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
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AR
Argentina
Prior art keywords
alkyl
alkylene
aryl
group
het
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ARP080104560A
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English (en)
Inventor
Ralf Anderskewitz
Domnic Martyres
Thomas Fox
Horst Dollinger
Pascale Pouzet
Christoph Hoenke
Peter Nickolaus
Klaus Klinder
Rolf Goeggel
Dennis Fiegen
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Boehringer Ingelheim Int
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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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