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
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    • 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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    • 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
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    • 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Engineering & Computer Science (AREA)
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  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
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  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
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  • Endocrinology (AREA)
  • Emergency 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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Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5789252B2 (ja) 2009-05-07 2015-10-07 インテリカイン， エルエルシー 複素環式化合物およびその使用
PL2448938T3 (pl) 2009-06-29 2014-11-28 Incyte Holdings Corp Pirymidynony jako inhibitory PI3K
US8759359B2 (en) * 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
EP2345643A1 (en) * 2009-12-29 2011-07-20 Polichem S.A. New tertiary 8-hydroxyquinoline-7-carboxamide derivatives and uses thereof
WO2011130342A1 (en) 2010-04-14 2011-10-20 Incyte Corporation FUSED DERIVATIVES AS ΡI3Κδ INHIBITORS
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
US20140031355A1 (en) * 2010-11-04 2014-01-30 Amgen Inc. Heterocyclic compounds and their uses
WO2012064973A2 (en) 2010-11-10 2012-05-18 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
JP5961187B2 (ja) 2010-12-20 2016-08-02 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｐｉ３ｋ阻害剤としてのｎ−（１−（置換フェニル）エチル）−９ｈ−プリン−６−アミン
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
HUE030869T2 (en) 2011-09-02 2017-06-28 Incyte Holdings Corp Heterocyclic amines as inhibitors of PI3K
BR112014014327A2 (pt) 2011-12-15 2017-06-13 Novartis Ag uso de inibidores da atividade ou função de pi3k
WO2013090725A1 (en) * 2011-12-15 2013-06-20 Philadelphia Health & Education Corporation NOVEL PI3K p110 INHIBITORS AND METHODS OF USE THEREOF
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
JP6434416B2 (ja) 2012-11-08 2018-12-05 ライゼン・ファーマシューティカルズ・エスアー ＰＤＥ４阻害剤とＰＩ３δ阻害剤または二重ＰＩ３δ−γキナーゼ阻害剤とを含有する薬学的組成物
EP2920172B1 (en) * 2012-11-16 2019-12-25 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
JP6437452B2 (ja) 2013-01-14 2018-12-12 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｐｉｍキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物
MX2015009057A (es) 2013-01-15 2015-10-05 Incyte Corp Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de cinasa pim.
TWI736135B (zh) 2013-03-01 2021-08-11 美商英塞特控股公司 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途
TW201605866A (zh) 2013-08-23 2016-02-16 英塞特公司 可用作ｐｉｍ激酶抑制劑之呋喃并－及噻吩并－吡啶甲醯胺化合物
UA119767C2 (uk) 2014-04-08 2019-08-12 Інсайт Корпорейшн Лікування b-клітинних злоякісних новоутворень із застосуванням комбінації інгібіторів jak та pi3k
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
US9637488B2 (en) 2015-01-29 2017-05-02 Fuqiang Ruan Heterocyclic compounds as inhibitors of class I PI3KS
WO2016130501A1 (en) 2015-02-09 2016-08-18 Incyte Corporation Aza-heteroaryl compounds as pi3k-gamma inhibitors
AU2016222556B2 (en) 2015-02-27 2020-08-27 Incyte Holdings Corporation Salts of Pl3K inhibitor and processes for their preparation
WO2016183071A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Hetero-tricyclic compounds and their use for the treatment of cancer
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US9540347B2 (en) 2015-05-29 2017-01-10 Incyte Corporation Pyridineamine compounds useful as Pim kinase inhibitors
WO2017000125A1 (en) * 2015-06-29 2017-01-05 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
US9708333B2 (en) 2015-08-12 2017-07-18 Incyte Corporation Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors
WO2017035366A1 (en) 2015-08-26 2017-03-02 Incyte Corporation Pyrrolopyrimidine derivatives as tam inhibitors
