AR122703A1 - Inhibidores de rip1k - Google Patents

Inhibidores de rip1k

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Publication number
AR122703A1
AR122703A1 ARP210101712A ARP210101712A AR122703A1 AR 122703 A1 AR122703 A1 AR 122703A1 AR P210101712 A ARP210101712 A AR P210101712A AR P210101712 A ARP210101712 A AR P210101712A AR 122703 A1 AR122703 A1 AR 122703A1
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AR
Argentina
Prior art keywords
occurrence
optionally substituted
independently
ora
alkyl
Prior art date
Application number
ARP210101712A
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English (en)
Inventor
Somasekhar Bhamidipati
Ihab Darwish
Mark Irving
Rao Kolluri
Esteban Masuda
Simon Shaw
Vanessa Taylor
Jiaxin Yu
Original Assignee
Rigel Pharmaceuticals Inc
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Application filed by Rigel Pharmaceuticals Inc filed Critical Rigel Pharmaceuticals Inc
Publication of AR122703A1 publication Critical patent/AR122703A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed 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
    • A61K31/41Heterocyclic 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
    • A61K31/41961,2,4-Triazoles
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further 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
    • A61K31/55Heterocyclic 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
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/554Heterocyclic 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 sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • C07D498/02Heterocyclic 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 two hetero rings
    • C07D498/04Ortho-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
    • C07D498/14Ortho-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
    • C07D498/22Heterocyclic 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 four or more hetero rings
    • 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-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
    • C07D513/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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

Abstract

En la presente descripción se describen compuestos inhibidores de quinasa, tales como compuestos inhibidores de proteína quinasa 1 que interactúa con el receptor (RIP1), así como también composiciones farmacéuticas y combinaciones que comprenden tales compuestos inhibidores. Los compuestos, composiciones farmacéuticas y/o combinaciones descritas pueden usarse para tratar o prevenir una enfermedad o afección asociada a quinasas, particularmente una enfermedad o afección asociada a RIP1. Reivindicación 1: Un compuesto de acuerdo con la fórmula (1) en donde X se selecciona de CH₂, O, S, S(O), S(O)₂ y NRᵃ; Rᵃ para cada aparición se selecciona de hidrógeno, alquilo C₁₋₆ y acilo C₁₋₆; Y¹, Y² y Y³ se seleccionan independientemente del grupo que consiste en N, N(Rᵃ), O, C(Rᵇ)₁₋₂ y C=O; Rᵇ se selecciona de hidrógeno, alquilo C₁₋₆ y halo; Z es C(Rᶜ) o NRᶜ; Rᶜ es una cadena de carbono insaturada C₁₋₄ opcionalmente sustituida con uno o más grupos R¹, opcionalmente interrumpida por 1 ó 2 heteroátomos seleccionados de O, N y S; RZ es N, CH o C(R¹) y junto con ZRᶜ y el carbono al que están unidos, forman un anillo heteroarilo de 5 ó 6 miembros o arilo de 6 miembros sustituido con m grupos R¹; R¹ es un enlazador-grupo R⁶, en donde el enlazador es un enlace, alcanilo (C₁-C₄), alquenilo (C₁-C₄) o alquinilo (C₁-C₄), opcionalmente sustituido por uno o más Rᵇ y R⁶ es Rᵉ, -C(Rᶠ)₃ o -C(Rᶠ)=C(Rᶠ)₂; R² es Rᵃ; el anillo B es heteroarilo de 5 - 10 miembros; R³, para cada aparición, se selecciona independientemente de Rᵇ y ORᵃ; L es O, NRᵃ o alquileno; W es arilo o heteroarilo de 5 - 10 miembros opcionalmente sustituido por p R⁴; R⁴ para cada aparición se selecciona de Rᵇ y ORᵃ; Rᵈ para cada aparición se selecciona independientemente de hidrógeno, alquilo C₁₋₆, aralquilo, arilo o heteroarilo C₅₋₁₀, o dos Rᵈ junto con un nitrógeno al que ambos están conectados forman un grupo heterocíclico C₃₋₁₀ opcionalmente sustituido por uno o más Rᵉ; Rᵉ es independientemente para cada aparición halo, -ORᵈ, -SRᵈ, -S(O)₂Rᵈ, -NRᵈRᵈ, -Si(Rᵃ)₃, -C(O)OH, -C(O)ORᵃ o -C(O)NRᵈRᵈ; Rᶠ es independientemente para cada aparición Rᵃ, Rᵇ o Rᵉ o dos grupos Rᶠ junto con el átomo de carbono unido al mismo proporcionan un grupo cicloalquilo C₃₋₆ o un grupo heterocíclico C₃₋₁₀, cada uno opcionalmente sustituido con uno o más Rᵉ; m es 1, 2, 3 ó 4; n es 0, 1 ó 2; y p es 0, 1, 2, 3, 4 ó 5.
ARP210101712A 2020-07-01 2021-06-22 Inhibidores de rip1k AR122703A1 (es)

Applications Claiming Priority (1)

