AR079529A1 - Derivados arilo y heteroarilo sustituidos y fundidos como inhibidores de la pi3k - Google Patents

Derivados arilo y heteroarilo sustituidos y fundidos como inhibidores de la pi3k

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Publication number
AR079529A1
AR079529A1 ARP100104746A ARP100104746A AR079529A1 AR 079529 A1 AR079529 A1 AR 079529A1 AR P100104746 A ARP100104746 A AR P100104746A AR P100104746 A ARP100104746 A AR P100104746A AR 079529 A1 AR079529 A1 AR 079529A1
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Argentina
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alkyl
nrc5rd5
independently selected
nrc5c
haloalkyl
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ARP100104746A
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Eddy W Yue
Andrew P Combs
Yun-Long Li
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Incyte Corp
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Medicinal Chemistry (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Emergency Medicine (AREA)
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  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Estos compuestos modulan la actividad de las fosfoinositida 3-quinasas (PI3Ks) y son de utilidad en el tratamiento de las enfermedades asociadas con la actividad de las PI3Ks, lo que, por ejemplo, incluye los trastornos inflamatorios, los trastornos inmunologicos, el cáncer y otras enfermedades. Reivindicacion 1: Se reivindica un compuesto de la formula (1) o una sal farmacéuticamente aceptable del mismo; donde el símbolo ôOö indica que el anillo es aromático; Z es O, S o NRA; Cy es cicloalquilo, heterocicloalquilo, arilo o heteroarilo, cada uno opcionalmente sustituido con 1, 2, 3, 4 o 5 grupos RC independientemente seleccionados; cada RC es seleccionado de manera independiente a partir de halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, halosulfanilo, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, C(=NRe)Rb, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb y S(O)2NRcRd; donde el alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, arilo, cicloalquilo, heteroarilo y heterocicloalquilo son cada uno opcionalmente sustituidos con 1, 2, 3, 4 o 5 sustituyentes seleccionados de manera independiente a partir de halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, halosulfanilo, CN, Cy1, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, NRcS(O)Rb, NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb y S(O)2NRcRd; W es CR3 o N; V es CR4 o N; X es CR5; Y es CR6 o N; y U es CR7 o N; o W es CR3 o N; V es CR4 o N; X es O o S; Y está ausente; y U es CR7 o N; o W es CR3 o N; V es N; X es CR5; Y está ausente; y U es NRA1; o W es CR3 o N; V es O o S; X es CR5; Y está ausente; y U es CR7 o N; con la salvedad que cuando Y esté presente, al menos uno de V, Y y U no es N; R1 es seleccionado de manera independiente a partir de H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6 y alquinilo C2-6 donde el alquilo C1-6, haloalquilo C1-6, alquenilo C2-6 y alquinilo C2-6 son cada uno opcionalmente sustituidos con 1, 2, 3 o 4 sustituyentes seleccionados de manera independiente a partir de halo, OH, CN, NR1+R2+, alcoxi C1-6, haloalcoxi C1-6, tio, alquiltio C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, carbamilo, alquilcarbamilo C1-6, di(alquil C1-6)carbamilo, carboxi, alquilcarbonoilo C1-6, alcoxi carbonoilo C1-6 y alquilcarbonoilamino C1-6; cada R1+ y R2+ es seleccionado de manera independiente a partir de H y alquilo C1-6; o cualquier R1+ y R2+, conjuntamente con el átomo de N al cual se encuentran acoplados, forman un grupo heterocicloalquilo de 3, 4, 5, 6 o 7 miembros, el cual es opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes seleccionados de manera independiente a partir de alquilo C1-6; R2, R3, R4, R5, R6 y R7 son cada uno seleccionado de manera independiente a partir de H, OH, NO2, CN, halo, alquilo C1-6, alquinilo C1-6, cicloalquilo C3-7, haloalquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, amino, alquilamino C1-6, di(alquil C1-6)amino, tio, alquiltio C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, carbamilo, alquilcarbamilo C1-6, di(alquil C1-6)carbamilo, carboxi, alquilcarbonoilo C1-6 y alcoxi carbonoilo C1-6; Ar es un heteroarilo, sustituido