公开(公告)号：EP1631542A1

公开(公告)日：2006-03-08

申请号：EP04759403.1

申请日：2004-04-12

申请人： Amgen, Inc. ,  Array Biopharma, Inc.

发明人： GRONEBERG, Robert, D. ,  ASKEW, Ben ,  D'AMICO, Derin ,  ZHAN, James ,  TORO, Andras ,  YONGBOO, Kim ,  MARESKA, David, A. ,  HAN, Nianh ,  FOTSCH, Christopher, H. ,  LIU, Qinglan ,  RIAHI, Babak ,  YANG, Kevin ,  LI, Aiwan ,  YUAN, Chester ,  BISWAS, Kaustav ,  HARRIED, Scott ,  NGUYEN, Tom ,  QIAN, Wenyuan ,  CHEN, Jian, J. ,  NOMAK, Rana

IPC分类号： C07C311/18 ,  C07D311/68 ,  C07D295/135 ,  C07D279/00 ,  C07D409/12 ,  A61K31/34 ,  A61K31/18 ,  A61K31/33 ,  A61P29/00 ,  A61P25/04

CPC分类号： C07C311/19 ,  C07C311/13 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07D205/04 ,  C07D207/12 ,  C07D207/16 ,  C07D207/20 ,  C07D209/14 ,  C07D209/16 ,  C07D209/40 ,  C07D209/52 ,  C07D211/38 ,  C07D211/44 ,  C07D211/46 ,  C07D211/60 ,  C07D211/70 ,  C07D213/42 ,  C07D213/56 ,  C07D213/64 ,  C07D215/38 ,  C07D215/40 ,  C07D215/42 ,  C07D217/22 ,  C07D233/54 ,  C07D239/74 ,  C07D271/08 ,  C07D277/64 ,  C07D279/02 ,  C07D285/14 ,  C07D295/125 ,  C07D295/13 ,  C07D295/135 ,  C07D307/14 ,  C07D307/28 ,  C07D307/79 ,  C07D307/81 ,  C07D311/68 ,  C07D317/58 ,  C07D333/20 ,  C07D333/24 ,  C07D333/58 ,  C07D333/62 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D407/06 ,  C07D407/12 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/08

摘要： Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

摘要翻译： 选择的化合物是有效的用于治疗疼痛和疾病，：如炎症介导的疾病的。 本发明包括新化合物，类似物，前体药物和药学上可接受的衍生物，药物组合物和用于预防的方法和治疗疾病和其它疾病或病症涉及疼痛，炎症等。 本主题发明因此涉及一种用于制造测试以及的中间体在寻求过程中有用的化合物的方法。

公开(公告)号：EP1799637A1

公开(公告)日：2007-06-27

申请号：EP05797852.0

申请日：2005-09-19

申请人： Amgen, Inc

发明人： ASKEW, JR, Ben, C. ,  AYA, Toshihiro ,  BISWAS, Kaustav ,  CAI, Guolin ,  CHEN, Jian, J. ,  FOTSCH, Christopher, H. ,  HAN, Nianhe ,  HUMAN, Jason, Brooks ,  LI, Aiwen ,  LIU, Qingyian ,  PETERKIN, Tanya ,  QIAN, Wenyuan ,  RIAHI, Babak ,  YUAN, Chester, Chenguang ,  ZHU, Jiawang

IPC分类号： C07C311/19 ,  C07D207/48 ,  C07D211/08 ,  A61K31/18 ,  A61K31/40 ,  A61K31/445

CPC分类号： C07D207/26 ,  C07C311/19 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2602/10 ,  C07D211/38 ,  C07D215/36 ,  C07D233/24 ,  C07D243/08 ,  C07D275/06 ,  C07D281/02 ,  C07D291/08 ,  C07D295/135 ,  C07D311/68

摘要： This invention is in the field of pharmaceutical agents and specifically relates to compounds, compositions, uses and methods for treating inflammation-related disorders, including pain.

摘要翻译： 本发明涉及药剂领域，具体涉及用于治疗炎症相关疾病（包括疼痛）的化合物，组合物，用途和方法。

公开(公告)号：EP3177618A1

公开(公告)日：2017-06-14

申请号：EP15766951.6

申请日：2015-08-05

申请人： Amgen Inc.

