AR057082A1 - Derivados de ciclohexilaminisoquinolona - Google Patents

Derivados de ciclohexilaminisoquinolona

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Publication number
AR057082A1
AR057082A1 ARP060103200A ARP060103200A AR057082A1 AR 057082 A1 AR057082 A1 AR 057082A1 AR P060103200 A ARP060103200 A AR P060103200A AR P060103200 A ARP060103200 A AR P060103200A AR 057082 A1 AR057082 A1 AR 057082A1
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Argentina
Prior art keywords
alkylene
alkyl
heterocyclyl
aryl
cycloalkyl
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ARP060103200A
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English (en)
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Sanofi Aventis Deutschland
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Publication of AR057082A1 publication Critical patent/AR057082A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/24Oxygen atoms
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Engineering & Computer Science (AREA)
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  • Diabetes (AREA)
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Abstract

Son estos compuestos utiles para el tratamiento y/o prevencion de enfermedades asociadas con la Rho-quinasa y/o la fosforilacion mediada por la Rho-quinasa de la fosfatasa de la cadena ligera de miosina, se divulgan composiciones que contienen tales compuestos. Reivindicacion 1: Un compuesto de formula (1), o de formula (1), donde: R1 es H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, (alquilenoC1-6)0-1-cicloalquiloC3-8, (alquilenoC1-6)0-1-heterocicliloC5-10, alquilenoC1-6]0-1-ariloC6-10, C(O)-alquiloC1-6, C(O)-alqueniloC2-6, C(O)-alquiniloC2-6, C(O)-(alquilenoC1-6)0-1-cicloalquiloC3-8, C(O)-(alquilenoC1-6)0-1-heterocicliloC5-10, o C(O)-(alquilenoC1-6)0-1-ariloC6-10; R2 es H, alquilo C1-6, (alquilenoC1-C6)0-1-R1', (alquilenoC1-6)0-1- O-alquiloC1-6, (alquilenoC1-6)0-1-O-R', (alquilenoC1-6)0-1-NH2, (alquilenoC1-6]0-1-NH-alquiloC1-6, (alquilenoC1-6)0-1, -N(alquiloC1-6)2, (alquilenoC1-6)0-1-CH(R')2, (alquilenoC1-6)0-1-C(O)-R', (alquilenoC1-6)0-1-C(O)NH2, (alquilenoC1-6)0-1-C(O)NH- R', o (alquilenoC1-6)0-1-C(O)N(R')2; R3 es H, halogeno, CN, alquilo C1-6, alquilenoC1-6-R', OH, O-R'', NH2, NHR'', NR''R'' o NH-C(O)-R''; R4 es H, halogeno, hidroxi, CN, alquilo C1-6, cicloalquilo C3-8, alquilenoC1-6-R'; R5 es H, halogeno, CN, NO2, alquilo C1-6, alquenilo C2-6, R', alquilenoC1-6-ariloC6-10, alquenilenoC2-6-ariloC6-10, alquilenoC1-6-heterocicliloC5-10, NH2, NH-R', NH-SO2H, NH-SO2-alquiloC1-6, NH-SO2-R', NH-C(O)-alquiloC1-6, NH-C(O)-R', C(O)N(alquiloC1-6)2, C(O)OH o C(O)O- alquiloC1-6; R6 y R6' son independientemente entre sí H, R', alquilo C1-8, alquilenoC1-6-R', alquilenoC1-6-O-alquilo(C1-6, alquilenoC1-6-O-R', alquilenoC1-6-CH(R')2, alquilenoC1-6-C(O)-R', alquilenoC1-6-C(O)NH2, alquilenoC1-6-C(O)NH-R', o alquilenoC1-6-C(O)N(R')2; R7 y R8 son independientemente entre sí H, halogeno, CN, NO2, alquilo C1-6, O-alquiloC1-6, O-(alquilenoC1-6)0-1-R', alquenilo C2-6, R', alquenilenoC2-6-ariloC6-10, alquilenoC1-6-R', NH2, NH-R', NH-SO2H, NH-SO2-alquiloC1-6, NH-SO2-R', SO2-NH2, SO2-NHR', NH-C(O)-alquiloC1-6, NH-C(O)-R', C(O)N(alquiloC1-6)2, C(O)OH o C(O)O-alquiloC1-6; R9 es halogeno o alquilo C1-6; n es 0, 1, 2, 3 o 4; y L es O o O-alquilenoC1-6; donde R' es cicloalquilo C3-8, heterociclilo C5-10 o arilo C6-10; y R'' es cicloalquilo C3-8, heterociclilo C5-10, arilo C6-10, alquilo C1-6, alquilenoC1-6-R', alquilenoC1-6-O-alquiloC1-6, alquilenoC1-6-O-R' o alquilenoC1-6-NRxRy; y donde Rx y Ry son independientemente entre sí alquilo C1-6, heterociclilo C5-10, arilo C6-10, alquilenoC1-4-heterocicliloC5-10, alquilenoC1-4-arilo C6-10, alquilenoC1-4-NH-alquiloC1-6, alquilenoC1-4-N(alquiloC1-6)2, alquilenoC1-4-N(ariloC6-10)2, o alquilenoC1-4-N(heterocicliloC5-10)2; y donde en los restos R4, R5, R7 y R8 uno átomo de hidrogeno del grupo alquilo o alquileno puede estar opcionalmente sustituido con OH, OCH3, COOH, COOCH3, NH2, NHCH3, N(CH3)2, CONH2, CONHCH3 o CON(CH3)2 o un grupo alquilo o alquileno puede estar halogenado una o más veces; y/o sus sales farmacéuticamente aceptables y/o formas estereoisoméricas y/o derivados fisiologicamente funcionales.
ARP060103200A 2005-07-26 2006-07-25 Derivados de ciclohexilaminisoquinolona AR057082A1 (es)

