AR037972A1 - Pirrolopirimidinas - Google Patents

Pirrolopirimidinas

Info

Publication number
AR037972A1
AR037972A1 ARP020105061A ARP020105061A AR037972A1 AR 037972 A1 AR037972 A1 AR 037972A1 AR P020105061 A ARP020105061 A AR P020105061A AR P020105061 A ARP020105061 A AR P020105061A AR 037972 A1 AR037972 A1 AR 037972A1
Authority
AR
Argentina
Prior art keywords
hal
replaced
groups
atoms
so2aa
Prior art date
Application number
ARP020105061A
Other languages
English (en)
Inventor
Eggenweiler Hans-Michael Dr
Wolf Michael Dr
Original Assignee
Merck Patent Gmbh
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
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR037972A1 publication Critical patent/AR037972A1/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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    • 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
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    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Abstract

Derivados de pirrolopirimidina que actúan como inhibidores de la fosfodiesterasa VII y pueden emplearse para el tratamiento de osteoporosis, tumores, caquexia, aterosclerosis, artritis reumatoidea, esclerosis múltiple, diabetes mellitus, procesos inflamatorios, alergias, asma, enfermedades autoinmunes, enfermedades del miocardio y SIDA. También se reivindican: proceso para preparar los compuestos, medicamento, uso para preparar medicamentos, combinación con antagonistas e inhibidores y kit. Reivindicación 1: Compuesto de la fórmula (1) caracterizado porque X es fenilo o Het, cada uno de los cuales está insustituido o monosustituido o polisustituido por R1 y/o R2, R1 y R2 son cada uno, en forma independiente entre sí, A, OH, OA, SA, SOA, SO2A, SO2NH2, SO2NHA, SO2AA', CN, NO2, NH2, NHA, NAA', NHCOA, NHCOOA, COOH, COOA, CONH2, CONHA, CONAA' o Hal, R1 y R2 son juntos, de modo alternativo, -OCH2O- u -OCH2CH2O-, R3 es A, OH, OA, SA, SOA, SO2A, SO2NH2, SO2NHA, SO2AA', CN, NO2, NH2, NHA, NHB, NAA', NHCOA, NHCOOA, NHCOB, NHCOOB, COOH, COOA, COOB, CONH2, CONHA, CONHB, CONAA' o Hal, R4, es alquilo o alquenilo ramificado o no ramificado que tiene hasta 10 átomos de carbono, que pueden estar sustituidos por 1 a 5 átomos de F y/o Cl y/o donde uno o mas grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NA, NHCO, NACO, NHCOO, o NACOO, o cicloalquilo o cicloalquenilo que tiene C3-7, donde uno o dos grupos CH2 pueden estar reemplazados por O, S, SO, SO2, SO2NH, SO2NA, NH, NHA, NHCONH, NACONH, NACONA, NHCO, NACO, NHCOO o NACOO, R5 es OH, OA, SA, SOA, SO2A, SO2NH2, SO2NHA, SO2AA', CN, NO2, NH2, NHA, NAA', NHCOA, NHCOOA, COOH, COOA, CONH2, CONHA, CONAA', o Hal, R6 es H, OH, OA, SA, SOA, SO2A, SO2NH2, SO2NHA, SO2AA', CN, NO2, NH2, NHA, NAA', NHCOA, NHCOOA, COOH, COOA, CONH2, CONHA, CONAA' o Hal, A y A' son cada uno, en forma independiente entre sí, alquilo o alquenilo ramificado o no ramificado que tiene hasta 10 átomos de carbono, que pueden estar sustituidos por 1 a 5 átomos de F y/o Cl y/o donde uno o mas grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NR7, NHCO, NR7CO, NHCOO o NR7COO, A y A' son juntos, de modo alternativo, alquileno que tiene C3-7, donde uno o dos grupos CH2 pueden estar reemplazados por CHR7, CHR7R8, O, S, SO, SO2, NH, NR7, NHCO, NR7CO, NHCOO o NR7COO, B es fenilo o Het, cada uno de los cuales está insustituido o monosustituido o polisustituido por R1 y/o R2, Het es un anillo heterocíclico aromático de 5 a 6 miembros que tiene 1-3 átomos de N, O y/o S esta insustituido, monosustituido, disustituido o trisustituido por A'', Hal o CF3, R7 y R8 son cada uno, en forma independiente entre sí, alquilo o alquenilo ramificado o no ramificado que tienen hasta 5 átomos de carbono, que pueden estar sustituidos por 1 a 5 átomos de F y/o Cl y/o donde uno o más grupos CH2 pueden estar reemplazados por O, S, SO, SO2, o NH, A'' es alquilo que tiene C1-6, y Hal es F, Cl, Br o I, y derivados, solvatos y estereoisómeros de los mismos de utilidad farmacéutica, incluyendo las mezclas de los mismos en todas las relaciones.
ARP020105061A 2001-12-24 2002-12-20 Pirrolopirimidinas AR037972A1 (es)

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DE10163991A DE10163991A1 (de) 2001-12-24 2001-12-24 Pyrrolo-pyrimidine

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KR (1) KR20040071252A (es)
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AR (1) AR037972A1 (es)
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AU (1) AU2002367090B2 (es)
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RU (1) RU2004122924A (es)
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HUP0402216A2 (hu) 2005-02-28
US20050059686A1 (en) 2005-03-17
JP2005520801A (ja) 2005-07-14
CA2471538C (en) 2011-03-22
MXPA04006235A (es) 2004-11-01
CN1608067A (zh) 2005-04-20
ATE411316T1 (de) 2008-10-15
ZA200405859B (en) 2005-05-17
BR0215308A (pt) 2004-12-21
DE50212917D1 (de) 2008-11-27
PL369728A1 (en) 2005-05-02
RU2004122924A (ru) 2005-05-27
KR20040071252A (ko) 2004-08-11
EP1458722B1 (de) 2008-10-15
WO2003055882A1 (de) 2003-07-10
AU2002367090A1 (en) 2003-07-15
US7498334B2 (en) 2009-03-03
CA2471538A1 (en) 2003-07-10
DE10163991A1 (de) 2003-07-03
AU2002367090B2 (en) 2008-11-13
ES2314132T3 (es) 2009-03-16

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