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公开(公告)号：US09353066B2
公开(公告)日：2016-05-31
申请号：US14422419
申请日：2013-08-15
发明人： Andrew M. Haidle , Jason Burch , Daniel Guay , Jacques Yves Gauthier , Joel Robichaud , Jean Francois Fournier , John Michael Ellis , Matthew Christopher , Solomon D. Kattar , Graham F. Smith , Alan B. Northrup
IPC分类号： C07D239/42 , C07D403/12 , A61K31/506 , A61K31/505 , C07D401/12 , C07D239/47
CPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , A61K45/06 , C07D239/47 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/10
摘要： The invention provides certain substituted phenyl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, 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).
摘要翻译： 本发明提供某些取代的式（I）的苯基化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，Rcy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）介导的疾病或病症的方法。
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公开(公告)号：US20220259188A1
公开(公告)日：2022-08-18
申请号：US17614732
申请日：2020-06-01
申请人： Hua ZHOU , John J. ACTON, III , Michael J. ARDOLINO , Yi-Heng CHEN , Peter H. FULLER , Anmol GULATI , Rebecca Elizabeth JOHNSON , William P. KAPLAN , Solomon D. KATTAR , Mitchell H. KEYLOR , Derun LI , Kaitlyn Marie LOGAN , Min LU , Gregori J. MORRIELLO , Santhosh F. NEELAMKAVIL , Barbara PIO , Nunzio SCIAMMETTA , Vladimir SIMOV , Jing SU , Luis TORRES , Xin YAN , Merck Sharp & Dohme Corp.
发明人： Hua Zhou , John J. Acton, III , Michael J. Ardolino , Yi-Heng Chen , Peter H. Fuller , Anmol Gulati , Rebecca Elizabeth Johnson , William P. Kaplan , Solomon D. Kattar , Mitchell H. Keylor , Derun Li , Kaitlyn Marie Logan , Min Lu , Gregori J. Morriello , Santhosh F. Neelamkavil , Barbara Pio , Nunzio Sciammetta , Vladimir Simov , Jing Su , Luis Torres , Xin Yan
IPC分类号： C07D405/14 , C07D487/08 , C07D409/14 , C07D403/04 , C07D403/14 , C07D498/04 , C07D498/08 , C07D487/10 , C07D401/14 , C07D471/10 , C07D491/107 , C07D471/04 , C07D487/04 , A61P25/16
摘要： The present invention is directed to substituted certain 1-pyrazolyl, 5-, 6-disubstituted indazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, and ring A are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of diseases, such as Parkinson's disease, in which LRRK-2 kinase is involved.
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公开(公告)号：US09969749B2
公开(公告)日：2018-05-15
申请号：US15515383
申请日：2015-09-25
发明人： Michael D. Altman , Brian M. Andresen , Jason D. Brubaker , Matthew L. Childers , Anthony Donofrio , Thierry Fischmann , Craig R. Gibeau , Solomon D. Kattar , Charles A. Lesburg , Jongwon Lim , John K. F. MacLean , Umar F. Mansoor , Alan B. Northrup , John M. Sanders , Luis Torres
IPC分类号： C07D498/04 , A61K45/06 , A61K31/517 , C07D403/04 , C07D239/94 , C07D401/04 , A61K31/5377 , C07D405/14 , C07D401/14 , C07D413/04 , C07D405/04 , C07D471/04 , A61K31/5383 , C07D491/048 , C07D417/04 , C07D409/04
CPC分类号： C07D498/04 , A61K31/517 , A61K31/5377 , A61K31/5383 , A61K45/06 , A61P37/00 , C07D239/94 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D491/048 , A61K2300/00
摘要： The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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4.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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公开(公告)号：US20150232428A1
公开(公告)日：2015-08-20
申请号：US14422419
申请日：2013-08-15
发明人： Andrew M. Haidle , Jason Burch , Daniel Guay , Jacques Yves Gauthier , Joel Robichaud , Jean Francois Fournier , John Michael Ellis , Matthew Christopher , Solomon D. Kattar , Graham F. Smith , Alan B. Northrup
IPC分类号： C07D239/42 , C07D239/47 , A61K31/506 , C07D403/12 , A61K31/505 , C07D401/12
CPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , A61K45/06 , C07D239/47 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/10
摘要： The invention provides certain substituted phenyl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, 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).
摘要翻译： 本发明提供某些取代的式（I）的苯基化合物或其药学上可接受的盐，其中R1，R2，R3，R4，Rcy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）介导的疾病或病症的方法。
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6.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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公开(公告)号：US20130131041A1
公开(公告)日：2013-05-23
申请号：US13719999
申请日：2012-12-19
发明人： Scott C. Berk , Joshua Close , Christopher Hamblett , Richard W. Heidebrecht , Solomon D. Kattar , Laura T. Kliman , Dawn M. Mampreian Hoffman , Joey L. Methot , Thomas Miller , David L. Soloman , Matthew G. Stanton , Paul Tempest , Anna Z. Zabierek
IPC分类号： C07D471/10 , C07D498/10 , C07D491/107 , C07D487/10
CPC分类号： C07D471/10 , C07D487/10 , C07D491/10 , C07D491/107 , C07D498/10
摘要： The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.
摘要翻译： 本发明涉及一类新的取代的螺环化合物。 这些化合物可以抑制组蛋白脱乙酰酶，适用于选择性诱导终末分化，阻止肿瘤细胞的细胞生长和/或细胞凋亡，从而抑制这些细胞的增殖。 因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。 本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统（CNS）的疾病，例如 神经退行性疾病 本发明进一步提供包含本发明化合物和易于遵循的这些药物组合物的安全给药方案的药物组合物，并且其在体内导致治疗有效量的这些化合物。
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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：US09932350B2
公开(公告)日：2018-04-03
申请号：US15515377
申请日：2015-09-25
申请人： MERCK SHARP & DOHME CORP. , Craig R. Gibeau , Solomon D. Kattar , Charles A. Lesburg , Jongwon Lim , John K. F. Maclean , Umar F. Mansoor , Alan B. Northrup , John M. Sanders , Graham F. Smith
发明人： Michael D. Altman , Jason D. Brubaker , Matthew L. Childers , Anthony Donofrio , Thierry Fischmann , Craig R. Gibeau , Solomon D. Kattar , Charles A. Lesburg , Jongwon Lim , John K. F. Maclean , Umar F. Mansoor , Alan B. Northrup , John M. Sanders , Graham F. Smith
IPC分类号： C07D491/08 , C07D239/94 , A61K31/517 , A61K45/06 , C07D239/88 , A61K31/5377 , C07D403/12 , C07D401/12 , C07D413/12 , A61K31/538 , C07D491/052 , A61K31/5386 , C07D491/048 , A61K31/55 , C07D405/12
CPC分类号： C07D491/08 , A61K31/517 , A61K31/5377 , A61K31/538 , A61K31/5386 , A61K31/55 , A61K45/06 , A61P29/00 , A61P35/00 , C07D239/88 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D491/048 , C07D491/052 , C07D498/08 , A61K2300/00
摘要： The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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