公开(公告)号：WO2007048070A3

公开(公告)日：2007-07-12

申请号：PCT/US2006041562

申请日：2006-10-23

Applicant: AMGEN INC ,  GERMAIN JULIE ,  ASKEW BENNY C JR ,  BAUER DAVID ,  CHOQUETTE DEBORAH ,  DIPIETRO LUCIAN V ,  GRACEFFA RUSSELL ,  HARMANAGE JEAN-CHRISTOPHE ,  HUANG QI ,  KIM JOSEPH L ,  LA DANIEL ,  LI AIWEN ,  NISHIMURA NOBUKO ,  NOMACK RANA ,  PATEL VINOD ,  POTASHMAN MICHELE ,  RIAHI BABAK ,  STORZ THOMAS ,  VAN DER PLAS SIMON ,  YANG KEVIN ,  YUAN CHESTER C

Inventor： GERMAIN JULIE ,  ASKEW BENNY C JR ,  BAUER DAVID ,  CHOQUETTE DEBORAH ,  DIPIETRO LUCIAN V ,  GRACEFFA RUSSELL ,  HARMANAGE JEAN-CHRISTOPHE ,  HUANG QI ,  KIM JOSEPH L ,  LA DANIEL ,  LI AIWEN ,  NISHIMURA NOBUKO ,  NOMACK RANA ,  PATEL VINOD ,  POTASHMAN MICHELE ,  RIAHI BABAK ,  STORZ THOMAS ,  VAN DER PLAS SIMON ,  YANG KEVIN ,  YUAN CHESTER C

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

CPC classification number: C07D471/04 ,  C07D487/04

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

Abstract translation: 所选化合物对于预防和治疗诸如血管生成介导的疾病等疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：WO2007048070A2

公开(公告)日：2007-04-26

申请号：PCT/US2006/041562

申请日：2006-10-23

Applicant: AMGEN INC. ,  GERMAIN, Julie ,  ASKEW, Benny, C., Jr. ,  BAUER, David ,  CHOQUETTE, Deborah ,  DIPIETRO, Lucian, V. ,  GRACEFFA, Russell ,  HARMANAGE, Jean-Christophe ,  HUANG, Qi ,  KIM, Joseph, L. ,  LA, Daniel ,  LI, Aiwen ,  NISHIMURA, Nobuko ,  NOMACK, Rana ,  PATEL, Vinod ,  POTASHMAN, Michele ,  RIAHI, Babak ,  STORZ, Thomas ,  VAN DER PLAS, Simon ,  YANG, Kevin ,  YUAN, Chester, C.

Inventor： GERMAIN, Julie ,  ASKEW, Benny, C., Jr. ,  BAUER, David ,  CHOQUETTE, Deborah ,  DIPIETRO, Lucian, V. ,  GRACEFFA, Russell ,  HARMANAGE, Jean-Christophe ,  HUANG, Qi ,  KIM, Joseph, L. ,  LA, Daniel ,  LI, Aiwen ,  NISHIMURA, Nobuko ,  NOMACK, Rana ,  PATEL, Vinod ,  POTASHMAN, Michele ,  RIAHI, Babak ,  STORZ, Thomas ,  VAN DER PLAS, Simon ,  YANG, Kevin ,  YUAN, Chester, C.

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

CPC classification number: C07D471/04 ,  C07D487/04

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

Abstract translation: 所选化合物对于预防和治疗诸如血管生成介导的疾病等疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：WO2010030954A1

公开(公告)日：2010-03-18

申请号：PCT/US2009/056748

申请日：2009-09-11

Applicant: AMGEN INC. ,  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.

Inventor： 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: C07D498/10 ,  C07D513/10 ,  A61K31/424 ,  A61K31/429 ,  A61P25/28

CPC classification number: C07D498/10 ,  C07D513/10

Abstract: 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).

Abstract translation: 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式（I）; 其中本文定义式（I）的A1，A2，A3，A4，A5，A6，T1，T2，W，X，Y和Z。 本发明还包括在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的疾病和病症的用途。 这种病症包括例如阿尔茨海默氏病，认知缺陷，认知障碍，精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。 本发明还包括式I的其它实施方案，可用于制备式（I）化合物的中间体和方法。

公开(公告)号：WO2008088540A3

公开(公告)日：2009-02-05

申请号：PCT/US2007025360

申请日：2007-12-12

Applicant: AMGEN INC ,  YUAN CHESTER C ,  HAN NIANHE ,  LIU QINGYIAN ,  MCMINN DUSTIN ,  POWERS JAY

Inventor： YUAN CHESTER C ,  HAN NIANHE ,  LIU QINGYIAN ,  MCMINN DUSTIN ,  POWERS JAY

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

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

Abstract: 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., 11ß-HSD1), and the use of the compounds of the invention in the preparation of medicaments for the treatment of hydroxysteroid dehydrogenase-associated conditions.

Abstract translation: （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，使用本发明的化合物和组合物治疗与羟基类固醇脱氢酶（例如11β-HSD1）相关病症的方法，以及本发明化合物在制备 用于治疗羟基类固醇脱氢酶相关病症的药物。

公开(公告)号：WO2008088540A4

公开(公告)日：2008-07-24

申请号：PCT/US2007/025360

申请日：2007-12-12

Applicant: AMGEN INC. ,  YUAN, Chester, C. ,  HAN, Nianhe ,  LIU, Qingyian ,  MCMINN, Dustin ,  POWERS, Jay

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

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

Abstract: The present invention provides N-cyclohexyl benzamide and benzeneacetamide compounds according to formula (I): where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , 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.

公开(公告)号：WO2008088540A2

公开(公告)日：2008-07-24

申请号：PCT/US2007025360

申请日：2007-12-12

Applicant: AMGEN INC ,  YUAN CHESTER C ,  HAN NIANHE ,  LIU QINGYIAN ,  MCMINN DUSTIN ,  POWERS JAY

Inventor： YUAN CHESTER C ,  HAN NIANHE ,  LIU QINGYIAN ,  MCMINN DUSTIN ,  POWERS JAY

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

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

Abstract: The present invention provides N-cyclohexyl benzamide and benzeneacetamide compounds according to formula (I): where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , 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., 11ß-HSD1), and the use of the compounds of the invention in the preparation of medicaments for the treatment of hydroxysteroid dehydrogenase-associated conditions.

Abstract translation: 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R 1，R 2，R 3，R 3， R 4，R 5，R 6，R 7，R 8，R 8，R 8， R 9，R 10，R 11，R 12，R 13，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11β-HSD1）相关的病症的用途，以及本发明化合物在制备 用于治疗羟基类固醇脱氢酶相关病症的药物。