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WO1994010977A1 - Compose pharmaceutique anti-microbien et induisant des interferons - Google Patents

Compose pharmaceutique anti-microbien et induisant des interferons Download PDF

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Publication number
WO1994010977A1
WO1994010977A1 PCT/RU1993/000209 RU9300209W WO9410977A1 WO 1994010977 A1 WO1994010977 A1 WO 1994010977A1 RU 9300209 W RU9300209 W RU 9300209W WO 9410977 A1 WO9410977 A1 WO 9410977A1
Authority
WO
WIPO (PCT)
Prior art keywords
πaρa
drug
hours
injections
chτο
Prior art date
Application number
PCT/RU1993/000209
Other languages
English (en)
Russian (ru)
Inventor
Nikolai Borisovich Leonidov
Nikolai Georgievich Selezenev
Original Assignee
Leonidov Nikolai B
Nikolai Georgievich Selezenev
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 Leonidov Nikolai B, Nikolai Georgievich Selezenev filed Critical Leonidov Nikolai B
Priority to US08/256,494 priority Critical patent/US5510387A/en
Priority to EP93922097A priority patent/EP0630644A4/fr
Priority to AU51212/93A priority patent/AU665127C/en
Publication of WO1994010977A1 publication Critical patent/WO1994010977A1/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C07C311/38—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
    • C07C311/39—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • 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
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide

Definitions

  • the claimed preparation for injections is predominantly water for injections.
  • the claimed medication can be used in the form of rectal candles, and this is useful, so that the content of the active substance is 12.5-17.5%.
  • any pharmaceutical base for candles can be used as a base.
  • the claimed medicinal product may be used for external use only, in combination with - 4 -
  • the claimed step-5 takes advantage of a high-potency-modifying activity (a pharmaceutical-aminobenzulfanilamide).
  • the claimed medical device does not have any annoying effect on its own.
  • the claimed preparation induces an infection in the serum of mice after 5 hours after administration (previous infection) with an activity of 40-80 units / ml, which takes up to 40-80 units / ml. ⁇ 72 hours ago, there was a decrease in rates in the world.
  • the inventive method is the following composition in wt /%: ⁇ -modification of para-aminobenzene sulfanes-amide - 2, 0; ⁇ polivinyl ⁇ i ⁇ - lidon - 3, 0; water for injection - other 12.61 + 3.1 13, 46 + 4, 14, 59 + 3, 9, 04 + 0, 81 , 84 + 0,
  • ⁇ ⁇ same v ⁇ emya is ⁇ lz ⁇ vanie zayavlyaem ⁇ g ⁇ ⁇ e ⁇ a ⁇ a in eg ⁇ ⁇ e ⁇ a ⁇ ev ⁇ iches ⁇ y d ⁇ ze, blag ⁇ - da ⁇ ya vys ⁇ y bi ⁇ d ⁇ s ⁇ u ⁇ n ⁇ s ⁇ i, m ⁇ zhe ⁇ usiliva ⁇ ba ⁇ e ⁇ i ⁇ s- ⁇ a ⁇ iches ⁇ e deys ⁇ vie ⁇ e ⁇ a ⁇ a ⁇ a and ⁇ em thus eg ⁇ ⁇ e ⁇ a ⁇ ev- 0 ⁇ iches ⁇ uyu e ⁇ e ⁇ ivn ⁇ s ⁇ .
  • the inventive product is found in the quality of an antimicrobial and internally induced drug.
  • the inventive preparation may be used in any pharmaceutical preparation.
  • the content of the active substance is 1.5–2.5 wt%.
  • the above studies on the selection of the optimal concentration of the active substance were shown in the declared range - eleven -
  • the claimed ⁇ e ⁇ a ⁇ a ⁇ for ine ⁇ tsy m ⁇ zhe ⁇ d ⁇ lni ⁇ el- n ⁇ s ⁇ de ⁇ zha ⁇ ⁇ livinil ⁇ i ⁇ lid ⁇ n niz ⁇ m ⁇ le ⁇ ulya ⁇ ny ⁇ i s ⁇ n ⁇ shenii ⁇ m ⁇ nen ⁇ v follows, in wt%: ⁇ is ⁇ alliches ⁇ aya ⁇ -m ⁇ di ⁇ i ⁇ atsiya ⁇ a ⁇ a amin ⁇ benz ⁇ lsul ⁇ anilamida-1, 5-2, 5 ⁇ livinil ⁇ i ⁇ lid ⁇ n niz ⁇ m ⁇ le ⁇ ulya ⁇ ny 2, 0-4, 0 ⁇ a ⁇ matsev ⁇ iches ⁇ y ⁇ azbavi ⁇ el ⁇ s ⁇ aln ⁇ e ⁇ vedenie ⁇ livinil ⁇ i ⁇ lid ⁇ na in s ⁇ s ⁇ av
  • the device is based on its indifference and ensuring the necessary sedimentary stability and absorbability
  • the inventive product can be used in the form of rectal candles, and, thus, the preferred content of the active material is 12.5–17.5 wt%.
  • the analysis of the above studies showed that the use of candles containing 12.5-17.5% of the active substance is secured by a 2.0 percent (2.0 percent).
  • any pharmaceutically acceptable base fat base, oil and other may be used. - 12 -
  • the inventive product can be used for other applications, and, as a result, it is a component that is in the form of a medium-mediated , 4-tetrahydroimidine and their mass ratio of 1: 1.
  • the claimed ⁇ e ⁇ a ⁇ a ⁇ in an ointment ⁇ isy ⁇ i for HA ⁇ uzhn ⁇ g ⁇ ⁇ imeneniya was is ⁇ y ⁇ an in ⁇ liniches ⁇ i ⁇ usl ⁇ viya ⁇ in naib ⁇ lee ⁇ yazhely ⁇ sluchaya ⁇ ⁇ udn ⁇ zazhivlyaemy ⁇ gn ⁇ yny ⁇ ⁇ an ⁇ azlichny ⁇ n ⁇ z ⁇ l ⁇ giches ⁇ i ⁇ ⁇ m ( ⁇ iches ⁇ i ⁇ ulcers ven ⁇ zn ⁇ g ⁇ ⁇ is ⁇ zhdeniya maly ⁇ d ⁇ 5 cm 2 and b ⁇ lshi ⁇ than 5 cm 2 and ⁇ az- me ⁇ v ⁇ sle ⁇ e ⁇ atsi ⁇ nny ⁇ gn ⁇ yny ⁇ ⁇ an).
  • Urological form of treatment Duration of treatment (days) and application of the known known ointment preparation
  • the manufacturing process of the product is carried out under aseptic conditions.
  • the resulting drug product for injections provides a special suspension with an optical density of 2, 3, after 5 minutes of failure, the value of an optical pressure of 2 is 2, 2
  • the Gynthological Control did not detect any changes in the domestic organizations. For example, 2.
  • the manufacturing process of the claimed product is carried out under aseptic conditions.
  • the Gynthological Control did not detect any changes in the domestic organizations.
  • mice were administered the claimed preparation in a dose of 50 mcg / 0.2 ml (1st group) and 5 mice in a dose of 150 mcg / 0, 2 ml (2nd group) were given an internal dose. Abandonment of arthritis after 5, 24 and 72 hours after the introduction of the drug. Connecting an appliance to the computer by removing the pressure from the circuit breaker is connected to the microphone.
  • mice The first group of mice was already 5 hours later at an average level of 40-80 units / ml, after 24 hours it was 160 units / ml and decreased to 20 units / ml for 72 hours.
  • the 2nd group was lively, after 5 hours after the introduction of the preparation, the level of the mixture was 80 units / ml, after 24 hours, it went up to 72 ml / d for 20 ml and increased to 20 ml.
  • Utilities are prepared by pouring. Each candle contains 0.3 g of the active substance and 1.7 g of the fat pharmaceutical product.
  • Obstruction from the ear vein takes place after 0.5, 1, 2, 4, 6 hours.
  • the concentration of the drug in the region is determined by the method of Prabssting-Gavrilov. Parallel tests are carried out with a pharmaceutical preparation for p-pa-aminobenzenesulfanilamide.
  • the maximum concentration is already after 0.5-1 hours after introduction and maintenance of the therapeutic concentration (in the range of 2-20 ⁇ g / ml) for 6 hours.
  • Ezinom has shown that there are no essential deviations from the normal normal structure.
  • the inventive drug possesses antimicrobial and interfering activity and is used in medical practice.

