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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
  • A61P7/10—Antioedematous agents; Diuretics

Definitions

• the present invention relates to the use of 8- (3-oxocyclopentyl) -1,3-dipropyl 7H-purine-2, 6- .dione and structure-like xanthines as diuretics.
• Diuretics play an important role in the treatment of edema, hypertension and other diseases.
• All animals received an oral water load of 5 ml / 100 g body weight using a pharyngeal tube.
• KFM 19 was dissolved in water and administered together with the water load (1 ml solution, 4 ml water) orally in doses of 0.01, 0.03, 0.1 and 0.3 mg / kg by gavage.
• Control animals received 5 ml of water.
• the excreted urine volume was measured two and five hours after application; the sodium and potassium content was determined by flame photometry, the chloride content was determined mercurimetrically.
• These compounds can also be used to treat diseases caused by disturbed chloride ion transport.
• R3 is a residue selected from the group consisting of furan, tetrahydrofuran, tetrahydrofuranone, thiophene, dithiol, Dithian or tetrahydrop ran which can carry one of the following substituents methyl, ethyl, propyl, butyl, CHO, CH 2 OR 4 , CH 2 OR 7 , COOR 4 , CONR 5 Rg,
• R3 is 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 a , Rfc, CH 3 , C 2 H5 or R a and R] -. together -CH 2 -CH 2 -,
• R 3 is a cyclopentanone or cyclohexanone
• R 3 is a cycloalkane or cycloalkene with 4-8
• Carbon atoms which can optionally be substituted by a straight-chain or branched alkenyl group having 2 to 4 carbon atoms, a cyclopentanone or cyclopentanol or cyclohexanone or cyclohexanol, which are in the ⁇ -position to the keto or hydroxyl group by C to C 4 alkenyl, C3 or C 4 alkynyl , Benzyl, -CH CH 2 CN, (CH 2 ) 3 NR 5 R5 R 5 equal to or different), CH 2 C00R 4 , CH 2 0R 4 can be substituted, where R 4 can be hydrogen, methyl, ethyl or propyl;
• R 4 is hydrogen, an alkyl group with 1 to 3
• R5 is hydrogen, an alkyl group having 1 to 3 carbon atoms; a cyclopropyl group, a benzyl group;
• R 7 prolinoyl, CO- (CH 2 ) 0 - 3 -CH 3 ,
• Another object of the present invention is the combination of compounds of general formula I, especially the compounds mentioned by name with loop diuretics - for example furosemide, bumetamides and etacrynic acid.
• the compounds of general formula I can be administered orally or parenterally or as a suppository.
• 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, dragées, capsules, wafers, powders, solutions, 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)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Pharmacology & Pharmacy (AREA)
• Chemical & Material Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• Medicinal Chemistry (AREA)
• General Health & Medical Sciences (AREA)
• Epidemiology (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Hematology (AREA)
• Engineering & Computer Science (AREA)
• Diabetes (AREA)
• General Chemical & Material Sciences (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Applications Claiming Priority (3)

Publications (1)

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• 1992
  • 1992-11-13 DE DE4238367A patent/DE4238367A1/de not_active Withdrawn
• 1993
  • 1993-11-11 JP JP6511709A patent/JPH08503204A/ja active Pending
  • 1993-11-11 KR KR1019950701869A patent/KR950703964A/ko not_active Application Discontinuation
  • 1993-11-11 AU AU54650/94A patent/AU5465094A/en not_active Abandoned
  • 1993-11-11 US US08/436,220 patent/US5599817A/en not_active Expired - Fee Related
  • 1993-11-11 SK SK607-95A patent/SK60795A3/sk unknown
  • 1993-11-11 CZ CZ951235A patent/CZ123595A3/cs unknown
  • 1993-11-11 EP EP94900128A patent/EP0667777A1/de not_active Withdrawn
  • 1993-11-11 WO PCT/EP1993/003158 patent/WO1994011000A1/de not_active Application Discontinuation
  • 1993-11-11 PL PL93308992A patent/PL308992A1/xx unknown
  • 1993-11-11 CA CA002148473A patent/CA2148473A1/en not_active Abandoned
  • 1993-11-11 HU HU9501397A patent/HUT72496A/hu unknown
  • 1993-11-12 MX MX9307082A patent/MX9307082A/es unknown
  • 1993-11-12 ZA ZA938453A patent/ZA938453B/xx unknown
  • 1993-11-12 IL IL10758993A patent/IL107589A0/xx unknown
  • 1993-11-13 CN CN93114496A patent/CN1090493A/zh active Pending
• 1995
  • 1995-05-12 FI FI952311A patent/FI952311A0/fi not_active Application Discontinuation
  • 1995-05-16 BG BG99638A patent/BG99638A/xx unknown

Non-Patent Citations (1)

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