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    Pyridine derivatives as CFTR modulators, in particular N-(6-(benzylamino)-5-methylpyridin-2-yl)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamide
    76.
    发明专利
    Pyridine derivatives as CFTR modulators, in particular N-(6-(benzylamino)-5-methylpyridin-2-yl)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamide 未知

    公开(公告)号：NZ588006A

    公开(公告)日：2012-08-31

    申请号：NZ58800609

    申请日：2009-03-25

    Applicant: VERTEX PHARMA

    Inventor： HADIDA-RUAH SARA ,  MILLER MARK ,  ZHOU JINGLAN ,  BEAR BRIAN ,  GROOTENHUIS PETER

    IPC: C07D405/12 ,  A61K31/44 ,  A61K31/4427 ,  A61P43/00 ,  C07D213/75 ,  C07D405/14 ,  C07D413/14

    Abstract: Disclosed herein is N-(6-(benzylamino)-5-methylpyridin-2-yl)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamide or a pharmaceutically acceptable salt thereof, processes for its preparation, compositions comprising said compounds and uses thereof. Said compound is useful as modulators of ATP-Binding Cassette (ABE) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator ("CFTR"), as such are useful in the treatment of condition, disease, or disorder selected from cystic fibrosis, hereditary emphysema, hereditary hemochromatosis, coagulation-fibrinolysis deficiencies, protein C deficiency, Type 1 hereditary angioedema, lipid processing deficiencies, familial hypercholesterolemia, Type 1 chylomicronemia, abetalipoproteinemia, lysosomal storage diseases, I-cell disease/pseudo-Hurler, mucopolysaccharidoses, Sandhof/Tay-Sachs, Crigler-Najjar type II, polyendocrinopathy/hyperinsulemia, diabetes mellitus, laron dwarfism, myleoperoxidase deficiency, primary hypoparathyroidism, melanoma, glycanosis CDG type 1, hereditary emphysema, congenital hyperthyroidism, osteogenesis imperfecta, hereditary ypofibrinogenemia, ACT deficiency, diabetes insipidus (di), neurophyseal di, neprogenic DI, Charcot-Marie Tooth syndrome, Perlizaeus-Merzbacher disease, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, progressive supranuclear plasy, Pick's disease, Huntington, spinocerebullar ataxia type I, spinal and bulbar muscular atrophy, dentatorubal pallidoluysian, myotonic dystrophy, as well as spongiform encephalopathies, hereditary Creutzfeldt-Jakob disease, Fabry disease, Straussler-Scheinker syndrome, COPD, dry-eye disease, and Sjögren's disease.

    ISOQUINOLINE MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
    77.
    发明专利
    ISOQUINOLINE MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS 未知

    公开(公告)号：NZ585980A

    公开(公告)日：2012-04-27

    申请号：NZ58598008

    申请日：2008-11-14

    Applicant: VERTEX PHARMA

    Inventor： HADIDA RUAH SARA ,  MILLER MARK ,  ZHOU JINGLAN ,  BEAR BRIAN ,  GROOTENHUIS PETER D

    IPC: C07D405/12 ,  A61K31/472 ,  A61K31/4725 ,  A61P11/00 ,  C07D217/22 ,  C07D401/04 ,  C07D405/14

    Abstract: The disclosure relates to a substituted isoquinoline derivative of the structural formula shown herein and pharmaceutically acceptable salt thereof, which is useful as a modulator of ATP-Binding Cassette ("ABC") transporter activity, including Cystic Fibrosis Transmembrane Conductance Regulator ("CFTR"). Said substituted isoquinoline compound may be suitable for treating ABC transporter mediated diseases selected from cystic fibrosis, asthma, smoke induced COPD, chronic bronchitis, rhinosinusitis, constipation, pancreatitis, pancreatic insufficiency, male infertility caused by congenital bilateral absence of the vas deferens, mild pulmonary disease, idiopathic pancreatitis, allergic bronchopulmonary aspergillosis, liver disease, hereditary emphysema, hereditary hemochromatosis, coagulation-fibrinolysis deficiencies, lipid processing deficiencies, lysosomal storage diseases, Crigler-Najjar type II, polyendocrinopathy/hyperinsulemia, Diabetes mellitus, Laron dwarfism, myleoperoxidase 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 several polyglutamine neurological disorders as well as spongiform encephalopathies, COPD, dry-eye disease and Sjogren's disease.

    Amide indole derivatives as modulators of ATP-binding cassette transporters
    79.
    发明专利
    Amide indole derivatives as modulators of ATP-binding cassette transporters 未知

    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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