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公开(公告)号:US20190381064A1
公开(公告)日:2019-12-19
申请号:US16547747
申请日:2019-08-22
Applicant: AMGEN INC.
Inventor: Paul E. HARRINGTON , Kate ASHTON , Sean P. BROWN , Matthew R. KALLER , Todd J. KOHN , Brian Alan LANMAN , Kexue LI , Yunxiao LI , Jonathan D. LOW , Ana Elena MINATTI , Alexander J. PICKRELL , Markian M. STEC , Joshua TAYGERLY
IPC: A61K31/553 , A61P35/02 , A61P35/00 , C07D498/08
Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
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公开(公告)号:US20230159510A1
公开(公告)日:2023-05-25
申请号:US17799077
申请日:2021-02-11
Applicant: AMGEN INC.
Inventor: Jennifer Rebecca ALLEN , Albert AMEGADZIE , Diane Jennifer BEYLKIN , Shon BOOKER , Matthew Paul BOURBEAU , John R. BUTLER , Michael J. FROHN , Sanne Ormholt Schroder GLAD , Birgitte Weinreich HUSEMOEN , Matthew R. KALLER , Todd J. KOHN , Brian Alan LANMAN , Kexue LI , Qingyian LIU , Patricia LOPEZ , Vu Van MA , Francesco MANONI , Jose MEDINA , Ana Elena MINATTI , Jorge PEIRO CADAHIA , Liping PETTUS , Alexander J. PICKRELL , Ian SARVARY , Nuria A. TAMAYO , Mikkel VESTERGAARD
IPC: C07D413/14 , C07D471/04 , C07D401/14 , C07D401/12 , C07D405/14
CPC classification number: C07D413/14 , C07D401/12 , C07D401/14 , C07D405/14 , C07D471/04
Abstract: Described herein are compounds of Formula I and pharmaceutically acceptable salt thereof, stereoisomers, tautomers as well as pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure: (I)
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公开(公告)号:US20170035744A1
公开(公告)日:2017-02-09
申请号:US15298748
申请日:2016-10-20
Applicant: AMGEN INC.
Inventor: Ning CHEN , Xiaoqi CHEN , Yinhong CHEN , Alan C. CHENG , Richard V. CONNORS , Jeffrey DEIGNAN , Paul John DRANSFIELD , Xiaohui DU , Zice FU , Julie Anne HEATH , Daniel HORNE , Jonathan HOUZE , Matthew R. KALLER , Aarif Yusuf KHAKOO , David John KOPECKY , Su-Jen LAI , Zhihua MA , Lawrence R. MCGEE , Julio C. MEDINA , Jeffrey T. MIHALIC , Nobuko NISHIMURA , Steven H. OLSON , Vatee PATTAROPONG , Gayathri SWAMINATH , Xiaodong WANG , Kevin YANG , Wen-Chen YEH , Mikkel V. DEBENEDETTO , Robert P. FARRELL , Simon J. HEDLEY , Ted C. JUDD , Frank KAYSER
IPC: A61K31/4439 , C07D239/30 , C07D241/18 , C07D213/61 , A61K31/695 , A61K31/444 , A61K31/497 , A61K31/437 , A61K31/501 , A61K45/06 , C07C311/13 , C07D241/12 , C07D239/34 , C07D295/16 , A61K31/506 , C07D239/26
CPC classification number: A61K31/506 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07C311/13 , C07D211/54 , C07D213/61 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/18 , C07D241/24 , C07D249/08 , C07D295/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/08
Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
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公开(公告)号:US20140045855A1
公开(公告)日:2014-02-13
申请号:US13958478
申请日:2013-08-02
Applicant: AMGEN INC.
Inventor: Kaustav BISWAS , Jian J. CHEN , Vijay Keshav GORE , Scott HARRIED , Daniel B. HORNE , Matthew R. KALLER , Vu Van MA , Kelvin SHAM , Wenge ZHONG
IPC: C07D491/052 , C07D401/12
CPC classification number: C07D491/052 , C07D215/40 , C07D311/68 , C07D401/12 , C07D471/04 , C07D491/04
Abstract: Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
Abstract translation: 色甘酸化合物和式I的衍生物是TRPM8的有用抑制剂。 这些化合物可用于治疗多种TRPM8介导的病症和病症,并且可用于制备用于治疗这种病症和病症的药物和药物组合物。 这些疾病的实例包括但不限于偏头痛和神经性疼痛。 式I的化合物具有以下结构:其中本文提供变量的定义。
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公开(公告)号:US20180319773A1
公开(公告)日:2018-11-08
申请号:US16033632
申请日:2018-07-12
Applicant: AMGEN INC.
