TRIAZOLOPYRIDINE JAK INHIBITOR COMPOUNDS AND METHODS Russian patent published in 2015 - IPC C07D471/04 A61K31/41 A61P29/00 A61P35/00 

Abstract RU 2561104 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula I or its pharmaceutically acceptable salts. The compounds according to the invention possess the properties of JAK2 kinase inhibitor. In formula

R1 represents H, C(O)ORa, wherein Ra means H or C1-C6 alkyl, phenyl, optionally substituted by 1-2 groups specified in C1-C6 alkyl which can be substituted in its turn by hydroxy, C1-C6 alkoxy, NRaRb group, wherein Ra and Rb independently represent H, C1-C6 alkyl, optionally substituted by C1-C6 alkoxy or morpholino, or together with N atom to which they are attached form piperazinyl substituted by C1-C6 alkyl, or morpholino, or S(O)1-2Ra group, wherein Ra means C1-C6 alkyl; ORa, wherein Ra means H, CF3, C1-C6 alkyl, optionally substituted by C1-C6 alkoxy, NRcRd, wherein Rc and Rd independently represent H or C1-C3 alkyl, by heterocyclyl specified in morpholinyl and pyrrolidinyl; halogen; CN; CF3; S(O)2Ra group, wherein Ra means C1-C6 alkyl, S(O)2NRaRb group, wherein Ra and Rb independently represent H, C1-C6 alkyl, NRaRb group, wherein Ra and Rb independently represent H or C1-C6 alkyl, or together with N atom to which they are attached form piperazinyl; heterocyclyl specified in tetrahydropyranyl, piperazinyl optionally substituted by C1-C6 alkyl or C1-C6alkoxyC1-C6alkyl, morpholinyl and pyrrolidinyl; C(O)NRaRb group, wherein Ra and Rb independently represent H, C1-C6 alkyl, C3-C6 cycloalkyl optionally substituted by hydroxy, or piperidinyl optionally substituted by C1-C6 alkyl, or together with N atom to which they are attached form piperazinyl substituted by acetyl, morpholino or piperidinyl substituted by hydroxy; the other values of R1, as well as of the other radicals are presented in the patent claim. The invention also refers to the specific compounds the structural formulas of which are presented in the patent claim.

EFFECT: new compounds which possess the properties of JAK2 kinase inhibitor are produced.

19 cl, 2 tbl, 438 ex

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RU 2 561 104 C2

Authors

Chzhu Bin-Jan'

Siu Majkl

Magnuson Stiven R.

Pastor Richard

Khajin Kheh

Isun Sjao

Tszifu Chzhehn

Sin Sjuj

Tszjun'Pin Chzhao

Lju Vendi

Dates

2015-08-20Published

2009-06-19Filed