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公开(公告)号：US11447465B2
公开(公告)日：2022-09-20
申请号：US16555946
申请日：2019-08-29
发明人： Jason Allan Wiles , Avinash S. Phadke , Milind Deshpande , Atul Agarwal , Dawei Chen , Venkat Rao Gadhachanda , Akihiro Hashimoto , Godwin Pais , Qiuping Wang , Xiangzhu Wang , Joel Charles Barrish , William Greenlee , Kyle J. Eastman
IPC分类号： C07D401/14 , C07D403/06 , C07D403/10 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D493/04 , C07D495/04 , C07D513/04 , C07F9/6558
摘要： Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, and Formula IV or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.
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2.发明授权公开(公告)号：US11407738B2
公开(公告)日：2022-08-09
申请号：US16867475
申请日：2020-05-05
发明人： Jason Allan Wiles , Avinash S. Phadke , Milind Deshpande , Atul Agarwal , Dawei Chen , Venkat Rao Gadhachanda , Akihiro Hashimoto , Godwin Pais , Qiuping Wang , Xiangzhu Wang , William Greenlee
IPC分类号： C07D403/14 , C07D403/04 , C07D401/14 , C07D471/04 , C07D413/14 , C07F9/6558 , C07D417/14 , C07D487/04 , C07D519/00 , C07D403/12 , C07D407/14 , C07D409/14 , C07D403/10 , C07D513/04 , C07D487/22 , A61P37/00 , A61P1/16 , A61P29/00 , C07D405/14 , C07D493/04
摘要： Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I′″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.
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公开(公告)号：US10428095B2
公开(公告)日：2019-10-01
申请号：US16148622
申请日：2018-10-01
发明人： Jason Allan Wiles , Avinash S. Phadke , Xiangzhu Wang , Dawei Chen , Akihiro Hashimoto , Venkat Rao Gadhachanda , Godwin Pais , Qiuping Wang , Atul Agarwal , Milind Deshpande
IPC分类号： C07D403/14 , C07F9/572 , C07D209/42 , C07D403/12 , C07D401/14 , C07D471/04 , C07D417/06 , C07D403/06 , C07D417/14 , C07F7/08 , C07D413/14 , C07D487/04 , C07D405/14 , C07D403/08 , C07D413/06 , C07F5/02 , C07F9/6561 , C07F9/6558 , A61K31/404 , A61K31/407 , A61K31/4162 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/549 , A61K31/55 , A61K31/675 , A61K31/683 , C07B59/00 , C07D209/14 , C07D209/40 , C07D405/12 , C07D417/12 , C07D487/14 , C07D491/113 , C07D495/04 , C07D513/04 , A61K9/00 , A61K31/4045 , A61K31/444 , A61K31/501 , A61K31/519 , C07D209/12 , C07D209/30 , C07D209/44 , C07D209/88 , C07D471/08
摘要： Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
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4.发明申请公开(公告)号：US20190185498A1
公开(公告)日：2019-06-20
申请号：US16276139
申请日：2019-02-14
发明人： Jason Allan Wiles , Venkat Rao Gadhachanda , Qiuping Wang , Godwin Pais , Akihiro Hashimoto , Dawei Chen , Xiangzhu Wang , Atul Agarwal , Milind Deshpande , Avinash S. Phadke
IPC分类号： A61K31/683 , C07F9/572 , C07D417/06 , C07F7/08 , C07D401/14 , C07D403/14 , C07D403/12 , C07D209/42 , C07D471/08 , C07D209/30 , C07D209/44 , C07D209/88 , C07D209/12 , A61K31/519 , A61K31/501 , A61K9/00 , A61K31/4045 , A61K31/444 , A61K31/675 , A61K31/404 , A61K31/407 , A61K31/4162 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/549 , A61K31/55 , C07F9/6558 , C07F9/6561 , C07D513/04 , C07B59/00 , C07D471/04 , C07D209/14 , C07D209/40 , C07D405/12 , C07D417/12 , C07D487/14 , C07D491/113 , C07D495/04 , C07D413/06 , C07D403/08 , C07D405/14 , C07D487/04 , C07D413/14 , C07D417/14 , C07D403/06 , C07F5/02
摘要： Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
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公开(公告)号：US10287301B2
公开(公告)日：2019-05-14
申请号：US16010081
申请日：2018-06-15
发明人： Jason Allan Wiles , Avinash S. Phadke , Milind Deshpande , Atul Agarwal , Dawei Chen , Venkat Rao Gadhachanda , Akihiro Hashimoto , Godwin Pais , Qiuping Wang , Xiangzhu Wang
IPC分类号： C07D513/04 , C07D403/14 , C07D403/06 , C07D401/14 , C07D471/04 , C07D417/14 , C07D487/04 , C07D405/14 , C07D409/14 , C07D495/04 , C07D493/04 , C07D413/14
摘要： Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.
