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filingDate 2006-06-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2009-07-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber RU-2008101371-A
titleOfInvention HALOGENIZED PYRAZOLO [1,5-a] PYRIMIDINES (OPTIONS), METHOD FOR PRODUCING THEM, PHARMACEUTICAL COMPOSITION BASED ON THEM, INTERMEDIATE COMPOUNDS AND METHOD FOR PRODUCING THEM (OPTIONS)
abstract 1. Halogenated pyrazolo [1,5-a] pyrimidines covered by the general structural formula (I):! ! where R represents alkyl (C1-C6); ! R1 is selected from the group consisting of alkyl (C1-C6) and alkynyl (C1-C6); ! X represents a halogen atom; and! Y is selected from the group consisting of -CO- and -SO2-,! and their pharmaceutically acceptable salts. ! 2. Pyrazolo [1,5-a] pyrimidines according to claim 1, in which R means methyl. ! 3. Pyrazolo [1,5-a] pyrimidines according to claim 1, in which R1 means methyl. ! 4. Pyrazolo [1,5-a] pyrimidines according to claim 1, wherein R1 is prop-2-ynyl. ! 5. Pyrazolo [1,5-a] pyrimidines according to claim 1, in which X means fluorine. ! 6. Pyrazolo [1,5-a] pyrimidines according to claim 1, in which X means chlorine. ! 7. Halogenated pyrazolo [1,5-a] pyrimidines selected from the group consisting of:! N- {2-fluoro-5- [3- (thiophen-2-carbonyl) pyrazolo [1,5-a] pyrimidin-7-yl] phenyl} -N-methyl-acetamide; ! N- {2-chloro-5- [3- (thiophen-2-carbonyl) pyrazolo [1,5-a] pyrimidin-7-yl] phenyl} -N-methyl-acetamide; ! N- {2-fluoro-5- [3- (thiophen-2-carbonyl) pyrazolo [1,5-a] pyrimidin-7-yl] phenyl} -N-methylmethanesulfonamide; ! N- {2-chloro-5- [3- (thiophen-2-carbonyl) -pyrazolo [1,5-a] pyrimidin-7-yl] phenyl} -N-methyl-methanesulfonamide and! N- {2-fluoro-5- [3- (thiophen-2-carbonyl) pyrazolo [1,5-a] pyrimidin-7-yl] phenyl} -N-prop-2-ynyl methanesulfonamide; ! and its pharmaceutically acceptable salt. ! 8. The method of obtaining pyrazolo [1,5-a] pyrimidines of the general formula (I) according to claim 1, wherein the intermediate of the formula (II) is reacted:! ! where R, R1, X and Y are as defined for formula (I) a Q means a corresponding leaving group selected from the group consisting of N (dialkyl (C1-C6)), alkylthio (C1-C6) group and alkoxy (C1 -C6) a group with an intermediate of formula (III):! ! and alternatively, the compounds formed during the reaction are reacted in
priorityDate 2005-06-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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