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公开(公告)号：US11773071B2
公开(公告)日：2023-10-03
申请号：US17153409
申请日：2021-01-20
申请人： Albireo AB
IPC分类号： C07D281/02 , C07D281/10 , A61K31/551 , A61P1/16
CPC分类号： C07D281/10 , A61P1/16
摘要： The invention relates to 1,5-benzothiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.
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公开(公告)号：US11014898B1
公开(公告)日：2021-05-25
申请号：US17144595
申请日：2021-01-08
申请人： Albireo AB
IPC分类号： A61K31/554 , A61P1/00 , C07D281/02 , C07D281/10 , A61P1/16
摘要： The invention relates to 1,5-benzothiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.
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公开(公告)号：US10995115B2
公开(公告)日：2021-05-04
申请号：US16545623
申请日：2019-08-20
申请人： ELOBIX AB
IPC分类号： C07D281/02 , C07D281/10 , C07K5/062
摘要： The present invention relates to a process for the preparation of certain 1,5-benzothiazepine compounds, and in particular to a process for the preparation of elobixibat. The process can be carried out under mild and safe conditions and may be used to prepare elobixibat on an industrial scale. The invention also relates to a process for the preparation of a crystalline monohydrate of elobixibat.
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公开(公告)号：US10946027B2
公开(公告)日：2021-03-16
申请号：US16597065
申请日：2019-10-09
IPC分类号： A61K31/554 , A61P25/24 , C07D281/02
摘要： Disclosed herein is an oxalate salt/co-crystal (tianeptine oxalate) of (RS)-7-(3-chloro-6-methyl-6,11-dihydrodibenzo[c,f] [1,2]thiazepin-11-ylamino)heptanoic acid S,S-dioxide (tianeptine) as shown in Formula I:
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公开(公告)号：US10449203B2
公开(公告)日：2019-10-22
申请号：US15856818
申请日：2017-12-28
IPC分类号： C07D281/02 , A61K31/554 , A61P25/24
摘要： Disclosed herein is an oxalate salt/co-crystal (tianeptine oxalate) of (RS)-7-(3-chloro-6-methyl-6,11-dihydrodibenzo[c,f] [1,2]thiazepin-11-ylamino)heptanoic acid S,S-dioxide (tianeptine) as shown in Formula I:
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公开(公告)号：US10428109B1
公开(公告)日：2019-10-01
申请号：US16370753
申请日：2019-03-29
申请人： ELOBIX AB
IPC分类号： C07D281/02 , C07D281/10 , C07K5/062 , A61K31/554 , A61P3/06
摘要： The present invention relates to a process for the preparation of certain 1,5-benzothiazepine compounds, and in particular to a process for the preparation of elobixibat. The process can be carried out under mild and safe conditions and may be used to prepare elobixibat on an industrial scale. The invention also relates to a process for the preparation of a crystalline monohydrate of elobixibat.
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公开(公告)号：US10183919B2
公开(公告)日：2019-01-22
申请号：US15125557
申请日：2015-03-12
申请人： Andrew C. Kruegel , Adam Henke , Madalee M. Gassaway , Marie-Laure Rives , Jonathan A. Javitch , Dalibor Sames
发明人： Andrew C. Kruegel , Adam Henke , Madalee M. Gassaway , Marie-Laure Rives , Jonathan A. Javitch , Dalibor Sames
IPC分类号： C07D281/02 , C07D417/12 , C07D513/04 , A61K31/554 , A61K45/06
摘要： The present invention provides a compound having the structure: or a pharmaceutically acceptable salt or ester thereof.
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公开(公告)号：US20160318917A1
公开(公告)日：2016-11-03
申请号：US15105306
申请日：2014-12-17
发明人： Jeffrey Charles Boehm , Thomas Glanmor Davies , Alison Jo-anne Woolford , Charlotte Mary Griffiths-Jones , Hendrika Maria Gerarda Willems , David Norton , Gordon Saxity , Thomas Daniel Heightman , Tindy Li , Jeffrey K. Kerns , Roderick S. Davis , Hongxing Yan
IPC分类号： C07D417/10 , C07D515/04 , C07D401/12 , C07D513/04 , C07D249/18 , C07D291/08 , C07D471/04 , C07D417/14 , C07D403/12 , C07D419/14 , C07D281/02 , C07D419/10 , C07D405/12
CPC分类号： C07D417/10 , C07D249/18 , C07D281/02 , C07D291/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/14 , C07D419/10 , C07D419/14 , C07D471/04 , C07D513/04 , C07D515/04
摘要： The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.
摘要翻译： 本发明涉及双芳基类似物，含有它们的药物组合物及其作为Nrf2调节剂的用途。
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公开(公告)号：US09029358B2
公开(公告)日：2015-05-12
申请号：US13941082
申请日：2013-07-12
申请人： Shionogi & Co., Ltd.
发明人： Naotake Kobayashi , Kazuo Ueda , Naohiro Itoh , Shinji Suzuki , Gaku Sakaguchi , Akira Kato , Akira Yukimasa , Akihiro Hori , Yuji Koriyama , Hidekazu Haraguchi , Ken Yasui , Yasuhiko Kanda
IPC分类号： C07D405/04 , C07D405/10 , A61K31/553 , C07D281/02 , C07D239/42 , A61K31/426 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/54 , A61K31/541 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/554 , C07D239/14 , C07D239/24 , C07D265/08 , C07D277/18 , C07D279/08 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04
CPC分类号： C07D417/14 , A61K9/0019 , A61K9/1623 , A61K9/2018 , A61K31/426 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/54 , A61K31/541 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/554 , C07D239/14 , C07D239/24 , C07D239/42 , C07D265/08 , C07D277/18 , C07D279/06 , C07D279/08 , C07D279/12 , C07D281/02 , C07D405/04 , C07D405/10 , C07D417/04 , C07D417/10 , C07D417/12 , C07D471/04
摘要： A composition having BACE 1 inhibitory activity containing a compound represented by the formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a, and R4b, is each independently a hydrogen atom, halogen, or hydroxyl etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt or a solvate thereof.
摘要翻译： 一种具有BACE 1抑制活性的组合物，其含有式（I）表示的化合物：其中环A为任选取代的碳环基或任选取代的杂环基; E为低级亚烷基; X是S，O或NR1; R1是氢原子或低级烷基; R2a，R2b，R3a，R3b，R4a和R4b各自独立地为氢原子，卤素或羟基等; n和m各自独立地为0〜3的整数， n + m为0〜3的整数， R5是氢原子或取代的低级烷基; 其药学上可接受的盐或其溶剂化物。
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公开(公告)号：US08394790B2
公开(公告)日：2013-03-12
申请号：US12447381
申请日：2007-10-25
申请人： Moshe Portnoy , Irit Gil-Ad , Avraham Weizman
发明人： Moshe Portnoy , Irit Gil-Ad , Avraham Weizman
IPC分类号： A61P25/18 , A61K31/554 , A61K31/55 , C07D495/00 , C07D281/02
CPC分类号： C07D495/04 , A61K31/551 , A61K47/542 , A61K47/55 , C07D403/04
摘要： The invention provides novel compounds and pharmaceutical compositions for the treatment of psychological and/or psychiatric diseases or disorders.
摘要翻译： 本发明提供用于治疗心理和/或精神疾病或病症的新型化合物和药物组合物。
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