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PE20191207A1 - Benzoisotiazol, isotiazolo[3,4-b]piridina, quinazolina, ftalazina, pirido[2,3-d]piridazina y derivados de pirido[2,3-d]pirimidina como inhibidores de kras g12c para tratar el cancer de pulmon, pancreatico o colorrectal - Google Patents

Benzoisotiazol, isotiazolo[3,4-b]piridina, quinazolina, ftalazina, pirido[2,3-d]piridazina y derivados de pirido[2,3-d]pirimidina como inhibidores de kras g12c para tratar el cancer de pulmon, pancreatico o colorrectal

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Publication number
PE20191207A1
PE20191207A1 PE2019001307A PE2019001307A PE20191207A1 PE 20191207 A1 PE20191207 A1 PE 20191207A1 PE 2019001307 A PE2019001307 A PE 2019001307A PE 2019001307 A PE2019001307 A PE 2019001307A PE 20191207 A1 PE20191207 A1 PE 20191207A1
Authority
PE
Peru
Prior art keywords
pyrid
alkyl
kras
inhibitors
cancer
Prior art date
Application number
PE2019001307A
Other languages
English (en)
Inventor
Brian Alan Lanman
Victor J Cee
Alexander J Pickrell
Anthony B Reed
Kevin C Yang
David John Kopecky
Hui-Ling Wang
Patricia Lopez
Kate Ashton
Shon Booker
Christopher M Tegley
Original Assignee
Amgen Inc
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 Amgen Inc filed Critical Amgen Inc
Publication of PE20191207A1 publication Critical patent/PE20191207A1/es

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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • A—HUMAN NECESSITIES
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A—HUMAN NECESSITIES
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    • C—CHEMISTRY; METALLURGY
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Abstract

REFERIDO A COMPUESTOS DE FORMULA (I) DONDE E1 Y E2 SON CADA UNO N O CR1; R1 H, HIDROXI, ALQUILO C1-6, ENTRE OTROS; R2 ES HALO, ALQUILO C1-6, HALOALQUILO C1-6, ENTRE OTROS; R3 ES HALO, ALQUILO C1-3, HALOALQUILO C1-2, ENTRE OTROS; R4 ES -L-A-NR7R4', ENTRE OTROS, EN DONDE EL ANILLO A ES UN ANILLO MONOCICLICO DE 4-7 MIEMBROS O BICICLICO DE 6-11 MIEMBROS EN FORMA DE PUENTE, CONDENSADO O DE TIPO ESPIRO; L ES UN ENLACE, ALQUILENO C1-6, -O-ALQUILENO C0-5, ENTRE OTROS; R4' ES H, ALQUILO C1-6, ENTRE OTROS; R7 ES H O ALQUILO C1-8. SON COMPUESTOS PREFERIDOS: 1-(4-(5-CLORO-7-FLUORO-6-(1H-INDOL-3-IL)-2,1-BENZOTIAZOL-3-IL)-1-PIPERAZINIL)-2-PROPEN-1-ONA; 1-(4-(5-CLORO-6-(2-FLUORO-6-HIDROXIFENIL)-2,1-BENZOTIAZOL-3-IL)-1-PIPERAZINIL)-2-PROPEN-1-ONA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE KRAS G12C SIENDO UTILES EN EL TRATAMIENTO DE CANCER PANCREATICO, ADENOCARCINOMA PULMONAR, O CANCER COLORRECTAL
PE2019001307A 2016-12-22 2017-12-21 Benzoisotiazol, isotiazolo[3,4-b]piridina, quinazolina, ftalazina, pirido[2,3-d]piridazina y derivados de pirido[2,3-d]pirimidina como inhibidores de kras g12c para tratar el cancer de pulmon, pancreatico o colorrectal PE20191207A1 (es)

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