AR087355A1 - Derivados de piridin-2(1h)-ona como inhibidores de jak - Google Patents
Derivados de piridin-2(1h)-ona como inhibidores de jakInfo
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- AR087355A1 AR087355A1 ARP120102737A ARP120102737A AR087355A1 AR 087355 A1 AR087355 A1 AR 087355A1 AR P120102737 A ARP120102737 A AR P120102737A AR P120102737 A ARP120102737 A AR P120102737A AR 087355 A1 AR087355 A1 AR 087355A1
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Abstract
Se describen un procedimiento para su preparación, composiciones farmacéuticas que los comprenden y su uso en terapia como inhibidores de quinasas Janus (JAK).Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable, o solvato, o N-óxido, o estereoisómero o derivado deuterado del mismo, en donde: m es 0, 1, 2 ó 3; cada uno de X e Y independientemente representa un átomo de nitrógeno o un grupo -CR6, en donde al menos uno de X e Y representa un grupo -CR6; cada uno de A y B representa independientemente un átomo de nitrógeno o un grupo -CR7, en donde al menos uno de A y B representa un grupo -CR7; D representa un átomo de nitrógeno o un grupo -CR5, en donde cuando uno de A y B representa un átomo de nitrógeno, D representa un grupo -CR5; W representa un grupo enlazador seleccionado de un grupo -NR8-, un grupo -(CR9R10)-, -O- o -S-; R1 representa un átomo de hidrógeno, un grupo alquilo lineal o ramificado C1-6, un grupo haloalquilo C1-4, un grupo hidroxialquilo C1-4, un grupo alcoxi C1-4, un grupo cicloalquilo C3-10, un grupo cicloalquenilo C3-10, un grupo arilo monocíclico o bicíclico C6-14, un grupo heteroarilo de 5 a 14 miembros que contiene al menos un heteroátomo seleccionado de O, S y N, o un grupo heterocíclico de 5 a 14 miembros que contiene al menos un heteroátomo seleccionado de O, S y N, en donde los grupos cicloalquilo, cicloalquenilo, arilo, heteroarilo y heterociclilo están no sustituidos o sustituidos con uno o más sustituyentes seleccionados de un átomo de halógeno, un grupo ciano, un grupo alquilo lineal o ramificado C1-6, un grupo haloalquilo C1-4, un grupo hidroxialquilo C1-4, un grupo alquilsulfonilo C1-4, un grupo cicloalquilo C3-7, un grupo fenilo, un grupo piridilo, un grupo pirimidinilo o un grupo piperidilo; cada uno de R2 y R7 independientemente representa un átomo de hidrógeno, un átomo de halógeno, un grupo ciano, un grupo alquilo lineal o ramificado C1-6, un grupo haloalquilo C1-4, un grupo hidroxialquilo C1-4, un grupo cicloalquilo C3-10, un grupo cicloalquenilo C3-10, un grupo arilo monocíclico o bicíclico C6-14, un grupo heteroarilo de 5 a 14 miembros que contiene al menos un heteroátomo seleccionado de O, S y N, un grupo heterocíclico de 5 a 14 miembros que contiene al menos un heteroátomo seleccionado de O, S y N, o un grupo bicíclico que es un grupo monocíclico arilo C6-9 o heteroarilo de 5 a 9 miembros condensado con un grupo cicloalquilo o heterocíclico de 5 a 9 miembros, donde dicho grupo heteroarilo o heterocíclico contiene al menos un heteroátomo seleccionado de O, S y N, en donde los grupos cicloalquilo, cicloalquenilo, arilo, heteroarilo y heterociclilo, y el grupo