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PE20200447A1 - Compuestos de biheteroarilo y usos de los mismos - Google Patents

Compuestos de biheteroarilo y usos de los mismos

Info

Publication number
PE20200447A1
PE20200447A1 PE2019002479A PE2019002479A PE20200447A1 PE 20200447 A1 PE20200447 A1 PE 20200447A1 PE 2019002479 A PE2019002479 A PE 2019002479A PE 2019002479 A PE2019002479 A PE 2019002479A PE 20200447 A1 PE20200447 A1 PE 20200447A1
Authority
PE
Peru
Prior art keywords
pyrimidin
biheteroaril
compounds
compound
dlk
Prior art date
Application number
PE2019002479A
Other languages
English (en)
Inventor
Anthony Estrada
Paul Gibbons
Terry Kellar
Wen Liu
Changyou Ma
Alan Olivero
Snahel Patel
Daniel Shore
Michael Siu
Kevin X Chen
Malcolm Huestis
Liting Dong
Joseph P Lyssikatos
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20200447A1 publication Critical patent/PE20200447A1/es

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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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Abstract

Referido a un compuesto de formula (I-I) o sus sales, en el que R1, R2 y R3 son cada uno independientemente H, F, Cl, Br, I, alquilo C1-6 o haloalquilo C1-6; X1 es N; X2 es N o CH; y A y Cy se selecciona entre el grupo que consiste en pirrolidina, piperidina, azetidina, entre otros. Un compuesto preferido es 5-[2-(3,3-difluoro-1-piperidil)-6-[(1S,4S)-2-oxa-5-azabiciclo[2.2.1]heptan-5-il]pirimidin-4-il]pirimidin-2-amina. Estos compuestos biheteroarilos inhiben la actividad de la doble quinasa de cremallera de leucina (DLK), siendo util para el tratamiento de enfermedades neurodegenerativas.
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