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
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero 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
  • A61K31/66—Phosphorus compounds
  • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K38/00—Medicinal preparations containing peptides
  • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
  • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
  • A61K38/19—Cytokines; Lymphokines; Interferons
  • A61K38/21—Interferons [IFN]
  • A61K38/212—IFN-alpha
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
  • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• • 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
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P31/12—Antivirals
  • A61P31/20—Antivirals for DNA viruses

Definitions

• the present invention relates to the use of phosphorus derivatives of alkaloids for the manufacture of a medicament for the treatment of hepatitis C.
• hepatitis C means a disease that has only been researched for a relatively short time. For a long time it was only known that there is a disease here that causes symptoms similar to the hepatitis A and hepatitis B diseases known to date, but that there are certain significant differences in the form of the disease. For a long time, the disease was therefore characterized as "hepatitis non-A non-B".
• Hepatitis C is a disease that is particularly prevalent in underdeveloped countries; It is believed that around 170 million people worldwide (i.e. approximately 4 times the amount of HIV infections) are infected with hepatitis C.
• AT 377 988 B and AT 354 644 B describe processes for the preparation of new phosphorus derivatives of alkaloids or of new salts of alkaloid derivatives of thiophosphoric acid. Such compounds have pharmacological activity and can be used as cytostatics.
• the object of the present invention is therefore the use of the reaction product of the alkaloids of Chelidonium majus L. with thiophosphoric acid triaziridide for the manufacture of a medicament for combating hepatitis C.
• Ukrain The above-mentioned implementation product will be briefly referred to below as "Ukrain"; the overwhelming majority of Ukrain has the following formula:
• IFN was tested in doses of 20, 50, 100, 200, 400, 600, 1000 IU / l blood, Ukrain in doses of 0.05, 0.1, 0.2, 0.5, 1.0 and 2, 0 ⁇ g / ml blood.
• Ten of the CHC patients examined were selected for the clinical Pilot trial with individual optimal IFN doses (0.5 to 2.0 ME (unit of measure) per injection, 6 patients, including 3 cases of HCV phenotype la) three times a week and Ukrain doses (0.25 to 2.5 mg per injection, 4 patients, including 2 HCV lb cases) every other day.
• the responses to the two compositions were shown to be different: 52.5% of all patients were sensitive to IFN and 73.1% to Ukrain, with the increase in the SH / SS ratio under the influence of the compositions being positive Effect and the reduction was assessed as a negative effect. Some patients have already shown a positive effect on the first dose of the preparations, others only on two or more doses.
• the optimal biological response to IFN in doses of 400, 200 and 100 IU / ml blood and to Ukrain in doses of 0.5, 0.1 and 0.2 ⁇ g / l blood was recorded more frequently.
• Standardized therapeutic IFN doses of 600 to 1000 IU / ml which correspond to in vivo injections of 3.0 to 5.0 ME doses, only showed a positive effect on the SH / SS system in 0 to 18.2% of the cases and a negative effect in 63.6 to 81.8% of cases, which is one of the reasons for the low effectiveness of IFN in CHC and the frequency of side effects in IFN therapy.
• 9 out of 10 patients were HCV-RNA negative in PCR: 3 after one month, 3 after three months of therapy with an individual IFN dose, 3 after three weeks of individual therapy with Ukrain. No serious side effects have been identified and treatment of all patients is ongoing.
• the response to Ukrain was shown to be different: 73.1% of all patients were sensitive to this composition, while in the same group of CHC patients, sensitivity to interferon-alpha 2b (IFN) was significantly lower, namely 46 2%. In the group of CHC patients who were IFN-resistant, the sensitivity to Ukrain was almost the same (71.4%). Furthermore, all 4 CHC patients with HCV phenotype lb were sensitive to Ukrain in vitro. The optimal biological response to Ukrain doses of 0.5, 0.1 and 0.2 ⁇ g / ml blood was frequently recorded.
• IFN interferon-alpha 2b
• the medicaments produced according to the invention preferably consist of an aqueous solution of the alkaloid phosphor derivatives or their salts used, optionally together with other auxiliaries known per se.
• the medicament according to the invention is preferably administered by injection, for example intraperitoneally, intramuscularly or intravenously, the dosage depending on the case and being related to the severity of the disease to be treated and the condition of the patient.

Landscapes

• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Veterinary Medicine (AREA)
• Animal Behavior & Ethology (AREA)
• Public Health (AREA)
• Pharmacology & Pharmacy (AREA)
• General Health & Medical Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Epidemiology (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Engineering & Computer Science (AREA)
• Virology (AREA)
• Oncology (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Communicable Diseases (AREA)
• Gastroenterology & Hepatology (AREA)
• Proteomics, Peptides & Aminoacids (AREA)
• Zoology (AREA)
• Immunology (AREA)
• Molecular Biology (AREA)
• Biotechnology (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Medicines Containing Material From Animals Or Micro-Organisms (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Nitrogen Condensed Heterocyclic Rings (AREA)

Priority Applications (13)

Applications Claiming Priority (2)

Publications (2)

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Family Applications (1)

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Cited By (3)

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• 2000
  • 2000-03-22 AT AT0048100A patent/AT408719B/de not_active IP Right Cessation
• 2001
  • 2001-03-20 CA CA002389173A patent/CA2389173A1/en not_active Abandoned
  • 2001-03-20 WO PCT/AT2001/000076 patent/WO2001070203A2/de active Application Filing
  • 2001-03-20 BR BR0107211-0A patent/BR0107211A/pt not_active IP Right Cessation
  • 2001-03-20 PL PL01365000A patent/PL365000A1/xx not_active Application Discontinuation
  • 2001-03-20 JP JP2001568401A patent/JP2003527414A/ja active Pending
  • 2001-03-20 AU AU2001239000A patent/AU2001239000A1/en not_active Abandoned
  • 2001-03-20 IL IL14931401A patent/IL149314A0/xx unknown
  • 2001-03-20 EA EA200200584A patent/EA200200584A1/ru unknown
  • 2001-03-20 CN CN01803046A patent/CN1416347A/zh active Pending
  • 2001-03-20 KR KR1020027005739A patent/KR20020087045A/ko not_active Application Discontinuation
  • 2001-03-20 MX MXPA02004993A patent/MXPA02004993A/es unknown
• 2002
  • 2002-04-24 IS IS6360A patent/IS6360A/is unknown
  • 2002-04-26 HR HR20020367A patent/HRP20020367A2/hr not_active Application Discontinuation
  • 2002-05-10 NO NO20022253A patent/NO20022253D0/no unknown
  • 2002-05-28 MA MA26657A patent/MA25509A1/fr unknown
  • 2002-09-12 BG BG107088A patent/BG107088A/xx unknown

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