COMPOUNDS AND COMPOSITIONS FOR SUPPRESSING SHP2 ACTIVITY Russian patent published in 2021 - IPC C07D471/04 C07D401/14 C07D403/14 C07D487/04 C07D495/04 C07D513/04 A61K31/4545 A61K31/497 A61K31/519 A61P35/00 

Abstract RU 2744988 C2

FIELD: organic chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, namely, the heterocyclic compound of formulas I and II. R1 is selected from

. R2 and R3, together with the nitrogen atom to which both R2 and R3 are attached, form a ring selected from piperidinyl, piperazinyl, 2-oxo-8-azaspiro[4.5]decan-8-yl, 8-azaspiro[4.5]decan-8-yl and pyrrolidinyl. The specified pyrrolidinyl, piperazinyl, 2-oxa-8-azaspiro[4.5]decan-8-yl, 8-azaspiro[4.5]decane-8-yl or piperidinyl are not substituted or are substituted by 1-3 groups independently selected from the amino group, methyl, ethyl, amino-methyl, methyl-amino group, hydroxyl, cyano group, fluor-methyl, fluoride and ((((5-methyl-2-oxo-1,3-dioxol-4-yl)methoxy)carbonyl)amino) methyl. R4 is a hydroxyl. R5 is selected from H and methyl. R6 is selected from hydrogen, methyl, and phenyl. R7 is selected from hydrogen, methyl, ethyl, phenyl, and benzyl. R8 is selected from hydrogen and methyl. Y1 is selected from N and CH. Y2 is CH. Y3 is selected from NH and CH2. Y4 represents N. Y5 represents N. The invention also relates to a pharmaceutical composition based on a compound of formula I or II, a method for treating a disease or disorder mediated by SHP2 activity, based on the use of this compound, and to specific heterocyclic compounds.

EFFECT: technical result is obtaining new heterocyclic compounds capable of inhibiting SHP2.

10 cl, 7 tbl, 67 ex

Similar patents RU2744988C2

Title Year Author Number
SPIRO-FUSED PIPERIDINE DERIVATIVES FOR APPLICATION AS INHIBITORS OF EXTERNAL MEDULLAR LAYER POTASSIUM CHANNEL 2013
  • Din Fa-Syan
  • Dun Shuchzhi
  • Fri Dzhessika
  • Gu Sin
  • Tszyan Tszinlun
  • Pasternak Aleksander
  • Tan Khajfyn
  • U. Chzhitsaj
  • Yuj Yan
  • Sudzuki Takao
RU2642066C2
BICYCLIC COMPOUNDS AS ALLOSTERIC SHP2 INHIBITORS 2018
  • Blank, Brian R.
  • Pitzen, Jennifer
  • Wang, Gang
  • Won, Walter S.
  • Tzitzilonis, Christos
  • Li, Jie Jack
  • Koltun, Elena S.
  • Aay, Naing
  • Buckl, Andreas
  • Mellem, Kevin
  • Semko, Christopher
  • Jogalekar, Ash
  • Kiss, Gert
  • Gill, Adrian
RU2776846C2
DERIVATIVE OF PYRIMIDINE AND A FIVE-MEMBERED NITROGEN-CONTAINING HETEROCYCLE, METHOD FOR PRODUCTION AND MEDICAL APPLICATIONS THEREOF 2019
  • Zou Hao
  • Li Zhengtao
  • Wang Yuanhao
  • Yu Jian
  • Zhu Wei
RU2775229C1
PHARMACEUTICAL COMBINATION CONTAINING ALK INHIBITOR AND SHP2 INHIBITOR 2018
  • Hao, Huaixiang
  • Li, Fang
  • Lamarche, Matthew J.
  • Wang, Hui-Qin
  • Dardaei Alghalandis, Leila
  • Engelman, Jeffrey Adam
RU2769132C2
PROTEIN TYROSIN PHOSPHATASE INHIBITORS 2020
  • Blake, James F.
  • Boys, Mark Laurence
  • Chicarelli, Mark Joseph
  • Cook, Adam W.
  • Elsayed, Mohamed S. A.
  • Fell, Jay Bradford
  • Fischer, John P.
  • Hinklin, Ronald Jay
  • Jiang, Yutong
  • Mcnulty, Oren T.
  • Mejia, Macedonio J.
  • Rodriguez, Martha E.
  • Wong, Christina E.
RU2799449C2
1,1,1-TRIFLUORO-3-HYDROXYPROPANE-2-YLCARBAMATE DERIVATIVES AS MAGL INHIBITORS 2018
  • Brodney, Michael Aaron
  • Butler, Christopher Ryan
  • Mcallister, Laura Ann
  • Helal, Christopher John
  • O'Neil, Steven Victor
  • Verhoest, Patrick Robert
RU2720203C1
CYCLIC CYANOENONE DERIVATIVES AS KEAP1 MODULATORS 2021
  • Altman, Michael
  • Candito, David, A.
  • Christian, Alec, H.
  • Di Pietro, Ornella
  • Lu, Min
  • Liu, Ping
  • Mansoor, Umar, Faruk
  • Mennie, Katrina, Marie
  • Musacchio, Andrew, J.
  • Palani, Anandan
  • Reutershan, Michael, H.
  • Shaw, David, Matthew
  • St-Gallay, Stephen
RU2822828C1
OXADIAZOLES AS MUSCARINIC RECEPTOR AGONISTS M AND/OR M 2019
  • Brown Giles Albert
  • Teobald Barry John
  • Tehan Benjamin Gerald
RU2817018C2
SUBSTITUTED BENZENE COMPOUNDS 2012
  • Kuntts Kevin Uejn
  • Chesuort Richard
  • Dunkan Kennet Uillyam
  • Kajlkhak Khajke
  • Varkholik Natali
  • Klaus Kristin
  • Natson Sara K.
  • Vigl Timoti Dzhejms Nelson
  • Seki Masasi
RU2629118C2
NEW SUBSTITUTED IMIDAZOPYRIDINE COMPOUNDS AS INDOLEAMINE-2,3-DIOXYGENASE AND/OR TRYPTOPHAN-2,3-DIOXYGENASE INHIBITORS 2017
  • Kouli Fillip M.
  • Makgouvan Meredit Enn
  • Braun Tomas Dzh.
  • Khan Yunsin
  • Lyu Kun
  • Pu Tsinlin
  • Vajs Alan
  • Chzhan Khuntszyun
  • Chzhou Khua
RU2741911C2

RU 2 744 988 C2

Authors

Chen, Zhuoliang

Fortanet, Jorge Garcia

Karki, Rajesh

Lamarche, Matthew J.

Majumdar, Dyuti

Perez, Lawrence Blas

Sendzik, Martin

Smith, Troy Douglas

Yang, Fan

Yu, Bing

Dates

2021-03-17Published

2017-06-12Filed