con 1, 2, 3, 4 o 5 grupos RD independientemente seleccionados; cada RD es seleccionado de manera independiente a partir de H, -(alquil C1-4)r-Cy1, halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, halosulfanilo, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe)NRc1Rd1, NRc1C(=NRe)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1 y S(O)2NRc1Rd1; RA es seleccionado a partir de H, alquilo C1-6, alquenilo C2-6 y alquinilo C2-6, RA1 es seleccionado a partir de H, alquilo C1-6, alquenilo C2-6 y alquinilo C2-6; cada Cy1 independientemente representa arilo, heteroarilo, cicloalquilo, o heterocicloalquilo, cada uno opcionalmente sustituido por 1, 2, 3, 4 o 5 sustituyentes seleccionados de manera independiente a partir de halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, halosulfanilo, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe)NRc1Rd1, NRc1C(=NRe)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1 y S(O)2NRc1Rd1; cada Ra, Rb, Rc y Rd es seleccionado de manera independiente a partir de H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo, donde el alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo es opcionalmente sustituido con 1, 2, 3, 4 o 5 sustituyentes seleccionados de manera independiente a partir de alquilo C1-6, haloalquilo C1-6, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(=NRf)NRc5Rd5, NRc5C(=NRf)NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5 y S(O)2NRc5Rd5; o cualquier Rc y Rd, conjuntamente con el átomo de N al cual se encuentran acoplados, forman un grupo heterocicloalquilo de 3, 4, 5, 6 o 7 miembros o un grupo heteroarilo, cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de manera independiente a partir de alquilo C1-6, haloalquilo C1-6, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(=NRf)NRc5Rd5, NRc5C(=NRf)NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5 y S(O)2NRc5Rd5; cada Re y Rf es seleccionado de manera independiente a partir de H, alquilo C1-6, CN, ORa5, SRb5, S(O)2Rb5, C(O)Rb5, S(O)2NRc5Rd5 y C(O)NRc5Rd5; cada Ra1, Rb1, Rc1 y Rd1 es seleccionado de manera independiente a partir de H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo, donde el alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo es opcionalmente sustituido con 1, 2, 3, 4 o 5 sustituyentes seleccionados de manera independiente a partir de alquilo C1-6, haloalquilo C1-6, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(=NRf)NRc5Rd5, NRc5C(=NRf)NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5 y S(O)2NRc5Rd5; o cualquier Rc1 y Rd1, conjuntamente con el átomo de N al cual se encuentran acoplados, forman un grupo heterocicloalquilo de 3, 4, 5, 6 o 7 miembros o un grupo heteroarilo, cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de manera independiente a partir de alquilo C1-6, haloalquilo C1-6, halo, CN, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(=NRf)NRc5Rd5, NRc5C(=NRf)NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5 y S(O)2NRc5Rd5; cada Ra5, Rb5, Rc5 y Rd5 es seleccionado de manera independiente a partir de H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo, donde el alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo es opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de manera independiente a partir de OH, CN, amino, halo, alquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquilamino C1-6, di(alquil C1-6)amino, haloalquilo C1-6 y haloalcoxi C1-6, o cualquier Rc5 y Rd5, conjuntamente con el átomo de N al cual se encuentran acoplados, forman un grupo heterocicloalquilo de 3, 4, 5, 6 o 7 miembros o grupo heteroarilo, cada uno opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de manera independiente a partir de OH, CN, amino, halo, alquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquilamino C1-6, di(alquil C1-6)amino, haloalquilo C1-6 y haloalcoxi C1-6; y r es igual a 0 o 1; con la salvedad que el compuesto es distinto a: 2-((1-(9H-fluoren-9-il)naftalen-2-il)metiltio)piridina; y 7'-((1H-benzo[d]imidazol-6-ilamino)metil)-N-metil-6,8'-biquinazolin-2-amina; o una sal farmacéuticamente aceptable del mismo.
ARP100104746A 2009-12-18 2010-12-17 Derivados arilo y heteroarilo sustituidos y fundidos como inhibidores de la pi3k AR079529A1 (es)

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