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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    • CCHEMISTRY; METALLURGY
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • AHUMAN NECESSITIES
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    • A61P13/08Drugs for disorders of the urinary system of the prostate
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    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06Antiabortive agents; Labour repressants
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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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    • C07ORGANIC CHEMISTRY
    • 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)
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  • General Health & Medical Sciences (AREA)
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  • Cardiology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
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  • Pulmonology (AREA)
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  • Urology & Nephrology (AREA)
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  • Hospice & Palliative Care (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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US (2) US8609691B2 (es)
EP (1) EP1912949B1 (es)
JP (1) JP5049970B2 (es)
KR (1) KR101336678B1 (es)
CN (1) CN101228132B (es)
AR (1) AR057082A1 (es)
AT (1) ATE521595T1 (es)
AU (1) AU2006274246B2 (es)
BR (1) BRPI0614063A2 (es)
CA (1) CA2615663C (es)
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MX (1) MX2008000956A (es)
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SI1899322T1 (sl) 2005-06-28 2010-01-29 Sanofi Aventis Izokinolinski derivati kot inhibitorji Rho-kinaze
AU2006274245B2 (en) 2005-07-26 2011-11-24 Sanofi-Aventis Piperidinyl-substituted isoquinolone derivatives as Rho-kinase inhibitors
CN101228132B (zh) 2005-07-26 2012-10-10 塞诺菲-安万特股份有限公司 作为Rho-激酶抑制剂的环己基胺异喹啉酮衍生物
US7893088B2 (en) 2006-08-18 2011-02-22 N.V. Organon 6-substituted isoquinoline derivatives
CA2663193A1 (en) * 2006-09-11 2008-03-20 N.V. Organon 2-(1-oxo-1h-isoquinolin-2-yl)acetamide derivatives
JP5313919B2 (ja) 2006-12-27 2013-10-09 サノフイ 新規な置換イソキノリン及びイソキノリノン誘導体
CN101611012B (zh) * 2006-12-27 2012-11-14 塞诺菲-安万特股份有限公司 环烷基胺取代的异喹啉衍生物
MX2009006517A (es) 2006-12-27 2009-06-26 Sanofi Aventis Nuevos derivados de isoquinolina e isoquinolinona sustituidos.
BRPI0722064A2 (pt) 2006-12-27 2014-04-01 Sanofi Aventis Derivados de isoquinolona substituídos por cicloalquilamina
MY154767A (en) 2006-12-27 2015-07-15 Sanofi Aventis Cycloalkyamine substituted isoquinoline and isoquinolinone derivatives
CA2673916C (en) 2006-12-27 2015-02-17 Sanofi-Aventis Substituted isoquinolone and isoquinolinone derivatives as inhibitors of rho-kinase
CL2008000973A1 (es) 2007-04-05 2009-01-02 Astrazeneca Ab Compuestos derivados de 1-oxo-isoquinolina; procedimiento de preparación; composición farmacéutica; y su uso en el tratamiento de enfermedades pulmonares obstructvas crónicas (epoc) y asma.
AU2008317353B2 (en) * 2007-10-24 2014-08-07 Merck Sharp & Dohme Llc Heterocycle phenyl amide T-type calcium channel antagonists
US8524737B2 (en) * 2008-06-24 2013-09-03 Sanofi Bi- and polycyclic substituted isoquinoline and isoquinolinone derivatives
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