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AR069075A1 - Piperidino - dihidrotienopirimidinas sustituidas - Google Patents

Piperidino - dihidrotienopirimidinas sustituidas

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Publication number
AR069075A1
AR069075A1 ARP080104560A ARP080104560A AR069075A1 AR 069075 A1 AR069075 A1 AR 069075A1 AR P080104560 A ARP080104560 A AR P080104560A AR P080104560 A ARP080104560 A AR P080104560A AR 069075 A1 AR069075 A1 AR 069075A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkylene
aryl
group
het
Prior art date
Application number
ARP080104560A
Other languages
English (en)
Inventor
Ralf Anderskewitz
Domnic Martyres
Thomas Fox
Horst Dollinger
Pascale Pouzet
Christoph Hoenke
Peter Nickolaus
Klaus Klinder
Rolf Goeggel
Dennis Fiegen
Original Assignee
Boehringer Ingelheim Int
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39154006&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR069075(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR069075A1 publication Critical patent/AR069075A1/es

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Abstract

Composiciones farmacéuticas que contienen a estos compuestos y uso de las mismas para el tratamiento de trastornos o enfermedades de las vías respiratorias o gastrointestinales, enfermedades inflamatorias de las articulaciones, la piel o los ojos, enfermedades del sistema nervioso periférico o central o enfermedades cancerígenas. Reivindicacion 1: Compuestos caracterizados porque tienen la formula (1) en la cual 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 que consiste en OR2.1, COOR2.1, CONR2.2R2.3, SR2.1, SO-R2.1, SO2-R2.1, arilo C6-10, -Het, Hetarilo, un cicloalquilo C3-10 monocíclico o bicíclico, CH2-NR2.2R2.3 y NR2.2R2.3, que de nuevo, puede estar eventualmente sustituido 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, CH2-NR2.2R2.3 y NR2.2R2.3, en donde Het es un heterociclo de uno a once miembros, mono- o bi-cíclico, saturado o parcialmente saturado, eventualmente condensado o eventualmente puenteado, que contiene 1, 2, 3 o 4 heteroátomos elegidos, independientemente uno de otro, del grupo consistente en N, S u O, y en donde Hetarilo es un heteroarilo de cinco a diez miembros, mono- o bi-cíclico, eventualmente condensado, que contiene 1, 2, 3 o 4 heteroátomos seleccionados, independientemente uno de otro, del grupo consistente en N, S u O, y en donde cicloalquilo puede estar saturado o parcialmente saturado, 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 mono- o bi-cíclico, aril C6-10-alquileno C1-6, Hetaril-alquileno C1-6, Het-alquileno C1-6, cicloalquil C3-10-alquileno C1-6, un arilo C6-10 mono- o bi-cíclico, heteroarilo y un -Het, que eventualmente puede estar sustituido con uno 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 son, de modo independiente entre sí, H o un radical que está seleccionado del grupo compuesto por alquilo C1-6, cicloalquilo C3-10 mono- o bicíclico, aril C6-10alquileno C1-6, heteroaril-alquileno C1-6, arilo C6-10 mono o bicíclico, Het, Hetarilo, CO-NH2, CO-NHCH3, CO-N(CH3)2, SO2 (alquilo C1-2), CO-R2.1y COOR2.1, que. eventualmente puede estar sustituido con uno o más radicales seleccionados del grupo consistente