FGFR INHIBITOR AND ITS APPLICATION Russian patent published in 2021 - IPC C07D471/14 C07D487/14 C07D519/00 A61K31/4985 A61K31/437 A61K31/4375 A61K31/519 A61P35/00 

Abstract RU 2745035 C1

FIELD: medicine.

SUBSTANCE: invention relates to an azatricyclic compound of formula

Formula (I),

where represents a double bond; one of X and Y is selected from N and the other from CR10; Z is N; each of R1, R2, R3, R4 and R5 is independently selected from H, halogen, C1-8 alkoxy; or R3 and R4 together with the carbon atom to which they are attached can form a 5-membered C 1-4 alkyl or halogen substituted or unsubstituted heteroaryl ring, the 5-membered heteroaryl ring containing 1, 2 or 3 heteroatoms independently selected from N, O or S; R6 is C1-8alkyl, phenyl, pyridyl, C3-8cycloalkyl, C5-6 heterocyclyl containing 1-2 ring heteroatoms selected from N and O; R6 is optionally substituted with R7; R7 is hydroxyl, halogen, C1-8alkyl, C1-8alkoxy, C3-8cycloalkyl, C3-8cycloalkyl substituted with C1-4alkyl, C5-10heterocyclyl containing 1-2 heteroatoms independently selected from nitrogen and oxygen, substituted with C1-4alkyl, C1-4alkylene-OH, -NR11R12, -oxo, - (CO) -C1-4alkyl, - (CO) -NR11R12, C1-4haloalkyl, C3-6cycloalkyl, C3-6cycloalkyl-OH, C4-6heterocyclyl containing 1-2 heteroatoms in the ring selected from nitrogen and oxygen, or C4-6heterocyclyl-C1-4alkyl containing 1-2 heteroatoms in the ring selected from N and O, C5-6heterocyclyl containing 1-2 heteroatoms selected from nitrogen and oxygen, C6heterocyclic carbonyl containing 1-2 nitrogen heteroatoms in the ring, substituted by C1-4 alkyl, -NR11R12, -NR11-C1-8alkylene-NR11R12, -C1-4alkylene-C5-6heterocyclyl containing 1-2 heteroatoms selected from nitrogen and oxygen, C1-4alkylene-C5-6heterocyclyl-C1-4alkyl containing 1-2 nitrogen heteroatoms in the ring, -C1-8alkoxy-C5-6heterocyclyl containing 1-2 heteroatoms in the ring, selected from nitrogen and oxygen, or in the case where R6 is phenyl, R7 is an unsubstituted C5-6 heterocyclic ring containing a nitrogen atom in the ring fused with R6; R10 is H, amino, C1-6alkyl, C3-8cycloalkyl; R10 is optionally substituted with R8; R8 is C1-8alkyl, C4-6heterocyclo-C1-6alkoxy substituted with - (CO) -C2-8alkenyl containing 1-2 heteroatoms selected from nitrogen and oxygen atoms in the ring, phenyl substituted with -NH- (CO) - C2-4 alkenyl or —NH- (CO) —C1-4 alkyl, C3-8 cycloalkyl, C5-6 heterocyclyl containing 1-2 heteroatoms selected from nitrogen and oxygen; mono-, bi- or spiro-C5-10heterocyclyl containing 1-2 nitrogen atoms; substituted by C1-4alkyl, C1-4alkyl (CO) -, C2-4alkenyl-C (O), C1-4alkyl (CO) -NH-, C2-4alkenyl-C (O) -NH- groups or - (CO) - C2-8 alkenyl-CN, mono-, bi- or spiroheterocyclyl containing 1-2 nitrogen atoms, -S (O2) C4-6heterocyclyl- (CO) -C2-4alkenyl, -NR11R12, substituted with C4-6 heterocyclyl- (CO) -C2-4 alkenyl containing 1-2 nitrogen heteroatoms in the ring, or -NR11R12; each of R11 and R12 is H, C1-8alkyl, which functions as an inhibitor of fibroblast growth factor receptors (FGFR) as well as a pharmaceutical composition based on it, and is used in treatment of diseases mediated by FGFR.

EFFECT: treatment of diseases mediated by FGFR.

