EP1309320A2 - Produits anthelminthiques permettant de prevenir les infections parasitaires chez l'homme et l'animal ii - Google Patents

Produits anthelminthiques permettant de prevenir les infections parasitaires chez l'homme et l'animal ii

Info

Publication number
EP1309320A2
EP1309320A2 EP01945311A EP01945311A EP1309320A2 EP 1309320 A2 EP1309320 A2 EP 1309320A2 EP 01945311 A EP01945311 A EP 01945311A EP 01945311 A EP01945311 A EP 01945311A EP 1309320 A2 EP1309320 A2 EP 1309320A2
Authority
EP
European Patent Office
Prior art keywords
alkyl
optionally substituted
formula
hydrogen
different
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP01945311A
Other languages
German (de)
English (en)
Inventor
Achim Harder
Georg Von Samson-Himmelstjerna
Bernd-Wieland Krüger
Heinz Mehlhorn
Jürgen Schmidt
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer AG
Original Assignee
Bayer 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 AG filed Critical Bayer AG
Publication of EP1309320A2 publication Critical patent/EP1309320A2/fr
Withdrawn legal-status Critical Current

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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • 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
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • A61P33/12—Schistosomicides

Definitions

  • Anthelmintics to prevent parasitic infections in humans and animals II
  • the present invention relates to compositions containing certain active substances suitable as repellents and their use for preventing infection of humans or animals with the infection stages of parasitic flatworms (plathelminths).
  • the agents are used on the skin against such stages of flatworms, so-called cercariae, which can penetrate through the skin into the host body.
  • a pretreatment of the skin according to the invention with anthelmintic substances can, however, protect against the penetration of the pathogens.
  • Hexachlorophene has a killing effect on cercariae from Schistosomas mansoni (Fripp, P.J. and Armstrong, F.L., The efficacy of hexachlorophene skin cleanser as a cercariae repellent. South African Med. J. 47: 1973, 526-527). Because of health risks, especially liver damage, hexachlorophene cannot be applied to the skin in humans. It is poisonous in contact with the skin and if swallowed, may cause malformations and may be carcinogenic [Commission of the European Communities, Directive 93/72 / EEC of 1 September. 1993, Appendix Vol. I and II (EU Hazardous Substances Ordinance) with additions up to 1999, Official Journal of EUL258A, 36th year, Oct. 16, 1993, additions up to 1997].
  • Niclosamide acts against the penetration of cercariae [Bruce, J.I. et al. (1992) Efficacy of niclosamide as apotential topical antipenetrant (TAP) against cercariae of Schistosoma mansoni in monkeys. Mem. Inst. Oswaldo Cruz 87:28 1-289.] Is toxicologically unsafe because it can cause inheritable genetic damage (Registry of Toxic Effects of Chemical Substances, National Institute of Occupational Safety and Health). Application on the skin after exposure in
  • N, N-Diethyl-m-toluamide acts on cercariae from Schistosoma mansoni [Salafsky, B. et al. Evaluation of N, N-diethyl-m-toluamide (DEET) as a topical agent for preventing skin penetration by cercariae of Schistosoma mansoni. At the. J. Trop. Med. Hyg. 58: 1998, 828-834).
  • DEET has some unfavorable properties. The effects of the anthelmintics described so far against infectious stages of plathelminths have so far only been tested on cercariae of the species Schistosoma mansoni, so that the effectiveness of these agents against other types of worms has not been demonstrated.
  • the agents according to the invention are suitable for providing effective protection for humans and animals against infections with plathelminths, in particular Schistosoma haematobium, Schistosoma japonicum, Trichobilharzia spp. and Omithobilharzia spp., but also Echinostoma spp. et al to offer.
  • the invention accordingly relates to
  • Y represents hydrogen, optionally substituted alkyl or the radical O-X,
  • X represents hydrogen, COR 1 COOR 12 , R l3 ,
  • R 1 represents optionally substituted alkyl or alkenyl radicals
  • R 2 , R 11 , R 12 and R 13 are identical or different and represent optionally substituted alkyl or alkenyl radicals
  • R 3 to R 10 are the same or different and represent hydrogen or optionally substituted alkenyl radicals, and where R 2 and R 3 together with the atoms to which they are attached can also form an optionally substituted monocyclic ring and
