AR072279A1 - Derivados de isoquinolina e isoquinolinona bi- y policiclicos sustituidos, uso del compuesto para producir un medicamento, y un medicamento en base al compuesto - Google Patents
Derivados de isoquinolina e isoquinolinona bi- y policiclicos sustituidos, uso del compuesto para producir un medicamento, y un medicamento en base al compuestoInfo
- Publication number
- AR072279A1 AR072279A1 ARP090102283A ARP090102283A AR072279A1 AR 072279 A1 AR072279 A1 AR 072279A1 AR P090102283 A ARP090102283 A AR P090102283A AR P090102283 A ARP090102283 A AR P090102283A AR 072279 A1 AR072279 A1 AR 072279A1
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- Prior art keywords
- alkyl
- alkylene
- aryl
- heterocycloalkyl
- cycloalkyl
- Prior art date
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- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000002131 composite material Substances 0.000 title 1
- 229940079593 drug Drugs 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical class C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 title 1
- 229940126601 medicinal product Drugs 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 52
- 125000002947 alkylene group Chemical group 0.000 abstract 22
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 15
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 11
- 229910052736 halogen Inorganic materials 0.000 abstract 10
- 150000002367 halogens Chemical class 0.000 abstract 10
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 8
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 5
- 125000004432 carbon atom Chemical group C* 0.000 abstract 5
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 4
- ORILYTVJVMAKLC-UHFFFAOYSA-N adamantane Chemical compound C1C(C2)CC3CC1CC2C3 ORILYTVJVMAKLC-UHFFFAOYSA-N 0.000 abstract 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 4
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 150000001721 carbon Chemical group 0.000 abstract 2
- 125000004122 cyclic group Chemical group 0.000 abstract 2
- 102000000568 rho-Associated Kinases Human genes 0.000 abstract 2
- 108010041788 rho-Associated Kinases Proteins 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- -1 C (O) R ' Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 206010030043 Ocular hypertension Diseases 0.000 abstract 1
- 229910018828 PO3H2 Inorganic materials 0.000 abstract 1
- 229910006069 SO3H Inorganic materials 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 abstract 1
- 230000001363 autoimmune Effects 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 208000029078 coronary artery disease Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 208000017169 kidney disease Diseases 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 230000026731 phosphorylation Effects 0.000 abstract 1
- 238000006366 phosphorylation reaction Methods 0.000 abstract 1
- 230000002685 pulmonary effect Effects 0.000 abstract 1
- 208000002815 pulmonary hypertension Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 abstract 1
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- C07D217/24—Oxygen atoms
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Abstract
