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AR098647A1 - Inhibidores de serina / treonina cinasa - Google Patents

Inhibidores de serina / treonina cinasa

Info

Publication number
AR098647A1
AR098647A1 ARP140104549A ARP140104549A AR098647A1 AR 098647 A1 AR098647 A1 AR 098647A1 AR P140104549 A ARP140104549 A AR P140104549A AR P140104549 A ARP140104549 A AR P140104549A AR 098647 A1 AR098647 A1 AR 098647A1
Authority
AR
Argentina
Prior art keywords
alkyl
independently
alkoxy
formula
halogen
Prior art date
Application number
ARP140104549A
Other languages
English (en)
Original Assignee
Genentech 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 Genentech Inc filed Critical Genentech Inc
Publication of AR098647A1 publication Critical patent/AR098647A1/es

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/53Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/16Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/16Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/12Heterocyclic 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 three hetero rings
    • C07D513/16Peri-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Los compuestos de fórmula (1) son inhibidores de la cinasa ERK. También se describen composiciones y métodos para tratar trastornos hiperproliferativos. Reivindicación 1: Un compuesto de fórmula (1) caracterizado porque: X¹ es N o CH; X² es NRᵃ, O ó S; X³ es (CR⁴₂)₁₋₃, CH₂NRᵇ, C(=O), C(=O)NRᵇ o C(=O)O con la condición de que: cuando X³ es CH₂NRᵇ, el resto tricíclico de fórmula (1) es un 6,7,8,9-tetrahidro-1,2,2a¹,6,8-pentaazabenzo[cd]azuleno, cuando X³ es C(=O)NRᵇ, el resto tricíclico de fórmula (1) es un 8,9-dihidro-1,2,2a¹,6,8-pentaazabenzo[cd]azulen-7(6H)-ona, cuando X³ es CH₂C(=O), el resto tricíclico de fórmula (1) es un 8,9-dihidro-1,2,2a¹,6-tetraazabenzo[cd]azulen-7(6H)-ona y cuando X³ es C(=O)O, el resto tricíclico de fórmula (1) es un 6H-8-oxa-1,2,2a¹,6-tetraazabenzo[cd]azulen-7(9H)-ona; X⁴ es CR²R³ o NR³ con la condición de que cuando X⁴ es NR³, X² es NRᵃ y X³ es C(=O); R¹ es (i) un heterociclilo de 4 a 7 miembros saturado o parcialmente insaturado o (ii) un heteroarilo de 5 a 6 miembros opcionalmente sustituido; R² se selecciona del grupo que consiste en: (a) alquilo C₁₋₁₀, (b) alquenilo C₁₋₁₀ (c) haloalquilo C₁₋₁₀, (d) cicloalquilo C₃₋₇ o cicloalquilo C₃₋₇-alquilo C₁₋₆; (e) halocicloalquilo C₃₋₇ o halocicloalquilo C₃₋₇-alquilo C₁₋₆; (f) hidroxialquilo C₁₋₁₀ o dihidroxialquilo C₁₋₁₀; (g) alcoxi C₁₋₃-alquilo C₁₋₆; (h) alquiltio C₁₋₃-alquilo C₁₋₆; (i) cianoalquilo C₁₋₁₀; (j) fenilo, fenil-alquilo C₁₋₃. fenoxi o benciloxi-alquilo C₁₋₃; (k) heteroarilo, heteroaril-alquilo C₁₋₃ o heteroariloxi en donde dicho resto heteroarilo se selecciona del grupo que consiste en pirazolilo, imidazolilo, oxazolilo, isoazolilo, tiazolilo, isotiazolilo, piridinilo, pirid-2(1H)-ona y 1-alquilpirid-2(1H)-ona y cada dicho heteroarilo está independientemente y opcionalmente sustituido con uno o más grupos seleccionados del grupo que consiste en halógeno, hidroxilo, óxido, alcoxi C₁₋₆, haloalcoxi C₁₋₆, ciano, cicloalquilo C₃₋₆ y alquilo C₁₋₆ en donde dicho alquilo C₁₋₆ está opcionalmente e independientemente sustituido con uno o más grupos seleccionados independientemente de; halógeno, oxo, hidroxilo o alcoxi C₁₋₆; y, (l) feniltio o feniltio-alquilo C₁₋₆; R³ y R⁴ es independientemente en cada aparición de hidrógeno o alquilo C₁₋₃; Rᵃ y Rᵇ son independientemente hidrógeno o alquilo C₁₋₃; o una sal farmacéuticamente aceptable de este; en donde cualquier resto fenilo es uno o más halógeno, ciano, hidroxilo, alcoxi C₁₋₆, haloalcoxi C₁₋₆ o alquilo C₁₋₆ opcionalmente sustituido en donde dicho alquilo C₁₋₆ está opcionalmente e independientemente sustituido con uno o más grupos seleccionados independientemente de halógeno, oxo hidroxilo o alcoxi C₁₋₆; y en donde cada cicloalquilo está independientemente y opcionalmente sustituido con uno a tres grupos halógeno, haloalquilo C₁₋₆, alcoxi C₁₋₆;o haloalcoxi C₁₋₆.
ARP140104549A 2013-12-06 2014-12-05 Inhibidores de serina / treonina cinasa AR098647A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361912905P 2013-12-06 2013-12-06

