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    Morpholine-spirocyclic piperidine amides as modulators of ion channels
    33.
    发明专利
    Morpholine-spirocyclic piperidine amides as modulators of ion channels 未知

    公开(公告)号：NZ615014A

    公开(公告)日：2016-08-26

    申请号：NZ61501412

    申请日：2012-03-13

    Applicant: VERTEX PHARMA

    Inventor： KALLEL EDWARD ADAM ,  ARUMUGAM VIJAYALAKSMI ,  HILGRAF NICOLE ,  GROOTENHUIS PETER DIEDERIK JAN ,  MILLER MARK THOMAS ,  HADIDA-RUAH SARA SABINA ,  BINCH HAYLEY MARIE ,  DENINNO MICHAEL PAUL ,  FANNING LEV TYLER DEWEY ,  JOSHI PRAMOD ,  PONTILLO JOSEPH ,  SILINA ALINA ,  SHETH URVI JAGDISHBHAI ,  HURLEY DENNIS JAMES ,  FRIEMAN BRYAN A

    IPC: C07D498/10 ,  A61K31/438 ,  A61K31/5386 ,  A61P29/00

    Abstract: Disclosed are 1’-benzoyl-spiro[morpholine-2,4’-piperidine] derivatives and analogues as represented by the general formula (I) wherein the substituents are as defined herein. Representative compounds include 1’-(4-(3-hydroxypentan-3-yl)-3-methylbenzoyl)-4-(pyrimidin-2-yl)-6-ethyl-spiro[morpholine-2,4’-piperidine], 1’-(4-isopropoxy-3-methylbenzoyl)-4-(benzyl)-6-hydroxyethyl-spiro[morpholine-2,4’-piperidine], 1’-(4-(cyclopropyl(hydroxy)methyl)-benzoyl)-4-(2,2,2-trifluoroethyl)-6-phenyl-spiro[morpholine-2,4’-piperidine], 1’-(4-(isopropoxy)-3-methylbenzoyl)-4-(2-butyn-1-yl)-6-(2-fluoroethyl)-spiro[morpholine-2,4’-piperidine]. Also disclosed is a pharmaceutical composition comprising a compound as defined above and a pharmaceutically acceptable carrier, for inhibiting a voltage gated sodium ion channel, and for treating or lessening the severity of a condition selected from acute, chronic, neuropathic, or inflammatory pain, arthritis, migraine, cluster headaches, trigeminal neuralgia, herpatic neuralgia, general neuralgias, epilepsy or epilepsy conditions, neurodegenerative disorders, psychiatric disorders, anxiety, depression, dipolar disorder, myotonia, arrhythmia, movement disorders, neuroendocrine disorders, ataxia, multiple sclerosis, irritable bowel syndrome, incontinence, visceral pain, osteoarthritis pain, postherpetic neuralgia, diabetic neuropathy, radicular pain, sciatica, back pain, head or neck pain, severe or intractable pain, nociceptive pain, breakthrough pain, postsurgical pain, cancer pain, stroke, cerebral ischemia, traumatic brain injury, amyotrophic lateral sclerosis, stress- or exercise induced angina, palpitations, hypertension, migraine, and abnormal gastro-intestinal motility.

    Pharmaceutical compositions comprising cftr modulators and administrations thereof
    35.
    发明专利
    Pharmaceutical compositions comprising cftr modulators and administrations thereof 未知

    公开(公告)号：NZ603044A

    公开(公告)日：2015-08-28

    申请号：NZ60304411

    申请日：2011-04-22

    Applicant: VERTEX PHARMA

    Inventor： KESHAVARZ-SHOKRI ALI ,  NUMA MEHDI ,  ALCACIO TIM EDWARD ,  KRAWIEC MARIUSZ ,  KAUSHIK RITU ROHIT ,  ZAMAN NOREEN TASNEEM ,  BINCH HAYLEY MARIE ,  YOUNG CHRISTOPHER RYAN ,  FANNING LEV TYLER DEWEY ,  ZHANG YUEGANG ,  ZLOKARNIK GREGOR ,  KADIYALA IRINA NIKOLAEVNA ,  ZHANG BEILI ,  VAN GOOR FREDRICK F ,  SHETH URVI JAGDISHBHAI ,  SILINA ALINA ,  VERWIJS MARINUS JACOBUS ,  MEDEK ALES ,  LEE ELAINE CHUNGMIN ,  ALARGOVA ROSSITZA GUEORGUIEVA ,  BOTFIELD MARTYN CURTIS ,  GROOTENHUIS PETER DIEDERIK JAN ,  LUISI BRIAN ,  YANG XIAOQING ,  HURLEY DENNIS JAMES

    IPC: A61K31/443 ,  A61K31/36 ,  A61K31/402 ,  A61K31/407 ,  A61K31/4418 ,  A61K31/4709 ,  C07D213/75 ,  C07D215/233 ,  C07D215/56 ,  C07D317/46 ,  C07D487/08

