公开(公告)号：US20230406844A1

公开(公告)日：2023-12-21

申请号：US18248407

申请日：2021-10-27

申请人： Peter H. FULLER ,  Anmol GULATI ,  Solomon D. KATTAR ,  Mitchell H. KEYLOR ,  Kaila A. MARGREY ,  Xin YAN ,  MERCK SHARP & DOHME CORP.

发明人： Peter H. Fuller ,  Anmol Gulati ,  Solomon D. Kattar ,  Mitchell H. Keylor ,  Kaila A. Margrey ,  Xin Yan

IPC分类号： C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D401/04 ,  C07D471/04 ,  C07D401/14 ,  C07D471/08 ,  C07D217/22 ,  C07D409/14

CPC分类号： C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D401/04 ,  C07D471/04 ,  C07D401/14 ,  C07D471/08 ,  C07D217/22 ,  C07D409/14

摘要： The present invention is directed to certain 2-aminoquinzaoline derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, and R3 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 such diseases in which LRRK-2 kinase is involved.

公开(公告)号：US20230023066A1

公开(公告)日：2023-01-26

申请号：US17769814

申请日：2020-10-20

申请人： Mitchell H. KEYLOR ,  Michael j. ARDOLINO ,  Ryan W. CHAU ,  Peter H. FULLER ,  Anmol GULATI ,  Rebecca Elizabeth JOHNSON ,  Solomon D. KATTAR ,  Kaila A. MARGREY ,  Gregori J. MOREIELLO ,  Santhosh F. NEELAMKAVIL ,  Xin YAN ,  Elsie C. YU ,  Cayetena Carmela ZARATE SAEZ ,  Merck Sharp & Dohme Corp.

发明人： Mitchell H. Keylor ,  Michael J. Ardolino ,  Ryan W. Chau ,  Peter H. Fuller ,  Anmol Gulati ,  Rebecca Elizabeth Johnson ,  Solomon D. Kattar ,  Kaila A. Margrey ,  Gregori J. Morriello ,  Santhosh F. Neelamkavil ,  Xin Yan ,  Elsie C. Yu ,  Cayetana Carmela Zarate Saez

IPC分类号： C07D403/14 ,  C07D405/14 ,  C07D403/12 ,  C07D417/14 ,  C07D401/14 ,  C07D413/14 ,  C07D409/14

摘要： The present invention is directed to substituted certain N-(heteroaryl)quinazolin-2-amine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein J, R3, and R4, 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.

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.

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.

公开(公告)号：US20160326156A1

公开(公告)日：2016-11-10

申请号：US15105316

申请日：2014-12-18

申请人： Thomas A. MILLER ,  Alessia PETROCCHI ,  Eric T. ROMEO ,  Dilrukshi VITHARANA ,  Solomon D. KATTAR ,  Alan B. NORTHRUP ,  Michael D. ALTMAN ,  Neville J. ANTHONY ,  MERCK SHARP & DOHME CORP.

发明人： Thomas A. Miller ,  Alessia Petrocchi ,  Eric T. Romeo ,  Dilrukshi Vitharana ,  Solomon D. Kattar ,  Alan B. Northrup ,  Michael D. Altman ,  Neville J. Anthony

IPC分类号： C07D417/12 ,  C07D495/04 ,  A61K31/437 ,  C07D471/04 ,  A61K31/444 ,  C07D491/048 ,  A61K31/517 ,  A61K31/519

CPC分类号： C07D417/12 ,  A61K31/437 ,  A61K31/444 ,  A61K31/517 ,  A61K31/519 ,  C07D413/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04

摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring A, and the subscripts n1, n2, and r 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： 本发明提供了式（I）（I）的某些噻唑取代的氨基杂芳基化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，环A和下标n 1，n 2和r如上定义 这里。 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。

公开(公告)号：US09353066B2

公开(公告)日：2016-05-31

申请号：US14422419

申请日：2013-08-15

申请人： Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

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。

公开(公告)号：US09969749B2

公开(公告)日：2018-05-15

申请号：US15515383

申请日：2015-09-25

申请人： MERCK SHARP & DOHME CORP.

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.

公开(公告)号：US09416111B2

公开(公告)日：2016-08-16

申请号：US14409200

申请日：2013-06-17

申请人： Merck Sharp & Dohme Corp.

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。

公开(公告)号：US20150232428A1

公开(公告)日：2015-08-20

申请号：US14422419

申请日：2013-08-15

申请人： Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

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。

公开(公告)号：US20150166486A1

公开(公告)日：2015-06-18

申请号：US14409200

申请日：2013-06-17

申请人： Merck Sharp & Dohme Corp.

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。