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AR044116A1 - Compuestos derivados de 5,7 diamino pirazolo [4,3-d] pirimidinas, intermediarios para su preparacion, composiciones farmaceuticas que los contienen y su uso para la fabricacion de medicamentos. - Google Patents

Compuestos derivados de 5,7 diamino pirazolo [4,3-d] pirimidinas, intermediarios para su preparacion, composiciones farmaceuticas que los contienen y su uso para la fabricacion de medicamentos.

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Publication number
AR044116A1
AR044116A1 ARP040101440A ARP040101440A AR044116A1 AR 044116 A1 AR044116 A1 AR 044116A1 AR P040101440 A ARP040101440 A AR P040101440A AR P040101440 A ARP040101440 A AR P040101440A AR 044116 A1 AR044116 A1 AR 044116A1
Authority
AR
Argentina
Prior art keywords
ring
cycloalkyl
sulfur
nitrogen
oxygen
Prior art date
Application number
ARP040101440A
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English (en)
Original Assignee
Pfizer Ltd
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
Priority claimed from GBGB0327748.0A external-priority patent/GB0327748D0/en
Application filed by Pfizer Ltd filed Critical Pfizer Ltd
Publication of AR044116A1 publication Critical patent/AR044116A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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
    • C07D487/04—Ortho-condensed systems
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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
    • A61K31/495—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
    • A—HUMAN NECESSITIES
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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Abstract

La presente se refiere a lo compuestos de fórmula (1), derivados de 5,7-diaminopirazolo[4,3-d]pirimidinas, intermediarios utilizados en su preparación, composiciones farmacéuticas que los contienen como principio activo y su uso en la fabricación de medicamentos inhibidores de la fosfodiesterasa tipo 5 específicos del guanilato, monofosfato cíclico (cGMP) para el tratamiento de la hipertensión. Reivindicación 1: Un compuesto de fórmula (1), en la que: R1 es un grupo cíclico seleccionado entre RA, RB, RC y RD, cada uno de los cuales está opcionalmente sustituido con uno o más grupos R7; R2 es hidrógeno o alquilo C1-2; R3 y R4 son cada uno de ellos independientemente alquilo C1-8, alquenilo C2-8, alquinilo C2-8 o cicloalquilo C3-10, cada uno de los cuales está opcionalmente sustituido con uno o más grupos R8, o RE, que está opcionalmente sustituido con uno o más grupos R9, o hidrógeno; o -NR3R4 forma RF, que está opcionalmente sustituido con uno o más grupos R10; R5 es alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6 o cicloalquilo C3-7, cada uno de los cuales está opcionalmente sustituido con uno o más grupos seleccionados entre hidroxi, alcoxi C1-6, haloalcoxi C1-6, cicloalquilo C3-7 y cicloalcoxi C3-7, o hidrógeno; R6, que puede estar unido a N1 o N2, es R6A o hidrógeno; R6 es alquilo C1-6, haloalquilo C1-6, alquenilo C2-6 o alquinilo C2-6, cada uno de los cuales está opcionalmente sustituido con alcoxi C1-6, (cicloalquil C3-6)alcoxi(C1-6), haloalcoxi C1-6 o un grupo cíclico seleccionado entre RJ, RK, RL y RM, o R6A es RN, cicloalquilo C3-7 o halocicloalquilo C3-7, cada uno de los cuales está opcionalmente sustituido con alcoxi C1-6 o haloalcoxi C1-6; R7 es halo, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, halocicloalquilo C3-10, oxo, fenilo, OR12, OC(O)R12, NO2, NR12R13, NR12C(O)R13, NR12CO2R14, C(O)R12, CO2R12, CONR12R13 o CN; R8 es halo, fenilo. alcoxi C1-6 fenilo, OR12, OC(O)R12, NO2, NR12R13, NR12C(O)R13, NR12CO2R14, C(O)R12, CO2R12, CONR12R13, CN, cicloalquilo C3-6, RG o RH, los dos últimos de los cuales están opcionalmente sustituidos con uno o más grupos R9; R9 es alquilo C1-6, haloalquilo C1-6 o CO2R12; R10 es halo, cicloalquilo C3-10, halocicloalquilo C3-10, fenilo, OR12, OC(O)R12, NO2, NR12R13, NR12C(O)R13, NR12CO2R14, C(O)R12, CO2R13, CONR12R13, CN, oxo, alquilo C1-6 o haloalquilo C1-6, los dos últimos de los cuales están opcionalmente sustituidos con R11; R11 es OH, fenilo, NR12R13 o NR12CO2R14; R12 y R13 son cada uno de ellos independientemente hidrógeno, alquilo C1-6 o haloalquilo C1-6; R14 es alquilo C1-6 o haloalquilo C1-6; RA y RJ son cada uno de ellos independientemente un grupo cicloalquilo C3-10 o cicloalquenilo C3-10, cada uno de los cuales puede ser bien monocíclico o, cuando hay un número apropiado de átomos en el anillo, policíclico y que puede estar condensado a: a) un anillo aromático monocíclico seleccionado entre un anillo de benceno y un anillo heteroaromático de 5 ó 6 eslabones conteniendo hasta tres heteroátomos seleccionados entre nitrógeno, oxígeno y azufre; o b) un anillo heterocíclico de 5, 6 ó 7 eslabones conteniendo hasta tres heteroátomos seleccionados entre nitrógeno, oxígeno y azufre; Rb y RK son cada uno de ellos independientemente un grupo fenilo o naftilo, cada uno de los cuales se puede condensar a: a) un anillo cicloalquilo C5-7 o cicloalquenilo C5-7; b) un anillo heteroalicíclico de 5, 6 ó 7 eslabones conteniendo hasta tres heteroátomos seleccionados entre nitrógeno, oxígeno y azufre; o c) un anillo heteroaromático de 5 ó 6 eslabones conteniendo hasta tres heteroátomos seleccionados entre nitrógeno, oxígeno y azufre; RC, RL y RN son cada uno de ellos independientemente un sistema de anillo monocíclico o, cuando hay un número apropiado de átomos en el anillo, policíclico saturado o parcialmente insaturado conteniendo entre 3 y 10 átomos en el anillo, de los que al menos uno es un heteroátomo seleccionado entre nitrógeno, oxígeno y azufre, dicho anillo se puede condensar a un grupo cicloalquilo C5-7 o cicloalquenilo C5-7 o un anillo aromático monocíclico seleccionado entre un anillo de benceno y un anillo heteroaromático de 5 ó 6 eslabones conteniendo hasta tres heteroátomos seleccionados entre nitrógeno, oxígeno y azufre; RD y RM son cada uno de ellos independientemente un anillo heteroaromático de 5 ó 6 eslabones conteniendo hasta tres heteroátomos seleccionados independientemente ente nitrógeno, oxígeno y azufre, dicho anillo se puede además condensar a: a) un segundo anillo heteroaromático de 5 ó 6 eslabones conteniendo hasta tres heteroátomos seleccionados entre nitrógeno, oxígeno y azufre; b) un anillo cicloalquilo C5-7 o cicloalquenilo C5-7; c) un anillo heteroalicíclico de 5, 6 ó 7 eslabones conteniendo hasta tres heteroátomos seleccionados entre nitrógeno, oxígeno y azufre; o d) un anillo de benceno; RE, RF y RG son cada uno de ellos independientemente un sistema de anillo monocíclico o, cuando hay un número apropiado de átomos en el anillo, policíclico saturado conteniendo entre 3 y 10 átomos en el anillo, de los que al menos uno es un heteroátomo seleccionado entre nitrógeno, oxígeno y azufre; y RH es un anillo heteroaromático de 5 ó 6 eslabones conteniendo hasta tres heteroátomos seleccionados independientemente entre nitrógeno, oxígeno y azufre; un tautómero del mismo o una sal, solvato o polimorfo de dicho compuesto o tautómero farmacéuticamente aceptable.
ARP040101440A 2003-04-29 2004-04-28 Compuestos derivados de 5,7 diamino pirazolo [4,3-d] pirimidinas, intermediarios para su preparacion, composiciones farmaceuticas que los contienen y su uso para la fabricacion de medicamentos. AR044116A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0309780 2003-04-29
GBGB0327748.0A GB0327748D0 (en) 2003-11-28 2003-11-28 Novel pharmaceuticals