Estos compuestos son utiles para el tratamiento y/o prevencion de enfermedades asociadas con Rho-quinasa y/o la fosforilacion mediada por Rho-quinasa, tales como enfermedades cardiovasculares, hipertension pulmonar y ocular, enfermedad coronaria, nefropatías, degeneracion neuronal, COPD y enfermedades autoinmunes. Reivindicacion 1: Un compuesto de la formula (1) en donde R1 es H, OH o NH2; R3 es H, halogeno, CN, alquilo C1-6, OH, NH2 o NHR'; R4 es H, halogeno, hidroxi, CN, alquilo C1-6, R' o alquilen C1-6-R'; R5 es H, halogeno, CN, alquilo C1-6, o R'; R7 es H, halogeno, CN, alquilo C1-6, O-alquilo C1-6, R' o SO2-NH2; R8 es H, halogeno o alquilo C1-6; R6 es un alquileno C1-4 unido al anillo de cicloalquilo, en el que el alquileno C1-4 forma un segundo enlace a un átomo de carbono diferente del anillo de cicloalquilo para formar un sistema de anillo bicíclico, en donde en el sistema de anillo bicíclico uno o dos átomos de carbono están reemplazados por un grupo independientemente seleccionado de O, N-R13, S, SO o SO2 o, si m y s son 2, m es 3 y s es 1, o m es 4 y s es 0, R6 es CH2-CH-(CH2)2, el cual está unido con un CH2 al anillo de cicloalquilo y los otros dos CH2 están unidos a diferentes átomos de carbono del anillo de cicloalquilo, y, si m es 3 y s es 3, R6 son dos grupos metileno unidos a diferentes átomos de carbono del anillo de cicloalquilo, en donde los grupos metileno del grupo CH2-CH-(CH2)2 están unidos a átomos de carbono del anillo de cicloalquilo y forman un sistema de adamantano de la formula (2) en donde L puede estar unido a cualquier átomo de carbono secundario o terciario, o R6, junto con R11 y el átomo de N forman un heterocicloalquilo C3-8 que está conectado en forma de un sistema de anillo espirocíclico para formar un residuo de la formula (3) en donde el sistema de anillo bicíclico o el sistema de adamantano o el sistema de anillo que contiene heterocicloalquilo C3-8 no está sustituido o está opcionalmente sustituido con R9; R9 es R', OH, halogeno, alquilo C1-6, O-alquilo C1-6, alquileno C1-6-R', alquenilo C2-6, alquinilo C2-6, alquileno C1-6-O-R', alquileno C1-6-CH[R']2, alquileno C1-6-C(O)-R', alquileno C1-6-C(O)NH2, alquileno C1-6-C(O)NH-R', alquileno C1-6-C(O)NH-alquilo C1-6, alquileno C1-6-C(O)N[alquilo C1-6]2, alquileno C1-6-C(O)N[R']2, alquileno C1-6-C(O)O-alquilo C1-6, COOH, C(O)O-alquilo C1-6, C(O)OR', C(O)-alquilo C1-6, C(O)R', CONH2, C(O)-NH-alquenilo C2-6, C(O)-NH-alquinilo C2-6, C(O)NH-alquilo C1-6, C(O)NHR', C(O)-NH-alquileno C1-6-R', C(O)N[alquilo C1-6]R', C(O)N[alquilo C1-6]2, C(O)-alquileno C1-6-R', o C(O)O-alquileno C1-6-R'; R11 y R12 son, independientemente entre sí, H, R', alquilo C1-6; alquilen C1-6-R', alquilen C1-6-O-alquilo C1-6, alquilen C1-6-O-R', alquilen C1-6-CH[R']2, alquilen C1-6-C(O)-R', alquilen C1-6-C(O)NH2, alquilen C1-6-C(O)NH-R', alquilen C1-6-C(O)NH-alquilo C1-6, alquilen C1-6-C(O)N[alquilo C1-6]2, alquilen C1-6-C(O)N[R']2, alquilen C1-6-C(O)O-alquilo C1-6, C(O)O-alquilo C1-6, C(O)OR', C(O)-alquilo C1-6, C(O)R', C(O)NH-alquilo C1-6, C(O)NHR', C(O)N[alquilo C1-6]R', C(O)N[alquilo C1-6]2, C(O)-alquilen C1-6-R', C(O)O-alquilen C1-6-R'; o R11 y R12, junto con el átomo de N al que están unidos, forman un grupo heterocicloalquilo C3-8; R13 es H o alquilo C1-6; n es 0, 1, 2, 3 o 4; m es 1, 2, 3 o 4; s es 0, 1, 2 o 3; L es O(CH2)p, S(CH2)p, S(O)(CH2)p, SO2(CH2)p, NH(CH2)p, N-alquil C1-6-(CH2)p, N-cicloalquil C3-6-(CH2)p; o N[alquileno C1-3-R']-(CH2)p; p es 0, 1, 2, 3 o 4; R' es cicloalquilo C3-8, heteroarilo