AR073314A1 - Derivados de indazol o de 4,5,6,7-tetrahidro-indazol - Google Patents

Derivados de indazol o de 4,5,6,7-tetrahidro-indazol

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Publication number
AR073314A1
AR073314A1 ARP090103661A ARP090103661A AR073314A1 AR 073314 A1 AR073314 A1 AR 073314A1 AR P090103661 A ARP090103661 A AR P090103661A AR P090103661 A ARP090103661 A AR P090103661A AR 073314 A1 AR073314 A1 AR 073314A1
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AR
Argentina
Prior art keywords
group
substituted
alkoxy
alkyl
hydroxy
Prior art date
Application number
ARP090103661A
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English (en)
Original Assignee
Hoffmann La Roche
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Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR073314A1 publication Critical patent/AR073314A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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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)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Estos compuestos son moduladores de FXR y pueden utilizarse como medicamentos. Reivindicacion 1: Compuestos de la formula (1) en la que R1 es un anillo elegido entre el grupo formado por fenilo, naftilo y heteroarilo, dicho anillo está sin sustituir o sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, halogeno, halogenoalquilo inferior, hidroxi, alcoxi inferior, halogenoalcoxi inferior y ciano; R2, R3, R4 y R5 con independencia entre sí se eligen entre el grupo formado por H, halogeno y alquilo inferior; R2' y R3' juntos y también R4' y R5' juntos se reemplazan por un doble enlace, o R2', R3', R4' y R5' son H; R6 se elige entre el grupo formado por H, metilo, etilo, hidroxi, metoxi, fluor, fluormetilo, difluormetilo y trifluormetilo; R7 se elige entre el grupo formado por alquilo inferior, cicloalquilo, cicloalquilalquilo inferior, alcoxialquilo inferior, fenilo sin sustituir o fenilo sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, halogeno, halogenoalquilo inferior, hidroxi, alcoxi inferior, halogenoalcoxi inferior y ciano; fenilalquilo inferior, en el que el fenilo está sin sustituir o sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, halogeno, halogenoalquilo inferior, hidroxi, alcoxi inferior, halogenoalcoxi inferior y ciano; heteroarilo sin sustituir o heteroarilo sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, halogeno, halogenoalquilo inferior, hidroxi, alcoxi inferior, halogenoalcoxi inferior y ciano; y heterociclilo; y R8 se elige entre el grupo formado por -C(O)-NH-R9, -CR11R12-OR10, -O-(CR11R12)n-R10; -CR11R12-SR10, -CR11R12-SO2-R10, -CR11R12-NR13-R10; -CH=CH-R10 y -(CH2)p-R10, en los que n es el numero 0 o 1, p es el numero 2, R9 se elige entre el grupo formado por alquilo inferior, cicloalquilo, cicloalquilalquilo inferior, cicloalquilo sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por hidroxi, carboxilo, tetrazolilo, carboxialquilo inferior, (alcoxi inferior)-carbonilo, alcoxicarbonilalquilo inferior, carboxilalcoxi inferior y alcoxicarbonilalcoxi inferior, heterociclilo, fenilo sin sustituir y fenilo sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, halogeno, halogenoalquilo inferior, hidroxi, alcoxi inferior, halogenoalcoxi inferior, carboxilo, tetrazolilo, (alcoxi inferior)carbonilo, alcoxicarbonilalquilo inferior, carboxialquilo inferior, carboxialcoxi inferior, alcoxicarbonilalcoxi inferior, ciano y cicloalquiloxi, en los que el grupo cicloalquilo esta sustituido por carboxilo, (alcoxi inferior)-carbonilo o tetrazolilo; R10 se elige entre el grupo formado por alquilo inferior, cicloalquilo, cicloalquilalquilo inferior, cicloalquilo sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por hidroxi, carboxilo, tetrazolilo, carboxialquilo inferior, (alcoxi inferior)-carbonilo, alcoxicarbonilalquilo inferior, carboxilalcoxi inferior y alcoxicarbonilalcoxi inferior, heterociclilo, piridilo sin sustituir y piridilo sustituido por carboxilo, (alcoxi inferior)-carbonilo o tetrazolilo, fenilo sin sustituir y fenilo sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, halogeno, halogenoalquilo inferior, hidroxi, alcoxi inferior, halogenoalcoxi inferior, carboxilo, tetrazolilo, (alcoxi inferior)carbonilo, alcoxicarbonilalquilo inferior, carboxialquilo inferior, carboxilalcoxi inferior, alcoxicarbonilalcoxi inferior, ciano y cicloalquiloxi, en los que el grupo cicloalquilo esta sustituido por carboxilo, (alcoxi inferior)-carbonilo o tetrazolilo; fenilalquilo inferior, en el que el fenilo está sin sustituir o sustituido por 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, halogeno, halogenoalquilo inferior, hidroxi, alcoxi inferior, halogenoalcoxi inferior, carboxilo, tetrazolilo, (alcoxi inferior)carbonilo, alcoxicarbonilalquilo inferior, carboxialquilo inferior, carboxilalcoxi inferior, alcoxicarbonilalcoxi inferior, ciano y cicloalquiloxi, en los que el grupo cicloalquilo esta sustituido por carboxilo, (alcoxi inferior)-carbonilo o tetrazolilo; R11 y R12 se eligen con independencia entre el grupo formado por H, alquilo inferior y halogenoalquilo inferior, o R11 y R12 junto con el átomo de C al que están unidos forman un anillo cicloalquilo o alcoxicicloalquilo; y R13 se elige entre el grupo formado por H, alquilo inferior y halogenoalquilo inferior; o las sales farmacéuticamente aceptables de los mismos.
ARP090103661A 2008-09-25 2009-09-23 Derivados de indazol o de 4,5,6,7-tetrahidro-indazol AR073314A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08165145 2008-09-25

Publications (1)

Publication Number Publication Date
AR073314A1 true AR073314A1 (es) 2010-10-28

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US (1) US8008505B2 (es)
EP (1) EP2344459B1 (es)
JP (1) JP5425911B2 (es)
KR (1) KR101372104B1 (es)
CN (1) CN102164899B (es)
AR (1) AR073314A1 (es)
AU (1) AU2009296048A1 (es)
BR (1) BRPI0919057A2 (es)
CA (1) CA2735886A1 (es)
ES (1) ES2446593T3 (es)
IL (1) IL211566A0 (es)
MX (1) MX2011002794A (es)
TW (1) TW201020235A (es)
WO (1) WO2010034649A1 (es)

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TW201020235A (en) 2010-06-01
AU2009296048A1 (en) 2010-04-01
IL211566A0 (en) 2011-05-31
JP2012503617A (ja) 2012-02-09
CN102164899A (zh) 2011-08-24
US8008505B2 (en) 2011-08-30
KR20110059895A (ko) 2011-06-07
EP2344459A1 (en) 2011-07-20
CA2735886A1 (en) 2010-04-01
MX2011002794A (es) 2011-04-05
WO2010034649A1 (en) 2010-04-01
KR101372104B1 (ko) 2014-03-07
JP5425911B2 (ja) 2014-02-26
ES2446593T3 (es) 2014-03-10
EP2344459B1 (en) 2013-12-25
CN102164899B (zh) 2014-11-26
BRPI0919057A2 (pt) 2018-01-09
US20100076027A1 (en) 2010-03-25

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