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公开(公告)号:AU2012244242A1
公开(公告)日:2012-11-15
申请号:AU2012244242
申请日:2012-10-26
Applicant: VERTEX PHARMA
Inventor: BEAR BRIAN , MCCARTNEY JASON , RUAH SARA S HADIDA , GROOTENHUIS PETER D J , MILLER MARK T
IPC: C07D317/68 , A61K31/36 , A61P11/00
Abstract: MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS Abstract Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette ("ABC") transporters or s fragments thereof, including Cystic Fibrosis transmembrane Conductance Regulator ("CFTR"). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
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公开(公告)号:HK1161259A1
公开(公告)日:2012-08-24
申请号:HK12102075
申请日:2012-02-29
Applicant: VERTEX PHARMA
Inventor: BINCH HAYLEY , FANNING LEV T D , HURLEY DENNIS , SHETH URVI , SILINA ALINA , YANG XIAOQING , BOTFIELD MARTYN , GROOTENHUIS PETER D J , GOOR FREDRICK VAN , NUMA MEHDI MICHEL DJAMEL
IPC: C07D20060101 , A61K20060101 , A61P20060101
Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.
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公开(公告)号:AU2006336504B2
公开(公告)日:2012-07-26
申请号:AU2006336504
申请日:2006-12-28
Applicant: VERTEX PHARMA
Inventor: MILLER MARK T , GROOTENHUIS PETER D J , MCCARTNEY JASON , RUAH SARA S HADIDA , BEAR BRIAN
IPC: C07D317/68 , A61K31/36 , A61P11/00
Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein: Each R1 is independently an optionally substituted C aliphatic, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted C membered cycloaliphatic or an optionally substituted 4 to 10 membered heterocycloaliphatic, carboxy, amido, amino, halo, or hydroxy, provided that at least one R is an optionally substituted aryl or an optionally substituted heteroaryl and said R is attached to the 3- or 4- position of the phenyl ring; R is hydrogen, an optionally substituted C aliphatic, an optionally substituted C cycloaliphatic, an optionally substituted phenyl, or an optionally substituted heteroaryl; Ring A is an optionally substituted cycloaliphatic or an optionally substituted heterocycloaliphatic where the atoms of ring A adjacent to C* are carbon atoms; Each R is an optionally substituted aryl or an optionally substituted heteroaryl; and n is 1, 2, 3, 4, or 5. Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette ("ABC") transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator ("CFTR"). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
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公开(公告)号:ZA201102900B
公开(公告)日:2012-07-25
申请号:ZA201102900
申请日:2011-04-18
Applicant: VERTEX PHARMA
Inventor: BINCH HAYLEY , FANNING LEV T D , HURLEY DENNIS J , SHETH URVI , SILINA ALINA , YANG XIAOQING , BOTFIELD MARTYN C , GROOTENHUIS PETER D J , VAN GOOR FREDERICK , NUMA MEHDI MICHEL DJAMEL
IPC: A61K20060101 , C07D20060101 , A61P20060101 , C12Q20060101
Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.
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公开(公告)号:CL2011001004A1
公开(公告)日:2012-03-16
申请号:CL2011001004
申请日:2011-05-05
Applicant: VERTEX PHARMA
Inventor: RUAH SARA S HADIDA , GROOTENHUIS PETER D J , MILLER MARK T MCCARTNEY JASON , VAN GOOR FREDRICK NUMA MEHDI MICHAEL DJAMEL
IPC: A61K31/404 , A61P3/00 , A61P25/00 , C07D405/12
Abstract: Compuestos heterocíclicos moduladores de transportadores de casetes de unión a atp (abc); composición farmacéutica; kit farmacéutico; útiles para tratar una afección, enfermedad o trastorno tal como fibrosis quística, enfisema hereditario, Alzheimer, diabetes, entre otras.
