公开(公告)号：ES2608474T3

公开(公告)日：2017-04-11

申请号：ES11729195

申请日：2011-04-21

Applicant: VERTEX PHARMA

Inventor： LEE ELAINE ,  TANOURY GERALD ,  HARRISON CRISTIAN ,  LITTLER BENJAMIN ,  ROSE PETER ,  HUGHES ROBERT ,  JUNG YOUNG CHUN ,  SIESEL DAVID ,  BELMONT DANIEL

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

Abstract: Un método para preparar un compuesto de fórmula I:**Fórmula** en la que, independientemente para cada caso: el anillo A es**Fórmula** se selecciona independientemente de -RJ, -ORJ, -N(RJ)2 , -NO2, halógeno, -CN, -C1-4haloalquilo, -C1- 4haloalcoxi, -C(O)N(RJ)2 , -NRJC(O)RJ, -SORJ, -SO2RJ, -SO2N(RJ)2 , -NRJSO2RJ, -CORJ, -CO2RJ, - NRJSO2N(RJ)2, -COCORJ ; RJ es hidrógeno o C1-6alifático; X es CN o CO2R; R es C1-6alifático o arilo; y m es un número entero de 0 a 3 inclusive; comprendiendo las etapas de a) hacer reaccionar un compuesto de fórmula IA en un primer disolvente orgánico**Fórmula** en la que, independientemente para cada caso: el anillo A es**Fórmula** se selecciona independientemente de -RJ, -ORJ, -N(RJ)2 , -NO2, halógeno, -CN, -C1-4haloalquilo, -C1- 4haloalcoxi, -C(O)N(RJ)2 , -NRJC(O)RJ, -SORJ, -SO2RJ, -SO2N(RJ)2 , -NRJSO2RJ, -CORJ, -CO2RJ, - NRJSO2N(RJ)2 , -COCORJ ; RJ es hidrógeno o C1-6alifático; m es un número entero de 0 a 3 inclusive; y Hal es un haluro; con un compuesto de fórmula IB:**Fórmula** en la que RJ es hidrógeno o C1-6alifático, para formar un compuesto de fórmula IC:**Fórmula** en la que, independientemente para cada caso: el anillo A es**Fórmula** R1 se selecciona independientemente de -RJ, -ORJ, N(RJ)2 , -NO2, halógeno, -CN, -C1-4haloalquilo, -C1- 4haloalcoxi, -C(O)N(RJ)2 , -NRJC(O)RJ, -SORJ, -SO2RJ, -SO2N(RJ)2 , -NRJSO2RJ, -CORJ, -CO2RJ, - NRJSO2N(RJ)2 , -COCORJ ; RJ es hidrógeno o C1-6alifático; X es CN o CO2R: R es C1-6alifático o arilo; y m es un número entero de 0 a 3 inclusive; y b) eliminar el -CO2RJ grupo a partir del compuesto IC en un segundo disolvente orgánico para formar un compuesto de fórmula I.

公开(公告)号：AU2016202569A1

公开(公告)日：2016-05-19

申请号：AU2016202569

申请日：2016-04-22

Applicant: VERTEX PHARMA

Inventor： LEE ELAINE CHUNGMIN ,  TANOURY GERALD J ,  HARRISON CRISTIAN ,  LITTLER BENJAMIN JOSEPH ,  ROSE PETER JAMISON ,  HUGHES ROBERT MICHAEL ,  JUNG YOUNG CHUN ,  SIESEL DAVID ANDREW ,  BELMONT DANIEL T

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

Abstract: PROCESS OF PRODUCING CYCLOALKYLCARBOXAMIDO-INDOLE 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 I), useful for treating CFTR mediated diseases such as cystic fibrosis.

公开(公告)号：SG184987A1

公开(公告)日：2012-11-29

申请号：SG2012078374

申请日：2011-04-21

Applicant: VERTEX PHARMA ,  LEE ELAINE CHUNGMIN

Inventor： TANOURY GERALD J ,  HARRISON CRISTIAN ,  LITTLER BENJAMIN JOSEPH ,  ROSE PETER JAMISON ,  HUGHES ROBERT MICHAEL ,  JUNG YOUNG CHUN ,  SIESEL DAVID ANDREW ,  LEE ELAINE CHUNGMIN ,  BELMONT DANIEL T

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.

公开(公告)号：NZ583848A

公开(公告)日：2012-07-27

申请号：NZ58384808

申请日：2008-09-15

Applicant: VERTEX PHARMA

Inventor： DEMATTEI JOHN ,  FENG YUSHI ,  HARRISON CRISTIAN ,  LOOKER ADAM ,  MUDUNURI PRAVEEN ,  ROEPER STEFANIE ,  ZHANG YUEGANG

IPC: A61P35/00 ,  A61K31/47 ,  A61P3/00 ,  A61P3/10 ,  A61P25/28 ,  A61P27/02 ,  C07D215/233

Abstract: Disclosed is N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide benzene sulfonate and N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide benzene sulfonate H2O. The compounds are used to treat CFTR-mediated diseases, cystic fibrosis, hereditary emphysema, COPD, dry-eye disease or Sjogren's disease.

