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2 617 988

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(51)

IPC

C07D471/04(2006-01-01)

C07D487/04(2006-01-01)

C07D491/04(2006-01-01)

C07D495/04(2006-01-01)

C07D401/12(2006-01-01)

C07D413/12(2006-01-01)

C07D417/12(2006-01-01)

A61K31/4355(2006-01-01)

A61K31/4365(2006-01-01)

A61K31/437(2006-01-01)

A61P35/00(2006-01-01)

(21) (22)

Application

2013114846, 2011-09-02

(24)

Start date

2011-09-02

(22)

Actual filing date

2011-09-02

(45)

Published

2017-05-02

(72)

Inventor

Bejr Kennet V.Baumajster TimmBakmelter Aleksandr Dzh.Klodfelter Karl Kh.Dragovich PiterGosselen FransisKhan BinsunLin TszyanRejnolds Dominik Dzh.Rot BryusSmit Chejz K.Van ChzhungoYuen Po-VajChzhen Syaochzhan

(73)

Holder

Forma Tiem, ElelsiDzhenentek, Ink.

NEW COMPOUNDS AND COMPOSITIONS FOR NAMPT INHIBITION Russian patent published in 2017 - IPC C07D471/04 C07D487/04 C07D491/04 C07D495/04 C07D401/12 C07D413/12 C07D417/12 A61K31/4355 A61K31/4365 A61K31/437 A61P35/00

Abstract RU 2617988 C2

FIELD: medicine, pharmacy.

SUBSTANCE: invention refers to the compound of IIB formula, or its pharmaceutically acceptable salts in which R represents a bicyclic nine-membered heteroaryl comprising 1, 2, 3 or 4 heteroatoms independently selected from N, S or O, wherein the said heteroaryl may be substituted by one or more substituents selected from the group consisting of oxo and halo; R¹ is-NHR⁴ andR⁴ is 3-10 membered cycloalkyl, aryl selected from phenyl and tetrahydronaphthalene, or 9-10 membered heteroaryl containing 1 or 2 heteroatoms selected from N and O; 3-10 membered cycloalkyl; aryl selected from phenyl and naphthalenyl; or 5-10-membered monocyclic or bicyclic heteroaryl comprising one or two heteroatoms selected from N, O and S; R² and R³ are hydrogen; values of other substitutes are specified in the invention formula; or where the compound is selected from a group consisting of compounds specified in the invention formula. Invention compounds have properties of nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. The invention also refers to individual compounds selected from the group indicated in the invention formula, to the pharmaceutical composition, method of treatment, compounds application and application of the pharmaceutical composition.

EFFECT: invention provides new compounds of IIB formula, with the properties of nicotinamide phosphoribosyltransferase inhibitor which can be used for hyperproliferative disorders treatment.

33 cl, 4 tbl, 25 ex

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RU 2 617 988 C2

Authors

Bejr Kennet V.

Baumajster Timm

Bakmelter Aleksandr Dzh.

Klodfelter Karl Kh.

Dragovich Piter

Gosselen Fransis

Khan Binsun

Lin Tszyan

Rejnolds Dominik Dzh.

Rot Bryus

Smit Chejz K.

Van Chzhungo

Yuen Po-Vaj

Chzhen Syaochzhan

Dates

2017-05-02—Published

2011-09-02—Filed