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
AR106595A1 (es) 2015-11-06 2018-01-31 Incyte Corp COMPUESTOS HETEROCÍCLICOS COMO INHIBIDORES DE PI3K-g
US20170190689A1 (en) 2016-01-05 2017-07-06 Incyte Corporation Pyridine and pyridimine compounds as pi3k-gamma inhibitors
PE20190175A1 (es) 2016-03-28 2019-02-01 Incyte Corp Compuestos de pirrolotriazina como inhibidores de tam
TW201803871A (zh) 2016-06-24 2018-02-01 英塞特公司 作為ＰＩ３Ｋ-γ抑制劑之雜環化合物
KR101798840B1 (ko) 2017-05-17 2017-11-17 주식회사 레고켐 바이오사이언스 신규 오토탁신 저해 화합물 및 이를 함유하는 약제학적 조성물
KR20200088308A (ko) 2017-09-27 2020-07-22 인사이트 코포레이션 Tam 억제제로서 유용한 피롤로트리아진 유도체의 염
JP7244504B2 (ja) 2017-10-18 2023-03-22 インサイト・コーポレイション ＰＩ３Ｋ－γ阻害剤としての三級ヒドロキシ基で置換された縮合イミダゾール誘導体
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
JP2021515767A (ja) 2018-03-07 2021-06-24 バイエル・アクチエンゲゼルシヤフト Ｅｒｋ５阻害剤の同定及び使用
WO2019232188A1 (en) 2018-06-01 2019-12-05 Incyte Corporation Dosing regimen for the treatment of pi3k related disorders
AR117600A1 (es) 2018-06-29 2021-08-18 Incyte Corp Formulaciones de un inhibidor de axl / mer
PT3847175T (pt) 2018-09-05 2024-04-16 Incyte Corp Formas cristalinas de um inibidor da fosfoinositídeo 3-quinase (pi3k)
WO2020077174A1 (en) * 2018-10-12 2020-04-16 Board Of Regents Of The University Of Nebraska Phosphodiesterase inhibitors
WO2020102198A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
WO2020102216A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Substituted heterocyclic derivatives as pi3k inhibitors
US11161838B2 (en) 2018-11-13 2021-11-02 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
US20230060425A1 (en) 2019-02-26 2023-03-02 Bayer Aktiengesellschaft Fused bicyclic heterocycle derivatives as pesticides
TW202114681A (zh) 2019-07-02 2021-04-16 美商ｅＦＦＥＣＴＯＲ醫療公司 轉譯抑制劑及其用途
WO2021257863A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
WO2022006457A1 (en) 2020-07-02 2022-01-06 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
WO2022006456A1 (en) 2020-07-02 2022-01-06 Incyte Corporation Tricyclic pyridone compounds as jak2 v617f inhibitors
WO2022046989A1 (en) 2020-08-27 2022-03-03 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
US11919908B2 (en) 2020-12-21 2024-03-05 Incyte Corporation Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors
US11958861B2 (en) 2021-02-25 2024-04-16 Incyte Corporation Spirocyclic lactams as JAK2 V617F inhibitors
TW202320787A (zh) * 2021-08-11 2023-06-01 大陸商泰州億騰景昂藥業股份有限公司 一種周期蛋白依賴性激酶抑制劑

Family Cites Families (135)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3169967A (en) * 1957-11-14 1965-02-16 Ciba Geigy Corp Methyl o-lower alkanoyl-reserpates
US3037980A (en) * 1955-08-18 1962-06-05 Burroughs Wellcome Co Pyrrolopyrimidine vasodilators and method of making them
US3506643A (en) * 1966-12-09 1970-04-14 Max Thiel N**6-aralkyl-adenosine derivatives
DE2139107A1 (de) 1971-08-04 1973-02-15 Merck Patent Gmbh Heterocyclisch substituierte adenosinverbindungen
US3962443A (en) * 1972-08-14 1976-06-08 Dainippon Pharmaceutical Co., Ltd. Antibacterial pharmaceutical compositions and processes for preparation thereof
DE2248232A1 (de) 1972-10-02 1974-04-11 Basf Ag 4-thiopyrimido eckige klammer auf 4,5-d eckige klammer zu pyrimidine
AR204003A1 (es) 1973-04-03 1975-11-12 Dainippon Pharmaceutical Co Procedimiento para preparar compuestos derivados del acido 2-(1-piperazinil)-5-oxopirido-(2,3-d)pirimidino-6-carboxilico y sus sales farmaceuticamente aceptables
US3862189A (en) * 1973-08-14 1975-01-21 Warner Lambert Co Aralkyl-substituted purines and pyrimidines as antianginal bronchodilator agents
US3936454A (en) * 1973-08-14 1976-02-03 Warner-Lambert Company 5-Amino-4-chloro-6-(substituted amino)-pyrimidines
DK3375A (es) 1974-01-25 1975-09-15 Ciba Geigy Ag
JPS58162949A (ja) * 1982-03-20 1983-09-27 Konishiroku Photo Ind Co Ltd ハロゲン化銀カラ−写真感光材料
JPS6190153A (ja) * 1984-10-09 1986-05-08 Fuji Photo Film Co Ltd ハロゲン化銀写真感光材料の処理方法
JPS6310746A (ja) * 1986-07-01 1988-01-18 Tanabe Seiyaku Co Ltd ナフタレン誘導体
