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
  • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• • 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
  • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P9/00—Drugs for disorders of the cardiovascular system
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P9/00—Drugs for disorders of the cardiovascular system
  • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Definitions

• the invention is based on the finding of novel physiological properties of the compound 9-methyl-4-phenyl-6H-thieno[3,2- ]-s-triazolo[4,3-a] [1,4]- diazepine, hereinafter Compound C.
• apo A-I apolipoprotein A-I
• Apo A-I is a major protein constituent of plasma high density lipoproteins (HDL).
• Low plasma levels of HDL are known to be associated with an increased incidence of coronary artery disease (CAD).
• CAD coronary artery disease
• apo B apoUpoprotein B
• the present invention relates to the use of Compound C for the manufacture of medicaments for the treatment and prevention of illnesses which are caused by low plasma apo A-I levels.
• illnesses are the above mentioned CAD, mainly myocardial infarction, and atherosclerosis.
• the invention relates to plasma apo A-I levels enhancing medicaments which contain Compound C as the active ingredient, as well as to a process for the manufacture of such medicaments, which process comprises bringing Compound C and, if desired, one or more other therapeutically valuable substances into a galenical administration form.
• the invention relates to a method of increasing plasma apo A-I levels in mammals, particularly human beings, which method comprises administering an effective amount of Compound C.
• the activity of Compound C on plasma levels of apo A-I can be demonstrated by standard methods. For example, male hamsters were fed a coco-nut enriched diet. Ten controls and five drug treated animals were used. Compound C was given mixed with the food at a daily dose of 30 mg/kg for 10 days. The experiment was conducted as described in J. Lipid Res. 36: 1567-1585, 1995.
• the mean concentrations in g/L or mg/dl at both day-1 and day 10 of the assay are as follows:
• Plasma parameter Control: Compound C: day-1 day 10 day-1 day 10
• apo A-I 1.00 ⁇ 0.08 0.97 ⁇ 0,09 0.91 ⁇ 0.08 1.30 ⁇ 0.15* apo B (g/L) 0.79 ⁇ 0.09 1.20 ⁇ 0.19* 0.84 ⁇ 0.11 1.20 ⁇ 0.35* triglycerides (mg/dl) 312 ⁇ 46 288 ⁇ 34** 197 ⁇ 23 307 ⁇ 19**
• Compound C did not induce any manifest adverse effect.
• the animals remained healthy, lively, kept eating and growing at normal rates and were not showing any signs of sedation.
• Compound C can be used as active ingredient in pharmaceutical preparations.
• the pharmaceutical preparations are administered orally, e.g. in the form of tablets, coated tablets, dragees, hard and soft gelatine capsules, solutions, emulsions or suspensions.
• the active ingredient can be mixed with pharmaceutically inert, inorganic or organic carriers in order to manufacture such preparations.
• Lactose, corn starch, talc, stearic acid or its salts can be used, for example, as carriers for tablets, coated tablets, dragees and hard gelatine capsules.
• Suitable carriers for soft gelatine capsules are, for example, vegetable oils, waxes or fats; depending on the nature of the active ingredient no carriers are, however, usually required in the case of soft gelatine capsules.
• Suitable carriers for the manufacture of solutions and syrups are, for examples, water, saccharose, invert sugar and glucose.
• the pharmaceutical preparations can also contain preservatives, solubilizers, stabilizers, wetting agents, emulsifiers, sweeteners, colorants, flavorants, salts for varying the osmotic pressure, buffers, coating agents or antioxidants. They can also contain other therapeutically valuable substances.
• Compound C can be used in the control or prevention of illnesses such as atherosclerosis and CAD, particularly myocardial infarction.
• the dosage can vary within wide limits and will, of course, be fitted to the individual requirements in each particular case.
• the daily dosage can be taken in one, two or three single doses, e.g. with food.
• a single dosage form contains from about 10 to 500 mg of Compound C.
• a hard gelatine capsule contains e.g. 30, 60, 125, 250 or 500 mg of Compound C and finely crystalline lactose to a final fill weight of 580-590 mg.

Landscapes

• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Epidemiology (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Cardiology (AREA)
• Heart & Thoracic Surgery (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Urology & Nephrology (AREA)
• Vascular Medicine (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
• Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Medicinal Preparation (AREA)
• Nitrogen Condensed Heterocyclic Rings (AREA)

Priority Applications (9)

Applications Claiming Priority (2)

Publications (1)

Family

ID=8219597

Family Applications (1)

Country Status (14)

Cited By (6)

Families Citing this family (30)

Citations (1)

Family Cites Families (2)

• 1996
  • 1996-08-30 CN CN96196835A patent/CN1101680C/zh not_active Expired - Fee Related
  • 1996-08-30 TR TR1998/00406T patent/TR199800406T1/xx unknown
  • 1996-08-30 ES ES96930137T patent/ES2188783T3/es not_active Expired - Lifetime
  • 1996-08-30 CA CA002230477A patent/CA2230477A1/en not_active Abandoned
  • 1996-08-30 JP JP9510839A patent/JPH11512107A/ja not_active Ceased
  • 1996-08-30 KR KR1019980701708A patent/KR19990044460A/ko not_active Ceased
  • 1996-08-30 BR BR9610390A patent/BR9610390A/pt not_active Application Discontinuation
  • 1996-08-30 EP EP96930137A patent/EP0853480B1/en not_active Expired - Lifetime
  • 1996-08-30 DK DK96930137T patent/DK0853480T3/da active
  • 1996-08-30 AU AU69303/96A patent/AU725249B2/en not_active Ceased
  • 1996-08-30 US US09/011,819 patent/US5854238A/en not_active Expired - Fee Related
  • 1996-08-30 WO PCT/EP1996/003814 patent/WO1997009048A1/en not_active Ceased
  • 1996-08-30 DE DE69625696T patent/DE69625696T2/de not_active Expired - Fee Related
  • 1996-08-30 AT AT96930137T patent/ATE230600T1/de not_active IP Right Cessation

Patent Citations (1)

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