公开(公告)号：EP2649065A1

公开(公告)日：2013-10-16

申请号：EP11802248.2

申请日：2011-12-07

申请人： Amgen Inc.

发明人： WANG, Hui-Ling ,  BISWAS, Kaustav ,  CEE, Victor J. ,  CHAVEZ JR., Frank ,  HERBERICH, Bradley ,  JACKSON, Claire L.M. ,  LEE, Matthew ,  NIXEY, Thomas ,  PETTUS, Liping H. ,  REED, Anthony B. ,  RZASA, Robert M. ,  RUMFELT, Shannon ,  TASKER, Andrew ,  WU, Bin ,  WURZ, Ryan ,  LANMAN, Brian, A.

IPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D491/107 ,  A61K31/497 ,  A61K31/437 ,  A61K31/506 ,  A61K31/444 ,  A61K31/4709

CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： The invention relates to bicyclic compounds of formula (1'), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

公开(公告)号：EP1670794A2

公开(公告)日：2006-06-21

申请号：EP04789334.2

申请日：2004-09-30

申请人： AMGEN INC.

发明人： CHEN, Ning ,  NIXEY, Thomas ,  NORMAN, Mark, H.

IPC分类号： C07D417/12 ,  C07D401/12 ,  C07D405/12

CPC分类号： C07D213/65 ,  C04B35/632 ,  C07D213/68 ,  C07D213/70 ,  C07D213/74 ,  C07D237/14 ,  C07D237/18 ,  C07D237/20 ,  C07D241/18 ,  C07D241/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14

摘要： Compounds having the general structure formula (I) and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

摘要翻译： 具有通式结构式（I）的化合物和含有它们的组合物，用于治疗急性，炎性和神经性疼痛，牙痛，一般性头痛，偏头痛，丛集性头痛，混合血管和非血管性综合征，紧张性头痛，一般炎症 ，关节炎，风湿性疾病，骨关节炎，炎症性肠病，炎症性眼病，炎性或不稳定性膀胱病症，牛皮癣，具有炎性成分的皮肤病，慢性炎症，炎症性疼痛和相关的痛觉过敏和异常性疼痛，神经性疼痛和相关的痛觉过敏和异常性疼痛， 糖尿病性神经病疼痛，灼痛，交感神经维持性疼痛，神经传导障碍综合征，哮喘，上皮组织损伤或功能障碍，单纯疱疹，呼吸道内脏动力障碍，泌尿生殖器，胃肠或血管区域，伤口，烧伤，过敏性皮肤反应，瘙痒症， 一般胃肠道 胃溃疡，十二指肠溃疡，腹泻，由坏死物质诱导的胃损伤，毛发生长，血管舒缩或过敏性鼻炎，支气管疾病或膀胱疾病。

公开(公告)号：EP2935311A1

公开(公告)日：2015-10-28

申请号：EP13821554.6

申请日：2013-12-17

申请人： Amgen Inc.

发明人： HOLDER, Jerry Ryan ,  SWAMINATH, Gayathri ,  MIRANDA, Leslie P. ,  ARAL, Jennifer ,  DOHERTY, Elizabeth M. ,  NIXEY, Thomas

IPC分类号： C07K7/08 ,  C07K7/60

CPC分类号： A61K47/48215 ,  A61K38/08 ,  A61K38/10 ,  A61K47/48415 ,  A61K47/60 ,  A61K47/6811 ,  C07K7/08 ,  C07K14/47 ,  C07K14/503

摘要： The application is directed to APJ receptor agonist analogs having increased stability relative to the wild type apelin-13 and methods of using the agonist analogs. The analogs can be used, inter alia, in cardiac disorders such as heart failure.

摘要翻译： 该应用涉及具有相对于野生型apelin-13的稳定性增加的APJ受体激动剂类似物和使用激动剂类似物的方法。 类似物尤其可用于心脏病，例如心力衰竭。

公开(公告)号：EP1976836A2

公开(公告)日：2008-10-08

申请号：EP06848110.0

申请日：2006-12-22

申请人： Amgen Inc.

