公开(公告)号：WO2013006634A9

公开(公告)日：2013-03-21

申请号：PCT/US2012045431

申请日：2012-07-03

Applicant: VERTEX PHARMA ,  TANOURY GERALD J ,  JUNG YOUNG CHUN ,  MAGDZIAK DEREK ,  LOOKER ADAM

Inventor： TANOURY GERALD J ,  JUNG YOUNG CHUN ,  MAGDZIAK DEREK ,  LOOKER ADAM

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07B2200/13 ,  C07D239/42 ,  C07F5/025 ,  C07F5/04

Abstract: The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of Janus kinases (JAK).

Abstract translation: 本发明涉及用于制备可用作Janus激酶（JAK）抑制剂的化合物的方法和中间体。

公开(公告)号：WO2013006634A3

公开(公告)日：2013-05-10

申请号：PCT/US2012045431

申请日：2012-07-03

Applicant: VERTEX PHARMA ,  TANOURY GERALD J ,  JUNG YOUNG CHUN ,  MAGDZIAK DEREK ,  LOOKER ADAM ,  KLINE BILLIE J ,  JURCIK VACLAV ,  DOMINGUEZ OLMO BEATRIZ

Inventor： TANOURY GERALD J ,  JUNG YOUNG CHUN ,  MAGDZIAK DEREK ,  LOOKER ADAM ,  KLINE BILLIE J ,  JURCIK VACLAV ,  DOMINGUEZ OLMO BEATRIZ

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07B2200/13 ,  C07D239/42 ,  C07F5/025 ,  C07F5/04

Abstract: The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of Janus kinases (JAK).

Abstract translation: 本发明涉及制备可用作Janus激酶（JAK）抑制剂的化合物的方法和中间体。

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：WO2009038683A3

公开(公告)日：2010-08-26

申请号：PCT/US2008010728

申请日：2008-09-15

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

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

IPC: C07D215/233

CPC classification number: C07D215/56 ,  A61K31/47 ,  A61K45/06 ,  C07D215/233

Abstract: Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide are described herein, including crystalline forms thereof.

Abstract translation: 本文描述了固体形式的N- [2,4-双（1,1-二甲基乙基）-5-羟基苯基] -1,4-二氢-4-氧代喹啉-3-甲酰胺，包括其结晶形式。

公开(公告)号：WO2005085236A3

公开(公告)日：2005-10-20

申请号：PCT/US2005006540

申请日：2005-02-28

Applicant: VERTEX PHARMA ,  CHARRIER JEAN-DAMIEN ,  DURRANT STEVEN ,  MORTIMORE MICHAEL ,  O'DONNELL MICHAEL ,  RUTHERFORD ALISTAIR ,  RAMAYA SHARN ,  STUDLEY JOHN R ,  TRUDEAU MARTIN ,  LOOKER ADAM

Inventor： CHARRIER JEAN-DAMIEN ,  DURRANT STEVEN ,  MORTIMORE MICHAEL ,  O'DONNELL MICHAEL ,  RUTHERFORD ALISTAIR ,  RAMAYA SHARN ,  STUDLEY JOHN R ,  TRUDEAU MARTIN ,  LOOKER ADAM

IPC: A61K38/04 ,  A61K38/06 ,  C07D207/16 ,  C07D209/52 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D417/06 ,  C07D417/12 ,  C07K5/02 ,  C07K5/04 ,  A61K31/401 ,  A61K31/4025 ,  A61K31/403 ,  A61K31/443 ,  A61P37/00

CPC classification number: C07D405/12 ,  A61K38/06 ,  C07D207/16 ,  C07D209/52 ,  C07D401/12 ,  C07D401/14 ,  C07D417/06 ,  C07D417/12 ,  C07K5/0202

Abstract: The present invention provides a compound of formula (I): wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula (I), and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.

Abstract translation: 本发明提供式（I）的化合物：其中变量如本文所定义。 本发明还提供制备式（I）化合物及其中间体，包含那些化合物的药物组合物的方法，以及使用该化合物和组合物的方法。

公开(公告)号：BR112021022832A2

公开(公告)日：2022-01-18

申请号：BR112021022832

申请日：2020-05-14

Applicant: VERTEX PHARMA

Inventor： LOOKER ADAM ,  MEDEK ALES ,  AMY BETH HALL ,  MAXWELL BRAD ,  CAVAN MCKEON BLIGH ,  DENNIS JAMES HURLEY ,  BOUCHER DIANE ,  GABRIELLE SIMONE FLEMING ,  XU JINWANG ,  JOHN PATRICK MAXWELL ,  STAVROPOULOS KATHY ,  KEVIN JAMES GAGNON ,  KEVIN MICHAEL COTTRELL ,  KIRK ALAN OVERHOFF ,  LEV TYLER DEWEY FANNING ,  MAC ARTHUR JOHNSON JR ,  ZAKY MARIAM ,  SPOSATO MARISA ,  LAI MEI-HSIU ,  MICHAEL AARON BRODNEY ,  MICHAEL JOHN BOYD ,  MICHAEL PHILIP CLARK ,  SHRESTHA MUNA ,  PEDRO MANUEL GARCIA BARRANTES ,  JONES PETER ,  PHILIPPE MARCEL NUHANT ,  TANG QING ,  REBECCA JANE SWETT ,  ROBERT DANIEL GIACOMETTI ,  ROBERT FRANCIS FIMOGNARI ,  RONALD LEE GREY JR ,  SAWANT RUPA ,  GUIDO SAMANTHA ,  SARAH CAROL HOOD ,  KESAVAN SARATHY ,  RODAY SETU ,  GIROUX SIMON ,  LIU SIYING ,  ROEPER STEFANIE ,  THOMSON STEPHEN ,  STEVEN M RONKIN ,  TIMOTHY LEWIS TAPLEY ,  UPUL KEERTHI BANDARAGE ,  DAMAGNEZ VERONIQUE ,  SHI YI