CA1324609C (en) 1986-07-30 1993-11-23 Eastman Kodak Company Photographic element and process
US4861701A (en) * 1987-10-05 1989-08-29 Eastman Kodak Company Photographic element and process comprising a compound which comprises two timing groups in sequence
AT388372B (de) 1987-10-08 1989-06-12 Tanabe Seiyaku Co Neue naphthalinderivate und sie enthaltende pharmazeutika
WO1989008113A1 (fr) * 1988-03-02 1989-09-08 Yoshitomi Pharmaceutical Industries, Ltd. COMPOSES DE 3,4-DIHYDROTHIENO[2,3-d]PYRIMIDINE ET LEURS APPLICATIONS PHARMACOLOGIQUES
US5208250A (en) * 1988-05-25 1993-05-04 Warner-Lambert Company Known and selected novel arylmethylenyl derivatives of thiazolidinones, imidazolidinones and oxazolidinones useful as antiallergy agents and anti-inflammatory agents
JPH07107055B1 (es) * 1990-04-25 1995-11-15
SU1712359A1 (ru) 1990-05-07 1992-02-15 Уфимский Нефтяной Институт Гидрохлорид 8 @ -гидроксихинолинового эфира 8-гидроксихинолин-7-карбоновой кислоты, в качестве бактерицида дл подавлени сульфатвосстанавливающих бактерий и культур РSеUDомоNаS и АRтнRовастеR
US5480883A (en) * 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
IL101860A0 (en) * 1991-05-31 1992-12-30 Ici Plc Heterocyclic derivatives
JP3108483B2 (ja) * 1991-09-30 2000-11-13 日清製粉株式会社 インドール誘導体およびこれを有効成分とする抗潰瘍薬
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
FR2714907B1 (fr) * 1994-01-07 1996-03-29 Union Pharma Scient Appl Nouveaux dérivés de l'Adénosine, leurs procédés de préparation, compositions pharmaceutiques les contenant.
US6342501B1 (en) * 1994-02-25 2002-01-29 The Regents Of The University Of Michigan Pyrrolo[2,3-d] pyrimidines as antiviral agents
JPH09176162A (ja) * 1995-12-22 1997-07-08 Toubishi Yakuhin Kogyo Kk チアゾリジンジオン誘導体及びその製造法並びにそれを含む医薬組成物
AU698419B2 (en) * 1996-07-03 1998-10-29 Dainippon Sumitomo Pharma Co., Ltd. A novel purine derivative
US5866702A (en) * 1996-08-02 1999-02-02 Cv Therapeutics, Incorporation Purine inhibitors of cyclin dependent kinase 2
US6630496B1 (en) * 1996-08-26 2003-10-07 Genetics Institute Llc Inhibitors of phospholipase enzymes
CA2309350C (en) * 1997-11-12 2007-04-03 Mitsubishi Chemical Corporation Purine derivatives and medicaments comprising the same as active ingredient
TW572758B (en) * 1997-12-22 2004-01-21 Sumitomo Pharma Type 2 helper T cell-selective immune response inhibitors comprising purine derivatives
US6828344B1 (en) * 1998-02-25 2004-12-07 Genetics Institute, Llc Inhibitors of phospholipase enzymes
US6479487B1 (en) * 1998-02-26 2002-11-12 Aventis Pharmaceuticals Inc. 6, 9-disubstituted 2-[trans-(4-aminocyclohexyl)amino] purines
CZ20003960A3 (cs) * 1998-05-04 2002-04-17 Zentaris Ag Deriváty indolu a jejich pouľití pro léčení maligních a jiných chorob vyvolaných patologickou proliferací buněk
JP4549534B2 (ja) * 1998-05-26 2010-09-22 中外製薬株式会社 複素環を有するインドール誘導体及びモノ又はジアザインドール誘導体
JP3997651B2 (ja) 1998-06-24 2007-10-24 コニカミノルタホールディングス株式会社 新規色素及び画像記録材料及び感熱転写材料及びインクジェット記録液
DE69942097D1 (de) 1998-08-11 2010-04-15 Novartis Ag Isochinoline derivate mit angiogenesis-hemmender wirkung
AU4963999A (en) 1998-08-25 2000-03-14 Uab Research Foundation, The Inhibitors of bacterial nad synthetase
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
JP2000281654A (ja) 1999-03-26 2000-10-10 Tanabe Seiyaku Co Ltd イソキノリン誘導体
DE19932571A1 (de) * 1999-07-13 2001-01-18 Clariant Gmbh Verfahren zur Herstellung von Biarylen unter Palladophosphacyclobutan-Katalyse
JP2001151771A (ja) 1999-09-10 2001-06-05 Kyowa Hakko Kogyo Co Ltd 含窒素芳香族複素環誘導体
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
EP1138328A1 (en) 2000-03-29 2001-10-04 Eli Lilly And Company Limited Naphthalene derivatives as CNS drugs
US6667300B2 (en) * 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
PL202623B1 (pl) 2000-06-28 2009-07-31 Smithkline Beecham Plc Sposób wytwarzania drobno zmielonego preparatu substancji leczniczej, drobno zmielona substancja lecznicza wytworzona tym sposobem i zawierająca ją kompozycja farmaceutyczna
ES2261437T3 (es) * 2000-07-05 2006-11-16 Astellas Pharma Inc. Derivados de propano-1,3-diona.
