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AR076794A1 - Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen - Google Patents

Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen

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Publication number
AR076794A1
AR076794A1 ARP100101791A ARP100101791A AR076794A1 AR 076794 A1 AR076794 A1 AR 076794A1 AR P100101791 A ARP100101791 A AR P100101791A AR P100101791 A ARP100101791 A AR P100101791A AR 076794 A1 AR076794 A1 AR 076794A1
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AR
Argentina
Prior art keywords
alkyl
heteroaryl
independently selected
alkylamino
heterocycloalkyl
Prior art date
Application number
ARP100101791A
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English (en)
Inventor
Argyrios G Arvanitis
James D Rodgers
Lixin Shao
Wenyu Zhu
Joseph Glenn
Stacey Shepard
Haisheng Wang
Louis Storace
Beverly Folmer
Original Assignee
Incyte Corp
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42543342&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR076794(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of AR076794A1 publication Critical patent/AR076794A1/es

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    • 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
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • C07D491/02—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 two hetero rings
    • C07D491/04—Ortho-condensed systems
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Abstract

Inhibidores de JAK, tal como inhibidores selectivos de JAK1, utiles en el tratamiento de enfermedades asociadas con JAK, entre las que se incluyen, por ejemplo, los trastornos inflamatorios y autoinmunes y también el cáncer. Reivindicacion 1: Un compuesto caracterizado porque es de formula (1) o una sal farmacéuticamente aceptable o N-oxido del mismo; donde X es ciano o halogeno; Y es CH o N; Z es hidrogeno, alquilo C1-4, alquilo C1-4 fluorado, o fluor; Ar es arilo C6-14, heteroarilo C1-14, cicloalquilarilo C7-14 fusionado, heterocicloalquilarilo C6-14 fusionado, cicloalquilheteroarilo C2-14 fusionado, o heterocicloalquilheteroarilo C2-14 fusionado, cada uno de los cuales está opcionalmente sustituido con 1, 2, 3, 4, 5 o 6 grupos R1 seleccionados en forma independiente; cada R1 se selecciona en forma independiente entre halogeno, ciano, nitro, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-13, cicloalquil C3-14-alquilo C1-4, heterocicloalquilo C2-14, heterocicloalquil C2-14-alquilo C1-4, arilo C6-14, aril C6-14-alquilo C1-4, heteroarilo C1-3, heteroaril C1-3-alquilo C1-4, -ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)NReRf, -C(=O)Rb, -C(=O)ORb, -C(=O)NReRf, -OC(=O)Rb, -OC(=O)NReRf, -NReRf, -NRcC(=O)Rd, -NRcC(=O)ORd, -NRcC(=O)NRd, -NRcS(=O)2Rd, y -NRbS(=O)2NReRf; donde dicho alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, y alquinilo C2-6 están cada uno opcionalmente sustituido con 1, 2, 3 o 4 grupos R1a seleccionados en forma independiente; y donde dicho cicloalquilo C3-14, cicloalquil C3-14-alquilo C1-4, heterocicloalquilo C2-14, heterocicloalquil C2-14-alquilo C1-4, arilo C6-14, aril C6-14-alquilo C1-4, heteroarilo C1-3, y heteroaril C1-3-alquilo C1-4 están cada uno opcionalmente sustituido con 1, 2, 3 o 4 grupos R2a seleccionados en forma independiente; cada R1a se selecciona en forma independiente entre halogeno, ciano, nitro, hidroxilo, alcoxi C1-4, haloalcoxi C1-4, alquiltio C1-4, alquilsulfinilo C1-4, alquilsulfonilo C1-4, amino, alquilamino C1-4, di-alquilamino C1-4, alquilcarbonilo C1-4, carboxi, alcoxicarbonilo C1-4, alquilcarbonilamino C1-4, di-alquilcarbonilamino C1-4, alcoxicarbonilamino C1-4, alcoxicarbonil C1-4-(alquil C1-4)amino, carbamilo, alquilcarbamilo C1-4, y di-aIquilcarbamilo C1-4; cada R2a se selecciona en forma independiente entre halogeno, ciano, nitro, hidroxilo, alquilo C1-4, haloalquilo C1-4, alquenilo C2-4, alquinilo C2-4, alcoxi C1-4, haloalcoxi C1-4, alquiltio C1-4, alquilsulfinilo C1-4, alquilsulfonilo C1-4, amino, alquilamino C1-4, di-alquilamino C1-4, alquilcarbonilo C1-4, carboxi, alcoxicarbonilo C1-4, alquilcarbonilamino C1-4, di-alquilcarbonilamino C1-4, alcoxicarbonilamino C1-4, alcoxicarbonil C1-4-(alquil C1-4)amino, carbamilo, alquilcarbamilo C1-4, y di-alquilcarbamilo C1-4; cada Ra, Rb, Rc, Rd, Re, y Rf se selecciona en forma independiente entre H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquilo C2-7, heterocicloalquil C2-7-alquilo C1-4, fenilo, fenil-alquilo C1-4, heteroarilo C1-7, y heteroaril C1-7-alquilo C1-4; donde dicho alquilo C1-6, haloalquilo C1-6, alquenilo C2-6 y alquinilo C2-6 están cada uno opcionalmente sustituido con 1, 2, 3 o 4 grupos Rx seleccionados en forma independiente; y donde dicho cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-4, heterocicloalquilo C2-7, heterocicloalquil C2-7-alquilo C1-4, fenilo, fenil-alquilo C1-4, heteroarilo C1-7, heteroaril C1-7-alquilo C1-4 están cada uno opcionalmente sustituido con 1, 2, 3 o 4 grupos Ry seleccionados en forma independiente; o cualquiera de Rc y Rd, junto con la unidad a la cual están unidos, pueden formar un anillo heterocicloalquilo de 3, 4, 5, 6 o 7 miembros, donde dicho anillo heterocicloalquilo está opcionalmente sustituido con 1, 2, 3 o 4 grupos seleccionados en forma independiente entre hidroxilo, alquilo C1-4, haloalquilo C1-4, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4, y di-alquilamino C1-4; o cualquiera de Re y Rf, junto con el átomo de nitrogeno al cual están unidos, pueden formar un anillo heteroarilo o heterocicloalquilo de 3, 4, 5, 6 o 7 miembros, donde dicho anillo heterocicloalquilo o heteroarilo está opcionalmente sustituido con 1, 2, 3 o 4 grupos seleccionados en forma independiente entre hidroxilo, alquilo C1-4, haloalquilo C1-4, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4, y di-alquilamino C1-4; cada Rx se selecciona en forma independiente entre hidroxilo, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4, y di-alquilamino C1-4; y cada Ry se selecciona en forma independiente entre hidroxilo, halogeno, ciano, nitro, alquilo C1-4, haloalquilo C1-4, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4, y di-alquilamino C1-4; siempre que no se exceda la valencia de cada átomo en las unidades opcionalmente sustituidas.
ARP100101791A 2009-05-22 2010-05-21 Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen AR076794A1 (es)

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Families Citing this family (112)

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Publication number Priority date Publication date Assignee Title
EP3838903B1 (en) 2005-12-13 2023-11-22 Incyte Holdings Corporation Pyrrolo[2,3-d]pyrimidine derivative as janus kinase inhibitor
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