公开(公告)号：WO2006122072A3

公开(公告)日：2007-05-03

申请号：PCT/US2006017817

申请日：2006-05-09

Applicant: VERTEX PHARMA ,  ANSELL GRAHAM ,  BLYTHE TODD A ,  JONES ANDREW D ,  LITTLER BENJAMIN ,  LOOKER ADAM ,  NYCE PHILIP L ,  SNOONIAN JOHN R

Inventor： ANSELL GRAHAM ,  BLYTHE TODD A ,  JONES ANDREW D ,  LITTLER BENJAMIN ,  LOOKER ADAM ,  NYCE PHILIP L ,  SNOONIAN JOHN R

IPC: C07C275/42 ,  C07C271/34 ,  C07D307/16 ,  C07D413/12

CPC classification number: C07D307/20 ,  C07D413/12

Abstract: The present invention relates to processes for preparing biaryl ureas derivatives and analogs thereof. The invention also provides compounds useful as intermediates in the processes of the present invention. The process is useful for preparing compounds that inhibit IMPDH.

Abstract translation: 本发明涉及制备联芳基脲衍生物及其类似物的方法。 本发明还提供了可用作本发明方法中的中间体的化合物。 该方法可用于制备抑制IMPDH的化合物。

公开(公告)号：EP3250562A4

公开(公告)日：2018-07-11

申请号：EP16744240

申请日：2016-01-29

Applicant: BIOMED VALLEY DISCOVERIES INC ,  VERTEX PHARMA

Inventor： DECRESCENZO GARY ,  WELSCH DEAN ,  VLAHOVA PETINKA I ,  BOERRIGTER STEPHAN X M ,  ARONOV ALEXANDER ,  KESHAVARZ-SHOKRI ALI ,  SCANGAS ALEXANDER N ,  STAVROPOULOS KATHY ,  LITTLER BENJAMIN ,  KADIYALA IRINA NIKOLAEVNA ,  ALARGOVA ROSSITZA GUEORGUIEVA

IPC: C07D401/04 ,  A61K31/4439 ,  A61K45/06 ,  A61P35/00

CPC classification number: C07D401/04 ,  A61K31/4439 ,  A61K45/06 ,  A61P35/00

Abstract: The present invention provides crystalline forms of a compound of formula (I): Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.

公开(公告)号：MX2012004790A

公开(公告)日：2013-02-01

申请号：MX2012004790

申请日：2010-10-21

Applicant: VERTEX PHARMA

Inventor： SHETH URVI ,  ROEPER STEFANIE ,  HURLEY DENNIS JAMES ,  AMBHAIKAR NARENDRA BHALCHANDRA ,  HUGHES ROBERT ,  LITTLER BENJAMIN ,  LEE ELAINE CHUNGMIN ,  NUMA MEHDI

IPC: C07D215/56 ,  C07D487/08

Abstract: La presente invención se relaciona con procesos para preparar formas en estado sólido de N-(4-(7-azabiciclo [2.2.1]heptan-7-il)-2-(trifluorometil)fenil)-4-oxo-5-(trifluorome til)-1,4-dihidroquinolina-3-carboxamida, entre las que se incluyen la Forma A del Compuesto 1, la Forma A-HC1 del Compuesto 1, la Forma B del Compuesto 1, y la Forma B-HC1 del compuesto 1, cualquier combinación de estas formas, las composiciones farmacéuticas de las mismas, y los métodos de tratamiento con las mismas.

公开(公告)号：NO20076307L

公开(公告)日：2007-12-07

申请号：NO20076307

申请日：2007-12-07

Applicant: VERTEX PHARMA

Inventor： SNOONIAN JOHN R ,  LOOKER ADAM ,  ANSELL GRAHAM ,  BLYTHE TODD A ,  JONES ANDREW D ,  LITTLER BENJAMIN ,  NYCE PHILIP L

IPC: C07C275/42 ,  C07C271/34 ,  C07D307/16 ,  C07D413/12

Abstract: The present invention relates to processes for preparing biaryl ureas derivatives and analogs thereof. The invention also provides compounds useful as intermediates in the processes of the present invention. The process is useful for preparing compounds that inhibit IMPDH.

