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1.发明申请VINYL FLUORIDE CYCLOPROPYL FUSED THIAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE 审中-公开作为β-分泌酶抑制剂的乙烯基氟化物环丙二烯化的噻嗪-2-胺化合物及其使用方法
公开(公告)号：WO2017024180A1
公开(公告)日：2017-02-09
申请号：PCT/US2016/045650
申请日：2016-08-04
Applicant: AMGEN INC.
Inventor： ALLEN, Jennifer, R. , AMEGADZIE, Albert , BOURBEAU, Matthew, P. , BROWN, James, A. , CHEN, Ning , FROHN, Michael, J. , LIU, Longbin , LIU, Qingyian , PETTUS, Liping, H. , QIAN, Wenyuan , REEVES, Corey, M. , SIEGMUND, Aaron, C.
IPC: A61K31/5415 , A61P25/28 , C07D417/10 , C07D417/14 , C07D471/04 , C07D491/056 , C07D279/08
CPC classification number: C07D417/10 , C07D279/08 , C07D417/14 , C07D471/04 , C07D491/056
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 A 4 , A 5 , A 6 , A 7 , and each of R a , R b , R 1 , R 2 , R 3 , R 8 R 9 and R 10 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.
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中的变量A4，A5，A6，A7以及式I的R a，R b，R 1，R 2，R 3，R 8 R 9和R 10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Aβ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。
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2.发明申请TRICYCLIC ALKYNES THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN 审中-公开与GLUCOKINASE法规蛋白质相互作用的TRICYCLIC ALKYNES
公开(公告)号：WO2014035872A1
公开(公告)日：2014-03-06
申请号：PCT/US2013/056593
申请日：2013-08-26
Applicant: AMGEN INC.
Inventor： ASHTON, Kate , FOTSCH, Christopher H. , KUNZ, Roxanne K. , LIU, Longbin , NISHIMURA, Nobuko , NORMAN, Mark H. , SIEGMUND, Aaron C. , ST. JEAN, JR., David J. , TAMAYO, Nuria A. , YANG, Kevin C.
IPC: C07D403/12 , C07D401/14 , C07D413/14 , C07D401/12 , C07D417/14 , A61K31/501 , A61K31/496 , A61P3/00
CPC classification number: C07D401/12 , C07D401/14 , C07D403/12 , C07D413/14 , C07D417/14
Abstract: The present invention relates to tricyclic alkyne compounds of formula I that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
Abstract translation: 本发明涉及与葡萄糖激酶调节蛋白相互作用的式I的三环炔化合物。 此外，本发明还涉及治疗2型糖尿病的方法，以及使用该化合物或其药学上可接受的盐涉及葡萄糖激酶调节蛋白的其它疾病和/或病症，以及含有该化合物或其药学上可接受的盐的药物组合物 它们。
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公开(公告)号：WO2010126895A1
公开(公告)日：2010-11-04
申请号：PCT/US2010/032593
申请日：2010-04-27
Applicant: AMGEN INC. , ANDREWS, Kristin , BO, Yunxin, Y. , BOOKER, Shon , CEE, Victor, J. , D'ANGELO, Noel , HERBERICH, Bradley, J. , HONG, Fang-Tsao , JACKSON, Claire, L., M. , LANMAN, Brian, A. , LIAO, Hongyu , LIU, Longbin , NISHIMURA, Nobuko , NORMAN, Mark, H. , PETTUS, Liping, H. , REED, Anthony, B. , SMITH, Adrian, L. , TADESSE, Seifu , TAMAYO, Nuria, A. , WU, Bin , WURZ, Ryan , YANG, Kevin
Inventor： ANDREWS, Kristin , BO, Yunxin, Y. , BOOKER, Shon , CEE, Victor, J. , D'ANGELO, Noel , HERBERICH, Bradley, J. , HONG, Fang-Tsao , JACKSON, Claire, L., M. , LANMAN, Brian, A. , LIAO, Hongyu , LIU, Longbin , NISHIMURA, Nobuko , NORMAN, Mark, H. , PETTUS, Liping, H. , REED, Anthony, B. , SMITH, Adrian, L. , TADESSE, Seifu , TAMAYO, Nuria, A. , WU, Bin , WURZ, Ryan , YANG, Kevin
IPC: C07D401/14 , C07D473/00 , A61K31/52 , A61P35/00
CPC classification number: C07D473/00 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.