en OH, halogeno, alquilo C1-6, arilo C6-10 y COOR2.1, o R2 es un cicloalquilo C3-10 mono o policíclico que eventualmente puede estar puenteado una o varias veces a través de grupos alquilo C1-3 y que eventualmente puede estar sustituido con un radical seleccionado del grupo compuesto por alcanol C1-6 ramificado o no ramificado, fluoroalquilo C1-3 , alquilen C1-3OR2.1, OR2.1, COOR2.1, -SO2-NR2.2R2.3, Het, -NH-COO(alquilo C1-6), -NH-CO-(alquilo C1-6), -NH-CO-O-(arilo C6-10), -NH-CO-(arilo C6-10), -NH-COO-Hetarilo, -NH-CO-Hetarilo, -NH-COO-(alquilen C1-3)-(arilo C6-10), -NH-CO-(alquilen C1-3)-(arilo C6-10), -N(alquil C1-3)-CO-(alquilo C1-6), -N(alquil C1-3)-CO-O-(arilo C6-10), -N(alquil C1-3)-CO-(arilo C6-10), -N(alquil C1-3)-CO-O-Hetarilo, -N(alquil C1-3)-CO-hetarilo, -N(alquil C1-3)-COO-(alquilen C1-3)-(arilo C6-10), -N(alquil C1-3)-CO-(alquilen C1-3)-(arilo C6-10), arilo C6-10, alquilo C1-6, aril C6-10-alquileno C1-6, Hetaril-alquileno C1-6, cicloalquilo C3-10 mono- o bicíclico y NR2.2 R2.3, que eventualmente puede estar sustituido con uno o varios radicales seleccionados del grupo compuesto por OH OR2.1, oxo halogeno, CF3, CHF2, CH2F, alquilo C1-6, arilo C6-10 y NR2.2R2.3, o R2 es un arilo C6-10 mono- o poli-cíclico, 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, CF3, CHF2, CH2F, 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 de nuevo, puede estar eventualmente sustituido 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 R2 es un radical seleccionado del grupo consistente en Het y Hetarilo, que eventualmente puede estar sustituido con uno o varios radicales seleccionados del grupo halogeno, OH, oxo, CF3, CHF2 y CH2F o con uno o varios radicales seleccionados del grupo OR2.1, alquilen C1-3-OR2.1, SR2.1,SO-R2.1, SO2-R2.1, COOR2.1, COR2.1, alcanol C1-6, cicloalquilo C3-10 mono- o bi-cíclico, 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, de nuevo, eventualmente, puede estar sustituido con uno o varios radicales seleccionados del grupo compuesto por OH, OR2.1 oxo, halogeno, CF3, CHF2, CH2F, alquilo C1-6,arilo C6-10, y NR2.2R2.3, o en donde NR1R2 son juntos un anillo heterocíclico C4-7 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-OR1, oxo, halogeno, alquilo C1-6, arilo C6-10, COOR2.1, CH2NR2.2-COO-R2.1, CH2NR2.2-CO-R2.1, CH2-NR2.2-CO-CH2-NR2.2R2.3, CH2-NR2.2-SO2-alquilo C1-3, CH2-NR2.2-SO2-NR2.2R2.3, CH2NR2.2-CO-NR2.2R2.3, CO-NR2.2R2.3, CH2-NR2.2R2.3 y NR2.2R2.3, y en donde R3 es un arilo C6-10, que, eventualmente, puede estar sustituido en posicion orto, para o meta con uno, dos o tres radicales seleccionados independientemente uno de otro, del grupo consistente en fluor cloro, bromo, hidroxi, CN, alquilo C1-6, fluoroalquilo C1-3, -alquilen C1-3-OR2.1, -alquilen C1-3-NR2.2R2.3, -NR2.2R2.3, O-R2.1, SO-R2.1, SO2R2.1, COOR2.1, CO-NH-(alquilen C1-6)-Hetarilo, -CO-NH-Hetarilo, -CO-N(CH3)-Het, -CO-N(CH3)-(alquilen C1-3)-Het, -CO-N(CH3)-(alquilen C1-3)-Hetarilo, -CO-N(cicloalquil C3-7)-Het, -CO-NR2.2R2.3, -CO-NH-(alquilen C1-6)-Het, NR2.2-CO-R2.1, arilo C6-10, aril C6-10-alquileno C1-2, Het-alquileno C1-2, -Het, -CO-Het, CO-N(CH3)-cicloalquilo C3-7, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-2, Hetaril-alquileno C1-2, y Hetarilo, en donde