bicíclico que es un grupo monocíclico arilo C6-9 o heteroarilo de 5 a 9 miembros condensado con un grupo cicloalquilo o heterocíclico de 5 a 9 miembros, están no sustituidos o sustituidos con uno o más sustituyentes seleccionados de un átomo de halógeno; un grupo ciano; un grupo alquilo lineal o ramificado C1-6 un grupo haloalquilo C1-4 un grupo hidroxialquilo C1-4 un grupo cicloalquilo C3-7 un grupo arilo monocíclico o bicíclico C6-14 un grupo heteroarilo de 5 a 14 miembros que contiene al menos un heteroátomo seleccionado de O, S y N; un grupo heterocíclico de 5 a 14 miembros que contiene al menos un heteroátomo seleccionado de O, S y N; un grupo -(CH2)1-3CN; un grupo -(CH2)nOR11; un grupo -NR11R12; un grupo -NR11C(O)-(CH2)n-R12; un grupo -NR11C(O)-(CH2)n-NR12R13; un grupo -C(O)-(CH2)1-3-CN; un grupo -C(O)-(CH2)n-R11; un grupo -(CH2)n’-C(O)-(CH2)n-NR11R12; un grupo -(CH2)n’-S(O)2(CH2)nR11; un grupo -(CH2)n’-S(O)2(CH2)nNR11R12; un grupo -NR11S(O)2(CH2)nR12 o un grupo -NR11S(O)2(CH2)nNR12R13; en donde cada n’ y n son 0, 1 ó 2; en donde dicho grupo arilo monocíclico o bicíclico C6-14 está no sustituido o sustituido adicionalmente con uno o más grupos carboxilo; cada uno de R3 y R4 independientemente representa un átomo de hidrógeno, un grupo haloalquilo C1-4, un grupo hidroxialquilo C1-4 o un grupo alquilo lineal o ramificado C1-6, donde dicho grupo alquilo está no sustituido o sustituido con uno o más sustituyentes seleccionados de un grupo alcoxi C1-4, un grupo ciano, un grupo cicloalquilo C3-7, un grupo fenilo, un grupo piridilo, un grupo pirimidinilo o un grupo piperidilo; cada uno de R5 y R6 independientemente representa un átomo de hidrógeno, un átomo de halógeno, un grupo ciano, un grupo alquilo lineal o ramificado C1-6, un grupo haloalquilo C1-4, un grupo hidroxialquilo C1-4, un grupo cicloalquilo C3-10, un grupo cicloalquenilo C3-10, un grupo arilo monocíclico o bicíclico C6-14, un grupo heteroarilo de 5 a 14 miembros que contiene al menos un heteroátomo seleccionado de O, S y N, o un grupo heterocíclico de 5 a 14 miembros que contiene al menos un heteroátomo seleccionado de O, S y N, un grupo -(CH2)nOR11; un grupo -NR11R12; un grupo -NR11C(O)-(CH2)n-R12; un grupo -NR11C(O)-(CH2)n-NR12R13; un grupo -C(O)-(CH2)1-3-CN; un grupo -C(O)-(CH2)n-R11; un grupo -C(O)-(CH2)n-NR11R12; un grupo -S(O)2(CH2)nR11; un grupo -S(O)2(CH2)nNR11R12; un grupo -NR11S(O)2(CH2)nR12 o un grupo -NR11S(O)2(CH2)nNR12R13; en donde cada n es 0, 1 o 2; en donde los grupos cicloalquilo, cicloalquenilo, arilo, heteroarilo, y heterociclilo están no sustituidos o sustituidos con uno o más sustituyentes seleccionados de un átomo de halógeno, un grupo ciano, un grupo alquilo lineal o ramificado C1-6, un grupo haloalquilo C1-4, un grupo hidroxialquilo C1-4, un grupo cicloalquilo C3-7, un grupo fenilo, un grupo piridilo, un grupo pirimidinilo, un grupo piperidilo, o un grupo -C(O)-(CH2)n-NR11R12; en donde n es 0, 1 ó 2; cada uno de R8, R9 y R10 independientemente representa un átomo de hidrógeno, un grupo haloalquilo C1-4, un grupo hidroxialquilo C1-4 o un grupo alquilo lineal o ramificado C1-6, donde dicho grupo