Abstract translation: 本发明涉及式I化合物或其药学上可接受的盐; 使用该化合物治疗疾病或病症如癌症的方法; 和含有这些化合物的药物组合物，其中变量如本文所定义。
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公开(公告)号：WO2019213516A1
公开(公告)日：2019-11-07
申请号：PCT/US2019/030593
申请日：2019-05-03
Applicant: AMGEN INC.
Inventor： ALLEN, John Gordon , ALLEN, Jennifer Rebecca , MINATTI, Ana Elena , XUE, Qiufen , WURZ, Ryan Paul , TEGLEY, Christopher M. , PICKRELL, Alexander J. , NGUYEN, Thomas T. , MA, Vu Van , LOPEZ, Patricia , LIU, Longbin , KOPECKY, David John , FROHN, Michael J. , CHEN, Ning , CHEN, Jian Jeffrey , SIEGMUND, Aaron C. , AMEGADZIE, Albert , TAMAYO, Nuria A. , BOOKER, Shon , GOODMAN, Clifford , WALTON, Mary , NISHIMURA, Nobuko , SHIN, Youngsook , LOW, Jonathan D. , CEE, Victor J. , REED, Anthony B. , WANG, Hui-Ling , LANMAN, Brian Alan
IPC: C07D403/04 , C07D403/14 , C07D471/04 , C07D487/04 , A61P35/00 , A61K31/519
Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
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5.发明申请
公开(公告)号：WO2018112094A1
公开(公告)日：2018-06-21
申请号：PCT/US2017/066197
申请日：2017-12-13
Applicant: AMGEN INC.
Inventor： ALLEN, Jennifer R. , BOURBEAU, Matthew P. , BROWN, James A. , CHEN, Ning , FROHN, Michael J. , FU, Zice , LIU, Longbin , LIU, Qingyian , PETTUS, Liping H. , QIAN, Wenyuan , REEVES, Corey , SIEGMUND, Aaron C.
IPC: C07D417/10 , C07D417/14 , C07D471/04 , C07D491/056 , C07D498/08 , C07D513/04 , A61P25/28 , A61K31/54
Abstract: The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A, X, R 2 , R 2 ', R 3 , R 4 , R 5 , R 6 , and R 7 of Formula I are defined herein. This disclosure 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, and other central nervous system conditions.
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Patent Agency Ranking
公开(公告)号：WO2009091374A2
公开(公告)日：2009-07-23
申请号：PCT/US2008/011724
申请日：2008-10-14
Applicant: AMGEN INC. , ALBRECHT, Brian K. , BAUER, David , BELLON, Steven , BODE, Christiane M. , BOOKER, Shon , BOEZIO, Alessandro , CHOQUETTE, Deborah , D'AMICO, Erin , HARMANGE, Jean-christophe , HIRAI, Satoko , HUNGATE, Randall W. , KIM, Tae-seong , LEWIS, Richard T. , LIU, Longbin , LOHMAN, Julia , NORMAN, Mark H. , POTASHMAN, Michelle , SIEGMUND, Aaron C. , SPRINGER, Stephanie , STEC, Markian , XI, Ning , YANG, Kevin , PETERSON, Emily, A. , ROMERO, Karina , COPELAND, Katrina, W.
Inventor： ALBRECHT, Brian K. , BAUER, David , BELLON, Steven , BODE, Christiane M. , BOOKER, Shon , BOEZIO, Alessandro , CHOQUETTE, Deborah , D'AMICO, Erin , HARMANGE, Jean-christophe , HIRAI, Satoko , HUNGATE, Randall W. , KIM, Tae-seong , LEWIS, Richard T. , LIU, Longbin , LOHMAN, Julia , NORMAN, Mark H. , POTASHMAN, Michelle , SIEGMUND, Aaron C. , SPRINGER, Stephanie , STEC, Markian , XI, Ning , YANG, Kevin , PETERSON, Emily, A. , ROMERO, Karina , COPELAND, Katrina, W.
