AR076486A1 - Inhibidores de fosfoinositida 3 kinasa y composiciones farmaceuticas que los contienen. - Google Patents

Inhibidores de fosfoinositida 3 kinasa y composiciones farmaceuticas que los contienen.

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Publication number
AR076486A1
AR076486A1 ARP100101435A ARP100101435A AR076486A1 AR 076486 A1 AR076486 A1 AR 076486A1 AR P100101435 A ARP100101435 A AR P100101435A AR P100101435 A ARP100101435 A AR P100101435A AR 076486 A1 AR076486 A1 AR 076486A1
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AR
Argentina
Prior art keywords
nrara
alkyl
crcrc
nra
orb
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ARP100101435A
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English (en)
Inventor
Shon Booker
Kristin Andrews
Victor J Cee
Kevin Yang
Nuria A Tamayo
Nobuko Nishimura
Bradley J Herberich
Mark H Norman
Longbin Liu
Claire L M Jackson
Fang-Tsao Hong
Anthony B Reed
Adrian L Smith
Hongyu Liao
Seifu Tadesse
Brian A Lanman
Angelo Noel D
Bin Wu
Ryan Wurz
Liping H Pettus
Yunxin Bo
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Amgen Inc
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Publication of AR076486A1 publication Critical patent/AR076486A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero 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
    • C07D417/14—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

La presente se refiere a compuestos de formula (1) y a usos para la fabricacion de medicamentos para tratar enfermedades o afecciones, tal como cáncer, usando los compuestos; y composiciones farmacéuticas que contienen los compuestos. Reivindicacion 1: Un compuesto de la formula (1), o una sal farmacéuticamente aceptable del mismo, caracterizado porque Ar1 es un anillo monocíclico o bicíclico de 5 hasta 10 miembros que puede contener desde cero hasta cuatro heteroátomos independientemente seleccionados de O, N o S, y cuyo anillo puede estar no substituido o substituido con grupos independientemente seleccionados de haloalquilo C1-4, halo, oxo, -OCHF2, -CN, nitro, -C(=O)NRaRa, -C(=O)Rb, -C(=O)ORb, -C(=NRa)NRaRa, -ORa, -OC(=O)Rb, -OC(=O)NRaRa, -O-alquilo C1-6N(Ra)C(=O)ORb, -OC(=O)N(Ra)S(=O)2Rb, -O-alquilo C2-6NRaRa, -O-alquilo C2-6ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Rb, -S(=O)2N(Ra)C(=O)ORb, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRa-alquilo C2-6NRaRa, -NRa-alquilo C2-6ORa, -alquilo C1-6, -alquenilo C2-6, o -alquinilo C2-6, en donde -alquilo C1-6, -alquenilo C2-6, o -alquinilo C2-6 se substituyen por 0, 1, 2 o 3 substituyentes independientemente seleccionados de haloalquilo C1-4, halo, ciano, nitro, -C(=O)Rb, -C(=O)ORb, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Rb, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Rb, -O-alquilo C2-6NRaRa, -O-alquilo C2-6ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Rb, -S(=O)2N(Ra)C(=O)ORb, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRa-alquilo C2-6NRaRa, -NRa-alquilo C2-6ORa, -N(Ra)(CRaRa)n-Y, -(CRaRa)nY, o -(CRaRa)nORa; Y es un anillo monocíclico saturado, parcialmente saturado o insaturado de 5, 6 o 7 miembros o anillo bicíclico de 6, 7, 8, 9 o 10 miembros que contiene 0, 1, 2, 3 o 4 heteroátomos independientemente seleccionados de N, O y S, el cual está substituido con 0, 1 o 2 substituyentes independientemente seleccionados de alquilo