AR098776A1 - Derivados del isocromeno como inhibidores de las fosfoinositido-3 quinasas - Google Patents

Derivados del isocromeno como inhibidores de las fosfoinositido-3 quinasas

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Publication number
AR098776A1
AR098776A1 ARP140104690A ARP140104690A AR098776A1 AR 098776 A1 AR098776 A1 AR 098776A1 AR P140104690 A ARP140104690 A AR P140104690A AR P140104690 A ARP140104690 A AR P140104690A AR 098776 A1 AR098776 A1 AR 098776A1
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Argentina
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substituted
group
alkyl
independently selected
aryl
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ARP140104690A
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English (en)
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Accetta Alessandro
Carzaniga Laura
Maria Capelli Anna
Biagetti Matteo
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Chiesi Farm Spa
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Publication of AR098776A1 publication Critical patent/AR098776A1/es

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    • 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
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    • A61K31/52—Purines, e.g. adenine
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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Abstract

Compuestos que inhiben las fosfoinositido-3 quinasas (PI3K), composiciones farmacéuticas que los comprenden y su uso terapéutico en el tratamiento de los trastornos asociados a las enzimas PI3K, por ejemplo: asma, EPOC o fibrosis pulmonar idiopática. Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), donde: cada R, cuando está presente, se selecciona en forma independiente entre el grupo que consiste en: OR⁶; SR⁶; S(O)q-R⁸; NR¹⁰R¹¹; halógeno; C₁₋₆ alquilo; C₁₋₆ haloalquilo; C₃₋₇ cicloalquilo; C₅₋₇ cicloalquenilo; C₂₋₆ alquenilo; C₂₋₆ alquinilo; arilo sustituido o no sustituido; y heteroarilo sustituido o no sustituido; R¹ y R² son ambos H o se combinan para formar un grupo oxo (=O); R³ y R⁴, iguales o diferentes, en cada caso se seleccionan en forma independiente entre el grupo que consiste en: H; C₁₋₆ alquilo; y C₁₋₆ haloalquilo; R⁵ se selecciona entre el grupo que consiste en: H; OR⁷; SR⁷; S(O)q-R⁹; halógeno; NR¹²R¹³; CN; C(O)NR¹²R¹³; COOR¹⁴; C₁₋₆ alquilo; C₁₋₆ haloalquilo; C₁₋₆ hidroxialquilo; C₁₋₆ aminoalquilo; C₃₋₇ cicloalquilo; arilo-C₁₋₃ alquilo; C₅₋₇ cicloalquenilo; C₂₋₆ alquenilo; C₂₋₆ alquinilo; C₂₋₆ aminoalquinilo; C₃₋₆ heterocicloalquilo sustituido o no sustituido; arilo sustituido o no sustituido; y heteroarilo sustituido o no sustituido; R⁶, R⁷ y R¹⁴, iguales o diferentes, se seleccionan en cada caso en forma independiente entre el grupo que consiste en: H; C₁₋₆ alquilo; C₁₋₆ haloalquilo; C₁₋₆ hidroxialquilo; C₁₋₆ aminoalquilo; aril-C₁₋₆ alquilo; C₁₋₆ alcanoilo; arilcarbonilo; y arilo-C₂₋₄ alcanoilo; R⁸ y R⁹, iguales o diferentes, se seleccionan en cada caso en forma independiente entre el grupo que consiste en C₁₋₆ alquilo; C₁₋₆ haloalquilo; C₁₋₆ hidroxialquilo; C₁₋₆ aminoalquilo; arilo sustituido o no sustituido; heteroarilo sustituido o no sustituido; y NR¹²R¹³; R¹⁰, R¹¹, R¹² y R¹³, iguales o diferentes, se seleccionan en cada caso en forma independiente entre el grupo que consiste en H, C₁₋₆ aminoalquilo, C₁₋₆ hidroxialquilo y C₁₋₆ alquilo, o tomados juntos con el átomo de nitrógeno al que se unen, R¹⁰ y R¹¹ o R¹² y R¹³ pueden formar un radical heterocíclico de 5 ó 6 miembros; Z, cuando está presente, es un átomo o un grupo seleccionado en cada caso en forma independiente entre O, NH, C(O), NHC(O), C(O)NH, S, S(O) y S(O)₂; m es cero o 1; n es 1 ó 2; p es cero o un entero en el rango entre 1 y 3; q es 1 ó 2; Cy se selecciona entre el grupo que consiste en: grupo C₅₋₆ heterocicloalquilo sustituido o no sustituido; arilo sustituido o no sustituido; y heteroarilo sustituido o no sustituido; o sales aceptables para uso farmacéutico del mismo.
ARP140104690A 2013-12-18 2014-12-16 Derivados del isocromeno como inhibidores de las fosfoinositido-3 quinasas AR098776A1 (es)

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