发明人： ALLEN, Jennifer R. ,  AMEGADZIE, Albert ,  BOURBEAU, Matthew P. ,  BROWN, James A. ,  CHEN, Jian J. ,  CHENG, Yuan ,  FROHN, Michael J. ,  GUZMAN-PEREZ, Angel ,  HARRINGTON, Paul E. ,  LIU, Longbin ,  LIU, Qingyian ,  LOW, Jonathan D. ,  MA, Vu Van ,  MANNING, James R. ,  MINATTI, Ana Elena ,  NGUYEN, Thomas T. ,  NISHIMURA, Nobuko ,  NORMAN, Mark H. ,  PETTUS, Liping H. ,  PICKRELL, Alexander J. ,  QIAN, Wenyuan ,  RUMFELT, Shannon ,  RZASA, Robert M. ,  SIEGMUND, Aaron C. ,  STEC, Markian M. ,  WHITE, Ryan D. ,  XUE, Qiufen

IPC分类号： C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  A61K31/5415 ,  A61P25/28 ,  C07D279/08

CPC分类号： C07D417/12 ,  C07D279/08 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D513/10

摘要： 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.

摘要翻译： 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 这些化合物具有通式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，以及由BACE的生物活性产生的化合物和组合物用于治疗与A-β斑块形成和沉积相关的病症和/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：EP2547686A1

公开(公告)日：2013-01-23

申请号：EP11714873.4

申请日：2011-03-14

申请人： Amgen Inc.

发明人： CHEN, Jian, J. ,  ZHONG, Wenge ,  YANG, Bryant ,  QIAN, Wenyuan ,  LOPEZ, Patricia ,  WHITE, Ryan ,  WEISS, Matthew ,  JUDD, Ted ,  POWERS, Timothy ,  CHENG, Yuan ,  DINEEN, Thomas ,  EPSTEIN, Oleg ,  LOW, Jonathan ,  MARX, Isaac ,  MINATTI, Ana Elena ,  PARAS, Nick, A. ,  POTASHMAN, Michele

IPC分类号： C07D498/10 ,  C07D498/20 ,  C07D513/10 ,  C07D513/20 ,  A61K31/537 ,  A61K31/5386 ,  A61K31/547 ,  A61P25/28

CPC分类号： C07D513/10 ,  C07D498/10 ,  C07D498/20 ,  C07D513/20

摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I): wherein A
1 , A
2 , A
3 , A
4 , A
5 , A
6 , R
2 , R
7 , X, Y and Z of Formula (I) are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).

公开(公告)号：EP2328903A1

公开(公告)日：2011-06-08

申请号：EP09737222.1

申请日：2009-09-11

申请人： Amgen Inc.

发明人： WHITE, Ryan ,  AMEGADZIE, Albert ,  BRYAN, Marian C. ,  CHEN, Jian J. ,  CHENG, Alan C. ,  DINEEN, Thomas ,  EPSTEIN, Oleg ,  GORE, Vijay Keshav ,  HUA, Zihao ,  HUMAN, Jason B. ,  HUANG, Hongbing ,  KREIMAN, Charles ,  LA, Daniel ,  LIU, Qingyian ,  MA, Vu Van ,  MARX, Isaac ,  PATEL, Vinod F. ,  QIAN, Wenyuan ,  WEISS, Matthew ,  YUAN, Chester C.

IPC分类号： C07D498/10 ,  C07D513/10 ,  A61K31/424 ,  A61K31/429 ,  A61P25/28

CPC分类号： C07D498/10 ,  C07D513/10

摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein A
1 , A
2 , A
3 , A
4 , A
5 , A
6 , T
1 , T
2 , W, X, Y and Z of Formula (I) are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula (I).

公开(公告)号：EP2041088A1

公开(公告)日：2009-04-01

申请号：EP07796466.6

申请日：2007-06-26

申请人： AMGEN INC.