公开(公告)号：CA2606780A1

公开(公告)日：2006-11-16

申请号：CA2606780

申请日：2006-05-09

Applicant: VERTEX PHARMA

Inventor： LOOKER ADAM ,  SNOONIAN JOHN R ,  NYCE PHILIP L ,  BLYTHE TODD A ,  ANSELL GRAHAM ,  JONES ANDREW D ,  LITTLER BENJAMIN

IPC: C07C275/42 ,  C07C271/34 ,  C07D307/16 ,  C07D413/12

Abstract: The present invention relates to processes for preparing biaryl ureas derivatives and analogs thereof. The invention also provides compounds useful as intermediates in the processes of the present invention. The process is useful for preparing compounds that inhibit IMPDH.

公开(公告)号：NZ772411A

公开(公告)日：2022-05-27

申请号：NZ77241116

申请日：2016-01-29

Applicant: VERTEX PHARMA ,  BIOMED VALLEY DISCOVERIES INC

Inventor： DECRESCENZO GARY ,  WELSCH DEAN ,  VLAHOVA PETINKA I ,  BOERRIGTER STEPHAN X M ,  ARONOV ALEXANDER ,  KESHAVARZ-SHOKRI ALI ,  SCANGAS ALEXANDER N ,  STAVROPOULOS KATHY ,  LITTLER BENJAMIN ,  KADIYALA IRINA NIKOLAEVNA ,  ALARGOVA ROSSITZA GUEORGUIEVA

IPC: C07D401/04

Abstract: The present invention provides crystalline forms of a compound of formula (I). Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.

公开(公告)号：AU2016211246A1

公开(公告)日：2017-08-10

申请号：AU2016211246

申请日：2016-01-29

Applicant: BIOMED VALLEY DISCOVERIES INC ,  VERTEX PHARMA

Inventor： DECRESCENZO GARY ,  WELSCH DEAN ,  VLAHOVA PETINKA I ,  BOERRIGTER STEPHAN X M ,  ARONOV ALEXANDER ,  KESHAVARZ-SHOKRI ALI ,  SCANGAS ALEXANDER N ,  STAVROPOULOS KATHY ,  LITTLER BENJAMIN ,  KADIYALA IRINA NIKOLAEVNA ,  ALARGOVA ROSSITZA GUEORGUIEVA

IPC: C07D401/04

Abstract: The present invention provides crystalline forms of a compound of formula (I). Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer. It has been discovered that crystalline forms of 4-(5-Chloro-2- isopropylaminopyridin-4-yl)-1 H-pyrrole-2-carboxylic acid [1 -(3-chlorophenyl)-2- hydroxyethyl]amide can be prepared which exhibit improved properties, e.g. surprisingly improved stability and improved solubility characteristics. Thus, the present invention provides crystalline 4-(5-Chloro-2- isopropylaminopyridin-4-yl)-1H-pyrrole-2-carboxylic acid [1 -(3-chlorophenyl)-2- hydroxyethyljamide.

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：NZ598277A

公开(公告)日：2014-03-28

申请号：NZ59827710

申请日：2010-09-17

Applicant: VERTEX PHARMA

Inventor： AMBHAIKAR NARENDRA BHALCHANDRA ,  HUGHES ROBERT ,  BEAR BRIAN RICHARD ,  FANNING LEV T D ,  LITTLER BENJAMIN

IPC: C07D487/08

Abstract: 598277 The present disclosure relates to a process for preparing azabicyclic compounds that are useful intermediates for synthesizing pharmaceutical compounds or salts thereof. The process comprises contacting trans-4-aminocyclohexanol with Boc anhydride to produce a compound of formula A, contacting a compound of formula A with methanesulfonic acid to produce a compound of formula B contacting a compound of formula B with trifluoroacetic acid to produce a compound of formula C and contacting a compound of formula C with hydroxide to produce a compound of formula 7.

公开(公告)号：AU2010295461A1

公开(公告)日：2012-03-08

申请号：AU2010295461

申请日：2010-09-17

Applicant: VERTEX PHARMA

Inventor： AMBHAIKAR NARENDRA BHALCHANDRA ,  BEAR BRIAN RICHARD ,  FANNING LEV T D ,  HUGHES ROBERT ,  LITTLER BENJAMIN

IPC: C07D487/08

Abstract: The present invention relates to a process for preparing azabicyclic compounds that are useful intermediates for synthesizing pharmaceutical compounds or salts thereof.