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AR074814A1 - Pirimidinas sustituidas como antagonistas del receptor ccr2 y usos de las mismas en medicamentos. - Google Patents

Pirimidinas sustituidas como antagonistas del receptor ccr2 y usos de las mismas en medicamentos.

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Publication number
AR074814A1
AR074814A1 ARP090104997A ARP090104997A AR074814A1 AR 074814 A1 AR074814 A1 AR 074814A1 AR P090104997 A ARP090104997 A AR P090104997A AR P090104997 A ARP090104997 A AR P090104997A AR 074814 A1 AR074814 A1 AR 074814A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkylene
heterocyclyl
ring
halogen
Prior art date
Application number
ARP090104997A
Other languages
English (en)
Inventor
Heiner Ebel
Sara Frattini
Christoph Hoenke
Thomas Trieselmann
Silke Hobbie
Riccardo Giovannini
Stefan Scheuerer
Patrick Tielmann
Original Assignee
Boehringer Ingelheim Int
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42049604&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR074814(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 AR074814A1 publication Critical patent/AR074814A1/es

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    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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Abstract

Antagonistas novedosos para el CCR2 (receptor 2 de quimioquina CC) y a su uso para proporcionar medicamentos para tratar afecciones y enfermedades, en especial enfermedades pulmonares tales como asma y EPOC. Reivindicación 1: Compuestos caracterizados por estar de acuerdo con la fórmula (1), en la que R1 es -L1-R7, en la que L1 es un enlazador seleccionado entre un enlace o un grupo seleccionado entre -alquileno C1-2 y -alquenileno C1-2 que comprende opcionalmente uno o más grupos seleccionados entre -O-, -C(O)- y -NH- en la cadena y que está opcionalmente sustituido con un grupo seleccionado entre -OH, -NH2, -alquilo C1-3, O-alquilo C1-6 y -CN, en la que R7 es un anillo seleccionado entre -cicloalquilo C3-8, -heterociclilo C3-8, -arilo C5-10, y -heteroarilo C5-10, en la que el anillo R7 está opcionalmente sustituido con uno o más grupos seleccionados entre -CF3, -O-CF3, -CN y -halógeno, o en la que el anillo R7 está opcionalmente sustituido con uno o más grupos seleccionados entre -alquilo C1-6, -O-alquilo C1-6, -arilo C5-10, -heteroarilo C5-10, -cicloalquilo C3-8, -heterociclilo C3-8, -alquenilo C1-6 y -alquinilo C1-6, estando opcionalmente sustituido con uno o más grupos seleccionadas entre -OH, -NH2, -alquilo C1-3, -O-alquilo C1-6, -CN, -CF3, -OCF3, halógeno y =O, o en la que el anillo R7 está opcionalmente sustituido además bi-valentemente en dos átomos vecinos en el anillo, de tal forma que se forma un anillo anelado con uno o más grupos seleccionados entre -alquileno C1-6, -alquenileno C2-6 y -alquinileno C4-6, donde uno o dos centros de carbono pueden reemplazarse opcionalmente por 1 o 2 heteroátomos seleccionados entre N, O y S, estando el grupo bivalente opcionalmente sustituido con uno o más grupos seleccionados entre -OH, -NH2, alquilo C1-3, -O-alquilo C1-6, -CN, -CF3, -OCF3, halógeno y =O; en la que R2 se selecciona entre -H, -halógeno, -CN, -O-alquilo C1-4, -alquilo C1-4, -CH=CH2, -C:::CH, -CF3, -OCF3, -OCF2H y -OCFH2; en la que R3 se selecciona entre -H, -metilo, -etilo, -propilo, -i-propilo, -ciclopropilo, -OCH3 y -CN; en la que R4 y R5 se seleccionan independientemente entre un par de electrones, -H y un grupo seleccionado entre -alquilo C1-6, -NH2, -cicloalquilo C3-8, -heterociclilo C3-8, -arilo C5-10, -heteroarilo C5-10, y -C(O)-N(R8R8'), donde R8 y R8' se seleccionan independientemente entre -H y -alquilo C1-6, y en la que R4 y R5, si son