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EP (1) EP1912949B1 (es)
JP (1) JP5049970B2 (es)
KR (1) KR101336678B1 (es)
CN (1) CN101228132B (es)
AR (1) AR057082A1 (es)
AT (1) ATE521595T1 (es)
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BRPI0613861B8 (pt) 2005-07-26 2021-05-25 Sanofi Aventis derivados de isoquinolona piperidinil-substituídos como inibidores de rho-cinase
RS52241B (en) 2005-07-26 2012-10-31 Sanofi CYCLOHEXYLAMINE ISOHINOLONE DERIVATIVES AS RHO-KINASE INHIBITORS
US7893088B2 (en) 2006-08-18 2011-02-22 N.V. Organon 6-substituted isoquinoline derivatives
US7906504B2 (en) * 2006-09-11 2011-03-15 N.V. Organon 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivatives
JP5405316B2 (ja) * 2006-12-27 2014-02-05 サノフイ シクロアルキルアミン置換イソキノリン誘導体
CN101616909B (zh) 2006-12-27 2013-09-11 塞诺菲-安万特股份有限公司 作为Rho-激酶抑制剂的被取代的异喹啉和异喹啉酮衍生物
WO2008077555A2 (en) 2006-12-27 2008-07-03 Sanofi-Aventis Substituted isoquinolines and their use as rho-kinase inhibitors
MX2009006517A (es) 2006-12-27 2009-06-26 Sanofi Aventis Nuevos derivados de isoquinolina e isoquinolinona sustituidos.
ATE490243T1 (de) 2006-12-27 2010-12-15 Sanofi Aventis Cycloalkylaminsubstituierte isochinolin- und isochinolinonderivate
ES2625266T3 (es) * 2006-12-27 2017-07-19 Sanofi Derivados de isoquinolona sustituidos con cicloalquilamina
TW200845988A (en) 2007-04-05 2008-12-01 Astrazeneca Ab New compounds and their uses 707
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