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公开(公告)号：US20210238192A1
公开(公告)日：2021-08-05
申请号：US17259673
申请日：2019-06-27
IPC分类号： C07D495/04 , A61P19/04 , C07C233/88 , C07D235/06 , C07D235/18 , C07C271/28 , C07C233/25 , C07D317/64 , C07C311/18 , C07D277/24 , C07D233/64 , C07D239/26 , C07C217/46 , C07D271/06 , C07C211/35 , C07C211/27 , C07C237/30 , C07D263/32 , C07D231/12 , C07D257/04 , C07D333/16 , C07C233/36 , C07D209/08 , C07D249/06 , C07D233/22 , C07D249/08 , C07C275/40 , C07C275/28 , C07D401/04
摘要： Disclosed herein are small molecule Vascular Adhesion Protein-1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof.
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公开(公告)号：US20210113560A1
公开(公告)日：2021-04-22
申请号：US17041611
申请日：2019-03-25
IPC分类号： A61K31/506 , A61K31/4725 , A61K31/433 , A61K31/4155 , A61K31/4439 , A61K31/166 , A61K31/4015 , A61K31/421 , A61K31/415 , A61K31/27 , A61K31/42 , A61K31/4045 , A61K31/497 , A61K31/423
摘要： Disclosed herein are methods of treating fibrotic disorders by administering compounds selective for CAPN1, CAPN2, and/or CAPN9 such that side effects, off pathway interactions, and/or toxicities are minimized Such methods may, for example, minimize unintended effects of therapeutic compounds by providing dosing and dosage forms that minimize the level of unbound drug within the relevant tissues of a patient undergoing treatment.
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公开(公告)号：US11339130B1
公开(公告)日：2022-05-24
申请号：US17032529
申请日：2020-09-25
发明人： Brad Owen Buckman , John Beamond Nicholas , Shendong Yuan , Marc Adler , Kumaraswamy Emayan , Jingyuan Ma
IPC分类号： C07D233/90 , C07D417/14 , C07C233/05 , C07D209/20 , C07D231/14 , C07D249/06 , C07D263/34 , C07D271/04 , C07D275/03 , C07D285/06 , C07D307/68 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D417/04 , A61P11/00
摘要： Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
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公开(公告)号：US11292801B2
公开(公告)日：2022-04-05
申请号：US16312916
申请日：2017-06-29
发明人： Brad Owen Buckman , Shendong Yuan , John Beamond Nicholas , Jingyuan Ma , Kumaraswamy Emayan , Marc Adler
IPC分类号： C07D498/18 , A61P1/16 , A61P13/12 , A61P11/00 , C07D245/06 , C07D267/00 , C07D405/12 , C07D407/12 , C07D413/12 , C07D471/18 , C07D498/04
摘要： Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to macrocyclic α-keto amide derivatives and their use as therapeutic agents.
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5.发明授权公开(公告)号：US10590084B2
公开(公告)日：2020-03-17
申请号：US16083189
申请日：2017-03-08
IPC分类号： C07D223/12 , C07D225/02 , C07D211/58 , C07K5/062 , A61P19/04 , A61K38/00
摘要： The present technology relates to cyclic keto-amide compounds of general formulae I to XXXII, compositions and kits thereof as calpain modulators and methods useful for the treatment of various diseases or disorders such as fibrotic disease or cancer which are associated or mediated, by calpains, such as CAPN1, CAPN2, and/or CAPN9. The present technology is also applicable to cyclic keto-amide compounds which inhibit myofibroblast differentiation.
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6.发明申请公开(公告)号：US20190194139A1
公开(公告)日：2019-06-27
申请号：US16083189
申请日：2017-03-08
IPC分类号： C07D223/12 , C07D225/02 , C07D211/58 , A61P19/04
CPC分类号： C07D223/12 , A61K38/00 , A61P19/04 , C07D211/58 , C07D225/02 , C07K5/06034
摘要： The present technology relates to cyclic keto-amide compounds of general formulae I to XXXII, compositions and kits thereof as calpain modulators and methods useful for the treatment of various diseases or disorders such as fibrotic disease or cancer which are associated or mediated, by calpains, such as CAPN1, CAPN2, and/or CAPN9. The present technology is also applicable to cyclic keto-amide compounds which inhibit myofibroblast differentiation.
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公开(公告)号：US20220347173A1
公开(公告)日：2022-11-03
申请号：US17255168
申请日：2019-06-27
发明人： Sharlene Lim , Prabha Ibrahim , Maria Fuentes
IPC分类号： A61K31/498 , A61K31/421 , A61K31/433 , A61K31/4439 , A61K31/166 , A61K31/415 , A61P1/16 , A61K45/06
摘要： Disclosed herein are methods of treating liver fibrosis by administering calpain inhibitors to subjects in need thereof.
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公开(公告)号：US20220324814A1
公开(公告)日：2022-10-13
申请号：US17718728
申请日：2022-04-12
发明人： Brad Owen Buckman , John Beamond Nicholas , Shendong Yuan , Marc Adler , Kumaraswamy Emayan , Jingyuan Ma
IPC分类号： C07D233/90 , A61P11/00 , C07C233/05 , C07D209/20 , C07D231/14 , C07D249/06 , C07D263/34 , C07D271/04 , C07D275/03 , C07D285/06 , C07D307/68 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D417/04 , C07D417/14
摘要： Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
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公开(公告)号：US20220257570A1
公开(公告)日：2022-08-18
申请号：US17629988
申请日：2020-07-28
IPC分类号： A61K31/433 , A61P25/28 , A61K9/20 , A61K9/48 , A61K9/10 , A61K9/00 , A61K31/166 , A61K31/415 , A61K31/343 , A61K31/138 , A61K31/135 , A61K31/554 , A61K31/4545 , A61K31/451 , A61K31/5415 , A61K31/19 , A61K31/55 , A61K31/53
摘要： Methods of treating neurological diseases and disorders associated with protein aggregation using calpain inhibitors are provided. Said neurological diseases associated with protein aggregation include polyglutamine expansion diseases such as Huntington's disease, Machado-Joseph disease, and spinocerebellar ataxias.
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公开(公告)号：US20210347727A1
公开(公告)日：2021-11-11
申请号：US16624849
申请日：2018-06-19
发明人： Brad Owen Buckman , Shendong Yuan , John Beamond Nicholas , Jingyuan Ma , Kumaraswamy Emayan , Marc Adler
IPC分类号： C07C233/78 , A61P19/04 , C07D311/84 , C07D265/38 , C07D319/24 , C07D209/90 , C07D307/91 , C07C233/62 , C07D317/68 , C07C233/76
摘要： Small molecule calpain modulator compositions and pharmaceutical compositions can be prepared and used as therapeutic agents. Exemplary compositions include non-macrocyclic a-keto amide derivatives. The therarapeutic agents can be used for treating fibrotic disease or a resulting secondary disease state or condition. The small molecules can competitively bind with calpastatin and/or inhibit calpain through contact with CAPN1, CAPN2, and/or CAPN9 enzymes.
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