AR053090A1 - Imidazotriazinas como inhibidores de proteina quinasas y su uso para la preparacion de medicamentos - Google Patents

Imidazotriazinas como inhibidores de proteina quinasas y su uso para la preparacion de medicamentos

Info

Publication number
AR053090A1
AR053090A1 ARP050102978A ARP050102978A AR053090A1 AR 053090 A1 AR053090 A1 AR 053090A1 AR P050102978 A ARP050102978 A AR P050102978A AR P050102978 A ARP050102978 A AR P050102978A AR 053090 A1 AR053090 A1 AR 053090A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkynyl
alkenyl
cycloalkenyl
cycloalkyl
Prior art date
Application number
ARP050102978A
Other languages
English (en)
Original Assignee
Osi Pharm Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Osi Pharm Inc filed Critical Osi Pharm Inc
Publication of AR053090A1 publication Critical patent/AR053090A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • 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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • A61P7/06—Antianaemics
    • 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
    • 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

Abstract

Compuesto de formula 1 y sales aceptables para uso farmacéutico de los mismos. Estos compuestos inhiben la enzima IGF-1R y son utiles para el tratamiento y/o prevencion de varias enfermedades y afecciones, que responden al tratamiento por inhibicion de tirosina quinasas, tales como el cancer Rivindicacion 1: Un compuesto representado por la formula 1 o una sal aceptable para uso farmacéutico del mismo, donde Q1 es arilo 1, heteroarilo1, ciclaolaquilo C3-10, heterocicililo, cicloalquenilo C3-10 o heterocicloalquenilo, cualquiera de los cuales se sustituye opcionalmente por uno a cinco sustituyentes independientes G10, R1 es alquilo C0-10, cicloalquilo C3-10, biciclo-alquilo C5-10, arilo, heteroarilo, aralquilo, heteroaralquilo, heterociclo o heterobiciclo-alquilo C5-10, cualquiera de los cuales se sustituye opcionalmente con uno o más sustituyentes independientes G11; G10 y G11 son cada uno independientemente halo, oxo, -CF3, -OCF3, -OR2, -NR2R3(R2a)j1, -C(O)R2, -CO2R2, -CONR2R3, -NO2, -S(O)j1R2, -SO2NR2R3, -NR2C(=O)R3, -NR2C(=O)NR3R2a, -NR2S(O)j1R3, -C(=S)OR2, -C(=O)SR2, -NR2C(=NR3)NR2aR3a, -NR2C(=NR3)OR2a, , NR2C(=NR3)SR2a, -OC(=O)OR2, -OC(=O)NR2R3, -OC(=O)OR2, -CO(=O)NR2R3, alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10-alquilo C1-10, alcoxi C1-10-alquenilo C2-10, alcoxi C1-10-alquinilo C2-10, alquitio C1-10-alquilo C1-10, alquiltio C1-10-alquenilo C2-10, alquiltio C1-10-alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquil C3-8-alquilo C1-10, cicloalquenil C3-8-alquilo C1-10, cicloalquil C3-8-alquenilo C2-10. cicloalquenil C3-8-alquenilo C2-10, cicloalquil C3-8-alquinilo C2-10, cicloalquenil C3-8-alquinilo C2-10, heterociclil-alquilo