WO1996005819A1 - Remede contre l'hypertension portale - Google Patents

Remede contre l'hypertension portale Download PDF

Info

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
Application number
PCT/JP1995/001605
Other languages
English (en)
Japanese (ja)
Inventor
Keizo Yoshida
Yasuhiro Kita
Original Assignee
Fujisawa Pharmaceutical Co., Ltd.
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 Fujisawa Pharmaceutical Co., Ltd. filed Critical Fujisawa Pharmaceutical Co., Ltd.
Publication of WO1996005819A1 publication Critical patent/WO1996005819A1/fr

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.
PCT/JP1995/001605 1994-08-19 1995-08-11 Remede contre l'hypertension portale WO1996005819A1 (fr)

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)

* Cited by examiner, † Cited by third party
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
Title
PROC. NATL. ACAD. SCI. U.S.A., Vol. 90, No. 21, (1993), pages 10130-10134. *

Similar Documents

Publication Publication Date Title
US9907787B2 (en) Method of supplementing the diet and ameliorating oxidative stress
US8426368B2 (en) Method of ameliorating oxidative stress and supplementing the diet
JP2002511838A (ja) 肺高血圧症およびその他の適応症用の一酸化窒素供与化合物および医薬組成物
BRPI0818118B1 (pt) Composição farmacêutica na forma de uma suspensão aquosa estabilizada de carisbamato e seu processo de formação
JP3852621B2 (ja) 血管内皮細胞機能改善剤
JP2012515154A (ja) 鎮痛分子及び／または鎮痙分子を経口経粘膜投与するための処方物
CN101325952B (zh) 用于急性肾衰竭的预防和治疗剂
US5547970A (en) Use of leflunomide for inhibiting tumor necrosis factor alpha
JPH0531523B2 (fr)
JPWO2003006019A1 (ja) 間質性膀胱炎治療用医薬組成物
JP6679616B2 (ja) 炎症及び疼痛の治療のための組成物及び方法
PL169716B1 (pl) Sposób wytwarzania 9-(3-cyjanofenylo)-3,4,6,7,9,10-heksahydro-1,8-(2H,5H)akrydynodionu PL PL PL
JP5680412B2 (ja) レオヌリンの使用およびその組成物
EP1004316A1 (fr) Remedes contre les complications du diabete
Szczeklik et al. Asthmatic attacks induced in aspirin-sensitive patients by diclofenac and naproxen.
HU206186B (en) Process for producing pharmaceutical compositions comprising amino acid derivatives having ace-inhibiting effect
WO1996005819A1 (fr) Remede contre l'hypertension portale
JP2642198B2 (ja) 胃粘膜障害治療剤
JP3253878B2 (ja) 鉄キレート化用製剤、その製剤の製法及び地中海貧血症の治療法
WO1997038691A1 (fr) Medicament pour neuropathie retinienne
CH675074A5 (fr)
Pentland et al. Failure of ejaculation with indoramin.
JP2018504439A (ja) 粘膜炎の治療のための組成物及び方法
CN116650490A (zh) 化合物mt-1207在降低尿酸方面的应用
JP2004231557A (ja) エピネフリン含有抗腫瘍剤

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A1

Designated state(s): CA JP KR US

AL Designated countries for regional patents

Kind code of ref document: A1

Designated state(s): AT BE CH DE DK ES FR GB GR IE IT LU MC NL PT SE

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
121 Ep: the epo has been informed by wipo that ep was designated in this application
122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: CA