NOVEL PYRROLE COMPOUNDS, SYNTHESIS METHOD THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME Russian patent published in 2017 - IPC C07D401/14 C07D405/14 C07D471/04 A61K31/4709 A61K31/5377 A61P35/00 

Abstract RU 2607788 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I) possessing inhibitory activity on Bcl-2 family proteins. In formula (I) (I) A1 is hydrogen, (C1-C6)polyhaloalkyl group or (C1-C6)alkyl group, A2 is hydrogen, (C1-C6)polyhaloalkyl group, (C1-C6)alkyl group or cycloalkyl group, T denotes a hydrogen atom, (C1-C6)alkyl group, optionally substituted with one-three halogen atoms, group (C1-C4)alkyl-NR1R2 or group (C1-C4)alkyl-OR6, R1 and R2 each independently from each other is a hydrogen atom or (C1-C6)alkyl group, or R1 and R2 form with a nitrogen atom bearing them, heterocycloalkyl, R3 is (C1-C6)alkyl group, cycloalkyl group, heterocycloalkyl group, aryl group or heteroaryl group, wherein one or more carbon atoms of previous groups or their possible substitutes can be deuterated, R4 is an aryl group or heteroaryl group, wherein one or more carbon atoms of previous groups or their possible substitutes can be deuterated, R5 is hydrogen or halogen atom, R6 is a hydrogen atom or a linear or branched (C1-C6)alkyl group, Ra, Rb, Rc and Rd each independently from other represents hydrogen, linear or branched (C1-C6)alkyl, halogen atom, a linear or branched (C1-C6)alkoxy group, hydroxy group, R7-CO-NH-(C0-C6)alkyl-, R7-SO2-NH-(C0-C6)alkyl-, R7-NH-CO-NH-(C0-C6)alkyl-, R7-O-CO-NH-(C0-C6)alkyl-, or substitutes of pair (Rb, Rc) form together with carbon atoms carrying them, a ring consisting of 5–6 ring members, which may contain 1–2 oxygen atoms, R7 is hydrogen, linear or branched (C1-C6)alkyl, aryl or heteroaryl. Invention also relates to methods of producing compounds of formula (I), to a pharmaceutical composition, use of a pharmaceutical composition for preparing a drug, use of compound of formula (I) for preparing a drug.

EFFECT: obtaining novel compounds of formula (I) possessing inhibitory activity on Bcl-2 family proteins.

37 cl, 2 tbl, 473 ex

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RU 2 607 788 C2

Authors

Le-Tiran Arno

Le-Digore Terri

Stark Zherom-Benua

Anlen Zhan-Mishel

Gijuzik Ann-Fransuaz

De-Nantej Gijom

Zhenest Olive

Fejesh Imre

Tatai Yanosh

Niergesh Miklosh

Dejvidson Dzhejms Eduard Pol

Marri Dzhejms Bruk

Chen Itszen

Dyuran Dide

Dates

2017-01-10Published

2014-07-22Filed