WO1996005819A1 - Remede contre l'hypertension portale - Google Patents
Remede contre l'hypertension portale Download PDFInfo
- Publication number
- WO1996005819A1 WO1996005819A1 PCT/JP1995/001605 JP9501605W WO9605819A1 WO 1996005819 A1 WO1996005819 A1 WO 1996005819A1 JP 9501605 W JP9501605 W JP 9501605W WO 9605819 A1 WO9605819 A1 WO 9605819A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- sat
- portal hypertension
- portal
- therapeutic agent
- compound
- Prior art date
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
- A61K31/16—Amides, e.g. hydroxamic acids
Definitions
- the present invention relates to a novel therapeutic agent for portal vein hypertension.
- the increased portal vein pressure associated with cirrhosis increased blood flow to the venous vein diverging from the portal vein, leading to bleeding from esophageal varices.
- bleeding caused by various surgical procedures is being treated quite effectively, but medical needs for drug therapy to prevent bleeding are increasing. high.
- vasopressin a ⁇ -blocker
- nitrite a ⁇ -blocker
- vasopressin lowers organ blood flow by its vasoconstriction, it also lowers portal venous blood flow, but it is not always easy to use.
- the present invention relates to the treatment of portal hypertension, and more specifically, the formula (I) (I)
- the present invention relates to a therapeutic agent for portal hypertension, which comprises as an active ingredient a compound represented by the formula or a pharmaceutically acceptable salt thereof.
- the compound represented by the formula (I), which is an active ingredient of the therapeutic agent for portal hypertension of the present invention, is known as a compound having a vasodilator action, an antithrombotic action, and the like.
- No. 152366 is not known to be effective as a therapeutic agent for portal hypertension.
- Salts of the compound (I) used as an active ingredient in the present invention include, for example, alkali salts such as sodium salts and potassium salts.
- Lithium metal salts for example, alkaline earth metal salts such as calcium salts, ammonium salts; ethanolamine salts, triethynoleamine salts, and dicyclohexylene salts
- examples thereof include a salt with an inorganic base such as an organic amine salt such as a silamine salt and a salt with an organic base.
- the compound (I) used as an active ingredient in the present invention contains stereoisomers, and a representative one thereof is (Sat) 1-1 (E) 14-ethynolate 2 — [(E) —Hydroxy imino] 1 5—2 Troll 3—Hexane amide (this compound is hereinafter referred to as FK 409).
- the compound (I) used as an active ingredient in the present invention and its pharmaceutically acceptable salt are nitric oxide (NO) donors, and the release reaction is considered. Is considered to degrade rapidly after absorption from the gastrointestinal tract and release NO.The concentration of NO in the portal vein system is high, making it an excellent therapeutic agent for portal hypertension. .
- the therapeutic agent for portal hypertension of the present invention can be prepared, for example, by mixing it with an organic or inorganic carrier or excipient suitable for external use, oral administration, or parenteral administration. It can be used in the form of a solid, semi-solid or liquid pharmaceutical preparation containing the active substance of the invention of the present invention.
- the active ingredient can be used, for example, in tablets, pellets, capsules, suppositories, injections, solutions, emulsions, suspensions, and any other form suitable for use. It can be mixed with conventional, non-toxic, pharmaceutically acceptable carriers.
- Carriers used include water, glucose, saccharose, arabia, gum, gelatin, mannitol, starch paste, magnesium trisilicate, tar Norek, corn starch, keratin, colloid silica, sugar potato starch, urea, and other solid, semi-solid or liquid preparations It is a suitable carrier and may also contain adjuvants, stabilizers, thickening and coloring agents and fragrances. Pharmaceutical preparations may also contain preservatives or bacteriostats to maintain the activity of the active ingredient stably in the desired preparation.
- the active substance in the drug may be the desired one depending on the extent or condition of the disease. It is contained in an amount sufficient to exert a therapeutic effect.
- the therapeutic agent for portal hypertension of the present invention In applying the therapeutic agent for portal hypertension of the present invention to humans, it is preferable to administer it intravenously, intramuscularly or orally.
- the dosage or therapeutically effective amount of the compound of interest for this invention will vary depending on the age and condition of the individual patient to be treated, but will usually be about 0.1 per day. ⁇ 100mgZ kg is administered, and generally, on average, about 0.5mg, 1rag, 5rag, lOrag, 50mg, 100mg, 250mg, 500mg power is administered at a time.
- FK409 was used by weighing 10 mg, dissolving in 20 ml of physiological saline, and diluting with physiological saline below (2 nilZ kg).
- Ni cardipine which has a commercially available vasodilatory effect, was used, 50 mg of this was weighed, and suspended in 10 ml of 0.5% methyl senorelose. 2 ml / kg).
- test substances were administered through a tube inserted into the duodenum on a rat fasted about 17 hours ago.
- Liver tissue blood flow was measured with a probe from a multichannel laser flowmeter (PER I MED AB Made in Sweden) at about 1 cm from the edge of the outer left lobe. The contact was measured.
- PER I MED AB Made in Sweden a multichannel laser flowmeter
- the significance test was performed on the pre-dose value and the solvent (physiological saline) (Friedman + Dunnett test and K rusk 1-Wa11is + Dunnett t test, respectively).
- the agent of the present invention has an effect of effectively lowering portal vein pressure, and is useful as a new therapeutic agent for portal hypertension.
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
Excellent remède contre l'hypertension portale, renfermant le composé représenté par la formule générale (I), ou un sel médicalement acceptable comme principe actif.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP19518294 | 1994-08-19 | ||
JP6/195182 | 1994-08-19 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO1996005819A1 true WO1996005819A1 (fr) | 1996-02-29 |
Family
ID=16336820
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/JP1995/001605 WO1996005819A1 (fr) | 1994-08-19 | 1995-08-11 | Remede contre l'hypertension portale |
Country Status (1)
Country | Link |
---|---|
WO (1) | WO1996005819A1 (fr) |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS59152366A (ja) * | 1982-12-31 | 1984-08-31 | Fujisawa Pharmaceut Co Ltd | 新規ニトロ脂肪族化合物、その製造法およびその用途 |
-
1995
- 1995-08-11 WO PCT/JP1995/001605 patent/WO1996005819A1/fr active Application Filing
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS59152366A (ja) * | 1982-12-31 | 1984-08-31 | Fujisawa Pharmaceut Co Ltd | 新規ニトロ脂肪族化合物、その製造法およびその用途 |
Non-Patent Citations (1)
Title |
---|
PROC. NATL. ACAD. SCI. U.S.A., Vol. 90, No. 21, (1993), pages 10130-10134. * |
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