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AR069076A1 - Piperazino- dihidrotienopirimidinas sustituidas en heterociclo - Google Patents

Piperazino- dihidrotienopirimidinas sustituidas en heterociclo

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Publication number
AR069076A1
AR069076A1 ARP080104561A ARP080104561A AR069076A1 AR 069076 A1 AR069076 A1 AR 069076A1 AR P080104561 A ARP080104561 A AR P080104561A AR P080104561 A ARP080104561 A AR P080104561A AR 069076 A1 AR069076 A1 AR 069076A1
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AR
Argentina
Prior art keywords
alkylene
aryl
alkyl
group
eventually
Prior art date
Application number
ARP080104561A
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English (en)
Inventor
Ralf Anderskewitz
Horst Dollinger
Thomas Fox
Domnic Martyres
Pascale Pouzet
Dennis Fiegen
Peter Nickolaus
Klaus Klinder
Rolf Goeggel
Christoph Hoenke
Original Assignee
Boehringer Ingelheim Int
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Publication date
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR069076A1 publication Critical patent/AR069076A1/es

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    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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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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Abstract

Compuestos, así como composiciones farmacéuticas que los contienen. Estos dihidrotienopirimidinsulfoxidos son apropiados para el tratamiento de trastornos o enfermedades gastrointestinales o de vías respiratorias, enfermedades inflamatorias de las articulaciones, la piel o los ojos, enfermedades del sistema nervioso periférico o central o enfermedades cancerosas. Reivindicacion 1: Compuestos caracterizados porque tienen la formula (1) en donde X es SO, o SO2; R1 es H, alquilo C1-6; R2 es H o un radical seleccionado del grupo consistente en alquilo C1-10 y alquenilo C2-6, que eventualmente puede estar sustituido con uno o varios radicales seleccionados de halogeno y fluoroalquilo C1-3, o que eventualmente puede estar sustituido con uno o varios radicales seleccionados del grupo consistente en OR2.1, COOR2.1, CONR2.2R2.3, SR2.1, SO-R2.1, SO2-R2.1, arilo C6-10, un Het, un Hetarilo, un cicloalquilo C3-10 monocíclico o bicíclico, CH2-NR2.2R2.3 y NR2.2R2.3, los cuales a su vez eventualmente pueden estar sustituidos con uno o varios radicales seleccionados del grupo consistente en OH, halogeno, OR2.1, oxo, CF3, CHF2, CH2F, alquilo C1-6, alcanol C1-6, arilo C6-10, COOR2.1, CH2NR2.2R2.3 y NR2.2R2.3, en donde R2.1 es H o un radical seleccionado del grupo consistente en alquilo C1-6, alcanol C1-6, haloalquilo C1-3, cicloalquilo C3-10 monocíclico o bicíclico, aril C6-10-alquileno C1-6, Hetaril-alquileno C1-6 monocíclico o bicíclico, Het-alquileno C1-6, cicloalquil C3-10-alquileno C1-6, un arilo C6-10 monocíclico o bicíclico, un Hetarilo y un Het, que eventualmente pueden estar sustituidos con uno o varios radicales seleccionados del grupo consistente en OH, O-(alquilo C1-3), halogeno, alquilo C1-6 y arilo C6-10, en donde R2.2 y R2.3, de manera independiente entre sí, son H o un radical seleccionado del grupo consistente en alquilo C1-6, cicloalquilo C3-10 monocíclico o bicíclico, aril C6-10-alquileno C1-6,, Hetaril-alquileno C1-6, arilo C6-10 monocíclico o bicíclico, Het, Hetarilo, CO-NH2, CO-NHCH3, CO-N(CH3)2, SO2-(alquilo C1-2), CO-R2.1 y COOR2.1, que eventualmente pueden estar sustituidos con uno o varios radicales seleccionados del grupo consistente en OH, halogeno, alquilo C1-6, arilo C6-10 y COOR2.1, en donde Het es un heterociclo de tres a once miembros, monocíclico o bicíclico, saturado o parcialmente saturado, eventualmente condensado o eventualmente puenteado, que contiene 1, 2, 3 o 4 heteroátomos seleccionados, de manera independiente entre sí, del grupo consistente en N, S u O, y en donde Hetarilo es un heteroarilo de cinco a once miembros, monocíclico o bicíclico, eventualmente condensado, que contiene 1, 2, 3 o 4 heteroátomos seleccionados, de manera independiente entre sí, del