WO2005103014A1 - Sels de 2,4-dioxo-5-(2-hydroxy-3,5-dichloro-benzylidene)imino-1,3-pyrimidine - Google Patents

Sels de 2,4-dioxo-5-(2-hydroxy-3,5-dichloro-benzylidene)imino-1,3-pyrimidine Download PDF

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Publication number
WO2005103014A1
WO2005103014A1 PCT/RU2005/000216 RU2005000216W WO2005103014A1 WO 2005103014 A1 WO2005103014 A1 WO 2005103014A1 RU 2005000216 W RU2005000216 W RU 2005000216W WO 2005103014 A1 WO2005103014 A1 WO 2005103014A1
Authority
WO
WIPO (PCT)
Prior art keywords
activity
compounds
άϊά
substance
dioxo
Prior art date
Application number
PCT/RU2005/000216
Other languages
English (en)
Russian (ru)
Inventor
Viktor Veniaminovich Tets
Georgy Viktorovich Tets
Viktor Iosifovich Krutikov
Original Assignee
Viktor Veniaminovich Tets
Georgy Viktorovich Tets
Viktor Iosifovich Krutikov
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 Viktor Veniaminovich Tets, Georgy Viktorovich Tets, Viktor Iosifovich Krutikov filed Critical Viktor Veniaminovich Tets
Publication of WO2005103014A1 publication Critical patent/WO2005103014A1/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Definitions

  • the invention is related to medicine, and specifically to pharmaceuticals, and in short - to synthetic and biologically active derivatives.
  • Zayavlenn ⁇ e vesches ⁇ v ⁇ imee ⁇ vy ⁇ azhennuyu ⁇ iv ⁇ mi ⁇ bnuyu a ⁇ ivn ⁇ s ⁇ , na ⁇ avlennuyu, ⁇ eimusches ⁇ venn ⁇ , ⁇ iv ⁇ azlichny ⁇ g ⁇ ib ⁇ v and ⁇ a ⁇ zhe ne ⁇ y ⁇ ba ⁇ e ⁇ y, ⁇ s ⁇ eyshi ⁇ and vi ⁇ us ⁇ v and ⁇ a ⁇ zhe ⁇ bladae ⁇ ⁇ iv ⁇ u ⁇ levym and ⁇ iv ⁇ b ⁇ levym deys ⁇ viem.
  • amphotericin ⁇ which is extremely toxic and is a portable large number of patients.
  • the closest chemical approach is claimed to be - 2,4-dioxo-5-arylidenimine-1, 3-pyrimidine in general
  • This material has been selected by us as a matter of quality.
  • a disadvantage of this material is its low activity in relation to certain microorganisms - mycobacteriums and chlamydia.
  • the objective of the invention is the development of a new pragmativnogo product of a wide range of operations, possessing
  • X is selected from the group: ⁇ , ⁇ réelle, ⁇ 4 + 20 were obtained by the interaction of 5-aminouracil or its alkali metals with dichlorosalicylic aldehyde. ⁇ Canal As a part of the distributor, a mixture of ethanol-water 1: 1 was used. Products were obtained with yields above 90% of the process. Synthesis of sodium salt of 2,4-dioxo-5- (2-hydroxy-3,5-di-25 hydrochlorobenzylidene) imino-1, 3-pyrimidine: 0.04 g of sodium hydroxide and 20 ml of water were placed in a flask.
  • EXAMPLE 4 Separation of the therapeutic effect of the claimed substance on an experimental infection caused by grabs of food 5 Sa ⁇ a.
  • the study was conducted on free white mice weighing 24-26 g. A lively introduced internal strain of S. ayssa ⁇ ⁇ -18 in a quantity of 1 x 10 9 bakt / live.
  • Compound I was introduced internally. In addition to the analogous scheme, they entered into the historical process of the deterioration of sodium or natstatin. Well, every group included 10 animals. The introduction of the drug had been carried out before the death of the last living person in a commercial, untreated group.
  • Compound I was administered at a dose of 5 mg / kg internal dose.
  • the switch was entered in a similar fashion and in the same quantity.
  • the effectiveness of 15 actions was evaluated by the number of survivors who survived the death of the last live, who died in the outpatient community. On the 10th day, all infected animals were killed. Among the living, having received the compound I, all living things remained alive. Protection was 100%. ⁇ group lively,
  • Example 6 Separation of the effective activity of the declared substance. A group of 3 times estimated the time required for keeping the appliance away from the source of thermal radiation. The lengthening of the reaction time after the internal administration of the drug (30 mg / kg) is more than 50%, indicates the presence of analgesic activity. As a comparative measure, analgin (2 mg / kg) was used. The results of 15 studies are shown in table 9. Table 9 The analgesic effect of the claimed substance
  • Example 7 Determination of the availability of a declared substance of a toxicity. Matter was given to white non-linear mice weighing 20-25 g (for 5 males and 5 females in each of the tested groups), with a separate stomach tube (1000 mg / kg) or outside ⁇ for 14 days. The absence of symptoms, property toxic effects, and
  • the data provided are indicative of
  • Example 8 Distribution of the activity of a declared substance by means of a simple virus. Antiviral activity was studied in relation to the virus.
  • Example 10 The division of the activity of the declared substance with the use of large-scale and large-scale bacteria.
  • EXAMPLE 11 Separation of the anti-hazardous activity of the declared substance by the use of a test ( ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ).
  • EXAMPLE 13 Division of activity of declared substances by means of mixtures that cause damage to products. ⁇
  • Ban As a model, butter was used, in addition, the mixtures named in case of 12 in 5 quantities of 10 5 types of oil were added.
  • the compounds I, II, III were also added (they were ready for sale on 10> other materials).
  • Compounds were added in the amount of 200 or 300 mg / kg. We incubated at 37 ° C, every day making quantitative seeding for food media intended for household bacteria and mowing. At the end of the oil, a diluent, ⁇ , was added to the oil, which was used for the preparation of compounds. After 24 hours of incubation in the online business, there is an increase in the quantity of introduced microcircuits by 10 times.
  • the compounds containing the claimed compounds in the amount of 300 mg / kg,
  • the data received indicates the possibility of using the claimed substance for the sale of products.

