AR100808A1 - Inhibidores de fosfatidilinositol 3-quinasa - Google Patents

Inhibidores de fosfatidilinositol 3-quinasa

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Publication number
AR100808A1
AR100808A1 ARP150101858A ARP150101858A AR100808A1 AR 100808 A1 AR100808 A1 AR 100808A1 AR P150101858 A ARP150101858 A AR P150101858A AR P150101858 A ARP150101858 A AR P150101858A AR 100808 A1 AR100808 A1 AR 100808A1
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AR
Argentina
Prior art keywords
optionally substituted
carbon atoms
substituted carbon
alkyl
hydrogen
Prior art date
Application number
ARP150101858A
Other languages
English (en)
Inventor
Chung Yeung Suet
j watkins William
Van Veldhuizen Joshua
L Stevens Kirk
W Phillips Barton
Patel Leena
Naduthambi Devan
A Loyer-Drew Jennifer
Kim Musong
Du Zhimin
Cai Shaopei
Original Assignee
Gilead Sciences Inc
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Publication date
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of AR100808A1 publication Critical patent/AR100808A1/es

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    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
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    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

Abstract

Reivindicación 1: Un compuesto caracterizado porque tiene la estructura de fórmula (1) en donde: n es 0, 1, 2, 3, ó 4; m es 0 ó 1; A es un enlace sencillo o C(O); B es C₁₋₆ alquilo, C₃₋₈ cicloalquilo, C₃₋₈ heteroalquilo, o C₃₋₈ heterocicloalquilo en donde cada una de las unidades estructurales alquilo, cicloalquilo, y heterocicloalquilo está sustituida opcionalmente con hidroxilo o C₁₋₆ alcoxi; R es hidrógeno o alquilo de uno a seis átomos de carbono opcionalmente sustituido; cada R¹ es seleccionado independientemente de halo, ciano, alquilo de uno a seis átomos de carbono opcionalmente sustituido, haloalquilo de uno a seis átomos de carbono opcionalmente sustituido, alcoxi de uno a seis átomos de carbono opcionalmente sustituido, sulfonilo opcionalmente sustituido, alquilsulfonilo de uno a seis átomos de carbono opcionalmente sustituido, arilo de 3 a 8 átomos de carbono opcionalmente sustituido, heteroarilo de tres a ocho átomos de carbono opcionalmente sustituido, cicloalquilo de tres a ocho átomos de carbono opcionalmente sustituido, y heterocicloalquilo de dos a ocho átomos de carbono opcionalmente sustituido; R² es hidrógeno, ciano, heterocicloalquilo de tres a ocho átomos de carbono opcionalmente sustituido, heteroarilo de tres a ocho átomos de carbono opcionalmente sustituido, -NR²ˣR²ˣ, -NR²ʸC(O)R²ˣ, -C(O)NR²ˣR²ʸ, -OR²ʸ, o -SO₂R²ᶻ, donde R²ˣ es hidrógeno, alquilo de uno a seis átomos de carbono opcionalmente sustituido, C₁₋₆ haloalquilo, C₆₋₁₀ arilo, cicloalquilo de tres a ocho átomos de carbono opcionalmente sustituido, heterocicloalquilo de dos a ocho átomos de carbono opcionalmente sustituido, C₄₋₈ heteroarilo; en donde R²ʸ es seleccionado independientemente de hidrógeno y C₁₋₆ alquilo; y en donde R²ᶻ es C₁₋₆ alquilo; R³ es hidrógeno, alquilo de uno a seis átomos de carbono opcionalmente sustituido, C₃₋₈ cicloalquilo, o C₆₋₁₀ arilo; R⁴ es un heteroarilo de seis a doce miembros que tiene al menos un grupo aromático y al menos dos heteroátomos seleccionados de N, O, o S, en donde el heteroarilo está sustituido opcionalmente con uno, dos o tres miembros seleccionados independientemente de halo, ciano, haloalquilo opcionalmente sustituido, alquilo de uno a seis átomos de carbono opcionalmente sustituido, y -NH₂; y R⁵ es hidrógeno o alquilo de uno a seis átomos de carbono opcionalmente sustituido, en donde R⁵ y R³ junto con los átomos a los cuales están unidos opcionalmente forman un anillo heterocíclico de cuatro u ocho miembros; o una sal, un isómero, o una mezcla farmacéuticamente aceptable de los mismos.
ARP150101858A 2014-06-13 2015-06-11 Inhibidores de fosfatidilinositol 3-quinasa AR100808A1 (es)

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US201462012172P 2014-06-13 2014-06-13

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AR100808A1 true AR100808A1 (es) 2016-11-02

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Country Status (18)

Country Link
US (1) US11021467B2 (es)
EP (1) EP3154960A1 (es)
JP (1) JP6455995B2 (es)
KR (1) KR20170012560A (es)
CN (1) CN106459005A (es)
AR (1) AR100808A1 (es)
AU (1) AU2015274696B2 (es)
BR (1) BR112016028642A2 (es)
CA (1) CA2952012A1 (es)
EA (1) EA201692268A1 (es)
HK (1) HK1231476A1 (es)
IL (1) IL248897A0 (es)
MA (1) MA40059A (es)
MX (1) MX2016016530A (es)
NZ (1) NZ726360A (es)
SG (1) SG11201609877XA (es)
TW (1) TW201625560A (es)
WO (1) WO2015191726A1 (es)

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BR112016028814A2 (pt) 2014-06-13 2017-08-22 Gilead Sciences Inc ?composição farmacêutica, métodos de tratamento de uma doença ou condição, de inibição de reações imunitárias ou crescimento excessivo ou destrutivo ou de proliferação de células cancerosas, kit, composto, um sal, um isômero, ou uma mistura farmaceuticamente aceitável do mesmo, e, uso de um composto, de um sal, de um isômero, ou de uma mistura farmaceuticamente aceitável do mesmo?
BR112016028818A2 (pt) 2014-06-13 2017-08-22 Gilead Sciences Inc composição farmacêutica, métodos de tratamento de uma doença ou condição, de inibição da atividade de um polipeptídeo de fosfatidilinositol 3-quinase e de inibição de reações imunes excessivas ou destrutivas ou crescimento ou proliferação de células cancerosas, kit, composto, sal, isômero, ou uma mistura farmaceuticamente aceitável do mesmo, e, uso de um composto, um sal, isômero, ou uma mistura farmaceuticamente aceitável do mesmo.
NZ727185A (en) * 2014-06-24 2018-04-27 Gilead Sciences Inc Phosphatidylinositol 3-kinase inhibitors
UA115296C2 (uk) 2014-07-04 2017-10-10 Люпін Лімітед Хінолізинонові похідні як інгібітори pi3k
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TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Hdac抑制劑與pd-l1抑制劑之組合治療
US11331331B2 (en) 2017-12-07 2022-05-17 Emory University N4-hydroxycytidine and derivatives and anti-viral uses related thereto
JP7450541B2 (ja) 2018-01-20 2024-03-15 サンシャイン・レイク・ファーマ・カンパニー・リミテッド 置換アミノピリミジン化合物及び使用方法
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