AR100806A1 - Inhibidores de fosfatidilinositol 3-quinasa - Google Patents

Inhibidores de fosfatidilinositol 3-quinasa

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Publication number
AR100806A1
AR100806A1 ARP150101856A ARP150101856A AR100806A1 AR 100806 A1 AR100806 A1 AR 100806A1 AR P150101856 A ARP150101856 A AR P150101856A AR P150101856 A ARP150101856 A AR P150101856A AR 100806 A1 AR100806 A1 AR 100806A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
carbon atoms
substituted carbon
alkyl
independently selected
Prior art date
Application number
ARP150101856A
Other languages
English (en)
Inventor
Chung Yeung Suet
Anne Treiberg Jennifer
Phillips Gary
W Phillips Barton
Perreault Stephane
Patel Leena
Kaplan Joshua
Evarts Jerry
Original Assignee
Gilead Sciences 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 Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of AR100806A1 publication Critical patent/AR100806A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • A61K31/495—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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    • A61K31/00—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
    • A61K31/495—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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • A—HUMAN NECESSITIES
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    • C07D471/02—Heterocyclic 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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    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
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    • 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
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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    • C07D513/02—Heterocyclic 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
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  • Diabetes (AREA)
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  • Neurology (AREA)
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  • Cardiology (AREA)
  • Rheumatology (AREA)
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Abstract

Los compuestos son inhibidores de las actividades de la fosfatidilinositol 3-quinasa (Pl3K) y son útiles para el tratamiento de condiciones mediadas por una o más isoformas de Pl3K. La presente solicitud provee adicionalmente composiciones farmacéuticas que incluyen un compuesto de fórmula (1), o sales, isómeros, tautómeros o mezclas de los mismos farmacéuticamente aceptables, y métodos para utilizar estos compuestos y composiciones para el tratamiento de condiciones mediadas por una o más isoformas de Pl3K. Reivindicación 1: Un compuesto caracterizado porque tiene la estructura de fórmula (1), en donde: X, Y, Z son seleccionados independientemente de C(R) o N, en donde al menos uno de X, Y, y Z es C(R); n es 0, 1, 2, 3, o 4; m es 0 ó 1; A es un enlace sencillo o C(O); cada R es seleccionado independientemente de hidrógeno, halo, alquilo opcionalmente sustituido, haloalquilo opcionalmente sustituido, y cicloalquilo opcionalmente sustituido; cada R¹ es seleccionado independientemente de halo, ciano, alquilo de uno a seis átomos de carbono opcionalmente sustituido, alcoxi de uno a seis átomos de carbono opcionalmente sustituido, hidroxi, cicloalquilo de tres a ocho átomos de carbono opcionalmente sustituido, y sulfonilo opcionalmente sustituido; cada R² es seleccionado independientemente de halo, alquilo de uno a seis átomos de carbono opcionalmente sustituido, haloalquilo de uno a seis átomos de carbono opcionalmente sustituido, y cicloalquilo de tres a ocho átomos de carbono opcionalmente sustituido; R³ es hidrógeno, alquilo de uno a seis átomos de carbono opcionalmente sustituido, cicloalquilo de tres a ocho átomos de carbono opcionalmente sustituido, o arilo de seis a diez átomos de carbono opcionalmente sustituido; R⁴ es un heteroarilo de seis a doce miembros que tiene al menos dos heteroátomos, en donde cada heteroátomo es seleccionado independientemente de N, O, o S, en donde el heteroarilo está sustituido opcionalmente con uno, dos o tres miembros seleccionado independientemente de halo, ciano, -NH₂, alquilo de uno a seis átomos de carbono opcionalmente sustituido, alquinilo de dos a seis átomos de carbono opcionalmente sustituido; y R⁵ es hidrógeno o alquilo de uno a seis átomos de carbono opcionalmente sustituido; R⁵ y R³ junto con los átomos a los cuales están unidos forman opcionalmente un anillo heterocíclico de cuatro a ocho miembros; o una sal, un isómero, o una mezcla de los mismos, farmacéuticamente aceptables.
ARP150101856A 2014-06-13 2015-06-11 Inhibidores de fosfatidilinositol 3-quinasa AR100806A1 (es)

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US201462011775P 2014-06-13 2014-06-13

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AR100806A1 true AR100806A1 (es) 2016-11-02

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US (1) US10308639B2 (es)
EP (1) EP3154961B1 (es)
JP (1) JP6383810B2 (es)
KR (1) KR20170015508A (es)
CN (1) CN106459012A (es)
AR (1) AR100806A1 (es)
AU (1) AU2015274626C1 (es)
BR (1) BR112016028876A2 (es)
CA (1) CA2952018A1 (es)
EA (1) EA201692266A1 (es)
ES (1) ES2763104T3 (es)
IL (1) IL248789A0 (es)
MX (1) MX2016016538A (es)
NZ (1) NZ726055A (es)
SG (1) SG11201609527PA (es)
TW (1) TW201625590A (es)
WO (1) WO2015191743A1 (es)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2763103T3 (es) 2014-06-13 2020-05-27 Gilead Sciences Inc Inhibidor de la fosfatidilinositol 3-quinasa
ES2763104T3 (es) 2014-06-13 2020-05-27 Gilead Sciences Inc Derivados de quinazolinona como inhibidores de fosfatidilinositol 3-quinasa
CN106458932A (zh) 2014-06-13 2017-02-22 吉利德科学公司 磷脂酰肌醇3‑激酶抑制剂
MX2016016517A (es) 2014-06-13 2017-05-01 Gilead Sciences Inc Inhibidores de fosfatidilinositol 3-cinasa.
NZ726360A (en) 2014-06-13 2018-04-27 Gilead Sciences Inc Phosphatidylinositol 3-kinase inhibitors
JP7381190B2 (ja) 2014-12-26 2023-11-15 エモリー・ユニバーシテイ Ｎ４－ヒドロキシシチジン及び誘導体並びにそれに関連する抗ウイルス用途
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
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
KR101932146B1 (ko) 2016-07-14 2018-12-24 주식회사 바이오웨이 Pi3k를 억제하는 신규한 퀴나졸리논 유도체 및 이를 포함하는 약학적 조성물
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