Classifications

• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07D—HETEROCYCLIC COMPOUNDS
  • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
  • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
  • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07D—HETEROCYCLIC COMPOUNDS
  • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
  • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
  • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
  • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
  • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D213/56—Amides
• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07D—HETEROCYCLIC COMPOUNDS
  • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
  • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
  • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
  • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07D—HETEROCYCLIC COMPOUNDS
  • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
  • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07D—HETEROCYCLIC COMPOUNDS
  • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
  • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
  • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
  • C07H13/00—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
  • C07H13/12—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by acids having the group -X-C(=X)-X-, or halides thereof, in which each X means nitrogen, oxygen, sulfur, selenium or tellurium, e.g. carbonic acid, carbamic acid

Definitions

• the residue is taken up with 100 ml of acetone and 10 ml of water, 0.68 g of imidazole base are added and the mixture is stirred overnight. After solvent evaporation under reduced pressure, the residue is treated with ethyl acetate. The organic phase is washed with water, diluted hydrochloric acid- and water to neutrality. After drying on sodium sul- phate and filtration, the solvent is evaporated under vacuum. The residue is crystallized from ethanol/water. Yield: 28 g (72%) .
• the test has been performed according to Di Rosa et al. (Di Rosa M. , Giround J.P., Willoughby D.A. - J. Path. Bact., vol. 104, 15, 1971).
• a 1% solution (0.15 ml) of carrageenin in 0.9% NaCl was injected into the pleural cavity of Sprague-Dawley rats, weighing about 250 g.
• the animals were sacrificed, the pleural exudate volumes were measured and the leukocytes total number was counted by a micro- cell-counter, being the cavity rinsed by 0.5 ml of a sali- ne medium.
• the % inhibition of leukocytes total number was calcu ⁇ lated versus control animals.
• the assayed compounds were administered orally, 1 mM/kg, 30' before the carrageenin injection in the pleural cavity.
• Table IV as not limi ⁇ ting example, the results obtained with some of the compo ⁇ unds of the invention are reported.
• the assay has been performed according to Gemmel et al. (Gemmel D.K. Cottney J., Lewis A.J. - Agents Actions, vol. 9, 107, 1979). 1 Ml of a rabbit anti-bovine-albumin serum (freeze-dried antibodies, dissolved in 2 ml of 0.9% NaCl) was injected into the caudal vena of Sprague-Dawley male rats.
• the assay has been performed according to Sharon (Sharon P., Stenson W.F. - Gastroenterology, vol. 88, 55, 1985) .
• the administered doses (via intra-bowel, during the bowel ligature and the local injection of the acetic acid) were 0.5 mM/kg, for all the tested compounds, dispersed" in carboxymethylcellulose. The % reduction of the ulceration index has been calculated versus untreated animals.
• the compounds of Table 1 have been subjected to the acute toxicity test in mice, by the oral route, in carbo ⁇ xymethylcellulose suspensions. All the LD proved to be higher than 1600 mg/kg.
• the doses will be dependent on the patient's weight, age and conditions and will be anyhow ranging from 50 to 1000 mg, from 1 to 4 times a day.

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• Chemical & Material Sciences (AREA)
• Organic Chemistry (AREA)
• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Engineering & Computer Science (AREA)
• Biochemistry (AREA)
• Biotechnology (AREA)
• General Health & Medical Sciences (AREA)
• Genetics & Genomics (AREA)
• Molecular Biology (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

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• 1984
  • 1984-11-29 IT IT23799/84A patent/IT1196348B/it active
• 1985
  • 1985-11-25 GR GR852834A patent/GR852834B/el unknown
  • 1985-11-26 AU AU52311/86A patent/AU5231186A/en not_active Abandoned
  • 1985-11-26 WO PCT/EP1985/000645 patent/WO1986003199A1/en not_active Application Discontinuation
  • 1985-11-26 EP EP86900097A patent/EP0236329A1/en not_active Withdrawn
  • 1985-11-26 JP JP61500163A patent/JPS62501703A/ja active Pending
  • 1985-11-26 ZA ZA859035A patent/ZA859035B/xx unknown
  • 1985-11-27 PT PT81566A patent/PT81566B/pt unknown
  • 1985-11-27 CN CN198585109554A patent/CN85109554A/zh active Pending
  • 1985-11-28 ES ES549359A patent/ES8701717A1/es not_active Expired
• 1986
  • 1986-07-21 DK DK346486A patent/DK346486A/da not_active Application Discontinuation
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