distintos de un par de electrones o son -H, están opcionalmente sustituidos independientemente con uno o más grupos seleccionados entre -halógeno, -OH, -CF3, -CN, -alquilo C1-6, -O-alquilo C1-6, -O-cicloalquilo C3-8, -O-heterociclilo C3-8, -O-arilo C5-10, -O-heteroarilo C5-10, -alquileno C0-6-CN, -alquileno C0-4-alquilo C1-4, -alquileno C0-4-O-cicloalquilo C3-8, -alquileno C0-4-O-heterociclilo C3-8, -alquileno C0-4-O-arilo C6-10, -alquileno C0-4-O-heteroarilo C5-10, -alquileno C0-4-Q-alquil C0-4-N(R9R9'), -alquileno C0-4-N(R10)-Q-alquilo C1-4, -alquileno C0-4-N(R10)-Q-cicloalquilo C3-8, -alquileno C0-4-N(R10)-Q-heterociclilo C3-8, -alquileno C0-4-N(R10)-Q-arilo C5-10, -alquileno C0-4-N(R10)-Q-heteroarilo C5-10, -alquileno C0-4-Q-N(R11R11'), -alquileno C0-4-N(R12)-Q-N(R13R13'), -alquileno C0-4-R14, -alquileno C0-4-Q-alquilo C1-6, -alquileno C0-4-Q-cicloalquilo C3-8, -alquileno C0-4-Q-heterociclilo C3-8, -alquileno C0-4-Q-arilo C5-10, -alquileno C0-4-Q-heteroarilo C5-1o, -alquileno C0-4-O-Q-N(R15R15') y -alquileno C0-4-N(R16)-Q-O-(R17), en la que Q se selecciona entre -C(O)- y -SO2-, en la que R12 y R16 se seleccionan independientemente entre -H, -alquilo C1-6 y -cicloalquilo C3-6, en la que R9, R9' R10, R11, R11', R13, R13', R15 y R15' se seleccionan independientemente entre -H, -alquilo C1-6 y -cicloalquilo C3-6, o en la que R9 y R9', R11 y R11', R13 y R13', R15 y R15' juntos forman un grupo -alquileno C2-6, en la que R14 y R17 se seleccionan independientemente entre -H, -alquilo C1-6, -arilo C5-10, -heteroarilo C5-10, -cicloalquilo C3-8 y -heterociclilo C3-8, donde dicho -heterociclilo C3-8 comprende opcionalmente nitrógeno y/o -SO2- en el anillo, y en la que R14 y R17 están opcionalmente sustituidos con uno o más grupos seleccionados entre -OH, -OCH3, -CF3, -OCF3, -CN, -halógeno, -alquilo C1-4, =O y -SO2-alquilo C1-4, o en la que R4 y/o R5 son independientemente un grupo de la estructura -L2-R18, en la que L2 se seleccione entre -NH- y -N(alquilo C1-4)-, en la que R18 se seleccione entre -arilo C5-10, -heteroarilo C5-10, -cicloalquilo C3-8 y -heterociclilo C3-8, en la que R18 está opcionalmente sustituido con uno o más grupos seleccionados entre halógeno, -CF3, -OCF3, -CN, -OH, -O-alquilo C1-4, -alquilo C1-6, -NH-C(O)-alquilo C1-6, -N(alquil C1-4)-C(O)-alquilo C1-6, -C(O)-alquilo C1-6, -S(O)2-alquilo C1-6, -NH-S(O)2-alquilo C1-6, -N(alquil C1-4)-S(O)2-alquilo C1-6 y -C(O)-O-alquilo C1-6, y en la que R4, R5 y R18 están opcionalmente sustituidos además con espirocicloalquilo C3-8 o espiro-heterociclilo C3-8 de tal forma que junto con R4, R5 y/o R18 se forma un espirociclo, donde dicho espiro-heterociclilo C3-8 comprende opcionalmente uno o más grupos seleccionados entre nitrógeno, -C(O)-, -SO2- y -N(SO2-alquilo C1-4)- en el anillo, o en la que R4, R5 y R18 están opcionalmente sustituidos además bivalentemente con uno o más grupos que forman anillos espirocíclicos o anelados seleccionados entre -alquileno C1-6, -alquenileno C2-6 y -alquinileno C4-6, donde uno o dos centros de carbono pueden reemplazarse opcionalmente por uno o dos heteroátomos seleccionados entre N, O y S y que puede estar opcionalmente sustituido con uno o más grupos en uno átomo del anillo o en dos átomos vecinos en el anillo seleccionados entre -OH, -NH2, -alquilo C1-3, O-alquilo C1-6, -CN, -CF3, -OCF3 y halógeno; en la que R6 se selecciona entre -H, -alquilo C1-4, -OH, -O-alquilo C1-4, -halógeno, -CN, -CF3 y -OCF3: en la que A se selecciona entre un enlace sencillo, =CH-, -CH2-, -O-, -S- y -NH-; en la que n es 1, 2 o 3; en la que Z es C o N, así como en forma de sus sales de adición de ácidos con ácidos farmacológicamente aceptables.
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