CA2500498C - Inhibiteurs de proteine regulant la permeabilite transmembranaire de la fibrose kystique (cftr) et uitlisations - Google Patents

Inhibiteurs de proteine regulant la permeabilite transmembranaire de la fibrose kystique (cftr) et uitlisations Download PDF

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Publication number
CA2500498C
CA2500498C CA2500498A CA2500498A CA2500498C CA 2500498 C CA2500498 C CA 2500498C CA 2500498 A CA2500498 A CA 2500498A CA 2500498 A CA2500498 A CA 2500498A CA 2500498 C CA2500498 C CA 2500498C
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Prior art keywords
group
cftr
hydroxyl
nitro
compound
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Expired - Fee Related
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CA2500498A
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English (en)
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CA2500498A1 (fr
Inventor
Alan Verkman
Tonghui Ma
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University of California San Diego UCSD
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University of California San Diego UCSD
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Priority claimed from US10/262,573 external-priority patent/US20040063695A1/en
Application filed by University of California San Diego UCSD filed Critical University of California San Diego UCSD
Publication of CA2500498A1 publication Critical patent/CA2500498A1/fr
Application granted granted Critical
Publication of CA2500498C publication Critical patent/CA2500498C/fr
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/549—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Endocrinology (AREA)
  • Toxicology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

L'invention concerne des compositions, des préparations pharmaceutiques et des procédés permettant d'inhiber la protéine CFTR, utiles pour l'étude et le traitement des maladies dont la médiation est assurée par la protéine CFTR. Les compositions et les préparations pharmaceutiques peuvent comprendre un ou plusieurs composés thiazolidinone, et par ailleurs un ou plusieurs vecteurs, excipients et/ou adjuvants pharmaceutiquement acceptables. Les procédés consistent, selon certaines variantes, à administrer au patient soufrant d'une maladie ou d'une affection dont la médiation est assurée par la protéine CFTR une quantité efficace de composé thiazolidinone. Sous d'autres variantes, on décrit des procédés inhibant la protéine CFTR qui consistent à mettre en contact des cellules du patient avec une quantité efficace de composé thiazolidinone. L'invention concerne également un modèle animal non humain de maladie dont la médiation est assurée par la protéine CFTR, résultant de l'administration d'un composé thiazolidinone à un animal non humain, en quantité suffisante pour inhiber la protéine CFTR.
CA2500498A 2002-09-30 2003-09-30 Inhibiteurs de proteine regulant la permeabilite transmembranaire de la fibrose kystique (cftr) et uitlisations Expired - Fee Related CA2500498C (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US10/262,573 US20040063695A1 (en) 2002-09-30 2002-09-30 Cystic fibrosis transmembrane conductance regulator protein inhibitors and uses thereof
US10/262,573 2002-09-30
US48025303P 2003-06-20 2003-06-20
US60/480,253 2003-06-20
PCT/US2003/031005 WO2004028480A2 (fr) 2002-09-30 2003-09-30 Inhibiteurs de proteine regulant la permeabilite transmembranaire de la fibrose kystique (cftr) et uitlisations

Publications (2)

Publication Number Publication Date
CA2500498A1 CA2500498A1 (fr) 2004-04-08
CA2500498C true CA2500498C (fr) 2012-08-21

Family

ID=32044981

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2500498A Expired - Fee Related CA2500498C (fr) 2002-09-30 2003-09-30 Inhibiteurs de proteine regulant la permeabilite transmembranaire de la fibrose kystique (cftr) et uitlisations

Country Status (13)

Country Link
EP (1) EP1549321A4 (fr)
JP (1) JP4977319B2 (fr)
KR (1) KR20050061501A (fr)
CN (1) CN100356922C (fr)
AP (1) AP2005003292A0 (fr)
AU (1) AU2003277162C1 (fr)
BR (1) BR0314943A (fr)
CA (1) CA2500498C (fr)
EA (1) EA009847B1 (fr)
MX (1) MXPA05003366A (fr)
NZ (1) NZ538809A (fr)
PL (1) PL376147A1 (fr)
WO (1) WO2004028480A2 (fr)

Cited By (1)

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Publication number Priority date Publication date Assignee Title
US8796321B2 (en) 2008-04-21 2014-08-05 Path Drug Solutions Compounds, compositions and methods comprising oxadiazole derivatives