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公开(公告)号:NZ571803A
公开(公告)日:2011-12-22
申请号:NZ57180307
申请日:2007-04-09
Applicant: VERTEX PHARMA
Inventor: VAN GOOR FREDRICK , YANG XIAOQING , RUAH SARA S HADIDA , GROOTENHUIS PETER D J , ZHOU JINGLAN , BEAR BRIAN , MILLER MARK T , MCCARTNEY JASON , NUMA MEHDI MICHEL JAMEL
IPC: C07D405/12 , A61K31/404 , A61P31/00 , C07D405/14
Abstract: Disclosed is a compound of formula Id e.g. 1-(Benzo[d][1,3]dioxol-5-yl)-N-(2-(2-methyl-4-(1H-tetrazol-5-yl)butan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide or a pharmaceutically acceptable salt thereof, wherein R1, R2, A, B and n are defined in the specification for treating or lessening the severity of a disease in a patient, wherein said disease is selected from cystic fibrosis, hereditary emphysema, hereditary hemochromatosis, coagulation-fibrinolysis deficiencies, Type 1 hereditary angioedema, Type 1 chylomicronemia, abetalipoproteinemia, lysosomal storage diseases, mucopolysaccharidoses, Sandhof/Tay-Sachs, Crigler-Najjar type II, polyendocrinopathy/hyperinsulemia, Diabetes mellitus, Laron dwarfism, myeloperoxidase deficiency, primary hypoparathyroidism, melanoma, glycanosis CDG type 1, congenital hyperthyroidism, osteogenesis imperfecta, hereditary hypofibrinogenemia, ACT deficiency, Diabetes insipidus, neurophyseal DI, neprogenic DI, Charcot-Marie Tooth syndrome, Perlizaeus-Merzbacher disease, neurodegenerative diseases, Parkinson's disease, amyotrophic lateral sclerosis, progressive supranuclear plasy, Pick's disease, polyglutamine neurological disorders, spongiform encephalopathies, Fabry disease, Straussler-Scheinker syndrome, COPD, dry-eye disease, or Sjogren's disease.
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公开(公告)号:SG174410A1
公开(公告)日:2011-11-28
申请号:SG2011066578
申请日:2010-03-19
Applicant: VERTEX PHARMA
Inventor: DEMATTEI JOHN , LOOKER ADAM R , NEUBERT-LANGILLE BOBBIANNA , TRUDEAU MARTIN , ROEPER STEFANIE , RYAN MICHAEL P , YAP DAHRIKA MILFRED LAO , KRUEGER BRIAN R , GROOTENHUIS PETER D J , VAN GOOR FREDERICK F , BOTFIELD MARTYN C , ZLOKARNIK GREGOR
Abstract: The invention provides a process for the preparation of a compound of Formula 1; comprising coupling a carboxylic acid of Formula 2; with an aniline of Formula 3; in the presence of a coupling agent.
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公开(公告)号:AU2010226400A1
公开(公告)日:2011-10-06
申请号:AU2010226400
申请日:2010-03-19
Applicant: VERTEX PHARMA
Inventor: JOHN DEMATTEI , LOOKER ADAM R , BOBBIANNA NEUBERT-LANGILLE , MARTIN TRUDEAU , STEFANIE ROEPER , RYAN MICHAEL P , LAO YAP DAHRIKA MILFRED , KRUEGER BRIAN R , GROOTENHUIS PETER D J , GOOR FREDRICK F VAN , BOTFIELD MARTYN C , GREGOR ZLOKARNIK
IPC: C07D215/233
Abstract: The invention provides a process for the preparation of a compound of Formula 1; comprising coupling a carboxylic acid of Formula 2; with an aniline of Formula 3; in the presence of a coupling agent.
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公开(公告)号:AU2010226393A1
公开(公告)日:2011-10-06
申请号:AU2010226393
申请日:2010-03-19
Applicant: VERTEX PHARMA
Inventor: XIAOQING YANG , HADIDA RUAH SARA S , GROOTENHUIS PETER D J , GOOR FREDRICK F VAN , BOTFIELD MARTYN C , GREGOR ZLOKARNIK
IPC: C07D215/233 , A61K31/47 , A61P3/00
Abstract: This invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R is COOH or CHOH.
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公开(公告)号:MX2011004374A
公开(公告)日:2011-05-23
申请号:MX2011004374
申请日:2009-10-23
Applicant: VERTEX PHARMA
Inventor: GROOTENHUIS PETER D J , ZHANG BEILI , KRAWIEC MARIUSZ , BOTFIELD MARTYN , GOOR FREDRICK VAN
IPC: C07D215/56 , A61K31/4704 , A61P1/00 , A61P11/00
Abstract: La presente invención se refiere a formas en estado sólido sustancialmente cristalinas y libres de N-(4-7-azabiciclo[2,2,1]he ptan-7-il)-2-(trifluorometil)fenil)-4-oxo-5- (trifluorometil)-1,4- dihidroquinolin-3-carboxamida (Forma A), sus composiciones farmacéuticas y métodos de tratamiento con ellas.
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