MORPHOLINO-SUBSTITUTED DERIVATIVES OF BICYCLIC PYRIMIDINE UREA OR CARBAMATE AS MTOR INHIBITORS Russian patent published in 2017 - IPC C07D495/04 A61K31/519 A61K31/5377 A61K31/5386 A61P9/00 A61P25/28 A61P35/00 

Abstract RU 2609208 C2

FIELD: pharmaceutics.

SUBSTANCE: invention relates to compounds of formula (I) and their pharmaceutically acceptable salts

. I

n formula (I) m is equal to 1; o equals 1 or 2; each R1 is independently selected from group consisting of H and unsubstituted C1-6alkyl; two R1 are possibly combined to form, together with ring, to which they are bonded, 8-oxa-3-azabicyclo[3.2.1]octane-3-yl or 3-oxa-8-azabicyclo[3.2.1]octane-8-yl ring; T1 is phenyl, where T1 is substituted by group N(R5a)C(O)N(R5bR5) and T1 is optionally additionally substituted with one or more R6, which are identical or different; R6 is halogen; each of R5a, R5b represents H; R5 represents H; T2; and C1-6alkyl, where C1-6alkyl is optionally substituted with one or more R8, which are identical or different; R8 represents halogen or OR9; R9 represents H; T2 is unsubstituted and selected from group consisting of phenyl, pyridyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, oxetanyl or tetrahydrofuranyl; Ra and Rb are selected to obtain one of formulae (Ik)–(Ip)

or Ra, Rb, T1 are selected to obtain formula (Iq)

R14, R14a, R14b, R14c are independently selected from group consisting of H; halogen or unsubstituted C1-6alkyl. Compounds of formula (I) possess mTOR inhibiting activity. Invention also relates to pharmaceutical composition containing compounds of formula (I), use of compounds for making drug and to method of treating.

EFFECT: novel compounds of formula (I) are obtained, which have mTOR inhibitor activity, which can be used for treating or preventing mTOR related diseases and disorders.

16 cl, 15 tbl, 82 ex

Similar patents RU2609208C2

Title Year Author Number
N-9-SUBSTITUTED PURINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE 2010
  • Kevin Khonlyun Lau
  • Vendi Li
  • Dzhozef P. Lissikatos
  • Chzhonkhua Pej
  • Kerk D. Robardzh
RU2607635C2
N-7 SUBSTITUTED PURINES AND PYRAZOLOPYRIMIDINES, COMPOSITIONS THEREOF AND METHODS FOR USE 2010
  • Li Vendi
  • Lissikatos Dzhozef P.
  • Pehj Chzhunkhua
  • Robardzh Kirk D.
RU2515541C2
MORPHOLINO-SUBSTITUTED DERIVATIVES OF UREA OR CARBAMATE AS MTOR INHIBITORS 2012
  • Lynch Rosemary
  • Cansfield Andrew David
  • Hardy Daniel Paul
  • Sunose Mihiro
  • Morel Adeline
  • Convery Laura
  • Adrego Rita
RU2616619C2
PYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE 2009
  • Bergeron Filipp
  • Koehn Frederik
  • Ehstrada Ehntoni
  • Kouler Majkl F. T.
  • Lo Kevin Khon Luen
  • Li Kuong
  • Lissikatos Dzhozef P.
  • Ortvajn Dehniel Fred
  • Pehj Chzhunkhua
  • Chzhao Sjanzhuj
RU2473549C2
MORPHOLINOPYRIMIDINE DERIVATIVES USEFUL FOR TREATING PROLIFERATIVE DISORDERS 2007
  • Finlej Moris Rajmond Verskojl
  • Morris Dzheffri
  • Pajk Kurt Gordon
RU2440349C2
BICYCLIC HETEROCYCLIC COMPOUNDS AND THEIR APPLICATIONS 2020
  • Kregg, Dzhejms Dzhozef
  • Bakl, Andreas
  • Aaj, Naing
  • Tambo-Ong, Arlin A.
  • Koltun, Elena S.
  • Dzhill, Edrian Liam
  • Tompson, Severin
  • Glidt, Mika Dzh.
RU2811612C2
NOVEL PYRIDOPYRIMIDINONE COMPOUNDS FOR MODULATION OF CATALYTIC ACTIVITY OF HISTONE LYSINE DEMETHYLASES (KDMS) 2015
  • Kim Myeong-Seop
  • Park Taesun
  • Yoon Taeyoung
  • Yang Seung Min
  • Kim Hae-Sun
  • Kim Jun Gyu
RU2684396C2
PYRAZOLAMINOPIRIMIDINE DERIVATIVES AS LEUCINE-REPEATING KINASE 2 (LRRK2) MODULATORS FOR TREATMENT OF PARKINSON DISEASE 2013
  • Bejker-Glenn Charlz
  • Chan Brajan K.
  • Dotson Dzhennafer
  • Estrada Entoni
  • Kheffron Timoti
  • Lissikatos Dzhozef
  • Svini Zakari Kevin
RU2637948C2
PYRIDOPYRIMIDINONES AND USE THEREOF AS MODULATORS OF N-METHYL-D-ASPARTATE RECEPTOR 2016
  • Volgraf Metyu
  • Tszyan Yu
  • Villemur Eliziya
  • Sellers Bendzhamin
  • U Goshen
  • Lu Ajtszyun
RU2717665C2
HETEROCYCLIC COMPOUNDS FOR TYROSINE KINASE 2 ACTIVITY MEDIATION 2020
  • Chen, Syanyan
  • Pan, Yujchen
RU2826012C2

RU 2 609 208 C2

Authors

Lynch Rosemary

Cansfield Andrew David

Hardy Daniel Paul

Feutrill John Thomas

Adrego Rita

Ellard Katie

Ladduwahetty Tammy

Dates

2017-01-31Published

2012-10-05Filed