NL8004534A - Geneesmiddel. - Google Patents
Geneesmiddel. Download PDFInfo
- Publication number
- NL8004534A NL8004534A NL8004534A NL8004534A NL8004534A NL 8004534 A NL8004534 A NL 8004534A NL 8004534 A NL8004534 A NL 8004534A NL 8004534 A NL8004534 A NL 8004534A NL 8004534 A NL8004534 A NL 8004534A
- Authority
- NL
- Netherlands
- Prior art keywords
- chloridarol
- compound
- normo
- improving
- medicament according
- Prior art date
Links
- KBFBRIPYVVGWRS-UHFFFAOYSA-N cloridarol Chemical compound C=1C2=CC=CC=C2OC=1C(O)C1=CC=C(Cl)C=C1 KBFBRIPYVVGWRS-UHFFFAOYSA-N 0.000 claims description 11
- 229960001261 cloridarol Drugs 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 5
- 150000001875 compounds Chemical class 0.000 claims description 4
- 239000008280 blood Substances 0.000 claims description 2
- 210000004369 blood Anatomy 0.000 claims description 2
- 238000000034 method Methods 0.000 claims 2
- 239000013543 active substance Substances 0.000 claims 1
- 229940127218 antiplatelet drug Drugs 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 6
- 241000700159 Rattus Species 0.000 description 2
- 235000012000 cholesterol Nutrition 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 150000003626 triacylglycerols Chemical class 0.000 description 2
- XTWYTFMLZFPYCI-KQYNXXCUSA-N 5'-adenylphosphoric acid Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](COP(O)(=O)OP(O)(O)=O)[C@@H](O)[C@H]1O XTWYTFMLZFPYCI-KQYNXXCUSA-N 0.000 description 1
- 229930091371 Fructose Natural products 0.000 description 1
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 1
- 239000005715 Fructose Substances 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000000378 dietary effect Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 208000006575 hypertriglyceridemia Diseases 0.000 description 1
- 231100001231 less toxic Toxicity 0.000 description 1
- 230000000444 normolipidemic effect Effects 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 1
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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
-
- 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
-
- 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
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Furan Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
Description
Λ i' \ i ί j VO 868
Betr.: Geneesmiddel.
De uitvinding Betreft een nieuwe therapeutische toepassing als normo-lipidemme-middel en plaatjes-antibindmiddel van de verbinding (2-benzofuryl)-(p-chloorfenyl)-carbinol met de formule 1 van het formuleblad, dat ook wel wordt aangeduid als chloridarol. Dit chlori-5 darol is reeds vermeld in het Britse octrooischrift 1.ΐ6θ.925, Belgisch octrooischrift 6½. 179 en Spaans octrooischrift 296.706,
Er werd nu gevonden, dat behalve de reeds bekende hart-eigen-schappen van deze verbinding, chloridarol ook een duidelijk normo-lipidemie en plaatjes-antibindingseffeet heeft.
10 Farmacologische proef
De normo-lipidemie-activiteit werd onderzocht met de fructose-hyperglyceridémieproef bij ratten volgens Nikkila en Ojola, Life Sci. i, 937 (1965).
De plaatjes-antibindingsactivitext werd onderzocht met een proef 15 die de variatie in het aantal plaatjes in circulatie na toediening van adenosinedifosforzuur bij ratten meet, volgens De Gaetano en Cavenaghi, Thrambosio Res. 10, 525 (1977).
Bij beide proeven vertoont chloridarol een activiteit, die vergelijkbaar is met die van chbfibrate. Chloridarol is echter tenminste 20 tweemaal zo weinig giftig als chlofibrate.
Clinische proef
Een behandeling met chloridarol in doses van 250 tot 2500 mg/dag van 200 patiënten met dislipidemie-syndremen en hoge plasmaspiegels aan triglyceriden en cholesterol, die niet verminderd konden worden door 25 een dieetbehandelingfwerd uitgevoerd. De verkregen resultaten bewezen, dat het produkt chloridarol het gehalte van het bloed aan triglyceride en cholesterol statistisch en clinisch significant verlaagt. De patiënten behandeld met chloridarol in de bovenweergegeven doses vertoonden reeds na een behandeling van 15 dagen tot 3 maanden een ver-30 laging van de cholesterolspiegel van 12 tot 30$ van de aanvangswaarde en van triglyceriden tussen 15 en 50$ van de aanvangswaarden.
