公开(公告)号：US20170267694A1

公开(公告)日：2017-09-21

申请号：US15387318

申请日：2016-12-21

Applicant: Gilead Sciences, Inc.

Inventor： Dustin Bringley ,  Johann Chan ,  Peter Fung ,  Katie Keaton ,  Olga Lapina ,  Henry Morrison ,  Dominika Pcion

IPC: C07D498/16 ,  A61K45/06 ,  A61K31/4985 ,  C07K5/083

CPC classification number: C07D498/16 ,  A61K31/4985 ,  A61K45/06 ,  C07K5/0808

Abstract: Crystalline forms of the anti-HCV compound (1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.

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：US08877931B2

公开(公告)日：2014-11-04

申请号：US13956905

申请日：2013-08-01

Applicant: Gilead Sciences, Inc.

Inventor： Dominika Pcion ,  Carrie Tomasi ,  Mark Charles Whitcomb ,  Eric D. Dowdy ,  Wenyi Fu ,  Patricia MacLeod

IPC: C07C45/00 ,  C07D215/00 ,  C07C49/84 ,  C07C67/12 ,  C07C43/225 ,  C07D215/56 ,  C07C67/343 ,  C07C45/46 ,  C07C45/30

CPC classification number: C07D215/56 ,  C07C43/225 ,  C07C45/30 ,  C07C45/46 ,  C07C49/84 ,  C07C67/12 ,  C07C67/343 ,  C07C69/738

Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.

公开(公告)号：US09862728B2

公开(公告)日：2018-01-09

申请号：US15387318

申请日：2016-12-21

Applicant: Gilead Sciences, Inc.

Inventor： Dustin Bringley ,  Johann Chan ,  Peter Fung ,  Katie Keaton ,  Olga Lapina ,  Henry Morrison ,  Dominika Pcion

IPC: C07D498/16 ,  C07K5/083 ,  A61K45/06 ,  A61K31/4985

CPC classification number: C07D498/16 ,  A61K31/4985 ,  A61K45/06 ,  C07K5/0808

Abstract: Crystalline forms of the anti-HCV compound (1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.

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：US20150175625A1

公开(公告)日：2015-06-25

申请号：US14575966

申请日：2014-12-18

Applicant: GILEAD SCIENCES, INC.

Inventor： Dustin Bringley ,  Johann Chan ,  Peter Fung ,  Katie Keaton ,  Olga Lapina ,  Henry Morrison ,  Dominika Pcion

IPC: C07D498/16 ,  A61K45/06 ,  A61K31/4985

CPC classification number: C07D498/16 ,  A61K31/4985 ,  A61K45/06 ,  C07K5/0808

Abstract: Crystalline forms of the anti-HCV compound (1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.

Abstract translation: 抗HCV化合物（1aR，5S，8S，9S，10R，22aR）-5-叔丁基-N - [（1R，2R）-2-（二氟甲基）-1 - {[（1- 甲基环丙基）磺酰基]氨基甲酰基}环丙基] -9-乙基-18,18-二氟-14-甲氧基-3,6-二氧代-1,1a，3,4,5,6,9,10,18,19,20 ，21,22,22a-十四氢-8H-7,10-亚甲基环丙烷[18,19] [1,10,3,6]二氧杂二氮杂环十二烷[11,12-b]喹喔啉-8-甲酰胺（化合物I） 其特征在于固态：还提供了制造方法和使用结晶形式的方法。

公开(公告)号：US09562058B2

公开(公告)日：2017-02-07

申请号：US14575966

申请日：2014-12-18

Applicant: GILEAD SCIENCES, INC.

Inventor： Dustin Bringley ,  Johann Chan ,  Peter Fung ,  Katie Keaton ,  Olga Lapina ,  Henry Morrison ,  Dominika Pcion

IPC: A61K31/4985 ,  C07D498/16 ,  A61K45/06 ,  C07K5/083

CPC classification number: C07D498/16 ,  A61K31/4985 ,  A61K45/06 ,  C07K5/0808

Abstract: Crystalline forms of the anti-HCV compound (1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.

Abstract translation: 抗HCV化合物（1aR，5S，8S，9S，10R，22aR）-5-叔丁基-N - [（1R，2R）-2-（二氟甲基）-1 - {[（1- 甲基环丙基）磺酰基]氨基甲酰基}环丙基] -9-乙基-18,18-二氟-14-甲氧基-3,6-二氧代-1,1a，3,4,5,6,9,10,18,19,20 ，21,22,22a-十四氢-8H-7,10-亚甲基环丙烷[18,19] [1,10,3,6]二氧杂二氮杂环十二烷[11,12-b]喹喔啉-8-甲酰胺（化合物I） 其特征在于固态：还提供了制造方法和使用结晶形式的方法。

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.