C0-10, heterociclil-alquenilo C2-10 o heterociclil-alquinilo C2-10, cualquiera de los cuales se sustituy opcionalmente con uno o mássustituyentes independientes halo, oxo, -CF3, -OCF3, -OR222, -NR222R333(R222a)j1a, -C(O)R222, -CO2R222, - CONR222R333, -NO2, -CN, S-(O)j1aR222, -SO2NR222R333, -NR222C(=O)R333, -NR222C(=O)OR333, -R222C(=O)NR333R222a, -NR222S(O)j1aR333, -C(=S)OR222, -C(=O)SR222, -NR222C(=NR333)NR222R333a, -NR222C(=NR333)OR222a, -NR222C(=NR333)SR222a, -OC(=O)OR222, - OC(=)NR222R333, -OC(=O)OR222, -OC(=O)NR222R333, -OC(=O)SR222, -SC(=O)OR222 o -SC(=O)NR222R333; o G10 es opcionalmente -(X1)n-(Y1)m-R4; O G41 es opcionalmente -(X1)n-(Y1)m-alquilo C0-10; o G10 y G41 son cada uno opcionalmente de manera independiente arilalquilo C0-10, arilalquenilo C2-10, arilalquinilo C2-10, hetarilalquilo C0-10, hetarilalquenilo C2-10 o hetarilalquinilo C2-10, cualquiera de los cuales se sustituye opcionalmente con uno o más sustituyentes independientes halo,-CF3, -OCF3, - OR222, -NR222R333(R222a)j1a, -C(O)R222, -CO2R222, -CONR222R333, -NO2, -CN, S-(O)j1aR222, -SO2NR222R333, -NR222C(=O)R333, -NR222C(=O)OR333, -R222C(=O)NR333R222a, -NR222S(O)j1aR333, -C(=S)OR222, -C(=O)SR222, -NR222C(=NR333)NR222R333a, - NR222C(=NR333)OR222a, -NR222C(=NR333)SR222a, -OC(=O)OR222, -OC(=)NR222R333, -OC(=O)OR222, -OC(=O)NR222R333, -OC(=O)SR222, -SC(=O)OR222 o -SC(=O)NR222R333; G11 es halo, oxo, -CF3, -OCF3, -OR21, -NR21R31(R21a)j3, -C(O)R21, -CO2R21, .CONR21R31, -NO2, - CN, -S(O)j3R21, -SO2NR21R31, -NR21C(=O)R31, -NR21C(=O)OR31, -NR21C(=O)NR31R21a, -NR21S(O)j3R31, -C(=S)OR21, -C(=S)OR21, -C(=O)SR21, -NR21C(=NR31)NR21aR31a, -NR21C(=NR31)OR21a, -NR21C(=NR31)SR21a, OC(=O)OR21, -OC(=O)NR21R31, -OC(=O)SR21, - SC(=O)OR21, -SC(=O)NR21R31, -P(O)OR21OR31, alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10-alquilo C1-10, alcoxi C1-10-alquenilo C2-10, alcoxi C1-10, alquiltio C1-10-alquilo C1-10, alquiltio C1-10-alquenilo C2-10, alquiltio C1-10- alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquil C3-8-alquilo C1-10, cicloalquenil C3-8-alquilo C1-10, cicloalquil C3-8-alquenilo C3-8-alquenilo C2-10, cicloalquenil C3-8-alquenilo C2-10, cicloalquil C3-8-alquinilo C2-10, cicloalquenil C3-8-alquinilo C2-10, heterociclil-alquilo C0-10, heterociclil-alquenilo C2-10 o heterociclil-alquinilo C2-10, cualquiera de los cuales se sustituye opcionalmente con uno o más sustituyentes independientes halo, oxo, -CF3, -OCF3, - OR2221, -NR2221R3331(R2221a)j3a, -C(O)R2221, -CO2R2221, -CONR2221R3331, NO2, -CN, -S(O)j3aR2221, SO2NR2221R3331, -NR2221C(=O)R3331, -NR2221C(=O)OR3331, -NR2221C(=O)NR3331R2221a, -NR2221S(O)j3aR3331, -C(=S)OR2221, -C(=O)SR2221, - NR2221C(=NR3331)NR2221aR3331a, -NR2221C(=NR3331)OR2221a, -NR2221C(=NR3331)SR2221a, -OC(=O)OR2221, -OC(=O)NR2221R3331, -OC(=O)SR2221, -SC(=O)OR2221, -P(O)OR2221OR3331 o -SC(=O)NR2221R3331; o