发明人： DE MORIN, Frenel, F. ,  CHEN, Jian J. ,  DOHERTY, Elizabeth M. ,  HITCHCOCK, Stephen ,  HUANG, Qi ,  KIM, Joseph, L. ,  LIU, Gang ,  NIXEY, Thomas ,  PARAS, Nick, A. ,  PETKUS, Jeffrey ,  RETZ, Daniel, M. ,  SMITH, Adrian, L. ,  TASKER, Andrew ,  ZHU, Jiawang

IPC分类号： C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D401/14

CPC分类号： C07D401/14 ,  C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have Formula (I) wherein R1 is Formula (II), (III) or (IV) and A1, A2, A3, A4, X, Z, Z', R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

公开(公告)号：EP1971598A1

公开(公告)日：2008-09-24

申请号：EP06837478.4

申请日：2006-11-13

申请人： Amgen Inc.

发明人： ZHONG, Wenge ,  HITCHCOCK, Stephen ,  ALBRECHT, Brian K ,  BARTBERGER, Michael ,  BROWN, James ,  BROWN, Ryan ,  CHAFFEE, Stuart C. ,  CHENG, Yuan ,  CROGHAN, Michael ,  GRACEFFA, Russell ,  HARRIED, Scott ,  HICKMAN, Dean ,  HORNE, Daniel ,  HUNGATE, Randall ,  JUDD, Ted ,  KALLER, Matthew ,  KREIMAN, Charles ,  LA, Daniel ,  LOPEZ, Patricia ,  MASSE, Craig E. ,  MONENSCHEIN, Holger ,  NGUYEN, Thomas ,  NIXEY, Thomas ,  PATEL, Vinod F. ,  PENNINGTON, Lewis ,  WEISS, Matthew ,  XUE, Qiufen ,  YANG, Bryant

IPC分类号： C07D405/12 ,  C07D413/12 ,  A61K31/44 ,  A61P25/28

CPC分类号： C07D405/12 ,  C07D311/68 ,  C07D413/12 ,  C07D491/052

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, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula (I), methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula (I), or compositions including them, to a subject. The invention also comprises further embodiments of Formulas (II) and (III), intermediates and processes useful for the preparation of compounds of the invention.

公开(公告)号：EP1963312A1

公开(公告)日：2008-09-03

申请号：EP06838016.1

申请日：2006-11-17

申请人： Amgen Inc.

发明人： XUE, Qiufen ,  ALBRECHT, Brian K. ,  ANDERSEN, Denise Lyn ,  BARTBERGER, Michael ,  BROWN, James ,  BROWN, Ryan ,  CHAFFEE, Stuart C. ,  CHENG, Yuan ,  CROGHAN, Michael ,  GRACEFFA, Russell ,  HARRIED, Scott ,  HITCHCOCK, Stephen ,  HUNGATE, Randall ,  JUDD, Ted ,  KALLER, Matthew ,  KREIMAN, Charles ,  LA, Daniel ,  LOPEZ, Patricia ,  MASSE, Craig E. ,  MONENSCHEIN, Holger ,  NGUYEN, Thomas ,  NIXEY, Thomas ,  PATEL, Vinod F. ,  PENNINGTON, Lewis ,  WEISS, Matthew ,  YANG, Bryant ,  ZHONG, Wenge

IPC分类号： C07D405/12 ,  C07D413/12 ,  A61K31/44 ,  A61P25/28

CPC分类号： C07D405/12 ,  C07D413/12

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 R1, W, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula (I), methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula (I), or compositions including them, to a subject. The invention also comprises further embodiments of Formulas (II) and (III), intermediates and processes useful for the preparation of compounds of the invention.

摘要翻译： 本发明包括用于调节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）的一类新化合物。 在一个实施方案中，所述化合物具有通式（I）其中R 1，W，B，R 3，R 4，R 5，i和j如本文所定义。 本发明还包括药物组合物，其包含一种或多种式（I）化合物，用于这些化合物的方法，包括治疗AD和相关疾病，通过施用式（I）化合物或包含它们的组合物， 到一个主题。 本发明还包括式（II）和（III）的其他实施方案，可用于制备本发明化合物的中间体和方法。

公开(公告)号：EP1963312B1

公开(公告)日：2014-07-02

申请号：EP06838016.1

申请日：2006-11-17

申请人： Amgen Inc.

