AR075633A1 - Compuestos moduladores de jak quinasa y sus metodos de uso - Google Patents

Compuestos moduladores de jak quinasa y sus metodos de uso

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Publication number
AR075633A1
AR075633A1 ARP100100585A ARP100100585A AR075633A1 AR 075633 A1 AR075633 A1 AR 075633A1 AR P100100585 A ARP100100585 A AR P100100585A AR P100100585 A ARP100100585 A AR P100100585A AR 075633 A1 AR075633 A1 AR 075633A1
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AR
Argentina
Prior art keywords
alkyl
halo
alkynyl
alkenyl
cycloalkyl
Prior art date
Application number
ARP100100585A
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English (en)
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Ambit Biosciences Corp
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Publication date
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Publication of AR075633A1 publication Critical patent/AR075633A1/es

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    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/535—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

Abstract

Se proveen en la presente compuestos de quinazolina para el tratamiento de enfermedades mediadas por JAK quinasa, que incluye enfermedades mediadas por JAK2 quinasa, JAK3 quinasa o TYK2 quinasa. Se proveen además composiciones farmacéuticas que comprenden el compuesto y métodos para usar los compuestos y composiciones. Reivindicacion 1: Un compuesto que tiene formula (1) o sus sales, solvatos o hidratos farmacéuticamente aceptables, en donde R1 y R2 se seleccionan de (i), (ii), (iii), (iv) y (v) como sigue: (i) R1 y R2 juntos forman =O, =S, =NR9 o =CR10R11; (ii) R1 y R2 son ambos -OR8, o R1 y R2, junto con el átomo de carbono al cual están unidos, forman dioxacicloalquilo; (iii) R1 es hidrogeno o halo; y R2 es halo; y (iv) R1 es alquilo, alquenilo, alquinilo, cicloalquilo o arilo, en donde el alquilo, alquenilo, alquinilo, cicloalquilo o arilo está opcionalmente sustituido por uno o mas sustituyentes seleccionados de halo, ciano, alquilo, -RxORw, -RxS(O)qRv, -RxNRyRz y -C(O)ORw; y R2 es hidrogeno, halo o -OR8; y (v) R1 es halo, deutero, -OR12, -NR13R14, o -S(O)qR15; y R2 es hidrogeno, deutero, alquilo, alquenilo, alquinilo, cicloalquilo o arilo, en donde el alquilo, alquenilo, alquinilo, cicloalquilo o arilo, está opcionalmente sustituido con uno o mas sustituyentes seleccionados de halo, ciano, alquilo, -RxORw, -RxS(O)qRv y -RxNRyRz; R3 es hidrogeno, halo, alquilo, ciano, haloalquilo, cicloalquilo, cicloalquilalquilo, hidroxi o alcoxi; R4 y R5 son cada uno independientemente hidrogeno o alquilo; cada R6 se selecciona independientemente de halo, alquilo, alquenilo, alquinilo, haloalquilo, cicloalquilo, RxOR18, RxNR19R20, y RxS(O)qRv, cada R7 se selecciona independientemente de halo, alquilo, haloalquilo o - RxORw; R8 es alquilo, alquenilo o alquinilo; R9 es hidrogeno, alquilo, haloalquilo, hidroxi, alcoxi o amino; R10 es hidrogeno o alquilo; R11 es hidrogeno, alquilo, haloalquilo o -C(O)OR8; R12 se selecciona de hidrogeno, alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, -C(O)Rv, -C(O)ORw y -C(O)NRyRz, en donde el alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, aralquilo, heteroarilo o heteroaralquilo están cada uno opcionalmente sustituidos por uno o mas sustituyentes independientemente seleccionados de halo, oxo, alquilo, hidroxi, alcoxi, amino y alquiltio; R13 y R14 se seleccionan como sigue: (i) R13 es hidrogeno o alquilo; y R14 se selecciona de