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EP0346408A1 - Utilisation de derives d'oxoquinazoline dans le traitement de l'hyperlipidemie - Google Patents

Utilisation de derives d'oxoquinazoline dans le traitement de l'hyperlipidemie

Info

Publication number
EP0346408A1
EP0346408A1 EP88909323A EP88909323A EP0346408A1 EP 0346408 A1 EP0346408 A1 EP 0346408A1 EP 88909323 A EP88909323 A EP 88909323A EP 88909323 A EP88909323 A EP 88909323A EP 0346408 A1 EP0346408 A1 EP 0346408A1
Authority
EP
European Patent Office
Prior art keywords
cooh
treatment
hyperlipidemia
compounds
tetrazol
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.)
Withdrawn
Application number
EP88909323A
Other languages
German (de)
English (en)
Inventor
Gerhard Rauber
Roland Stechert
Kurt Schromm
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 EP0346408A1 publication Critical patent/EP0346408A1/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14—Ortho-condensed systems

Definitions

  • the invention relates to the use of certain known oxoquinazoline derivatives in the treatment of hyperlipidemia.
  • Atherosclerosis plays a causal role in the genesis of various clinical pictures. So e.g. in the development of coronary artery disease, myocardial infarction and peripheral circulatory disorders.
  • Hyperlipidemia in particular hypercholesterolemia, is considered to be one of the main causes.
  • Numerous so-called lipid-lowering agents are commercially available for treating such an increase in blood lipid values. These are essentially divided into 3 groups:
  • Resorbierb 'are antilipidemic agents (clofibric acid and its derivatives, for example).
  • Non-absorbable antilipidemics e.g. cholestyramine and sitosterol.
  • a reduction in the total cholesterol content of about 20-25% can generally be expected when using the lipid-lowering agents.
  • R to R 4 have the following meaning:
  • R. and R 2 have the following meaning:
  • R 1 and R 2 have the following meaning:
  • R .. and R ⁇ have the following meaning:
  • the ingredients are processed in the usual way to tablets of 300 mg.
  • the ingredients are mixed well and the mixture is filled into 400 mg portions in gelatin capsules.
  • the compounds which can be used according to the invention for example the 11-oxo-II-H-pyrido- [2, l-b] -quinazoline-2-carboxylic acid and its salts, have the advantage of better tolerability. No treatment-specific side effects were found in the treatment of more than 1000 patients with this compound in another indication area.
  • the compounds are processed in the customary manner into customary pharmaceutical preparations.
  • Oral use is clearly in the foreground, preferably in the form of capsules; but all other oral dosage forms are also suitable, for example tablets, coated tablets, granules, suspensions, slow-release forms.
  • the dose per day is about 100-1000 mg; it can be administered in 1-3 single doses.
  • the result means an 18 percent reduction in total cholesterol.
  • a significant reduction in the triglyceride level was achieved with 100 mg / kg per day (in two identical doses), e.g. 34% reduction compared to the control in normolipemic rats.
  • the uric acid level was advantageously reduced by 38%. It is therefore possible to treat hyperlipidemia and hyperuricaemia with one substance. In this way, undesirable interactions, such as can occur in the otherwise necessary treatment with one active ingredient against hyperuricaemia and against hyperlipidaemia, can be avoided from the outset.

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

On utilise pour traiter l'hyperlipidémie des composés ayant les formules (I), (II), (III), (IV), dans lesquelles les résidus R1 à R4 ont la définition donnée dans la description, et se présentant sous forme de préparations galéniques usuelles.
EP88909323A 1987-10-15 1988-10-12 Utilisation de derives d'oxoquinazoline dans le traitement de l'hyperlipidemie Withdrawn EP0346408A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE3734909 1987-10-15
DE19873734909 DE3734909A1 (de) 1987-10-15 1987-10-15 Verwendung von oxochinazolinderivaten bei der behandlung der hyperlipidaemie

Publications (1)

Publication Number Publication Date
EP0346408A1 true EP0346408A1 (fr) 1989-12-20

Family

ID=6338388

Family Applications (2)

Application Number Title Priority Date Filing Date
EP88909323A Withdrawn EP0346408A1 (fr) 1987-10-15 1988-10-12 Utilisation de derives d'oxoquinazoline dans le traitement de l'hyperlipidemie
EP88117087A Expired - Lifetime EP0312076B1 (fr) 1987-10-15 1988-10-14 Emploi des dérivés de l'oxoquinazoline pour le traitement de l'hyperlipémie

Family Applications After (1)

Application Number Title Priority Date Filing Date
EP88117087A Expired - Lifetime EP0312076B1 (fr) 1987-10-15 1988-10-14 Emploi des dérivés de l'oxoquinazoline pour le traitement de l'hyperlipémie

Country Status (7)

Country Link
EP (2) EP0346408A1 (fr)
JP (1) JPH01132520A (fr)
KR (1) KR890701106A (fr)
DE (1) DE3734909A1 (fr)
DK (1) DK285589A (fr)
HU (1) HUT53289A (fr)
WO (1) WO1989003215A1 (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUT63629A (en) * 1992-03-03 1993-09-28 Sandoz Ag Process for producing substituted phenylquinazoline derivatives and pharmaceutical compositions comprising same
EP4259628A2 (fr) * 2020-12-10 2023-10-18 Merck Patent GmbH Matériaux pour dispositifs électroluminescents organiques
PT119467A (pt) * 2024-05-17 2025-11-17 Inst Superior Tecnico Método implementado por computador para avaliação da gravidade de uma estenose coronária em repouso ou sob hiperemia

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO8903215A1 *

Also Published As

Publication number Publication date
KR890701106A (ko) 1989-12-19
DK285589D0 (da) 1989-06-12
DE3734909A1 (de) 1989-04-27
EP0312076B1 (fr) 1991-09-25
HUT53289A (en) 1990-10-28
JPH01132520A (ja) 1989-05-25
HU886315D0 (en) 1990-09-28
EP0312076A1 (fr) 1989-04-19
WO1989003215A1 (fr) 1989-04-20
DK285589A (da) 1989-06-12

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Legal Events

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PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

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Effective date: 19890610

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Effective date: 19900921

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18D Application deemed to be withdrawn

Effective date: 19920108