AR096654A1 - Derivados de benzimidazol como inhibidores selectivos de proteína quinasa - Google Patents

Derivados de benzimidazol como inhibidores selectivos de proteína quinasa

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Publication number
AR096654A1
AR096654A1 ARP140102316A ARP140102316A AR096654A1 AR 096654 A1 AR096654 A1 AR 096654A1 AR P140102316 A ARP140102316 A AR P140102316A AR P140102316 A ARP140102316 A AR P140102316A AR 096654 A1 AR096654 A1 AR 096654A1
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AR
Argentina
Prior art keywords
group
heteroaryl
hydrogen
alkyl
aryl
Prior art date
Application number
ARP140102316A
Other languages
English (en)
Inventor
Picoul Willy
Moussy Alain
Schalon Claire
Benjahad Abdellah
Pez Didier
Chevenier Emmanuel
Sandrinelli Franck
Martin Jason
Original Assignee
Ab Science
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 Ab Science filed Critical Ab Science
Publication of AR096654A1 publication Critical patent/AR096654A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Birds (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Estos compuestos modulan, regulan y/o inhiben de forma selectiva la transducción, de señal mediada por ciertas proteínas quinasas nativas y/o mutantes involucradas en una variedad, de enfermedades humanas y animales tales como trastornos proliferativos celulares, metabólicos, alérgicos y degenerativos. En forma más particular, estos compuestos son inhibidores potentes y selectivos de un c-kit nativo y/o mutante. Reivindicación 1: Un compuesto de fórmula (1), donde: A es un grupo arilo o un grupo heteroarilo; n es 1, 2, 3, 4 ó 5; cada R¹ es, independientemente, un hidrógeno, un halógeno, un NH₂, un OH, un CN, un grupo alquilo o un grupo arilo o un grupo heteroarilo, donde el grupo alquilo, el grupo arilo y el grupo heteroarilo son insustituidos o sustituidos por uno o más sustituyentes seleccionados entre un halógeno, un grupo alquilo C₁₋₆ ramificado o lineal, un grupo alcoxi C₁₋₄, un grupo haloalquilo C₁₋₄, un grupo hidroxialquilo C₁₋₄, un grupo cicloalquilo C₃₋₇, un grupo arilo, un grupo heteroarilo, un grupo heterocicloalquilo, un hidroxilo, un tioalquilo, un ciano, un haloalcoxi, un grupo solubilizante, un grupo -NRR, -NR-CO-R, -CONRR, -SO₂NRR, -NRSO₂R donde R y R se seleccionan, cada uno en forma independiente, entre hidrógeno, un grupo alquilo o un grupo arilo o un grupo heteroarilo; R², R³ y R⁴ se seleccionan, cada uno en forma independiente, entre hidrógeno, halógeno, ciano, un grupo alquilo C₁₋₆, un grupo cicloalquilo C₃₋₇, un grupo alcoxi C₁₋₄, un grupo haloalquilo C₁₋₄, un grupo -NRR, -NR-CO-R, -CONRR donde R y R se seleccionan, cada uno en forma independiente, entre hidrógeno, o un grupo alquilo C₁₋₆; R⁵ es hidrógeno, un grupo alquilo C₁₋₆ o un grupo solubilizante; X es -(C=O)-, -O-, -S-, -NR⁶- o -(CH₂)ₙ- donde n es 0, 1 ó 2 y R⁶ representa un hidrógeno, un grupo alquilo C₁₋₆ o un grupo solubilizante; Q es un grupo alquilo o un grupo arilo o un grupo heteroarilo o un grupo heterocicloalquilo, donde el grupo alquilo, el grupo arilo, el grupo heteroarilo, y el grupo heterocicloalquilo son insustituidos o sustituidos por uno o más sustituyentes seleccionados entre un halógeno, un halometilo, un grupo alquilo C₁₋₆ ramificado o lineal, un grupo alcoxi C₁₋₄, un grupo haloalquilo C₁₋₄, un grupo hidroxialquilo C₁₋₄, un grupo cicloalquilo C₃₋₇, un grupo arilo, un grupo heteroarilo, un grupo heterocicloalquilo, un hidroxilo, un tioalquilo, un ciano, un haloalcoxi, un -CºC-R, un grupo solubilizante, un grupo -NRR, -NR-CO-R, -CONRR, SO₂R, -SO₂NRR, -NRSO₂R, -(CH₂)ₚ-NRR, -O-(CH₂)q-NRR, -(CH₂)ₚ-R, -O-(CH₂)q-R donde R y R se seleccionan, cada uno en forma independiente, entre hidrógeno, un grupo alquilo, o un grupo arilo o un grupo heteroarilo, R es un heteroarilo o un grupo heterocicloalquilo, p es 1 ó 2 y q es 2 ó 3.
ARP140102316A 2013-06-20 2014-06-19 Derivados de benzimidazol como inhibidores selectivos de proteína quinasa AR096654A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP13305837 2013-06-20

Publications (1)

Publication Number Publication Date
AR096654A1 true AR096654A1 (es) 2016-01-27

Family

ID=48741004

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140102316A AR096654A1 (es) 2013-06-20 2014-06-19 Derivados de benzimidazol como inhibidores selectivos de proteína quinasa

Country Status (6)

Country Link
US (1) US10202370B2 (es)
EP (1) EP3010906B1 (es)
AR (1) AR096654A1 (es)
HK (1) HK1222396A1 (es)
TW (1) TW201534597A (es)
WO (1) WO2014202763A1 (es)

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BR112021018168B1 (pt) 2019-03-21 2023-11-28 Onxeo Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer
AU2020378630A1 (en) 2019-11-08 2022-05-26 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
IL293592A (en) 2019-12-06 2022-08-01 Vertex Pharma Transduced tetrahydrofurans as sodium channel modulators
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
US20230192626A1 (en) * 2020-05-26 2023-06-22 Baylor College Of Medicine Novel soluble epoxide hydrolase inhibitors and method of use thereof
CN115916777A (zh) * 2020-07-09 2023-04-04 苏州爱科百发生物医药技术有限公司 一种atx抑制剂及其制备方法和应用
CN114380817B (zh) * 2020-10-21 2024-06-21 中国医学科学院药物研究所 苯并咪唑并2-氨基-1,3,4-噻二唑化合物及其制法和药物用途
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CN115850258A (zh) * 2022-12-27 2023-03-28 东北林业大学 一种马赛替尼的合成方法

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Also Published As

Publication number Publication date
TW201534597A (zh) 2015-09-16
US20160152608A1 (en) 2016-06-02
HK1222396A1 (zh) 2017-06-30
EP3010906A1 (en) 2016-04-27
EP3010906B1 (en) 2019-06-12
WO2014202763A1 (en) 2014-12-24
US10202370B2 (en) 2019-02-12

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