公开(公告)号：US10030033B2

公开(公告)日：2018-07-24

申请号：US15227527

申请日：2016-08-03

申请人： Gilead Sciences, Inc.

发明人： 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分类号： C07D498/16 ,  C07D403/12 ,  C07D498/18 ,  C07C271/34 ,  C07D241/44 ,  C07C205/57 ,  C07C233/09 ,  C07C251/12 ,  C07C255/61

摘要： 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：US20170210756A1

公开(公告)日：2017-07-27

申请号：US15227527

申请日：2016-08-03

申请人： Gilead Sciences, Inc.

发明人： 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分类号： C07D498/18 ,  C07C271/34 ,  C07C255/61 ,  C07C205/57 ,  C07C233/09 ,  C07C251/12 ,  C07D403/12 ,  C07D241/44

CPC分类号： 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

摘要： 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：US09440991B2

公开(公告)日：2016-09-13

申请号：US14576143

申请日：2014-12-18

申请人： GILEAD SCIENCES, INC.

发明人： 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分类号： C07D403/12 ,  C07D413/14 ,  C07D498/16 ,  C07C227/02 ,  C07D453/02 ,  C07C209/00 ,  C07C51/09 ,  C07K5/083

CPC分类号： 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

摘要： 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：US09809559B2

公开(公告)日：2017-11-07

申请号：US15231411

申请日：2016-08-08

申请人： Gilead Sciences, Inc.

发明人： Brandon H. Brown ,  Ernest A. Carra ,  Jeffrey N. Hemenway ,  Henry Morrison ,  Troy Reynolds ,  Bing Shi ,  Dimitrios Stefanidis ,  Fang Wang ,  Matthew Robert Warr ,  James Andrew Whitney ,  Yan Xin

IPC分类号： A61K31/535 ,  A61K31/5377 ,  C07D239/42 ,  C07D265/30

CPC分类号： C07D239/42 ,  A61K31/535 ,  A61K31/5377 ,  C07B2200/13 ,  C07D265/30

摘要： The present invention relates to stable novel salt forms of N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide that are suitable for the preparation of pharmaceutical formulations thereof, and their therapeutic use.

公开(公告)号：US20150361050A1

公开(公告)日：2015-12-17

申请号：US14736690

申请日：2015-06-11

申请人： Gilead Sciences, Inc.

发明人： Brandon H. Brown ,  Ernest A. Carra ,  Jeffrey N. Hemenway ,  Henry Morrison ,  Troy Reynolds ,  Bing Shi ,  Dimitrios Stefanidis ,  Fang Wang ,  Matthew Robert Warr ,  James Andrew Whitney ,  Yan Xin

IPC分类号： C07D239/42

CPC分类号： C07D239/42 ,  A61K31/535 ,  A61K31/5377 ,  C07B2200/13 ,  C07D265/30

摘要： The present invention relates to stable novel salt forms of N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide that are suitable for the preparation of pharmaceutical formulations thereof, and their therapeutic use.

摘要翻译： 本发明涉及适用于制备其药物制剂的N-（氰基甲基）-4-（2-（4-吗啉代苯基氨基）嘧啶-4-基）苯甲酰胺的稳定的新型盐及其治疗用途。

公开(公告)号：US20180022708A1

公开(公告)日：2018-01-25

申请号：US15680024

申请日：2017-08-17

申请人： Gilead Sciences, Inc.

发明人： Brandon Heath Brown ,  Troy Reynolds

IPC分类号： C07D233/64

CPC分类号： C07D233/64 ,  C07B2200/13 ,  C07D233/56 ,  C07D401/14

摘要： The present disclosure provides processes for the preparation of a compound of formula: which exhibits apoptosis signal-regulating kinase (“ASK1”) inhibitory activity and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis. The disclosure also provides compounds that are synthetic intermediates.

公开(公告)号：US20160347719A1

公开(公告)日：2016-12-01

申请号：US15231411

申请日：2016-08-08

申请人： Gilead Sciences, Inc.

发明人： Brandon H. Brown ,  Ernest A. Carra ,  Jeffrey N. Hemenway ,  Henry Morrison ,  Troy Reynolds ,  Bing Shi ,  Dimitrios Stefanidis ,  Fang Wang ,  Matthew Robert Warr ,  James Andrew Whitney ,  Yan Xin

IPC分类号： C07D239/42

CPC分类号： C07D239/42 ,  A61K31/535 ,  A61K31/5377 ,  C07B2200/13 ,  C07D265/30

摘要： The present invention relates to stable novel salt forms of N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide that are suitable for the preparation of pharmaceutical formulations thereof, and their therapeutic use.

公开(公告)号：US09469613B2

公开(公告)日：2016-10-18

申请号：US14736690

申请日：2015-06-11

申请人： Gilead Sciences, Inc.

发明人： Brandon H. Brown ,  Ernest A. Carra ,  Jeffrey N. Hemenway ,  Henry Morrison ,  Troy Reynolds ,  Bing Shi ,  Dimitrios Stefanidis ,  Fang Wang ,  Matthew Robert Warr ,  James Andrew Whitney ,  Yan Xin

IPC分类号： A61K31/535 ,  C07D265/30 ,  C07D239/42 ,  A61K31/5377

CPC分类号： C07D239/42 ,  A61K31/535 ,  A61K31/5377 ,  C07B2200/13 ,  C07D265/30

摘要： The present invention relates to stable novel salt forms of N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide that are suitable for the preparation of pharmaceutical formulations thereof, and their therapeutic use.

摘要翻译： 本发明涉及适于制备其药物制剂的N-（氰基甲基）-4-（2-（4-吗啉代苯基氨基）嘧啶-4-基）苯甲酰胺的稳定的新型盐及其治疗用途。