alquilo está no sustituido o sustituido con uno o más sustituyentes seleccionados de un grupo alcoxi C1-4, un grupo ciano, un grupo cicloalquilo C3-7, un grupo fenilo, un grupo piridilo, un grupo pirimidinilo o un grupo piperidilo; R11, R12 y R13 representan independientemente cada uno un átomo de hidrógeno; un grupo haloalquilo C1-4 un grupo hidroxialquilo C1-4 un grupo heterocíclico de 5 a 9 miembros que contiene uno, dos o tres heteroátomos seleccionados de O, S y N, en donde el grupo heterocíclico está no sustituido o sustituido por uno o más sustituyentes seleccionados de un átomo de halógeno, un grupo hidroxilo, un grupo alquilo C1-4 lineal o ramificado, un grupo haloalquilo C1-4 o un grupo hidroxialquilo C1-4, o un grupo alquilo C1-6 lineal o ramificado, en donde el grupo alquilo está no sustituido o sustituido por uno o más sustituyentes seleccionados de un grupo alcoxi C1-4, un grupo ciano, un grupo cicloalquilo C3-7, un grupo fenilo, un grupo piridilo, un grupo pirimidinilo o un grupo piperidilo; en donde el compuesto de fórmula (1) es distinto que: a) 3-[[5-cloro-2-[[2,5-dimetil-4-(piperidin-4-il)fenil]amino]pirimidin-4-il]amino]piridin-2(1H)-ona; y b) 2-[7-[[5-cloro-4-[(2-oxo-1,2-dihidropiridin-3-il)amino]pirimidin-2-il]amino]-8-metoxi-1,2,4,5-tetrahidrobenzo[d]azepin-3-il]-N,N-dimetilacetamida.
Applications Claiming Priority (1)
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EP11382263A EP2554544A1 (en) | 2011-08-01 | 2011-08-01 | Pyridin-2(1h)-one derivatives as jak inhibitors |
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AR087355A1 true AR087355A1 (es) | 2014-03-19 |
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ARP120102737A AR087355A1 (es) | 2011-08-01 | 2012-07-27 | Derivados de piridin-2(1h)-ona como inhibidores de jak |
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US (1) | US9034311B2 (es) |
EP (2) | EP2554544A1 (es) |
JP (1) | JP2014521673A (es) |
KR (1) | KR20140044865A (es) |
CN (1) | CN103702991A (es) |
AR (1) | AR087355A1 (es) |
AU (1) | AU2012292276A1 (es) |
BR (1) | BR112014002245A2 (es) |
CA (1) | CA2839805A1 (es) |
CL (1) | CL2014000203A1 (es) |
CO (1) | CO6852079A2 (es) |
CR (1) | CR20140031A (es) |
EA (1) | EA201400182A1 (es) |
GT (1) | GT201400017A (es) |
MX (1) | MX2014000635A (es) |
PE (1) | PE20141409A1 (es) |
UY (1) | UY34212A (es) |
WO (1) | WO2013017461A1 (es) |
ZA (1) | ZA201309187B (es) |
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PE20170682A1 (es) | 2014-08-04 | 2017-06-15 | Nuevolution As | Derivados de pirimidina sustituidos con heterociclilo opcionalmente condensados utiles para el tratamiento de enfermedades inflamatorias, metabolicas, oncologicas y autoinmunitarias |
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WO2017211303A1 (en) | 2016-06-07 | 2017-12-14 | Jacobio Pharmaceuticals Co., Ltd. | Novel heterocyclic derivatives useful as shp2 inhibitors |
US10988466B2 (en) | 2017-03-23 | 2021-04-27 | Jacobio Pharmaceuticals Co., Ltd. | Heterocyclic derivatives useful as SHP2 inhibitors |
AU2018337138B2 (en) | 2017-09-21 | 2021-04-01 | Beijing Scitech-Mq Pharmaceuticals Limited | 2-substituted pyrazole amino-4-substituted amino-5-pyrimidine formamide compound, composition, and application thereof |