  • n and m are the same or different and represent 0 or 1, with the proviso that X is not hydrogen or R 13 if n and m are 0.
  • X represents hydrogen, COR 11 or R 13 ,
  • R 1 represents Ci-C-alkyl or C 3 -C 7 -alkenyl
  • R 2 , R n , R 13 are the same or different and are C 3 -C 6 alkyl
  • R 3 to R 6 are the same or different and stand for hydrogen or Ci- - alkyl, where R 2 and R 3 together with the atoms to which they are attached can form a 5- or 6-membered monocyclic ring and n for 1 and
  • R 2 and R 3 very particularly preferably form, together with the atoms to which they are attached, a 5- or 6-membered monocyclic ring, in particular a piperazine ring.
  • the mosquitoes with their bites can transmit diseases such as malaria, various viruses, filaria and parasites, especially in the tropics.
  • the agents according to the invention now enable simultaneous prevention against infections with platinum helminths and protection against mosquitoes with one agent. This avoids the need to use two different, possibly incompatible agents on the skin at the same time.
  • the agents according to the invention can also contain all customary auxiliaries and additives which are used in formulations for topical application.
  • the active ingredients are used directly or in the form of suitable preparations dermally or with the aid of shaped articles containing active ingredients, e.g. Strips, plates, ribbons, collars, ear tags, limb straps, marking devices.
  • the dermal application happens e.g. in the form of bathing, diving (dipping), spraying (spraying), pouring on (pour-on or spot-on), washing, shampooing, watering, powdering.
  • Suitable preparations are:
  • Emulsions and suspensions for dermal use and semi-solid preparations are Emulsions and suspensions for dermal use and semi-solid preparations
  • Formuherungen in which the active ingredient is processed in an ointment base or in an oil in water or water in oil emulsion base;
  • Solid preparations such as powders, shaped articles containing active ingredients.
  • Solutions for use on the skin are dripped on, spread on, rubbed in, sprayed on, sprayed on or applied by dipping (dipping), bathing or washing.
  • the solutions are prepared by dissolving the active ingredient in a suitable solvent and possibly adding additives such as solubilizers, acids, bases, buffer salts, antioxidants, preservatives.
  • solvents such as
  • Alcohols such as ethanol, butanol, benzyl alcohol, glycerin, hydrocarbons, propylene glycol, polyethylene glycols, N-methyl-pyrrolidone, and mixtures thereof.
  • the active ingredients can optionally also be dissolved in physiologically compatible vegetable or synthetic oils.
  • solubilizers solvents which require the active ingredient to be dissolved in the main solvent or prevent it from precipitating.
  • solvents which require the active ingredient to be dissolved in the main solvent or prevent it from precipitating.
  • examples are polyvinyl pyrrolidone, polyoxyethylated castor oil, polyoxyethylated sorbitan esters.
  • Preservatives are: benzyl alcohol, trichlorobutanol, p-hydroxybenzoic acid ester, n-butanol.
  • Gels that are applied or spread on the skin are produced by adding enough thickening agent to solutions that have been prepared as described above to produce a clear mass with an ointment-like consistency.
  • the thickeners specified above are used as thickeners. Pour-on formulations are poured or sprayed onto limited areas of the skin, the active ingredient being distributed over the surface of the body.
  • pour-on formulations are prepared by dissolving, suspending or emulsifying the active ingredient in suitable skin-compatible solvents or solvent mixtures. If necessary, further auxiliaries such as dyes, antioxidants, light stabilizers and adhesives are added.
  • solvents water, alkanols, glycols, polyethylene glycols, polypropylene glycols, glycerol, aromatic alcohols such as benzyl alcohol, phenylethanol, phenoxyethanol, esters such as ethyl acetate, butyl acetate, benzylbenzoate, ethers such as alkylene glycol alkyl ethers such as dipropylene glycol monomethyl ether, diethylene glycol, monobutyl glycol, monobutyl glycol Methyl ethyl ketone, aromatic and / or aliphatic hydrocarbons, vegetable or synthetic oils, DMF, dimethylacetamide, N-methylpyrrolidone, 2-dimethyl-4-oxy-methylene-l, 3-dioxolane.
  • aromatic alcohols such as benzyl alcohol, phenylethanol, phenoxyethanol
  • esters such as ethyl acetate, butyl acetate
  • benzylbenzoate

