公开(公告)号：US20170210756A1

公开(公告)日：2017-07-27

申请号：US15227527

申请日：2016-08-03

Applicant: Gilead Sciences, Inc.

Inventor： Amy Cagulada ,  Johann Chan ,  Lina Chan ,  Denise A. Colby ,  Kapil Kumar Karki ,  Darryl Kato ,  Katie Ann Keaton ,  Sudha Kondapally ,  Christopher Levins ,  Adam Littke ,  Ruben Martinez ,  Dominika Pcion ,  Troy Reynolds ,  Bruce Ross ,  Michael Sangi ,  Adam J. Schrier ,  Pamela Seng ,  Dustin Siegel ,  Nathan Shapiro ,  Donald Tang ,  James G. Taylor ,  Jonathan Tripp ,  Andrew W. Waltman ,  Lawrence Yu

IPC: C07D498/18 ,  C07C271/34 ,  C07C255/61 ,  C07C205/57 ,  C07C233/09 ,  C07C251/12 ,  C07D403/12 ,  C07D241/44

CPC classification number: C07D498/18 ,  C07C51/09 ,  C07C205/57 ,  C07C209/00 ,  C07C227/02 ,  C07C233/09 ,  C07C251/12 ,  C07C255/61 ,  C07C271/34 ,  C07C2601/02 ,  C07D241/44 ,  C07D403/12 ,  C07D453/02 ,  C07D498/16 ,  C07K5/0808

Abstract: The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

公开(公告)号：US09029534B2

公开(公告)日：2015-05-12

申请号：US14154313

申请日：2014-01-14

Applicant: Gilead Sciences, Inc.

Inventor： Denise A. Colby ,  Andrew Anthony Martins ,  Benjamin James Roberts ,  Robert William Scott ,  Nicole S. White

IPC: C07F9/06 ,  C07F9/6558 ,  C07F9/6561

CPC classification number: C07F9/65616 ,  C07F9/6512 ,  C07F9/65583

Abstract: Methods for isolating 9-{(R)-2-[((S)—{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine (compound 16): a method for preparing, in high diastereomeric purity, intermediate compounds 13 and 15: and a method for preparing intermediate compound 12: 9-{(R)-2-[((S)—{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine has anti-viral properties.

Abstract translation: 分离9 - {（R）-2 - [（（S） - {[（S）-1-（异丙氧基羰基）乙基]氨基}苯氧基氧膦基）甲氧基]丙基}腺嘌呤（化合物16）的方法： 中间体化合物13和15：和中间体化合物12的制备方法：9 - {（R）-2 - [（（S） - {[（S）-1-（异丙氧基羰基）乙基]氨基} 苯氧基氧膦基）甲氧基]丙基}腺嘌呤具有抗病毒性质。

公开(公告)号：US09676804B2

公开(公告)日：2017-06-13

申请号：US15135357

申请日：2016-04-21

Applicant: Gilead Sciences, Inc.

Inventor： Denise A. Colby ,  Andrew Anthony Martins ,  Benjamin James Roberts ,  Robert William Scott ,  Nicole S. White

IPC: C07F9/6561

CPC classification number: C07F9/65616 ,  C07F9/6512 ,  C07F9/65583

Abstract: Methods for isolating 9-{(R)-2-[((S)—{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine (compound 16): a method for preparing in high diastereomeric purity, intermediate compounds 13 and 15: and a method for preparing intermediate compound 12: 9-{(R)-2-[((S)—{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine has anti-viral properties.

公开(公告)号：US20150291638A1

公开(公告)日：2015-10-15

申请号：US14681955

申请日：2015-04-08

Applicant: Gilead Sciences, Inc.

Inventor： Denise A. Colby ,  Andrew Anthony Martins ,  Benjamin James Roberts ,  Robert William Scott ,  Nicole S. White

IPC: C07F9/6512

CPC classification number: C07F9/65616 ,  C07F9/6512 ,  C07F9/65583

Abstract: Methods for isolating 9-{(R)-2-[((S)-{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine (compound 16): a method for preparing, in high diastereomeric purity, intermediate compounds 13 and 15: and a method for preparing intermediate compound 12: 9-{(R)-2-[((S)-{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine has anti-viral properties.

Abstract translation: 分离9 - {（R）-2 - [（（S） - {[（S）-1-（异丙氧基羰基）乙基]氨基}苯氧基氧膦基）甲氧基]丙基}腺嘌呤（化合物16）的方法： 中间体化合物13和15：和中间体化合物12的制备方法：9 - {（R）-2 - [（（S） - {[（S）-1-（异丙氧基羰基）乙基]氨基} 苯氧基氧膦基）甲氧基]丙基}腺嘌呤具有抗病毒性质。

公开(公告)号：US09440991B2

公开(公告)日：2016-09-13

申请号：US14576143

申请日：2014-12-18

Applicant: GILEAD SCIENCES, INC.