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention se rapporte à la médecine, et plus particulièrement à la pharmacologie, et notamment aux dérivés bioactifs synthétiques de pyrimidine. Les sels de 2,4-dioxo-5-(2-hydroxy-3,5-dichloro-benzylidene)imino-1,3-pyrimidine correspondent à la formule générale (I), X étant choisi dans le groupe Na, K, NH4 +, ont une activité biologique dirigée principalement contre de différents champignons, virus et bactéries et peuvent s'utiliser également avec le même but en médecine vétérinaire, en cosmétique, en bâtiment et dans les industries alimentaire, du cuir, du bois et autres.
PCT/RU2005/000216 2004-04-20 2005-04-19 Sels de 2,4-dioxo-5-(2-hydroxy-3,5-dichloro-benzylidene)imino-1,3-pyrimidine WO2005103014A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
RU2004112573 2004-04-20
RU2004112573/04A RU2260590C1 (ru) 2004-04-20 2004-04-20 Соли 2,4-диоксо-5-(2-гидрокси-3,5-дихлорбензилиден)имино-1,3-пиримидина

Publications (1)

Publication Number Publication Date
WO2005103014A1 true WO2005103014A1 (fr) 2005-11-03

Family

ID=35196908

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/RU2005/000216 WO2005103014A1 (fr) 2004-04-20 2005-04-19 Sels de 2,4-dioxo-5-(2-hydroxy-3,5-dichloro-benzylidene)imino-1,3-pyrimidine

Country Status (2)

Country Link
RU (1) RU2260590C1 (fr)
WO (1) WO2005103014A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8987277B2 (en) 2010-12-06 2015-03-24 Viktor Veniaminovich Tets Fungicide
US9895371B2 (en) 2014-06-24 2018-02-20 Viktor Veniaminovich Tets Fungicidal agent
US10624892B2 (en) 2015-08-04 2020-04-21 Viktor Veniaminovich Tets Agent against fungal infections

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2669555C1 (ru) * 2018-01-19 2018-10-12 Федеральное государственное бюджетное образовательное учреждение высшего образования "Санкт-Петербургский государственный химико-фармацевтический университет" Министерства здравоохранения Российской Федерации (ФГБОУ ВО СПХФУ Минздрава России) 6-Оксо-1-фенил-2-(фениламино)-1,6-дигидропиримидин-4-олят натрия и способ его получения

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3361745A (en) * 1964-10-14 1968-01-02 Searle & Co 1-alkenyl-3-alkyl-6-amino-5-(substituted-methyleneamino)-1, 2, 3, 4-tetrahydro-2, 4-pyrimidinediones
WO2000029389A1 (fr) * 1998-11-18 2000-05-25 Elena Alexandrovna Izaxon 6-(3-carboxymethylphenyl)-amino-uracyle ayant une action biologique
RU2198166C2 (ru) * 1998-12-04 2003-02-10 Ашкинази Римма Ильинична 2,4-диоксо-5-арилиденимино-1,3-пиримидины

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3361745A (en) * 1964-10-14 1968-01-02 Searle & Co 1-alkenyl-3-alkyl-6-amino-5-(substituted-methyleneamino)-1, 2, 3, 4-tetrahydro-2, 4-pyrimidinediones
WO2000029389A1 (fr) * 1998-11-18 2000-05-25 Elena Alexandrovna Izaxon 6-(3-carboxymethylphenyl)-amino-uracyle ayant une action biologique
RU2198166C2 (ru) * 1998-12-04 2003-02-10 Ашкинази Римма Ильинична 2,4-диоксо-5-арилиденимино-1,3-пиримидины

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8987277B2 (en) 2010-12-06 2015-03-24 Viktor Veniaminovich Tets Fungicide
US9895371B2 (en) 2014-06-24 2018-02-20 Viktor Veniaminovich Tets Fungicidal agent
US10154996B2 (en) 2014-06-24 2018-12-18 Viktor Veniaminovich Tets Fungicidal agent
US10624892B2 (en) 2015-08-04 2020-04-21 Viktor Veniaminovich Tets Agent against fungal infections

Also Published As

Publication number Publication date
RU2260590C1 (ru) 2005-09-20

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