NOVEL NICOTINAMIDE DERIVATIVE OR ITS SALT Russian patent published in 2016 - IPC C07D213/82 C07D401/12 C07D401/14 C07D405/14 C07D409/14 C07D413/12 C07D471/04 A61K31/44 A61K31/455 A61P9/00 A61P37/00 

Abstract RU 2576623 C2

FIELD: chemistry.

SUBSTANCE: invention relates to nicotinamide derivative, represented by the following formula

wherein R1 represents substituent, represented by the following formula R3 represents hydrogen atom or C1-6 alkyl, C3-8 cycloalkyl, phenyl, pyridyl or thienyl groups, each of which optionally contains substituent, selected from the group of substituents α1-1; group of substituents α1-1: halogen atom and C1-6 alkyl, C3-8 cycloalkyl, C1-6 alkoxy, C1-6 alkylthio, phenyl and pyrazolyl groups, each of which optionally contains halogen atom. R4 represents hydrogen atom, C1-6 alkyl group or C3-8 cycloalkyl group, R5 represents hydroxygroup, halogen atom or C1-6 alkyl or C1-6 alkoxy group, each of which optionally contains phenyl group, n represents integer number from 0 to 2, when n has value 2, R5 can be similar or different from each other and two R5, together with carbon atom, which they are bound to, can form C3-8 cycloalkane ring, X1 represents oxygen atom or -N(R6)- (wherein R6 represents hydrogen atom or acyl group), "*" represents binding site and R2 represents pyridyl, indazolyl, phenyl, pyrazole pyridyl, benzisoxazolyl, pyrimidinyl or quinolyl group, each of which optionally contains substituent, selected from the group of substituents α2-1; group of substituents α2-1: halogen atom and C1-6 alkyl, C3-8 cycloalkyl, C1-6 alkoxy, (di) C1-6 alkylamino, acyl, pyrazolyl, triazolyl, morpholinyl and pyrrolizyl groups, each of which optionally contains substituent, selected from the group of substituents β2-1; group of substituents β2-1: halogen atom, oxo and C1-6 alkyl and C1-6 alkoxy groups.

EFFECT: compounds possess excellent Syk-inhibiting activity.

19 cl, 8 tbl

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RU 2 576 623 C2

Authors

Fudzivara Khidejasu

Midzumoto Sinsuke

Kubo Jokhei

Nakata Khijoku

Nagivara Sindzi

Baba Jasutaka

Tamura Takasi

Kunijosi Khidenobu

Masiko Tomojuki

Jamamoto Mari

Dates

2016-03-10Published

2011-12-28Filed