C5-10, heterocicloalquilo C3-8, arilo C6-10; en donde en los restos R3 a R13 alquilo o alquileno está no sustituido o está opcionalmente sustituido una o más veces con OH, OCH3, C(O)OH, C(O)OCH3, NH2, NHCH3, N(CH3)2, C(O)NH2, C(O)NHCH3 o C(O)N(CH3)2; en donde en los restos R3 a R13 cicloalquilo o heterocicloalquilo está no sustituido o está opcionalmente sustituido una o más veces con alquilo C1-6, halogeno, OH, OCH3, C(O)OH, C(O)OCH3, NH2, NHCH3, N(CH3)2, C(O)NH2, C(O)NHCH3 o C(O)N(CH3)2, en donde en los restos R3 a R13 alquilo o alquileno no está sustituido o está opcionalmente sustituido una o más veces con halogeno; en donde en los restos R3 a R13 arilo C6-10 y heteroarilo C5-10 están no sustituidos o están opcionalmente sustituidos, una o más veces, con un grupo independientemente seleccionado de halogeno, OH, NO2, N3, CN, C(O)-alquilo C1-6, C(O)-arilo C6-10, C(O)OH, C(O)Oalquilo C1-6, C(O)NH2, C(O)NHalquilo C1-6, C(O)N[alquilo C1-6]2, cicloalquilo C3-8, alquilo C1-6, alquileno C1-6-NHalquilo C1-6, alquileno C1-6-N[alquilo C1-6]2, alquenilo C2-6, alquinilo C2-6, O-alquilo C1-6, O-C(O)-alquilo C1-6, PO3H2, SO3H, SO2-NH2, SO2NHalquilo C1-6, SO2N[alquilo C1-6]2, S-alquilo C1-6; SO-alquilo C1-6, SO2-alquilo C1-6, SO2-N=CH-N[alquilo C1-6]2, SF5, C(NH)(NH2), NH2, NH-alquilo C1-6, N[alquilo C1-6]2, NH-C(O)-alquilo C1-6, NH-C(O)O-alquilo C1-6, NH-SO2-alquilo C1-6, NH-SO2-arilo C6-10, NH-SO2-heteroarilo C5-10, NH-SO2-heterocicloalquilo C3-8, Nalquilo C1-6-C(O)-alquilo C1-6, Nalquilo C1-6-C(O)O-alquilo C1-6, Nalquilo C1-6-C(O)-NH-alquilo C1-6, arilo C6-10, alquileno C1-6-arilo C6-10, O-arilo C6-10, O-alquileno C1-6-arilo C6-10, heteroarilo C5-10, heterocicloalquilo C3-8, alquileno C1-6-heteroarilo C5-10, alquileno C1-6-heterocicloalquilo C3-8, O-alquileno C1-6-heteroarilo C5-10, O-alquileno C1-6-heterocicloalquilo C3-8, en donde dicho arilo C6-10, heteroarilo C5-10, heterocicloalquilo C3-8 o cicloalquilo C3-8 puede estar sustituido, una a tres veces, con un grupo, independientemente seleccionado de halogeno, OH, NO2, CN, O-alquilo C1-6, alquilo C1-6, NH2, NHalquilo C1-6, N[alquilo C1-6]2, SO2CH3, C(O)OH, C(O)O-alquilo C1-6, C(O)NH2, alquileno C1-6-O-alquilo C1-6, alquileno C1-6-O-arilo C6-10 u O-alquileno C1-6-arilo C6-10; o en los que arilo C6-10 está sustituido vecinalmente con un grupo O-alquilen C1-4-O, con lo que se forma, junto con los átomos de carbono a los que están unidos los átomos de oxígeno, un anillo de 5-8 miembros; y en donde los sustituyentes arilo de grupos arilo C6-10, heteroarilo C5-10, heterocicloalquilo C3-8 y cicloalquilo C3-8 pueden no estar adicionalmente sustituidos con un grupo que contiene arilo, heteroarilo, heterocicloalquilo o cicloalquilo; sus formas estereoisoméricas y/o tautoméricas y/o sus sales farmacéuticamente aceptables.
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ARP090102283A AR072279A1 (es) | 2008-06-24 | 2009-06-22 | Derivados de isoquinolina e isoquinolinona bi- y policiclicos sustituidos, uso del compuesto para producir un medicamento, y un medicamento en base al compuesto |
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EP (1) | EP2303845B1 (es) |
JP (1) | JP5715561B2 (es) |
KR (1) | KR101692211B1 (es) |
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AR (1) | AR072279A1 (es) |
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