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USRE50453E1 (en) 2006-04-07 2025-06-10 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
NZ611485A (en) 2006-04-07 2014-09-26 Vertex Pharma Modulators of atp-binding cassette transporters
US7645789B2 (en) 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
WO2008121877A2 (fr) 2007-04-02 2008-10-09 Institute For Oneworld Health Composés inhibiteurs de cftr et leurs utilisations
HUE028426T2 (en) * 2007-08-24 2016-12-28 Vertex Pharma Isothiazolopyridinones for (inter alia) treating cystic fibrosis
WO2009064959A1 (fr) 2007-11-16 2009-05-22 Vertex Pharmaceuticals Incorporated Modulateurs d'isoquinoléine de transporteurs de cassette de liaison à l'atp
NZ585880A (en) 2007-12-07 2012-08-31 Vertex Pharma Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3] dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid
MX2010010343A (es) * 2008-03-25 2010-10-15 Univ California Inhibidores solubles en agua de molecula pequeña del regulador de conductancia transmembrana de fibrosis quistica.
US8227615B2 (en) 2008-03-31 2012-07-24 Vertex Pharmaceutical Incorporated Pyridyl derivatives as CFTR modulators
US8236838B2 (en) 2008-04-21 2012-08-07 Institute For Oneworld Health Compounds, compositions and methods comprising isoxazole derivatives
US20110237528A1 (en) * 2008-09-19 2011-09-29 Institute For Oneworld Health Compositions and methods comprising imidazole and triazole derivatives
US8343976B2 (en) 2009-04-20 2013-01-01 Institute For Oneworld Health Compounds, compositions and methods comprising pyrazole derivatives
US20120219543A1 (en) * 2009-10-20 2012-08-30 Raphael Scharfmann Methods and pharmaceutical compositions for the treatment of disorders of glucose homeostasis
NZ700556A (en) 2010-03-25 2016-04-29 Vertex Pharma Solid forms of (r)-1(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-n-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl) cyclopropanecarboxamide
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
DK2555754T3 (en) 2010-04-07 2016-04-18 Vertex Pharma Solid forms of 3- (6- (1- (2,2-difluoro-benzo [d] [1,3] dioxol-5-yl) cyclopropanecarboxamido) -3-methylpyridin-2-yl) -benzoic acid
ES3017582T3 (en) 2010-04-07 2025-05-13 Vertex Pharma Pharmaceutical compositions of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyriodin-2-yl)benzoic acid and administration thereof
SG10201913594UA (en) 2010-04-22 2020-02-27 Vertex Pharma Process of producing cycloalkylcarboxamido-indole compounds
US8563593B2 (en) 2010-06-08 2013-10-22 Vertex Pharmaceuticals Incorporated Formulations of (R)-1-(2,2-difluorobenzo[D] [1,3] dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide
JP2013536231A (ja) 2010-08-23 2013-09-19 バーテックス ファーマシューティカルズ インコーポレイテッド （ｒ）−１−（２，２−ジフルオロベンゾ［ｄ］［１，３］ジオキソール−５−イル）−ｎ−（１−（２，３−ジヒドロキシプロピル）−６−フルオロ−２−（１−ヒドロキシ−２−メチルプロパン−２−イル）−１ｈ−インドール−５−イル）シクロプロパンカルボキサミドを含む医薬組成物およびその投与
CN102133402B (zh) * 2011-03-24 2013-06-12 首都医科大学附属北京同仁医院 囊性纤维化跨膜转导调节因子抑制剂在制备治疗糖尿病药物中的应用
JP6014816B2 (ja) 2011-05-10 2016-10-26 国立大学法人神戸大学 Ｒａｓ機能阻害作用を有するチオキソチアゾリジン誘導体
CN104039775B (zh) 2011-11-08 2017-03-01 弗特克斯药品有限公司 Atp‑结合盒转运蛋白的调节剂
CN108066306B (zh) 2012-01-25 2021-09-07 沃泰克斯药物股份有限公司 药物制剂及其制备方法
AU2013290444B2 (en) 2012-07-16 2018-04-26 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (R)-1-(2,2-diflurorbenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl) cyclopropanecarboxamide and administration thereof
HUE070382T2 (hu) 2012-11-02 2025-06-28 Vertex Pharma Gyógyászati készítmények CFTR közvetített betegségek kezelésére
FR2999191B1 (fr) 2012-12-12 2016-02-05 Lesaffre & Cie Souches probiotiques pour le traitement et/ou la prevention de la diarrhee
MX387720B (es) 2014-04-15 2025-03-12 Vertex Pharma Composiciones farmacéuticas para el tratamiento de enfermedades mediadas por el regulador de conductancia de transmembrana de fibrosis quística.
CN112250627B (zh) 2014-10-06 2024-02-02 弗特克斯药品有限公司 囊性纤维化跨膜转导调节因子调节剂
CN104398509B (zh) * 2014-11-13 2017-01-11 四川大学华西第二医院 CFTR抑制剂CFTRinh-172在制备防治白血病细胞介导的疾病的药物中的应用
CN104788423B (zh) * 2015-03-13 2016-10-26 成都理工大学 一种新的囊性纤维化跨膜传导调节因子抑制剂
ES2901002T3 (es) 2015-12-24 2022-03-21 Univ California Derivados de N-[5-[(3,4-dimetoxifenil)metil]-1,3,4-tiadiazol-2-il]-2-metoxi-bencenoacetamida y compuestos relacionados como activadores de CFTR para tratar estreñimiento o colestasis
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* Cited by examiner, † Cited by third party
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Also Published As

Publication number Publication date
AU2003277162A1 (en) 2004-04-19
CA2500498A1 (fr) 2004-04-08
WO2004028480A2 (fr) 2004-04-08
KR20050061501A (ko) 2005-06-22
EP1549321A2 (fr) 2005-07-06
JP2006503853A (ja) 2006-02-02
CN1684686A (zh) 2005-10-19
EA009847B1 (ru) 2008-04-28
AU2003277162C1 (en) 2009-12-24
NZ538809A (en) 2008-06-30
EA200500583A1 (ru) 2005-12-29
EP1549321A4 (fr) 2007-05-23
CN100356922C (zh) 2007-12-26
WO2004028480A3 (fr) 2004-07-01
BR0314943A (pt) 2005-08-02
AP2005003292A0 (en) 2005-06-30
MXPA05003366A (es) 2005-10-05
PL376147A1 (en) 2005-12-27
AU2003277162B2 (en) 2009-07-16
JP4977319B2 (ja) 2012-07-18

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