    Abstract: Disclosed is a pharmaceutical composition comprising one of the following combinations: a) Compound 1 and Compound 2 Form I; b) Compound 1 Form A and Compound 2 Form I; c) Compound 1 Form A and Compound 2 Tablet Formulation; d) Compound 1 Form A-HCl and Compound 2 Form I; e) Compound 1 Form B-HCl and Compound 2 Form I; f) Compound 1 Form B, and Compound 2 Form I; g) Compound 1 Form A-HCl and Compound 2 Tablet Formulation; h) Compound 1 Form B-HCl and Compound 2 Tablet Formulation; and i) Compound 1 Form B, and Compound 2 Tablet Formulation, wherein Compound 1 is N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide; Compound 2 is lumacaftor (VX-809 / 3-{ 6-{ [1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropanecarbonyl]amino} -3-methylpyridin-2-yl} benzoic acid); Compound 1 Form A is characterized by a peak at about 7.9 degrees and a peak at about 11.9 degrees in an X-ray powder diffraction obtained using Cu K alpha radiation; Compound 1 Form A-HCl is characterized by a peak at about 7.1 degrees, a peak at about 8.2 degrees, a peak at about 14.1 degrees, and a peak at about 21.2 degrees in an X-ray powder diffraction obtained using Cu K alpha radiation; Compound 1 Form B-HCl is characterized by a peak at about 8.3 degrees, a peak at about 9.0 degrees, a peak at about 13.0 degrees, a peak at about 18.0 degrees, and a peak at about 23.0 degrees in an X-ray powder diffraction obtained using Cu K alpha radiation; Compound 1 Form B is characterized by a peak at about 6.7 degrees, a peak at about 10.0 degrees, a peak at about 11.2 degrees, a peak at about 13.4 degrees, a peak at about 24.2 degrees in an X-ray powder diffraction obtained using Cu K alpha radiation; Compound 2 Form I is characterized by the following peaks in an X-ray powder diffraction obtained using Cu K alpha radiation: a peak at 15.4 degrees, a peak at 16.3 degrees, and a peak at 14.5 degrees; and Compound 2 Tablet Formulation comprises: a. Compound 2 Form I in an amount ranging from about 20 wt% to about 80 wt% by weight of the composition; b. a filler comprising microcrystalline cellulose in an amount ranging from about 20 wt% to about 50 wt% by weight of the composition; c. a disintegrant comprising sodium croscarmellose sodium in an amount ranging from about 1 wt% to about 5 wt% by weight of the composition; d. a surfactant comprising sodium lauryl sulfate in an amount ranging from about 2 wt% to about 0.3 wt% by weight of the composition; e. a diluent comprising mannitol in an amount ranging from about 1 wt% to about 30 wt% by weight of the composition; f. a lubricant comprising magnesium stearate in an amount ranging from about 0.3 wt% to about 5 wt% by weight of the composition; and g. at least one of: a binder comprising polyvinylpyrrolidone in an amount ranging from about 0.1 wt% to about 5 wt% by weight of the composition and a glidant comprising colloidal silica in an amount ranging from about 0.05 wt% to about 2 wt% by weight of the composition, or Compound 2 Tablet Formulation comprises: a. about 30 wt% of Compound 2 Form I by weight of the composition; b. about 42 wt% of microcrystalline cellulose by weight of the composition; c. about 21 wt% of mannitol by weight of the composition; d. about 3 wt% of sodium croscarmellose sodium by weight of the composition; e. about 1 wt% of sodium lauryl sulfate by weight of the composition; f. about 2.5 wt% of magnesium stearate by weight of the composition; and g. about 0.5 wt% of colloidal silica by weight of the composition; wherein the composition is intended for use in treating a CFTR mediated disease in a human, wherein the CFTR mediated disease is 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 (CBAVD), mild pulmonary disease, idiopathic pancreatitis, allergic bronchopulmonary aspergillosis (ABPA), liver disease, hereditary emphysema, hereditary hemochromatosis, coagulation-fibrinolysis deficiencies, such as protein C deficiency, Type 1 hereditary angioedema, lipid processing deficiencies, such as familial hypercholesterolemia, Type 1 chylomicronemia, abetalipoproteinemia, lysosomal storage diseases, such as 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, congenital hyperthyroidism, osteogenesis imperfecta, hereditary hypofibrinogenemia, ACT deficiency, Diabetes insipidus (DI), neurophyseal DI, neprogenic DI, Charcot-Marie Tooth syndrome, Perlizaeus-Merzbacher disease, neurodegenerative diseases such as Alzheimer’s disease, Parkinson’s disease, amyotrophic lateral sclerosis, progressive supranuclear plasy, Pick’s disease, several polyglutamine neurological disorders such as Huntington’s, spinocerebullar ataxia type I, spinal and bulbar muscular atrophy, dentatorubal pallidoluysian, and myotonic dystrophy, as well as spongiform encephalopathies, such as hereditary Creutzfeldt-Jakob disease (due to prion protein processing defect), Fabry disease, Straussler-Scheinker syndrome, COPD, dry-eye disease, or Sjogren’s disease, Osteoporosis, Osteopenia, bone healing and bone growth (including bone repair, bone regeneration, reducing bone resorption and increasing bone deposition), Gorham’s Syndrome, chloride channelopathies such as myotonia congenita (Thomson and Becker forms), Bartter’s syndrome type III, Dent’s disease, hyperekplexia, epilepsy, lysosomal storage disease, Angelman syndrome, and Primary Ciliary Dyskinesia (PCD), a term for inherited disorders of the structure and/or function of cilia, including PCD with situs inversus (also known as Kartagener syndrome), PCD without situs inversus and ciliary aplasia.

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