-
公开(公告)号：US10246429B2
公开(公告)日：2019-04-02
申请号：US15749895
申请日：2016-08-04
Applicant: AMGEN INC.
Inventor： Jennifer R. Allen , Albert Amegadzie , Matthew P. Bourbeau , James A. Brown , Ning Chen , Michael J. Frohn , Longbin Liu , Qingyian Liu , Liping H. Pettus , Wenyuan Qian , Corey M. Reeves , Aaron C. Siegmund
IPC: C07D417/10 , C07D279/08 , C07D417/14 , C07D471/04 , C07D491/056 , A61P25/28 , A61P25/00 , A61P25/16 , C07D491/08 , C07D491/107 , C07D498/10 , C07F7/08
Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A7, and each of Ra, Rb, R1, R2, R3, R8 R9 and R10 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions.
-
公开(公告)号：US20140148435A1
公开(公告)日：2014-05-29
申请号：US14170146
申请日：2014-01-31
Applicant: AMGEN INC.
Inventor： Jennifer R. Allen , Jian J. Chen , Michael J. Frohn , Matthew R. Kaller , Qingyian Liu , Thomas T. Nguyen , Alexander J. Pickrell , Wenyuan Qian , Robert M. Rzasa , Wenge Zhong
IPC: C07D471/04 , A61K31/517 , A61K45/06 , C07D403/14 , C07D401/14 , A61K31/497
CPC classification number: C07D471/04 , A61K31/497 , A61K31/517 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
Abstract translation: 式（I）的氮杂环丁烷和哌啶化合物：如说明书中所定义，含有它们的组合物，以及制备这些化合物的方法及其中间体。 本文还提供治疗认知障碍或通过抑制PDE10可治疗的疾病的方法，例如亨廷顿舞蹈病，精神分裂症，双相障碍，强迫症等。
-
公开(公告)号：US08691986B2
公开(公告)日：2014-04-08
申请号：US13917699
申请日：2013-06-14
Applicant: Amgen Inc.
Inventor： Jennifer R. Allen , Jian J. Chen , Michael J. Frohn , Matthew R. Kaller , Qingyian Liu , Thomas T. Nguyen , Alexander J. Pickrell , Wenyuan Qian , Robert M. Rzasa , Wenge Zhong
IPC: C07D241/00 , C07D239/70 , C07D471/02 , C07D215/00
CPC classification number: C07D471/04 , A61K31/497 , A61K31/517 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
Abstract translation: 式（I）的氮杂环丁烷和哌啶化合物：如说明书中所定义，含有它们的组合物，以及制备这些化合物的方法及其中间体。 本文还提供治疗认知障碍或通过抑制PDE10可治疗的疾病的方法，例如亨廷顿舞蹈病，精神分裂症，双相障碍，强迫症等。
-
公开(公告)号：US09303028B2
公开(公告)日：2016-04-05
申请号：US14170146
申请日：2014-01-31
Applicant: AMGEN INC.
Inventor： Jennifer R. Allen , Jian J. Chen , Michael J. Frohn , Matthew R. Kaller , Qingyian Liu , Thomas T. Nguyen , Alexander J. Pickrell , Wenyuan Qian , Robert M. Rzasa , Wenge Zhong
IPC: A61K31/497 , A61K31/517 , C07D401/14 , C07D403/14 , C07D471/04 , A61K45/06
CPC classification number: C07D471/04 , A61K31/497 , A61K31/517 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
Abstract translation: 式（I）的氮杂环丁烷和哌啶化合物：如说明书中所定义，含有它们的组合物，以及制备这些化合物的方法及其中间体。 本文还提供治疗认知障碍或通过抑制PDE10可治疗的疾病的方法，例如亨廷顿舞蹈病，精神分裂症，双相障碍，强迫症等。
-
公开(公告)号：US20130225552A1
公开(公告)日：2013-08-29
申请号：US13780557
申请日：2013-02-28
Applicant: Amgen Inc.