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (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

Composé pharmaceutique anti-microbien et induisant des interférons, contenant une substance active ainsi qu'un agent de dilution pharmaceutiquement adapté, dans lequel la substance active est une modification η cristalline de sulfanilamide de para-aminobenzole.
PCT/RU1993/000209 1992-11-16 1993-08-31 Compose pharmaceutique anti-microbien et induisant des interferons WO1994010977A1 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
US08/256,494 US5510387A (en) 1992-11-16 1993-08-31 Antimicrobial interferon-inducing medicament
EP93922097A EP0630644A4 (fr) 1992-11-16 1993-08-31 Compose pharmaceutique anti-microbien et induisant des interferons.
AU51212/93A AU665127C (en) 1992-11-16 1993-08-31 Anti-microbial and interferon-inducing pharmaceutical compound

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
RU92671814 1992-11-16
RU92-006718/14 1992-11-16
RU93401514 1993-01-20
RU93-004015/14 1993-01-20

Publications (1)

Publication Number Publication Date
WO1994010977A1 true WO1994010977A1 (fr) 1994-05-26

Family

ID=26653733

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/RU1993/000209 WO1994010977A1 (fr) 1992-11-16 1993-08-31 Compose pharmaceutique anti-microbien et induisant des interferons

Country Status (1)

Country Link
WO (1) WO1994010977A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0630644A4 (fr) * 1992-11-16 1996-02-28 Leonidov Nikolai B Compose pharmaceutique anti-microbien et induisant des interferons.

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2321283A1 (fr) * 1975-05-14 1977-03-18 Parcor Medicament nouveau a activite antibacterienne
FR2361103A1 (fr) * 1976-07-15 1978-03-10 Basf Ag Solutions de sulfonamide-trimethoprime
US4401663A (en) * 1981-06-30 1983-08-30 The Procter & Gamble Company Novel sulfonamide derivatives
DE3800256A1 (de) * 1987-01-08 1988-07-21 Squibb & Sons Inc Bioadhaesive suppositorienmassen
US5151265A (en) * 1987-11-03 1992-09-29 Genentech, Inc. Gamma interferon formulation

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2321283A1 (fr) * 1975-05-14 1977-03-18 Parcor Medicament nouveau a activite antibacterienne
FR2361103A1 (fr) * 1976-07-15 1978-03-10 Basf Ag Solutions de sulfonamide-trimethoprime
US4401663A (en) * 1981-06-30 1983-08-30 The Procter & Gamble Company Novel sulfonamide derivatives
DE3800256A1 (de) * 1987-01-08 1988-07-21 Squibb & Sons Inc Bioadhaesive suppositorienmassen
US5151265A (en) * 1987-11-03 1992-09-29 Genentech, Inc. Gamma interferon formulation

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of EP0630644A4 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0630644A4 (fr) * 1992-11-16 1996-02-28 Leonidov Nikolai B Compose pharmaceutique anti-microbien et induisant des interferons.

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