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AR044116A1 true AR044116A1 (es) 2005-08-24

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ARP040101440A AR044116A1 (es) 2003-04-29 2004-04-28 Compuestos derivados de 5,7 diamino pirazolo [4,3-d] pirimidinas, intermediarios para su preparacion, composiciones farmaceuticas que los contienen y su uso para la fabricacion de medicamentos.

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US (2) US7262192B2 (es)
EP (1) EP1620437B1 (es)
JP (2) JP4015176B2 (es)
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AR (1) AR044116A1 (es)
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JP4015176B2 (ja) 2003-04-29 2007-11-28 ファイザー・インク 高血圧症の治療に有用な５，７−ジアミノピラゾロ４，３−ジピリミジン類
GB0322552D0 (en) 2003-09-26 2003-10-29 Astrazeneca Uk Ltd Therapeutic treatment
US7572799B2 (en) 2003-11-24 2009-08-11 Pfizer Inc Pyrazolo[4,3-d]pyrimidines as Phosphodiesterase Inhibitors
GB0327319D0 (en) * 2003-11-24 2003-12-24 Pfizer Ltd Novel pharmaceuticals
GB0327323D0 (en) * 2003-11-24 2003-12-31 Pfizer Ltd Novel pharmaceuticals
EP1742950B1 (en) 2004-04-07 2008-12-17 Pfizer Limited Pyrazolo[4,3-d] pyrimidines
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