公开(公告)号：US09918939B2

公开(公告)日：2018-03-20

申请号：US14906248

申请日：2014-07-29

Applicant: Gilead Connecticut, Inc.

Inventor： Melissa Jean Casteel ,  Bei Li ,  Rowchanak Pakdaman ,  Diana Sperger ,  Dimitrios Stefanidis

IPC: A61K31/537 ,  A61K9/20 ,  C07C309/66 ,  C07D487/04 ,  A61K31/5377 ,  A61K47/10 ,  A61K47/38 ,  B29B9/10 ,  B29C43/00 ,  B29C43/02 ,  A61K9/28

CPC classification number: A61K9/2095 ,  A61K9/2027 ,  A61K9/2866 ,  A61K31/5377 ,  A61K47/10 ,  A61K47/38 ,  B29B9/10 ,  B29C43/003 ,  B29C43/02 ,  B29K2995/0056 ,  C07C309/66 ,  C07D487/04

Abstract: Disclosed are pharmaceutical compositions comprising a compound having the formula: or a pharmaceutically acceptable salt thereof, or a hydrate of thereof, and at least one pharmaceutically acceptable polymer. The pharmaceutically acceptable salt of the compound of Formula I, or a hydrate thereof, can be a mesylate salt, including, for example, a mono-mesylate or a bis-mesylate salt, or a hydrate thereof. Also disclosed are methods of use for the pharmaceutical composition.

公开(公告)号：US20170020821A1

公开(公告)日：2017-01-26

申请号：US15178164

申请日：2016-06-09

Applicant: Gilead Connecticut, Inc.

Inventor： Melissa Jean Casteel ,  Bei Li ,  Rowchanak Pakdaman ,  Diana Sperger ,  Dimitrios Stefanidis

IPC: A61K9/20 ,  B29B9/10 ,  B29C43/02 ,  A61K31/5377 ,  B29C43/00

CPC classification number: A61K9/2095 ,  A61K9/2027 ,  A61K9/2866 ,  A61K31/5377 ,  A61K47/10 ,  A61K47/38 ,  B29B9/10 ,  B29C43/003 ,  B29C43/02 ,  B29K2995/0056 ,  C07C309/66 ,  C07D487/04

Abstract: Disclosed are pharmaceutical compositions comprising a compound having the formula: or a pharmaceutically acceptable salt thereof, or a hydrate of thereof, and at least one pharmaceutically acceptable polymer. The pharmaceutically acceptable salt of the compound of Formula I, or a hydrate thereof, can be a mesylate salt, including, for example, a mono-mesylate or a bis-mesylate salt, or a hydrate thereof. Also disclosed are methods of use for the pharmaceutical composition.

Abstract translation: 或其药学上可接受的盐，或其水合物，和至少一种药学上可接受的聚合物。 式I化合物或其水合物的药学上可接受的盐可以是甲磺酸盐，包括例如单甲磺酸酯或双甲磺酸盐或其水合物。 还公开了用于药物组合物的方法。

公开(公告)号：US09949932B2

公开(公告)日：2018-04-24

申请号：US15178164

申请日：2016-06-09

Applicant: Gilead Connecticut, Inc.

Inventor： Melissa Jean Casteel ,  Bei Li ,  Rowchanak Pakdaman ,  Diana Sperger ,  Dimitrios Stefanidis

IPC: C07D487/04 ,  A61K9/00 ,  B01J2/00 ,  B01J2/16 ,  A61K9/20 ,  C07C309/66 ,  A61K31/5377 ,  A61K47/10 ,  A61K47/38 ,  B29B9/10 ,  B29C43/00 ,  B29C43/02 ,  A61K9/28

CPC classification number: A61K9/2095 ,  A61K9/2027 ,  A61K9/2866 ,  A61K31/5377 ,  A61K47/10 ,  A61K47/38 ,  B29B9/10 ,  B29C43/003 ,  B29C43/02 ,  B29K2995/0056 ,  C07C309/66 ,  C07D487/04

Abstract: Disclosed are pharmaceutical compositions comprising a compound having the formula: or a pharmaceutically acceptable salt thereof, or a hydrate of thereof, and at least one pharmaceutically acceptable polymer. The pharmaceutically acceptable salt of the compound of Formula I, or a hydrate thereof, can be a mesylate salt, including, for example, a mono-mesylate or a bis-mesylate salt, or a hydrate thereof. Also disclosed are methods of use for the pharmaceutical composition.

公开(公告)号：US20180099971A1

公开(公告)日：2018-04-12

申请号：US15788583

申请日：2017-10-19

Applicant: Gilead Connecticut, Inc.

Inventor： Tim G. Elford ,  Peter Chee-Chu Fung ,  Michael Laird Hurrey ,  Dimitrios Stefanidis ,  Dragos Vizitiu

IPC: C07D487/04 ,  C07C309/04

CPC classification number: C07D487/04 ,  C07C309/04

Abstract: Polymorphs of a bis-mesylate salt of a compound of Formula I: or a hydrate thereof, are provided. The bis-mesylate salt may also be depicted as a compound of Formula IA: Provided herein are also compositions thereof, methods for their preparation and methods for such polymorphs.

公开(公告)号：US09382256B2

公开(公告)日：2016-07-05

申请号：US14445970

申请日：2014-07-29

Applicant: Gilead Connecticut, Inc.