Inventor： Jennifer R. Allen , Albert Amegadzie , Kristin L. Andrews , James Brown , Jian J. Chen , Ning Chen , Essa Hu Harrington , Qingyian Liu , Thomas T. Nguyen , Alexander J. Pickrell , Wenyuan Qian , Shannon Rumfelt , Robert M. Rzasa , Chester Chenguang Yuan , Wenge Zhong
IPC: C07D487/04 , C07D513/04 , C07D471/04 , C07D498/04 , C07D473/00
CPC classification number: C07D487/04 , C07D417/12 , C07D471/04 , C07D473/00 , C07D473/30 , C07D473/34 , C07D473/40 , C07D498/04 , C07D513/04 , C07D519/00
Abstract: Heterobicyclic compounds of Formula (I): or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, Huntington's Disease, and the like.
Abstract translation: 式（I）的异双环化合物：或其药学上可接受的盐，互变异构体或立体异构体，以及含有它们的组合物，以及制备这些化合物的方法。 本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，双相情感障碍，强迫症，亨廷顿舞蹈病等。
-
Patent Agency Ranking
6.发明授权Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use 有权环丙基稠合噻嗪-2-胺化合物作为β-分泌酶抑制剂和使用方法公开(公告)号：US09550762B2
公开(公告)日：2017-01-24
申请号：US14819256
申请日：2015-08-05
Applicant: AMGEN INC.
Inventor： Jennifer R. Allen , Albert Amegadzie , Matthew P. Bourbeau , James A. Brown , Jian J. Chen , Yuan Cheng , Michael J. Frohn , Angel Guzman-Perez , Paul E. Harrington , Longbin Liu , Qingyian Liu , Jonathan D. Low , Vu Van Ma , James Manning , Ana Elena Minatti , Thomas T. Nguyen , Nobuko Nishimura , Mark H. Norman , Liping H. Pettus , Alexander J. Pickrell , Wenyuan Qian , Shannon Rumfelt , Robert M. Rzasa , Aaron C. Siegmund , Markian M. Stec , Ryan D. White , Qiufen Xue
IPC: C07D417/12 , C07D417/14 , C07D471/04 , C07D513/10 , C07D417/04 , C07D279/08
CPC classification number: C07D417/12 , C07D279/08 , C07D417/04 , C07D417/14 , C07D471/04 , C07D513/10
Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, and each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
Abstract translation: 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 所述化合物具有通式I：其中式I中的变量A4，A5，A6，A8以及R 1，R b，R 1，R 2，R 3和R 7各自独立地定义。 本发明还提供包含该化合物的药物组合物，以及该化合物和组合物用于治疗由BACE的生物学活性产生的与A-β斑块形成和沉积有关的病症和/或病症的用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明还提供式II和III的化合物及其分子式实施方案，用于制备本发明化合物的中间体和方法。
-
7.发明授权Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use 有权全氟化的5,6-二氢-4H-1,3-恶嗪-2-胺化合物作为β-分泌酶抑制剂和使用方法公开(公告)号：US09296734B2
公开(公告)日：2016-03-29
申请号：US14192710
申请日：2014-02-27
Applicant: AMGEN INC.
Inventor： Ana Elena Minatti , Jonathan D. Low , Jennifer R. Allen , Jian Chen , Ning Chen , Yuan Cheng , Ted Judd , Qingyian Liu , Patricia Lopez , Wenyuan Qian , Shannon Rumfelt , Robert M. Rzasa , Nuria A. Tamayo , Qiufen Xue , Bryant Yang , Wenge Zhong
IPC: C07D413/14 , C07D413/12 , C07D471/04 , C07D513/04 , C07F7/08 , C07D413/04 , C07D413/10 , C07D265/08 , C07D498/04
CPC classification number: C07D413/14 , C07D265/08 , C07D413/04 , C07D413/10 , C07D413/12 , C07D471/04 , C07D498/04 , C07D513/04 , C07F7/0812
Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of R1 and R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.