Inventor： Amy Cagulada ,  Johann Chan ,  Lina Chan ,  Denise A. Colby ,  Kapil Kumar Karki ,  Darryl Kato ,  Katie Ann Keaton ,  Sudha Kondapally ,  Chris Levins ,  Adam Littke ,  Ruben Martinez ,  Dominika Pcion ,  Troy Reynolds ,  Bruce Ross ,  Michael Sangi ,  Adam J. Schrier ,  Pamela Seng ,  Dustin Siegel ,  Nathan Shapiro ,  Donald Tang ,  James G. Taylor ,  Jonathan Tripp ,  Andrew W. Waltman ,  Lawrence Yu

IPC: C07D403/12 ,  C07D413/14 ,  C07D498/16 ,  C07C227/02 ,  C07D453/02 ,  C07C209/00 ,  C07C51/09 ,  C07K5/083

CPC classification number: C07D498/18 ,  C07C51/09 ,  C07C205/57 ,  C07C209/00 ,  C07C227/02 ,  C07C233/09 ,  C07C251/12 ,  C07C255/61 ,  C07C271/34 ,  C07C2601/02 ,  C07D241/44 ,  C07D403/12 ,  C07D453/02 ,  C07D498/16 ,  C07K5/0808

Abstract: The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

公开(公告)号：US09346841B2

公开(公告)日：2016-05-24

申请号：US14681955

申请日：2015-04-08

Applicant: Gilead Sciences, Inc.

Inventor： Denise A. Colby ,  Andrew Anthony Martins ,  Benjamin James Roberts ,  Robert William Scott ,  Nicole S. White

IPC: C07F9/6512 ,  C07F9/6561 ,  C07F9/6558

CPC classification number: C07F9/65616 ,  C07F9/6512 ,  C07F9/65583

Abstract: Methods for isolating 9-{(R)-2-[((S)-{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine (compound 16): a method for preparing, in high diastereomeric purity, intermediate compounds 13 and 15: and a method for preparing intermediate compound 12: 9-{(R)-2-[((S)-{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine has anti-viral properties.

公开(公告)号：US10030033B2

公开(公告)日：2018-07-24

申请号：US15227527

申请日：2016-08-03

Applicant: Gilead Sciences, Inc.

Inventor： Amy Cagulada ,  Johann Chan ,  Lina Chan ,  Denise A. Colby ,  Kapil Kumar Karki ,  Darryl Kato ,  Katie Ann Keaton ,  Sudha Kondappally ,  Chris Levins ,  Adam Littke ,  Ruben Martinez ,  Dominika Pcion ,  Troy Reynolds ,  Bruce Ross ,  Michael Sangi ,  Adam J. Schrier ,  Pamela Seng ,  Dustin Siegel ,  Nathan Shapiro ,  Donald Tang ,  James G. Taylor ,  Jonathan Tripp ,  Andrew W. Waltman ,  Lawrence Yu

IPC: C07D498/16 ,  C07D403/12 ,  C07D498/18 ,  C07C271/34 ,  C07D241/44 ,  C07C205/57 ,  C07C233/09 ,  C07C251/12 ,  C07C255/61

Abstract: The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

公开(公告)号：US20140128602A1

公开(公告)日：2014-05-08

申请号：US14154313

申请日：2014-01-14

Applicant: Gilead Sciences, Inc.

Inventor： Denise A. Colby ,  Andrew Anthony Martins ,  Benjamin James Roberts ,  Robert William Scott ,  Nicole S. White

IPC: C07F9/6558

CPC classification number: C07F9/65616 ,  C07F9/6512 ,  C07F9/65583

Abstract: Methods for isolating 9-{(R)-2-[((S)—{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine (compound 16): a method for preparing, in high diastereomeric purity, intermediate compounds 13 and 15: and a method for preparing intermediate compound 12: 9-{(R)-2-[((S)—{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine has anti-viral properties.

Abstract translation: 分离9 - {（R）-2 - [（（S） - {[（S）-1-（异丙氧基羰基）乙基]氨基}苯氧基氧膦基）甲氧基]丙基}腺嘌呤（化合物16）的方法： 中间体化合物13和15：和中间体化合物12的制备方法：9 - {（R）-2 - [（（S） - {[（S）-1-（异丙氧基羰基）乙基]氨基} 苯氧基氧膦基）甲氧基]丙基}腺嘌呤具有抗病毒性质。

公开(公告)号：US08664386B2

公开(公告)日：2014-03-04

申请号：US13573666

申请日：2012-10-03

Applicant: Gilead Sciences, Inc.

Inventor： Denise A. Colby ,  Andrew Anthony Martins ,  Benjamin James Roberts ,  Robert William Scott ,  Nicole S. White

IPC: C07F9/06

CPC classification number: C07F9/65616 ,  C07F9/6512 ,  C07F9/65583

Abstract: Methods for isolating 9-{(R)-2-[((S)-{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine (compound 16): a method for preparing, in high diastereomeric purity, intermediate compounds 13 and 15: and a method for preparing intermediate compound 12: 9-{(R)-2-[((S)-{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine has anti-viral properties.

Abstract translation: 分离9 - {（R）-2 - [（（S） - {[（S）-1-（异丙氧基羰基）乙基]氨基}苯氧基氧膦基）甲氧基]丙基}腺嘌呤（化合物16）的方法： 中间体化合物13和15：和中间体化合物12的制备方法：9 - {（R）-2 - [（（S） - {[（S）-1-（异丙氧基羰基）乙基]氨基} 苯氧基氧膦基）甲氧基]丙基}腺嘌呤具有抗病毒性质。