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NI201600170A - Pirazolopiridinas y pirazolopirimidinas - Google Patents

Pirazolopiridinas y pirazolopirimidinas

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Publication number
NI201600170A
NI201600170A NI201600170A NI201600170A NI201600170A NI 201600170 A NI201600170 A NI 201600170A NI 201600170 A NI201600170 A NI 201600170A NI 201600170 A NI201600170 A NI 201600170A NI 201600170 A NI201600170 A NI 201600170A
Authority
NI
Nicaragua
Prior art keywords
alkyl
cycloalkyl
phenyl
heteroaryl
halo
Prior art date
Application number
NI201600170A
Other languages
English (en)
Inventor
Wadsworth Coe Jotham
Martin Dehnhardt Christoph
Jones Peter
Anil Sabnis Yogesh
Walter Strohbach Joseph
Michel Wakenhut Florian
Alistair Whitlock Gavin
Original Assignee
Pfizer
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=53264695&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NI201600170(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer filed Critical Pfizer
Publication of NI201600170A publication Critical patent/NI201600170A/es

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    • 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
    • A61K31/505—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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    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
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Abstract

Un compuesto que tiene la estructura: (I), o una de sus sales farmacéuticamente aceptables o un solvato farmacéuticamente aceptable de dicho compuesto o sal farmacéuticamente aceptable, en donde A y A' son, de modo independiente, C o N, donde C puede no estar sustituido o puede estar sustituido con halo o alquilo C1-C6; R y R0 se seleccionan, de modo independiente, del grupo que consiste en H, alquilo C1-C6, hidroxi(alquilo C1-C6), fenil(alquilo C1-C6) y -(CH2)n-W, donde W es cicloalquilo C3-C8, fenilo, naftilo, heteroarilo de 5 ó 6 miembros o heterocíclico que contiene 1-3 átomos de N, S y/u O, -SO2-R', -NHSO2-R', -NR"SO2-R' y SR', donde R' y R'' son, de modo independiente, alquilo C1-C6 o cicloalquilo C3-C8, etc.; en donde cada uno de dichos alquilo, cicloalquilo, heterocíclico, fenilo, naftilo o heteroarilo puede no estar sustituido o puede estar sustituido con fenilo, heteroarilo, etc.; o R y R0 y el átomo de N al que están unidos forman un anillo heterocíclico monocíclico o bicíclico que puede no estar sustituido o puede estar sustituido con (a) halo, hidroxi, heteroarilo, alquilo C1-C6, alcoxi C1-C6, etc. o (b) -(CH2)n-W, donde W es cicloalquilo C3-C8, fenilo, etc.; R1 es H, halo o ciano; R2 y R2' son, de modo independiente, H, alquilo C1-C6, ciano, alcoxi C1-C6, alquil C1-C6-tio o cicloalquilo C3-C8, donde alquilo, alcoxi o cicloalquilo está opcionalmente sustituido con uno o varios átomos de flúor; X es un enlace, -CO-, -CONH-, -SO2-, -SONH- o -(CH2)m--; R3 es H, alquilo C1-C4, fenilo, naftilo, heteroarilo de 5 ó 6 miembros o heterocíclico que contiene 1-3 átomos de N, un heteroarilo de 5 miembros o heterocíclico, etc. o (c) 2 átomos de O o S y 0-2 átomos de N; en donde cada uno de dichos fenilo, naftilo, heteroarilo o heterocíclico está opcionalmente sustituido con alquilo, 1 sustituyente -Y-R4 y/o 1-4 sustituyentes seleccionados cada uno, de modo independiente, de R5; siempre que, cuando X es -CO- o -SO2-, R3 no sea H; Y es un enlace, -(CH2)m- u -O-; R4 es (a) H, alquilo C1-C6, cicloalquilo C3-C8, halo, oxo, -OR6, -NR7R8, -SR6, -SOR9, -SO2R9, -COR6, -OCOR6, -COOR6, -NR6COR6, -CONR7R8, etc.; (b) fenilo o naftilo, estando dicho fenilo y naftilo opcionalmente sustituidos con 1-5 sustituyentes seleccionados de alquilo C1-C6, cicloalquilo C3-C8, halo, ciano, -OR6, -NR7R8, etc.; o (c) un heteroarilo monocíclico saturado o parcialmente insaturado de 3 a 8 miembros, etc.; R6 es H, alquilo C1-C6 o cicloalquilo C3-C8, etc.; R7 y R8 son cada uno, de modo independiente, H, alquilo C1-C6 o cicloalquilo C3-C8 o se toman junto con el átomo de nitrógeno al que están unidos para formar un anillo heterocíclico saturado de 4, 5 ó 6 miembros que contiene 1-2 átomos de nitrógeno o 1 átomo de nitrógeno y 1 átomo de oxígeno, dicho alquilo C1-C6 está opcionalmente sustituido con cicloalquilo C3-C8, halo, etc. y estando dicho anillo heterocíclico opcionalmente sustituido con uno o varios grupos alquilo C1-C6 o cicloalquilo C3-C8; R9 es alquilo C1-C6 o cicloalquilo C3-C8; y, m y n son, de modo independiente, 0, 1, 2 ó 3. La invención también se refiere a sales farmacéuticamente aceptables de estos compuestos y solvatos farmacéuticamente aceptables; a composiciones que contienen tales compuestos; y a los usos de tales compuestos en el tratamiento de diversas enfermedades, en particular asma y EPOC.
NI201600170A 2014-05-14 2016-11-11 Pirazolopiridinas y pirazolopirimidinas NI201600170A (es)

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US (2) US9518052B2 (es)
EP (1) EP3143021B1 (es)
JP (1) JP6663857B2 (es)
KR (1) KR20170002623A (es)
CN (1) CN106459048A (es)
AP (1) AP2016009562A0 (es)
AR (1) AR100438A1 (es)
AU (1) AU2015260905A1 (es)
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