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公开(公告)号：US20190255055A1
公开(公告)日：2019-08-22
申请号：US16311533
申请日：2017-06-20
申请人： The Regents of the University of Michigan , Indiana University Research and Technology Corporation
IPC分类号： A61K31/519 , A61P31/00 , A61P35/00 , A61K45/06 , C07D487/04
摘要： This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a thiopyrimidinone structure which function as inhibitors of ALDH protein, and their use as therapeutics for the treatment of cancer and other diseases.
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公开(公告)号：US11944626B2
公开(公告)日：2024-04-02
申请号：US16311533
申请日：2017-06-20
申请人： The Regents of the University of Michigan , Indiana University Research and Technology Corporation
IPC分类号： A61K31/519 , A61K31/337 , A61K31/4745 , A61K31/522 , A61K31/555 , A61K31/7068 , A61K39/395 , A61K45/06 , A61P31/00 , A61P35/00 , C07D487/04
CPC分类号： A61K31/519 , A61K31/337 , A61K31/4745 , A61K31/522 , A61K31/555 , A61K31/7068 , A61K39/395 , A61K45/06 , A61P31/00 , A61P35/00 , C07D487/04 , A61K31/522 , A61K2300/00 , A61K31/555 , A61K2300/00 , A61K31/337 , A61K2300/00 , A61K31/4745 , A61K2300/00 , A61K31/7068 , A61K2300/00
摘要： This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a thiopyrimidinone structure which function as inhibitors of ALDH protein, and their use as therapeutics for the treatment of cancer and other diseases.
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公开(公告)号：US20210122712A1
公开(公告)日：2021-04-29
申请号：US17076852
申请日：2020-10-22
发明人： Scott D. Larsen , James A. Shayman , Kim Hutchings , Neil Moss , Qin Jiang , Nicholas Mayhew , Emily Freeman , Zohreh Saijadi Hashemi
IPC分类号： C07D205/04 , C07D207/09 , C07D405/12
摘要： Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.
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公开(公告)号：US10329283B2
公开(公告)日：2019-06-25
申请号：US15738606
申请日：2016-06-27
发明人： Scott D. Larsen , John J. G. Tesmer , Helen Waldschmidt , Kristoff Homan , Michael William Wilson
IPC分类号： C07D405/14 , C07D401/14 , C07D401/12 , C07D405/12 , A61P9/00 , A61P9/12
摘要： Disclosed herein are novel GRK inhibitors and methods for their use in treating or preventing heart disease, such as cardiac failure, cardiac hypertrophy, and hypertension. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof, wherein the substituents are as described.
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公开(公告)号：US20150297577A1
公开(公告)日：2015-10-22
申请号：US14647770
申请日：2013-11-26
发明人： Ronald Buckanovich , Scott D. Larsen , Kun Yang
IPC分类号： A61K31/4439 , A61K45/06 , A61K31/437 , A61K31/136 , A61K31/4035
CPC分类号： A61K31/4439 , A61K31/136 , A61K31/337 , A61K31/4035 , A61K31/404 , A61K31/437 , A61K31/555 , A61K33/24 , A61K45/06 , C07D209/04 , C07D401/04 , C07D471/04 , G01N33/574 , A61K2300/00
摘要： The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against cancer stem cells.
摘要翻译： 本发明涉及化学化合物，其发现方法及其治疗和研究用途。 特别地，本发明提供了作为抗癌干细胞的治疗剂的化合物。
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6.发明公开公开(公告)号：US20230212123A1
公开(公告)日：2023-07-06
申请号：US17920794
申请日：2021-04-20
IPC分类号： C07D213/64 , C07D213/65 , C07D213/40 , C07D213/68 , C07D401/06 , C07D213/61 , A61K45/06
CPC分类号： C07D213/64 , A61K45/06 , C07D213/40 , C07D213/61 , C07D213/65 , C07D213/68 , C07D401/06
摘要： Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.
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公开(公告)号：US20180186779A1
公开(公告)日：2018-07-05
申请号：US15738606
申请日：2016-06-27
发明人： Scott D. Larsen , John J.G. Tesmer , Helen Waldschmidt , Kristoff Homan , Michael William Wilson
IPC分类号： C07D405/14 , C07D405/12 , C07D401/12 , C07D401/14 , A61P9/00 , A61P9/12
CPC分类号： C07D405/14 , A61P9/00 , A61P9/12 , C07D401/12 , C07D401/14 , C07D405/12
摘要： Disclosed herein are novel GRK inhibitors and methods for their use in treating or preventing heart disease, such as cardiac failure, cardiac hypertrophy, and hypertension. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof, wherein the substituents are as described.
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公开(公告)号：US09468632B2
公开(公告)日：2016-10-18
申请号：US14647770
申请日：2013-11-26
发明人： Ronald Buckanovich , Scott D. Larsen , Kun Yang
IPC分类号： A61K31/404 , A61K31/4439 , A61K45/06 , A61K31/337 , A61K31/555 , A61K33/24 , C07D401/04 , C07D471/04 , C07D209/04 , G01N33/574 , A61K31/136 , A61K31/4035 , A61K31/437
CPC分类号： A61K31/4439 , A61K31/136 , A61K31/337 , A61K31/4035 , A61K31/404 , A61K31/437 , A61K31/555 , A61K33/24 , A61K45/06 , C07D209/04 , C07D401/04 , C07D471/04 , G01N33/574 , A61K2300/00
摘要： The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against cancer stem cells.
摘要翻译： 本发明涉及化学化合物，其发现方法及其治疗和研究用途。 特别地，本发明提供了作为抗癌干细胞的治疗剂的化合物。
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公开(公告)号：US20150132352A1
公开(公告)日：2015-05-14
申请号：US14397798
申请日：2013-05-02
发明人： Hongmin Sun , Bryan Yestrepsky , David Ginsburg , Scott D. Larsen
IPC分类号： A61K31/517 , A01N43/54 , C07D471/10 , C07D491/107 , C07D487/10 , A61L31/16 , A61K31/505 , A61K31/5377 , A01N43/84 , A61K45/06 , A61L31/08 , C07D239/70 , C07D239/56
CPC分类号： A61K31/517 , A01N43/54 , A01N43/84 , A01N43/90 , A61K31/505 , A61K31/5377 , A61K45/06 , A61L31/08 , A61L31/16 , A61L2300/404 , C07D239/56 , C07D239/70 , C07D471/10 , C07D487/10 , C07D491/107
摘要： The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).
摘要翻译： 本发明涉及化学化合物，其发现方法及其治疗和研究用途。 特别地，本发明提供了作为抗细菌感染（例如生物膜）的治疗剂的化合物。
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公开(公告)号：US10023564B2
公开(公告)日：2018-07-17
申请号：US15501888
申请日：2015-08-10
IPC分类号： C07D413/14 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14
摘要： Disclosed herein are novel GRK2 inhibitors and methods for their use in treating or preventing heart disease, such as cardiac failure, cardiac hypertrophy, and hypertension. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof: wherein the substituents are as described.
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