C1-8, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-4, halo, -CN, nitro, -C(=O)Rb, -C(=O)ORb, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Rb, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Rb, -O-alquilo C2-6NRaRa, -O-alquilo C2-6ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Rb, -S(=O)2N(Ra)C(=O)ORb, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRa-alquilo C2-6NRaRa o -NRa-alquilo C2-6ORa; cada Ra es independientemente hidrogeno o Rb; cada Rb es independientemente fenilo, bencilo, alquilo C1-6, heterocicloalquilo C4-8, o cicloalquilo C3-8, en donde el fenilo, bencilo, alquilo C1-6, heterocicloalquilo C4-8 o cicloalquilo C3-8 está substituido por 0, 1, 2 o 3 substituyentes independientemente seleccionados de halo, -OH, -S(=O)2Rb, -O-alquilo C2-6ORa, alquilo C1-4, haloalquilo C1-3, -O-alquilo C1-4, -NH2, -CN, o NRaRa; cada Rc es independientemente hidrogeno, -ORa, -NRaRa, -CF3, alquilo C1-6, o el grupo CRcRc puede formar un anillo de cicloalquilo C3-8; cada n es independientemente 0, 1, 2 o 3; cada Z1, Z2, Z3 o Z4 está independientemente seleccionado de N, NR o CR; o Z1 y Z2, Z2 y Z3, o Z3 y Z4, cuando NR o CR, puede formar un anillo de 5 o 6 miembros cuando los dos R se toman junto con los átomos de carbono o nitrogeno a los cuales se enlazan, y el anillo puede contener desde cero hasta tres heteroátomos independientemente seleccionados de O, N o S, y el anillo puede estar no substituido o substituido con grupos independientemente seleccionados de haloalquilo C1-4, halo, -CN, nitro, -C(=O)NRaRa, -C(=O)Rb, -C(=O)ORb, -C(=NRa)NRaRa, -ORa, -OC(=O)Rb, -OC(=O)NRaRa, -O-alquilo C1-6N(Ra)C(=O)ORb, -OC(=O)N(Ra)S(=O)2Rb, -O-alquilo C2-6NRaRa, -O-alquilo C2-6ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Rb, -S(=O)2N(Ra)C(=O)ORb, -S(=O)2N(Ra)C(=O)NRaRa, -(CRcRc)nNRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRa-alquilo C2-6NRaRa, -NRa-alquilo C2-6ORa, -(CRcRc)n-heterocicloalquilo C4-8, -(CRcRc)n-arilo C6-8, -(CRcRc)n-heteroarilo C5-8, -(CRcRc)nO(CRcRc)n-arilo C6-8, -(CRcRc)nN(Ra)(CRcRc)n-arilo C6-8, -(CH2)nN(Ra)(CRcRc)n-heteroarilo C5-8, -(CRcRc)nO(CRcRc)n-heteroarilo C5-8, -alquilo C1-6, -alquenilo C2-6, o -alquinilo C2-6, en donde el alquilo C1-6, alquenilo C2-6, alquinilo C2-6, heterocicloalquilo C4-8, arilo C6-8 o heteroarilo C5-8 se substituyen por 0, 1, 2 o 3 substituyentes independientemente seleccionados de haloalquilo C1-4, halo, ciano, nitro, -C(=O)Rb, -C(=O)ORb, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Rb, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Rb, -O-alquilo C2-6NRaRa, -O-alquilo C2-6ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Rb, -S(=O)2N(Ra)C(=O)ORb, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRa-alquilo C2-6NRaRa, -NRa-alquilo C2-6ORa, -N(Ra)(CRaRa)n-Y, -(CRaRa)nY, o -(CRaRa)nORa; cada R está independientemente seleccionado de hidrogeno, oxo, haloalquilo C1-4, halo, -OCHF2, -CN, nitro, -C(=O)NRaRa, -C(=O)Rb, -C(=O)ORb, -C(=NRa)NRaRa, -ORa, -OC(=O)Rb, -(CRaRa)nORa, -OC(=O)NRaRa, -O-alquilo C1-6N(Ra)C(=O)ORb, -OC(=O)N(Ra)S(=O)2Rb, -O-alquilo C2-6NRaRa, -O-alquilo C2-6ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Rb, -S(=O)2N(Ra)C(=O)ORb, -S(=O)2N(Ra)C(=O)NRaRa, -(CRcRc)nNRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRa-alquilo C2-6NRaRa, -NRa-alquilo C2-6ORa, -(CRcRc)n-heterocicloalquilo C4-8, -(CRcRc)n-arilo C6-8, -(CRcRc)n-heteroarilo C5-8, -(CRcRc)n-O(CRcRc)n-arilo C6-8, -(CRcRc)n-cicloalquilo C3-8, -(CRcRc)n-heterocicloalquilo C4-8, -(CRcCRc)nO(CRcCRc)nCF3, -(CRcCRc)nN(CRcRc)ORa, -(CRcRc)nN(Ra)(CRcRc)n-arilo