JP7167146B2 (ja) | 2017-11-06 | 2022-11-08 | ブリストル-マイヤーズ スクイブ カンパニー | Hpk1阻害剤として有用なイソフラノン化合物 |
CN110372664A (zh) * | 2018-04-13 | 2019-10-25 | 华东理工大学 | 选择性jak2抑制剂及其应用 |
EP3846793B1 (en) | 2018-09-07 | 2024-01-24 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
US11447479B2 (en) | 2019-12-20 | 2022-09-20 | Nuevolution A/S | Compounds active towards nuclear receptors |
WO2021198955A1 (en) | 2020-03-31 | 2021-10-07 | Nuevolution A/S | Compounds active towards nuclear receptors |
JP2023519605A (ja) | 2020-03-31 | 2023-05-11 | ヌエヴォリューション・アクティーゼルスカブ | 核内受容体に対して活性な化合物 |
KR102503968B1 (ko) | 2022-09-22 | 2023-02-28 | 이진석 | 실꼬리 절단장치 및 그를 구비하는 양말 편직기 |
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-
2011
- 2011-08-01 EP EP11382263A patent/EP2554544A1/en not_active Withdrawn
-
2012
- 2012-07-23 US US14/236,340 patent/US9034311B2/en not_active Expired - Fee Related
- 2012-07-23 WO PCT/EP2012/064426 patent/WO2013017461A1/en active Application Filing
- 2012-07-23 BR BR112014002245A patent/BR112014002245A2/pt not_active IP Right Cessation
- 2012-07-23 EA EA201400182A patent/EA201400182A1/ru unknown
- 2012-07-23 EP EP12737308.2A patent/EP2739616A1/en not_active Withdrawn
- 2012-07-23 KR KR1020147001602A patent/KR20140044865A/ko not_active Application Discontinuation
- 2012-07-23 CA CA2839805A patent/CA2839805A1/en not_active Abandoned
- 2012-07-23 MX MX2014000635A patent/MX2014000635A/es not_active Application Discontinuation
- 2012-07-23 JP JP2014523281A patent/JP2014521673A/ja active Pending
- 2012-07-23 AU AU2012292276A patent/AU2012292276A1/en not_active Abandoned
- 2012-07-23 PE PE2014000084A patent/PE20141409A1/es not_active Application Discontinuation
- 2012-07-23 UY UY0001034212A patent/UY34212A/es unknown
- 2012-07-23 CN CN201280036953.2A patent/CN103702991A/zh active Pending
- 2012-07-27 AR ARP120102737A patent/AR087355A1/es unknown
-
2013
- 2013-12-06 ZA ZA2013/09187A patent/ZA201309187B/en unknown
-
2014
- 2014-01-17 CO CO14008772A patent/CO6852079A2/es not_active Application Discontinuation
- 2014-01-22 CR CR20140031A patent/CR20140031A/es unknown
- 2014-01-27 CL CL2014000203A patent/CL2014000203A1/es unknown
- 2014-01-30 GT GT201400017A patent/GT201400017A/es unknown
Also Published As
Publication number | Publication date |
---|---|
PE20141409A1 (es) | 2014-10-01 |
EP2554544A1 (en) | 2013-02-06 |
NZ618904A (en) | 2015-06-26 |
MX2014000635A (es) | 2014-04-30 |
KR20140044865A (ko) | 2014-04-15 |
JP2014521673A (ja) | 2014-08-28 |
CA2839805A1 (en) | 2013-02-07 |
WO2013017461A1 (en) | 2013-02-07 |
US20140271543A1 (en) | 2014-09-18 |
CO6852079A2 (es) | 2014-01-30 |
EP2739616A1 (en) | 2014-06-11 |
UY34212A (es) | 2013-02-28 |
US9034311B2 (en) | 2015-05-19 |
BR112014002245A2 (pt) | 2017-03-07 |
CR20140031A (es) | 2014-05-13 |
CN103702991A (zh) | 2014-04-02 |
EA201400182A1 (ru) | 2014-06-30 |
CL2014000203A1 (es) | 2014-07-11 |
GT201400017A (es) | 2015-07-13 |
ZA201309187B (en) | 2014-08-27 |
AU2012292276A1 (en) | 2014-02-20 |
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