公开(公告)号：CA2578739A1

公开(公告)日：2006-03-16

申请号：CA2578739

申请日：2005-08-31

Applicant: VERTEX PHARMA

Inventor： HURLEY DENNIS J ,  NEUBERT TIMOTHY D ,  JOSHI PRAMOD ,  KRENITSKY PAUL ,  SHETH URVI ,  FANNING LEV T D ,  TERMIN ANDREAS P ,  GONZALEZ JESUS E III ,  WILSON DEAN M ,  BOGER JOSHUA S

IPC: C07D239/94 ,  A61K31/498 ,  A61P9/06 ,  A61P25/00 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14

Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

公开(公告)号：AU2016203414A1

公开(公告)日：2016-06-23

申请号：AU2016203414

申请日：2016-05-25

Applicant: VERTEX PHARMA

Inventor： CHARRIER JEAN-DAMIEN ,  DURRANT STEVEN ,  KAY DAVID ,  O'DONNELL MICHAEL ,  KNEGTEI RONALD ,  MACCORMICK SOMHAIRLE ,  PINDER JOANNE ,  VIRANI ANISA ,  YOUNG STEPHEN ,  BINCH HAYLEY ,  CLEVELAND THOMAS ,  FANNING LEV ,  HURLEY DENNIS ,  JOSHI PRAMOD ,  SHETH URVI ,  SILINA ALINA

IPC: C07D401/04 ,  A61K31/4965 ,  A61P35/00 ,  C07D403/04 ,  C07D413/04

Abstract: Abstract The present invention relates to pyrazine compounds, pharmaceutical compositions comprising them, and methods for inhibiting ATR protein kinase for treating various diseases, disorders, and conditions including cancer, HIV, hepatitis, adenovirus and psoriasis. Additionally the invention discloses processes for preparing the compounds, intermediates used in the preparation, and methods of using the compounds in in vitro applications including 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.

公开(公告)号：PL2349263T3

公开(公告)日：2014-11-28

申请号：PL09822784

申请日：2009-10-23

Applicant: VERTEX PHARMA

Inventor： BINCH HAYLEY ,  FANNING LEV T D ,  HURLEY DENNIS ,  SHETH URVI ,  SILINA ALINA ,  YANG XIAOQING ,  BOTFIELD MARTYN ,  GROOTENHUIS PETER D J ,  VAN GOOR FREDRICK ,  NUMA MEHDI MICHEL DJAMEL

IPC: A61K31/439 ,  C07D453/04 ,  C12Q1/02

公开(公告)号：NZ600707A

公开(公告)日：2014-09-26

申请号：NZ60070710

申请日：2010-12-10

Applicant: VERTEX PHARMA

Inventor： VAN GOOR FREDRICK F ,  SILINA ALINA ,  SHETH URVI ,  VAIRAGOUNDAR RAJENDRAN ,  HAZLEWOOD ANNA R ,  NUMA MEHDI ,  HADIDA RUAH SARA S ,  BINCH HAYLEY ,  HURLEY DENNIS JAMES ,  FANNING LEV T D ,  BOTFIELD MARTYN C ,  TENHUIS PETER DIEDERIK JAN ,  ZHOU JINGLAN

IPC: C07D215/56 ,  A61K31/47 ,  A61K31/4709 ,  A61P11/00 ,  A61P11/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/08 ,  G01N33/50

Abstract: The present disclosure relates to 4-oxo-1H-quinoline-3-carboxamides as modulators of ATP-Binding Cassette (”ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present disclosure also relates to methods of treating ABC transporter mediated diseases using such modulators. 6,7-difluoro-N-(2-fluoro-5-hydroxy-4-tert-butyl-phenyl)-4-oxo-1H-quinoHne-3-carboxarnide; N-[4-(3,3-dimethylpyrrolidin-1-yl)-2-(trifluoromethyl)phenyl]-6-methyl-4-oxo-1H-quinoline-3-carboxamide; 8-cyano-N-(5-hydroxy-2,4-ditert-butyl-phenyl)-4-oxo-1H-quinaline-3-carboxamide; and (2S,3S)-methyl 3-methyl-1-(4-(4-oxo-1,4-dihydroquinoline-3-carboxamide)-3-(trifluoromethyl)phenyl)pyrrolidine-2-carboxylate. conditions which may be treated by the compounds of the disclosure include: cystic fibrosis, chronic bronchitis, recurrent bronchitis, acute bronchitis, male infertility caused by congenital bilateral absence of the vas deferens (CBAVD), female infertility caused by congenital absence of the uterus and vagina (CAUV), idiopathic chronic pancreatitis (ICP), idiopathic recurrent pancreatitis, idiopathic acute pancreatitis, chronic rhinosinusitis, primary sclerosing cholangitis, diabetes, dry eye, constipation, allergic bronchopulmonary aspergillosis (ABPA), bone diseases, and asthma

