AR098414A1 - PIPERAZINAS DE PIRAZOLO SUSTITUIDO COMO INHIBIDORES DE CASEÍNA QUINASA 1 d/e - Google Patents

PIPERAZINAS DE PIRAZOLO SUSTITUIDO COMO INHIBIDORES DE CASEÍNA QUINASA 1 d/e

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Publication number
AR098414A1
AR098414A1 ARP140104277A ARP140104277A AR098414A1 AR 098414 A1 AR098414 A1 AR 098414A1 AR P140104277 A ARP140104277 A AR P140104277A AR P140104277 A ARP140104277 A AR P140104277A AR 098414 A1 AR098414 A1 AR 098414A1
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Argentina
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substituted
independently selected
nrara
heterocyclyl
alkyl
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ARP140104277A
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English (en)
Inventor
Velaparthi Upender
Padmakar Darne Chetan
Liu Peiying
D Wittman Mark
C Pearce Bradley
Araujo Erika
Dasgupta Bireshwar
Surendran Nair Jalathi
Kumaran Janakiraman Sakthi
Reddy Rachamreddy Chandrasekhar
Mallikarjuna Rao Mettu
Mozhi Selvan Subbiah Karuppiah Arul
Subba Reddy Bandreddy
Nagalakshmi Pulicharla
Onkardas Bora Rajesh
Holehatti Maheshwarappa Shilpa
Selvakumar Kumaravel
Mullick Dibakar
Sistla Ramesh
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Bristol Myers Squibb Co
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Publication of AR098414A1 publication Critical patent/AR098414A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—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 three hetero rings
    • C07D487/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—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
    • C07D491/12—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 three hetero rings
    • C07D491/14—Ortho-condensed systems
    • C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—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
    • C07D491/12—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 three hetero rings
    • C07D491/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Sales de aquellos aceptables desde el punto de vista farmacéutico. Los compuestos inhiben la actividad de la proteína quinasa, lo cual los vuelve útiles como agentes antineoplásicos. Reivindicación 1: Un compuesto caracterizado por la fórmula (1), o una sal de este aceptable desde el punto de vista farmacéutico, en donde X se selecciona independientemente de O y NH; R¹ se selecciona independientemente de carbociclilo sustituido con 1 - 5 R⁵, y heterociclilo que comprende átomos de carbono y 1 a 3 heteroátomos seleccionados de N, NR⁴, O, S, y sustituidos con 1 - 5 R⁵; R² se selecciona independientemente de (i) alquilo opcionalmente sustituido con F, Cl, Br, ORᵇ, CN, NRᵃRᵃ, -C(=O)NRᵃRᵃ, C₂₋₆ alquenilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquinilo sustituido con 0 - 5 Rᵉ, carbociclilo sustituido con 1 - 8 R⁷ y heterociclilo que comprende átomos de carbono y 1 a 4 heteroátomos seleccionados de N, NR⁶, O, S, y sustituidos con 1 - 8 R⁷, (ii) cicloalquilo sustituido con 1 - 8 R⁷, y (iii) cicloheteroalquilo sustituido con 1 - 8 R⁷; R³ᵃ, R³ᵇ, R³ᶜ, R³ᵈ, R³ᵉ y R³ᶠ se seleccionan independientemente de H, CN, C₁₋₄ alquilo sustituido con 1 - 3 R⁸, -C(=O)ORᵇ, -C(=O)NRᵃRᵃ, -C(=O)Rᵇ, -NRᵃC(=O)Rᵇ, -NRᵃC(=O)ORᵇ, -(CH₂)ʳ-carbociclilo sustituido con 1 - 3 R⁸ y -(CH₂)ʳ-heterociclilo sustituido con 1 - 3 R⁸; de manera alternativa, R³ᵃ y R³ᵇ, o R³ᶜ y R³ᵈ o R³ᵉ y R³ᶠ, junto con el átomo de carbono al que están unidos, forman un anillo spiro carbocíclico o heterocíclico que comprende átomos de carbono y 1 a 4 heteroátomos seleccionados de N, O, S, cada uno sustituido con 1 - 5 R⁸; de manera alternativa, R³ᵃ y R³ᶜ, o R³ᵇ y R³ᵈ, juntos forman un anillo heterocíclico que comprende átomos de carbono y 1 a 4 heteroátomos seleccionados de N, O, S, y sustituidos con 1 - 5 R⁸; R⁴ se selecciona independientemente de H, C₁₋₄ alquilo sustituido con 0 - 3 Rᵉ, -(CH₂)ʳCN, -(CH₂)ʳORᵇ, (CH₂)ʳS(O)ₚRᶜ, -(CH₂)ʳC(=O)Rᵇ, -(CH₂)ʳNRᵃRᵃ, -(CH₂)ʳC(=O)NRᵃRᵃ, -(CH₂)ʳNRᵃC(=O)Rᵇ, -(CH₂)ʳNRᵃC(=O)ORᵇ, -(CH₂)ʳOC(=O)NRᵃRᵃ, -(CH₂)ʳNRᵃC(=O)NRᵃRᵃ, -(CH₂)ʳC(=O)ORᵇ, -(CH₂)ʳS(O)₂NRᵃRᵃ, -(CH₂)ʳNRᵃS(O)₂NRᵃRᵃ, -(CH₂)ʳNRᵃS(O)₂Rᶜ, (CH₂)ʳ-carbociclilo sustituido con 0 - 3 Rᵉ y -(CH₂)ʳ-heterociclilo sustituido con 0 - 3 Rᵉ; R⁵, en cada caso, se selecciona independientemente de H, C₁₋₄ alquilo sustituido con 0 - 3 Rᵉ, F, Cl, Br, =O, CN, NO₂, -ORᵇ, -(CH₂)ʳCN, -(CH₂)ʳORᵇ, (CH₂)ʳS(O)ₚRᶜ, -(CH₂)ʳC(=O)Rᵇ, -(CH₂)ʳNRᵃRᵃ, -(CH₂)ʳC(=O)NRᵃRᵃ, -(CH₂)ʳNRᵃC(=O)Rᵇ, -(CH₂)ʳNRᵃC(=O)ORᵇ, -(CH₂)ʳOC(=O)NRᵃRᵃ, -(CH₂)ʳNRᵃC(=O)NRᵃRᵃ, -(CH₂)ʳC(=O)ORᵇ, -(CH₂)ʳS(O)₂NRᵃRᵃ, -(CH₂)ʳNRᵃS(O)₂NRᵃRᵃ, -(CH₂)ʳNRᵃS(O)₂Rᶜ, (CH₂)ʳ-carbociclilo sustituido con 0 - 3 Rᵉ y -(CH₂)ʳ-heterociclilo sustituido con 0 - 3 Rᵉ; R⁶ se selecciona independientemente de H, -C(=O)Rᵇ, -CO(=O)Rᵇ, -S(O)ₚRᶜ, C₁₋₆ alquilo sustituido con 0 - 5 Rᵉ; -(CH₂)ʳ-C₃₋₆ carbociclilo sustituido con 0 - 5 Rᵉ y -(CH₂)ʳ-heterociclilo sustituido con 0 - 5 Rᵉ; R⁷, en cada caso, se selecciona independientemente de H, F, Cl, Br, =O, -(CRᵈRᵈ)ʳCN, NO₂, -(CRᵈRᵈ)ʳORᵇ, -S(O)ₚRᶜ, -C(=O)Rᵇ, -(CRᵈRᵈ)ʳNRᵃRᵃ, -(CRᵈRᵈ)ʳC(=O)NRᵃRᵃ, -NRᵃ(=O)Rᵇ, -NRᵃC(=O)ORᵇ, -OC(=O)NRᵃRᵃ, -NRᵃC(=O)NRᵃRᵃ, -(CRᵈRᵈ)ʳC(=O)ORᵇ, -S(O)₂NRᵃRᵃ, -NRᵃS(O)₂NRᵃRᵃ, -NRᵃS(O)₂Rᶜ, C₁₋₆ alquilo sustituido con 0 - 5 Rᵉ, -(CRᵈRᵈ)ʳ-C₃₋₆ carbociclilo sustituido con 0 - 5 Rᵉ y -(CRᵈRᵈ)ʳ-heterociclilo sustituido con 0 - 5 Rᵉ; R⁸, en cada caso, se selecciona independientemente de H, F, Cl, Br, CN, C₁₋₆ alquilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquenilo, C₂₋₆ alquinilo, -(CH₂)ʳ-C₃₋₆ cicloalquilo sustituido con 0 - 5 Rᵉ, -(CH₂)ʳ-arilo sustituido con 0 - 5 Rᵉ, -(CH₂)ʳ-heterociclilo sustituido con 0 - 5 Rᵉ, CO₂H, -(CH₂)ʳORᵇ y -(CH₂)ʳNRᵃRᵃ; Rᵃ, en cada caso, se selecciona independientemente de H, CN, C₁₋₆ alquilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquenilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquinilo sustituido con 0 - 5 Rᵉ, -(CH₂)ʳ-C₃₋₁₀ carbociclilo sustituido con 0 - 5 Rᵉ y -(CH₂)ʳ-heterociclilo sustituido con 0 - 5 Rᵉ; o Rᵃ y Rᵃ, junto con el átomo de nitrógeno al que están unidos, forman un anillo heterocíclico sustituido con 0 - 5 Rᵉ; Rᵇ, en cada caso, se selecciona independientemente de H, C₁₋₆ alquilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquenilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquinilo sustituido con 0 - 5 Rᵉ, -(CH₂)ʳ-C₃₋₁₀ carbociclilo sustituido con 0 - 5 Rᵉ y -(CH₂)ʳ-heterociclilo sustituido con 0 - 5 Rᵉ; Rᶜ, en cada caso, se selecciona independientemente de C₁₋₆ alquilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquenilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquinilo sustituido con 0 - 5 Rᵉ, C₃₋₆ carbociclilo y heterociclilo; Rᵈ, en cada caso, se selecciona independientemente de H y C₁₋₄ alquilo sustituido con 0 - 5 Rᵉ; Rᵉ, en cada caso, se selecciona independientemente de F, Cl, Br, CN, NO₂, =O, C₁₋₆ alquilo sustituido con 0 - 5 Rᶠ, C₂₋₆ alquenilo, C₂₋₆ alquinilo, -(CH₂)ʳ-C₃₋₆ cicloalquilo, -(CH₂)ʳ-arilo, -(CH₂)ʳ-heterociclilo, CO₂H, -(CH₂)ʳORᶠ, SRᶠ, y -(CH₂)ʳNRᶠRᶠ; Rᶠ, en cada caso, se selecciona independientemente de H, C₁₋₅ alquilo, opcionalmente sustituido con F, Cl, Br, C₃₋₆ cicloalquilo y fenilo, o Rᶠ y Rᶠ junto con el átomo de nitrógeno al que están unidos, forman un anillo heterocíclico opcionalmente sustituido con C₁₋₄ alquilo; p, en cada caso, se selecciona independientemente de 0, 1 y 2; y r, en cada caso, se selecciona independientemente de 0, 1, 2, 3 y 4.
ARP140104277A 2013-11-14 2014-11-13 PIPERAZINAS DE PIRAZOLO SUSTITUIDO COMO INHIBIDORES DE CASEÍNA QUINASA 1 d/e AR098414A1 (es)

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US (3) US9598423B2 (es)
EP (2) EP3068784B1 (es)
JP (2) JP6494624B2 (es)
CN (2) CN105916856B (es)
AR (1) AR098414A1 (es)
ES (2) ES2718218T3 (es)
TW (1) TW201605859A (es)
UY (1) UY35834A (es)
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