公开(公告)号：EP1753736A2

公开(公告)日：2007-02-21

申请号：EP05756354.6

申请日：2005-05-24

申请人： Amgen Inc. ,  BIOVITRUM AB

发明人： HENRIKSSON, Martin ,  HOMAN, Evert ,  JOHANSSON, Lars ,  VALLGARDA, Jerk ,  WILLIAMS, Meredith ,  BERCOT, Eric ,  FOTSCH, Christopher, H. ,  LI, Aiwen ,  CAI, Guolin ,  HUNGATE, Randall, W. ,  YUAN, Chester, Chenguang ,  TEGLEY, Chirstopher ,  ST. JEAN, David ,  HAN, Nianhe ,  HUANG, Qi ,  LIU, Qingyian ,  BARTBERGER, Michael D. ,  MONIZ, George, A. ,  FRIZZLE, Matthew, J.

IPC分类号： C07D277/54 ,  C07D263/48 ,  A61K31/42 ,  A61K31/426 ,  A61P3/04 ,  A61P3/00 ,  A61P3/06 ,  A61P3/10 ,  A61P19/10 ,  A61P31/12 ,  A61P29/00 ,  A61P25/28 ,  A61P25/24

CPC分类号： C07D417/06 ,  C07D263/34 ,  C07D263/48 ,  C07D275/03 ,  C07D277/42 ,  C07D277/54 ,  C07D277/60 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/10 ,  C07F7/1856

摘要： The present invention relates to compounds with the formula (I), (II), (III) or (IV): (I) (II), (III), or (IV), wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

公开(公告)号：EP1951696A2

公开(公告)日：2008-08-06

申请号：EP06844335.7

申请日：2006-11-13

申请人： Amgen Inc. ,  BIOVITRUM AB

发明人： HENRIKSSON, Martin ,  HOMAN, Evert ,  JOHANSSON, Lars ,  VALLGARDA, Jerk ,  WILLIAMS, Meredith ,  BERCOT, Eric, A. ,  FOTSCH, Christopher, H. ,  LI, Aiwen ,  CAI, Guolin ,  HUNGATE, Randall, W. ,  YUAN, Chester, Chenguang ,  TEGLEY, Christopher ,  ST. JEAN, David, J., Jr. ,  HAN, Nianhe ,  HUANG, Qi ,  LIU, Qingyian ,  BARTBEGER, Michael, D. ,  MONIZ, George, A. ,  FRIZZLE, Matthew, J. ,  MARSHALL, Teresa, L.

IPC分类号： C07D277/54 ,  C07D277/60 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  A61K31/426 ,  A61K31/427

CPC分类号： C07D277/54 ,  C07D277/60 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： The present invention relates to thiazolinones and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11- β-hydroxysteroid dehydrogenase type 1 enzyme.

公开(公告)号：EP1753736B1

公开(公告)日：2008-12-17

申请号：EP05756354.6

申请日：2005-05-24

申请人： Amgen Inc. ,  BIOVITRUM AB

发明人： HENRIKSSON, Martin ,  HOMAN, Evert ,  JOHANSSON, Lars ,  VALLGARDA, Jerk ,  WILLIAMS, Meredith ,  BERCOT, Eric ,  FOTSCH, Christopher, H. ,  LI, Aiwen ,  CAI, Guolin ,  HUNGATE, Randall, W. ,  YUAN, Chester, Chenguang ,  TEGLEY, Chirstopher ,  ST. JEAN, David ,  HAN, Nianhe ,  HUANG, Qi ,  LIU, Qingyian ,  BARTBERGER, Michael D. ,  MONIZ, George, A. ,  FRIZZLE, Matthew, J.

IPC分类号： C07D277/54 ,  C07D263/48 ,  A61K31/42 ,  A61K31/426 ,  A61P3/04 ,  A61P3/00 ,  A61P3/06 ,  A61P3/10 ,  A61P19/10 ,  A61P31/12 ,  A61P29/00 ,  A61P25/28 ,  A61P25/24

CPC分类号： C07D417/06 ,  C07D263/34 ,  C07D263/48 ,  C07D275/03 ,  C07D277/42 ,  C07D277/54 ,  C07D277/60 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D513/10 ,  C07F7/1856

摘要： The present invention relates to compounds with the formula (I), (II), (III) or (IV): (I) (II), (III), or (IV), wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-β-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.