Abstract translation: 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 化合物具有通式I：其中式I中的各个R 1和R 2，R 3和R 7各自独立地定义的变量A4，A5，A6，A8在本文中定义。 本发明还提供包含该化合物的药物组合物，以及用于治疗由BACE的生物学活性产生的A-β斑块形成和沉积相关的病症和/或病症的化合物和组合物的相应用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明还提供式II和III的化合物及其分式实施方案，可用于制备式I-III化合物的中间体和方法和方法。
-
8.发明授权Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use 有权全氟化环丙基稠合的1,3-恶嗪-2-胺化合物作为β-分泌酶抑制剂和使用方法公开(公告)号：US09085576B2
公开(公告)日：2015-07-21
申请号：US14199844
申请日：2014-03-06
Applicant: AMGEN INC.
Inventor： Ana Elena Minatti , Jonathan D. Low , Jennifer R. Allen , Albert Amegadzie , James Brown , Michael J. Frohn , Angel Guzman-Perez , Paul E. Harrington , Patricia Lopez , Vu Van Ma , Nobuko Nishimura , Wenyuan Qian , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Adrian L. Smith , Ryan White , Qiufen Xue
IPC: C07D471/04 , C07D265/12 , C07D417/12 , C07D417/14 , C07D413/12 , C07D413/14 , A61K31/537 , C07D413/10 , C07D491/048
CPC classification number: C07D413/12 , C07D265/12 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048
Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
Abstract translation: 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 化合物具有通式I：其中式I中的每个R a，R b，R 1，R 2，R 3和R 7各自独立地定义的变量A4，A5，A6，A8在本文中定义。 本发明还提供包含该化合物的药物组合物，以及该化合物和组合物用于治疗由BACE的生物学活性产生的与A-β斑块形成和沉积有关的病症和/或病症的用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明还提供式II和III的化合物及其分子式实施方案，用于制备本发明化合物的中间体和方法。
-
公开(公告)号：US09174992B2
公开(公告)日：2015-11-03
申请号：US13780557
申请日：2013-02-28
Applicant: Amgen Inc.
Inventor： Jennifer R. Allen , Albert Amegadzie , Kristin L. Andrews , James Brown , Jian J. Chen , Ning Chen , Essa Hu Harrington , Qingyian Liu , Thomas T. Nguyen , Alexander J. Pickrell , Wenyuan Qian , Shannon Rumfelt , Robert M. Rzasa , Chester Chenguang Yuan , Wenge Zhong
IPC: C07D419/14 , C07D419/12 , C07D487/04 , C07D498/04 , C07D473/00 , C07D471/04 , C07D513/04 , C07D417/12 , C07D473/30 , C07D473/34 , C07D473/40 , C07D519/00
CPC classification number: C07D487/04 , C07D417/12 , C07D471/04 , C07D473/00 , C07D473/30 , C07D473/34 , C07D473/40 , C07D498/04 , C07D513/04 , C07D519/00
Abstract: Heterobicyclic compounds of Formula (I): or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, Huntington's Disease, and the like.
Abstract translation: 式（I）的异双环化合物：或其药学上可接受的盐，互变异构体或立体异构体，以及含有它们的组合物，以及制备这些化合物的方法。 本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，双相情感障碍，强迫症，亨廷顿舞蹈病等。
-
公开(公告)号：US20130338138A1
公开(公告)日：2013-12-19
申请号：US13917699
申请日：2013-06-14
Applicant: AMGEN INC.
Inventor： Jennifer R. Allen , Jian J. Chen , Michael J. Frohn , Matthew R. Kaller , Qingyian Liu , Thomas T. Nguyen , Alexander J. Pickrell , Wenyuan Qian , Robert M. Rzasa , Wenge Zhong
IPC: C07D401/14 , C07D471/04 , A61K31/517 , A61K31/497 , A61K45/06
CPC classification number: C07D471/04 , A61K31/497 , A61K31/517 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
Abstract translation: 式（I）的氮杂环丁烷和哌啶化合物：如说明书中所定义，含有它们的组合物，以及制备这些化合物的方法及其中间体。 本文还提供治疗认知障碍或通过抑制PDE10可治疗的疾病的方法，例如亨廷顿舞蹈病，精神分裂症，双相障碍，强迫症等。
-
-
-
-
-
-
-
-
-
Search Results
15
records
(took 0.046 seconds)