IPC: C07D231/56 ,  A61K31/4162 ,  A61K31/429 ,  A61P1/16 ,  A61P11/00 ,  C07D487/04 ,  C07D498/18 ,  C07D513/04

Abstract: pirrois tricíclicos condensados como moduladores da alfa-1 antitripsina. a divulgação fornece compostos úteis para tratar a deficiência de alfa-1 antitripsina (aatd), de acordo com a fórmula (i), seus tautômeros, sais farmaceuticamente aceitáveis dos compostos, sais farmaceuticamente aceitáveis dos tautômeros, derivados deuterados dos compostos, derivados deuterados dos tautômeros e derivados deuterados dos sais, formas sólidas desses compostos e processos para produzir esses compostos.

公开(公告)号：CA3114672A1

公开(公告)日：2020-04-23

申请号：CA3114672

申请日：2019-10-04

Applicant: VERTEX PHARMA

Inventor： BLIGH CAVAN MCKEON ,  BRODNEY MICHAEL AARON ,  ECCLES MARY ELIZABETH ,  GAGNON KEVIN JAMES ,  HOOD SARAH CAROL ,  HUSSEY JOSHUA KENNEDY ,  LOOKER ADAM ,  MAXWELL JOHN PATRICK ,  MEDEK ALES ,  NAVAMAL METTACHIT ,  RODAY SETU ,  ROEPER STEFANIE ,  SAWANT RUPA ,  SHI YI ,  TANG QING ,  WALDO MICHAEL ,  BANDARAGE UPUL KEERTHI ,  BOUCHER DIANE M ,  BOYD MICHAEL JOHN ,  DAMAGNEZ VERONIQUE ,  DEWEY FANNING LEV TYLER ,  FIMOGNARI JR ,  GARCIA BARRANTES PEDRO M ,  GIROUX SIMON ,  GREY JR ,  HALL AMY BETH ,  HURLEY DENNIS JAMES ,  JOHNSON JR ,  JONES PETER ,  KESAVAN SARATHY ,  NUHANT PHILIPPE MARCEL ,  SWETT REBECCA JANE ,  TAPLEY TIMOTHY LEWIS ,  THOMSON STEPHEN A ,  XU JINWANG ,  MAXWELL BRAD D ,  COTTRELL KEVIN MICHAEL

IPC: C07D487/04 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/7056 ,  C07D471/14 ,  C07D487/14 ,  C07D519/00 ,  C07H13/02

Abstract: Novel compounds, compositions, and methods of using and preparing the same, which may be useful for treating alpha-1 antitrypsin deficiency (AATD).

公开(公告)号：BRPI1013338A2

公开(公告)日：2016-03-29

申请号：BRPI1013338

申请日：2010-04-27

Applicant: VERTEX PHARMA

Inventor： LOOKER ADAM ,  TANOURY GERALD J ,  COCHRAN JOHN E ,  CHEN MINZHANG ,  JURKAUSKAS VALDAS

IPC: C07D209/52 ,  A61K31/403 ,  C07D471/08

公开(公告)号：AU2008301907B2

公开(公告)日：2014-02-20

申请号：AU2008301907

申请日：2008-09-15

Applicant: VERTEX PHARMA

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

IPC: C07D215/233

Abstract: Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide are described herein, including crystalline forms thereof.

公开(公告)号：NZ600865A

公开(公告)日：2014-01-31

申请号：NZ60086508

申请日：2008-09-15

Applicant: VERTEX PHARMA

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

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

Abstract: 600865 Disclosed is N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1)• PEG 400 (polyethylene glycol)•KOAc (potassium acetate). Also disclosed are crystalline form and x-ray powder diffraction patterns of Compound 1•PEG 400•KOAc, pharmaceutical combinations comprising Compound 1•PEG 400•KOAc, methods of making Compound 1•PEG 400•KOAc and the use of Compound 1•PEG 400•KOAc in the manufacture of a medicament. The medicament is useful in the treatment of cystic fibrosis, hereditary emphysema, hereditary hemochromatosis, coagulation- fibrinolysis deficiencies, lipid processing deficiencies, lysosomal storage diseases, neurodegenerative diseases, polyglutamine neurological disorders, spongiform encephalopathies, COPD, dry-eye disease, and Sjogren’s disease.