Landscapes

  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

La présente invention concerne des produits contenant certains principes actifs utilisés comme agents répulsifs et leur utilisation pour prévenir les infections dues aux plathelminthes aux stades d'infection chez l'homme et l'animal.
EP01945311A 2000-07-06 2001-06-25 Produits anthelminthiques permettant de prevenir les infections parasitaires chez l'homme et l'animal ii Withdrawn EP1309320A2 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10032879 2000-07-06
DE10032879A DE10032879A1 (de) 2000-07-06 2000-07-06 Anthelmintika zur Verhinderung von parasitären Infektionen bei Mensch und Tier II
PCT/EP2001/007200 WO2002002087A2 (fr) 2000-07-06 2001-06-25 Produits anthelminthiques permettant de prevenir les infections parasitaires chez l'homme et l'animal ii

Publications (1)

Publication Number Publication Date
EP1309320A2 true EP1309320A2 (fr) 2003-05-14

Family

ID=7648013

Family Applications (1)

Application Number Title Priority Date Filing Date
EP01945311A Withdrawn EP1309320A2 (fr) 2000-07-06 2001-06-25 Produits anthelminthiques permettant de prevenir les infections parasitaires chez l'homme et l'animal ii

Country Status (13)

Country Link
US (1) US20040014813A1 (fr)
EP (1) EP1309320A2 (fr)
JP (1) JP2004501959A (fr)
KR (1) KR20030017542A (fr)
CN (1) CN1440280A (fr)
AU (1) AU2001267565A1 (fr)
BR (1) BR0112369A (fr)
CA (1) CA2413581A1 (fr)
DE (1) DE10032879A1 (fr)
HU (1) HUP0301298A3 (fr)
PL (1) PL359596A1 (fr)
WO (1) WO2002002087A2 (fr)
ZA (1) ZA200300055B (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102006007549A1 (de) * 2006-02-16 2007-08-30 Lanxess Deutschland Gmbh Öl-in-Wasser-Formulierung zur Arthropoden- und Plathelminthen-Abwehr
DE102006007547A1 (de) * 2006-02-16 2007-08-30 Lanxess Deutschland Gmbh Gel-Formulierung zur Arthropoden- und Plathelminthen-Abwehr
DE102006007546A1 (de) * 2006-02-16 2007-08-30 Saltigo Gmbh Wasser-in-Öl-Formulierung zur Arthropoden-und Plathelminthen-Abwehr

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3708033A1 (de) * 1987-03-12 1988-09-22 Bayer Ag Mittel zur insekten- und milbenabwehr

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO0202087A2 *

Also Published As

Publication number Publication date
US20040014813A1 (en) 2004-01-22
WO2002002087A2 (fr) 2002-01-10
HUP0301298A3 (en) 2005-04-28
DE10032879A1 (de) 2002-01-17
JP2004501959A (ja) 2004-01-22
CN1440280A (zh) 2003-09-03
HUP0301298A2 (hu) 2003-08-28
PL359596A1 (en) 2004-08-23
BR0112369A (pt) 2003-05-13
CA2413581A1 (fr) 2003-01-03
KR20030017542A (ko) 2003-03-03
AU2001267565A1 (en) 2002-01-14
ZA200300055B (en) 2004-01-30
WO2002002087A3 (fr) 2002-06-20

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Owner name: BAYER HEALTHCARE AG

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Effective date: 20060117