公开(公告)号：EP3897852A1

公开(公告)日：2021-10-27

申请号：EP19842520.9

申请日：2019-12-20

申请人： Amgen Inc.

发明人： TAMAYO, Nuria A. ,  BANERJEE, Abhisek ,  BROWN, James Alexander ,  FROHN, Michael J. ,  CHEN, Jian Jeffrey ,  LI, Kexue ,  LIU, Qingyian ,  LOW, Jonathan Dante ,  MA, Vu ,  PETTUS, Liping H. ,  WALTON, Mary Catherine ,  MINATTI, Ana Elena ,  BOURBEAU, Matthew Paul ,  JIA, Lei

IPC分类号： A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  A61K31/506 ,  C07D419/14 ,  C07D491/044

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：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：EP2121580A2

公开(公告)日：2009-11-25

申请号：EP07853344.5

申请日：2007-12-12

申请人： Amgen Inc.

发明人： YUAN, Chester, C. ,  HAN, Nianhe ,  LIU, Qingyian ,  MCMINN, Dustin ,  POWERS, Jay

IPC分类号： C07C233/81 ,  C07C233/74 ,  C07D213/40 ,  C07C233/23

CPC分类号： C07C233/74 ,  C07C237/22 ,  C07C271/12 ,  C07C2601/02 ,  C07C2601/14 ,  C07D213/30 ,  C07D213/40

摘要： The present invention provides N-cyclohexyl benzamide and benzeneacetamide compounds according to formula (I): where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, m, n, p, and q are as defined in the description; as well as pharmaceutical compositions comprising the same, methods of use of the compounds and compositions of the invention for the treatment of conditions associated with hydroxysteroid dehydrogenases (e.g., 11β-HSD1), and the use of the compounds of the invention in the preparation of medicaments for the treatment of hydroxysteroid dehydrogenase-associated conditions.

摘要翻译： 本发明提供了式（I）的N-环己基苯甲酰胺和苯乙酰胺化合物：其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11，R12，R13，m，n，p ，和q如说明书中所定义; 以及包含其的药物组合物，使用本发明化合物和组合物的方法用于治疗与羟基类固醇脱氢酶（例如，11＆amp; -HSD1）相关的病症，以及本发明化合物在制剂中的用途 的用于治疗羟类固醇脱氢酶相关病症的药物。

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：EP4103558A1

公开(公告)日：2022-12-21

申请号：EP21719299.6

申请日：2021-02-11

申请人： Amgen Inc.

发明人： ALLEN, Jennifer Rebecca ,  AMEGADZIE, Albert ,  BEYLKIN, Diane Jennifer ,  BOOKER, Shon ,  BOURBEAU, Matthew Paul ,  BUTLER, John R. ,  FROHN, Michael J. ,  GLAD, Sanne Ormholt Schroder ,  HUSEMOEN, Birgitte Weinreich ,  KALLER, Matthew R. ,  KOHN, Todd J. ,  LANMAN, Brian Alan ,  LI, Kexue ,  LIU, Qingyian ,  LOPEZ, Patricia ,  MA, Vu Van ,  MANONI, Francesco ,  MEDINA, Jose ,  MINATTI, Ana Elena ,  PEIRO CADAHIA, Jorge ,  PETTUS, Liping ,  PICKRELL, Alexander J. ,  SARVARY, Ian ,  TAMAYO, Nuria A. ,  VESTERGAARD, Mikkel

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  A61P35/00 ,  A61K31/435

公开(公告)号：EP3897855A1

公开(公告)日：2021-10-27

申请号：EP19845855.6

申请日：2019-12-20

申请人： Amgen Inc.

发明人： TAMAYO, Nuria A. ,  BANERJEE, Abhisek ,  BROWN, James Alexander ,  FROHN, Michael J. ,  CHEN, Jian Jeffrey ,  LI, Kexue ,  LIU, Qingyian ,  LOW, Jonathan Dante ,  MA, Vu ,  PETTUS, Liping H. ,  WALTON, Mary Catherine ,  MINATTI, Ana Elena ,  BOURBEAU, Matthew Paul ,  JIA, Lei ,  NGUYEN, Thomas T. ,  NISHIMURA, Nobuko ,  XUE, Qiufen May ,  ALLEN, John Gordon

IPC分类号： A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  A61K31/497 ,  A61K31/444