G11 es arilalquilo C0-10, arilalquenilo C2-10, o G11 es arilalquilo C0-10, arilalquenilo C2-10, arilalquinilo C2-10, hetarilalquilo C0-10, hetarilalquenilo C2-10 o hetarilalquinilo C2-10, cualquiera de los cuales se sustituye opcionalmente con uno o más hetarilalquinilo C2-10, cualquiera de los cuales se sustituye opcionalmente con uno o más sustituyentes independientes halo, -CF3, -OCF3, -OR2221, -NR2221R3331(R2221a)j3a, -C(O)R2221, -CO2R2221, -CONR2221R3331, -NO2, -CN, -S(O)j3aR2221, -SO2NR2221R3331, -NR2221C(=O)R3331, -NR2221C(=O)OR3331, - NR2221C(=O)NR3331R2221a, -NR2221S(O)j3aR3331, -C(=S)OR2221, -C(=O)SR2221, -NR2221C(=NR3331)NR2221aR3331a, -NR2221C(=NR3331)OR2221a, -NR2221C(=NR3331)SR2221a, -OC(=O)OR2221, -OC(=O)NR2221R3331, -OC(=O)SR2221, -SC(=O)OR2221, -P(O)OR2221OR3331 o - SC(=O)NR2221R3331; o G11 es C, tomado junto con el carbono al cual se encuentra unido forma un doble enlace C=C que se sustituye con R5 y G12, R2, R2a, R3, R3a, R222, Rrrr1, R333, R333a, R21, R21a, R31, R31a, R2221, R2221a, R3331 y R3331a son cada uno independientemente alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10-alquilo C1-10, alquilo C1-10-alquenilo C2-10, alcoxi C1-10-alquinilo C2-10, alquiltio C1-10-alquilo C1-10, alquiltio C1-10-alquenilo C2-10, alquiltio C1-10- alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquil C3-8-alquilo C1-10, cicloalquenil C3-8-alquilo C1-10, cicloalquil C3-8-alquenilo C2-10, cicloalquenil C3-8-alquenilo C2-10, cicloalquil C3-8-alquinilo C2-10, cicloalquenil C3-8- alquinilo C2-10, heterociclil-alquilo C0-10, heterociclil-alquenilo C2-10, heterociclil-alquinilo C2-10, arilalquilo C0-10, arilalquenilo C2-10, arilalquinilo C2-10, hetarilalquenilo C2-10 o hetarialquinilo C2-10, cualquiera de los cuales se sustituye opcionalmente con uno o más sustituyentes independientes G13 o en el caso de -NR2R3(R2a)j1 o -NR21R31(R21a)j3 o -NR222R333(R222a)j1a o -NR222R333(R222a)j2a o -NR2221R3331(R2221a)j3a, R2 y R3 o R21 y R31 o R222 y R333 o R2221 y R3331, respectivamente, se toman opcionalmente junto con el átomo de nitrogeno al cual se encuentran unidos para formar un anillo saturado o no saturado de 3-10 miembros, donde dicho anillo se sustituye opcionalmente con uno o más sustituyentes independientes G14 y donde dicho anillo incluye opcionalmente uno o más heteroátomos independientes distintos de nitrogeno a los cuales R2 y R3 o R222 y R333 o R2221 y R3331 se encuentran unidos; X1 e Y1 son cada uno independientemente -O-, -NR7-, - S(O)j4-, -CR5R6-, -N(C(O)OR7), -N(C(O)R7)-, -N(SO2R7)-, -CH2O-, -CH2S-, -CH2H(R7)-, -CH(NR7)-, -CH2N(C(O)R7)-, -CH2N(C(O)OR7)-, -CH2N(SO2R7)-, -CH(NHR7)-, -CH(NHC(O)R7)-, -CH(NHSO2R7)-, -CH(NHC(O)OR7)-, -CH(OC(O)R7-, -CH(OC(O)NHR7)-, -CH=CH-, -C:::C- , -C(=NOR7)-, -C(O)-, -CH(OR7)-, -C(O)N(R7)-, -N(R7)C(O)-, -N(R7)S(O)-, -N(R7)S(O)2-OC(O)N(R7)-, -N(R7)C(O)N(R8)-, -NR7C(O)-O-, -S(O)N(R7)-, -S(O)2N(R7)-, -N(C(O)R7S(O)-, -N(C(O)R7)S(O)2-, -N(R7)S(O)N(R8)-, -N(R7)S(O)2N(R8)-, -C(O)N(R7)C(O)-, - S(O)N(R7)C(O)-, -S(O)2N(R7)C(O)-, -OS(O)N(R7)-, -OS(O)2N(R7)-, -N(R7)S(O)-O-, -N(R7)S(O)2-O-, -N(R7)S(O)C(O)-, -N(R7)S(O)2C(O)-, -SON(C(O)R7)-, -SO2N(C(O)R7)-, -N(R7)SON(R8)-, -(R7)SO2N(R8)-, -N(R7)SO2N(R8)-, -C(O)-O-, N(R7)P(OR8)-O-, -N(R7)P(OR8)- , -N(R7)P(O)(OR8)-O-, -N(R7)P(O)(OR8)-, N(C(O)R7)P(OR8)-O-, -N(C(O)R7)P(OR8)-, -N(C(O)R7)P(O)(OR8)-O-, -N(C(O)R7)P(OR8)-, -CH(R7)S(O)-, -CH(R7)S(O)2, --CH(R7)N(C(O)OR8)-, -CH(R7)N(C(O)R8)-, -CH(R7)N(SO2R8)-, -CH(R7)-O-. --CH(R7)S-, CH(R7)N(R8)-, - CH(R7)N(C(O)R8)-, -CH(R7)N(C(O)OR8)-, -CH(R7)N(SO2R8)-, -CH(R7)C(=NOR8)-, -CH(R7)C(O)-, -CH(R7)CH(OR8)-, -CH(R7)C(O)N(R8)-, -CH(R7)N(R8)C(O)-, -CH(R7)N(R8)S(O)-, -CH(R7)N(R8)S(O)2-, -CH(R7)OC(O)N(R8)-, -CH(R7)N(R8)C(O)N(R7a)-, -CH(R7)NR8C(O)-O-, - CH(R7)S(O)N(R8)-, -CH(R7)S(O)2N(R8)-, -CH(R7)N(C(O)R8)S(O)-, -CH(R7)N(C(O)R8)S(O)-, -CH(R7)N(R8)S(O)N(R7a)-, -CH(R7)N(R8)S(O)2N(R7a)-, -CH(R7)C(O)N(R8)C(O)-, -CH(R7)S(O)N(R8)C(O)-, -CH(R7)S(O)2N(R8)C(O)-, -CH(R7)OS(O)N(R8)-, -CH(R7)OS(O)2N(R8)-, - CH(R7)N(R8)S(O)-O-, -CH(R7)N(R8)S(O)2-O-, -CH)R7)N(R8)S(O)C(O)-, -CH(R7)N(R8)S(O)2C(O)-, -CH(R7)SON(C(O)R8)-, -CH(R7)SO2N(C(O)R8)-, -CH(R7)N(R8)SON(R7a)-, -CH(R7)N(R8)SO2N(R7Aa)-, -CH(R7)C(O)-O-, -CH(R7)N(R8)P(OR7a)-O-, -CH(R7)N(R8)P(OR7a)-, - CH(R7)N(R8)P(O)(OR7a)-O-, -CH(R7)N(R8)P(O)(OR7a)-, -CH(R7)N(C(O)R8)P(OR7a)-O-, -CH(R7)N(O)R8)P(OR7a)-, -CH(R7)N(C(O)R8)P(O)OR7a)-O- o -CH(R7)N(C(O)R8)P(OR7a)-; o X1 e Y1 se representan cada uno independientemente por una de las siguientes formulas estructurales: 1, 2, 3, 4, 5 0 6, R10 tomado junto con la fosfinamida o fosfonamida, forman un sistema anular arilo, heteroarilo o heterociclilo de 5, 6 o 7 miembros; R5, R6, G12, G13, G14 y G15 son cada uno independientemente alquilo C0- 10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-10-alquilo C1-10, alcoxi C1-10-alquenilo C2-10, alcoxi C1-10-alquinilo C2-10, alquiltio C1-10-alquilo C1-10, alquiltio C1-10-alquenilo C2-10, alquiltio C1-10-alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquil C3-8-alquilo C1-10, cicloalquenil C3-8-alquilo C1-10, cicloalquil C3-8-alquenilo C2-10, cicloalquenil C3-8-alquenilo C2-10, cicloalquil C3-8-alquinilo C2-10, cicloalquenil C3-8-alquinilo C2-10, hererociclil-alquilo C0-10, heterociclil-alquenilo C2-10, heterociclil-alquinilo C2-10, aralquilo C0-10, arilalquenilo C2-10, arilalquinilo C2-10, hetarilalquilo C0-10, hetarilalquenilo C2-10 o hetarilalquenilo C2-10 o hetarilalquinilo C2-10, cualquiera de
ARP050102978A 2004-07-20 2005-07-19 Imidazotriazinas como inhibidores de proteina quinasas y su uso para la preparacion de medicamentos AR053090A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US58951404P 2004-07-20 2004-07-20