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公开(公告)号：US10138225B2
公开(公告)日：2018-11-27
申请号：US15247440
申请日：2016-08-25
发明人： Jason Allan Wiles , Avinash S. Phadke , Milind Deshpande , Atul Agarwal , Dawei Chen , Venkat Rao Gadhachanda , Akihiro Hashimoto , Godwin Pais , Qiuping Wang , Xiangzhu Wang
IPC分类号： A61K31/416 , A61K31/404 , C07D403/14 , C07D403/06 , C07D401/14 , C07D413/14 , C07D471/08 , C07D513/04 , C07D495/04
摘要： Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an amide substituent (R32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein are capable of reducing the excessive activation of complement.
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公开(公告)号：US20180291047A1
公开(公告)日：2018-10-11
申请号：US16006533
申请日：2018-06-12
发明人： Jason Allan Wiles , Godwin Pais , Akihiro Hashimoto , Venkat Rao Gadhachanda , Qiuping Wang , Dawei Chen , Xiangzhu Wang , Atul Agarwal , Milind Deshpande , Avinash S. Phadke
IPC分类号： C07F9/572 , C07D417/06 , C07F7/08 , C07D401/14 , C07D403/14 , C07D403/12 , C07D209/42 , C07D471/08 , C07D209/30 , C07D209/44 , C07D209/88 , C07D209/12 , A61K31/519 , A61K31/501 , A61K9/00 , A61K31/4045 , A61K31/444 , A61K31/675 , A61K31/404 , A61K31/407 , A61K31/4162 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/549 , A61K31/55 , A61K31/683 , C07F9/6558 , C07F9/6561 , C07D513/04 , C07B59/00 , C07D209/14 , C07D209/40 , C07D405/12 , C07D417/12 , C07D487/14 , C07D491/113 , C07D495/04 , C07D413/06 , C07D403/08 , C07D405/14 , C07D487/04 , C07D413/14 , C07D417/14 , C07D403/06 , C07F5/02 , C07D471/04
摘要： Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R12 or R13 on the A group is an alkyne (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
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8.发明申请公开(公告)号：US20180179186A1
公开(公告)日：2018-06-28
申请号：US15905524
申请日：2018-02-26
发明人： Jason Allan Wiles , Avinash S. Phadke , Milind Deshpande , Atul Agarwal , Dawei Chen , Venkat Rao Gadhachanda , Akihiro Hashimoto , Godwin Pais , Qiuping Wang , Xiangzhu Wang , William Greenlee
IPC分类号： C07D403/04 , A61P37/00 , A61P29/00 , A61P1/16 , C07D493/04 , C07D403/14 , C07D401/14 , C07D487/04 , C07D417/14 , C07D405/14 , C07F9/6558 , C07D471/04 , C07D413/14 , C07D519/00
摘要： Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I′″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.
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公开(公告)号：US20180177761A1
公开(公告)日：2018-06-28
申请号：US15905427
申请日：2018-02-26
发明人： Jason Allan Wiles , Avinash S. Phadke , Milind Deshpande , Atul Agarwal , Dawei Chen , Venkat Rao Gadhachanda , Akihiro Hashimoto , Godwin Pais , Qiuping Wang , Xiangzhu Wang
IPC分类号： A61K31/404 , A61K31/506 , A61K31/444 , A61K31/501 , A61K31/55 , A61K31/519 , A61K31/5383 , A61K31/4439 , A61K9/00
摘要： Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an amino substituent (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.
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公开(公告)号：US10000516B2
公开(公告)日：2018-06-19
申请号：US15247424
申请日：2016-08-25
发明人： Jason Allan Wiles , Avinash S. Phadke , Milind Deshpande , Atul Agarwal , Dawei Chen , Venkat Rao Gadhachanda , Akihiro Hashimoto , Godwin Pais , Qiuping Wang , Xiangzhu Wang
IPC分类号： C07F9/6561 , C07F9/6558
CPC分类号： C07F9/6561 , C07F9/65583
摘要： Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is a phosphonate substituent (R32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.
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