公开(公告)号：SG10201913313QA

公开(公告)日：2020-03-30

申请号：SG10201913313Q

申请日：2014-12-12

Applicant: VERTEX PHARMA

Inventor： ANDERSON COREY ,  HADIDA-RUAH SARA ,  GOLEC JULIAN MARIAN ,  ZHANG BEILI ,  LITTLER BENJAMIN ,  KESHAVARZ-SHOKRI ALI ,  ALCACIO TIM ,  BELMONT DANIEL

Abstract: The invention relates to a process and intermediates for preparing prodrug compounds of formula I: wherein R2, R3, R5, R7 and X are as defined herein.

公开(公告)号：NZ734535A

公开(公告)日：2019-05-31

申请号：NZ73453511

申请日：2011-04-21

Applicant: VERTEX PHARMA

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

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

Abstract: Provided is a method of synthesising compounds of general formula (III) which are useful intermediates for the preparation of analogues of Tezacaftor / VX-661. Key to the process is the neutralising step to produce the free base of the compound of formula IIID-a. Also provided are the analogues of Tezacaftor when prepared by the claimed process.

公开(公告)号：SG11201705924RA

公开(公告)日：2017-08-30

申请号：SG11201705924R

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.

公开(公告)号：CA2975048A1

公开(公告)日：2016-08-04

申请号：CA2975048

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：NZ563478A

公开(公告)日：2011-04-29

申请号：NZ56347806

申请日：2006-05-09

Applicant: VERTEX PHARMA

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

IPC: C07C275/42 ,  C07C271/34 ,  C07C275/28 ,  C07D263/32 ,  C07D307/12 ,  C07D307/16 ,  C07D413/12

Abstract: Disclosed is a process for the preparation of ureido-benzylcarbamate derivatives as represented by the general formula (I), wherein Y is zero; R1 or R2 is selected from hydrogen, methyl, ethyl or phenyl; and the other of R1 or R2 is selected from -CH2OH, -CH2CN, -CH2CH2CN, or -CH2N(CH2CH3)2; or wherein R1 and R2 are taken together to form a 3-tetrahydrofuranyl moiety; R9 is hydrogen, (S)-methyl, (S)-ethyl, or (S)-hydroxymethyl; R10 is selected from -C=N or 5-oxazolyl; R11 is methoxy, ethoxy or isopropoxy; and wherein the other substituents are as defined herein; said process comprises the step of reacting a compound of formula II with a compound of formula III under suitable conditions.

公开(公告)号：CA2772792A1

公开(公告)日：2011-03-24

申请号：CA2772792

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.

公开(公告)号：AU2006244173A1

公开(公告)日：2006-11-16

申请号：AU2006244173

申请日：2006-05-09

Applicant: VERTEX PHARMA

Inventor： ANSELL GRAHAM ,  LOOKER ADAM ,  BLYTHE TODD A ,  NYCE PHILIP L ,  SNOONIAN JOHN R ,  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.