Publications (1)

Publication Number Publication Date
AR098647A1 true AR098647A1 (es) 2016-06-01

Family

ID=52350292

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140104549A AR098647A1 (es) 2013-12-06 2014-12-05 Inhibidores de serina / treonina cinasa

Country Status (23)

Country Link
US (5) US9867833B2 (es)
EP (1) EP3077401B1 (es)
JP (2) JP6449293B2 (es)
KR (1) KR102359759B1 (es)
CN (1) CN106029672B (es)
AR (1) AR098647A1 (es)
AU (1) AU2014360455B2 (es)
BR (1) BR112016012844B1 (es)
CA (1) CA2932729C (es)
CL (1) CL2016001368A1 (es)
CR (1) CR20160309A (es)
EA (1) EA031243B1 (es)
IL (1) IL246017B (es)
MA (1) MA39170B1 (es)
MX (1) MX368443B (es)
MY (1) MY176049A (es)
PE (1) PE20160886A1 (es)
PH (1) PH12016501071B1 (es)
SG (1) SG11201604573WA (es)
TW (1) TWI557126B (es)
UA (1) UA120506C2 (es)
WO (1) WO2015085007A1 (es)
ZA (1) ZA201604461B (es)

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* Cited by examiner, † Cited by third party
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CN104755478B (zh) 2012-10-16 2017-10-10 霍夫曼-拉罗奇有限公司 丝氨酸/苏氨酸激酶抑制剂
US9532987B2 (en) 2013-09-05 2017-01-03 Genentech, Inc. Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases
PE20160886A1 (es) 2013-12-06 2016-09-14 Genentech Inc Inhibidores de serina/treonina cinasa
WO2015103133A1 (en) 2013-12-30 2015-07-09 Genentech, Inc. Serine/threonine kinase inhibitors
BR112016015236B1 (pt) * 2013-12-30 2023-11-14 Array Biopharma Inc. Composto, composições farmacêuticas, usos de um composto e método in vitro de inibição da atividade da proteína quinase erk
JP6877423B2 (ja) 2015-11-09 2021-05-26 アストラゼネカ・アクチエボラーグAstrazeneca Aktiebolag がんの処置において有用なジヒドロイミダゾピラジノン誘導体
WO2017180581A1 (en) 2016-04-15 2017-10-19 Genentech, Inc. Diagnostic and therapeutic methods for cancer
KR102811888B1 (ko) 2017-09-08 2025-05-27 에프. 호프만-라 로슈 아게 암의 진단 및 치료 방법
US20210008047A1 (en) 2018-02-13 2021-01-14 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
BR112021024546A2 (pt) * 2019-06-06 2022-02-08 Hutchison Medipharma Ltd Compostos tricíclicos e uso dos mesmos
CN116583524B (zh) * 2021-02-03 2025-06-13 江苏恒瑞医药股份有限公司 稠三环类细胞周期蛋白-依赖性激酶抑制剂及其制备方法和医药用途

