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：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：US20160347719A1

公开(公告)日：2016-12-01

申请号：US15231411

申请日：2016-08-08

Applicant: Gilead Sciences, Inc.

Inventor： 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: C07D239/42

CPC classification number: C07D239/42 ,  A61K31/535 ,  A61K31/5377 ,  C07B2200/13 ,  C07D265/30

Abstract: 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

Applicant: Gilead Sciences, Inc.

Inventor： 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: A61K31/535 ,  C07D265/30 ,  C07D239/42 ,  A61K31/5377

CPC classification number: C07D239/42 ,  A61K31/535 ,  A61K31/5377 ,  C07B2200/13 ,  C07D265/30

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20200277293A1

公开(公告)日：2020-09-03

申请号：US16641331

申请日：2018-08-10

Applicant: Gilead Sciences, Inc.

Inventor： Tim G. Elford ,  Peter Chee-Chu Fung ,  Paul Robert Hartmeier ,  Jesper Alexis Jernelius ,  Henry Morrison

IPC: C07D487/04

Abstract: Polymorphs of a bis-mesylate salt of a compound of Formula I: are provided.

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：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：US20210024537A1

公开(公告)日：2021-01-28

申请号：US16924924

申请日：2020-07-09

Applicant: Gilead Sciences, Inc.

Inventor： Michael Geier ,  Luke Humphreys ,  Norihiro Ikemoto ,  Sean Liew ,  Henry Morrison ,  Mark E. Scott ,  Vimal Varghese

IPC: C07D495/04 ,  C07D309/12 ,  C07D493/10 ,  A61P3/00 ,  C12P7/42

Abstract: The present disclosure provides solid forms, including a salt or co-crystal, of Compound I: which exhibits Acetyl-CoA carboxylase (“ACC”) inhibitory activity and may be useful in treating ACC mediated diseases. Also provided herein are processes or steps for the preparation of a Compound I and intermediates useful for the processes or steps described herein.

公开(公告)号：US20180298025A1

公开(公告)日：2018-10-18

申请号：US15910744

申请日：2018-03-02

Applicant: Gilead Sciences, Inc.

Inventor： Michael Geier ,  Luke Humphreys ,  Norihiro Ikemoto ,  Sean Liew ,  Henry Morrison ,  Mark E. Scott ,  Vimal Varghese

IPC: C07D495/04 ,  C07D309/12 ,  C12P7/42 ,  C07D493/10

Abstract: The present disclosure provides solid forms, including a salt or co-crystal, of Compound I: which exhibits Acetyl-CoA carboxylase (“ACC”) inhibitory activity and may be useful in treating ACC mediated diseases. Also provided herein are processes or steps for the preparation of a Compound I and intermediates useful for the processes or steps described herein.

公开(公告)号：US09809559B2

公开(公告)日：2017-11-07

申请号：US15231411

申请日：2016-08-08

Applicant: Gilead Sciences, Inc.

Inventor： 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: A61K31/535 ,  A61K31/5377 ,  C07D239/42 ,  C07D265/30

CPC classification number: C07D239/42 ,  A61K31/535 ,  A61K31/5377 ,  C07B2200/13 ,  C07D265/30

Abstract: 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.