Publications (1)

Publication Number Publication Date
AR053090A1 true AR053090A1 (es) 2007-04-25

Family

ID=35482337

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050102978A AR053090A1 (es) 2004-07-20 2005-07-19 Imidazotriazinas como inhibidores de proteina quinasas y su uso para la preparacion de medicamentos

Country Status (18)

Country Link
US (1) US7741324B2 (es)
EP (1) EP1781660A1 (es)
JP (1) JP4918038B2 (es)
KR (1) KR20070035087A (es)
CN (1) CN101084218A (es)
AP (1) AP2007003924A0 (es)
AR (1) AR053090A1 (es)
AU (1) AU2005267120B2 (es)
BR (1) BRPI0513565A (es)
CA (1) CA2574594A1 (es)
EA (1) EA200700220A1 (es)
IL (1) IL180806A0 (es)
MX (1) MX2007000822A (es)
MY (1) MY139689A (es)
NO (1) NO20070917L (es)
RU (1) RU2007106068A (es)
TW (1) TW200613306A (es)
WO (1) WO2006012422A1 (es)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7026500B2 (en) * 2000-08-24 2006-04-11 University Of Tennessee Research Foundation Halogenated selective androgen receptor modulators and methods of use thereof
CA2561950C (en) 2004-04-02 2010-04-20 Osi Pharmaceuticals, Inc. 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors
ES2436877T3 (es) * 2005-11-17 2014-01-07 OSI Pharmaceuticals, LLC Intermedios para la preparación de inhibidores de mTOR bicíclicos condensados
US8575164B2 (en) * 2005-12-19 2013-11-05 OSI Pharmaceuticals, LLC Combination cancer therapy
WO2007087395A2 (en) * 2006-01-25 2007-08-02 Osi Pharmaceuticals, Inc. UNSATURATED mTOR INHIBITORS
GEP20125658B (en) * 2006-11-22 2012-10-10 Incyte Corp Imidazotriazines and imidazo pyrimidines as kinase inhibitors
US8809273B2 (en) 2007-03-28 2014-08-19 Pharmacyclics, Inc. Inhibitors of Bruton's tyrosine kinase
EP2561875A3 (en) * 2007-03-28 2013-06-12 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
EP2145205B1 (en) * 2007-05-01 2019-09-18 QUALCOMM Incorporated Position location for wireless communication systems
US8130700B2 (en) 2007-06-15 2012-03-06 Silver Spring Networks, Inc. Method and system for providing network and routing protocols for utility services
WO2009091939A1 (en) * 2008-01-18 2009-07-23 Osi Pharmaceuticals, Inc. Imidazopyrazinol derivatives for the treatment of cancers
EA018144B1 (ru) * 2008-03-19 2013-05-30 Оси Фармасьютикалз, Инк. СОЛЕВЫЕ ФОРМЫ ИНГИБИТОРА mTOR
ES2396613T3 (es) * 2008-05-19 2013-02-22 OSI Pharmaceuticals, LLC Imidazopirazinas e imidazotriazinas sustituidas
HUE034716T2 (hu) * 2008-05-21 2018-02-28 Incyte Holdings Corp 2-Fluor-N-metil-4-[7-(kinolin-6-il-metil)-imidazo[1,2-b][1,2,4]triazin-2-il]benzamid sói és eljárások ezek elõállítására
WO2010002877A2 (en) 2008-07-03 2010-01-07 Biota Scientific Management Bycyclic nucleosides and nucleotides as therapeutic agents
DE102009005193A1 (de) * 2009-01-20 2010-07-22 Merck Patent Gmbh Neue heterocyclische Verbindungen als MetAP-2 Inhibitoren
CN102405214A (zh) 2009-04-20 2012-04-04 Osi药物有限责任公司 C-吡嗪-甲胺的制备
JP2012526138A (ja) * 2009-05-07 2012-10-25 オーエスアイ・ファーマシューティカルズ，エルエルシー 副腎皮質癌を治療するためのｏｓｉ−９０６の使用
JP5714030B2 (ja) * 2010-02-03 2015-05-07 インサイト コーポレーションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｃ−Ｍｅｔ阻害剤としてのイミダゾ［１，２−ｂ］［１，２，４］トリアジン
US20130005733A1 (en) 2010-03-09 2013-01-03 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
MX342405B (es) 2010-06-03 2016-09-28 Pharmacyclics Inc El uso de inhibidores de la tirosina quinasa de bruton (btk).
AU2012212075A1 (en) 2011-02-02 2013-07-18 Amgen Inc. Methods and compositons relating to inhibition of IGF-1R
EA022586B1 (ru) 2011-02-23 2016-01-29 Пфайзер Инк. ИМИДАЗО[5,1-f][1,2,4]ТРИАЗИНЫ ДЛЯ ЛЕЧЕНИЯ НЕВРОЛОГИЧЕСКИХ РАССТРОЙСТВ
BR112014000653A2 (pt) 2011-07-13 2017-02-14 Pharmacyclics Inc inibidores de tirosina quinase de bruton