Inventor: Ning CHEN , Xiaoqi CHEN , Yinhong CHEN , Alan C. CHENG , Richard V. CONNORS , Jeffrey DEIGNAN , Paul John DRANSFIELD , Xiaohui DU , Zice FU , Julie Anne HEATH , Daniel B. HORNE , Jonathan HOUZE , Matthew R. KALLER , Aarif Yusuf KHAKOO , David John KOPECKY , Su-Jen LAI , Zhihua MA , Lawrence R. MCGEE , Julio C. MEDINA , Jeffrey T. MIHALIC , Nobuko NISHIMURA , Steven H. OLSON , Vatee PATTAROPONG , Gayathri SWAMINATH , Xiaodong WANG , Kevin YANG , Wen-Chen YEH , Mikkel V. DEBENEDETTO , Robert P. FARRELL , Simon J. HEDLEY , Ted C. JUDD , Frank KAYSER
IPC: C07D401/14 , C07D401/12 , A61K31/437 , C07D417/14 , A61K45/06 , C07B57/00 , C07B59/00 , C07D211/54 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D241/12 , C07D241/24 , C07D249/08 , C07D471/04 , C07D413/14 , C07D413/04 , C07D401/04 , C07D213/61 , C07D239/34 , C07D241/18 , C07F7/08 , C07D295/16 , C07C311/13 , A61K31/695 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , C07D405/14
CPC classification number: C07D401/14 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07C311/13 , C07D211/54 , C07D213/61 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/18 , C07D241/24 , C07D249/08 , C07D295/16 , C07D401/04 , C07D401/12 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/08
Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
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公开(公告)号:US20170281625A1
公开(公告)日:2017-10-05
申请号:US15629567
申请日:2017-06-21
Applicant: AMGEN INC.
Inventor: Ning Chen , Xiaoqi CHEN , Yinhong CHEN , Zice FU , Julie Anne HEATH , Daniel B. HORNE , Matthew R. KALLER , Aarif Yusuf KHAKOO , David John KOPECKY , Zhihua MA , Jeffrey T. MIHALIC , Gayathri SWAMINATH , Xiaodong WANG , Wen-Chen YEH
IPC: A61K31/506 , A61K45/06 , A61K31/497
CPC classification number: A61K31/506 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07C311/13 , C07D211/54 , C07D213/61 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/18 , C07D241/24 , C07D249/08 , C07D295/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/08
Abstract: Methods of treating heart failure include administering to a subject having heart failure an effective amount of a triazole compound that is an agonist of the APJ receptor, a pharmaceutically acceptable salt of the compound, or a mixture thereof. Compounds particularly useful in such methods are provided herein.
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公开(公告)号:US20170044131A1
公开(公告)日:2017-02-16
申请号:US15298434
申请日:2016-10-20
Applicant: AMGEN INC.
Inventor: Ning CHEN , Xiaoqi CHEN , Yinhong CHEN , Alan C. CHENG , Richard V. CONNORS , Jeffrey DEIGNAN , Paul John DRANSFIELD , Xiaohui DU , Zice FU , Julie Anne HEATH , Daniel B. HORNE , Jonathan HOUZE , Matthew R. KALLER , Aarif Yusuf KHAKOO , David John KOPECKY , Su-Jen LAI , Zhihua MA , Lawrence R. MCGEE , Julio C. MEDINA , Jeffrey T. MIHALIC , Nobuko NISHIMURA , Steven H. OLSON , Vatee PATTAROPONG , Gayathri SWAMINATH , Xiaodong WANG , Kevin YANG , Wen-Chen YEH , Mikkel V. DEBENEDETTO , Robert P. FARRELL , Simon J. HEDLEY , Ted C. JUDD , Frank KAYSER
IPC: C07D401/04 , A61K45/06 , C07D401/14 , A61K31/506 , C07D417/14 , A61K31/444 , A61K31/497 , A61K31/513 , C07D471/04 , A61K31/4439 , C07D413/14
CPC classification number: A61K31/506 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07C311/13 , C07D211/54 , C07D213/61 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/18 , C07D241/24 , C07D249/08 , C07D295/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/08
Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
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公开(公告)号:US20200171043A1
公开(公告)日:2020-06-04
申请号:US16783269
申请日:2020-02-06
Applicant: AMGEN INC.