este radical puede estar eventualmente sustituido con uno o varios radicales seleccionados del grupo por consistente OH, halogeno, -fluoroalquilo C1-3. oxo, metilo y fenilo, o en donde R3 es un radical seleccionado del. grupo consistente en Het y 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, -alquilen C1-3-NR2.2R2.3, -NR2.2R2.3, SO-R2.1, SO2-R2.1, -OR2.1, COOR2.1, SO2-(CH3), SO2-(CH2-CH3), arilo C6-10, Het, cicloalquilo C3-7 y Hetarilo, que de nuevo, eventualmente puede estar sustituido con uno o varios radicales seleccionados del grupo consistente en OH, halogeno, -fluoroalquilo C1-3, alquilo C1-6, arilo C6-10, -COO(alquilo C1-3) y O-(alquilo C1-3), o en donde R3 es un radical seleccionado del grupo consistente en alquilo C1-6, -arilo C6-10, -alquilen C1-3 arilo C6-10, Hetarilo, y Het, que, eventualmente puede estar sustituido, en posicion orto para o meta con uno, dos o tres radicales seleccionados independientemente del grupo consistente en fluor, cloro, bromo, hidroxi, CN, alquilo C1-3, CO-(alquilo C1-6), -fluoroalquilo C1-3, -CO-(alquilo C1-5), -CO-(fluoroalquilo C1-3), CO-NH-alquilen C1-6-Hetarilo, -CO-N(alquil C1-3)-(alquilen C1-6)-Hetarilo, -CO-N(alquil C1-3)-Het, CO-N(cicloalquil C3-7)-Het, alquilen C1-3-OR2.1, alquilen C1-3-NR2.2R2.3, NR2.2R2.3, OR2.1, SO-R2.1, SO2R2.1, COOH, COO-(alquilo C1-4), -O-alquilen C1-3-N(alquilo C1-3)2, CO-NR2.2R2.3, NR2.2-CO-R2.1, arilo C6-10, aril C6-10-alquileno C1-2, Het-alquileno C1-2, -CO-Het, Het, CO-cicloalquilo C3-7, -CO-N(alquil C1-3)-cicloalquilo C3-7, cicloalquilo C3-7, cicloalquil C3-7-alquileno C1-2, Hetaril-alquileno C1-2, y Hetarilo, que de nuevo, eventualmente puede estar sustituido con 1, 2, 3 o 4 radicales seleccionados, independientemente uno de otro, del grupo consistente en F, CI, Br, metilo O-metilo, etilo, O-etilo, OH, oxo y CF3, y en-donde, R4 es H, CN, OH, CF3, CHF2, CH2F, F, metilo, etilo, -O-(alquilo C1-3), alquilen C1-3-OH, -COO(alquilo C1-3), -CO-Het, -(alquilen C1-2)-NH-SO2-(alquilo C1-2), -(alquilen C1-2)-N(alquil C1-3)-SO2-(alquilo C1-2), -(alquilen C1-2)-O-(alquilen C1-2)-arilo C6-10, -alquilen C1-3-O-alquilo C1-3, -(alquilen C1-2)-N(alquil C1-3)-CO-(alquilo C1-2), -NH-CO-(alquilen C1-3)-O-(alquilo C1-3), -alquilen C1-3-NH-CO-(alquilo C1-2), -alquilen C1-3-NH-CO-(alquilen C1-3)-N(alquilo C1-3)2, -O-(alquilen C1-2)-arilo C6-10, -alquilen C1-3-NH-CO-(alquilen C1-3)-O-(alquilo C1-3), -CO-(arilo C6-10), -(alquilen C1-2)-N(alquil C1-3)-CO-(alquilen C1-2)-O-(alquilo C1-3), en donde el arilo en los radicales anteriores puede estar sustituido eventualmente de nuevo con uno o varios otros radicales seleccionados del grupo F, Cl, Br, metilo, etilo, propilo, isopropilo, ciclopropilo, O-metilo, -O-etilo,-O-propilo, -O-isopropilo, -O-ciclopropilo, -OH y CF3, o en donde R3 y R4 en comun, forman un heterociclo mono- o bi-cíclico insaturado, saturado o parcialmente saturado, 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 halogeno, OH, oxo, fluoroalquilo C1-3, CN, alquilo C1-6, OR2.1, COOR2.1, SO-R2.1, SO2-R2.1, -alquilen C1-3-Nr2.2R2.3, -NR2.2R2.3, arilo C6-10, cicloalquilo C3-7, Het y Hetarilo; así como sales farmacologicamente compatibles de los mismos.
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