13-11-2014 дата публикации
Номер: US20140336207A1
Принадлежит:
The present invention relates to a pyrrole six-membered heteroaryl ring derivative, the preparation method therefor, and the medicinal uses thereof. Specifically, the present invention relates to a new pyrrole six-membered herteroaryl ring derivative as represented by formula (I), the preparation method therefor, a medicinal composition comprising the derivative, and a therapeutic method using same, and, in particular, the uses as a JAK inhibitor and an immunosuppressor. Substituents in formula (I) have the same definitions as in the description. 8. The compound of formula (I) claim 1 , or a tautomer claim 1 , mesomer claim 1 , racemate claim 1 , enantiomer claim 1 , diastereomer claim 1 , or mixture thereof claim 1 , or a pharmaceutically acceptable salt thereof according to claim 1 , wherein L is a bond.9. The compound of formula (I) claim 1 , or a tautomer claim 1 , mesomer claim 1 , racemate claim 1 , enantiomer claim 1 , diastereomer claim 1 , or mixture thereof claim 1 , or a pharmaceutically acceptable salt thereof according to claim 1 , wherein Ris selected from the group consisting of alkyl claim 1 , heteroaryl claim 1 , —(CH)C(O)OR claim 1 , —C(O)R claim 1 , —C(O)NRR claim 1 , and —S(O)R claim 1 , wherein the alkyl or heteroaryl is optionally substituted with one or more groups selected from the group consisting of halogen claim 1 , hydroxyl claim 1 , cyano claim 1 , and —(CH)C(O)OR;{'sup': 15', '18', '18', '18', '18', '18', '18', '19', '20, 'sub': 12', 'n', '2', '2, 'Ris selected from the group consisting of hydrogen, alkyl, cycloalkyl, heterocyclyl, alkenyl, alkynyl, aryl, and heteroaryl, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more groups selected from the group consisting of alkyl, halogen, hydroxy, cyano, amino, nitro, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, —(C)C(O)OR, —OC(O)R, —C(O)R, —S(O)R, —NHC(O)(O)R, —NHS(O)R, and —NRR;'}{'sup': 16', '17', '18, 'Rand Rare each ...
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