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).

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.

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.

Inventor： BACON, Elizabeth M. ,  COTTELL, Jeromy J. ,  LINK, John O. ,  TREJO MARTIN, Teresa Alejandra

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。

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.

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.

Inventor： LINK, John O. ,  COTTELL, Jeromy J. ,  TREJO MARTIN, Teresa Alejandra ,  BACON, Elizabeth M.

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。

公开(公告)号：WO2020036979A1

公开(公告)日：2020-02-20

申请号：PCT/US2019/046380

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 ,  TAYLOR, James G. ,  WRIGHT, Nathan E. ,  YANG, Zheng-Yu ,  ZIPFEL, Sheila M.

IPC: A61P29/00 ,  C07D487/04 ,  A61K31/506

Abstract: A compound of Formula (I) pharmaceutically acceptable salts thereof, deuterated analogs thereof, compositions thereof, and methods of treating disease using a compound thereof are disclosed.

公开(公告)号：WO2020036830A1

公开(公告)日：2020-02-20

申请号：PCT/US2019/046026

申请日：2019-08-09

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 ,  A61K31/5025 ,  A61P29/00

Abstract: A compound of Formula (I), pharmaceutically acceptable salts thereof, deuterated analogs thereof, compositions thereof, and methods of treating disease using a compound thereof are disclosed.

公开(公告)号：WO2015191526A2

公开(公告)日：2015-12-17

申请号：PCT/US2015/034823

申请日：2015-06-09

Applicant: GILEAD SCIENCES, INC.

Inventor： BACON, Elizabeth M. ,  COTTELL, Jeromy J. ,  LINK, John O. ,  TREJO MARTIN, Teresa Alejandra ,  ZIPFEL, Sheila

IPC: C07D493/06

CPC classification number: C07D493/06

Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as to processes and intermediates useful for preparing such compounds.

Abstract translation: 本公开涉及抗病毒化合物，含有这些化合物的组合物，以及包括给予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。

公开(公告)号：WO2013173492A1

公开(公告)日：2013-11-21

申请号：PCT/US2013/041205

申请日：2013-05-15

Applicant: GILEAD SCIENCES, INC.

Inventor： LINK, John O. ,  COTTELL, Jeromy J. ,  TREJO MARTIN, Teresa Alejandra ,  BACON, Elizabeth M.

IPC: C07D403/14 ,  A61K31/4178 ,  A61P31/14

CPC classification number: C07D403/14 ,  A61K31/4178 ,  A61K31/7056 ,  A61K31/7064 ,  A61K31/7072 ,  A61K38/21 ,  A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  A61K2300/00

Abstract: The invention is related to anti-viral compounds, 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: 本发明涉及抗病毒化合物，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。