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CA2817629C (en) 2010-11-23 2019-08-13 Abbvie Inc. Salts and crystalline forms of an apoptosis-inducing agent
WO2012118850A1 (en) 2011-02-28 2012-09-07 Array Biopharma Inc. Serine/threonine kinase inhibitors
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EP3321262B1 (en) * 2012-03-01 2021-01-13 Array Biopharma, Inc. Serine/threonine kinase inhibitors
KR20150047597A (ko) 2012-08-27 2015-05-04 어레이 바이오파마 인크. 과증식성 질환의 치료를 위한 세린/트레오닌 키나아제 억제제
CN104755478B (zh) 2012-10-16 2017-10-10 霍夫曼-拉罗奇有限公司 丝氨酸/苏氨酸激酶抑制剂
US9532987B2 (en) 2013-09-05 2017-01-03 Genentech, Inc. Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases
PE20160886A1 (es) 2013-12-06 2016-09-14 Genentech Inc Inhibidores de serina/treonina cinasa
WO2015103133A1 (en) 2013-12-30 2015-07-09 Genentech, Inc. Serine/threonine kinase inhibitors
BR112016015236B1 (pt) 2013-12-30 2023-11-14 Array Biopharma Inc. Composto, composições farmacêuticas, usos de um composto e método in vitro de inibição da atividade da proteína quinase erk
TWI762806B (zh) 2014-04-09 2022-05-01 美商建南德克公司 作為erk抑制劑之化合物

Also Published As

Publication number Publication date
MX2016007352A (es) 2016-09-08
US11376260B2 (en) 2022-07-05
KR20160093703A (ko) 2016-08-08
MX368443B (es) 2019-10-02
US20190192534A1 (en) 2019-06-27
EP3077401A1 (en) 2016-10-12
US10278975B2 (en) 2019-05-07
EP3077401B1 (en) 2018-04-18
SG11201604573WA (en) 2016-07-28
MA39170B1 (fr) 2019-05-31
AU2014360455A1 (en) 2016-07-07
UA120506C2 (uk) 2019-12-26
KR102359759B1 (ko) 2022-02-09
US9867833B2 (en) 2018-01-16
PH12016501071A1 (en) 2016-07-25
NZ721361A (en) 2021-07-30
IL246017B (en) 2019-10-31
CA2932729C (en) 2021-02-23
US20210106593A1 (en) 2021-04-15
TW201522338A (zh) 2015-06-16
IL246017A0 (en) 2016-08-02
TWI557126B (zh) 2016-11-11
US10517878B2 (en) 2019-12-31
JP2019034970A (ja) 2019-03-07
BR112016012844A2 (es) 2017-08-08
US10842799B2 (en) 2020-11-24
CN106029672A (zh) 2016-10-12
MY176049A (en) 2020-07-22
US20150182537A1 (en) 2015-07-02
JP2016539153A (ja) 2016-12-15
PE20160886A1 (es) 2016-09-14
EA201691177A1 (ru) 2016-10-31
MA39170A1 (fr) 2018-04-30
WO2015085007A1 (en) 2015-06-11
US20200078371A1 (en) 2020-03-12
ZA201604461B (en) 2022-05-25
CA2932729A1 (en) 2015-06-11
BR112016012844B1 (pt) 2023-01-10
CN106029672B (zh) 2019-03-29
CR20160309A (es) 2016-08-25
AU2014360455B2 (en) 2018-05-10
PH12016501071B1 (en) 2019-04-26
US20180000833A1 (en) 2018-01-04
CL2016001368A1 (es) 2016-12-09
EA031243B1 (ru) 2018-12-28
JP6449293B2 (ja) 2019-01-09

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