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公开(公告)号：US11274111B2
公开(公告)日：2022-03-15
申请号：US16973623
申请日：2019-06-14
发明人： Abdelghani Abe Achab , Jared N. Cumming , Christian Fischer , Symon Gathiaka , Charles A. Lesburg , Derun Li , Min Lu , Matthew J. Mitcheltree , Anandan Palani , Rachel L. Palte , David L. Sloman , Hongjun Zhang
摘要： Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula (I) act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.
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公开(公告)号：US10975084B2
公开(公告)日：2021-04-13
申请号：US16341313
申请日：2017-10-06
申请人： Merck Sharp & Dohme Corp. , Umar Faruk Mansoor , Christian Fischer , Phieng Siliphaivanh , Luis Torres , Hakan Gunaydin , David L. Sloman
发明人： Umar Faruk Mansoor , Christian Fischer , Phieng Siliphaivanh , Luis Torres , Hakan Gunaydin , David L. Sloman
IPC分类号： C07D487/04
摘要： The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors.
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3.发明授权Substituted diazine and triazine spleen tyrosine kinease (Syk) inhibitors 有权取代的二嗪和三嗪脾脏酪氨酸激酶（Syk）抑制剂公开(公告)号：US09416111B2
公开(公告)日：2016-08-16
申请号：US14409200
申请日：2013-06-17
发明人： Andrew M. Haidle , Michael D. Altman , Solomon D. Kattar , Matthew Christopher , John Michael Ellis , Christian Fischer , Alan B. Northrup , Kaleen Konrad Childers
IPC分类号： A61K31/506 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D417/14 , C07D239/42 , A61K45/06 , C07D413/14 , C07D409/14 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , C07D239/47 , C07D239/48 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/12 , C07D413/12
CPC分类号： C07D239/42 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61K45/06 , C07D239/47 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The invention provides certain substituted diazine and triazine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
摘要翻译： 本发明提供了式（I）（I）的某些取代的二嗪和三嗪化合物或其药学上可接受的盐，其中R1，R2，R3，R4，Rcy，Cy和t如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）激酶介导的疾病或病症的方法。
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4.发明申请SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINEASE (SYK) INHIBITORS 有权取代的DIAZINE和TRIAZINE SPLEEN TYROSINE KINEASE（SYK）抑制剂公开(公告)号：US20150166486A1
公开(公告)日：2015-06-18
申请号：US14409200
申请日：2013-06-17
发明人： Andrew M. Haidle , Michael D. Altman , Solomon D. Kattar , Matthew Christopher , John Michael Ellis , Christian Fischer , Alan B. Northrup , Kaleen Konrad Childers
IPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D403/04 , C07D403/12 , A61K31/55 , C07D405/12 , A61K31/541 , C07D401/12 , C07D413/12 , A61K31/5377 , A61K31/551 , A61K31/506 , C07D409/12
CPC分类号： C07D239/42 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61K45/06 , C07D239/47 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The invention provides certain substituted diazine and triazine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
摘要翻译： 本发明提供了式（I）（I）的某些取代的二嗪和三嗪化合物或其药学上可接受的盐，其中R1，R2，R3，R4，Rcy，Cy和t如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）激酶介导的疾病或病症的方法。
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公开(公告)号：US20150148327A1
公开(公告)日：2015-05-28
申请号：US14409151
申请日：2013-06-17
发明人： Andrew M. Haidle , Sandra Lee Knowles , Solomon D. Kattar , Denis Deschenes , Jason Burch , Joel Robichaud , Matthew Christopher , Michael D. Altman , James P. Jewell , Alan B. Northrup , Marc Blouin , John Michael Ellis , Hua Zhou , Christian Fischer , Adam J. Schell , Michael H. Reutershan , Brandon M. Taoka , Anthony Donofrio , Joel Robichaud
IPC分类号： C07D401/12 , A61K31/506 , C07D471/04 , C07D498/04 , A61K31/5383 , A61K31/551 , C07D405/14 , C07D401/14 , C07D471/10 , C07D491/107 , C07D491/113 , C07D417/14 , C07D413/14 , C07D487/04 , A61K31/5377
