GUANIDINE COMPOUNDS AND COMPOSITIONS FOR INHIBITING NAMPT Russian patent published in 2016 - IPC C07D211/74 C07D401/10 C07D401/12 C07D487/04 A61K31/437 A61K31/4406 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula II:

,

where Ar¹ represents a 6-10-member heteroaryl, where heteroaryl relates to a monocyclic or bicyclic heteroaryl containing 1, 2 or 3 heteroatoms selected from N, S or O, provided that two adjacent heteroatoms in ring can not both represent S or both represent O; Ar² is phenyl; R¹ is phenyl, 5-12-member heterocycloalkyl or 5-12-member heteroaryl (i), where each of said phenyl, heterocycloalkyl and heteroaryl is either unsubstituted or optionally independently substituted with 1, 2, 3, 4 or 5 substitutes, which can be identical or different and are independently selected from a group consisting of: halogen, cyano, alkyl, halogenalkyl, alkoxy, halogenalkoxy, -NR^aR^b, -CON^aR^b, -S(O)₂-alkyl,-S(O)₂N(alkyl)₂, -(CH₂)_qaryl, -(CH₂)_qheteroaryl and -(CH₂)_qheterocycloalkyl, (ii) where each of said phenyl can further be unsubstituted or substituted with one or more substitutes, such as halogen, cyano, alkyl or alkoxy, or can be optionally condensed with independently selected arylheteroaryl or heterocycloalkyl; R^a and R^b independently represent H, alkyl,-S(O)₂alkyl and cycloalkyl, or R^a and R^bcan form a 5- or 6-member heterocycloalkyl group together with a nitrogen atom to which they are bonded, where said heterocycloalkyl group may contain one or more additional heteroatoms selected from N, S or O; (iii) said 5-12-member heterocycloalkyl contains 1, 2 or 3 heteroatoms selected from N, S or O; (iv) said 5-12-member heteroaryl contains 1, 2 or 3 heteroatoms selected from N, S or O; R² and R³ represent H, m, n, p and q independently are equal to 0, 1 or 2; and their pharmaceutically acceptable salts.

EFFECT: compounds can be used to inhibit NAMPT.

29 cl, 3 tbl, 5 ex