AR087354A1 - Inhibidores selectivos de la proteina quinasa - Google Patents

Inhibidores selectivos de la proteina quinasa

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Publication number
AR087354A1
AR087354A1 ARP120102736A ARP120102736A AR087354A1 AR 087354 A1 AR087354 A1 AR 087354A1 AR P120102736 A ARP120102736 A AR P120102736A AR P120102736 A ARP120102736 A AR P120102736A AR 087354 A1 AR087354 A1 AR 087354A1
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AR
Argentina
Prior art keywords
group
optionally substituted
hydrogen
alkyl group
alkyl
Prior art date
Application number
ARP120102736A
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English (en)
Inventor
Alain Moussy
Abdellah Benjahad
Willy Picoul
Anne Lermet
Didier Pez
Jason Martin
Franck Sandrinelli
Emmanuel Chevenier
Original Assignee
Ab Science
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Publication of AR087354A1 publication Critical patent/AR087354A1/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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/435—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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/435—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
    • A61K31/445—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/495—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/435—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Abstract

Estos compuestos modulan, regulan y/o inhiben, en forma selectiva, la señal de transducción mediada por algunas proteínas quinasa nativas y/o mutantes implicadas en diversas enfermedades humanas o animales, tales como los trastornos de proliferación celular, metabólicos, alérgicos y degenerativos. Más particularmente, estos compuestos son potentes y selectivos inhibidores de c-kit nativa y/o mutante.Reivindicación 1: Un compuesto de fórmula (1), o una de sus sales farmacéuticamente aceptables, caracterizado porque: A es un anillo heterociclo de cinco o seis miembros; R1 es hidrógeno, halógeno, un grupo alquilo C1-10, un grupo tioalquilo C1-10 o un grupo alcoxi C1-10; R2 es halógeno, un grupo arilo, un grupo haloalquilo C1-10 o alquilo C1-10, opcionalmente sustituido por, al menos, un heteroátomo opcionalmente sustituido por un haloalquilo C1-10 o alquilo C1-10 opcionalmente sustituido por un grupo solubilizante; así como también un grupo alcoxi C1-10, un grupo tioalquilo C1-10 o un grupo haloalcoxi C1-10; así como también un grupo -COOR, -NRR’, -NR-CO-R’, -CONRR’, -SO2NRR’ o -NR-SO2-R’ donde R y R’ se seleccionan cada uno, independientemente, entre hidrógeno, un grupo arilo, un grupo heteroarilo, un grupo alquilo C1-10 opcionalmente sustituido por, al menos, un heteroátomo opcionalmente sustituido por un grupo alquilo C1-10 opcionalmente sustituido por un grupo solubilizante; así como también un grupo heterociclo o un grupo solubilizante; R3 es hidrógeno, halógeno, ciano, un grupo alquilo C1-10 o un grupo alcoxi C1-10; así como también un grupo CF3, -NRR’, -NR-CO-R’, -CONRR’, -SO2NRR’ donde R y R’ se seleccionan cada uno, independientemente, entre hidrógeno, un grupo alquilo C1-10 opcionalmente sustituido por, al menos, un heteroátomo opcionalmente sustituido por un grupo alquilo C1-10, opcionalmente sustituido por un grupo solubilizante; así como también un grupo heterociclo o un grupo solubilizante; Q es O ó S; W es N o CR4; R4 es hidrógeno, ciano, CF3, halógeno, un grupo tioalquilo C1-10, un grupo alquilo C1-10 opcionalmente sustituido por, al menos, un heteroátomo opcionalmente sustituido por un grupo alquilo C1-10, opcionalmente sustituido por un grupo solubilizante; así como también un grupo alcoxi C1-10 o un grupo haloalcoxi C1-10, un grupo solubilizante, un heterociclo, un grupo -CO-NRR’, SO2-NRR’, -NRR’, NR-CO-R’ o NR-SO2R’, donde R y R’ se seleccionan cada uno, independientemente, entre hidrógeno, un grupo alquilo C1-10 opcionalmente sustituido por, al menos, un heteroátomo, opcionalmente sustituido por un grupo alquilo C1-10, opcionalmente sustituidos por un grupo solubilizante o por un grupo heterociclo; X es N o CR5; R5 es hidrógeno, ciano, halógeno, un grupo alquilo C1-10 o un grupo alcoxi C1-10, -CO-OR, -CO-NRR’, donde R y R’ se seleccionan cada uno, independientemente, entre hidrógeno, un grupo alquilo C1-10 opcionalmente sustituido por, al menos, un heteroátomo opcionalmente sustituido por un grupo alquilo C1-10, opcionalmente sustituido por un grupo solubilizante o por un grupo heterociclo.
ARP120102736A 2011-07-27 2012-07-27 Inhibidores selectivos de la proteina quinasa AR087354A1 (es)

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US201161512165P 2011-07-27 2011-07-27

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AR087354A1 true AR087354A1 (es) 2014-03-19

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Country Link
US (1) US9168245B2 (es)
EP (1) EP2736904B1 (es)
JP (1) JP5944503B2 (es)
KR (1) KR101924247B1 (es)
CN (1) CN103717591B (es)
AR (1) AR087354A1 (es)
AU (1) AU2012288900B2 (es)
BR (1) BR112014001977A2 (es)
CA (1) CA2840029C (es)
CL (1) CL2014000007A1 (es)
ES (1) ES2573831T3 (es)
IL (1) IL230504A0 (es)
MX (1) MX2014001079A (es)
RU (1) RU2612972C2 (es)
TW (1) TW201311676A (es)
WO (1) WO2013014170A1 (es)
ZA (1) ZA201400465B (es)

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