EP2033952B1 (en) * 2001-03-01 2012-08-29 Shionogi&Co., Ltd. Nitrogen-containing Heteroaryl compounds having HIV Integrase Inhibitory Activity
UA76977C2 (en) * 2001-03-02 2006-10-16 Icos Corp Aryl- and heteroaryl substituted chk1 inhibitors and their use as radiosensitizers and chemosensitizers
WO2002078700A1 (en) * 2001-03-30 2002-10-10 Smithkline Beecham Corporation Pyralopyridines, process for their preparation and use as therapteutic compounds
WO2002088124A2 (en) * 2001-04-27 2002-11-07 Smithkline Beecham Corporation Pyrazolo'1,5-a!pyridine derivatives
CZ294535B6 (cs) * 2001-08-02 2005-01-12 Ústav Experimentální Botaniky Avčr Heterocyklické sloučeniny na bázi N6-substituovaného adeninu, způsoby jejich přípravy, jejich použití pro přípravu léčiv, kosmetických přípravků a růstových regulátorů, farmaceutické přípravky, kosmetické přípravky a růstové regulátory tyto sloučeniny obsahující
US8124625B2 (en) * 2001-09-14 2012-02-28 Shionogi & Co., Ltd. Method of enhancing the expression of apolipoprotein AI using olefin derivatives
MXPA04002243A (es) 2001-09-19 2004-06-29 Aventis Pharma Sa Compuestos quimicos.
BR0212829A (pt) * 2001-09-26 2004-08-03 Bayer Pharmaceuticals Corp Derivados de 1,8-naftiridina e seu uso para tratar diabetes e distúrbios relacionados
ATE335490T1 (de) 2001-10-30 2006-09-15 Novartis Pharma Gmbh Staurosporin-derivate als hemmer der flt3- rezeptor-tyrosinkinase-wirkung
US7262164B2 (en) * 2001-11-09 2007-08-28 Enzon, Inc. Polymeric thiol-linked prodrugs employing benzyl elimination systems
TW200301135A (en) * 2001-12-27 2003-07-01 Otsuka Maryland Res Inst Inc Pharmaceutical compositions comprising a multifunctional phosphodiesterase inhibitor and an adenosine uptake inhibitor
ES2291628T3 (es) * 2002-04-03 2008-03-01 Bristol-Myers Squibb Company Compuestos triciclicos a base de tiofeno y composiciones farmaceuticas que comprenden dichos compuestos.
KR20050006221A (ko) * 2002-05-06 2005-01-15 제네랩스 테크놀로지스, 인코포레이티드 Ｃ형 간염 바이러스 감염 치료용의 뉴클레오시드 유도체
TW200406374A (en) 2002-05-29 2004-05-01 Novartis Ag Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
MXPA05003193A (es) * 2002-09-27 2005-06-08 Sumitomo Pharma Compuesto de adenina novedoso y uso del mismo.
