AR059886A1 - Derivados de amidas como inhibidores de renina - Google Patents

Derivados de amidas como inhibidores de renina

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Publication number
AR059886A1
AR059886A1 ARP070100947A ARP070100947A AR059886A1 AR 059886 A1 AR059886 A1 AR 059886A1 AR P070100947 A ARP070100947 A AR P070100947A AR P070100947 A ARP070100947 A AR P070100947A AR 059886 A1 AR059886 A1 AR 059886A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
alkoxy
ch2ch2
ch2ch2ch2
Prior art date
Application number
ARP070100947A
Other languages
English (en)
Original Assignee
Actelion Pharmaceuticals Ltd
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
Application filed by Actelion Pharmaceuticals Ltd filed Critical Actelion Pharmaceuticals Ltd
Publication of AR059886A1 publication Critical patent/AR059886A1/es

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    • CCHEMISTRY; METALLURGY
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/42Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of mineralocorticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicacion 1: Un compuesto de la Formula (1) donde X representa CH, N, o N+-O-; W representa un fenilo para-sustituido, un piridilo para-sustituido, o un tiazolilo; V representa -CH2CH2CH2-, -CH2CH2-A-, -CH2-A-CH2-, -A-CH2CH2-, -CH2CH2CH2CH2-, - A-CH2CH2CH2-, -CH2-A-CH2CH2-, -CH2CH2-A-CH2-, -CH2CH2CH2-A-, -A-CH2CH2-B-, CH2CH2CH2CH2CH2-, -A-CH2CH2CH2CH2-, -CH2-A-CH2CH2CH2-, -CH2CH2-A-CH2CH2, -CH2CH2CH2-A-CH2-, -CH2CH2CH2CH2-A-, -A-CH2CH2CH2-B-, CH2-A-CH2CH2-B-, -A-CH2CH2-B-CH2-, -A-CH2CH2CH2- B-CH2-, -CH2-A-CH2CH2CH2-B-, o -O-CH2-Q-, donde Q está ligado al grupo U de Formula 1, o V representa un pirrodinilo de la Formula (2); U representa arilo no sustituido; arilo mono-, di-, tri- o tetra-sustituido, donde los sustituyentes se seleccionan independientemente del grupo formado por alquilo-C1-7, -CF3, halogeno, e hidroxi-alquilo-C1-7; o heteroarilo de cinco miembros con dos heteroátomos seleccionados independientemente entre nitrogeno, oxígeno y azufre, donde dicho radical heteroarilo está opcionalmente mono-, di- o tri-sustituido, donde los sustituyentes se seleccionan independientemente del grupo formado por alquilo-C1-7, alcoxi-C1-7, -CF3, -OCF3, y halogeno; Q representa un heteroarilo de cinco miembros con dos o tres heteroátomos seleccionados independientemente entre O y N; L representa -CH2-CH2-, -CH2-CH(R6)-CH2-, -CH2-N(R7)-CH2-, -CH2-O-CH2-, o -CH2-S-CH2-; A y B representan independientemente uno del otro -O- o -S-; R1 representa alquilo-C1-7 o cicloalquilo; R2 representa halogeno o alquilo-C1-7; R3 representa hidrogeno, halogeno, alquilo-C1-7, alcoxi-C1-7, o -CF3; R4 representa hidrogeno; alquilC1-7-O-(CH2)0-4-CH2-; CF3-O-(CH2)0-4-CH2-; R'2N-(CH2)0-4-CH2-, donde R' se selecciona independientemente del grupo formado por hidrogeno, alquilo-C1-7 (opcionalmente sustituido con uno a tres fluor), ciclopropilo (opcionalmente sustituido con uno a tres fluor), ciclopropil-alquilo-C1-7 (opcionalmente sustituido con uno a tres fluor), y -C(=O)-R'' donde R'' es alquiloC1-4, alcoxiC1-4, -CF3, -CH2-CF3, o ciclopropilo; o R13-C(=O)-(O)0-1-(CH2)0-4, donde R13 es alquiloC1-4, alcoxiC1-4, o ciclopropilo; donde R' y R'' preferiblemente no representan hidrogeno al mismo tiempo; R5 representa hidroxi, alcoxi-C1-7, hidroxi-alquilo-C1-7, dihidroxi-alquilo-C1-7, dihidroxi-alquilo-C1-7, alcoxi-C1-7-alquilo-C1-7, alcoxi-C1-7-alcoxi-C1-7-alquilo-C1-7, hidroxi-alcoxi-C1-7-alquilo-C1-7, carbamoil-alcoxi-C1-7, o alquilC1-7-carboniloxi; R6 representa -H, -CH2OR9, -CH2NR8R9, -CH2NR8COR9, -CH2NR8SO2R9, -CO2R9, -CH2OCONR8R9, -CONR8R9, -CH2NR8CONR8'R9, -CH2SO2NR8R9, -CH2SR9, -CH2SOR9, o -CH2SO2R9; R7 representa -R9, -COR9, -COOR11, -CONR8R9, -C(NR8)NR8'R9, -CSNR8R9, CSNR8R9, -SO2R9, o - SO2NR8R9; o R7 representa un radical de la Formulas (3) donde T representa -CH2-, -NH- o -O-, r es un numero entero entre 1 y 6 y s es un numero entero entre 1 y 4; R8 y R8' representan independientemente hidrogeno, alquilo-C1-7, alquenilo.C2-7, cicloalquilo, o cicloalquil-alquilo-C1-7, donde alquilo-C1-7, cicloalquilo, y cicloalquil-alquilo-C1-7 pueden estar sustituidos con uno, dos, o tres halogenos; R9 representa hidrogeno, alquilo-C1-7, cicloalquilo, o cicloalquil-alquilo-C1-7, donde alquilo-C1-7, cicloalquilo, y cicloalquil-alquilo-C1-7 pueden estar mono-, di- o tri-sustituidos, donde los sustituyentes se seleccionan independientemente del grupo formado por halogeno, hidroxi, -OCOR12, -COOR12, alcoxi-C1-7, ciano, SO2R12, - CONR12R12', morfolin-4-il-co-, ((4-alquilC1-7)piperazin-1-il)-CO-, -NHC(NH)NH2, -NR10R10' y alquilo-C1-7, con la condicion de que un átomo de carbono esté ligado a lo sumo a un heteroátomo en caso de que este átomo de carbono esté sp3-hibridizado; R10 y R10' representan independientemente hidrogeno, alquilo-C1-7, cicloalquilo, cicloalquil-alquilo-C1-7, hidroxi, alquilo-C1-7, -COOR8, o -CONH2; R11 representa halogeno, alquilo-C1-7, alcoxi-C1-7, -CF3, o hidrogeno; R12 y R12' representan independientemente hidrogeno, alquilo-C1-7, alquenilo-C2-7, cicloalquilo, o cicloalquil-alquilo-C1-7, donde alquilo-C1-7, cicloalquilo, y cicloalquil-alquilo-C1-7 pueden estar sustituidos con uno, dos, o tres halogenos; n representa el numero entero 0 o 1; y m representa el numero entero 0 o 1, con la condicion de que m representa el numero entero 1 si n representa el numero entero 1; y a sales de los mismos. También comprende aspectos relacionados que incluyen procesos para la preparacion de los compuestos, composiciones farmacéuticas que contienen uno o más de dichos compuestos y especialmente su uso como inhibidores de renina.
ARP070100947A 2006-03-08 2007-03-07 Derivados de amidas como inhibidores de renina AR059886A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IB2006050724 2006-03-08