Dit geneesmiddel kan gedurende een lange tijd worden toegediend, omdat het geen invloed op de functies van de belangrijkste organen en kanalen heeft.
800 4 5 34 35
Claims (4)
1. De verbinding (2-benzofuryl)-(p-chloorfenyl)-carbinol met de formule 1, indien gebruikt bij een therapie als normo-lipidemie- en plaatj e s-antihindingsmiddel.
2. Geneesmiddel met daarin de bovenweergegeven verbinding als ac-5 tieve stof in ccmbinatie met. dragers en/of excipiëntia.
3. Geneesmiddel volgens conclusie 2 in een passende vorm voor orale, parenterale of rectale toediening. U. Geneesmiddel volgens conclusie 2 of 3 in de vorm van eenheids-doseringen. 10 5· Werkwijze voor het verbeteren van de bloed-lipidespiegel door toediening van chloridarol.
6. Werkwijze voor het verbeteren van de plaatjes-bindingseigenschap-pen door toediening van chloridarol. * 800 45 34 ~ί* { ^ _π ΟΗ 3004534 A. Ifenarini S.A.4.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT7909513A IT1207887B (it) | 1979-08-10 | 1979-08-10 | Uso in terapia del prodotto (2benzofuril)-(p-clorofenil)-carbino lo(cloridarol dci)come normolipide mizzante e antiaggregante piastrinico |
| IT951379 | 1979-08-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NL8004534A true NL8004534A (nl) | 1981-02-12 |
Family
ID=11131363
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NL8004534A NL8004534A (nl) | 1979-08-10 | 1980-08-08 | Geneesmiddel. |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US4296124A (nl) |
| JP (1) | JPS5645413A (nl) |
| BE (1) | BE884691A (nl) |
| CA (1) | CA1155395A (nl) |
| CH (1) | CH648756A5 (nl) |
| DE (1) | DE3029421A1 (nl) |
| FR (1) | FR2463135A1 (nl) |
| GB (1) | GB2056280A (nl) |
| IT (1) | IT1207887B (nl) |
| LU (1) | LU82700A1 (nl) |
| NL (1) | NL8004534A (nl) |
| ZA (1) | ZA804822B (nl) |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1160925A (en) * | 1967-02-08 | 1969-08-06 | Menarini Sas | 2-Substituted Benzofuran Derivatives |
-
1979
- 1979-08-10 IT IT7909513A patent/IT1207887B/it active
-
1980
- 1980-08-01 GB GB8025197A patent/GB2056280A/en not_active Withdrawn
- 1980-08-02 DE DE19803029421 patent/DE3029421A1/de active Granted
- 1980-08-07 ZA ZA00804822A patent/ZA804822B/xx unknown
- 1980-08-08 NL NL8004534A patent/NL8004534A/nl not_active Application Discontinuation
- 1980-08-08 CH CH6040/80A patent/CH648756A5/it not_active IP Right Cessation
- 1980-08-08 LU LU82700A patent/LU82700A1/fr unknown
- 1980-08-08 JP JP10839080A patent/JPS5645413A/ja active Granted
- 1980-08-08 BE BE0/201683A patent/BE884691A/fr not_active IP Right Cessation
- 1980-08-11 FR FR8017691A patent/FR2463135A1/fr active Granted
- 1980-08-11 CA CA000357982A patent/CA1155395A/en not_active Expired
- 1980-08-11 US US06/176,867 patent/US4296124A/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| CH648756A5 (it) | 1985-04-15 |
| IT1207887B (it) | 1989-06-01 |
| JPH0153244B2 (nl) | 1989-11-13 |
| FR2463135B1 (nl) | 1983-08-12 |
| LU82700A1 (fr) | 1980-12-15 |
| JPS5645413A (en) | 1981-04-25 |
| US4296124A (en) | 1981-10-20 |
| FR2463135A1 (fr) | 1981-02-20 |
| IT7909513A0 (it) | 1979-08-10 |
| DE3029421A1 (de) | 1981-02-26 |
| CA1155395A (en) | 1983-10-18 |
| BE884691A (fr) | 1980-12-01 |
| ZA804822B (en) | 1981-08-26 |
| DE3029421C2 (nl) | 1990-02-22 |
| GB2056280A (en) | 1981-03-18 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A85 | Still pending on 85-01-01 | ||
| BA | A request for search or an international-type search has been filed | ||
| BB | A search report has been drawn up | ||
| BC | A request for examination has been filed | ||
| BV | The patent application has lapsed |