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
EA013811B1 (ru) 2002-11-21 2010-08-30 Новартис Вэксинес Энд Дайэгностикс, Инк. 2,4,6-тризамещённые пиримидины, являющиеся ингибиторами фосфотидилинозитол(pi)-3-киназы, и их применение при лечении рака
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
JP4500689B2 (ja) * 2002-12-26 2010-07-14 エーザイ・アール・アンド・ディー・マネジメント株式会社 選択的エストロゲン受容体モジュレーター
CZ294538B6 (cs) * 2002-12-30 2005-01-12 Ústav Experimentální Botaniky Akademie Vědčeské Re Substituční deriváty N6-benzyladenosinu, způsob jejich přípravy, jejich použití pro přípravu léčiv, kosmetických přípravků a růstových regulátorů, farmaceutické přípravky, kosmetické přípravky a růstové regulátory tyto sloučeniny obsahující
RU2233842C1 (ru) 2003-01-13 2004-08-10 Петров Владимир Иванович Производные пурина, обладающие противовирусной активностью
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
US7129264B2 (en) * 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
CA2524376A1 (en) * 2003-05-05 2004-12-16 Neurogen Corporation Substituted imidazolopyrazine and triazolopyrazyne derivatives: gabaa receptor ligands
JP4570015B2 (ja) 2003-07-14 2010-10-27 クミアイ化学工業株式会社 ２−イソオキサゾリン誘導体及びそれを有効成分として含有する除草剤
WO2005028434A2 (en) * 2003-09-18 2005-03-31 Conforma Therapeutics Corporation Novel heterocyclic compounds as hsp90-inhibitors
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
JP2007520559A (ja) * 2004-02-03 2007-07-26 アボット・ラボラトリーズ 治療薬としてのアミノベンゾオキサゾール類
JPWO2005077948A1 (ja) * 2004-02-16 2008-01-10 第一製薬株式会社 抗真菌作用複素環化合物
CN1560035A (zh) * 2004-03-12 2005-01-05 沈阳药科大学 5－羟基吲哚－3－羧酸脂类衍生物
US20070225303A1 (en) * 2004-03-26 2007-09-27 Haruhisa Ogita 8-Oxoadenine Compound
EP1740587A4 (en) * 2004-04-02 2009-07-15 Adenosine Therapeutics Llc SELECTIVE ANTAGONISTS OF A2A ADENOSINE RECEPTORS
US20060074102A1 (en) * 2004-05-14 2006-04-06 Kevin Cusack Kinase inhibitors as therapeutic agents
GB0420719D0 (en) * 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
MX2007004699A (es) * 2004-10-19 2007-06-14 Novartis Vaccines & Diagnostic Derivados de indol y bencimidazol.
EP1807417A2 (en) * 2004-11-04 2007-07-18 Neurogen Corporation Pyrazolylmethyl heteroaryl derivatives
WO2006056399A2 (en) 2004-11-24 2006-06-01 Novartis Ag Combinations of jak inhibitors and at least one of bcr-abl, flt-3, fak or raf kinase inhibitors
AU2006214190A1 (en) * 2005-02-17 2006-08-24 Icos Corporation Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation
EP1924265A4 (en) * 2005-08-16 2010-06-02 Genzyme Corp COMPOUNDS BINDING TO CHEMOKINE RECEPTORS
US7642270B2 (en) * 2005-09-14 2010-01-05 Janssen Pharmaceutica N.V. 5-oxo-5,8-dihydro-pyrido-pyrimidine as inhibitors of c-fms kinase
JPWO2007034817A1 (ja) * 2005-09-22 2009-03-26 大日本住友製薬株式会社 新規アデニン化合物
GB0520657D0 (en) 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds
EP1783114A1 (en) 2005-11-03 2007-05-09 Novartis AG N-(hetero)aryl indole derivatives as pesticides
US7557213B2 (en) * 2005-11-10 2009-07-07 Chemocentryx, Inc. Substituted quinolones and methods of use
PE20071025A1 (es) * 2006-01-31 2007-10-17 Mitsubishi Tanabe Pharma Corp Compuesto amina trisustituido
US20080009508A1 (en) * 2006-07-10 2008-01-10 Lucie Szucova 6,9-Disubstituted Purine Derivatives And Their Use For Treating Skin
US20100035756A1 (en) * 2006-07-12 2010-02-11 Syngenta Limited Triazolophyridine derivatives as herbicides
WO2008032033A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidazolyl-2-morpholino-6-piperazinylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
EP1972631A1 (en) 2007-03-23 2008-09-24 Novartis AG Imidazopyridazines as PI3K lipid kinase inhibitors
WO2008055013A2 (en) * 2006-10-31 2008-05-08 Janssen Pharmaceutica N.V. 5-oxo-5,8 - dihydro - pyrido - pyrimidines as inhibitors of c-fms kinase