34 cl, 3 dwg, 12 tbl, 148 ex

Similar patents RU2745035C1

Title Year Author Number
SUBSTITUTED COMPOUNDS OF PYRIDINE AZOLOPYRIMIDINE-5-(6H)-ONE 2013
  • Allan Emi
  • Branstetter Brajan
  • Dik Brajan
  • Vajnkhaus Majkl I.
  • Gomez Loran
  • Merron Temi Dzho
  • Piters Marko
RU2653054C2
PIPERIDINE DERIVATIVES 2011
  • Baumann Karlkhajnts
  • Flor Aleksandr
  • Getshi Ehrvin
  • Grin Ljuk
  • Zholidon Siniz
  • Knust Khenner
  • Limberg An'Ja
  • Luehbbers Tomas
  • Tomas Ehndrju
RU2554353C2
QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR RECEPTOR INHIBITORS 2015
  • Verner Erik
  • Bremeld Kennet Albert
RU2721723C2
PYRIDAZINE DERIVATIVES AS RORc MODULATORS 2017
  • Bronner, Sara M.
  • Krouford, Dzhejms Dzh.
  • Kridlend, Endryu
  • Ser, Patrik
  • Fauber, Bendzhamin
  • Gansiya, Emanuela
  • Gobbi, Alberto
  • Kherli, Kristofer
  • Killen, Dzhonatan
  • Li, Vendi
  • Rene, Olive
  • Van Nil, Monik Bodil
  • Uord, Styuart
  • Uinship, Pol
  • Zbig, Dzhejson
RU2757571C2
PHENOXYMETHYL DERIVATIVES 2016
  • Khert Zherom
  • Khuntsiker Daniel
  • Kyune Kholger
  • Lyubbers Tomas
  • Martin Rajner E.
  • Mattej Patritsio
  • Najdkhart Verner
  • Rikhter Khans
  • Rudolf Markus
  • Pinar Emmanyuel
RU2746481C1
2,6-SUBSTUTED-4-MONOSUBSTITUTED AMINO-PYRIMIDINES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS 2005
  • Lim Sungtaek
  • Kharris Kejt Dzhon
  • Stefani Dehvid
  • Gardner Charl'Z Dzh.
  • Tsao Bin
  • Boffi Rehj
  • Gillespi Timoti A.
  • Agiar Zhuasi K.
  • Khant Khejzel Dzh.
  • Desho Ehl'Za A.
RU2417990C2
SELECTIVE HDAC6 INHIBITORS 2018
  • Vergani, Barbara
  • Caprini, Gianluca
  • Fossati, Gianluca
  • Lattanzio, Maria
  • Marchini, Mattia
  • Pavich, Gianfranco
  • Pezzuto, Marcello
  • Ripamonti, Chiara
  • Sandrone, Giovanni
  • Steinkuhler, Christian
  • Stevenazzi, Andrea
RU2764718C2
DIAMINOTRIAZOLES, SUITABLE AS INHIBITORS OF PROTEIN KINASES 2003
  • Pirs Al'Bert K.
  • Ehrnost Majkl
  • Dehvis Robert Dzh.
  • Forster Kornelija Dzh.
  • Galullo Vinsent
  • Grej Ronal'D
  • Ledebur Mark
  • Tjan' Shi-Kaj
  • Sjuj Tszin'Van
  • Binch Khehjli
  • Ledford Brajan
  • Messersmit Dehvid
  • Nantakumar Suganti
  • Dzhajaradzh Ehndrju
  • Van Tszjan'
  • Salituro Franchesko G.
  • Khenkel Grehg
RU2350606C2
COMPOUND BASED ON DIHYDRONAPTHYRIDINONE, METHOD OF ITS OBTAINING, AND ITS USE IN MEDICINE 2021
  • Zhou, Fusheng
  • Xu, Xiaoming
  • Zhang, Leitao
  • Li, Xin
  • Tang, Lili
  • Lan, Jiong
RU2809869C1
INHIBITORS OF FIBROBLAST GROWTH FACTOR RECEPTOR 2013
  • Bifalko Nil Ml.
  • Brojmans Natasha
  • Khodaus Brajan L.
  • Kim Dzhozef L.
  • Miduturu Chandrasekkhar V.
  • Venglovski Stiven Mark
RU2679130C2

RU 2 745 035 C1

Authors

Xu, Xiaofeng

Wang, Jiabing

Ding, Lieming

Liu, Xiangyong

Dates

2021-03-18Published

2018-02-27Filed