公开(公告)号：US09035072B2

公开(公告)日：2015-05-19

申请号：US13642642

申请日：2011-04-21

Applicant: Daniel T. Belmont ,  Cristian Harrison ,  Robert Michael Hughes ,  Young Chun Jung ,  Elaine Chungmin Lee ,  Benjamin Joseph Littler ,  Peter Jamison Rose ,  David Andrew Siesel ,  Gerald J. Tanoury

Inventor： Daniel T. Belmont ,  Cristian Harrison ,  Robert Michael Hughes ,  Young Chun Jung ,  Elaine Chungmin Lee ,  Benjamin Joseph Littler ,  Peter Jamison Rose ,  David Andrew Siesel ,  Gerald J. Tanoury

IPC: C07D209/40 ,  C07D405/12 ,  C07D209/12 ,  C07D317/46 ,  C07D317/60

CPC classification number: C07D317/46 ,  C07C209/74 ,  C07C225/06 ,  C07D209/12 ,  C07D317/60 ,  C07D405/12

Abstract: The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), useful for treating CFTR mediated diseases such as cystic fibrosis.

Abstract translation: 本发明的特征在于制备化合物如（R）-1-（2,2-二氟苯并[d] [1,3]间二氧杂环戊烯-5-基）-N-（1-（2,3-二羟基丙基） -6-氟-2-（1-羟基-2-甲基丙-2-基）-1H-吲哚-5-基）环丙烷甲酰胺（化合物1），可用于治疗CFTR介导的疾病如囊性纤维化。

公开(公告)号：US08461342B2

公开(公告)日：2013-06-11

申请号：US13450805

申请日：2012-04-19

Applicant: David Andrew Siesel

Inventor： David Andrew Siesel

IPC: C07D405/00

CPC classification number: C07D405/12 ,  C07D213/73 ,  C07D213/74 ,  C07D317/60

Abstract: The present invention relates to a process of providing the 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in substantially free form (Compound 1).

公开(公告)号：US06307058B1

公开(公告)日：2001-10-23

申请号：US09604570

申请日：2000-06-27

Applicant: Balwant Singh ,  David Andrew Siesel ,  Laurence Wu-Kwang Chang

Inventor： Balwant Singh ,  David Andrew Siesel ,  Laurence Wu-Kwang Chang

IPC: C07D23340

CPC classification number: C07D233/40 ,  C08F8/30 ,  C08F22/38 ,  D21H21/16

Abstract: Acyl imidazolidinones and compositions containing the same are disclosed, which are particularly suitable for use as self-crosslinkers and can also be used as wet adhesion properties, especially in latex-based polymer systems. Processes for preparing such compounds, compositions containing the same, as well as additional uses thereof are also disclosed.

Abstract translation: 公开了酰基咪唑啉酮和含有它们的组合物，其特别适合用作自交联剂并且还可以用作湿粘合性能，特别是在基于胶乳的聚合物体系中。 还公开了制备此类化合物的方法，含有该化合物的组合物及其其用途。

公开(公告)号：US20130274477A1

公开(公告)日：2013-10-17

申请号：US13913876

申请日：2013-06-10

Applicant: David Andrew Siesel

Inventor： David Andrew Siesel

IPC: C07D405/12

CPC classification number: C07D405/12 ,  C07D213/73 ,  C07D213/74 ,  C07D317/60

Abstract: The present invention relates to a process of providing the 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in substantially free form (Compound 1).

公开(公告)号：US20130184292A1

公开(公告)日：2013-07-18

申请号：US13631759

申请日：2012-09-28

Applicant: Jean-Damien Charrier ,  John Studley ,  Francoise Yvonne Theodora Marie Pierard ,  Steven John Durrant ,  Benjamin Joseph Littler ,  Robert Michael Hughes ,  David Andrew Siesel ,  Paul Angell ,  Armando Urbina ,  Yi Shi

Inventor： Jean-Damien Charrier ,  John Studley ,  Francoise Yvonne Theodora Marie Pierard ,  Steven John Durrant ,  Benjamin Joseph Littler ,  Robert Michael Hughes ,  David Andrew Siesel ,  Paul Angell ,  Armando Urbina ,  Yi Shi

IPC: C07D413/04 ,  C07D413/14 ,  C07D241/20 ,  C07C251/48

CPC classification number: C07D413/04 ,  C07C251/48 ,  C07D241/20 ,  C07D413/14

Abstract: The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention.The compounds of this invention have formula I or II: wherein the variables are as defined herein.