C6-8, -(CRcRc)nN(Ra)(CRcRc)n-heteroarilo C5-8, -(CRcRc)nO(CRcRc)n-heteroarilo C5-8, -alquilo C1-6, -alquenilo C2-6, o -alquinilo C2-6, en donde alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo C6-8, heterocicloalquilo C4-8, cicloalquilo C3-8 o heteroarilo C5-8 se substituyen por 0, 1, 2 o 3 substituyentes independientemente seleccionados de haloalquilo C1-4, halo, oxo, alquilo C1-6, ciano, nitro, -C(=O)Rb, -C(=O)ORb, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Rb, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Rb, -O-alquilo C2-6NRaRa, -Oalquilo C2-6ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Rb, -S(=O)2N(Ra)C(=O)ORb, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRa-alquilo C2-6NRaRa o -NRa-alquilo C2-6ORa; -N(Ra)(CRaRa)n-Y, -(CRaRa)nY, -(CRaRa)n-cicloalquilo C3-8, o -(CRaRa)nORa; Q es un resto de formula (2); R2 es metilo o etilo; Z5 es N o CRc; Z9 es N, NR o CR; Z10 es N, NR, o CR, o Z9 y Z10 puede formar un anillo de 5 o 6 miembros cuando los dos R se toman junto con los átomos de carbono o nitrogeno a los cuales se enlazan, y el anillo puede contener desde cero hasta tres heteroátomos independientemente seleccionados de O, N o S, y el anillo puede estar no substituido o substituido con grupos independientemente seleccionados de haloalquilo C1-4, halo, -CN, nitro, -C(=O)NRaRa, -C(=O)Rb, -C(=O)ORb, -C(=NRa)NRaRa, -ORa, -OC(=O)Rb, -OC(=O)NRaRa, -O-alquilo C1-6N(Ra)C(=O)ORb, -OC(=O)N(Ra)S(=O)2Rb, -O-alquilo C2-6NRaRa, -O-alquilo C2-6ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Rb, -S(=O)2N(Ra)C(=O)ORb, -S(=O)2N(Ra)C(=O)NRaRa, -(CRcRc)nNRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRa-alquilo C2-6NRaRa, -NRa-alquilo C2-6ORa, -(CRcRc)n-cicloalquilo C3-8, -(CRcRc)n-heterocicloalquilo C4-8, -(CRcRc)n-arilo C6-8, -(CRcRc)n-heteroarilo C5-8, -(CRcRc)nO(CRcRc)n-arilo C6-8, -(CRcRc)nN(Ra)(CRcRc)n-arilo C6-8, -(CRcRc)nN(Ra)(CRcRc)n-heteroarilo C5-8, (CRcRc)nO(CRcRc)n-heteroarilo C5-8, -alquilo C1-6, -alquenilo C2-6, o -alquinilo C2-6, en donde alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, heterocicloalquilo C4-8, arilo C6-8 o heteroarilo C5-8 se substituyen por 0, 1, 2 o 3 substituyentes independientemente seleccionados de haloalquilo C1-4, halo, ciano, nitro, -C(=O)Rb, -C(=O)ORb, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Rb, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Rb, -O-alquilo C2-6NRaRa, -O-alquilo C2-6ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Rb, -S(=O)2N(Ra)C(=O)ORb, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRa-alquilo C2-6NRaRa o -NRa-alquilo C2-6ORa; -N(Ra)(CRaRa)n-Y, -(CRaRa)nY, o -(CRaRa)nORa; y el grupo NRaRa, ya sea solo o una parte de un grupo más grande, puede ser un anillo heterocíclico de 4 hasta 6 miembros en donde los dos Ra tomados junto con el átomo de nitrogeno a los cuales se enlazan forman un anillo que puede tener desde cero hasta un heteroátomo adicional seleccionado de N, O o S, y el anillo puede estar substituido o no substituido con desde 1 hasta 3 substituyentes independientemente seleccionados de oxo, halo, -CN, nitro, -C(=O)Rc, -C(=O)ORc, -ORc, -OC(=O)Rc, -SRc, -S(=O)Rc, -S(=O)2Rc, -S(=O)2NRcRc, -NRcRc, -alquilo C1-6, -alquenilo C2-6, o -alquinilo C2-6.
ARP100101435A 2009-04-28 2010-04-28 Inhibidores de fosfoinositida 3 kinasa y composiciones farmaceuticas que los contienen. AR076486A1 (es)

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