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US202063047194P 2020-07-01 2020-07-01

Publications (1)

Publication Number Publication Date
AR122703A1 true AR122703A1 (es) 2022-09-28

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ID=76972022

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ARP210101712A AR122703A1 (es) 2020-07-01 2021-06-22 Inhibidores de rip1k

Country Status (19)

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US (2) US11667643B2 (es)
EP (1) EP4175714A1 (es)
JP (1) JP2023532718A (es)
KR (1) KR20230033712A (es)
CN (1) CN116209662A (es)
AR (1) AR122703A1 (es)
AU (1) AU2021300831A1 (es)
BR (1) BR112022026908A2 (es)
CA (1) CA3183296A1 (es)
CL (1) CL2022003812A1 (es)
CO (1) CO2023000051A2 (es)
CR (1) CR20220685A (es)
DO (1) DOP2022000300A (es)
EC (1) ECSP22097749A (es)
IL (1) IL299128A (es)
MX (1) MX2023000138A (es)
PE (1) PE20230730A1 (es)
TW (1) TWI824259B (es)
WO (1) WO2022005898A1 (es)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR122703A1 (es) 2020-07-01 2022-09-28 Rigel Pharmaceuticals Inc Inhibidores de rip1k
WO2023240379A1 (zh) * 2022-06-13 2023-12-21 南京医工医药技术有限公司 咪唑啉酮衍生物及其用途

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EP2192838A4 (en) 2007-08-15 2011-07-27 Harvard College HETEROCYCLIC NEKROPTOSIS HEMMER
TWI638815B (zh) 2013-02-15 2018-10-21 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺類(一)
JP2016514693A (ja) 2013-03-15 2016-05-23 プレジデント アンド フェローズ オブ ハーバード カレッジ ハイブリッド型ネクロトーシス阻害剤
EP3182974A1 (en) 2014-08-21 2017-06-28 GlaxoSmithKline Intellectual Property Development Limited Heterocyclic amides as rip1 kinase inhibitors as medicaments
JP2018505199A (ja) 2015-02-13 2018-02-22 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited (S)−5−ベンジル−N−(5−メチル−4−オキソ−2,3,4,5テトラヒドロベンゾ[b][1,4]オキサゼピン−3−イル)−4H−1,2,4−トリアゾール−3−カルボキサミドの結晶形
KR102603915B1 (ko) 2015-07-02 2023-11-21 에프. 호프만-라 로슈 아게 이환형 락탐 및 이의 사용 방법
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JP6754772B2 (ja) 2015-10-23 2020-09-16 武田薬品工業株式会社 複素環化合物
WO2017109724A1 (en) 2015-12-21 2017-06-29 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
KR20180114910A (ko) 2016-02-05 2018-10-19 데날리 테라퓨틱스 인크. 수용체-상호작용 단백질 키나제 1의 억제제
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ES2947446T3 (es) 2018-05-03 2023-08-09 Rigel Pharmaceuticals Inc Compuestos inhibidores de RIP1 y métodos para fabricar y usar los mismos
JP2022511213A (ja) 2018-06-26 2022-01-31 シャンハイ インスティテュート オブ オーガニック ケミストリー,チャイニーズ アカデミー オブ サイエンシズ 細胞壊死阻害剤、その調製方法およびその使用
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CN111138448B (zh) 2018-11-02 2022-08-02 中国科学院上海药物研究所 抑制rip1激酶的杂环酰胺及其用途
AU2020341681B2 (en) 2019-09-06 2024-02-15 Rigel Pharmaceuticals, Inc. RIP1 inhibitory compounds and methods for making and using the same
CR20220075A (es) 2019-09-06 2022-07-14 Rigel Pharmaceuticals Inc Compuestos inhibidores de rip1 y métodos para prepararlos y usarlos
US11578078B2 (en) 2019-11-07 2023-02-14 Rigel Pharmaceuticals, Inc. Heterocyclic RIP1 inhibitory compounds
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AR122703A1 (es) 2020-07-01 2022-09-28 Rigel Pharmaceuticals Inc Inhibidores de rip1k

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JP2023532718A (ja) 2023-07-31
TW202214225A (zh) 2022-04-16
IL299128A (en) 2023-02-01
TWI824259B (zh) 2023-12-01
ECSP22097749A (es) 2023-03-31
DOP2022000300A (es) 2023-03-31
US20220009936A1 (en) 2022-01-13
BR112022026908A2 (pt) 2023-03-14
EP4175714A1 (en) 2023-05-10
US11667643B2 (en) 2023-06-06
WO2022005898A1 (en) 2022-01-06
CA3183296A1 (en) 2022-01-06
MX2023000138A (es) 2023-04-11
AU2021300831A1 (en) 2023-01-19
PE20230730A1 (es) 2023-05-03
US20230265100A1 (en) 2023-08-24
CO2023000051A2 (es) 2023-04-17
CL2022003812A1 (es) 2023-08-18
CR20220685A (es) 2023-03-28
KR20230033712A (ko) 2023-03-08
CN116209662A (zh) 2023-06-02

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