EP2776042B1 (en) 2011-11-11 2019-03-20 Duke University Combination drug therapy for the treatment of solid tumors
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
CN107082783B (zh) 2012-01-26 2019-03-22 H.隆德贝克有限公司 具有咪唑并三嗪酮骨架的pde9抑制剂
CN103374001B (zh) * 2012-04-19 2015-10-28 山东轩竹医药科技有限公司 咪唑并三嗪类mTOR抑制剂
KR20150015021A (ko) 2012-06-04 2015-02-09 파마시클릭스, 인코포레이티드 브루톤 타이로신 키나아제 저해제의 결정 형태
US8980259B2 (en) 2012-07-20 2015-03-17 Novartis Ag Combination therapy
AU2013293087B2 (en) 2012-07-24 2017-08-31 Pharmacyclics Llc Mutations associated with resistance to inhibitors of Bruton's tyrosine kinase (BTK)
PE20151495A1 (es) 2012-11-15 2015-10-23 Pharmacyclics Inc Compuestos de pirrolopirimidina como inhibidores de quinasas
MA38961A1 (fr) 2013-09-30 2018-05-31 Pharmacyclics Llc Composés 3-phenyl-1h-pyrazolo[3,4-d]pyrimidin-4-ylamine substitués inhibiteurs de la tyrosine kinase de bruton utilisés pour traiter par exemple les maladies auto-immunes, respiratoires et inflammatoires, cancer, mastocytose et osteoporose
WO2015058084A1 (en) * 2013-10-18 2015-04-23 Medivation Technologies, Inc. Heterocyclic compounds and methods of use
WO2015081783A1 (zh) * 2013-12-06 2015-06-11 江苏奥赛康药业股份有限公司 吡咯并[2,1-f][1,2,4]三嗪类衍生物及其制备方法和用途
WO2015143400A1 (en) 2014-03-20 2015-09-24 Pharmacyclics, Inc. Phospholipase c gamma 2 and resistance associated mutations
CA2959602A1 (en) 2014-08-01 2016-02-04 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
WO2016022942A1 (en) 2014-08-07 2016-02-11 Pharmacyclics Llc Novel formulations of a bruton's tyrosine kinase inhibitor
RU2017133990A (ru) 2015-03-03 2019-04-05 Фармасайкликс Элэлси Фармацевтические лекарственные формы ингибитора тирозинкиназы брутона
DK3303339T3 (da) 2015-07-07 2021-04-12 H Lundbeck As Pde9-inhibitorer med imidazotriazinonskelet og imidazopyrazinonskelet til behandling af perifere sygdomme
US10053465B2 (en) 2015-08-26 2018-08-21 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
WO2017129763A1 (en) 2016-01-28 2017-08-03 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of signet ring cell gastric cancer
UA123785C2 (uk) 2016-03-28 2021-06-02 Інсайт Корпорейшн Сполуки піролотриазину як інгібітори tam
JP2020511462A (ja) 2016-12-03 2020-04-16 ジュノー セラピューティクス インコーポレイテッド キナーゼ阻害剤との組み合わせで治療用ｔ細胞を使用するための方法および組成物
JP2020535168A (ja) 2017-09-27 2020-12-03 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩
EP3813800A1 (en) 2018-06-29 2021-05-05 Incyte Corporation Formulations of an axl/mer inhibitor
WO2023196975A1 (en) * 2022-04-08 2023-10-12 Shy Therapeutics, Llc Compounds that interact with ras superfamily proteins for treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5217999A (en) 1987-12-24 1993-06-08 Yissum Research Development Company Of The Hebrew University Of Jerusalem Styryl compounds which inhibit EGF receptor protein tyrosine kinase
CA2078214C (en) 1990-04-02 1995-03-28 Robert Lee Dow Benzylphosphonic acid tyrosine kinase inhibitors
US5302606A (en) 1990-04-16 1994-04-12 Rhone-Poulenc Rorer Pharmaceuticals Inc. Styryl-substituted pyridyl compounds which inhibit EGF receptor tyrosine kinase
DE69222637T2 (de) 1991-05-10 1998-02-26 Rhone Poulenc Rorer Int Bis mono- und bicyclische aryl- und heteroarylderivate mit inhibierender wirkung auf die egf und/oder pdgf-rezeptor tyrosinkinase
US6645969B1 (en) 1991-05-10 2003-11-11 Aventis Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
WO1992021660A1 (en) 1991-05-29 1992-12-10 Pfizer, Inc. Tricyclic polyhydroxylic tyrosine kinase inhibitors