公开(公告)号：PT2349263E

公开(公告)日：2014-07-28

申请号：PT09822784

申请日：2009-10-23

Applicant: VERTEX PHARMA

Inventor： BOTFIELD MARTYN ,  GOOR FREDRICK VAN ,  BINCH HAYLEY ,  FANNING LEV T D ,  HURLEY DENNIS ,  SHETH URVI ,  SILINA ALINA ,  YANG XIAOQING ,  GROOTENHUIS PETER D J ,  NUMA MEHDI MICHEL DJAMEL

IPC: A61K31/439 ,  C07D453/04 ,  C12Q1/02

公开(公告)号：NZ600172A

公开(公告)日：2014-07-25

申请号：NZ60017210

申请日：2010-10-21

Applicant: VERTEX PHARMA

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

IPC: C07D215/56 ,  C07D487/08

Abstract: Disclosed herein is a process for producing the hydrochloride salt of Compound 1 having solid Form A-HCl comprising: (a) reacting Compound 2 with the hydrochloride salt of Formula 3 (3-HCl) in the presence of a coupling agent, a base, and a polar aprotic solvent; wherein the coupling agent is selected from the group consisting of 2-chloro-1,3-dimethyl-2-imidazolium tetrafluoroborate, 2-(1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate (HBTU), 2-chloro-4,6-dimethoxy-1,3,5-triazine, 1-H-benzotriazolium-1-[bis(dimethyl amino)methylene]-5-chlorohexafluorophosphate (HCTU), 2-(1H-7-Azabenzotriazol-1-yl)-1,1,3,3-tetramethyl uronium hexafluorophosphate (RA TU), 1-hydroxybenzotriazole (HOBT)/ 1-(3-(dimethylamino)propyl)-3-ethyl-carbodiimide hydrochloride (EDCl), and propane phosphonic anhydride; wherein the base is selected from the group consisting of K2CO3, Et3N, N-methylmorpholine (NMM), pyridine, and diisopropylethyl amine (DIEA); and wherein the polar aprotic solvent is selected from the group consisting of ethyl acetate, isopropyl acetate, tetrahydrofuran, methylethyl ketone, N-Methyl-2-pyrrolidone, acetonitrile, N,N-dimethyl formamide, and 2- methyltetrahydrofuran; and (b) treating a mixture comprising the product of step (a) with HCl; wherein step (a) is performed at a reaction temperature that is maintained between 15°C and 70°C.

公开(公告)号：UA104601C2

公开(公告)日：2014-02-25

申请号：UAA201106356

申请日：2009-10-23

Applicant: VERTEX PHARMA

Inventor： BINCH HAYLEY ,  FANNING LEV T D ,  HURLEY DENNIS ,  SHETH URVI ,  SILINA ALINA ,  YANG XIAOQING ,  BOTFIELD MARTYN ,  GROOTENHUIS PETER D J ,  VAN GOOR FREDRICK ,  NUMA MEHDI MICHEL DJAMEL

IPC: C07D451/02 ,  A61K31/439 ,  A61P11/00

Abstract: Данийвинахідстосуєтьсямодуляторіврегуляторатрансмембранноїпровідностіпримуковісцидозі (CFTR), їхкомпозиційі способівїхньогозастосування. Данийвинахідтакожстосуєтьсяспособівлікуваннязахворюваньпривикористаннімодуляторів CFTR.

公开(公告)号：ZA201202915B

公开(公告)日：2013-06-26

申请号：ZA201202915

申请日：2012-04-20

Applicant: VERTEX PHARMA

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

IPC: C07D20060101

公开(公告)号：MX2012006764A

公开(公告)日：2012-11-23

申请号：MX2012006764

申请日：2010-12-10

Applicant: VERTEX PHARMA

Inventor： BOTFIELD MARTYN C ,  SILINA ALINA ,  BINCH HAYLEY ,  ZHOU JINGLAN ,  FANNING LEV T D ,  SHETH URVI ,  RUAH SARA S HADIDA ,  GOOR FREDRICK F VAN ,  HURLEY DENNIS JAMES ,  NUMA MEHDI ,  VAIRAGOUNDAR RAJENDRA ,  HAZLEWOOD ANNA R ,  GROOTENHUIS PETER DIEDERIK JAN

IPC: C07D215/56 ,  A61K31/4709 ,  A61P11/00 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/08

Abstract: La presente invención se relaciona con 4-oxo-1H-quinolin-3-carboxa midas como moduladores de transportadores del Casete de Unión con ATP ("ABC") o fragmentos de los mismos, entre los que se incluyen el Regulador de Conductancia Transmembrana de Fibrosis Quística, las composiciones de los mismos, y los métodos con los mismos. La presente invención también se relaciona con los métodos para tratar enfermedades provocadas por el transportador del ABC utilizando estos moduladores.

公开(公告)号：AU2010310612A2

公开(公告)日：2012-08-16

申请号：AU2010310612

申请日：2010-10-21

Applicant: VERTEX PHARMA

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

IPC: C07D215/56 ,  C07D487/08

Abstract: The present invention relates to processes for preparing solid state forms of N-(4-(7-azabicyclo[2.2. 1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, including Compound 1 Form A, Compound 1 Form A- HCl, Compound 1 Form B, and Compound 1 Form B-HCl, any combination of these forms, pharmaceutical compositions thereof, and methods of treatment therewith.