DERIVATIVES OF PYRROLOPYRIMIDINE USEFUL AS JAK-KINASES INHIBITORS Russian patent published in 2017 - IPC C07D487/04 C07D209/52 C07D403/04 C07D221/04 C07D209/44 C07D217/06 A61K31/519 A61P37/06 A61P35/00 

Abstract RU 2618673 C2

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 C1-2alkyl; R1 is selected from hydrogen, C1-4alkyl, heteroaryl, - (CH2)nC(O)OR15, -C(O)R15, -C(O)NR16R17, and -S(O)mR15, where each of alkyl or heteroaryl is possible is substituted with 1-3 groups selected from halogen, hydroxy, cyano, C1-2alkyl, C1-2alkoxy, C3cycloalkyl, C6aryl, pyridine and - (CH2)nC(O)OR15; R2 or R4 is independently selected from hydrogen and C1-2alkyl; R or R3 is independently selected from hydrogen and halogen; R5 or R6 is independently selected from hydrogen and C1-2alkyl; R7, R8, R9 or R10 is independently selected from hydrogen, C1-2alkyl and hydroxyC1-2alkyl; R11, R12, R13 or R14 is independently selected from hydrogen or R11 and R12 or R13 and R14 taken together form an oxo group; R15 is selected from C1-4alkyl, C3cycloalkyl, C2alkenyl, C6aryl and pyridine, wherein each of alkyl, cycloalkyl or heteroaryl is optionally substituted with 1 to 4 groups selected from halogen, hydroxy, cyano, C1-4alkoxy, C6aryl, tetrazole, -NR19R20, -S(O)mR18, -NHC(O)OR18 and -NHS(O)mR18; R16 or R17 is independently selected from hydrogen, C1-3alkyl and heteroaryl, wherein heteroaryl is optionally substituted by one selected from C1-2alkyl, hydroxy, C1-2alkoxy, C3cycloalkyl, hydroxyC1alkyl and-OR18; R18 is selected from C1-4alkyl and hydroxyC1-4alkyl; R19 or R20 is 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

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RU 2 618 673 C2

Authors

Chzhan Syuetszyun

Dun Tsin

Lyu Bonyan

Chzhu Yaopin

Li Syaotao

Lan Tszyun

Dates

2017-05-10Published

2012-12-19Filed