公开(公告)号：CA2797118C

公开(公告)日：2021-03-30

申请号：CA2797118

申请日：2011-04-21

Applicant: VERTEX PHARMA

Inventor： TANOURY GERALD J ,  HARRISON CRISTIAN ,  LITTLER BENJAMIN JOSEPH ,  ROSE PETER JAMISON ,  HUGHES ROBERT MICHAEL ,  JUNG YOUNG CHUN ,  SIESEL DAVID ANDREW ,  BELMONT DANIEL T ,  LEE ELAINE CHUNGMIN ,  NUGENT WILLIAM A

IPC: C07D209/12 ,  C07D405/12

Abstract: The present invention features processes for preparing a compound of formula III: (see formula III) compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-( 1 -hydroxy-2-methylpropan-2-yl)- 1 H-indol-5-yl)cyclopropanecarboxamide (Compound 1), useful for treating CFTR mediated diseases such as cystic fibrosis.

公开(公告)号：SG10201913594UA

公开(公告)日：2020-02-27

申请号：SG10201913594U

申请日：2011-04-21

Applicant: VERTEX PHARMA

Inventor： TANOURY GERALD ,  HARRISON CRISTIAN ,  LITTLER BENJAMIN ,  ROSE PETER ,  HUGHES ROBERT ,  JUNG YOUNG CHUN ,  SIESEL DAVID ,  LEE ELAINE ,  BELMONT DANIEL

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.

公开(公告)号：CA3085006A1

公开(公告)日：2019-06-13

申请号：CA3085006

申请日：2018-12-07

Applicant: VERTEX PHARMA

Inventor： ANGELL PAUL T ,  HARRISON CRISTIAN ,  HUGHES ROBERT M ,  LEWANDOWSKI BERENICE ,  LITTLER BENJAMIN J ,  MELILLO VITO ,  NUGENT WILLIAM A ,  SIESEL DAVID ANDREW ,  SMITH DAVID ,  STUDLEY JOHN

IPC: C07D401/14 ,  C07D231/20 ,  C07D401/04 ,  C07D405/04

Abstract: The disclosure provides processes for preparing a compound of Formula (I).

公开(公告)号：NZ717669A

公开(公告)日：2017-09-29

申请号：NZ71766911

申请日：2011-04-21

Applicant: VERTEX PHARMA

Inventor： LEE ELAINE CHUNGMIN ,  HUGHES ROBERT MICHAEL ,  ROSE PETER JAMISON ,  TANOURY GERALD J ,  BELMONT DANIEL T ,  HARRISON CRISTIAN ,  SIESEL DAVID ANDREW ,  LITTLER BENJAMIN JOSEPH ,  JUNG YOUNG CHUN

IPC: C07D209/12

Abstract: intermediates for the preparation of Tezacaftor(VX-661) and its analogues. The intermediates are protecting group (P) bearing indole derivatives of formula III. the protecting group may be one of acetyl, benzoyl, benzyl, methoxyethoxymethyl, dimethoxytrityl, methoxymethyl, methoxytrityl, p-methoxybenzyl, pivaloyl, tetrahydropyranyl, trityl, or trimethylsilyl.

公开(公告)号：ES2622154T3

公开(公告)日：2017-07-05

申请号：ES12794811

申请日：2012-11-08

Applicant: VERTEX PHARMA

Inventor： LOOKER ADAM ,  LITTLER BENJAMIN ,  CHOUDHURY ANUSUYA ,  HARRISON CRISTIAN ,  VELURI RAVIKANTH ,  RYAN MICHAEL ,  JIANG LICONG ,  LUSS-LUSIS EDUARD

IPC: C07D405/12 ,  A61K31/405 ,  A61K31/553 ,  A61P1/00 ,  A61P3/00 ,  A61P11/00 ,  A61P25/00 ,  A61P27/00 ,  A61P35/00 ,  C07D405/14 ,  C07D498/04

Abstract: Un compuesto de formula II:**Fórmula** una sal farmaceuticamente aceptable del mismo, en la que independientemente para cada caso: R es H, OH, OCH3 o dos R tomados juntos forman -OCH2 O-o-OCF2 O-; R1 es H o hasta dos alquilo C1-C6; R2 es H o halo; R3 es H o alquilo C1-C6; Y es O o NR4; y R4 es H o alquilo C1-C6.

公开(公告)号：SG10201505700QA

公开(公告)日：2015-08-28

申请号：SG10201505700Q

申请日：2011-04-21

Applicant: VERTEX PHARMA

Inventor： TANOURY GERALD J ,  HARRISON CRISTIAN ,  LITTLER BENJAMIN JOSEPH ,  ROSE PETER JAMISON ,  HUGHES ROBERT MICHAEL ,  JUNG YOUNG CHUN ,  SIESEL DAVID ANDREW ,  LEE ELAINE CHUNGMIN ,  BELMONT DANIEL T

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.