发明人： XUE, Qiufen ,  ALBRECHT, Brian K. ,  ANDERSEN, Denise Lyn ,  BARTBERGER, Michael ,  BROWN, James ,  BROWN, Ryan ,  CHAFFEE, Stuart C. ,  CHENG, Yuan ,  CROGHAN, Michael ,  GRACEFFA, Russell ,  HARRIED, Scott ,  HITCHCOCK, Stephen ,  HUNGATE, Randall ,  JUDD, Ted ,  KALLER, Matthew ,  KREIMAN, Charles ,  LA, Daniel ,  LOPEZ, Patricia ,  MASSE, Craig E. ,  MONENSCHEIN, Holger ,  NGUYEN, Thomas ,  NIXEY, Thomas ,  PATEL, Vinod F. ,  PENNINGTON, Lewis ,  WEISS, Matthew ,  YANG, Bryant ,  ZHONG, Wenge

IPC分类号： C07D405/12 ,  C07D413/12 ,  A61K31/44 ,  A61P25/28

CPC分类号： C07D405/12 ,  C07D413/12

公开(公告)号：EP2504315A1

公开(公告)日：2012-10-03

申请号：EP10782786.7

申请日：2010-11-19

申请人： Amgen Inc.

发明人： CHENG, Yuan ,  POWERS, Timothy ,  ASHTON, Kate ,  BROWN, James ,  HARRIED, Scott ,  HITCHCOCK, Stephen ,  JUDD, Ted ,  LOPEZ, Patricia ,  NIXEY, Thomas ,  PARAS, Nick A, ,  POON, Steve F. ,  ST. JEAN JR., David J. ,  XUE, Qiufen ,  ZHONG, Wenge

IPC分类号： C07D215/38 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D417/04 ,  A61K31/4709 ,  A61P25/28

CPC分类号： C07D215/38 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D417/04

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 ring A, B
1 , B
2 , B
3 , L, R
1 , R
4 , R
5 and m 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 (AD), 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：EP1991530A1

公开(公告)日：2008-11-19

申请号：EP07751202.8

申请日：2007-02-20

申请人： Amgen Inc. ,  Memory Pharmaceuticals Corporation

发明人： ARRINGTON, Mark, P. ,  LIU, Ruiping ,  HOPPER, Allen, T. ,  CONTICELLO, Richard, D. ,  NGUYEN, Truc, M. ,  GAUSS, Carla, Maria ,  BURLI, Roland ,  HITCHCOCK, Stephen, A. ,  HU, Essa ,  KUNZ, Roxanne ,  NIXEY, Thomas ,  RUMFELT, Shannon

IPC分类号： C07D237/28 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/10 ,  C07D405/14 ,  C07D409/10 ,  C07D409/14 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10

CPC分类号： C07D237/28 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/10 ,  C07D405/14 ,  C07D409/10 ,  C07D409/14 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： The present invention is directed tojcjnnoline compounds of formula (I) that are PDE 1 inhibitors, pharmaceutical compositions containing such compounds and process for preparing such compounds. This invention is also directed to methods of treating diseases treatable by inhibition of PDElO enzyme, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

摘要翻译： 本发明涉及作为PDE1抑制剂的式（I）的炔丙醇化合物，含有此类化合物的药物组合物以及制备此类化合物的方法。 本发明还涉及治疗通过抑制PDE10酶如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，双相型障碍，强迫性障碍等可治疗的疾病的方法。

公开(公告)号：EP1653960A2

公开(公告)日：2006-05-10

申请号：EP04780799.5

申请日：2004-08-11

申请人： AMGEN INC.

发明人： HULME, Christopher ,  TEMPEST, Paul ,  MA, Vu ,  NIXEY, Thomas ,  BALOW, Guity

IPC分类号： A61K31/496 ,  C07D401/14 ,  C07D403/06

CPC分类号： C07D257/04 ,  C07D401/06 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12

摘要： Novel compounds, or pharmaceutically-acceptable salts, tautomers or prodrugs thereof, of Formula (I) wherein A, W, X, Z, R1-R3, and R8 are as defined in the specification, are provided. Also provided are methods of treating or preventing a melanin concentrating hormone-mediated disorder in a subject, comprising administering to a subject in need of such treatment or prevention a compound of Formula (I).