MX9304801A (es) 1992-08-06 1997-06-28 Warner Lambert Co 2-toindoles (selenoidoles) disulfuros (seleniduros) relacinados, los cuales inhiben a las proteinas tirosina cinasas y los cuales tienen propiedades anti-tumorales.
CA2140440A1 (en) 1992-08-06 1994-02-17 Ellen M. Dobrusin 2-thioindoles (selenoindoles) and related disulfides (selenides) which inhibit protein tyrosine kinases and which have antitumor properties
GB9226855D0 (en) 1992-12-23 1993-02-17 Erba Carlo Spa Vinylene-azaindole derivatives and process for their preparation
JPH07133280A (ja) 1993-11-09 1995-05-23 Takeda Chem Ind Ltd セフェム化合物、その製造法および抗菌組成物
US5584409A (en) * 1995-09-18 1996-12-17 Chemberlen; Christopher H. One direction ventilation valves
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
CH690773A5 (de) 1996-02-01 2001-01-15 Novartis Ag Pyrrolo(2,3-d)pyrimide und ihre Verwendung.
JP2000506880A (ja) 1996-03-15 2000-06-06 ゼネカ・リミテッド シンノリン誘導体及びその使用
US6232299B1 (en) 1996-05-01 2001-05-15 Eli Lilly And Company Use of protein kinase C inhibitors to enhance the clinical efficacy of oncolytic agents and radiation therapy
EP0915698A4 (en) 1996-05-01 1999-08-11 Lilly Co Eli TREATMENT PROCEDURE FOR VEGF-RELATED DISEASES
UA54427C2 (uk) 1996-05-01 2003-03-17 Елі Ліллі Енд Компані Спосіб лікування очних захворювань, які пов'язані з фактором васкулярного ендотеліального росту
GB9707800D0 (en) 1996-05-06 1997-06-04 Zeneca Ltd Chemical compounds
EP1114053A1 (en) 1998-09-18 2001-07-11 Basf Aktiengesellschaft Pyrrolopyrimidines as protein kinase inhibitors
WO2000035455A1 (en) 1998-12-15 2000-06-22 Telik, Inc. Heteroaryl-aryl ureas as igf-1 receptor antagonists
BR0010482A (pt) * 1999-05-21 2002-04-23 Bristol Myers Squibb Co Inibidores pirrolotriazìnicos de cinases
US6982265B1 (en) 1999-05-21 2006-01-03 Bristol Myers Squibb Company Pyrrolotriazine inhibitors of kinases
WO2001072751A1 (en) * 2000-03-29 2001-10-04 Knoll Gesellschaft Mit Beschraenkter Haftung Pyrrolopyrimidines as tyrosine kinase inhibitors
MXPA03008560A (es) 2001-03-22 2004-06-30 Abbot Gmbh & Co Kg Pirazolopirimidinas como agentes terapeuticos.
AR035885A1 (es) 2001-05-14 2004-07-21 Novartis Ag Derivados de 4-amino-5-fenil-7-ciclobutilpirrolo (2,3-d)pirimidina, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos derivados para la preparacion de una composicion farmaceutica
SE0102168D0 (sv) 2001-06-19 2001-06-19 Karolinska Innovations Ab New use and new compounds
JP3933420B2 (ja) * 2001-07-24 2007-06-20 出光ユニテック株式会社 収納袋の排気弁
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
US7115617B2 (en) 2001-08-22 2006-10-03 Amgen Inc. Amino-substituted pyrimidinyl derivatives and methods of use
GB0122560D0 (en) 2001-09-19 2001-11-07 Aventis Pharma Ltd Chemical compounds
MXPA04002243A (es) 2001-09-19 2004-06-29 Aventis Pharma Sa Compuestos quimicos.
US6827492B2 (en) * 2001-12-05 2004-12-07 Leland B. Cook One-way concealed-valve vented storage bag
SE0104140D0 (sv) 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
US20050215564A1 (en) 2002-02-14 2005-09-29 Stiles Charles D Methods and compositions for treating hyperproliferative conditions
PT1476192E (pt) 2002-02-14 2007-07-26 Dana Farber Cancer Inst Inc Métodos e composições para tratar condições hierproliferativas
DE10230604A1 (de) * 2002-07-08 2004-01-29 Bayer Ag Heterocyclisch substituierte Imidazotriazine
DE10230605A1 (de) 2002-07-08 2004-01-29 Bayer Ag Substituierte Imidazotriazine
UA80171C2 (en) * 2002-12-19 2007-08-27 Pfizer Prod Inc Pyrrolopyrimidine derivatives
CA2518740C (en) 2003-03-12 2011-01-11 Pfizer Products Inc. Pyridyloxymethyl and benzisoxazole azabicyclic derivatives
CA2561950C (en) * 2004-04-02 2010-04-20 Osi Pharmaceuticals, Inc. 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors

Also Published As

Publication number Publication date
AU2005267120A1 (en) 2006-02-02
AU2005267120B2 (en) 2011-06-02
CA2574594A1 (en) 2006-02-02
WO2006012422A1 (en) 2006-02-02
BRPI0513565A (pt) 2008-05-06
CN101084218A (zh) 2007-12-05
MY139689A (en) 2009-10-30
JP4918038B2 (ja) 2012-04-18
TW200613306A (en) 2006-05-01
US20060019957A1 (en) 2006-01-26
KR20070035087A (ko) 2007-03-29
EP1781660A1 (en) 2007-05-09
IL180806A0 (en) 2007-06-03
RU2007106068A (ru) 2008-08-27
JP2008507546A (ja) 2008-03-13
NO20070917L (no) 2007-03-19
US7741324B2 (en) 2010-06-22
AP2007003924A0 (en) 2007-02-28
EA200700220A1 (ru) 2007-08-31
MX2007000822A (es) 2007-04-02

Similar Documents

Publication Publication Date Title
AR053090A1 (es) Imidazotriazinas como inhibidores de proteina quinasas y su uso para la preparacion de medicamentos
AR048518A1 (es) Inhibidores heterobiciclicos de proteina quinasas sustituidos con anillos 6,6 -biciclicos
CY1120342T1 (el) Ανταγωνιστης πολυκυκλικου lpa1 και χρησεις εξ' αυτου
CY1118842T1 (el) Αναισθητικες ενωσεις και σχετιζομενες μεθοδοι χρησεις
MA42232B1 (fr) Nouveaux dérivés d'acide aminé, leur procédé de préparation et compositions pharmaceutiques les contenant
NI201200172A (es) Activadores de guanilato ciclasa soluble
ECSP14013189A (es) Inhibidores de la replicación de los virus de la gripe
AR085039A1 (es) DERIVADOS DE PURINA, COMPOSICIONES FARMACEUTICAS QUE LOS COMPRENDEN Y SU USO EN LA PREPARACION DE MEDICAMENTOS PARA TRATAR ENFERMEDADES MODULADAS POR LA INHIBICION DE LA PI3K DE CLASE I Y/O mTOR
CY1117085T1 (el) C7-φθορο υποκατεστημενες ενωσεις τετρακυκλινης
EA201590453A1 (ru) Конденсированные бициклические производные сульфамоила и их применение в качестве лекарственных препаратов для лечения гепатита b
AR074826A1 (es) Regimen de dosificacion para un agonista de los receptores de s1p
RU2012153164A (ru) Производные мочевины и их терапевтическое применение при лечении, среди прочего, заболеваний дыхательного пути
MX2020004283A (es) Derivados de piridincarbonilo y usos terapéuticos de los mismos como inhibidores de trpc6.
CO7280475A2 (es) Derivados de azaindol que actuan como inhibidores de pi3k
AR087868A1 (es) Compuestos de triazolopiridina como moduladores de la tirosina quinasa c-met
BR112015028760A2 (pt) compostos para inibição de cepas de integrase do hiv-1 resistentes a drogas
PE20210478A1 (es) Compuestos heteroaromaticos como inhibidores de vanina
CO2021014210A2 (es) Compuestos de pirrol
CL2022002975A1 (es) Compuestos y composiciones para inhibir la actividad de hif2-alfa y sus métodos de uso
AR088414A1 (es) Derivados sustituidos de indol
AR096727A1 (es) Derivados terapéuticamente activos de estratrien-tiazol
RU2015115398A (ru) N-ацетил-L-цистеин для применения в экстракорпоральном оплодотворении
EA201071272A1 (ru) Новые производные аминокислот, способ их получения и применение
AR119143A1 (es) Compuesto de 1h-pirrolo[3,2-b]piridin-5-ilo, composición farmacéutica que lo comprende y su uso para fabricar un medicamento
RU2018130994A (ru) Новое соединение бисфосфоновой кислоты

Legal Events

Date Code Title Description
FA Abandonment or withdrawal