPC分类号： C07D487/08 , A61K31/551 , A61P35/00
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公开(公告)号：EP3814348A1
公开(公告)日：2021-05-05
申请号：EP19744923.4
申请日：2019-06-26
发明人： VELAPARTHI, Upender , CHUPAK, Louis S. , DARNE, Chetan Padmakar , DING, Min , GENTLES, Robert G. , HUANG, Yazhong , KAMBLE, Manjunatha Narayana Rao , MARTIN, Scott W. , MANNOORI, Raju , MCDONALD, Ivar M. , OLSON, Richard E. , RAHAMAN, Hasibur , JALAGAM, Prasada Rao , ROY, Saumya , TONUKUNURU, Gopikishan , VELAIAH, Sivasudar , WARRIER, Jayakumar Sankara , ZHENG, Xiaofan , TOKARSKI, John S. , DASGUPTA, Bireshwar , REDDY, Kotha Rathnakar , RAJA, Thiruvenkadam
IPC分类号： C07D471/04 , A61P35/00 , A61K31/496
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公开(公告)号：EP3341372A1
公开(公告)日：2018-07-04
申请号：EP16759926.5
申请日：2016-08-23
发明人： BORZILLERI, Robert M. , FINK, Brian E. , HARIKRISHNAN, Lalgudi S. , VELAPARTHI, Upender , BALIGAR, Vishweshwaraiah , RAHAMAN, Hasibur , WARRIER, Jayakumar Sankara
IPC分类号： C07D473/34 , A61K31/52 , A61P35/00
CPC分类号： A61K31/52 , A61K2121/00 , A61P35/02 , C07D473/34
摘要： The invention relates generally to compounds of formula (I) that modulate the activity of TGFβR-1 and TGFβR-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
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公开(公告)号：EP3325484A1
公开(公告)日：2018-05-30
申请号：EP16747941.9
申请日：2016-07-21
发明人： HARIKRISHNAN, Lalgudi S. , FINK, Brian E. , BORZILLERI, Robert M. , TONUKUNURU, Gopikishan , RAHAMAN, Hasibur , WARRIER, Jayakumar Sankara , SESHADRI, Balaji
IPC分类号： C07D487/04 , A61P35/00 , A61K31/53
CPC分类号： C07D487/04 , A61K31/53 , A61K31/541
摘要： The invention relates generally to compounds that modulate the activity of TGFβR-1 and TGFβ R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
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公开(公告)号：EP3265454A1
公开(公告)日：2018-01-10
申请号：EP16710547.7
申请日：2016-02-26
发明人： KINSELLA, Todd , GELMAN, Marina , HONG, Hui , DARWISH, Ihab, S. , SINGH, Rajinder , YU, Jiaxin , BORZILLERI, Robert, M. , VELAPARTHI, Upender , LIU, Peiying , DARNE, Chetan , RAHAMAN, Hasibur , WARRIER, Jayakumar, Sankara
IPC分类号： C07D401/04 , C07D403/04 , C07D417/04 , C07D471/04 , C07D487/04 , A61K31/4164 , A61K31/426 , A61P35/00
摘要： Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.
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