CN101589046B (zh) * 2006-12-29 2011-09-21 弗·哈夫曼-拉罗切有限公司 氮杂螺环衍生物
US20080194616A1 (en) * 2007-02-05 2008-08-14 Xenon Pharmaceuticals Inc. Pyridopyrimidinone compounds useful in treating sodium channel-mediated diseases or conditions
PE20081887A1 (es) * 2007-03-20 2009-01-16 Dainippon Sumitomo Pharma Co Nuevo compuesto de adenina
UA98955C2 (ru) * 2007-03-23 2012-07-10 Амген Инк. Гетероциклические соединения и их применение
US8039505B2 (en) * 2007-04-11 2011-10-18 University Of Utah Research Foundation Compounds for modulating T-cells
US9603848B2 (en) * 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
US8633186B2 (en) * 2007-06-08 2014-01-21 Senomyx Inc. Modulation of chemosensory receptors and ligands associated therewith
JP2010531304A (ja) * 2007-06-18 2010-09-24 ユニバーシティ オブ ルイビル リサーチ ファウンデーション、インコーポレイテッド 抗悪性腫瘍活性を有するｐｆｋｆｂ３阻害物質ファミリー
CA2691444C (en) * 2007-06-29 2016-06-14 Gilead Sciences, Inc. Purine derivatives and their use as modulators of toll-like receptor 7
WO2009042294A2 (en) * 2007-08-10 2009-04-02 Burnham Institute For Medical Research Tissue-nonspecific alkaline phosphatase (tnap) activators and uses thereof
JP2009076865A (ja) 2007-08-29 2009-04-09 Fujifilm Corp 有機電界発光素子
JP2009080233A (ja) 2007-09-26 2009-04-16 Kyocera Mita Corp 電子写真感光体
CZ300774B6 (cs) * 2007-10-05 2009-08-05 Univerzita Palackého Substituované 6-(alkylbenzylamino)purinové deriváty pro použití jako antagonisté cytokininových receptoru a prípravky obsahující tyto slouceniny
JP2009120686A (ja) 2007-11-14 2009-06-04 Toyo Ink Mfg Co Ltd 光重合開始剤、重合性組成物、および重合物の製造方法。
CA2709784A1 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2009081105A2 (en) * 2007-12-21 2009-07-02 Ucb Pharma S.A. Quinoxaline and quinoline derivatives as kinase inhibitors
US7960397B2 (en) * 2007-12-28 2011-06-14 Institute Of Experimental Botany, Academy Of Sciences Of The Czech Republic 6,9-disubstituted purine derivatives and their use as cosmetics and cosmetic compositions
AU2009211004C1 (en) * 2008-01-11 2013-08-01 Natco Pharma Limited Novel pyrazolo [3, 4 -d] pyrimidine derivatives as anti -cancer agents
US9089572B2 (en) * 2008-01-17 2015-07-28 California Institute Of Technology Inhibitors of p97
US8026271B2 (en) * 2008-07-11 2011-09-27 National Health Research Institutes Formulations of indol-3-yl-2-oxoacetamide compounds
EP2387575B1 (en) * 2009-01-15 2013-09-04 Anvyl, LLC Alpha7 nicotinic acetylcholine receptor allosteric modulators, their derivatives and uses thereof
JP5789252B2 (ja) * 2009-05-07 2015-10-07 インテリカイン， エルエルシー 複素環式化合物およびその使用
PL2448938T3 (pl) * 2009-06-29 2014-11-28 Incyte Holdings Corp Pirymidynony jako inhibitory PI3K
ES2644286T3 (es) * 2009-10-22 2017-11-28 Gilead Sciences, Inc. Derivados de purina o deazapurina útiles para el tratamiento de (entre otros) infecciones víricas
US8759359B2 (en) * 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
JP2011136925A (ja) 2009-12-28 2011-07-14 Dainippon Sumitomo Pharma Co Ltd 含窒素二環性化合物
US8633183B2 (en) 2010-01-26 2014-01-21 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
WO2011130342A1 (en) 2010-04-14 2011-10-20 Incyte Corporation FUSED DERIVATIVES AS ΡI3Κδ INHIBITORS
US9062055B2 (en) * 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
JP5961187B2 (ja) * 2010-12-20 2016-08-02 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｐｉ３ｋ阻害剤としてのｎ−（１−（置換フェニル）エチル）−９ｈ−プリン−６−アミン
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
CN103930422A (zh) * 2011-07-19 2014-07-16 无限药品股份有限公司 杂环化合物及其用途
HUE030869T2 (en) * 2011-09-02 2017-06-28 Incyte Holdings Corp Heterocyclic amines as inhibitors of PI3K
AR090548A1 (es) * 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k

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