MORPHOLINO-SUBSTITUTED DERIVATIVES OF UREA OR CARBAMATE AS MTOR INHIBITORS Russian patent published in 2017 - IPC C07D251/22 C07D401/12 C07D407/12 C07D413/04 A61K31/53 A61P37/00 A61P35/00 

Abstract RU 2616619 C2

FIELD: pharmacology.

SUBSTANCE: invention relates to compounds of formula (I) , where m equals 1 or 2; n equals 0, 1 or 2; each of R1 is independenly selected from the group consisting of C1-6alkyl, where C1-6alkyl is probably substitued with one R3; probably, two R1 are joint with a ring to which they are attached to form 8-membered heterobicycle; R3 is OR4; R4 is H; T0 is phenyl where T0 is substituted with the group N (R5a) C(O) N (R5bR5); R5a, R5b are independently selected from the group consisting of H; R5 is T2 or C1-6alkyl, where C1-6alkyl is probably substituted with 1-4 R8, which are the same or different; R8 is halogen; OR9; N (R9R9a); R9, R9a are independently selected from the group consisting of H; T2 is C3-7cycloalkyl; 4-6-membered heterocyclyl, wherein 1 circular atom is substituted with oxygen heteroatom; 6-membered aromatic heterocyclyl, wherein 1 circular atom is substituted with nitrogen heteroatom; and phenyl, wherein T2 is probably substituted with one or two R10, which are the same or different; R10 is halogen; OR11; or C1-6alkyl, where C1-6alkyl is probably substituted with one R12; R11 is H; R12 is OR13; R13 is H; T1 is phenyl or 6-membered aromatic heterocycle, wherein 1 carbon atom is substituted with nitrogen heteroatom, wherein T1 is substituted with a group S(O)2R14 and is probably additionally substituted with one R15; R15 is halogen; R14 is C1-6alkyl or unsubstituted 5-membered heterocyclyl ring, wherein 1 circular atom is substituted with nitrogen heteroatom. Compounds of formula (I) possess mTOR inhibitory activity. The invention also relates to a pharmaceutical composition, to compound application for drug manufacture and to a treatment method.

EFFECT: new compounds of formula are obtained, which are useful for treatment or prevention of mTOR-related diseases and disorders.

21 cl, 6 tbl, 44 ex

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RU 2 616 619 C2

Authors

Lynch Rosemary

Cansfield Andrew David

Hardy Daniel Paul

Sunose Mihiro

Morel Adeline

Convery Laura

Adrego Rita

Dates

2017-04-18Published

2012-09-21Filed