CH648756A5 - (2-benzofuril)-(p-clorofenil)-carbinolo come normolipidemizzante e antiaggregante piastrinico. - Google Patents
(2-benzofuril)-(p-clorofenil)-carbinolo come normolipidemizzante e antiaggregante piastrinico. Download PDFInfo
- Publication number
- CH648756A5 CH648756A5 CH6040/80A CH604080A CH648756A5 CH 648756 A5 CH648756 A5 CH 648756A5 CH 6040/80 A CH6040/80 A CH 6040/80A CH 604080 A CH604080 A CH 604080A CH 648756 A5 CH648756 A5 CH 648756A5
- Authority
- CH
- Switzerland
- Prior art keywords
- cloridarol
- carbinol
- antiplatelet
- cholesterol
- activity
- Prior art date
Links
- 230000000702 anti-platelet effect Effects 0.000 title claims 3
- 239000003146 anticoagulant agent Substances 0.000 title claims 3
- 239000000561 aggregant Substances 0.000 title 1
- 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 8
- 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 claims 6
- 229960001261 cloridarol Drugs 0.000 claims 6
- 235000012000 cholesterol Nutrition 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 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 claims 2
- 241000700159 Rattus Species 0.000 claims 2
- 230000002776 aggregation Effects 0.000 claims 2
- 238000004220 aggregation Methods 0.000 claims 2
- 239000000969 carrier Substances 0.000 claims 2
- KNHUKKLJHYUCFP-UHFFFAOYSA-N clofibrate Chemical compound CCOC(=O)C(C)(C)OC1=CC=C(Cl)C=C1 KNHUKKLJHYUCFP-UHFFFAOYSA-N 0.000 claims 2
- 229960001214 clofibrate Drugs 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 230000000444 normolipidemic effect Effects 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 150000003626 triacylglycerols Chemical class 0.000 claims 2
- 229930091371 Fructose Natural products 0.000 claims 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 claims 1
- 239000005715 Fructose Substances 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 229940127218 antiplatelet drug Drugs 0.000 claims 1
- 230000036765 blood level Effects 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 235000005911 diet Nutrition 0.000 claims 1
- 230000000378 dietary effect Effects 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000001258 dyslipidemic effect Effects 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 230000007774 longterm Effects 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000000144 pharmacologic effect Effects 0.000 claims 1
- 230000036470 plasma concentration Effects 0.000 claims 1
- 239000000106 platelet aggregation inhibitor Substances 0.000 claims 1
- NCEXYHBECQHGNR-QZQOTICOSA-N sulfasalazine Chemical compound C1=C(O)C(C(=O)O)=CC(\N=N\C=2C=CC(=CC=2)S(=O)(=O)NC=2N=CC=CC=2)=C1 NCEXYHBECQHGNR-QZQOTICOSA-N 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 230000001988 toxicity Effects 0.000 claims 1
- 231100000419 toxicity Toxicity 0.000 claims 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 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)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (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
648756
2
Claims (4)
- RIVENDICAZIONI 1. Il composto costituito da (2-benzofuril)-(p-clorofenil)--carbinolo della formula ganti piastrinici.
- 2. Composizione farmaceutica comprendente il composto di cui alla rivendicazione 1 come ingrediente attivo in associazione con veicolanti o eccipienti.
- 3. Composizione secondo la rivendicazione 2, in forme di somministrazione orale, parenterale o rettale.
