Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-07-02
1998-11-10
Fan, Jane
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546264, C07D40106, A61K 3144
Patent
active
058344918
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to substituted bis(2-aminopyridine)s, to a process for preparing them and also to the applications of bis(2-aminopyridine)s, substituted or otherwise, as a medicinal product, in particular as medicinal products which are active against intraerythrocytic parasitoses such as malaria or babesiosis (or piroplasmosis).
Antimalarial and antibabesiosis activity is understood to mean the capacity to prevent the development of the parasite inside the erythrocyte and/or erythrocytic invasion, and to bring about the death of the parasites initially present.
Malaria or paludism remains the most important parasitic disease rampant in the intertropical regions. The World Health Organization estimates that there are some 350 million cases of malaria worldwide, 90% of them in Africa, causing the death of 1.5 to 2.7 million people per annum. From 1940 onwards, synthetic anti-folates such as Fansidar.RTM. (sulphonamide/pyrimethamine) and quinolines such as Nivaquine.RTM. (chloroquine) were employed to combat the disease. However, from the 1960s onwards, resistance appeared and necessitated the development of new active molecules, among them Lariam.RTM. (mefloquine) or Halfan.RTM. (halofantrine); nevertheless, these new molecules have also led to the emergence of new types of resistance, specific resistance but also cross-resistance. The emergence of chloroquine-resistant strains of Plasmodium falciparum in South-East Asia and in Latin America and the general expansion of these drug-resistance phenomena impose a limit on the effective treatment of malaria. In addition, the resistance to each of the new compounds, mefloquine and halofantrine, is also considerable and gives rise to a cross-resistance between these two substances.
Other substances such as artemisinine and its derivatives (artemether, artether, artesunate and dihydroartemisinine) are also used in China and in South-East Asia. However, these substances have the drawback of possessing a short half-life and low water-solubility.
Babesiosis, also known as piroplasmosis, is, like malaria, an intraerythrocytic parasitosis transmitted by tick bites, which affects many domestic and wild animal species and whose agent is a protozoan of the genus Babesia. There is thus a bovine babesiosis caused by Babesia bovis, Babesia bigemina, Babesia major and Babesia divergens which are responsible for considerable losses in cattle farming, in particular in developing countries. A canine babesiosis with Babesia canis and Babesia gibsoni, an equine babesiosis with Babesia equi and cabalii and even a rare but severe human babesiosis due to Babesia divergens and Babesia microti are also found.
Few substances are active against Babesia, and they are generally toxic (imidocarb and amicarbalide). Other products prove active in vitro without, however, giving good results in vivo, such as tubercidin, tetracycline or menoctone.
As early as 1984, McColm (Ann. Trop. Med. Parasitol., 78, (4), 345) stressed the increased resistance of Babesia towards classical antimicrobials such as tylosin, rifamycin and gramicidin D.
Consequently, it was the Applicant's objective to provide new products which are active against intraerythrocytic parasites.
The subject of the present invention is substituted bis(2-aminopyridine)s of general formula (I), ##STR2## in which: Q represents: total from 6 to 34 carbon atoms, represent: C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy radicals, and R.sub.4 is not a hydrogen atom when Q represents a linkage (CH.sub.2).sub.m with m between 6 and 20, as well as their addition salts.
Among the addition salts with acids, there may be mentioned those formed with inorganic acids such as hydrochloric, hydrobromic, nitric, sulphuric or phosphoric acids or organic acids such as acetic, propionic, maleic, benzoic, succinic, methanesulphonic, para-toluenesulphonic, fumaric and hydroxyethanesulphonic acids.
The expression C.sub.6 -C.sub.20 alkyl denotes saturated or unsaturated, linear or branched alkyl groups.
The expression aryl denotes, for example
REFERENCES:
patent: 4206215 (1980-06-01), Bailey
CA 98:4464, Inokuma et al., 1983.
Ancelin Marie-Laure
Bourguignon Jean-Jacques
Calas Michele
Giral Louis
Vial Henri
Fan Jane
Virbac
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