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公开(公告)号：WO2018145021A1
公开(公告)日：2018-08-09
申请号：PCT/US2018/016893
申请日：2018-02-05
Applicant: GILEAD SCIENCES, INC.
Inventor： BACON, Elizabeth M. , CHIN, Elbert , COTTELL, Jeromy J. , KATANA, Ashley Anne , KATO, Darryl , LINK, John O. , SHAPIRO, Nathan , TREJO MARTIN, Teresa Alejandra , YANG, Zheng-Yu
IPC: C07D403/12 , C07D405/14 , C07C275/16 , C07D401/12 , C07D471/08 , C07D487/08 , C07D487/10 , C07D491/04 , C07C243/28 , A61K31/495 , A61K31/504 , A61K31/506 , A61K31/5365 , A61K31/4155 , A61K31/337
Abstract: The invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, the compound of formula (I) for use in therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS symptoms in a mammal using compounds of Formula I. Preferred compounds are N-[(2S) -1-[2-[(2S,3S)-2-hydroxy-3-[[(2S)-2-(methoxycarbonylamino) -3,3-dimethylbutanoyl]amino]-4-phenylbutyl]-2-[(phenyl) methyl]hydrazinyl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate atazanavir (ATV) analogues substituted by several heterocycles, such as e.g. pyrazole (Rl); e.g. oxetane (substituent of X2); e.g. pyridine or pyrimidine (X1); e.g. piperazine or 3,8-diazabicyclo[3.2.1]octan (X2).
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公开(公告)号：WO2022109182A1
公开(公告)日：2022-05-27
申请号：PCT/US2021/059960
申请日：2021-11-18
Applicant: GILEAD SCIENCES, INC.
Inventor： BRIZGYS, Gediminas J. , CASSIDY, James S. , CHOU, Chienhung , COTTELL, Jeromy J. , HUNG, Chao-I , KOLAHDOUZAN, Kavoos , TAYLOR, James G. , WRIGHT, Nathan E. , YANG, Zheng-Yu
IPC: C07D401/14 , C07D401/12 , C07D405/14 , A61K31/4545 , A61P1/16 , A61P3/00 , A61P9/00 , A61P25/00 , A61K45/06
Abstract: The present disclosure provides glucagon-like peptide-1 receptor (GLP-1R) agonists of Formula (l-A), as well as pharmaceutical compositions and therapeutic uses thereof. The compounds are generally useful for treating a GLP-1R mediated disease or condition in a human such as non-alcoholic steatohepatitis (NASH), obesity or type 2 diabetes.
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公开(公告)号：WO2022225941A1
公开(公告)日：2022-10-27
申请号：PCT/US2022/025364
申请日：2022-04-19
Applicant: GILEAD SCIENCES, INC.
Inventor： ARMSTRONG, Megan K. , CASSIDY, James S. , CHIN, Elbert , CHOU, Chienhung , COTTELL, Jeromy J. , HUNG, Chao-I , KOLAHDOUZAN, Kavoos , LIN, David W. , MITCHELL, Michael L. , ROBERTS, Ezra , SCHROEDER, Scott D. , SHAPIRO, Nathan D. , TAYLOR, James G. , THOMAS-TRAN, Rhiannon , WRIGHT, Nathan E. , YANG, Zheng-Yu
IPC: C07D401/10 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D491/048 , C07D493/04 , C07D493/08 , C07D493/10 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61P1/16 , A61P3/04 , A61P3/10
Abstract: The present disclosure provides GLP-1R agonists, and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition in a human.
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公开(公告)号：WO2020036986A1
公开(公告)日：2020-02-20
申请号：PCT/US2019/046391
申请日：2019-08-13
Applicant: GILEAD SCIENCES, INC.
Inventor： AMMANN, Stephen , BACON, Elizabeth M. , BRIZGYS, Gediminas , CHIN, Elbert , CHOU, Chienhung , COTTELL, Jeromy J. , NDUKWE, Marilyn , SHATSKIKH, Marina , TAYLOR, James G. , WRIGHT, Nathan E. , YANG, Zheng-Yu , ZIPFEL, Sheila M.
IPC: C07D487/04 , A61P29/00 , A61K31/5025
Abstract: A compound of Formula (I): (I) pharmaceutically acceptable salts thereof, deuterated analogs thereof, compositions thereof, and methods of treating disease using a compound thereof are disclosed.
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公开(公告)号：WO2014100500A1
公开(公告)日：2014-06-26
申请号：PCT/US2013/076734
申请日：2013-12-19
Applicant: GILEAD SCIENCES, INC.
IPC: C07D491/04 , A61K31/4188 , A61P31/12
CPC classification number: C07D491/052 , A61K31/352 , A61K31/4188 , A61K31/7056 , A61K31/7068 , A61K31/7072 , A61K38/21 , A61K45/06 , C07D491/04
Abstract: The disclosure is related to compounds having a polycyclic core and at least one 2,6-dimethyltetrahydro-2H-pyran-4-yl, 4- methyltetrahydro-2H-pyran-4-yl, or tetrahydro-2H-pyran-3-yl capping group, which compounds are provided for use in pharmaceutical compositions and methods for treating hepatitis C (HCV).