- 4. Composizione secondo le rivendicazioni 2 e 3, nelle forme e nei dosaggi unitari.La presente invenzione si riferisce ad una nuova utilizzazione in terapia quale normolipidemizzante e antiaggre-gante piastrinico del composto (2-benzofuril)-(p-clorofenil)--carbinolo (Cloridarol, DCI) della formula già oggetto di domanda di brevetto in Italia depositata in data 22.2.1963 n. 93 reg. 86 e oggetto dei brevetti U. I. n. 1 160 925, belga n. 644 176 e spagnolo n. 296 706 a nome di A. Menarmi S.a.s. Firenze.È stato scoperto infatti che oltre alle già note proprietà terapeutiche a livello cardiaco per le quali il suddetto prodotto è largamente impiegato in terapia in vari paesi, il Cloridarol esplica marcata attività normolipidemizzante 5 e antiaggregante piastrinico.Sperimentazione farmacologica L'attività normolipidemizzante è stata saggiata con il test della ipergliceridemia da fruttosio nel ratto secondo io E. A. Nikkila e K. Ojola, Life Sci., 4, 937 (1965).L'attività antiaggregante piastrinica è stata saggiata con il test che misura la variazione del numero di piastrine in circolo dopo somministrazione di ADP (acido adenosin difosforico) nel ratto secondò G. De Gaetano e A. E. Cave-15 naghi, Thrombosis Res. 10, 525 (1977).In entrambi i tests il Cloridarol esplica un'attività comparabile a quella del Clofibrate. Il Cloridarol presenta però una tossicità almeno due volte inferiore a quella del Clofibrate.20Sperimentazione clinica Sono stati trattati con cloridarol a dosi comprese tra 250 e 2500 mg/die, 200 pazienti previamente selezionati per essere portatori di sindromi dislipidemiche caratteriz-25 zate da un alto tasso plasmatico di trigliceridi e colesterolo non riducibili con trattamento dietetico. I risultati ottenuti documentano concordemente che il prodotto è dotato delle capacità di ridurre il tasso ematico dei trigliceridi e del colesterolo in modo statisticamente e clinicamente significa-30 tivo. I pazienti trattati con cloridarol alle dosi di cui sopra mostrano, già dopo un periodo di trattamento compreso tra 15 giorni e 3 mesi, una riduzione della colesterolemia compresa fra il 12 ed il 30% dei valori basali e della trigli-ceridemia compresa fra il 15 ed il 50% dei valori basali. 35 II farmaco può essere somministrato a lungo termine, dato che non altera la funzione dei principali organi e apparati.v
Applications Claiming Priority (1)
| 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CH648756A5 true CH648756A5 (it) | 1985-04-15 |
Family
ID=11131363
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CH6040/80A CH648756A5 (it) | 1979-08-10 | 1980-08-08 | (2-benzofuril)-(p-clorofenil)-carbinolo come normolipidemizzante e antiaggregante piastrinico. |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US4296124A (it) |
| JP (1) | JPS5645413A (it) |
| BE (1) | BE884691A (it) |
| CA (1) | CA1155395A (it) |
| CH (1) | CH648756A5 (it) |
| DE (1) | DE3029421A1 (it) |
| FR (1) | FR2463135A1 (it) |
| GB (1) | GB2056280A (it) |
| IT (1) | IT1207887B (it) |
| LU (1) | LU82700A1 (it) |
| NL (1) | NL8004534A (it) |
| ZA (1) | ZA804822B (it) |
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 LU LU82700A patent/LU82700A1/fr unknown
- 1980-08-08 CH CH6040/80A patent/CH648756A5/it not_active IP Right Cessation
- 1980-08-08 NL NL8004534A patent/NL8004534A/nl not_active Application Discontinuation
- 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 CA CA000357982A patent/CA1155395A/en not_active Expired
- 1980-08-11 US US06/176,867 patent/US4296124A/en not_active Expired - Lifetime
- 1980-08-11 FR FR8017691A patent/FR2463135A1/fr active Granted
Also Published As
| Publication number | Publication date |
|---|---|
| IT1207887B (it) | 1989-06-01 |
| FR2463135B1 (it) | 1983-08-12 |
| US4296124A (en) | 1981-10-20 |
| IT7909513A0 (it) | 1979-08-10 |
| NL8004534A (nl) | 1981-02-12 |
| BE884691A (fr) | 1980-12-01 |
| DE3029421A1 (de) | 1981-02-26 |
| DE3029421C2 (it) | 1990-02-22 |
| FR2463135A1 (fr) | 1981-02-20 |
| CA1155395A (en) | 1983-10-18 |
| JPH0153244B2 (it) | 1989-11-13 |
| GB2056280A (en) | 1981-03-18 |
| JPS5645413A (en) | 1981-04-25 |
| ZA804822B (en) | 1981-08-26 |
| LU82700A1 (fr) | 1980-12-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PL | Patent ceased |