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公开(公告)号：US20170360800A1
公开(公告)日：2017-12-21
申请号：US15532548
申请日：2015-12-01
发明人： Christian Fischer , Stephane L. Bogen , Matthew Lloyd Childers , Francesc Xavier Fradera Llinas , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Dann L. Parker, Jr. , Nunzio Sciammetta , Patrick Pengcheng Shao , David L. Sloman , Wanying Sun , Feroze Ujjainwalla
IPC分类号： A61K31/5513 , C07D471/14 , C07D471/04 , A61K45/06 , C07D519/00 , A01N43/00
CPC分类号： A61K31/5513 , A01N43/00 , A61K31/551 , A61K45/06 , A61P35/00 , C07D471/04 , C07D471/14 , C07D519/00 , A61K2300/00
摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is —C(R1)= or —N═; and X is selected from the group consisting of: (II-i), (II-ii), (I) (II-iii), and (II-iv). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
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公开(公告)号：US10086000B2
公开(公告)日：2018-10-02
申请号：US15532548
申请日：2015-12-01
发明人： Christian Fischer , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Dann L. Parker, Jr. , Nunzio Sciammetta , Pengcheng P. Shao , David L. Sloman , Wanying Sun , Feroze Ujjainwalla , Chunhui Huang
IPC分类号： C07D471/04 , A61K31/5513 , A61K45/06 , C07D471/14 , A01N43/00 , C07D519/00
摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is —C(R1)= or —N═; and X is selected from the group consisting of: (II-i), (II-ii), (I) (II-iii), and (II-iv). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
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公开(公告)号：US10508108B2
公开(公告)日：2019-12-17
申请号：US15532552
申请日：2015-12-01
发明人： Christian Fischer , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , J. Michael Ellis , Sara Esposite , Dawn M. Hoffman , Chunhui Huang , Solomon D. Kattar , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Dann L. Parker, Jr. , Michael H. Reutershan , Nunzio Sciammetta , Pengcheng P. Shao , David L. Sloman , Wanying Sun , Feroze Ujjainwalla , Zhicai Wu , Yang Yu , Craig R. Gibeau
IPC分类号： C07D471/04 , C07D471/14 , C07D519/00
摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is —C(R1)═ or —N═; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
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公开(公告)号：US20170369507A1
公开(公告)日：2017-12-28
申请号：US15532549
申请日：2015-12-01
发明人： Fischer Christian , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , Michael J. Ellis , Sara Esposite , Qingmei Hong , Chunhui Huang , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Ryan D. Otte , Dann L. Parker, Jr. , Michael H. Reutershan , Nunzio Sciammetta , Patrick Pengcheng Shao , David L. Sloman , Feroze Ujjainwalla , Catherine White , Zhicai Wu , Yang Yu , Kake Zhao , Craig R. Gibeau
IPC分类号： C07D498/08 , C07D471/04 , C07D498/10 , C07D471/08 , A01N43/00
CPC分类号： C07D498/08 , A01N43/00 , A61K31/551 , C07D471/04 , C07D471/08 , C07D471/14 , C07D498/04 , C07D498/10
摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
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公开(公告)号：US20170362220A1
公开(公告)日：2017-12-21
申请号：US15532552
申请日：2015-12-01
发明人： Christian Fischer , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , Michael J. Ellis , Sara Esposite , Dawn M. Hoffman , Chunhui Huang , Solomon D. Kattar , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Dann L. Parker, Jr. , Michael H. Reutershan , Nunzio Sciammetta , Patrick Pengcheng Shao , David L. Sloman , Wanying Sun , Feroze Ujjainwalla , Zhicai Wu , Yang Yu , Craig R. Gibeau
IPC分类号： C07D471/04 , C07D519/00 , C07D471/14
CPC分类号： C07D471/04 , C07D471/14 , C07D519/00
摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is —C(R1)═ or —N═; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
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公开(公告)号：US09353101B2
公开(公告)日：2016-05-31
申请号：US14398165
申请日：2013-04-26
发明人： John J. Acton, III , Feng Ye , Petr Vachal , Deyou Sha , James F. Dropinski , Lin Chu , Debra Ondeyka , Alexander J. Kim , Vincent J. Colandrea , Yi Zang , Fengqi Zhang , Guizhen Dong
IPC分类号： C07D417/14 , C07D413/14 , A61K31/506 , A61K31/5377 , A61K31/444 , A61K45/06
CPC分类号： C07D417/14 , A61K31/444 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D413/14
摘要： Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis.
摘要翻译： 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于提高人类患者的HDL-胆固醇和降低LDL-胆固醇，并用于治疗或预防动脉粥样硬化。
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公开(公告)号：US20150111866A1
公开(公告)日：2015-04-23
申请号：US14398165
申请日：2013-04-26
发明人： John J. Acton, III , Feng Ye , Petr Vachal , Deyou Sha , James F. Dropinski , Lin Chu , Debra Ondeyka , Alexander J. Kim , Vincent J. Colandrea , Yi Zang , Fengqi Zhang , Guizhen Dong
IPC分类号： C07D417/14 , A61K45/06 , A61K31/5377 , A61K31/444 , C07D413/14 , A61K31/506
CPC分类号： C07D417/14 , A61K31/444 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D413/14
摘要： Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis.
摘要翻译： 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于提高人类患者的HDL-胆固醇和降低LDL-胆固醇，并用于治疗或预防动脉粥样硬化。
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