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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
Authority
AR
Argentina
Prior art keywords
substituted
group
alkyl
independently selected
aryl
Prior art date
Application number
ARP140104690A
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English (en)
Inventor
Accetta Alessandro
Carzaniga Laura
Maria Capelli Anna
Biagetti Matteo
Original Assignee
Chiesi Farm Spa
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Filing date
Publication date
Application filed by Chiesi Farm Spa filed Critical Chiesi Farm Spa
Publication of AR098776A1 publication Critical patent/AR098776A1/es

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • 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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Application Number Priority Date Filing Date Title
EP13197986 2013-12-18

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AR098776A1 true AR098776A1 (es) 2016-06-15

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ARP140104690A AR098776A1 (es) 2013-12-18 2014-12-16 Derivados del isocromeno como inhibidores de las fosfoinositido-3 quinasas

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US (1) US9321776B2 (es)
EP (1) EP3083617B1 (es)
JP (1) JP6617973B2 (es)
KR (1) KR102371570B1 (es)
CN (1) CN105829308B (es)
AR (1) AR098776A1 (es)
AU (1) AU2014368725B2 (es)
CA (1) CA2934135C (es)
CL (1) CL2016001543A1 (es)
CY (1) CY1122098T1 (es)
DK (1) DK3083617T3 (es)
EA (1) EA035173B1 (es)
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