发明人： HITCHCOCK, Stephen ,  AMAGADZIE, Albert ,  QIAN, Wenyuan ,  XIA, Xiaoyang ,  HARRIED, Scott S.

IPC分类号： C07D213/36 ,  C07D243/08 ,  C07D295/14 ,  C07D333/20 ,  A61P25/18 ,  A61K31/495 ,  C07D241/04

CPC分类号： C07D241/04 ,  A61K31/495 ,  A61K31/551 ,  A61K33/00 ,  C07D213/36 ,  C07D241/08 ,  C07D243/08 ,  C07D295/15 ,  C07D333/20

摘要： The present invention provides compounds of formula (I) that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

公开(公告)号：EP1656355B1

公开(公告)日：2008-03-12

申请号：EP04820712.0

申请日：2004-06-21

申请人： AMGEN INC.

发明人： CHEN, Jian, J. ,  ASKEW, Ben, C. ,  BISWAS, Kaustav ,  CHAU, Jennifer, N. ,  D'AMICO, Derin, C. ,  HARRIED, Scott ,  NGUYEN, Thomas ,  QIAN, Wenyuan ,  ZHU, Jiawang ,  FOTSCH, Christopher, H. ,  HAN, Nianhe ,  LI, Aiwen ,  LIU, Qingyian ,  NISHIMURA, Nobuko ,  NOMAK, Rana ,  PETERKIN, Tanya ,  RIAHI, Babak ,  YANG, Kevin ,  YUAN, Chester, Chenguang

IPC分类号： A61K31/495 ,  C07D241/08 ,  C07D243/08 ,  C07D245/02 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14

CPC分类号： C07D241/08 ,  C07D243/08 ,  C07D245/02 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14

摘要： Compounds (I) are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

公开(公告)号：EP2864317A1

公开(公告)日：2015-04-29

申请号：EP13731237.7

申请日：2013-06-14

申请人： AMGEN, INC.

发明人： ALLEN, Jennifer R. ,  CHEN, Jian J. ,  FROHN, Michael J. ,  KALLER, Matthew Richard ,  LIU, Qingyian ,  NGUYEN, Thomas T. ,  PICKRELL, Alexander J. ,  QIAN, Wenyuan ,  RZASA, Robert M. ,  ZHONG, Wenge

IPC分类号： C07D401/14 ,  C07D403/14 ,  A61K31/497 ,  A61P25/00

CPC分类号： C07D471/04 ,  A61K31/497 ,  A61K31/517 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

摘要： 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.

公开(公告)号：EP2820014A1

公开(公告)日：2015-01-07

申请号：EP13709033.8

申请日：2013-02-28

申请人： Amgen Inc.

发明人： ALLEN, Jennifer R. ,  AMEGADZIE, Albert ,  ANDREWS, Kristin L. ,  BROWN, James ,  CHEN, Jian J. ,  CHEN, Ning ,  HARRINGTON, Essa Hu ,  LIU, Qingyian ,  NGUYEN, Thomas T. ,  PICKRELL, Alexander J. ,  QIAN, Wenyuan ,  RUMFELT, Shannon ,  RZASA, Robert M. ,  YUAN, Chester Chenguang ,  ZHONG, Wenge

IPC分类号： C07D417/12 ,  C07D471/04 ,  C07D473/00 ,  C07D473/30 ,  C07D473/34 ,  C07D473/40 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00 ,  A61K31/437 ,  A61P25/18

CPC分类号： C07D487/04 ,  C07D417/12 ,  C07D471/04 ,  C07D473/00 ,  C07D473/30 ,  C07D473/34 ,  C07D473/40 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

摘要： Heterobicyclic compounds of Formula (I): (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.

公开(公告)号：EP2231601B1

公开(公告)日：2014-06-18

申请号：EP08859859.4

申请日：2008-12-11

申请人： Amgen Inc.

发明人： HITCHCOCK, Stephen ,  QIAN, Wenyuan ,  AMEGADZIE, Albert

IPC分类号： C07D211/50 ,  C07D241/06 ,  A61K31/496 ,  A61K31/4523 ,  A61P25/18

CPC分类号： C07D211/50 ,  C07D241/06