Inventor： Melissa Jean Casteel ,  Bei Li ,  Rowchanak Pakdaman ,  Diana Sperger ,  Dimitrios Stefanidis

IPC: A61K31/495 ,  C07D487/04 ,  A61K9/20 ,  C07C309/66 ,  A61K31/5377 ,  A61K9/28

CPC classification number: A61K9/2095 ,  A61K9/2027 ,  A61K9/2866 ,  A61K31/5377 ,  A61K47/10 ,  A61K47/38 ,  B29B9/10 ,  B29C43/003 ,  B29C43/02 ,  B29K2995/0056 ,  C07C309/66 ,  C07D487/04

Abstract: Disclosed are pharmaceutical compositions comprising a compound having the formula: or a pharmaceutically acceptable salt thereof, or a hydrate of thereof, and at least one pharmaceutically acceptable polymer. The pharmaceutically acceptable salt of the compound of Formula I, or a hydrate thereof, can be a mesylate salt, including, for example, a mono-mesylate or a bis-mesylate salt, or a hydrate thereof. Also disclosed are methods of use for the pharmaceutical composition.

Abstract translation: 公开了包含具有下式的化合物或其药学上可接受的盐，或其水合物和至少一种药学上可接受的聚合物的药物组合物。 式I化合物或其水合物的药学上可接受的盐可以是甲磺酸盐，包括例如单甲磺酸酯或双甲磺酸盐或其水合物。 还公开了用于药物组合物的方法。

公开(公告)号：US09657023B2

公开(公告)日：2017-05-23

申请号：US14446011

申请日：2014-07-29

Applicant: Gilead Connecticut, Inc.

Inventor： Tim G. Elford ,  Peter Chee-Chu Fung ,  Michael Laird Hurrey ,  Dimitrios Stefanidis ,  Dragos Vizitiu

IPC: C07D487/04 ,  C07C309/04

CPC classification number: C07D487/04 ,  C07C309/04

Abstract: Polymorphs of a bis-mesylate salt of a compound of Formula I: or a hydrate thereof, are provided. The bis-mesylate salt may also be depicted as a compound of Formula IA: Provided herein are also compositions thereof, methods for their preparation and methods for such polymorphs.

公开(公告)号：US20160168155A1

公开(公告)日：2016-06-16

申请号：US14907767

申请日：2014-07-29

Applicant: GILEAD CONNECTICUT, INC.

Inventor： Peter Chee-Chu Fung ,  Dimitrios Stefanidis ,  Dragos Vizitiu ,  Tim G. Elford ,  Michael Laird Hurrey

IPC: C07D487/04

CPC classification number: C07D487/04 ,  C07C309/04

Abstract: Polymorphs of a bis-mesylate salt of a compound of Formula (I): or a hydrate thereof, are provided. The bis-mesylate salt may also be depicted as a compound of Formula (IA): Provided herein are also compositions thereof, methods for their preparation and methods for such polymorphs.

Abstract translation: 提供式（I）化合物的双甲磺酸盐或其水合物的多晶型物。 双甲磺酸盐也可以描述为式（IA）的化合物：本文还提供其组合物，其制备方法和这些多晶型物的方法。

公开(公告)号：US20160166580A1

公开(公告)日：2016-06-16

申请号：US14906248

申请日：2014-07-29

Applicant: GILEAD CONNECTICUT, INC.

Inventor： Melissa Jean Casteel ,  Bei Li ,  Rowchanak Pakdaman ,  Diana Sperger ,  Dimitrios Stefanidis

IPC: A61K31/5377 ,  A61K47/10 ,  A61K47/38

CPC classification number: A61K9/2095 ,  A61K9/2027 ,  A61K9/2866 ,  A61K31/5377 ,  A61K47/10 ,  A61K47/38 ,  B29B9/10 ,  B29C43/003 ,  B29C43/02 ,  B29K2995/0056 ,  C07C309/66 ,  C07D487/04

Abstract: Disclosed are pharmaceutical compositions comprising a compound having the formula: or a pharmaceutically acceptable salt thereof, or a hydrate of thereof, and at least one pharmaceutically acceptable polymer. The pharmaceutically acceptable salt of the compound of Formula I, or a hydrate thereof, can be a mesylate salt, including, for example, a mono-mesylate or a bis-mesylate salt, or a hydrate thereof. Also disclosed are methods of use for the pharmaceutical composition.

公开(公告)号：US10266539B2

公开(公告)日：2019-04-23

申请号：US15788583

申请日：2017-10-19

Applicant: Gilead Connecticut, Inc.

Inventor： Tim G. Elford ,  Peter Chee-Chu Fung ,  Michael Laird Hurrey ,  Dimitrios Stefanidis ,  Dragos Vizitiu

IPC: C07D487/04 ,  C07C309/04

Abstract: Polymorphs of a bis-mesylate salt of a compound of Formula I: or a hydrate thereof, are provided. The bis-mesylate salt may also be depicted as a compound of Formula IA: Provided herein are also compositions thereof, methods for their preparation and methods for such polymorphs.

公开(公告)号：US20170217967A1

公开(公告)日：2017-08-03

申请号：US15484844

申请日：2017-04-11

Applicant: Gilead Connecticut, Inc.

Inventor： Tim G. Elford ,  Peter Chee-Chu Fung ,  Michael Laird Hurrey ,  Dimitrios Stefanidis ,  Dragos Vizitiu

IPC: C07D487/04

CPC classification number: C07D487/04 ,  C07C309/04

Abstract: Polymorphs of a bis-mesylate salt of a compound of Formula I: or a hydrate thereof, are provided. The bis-mesylate salt may also be depicted as a compound of Formula IA: Provided herein are also compositions thereof, methods for their preparation and methods for such polymorphs.