4-AMINO-2-(4-METHYLPIPERAZINE-1-YL)-5-(2,3,5-TRICHLOROPHENYL)- -PYRIMIDINE AND ITS SALTS OF ACID ADDITION, METHODS OF THEIR SYNTHESIS (VARIANTS) AND PHARMACEUTICAL COMPOSITION Russian patent published in 2001 - IPC

Abstract RU 2171256 C2

FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention relates to the novel compound, 4-amino-2-(4-methyl- piperazine-1-yl)-5-(2,3,5-trichlorophenyl)-pyrimidine (compound A) and its salts of acid addition, methods of their synthesis (variants) and pharmaceutical composition. The first method of synthesis of compound (A) or its salts involves interaction of compound of the formula (I) where L is the group to be removed and Y is cyano-group with compound of the formula (II) or its salt. Another method of synthesis involves interaction of compound of the formula (IV) where Y is cyano-group and R10 and R11 are alkyl or in common they form the group -(C(R)2)n where R means hydrogen atom or alkyl and n = 2-4 with compound of the formula (II). Indicated compounds are able to inhibit glutamate release and can be used for treatment of patients with disorders of central nervous system, for example, for prophylaxis of cerebral ischemic damages. Pharmaceutical composition shows property of inhibitor of glutamate release and has the compound (A) as an active component or its pharmaceutically acceptable salt of acid addition and pharmaceutically acceptable carrier. Composition is made in the form for oral intake. EFFECT: new compound indicated above, improved method of synthesis, valuable medicinal properties. 18 cl, 1 tbl, 1 ex

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RU 2 171 256 C2

Authors

Miller Ehlistehjr Ehjnsli

Nobbz Mal'Kol'M Stjuart

Gajd Richard Martin

Lich Majkl Dzhon

Dates

2001-07-27Published

1989-12-06Filed