Pyrimidine compound and anti-rotavirus composition

Details Pyrimidine compound and anti-rotavirus composition Pyrimidine compound and anti-rotavirus composition

1997-05-06

2000-06-27

Ford, John M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

544319, 544323, 544320, 544322, 544326, 544329, 544332, 514272, 514269, 514256, C07D23948, C07D23947, A61K 31505

Patent

active

060807504

ABSTRACT:
A pyrimidine compound of the formula [I] ##STR1## wherein R1 is H, C.sub.1 -C.sub.4 lower alkyl, halogen atom, --OH, C.sub.1 -C.sub.4 lower alkoxy, C.sub.1 -C.sub.6 hydroxy(lower)alkoxy or --NH.sub.2 ; R2 is H, --NH.sub.2 or --NHCOCH.sub.3 ; R3 is --NR5(CH.sub.2)i--CH.sub.2 OH; R4 is H, halogen atom, --NH.sub.2, --CN, --CHO, --CH.sub.2 OH, --COOH, --CH.sub.2 NH.sub.2, --CONH.sub.2 or --CH.dbd.N--A wherein A is --OH, C.sub.1 -C.sub.4 lower alkyl or C.sub.1 -C.sub.4 lower alkoxy; R5 is H or C.sub.1 -C.sub.4 lower alkyl; and i is an integer of 1 to 4, and an anti-rotavirus agent comprising, as an active ingredient, a compound of the formula [I] wherein R3 is a group selected from the following: ##STR2## The novel pyrimidine compound of the present invention and related derivatives thereof have superior anti-rotavirus action and are useful for the prophylaxis and treatment of rotaviral diseases.

REFERENCES:
patent: 3034954 (1962-05-01), Darlington
patent: 4523945 (1985-06-01), Mengel et al.
patent: 4939252 (1990-07-01), Schwartz
Parkanyi et al., "Synthesis of Acyclic Nucleoside Analogs of 6-Substituted 2-Aminopurines and 2-Amino-8-azapurines", J. Heterocylic Chem., 27, 1409-1413 (1990).
Eger et al., "Sythesis of New Acyclic Pyrimidine Nucleoside Analogs as Potential Antiviral Drugs", J. Med. Chem., 37, 3057-3061 (1994).
Oonishi et al., "Preparation of 6-(((1',2'-bis(hydroxymethyl)propan-1'-yl)methyl)pyrimidine derivatives as intermediates for antiviral purine nucleoside analogs", Chemical Abstracts, 124, No. 25, 1405 (1996).
Botta et al, Chemical Abstracts, vol. 122, entry 81278 (1995).

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