grupo consistente en N, S u O, y en donde cicloalquilo puede estar saturado o parcialmente saturado, o bien R2 significa un cicloalquilo C3-10 monocíclico o policíclico, que eventualmente puede estar puenteado una vez o varias veces a través de grupos alquilo C1-3 y que eventualmente puede estar sustituido con un radical seleccionado del grupo consistente en alcanol C1-6 ramificado o sin ramificar, fluoroalquilo C1-3, alquilen C1-3-OR2.1, OR2.1, COOR2.1, SO2-NR2.2R2.3, Het, arilo C6-10, alquilo C1-6, aril C6-10-alquileno C1-6, Hetaril-alquileno C1-6, cicloalquilo C3-10 monocíclico o bicíclico y NR2.2R2.3, que eventualmente pueden estar sustituidos con uno o varios radicales seleccionados del grupo consistente en OH, OR2.1, oxo halogeno, CF3, CHF2, CH2F, alquilo C1-6, arilo C6-10 y NR2.2R2.3, o bien R2 significa un arilo C6-10 monocíclico o policíclico, que eventualmente puede estar sustituido con OH, SH o halogeno o con uno o varios radicales seleccionados del grupo consistente en OR2.1, COOR2.1, NR2.2R2.3, CH2-NR2.2R2.3, cicloalquilo C3-10, Het, alquilo C1-6, fluoroalquilo C1-3, aril C6-10-alquileno C1-6, Het-alquileno C1-6, Hetaril-alquileno C1-6, arilo C6-10, SO2-CH3, SO2-CH2CH3 y SO2-NR2.2R2.3, que a su vez pueden estar sustituidos con uno o varios radicales seleccionados del grupo consistente en OH, OR2.1, CF3, CHF2, CH2F, oxo, halogeno, CF3, CHF2, CH2F, alquilo C1-6, arilo C6-10 y NR2.2R2.3, o bien R2 es un radical seleccionado de un grupo consistente en Het y Hetarilo, que .eventualmente. puede estar sustituido con uno o varios radicales seleccionados del grupo de halogeno, OH, oxo, CF3, CHF2 y CH2F, o con uno o varios radicales seleccionados del grupo de OR2.1, alquilen C1-3-OR2.1, SR2.1, SOR2.1 y SO2R2.1, COOR2.1, COR2.1, alcanol C1-6, cicloalquilo C3-10, arilo C6-10, alquilo C1-6, aril C6-10-alquileno C1-6, Hetaril-alquileno C1-6, Het, Hetarilo, alquilen C1-3-OR2.1 y NR2.2R2.3, que eventualmente pueden. estar, sustituidos a su vez con uno o varios radicales seleccionados del grupo consistente en OH, OR2.1, oxo, halogeno, CF3, CHF2, CH2F, alquilo C1-6, arilo C6-10 y NR2.2R2.3, o en donde NR1R2 significan conjuntamente un anillo heterocíclico de cuatro a siete miembros, que eventualmente puede estar puenteado, que contiene 1, 2 o 3 heteroátomos seleccionados del grupo consistente en N, O y S, y que eventualmente puede estar sustituido con uno o varios radicales seleccionados del grupo consistente en OH, OR2.1, alquilen C1-3-OR2.1, oxo, halogeno, alquilo C1-6, arilo C6-10, COOR2.1, CH2-NR2.2-COO-R2.1, ÇH2-NR2.2-CO-R2.1, CH2-NR2.2-CO-CH2-NR2.2R2.3, CH2-NR2.2SO2-alquilo C1-3, CH2-NR2.2-SO2-NR2.2R2.3, CH2-NR2.2-CO-NR2.2R2.3, CO-NR2.2R2.3, CH2-NR2.2R2.3 y NR2.2R2.3, y en donde R3 es un radical seleccionado del grupo consistente en un Het y un Hetarilo, que eventualmente puede estar sustituido con uno o varios radicales seleccionados del grupo consistente en halogeno, fluoroalquilo C1-3, CN, OH, oxo, alquilo C1-6, -O-R2.1, -COOR2.1, SOR2.1, SO2R2.1, arilo C6-10, alquilen C1-3-arilo C6-10, alquilen C1-3-NR2.2R2.3, -NR2.2R2.3, un cicloalquilo C3-10, un alquilen C1-3-cicloalquilo C3-10, un Het, un Hetarilo, alquilen C1-3-Hetarilo, y alquilen C1-3-Het, que a su vez pueden estar eventualmente sustituidos con uno o varios radicales seleccionados del grupo de OH, halogeno, fluoroalquilo C1-3, alquilo C1-6, arilo. C6-10, -COO(alquilo C1-3) y O-(alquilo C1-3); y sales farmacologicamente tolerables de los mismos.
ARP080104561A 2007-10-19 2008-10-17 Piperazino- dihidrotienopirimidinas sustituidas en heterociclo AR069076A1 (es)

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EP2205609B1 (de) 2007-10-19 2017-03-29 Boehringer Ingelheim International GmbH Heterocyclus-substituierte piperazino-dihydrothienopyrimidine
US8486948B2 (en) 2007-10-19 2013-07-16 Boehringer Ingelheim International Gmbh Piperazinodihydrothienopyrimidine derivatives
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US8609672B2 (en) 2010-08-27 2013-12-17 University Of The Pacific Piperazinylpyrimidine analogues as protein kinase inhibitors
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