hidrogeno, alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, alcoxi, -C(O)Rv, -C(O)ORw, C(O)NRyRz y -S(O)qRv, en donde el alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, aralquilo, heteroarilo o heteroaralquilo están cada uno opcionalmente sustituidos por uno o mas sustituyentes independientemente seleccionados de halo, oxo, alquilo, hidroxi, alcoxi, amino y alquiltio; o (ii) R13 y R14, junto con el átomo de nitrogeno al cual están unidos, forman heterociclilo o heteroarilo en donde el heterociclilo o heteroarilo está opcionalmente sustituido por uno o mas sustituyentes independientemente seleccionados de halo, alquilo, hidroxi, alcoxi, amino y alquiltio y en donde el heterociclilo también está opcionalmente sustituido con oxo; R15 es alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, -C(O)NRyRz o -NRyRz, en donde el alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, aralquilo, heteroarilo o heteroaralquilo están cada uno opcionalmente sustituidos por uno o mas sustituyentes independientemente seleccionados de halo, oxo, alquilo, hidroxi, alcoxi, amino y alquiltio; R18 es hidrogeno, alquilo, haloalquilo, hidroxi-C2-6alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, aralquilo, heteroarilo o heteroarilalquilo; en donde R18 está opcionalmente sustituido por 1 a 3 grupos Q1, cada Q1 independientemente seleccionado de alquilo, hidroxilo, halo, haloalquilo, alcoxi, ariloxi, alcoxialquilo, alcoxicarbonilo, alcoxisulfonilo, carboxilo, cicloalquilo, heterociclilo, arilo, heteroarilo, haloarilo y amino; R19 y R20 se seleccionan como sigue: (i) R19 y R20 son cada uno independientemente hidrogeno o alquilo; o (ii) R19 y R20, junto con el átomo de nitrogeno al cual están unidos, forman un heterociclilo o heteroarilo que está opcionalmente sustituido por 1 a 2 grupos cada uno independientemente seleccionado de halo, alquilo, haloalquilo, hidroxilo y alcoxi; cada Rx es independientemente alquileno o un enlace directo; Rv es hidrogeno, alquilo, alquenilo o alquinilo; Rw es independientemente hidrogeno, alquilo, alquenilo, alquinilo o haloalquilo; Ry y Rz se seleccionan como sigue: (i) Ry y Rz son cada uno independientemente hidrogeno, alquilo, alquenilo, alquinilo, cicloalquilo o haloalquilo; (ii) Ry y Rz, junto con el átomo de nitrogeno al cual están unidos, forman un heterociclilo o heteroarilo que está opcionalmente sustituido por 1 a 2 grupos cada uno independientemente seleccionado de halo, alquilo, haloalquilo, hidroxilo y alcoxi; n es 0-4; p es 0-5; y cada q es independientemente 0, 1 o 2.
ARP100100585A 2009-02-27 2010-02-26 Compuestos moduladores de jak quinasa y sus metodos de uso AR075633A1 (es)

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US15644709P 2009-02-27 2009-02-27
US29408310P 2010-01-11 2010-01-11
US29449010P 2010-01-13 2010-01-13

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AR075633A1 true AR075633A1 (es) 2011-04-20

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US (3) US8349851B2 (es)
EP (1) EP2401267B1 (es)
JP (1) JP5746981B2 (es)
KR (1) KR20110124787A (es)
CN (3) CN105601619A (es)
AR (1) AR075633A1 (es)
AU (1) AU2010217929B2 (es)
BR (1) BRPI1013347A2 (es)
CA (1) CA2752885A1 (es)
DK (1) DK2401267T3 (es)
ES (1) ES2456275T3 (es)
HK (1) HK1165789A1 (es)
HR (1) HRP20140174T1 (es)
IL (1) IL214768A (es)
MX (1) MX2011008995A (es)
MY (1) MY159327A (es)
NZ (1) NZ594661A (es)
PL (1) PL2401267T3 (es)
PT (1) PT2401267E (es)
RU (1) RU2529019C2 (es)
SG (1) SG173852A1 (es)
SI (1) SI2401267T1 (es)
TW (1) TWI476192B (es)
WO (1) WO2010099379A1 (es)
ZA (1) ZA201106126B (es)

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