AR099367A1 - Inhibidores de la tirosina quinasa de bruton - Google Patents

Inhibidores de la tirosina quinasa de bruton

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Publication number
AR099367A1
AR099367A1 ARP140104561A ARP140104561A AR099367A1 AR 099367 A1 AR099367 A1 AR 099367A1 AR P140104561 A ARP140104561 A AR P140104561A AR P140104561 A ARP140104561 A AR P140104561A AR 099367 A1 AR099367 A1 AR 099367A1
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Argentina
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substituted
unsubstituted
heterocycloalkyl
independently
cycloalkyl
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ARP140104561A
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English (en)
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D Thomas William
Chen Wei
J Jia Zhaozhong
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Pharmacyclics Inc
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Publication of AR099367A1 publication Critical patent/AR099367A1/es

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    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
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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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
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    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/53—Heterocyclic 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
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C07D417/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D471/00—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
    • 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
    • C07D471/04—Ortho-condensed systems

Abstract

Se divulgan inhibidores reversibles e irreversibles de la tirosina quinasa de Bruton (Btk). Se divulgan asimismo composiciones farmacéuticas que incluyen a dichos compuestos. Además se describe el uso de los inhibidores Btk, ya sea solos o combinados con otros agentes terapéuticos, para el tratamiento de enfermedades o condiciones autoinmunes, enfermedades o condiciones heteroinmunes, cáncer, incluyendo linfoma, y enfermedades o condiciones inflamatorias. Reivindicación 1: Un compuesto de fórmula (1) caracterizado porque tiene la estructura descripta, en donde: el anillo A es C₃₋₆ cicloalquilo sustituido o sin sustituir, C₂₋₇ heterocicloalquilo sustituido o sin sustituir, C₆₋₁₂ arilo sustituido o sin sustituir, o C₁₋₁₂ heteroarilo sustituido o sin sustituir; W es -C(R²)- o -N-; X es -C(R²)- o -N-; Y está opcionalmente presente y cuando está presente es -CH₂O-, -OCH₂-, -OCH₂CH₂O-, -O-, -N(R³)-, -C(O)-, -N(R³)C(O)-, -C(O)N(R³)-, -N(R³)C(O)N(R³)-, -S(O)-, -S(O)₂-, -N(R³)S(O)₂-, -S(O)₂N(R³)-, -C(=NH)-, -C(=NH)N(R³)-, -C(=NH)N(R³)-, o C₁₋₄ alquileno sustituido o sin sustituir; Z está opcionalmente presente y cuando está presente es C₁₋₃ alquilo sustituido o sin sustituir, C₃₋₆ cicloalquilo sustituido o sin sustituir, C₂₋₇ heterocicloalquilo sustituido o sin sustituir, C₆₋₁₂ arilo sustituido o sin sustituir, o C₁₋₁₂ heteroarilo sustituido o sin sustituir; G es un compuesto de fórmula (2), ó (3); R¹ es -R⁴, -CH₂R⁴, -C(O)R⁹, -C(O)C(O)R⁹, -C(O)OR⁴, -C(O)N(R³)(R⁴), o -S(O)₂R⁹; R¹ es -C(O)R⁹-, -C(O)C(O)R⁹, -C(O)OR⁴, -C(O)N(R³)(R⁴), o -S(O)₂R⁹; cada R² es independientemente H, C₁₋₄ alquilo sustituido o sin sustituir, -CN, o halógeno; cada R³ es independientemente H, o C₁₋₄ alquilo sustituido o sin sustituir; cada R⁴ es independientemente H, C₁₋₆alquilo sustituido o sin sustituir, C₃₋₆ cicloalquilo sustituido o sin sustituir, C₂₋₇ heterocicloalquilo sustituido o sin sustituir, C₆₋₁₂ arilo sustituido o sin sustituir, o C₁₋₁₂ heteroarilo sustituido o sin sustituir; R⁵ es H, C₁₋₄ alquilo sustituido o sin sustituir, C₃₋₆ cicloalquilo sustituido o sin sustituir, C₂₋₇ heterocicloalquilo sustituido o sin sustituir, C₆₋₁₂ arilo sustituido o sin sustituir, o C₁₋₁₂ heteroarilo sustituido o sin sustituir; o R¹ y R⁵ junto con el átomo de nitrógeno al que están unidos se combinan para formar un anillos de C₂₋₉ heterocicloalquilo sustituido o sin sustituir; cada R⁶ es independientemente halógeno, -CN, -OH, -NH₂, sustituido o C₁₋₄ alcoxilo sin sustituir, C₁₋₄ alquilo sustituido o sin sustituir, C₃₋₆ cicloalquilo sustituido o sin sustituir, C₂₋₆ heterocicloalquilo sustituido o sin sustituir, o -N(R³)₂; o R¹ y R⁶ se combinan para formar un anillo de C₂₋₉ heterocicloalquilo sustituido o sin sustituir; cada R⁷ es independientemente halógeno, -CN, -OH, -NH₂, C₁₋₄ alcoxilo sustituido o sin sustituir, C₁₋₄ alquilo sustituido o sin sustituir, C₃₋₆ cicloalquilo sustituido o sin sustituir, C₂₋₆ heterocicloalquilo sustituido o sin sustituir, o -N(R³)₂; R⁹ es -R⁴, o un resto de fórmula (4); R¹⁰ es H, halógeno, -CN, o -L¹-L²; R¹¹ y R¹² son independientemente H, halógeno, -CN, o -L¹-L²; o R¹¹ y R¹² tomados juntos forman un enlace; cada L¹ está opcionalmente presente y cuando está presente cada L¹ es independientemente C₁₋₆ alquilo sustituido o sin sustituir, C₃₋₆ cicloalquilo sustituido o sin sustituir, C₁₋₆ heteroalquilo sustituido o sin sustituir, C₂₋₇ heterocicloalquilo sustituido o sin sustituir, C₆₋₁₂ arilo sustituido o sin sustituir, C₁₋₁₂ heteroarilo sustituido o sin sustituir, -C(=O)-, -O-, o -S-; cada L² es independientemente H, C₁₋₆ alquilo sustituido o sin sustituir, C₃₋₆ cicloalquilo sustituido o sin sustituir, C₁₋₆ heteroalquilo sustituido o sin sustituir, C₂₋₇ heterocicloalquilo sustituido o sin sustituir, C₆₋₁₂ arilo sustituido o sin sustituir, C₁₋₁₂ heteroarilo sustituido o sin sustituir o -N(R¹³)₂; cada R¹³ es independientemente H, C₁₋₆ alquilo, C₃₋₆ cicloalquilo, C₁₋₆ heteroalquilo, C₂₋₇ heterocicloalquilo, C₆₋₁₂ arilo, o C₁₋₁₂ heteroarilo; n es 0 - 3; p es 0 - 3; y q es 0 - 3; o un solvato farmacéuticamente aceptable, sal farmacéuticamente aceptable, o profármaco farmacéuticamente aceptable del mismo; con la condición de que i) cuando W es N, y R¹ es H, t-Boc, o -C(O)-CH=CH₂; entonces X es distinto de C-Et o N; y ii) cuando W es N, G es el compuesto de fórmula (3); entonces X es CH o N; iii) cuando W es N, y X es CH; entonces R¹ es distinto de -C(O)Me, o t-Boc; y iv) cuando n es 0; entonces cada uno de p y q es independientemente 0, 1, ó 2.
ARP140104561A 2013-12-05 2014-12-05 Inhibidores de la tirosina quinasa de bruton AR099367A1 (es)

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EP (1) EP3077388A1 (es)
JP (3) JP6345786B2 (es)
KR (1) KR20160093675A (es)
CN (1) CN105960404B (es)
AR (1) AR099367A1 (es)
AU (3) AU2014360446A1 (es)
BR (1) BR112016012728A2 (es)
CA (1) CA2932609A1 (es)
MX (2) MX2016007111A (es)
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WO (1) WO2015084998A1 (es)

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JP2018522823A (ja) * 2015-06-02 2018-08-16 ファーマサイクリックス エルエルシー ブルトン型チロシンキナーゼの阻害剤
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JP2022505987A (ja) * 2018-10-22 2022-01-14 エスカー セラピューティクス，インコーポレイテッド Ｔｙｋ２阻害剤およびその使用
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KR20210149757A (ko) 2019-04-09 2021-12-09 누릭스 테라퓨틱스 인코포레이티드 Cbl-b 억제용의 3-치환된 피페리딘 화합물, 및 암 백신 및/또는 종양용해 바이러스와 조합된 cbl-b 억제제의 용도
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