Abstract translation: 本发明涉及制备用作ATR激酶抑制剂的化合物的方法和中间体，例如氨基吡嗪 - 异恶唑衍生物和相关分子。 本发明还涉及可用作ATR蛋白激酶抑制剂的化合物。 本发明涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 和本发明化合物的固体形式。 本发明的化合物具有式I或II：其中变量如本文所定义。

公开(公告)号：US20130324743A1

公开(公告)日：2013-12-05

申请号：US13642642

申请日：2011-04-21

Applicant: Daniel T. Belmont ,  Cristian Harrison ,  Robert Michael Hughes ,  Young Chun Jung ,  Elaine Chungmin Lee ,  Benjamin Joseph Littler ,  Peter Jamison Rose ,  David Andrew Siesel ,  Gerald J. Tanoury

Inventor： Daniel T. Belmont ,  Cristian Harrison ,  Robert Michael Hughes ,  Young Chun Jung ,  Elaine Chungmin Lee ,  Benjamin Joseph Littler ,  Peter Jamison Rose ,  David Andrew Siesel ,  Gerald J. Tanoury

IPC: C07D405/12

CPC classification number: C07D317/46 ,  C07C209/74 ,  C07C225/06 ,  C07D209/12 ,  C07D317/60 ,  C07D405/12

Abstract: The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), useful for treating CFTR mediated diseases such as cystic fibrosis.

Abstract translation: 本发明的特征在于制备化合物如（R）-1-（2,2-二氟苯并[d] [1,3]间二氧杂环戊烯-5-基）-N-（1-（2,3-二羟基丙基） -6-氟-2-（1-羟基-2-甲基丙-2-基）-1H-吲哚-5-基）环丙烷甲酰胺（化合物1），可用于治疗CFTR介导的疾病如囊性纤维化。

公开(公告)号：US20130089625A1

公开(公告)日：2013-04-11

申请号：US13631732

申请日：2012-09-28

Applicant: Jean-Damien Charrier ,  Pierre-Henri Storck ,  John Studley ,  Francoise Yvonne Theodora Marie Pierard ,  Steven John Durrant ,  Benjamin Joseph Littler ,  Paul Angell ,  Robert Michael Hughes ,  David Andrew Siesel ,  Armando Urbina ,  Carl Zwicker ,  Nicholas LoConte ,  Timothy Barder

Inventor： Jean-Damien Charrier ,  Pierre-Henri Storck ,  John Studley ,  Francoise Yvonne Theodora Marie Pierard ,  Steven John Durrant ,  Benjamin Joseph Littler ,  Paul Angell ,  Robert Michael Hughes ,  David Andrew Siesel ,  Armando Urbina ,  Carl Zwicker ,  Nicholas LoConte ,  Timothy Barder

IPC: C07D413/14 ,  A61K45/06 ,  A61N5/10 ,  A61K31/4745 ,  A61K31/7068 ,  A61K31/497 ,  A61K33/24

CPC classification number: C07D413/14 ,  A61K31/4745 ,  A61K31/497 ,  A61K31/7068 ,  A61K33/24 ,  A61K45/06 ,  A61N5/10

Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; solid forms of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I-1: wherein the variables are as defined herein.Additionally, the compounds of this invention have formula II: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined herein.

Abstract translation: 本发明涉及可用作ATR蛋白激酶抑制剂的化合物。 本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 固体形式的本发明化合物; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。 本发明的化合物具有式I-1：其中变量如本文所定义。 此外，本发明的化合物具有式II：或其药学上可接受的盐，其中变量如本文所定义。