DIHYDROPYRIMIDINES, INTERMEDIATE PRODUCTS AND MEDICINAL AGENT Russian patent published in 2005 - IPC C07D401/04 C07D401/14 C07D417/14 A61K31/506 A61P1/16 C07D239/00 C07D213/00 C07D215/00 C07D239/00 C07D213/00 C07D277/62 

Abstract RU 2245881 C9

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to new derivatives of dihydropyrimidine of the general formula (I):

or its isomeric form of the formula (Ia):

that can be used, for example, for treatment and prophylaxis of hepatitis B. In indicated formulas R1 means unsubstituted phenyl or phenyl substituted once or many times with similar or different substitutes taken among the group including halogen atom, trifluoromethyl group, nitro-, amino-group, hydroxyl and alkyl with 1-6 carbon atoms, or residues of formulas:

, or ; R2 means residue of the formula -XR5 wherein X means a bond or oxygen atom; R5 means alkenyl with 2-4 carbon atoms or alkyl with 1-4 carbon atoms that can be unsubstituted or substituted with phenoxy-group; R3 means amino-group, alkyl with 1-4 carbon atoms or cyclopropyl; R4 means pyridyl that is substituted with up to three times with similar or different substitutes taken among the group including halogen atom, trifluoromethyl group, alkoxy-group with 1-6 carbon atoms and alkyl with 1-6 carbon atoms, and their salts. Also, invention relates to 3,5-difluoro-2-pyridincarboxyimidamide and 3,5-difluoro-2-pyridincarbonitrile that can be sued as intermediates products for preparing compounds of the formula (I) or (Ia) and to a medicinal gent.

EFFECT: improved preparing method, valuable medicinal properties of compounds.

10 cl, 2 sch, 4 tbl, 9 ex

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RU 2 245 881 C9

Authors

Shtol'Tefus Jurgen

Goldman Zigfrid

Krehmer Tomas

Shlemmer Karl-Khajnts

Nivener Ul'Rikh

Pehssens Arnol'D

Grehf Ehrvin

Lottmann Shtefan

Deres Kark

Veber Olaf

Shtelting Jorn

Dates

2005-02-10Published

1999-04-07Filed