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WO1994003173A1 - Utilisation de 8-(3-oxocyclopentyle)-1,3-dipropyle-7h-purine-2,6-dione pour le traitement symptomatique de la fibrose cystique - Google Patents

Utilisation de 8-(3-oxocyclopentyle)-1,3-dipropyle-7h-purine-2,6-dione pour le traitement symptomatique de la fibrose cystique Download PDF

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Publication number
WO1994003173A1
WO1994003173A1 PCT/EP1993/002000 EP9302000W WO9403173A1 WO 1994003173 A1 WO1994003173 A1 WO 1994003173A1 EP 9302000 W EP9302000 W EP 9302000W WO 9403173 A1 WO9403173 A1 WO 9403173A1
Authority
WO
WIPO (PCT)
Prior art keywords
group
methyl
coor
propyl
substituted
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.)
Ceased
Application number
PCT/EP1993/002000
Other languages
German (de)
English (en)
Inventor
Ulrike Küfner-Mühl
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.)
Boehringer Ingelheim International GmbH
Boehringer Ingelheim GmbH
Original Assignee
Boehringer Ingelheim International GmbH
Boehringer Ingelheim GmbH
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Boehringer Ingelheim International GmbH, Boehringer Ingelheim GmbH filed Critical Boehringer Ingelheim International GmbH
Publication of WO1994003173A1 publication Critical patent/WO1994003173A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine

Definitions

  • the present invention relates to the use of 8- (3- ⁇ xocyclopentyl) -1,3-dipropyl-7H-purine-2,6-dione in particular in R (+) - 8- (3-oxocyclopentyl) -1,3-dipropyl - 7H-purine-2,6-dione of its (-) - enantiomer and structure-like compound for the symptomatic treatment of cystic fibrosis.
  • A. antagonists the efflux of chloride ions from CF PAC cells increases. The cells originate from a pancreatic adenocarcinoma cell line which was isolated from patients suffering from cystic fibrosis (CF). The action of the xanthine could be reduced by agonists, e.g. 2-chloroadenosine can be blocked. Interestingly, an increase in efflux was only observed in cells from patients with cystic fibrosis.
  • R a cyclopentane or cyclohexane, substituted by methyl, ethyl, propyl, isopropyl, t-butyl, allyl, vinyl, phenyl or benzyl, where a hydroxyl group may be present as the geminal substituent;
  • R, R, CH 3 , C 2 H 5 or
  • R_ is a cyclopentanone or cyclohexanone
  • R 3 is a cycloalkane or cycloalkene with 4-8
  • Carbon atoms which may be a straight-chain or branched
  • Carbon atoms can be substituted, a cyclopentanone or cyclopentanol or
  • Cyclohexanone or cyclohexanol which is in the ⁇ -position to the keto or hydroxy group by C_ to C 4 alkenyl, C 3 or
  • CH _ 6NRo, .R 1 - Rb c equal to or different
  • CH 2 COOR 4 CH 2 OR 4 can be substituted, where R 4 can be hydrogen, methyl, ethyl or propyl
  • R hydrogen, an alkyl group having 1 to 3 carbon atoms, a cyclopropyl group, a cyclopentyl group, benzyl an allyl group, a propargyl group, a triphenylmethyl group;
  • Hydrogen an alkyl group having 1 to 3 carbon atoms; a cyclopropyl group, a benzyl group;
  • the compounds of general formula I can be administered orally, parenterally as suppositories or by inhalation.
  • the compounds are present as active ingredients in conventional dosage forms, e.g. in compositions consisting essentially of an inert pharmaceutical carrier and an effective dose of the active ingredient, e.g. Tablets, dragees, xapsules, wafers, powders, solutions, propellant mixtures, suspensions, emulsions, syrups, suppositories, etc.
  • An effective dose of the compounds in the indication claimed according to the invention is between 5 and 100 mg per dose, preferably between 10 and 50 mg for oral use.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

e invention concerns the use of 8-(3-oxocyclopentyl)-1,3-dipropyl-7H-purine-2,6-dione.\!
PCT/EP1993/002000 1992-08-01 1993-07-28 Utilisation de 8-(3-oxocyclopentyle)-1,3-dipropyle-7h-purine-2,6-dione pour le traitement symptomatique de la fibrose cystique Ceased WO1994003173A1 (fr)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
DE4225501 1992-08-01
DEP4225501.5 1992-08-01
DEP4230398.2 1992-09-11
DEP4230397.4 1992-09-11
DE4230397 1992-09-11
DE4230398 1992-09-11
DEP4236867.7 1992-10-31
DE4236867 1992-10-31

Publications (1)

Publication Number Publication Date
WO1994003173A1 true WO1994003173A1 (fr) 1994-02-17

Family

ID=27435547

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1993/002000 Ceased WO1994003173A1 (fr) 1992-08-01 1993-07-28 Utilisation de 8-(3-oxocyclopentyle)-1,3-dipropyle-7h-purine-2,6-dione pour le traitement symptomatique de la fibrose cystique

Country Status (1)

Country Link
WO (1) WO1994003173A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5646156A (en) * 1994-04-25 1997-07-08 Merck & Co., Inc. Inhibition of eosinophil activation through A3 adenosine receptor antagonism
WO1999038532A3 (fr) * 1998-01-28 1999-09-30 Link Technology Inc Methodes de traitement et de prevention de la fibrose et de la sclerose

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0374808A2 (fr) * 1988-12-22 1990-06-27 Boehringer Ingelheim Kg Dérivés de xanthine à activité antagoniste d'adénosine
WO1992000297A1 (fr) * 1990-06-22 1992-01-09 Boehringer Ingelheim Kg Nouveaux derives de xanthine

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0374808A2 (fr) * 1988-12-22 1990-06-27 Boehringer Ingelheim Kg Dérivés de xanthine à activité antagoniste d'adénosine
WO1992000297A1 (fr) * 1990-06-22 1992-01-09 Boehringer Ingelheim Kg Nouveaux derives de xanthine

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
PROC. NATL. ACAD. SCI. U.S.A., Vol. 89, No. 12, 15 June 1992, pages 5562-5566, O. EIDELMAN et al., "A1 Adenosine - Receptor Antagonists Activate Chloride Efflux From Cystic Fibrosis Cells". *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5646156A (en) * 1994-04-25 1997-07-08 Merck & Co., Inc. Inhibition of eosinophil activation through A3 adenosine receptor antagonism
WO1999038532A3 (fr) * 1998-01-28 1999-09-30 Link Technology Inc Methodes de traitement et de prevention de la fibrose et de la sclerose
US6117445A (en) * 1998-01-28 2000-09-12 Link Technology Inc. Methods for the prevention and treatment of fibrosis and sclerosis

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