IPC: C07D471/04 , C07D487/04 , C07D493/04 , C07D495/04 , C07D498/04 , A61K31/4355
CPC classification number: A61K31/538 , A61K31/437 , A61K31/497 , A61K31/5025 , A61K31/506 , A61K31/52 , A61K31/5377 , A61K45/06 , C07D403/12 , C07D471/04 , C07D473/34 , C07D487/04 , C07D493/04 , C07D495/04 , C07D498/04 , C07D519/00
Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF 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HGF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。
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7.发明申请
公开(公告)号：WO2020050890A3
公开(公告)日：2020-03-12
申请号：PCT/US2019/036626
申请日：2019-06-11
Applicant: AMGEN INC.
Inventor： ALLEN, John Gordon , LANMAN, Brian Alan , CHEN, Jian , REED, Anthony B. , CEE, Victor J. , LIU, Longbin , LOPEZ, Patricia , WURZ, Ryan Paul , NGUYEN, Thomas T. , BOOKER, Shon , ALLEN, Jennifer Rebecca , CHU-MOYER, Margaret , AMEGADZIE, Albert , CHEN, Ning , GOODMAN, Clifford , LOW, Jonathan D. , MA, Vu Van , MINATTI, Ana Elena , NISHIMURA, Nobuko , PICKRELL, Alexander J. , WANG, Hui-Ling , SHIN, Youngsook , SIEGMUND, Aaron C. , YANG, Kevin C. , TAMAYO, Nuria A. , WALTON, Mary , XUE, Qiufen
IPC: C07D471/04 , C07D487/04 , A61K31/519 , A61K31/551 , A61P35/00 , A61K45/06
Abstract: Provided herein are KRAS G12C inhibitors, such as [Insert Compound Here] composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
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公开(公告)号：WO2019241157A1
公开(公告)日：2019-12-19
申请号：PCT/US2019/036397
申请日：2019-06-10
Applicant: AMGEN INC.
Inventor： CHEN, Jian , TAMAYO, Nuria A. , LIU, Longbin , WANG, Hui-Ling , LANMAN, Brian Alan , WURZ, Ryan Paul , SHIN, Youngsook , CEE, Victor J.
IPC: C07D471/04 , A61K31/4375 , A61P35/00
Abstract: Provided herein are KRAS G12C inhibitors, such as composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
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公开(公告)号：WO2018217651A1
公开(公告)日：2018-11-29
申请号：PCT/US2018/033714
申请日：2018-05-21
Applicant: AMGEN INC.
Inventor： LANMAN, Brian Alan , CHEN, Jian , REED, Anthony B. , CEE, Victor J. , LIU, Longbin , KOPECKY, David John , LOPEZ, Patricia , WURZ, Ryan Paul , NGUYEN, Thomas T. , BOOKER, Shon , NISHIMURA, Nobuko , SHIN, Youngsook , TAMAYO, Nuria A. , ALLEN, John Gordon , ALLEN, Jennifer Rebecca
IPC: C07D471/04 , A61K31/519 , A61P35/00 , C07D475/00
Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
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10.发明申请
公开(公告)号：WO2013123444A1
公开(公告)日：2013-08-22
申请号：PCT/US2013/026508
申请日：2013-02-15
Applicant: AMGEN INC.
Inventor： ASHTON, Kate , BOURBEAU, Matthew, Paul , HONG, Fang-Tsao , LIU, Longbin , NISHIMURA, Nobuko , NORMAN, Mark, H. , POON, Steve, F. , STEC, Markian, M. , ST. JEAN, David, J., JR , TAMAYO, Nuria, A. , YANG, Kevin, C.
IPC: C07D403/12 , C07D401/14 , A61K31/44 , A61K31/496 , A61K31/505 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D403/14 , C07D213/52 , A61P3/08
CPC classification number: C07D403/12 , C07D213/52 , C07D213/71 , C07D213/73 , C07D401/12 , C07D401/14 , C07D405/14 , C07D407/12 , C07D407/14 , C07D417/12
Abstract: The present invention relates to sulfonyl compounds that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
Abstract translation: 本发明涉及与葡萄糖激酶调节蛋白相互作用的磺酰化合物。 此外，本发明还涉及治疗2型糖尿病的方法，以及使用该化合物或其药学上可接受的盐涉及葡萄糖激酶调节蛋白的其它疾病和/或病症，以及含有该化合物或其药学上可接受的盐的药物组合物 它们。
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