Inventor: Paul E. HARRINGTON , Kate ASHTON , Sean P. BROWN , Matthew R. KALLER , Todd J. KOHN , Brian Alan LANMAN , Kexue LI , Yunxiao LI , Jonathan D. LOW , Ana Elena MINATTI , Alexander J. PICKRELL , Markian M. STEC , Joshua TAYGERLY
IPC: A61K31/553 , C07D498/08 , A61P35/00 , A61P35/02
Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
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公开(公告)号:US20170042872A1
公开(公告)日:2017-02-16
申请号:US15297940
申请日:2016-10-19
Applicant: AMGEN INC.
Inventor: Ning CHEN , Xiaoqi CHEN , Yinhong CHEN , Alan C. CHENG , Richard V. CONNORS , Jeffrey DEIGNAN , Paul John DRANSFIELD , Xiaohui DU , Zice FU , Julie Anne HEATH , Daniel B. HORNE , Jonathan HOUZE , Matthew R. KALLER , Aarif Yusuf KHAKOO , David John KOPECKY , Su-Jen LAI , Zhihua Ma , Lawrence R. MCGEE , Julio C. MEDINA , Jeffrey T. MIHALIC , Nobuko NISHIMURA , Steven H. OLSON , Vatee PATTAROPONG , Gayathri SWAMINATH , Xiaodong WANG , Kevin YANG , Wen-Chen YEH , Mikkel V. DEBENEDETTO , Robert P. FARRELL , Simon J. HEDLEY , Ted C. Judd , Frank KAYSER
IPC: A61K31/4439 , A61K31/695 , A61K31/501 , A61K31/497 , A61K31/444 , A61K45/06 , A61K31/506
CPC classification number: A61K31/506 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07C311/13 , C07D211/54 , C07D213/61 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/18 , C07D241/24 , C07D249/08 , C07D295/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/08
Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
Abstract translation: 其中在这里提供变量的定义。
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公开(公告)号:US20170042871A1
公开(公告)日:2017-02-16
申请号:US15297487
申请日:2016-10-19
Applicant: AMGEN INC.
Inventor: Ning Chen , Xiaoqi CHEN , Yinhong CHEN , Alan C. CHENG , Richard V. CONNORS , Jeffrey DEIGNAN , Paul John DRANSFIELD , Xiaohui DU , Zice FU , Julie Anne HEATH , Daniel B. HORNE , Jonathan HOUZE , Matthew R. KALLER , Aarif Yusuf KHAKOO , David John KOPECKY , Su-Jen LAI , Zhihua MA , Lawrence R. MCGEE , Julio C. MEDINA , Jeffrey T. MIHALIC , Nobuko NISHIMURA , Steven H. OLSON , Vatee PATTAROPONG , Gayathri SWAMINATH , Xiaodong WANG , Kevin YANG , Wen-Chen YEH , Mikkel V. DEBENEDETTO , Robert P. FARRELL , Simon J. HEDLEY , Ted C. JUDD , Frank KAYSER
IPC: A61K31/4439 , A61K31/501 , A61K31/444 , A61K31/506 , A61K31/497
CPC classification number: A61K31/506 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/513 , A61K31/695 , A61K45/06 , C07B57/00 , C07B59/002 , C07B2200/05 , C07B2200/07 , C07C311/13 , C07D211/54 , C07D213/61 , C07D213/71 , C07D213/82 , C07D239/26 , C07D239/30 , C07D239/34 , C07D241/12 , C07D241/18 , C07D241/24 , C07D249/08 , C07D295/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07F7/08
Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
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