Abstract translation: 本公开涉及具有多环核心和至少一个2,6-二甲基四氢-2H-吡喃-4-基，4-甲基四氢-2H-吡喃-4-基或四氢-2H-吡喃-3-基的四氢-2H-吡喃-3-基 封端组，其提供用于药物组合物和治疗丙型肝炎（HCV）的方法。
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Patent Agency Ranking
公开(公告)号：WO2021154796A1
公开(公告)日：2021-08-05
申请号：PCT/US2021/015197
申请日：2021-01-27
Applicant: GILEAD SCIENCES, INC.
Inventor： AMMANN, Stephen , BRIZGYS, Gediminas , CASSIDY, James S. , CHIN, Elbert , CHOU, Chienhung , COTTELL, Jeromy J. , HUNG, Chao-I , KOLAHDOUZAN, Kavoos , SHORE, Daniel G. , SZEWCZYK, Suzanne M. , TAYLOR, James G. , THOMAS-TRAN, Rhiannon , WRIGHT, Nathan E. , YANG, Zheng-Yu
IPC: C07D405/10 , C07D405/14 , C07D409/14 , C07D493/04 , C07D498/04 , A61K31/4184 , A61K31/4439 , A61P1/16 , A61P3/04 , A61P3/10 , A61P9/00 , A61P13/12 , A61P19/02 , A61P25/16
Abstract: The present disclosure provides GLP-1R agonists, and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition.
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公开(公告)号：WO2021081207A1
公开(公告)日：2021-04-29
申请号：PCT/US2020/056867
申请日：2020-10-22
Applicant: GILEAD SCIENCES, INC.
Inventor： AMMANN, Stephen E. , BRIZGYS, Gediminas J. , CASSIDY, James S. , CHIN, Elbert , CHOU, Chienhung , COTTELL, Jeromy J. , GRAUPE, Michael , HUNG, Chao-I , KOLAHDOUZAN, Kavoos , SCHROEDER, Scott D. , SHAPIRO, Nathan D. , SHORE, Daniel G. , SZEWCZYK, Suzanne M. , TAYLOR, James G. , THOMAS-TRAN, Rhiannon , WRIGHT, Nathan E. , YANG, Zheng-Yu , ZIPFEL, Sheila M.
IPC: C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D405/14 , C07D413/14 , C07D417/10 , C07D417/14 , C07D471/04 , C07D471/10 , C07D493/10 , A61P3/10 , A61K31/4427
Abstract: The present disclosure provides GLP-1R agonists, and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition in a human.
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公开(公告)号：WO2020014468A1
公开(公告)日：2020-01-16
申请号：PCT/US2019/041382
申请日：2019-07-11
Applicant: GILEAD SCIENCES, INC.
Inventor： AMMANN, Stephen , BACON, Elizabeth M. , BRIZGYS, Gediminas , CHIN, Elbert , CHOU, Chienhung , COTTELL, Jeromy J. , NDUKWE, Marilyn , TAYLOR, James G. , WRIGHT, Nathan E. , YANG, Zheng-YU , ZIPFEL, Sheila M.
IPC: C07D487/04 , A61P17/06 , A61K31/5025
Abstract: A compound of Formula (I): (I) pharmaceutically acceptable salts thereof, deuterated analogs thereof, compositions thereof, and methods of treating disease using a compound thereof, wherein the variable substituents are disclosed herein.
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公开(公告)号：WO2013173488A1
公开(公告)日：2013-11-21
申请号：PCT/US2013/041201
申请日：2013-05-15
Applicant: GILEAD SCIENCES, INC.
IPC: C07D491/052 , A61K31/4188
CPC classification number: C07D491/052 , A61K31/4188 , A61K31/7056 , A61K31/7068 , A61K31/7072 , A61K38/21 , A61K45/06 , C07D491/04 , A61K2300/00
Abstract: The disclosure is related to anti-viral compounds of formula (I), compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
Abstract translation: 本公开涉及式（I）的抗病毒化合物，含有这些化合物的组合物和包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。
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公开(公告)号：WO2022192430A1
公开(公告)日：2022-09-15
申请号：PCT/US2022/019596
申请日：2022-03-09
Applicant: GILEAD SCIENCES, INC.
Inventor： BRIZGYS, Gediminas J. , CHOU, Chienhung , COTTELL, Jeromy J. , HUNG, Chao-I , MITCHELL, Michael L. , SCHROEDER, Scott D. , SHAPIRO, Nathan D. , SZEWCZYK, Suzanne M. , TAYLOR, James G. , WRIGHT, Nathan E. , ZIPFEL, Sheila M.
IPC: A61P1/00 , A61P5/00 , A61P9/00 , A61P19/00 , A61P25/00 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , A61K31/4184
Abstract: The present disclosure provides GLP-1R agonists of formula (I), and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition in a human.
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