DERIVATIVES OF PYRROLOPYRIMIDINE USEFUL AS JAK-KINASES INHIBITORS
FIELD: chemistry.SUBSTANCE: invention relates to a heterocyclic compound of the formula(I) or to its enantiomer, a diastereomer and a mixture thereof and a pharmaceutically acceptable salt thereof, wherein A: CH or N; L: bond or Calkyl; Ris selected from hydrogen, Calkyl, heteroaryl, - (CH)C(O)OR, -...
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Zusammenfassung: | FIELD: chemistry.SUBSTANCE: invention relates to a heterocyclic compound of the formula(I) or to its enantiomer, a diastereomer and a mixture thereof and a pharmaceutically acceptable salt thereof, wherein A: CH or N; L: bond or Calkyl; Ris selected from hydrogen, Calkyl, heteroaryl, - (CH)C(O)OR, -C(O)R, -C(O)NRR, and -S(O)R, where each of alkyl or heteroaryl is possible is substituted with 1-3 groups selected from halogen, hydroxy, cyano, Calkyl, Calkoxy, Ccycloalkyl, Caryl, pyridine and - (CH)C(O)OR; Ror Ris independently selected from hydrogen and Calkyl; R or Ris independently selected from hydrogen and halogen; Ror Ris independently selected from hydrogen and Calkyl; R, R, Ror Ris independently selected from hydrogen, Calkyl and hydroxyCalkyl; R, R, Ror Ris independently selected from hydrogen or Rand Ror Rand Rtaken together form an oxo group; Ris selected from Calkyl, Ccycloalkyl, Calkenyl, Caryl and pyridine, wherein each of alkyl, cycloalkyl or heteroaryl is optionally substituted with 1 to 4 groups selected from halogen, hydroxy, cyano, Calkoxy, Caryl, tetrazole, -NRR, -S(O)R, -NHC(O)ORand -NHS(O)R; Ror Ris independently selected from hydrogen, Calkyl and heteroaryl, wherein heteroaryl is optionally substituted by one selected from Calkyl, hydroxy, Calkoxy, Ccycloalkyl, hydroxyCalkyl and-OR; Ris selected from Calkyl and hydroxyCalkyl; Ror Ris independently selected from the group consisting of hydrogen; M is 0, 1 or 2; N is 0 or 1; P is 0, 1 or 2; Q is 0 or 1; S is 1 or 2; And t is 1 or 2. The invention also relates to particular intermediates, a process for the preparation of a compound of formula (I), a pharmaceutical composition based on it, the use of a compound of formula (I), a method for inhibiting JAK kinases, and a method for treating certain diseases of the immune system.EFFECT: new heterocyclic compounds possessing the activity of JAK-kinase inhibitor have been obtained.22 cl, 7 tbl, 158 ex
Изобретение относится к области органической химии, а именно к гетероциклическому соединению формулы (I) или к его энантиомеру, диастереомеру и их смеси и к его фармацевтически приемлемой соли, где А: СН или N; L: связь или Салкил; Rвыбран из водорода, Салкила, гетероарила, -(СН)C(O)OR, -C(O)R, -C(O)NRR, и -S(O)R, где каждый из алкила или гетероарила возможно замещен 1-3 группами, выбранными из галогена, гидрокси, циано, Салкила, Салкокси, Сциклоалкила, Сарила, пиридина и -(CH)C(O)OR; Rили Rнезависимо выбран из водорода и Cалкила; R или Rнезависимо |
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