WO2005041974A1 - Agents pour la reduction ponderale - Google Patents

Agents pour la reduction ponderale Download PDF

Info

Publication number
WO2005041974A1
WO2005041974A1 PCT/EP2004/011398 EP2004011398W WO2005041974A1 WO 2005041974 A1 WO2005041974 A1 WO 2005041974A1 EP 2004011398 W EP2004011398 W EP 2004011398W WO 2005041974 A1 WO2005041974 A1 WO 2005041974A1
Authority
WO
WIPO (PCT)
Prior art keywords
carbon atoms
straight
chain
branched
hydrogen
Prior art date
Application number
PCT/EP2004/011398
Other languages
German (de)
English (en)
Inventor
Hilmar Bischoff
Harald Mayer
Axel Schmidt
Original Assignee
Bayer Healthcare Ag
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 Bayer Healthcare Ag filed Critical Bayer Healthcare Ag
Publication of WO2005041974A1 publication Critical patent/WO2005041974A1/fr

Links

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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents

Definitions

  • the wild, zoo and gander animals include animals which are e.g. naturally occurring in the environment and for various reasons are mostly kept in captivity.
  • the active compounds can also be dissolved in physiologically tolerated vegetable or synthetic oils which are suitable for injection.
  • Pour-on formulations are infused or sprayed onto limited areas of the skin, whereby the active ingredient either penetrates the skin and acts systemically or spreads on the body surface.
  • Suspensions may be administered orally, dermally or as an injection. They are prepared by suspending the active ingredient in a carrier liquid optionally with the addition of further auxiliaries, such as wetting agents, dyes, absorption-promoting substances, preservatives, antioxidants, light stabilizers.
  • auxiliaries such as wetting agents, dyes, absorption-promoting substances, preservatives, antioxidants, light stabilizers.
  • carrier liquids As carrier liquids, all homogeneous solvents and solvent mixtures may be mentioned.
  • Organic substances are e.g. Sugar, cellulose, food and feed such as milk powder, animal meal, cereal flours and meals, starches.
  • the active compounds may also be present in the preparations in admixture with synergists or with other active ingredients.
  • Suitable combination components are substances which are also used for weight loss, examples being orlistat, fenfluramine, dexfenfluramine, tungstates (eg sodium tungstate).
  • the combined application with biological approaches is possible, for. B. immunization or neutralizing antibodies.
  • Ready-to-use preparations usually contain the active compounds in concentrations of from 0.1 ppm (w / w) to 95 percent by weight, preferably from 1 ppm (w / w) to 90 percent by weight.
  • Medicated feed usually contains 1 ppm to 100 ppm (w / w) of active ingredient.
  • Other pharmaceutical formulations usually contain at least 0.1% by weight, preferably at least 0.5% by weight.
  • the animals (obese fa, fa sugar rats) were weighed before treatment and randomized in groups of 8 animals. The animals received a calorie-enriched diet for 4 weeks. The compound of the formula (A) was orally administered at a concentration of 15 ppm (15 mg / kg diet) with the feed.
  • the body weight gain after 4 weeks was 74g in the control group without active ingredient in the feed.
  • the animals receiving 15 ppm of the compound of formula (A) with the diet increased 66% less in the 4 weeks, namely only 25 g. Much of this decreased body weight gain is due to a reduction in body fat.
  • the animals treated with the compound of the formula (A) had a 32% lower fat content (epidydimal and perirenal body fat) after these 4 weeks compared with the untreated control animals.

Landscapes

  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Obesity (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Child & Adolescent Psychology (AREA)
  • Nutrition Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

L'invention concerne l'utilisation de pyrimido[1,2-a]indoles particuliers pour la réduction pondérale, notamment chez des animaux en surpoids.
PCT/EP2004/011398 2003-10-22 2004-10-12 Agents pour la reduction ponderale WO2005041974A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10349175A DE10349175A1 (de) 2003-10-22 2003-10-22 Mittel zur Gewichtsreduktion
DE10349175.9 2003-10-22

Publications (1)

Publication Number Publication Date
WO2005041974A1 true WO2005041974A1 (fr) 2005-05-12

Family

ID=34442211

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2004/011398 WO2005041974A1 (fr) 2003-10-22 2004-10-12 Agents pour la reduction ponderale

Country Status (6)

Country Link
AR (1) AR046057A1 (fr)
DE (1) DE10349175A1 (fr)
GT (1) GT200400212A (fr)
PE (1) PE20050649A1 (fr)
TW (1) TW200528454A (fr)
WO (1) WO2005041974A1 (fr)

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6114341A (en) * 1996-04-04 2000-09-05 Bayer Aktiengesellschaft Pyrimido[1,2-a]indoles

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6114341A (en) * 1996-04-04 2000-09-05 Bayer Aktiengesellschaft Pyrimido[1,2-a]indoles

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
HALLER C ET AL: "Pharmacologic agents for weight reduction", JOURNAL OF GENDER-SPECIFIC MEDICINE 2002 UNITED STATES, vol. 5, no. 5, 2002, pages 16 - 21, XP009042556, ISSN: 1523-7036 *

Also Published As

Publication number Publication date
DE10349175A1 (de) 2005-05-19
AR046057A1 (es) 2005-11-23
PE20050649A1 (es) 2005-10-27
GT200400212A (es) 2005-06-06
TW200528454A (en) 2005-09-01

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