CPC分类号： C07D401/12 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/551 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/08 , C07D491/107 , C07D491/113 , C07D498/04 , A61K2300/00
摘要： The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
摘要翻译： 本发明提供了式（I）的某些取代的吡啶或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，Rcy，Cy和t如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）激酶介导的疾病或病症的方法。
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6.发明申请2-Pyridyl Carboxamide-Containing Spleen Tyrosine Kinase (SYK) Inhibitors 有权含2-吡啶基羧酰胺的脾脏酪氨酸激酶（SYK）抑制剂公开(公告)号：US20140243336A1
公开(公告)日：2014-08-28
申请号：US14349551
申请日：2012-10-01
发明人： Michael D. Altman , Corey E. Bienstock , John W. Butcher , Kaleen Konrad Childers , Maria Emilia Di Francesco , Anthony Donofrio , John Michael Ellis , Christian Fischer , Andrew M. Haidle , James P. Jewell , Sandra Lee Knowles , Alan B. Northrup , Ryan D. Otte , Scott L. Peterson , Graham Frank Smith
IPC分类号： C07D401/14 , A61K31/444 , C07D405/14 , C07D487/04 , A61K31/506 , C07D409/14 , A61K31/5377 , A61K31/519 , A61K31/496 , A61K31/4439 , C07D213/81 , A61K31/5025
CPC分类号： A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/5025 , A61K31/506 , A61K31/519 , A61K31/5377 , C07D213/81 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D495/04
摘要： The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
摘要翻译： 本发明提供了具有式（I）的某些含2-吡啶甲酰胺的化合物或其药学上可接受的盐，其中A和B如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）激酶介导的疾病或病症的方法。
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公开(公告)号：US20200048259A1
公开(公告)日：2020-02-13
申请号：US16341323
申请日：2017-10-06
申请人： Umar Faruk MANSOOR , Christian FISCHER , Phieng SILIPHAIVANH , Hakan GUNAYDIN , Merck Sharp & Dohme Corp.
IPC分类号： C07D487/04
摘要： The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib): (I) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors.
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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：US20150336948A1
公开(公告)日：2015-11-26
申请号：US14404208
申请日：2013-05-24
发明人： Michael D. Altman , Christian Fischer , Jason D. Katz , Theresa M. Williams , Xu-Fang Zhang , Hua Zhou
IPC分类号： C07D471/04 , C07D231/12
CPC分类号： C07D471/04 , C07B59/002 , C07B2200/05 , C07D231/12 , C07D471/08
摘要： The present invention is directed to isotopically labeled biaryl urea compounds which possess high affinity to neurofibrillary tangles (NFTs), and thus are useful to determine the amount and distribution of NFTs in brain. The isotopically labeled biaryl urea compounds may also be useful as PET tracers and in competition assays to identify other compounds that may serve as PET tracers.
摘要翻译： 本发明涉及对神经原纤维缠结（NFT）具有高亲和力的同位素标记的联芳基脲化合物，因此可用于确定脑中NFT的量和分布。 同位素标记的联芳基脲化合物也可用作PET示踪剂，并用于竞争测定以鉴定可用作PET示踪剂的其它化合物。
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公开(公告)号：US20140296203A1
公开(公告)日：2014-10-02
申请号：US14353381
申请日：2012-10-25
发明人： Jongwon Lim , Elizabeth Helen Kelley , Joey L. Methot , Hua Zhou , Alessia Petrocchi , Faruk Mansoor , Christian Fischer , Brendan O'Boyle , David Joseph Guerin , Corey E. Bienstock , Christopher W. Boyce , Matthew H. Daniels , Danielle Falcone , Ronald D. Ferguson , Salem Fevrier , Xianhai Huang , Kathryn Ann Lipford , David L. Sloman , Kevin Wilson , Wei Zhou , David Witter , Milana M. Maletic , Phieng Siliphaivanh
IPC分类号： C07D471/04 , A61K31/444 , A61K31/437 , A61K45/06 , A61K31/501 , A61K31/4709 , A61K31/5377 , A61K31/496 , A61K31/4545 , A61K31/506
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D519/00
摘要： Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
摘要翻译： 公开了式（1）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1）的化合物治疗癌症的方法。
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