Publications (1)

Publication Number Publication Date
AR059886A1 true AR059886A1 (es) 2008-05-07

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ID=38475245

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070100947A AR059886A1 (es) 2006-03-08 2007-03-07 Derivados de amidas como inhibidores de renina

Country Status (18)

Country Link
US (1) US20090062342A1 (es)
EP (1) EP1994026A2 (es)
JP (1) JP2009529033A (es)
KR (1) KR20090008211A (es)
CN (1) CN101395149A (es)
AR (1) AR059886A1 (es)
AU (1) AU2007224368A1 (es)
BR (1) BRPI0708567A2 (es)
CA (1) CA2642436A1 (es)
CL (1) CL2007000595A1 (es)
IL (1) IL193885A0 (es)
MA (1) MA30296B1 (es)
MX (1) MX2008011340A (es)
NO (1) NO20084186L (es)
NZ (1) NZ571595A (es)
TW (1) TW200800897A (es)
WO (1) WO2007102127A2 (es)
ZA (1) ZA200808540B (es)

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DE602005020314D1 (de) * 2004-08-25 2010-05-12 Actelion Pharmaceuticals Ltd Bicyclononen-derivate als renin-inhibitoren
GEP20115206B (en) * 2005-05-27 2011-04-26 Actelion Pharmaceuticals Ltd Novel piperidine carboxylic acid amide derivatives
EP1981847A1 (en) * 2006-02-02 2008-10-22 Actelion Pharmaceuticals Ltd. Secondary amines as renin inhibitors
US8129538B1 (en) 2007-03-28 2012-03-06 Takeda Pharmaceutical Company Limited Renin inhibitors
EP2162436A4 (en) 2007-05-24 2010-08-04 Merck Frosst Canada Ltd NEW CASE OF RENININHIBITORS
AU2008288648A1 (en) 2007-08-20 2009-02-26 Merck Frosst Canada Ltd. Renin inhibitors
EP2229363A4 (en) * 2007-12-04 2010-12-15 Merck Frosst Canada Ltd Renin Inhibitors
CA2722734C (en) 2008-05-05 2013-11-05 Merck Frosst Canada Ltd. 3,4-substituted piperidine derivatives as renin inhibitors
US20120190701A1 (en) * 2009-08-18 2012-07-26 Merck Sharp & Dohme Corp. Renin inhibitors
EP2832724A4 (en) * 2012-03-29 2015-09-23 Toray Industries NIPETIC ACID DERIVATIVE AND ITS USE FOR MEDICAL PURPOSES
WO2017082393A1 (ja) * 2015-11-12 2017-05-18 学校法人 聖マリアンナ医科大学 緑内障予防治療剤
JP2023545399A (ja) 2020-10-01 2023-10-30 バイエル アクチェンゲゼルシャフト ベンズアルデヒドオキシムおよびその製造方法

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ZA200808419B (en) * 2006-03-03 2009-12-30 Actelion Pharmaceuticals Ltd Primary amines as renin inhibitors

Also Published As

Publication number Publication date
NO20084186L (no) 2008-10-07
NZ571595A (en) 2010-06-25
US20090062342A1 (en) 2009-03-05
CL2007000595A1 (es) 2008-01-04
BRPI0708567A2 (pt) 2011-05-31
TW200800897A (en) 2008-01-01
IL193885A0 (en) 2009-09-22
KR20090008211A (ko) 2009-01-21
MX2008011340A (es) 2008-09-12
JP2009529033A (ja) 2009-08-13
WO2007102127A3 (en) 2008-04-03
CA2642436A1 (en) 2007-09-13
MA30296B1 (fr) 2009-03-02
EP1994026A2 (en) 2008-11-26
ZA200808540B (en) 2009-12-30
CN101395149A (zh) 2009-03-25
AU2007224368A1 (en) 2007-09-13
WO2007102127A2 (en) 2007-09-13

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