CA2500498C - Cystic fibrosis transmembrane conductance regulator protein inhibitors and uses thereof - Google Patents

Cystic fibrosis transmembrane conductance regulator protein inhibitors and uses thereof 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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CA
Canada
Prior art keywords
group
cftr
hydroxyl
nitro
compound
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CA2500498A
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English (en)
French (fr)
Other versions
CA2500498A1 (en
Inventor
Alan Verkman
Tonghui Ma
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of California San Diego UCSD
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University of California San Diego UCSD
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Filing date
Publication date
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/en
Application granted granted Critical
Publication of CA2500498C publication Critical patent/CA2500498C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Endocrinology (AREA)
  • Toxicology (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2500498A 2002-09-30 2003-09-30 Cystic fibrosis transmembrane conductance regulator protein inhibitors and uses thereof Expired - Fee Related CA2500498C (en)

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 (en) 2002-09-30 2003-09-30 Cystic fibrosis transmembrane conductance regulator protein inhibitors and uses thereof

Publications (2)

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

Family

ID=32044981

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2500498A Expired - Fee Related CA2500498C (en) 2002-09-30 2003-09-30 Cystic fibrosis transmembrane conductance regulator protein inhibitors and uses thereof

Country Status (13)

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

Cited By (1)

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US8796321B2 (en) 2008-04-21 2014-08-05 Path Drug Solutions Compounds, compositions and methods comprising oxadiazole derivatives

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US7645789B2 (en) 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
USRE50453E1 (en) 2006-04-07 2025-06-10 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US7776905B2 (en) 2006-04-07 2010-08-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US8283351B2 (en) 2007-04-02 2012-10-09 Institute For Oneworld Health Cyclic and acyclic hydrazine derivatives compositions including them and uses thereof
WO2009038913A2 (en) * 2007-08-24 2009-03-26 Vertex Pharmaceuticals Incorporated Isothiazolopyridinones useful for the treatment of (inter alia) cystic fibrosis
HRP20140103T1 (hr) 2007-11-16 2014-05-09 Vertex Pharmaceuticals Inc. Izokinolinski modulatori transportera atp-vežuä†e kazete
HUE031913T2 (en) 2007-12-07 2017-08-28 Vertex Pharma Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid
JP2011517674A (ja) * 2008-03-25 2011-06-16 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 嚢胞性線維症膜コンダクタンス制御因子の水溶性小分子阻害剤
DK2615085T3 (en) 2008-03-31 2015-10-05 Vertex Pharma Pyridyl derivatives as CFTR modulators
US8236838B2 (en) 2008-04-21 2012-08-07 Institute For Oneworld Health Compounds, compositions and methods comprising isoxazole derivatives
WO2010033626A1 (en) * 2008-09-19 2010-03-25 Institute For Oneworld Health Compounds, 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
WO2011048070A1 (en) * 2009-10-20 2011-04-28 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of disorders of glucose homeostasis
LT2826776T (lt) 2010-03-25 2021-01-11 Vertex Pharmaceuticals Incorporated (r)-1(2,2-difluorbenzo(d)(1,3)dioksol-5-il)-n-(1-(2,3-dihidroksipropil)-6-fluor-2-(1-hidroksi-2-metilpropan-2-il)-1h-indol-5-il)-ciklopropankarboksamido kieta amorfinės formos dispersija
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
NZ602795A (en) 2010-04-07 2015-01-30 Vertex Pharma Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
RS62767B1 (sr) 2010-04-07 2022-01-31 Vertex Pharma Farmaceutski sastavi 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il) ciklopropankarboksamido)-3-metilpiriodin-2-il)benzojeve kiseline i njihova primena
CN105130948A (zh) 2010-04-22 2015-12-09 弗特克斯药品有限公司 制备环烷基甲酰胺基-吲哚化合物的方法
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
US20120046330A1 (en) 2010-08-23 2012-02-23 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions 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 and administration thereof
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
WO2012153775A1 (ja) 2011-05-10 2012-11-15 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
RU2640420C2 (ru) 2011-11-08 2018-01-09 Вертекс Фармасьютикалз Инкорпорейтед Модуляторы транспортеров атф-связывающей кассеты
MX355183B (es) 2012-01-25 2018-04-09 Vertex Pharma Formulaciones de acido 3- (6- (1- (2.2- difluorobenzo [d] [1,3] dioxol-5-il) ciclopropancarboxamido) -3- metilpiridin-2-il) benzoico.
CA2878057A1 (en) 2012-07-16 2014-01-23 Rossitza Gueorguieva Alargova Pharmaceutical compositions 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 and administration thereof
SMT202500078T1 (it) 2012-11-02 2025-03-12 Vertex Pharma Composizioni farmaceutiche per il trattamento di malattie mediate da cftr
FR2999191B1 (fr) 2012-12-12 2016-02-05 Lesaffre & Cie Souches probiotiques pour le traitement et/ou la prevention de la diarrhee
JP6543268B2 (ja) 2014-04-15 2019-07-10 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Vertex Pharmaceuticals Incorporated 嚢胞性線維症膜コンダクタンス調節因子が媒介する疾患を処置するための医薬組成物
RS60906B1 (sr) 2014-10-06 2020-11-30 Vertex Pharma Modulatori regulatora transmembranske provodljivosti za cističnu fibrozu
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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WO2019018395A1 (en) 2017-07-17 2019-01-24 Vertex Pharmaceuticals Incorporated METHODS OF TREATING CYSTIC FIBROSIS
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Cited By (1)

* Cited by examiner, † Cited by third party
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

Also Published As

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

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