TRICYCLIC COMPOUND AND JAK INHIBITOR Russian patent published in 2018 - IPC C07D471/14 A61K31/519 A61K31/4375 A61P29/00 A61P43/00 A61P19/02 

Abstract RU 2674262 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a new tricyclic compound (variants) corresponding to the general formula I, II or III, or its pharmaceutically acceptable salt, which has inhibitory activity against JAK. Compounds can be used as a prophylactic, therapeutic agent or agent for alleviating diseases for which JAK inhibition is effective, in particular for the treatment of rheumatoid arthritis. Tricyclic compound corresponds to the formula (I), (II) or (III)

. In compound of formula (I) A1 represents C3-7 cycloalkylene group, L1 represents C1-6 alkylene group, X1 represents O or NH, and when X1 is O, R1 represents C1-6 haloalkyl group, cyano-C1-6 haloalkyl group or cyano-C1-6 alkyl group, and when X1 represents NH, R1 is a cyano-C1-6 haloalkyl group or cyano-C1-6 alkyl group. In the compound of formula (II) A2 represents C3-7 cycloalkylene group, L2 represents C1-6 alkylene group, R2 is a 5-membered heteroaromatic group containing 2 nitrogen atoms in the ring (heterocyclic group may be substituted by one or two identical or different substituents independently selected from the group including halogen atoms, C1-4 alkyl groups and C1-4 haloalkyl groups). In the compound of formula (III) A3 represents C3-7 cycloalkylene group, L3 presents C1-6 alkylene group, X3 represents O or NH, and when X3 is O, R3 represents C1-6 haloalkyl group, cyano-C1-6 haloalkyl group or cyano-C1-6 alkyl group, and when X3 represents NH, R3 is cyano-C1-6 haloalkyl group or cyano-C1-6 alkyl group.

EFFECT: tricyclic compound and an inhibitor of JAK are proposed.

38 cl, 5 tbl, 41 ex

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RU 2 674 262 C2

Authors

Watanabe, Tsuneo

Takahashi, Keiji

Hayashi, Keishi

Nakamura, Takanori

Minami, Masataka

Kurihara, Kazunori

Yamamoto, Akio

Nishimura, Takuya

Uni, Miyuki

Kamiyama, Toshihiko

Iwamoto, Shunsuke

Dates

2018-12-06Published

2015-05-11Filed